Diltiazem Lannacher p / o prolonged-release tablets 180mg, No. 30

• arterial hypertension;

• prevention of angina attacks (including Prinzmetal's angina);

• prevention of attacks of supraventricular arrhythmias (paroxysmal tachycardia, atrial fibrillation or flutter, extrasystole).

The drug is taken orally, before meals, without chewing and drinking a small amount of liquid.

The dosage regimen is set individually.

The initial dose of Diltiazem Lannacher is 1 tab. (90 mg) 2 times / day. The average daily dose is 180-270 mg. The maximum daily dose is 360 mg.

The dosage regimen can be adjusted only after 2 weeks. With long-term treatment with a good therapeutic effect, a dose reduction is possible.

Active ingredient: diltiazem hydrochloride - 180 mg

Excipients: lactose monohydrate - 120 mg, copolymer of methyl methacrylate and ethyl acrylate [2: 1] - 9 mg, copolymer of methacrylic acid and ethyl acrylate [1: 1] - 79.5 mg, copolymer of methyl methacrylate, trimethylammonioethyl methacrylate chloride 1: 2: 0.1] [ - 15 mg, hypromellose 5 mPa * s - 15 mg, magnesium stearate - 1.5 mg.

Shell composition: macrogol 6000 - 2.996 mg, hypromellose 5 mPa * s - 2.5 mg, titanium dioxide - 1.356 mg, talc - 12.404 mg, copolymer of methyl methacrylate and ethyl acrylate [2: 1] - 0.744 mg.

• sinoatrial and AV-blockade of II and III degrees (except for patients with a pacemaker);

• severe bradycardia;

• sick sinus syndrome without the use of an artificial pacemaker;

• cardiogenic shock;

• Wolff-Parkinson-White syndrome;

• Laun-Ganong-Levin syndrome in combination with atrial flutter or fibrillation (except for patients with a pacemaker);

• severe arterial hypotension (systolic blood pressure less than 90 mm Hg);

• acute heart failure;

• chronic heart failure (in the stage of decompensation);

• myocardial infarction with signs of left ventricular failure;

• wide-complex ventricular tachycardia;

• pregnancy;

• lactation period;

• age up to 18 years (efficacy and safety have not been established);

• lactose intolerance, lactase deficiency and glucose-galactose malabsorption;

• hypersensitivity to the drug and to other benzothiazepine derivatives.

The drug should be used with caution in patients with severe hepatic and renal dysfunction, acute porphyria, severe aortic stenosis, in the acute phase of myocardial infarction (without signs of left ventricular failure), with hypertrophic obstructive cardiomyopathy, mild and moderate arterial hypotension, AV - I degree blockade or lengthening of the PQ interval, simultaneous use with beta-blockers or digoxin, compensated chronic heart failure, with a tendency to bradycardia, in old age.

Trade name of the drug:

Diltiazem Lannacher

International Non-Proprietary Name (INN):

diltiazem

Dosage form:

prolonged-release film-coated tablets.

Clinical and pharmacological group: Calcium channel blocker

Pharmaco-therapeutic group: Blocker of 'slow' calcium channels

pharmachologic effect

Diltiazem is a benzothiazepine derivative; possesses antiarrhythmic, antianginal and hypotensive activity. A blocker of slow calcium channels (BMCC), reduces the intracellular content of calcium ions in cardiomyocytes and smooth muscle cells, expands coronary and peripheral arteries and arterioles, reduces total peripheral vascular resistance (OPSS), smooth muscle tone, increases coronary, cerebral and renal blood flow, decreases heart rate (HR).

The antiarrhythmic effect is due to the suppression of the transport of ionized calcium in the tissues of the heart, which leads to an increase in the effective refractory period and lengthening of the conduction time in the atrioventricular (AV) node (it is of clinical importance in patients with sick sinus syndrome, elderly patients in whom calcium channel blockade can prevent the generation of an impulse in the sinus node and cause sinoatrial block). Normal atrial action potential or intraventricular conduction does not change (normal sinus rhythm is usually not affected), but when the amplitude of atrial contraction decreases, the rate of depolarization and conduction rate decrease. The anterograde effective refractory period in additional bypass conduction bundles can be shortened.

