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Isoptin CP 240 extended-release tablets 240 mg 30 pcs.

In vitro studies indicate that verapamil hydrochloride is metabolized by the cytochrome P450 isoenzymes CYP3A4, CYP1A2, CYP2C8, CYP2C9 and CYP2C18. A clinically significant interaction was observed with concomitant use of CYP3A4 inhibitors, which caused an increase in plasma levels of verapamil, while CYP3A4 inducers decreased its plasma concentration. Accordingly, when using such agents simultaneously, the possibility of interaction should be taken into account. The table provides a list of possible drug interactions due to changes in their pharmacokinetic parameters. Possible drug interactions when taking Verapamil: Alpha blockers. Prazosin. An increase in prazosin Cmax (~40%) does not affect the half-life of prazosin. Terazosin. Increased terazosin AUC (~24%) and Cmax (~25%). Antiarrhythmic drugs. Flecainide. Minimal effect on flecainide plasma clearance (<~10%); does not affect the clearance of verapamil in plasma. Quinidine. Decreased oral clearance of quinidine (~35%). Medicines for the treatment of asthma. Theophylline. Decreased oral and systemic clearance of quinidine (~20%). For smokers there is a decrease of ~11%. Anticonvulsants. Carbamazepine. Increased AUC of carbamazepine (~46%) in patients with resistant partial epilepsy. Antidepressants. Imipramine. Increase in AUC of imipramine (~15%) Does not affect the level of the active metabolite, desipramine. Antidiabetic agents. Glyburide. Smachglyburide increases (~28%), AUC (~26%). Antimicrobial agents. Erythromycin. Verapamil levels may increase. Rifampicin. The AUC of verapamil (~97%), Cmax (~94%), and oral bioavailability (~92%) decreases. Telithromycin. Verapamil levels may increase. Antitumor drugs. Doxorubicin. The half-life of doxorubicin decreases (~27%) and Cmax (~38%)*. Barbiturates. Phenobarbital. The oral clearance of verapamil increases by 5 times. Benzodiazepines and other tranquilizers. Buspirone. The AUC of buspirone, Cmax, increases by 3.4 times. Midazolam. The AUC of midazolam increases (~ 3 times) and Cmax (~ 2 times). Beta blockers. Metoprolol. The AUC of metoprolol (~32.5%) and Cmax (~41%) increases in patients with angina pectoris. Propranolol. Propranolol AUC (~65%) and Cmax (~94%) increase in patients with angina pectoris. Cardiac glycosides. Digitoxin. The total clearance (~27%) and extrarenal clearance (~29%) of digitoxin decreases. Digoxin. In healthy volunteers, Cmax increases by ~45-53%, Css by ~42% and AUC by ~52%. H2 receptor antagonists. Cimetidine. The AUC of R- (~25%) and S-(~40%) verapamil increases with a corresponding decrease in the clearance of R- and S-verapamil. Immunological agents. Cyclosporine. AUC, Css, Cmax increases by ~45%. Sirolimus. There may be an increase in sirolimus levels. Tacrolimus. Tacrolimus levels may increase. Lipid lowering agents. Atorvastatin. Possible increase in atorvastatin levels. Lovastatin. Possible increase in lovastatin levels. Simvastatin. The AUC (~2.6 times) and Cmax (~4.6 times) of simvastatin increases. Serotonin receptor antagonists. Almotriptan. The AUC (~20%) and Cmax (~24%) of almotriptan are increased. Uricosuric drugs. Sulfinpyrazone. Increased oral clearance of verapamil (~ 3 times), decreased bioavailability (~ 60%). Other. Grapefruit juice. Increased AUC of R- (~49%) and S-(~37%) verapamil and Cmax of R-(~75%) and S-(~51%) verapamil. Elimination half-time and renal clearance were unchanged. St. John's wort. The AUC of R- (~78%) and S-(~80%) verapamil decreases with a corresponding decrease in Cmax. * in patients with advanced neoplasms, verapamil does not affect the level or clearance of doxirubicin. In patients with small cell lung cancer, verapamil reduced the half-life and Cmax of doxirubicin. Antiarrhythmic drugs, beta blockers. Mutual enhancement of effects on the cardiovascular system is possible (more pronounced atrioventricular block, more significant decrease in heart rate, development of heart failure and increased hypotension). Antihypertensives, diuretics, vasodilators. Strengthening the hypotensive effect. Prazosin, terazosin. Additive hypotensive effect. Antiviral and drugs for the treatment of HIV infection. Ritonavir and antiviral drugs may inhibit the metabolism of verapamil, resulting in increased plasma concentrations. In this regard, the dose of verapamil should be reduced. Quinindine. Hypotension. Patients with hypertrophic obstructive cardiomyopathy may develop pulmonary edema. Carbamazepine. Increased plasma levels of carbamazepine and increased neurotoxicity. Adverse reactions characteristic of carbamazepine, such as diplopia, headache, ataxia or dizziness, may occur. Lithium. Increased lithium neurotoxicity. Rifampicin. May reduce the hypotensive effect of verapamil. Sulfinpyrazone. May reduce the hypotensive effect of verapamil. Muscle relaxants. The effect of muscle relaxants may be enhanced. Aspirin (acetylsalicylic acid). Increased bleeding. Ethanol (alcohol). Increased plasma ethanol levels. HMG-Co A reductase inhibitors (statins). Simvastatin/lovastatin. Concomitant use with verapamil may result in increased serum levels of simvastatin or lovastatin. In patients receiving verapamil, treatment with HMG-CoA reductase inhibitors (i.e. simvastatin/lovastatin) should be started at the lowest possible doses and increased thereafter. If it is necessary to prescribe verapamil to patients already receiving HMG-CoA reductase inhibitors, it is necessary to review and reduce their doses according to the concentration of cholesterol in the blood serum. Similar tactics should be followed when concomitantly prescribing verapamil with atorvastatin (although there is no clinical data confirming the interaction of verapamil and atorvastatin), since pharmacokinetic studies are clearly known to confirm that verapamil had a similar effect on the level of atorvastatin. Fluvastatin, pravastatin and rosuvastatin are not metabolized by CYP3A4 isoenzymes, so their interaction with verapamil is least likely.

