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Thursday, August 2, 2012

Griseofulvin

Class: Antifungals, Miscellaneous
VA Class: AM700
CAS Number: 126-07-8
Brands: Grifulvin V, Gris-PEG

Introduction

Antifungal antibiotic produced by Penicillium.¹⁰⁴ ¹²⁵

Uses for Griseofulvin

Dermatophytoses

Treatment of dermatophytoses of the skin, scalp, and nails, including tinea barbae (ringworm of bearded areas of face and neck), tinea capitis (scalp ringworm), tinea corporis (ringworm of the body), tinea cruris (jock itch; groin ringworm), tinea pedis (athlete’s foot, foot ringworm), and tinea unguium (onychomycosis; nail ringworm) caused by Trichophyton, Microsporum, or Epidermophyton floccosum.¹⁰⁴ ¹²⁵

A drug of choice for treatment of tinea capitis;¹²⁴ ¹³¹ ¹³² ¹³³ ¹³⁵ ¹⁴⁰ ¹⁴¹ prolonged therapy usually is necessary to cure the infection and poor compliance may affect response to the drug.¹³¹ ¹³⁵ ¹³⁸ ¹⁴⁰ ¹⁴¹ Tinea barbae and tinea capitis generally require treatment with an oral antifungal.¹²⁴ ¹³¹ ¹³⁵ ¹³⁷ ¹⁴⁰

Tinea corporis and tinea cruris generally can be effectively treated using a topical antifungal; an oral antifungal may be necessary if the disease is extensive, dermatophyte folliculitis is present, the infection does not respond to topical therapy, or the patient is immunocompromised or has coexisting disease (e.g., diabetes mellitus).¹²⁴ ¹³⁰ ¹³¹ ¹³² ¹³³ ¹³⁴ ¹³⁶ ¹⁴⁰

While topical antifungals usually are effective for treatment of acute, uncomplicated tinea manuum and tinea pedis,¹²⁴ ¹³¹ ¹³² ¹³⁴ ¹³⁶ ¹⁴⁰ an oral antifungal usually is necessary for treatment of severe, chronic, or recalcitrant tinea pedis,¹²⁴ chronic moccasin-type (dry-type) tinea pedis, and for treatment of tinea unguium (onychomycosis).¹³¹ ¹³⁴ ¹³⁶ ¹⁴⁰

Griseofulvin Dosage and Administration

Administration

Oral Administration

Administer orally.¹⁰⁴ ¹²⁵

When microsize griseofulvin (Grifulvin V) tablets are used, absorption may be improved if given after a high-fat meal.¹²⁵

Dosage

Dosage varies depending on whether the drug is administered as griseofulvin microsize (Grifulvin V) or griseofulvin ultramicrosize (Gris-PEG).¹⁰⁴ ¹²⁴ ¹²⁵

Dosage and duration of treatment should be individualized according to the requirements and response of the patient.¹⁰⁴ ¹⁰⁴ Griseofulvin generally should be continued for ≥4–12 weeks for treatment of tinea capitis;¹⁰⁴ ¹²⁴ ¹²⁵ ¹³² ¹³³ ¹³⁵ ¹⁴⁰ ¹⁴¹ ≥2–4 weeks for treatment of tinea corporis;¹⁰⁴ ¹²⁴ ¹²⁵ ≥4–8 weeks for tinea pedis; and from 4–6 months to a year or longer for tinea unguium.¹⁰⁴ ¹²⁴ ¹²⁵

Pediatric Patients

Dermatophytoses

Microsize (Grifulvin V)

Oral

10–11 mg/kg daily, although dosages up to 20–25 mg/kg daily have been used.¹²⁴ ¹²⁵ ¹⁴⁰

Manufacturer suggests that those weighing approximately 14–23 kg may receive 125–250 mg daily and that those weighing >23 kg may receive 250–500 mg daily.¹²⁵

AAP recommends 10–20 mg/kg (maximum 1 g) daily in 1 or 2 doses.¹²⁴ For tinea capitis, AAP recommends 15–20 mg/kg once daily.¹²⁴

Ultramicrosize (Gris-PEG)

Oral

Children >2 years of age: Usually 7.3 mg/kg daily,¹⁰⁴ although dosages up to 10–15 mg/kg daily have been used.¹⁴⁰

Manufacturer suggests that those weighing approximately 16–27 kg may receive 125–187.5 mg daily and those weighing >27 kg may receive 187.5–375 mg daily.¹⁰⁴

AAP recommends 5–10 mg/kg (maximum 750 mg) once daily.¹²⁴

Adults

Dermatophytoses

Microsize (Grifulvin V)

Oral

500 mg daily for treatment of tinea capitis, tinea corporis, or tinea cruris.¹²⁵ For more difficult infections (e.g., tinea pedis, tinea unguium), 1 g daily.¹²⁵

Ultramicrosize (Gris-PEG)

Oral

375 mg once daily or in divided doses for treatment of tinea capitis, tinea corporis, or tinea cruris.¹⁰⁴ For more difficult infections (e.g., tinea pedis, tinea unguium), 750 mg daily given in divided doses.¹⁰⁴

Cautions for Griseofulvin

Contraindications

Hypersensitivity to griseofulvin.¹⁰⁴ ¹²⁵

Porphyria or hepatocellular failure.¹⁰⁴ ¹²⁵

Pregnant women.¹⁰⁴ ¹²⁵ (See Fetal/Neonatal Morbidity and Mortality under Cautions.)

Warnings/Precautions

Warnings

Fetal/Neonatal Morbidity and Mortality

May cause fetal toxicity when administered to pregnant women.¹⁰¹ ¹⁰⁴ ¹¹¹ ¹¹⁷ ¹¹⁸ ¹²⁵

Some animal studies indicate that griseofulvin may be embryotoxic and teratogenic.¹⁰¹ ¹⁰⁴ ¹⁰⁶ ¹¹³ ¹¹⁴ ¹¹⁵ ¹¹⁶ ¹²⁵ There have been 2 cases of conjoined twins born to women who received griseofulvin during the first trimester of pregnancy; some women who received the drug during pregnancy reportedly have had spontaneous abortions or delivered infants with other congenital malformations.¹⁰¹ ¹⁰⁴ ¹¹¹ ¹¹⁷ ¹¹⁸ ¹⁰⁴ ¹²⁵

Griseofulvin should not be used in women who are pregnant¹⁰⁴ ¹²⁵ or intend to become pregnant within 1 month after treatment.¹²⁵

Women should use additional contraceptive precautions during griseofulvin treatment and for 1 month after the drug is discontinued.¹²⁵ One manufacturer recommends that men wait at least 6 months after completing griseofulvin treatment before fathering a child.¹²⁵

If a patient becomes pregnant while receiving griseofulvin, they should be advised of the potential hazard to the fetus.¹⁰⁴

