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Diltiazem ONE OF The CALCIUM CHANNEL BLOCKER DRUGS DILTIAZEM 1 Generic Name: diltiazem (dil TYE a zem). Brand Names: Cardizem, Cardizem CD, Cardizem LA, Cardizem SR, Cartia XT, Dilacor XR, Diltia XT, Tiazac. DILTIAZEM 2 Description : Diltiazem hydrochloride, is a Calcium channel antagonist and widely used in the treatment of certain types of cardiovascular. Chemically : Chemically, diltiazem hydrochloride is 1,5Benzothiazepin-4(5H)-one,3-(acetyloxy)-5[2(dimethylamino)ethyl]-2,-3-dihydro-2( 4methoxyphenyl)-, mono-hydrochloride, (+ )-cis. DILTIAZEM 3 The chemical structure : DILTIAZEM 4 Physical properties : Diltiazem hydrochloride It is soluble in water, methanol and chloroform and has a molecular weight of 450.98 . the drug was stable at storage temperatures, 5-55°C, for 12 weeks. DILTIAZEM 5 Clinical Pharmacology : Diltiazem (DTZ) is a calcium antagonist widely used in the treatment of angina and-related heart diseases. The therapeutic effects of diltiazem hydrochloride its ability to inhibit the cellular influx of calcium ions during membrane depolarization of cardiac and vascular smooth muscle. DILTIAZEM 6 Pharmacodynamic : DILTIAZEM 7 1- Mechanisms of Action: Diltiazem blocks the transport of calcium into the smooth muscle cell. Since calcium is important in muscle contraction. blocking calcium transport relaxes artery muscle and dilates coronary arteries and other arteries of the body DILTIAZEM 8 Hypertension: Diltiazem produces its antihypertensive effect by relaxation of vascular smooth muscle. Angina : This is With calcium antagonists has several advantages. Unlike other antianginal agents it does not alter heart rate, blood pressure, or conduction. DILTIAZEM 9 2- Pharmacological Effect : Like other calcium channel antagonists, diltiazem decreases SA and AV conduction and has a negative inotropic effect. Diltiazem hydrochloride decreases vascular resistance (VR), increases cardiac output (COP) (by increasing stroke volume), and produces a slight decrease in heart rate. DILTIAZEM 10 Pharmacokinetic : DILTIAZEM 11 1. Absorption : Diltiazem is well absorbed from the gastrointestina1tract . Route of drug administeration: Intranasal, Intraperitoneal,Oral, Intracerebroventricular,Intravenous. DILTIAZEM 12 2. Distribution : The plasma half-life of diltiazem is approximately 3.0-4.5 h. Therapeutic blood levels of diltiazem appear to be in the range of 40-200 ng/mL. The diltiazem hcl is 70% to80% bound to plasma protein. DILTIAZEM 13 3. Metabolism : Diltiazem hydrochloride is metabolized by the liver it is hepatic first-pass effect . The two primary metabolites of diltiazem are desacetyldiltiazem and desmethyldiltiazem. Drugs which induce or inhibit hepatic microsomal enzymes may alter diltiazem disposition. DILTIAZEM 14 4. Excreation : The diltiazem excreated by kidney and in bile. Diltiazem metabolites have been identified in the urine of humans. Only 2% to 4% of unchanged diltiazem appears in the urine. These metabolites are more slowly excreted. The elimination half-life after single or multiple dosing is 4 to 9.5 hours (mean 6.5 hours). DILTIAZEM 15 CONTRAINDICATION DILTIAZEM 16 1. Cardiac Conduction : Diltiazem hydrochloride prolongs AV node refractory periods. 2. Congestive Heart Failure : Diltiazem has a negative inotropic effect. DILTIAZEM 17 3. Hypotension : Decreases in blood pressure. 4. Acute Hepatic Injury : Mild elevations of transaminases with and without elevation in alkaline phosphatase and bilirubin. DILTIAZEM 18 5. Nursing Mothers : Diltiazem is excreted in human milk. 6. Pregnancy : Have embryo and fetal lethality, a propensity to cause abnormalities of the skeleton, heart, retina, and tongue of embryo. DILTIAZEM 19 Drug Interactions DILTIAZEM 20 1. Beta Blockers : Diltiazem hydrochloride with propranolol resulted in increased propranolol 50%. 