Isoptin tablets instructions for use. Isoptin for the treatment of arterial hypertension in the form of tablets and solution
When our blood pressure rises and other disturbances in the functioning of the heart are observed, causing a deterioration in the general condition, we turn to medications that have a positive effect on the cardiovascular system. “Isoptin” precisely belongs to the category of cardiac drugs that normalize the functioning of the heart and blood vessels.
ATX code
C08DA01 Verapamil
Active ingredients
Verapamil
Pharmacological group
Calcium channel blockers
Pharmacological action
Antianginal drugs
Antihypertensive drugs
Antiarrhythmic drugs
Indications for use Isoptin
Indications for the use of Isoptin are also slightly different if they are considered in relation to what is prescribed by the doctor: taking tablets or injections.
So, for example, the prescription of tablets is justified in the following situations:
- diagnosed with arterial hypertension (stable high blood pressure),
- in case of hypertensive crisis,
- thickening of the wall of one of the heart ventricles (diagnosis: hypertrophic cardiomyopathy),
- for the treatment of cardiac ischemia (vasospastic, chronic stable and unstable angina),
- in case of heart rhythm disturbances: sudden attacks of rapid heartbeat (paroxysmal supraventricular tachycardia (PVT), which is one of the variants of arrhythmia), tachyarrhythmic form of atrial fibrillation (atrial fibrillation and flutter), the appearance of additional defective heart contractions (supraventricular extrasystole).
“Isoptin” in the form of an injection solution is used as monotherapy for mild forms of hypertension and as part of complex treatment for its severe, complicated manifestations, for angiospastic angina (against the background of vasospasm) and exertional angina. But most often it is used for the treatment of supraventricular tachyarrhythmias, when restoration of normal heart rhythm is required during PVT, as well as for correction of heart rate in atrial fibrillation of the tachyarrhythmic type (with the exception of Wolff-Parkinson-White and Lawn-Ganong-Levine syndromes).
Release form
The following dosage forms of the drug “Isoptin” can be found on sale:
Ordinary tablets 40 mg (white, film-coated, round in shape, convex on both sides, the number 40 is engraved on one side, and a triangle sign on the other). The tablets are placed in blisters:
- 20 pieces each (package contains either 1 or 5 blisters).
Ordinary tablets 80 mg (white, film-coated, round in shape, convex on both sides, on one side the inscription “ISOPTIN 80” is engraved, on the other - “KNOOL” and a line mark for dividing the tablet into 2 parts). Tablets are packaged in blisters:
- 10 pieces each (package contains either 2 or 10 blisters),
- 20 pieces each (package contains either 1 or 5 blisters),
- 25 pieces each (4 blisters per package).
Tablets CP240 prolonged (long-term) action 240 mg (light green in color, oblong in shape, reminiscent of capsules, 2 identical triangles are engraved on one side, there are division marks on both sides). Tablets in blisters:
- 10 pieces each (packing 2, 3, 5 or 10 blisters),
- 15 pieces each (in a package of 2,3,5 or 10 blisters),
- 20 pieces each (packing 2, 3.5 or 10 blisters).
Solution for intravenous administration in colorless glass ampoules of 2 ml (transparent liquid without a specific color). Ampoules are placed in transparent trays of 5, 10 and 50 pieces. Each pallet is packed in a separate thin cardboard box.
The main active ingredient of the drug "Isoptin" is verapamil, presented in the form of hydrochloride. He is known to many for the drug of the same name.
The composition of Isoptin has certain differences depending on the form of release of the drug. So tablets can contain 40, 80 or 240 mg of the main active ingredient plus excipients present in the tablet or its shell.
Auxiliary components in Isoptin tablets:
- pyrogenic or colloidal silicon dioxide as an adsorbent,
- Dicalcium phosphate dihydrate as a light source of calcium,
- croscarmellose sodium as a leavening agent,
- microcrystalline cellulose to cleanse the body,
- magnesium stearate to give the tablets a uniform consistency.
In turn, the film shell of the tablets consists of talc, hypromellose 3 mPa, sodium lauryl sulfate, macrogol and titanium dioxide.
An ampoule of Isoptin solution, in addition to verapamil hydrochloride in an amount of 5 mg, contains: NaCl and hydrochloric acid (HCl) with a concentration of 36%, diluted with water for injection.
Pharmacodynamics
"Isoptin" belongs to a group of antianginal drugs called calcium antagonists. These drugs help reduce the oxygen demand of the main heart muscle, provide a vasodilating effect on the coronary arteries and protect against overload of them and the heart muscle with calcium. The drug is able to limit the flow of calcium ions through the membrane into the muscle tissue of the heart and blood vessels.
Having a vasodilating effect, it helps lower blood pressure by reducing peripheral vascular resistance without increasing heart rate (a common reflex reaction). The antiangial effect of the drug "Isoptin" in the treatment of angina pectoris is based on its relaxing effect on cardiomyocytes (muscle cells that make up the heart wall), as well as on reducing the tone of peripheral vessels, thereby reducing the load on the atria. A reduction in the flow of calcium ions into myocytes leads to inhibition of the conversion of energy into work, and therefore to a slowdown in heart rate.
The use of Isoptin in the treatment of supraventricular tachyarrhythmias is justified due to its ability to delay the passage of nerve impulses through the atrioventricular node, block the conduction of the sinoatrial node and reduce the duration of the refractory period in the atrioventricular plexus. In this way, an optimal heart rate is achieved and the normal (sinus) rhythm of the heart is restored.
The drug has a selective effect and belongs to the group of dose-dependent drugs. If the disease proceeds while maintaining normal heart rate, then taking the drug will not affect them in any way, and if the heart rate decreases, it will be insignificant.
In addition to the antiangial and vasodilating (relaxation of vascular muscles) effects, the drug has a diuretic (diuretic) effect.
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Pharmacokinetics
The active ingredient of the drug “Isoptin” is almost 90% absorbed in the intestines, and its absorption does not depend on food intake. The bioavailability of the drug ranges from 10 to 35% both when taking tablets orally and when injecting the solution intravenously.
In case of coronary heart disease and hypertension, there is no relationship between the content of verapamil in the patient’s blood and the resulting therapeutic effect.
Metabolism of the drug occurs in the parenchymal cells of the liver, where it is almost completely biotransformed. It is able to pass relatively easily through placental tissue, since about 25% of the drug is found in the vessels of the navel.
The only active metabolite of Isoptin is norverapamil. Its maximum concentration in the blood is observed 6 hours after taking 1 dose of the drug. The half-life may vary significantly (2.5-7.5 hours with a single dose and 4.5-12 hours with repeated administration). When using a solution for intravenous injection, the half-life of the drug can range from 4 minutes to 5 hours.
The therapeutic concentration of the drug in the blood is observed on the 5th day after repeated administration of the drug.
“Isoptin” is able to penetrate and be excreted from the body along with breast milk, but its content there is so small that it does not cause unwanted symptoms in a nursing infant. The half-life in this case will be about 3-7 hours, but with repeated use it can increase to 14 hours.
Most of the drug "Isoptin" and its metabolites are excreted through the kidneys and only 16% is eliminated through the intestines.
In the case of extended-release tablets, the elimination of the drug from the body is slower. 50% of the administered dose of the drug is removed from the body during the first day. On the second day, 60% elimination was noted, and on the 5th day, 70% of the drug was eliminated.
In patients with renal failure and severe forms of liver failure, an extension of the half-life and an increase in bioavailability are noted.
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Use of Isoptin during pregnancy
The use of the drug "Isoptin" during pregnancy and breastfeeding is considered unsafe due to the lack of practical information about its effect on the course of pregnancy and the health of the fetus. Theoretically, the drug is considered quite safe, therefore, if the risk from using the drug is supposedly less than the expected benefit, it can be prescribed in tablet form, as prescribed by a doctor, during pregnancy. But breastfeeding will have to be stopped during drug therapy.
