Isoptin
Instructions for use:
- 1. Release form and composition
- 2. Indications for use
- 3. Contraindications
- 4. Method of application and dosage
- 5. Side effects
- 6. Special instructions
- 7. Drug interactions
- 8. Analogs
- 9. Terms and conditions of storage
- 10. Conditions for dispensing pharmacies
Prices in online pharmacies:
from 326 rub.
Buy
Isoptin is a drug with hypotensive, antiarrhythmic and antianginal effects.
Release form and composition
Isoptin is available in the following dosage forms:
- Film-coated tablets: white, biconvex, round; 40 mg each - with the inscription "40" on one side and engraving in the form of a triangle on the other; 80 mg each - with the inscription "ISOPTIN 80" on one side and a dividing line and the inscription "KNOLL on the other" (tablets of 40 and 80 mg: 10 pcs. in blisters, 2 or 10 blisters in a cardboard box; 20 pcs. in blisters, 1 or 5 blisters in a cardboard box; 80 mg tablets: 25 pcs. in blisters, 4 blisters in a cardboard box);
- Solution for intravenous administration: colorless, transparent (2 ml each in colorless glass ampoules, 5, 10 or 50 ampoules in trays or blisters, 1 blister or tray in a cardboard box).
The composition of 1 tablet includes:
- Active ingredient: verapamil - 40 or 80 mg (in the form of hydrochloride);
- Auxiliary components (40/80 mg, respectively): calcium hydrogen phosphate dihydrate - 70/140 mg; microcrystalline cellulose - 23/46 mg; colloidal silicon dioxide - 0.7 / 1.4 mg; croscarmellose sodium - 1.8 / 3.6 mg; magnesium stearate - 1.5 / 3 mg.
The composition of the film shell (40/80 mg, respectively): sodium lauryl sulfate - 0.1 / 0.1 mg; hypromellose 3 mPa - 1.7 / 2 mg; talc - 4 / 4.5 mg; macrogol 6000 - 2 / 2.3 mg; titanium dioxide - 1 / 1.1 mg.
The composition of 1 ampoule includes:
- Active ingredient: verapamil - 5 mg (in the form of hydrochloride);
- Auxiliary components: hydrochloric acid 36% - to bring the pH; sodium chloride - 17 mg; water for injection - up to 2 ml.
Indications for use
Isoptin in tablet form is prescribed for the treatment of the following diseases:
- Arterial hypertension;
- Paroxysmal supraventricular tachycardia;
- Ischemic heart disease, including unstable angina pectoris, chronic stable angina pectoris (classic exertional angina), Prinzmetal's angina (angina pectoris caused by vasospasm);
- Atrial fibrillation / flutter accompanied by tachyarrhythmia (except for Laun-Ganong-Levin (LGL) and Wolff-Parkinson-White (WPW)).
The drug in the form of a solution for intravenous administration is used in the treatment of supraventricular tachyarrhythmias. Isoptin is prescribed for the following indications:
- Restoration of sinus rhythm in paroxysmal supraventricular tachycardia, including conditions associated with the presence of additional pathways (Laun-Ganong-Levin and Wolff-Parkinson-White syndromes);
- Control of the ventricular rate during atrial fibrillation and atrial flutter (tachyarrhythmic variant), except in cases where atrial fibrillation or atrial flutter is associated with the presence of additional pathways (Laun-Ganong-Levin and Wolff-Parkinson-White syndromes).
Contraindications
- AV block II-III degree (except for patients with an artificial pacemaker);
- Syndrome of weakness of the sinus node (syndrome "bradycardia-tachycardia", except for patients with an artificial pacemaker);
- Atrial fibrillation / flutter in the presence of additional conduction pathways (Laun-Ganong-Levin and Wolff-Parkinson-White syndrome);
- Age under 18 years (the effectiveness and safety of the drug for this age group of patients have not been established);
- Hypersensitivity to drug components.
Additional contraindications for taking Isoptin in tablet form are:
- Chronic heart failure;
- Acute myocardial infarction, complicated by severe arterial hypotension, bradycardia and left ventricular failure;
- Cardiogenic shock;
- Simultaneous reception with colchicine.
Intravenous administration of Isoptin is contraindicated in the presence of the following diseases / conditions:
- Arterial hypotension or cardiogenic shock (other than those caused by arrhythmia);
- Morgagni-Adams-Stokes syndrome;
- Sinoauricular block;
- Ventricular tachycardia with wide QRS complexes (more than 0.12 seconds);
- Chronic heart failure IIB-III stage (except caused by supraventricular tachycardia, which should be treated with verapamil);
- Pre-use of disopyramide (within 48 hours);
- Simultaneous intravenous administration of beta-blockers;
- Pregnancy and lactation.
Isoptin in all medicinal forms should be used with caution in bradycardia and AV block of the 1st degree.
Inside, the drug is prescribed with caution for severe functional disorders of the kidneys and liver, arterial hypotension, diseases related to neuromuscular transmission, including Lambert-Eaton syndrome, myasthenia gravis and Duchenne muscular dystrophy.
Intravenous administration is recommended with caution in elderly patients, as well as in the following diseases: heart failure, severe aortic stenosis, myocardial infarction with left ventricular failure, mild or moderate arterial hypotension, renal and / or hepatic failure.
Method of administration and dosage
Isoptin in the form of tablets is taken orally, swallowing whole (you cannot chew or dissolve) and washed down with water. It is preferable to take the drug during or immediately after a meal.
The scheme of using Isoptin is determined individually, taking into account the severity of the disease and the clinical picture.
For all recommended indications, the average daily dose is 240-480 mg. With prolonged therapy, the daily dose of 480 mg should not be exceeded. At the maximum daily dose, Isoptin should be taken only in a hospital setting.
The initial single dose is 40-80 mg, the frequency of administration is 3-4 times a day.
Patients with functional disorders of the liver are recommended to start therapy with a single dose of 40 mg. Frequency rate of admission - 2-3 times a day. In the future, the doctor selects the dose individually.
Isoptin in the form of a solution for injection can only be administered intravenously.
The introduction should be carried out slowly with continuous monitoring of the ECG and blood pressure for at least 2 minutes (in elderly patients - 3 minutes, which reduces the risk of undesirable effects).
The initial dose is 5-10 mg (0.075-0.15 mg / kg body weight). In case of an inadequate response to the first injection, a repeated dose (10 mg) can be administered after 30 minutes.
Side effects
During therapy, the development of disorders from some body systems is possible:
- Digestive system: pain and discomfort in the abdomen, vomiting, nausea, constipation, intestinal obstruction; in some cases - a transient increase in the blood plasma of the activity of hepatic transaminases and alkaline phosphatase; rarely - gingival hyperplasia (soreness, bleeding, swelling), increased appetite, diarrhea;
- Cardiovascular system: severe bradycardia, facial redness, atrioventricular blockade, a marked decrease in blood pressure, the appearance of symptoms of heart failure when using high doses of the drug, especially in predisposed patients; palpitations, tachycardia, arrest of the sinus node; rarely - arrhythmia (including flutter and fibrillation of the ventricles), angina pectoris up to the development of myocardial infarction (especially in patients with severe obstructive coronary artery disease), bradycardia;
- Nervous system: general weakness, anxiety, depression, drowsiness, extrapyramidal disorders (stiffness of the legs or arms, ataxia, shuffling gait, mask-like face, difficulty swallowing, trembling of hands and fingers), headache, dizziness, convulsions during drug administration, tremor, paresthesia; in rare cases - lethargy, increased nervous irritability, fatigue;
- Allergic reactions: exudative erythema multiforme, facial flushing, skin rash, itching, Stevens-Johnson syndrome, bronchospasm;
- Others: weight gain; very rarely - arthritis, agranulocytosis, transient blindness at the peak of drug concentration in the blood, asymptomatic thrombocytopenia, pulmonary edema, development of peripheral edema, fatigue, hyperprolactinemia, gynecomastia, impotence, galactorrhea, muscle weakness, increased sweating, joint pain, myalgia.
Most of the listed side effects are typical for all dosage forms of Isoptin.
special instructions
It is impossible to abruptly cancel taking Isoptin. It is recommended to reduce the dose gradually until therapy is completely discontinued.
Intravenous administration of Isoptin can cause a transient decrease in blood pressure, which is usually not clinically manifested, but may be accompanied by the development of dizziness.
Insufficiency of blood circulation (except for severe or caused by arrhythmia) before starting therapy with Isoptin must be compensated for with diuretics and cardiac glycosides. In patients with severe to moderate heart failure during therapy, there may be an acute progression of circulatory failure.
The solution does not contain antimicrobial or bacteriostatic agents and is intended for simultaneous intravenous administration.
Isoptin remains stable for at least 24 hours (when stored at temperatures up to 25 ° C in a dark place) in most large volume parenteral solutions. After taking a portion of the contents of any volume, the unused solution should be immediately destroyed.
To avoid disturbance of stability, it is not recommended to dilute Isoptin with sodium lactate solutions in plastic bags made of polyvinyl chloride. Avoid mixing Isoptin solutions with amphotericin B, albumin, hydralazine hydrochloride or trimethoprim and sulfamethoxazole.
Verapamil hydrochloride precipitates in any solution with a pH greater than 6.
Isoptin, depending on individual characteristics, can change the reaction rate, impairing the ability to drive a car and perform work requiring increased attention.
