A calcium channel blocker of the dihydropyridine type.
It is regarded as specific to the L-type calcium channel blocker, they also possess nonspecific activity towards other voltage-dependent calcium channels.
L-type calcium blocker that can reduce chronic lung disease hypoxic pulmonary vasoconstriction by more than 50%.
Nifedipine, is used to manage angina, high blood pressure, Raynaud’s phenomenon, premature labor, and Prinzmetal angina.
Brand name Adalat and Procardia.
It may be used to treat severe hypertension in pregnancy.
Its use in preterm labor may allow more time for steroids to improve the baby’s lung function and provide time for transfer of the mother to a well qualified medical facility before delivery.
Nifedipine is taken by mouth.
It comes in fast and slow release formulations.
Pregnancy category US: C (Risk not ruled out).
Routes of administration by mouth, topical.
Bioavailability 45-56%
Protein binding 92-98%
Metabolism Gastrointestinal, Liver
Elimination half-life 2 hours
Excretion Kidneys: >50%, Biliary: 5-15%
Common side effects include lightheadedness, headache, feeling tired, leg swelling, cough, and shortness of breath.
Serious side effects include: hypotension and heart failure.
Use in pregnancy is safe
It is not recommended during breastfeeding
Its approved uses are for the long-term treatment of hypertension and angina pectoris.
While hypertension guidelines generally favor diuretics and ACE inhibitors, calcium channel antagonists, along with thiazide diuretics, are still favored as primary treatment for patients over 55 and black patients patients
Nifedipine has been used frequently as a tocolytic, an agent that delays premature labor, but a Cochrane review has concluded that it few benefits over placebo or no treatment for prolongation of pregnancy.
Raynaud’s phenomenon treated with nifedipine shows modest benefit of 33% decrease in attack severity, and a reduction in absolute number of attacks per week.
Topical nifedipine has been shown is as effective as topical nitrates for anal fissures.
Can also be used in high-altitude medicine to treat high altitude pulmonary edema.
Other uses include: spasms of the esophagus such as from cancer or tetanus.
Can be used in the treatment of renal calculi.
Nifedipine use may bae associated with dizziness or fainting after taking the first few doses.
Tachycardia may occur as a reaction to this drug.
Consuming anything containing grapefruit or grapefruit juice, raises blood nifedipine levels, perhaps by
inhibition of CYP3A4-mediated metabolism.
Acute overdosage associated adverse effects include: lethargy, bradycardia, marked hypotension and loss of consciousness.
The drug may be quantified in blood or plasma to confirm a diagnosis of poisoning.
It may act as an antagonist of the mineralocorticoid receptor, or as an antimineralocorticoid.
A meta-analysis demonstrated harm mainly in short-acting forms, and high dose nifedipine could cause large fluctuations in blood pressure.