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Medications Lexicon

How does this medication work? What will it do for me?

Lomitapide belongs to the class of medications called triglyceride transfer protein inhibitors. It is used, in addition to a low-fat diet and other lipid lowering medications, to reduce the amount of LDL cholesterol ("bad" cholesterol) in the blood, for adults who have a genetic condition called homozygous familial hypercholesterolemia (HoFH) that causes the body to produce too much LDL cholesterol.

In the liver and gut cells, fatty substances are built into larger fat particles that are then released into the blood stream. Lomitapide works by blocking the production of these larger particles, reducing the amount of cholesterol in the blood.

This medication may be available under multiple brand names and/or in several different forms. Any specific brand name of this medication may not be available in all of the forms or approved for all of the conditions discussed here. As well, some forms of this medication may not be used for all of the conditions discussed here.

Your doctor may have suggested this medication for conditions other than those listed in these drug information articles. If you have not discussed this with your doctor or are not sure why you are taking this medication, speak to your doctor. Do not stop taking this medication without consulting your doctor.

Do not give this medication to anyone else, even if they have the same symptoms as you do. It can be harmful for people to take this medication if their doctor has not prescribed it.

How should I use this medication?

The recommended starting dose of lomitapide for adults is 5 mg taken once daily. After 2 weeks, the dose can be increased to 10 mg taken once daily. If necessary, the dose can be increased at 4 week intervals as it is tolerated. The maximum recommended dose is 60 mg daily. 

Lomitapide capsules should be swallowed whole with a glass of water. Do not open, crush, dissolve, or chew the capsules.

Food may cause side effects such as nausea and diarrhea, therefore, this medication should be taken without food, at least 2 hours after the evening meal.

Your doctor may also prescribe Vitamin E and essential fatty acids for you to take while you are taking lomitapide.  These supplements should not be taken at the same time as lomitapide. It is recommended that these dietary supplements be taken in the morning. 

Many things can affect the dose of medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones listed here, do not change the way that you are taking the medication without consulting your doctor.

It is important to take this medication exactly as prescribed by your doctor.

If you miss a dose, skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for a missed one. If you are not sure what to do after missing a dose, contact your doctor or pharmacist for advice.

Store this medication at room temperature, protect it from light and moisture, and keep it out of the reach of children.

Do not dispose of medications in wastewater (e.g. down the sink or in the toilet) or in household garbage. Ask your pharmacist how to dispose of medications that are no longer needed or have expired.

What form(s) does this medication come in?

5 mg
Each orange, hard gelatin capsule, printed with black ink "A733" and "5 mg", contains 6 mg lomitapide mesylate equivalent to 5 mg free base. Nonmedicinal ingredients: gelatin, lactose white monohydrate, magnesium stearate, microcrystalline cellulose, pregelatinized starch, red iron oxide, silicon dioxide, sodium starch glycolate, and titanium dioxide.

10 mg
Each orange/white, hard gelatin capsule, printed with black ink "A733" and "10 mg", contains 11 mg lomitapide mesylate equivalent to 10 mg free base. Nonmedicinal ingredients: gelatin, lactose white monohydrate, magnesium stearate, microcrystalline cellulose, pregelatinized starch, red iron oxide, silicon dioxide, sodium starch glycolate, and titanium dioxide.

20 mg
Each white, hard gelatin capsule, printed with black ink "A733" and "20 mg", contains 23 mg lomitapide mesylate equivalent to 20 mg free base. Nonmedicinal ingredients: gelatin, lactose white monohydrate, magnesium stearate, microcrystalline cellulose, pregelatinized starch, silicon dioxide, sodium starch glycolate, and titanium dioxide.

Who should NOT take this medication?

Do not take this medication if you:

  • are allergic to lomitapide or any ingredients of the medication
  • have moderate-to-severe liver impairment
  • have chronic bowel disease, such as inflammatory bowel disease or malabsorption
  • are using any of the following medications:
    • "azole" antifungals (e.g., fluconazole, itraconazole, voriconazole)
    • macrolide antibiotics (e.g., clarithromycin, erythromycin)
    • calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
    • HIV protease inhibitors (e.g., lopinavir, ritonavir, saquinavir)
    • nefazodone
  • are or may be pregnant
  • have one of the following rare hereditary diseases:
    • galactose intolerance
    • Lapp-lactase deficiency
    • glucose-galactose malabsorption

What side effects are possible with this medication?

