Indications

Lipitin is indicated as an adjunct to diet to reduce elevated total cholesterol, LDL cholesterol, apolipoprotein B (Apo-B) and triglycerides levels in following diseases when response to diet and other non-pharmacological measures is inadequate.

• To reduce total cholesterol and LDL cholesterol in patients with heterozygous and homozygous familial hypercholesterolemia.
• To reduce elevated cholesterol and triglycerides in patient with mixed dyslipidemia (Fredrickson Type Ia and Ib).
• For the treatment of patients with elevated serum triglyceride levels in hypertriglyceridaemia (Fredrickson Type IV).
• For the treatment of patients with dysbetalipoproteinaemia (Fredrickson Type III).
• To reduce cardiac ischaemic events in patients with asymptomatic or mild to moderate symptomatic coronary artery disease with elevated LDL-cholesterol level.
• To reduce total and LDL-cholesterol concentrations patients with hypercholesterolemia associated with or exacerbated by diabetes mellitus or renal transplantation.

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Pharmacology

Atorvastatin is a selective inhibitor of HMG-CoA reductase. This enzyme is the rate-limiting enzyme responsible for the conversion of HMG-CoA to mevalonate, a precursor of sterols, including cholesterol. Atorvastatin lowers plasma cholesterol and lipoprotein levels by inhibiting HMG-CoA reductase and cholesterol synthesis in the liver and increases the number of hepatic LDL receptors on the cell surface for enhanced uptake and catabolism of LDL.

Absorption: Atorvastatin is rapidly absorbed after oral administration; maximum plasma concentrations occur within 1 to 2 hours. Extent of absorption increases in proportion to Atorvastatin dose. The absolute bioavailability of Atorvastatin (parent drug) is approximately 14% and the systemic availability of HMG-CoA reductase inhibitory activity is approximately 30%.

Distribution: Mean volume of distribution of Atorvastatin is approximately 381 liters. Atorvastatin is 98% bound to plasma proteins. A blood/plasma ratio of approximately 0.25 indicates poor drug penetration into red blood cells. Based on observations in rats, Atorvastatin is likely to be secreted in human milk.

Metabolism: Atorvastatin is extensively metabolized to ortho- and parahydroxylated derivatives and various beta-oxidation products. In vitro inhibition of HMG-CoA reductase by ortho- and parahydroxylated metabolites is equivalent to that of Atorvastatin. Approximately 70% of circulating inhibitory activity for HMG-CoA reductase is attributed to active metabolites. In vitro studies suggest the importance of Atorvastatin metabolism by cytochrome P450 3A4, consistent with increased plasma concentrations of Atorvastatin in humans following coadministration with erythromycin, a known inhibitor of this isozymes. In animals, the ortho-hydroxy metabolite undergoes further glucuronidation.

Excretion: 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 recirculation. Mean plasma elimination half-life of Atorvastatin in humans is approximately 14 hours, but the half-life of inhibitory activity for HMG-CoA reductase is 20 to 30 hours due to the contribution of active metabolites. Less than 2% of a dose of Atorvastatin is recovered in urine following oral administration.

Dosage & Administration

Primary hypercholesterolaemia and combined hyperlipidaemia-

• Adults: Usually 10 mg once daily; if necessary, may be increased at intervals of at least 4 weeks to max. 80 mg once daily.
• Child (10-18 years): Initially 10 mg once daily, increased if necessary at intervals of at least 4 weeks to usual max. 20 mg once daily.

Familial hypercholesterolaemia-

• Adults: 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 hypercholesterolaemia).
• Child (10-18 years): Initially 10 mg once daily, increased if necessary at intervals of at least 4 weeks to usual max. 80 mg once daily.

Prevention of cardiovascular events-

• Adults: Initially 10 mg once daily adjusted according to response.

Another guideline: 

The patient should be placed on a standard cholesterol-lowering diet before receiving Atorvastatin and should continue on this diet during treatment with Atorvastatin. The recommended starting dose of Atorvastatin is 10 or 20 mg once daily. Patients who require a large reduction in LDL-C (more than 45%) may be started at 40 mg once daily. The dosage range of Atorvastatin is 10 to 80 mg once daily. Atorvastatin can be administered as a single dose at any time of the day, with or without food. After initiation of Atorvastatin lipid levels should be analyzed within 2 to 4 weeks and dosage adjusted accordingly.

