Isoptin

When we have increased blood pressure and other cardiac arrhythmias that cause a worsening of the general condition, we seek help with medicines that have a positive effect on the cardiovascular system. Isoptin is one of the heart drugs that normalize the work of the heart and blood vessels.

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Indications Isoptin

Indications for use of "Isoptin" are also slightly different if they are considered relative to what is prescribed by a doctor: taking pills or injecting.

For example, the purpose of tablets is justified in such situations:

• diagnosed with hypertension (stable high blood pressure),
• with hypertensive crisis,
• thickening of the wall of one of the cardiac ventricles (diagnosis: hypertrophic cardiomyopathy),
• for the treatment of cardiac ischemia (vasospastic, chronic stable and unstable angina),
• with heart rhythm disturbances: sudden attacks of rapid heartbeat (paroxysmal supraventricular tachycardia (PNT), which is one of the variants of arrhythmia), tachyarrhythmic form of atrial fibrillation (flickering and fluttering of the atria), the appearance of additional inferior cardiac contractions (supraventricular extrasystole).

Isoptin in the form of injection solution is used as a monotherapy for mild forms of hypertension and as part of complex treatment for its severe, complicated manifestations, with angiospastic angina (against the background of vasospasm) and angina pectoris. But most often it is used for the treatment of supraventricular tachyarrhythmias, when it is necessary to restore the normal rhythm of the heart with PNT, and also to correct the heart rate in atrial fibrillation of tachyarrhythmic type (with the exception of Wolff-Parkinson-White and Low-Ganong-Levin syndromes).

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Release form

On sale it is possible to find such medicinal forms of the preparation "Isoptin":

Tablets ordinary 40 mg (white in a film shell, rounded, convex on both sides, on one side is engraved the figure 40, on the other - the sign of a triangle). The tablets are placed in blisters:

• on 10 pieces (in packing or 2, or 10 blisters),
• on 20 pieces (in packing or 1, or 5 blisters).

Tablets of ordinary 80 mg (white in a film shell, round in shape, convex on both sides, on one side there is an inscription "ISOPTIN 80", on the other - "KNOOL" and risk for dividing the tablet into 2 parts). Tablets are packaged in blisters:

• on 10 pieces (in packing or 2, or 10 blisters),
• on 20 pieces (in packing or 1, or 5 blisters),
• on 25 pieces (in packing 4 blisters).

Tablets CP240 prolonged (prolonged) action 240 mg (light green hue, elongated shape resembling capsules, on the one hand are engraved with 2 identical triangles, the risks for division are on both sides). Tablets in blisters:

• for 10 pieces (in the package 2,3,5 or 10 blisters),
• on 15 pieces (in a package 2,3,5 or 10 blisters),
• for 20 pieces (in the package 2.3.5 or 10 blisters).

Solution for intravenous administration in glass colorless ampoules of 2 ml (a clear liquid that does not have a specific color). Ampoules are placed in transparent pallets of 5, 10 and 50 pieces. Each pallet is packed in a separate box of thin cardboard.

The main active substance of the drug "Isoptin" is verapamil, which is presented as a hydrochloride. It is known to many by the drug of the same name.

The composition of "Isoptin" has some differences depending on the form of release of the drug. Thus, the tablets may contain 40, 80 or 240 mg of the main active ingredient plus the adjuvants present in the tablet or its envelope.

Auxiliary components in tablets "Isoptin":

• pyrogenic, or colloidal silicon dioxide as an adsorbent,
• dicalcium phosphate dihydrate as a light source of calcium,
• croscarmellose sodium as a disintegrant,
• microcrystalline cellulose for cleaning the body,
• magnesium stearate to give the composition of tablets a uniform consistency.

In turn, the film membrane of the tablets consists of talc, hypromellose 3 mPa, sodium lauryl sulfate, macrogol and titanium dioxide.

Ampoule solution Isoptin, in addition to hydrochloride verapamil in an amount of 5 mg contains: NaCl and hydrochloric acid (HCl) at a concentration of 36%, diluted with water for injection. 

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Pharmacodynamics

Isoptin belongs to the group of antianginal drugs, which are called calcium antagonists. These drugs help reduce the need for the main cardiac muscle in oxygen, provide a vasodilating effect against the coronary arteries and protection against overloading them and 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.

Possessing a vasodilator effect, it helps reduce blood pressure by decreasing the resistance of peripheral vessels without increasing the heart rate (a frequent reflex reaction). The anti-anginal effect of Isoptin in the treatment of angina is based on its relaxing effect on cardiomyocytes (muscle cells constituting the heart wall), as well as on reducing the tone of peripheral vessels, thereby reducing the load on the atrium. Reducing the flow of calcium ions to the myocytes leads to inhibition of the conversion of energy into work, and hence to a slowing of the heart rate.

