olmesartan

Absorption: Olmesartan medoxomil is a prodrug that is converted to olmesartan (the active component); 26% bioavailability of olmesartan.

Distribution: Crosses the placenta.

Protein Binding: 99%.

Metabolism/Excretion: No further metabolism following conversion of prodrug to active drug; 35–50% excreted unchanged in urine; remainder eliminated in feces via bile.

Half-Life: 13 hr.

Time/Action Profile ⬆ ⬇

(antihypertensive effect with chronic dosing)

ROUTE	ONSET	PEAK	DURATION
PO	within 1 wk	2 wk	24 hr

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)
OB: Pregnancy (may cause fetal harm).
Lactation: Lactation.
Pedi: Children 1 yr (may have effects on development of immature kidneys)

Use Cautiously in:

Volume- or salt-depleted patients or patients receiving high doses of diuretics (correct deficits before initiating therapy or initiate at lower doses);
Renal impairment or diabetes (↑ risk of hyperkalemia)
Black patients (may not be as effective);
Renal impairment due to primary renal disease or HF (may worsen renal function);
Rep: Women of reproductive potential;
Pedi: Children 1–6 yr (effectiveness not established).

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypotension

F and E: hyperkalemia

GI: sprue-like enteropathy

GU: impaired renal function

Neuro: dizziness

Misc: ANGIOEDEMA

Interactions ⬆ ⬇

Drug-drug:

Additive hypotension with other antihypertensives .
NSAIDs and selective COX-2 inhibitors may blunt the antihypertensive effect and ↑ the risk of renal dysfunction.
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.
↑levels and may ↑ risk of lithium toxicity.
Colesevelam may ↓ levels; administer olmesartan ≥4 hr before colesevelam

Route/Dosage ⬆ ⬇

PO (Adults ): 20 mg once daily; may be ↑ up to 40 mg daily (initiate therapy at a lower dose in patients receiving diuretics or who are volume depleted).
PO (Children 6–16 yr): ≥35 kg: 20 mg once daily; may be ↑ after 2 wk up to 40 mg once daily; 20–34.9 kg: 10 mg once daily; may be ↑ after 2 wk up to 20 mg once daily.

Availability ⬆ ⬇

(Generic available)

Tablets: 5 mg; 20 mg; 40 mg
In combination with: hydrochlorothiazide (Benicar HCT), amlodipine (Azor); amlodipine and hydrochlorothiazide (Tribenzor); seeAppendix [not included in this PDA edition].

Assessment ⬆ ⬇

Assess BP (sitting, lying, standing) and pulse periodically during therapy. If hypotension occurs, place patient in supine position. May give an IV infusion of normal saline. A transient hypotensive response is not a contraindication to further therapy; can usually be continued without difficulty once the blood pressure has stabilized.
Monitor frequency of prescription refills to determine adherence to therapy.
Assess patient for signs of angioedema (dyspnea, facial swelling). May rarely cause angioedema.
Monitor patient for signs and symptoms of sprue-like enteropathy (severe, chronic diarrhea with substantial weight loss). May develop mo or years after start of olmesartan. May require hospitalization and discontinuation of therapy.

Lab Test Considerations:

Monitor renal function. May cause ↑ BUN and serum creatinine.May rarely cause slight ↓ in hemoglobin and hematocrit.
- May occasionally cause ↑ AST, ALT, and total serum bilirubin.
- Monitor serum electrolytes periodically during therapy. May cause hyperkalemia.

Implementation ⬆ ⬇

Correct volume depletion, if possible, before initiation of therapy.
- Doses greater than 40 mg do not appear to have a greater effect. Twice daily dosing offers no advantage over the same total dose given once daily.
PO: Administer once daily without regard to food.
- For children unable to swallow tablets, pharmacist can make a suspension.

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 before 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. See Food Sources for Specific Nutrients.
Encourage patient to comply with additional interventions for hypertension (weight reduction, low-sodium diet, smoking cessation, moderation of alcohol consumption, regular exercise, and 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 position changes 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 and 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 to avoid concurrent use of Rx, OTC, and herbal products, especially NSAIDs and cough, cold, or allergy medications, without consulting health care professional.
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 of risk and discontinue olmesartan as soon and pregnancy is detected. Advise patient to notify health care professional if pregnancy is planned or suspected, and to avoid breastfeeding during therapy. If used during pregnancy, perform serial ultrasound examinations to assess the intra-amniotic environment. Fetal testing for oligohydramnios may be used, based on the wk of gestation; may not appear until after fetus has sustained irreversible injury. Monitor infants exposed to olmesartan in utero for hypotension, oliguria, and hyperkalemia. If oliguria or hypotension occur, use measures to maintain adequate blood pressure and renal perfusion. May require exchange transfusions or dialysis to reversing hypotension and supporting renal function.
Emphasize the importance of follow-up exams to evaluate effectiveness of medication.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇

Time/Action Profile ⬆ ⬇

Contraind./Precautions ⬆ ⬇

Adv. Reactions/Side Effects ⬆ ⬇

Interactions ⬆ ⬇

Route/Dosage ⬆ ⬇

Availability ⬆ ⬇

Assessment ⬆ ⬇

Implementation ⬆ ⬇

Patient/Family Teaching ⬆ ⬇

Evaluation/Desired Outcomes ⬆ ⬇

US Brand Names ⬆ ⬇

Canadian Brand Names ⬆ ⬇

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