Trade Name: Lovastatin

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Manufacturer: NuCare Pharmaceuticals, Inc.

Presentation: TABLET, HUMAN PRESCRIPTION DRUG

Strength: 10 mg/1

Storage and handling

LOVASTATIN HMG-CoA Reductase Inhibitor [EPC],Hydroxymethylglutaryl-CoA Reductase Inhibitors [MoA]

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  1. These products are NOT FOR SALE in US territories. We offer them for Exports outside of US Territories to Trade Professionals or patients with a valid prescription.
  2. Trademark shown are property of their respective owners and GNH India does not lay any claim on them.
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  • Rx only
  • Lovastatin is a cholesterol lowering agent isolated from a strain of n n n n n n n n n After oral ingestion, lovastatin, which is an inactive lactone, is hydrolyzed to the corresponding u03b2-hydroxyacid form. This is a principal metabolite and an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase. This enzyme catalyzes the conversion of HMG-CoA to mevalonate, which is an early and rate limiting step in the biosynthesis of cholesterol.nn nn n nn n nn
  • Lovastatin is [1 n n n n n n n n n u00a0 -[1u03b1(n n n n n n n n n *), 3u03b1, 7u03b2, 8u03b2(2 n n n n n n n n n u00a0 *,4 n n n n n n n n n u00a0 *),8au03b2]]-1,2,3, 7,8,8a-hexahydro-3,7-dimethyl-8-[2-(tetrahydro-4-hydroxy-6-oxo-2 n n n n n n n n n -pyran-2-yl)ethyl]-1-naphthalenyl 2-methylbutanoate. The empirical formula of lovastatin is C n n n n n n n n n H n n n n n n n n n O n n n n n n n n n and its molecular weight is 404.55. Its structural formula is:nn nn n nn n nn
  • Lovastatin is a white, nonhygroscopic crystalline powder that is insoluble in water and sparingly soluble in ethanol, methanol, and acetonitrile.n
  • Lovastatin tablets are supplied as 10 mg, 20 mg and 40 mg tablets for oral administration. In addition to the active ingredient lovastatin, each tablet contains the following inactive ingredients: lactose monohydrate, magnesium stearate, microcrystalline cellulose, poloxamer, pregelatinized starch, sodium starch glycolate, butylated hydroxyaniso and talc. Butylated hydroxyanisole (BHA) is added as a preservative.n
  • The involvement of low-density lipoprotein cholesterol (LDL-C) in atherogenesis has been well-documented in clinical and pathological studies, as well as in many animal experiments. Epidemiological and clinical studies have established that high LDL-C and low high-density lipoprotein cholesterol (HDL-C) are both associated with coronary heart disease. However, the risk of developing coronary heart disease is continuous and graded over the range of cholesterol levels and many coronary events do occur in patients with total cholesterol (total-C) and LDL-C in the lower end of this range.n
  • Lovastatin has been shown to reduce both normal and elevated LDL-C concentrations. LDL is formed from very low-density lipoprotein (VLDL) and is catabolized predominantly by the high affinity LDL receptor. The mechanism of the LDL-lowering effect of lovastatin may involve both reduction of VLDL-C concentration, and induction of the LDL receptor, leading to reduced production and/or increased catabolism of LDL-C. Apolipoprotein B also falls during treatment with lovastatin. n
  • Lovastatin is a specific inhibitor of HMG-CoA reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate. The conversion of HMG-CoA to mevalonate is an early step in the biosynthetic pathway for cholesterol.n
  • Lovastatin is a lactone, which is readily hydrolyzed n n n n n n n n n to the corresponding u03b2-hydroxyacid, a strong. inhibitor of HMG-CoA reductase. Inhibition of HMG-CoA reductase is the basis for an assay in pharmacokinetic studies of the u03b2-hydroxyacid metabolites (active inhibitors) and, following base hydrolysis, active plus latent inhibitors (total inhibitors) in plasma following administration of lovastatin.nn nn n nn n nn
  • Following an oral dose of n n n n n n n n n C-labeled lovastatin in man, 10% of the dose was excreted in urine and 83% in feces. The latter represents absorbed drug equivalents excreted in bile, as well as any unabsorbed drug. Plasma concentrations of total radioactivity (lovastatin plus n n n n n n n n n C-metabolites) peaked at 2 hours and declined rapidly to about 10% of peak by 24 hours postdose. Absorption of lovastatin, estimated relative to an intravenous reference dose, in each of four animal species tested, averaged about 30% of an oral dose. In animal studies, after oral dosing, lovastatin had high selectivity for the liver, where it achieved substantially higher concentrations than in non-target tissues. Lovastatin undergoes extensive first-pass extraction in the liver, its primary site of action, with subsequent excretion of drug equivalents in the bile. As a consequence of extensive hepatic extraction of lovastatin, the availability of drug to the general circulation is low and variable. In a single dose study in four hypercholesterolemic patients, it was estimated that less than 5% of an oral dose of lovastatin reaches the general circulation as active inhibitors. Following administration of lovastatin tablets the coefficient of variation, based on between-subject variability, was approximately 40% for the area under the curve (AUC) of total inhibitory activity in the general circulation.nn nn n nn n nn