Many medications can cause side effects. A side effect is an unwanted response to a medication when it is taken in normal doses. Side effects can be mild or severe, temporary or permanent.

The side effects listed below are not experienced by everyone who takes this medication. If you are concerned about side effects, discuss the risks and benefits of this medication with your doctor.

The following side effects have been reported by at least 1% of people taking this medication. Many of these side effects can be managed, and some may go away on their own over time.

Contact your doctor if you experience these side effects and they are severe or bothersome. Your pharmacist may be able to advise you on managing side effects.

  • belching/burping
  • constipation
  • decreased appetite
  • diarrhea
  • gas
  • heartburn
  • nausea
  • stomach cramping or pain
  • vomiting
  • weight loss

Although most of the side effects listed below don't happen very often, they could lead to serious problems if you do not check with your doctor or seek medical attention.

Check with your doctor as soon as possible if any of the following side effects occur:

  • signs of  liver problems (e.g., nausea, vomiting, diarrhea, loss of appetite, weight loss, yellowing of the skin or whites of the eyes, dark urine, pale stools)
  • signs of muscle breakdown (e.g., unexplained muscle pain or spasm, muscle cramps, dark brown urine)

Some people may experience side effects other than those listed. Check with your doctor if you notice any symptom that worries you while you are taking this medication.

Are there any other precautions or warnings for this medication?

Before you begin using a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health. These factors may affect how you should use this medication.

Alcohol use: Consuming alcohol when taking this medication increases the risk of liver damage. It is advisable to limit the amount of alcohol to no more than one drink daily while you are taking lomitapide.

Birth control: Women who may become pregnant while taking this medication should use effective birth control. Diarrhea or vomiting caused by lomitapide may cause oral contraceptives (birth control pills) to become ineffective. Use a second method of birth control until these symptoms subside.

Kidney function: Kidney disease or reduced kidney function may cause this medication to build up in the body, causing side effects. If you have reduced kidney function or kidney disease, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Liver function: Lomitapide may reduce liver function and cause a fatty liver. Liver disease or reduced liver function may cause this medication to build up in the body, causing side effects. If you have liver problems, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed. Your doctor may want to test your liver function regularly with blood tests while you are taking this medication.

If you experience symptoms of liver problems such as fatigue, feeling unwell, loss of appetite, nausea, yellowing of the skin or whites of the eyes, dark urine, pale stools, abdominal pain or swelling, and itchy skin, contact your doctor immediately.

Pregnancy: This medication should not be used by a woman who is pregnant as it may cause harm to the developing baby. If you become pregnant while taking this medication, contact your doctor immediately.

Breast-feeding: It is not known if lomitapide passes into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.

Children: The safety and effectiveness of using this medication have not been established for children.

What other drugs could interact with this medication?

There may be an interaction between lomitapide and any of the following:

