EDARBI
Clinical safety rating
cautionComprehensive clinical and safety monograph for EDARBI (EDARBI).
Angiotensin II receptor blocker (ARB) that selectively blocks the binding of angiotensin II to AT1 receptors, leading to vasodilation, reduced aldosterone secretion, and decreased blood pressure.
| Metabolism | Primarily metabolized by CYP2C9 and CYP3A4; undergoes dehydrogenation and decarboxylation. |
| Excretion | Approximately 60% of dose is excreted in feces (primarily as unchanged drug) and 33% in urine (as metabolites, predominantly glucuronide conjugates). |
| Half-life | Approximately 20-22 hours in normal subjects; allows once-daily dosing. Half-life increases in moderate to severe hepatic impairment. |
| Protein binding | High (>99% bound to serum proteins, mainly albumin). |
| Volume of Distribution | Approximately 0.9 L/kg (total Vdss of about 86 L), indicating extensive distribution into tissues. |
| Bioavailability | Absolute bioavailability is about 15% due to extensive first-pass metabolism (CYP2C9, UGT1A3). |
| Onset of Action | Usually within 2 hours following oral administration; peak antihypertensive effect is achieved after 4-6 weeks of therapy. |
| Duration of Action | Dosing interval of 24 hours; antihypertensive effect persists over the 24-hour dosing interval with once-daily administration. |
| Molecular Weight | 558.65 |
EDARBI (azilsartan medoxomil) is administered orally. The recommended starting dose is 40 mg once daily. For patients requiring further blood pressure reduction, the dose may be increased to 80 mg once daily. Maximal antihypertensive effect is attained within 2 weeks.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment is required for patients with mild to moderate renal impairment (eGFR ≥30 mL/min/1.73 m²). For patients with severe renal impairment (eGFR <30 mL/min/1.73 m²) or end-stage renal disease (ESRD), caution is advised; no specific dosing recommendations are available due to limited data. Avoid use in patients undergoing dialysis. |
| Liver impairment | No dose adjustment is needed for mild hepatic impairment (Child-Pugh class A). For moderate hepatic impairment (Child-Pugh class B), the recommended starting dose is 40 mg once daily; maximum dose is 40 mg once daily. EDARBI should not be used in patients with severe hepatic impairment (Child-Pugh class C). |
| Pediatric use | Safety and efficacy in pediatric patients (<18 years) have not been established. Therefore, no dosing recommendation is provided. |
| Geriatric use | No dose adjustment is required for elderly patients (≥65 years). However, as with all patients, initiate at 40 mg once daily; consider cautious titration due to potential greater sensitivity and increased risk of hypotension. |
| 1st trimester | Use in first trimester is associated with a low risk of teratogenicity; however, due to the risk of oligohydramnios in the second and third trimesters, it is generally recommended to avoid use throughout pregnancy. |
| 2nd trimester | Use in second trimester is associated with fetal renal dysfunction, oligohydramnios, and skull ossification defects. Contraindicated. |
| 3rd trimester | Use in third trimester can cause fetal and neonatal renal failure, oligohydramnios, and death. Contraindicated. |
Clinical note
Comprehensive clinical and safety monograph for EDARBI (EDARBI).
| Placental transfer | Crosses the placenta in humans; detected in fetal cord blood. |
| Breastfeeding | Not recommended during breastfeeding as it may cause adverse effects in the infant; no adequate human data available. |
| Lactation Rating | L4 - Possibly Hazardous |
| Teratogenic Risk | Drugs acting directly on the renin-angiotensin system (RAS) can cause fetal and neonatal morbidity and death when used in pregnancy. First-trimester exposure: Potential for fetal renal damage, oligohydramnios, and skull ossification defects. Second and third trimester exposure: Increased risk for oligohydramnios, fetal renal dysfunction, skull hypoplasia, hypotension, and anuria. Use is contraindicated in pregnancy, especially in second and third trimesters. |
| Fetal Monitoring | Monitor maternal blood pressure and renal function. If inadvertent exposure occurs during pregnancy, perform serial ultrasound assessments for amniotic fluid volume, fetal renal function, and fetal skull development. |
| Fertility Effects | No human data on fertility effects. Animal studies show no adverse effects on male or female fertility at clinically relevant doses. |
■ FDA Black Box Warning
No FDA boxed warnings.
| Serious Effects |
Concomitant use with aliskiren in patients with diabetes mellitusHistory of angioedema related to previous ACE inhibitor or ARB therapyPregnancy (second and third trimesters)
| Precautions | Fetal toxicity: Avoid in pregnancy; discontinue if pregnancy occurs, Hypotension in volume-depleted patients, Renal function impairment: Monitor serum creatinine and potassium, Hyperkalemia: Risk in patients with renal impairment or on potassium-sparing diuretics, Avoid use in patients with bilateral renal artery stenosis |
| Food/Dietary | No significant food interactions. May be taken with or without food. Avoid excessive intake of potassium-rich foods (e.g., bananas, oranges, potatoes, tomatoes) and salt substitutes containing potassium, especially in patients with renal impairment or those on concomitant RAAS inhibitors or potassium-sparing diuretics. |
| Clinical Pearls | Edarbi (azilsartan medoxomil) is an angiotensin II receptor blocker (ARB) with high receptor affinity and a long half-life (~11 hours), allowing once-daily dosing. It is a prodrug that is rapidly hydrolyzed to the active moiety azilsartan. Onset of action within 2 weeks; maximum effect may take 4-6 weeks. Monitor renal function and serum potassium, especially in patients with renal impairment, diabetes, or those taking NSAIDs or potassium-sparing diuretics. Avoid use in pregnancy (category D). Dose adjustment recommended for patients with hepatic impairment (Child-Pugh class B). |
| Patient Advice | Take exactly as prescribed, usually once daily, with or without food. · Do not take if pregnant or planning to become pregnant; use effective contraception. · Avoid salt substitutes containing potassium unless approved by your doctor. · Report symptoms such as dizziness, fainting, rapid heartbeat, or signs of kidney problems (e.g., swelling, decreased urination). · If you miss a dose, take it as soon as you remember, but skip if it is almost time for the next dose. Do not double the dose. · Avoid nonsteroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen or naproxen without medical advice. |
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