Amlodipine


Description

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 calci...

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Pharmacology

Indication

Amlodipine may be used alone or in combination with other antihypertensive and antianginal agents fo... Read more

Pharmacodynamic

**General pharmacodynamic effects**

Amlodipine has a strong affinity for cell membranes, modulati...
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Mechanismofaction

**Mechanism of action on blood pressure**

Amlodipine is considered a peripheral arterial vasodila...
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Absorption

Amlodipine absorbed slowly and almost completely from the gastrointestinal tract. Peak plasma concen... Read more

Proteinbinding

About 98% [ Read more

Volumeofdistribution

21 L/kg [ 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... Read more

Halflife

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

Plasma elimination half-life...
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Routeofelimination

Elimination from the plasma occurs in a biphasic with a terminal elimination half-life of about 30–5... Read more

Toxicity

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

**Overdose**

An overdose of amlodipi...
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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 natural licorice.
    • Grapefruit down regulates post-translational expression of CYP3A4, the major metabolizing enzyme of amlodipine. Grapefruit, in all forms (e.g. whole fruit, juice and rind), can significantly increase serum levels of amlodipine and may cause toxicity. Avoid grapefruit products while on this medication.
    • Take without regard to meals.

    Interactions

    Type in a drug name to check for interaction with Amlodipine

    The metabolism of (R)-warfarin can be decreased when combined with Amlodipine.
    The metabolism of (S)-Warfarin can be decreased when combined with Amlodipine.
    1-benzylimidazole may decrease the antihypertensive activities of Amlodipine.
    The risk or severity of hypoglycemia can be increased when Amlodipine is combined with 2,4-thiazolidinedione.
    2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Amlodipine.
    2,5-Dimethoxy-4-ethylthioamphetamine may decrease the antihypertensive activities of Amlodipine.
    The metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Amlodipine.
    4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Amlodipine.
    The metabolism of 4-hydroxycoumarin can be decreased when combined with Amlodipine.
    4-Methoxyamphetamine may decrease the antihypertensive activities of Amlodipine.
    The metabolism of 5-androstenedione can be decreased when combined with Amlodipine.
    5-methoxy-N,N-dimethyltryptamine may decrease the antihypertensive activities of Amlodipine.
    The metabolism of Amlodipine can be decreased when combined with 6-Deoxyerythronolide B.
    The metabolism of 6-O-benzylguanine can be decreased when combined with Amlodipine.
    The metabolism of Amlodipine can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
    7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypotensive activities of Amlodipine.
    The metabolism of 9-aminocamptothecin can be decreased when combined with Amlodipine.
    The therapeutic efficacy of Abafungin can be increased when used in combination with Amlodipine.
    The metabolism of Amlodipine can be increased when combined with Abatacept.
    Abediterol may decrease the antihypertensive activities of Amlodipine.

    References

    • 1 . Nayler WG, Gu XH: The unique binding properties of amlodipine: a long-acting calcium antagonist. J Hum Hypertens. 1991 Aug;5 Suppl 1:55-9. [PubMed: 1834847]
    • 2 . van Zwieten PA: Amlodipine: an overview of its pharmacodynamic and pharmacokinetic properties. Clin Cardiol. 1994 Sep;17(9 Suppl 3):III3-6. [PubMed: 9156957]
    • 3 . Fares H, DiNicolantonio JJ, O'Keefe JH, Lavie CJ: Amlodipine in hypertension: a first-line agent with efficacy for improving blood pressure and patient outcomes. Open Heart. 2016 Sep 28;3(2):e000473. doi: 10.1136/openhrt-2016-000473. eCollection 2016. [PubMed: 27752334]
    • 4 . Flynn JT, Nahata MC, Mahan JD Jr, Portman RJ: Population pharmacokinetics of amlodipine in hypertensive children and adolescents. J Clin Pharmacol. 2006 Aug;46(8):905-16. doi: 10.1177/0091270006289844. [PubMed: 16855075]
    • 5 . Meredith PA, Elliott HL: Clinical pharmacokinetics of amlodipine. Clin Pharmacokinet. 1992 Jan;22(1):22-31. doi: 10.2165/00003088-199222010-00003. [PubMed: 1532771]
    • 6 . Faulkner JK, McGibney D, Chasseaud LF, Perry JL, Taylor IW: The pharmacokinetics of amlodipine in healthy volunteers after single intravenous and oral doses and after 14 repeated oral doses given once daily. Br J Clin Pharmacol. 1986 Jul;22(1):21-5. [PubMed: 2943308]
    • 7 . Apo amlodipine tablets, MedSafe NZ [File]

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