In hypercholesterolemia in Pediatric Patients (10-17 years of age) the recommended starting dose of Atorvastatin is 10 mg/day; the maximum recommended dose is 20 mg/day (doses greater than 20 mg have not been studied in this patient population). Doses should be individualized according to the recommended goal of therapy. Adjustments should be made at intervals of 4 weeks or more.

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Interaction

The risk of myopathy during treatment with drugs of this class is increased with concurrent administration of cyclosporine, fibric acid derivatives, niacin (nicotinic acid), erythromycin, azole antifungals.

Antacid: When atorvastatin and antacid suspension were coadministered, plasma concentrations of atorvastatin decreased approximately 35%. However, LDL-C reduction was not altered.

Colestipol: Plasma concentrations of atorvastatin decreased approximately 25% when colestipol and atorvastatin were coadministered. However, LDL-C reduction was greater when atorvastatin and colestipol were coadministered than when either drug was given alone.

Digoxin: When multiple doses of atorvastatin and digoxin were coadministered, steady-state plasma digoxin concentrations increased by approximately 20%. Patients taking digoxin should be monitored appropriately.

Erythromycin: In healthy individuals, plasma concentrations of atorvastatin increased approximately 40% with coadministration of atorvastatin and erythromycin, a known inhibitor of cytochrome P450 3A4.

Oral Contraceptives: Coadministration of atorvastatin and an oral contraceptive increased AUC values for norethindrone and ethinyl estradiol by approximately 30% and 20%. These increases should be considered when selecting an oral contraceptive for a woman taking atorvastatin.

Warfarin: Lipitin had no clinically significant effect on prothrombin time when administered to patients receiving chronic warfarin treatment.

Contraindications

Atorvastatin should not be used in patient with hypersensitivity to any component of this medication. Atorvastatin is contraindicated in active liver disease or unexplained persistent elevations of serum transaminases. It is also contraindicated in patient with history of serious adverse reaction to prior administration of HMG-CoA reductase inhibitors.

Side Effects

Lipitin is generally well-tolerated. The most frequent side effects related to Lipitin are constipation, flatulence, dyspepsia, abdominal pain. Other side effects includes infection, headache, back pain, rash, asthenia, arthralgia, myalgia.

Pregnancy & Lactation

Pregnancy: Atorvastatin is contraindicated during pregnancy. Safety in pregnant women has not been established. No controlled clinical trials with atorvastatin have been conducted in pregnant women. Rare reports of congenital anomalies following intrauterine exposure to HMG-CoA reductase inhibitors have been received. Animal studies have shown toxicity to reproduction. Maternal treatment with atorvastatin may reduce the fetal levels of mevalonate which is a precursor of cholesterol biosynthesis. Atorvastatin should not be used in women who are pregnant, trying to become pregnant or suspect they are pregnant. Treatment with atorvastatin should be suspended for the duration of pregnancy or until it has been determined that the woman is not pregnant

Lactation: It is not known whether atorvastatin or its metabolites are excreted in human milk. In rats, plasma concentrations of atorvastatin and its active metabolites are similar to those in milk. Because of the potential for serious adverse reactions, women taking atorvastatin should not breastfeed their infants. Atorvastatin is contraindicated during breastfeeding.

Precautions & Warnings

Liver effects: Liver function tests should be performed before the initiation of treatment and periodically thereafter. Lipitin should be used with caution in patients who consume substantial quantities of alcohol or have a history of liver disease. Lipitin therapy should be discontinued if markedly elevated CPK levels occur or myopathy is diagnosed or suspected.

Use in Special Populations

Geriatric: Plasma concentrations of Lipitin are higher (approximately 40% for Cmax and 30% for AUC) in healthy elderly subjects (age 65 years) than in young adults. Clinical data suggest a greater degree of LDL-lowering at any dose of drug in the elderly patient population compared to younger adults.

Pediatric: Pharmacokinetic data in the pediatric population are not available.

Gender: There is no clinically significant difference in LDL-C reduction with Lipitin between men and women.

Renal Insufficiency: Renal disease has no influence on the plasma concentrations or LDL-C reduction of Lipitin; thus, dose adjustment in patients with renal dysfunction is not necessary.

Hemodialysis: Hemodialysis is not expected to significantly enhance clearance of Lipitin since the drug is extensively bound to plasma proteins.

Hepatic Insufficiency: In patients with chronic alcoholic liver disease, plasma concentrations of Lipitin are markedly increased.

Overdose Effects

Specific treatment is not available for atorvastatin overdose. The patient should be treated symptomatically and supportive measures instituted, as required. Liver function tests should be performed and serum CK levels should be monitored. Due to extensive atorvastatin binding to plasma proteins, hemodialysis is not expected to significantly enhance atorvastatin clearance.

