Overview
DESCRIPTION Ivermectin is a semisynthetic, anthelmintic agent for oral administration. Ivermectin is derived from the avermectins, a class of highly active broad-spectrum, anti-parasitic agents isolated from the fermentation products of Streptomyces avermitilis . Ivermectin is a mixture containing at least 90% 5- O -demethyl-22,23-dihydroavermectin A 1a and less than 10% 5- O-...
Mechanism of Action
CLINICAL PHARMACOLOGY Pharmacokinetics Following oral administration of ivermectin, plasma concentrations are approximately proportional to the dose. In two studies, after single 12-mg doses of ivermectin in fasting healthy volunteers (representing a mean dose of 165 mcg/kg), the mean peak plasma concentrations of the major component (H 2 B 1a ) were 46.6 (±21.9) (range: 16.4 to 101.1) and 30.6 (±15.6) (range: 13.9 to 68.4) ng/mL, respectively, at approximately 4 hours after dosing. Ivermectin is metabolized in the liver, and ivermectin and/or its metabolites are excreted almost exclusively in the feces over an estimated 12 days, with less than 1% of the administered dose excreted in the urine.
Indications
- INDICATIONS AND USAGE Ivermectin is indicated for the treatment of the following infections: Strongyloidiasis of the intestinal tract Ivermectin is indicated for the treatment of intestinal (i.e., nondisseminated) strongyloidiasis due to the nematode parasite Strongyloides stercoralis . This indication is based on clinical studies of both comparative and open-label designs, in which 64-100% of infected patients were cured following a single 200-mcg/kg dose of ivermectin (See CLINICAL PHARMACOLOGY, Clinical Studies ).
Common Doses
- 200 mcg
- 150 mcg
Dosage
DOSAGE AND ADMINISTRATION Strongyloidiasis The recommended dosage of ivermectin Tablets for the treatment of strongyloidiasis is a single oral dose designed to provide approximately 200 mcg of ivermectin per kg of body weight. See Table 1 for dosage guidelines. Patients should take tablets on an empty stomach with water (See CLINICAL PHARMACOLOGY, Pharmacokinetics ). In general, additional doses are not necessary. However, follow-up stool examinations should be performed to verify eradication of infection (See CLINICAL PHARMACOLOGY, Clinical Studies ).
Contraindications
- CONTRAINDICATIONS Ivermectin Tablets are contraindicated in patients who are hypersensitive to any component of this product.
Side Effects
- ADVERSE REACTIONS Strongyloidiasis In four clinical studies involving a total of 109 patients given either one or two doses of 170 to 200 mcg/kg of ivermectin, the following adverse reactions were reported as possibly, probably, or definitely related to ivermectin: Body as a Whole: asthenia/fatigue (0.9%), abdominal pain (0.9%) Gastrointestinal: anorexia (0.9%), constipation (0.9%), diarrhea (1.8%), nausea (1.8%), vomiting (0.9%) Nervous System/Psychiatric: dizziness (2.8%), somnolence (0.9%), vertigo (0.9%), tremor (0.9%) Skin: pruritus (2.8%), rash (0.9%), and urticaria (0.9%).
Interactions
- Drug Interactions Post-marketing reports of increased INR (International Normalized Ratio) have been rarely reported when ivermectin was co-administered with warfarin.