diltiazem | Diltiazem retard capsules prolong. d 180 mg 30 pcs.

Latin name

DILTIAZEM RETARD

Release form

Sustained-release gelatin capsules No. 2, pink with a purple tint, the contents of the capsules are granules of white or almost white.

Packing

30 pcs

Pharmacological action

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

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

Antianginal effect due to the expansion of peripheral blood vessels and the reduction in systemic blood pressure (afterload), which leads to a decrease in the tension of the myocardial wall and its oxygen demand. In 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.

Antihypertensive effect due to dilatation of resistive vessels and a decrease in OPSS. The degree of decrease in blood pressure (BP) correlates with its baseline (in patients with normal blood pressure there is a minimal effect on blood pressure). Lowers blood pressure both in the "lying" and "standing" position. Rarely causes postural arterial hyiotension 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 renin-angiotensin-aldosterone system (RAAS). Reduces renal and peripheral effects of angiotensin II. It improves diastolic relaxation of the myocardium with arterial hypertension, coronary heart disease, hypertrophic cardiomyopathy, and reduces platelet aggregation.

It has minimal effect on the smooth muscles of the gastrointestinal tract (GIT). For prolonged (8 months) therapy, tolerance does not develop. Does not affect the lipid profile of the blood.

Able to cause regression of left ventricular hypertrophy in patients with arterial hypertension. The onset of action by ingestion is 2-3 hours. The duration of action is 12-24 hours.

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

Indications

prevention of paroxysmal supraventricular tachycardia

arterial hypertension

prevention of angina attacks (including Prinzmetal angina).

Contraindications

cardiogenic shock,

sinoatrial and AV block II and III degree (except for patients with a pacemaker)

Wolf-Parkinson-White syndrome

Laun-Ganong-Levin syndrome in combination with flutter or atrial fibrillation (except for patients with a pacemaker) srdlp decompensation stage)

acute heart failure

myocardial infarction with signs of left ventricular failure

sinus node weakness syndrome without the use of an artificial pacemaker

severe arterial r Potenza (systolic blood pressure less than 90 mmHg )

severe bradycardia

ventricular tachycardia with a wide complex of QRS

porphyria

pregnancy

lactation period

age up to 18 years (efficacy and safety not established)

intolerance to fructose and glucose / galactose malabsorption syndrome or and other benzothiazepine derivatives.

Caution: use in patients with severe hepatic and renal impairment, severe stenosis of the aortic orifice, in the acute phase of myocardial infarction (without signs of left ventricular failure), hypertrophic obstructive cardiomyopathy (GOKMP), arterial hypotension, grade I AV block or prolonged interval PQ, with simultaneous use with beta-blockers or digoxin, compensated chronic heart failure, with a tendency to bradycardia, in old age.

Composition

1 caps.

diltiazem 180 mg

Excipients: sugar grains (sucrose, starch syrup), a copolymer of methyl methacrylate, trimethylammonioethyl methacrylate and ethyl acrylate (1: 2: 0.1) a copolymer of methyl methacrylate, trimethylammonioethyl methacrylate parachloride: 0.2, and 1.

Capsule shell composition: titanium dioxide, sunset yellow dye, crimson dye (Ponceau 4R), patented blue dye, diamond black dye, gelatin.

Dosage and administration

Tablets should be taken orally, before meals, whole, without chewing or crushing, with a small amount of liquid.

The initial dose of Diltiazem Retard is 1 tablet of 90 mg 2 times a day. The average daily dose is 180-240 mg. Correction of the dosage regimen can be carried out only after 2 weeks.

The maximum dose is 360 mg / day (used only in a hospital).

Side effects of

From the cardiovascular system: angina pectoris, arrhythmia, bradycardia (less than 50 beats / min) or tachycardia, AV block, blockade of the bundle branch block, development or worsening of heart failure, changes in ECG, blood flow, marked decrease in blood pressure, palpitations, fainting, ventricular extrasystole.

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

From the digestive system: dry oral mucosa, anorexia, constipation or diarrhea, taste disturbance, dyspepsia, moderate increase in alkaline phosphatase (ALP) activity, aspartate aminotransferase (ACT), alanine aminotransferase (ALT), lactate dehydrogenase (LDH) weight gain.

