section name header

Pronunciation ⬇

loe-SAR-tan

Classifications ⬆ ⬇

Therapeutic Classification: antihypertensives

Pharmacologic Classification: angiotensin II receptor antagonists

Indications ⬆ ⬇

REMS

Action ⬆ ⬇

  • Blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II at various receptor sites, including vascular smooth muscle and the adrenal glands.
Therapeutic effects:
  • Lowering of BP in hypertensive patients.
  • Decreased progression of diabetic nephropathy.
  • Decreased incidence of stroke in patients with hypertension and left ventricular hypertrophy (effect may be less in black patients).

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed but undergoes extensive first-pass hepatic metabolism, resulting in 33% bioavailability.

Distribution: Crosses the placenta.

Protein Binding: 99%.

Metabolism/Excretion: Undergoes extensive first-pass hepatic metabolism; 14% is converted to an active metabolite. 4% excreted unchanged in urine; 6% excreted in urine as active metabolite; some biliary elimination also occurs.

Half-Life: 2 hr (6–9 hr for metabolite).

Time/Action Profile ⬆ ⬇

(antihypertensive effect‡)
ROUTEONSETPEAKDURATION
PO6 hr3–6 wks24 hr

‡Onset of antihypertensive effect with chronic dosing.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects ⬆ ⬇

CV: chest pain, edema, hypotension

EENT: nasal congestion

Endo: hypoglycemia

F and E: hyperkalemia

GI: diarrhea, abdominal pain, dyspepsia, nausea

GU: renal impairment

Metab: weight gain

MS: back pain, myalgia

Neuro: dizziness, fatigue, headache, insomnia, weakness

Misc: ANGIOEDEMA, fever

Interactions ⬆ ⬇

Drug-drug:

Route/Dosage ⬆ ⬇

Renal Impairment

Hepatic Impairment

Availability ⬆ ⬇

(Generic available)

Assessment ⬆ ⬇

Lab Test Considerations:

Implementation ⬆ ⬇

Patient/Family Teaching ⬆ ⬇

Evaluation/Desired Outcomes ⬆ ⬇

US Brand Names ⬆ ⬇

Cozaar

Code ⬆

NDC Code