Description of the drug DILTIAZEM LANNACHER
When used simultaneously with beta-blockers (including propranolol, atenolol, metoprolol, pindolol, sotalol), an additive cardiodepressive effect is possible along with an increase in the antianginal effect in most patients. Patients with pre-existing left ventricular dysfunction or conduction disturbances are at increased risk of developing severe and life-threatening bradycardia.
Diltiazem inhibits the metabolism of propranolol, metoprolol, but not atenolol.
When used simultaneously with amiodarone, the negative inotropic effect, bradycardia, conduction disturbances, and AV block are enhanced.
Since diltiazem inhibits the CYP3A4 isoenzyme, which is involved in the metabolism of atorvastatin, lovastatin and simvastatin, drug interactions due to increased plasma concentrations of statins are theoretically possible. Cases of rhabdomyolysis have been described.
When used simultaneously with buspirone, the concentration of buspirone in the blood plasma increases, its therapeutic and side effects increase.
When used simultaneously with vecuronium chloride, the duration of neuromuscular blockade may be increased.
When used simultaneously with digoxin and digitoxin, it is possible to increase the concentrations of digoxin and digitoxin in the blood plasma.
When used simultaneously with imipramine, the concentration of imipramine in the blood plasma increases and there is a risk of developing undesirable changes on the ECG.
Cases of increased plasma concentrations of trimipramine and nortriptyline when used simultaneously with diltiazem have been described.
Diltiazem increases the bioavailability of imipramine by reducing its clearance. Changes in the ECG are due to an increase in the concentration of imipramine in the blood plasma and the additive inhibitory effect of diltiazem and imipramine on AV conduction. Diltiazem is believed to interact in the same way with trimipramine and nortriptyline.
When used simultaneously with insulin, a case of decreased insulin effectiveness has been described.
Due to the inhibition of the metabolism of anticonvulsants in the liver under the influence of diltiazem and a decrease in their clearance from the body, it is possible to increase the concentrations of carbamazepine and phenytoin in the blood plasma with the risk of developing toxic effects.
When used simultaneously with lithium carbonate, cases of the development of acute parkinsonism syndrome and psychosis have been described.
When used simultaneously with midazolam, triazolam, the concentration of midazolam and triazolam in the blood plasma increases and their effects are enhanced due to the inhibition of the CYP3A4 isoenzyme under the influence of diltiazem, with the participation of which the metabolism of these benzodiazepines is carried out.
When used simultaneously with sodium amidotrizoate, the antihypertensive effect of diltiazem may be enhanced.
When used simultaneously with sodium nitroprusside, a significant increase in effectiveness in controlled arterial hypotension is possible.
When used simultaneously with nifedipine, the antihypertensive effect is enhanced.
Rifampicin induces liver enzyme activity, accelerating the metabolism of diltiazem, which leads to a decrease in its effectiveness.
When used simultaneously with theophylline, a slight decrease in the metabolism of theophylline in the liver is possible, apparently due to inhibition of the CYP1A2 isoenzyme under the influence of diltiazem.
When used concomitantly with cisapride, a case of impaired consciousness has been described, apparently due to a pronounced prolongation of the QT interval. It is believed that diltiazem inhibits the activity of the CYP3A4 isoenzyme, which leads to increased plasma concentrations of cisapride and possibly increased cardiotoxicity.
With simultaneous use, diltiazem inhibits the metabolism of cyclosporine in the liver, which leads to a decrease in its elimination and an increase in plasma concentrations. At the same time, a decrease in the manifestations of nephrotoxicity and an increase in the immunosuppressive effect were noted.
When used simultaneously with cimetidine, the concentration of diltiazem in the blood plasma increases due to inhibition of its oxidative metabolism in the liver under the influence of cimetidine. The effects of diltiazem may be enhanced.
When used simultaneously with enflurane, cases of impaired AV conduction of the myocardium have been reported.
Diltiazem tablets - reviews
Alla Valentinovna
https://pharm-market.ru/catalog/diltiazem.aspx
Previously, my blood pressure often increased, and as a result, arrhythmia could begin. The condition was very bad then. But recently my GP prescribed me Diltiazem Regard. I use it according to the instructions, 2 tablets 3 times a day and am very pleased with its effect. My condition has stabilized, I feel much better now, calmer and my mood has improved.
Kaleria
https://pharm-market.ru/catalog/diltiazem.aspx
Oh, and for us, thank God, everything worked out somehow without any side effects. My husband developed a terrible arrhythmia and our doctor advised him to take diltiazem. My husband took it three times a day as directed. Now his condition has stabilized. We can conclude that the drug is very effective.
valentine
Mild dizziness sometimes occurs after taking diltiazem. But this drug works effectively. It lowers blood pressure gradually. This is precisely its advantage.
