Lomitapide (Oral)

Along with a healthy diet and exercise program, lomitapide is used to help lower cholesterol in patients, thereby reducing the risk of heart problems developing.


Lomitapide is a prescription drug which is only made available currently through a Risk Evaluation and Mitigation Strategy, which the FDA requires of any drug which carries certain risks as well as benefits to patients. It is available in capsule form and must be used under doctor supervision so that any signs of adverse symptoms can quickly be identified and treated.

This medication reduces the levels of low-density lipoproteins (LDL) and non-high-density lipoprotein (non-HDL), in addition to lowering the level of a protein which is known to be a carrier of bad cholesterol in the bloodstream. However, the medication is not used in standalone mode by doctors, and they will always prescribe a program of low-fat diet as well as healthy foods to take their place, all in conjunction with regular exercise. The combined effects of this holistic approach is what is most effective in lowering bad cholesterol.

The specific kind of high cholesterol medical condition which lomitapide is most effective in managing is one which is inherited, and is known as homozygous familial hypercholesterolemia. This condition is known to cause high levels of cholesterol in patients consistently, even if they are living a reasonably healthy lifestyle. The risk associated with taking this medication, and the reason it is only available through the REMS program, is that it has a tendency to cause elevated levels of liver enzymes, as well as increased fatty deposits in the liver, and the potential to make the liver toxic. For this reason, patients being treated with lomitapide must be closely monitored by a doctor, so that any impact on the liver can be assessed and treated immediately, if necessary.

Condition Treated

High Cholesterol

Type Of Medicine


Side Effects

As is the case with most medications, lomitapide may carry certain side effects in addition to the beneficial medical impact that it has on a patient. If you should experience any of the side effects listed below to a degree which makes it uncomfortable for you, you should contact your doctor at the earliest opportunity or at the next appointment, so you can describe which side effects you are feeling, and how severe they are in your case.

One of the first side effects to be concerned about is the possibility of an allergic reaction because the symptoms in this case can become extreme to the point where they are life-threatening. Some of the signs to look for in an allergic reaction are the following:

  • Hives and/or rashes appearing on skin surfaces
  • Itchiness at various locations around the body
  • Dizziness or lightheadedness, often with the sensation you are about to faint
  • Tightness in the chest, sometimes accompanied by extreme difficulty with breathing
  • Pronounced swelling or puffiness around the eyelids, or on the tongue, lips, or throat.

While allergic reactions to this medication are extremely rare, there are other side effects which are more commonly experienced by patients. Some patients may experience no side effects whatsoever when taking lomitapide, but others may experience several side effects, and some of them may even be severe. One of the primary differences in the kind of experience a patient will have when taking this medication is due to personal body chemistry, and this accounts for the wide difference in experiences.

Some of the most commonly reported side effects for patients taking lomitapide are the following:

  • Pain or cramping in the abdomen
  • Unexplained weakness or tiredness
  • Profuse sweating
  • Nausea and vomiting
  • Fast or irregular heartbeat
  • Urine which is dark-colored
  • Pain or cramping in the stomach
  • Chest discomfort or pains
  • Heaviness or tightness in the chest
  • Fevers and/or chills
  • Loss of appetite
  • Light-colored stools
  • Difficulty with breathing
  • Yellowish tinge to the skin or around the eyes
  • Pain in the arms, jaw, or lower back
  • Acid or sour stomach
  • Persistent diarrhea
  • Light-headedness or dizziness
  • Rapid weight loss
  • Uncharacteristic belching
  • Constipation
  • Persistent coughing
  • Excess gas in the intestines or in the stomach
  • More frequent bowel movements
  • Difficulty with sleeping
  • Swelling in the area of the stomach or abdomen
  • Runny nose or stuffy nose
  • Pressure on the stomach
  • Shivering and trembling
  • Sore throat
  • Upset stomach
  • Difficulty with having bowel movements
  • General feeling of illness or discomfort
  • Persistent headaches
  • Frequent heartburn
  • Pain in the joints
  • Muscle pains and aches
  • Frequent flatulence
  • Full or bloated sensation
  • Unusual weakness in the limbs.


