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TCL-RTCL-R

TCL-R

Atorvastatin

HMG-CoA reductase catalyzes the conversion of HMG-CoA to mevalonate which is the major rate limiting step in the cholesterol synthesis pathway. The main mechanism of reduction of low density lipoprotein (LDL) cholesterol is that, following inhibition of HMG-CoA reductase activity, the LDL receptor density on the liver cell is increased and this leads to an increased removal of LDL cholesterol from the plasma and increased catabolism of LDL cholesterol.
TCL-R is rapidly absorbed after oral administration, maximum plasma levels occur within 1 to 2 hours. The absolute bioavailability of Atorvastatin (parent drug) is approximately 12% and the systemic availability of HMG-CoA reductase inhibitory activity is approximately 30%. Although food reduces the rate and extent of drug absorption by approximately 25% & 9% respectively. Atorvastatin is approximately 98% bound to plasma proteins. Atorvastatin and its metabolites are eliminated primarily in bile following hepatic and/or extra hepatic metabolism, however the drug does not appear to undergo enterohepatic circulation. The mean plasma elimination half-life of Atorvastatin in human is approximately 14 hours, but the half-life of inhibitory activity of HMG-CoA reductase is 20 to 30 hours due to the contribution of active metabolites.

Product Details

Presentation

TCL-R 10 Tablet: Each film coated tablet contains Atorvastatin Calcium Trihydrate equivalent to Atorvastatin 10 mg.
TCL-R 20 Tablet: Each film coated tablet contains Atorvastatin Calcium Trihydrate equivalent to Atorvastatin 20 mg.

Pharmacology

HMG-CoA reductase catalyzes the conversion of HMG-CoA to mevalonate which is the major rate limiting step in the cholesterol synthesis pathway. The main mechanism of reduction of low density lipoprotein (LDL) cholesterol is that, following inhibition of HMG-CoA reductase activity, the LDL receptor density on the liver cell is increased and this leads to an increased removal of LDL cholesterol from the plasma and increased catabolism of LDL cholesterol.
TCL-R is rapidly absorbed after oral administration, maximum plasma levels occur within 1 to 2 hours. The absolute bioavailability of Atorvastatin (parent drug) is approximately 12% and the systemic availability of HMG-CoA reductase inhibitory activity is approximately 30%. Although food reduces the rate and extent of drug absorption by approximately 25% & 9% respectively. Atorvastatin is approximately 98% bound to plasma proteins. Atorvastatin and its metabolites are eliminated primarily in bile following hepatic and/or extra hepatic metabolism, however the drug does not appear to undergo enterohepatic circulation. The mean plasma elimination half-life of Atorvastatin in human is approximately 14 hours, but the half-life of inhibitory activity of HMG-CoA reductase is 20 to 30 hours due to the contribution of active metabolites.

Indication

1. In patients unresponsive to diet and other non-pharmacological measures, TCL-R is indicated for the reduction of elevated total cholesterol, LDL-cholesterol, apolipoprotein B and triglycerides.
2. In patients with primary hypercholesterolemia, heterozygous familial hypercholesterolaemia or mixed dyslipidaemia.
3. In patients with elevated serum triglyceride levels.
4. In patients with primary dysbetalipoproteinaemia.
5. In patients with homozygous familial hypercholesterolaemia as an adjunct to other lipid lowering treatments.

Dosage & Administration

Patients should be placed on a standard cholesterol-lowering diet before receiving Atorvastatin & should continue on this diet during treatment with TCL-R.
Primary hypercholesterolemia and combined hyperlipidemia: Usually 10 mg once daily. If necessary may be increased at intervals of at least 4 weeks to max 80 mg once daily; child 10-17 years usually 10 mg once daily.
Familial hypercholesterolemia: Initially 10 mg daily, increased at intervals of at least 4 weeks to 40 mg once daily; if necessary, further increased to max. 80 mg once daily or 40 mg once daily combined with anion-exchange resin in heterozygous familial hypercholesterolemia; child 10-17 years up to 20 mg once daily.
Prevention of cardiovascular events in type 2 diabetes: 10 mg once daily.

Contraindications

Hypersensitivity to any of the ingredients of this medication, active liver disease or unexplained persistent elevations of serum transaminases, pregnancy and breast feeding and in woman of childbearing potential not using contraceptives.

Warning & Precautions

TCL-R should be used with caution in patients with a history of liver disease or alcoholism. Patients with signs and symptoms of myopathy should have their creatine phosphokinase (CPK) levels monitored. TCL-R should be discontinued if CPK levels are markedly or persistently raised or myopathy is diagnosed or suspected.

Side effects

Atorvastatin is generally well tolerated. Side effects reported commonly include constipation, flatulence, dyspepsia, abdominal pain, headache, nausea, myalgia, diarrhoea, asthenia and insomnia. Others include muscle cramps, paresthesia, pancreatitis, hepatitis, cholestatic, anorexia, vomiting, pruritus, rash.

Drug interaction

Erythromycin, oral contraceptives, colestipol, digoxin, cyclosporine, fibric acid derivatives, azole, antifungals, niacin, antacid, warfarin, cimetidine.

Use in special groups

Use in Prgenancy & lactation: Atorvastatins are not recommended for use during pregnancy. An interval of 1 month should be allowed from stopping an Atorvastatin treatment to conception in the event of planning a pregnancy. Use of HMG-CoA reductase inhibitors during breast-feeding is not recommended because of the potential for serious adverse effects in nursing infants.
Pediatric: Safety and efficacy of TCL-R have not been established in children.
Geriatric : Efficacy and safety in older patients have been established & the recommended doses are similar to that of adult patients.

Packing

TCL-R 10 Tablet: Each box contains 30's tablets in blister pack.
TCL-R 20 Tablet: Each box contains 10's tablets in blister pack.

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