"Nov. 12, 2012 -- The requirement to fast before a cholesterol check can be a major inconvenience.
People who forget to fast may be told to reschedule their appointments. For those who remember, sitting in a doctor's waiting room with "...
- Clinician Information:
Juxtapid Side Effects Center
Reviewed by Melissa Conrad Stöppler, MD
Juxtapid (lomitapide) is indicated as an adjunct to a low-fat diet and other lipid-lowering treatments to help manage cholesterol. Juxtapid belongs to a class of drugs called microsomal triglyceride transfer protein inhibitors. The most common adverse reactions are diarrhea, nausea, vomiting, dyspepsia, and abdominal pain.
Juxtapid is taken orally . Juxtapid should be taken once daily, whole, with water and without food, at least 2 hours after evening meal. While on Juxtapid therapy, patients must avoid grapefruit juice. CYP3A4 inhibitors such as Serzone, Sporanox, Nizoral, Vfend, Reyataz, Biaxan and Ketek are contraindicated with Juxtapid. Juxtapid also reacts with warfarin (Coumadin), simvastatin (Zocor), and lovastatin (Altocor, Altoprev, Mevacor). Before treatment, women of reproductive potential must test negative for pregnancy. Juxtapid should not be used in pregnant women or nursing mothers.
Our Juxtapid (lomitapide) Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication.
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
What is Prescribing information?
The FDA package insert formatted in easy-to-find categories for health professionals and clinicians.
Juxtapid FDA Prescribing Information: Side Effects
The following important adverse reactions have been observed and are discussed in detail in other sections of the label:
- Risk of hepatotoxicity [see WARNINGS AND PRECAUTIONS]
- Reduced absorption of fat-soluble vitamins, and serum fatty acids [see WARNINGS AND PRECAUTIONS]
- Gastrointestinal adverse reactions [see WARNINGS AND PRECAUTIONS]
Clinical Trials Experience
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
One single-arm, open-label, 78-week trial has been conducted in 29 patients with HoFH, 23 of whom completed at least one year of treatment. The initial dosage of JUXTAPID was 5 mg daily, with titration up to 60 mg daily during an 18-week period based on safety and tolerability. In this trial, the mean age was 30.7 years (range, 18 to 55 years), 16 (55%) patients were men, 25 (86%) patients were Caucasian, 2 (7%) were Asian, 1 (3%) was African American, and 1 (3%) was multi-racial [see Clinical Studies].
Five (17%) of the 29 patients with HoFH that participated in the clinical trial discontinued treatment due to an adverse reaction. The adverse reactions that contributed to treatment discontinuations included diarrhea (2 patients; 7%) and abdominal pain, nausea, gastroenteritis, weight loss, headache, and difficulty controlling INR on warfarin (1 patient each; 3%).
The most common adverse reactions were gastrointestinal, reported by 27 (93%) of 29 patients. Adverse reactions reported by ≥ 8 (28%) patients in the HoFH clinical trial included diarrhea, nausea, vomiting, dyspepsia, and abdominal pain. Other common adverse reactions, reported by 5 to 7 (17-24%) patients, included weight loss, abdominal discomfort, abdominal distension, constipation, flatulence, increased ALT, chest pain, influenza, nasopharyngitis, and fatigue.
The adverse reactions reported in at least 10% of patients during the HoFH clinical trial are presented in Table 3.
Table 3: Adverse Reactions Reported in ≥ 10% of
Patients in the Clinical Trial in HoFH
|ADVERSE REACTION||N (%)|
|Abdominal pain||10 (34)|
|Abdominal discomfort||6 (21)|
|Abdominal distension||6 (21)|
|Gastroesophageal reflux disease||3 (10)|
|Defecation urgency||3 (10)|
|Rectal tenesmus||3 (10)|
|Decreased weight||7 (24)|
|Increased ALT||5 (17)|
|Chest pain||7 (24)|
|Back pain||4 (14)|
|Nervous System Disorders|
|Pharyngolaryngeal pain||4 (14)|
|Nasal congestion||3 (10)|
|Angina pectoris||3 (10)|
Adverse reactions of severe intensity were reported by 8 (28%) of 29 patients, with the most common being diarrhea (4 patients, 14%), vomiting (3 patients, 10%), increased ALT or hepatotoxicity (3 patients, 10%), and abdominal pain, distension, and/or discomfort (2 patients, 7%).
During the HoFH clinical trial, 10 (34%) of 29 patients had at least one elevation in ALT and/or AST ≥ 3x ULN (see Table 4). No clinically meaningful elevations in total bilirubin or alkaline phosphatase were observed. Transaminases typically fell within one to four weeks of reducing the dose or withholding JUXTAPID.
Table 4: Patient Incidence
of Transaminase Elevations During the HoFH Clinical Trial
|≥ 3 to < 5 x ULN||6 (21%)|
|≥ 5 to < 10 x ULN||3 (10%)|
|≥ 10 to < 20 x ULN||1 (3%)|
|≥ 20x ULN||0|
|≥ 3 to < 5 x ULN||5 (17%)|
|≥ 5 to < 10 x ULN||1 (3%)|
|≥ 10 to < 20 x ULN||0|
|≥ 20x ULN||0|
|Upper limits of normal (ULN) ranged from 33-41 international units/L for ALT and 36-43 international units/L for AST.|
Among the 19 patients who enrolled in an extension study following the HoFH clinical trial, one discontinued because of increased transaminases that persisted despite several dose reductions, and one temporarily discontinued because of markedly elevated transaminases (ALT 24x ULN, AST 13x ULN) that had several possible causes, including a drug-drug interaction between JUXTAPID and the strong CYP3A4 inhibitor clarithromycin [see DRUG INTERACTIONS].
Hepatic fat was prospectively measured using magnetic resonance spectroscopy (MRS) in all eligible patients during the HoFH clinical trial. After 26 weeks, the median absolute increase in hepatic fat from baseline was 6%, and the mean absolute increase was 8% (range, 0% to 30%). After 78 weeks, the median absolute increase in hepatic fat from baseline was 6%, and the mean absolute increase was 7% (range, 0% to 18%). Among the 23 patients with evaluable data, on at least one occasion during the trial, 18 (78%) exhibited an increase in hepatic fat > 5% and 3 (13%) exhibited an increase > 20%. Data from individuals who had repeat measurements after stopping JUXTAPID show that hepatic fat accumulation is reversible, but whether histological sequelae remain is unknown.
Read the entire FDA prescribing information for Juxtapid (Lomitapide Capsules) »
Additional Juxtapid Information
Report Problems to the Food and Drug Administration
You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.
Tips to keep it under control.