The antianginal effect is due to the expansion of peripheral vessels and a decrease in systemic blood pressure (afterload), which leads to a decrease in the stress of the myocardial wall and its oxygen demand. At concentrations that do not lead to the appearance of a negative inotropic effect, it causes relaxation of the smooth muscles of the coronary vessels and dilatation of both large and small arteries.

The antihypertensive effect is due to the dilatation of resistive vessels and a decrease in the systemic vascular resistance. The degree of decrease in blood pressure correlates with its initial level (in 'normotonics' there is a minimal effect on blood pressure). Reduces blood pressure both in the supine position and standing. Rarely causes postural arterial hypotension and reflex tachycardia. Does not change or slightly reduces the maximum heart rate during exercise. Long-term therapy does not lead to hypercatecholaminemia, an increase in the activity of the RAAS. Reduces the renal and peripheral effects of angiotensin II. Improves diastolic relaxation of the myocardium in arterial hypertension, coronary artery disease, hypertrophic obstructive cardiomyopathy, reduces platelet aggregation.

Has a minimal effect on the smooth muscles of the gastrointestinal tract. During long-term (8 months) therapy, tolerance does not develop. Does not affect blood lipid profile.

Able to cause regression of left ventricular hypertrophy in patients with arterial hypertension.

The onset of action when taken orally is 2-3 hours. The duration of action is -12-14 hours. The maximum severity of the hypotensive effect is achieved within 2 weeks.

Pharmacokinetics

Absorption and distribution

After oral administration, it is rapidly and almost completely absorbed from the gastrointestinal tract. Time to reach Cmax in blood plasma is 6-14 hours. Plasma protein binding is 70-80% (with albumin - 35-40%). Penetrates into breast milk.

Metabolism

It is extensively metabolized in the liver by deacetylation and demethylation (with the participation of isoenzymes CYP3A4, CYP3A5 and CYP3A7) with the formation of an active metabolite of deacetyldyltiazem, which is determined in plasma in 5-10 times lower concentration than diltiazem, and has 2-4 times less activity.

Withdrawal

T1 / 2 diltiazem when taken orally is biphasic: early - 20-30 minutes, final - 3.5 hours (5-8 hours - with high and repeated doses). T1 / 2 of the drug Diltiazem Lannacher in the dosage form of a tablet of prolonged action of 90 mg and 180 mg is up to 10 hours.It is excreted through the intestines with bile (65%) and kidneys (35%, including 2-4% unchanged) ...

The pharmacokinetics of diltiazem does not change with prolonged use. The drug does not cumulate and does not induce its own metabolism.

Pharmacokinetics in special clinical situations

In patients with angina pectoris and impaired renal function, the pharmacokinetics of diltiazem does not change. Not excreted during hemodialysis and peritoneal dialysis.

In patients with hepatic insufficiency, bioavailability increases and T1 / 2 is lengthened.

In old age, clearance of diltiazem may also be reduced.

Indications

• arterial hypertension;

• prevention of angina attacks (including Prinzmetal's angina);

• prevention of attacks of supraventricular arrhythmias (paroxysmal tachycardia, atrial fibrillation or flutter, extrasystole).

Dosage regimen

The drug is taken orally, before meals, without chewing and drinking a small amount of liquid.

The dosage regimen is set individually.

The initial dose of Diltiazem Lannacher is 1 tab. (90 mg) 2 times / day. The average daily dose is 180-270 mg. The maximum daily dose is 360 mg.

The dosage regimen can be adjusted only after 2 weeks. With long-term treatment with a good therapeutic effect, a dose reduction is possible.

Side effect

From the side of the cardiovascular system: bradycardia, ventricular premature beats, chronic heart failure, sinoauricular blockade, AV blockade up to asystole, marked decrease in blood pressure, fainting, skin redness, angina pectoris, arrhythmia (including flutter and fibrillation of the ventricles), tachycardia, shortness of breath, peripheral edema. When used in high doses - angina pectoris, bradycardia, AV blockade.

From the digestive system: dry mouth, increased appetite, vomiting, nausea, heartburn, diarrhea, hypertrophic gingivitis, constipation, hypercreatininemia, abdominal pain, abnormal liver function, intestinal obstruction.

From the nervous system: headache, general weakness, asthenia, fatigue, anxiety, dizziness, drowsiness, insomnia, depression, a state of pathological fear, extrapyramidal disorders, parkinsonism (ataxia, mask-like face, shuffling gait, stiffness of the arms or legs, trembling hands and fingers, difficulty swallowing). When used in high doses - paresthesia.

