Isoptin SR 240, retard pills 240mg, 30pcs

Composition

Active ingredient: verapamil hydrochloride 240 mg. Auxiliary substances: microcrystalline cellulose – 78.8 mg, sodium alginate-320.0 mg, povidone-KZO-48.0 mg, magnesium stearate-3.2 mg, water-30.0 mg. Film coating: hypromellose-2910 – 4.90 mg, macrogol-400 – 1,26 mg, macrogol-6000 – 0,84 mg, talc – of 8.40 mg, titanium dioxide – 6,16 mg, lacquer aluminum: the dye quinoline yellow (E 104) + dye Indigo Carmine (E 132) – 0,14 mg, wax mountain glycol and 0.30 mg.

Pharmacological action

Calcium channel blocker. Inhibits the transmembrane flow of calcium ions into the smooth muscle cells of the myocardium and blood vessels. It has antianginal, antiarrhythmic and antihypertensive effects.

The antianginal effect is associated with a direct effect on the myocardium and an effect on peripheral hemodynamics (reduces the tone of peripheral arteries, OPSS). The blockade of calcium ions entering the cell leads to a decrease in the transformation of the energy contained in the macroergic ATP bonds into mechanical work and to a decrease in myocardial contractility.

The antihypertensive effect of the drug is due to a decrease in peripheral vascular resistance without a reflex increase in heart rate. Blood pressure begins to decrease immediately on the first day of treatment, and this effect persists with long-term therapy. The drug Isoptin SR 240 is used for the treatment of all types of arterial hypertension: for monotherapy of mild or moderate arterial hypertension, in combination with other antihypertensive agents, especially with diuretics and (in accordance with recent observations) ACE inhibitors, the drug has a vasodilating, negative ino – and chronotropic effect.

The drug has a pronounced antiarrhythmic effect, especially effective in supraventricular arrhythmia. Delays the conduction of the pulse in the AV node, as a result of which the sinus rhythm is restored and/or the heart rate is normalized, depending on the type of arrhythmia. Normal heart rate does not change or decreases slightly.

Pharmacokinetics

Suction

When taken orally, it is rapidly and almost completely absorbed in the small intestine. The degree of absorption is 90-92%. The average systemic bioavailability in healthy volunteers after a single dose of the drug is 22%. Studies in patients with atrial fibrillation or angina have shown that the average bioavailability levels are 35% and 24% after a single oral dose and an intravenous dose, respectively. With repeated use of the drug, bioavailability increases almost 2-fold compared to a single dose (this effect is probably due to partial saturation of the liver enzyme systems and/or a transient increase in blood circulation in the liver after a single dose of verapamil).

Distribution

In CHD and arterial hypertension, no correlation was found between the therapeutic effect and the drug concentration in blood plasma; there is only a definite relationship between the drug level in blood plasma and the effect on the PR interval.

After taking a long-acting dosage form, the plasma concentration curve of verapamil stretches and becomes more flat than when administered with a normal release dosage form.

Binding to plasma proteins is 90%.

Penetrates the placental barrier; concentrations detected in the umbilical vein blood plasma were 20-92% of maternal plasma concentrations.

It is excreted in breast milk, but when using therapeutic doses, its concentrations are so low that a clinical effect in newborns is unlikely.

Metabolism

Verapamil undergoes a “first pass” effect through the liver. It is almost completely metabolized. The main metabolite is norverapamil, which has pharmacological activity; other metabolites are mostly inactive.

The elimination

of T1 / 2 is from 3 to 7 hours after a single oral use of the drug. With repeated use, T1 / 2 of verapamil can increase almost 2 times compared to a single dose.

Verapamil and its metabolites are mainly excreted via the kidneys (3-4% unchanged). Within 24 hours,50% of the administered dose is eliminated, within 48 hours – 55-60%, within 5 days-70%. Up to 16% is excreted in the faeces.

Pharmacokinetics in special clinical cases

In patients with hepatic insufficiency, compared with those with normal liver function, the bioavailability of verapamil was much higher, and an elongation of T1 / 2 was observed.

Recent results indicate that there are no differences in the pharmacokinetics of verapamil in individuals with normal renal function and in patients with end-stage renal failure.

Indications

• arterial hypertension;
• chronic stable angina (tension angina);
• angina caused by vascular spasm (Prinzmetal angina, variant);
• paroxysmal supraventricular tachycardia;
• atrial fibrillation / flutter accompanied by tachyarrhythmia (except for WPW syndrome).

Use during pregnancy and lactation

There are insufficient data on the use of Isoptin® CP 240 in pregnant women. The drug Isoptin® CP 240 can only be used during pregnancy if the benefit to the mother outweighs the potential risk to the fetus/child. Verapamil and its metabolites are excreted in breast milk. Taking into account the possibility of serious side effects in infants, the drug Isoptin® CP 240 should only be used during breastfeeding if the benefit to the mother outweighs the potential risk to the child.

Contraindications

• hypersensitivity to the Active ingredient or auxiliary components of the drug;
• cardiogenic shock,
• atrioventricular block II and III degree (except in patients with a functioning pacemaker);
• the syndrome of weakness of the sinus node (except for patients with a functioning pacemaker);
• heart failure with reduced ejection fraction less than 35% and/or jamming pressure of the pulmonary artery of more than 20 mm Hg. article (with the exception of heart failure caused by supraventricular tachycardia treated with verapamil);
• atrial fibrillation/atrial flutter in the presence of accessory pathways (including in patients with the syndrome Wolff-Parkinson-white, the Lawn Ganong-Levin). These patients are at risk of developing ventricular tachyarrhythmia, including ventricular fibrillation when taking verapamil; use with ivabradine (see the section “Interaction with other drugs”);
• pregnancy;
• breastfeeding (efficacy and safety have not been established);
• children under 18 years of age (efficacy and safety have not been established).

