Dosing and uses of Benicar (olmesartan)
Adult dosage forms and strengths
tablet
- 5mg
- 20mg
- 40mg
Hypertension
20 mg/day PO initially; may be increased to 40 mg/day PO after 2 weeks; a diuretic may be added
Dosing Modifications
Renal impairment
- CrCl <40 mL/min: No adjustment needed
- CrCl <20 mL/min: Consider using lower initial dosage and not exceeding 20 mg/day
Hepatic impairment
- No need for initial dosage adjustment
Dosing Considerations
Volume-depleted patients: Consider lower initial dosage
Also given in combination with hydrochlorothiazide (Benicar HCT)
Pediatric dosage forms and strengths
tablet
- 5mg
- 20mg
- 40mg
Hypertension
<6 years
- Safety and efficacy not established (see Cautions)
6-16 years
- <20 kg: Safety and efficacy not established
- 20-35 kg: 10 mg/day PO initially; after 2 weeks, may be increased if response is inadequate; dosage range: 10-20 mg/day
- >35 kg: 20 mg/day PO initially; after 2 weeks, may be increased if response is inadequate; dosage range: 20-40 mg/day
Geriatric dosage forms and strengths
A lower starting dosage may be used
Hypertension
5-10 mg/day PO initially; may be increased to 40 mg/day PO after 2 weeks (with monitoring of blood pressure); a diuretic may be added
Benicar (olmesartan) adverse (side) effects
1-10%
Dizziness
Headache
Fatigue
Diarrhea
Hyperglycemia
Hypertriglyceridemia
Back pain
Bronchitis
Inflicted injury
Flulike symptoms
Pharyngitis
Rhinitis
Sinusitis
Upper respiratory tract infection (URTI)
Frequency not defined (selected)
Anaphylactic reaction
Angioedema
Facial edema
Rhabdomyolysis
Hyperkalemia
Tachycardia
Hypercholesterolemia
Gastroenteritis
Hyperlipidemia
Warnings
Black box warnings
Discontinue as soon as possible when pregnancy is detected; drug affects renin-angiotensin system, causing oligohydramnios, which may result in fetal injury or death
Contraindications
Hypersensitivity
Do not coadminister with aliskiren in patients with diabetes mellitus or with renal impairment (ie, GFR <60 mL/min/1.73 m²)
Cautions
Angioedema, severe congestive heart failure (CHF), surgery or anesthesia, volume depletion (consider lower dosage)
Coadministration with mTOR inhibitors (eg, temsirolimus) may increased risk for angioedema
Risk of hypotension, especially in patients with volume or salt depletion secondary to salt restriction or prolonged diuretic treatment
Risk of hyperkalemia
Use with caution in renal artery stenosis; avoid in bilateral renal artery stenosis
Renal impairment reported
Intestinal problems (ie, sprue-like enteropathy) reported; symptoms may include severe, chronic diarrhea with substantial weight loss
Dual blockade of the renin-angiotensin system with angiotensin-receptor blockers (ARBs), angiotensin-converting enzyme (ACE) inhibitors, or aliskiren is associated with increased risk of hypotension, hyperkalemia, and altered renal function (including acute renal failure) in comparison with monotherapy; closely monitor blood pressure
Children <1 year of age must not receive olmesartan for hypertension; drugs that act directly on the renin-angiotensin-aldosterone system can have adverse effects on the development of immature kidneys
Pregnancy and lactation
Pregnancy category: 1st trimester, C; 2nd and 3rd trimesters, d
Lactation: No human data; use with caution
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Benicar (olmesartan)
Mechanism of action
Blocks binding of angiotensin II to type 1 angiotensin II receptors; blocks vasoconstrictor and aldosterone-secreting effects of angiotensin II
Absorption
Bioavailability: 26%
Onset: <2 weeks
Peak response: 4-6 weeks
Duration: 24 hr
Peak plasma time: 1-2 hr
Distribution
Protein bound: 99%
Vd: 17 L; does not cross blood-brain barrier
Metabolism
Rapidly and completely deesterified to active olmesartan in intestinal wall; no further metabolism occurs
Metabolites: RNH-6270 (deesterified olmesartan; active)
Elimination
Half-life: 13 hr
Renal clearance: 0.5-0.8 L/hr
Total body clearance: 1.3 L/hr
Excretion: Bile (50-65%), urine (35-50%)
