Ivacure

Approved Indications:

• Onchocerciasis (River Blindness): Treatment of infection caused by Onchocerca volvulus.
• Strongyloidiasis: Treatment of Strongyloides stercoralis infection.
• Other Helminth Infections:
• Scabies (including crusted scabies).
• Pediculosis (head lice).
• Filariasis caused by Wuchereria bancrofti (used in mass drug administration).
• Off-label/Clinically Accepted Uses:
• Treatment of other parasitic infections such as Demodex mites.
• Investigational use in some viral diseases (e.g., off-label use in COVID-19 with limited evidence and not widely approved).

Adults:

• Strongyloidiasis and Onchocerciasis:
  150–200 mcg/kg orally as a single dose. Repeat dosing intervals vary by indication (e.g., every 3–6 months for onchocerciasis).
• Scabies:
  200 mcg/kg orally, repeated after 1–2 weeks.
• Pediculosis:
  Single dose of 200 mcg/kg orally, may repeat if needed.

Pediatrics:

• Approved for children ≥15 kg body weight.
• Dose: 150–200 mcg/kg orally, similar frequency as adults.

Elderly:

• No dose adjustment required; monitor for tolerance.

Special Populations:

• Renal Impairment: Use with caution; limited data.
• Hepatic Impairment: Use caution in moderate to severe impairment due to hepatic metabolism.

Administration:

• Oral tablets, taken with water on an empty stomach (1 hour before or 2 hours after a meal) to maximize absorption.

Ivermectin exerts its antiparasitic effect by binding selectively and with high affinity to glutamate-gated chloride ion channels present in invertebrate nerve and muscle cells. This binding increases permeability to chloride ions, leading to hyperpolarization, paralysis, and death of the parasite. It does not readily cross the blood-brain barrier in humans, minimizing neurotoxicity. Ivermectin is effective against a broad range of parasites by disrupting neurotransmission and muscle function.

• Absorption: Rapid oral absorption, peak plasma concentrations reached in 4 hours.
• Bioavailability: Increased when taken with a high-fat meal.
• Distribution: Highly lipophilic; wide distribution including skin and fat tissues.
• Metabolism: Extensive hepatic metabolism via CYP3A4 to inactive metabolites.
• Half-life: Approximately 12–36 hours.
• Elimination: Primarily fecal (~90%); minimal renal excretion.

• Pregnancy:
  FDA Category C. Animal studies show some risk at high doses. Use only if clearly needed and after risk-benefit assessment.
• Lactation:
  Excreted in low concentrations in breast milk. Caution advised; avoid breastfeeding if possible during treatment.

• Primary Class: Anthelmintic (Antiparasitic agent)
• Subclass: Macrocyclic lactone

• Known hypersensitivity to ivermectin or formulation excipients.
• Use in children weighing less than 15 kg or under 5 years of age (limited safety data).
• Coadministration with drugs causing significant CNS depression should be cautious.

• Central Nervous System Effects: Rare neurotoxicity (dizziness, ataxia, seizures) especially with overdose or blood-brain barrier disruption.
• Mazzotti Reaction: In onchocerciasis, inflammatory reaction due to dying microfilariae; monitor closely.
• Liver Dysfunction: Caution in severe hepatic impairment.
• Use in Immunocompromised Patients: Monitor closely for adverse effects.
• Avoid coadministration with other neurotoxic drugs when possible.

Common:

• Mild gastrointestinal symptoms (nausea, diarrhea).
• Dizziness, headache.
• Fatigue.
• Skin rash or pruritus (especially in onchocerciasis treatment).

Less Common:

• Fever.
• Hypotension.
• Muscle pain.

Serious/Rare:

• Severe allergic or hypersensitivity reactions.
• Neurotoxicity symptoms (rare).
• Mazzotti reaction in filariasis patients.

• CYP3A4 inhibitors (e.g., ketoconazole, erythromycin): May increase ivermectin plasma levels and toxicity risk.
• CYP3A4 inducers (e.g., rifampin): May reduce efficacy by lowering plasma levels.
• Other CNS depressants: Additive sedation or neurotoxicity risk.
• Food, especially high-fat meals, may increase bioavailability.

• Ivermectin remains first-line for strongyloidiasis and onchocerciasis according to WHO guidelines.
• Not approved for COVID-19 treatment; recent health authorities caution against off-label use outside clinical trials.
• Updated safety monitoring advised in mass drug administration programs.

• Store at 20°C to 25°C (68°F to 77°F).
• Protect from moisture and light.
• Keep tablets in original container until use.
• No refrigeration or special handling required.