Lipitor is brand for atorvastatin. Atorvastatin is a statin medication used to prevent cardiovascular disease in those at high risk and treat abnormal lipid levels. For the prevention of cardiovascular disease, statins are a first-line treatment. It is taken by mouth. Atorvastatin belongs to a group of drugs called HMG CoA reductase inhibitors, or "statins." Atorvastatin is used together with diet to lower blood levels of "bad" cholesterol (low-density lipoprotein, or LDL), to increase levels of "good" cholesterol (high-density lipoprotein, or HDL), and to lower triglycerides (a type of fat in the blood). Atorvastatin is used to treat high cholesterol, and to lower the risk of stroke, heart attack, or other heart complications in people with type 2 diabetes, coronary heart disease, or other risk factors. Atorvastatin is used in adults and children who are at least 10 years old.
It is available under a number of trade names Lipitor by Pfizer.
Drug Fact
Class : Statin / Dyslipidaemic Agents
Category : Prescription Only
Uses : prevent cardiovascular disease in those at high risk and treat abnormal lipid levels
Consumed by : adults and children who are at least 10 years old.
Pregnancy category : X
Category X: Studies in animals or human beings have demonstrated foetal abnormalities or there is evidence of foetal risk based on human experience or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated in women who are or may become pregnant.
Dosage form : tablet
Administration
May be taken with or without food. Avoid excessive consumption (>1 L/day) of grapefruit juice.
Dosage/Direction for Use
Adult : PO Heterozygous familial hypercholesterolaemia; Nonfamilial hypercholesterolaemia; Mixed dyslipidaemia Dose is individualised according to baseline LDL-C levels, the goal of therapy, and patient response. Usual initial dose: 10 or 20 mg once daily, may be adjusted according to response at 2-4 weeks interval. Usual range: 10-80 mg once daily. Max: 80 mg/day. Familial homozygous hypercholesterolaemia As an adjunct to other lipid-lowering treatments (e.g. LDL apheresis): 10-80 mg daily. Prophylaxis of cardiovascular events in high-risk patient Primary prevention: Initial: 10 mg daily, may be given at higher doses as necessary to attain LDL-cholesterol levels according to current guidelines.
Dosage Details
Oral
Familial homozygous hypercholesterolaemia
Adult: As an adjunct to other lipid-lowering treatments (e.g. LDL apheresis): 10-80 mg daily.
Oral
Heterozygous familial hypercholesterolaemia, Mixed dyslipidaemia, Nonfamilial hypercholesterolaemia
Adult: Dose is individualised according to baseline LDL-C levels, the goal of therapy, and patient response. Usual initial dose: 10 or 20 mg once daily. May be adjusted according to response at 2-4 weeks interval. Usual range: 10-80 mg once daily. Max: 80 mg daily. Patients who require >45% reduction in LDL-cholesterol: May initiate at 40 mg once daily.
Child: Heterozygous familial hypercholesterolaemia: 10-17 years Initially, 10 mg once daily. May adjust according to response at 4 weeks interval. Usual dose range: 10-20 mg once daily.
Oral
Prophylaxis of cardiovascular events in high-risk patients
Adult: Primary prevention: Initially, 10 mg daily. May be given at higher doses as necessary to attain LDL-cholesterol levels according to current guidelines.
Special Patient Group
Patients taking clarithromycin, itraconazole, fosamprenavir, ritonavir (plus darunavir, fosamprenavir, or saquinavir), elbasvir/grazoprevir: Use lowest effective atorvastatin dose. Max: 20 mg daily.
Patients taking boceprevir, nelfinavir: Use lowest effective atorvastatin dose. Max: 40 mg daily.
Contraindications
Active liver disease, unexplained persistent serum transaminase elevation. Pregnancy and lactation. Concomitant use with ciclosporin, systemic fusidic acid, telaprevir, glecaprevir/pibrentasvir and tipranavir/ritonavir combinations.
Special Precautions
Patients with diabetes mellitus, hypothyroidism, hereditary muscular disorders, recent stroke, transient ischaemic attack, severe acute infection, hypotension, major surgery, predisposing factors for rhabdomyolysis, severe metabolic disorder and uncontrolled seizures. Not indicated for elevated chylomicrons as the primary lipid abnormality. Patients who consume large quantities of alcoholic beverages. Renal impairment. Children. Patients taking concomitant CYP3A4 inhibitors [e.g. clarithromycin, itraconazole, fosamprenavir, ritonavir (plus darunavir, fosamprenavir, or saquinavir), elbasvir/grazoprevir, boceprevir and nelfinavir].