Sensitivity Reactions

Hypersensitivity Reactions

Hypersensitivity reactions (e.g., rash, urticaria, erythema multiforme-like reactions, angioneurotic edema) have been reported.¹⁰⁴

Because griseofulvin is derived from Penicillium, there is a possibility of cross-sensitivity with penicillin.¹⁰⁴ ¹²⁵ Patients with known penicillin hypersensitivity have received griseofulvin without such reactions.¹⁰⁴ ¹²⁵

If hypersensitivity reaction occurs, discontinue griseofulvin and initiate appropriate therapy.¹⁰⁴

Photosensitivity Reactions

Photosensitivity reactions have been reported.¹⁰⁴ ¹²⁵ Lupus erythematosus may be aggravated if a photosensitivity reaction occurs.¹²⁵

Avoid exposure to intense natural or artificial sunlight during griseofulvin treatment.¹⁰⁴

General Precautions

Selection and Use of Antifungals

Prior to administration of griseofulvin for dermatophytoses, diagnosis should be confirmed either by direct microscopic examination of scrapings from infected tissue mounted in potassium hydrochloride (KOH) or by culture.¹⁰⁴ ¹²⁵

Should not be used for treatment of minor or trivial dermatophytoses that may respond to topical antifungals alone.¹⁰⁴ ¹²⁵

General hygiene measures should be observed to control sources of infection or reinfection.¹⁰⁴ ¹²⁵ Concomitant use of topical antifungals or antibacterials may be required, particularly for treatment of tinea pedis (athlete’s foot, foot ringworm).¹⁰⁴ ¹²⁵ In some forms of tinea pedis, yeasts and bacteria may also be involved and griseofulvin is ineffective against these organisms.¹⁰⁴ ¹²⁵

Not effective and should not be used for treatment of pityriasis (tinea) versicolor or cutaneous Candida infections.¹⁰⁴ ¹²⁵ ^a

Not effective and should not be used for treatment of systemic fungal infections, including blastomycosis, candidiasis, chromoblastomycosis, coccidioidomycosis, cryptococcosis, histoplasmosis, or sporotrichosis.¹⁰⁴ ¹²⁵ ^a Safety and efficacy not established for prevention of fungal infections.¹⁰⁴ ¹²⁵

Not effective and should not be used for treatment of bacterial infections, including actinomycosis or nocardiosis.¹⁰⁴ ¹²⁵

Laboratory Monitoring

Periodically assess organ system functions, including renal, hepatic, and hematopoietic, during prolonged therapy.¹⁰⁴ ¹²⁵

Specific Populations

Pregnancy

Category C.^b (See Fetal/Neonatal Morbidity and Mortality under Cautions.)

Pediatric Use

Safety and efficacy of ultramicrosize griseofulvin not established in children ≤2 years of age.¹⁰⁴ Microsize griseofulvin has been used in children as young as 3 months of age.¹³⁸

Hepatic Impairment

Contraindicated in patients with hepatocellular failure.¹⁰⁴

Common Adverse Effects

Hypersensitivity reactions (rash, urticaria); GI effects (oral thrush, nausea, vomiting, epigastric distress, diarrhea); CNS effects (headache, fatigue, dizziness, insomnia, mental confusion, impaired performance of routine activities).¹⁰⁴ ¹²⁵

Interactions for Griseofulvin

Specific Drugs

Drug	Interaction	Comments
Alcohol	Tachycardia, flushing, and potentiation of alcohol effects has been reported in patients receiving griseofulvin¹⁰⁴ ^a	Although clinical importance is unclear, some clinicians suggest that patients be warned of a possible reaction and to avoid alcohol during griseofulvin therapy^a
Anticoagulants, oral (warfarin)	Decreased PT reported¹⁰⁴ ¹²⁵ ^a	Use concomitantly with caution; adjust anticoagulant dosage if needed during and after griseofulvin treatment¹⁰⁴ ¹²⁵ ^a
Aspirin	Possible decreased plasma salicylate concentrations¹²⁷
Barbiturates	Possible decreased antifungal activity¹⁰⁴ ¹²⁵ Phenobarbital: Possible decreased griseofulvin concentrations^a	Dosage adjustment of griseofulvin may be necessary¹⁰⁴ ¹²⁵ Phenobarbital: Avoid concomitant use;^a if concomitant use is necessary, administer griseofulvin in 3 divided doses daily to maximize absorption, monitor griseofulvin concentrations, and adjust dosage of the antifungal if necessary^a
Cyclosporine	Possible decreased concentrations of cyclosporine¹²⁸
Hormonal contraceptives (oral contraceptives)	Amenorrhea, increased breakthrough bleeding, and possibility of decreased contraceptive efficacy reported with concomitant use¹⁰⁰ ¹⁰⁴ ¹⁰⁵ ¹²⁵	The possibility of decreased contraceptive efficacy should be considered if griseofulvin is used concomitantly¹⁰⁰ ¹⁰⁵ ¹²⁹
Theophylline	Increased clearance and decreased theophylline half-life reported in some patients; extent of this interaction appears to vary and increased clearance of theophylline is not evident in all individuals who receive the drugs concomitantly¹²⁶

Griseofulvin Pharmacokinetics

Absorption

Bioavailability

Absorption of microsize griseofulvin is variable¹²⁵ and unpredictable and ranges from 25–70% of an oral dose;^a peak serum concentrations attained 4 hours after a dose.¹²⁵

Ultramicrosize griseofulvin is almost completely absorbed following oral administration.^a

Food

Absorption of microsize griseofulvin may be enhanced by administration after a high-fat meal.¹²⁵ ^a

Distribution

Extent

Following oral absorption, griseofulvin is concentrated in skin, hair, nails, liver, fat, and skeletal muscles.^a The drug can be detected in the outer layers of the stratum corneum soon after ingestion.^a

Griseofulvin is deposited in keratin precursor cells and has greater affinity for diseased tissue.¹⁰⁴ The drug is tightly bound to new keratin.¹⁰⁴

Griseofulvin concentrations in skin are higher in warm climates than in cold, possibly because the drug is dissolved in perspiration and deposited in the horny layer of skin when perspiration evaporates.^a This explanation has also been used to account for the reversed concentration gradient of the drug in skin; highest concentrations are found in the outermost horny layer, while concentrations are much lower in deeper layers.^a

Elimination

Metabolism

Oxidatively demethylated and conjugated with glucuronic acid, principally in the liver.^a The major metabolite, 6-desmethylgriseofulvin, is microbiologically inactive.^a

Elimination Route

About 30% of a single oral dose of microsize griseofulvin is excreted in urine within 24 hours as 6-desmethylgriseofulvin and its glucuronide conjugate; 50% of the dose is excreted in urine within 5 days.^a Unchanged griseofulvin in the urine accounts for <1% of the administered drug.^a Approximately one-third of a single dose of microsize griseofulvin is excreted in feces within 5 days.^a Griseofulvin also is excreted in perspiration.^a

