Lovastatin / niacin Side Effects
Some side effects of lovastatin / niacin may not be reported. Always consult your doctor or healthcare specialist for medical advice. You may also report side effects to the FDA.
For the Consumer
Applies to lovastatin / niacin: oral tablet extended release
Get emergency medical help if you have any of these signs of an allergic reaction while taking lovastatin / niacin: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.
Stop taking this medicine and call your doctor at once if you a serious side effect such as:
unexplained muscle pain, tenderness, or weakness;
confusion, memory problems;
fever, unusual tiredness, and dark colored urine;
chest pain, extreme dizziness, feeling like you might pass out;
swelling, weight gain, urinating less than usual or not at all;
high blood sugar (increased thirst, increased urination, hunger, dry mouth, fruity breath odor, drowsiness, dry skin, blurred vision, weight loss); or
nausea, upper stomach pain, itching, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes).
Less serious side effects of lovastatin / niacin may include:
headache, mild dizziness;
diarrhea, mild nausea, stomach pain or indigestion;
mild skin rash;
flushing (warmth, redness, or tingly feeling); or
cold symptoms such as stuffy nose, sneezing, sore throat.
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects.
For Healthcare Professionals
Applies to lovastatin / niacin: oral tablet extended release
Musculoskeletal side effects associated with the administration of lovastatin have included elevations in creatine kinase, muscle cramps, myopathy, and rhabdomyolysis. Other musculoskeletal side effects reported with HMG-CoA reductase inhibitors have included arthralgia and myalgia.
In addition, some data have suggested that exposure to HMG-CoA reductase inhibitors is associated with a decreased risk of bone fractures in persons older than 50 years of age.
Lovastatin has been associated with rare cases of severe myopathy and rhabdomyolysis, manifested as elevations in creatine kinase, myoglobinuria, proteinuria, and renal failure. These conditions appear to be dose related, usually occurring with doses greater than 30 mg per day.
Concomitant use of lovastatin-niacin and potent inhibitors of CYP450 3A4 (i.e., cyclosporine, antifungal azoles, macrolide antibiotics, ketolide antibiotics, HIV protease inhibitors, large amounts of grapefruit juice) or other drugs known to cause myopathy (i.e., gemfibrozil) is associated with an increased risk of myotoxicity.
Myopathy and/or rhabdomyolysis have also been reported when lovastatin is used in combination with lipid-altering doses (greater than or equal to 1 g/day) of niacin.
Patients should be instructed to report promptly symptoms of muscle pain, weakness, or tenderness. If such symptoms develop, creatine kinase should be measured, and if markedly elevated, lovastatin should be discontinued. The value of routine monitoring of creatine kinase is not known. In some studies up to 11% of patients experienced elevations in creatine kinase while on lovastatin. In most cases these elevations were mild, transient, and not associated with clinical symptoms.
Itraconazole used concomitantly with lovastatin has led to one reported case of severe rhabdomyolysis in a 63-year-old woman. Caution should be exercised when HMG-CoA reductase inhibitors and azole antifungals are prescribed concurrently.
Dermatologic side effects associated with the administration of lovastatin have included rash and pruritus. Other dermatologic side effects reported with HMG-CoA reductase inhibitors have included erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, photosensitivity, dermatomyositis, purpura, and alopecia. These effects may be manifestations of a hypersensitivity reaction.
Dermatologic side effects associated with the administration of niacin have included flushing (facial and whole body) and pruritus. Rare cases of hyperpigmentation and acanthosis nigricans have been reported.
Niacin-related flushing (facial and whole body) and pruritus occur as a result of stimulation and release of prostaglandins and have been major drawbacks of this drug. These symptoms have occurred in up to 78% of patients and usually resolved after 2 weeks of continued therapy. Flushing can be minimized with use of an extended release form of the drug, gradual dosage titration (over 2 to 3 months), and by administering the dosage during or within 30 minutes after meals. Aspirin (325 mg), if not otherwise contraindicated), taken within 30 minutes of niacin ingestion and avoidance of hot beverages and alcohol which can aggravate flushing by causing peripheral vasodilation may be recommended to reduce flushing.
