Diltiazem (HCl)

Diltiazem is an anti-arrhythmic agent. Diltiazem (HCl) is a calcium channel blocking agent. It lowers the blood pressure by blocking calcium and relaxes the heart muscle and dilates the heart blood vessels. It has been known since the late 1800s that calcium influx was necessary for the contraction of muscle. The discovery of these channels also made possible the developemnet of clinically useful blocking drugs.


Adult Dose
Dose: 30 to 60 mg
Single Dose: 45 (45)
Frequency: 8 hourly
Route: PO
Instructions: Maximum dose: 480 mg/day.
Neonatal
Paedriatic
Characteristics
. It is of Synthetic origin and belongs to Benzothiazepin. It belongs to Calcium L-channel antagonist pharmacological group on the basis of mechanism of action. The Molecular Weight of Diltiazem (HCl) is 451.00. It is weakly acidic drug and Its pKa is 7.7.
Contraindications
Diltiazem (HCl) is contraindicated in conditions like Bradycardia,Sick sinus syndrome,Av block of ii &iii degree.
Effects
The severe or irreversible adverse effects of Diltiazem (HCl), which give rise to further complications include Heart block, Hypoglycemia, GI hemorrhage.Diltiazem (HCl) produces potentially life-threatening effects which include Paralytic ileus, Pedal edema, Impaired left vntricular function, Facial flushing, Sinus arrest, Facial flushing, Acute hepatic injury, Atrioventricular conduction disturbances. which are responsible for the discontinuation of Diltiazem (HCl) therapy.The signs and symptoms that are produced after the acute overdosage of Diltiazem (HCl) include Hypotension, Junctional bradycardia, Low cardiac output.The symptomatic adverse reactions produced by Diltiazem (HCl) are more or less tolerable and if they become severe, they can be treated symptomatically, these include Dizziness, Headache, Drowsiness, Fever, Constipation, Insomnia, Skin rashes, Peripheral edema, Bradycardia, GI upset, Hypotension, Weight gain, Flushing, Asthenia, Swelling, AV Block, Sore throat, Skin rashes, dizziness, Fainting.
Indications
'Diltiazem (HCl) is primarily indicated in conditions like Atrial fibrillation, Cardiac arrhythmia, Coronary artery spasm, Hypertension, Migraine, Moderate to severe reflux oesophagitis, Myocardial infarction, Oesophageal motility disorders, Pulmonary hypertension, Raynaud''s phenomenon, Stable angina pectoris, Unstable angina.'
Interactions
Diltiazem (HCl) is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementAcebutololDiltiazem may enhance the hypotensive effect of Acebutolol. Bradycardia and signs of heart failure have also been reported.Diltiazem may decrease the metabolism, via CYP isoenzymes, of Acebutolol. ModerateThough usually safe and effective during concomitant use, monitor for increased evidence of bradycardia, hypotension, or signs of heart failure during concomitant use of Acebutolol and Diltiazem.Ophthalmic beta-blockers are likely of little concern.AdinazolamAlprazolamAmiodarone (HCl)Diltiazem may enhance the bradycardic effect of Amiodarone. Sinus arrest has been reported.MajorMonitor increased therapeutic effects, and potential signs of toxicity (eg, bradycardia, sinus arrest, and decreased cardiac output), of Diltiazem if amiodarone is initiated/dose increased, or decreased effects if amiodarone is discontinued/dose decreased.AmobarbitalBarbiturates reduces hypotensive effects of Diltiazem.MajorAtenololDiltiazem may enhance the hypotensive effect of Atenolol. Bradycardia and signs of heart failure have also been reported.Diltiazem may decrease the metabolism, via CYP isoenzymes, of Atenolol.ModerateThough usually safe and effective during concomitant use, monitor bradycardia, hypotension, or signs of heart failure during concomitant use of Atenolol and Diltiazem. phthalmic beta-blockers are of little concern.Betaxolol (HCl)Increased risk of AV block and bradycardia when beta-blockers (e.g Betaxolol) given with Diltiazem. MajorBisoprolol (Fumarate)Severe hypotension and heart failure when beta-blockers given with Diltiazem.Buspirone (HCl)CarbamazepineCarbamazepine decrease plasma concentration of diltiazem by induction of CYP450 3A4.ModerateThis combination should be avoided.Carteolol (HCl)CilostazoleCimetidine (HCl)Cyclosporin ADigoxinDiltiazem (HCl) [Calcium Channel Blocker (Nondihydropyridine)] may enhance the AV-blocking effect of Digoxin. Diltiazem (HCl) may decrease the metabolism of Digoxin. MajorMonitor for increased therapeutic/toxic effects of digoxin if Diltiazem (HCl) is initiated/dose increased, or decreased effects if Diltiazem (HCl) is discontinued/dose decreased.DisopyramideDiltiazem inhibit CYP450 3A4 result in decrease clearance