Amlodipine Besylate

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Therapeutic Class

  • Calcium Channel Blocker
  • Cardiovascular Agent
  • Dihydropyridine

Mechanism of Action
Amlodipine besylate is a long-acting dihydropyridine calcium channel blocker that exerts its effect by blocking the transmembrane influx of calcium ions into cardiac and vascular smooth muscles. It also reduces peripheral vascular resistance and lowers blood pressure by causing a direct vasodilation in the peripheral arteries of the vascular smooth muscle. Its therapeutic effect on vasospastic angina is through inhibition of coronary spasm .

Pharmacokinetics
about 30 h to 50 h
Hepatic
Oral: time to peak concentration, 6 h to 12 h
Protein binding: approximately 93%
Renal: 60% as metabolites, 10% unchanged
Bioavailability: 64% to 90%
Impaired hepatic function: 56 h
Effect of food: bioavailability not altered

Patient Advice

  • Patient should avoid activities requiring coordination until drug effects are realized, as drug may cause dizziness.
  • This drug may cause palpitations, peripheral edema, fatigue, skin-flushing, angina, or myocardial infarction.
  • Instruct patient to report signs/symptoms of hypotension or exacerbation of angina with initial dosing and dose changes.
  • Advise patient against sudden discontinuation of drug.
  • Patient should not drink alcohol while taking drug.

Dosing - Adult

  • Hypertension: initial, 5 mg ORALLY once daily; maintenance 5-10 mg ORALLY once daily
  • Stable angina: 5-10 mg ORALLY once daily
  • Variant angina: 5 to 10 mg ORALLY once daily

Dosing - Dose Adjustment

  • liver disease and hypertension: starting dose 2.5 mg once daily
  • elderly, fragile, or small: for hypertension, or when adding to other antihypertensive therapy starting dose 2.5 mg once daily

Warnings - Precautions

  • aortic stenosis
  • CHF
  • exacerbation of angina during initiation of therapy, after dose increases, or withdrawal of beta blocker therapy
  • hypotension (initially or after dose increases)
  • liver impairment
  • persistent progressive dermatologic reactions

Adverse Effects - Common

  • Cardiovascular: Palpitations, Peripheral edema
  • Dermatologic: Flushing
  • Neurologic: Dizziness, Headache
  • Other: Fatigue

Adverse Effects - Serious
Cardiovascular: Angina, Cardiac dysrhythmia (rare), Myocardial infarction

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