Diltiazem lannaher prolong tab. n / 180 mg film about 30 pc

Description

Composition
Active substance:
1 tablet contains: diltiazem hydrochloride, 90 mg, 180 mg ;.
Excipients:
Lactose monohydrate 60.0 / 120.0 mg methyl methacrylate-ethyl acrylate copolymer, [2: 1] 4.5 / 9.0 mg of methacrylic acid ethyl acrylate copolymer (1: 1) 57.75 / 79.5 mg, methylmethacrylate, trimetilammonioetilmetakrilata chloride and ethyl acrylate copolymer [1: 2: 0.1] 7.5 / 15.0 mg hypromellose 5 mPa * s 9,5 / 15,0 mg magnesium stearate 0.75 / 1.5 mg; sheath: Macrogol 6000 2.247 / 2.996 mg Hypromellose 5 mPa * s 1,875 / 2,500 mg titanium dioxide 1.017 / 1.356 mg talc 9.303 / 12.404 mg methyl methacrylate-ethyl acrylate copolymer, [2: 1] 0.558 / 0.744 mg.
Description:
Round biconvex tablets, film-coated white color, cross-sectional kernel white tablets.
Product form:
Prolonged action tablets, film-coated 90 and 180 mg.
10 tablets in PVC / Al blister.
2 blisters (tablet 90 mg) and 3 blisters (180 mg tablet), together with instructions for use in a cardboard box.
Contraindications
Increased sensitivity to the drug and other derivatives benzothiazepine sinoatrialnaya and atrioventricular block II and III degree (except for patients with a pacemaker), bradycardia, sinus syndrome without pacemaker, cardiogenic shock, Wolff-Parkinson-White syndrome Lown-Ganong-Levine in conjunction with atrial flutter or atrial fibrillation (except for patients with a pacemaker), marked hypotension (systolic blood pressure less than 90 mm Hg. v.), st Paradise heart failure, chronic heart failure (decompensation), myocardial infarction with signs of left ventricular failure, ventricular tachycardia with a wide QRS complex, pregnancy, lactation, age under 18 years (effectiveness and safety have not been established), lactose intolerance, lactase deficiency and glucose-galactose malabsorption.
Caution should be used in patients with severe liver and kidney disease, acute porphyria, severe aortic stenosis, in the acute phase of myocardial infarction (without signs of left ventricular failure), hypertrophic obstructive cardiomyopathy, mild to moderate arterial hypotension, atrioventricular block I degree or lengthening the interval PQ, while the use of beta-blockers or digoxin, compensated chronic heart failure, with a tendency to bradika di-, in old age.
Dosage
180 mg
Indications
Arterial hypertension
Prevention of angina attacks (including Prinzmetal angina)
Prevention of seizures supraventricular arrhythmias (paroxysmal tachycardia, atrial flutter or flicker, arrythmia).
Interaction with other drugs
pharmacodynamic
When concomitantly with antihypertensive drugs diltiazem there is a growing anti-hypertensive action.
At the same time taking digoxin and diltiazem may increase blood concentrations of digoxin.
When concomitantly with diltiazem, antiarrhythmics, beta-blockers, cardiac glycosides may develop bradycardia, a violation of atrioventricular conduction, the emergence of symptoms of heart failure.
While the use of adenosine, an increased risk of prolonged bradycardia.
Salicylates further ability to inhibit platelet aggregation.
Ethanol: increased antihypertensive effect.
Procainamide, quinidine and other drugs causing prolongation of the interval QT, increase the risk of a significant lengthening.
Means for inhalation anesthesia (hydrocarbon derivatives), thiazide diuretics, and other drugs which reduce blood pressure, increase the hypotensive effects of diltiazem.
Phenytoin reduces the effect of diltiazem.
Antipsihooticheskie agents (neuroleptics) increase the antihypertensive effect of diltiazem.
The simultaneous appointment of nitrates (including long-acting forms).
Formulations may enhance lithium neurotoxic action of diltiazem (nausea, vomiting, diarrhea, ataxia, tremor, and / or tinnitus).
Indomethacin and other nonsteroidal anti-inflammatory drugs, glucocorticoids and estrogens, and sympathetic drugs reduce the hypotensive effect.
Enhances cardiodepressive action of general anesthetics.
pharmacokinetic
Cimetidine process weakens diltiazem biotransformation in the liver, excretion it slows, increasing the duration of action of diltiazem.
Diltiazem increases the concentration of theophylline and karmazepina blood plasma (40-70%) and increases the risk of adverse reactions, including ataxia, nystagmus, diplopia, headaches, vomiting, confusion, and also increases the concentration of cyclosporine, digoxin (50%), imipramine, lithium, and midazolam.
