Understanding The Pharmacology Of Nifedipine

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Nifedipine is an anti-hypertensive medication belonging to the class of dihydropyridine calcium channel blockers.
It primarily acts on vascular smooth muscle cells to cause vasodilation.
Major indications of nifedipine include the following.
In the treatment of hypertension and hypertensive emergencies.
Angina pectoris.
For Raynaud’s phenomenon to reduce vasospasm in peripheral arteries.
And as a tocolytic agent in preterm labor to inhibit uterine contractions.
Nifedipine works by blocking L-type calcium channels in vascular smooth muscle cells, which causes arterial vasodilation.
This in turn reduces systemic vascular resistance and thereby the blood pressure.
In addition, nifedipine action causes reduced myocardial oxygen demand, which benefits angina patients.
Unlike non-dihydropyridine calcium channel blockers such as verapamil and diltiazem, nifedipine has minimal direct effect on cardiac conduction.
Nifedipine is taken orally.
Both immediate release and extended-release tablets are available.
Sublingual and intravenous routes are less commonly used.
Nifedipine is well absorbed into the body with an oral bioavailability of 45 to 75%.
Once in blood, it is highly plasma protein bound.
The drug is extensively metabolized in the liver by CYP3A4 enzyme.
It is mainly excreted as metabolites in the urine.
Major adverse effects of nifedipine include the following.
Cardiovascular effects such as hypotension, reflex tachycardia, especially with immediate release formulations, and peripheral edema due to capillary leakage and vasodilation.
Neurological effects such as Dizziness, headache, and flushing.
And gastrointestinal effects such as nausea and constipation.
Absolute contraindications for nifedipine therapy include the following.
Severe hypotension, where systolic blood pressure is less than 90 millimeters of mercury.
Cardiogenic shock.
And acute myocardial infarction.
Relative contraindications include Heart failure with reduced ejection fraction.
Severe aortic stenosis, as vasodilation can cause severe hypotension.
And hepatic impairment, which may prolong drug action.

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