Lochol

Each tablet contains Simvastatin 10 mg, 20 mg, 40 mg, 80 mg.

LOCHOL composed of simvastatin, an inactive lactone, which is hydrolyzed to the corresponding β-hydroxy acid form which inhibits 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase. Inhibition of HMG-CoA reductase prevents conversion of HMG-CoA to mevalonate, an early step in cholesterol biosynthesis.
Simvastatin is effective in reducing total plasma cholesterol (total-C), low-density lipoprotein cholesterol (LDL-C), very low-density lipoprotein cholesterol (VLDL-C), plasma triglyceride (TG) and increases high-density lipoprotein cholesterol (HDL-C) in heterozygous familial/non-familial hypercholesterolemia and in mixed hyperlipidemia when elevated cholesterol was cause for concern and diet alone has been insufficient.

Hyperlipidemia: Adjunct to diet to reduce elevated total and LDL cholesterol level in primary hypercholesterolemia and mixed dyslipidemia (Type IIa and IIb) when the response to diet and other nonpharmacological measures alone has been inadequate.
Coronary heart disease: To reduce the risk of total mortality by reducing coronary death; to reduce the risk of non-fatal myocardial infarction; reduce the risk of undergoing myocardial revascularization procedures and reduce the risk of stroke and transient ischemic attacks (TIA).

Before the treatment, the patient should be place on a standard cholesterol-lowing diet before receiving simvastatin and should continue on this diet during treatment with simvastatin.
Hyperlipidemia: The usual starting dose is 10-20 mg/day given as a single dose in the evening. The recommended dosing range is 5-80 mg/day as a single dose in the evening. Adjustments of dosage should be made at intervals of not less than 4 weeks.
Coronary heart disease: The usual starting dose is 10-20 mg/day given as a single dose in the evening. The maximum dose is 80 mg/day as a single dose in the evening. Adjustments of dosage should be made at intervals of not less than 4 weeks.

A few case of overdose with simvastatin have occurred; no patients had any specific symptoms. All recovered without sequelae. The maximum dose taken was 450 mg.
When patients take overdose of simvastatin, treatment symptomatically and institute supportive measures as required. The dialyzability of this agent and its metabolites is not known.

Hypersensitivity to any component of these products and HMG-CoA reductase inhibitors.
Active liver disease or unexplained persistent elevation of serum transaminase.
Pregnancy, lactation.

Muscle effects: Elevation of creatine kinase (CK) levels (from skeletal muscle) have been seen commonly. Therapy with HMG-CoA reductase inhibitors has been associated with myopathy. Myopathy should be considered in any patient with diffuse myalgias, muscle tenderness and/or marked elevations of CK levels (10 times the upper limit of normal). Therapy should be discontinued if markedly elevated CK level occur or if myopathy is diagnosed or suspected. The risk of myopathy with HMG-CoA reductase inhibitors is known to be increased by concomitant immunosuppressive therapy including cyclosporin, and by concomitant therapy with a fibric acid derivative or lipid-lowering doses of niacin (nicotinic acid).
Monitoring carefully patients for any signs and symptoms of muscle pain, tenderness, or weakness, particularly during the initial months of therapy and during any periods of upward dosage titration of drug. Simvastatin therapy should be discontinued if these signs are suspected. When patients were promptly discontinued from treatment, muscle symptoms and CK increases resolved.
Hepatic effects: It is recommended that liver function tests should be performed before treatment begins, at 6 and 12 weeks after initiation of therapy and after dose elevation and periodically thereafter (about 6 month intervals) in all patients especially in patients who develop elevated progression (three times the upper limit of normal) and persistence, the drug should be discontinued. Active liver disease or unexplained transaminase elevation are contraindication to the use of simvastatin.
Diet: Before instituting therapy, attempt to control hypercholesterolemia with diet, exercise and weight reduction on obese patients.
Homozygous familial hypercholesterolemia: Simvastatin is less effective in patients with rare homozygous familial hypercholesterolemia, possibly because of a decrease in functional LDL receptors.
Sleep disturbance: Simvastatin may interfere with sleep causing insomnia.
Photosensitivity: Photosensitivity may occur; therefore, caution patients to take protective measures against exposure to ultraviolet or sunlight (ie. sunscreens, protective clothing).
Use in Pregnancy & Lactation: See Use in Pregnancy & Lactation section for further information.
Use in Children: Safety and effectiveness in children have not been established simvastatin is not recommended for use in children.

Use in Pregnancy: Simvastatin are not recommended for use during pregnancy or in a woman who plans to become pregnant in the near future. If pregnancy occurs during therapy, it is recommended that the drug should be discontinued for the duration of the pregnancy.
Use in Lactation: It is not known whether simvastatin is excreted in human breast milk. However, use of simvastatin while breast-feeding is not recommended, because of the potential for serious adverse effects in nursing infants.

Simvastatin is generally well-tolerated. The most adverse effects have been mild and transient in nature such as nausea, vomiting, diarrhea, skin rash, dyspepsia, pruritus, alopecia, dizziness, muscle cramps, myalgia, pancreatitis, peripheral neuropathy and anemia.
Other adverse effects rarely occur such as rhabdomyolysis, hepatitis and jaundice. An apparent hypersensitivity syndrome has been reported rarely which has included some of the following features: angioedema, lupus-like syndrome, polymyalgia rheumatica, vasculitis, thrombocytopenia, eosinophilia, Erythrocyte sedimentation rate (ESR) increased, arthritis, arthralgia, urticaria, photosensitivity, fever, flushing, dyspnea and malaise.
Laboratory test finding: Marked increases of serum transaminase, alkaline phosphatase, gamma-glutamyl transpeptidase and creatine kinase (CK).

Simvastatin may interact with: CYP3A4: Simvastatin has no CYP3A4 inhibitory activity; therefore it is no expected to affect plasma levels of other drugs metabolized by CYP3A4. However, simvastatin itself is a substrate for CYP3A4. Potent inhibitors of CYP3A4 may increase the risk of myopathy by increasing the plasma level of HMG-CoA reductase inhibitory activity during simvastatin therapy. These include cyclosporin, itraconazole, ketoconazole, erythromycin, clarithromycin, HIV protease inhibitors and nefazodone.
Gemfibrozil and other fibrates, niacin (lipid-lowering dose ≥1 gram/day: These drugs increase the risk of myopathy when given concomitantly with simvastatin, probably because they can produce myopathy when given alone.
Propranolol: Decrease in antihyperlipidemic activity may occur.
Warfarin: Anticoagulant effect of warfarin may be increased; therefore, prothrombin time should be determined before starting simvastatin and frequently enough during early therapy to ensure that no significant alteration of prothrombin time occurs.

Store below 30°C.

Dyslipidaemic Agents

C10AA01 - simvastatin ; Belongs to the class of HMG CoA reductase inhibitors. Used in the treatment of hyperlipidemia.

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