Atorvastatin |
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Atorvastatin (Lipitor, Pfizer), is a member of the drug class known as statins, used for lowering blood cholesterol. It also stabilizes plaque and prevents strokes through anti-inflammatory and other mechanisms.
Atorvastatin inhibits HMG-CoA reductase, the rate-determining enzyme located in hepatic tissue that produces mevalonate, a small molecule used in the synthesis of cholesterol and other mevalonate derivatives. This lowers the amount of cholesterol produced which in turn lowers the total amount of LDL cholesterol. Atorvastatin was first synthesized in 1985 by Bruce Roth while working at Parke-Davis Warner-Lambert Company (now Pfizer). With 2008 sales of US$12.4 billion, Lipitor is likely the top-selling drug in the world. US patent protection is scheduled to expire in June 2011. However, Pfizer made an agreement with Ranbaxy Laboratories to delay the generic launch in the US until November 2011.
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| Dosage |
Packing |
Price |
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| 10 mg |
90 tab (manuf. Hexal AG Germany) |
USD 98.00 |
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Atorvastatin generic (generic - what is it?)
| Dosage |
Packing |
Price |
Add to basket |
| 10 mg |
100 tab ($0.64 per tab, manuf. in India) |
USD 58.00 |
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| 20 mg |
100 tab ($0.98 per tab, manuf. in India) |
USD 89.00 |
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Atorvastatin: Medications and Prescriptions
Generic name: atorvastatin
Product Brand Name: Lipitor
Product Manufacturer: Hexal AG Germany
Atorvastatin description
As with other statins, atorvastatin is a competitive inhibitor of HMG-CoA reductase. Unlike most others, however, it is a completely synthetic compound. HMG-CoA reductase catalyzes the reduction of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) to mevalonate, which is the rate-limiting step in hepatic cholesterol biosynthesis. Inhibition of the enzyme decreases de novo cholesterol synthesis, increasing expression of low-density lipoprotein receptors (LDL receptors) on hepatocytes. This increases LDL uptake by the hepatocytes, decreasing the amount of LDL-cholesterol in the blood. Like other statins, atorvastatin also reduces blood levels of triglycerides and slightly increases levels of HDL-cholesterol.
In clinical trials, the combination of ezetimibe (Zetia) and Lipitor lowered cholesterol more effectively than Vytorin (ezetimibe + simvastatin).
Indications
Hypercholesterolemia (heterozygous familial and nonfamilial) and mixed dyslipidemia (Fredrickson types IIa and IIb) to reduce total cholesterol, LDL-C, apo-B, Triglycerides levels, and CRP as well as increase HDL levels.
Heterozygous familial hypercholesterolemia in pediatric patients
Homozygous familial hypercholesterolemia
Hypertriglyceridemia (Fredrickson Type IV)
Primary dysbetalipoproteinemia (Fredrickson Type III)
It has also been used in the treatment of combined hyperlipidemia.
Prophylaxis for myocardial infarction, stroke, unstable angina, and revascularization.*prophylaxis in patients with multiple risk factors without evident CHD.
Myocardial infarction and stroke prophylaxis in patients with type II diabetes.
Concomitant Therapy Considerations
Atorvastatin may be used in combination with bile acid resins. It is not recommended to combine statin treatment with fibrates because of the increased risk of myopathy related adverse reactions[6].Drug dose must be adjusted according to age of patient, and must be lowered in Hepatic insufficiency
Contraindications:
Active liver disease: cholestasis, hepatic encephalopathy, hepatitis, and jaundice.
Unexplained elevations in AST or ALT levels
Pregnancy.
Breast-feeding.
Precaution must be taken when treating with atorvastatin, because rarely it may lead to rhabdomyolysis, it may be very serious leading to acute renal failure due to myoglobinuria. If rhabdomyolysis is suspected or diagnosed, atorvastatin therapy should be discontinued immediately. Also Atorvastatin should be discontinued if a patient has markedly elevated CPK levels or if a myopathy is suspected or diagnosed. The likelihood of developing a myopathy is increased by the co-administration of cyclosporine, fibric acid derivatives, erythromycin, niacin, and azole antifungals
Atorvastatin is absolutely contraindicated in pregnancy, it is likely to cause harm to fetal development because of the importance of cholesterol and various products in the cholesterol biosynthesis pathway for fetal development, including steroid synthesis and cell membrane production. It is not recommended that nursing mothers take atorvastatin due to the possibility of adverse reactions in nursing infants, since experiments with rats indicate that atorvastatin is likely to be secreted into human milk
How supplied
Atorvastatin calcium tablets are currently marketed by Pfizer under the trade name Lipitor, in tablets (10, 20, 40 or 80 mg) for oral administration. Tablets are white, elliptical, and film coated. Pfizer also packages the drug in combination with other drugs, such as is the case with its Caduet. In some countries, atorvastatin calcium is made in tablet form by generic drug makers under various brand names including Atoris, Atorlip, Lipvas, Sortis, Torvast, Torvacard, Totalip, and Tulip.
Side effects:
....As stated earlier, myopathy with elevation of creatinine kinase (CK) and rhabdomyolysis are the most serious, although rare <1%.
....Headache is the most common side effect, occurring in more than 10% of patients.
Side effects that occur in 1-10% of patients taking atorvastatin include:
Weakness
Insomnia and dizziness.
Chest pain and peripheral edema.
Rash
Abdominal pain, constipation, diarrhea, dyspepsia, flatulence, nausea.
Urinary tract infection.
Arthralgia, myalgia, back pain, arthritis.
Sinusitis, pharyngitis, bronchitis, rhinitis.
Infection, flu-like syndrome, allergic reaction.
Elevation of alanine transaminase (ALT) and aspartate transaminase AST) has been described in a few cases.
Other very rare side effects occurring in less than 1% of patients are: alopecia, anaphylaxis, angina, angioneurotic edema, arrhythmia, bullous rashes, cholestatic jaundice, deafness, dyspnea, erythema multiforme, esophagitis, facial paralysis, glaucoma, gout, hepatitis, hyperkinesia, impotence, migraine, myasthenia, myositis, nephritis, pancreatitis, paresthesia, peripheral neuropathy, petechiae, photosensitivity, postural hypotension, pruritus, rectal hemorrhage, rhabdomyolysis, somnolence, Stevens-Johnson syndrome, syncope, tendinous contracture, thrombocytopenia, tinnitus, torticollis, toxic epidermal necrolysis, urticaria, vaginal hemorrhage, and vomiting.
Atorvastatin notes:
Atorvastatin (brand name Lipitor) is an oral drug used for lowering cholesterol levels in the blood. It also stabilizes plaque and prevents strokes through anti – inflammatory mechanisms. It belongs to the class of drugs referred to as statins. All statins, including Atorvastatin, prevent the production of cholesterol in the liver by blocking HMG-CoA reductase, an enzyme that makes cholesterol.
FDA approved Atorvastatin, also reduces the concentration of triglycerides in the blood and raises the concentrations of HDL cholesterol, which is known to be the “good” blood cholesterol. Atorvastatin has rapid oral absorption with an approximate time to maximum plasma concentration of 1–2 hours.
Precaution must be taken when treating with atorvastatin, because it may lead to rhabdomyolysis, which may be very serious leading to acute renal failure due to myoglobinuria. If rhabdomyolysis is suspected or diagnosed, atorvastatin therapy should be discontinued immediately. In addition, Atorvastatin should be discontinued if a patient has markedly elevated CPK levels or if a myopathy is suspected or diagnosed.
The elderly patients show a greater pharmacodynamic response to atorvastatin at any dose, therefore, this population may have lower effective doses. It has also been used in the treatment of combined hyperlipidemia and is absolutely contraindicated in the case of pregnancy due to the possibility of adverse reactions.
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Drug category:Antilipemic agents
 Atorvastatin
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