Nifedipine

Nifedipine Uses, Dosage, Side Effects, Food Interaction and all others data.

Nifedipine is an inhibitor of Calcium Channel Blocker that blocks the transmembrane influx of Calcium ions into muscle cells. Nifedipine has selective effects as a dilator of arterial vessels. Nifedipine dilates main coronary and systemic arteries. As a result blood pressure falls and this elicits a sympathetic reflex response causing tachycardia and an increased cardiac output. Pulmonary arterial pressure also falls. Nifedipine has direct negative inotropic effects on cardiac muscles and these effects are seen at higher doses than dose which causes arterial vasodilatation.

Nifedipine is an inhibitor of L-type voltage gated calcium channels that reduces blood pressure and increases oxygen supply to the heart. Immediate release nifedipine's duration of action requires dosing 3 times daily. Nifedipine dosing is generally 10-120mg daily. Patients should be counselled regarding the risk of excessive hypotension, angina, and myocardial infarction.

Trade Name Nifedipine
Availability Prescription only
Generic Nifedipine
Nifedipine Other Names Nifedipine, Nifedipino, Nifedipinum
Related Drugs amlodipine, aspirin, lisinopril, metoprolol, losartan, furosemide, carvedilol, hydrochlorothiazide, propranolol, spironolactone
Weight 10mg, , 20mg
Type Tablet
Formula C17H18N2O6
Weight Average: 346.3346
Monoisotopic: 346.116486318
Protein binding

Nifedipine is 92-98% protein bound in serum. Nifedipine is 97±12% bound in a 40g/L solution of pure albumin. Nifedipine is 51.4±5.9% protein bound in a 50mg/100mL solution of alpha-1-acid glycoprotein, and 75.5±3.5% protein bound in a 150mg/mL solution.

Groups Approved
Therapeutic Class Calcium-channel blockers
Manufacturer Zydus Cadila Healthcare Ltd, Albion Pharmaceuticals Ltd, Morningside Healthcare Ltd, Dexa Medica, Kimia Farma, Impulse Pharma Pvt Limited, Navketan Pharma Pvt Ltd
Available Country India, Bangladesh, United Kingdom, United States, Indonesia, Netherlands, Nigeria
Last Updated: September 19, 2023 at 7:00 am
Nifedipine
Nifedipine

Uses

Nifedipine is used for the management of all types of essential & renal hypertension. Also used for the management of hypertension during pregnancy & during coronary by pass surgery.

Nifedipine is also used for prophylaxis and the treatment of unstable & variant angina, myocardial infarction, and silent myocardial ischaemia. Moreover Nifedipine is also used in Raynaud's phenomenon & heart failure.

Nifedipine is also used to associated treatment for these conditions: Achalasia, Anal Fissures, Chronic Stable Angina Pectoris, High Blood Pressure (Hypertension), Hypertensive Emergency, Premature Labour, Proctalgia, Pulmonary Edemas, Pulmonary Hypertension (PH), Raynaud's Phenomenon, Ureteral Calculus, Vasospastic Angina

How Nifedipine works

Nifedipine blocks voltage gated L-type calcium channels in vascular smooth muscle and myocardial cells. This blockage prevents the entry of calcium ions into cells during depolarization, reducing peripheral arterial vascular resistance and dilating coronary arteries. These actions reduce blood pressure and increase the supply of oxygen to the heart, alleviating angina.

Dosage

Nifedipine dosage

Nifedipine 10 mg:

  • Angina: Initially 10 mg 3 times daily with food increased to 20 mg 3 times daily if necessary, in elderly patients, initially 5 mg 3 times daily.
  • Raynaud's Phenomenon: 10 mg 3 times daily; maximum 60 mg daily. In urgent cases, the tablet should be dissolved under the tongue like a sublingual tablet. The effect occurs within some minutes.

Nifedipine 20 mg: 

The starting dose for patients, not previously prescribed Nifedipine products is one tablet once daily. The recommended dose in hypertension and angina prophylaxis is 20 mg twice daily during or after food. Dosage may be adjusted within the range 10 mg twice daily to 40 mg twice daily.

Patients with liver dysfunction should commence therapy with 10 mg twice daily with careful monitoring. 

Patients with renal impairment do not require adjustment of dosage.

Side Effects

Headache, flushing, lethargy, gravitational oedema rash, nausea, increased frequency of micturation, eye pain, gum hyperplasia, depression, tremor, photosensitivity and few cases of jaundice have been reported. These reactions may regress on discontinuation of therapy. Its introduction may induce attacks of ischaemic pain in some patients with angina pectoris.