Description of the drug ISOPTIN

When used simultaneously with antihypertensive drugs (vasodilators, thiazide diuretics, ACE inhibitors), the antihypertensive effect is mutually enhanced.

When used simultaneously with beta-blockers, antiarrhythmic drugs, and inhalation anesthesia agents, the risk of developing bradycardia, AV blockade, severe arterial hypotension, and heart failure increases due to the mutual increase in the inhibitory effect on the automatism of the sinoatrial node and AV conduction, contractility and conductivity. myocardium.

When verapamil is administered parenterally to patients who have recently received beta-blockers, there is a risk of developing arterial hypotension and asystole.

When used simultaneously with nitrates, the antianginal effect of verapamil is enhanced.

When used simultaneously with aliskiren, its plasma concentration increases and the risk of side effects increases.

When used simultaneously with amiodarone, the negative inotropic effect, bradycardia, conduction disturbances, and AV block are enhanced.

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

When used simultaneously with acetylsalicylic acid, cases of increased bleeding time due to additive antiplatelet effect have been described.

When used simultaneously with buspirone, the concentration of buspirone in the blood plasma increases, and its therapeutic and side effects increase.

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

When used simultaneously with digoxin, cases of increased concentrations of digitoxin in the blood plasma have been described.

When used simultaneously with digoxin, the concentration of digoxin in the blood plasma increases.

When used concomitantly with disopyramide, severe 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 increased negative inotropic effects.

When used simultaneously 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.

When used simultaneously with imipramine, the concentration of imipramine in the blood plasma increases and there is a risk of developing undesirable changes on the ECG. Verapamil increases the bioavailability of imipramine by reducing 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.