There is a medication guide which will be issued with this drug, and every patient should read this information carefully, and make sure that it is understood before taking the drug. If you have any questions, your doctor will be able to answer them for you, so that you have a full understanding of proper usage.

Lomitapide should be taken two hours before an evening meal, on an empty stomach. If you don't have a problem swallowing pills, you should swallow the entire capsule with a glass of water without chewing, crushing, breaking, or dissolving the capsule. If you have difficulty with swallowing pills in this manner, you should alert your doctor to this fact right away, because this medication may not be appropriate for you.

It's also possible that in addition to lomitapide, your doctor will recommend that you take vitamin and fatty acid supplements along with it, to help avoid any kind of problems with your stomach. If you are concurrently taking cholestyramine or colesevelam, either of these must be ingested at least four hours before taking lomitapide.

While you are being treated with this medicine, you should avoid alcohol entirely, because it can cause fairly severe problems with your liver. You should also avoid drinking grapefruit juice for the entire time frame that you are taking lomitapide.

A standard dosage of lomitapide recommended for adults for the treatment of bad cholesterol is 5 mg once each day, although your doctor will likely make adjustments to this dosage, depending on its effectiveness in treating the condition, as well as your body's tolerance to the medication. It is rare for any patient to be prescribed a dosage exceeding 60 mg in a single day. Any pediatric patients for whom lomitapide is prescribed will need to have a specific dosage calculated for them by the family doctor.

If you should miss a dosage of lomitapide, the best thing to do is simply skip that dosage, and wait until the next regularly scheduled dosage. You should not double up on doses simply to get back on schedule with your normal routine. If for some reason you should discontinue taking lomitapide for more than a week, do not start up again without consulting with your doctor, as you may be subject to adverse effects from the sudden restart of treatment.


There is a possibility when taking lomitapide, that it may interact with other medications you may be concurrently taking. When drug interactions occur, there is always the potential for any side effects that you are experiencing to become worsened, or to trigger new side effects entirely. It's also possible that either of the two drugs, or both of them, will have their effectiveness diminished by an interaction. Since neither of these scenarios is favorable, both doctor and patient should do everything possible to prevent the potential for drug interactions.

As the patient, you should do your part by preparing a list of all medications you are currently using, including vitamins, herbal supplements, other prescription drugs, and over-the-counter drugs, as well as all of the dosages of each one of these. Your doctor will be able to review this list, and make a determination on whether or not any of these medications might interfere with lomitapide.

You can also take a copy of this medication list with you to any health care clinic where your primary care doctor may not be in residence, or to an emergency room clinic if you should have a need for unplanned medical treatment. Any doctor at one of these facilities will be able to review your list and prescribe a program of treatment for your medical condition which does not conflict with any of the drugs you are taking.

While you are taking lomitapide, you should not eat grapefruit or drink grapefruit juice, because there is strong possibility that it will produce undesirable side effects. You should avoid eating foods that are high in fats or cholesterol because lomitapide will not be as effective if you continue to eat foods that are high in cholesterol and fats. You should not drink alcohol while taking lomitapide because it can produce some undesirable side effects on your liver. When you are taking either cholestyramine or colesevelam in conjunction with lomitapide, you should make sure to take those other medicines at least four hours before taking lomitapide, and under no circumstances should you take either one of them at the same time as lomitapide.