Alexandra Batistova
https://www.piluli.ru/product/Diltiazem/review
She took Diltiazem as part of a complex treatment for arrhythmia. I noticed that my blood pressure began to rise a little, I was tempted to take another drug, but the doctor said that this was a side effect. I had to cancel because with my diagnosis I can’t experience pressure surges. These pills are probably good for those who do not have problems with blood pressure.
Inessa
https://www.apreka.ru/?l=diltiazem_tabletki
I have been taking Diltiazem for about three months. At first I took 60 mg 3 times a day, but since I often forgot about taking it at lunch, I wasn’t happy with it. I switched to taking 90 mg morning and evening, it’s more convenient.
2 weeks after starting treatment, I began to notice a sharp decrease in blood pressure, the doctor advised me to reduce the dose to 60 mg 2 times a day. I stopped at this level. Since I inject insulin, the doctor warned that it might be necessary to reconsider the insulin dose, but everything turned out fine. Selecting the dose of the drug was somewhat delayed, almost a month, which brought its own concerns, but with previous medications it was even longer. I think it’s positive that when climbing stairs I don’t feel the same discomfort and shortness of breath.
What makes it a little uncomfortable is that you have to swallow the tablet whole; for me it’s like a test, but I’ve already gotten the hang of it.
The price of the drug is a little high, I thought about switching to substitutes, but my health has improved so much that I’ll probably stick with Diltiazem. The fact that there is no need to combine multiple medications is also in favor of Diltiazem. Of course, no matter how suitable the drug is, it is necessary to constantly monitor the pressure, although I increasingly listen to my perception of well-being and forget about this event.
Diltiazem Lannacher 90 mg 20 pcs. extended-release tablets
pharmachologic effect
Diltiazem is a benzothiazepine derivative;
has antiarrhythmic, antianginal and hypotensive activity. Slow calcium channel blocker (SCBC), reduces the intracellular content of calcium ions in cardiomyocytes and smooth muscle cells, dilates coronary and peripheral arteries and arterioles, reduces total peripheral vascular resistance (TPVR), smooth muscle tone, increases coronary, cerebral and renal blood flow, reduces 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 prolongation of conduction time in the atrioventricular (AV) node (of clinical significance in patients with sick sinus syndrome, elderly patients in whom blockade of calcium channels can prevent the generation of an impulse in the sinus node and cause sinoatrial block). The normal atrial action potential or intraventricular conduction is not affected (normal sinus rhythm is usually not affected), but as the amplitude of atrial contraction decreases, the rate of depolarization and conduction velocity decrease. The anterograde effective refractory period in additional bypass conduction bundles may 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 myocardial wall tension and its oxygen demand. In concentrations that do not lead to 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 dilatation of resistive vessels and a decrease in peripheral vascular resistance. The degree of reduction in blood pressure correlates with its initial level (in “normotensives” there is a minimal effect on blood pressure). Reduces blood pressure both in the supine and standing positions. Rarely causes postural hypotension and reflex tachycardia. Does not change or slightly reduces maximum heart rate during exercise. Long-term therapy does not lead to hypercatecholaminemia or increased RAAS activity. Reduces the renal and peripheral effects of angiotensin II. Improves diastolic relaxation of the myocardium in arterial hypertension, coronary heart disease, hypertrophic obstructive cardiomyopathy, reduces platelet aggregation.
Has minimal effect on the smooth muscles of the gastrointestinal tract. During long-term (8 months) therapy, tolerance does not develop. Does not affect the blood lipid profile.
Can 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.
Composition and release form Diltiazem Lannacher 90 mg 20 pcs. extended-release tablets
Tablets - 1 tablet:
- Active substance: diltiazem hydrochloride 90 mg.
- Excipients: lactose monohydrate - 120 mg, copolymer of methyl methacrylate and ethyl acrylate [2:1], copolymer of methacrylic acid and ethyl acrylate [1:1], copolymer of methyl methacrylate, trimethylammonioethyl methacrylate chloride and ethyl acrylate [1:2:0.1], hypromellose 5 mPa*s , magnesium stearate.
- Shell composition: macrogol 6000, hypromellose 5 mPa*s, titanium dioxide, talc, copolymer of methyl methacrylate and ethyl acrylate [2:1].
10 pieces. - blisters (2) - cardboard packs.
