candesartan

Absorption: Candesartan cilexetil is a prodrug that is converted to candesartan (the active component); 15% bioavailability of candesartan.

Distribution: Minimally distributed to tissues.

Protein Binding: >99%.

Metabolism/Excretion: Minor metabolism by the liver; 33% excreted in urine; 67% in feces (via bile).

Half-Life: 9 hr.

Time/Action Profile ⬆ ⬇

(antihypertensive effect)

ROUTE	ONSET	PEAK	DURATION
PO	within 2 wk	4–6 wk	unknown

Contraind./Precautions ⬆ ⬇

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);
Severe hepatic impairment;
OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

Volume- or salt-depleted patients or patients receiving large doses of diuretics (correct deficits before initiating therapy or initiate at lower doses);
Black patients (may not be as effective);
Impaired renal function due to primary renal disease or HF (may worsen renal function);
Rep: Women of reproductive potential;
Pedi: Children <1 yr (safety and effectiveness not established).

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypotension, chest pain, edema

F and E: hyperkalemia

GI: abdominal pain, diarrhea, nausea

GU: renal impairment

MS: arthralgia, back pain

Neuro: dizziness, fatigue, headache, dizziness, fatigue, headache

Misc: ANGIOEDEMA

Interactions ⬆ ⬇

Drug-drug:

NSAIDs and selective COX-2 inhibitors may blunt the antihypertensive effect and ↑ risk of renal impairment.
Additive hypotension with other antihypertensives.
Excessive hypotension may occur with concurrent use of diuretics.
Potassium-sparing diuretics, potassium-containing salt substitutes, or potassium supplements may ↑ risk of hyperkalemia.
↑risk of hyperkalemia, renal dysfunction, hypotension, and syncope ACE inhibitors or aliskiren; avoid concurrent use with aliskiren in patients with diabetes or CCr <60 mL/min.
May ↑ levels and risk of toxicity of lithium.

Route/Dosage ⬆ ⬇

Hypertension

PO (Adults ): 16 mg once daily; may ↑ up to 32 mg/day in 1–2 divided doses (initiate therapy at a lower dose in patients who are receiving diuretics or are volume depleted).
PO (Children 6–16 yr and >50 kg): 8–16 mg/day (in 1–2 divided doses); may ↑ up to 32 mg/day (in 1–2 divided doses).
PO (Children 6–16 yr and <50 kg): 4–8 mg/day (in 1–2 divided doses); may ↑ up to 16 mg/day (in 1–2 divided doses).
PO (Children 1–5 yr): 0.2 mg/kg/day (in 1–2 divided doses); may ↑ up to 0.4 mg/kg/day (in 1–2 divided doses).

Hepatic Impairment

PO (Adults ): Moderate hepatic impairment: Initiate at 8 mg once daily.

Heart Failure

PO (Adults ): 4 mg once daily initially; may double dose every 2 wk, up to target dose of 32 mg once daily.

Availability ⬆ ⬇

(Generic available)

Tablets: 4 mg; 8 mg; 16 mg; 32 mg
In combination with: hydrochlorothiazide (Atacand HCT). See Appendix [not included in this PDA edition].

Assessment ⬆ ⬇

Assess BP and HR for orthostatic changes during dose escalation and periodically during therapy.
Assess patients for signs of angioedema (dyspnea, facial swelling).
HF: Monitor daily weight and assess routinely for resolution of fluid overload (peripheral edema, rales/crackles, dyspnea, weight gain, jugular venous distention).

Lab Test Considerations:

Monitor renal function. May ↑ in BUN and serum creatinine.
- May ↑ AST, ALT, and serum bilirubin.
- Monitor potassium periodically. May cause hyperkalemia.
- May cause neutropenia, leukopenia, and agranulocytosis.

Implementation ⬆ ⬇

Correct volume depletion before starting therapy.
PO: An oral solution may be prepared by crushing the tablets.

Patient/Family Teaching ⬆ ⬇

Emphasize importance of taking as directed at the same time each day, even if feeling well. Take missed doses as soon as remembered if not almost time for next dose; do not double doses. Warn patient not to discontinue therapy unless directed by health care provider. Advise patient to read Patient Information prior to starting and with each Rx 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 provider. See Food Sources for Specific Nutrients.
Advise patient to avoid sudden position changes to ↓ risk of orthostatic hypotension. Advise that use of alcohol, standing for long periods, exercising, and hot weather may ↑ orthostasis.
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 provider of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care provider before taking any new medications, especially NSAIDs and cough, cold, or allergy remedies.
Instruct patient to notify health care provider of medication regimen before treatment or surgery.
Instruct patient to notify health care provider immediately if swelling of face, eyes, lips, or tongue or if difficulty swallowing or breathing occur.
May cause fetal harm. Advise women of reproductive potential to use effective contraception, notify health care provider immediately if pregnancy is planned or suspected, and avoid breastfeeding. Candesartan should be discontinued as soon as possible when pregnancy is detected. Conduct serial ultrasound exams in pregnant patients exposed to candesartan; may cause oligohydramnios. Monitor infants exposed to candesartan in utero for hypotension, oliguria, and hyperkalemia. If oliguria or hypotension occurs, support BP and renal perfusion. Exchange transfusions or dialysis may be required as a means of reversing hypotension and/or substituting for disordered renal function.
Emphasize 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, smoking cessation, moderation of alcohol consumption, regular exercise, stress management).
- Instruct patient and family on proper technique for monitoring BP. Advise them to check BP at least weekly and to report significant changes.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