Contraindicated in:
Use Cautiously in:
CV: hypotension, chest pain, edema, tachycardia.
Derm: rash.
EENT: nasal congestion, pharyngitis, rhinitis, sinusitis.
GI: abdominal pain, diarrhea, drug-induced hepatitis, dyspepsia, nausea, vomiting.
GU: impaired renal function.
F and E: hyperkalemia.
MS: arthralgia, back pain, myalgia.
Neuro: dizziness, anxiety, depression, fatigue, headache, insomnia, weakness.
Misc: ANGIOEDEMA.
Drug-Drug:
Azilsartan
(generic available)
Candesartan
(generic available)
Irbesartan
(generic available)
Losartan
(generic available)
Olmesartan
(generic available)
Telmisartan
(generic available)
Valsartan
(generic available)
Azilsartan
Candesartan
Hepatic Impairment
Irbesartan
Losartan
Hepatic Impairment
Renal Impairment
Olmesartan
Telmisartan
Valsartan
Oral tablets and suspension are NOT interchangeable on a mg-per-mg basis. These dosage forms should not be combined to arrive at a particular dose.
azilsartan: Edarbi
candesartan: Atacand
irbesartan: Avapro
losartan: Cozaar
olmesartan: Benicar
telmisartan: Micardis
valsartan: Diovan
Therapeutic Classification: antihypertensives
Pharmacologic Classification: angiotensin II receptor antagonists
Absorption: Azilsartan Azilsartan medoxomil is converted to azilsartan, the active component. 60% absorbed; Candesartan Candesartan cilexetil is converted to candesartan, the active component; 15% bioavailability of candesartan; Irbesartan 6080% absorbed after oral administration; Losartan well absorbed, with extensive first-pass hepatic metabolism, resulting in 33% bioavailability; Olmesartan Olmesartan medoxomil is converted to olmesartan, the active component; 26% bioavailability of olmesartan; Telmisartan 4258% absorbed following oral administration (bioavailability ↑ in patients with hepatic impairment); Valsartan 1035% absorbed following oral administration; systemic exposure 60% higher with the suspension compared to tablets.
Distribution: All angiotensin receptor blockers (ARBs) cross the placenta; Candesartan enters breast milk.
Protein Binding: All ARBs are >90% protein-bound.
Metabolism/Excretion: Azilsartan 50% metabolized by the liver, primarily by the CYP2C9 enzyme system. 55% eliminated in feces, 42% in urine (15% as unchanged drug); Candesartan Minor metabolism by the liver; 33% excreted in urine, 67% in feces (via bile); Irbesartan Some hepatic metabolism; 20% excreted in urine, 80% in feces; Losartan 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; Olmesartan 3050% excreted unchanged in urine, remainder eliminated in feces via bile; Telmisartan Excreted mostly unchanged in feces via biliary excretion; Valsartan Minor metabolism by the liver; 13% excreted in urine, 83% in feces.
Half-life: Azilsartan 11 hr; Candesartan 9 hr; Irbesartan 1115 hr; Losartan 2 hr (69 hr for metabolite); Olmesartan 13 hr; Telmisartan 24 hr; Valsartan 6 hr.
(antihypertensive effect with chronic dosing)
DRUG | ONSET | PEAK | DURATION |
---|---|---|---|
Azilsartan | within 2 hr | 18 hr | 24 hr |
Candesartan | 24 hr | 4 wk | 24 hr |
Irbesartan | within 2 hr | 2 wk | 24 hr |
Losartan | 6 hr | 36 wk | 24 hr |
Olmesartan | within 1 wk | 2 wk | 24 hr |
Telmisartan | within 3 hr | 4 wk | 24 hr |
Valsartan | within 2 hr | 4 wk | 24 hr |