Isradipine

May be taken with or without food.

Patient with CHF, severe aortic stenosis, hypertrophic cardiomyopathy with outflow tract obstruction. Hepatic impairment. Pregnancy and lactation.

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.

PO: C

Monitor blood pressure, heart rate; signs and symptoms of heart failure.

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.

Increased serum concentration with cimetidine. Reduced serum concentration with rifampicin. Concomitant use with fentanyl anaesthesia may result to severe hypotension.

May cause a false-positive aldosterone/renin ratio.

Description:
Mechanism of Action: 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).

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.

Store between 20-25°C. Protect from humidity, moisture, and light.

Thuốc đối kháng calci

C08CA03 - isradipine ; Belongs to the class of dihydropyridine derivative selective calcium-channel blockers with mainly vascular effects. Used in the treatment of cardiovascular diseases.

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.