Verapamil 240mg pills with prolonged action pokr about. x20
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Description
Verapamil - oblong, biconvex pills of prolonged action, coated with a grayish-blue color, with a risk on one side. Verapamil is one of the main drugs of the “slow” calcium channel blocker group. It has antiarrhythmic, antianginal and antihypertensive activity.
Active ingredients
Verapamil
Release form
Pills
Composition
Verapamil hydrochloride, lactose monohydrate, microcrystalline cellulose, magnesium stearate, sodium alginate, hydroxypropyl methylcellulose.
Pharmacological effect
Verapamil is one of the main drugs of the “slow” calcium channel blocker group. It has antiarrhythmic, antianginal and antihypertensive activity. The drug reduces the oxygen demand of the myocardium by reducing myocardial contractility and reducing heart rate (HR). It causes expansion of the coronary vessels of the heart and increases coronary blood flow, reduces the tone of the smooth muscles of the peripheral arteries and the total peripheral vascular resistance. Verapamil significantly slows down the atrioventricular (AV) conduction, suppresses the automatism of the sinus node, which allows the use of the drug for the treatment of supraventricular arrhythmias. Verapamil is the drug of choice for treating angina pectoris of vasospastic genesis (Prinzmetal stenocardia). It has an effect on exertional angina, as well as in the treatment of angina pectoris with supraventricular rhythm disturbances.
Pharmacokinetics
Absorption: when taken orally, about 90-92% of verapamil is absorbed in the gastrointestinal tract, however, bioavailability is low and is approximately 20% due to intensive metabolism during the "first pass" through the liver. The concentration of verapamil in the blood plasma increases gradually. Maximum plasma concentrations are 81.34 ng / ml. Tmax averages 4.75 hours. Relatively high therapeutic plasma concentrations (51.6 ng / ml) are detected 24 hours after taking the drug by mouth. About 90% of the drug is bound to plasma proteins. Distribution: The average half-life for a single dose is 2.8 - 7.4 hours, while taking repeated doses - 4.5 -12 hours.The elimination half-life from plasma in the elderly is increasing. Verapamil penetrates the placental barrier and is found in breast milk. Metabolism: metabolized during the "first pass" through the liver. 12 metabolites detected. The main metabolite is norverapamil, which has pharmacological activity, other metabolites are mostly inactive. Excretion: about 70% of the dose of the drug is excreted in the urine, and about 16% or more excreted in the feces within five days when the drug is used orally. About 3–4% is excreted unchanged.
Indications
Arterial hypertension, Prevention of angina attacks (including Prinzmetal's angina), Prevention of supraventricular tachycardias.
Contraindications
Hypersensitivity to the components of the drug, severe bradycardia, cardiogenic shock, sinoatrial blockade, atrioventricular blockade II and III degree, sick sinus syndrome (bradycardia-tachycardia syndrome), sinoatrial blockade, pronounced arterial hypotension, wrist ward syndrome, marked cholangiopathy, tachycardia syndrome, marked stenoatrial block myocardial infarction (with symptoms of bradycardia, severe hypotension, left ventricular failure), age up to 18 years (efficacy and safety have not been established), pregnant nce and lactation.
Precautionary measures
To take the drug with caution in case of atrioventricular block I, chronic heart failure, arterial hypotension (systolic blood pressure less than 90 mm Hg), atrial fibrillation / flutter with Wolf-Parkinson-White syndrome (risk of ventricular tachycardia), impaired liver function.
Use during pregnancy and lactation
Contraindicated.
Dosage and administration
To accept during food or right after food, washing down with a small amount of water. Tablets do not chew. Doses of the drug are selected individually.