Therapeutic Class

Other Anti-anginal & Anti-ischaemic drugs, Statins

Storage Conditions

Keep in a dry place away from light and heat. Keep out of the reach of children.

Chemical Structure

Common Questions about Lipitin 10 mg Tablet

What is Lipitin 10 mg Tablet?

Lipitin 10 mg Tablet is a selective inhibitor of HMG-CoA reductase. It is used to avoid heart attacks and Primary Hypercholesterolemia. It is also used to treat conditions such as Mixed Dyslipidemia and Hypertriglyceridemia.

How should I take Lipitin 10 mg Tablet?

Lipitin 10 mg Tablet should be taken by mouth once daily, at the same time each day. It can be taken with or without food.

What are the uses of Lipitin 10 mg Tablet?

Lipitin 10 mg Tablet is used for the treatment of diseases like Mixed Dyslipidemia and Hypertriglyceridemia. Besides these, it can also be used to treat conditions like heart attacks and Primary Hypercholesterolemia.

What are the Side Effects of Lipitin 10 mg Tablet?

This is a list of possible side-effects which may occur due to the constituting ingredients of Lipitin 10 mg Tablet. These side-effects have been observed and not necessarily occur. Some of these side-effects may be serious. These include cough, muscle pain, breathing difficulty and running nose.

What are the instructions for storage and disposal Lipitin 10 mg Tablet?

Lipitin 10 mg Tablet should be stored at room temperature, away from heat and direct light. Keep it away from the reach of children and pets.

Is Lipitin 10 mg Tablet used for lowering cholesterol?

Lipitin 10 mg Tablet comes under the class of drugs termed as statins and helps in decreasing the level of lipids or fats. It is used to lower cholesterol and triglycerides present in the blood. However, you must take a cholesterol-lowering diet during the course of treatment.

Will taking Lipitin 10 mg Tablet increase my risk of diabetes?

If you have type 2 diabetes, then consuming Lipitin 10 mg Tablet can slightly affect your health as Lipitin 10 mg Tablet is known to increase the blood sugar levels. In such a case, regular monitoring of blood sugar level during the course of treatment is important.

For how long do I need to take Lipitin 10 mg Tablet? Is it safe for long-term use?

Lipitin 10 mg Tablet should be taken for a duration that a doctor has prescribed it. If you stop taking this medicine without completing the full course, then it can worsen your condition. This medicine is considered safe for long term use if you take it exactly as directed by the doctor.

Does Lipitin 10 mg Tablet cause weight loss?

No studies report that Lipitin 10 mg Tablet can cause weight loss. This is a very unusual side effect. If you encounter weight loss after the course of medication, then doctor consultation is suggested.

Can I stop taking Lipitin 10 mg Tablet?

Do not stop taking Lipitin 10 mg Tablet without informing your doctor. Completing the course of medication is necessary or it can worsen your condition.

Does Lipitin 10 mg Tablet cause memory loss?

Memory loss is a very rare side effect of Lipitin 10 mg Tablet. You must consult a doctor if you experience it.

Does Lipitin 10 mg Tablet make you tired?

Lipitin 10 mg Tablet can make you feel tired. Although the exact reason behind this is still not known.

Can Lipitin 10 mg Tablet be prescribed to children?

Lipitin 10 mg Tablet should be used by adults. Children above 10 years of age can also use it however caution must be exercised. Lipitin 10 mg Tablet should not be given to children who are less than 10 years old.

Is Lipitin 10 mg Tablet a blood thinner?

Lipitin 10 mg Tablet does not cause thinning of the blood. This medication lowers cholesterol and prevents the chances of stroke and heart attack.

Quick Tips

• In general, Lipitin 10 mg Tablet is safe. It may cause diarrhea, gas or an upset stomach. If any of these happen to you, take it with food.
• Inform your doctor if you experience fatigue, muscle weakness or muscle pain.
• Your doctor may check your liver function before starting the treatment and regularly thereafter. Inform your doctor if you notice signs of liver problems such as stomach pains, unusually dark urine or yellowing of skin or eyes.
• Inform your doctor if you have kidney disease, liver disease or diabetes before starting treatment with this medicine. If you are diabetic, monitor your blood sugar level regularly as Lipitin 10 mg Tablet may cause an increase in your blood sugar level.
• Do not take Lipitin 10 mg Tablet if you are pregnant, planning a pregnancy or breastfeeding.

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