Altoprev (lovastatin)

In patients receiving danazol, diltiazem, dronedarone, or verapamil concomitantly with lovastatin, dosage of lovastatin should be initiated at 10 mg daily and should not exceed 20 mg daily. In patients receiving amiodarone concomitantly with lovastatin, dosage of lovastatin should not exceed 40 mg daily.

No dosing information is available for this tab.

No dosing information is available for this tab.

No dosing information is available for this tab.

Lovastatin is metabolized by cytochrome P-450 isoenzyme (CYP) 3A4 but has no CYP3A4 inhibitory activity. Lovastatin is a substrate of P-glycoprotein (P-gp) and organic anion transporter protein (OATP) 1B1.

Drug interaction studies have not been performed with lovastatin extended-release and the types, frequencies, and magnitude of drug interactions that may be encountered may differ from the drug interactions encountered with lovastatin immediate-release. The manufacturer of lovastatin extended-release recommends caution when extrapolating lovastatin immediate-release drug interactions and that the monitoring of the pharmacologic effects of the drug and/or other concomitantly administered drugs be undertaken where appropriate.

There are no contraindication interactions for this drug.

There are no severe interactions for this drug.

There are no moderate interactions for this drug.

*Hypersensitivity to lovastatin or any component of the formulation.

*Active liver disease or unexplained, persistent elevations of serum transaminases.

*Concomitant therapy with strong inhibitors of cytochrome P-450 (CYP) isoenzyme 3A4 (e.g., clarithromycin, cobicistat-containing preparations, erythromycin, HIV protease inhibitors, itraconazole, ketoconazole, nefazodone, posaconazole,voriconazole).

*Nursing mothers. The manufacturer states that lovastatin is contraindicated in women who are pregnant or may become pregnant; however, because statins may prevent serious or potentially fatal cardiovascular events in certain high-risk patients who are pregnant, FDA has requested that the contraindication in pregnant women be removed from the prescribing information for all statins.

There are no contraindication contraindications for this drug.

There are no severe contraindications for this drug.

There are no moderate contraindications for this drug.

Adverse effects reported in at least 2% of patients receiving immediate-release lovastatin include GI disturbances (e.g., flatulence, diarrhea, abdominal pain, constipation, nausea), headache, and myalgia.

Adverse effects reported in at least 5% of patients receiving extended-release lovastatin include infection, headache, and accidental injury.

There are no severe adverse reactions for this drug.

There are no less severe adverse reactions for this drug.

No enhanced messaging available.

Safety and effectiveness of lovastatin immediate-release tablets for the treatment of patients 10 to 17 years of age with heterozygous familial hypercholesterolemia (HeFH) have been established in controlled clinical trials of 48 weeks' duration in adolescent boys and controlled clinical trials of 24 weeks' duration in girls who were at least 1 year post-menarche. The adverse effect profile of lovastatin immediate-release tablets (10-40 mg daily for at least 24 weeks) generally was similar to that of placebo; dosages exceeding 40 mg daily have not been evaluated in this population. There were no detectable adverse effects on growth or sexual maturation in adolescent boys or on duration of menstrual cycle in girls. If therapy with lovastatin is considered, the manufacturer states that adolescent girls should be advised to use effective and appropriate contraceptive methods during therapy to reduce the likelihood of unintended pregnancy. Safety and efficacy of lovastatin have not been evaluated in prepubertal children or in children younger than 10 years of age; however, experts state that statins may be considered as young as 8 years of age+ in the presence of concerning family history, extremely elevated LDL-cholesterol level, or elevated lipoprotein (a), in the context of informed shared decision-making and counseling with the patient and family.

Safety and efficacy of lovastatin as extended-release tablets have not been established in children or adolescents younger than 20 years of age. Therefore, the manufacturer states that this preparation should not be used in this population.

All statins were previously contraindicated in pregnant women because the fetal risk with these drugs was thought to outweigh any possible benefit. This determination was based on several factors including safety signals from animal data. Lovastatin has produced skeletal malformations in offspring of pregnant mice and rats receiving dosages of 80 mg/kg daily during gestation (7 times the human dose based on body surface area and 5 times the human exposure based on AUC, respectively). In addition, congenital anomalies including severe CNS defects and unilateral limb deficiencies were reported in a case series of pregnant women who were exposed to a lipophilic statin during the first trimester. Because statins decrease synthesis of cholesterol and possibly other products of the cholesterol biosynthetic pathway, there is also a concern that these drugs can potentially cause fetal harm. More recent data from case series and observational cohort studies have not shown evidence of an increased risk of major birth defects with statin use during pregnancy, and this was observed after controlling for potential confounders such as maternal age, diabetes mellitus, hypertension, obesity, and alcohol and tobacco use. The overall evidence from animal studies suggests limited potential for statins to cause malformations or other adverse fetal effects. While an increased risk of miscarriage has been reported in pregnant women exposed to statins, it is not clear whether this effect is related to the drugs or to other confounding factors. FDA conducted a comprehensive review of all available clinical and nonclinical data related to statin use in pregnant women and concluded that the totality of evidence suggests limited potential for statins to cause malformations and other adverse embryofetal effects. Because statins may prevent serious or potentially fatal cardiovascular events in certain high-risk patients who are pregnant, FDA has requested that the contraindication in pregnant women be removed from the prescribing information for all statins. While FDA still advises that most pregnant patients discontinue statins because of the possibility of fetal harm, there may be some patients (e.g., those with homozygous familial hypercholesterolemia or established cardiovascular disease) in whom continued therapy may be beneficial; therefore, decisions should be individualized based on the patient's risks versus benefits. Patients who become pregnant or suspect that they are pregnant while receiving a statin should notify their clinician who can advise them on the appropriate course of action.

It is not known whether lovastatin is distributed into human milk; however, other statins are distributed into human milk. Because of the potential for serious adverse reactions from lovastatin in nursing infants, the drug is contraindicated in nursing women; women who require lovastatin therapy should not breast-feed their infants. Many patients can stop statin therapy temporarily until breast-feeding is complete; patients who require ongoing statin treatment should not breast-feed and should use alternatives such as infant formula.

In geriatric patients (>=65 years of age), the usual initial dosage of lovastatin extended-release is 20 mg once daily at bedtime. Higher dosages should be used only after careful consideration of the potential risks and benefits.

Results of a pharmacokinetic study in a limited number of patients receiving lovastatin immediate-release tablets (80 mg daily) indicate that mean plasma levels of HMG-CoA reductase inhibitory activity are approximately 45% higher in geriatric patients (70-78 years of age) than in younger adults (18-30 years of age). However, data from clinical studies and other reported clinical experience employing various preparations of lovastatin suggest that safety and efficacy of the drug in geriatric patients appear to be similar to those in younger adults. Although dosage adjustment based on age-related pharmacokinetic differences does not appear to be necessary for geriatric patients, greater sensitivity in some older patients cannot be ruled out. Because advanced age (65 years of age or older) is a predisposing factor for myopathy, including rhabdomyolysis, the manufacturer states that lovastatin should be prescribed with caution in this population. Lower initial dosages of extended-release lovastatin are recommended in geriatric patients.

Because patients older than 75 years of age may have a higher risk of adverse effects and lower adherence to therapy, the expected benefits versus adverse effects should be considered before initiating statin therapy in this population.