Amlodipine

Amlodipine
ATC Code C08CA01
Formula C20H25ClN2O5
Molar Mass (g·mol−1) 408,88
Physical State solid
Melting Point (°C) 134–136
PKS Value 9.4
CAS Number 88150-42-9
PUB Number 2162
Drugbank ID DB00381
Solubility low in water

Basics

Amlodipine is an antihypertensive drug belonging to the group of calcium channel blockers of the nifedipine type. It is used to treat essential hypertension and to prevent and treat angina pectoris symptoms. Because of its high selectivity for peripheral blood vessels, amlodipine has a lower risk of disturbances in cardiac activity and conduction of excitation.

Amlodipine is available by prescription and often as a combination preparation with other antihypertensives in tablet form.

Pharmacology

Pharmacodynamics

Amlodipine has high selectivity and affinity for calium channels in the periphery. Thus, it mainly affects the smooth muscle of blood vessels. There it binds to calcium channels and blocks them. As a result, calcium ions can no longer flow in and a contraction is prevented, because calcium is essential for the transmission of stimuli and the subsequent contraction of the muscle fibers. The block causes the blood vessels to dilate, resulting in a reduction in blood pressure.

Pharmacokinetics

Amlodipine is absorbed very slowly but almost entirely in the gastrointestinal tract. Because of the slow absorption, peak concentrations in blood plasma are reached only after 6-12 hours. The bioavailability of amlodipine is between 64-90%. Plasma protein binding is about 94% and the plasma half-life is very high at about 30-50 hours. This high half-life makes amlodipine particularly attractive as a drug, as it means it only needs to be taken once a day. A major part of the dose is broken down by the liver and subsequently excreted in the urine.

Drug interactions

Amlodipine should not be taken together with drugs which inhibit enzymes of CYP 450 family. Furthermore it should not be taken concomitantly with diltiazem and clarithromycin.

Amolidpine itself may increase the plasma concentrations of simvastatin, tacrolimus and cylcosporine. Therefore, they should not be taken together.

Toxicity

Overdose may result in severe peripheral vasodilation with severely lowered blood pressure and reflex tachycardia. Prolonged hypotension may cause shock and in the worst case may be fatal.

There is no evidence that amlodipine is carcinogenic or mutagenic.

There are no studies showing that amlodipine is not harmful to fertility. Therefore, the drug should only be taken during pregnancy if the benefit outweighs the possible risk.

Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter ist Autor zu pharmazeutischen Themen in der Medizin-Redaktion von Medikamio. Er befindet sich im letzten Semester seines Pharmaziestudiums an der Universität Wien und liebt das wissenschaftliche Arbeiten im Bereich der Naturwissenschaften.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer ist seit 2020 freie Autorin bei Medikamio und studierte Pharmazie an der Universität Wien. Sie arbeitet als Apothekerin in Wien und ihre Leidenschaft sind pflanzliche Arzneimittel und deren Wirkung.

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