Contraindications
Isoptin, like most heart medications, has quite a few contraindications for use, which must be taken into account in order to avoid sad and sometimes tragic consequences.
General contraindications for all forms of the drug are:
- disruption of the conduction of nerve impulses from the atria to the ventricles (2nd and 3rd degree atrioventricular block), if it is not controlled by a special pacemaker,
- weakness of the pacemaker, as the sinus node is called, with alternating episodes of tachycardia and bradycardia,
- atrial fibrillation in the presence of additional pathways in the heart, which is characteristic of Wolff-Parkinson-White and Lown-Ganong-Levine syndromes,
- intolerance to individual components of the drug.
The drug is not used to treat patients under 18 years of age. This is due to the lack of information about the effect of Isoptin on the children's body.
Prescribing the drug to patients with 1 degree of atrioventricular block, as well as to those whose heart rate is less than 50 beats per minute, is considered undesirable. If the patient's upper pressure reading is below 90 mm Hg. he will also have to choose a different drug.
Taking pills is also contraindicated:
- in case of acute myocardial infarction against the background of greatly reduced blood pressure and pulse, complicated by insufficiency of left cardiac ventricular function,
- severe cases of left ventricular failure (cardiogenic shock),
- during therapy with Colchicine, used to treat gout.
Contraindications for using the drug in the form of a solution:
- persistently low blood pressure (arterial hypotension),
- cardiogenic shock, if it did not occur due to cardiac arrhythmia,
- fainting caused by a sudden, acute disturbance of the heart rhythm (Morgagni-Adams-Stokes syndrome),
- slowing down or completely stopping the flow of impulses from the sinus node to the atria (sinoauricular block),
- increased heart rate due to rapid work of the heart ventricles (ventricular tachycardia),
- chronic heart failure, if its cause is not supraventricular tachycardia,
- periods of pregnancy and lactation,
Isoptin injections are not given within 2 days after the end of Disopyramide therapy. The simultaneous administration of Isoptin and beta-blockers is not practiced.
Side effects Isoptin
It is possible that even the correct use of the drug, depending on the individual characteristics of the patient’s body and his reaction to a particular drug, may be accompanied by symptoms that are not related to the main purpose of the drug. We are talking about the side effects of drugs, which can be positive (useful), but most often the situation is exactly the opposite.
So, taking Izodinit may be accompanied by some unpleasant symptoms that occur with varying frequencies.
The gastrointestinal tract may react to the drug by causing some digestive problems. Most often, patients taking Isoptin experience stool disturbances in the form of constipation, nausea, and much less commonly, diarrhea. Some note an increase in appetite, while others take the drug, noticeable swelling of the gums appears, which subsequently begin to hurt and bleed, while others complain of intestinal obstruction. If the patient has certain abnormalities in the liver, an increase in the level of enzymes (liver transaminase and alkaline phosphatase) in the blood may be observed.
Some undesirable disturbances can also be observed in the functioning of the cardiovascular system. The most common of them are bradycardia (pulse less than 50 beats per minute) or, conversely, increased heart rate at rest (tachycardia), a fairly strong decrease in blood pressure (hypotension), and increased symptoms of heart failure. But the appearance or intensification of signs of angina is rare, although sometimes this condition against the background of severe damage to the coronary arteries can be accompanied by myocardial infarction. Cases of heart rhythm disturbances, including ventricular fibrillation/flutter (arrhythmias), are far from common.
It was noted above that intravenous injections should be carried out slowly, otherwise the following life-threatening conditions may be observed: complete cessation of impulses from the atrium to the ventricles (3rd degree AV block), a strong decrease in pressure with the development of acute vascular insufficiency (collapse), arrest heart (asystole).
The central and peripheral nervous systems may react to taking Izonidine with headaches, dizziness, and short-term loss of consciousness (fainting). Some patients note increased fatigue, inhibition of reactions and drowsiness, while in others, taking the medication can cause depression with increased anxiety. Also, in some cases, tremors of the arms and hands, impaired swallowing function, kinetic disturbances in the work of the upper and lower extremities, a shuffling gait, etc. are observed.
Among the reactions of the immune system, one can highlight allergic manifestations such as skin rashes, itching, redness of the skin, and the development of Stevens-Johnson syndrome.
Other side effects of the drug include weight gain, swelling of the lungs and extremities, increased platelet levels (thrombocytopenia), decreased white blood cell levels (agranulocytosis), enlarged mammary glands (gynecomastia) and the appearance of discharge from them (galactorrhea), increased prolactin hormone (hyperprolactinemia). , joint pathologies.
When large doses of the drug are administered intravenously, temporary loss of vision may occur when they accumulate in the blood plasma.
Directions for use and doses
To help your heart do its hard work and not cause other troubles, you need to carefully listen to your doctor’s recommendations regarding taking medications. The advice of girlfriends and neighbors will do when it comes to a recipe for a delicious cake or roast, but not when taking any other medications, especially heart medications. When it comes to our “engine,” taking heart medications strictly in terms of dose and method of administration is the key to not only effective, but also safe treatment.
“Isoptin” refers to drugs that improve heart function, which means all of the above applies to it in full.
So, how to take the drug correctly so that, having cured one thing, not cripple another. The instructions for the drug indicate that it is advisable to combine the intake of Isoptin tablets with a meal, or take the drug immediately after a meal. However, the tablet form of the drug is not intended for resorption or crushing when taken. Tablets (regular and extended-release) should be swallowed whole with plenty of water (usually half a glass of water). This ensures a gentle effect on the gastric mucosa and creates optimal conditions for the absorption of this dosage form.
The tablets are taken orally, i.e. through the mouth. They are not used for any other purposes. The dosage depends on the age of the patient and, of course, on the diagnosis.
Adult patients: the initial daily dose for angina pectoris, atrial fibrillation and hypertension, depending on the severity of the pathology and the body's reaction, ranges from 120 to 240 mg. In case of hypertension, the dosage (according to the attending physician) can be increased to 480 mg, and in case of cardiomyopathy, temporarily even up to 720 mg per day. The recommended frequency of administration is 3 times a day.
The effective dose for extended-release tablets ranges from 240 to 360 mg. Long-term use of the drug does not allow increasing the dose above 480 mg per day, except for a short time.
If the patient has liver dysfunction, it is recommended to take tablets with a minimum dosage. The daily dose with 2-3 doses will be 80-120 mg.
Isoptin solution can only be used for intravenous injections. Slow administration of the drug is indicated over at least 2 minutes. In this case, monitoring of blood pressure and heart rate is necessary. In elderly patients, the drug should be administered even more slowly (at least 3 minutes).
The effective initial dose is calculated based on the ratio: per 1 kg of patient weight there should be from 0.075 to 0.15 mg of the drug in solution. Usually this is 2-4 ml (1-2 ampoules or 5-10 mg verapamil hydrochloride). If the expected result does not occur within half an hour, it’s time to give another injection with a dosage of 10 ml.
The duration of the therapeutic course is determined individually by the attending physician.
Children: the dosage depends on the age of the small patient. Despite the fact that Isoptin can be used even to treat newborns, doctors prefer to resort to this practice extremely rarely, if there are no other treatment options at the moment, in order to avoid possible serious consequences (single cases of child death after injection have been noted). The dosage for newborns is from 0.75 to 1 mg (for babies up to 12 months - up to 2 mg), which in terms of solution will be 0.3-0.4 (0.3-0.8) ml.
The effective dose of “Isoptin” for children older than one year (up to 5 years) is 2-3 mg (in the form of a solution - 0.8-1.2 ml), for children over 5 years old (up to 14 years) - from 2.5 to 5 mg (in the form of a solution - from 1 to 2 ml).