Endocrine side effects of lovastatin have included hypospermia. Other endocrine side effects of HMG-CoA reductase inhibitors have included gynecomastia and thyroid dysfunction.
Rare incidences of altered thyroid function tests associated with the use of niacin have been reported. Changes appeared to be due to decreased thyroid binding capacity and concentration of thyroid binding globulin.
Gastrointestinal side effects are among the most common complaints in patients on lovastatin. These effects tend to be mild and transient in nature and will often dissipate with continued therapy.
Gastrointestinal side effects associated with the administration of lovastatin have included flatulence (to 6%), abdominal pain (to 6%), diarrhea (to 6%), constipation (to 5%), nausea (to 5%), dyspepsia, and heartburn. Other gastrointestinal side effects of HMG-CoA reductase inhibitors have included pancreatitis, anorexia, and vomiting.
Gastrointestinal side effects associated with the administration of niacin have included exacerbation of peptic ulcer disease, nausea, vomiting, diarrhea, and dyspepsia. Persistent fatigue, nausea or anorexia may be a sign of hepatotoxicity.
Niacin has been shown to increase plasma homocysteine levels. Homocysteine is an independent risk factor for arterial occlusive disease. Clinical implications of these increases and the influence of folic acid supplementation as a means to decrease homocysteine levels remain to be determined.
Cardiovascular side effects associated with the administration of niacin generally have been rare and have included transient tachycardia, hypotension and dizziness. The Coronary Drug Project (1975) reported a significant increase in cardiac arrhythmias associated with the use of niacin; some experts consider preexisting arrhythmias or angina pectoris contraindications to its use.
Niacin have been shown to increase plasma homocysteine levels. Homocysteine is an independent risk factor for arterial occlusive disease. Clinical implications of these increases and the influence of folic acid supplementation as a means to decrease homocysteine levels remain to be determined.
Halkin, et al report a case in which use of both lovastatin and pravastatin on different occasions in the same patient led to reversible impotence. The impotence resolved within 2 weeks after discontinuation of the HMG-CoA reductase inhibitor.
Genitourinary side effects associated with the administration of HMG-CoA reductase inhibitors, including lovastatin, have included erectile dysfunction.
Genitourinary side effects associated with the administration of niacin have included decreased sexual function in up to 3% and 22% of male patients who have taken unmodified and timed release niacin, respectively.
Hematologic side effects associated with the administration of HMG-CoA reductase inhibitors have included hemolytic anemia, thrombocytopenia, and leukopenia. These effects may be manifestations of a hypersensitivity reaction.
Hematologic side effects associated with the administration of niacin have included coagulopathies associated with elevations of liver function enzymes.
Hypersensitivity side effects associated with the administration of lovastatin have been reported rarely with HMG-CoA reductase inhibitors and have included anaphylaxis, angioedema, urticaria, fever (including severe hyperthermia), chills, flushing, malaise, and dyspnea.
Hepatic side effects associated with the administration of lovastatin have included elevations in liver function enzyme tests (to 2%). Other hepatic side effects reported with HMG-CoA reductase inhibitors have included hepatitis, including chronic active hepatitis, cholestatic jaundice, fatty change in the liver, cirrhosis, and fulminant hepatic necrosis.
Hepatic side effects associated with the administration of niacin have included hepatic toxicity.
Persistent elevations in liver function tests to three times normal values have been reported in up to 2% of patients on lovastatin in clinical trials. Overall, 1.5% of patients were withdrawn from study due to elevations in serum transaminases. While most patients remained asymptomatic with these elevations, cases of cholestatic jaundice and hepatitis have been reported.
