abametapir (Discontinued)

Brand and Other Names:Xeglyze

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

topical lotion

  • 0.74%

Head Lice

Indicated for topical treatment of head lice infestation

Apply to dry hair in an amount sufficient (up to the full content of one bottle) to thoroughly coat the hair and scalp

Use in context of overall lice management program

  • 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

Dosage Forms & Strengths

topical lotion

  • 0.74%

Head Lice

Indicated for topical treatment of head lice infestation in children and adolescents aged ≥6 months

<6 months: Safety and efficacy not established

≥6 months

  • Apply to dry hair in an amount sufficient (up to the full content of one bottle) to thoroughly coat the hair and scalp
  • Use in context of overall lice management program

    • 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
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Interactions

Interaction Checker

and abametapir

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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             activity indicator 

            Contraindicated (0)

              Serious - Use Alternative (0)

                Monitor Closely (0)

                  Minor (0)

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                    Adverse Effects

                    1-10%

                    Erythema (4%)

                    Rash (3.2%)

                    Scalp erythema/edema (3.2%)

                    Skin burning sensation (2.6%)

                    Vomiting (1.7%)

                    Contact dermatitis (1.7%)

                    Scalp pruritus (1.4%)

                    Eye irritation (1.2-1.7%)

                    Hair color changes (1%)

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                    Warnings

                    Contraindications

                    None

                    Cautions

                    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; if accidentally swallowed, advise to call Poison Control Center at 1-800-222-1222

                    Drug interaction overview

                    • 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
                    • If this is not feasible, avoid abametapir use
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                    Pregnancy & Lactation

                    Pregnancy

                    No data are available on use in pregnant females to evaluate for drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes

                    Animal data

                    • 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 in rats and rabbits, respectively
                    • Highest dose evaluated in rabbits was limited due to maternal toxicity associated with the vehicle used in the study

                    Lactation

                    No data are available regarding presence in human milk, effects on breastfed infants, or on milk production

                    Pregnancy Categories

                    A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

                    B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

                    C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

                    D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

                    X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

                    NA: Information not available.

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                    Pharmacology

                    Mechanism of Action

                    • Metalloproteinase inhibitor
                    • Metalloproteinases have a role in physiological processes critical to egg development and survival of lice

                    Absorption

                    Peak plasma time: 0.57-1.54 hr

                    Peak plasma concentration

                    • 6 months to <1 year: 228-418 ng/mL
                    • 1 to <2 years: 147-209 ng/mL
                    • 2 to <3 years: 160-206 ng/mL
                    • 3 to 17 years: 52-121 ng/mL

                    AUC

                    • 6 months to <1 year: 688-1057 ng⋅hr/mL
                    • 1 to <2 years: 406-446 ng⋅hr/mL
                    • 2 to <3 years: 602-633 ng⋅hr/mL
                    • 3 to 17 years: 194-330 ng⋅hr/mL

                    Distribution

                    Protein bound

                    • Abametapir: 91.3-92.3%
                    • Abametapir carboxyl (metabolite): 96-97.5%

                    Metabolism

                    Extensively metabolized, primarily by CYP1A2 to a mono-hydroxylated metabolite (abametapir hydroxyl) and further to a mono-carboxylated metabolite (abametapir carboxyl)

                    Elimination

                    Excretion of abametapir and its human metabolites was not examined

                    Half-life (adults): 21 hr; ~71 hr or longer (abametapir carboxyl)

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                    Administration

                    Topical Administration

                    Topical use only

                    Not for oral, ophthalmic, or intravaginal use

                    Treatment involves a single application

                    Shake well before use

                    Apply to dry hair in an amount (up to the full content of one bottle) sufficient to thoroughly coat the hair and scalp

                    Massage into the scalp and throughout the hair

                    Avoid contact with eyes

                    Leave on the hair and scalp for 10 min and then rinse off with warm water

                    Wash hands after application; shampoo hair any time after the treatment

                    Discard any unused product; do not flush contents down sink or toilet

                    Storage

                    Store upright at room temperature, 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86ºF)

                    Do not refrigerate or freeze

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                    Images

                    No images available for this drug.
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                    Patient Handout

                    A Patient Handout is not currently available for this monograph.
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                    Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.