Half-life

9–24 hours.^a

Stability

Storage

Oral

Tablets

Microsize or ultramicrosize: 15–30°C in tight, light-resistant container.¹⁰⁴ ¹²⁵

Suspension

Microsize: Room temperature in tight, light-resistant container.¹²⁵

Actions and SpectrumActions

Structurally unrelated to other antifungals (e.g., allylamines, azoles, echinocandins, polyenes, pyrimidines).^a

Usually fungistatic in action.¹⁰⁴ ¹²⁵ ^a

Antifungal activity principally involves disruption of the fungal cell’s mitotic spindle structure.^a Although the effect on mitosis is similar to that caused by colchicine, a different mechanism is probably involved.^a Griseofulvin may cause production of defective DNA which is unable to replicate.^a

Griseofulvin is deposited in keratin precursor cells and is tightly bound to new keratin, resulting in an environment unfavorable for fungal invasion.¹⁰⁴ ¹²⁵ ^a Infected skin, hair, or nails are then replaced with tissue not infected with the dermatophyte.¹²⁵ ^a

Limited spectrum of antifungal activity.¹⁰⁴ ¹²⁵ ^a Active against most dermatophytes, but not active against yeasts or other fungi, including Aspergillus, Blastomyces, Candida, Cryptococcus, Coccidioides, Histoplasma, Saccharomyces, Sporotrichum, or Malassezia furfur (Pityrosporum orbiculare).¹⁰⁴ ¹²⁵ ^a

Dermatophytes: Active against Epidermophyton floccosum, Microsporum audouini, M. canis, M. gypseum, Trichophyton crateriform, T. gallinae, T. interdigitalis, T. megnini, T. mentagrophytes, T. rubrum, T. schoenleinii, T. sulphureum, T. tonsurans, and T. verrucosum.¹⁰⁴ ¹²⁵

Advice to Patients

Importance of using griseofulvin for the full, prescribed treatment period, even if symptoms improve; importance of consulting with clinician if the condition does not improve after a full course of therapy.

Advise patients to avoid exposure to intense natural or artificial sunlight during griseofulvin treatment since photosensitivity reactions can occur.¹⁰⁴ ¹²⁵

Importance of discontinuing use and contacting clinician if signs or symptoms of sensitization occur (e.g., rash, urticaria).¹⁰⁴ ¹²⁵

Importance of informing clinicians of existing or contemplated therapy, including prescription and OTC drugs, as well as any concomitant illnesses.

Importance of women informing clinicians if they are or plan to become pregnant or to breast-feed. (See Fetal/Neonatal Morbidity and Mortality under Cautions.)

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

Preparations

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

Griseofulvin Microsize
Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Suspension	125 mg/5 mL	Grifulvin V (with alcohol 0.2% parabens and propylene glycol)	Ortho-Neutrogena
	Tablets	500 mg	Grifulvin V (scored)	Ortho-Neutrogena

Griseofulvin Ultramicrosize
Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Tablets, film-coated	125 mg	Gris-PEG (with methylparaben; scored)	Pedinol
		250 mg	Gris-PEG (with methylparaben and povidone; scored)	Pedinol

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 03/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Grifulvin V 500MG Tablets (ORTHO DERM): 30/$139.98 or 90/$395.99

Griseofulvin Microsize 125MG/5ML Suspension (PATRIOT PHARMACEUTICALS LLC): 120/$42.99 or 360/$115.98

Gris-PEG 125MG Tablets (PEDINOL): 90/$196 or 270/$555.97

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 July 2006. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

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102. Madhok R, Zoma A, Capell H. Fatal exacerbation of systemic lupus erythematosus after treatment with griseofulvin. BMJ. 1985; 291:249-50. [IDIS 203029] [PubMed 3926142]

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104. Pedinol Pharmacal. Gris-PEG (griseofulvin ultramicrosize) tablets prescribing information. In: Physician’s desk reference. 56th ed. Montvale, NJ: Medical Economics Company Inc; 2002:2661-2.

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112. Knudsen LB. No association between griseofulvin and conjoined twinning. Lancet. 1987; 2:1097. [PubMed 2890014]

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More Griseofulvin resources

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

Griseofulvin Prescribing Information (FDA)

Griseofulvin Professional Patient Advice (Wolters Kluwer)

Griseofulvin Microsize Oral Suspension MedFacts Consumer Leaflet (Wolters Kluwer)

griseofulvin Concise Consumer Information (Cerner Multum)

griseofulvin Advanced Consumer (Micromedex) - Includes Dosage Information

Gris-PEG Prescribing Information (FDA)

Gris-PEG Ultramicrosize Tablets MedFacts Consumer Leaflet (Wolters Kluwer)

Grisactin 250 Concise Consumer Information (Cerner Multum)

Compare Griseofulvin with other medications

Dermatophytosis
Onychomycosis, Fingernail
Onychomycosis, Toenail
Tinea Barbae
Tinea Capitis
Tinea Corporis
Tinea Cruris
Tinea Pedis

Wednesday, August 1, 2012

Permapen Isoject

penicillin G benzathine

Dosage Form: Injectable Suspension 1,200,000 units

STORE BETWEEN 2°–8°C (36°–46°F)

SHAKE WELL BEFORE USING

Permapen Isoject Description

Permapen® (Penicillin G Benzathine) Injectable Suspension, a sterile antibacterial agent, is a repository penicillin compound which provides blood levels for long periods following its intramuscular injection. This property is the result of its extremely low solubility in water. Each milliliter contains 600,000 units of penicillin G benzathine; 0.006 grams sodium citrate; 0.003 grams polyvinylpyrrolidone; 0.010 grams lecithin, and 0.003 grams sodium carboxymethylcellulose in an aqueous suspension. Permapen also contains methylparaben 0.09% and propylparaben 0.01% as preservatives.

Chemically, Permapen is 3,3-dimethyl-7-oxo-6-(2-phenylacetamido)-4 thia-l azabicyclo [3.2.0] heptane-2-carboxylic acid compound with N,N'-dibenzylethylenediamine (2:1) tetrahydrate. It is prepared by the reaction of dibenzyl-tetrahydrate-ethylenediamine with 2 molecules of penicillin G.

It has a molecular weight of 981.19 and the following chemical structure:

Formula

C16H20N2•2C16Hl8N2O4S•4H2O

Penicillin G benzathine occurs as a white crystalline powder and is very slightly soluble in water.

The pH of the injectable suspension is between 5.0–7.5.

Permapen Isoject - Clinical Pharmacology

Intramuscular penicillin G benzathine is absorbed very slowly into the blood stream from the intramuscular site and converted by hydrolysis to penicillin G. This combination of hydrolysis and slow absorption results in blood serum levels much lower than those of other parenteral penicillins.

Approximately 60% of penicillin G is bound to serum protein. The drug is distributed throughout the body tissues in widely varying amounts. Highest levels are found in the kidneys with lesser amounts in the liver, skin, and intestines. Penicillin G penetrates into all other tissues and the spinal fluid to a lesser degree. With normal kidney function the drug is excreted rapidly by tubular excretion. A small amount is secreted into the bile. In neonates and young infants, and in individuals with impaired kidney function, excretion is considerably delayed.

Microbiology

Penicillin G exerts a bactericidal action against penicillin-susceptible microorganisms during the stage of active multiplication. It acts through the inhibition of biosynthesis of cell wall mucopeptide. It is not active against the penicillinase-producing bacteria, which includes many strains of staphylococci.

While in vitro studies have demonstrated the susceptibility of most strains of the following organisms, clinical efficacy for infections other than those included in the INDICATIONS AND USAGE section has not been documented. Penicillin G exerts high in vitro activity against staphylococci (except penicillinase-producing strains), streptococci (groups A, C, G, H, L, and M), and pneumococci. Other organisms sensitive to penicillin G are: Corynebacterium diphtheriae, Bacillus anthracis, Clostridia, Actinomyces bovis, Streptobacillus moniliformis, Listeria monocytogenes, and Leptospira. Treponema pallidum is extremely sensitive to the bactericidal action of penicillin G.

Penicillin acts synergistically with gentamicin or tobramycin against many strains of enterococci.

Indications and Usage for Permapen Isoject

Intramuscular penicillin G benzathine is indicated in the treatment of infections in both children and adults due to penicillin G-susceptible microorganisms that are susceptible to the low and very prolonged serum levels common to this particular dosage form in the indications listed below. Therapy should be guided by clinical response.

Note: When high sustained serum levels are required, injectable penicillin G either IM or IV should be used.

The following infections will usually respond to adequate dosages of intramuscular penicillin G benzathine:

Upper Respiratory Tract (pharyngitis): streptococci (group A – without bacteremia).

Venereal Infections: Syphilis

Yaws, bejel, and pinta.

Medical Conditions in Which Penicillin G Benzathine Therapy is Indicated As Prophylaxis

Rheumatic fever and/or chorea: Prophylaxis with penicillin G benzathine has proven effective in preventing recurrence of these conditions. It has also been used as follow-up prophylactic therapy for rheumatic heart disease and acute glomerulonephritis.

Contraindications

A history of a previous hypersensitivity reaction to any penicillin is a contraindication.

Warnings

Serious and occasionally fatal hypersensitivity (anaphylactoid) reactions have been reported in patients on penicillin therapy. These reactions are more likely to occur in individuals with a history of penicillin hypersensitivity and/or a history of sensitivity to multiple allergens. There have been reports of individuals with a history of penicillin hypersensitivity who have experienced severe reactions when treated with cephalosporins. Before initiating therapy with any penicillin, careful inquiry should be made concerning previous hypersensitivity reactions to penicillin, cephalosporins, and other allergens. If an allergic reaction occurs, the drug should be discontinued and the appropriate therapy instituted. Serious anaphylactoid reactions require immediate emergency treatment with epinephrine. Oxygen, intravenous steroids, and airway management–including intubation, should be administered as indicated.

Precautions

General

Penicillin should be used with caution in individuals with histories of significant allergies and/or asthma.

Intramuscular therapy: Care should be taken to avoid intravenous administration, accidental intraarterial administration, or injection into or near major peripheral nerves or blood vessels, since many injections may produce neurovascular damage.

As with all intramuscular preparations, penicillin G benzathine should be injected well within the body of a relatively large muscle.

ADULTS: The preferred site is the upper outer quadrant of the buttock (i.e., gluteus maximus), or the mid-lateral thigh.

CHILDREN: It is recommended that intramuscular injections be given preferably in the mid-lateral muscles of the thigh. In infants and small children the periphery of the upper outer quadrant of the gluteal region should be used only when necessary, such as in burn patients, in order to minimize the possibility of damage to the sciatic nerve.

The deltoid area should be used only if well developed such as in certain adults and older children, and then only with caution to avoid radial nerve injury. Intramuscular injections should not be made into the lower and mid-third of the upper arm. As with all intramuscular injections, aspiration is necessary to help avoid inadvertent injection into a blood vessel.

Irritation at the site of injection may occur. In addition, subcutaneous and fat–layer injections should be avoided since they may cause pain and induration. If these occur, they may be relieved by the application of an ice pack.

In streptococcal infections, therapy must be sufficient to eliminate the organism (10 days minimum), otherwise the sequelae of streptococcal disease may occur. Cultures should be taken following completion of treatment to determine whether streptococci have been eradicated.

The use of antibiotics may result in overgrowth of nonsusceptible organisms. Constant observation of the patient is essential. If new infections due to bacteria or fungi appear during therapy, the drug should be discontinued and appropriate measures taken. Whenever allergic reactions occur, penicillin should be withdrawn unless, in the opinion of the physician, the condition being treated is life threatening and amenable only to penicillin therapy.

Laboratory Tests

In prolonged therapy with penicillin, periodic evaluation of the renal, hepatic and hematopoietic systems for organ dysfunction is recommended. This is particularly important in prematures, neonates and other infants, and when high doses are used.

When treating gonococcal infections in which primary and secondary syphilis are suspected, proper diagnostic procedures, including dark field examinations, should be done before receiving penicillin and monthly serological tests made for at least four months. All cases of penicillin-treated syphilis should receive clinical and serological examinations every six months for two to three years.

In streptococcal infections, cultures should be taken following completion of treatment to determine whether streptococci have been eradicated.

Drug Interactions

Concurrent administration of bacteriostatic antibiotics (e.g., erythromycin, tetracycline) may diminish the bactericidal effects of penicillins by slowing the rate of bacterial growth. Bactericidal agents work most effectively against the immature cell wall of rapidly proliferating microorganisms. This has been demonstrated in vitro; however, the clinical significance of this interaction is not well documented. There are few clinical situations in which the concurrent use of "static" and "cidal" antibiotics are indicated. However, in selected circumstances in which such therapy is appropriate, using adequate doses of antibacterial agents and beginning penicillin therapy first, should minimize the potential for interaction.

Penicillin blood levels may be prolonged by concurrent administration of probenecid which blocks the renal tubular secretion of penicillins.

Displacement of penicillins from plasma protein binding sites will elevate the level of free penicillin in the serum.

Carcinogenesis, Mutagenesis, Impairment of Fertility

No information or long term studies are available on the carcinogenesis, mutagenesis, or impairment of fertility with the use of penicillins.