Before using the drug “Isoptin” in children, it is advisable to take a course of drugs based on digitalis or its derivatives, which will help reduce the symptoms of heart failure and shorten the course of treatment with “Isoptin”.
Overdose
In principle, therapy with large doses of the drug "Isoptin" should be carried out in a hospital setting under the supervision of the attending physician, which in most cases excludes an overdose of the drug. If for some reason this happens, you must urgently take all necessary measures to remove particles of the drug from the body as soon as possible.
How to determine that an overdose is occurring? Most likely based on the following signs:
- very strong drop in blood pressure levels up to critical levels,
- complete loss of consciousness while taking the drug,
- state of shock
- the appearance of symptoms of AV heart block of the 1st or 2nd degree, and sometimes even the onset of complete blockade is possible (3rd degree),
- the appearance of signs of ventricular tachycardia,
- sinus bradycardia with a pulse rate below 55 beats per minute.
Sometimes, while taking Isoptin in large doses (especially when administered intravenously), cases of cardiac arrest have been reported. And the patients were not always saved.
The severity of overdose symptoms depends on the dose of the drug taken by the patient, the patient’s age, the timeliness and completeness of first aid, which consists of stopping the process of intoxication of the body.
If everything points to an overdose of Isoptin tablets, you must first take measures to remove the drug from the gastrointestinal tract. For this purpose, you can induce vomiting in the patient (through mechanical action on the root of the tongue or taking emetics), carry out measures to lavage the stomach and empty the intestines (enemas, laxatives). In case of critically weak intestinal motility and in the case of using extended-release tablets, gastric lavage measures are relevant even within 12 hours after taking the drug.
If a prolonged form of the drug was used in the treatment of diseases, it must be taken into account that its effect can be felt over the next 2 days, during which particles of the tablets will be released in the intestines, where they are absorbed and transported into the blood. Individual particles of the drug can be located along the entire gastrointestinal tract, creating additional foci of poisoning, which cannot be removed by conventional gastric lavage.
In case of cardiac arrest, standard resuscitation measures are carried out (direct and indirect cardiac massage, artificial respiration).
A specific antidote for verapramil is calcium gluconate, a 10% solution of which is injected in a volume of 10 to 30 ml. Repeated administration of calcium is carried out by drip (infusion rate 5 mmol per hour).
Cardiac arrest, AV block, sinus bradycardia, in addition to electrical stimulation of the heart, require the use of the following drugs: Isoprenaline, Orciprenaline, and atropine-type drugs.
With a strong decrease in blood pressure, Dopamine, Dobutamine, and Norepinephrine are used. If there are persistent symptoms of myocardial failure, the first 2 drugs in combination with calcium supplementation will be useful.
Interactions with other drugs
The cardiac drug “Isoptin” tends to react with many drugs, therefore, you should inform your doctor about taking any other drug during therapy using “Isoptin” in order to avoid unpleasant and dangerous consequences, including an overdose of verapramil.
Thus, the simultaneous use of Isoptin and drugs that lower blood pressure leads to the fact that the effect of both drugs is noticeably enhanced, which can lead to a sharp drop in blood pressure.
The likelihood of developing various complications in the form of a drop in heart rate and blood pressure, the development of AV heart block or heart failure increases if Isoptin is taken together with beta-blockers, drugs for arrhythmia, and drugs for inhalation anesthesia. This is due to the increased inhibitory effect of drugs on the conductivity and functioning of the sinus node and cardiac myocardium.
“Isoptin” with the parallel use of certain drugs (antihypertensive drugs aliskiren (“Rasilez”), tranquilizers based on buspirone (“Spitomin”, “Buspirone”), cardiac glycoside “Digoxin”, anti-tumor antibiotic “Doxorubicin”, drug for the treatment of gout “Colchicine” ", the bronchodilator "Theophylline" and the antiarrhythmic drug "Quinidine") can increase their concentration in the blood plasma, enhancing their effect and provoking the development of side effects. Most often, there is an excessive drop in pressure or the development of AV block.
An increase in the concentration of drugs in the blood under the influence of Isoptin is also observed when it is taken simultaneously with the alpha-blockers Prazosin and Terazosin, the immunosuppressant Cyclosporin, the anticonvulsant Karmazepine, the antiepileptic drug Valproic acid and muscle relaxants.
It is possible to increase the blood content of the active substance of the sedative drug "Midazolam" and ethanol with simultaneous therapy with these drugs and "Isoptin".
Simultaneous use of Isoptin with the antiarrhythmic drugs Amidaron and Desopyramide provokes a significant decrease in the force of heart contractions, causing bradycardia and collapse, decreased conduction of impulses in the heart, and AV block of varying degrees.
Simultaneous therapy with Isoptin and the antiarrhythmic drug Flecainide can negatively affect the contractility of the main cardiac muscle and slow down AV conduction.
“Isoptin” may interact with some statins (atorvastatin, lovastatin, simvastatin), since it inhibits the action of the CYP3A4 isoenzyme, which is involved in the metabolism of the above statins. At the same time, the level of statins in the blood plasma increases, which can lead to the destruction of muscle cells.
When veraptamil is administered intravenously to patients undergoing beta-blocker treatment, there is a high risk of a severe drop in blood pressure and cardiac arrest.
An increase in the antianginal effect of Isoptin is observed against the background of parallel administration of nitrates used to treat cardiac ischemia.
Taking acetylsalicylic acid during Isoptin therapy increases the likelihood of various bleedings.
The combination of Isoptin with the muscle relaxant Dantrolene is also considered potentially dangerous, since their interaction can cause the death of the patient due to the development of ventricular fibrillation.
Non-steroidal anti-inflammatory drugs (Diclofenac), the anti-tuberculosis drug Rifampicin, barbiturates (Phenytoin, Phenobarbital) and nicotine can reduce the content of verapamil in the blood, largely due to the acceleration of its metabolism in the liver and rapid elimination from the body. In this regard, all the beneficial effects of Isoptin are noticeably weakened.
But the antiulcer drug Cimetidine, on the contrary, enhances the effect of verapamil, which is part of the Isoptin tablets. But it does not have any effect on the kinetic properties of Isoptin when administered intravenously.
The results of the interaction between Isoptin and the antidepressant Imipramine (Melipramine) are visible on the cardiogram in the form of indicators indicating a decrease in atrioventricular conduction.
It is undesirable to carry out simultaneous therapy with the antiherpentine drug Clonidine (Clonidine), since there is a risk of cardiac arrest.
It is difficult to predict the results of drug interactions with lithium preparations (lithium carbonate). Dangerous situations such as the development of severe bradycardia and disruption of the structure and functions of the nervous system (neurotoxicity) are possible. Sometimes there is a decrease in the lithium content in the blood, which negatively affects the patient’s mental health.
Taking the antipsychotic "Sertindol" ("Serdolect") during therapy with "Isoptin" increases the likelihood of developing ventricular arrhythmias.
"Isoptin" is able to enhance the muscle relaxant effect of tubocurarine and vecuronium chlorides.
Estrogens and sympathomimetics can significantly reduce the hypotensive effect of Isoptin.
The use of anesthetics (Enflurane, Etomidate) during treatment with Isoptin should be carried out with caution, since the latter can prolong the effect of anesthesia, significantly inhibiting the activity of the cardiovascular system.
I20 Angina [angina pectoris]
I21 Acute myocardial infarction
I25 Chronic ischemic heart disease
I47.1 Supraventricular tachycardia
I49.4 Other and unspecified depolarization
I49.9 Heart rhythm disorder, unspecified
R07.2 Pain in the heart area
Manufacturer
Abbey Deutschland GmbH & Co. KG for Abbott Laboratories GmbH, Germany
Compound
active ingredient: 1 tablet contains verapamil hydrochloride 40 mg or 80 mg; excipients: calcium hydrogen phosphate dihydrate, cellulose
microcrystalline, colloidal anhydrous silicon dioxide, croscarmellose sodium, magnesium stearate, hypromelose, sodium lauryl sulfate, macrogol 6000, talc, titanium dioxide (E 171).
