Verapamil
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Clinical Pharmacology
Verapamil is a selective class I calcium channel blocker. The main pharmacological properties of the drug are due to its ability to prevent the entry of calcium ions into the cardiomyocytes and smooth muscle cells of the vascular wall through the slow calcium channel of the membrane. Verapamil has antiarrhythmic, antianginal and hypotensive activity. Reduces myocardial oxygen demand by reducing myocardial contractility and heart rate reduction. Causes expansion of the coronary arteries and an increase in coronary blood flow. The antihypertensive effect of verapamil is associated with a decrease in the tone of the smooth muscles of the peripheral arteries and with the ability to reduce the round fist. Slowing down AV conduction, Verapamil has an antiarrhythmic effect in supraventricular arrhythmias; normal heart rate remains unchanged or decreases slightly.
Verapamil also has some natriuretic and diuretic effects by reducing tubular reabsorption.
Indications
- prevention of angina attacks (including Prinzmetal stenocardia);
- treatment and prevention of supraventricular arrhythmias (paroxysmal supraventricular tachycardia, atrial fibrillation, atrial flutter, extrasystole);
- arterial hypertension.
Composition
1 tablet contains 40 mg of verapamil.
Verapamil is marketed under different brands and generic names, and comes in different dosage forms:
Brand name | Manufacturer | Country | Dosage form |
---|---|---|---|
Verapamil | Alkaloid | Macedonia | pills |
Isoptin SR 240 | Abbott | USA | pills |
Verapamil | AVVA RUS | Russia | pills |
Verapamil | Ozon | Russia | pills |
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Dosage and Administration
Dosage regimen is individual. Inside adults - in the initial dose of 40-80 mg 3 times / day. For dosage forms of prolonged action, the single dose should be increased, and the frequency of administration should be reduced. Children aged 6-14 years - 80-360 mg / day, up to 6 years - 40-60 mg / day; reception frequency - 3-4 times / day. If necessary, verapamil can be administered intravenously (slowly, under the control of blood pressure, heart rate, and ECG). A single dose for adults is 5-10 mg, in the absence of effect after 20 minutes it is possible to re-enter in the same dose. A single dose for children aged 6-14 years is 2.5-3.5 mg, 1-5 years - 2-3 mg, up to 1 year - 0.75-2 mg. For patients with severely impaired liver function, the daily dose of verapamil should not exceed 120 mg. The maximum dose: adults with oral administration - 480 mg / day.
Adverse reactions
Since the cardiovascular system: bradycardia (less than 50 beats / min), a pronounced decrease in blood pressure, the development or aggravation of heart failure, tachycardia; rarely - angina, up to the development of myocardial infarction (especially in patients with severe obstructive damage to the coronary arteries), arrhythmia (including flicker and ventricular flutter); with rapid i.v. administration - AV-blockade of the III degree, asystole, collapse.
CNS and peripheral nervous system: dizziness, headache, fainting, anxiety, lethargy, increased fatigue, asthenia, drowsiness, depression, extrapyramidal disorders (ataxia, mask-like face, shuffling gait, stiffness of arms or legs, trembling hands and fingers, difficulty swallowing).
On the part of the digestive system: nausea, constipation (rarely - diarrhea), gingival hyperplasia (bleeding, soreness, swelling), increased appetite, increased activity of hepatic transaminases and alkaline phosphatase.
Allergic reactions: pruritus, skin rash, flushing of the skin of the face, erythema multiforme exudative (including Stevens-Johnson syndrome).
Others: weight gain, very rarely - agranulocytosis, gynecomastia, hyperprolactinemia, galactorrhea, arthritis, transient vision loss on the background of Cmax, pulmonary edema, thrombocytopenia asymptomatic, peripheral edema.
Contraindications
Severe arterial hypotension, AV block II and III degree, sinoatrial block and SSS (except for patients with a pacemaker), WPW-syndrome or Launa-Gannga-Levin syndrome in combination with atrial flutter or atrial fibrillation (except for patients with a pacemaker), pregnancy, age lactation, hypersensitivity to verapamil.
Drug interactions
Increases plasma levels of digoxin, cyclosporine, theophylline, carbamazepine, decreases - lithium. Reduces the antibacterial activity of rifampicin, depriving effect of phenobarbital, reduces the clearance of metoprolol and propranolol, enhances the action of muscle relaxants. Rifampicin, sulfinpirazon, phenobarbital, calcium salts, vitamin D - weaken the effect. Antihypertensive drugs (diuretics, vasodilators), tricyclic and tetracyclic antidepressants and antipsychotics: antianginal - nitrates. Beta-blockers, IA class antiarrhythmics, cardiac glycosides, inhalation anesthetics, radiopaque substances potentiate (mutually) the inhibitory effect on the sinoatrial node automatism, AV conductivity and myocardial contractility. With simultaneous use of verapamil with acetylsalicylic acid - increased bleeding. Cimetidine increases plasma content of verapamil.
Pregnancy and Lactation
The use of verapamil during pregnancy is possible only when the expected benefit to the mother outweighs the potential risk to the fetus. Category of action on the fetus by the FDA - C. At the time of treatment should stop breastfeeding (verapamil is excreted in breast milk).
Special instructions
With caution prescribed to patients with hypertrophic cardiomyopathy, complicated by left ventricular obstruction, high wedging pressure in the pulmonary capillaries, paroxysmal nocturnal dyspnea or orthopnea, impaired function of the sinus node. When prescribing to patients with severe liver dysfunction and neuromuscular transmission (Duchenne myopathy), constant medical monitoring and, possibly, dose reduction are necessary.
Overdosage
Symptoms: arterial hypotension, bradycardia, AV blockade, cardiogenic shock, coma, asystole.
Treatment: calcium gluconate is used as a specific antidote (10–20 ml of a 10% solution IV); for bradycardia and AV block, atropine, isoprenaline or ortsiprenalin are administered; hypotension - plasma solutions, dopamine, norepinephrine; with signs of heart failure - dobutamine.
- Brand name: Verapamil
- Active ingredient: Verapamil
- Dosage form: Pills.
- Manufacturer: Alkaloid
- Country of Origin: Macedonia
Studies and clinical trials of Verapamil (Click to expand)
- Resistance to the chemosensitizer verapamil in a multi-drug-resistant (MDR) human multiple myeloma cell line
- Verapamil inhibits tumor protease production, local invasion and metastasis development in murine carcinoma cells
- Treatment of no-reflow in degenerated saphenous vein graft interventions: Comparison of intracoronary verapamil and nitroglycerin
- Verapamil inhibition of enzymatic product efflux leads to improved detection of β-galactosidase activity in lacZ-transfected cells
- The calcium channel blocker verapamil in hypokalemic periodic paralysis
- Phosphatidic acid induces calcium influx in neutrophils via verapamil-sensitive calcium channels
- Comparison of protection by propranolol, bepridil, verapamil, and captopril on depleting ATP, ADP, and AMP in heart, brain, and liver by anoxia plus isoprenaline
- ENANTIOSELECTIVE DISTRIBUTION OF VERAPAMIL AND NORVERAPAMIL INTO HUMAN AND RAT ERYTHROCYTES: THE ROLE OF PLASMA PROTEIN BINDING
- PHARMACOKINETICS OF THE ENANTIOMERS OF VERAPAMIL AFTER INTRAVENOUS AND ORAL ADMINISTRATION OF RACEMIC VERAPAMIL IN A RAT MODEL
- Concurrent treatment with verapamil suppresses immune and behavioural response to endogenous cannabinoid anandamide
- NMDA Receptor-blocker Ketamine Protects During Acute Carbon Monoxide Poisoning, While Calcium Channel-blocker Verapamil Does Not
- Enantioselective binding of propranolol, disopyramide, and verapamil to human α1-acid glycoprotein
- Chiral recognition of verapamil by cyclodextrins studied with capillary electrophoresis, NMR spectroscopy, and electrospray ionization mass spectrometry
- Effect of acute physostigmine and verapamil treatment on aggressive and depressive behavior in rats with lesioned nucleus basalis magnocellularis
- Effect of acute verapamil treatment on body temperature in nucleus basalis magnocellularis-lesioned rats
- Effect of acute verapamil treatment on cold restraint-induced gastric lesions in rats with lesioned nucleus basalis magnocellularis
- The protective potential of the combination of verapamil and cimetidine on cisplatin-induced nephrotoxicity in man
- Addition of verapamil and tamoxifen to the initial chemotherapy of small cell lung cancer a phase I/II study
- Doxorubicin for unresectable hepatocellular carcinoma. A prospective study on the addition of verapamil
- Enhancement of cytotoxicity of doxorubicin by verapamil in the hepatic artery infusion for liver tumors in rats
- Verapamil-reversing concentrations induce blood flow changes that could counteract in vivo the MDR-1-modulating effects
- A phase I trial of intrahepatic Verapamil and doxorubicin. Regional therapy to overcome multidrug resistance
- A phase III randomized study of oral verapamil as a chemosensitizer to reverse drug resistance in patients with refractory myeloma. A southwest oncology group study
- Enzyme-Mediated Synthesis of (S)- and (R)-Verapamil