It enhances the action of hypoglycemic agents for oral administration (e.g., chlorpropamide and glipizide).
With simultaneous use of diltiazem and cyclosporine in patients with kidney transplant, may develop intoxication last paresthesia. Therefore it is necessary to closely monitor the level of plasma concentration of cyclosporine in this group of patients. Eating increases the absorption and bioavailability of diltiazem by 20-30%.
May increase the bioavailability of propranolol. Moratsizina increases the concentration in blood plasma.
Phenobarbital, diazepam, rifampicin reduce the concentration of diltiazem in the blood plasma.
Increasing the concentration of quinidine in the blood, valproic acid (may require dose reduction).
Antiviral agents: ritonavir may increase plasma concentrations of BCCI.
Anxiolytics and hypnotics: diltiazem inhibits midazolam metabolism (increased plasma concentration with increased sedation.
BCCI: elimination of nifedipine diltiazem reduced (increased plasma concentration).
Diltiazem significantly increases the concentration of lovastatin in the blood plasma. Also enhances the effect of simvastatin, so their simultaneous use of simvastatin dose should be reduced. With simultaneous use of diltiazem, lovastatin and simvastatin necessary to monitor patients, due to the potential development of myositis and rhabdomyolysis.
Overdose
Symptoms: bradycardia, marked reduction of blood pressure, turning into a collapse, impaired atrioventricular and sinoatrial conduction, heart failure, cardiogenic shock, asystole, nausea, vomiting, metabolic acidosis, hyperkalemia.
Treatment: depending on the severity of the manifestations of overdose. It is necessary to wash out the stomach, activated charcoal to appoint further treatment is symptomatic. If necessary, it is recommended to assign atropine, isoprenaline, dopamine or dobutamine, and, when expressed conduction disturbances may use pacing.
Hemodialysis and peritoneal dialysis are not effective.
pharmachologic effect
Pharmacological group:
Blocker “slow” calcium channels.
Pharmacodynamics:
Diltiazem is a benzothiazepine derivative; It possesses antiarrhythmic, antianginal and antihypertensive activity. Blocker “slow” calcium channel (BCCI), reduces the intracellular concentration of calcium ions in cardiomyocytes and smooth muscle cells, dilates coronary and peripheral arteries and arterioles, decreases total peripheral vascular resistance (TPR), smooth muscle tone, strengthens the coronary, cerebral and renal blood flow , slows the heart rate (HR).
Antiarrhythmic effect due to inhibition of transport of ionized calcium in the cardiac tissue, that causes an increase in the effective refractory period and lengthening the time of the in atrioventricular (AV) node (having clinical significance for patients with sick sinus syndrome, elderly patients whose calcium channel blockade may prevent the generation of momentum in the sinus node and cause sinoatrialnuyu (SA) blockade). Normal atrial action potential or intraventricular conduction are not changed (to a normal sinus rhythm is usually not affected), but with a decrease in the amplitude of atrial contraction depolarization rate and the rate of decrease. Anterograde effective refractory period for additional bypass of 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 reduction of myocardial wall stress and its oxygen requirements. At concentrations that do not lead to the emergence of a negative inotropic effect, causing relaxation of smooth muscle and dilation of the coronary vessels, both large and small arteries.
The antihypertensive action is due to dilatation of resistance vessels and decreased peripheral vascular resistance. The degree of lowering blood pressure (BP) is correlated with its initial level (at “normotensive” there is minimal effect on BP). Lowers blood pressure in the position of “lying” and “standing”. Rarely causes postural hypotension and reflex tachycardia. It does not change or slightly reduces the maximum heart rate during exercise. Prolonged therapy does not lead to hypercatecholaminemia, increased activity of the renin-angiotensin-aldosterone system. Decreases renal and peripheral effects of angiotensin II. Improves diastolic myocardial relaxation in arterial hypertension, ischemic heart disease, hypertrophic obstructive cardiomyopathy, reduces platelet aggregation.
It has a minimal effect on the smooth muscles of the gastrointestinal tract (GIT). During the long-term (8 months.) Therapy did not develop tolerance. No effect on blood lipid profile.
Able to induce regression of left ventricular hypertrophy in hypertensive patients. The onset of action when taken orally -. 2-3 hour duration of action is – 12-14 hours.
Maximum severity of the hypotensive effect is achieved within 2 weeks.
Pharmacokinetics:
Once inside quickly and almost completely absorbed from the gastrointestinal tract. The time to reach maximum plasma concentration -. 6-14 hours Connection to plasma proteins is 70-80% (albumin – 35-40%). Is extensively metabolized in the liver by demethylation and deacetylation (involving isozymes CYP3A4, CYP3A5 and CYP3A7) to form the active metabolite dezatsetildiltiazema which is determined in plasma by 5-10 times lower concentration than diltiazem and has 2-4 times less activity. It passes into breast milk.