Some of the medications which are most commonly checked by doctors for the potential of interaction with lomitapide are those on the list below:

  • Benzonatate
  • Carisoprodol
  • Phenazopyridine
  • Armodafinil
  • Esomeprazole
  • Diphenhydramine
  • Dicyclomine
  • Mesalamine
  • Sumatriptan
  • Estradiol topical
  • Pentosan polysulfate sodium
  • Amitriptyline
  • Mipomersen
  • Polyethylene glycol 3350
  • Metreleptin
  • Rizatriptan
  • Bifidebacterium infantis
  • Lactobacillus acidophilus
  • Immunoglobulin subcutaneous
  • Benzoic acid
  • Sodium salicylate
  • Methanamine
  • Sucralfate
  • Buspirone,

In addition to medications which may interact with lomitapide, the drug can also impact some medical conditions which you may have. If you have any of the medical conditions listed below in your medical history, you should consult with your doctor before taking lomitapide:

  • Liver impairment
  • Vitamin deficiency
  • Galactosemia
  • Renal impairment
  • Alcoholic abuse.


While you are being treated with lomitapide, you should be sure to keep all scheduled appointments with your doctor, because it would be very important to monitor your cholesterol levels during this time frame, and it will also be very important to ensure that no harm is being imparted to your liver. For this purpose, it is likely that you will need to have blood tests taken periodically to assess any potential damage to your liver.

If you should notice that you develop severe diarrhea, experience changes to your frequency of urination, or that you experience severe light-headedness or tiredness when taking lomitapide, you should contact your doctor as soon as possible and report these symptoms.

If you are taking either lovastatin or simvastatin in conjunction with lomitapide there is a potential for a serious muscle problem to develop called myopathy. If you should notice any unexplained muscle weakness, tenderness, or pains, you should report these to your doctor as soon as possible.

You should also contact your doctor if you develop any kinds of pains in your stomach, or if you notice dark-colored urine, pale stools, decreasing appetite, nausea and vomiting, or a yellowish color to your skin or eyes. All of these could be symptomatic of a liver problem, which would necessitate either a reduction in dosage level or discontinuance of the medication.

Any women of child-bearing age, should not become pregnant while taking lomitapide, and that means that effective means of birth control should always be used while on a program of treatment with this medicine. In fact, before even being prescribed lomitapide, your doctor will require a negative pregnancy test, to ensure that you are not pregnant before beginning the program.

If you were to become pregnant while using lomitapide, there is a definite potential for harm to the unborn fetus, so this is something that should be avoided at all costs. If you should miss a period while being treated with lomitapide, you should immediately contact your doctor and have a pregnancy test taken.

There are a number of medications which you should not take while you are also taking lomitapide, due to the danger of causing serious side effects. Those medications are the following:

  • Aprepitant
  • Boceprevir
  • Conivaptan
  • Crizotinib
  • Diltiazem
  • Imatinib
  • Atazanavir
  • Ritonavir
  • Ciprofloxacin
  • Clarithromycin
  • Erythromycin
  • Fluconazole
  • Nefazodone
  • Lopinavir
  • Saquinavir
  • Ketoconazole
  • Itraconazole.


Lomitapide should be stored at room temperature in a location which is not subject to any extremes of direct light, cold, heat, or humidity, since any of these could degrade the effectiveness of the medication. It should also be stored in a location well out of the reach of any household pets or small children since indigestion could cause serious problems for them. If you suspect that a child has swallowed lomitapide, you should contact your Poison Control Center immediately and follow any instructions that are given. You should also not store lomitapide in a weekly pill reminder because these containers seldom have locking mechanisms which prevent unwanted access.

If your lomitapide medication expires, or if you have unused medication which you don't need, you should not simply flush it down the sink or down the toilet, as this could eventually cause harm to others. Instead, you should discard any unused medication according to proper disposal methods given you by your doctor or pharmacist. Lacking this information, you can also consult the FDA website on the safe disposal of medicines.


Lomitapide is a medication used in the treatment of a specific kind of high cholesterol which is inherited from family members, and which is only available by prescription and through a REMS program which requires constant monitoring and evaluation of patient progress. It is most effective when used in a program that includes a diet low in fats and cholesterol, and with proper exercise. There is a potential for this medication to cause liver damage to a patient, and it is for this reason that the drug is included in the REMS program.