Universal reference book for medicines

Active substance: diltiazem

Type: Calcium channel blocker

Manufacturer: SC ROMPHARM Company (Romania)
Composition, form of production and packaging
Capsules of prolonged action
hard gelatinous, в„–4, yellow;
the contents of the capsules are granules of white or almost white color.
1 caps.

diltiazem 90 mg

Auxiliary substances: sugar grits (sucrose, molasses starch), copolymer of methyl methacrylate, trimethylammonioethyl methacrylate and ethyl acrylate (1: 2: 0.1) copolymer of methyl methacrylate, trimethylammonioethyl methacrylate chloride and ethyl acrylate (1: 2: 0.2), paraffin, talc.

The composition of the capsule shell: titanium dioxide, dye quinoline yellow, dye sunset yellow, gelatin.

7 pcs.
- packings cellular planimetric (3) - packs cardboard.
Capsules of prolonged action hard gelatinous, в„–2, pink color with a violet shade;
the contents of the capsules are granules of white or almost white color.
1 caps.

diltiazem 180 mg

Auxiliary substances: sugar grits (sucrose, molasses starch), copolymer of methyl methacrylate, trimethylammonioethyl methacrylate and ethyl acrylate (1: 2: 0.1) copolymer of methyl methacrylate, trimethylammonioethyl methacrylate chloride and ethyl acrylate (1: 2: 0.2), paraffin, talc.

The composition of the capsule shell: titanium dioxide, dye sunset yellow, dye crimson (Ponso 4R), dye blue patented, dye diamond black, gelatin.

10 pieces.
- packings cellular planimetric (3) - packs cardboard.

Description of the drug approved by the manufacturer for the printed edition of 2011.


Diltiazem is a derivative of benzothiazepines;
has antiarrhythmic, antianginal and hypotensive activity. The "slow" calcium channel blocker reduces the intracellular calcium content in cardiomyocytes and smooth muscle cells, expands coronary and peripheral arteries and arterioles, reduces the overall peripheral vascular resistance (OPSS), smooth muscle tone, strengthens coronary, cerebral and renal blood flow, decreases the heart rate (heart rate).
The antiarrhythmic effect is caused by the suppression of the ionized calcium transport in the heart tissues, which leads to an increase in the effective refractory period and an extension of the time spent in the atrioventicular (AV) node (has clinical significance in patients with sinus node weakness syndrome, elderly patients in whom calcium channel blockade may prevent generation of a pulse in the sinus node and cause a sinoatrial (SA) blockage.The normal atrial action potential or intraventricular
(the normal sinus rhythm is usually not affected), but with a decrease in the amplitude of atrial contraction, the rate of depolarization and the rate of conduction decrease. The 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.
Antihypertensive effect is due to dilatation of resistive vessels and a decrease in OPSS.
The degree of reduction in blood pressure (BP) correlates with its baseline (in patients with normal blood pressure, a minimal effect on blood pressure is noted). Reduces blood pressure in both the "lying" and "standing" positions. Rarely causes postural arterial hyiotension and refractory tachycardia. Does not change or slightly reduces the maximum heart rate under the load. Long-term therapy does not lead to hyperkatecholamineemia, increased activity of the renin-angiotensin-aldosterone system (RAAS). Reduces the renal and peripheral effects of angiotensin II. 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 onset of action with oral administration is 2-3 hours. The duration of action is 12-24 hours.
The maximum severity of the hypotensive effect is achieved within 2 weeks.


When ingested quickly and almost completely absorbed in the gastrointestinal tract (90%).
Time to reach the maximum concentration in blood plasma - 6-14 hours. The values ​​of plasma concentrations in individual patients are very different. Communication with plasma proteins is 70-80% (with albumins - 35-40%). The volume of distribution of diltiazem 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 the "first passage" mainly through the liver.In the liver, it is metabolized by deacetylation and demethylation (with the participation of CYPZA4, CYP3A5 and CYP3A7 isoenzymes) to form an active metabolite of deacetyl-dithiasem, which is 5-10 times less in plasma than the original diltiazem and has a 2-4-fold lower activity.

