Diltiazem


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intravenous
Cardiac arrhythmias
Adult: Initially, 250 mcg/kg via bolus injection over 2 minutes. May give a further dose of 350 mcg/kg after 15 minutes if needed. In patients with atrial fibrillation or flutter: Following bolus injection, initiate infusion at rate of 5-10 mg/hour, may increase in increments of 5 mg/hour up to Max of 15 mg/hour. May continue infusion for up to 24 hours.

Oral
Angina pectoris
Adult: Conventional tab: 30 mg 4 times daily, may increase dose gradually in divided doses at 1-2 day intervals until desired response is achieved. Max: 360 mg daily in divided doses. Modified-release tab/cap: Initially, 60 mg tid, may increase to 360 mg daily in divided doses or 480 mg daily, as necessary. Dosage adjustment and dose frequency may vary depending on the formulation.
Elderly: Modified-release tab/cap: Initially, 60 mg bid, may increase carefully to 240 mg once daily if heart rate remains >50 beats/min.

Oral
Hypertension
Adult: Modified-release cap: Initially, 90-120 mg bid, may increase to 180 mg bid if necessary. Max: 360 mg daily.
Elderly: Modified-release cap: Initially, 60 mg bid, may increase carefully to 240 mg once daily.
Renal Impairment
Angina pectoris: Modified-release tab/cap: Initially, 60 mg bid, may increase carefully to 240 mg once daily if heart rate remains >50 beats/min.

Hypertension: Modified-release cap: Initially, 60 mg bid, may increase carefully to 240 mg once daily.
Hepatic Impairment
Angina pectoris: Modified-release tab/cap: Initially, 60 mg bid, may increase carefully to 240 mg once daily if heart rate remains >50 beats/min.

