Ivermectin
- Atc Codes:P02CF01
- CAS Codes:70288-86-7#70161-11-4#70209-81-3
- PHARMGKB ID:70288-86-7#70161-11-4#70209-81-3
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Substrate of
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
France: Stromectol; Greece: Stromectol; Netherlands: Stromectol.
North America
USA: Stromectol.
Latin America
Argentina: Dermoper IV, Detebencil, Ivertal, Securo; Brazil: Leverctin, Revectina, Vermectil; Mexico: Ivexterm.
Asia
Japan: Stromectol.
Drug combinations
Chemistry
Ivermectin: C~48~H~74~O~14~ (component H~2~B~1a~). Mw: 875.09; C~47~H~72~O~14~ (component H~2~B~1b~). Mw: 861.07. CAS-70288-86-7 (1979).
Component H~2~B~1a~: (1) Avermectin A~1a~, 5-O-demethyl-22,23-dihydro-; (2)(2aE,4E,8E)-(5’S,6S,6’R,7S,11R,13R,15S,17aR,20R,20aR,20bS)-6′-(S)-sec-Butyl-3′,4′,5′,6,6′,7,10,11,14,15,17a,20,20a,20b-tetra-decahydro-20,20b-dihydroxy[11,15-methano-2H,13H,17H-furo[4,3,2-pg][2,6]benzodioxacyclooctadecin-13,2′-[2H]pyran]-7-yl 2,6-dideoxy-4-O-(2,6-dideoxy-3-O-methyl-α-L-arabino-hexopyranosyl)-3-O-methyl-α-L-arabino-hexopyranoside. CAS-70161-11-4 (component B~1a~)
Component H~2~B~1b~: (1) Avermectin A~1a~, 5-O-demethyl-25-de(1-methylpropyl)-22,23-dihydro-25-(1-methylethyl)-; (2)(2aE,4E,8E)-(5’S,6S,6’R,7S,11R,13R,15S,17aR,20R,20aR,20bS)-3′,4′,5′,6,6′,7,10,11,-oxospiro[11,15-methano-2H,13H,17H-furo[4,3,2-pg][2,6]benzodioxacyclooctadecin-13,2′[2H]pyran]-7-yl 2,6-dideoxy-4-O-(2,6-dideoxy-3-O-methyl-α-L-arabino-hexopyranosyl)-3-O-methyl-a-L-arabino-hexopyranoside. CAS-70209-81-3 (component B~1b~)
Pharmacologic Category
Anthelmintics. (ATC-Code: P02CF01).
Mechanism of action
Binds selectively to glutamate-gated chloride ion channels, increasing permeability of cell membranes to chloride ions, leading to hyperpolarization of nerve or muscle cell, and death of parasite.
Therapeutic use
Treatment of the following infections: strongyloidiasis of intestinal tract due to nematode parasite Strongyloides stercoralis (active against intestinal forms). Onchocerciasis due to nematode parasite Onchocerca volvulus (active against immature form).
Pregnancy and lactiation implications
Teratogenic effects observed in animal studies. Safety not established in pregnant women. Use not recommended during pregnancy or lactation.
Unlabeled use
Treatment of other parasitic infections including Ascaris lumbricoides, Bancroftian filariasis, Brugia malayi, scabies, Enterobius vermicularis, Mansonella ozzardi, Gnathostomia spingerum, Mansonella ozzardi, Mansonella streptocera, pediculosis pubis, Trichuris trichiura.
Contraindications
Hypersensitivity to ivermectin or any component of the formulation.
Warnings and precautions
Mazzotti reactions might occur and may include pruritus, edema, frank urticarial rash (papular and pustular), fever, arthralgia/synovitis, and lymph node enlargement/tenderness (e.g. axillary, cervical, inguinal). Ocular reactions (e.g. abnormal sensation in eyes, eyelid edema, anterior uveitis, conjunctivitis, limbitis, keratitis, chorioretinitis or choroiditis) might occur. Not recommended in impaired blood-brain barrier (e.g. meningitis, African trypanosomiasis) or CNS disorders which may increase CNS penetration of drug (potential interaction with CNS GABA receptors). Back pain, conjunctival hemorrhage, dyspnea, urinary and/or fecal incontinence, difficulty standing or walking, mental status changes, confusion, lethargy, stupor, seizures, coma, dysarthria or aphasia, fever, headache, or chills reported. Serious and/or fatal encephalopathy reported (rarely) during treatment in patients with loiasis.