Aralen

chloroquine phosphate

Dosage Form: Tablets, USP

For Malaria and Extraintestinal Amebiasis

Aralen Description

Aralen, chloroquine phosphate, USP, is a 4-aminoquinoline compound for oral administration. It is a white, odorless, bitter tasting, crystalline substance, freely soluble in water.

Aralen is an antimalarial and amebicidal drug.

Chemically, it is 7-chloro-4-[[4-(diethylamino)-1-methylbutyl]amino]quinoline phosphate (1:2) and has the following structural formula:

Each tablet contains 500 mg of chloroquine phosphate USP, equivalent to 300 mg chloroquine base.

Inactive Ingredients: Carnauba Wax, Colloidal Silicon Dioxide, Dibasic Calcium Phosphate, Hydroxypropyl Methylcellulose, Magnesium Stearate, Microcrystalline Cellulose, Polyethylene Glycol, Polysorbate 80, Pregelatinized Starch, Sodium Starch Glycolate, Stearic Acid, Titanium Dioxide.

Aralen - Clinical Pharmacology

Chloroquine is rapidly and almost completely absorbed from the gastrointestinal tract, and only a small proportion of the administered dose is found in the stools. Approximately 55% of the drug in the plasma is bound to nondiffusible plasma constituents. Excretion of chloroquine is quite slow, but is increased by acidification of the urine. Chloroquine is deposited in the tissues in considerable amounts. In animals, from 200 to 700 times the plasma concentration may be found in the liver, spleen, kidney, and lung; leukocytes also concentrate the drug. The brain and spinal cord, in contrast, contain only 10 to 30 times the amount present in plasma.

Chloroquine undergoes appreciable degradation in the body. The main metabolite is desethylchloroquine, which accounts for one fourth of the total material appearing in the urine; bisdesethylchloroquine, a carboxylic acid derivative, and other metabolic products as yet uncharacterized are found in small amounts. Slightly more than half of the urinary drug products can be accounted for as unchanged chloroquine.

Microbiology

Mechanism of Action

Chloroquine is an antimalarial agent. While the drug can inhibit certain enzymes, its effect is believed to result, at least in part, from its interaction with DNA. However, the mechanism of plasmodicidal action of chloroquine is not completely certain.

Activity in vitro and in vivo

Chloroquine is active against the erythrocytic forms of Plasmodium vivax. Plasmodium malariae, and susceptible strains of Plasmodium falciparum (but not the gametocytes of P. falciparum). It is not effective against exoerythrocytic forms of the parasite.

In vitro studies with trophozoites of Entamoeba histolytica have demonstrated that chloroquine also possesses amebicidal activity comparable to that of emetine.

Drug Resistance

Resistance of Plasmodium falciparum to chloroquine is widespread and cases of Plasmodium vivax resistance have been reported.

Indications and Usage for Aralen

Aralen is indicated for the suppressive treatment and for acute attacks of malaria due to P. vivax, P.malariae, P. ovale, and susceptible strains of P. falciparum. The drug is also indicated for the treatment of extraintestinal amebiasis.

Aralen does not prevent relapses in patients with vivax or malariae malaria because it is not effective against exoerythrocytic forms of the parasite, nor will it prevent vivax or malariae infection when administered as a prophylactic. It is highly effective as a suppressive agent in patients with vivax or malariae malaria, in terminating acute attacks, and significantly lengthening the interval between treatment and relapse. In patients with falciparum malaria it abolishes the acute attack and effects complete cure of the infection, unless due to a resistant strain of P. falciparum.

Contraindications

Use of this drug is contraindicated in the presence of retinal or visual field changes either attributable to 4-aminoquinoline compounds or to any other etiology, and in patients with known hypersensitivity to 4-aminoquinoline compounds. However, in the treatment of acute attacks of malaria caused by susceptible strains of plasmodia, the physician may elect to use this drug after carefully weighing the possible benefits and risks to the patient.

Warnings

It has been found that certain strains of P. falciparum have become resistant to 4-aminoquinoline compounds (including chloroquine and hydroxychloroquine). Chloroquine resistance is widespread and, at present, is particularly prominent in various parts of the world including sub-Saharan Africa, Southeast Asia, the Indian subcontinent, and over large portions of South America, including the Amazon basin1.

Before using chloroquine for prophylaxis, it should be ascertained whether chloroquine is appropriate for use in the region to be visited by the traveler. Chloroquine should not be used for treatment of P. falciparum infections acquired in areas of chloroquine resistance or malaria occurring in patients where chloroquine prophylaxis has failed.

Patients infected with a resistant strain of plasmodia as shown by the fact that normally adequate doses have failed to prevent or cure clinical malaria or parasitemia should be treated with another form of antimalarial therapy.

Irreversible retinal damage has been observed in some patients who had received long-term or high-dosage 4-aminoquinoline therapy. Retinopathy has been reported to be dose related.

When prolonged therapy with any antimalarial compound is contemplated, initial (base line) and periodic ophthalmologic examinations (including visual acuity, expert slit-lamp, funduscopic, and visual field tests) should be performed.

If there is any indication (past or present) of abnormality in the visual acuity, visual field, or retinal macular areas (such as pigmentary changes, loss of foveal reflex), or any visual symptoms (such as light flashes and streaks) which are not fully explainable by difficulties of accommodation or corneal opacities, the drug should be discontinued immediately and the patient closely observed for possible progression. Retinal changes (and visual disturbances) may progress even after cessation of therapy.

All patients on long-term therapy with this preparation should be questioned and examined periodically, including testing knee and ankle reflexes, to detect any evidence of muscular weakness. If weakness occurs, discontinue the drug.

A number of fatalities have been reported following the accidental ingestion of chloroquine, sometimes in relatively small doses (0.75 g or 1 g chloroquine phosphate in one 3-year-old child). Patients should be strongly warned to keep this drug out of the reach of children because they are especially sensitive to the 4-aminoquinoline compounds.

Use of Aralen in patients with psoriasis may precipitate a severe attack of psoriasis. When used in patients with porphyria the condition may be exacerbated. The drug should not be used in these conditions unless in the judgment of the physician the benefit to the patient outweighs the potential risks.

Usage in Pregnancy

Radioactively tagged chloroquine administered intravenously to pregnant pigmented CBA mice passed rapidly across the placenta and accumulated selectively in the melanin structures of the fetal eyes. It was retained in the ocular tissues for five months after the drug had been eliminated from the rest of the body2. There are no adequate and well-controlled studies evaluating the safety and efficacy of chloroquine in pregnant women. Usage of chloroquine during pregnancy should be avoided except in the suppression or treatment of malaria when in the judgment of the physician the benefit outweighs the potential risk to the fetus.

Precautions

Hematological Effects/Laboratory Tests

Complete blood cell counts should be made periodically if patients are given prolonged therapy. If any severe blood disorder appears which is not attributable to the disease under treatment, discontinuance of the drug should be considered.

The drug should be administered with caution to patients having G-6-PD (glucose-6 phosphate dehydrogenase) deficiency.

Auditory Effects

In patients with preexisting auditory damage, chloroquine should be administered with caution. In case of any defects in hearing, chloroquine should be immediately discontinued, and the patient closely observed (see ADVERSE REACTIONS).

Hepatic Effects

Since this drug is known to concentrate in the liver, it should be used with caution in patients with hepatic disease or alcoholism or in conjunction with known hepatotoxic drugs.

Central Nervous System Effects

Patients with history of epilepsy should be advised about the risk of chloroquine provoking seizures.

Drug Interactions

Antacids and kaolin: Antacids and kaolin can reduce absorption of chloroquine; an interval of at least 4 hours between intake of these agents and chloroquine should be observed.

Cimetidine: Cimetidine can inhibit the metabolism of chloroquine, increasing its plasma level. Concomitant use of cimetidine should be avoided.

Ampicillin: In a study of healthy volunteers, chloroquine significantly reduced the bioavailability of ampicillin. An interval of at least two hours between intake of this agent and chloroquine should be observed.

Cyclosporine: After introduction of chloroquine (oral form), a sudden increase in serum cyclosporine level has been reported. Therefore, close monitoring of serum cyclosporine level is recommended and, if necessary, chloroquine should be discontinued.

Mefloquine: Co-administration of chloroquine and mefloquine may increase the risk of convulsions.

The blood concentrations of chloroquine and desethylchloroquine (the major metabolite of chloroquine, which also has antimalarial properties) were negatively associated with log antibody titers. Chloroquine taken in the dose recommended for malaria prophylaxis can reduce the antibody response to primary immunization with intradermal human diploid-cell rabies vaccine.

Pregnancy

See WARNINGS, Usage in Pregnancy.

Nursing Mothers

Because of the potential for serious adverse reactions in nursing infants from chloroquine, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the potential clinical benefit of the drug to the mother.

The excretion of chloroquine and the major metabolite, desethylchloroquine, in breast milk was investigated in eleven lactating mothers following a single oral dose of chloroquine (600 mg base). The maximum daily dose of the drug that the infant can receive from breastfeeding was about 0.7% of the maternal start dose of the drug in malaria chemotherapy. Separate chemoprophylaxis for the infant is required. See DOSAGE AND ADMINISTRATION.

Pediatric Use

See WARNINGS and DOSAGE AND ADMINISTRATION.

Geriatric Use

Clinical studies of Aralen did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. However, this drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection and it may be useful to monitor renal function.

