Drug reference

Atorvastatin

Statin · Antilipidemic

Also known as Atorvastatin calcium, Lipitor, Storvas, Atorva

START

10–20 mg PO once daily

TYPICAL MAX

80 mg/day

STOP IF

Active liver disease · pregnancy

WATCH

Myalgia/CK · ALT/AST

CDSCO approvedSchedule HJan AushadhiNPPA price-controlledATC C10AA05

Dose laddermg/d

Renal dose adjustmenteGFR mL/min/1.73m²

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours

ONSET: 1h · plasma absorption
PEAK: 1.5h · Cmax (parent)
t½: 14h · parent t½ (metabolites 20-30h)
DURATION: 1d · once-daily lipid effect

EXCRETION

Biliary/fecal · CYP3A4 substrate

route + CYP

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

Category X — contraindicated, embryonic harm

FDA category + note

Top interactionssee all 12 →

AtazanavirSevereTextbook-citedKDT 7e · p948
ClarithromycinSevereTextbook-citedKDT 7e · p948
DarunavirSevereTextbook-citedKDT 7e · p948
ErythromycinSevereTextbook-citedKDT 7e · p948

Available in India

1,560 branded formulations and 359 fixed-dose combinations. Look up specific brands in the Drugs workspace.

Jan Aushadhi — generic available at GoI pharmacies

Mechanism

Atorvastatin selectively inhibits 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, an enzyme critical for cholesterol synthesis in the liver. This inhibition reduces intracellular cholesterol levels, which in turn upregulates LDL receptors on hepatocyte surfaces. The increased expression of LDL receptors leads to enhanced uptake and catabolism of circulating LDL-cholesterol, effectively lowering plasma cholesterol and triglyceride levels.

Indications

Primary hypercholesterolemia (Type IIa)Mixed dyslipidemia (Type IIb)Homozygous familial hypercholesterolemiaPrimary prevention of cardiovascular disease in adults with multiple risk factorsSecondary prevention of cardiovascular events in patients with established coronary heart diseaseHeterozygous familial hypercholesterolemia in pediatric patients (10-17 years old)HypercholesterolemiaReduction of LDL-C levelsTreat dyslipidemias, especially elevated LDL-CChildren aged 11 years and older with heterozygous FHPrimary hyperlipidaemias with raised LDL and total CH levels, with or without raised TG levels (Type IIa, IIb, V)Secondary hypercholesterolaemia (e.g., in diabetes, nephrotic syndrome)Greater reduction in TGs if same was raised at baselineIntensive lipid-lowering therapy in NSTE-ACS, prior to PCI and continued thereafter, to reduce both early and late recurrent ischemic events

Dosing

Adult: Initial dose 10-20 mg orally once daily. Dosing range is 10-80 mg once daily. Adjust dose at 2-4 week intervals based on lipid levels and therapeutic response. Doses should be taken at the same time each day, with or without food.
Pediatric: For Heterozygous Familial Hypercholesterolemia (10-17 years old): Initial dose 10 mg orally once daily. Max dose 20 mg once daily. Adjust dose based on response and tolerability.
Renal adjustment: No dose adjustment is necessary for patients with renal impairment. Use with caution in severe renal impairment (eGFR <30 mL/min/1.73m2). However, close monitoring is advised for adverse effects like myopathy/rhabdomyolysis in this group, particularly with concomitant medications increasing atorvastatin exposure (e.g., cyclosporine, strong CYP3A4 inhibitors).…
Max dose: 80 mg/day

Pharmacokinetics

Onset

Within 2 weeks for significant lipid-lowering effects

Peak effect

1-2 hours (plasma concentration of parent drug); 2-4 weeks (maximum lipid-lowering effect)

Duration

Long-acting due to active metabolites

Half-life

~14 hours (parent drug), 20-30 hours (active metabolites)

Bioavailability

~12%

Protein binding

>98%

Metabolism

Extensive hepatic metabolism primarily via CYP3A4 to active ortho- and parahydroxylated metabolites, as well as via glucuronidation. Substrate of OATP1B1, OATP1B3, and P-glycoprotein.

