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

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

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The metabolism of (R)-warfarin can be decreased when combined with Amlodipine.
(S)-Warfarin
The metabolism of (S)-Warfarin can be decreased when combined with Amlodipine.
1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid
1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid may decrease the antihypertensive activities of Amlodipine.
1-benzylimidazole
1-benzylimidazole may decrease the antihypertensive activities of Amlodipine.
2,4-thiazolidinedione
The risk or severity of hypoglycemia can be increased when Amlodipine is combined with 2,4-thiazolidinedione.
2,5-Dimethoxy-4-ethylamphetamine
2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Amlodipine.
2,5-Dimethoxy-4-ethylthioamphetamine
2,5-Dimethoxy-4-ethylthioamphetamine may decrease the antihypertensive activities of Amlodipine.
4-Bromo-2,5-dimethoxyamphetamine
4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Amlodipine.
4-Methoxyamphetamine
4-Methoxyamphetamine may decrease the antihypertensive activities of Amlodipine.
5-methoxy-N,N-dimethyltryptamine
5-methoxy-N,N-dimethyltryptamine may decrease the antihypertensive activities of Amlodipine.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypotensive activities of Amlodipine.
Abafungin
The therapeutic efficacy of Abafungin can be increased when used in combination with Amlodipine.
Abatacept
The metabolism of Amlodipine can be increased when combined with Abatacept.
Abediterol
Abediterol may decrease the antihypertensive activities of Amlodipine.
Abemaciclib
The serum concentration of Abemaciclib can be increased when it is combined with Amlodipine.
Abexinostat
The risk or severity of QTc prolongation can be increased when Amlodipine is combined with Abexinostat.
Acalabrutinib
The metabolism of Amlodipine can be decreased when combined with Acalabrutinib.
Acarbose
The risk or severity of hypoglycemia can be increased when Amlodipine is combined with Acarbose.
Acebutolol
The risk or severity of QTc prolongation can be increased when Amlodipine is combined with Acebutolol.
Aceclofenac
The therapeutic efficacy of Amlodipine can be decreased when used in combination with Aceclofenac.
9 References
  1. 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. 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. 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. 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. 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. 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. 7 . FDA Approved Drug Products: Amlodipine Oral Tablets Link
  8. 8 . FDA Approved Drug Products: Amlodipine Oral Suspension Link
  9. 9 . Apo amlodipine tablets, MedSafe NZ File