Adarbi

• Hypertension:
  Azilsartan medoxomil is indicated for the treatment of essential hypertension to lower blood pressure in adults. It can be used as monotherapy or in combination with other antihypertensive agents.
• Off-label Uses (Clinically Accepted):
• Adjunctive treatment in heart failure management (limited data).
• Potential benefit in patients with diabetic nephropathy or chronic kidney disease (ongoing studies).
• May be used to reduce cardiovascular risk associated with hypertension.

Route: Oral

Adults:

• Initial Dose: 40 mg once daily.
• Maintenance Dose: 40 mg to 80 mg once daily.
• Dose may be adjusted based on blood pressure response.
• Maximum dose: 80 mg/day.

Special Populations:

• Elderly: No initial dose adjustment required; monitor blood pressure and renal function.
• Renal Impairment: Use with caution in patients with severe renal impairment (eGFR <30 mL/min/1.73 m²); dose adjustment not specifically required but careful monitoring advised.
• Hepatic Impairment: Use with caution in mild to moderate hepatic impairment; avoid use in severe hepatic impairment due to lack of data.

Administration Tips:

• Can be taken with or without food.
• Administer at the same time each day for consistent blood levels.
• Tablets should be swallowed whole.

Azilsartan medoxomil is a prodrug rapidly converted in the gastrointestinal tract to azilsartan, a selective angiotensin II receptor type 1 (AT1) antagonist. By blocking AT1 receptors, azilsartan inhibits the vasoconstrictive and aldosterone-secreting effects of angiotensin II, resulting in vasodilation, reduced peripheral vascular resistance, decreased sodium and water retention, and ultimately lowered blood pressure. This blockade also reduces the cardiac and vascular remodeling associated with hypertension.

• Absorption:
  Azilsartan medoxomil is well absorbed orally and rapidly hydrolyzed to azilsartan.
  Absolute bioavailability of azilsartan is approximately 60%.
  Peak plasma concentrations occur within 1.5 to 3 hours after dosing.
• Distribution:
  Plasma protein binding is approximately 99% (mainly to albumin).
• Metabolism:
  Metabolized primarily via CYP2C9-mediated O-deethylation and glucuronidation.
• Half-life:
  Effective plasma half-life is approximately 11 hours, supporting once-daily dosing.
• Elimination:
  Excreted via feces (~55%) and urine (~42%) mostly as metabolites.

• Pregnancy:
  Classified as FDA Pregnancy Category D. Use is contraindicated in the second and third trimesters due to risk of fetal toxicity, including renal dysfunction, oligohydramnios, and death. If pregnancy is detected, discontinue immediately.
• Lactation:
  It is unknown whether azilsartan is excreted in human milk; breastfeeding is not recommended during treatment.

• Primary Therapeutic Class: Antihypertensive
• Subclass: Angiotensin II receptor blocker (ARB) – selective AT1 receptor antagonist

• Known hypersensitivity to azilsartan, azilsartan medoxomil, or any excipients.
• Pregnancy, especially second and third trimesters.
• Concomitant use with aliskiren in patients with diabetes mellitus or renal impairment (eGFR <60 mL/min/1.73 m²).
• Severe hepatic impairment (due to lack of safety data).

• Hypotension: Risk increased in volume- or salt-depleted patients.
• Renal Function: May cause renal impairment; monitor renal function periodically, especially in patients with pre-existing renal disease or heart failure.
• Hyperkalemia: Monitor serum potassium due to risk of elevation, especially in patients on potassium-sparing diuretics or potassium supplements.
• Angioedema: Rare but potentially fatal; discontinue immediately if angioedema occurs.
• Surgery/Anesthesia: May enhance hypotensive effects during anesthesia or surgery; monitor blood pressure carefully.

Common (>1%):

• Dizziness
• Fatigue
• Diarrhea
• Increased serum creatinine
• Hypotension

Less Common/Rare:

• Hyperkalemia
• Angioedema
• Renal impairment
• Syncope
• Headache

• Potassium-sparing diuretics, potassium supplements, or potassium-containing salt substitutes: May increase risk of hyperkalemia.
• NSAIDs: May reduce antihypertensive effect and increase risk of renal impairment.
• Aliskiren: Contraindicated in diabetics or renal impairment due to increased risk of adverse effects.
• Lithium: Increased lithium toxicity risk due to decreased renal clearance.
• CYP2C9 inhibitors: May increase azilsartan plasma concentrations slightly; monitor patient.

• Azilsartan medoxomil is recognized in hypertension guidelines as an effective ARB with a favorable safety profile and once-daily dosing.
• Recent comparative studies suggest superior or comparable efficacy versus other ARBs and ACE inhibitors in lowering blood pressure.
• Monitoring renal function and potassium remains a priority in clinical practice.

• Store tablets at 20°C to 25°C (68°F to 77°F).
• Protect from moisture and light.
• Keep container tightly closed.
• Avoid freezing.