AZOR
Clinical safety rating
cautionComprehensive clinical and safety monograph for AZOR (AZOR).
Amlodipine is a dihydropyridine calcium channel blocker that inhibits calcium ion influx across cardiac and vascular smooth muscle cells, causing vasodilation and reduced peripheral vascular resistance. Olmesartan is an angiotensin II receptor blocker (ARB) that selectively blocks AT1 receptors, inhibiting vasoconstriction and aldosterone secretion.
| Metabolism | Amlodipine is extensively metabolized in the liver via CYP3A4 to inactive metabolites. Olmesartan is metabolized by the liver to a minor extent; it undergoes glucuronidation and some oxidation by CYP2C9. |
| Excretion | Renal: 90% (amlodipine: 60% as metabolites, 10% as parent; olmesartan: 35-50% as parent via urine, rest in feces via bile). Fecal: 10% |
| Half-life | Amlodipine: 30-50 h (terminal); supports once-daily dosing. Olmesartan: 10-15 h (terminal); once-daily dosing effective |
| Protein binding | Amlodipine: ~93% bound to plasma proteins. Olmesartan: >99% bound to albumin |
| Volume of Distribution | Amlodipine: 21 L/kg (large, extensive tissue distribution). Olmesartan: 17-30 L (approximate, Vd not typically reported per kg); distribution into tissues |
| Bioavailability | Oral: amlodipine 64-90% (high, first-pass ~10%); olmesartan 26% (oral, complete absorption reduced by first-pass ester hydrolysis) |
| Onset of Action | Oral: amlodipine 30-50 min (vasodilation); olmesartan 1-2 h (angiotensin II blockade). Peak effect: antihypertensive within 24 h |
| Duration of Action | Amlodipine: 24 h (once-daily due to long half-life). Olmesartan: 24 h (dose-dependent). Clinical: sustained BP reduction over 24 h |
| Molecular Weight | 791.28 |
AZOR is a combination of amlodipine and olmesartan. Typical adult dose: one tablet orally once daily. Available strengths: amlodipine/olmesartan 5mg/20mg, 5mg/40mg, 10mg/20mg, 10mg/40mg. Dose can be titrated based on blood pressure response.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment is required for mild to moderate renal impairment (CrCl ≥30 mL/min). For severe renal impairment (CrCl <30 mL/min), use with caution; maximum dose of olmesartan is 20 mg once daily. Monitor serum potassium and creatinine. |
| Liver impairment | No dose adjustment for mild hepatic impairment (Child-Pugh A). For moderate to severe hepatic impairment (Child-Pugh B or C), amlodipine half-life is prolonged; initiate with amlodipine 2.5 mg and olmesartan 10 mg, and titrate slowly. Use caution; contraindicated in severe hepatic impairment with cholestasis? Not specifically contraindicated but not recommended. |
| Pediatric use | Safety and efficacy in pediatric patients <18 years have not been established. Not recommended for use in children. |
| Geriatric use | In elderly patients (≥65 years), start with the lowest available dose (amlodipine/olmesartan 5/20 mg daily) and titrate slowly due to increased sensitivity and potential for hypotension. Monitor renal function and electrolytes closely in geriatric patients. |
| 1st trimester | Contraindicated due to risk of fetal hypotension, renal dysfunction, and oligohydramnios; can cause fetal and neonatal toxicity. |
| 2nd trimester | Contraindicated due to risk of fetal renal impairment and oligohydramnios; potential for fetal skull hypoplasia. |
| 3rd trimester | Contraindicated due to risk of fetal renal failure, oligohydramnios, and neonatal hypotension. |
Clinical note
Comprehensive clinical and safety monograph for AZOR (AZOR).
| Placental transfer | Both components cross placenta; amlodipine and olmesartan are detected in fetal circulation. |
| Breastfeeding | Excreted in human milk; limited data available. Discontinue nursing or drug due to potential for adverse effects in nursing infant, especially hypotension and renal impairment. |
| Lactation Rating | L4 (Possibly Hazardous) – avoid breastfeeding if possible. |
| Teratogenic Risk | Pregnancy Category D. First trimester: Potential for fetal toxicity (oligohydramnios, fetal/neonatal renal dysfunction, skull hypoplasia) due to olmesartan action on renin-angiotensin system; avoid use. Second trimester: Continued risk of fetal renal impairment and oligohydramnios. Third trimester: High risk of fetal/neonatal renal failure, hypotension, hyperkalemia, and skull ossification defects; contraindicated. |
| Fetal Monitoring | Monitor maternal blood pressure, renal function (serum creatinine, BUN), and serum potassium. Fetal monitoring: serial ultrasound for amniotic fluid volume, fetal growth, and renal anatomy. If oligohydramnios occurs, consider drug discontinuation. Neonatal monitoring for hypotension, hyperkalemia, and renal function after delivery. |
| Fertility Effects | No specific human data on AZOR's effects on fertility. Olmesartan and amlodipine are not known to impair fertility in animal studies. ACE inhibitors/ARBs may theoretically affect reproductive function via renin-angiotensin system modulation, but no clinical evidence of significant fertility impairment with AZOR. |
■ FDA Black Box Warning
None
| Serious Effects |
PregnancyHypersensitivity to amlodipine, olmesartan, or any ingredientConcomitant use with aliskiren in patients with diabetes mellitus or renal impairment (GFR <60 mL/min/1.73 m²)
| Precautions | Fetal toxicity (detectable in second and third trimesters): drugs acting on the renin-angiotensin system can cause oligohydramnios, fetal renal dysfunction, and death, Avoid concomitant use with aliskiren in patients with diabetes, Hypotension in volume/depleted patients, Increased angina or myocardial infarction with calcium channel blockers, particularly with severe obstructive coronary artery disease, Peripheral edema is dose-dependent and more common with amlodipine, Hepatic impairment: lower starting dose, Renal artery stenosis, Electrolyte imbalances |
| Food/Dietary | Avoid grapefruit and grapefruit juice due to CYP3A4 inhibition increasing amlodipine levels. No other significant food interactions. |
| Clinical Pearls | AZOR is a fixed-dose combination of amlodipine (calcium channel blocker) and olmesartan (angiotensin II receptor blocker). Monitor serum potassium and creatinine, especially in renal impairment or concomitant ACE inhibitor use. Avoid in pregnancy (use effective contraception). May cause dizziness or peripheral edema, often dose-related. |
| Patient Advice | Take exactly as prescribed, usually once daily, with or without food. · Avoid grapefruit or grapefruit juice as it can increase amlodipine levels. · Notify your doctor if you become pregnant or plan to become pregnant. · Do not stop taking suddenly; consult your doctor before discontinuing. · Report lightheadedness, fainting, or significant swelling in your ankles or feet. · Use caution when driving or operating machinery until you know how this medication affects you. |
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