Drug interactions
With the simultaneous use of Isoptin with inhibitors of the isoenzyme CYP3A4, an increase in the concentration of verapamil in the blood plasma is observed, with inducers of the isoenzyme CYP3A4 - a decrease in its concentration (interaction should be taken into account while using such agents)
With the simultaneous use of Isoptin with some drugs, undesirable effects may occur (C ss - the average equilibrium concentration of the substance in the blood plasma, C max - the maximum concentration of the substance in the blood plasma, AUC - the area under the pharmacokinetic curve "concentration-time", T1 / 2 - half-life):
- Prazosin: an increase in its C max, T 1/2 of prazosin does not change;
- Terazosin: an increase in its AUC and C max;
- Quinidine: decrease in its clearance;
- Theophylline: decrease in its systemic clearance;
- Carbamazepine: an increase in its AUC in patients with persistent partial epilepsy;
- Imipramine: increasing its AUC; on the concentration of the active metabolite of imipramine - desipramine, Isoptin has no effect;
- Glibenclamide: an increase in its C max and AUC;
- Clarithromycin, erythromycin, telithromycin: an increase in the concentration of verapamil is possible;
- Rifampicin: decrease in AUC, C max and oral bioavailability of verapamil;
- Doxorubicin: an increase in its AUC and C max in patients with small cell lung cancer;
- Phenobarbital: increased clearance of verapamil;
- Buspirone, midazolam: an increase in their AUC and C max;
- Metoprolol, propranolol: an increase in their AUC and C max in patients with angina pectoris;
- Digitoxin: a decrease in its total and extrarenal clearance;
- Digoxin: an increase in its C max, AUC and C ss;
- Cimetidine: an increase in the AUC of the R-enantiomer and S-enantiomer of verapamil with a corresponding decrease in the clearance of R- and S-verapamil;
- Cyclosporin: an increase in its AUC, C ss, C max;
- Sirolimus, tacrolimus, lovastatin: their concentration may increase;
- Atorvastatin: an increase in its concentration and AUC is possible;
- Simvastatin, almotriptan: an increase in their AUC and C max;
- Sulfinpyrazone: an increase in the clearance of verapamil and a decrease in its bioavailability;
- St. John's wort: a decrease in the AUC of the R-enantiomer and the S-enantiomer of verapamil with a corresponding decrease in C max;
- Grapefruit juice: an increase in AUC and C max of the R-enantiomer and S-enantiomer of verapamil (renal clearance and T 1/2 do not change);
- Terazosin, prazosin: additive hypotensive effect;
- Diuretics, antihypertensive drugs, vasodilators: increased antihypertensive effect;
- Ritonavir and other antiviral agents for the treatment of HIV infection: it is possible to inhibit the metabolism of verapamil, which can lead to an increase in its concentration in the blood plasma (while using the Isoptin dose, it should be reduced);
- Quinidine: it is possible to increase the hypotensive effect; in patients with hypertrophic obstructive cardiomyopathy, pulmonary edema may develop;
- Carbamazepine: increasing its concentration in blood plasma; possible development of adverse reactions characteristic of carbamazepine (headache, diplopia, dizziness or ataxia);
- Lithium: increasing its neurotoxicity;
- Rifampicin, sulfinpyrazone: it is possible to reduce the hypotensive effect of verapamil;
- Muscle relaxants: it is possible to enhance their effect;
- Acetylsalicylic acid: increased bleeding;
- Colchicine: a significant increase in its concentration in the blood is possible;
- Ethanol (alcohol): an increase in its concentration in blood plasma;
- Beta-blockers, antiarrhythmics: mutual enhancement of cardiovascular effects (more significant decrease in heart rate, more pronounced AV block, increased arterial hypotension and the development of symptoms of heart failure).
Patients taking Isoptin, treatment with lipid-lowering drugs - inhibitors of HMG-CoA reductase (lovastatin, simvastatin, atorvastatin), should be started with the lowest possible doses, which are gradually increased with continued therapy. If it is necessary to use Isoptin in patients already receiving HMG-CoA reductase inhibitors, it is necessary to consider the possibility of reducing the dose of statins and re-titrating the dose, taking into account the concentration of cholesterol in serum. Fluvastatin, rosuvastatin and pravastatin are not metabolized by the CYP3A4 isoenzyme, so their interaction with verapamil is the least likely.
Analogs
Isoptin analogues are: Isoptin SR 240, Verapamil, Verapamil Sopharma, Verapamil Darnitsa, Verapamil-Eskom, Verogalid ER 240, Verapamil hydrochloride, Finoptin, Lekoptin.
Terms and conditions of storage
Keep out of the reach of children at a temperature: tablets - 15-25 ° C, solution for intravenous administration - up to 25 ° C.
The shelf life is 5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Isoptin: prices in online pharmacies
|
Drug name Price Pharmacy |
|
Isoptin SR 240 240 mg film-coated tablets of prolonged action 30 pcs. 326 RUB Buy |
|
Isoptin SR 240 tablets p.o. with prolonged release. 240mg 30 Pcs. 388 r Buy |
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
