Description

Simple

A heart medication used to treat high blood pressure and chest pain caused by heart disease.

Clinical

A calcium channel blocker used to treat hypertension and angina.

Overview

Amlodipine, initially approved by the FDA in 1987, is a popular antihypertensive drug belonging to the group of drugs called _dihydropyridine calcium channel blockers_. Due to their selectivity for the peripheral blood vessels, dihydropyridine calcium channel blockers are associated with a lower incidence of myocardial depression and cardiac conduction abnormalities than other calcium channel blockers [5].

Amlodipine is commonly used in the treatment of high blood pressure and angina. Amlodipine has antioxidant properties and an ability to enhance the production of nitric oxide (NO), an important vasodilator that decreases blood pressure [3]. The option for single daily dosing of amlodipine is an attractive feature of this drug [FDA label].

Pharmacology

Indication

Amlodipine may be used alone or in combination with other antihypertensive and antianginal agents for the treatment of the following conditions [FDA label]:

• Hypertension

• Coronary artery disease

• Chronic stable angina

• Vasospastic angina (Prinzmetal’s or Variant angina)

• Angio... Read more

Pharmacodynamic

**General pharmacodynamic effects**

Amlodipine has a strong affinity for cell membranes, modulating calcium influx by inhibiting selected membrane calcium channels. This drug's unique binding properties allow for its long-acting action and less frequent dosing regimen [ Read more

Mechanism of action

**Mechanism of action on blood pressure**

Amlodipine is considered a peripheral arterial vasodilator that exerts its action directly on vascular smooth muscle to lead to a reduction in peripheral vascular resistance, causing a decrease in blood pressure. Amlodipine is a dihydropyridine calcium an... Read more

Absorption

Amlodipine absorbed slowly and almost completely from the gastrointestinal tract. Peak plasma concentrations are achieved 6-12 hours after oral administration. The estimated bioavailability of amlodipine is 64-90%. Steady-state plasma amlodipine levels are achieved after 7-8 days of consecutive dail... Read more

Protein binding

About 98% [5], [ Read more

Volume of distribution

21 L/kg [5], [ Read more

Clearance

Total body clearance (CL) has been calculated as 7 ± 1.3 ml/min/kg (0.42 ± 0.078 L/ h/kg) in healthy volunteers [ Read more

Half life

The terminal elimination half-life of about 30–50 hours [FDA label].

Plasma elimination half-life is 56 hours in patients with impaired hepatic function, titrate slowly when administering this drug to patients with severe hepatic impairment [FDA label].

Route of elimination

Elimination from the plasma occurs in a biphasic with a terminal elimination half-life of about 30–50 hours. Steady-state plasma levels of amlodipine are reached after 7-8 days of consecutive daily dosing [FDA label]. Amlodipine is 10% excreted as unchanged drug in the urine. Amlodipine can be init... Read more

Toxicity

**Acute oral toxicity (LD50)**: 37 mg/kg (mouse) [MSDS].

**Overdose**

An overdose of amlodipine could result in a high degree of peripheral vasodilatation with a possibility of reflex tachycardia. Significant and prolonged hypotension leading to shock and fatal outcomes have been reported [FD... Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Edema US
  • Kind: experimental
    • Percent: 1.8-10.8%
  • Kind: placebo
    • Percent: 0.6%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 7.3
  • Clinical Trial
    Palpitation US
  • Kind: experimental
    • Percent: 0.7-4.5%
  • Kind: placebo
    • Percent: 0.6%
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 4.5%
  • Kind: placebo
    • Percent: 2.8%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 1.1-3.4%
  • Kind: placebo
    • Percent: 1.1%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 2.9%
  • Kind: placebo
    • Percent: 1.9%
  • Clinical Trial
    Flushing US
  • Kind: experimental
    • Percent: 0.7-2.6%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: 1.6%
  • Kind: placebo
    • Percent: 0.3%
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 1.4%
  • Kind: placebo
    • Percent: 0.6%
  • Clinical Trial
    Arrhythmia US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Chest Pain US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Hypotension US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Bradycardia US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Malaise US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Pain US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Asthenia US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Back Pain US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Hot Flushes US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Sexual Dysfunction US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Insomnia US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Nervousness US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Rigors US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Weight Gain US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Weight decrease US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Depersonalization US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Anxiety US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Dyspnea US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Depression US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Abnormal dreams US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Pruritus US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Rash US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Epistaxis US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Erythema multiforme US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Angioedema US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Postural Hypotension US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Tachycardia US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Postural dizziness US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Syncope US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Peripheral ischemia US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Tremor US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Paresthesia US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Hypoesthesia US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Peripheral neuropathy US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Vasculitis US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Diarrhea US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Dysphagia US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Dyspepsia US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Constipation US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Anorexia US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports
    Vertigo US
  • Kind: experimental
    • Percent: 0.1-1%
  • Varying Reports

    Contraindications

    • Regions: US
    • Patient Conditions:
        • Name: Known sensitivity to amlodipine
        • Drugbank Id: DBCOND0117818

    Food Interactions

    Avoid grapefruit products.

    Avoid natural licorice.

    Take with or without food. The absorption is unaffected by food.