Generic Name and Formulations:
Lomitapide mesylate 5mg, 10mg, 20mg, 30mg, 40mg, 60mg; caps.
Indications for JUXTAPID:
As an adjunct to low-fat diet and other lipid-lowering treatments, including LDL apheresis where available, to reduce LDL-C, total cholesterol, apo B, and non-HDL-C in patients with homozygous familial hypercholesterolemia (HoFH).
Limitations Of use:
Not established in patients with hypercholesterolemia who do not have HoFH, including those with heterozygous familial hypercholesterolemia (HeFH). Effect on cardiovascular morbidity, mortality has not been determined.
Before starting: measure ALT, AST, alkaline phosphatase, total bilirubin; obtain (–) pregnancy test; initiate low-fat diet supplying <20% of energy from fat. Swallow whole. Take 2hrs after PM meal with water. Initially 5mg once daily. Titrate dose based on safety and tolerability: increase to 10mg daily after at least 2 weeks; and then at a minimum of 4-week intervals, to 20mg, 40mg, and up to max 60mg daily. Supplement with daily Vit.E, linoleic acid, ALA, EPA, and DHA. ESRD on dialysis, baseline mild hepatic impairment: max 40mg daily. Concomitant weak CYP3A4 inhibitors (eg, alprazolam, amiodarone, amlodipine, atorvastatin, bicalutamide, cilostazol, cimetidine, cyclosporine, fluoxetine, fluvoxamine, ginkgo, goldenseal, isoniazid, lapatinib, nilotinib, pazopanib, ranitidine, ranolazine, ticagrelor, zileuton): max 30mg daily; except oral contraceptives: max 40mg daily. Dose adjustments for elevated transaminases: see full labeling.
<18yrs: not established.
Pregnancy (Cat.X). Concomitant moderate (eg, amprenavir, aprepitant, atazanavir, ciprofloxacin, crizotinib, darunavir/ritonavir, diltiazem, erythromycin, fluconazole, fosamprenavir, imatinib, verapamil) or strong (eg, boceprevir, clarithromycin, conivaptan, indinavir, itraconazole, ketoconazole, lopinavir/ritonavir, mibefradil, nefazodone, nelfinavir, posaconazole, ritonavir, saquinavir, telaprevir, telithromycin, tipranavir/ritonavir, voriconazole) CYP3A4 inhibitors. Moderate to severe hepatic impairment, active liver disease, unexplained persistent elevations of serum transaminases.
Risk of hepatotoxicity.
Elevations in transaminases and increases in hepatic fat may occur; measure ALT, AST, alkaline phosphatase, total bilirubin before initiating therapy, and then ALT, AST monthly or before any dose increase for 1st year; subsequently, at least every 3 months. Adjust dose if ALT or AST are ≥3xULN; discontinue if clinically significant liver injury, bilirubin ≥2xULN, or active liver disease occurs. Adhere to low-fat diet to reduce risk of GI effects. Galactose intolerance, Lapp lactase deficiency, glucose-galactose malabsorption: avoid. Chronic bowel or pancreatic diseases that predispose to malabsorption. Renal impairment. Females of reproductive potential: use effective contraception. Nursing mothers: not recommended.
Microsomal triglyceride transfer protein (MTP) inhibitor.
See Contraindications and Adults. Potentiated by CYP3A4 inhibitors (omit grapefruit juice). Potentiates warfarin; monitor INR. Risk of myopathy (including rhabdomyolysis) with simvastatin or lovastatin; reduce simvastatin dose by 50% (limit to 20mg daily [or 40mg daily for those previously tolerated simvastatin 80mg daily for ≥1 year without muscle toxicity]) or consider reducing lovastatin dose when initiating lomitapide. Consider dose reduction of P-gp substrates. Max one alcoholic drink/day. Caution with other hepatotoxic drugs (eg, isotretinoin, amiodarone, acetaminophen, methotrexate, tetracyclines, tamoxifen). Concomitant other LDL-lowering drugs: not recommended. Separate bile acid sequestrants by at least 4hrs.
Diarrhea (if severe, consider reducing dose or suspending use), nausea, dyspepsia, vomiting, abdominal pain; hepatotoxicity (including steatohepatitis, hepatic failure) possible, reduced absorption of fat soluble vitamins.
Juxtapid REMS Program: only certified providers and pharmacies may prescribe and distribute.
Hepatic (CYP3A4; 1A2, 2B6, 2C8, 2C19 (minor); 99.8% protein bound.
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