Adverse Reactions

Special Senses: Ocular: Irreversible retinal damage in patients receiving long-term or high-dosage 4-aminoquinoline therapy; visual disturbances (blurring of vision and difficulty of focusing or accommodation); nyctalopia; scotomatous vision with field defects of paracentral, pericentral ring types, and typically temporal scotomas, e.g., difficulty in reading with words tending to disappear, seeing half an object, misty vision, and fog before the eyes. Reversible corneal opacities have also been reported.

Auditory: Nerve type deafness; tinnitus, reduced hearing in patients with preexisting auditory damage.

Musculoskeletal system: Skeletal muscle myopathy or neuromyopathy leading to progressive weakness and atrophy of proximal muscle groups, which may be associated with mild sensory changes, depression of tendon reflexes and abnormal nerve conduction, have been noted.

Gastrointestinal system: Hepatitis, increased liver enzymes, anorexia, nausea, vomiting, diarrhea, abdominal cramps.

Skin and appendages: Rare reports of erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, exfoliative dermatitis and similar desquamation-type events. Pleomorphic skin eruptions, skin and mucosal pigmentary changes; lichen planus-like eruptions, pruritus, urticaria, anaphylactic/anaphylactoid reaction including angioedema, photosensitivity and hair loss and bleaching of hair pigment.

Hematologic system: Rarely, pancytopenia, aplastic anemia, reversible agranulocytosis, thrombocytopenia and neutropenia.

Nervous system: Convulsive seizures, mild and transient headache, polyneuritis. Neuropsychiatric changes including psychosis, delirium, anxiety, agitation, insomnia, confusion, hallucinations, personality changes, and depression.

Cardiovascular system: Rarely, hypotension, electrocardiographic change (particularly, inversion or depression of the T-wave with widening of the QRS complex), and cardiomyopathy.

Overdosage

Symptoms

Chloroquine is very rapidly and completely absorbed after ingestion. Toxic doses of chloroquine can be fatal. As little as 1 g may be fatal in children. Toxic symptoms can occur within minutes. These consist of headache, drowsiness, visual disturbances, nausea and vomiting, cardiovascular collapse, shock and convulsions followed by sudden and early respiratory and cardiac arrest. Hypokalemia has been observed with arrhythmias in cases of intoxication. The electrocardiogram may reveal atrial standstill, nodal rhythm, prolonged intraventricular conduction time, and progressive bradycardia leading to ventricular fibrillation and/or arrest.

Treatment

Treatment is symptomatic and must be prompt with immediate evacuation of the stomach by emesis (at home, before transportation to the hospital) or gastric lavage until the stomach is completely emptied. If finely powdered, activated charcoal is introduced by stomach tube, after lavage, and within 30 minutes after ingestion of the antimalarial, it may inhibit further intestinal absorption of the drug. To be effective, the dose of activated charcoal should be at least five times the estimated dose of chloroquine ingested.

Convulsions, if present, should be controlled before attempting gastric lavage. If due to cerebral stimulation, cautious administration of an ultra short-acting barbiturate may be tried but, if due to anoxia, it should be corrected by oxygen administration and artificial respiration. Monitor ECG. In shock with hypotension, a potent vasopressor should be administered. Replace fluids and electrolytes as needed. Cardiac compressing or pacing may be indicated to sustain the circulation. Because of the importance of supporting respiration, tracheal intubation or tracheostomy, followed by gastric lavage, may also be necessary. Peritoneal dialysis and exchange transfusions have also been suggested to reduce the level of the drug in the blood.

Intervention options can involve: diazepam for life-threatening symptoms, seizures and sedation, epinephrine for treatment of vasodilation and myocardial depression, potassium replacement with close monitoring of serum potassium levels.

A patient who survives the acute phase and is asymptomatic should be closely observed for at least six hours. Fluids may be forced, and sufficient ammonium chloride (8 g daily in divided doses for adults) may be administered for a few days to acidify the urine to help promote urinary excretion in cases of both overdosage or sensitivity.

Aralen Dosage and Administration

The dosage of chloroquine phosphate is often expressed in terms of equivalent chloroquine base. Each 500 mg tablet of Aralen contains the equivalent of 300 mg chloroquine base. In infants and children the dosage is preferably calculated by body weight.

Malaria

Suppression — Adult Dose: 500 mg (= 300 mg base) on exactly the same day of each week.

Pediatric Dose: The weekly suppressive dosage is 5 mg calculated as base, per kg of body weight, but should not exceed the adult dose regardless of weight.

If circumstances permit, suppressive therapy should begin two weeks prior to exposure. However, failing this in adults, an initial double (loading) dose of 1 g (= 600 mg base), or in children 10 mg base/kg may be taken in two divided doses, six hours apart. The suppressive therapy should be continued for eight weeks after leaving the endemic area.

For Treatment of Acute Attack

Adults: An initial dose of 1 g (= 600 mg base) followed by an additional 500 mg (= 300 mg base) after six to eight hours and a single dose of 500 mg (= 300 mg base) on each of two consecutive days. This represents a total dose of 2.5 g chloroquine phosphate or 1.5 g base in three days.

The dosage for adults of low body weight and for infants and children should be determined as follows:

First dose: 10 mg base per kg (but not exceeding a single dose of 600 mg base).

Second dose: (6 hours after first dose) 5 mg base per kg (but not exceeding a single dose of 300 mg base).

Third dose: (24 hours after first dose) 5 mg base per kg.

Fourth dose: (36 hours after first dose) 5 mg base per kg.

For radical cure of vivax and malariae malaria concomitant therapy with an 8-aminoquinoline compound is necessary.

Extraintestinal Amebiasis

Adults, 1 g (600 mg base) daily for two days, followed by 500 mg (300 mg base) daily for at least two to three weeks. Treatment is usually combined with an effective intestinal amebicide.

Geriatric Use

See PRECAUTIONS, Geriatric Use.

How is Aralen Supplied

Tablets containing 500 mg chloroquine phosphate USP, equivalent to 300 mg of chloroquine base, bottles of 25 (NDC 0024-0084-01).

White, film-coated convex, discoid tablet, 1/2 inch in diameter with an uncoated core, printed in black ink with a stylized "W" on one side and an "A77" on the other side.

Dispense in tight, light-resistant container as defined in the USP/NF.

Store at 25° C (77° F); excursions permitted to 15° – 30° C (59° – 86° F) [see USP Controlled Room Temperature]

REFERENCES

1. Malaria Deaths Following Inappropriate Malaria Chemoprophylaxis – United States, 2001. MMWR Weekly, 2001; 50(28): 597–599.


2. Ullberg S, Lindquist N G, Sjostrand S E: Accumulation of chorioretinotoxic drugs in the foetal eye. Nature 1970; 227: 1257.

Manufactured for:

sanofi-aventis U.S. LLC

Bridgewater, NJ 08807

Revised September 2008

© 2008 sanofi-aventis U.S. LLC

Aralen  chloroquine phosphate  tablet, film coated

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 0024-0084 Route of Administration ORAL DEA Schedule

INGREDIENTS Name (Active Moiety) Type Strength chloroquine phosphate (chloroquine) Active 500 MILLIGRAM  In 1 TABLET carnauba wax Inactive   colloidal silicon dioxide Inactive   dibasic calcium phosphate Inactive   hydroxypropyl methylcellulose Inactive   magnesium stearate Inactive   microcrystalline cellulose Inactive   polyethylene glycol Inactive   polysorbate 80 Inactive   pregelatinized starch Inactive   sodium starch glycolate Inactive   stearic acid Inactive   titanium dioxide Inactive

Product Characteristics Color white Score no score Shape ROUND Size 13mm Flavor Imprint Code W;A77 Contains          Coating true Symbol true

Packaging # NDC Package Description Multilevel Packaging 1 0024-0084-01 25 TABLET In 1 BOTTLE, PLASTIC None

Revised: 12/2008sanofi-aventis U.S. LLC

More Aralen resources

• Aralen Side Effects (in more detail)
• Aralen Dosage
• Aralen Use in Pregnancy & Breastfeeding
• Aralen Drug Interactions
• Aralen Support Group
• 0 Reviews for Aralen - Add your own review/rating

Compare Aralen with other medications

• Amebiasis
• Malaria
• Malaria Prevention
• Sarcoidosis

Halog Ointment, USP

Dosage Form: ointment


(Halcinonide Ointment, USP) 0.1%

FOR TOPICAL USE ONLY.

NOT FOR OPHTHALMIC, ORAL, OR INTRAVAGINAL USE.

Rx only

Halog Ointment, USP Description

The topical corticosteroids constitute a class of primarily synthetic steroids used as anti-inflammatory and antipruritic agents. The steroids in this class include halcinonide. Halcinonide is designated chemically as 21-Chloro-9-fluoro-11β, 16α, 17-trihydroxypregn-4-ene-3,20- dione cyclic 16,17-acetal with acetone. Graphic formula:

C24H32ClFO5, MW 454.96, CAS-3093-35-4

Each gram of 0.1% HALOG OINTMENT (Halcinonide Ointment, USP) contains 1 mg halcinonide in Plastibase® (Plasticized Hydrocarbon Gel), a mineral oil and polyethylene gel base, polyethylene glycol 300, polyethylene glycol 400, polyethylene glycol 1450, and polyethylene glycol 6000 distearate with butylated hydroxytoluene as an antioxidant.

Halog Ointment, USP - Clinical Pharmacology

Topical corticosteroids share anti-inflammatory, antipruritic and vasoconstrictive actions.

