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Rendapid

Rendapid - General Information

A derivative of lovastatin and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (hydroxymethylglutaryl COA reductases), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL receptors, it increases breakdown of LDL cholesterol. [PubChem]

Pharmacology of Rendapid

Rendapid, the methylated form of lovastatin, is an oral antilipemic agent which inhibits HMG-CoA reductase. simvastatin is used in the treatment of primary hypercholesterolemia and is effective in reducing total and LDL-cholesterol as well as plasma triglycerides and apolipoprotein B.

Rendapid for patients

Patients should be advised about substances they should not take concomitantly with simvastatin and be advised to report promptly unexplained muscle pain. tenderness, or weakness. Patients should also be advised to inform other physicians prescribing a new medication that they are taking ZOCOR.

Rendapid Interactions

Simvastatin is metabolized by CYP3A4 but has no CYP3A4 inhibitory activity; therefore it is not expected to affect the plasma concentrations of other drugs metabolized by CYP3A4. Potent inhibitors of CYP3A4 (below) increase the risk of myopathy by reducing the elimination of simvastatin.

HIV protease inhibitors

Large quantities of grapefruit juice (>1 quart daily)

Interactions with lipid-lowering drugs that can cause myopathy when given alone

The risk of myopathy is increased by gemfibrozil and to a lesser extent by other fibrates and niacin (nicotinic acid) (?1 g/day).

Other drug interactions

Danazol: The risk of myopathy/rhabdomyolysis is increased by concomitant administration of danazol particularly with higher doses of simvastatin

Amiodarone or Verapamil: The risk of myopathy/rhabdomyolysis is increased by concomitant administration of amiodarone or verapamil with higher doses of simvastatin

Propranolol: In healthy male volunteers there was a significant decrease in mean Cmax, but no change in AUC, for simvastatin total and active inhibitors with concomitant administration of single doses of ZOCOR and propranolol. The clinical relevance of this finding is unclear. The pharmacokinetics of the enantiomers of propranolol were not affected.

Digoxin: Concomitant administration of a single dose of digoxin in healthy male volunteers receiving simvastatin resulted in a slight elevation (less than 0.3 ng/mL) in digoxin concentrations in plasma (as measured by a radioimmunoassay) compared to concomitant administration of placebo and digoxin. Patients taking digoxin should be monitored appropriately when simvastatin is initiated.

Warfarin: In two clinical studies, one in normal volunteers and the other in hypercholesterolemic patients, simvastatin 20-40 mg/day modestly potentiated the effect of coumarin anticoagulants: the prothrombin time, reported as International Normalized Ratio (INR), increased from a baseline of 1.7 to 1.8 and from 2.6 to 3.4 in the volunteer and patient studies, respectively. With other reductase inhibitors, clinically evident bleeding and/or increased prothrombin time has been reported in a few patients taking coumarin anticoagulants concomitantly. In such patients, prothrombin time should be determined before starting simvastatin and frequently enough during early therapy to ensure that no significant alteration of prothrombin time occurs. Once a stable prothrombin time has been documented, prothrombin times can be monitored at the intervals usually recommended for patients on coumarin anticoagulants. If the dose of simvastatin is changed or discontinued, the same procedure should be repeated. Simvastatin therapy has not been associated with bleeding or with changes in prothrombin time in patients not taking anticoagulants.

Rendapid Contraindications

Hypersensitivity to any component of this medication.

Active liver disease or unexplained persistent elevations of serum transaminases

Pregnancy and lactation. Atherosclerosis is a chronic process and the discontinuation of lipid-lowering drugs during pregnancy should have little impact on the outcome of long-term therapy of primary hypercholesterolemia. Moreover, cholesterol and other products of the cholesterol biosynthesis pathway are essential components for fetal development, including synthesis of steroids and cell membranes. Because of the ability of inhibitors of HMG-CoA reductase such as ZOCOR to decrease the synthesis of cholesterol and possibly other products of the cholesterol biosynthesis pathway, ZOCOR is contraindicated during pregnancy and in nursing mothers. ZOCOR should be administered to women of childbearing age only when such patients are highly unlikely to conceive. If the patient becomes pregnant while taking this drug, ZOCOR should be discontinued immediately and the patient should be apprised of the potential hazard to the fetus.

Additional information about Rendapid

Rendapid Indication: For the treatment of hypercholesterolemia. Mechanism Of Action: The 6-membered lactone ring of simvastatin is hydrolyzed in vivo to generate mevinolinic acid, an active metabolite structurally similar to HMG-CoA (hydroxymethylglutaryl CoA). Once hydrolyzed, simvastatin competes with HMG-CoA for HMG-CoA reductase, a hepatic microsomal enzyme. Interference with the activity of this enzyme reduces the quantity of mevalonic acid, a precursor of cholesterol. Drug Interactions: Not Available Food Interactions: Avoid drastic changes in dietary habit. Avoid alcohol. Avoid taking with grapefruit juice. Generic Name: Simvastatin Synonyms: Not Available Drug Category: Anticholesteremic Agents; Antilipemic Agents; Hydroxymethylglutaryl-CoA Reductase Inhibitors Drug Type: Small Molecule; Approved Other Brand Names containing Simvastatin: Cholestat; Coledis; Colemin; Corolin; Denan; Labistatin; Lipex; Lodales; Medipo; Nivelipol; Pantok; Rendapid; Simovil; Simvastatin [Usan-Ban-Inn]; Simvastatina [Spanish]; Simvastatine [French]; Simvastatinum [Latin]; Sinvacor; Sivastin; Synvinolin; Vasotenal; Vytorin; Zocor; Zocord; Absorption: Absorption of simvastatin, estimated relative to an intravenous reference dose, in each of two animal species tested, averaged about 85% of an oral dose. In animal studies, after oral dosing, simvastatin achieved substantially higher concentrations in the liver than in non-target tissues. Toxicity (Overdose): Not Available Protein Binding: Both simvastatin and its b-hydroxyacid metabolite are highly bound (approximately 95%) to human plasma proteins. Biotransformation: Hepatic, simvastatin is a substrate for CYP3A4. Half Life: 3 hours Dosage Forms of Rendapid: Tablet Oral Chemical IUPAC Name: [(1S,3R,7S,8S,8aR)-8-[2-[(2R,4R)-4-hydroxy-6-oxooxan-2-yl]ethyl]-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl] 2,2-dimethylbutanoate Chemical Formula: C25H38O5 Simvastatin on Wikipedia: http://en. wikipedia. org/wiki/Simvastatin Organisms Affected: Humans and other mammals