section name header

Pronunciation

atorvastatin: a-TORE-va-stat-in

fluvastatin: FLOO-va-sta-tin

lovastatin: LOE-va-sta-tin

pitavastatin: pi-TAVa-sta-tin

pravastatin: PRA-va-sta-tin

rosuvastatin: roe-SOO-va-sta-tin

simvastatin: SIM-va-sta-tin

Classifications

Therapeutic Classification: lipid-lowering agents

Pharmacologic Classification: hmg coa reductase inhibitors

Indications

REMS


AtorvastatinAtorvastatin and pravastatinFluvastatinFluvastatin and lovastatinLovastatinPravastatinSimvastatinRosuvastatinRosuvastatinRosuvastatin

Action

  • Inhibit an enzyme, 3-hydroxy-3-methylglutaryl-­coenzyme A (HMG-CoA) reductase, which is responsible for catalyzing an early step in the synthesis of cholesterol.
Therapeutic effects:
  • Lower total and LDL-C and triglycerides. Slightly increase HDL-C.
  • Slow the progression of coronary atherosclerosis with resultant decrease in CHD-related events.

Pharmacokinetics

Absorption: Atorvastatin: Rapidly absorbed but undergoes extensive GI and hepatic metabolism, resulting in 14% bioavailability; Fluvastatin: 98% absorbed after oral administration, but undergoes extensive first-pass metabolism resulting in 24% bioavailability; Lovastatin, pravastatin: Poorly and variably absorbed after oral administration; Pitavastatin: well absorbed (51%) after oral administration; Rosuvastatin: 20% absorbed following oral administration; Simvastatin: 85% absorbed but rapidly metabolized.

Distribution: Atorvastatin: probably enters breast milk. Fluvastatin: enters breast milk. Lovastatin: crosses the blood-brain barrier and placenta. Pravastatin: small amounts enter breast milk. Pitavastatin, rosuvastatin, and simvastatin: unknown.

Protein Binding: Atorvastatin, fluvastatin, pitavastatin, and simvastatin: >98%.

Metabolism/Excretion: All agents are extensively metabolized by the liver; amount excreted unchanged in urine: Atorvastatin:<2%, Lovastatin: 10%, Fluvastatin: 5%, Pitavastatin: 15%, Pravastatin: 20%, and Simvastatin: 13%.

Half-Life: Atorvastatin: 14 hr; Fluvastatin: 1.2 hr; Lovastatin: 3 hr; Pitavastatin: 12 hr; Pravastatin: 1.3–2.7 hr; Rosuvastatin: 19 hr; Simvastatin: unknown.

Time/Action Profile

( cholesterol-lowering effect)

ROUTEONSETPEAKDURATION*
Atorvastatinunknownunknown20–30 hr
Fluvastatin1–2 wk4–6 wkunknown
Lovastatin2 wk4–6 wk6 wk
Pitavastatinwithin 4 wk4 wkunknown
Pravastatinseveral days2–4 wkunknown
Rosuvastatinunknown2–4 wkunknown
Simvastatinseveral days2–4 wkunknown

* After discontinuation.

Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

CV: chest pain, peripheral edema

Derm: rash, pruritus

EENT: rhinitis, blurred vision (lovastatin)

Endo: hyperglycemia

GI: abdominal cramps, constipation, diarrhea, flatus, heartburn, liver enzymes, altered taste, drug-induced hepatitis, dyspepsia, nausea, pancreatitis

GU: erectile dysfunction

MS: arthralgia, arthritis, immune-mediated necrotizing myopathy (IMNM), myalgia, myopathy ( with simvastatin 80 mg/day dose), RHABDOMYOLYSIS

Neuro: amnesia, confusion, dizziness, headache, insomnia, memory loss, weakness

Resp: bronchitis

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANGIOEDEMA AND URTICARIA)

Interactions

Atorvastatin, lovastatin, simvastatin, and rosuvastatin are metabolized by the CYP3A4 metabolic pathway. Fluvastatin is metabolized by CYP2C9. Pravastatin is not metabolized by the CYP P450 system.

Route/Dosage

Atorvastatin

Fluvastatin

Lovastatin

Renal Impairment

Pitavastatin

Renal Impairment

Pravastatin

Renal Impairment

Rosuvastatin

Renal Impairment

Simvastatin

Renal Impairment

Availability

Atorvastatin

(Generic available)

Fluvastatin

(Generic available)

Lovastatin

(Generic available)

Pitavastatin

(Generic available)

Pravastatin

(Generic available)

Rosuvastatin

(Generic available)

Simvastatin

(Generic available)

Assessment

Lab Test Considerations:

Implementation

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

atorvastatin: Atorvaliq, Lipitor,

fluvastatin: Lescol, , Lescol XL,

lovastatin: Mevacor,

pitavastatin: Livalo, Zypitamag,

pravastatin: Pravachol,

rosuvastatin: Crestor, Ezallor Sprinkle,

simvastatin: FloLipid, Zocor