Product Name: Nifedipine
Generic Name: Nifedipine
Common Brands: Adalat, Nicardia, Procardia
Pharmaceutical Categories: Cardio, Blood Pressure, Cholesterol
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Here is an additional general information about this medication active ingredient nifedipine:
Nifedipine is aSelective calcium channel blocker class II, a derivative of dihydropyridine. This medication inhibits the entry of calcium into cardiomyocytes and vascular smooth muscle cells. Nifedipine has antianginal and hypotensive action. This drug lowers the tone of vascular smooth muscle. Nifedipine dilates coronary and peripheral arteries, lowers blood pressure and slightly - myocardial contractility, reduces afterload and myocardial oxygen demand. This medicine improves coronary blood flow. Nifedipine practically does not possess antiarrhythmic activity, it does not inhibit the conductance of myocardium.
When administered orally Nifedipine is rapidly absorbed from the gastrointestinal tract. This drug undergoes metabolism in the "first pass" through the liver. The protein binding is 92-98%. Nifedipine metabolized in the liver to form inactive metabolites. T1/2 is about 2 hours. This medication excreted mainly by the kidneys as metabolites in trace amounts in unchanged form; 20% is excreted from the gut in the form of metabolites.
Why is Nifedipine prescribed?
Prevention of angina attacks (including vasospastic angina), in some cases - relief of angina attacks, hypertension, hypertensive crises, Raynaud's disease.
Dosage and administration
The dosing regimen is individual. For oral administration the initial dose is 10 mg 3-4 times / day. If necessary the dose gradually increased up to 20 mg 3-4 times / day. In some cases (variant angina, severe hypertension) for a short time the dose can be increased to 30 mg 3-4 times / day. For relief of hypertensive crisis, as well as angina attack this drug can be used sublingually in 10-20 mg (rarely 30 mg).
To IN relieve an angina attack or hypertensive crisis - 5 mg for 4-8 hours.
Intracoronary dose for relief of acute coronary artery spasm injected bolus is 100-200 mcg. With stenosis of major coronary vessels starting dose is 50-100 micrograms.
The maximum daily dose: oral - 120 mg, IV - 30 mg.
Nifedipine side effects, adverse reactions
Cardiovascular: flushing of the skin, a feeling of warmth, tachycardia, hypotension, peripheral edema; rarely - bradycardia, ventricular tachycardia, asystole, increased angina attacks.
Digestive system: nausea, heartburn, diarrhea, rarely - liver function impairment and in rare cases - gingival hyperplasia. The chronic administration in high doses may cause dyspeptic symptoms, elevated liver enzymes, intrahepatic cholestasis.
CNS and peripheral nervous system: headache. The chronic administration in high doses may cause paresthesia, muscle pain, tremors, visual disturbances light, and sleep disorders.
Hemopoietic system: in rare cases - leukopenia, thrombocytopenia.
Urinary system: an increase in daily diuresis. The chronic administration in high doses may cause renal dysfunction.
Endocrine system: in rare cases - gynecomastia.
Allergic reactions: skin rash.
Local reactions: for IV injections might burning at the injection site.
Within 1 min after intracoronary administration it can be a result in the negative inotropic action of nifedipine, the increase in heart rate, hypotension, and these symptoms gradually disappear within 5-15 minutes.
Hypotension (systolic blood pressure below 90 mm Hg), collapse, cardiogenic shock, severe heart failure, severe aortic stenosis; increased sensitivity to nifedipine.
Using during pregnancy and breastfeeding
Adequate and well-controlled studies safety of nifedipine in pregnancy was not been conducted. The use of Nifedipine in pregnancy is not recommended.
Because nifedipine is excreted in breast milk, you should avoid its use during lactation or to stop breastfeeding during the treatment with this medication.
In experimental studies it have been revealed embryotoxic, fetotoxic and teratogenic effects of nifedipine.
Category effects on the fetus by FDA - C.
In patients with stable angina at the beginning of treatment paradoxical enhancement anginalnyh pain may occurs, with pronounced coronary sclerosis and unstable angina - the aggravation of myocardial ischemia. Not recommended to use short-acting drugs for long-term treatment of angina or hypertension, because it is possible the development of unpredictable changes in BP and reflex angina.
Nifedipine drug interactions
Nitrates, beta-blockers, diuretics, tricyclic antidepressants, fentanyl, alcohol increase the hypotensive effect of Nifedipine. This medication increases the activity of theophylline reduces the renal clearance of digoxin. Nifedipine increases the side effects of vincristine (reduced elimination); increases the bioavailability of cephalosporins (cefixime). Cimetidine and ranitidine increase the level of this drug in plasma. Diltiazem slows the metabolism (requires dose reduction of nifedipine) of Nifedipine. This medicine is incompatible with rifampicin (accelerates biotransformation and does not allow to create effective concentration). Grapefruit juice (large quantity) increases its bioavailability.
Nifedipine in case of emergency / overdose
Symptoms: sudden bradycardia, bradyarrhythmia, hypotension, in severe cases - collapse, slowing conduction. When you receive a large number of retard-tablets symptoms of intoxication occur no earlier than 3-4 h and may additionally be expressed in loss of consciousness up to coma, cardiogenic shock, convulsions, hyperglycemia, metabolic acidosis, hypoxia.
Treatment: gastric lavage, activated charcoal method, injections of norepinephrine, calcium chloride or calcium gluconate in a solution of atropine (IV). Hemodialysis is ineffective.