ivermectin (Rx)

Frequency Not Defined

Abdominal pain

Asthenia

Hypotension

Mild EKG changes

Peripheral & facial edema

Transient tachycardia

Dizziness

Headache

Hyperthermia

Insomnia

Somnolence

Vertigo

Pruritus

Rash

Urticaria

Diarrhea

Nausea

Vomiting

Eosinophilia

Leukopenia

ALT/AST increased

Limbitis

Myalgia

Tremor

Blurred vision

Mild conjunctivitis

Punctate opacity

Mazzotti reaction (with onchocerciasis)

Edema

Fever

Lymphadenopathy

Ocular damage

Pruritus rash

Conjunctival hemorrhage (with onchocerciasis)

Hepatitis

Contraindications

Hypersensitivity to ivermectin

Cautions

May cause cutaneous and/or systemic reactions

Does not kill adult Onchocerca volvulus, only microfilariae

Not active against disseminated Strongyloides, only intestinal

Potential risk of Mazzotti reactions (cutaneous and systemic adverse effects)

May be required to repeat treatments in immunocompromised patients

Suppressive therapy (monthly) may be necessary to control extraintestinal strongyloidiasis

Perform pretreatment assessment for Loa loa infection in any patient with significant exposure to endemic areas; serious and/or fatal encephalopathy reported during treatment in patients with loiasis

Pregnancy category: C

Pregnancy

There are no studies in pregnant women; epidemiologic studies during pregnancy are insufficient to inform a drug-associated risk of adverse developmental outcomes, because either the timing of administration during gestation was not accurately ascertained or the administration occurred only during the second trimester; however, systemic exposure from topical use of ivermectin is much lower than that from oral use

In animal reproduction studies, ivermectin induced adverse developmental outcomes when orally administered to pregnant mice, rats and rabbits during the period of organogenesis only at or near doses that were maternally toxic to the pregnant females

Lactation

There is information available on the presence of ivermectin in human milk in 4 lactating women after a single 150 mcg/kg oral dose of ivermectin; however, there is insufficient information from this study to determine effects of ivermectin on breastfed infant or on milk production

Topical ivermectin systemic exposure is much lower than that for oral ivermectin; furthermore, amount of ivermectin present in human milk after topical application to lactating women has not been studied

The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for therapy and any potential adverse effects on breastfed infant or from underlying maternal condition

Lactation: Enters breast milk (AAP Committee states compatible with nursing)

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.

Mechanism of Action

Binds glutamate-gated Cl ion channels in invertebrate nerve and muscle cells; produces paralysis, death of parasite

Absorption

Well absorbed

Peak serum time: 4 hr

Peak effect: 3-6 months (treatment of orchocerciasis); 3 months (treatment of strongyloides)

Distribution

Protein bound: 93%

Vd: 3-3.5 L/kg

Does not cross blood-brain barrier

Metabolism

Hepatic (CYP3A4, CYP2D6, CYP2E1)

Elimination

Half-life: 18 hr

Excretion: Feces; urine (<1%)