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Isoptin

Isoptin
Isoptin is prescribed for coronary artery disease, unstable angina, vasospastic angina, postinfarction angina in patients without heart failure, arrhythmia, arterial hypertension.

Brand: Verapamil

Availability: In Stock
Average Delivery Time: 9 Days
Exp. Date: November 2023
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Isoptin 240 mg
270 pills - 240 mg
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$291.93 $1.08 $196.50 Add to cart
180 pills - 240 mg
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$199.99 $1.11 $125.63 Add to cart
120 pills - 240 mg
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$143.51 $1.20 $73.57 Add to cart
90 pills - 240 mg
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$113.99 $1.27 $48.82 Add to cart
60 pills - 240 mg $83.99 $1.40 $24.55 Add to cart
30 pills - 240 mg $54.27 $1.81 No Add to cart
Isoptin 120 mg
270 pills - 120 mg
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$194.35 $0.72 $183.20 Add to cart
180 pills - 120 mg
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$137.51 $0.76 $114.19 Add to cart
120 pills - 120 mg $98.99 $0.82 $68.81 Add to cart
90 pills - 120 mg $79.99 $0.89 $45.86 Add to cart
60 pills - 120 mg $61.99 $1.03 $21.91 Add to cart
30 pills - 120 mg $41.95 $1.40 No Add to cart
Isoptin 40 mg
270 pills - 40 mg
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$121.85 $0.45 $85.11 Add to cart
180 pills - 40 mg $88.99 $0.49 $48.98 Add to cart
120 pills - 40 mg $67.05 $0.56 $24.93 Add to cart
90 pills - 40 mg $56.99 $0.63 $12.00 Add to cart
60 pills - 40 mg $45.99 $0.77 No Add to cart

Product description

Pharmacological action of the drug Isoptin

Buy Isoptin in Canada

Class I selective calcium channel blocker, a phenylalkylamine derivative. It has antianginal, antiarrhythmic and antihypertensive effects.

The antianginal effect is associated with both a direct effect on the myocardium and with an effect on peripheral hemodynamics (reduces the tone of peripheral arteries, OPSS). The blockade of calcium entry into the cell leads to a decrease in the transformation of energy contained in the high-energy ATP bonds into mechanical work, and a decrease in myocardial contractility. Reduces myocardial oxygen demand, has a vasodilating, negative foreign and chronotropic effect. Increases the period of diastolic relaxation of the left ventricle, reduces the tone of the myocardial wall.

The antihypertensive effect of verapamil may also be due to a decrease in the OPSS.

Verapamil significantly reduces AV conduction, lengthens the refractory period and suppresses the automatism of the sinus node. It has an antiarrhythmic effect in supraventricular arrhythmias.

Pharmacokinetics

When ingested, more than 90% of the dose is absorbed. Protein binding - 90%. Metabolized during the "first pass" through the liver. The main metabolite is norverapamil, which has less pronounced hypotensive activity than unchanged verapamil.

T1/2 when taking a single dose is 2.8-7.4 hours, when taking repeated doses - 4.5-12 hours (due to saturation of the liver enzyme systems and an increase in the concentration of verapamil in the blood plasma). After intravenous administration, the initial T1/2 is about 4 minutes, the final one is 2-5 hours.

It is excreted mainly by the kidneys and 9-16% through the intestines.

Indications of the active substances of Isoptin®

 Isoptin for the treatment of heart problems

Treatment and prevention of coronary artery disease: chronic stable angina (exertional angina), unstable angina, vasospastic angina (Prinzmetal angina / variant angina).

Treatment and prevention of cardiac arrhythmias: paroxysmal supraventricular tachycardia, chronic form of atrial flutter and atrial fibrillation (tachyarrhythmia variant), supraventricular extrasystole.

Arterial hypertension. Hypertensive crisis.

Hypertrophic cardiomyopathy.

Dosing regimen of the drug Isoptin

Isoptin drug appearance

Individual. Inside for adults - at an 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 decreased. 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 injected 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, repeated administration at the same dose is possible. A single dose for children aged 6-14 years is 2.5-3.5 mg, 1-5 years old - 2-3 mg, up to 1 year old - 0.75-2 mg. For patients with severe hepatic dysfunction, the daily dose of verapamil should not exceed 120 mg.

