- March 15, 2022
- Newsletter
- 617-430-5616
Menu
Menu
Menu
Menu
Menu
Menu
Brand Name :
Altoprev, Mevacor
Synonyms :
lovastatin
Class :
HMG-CoA Reductase Inhibitors, Lipid-Lowering Agents, Statins
Dosage Forms & Strengths
Tablet
10mg
20mg
40mg
Tablets, extended-release
20mg
40mg
60mg
Altoprev (Extended release):
10 to 60 mg orally every night at bedtime
Mevacor (Immediate release):
Initial dose: 20 mg orally once daily with an evening meal
may divide the daily dose twice a day;
alter dose at 4-week intervals if necessary; maximum daily dose: 80 mg
Dose Adjustments
Dosing Considerations
Danazol, diltiazem, or verapamil coadministration: Do not take over 20 mg of lovastatin daily.
Amiodarone coadministration: Do not take more than 40 mg of lovastatin daily.
Avoid drinking significant amounts of grapefruit juice (more than 1 quart daily).
Management of overdose
Overdosing on the medicine may cause adverse effects such as peripheral neuropathy, diarrhea, higher LFTs, myopathy, rhabdomyolysis, increased K+, and eye lens opacities.
Supportive care is provided.
Dosing Modifications
Renal Impairment
Renal impairment (severe; CrCl>30 mL/min): Doses more than 20 mg/day should be carefully assessed and, if required, administered cautiously.
Dosage Forms & Strengths
Tablet
10mg
20mg
40mg
Tablets, extended-release
20mg
40mg
60mg
heterozygous familial hypercholesterolemia
10 to 17 years: 20 to 40 mg orally every day
Do not exceed 40mg/day
If the patient needs a lesser LDL-C decrease, start with 10 mg/day
Refer adult dosing
may enhance the serum concentration when combined
may increase the myopathic effect of HMG-CoA Reductase Inhibitors
may increase the adverse effect of HMG-CoA Reductase Inhibitors
may enhance the serum concentration when combined
may increase the adverse effect of HMG-CoA Reductase Inhibitors
may enhance the serum concentration when combined
may enhance the serum concentration when combined
may enhance the serum concentration of HMG-CoA Reductase Inhibitors
may enhance the serum concentration when combined
may enhance the serum concentration when combined
may enhance the serum concentration when combined
may enhance the serum concentration of OATP1B1/1B3 Substrates
may enhance the serum concentration of HMG-CoA Reductase Inhibitors
may enhance the serum concentration when combined
may enhance serum concentrations of the active metabolites
may enhance serum concentrations of the active metabolites
may enhance serum concentrations of the active metabolites
may enhance serum concentrations of the active metabolites
may enhance serum concentrations of the active metabolites
may enhance the serum concentration when combined
may enhance the serum concentration when combined
may increase the adverse effect of HMG-CoA Reductase Inhibitors
may increase the myopathic effect of HMG-CoA Reductase Inhibitors
may enhance the serum concentration when combined
may enhance the serum concentration of OATP1B1/1B3 Substrates
may enhance the serum concentration when combined
It may enhance the effect when combined with miconazole vaginal by affecting CYP3A4 metabolism
lovastatin increases the effect of lapatinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
It may enhance the toxicity when combined with mipomersen
may increase the myopathic effect of HMG-CoA Reductase Inhibitors
may increase the myopathic effect of HMG-CoA Reductase Inhibitors
may increase the myopathic effect of HMG-CoA Reductase Inhibitors
may enhance the serum concentration when combined
may enhance the serum concentration when combined
may enhance the serum concentration when combined
may enhance the serum concentration when combined
may enhance the serum concentration when combined
may enhance the serum concentration of HMG-CoA Reductase Inhibitors
may enhance the serum concentration of OATP1B1/1B3 Substrates
may increase the myopathic effect of HMG-CoA Reductase Inhibitors
may enhance the serum concentration when combined
may increase the anticoagulant effect of HMG-CoA Reductase Inhibitors
may increase the anticoagulant effect of HMG-CoA Reductase Inhibitors
may increase the anticoagulant effect of HMG-CoA Reductase Inhibitors
may increase the anticoagulant effect of HMG-CoA Reductase Inhibitors
may increase the anticoagulant effect of HMG-CoA Reductase Inhibitors
It may enhance toxicity when combined with cholic acid by diminishing the elimination
the effect of lovastatin is decreased by lorlatinib, by altering intestinal or hepatic CYP3A4 enzyme metabolism
may enhance the serum concentration of elbasvir/grazoprevir
may enhance the serum concentration when combined
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may increase the serum concentration
may decrease the serum concentration
may decrease the serum concentration
may decrease the serum concentration
may decrease the serum concentration
may decrease the serum concentration
they decrease the absorption of fibric acid derivatives
bezafibrate increases the effect of myopathy on HMG-CoA reductase inhibitors
Actions and Spectrum:
Frequency defined
>10%
CPK elevation (11%)
1-10%
Abdominal pain (2-3%)
Diarrhea (2-3%)
Nausea (2-3%)
Weakness (1-2%)
Rash (0.8-1%)
Dizziness (0.5-1%)
Constipation (2-3%)
Myalgia (2-3%)
Dyspepsia (1-2%)
Blurred vision (0.8-1%)
Muscle cramps (0.6-1%)
Flatulence (4-5%)
<1%
Increased LFTs
Myopathy
Dermatomyositis
Hepatotoxicity
Rhabdomyolysis
Post-marketing reports
Interstitial lung disease
Contraindications/caution:
Contraindications:
Caution:
Pregnancy consideration: It is contraindicated in pregnancy and should not be used.
Lactation: Excretion of the drug in human breast milk is unknown
Pregnancy category:
Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.
<b>Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: There is no data available for the drug under this category
Pharmacology:
lovastatin is a medication that belongs to a class of drugs known as HMG-CoA reductase inhibitors, or statins. It works by inhibiting the enzyme HMG-CoA reductase, which is involved in the production of cholesterol in the liver.
By inhibiting this enzyme, lovastatin reduces the cholesterol produced in the liver, decreasing blood cholesterol levels. lovastatin also increases the number of low-density lipoprotein (LDL) receptors on the surface of liver cells, which enhances the removal of LDL cholesterol from the bloodstream.
Pharmacodynamics:
The pharmacodynamics of lovastatin involves its effects on lipid metabolism and cholesterol synthesis. lovastatin is a competitive inhibitor of HMG-CoA reductase. This enzyme plays a vital role in cholesterol biosynthesis in the liver.
By inhibiting HMG-CoA reductase, lovastatin decreases the cholesterol produced in the liver. This leads to an upregulation of LDL receptors on the surface of liver cells, which enhances the clearance of LDL cholesterol from the bloodstream. Additionally, lovastatin has been shown to increase high-density lipoprotein (HDL) cholesterol levels, often called “good” cholesterol.
Pharmacokinetics:
Absorption
lovastatin is well absorbed after oral administration and undergoes extensive first-pass metabolism in the liver, resulting in low systemic bioavailability. The absorption of lovastatin is increased when it is taken with food.
Distribution
lovastatin is highly protein-bound (95%) in the plasma, primarily to albumin. It has a volume of distribution of approximately 481 liters, indicating that it is widely distributed throughout the body.
Metabolism
lovastatin is extensively metabolized in the liver by the cytochrome P450 (CYP) enzyme system, primarily by the CYP3A4 isoenzyme, to its active metabolite, lovastatin acid. This active metabolite is responsible for the cholesterol-lowering effects of the drug.
Elimination and Excretion
lovastatin and its metabolites are excreted primarily in the feces, with only a tiny amount in the urine. The elimination half-life of lovastatin is approximately 1-2 hours, with its active metabolite, lovastatin acid, having a half-life of approximately 3 hours.
Administration:
lovastatin is a medication used to lower cholesterol levels in the blood. It belongs to a class of drugs called statins. The usual starting dose for lovastatin is 20 mg, taken once daily with the evening meal. However, the dose may be adjusted based on individual patient response and tolerability. The maximum recommended dose is 80 mg per day.
lovastatin should be taken regularly, at the same time each day, to achieve the best results. It can be taken with or without food, but taking it with a meal is recommended to help improve its absorption and reduce the risk of stomach upset.
It is essential to follow the dosing instructions provided by your healthcare provider or pharmacist and stay within the recommended dose, as this can increase the risk of side effects. Additionally, it is essential to continue taking lovastatin as directed, even if you feel well. High cholesterol levels often do not cause symptoms but can lead to serious health problems.
Patient information leaflet
Generic Name: lovastatin
Why do we use lovastatin?
ADVERTISEMENT