  • Both lovastatin and its u03b2-hydroxyacid metabolite are highly bound (>95%) to human plasma proteins. Animal studies demonstrated that lovastatin crosses the blood-brain and placental barriers.n
  • The major active metabolites present in human plasma are the u03b2-hydroxyacid of lovastatin, its 6'-hydroxy derivative, and two additional metabolites. Peak plasma concentrations of both active and total inhibitors were attained within 2 to 4 hours of dose administration. While the recommended therapeutic dose range is 10 to 80 mg/day, linearity of inhibitory activity in the general circulation was established by a single dose study employing lovastatin tablet dosages from 60 to as high as 120 mg. With a once-a-day dosing regimen, plasma concentrations of total inhibitors over a dosing interval achieved a steady state between the second and third days of therapy and were about 1.5 times those following a single dose. When lovastatin was given under fasting conditions, plasma concentrations of total inhibitors were on average about two-thirds those found when lovastatin was administered immediately after a standard test meal.n
  • In a study of patients with severe renal insufficiency (creatinine clearance 10 to 30 mL/min), the plasma concentrations of total inhibitors after a single dose of lovastatin were approximately two-fold higher than those in healthy volunteers.n
  • In a study including 16 elderly patients between 70 to 78 years of age who received lovastatin 80 mg/day, the mean plasma level of HMG-CoA reductase inhibitory activity was increased approximately 45% compared with 18 patients between 18 to 30 years of age (see n n n n n n n n n , n n n n n n n n n ).nn nn n nn n nn
  • Although the mechanism is not fully understood, cyclosporine has been shown to increase the AUC of HMG-CoA reductase inhibitors. The increase in AUC for lovastatin and lovastatin acid is presumably due, in part, to inhibition of CYP3A4.n
  • The risk of myopathy is increased by high levels of HMG-CoA reductase inhibitory activity in plasma. Strong inhibitors of CYP3A4 can raise the plasma levels of HMG-CoA reductase inhibitory activity and increase the risk of myopathy (see n n n n n n n n n , n n n n n n n n n and n n n n n n n n n , n n n n n n n n n ).nn nn n nn n nn
  • Lovastatin is a substrate for cytochrome P450 isoform 3A4 (CYP3A4) (see n n n n n n n n n , n n n n n n n n n .) Grapefruit juice contains one or more components that inhibit CYP3A4 and can increase the plasma concentrations of drugs metabolized by CYP3A4. In one studyn n n n n n n n n , 10 subjects consumed 200 mL of double-strength grapefruit juice (one can of frozen concentrate diluted with one rather than 3 cans of water) three times daily for 2 days and an additional 200 mL double-strength grapefruit juice together with and 30 and 90 minutes following a single dose of 80 mg lovastatin on the third day. This regimen of grapefruit juice resulted in a mean increase in the serum concentration of lovastatin and its u03b2-hydroxyacid metabolite (as measured by the area under the concentration-time curve) of 15-fold and 5-fold, respectively [as measured using a chemical assay-high performance liquid chromatography.] In a second study, 15 subjects consumed one 8 oz glass of single-strength grapefruit juice (one can of frozen concentrate diluted with 3 cans of water) with breakfast for 3 consecutive days and a single dose of 40 mg lovastatin in the evening of the third day. This regimen of grapefruit juice resulted in a mean increase in the plasma concentration (as measured by the area under the concentration-time curve) of active and total HMG-CoA reductase inhibitory activity [using an enzyme inhibition assay both before (for active inhibitors) and after (for total inhibitors) base hydrolysis] of 1.34-fold and 1.36-fold, respectively, and of lovastatin and its u03b2-hydroxyacid metabolite [measured using a chemical assay-liquid chromatography/tandem mass spectrometry-different from that used in the firstn n n n n n n n n study] of 1.94-fold and 1.57-fold, respectively. The effect of amounts of grapefruit juice between those used in these two studies on lovastatin pharmacokinetics has not been studied.nn nn n nn n nn
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  • * Results based on a chemical assay.n
  • u2020 Lovastatin acid refers to the u03b2-hydroxyacid of lovastatin.n
  • u2021 The mean total AUC of lovastatin without itraconazole phase could not be determined accurately. Results could be representative of strong CYP3A4 inhibitors such as ketoconazole, posaconazole, clarithromycin, telithromycin, HIV protease inhibitors, and nefazodone.n
  • u00a7 Estimated minimum change.n