Description
white biconvex film-coated tablets, “40” is indicated on one side, and the company’s trademark on the other;
white biconvex film-coated tablets, “Isoptin 80” is indicated on one side, and the company’s trademark above the risks on the other.
Pharmacological action
Verapamil blocks the transmembrane flow of calcium ions into cardiomyocytes and vascular smooth muscle cells. It directly reduces the myocardial oxygen demand by influencing energy-consuming metabolic processes in myocardial cells and indirectly affects the reduction of afterload. By blocking the calcium channels of the smooth muscle cells of the coronary arteries, blood flow to the myocardium is increased, even in post-stenotic areas, and spasm of the coronary arteries is relieved. The antihypertensive effectiveness of verapamil is due to a decrease in peripheral vascular resistance without an increase in heart rate as a reflex response. No undesirable changes in physiological blood pressure values were observed. Verapamil has a pronounced antiarrhythmic effect, especially in cases of supraventricular arrhythmia. It delays the conduction of the impulse in the atrioventricular node, as a result of which, depending on the type of arrhythmia, sinus rhythm is resumed and/or the ventricular rate is normalized. The normal heart rate does not change or decreases slightly.
Pharmacokinetics
Verapamil is rapidly and almost completely absorbed in the small intestine. The degree of absorption is more than 90%. The average absolute bioavailability in healthy people after a single dose of the drug is 22%, which is explained by extensive hepatic first-pass metabolism. Bioavailability increases 2 times after repeated doses.
Peak plasma concentrations are achieved 1 to 2 hours after administration of the immediate-release tablets. The half-life is 3-7 hours for a one-time dose and 4.5 - 12 hours for a course dose. Plasma protein binding - 90%. Verapamil is almost completely metabolized, resulting in the formation of various metabolites. Among these metabolites, only norverapamil is pharmacologically active (as determined in experiments on dogs). Verapamil and its metabolites are excreted mainly by the kidneys, only 3-4% is excreted unchanged. About 50% of the administered dose is eliminated within 24 hours, 70% is eliminated within 5 days. Up to 16% of the drug is excreted in feces. Recent evidence suggests that there is no difference in the pharmacokinetics of verapamil in people with healthy kidneys and in patients with end-stage renal disease. The half-life is increased in patients with cirrhosis due to low clearance and large volume of distribution.
Indications for use
Coronary heart disease, including: stable angina pectoris;
Unstable angina (progressive angina, rest angina),
Vasospastic angina (variant angina, Prinzmetal angina),
Post-infarction angina in patients without heart failure, unless P-blockers are indicated.
Arrhythmias: paroxysmal supraventricular tachycardia; atrial flutter/fibrillation with rapid atrioventricular conduction (except for Wolff-Parkinson-White syndrome (WPW).
Arterial hypertension.
Contraindications
Cardiogenic shock.
Acute myocardial infarction with complications (bradycardia, arterial hypotension, left ventricular failure).
II and III degrees of atrioventricular block (except for patients who have an artificial pacemaker implanted) and sinoatrial block.
Sick sinus syndrome (except for patients who have an artificial pacemaker implanted). ,
Known hypersensitivity to verapamil or any other component of the drug.
Congestive heart failure.
Atrial fibrillation/flutter in the presence of additional pathways (WPW syndrome and LGL syndrome).
During treatment with Isoptin, do not simultaneously use intravenously (3-adrenergic blockers (except for intensive care).
Pregnancy and lactation
The drug should not be taken in the first and second trimesters of pregnancy. Admission in the third trimester of pregnancy is only in case of emergency, when the result outweighs the risk to the mother and child. Verapamil crosses the placenta and is detected in umbilical cord blood.
The biologically active substance passes into breast milk. Limited oral data in humans indicate that the dose of verapamil delivered to the newborn is low (0.1 - 1% of the maternal dose), so the use of verapamil may be compatible with breastfeeding. Given the risk of serious adverse reactions in breastfed neonates, verapamil should only be used during breastfeeding if absolutely necessary for the mother.
Directions for use and doses
Doses are selected individually for each patient. The drug should be taken without sucking or chewing with a sufficient amount of liquid (for example, 1 glass of water, never grapefruit juice), preferably during or immediately after a meal.
Adults and adolescents weighing more than 50 kg:
Coronary heart disease, paroxysmal supraventricular tachycardia, atrial flutter/fibrillation
Children of senior preschool age up to 6 years, only with heart rhythm disturbances: the recommended dosage is in the range of 80 - 120 mg per day, divided into 2 - 3 single doses.
Children 6-14 years old, only for heart rhythm disturbances: recommended dosage in the range of 80 - 360 mg per day divided into 2 - 4 single doses.
Liver dysfunction
In patients with impaired liver function, depending on the severity, the effect of verapamil hydrochloride is enhanced and prolonged due to slower breakdown of the drug. Therefore, in such cases, the dosage should be set with particular caution and start with small doses (for example, for patients with impaired liver function, first 2-3 times a day 40 mg, respectively 80 - 120 mg per day).
Do not take the drug lying down.
Verapamil hydrochloride should not be administered to patients with myocardial infarction within 7 days of the event.
After long-term therapy, the drug should be discontinued, gradually reducing the dose.
The duration of treatment is determined by the doctor individually and depends on the patient’s condition and the course of the disease.
Side effect
The following adverse reactions have been reported during post-marketing use of verapamil or in phase IV clinical studies. Given the impossibility of accurately counting patients during post-marketing use of the drug, adverse reactions are presented without calculating their frequency, but are classified by organ system. Cardiovascular system disorders: AV block I, II or III degree, sinus bradycardia, sinus node arrest, peripheral edema, palpitations, increased heart rate (tachycardia), arterial hypotension, flushing, cardiac arrest may develop or worsen failure. Gastrointestinal disorders: nausea, vomiting, constipation, pain, abdominal discomfort, intestinal obstruction, gum hyperplasia (gingivitis and bleeding).
Neurological disorders: headache, extrapyramidal disorders, dizziness, paresthesia, tremor may occur.
Disorders of the hearing and vestibular apparatus: dizziness, ringing in the ears.
Changes in the skin and subcutaneous tissues: angioedema, Stevens-Johnson syndrome, erythema multiforme, maculopapular rash, alopecia, erythromelalgia, urticaria, itching, hemorrhages in the skin or mucous membranes (purpura) were observed.
Disorders of the reproductive system and mammary glands: erectile dysfunction, gynecomastia, galactorrhea.
Disorders of the musculoskeletal system and connective tissue: myalgia, arthralgia, muscle weakness.
Immune system disorders: hypersensitivity.
General disorders: fatigue.
Studies: increased levels of liver enzymes and serum prolactin levels.
There has been a single post-marketing report of paralysis (tetraparesis) associated with the combined use of verapamil and colchicine. This may be due to the penetration of colchicine through the blood-brain barrier as a result of verapamil inhibition of CYP3A4 and P-gp. The combined use of colchicine and verapamil is not recommended.