The maximum daily oral dose for adults is 480 mg.

Contraindications for use

Cardiogenic shock, heart failure, severe impaired contractile function of the left ventricle, severe hypotension (systolic blood pressure less than 90 mm Hg), bradycardia; SSSU, sinoatrial blockade, AV block II and III degree (except for patients with a pacemaker); atrial flutter and fibrillation in combination with WPW syndrome or Lown-Ganong-Levin syndrome (except for patients with a pacemaker); simultaneous reception with colchicine, dantrolene, aliskiren, sertindole; pregnancy, lactation (breastfeeding); hypersensitivity to verapamil.

Application during pregnancy and lactation

Verapamil is contraindicated during pregnancy and lactation.

Application for violations of liver function

With caution should be used in liver failure.

Application for impaired renal function

Caution should be used in renal failure.

Use in children

With caution should be used in children and adolescents under the age of 18 years (efficacy and safety have not been studied).

Use in elderly patients

Use with caution in elderly patients.

Special instructions

Caution should be used in case of AV blockade of the 1st degree, bradycardia, severe stenosis of the aortic opening, chronic heart failure, with mild or moderate arterial hypotension, in the acute phase of myocardial infarction, obstructive hypertrophic cardiomyopathy, with hepatic and / or renal failure, in elderly patients, children and adolescents under the age of 18 years (efficacy and safety of use have not been studied).

If necessary, a combination therapy of angina pectoris and arterial hypertension with verapamil and beta-blockers is possible. However, intravenous administration of beta-blockers should be avoided while using verapamil.

Influence on the ability to drive vehicles and control mechanisms

After taking verapamil, individual reactions (drowsiness, dizziness) are possible, affecting the patient's ability to perform work that requires a high concentration of attention and speed of psychomotor reactions.

Drug interaction

With simultaneous use with antihypertensive drugs (vasodilators, thiazide diuretics, ACE inhibitors), the antihypertensive action is mutually reinforced.

With simultaneous use with beta-blockers, antiarrhythmic agents, agents for inhalation anesthesia, the risk of developing bradycardia, AV blockade, severe arterial hypotension, heart failure increases, due to the mutual strengthening of the inhibitory effect on the automatism of the sinoatrial node and AV conduction, contractility and conductivity myocardium.

With parenteral administration of verapamil to patients who have recently received beta-blockers, there is a risk of arterial hypotension and asystole.

With simultaneous use with nitrates, the antianginal effect of verapamil is enhanced.

With simultaneous use with aliskiren, its concentration in plasma increases and the risk of side effects increases.

With simultaneous use with amiodarone, the negative inotropic effect, bradycardia, conduction disturbances, AV blockade are enhanced.

Since verapamil inhibits the isoenzyme CYP3A4, which is involved in the metabolism of atorvastatin, lovastatin and simvastatin, drug interactions are theoretically possible due to an increase in plasma concentrations of statins. Cases of the development of rhabdomyolysis are described.

With simultaneous use with acetylsalicylic acid, cases of increased bleeding time due to additive antiplatelet action have been described.

With simultaneous use with buspirone, the concentration of buspirone in the blood plasma increases, its therapeutic and side effects increase.

With the simultaneous administration of verapamil and dantrolene (i.v.) in experimental studies in animals, ventricular fibrillation with a lethal outcome was observed. This combination is potentially dangerous.

With simultaneous use with digoxin, cases of an increase in the concentration of digitoxin in blood plasma have been described.

With simultaneous use with digoxin, the concentration of digoxin in the blood plasma increases.

With simultaneous use with disopyramide, severe arterial hypotension and collapse are possible, especially in patients with cardiomyopathy or decompensated heart failure. The risk of developing severe manifestations of drug interactions is apparently associated with an increase in the negative inotropic effect.

With simultaneous use with diclofenac, the concentration of verapamil in the blood plasma decreases; with doxorubicin - the concentration of doxorubicin in the blood plasma increases and its effectiveness increases.

