• Diltiazem general information

      • Diltiazem (Diltiazem): instruction, and the use of a formula

      • Code CAS

      • Feature substance Diltiazem

      • Pharmacology

      • Application of the substance Diltiazem

      • Contraindications

      • Restrictions on the use

      • Application of pregnancy and breastfeeding

      • Side effects of substance Diltiazem

      • Interaction

      • Overdose

      • Dosing and Administration

      • Precautions substance Diltiazem

Cardizem Diltiazem 30, 60, 90, 120, 180 mg
Most popular brand: Cardizem
Active ingredient: Diltiazem
Available dosage forms: 30, 60, 90, 120, 180 mg
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Diltiazem general information

Swollen gums could also manifest as a consequence of side effects of certain medications, like diltiazem, amlodipine, felodipine, phenytoin, etc.. Taking initial loading doses for a prolonged time period can also earn a person vulnerable to hypercalcemia. This could lead to severe side consequences. Not only that, They are advised to keep away from drugs that bring about blood vessel constriction. This may occur because of number of reasons, but mostly is because of the exact factors which are involved in blood vessel narrowing. More tests may be necessary to set a comprehensive symptom picture related to the raised blood pressure.

If any one of the side effects are felt, the individual need to immediately search for medical care. In case the patient does not receive relief from these, or if the symptoms are extremely severe, surgical intervention or several other options could possibly be resorted to. It might be a substantial source of patient over treatment. This permits them to be utilized in the therapy for heart arrhythmia. A number of studies have shown that it could end up being beneficial in the therapy for anxiety. Its use was found to be beneficial for treating depression and obsessive-compulsive disorder.

Heart medicine that’s healthy as well as happy! I’ll take these medicines for the remainder of my own life. Remember to know when to utilize drugs like epinephrine, vasopressin, and atropine. Then ask your physician to compare your blood pressure readings at a following date to determine what progress you’ve made. You might have read some healthcare papers on the drug. They could save you from administering the incorrect dose of the drug.

Drug-induced lupus erythematosus is connected with the application of certain drugs which are prescribed for remedying heart circumstances, thyroid issues, superior blood pressure, and neuropsychiatric disorders. Due to this, the drug might also be used for healing abnormal heart rhythms together with high blood pressure. For this reason, the drug is, in addition, frequently used for improving abnormal heart rhythms. Though people that have AV block but make use of a pacemaker are permitted to make use of the drug. Now that’s really a substantial amount and there are really no side results. This drug ought to be combined with well balanced calorie controlled diet that’s rich in vegetables and fruits.

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Diltiazem (Diltiazem): instruction, and the use of a formula

Code CAS

Feature substance Diltiazem

benzothiazepine derivative. White or off-white crystalline powder with a bitter taste. Insensitive to light. Soluble in water, methanol, chloroform.

Pharmacology

Mode of action -. Antianginal, hypotensive, antiarrhythmic

voltage-blocking calcium channels L – type and inhibits the entry of calcium ions in the depolarization phase cardiomyocytes and smooth muscle cells. As a result of inhibition of calcium flux slow depolarization in excitable tissues cells inhibits the formation of the building and divides the process of “excitation – contraction.” It decreases myocardial contractility, reduces heart rate and slows AV conduction. It relaxes smooth muskulatu vessels, lowers systemic vascular resistance. It has a dose-dependent antihypertensive effect in mild to moderate hypertension. The degree of reduction in blood pressure correlated with the level of hypertension (in people with normal blood pressure is marked only the minimum of his fall). Antihypertensive action is shown in both the horizontal and vertical position. Rarely cause postural hypotension and reflex tachycardia. It does not change or slightly reduces the maximum heart rate under load.

