Nifedipine


Generic Medicine Info
Indications and Dosage
Oral
Prinzmetal's angina
Adult: As extended-release tab/cap: 10-40 mg bid or 30-90 mg once daily, depending on the preparation (refer to detailed product guideline). Dosage must be adjusted according to patient response.
Elderly: Dose reduction may be necessary.

Oral
Hypertension
Adult: As extended-release tab/cap: 10-40 mg bid or 20-90 mg once daily, depending on the preparation (refer to detailed product guideline). Dosage must be adjusted according to patient response.
Elderly: Dose reduction may be necessary.

Oral
Angina pectoris
Adult: Prophylaxis of chronic stable cases: Monotherapy or in combination with β-blockers: As extended-release tab/cap: 10-40 mg bid or 30-90 mg once daily, depending on the preparation (refer to detailed product guideline). Dosage must be adjusted according to patient response.
Elderly: Dose reduction may be necessary.

Oral
Raynaud's syndrome
Adult: As immediate-release softgel cap: Initially, 5 mg tid, may be adjusted according to patient response up to Max 20 mg tid.
Elderly: Dose reduction may be necessary.
Hepatic Impairment
Dose reduction may be necessary.
Administration
Immediate-Release: May be taken with or without food. Avoid grapefruit juice.
Contraindications
Cardiogenic shock, clinically significant aortic stenosis, unstable angina, during or within 1 month of MI, acute attacks of angina; secondary prevention of MI. Concomitant use with rifampicin.
Special Precautions
Patient with hypotension, poor cardiac reserve, heart failure, hypertrophic cardiomyopathy with outflow tract obstruction, diabetes mellitus; undergoing major surgery. Extended-release form: Patient with oesophageal obstruction, Kock pouch (ileostomy after proctocolectomy), inflammatory bowel disease, gastrointestinal strictures (e.g. severe gastrointestinal narrowing, obstruction, bowel resection, gastric bypass, colon cancer, vertical banded gastroplasty). Immediate-release preparations are not recommended to manage angina or hypertension. Avoid abrupt withdrawal. Hepatic impairment. Elderly. Pregnancy and lactation.
Adverse Reactions
Significant: Peripheral oedema, reflex tachycardia, increased angina or MI, cardiac ischaemic pain, symptomatic hypotension with or without syncope; impaired glucose tolerance. Rarely, bezoar formation (use of extended-release formulation in patients with gastrointestinal strictures).
Gastrointestinal disorders: Constipation, abdominal pain, dyspepsia, flatulence, dry mouth, nausea.
General disorders and administration site conditions: Feeling unwell, oedema, fatigue.
Musculoskeletal and connective tissue disorders: Muscle cramps.
Nervous system disorders: Headache, dizziness, tremors.
Psychiatric disorders: Nervousness, mood changes.
Respiratory, thoracic and mediastinal disorders: Nasal congestion, cough, wheezing, sore throat, dyspnoea.
Vascular disorders: Vasodilatation, flushing.
Patient Counseling Information
This drug may cause dizziness, lethargy, and transient blindness due to severe hypotension; if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor blood pressure, heart rate, LFTs; signs and symptoms of heart failure and peripheral oedema.
Overdosage
Symptoms: Hypotension, tachycardia, bradycardia, hyperglycaemia, metabolic acidosis, hypoxia, cardiogenic shock with pulmonary oedema, and disturbances of consciousness leading to coma. Management: Symptomatic and supportive treatment. Activated charcoal may be given if the ingestion of a potentially toxic amount is within 1 hour. Alternatively, gastric lavage may be considered in adults if potentially life-threatening overdose occurs within 1 hour. Treat hypotension as a result of cardiogenic shock and arterial vasodilatation with Ca (10-20 mL of a 10% Ca gluconate solution administered IV over 5-10 minutes). May continue treatment with ECG monitoring if the effects are inadequate. May administer vasoconstricting sympathomimetics (e.g. dopamine, norepinephrine) if an insufficient increase in blood pressure is achieved with Ca. Symptomatic bradycardia may be treated with atropine.
Drug Interactions
May cause additive hypotensive effects with IV Mg sulfate and other antihypertensive agents (e.g. β-blockers, ACE inhibitors, diuretics). Increased exposure and plasma concentration with erythromycin, ritonavir, ketoconazole, fluoxetine, nefazodone, quinupristin/dalfopristin, cisapride, valproic acid, cimetidine, diltiazem. May increase plasma levels of digoxin and tacrolimus. Decreased exposure with phenytoin, carbamazepine, phenobarbital. May reduce plasma concentrations of quinidine.
Potentially Fatal: Decreased bioavailability and efficacy with rifampicin.
Food Interaction
Avoid concomitant use with grapefruit or grapefruit juice as it increases plasma levels of nifedipine. May reduce serum levels with St. John’s wort. May elevate serum concentrations with alcohol. Food may decrease the rate but not the extent of absorption.
Lab Interference
May cause false-negative aldosterone/renin ratio (ARR) and falsely increase the spectrophotometric values of urinary vanillylmandelic acid. May lead to false-positive result when performing barium contrast x-ray.
Action
Description: Nifedipine, is a dihydropyridine Ca-channel blocker that prevents Ca ions from entering the slow channels or select voltage-sensitive areas of the vascular smooth muscle and myocardium during depolarisation, producing coronary vascular smooth muscle relaxation and coronary vasodilation. It also reduces peripheral and coronary vascular resistance, resulting in increased coronary blood flow, cardiac output and stroke volume while lowering afterload.
Onset: Immediate-release: Approx 20 minutes.
Pharmacokinetics:
Absorption: Rapidly and almost completely absorbed from the gastrointestinal tract. May decrease the rate but not the extent of absorption with food. Bioavailability: 40-77% (immediate-release); 65-89% (extended-release). Time to peak plasma concentration: 30-60 minutes (immediate-release).
Distribution: Crosses the placenta and enters breast milk. Plasma protein binding: Approx 92-98%.
Metabolism: Extensively oxidised in the liver by CYP3A4 isoenzyme into inactive metabolites. Undergoes extensive hepatic first-pass metabolism.
Excretion: Via urine (60-80% as inactive metabolites); faeces. Elimination half-life: Approx 2-5 hours.
Chemical Structure

