Ivermectin (Page 2 of 3)

11 DESCRIPTION

Ivermectin Lotion, for topical administration, is an off-white/tan lotion containing 0.5% ivermectin.

Ivermectin, the active ingredient, is a pediculicide, derived from the fermentation of a soil dwelling actinomycete, Streptomyces avermitilis.

Ivermectin is a mixture containing at least 90% 5-O -demethyl-22,23-dihydroavermectin A1a and less than 10% 5-O -demethyl-25-de(1-methylpropyl)-22,23-dihydro25-(1-methylethyl) avermectin A1a , generally referred to as 22,23-dihydroavermectin B1a and B1b , or H2 B1a and H2 B1b , respectively. The respective empirical formulas are C48 H74 O14 and C47 H72 O14 , with molecular weights of 875.10 and 861.07, respectively. The structural formulas are:

Chemical Structure
(click image for full-size original)
Component H2 B1a : R = CH2 CH3 Component H2 B1b : R = CH3

Ivermectin Lotion contains the following inactive ingredients: butylated hydroxyanisole, castor oil, cetyl alcohol, citric acid anhydrous, crodalan AWS, cyclomethicone, glycerin, imidurea, lanolin alcohols, methylparaben, oleyl alcohol, olive oil, propylene glycol, propylparaben, purified water, shea butter, sodium citrate anhydrous, sorbitan tristearate and stearyl alcohol.

12 CLINICAL PHARMACOLOGY

12.1 Mechanism of Action

Ivermectin, a member of the avermectin class, causes death of parasites, primarily through binding selectively and with high affinity to glutamate-gated chloride channels, which occur in invertebrate nerve and muscle cells. This leads to an increase in the permeability of the cell membrane to chloride ions with hyperpolarization of the nerve or muscle cell, resulting in paralysis and death of the parasite. Compounds of this class may also interact with other ligand-gated chloride channels, such as those gated by the neurotransmitter gamma-aminobutyric acid (GABA). The selective activity of compounds of this class is attributable to the fact that some mammals do not have glutamate-gated chloride channels, the avermectins have a low affinity for mammalian ligand-gated chloride channels, and ivermectin does not readily cross the blood-brain barrier in humans.

12.2 Pharmacodynamics

The pharmacodynamics of Ivermectin Lotion are unknown.

12.3 Pharmacokinetics

The absorption of ivermectin from Ivermectin Lotion was evaluated in a clinical study in subjects aged from 6 months to 3 years. This study evaluated pharmacokinetics in 20 lice infested subjects, and 13 of these subjects weighed 15 kg or less (overall weight range 8.5 to 23.9 kg). All enrolled subjects received a single treatment with Ivermectin Lotion. The systemic ivermectin exposure was evaluated using an assay with a lower limit of quantitation of 0.05 ng/mL. The mean (± standard deviation) plasma maximum concentration (Cmax ) and area under the concentration-time curve from 0 to time of last measurable concentration (AUC0-tlast ) were 0.24 ± 0.23 ng/mL and 6.7 ± 11.2 hr∙ng/mL, respectively. These levels are much lower than those observed following oral administration of 165 mcg/kg dose of ivermectin.

13 NONCLINICAL TOXICOLOGY

13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility

Long-term studies in animals have not been performed to evaluate the carcinogenic potential of Ivermectin Lotion or ivermectin.

Ivermectin was not genotoxic in vitro in the Ames test, the mouse lymphoma assay, or the unscheduled DNA synthesis assay in human fibroblasts.

Ivermectin had no adverse effects on fertility in rats at repeated oral doses of up to 3.6 mg/kg/day.

14 CLINICAL STUDIES

Two identical multi-center, randomized, double-blind, vehicle-controlled studies were conducted in subjects 6 months of age and older with head lice infestation. All subjects received a single application of either Ivermectin Lotion or vehicle control with instructions not to use a nit comb. For the evaluation of efficacy, the youngest subject from each household was considered to be the index subject of the household (N=289). Other enrolled infested household members received the same treatment as the youngest subject and were evaluated for all safety parameters [see Adverse Reactions (6.1)].

The primary efficacy was assessed as the proportion of index subjects who were free of live lice at day 2 and through day 8 to the final evaluation 14 (+2) days following a single application. Subjects with live lice present at any time up to the final evaluation were considered treatment failures. Table 1 contains the proportion of subjects who were free of live lice in each of the two trials.

Table 1: Proportion of Subjects Free of Live Lice 14 Days After Treatment
Study Vehicle% (n/N) Ivermectin Lotion% (n/N)
Study 1 16.2% (12/74) 76.1% (54/71)
Study 2 18.9% (14/74) 71.4% (50/70)

16 HOW SUPPLIED/STORAGE AND HANDLING

Ivermectin Lotion, 0.5% is supplied in a 4 oz (117 g) white laminate tube (NDC 51672-4211-8).

Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Do not freeze.

17 PATIENT COUNSELING INFORMATION

“See FDA-approved patient labeling (Patient Information)“.