Pregnancy

Pregnancy Category B – Teratogenic Effects

Reproduction studies in the mouse, rat and rabbit have revealed no evidence of impaired fertility or harm to the fetus due to penicillin G. Human experience with the penicillins during pregnancy has not shown any positive evidence of adverse effects on the fetus. There are, however, no adequate and well controlled studies in pregnant women showing conclusively that harmful effects of these drugs on the fetus can be excluded. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

Nursing Mothers

Pencillin G benzathine has been reported in milk. Caution should be exercised when penicillin G benzathine is administered to a nursing woman.

Pediatric Use

Pencillins are excreted largely unchanged by the kidney. Because of incompletely developed renal function in infants, the rate of elimination will be slow. Use caution in administering to newborns and evaluate organ system function frequently.

Adverse Reactions

The hypersensitivity reactions reported are skin eruptions (maculopapular to exfoliative dermatitis), urticaria and other serum sickness reactions, laryngeal edema and anaphylaxis. Fever and eosinophilia may frequently be the only reaction observed. Hemolytic anemia, leucopenia, thrombocytopenia, neuropathy, and nephropathy are infrequent reactions and usually associated with high doses of parenteral penicillin.

Overdosage

Penicillin in overdosage has the potential to cause neuromuscular hyperirritability. In case of overdosage discontinue medication, treat symptomatically, and institute supportive measures as required.

Penicillin G is hemodialyzable.

Permapen Isoject Dosage and Administration

Administer by deep IM injection in the upper outer quadrant of the buttock. In infants and small children, the mid-lateral aspect of the thigh may be preferable. When doses are repeated, vary the injection site (see PRECAUTIONS).

Pediatric Dosage Schedule

In children under 12 years of age, dosage should be adjusted in accordance with the age and weight of the child and the severity of the infection. Under 2 years of age, the dose may be divided between the two buttocks if necessary.

Streptococcal Infections (group A) pharyngitis

A single injection of 900,000 units for older children; l,200,000 units for adults.

Venereal Infections

Syphilis

Primary, secondary, and latent: 2.4 million units (1 dose).

Late Syphilis (tertiary and neurosyphilis)

3 million units at 7 day intervals for a total of 6–9 million units.

Congenital Syphilis (asymptomatic with normal cerebrospinal fluid)

Under 2 years of age–50,000 units/kg body weight in a single dose; ages 2–12 years–adjust dosage based on adult dosage schedule.

Yaws, Bejel, and Pinta

1.2 million units (1 injection).

Prophylaxis

For rheumatic fever and glomerulonephritis.

Following an acute attack, penicillin G benzathine (parenteral) may be given in doses of 1,200,000 units once a month or 600,000 units every 2 weeks.

Parenteral drug products should be visually inspected for particulate matter and discoloration prior to administration, whenever solution and container permit.

How is Permapen Isoject Supplied

Permapen (Penicillin G Benzathine) Injectable Suspension is supplied in an ISOJECT syringe: 1,200,000 units in packages of 10 (NDC 0049-0210-35). ISOJECT is a pre-filled disposable syringe unit with a 20-gauge, 1¼ inch needle. Each 2 mL contains 1,200,000 units penicillin G benzathine; 0.0l2 g sodium citrate; 0.006 g polyvinylpyrrolidone; 0.020 g lecithin, and 0.006 g sodium carboxymethylcellulose. Preservatives: methylparaben 0.09%, propylparaben 0.01%.

The product should be stored between 2°–8°C (36°–46°F). Keep from freezing.

Rx only

23-1173-00-3

PERMAPEN
penicillin g benzathine injection, suspension

Product Information
Product Type	HUMAN PRESCRIPTION DRUG	NDC Product Code (Source)	0049-0210
Route of Administration	INTRAMUSCULAR	DEA Schedule

INGREDIENTS
Name (Active Moiety)	Type	Strength
penicillin G benzathine (penicillin)	Active	600000 UNITS In 1 MILLILITER
sodium citrate	Inactive
polyvinylpyrrolidone	Inactive
lecithin	Inactive
sodium carboxymethylcellulose	Inactive
methylparaben	Inactive
propylparaben	Inactive

Product Characteristics
Color		Score
Shape		Size
Flavor		Imprint Code
Contains

Packaging
#	NDC	Package Description	Multilevel Packaging
1	0049-0210-35	10 SYRINGE In 1 PACKAGE	contains a SYRINGE
1		2 mL (MILLILITER) In 1 SYRINGE	This package is contained within the PACKAGE (0049-0210-35)

Revised: 04/2006Roerig

More Permapen Isoject resources

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

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Actinomycosis
Anthrax
Anthrax Prophylaxis
Aspiration Pneumonia
Bacterial Infection
Clostridial Infection
Congenital Syphilis
Cutaneous Bacillus anthracis
Deep Neck Infection
Diphtheria
Endocarditis
Fusospirochetosis, Trench Mouth
Joint Infection
Leptospirosis
Lyme Disease, Arthritis
Lyme Disease, Carditis
Lyme Disease, Erythema Chronicum Migrans
Lyme Disease, Neurologic
Meningitis
Meningitis, Meningococcal
Meningitis, Pneumococcal
Neurosyphilis
Otitis Media
Pneumonia
Prevention of Perinatal Group B Streptococcal Disease
Rat-bite Fever
Rheumatic Fever Prophylaxis
Skin Infection
Strep Throat
Syphilis, Early
Syphilis, Latent
Tertiary Syphilis
Tonsillitis/Pharyngitis
Upper Respiratory Tract Infection

Monurol

Generic Name: Fosfomycin Tromethamine
Class: Urinary Anti-infectives
VA Class: AM900
Chemical Name: (1R,2S)-(1,2-Epoxypropyl)phosphonic acid, compound with 2-amino-2-(hydroxymethyl)-1,3-propanediol (1:1)
Molecular Formula: C₃H₇O₄P•C₄H₁₁N O₁₃
CAS Number: 78964-85-9

Introduction

Antibacterial; phosphonic acid derivative.¹

Uses for Monurol

Urinary Tract Infections (UTIs)

Treatment of uncomplicated UTIs (acute cystitis) in women when UTIs are caused by susceptible Escherichia coli or Enterococcus faecalis (formerly Streptococcus faecalis).¹ ² ³ ⁴ ⁵

Do not use for treatment of pyelonephritis or perinephric abscesses.¹

If persistence or reappearance of bacteriuria occurs after fosfomycin treatment, do not repeat treatment; select another anti-infective.¹

Monurol Dosage and Administration

Administration

Oral Administration

Administer orally.¹

May be taken with or without food.¹

Prepare oral solution by adding contents of a single-dose packet (sachet) containing 3 g of the drug to 90–120 mL of water;¹ do not use hot water.¹ Ingest immediately after preparation.¹

Do not administer as dry granules.¹

Dosage

Available as fosfomycin tromethamine; dosage expressed in terms of fosfomycin.¹

Adults

Urinary Tract Infections (UTIs)

Uncomplicated UTIs

Oral

3 g as a single dose.¹

Special Populations

Hepatic Impairment

No specific dosage recommendations at this time.¹

Renal Impairment

Dosage adjustment not necessary.⁶ (See Pharmacokinetics.)