Overdose
Symptoms of poisoning from a verapamil overdose depend on the amount of the drug taken, the time at which detoxification measures were taken, and the age of the patient. The following symptoms predominate: a significant decrease in blood pressure, heart rhythm disturbances (bradycardia, borderline rhythms with atrioventricular dissociation and high-degree atrioventricular block), which can lead to shock and cardiac arrest, impaired consciousness to a coma, stupor, hyperglycemia, hypokalemia, metabolic acidosis , hypoxia, cardiogenic shock with pulmonary edema, renal dysfunction and convulsions. Therapeutic measures aimed at removing substances from the body and restoring the stability of the cardiovascular system. General measures: gastric lavage is recommended even if more than 12 hours have passed since taking the drug and gastrointestinal motility is not determined (absence of bowel sounds). General resuscitation measures include chest compressions, artificial respiration, defibrillation, and cardiac pacing. Hemodialysis is not indicated. It is possible to use hemofiltration and plasmapheresis (calcium antagonists bind well to plasma proteins). Special measures: elimination of cardiodepressive effects, arterial hypotension and bradycardia. A specific antidote is calcium: 10 - 20 ml of a 10% solution of calcium gluconate (2.25-4.5 mmol) is administered intravenously. If necessary, you can repeat the administration or perform an additional drip infusion (for example, 5 mmol/hour). Additional measures: for AV block of the second and third degree, sinus bradycardia, cardiac arrest, atropine, isoprenaline, orciprenaline or cardiac stimulation are used. In case of arterial hypotension as a result of cardiogenic shock and arterial vasodilation, dopamine (up to 25 mcg/kg per minute), dobutamine (up to 15 mcg/kg per minute) or norepinephrine is used. Serum calcium concentrations should be within the upper limit of normal or slightly above normal. Due to vasodilation, a replacement fluid (Ringer's solution or saline) is administered in the early stages.
Interaction with other drugs
Verapamil hydrochloride is metabolized by cytochrome P450 CYP3A4, CYP1A2, CYP2C8, CYP2C9 and CYP2C18. Verapamil is an inhibitor of CYP3A4 and P-glycoprotein (P-gp) enzymes. Clinically important interactions have been reported with CYP3A4 inhibitors, which were accompanied by increased plasma levels of verapamil, while CYP3A4 inducers caused a decrease in plasma levels of verapamil hydrochloride, therefore monitoring for interactions with other drugs is necessary.
Antiarrhythmic drugs, /3-adrenergic blockers: mutual enhancement of cardiovascular action (high degree atrioventricular block, significant decrease in heart rate, the appearance of heart failure, significant decrease in blood pressure).
Quinidine: decreased oral clearance of quinidine (-35%). May develop
arterial hypotension, and in patients with hypertrophic obstructive cardiomyopathy - pulmonary edema.
Flecainidine: minimal effect on plasma clearance of flecainidine (<~10%); не влияет на клиренс верапамила в плазме крови.
Metoprolol: increase in metoprolol AUC (-32.5%) and Cmax (-41%) in patients with angina pectoris.
Propranolol: increased propranolol AUC (-65%) and C max (-94%) in patients with angina pectoris.
Antihypertensives, diuretics, vasodilators: increased hypotensive effect. Prazosin, terazosin: additional hypotensive effect (prazosin: increase in Cmax of prazosin (-40%) without affecting the half-life; terazosin: increase in AUC of terazosin (-24%) and Cmax (~25%)).
Antiviral (HIV) agents: Plasma concentrations of verapamil may be increased. Use with caution or a dose reduction of verapamil may be necessary.
Carbamazepine: increased levels of carbamazepine, increased neurotoxic side effects of carbamazepine - diplopia, headache, ataxia, dizziness. Increased AUC of carbamazepine (-46%) in patients with refractory partial epilepsy.
Lithium: increased neurotoxicity of lithium.
Antimicrobial agents:
Clarithromycin, erythromycin, telithromycin: increased verapamil levels may occur. Rifampin: may reduce the hypotensive effect. Decreased verapamil AUC (-97%), Cmax (~94%), bioavailability after oral administration (-92%).
Colchicine: Combination with verapamil is not recommended due to increased exposure to colchicine. I
Sulfinpyrazone: increased oral clearance of verapamil by 3 times, bioavailability by 60%. The hypotensive effect may be reduced.
Neuromuscular blockers: possible increased effect due to verapamil hydrochloride. Acetylsalicylic acid: increased risk of bleeding.
Ethanol: increased plasma ethanol levels.
HMG-CoA reductase inhibitors: Treatment with HMG-CoA reductase inhibitors (simvastatin, atorvastatin, lovastatin) in patients taking verapamil should begin with the lowest possible doses and gradually increase. If a patient who is already taking verapamil needs to be prescribed an HMG-CoA reductase inhibitor, the necessary reduction in the dose of statins should be taken into account and the dosage should be adjusted according to the concentration of cholesterol in the blood plasma.
Atorvastatin: Increased levels of atorvastatin may occur. Atorvastatin increases the AUC of verapamil by approximately 42.8%.
Lovastatin: Lovastatin levels may increase.
Simvastatin: increase in AUC of simvastatin by approximately 2.6 times, Cmax of simvastatin by 4.6 times.
Fluvastatin, pravastatin and rosuvastatin are not metabolized by CYP3A4 and do not interact with verapamil.
Digoxin: in healthy people, digoxin C max increases by 45-53%, C ss - by 42%, AUC - by 52%.
Digitoxin: decreased digitoxin clearance (-27%) and extrarenal clearance (-29%).
Cimetidine: The AUC of R- (-25%) and S-verapamil (-40%) increases with a corresponding decrease in the clearance of R- and S-verapamil.
Antidiabetic drugs (glyburide): glyburide C max increases by approximately 28%, AUC by 26%.
Theophylline: reduction in oral and systemic clearance by approximately 20%, in smokers by 11%.
Imipramine: increased AUC (-15%) without affecting the active metabolite desipramine. Doxorubicin: with simultaneous use of doxorubicin and verapamil (oral), the AUC (-89%) and C max of doxorubicin in blood plasma (-61%) increases in patients with small cell lung cancer. In patients with a progressive tumor, no significant changes in the pharmacokinetics of doxorubicin are observed with simultaneous intravenous administration of verapamil.
Phenobarbital: increases the oral clearance of verapamil by 5 times.
Buspirone: increase in AUC and Cmax by 3-4 times.
Midazolam: increase in AUC by 3 times and Cmax by 2 times.
Almotriptan: increase in AUC by 20%, Cmax - by 24%. .
Sulfinpyrazone" increases the oral clearance of verapamil by 3 times, bioavailability by 60%.
Immunological drugs:
Cyclosporine: increase in AUC, C max Css by approximately 45%.
Everolimus, sirolimus, tacrolimus: levels of these drugs may increase. Grapefruit juice: AUC of R- (-49%) and S-verapamil (-37%) increases, Cmax of R- (-75%) and S-verapamil (-51%) increases without changing half-life and renal clearance.
St. John's wort: AUC of R- (-78%) and S-verapamil (-80%) decreases with a corresponding decrease in Cmax.
Features of application
When using verapamil and determining its dose, special attention should be paid to patients:
With AV blockade of the first degree;
With arterial hypotension (systolic blood pressure< 90 мм рт. ст.);
With bradycardia (heart rate less than 50 beats per minute);
With severe liver failure;
With disorders of neuromuscular conduction (myasthenia gravis, Eaton-Lambert syndrome, progressive Duchenne muscular dystrophy).
Although data from validated comparative studies have shown that renal impairment does not affect the pharmacokinetics of verapamil in patients with end-stage renal disease, there have been several reports suggesting that verapamil should be used with caution and close monitoring in patients with renal impairment. Verapamil cannot be removed by hemodialysis.
40 mg: 20 tablets in a blister, 5 blisters in a cardboard box or 25 tablets in a blister, 4 blisters in a cardboard box;
80 mg: 20 tablets in a blister, 5 blisters in a cardboard box.
Storage conditions
Store out of the reach of children at a temperature not exceeding 25°C.
In this medical article you can familiarize yourself with the drug Isoptin. The instructions for use will explain in what cases you can take tablets and dragees 40 mg and 80 mg, 240 mg (Forte), injections in injection ampoules, what the medicine helps with, what are the indications for use, contraindications and side effects. The annotation presents the forms of release of the drug and its composition.
In the article, doctors and consumers can only leave real reviews about Isoptin, from which you can find out whether the medicine has helped in the treatment of heart rhythm disorders in adults and children, for which it is also prescribed. The instructions list analogues of Isoptin, prices of the drug in pharmacies, as well as its use during pregnancy.
