Aceril

 2.5 mg Tablet
Ibn Sina Pharmaceuticals Ltd.

Unit Price: ৳ 5.00 (3 x 10: ৳ 150.00)

Strip Price: ৳ 50.00

Indications
  • Hypertension:
    • Management of mild to severe hypertension to reduce blood pressure and risk of cardiovascular events.
  • Heart Failure:
    • Treatment of symptomatic heart failure following myocardial infarction or with reduced left ventricular function.
  • Post-Myocardial Infarction:
    • Reduction of mortality and morbidity in patients with acute myocardial infarction complicated by heart failure or left ventricular dysfunction.
  • Prevention of Cardiovascular Events:
    • In high-risk patients with coronary artery disease, diabetes mellitus, or other risk factors, to reduce risk of myocardial infarction, stroke, and cardiovascular death.
  • Diabetic Nephropathy:
    • To slow progression of kidney disease in type 1 and type 2 diabetic patients with proteinuria.
  • Off-label Uses:
    • Management of chronic kidney disease in non-diabetic patients.
    • Secondary prevention of stroke in hypertensive patients.
Dosage & Administration
  • Adults (Hypertension):
    • Initial dose: 2.5 mg orally once daily.
    • Maintenance dose: 2.5–20 mg per day, given once or twice daily.
    • Dose titration based on blood pressure response and tolerability.
  • Heart Failure/Post-MI:
    • Initial dose: 1.25 mg orally twice daily.
    • Maintenance dose: 2.5–10 mg twice daily.
  • Elderly:
    • Start at lower doses (1.25 mg once daily) and titrate carefully due to increased sensitivity.
  • Renal Impairment:
    • Initial dose reduction recommended (e.g., 1.25 mg daily) for creatinine clearance <40 mL/min.
    • Monitor serum potassium and renal function closely.
  • Hepatic Impairment:
    • Use with caution; no specific dose adjustment but monitor clinical response.
  • Route:
    • Oral administration.
  • Duration:
    • Chronic, daily use as prescribed.
Mechanism of Action (MOA)

Ramipril is a prodrug converted in the liver to ramiprilat, an active angiotensin-converting enzyme (ACE) inhibitor. It blocks the conversion of angiotensin I to angiotensin II, a potent vasoconstrictor. This leads to vasodilation, decreased aldosterone secretion, reduced sodium and water retention, and lowered peripheral vascular resistance. These effects result in decreased blood pressure, reduced cardiac workload, and protection against cardiac and renal remodeling.

Pharmacokinetics
  • Absorption: Well absorbed orally; peak plasma concentration in about 1 hour.
  • Bioavailability: Approximately 28% due to first-pass metabolism.
  • Distribution: Widely distributed; plasma protein binding ~73%.
  • Metabolism: Hepatic conversion to active metabolite ramiprilat.
  • Elimination: Ramiprilat has a half-life of about 13-17 hours; primarily eliminated renally.
  • Onset of Action: Blood pressure reduction begins within 1 week; full effect within 2-4 weeks.
  • Steady State: Achieved in 3-5 days.
Pregnancy Category & Lactation
  • Pregnancy:
    • FDA Category D (Contraindicated in 2nd and 3rd trimesters) due to risk of fetal toxicity including renal dysfunction, oligohydramnios, and death. Discontinue as soon as pregnancy is detected.
  • Lactation:
    • Ramipril is excreted in breast milk in small amounts; caution advised when administered to nursing mothers.
Therapeutic Class
  • Antihypertensive
  • Angiotensin-converting enzyme (ACE) inhibitor
  • Cardioprotective agent
Contraindications
  • Known hypersensitivity to ramipril or other ACE inhibitors.
  • History of angioedema related to previous ACE inhibitor therapy.
  • Hereditary or idiopathic angioedema.
  • Pregnancy (especially 2nd and 3rd trimesters).
  • Severe renal impairment or bilateral renal artery stenosis.
  • Concomitant use with aliskiren in diabetic patients.
Warnings & Precautions
  • Risk of angioedema; emergency treatment required if swelling occurs.
  • Monitor for hyperkalemia, especially in patients on potassium-sparing diuretics or supplements.
  • May cause hypotension, particularly in volume- or salt-depleted patients.
  • Monitor renal function periodically.
  • Use with caution in patients with bilateral renal artery stenosis or aortic stenosis.
  • Avoid NSAIDs concomitantly due to risk of renal impairment.
  • Not recommended during pregnancy.
Side Effects

Common:

  • Cough (dry, persistent)
  • Dizziness, hypotension
  • Fatigue
  • Headache
  • Nausea

Serious:

  • Angioedema
  • Hyperkalemia
  • Acute renal failure
  • Neutropenia/agranulocytosis (rare)
  • Hepatic dysfunction (rare)
Drug Interactions

 

  • Potassium-sparing diuretics, potassium supplements: Increased risk of hyperkalemia.
  • NSAIDs: May reduce antihypertensive effect and increase risk of renal impairment.
  • Diuretics: May cause additive hypotension.
  • Lithium: Increased lithium toxicity risk.
  • Other antihypertensives: Additive blood pressure lowering effect.
  • Aliskiren: Contraindicated in diabetic patients due to increased risk of renal impairment and hyperkalemia.
Recent Updates or Guidelines
  • Updated hypertension guidelines recommend ACE inhibitors like ramipril as first-line agents for hypertension, heart failure, and renal protection, especially in diabetics.
  • Newer studies reaffirm cardiovascular and renal protective benefits beyond blood pressure lowering.
  • Caution advised with combined use of ACE inhibitors and direct renin inhibitors (aliskiren) in patients with diabetes or renal impairment.
  • Monitoring protocols for hyperkalemia and renal function emphasized.
Storage Conditions
  • Store at 20°C to 25°C (68°F to 77°F).
  • Protect from moisture and light.
  • Keep in tightly closed containers.
  • Do not freeze.
Available Brand Names