The mechanism of anti-inflammatory activity of the topical corticosteroids is unclear. Various laboratory methods, including vasoconstrictor assays, are used to compare and predict potencies and/or clinical efficacies of the topical corticosteroids. There is some evidence to suggest that a recognizable correlation exists between vasoconstrictor potency and therapeutic efficacy in man.

Pharmacokinetics

The extent of percutaneous absorption of topical corticosteroids is determined by many factors including the vehicle, the integrity of the epidermal barrier, and the use of occlusive dressings.

Topical corticosteroids can be absorbed from normal intact skin. Inflammation and/or other disease processes in the skin increase percutaneous absorption. Occlusive dressings substantially increase the percutaneous absorption of topical corticosteroids. Thus, occlusive dressings may be a valuable therapeutic adjunct for treatment of resistant dermatoses (see DOSAGE AND ADMINISTRATION).

Once absorbed through the skin, topical corticosteroids are handled through pharmacokinetic pathways similar to systemically administered corticosteroids. Corticosteroids are bound to plasma proteins in varying degrees. Corticosteroids are metabolized primarily in the liver and are then excreted by the kidneys. Some of the topical corticosteroids and their metabolites are also excreted into the bile.

Indications and Usage for Halog Ointment, USP

HALOG OINTMENT (Halcinonide Ointment, USP) 0.1% is indicated for the relief of the inflammatory and pruritic manifestations of corticosteroidresponsive dermatoses.

Contraindications

Topical corticosteroids are contraindicated in those patients with a history of hypersensitivity to any of the components of the preparations.

Precautions

General

Systemic absorption of topical corticosteroids has produced reversible hypothalamic-pituitary-adrenal (HPA) axis suppression, manifestations of Cushing’s syndrome, hyperglycemia, and glucosuria in some patients.

Conditions which augment systemic absorption include the application of the more potent steroids, use over large surface areas, prolonged use, and the addition of occlusive dressings.

Therefore, patients receiving a large dose of any potent topical steroid applied to a large surface area or under an occlusive dressing should be evaluated periodically for evidence of HPA axis suppression by using the urinary free cortisol and ACTH stimulation tests, and for impairment of thermal homeostasis. If HPA axis suppression or elevation of the body temperature occurs, an attempt should be made to withdraw the drug, to reduce the frequency of application, substitute a less potent steroid, or use a sequential approach when utilizing the occlusive technique.

Recovery of HPA axis function and thermal homeostasis are generally prompt and complete upon discontinuation of the drug. Infrequently, signs and symptoms of steroid withdrawal may occur, requiring supplemental systemic corticosteroids. Occasionally, a patient may develop a sensitivity reaction to a particular occlusive dressing material or adhesive and a substitute material may be necessary.

Children may absorb proportionally larger amounts of topical corticosteroids and thus be more susceptible to systemic toxicity (see PRECAUTIONS: Pediatric Use).

If irritation develops, topical corticosteroids should be discontinued and appropriate therapy instituted.

In the presence of dermatological infections, the use of an appropriate antifungal or antibacterial agent should be instituted. If a favorable response does not occur promptly, the corticosteroid should be discontinued until the infection has been adequately controlled.

This preparation is not for ophthalmic, oral, or intravaginal use.

Information for the Patient

Patients using topical corticosteroids should receive the following information and instructions:

1. This medication is to be used as directed by the physician. It is for dermatologic use only. Avoid contact with the eyes.


2. Patients should be advised not to use this medication for any disorder other than for which it was prescribed.


3. The treated skin area should not be bandaged or otherwise covered or wrapped as to be occlusive unless directed by the physician.


4. Patients should report any signs of local adverse reactions especially under occlusive dressing.


5. Parents of pediatric patients should be advised not to use tight-fitting diapers or plastic pants on a child being treated in the diaper area, as these garments may constitute occlusive dressings.

Laboratory Tests

A urinary free cortisol test and ACTH stimulation test may be helpful in evaluating HPA axis suppression.

Carcinogenesis, Mutagenesis and Impairment of Fertility

Long-term animal studies have not been performed to evaluate the carcinogenic potential or the effect on fertility of topical corticosteroids.

Studies to determine mutagenicity with prednisolone and hydrocortisone showed negative results.

Pregnancy

Teratogenic Effects: Category C

Corticosteroids are generally teratogenic in laboratory animals when administered systemically at relatively low dosage levels. The more potent corticosteroids have been shown to be teratogenic after dermal application in laboratory animals. There are no adequate and well-controlled studies in pregnant women on teratogenic effects from topically applied corticosteroids. Therefore, topical corticosteroids should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Drugs of this class should not be used extensively on pregnant patients, in large amounts, or for prolonged periods of time.

Nursing Mothers

It is not known whether topical administration of corticosteroids could result in sufficient systemic absorption to produce detectable quantities in breast milk. Systemically administered corticosteroids are secreted into breast milk in quantities not likely to have a deleterious effect on the infant. Nevertheless, caution should be exercised when topical corticosteroids are administered to a nursing woman.

Pediatric Use

Pediatric patients may demonstrate greater susceptibility to topical corticosteroid-induced HPA axis suppression and Cushing’s syndrome than mature patients because of a larger skin surface area to body weight ratio.

HPA axis suppression, Cushing’s syndrome, and intracranial hypertension have been reported in children receiving topical corticosteroids. Manifestations of adrenal suppression in children include linear growth retardation, delayed weight gain, low plasma cortisol levels, and absence of response to ACTH stimulation. Manifestations of intracranial hypertension include bulging fontanelles, headaches, and bilateral papilledema.

Administration of topical corticosteroids to children should be limited to the least amount compatible with an effective therapeutic regimen. Chronic corticosteroid therapy may interfere with the growth and development of children.

Geriatric Use

Clinical studies of 0.1% HALOG OINTMENT did not include sufficient numbers of patients aged 65 years and over to determine whether they respond differently from younger patients. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range.

Adverse Reactions

The following local adverse reactions are reported infrequently with topical corticosteroids, but may occur more frequently with the use of occlusive dressings (reactions are listed in an approximate decreasing order of occurrence): burning, itching, irritation, dryness, folliculitis, hypertrichosis, acneiform eruptions, hypopigmentation, perioral dermatitis, allergic contact dermatitis, maceration of the skin, secondary infection, skin atrophy, striae, and miliaria.

Overdosage

Topically applied corticosteroids can be absorbed in sufficient amounts to produce systemic effects (see PRECAUTIONS: General).

Halog Ointment, USP Dosage and Administration

Apply a thin film of 0.1% HALOG OINTMENT (Halcinonide Ointment, USP) to the affected area two to three times daily.

Occlusive Dressing Technique

Occlusive dressings may be used for the management of psoriasis or other recalcitrant conditions. Apply a thin film of ointment to the lesion, cover with a pliable nonporous film, and seal the edges. If needed, additional moisture may be provided by covering the lesion with a dampened clean cotton cloth before the nonporous film is applied or by briefly wetting the affected area with water immediately prior to applying the medication. The frequency of changing dressings is best determined on an individual basis. It may be convenient to apply HALOG OINTMENT under an occlusive dressing in the evening and to remove the dressing in the morning (i.e., 12-hour occlusion). When utilizing the 12-hour occlusion regimen, additional ointment should be applied, without occlusion, during the day. Reapplication is essential at each dressing change.

If an infection develops, the use of occlusive dressings should be discontinued and appropriate antimicrobial therapy instituted.

How is Halog Ointment, USP Supplied

HALOG® OINTMENT (Halcinonide Ointment, USP) 0.1% is supplied as tubes containing 15 g (NDC 10631-096-15), 30 g (NDC 10631-096-20), and 60 g (NDC 10631-096-30).

Storage

Store at room temperature; avoid excessive heat (104º F).

RANBAXY

Jacksonville, FL 32257 USA

July 2009

PACKAGE LABEL PRINCIPAL DISPLAY PANEL

Halog Ointment 15 gm Tube

Halog Ointment 15 gm Carton

Halog Ointment 30 gm Tube

Halog Ointment 30 gm Carton

Halog Ointment 60 gm Tube

Halog Ointment 60 gm Carton

HALOG  OINTMENT halcinonide  ointment

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 10631-096 Route of Administration TOPICAL DEA Schedule

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength HALCINONIDE (HALCINONIDE) HALCINONIDE 1 mg  in 1 g

Inactive Ingredients Ingredient Name Strength POLYETHYLENE GLYCOL 300   POLYETHYLENE GLYCOL 400   POLYETHYLENE GLYCOL 1450   POLYETHYLENE GLYCOL 6000   BUTYLATED HYDROXYTOLUENE   MINERAL OIL

Product Characteristics Color      Score      Shape Size Flavor Imprint Code Contains

Packaging # NDC Package Description Multilevel Packaging 1 10631-096-15 15 g In 1 TUBE None 2 10631-096-20 30 g In 1 TUBE None 3 10631-096-30 60 g In 1 TUBE None

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
NDA	NDA017824	05/19/2009

Labeler - Ranbaxy Laboratories Inc. (169932519)

Registrant - Ranbaxy Laboratories Inc. (169932519)

Establishment
Name	Address	ID/FEI	Operations
Contract Pharmaceuticals Limited		248761249	manufacture

Revised: 09/2009Ranbaxy Laboratories Inc.

