Diltiazem pills 90 mg 30 pcs
Condition: New product
1000 Items
Rating:
Be the first to write a review!
More info
Active ingredients
Diltiazem
Release form
Pills
Composition
1 caps diltiazem 90 mg. Auxiliary substances: sugar krupka (sucrose, starch syrup), copolymer of methyl methacrylate, trimethylammonioethyl methacrylate and ethyl acrylate (1: 2: 0.
Pharmacological effect
Diltiazem is a benzothiazepine derivative; possesses antiarrhythmic, antianginal and hypotensive activity. The "slow" calcium channel blocker (BMCC), reduces intracellular calcium in cardiomycetes and smooth muscle cells, dilates coronary and peripheral arteries and arterioles, reduces total peripheral vascular resistance (OPS), smooth muscle tone, strengthens coronary, cerebral and renal blood flow lowers heart rate (HR). The antiarrhythmic effect is due to the suppression of ionized calcium transport in the heart tissues, 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 sick sinus syndrome, elderly patients who have calcium channel blockade prevent impulse generation in the sinus node and cause a sinoatrial (SA) blockade. Normal atrial action potential or intraventricular held They do not change (normal sinus rhythm usually does not affect), but if the atrial contraction decreases, the depolarization rate and conduction rate decrease. The anterograde effective refractory period in additional bypass conduction bundles may be shortened. afterload), which leads to a decrease in the tension 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 the resistive vessels and the decrease in round fist. The degree of blood pressure reduction (BP) correlates with its baseline (in patients with normal blood pressure, there is a minimal effect on blood pressure).Reduces blood pressure in the "lying" and "standing". Rarely causes postural arterial hypotension and refractory 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 the renal and peripheral effects of angiotensin II. It improves diastolic relaxation of myocardium in case of arterial hypertension, coronary heart disease, hypertrophic cardiomyopathy, reduces platelet aggregation. It has a minimal effect on the smooth muscles of the gastrointestinal tract (GIT). For a long time (8 months) of 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 for ingestion is 2-3 hours. Duration of action is 12-24 hours. The maximum severity of the hypotensive effect is achieved within 2 weeks.
Pharmacokinetics
When ingestion is quickly and almost completely absorbed in the gastrointestinal tract (90%). The time to reach the maximum concentration in the blood plasma is 6-14 hours. The concentration values in the blood plasma of individual patients are very different. Communication with plasma proteins is 70-80% (with albumin - 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 is extensively metabolized, due to the effect of "first pass" mainly through the liver. In the liver, it is metabolized by deacetylation and demethylation (with the participation of CYPZA4, CYP3A5 and CYP3A7 isoenzymes) with the formation of the active metabolite deacetyldylthiazem, which is determined in plasma in 5-10 times lower concentration than the original diltiazem, and has 2-4 times less activity. T1 / 2 when taken orally is biphasic: early - 20-30 minutes, final - 3.5 hours (5-8 hours - at high and repeated doses). Excreted through the intestines with bile (65%) and kidneys (35%, including 2-4% unchanged). The pharmacokinetics of diltiazem with prolonged use does not change. Diltiazem does not accumulate and does not induce its own metabolism. In patients with angina and impaired renal function, the pharmacokinetics of diltiazem do not change. In patients with liver failure, bioavailability increases and T1 / 2 is lengthened. In old age, the clearance of diltiazem can also be reduced.It is not displayed during hemodialysis and peritoneal dialysis.
Indications
- prevention of paroxysmal supraventricular tachycardia - arterial hypertension - prevention of attacks of angina pectoris (including Prinzmetal angina pectoris).
Contraindications
- cardiogenic shock, - sinoatrial and AV block II and III degrees (except for patients with a pacemaker) - Wolff-Parkinson-White syndrome - Launa-Gannga-Levine syndrome in combination with atrial flutter or atrial fibrillation (except for patients with a pacemaker) - chronic heart failure (at the stage of decompensation) - acute heart failure - myocardial infarction with signs of left ventricular failure - sick sinus syndrome without the use of an artificial pacemaker - marked artery Hypotension (systolic blood pressure less than 90 mm Hg) - severe bradycardia - ventricular tachycardia with a wide range of QRS - porphyria - pregnancy - lactation period - age up to 18 years (efficacy and safety have not been established) - intolerance to fructose and glucose absorption disorder / galactose or sucrase / isomaltase deficiency - hypersensitivity to the drug and to other benzothiazepine derivatives. With caution: use in patients with severe impaired liver and kidney function, severe stenosis of the aortic mouth, in the acute phase of myocardial infarction (without signs of left ventricular failure), hypertrophic obstructive cardiomyopathy (GOKMP), arterial hypotension, AV block I degree or prolonged PQ interval , with simultaneous use with beta-blockers or digoxin, compensated for chronic heart failure, with a tendency to bradycardia, in old age.
Use during pregnancy and lactation
Diltiazem retard is contraindicated for use during pregnancy and during lactation (diltiazem penetrates into breast milk). Women at child-bearing age before the appointment of Diltiazem retard should be excluded pregnancy.
Dosage and administration
Tablets should be taken orally, before meals, entirely, without chewing and crushing, washing down with a small amount of liquid. The initial dose of Diltiazem retard is 1 tablet, 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).