From the skin: petechiae, photosensitization, skin itching, urticaria.

Other: amblyopia, increased activity of creatine phosphokinase (CPK), shortness of breath, nosebleeds, eye irritation, hyperglycemia, hyperuricemia, impotence, muscle cramps, nasal congestion, nocturia, bone-joint pain, polyuria, sexual dysfunction, tinnitus.

Post-marketing experience: allergic reactions, alopecia, angioedema (including facial edema and periorbital edema), erythema multiforme (including Stevens-Johnson syndrome), toxic eidermal necrolysis, extrapyramidal syndrome, gum hyperplasia, hemolytic anemia, prolonged bleeding time, leukopenia, purpura, retinopathy, myopathy, myopathy exfoliative dermatitis. There have been cases of generalized rash, which in some cases was a manifestation of leukocytoclastic vasculitis, cases of myocardial infarction, which is not always easy to distinguish from manifestations of an existing disease, have been reported.

Drug Interactions

Pharmacodynamic

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

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

With concomitant use with antiarrhythmic drugs, beta-blockers, cardiac glycosides, bradycardia, impaired atrioventricular conduction, and the appearance of symptoms of heart failure are possible.

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

Salicylates further inhibit platelet aggregation ability.

Ethanol: increased hypotensive effect.

procainamide, quinidine and other drugs, causing prolongation of the QT interval, increase the risk of its significant lengthening.

Inhalation anesthetics (hydrocarbon derivatives), thiazide diuretics, and other blood pressure lowering drugs enhance the hypotensive effect of diltiazem.

Phenytoin reduces the effect of diltiazem.

Antipsychotics (antipsychotics) enhance the hypotensive effect. Possible simultaneous administration of nitrates (including prolonged forms). Lithium preparations can enhance the neurotoxic effect of diltiazem (nausea, vomiting, diarrhea, ataxia, trembling and / or tinnitus).

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

Pharmacokinetic

Concomitant use 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 the blood plasma (40-70%) and increases the risk of adverse reactions, including ataxia, nystagmus, diplopia, headache, vomiting, confusion, and also increases the concentration of cyclosporine, digoxin (up to 50%), imipramine, lithium and midazolam.

Enhanced 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, intoxication and paresthesia may develop. Therefore, it is necessary to control plasma concentrations of cyclosporine in this group of patients. Eating increases the absorption and bioavailability of diltiazem to 20-30%. May increase the bioavailability of propranolol. Increases the concentration of morazizin in blood plasma.

Phenobarbital, diazepam, rifampicin reduce the concentration of diltiazem in blood plasma. Increases the concentration in the blood of quinidine, valproic acid (dose reduction may be required).

Antiviral agents: ritonavir may increase plasma concentrations of BMCC.

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

BMKK: excretion of nifedipine is reduced by diltiazem (increased plasma concentration).

Diltiazem significantly increases the concentration of lovastatin in blood plasma. It also enhances the effect of simvastatin, so when they are used simultaneously, the dose of simvastatin must be reduced. With the simultaneous use of diltiazem with lovastatin and simvastatin, patient monitoring is necessary, due to the possibility of developing myositis or rhabdomyolysis.

Overdose

Symptoms: severe bradycardia, marked decrease in blood pressure, leading to collapse, impaired atrioventricular and sinoatrial conduction, confusion, stupor, nausea, vomiting, metabolic acidosis, hyperglycemia, heart failure, cardiac insufficiency, cardiac insufficiency, cardiac insufficiency, cardiac failure.

Treatment: depending on the severity of an overdose. It is necessary to rinse the stomach, take activated charcoal, symptomatic further treatment. If necessary, it is recommended to prescribe atropine, isoprenaline, dopamine or dobutamine, and also, with severe conduction disturbances, the use of pacemaking is possible.

Hemodialysis and peritoneal dialysis are ineffective.

Storage Conditions

In a dry, dark place at a temperature not exceeding 25 РC.

Pharmacy leave conditions

Prescription

Form of Treatment

kapsul prolongirovannogo action

K.O.Romfarm Company SRL, Romania