Hypertension: Modified-release cap: Initially, 60 mg bid, may increase carefully to 240 mg once daily.
Cách dùng
Normal Release Prep: May be taken with or without food.
Hướng dẫn pha thuốc
IV infusion: Further dilute solution with 0.9% NaCl, dextrose 5% in water, dextrose 5% in water with 0.45% NaCl to make a Max final concentration of 1 mg/mL.
Chống chỉ định
Sick sinus syndrome, 2nd or 3rd degree atrioventricular (AV) block without a functioning pacemaker, severe bradycardia (<50 beats/minute), hypotension (<90 mmHg systolic), severe CHF, acute myocardial infarction and pulmonary congestion; IV: atrial fibrillation or flutter with accessory bypass tract (e.g. Wolff-Parkinson-White syndrome), ventricular tachycardia. Lactation. Concomitant use with ivabradine, dantrolene and IV β-blockers.
Thận trọng
Patient with reduced left ventricular dysfunction, intestinal obstruction, 1st degree AV block; diabetes mellitus, pre-existing bronchial hyperactivity, supraventricular arrhythmias with comprised haemodynamics (IV). Renal and hepatic impairment. Elderly. Pregnancy.
Phản ứng phụ
Significant: AV block or sinus bradycardia, hypotension with or without syncope, mood changes, bronchospasm (including asthma aggravation). Rarely, elevated hepatic transaminases (e.g. alkaline phosphatase, LDH, AST, ALT), hepatic injury.
Cardiac disorders: Palpitations, ventricular extrasystoles (IV).
Gastrointestinal disorders: Constipation, dyspepsia, gastric pain, nausea.
General disorders and admin site conditions: Malaise, asthenia; inj site reaction (e.g. itching, burning).
Metabolism and nutrition disorders: Oedema, peripheral oedema.
Nervous system disorders: Headache, dizziness.
Skin and subcutaneous tissue disorders: Erythema multiforme including Stevens-Johnson syndrome, toxic epidermal necrolysis; exfoliative dermatitis.
Vascular disorders: Flushing.
IV/Parenteral/PO: C
Thông tin tư vấn bệnh nhân
This drug may cause dizziness and malaise, if affected, do not drive or operate machinery. Avoid abrupt withdrawal.
Monitoring Parameters
Monitor heart rate, blood pressure, ECG, kidney and liver function, signs and symptoms of respiratory impairment.
Quá liều
Symptoms: Hypotension leading to collapse and acute kidney injury, sinus bradycardia with or without isorhythmic dissociation, sinus arrest, atrioventricular (AV) conduction disturbances, cardiac arrest. Management: Supportive and symptomatic treatment. Manage conduction disturbances and heart block with cardiac pacing. Perform gastric lavage and administer activated charcoal and/or IV calcium for ventilatory support. Consider corrective treatments such as atropine, vasopressors (e.g. dopamine, norepinephrine), and inotropic agents (e.g. isoproterenol, dopamine, dobutamine) for bradycardia, hypotension, and cardiac failure, respectively.
Tương tác
Increased depression of cardiac conduction, risk of bradycardia and AV block with amiodarone, digoxin, and clonidine. Potentiated depressive effects on cardiac contractility, conductivity, and automaticity, and vascular dilatation of anaesthetics. Increased antihypertensive effect with α-antagonists. Increased serum concentration of ciclosporin, phenytoin, carbamazepine, cilostazol, benzodiazepine (e.g. midazolam, triazolam), buspirone, quinidine, corticosteroids (e.g. methylprednisolone), lithium and theophylline. Increased plasma concentration with CYP3A4 inhibitors (e.g. cimetidine). Decreased serum concentration with CYP3A4 inducers (e.g. rifampicin). Increased cardiovascular effect (e.g. hypotension) of IV ionic X-ray contrast media. May enhance effects of antiplatelet drugs. Increased risk of myopathy and rhabdomyolysis with concomitant use of statins metabolised by CYP3A4 (e.g. atorvastatin, fluvastatin, simvastatin).
Potentially Fatal: Increased risk of lethal ventricular fibrillation with dantrolene infusion. Enhanced hypotensive effect, increased risk of bradycardia and signs of heart failure with β-blockers. Increased bradycardic effect of ivabradine.
Food Interaction
Increased serum concentration with grapefruit or grapefruit juice. Decreased serum concentration with St John’s wort.
Tác dụng
Description: Diltiazem, a benzothiazepine calcium channel blocker, inhibits the influx of Ca ions during depolarisation of the vascular smooth muscles and myocardium thereby producing relaxation of coronary vascular muscles and coronary vasodilation and increases myocardial oxygen delivery.
Onset: Oral: 30-60 minutes (immediate release); IV: 3 minutes (bolus).
Duration: IV: 1-3 hours (bolus); 0.5-10 hours (continuous infusion, after discontinuation).
Pharmacokinetics:
Absorption: Almost completely absorbed from the gastrointestinal tract after oral administration. Bioavailability: Approx 40% (oral). Time to peak plasma concentration: 2-4 hours (immediate-release); 11-18 hours (extended-release tab); 10-14 hours (extended-release cap).
Distribution: Present in breastmilk. Volume of distribution: 3-13 L/kg. Plasma protein binding: 70-80%.
Metabolism: Undergoes extensive first-pass metabolism by CYP450 and conjugation to N-monodesmethyldiltiazem, desacetyldiltiazem, desacetyl-N-monodesmethyldiltiazem, desacetyl-O-desmethyldiltiazem and desacetyl-N,O-desmethydiltiazem.
Excretion: Via urine (2-4% as unchanged drug), faeces. Elimination half-life: Oral: 3-4.5 hours (immediate-release); 6-9 hours (extended-release tab); 4-9.5 hours (extended-release cap). IV: Approx 3-4 hours; 4-5 hours (continuous infusion).
Đặc tính

Chemical Structure Image

Source: National Center for Biotechnology Information. PubChem Database. Diltiazem, CID=39186, https://pubchem.ncbi.nlm.nih.gov/compound/Diltiazem (accessed on Jan. 21, 2020)

Bảo quản
Cap/tab: Store at 25°C. Protect from light. Avoid excessive heat and humidity. Solution for injection: Store between 2-8°C. Do not freeze.
Phân loại MIMS
Phân loại ATC
C08DB01 - diltiazem ; Belongs to the class of benzothiazepine derivative selective calcium-channel blockers with direct cardiac effects. Used in the treatment of cardiovascular diseases.
References
Anon. Diltiazem. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 09/08/2019.

Buckingham R (ed). Diltiazem Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 09/08/2019.

Cardizem Tablet, Coated (Sanofi-Aventis US LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 24/11/2014.

Diltiazem Hydrochloride Extended-Release Capsule (Ingenus Pharmaceuticals, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 09/08/2019.

Diltiazem Hydrochloride Injection (Akorn, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 24/11/2014.

Diltiazem Hydrochloride Solution for Injection (Hospira, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 09/08/2019.

Diltiazem Hydrochloride Tablet (Clinical Solutions Wholesale, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 09/08/2019.

McEvoy GK, Snow EK, Miller J et al (eds). Diltiazem Hydrochloride. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 24/11/2014.

Tiazac Extended-Release Capsules. U.S. FDA. https://www.fda.gov/. Accessed 24/11/2014.

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