Pharmaceutical Intermediate Verapamil Powder Verapamil hydrochloride
Product Description
Product Details
| Product Name |
Verapamil |
| CAS No. |
23313-68-0 |
| Appearance and shape |
White Powder |
| MF |
C27H39ClN2O4 |
| MW |
491.06 |
Verapamil Hydrochloride, Verapamil Hydrochloride, molecular weight 491.06, CAS No. 152-11-4, prepared from guaiacol. It is mainly used for paroxysmal supraventricular tachycardia, but also for angina pectoris, hypertension and hypertrophic infarct cardiomyopathy.
Application&Function
Pharmacological action
Verapamil blocks calcium ions from entering the cell through the heart and blood vessel muscle membranes. It directly reduces the oxygen requirement of the myocardium by intervening in the metabolic process of energy consumption in the cardiomyocytes, and indirectly reduces the afterload. Verapamil increases calcium blockade of coronary vascular smooth muscle tissue even after stenosis, and also alleviates coronary artery decay
The mechanism of verapamil's antihypertensive effect is to reduce peripheral vascular resistance without causing a rebound heart rate increase of 6 - generally not affecting normal blood pressure.
Verapamil has good antiarrhythmic effect, especially for supraventricular arrhythmias. It slows conduction of the AV node. Depending on the type of arrhythmia, verapamil can restore sinus rhythm and/or normalize ventricular rate. Verapamil had no effect on normal heart rate or caused only a slight decrease in heart rate.
pharmacokinetics
More than 90% of verapamil is absorbed by oral administration. There is a first-pass effect through the portal vein. The bioavailability is only 20% to 35%. The binding rate of hemagglutinin was about 90%. The peak concentration is reached within 1~2 hours after a single dose is taken orally, and the effect lasts for 6~8 hours. The average half-life is 2.8-4.4 hours, which may be prolonged in incremental periods. Long-term oral administration (at least 30% dosing at 6-hour intervals) increases the half-life to 4.5-12.0 hours. The clearance half-life of elderly patients may be prolonged.
Verapamil is mostly metabolized in the liver after oral administration in healthy people. 13 metabolites were detected in urine. With the exception of meverapamil, all metabolites are trace amounts. The cardiovascular activity of norverapamil is that verapamil can achieve stable blood concentrations that are essentially the same as verapamil. Verapamil and its metabolites are mainly excreted through the kidney pathway, of which 3-4% is the original drug, and about 16% of the drug is excreted through the stool. After taking verapamil orally, 50% of the drug will be eliminated from the body within 24 hours and approximately 70% within 5 days. Studies on patients with end-stage renal failure and normal renal function showed that renal dysfunction did not affect the metabolism of verapamil; In patients with cirrhosis, the drug clearance half-life is prolonged (14-16 hours) due to decreased oral clearance (to 30% of normal) and increased drug distribution volume.
Specification
About US
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