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)
  • Tablets: 25 mg; 50 mg; 100 mg
  • In combination with: hydrochlorothiazide (Hyzaar); see Appendix [not included in this PDA edition]).

Assessment

  • Assess BP (lying, sitting, standing) and pulse frequently during initial dose adjustment and periodically during therapy. Notify health care professional of significant changes.
  • Monitor frequency of prescription refills to determine compliance.
  • Assess patient for signs of angioedema (dyspnea, facial swelling). May rarely cause angioedema.

Lab Test Considerations:

  • Monitor renal function. May cause BUN and serum creatinine.
    • May cause AST, ALT, and serum bilirubin.
    • May cause hyperkalemia.
    • May cause slight hemoglobin and hematocrit.

Implementation

  • Do not confuse Cozaar with Colace or Zocor.
    • Correct volume depletion, if possible, before initiation of therapy.
  • PO: Administer once daily. For patients with difficulty swallowing tablets, pharmacist can compound an oral suspension; stable for 4 wk if refrigerated. Shake suspension before each use.

Patient/Family Teaching

  • Emphasize the importance of continuing to take as directed, even if feeling well. Take missed doses as soon as remembered if not almost time for next dose; do not double doses. Medication controls but does not cure hypertension. Instruct patient to take medication at the same time each day. Warn patient not to discontinue therapy unless directed by health care professional.
  • Caution patient to avoid salt substitutes containing potassium or foods containing high levels of potassium or sodium unless directed by health care professional. SeeFood Sources for Specific Nutrients.
  • Caution patient to avoid sudden changes in position to decrease orthostatic hypotension. Use of alcohol, standing for long periods, exercising, and hot weather may increase orthostatic hypotension.
  • May cause dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
  • Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
  • Instruct patient to notify health care professional of medication regimen before treatment or surgery.
  • Instruct patient to notify health care professional if swelling of face, eyes, lips, or tongue or if difficulty swallowing or breathing occur.
  • Rep: May cause fetal harm. Advise females of reproductive potential to use contraception and notify health care professional if pregnancy is planned or suspected, or if breastfeeding. Losartan should be discontinued as soon as possible when pregnancy is detected. Avoid breastfeeding.
  • Emphasize the importance of follow-up exams to evaluate effectiveness of medication.
  • Hypertension: Encourage patient to comply with additional interventions for hypertension (weight reduction, low-sodium diet, discontinuation of smoking, moderation of alcohol consumption, regular exercise, stress management). Medication controls but does not cure hypertension.
    • Instruct patient and family on proper technique for monitoring BP. Advise them to check BP at least weekly and to report significant changes.

Evaluation/Desired Outcomes

  • Decrease in BP without appearance of excessive side effects.
  • Delayed progression of diabetic nephropathy in patients with type 2 diabetes.
  • Decreased incidence of stroke in patients with hypertension and left ventricular hypertrophy.

US Brand Names

Cozaar

Code

NDC Code