1. Pharmacology
Amlodipine Besilate is a dihydropyridine calcium channel blocker.
It inhibits the influx of calcium ions into vascular smooth muscle and cardiac muscle.
This leads to vasodilation, reduced peripheral resistance, and lowered blood pressure.
It also reduces myocardial oxygen demand, making it effective for angina pectoris.
2. Dosage & Administration
Adults
Hypertension/Angina: Starting dose is usually 5 mg once daily, can be increased to 10 mg once daily depending on patient response.
Elderly or Hepatic Impairment
Start with 2.5 mg once daily.
Children (6–17 years)
2.5 to 5 mg once daily (only for hypertension).
Route: Oral, with or without food.
3. Interaction
CYP3A4 inhibitors (e.g., ketoconazole, erythromycin): may increase amlodipine levels.
CYP3A4 inducers (e.g., rifampicin, phenytoin): may reduce efficacy.
May enhance effects of other antihypertensives.
Simvastatin: dose should not exceed 20 mg daily when co-administered.
4. Contraindications
Hypersensitivity to amlodipine or any component of the formulation.
Cardiogenic shock.
Severe aortic stenosis.
Unstable angina (except when being treated with beta-blockers).
Severe hypotension (SBP < 90 mmHg).
5. Side Effects
Common:
Edema (especially peripheral)
Fatigue
Dizziness
Palpitations
Flushing
Nausea
Less common:
Abdominal pain
Sleep disturbances
Muscle cramps
Gynecomastia (rare)
6. Pregnancy & Lactation
Pregnancy Category C
No adequate studies in pregnant women; use only if potential benefit justifies risk.
Lactation:
Unknown if excreted in breast milk; caution is advised.
7. Precautions & Warnings
Use cautiously in patients with heart failure, hepatic impairment, or severe hypotension.
Monitor BP regularly.
Avoid abrupt withdrawal in angina or coronary artery disease.
Use lower doses in elderly.
8. Overdose Effects
Symptoms: Hypotension, dizziness, reflex tachycardia.
Treatment: Supportive care, monitoring. IV fluids, vasopressors (like dopamine), and calcium infusion may be used in severe cases.
9.Therapeutic Class
Calcium Channel Blockers (Dihydropyridine group)
Antihypertensive & Antianginal Agent
10. Storage Conditions
Store below 25°C.
Protect from light and moisture.
Keep out of reach of children.
11. Chemical Structure
IUPAC Name:
3-Ethyl 5-methyl 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate
Molecular Formula:
C₂₀H₂₅ClN₂O₅
Molecular Weight:
408.88 g/mol
Structural Formula: