IVERKOT 6

Dosage

Children: Refer to specific formulation guidelines as excipients are not dosed individually.

Adults: Refer to specific formulation guidelines as excipients are not dosed individually.

Mechanism of action

Excipients do not have a pharmacological mechanism of action in the way active drugs do; instead, they facilitate the delivery and absorption of the active pharmaceutical ingredients (APIs) in the body, improving the overall pharmacokinetics and bioavailability of the medication.

Pharmacodynamics

As excipients are inactive, they do not have pharmacodynamic properties. However, the choice of excipient can influence the release profile of the active ingredient, alter the drug's stability, and affect the solubility and bioavailability of the drug, which are critical for ensuring that the intended therapeutic effects are achieved.

Pharmacokinetics

Excipients generally do not undergo pharmacokinetic processes like absorption, distribution, metabolism, and excretion as active drugs do. They are usually considered inert, but their physical and chemical properties can influence the pharmacokinetics of the active ingredients they accompany. For example, some excipients may enhance the solubility of the active ingredient, facilitating better absorption in the gastrointestinal tract.

Pregnancy

Safety during pregnancy has not been established for all excipients. Some may pose risks while others are generally considered safe. Consultation with healthcare professionals is advised.

Breast-feeding

The safety of excipients during breastfeeding varies depending on the specific excipient. It is essential to consult healthcare professionals.

Storage

Excipients should be stored according to the specific requirements of the formulation they are a part of. Generally, they should be kept in a cool, dry place away from light.

Indications

• Onchocerciasis (river blindness)
• Strongyloidiasis
• Scabies (especially hyperkeratotic or crusted scabies)
• Lymphatic filariasis
• Other helminth infections

Dosage

Children: Child 6 months–17 years: 100 mg for 1 dose;

Adults: Adult: Initially 1 mg/kg daily on the first day, then increased to 6 mg/kg daily in divided doses, gradually increased over 3 days. Maximum 9 mg/kg per day. For scabies, 100 mg for 1 dose; if reinfection occurs, a second dose may be given after 2 weeks.

Mechanism of action

Ivermectin binds selectively to glutamate-gated chloride channels, leading to increased permeability of the cell membrane to chloride ions. This results in hyperpolarization of the nerve or muscle cells in the parasites, causing paralysis and death. It also interacts with other chloride channels, which may contribute to its antiparasitic effects.

Pharmacodynamics

Ivermectin exhibits broad-spectrum activity against a variety of parasites, including nematodes and arthropods. Its effectiveness is attributed to its ability to paralyze and kill parasites, thus facilitating their expulsion from the host. The drug has a long half-life, allowing for effective dosing regimens, and it is generally well-tolerated in patients.

Pharmacokinetics

Ivermectin is rapidly absorbed following oral administration, with peak plasma concentrations occurring within 4 to 6 hours. It is extensively distributed throughout the body, including the central nervous system. The drug undergoes hepatic metabolism, primarily via cytochrome P450, and is eliminated with a half-life of approximately 18 hours. Excretion occurs mainly in the feces, with a smaller proportion eliminated in urine.

Contra-indications

• Blood disorders
• Epilepsy
• Sjögren’s syndrome

Adverse effects

• Diarrhoea
• Dizziness
• Headache
• Influenza-like illness
• Insomnia
• Myalgia
• Nausea
• Rash
• Seizure
• Taste alteration
• Vomiting
• Skin reactions
• Abnormal sensation in eye
• Anaemia
• Appetite decrease
• Asthenia
• Asthma exacerbated
• Chest discomfort
• Confusion
• Conjunctival haemorrhage
• Constipation
• Gastrointestinal discomfort
• Headache
• Hepatitis
• Hypotension
• Joint disorders
• Leukopenia
• Myalgia
• Nausea
• Oedema
• Pain
• Psychiatric disorder
• Severe cutaneous adverse reactions
• Stupor
• Tachycardia
• Tremor
• Urinary incontinence
• Vertigo

Interactions

• Coumarins: Unknown (increases anticoagulant effect)
• Levamisole: Unknown (increases exposure)

Precautions

• Use with caution in hepatic impairment
• Avoid sun exposure when using topical formulations

Pregnancy

Embryotoxic in animal studies, avoid if possible.

Breast-feeding

Manufacturer advises avoid-limited information available; ensure infant does not come in contact with treated areas.

Storage

Store in a cool, dry place away from direct sunlight.

Formulations

• Tablets
• Topical formulation