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QuickView for Pravastatin (compound)


PubChem
Name: Pravastatin
PubChem Compound ID: 10071008
Description: An antilipemic fungal metabolite isolated from cultures of Nocardia autotrophica. It acts as a competitive inhibitor of HMG CoA reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES).
Molecular formula: C23H36O7
Molecular weight: 424.528 g/mol
DrugBank
Identification
Name: Pravastatin
Name (isomeric): DB00175
Drug Type: small molecule
Description: An antilipemic fungal metabolite isolated from cultures of Nocardia autotrophica. It acts as a competitive inhibitor of HMG CoA reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES).
Synonyms:
Pravastatine [French]; Pravastatina [Spanish]; Pravastatin Sodium; Pravastatinum [Latin]
Brand: Pravaselect, Mevalotin, Oliprevin, Lipostat, Elisor, Pravachol, Selipran, Mevinolin, Vasten, Selectin
Category: HMG-CoA Reductase Inhibitors, Anticholesteremic Agents, Hydroxymethylglutaryl-CoA Reductase Inhibitors
CAS number: 81093-37-0
Pharmacology
Indication: For the treatment of hypercholesterolemia and to reduce the risk of cardiovascular disease.
Pharmacology:
The primary cause of cardiovascular (CV) disease is atherosclerotic plaque formation and sustained elevation of cholesterol in the blood increases the risk of CV disease. Pravastatin lowers hepatic production of cholesterol by competitively inhibiting HMG-CoA reductase, the enzyme that catalyzes the rate-limiting step in the cholesterol biosynthesi...
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Mechanism of Action:
Pravastatin is structurally similar to the HMG, a substituent of the endogenous substrate of HMG-CoA reductase. Unlike its parent compound, mevastatin, and statins such as lovastatin and simvastatin, pravastatin does not need to be activated in vivo. Its hydrolyzed lactone ring mimics the tetrahedral intermediate produced by the reductase al...
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Absorption: Average oral absorption of pravastatin is 34% and absolute bioavailability is 17%.
Protein binding: 50%
Biotransformation: Hepatic, there is a small amount of metabolism by P450 enzymes, but this effect is so minimal that inhibitory pharmacokinetic drug interactions have no real effect on its overall activity and elimination. An in vitro study which found moderate affinity for P450 2C9 (major), 2D6 and 3A4.
Route of elimination: Approximately 20% of a radiolabeled oral dose is excreted in urine and 70% in the feces.
Half Life: 77 hours
Toxicity: Side effects include diarrhea, nausea, constipation, gas abdominal pain, myopathy, myositis, rhabdomyolysis, and hepatotoxicity. LD50=mg/kg (orally in rat)
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Avoid alcohol.
Take without regard to meals.
Avoid drastic changes in dietary habit.
Drug interaction:
ColchicineIncreased risk of rhabdomyolysis with this combination
FenofibrateIncreased risk of myopathy/rhabdomyolysis
CyclosporinePossible myopathy and rhabdomyolysis
ColesevelamBile Acid Sequestrants may decrease the serum concentration of Pravastatin. Administer pravastatin at least 1 hour before or 4 hours after administration of bile-acid resins (eg, cholestyramine, colestipol, colesevelam) to minimize the risk for any significant interaction.
BezafibrateIncreased risk of myopathy/rhabdomyolysis
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