Abametapir

Aug 3, 2022

Class: Scabicides and Pediculicides
Chemical Name: 5-methyl-2-(5-methylpyridin-2-yl)pyridine
Molecular Formula: C12H12N2
CAS Number: 1134-35-6
Brands: Xeglyze

Introduction

Abametapir is a pediculicide.

Uses for Abametapir

Abametapir has the following uses:

Abametapir lotion is indicated for the topical treatment of head lice infestation in patients 6 months of age and older. Abametapir should be used in the context of an overall lice management program:

Wash (with hot water) or dry-clean all recently worn clothing, hats, used bedding and towels.

Wash personal care items such as combs, brushes and hair clips in hot water.

Use a fine-tooth comb or special nit comb to remove dead lice and nits.

Abametapir Dosage and Administration

General

Abametapir is available in the following dosage form(s) and strength(s):

Lotion: 0.74% (w/w).

Dosage

It is essential that the manufacturer’s labeling be consulted for more detailed information on dosage and administration of this drug. Dosage summary:

Pediatric Patients

Dosage and Administration
  • For topical use only. Not for oral, ophthalmic, or intravaginal use.
  • Shake well before use.
  • Apply abametapir lotion to dry hair in an amount sufficient (up to the full content of one bottle) to thoroughly coat the hair and scalp. Avoid contact with eyes.
  • Massage abametapir lotion into the scalp and throughout the hair; leave on the hair and scalp for 10 minutes and then rinse off with warm water.
  • Wash hands after application. Hair may be shampooed any time after the treatment.
  • Treatment with abametapir lotion involves a single application. Discard any unused product. Do not flush contents down sink or toilet.

Adults

Dosage and Administration
  • For topical use only. Not for oral, ophthalmic, or intravaginal use.
  • Shake well before use.
  • Apply abametapir lotion to dry hair in an amount sufficient (up to the full content of one bottle) to thoroughly coat the hair and scalp. Avoid contact with eyes.
  • Massage abametapir lotion into the scalp and throughout the hair; leave on the hair and scalp for 10 minutes and then rinse off with warm water.
  • Wash hands after application. Hair may be shampooed any time after the treatment.
  • Treatment with abametapir lotion involves a single application. Discard any unused product. Do not flush contents down sink or toilet.

Detailed Abametapir topical dosage information

Cautions for Abametapir

Contraindications

None.

Warnings/Precautions

Risk of Neonatal Benzyl Alcohol Toxicity

Abametapir lotion contains benzyl alcohol. Systemic exposure to benzyl alcohol has been associated with serious and fatal adverse reactions including “gasping syndrome” in neonates and low birth weight infants. The “gasping syndrome” is characterized by central nervous system depression, metabolic acidosis, and gasping respirations. The minimum amount of benzyl alcohol at which toxicity may occur is not known. Premature and low-birth weight infants may be more likely to develop toxicity.

The safety and effectiveness of abametapir lotion have not been established in pediatric patients below the age of 6 months. Use is not recommended in pediatric patients under 6 months of age because of the potential for increased systemic absorption.

Risk of Benzyl Alcohol Toxicity from Accidental Ingestion

In order to prevent accidental ingestion in pediatric patients, abametapir lotion should only be administered under direct supervision of an adult.

Ingestion of benzyl alcohol in large quantities may result in gastrointestinal (nausea, vomiting, diarrhea) and central nervous system (headache, ataxia, convulsions, coma) adverse reactions. Serious adverse reactions may include respiratory depression and death. If accidentally swallowed, advise the patient or the caregiver to call their Poison Control Center at 1-800-222-1222.

Specific Populations

Pregnancy

Risk Summary: There are no available data on abametapir use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. In embryofetal development studies conducted with oral administration of abametapir during organogenesis, no evidence of fetal harm or malformations, independent of maternal toxicity were observed in pregnant rats and rabbits at doses that produced exposures up to 50 times and equivalent to the maximum recommended human dose (MRHD) in rats and rabbits, respectively. The highest dose evaluated in rabbits was limited due to maternal toxicity associated with the vehicle used in the study.

The background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively.

Animal Data: Systemic embryofetal development studies were performed in rats and rabbits. Oral doses of 10, 25 and 75 mg/kg/day abametapir were administered during the period of organogenesis (gestational days 6–17) to pregnant rats. In the presence of maternal toxicity, embryofetal toxicity (lower fetal body weights and delayed ossification) was noted at 75 mg/kg/day. No treatment related effects on malformations were noted at 75 mg/kg/day (50 times the MRHD based on Cmax comparisons).