The use of "Isoptin" in the therapy of supraventricular tachyarrhythmias is justified due to its ability to delay the passage of nerve impulses from the atrioventricular node, block the conductivity of the sinoatrial node, and reduce the duration of the refractory period in the atriventicular plexus. Thus, the optimal heart rate and the restoration of the normal (sinus) rhythm of the heart are achieved.

The drug has a selective effect and belongs to the group of dose-dependent drugs. If the disease occurs with the preservation of normal heart rate, then the drug will not affect them, and if the heart rate decreases, it is insignificant.

In addition to antianginal and vasodilating (relaxation of the muscles of the vessels), the action behind the drug was marked by a diuretic (diuretic) effect.

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Pharmacokinetics

The active substance of the preparation "Isoptin" is absorbed almost 90% in the intestine, and its assimilation does not depend on the intake of food. Indicators of bioavailability of the drug range from 10 to 35%, both with oral administration of tablets, and with intravenous infusion of the solution.

In CHD and hypertension, there is no correlation 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 exposed to biotransformation. It is relatively easy to pass through the placenta tissue, as about 25% of the drug is found in the vessels of the navel.

The only active metabolite of Isoptin is noravapamil. The maximum concentration in the blood is observed after 6 hours after taking 1 dose of the drug. The parameters of the half-life can vary significantly (2.5-7.5 hours with a single admission and 4.5-12 hours with repeated administration). When using a solution for IV injections, the half-life of the drug can be from 4 minutes to 5 hours.

The therapeutic concentration of the drug in the blood is observed on the 5th day after the repeated administration of the drug.

Isoptin is able to penetrate and excrete from the body together with breast milk, but its content there is so small that it does not cause unwanted symptoms in the infant. The half-life in this case will be of the order of 3-7 hours, but with repeated admission it can increase to 14 hours.

Most of the drug "Isoptin" and its metabolites is excreted by the kidneys and only 16% is eliminated through the intestine.

In the case of long-acting tablets, the removal 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. The second day marked the withdrawal of 60%, and the 5th - 70% of the drug.

In patients with renal insufficiency and severe forms of liver failure, the half-life is prolonged and bioavailability is increased.

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Dosing and administration

To help your heart carry out its hard work and not bring other ills, you need to listen carefully to the doctor's recommendations for taking medications. The advice of girlfriends and neighbors will suit, if it is a question of a recipe for a delicious cake or a roast, but not about taking any other drugs, especially cardiac ones. When it comes to our "motor," the strict dosage and method of administration of cardiac medications is the key to not only effective but also safe treatment.

"Isoptin" refers to drugs that improve the work of the heart, and therefore all of the above applies to it in full.

So, how to correctly take the drug to cure one, do not maim the other. In the instruction to the preparation it is noted that the reception of "Isoptin" in tablets is desirable to be combined with food intake, or to take the drug immediately after eating. In this case, the tablet form of the preparation is not intended for resorption or grinding of it when taken. Tablets (usual and prolonged action) must be swallowed whole, washed down with water in sufficient quantities (usually take half a cup of water). This ensures a gentle effect on the gastric mucosa, and optimal conditions for absorption of this dosage form are created.

The taking of tablets is done internally orally, i.e. Through the mouth. They are not used for any other purposes. Dosage depends on the patient's age and, of course, on the diagnosis.

Adult patients: the initial daily dose for angina pectoris, atrial fibrillation and hypertensive disease, depending on the severity of the pathology and the reaction of the body varies from 120 to 240 mg. In the case of hypertension, the dosage (according to the indications of the attending physician) can be increased to 480 mg, and with cardiomyopathy temporarily even up to 720 mg per day. The recommended frequency of reception is 3 times a day.

The effective dose for prolonged-action tablets ranges from 240 to 360 mg. Long-term use of the drug does not allow you to increase the dose above 480 mg per day, except for a short time.

If the patient has abnormalities in the liver, recommended the taking of tablets with a minimum dosage. The daily dose at 2-3 times will be 80-120 mg.

Isoptin solution can be used only for intravenous injections. It is shown the slow administration of the drug, for at least 2 minutes. It is necessary to monitor the indicators of blood pressure and heart rate. In elderly patients, the drug should be administered more slowly (at least 3 minutes).