Long-term therapy is not soprovovozhdaetsya giperkateholaminemii, increased activity of the renin – angiotensin – aldosterone system. Decreases renal and peripheral effects of angiotensin II. Antianginal effect is due to a decrease in myocardial oxygen demand, due to a decrease in heart rate and systemic blood pressure. vasodilation epicardial vessels, the ability to eliminate koronarospazm. It relaxes the smooth muscles of the coronary vessels in a concentration that does not cause negative inotropic effect. Efficiency with supraventricular tachycardia associated with an increase (20%) effective and functional refractory period of AV node and extension of time in the AV node (in normal heart rate effects on the AV node is minimal). It slows down the ventricular rate in patients with high ventricular rate during fibrillation and atrial flutter. Restores normal sinus rhythm of paroxysmal supraventricular tachycardia, interrupts the circulation of excitation in the type of re – entry at nodal tachycardia and tachycardia with reciprocal conduct, including WPW – syndrome e Long-term use is accompanied by a slight increase in the sinoatrial PR interval on the ECG.. The syndrome sick sinus significantly prolongs sinus cycle. When fibrillation and atrial flutter in a bolus injection effectively lowers the heart rate (not less than 20% in 95% of patients). The action usually occurs within 3 minutes and reaches its maximum in the range of 2 – 7 min. Curtailment rate is maintained for 1 –. 3h Prolonged infusion, decrease heart rate by 20% is observed in 83% of patients and persists after the administration for a period of from 0.5 h to 10 h Efficiency in restoring sinus rhythm in paroxysmal supraventricular tachycardia is 88. % within 3 min. In patients with severe left ventricular changes (heart failure, myocardial infarction, hypertrophic cardiomyopathy) does not alter the contractility, the final Dad in the left ventricle and the pulmonary capillary wedge pressure. It has a minimal effect on the smooth muscles of the gastrointestinal tract. Long-term (8 months) therapy is not accompanied by the development of tolerance and changes in plasma lipid profile. Able to cause regression of left ventricular hypertrophy in patients with hypertension. The usual therapeutic doses has no effect on mortality, but in patients with symptoms of pulmonary congestion increased incidence of heart – cardiovascular complications by 40%. In patients with acute myocardial infarction thrombolytic therapy on the background of plasminogen activator increased incidence of hemorrhagic complications in 5 times.

Good (more than 90% of the dose) is absorbed from the gastrointestinal tract. Bioavailability is 40% (pronounced effect “first pass” through the liver). C max is achieved through a 2 – 4 h (Table.), 3,9 – 4,3 h (capsules 180 mg.), 5 – 7 hours (Table retard.) 6 – 14 h ( caps. Prolong.). The volume of distribution of 5.3 l / kg. T 1/2 is 1 – 3 hours (with on / in the introduction), 3 – 4,5 hours (Table.) 5 – 7 hours (Table retard.), 7,3 – 14 7 h (caps. 180 mg). Associated with the plasma protein by 70 – 80% (40% ; with the acid alpha – glycoprotein 30% ; with albumin). The action develops within 3 minutes with the rapid on / in the introduction, through a 2 – 3 hours (CBSA prolong..) Or 30 – 60 min (Table.) In the appointment of the inside. The duration of the ingestion of 4 – 8 hours (see Table.) And 12 – 24 h (CBSA prolong..). It is metabolized in the liver by deacetylation, demethylation with the participation of cytochrome P450 (in addition to conjugation). Two main metabolites detected in plasma after oral administration ; deatsetildiltiazem and dezmetildiltiazem. Deacetylated metabolite has coronary vasodilator properties (plasma concentration is 10 – 20% active ; 25 – 50% of that of diltiazem), is capable of accumulation. For a single intravenouslytroduction of these metabolites are not found in plasma. Concentrated in bile and undergoes enterohepatic circulation. Excretion (including metabolites) is carried out mainly through the digestive tract (65%) and to a lesser extent by the kidneys (35%). The urine metabolites determined 5 and 2 – 4% unchanged drug. Penetrates into breast milk. With prolonged ingestion increased bioavailability and decreased clearance, which leads to increased therapeutic effects and side effects.

Based on the results obtained in 21 – 24 – month experiments on rats and mice and bacterial tests in vitro, does not have carcinogenic and mutagenic activity. In experiments on rats, mice, rabbits at doses in the 5 – 10 times the recommended daily dose for a person causes the death of embryos and fetuses, decreased survival of newborn rats and the development of skeletal abnormalities. At doses of 20 or more times higher than recommended for humans, increased incidence of stillbirths in experimental animals.

It is possible to use in transplantation: after kidney transplantation (prevention of graft failure) during immunosuppressive therapy (to reduce the nephrotoxicity of cyclosporin A).