Side effects
The most frequently observed (in many cases, the connection with the intake of the drug is not installed): 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%: On the part of the cardiovascular system: angina, arrhythmia, bradycardia (less than 50 beats / min) or tachycardia, AV-blockade, blockade of the bundle of His, development or worsening of heart failure, changes in the ECG, "flushes "blood, marked decrease in blood pressure, palpitations, fainting, ventricular extrasystole. Nervous system disorders: 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, taste disturbance, dyspepsia, moderate increase in alkaline phosphatase (alkaline phosphatase) activity, aspartate aminotransferase (ACT), alanine aminotransferase (ALT), lactate dehydrogenase (LDH); thirst, vomiting, weight gain. On the part of the skin: petechiae, photosensitivity, pruritus, urticaria. Others: amblyopia, increased activity of creatine phosphokinase (CPK), shortness of breath, nose bleeding, eye irritation, hyperglycemia, hyperuricemia, impotence, muscle cramps, nasal congestion, nocturia, bone and joint pain, polyuria, sexual dysfunction, tinnitus. Posmarketingovy experience: allergic reactions, alopecia, angioneurotic edema (including edema of the face and periorbital edema), erythema multiforme (including Stevens-Johnson syndrome), toxic eiidermalny necrolysis, extrapyramidal syndrome, gingival hyperplasia, hemolytic anemia, prolonged bleeding time, leukopenia, purpura, retinopathy, myopathy, thrombocytopenia, exfoliative dermatitis. Cases of a generalized rash were observed, 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.
Overdose
Symptoms: severe bradycardia, marked reduction in blood pressure, turning into collapse, violation of atrioventricular and sinoatrial conduction, confusion, stupor, nausea, vomiting, metabolic acidosis, hyperglycemia, heart failure, cardiogenic shock, asystole. Treatment: depending on the severity of manifestations of overdose. It is necessary to wash the stomach, take activated charcoal, further symptomatic treatment. If necessary, it is recommended to prescribe atropine, isoprenaline, dopamine or dobutamine, as well as, in case of marked conduction disturbances, the use of pacing is possible. Hemodialysis and peritoneal dialysis are ineffective.
Interaction with other drugs
Pharmacodynamic With simultaneous use of diltiazem with antihypertensives, an increase in the hypotensive effect is noted. At the same time taking diltiazem and digoxin, it is possible to increase the concentration of digoxin in the blood. When taken concomitantly with antiarrhythmic agents, beta-blockers, cardiac glycosides, bradycardia may develop, impaired atrioventricular conduction, and symptoms of heart failure appear. With simultaneous use with adenosine increased risk of prolonged bradycardia. Salicylates further inhibit the ability of platelet aggregation. Ethanol: increased hypotensive effect. Procainamide, quinidine, and other drugs that prolong the QT interval increase the risk of significant prolongation. Means for inhalation anesthesia (derivatives of hydrocarbons), thiazide diuretics, and other means of reducing blood pressure increase the hypotensive effect of diltiazem. Phenytoin reduces the effect of diltiazem. Antipsychotics (neuroleptics) enhance the hypotensive effect. Perhaps the simultaneous appointment of nitrates (including prolonged forms). Lithium preparations may enhance the neurotoxic effect of diltiazem (nausea, vomiting, diarrhea, ataxia, tremors, and / or tinnitus). Indomethacin and other nonsteroidal anti-inflammatory drugs (NSAIDs), glucorticosteroids and estrogens, as well as symptomatic drugs reduce the hypotensive effect.Pharmacokinetic Simultaneous 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. Strengthening the action of hypoglycemic agents for oral administration (for example, chlorpropamid and glipizida). With simultaneous use of diltiazem and cyclosporine in patients with a transplanted kidney, the development of intoxication and paresthesia are possible. Therefore, it is necessary to control plasma concentrations of cyclosporin in this group of patients. Meal increases absorption and bioavailability of a diltiazem to 20-30%. May increase the bioavailability of propranolol. Increases the concentration of moracizin in the blood plasma. Phenobarbital, diazepam, rifampicin reduce the concentration of diltiazem in the blood plasma. Increases the concentration of quinidine in the blood, valproic acid (may require a dose reduction). Antiviral agents: ritonavir may increase plasma concentrations of BCCA. Anxiolytics and hypnotics: diltiazem inhibits midazolam metabolism (increased plasma concentration with increased sedative effect). BMCC: elimination of nifedipine is reduced by diltiazem (increased plasma concentration). Diltiazem significantly increases the concentration of lovastatin in the blood plasma. Also enhances the effect of simvastatin, therefore, with their simultaneous use of a dose of simvastatin must be reduced. With simultaneous use of diltiazem with lovastatin and simvastatin, patient monitoring is necessary because of the possibility of developing myositis or rhabdomyolysis.
special instructions
Diltiazem retard reduces myocardial conductivity, so it should be used with extreme caution in patients with AV block I degree and bradycardia. Caution is also needed when used in patients with impaired left ventricular function. Diltiazem retard is prescribed with caution to patients already taking other drugs, in particular, beta-blockers. In this group of patients, the treatment process should be carried out under the careful supervision of a cardiologist.Diltiazem retard is prescribed with caution in patients with renal or hepatic insufficiency; in this group of patients, if necessary, reduce the prescribed dose of the drug and monitor the concentration of urea in 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 adjusted individually. Since diltiazem reduces OPSD and may cause secondary arterial hypotension, it is necessary to monitor blood pressure, in particular, at the beginning of a course of treatment, while therapeutic doses have not yet been clarified. In the case of persistent skin rash that develops into erythema multiforme and exfoliative dermatitis, the use of Diltiazem retard should be stopped. If, during therapy, the patient needs to undergo a general anesthetic surgery, it is necessary to inform the anesthesiologist about the nature of the therapy (the patient takes Diltiazem retard). Elderly patients may increase the half-life of diltiazem. Effect on the ability to drive vehicles and control mechanisms It has not yet been established that the use of diltiazem in recommended doses has an impact on the psychomotor activity of the patient. In patients with hypersensitivity, it can (in particular at the beginning of a 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, quick mental and motor responses.