VETo-MIDIUM 1000MG/ML POWDER

Indications

• African sleeping sickness (Trypanosomiasis)
• Trypanosoma brucei gambiense infections

Dosage

Children: Refer to the BNF for Children for appropriate paediatric dosing guidelines.

Adults: Refer to the latest clinical guidelines or BNF for specific dosing information.

Mechanism of action

Isomethamidium exerts its effects by inhibiting the activity of the enzyme cytochrome c oxidase in the mitochondrial respiratory chain of the trypanosomes. This inhibition leads to a decrease in ATP production, ultimately resulting in the death of the parasite. Additionally, isomethamidium may impact the membrane potential of the trypanosomal cells, further contributing to its antiparasitic activity.

Pharmacodynamics

The pharmacodynamics of isomethamidium involve its selective toxicity towards trypanosomes, allowing it to effectively target and kill the parasites while having minimal effects on human cells. The drug demonstrates a dose-dependent response, with higher concentrations leading to increased lethality against the parasite. The onset of action varies depending on the severity of the infection and the specific strain of the parasite.

Pharmacokinetics

Isomethamidium is administered intramuscularly and has a relatively good bioavailability. It is distributed throughout the body, with a tendency to accumulate in tissues such as the liver and spleen. The drug is metabolized in the liver, with metabolites excreted primarily via the urine. The half-life of isomethamidium varies, but it generally exhibits a prolonged duration of action, allowing for once-daily dosing in some cases.

Contra-indications

• Hypersensitivity to isomethamidium
• Severe liver impairment
• Severe renal impairment

Adverse effects

• Hypotension
• Dizziness
• Nausea
• Vomiting
• Abdominal pain
• Headache

Interactions

• May interact with other antihypertensive agents, potentially leading to additive hypotensive effects
• Caution with concomitant use of drugs that affect liver enzymes, as isomethamidium is metabolized in the liver

Precautions

• Use with caution in patients with a history of cardiovascular disease
• Monitor blood pressure regularly during treatment
• Consider potential drug interactions before prescribing

Pregnancy

Isomethamidium should only be used during pregnancy if the potential benefit justifies the potential risk to the fetus. There are limited studies on its safety in pregnant women.

Breast-feeding

Caution is advised when administering isomethamidium to breastfeeding mothers. The effects on the nursing infant are unknown.

Storage

Store in a cool, dry place away from light. Keep out of reach of children.

Formulations

• Injectable solution