  • u00b6 The effect of amounts of grapefruit juice between those used in these two studies on lovastatin pharmacokinetics has not been studied.n
  • # Double-strength: one can of frozen concentrate diluted with one can of water.n
  • Grapefruit juice was administered TID for 2 days, and 200 mL together with single dose lovastatin and 30 and 90 minutes following single dose lovastatin on Day 3.n
  • u00de Single-strength: one can of frozen concentrate diluted with 3 cans of water. Grapefruit juice was administered with breakfast for 3 days, and lovastatin was administered in the evening on Day 3.n
  • u00df Cyclosporine-treated patients with psoriasis or post kidney or heart transplant patients with stable graft function, transplanted at least 9 months prior to study.n
  • u00e0 ND = Analyte not determined.n
  • u00e8 Lactone converted to acid by hydrolysis prior to analysis. Figure represents total unmetabolized acid and lactone.n
  • Therapy with lovastatin should be a component of multiple risk factor intervention in those individuals with dyslipidemia at risk for atherosclerotic vascular disease. Lovastatin should be used in addition to a diet restricted in saturated fat and cholesterol as part of a treatment strategy to lower total-C and LDL-C to target levels when the response to diet and other nonpharmacological measures alone has been inadequate to reduce risk.n
  • Hypersensitivity to any component of this medication.n
  • Active liver disease or unexplained persistent elevations of serum transaminases (see n n n n n n n n n ).nn nn n nn n nn
  • Concomitant administration with strong CYP3A4 inhibitors (e.g., itraconazole, ketoconazole, posaconazole, voriconazole, HIV protease inhibitors, boceprevir, telaprevir, erythromycin, clarithromycin, telithromycin ,nefazodone, and cobicistat-containing products) (see n n n n n n n n n , n n n n n n n n n .nn nn n nn n nn
  • No data
  • No data
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  • Reproductive Toxicology
  • After oral administration of lovastatin to mice, the median lethal dose observed was >15 g/m n n n n n n n n n .nn nn n nn n nn
  • Five healthy human volunteers have received up to 200 mg of lovastatin as a single dose without clinically significant adverse experiences. A few cases of accidental overdosage have been reported; no patients had any specific symptoms, and all patients recovered without sequelae. The maximum dose taken was 5 to 6 g.n
  • Until further experience is obtained, no specific treatment of overdosage with lovastatin can be recommended.n
  • The dialyzability of lovastatin and its metabolites in man is not known at present.n
  • The patient should be placed on a standard cholesterol-lowering diet before receiving lovastatin and should continue on this diet during treatment with lovastatin (see NCEP Treatment Guidelines for details on dietary therapy). Lovastatin should be given with meals.n
  • The usual recommended starting dose is 20 mg once a day given with the evening meal. The recommended dosing range is 10 to 80 mg/day in single or two divided doses; the maximum recommended dose is 80 mg/day. Doses should be individualized according to the recommended goal of therapy (see NCEP Guidelines and n n n n n n n n n ). Patients requiring reductions in LDL-C of 20% or more to achieve their goal (see n n n n n n n n n ) should be started on 20 mg/day of lovastatin. A starting dose of 10 mg may be considered for patients requiring smaller reductions. Adjustments should be made at intervals of 4 weeks or more.nn nn n nn n nn
  • Cholesterol levels should be monitored periodically and consideration should be given to reducing the dosage of lovastatin if cholesterol levels fall significantly below the targeted range.n
  • In patients taking danazol, diltiazem, dronedarone or verapamil concomitantly with lovastatin, therapy should begin with 10 mg of lovastatin and should not exceed 20 mgn n n n n n n n n day (see n n n n n n n n n , n n n n n n n n n n , n n n n n n n n n , n n n n n n n n n , n n n n n n n n n ).nn nn n nn n nn
  • Lovastatin Tablets USP (white to off white round, unscored tablets) containing 10mg of lovastatin and engraved with u201cCTIu201d
  • 141 ----Bottle of 30 (NDC 66267-506-30), Bottle of 90 (NDC 66267-506-90)
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  • Pediatrics
  • Store at 20u00ba to 25u00ba C (68u00ba to 77u00ba F). [See USP Controlled Room Temperature.] Lovastatin Tablets must be protected from light and stored in a well-closed, light-resistant container.
  • Manufactured and Distributed By:n n n n n nCarlsbad Technology, Inc.n n n n n n5923 Balfour Courtn n n n n nCarlsbad, CA 92008n n nn
  • Revised December 2014n n n n n nCTI-13 Rev. In n nn
  • No data

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GNH India is WHO GDP and ISO 9001 2015 Certified Pharmaceutical Wholesaler, Supplier, Exporters from India of Lovastatin (Lovastatin) which is also known as Lovastatin and Manufactured by NuCare Pharmaceuticals, Inc.. It is available in strength of 10 mg/1.

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