Liver function tests should be closely monitored. Lovastatin should be discontinued in patients with persistent, significant elevations (three times the upper limit of normal) in liver function parameters.
Hepatotoxicity has been reported in 2% to 3% of patients who have taken larger doses (3 grams or more daily) of niacin or who have used timed release preparations. Hepatotoxicity usually reverses within one week after drug discontinuation, but sometimes can be avoided with dosage reductions or switching to crystalline niacin (if hepatotoxicity developed while using a timed release preparation). Clinical monitoring of patient response and tolerance, including laboratory evaluation of liver function tests is generally recommended.
Dose-related increases in aspartate aminotransferase and alkaline phosphatase have been associated with dosage increases greater than 2.5 grams over 1 month. Computerized tomography has revealed changes consistent with focal fatty liver in some cases. Although these changes usually resolve with dose reduction, continued routine monitoring of liver function tests is recommended. Rare cases of fulminant, even fatal, hepatic failure have been reported.
In one retrospective analysis of 969 predominantly elderly male veterans treated for dyslipoproteinemia with controlled release niacin (average dose 3.1 grams/day), the incidences of possible and probable hepatotoxicity (biochemical criteria) were 2.2% and 4.7%, respectively. Predisposing risk factors included high dose, alcohol use, preexisting liver disease, and concurrent oral sulfonylurea use. The incidence of hepatotoxicity was significantly less among patients who were taking an average daily dose of 2.1 grams.
Immunologic side effects associated with the administration of lovastatin have included a lupus-like syndrome with positive ANA and elevated ESR. Other immunologic side effects of HMG-CoA reductase inhibitors have included polymyalgia rheumatica and vasculitis.
Nicotinic acid competes with uric acid for excretion by the kidneys. Hyperuricemia associated with niacin appears to be more common in men.
Metabolic side effects associated with the administration of lovastatin have included a case report of hyperkalemia in a patient with mild renal insufficiency on concomitant lisinopril. A positive rechallenge implicated lovastatin as a confounding factor in this case.
Metabolic changes associated with niacin have included hyperuricemia and hyperglycemia. Clinical monitoring of patient response and tolerance, including laboratory evaluations of serum uric acid and blood glucose levels, is recommended in patients with a history of gout or diabetes mellitus.
Nervous system side effects associated with the administration of lovastatin have included headache (9%) and dizziness (2%). In addition, one study demonstrated an increase in sleep latency and total wake time in patients treated with lovastatin as compared to patients treated with pravastatin. Other nervous system side effects reported with HMG-CoA reductase inhibitors have included cranial nerve dysfunction, tremor, vertigo, memory loss, paresthesias, peripheral neuropathy, and peripheral nerve palsy.
Nervous system side effects associated with the administration of niacin have included paresthesias, headache, fatigue, and insomnia.
Niacin appears to cause a reversible toxic cystoid maculopathy in approximately 0.7% of patients taking at least 1.5 grams daily. The maculopathy typically has been reversible upon discontinuation of therapy.
Ocular side effects associated with the administration of HMG-CoA reductase inhibitors have included progression of cataracts and ophthalmoplegia. There is no evidence to support adverse effects of lovastatin on the human lens.
Ocular side effects associated with the administration of niacin have included amblyopia, sicca syndromes, blurred vision, eyelid edema, and macular edema. In this study, 7% of 102 patients taking niacin discontinued therapy due to adverse ocular side effects.
Psychiatric side effects associated with the administration of HMG-CoA reductase inhibitors have included anxiety, depression, insomnia, and decreased libido.
Renal side effects associated with the administration of lovastatin have included acute renal failure secondary to rhabdomyolysis.
Other side effects associated with the administration of lovastatin-niacin have included headache, back pain, and migraine. Fatigue, cognitive impairment (e.g., memory loss, forgetfulness, amnesia, memory impairment, confusion), depression, peripheral nerve palsy, dermatomyositis, and progression of cataracts have been reported in postmarketing experience with lovastatin.
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