tel-mi-SAR-tan

Therapeutic Classification: antihypertensives

Pharmacologic Classification: angiotensin II receptor antagonists

• Hypertension (as monotherapy or in combination with other antihypertensive agents).
• Reduction of risk of MI, stroke, or cardiovascular death in patients 55 yr who are at high risk for cardiovascular events and are unable to take ACE inhibitors.

• Blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II at various receptor sites, including vascular smooth muscle and the adrenal glands.

• Lowering of BP.
• Reduction of risk of MI, stroke, or cardiovascular death.

Absorption: 42–58% absorbed following oral administration (bioavailability increased in patients with hepatic impairment).

Distribution: Crosses the placenta.

Protein Binding: 99.5%.

Metabolism/Excretion: Excreted mostly unchanged in feces via biliary excretion.

Half-life: 24 hr.

(antihypertensive effect)

*After single dose.

†Chronic dosing.

Contraindicated in:

• Hypersensitivity
• Bilateral renal artery stenosis
• Concurrent use with aliskiren in patients with diabetes or moderate to severe renal impairment (CCr <60 mL/min)
• OB: Pregnancy
• Lactation: Lactation.

Use Cautiously in:

• Volume- or salt-depleted patients or patients receiving large doses of diuretics (correct deficits before initiating therapy)
• Black patients (may not be as effective)
• Renal impairment caused by primary renal disease or heart failure (may worsen renal function)
• Obstructive biliary disorders or hepatic impairment
• Women of reproductive potential
• Pedi: Safety and effectiveness not established in children.

CV: hypotension.

EENT: sinusitis.

F and E: hyperkalemia.

GI: abdominal pain, diarrhea, dyspepsia.

GU: renal impairment.

MS: back pain, myalgia.

Neuro: dizziness, fatigue, headache.
Misc: ANGIOEDEMA.

Drug-Drug:

• Additive hypotensive effects with other antihypertensives.
• Excessive hypotension may occur with concurrent use of diuretics.
• ↑risk of hyperkalemia with concurrent use of potassium supplements, potassium-containing salt substitutes, or potassium-sparing diuretics.
• ↑risk of hyperkalemia, renal dysfunction, hypotension, and syncope with concurrent use of ACE inhibitors or aliskiren; avoid concurrent use with aliskiren in patients with diabetes or CCr <60 mL/min; avoid concurrent use with ACE inhibitors.
• May ↑ serum digoxin levels.
• NSAIDs and selective COX-2 inhibitors may blunt the antihypertensive effect and ↑ the risk of renal dysfunction.
• ↑risk of renal dysfunction when used with ramipril; concurrent use not recommended.

Hypertension

• PO (Adults): 40 mg once daily (volume-depleted patients should start with 20 mg); may be titrated up to 80 mg/day.

Cardiovascular Risk Reduction

• PO (Adults): 80 mg once daily.

(Generic available)

• Tablets: 20 mg; 40 mg; 80 mg;
• In combination with: hydrochlorothiazide (Micardis HCT); amlodipine; seeAppendix [not included in this PDA edition].

• 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 patients for signs of angioedema (dyspnea, facial swelling).

• Monitor renal function. May cause ↑ BUN and serum creatinine.
  • May cause hyperkalemia.

• Volume depletion should be corrected, if possible, before initiation of therapy.
• PO: May be administered without regard to meals.

• 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. Instruct patient to take medication at the same time each day. Warn patient not to discontinue therapy unless directed by health care professional. Advise patient to read Patient Information prior to starting therapy and with each refill in case of changes.
• Caution patient to avoid salt substitutes containing potassium or foods containing high levels of potassium or sodium unless directed by health care professional. SeeAppendix M.
• 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.
• 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.
• Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications, especially NSAIDs, cough, cold, or allergy remedies.
• 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.
• Emphasize the importance of follow-up exams to evaluate effectiveness of medication.
• 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. If pregnancy is detected, discontinue medication as soon as possible.

• Decrease in BP without appearance of excessive side effects.
• Decreased risk of MI, stroke, or cardiovascular death.

Micardis