T 1/2 for oral administration is biphasic: early - 20-30 minutes, final - 3.5 hours (5-8 hours - with high and repeated doses).

It is excreted through the intestines with bile (65%) and kidneys (35%, including 2-4% unchanged).

The pharmacokinetics of diltiazem for prolonged use does not change.
Diltiazem 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 T 1/2 is lengthened. In the elderly, the diltiazem clearance can also be reduced. It is not excreted in hemodialysis and peritoneal dialysis.

- prevention of paroxysmal supraventricular tachycardia;

- arterial hypertension;

- prevention of attacks of angina pectoris (including stenocardia of Prinzmetal).


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

The initial dose of the drug Diltiazem retard is 1 tablet of 90 mg 2 times a day.
The average daily dose is 180-240 mg. Correction of the dosing regimen can be carried out only after 2 weeks.
The maximum dose is 360 mg / day (used only in the hospital).


The most frequently observed (in many cases, the connection with the drug is not established): peripheral edema (2.4%), headache (2.1%), nausea (1.9%), dizziness (1.5%), skin rash (1.3%), asthenia ( 1.2%).

With a frequency of less than 1%:

From the cardiovascular system : angina, arrhythmia, bradycardia (less than 50 beats per minute) or tachycardia, AV blockade, blockage of the bundle of the bundle, development or worsening of heart failure, changes in the ECG, blood tides, marked decrease in blood pressure , palpitation, fainting, ventricular extrasystole.

From the nervous system: sleep disturbance, amnesia, depression, gait disturbance, hallucinations, insomnia, nervousness, paresthesia, personality changes, drowsiness, tremor.

On the part of the digestive system: dryness of the oral mucosa, anorexia, constipation or diarrhea, a taste disorder, dyspepsia, a moderate increase in the activity of alkaline phosphatase (ACP), aspartate aminotransferase (ACT), alanine aminotransferase (ALT), lactate dehydrogenase (LDH);
thirst, vomiting, weight gain.
From the skin: petechiae, photosensitization, itching, hives.

Other: amblyopia, increased activity of creatine phosphokinase (CK), dyspnea, epistaxis, eye irritation, hyperglycemia, hyperuricemia, impotence, muscle cramps, nasal congestion, nocturia, osteoarticular pain, polyuria, sexual dysfunction, ringing in the ears.

Postmarketing experience: allergic reactions, alopecia, angioedema, including edema of the face and periorbital edema, erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis, extrapyramidal syndrome, gingival hyperplasia, hemolytic anemia, lengthening bleeding time, leukopenia, purpura, retinopathy, myopathy, thrombocytopenia, exfoliative dermatitis.
There were cases of generalized rash, which in some cases was a manifestation of leukocytoclastic vasculitis; reported cases of myocardial infarction, which is not always easy to distinguish from the manifestations of the existing disease.

- cardiogenic shock,

- sinoatrial and AV-blockade of II and III degree (except for 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;

- syndrome of weakness of the sinus node without the use of an artificial pacemaker;

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

- pronounced bradycardia;

- Ventricular tachycardia with a wide complex of QRS;

- porphyria;

- Pregnancy;

- lactation period;

- age under 18 years (effectiveness and safety not established);

- fructose intolerance and glucose / galactose absorption disorder or sugarase / isomaltase deficiency;

- Hypersensitivity to the drug and to other benzothiazepine derivatives.

With caution: use in patients with severe impairment of liver and kidney function, severe stenosis of the aortic orifice, in the acute phase of myocardial infarction (without signs of left ventricular failure), hypertrophic obstructive cardiomyopathy (GOCMP), arterial hypotension, AV blockade of degree I, or PQ interval prolongation , with simultaneous use with beta-blockers or digoxin, compensated chronic heart failure, with a tendency to bradycardia, in the elderly.