Side effects
Since the cardiovascular system: sinus bradycardia, sinoatrial block, asystolia, AV block I, II and III degree, bradyarrhythmic form of atrial fibrillation, development or increase in symptoms of heart failure, lower blood pressure, heartbeat, tachycardia.From the side of the central nervous system: rarely - dizziness, drowsiness, lethargy, headache, feeling tired, irritability, tremor, erythromelalgia or paresthesia. On the part of the digestive tract: constipation, nausea, vomiting, intestinal obstruction, pain or discomfort in the abdomen. Laboratory indicators: increased activity of liver enzymes, alkaline phosphatase, increased prolactin levels. Allergic reactions: rash, urticaria, angioedema, Stevens-Johnson syndrome. Other: flushing, peripheral edema, very rarely - myalgia and arthralgia. It was reported about cases of galactorrhea and impotence, gynecomastia, gum hyperplasia.
Overdose
A pronounced decrease in blood pressure (in some cases to levels that cannot be measured), shock, loss of consciousness, AV block I, II degree, often as Wenckebach periods with or without a sliding rhythm, complete AV block with full atrioventricular dissociation, sliding out , cardiac arrest, sinus bradycardia, sinus stop, heart failure, asystole, sinoatrial blockade. Assistance: with early detection (it must be borne in mind that the active substance is released and absorbed in the intestine within 48 hours after taking the drug inside) - gastric lavage is recommended in all cases, if at least 12 hours have passed since taking the drug, and at a later date with reduced GI motility (lack of intestinal noise during auscultation). The treatment is symptomatic and depends on the clinical picture of the overdose. Calcium is a specific antidote: 10-30 ml of 10% solution of calcium gluconate is administered as an intravenous injection (2.25 - 4.5 mmol), if necessary, re-administered or as a slow drip infusion (for example, 5 mmol / hour). In the case of atrioventricular block II or III, sinus bradycardia, cardiac arrest: atropine, isoprenaline, ortsiprenalin or stimulation of the heart. In case of arterial hypotension: dopamine, dobutamine, norepinephrine (norepinephrine). Hemodialysis is not effective.
Interaction with other drugs
With the simultaneous appointment of the drug Verapamil with carbamazepine, there is an increase in the action of the latter and the risk of toxic lesions of the nervous system increases. The prescription of verapamil to patients who receive lithium for a long time increases the risk of a neurotoxic effect of lithium drugs.Simultaneous use with rifapicin or phenobarbital, reduces the effectiveness of verapamil. Cimetidine enhances the action of verapamil. Combined use with other antihypertensive drugs, diuretics, vasodilators leads to mutual enhancement of their action. The combination with beta-blockers can lead to an increase in the negative inotropic effect, an increase in the risk of AV conduction disturbances, and bradycardia. While taking the drug Verapamil and digoxin, theophylline, cyclosporine or hiiidina, it is possible to increase the blood concentration of the above drugs during therapy with Verapamil. With lipid-lowering drugs: atorvastatin (increased serum levels of atorvastatin), lovastatin (increased serum levels of lovastatin), simvastatin (approximately 2.6 times the AUC, and a maximum concentration of approximately 4.6 times simvastatin). Patients receiving verapamil, treatment with HMG-CoA reductase inhibitors should begin with the lowest possible doses, which gradually increase. If it is necessary to prescribe verapamil to patients already receiving HMG-CoA reductase inhibitors, their dose should be reconsidered according to the concentration of cholesterol in the blood serum. Fluvastatin, pravastatin and rosuvastatin are not metabolized by the action of CYP3A4 isoenzymes, therefore their interaction with verapamil is least likely. With almotriptan, an increase in AUC by approximately 20% and a maximum concentration of almotriptan by approximately 24%. Grapefruit juice - an increase in AUC and maximum concentration of verapamil. St. John's wort - decreases the AUC of verapamil with a corresponding decrease in the maximum concentration. Doxorubicin - reduces the half-life of doxorubicin (approximately 27%) and maximum concentration (approximately 38%). In patients with advanced neoplasms, verapamil does not affect the level or clearance of doxorubicin. In patients with small cell lung cancer, verapamil reduces the half-life and the maximum concentration of doxorubicin. Hypoglycemic agents (glyburide) - an increase in the maximum concentration of glyburide (approximately 28%), AUC (approximately 26%). Aspirin (acetylsalicylic acid) - increase bleeding.