More Halog Ointment, USP resources

• Halog Ointment, USP Side Effects (in more detail)
• Halog Ointment, USP Use in Pregnancy & Breastfeeding
• Halog Ointment, USP Drug Interactions
• Halog Ointment, USP Support Group
• 0 Reviews for Halog, - Add your own review/rating

Compare Halog Ointment, USP with other medications

• Atopic Dermatitis
• Dermatitis
• Eczema
• Psoriasis

UltimateCare ONE NF

prenatal vitamin supplement

Dosage Form: capsule
UltimateCare ONE NF

A once-daily prenatal vitamin supplement, including key omega-3 fatty acids (DHA and EPA) and 1 mg folic acid.

Rx Only

UltimateCare ONE NF Description

UltimateCare ONE NF is a prescription prenatal/postnatal multivitamin/mineral capsule with omega-3 fatty acids. Each maroon soft gelatin capsule for oral administration contains:

* Vitamin C Complex is a pharmaceutical grade material consisting of calcium ascorbate and calcium threonate.
Essential Fatty Acids:
Omega-3 Fatty Acids	500 mg
Docosahexaenoic Acid (DHA)	350 mg
Eicosapentaenoic Acid (EPA)	100 mg
α-Linolenic Acid (ALA)	50 mg
Vitamins:
Vitamin C Complex*   (as calcium ascorbate and calcium threonate)	25 mg
Vitamin D3 (cholecalciferol)	800 IU
Vitamin E (dl-alpha-tocopheryl acetate)	15 IU
Vitamin B2 (riboflavin, USP)	1.5 mg
Vitamin B3 (niacinamide)	10 mg
Vitamin B6 (pyridoxine hydrochloride)	50 mg
Folic Acid, USP	1 mg
Biotin	300 mcg
Minerals:
Calcium	100 mg
Iron (elemental iron)
Carbonyl iron	20 mg
Ferrous Asparto Glycinate	7 mg
Iodine	150 mcg
Magnesium (magnesium oxide)	50 mg
Zinc (zinc oxide, USP)	5 mg
Other:
Docusate Sodium	50 mg

Inactive Ingredients: Gelatin, Glycerin, Purified Water, Yellow Bees Wax, Natural Creamy Orange Flavor, Lecithin, FD&C Red #40, Titanium Oxide, Ethyl Vanillin, FD&C Yellow #6, and FD&C Blue #1.

INDICATIONS

UltimateCare ONE NF is indicated to provide vitamin/mineral and omega-3 fatty acid supplementation throughout pregnancy, during the postnatal period for both lactating and non-lactating mothers, and throughout the childbearing years. It is also useful for improving nutritional status prior to conception.

Contraindications

This product is contraindicated in patients with a known hypersensitivity to any of the ingredients.

Warnings

Folic acid alone is improper therapy in the treatment of pernicious anemia and other megaloblastic anemias where vitamin B12 is deficient. Folic acid in doses above 0.1 mg daily may obscure pernicious anemia, in that hematologic remission can occur while neurological manifestations remain progressive.

WARNING

Accidental overdose of iron-containing products is a leading cause of fatal poisoning in children under 6. Keep this product out of reach of children. In case of accidental overdose, call a doctor or poison control center immediately.

THIS PRODUCT CONTAINS SOY.

Precautions

General

Do not exceed recommended dosage. UltimateCare ONE NF should be used with caution in patients with known sensitivity or allergy to fish.

Pediatric Use

Safety and effectiveness in pediatric patients have not been established.

Geriatric Use

Clinical studies on this product have not been performed to determine whether elderly subjects respond differently from younger subjects. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

Adverse Reactions

Allergic sensitization has been reported following both oral and parenteral administration of folic acid.

UltimateCare ONE NF Dosage and Administration

Usual dosage is one capsule daily, or as prescribed by a physician.

How is UltimateCare ONE NF Supplied

UltimateCare ONE NF prenatal/postnatal multivitamin/mineral capsules are maroon soft gelatin capsules, imprinted "TL050", packaged in bottles of 30 capsules (NDC 13811-050-30).

Store at 20°-25°C (68°-77°F); excursions permitted to 15°-30°C (59°-86°F). [see USP Controlled Room Temperature].

Call your doctor about side effects.

You may report side effects by calling 888 9 TRIGEN (888-987-4436) .

KEEP THIS AND ALL DRUGS OUT OF REACH OF CHILDREN.

Rx Only

Manufactured for:

TRIGEN Laboratories, Inc.

Sayreville, NJ 08872

09/11

PRINCIPAL DISPLAY PANEL - 30 Softgel Capsule Bottle Label

Rx Only

NDC 13811-050-30

30 Softgel Capsules

UltimateCare

ONE NF

with DHA and EPA

TRIGEN

LABORATORIES

ULTIMATECARE   ONE NF omega-3 fatty acids, doconexent, icosapent, linolenic acid, calcium ascorbate, calcium threonate, cholecalciferol, .alpha.-tocopherol acetate, dl-, riboflavin, niacinamide, pyridoxine hydrochloride, folic acid, biotin, calcium, iron, ferrous asparto glycinate, iodine, magnesium oxide, zinc oxide, and docusate sodium  capsule

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 13811-050 Route of Administration ORAL DEA Schedule

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength Omega-3 Fatty Acids (Omega-3 Fatty Acids) Omega-3 Fatty Acids 500 mg Doconexent (Doconexent) Doconexent 350 mg Icosapent (Icosapent) Icosapent 100 mg Linolenic Acid (Linolenic Acid) Linolenic Acid 50 mg Calcium Ascorbate (Calcium Ascorbate) Calcium Ascorbate 24 mg Calcium Threonate (Calcium Threonate) Calcium Threonate 1 mg Cholecalciferol (Cholecalciferol) Cholecalciferol 800 [iU] .Alpha.-Tocopherol Acetate, DL- (.Alpha.-Tocopherol Acetate, DL-) .Alpha.-Tocopherol Acetate, DL- 15 [iU] Riboflavin (Riboflavin) Riboflavin 1.5 mg Niacinamide (Niacinamide) Niacinamide 10 mg Pyridoxine Hydrochloride (Pyridoxine) Pyridoxine Hydrochloride 50 mg Folic Acid (Folic Acid) Folic Acid 1 mg Biotin (Biotin) Biotin 300 ug Calcium (Calcium Cation) Calcium 100 mg Iron (Iron) Iron 20 mg Ferrous Asparto Glycinate (Ferrous Asparto Glycinate) Ferrous Asparto Glycinate 7 mg Iodine (Iodine) Iodine 150 ug Magnesium Oxide (Magnesium Oxide) Magnesium Oxide 50 mg Zinc Oxide (Zinc Oxide) Zinc Oxide 5 mg Docusate Sodium (Docusate) Docusate Sodium 50 mg

Inactive Ingredients Ingredient Name Strength Gelatin   Glycerin   Water   Yellow Wax   FD&C Red No. 40   Titanium Dioxide   Ethyl Vanillin   FD&C Yellow No. 6   FD&C Blue No. 1

Product Characteristics Color RED (maroon) Score no score Shape CAPSULE Size 27mm Flavor ORANGE (Creamy Orange) Imprint Code TL050 Contains

Packaging # NDC Package Description Multilevel Packaging 1 13811-050-30 30 CAPSULE In 1 BOTTLE None

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
Unapproved drug other		12/04/2009

Labeler - TRIGEN Laboratories, Inc. (830479668)

Revised: 09/2011TRIGEN Laboratories, Inc.

More UltimateCare ONE NF resources

• UltimateCare ONE NF Side Effects (in more detail)
• UltimateCare ONE NF Use in Pregnancy & Breastfeeding
• UltimateCare ONE NF Drug Interactions
• 0 Reviews for UltimateCare ONE NF - Add your own review/rating

• Advance Care Plus Concise Consumer Information (Cerner Multum)


• Cal-Nate MedFacts Consumer Leaflet (Wolters Kluwer)


• CareNatal DHA MedFacts Consumer Leaflet (Wolters Kluwer)


• CitraNatal 90 DHA MedFacts Consumer Leaflet (Wolters Kluwer)


• Duet DHA with Ferrazone MedFacts Consumer Leaflet (Wolters Kluwer)


• Folbecal MedFacts Consumer Leaflet (Wolters Kluwer)


• Gesticare DHA MedFacts Consumer Leaflet (Wolters Kluwer)


• MultiNatal Plus MedFacts Consumer Leaflet (Wolters Kluwer)


• Multifol Plus Concise Consumer Information (Cerner Multum)


• Neevo Caplets MedFacts Consumer Leaflet (Wolters Kluwer)


• Neevo DHA MedFacts Consumer Leaflet (Wolters Kluwer)


• OB Complete 400 MedFacts Consumer Leaflet (Wolters Kluwer)


• PreNexa MedFacts Consumer Leaflet (Wolters Kluwer)


• Prenate Elite tablets


• Prenate Elite MedFacts Consumer Leaflet (Wolters Kluwer)


• PrimaCare Advantage MedFacts Consumer Leaflet (Wolters Kluwer)


• PrimaCare ONE capsules


• PrimaCare One MedFacts Consumer Leaflet (Wolters Kluwer)


• Se-Natal 19 Chewable Tablets MedFacts Consumer Leaflet (Wolters Kluwer)


• Triveen-One MedFacts Consumer Leaflet (Wolters Kluwer)


• Ultra NatalCare MedFacts Consumer Leaflet (Wolters Kluwer)


• Vitafol-One MedFacts Consumer Leaflet (Wolters Kluwer)

Compare UltimateCare ONE NF with other medications

• Vitamin/Mineral Supplementation during Pregnancy/Lactation

Neulactil Tablets (Winthrop Pharmaceuticals UK Ltd)

1. Name Of The Medicinal Product

Neulactil Tablets 2.5 mg

Neulactil Tablets 10 mg

2. Qualitative And Quantitative Composition

Pericyazine 2.5 mg

Pericyazine 10 mg

3. Pharmaceutical Form

2.5mg tablets: Circular, very pale lime-yellow tablet, with one face impressed Neulactil just inside the perimeter. Break-line on reverse.