Chemical Structure Image
Nifedipine

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 4485, Nifedipine. https://pubchem.ncbi.nlm.nih.gov/compound/Nifedipine. Accessed Dec. 21, 2020.

Storage
Store below 30°C. Protect from light and moisture.
MIMS Class
Anti-Anginal Drugs / Calcium Antagonists
ATC Classification
C08CA05 - nifedipine ; Belongs to the class of dihydropyridine derivative selective calcium-channel blockers with mainly vascular effects. Used in the treatment of cardiovascular diseases.
References
Adalat 5 mg Soft Capsules (Bayer plc). MHRA. https://products.mhra.gov.uk/. Accessed 03/08/2020.

Adalat LA 20 mg Prolonged-release Tablets (Bayer plc). MHRA. https://products.mhra.gov.uk/. Accessed 03/08/2020.

Adalat Retard 10 mg Modified-release Tablets (Bayer plc). MHRA. https://products.mhra.gov.uk/. Accessed 03/08/2020.

Adalat Retard Tablet (Bayer Co. [Malaysia] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 02/12/2020.

Anon. Nifedipine. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 04/08/2020.

Anon. Nifedipine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/08/2020.

Buckingham R (ed). Nifedipine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/08/2020.

Coracten SR Capsules 10 mg (UCB Pharma Limited). MHRA. https://products.mhra.gov.uk/. Accessed 03/08/2020.

Joint Formulary Committee. Nifedipine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/08/2020.

Nifecard XL (Sandoz). MIMS Hong Kong. http://www.mims.com/hongkong. Accessed 02/12/2020.

Procardia Capsule (Pfizer Laboratories Div Pfizer Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 03/08/2020.

Procardia XL Tablet, Film-coated, Extended Release (Pfizer Laboratories Div Pfizer Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 03/08/2020.

Tensipine MR 10, Tensipine MR 20 (Genus Pharmaceuticals Limited). MHRA. https://products.mhra.gov.uk/. Accessed 03/08/2020.

Valni 20 Retard (Tillomed Laboratories Ltd). MHRA. https://products.mhra.gov.uk/. Accessed 03/08/2020.

Disclaimer: This information is independently developed by MIMS based on Nifedipine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2021 MIMS. All rights reserved. Powered by MIMS.com
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