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Pravastatin Sodium

Pronunciation

Pronunciation: PRUH-vuh-stuh-tin SO-dee-uhm
Class: HMG-CoA reductase inhibitor

Trade Names

Pravachol
- Tablets 20 mg
- Tablets 40 mg
- Tablets 80 mg

Pravastatin Sodium
- Tablets 10 mg

Apo-Pravastatin (Canada)
CO Pravastatin (Canada)
Gen-Pravastatin (Canada)
Novo-Pravastatin (Canada)
Nu-Pravastatin (Canada)
PMS-Pravastatin (Canada)
ratio-Pravastatin (Canada)
Sandoz Pravastatin (Canada)

Pharmacology

Increases rate at which body removes cholesterol from blood and reduces production of cholesterol in body by inhibiting enzyme that catalyzes early rate-limiting step in cholesterol synthesis.

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Pharmacokinetics

Absorption

Rapidly absorbed (34%). T max is 1 to 1.5 h. Bioavailability is 17%. Food reduces systemic bioavailability.

Distribution

Protein binding is approximately 50%.

Metabolism

Extensive first-pass extraction in the liver. The major degradation product is 3-alpha-hydroxy isomeric metabolite.

Elimination

Urine (20% excreted); feces (70% excreted). The t ½ is 77 h.

Special Populations

Elderly

Mean AUC was approximately 27% greater and mean cumulative urinary excretion was approximately 19% lower in elderly men. Mean AUC was approximately 46% higher and mean cumulative urinary excretion was approximately 18% lower in elderly women.

Indications and Usage

As an adjunct to diet for reduction of elevated total and LDL cholesterol, apolipoprotein B, and triglyceride levels and to increase HDL cholesterol in patients with primary hypercholesterolemia and mixed dyslipidemia (Frederickson types IIa and IIb); as adjunctive therapy to diet for treatment of patients with elevated serum triglyceride levels (Frederickson type IV); treatment of primary dysbetalipoproteinemia (Frederickson type III) who do not respond adequately to diet; in hypercholesterolemic patients without clinically evident coronary heart disease (CHD) to reduce risk of MI or CV mortality with no increase in death from noncardiovascular causes; in patients with clinically evident CHD, to reduce risk of total mortality by reducing coronary death, MI, undergoing myocardial revascularization procedures, stroke, and stroke/transient ischemic attack and slow progression of coronary arteriosclerosis.

Contraindications

Active liver disease or unexplained persistent elevations of LFTs; pregnancy; lactation.

Dosage and Administration

Adults

PO 10 to 40 mg/day.

Children 8 to 13 yr of age

PO 20 mg once daily.

Children 14 to 18 yr of age

PO 40 mg once daily.

General Advice

  • Administer without regard to meals. Administer with food if GI upset occurs.
  • Administer pravastatin at least 1 h before or 4 h after administration of a bile acid sequestrant (eg, cholestyramine).

Storage/Stability

Store tablets at controlled room temperature (59° to 86°F). Protect from moisture and light.

Drug Interactions

Bile acid sequestrants

Large decrease in pravastatin bioavailability.

Cyclosporine, gemfibrozil

Severe myopathy or rhabdomyolysis; decreased urinary excretion and protein binding of pravastatin.

Protease inhibitors (eg, ritonavir)

Pravastatin plasma levels may be reduced, decreasing the efficacy.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Chest pain.

CNS

Headache; dizziness.

Dermatologic

Rash; pruritus.

EENT

Dysfunction of certain cranial nerves (including alteration of taste, impairment of extraocular movement, facial paresis); lens opacities.

GI

Nausea; vomiting; diarrhea; abdominal pain; constipation; flatulence; heartburn; dyspepsia; pancreatitis.

Genitourinary

Urinary abnormality.

Hepatic

Hepatitis; jaundice; fatty changes in liver; cirrhosis; fulminant hepatic necrosis; hepatoma; increased serum transaminases.

Respiratory

Common cold; rhinitis; cough; influenza.

Miscellaneous

Localized pain; myalgia; myopathy; rhabdomyolysis; fatigue; paresthesia; peripheral neuropathy. An apparent hypersensitivity syndrome has been reported rarely that has included 1 or more of the following features: anaphylaxis; angioedema; lupus erythematous-like syndrome; polymyalgia rheumatica; vasculitis; purpura; thrombocytopenia; leukopenia; hemolytic anemia; positive antinuclear antibodies; increase in erythrocyte sedimentation rate; arthritis; arthralgia; urticaria; asthenia; photosensitivity; fever; chills; flushing; malaise; dyspnea; toxic epidermal necrolysis; erythema multiforme, including Stevens-Johnson syndrome.

Precautions

Monitor

Myopathy

Monitor patient for symptoms of myopathy (muscle pain, tenderness, weakness) when medication is started and when dose is increased.

Serum transaminases

Assess serum transaminases before starting therapy, before increasing the dose, and periodically thereafter as clinically indicated.


Pregnancy

Category X .

Lactation

Excreted in breast milk.

Children

Use in children not recommended.

Renal Function

Monitor patients closely.

Hepatic Function

Use with caution in patients who consume substantial quantities of alcohol or those with history of liver disease. Marked, persistent increases in serum transaminases have occurred.

Skeletal muscle effects

Rhabdomyolysis with renal dysfunction secondary to myoglobinuria has occurred. Ensure that therapy is temporarily withheld in patient with an acute, serious condition suggestive of myopathy or predisposing to the development of renal failure secondary to rhabdomyolysis (eg, sepsis, hypotension, major surgery).

Patient Information

  • Advise patient that dose of medication may change, based on results of cholesterol blood tests, in an effort to reach LDL-C goal.
  • Advise patient to take prescribed dose once daily without regard to meals, but to take with food if stomach upset occurs.
  • Advise patient to try to take each dose at about the same time each day.
  • Advise patient that if a dose is missed to take as soon as remembered but to never take more than 1 dose of pravastatin a day.
  • Caution patient not to change the dose or stop taking unless advised by health care provider.
  • Advise patient that pravastatin helps control, but does not cure, cholesterol abnormality and to continue taking as prescribed when LDL-C goal has been reached.
  • Instruct patient to continue taking other cholesterol-lowering medications as prescribed by health care provider.
  • Advise patient who is also taking a bile acid sequestrant (eg, cholestyramine) to take the pravastatin at least 1 h before or 4 h after the sequestrant.
  • Instruct patient to immediately notify health care provider if experiencing any unexplained muscle pain, tenderness, and/or weakness, or if they note any other unusual feelings.
  • Emphasize to patient importance of other modalities on cholesterol control: dietary changes (reduced saturated fat intake, increase soluble fiber intake), weight control, regular exercise, and smoking cessation.
  • Advise women of childbearing potential to use effective contraception during treatment with pravastatin.

Copyright © 2009 Wolters Kluwer Health.

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