Isoptin is a synthetic drug that is prescribed for the treatment and prevention of angina pectoris, arrhythmia and hypertension. INN (International non-proprietary name) of the drug Verapamil. He got this name because of the active substance that is part of it. The drug quickly removes the symptoms of hypertension, moreover, it acts for a long time.

Release form

The medicine is produced in 3 forms:

Indications for the use of the drug

Isoptin (Verapamil) may be prescribed in such cases:

Compound

The composition of the drug "Isoptin" depends on the form of its release:

How to take pills?

Take the drug in tablet form according to the following rules:

Isoptin Retard - tablets of prolonged action

The drug "Isoptin SR" has a long-lasting effect than the usual tablets "Isoptin".

So, this medicine has such advantages:

The drug "Isoptin SR" is advisable to prescribe to those patients who:

The method and features of the use of tablets "Isoptin Retard"

Take them after meals with a glass of water. Depending on the type and severity of the disease, the patient may be prescribed a different dosage - from 120 to 360 mg at a time.

The drug can be taken for a long time, but then the daily dose of the drug should not exceed 2 tablets. Usually, the specialist prescribes the patient the drug "Isoptin Retard" at a dosage of 120 or 240 mg in the morning. Additional reception is possible only in the evening.

It is possible to increase the dosage of the drug "Isoptin SR" not earlier than 2 weeks after the start of the intake.

In case of an overdose, symptoms such as hypotension, loss of consciousness, shock, weakness, dizziness, darkening of the eyes, decreased pulse rate, heart pain, convulsions, etc.

For treatment, the patient needs:

The drug "Isoptin" in ampoules is used only in stationary conditions, because the solution is administered intravenously. The advantage of the drug in the form of a solution is that the drug is absorbed faster, respectively, the best therapeutic effect is achieved.

The solution "Isoptin" is administered under the supervision of a doctor. The initial dose is 5 mg. If no effect is observed, then a possible re-introduction after 10 minutes. The drug can also be administered drip at a dosage of 5-10 mg / h. The drug is pre-diluted in glucose solution, saline or other liquids recommended by the doctor.

Important Information

Side effects

Isoptin tablets can cause various undesirable manifestations from many organs and systems:

Contraindications

The described drug should not be prescribed to patients who have the following health problems or features:

Analogues of the drug "Isoptin"

This medicine has several dozen substitutes. So, according to the active substance, drugs such as Veropamil, Lekoptin, Kaveril, Finoptin, etc. can be distinguished. By a similar action, drugs such as Kaveril, Amlodak, etc. can be distinguished.

Interaction with other drugs

If, in addition to Isoptin tablets, a person takes other medications (blockers, painkillers, anti-inflammatory and other drugs), then it is necessary to consult with your doctor about the parallel use of these drugs in order to avoid negative effects.

Price

The price of the drug "Isoptin" in tablets varies between 350-400 rubles for 30 pills. The cost of tablets "Isoptin Retard" of prolonged action is about 600-650 rubles.

Catad_pgroup Calcium channel blockers

Isoptin for injection - instructions for use

Currently, the drug is not listed in the State Register of Medicines or the specified registration number has been excluded from the register.

Registration number:

P N015547/01

Active substance:

Verapamil

Dosage form:

solution for intravenous administration

Compound:

For 2 ml of solution:

active substance: verapamil hydrochloride 5.0 mg;

Excipients: sodium chloride 17.0 mg, 36% hydrochloric acid - to adjust the pH, water for injection - up to 2 ml.

Description:

Clear colorless solution.

Pharmacotherapeutic group:

Blocker of "slow" calcium channels

ATH:

C.08.D.A.01

Pharmacodynamics:

Verapamil blocks the transmembrane entry of calcium ions (and possibly sodium ions) through "slow" channels into the cells of the myocardial conduction system and smooth muscle cells of the myocardium and blood vessels. The antiarrhythmic effect of verapamil is probably due to its effect on the "slow" channels in the cells of the conduction system of the heart.

The electrical activity of the sinoatrial (SA) and atrioventricular (AV) nodes largely depends on calcium entering the cells through "slow" channels. By inhibiting this supply of calcium,
verapamil slows atrioventricular (AV) conduction and increases the effective refractory period in the AV node in proportion to heart rate (HR). This effect results in a decrease in ventricular rate in patients with atrial fibrillation and/or atrial flutter. Terminating the re-entry of excitation in the AV node,
verapamil can restore correct sinus rhythm in patients with paroxysmal supraventricular tachycardia, including Wolff-Parkinson-White (WPW) syndrome.

Verapamil has no effect on accessory conduction pathways, does not affect the normal atrial action potential or intraventricular conduction time, but reduces the amplitude, rate of depolarization, and conduction in altered atrial fibers.

Verapamil does not cause spasm of the peripheral arteries and does not change the total calcium content in the blood serum. Reduces afterload and myocardial contractility. In most patients, including patients with organic heart disease, the negative inotropic effect of verapamil is offset by a decrease in afterload, the cardiac index usually does not decrease, but in patients with moderate and severe heart failure (pulmonary artery wedge pressure more than 20 mm Hg, ejection fraction of the left ventricle is less than 35%), acute decompensation of chronic heart failure can be observed.

The maximum therapeutic effect is observed 3-5 minutes after a bolus intravenous administration of verapamil.

Standard therapeutic doses of verapamil 5-10 mg intravenously cause a transient, usually asymptomatic, decrease in normal blood pressure (BP), systemic vascular resistance and contractility; the filling pressure of the left ventricle slightly increased.

Pharmacokinetics:

Verapamil hydrochloride is a racemic mixture consisting of the same amount of R-enantiomer and 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. Steady-state plasma concentrations of norverapamil and verapamil are similar. Equilibrium concentration with prolonged use once a day is reached after 3-4 days.

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 intensive metabolism. Metabolic Research in vitro showed that
Verapamil is metabolized by CYP3A4, CYP1A2, CYP2C8, CYP2C9 and CYP2C18 cytochrome P450 isoenzymes.

In healthy volunteers after oral administration
Verapamil undergoes extensive metabolism in the liver, with 12 metabolites detected, most of which are in trace amounts. The main metabolites have been 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.

breeding

With intravenous administration, the curve of change in the concentration of verapamil in the blood is biexponential in nature with a fast early distribution phase (half-life (T 1/2) - about 4 minutes) and a slower terminal elimination phase (T 1/2 - 2-5 hours).

Within 24 hours, about 50% of the dose of verapamil is excreted by the kidneys, within five days - 70%. Up to 16% of a dose of verapamil is excreted through the intestines. Approximately 3-4% of verapamil is excreted by the kidneys unchanged. 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 taken by patients with arterial hypertension. T 1/2 may be increased in elderly patients. The relationship between the antihypertensive effect of verapamil and age has not been identified.

Impaired kidney function

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

Indications for use

For the treatment of supraventricular tachyarrhythmias, including:

Restoration of sinus rhythm in paroxysmal supraventricular tachycardia, including conditions associated with the presence of additional pathways in Wolff-Parkinson-White (WPW) and Lown-Ganong-Levin (LGL) syndromes.

In the presence of clinical indications, it is advisable to try to influence the vagus nerve (for example, the Valsalva maneuver) before using the drug Isoptin®;

Temporary control of the frequency of ventricular contractions in atrial flutter and fibrillation (tachyarrhythmic variant), except in cases where atrial flutter or fibrillation is associated with the presence of additional pathways (WPW and LGL syndromes).

Contraindications

Hypersensitivity to the active substance or auxiliary components of the drug;

Cardiogenic shock;

Atrioventricular block II or III degree, with the exception of patients with an artificial pacemaker;

Sick sinus syndrome, with the exception of patients with an artificial pacemaker;

Heart failure with reduced left ventricular ejection fraction less than 35% and/or pulmonary artery wedge pressure greater than 20 mm Hg. Art., with the exception of heart failure caused by supraventricular tachycardia, to be treated with verapamil;

Severe arterial hypotension (systolic blood pressure less than 90 mm Hg);

Atrial fibrillation / flutter in the presence of additional pathways (Wolf-Parkinson-White, Lown-Ganong-Levin syndromes). These patients are at risk of developing ventricular tachyarrhythmia, incl. ventricular fibrillation in the case of verapamil;

Ventricular tachycardia with wide QRS complexes (> 0.12 sec.) (see section "Special Instructions");

Simultaneous use with beta-blockers, intravenously.
Verapamil and beta-blockers should not be administered simultaneously (within several hours), since both drugs can reduce myocardial contractility and AV conduction (see section "Interaction with other drugs");

The use of disopyramide 48 hours before and 24 hours after taking verapamil;

Pregnancy, breastfeeding period (efficacy and safety have not been established);

Age up to 18 years (efficacy and safety not established).

Carefully:

Severe decrease in blood pressure, acute myocardial infarction, left ventricular dysfunction, AV block I degree, bradycardia, asystole, hypertrophic obstructive cardiomyopathy, heart failure.

Impaired kidney function and / or severe liver dysfunction.

Diseases affecting the neuromuscular transmission (myasthenia gravis, Lambert-Eaton syndrome, Duchenne muscular dystrophy).

Simultaneous administration with cardiac glycosides, quinidine, flecainide, simvastatin, lovastatin, atorvastatin; ritonavir and other antiviral drugs for the treatment of HIV infection; beta-blockers for oral administration; means that bind to plasma proteins (see section "Interactions with other drugs").

Elderly age.

Pregnancy and lactation:

There are no sufficient data on the use of the drug Isoptin® in pregnant women. Animal studies do not reveal direct or indirect toxic effects on the reproductive system. Due to the fact that the results of drug studies in animals do not always predict the response to treatment in humans, the drug Isoptin® can be used during pregnancy only if the benefit to the mother outweighs the potential risk to the fetus / child.

Verapamil crosses the placental barrier and is found in the blood of the umbilical vein during childbirth.
Verapamil and its metabolites are excreted in breast milk. The limited data available regarding the oral administration of Isoptin® indicate that the dose of verapamil given to infants with mother's milk is quite low (0.1-1% of the dose of verapamil taken by the mother), and the use of verapamil may be compatible with feeding breast. However, a risk to newborns and infants cannot be ruled out.

Given the possibility of serious side effects in infants, Isoptin® should be used during breastfeeding only if the benefit to the mother outweighs the potential risk to the baby.

Dosage and administration

Only intravenously.

Intravenous administration should be carried out slowly over at least 2 minutes with continuous monitoring of the ECG (electrocardiogram) and blood pressure.

In elderly patients and the introduction is carried out for at least 3 minutes to reduce the risk of unwanted effects.

Initial dose is 5-10 mg (0.075-0.15 mg / kg of body weight).

Repeat dose is 10 mg (0.15 mg / kg body weight), administered 30 minutes after the first injection with an inadequate response to the first injection.

Stability

Isoptin® is compatible with the most commonly used large volume parenteral solutions and is chemically stable in them for at least 24 hours at 25°C protected from light.

Before use, the parenteral dosage form should be evaluated visually for the presence of sediment and discoloration. Do not use if solution is cloudy or vial seal is broken.

The remaining unused solution should be destroyed immediately after taking a portion of the contents of any volume.

Incompatibility

In order to avoid compromising stability, it is not recommended to dilute Isoptin® with sodium lactate solutions for injection in polyvinyl chloride bags. Mixing with solutions of albumin, amphotericin B, hydralazine hydrochloride or trimethoprinem and sulfamethoxazole should be avoided.

Verapamil precipitates in any solution with a pH greater than 6.0.

Side effect

Side effects identified during clinical trials and post-marketing use of the drug Isoptin® are presented below by organ systems and the frequency of their occurrence in accordance with the WHO classification: very often (> 1/10); often (from? 1/100 to<1/10); нечасто (от?1/1000 до <1/100); редко (от?1/10000 до <1/1000); очень редко (<1/10000); частота неизвестна (невозможно определить на основании доступных данных).

The following side effects were most often observed: headache, dizziness, nausea, constipation, abdominal pain, bradycardia, tachycardia, palpitations, a pronounced decrease in blood pressure, flushing of blood to the skin of the face, peripheral edema and increased fatigue.

Immune system disorders:

frequency unknown: hypersensitivity.

Metabolic and nutritional disorders:

frequency unknown: hyperkalemia.

Mental disorders:

rarely: drowsiness.

Nervous system disorders:

often: dizziness, headache;

rarely: paresthesia, tremor;

frequency unknown: extrapyramidal disorders, paralysis (tetraparesis) 1, convulsive seizures.

Hearing disorders and labyrinth disorders:

rarely: tinnitus;

frequency unknown: twitches.

Heart disorders:

often: bradycardia;

infrequently: palpitations, tachycardia;

frequency unknown: AV blockade I, II, III degree; heart failure, sinus arrest ("sinus arrest"), sinus bradycardia, asystole.

Vascular disorders:

often: "flushing" of blood to the skin of lime, a pronounced decrease in blood pressure.

Respiratory, thoracic and mediastinal disorders:

frequency unknown: bronchospasm, shortness of breath.

Gastrointestinal disorders:

often: constipation, nausea;

infrequently: abdominal pain;

rarely: vomiting;

frequency unknown: abdominal discomfort, gingival hyperplasia, intestinal obstruction.

Skin and subcutaneous tissue disorders:

rarely: hyperhidrosis;

frequency unknown: angioedema, Stevens-Johnson syndrome, erythema multiforme, alopecia, pruritus, pruritus, purpura. maculopapular rash, urticaria.

Musculoskeletal and connective tissue disorders:

frequency unknown: arthralgia, muscle weakness, myalgia.

Renal and urinary tract disorders:

frequency unknown: renal failure.

Genital and breast disorders:

frequency unknown: erectile dysfunction, galactorrhea, gynecomastia.

General disorders:

often: peripheral edema;

infrequently: increased fatigue.

Laboratory and instrumental data:

frequency unknown: increased concentration of prolactin, increased activity of liver enzymes.

1 - during the period of post-registration use of Isoptina®, a single case of paralysis (tetraparesis) associated with the combined use of verapamil and colchicine was reported. This could be due to the penetration of colchicine through the blood-brain barrier due to the suppression of the activity of the CYP3A4 isoenzyme and P-glycoprotein under the action of verapamil (see section "Interaction with other drugs").

Overdose:

Symptoms: pronounced decrease in blood pressure; bradycardia, turning into AV blockade and stopping the activity of the sinus node ("sinus arrest"); hyperglycemia, stupor and metabolic acidosis. There are reports of deaths due to overdose.

Treatment: supportive symptomatic therapy should be carried out. For clinically significant hypotensive reactions or AV block, vasopressor drugs or pacing should be given, respectively. Asystole should be treated with beta-adrenergic stimulation (isoprenaline), other vasopressor drugs, or resuscitation. Hemodialysis is ineffective.

Interaction

In patients with severe cardiomyopathy, chronic heart failure, or after a myocardial infarction, the simultaneous administration of verapamil and intravenous beta-blockers or disopyramide in rare cases led to the development of serious adverse events.

The simultaneous use of intravenous verapamil with drugs that suppress adrenergic function may lead to an increase in the antihypertensive effect.

Metabolic Research in vitro testify that
Verapamil is metabolized by the action of cytochrome P450 isoenzymes CYP3A4, CYP1A2, CYP2C8, CYP2C9 and CYP2C18.

Verapamil is an inhibitor of the CYP3A4 isoenzyme and P-glycoprotein. A clinically significant interaction was noted with simultaneous use with inhibitors of the CYP3A4 isoenzyme, while an increase in the concentration of verapamil in the blood plasma was observed, while inducers of the CYP3A4 isoenzyme reduced the concentration of verapamil in the blood plasma. With the simultaneous use of such drugs, the possibility of this interaction should be considered.

The table below provides data on possible drug interactions due to pharmacokinetic parameters.

Possible interactions associated with the CYP-450 isoenzyme system
A drug	Possible drug interaction	Comment
Alpha blockers
Prazosin	An increase in C m ax of prazosin (~40%) does not affect T 1/2 of prazosin.	Additional antihypertensive action.
Terazosin	An increase in the AUC of terazosin (-24%) and C m ax (~ 25%).
Antiarrhythmic drugs
Flecainide	Minimal effect on plasma clearance of flecainide (<~10 %); не влияет на клиренс верапамила в плазме крови.
	Decreased oral clearance of quinidine (~35%).	Pronounced decrease in blood pressure. Pulmonary edema may occur in patients with hypertrophic obstructive cardiomyopathy.
Means for the treatment of bronchial asthma
Theophylline	Decreased oral and systemic clearance (~20%).	Decreased clearance in smoking patients (~11%).
Anticonvulsants / antiepileptics
Carbamazepine	Increased AUC of carbamazepine (~46%) in patients with sustained partial epilepsy.	An increase in the concentration of carbamazepine, which can lead to the development of such side effects of carbamazepine as diplopia, headache, ataxia or dizziness.
Phenytoin	Decreased plasma concentrations of verapamil.
Antidepressants
Imipramine	Increase in AUC of imipramine (~15%).	Does not affect the concentration of the active metabolite, desipramine.
Hypoglycemic agents
Glibenclamide	An increase in C m ax of glibenclamide (-28%), AUC (~26%).
Antigout agents
Colchicine	Increase in AUC of colchicine (~ 2.0 times) and C m ah (~ 1.3 times).	Reduce the dose of colchicine (see instructions for use of colchicine).
Antimicrobials
Clarithromycin
Erythromycin	An increase in the concentration of verapamil is possible.
Rifampicin	Decreased AUC (~97%), Cmax (~94%), bioavailability (~92%) of verapamil.
Telithromycin	An increase in the concentration of verapamil is possible.
Anticancer drugs
Doxorubicin	An increase in AUC (104%) and C m ax (61%) of doxorubicin.	In patients with small cell lung cancer.
Barbiturates
Phenobarbital	Increase in oral clearance of verapamil ~ 5 times.
Benzodiazepines and other tranquilizers
Buspirone	Increase in AUC and C m ah buspirone ~ 3.4 times.
Midazolam	Increase in AUC (~ 3 times) and Cmax (~ 2 times) of midazolam.
Beta blockers
metoprolol	An increase in AUC (-32.5%) and Cmax (-41%) of metoprolol in patients with angina pectoris.	See section "Special Instructions".
propranolol	An increase in AUC (-65%) and C m ax (-94%) of propranolol in patients with angina pectoris.
cardiac glycosides
Digitoxin	Decreased total clearance (-27%) and extrarenal clearance (-29%) of digitoxin.
Digoxin	An increase in C m ax (by -44%), C 12 h (by -53%), C ss (by -44%) and AUC (by -50%) of digoxin in healthy volunteers.	Reduce the dose of digoxin. See section "Special Instructions".
H 2 receptor antagonists
Cimetidine	An increase in the AUC of R- (-25%) and S- (-40%) verapamil with a corresponding decrease in the clearance of R- and S-verapamil.
Immunological/immunosuppressive agents
Cyclosporine	Increase in AUC, C ss , C max (by - 45%) of cyclosporine.
everolimus	Everolimus: increase in AUC (~ 3.5 times) and Cmax (~ 2.3 times) Verapamil: increase in Chough (the concentration of the drug in the blood plasma immediately before taking its next dose) (~ 2.3 times).	It may be necessary to determine the concentration and titrate the dose of everolimus.
Sirolimus	Increase in AUC of sirolimus (~ 2.2 times); increase in AUC S-verapamil (~ 1.5 times).	It may be necessary to determine the concentration and titrate the dose of sirolimus.
Tacrolimus	An increase in the concentration of tacrolimus is possible.
Lipid-lowering agents (HMG-CoA reductase inhibitors)
Atorvastatin	It is possible to increase the concentration of atorvastatin in the blood plasma, an increase in the AUC of verapamil - 43%.	Additional information is provided below.
Lovastatin	It is possible to increase the concentration of lovastatin and the AUC of verapamil (~ 63%) and C m ax (~ 32%) in plasma
Simvastatin	Increase in AUC (~ 2.6 times) and C m ah (~ 4.6 times) of simvastatin.
Serotonin receptor agonists
Almotriptan	Increase in AUC (~20%) and C m ah (~24%) of almotriptan.
Uricosuric agents
Sulfinpyrazone	An increase in oral clearance of verapamil (~ 3 times), a decrease in its bioavailability (~ 60%).	The antihypertensive effect may decrease.
Other
Grapefruit juice	An increase in AUC R- (~ 49%) and S- (~ 37%) of verapamil and C m x R- (~ 75%) and S-C-51%) of verapamil.	T 1/2 and renal clearance did not change. Grapefruit juice should not be taken with verapamil.
St. John's wort	A decrease in AUC R- (~ 78%) and S- (~ 80%) of verapamil with a corresponding decrease in C m ax.

Other drug interactions

Antiviral drugs for the treatment of HIV infection

Ritonavir and other antiviral drugs for the treatment of HIV infection can inhibit the metabolism of verapamil, which leads to an increase in its concentration in blood plasma. Therefore, with the simultaneous use of such drugs and verapamil, care should be taken or the dose of verapamil should be reduced.

Lithium

An increase in lithium neurotoxicity was observed during the simultaneous administration of verapamil and lithium in the absence of changes or an increase in the concentration of lithium in the blood serum. However, the addition of verapamil also led to a decrease in serum lithium concentrations in patients taking oral lithium for a long time. With the simultaneous use of these drugs, careful monitoring of patients is necessary.

Drugs that block neuromuscular conduction

Clinical data and preclinical studies suggest that
verapamil may potentiate the effect of drugs that block neuromuscular conduction (such as curariform and depolarizing muscle relaxants). Therefore, it may be necessary to reduce the dose of verapamil and / or the dose of drugs that block neuromuscular conduction, while using them simultaneously.

Acetylsalicylic acid (as an antiplatelet agent)

Increased risk of bleeding.

Ethanol (alcohol)

Increasing the concentration of ethanol in the blood plasma and slowing down its excretion. Therefore, the effect of ethanol can be enhanced.

HMG-CoA inhibitors - reductases (statins)

Patients receiving
verapamil, treatment with HMG-CoA reductase inhibitors (i.e., simvastatin, atorvastatin, or lovastatin) should be started at the lowest possible dose, which is then increased. If it is necessary to assign
Verapamil patients already receiving HMG-CoA reductase inhibitors should be reviewed and their doses reduced according to the concentration of cholesterol in the blood serum.

fluvastatin,
pravastatin and
rosuvastatin is not metabolized by CYP3A4 isoenzymes, so their interaction with verapamil is less likely.

Plasma protein-binding agents

Verapamil, as a highly protein-binding agent, should be used with caution when taken concomitantly with other drugs with a similar ability.

Means for inhalation general anesthesia

With the combined use of drugs for inhalation anesthesia and blockers of "slow" calcium channels, which include
verapamil, the dose of each agent should be carefully titrated until the desired effect is achieved in order to avoid excessive oppression of the cardiovascular system.

Antihypertensives, diuretics, vasodilators

Enhancement of antihypertensive action.

cardiac glycosides

Verapamil for intravenous administration was used in conjunction with cardiac glycosides. Because these drugs slow AV conduction, patients should be monitored for early detection of AV block or severe bradycardia.

Quinidine

Intravenous verapamil has been administered to a small group of patients receiving
quinidine inside. There are several reports of cases of a pronounced decrease in blood pressure when quinidine is taken orally and verapamil intravenously, so this combination of drugs should be used with caution.

Flecainide

A study involving healthy volunteers showed that the combined use of verapamil and flecainide may have an additive effect with a decrease in myocardial contractility, slowing of AV conduction and myocardial repolarization.

Disopyramide

Before receiving data on a possible interaction between verapamil and disopyramide, disopyramide should not be prescribed 48 hours before or 24 hours after the use of verapamil (see section "Contraindications").

Beta blockers

Verapamil for intravenous administration was prescribed to patients receiving oral beta-blockers. The possibility of adverse interactions must be considered, since both drugs can reduce myocardial contractility or AV conduction. The simultaneous administration of verapamil and intravenous beta-blockers has led to the development of serious adverse reactions, especially in patients with severe cardiomyopathy, chronic heart failure or after myocardial infarction (see section "Contraindications").

Special instructions:

Rarely, life-threatening side effects may develop (atrial fibrillation / flutter with a high ventricular rate, with the presence of additional pathways, severe arterial hypotension or severe bradycardia / asystole).

Acute myocardial infarction

Isoptin® should be used with caution in patients with acute myocardial infarction complicated by bradycardia, severe hypotension or left ventricular dysfunction.

Heart block / AV block I degree / Bradycardia / A systole

Verapamil affects the AV and SA nodes and slows down AV conduction. The drug Isoptin® should be used with caution, since the development of AV block II or III degree (see section "Contraindications") or single-beam, two-beam or three-beam blockade of the His bundle legs requires discontinuation of verapamil and appropriate therapy if necessary.

Verapamil affects the AV and SA nodes and, in rare cases, can cause second or third degree AV block, bradycardia, and, in extreme cases, asystole. These events are most likely in patients with sick sinus syndrome, which is more common in older patients.

Asystole in patients without sinus node weakness is usually brief (several seconds) with spontaneous return to atrioventricular or normal sinus rhythm. If sinus rhythm is not restored in a timely manner, appropriate treatment should be instituted immediately.

Beta-blockers and antiarrhythmics

Mutual strengthening of the effect on the cardiovascular system (high-degree AV blockade, a significant decrease in heart rate, exacerbation of heart failure and a pronounced decrease in blood pressure). Asymptomatic bradycardia (36 beats/min) with rhythm migration along the atrium was observed in a patient taking
timolol (beta-blocker) in the form of eye drops and
verapamil inside.

Digoxin

In the case of simultaneous administration of verapamil with digoxin, the dose of digoxin should be reduced. See section "Interaction with other drugs".

Heart failure

Patients with heart failure and a left ventricular ejection fraction of more than 35% should be stable before starting Isoptin® and should be treated appropriately thereafter.

Pronounced decrease in blood pressure

Intravenous administration of the drug Isoptin® often causes a decrease in blood pressure below baseline values, usually transient and asymptomatic, but may be accompanied by dizziness.

HMG-CoA reductase inhibitors (statins)

See section "Interaction with other drugs".

Neuromuscular Transmission Disorders

Isoptin® should be used with caution in patients with diseases affecting neuromuscular transmission (myasthenia gravis, Lambert-Eaton syndrome, Duchenne muscular dystrophy).

Impaired kidney function

Conducted comparative studies demonstrate that the pharmacokinetics of verapamil remains unchanged in patients with end-stage renal disease. However, some reports suggest that Isoptin should be used with caution and under close supervision in patients with impaired renal function.
Verapamil is not excreted by hemodialysis.

Impaired liver function

Isoptin should be used with caution in patients with severe hepatic impairment.

Ventricular tachycardia

Intravenous administration of the drug Isoptin® to patients with ventricular tachycardia with wide QRS complexes (> 0.12 sec.) Can lead to a pronounced deterioration in hemodynamics and ventricular fibrillation. Before starting treatment, proper diagnosis and exclusion of wide QRS ventricular tachycardia is mandatory.

Influence on the ability to drive a vehicle:

The drug Isoptin® can affect the speed of psychomotor reactions due to the antihypertensive effect and as a result of individual sensitivity. During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions. This is especially important at the beginning of treatment, when increasing the dose or when switching from therapy with another drug.

Release form:

Solution for intravenous administration, 5 mg/2 ml.

Package:

2 ml in colorless type I hydrolytic glass ampoules with a blue break point.

5, 10 or 50 ampoules in a cardboard tray or PVC or polystyrene blister, closed with paper foil, together with instructions for use in a cardboard box.

Storage conditions:

Store at a temperature not exceeding 25 °C.

Keep out of the reach of children.

Best before date:

Do not use after the expiry date stated on the package.

Conditions for dispensing from pharmacies:

On prescription

Registration certificate holder:

Registration Authorization Holder: Abbott GmbH & Co. KG

Manufacturer

EBEWE PHARMA, Ges.m.b.H.Nfg.KG Austria
EBEWE PHARMA GmbH Nfg KG. Austria Representation: ABBOTT LABORATORIES LLC

Isoptin (amp.5mg-2ml N5) Austria Abbott Laboratories [Germany] produced by Ebewe F

Description of the active substance (INN) Verapamil.

Pharmacology : pharmachologic effect - antianginal, hypotensive, antiarrhythmic . It blocks calcium channels (acts from the inside of the cell membrane) and lowers the transmembrane calcium current.

Indications : Paroxysmal supraventricular tachycardia (except for WPW syndrome), sinus tachycardia, atrial extrasystole, atrial fibrillation and flutter, angina pectoris (including Prinzmetal, tension, post-infarction), arterial hypertension, hypertensive crisis, idiopathic hypertrophic subaortic stenosis, hypertrophic cardiomyopathy.

Contraindications : Hypersensitivity, severe hypotension, cardiogenic shock, II and III degree AV block, myocardial infarction (acute or recent and complicated by bradycardia, hypotension, left ventricular failure), chronic heart failure stage III, WPW syndrome and sick sinus syndrome (if not implanted pacemaker), sinoatrial blockade, Morgagni-Adams-Stokes syndrome, digitalis intoxication, severe aortic stenosis, pregnancy, breast-feeding.

Application restrictions : AV blockade of the I degree, chronic heart failure of the I and II stages, severe bradycardia (less than 50 bpm), mild or moderate hypotension, severe myopathy (Duchenne syndrome), abnormal liver or kidney function, ventricular tachycardia with a wide QRS complex (for in / in the conduct).

Use during pregnancy and lactation : Contraindicated in pregnancy. At the time of treatment should stop breastfeeding.

Side effects : From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): hypotension, bradycardia (sinus), AV blockade, heart failure.

From the nervous system and sensory organs: headache, dizziness, nervousness, lethargy, drowsiness, weakness, fatigue, paresthesia.

From the digestive tract: nausea, dyspepsia, constipation; rarely - gingival hyperplasia, increased activity of hepatic transaminases, alkaline phosphatase.

Allergic reactions: skin rash, urticaria, pruritus; rarely - angioedema, Stevens-Johnson syndrome.

Others: flushing of the skin of the face, bronchospasm (with intravenous administration), peripheral edema, very rarely - gynecomastia, increased secretion of prolactin (separate cases).

Interaction : Increases plasma levels of digoxin, cyclosporine, theophylline, carbamazepine, reduces - lithium. Weakens the antibacterial activity of rifampicin, the depriming effect of phenobarbital, the clearance of metoprolol and propranolol, enhances the effect of muscle relaxants. Rifampicin, sulfinpyrazone, phenobarbital, calcium salts, vitamin D - weaken the effect. The hypotensive effect is enhanced by antihypertensive drugs (diuretics, vasodilators), tricyclic and tetracyclic antidepressants and antipsychotics: antianginal - nitrates. Beta-blockers, class IA antiarrhythmics, cardiac glycosides, inhalation anesthetics, radiopaque agents potentiate (mutually) inhibitory effect on the automatism of the sinoatrial node, AV conduction and myocardial contractility. With simultaneous use with acetylsalicylic acid - increased existing bleeding. Cimetidine increases plasma levels of verapamil.

Overdose : Symptoms: arterial hypotension, bradycardia, AV blockade, cardiogenic shock, coma, asystole.

Treatment: as a specific antidote, calcium gluconate is used (10-20 ml of a 10% solution in / in); with bradycardia and AV blockade, atropine, isoprenaline or orciprenaline are administered; with hypotension - plasma-substituting solutions, dopamine, norepinephrine; with the manifestation of signs of heart failure - dobutamine.

Dosage and administration : Inside, during or immediately after a meal, drinking plenty of fluids.

angina pectoris - 80-120 mg 3 times a day, against the background of impaired liver function, in old age - 40 mg 3 times a day.

Arrhythmias- in chronic atrial fibrillation during therapy with cardiac glycosides - 240-320 mg / day in 2-3 doses; for the prevention of paroxysmal supraventricular tachycardia - 240-480 mg / day in 2-3 doses.

hypertension - 80 mg 3 times a day, if necessary - up to 360 mg / day; elderly patients or short stature - 40 mg 3 times a day; children under 6 years old - 40-60 mg / day, 6-14 years old - 80-360 mg / day in 3-4 doses. In the form of dosage forms of prolonged action for hypertension - 180-240 mg / day once in the morning; with insufficient effectiveness, the dose is increased as follows: 240 mg in the morning, then 180 mg in the morning + 180 mg in the evening (possibly 240 mg in the morning + 120 mg in the evening) and then 240 mg 2 times a day with an interval of 12 hours, for elderly or small patients - 120 mg; in the absence of an adequate effect after a dose of 120 mg, it is successively increased to 180, 240, 360 and 480 mg once in the morning.

For angina pectoris and arrhythmias: in the form of retard forms of 120-240 mg 2 times a day with an interval of 12 hours. Tablets of 200 mg: 1 tab. 1-2 times a day or 2 tablets. 1 time per day.

Dosage forms of 24-hour controlled release (taken orally only as a whole) - for hypertension, 180 mg once a night; if necessary, the dose is sequentially increased to 240 mg at night, 360 mg (2 tablets of 180 mg) at night and then 480 mg (2 tablets of 240 mg) at night.

In / in slowly: for adults, the initial dose is 5-10 mg (for at least 2 minutes), with insufficient effect, it is possible to re-administer after 30 minutes at a dose of 10 mg. Children under 1 year under ECG control at a dose of 0.1-0.2 mcg / kg (usually a single dose is 0.75-2 mg), for at least 2 minutes, children 1-15 years old at a dose of 0.1- 0.3 mg/kg for at least 2 minutes (usually a single dose is not more than 2-5 mg). With a hypertensive crisis - 5-10 mg intravenously slowly.

Precautionary measures : Precautions are prescribed to patients with hypertrophic cardiomyopathy complicated by left ventricular obstruction, high wedge pressure in the pulmonary capillaries, paroxysmal nocturnal dyspnea or orthopnea, dysfunction of the sinoatrial node. When administered to patients with severe impairment of liver function and neuromuscular transmission (Duchenne myopathy), constant medical supervision and, possibly, dose reduction are necessary. It is recommended to use with caution during work for drivers of vehicles and people whose profession is associated with increased concentration of attention (reaction speed decreases), it is recommended to exclude alcohol.

special instructions : The injection form is incompatible with albumin, injection forms of amphotericin B, hydralazine, sulfamethoxazole, trimethoprim and may precipitate in solution with a pH above 6.0.

Calcium channel blockers are one of the less common, but very effective types of drugs for the treatment of hypertension. They do not affect the renin-angiotensin-aldosterone system, but at the same time contribute to vasodilation. And this effect is achieved by reducing the flow of calcium into smooth muscle tissues.

Inhibitors of this type do not bind directly to calcium. They interact with L-type channels, which just ensure the penetration of Ca2 into the cells of smooth muscle tissues. Due to this action of drugs of this type, vascular tone decreases, pressure decreases, the load on the heart decreases and the intensity of the heartbeat normalizes. Thus, calcium antagonists not only have a pronounced hypotensive effect, but also eliminate the symptoms of angina pectoris. It is interesting that initially such funds were used specifically for the second problem.

The well-known Isoptin Retard also belongs to potassium antagonists. It is used in cases where the use of funds aimed at blocking angiotensin-2 is undesirable.

General description of the drug

Isoptin is a drug that belongs to calcium channel antagonists. It has a direct effect on the heart and contains in its composition the active substance, which is a derivative of phenylalkylamine.

Thus, the described medicine can be used not only for the treatment of hypertension, but also for the fight against certain heart diseases. At the same time, Isoptin is used most often as "cores".

The active ingredient of Isoptin is. This substance belongs to papaverine derivatives. And it was this name that bore the first remedy related to calcium channel blockers.

The drug has a prolonged action and is excreted from the body for a long time. At the same time, depending on the individual characteristics of the organism and the disease for which Isoptin is prescribed, it can be taken either once or twice a day.

Forms of release, terms of sale and storage of the drug:

1. The tool has two forms of release. It is sold in the form of tablets and ampoules for injection. The list of additional ingredients that make up the drug depends on this factor.
2. The calcium channel blocker is available by prescription. Only with the permission of a specialist can you take this remedy.
3. The shelf life of Isoptin in tablets is three years from the date of issue, and in ampoules - 5 years. After this time has elapsed, the tool becomes unsafe to use.
4. Store the drug at room temperature out of the reach of children. It also needs to be protected from sunlight.
5. Produces a medicine with the same name Germany and Greece.

Release forms

This medicine is sold in the form of ampoules with a solution for injections and in the form of tablets. Such forms differ not only in their application, but also in the amount of active ingredient in one serving, and in the list of additional ingredients.

Isoptin release forms:

1. Isoptin tablets are available in dosages of 40, 80, 120 and 240 mg. They are white or green in color, and round, convex on both sides, shape. On one side of each tablet there is an engraving with the dosage of the active substance in the composition, and on the other - the emblem of the manufacturer or the name of the drug. Separation risk is available on each serving of the drug. As additional ingredients, the composition contains: calcium hydrogen phosphate dihydrate, sodium croscarmellose, microcrystalline cellulose, colloidal silicon dioxide, magnesium stearate, titanium dioxide, sodium lauryl sulfate, macrogol, talc.
2. Isoptin in 2 ml ampoules contains 5 mg of the working ingredient. Has no color and smell. As additional components are used: hydrochloric acid, saline, sodium chloride.

Tablets are sold in plastic blisters of 10 pcs. One carton can contain from 1 to 10 plates with tablets.

5, 10 or 50 ampoules are placed in plastic trays. One package includes one tray with the drug.

Pharmacology Isoptin

Verapamil blocks slow-type channels through which calcium enters smooth muscle tissues, as well as heart cells. To some extent, this drug can slow down the flow of sodium into the tissues.

When calcium is blocked by Isoptin, AV conduction also decreases. At the same time, the refractory period in the AV node increases, equating to the intensity of contractions of the heart muscle.

This reduces the intensity of ventricular contractions. This greatly facilitates the condition of patients suffering from arrhythmia.

Also, the drug is useful for supraventricular tachycardia. It normalizes sinus rhythm by blocking the secondary input of excitation in the atrioventricular node.

The drug has a positive effect on damaged fibers of the atrial muscle, reducing the intensity of conduction, depolarization and amplitude in them. At the same time, it does not affect the conduction parameters inside the ventricles, does not change the normal potential of the atrial work, and does not block the work of the auxiliary pathways.

The drug significantly reduces myocardial oxygen demand, by influencing some processes in this organ that require additional energy. Also acting indirectly, it reduces the load on the heart.

It is worth noting the antihypertensive qualities of the drug. The decrease in pressure occurs due to the relaxation of spasmodic muscles. In this case, the heart rate does not change.

In most cases, in the presence of cardiac pathologies, the negative inotropic effect of Isoptin is compensated by reducing the load on this organ. Therefore, usually an increase in the cardiac index is not observed.

However, there are cases of acute decompensation of the disease in patients with severe and moderate chronic heart failure.

Pharmacokinetics of the drug

The active substance of Isoptin, verapamil, is a racemic substance, which is formed from S and R enantiomers. It is metabolized in the liver to form 12 compounds. Most of them do not have a pronounced therapeutic activity. Only one of the metabolites, which is called norverapamil, has a 20% potency (compared to the potency of the active ingredient unchanged). The effectiveness of this metabolite has been determined by conducting experiments on dogs.

The agent is quickly and almost completely absorbed from the intestine into the blood. This indicator is not affected by the time of eating.

With the initial intake of Isoptin, the bioavailability of verapamil is equal to 22%. With repeated use of the tool, this figure doubles. Food intake also has no effect on bioavailability.

The maximum concentration of unchanged active substance is reached approximately one hour after its administration. At the same time, the largest amount of its main active metabolite is found. At this time, the maximum effectiveness of the remedy is usually noted.

The level of distribution of verpalamine is quite high. It can reach from 1.6 to 6.8 liters per kilogram.

The active substance of the drug and its metabolite are 90% combined with blood elements. Therefore, with its overdose, hemodialysis is ineffective.

The half-life of the drug can last up to 7 hours. In this case, the excretion of 50% of the dose taken through the kidneys is observed during the day, and the rest of the drug is removed from the body in five days. At the same time, only 16% of the total volume of the drug is found in the feces.

In the elderly and patients with pathological liver function, an increase in the half-life of the drug is observed. However, this does not affect its therapeutic properties.

The principle of operation of the tool

Calcium channel blockers, unlike many other antihypertensive drugs, do not affect the hormones that cause vasoconstriction. They provide pressure reduction and a positive effect on the heart through a different mechanism of action.

The principle of action of Isoptin:

1. The drug blocks the transmembrane Ca flow into vascular smooth muscle tissues and into myocardial cardiomyocytes. It is calcium ions that increase excitability, conductivity and intensity of metabolic processes, as well as increase muscle contractility and myocardial oxygen demand. Therefore, with a decrease in the concentration of this substance, these indicators fall.
2. This reduces the load on the heart and myocardial contractility. It also normalizes the heart rate. This leads to a decrease in our body's "pump" for oxygen.
3. Also, when using the drug, an increase in the lumen in the coronary vessels occurs and spasm is removed from them. This also speeds up blood flow. This action extends even to those areas that were previously subject to stenosis.
4. The tone of the arteries of the peripheral type, as well as the overall vascular resistance, fall. Due to this, blood circulation is normalized and blood pressure is lowered.
5. At the same time, an increase in the vascular lumen does not cause an increase in heart rate.
6. In addition, the drug is able to slow down the passage of an impulse in the atrioventricular node, normalizing sinus rhythm and ventricular contractility. Thus, the antiarrhythmic effect of the drug is ensured.

Who is prescribed the medicine

Isoptin is used in a fairly wide range of cases. In this case, injections and tablets are usually used for different purposes.

What are the tablets used for?

1. Hypertension of the classical type. Basically, the remedy is used in the first and second stages of the development of this disease;
2. Supraventricular tachycardia of paroxysmal type;
3. Ischemia of the heart muscle and angina pectoris of various types;
4. Tachyarrhythmia, accompanied by flutter and atrial fibrillation.

Injections are used in two cases. And usually they are treated in a hospital.

What are injections used for?

1. Supraventricular tachycardia of paroxysmal type. The drug is used to normalize sinus rhythm.
2. Tachyarrhythmia, accompanied by flutter and atrial fibrillation. The drug is used to stabilize ventricular contractions.

Advantages and disadvantages of Isoptin

Isoptin is more commonly used to treat heart disease than to treat hypertension. However, in some cases, the use of the drug is necessary, especially if the patient is faced with several pathologies at once, in which the drug is prescribed.

It is worth noting that the drug Isoptin has a fairly extensive list of advantages. Therefore, cardiologists often prescribe it to their patients.

Advantages of Isoptin:

1. It has a fairly wide range of activities. Isoptin has antianginal, antiarrhythmic and hypotensive effects.
2. It is prescribed for a wide range of diseases. This is especially useful if hypertension is combined with arrhythmia, angina pectoris or tachycardia.
3. Available in ampoules and injections.
4. Has a long-term effect. After taking the drug will act within a day. Therefore, it is usually prescribed only once a day.
5. The effectiveness of the drug is not affected by the age, race and gender of the patient. Also, these indicators do not depend on the level of renin in the blood.
6. Influencing the conductivity of calcium in smooth muscle tissue, Isoptin does not change its concentration in the body. Therefore, patients taking this drug do not experience a deficiency of this substance.
7. The speed of action and effectiveness of the drug does not change with food intake. Therefore, it can be consumed both before meals and after it.
8. In most cases, the drug does not adversely affect the kidneys.

Despite the advantages, this calcium channel blocker has some disadvantages. And they also need to be taken into account.

Disadvantages of the drug:

1. Isoptin has a mild hypotensive effect. Therefore, in the later stages of hypertension, it will be useless.
2. In the presence of dysfunction of the heart muscle of a chronic type, Isoptin can provoke the transition of the disease to the acute stage of decompensation.
3. Calcium channel blockers cannot be combined with a fairly extensive list of medications. This group of drugs cannot be combined even with the use of certain fruits.
4. The drug has an extensive list of side effects. However, most of them occur quite rarely.

What negative phenomena can occur while taking Isoptin

Isoptin has many possible side effects. The risk of their occurrence, of course, is small, but still they must be taken into account when taking the drug.

Possible negative consequences of taking Isoptin:

Organ groups	Negative consequences of taking Isoptin
Nervous system	Chronic fatigue, sleep disturbances, paresthesia, paralysis, pain in the head, mood swings, dizziness, tremor of the limbs.
Heart and blood vessels	Acute hypotension, sinus node dysfunction, bradycardia, cardiac muscle dysfunction, flushing, bradycardia.
The immune system	Angioedema, urticaria, rash, allergic dermatitis, itching, redness of the skin.
Skin and fiber	Hyperhidrosis, erythema, purpura, Stevens-Johnson disease.
Respiratory system	Bronchial spasm, laryngeal edema, shortness of breath, cough.
Digestive organs	Dryness of the oral mucosa, pain in the abdomen, intestinal obstruction, loosening of the stool, fastening of the stool, vomiting, feeling of nausea, hyperplasia of the gums.
Muscles, bones and joints	Arthralgia, muscle spasms, arthralgia.
urinary tract	Kidney dysfunction.
Sex organs	Gynecomastia, impotence, galactorrhea.
Laboratory indicators	Hyperkalemia, an increase in the concentration of liver enzymes, an increase in the concentration of prolactin.
Other ailments	Fever, fatigue.

The described negative phenomena usually occur if the storage conditions of the drug were violated, there were contraindications to its use, or the dosage recommended by the doctor was exceeded. In any case, if such symptoms occur, you should immediately consult a specialist. He will find out what is the cause of the ailment and, if necessary, revise the treatment.

Who should not be treated with a calcium channel blocker

Isoptin can be used only with the permission of a doctor, because there are serious contraindications to the use of this medication.

In what cases is it forbidden to take Isoptin:

• The period of bearing a child;
• Negative reaction of the body to the components of the drug;
• Shock is cardiogenic;
• Lown-Ganong-Levin disease;
• Blockade of AV 1 and 2 severity (it is possible to use the drug in the presence of a special pacemaker);
• Sinus node dysfunction (the drug can also be used in the presence of a special pacemaker);
• Heart failure, with ventricular output values ​​up to 35, pulmonary wedging from 20 (the exception is those cases in which cardiac dysfunction is a consequence of supraventricular tachycardia);
• Wolff-Parkinson-White pathology;
• lactation period;
• Minor children.

Studies regarding the use of Isoptin during pregnancy have only been conducted in animals. During their course, no negative effect of the drug on the fetus was revealed, however, it was found that verapamil can penetrate the placenta. It is present in the blood of the umbilical vein of a newborn whose mother has taken this medicine.

Since experiments on rodents and dogs do not give an exact answer to the question of how safe the described medication is during pregnancy, it is not recommended to use it during this period. However, it is prescribed if it is vital for the mother.

The drug in small doses can pass into breast milk. And even this small amount of the drug can be enough to cause dangerous side effects in a child. Therefore, it is not recommended to combine breastfeeding and taking Isoptin.

Who needs to be especially careful when using

There are cases in which taking Isoptin is not contraindicated, but can be carried out only in case of urgent need and under the close supervision of a physician. Since in such situations the risk of developing serious side effects greatly increases.

When the drug should be taken with extreme caution:

• Atrioventricular blockade of the 1st degree;
• Hypotension;
• Left ventricular dysfunction;
• bradycardia;
• cardiomyopathy;
• asystole;
• liver dysfunction;
• severe kidney disease;
• problems with neuromuscular transmission;
• Age after 75 years.

Overdose of the drug

Isoptin should be taken according to the instructions for use. Exceeding the maximum allowable dose of this drug causes acute drug intoxication.

Symptoms of an overdose of Isoptin are usually very pronounced. At the same time, cases of death as a result of taking an excessively large dose of the drug are known.

Signs of an overdose of Isoptin:

• Acute hypotension;
• Stupor;
• Stopping the sinus node;
• Nausea and vomiting;
• hyperglycemia;
• AV block;
• bradycardia;
• metabolic acidosis;
• Death.

When taking an excessively large dose of the drug, it is urgent to wash the stomach and intestines. After that, an ambulance must be called.

Symptomatic therapy is used in the hospital. The patient may be prescribed pacemakers, vasopressor drugs, calcium preparations, beta-adrenergic stimulants. Various resuscitation measures may also be needed. Hemodialysis in this case is not effective.

Compatibility of Isoptin with other substances

Isoptin can be used not only as the only drug in the treatment. Sometimes it is included in the therapeutic complex in combination with other drugs. In this case, it is important to consider how the described calcium blocker behaves in tandem with other substances.

Interaction of Isoptin with other means:

Drug groups	Effects from their combination with Isoptin
Alpha blockers	Increasing the maximum concentration of the drug. Increasing the antihypertensive ability of the drug.
Antiarrhythmic drugs	Probable development of acute hypotension.
Anti-asthma medicines	An increase in the severity of the drug's action.
Antidiabetic drugs	An increase in the severity of the action of hypoglycemic agents. Hypoglycemia may develop.
Anti-gout medicines	Increasing the severity of the action of gout remedies. It is necessary to change their dosage.
Erythromycin, clarithromycin, telithromycin.	An increase in the hypotensive effect of Isoptin.
Rifampicin	Decreased hypotensive effect of Isoptin.
Doxorubicin	Increasing the severity of the action of an anticancer agent. Dose revision required.
Barbiturates	Increased oral clearance of the drug.
tranquilizers	Acute hypotension may develop.
Beta blockers	Increased antihypertensive effect of the drug. There is a high chance of dangerous side effects from the heart.
cardiac glycosides	The maximum concentration of glycosides increases. Doses need to be reviewed.
Immunological preparations	Increase in the maximum concentration of immunological drugs. Dose adjustment required.
Lipid-lowering drugs	Increase in the maximum concentration of lipid-lowering drugs. Their dosage needs to be adjusted.
Serotonin receptor blockers	Increase in the maximum concentration of serotonin receptors.
Uricosuric drugs	Decreased hypotensive ability of Isoptin
grapefruit juice	A significant increase in the concentration of Isoptin.
St. John's wort	The effectiveness of Isoptin decreases
Medicines for HIV infections	Increasing the maximum concentration of Isoptin. Dose adjustment required.
Products containing lithium	Perhaps the development of intoxication with lithium.
Muscle conduction inhibitors	An increase in the severity of the effectiveness of both types of funds. Their dose needs to be adjusted.
Aspirin	There may be bleeding.
Antihypertensive drugs	Strengthening the antihypertensive effect of all drugs used.
ethanol	Strengthening the negative effect of ethanol.

Instructions for use of the drug

Isoptin in the form of tablets is taken orally, regardless of the meal. It must be swallowed without chewing, drinking plenty of liquid.

The doctor selects the regimen for taking the drug individually for each patient, however, there are general positions for the use of this medication.

When treating with Isoptin, the dosage of the drug is usually increased gradually. The starting dosage is 80 mg of the drug once a day. After a week of taking the remedy, in the absence of the desired effect, this amount can be doubled. The recommended daily dose is 240-360 mg of the drug. This amount of medicine can be divided into 2 doses.

The maximum dose of Isoptin is 480 mg. However, this amount of funds can be taken only in a hospital under the supervision of a doctor.

Patients with pathologies of the liver and people after 70 years of age should start treatment with 40 mg. In most cases, this dosage is enough.

Patients with liver and kidney disease should take the drug with extreme caution.

What else you need to know for those who take Isoptin

Even following the instructions for the use of Isoptin, you need to take into account some of the nuances associated with it. Only in this case, the treatment will be as effective and safe as possible.

Tips for using the tool:

1. Isoptin cannot be combined with grapefruit juice. Otherwise, the concentration of the drug may increase up to 70%. Thus, taking the medicine in the correct dosage along with this product, the patient may experience symptoms of intoxication.
2. Experts recommend taking Isoptin during or immediately after a meal. This will help reduce its negative impact on the stomach.
3. When taking Isoptin, you can use hemodialysis. The effectiveness of the drug in this case will not be reduced.
4. Reception of Isoptin cannot be combined with the use of alcohol. In this case, the negative effect of ethyl alcohol on the body will increase significantly.
5. It is advisable to take the drug at the same time. This will ensure its maximum efficiency and safety.

One tablet of Isoptin SR 240 contains 240 mg verapamil hydrochloride .

Additional substances: povidone K30, microcrystalline cellulose, sodium alginate, magnesium stearate, water.

Coating composition: aluminum varnish, hypromellose, macrogol 6000, macrogol 400, talc, titanium dioxide, glycol wax.

Release form

Light green long-acting tablets, oblong in shape, transverse serifs on both sides, two symbols in the form of a triangle are engraved on one edge.

pharmachologic effect

Antiarrhythmic, antianginal and antihypertensive action.

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

Belongs to a group calcium channel blockers . Suppresses transmembrane ion transport calcium in vascular cells and smooth myocytes of the myocardium. It has antiarrhythmic, antianginal and antihypertensive effects.

Antihypertensive the effect of the drug is due to a weakening of the resistance of peripheral vessels without a reflex increase in heart rate. The pressure begins to decrease already on the first day of therapy and this effect is maintained during long-term therapy. Isoptin SR 240 is used for the treatment of all types: in combination with other antihypertensive drugs (diuretics and ACE inhibitors ) renders vasodilator, negative inotropic and chronotropic action; in the form of monotherapy compensated arterial hypertension .

Antianginal the action is associated with an effect on hemodynamics and the myocardium (lowers the tone of the arteries of the peripheral type, the resistance of the walls of the vessels). Inhibition of ion transport calcium inside the cell causes a decrease in energy transformation ATP in mechanical work and weakening of myocardial contractility.

The drug also has a strong antiarrhythmic action, mainly supraventricular . Inhibits nerve impulse conduction AV node restoring normal sinus rhythm. The normal frequency of myocardial contractions does not change or decreases slightly.

Pharmacokinetics

Absorbed quickly and completely (90-92%) in the small intestine. The average bioavailability is 22% in healthy individuals, in patients with cardiac pathology it can reach 35%.

Binding to blood proteins by 90%. The drug is able to cross the placenta and be excreted in breast milk. Metabolized almost completely in the liver. Main – norverapamil is active, other metabolites are inactive.

The half-life is 4-6 hours after a single dose. They are excreted mainly in the urine. Up to 16% is evacuated with feces.

Indications for use

Indications for use Isoptin SR 240:

• voltage;
• arterial hypertension;
• angina pectoris caused by vasospasm;
• atrial fibrillation on the background tachyarrhythmias (Besides );
• supraventricular paroxysmal.

Contraindications

Absolute contraindications:

• complicated ( hypotension, bradycardia, left ventricular failure );
• sinoatrial blockade;
• bradycardia-tachycardia syndrome;
• cardiogenic shock;
• AV block second or third degree.

Relative contraindications:

• arterial hypotension;
• AV block first degree;
• bradycardia;
• atrial fibrillation on the background WPW syndrome;
• heart failure.

Side effects

• Circulatory reactions: , AV blockade, tachycardia , sensation of heartbeat, aarterial hypotension , enhancement of features heart failure.
• Reactions of nervous activity:, fatigue, nervousness,.
• Digestive reactions: vomiting, nausea, intestinal obstruction, abdominal pain, increased levels of hepatic reversible gingival hyperplasia.
• Reactions from the musculoskeletal system: pain in muscles and joints.
• Allergic reactions: exanthema, Stevens-Johnson syndrome.
• Reactions from the hormonal sphere: an increase in the level prolactin, galactorrhea , reversible gynecomastia, .
• Other reactions: erythromelalgia , , tides .

Instructions for use Isoptin SR 240 (Method and dosage)

Instructions for use Isoptin SR 240 indicates that the average dose of the drug is 240-360 mg per day. With prolonged treatment, it is not recommended to exceed a dose of 480 mg per day. Tablets should be taken during or immediately after a whole meal with water.

At arterial hypertension appoint 240 mg of the drug once a day in the morning. If a slow decrease in pressure is necessary, it is recommended to start treatment with 120 mg once a day in the morning.

At ischemic heart disease (exertional angina, Prinzmetal's angina ) the drug is prescribed 120-240 mg twice a day (morning and evening).

At supraventricular paroxysmal tachycardia or atrial fibrillation on the background tachyarrhythmias the drug is prescribed 120-240 mg twice a day.

In case of violation of the liver, treatment with the drug should begin with low doses of 40 mg twice a day.

The duration of treatment with the drug is not limited.

Overdose

Symptoms of an overdose of the drug depend on the dose of the drug taken, the time of the implementation of detoxification measures and the ability of the myocardium to contract. There are reports of fatal cases of overdose.

Signs: pressure drop , shock, AV block , loss of consciousness, slipping rhythm, sinus bradycardia , cardiac arrest.

Treatment: gastric lavage, reception emetic and laxatives . If necessary, perform artificial respiration, closed heart massage and electrical stimulation of the heart.

Terms of sale

Purchase is possible only by prescription.

Storage conditions

Store in its original packaging at temperatures up to 24 degrees. Keep away from children

Best before date

Three years.

special instructions

There may be individual reactions to the drug that lead to a decrease in the ability to control mobile mechanisms.

Analogues

Coincidence in the ATX code of the 4th level:

Analogues Isoptin SR 240: Hydrochloride, Verapamil Darnitsa, Verogalid ER 240, Izoprtin SR,.

children

There are no studies that confirm the safety of the use of the drug in children, so it is recommended to avoid prescribing verapamil for this category of people.

During pregnancy and lactation

When this drug is prescribed only according to strict indications, when it is not prescribed at all.