Felodipine


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Angina pectoris
Adult: Initially, 5 mg daily, may increase to 10 mg daily as necessary.
Elderly: Initially, 2.5 mg daily.

Oral
Hypertension
Adult: Initially, 5 mg daily. Individualised dose may be adjusted based on patient response. Usual dose: 2.5-10 mg daily.
Elderly: Initially, 2.5 mg daily. Monitor blood pressure during titration.
Hepatic Impairment
Initially, 2.5 mg daily. Monitor blood pressure during titration.
Cách dùng
May be taken with or without food. Take w/o food or w/ a light meal. Avoid grapefruit juice.
Chống chỉ định
Decompensated heart failure, acute myocardial infarction, unstable angina pectoris, significant cardiac valvular obstruction, cardiac outflow obstruction. Pregnancy.
Thận trọng
Patient with pronounced gingivitis/periodontitis, severe aortic stenosis, heart failure, hypertrophic cardiomyopathy with outflow tract obstruction. Hepatic impairment. Elderly. Lactation.
Phản ứng phụ
Significant: Tachycardia, myocardial ischaemia, peripheral oedema, angina, rarely, hypotension with or without syncope.
Cardiac disorders: Palpitations.
Gastrointestinal disorders: Nausea, abdominal pain, vomiting, mild gingival hyperplasia.
General disorders and admin site conditions: Fatigue.
Investigations: Very rarely, increased hepatic enzymes.
Nervous system disorders: Headache, dizziness.
Vascular disorders: Flushing.
Thông tin tư vấn bệnh nhân
This drug may cause dizziness, fatigue, nausea and headache, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor blood pressure and heart rate. Monitor blood pressure and heart rate. Assess for development of peripheral oedema.
Quá liều
Symptoms: Excessive peripheral vasodilation with marked hypotension, bradycardia. Management: Symptomatic treatment. Administration of activated charcoal and perform gastric lavage within 1 hour of ingestion. For severe hypotension, elevate legs and place patient in supine position. In case of bradycardia, 0.5-1 mg atropine IV may be given, if insufficient, plasma volume may be increased by infusion. May consider sympathomimetic agents based on clinical decision.
Tương tác
Increased plasma concentrations with CYP3A4 inhibitors (e.g. cimetidine, erythromycin, itraconazole, ritonavir). Decrease plasma concentrations with CYP3A4 inducers (e.g. phenytoin, carbamazepine, rifampicin, barbiturates, efavirenz). May increase serum concentration of tacrolimus.
Food Interaction
Increased plasma concentration with high-fat meal. Increased plasma concentration with grapefruit or grapefruit juice. Decreased plasma concentration with St. John’s wort.
Lab Interference
May result to false-negative aldosterone/renin ration (ARR).
Tác dụng
Description: Felodipine, a dihydropyridine Ca-channel blocker, produces coronary vascular smooth muscle relaxation and coronary vasodilation by inhibiting the entry of Ca ions in select voltage-sensitive areas of vascular smooth muscle and myocardium during depolarisation. It also increases myocardial oxygen delivery in cases of vasospastic angina.
Onset: 2-5 hours.
Duration: 24 hours.
Pharmacokinetics:
Absorption: Almost completely absorbed from the gastrointestinal tract. Increased plasma concentration with high fat meal. Bioavailability: Approx 15%. Time to peak plasma concentration: 2.5-5 hours.
Distribution: Enters breast milk. Plasma protein binding: >99%.
Metabolism: Undergoes extensive hepatic first-pass metabolism by CYP3A4 enzyme.
Excretion: Via urine (approx 70% as metabolites), faeces (10%). Elimination half-life: 11-16 hours (immediate release).
Đặc tính

Chemical Structure Image
Felodipine

Source: National Center for Biotechnology Information. PubChem Database. Felodipine, CID=3333, https://pubchem.ncbi.nlm.nih.gov/compound/Felodipine (accessed on Jan. 20, 2020)

Bảo quản
Store below 30°C. Protect from light.
Phân loại ATC
C08CA02 - felodipine ; Belongs to the class of dihydropyridine derivative selective calcium-channel blockers with mainly vascular effects. Used in the treatment of cardiovascular diseases.
References
Anon. Felodipine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 01/04/2019.

Buckingham R (ed). Felodipine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/04/2019.

Felodipine (Glenmark Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 01/04/2019.

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