From the side of the organ of vision: visual impairment (transient blindness).

Allergic reactions: increased photosensitivity, itching, skin rash, flushing of the facial skin, Stevens-Johnson syndrome, erythema multiforme, exfoliative dermatitis.

Other: taking the drug can lead to an increase in the concentration of liver enzymes in the blood serum, peripheral edema.

When used in high doses - pulmonary edema (difficulty breathing, cough, stridor breathing), thrombocytopenia, agranulocytosis, galactorrhea, weight gain.

With a sharp withdrawal of the drug , withdrawal syndrome may develop with concomitant tachycardia, arterial hypertension and worsening of the course of angina pectoris.

Contraindications for use

• sinoatrial and AV-blockade of II and III degrees (except for patients with a pacemaker);

• severe bradycardia;

• sick sinus syndrome without the use of an artificial pacemaker;

• cardiogenic shock;

• Wolff-Parkinson-White syndrome;

• Laun-Ganong-Levin syndrome in combination with atrial flutter or fibrillation (except for patients with a pacemaker);

• severe arterial hypotension (systolic blood pressure less than 90 mm Hg);

• acute heart failure;

• chronic heart failure (in the stage of decompensation);

• myocardial infarction with signs of left ventricular failure;

• wide-complex ventricular tachycardia;

• pregnancy;

• lactation period;

• age up to 18 years (efficacy and safety have not been established);

• lactose intolerance, lactase deficiency and glucose-galactose malabsorption;

• hypersensitivity to the drug and to other benzothiazepine derivatives.

The drug should be used with caution in patients with severe hepatic and renal dysfunction, acute porphyria, severe aortic stenosis, in the acute phase of myocardial infarction (without signs of left ventricular failure), with hypertrophic obstructive cardiomyopathy, mild and moderate arterial hypotension, AV - I degree blockade or lengthening of the PQ interval, simultaneous use with beta-blockers or digoxin, compensated chronic heart failure, with a tendency to bradycardia, in old age.

Application during pregnancy and lactation

Diltiazem Lannacher is contraindicated during pregnancy and lactation.

For women of childbearing age, pregnancy should be excluded before diltiazem is prescribed.

Application for violations of liver function

The drug should be used with caution in patients with severe liver dysfunction.

Application for impaired renal function

The drug should be used with caution in patients with severe renal impairment.

Application in children

The use of the drug under the age of 18 is contraindicated (efficacy and safety have not been established).

Use in elderly patients

The drug should be used with caution in old age.

special instructions

Diltiazem reduces myocardial conductivity, therefore, it is prescribed with extreme caution in patients with grade I AV block and bradycardia. Caution is also required when used in patients with impaired left ventricular function of the heart.

Diltiazem is used with caution in patients already taking other drugs, in particular beta-blockers. In this group of patients, the treatment process should be carried out under the close supervision of a cardiologist.

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

For elderly patients, the dose is selected individually, because T1 / 2 of diltiazem may increase.

Because diltiazem reduces OPSS and can cause secondary arterial hypotension, it is necessary to control blood pressure, in particular, at the beginning of the course of treatment, while the therapeutic doses have not yet been clarified.

In case of persistent skin rashes developing into erythema multiforme and exfoliative dermatitis, Diltiazem Lannacher should be discontinued.

If during therapy the patient needs to undergo surgery under general anesthesia, it is necessary to inform the anesthesiologist about the nature of the therapy (the patient is taking Diltiazem Lannacher).

While taking the drug Diltiazem Lannacher, the use of alcoholic beverages is not recommended.

Influence on the ability to drive vehicles and use mechanisms

The use of the drug Diltiazem Lannacher can adversely affect the performance of work that requires a high speed of mental and physical reactions (for example, driving vehicles, mechanisms, working at height).

Overdose

Symptoms: bradycardia, marked decrease in blood pressure, turning into collapse, violation of atrioventricular and sinoatrial conduction, heart failure, cardiogenic shock, asystole, nausea, vomiting, metabolic acidosis, hyperkalemia.