Diltiazem half-period ingestion is biphasic: early – 20-30 min, final – 3.5 hours (5-8 hours – and repeated at high doses). The half-life of the drug Diltiazem Lannaher in a dosage form with prolonged action tablets 90 mg and 180 mg up to 10 hours. The deduced through the intestine in bile (65%) and kidneys (35%, including 2.4% unchanged).
The pharmacokinetics of diltiazem with prolonged use is not changed.
The drug does not accumulates and does not induce its own metabolism. In patients with angina and impaired renal function The pharmacokinetics of diltiazem is not changed. In patients with hepatic insufficiency increases the bioavailability and half-life is prolonged. In old age may be reduced clearance of diltiazem. It does not appear in hemodialysis and peritoneal dialysis.
Pregnancy and breast-feeding
During pregnancy and lactation Lannaher Diltiazem is contraindicated.
Women of childbearing age before the appointment of diltiazem should exclude pregnancy.
Conditions of supply of pharmacies
On prescription.
side effects
With the cardiovascular system: bradycardia, ventricular arrythmia, congestive heart failure, sinus block, atrioventricular block up to asystole, marked reduction in blood pressure, fainting, flushing, angina, arrhythmia (including atrial and ventricular fibrillation), tachycardia, shortness of breath , peripheral edema.
From the digestive system: dry mouth, increased appetite, vomiting, nausea, heartburn, diarrhea, hypertrophic gingivitis, constipation, hypercreatininemia, abdominal pain, abnormal liver function, ileus.
Central nervous system: headache, fatigue, asthenia, fatigue, anxiety, dizziness, somnolence, insomnia, depression, pathological fear ekstrapirapidnye disorders, Parkinson’s disease (ataxia, “mask-like” face, “shuffling” gait, stiff arms or legs, trembling hands and fingers, difficulty in swallowing).
When used in high doses – paresthesia.
From the senses: visual disturbances (transient blindness).
Allergic reactions: increased sensitivity, itching, skin rash, redness of the skin, Stevens-Johnson syndrome, erythema multiforme, exfoliative dermatitis.
Miscellaneous: the drug can lead to increased concentrations of “liver” enzymes in serum, peripheral edema.
When used in high doses – pulmonary edema (difficulty breathing, cough, stridor), anemia, agranulocytosis, galactorrhea, increased body mass.
With a sharp lifting of the drug may develop a syndrome of “cancellation” with accompanying tachycardia, hypertension and worsening of angina.
special instructions
Diltiazem reduces conductivity infarction, so its prescribed with caution in patients with AV blockade degree I and bradycardia. Caution is needed, and when used in patients with impaired left ventricular function.
Diltiazem administered with caution in patients already receiving other drugs, such as beta-blockers. In these patients the treatment process should be carried out under the close supervision of a cardiologist.
Diltiazem administered with caution to patients with renal or hepatic insufficiency; in this group of patients should be reduced, if necessary assignable dosage and monitor the urea concentration in urine creatinine. In patients with impaired liver function, the daily dose should not exceed 90 mg is recommended to conduct regular monitoring of liver function.
For elderly patients the dose is adjusted individually, as may increase the half-life of diltiazem.
Since diltiazem reduces round and can cause secondary hypotension is necessary to control blood pressure, particularly in the early course of treatment, while therapeutic doses have not yet clarified.
In case of persistent skin rashes developing into erythema multiforme and exfoliative dermatitis – receiving Diltiazem drug Lannaher should be discontinued.
If during therapy the patient needed surgery under general anesthesia, it is necessary to inform the anesthesiologist about the nature of the therapy (the patient is taking diltiazem Lannaher).
The effect on the ability of control of vehicles and mechanisms
Use of the drug Diltiazem Lannaher can adversely affect the performance of work, requiring a high rate of mental and physical reactions (e.g., management of vehicles, machinery, working at height and the like). During the administration of the drug Diltiazem Lannaher not recommended for drinking.
Storage conditions
Store at a temperature not higher than 30 C.
Keep out of the reach of children.
Dosing and Administration
The tablets should be taken orally before meals, with liquid squeezed small amount of liquid. The mode set individually.
Starting Diltiazem Lannaher dose is 1 tablet of 90 mg 2 times a day. The average daily dose is 180-270 mg. Correction dosing regimen can be carried out only after 2 weeks. The maximum daily dose is 360 mg. Long-term treatment with a good therapeutic effect may reduce the dose.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist