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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