Diltiazem-Teva - instructions for use, dose, side effects, contraindications

Active substanceDiltiazemDiltiazem

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Dosage form: & nbspfilm coated tablets

Composition:

Each tablet contains:

Active ingredient: Diltiazema hydrochloride - 30 mg or 60 mg.

Excipients: lactose, polyvinyl acetate, magnesium stearate, macrogol 4000, macrogol 6000, giprolose, talc.

Description:

Tablets 30 mg. Tablets biconvex, covered with a film shell, white with engraving "ABIC" on one side.

Tablets 60 mg. Tablets biconvex, covered with a film shell, white with engraving "ABIC" on one side and with a risk on the other side.

Pharmacotherapeutic group:The blocker of "slow" calcium channels

ATX: & nbsp

C.08.D.B.01 Diltiazem

C.05.A.E.03 Diltiazem

Pharmacodynamics:

Diltiazem is a derivative of benzodiazepines; has antiarrhythmic, antianginal and hypotensive activity.The "slow" calcium channel blocker reduces the intracellular content of calcium ions in cardiomyocytes and smooth muscle cells, expands coronary and peripheral arteries and arterioles, reduces overall peripheral vascular resistance (OPSS), smooth muscle tone, strengthens coronary, cerebral and renal blood flow , reduces the heart rate (heart rate).

The antiarrhythmic effect is due to the suppression of the transport of ionized calcium in the heart tissues, which leads to an increase in the effective refractory period, and an extension of the time spent in the atrioventricular (AV) node (has clinical significance in patients with sinus node weakness syndrome, elderly patients in whom blockade of calcium channels can interfere with the generation of a pulse in the sinus node and cause a sinoatrial (SA) blockade. The normal atrial action potential or intraventricular conduction does not change (normal sinus rhythm is usually unaffected), but with a decrease in the amplitude of atrial contraction, the rate of depolarization and speed of conduction decrease.Anterograde effective refractory period in additional bypass beams of conduction may be shortened.

Antianginal action is due to the expansion of peripheral vessels and a decrease in systemic arterial pressure (afterload), which leads to a decrease in the stress of the wall of the myocardium and its need for oxygen. In concentrations that do not lead to the appearance of a negative inotropic effect, it causes the relaxation of the smooth muscles of the coronary vessels and the dilatation of both large and small arteries.

Hypotensive effect is caused by dilatation of resistive vessels and a decrease in OPSS. The degree of decrease in blood pressure (BP) correlates with its baseline level (in patients with normal blood pressure there is minimal effect on BP). Reduces blood pressure in both lying and standing. Rarely causes postural arterial hypotension and refractory tachycardia. Does not change or slightly reduces the maximum heart rate under the load. Long-term therapy does not lead to hyperkatecholamineemia, an increase in the activity of the renin-angiotensin-aldosterone system. Reduces renal and peripheral effects of angiotensin I.Improves diastolic relaxation of the myocardium with arterial hypertension, coronary heart disease, hypertrophic cardiomyopathy, reduces platelet aggregation. Has a minimal effect on the smooth muscles of the gastrointestinal tract (GIT). During a long (8 months) therapy, tolerance does not develop. Does not affect the lipid profile of the blood.

It is able to cause regression of left ventricular hypertrophy in patients with arterial hypertension.

The maximum severity of the hypotensive effect is achieved within 2 weeks.

Pharmacokinetics:

When ingested quickly and almost completely absorbed in the gastrointestinal tract (GIT). The maximum concentration in the blood plasma is reached after 4-6 hours after administration. Values of plasma concentrations in individual patients are very different. Communication with plasma proteins is 70-80%. The volume of distribution of the drug in the body is about 5.3 l / kg body weight.

After absorption from the gastrointestinal tract, the active substance undergoes intensive metabolism, due to the effect of "first passage" mainly through the liver. In the liver, it is metabolized with the formation of several intermediate metabolic products, most of which are excreted from the body by bile (65%), and to a lesser extent by kidneys (35%).The half-life is 4-10 hours.

The pharmacokinetics of diltiazem for prolonged use does not change.

The drug does not cumulate or induce its own metabolism.

In patients with angina and impaired renal function, the pharmacokinetics of diltiazem does not change. In patients with hepatic insufficiency, bioavailability increases and the half-life is prolonged. In the elderly, the diltiazem clearance can also be reduced. It is not excreted in hemodialysis and peritoneal dialysis.

Indications:

1 Prevention of angina attacks (including Prinzmetal angina pectoris);

2 arterial hypertension

3 prevention of attacks of supraventricular arrhythmias (paroxysmal tachycardia, flicker or atrial flutter, extrasystole).