  • abiraterone
  • acetaminophen
  • acetazolamide
  • alcohol
  • aliskiren
  • alpha blockers (e.g., alfuzosin, doxazosin, silodosin, tamsulosin)
  • amiodarone
  • anastrozole
  • angiotensin receptor blockers (ARBs; e.g., candasartan, irbesartan, losartan)
  • anticancer medications (e.g., cabazitaxel, docetaxel, doxorubicin, etoposide, ifosfamide, irinotecan, vincristine)
  • apomorphine
  • aprepitant
  • aripiprazole
  • atomoxetine
  • azelastine
  • "azole" antifungals (e.g., itraconazole, ketoconazole, voriconazole)
  • barbiturates (e.g., pentobarbital, phenobarbital)
  • benzodiazepines (e.g., chlordiazepoxide, clonazepam, diazepam, lorazepam)
  • bicalutamide
  • boceprevir
  • bosentan
  • bromocriptine
  • budesonide
  • buprenorphine
  • buspirone
  • busulfan
  • calcitriol
  • calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
  • canagliflozin
  • carbamazepine
  • carvedilol
  • cetirizine
  • cholestyramine
  • chloroquine
  • ciprofloxacin
  • cisapride
  • clozapine
  • colchicine
  • colesevelam
  • colestipol
  • conivaptan
  • cyclosporine
  • cyproterone
  • danazol
  • dantrolene
  • dapsone
  • dabigatran
  • deferasirox
  • desipramine
  • dexamethasone
  • diclofenac
  • digoxin
  • dihydroergotamine
  • disulfiram
  • disopyramide
  • dofetilide
  • doxycycline
  • dronedarone
  • entacapone
  • eplerenone
  • ergotamine
  • estrogens (e.g., conjugated estrogen, estradiol, ethinyl estradiol)
  • ethosuximide
  • etoposide
  • everolimus
  • felbamate
  • fentanyl
  • flutamide
  • "gliptin" diabetes medications (e.g., linagliptin, saxagliptin, sitagliptin)
  • glyburide
  • grapefruit juice
  • guanfacine
  • haloperidol
  • HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs; e.g., delaviridine, efavirenz, etravirine, nevirapine)
  • HIV protease inhibitors (e.g., atazanavir, indinavir, ritonavir, saquinavir)
  • hydralazine
  • hydrocodone
  • hydrocortisone
  • isoniazid
  • ivacaftor
  • lansoprazole
  • lidocaine
  • lomustine
  • loperamide
  • lurasidone
  • macrolide antibiotics (e.g., clarithromycin, erythromycin)
  • maraviroc
  • mefloquine
  • mestranol
  • methadone
  • methylprednisolone
  • metronidazole
  • mifepristone
  • mirtazapine
  • modafinil
  • montelukast
  • nadolol
  • nateglinide
  • nefazodone
  • nilotinib
  • nitrates (e.g., isosorbide dinitrate,  isosorbide mononitrate)
  • norfloxacin
  • olanzapine
  • ondansetron
  • oxcarbazepine
  • oxybutynin
  • oxycodone
  • paliperidone
  • perampanel
  • phenytoin
  • phosphodiesterase 5 inhibitors (e.g., sildenafil, tadalafil, vardenafil)
  • pilocarpine
  • pimecrolimus
  • pimozide
  • praziquantel
  • prednisolone
  • primidone
  • primaquine
  • progestins (e.g., dienogest, levonorgestrel, medroxyprogesterone, norethindrone)
  • proton pump inhibitors (e.g., lansoprazole, omeprazole)
  • quetiapine
  • quinidine
  • quinine
  • ranitidine
  • repaglinide
  • rifabutin
  • rifampin
  • rilpivirine
  • rivaroxaban
  • romidepsin
  • St. John's wort
  • salmeterol
  • saxagliptin
  • selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine, fluoxetine, paroxetine, sertraline)
  • selegiline
  • simeprevir
  • sirolimus
  • "statin" anti-cholesterol medications (e.g., atorvastatin, lovastatin, simvastatin)
  • stiripentol
  • tacrolimus
  • tamoxifen
  • telaprevir
  • temsirolimus
  • teniposide
  • tetracycline
  • theophylline
  • ticagrelor
  • ticlopidine
  • tocilizumab
  • tolterodine
  • tolvaptan
  • trabectedin
  • tramadol
  • trazodone
  • tretinoin
  • tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)
  • trimethoprim
  • tyroside kinase inhibitors (e.g., dasatinib, imatinib, pazopanib)
  • ulipristal
  • venlafaxine
  • warfarin
  • zafirlukast
  • zolpidem
  • zonisamide
  • zopiclone

If you are taking any of these medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to:

  • stop taking one of the medications,
  • change one of the medications to another,
  • change how you are taking one or both of the medications, or
  • leave everything as is.

An interaction between two medications does not always mean that you must stop taking one of them. Speak to your doctor about how any drug interactions are being managed or should be managed.

Medications other than those listed above may interact with this medication. Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications you are taking. Also tell them about any supplements you take. Since caffeine, alcohol, the nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them.

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