and increases plasma concentration of Disopyramide. ModerateUse this combination with caution or dose adjustments are required.EnfluraneAdditive pharmacological actions are reported when enflurane giving with diltiazem.Effects include risk of cardiac depression,hypotension,cardiovascular collapse and ventricular impairment.ModerateHemodynamic and electrocardiographic monitoring are required during operation and discontinuation of diltiazem prior to surgery is not advised in coronary heart disease patient due to rebound effect. FosphenytoinHuman InsulinImipramine (HCl)Insulin LisproLabetalolLabetalol with Diltiazem(HCl) may trigger irregular heart beat.LithiumLurasidoneDiltiazem is a Moderate CYP3A4 inhibitor, increases Cmax and AUC of lurasidonemaximum dose of lurasidone should be 40mg/dMetoprolol (Tartrate)Diltiazem may enhance the hypotensive effect of metoprolol. Bradycardia and signs of heart failure have also been reported.Diltiazem may decrease the metabolism, via CYP isoenzymes, of metoprolol.ModerateThough usually safe and effective during concomitant use, monitor bradycardia, hypotension, or signs of heart failure during concomitant use of Metoprolol and Diltiazem. phthalmic beta-blockers are of little concern.MidazolamNitroprussideShould not be use concurrently without doctor or pharmacist approval.Nortriptyline (HCl)ParegoricThe concomitant administration of agents with hypotensive effects and psychotherapeutic agents (e.g., anxiolytics, sedatives, hypnotics, antidepressants, antipsychotics), narcotic analgesics, alcohol, or muscle relaxants may additively increase hypotensive and/or central nervous system depressant effects.ModerateDuring concomitant use of these drugs, patients should be monitored for hypotension and excessive or prolonged CNS depression. Ambulatory patients should be made aware of the possibility of additive effects (e.g., drowsiness, dizziness, lightheadedness, confusion, orthostasis, fainting) and be cautioned about driving, operating machinery, or performing other hazardous tasks, and to arise slowly from a sitting or lying position. Patients should also be advised to notify their doctor if they experience excessive side effects that interfere with their normal activities, or dizziness and fainting.PhenobarbitonePhenytoin (Na)Phenytoin markedly decreases serum levels of Diltiazem through inducing their first pass metabolism and systemic clearance while diltiazem increases phenytoin plasma levels by inhibiting CYP450 3A4 metabolism. Monitoring of the altered effects are required.Porcine InsulinPramipexoleDiltiazem (HCl) decrease the clearance of pramipexole by ~20%.Propranolol (HCl)Both agents act additivelly and reduces the rate,conduction and contractilityof heart results in severe congestive heart failure,hypotension and angina.MajorHemodynamic responses and tolerance should be monitored closely and adjust the dose of one or both agents. Symptoms like fainting, swelling of extremities, weight gain and shortness of breath should be reported promptly.RifampicinTheophyllineDiltiazem inhibit the CYP450 3A4 hepatic metabolism of Theophylline results in increased serum level of theophylline.ModerateClinical monitoring of response and tolerance is recommended. Report should be given if observe any sign of theophylline toxicity.TicagrelorDiltiazem is a moderate CYP3A4 inhibitor, increase Cmax of Ticagrelor by 69%TriazolamVORICONAZOLEVoriconazole may increase the serum concentration of diltiazem by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of diltiazem if voriconazole is initiated, discontinued or dose changed. These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Interfrence
Liver Function Test (LFT)
Risks
Drug should not be given to Paediatrics, Pregnant Mothers, and Neonates.If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.
Storage
Inj Store at room temperature or refrigerator. Do not Freeze. Use within 1 month if kept at room temperature. Tab, Caps Store in a well closed container, Below 40°C. Protect from Sunlight and Moisture.
Warnings
Diltiazem should be used with caution in patients with kidney or liver impairment, vetricular dysfunction, severe bradycardia, cardiogenic shock or congestive heart failure, sinoatrial nodal dysfunction. Consider decrease in dose of calcium channel blockers and monitor drug response in cirrhosis patients. Diltiazem should not be used in patient with acute myocardial infarction. It is classified as pregnancy category C and should be used during pregnancy with caution only when the benefit outweighs the risk to fetus.
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