Geriatric Patients

Dosage adjustment not necessary.¹ (See Geriatric Use under Cautions.)

Cautions for Monurol

Contraindications

Known hypersensitivity to fosfomycin or any ingredient in the formulation.¹

Warnings/Precautions

General Precautions

Retreatment

Do not use more than a single dose to treat a single episode of acute cystitis; repeated daily doses do not enhance efficacy and increase incidence of adverse events.¹

Selection and Use of Anti-infectives

Obtain urine specimens for culture and in vitro susceptibility testing before and after completion of therapy.¹

To reduce development of drug-resistant bacteria and maintain effectiveness of fosfomycin and other antibacterials, use only for treatment of infections proven or strongly suspected to be caused by susceptible bacteria.¹

Specific Populations

Pregnancy

Category B.¹

Lactation

Not known whether distributed into breast milk.¹

Potential for serious adverse reactions in nursing infants; discontinue nursing or do not administer drug.¹

Pediatric Use

Safety and efficacy not established in children ≤12 years of age.¹ Manufacturer make no specific dosage recommendations for pediatric patients.¹

Geriatric Use

Insufficient experience in those ≥65 years of age to determine whether they respond differently than younger adults.¹ No evidence of substantial differences in safety and efficacy relative to younger adults.¹

Although dosage adjustment not usually necessary, select dosage with caution because of age-related decreases in hepatic, renal, and/or cardiac function and potential for concomitant disease and drug therapy.¹

Common Adverse Effects

Diarrhea.¹

Interactions for Monurol

Drugs that Increase GI Motility

May decrease serum and urine concentrations of fosfomycin.¹

Specific Drugs

Drug	Interaction	Comments
Cimetidine	Pharmacokinetics of fosfomycin not affected¹
Metoclopramide	Decreased serum concentrations and decreased urinary excretion of fosfomycin¹

Monurol Pharmacokinetics

Absorption

Bioavailability

Fosfomycin tromethamine is rapidly absorbed following oral administration and converted to the free acid, fosfomycin.¹ Peak serum concentrations attained within 2–4 hours.¹

Food

Food decreases oral bioavailability;¹ bioavailability is 37% and 30% under fasting and fed conditions, respectively.¹

Cumulative amount of drug excreted in urine is similar whether the drug is given with or without food.¹

Distribution

Extent

Distributed to kidneys, bladder wall, prostate, and seminal vesicles.¹

Crosses the placenta.¹

Plasma Protein Binding

Not bound to plasma proteins.¹

Elimination

Elimination Route

Eliminated unchanged in urine (38% of an oral dose) and feces (18% of an oral dose).¹

Peak urine concentrations achieved within 2–4 hours or 6–8 hours under fasting or fed conditions, respectively; cumulative amount excreted in urine is similar.¹

Half-life

5.7 hours.¹

Special Populations

Geriatric adults: Pharmacokinetics similar to that reported in younger adults.¹

Renal impairment: Decreased elimination and prolonged half-life.¹ Half-life ranges up to 50 hours in patients with renal impairment.¹

Stability

Storage

Oral

Powder

25°C (may be exposed to 15–30°C).¹

Actions and SpectrumActions

Phosphonic acid derivative,⁵ synthetic antibacterial agent.¹

Bactericidal in urine when administered in therapeutic doses.¹ ⁵

Antibacterial activity results from interference with bacterial cell wall synthesis by inhibiting the enzyme enolpyruvyl transferase that catalyzes the formation of uridine diphosphate-N-acetylmuramic acid in the first step of bacterial cell wall synthesis.¹ ⁴ ⁵ Also reduces adherence of bacteria to uroepithelial cells.¹ ⁵

Active in vitro against a broad spectrum of gram-negative and gram-positive bacteria, including those commonly associated with uncomplicated UTIs.¹ ⁴ ⁵ Active in vitro and in vivo against Escherichia coli and Enterococcus faecalis.¹

Cross-resistance generally does not occur between fosfomycin and other antibacterial agents (e.g., β-lactams, aminoglycosides).¹

Advice to Patients

Importance of diluting granules with water (not hot water) just prior to administration.¹

Advise patient that fosfomycin may be taken with or without food.¹

Importance of contacting clinician if UTI symptoms do not improve within 2–3 days after treatment.¹

Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.¹

Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.¹

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.

Fosfomycin Tromethamine
Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	For solution	3 g (of fosfomycin) per packet	Monurol Sachet	Forest

Comparative Pricing

Monurol 3GM Packet (FOREST): 1/$50.86 or 3/$139.89

Disclaimer

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions January 2008. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. Forest Pharmaceuticals, Inc. Monurol (fosfomycin tromethamine) powder prescribing information. St. Louis, MO; 2004 May.

2. Elhanan G, Tabenkin H, Yahalom R et al. Single-dose fosfomycin trometamol versus 5-day cephalexin regimen for treatment of uncomplicated lower urinary tract infections in women. Antimicrob Agents Chemother. 1994; 38:2612-4. [IDIS 337800] [PubMed 7872756]

3. Selvaggi FP, Ditonno P, Traficante A et al. Fosfomycin trometamol (Monuril) versus norfloxacin in single dose for adult female uncomplicated UTIs: multicenter randomized, double-blind study. Chemotherapy. 1990; 36(Suppl 1):31-3. [IDIS 297402] [PubMed 2085986]

4. Reeves DS. Fosfomycin trometamol. J Antimicrob Chemother. 1994; 34:853-8. [IDIS 343321] [PubMed 7730229]

5. Patel SS, Balfour JA, Bryson HM. Fosfomycin tromethamine: a review of its antibacterial activity, pharmacokinetic properties and therapeutic efficacy as a single-dose oral treatment for acute uncomplicated lower urinary tract infections. Drugs. 1997; 53:637-56. [PubMed 9098664]

6. Forest Pharmaceuticals, Inc, St. Louis, MO: Personal communication.

More Monurol resources

Monurol Side Effects (in more detail)
Monurol Use in Pregnancy & Breastfeeding
Monurol Drug Interactions
Monurol Support Group
1 Review for Monurol - Add your own review/rating

Monurol Prescribing Information (FDA)

Monurol Concise Consumer Information (Cerner Multum)

Monurol Advanced Consumer (Micromedex) - Includes Dosage Information

Monurol MedFacts Consumer Leaflet (Wolters Kluwer)

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Bladder Infection
Transurethral Prostatectomy

Tuesday, July 31, 2012

Loprox Cream

Dosage Form: cream

FOR DERMATOLOGIC USE ONLY.

NOT FOR USE IN EYES.

Rx Only

Loprox Cream Description

Loprox® Cream (ciclopirox) 0.77% is for topical use.