With simultaneous use with imipramine, the concentration of imipramine in the blood plasma increases and there is a risk of developing unwanted changes on the ECG. Verapamil increases the bioavailability of imipramine by decreasing its clearance. Changes in the ECG are due to an increase in the concentration of imipramine in the blood plasma and the additive inhibitory effect of verapamil and imipramine on AV conduction.

With simultaneous use with carbamazepine, the effect of carbamazepine increases and the risk of side effects from the central nervous system increases due to inhibition of the metabolism of carbamazepine in the liver under the influence of verapamil.

With simultaneous use with clonidine, cases of cardiac arrest in patients with arterial hypertension have been described.

Increases the plasma concentration of colchicine (a substrate of CYP3A isoenzyme and P-glycoprotein).

When used simultaneously with lithium carbonate, the manifestations of drug interactions are ambiguous and unpredictable. Cases of increased effects of lithium and the development of neurotoxicity, a decrease in the concentration of lithium in the blood plasma, and severe bradycardia are described.

The vasodilating effect of alpha-blockers and calcium channel blockers can be additive or synergistic. With the simultaneous use of terazosin or prazosin and verapamil, the development of severe arterial hypotension is partly due to pharmacokinetic interaction: an increase in Cmax and AUC of terazosin and prazosin.

With simultaneous use, rifampicin induces the activity of liver enzymes, accelerating the metabolism of verapamil, which leads to a decrease in its clinical effectiveness.

With simultaneous use with sertindole, the risk of developing ventricular cardiac arrhythmias, especially ventricular arrhythmias of the "pirouette" type, increases.

With simultaneous use, the concentration of theophylline in the blood plasma increases.

With simultaneous use with tubocurarine chloride, vecuronium chloride, it is possible to enhance the muscle relaxant effect.

With simultaneous use with phenytoin, phenobarbital, a significant decrease in the concentration of verapamil in the blood plasma is possible.

With simultaneous use with fluoxetine, the side effects of verapamil are enhanced due to a slowdown in its metabolism under the influence of fluoxetine.

With simultaneous use, the clearance of quinidine decreases, its concentration in blood plasma increases and the risk of side effects increases. Cases of arterial hypotension have been observed.

With the simultaneous use of verapamil inhibits the metabolism of cyclosporine in the liver, which leads to a decrease in its excretion and an increase in plasma concentration. This is accompanied by an increase in the immunosuppressive effect, a decrease in the manifestations of nephrotoxicity is noted.

With simultaneous use with cimetidine, the effects of verapamil are enhanced.

With simultaneous use with enflurane, prolongation of anesthesia is possible.

When used simultaneously with etomidate, the duration of anesthesia is increased.

Side effect

From the side of the cardiovascular system: bradycardia (less than 50 beats / min), a marked decrease in blood pressure, development or worsening of heart failure, tachycardia; rarely - angina pectoris, up to the development of myocardial infarction (especially in patients with severe obstructive coronary artery disease), arrhythmia (including fibrillation and flutter of the ventricles); with rapid intravenous administration - AV block of the III degree, asystole, collapse.

From the side of the central nervous system and peripheral nervous system: dizziness, headache, fainting, anxiety, lethargy, fatigue, asthenia, drowsiness, depression, extrapyramidal disorders (ataxia, mask-like face, shuffling gait, stiffness of the hands or feet, trembling of the hands and fingers, difficulty swallowing).

From the digestive system: nausea, constipation (rarely diarrhea), gingival hyperplasia (bleeding, soreness, swelling), increased appetite, increased activity of hepatic transaminases and alkaline phosphatase.

Allergic reactions: itching, skin rash, flushing of the facial skin, erythema multiforme exudative (including Stevens-Johnson syndrome).

Others: weight gain, very rarely - agranulocytosis, gynecomastia, hyperprolactinemia, galactorrhea, arthritis, transient loss of vision against the background of maximum plasma concentration (with intravenous administration), pulmonary edema, asymptomatic thrombocytopenia, peripheral edema.