Contraindications:

Hypersensitivity to the drug and to other benzodiazepine derivatives, cardiogenic shock, sinoauric blockade, sinoatrial and atrioventricular blockade of II and III degree (with the exception of patients with a pacemaker), Wolff-Parkinson-White syndrome, Laun-Ganong-Levin syndrome in combination with flutter or atrial fibrillation (except for patients with a pacemaker),chronic heart failure (in the stage of decompensation), acute heart failure, myocardial infarction with signs of left ventricular failure, sinus node weakness syndrome without the use of an artificial pacemaker, pronounced arterial hypotension (systolic blood pressure less than 90 mm Hg), pronounced bradycardia, ventricular tachycardia with a wide complex QRS, pregnancy, lactation, age under 18 years (efficacy and safety not established).

Carefully:

Carefully apply in patients with severe impairment of liver and kidney function, acute porphyria, severe stenosis of the aortic aorta, mild to moderate degree of arterial hypotension, atrioventricular blockade of degree I, or lengthening of the interval PQ, when concomitant administration with beta-blockers or digoxin, chronic heart failure, a tendency to bradycardia, in the elderly.

Pregnancy and lactation:

Diltiazem is contraindicated for use during pregnancy and during breast-feeding.

Women in child-bearing age before the appointment of diltiazem should be excluded from pregnancy.

Dosing and Administration:

Tablets should be taken orally, before meals, whole, not liquid and not crumbling, with a small amount of liquid.

The dosage regimen is set individually, depending on the severity of the disease and the patient's condition.

The initial dose is 30 mg.

Treatment begins with 60-120 mg 2 times a day or 180-240 mg once a day, followed by correction of the dosing regimen after 2 weeks.

The maximum dose is 360 mg / day.

In elderly patients, as well as for violations of the liver and / or kidney function, treatment starts with lower doses, with taking 1 tablet (30 mg) once a day.

Side effects:

From the cardiovascular system: bradycardia, ventricular extrasystole, chronic heart failure, sinoauric blockade, atrioventricular blockade up to asystole, marked decrease in blood pressure, fainting, redness of the skin, rarely angina, arrhythmia (including flutter and fibrillation of the ventricles), tachycardia, dyspnea, peripheral edema. When used in high doses - angina, bradycardia, atrioventricular block.

From the digestive tract: dry mouth, increased appetite, vomiting,nausea, heartburn, diarrhea, hypertrophic gingivitis, constipation, hypercreatininaemia, abdominal pain, impaired liver function, intestinal obstruction.

From the central nervous system and sense organ: headache, general weakness, asthenia, fatigue, anxiety, dizziness, drowsiness, insomnia, depression, a condition of pathological fear, extrapyramidal disorders, parkinsonism (ataxia, "masky" face, shuffling gait, stiffness of hands or feet, trembling of hands and fingers, difficulty swallowing).

When used in high doses - paresthesia, visual impairment (transient blindness).

Allergic reactions: increased photosensitivity, itching, skin rash, hyperemia of the skin of the face, Stevens-Johnson syndrome. Very rarely - polymorphic erythema, exfoliative dermatitis.

Other: Very rarely, taking the drug leads to an increase in concentrations "hepatic" enzymes in the serum, peripheral edema.

When used in high doses of pulmonary edema (difficulty breathing, coughing, stridoroznoe respiration); rarely - thrombocytopenia, agranulocytosis, galactorrhea, weight gain.

With a sharp withdrawal of the drug can develop a syndrome of "withdrawal" with concomitant tachycardia, hypertension and worsening of the course of angina.

Overdose:

Symptoms: bradycardia, pronounced decrease in blood pressure, passing into collapse, violation of atrioventricular conduction, confusion, stupor, nausea, vomiting, metabolic acidosis, hyperglycemia, heart failure, cardiogenic shock, asystole.

Treatment: depending on the severity of the overdose. It is necessary to wash the stomach, appoint Activated carbon, further treatment is symptomatic. If necessary, it is recommended that atropine, isoproterenol, dopamine or dobutamine, and also, with pronounced conduction disorders, the use of electrocardiostimulation is possible.

Hemodialysis and peritoneal dialysis are not effective.

Interaction:

Pharmacodynamic

Simultaneous use of diltiazem with antihypertensive drugs increased hypotensive effect.

With the simultaneous administration of diltiazem and digoxin it is possible to increase the concentration of digoxin in the blood.

With simultaneous reception with antiarrhythmic drugs, beta-adrenoblockers, cardiac glycosides, bradycardia, violation of atrioventricular conduction, the appearance of symptoms of heart failure may develop. When used simultaneously with adenosine, increased risk of prolonged bradycardia.

Salicylates additionally inhibited the ability to aggregate platelets.

Ethanol: increased hypotensive effect.

Pharmacokinetic

Simultaneous application with cimetidine leads to a significant increase in plasma concentrations of diltiazem, which in turn can lead to its toxic effect on the cardiovascular system.

Diltiazem increases concentration theophylline and carbamazepine in blood plasma (40- TO%) and increases the risk of adverse reactions, incl. ataxia, nystagmus, diplopia, headache, vomiting, confusion, and also increases concentration cyclosporine, digoxin (up to 50%), imipramine, lithium and midazolam. The effect of oral hypoglycemic agents (eg, clorprapamid and glipizide) is increasing.

With the simultaneous use of diltiazem and cyclosporine in patients with a transplanted kidney, it is possible to develop intoxication, paresthesia. Therefore, it is necessary to closely monitor the plasma concentrations of cyclosporine in this group of patients. Food intake increases the absorption and bioavailability of diltiazem up to 20-30%. Procainamide, quinidine and other drugs that cause lengthening of the interval QT, increase the risk of significant lengthening.

May increase bioavailability propranolol.

Increases the content moracisin in the blood plasma.

Means for inhalation anesthesia (derivatives of hydrocarbons), thiazide diuretics and other drugs that reduce blood pressure, enhance the hypotensive effect of diltiazem.

Phenobarbital, diazepam, rifampicin reduce the concentration of diltiazem.

Phenytoin reduces the effect of diltiazem.

Increases concentration in the blood quinidine, valproic acid (a dose reduction may be required).

Antipsychotic drugs (antipsychotics) increase the hypotensive effect. Antiviral drugs: ritonavir can increase plasma concentrations of BCC.

Anxiolytics and hypnotics: diltiazem inhibits the metabolism of midazolam (increased plasma concentration with increased sedation).

BCCI: elimination of nifedipine is reduced by diltiazem (plasma concentration is increased).

Diltiazem significantly increases the concentration of lovastatin in blood plasma. It also increases the action of simvastatin, so when using them simultaneously, simvastatin should be lowered. With the simultaneous use of diltiazem with lovastatin and simvastatin, patients should be monitored, because of the possibility of myositis or rhabdomyolysis.

Possible simultaneous appointment nitrates (including prolonged forms). Strengthens the cardiodepressive action of drugs for general anesthesia.

Preparations lithium may potentiate neurotoxic effects of diltiazem (nausea, vomiting, diarrhea, ataxia, tremor, and / or tinnitus).

Indomethacin and other non-steroidal anti-inflammatory drugs (NSAIDs), glucocorticosteroids and estrogens, as well as symptomatic drugs reduce the hypotensive effect.

Special instructions:

Diltiazem reduces the conductance of the myocardium, so it is with particular caution prescribed to patients with AV blockade of the I degree and bradycardia. Caution is also needed when appointing patients with a violation of the function of the left ventricle of the heart.

Diltiazem with caution appoint patients already taking other medications, in particular, blockers of β-adrenergic receptors for oral administration. In this group of patients, the treatment process should be performed under the close supervision of the cardiologist.

Diltiazem with caution appoint to patients with renal or hepatic insufficiency; in this group of patients, if necessary, reduce the prescribed doses of the drug and monitor the urea content in the urine, creatinine. In patients with impaired liver function, the daily dose should not exceed 90 mg and it is recommended to regularly monitor liver function.

For elderly patients, the dose is selected individually.

As diltiazem reduces OSSS and can cause secondary arterial hypotension, it is necessary to monitor blood pressure, in particular, at the beginning of the course treatment, while therapeutic doses are not yet specified.

In case of occurrence of persistent skin rashes accruing to polymorphic erythema and exfoliative dermatitis, the drug should be discontinued.

If during the therapy the patient is required to undergo surgery under general anesthesia, it is necessary to inform the anesthetist about the nature of the therapy.

In elderly patients, the half-life of diltiazem may increase.

Effect on the ability to drive transp. cf. and fur:

Until now, it has not been established that taking diltiazem in recommended doses affects the psychomotor activity of the patient. In patients with hypersensitivity, it can (in particular at the beginning of the course of treatment) cause an excessive decrease in blood pressure, dizziness and a transient decrease in the ability to drive vehicles and engage in other potentially dangerous activities requiring increased attention, rapid mental and motor reaction.

Form release / dosage:

Film coated tablets 30 mg, 60 mg.

Packaging:

For 10 tablets in a blister of a combined material (PVC / aluminum foil).

3 blisters together with instructions for use in a cardboard bundle.

Storage conditions:

Store in a dry place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

Film coated tablets 30 mg - 4 years.

The tablets covered with a film cover of 60 mg - 3 years.

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

Terms of leave from pharmacies:On prescription

Registration number:П N012863 / 01

Date of registration:05.05.2008

Expiration Date:Unlimited

The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel

Manufacturer: & nbsp

TEVA Pharmaceutical Industries, Ltd. Israel

Representation: & nbspTeva Teva Israel

Information update date: & nbsp20.03.2018

Illustrated instructions

Instructions

Diltiazem Teva (Diltiazem-Teva)