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Lomitapide is approved for adjuvant treatment of HoFH in many countries and has important clinical value.
1. Generic name : Lomitapide (Lomitapide)
2. Trade name : JUXTAPID™
3. Dosage form : Oral hard capsule
< b>4. Main ingredient :Each capsule contains lomitapide mesylate (equivalent to 5mg, 10mg or 20mg base)
5. Excipients : Pregelatinized starch, microcrystalline cellulose, lactose monohydrate, silicon dioxide, magnesium stearate; capsule shell contains gelatin, titanium dioxide, iron oxide red (5mg/10mg specification) and black printing ink.
1. Homozygous familial hypercholesterolemia (HoFH) : As an adjunct to low-fat diet and other lipid-lowering treatments (including LDL plasma exchange), it is used to reduce low-density lipoprotein cholesterol (LDL-C), total cholesterol (TC), apolipoprotein B (apoB) and non-HDL cholesterol (non-HDL-C).
2. Limitation : The safety and effectiveness in non-HoFH patients have not been established, and the impact on cardiovascular outcomes has not been clear.
3. Specifications and properties of
1. Specifications of : 5mg (orange/orange capsules), 10mg (orange/white capsules), 20mg (white/white capsules), 28 capsules per bottle.
2. Characteristics : Opaque hard capsule, printed with a black logo "A733" and the corresponding dosage.
1. Initial treatment : 5 mg once a day, take on an empty stomach (at least 2 hours after a meal), swallow the whole tablet.
2. Dose titration : Gradually increase to 10mg (≥2 weeks later), 20mg (≥4 weeks later), 40mg (≥4 weeks later) based on tolerance, up to a maximum of 60mg/day.
3. Missed dose handling : Skip the missed dose and take it at the original planned time the next day; if the interruption exceeds 1 week, re-evaluation is required.
4. Nutritional supplement : Daily supplement of vitamin E (400IU) and essential fatty acids (such as linoleic acid, EPA/DHA) is required.
1. Abnormal liver function : When ALT/AST ≥ 3 times the upper limit of normal (ULN), the dose needs to be reduced or suspended; when ≥ 5 times ULN, the drug needs to be discontinued.
2. Special groups :
The dose for dialysis patients with end-stage renal disease or mild liver injury (Child-PughA) should not exceed 40 mg/day.
Contraindicated for moderate to severe liver damage (Child-PughB/C).
1. Monitoring requirements : Baseline and regular detection of ALT/AST, alkaline phosphatase, and total bilirubin; pregnant women need contraception.
2. Dietary restrictions : Strictly follow a low-fat diet (fat provides energy <20%) and avoid alcohol (≤1 cup per day).
3. Drug interaction :
It is prohibited to use strong/moderate CYP3A4 inhibitors (such as clarithromycin, itraconazole) in combination.
When combined with weak CYP3A4 inhibitors (such as atorvastatin), the dose should not exceed 30 mg/day.
Warfarin requires close monitoring of INR.
1. Pregnant women : Disabled (animals show teratogenicity).
2. During lactation : Discontinue medication or stop breastfeeding.
3. Children : Safety has not been established.
4. Elderly people : Be cautious and consider decreased liver and kidney function.
1. Common (≥28%) : Diarrhea (79%), nausea (65%), vomiting (34%), indigestion (38%), abdominal pain (34%).
2. Severe but rare : Hepatotoxicity (increased ALT/AST, hepatic steatosis), gastrointestinal bleeding, myopathy (combined with statins).
1. Women who are pregnant or planning pregnancy.
2. Combined use with strong/moderate CYP3A4 inhibitors.
3. Moderate to severe liver damage or active liver disease.
1. CYP3A4 inhibitor : Significantly increases the plasma concentration of lomitapide (strong inhibitors can increase it 27 times).
2. Statin : The dose of simvastatin needs to be halved (lomitapide doubles the exposure).
3. P-gp substrate : It may increase the absorption of digoxin and other drugs, so dosage reduction needs to be considered.
Save at room temperature (20-25°C), avoid moisture and light, and keep the container tightly closed.
Manufacturer :Aegerion Pharmaceuticals, Inc. (USA)
Note : If persistent diarrhea, jaundice or severe abdominal pain occurs during medication, seek medical attention immediately. Specific medication must comply with the requirements of the JUXTAPIDREMS plan.