Adverse Reactions
Significant: Myopathy, myalgia, diabetes mellitus, persistent serum transaminase elevations. Rarely, immune-mediated necrotising myopathy (IMNM), interstitial lung disease.
Blood and lymphatic system disorders: Thrombocytopenia.
Ear and labyrinth disorders: Tinnitus, hearing loss.
Eye disorders: Blurred vision.
Gastrointestinal disorders: Diarrhoea, constipation, nausea, dyspepsia, dysgeusia, flatulence.
General disorders and admin site conditions: Malaise, asthenia, fatigue, pyrexia.
Hepatobiliary disorders: Cholestasis.
Investigations: Abnormal LFT, elevated serum creatine kinase, WBC urine positive.
Metabolism and nutrition disorders: Hyperglycaemia.
Musculoskeletal and connective tissue disorders: Muscle spasms, joint swelling, musculoskeletal and extremity pain.
Nervous system disorders: Headache, dizziness, paraesthesia, amnesia.
Psychiatric disorders: Insomnia, nightmares.
Renal and urinary disorders: UTI.
Reproductive system and breast disorders: Rarely, gynaecomastia.
Respiratory, thoracic and mediastinal disorders: Nasopharyngitis, pharyngolaryngeal pain.
Skin and subcutaneous tissue disorders: Alopecia, skin rash, pruritus, urticaria.
Vascular disorders: Epistaxis.
Potentially Fatal: Severe rhabdomyolysis with acute renal failure, hepatitis, hepatic failure. Rarely, Stevens-Johnson syndrome, anaphylaxis, toxic epidermal necrolysis.
Pregnancy Category (US FDA)
PO: X
MonitoringParameters
Monitor lipid panel (e.g. total cholesterol, HDL, LDL, triglycerides) at baseline, 2-12 weeks after initiation, and 12-48 weeks thereafter. Monitor serum creatine kinase (CK) and LFT at baseline and periodically thereafter. Check for signs and symptoms of increased CK suggestive of myopathy (e.g. fever, muscle pain, weakness, stiffness, cramping, generalized fatigue).
Drug Interactions
May increase risk of myopathy and rhabdomyolysis with moderate to potent CYP3A4 inhibitors (e.g. HIV and HCV protease inhibitors, itraconazole, ketoconazole, clarithromycin, eryhthromycin, verapamil, diltiazem), fenofibrate, gemfibrozil, ezetimibe, niacin, colchicine, fixed combination of lopinavir/ritonavir. Concomitant use with CYP3A4 inducers (e.g. rifampicin, efavirenz, phenytoin), Al or Mg antacids, and colestipol may reduce plasma concentrations of atorvastatin. May increase serum levels of digoxin and oral contraceptives (e.g. norethindrone, ethinyl estradiol).
Potentially Fatal: Concomitant use with ciclosporin, telaprevir, glecaprevir/pibrentasvir and tipranavir/ritonavir combinations may potentiate risk of myopathy or rhabdomyolysis. Coadministration with or within 7 days of stopping systemic fusidic acid may increase risk of fatal rhabdomyolysis.
Food Interaction
Grapefruit or grapefruit juice intake may elevate serum concentrations of atorvastatin. Red yeast rice may increase risk for toxic effects. Large consumption of alcoholic beverages may potentiate risk for hepatic impairment. Decreased plasma concentrations with St. John’s wort.
Action
Description: Atorvastatin selectively and competitively inhibits HMG-CoA reductase, the enzyme that catalyses the conversion of HMG-CoA to produce mevalonate. The reduction of mevalonate production results to a compensatory increase in the expression of LDL receptors and stimulation of LDL catabolism, consequently lowering LDL-cholesterol levels.
Onset: Initial effect: 3-5 days.
Pharmacokinetics:
Absorption: Rapidly absorbed from the gastrointestinal tract. Bioavailability: Approx 12-14%. Time to peak plasma concentration: 1-2 hours.
Distribution: Volume of distribution: Approx 381 L. Plasma protein binding: ≥98%.
Metabolism: Metabolised in the liver by CYP3A4 isoenzyme to active ortho- and parahydroxylated derivatives, and inactive β-oxidation metabolites. Undergoes extensive first-pass metabolism in the gastrointestinal mucosa and liver.
Excretion: Mainly via bile; via urine (<2% as unchanged drug). Elimination half-life: Approx 14 hours.
Chemical Structure
Storage
Store between 20-25°C.
ATC Classification
C10AA05 - atorvastatin ; Belongs to the class of HMG CoA reductase inhibitors. Used in the treatment of hyperlipidemia.
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