When used simultaneously with carbamazepine, the effect of carbamazepine is enhanced 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.

When used simultaneously with clonidine, cases of cardiac arrest in patients with arterial hypertension have been described.

Increases plasma concentrations of colchicine (substrate of the isoenzyme CYP3A 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 have been described.

The vasodilating effects of alpha-blockers and calcium channel blockers may 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:

increased 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.

When used simultaneously with sertindole, the risk of developing ventricular cardiac arrhythmias, especially ventricular arrhythmias, increases.

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

When used simultaneously with tubocurarine chloride and vecuronium chloride, the muscle relaxant effect may be enhanced.

When used simultaneously with phenytoin and phenobarbital, a significant decrease in the concentration of verapamil in the blood plasma is possible.

When used simultaneously with fluoxetine, the side effects of verapamil increase due to a slowdown in its metabolism under the influence of fluoxetine.

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

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

When used simultaneously with cimetidine, the effects of verapamil are enhanced.

When used simultaneously with enflurane, prolongation of anesthesia is possible.

When used simultaneously with etomidate, the duration of anesthesia increases.

Isoptin®

Verapamil hydrochloride is a racemic mixture consisting of equal amounts of the R-enantiomer and the S-enantiomer.

Norverapamil is one of 12 metabolites found in urine. The pharmacological activity of norverapamil is 10-20% of the pharmacological activity of verapamil, and the proportion of norverapamil is 6% of the excreted drug. The equilibrium concentrations of norverapamil and verapamil in blood plasma are similar. Equilibrium concentration with long-term use once a day is achieved after 3-4 days.

Suction

More than 90% of verapamil is rapidly absorbed in the small intestine after oral administration. The average systemic bioavailability after a single oral dose of verapamil is 22%, which is due to the pronounced effect of “first pass” through the liver. The bioavailability of verapamil increases approximately 2-fold with repeated use.

The time to reach the maximum concentration (TCmax) of verapamil in the blood plasma is 1-2 hours. The maximum concentration of norverapamil in blood plasma is achieved approximately 1 hour after taking verapamil. Food intake does not affect the bioavailability of verapamil.

Distribution

Verapamil is well distributed in body tissues, the volume of distribution (Vd) in healthy volunteers is 1.8-6.8 l/kg. Communication with blood plasma proteins is about 90%.

Metabolism

Verapamil undergoes extensive metabolism. Metabolic studies in vitro

showed that verapamil is metabolized by cytochrome P450 isoenzymes CYP3A4, CYP1A2, CYP2C8, CYP2C9 and CYP2C18. In healthy volunteers, after oral administration, verapamil undergoes intensive metabolism in the liver, with 12 metabolites detected, most of which are in trace amounts. The main metabolites were identified as the N and O-dealkylated forms of verapamil. Among the metabolites, only norverapamil has a pharmacological effect (about 20% compared to the parent compound), which was revealed in a study in dogs.

Removal

The half-life (T1/2) after taking verapamil orally is 3-7 hours. Within 24 hours, about 50% of the verapamil dose is excreted by the kidneys, within five days - 70%. Up to 16% of the verapamil dose is excreted through the intestines. Approximately 3-4% of verapamil is excreted unchanged by the kidneys. The total clearance of verapamil approximately coincides with the hepatic blood flow, i.e. about 1 l/h/kg (range: 0.7-1.3 l/h/kg).

Special patient groups

Elderly patients

Age may affect the pharmacokinetic parameters of verapamil when administered to patients with arterial hypertension. T1/2 may be increased in elderly patients. There was no relationship between the antihypertensive effect of verapamil and age.

Renal dysfunction

Impaired renal function does not affect the pharmacokinetic parameters of verapamil, which was revealed in comparative studies involving patients with end-stage renal failure and patients with normal renal function. Verapamil and norverapamil are practically not excreted during hemodialysis.

Liver dysfunction

In patients with impaired liver function, T1/2 is prolonged due to lower oral clearance of verapamil and higher Vd.