Isradipine


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Hypertension
Adult: Initially, 2.5 mg bid; may increase, if necessary, in increments of 5 mg daily at 2-4 weeks intervals up to Max of 20 mg daily.
Cách dùng
May be taken with or without food.
Thận trọng
Patient with CHF, severe aortic stenosis, hypertrophic cardiomyopathy with outflow tract obstruction. Hepatic impairment. Pregnancy and lactation.
Tác dụng không mong muốn
Significant: Angina, MI (during initiation or dose titration); reflex tachycardia resulting in angina and/or MI (in patients with obstructive coronary disease); peripheral oedema. Rarely, symptomatic hypotension with or without syncope.
Cardiac disorders: Palpitations, chest pain, tachycardia.
Gastrointestinal disorders: Nausea, diarrhoea, vomiting, abdominal distress.
General disorders and administration site conditions: Fatigue, weakness.
Nervous system disorders: Headache, dizziness.
Renal and urinary disorders: Pollakiuria.
Respiratory, thoracic and mediastinal disorders: Dyspnoea.
Skin and subcutaneous tissue disorders: Rash.
Vascular disorders: Flushing.
Chỉ số theo dõi
Monitor blood pressure, heart rate; signs and symptoms of heart failure.
Quá liều
Symptoms: Lethargy, sinus tachycardia, excessive peripheral vasodilation; prolonged systemic hypotension and tachycardia. Management: Symptomatic and supportive treatment. Induce emesis, perform gastric lavage, and administer activated charcoal followed in 30 minutes by saline cathartic. May administer vasoconstrictor (e.g. epinephrine, norepinephrine, levarterenol) for clinically significant hypotension. May administer IV Ca salts or glucagon for refractory hypotension or in atrioventricular conduction disturbances.
Tương tác
Increased serum concentration with cimetidine. Reduced serum concentration with rifampicin. Concomitant use with fentanyl anaesthesia may result to severe hypotension.
Ảnh hưởng đến kết quả xét nghiệm
May cause a false-positive aldosterone/renin ratio.
Tác dụng
Description: Isradipine is a dihydropyridine Ca channel blocker which inhibits Ca ion influx into cardiac and smooth muscle during depolarisation, thereby producing relaxation which results in coronary vasodilation and reduction of blood pressure.
Onset: 2-3 hours; full hypotensive effect may not occur for 2-4 weeks.
Duration: >12 hours.
Pharmacokinetics:
Absorption: Almost completely absorbed from the gastrointestinal tract. Bioavailability: 15-24%. Time to peak plasma concentration: 1-1.5 hours.
Distribution: Crosses the placenta. Volume of distribution: 3 L/kg. Plasma protein binding: Approx 95%.
Metabolism: Extensively metabolised in the liver by CYP3A4 isoenzyme via oxidation and ester cleavage into 6 inactive metabolites; undergoes extensive first-pass metabolism.
Excretion: Via urine (60-65% as metabolites); faeces (25-30%). Elimination half-life: 1.5-2 hours (alpha); 8 hours (terminal).
Đặc tính

Chemical Structure Image
Isradipine

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 3784, Isradipine. https://pubchem.ncbi.nlm.nih.gov/compound/3784. Accessed July 26, 2022.

Bảo quản
Store between 20-25°C. Protect from humidity, moisture, and light.
Phân loại MIMS
Thuốc đối kháng calci
Phân loại ATC
C08CA03 - isradipine ; Belongs to the class of dihydropyridine derivative selective calcium-channel blockers with mainly vascular effects. Used in the treatment of cardiovascular diseases.
Tài liệu tham khảo
Anon. Isradipine. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 01/07/2022.

Anon. Isradipine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 01/07/2022.

Buckingham R (ed). Isradipine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/07/2022.

Isradipine Capsule (AvPAK). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 01/07/2022.

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