Description of the dosage form
Extended-release tablets, white film-coated, round, biconvex, with a white core in cross-section.
Directions for use and doses
The drug is taken orally, before meals, without chewing and with a small amount of liquid.
The dosage regimen is set individually.
The initial dose of Diltiazem Lannacher is 1 tablet. (90 mg) 2 times/day. The average daily dose is 180-270 mg. The maximum daily dose is 360 mg.
Correction of the dosage regimen can be carried out only after 2 weeks. With long-term treatment with a good therapeutic effect, it is possible to reduce the dose.
Pharmacokinetics
Suction and distribution
After oral administration, it is quickly and almost completely absorbed from the gastrointestinal tract. The time to reach Cmax in blood plasma is 6-14 hours. Binding to blood plasma proteins is 70-80% (with albumin - 35-40%). Passes into breast milk.
Metabolism
Intensively metabolized in the liver by deacetylation and demethylation (with the participation of isoenzymes CYP3A4, CYP3A5 and CYP3A7) to form the active metabolite desacetyldiltiazem, which is determined in plasma at 5-10 times lower concentrations than diltiazem and has 2-4 times less activity.
Removal
T1/2 of 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 extended-release tablets 90 mg and 180 mg is up to 10 hours. Excreted through the intestines with bile (65%) and kidneys (35%, including 2-4% unchanged) .
The pharmacokinetics of diltiazem does not change with long-term use. The drug does not accumulate or 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. It is not excreted during hemodialysis and peritoneal dialysis.
In patients with liver failure, bioavailability increases and T1/2 lengthens.
In old age, the clearance of diltiazem may also be reduced.
Indications for use Diltiazem Lannacher 90 mg 20 pcs. extended-release tablets
- Arterial hypertension;
- prevention of angina attacks (including Prinzmetal's angina);
- prevention of attacks of supraventricular arrhythmias (paroxysmal tachycardia, atrial fibrillation or flutter, extrasystole).
Contraindications
- 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;
- Lown-Ganong-Levine 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;
- ventricular tachycardia with a wide QRS complex;
- pregnancy;
- lactation period;
- age under 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 liver and kidney dysfunction, 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, AV block I degree or prolongation of the PQ interval, when used simultaneously with beta-blockers or digoxin, compensated chronic heart failure, with a tendency to bradycardia, in old age.
Application of Diltiazem Lannacher 90 mg 20 pcs. extended-release tablets during pregnancy and breastfeeding
During pregnancy and breastfeeding, Diltiazem Lannacher is contraindicated.
Women of childbearing potential should exclude pregnancy before prescribing diltiazem.
Use in children
The use of the drug is contraindicated in people under 18 years of age (efficacy and safety have not been established).
special instructions
Diltiazem reduces myocardial conductivity, so it is prescribed with extreme caution to patients with first-degree AV block and bradycardia. Caution is also necessary when used in patients with impaired left ventricular function.
Diltiazem should be prescribed with caution to 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 should be used with caution in patients with renal or hepatic impairment; In this group of patients, if necessary, the prescribed dose of the drug should be reduced and the content of urea in the urine and creatinine should be monitored. In patients with impaired liver function, the daily dose should not exceed 90 mg, and regular monitoring of liver function is recommended.
For elderly patients, the dose is selected individually, because T1/2 of diltiazem may increase.
Because diltiazem reduces the peripheral vascular resistance and can cause secondary arterial hypotension; it is necessary to control blood pressure, in particular at the beginning of a course of treatment, while 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 requires surgery under general anesthesia, it is necessary to inform the anesthesiologist about the nature of the therapy being performed (the patient is taking Diltiazem Lannacher).
Drinking alcohol is not recommended while taking Diltiazem Lannacher.
Impact on the ability to drive vehicles and operate machinery
The use of the drug Diltiazem Lannacher may negatively affect the performance of work that requires a high speed of mental and physical reactions (for example, driving vehicles, operating machinery, working at heights).
Overdose
Symptoms: bradycardia, marked decrease in blood pressure, turning into collapse, impaired atrioventricular and sinoatrial conduction, heart failure, cardiogenic shock, asystole, nausea, vomiting, metabolic acidosis, hyperkalemia.
Treatment: depending on the severity of the overdose. It is necessary to rinse the stomach, prescribe activated charcoal, further treatment is symptomatic. If necessary, it is recommended to prescribe atropine, isoprenaline, dopamine or dobutamine, and also, in case of severe conduction disturbances, the use of cardiac pacing is possible. Hemodialysis and peritoneal dialysis are not effective.