Each gram of LOPROX® Cream contains 7.70 mg of ciclopirox (as ciclopirox olamine) in a water miscible vanishing cream base consisting of Purified Water USP, Cetyl Alcohol NF, Light Mineral Oil NF, Octyldodecanol NF, Stearyl Alcohol NF, Polysorbate 60 NF, Myristyl Alcohol, Sorbitan Monostearate NF, Lactic Acid USP, and Benzyl Alcohol NF (1%) as preservative.

LOPROX® Cream contains a synthetic, broad-spectrum, antifungal agent ciclopirox (as ciclopirox olamine). The chemical name is 6-cyclohexyl-1-hydroxy-4-methyl-2(1H)-pyridone, 2-aminoethanol salt.

The CAS Registry Number is 41621-49-2. The chemical structure is:

Loprox Cream - Clinical Pharmacology

Ciclopirox is a broad-spectrum, antifungal agent that inhibits the growth of pathogenic dermatophytes, yeasts, and Malassezia furfur. Ciclopirox exhibits fungicidal activity in vitro against isolates of Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, Microsporum canis, and Candida albicans.

Pharmacokinetic studies in men with tagged ciclopirox solution in polyethylene glycol 400 showed an average of 1.3% absorption of the dose when it was applied topically to 750 cm2 on the back followed by occlusion for 6 hours. The biological half-life was 1.7 hours and excretion occurred via the kidney. Two days after application only 0.01% of the dose applied could be found in the urine. Fecal excretion was negligible.

Penetration studies in human cadaverous skin from the back, with LOPROX® Cream with tagged ciclopirox showed the presence of 0.8 to 1.6% of the dose in the stratum corneum 1.5 to 6 hours after application. The levels in the dermis were still 10 to 15 times above the minimum inhibitory concentrations.

Autoradiographic studies with human cadaverous skin showed that ciclopirox penetrates into the hair and through the epidermis and hair follicles into the sebaceous glands and dermis, while a portion of the drug remains in the stratum corneum.

Draize Human Sensitization Assay, 21-Day Cumulative Irritancy study, Phototoxicity study, and Photo-Draize study conducted in a total of 142 healthy male subjects showed no contact sensitization of the delayed hypersensitivity type, no irritation, no phototoxicity, and no photo-contact sensitization due to LOPROX® Cream.

Indications and Usage for Loprox Cream

LOPROX® Cream is indicated for the topical treatment of the following dermal infections: tinea pedis, tinea cruris, and tinea corporis due to Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, and Microsporum canis; candidiasis (moniliasis) due to Candida albicans; and tinea (pityriasis) versicolor due to Malassezia furfur.

Contraindications

LOPROX® Cream is contraindicated in individuals who have shown hypersensitivity to any of its components.

Warnings

LOPROX® Cream is not for ophthalmic use.

Keep out of reach of children.

Precautions

If a reaction suggesting sensitivity or chemical irritation should occur with the use of LOPROX® Cream, treatment should be discontinued and appropriate therapy instituted.

Information for Patients

The patient should be told to:

Use the medication for the full treatment time even though symptoms may have improved and notify the physician if there is no improvement after four weeks.

Inform the physician if the area of application shows signs of increased irritation (redness, itching, burning, blistering, swelling, or oozing) indicative of possible sensitization.

Avoid the use of occlusive wrappings or dressings.

Carcinogenesis, Mutagenesis, Impairment of Fertility

A carcinogenicity study in female mice dosed cutaneously twice per week for 50 weeks followed by a 6-month drug-free observation period prior to necropsy revealed no evidence of tumors at the application site.

The following in vitro and in vivo genotoxicity tests have been conducted with ciclopirox olamine: studies to evaluate gene mutation in the Ames Salmonella/Mammalian Microsome Assay (negative) and Yeast Saccharomyces Cerevisiae Assay (negative) and studies to evaluate chromosome aberrations in vivo in the Mouse Dominant Lethal Assay and in the Mouse Micronucleus Assay at 500 mg/kg (negative).

The following battery of in vitro genotoxicity tests were conducted with ciclopirox: a chromosome aberration assay in V79 Chinese Hamster Cells, with and without metabolic activation (positive); a gene mutation assay in the HGPRT - test with V79 Chinese Hamster Cells (negative); and a primary DNA damage assay (i.e., unscheduled DNA Synthesis Assay in A549 Human Cells (negative)). An in vitro Cell Transformation Assay in BALB/C3T3 Cells was negative for cell transformation. In an in vivo Chinese Hamster Bone Marrow Cytogenetic Assay, ciclopirox was negative for chromosome aberrations at 5,000 mg/kg.

Pregnancy Category B

Reproduction studies have been performed in the mouse, rat, rabbit, and monkey (via various routes of administration) at doses 10 times or more the topical human dose and have revealed no significant evidence of impaired fertility or harm to the fetus due to ciclopirox. There are, however, no adequate or well-controlled studies in pregnant woman. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

Nursing Mothers

It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when LOPROX® Cream is administered to a nursing woman.

Pediatric Use

Safety and effectiveness in pediatric patients below the age of 10 years have not been established.

Adverse Reactions

In all controlled clinical studies with 514 patients using LOPROX® Cream and in 296 patients using the vehicle cream, the incidence of adverse reactions was low. This included pruritus at the site of application in one patient and worsening of the clinical signs and symptoms in another patient using ciclopirox cream and burning in one patient and worsening of the clinical signs and symptoms in another patient using the vehicle cream.

Loprox Cream Dosage and Administration

Gently massage LOPROX® Cream into the affected and surrounding skin areas twice daily, in the morning and evening. Clinical improvement with relief of pruritus and other symptoms usually occurs within the first week of treatment. If a patient shows no clinical improvement after four weeks of treatment with LOPROX® Cream, the diagnosis should be redetermined. Patients with tinea versicolor usually exhibit clinical and mycological clearing after two weeks of treatment.

How is Loprox Cream Supplied

Loprox® Cream (ciclopirox) 0.77% is supplied in 15 gram (NDC 99207-015-15), 30 gram (NDC 99207-015-30), and 90 gram (NDC 99207-015-90) tubes.

Store at 15°– 30°C (59°– 86°F).

Manufactured for:

MEDICIS, The Dermatology Company®

Scottsdale, AZ 85258

Prescribing Information as of January 2005.