Ћечение: в зависимости от т¤жести про¤влений передозировки. Ќеобходимо промыть желудок, назначить активированный уголь, дальнейшее лечение симптоматическое. ѕри необходимости рекомендуетс¤ назначить атропин, изопреналин, допамин или добутамин, а также, при выраженных нарушени¤х проводимости, возможно применение электрокардиостимул¤ции. vемодиализ и перитонеальный диализ не эффективны.

Ћекарственное взаимодействие

‘армакодинамическое взаимодействие

ѕри одновременном приеме дилтиазема с гипотензивными средствами отмечаетс¤ усиление антигипертензивного действи¤.

ѕри одновременном приеме дилтиазема и дигоксина возможно повышение концентрации дигоксина в крови.

ѕри одновременном приеме дилтиазема с антиаритмическими средствами, бета-адреноблокаторами, сердечными гликозидами возможно развитие брадикардии, нарушение AV-проводимости, по¤вление симптомов сердечной недостаточности.

ѕри одновременном применении с аденозином повышен риск развити¤ пролонгированной брадикардии.

—алицилаты дополнительно угнетают способность к агрегации тромбоцитов.

Ётанол усиливает антигипертензивный эффект.

ѕрокаинамид, хинидин и другие лекарственные средства, вызывающие удлинение интервала QT, повышают риск его значительного удлинени¤.

—редства дл¤ ингал¤ционной анестезии (производные углеводородов), тиазидные диуретики и другие лекарственные средства, снижающие ј?, усиливают гипотензивный эффект дилтиазема.

‘енитоин снижает эффект дилтиазема.

јнтипсихотические средства (нейролептики) усиливают антигипертензивный эффект дилтиазема.

¬озможно одновременное назначение нитратов (в т.ч. пролонгированных форм).

ѕрепараты лити¤ могут усиливать нейротоксическое действие дилтиазема (тошнота, рвота, диаре¤, атакси¤, дрожание и/или шум в ушах).

»ндометацин и другие Ќѕ¬ѕ, v — и эстрогены, а также симпатические лекарственные средства снижают гипотензивный эффект.

”силивает кардиодепрессивное действие общих анестетиков.

‘армакокинетическое взаимодействие

?иметидин ослабл¤ет процесс биотрансформации дилтиазема в печени, замедл¤ет его выведение, увеличива¤ продолжительность действи¤ дилтиазема.

?илтиазем увеличивает концентрацию теофиллина и карбамазепина в плазме крови (40-70%) и повышает риск возникновени¤ побочных реакций, в т.ч. атаксии, нистагма, диплопии, головной боли, рвоты, спутанности сознани¤, а также увеличивает концентрации циклоспорина, дигоксина (до 50%), имипрамина, лити¤ и мидазолама.

”силивает действие гипогликемических средств дл¤ приема внутрь (например, хлорпропамида и глипизида).

ѕри одновременном применении дилтиазема и циклоспорина у больных с пересаженной почкой, возможно развитие интоксикации последним, парестезии. ѕоэтому необходимо внимательно следить за уровнем плазменных концентраций циклоспорина у данной группы пациентов.

ѕрием пищи увеличивает всасывание и биодоступность дилтиазема на 20-30%.

ћожет повышать биодоступность пропранолола.

ѕовышает концентрацию морацизина в плазме крови.

‘енобарбитал, диазепам, рифампицин снижают концентрацию дилтиазема в плазме крови.

ѕовышает концентрацию в крови хинидина, вальпроевой кислоты (может потребоватьс¤ снижение дозы).

–итонавир может повышать плазменные концентрации Ѕћ  .

?илтиазем угнетает метаболизм мидазолама (повышаетс¤ плазменна¤ концентраци¤ с усилением седативного действи¤).

¬ыведение нифедипина снижаетс¤ дилтиаземом (повышаетс¤ плазменна¤ концентраци¤).

?илтиазем значительно увеличивает концентрацию ловастатина в плазме крови. “акже усиливает действие симвастатина, поэтому при их одновременном применении дозы симвастатина необходимо снизить. ѕри одновременном применении дилтиазема с ловастатином и симвастатином необходим контроль за пациентами из-за возможности развити¤ миозита или рабдомиолиза.

”слови¤ хранени¤

The drug should be stored out of the reach of children at a temperature not exceeding 30 ? C.

Shelf life

Shelf life is 3 years. Do not use after the expiration date.

Terms of sale

The drug is available with a prescription.

Contacts for inquiries

BAUSH HEALTH LLC (Russia)