Diltiazem retard is contraindicated for use during pregnancy and during lactation (diltiazem penetrates into breast milk).

Women in childbearing age before the appointment of Diltiazem retard should be excluded from pregnancy.


Use with caution in patients with severe renal dysfunction.


Diltiazem retard with caution appoint to patients with hepatic insufficiency;
In this group of patients, if necessary, the prescribed doses of the drug should be reduced.In patients with impaired liver function, the daily dose should not exceed 90 mg and it is recommended to regularly monitor liver function.

Contraindicated in children under 18 years.


Use with caution in old age.

For elderly patients, the dose is selected individually.


Diltiazem retard reduces conduction of the myocardium, so it should be used with extreme caution in patients with grade I AV blockade and bradycardia.
Caution is also needed when used in patients with left ventricular dysfunction.
Diltiazem retard with caution appoint patients already taking other medications, in particular, beta-blockers.
In this group of patients, the treatment process should be carried out under the close supervision of a cardiologist.
Diltiazem retard with caution prescribed to patients with renal or hepatic insufficiency;
In this group of patients, if necessary, reduce the prescribed doses of the drug and control the concentration of urea 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.

Since diltiazem reduces OPSS 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 persistent skin rash, which develop into multiforme erythema and exfoliative dermatitis, diltiazem retard should be stopped.

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 (the patient takes Diltiazem retard).

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

Impact on the ability to drive vehicles and manage machinery

To date, it has not been established that the administration of 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.

Symptoms: pronounced bradycardia, marked decrease in blood pressure, which leads to collapse, violation of atrioventricular and sinoatrial conductance, 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, take activated charcoal, further treatment is symptomatic. If necessary, it is recommended to appoint atropine, isoprenaline, dopamine or dobutamine, and, in case of severe conduction disorders, it is possible to use electrocardiostimulation.
Hemodialysis and peritoneal dialysis are ineffective.



With the simultaneous use of diltiazem with antihypertensive drugs, there is an increase in hypotensive effect.

With the simultaneous administration of diltiazem and digoxin, an increase in the concentration of digoxin in the blood is possible.

With simultaneous reception with antiarrhythmic drugs, beta-adrenoblockers, cardiac glycosides, bradycardia, violation of atrioventricular conduction, the appearance of symptoms of heart failure may develop.

With simultaneous use with adenosine, the risk of developing a prolonged bradycardia is increased.

Salicylates additionally inhibit the ability to aggregate platelets.

Ethanol: increased hypotensive effect.

Procainamide, quinidine and other drugs that cause prolongation of the QT interval increase the risk of its significant lengthening.

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

Phenytoin reduces the effect of diltiazem.

Antipsychotic drugs (antipsychotics) increase the hypotensive effect.
The simultaneous administration of nitrates (including prolonged forms) is possible. Lithium preparations can enhance the neurotoxic effect 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.


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 the concentration of theophylline and carbamazepine in blood plasma (40-70%) and increases the risk of adverse reactions, including.
ataxia, nystagmus, diplopia, headache, vomiting, confusion, and increases the concentrations of cyclosporine, digoxin (up to 50%), imipramine, lithium and midazolam.
Enhance the effect of hypoglycemic agents for oral administration (eg, chlorpropamide and glipizide).

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 monitor plasma concentrations of cyclosporine in this group of patients. Food intake increases the absorption and bioavailability of diltiazem up to 20-30%. May increase the bioavailability of propranolol. Increases the concentration of moracisin in the blood plasma.
Phenobarbital, diazepam, rifampicin reduce the concentration of diltiazem in the blood plasma.
Increases the concentration in the blood of quinidine, valproic acid (a dose reduction may be required).
Antiviral agents: ritonavir can increase plasma concentrations of BCCC.

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, monitoring of patients is necessary, because of the possibility of developing myositis or rhabdomyolysis.

On prescription.


In a dry, the dark place at a temperature of no higher than 25 В° C.
Keep out of the reach of children. Shelf life - 3 years.
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