The effective initial dose is calculated based on the ratio: 1 kg of the patient's weight should be from 0.075 to 0.15 mg of the drug in solution. Usually it 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 do another injection with a dosage of 10 ml.

The duration of the therapeutic course is set individually by the attending physician.

Children: dosage depends on the age of the small patient. Despite the fact that "Isoptin" can be used even for the treatment of newborns, doctors prefer to resort to this practice very rarely, if other options for therapy are not available at present, in order to avoid possible serious consequences (isolated cases of death of the child after injection). Dosage for newborns is from 0.75 to 1 mg (for children up to 12 months - up to 2 mg), which in terms of the solution will be 0.3-0.4 (0.3-0.8) ml.

The effective dose of "Isoptin" for children over the age of 5 years is 2-3 mg (in the form of a solution - 0.8-1.2 ml), for children over 5 years (up to 14 years) - from 2.5 to 5 mg (in the form of a solution - from 1 to 2 ml).

Before using Isoptin in children, it is advisable to take a course with drugs based on digitalis or its derivatives, which will help reduce the symptoms of heart failure and reduce the course of treatment with Isoptin.

[10], [11], [12]

Use Isoptin during pregnancy

Use of the drug "Isoptin" during pregnancy and breastfeeding is considered unsafe because of the lack of proven in practice information about its effect on pregnancy and fetal health. Theoretically, the drug is considered quite safe, so if the risk of using the drug is supposedly less than the expected benefit, it can be prescribed in a tablet form by the doctor's indication even during pregnancy. But breastfeeding for the duration of therapy with the drug will have to stop.

Contraindications

Isoptin, like most cardiac drugs, has a lot of contraindications to use, which must be taken into account in order to avoid sad, and sometimes tragic, consequences.

Common contraindications for all forms of the drug are:

• impairment of conduction of nerve impulses from the atria to the ventricles (atrioventicular blockade of 2 and 3 degrees), if it is not controlled by a special pacemaker,
• the 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 Laun-Ganong-Levin syndromes,
• intolerance of individual components of the drug.

Do not apply the drug and to treat patients younger than 18 years. This is due to the lack of information about the effect of "Isoptin" on children's body.

It is considered undesirable to prescribe the drug to patients with 1 degree of atrioventicular blockade, as well as those with a heart rate of less than 50 beats per minute. If the upper pressure indicator of the patient is below 90 mm Hg he will also have to choose another drug.

The taking of tablets is also contraindicated:

• with acute myocardial infarction against a background of greatly reduced pressure and pulse, complicated by the failure of the function of the left cardiac ventricle,
• severe cases of left ventricular failure (cardiogenic shock),
• with the therapy "Colchicine", used to treat gout.

Contraindications to use the drug as a solution:

• Stably low blood pressure (arterial hypotension),
• cardiogenic shock, if it did not arise from a violation of the heart rhythm,
• syncope caused by sudden acute cardiac arrhythmia (Morgagni-Adams-Stokes syndrome),
• slowing or completely stopping the delivery of a pulse from the sinus node to the atria (sinoauric blockade),
• increased heart rate due to rapid operation of the cardiac ventricles (ventricular tachycardia),
• chronic heart failure, if its cause is not supraventricular tachycardia,
• periods of pregnancy and lactation,

Injections of Isoptin are not done within 2 days after the end of therapy with Dizopiramid. The simultaneous introduction of "isoptin" and beta-blockers is not practiced either.

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Side effects Isoptin

It is possible that even the correct administration of the drug depending on the individual characteristics of the patient's body and its response to a certain drug may be accompanied by symptoms that are not related to the main purpose of the drug. It is about the side effects of drugs that can be positive (useful), but more often than not it is the exact opposite.

So, the reception of "Isodinite" can be accompanied by some unpleasant symptoms, which occur with different frequency.

GASTROINTESTINAL TRACT can react to a preparation by occurrence of some problems with digestion. Most often, patients taking Isoptin, there are violations of stool in the form of constipation, nausea, much less often diarrhea. Some people note an increase in appetite, others have a noticeable swelling of the gums on the background of the drug, which subsequently begin to ache and bleed, while others complain of an intestinal obstruction. If the patient has certain abnormalities in the functioning of the liver, an increase in the level of enzymes (hepatic transaminase and alkaline phosphatase) can be observed in the blood.

Some undesirable disturbances can be observed in the work of the cardiovascular system. The most frequent of them are a bradycardia (pulse less than 50 beats per minute) or, on the contrary, a quickening of the pulse at rest (tachycardia), a sufficiently strong decrease in pressure (hypotension), an increase in the symptoms of heart failure. But the appearance or intensification of angina symptoms is rare, although sometimes this condition against a background of severe coronary artery disease can be accompanied by myocardial infarction. Far from frequent are cases of heart rhythm disturbances, including fibrillation / flutter of the ventricles (arrhythmias).

