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Abametapir

Medically reviewed by Drugs.com. Last updated on Aug 31, 2023.

Pronunciation

(A ba MET a pir)

Index Terms

Pharmacologic Category

Pharmacology

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.

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%.

Use: Labeled Indications

Head lice: Treatment of head lice infestation in patients ≥6 months of age.

Contraindications

There are no contraindications listed in the manufacturer's labeling.

Dosing: Adult

Head lice: Topical: Apply amount sufficient to thoroughly coat dry hair and scalp (up to the contents of 1 full bottle); massage into scalp and throughout hair, leave on for 10 minutes, and then rinse with warm water. Note: Treatment involves a single application; do not re-treat.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Note: Should be used in conjunction with nit management (eg, washing bedding/clothing/personal items, combing nits out with fine-tooth comb).

Head lice: Infants ≥6 months, Children, and Adolescents: Topical: Apply sufficient amount to dry hair/scalp to fully coat hair and scalp; may need to use entire bottle (210 mL); leave on hair for 10 minutes, then rinse with water. May shampoo any time after product is rinsed out. Note: Treatment involves a single application; do not retreat.

Administration

Topical: For topical use only; not for oral, ophthalmic, or intravaginal use. Shake bottle well before use; apply to dry hair and massage into scalp and throughout hair. Avoid contact with eyes; rinse with warm water after 10 minutes. Wash hands after application. Hair may be shampooed at any time after treatment. Use in conjunction with 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; and use a fine-tooth comb or special nit comb to remove dead lice and nits.

Storage

Store upright at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Do not refrigerate or freeze. Discard unused product; do not flush contents down sink or toilet.

Drug Interactions

CYP1A2 Substrates (High risk with Inhibitors): Abametapir may increase the serum concentration of CYP1A2 Substrates (High risk with Inhibitors). Avoid combination

CYP2B6 Substrates (High risk with Inhibitors): Abametapir may increase the serum concentration of CYP2B6 Substrates (High risk with Inhibitors). Avoid combination

CYP3A4 Substrates (High risk with Inhibitors): Abametapir may increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

1% to 10%:

Dermatologic: Burning sensation of skin (3%), contact dermatitis (2%), erythema of skin (4%), hair discoloration (1%), localized erythema (scalp: ≤3%), skin rash (3%)

Gastrointestinal: Vomiting (2%)

Local: Localized edema (scalp: ≤3%), local pruritus (scalp: 1%)

Ophthalmic: Eye irritation (1% to 2%)

Warnings/Precautions

Special populations:

• Pediatric patients: Use under direct adult supervision. Keep out of reach of children. Use is not recommended for infants <6 months of age due to the potential for increased systemic absorption.

Dosage form specific issues:

• Benzyl alcohol and derivatives: Some dosage forms may contain benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity ("gasping syndrome") in neonates; the "gasping syndrome" consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension, and cardiovascular collapse (AAP 1997; CDC 1982); some data suggest that benzoate displaces bilirubin from protein binding sites (Ahlfors 2001); avoid or use dosage forms containing benzyl alcohol with caution in neonates. See manufacturer's labeling.

Pregnancy Considerations

Adverse events were not observed in animal reproduction studies conducted following oral administration.

Patient Education

What is this drug used for?

• It is used to treat head lice.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Application site burning, itching, redness, or irritation

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine’s uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

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Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.