Drug information of Abametapir

Abametapir

Drug group:

Abametapir is a novel pediculicidal metalloproteinase inhibitor used to treat infestations of head lice

Mechanism of effect

Abametapir (5,5’-dimethyl 2,2’-bipyridinyl) is a metalloproteinase inhibitor; metalloproteinases have a role in physiological processes critical to egg development and survival of lice.

Pharmacodynamic

Abametapir has been shown to inhibit all stages of embryo development in both head and body lice by interfering with enzymes critical to this process.

Pharmacokinetics

Metabolism

Extensively metabolized by CYP1A2 to abametapir hydroxyl and further to abametapir carboxyl.

Time to Peak

0.57 to 1.54 hours.

Half-Life Elimination

Abametapir: 21 hours; abametapir carboxyl: 71 ± 40 hours.

Protein Binding

Abametapir: 91.3% to 92.3%; abametapir carboxyl: 96% to 97.5%.

Drug indications

Head Lice

Dosage

Apply amount sufficient to thoroughly coat dry hair and scalp (up to the contents of 1 full bottle). Infants ≥6 months, Children, and Adolescents, Apply sufficient amount to dry hair/scalp to fully coat hair and scalp; may need to use entire bottle (210 mL); massage into scalp and throughout hair, leave on for 10 minutes, and then rinse with warm water.  Treatment involves a single application; do not re-treat.

Drug contraindications

None

Side effects

vomiting , Rash , Stinging/burning of scalp

Erythema

Rash

Scalp erythema/edema

Skin burning sensation

Vomiting

Contact dermatitis

Scalp pruritus

Eye irritation

Hair color changes

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Alerts

-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

-Safety and effectiveness have not been established in pediatric patients aged <6 months

-Use is not recommended in pediatric patients aged <6 months because of the potential for increased systemic absorption

-In order to prevent accidental ingestion in pediatric patients, only administer under direct supervision of an adult

-Ingestion of benzyl alcohol in large quantities may result in gastrointestinal (eg, nausea, vomiting, diarrhea) and CNS (eg, headache, ataxia, convulsions, coma) adverse reactions; serious adverse reactions may include respiratory depression and death;

-In vitro studies suggest potential for abametapir to inhibit CYP3A4, CYP2B6, and CYP1A2 enzymes following a single application.Coadministration with substrates of these enzymes may lead to increased systemic concentrations of the interacting drugs

.Avoid administration of drugs that are substrates of CYP3A4, CYP2B6, or CYP1A2 within 2 weeks after abametapir application

 

Points of recommendation

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

-Wash personal care items (eg, combs, brushes, hair clips) in hot water

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

Pregnancy level

HAVE NOT BEEN ESTABLISHED

-There is no data on use in pregnant women to know this drugs risks, including the risk of fetal harm or reproductive effects.

-Animal data of oral administration at exposures up to 50 times the maximum recommended human dose given during organogenesis did not show fetal harm or malformations independent of maternal toxicity.

Breast feeding warning

-There is no information regarding this drug on the presence in human milk, the effects on a breastfed infant, or effects on milk production.
-Consider the developmental and health benefits of breastfeeding along with the mother's clinical need for this medication as well as any potential adverse effects from this drug or the underlying maternal condition.

Drug forms

Xeglyze

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