It was noted above that intravenous injections should be carried out slowly, otherwise the following life-threatening conditions may occur: complete cessation of the arrival of impulses from the atrium to the ventricles (AV blockade of the third degree), a strong decrease in pressure with the development of acute vascular insufficiency (collapse), stopping heart (asystole).

Central and peripheral nervous systems for taking "Isonidine" can respond with headaches, dizziness, short-term loss of consciousness (fainting). Some patients report increased fatigue, retardation of reactions and drowsiness, while in others, taking medication can cause depressive conditions with increased anxiety. Also in some cases, tremors of hands and hands, impaired swallowing, kinetic disorders in the work of upper and lower extremities, shuffling gait, etc. Are observed.

Among the reactions of the immune system, you can identify such allergic manifestations as skin rashes, itchy skin, reddening of the skin, the development of Stevens-Johnson syndrome.

Among the other side effects of the drug, weight gain, swelling of the lungs and extremities, increased platelet count (thrombocytopenia), a decrease in the level of leukocytes (agranulocytosis), an increase in the mammary glands (gynecomastia) and the appearance of secretions from them (galactorrhea), an increase in the hormone prolactin (hyperprolactinemia) , pathology of the joints.

With intravenous administration of large doses of the drug when they accumulate in the blood plasma, there may be a temporary loss of vision.

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Overdose

In principle, the therapy with large doses of Isoptin should be performed in a hospital under the supervision of the attending physician, which in most cases excludes overdose by the drug. If, for some reason, this happens, you need to take all the necessary measures urgently to remove the drug particles from the body as soon as possible.

How can I tell if there is an overdose? Most likely on the basis of available signs:

• a very strong fall in blood pressure indicators up to critical levels,
• complete loss of consciousness on the background of taking the drug,
• state of shock,
• the appearance of symptomatic AV blockade of the heart 1 or 2 degrees, and sometimes even possible the onset of a complete blockade (grade 3),
• the appearance of signs of ventricular tachycardia,
• sinus bradycardia with a pulse rate below 55 beats per minute.

Sometimes during the reception of "Isoptin" in large doses (especially with intravenous administration), there were cases of cardiac arrest. And it was not always possible to save the patients.

The severity of the symptoms of an overdose depends on the dose of the drug taken by the patient, the age of the patient, the timeliness and completeness of first aid, consisting in stopping the process of intoxication of the body.

If everything indicates an overdose of "Isoptin" tablets, you must first take measures to remove the drug from the digestive tract. To this end, you can cause the patient to vomit (by mechanical action on the root of the tongue or taking emetics), to carry out measures for washing the stomach and releasing the intestines (enema, laxatives). With critically weak intestinal motility and in the case of using prolonged action tablets, stomach washing activities are relevant even within 12 hours after taking the drug.

If the prolonged form of the drug was used in the therapy of diseases, it should be taken into account that its effect can be felt within the next 2 days, during which the particles of the tablets will be released in the intestines where their absorption and transport to the blood take place. Individual particles of the drug can be located along the entire gastrointestinal tract, creating additional foci of poisoning, which can not be removed by routine gastric lavage.

In the event of cardiac arrest, routine resuscitation measures (direct and indirect cardiac massage, artificial respiration) are performed.

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 drip (rate of administration of 5 mmol per hour).

Cardiac arrest, AV blockade, sinus bradycardia in addition to electrostimulation of the heart require the appointment of the following drugs: "Isoprenaline", "Orciprenaline", drugs atropine series.

With a strong decline in blood pressure indicators, Dopamine, Dobutamine, and Noradrenaline are used. If there is a persistent symptomatology of myocardial insufficiency, the first 2 drugs in combination with calcium intake will be useful.

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Interactions with other drugs

The heart drug "Isoptin" has the ability to react with many drugs, therefore, it is necessary to inform the attending physician about taking any other drug during therapy with "Isoptin" to avoid unpleasant and dangerous consequences, including an overdose of verapramil.

So, the simultaneous administration of "Isoptin" and drugs that lower the pressure, leads to the fact that the effect of both drugs is significantly 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 blockade of the heart or heart failure increases if Isoptin is taken together with beta-blockers, arrhythmia drugs, drugs for inhalation anesthesia. This is due to the increased oppressive effect of drugs on the conductivity and work of the sinus node and cardiac myocardium.

