Ivermectin

IVERMECTIN- ivermectin cream
Prasco Laboratories

SPL PRODUCT DATA ELEMENTS SECTION

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1 INDICATIONS AND USAGE

Ivermectin cream is indicated for the treatment of inflammatory lesions of rosacea.

2 DOSAGE AND ADMINISTRATION

Apply to the affected areas of the face once daily. Use a pea-size amount for each area of the face (forehead, chin, nose, each cheek) that is affected. Spread as a thin layer, avoiding the eyes and lips.
Ivermectin cream is not for oral, ophthalmic, or intravaginal use.

3 DOSAGE FORMS AND STRENGTHS

Cream, 1%.
Each gram of Ivermectin cream contains 10 mg of ivermectin in a white to pale yellow cream base. Ivermectin cream is supplied in tubes of 45 g.

4 CONTRAINDICATIONS

None.

6 ADVERSE REACTIONS

6.1 Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
During clinical trials, 2047 subjects with inflammatory lesions of rosacea received Ivermectin cream once daily. A total of 1555 subjects were treated once daily for more than 12 weeks, and 519 for approximately one year.
Adverse reactions, reported in ≤ 1% of subjects treated with Ivermectin cream for at least 3 months in vehicle-controlled clinical trials, included skin burning sensation and skin irritation.

6.2 Postmarketing Experience

Because adverse reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
Local adverse reactions: contact dermatitis and allergic dermatitis.

7 DRUG INTERACTIONS

In vitro studies have shown that Ivermectin cream, at therapeutic concentrations, neither inhibits nor induces cytochrome P450 (CYP450) enzymes.

8 USE IN SPECIFIC POPULATIONS

8.1 Pregnancy

Pregnancy Category C.
There are no adequate and well-controlled studies in pregnant women. Ivermectin cream should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Note: The animal multiples of human exposure calculations were based on AUC comparisons. The maximum topical human dose (MTHD) of Ivermectin cream is 1 g applied once daily.

Systemic embryofetal development studies were conducted in rats and rabbits. Oral doses of 1.5, 4, and 12 mg/kg/day ivermectin were administered during the period of organogenesis (gestational days 6–17) to pregnant female rats. Maternal death occurred at 12 mg/kg/day (1909X MTHD). Cleft palate occurred in the fetuses from the 12 mg/kg/day (1909X MTHD) group. No treatment related effects on embryofetal toxicity or teratogenicity were noted at 4 mg/kg/day (708X MTHD). Oral doses of 0.5, 1.5, 2.5, 3.5 and 4.5 mg/kg/day ivermectin were administered during the period of organogenesis (gestational days 7–20) to pregnant female rabbits. Maternal death occurred at doses >2.5 mg/kg/day (72X MTHD). Carpal flexure occurred in the fetuses from the 4.5 mg/kg/day (354X MTHD) group. Fetal weight decrease was noted at 3.5 mg/kg/day (146X MTHD). No treatment related effects on embryofetal toxicity were noted at 2.5 mg/kg/day (72X MTHD) and no treatment related effects on teratogenicity were noted at 3.5 mg/kg/day (146X MTHD).

A pre- and postnatal development study was conducted in rats. Oral doses of 1, 2 and 4 mg/kg/day ivermectin were administered to pregnant female rats during gestational days 6-20 and lactation days 2-20. Neonatal death occurred at doses >2 mg/kg/day. Behavior development of newborn rats was adversely affected at all doses.

8.3 Nursing Mothers

Following oral administration, ivermectin is excreted in human milk in low concentrations. Excretion in human milk following topical administration has not been evaluated. In oral studies in rats, ivermectin was excreted in the milk of nursing mothers and neonatal toxicity was observed in the litters. The blood-brain barrier in neonatal rats may not be fully developed at birth. Because of the potential for serious adverse reactions from Ivermectin cream in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

8.4 Pediatric Use

Safety and effectiveness of Ivermectin cream in pediatric patients have not been established.

8.5 Geriatric Use

Of the 1371 subjects in the two pivotal clinical studies of Ivermectin cream, 170 (12.4%) were 65 and over, while 37 (2.7%) were 75 and over. No overall differences in safety or effectiveness were observed between these subjects and younger subjects, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out.

10 OVERDOSAGE

In accidental or significant exposure to unknown quantities of veterinary formulations of ivermectin in humans, either by ingestion, inhalation, injection, or exposure to body surfaces, the following adverse effects have been reported most frequently: rash, edema, headache, dizziness, asthenia, nausea, vomiting, and diarrhea. Other adverse effects that have been reported include: seizure, ataxia, dyspnea, abdominal pain, paresthesia, urticaria, and contact dermatitis.

In case of accidental ingestion, supportive therapy, if indicated, should include parenteral fluids and electrolytes, respiratory support (oxygen and mechanical ventilation if necessary) and pressor agents if clinically significant hypotension is present. Induction of emesis and/or gastric lavage as soon as possible, followed by purgatives and other routine anti-poison measures, may be indicated if needed to prevent absorption of ingested material.

11 DESCRIPTION

Ivermectin cream, 1% is a white to pale yellow hydrophilic cream. Each gram of Ivermectin cream contains 10 mg of ivermectin. It is intended for topical use.

Ivermectin is a semi-synthetic derivative isolated from the fermentation of Streptomyces avermitilis that belongs to the avermectin family of macrocyclic lactones.

Ivermectin is a mixture containing not less than 95.0% and not more than 102.0% of 5-O-demethyl-22,23-dihydroavermectin A1a plus 5-O-demethyl-25-de(1-methylpropyl)-25-(1-methylethyl)-22,23-dihydroavermectin A1a , generally referred to as 22,23-dihydroavermectin B1a and B1b or H2 B1a and H2 B1b , respectively; and the ratio (calculated by area percentage) of component H2 B1a /(H2 B1a + H2 B1b ) is not less than 90.0%. The respective empirical formulas of H2 B1a and H2 B1b are C48 H74 O14 and C47 H72 O14 with molecular weights of 875.10 and 861.07 respectively.

The structural formulas are:

ivermectin-chem-struct
(click image for full-size original)

Component H2 B1a : R = C2 H5 , Component H2 B1b : R = CH3 .

Ivermectin cream contains the following inactive ingredients: carbomer copolymer type B, cetyl alcohol, citric acid monohydrate, dimethicone, edetate disodium, glycerin, isopropyl palmitate, methylparaben, oleyl alcohol, phenoxyethanol, polyoxyl 20 cetostearyl ether, propylene glycol, propylparaben, purified water, sodium hydroxide, sorbitan monostearate, and stearyl alcohol.

12 CLINICAL PHARMACOLOGY

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