Excretion

Primarily biliary/fecal excretion (70% in bile and feces)

Contraindications

Active liver disease or unexplained persistent elevations of serum transaminases
Pregnancy
Breastfeeding
Hypersensitivity to atorvastatin or any component of the formulation
Concomitant use with glecaprevir/pibrentasvir

Side effects

Common

MyalgiaArthralgiaDiarrheaNauseaDyspepsiaHeadacheNasopharyngitisInsomniaUrinary tract infectionMuscle sorenessWeaknessGastrointestinal complaintsRashes (uncommon)Sleep disturbances (uncommon)Muscle aches (10%)

Serious

Rhabdomyolysis with acute renal failure (rare, but life-threatening)
Hepatotoxicity (elevated liver enzymes, rare hepatic failure)
Immune-mediated necrotizing myopathy (IMNM)
New-onset diabetes mellitus (dose-dependent)
Interstitial lung disease (rare)
Angioedema
Pancreatitis
Myopathy
Rhabdomyolysis
Hepatotoxicity
Rise in serum transaminase
Liver damage (rare)
Myopathy (rare, < 1 per 1000)
Rhabdomyolysis (fatalities on record)

Pregnancy & lactation

Pregnancy

Category X — contraindicated, embryonic harm

Lactation

Contraindicated. Atorvastatin is excreted into breast milk and has the potential for serious adverse reactions in nursing infants.

Drug interactions

Atazanavir

Severe

Textbook-cited

Increased risk of rhabdomyolysis and myopathy.

Avoid concurrent use; if needed, use lowest statin dose

Source: KDT 7e · p948

Clarithromycin

Severe

Textbook-cited

Increased risk of rhabdomyolysis and myopathy.

Avoid concurrent use; if needed, use lowest statin dose

Source: KDT 7e · p948

Darunavir

Severe

Textbook-cited

Increased risk of rhabdomyolysis and myopathy.

Avoid concurrent use; if needed, use lowest statin dose

Source: KDT 7e · p948

Erythromycin

Severe

Textbook-cited

Increased risk of rhabdomyolysis and myopathy.

Avoid concurrent use; if needed, use lowest statin dose

Source: KDT 7e · p948

Fluconazole

Severe

Textbook-cited

Increased risk of rhabdomyolysis and myopathy.

Avoid concurrent use; if needed, use lowest statin dose

Source: KDT 7e · p948

Gemfibrozil

Severe

Textbook-cited

Increased risk of myopathy and rhabdomyolysis.

Use with caution; monitor for muscle symptoms and CK levels

Source: KDT 7e · p949

Itraconazole

Severe

Textbook-cited

Increased risk of rhabdomyolysis and myopathy.

Avoid concurrent use; if needed, use lowest statin dose

Source: KDT 7e · p948

Ketoconazole

Severe

Textbook-cited

Increased risk of rhabdomyolysis and myopathy.

Avoid concurrent use; if needed, use lowest statin dose

Source: KDT 7e · p948

Lopinavir

Severe

Textbook-cited

Increased risk of rhabdomyolysis and myopathy

Avoid concurrent use; if needed, use lowest statin dose

Source: KDT 7e · p948

Nicotinic Acid

Severe

Textbook-cited

Increased risk of myopathy and rhabdomyolysis

Use with caution; monitor for muscle symptoms and CK levels

Source: KDT 7e · p949

Ritonavir

Severe

Textbook-cited

Increased risk of rhabdomyolysis and myopathy.

Avoid concurrent use; if needed, use lowest statin dose

Source: KDT 7e · p948

Azole Antifungals

Severe

Textbook

Increased plasma concentrations of statins and their active metabolites, leading to an increased risk of myopathy and rhabdomyolysis.

Consider using pravastatin, fluvastatin, or rosuvastatin, as they are not extensively metabolized by CYP3A4. Carefully weigh the benefits against the risk of myopathy.

Source: G&G 14e · p736