REG TM MEDICIS

IN – 5184/S

158199/2

LOPROX
ciclopirox olamine cream

Product Information
Product Type	HUMAN PRESCRIPTION DRUG	NDC Product Code (Source)	99207-015
Route of Administration	TOPICAL	DEA Schedule

INGREDIENTS
Name (Active Moiety)	Type	Strength
ciclopirox olamine (ciclopirox)	Active	7.7 MILLIGRAM In 1 GRAM
Water	Inactive
Cetyl Alcohol	Inactive
Light Mineral Oil	Inactive
Octyldodecanol	Inactive
Stearyl Alcohol	Inactive
Polysorbate 60	Inactive
Myristyl Alcohol	Inactive
Sorbitan Monostearate	Inactive
Lactic Acid	Inactive
Benzyl Alcohol (1%)	Inactive

Product Characteristics
Color		Score
Shape		Size
Flavor		Imprint Code
Contains

Packaging
#	NDC	Package Description	Multilevel Packaging
1	99207-015-15	15 g (GRAM) In 1 TUBE	None
2	99207-015-30	30 g (GRAM) In 1 TUBE	None
3	99207-015-90	90 g (GRAM) In 1 TUBE	None

Revised: 03/2007MEDICIS, The Dermatology Company

More Loprox Cream resources

Loprox Cream Side Effects (in more detail)
Loprox Cream Use in Pregnancy & Breastfeeding
Loprox Cream Support Group
9 Reviews for Loprox - Add your own review/rating

Compare Loprox Cream with other medications

Cutaneous Candidiasis
Onychomycosis, Fingernail
Onychomycosis, Toenail
Seborrheic Dermatitis
Tinea Corporis
Tinea Cruris
Tinea Pedis
Tinea Versicolor

Monday, July 30, 2012

Topcare Ibuprofen Junior Strength Chewable

Generic Name: ibuprofen

Dosage Form: tablet, chewable
Topco Ibuprofen Tablets 100 mg Drug Facts

Active ingredient (in each tablet)

Ibuprofen 100 mg (NSAID)*

*nonsteroidal anti-inflammatory drug

Purpose

Pain reliever/fever reducer

Uses

temporarily:

reduces fever

relieves minor aches and pains due to the common cold, flu, sore throat, headaches and toothaches

Warnings

Allergy alert: Ibuprofen may cause a severe allergic reaction, especially in people allergic to aspirin. Symptoms may include:

hives

facial swelling

asthma (wheezing)

shock

skin reddening

rash

blisters

If an allergic reaction occurs, stop use and seek medical help right away.

Stomach bleeding warning: This product contains an NSAID, which may cause severe stomach bleeding. The chances are higher if your child:

has had stomach ulcers or bleeding problems

takes a blood thinning (anticoagulant) or steroid drug

takes other drugs containing prescription or nonprescription NSAIDs [aspirin, ibuprofen, naproxen, or others]

takes more or for a longer time than directed

Sore throat warning: Severe or persistent sore throat or sore throat accompanied by high fever, headache, nausea, and vomiting may be serious. Consult doctor promptly. Do not use more than 2 days or administer to children under 3 years of age unless directed by doctor.

Do not use

if the child has ever had an allergic reaction to any other pain reliever/fever reducer

right before or after heart surgery

Ask a doctor before use if

child has problems or serious side effects from taking pain relievers or fever reducers

stomach bleeding warning applies to your child

child has a history of stomach problems, such as heartburn

child has not been drinking fluids

child has lost a lot of fluid due to vomiting or diarrhea

child has high blood pressure, heart disease, liver cirrhosis, or kidney disease

child has asthma

child is taking a diuretic

Ask a doctor or pharmacist before use if the child is

under a doctor’s care for any serious condition

taking any other drug

When using this product

mouth or throat burning may occur; give with food or water

take with food or milk if stomach upset occurs

the risk of heart attack or stroke may increase if you use more than directed or for longer than directed

Stop use and ask a doctor if

child experiences any of the following signs of stomach bleeding:

feels faint

vomits blood

has bloody or black stools

has stomach pain that does not get better

the child does not get any relief within the first day (24 hours) of treatment

fever or pain gets worse or lasts more than 3 days

redness or swelling is present in the painful area

any new symptoms appear

Keep out of reach of children.

In case of overdose, get medical help or contact a Poison Control Center right away. (1-800-222-1222)

Directions

this product does not contain directions or complete warnings for adult use

do not give more than directed

do not give longer than 10 days, unless directed by a doctor (see Warnings)

find the right dose on chart below. If possible, use weight to dose; otherwise use age.

if needed, repeat dose every 6-8 hours

do not use more than 4 times a day

Dosing Chart
Weight (lb)	Age (yr)	Tablets
under 24	under 2	ask a doctor
24-35	2-3	1
36-47	4-5	1 ½
48-59	6-8	2
60-71	9-10	2 ½
72-95	11	3

Other information

phenylketonurics: contains phenylalanine 6 mg per tablet

do not use if printed seal under cap is broken or missing

store at 20-25°C (68-77°F)

see end panel for lot number and expiration date

Inactive ingredients

acesulfame potassium, aspartame, carnauba wax, croscarmellose sodium, FD&C yellow no. 6 aluminum lake, flavors, hypromellose, magnasweet 180, magnesium stearate, mannitol, prosweet, silicon dioxide, sodium lauryl sulfate, soybean oil, succinic acid, whey protein concentrate

Questions or comments?

1-888-423-0139

Principal Display Panel

See New Warnings Information

For Ages 2 to 11

Junior Strength

Ibuprofen Tablets 100 mg

Pain Reliever/Fever Reducer (NSAID)

Lasts Up to 8 Hours

Actual Size

Compare to Motrin® Junior Strength active ingredient

Ibuprofen Tablets 100 mg Carton

TOPCARE IBUPROFEN JUNIOR STRENGTH
ibuprofen tablet, chewable

Product Information
Product Type	HUMAN OTC DRUG	NDC Product Code (Source)	36800-461
Route of Administration	ORAL	DEA Schedule

Active Ingredient/Active Moiety
Ingredient Name	Basis of Strength	Strength
IBUPROFEN (IBUPROFEN)	IBUPROFEN	100 mg

Inactive Ingredients
Ingredient Name	Strength
No Inactive Ingredients Found

Product Characteristics
Color	ORANGE	Score	2 pieces
Shape	ROUND	Size	13mm
Flavor	ORANGE	Imprint Code	L461
Contains

Packaging
#	NDC	Package Description	Multilevel Packaging
1	36800-461-62	1 BOTTLE In 1 CARTON	contains a BOTTLE
1		24 TABLET In 1 BOTTLE	This package is contained within the CARTON (36800-461-62)

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
ANDA	ANDA076359	05/28/2004

Labeler - Topco Associates LLC (006935977)

Revised: 07/2009Topco Associates LLC

More Topcare Ibuprofen Junior Strength Chewable resources

Topcare Ibuprofen Junior Strength Chewable Side Effects (in more detail)
Topcare Ibuprofen Junior Strength Chewable Dosage
Topcare Ibuprofen Junior Strength Chewable Use in Pregnancy & Breastfeeding
Drug Images
Topcare Ibuprofen Junior Strength Chewable Drug Interactions
Topcare Ibuprofen Junior Strength Chewable Support Group
51 Reviews for Topcare Ibuprofen Junior Strength Chewable - Add your own review/rating

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