Ivermectin

Products

Ivermectin is commercially available in some countries in tablet form (Stromectol). It has not yet been registered in many countries and therefore must be imported from abroad if needed. Ivermectin has been used medicinally since the 1980s, initially primarily as a veterinary drug. This article refers to peroral administration in humans. See also under the article ivermectin cream (Soolantra).

Structure and properties

Ivermectin is a mixture of the two ivermectin components H2B1a and H2B1b. The two molecules differ structurally only by a methylene group. Ivermectin exists as a white to yellowish white, crystalline and weakly hygroscopic powder. The macrocyclic lactone is practically insoluble in water. It is a semisynthetic derivative of an avermectin formed by . This bacterium was discovered in a soil sample from Japan.

Effects

Ivermectin (ATC P02CF01) has antiparasitic and anthelmintic properties. The effects are due to binding to glutamate-gated chloride channels found in nerve and muscle cells. The result is increased permeability of cell membranes to chloride ions and hyperpolarization. This leads to paralysis and death of the parasites. The half-life of ivermectin is approximately 18 hours. Furthermore, ivermectin has also shown antiviral effects against various viruses.

Indications

Indications and indications for use include:

  • Nematodes (strongyloidiasis, river blindness).
  • Scabies (Scabies)
  • Head lice, crabs
  • Rosacea see under ivermectin cream

Off-label use:

  • In 2020, ivermectin was investigated for the treatment of coronavirus disease Covid-19. In vitro, it has shown potent antiviral effects against SARS-CoV-2 (Caly et al, 2020).

Dosage

According to the professional information. The tablets are usually taken as a single dose and fasting. The dose depends on body weight.

Contraindications

  • Hypersensitivity
  • Pregnancy and lactation
  • Children with a body weight under 15 kg

Full precautions can be found in the drug label.

Interactions

Ivermectin is a substrate of CYP3A4 and P-glycoprotein. It should not be taken concomitantly with diethylcarbamazine. An interaction with warfarin has been described.

Adverse Effects

Adverse effects are often a result of the parasites dying and are therefore dependent on the disease. Possible adverse effects include, for example, in the treatment of strongyloidiasis: