Active substanceVerapamilVerapamil
Similar drugsTo uncover
  • Verapamil
    solution in / in 
    Alkaloid, JSC     Macedonia
  • Verapamil
    pills inwards 
    VALENTA PHARM, PAO     Russia
  • Verapamil
    solution in / in 
    BIOSINTEZ, PAO     Russia
  • Verapamil
    solution in / in 
    ATOLL, LLC     Russia
  • Verapamil
    pills inwards 
    AKRIKHIN HFK, JSC     Russia
  • Verapamil
    pills inwards 
  • Verapamil
    pills inwards 
    AVEKSIMA, JSC     Russia
  • Verapamil
    pills inwards 
    Alkaloid, JSC     Macedonia
  • Verapamil
    pills inwards 
    Alkaloid, JSC     Macedonia
  • Verapamil
    pills inwards 
    AVVA RUS, OJSC     Russia
  • Verapamil
    pills inwards 
    OZONE, LLC     Russia
  • Verapamil
    pills inwards 
    NORTH STAR, CJSC     Russia
  • Verapamil Sopharma
    pills inwards 
    Unifarm JSC     Bulgaria
  • Verapamil-OBL
    pills inwards 
  • Verapamil-LekT
    pills inwards 
  • Verapamil-SZ
    pills inwards 
    NORTH STAR, CJSC     Russia
  • Verapamil-Eskom
    solution in / in 
    ESKOM NPK, OAO     Russia
  • The verohalide EP 240
    pills inwards 
  • Isoptin®
    pills inwards 
    Abbott GmbH & Co. KG     Germany
  • Isoptin®
    solution in / in 
    Abbott GmbH & Co. KG     Germany
  • Isoptin® CP 240
    pills inwards 
    Abbott GmbH & Co. KG     Germany
  • Finoptin®
    pills inwards 
    Orion Corporation     Finland
  • Dosage form: & nbspsolution for intravenous administration
    Composition:
    Active substance: verapamil hydrochloride (in terms of 100% substance) - 2.5 mg.
    Excipients: sodium chloride-8.5 mg, citric acid 18.49 mg, 1M sodium hydroxide solution 0.175 ml, 0.1 M hydrochloric acid 0.120 ml, water for injection 1.0 ml.
    Description:Transparent colorless liquid.
    Pharmacotherapeutic group:The blocker of "slow" calcium channels
    ATX: & nbsp

    C.08.D.A.01   Verapamil

    C.08.D.A   Phenylalkylamine derivatives

    Pharmacodynamics:
    Verapamil - a derivative of diphenylalkylamine, inhibits the transmembrane transport of calcium ions to the contractile fibers smoothlyomuscular cells. Has antiarrhythmic, antianginal and hypotensive action.

    Antiarrhythmic action is probably associated with its effect on the "slow" channels in the cells of the conduction system of the heart. Electrical activity of sinoatrial and atrioventricular (AV) node is largely dependent on the entry of calcium ions into the cells through the "slow" channels.Inhibiting calcium intake, verapamil slows down AV conduct and increase the effective refractory period in AV The site is proportional to the heart rate (heart rate). This effect leads to a decrease in the frequency of ventricular contractions in patients with atrial fibrillation and / or atrial flutter. Terminating the re-entry of excitation in AV node, verapamil can restore the correct sinus rhythm in patients with paroxysmal supraventricular tachycardia, including Wolff-Parkinson-White syndrome (WPW). Verapamil does not interfere with conduction through additional conductive pathways.

    Verapamil does not affect the unchanged atrial action potential and the time of intraventricular conduction, but lowers the amplitude, speed of depolarization and conduction in altered atrial fibers.

    The antianginal effect is associated with both direct action on the myocardium and with influence on peripheral hemodynamics (reduces the tone of peripheral arteries, general Pperipheral vascular resistance). The blockade of calcium ions entering the cell leads to a decrease in the transformation of the energy encapsulated in the macroergic ATP bonds into mechanical work, a decrease in the contractility of the myocardium.Reduces the need for myocardium in oxygen, has a vasodilating, negative, foreign and chronotropic effect.

    With intravenous bolus injection, the maximum effect develops in 3-5 minutes. Intravenous administration of 5-10 mg causes a transient (usually asymptomatic) decrease in normal blood pressure (BP), systemic vascular resistance and contractility; the filling pressure of the left ventricle slightly increases. The antianginal effect is dose-dependent, tolerance does not arise.

    Pharmacokinetics:

    Fast metabolismis healed in the liver by N-dealkylation and O-demethylation, with the formation of several metabolites (when ingested, 12 are identified, most of which are found only in trace amounts). Accumulation of the drug and its metabolites in the body explains the increased effect of course treatment. The main pharmacologically active metabolite is noraverapamil (20% of the hypotensive activity of verapamil). In the metabolism of the drug, isozymes participate CYP3A4, CYP3A5 and CYP3A7.

    Connection with blood plasma proteins - 90%.

    Penetrates through the blood-brain barrier and placental barrier (20-92% concentration in the blood plasma of the mother) and in breast milk (in low concentrations).

    Half-life (T1/2) with intravenous administration - biphasic: about 4 min. - early and 2-5 hours - final. With hepatic insufficiency increases bioavailability and lengthens T1/2. It is excreted by 70% of the kidneys (3-5% unchanged), 16-25% - with bile. It is not excreted by hemodialysis.

    Indications:

    For the treatment of supraventricular tachyarrhythmias:

    - restoration of sinus rhythm in paroxysmal supraventricular tachycardia, including conditions associated with the presence of additional pathways (Wolff-Parkinson-White-Lohun-Ganong-Levin syndrome)

    - control of the frequency of ventricular contractions during flutter and atrial fibrillation (tachyarrhythmic variant), with the exception of cases when flutter or atrial fibrillation is associated with the presence of additional pathways (Wolff-Parkinson-White and Louna-Ganong-Levin syndromes)

    Contraindications:

    Hypersensitivity to the drug and other components of the drug, severe arterial hypotension (systolic blood pressure (BP) less than 90 mmHg) or cardiogenic shock, atrioventricular blockade of II and III degree (excluding patients with an artificial pacemaker), Morgagni-Adams syndrome - Stokes,sinus node weakness syndrome (except for patients with an artificial pacemaker), sinoauric blockade, Wolff-Parkinson-White and Louna-Ganong-Levin syndrome in combination with atrial flutter or fibrillation (with the exception of patients with a pacemaker), ventricular tachycardia with broad, complex QRS (more than 0.12 seconds), chronic heart failure II-III stages (except for supraventricular tachycardia), simultaneous use of beta-blockers (intravenously), colchicine, preliminary (within 48 hours) use of disopyramide, pregnancy, lactation, age under 18 years (efficacy and safety not established).

    Carefully:

    AV blockade of the first degree, bradycardia, idiopathic hypertrophic subaortic stenosis, chronic heart failure, myocardial infarction with left ventricular failure, hepatic and / or renal failure, delayed neuromuscular transmission, advanced age, mild or moderate degree of arterial hypotension, concomitant use with beta-blockers (for oral administration), cardiac glycosides.

    Dosing and Administration:

    Only intravenously!

    The initial dose for intravenous administration is 5 mg (contents 1 ampoule) for 2 minutes with continuous ECG and AD control (injected slowly!).

    In elderly patients, the administration is carried out for at least 3 minutes to reduce the risk of adverse reactions.

    In the absence of an adequate reaction, the administration of the drug is repeated (5 mg) after 5-10 minutes or 10 mg after 30 minutes.

    Side effects:

    From the cardiovascular system: marked decrease in blood pressure, bradycardia, tachycardia.

    From the central nervous system: headache, dizziness, drowsiness (rarely).

    From the digestive tract: nausea, a feeling of discomfort in the abdomen.

    Allergic reactions: skin rash, hives, itching, angioedema, Stevens-Johnson syndrome, sweating, multiforme exudative erythema.

    Other: bronchospasm, convulsions (several cases), paralysis (tetraparesis), associated with the combined use of verapamil and colchicine (single).

    Overdose:

    Symptoms: bradycardia, turning into AV blockade, sometimes in asystole, marked decrease in blood pressure, heart failure, shock, sinoatrial blockade, hyperglycemia, metabolic acidosis. There are reports of deaths from overdose.

    Treatment: with rhythm and conduction disturbances - intravenously isoprenaline, norepinephrine, atropine, 10-20 ml of 10% calcium gluconate solution, artificial pacemaker; intravenously infusion of plasma-substituting solutions. To increase blood pressure in patients with hypertrophic cardiomyopathy, alpha-adrenergic stimulants (phenylephrine); do not use isoprenaline and norepinephrine. Hemodialysis is ineffective.

    Interaction:
    With the simultaneous use of verapamil:
    - increases the AUC (area under the concentration-time curve) of carbamazepine in patients with persistent partial epilepsy (risk of side effects such as diplopia, headache, ataxia and dizziness).
    - increases AUC, Css (clearance) and Cmax (maximum concentration of the drug) cyclosporine.
    - increases AUC and Cmax of glibenclamide.
    - increases the concentration of sirolimus and tacrolimus.
    - significantly increases AUC and Cmax buspirone and midazolam.
    - increases the concentration of theophylline (due to lower clearance), ethanol (and lengthens its effect), the concentration of quinidine (the risk of pronounced reduction in blood pressure).
    - can increase the concentration of atorvastatin and lovastatin.
    - increases significantly AUC and Cmax simvastatin.
    - increases AUC and Cmax of almotriptan.
    - increases the concentration of cardiac glycosides (requires careful observation and a lower dose of glycosides).
    - increases AUC and Cmax metoprolol and propranolol in patients with angina.
    - increases the plasma concentration of colchicine (substrate for CYP3A and p-glycoprotein).
    - when ingested significantly increases AUC and Cmax doxorubicin.
    - slightly increases the AUC of imipramine; does not affect the concentration of the active metabolite, desipramine.
    - increases the Cmax of prazosin and terazosin and AAC terazosin.
    - inhibitors of CYP3A (including erythromycin, ritonavir and other antiviral HIV drugs), telithromycin increase plasma concentrations of verapamil.
    - grapefruit juice increases AUC and Cmax R- and S-isomer verapamil.
    - cimetidine increases the bioavailability of verapamil by almost 40-50% (due to a decrease in hepatic metabolism), so it may be necessary to reduce the dose of the latter.
    - rifampicin can significantly reduce bioavailability (up to 92%), as well as AUC and Cmax verapamil.
    - Phenobarbital increases the clearance of verapamil 5 times.
    - sulfinpyrazone increases the clearance of verapamil by about 3 times and reduces bioavailability (60%).
    - preparations of St. John's wort penetrate the AUC R- and S-isomers of verapamil and, respectively, Cmax.
    - while simultaneous use with inhalation anesthetics increases the risk of bradycardia, atrioventricular blockade, heart failure.
    - a combination with beta-blockers can lead to an increase in the negative inotropic effect, an increased risk of developing atrioventricular conduction disorders, bradycardia (the administration of verapamil and beta-blockers should be performed at intervals of several hours)
    - prazosin and other alpha-blockers, as well as other antihypertensive agents (angiotensin-converting enzyme inhibitors, vasodilators, diuretics, beta-blockers) intensify the hypotensive effect.
    - disopyramide and flecainide should not be administered within 48 hours or 24 hours after the use of verapamil (summation of a negative inotropic effect, up to a lethal outcome).
    - increases the risk of neurotoxic effect of lithium preparations.
    - strengthens the action of peripheral muscle relaxants (a change in the dosage regimen may be required).
    - while concomitant use with acetylsalicylic acid showed a slightly greater increase in bleeding time than with acetylsalicylic acid alone.
    - carbamazepine and lithium increases the risk of neurotoxic effects.
    - antiarrhythmics, beta-blockers (more severe atrioventricular block, more significant heart rate reduction, development of heart failure and increased arterial hypotension). Patients taking digitalis preparations, quinidine, disopyramide, flecainide and other artiarrhythmic drugs, must be carefully observed.
    Special instructions:

    Heart failure must first be compensated.

    In the treatment it is necessary to control the functions of the cardiovascular system, the respiratory system, the content of glucose and electrolytes in the blood, the volume of circulating blood and the amount of excreted urine.

    Intravenous administration of verapamil often causes a transient reduction in blood pressure that usually does not appear clinically, but which can be accompanied by dizziness.

    In patients with chronic heart failure (pulmonary artery wedge pressure more than 20 mm Hg, ejection fraction less than 30%), with the appointment of verapamil, acute progression of circulatory failure can be observed.

    Form release / dosage:

    Solution for intravenous administration 2.5 mg / ml.

    Packaging:

    2 ml of the drug in ampoules.

    For 5 or 10 ampoules in contour cell packs from a polyvinyl chloride film.

    By 1 or 2 contour acrylic packaging together with instructions for use in a cardboard pack.

    Storage conditions:

    In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

    Shelf life:

    2 years. Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-000167/09
    Date of registration:16.01.2009
    Expiration Date:Unlimited
    The owner of the registration certificate:ESKOM NPK, OAO ESKOM NPK, OAO Russia
    Manufacturer: & nbsp
    Information update date: & nbsp29.01.2017
    Illustrated instructions
      Instructions
      Up