Side effects

Dizziness, headache; bradycardia; “flushes” of blood to the skin of the face, marked decrease in blood pressure; constipation, nausea; peripheral edema.

Interaction

In vitro metabolic studies indicate that verapamil is metabolized by cytochrome P450 isoenzymes CYP3A4, CYP1A2, CYP2C8, CYP2C9, and CYP2C18. Verapamil is an inhibitor of the CYP3A4 isoenzyme and P-glycoprotein. Clinically significant interactions were observed when co-administered with inhibitors of the CYP3A4 isoenzyme, with an increase in the concentration of verapamil in the blood plasma, while inducers of the CYP3A4 isoenzyme reduced the concentration of verapamil in the blood plasma. Therefore, patients should be monitored for drug interactions. HIV medications: Some HIV medications, such as ritonavir, can inhibit the metabolism of verapamil, which leads to an increase in its concentration in blood plasma. Caution should be exercised or the dose of verapamil should be reduced. Antihypertensive agents, diuretics, vasodilators: increased antihypertensive effect

How to take, course of use and dosage

Isoptin CP 240 is taken orally, without chewing, during or after meals, with a small amount of liquid,240-360 mg (the dose is selected individually).

With long-term therapy, the daily dose of Isoptin SR 240 should not exceed 480 mg. Usually prescribed in the morning for 240 mg. If a slow decrease in blood pressure is desirable,120 mg is prescribed.

Overdose

Symptoms of poisoning as a result of an overdose of Isoptin CP 240 depend on the amount of the drug taken, the time of detoxification measures, and the age-dependent contractility of the myocardium. Fatal cases have been reported as a result of overdose.

Symptoms: drop in blood pressure (in some cases to levels that cannot be measured), shock, loss of consciousness, grade I or II AV block, often in the form of Wenckebach periods with or without a slipping rhythm, complete AV block with complete AV dissociation, slipping rhythm, cardiac arrest; sinus bradycardia, sinus node arrest.

In case of overdose of Isoptin CP 240, it should be borne in mind that the Active ingredient is released and absorbed from the intestine within 48 hours after ingestion of the drug. Depending on the time of taking the drug, individual conglomerates of swollen tablet residues, acting as active depots, will be located throughout the gastrointestinal tract.

Treatment: measures aimed at removing the drug are indicated (for example, induce vomiting, flush the stomach and intestines in combination with an endoscopic examination, prescribe laxatives, emetics). If there is no motility of the stomach and intestines (signs of peristalsis during auscultation), then it is advisable to conduct gastric lavage even 12 hours after taking the drug orally. Common emergency resuscitation measures include indoor heart massage, CPR, and electrical heart stimulation.

Effects associated with cardiac suppression, hypotension, and bradycardia should be excluded.

Calcium is a specific antidote: 10-30 ml of 10% calcium gluconate solution is administered as an intravenous infusion (2.25-4.5 mmol), if necessary, re-administered or as a slow drip infusion (5 mmol / h).

In the case of AV block II or III degree, sinus bradycardia, cardiac arrest, use of atropine, isoprenaline, orciprenaline, and cardiac stimulation is indicated.

In case of arterial hypotension, dopamine, dobutamine, norepinephrine (norepinephrine) are administered.

In case of persistent signs of myocardial insufficiency, dopamine and dobutamine are administered, and if necessary, additional calcium is administered.

Description

Light green oblong-shaped tablets, film-coated. Tablets on both sides have transverse risks. Two ” A ” signs are engraved on one side.

Special instructions

Acute myocardial infarction: Isoptin® CP 240 should be used with caution in patients with acute myocardial infarction complicated by bradycardia, a marked decrease in blood pressure, or left ventricular dysfunction.

Beta-blockers and antiarrhythmic drugs: mutual enhancement of the effect on the cardiovascular system (high-grade antrioventricular block, significant decrease in heart rate, exacerbation of heart failure and a pronounced decrease in blood pressure).

Asymptomatic bradycardia (36 beats / min) with atrial rhythm migration was observed in a patient taking timolol (beta-blocker) in the form of eye drops and verapamil orally at the same time.

Digoxin: in case of concomitant use of Isoptin® CP 240 with digoxin should reduce the dose of digoxin. Heart failure: in patients with mild to moderate heart failure and a left ventricular ejection fraction greater than 35%, it is necessary to achieve a stable condition before starting Isoptin®. CP 240 and conduct appropriate therapy in the future.

Neuromuscular transmission disorders: Isoptin® CP 240 should be used with extreme caution in patients with diseases affecting neuromuscular transmission (myasthenia gravis, Lambert-Eaton syndrome, Duchenne muscular dystrophy).

Impaired renal function: verapamil should be used with caution and under close supervision in patients with impaired renal function. Verapamil is not eliminated by hemodialysis.

Impaired liver function: it should be used with extreme caution in patients with severe hepatic impairment.

Form of production

Tablets

Storage conditions

At a temperature not exceeding 25 °C

Shelf life

1 year

Active ingredient

Verapamil

Conditions of release from pharmacies

By prescription

Dosage form

long-acting tablets