Application of the substance Diltiazem

angina (stable vasospastic); prevention of coronary spasm during coronary angiography or coronary artery bypass surgery; hypertension (monotherapy or in combination with other antihypertensive drugs), including after myocardial infarction (mostly retard form when contraindicated beta – blockers) in patients with concomitant angina (in the presence of contraindications to beta – blockers) in patients with diabetic nephropathy (when ACE inhibitors are contraindicated); paroxysmal supraventricular tachycardia.

Contraindications

Hypersensitivity, severe hypotension (Sad less than 90 mm Hg..), Cardiogenic shock, left ventricular systolic dysfunction (clinical and radiological signs of stagnation in the lung, the left ventricular ejection fraction less than 35 – 40%), including . acute myocardial infarction, sinus bradycardia (. less than 55 beats / min), sinus node weakness syndrome (if a pacemaker), sinoatrial and AV blockade II – III degree (without pacemaker), WPW – syndrome and Lown syndrome; Ganong ; Levin with paroxysmal atrial fibrillation or flutter (except for patients with a pacemaker), pregnancy, breast-feeding.

Restrictions on the use

sinoatrial and AV blockade degree I, marked aortic stenosis, intraventricular violation of excitation (blockade of the left or right bundle branch), chronic heart failure, renal and / or hepatic insufficiency, elderly, children (efficacy and safety have not been determined ) age.

Application of pregnancy and breastfeeding

is contraindicated in pregnancy.

Category effects on the fetus by FDA ; C.

breast-feeding should be discontinued at the time of treatment.

Side effects of substance Diltiazem

From the cardio – vascular system and blood (blood, hemostasis): transient hypotension; bradycardia, conduction disturbances I level, a decrease in cardiac output, heart rate, fainting, eosinophilia.

From the nervous system and sensory organs: headache, dizziness, weakness, fatigue.

With the genitourinary system: peripheral edema, violation of potency (individual cases).

From the digestive tract: dyspepsia (constipation or diarrhea, nausea, heartburn and other more common in elderly patients.), Gingival hyperplasia mucous membrane (rarely).

For the skin: sweating, reddening of the skin.

Allergic reactions: skin rash and itching, rare ; exudative erythema multiforme.

Other: increased activity of transaminases (ALT AST.), LDH and alkaline phosphatase. hyperglycemia (isolated cases).

Interaction

It increases the plasma levels of , , , . It can enhance the depressant effect of anesthetics on contractility, conductivity and automaticity of the heart. It weakens the nephrotoxic effects of cyclosporine A. cimetidine increases the plasma diltiazem, digoxin ; potentiates tahisistolicheskoy efficiency in the form of atrial fibrillation. Antiarrhythmic agents or beta – blockers contribute to the development of bradycardia, AV conduction disorders, heart failure symptoms. Antihypertensive drugs increase the hypotensive effect. A solution of diltiazem is not compatible with furosemide solution.

Overdose

Symptoms: bradycardia, hypotension, intracardiac blockade and heart failure.

Treatment: gastric lavage, the appointment of activated carbon, plasmapheresis and hemoperfusion using activated carbon. The properties have an antidote calcium supplements (calcium gluconate) with on / in the introduction, symptomatic therapy ; atropine, isoproterenol, dopamine or dobutamine, diuretics, infusion liquids. At high degrees of AV block may conduct electrical pacing.

Dosing and Administration

Inside, is not liquid at 30 mg 3 – 4 times a day; if necessary ; to 240 mg / day. Against the background of impaired renal or hepatic function, in elderly initial dose of 60 mg / day in 2 divided doses. Dosage forms with prolonged action: 90 mg 2 – 3 times a day, or 120 – 180 mg 2 times a day at intervals of 12 hours or at 200 – 300 mg 1 time per day. The maximum daily dose of ; 360 mg.

Precautions substance Diltiazem

In patients receiving long-acting formulations are not recommended in / with the introduction of beta – blockers. Caution should be used to normalize heart rhythm in patients with impaired hemodynamics, or in conjunction with drugs that reduce peripheral vascular resistance. contractility and conductivity of the myocardium. Parenteral administration is possible with vehicles and equipment (including defibrillator) to provide emergency assistance. Prolonged / introduction requires constant monitoring of ECG and blood pressure.

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