The instructions for use classify the drug Isoptin as a drug that has hypotensive, antiarrhythmic and antianginal effects.
Release form and composition
The medicine Isoptin is sold in the form of ampoules with a solution for injections and in the form of tablets. These forms differ not only in their use, but also in the amount of active ingredient in one serving and the list of additional ingredients.
Isoptin tablets are available in dosages of 40, 80, 120 and 240 mg. They are white or green in color, and have a round shape, convex on both sides. 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. There is a separation mark on each portion of the drug.
Isoptin SR (retard). A more powerful product, which is produced in the form of green pills with an active substance mass of 240 mg.
5, 10 or 50 ampoules are placed in plastic trays. One package includes one pallet with the drug. Tablets are sold in plastic blisters of 10 pcs. One cardboard package can contain from 1 to 10 plates with tablets.
Isoptin in 2 ml ampoules contains 5 mg of the working ingredient. It is colorless and odorless. The following additional components are used: hydrochloric acid, saline solution, sodium chloride.
Pharmacological action
Isoptin is a selective class I calcium channel blocker, a diphenylalkylamine derivative that has antianginal, antihypertensive and antiarrhythmic effects.
The antianginal effect is associated with a direct effect on the myocardium and with an effect on peripheral hemodynamics. Blockade of calcium entry into the cell leads to a decrease in the transformation of energy contained in high-energy bonds of ATP into mechanical work, a decrease in myocardial contractility and myocardial oxygen demand. The drug has a vasodilating, negative ino- and chronotropic effect. Increases the period of diastolic relaxation of the left ventricle, reduces the tone of the myocardial wall.
A decrease in OPSS may be due to the antihypertensive effect of Isoptin.
The drug reduces AV conduction, prolongs the refractory period and suppresses the automaticity of the sinus node. Has an antiarrhythmic effect in supraventricular arrhythmias.
Indications for use
What does Isoptin help with? The instructions indicate that the drug is prescribed for the treatment of:
- Atrial fibrillation and flutter, which are accompanied by tachyarrhythmia (with the exception of WPW syndrome).
- Arterial hypertension: as monotherapy in mild or moderate cases, as part of combination treatment in severe cases.
- Angiospastic angina (Prinzmetal's angina).
- Paroxysmal supraventricular tachycardia.
- Stable angina.
Instructions for use
Isoptin is prescribed by the attending physician based on clinical indications, severity of the disease and a detailed study of the patient’s medical history.
The tablets are taken orally, without chewing during meals, with water.
Dosage and treatment period are determined individually; usually treatment begins with a dose of 40-80 mg 3-4 times a day. The maximum daily dose of 480 mg per day according to the instructions should be taken only under the supervision of a doctor in a hospital.
Isoptin solution is intended only for intravenous administration, the procedure is carried out very slowly, while monitoring electrocardiography and the patient’s blood pressure. According to the instructions, the initial dose is 5-10 mg; if necessary, after half an hour, the drug can be repeated at a dose of 10 mg. The treatment period is determined by the doctor.
Contraindications
Absolute:
- complicated myocardial infarction (hypotension, bradycardia, left ventricular failure);
- sinoatrial block;
- AV block of the second or third degree;
- cardiogenic shock;
- bradycardia-tachycardia syndrome.
Relative contraindications:
- heart failure;
- arterial hypotension;
- atrial fibrillation due to WPW syndrome;
- AV block of the first degree;
- bradycardia.
Side effects
When taking Isoptin, various side effects may occur: muscle and joint pain, bradycardia, constipation, depression, nausea, peripheral edema, fainting, headache, allergic skin reactions, collapse, increased heart rate, angina pectoris.
Children, pregnancy and breastfeeding
Isoptin should not be used during pregnancy and lactation.
In childhood
Should be used with caution in patients under 18 years of age.
Special instructions
When taking Isoptin, it is better to temporarily avoid work that requires attention and precision. Driving should be temporarily stopped.
The peculiarity of taking the drug is that the drug must be discontinued abruptly; the dosage should be reduced gradually.
Drug interactions
With the simultaneous use of Isoptin with inhibitors of the CYP3A4 isoenzyme, an increase in the concentration of verapamil in the blood plasma is observed, with inducers of the CYP3A4 isoenzyme - a decrease in its concentration (the interaction should be taken into account when using such drugs simultaneously).
When Isoptin is used simultaneously with certain drugs, undesirable effects may occur (Css is the average equilibrium concentration of the substance in the blood plasma, Cmax is the maximum concentration of the substance in the blood plasma, AUC is the area under the pharmacokinetic concentration-time curve, T1/2 is the half-life ):
- Theophylline: decrease in its systemic clearance;
- : increase in its AUC in patients with resistant partial epilepsy;
- Metoprolol, propranolol: increase in their AUC and Cmax in patients with angina pectoris;
- Buspirone, midazolam: increase in their AUC and Cmax;
- Quinidine: possible increased hypotensive effect; in patients with hypertrophic obstructive cardiomyopathy, pulmonary edema may develop;
- Acetylsalicylic acid: increased bleeding;
- Grapefruit juice: increase in AUC and Cmax of the R-enantiomer and S-enantiomer of verapamil (renal clearance and T1/2 do not change);
- Quinidine: decreased clearance;
- Cyclosporine: increase in its AUC, Css, Cmax;
- Beta-blockers, antiarrhythmic drugs: mutual enhancement of cardiovascular effects (more significant decrease in heart rate, more pronounced AV blockade, increased arterial hypotension and development of symptoms of heart failure);
- Sulfinpyrazone: increased clearance of verapamil and decreased bioavailability;
- Diuretics, antihypertensives, vasodilators: increased hypotensive effect;
- Cimetidine: increased AUC of the R-enantiomer and S-enantiomer of verapamil with a corresponding decrease in the clearance of R- and S-verapamil;
- Carbamazepine: increasing its concentration in blood plasma; it is possible to develop adverse reactions characteristic of carbamazepine (headache, diplopia, dizziness or ataxia);
- Prazosin: increase in its Cmax, T1/2 of prazosin does not change;
- Terazosin: increase in its AUC and Cmax;
- Phenobarbital: increased clearance of verapamil;
- Digoxin: increase in its Cmax, AUC and Css;
- Glibenclamide: increase in its Cmax and AUC;
- Clarithromycin, erythromycin, telithromycin: possible increased concentrations of verapamil;
- Imipramine: increase in its AUC; Isoptin has no effect on the concentration of the active metabolite of imipramine - desipramine;
- Doxorubicin: an increase in its AUC and Cmax in patients with small cell lung cancer;
- Ritonavir and other antiviral drugs for the treatment of HIV infection: inhibition of the metabolism of verapamil is possible, which can lead to an increase in its concentration in the blood plasma (with simultaneous use of the dose of Isoptin should be reduced);
- : possible increase in its concentration and AUC;
- St. John's wort: decrease in AUC of the R-enantiomer and S-enantiomer of verapamil with a corresponding decrease in Cmax;
- Sirolimus, tacrolimus, lovastatin: their concentrations may increase;
- Ethanol (alcohol): an increase in its concentration in the blood plasma;
- Rifampicin: decreased AUC, Cmax and bioavailability of verapamil when taken orally;
- Terazosin, prazosin: additive hypotensive effect;
- Simvastatin, almotriptan: increase in their AUC and Cmax;
- Rifampicin, sulfinpyrazone: the hypotensive effect of verapamil may be reduced;
- Digitoxin: reduction of its general and extrarenal clearance;
- Muscle relaxants: their effect may be enhanced;
- Colchicine: a significant increase in its concentration in the blood is possible;
- Lithium: increased neurotoxicity.
