Description

Simple

A medication used to lower the amount of cholesterol in the blood and decrease the chance of having a heart attack or stroke.

Clinical

An HMG-CoA reductase inhibitor used to lower lipid levels and reduce the risk of cardiovascular disease including myocardial infarction and stroke.

Overview

Atorvastatin, also known as the brand name product Lipitor, is a lipid-lowering drug belonging to the statin class of medications. By inhibiting the endogenous production of cholesterol within the liver, statins lower abnormal cholesterol and lipid levels and ultimately reduce the risk of cardiovascular disease. More specifically, statin medications competitively inhibit the enzyme hydroxymethylglutaryl-coenzyme A (HMG-CoA) Reductase,[8] which catalyzes the conversion of HMG-CoA to mevalonic acid. This is the third step in a sequence of metabolic reactions involved in the production of several compounds involved in lipid metabolism and transport including cholesterol, low-density lipoprotein (LDL) (sometimes referred to as "bad cholesterol"), and very low-density lipoprotein (VLDL). Prescribing of statin medications is considered standard practice following any cardiovascular events and for people with a moderate to high risk of development of CVD, such as those with Type 2 Diabetes. The clear evidence of the benefit of statin use coupled with very minimal side effects or long term effects has resulted in this class becoming one of the most widely prescribed medications in North America.[Read more

Pharmacology

Indication

Atorvastatin is approved for the treatment of several types of dyslipidemias including:

- Primary hyperlipidemia and mixed dyslipidemia in adults.
- Hypertriglyceridemia.
- Primary dysbetalipoproteinemia.
- Homozygous familial hypercholesterolemia.
- Heterozygous familial hypercholesterolemia... Read more

Pharmacodynamic

Atorvastatin is an oral antilipemic agent which reversibly inhibits HMG-CoA reductase. It is used to lower total cholesterol, low density lipoprotein-cholesterol (LDL-C), apolipoprotein B (apoB), non-high density lipoprotein-cholesterol (non-HDL-C), and trigleride (TG) plasma concentrations while in... Read more

Mechanism of action

Atorvastatin is a statin medication and a competitive inhibitor of the enzyme HMG-CoA (3-hydroxy-3-methylglutaryl coenzyme A) reductase, which catalyzes the conversion of HMG-CoA to mevalonate, an early rate-limiting step in cholesterol biosynthesis.[ Read more

Absorption

Atorvastatin presents a dose-dependent and non-linear pharmacokinetic profile.[4] It is very rapidly absorbed after oral admin... Read more

Protein binding

Atorvastatin is highly bound to plasma proteins and over 98% of the administered dose is found in a bound form.[38,39 Read more

Volume of distribution

The reported volume of distribution of atorvastatin is of 380 L.[38,39]

Clearance

The registered total plasma clearance of atorvastatin is of 625 ml/min.[5]

Half life

The half-life of atorvastatin is 14 hours while the half-life of its metabolites can reach up to 30 hours.[38,39]

Route of elimination

Atorvastatin and its metabolites are mainly eliminated in the bile without enterohepatic recirculation. The renal elimination of atorvastatin is very minimal and represents less than 1% of the eliminated dose.[38, Read more

Toxicity

The reported LD50 of oral atorvastatin in mice is higher than 5000 mg/kg.[MSDS] In cases of overdose with atorvastatin, there is reported symptoms of complicated breathing, jaundice, liver damage, dark urine, muscle pain, and seizures.[ Read more

Adverse Effects

Contraindications

  • Route:
    • Oral
  • Dose Form:
    • Tablet
  • Hypersensitivity:
    • true
  • Regions: US
  • Regions: US
  • Patient Conditions:
      • Name: Nursing mothers
      • Drugbank Id: DBCOND0107390
  • Regions: US
  • Patient Conditions:
      • Name: Pregnancy
      • Drugbank Id: DBCOND0018394
  • Regions: US
  • Patient Conditions:
      • Name: Active liver disease
      • Drugbank Id: DBCOND0107507
      • Modification Of:
        • Condition Status: active
        • Base:
          • Name: Liver Disease
          • Drugbank Id: DBCOND0028338

Food Interactions

  • Avoid alcohol.
  • Avoid drastic changes in dietary habit.
  • Avoid taking grapefruit or grapefruit juice throughout treatment. Grapefruit can significantly increase serum levels of this product.
  • Food may decrease maximum plasma levels and area under the curve, but this is clinically inconsequential according to the manufacturer.
  • Take with low fat meal.

Interactions

Type in a drug name to check for interaction with Atorvastatin
Type a drug name in the box above to get started
  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The metabolism of (R)-warfarin can be decreased when combined with Atorvastatin.
(S)-Warfarin
The metabolism of (S)-Warfarin can be decreased when combined with Atorvastatin.
4-Methoxyamphetamine
The metabolism of 4-Methoxyamphetamine can be decreased when combined with Atorvastatin.
5-methoxy-N,N-dimethyltryptamine
The metabolism of 5-methoxy-N,N-dimethyltryptamine can be decreased when combined with Atorvastatin.
6-Deoxyerythronolide B
The risk or severity of adverse effects can be increased when 6-Deoxyerythronolide B is combined with Atorvastatin.
7-ethyl-10-hydroxycamptothecin
The metabolism of Atorvastatin can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
Abafungin
The risk or severity of myopathy can be increased when Abafungin is combined with Atorvastatin.
Abatacept
The metabolism of Atorvastatin can be increased when combined with Abatacept.
Abemaciclib
The serum concentration of Abemaciclib can be increased when it is combined with Atorvastatin.
Abiraterone
The metabolism of Atorvastatin can be decreased when combined with Abiraterone.
Acalabrutinib
The metabolism of Atorvastatin can be decreased when combined with Acalabrutinib.
Acebutolol
The serum concentration of Acebutolol can be increased when it is combined with Atorvastatin.
Acenocoumarol
The metabolism of Acenocoumarol can be decreased when combined with Atorvastatin.
Acetaminophen
The metabolism of Atorvastatin can be decreased when combined with Acetaminophen.
Acetazolamide
The metabolism of Atorvastatin can be decreased when combined with Acetazolamide.
Acetohexamide
The metabolism of Acetohexamide can be decreased when combined with Atorvastatin.
Acetylcysteine
The excretion of Atorvastatin can be decreased when combined with Acetylcysteine.
Acetyldigoxin
The serum concentration of Acetyldigoxin can be increased when it is combined with Atorvastatin.
Acetylsalicylic acid
The serum concentration of Acetylsalicylic acid can be increased when it is combined with Atorvastatin.
Acipimox
Acipimox may increase the myopathic rhabdomyolysis activities of Atorvastatin.
39 References
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