Oral doses of 4, 16 and 40 mg/kg/day abametapir were administered during the period of organogenesis (gestational days 6–19) to pregnant rabbits. No treatment related effects on embryofetal toxicity or malformations were noted at 40 mg/kg/day (approximately 1 time the MRHD based on Cmax comparisons). Maternal toxicity related to the vehicle limited the maximum dose in pregnant rabbits.

In a perinatal and postnatal development study in rats, oral doses of 10, 25 and 75 mg/kg/day were administered from the beginning of organogenesis (gestational day 6) through the end of lactation (lactation day 20). In the presence of maternal toxicity, embryofetal lethality, and decreased fetal body weight gain were noted at 75 mg/kg/day. No treatment related effects on postnatal development were noted at 75 mg/kg/day (47 times the MRHD based on Cmax comparisons).

Lactation

No data are available regarding the presence of abametapir in human milk or the effects of abametapir on the breastfed infant or on milk production. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for abametapir and any potential adverse effects on the breastfed child from abametapir or from the underlying maternal condition.

Pediatric Use

The safety and effectiveness of abametapir lotion have been established in pediatric patients 6 months of age and older.

The safety and effectiveness of abametapir lotion have not been established in pediatric patients below the age of 6 months. Abametapir lotion is not recommended in pediatric patients under 6 months of age because of the potential for increased systemic absorption due to a high ratio of skin surface to body mass and the potential for an immature skin barrier.

Abametapir lotion contains benzyl alcohol. Benzyl alcohol has been associated with serious adverse reactions and death in neonates and low birth-weight infants. The “gasping syndrome” (characterized by central nervous system depression, metabolic acidosis, gasping respirations, and high levels of benzyl alcohol and its metabolites found in the blood and urine) has been associated with intravenously administered benzyl alcohol dosages >99 mg/kg/day in neonates and low birthweight infants. Additional symptoms may include gradual neurological deterioration, seizures, intracranial hemorrhage, hematologic abnormalities, skin breakdown, hepatic and renal failure, hypotension, bradycardia, and cardiovascular collapse.

The minimum amount of benzyl alcohol at which toxicity may occur is not known. Premature and low-birthweight infants, as well as patients receiving high dosages, may be more likely to develop toxicity.

Because of the risk of accidental ingestion, abametapir lotion should be administered to pediatric patients only under direct adult supervision. (See Risk of Benzyl Alcohol Toxicity from Accidental Ingestion under Cautions: Warnings/Precautions.)

Geriatric Use

Clinical studies of abametapir lotion did not include sufficient numbers of subjects aged 65 years and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between elderly and younger subjects.

Common Adverse Effects

Most common adverse reactions (incidence of ≥1%) were erythema, rash, skin burning sensation, contact dermatitis, vomiting, eye irritation, pruritus, and hair color changes.

Drug Interactions

Specific Drugs

It is essential that the manufacturer’s labeling be consulted for more detailed information on interactions with this drug, including possible dosage adjustments. Interaction highlights:

For 2 weeks after application of abametapir lotion, avoid taking drugs that are substrates of CYP3A4, CYP2B6 or CYP1A2. Otherwise, avoid use of abametapir lotion.

Abametapir topical drug interactions  (more detail)

Actions

Mechanism of Action

Abametapir is a metalloproteinase inhibitor. Metalloproteinases have a role in physiological processes critical to egg development and survival of lice.

Advice to Patients

Patient Counseling Information

Advise the patient or caregiver to read the FDA-approved patient labeling (Patient Information and Instructions for Use).

Inform the patient and caregiver of the following instructions:

Do not ingest abametapir lotion.

Keep out of reach of children. Use on children should be under the direct supervision of an adult because of the risk of benzyl alcohol toxicity.

Avoid contact with eyes.

Wash hands after application.

Hair may be shampooed any time after the treatment.

Treatment with abametapir lotion involves a single application. Do not retreat.

Discard any unused portion. Do not flush contents down sink or toilet.

Additional Information

AHFSfirstRelease. For additional information until a more detailed monograph is developed and published, the manufacturer’s labeling should be consulted. It is essential that the manufacturer’s labeling be consulted for more detailed information on usual uses, dosage and administration, cautions, precautions, contraindications, potential drug interactions, laboratory test interferences, and acute toxicity.

source :: https://www.drugs.com/monograph/abametapir.html