Dilacoran-Retard (Calan) 180mg 15 Tabs, Verapamil
THIS IS A BRAND MEDICATION
Treatment of angina pectoris, rhythm disorders and hypertension
ABBOTT LABORATORIES DE MEXICO, SA de CV
And dosage form:
Each tablet contains:
Verapamil hydrochloride and 80 mg 40 .........
Excipient cbp 1 tablet ......................
Verapamil hydrochloride is indicated for the treatment of coronary artery disease, including: chronic stable angina; unstable angina (angina crescendo angina at rest); vasospastic angina pectoris (Prinzmetal angina, variant angina); angina post-myocardial infarction in patients without heart failure, if not indicated blockers administration?.
It is also indicated in heart rhythm disorders such as paroxysmal supraventricular tachycardia, atrial fibrillation / atrial flutter with rapid atrioventricular conduction (except syndrome Wolf-Parkinson-White or Lown-Ganong Levine) and in the treatment of hypertension.
Pharmacokinetics in Humans:
Metabolism and Elimination: More than 90% of the administered dose of verapamil, are rapidly absorbed in the small intestine. Systemic availability average of the parent compound, after a single dose is 22% due to an extensive first-pass hepatic metabolism. Bioavailability is about 2 times higher with repeated administration. The maximum concentration in plasma is reached between the 1st and 2nd hour after administration of immediate release tablets. The elimination half-life is 3-7 hours. Approximately 90% of verapamil, binds to plasma proteins. The drug is extensively metabolized. Metabolites are generated in various human (12 have been identified). Of these metabolites have appreciable norverapamil only pharmacological effect (approximately 20% of the parent compound effect) was observed in a study in dogs.
Verapamil hydrochloride and its metabolites are primarily excreted by the kidneys. Only 3-4% of the drug excreted by the kidney is removed intact. Fifty percent of the dose is excreted through the kidneys in the first 24 hours, 70% in five days. Up to 16% of the dose is excreted in the feces. The deterioration of renal function has no effect on the pharmacokinetics of verapamil, as demonstrated in controlled trials in patients with end-stage renal failure and subjects with healthy kidneys. The elimination half-life is prolonged in patients with impaired liver function due to a reduced oral clearance and a larger volume distribution.
Pharmacodynamics Verapamil blocks the transmembrane influx of calcium into cardiac and vascular muscle cells. Directly reduces myocardial oxygen demand through metabolic processes involved in energy consumer in the cardiac muscle cells and indirectly by reducing afterload.
The calcium blocking effect on vascular smooth muscle of coronary arteries increases myocardial perfusion, even in the post-stenotic tissue relaxes coronary spasm.
The antihypertensive action of verapamil is based on reducing peripheral vascular resistance without reflex increase in heart rate. Normal blood pressure is not appreciably affected.
Verapamil hydrochloride possesses antiarrhythmic effects, particularly in the presence of supraventricular arrhythmias. Conduction slows atrioventricular node. The result, depending on the type of rhythm disorder, is the restoration of sinus rhythm and / or normalization of ventricular rate. The normal heart rate is not affected or is only slightly.
Verapamil hydrochloride is contraindicated in:
Hypersensitivity to the active substance or any of the inactive ingredients.
Acute myocardial infarction with complications.
AV block of second and third degree, except for patients with a functioning artificial pacemaker.
Sick sinus syndrome except in patients with functioning artificial pacemaker.
Congestive heart failure.
Fibrillation / atrial flutter and syndromes of Wolff-Parkinson-White, Lown-Ganong Levine).
Use with caution in the presence of:
AV block first degree.
Severely impaired liver function.
Effects on ability to use machines Depending on individual response, verapamil may affect the ability to react to the point of impairing the ability to drive a car, operate machinery or work under dangerous conditions. This applies mainly to the following conditions: at baseline, with increasing dose, changing other therapy and when used with alcohol.
Use in Pregnancy and Lactation:
There are no adequate data from the use of verapamil hydrochloride in pregnant women. Verapamil hydrochloride should be used during pregnancy only if clearly needed.
Verapamil crosses the placenta and has been measured in the blood of the umbilical cord.
Verapamil hydrochloride is excreted in human milk. It should stop breastfeeding during treatment with verapamil.