2. Cimetidine : Increase in diltiazem plasma levels (58%) after a 1-week course of treatment. DILTIAZEM 21 3. Digitalis : Diltiazem hydrochloride with digoxin increased plasma digoxin concentrations approximately 20%. 4. Cyclosporine : A reduction of cyclosporine dos ranging from 15% to 48% . The effect of cyclosporine on diltiazem plasma concentrations has not been evaluated. DILTIAZEM 22 5. Carbamazepine : Diltiazem with carbamazepine result in elevated serum levels of carbamazepine (40% to 72% increase). 6. Benzodiazepines : Diltiazem increased of benzodiazepines (midazolam and triazolam). DILTIAZEM 23 7. Lovastatin : Diltiazem (120 mg)with lovastatin resulted in a 3-4 times increase in lovastatin. 8. Rifampin : Rifampin with diltiazem lowered the diltiazem plasma concentrations to undetectable levels. DILTIAZEM 24 9. Anesthetics : with anesthetics may be potentiated by calcium channel blockers. DILTIAZEM 25 ADVERSE REACTIONS DILTIAZEM 26 1. Cardiovascular : Angina, arrhythmia, AV block (second- or third-degree), congestive heart failure, hypotension, palpitations, tachycardia. 2. Nervous System : Abnormal dreams, gait abnormality, hallucinations, insomnia, nervousness, personality change, tremor. DILTIAZEM 27 3. Gastrointestinal : Anorexia, constipation, diarrhea, dry mouth, nausea,vomiting, weight increase. 4. Dermatological : Petechiae, photosensitivity, pruritus. DILTIAZEM 28 OVERDOSAGE The toxic dose in man is not known. The resultant are bradycardia, hypotension, heart block, and cardiac failure. DILTIAZEM 29 1. Bradycardia : Administer atropine (0.60 to 1.0 mg). 2. High-Degree AV Block : Administer atropine (0.60 to 1.0 mg). should be treated with cardiac pacing. 3. Cardiac Failure : Administer inotropic agents (isoproterenol, dopamine, or dobutamine) and diuretics. 4. Hypotension : Vasopressors (e.g., dopamine or levarterenol bitartrate). DILTIAZEM 30 DOSAGE AND ADMINISTRATION DILTIAZEM 31 1. Hypertension : Usual starting doses are 120 to 240 mg once daily. usually observed by 14 days of chronic therapy. 2. Angina : Starting with a dose of 120 mg to 180 mg once daily. over 7 to 14 days. DILTIAZEM 32 Route of drug administeration: Intranasal,Intraperitoneal,Oral, Intracerebroventricular,Intravenous. DILTIAZEM 33 Doasage : Usual capsules contain diltiazem hydrochloride beads at doses of 120,180,240,300,360and 420 mg. DILTIAZEM 34 Side Effects DILTIAZEM 35 Less serious side effects : Flushing(redness). headache. Constipation,diarrhea,or nausea. Fatigue or triedness . Decrease blood pressure and worsening. rash. Difficulty urinating. Slow heart rate Tingaling sensation in the arm. but more common slow heart rate and constipation. DILTIAZEM 36 More serious side effects : Allergic reaction. Abnormal behavior or psychosis. Jaundice. Sever dizziness. Slurred speech. Confusion.. Pruritis Leg swelling. Heart failure. DILTIAZEM 37 Conclusion: Amldipine: it is widely used ca channel blocker in controlling morning blood pressure because of its long half life 30-50h . Nifedipine: Is used in treatment of hypertension,angina and to control preterm labour.It is not used if there is ischemic heart disease,hepatic dysfunction or chronic malabsorption syndrome. DILTIAZEM 38 Feldopine(piendil): Is indicated mainly for treatment hypertension and arrhythmia and the most common side effect reported with feldopine administerated as monotherepy were peripheral edema and headache. DILTIAZEM 39 Verpamil: It is used to tretment stable angina,un stable angina .Most common adverse reaction : constipation ,dizziness and nausea. DILTIAZEM 40 Diltiazem : its used to treatment the high blood pressure ,control chest pain and to slow unusually fast heartbeats. contraindication:is pregnancy ,nursing mother,allergic reaction ,kidney,liver,BV,or heart disease. DILTIAZEM 41 Thank you DILTIAZEM 42 Provised by: Dr. Hanan Produced by: Ahlam Fahd DILTIAZEM 43