10mg tablets: Circular, very pale lime-yellow tablet, with one face impressed Neulactil just inside the perimeter around a central 10. Break-line on reverse.

4. Clinical Particulars

4.1 Therapeutic Indications

a) In adults with schizophrenia or other psychoses, for the treatment of symptoms or prevention of relapse.

b) In anxiety, psychomotor agitation, violent or dangerously impulsive behaviour. Neulactil is used as an adjunct to the short-term management of these conditions.

4.2 Posology And Method Of Administration

Route of administration: oral .

Dosage requirement varies with the individual and the severity of the condition being treated. Initial dosage should be low with progressive increases until the desired response is obtained, after which dosage should be adjusted to maintain control of the symptoms.

Severe conditions

Indication (a)

Adults: Initially 75 mg per day in divided doses. Dosage should be increased by 25 mg per day at weekly intervals until the optimum effect is achieved. Maintenance therapy would not normally be expected to exceed 300 mg per day.

Elderly: Initially 15-30 mg per day in divided doses. If this is well tolerated the dosage may be increased if necessary for optimum control of behaviour.

Mild or moderate conditions

Indication (b)

Adults: Initially 15-30 mg daily, divided into two portions with a larger dose being given in the evening.

Elderly: 5-10 mg per day is suggested as a starting dose. It may be divided so that a larger portion is given in the evening. Half or quarter the normal adult dose may be sufficient for maintenance therapy.

Neulactil tablets are not recommended for children.

4.3 Contraindications

See use in pregnancy below. Known hypersensitivity to pericyazine or to any of the other ingredients.

4.4 Special Warnings And Precautions For Use

Neuroleptics should be avoided in patients with liver or renal dysfunction, Parkinson's disease, hypothyroidism, cardiac failure, phaeochromocytoma, myasthenia gravis, prostrate hypertrophy. It should be avoided in patients known to be hypersensitive to phenothiazines or with a history of narrow angle glaucoma or agranulocytosis. It should be used with caution in the elderly, particularly during very hot or very cold weather (risk of hyper-hypothermia).

Close monitoring is required in patients with epilepsy or a history of seizures, as phenothiazines may lower the seizure threshold.

As agranulocytosis may occur rarely, regular monitoring of the complete blood count is recommended.

It is imperative that treatment be discontinued in the event of unexplained fever, as this may be a sign of neuroleptic malignant syndrome (pallor, hyperthermia, autonomic dysfunction, altered consciousness, muscle rigidity). Signs of autonomic dysfunction, such as sweating and arterial instability, may precede the onset of hyperthermia and serve as early warning signs. Although neuroleptic malignant syndrome may be idiosyncratic in origin, dehydration and organic brain disease are predisposing factors.

The occurrence of unexplained infections or fever may be evidence of blood dyscrasia (see section 4.8 below), and requires immediate haematological investigation.

Acute withdrawal symptoms, including nausea, vomiting and insomnia, have very rarely been reported following the abrupt cessation of high doses of neuroleptics. Relapse may also occur, and the emergence of extrapyramidal reactions has been reported. Therefore, gradual withdrawal is advisable.

In schizophrenia, the response to neuroleptic treatment may be delayed. If treatment is withdrawn, the recurrence of symptoms may not become apparent for some time.

Neuroleptic phenothiazines may potentiate QT interval prolongation which increases the risk of onset of serious ventricular arrhythmias of the torsade de pointes type, which is potentially fatal (sudden death). QT prolongation is exacerbated, in particular, in the presence of bradycardia, hypokalaemia, and congenital or acquired (i.e. drug induced) QT prolongation. The risk-benefit should be fully assessed before Neulactil treatment is commenced. If the clinical situation permits, medical and laboratory evaluations (e.g. biochemical status and ECG) should be performed to rule out possible risk factors (e.g. cardiac disease; family history of QT prolongation; metabolic abnormalities such as hypokalaemia, hypocalcaemia or hypomagnesaemia; starvation; alcohol abuse; concomitant therapy with other drugs known to prolong the QT interval) before initiating treatment with Neulactil and during the initial phase of treatment, or as deemed necessary during the treatment (see also sections 4.5 and 4.8).

Avoid concomitant treatment with other neuroleptics (see section 4.5).

Stroke: In randomised clinical trials versus placebo performed in a population of elderly patients with dementia and treated with certain atypical antipsychotic drugs, a 3-fold increase of the risk of cerebrovascular events has been observed. The mechanism of such risk increase is not known. An increase in the risk with other antipsychotic drugs or other populations of patients cannot be excluded. Neulactil should be used with caution in patients with stroke risk factors.

As with all antipsychotic drugs, Neulactil should not be used alone where depression is predominant. However, it may be combined with antidepressant therapy to treat those conditions in which depression and psychosis coexist.

Because of the risk of photosensitisation, patients should be advised to avoid exposure to direct sunlight.

In those frequently handling preparations of phenothiazines, the greatest care must be taken to avoid contact of the drug with the skin, since contact skin sensitisation occurs rarely.

4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction

Interactions of phenothiazine neuroleptics:

The CNS depressant actions of neuroleptic agents may be intensified (additively) by alcohol, barbiturates and other sedatives. Respiratory depression may occur.

The hypotensive effect of most antihypertensive drugs, especially alpha adrenoceptor blocking agents may be exaggerated by neuroleptics.

There is an increased risk of arrhythmias when neuroleptics are used with concomitant QT prolonging drugs (including certain antiarrhythmics, antidepressants, and other antipsychotics) and drugs causing electrolyte imbalance (see sections 4.4 and 4.8).

The mild anticholinergic effect of neuroleptics may be enhanced by other anticholinergic drugs, possibly leading to constipation, heat stroke, etc.

The action of some drugs may be opposed by neuroleptics; these include amfetamine, levodopa, clonidine, guanethidine, adrenaline.

Where treatment for neuroleptic-induced extrapyramidal symptoms is required, anticholinergic antiparkinsonian agents should be used in preference to levodopa, since neuroleptics antagonise the antiparkinsonian action of dopaminergics.

Anticholinergic agents may reduce the antipsychotic effect of neuroleptics.

Some drugs interfere with absorption of neuroleptic agents: antacids, anti-Parkinson drugs, lithium. Increases or decreases in the plasma concentrations of a number of drugs, e.g: propranolol, phenobarbital have been observed but were not of clinical significance. High doses of neuroleptics may reduce the response to hypoglycaemic agents the dosage of which might have to be raised.

In patients treated concurrently with neuroleptics and lithium, there have been rare reports of neurotoxicity.

Adrenaline must not be used in patients overdosed with neuroleptics.

Simultaneous administration of desferrioxamine and prochlorperazine has been observed to induce a transient metabolic encephalopathy characterised by loss of consciousness for 48-72 hours. It is possible this may occur with Neulactil since it shares many of the pharmacological properties of prochlorperazine.

There is an increased risk of agranulocytosis when neuroleptics are used concurrently with drugs with myelosuppressive potential, such as carbamazepine or certain antibiotics and cytotoxics.

4.6 Pregnancy And Lactation

There is inadequate evidence of the safety of Neulactil in human. There is evidence with some neuroleptics of harmful effects in animals. Like other drugs Neulactil should be avoided in pregnancy unless the physician considers it essential. It may occasionally prolong labour and at such a time should be withheld until the cervix is dilated 3-4 cm. Possible adverse effects on the foetus include lethargy or paradoxical hyperexcitability, tremor and low Apgar score.

Phenothiazines may be excreted in milk, therefore breastfeeding should be suspended during treatment.

4.7 Effects On Ability To Drive And Use Machines

Patients should be warned about drowsiness during early days of treatment, and advised not to drive or operate machinery. The elderly are particularly susceptible to postural hypotension.

4.8 Undesirable Effects

Liver function: jaundice, occurs in a very small percentage of patients taking neuroleptics. A premonitory sign may be a sudden onset of fever after one to three weeks of treatment followed by the development of jaundice. Neuroleptic jaundice has the biochemical and other characteristics of obstructive (cholestatic) jaundice and is associated with obstruction of the canaliculi by bile thrombi; the frequent presence of an accompanying eosinophilia indicates the allergic nature of this phenomenon. Liver injury has been reported very rarely in patients treated with pericyazine. Treatment should be withheld on the development of jaundice.

Cardiorespiratory: hypotension, usually postural, commonly occurs. Elderly or volume depleted subjects are particularly susceptible.

ECG changes, include QT prolongation (as with other neuroleptics), ST depression, U-Wave and T-Wave changes. Cardiac arrhythmias, including ventricular arrhythmias and atrial arrhythmias, a-v block, ventricular tachycardia, which may result in ventricular fibrillation or cardiac arrest have been reported during neuroleptic phenothiazine therapy, possibly related to dosage. Pre-existing cardiac disease, old age, hypokalaemia and concurrent tricyclic antidepressants may predispose.

There have been isolated reports of sudden death, with possible cases of cardiac origin (see section 4.4, above), as well as cases of unexplained sudden death, in patients receiving neuroleptic phenothiazines.

Respiratory depression is possible in susceptible patients.

Blood picture: a mild leukopenia occurs in up to 30% of patients on prolonged high dosage of neuroleptics; agranulocytosis may occur rarely; it is not dose-related.

Extrapyramidal: acute dystonias or dyskinesias, usually transitory are commoner in children and young adults, and usually occur within the first four days of treatment or after dosage increases.

• Akathisia characteristically occurs after large initial doses.

• Parkinsonism is commoner in adults and the elderly. It usually develops after weeks or months of treatment. One or more of the following may be seen: tremor, rigidity, akinesia, or other features of Parkinsonism. Commonly just tremor.

• Tardive dyskinesia: if this occurs it is usually, but not necessarily after prolonged or high dosage. It can even occur after treatment has been stopped. Dosage should therefore be kept low whenever possible.

Skin and eyes: contact skin sensitisation may occur rarely in those frequently handling preparations of phenothiazines (see section 4.4, above. Skin rashes of various kinds may also be seen in patients treated with the drug. Patients on high dosage should be warned that they may develop photosensitivity in sunny weather and should avoid exposure to direct sunlight.

Endocrine: hyperprolactinaemia which may result in galactorrhoea, gynaecomastia, amenorrhoea; impotence.

Priapism has very rarely been reported in patients treated with peryciazine

Neuroleptic malignant syndrome (hyperthermia, rigidity autonomic dysfunction and altered consciousness) may occur with any neuroleptic.

Minor side effects are nasal stuffiness, dry mouth, insomnia, agitation

4.9 Overdose

Toxicity and treatment of overdosage:

Symptoms of neuroleptic overdosage include drowsiness or loss of consciousness, hypotension, tachycardia, ECG changes, ventricular arrhythmias and hypothermia. Severe extrapyramidal dyskinesias may occur.

If the patient is seen sufficiently soon (up to 6 hours) after ingestion of a toxic dose, gastric lavage may be attempted. Pharmacological induction of emesis is unlikely to be of any use. Activated charcoal should be given. There is no specific antidote. Treatment is supportive.

Generalised vasodilatation may result in circulatory collapse; raising the patient's legs may suffice; in severe cases, volume expansion by intravenous fluids may be needed; infusion fluids should be warmed before administration in order not to aggravate hypothermia.

Positive inotropic agents such as dopamine may be tried if fluid replacement is insufficient to correct the circulatory collapse. Peripheral vasoconstrictor agents are not generally recommended; avoid the use of adrenaline.

Ventricular or supraventricular tachy-arrhythmias usually respond to restoration of normal body temperature and correction of circulatory or metabolic disturbances. If persistent or life threatening, appropriate anti-arrhythmic therapy may be considered. Avoid lidocaine, and as far as possible long acting, anti-arrhythmic drugs.

Pronounced central nervous system depression requires airway maintenance or, in extreme circumstances, assisted respiration. Severe dystonic reactions usually respond to procyclidine (5-10 mg) or orphenedrine (20-40 mg) administered intramuscularly or intravenously. Convulsions should be treated with intravenous diazepam.

Neuroleptic malignant syndrome should be treated with cooling. Dantrolene sodium may be tried.

5. Pharmacological Properties

5.1 Pharmacodynamic Properties

Pericyazine is a neuroleptic with cardiovascular and antihistamine effects similar to those of chlorpromazine, but it has a stronger antiserotonin effect and a powerful central sedative effect.

5.2 Pharmacokinetic Properties

Kinetics: there is little information about plasma concentrations, distribution and excretion in humans. The rate of metabolism and excretion of phenothiazines decreases in old age.

5.3 Preclinical Safety Data

There are no preclinical data of relevance to the prescriber which are additional to that already included in other sections of the SPC.

6. Pharmaceutical Particulars

6.1 List Of Excipients

Lactose, anhydrous

Cellulose, microcrystalline (E460)

Sodium starch glycolate

Magnesium stearate

Silica, colloidal anhydrous (E551)

Methyl parahydroxybenzoate (E218)

6.2 Incompatibilities

None known.

6.3 Shelf Life

60 months.

6.4 Special Precautions For Storage

Protect from light.

6.5 Nature And Contents Of Container

PVDC coated UPVC aluminium foil blister containing 84 tablets.

6.6 Special Precautions For Disposal And Other Handling

None stated.

7. Marketing Authorisation Holder

Sanofi-aventis

One Onslow Street

Guildford

Surrey

GU1 4YS

UK

8. Marketing Authorisation Number(S)

2.5mg tablets: PL 04425/0586

10mg tablets: PL 04425/0587

9. Date Of First Authorisation/Renewal Of The Authorisation

2.5mg tablets: 15 October 2006

10mg tablets: 1 September 1997

10. Date Of Revision Of The Text

15 August 2007

Legal Category

POM

Parcaine

Generic Name: proparacaine (Ophthalmic route)

proe-PAR-a-kane

Commonly used brand name(s)

In the U.S.

• Alcaine


• Ocu-Caine


• Ophthetic


• Parcaine

Available Dosage Forms:

• Solution

Therapeutic Class: Anesthetic, Local

Chemical Class: Amino Ester

Uses For Parcaine

Proparacaine eye drops are used to numb the eye before surgery, certain tests, or procedures. The eye drops are used to prevent pain during the procedure.

Proparacaine belongs to the group of medicines called local anesthetics. It works by blocking the pain signals at the nerve endings in the eye.

This medicine is to be administered only by or under the direct supervision of an eye doctor.

Before Using Parcaine

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Although appropriate studies on the relationship of age to the effects of proparacaine eye drops have not been performed in the pediatric population, no pediatric-specific problems have been documented to date.

Geriatric

No information is available on the relationship of age to the effects of proparacaine eye drops in geriatric patients.

Pregnancy

	Pregnancy Category	Explanation
All Trimesters	C	Animal studies have shown an adverse effect and there are no adequate studies in pregnant women OR no animal studies have been conducted and there are no adequate studies in pregnant women.

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. Tell your healthcare professional if you are taking any other prescription or nonprescription (over-the-counter [OTC]) medicine.

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Heart disease or


• Hyperthyroidism (overactive thyroid)—May cause side effects to become worse.

Proper Use of proparacaine

This section provides information on the proper use of a number of products that contain proparacaine. It may not be specific to Parcaine. Please read with care.

A nurse or other trained health professional will give you this medicine. The eye drops are placed directly in the eye.

Precautions While Using Parcaine

Your doctor will check your progress closely while you are receiving this medicine. This will allow your doctor to see if the medicine is working properly and to decide if you should continue to receive it.

It is very important to protect your eye from injury while it is still numb. Do not touch or rub the eye. Do not use additional eye drops in the eye until your doctor tells you to. Protect your eye from dust particles, sand, or anything that might cause irritation.

Parcaine Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor or nurse immediately if any of the following side effects occur:

Rare

• Blurred vision


• redness of the clear part of the eye


• sensitivity to light


• severe stinging in the eye


• tearing


• throbbing eye pain

Incidence not known

• Bloody eye


• burning, stinging, itching, redness, or irritation of the eye


• change in vision

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

Incidence not known

• Dry skin with cracking


• grooves or lines in the skin of the fingertips


• skin rash, hives, itching, or redness

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

The information contained in the Thomson Reuters Micromedex products as delivered by Drugs.com is intended as an educational aid only. It is not intended as medical advice for individual conditions or treatment. It is not a substitute for a medical exam, nor does it replace the need for services provided by medical professionals. Talk to your doctor, nurse or pharmacist before taking any prescription or over the counter drugs (including any herbal medicines or supplements) or following any treatment or regimen. Only your doctor, nurse, or pharmacist can provide you with advice on what is safe and effective for you.

The use of the Thomson Reuters Healthcare products is at your sole risk. These products are provided "AS IS" and "as available" for use, without warranties of any kind, either express or implied. Thomson Reuters Healthcare and Drugs.com make no representation or warranty as to the accuracy, reliability, timeliness, usefulness or completeness of any of the information contained in the products. Additionally, THOMSON REUTERS HEALTHCARE MAKES NO REPRESENTATION OR WARRANTIES AS TO THE OPINIONS OR OTHER SERVICE OR DATA YOU MAY ACCESS, DOWNLOAD OR USE AS A RESULT OF USE OF THE THOMSON REUTERS HEALTHCARE PRODUCTS. ALL IMPLIED WARRANTIES OF MERCHANTABILITY AND FITNESS FOR A PARTICULAR PURPOSE OR USE ARE HEREBY EXCLUDED. Thomson Reuters Healthcare does not assume any responsibility or risk for your use of the Thomson Reuters Healthcare products.

More Parcaine resources

• Parcaine Use in Pregnancy & Breastfeeding
• Parcaine Support Group
• 0 Reviews · Be the first to review/rate this drug

• Alcaine Drops MedFacts Consumer Leaflet (Wolters Kluwer)


• Alcaine Prescribing Information (FDA)


• Ophthetic Prescribing Information (FDA)

Pralatrexate

Class: Antineoplastic Agents
VA Class: AN300
Chemical Name: (2S)-2[[4-[1RS)-1[2,4-diaminopteridin-6-yl)methyl]but-3-ynyl]benzoyl]amino]pentanedioic acid
Molecular Formula: C₂₃H₂₃N₇O₅
CAS Number: 146464-95-1
Brands: Folotyn

Introduction

Antineoplastic agent; a folic acid antagonist.^{1 3 4 5 6 7 8 9}

Uses for Pralatrexate

Peripheral T-cell Lymphoma (PTCL)

Treatment of relapsed or refractory peripheral T-cell lymphoma (PTCL).^{1 2} Efficacy determined based on overall response rate; clinical benefit (e.g., improvement in progression-free or overall survival) not established.¹

Designated an orphan drug by FDA for this condition.²

Pralatrexate Dosage and Administration

General

• 
  

  Consult specialized references for procedures for proper handling and disposal of antineoplastics.¹

  
  


• 
  

  Monitor CBCs and severity of mucositis and other treatment-related toxicities (e.g., hepatotoxicity) weekly prior to each dose.¹ Administer pralatrexate only when mucositis is grade 1 or lower, platelet count ≥100,000/mm³ (prior to first dose) or ≥50,000/mm³ (prior to subsequent doses), and ANC ≥1000/mm³.¹ Perform serum chemistry tests, including hepatic and renal function tests, before administration of first and fourth pralatrexate doses of each treatment cycle.¹ (See Dosage Modification for Toxicity under Dosage and Administration.)

  
  

Vitamin Supplementation

• 
  

  To reduce toxicity, all patients should take low-dose oral folic acid (1–1.25 mg daily) starting 10 days before the first dose of pralatrexate; continue folic acid during therapy and for 30 days after the last dose of pralatrexate.¹

  
  


• 
  

  Administer one IM injection of vitamin B₁₂ (1 mg) within 10 weeks of the first dose of pralatrexate and then once every 8–10 weeks; subsequent injections may be given on the same day as pralatrexate.¹ (See Folate and Vitamin B₁₂ Supplementation under Cautions.)

  
  

Administration

IV Administration

For solution compatibility information, see Compatibility under Stability.

Administer undiluted by rapid IV injection only.¹

Administer into the side port of a free-flowing IV infusion of 0.9% sodium chloride.¹

Prepare and handle cautiously; use protective gloves and other protective clothing. ¹ If skin contact occurs, immediately wash affected area(s) throughly with soap and water; if mucosal contact occurs, flush throughly with water. ¹

Using aseptic technique, withdraw appropriate volume of pralatrexate 20-mg/mL injection into a syringe for immediate use.¹ Do not dilute.¹

Pralatrexate injection contains no preservatives, and vials are intended for single-use only; discard any unused portions.¹

Rate of Administration

Administer by rapid injection over 3–5 minutes.¹

Dosage

Adults

Peripheral T-cell Lymphoma

IV

30 mg/m² once weekly for 6 weeks, followed by 1 week of rest. ¹ Continue this 7-week cycle until disease progression or toxicity occurs.¹

Monitor CBCs and assess severity of mucositis and other treatment-related toxicities (e.g., hepatotoxicity) weekly just prior to each dose.¹ Administer subsequent doses only when mucositis severity is grade 1 or lower, platelet count ≥50,000/mm³, and ANC ≥1000/mm³ on day of treatment.¹ (See Dosage Modification for Toxicity under Dosage and Administration.)

Dosage Modification for Toxicity

Adjust subsequent doses based on severity of mucositis, hematologic counts (i.e., ANC, platelet count), and/or presence of other treatment-related toxicities (e.g., hepatotoxicity) determined on the day of treatment.¹ Depending on severity of toxicity, may need to omit and/or reduce subsequent doses or discontinue pralatrexate permanently.^{1 11} (See Tables 1–3.) Omitted doses should not be made up at the end of the treatment cycle; dosages reduced following drug-related adverse effects should not be re-escalated.¹

Mucositis

Assess severity of mucositis weekly just prior to each dose. ¹ Administer subsequent dose only if mucositis is grade 1 or lower on day of treatment.¹ (See Table 1.)

Per National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (NCI CTCAE version 3.0).

Table 1: Recommended Dosage Modification for Mucositis

Mucositis Grade on Day of Treatment	Recommended Action
Grade 2	Omit dose; when mucositis improves (to grade 1 or lower), resume pralatrexate at prior dose1
Grade 2 recurrence	Omit dose; when mucositis improves (to grade 1 or lower), resume pralatrexate at a reduced dose of 20 mg/m21
Grade 3	Omit dose; when mucositis improves (to grade 1 or lower), resume pralatrexate at a reduced dose of 20 mg/m21
Grade 4	Discontinue pralatrexate permanently1 11

Hematologic Toxicity

Monitor CBCs weekly just prior to each dose.¹ Administer subsequent doses only when platelet count ≥50,000/mm³ and ANC ≥1000/mm³ on day of treatment.¹ (See Table 2.)

Table 2. Recommended Dosage Modification for Hematologic Toxicity

Blood Count on Day of Treatment	Duration of Toxicity	Recommended Action
Platelet count <50,000/mm3	1 week	Omit dose; when platelet count ≥50,000/mm3, resume pralatrexate at prior dose1
2 weeks	Omit dose; when platelet count ≥50,000/mm3, resume pralatrexate at a reduced dose of 20 mg/m21
3 weeks	Discontinue pralatrexate permanently1 11
ANC of 500–1000/mm3 without fever	1 week	Omit dose; when ANC ≥1000/mm3, resume pralatrexate at prior dose1
ANC of 500–1000/mm3 with fever or ANC <500/mm3	1 week	Omit dose; initiate growth factor (e.g., filgrastim, sargramostim) support; when ANC ≥1000/mm3, resume pralatrexate at prior dose and continue growth factor support1
2 weeks or recurrence	Omit dose; initiate growth factor (e.g., filgrastim, sargramostim) support; when ANC ≥1000/mm3, resume treatment at a reduced dose of 20 mg/m2 and continue growth factor support1
3 weeks or second recurrence	Discontinue therapy permanently1 11

Other Treatment-related Toxicities

Per National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (NCI CTCAE version 3.0).

Table 3. Recommended Dosage Modification for Other Treatment-related Toxicities (e.g., Hepatotoxicity)

Toxicity Grade on Day of Treatment	Recommended Action
Grade 3	Omit dose; when toxicity improves (to grade 2 or lower), resume pralatrexate at a reduced dose of 20 mg/m21
Grade 4	Discontinue pralatrexate permanently1 11

Special Populations

Geriatric Patients

No dosage adjustments required in geriatric patients (≥65 years of age) with normal renal function except those recommended for all patients.¹

Cautions for Pralatrexate

Contraindications

• 
  

  No known contraindications.¹

  
  

Warnings/Precautions

Hematologic Toxicity

Risk of thrombocytopenia, anemia, and neutropenia.¹

Monitor CBCs weekly just prior to each dose.¹ Adjust dosage based on ANC and platelet count determined on day of treatment.¹ (See Hematologic Toxicity under Dosage and Administration.)

Mucositis

Risk of mucositis (i.e., stomatitis or mucosal inflammation of the GI and GU tracts).^{1 3 4 5} Typically occurs within 2–5 days after initiation of pralatrexate.¹¹

To reduce risk of mucositis, supplement with folic acid and vitamin B₁₂ before and during pralatrexate therapy.¹ (See General under Dosage and Administration.)

If mucositis is grade 2 or greater, may need to omit and/or reduce subsequent dose or discontinue pralatrexate permanently.^{1 11} (See Mucositis under Dosage and Administration.)

Consult manufacturer's labeling and/or other published guidelines (e.g., from National Comprehensive Cancer Network [NCCN]) for other strategies to prevent and manage mucositis.^{11 14}

Folate and Vitamin B₁₂ Supplementation

Folic acid and vitamin B₁₂ needed to prevent treatment-related hematologic and GI toxicity (i.e., mucositis).^{1 5} (See General under Dosage and Administration.) Use of these supplements associated with reduction in severity of GI toxicity.⁵

Fetal/Neonatal Morbidity and Mortality

May cause fetal harm; embryotoxicity, fetotoxicity, and fetal lethality demonstrated in animals.¹ Avoid pregnancy during therapy.¹ If used during pregnancy or if patient becomes pregnant, apprise of potential fetal hazard.¹

Hepatotoxicity

Elevated ALT/AST concentrations reported.¹ Perform liver function tests prior to the first and fourth doses of each treatment cycle.¹ If hepatotoxicity is grade 3 or greater, may need to omit and/or reduce subsequent dose or discontinue pralatrexate permanently.^{1 11} (See Table 3.)

Adequate Patient Evaluation and Monitoring

Administer under supervision of qualified clinicians experienced in the use of cytotoxic therapy.¹

Monitor CBCs, including platelet counts and ANCs, prior to initiation of therapy and weekly during therapy (i.e., just prior to each dose).¹

Assess for presence and severity of mucositis weekly during therapy (i.e., just prior to each dose).¹

Perform chemistry tests, including hepatic and renal function tests, prior to the first and fourth doses of each treatment cycle.¹

Specific Populations

Pregnancy

Category D.¹ (See Fetal/Neonatal Morbidity and Mortality under Cautions.)

