Ivermectin (ivermectin)

Ivermectin, a semisynthetic, avermectin-derivative, is used topically as a pediculicide.

Ivermectin is a semisynthetic, avermectin-derivative used as an anthelmintic, pediculicide, and scabicide. Avermectins are macrocyclic lactones isolated from the fermentation products of Streptomyces avermitilis and are similar to macrolide antibacterials but possess no antibacterial properties. Ivermectin is a mixture of 2 chemically modified avermectins: at least 90% is 22,23-dihydroavermectin B1a (H2B1a) and less than 10% is 22,23-dihydroavermectin B1b (H2B1b).

Ivermectin binds selectively and with high affinity to glutamate-gated chloride ion channels in invertebrate nerve and muscle cells, leading to an increase in the permeability of the cell membrane to chloride ions with hyperpolarization of the cell leading to paralysis and death of the parasite. Ivermectin also appears to interact with other ligand-gated chloride channels, such as those gated by gamma-aminobutyric acid (GABA).

Topically applied ivermectin is pediculicidal, but is not ovicidal. In vitro studies indicate that ivermectin has activity against human head lice (Pediculus humanus capitis) and has shown activity against a permethrin-resistant strain. Topical administration has resulted in death of nearly all newly hatched nymphs and adult lice within 48 hours.

There is some evidence suggesting that ivermectin may interfere with louse mouthparts, resulting in impaired feeding in treated lice.

For the topical treatment of pediculosis capitis (head lice infestation), ivermectin is commercially available as a 0.5% lotion in a vehicle that includes olive oil, oleyl alcohol, Crodalan AWS, lanolin alcohol, cyclomethicone, shea butter, sodium citrate, sorbitan tristearate, methylparaben, propylparaben, and citric acid. The lotion is off-white to tan in color.

Low concentrations of ivermectin are absorbed following topical application. Following a single topical application of ivermectin 0.5% lotion in 20 children (6 months to 3 years of age) with head lice infestation, the mean peak plasma concentration of the drug was 0.24 ng/mL (lower limit of quantitation 0.05 ng/mL) and the mean area under the concentration-time curve (AUC) was 6.7 hrxng/mL. These values are lower than those observed following an oral dose of 165 mcg/kg of ivermectin.

Systemically absorbed ivermectin is metabolized in the liver, principally by CYP3A4, and eliminated almost exclusively in feces.

USES: This medication is used to treat a certain skin condition called rosacea, a type of adult acne. Ivermectin may help to decrease symptoms caused by rosacea, such as redness, swelling, and pimples.

Generic name: ivermectin
Pronunciation: (EYE-ver-MEK-tin)
Drug class: Acne Antibiotics
Therapeutic class: Dermatological

The following indications are listed for Ivermectin:

• Acne Rosacea

Also known as: Acne Erythematosa, Rosacea.