Formulary
Lomitapide: Indications, Dosing, Side Effects and Interactions
Lomitapide, an inhibitor of microsomal triglyceride transfer protein (MTP), reduces lipoprotein secretion and circulating concentrations of lipoprotein-borne...
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Lomitapide: Indications, Dosing, Side Effects and Interactions
Lomitapide, an inhibitor of microsomal triglyceride transfer protein (MTP), reduces lipoprotein secretion and circulating concentrations of lipoprotein-borne...
Drug action
Lomitapide, an inhibitor of microsomal triglyceride transfer protein (MTP), reduces lipoprotein secretion and circulating concentrations of lipoprotein-borne lipids such as cholesterol and triglycerides.
Indications and dose
**Adjunct to dietary measures and other lipid-regulating drugs with or without low-density lipoprotein apheresis in homozygous familial hypercholesterolaemia (under expert supervision)**
- **Adult** (By Mouth): Initially 5 mg daily for 2 weeks, dose to be taken at least 2 hours after evening meal, then increased if necessary to 10 mg daily, for at least 4 weeks, then increased to 20 mg daily for at least 4 weeks, then increased in steps of 20 mg daily, adjusted at intervals of at least 4 weeks; maximum 60 mg per day.
Cautions
Concomitant use of hepatotoxic drugs; lomitapide can interfere with the absorption of fat-soluble nutrients and supplementation of vitamin E and fatty acids is required; patients over 65 years
Contraindications
Significant or chronic bowel disease
Side effects
Common or very common Aerophagia; appetite abnormal; asthenia; burping; constipation; diarrhoea; dizziness; gastrointestinal discomfort; gastrointestinal disorders; haemorrhage; headaches; hepatic disorders; increased risk of infection; muscle complaints; nausea; skin reactions; vomiting; weight decreased Uncommon Anaemia; chest pain; chills; dehydration; drowsiness; dry mouth; eye swelling; fever; gait abnormal; hyperhidrosis; joint disorders; malaise; pain in extremity; paraesthesia; throat lesion; upper-airway cough syndrome; vertigo Frequency not known Alopecia Side-effects, further information Reduce dose if serum transaminases raised during treatment (consult product literature).
Interactions
**Other interactions (6):**
- LIPID-MODIFYING AGENTS Lomitapide Interaction not studied with any of the components of Elvitegravir/Cobicistat/Emtricitabine/Tenofovir Alafenamide Gilead.
- Lomitapide is highly dependent on CYP3A for its metabolism and co-administration with Elvitegravir/Cobicistat/Emtricitabine/Tenofovir Alafenamide Gilead may result in increased concentrations of...
- Lipid-modifying agents Lomitapide CYP3A4 inhibitors increase the exposure of lomitapide, with strong inhibitors increasing exposure approximately 27-fold.
- Due to CYP3A inhibition by lopinavir/ritonavir, concentrations of lomitapide are expected to increase.
- Lomitapide: The risk of myopathy and rhabdomyolysis may be increased by concomitant administration of lomitapide with simvastatin (see sections 4.3 and 4.4).
- Lomitapide Diltiazem (a moderate CYP3A4 inhibitor) may increase lomitapide plasma concentrations through CYP3A4 inhibition leading to increased risk of elevations in liver enzymes (see section 4.3).
Pregnancy
Avoid-teratogenicity and embryotoxicity in animal studies.
Breast feeding
Manufacturer advises avoid-no information available.
Hepatic impairment
Manufacturer advises avoid in moderate to severe impairment, or if unexplained persistent abnormal liver function tests. Dose adjustments Manufacturer advises max. 40 mg daily in mild impairment.
Renal impairment
Dose adjustments Max. 40 mg daily in end-stage renal disease. M
Medicinal forms
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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