Toxicity

The oral LD50 in rats is 1022mg/kg and in mice is 202mg/kg.

Patients experiencing an overdose may present with hypotension, sinus node dysfunction, atrioventricular node dysfunction, and reflex tachycardia. Overdose may be managed by monitoring cardiovascular and respiratory function; elevating extremities; and administering vasopressors, fluids, and calcium infusions.

Precaution

Tablets should be swallowed whole and should not be bitten, chewed or broken up. It should be used with caution in patient whose cardiac reserve is poor. Should be withdrawn if ischaemic pain occurs or existing pain worsens shortly after initiating treatment. Use in diabetic patients requires adjustment of their control. Since the absorption of the drug could be modified by renal disease, caution should be exercised in treating such patients.

Interaction

  • ACE inhibitors: Enhanced hypotensive effect.
  • Anti-arrythmics: Plasma concentration of quinidine is reduced.
  • Anti-bacterials: Rifampicin possibly increases metabolism of Nifedipine.
  • Anti-epileptics: Plasma concentration of phenytoin increases.
  • Antipsychotics: Enhanced hypotensive effect.
  • β-blockers: Occasionally severe hypotension and heart failure may occur.
  • Cyclosporin: Plasma concentration of Nifedipine possibly increases.
  • Muscle relaxants: Effect of muscle relaxants e.g. tubocurarine increases.
  • Ulcer healing drugs: Metabolism of Nifedipine increases.

Food Interaction

  • Avoid excessive or chronic alcohol consumption.
  • Avoid grapefruit products. Grapefruit down-regulates post-translational expression of CYP3A4, the major metabolizing enzyme of nifedipine. Grapefruit, in all forms (e.g. whole fruit, juice and rind), can significantly increase serum levels of nifedipine and may cause toxicity. Avoid grapefruit products while on this medication.
  • Avoid natural licorice.
  • Take with or without food.

[Moderate] GENERALLY AVOID: The consumption of grapefruit juice may be associated with significantly increased plasma concentrations of some calcium channel blockers (CCBs) when they are administered orally.

The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit.

The interaction has been reported with the dihydropyridine CCBs (in roughly decreasing order of magnitude) felodipine, nisoldipine, nifedipine, and nimodipine, often with a high degree of interindividual variability.

Grapefruit juice caused more than twofold increases in felodipine, nifedipine, and nisoldipine AUCs.



MANAGEMENT: The manufacturers of nifedipine and nisoldipine recommend avoiding grapefruit juice.

Patients treated orally with other calcium channel blockers should be advised to avoid consumption of large amounts of grapefruits and grapefruit juice to prevent any undue fluctuations in serum drug levels.

Increased effects on blood pressure may persist for up to 4 days after the consumption of grapefruit juice.

Monitoring for calcium channel blocker adverse effects (e.g., headache, hypotension, syncope, tachycardia, edema) is recommended.

Nifedipine Hypertension interaction

[Major] For the long-term treatment of hypertension, only the extended-release formulations of nifedipine should be used.

The US National Heart, Lung, and Blood Institute and the FDA Cardiovascular and Renal Drug Advisory Committee have issued warnings against the use of immediate-release nifedipine for this purpose based on review of three epidemiologic studies of patients with hypertension and unstable angina who were treated with calcium channel blockers (CCBs) and at least two meta-analyses of randomized, controlled trials that included patients receiving CCBs.

Two of the case-control studies found an increased risk of myocardial infarction (MI) in patients taking immediate-release nifedipine, although the third did not. The use of immediate-release nifedipine (orally or sublingually) is also contraindicated for acute reduction of blood pressure.

Profound hypotension, acute myocardial infarction, and deaths have been reported when nifedipine was used in this manner.

Nifedipine multivitamins interaction

[Moderate] Calcium-containing products may decrease the effectiveness of calcium channel blockers by saturating calcium channels with calcium.

Calcium chloride has been used to manage acute severe verapamil toxicity.

Management consists of monitoring the effectiveness of calcium channel blocker therapy during coadministration with calcium products.

Volume of Distribution

The steady state volume of distribution of nifedipine is 0.62-0.77L/kg and the volume of distribution of the central compartment is 0.25-0.29L/kg.

Elimination Route

Sublingual dosing leads to a Cmax of 10ng/mL, with a Tmax of 50min, and an AUC of 25ng*h/mL. Oral dosing leads to a Cmax of 82ng/mL, with a Tmax of 28min, and an AUC of 152ng*h/mL.

Nifedipine is a Biopharmaceutics Classification System Class II drug, meaning it has low solubility and high intestinal permeability. It is almost completely absorbed in the gastrointestinal tract but has a bioavilability of 45-68%, partly due to first pass metabolism.