Lactation

Not known whether pralatrexate is distributed into milk.¹ Discontinue nursing or the drug.¹

Pediatric Use

Safety and efficacy not established.¹

Geriatric Use

No overall differences in safety and efficacy relative to younger adults.¹ However, possible increased incidence of mucositis in patients ≥65 years of age compared with younger adults.¹¹

Age-related decline in renal function may result in reduced clearance of and increased exposure to pralatrexate.¹

Hepatic Impairment

Safety and efficacy not established.¹

Renal Impairment

Safety and efficacy not established.¹ However, pralatrexate clearance shown to decrease with declining Cl_cr.¹ Use with caution in patients with moderate or severe renal impairment.¹

Common Adverse Effects

Mucositis,¹ thrombocytopenia,^{1 3 4} nausea,¹ fatigue,¹ anemia,¹ constipation,¹ edema,¹ pyrexia.¹ cough,¹ epistaxis,¹ vomiting,¹ neutropenia,¹ diarrhea.¹

Interactions for Pralatrexate

No formal drug interactions studies to date.¹

Not a substrate, inhibitor, or inducer of CYP isoenzymes.¹

Not a substrate or inhibitor of the P-glycoprotein transport system.¹

Drugs Affecting or Metabolized by Hepatic Microsomal Enzymes

Pharmacokinetic interaction unlikely with drugs affecting or metabolized by CYP isoenzymes.¹

Drugs Eliminated by Renal Excretion

Possible pharmacokinetic interaction (delayed clearance of pralatrexate) with drugs that undergo substantial renal excretion.¹

Specific Drugs

Drug	Interaction
Co-trimoxazole	Possible delayed renal clearance of pralatrexate1
NSAIAs	Possible delayed renal clearance of pralatrexate1
Probenecid	Possible delayed clearance of and increased exposure to pralatrexate1

Pralatrexate Pharmacokinetics

Absorption

Bioavailability

Following rapid IV injection (30 mg/m² over 3–5 minutes) once weekly for 6 weeks in 7-week cycles, peak plasma concentration and AUC increased proportionally with dose.¹

Pharmacokinetics did not change significantly over multiple treatment cycles, and no accumulation of pralatrexate observed.¹

Distribution

Extent

Not known whether pralatrexate is distributed into milk.¹ (See Lactation under Cautions.)

Plasma Protein Binding

Approximately 67%.¹

Elimination

Metabolism

Not substantially metabolized by phase I CYP isoenzymes or phase II hepatic glucuronidases.¹

Elimination Route

Approximately 34% eliminated in urine as unchanged drug.¹

Half-life

12–18 hours.¹

Special Populations

Pharmacokinetics not studied in patients with hepatic impairment.¹

Clearance of pralatrexate decreases with decreasing Cl_cr.¹

Pharmacokinetics not substantially affected by gender.¹

Stability

Storage

Parenteral

Injection

2–8°C.¹ Store unopened vials in original carton to protect from light until used.¹ Once in syringe, use immediately.¹

Unopened vials stored in original carton at room temperature are stable for 72 hours.¹ Discard any vials stored at room temperature for >72 hours.¹

Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

Parenteral

Solution Compatibility

Y-Site Compatibility

Compatible
Sodium chloride 0.9%1

ActionsActions

• 
  

  Inhibits dihydrofolate reductase (DHFR); disrupts folate-dependent metabolic processes that are essential for cell replication, resulting in cytotoxicity against tumor cells.^{1 6 8 11}

  
  


• 
  

  Structural modification in the 10-position allows pralatrexate to selectively and efficiently enter cells expressing reduced-folate carrier type 1 (RFC-1)^{4 5 6 7 8 10 11} and to undergo enhanced intracellular polyglutamylation by the enzyme folylpolyglutamate synthetase (FPGS).^{6 7 8 11} In preclinical studies, pralatrexate demonstrated enhanced intracellular transport (due to greater affinity for RFC-1),⁴ increased intracellular drug retention and accumulation (due to enhanced polyglutamylation), and improved cytotoxicity compared with other folic acid antagonists (e.g., methotrexate, pemetrexed).^{6 7 8 9 10 11} Down-regulation and/or inhibition of effective RFC-1 transport and/or polyglutamylation have been proposed as possible mechanisms of resistance to methotrexate and other folic acid antagonists.^{8 15}

  
  

Advice to Patients

• 
  

  Importance of taking folic acid and vitamin B₁₂ to reduce the risk of adverse effects.^{1 13}

  
  


• 
  

  Risk of mucositis.¹ Importance of immediately informing clinicians of redness and/or soreness in the mucous membranes, including the mouth, lips, throat, and other areas along the GI tract and genital areas.^{11 13} Importance of understanding measures to prevent mucositis and to minimize discomfort should it occur.^{1 13}

  
  


• 
  

  Risk of thrombocytopenia, anemia, and neutropenia.¹ Importance of reporting any unusual bleeding (e.g., nosebleed), bruising, weakness, fatigue, pallor, shortness of breath, or fever or other manifestations of infection (e.g., chills, cough, pain or burning upon urination).¹³

  
  


• 
  

  Necessity of obtaining CBCs as well as renal and liver function tests periodically.¹

  
  


• 
  

  Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.^{1 13} Apprise patient of potential hazard to the fetus if used during pregnancy; women of childbearing potential should avoid becoming pregnant.¹

  
  


• 
  

  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription (e.g., co-trimoxazole, probenecid) and OTC drugs (e.g., NSAIAs), as well as any concomitant illnesses.^{1 13}

  
  


• 
  

  Importance of informing patients of other important precautionary information.¹ (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Pralatrexate

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Parenteral	Injection, for IV use only	20 mg/mL	Folotyn (available in single-dose vials)	Allos

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions February 2011. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. Allos Therapeutics, Inc. Folotyn (pralatrexate) injection prescribing information. Westminster, CO; 2009 Sep.

2. Food and Drug Administration. Orphan designation pursuant to Section 526 of the Federal Food and Cosmetic Act as amended by the Orphan Drug Act. (P.L. 97-414). Rockville, MD; From FDA website (); accessed 2009 Nov 3.

3. O'Connor O, Pro B, Pinter-Brown L et al. PROPEL; Results of the pivotal, multicenter, phase II study of pralatrexate in patients with relapsed or refractory peripheral T-cell lymphoma (PTCL). J Clin Oncol. 2009; 17(suppl): Abstract 8561 (presented at the 45th Annual ASCO meeting. Orlando, FL: 2009 May 29.

4. O'Connor OA, Horwitz S, Hamlin P et al. Phase II-I-II study of two different doses and schedules of pralatrexate, a high-affinity substrate for the reduced folate carrier, in patients with relapsed or refractory lymphoma reveals marked activity in T-cell malignancies. J Clin Oncol. 2009; 27:4357-64. [PubMed 19652067]

5. Mould DR, Sweeney K, Duffull SB et al. A population pharmacokinetic and pharmacodynamic evaluation of pralatrexate in patients with relapsed or refractory non-Hodgkin's or Hodgkin's lymphoma. Clin Pharmacol Ther. 2009; 86:190-6. [PubMed 19474785]

6. Molina JR. Pralatrexate, a dihydrofolate reductase inhibitor for the potential treatment of several malignancies. IDrugs. 2008; 11:508-21. [PubMed 18600598]

7. Kisliuk RL. Deaza analogs of folic acid as antitumor agents. Curr Pharm Des. 2003; 9:2615-25. [PubMed 14529545]

8. Izbicka E, Diaz A, Streeper R et al. Distinct mechanistic activity profile of pralatrexate in comparison to other antifolates in in vitro and in vivo models of human cancers. Cancer Chemother Pharmacol. 2009; 64:993-9. [PubMed 19221750]

9. Wang ES, O'Connor O, She Y et al. Activity of a novel anti-folate (PDX, 10-propargyl 10-deazaaminopterin) against human lymphoma is superior to methotrexate and correlates with tumor RFC-1 gene expression. Leuk Lymphoma. 2003; 44:1027-35. Abstract. [PubMed 12854905]

10. O'Connor OA, Hamlin PA, Portlock C et al. Pralatrexate, a novel class of antifol with high affinity for the reduced folate carrier-type 1, produces marked complete and durable remissions in a diversity of chemotherapy refractory cases of T-cell lymphoma. Br J Haematol. 2007; 139:425-8. [PubMed 17910632]

11. Allos Therapeutics, Inc., Westminster, CO: Personal communication.

12. Justice RL. Pralatrexate: FDA approval package. NDA number: 22-468. Rockville, MD: US Food and Drug Administration. From FDA website (). Accessed 2010 Jan 28.

13. Allos Therapeutics, Inc. Folotyn (pralatrexate) injection patient information. Westminster, CO. Accessed 2010 Feb 4.

14. Bensinger W, Schubert M, Ang KK et al. NCCN Task Force Report. prevention and management of mucositis in cancer care. J Natl Compr Canc Netw. 2008; 6 Suppl 1:S1-21. [PubMed 18289497]

15. Mauritz R, Peters GJ, Priest DG et al. Multiple mechanisms of resistance to methotrexate and novel antifolates in human CCRF-CEM leukemia cells and their implications for folate homeostasis. Biochem Pharmacol. 2002; 63:105-15. [PubMed 11841783]

More Pralatrexate resources

• Pralatrexate Side Effects (in more detail)
• Pralatrexate Use in Pregnancy & Breastfeeding
• Pralatrexate Drug Interactions
• Pralatrexate Support Group
• 0 Reviews for Pralatrexate - Add your own review/rating

• Pralatrexate Professional Patient Advice (Wolters Kluwer)


• Pralatrexate MedFacts Consumer Leaflet (Wolters Kluwer)


• Folotyn Prescribing Information (FDA)


• Folotyn Consumer Overview


• pralatrexate Intravenous Advanced Consumer (Micromedex) - Includes Dosage Information

Compare Pralatrexate with other medications

• Lymphoma
• Non-Hodgkin's Lymphoma
• Peripheral T-cell Lymphoma