Inform the patient and caregiver of the following instructions:

  • Use Ivermectin Lotion in the context of an overall lice management program.
  • Apply Ivermectin Lotion to dry scalp and dry scalp hair.
  • Wash hands after applying Ivermectin Lotion.
  • Leave Ivermectin Lotion on the hair and scalp for 10 minutes, and then rinse off with water.
  • For single use only; do not re-treat.
  • It is recommended to wait 24 hours before applying shampoo to hair and scalp.
  • Discard tube after use.
  • Avoid contact with eyes.
  • Do not swallow Ivermectin Lotion.
  • Keep out of reach of children. Use on children should be under the direct supervision of an adult.
  • Advise a lactating woman to avoid accidental transfer of Ivermectin Lotion directly to breast area where the infant might directly ingest the drug.

Manufactured by: Taro Pharmaceutical Industries Ltd.
Haifa Bay, Israel, 2624761
Dist. by: Taro Pharmaceuticals U.S.A., Inc.
Hawthorne, NY 10532

Issued: December, 2019
21180-1219-0 809

Patient Information Ivermectin (eye” ver mek’ tin) Lotion, 0.5%
Important: For use on scalp hair and scalp only. Do not use Ivermectin Lotion in your eyes, mouth, or vagina.
What is Ivermectin Lotion? Ivermectin Lotion is a prescription medicine for topical use on the hair and scalp only. Ivermectin Lotion is used to treat head lice in people 6 months of age and older. It is not known if Ivermectin Lotion is safe and effective for children under 6 months of age.
Before you use Ivermectin Lotion, tell your healthcare provider about all of your medical conditions, including if you or your child:
  • have any skin conditions or sensitivities
  • are pregnant or plan to become pregnant. It is not known if Ivermectin Lotion can harm your unborn baby
  • are breastfeeding or plan to breastfeed. Ivermectin has been found in breast milk when taken by mouth and may pass into breast milk after using Ivermectin Lotion. If you use Ivermectin Lotion and breastfeed your baby:
    • avoid accidental transfer of Ivermectin Lotion to your breast to help prevent ingestion by your baby.
    • talk to your healthcare provider about the best way to feed your baby during treatment with Ivermectin Lotion.
How should I use Ivermectin Lotion?
  • See the detailed “Instructions for Use” at the end of this leaflet.
  • Use Ivermectin Lotion exactly as prescribed. Your healthcare provider will prescribe the treatment that is right for you.
  • Use Ivermectin Lotion when your hair is dry.
  • It is important to use enough Ivermectin Lotion to completely coat all of your hair and scalp. Leave Ivermectin Lotion on your hair and scalp for a full 10 minutes, and then rinse off with water.
  • You need to completely cover all the scalp and hair with lotion.
  • Children will need an adult to apply Ivermectin Lotion for them.
  • It is recommended to wait 24 hours before applying shampoo to hair and scalp.
  • Do not swallow Ivermectin Lotion. If swallowed, call your healthcare provider or go to the nearest emergency room right away.
  • Do not get Ivermectin Lotion into your eyes. If Ivermectin Lotion gets in your eye, gently flush with water.
  • Wash your hands after applying Ivermectin Lotion.
When you complete your treatment with Ivermectin Lotion, do not use Ivermectin Lotion again without talking to your healthcare provider first.
What are the possible side effects of Ivermectin Lotion?The most common side effects of Ivermectin Lotion include:
  • eye redness or soreness
  • eye irritation
  • dandruff
  • dry skin
  • burning sensation of the skin
These are not all the possible side effects of Ivermectin Lotion. For more information, ask your healthcare provider or pharmacist.Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.
How should I store Ivermectin Lotion?
  • Store Ivermectin Lotion at room temperature between 68°F to 77°F (20°C to 25°C).
  • Do not freeze Ivermectin Lotion.
  • Safely throw away any unused Ivermectin Lotion.
Keep Ivermectin Lotion and all medicines out of reach of children.
General information about the safe and effective use of Ivermectin Lotion. Medicines are sometimes prescribed for purposes other than those listed in a Patient Information leaflet. Do not use Ivermectin Lotion for a condition for which it was not prescribed. Do not give Ivermectin Lotion to other people, even if they have the same symptoms you have. It may harm them. You can also ask your healthcare provider or pharmacist for information about Ivermectin Lotion that is written for health professionals.
What are the ingredients in Ivermectin Lotion? Active: Ivermectin 0.5%Inactive ingredients: butylated hydroxyanisole, castor oil, cetyl alcohol, citric acid anhydrous, crodalan AWS, cyclomethicone, glycerin, imidurea, lanolin alcohols, methylparaben, oleyl alcohol, olive oil, propylene glycol, propylparaben, purified water, shea butter, sodium citrate anhydrous, sorbitan tristearate and stearyl alcohol.Manufactured by: Taro Pharmaceutical Industries Ltd., Haifa Bay, Israel, 2624761 Dist. by: Taro Pharmaceuticals U.S.A., Inc. Hawthorne, NY 10532 Issued: December, 2019 21180-1219-0 809

All MedLibrary.org resources are included in as near-original form as possible, meaning that the information from the original provider has been rendered here with only typographical or stylistic modifications and not with any substantive alterations of content, meaning or intent.

This site is provided for educational and informational purposes only, in accordance with our Terms of Use, and is not intended as a substitute for the advice of a medical doctor, nurse, nurse practitioner or other qualified health professional.

Privacy Policy | Copyright © 2022. All Rights Reserved.