"Isoptin" with the parallel taking of some drugs (antihypertensive drugs aliskirena ("Racileus"), tranquilizers based on buspirone (Spitomin, Buspiron), cardiac glycoside Digoxin, pro-vivo antibiotic Doxorubicin, remedy for gout "Kolkhitsin ", Bronchodilator" Theophylline "and antiarrhythmic drug" Quinidine ") is able to increase their concentration in blood plasma, strengthening their action and provoking the development of side effects. Most often, there is an excessive pressure drop or the development of the AV blockade.

An increase in the concentration of drugs in the blood under the influence of "Isoptin" is observed when it is simultaneously taken with alpha-blockers "Prazozin" and "Terazozin", immunosuppressant "Ciclosporin", anticonvulsant "Karmazepin", antiepileptic drug "Valproic acid" and muscle relaxants.

It is possible to increase the blood content of the active substance of the sedative medication "Midazolam" and ethanol with simultaneous therapy with these drugs and "Isoptin".

Simultaneous reception of "Isoptin" with antiarrhythmic drugs "Amidaron" and "Desopyramid" provokes a significant decrease in the force of the heartbeats, causing bradycardia and collapse, reduction in conduction of impulses in the heart, AV blockade of various degrees.

Simultaneous therapy "with isoptin and antiarrhythmic drug" Flecainide "can adversely affect the contractility of the main cardiac muscle and slow the AV conduction.

"Isoptin" can enter into a drug interaction with some statins (atorvastatin, lovastatin, simvastatin), since it extinguishes the action of the isoenzyme CYP3A4, which takes part in the metabolism of the above statins. In this case, the level of statins in the blood plasma increases, which can lead to the destruction of cells of muscle tissue.

With the intravenous administration of veraptamyl drugs, patients undergoing beta-blocker therapy are at high risk for a significant drop in blood pressure and cardiac arrest.

Strengthening the antianginal action of "Isoptin" is observed against the background of a parallel intake of nitrates used to treat cardiac ischemia.

The intake of acetylsalicylic acid against the background of therapy with "Isoptin" increases the likelihood of various bleeding.

It is also potentially dangerous that the combination of Isoptin with the muscle relaxant Dantrolen is considered, since their interaction can cause the death of a patient associated with the development of ventricular fibrillation.

Nonsteroidal anti-inflammatory drugs (Diclofenac), anti-tuberculosis drug Rifampicin, barbiturates (Phenytoin, Phenobarbital) and nicotine are able to 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 useful actions of Isoptin are noticeably weakened.

But the antiulcer drug "Cimetidine", on the contrary, strengthens the action of verapamil, which is a part of the tablets "Isoptin". But it has no effect on the kinetic features of Isoptin when administered intravenously.

The results of the interaction of Isoptin and the antidepressant Imipramine (Melipramine) are visible on the cardiogram in the form of indices indicating a decrease in atrioventricular conduction.

It is not advisable to carry out simultaneous therapy with an antiperpentensive drug "Clonidine" ("Clofelin"), since there is a risk of cardiac arrest.

It is difficult to predict the results of drug interaction with lithium preparations (lithium carbonate). Possible such dangerous situations as the development of severe bradycardia and a violation of the structure and functions of the nervous system (neurotoxicity). Sometimes there is a decrease in the content of lithium in the blood, which negatively affects the patient's mental health.

The administration of the neuroleptic "Sertindol" ("Serdolect") against the background of therapy with "Isoptin" increases the likelihood of developing ventricular arrhythmias.

"Isoptin" is able to enhance the miorelaksiruyuschee action of chlorides of tubocurarine and vecuronium.

Estrogens and sympathomimetics can significantly reduce the hypotensive effect of Isoptin.

The use of anesthetics ("Enflurane", "Etomidat") during treatment with "Isoptin" should be carried out with caution, as the latter can prolong the action of anesthesia, significantly inhibiting the activity of the cardiovascular system.

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Storage conditions

The storage conditions of various forms of the drug provide for the preservation of its effectiveness for the specified time at a temperature not exceeding 25 degrees. Keep away from children.

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Special instructions

It is not forbidden to apply Isoptin and alpha-blockers during combined therapy of angina and hypertension. But in this case, intravenous administration of alpha-blockers is not allowed.

The drug can cause individual reactions of drowsiness and dizziness, which will negatively affect the performance of work that requires increased attention.

When treating "Isoptin" you need to refrain from smoking and drinking alcohol.

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Shelf life

Store solution and tablets "Isoptin" can be no more than 5 years. Shelf life of the drug prolonged action is 36 months (3 years). 

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