Side effects Diltiazem Lannacher 90 mg 20 pcs. extended-release tablets
From the cardiovascular system: bradycardia, ventricular extrasystole, chronic heart failure, sinoauricular block, AV blockade up to asystole, marked decrease in blood pressure, fainting, redness of the skin, angina pectoris, arrhythmia (including flutter and ventricular fibrillation), tachycardia, shortness of breath, peripheral edema. When used in high doses - angina, bradycardia, AV block.
From the digestive system: dry mouth, increased appetite, vomiting, nausea, heartburn, diarrhea, hypertrophic gingivitis, constipation, hypercreatininemia, abdominal pain, impaired liver function, intestinal obstruction.
From the nervous system: headache, general weakness, asthenia, increased 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 of hands and fingers, difficulty swallowing). When used in high doses - paresthesia.
From the organ of vision: visual impairment (transient blindness).
Allergic reactions: increased photosensitivity, itching, skin rash, facial skin flushing, Stevens-Johnson syndrome, erythema multiforme, exfoliative dermatitis.
Other: taking the drug may lead to increased concentrations of liver enzymes in the blood serum and peripheral edema.
When used in high doses - pulmonary edema (difficulty breathing, cough, wheezing), thrombocytopenia, agranulocytosis, galactorrhea, weight gain.
If the drug is abruptly discontinued, withdrawal syndrome may develop with concomitant tachycardia, arterial hypertension and worsening of angina.
Drug interactions
Pharmacodynamic interaction
When diltiazem is taken concomitantly with antihypertensive drugs, an enhanced antihypertensive effect is observed.
When taking diltiazem and digoxin simultaneously, it is possible to increase the concentration of digoxin in the blood.
When taking diltiazem simultaneously with antiarrhythmic drugs, beta-blockers, cardiac glycosides, bradycardia, impaired AV conduction, and symptoms of heart failure may develop.
When used simultaneously with adenosine, the risk of developing prolonged bradycardia is increased.
Salicylates additionally inhibit the ability of platelet aggregation.
Ethanol enhances the antihypertensive effect.
Procainamide, quinidine, and other drugs known to prolong the QT interval increase the risk of significant QT prolongation.
Inhalation anesthesia agents (hydrocarbon derivatives), thiazide diuretics and other drugs that lower blood pressure enhance the hypotensive effect of diltiazem.
Phenytoin reduces the effect of diltiazem.
Antipsychotics (neuroleptics) enhance the antihypertensive effect of diltiazem.
Simultaneous administration of nitrates (including prolonged forms) is possible.
Lithium preparations may enhance the neurotoxic effects of diltiazem (nausea, vomiting, diarrhea, ataxia, tremors and/or tinnitus).
Indomethacin and other NSAIDs, corticosteroids and estrogens, as well as sympathetic drugs reduce the hypotensive effect.
Strengthens the cardiodepressive effect of general anesthetics.
Pharmacokinetic interaction
Cimetidine weakens the process of biotransformation of diltiazem in the liver, slows down its elimination, increasing the duration of action of diltiazem.
Diltiazem increases the concentration of theophylline and carbamazepine in the blood plasma (40-70%) and increases the risk of adverse reactions, incl. ataxia, nystagmus, diplopia, headache, vomiting, confusion, and also increases the concentrations of cyclosporine, digoxin (up to 50%), imipramine, lithium and midazolam.
Enhances the effect of oral hypoglycemic agents (for example, chlorpropamide and glipizide).
With the simultaneous use of diltiazem and cyclosporine in patients with a kidney transplant, the development of intoxication with the latter and paresthesia is possible. Therefore, it is necessary to closely monitor the level of plasma concentrations of cyclosporine in this group of patients.
Eating increases the absorption and bioavailability of diltiazem by 20-30%.
May increase the bioavailability of propranolol.
Increases the concentration of moracizine in blood plasma.
Phenobarbital, diazepam, rifampicin reduce the concentration of diltiazem in the blood plasma.
Increases blood concentrations of quinidine and valproic acid (dose reduction may be required).
Ritonavir may increase plasma concentrations of BMCC.
Diltiazem inhibits the metabolism of midazolam (plasma concentration increases with increased sedative effect).
The elimination of nifedipine is reduced by diltiazem (plasma concentration increases).
Diltiazem significantly increases the plasma concentration of lovastatin. It also enhances the effect of simvastatin, therefore, when used simultaneously, the dose of simvastatin must be reduced. When diltiazem is used concomitantly with lovastatin and simvastatin, patient monitoring is necessary due to the possibility of developing myositis or rhabdomyolysis.