Analogues of the drug Isoptin
Analogues are determined by structure:
- Verogalide EP 240 mg;
- Verapamil hydrochloride solution for injection 0.25%;
- Isoptin SR 240;
- Kaveril;
- Lekoptin;
- Vero Verapamil;
- Finoptin;
- Veracard.
Vacation conditions and price
The average cost of Isoptin 30 tablets of 40 mg varies in the range of 310 - 355 rubles. For Isoptin SR you need to pay 605 - 656 rubles, and the injection solution costs about 612 - 705 rubles. To purchase medicines, you need a prescription from a doctor.
The instructions indicate that the drug must be stored in a dry, cool place out of reach of children. Shelf life – 3 years.
Post Views: 305
Composition and release form
1 ampoule with 2 ml of injection solution contains verapamil hydrochloride 5 mg; in a box 5 or 50 pcs.
1 film-coated tablet - 40 and 80 mg; 20 pcs in a blister, 5 blisters in a box.
Pharmacological action
Pharmacological action- hypotensive, antiarrhythmic, antianginal.Inhibits the transmembrane flow of calcium ions in myocardial and vascular smooth muscle cells (causes vasodilation), reduces peripheral vascular resistance without a reflex increase in heart rate, and reduces myocardial contractility.
Indications of the drug Isoptin ®
Arterial hypertension, coronary artery disease, atrial fibrillation (paroxysmal supraventricular tachycardia).
Contraindications
Cardiogenic shock, acute complicated myocardial infarction, severe conduction disturbances, sick sinus syndrome.
Use during pregnancy and breastfeeding
With caution, especially in the first trimester.
Side effects
Myocardial rhythm and conduction disturbances, heart failure, hypotension, edema, myalgia, arthralgia, allergic reactions, etc.
Interaction
Increases the effects (including side effects) of beta-blockers. Increases hypotension when combined with other antihypertensive drugs.
Directions for use and doses
Pills: orally - 40-80 mg 3-4 times a day after meals; a maintenance dose can be used for a long period.
Solution for injection: IV, under the control of ECG and blood pressure, either slowly (within 2 minutes) in an initial dose of 5 mg (if ineffective, repeat 5 mg after 5-10 minutes), or drip (to maintain the effect) - 5-10 mg/ h in saline solution, glucose solution or other solutions with a pH less than 6.5, total dose - 100 mg/day.
Storage conditions for the drug Isoptin ®
At a temperature not exceeding 25 °C.Keep out of the reach of children.
Shelf life of the drug Isoptin ®
5 years.Do not use after the expiration date stated on the package.
Synonyms of nosological groups
| Category ICD-10 | Synonyms of diseases according to ICD-10 |
|---|---|
| I10 Essential (primary) hypertension | Arterial hypertension |
| Arterial hypertension | |
| Arterial hypertension | |
| Sudden increase in blood pressure | |
| Hypertensive state | |
| Hypertensive crises | |
| Hypertension | |
| Arterial hypertension | |
| Hypertension is malignant | |
| Essential hypertension | |
| Hypertension | |
| Hypertensive crises | |
| Hypertensive crisis | |
| Hypertension | |
| Malignant hypertension | |
| Malignant hypertension | |
| Isolated systolic hypertension | |
| Hypertensive crisis | |
| Primary arterial hypertension | |
| Essential arterial hypertension | |
| Essential arterial hypertension | |
| Essential hypertension | |
| Essential hypertension | |
| I15 Secondary hypertension | Arterial hypertension |
| Arterial hypertension | |
| Arterial hypertension of crisis course | |
| Arterial hypertension complicated by diabetes mellitus | |
| Arterial hypertension | |
| Vasorenal hypertension | |
| Sudden increase in blood pressure | |
| Hypertensive circulatory disorder | |
| Hypertensive state | |
| Hypertensive crises | |
| Hypertension | |
| Arterial hypertension | |
| Hypertension is malignant | |
| Hypertension, symptomatic | |
| Hypertensive crises | |
| Hypertensive crisis | |
| Hypertension | |
| Malignant hypertension | |
| Malignant hypertension | |
| Hypertensive crisis | |
| Exacerbation of hypertension | |
| Renal hypertension | |
| Renovascular hypertension | |
| Renovascular hypertension | |
| Symptomatic arterial hypertension | |
| Transient arterial hypertension | |
| I20 Angina [angina pectoris] | Heberden's disease |
| Angina pectoris | |
| Angina attack | |
| Recurrent angina | |
| Spontaneous angina | |
| Stable angina | |
| Angina syndrome X | |
| Angina pectoris | |
| Angina (attack) | |
| Angina pectoris | |
| Angina at rest | |
| Angina pectoris progressive | |
| Mixed angina | |
| Angina pectoris spontaneous | |
| Angina pectoris stable | |
| Chronic stable angina | |
| I21 Acute myocardial infarction | Left ventricular infarction |
| Myocardial infarction without Q wave | |
| Myocardial infarction in the acute period | |
| Non-transmural myocardial infarction (subendocardial) | |
| Acute myocardial infarction | |
| Myocardial infarction with and without pathological Q waves | |
| Transmural myocardial infarction | |
| Myocardial infarction complicated by cardiogenic shock | |
| Nontransmural myocardial infarction | |
| Acute phase of myocardial infarction | |
| Acute myocardial infarction | |
| Subacute stage of myocardial infarction | |
| Subacute period of myocardial infarction | |
| Subendocardial myocardial infarction | |
| Thrombosis of the coronary artery(s) | |
| Impending myocardial infarction | |
| I25 Chronic ischemic heart disease | Coronary heart disease due to hypercholesterolemia |
| Chronic ischemic heart disease | |
| Myocardial ischemia in arteriosclerosis | |
| Recurrent myocardial ischemia | |
| Coronary heart disease | |
| Stable ischemic heart disease | |
| Percutaneous transluminal angioplasty | |
| I47.1 Supraventricular tachycardia | Supraventricular paroxysmal tachycardia |
| Supraventricular tachyarrhythmia | |
| Supraventricular tachycardia | |
| Supraventricular arrhythmias | |
| Supraventricular paroxysmal tachycardia | |
| Supraventricular tachyarrhythmias | |
| Supraventricular tachycardia | |
| Neurogenic sinus tachycardia | |
| Orthodromic tachycardia | |
| Paroxysmal supraventricular tachycardia | |
| Paroxysm of supraventricular tachycardia | |
| Paroxysm of supraventricular tachycardia in WPW syndrome | |
| Paroxysm of atrial tachycardia | |
| Paroxysmal supraventricular tachyarrhythmia | |
| Paroxysmal supraventricular tachycardia | |
| Polytopic atrial tachycardia | |
| Atrial arrhythmia | |
| Atrial true tachycardia | |
| Atrial tachycardia | |
| Atrial tachycardia with AV block | |
| Reperfusion arrhythmia | |
| Berzold-Jarisch reflex | |
| Recurrent sustained supraventricular paroxysmal tachycardia | |
| Symptomatic ventricular tachycardias | |
| Wolff-Parkinson-White syndrome | |
| Sinus tachycardia | |
| Supraventricular paroxysmal tachycardia | |
| Supraventricular extrasystole | |
| Supraventricular arrhythmias | |
| Tachycardia from AV junction | |
| Supraventricular tachycardia | |
| Tachycardia orthodromic | |
| Sinus tachycardia | |
| Junctional tachycardia | |
| Chaotic polytopic atrial tachycardia | |
| I49.4 Other and unspecified premature depolarization | Extrasystolic arrhythmia |
| Extrasystole | |
| Extrasystole, unspecified | |
| I49.9 Heart rhythm disorder, unspecified | AV reentrant tachycardia |
| AV nodal reentrant tachycardia | |
| Antidromic reentrant tachycardia | |
| Arrhythmias | |
| Arrhythmia | |
| Cardiac arrhythmia | |
| Arrhythmia due to hypokalemia | |
| Ventricular arrhythmia | |
| Ventricular tachyarrhythmia | |
| High frequency of ventricular contraction | |
| Atrial fibrillation tachysystolic arrhythmia | |
| Heart rhythm disturbance | |
| Heart rhythm disturbances | |
| Heart rhythm disturbances | |
| Paroxysmal supraventricular arrhythmia | |
| Paroxysmal supraventricular arrhythmia | |
| Paroxysmal supraventricular tachycardia | |
| Paroxysmal rhythm disorder | |
| Paroxysmal atrioventricular rhythm | |
| Precordial pathological pulsation | |
| Cardiac arrhythmias | |
| Supraventricular tachyarrhythmia | |
| Supraventricular tachycardia | |
| Supraventricular arrhythmias | |
| Tachyarrhythmia | |
| Extrasystolic arrhythmia | |
| R07.2 Pain in the heart area | Pain syndrome during myocardial infarction |
| Pain in cardiac patients | |
| Cardialgia | |
| Cardialgia against the background of dyshormonal myocardial dystrophy | |
| Cardiac syndrome | |
| Cardioneurosis | |
| Myocardial ischemic pain | |
| Neuroses of the heart | |
| Pericardial pain | |
| Pseudoangina | |
| Functional cardialgia |
Isoptin is a calcium channel blocker that has antihypertensive and antiarrhythmic effects, reducing myocardial oxygen demand.
Release form and composition
Dosage forms of Isoptin:
- Film-coated tablets;
- Solution for intravenous administration.
Composition of tablets:
- 40 or 80 mg verapamil hydrochloride;
- Excipients: croscarmellose sodium, microcrystalline cellulose, calcium hydrogen phosphate dihydrate, magnesium stearate, colloidal silicon dioxide;
- Shell composition: sodium lauryl sulfate, hypromellose 3 mPa, titanium dioxide, macrogol 6000.
Isoptin tablets are sold in blisters:
- 10 pcs., 2 or 10 blisters per package;
- 20 pcs., 1 or 5 blisters per package.
One ampoule with solution contains:
- 5 mg verapamil hydrochloride;
- Additional components: 36% hydrochloric acid, sodium chloride and injection water.
The solution is sold in ampoules of 2 ml, 5 or 50 ampoules in a cardboard box.
Indications for use
Isoptin tablets are used for:
- Arterial hypertension;
- Paroxysmal supraventricular tachycardia;
- Coronary heart disease, incl. for angina caused by vasospasm, unstable angina, chronic stable angina;
- Atrial fibrillation or flutter accompanied by tachyarrhythmia (with the exception of Lown-Ganong-Levine and Wolff-Parkinson-White syndrome).
In the form of a solution, the drug is used for:
- Restoration of sinus rhythm in paroxysmal supraventricular tachycardia, including Lown-Ganong-Levine (LGL) and Wolff-Parkinson-White (WPW) syndromes;
- Controlling the frequency of ventricular contractions during atrial fibrillation and flutter, with the exception of LGL and WPW syndromes.
Contraindications
The use of Isoptin is contraindicated in:
- Cardiogenic shock;
- Sick sinus syndrome, with the exception of patients with an artificial pacemaker;
- Acute myocardial infarction, complicated by bradycardia, left ventricular failure and severe arterial hypotension;
- Chronic heart failure;
- AV block II or III degree, with the exception of patients with an artificial pacemaker;
- Atrial fibrillation/flutter in the presence of additional conduction pathways (with LGL and WPW syndromes).
In addition, the drug is not prescribed:
- In case of hypersensitivity to any component of Isoptin;
- Simultaneously with colchicine;
- Children and teenagers under 18 years of age;
- During pregnancy;
- When breastfeeding;
- Simultaneously with beta-blockers (in the case of intravenous use of Isoptin).
The drug is used with caution when:
- Bradycardia;
- Severe liver/kidney dysfunction;
- AV blockade of the first degree;
- Arterial hypotension;
- Diseases associated with neuromuscular transmission, including Duchenne muscular dystrophy, myasthenia gravis, Lambert-Eaton syndrome.
Directions for use and dosage
Isoptin solution is intended for slow intravenous injections with continuous monitoring of ECG and blood pressure. Enter it:
- slowly intravenously (over at least 2 minutes, for elderly people - 3 minutes) at an initial dose of 5 mg, if ineffective - at the same dosage again after 5-10 minutes;
- IV drip (to maintain the effect) at a dose of 5-10 mg/h in a glucose solution, physiological or other solution with a pH less than 6.5. The general dosage is 100 mg per day.
In the form of tablets, Isoptin should be taken with meals or immediately after meals, without breaking or chewing, with water.
At the beginning of treatment, 40-80 mg is prescribed three or four times a day. In the future, the dosage is determined individually, taking into account the type of disease and clinical picture.
The average daily dose is 240-480 mg, but the maximum dose can only be taken in a hospital.
Isoptin should not be discontinued abruptly; the dosage should be gradually reduced.
Side effects
When using Isoptin, the following side effects may occur:
- Hypersensitivity reactions;
- Dizziness, headache, paresthesia, increased fatigue, tremor, extrapyramidal disorders (stiffness of the arms and/or legs, mask-like face, ataxia, difficulty swallowing, tremors of the hands and fingers, shuffling gait);
- Arrest of the sinus node, marked decrease in blood pressure, tachycardia, peripheral edema, sinus bradycardia, AV block (grades I, II, III), heart failure, palpitations, flushing of the face;
- Nausea, vomiting, gum hyperplasia, intestinal obstruction, constipation, abdominal pain or discomfort;
- Pruritus, maculopapular rash, Stevens-Johnson syndrome, urticaria, angioedema, purpura, alopecia, erythema multiforme;
- Muscle weakness, arthralgia, myalgia;
- Tinnitus;
- Galactorrhea, erectile dysfunction, gynecomastia;
- Hyperprolactinemia, increased activity of liver enzymes.
An overdose of verapamil hydrochloride is manifested by a pronounced decrease in blood pressure, hyperglycemia, sinus bradycardia, turning into high-degree AV block, stupor, sinus node arrest and metabolic acidosis. There are data on cases of deaths. If the patient has taken too large a dose of Isoptin, gastric and intestinal lavage should be done, and activated charcoal should be taken. In the future, symptomatic and supportive therapy, parenteral administration of beta-agonists and calcium preparations are indicated. Hemodialysis is ineffective.
Special instructions
The concentration of verapamil in the blood can be increased by clarithromycin, erythromycin, telithromycin and antiviral drugs intended to treat HIV infection. Isoptin helps increase the concentration of sirolimus, tacrolimus, atorvastatin, lovastatin, carbamazepine.
With the simultaneous use of antiarrhythmic drugs and beta-blockers, a mutual increase in cardiovascular effects is observed, which is manifested by more pronounced AV blockade, a significant decrease in heart rate, the development of symptoms of heart failure and increased arterial hypotension.
In the case of combined use of Isoptin with quinidine, the hypotensive effect may be enhanced; in patients with hypertrophic obstructive cardiomyopathy there is a risk of developing pulmonary edema.
A decrease in antihypertensive effect is observed when the drug is combined with sulfinpyrazone and rifampicin.
Verapamil increases the neurotoxicity of lithium and enhances the effect of muscle relaxants.
During treatment with Isoptin:
- It is not recommended to drink alcoholic beverages;
- Care should be taken when driving a car and performing potentially dangerous types of work;
- Acetylsalicylic acid should be avoided.
Analogues
Verapamil, Verapamil-LekT, Verapamil Sopharma, Verapamil-ratiopharm, Verapamil-Ferein, Verapamil-Eskom, Verogalid ER 240, Isoptin SR 240, Finoptin.
Terms and conditions of storage
Isoptin should be stored in a dark place at a temperature of 15-25 ºС. Shelf life – 5 years.
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