Half Life

The terminal elimination half life of nifedipine is approximately 2 hours.

Clearance

The total body clearance of nifedipine is 450-700mL/min.

Elimination Route

Nifedipine is 60-80% recovered in the urine as inactive water soluble metabolites, and the rest is eliminated in the feces as metabolites.

Pregnancy & Breastfeeding use

There are no adequate and well controlled studies in pregnant women. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Contraindication

Cardiogenic shock, advanced aortic stenosis, nursing mothers, GI obstruction, inflammatory bowel disease, hypotension.

Storage Condition

Protect from strong light, store in a cool place in the original pack

Innovators Monograph

You find simplified version here Nifedipine

Nifedipine contains Nifedipine see full prescribing information from innovator Nifedipine Monograph, Nifedipine MSDS, Nifedipine FDA label

FAQ

What is Nifedipine used for?

Nifedipine is a calcium channel blocker medication used to manage angina, high blood pressure, Raynaud's phenomenon, and premature labor. It is one of the treatments of choice for Prinzmetal angina. It may be used to treat severe high blood pressure in pregnancy.

How safe is Nifedipine ?

Nifedipine is generally safe to take for a long time. In fact, it works best when you take it for a long time.

How does Nifedipine work?

Nifedipine works by blocking calcium going into muscles in the heart and blood vessels.

What are the common side effects of Nifedipine?

The most common side effects include headache, flushing, constipation, feeling tired and swollen ankles. These usually improve after a few days of treatment.

Is Nifedipine safe during pregnancy?

Nifedipine are safe for use in pregnancy.

Is Nifedipine safe during breastfeeding?

Nifedipine passes into breast milk in amounts that are probably too small to be harmful to a nursing infant. It's generally considered OK to breastfeed while taking Nifedipine.

Can I drink alcohol with Nifedipine?

Yes, you can drink alcohol with Nifedipine. However, drinking alcohol can increase the blood pressure-lowering effect of Nifedipine, which can make you feel dizzy or light-headed.

Can I drive after taking Nifedipine?

As Nifedipine can occasionally make some people feel dizzy or weary you should make sure you know how you react to it before driving or operating machinery. Avoid doing these potentially hazardous activities if affected.

When should be taken of Nifedipine?

The extended-release tablet should be taken once daily on an empty stomach, either 1 hour before or 2 hours after a meal. To help you remember to take Nifedipine, take it at around the same time(s) every day.

How often can I take Nifedipine?

The capsule is usually taken three or four times a day.

How long does Nifedipine take to work?

Nifedipine is quickly absorbed when taken orally and peak blood levels occur in approximately 30 minutes.

How long does Nifedipine stay in my system?

The elimination half-life of Nifedipine is approximately two hours.

Can I take Nifedipine for a long time?

Nifedipine oral tablet is used for long-term treatment.

How long can I take Nifedipine?

Your doctor will probably start you on a low dose of Nifedipine and gradually increase your dose, generally once every 7 to 14 days.

What happens if I miss a dose?

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

Who should not take Nifedipine?

You should not take Nifedipine if you have follwing problem of below:

  • porphyria.
  • myasthenia gravis, a skeletal muscle disorder.
  • a sudden worsening of angina called acute coronary syndrome.
  • severe narrowing of the aortic heart valve.
  • severe heart failure.
  • low blood pressure.
  • significantly low blood pressure.
  • hardening of the liver

When is Nifedipine contraindicated?

Nifedipine is a dihydropyridine calcium-channel blocker and is contraindicated in patients with known serious dihydropyridine hypersensitivity.

What happen If I stop taking Nifedipine?

Talk to your doctor if you want to stop taking Nifedipine. Stopping Nifedipine may cause your blood pressure to rise and this may increase your risk of heart attack and stroke.

Can Nifedipine affects my heart ?

Nifedipine retard increased the heart rate of patients with ischemic heart disease only during the day and reduced parasympathetic activity.

Can Nifedipine affect my kidneys?

If it continues for a long time, the heart and arteries may not function properly. This can damage the blood vessels of the brain, heart, and kidneys, resulting in a stroke, heart failure, or kidney failure

Can Nifedipine affects my liver ?

The severity of liver injury from Nifedipine ranges from mild and transient serum enzyme elevations to self-limited jaundice to an alcoholic hepatitis-like syndrome. Complete recovery is expected after stopping the drug and recovery is usually rapid.

Will Nifedipine affect my fertility?

There's no clear evidence to suggest that taking Nifedipine will reduce fertility in either men or women.

*** Taking medicines without doctor's advice can cause long-term problems.
Share