Amdoper

FDA-Approved Uses

• Hypertension (Adults and Children ≥6 years)
  Used alone or with other antihypertensive agents to lower blood pressure and reduce cardiovascular risk.
• Chronic Stable Angina
  Effective in reducing frequency and severity of anginal attacks, regardless of physical activity level.
• Vasospastic (Prinzmetal’s) Angina
  Relieves coronary artery spasm and prevents episodes of angina.
• Coronary Artery Disease (CAD) Without Heart Failure
  Reduces the risk of hospitalization due to angina in patients with documented CAD.

Clinically Accepted Off-Label Uses

• Raynaud's Phenomenon
  Helps relieve vasospasm in extremities by promoting peripheral vasodilation.
• Hypertension in Renal Transplant Recipients
  Well-tolerated and effective in controlling post-transplant hypertension.
• Hypertension in Pregnancy (Non-severe cases)
  Used cautiously when benefits outweigh risks; considered in 2nd or 3rd trimester under specialist supervision.
• Silent Myocardial Ischemia
  Used in patients with asymptomatic ischemia for coronary vasodilation and ischemic burden reduction.
• Left Ventricular Hypertrophy (LVH)
  Amlodipine reduces LV mass in hypertensive patients.

রেজিস্টার্ড চিকিৎসকের পরামর্শ ছাড়া ওষুধ সেবন করবেন না।

Adults

• Hypertension: Start with 5 mg once daily; adjust up to a maximum of 10 mg once daily based on clinical response.
• Angina & CAD: Initial dose 5–10 mg once daily. Most patients require 10 mg for full anti-anginal effect.

Pediatrics (6–17 years)

• Hypertension: Start with 2.5 mg once daily. Maximum recommended dose is 5 mg/day.

Geriatrics

• Increased systemic exposure possible. Start with 2.5 mg once daily, titrate cautiously.

Hepatic Impairment

• Start at lower dose (2.5 mg once daily). Clearance is significantly reduced; careful titration required.

Renal Impairment

• No dosage adjustment needed. Drug is not significantly removed by dialysis.

Amlodipine inhibits the influx of extracellular calcium ions across the cell membranes of both vascular smooth muscle and cardiac muscle by selectively blocking L-type calcium channels. This inhibition causes a reduction in peripheral vascular resistance (afterload), leads to vasodilation, and reduces blood pressure. In the coronary vasculature, it enhances oxygen delivery by dilating large arteries and arterioles and prevents spasm, reducing myocardial oxygen demand and alleviating angina symptoms. It does not significantly affect heart rate or myocardial contractility at therapeutic doses.

• Absorption: Slowly but well absorbed after oral administration. Peak plasma concentrations reached in 6–12 hours. Absolute bioavailability: 64–90%.
• Distribution: Highly bound to plasma proteins (~93–98%). Volume of distribution is about 21 L/kg, indicating extensive tissue distribution.
• Metabolism: Extensively metabolized by the liver via CYP3A4 to inactive metabolites.
• Excretion: Elimination half-life ranges from 30 to 50 hours, allowing once-daily dosing. ~60% excreted in urine as metabolites, ~10% as unchanged drug.
• Special Populations:
• Hepatic impairment: Reduced clearance, prolonged half-life.
• Renal impairment: Pharmacokinetics not significantly altered.

• Pregnancy: No longer classified under FDA’s pregnancy category system. Animal studies showed fetal toxicity at high doses. No adequate, controlled studies in pregnant women. Use only if clearly needed and under supervision.
• Lactation: Excreted in human milk in small amounts. No reported adverse effects in breastfed infants. Considered compatible with breastfeeding by expert consensus, but monitor infants for hypotension, poor feeding, or irritability.

• Class: Antihypertensive / Antianginal
• Subclass: Calcium Channel Blocker (CCB) – Dihydropyridine group (3rd generation, long-acting)

• Known hypersensitivity to amlodipine, dihydropyridines, or any component of the formulation.
• Severe hypotension (systolic BP <90 mmHg)
• Cardiogenic shock
• Obstructive outflow tract stenosis (e.g., advanced aortic stenosis)
• Unstable angina (except in vasospastic angina)

• Hypotension: Risk increased in volume-depleted patients; monitor blood pressure closely.
• Worsening Angina or MI: Especially in patients with severe obstructive coronary disease upon dose initiation or up-titration.
• Hepatic Impairment: Clearance reduced; dose titration required with close monitoring.
• Heart Failure: Use with caution; may cause fluid retention, though amlodipine is generally safe in stable HF.
• Peripheral Edema: Dose-dependent; may require dose reduction or switch to alternate agent.
• Reflex Tachycardia: Rare but possible, especially in severe vasodilation.

Common (≥1%)

• Cardiovascular: Peripheral edema, palpitations, flushing
• CNS: Headache, dizziness, fatigue
• GI: Nausea, abdominal pain
• Respiratory: Dyspnea

Less Common / Rare (<1%)                                                                            

• Hepatic: Elevated liver enzymes, jaundice
• Hematologic: Leukopenia, thrombocytopenia (rare)
• Dermatologic: Rash, pruritus, angioedema
• Musculoskeletal: Myalgia, arthralgia

Note: Most side effects are dose-dependent and reversible upon dose reduction or discontinuation.

• CYP3A4 Inhibitors (e.g., ketoconazole, clarithromycin): May increase plasma levels of amlodipine; monitor for hypotension.
• Simvastatin: Amlodipine increases plasma concentration; limit simvastatin dose to 20 mg/day.
• Cyclosporine and Tacrolimus: Risk of increased blood levels; monitor concentrations.
• Grapefruit Juice: Minimal interaction, unlike other CCBs, but caution still advised.
• Alcohol or other antihypertensives: Additive hypotensive effect.

• FDA: Maintains dose restriction for simvastatin when used with amlodipine (20 mg/day max).
• NICE & ESC Guidelines: Endorse amlodipine as a first-line agent in Black patients or those >55 years with hypertension.
• KDIGO: Supports its use in post-transplant hypertension due to favorable renal hemodynamics.
• No recent black box warnings or major labeling changes.

• Temperature: Store between 20–25°C (68–77°F)
• Excursion Tolerance: Permitted between 15–30°C (59–86°F)
• Humidity/Light: Protect from excessive moisture and direct light.
• Handling: Store tablets in original container until use.