Nifedipine

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trade names: Procardia, Procardia XL; drug class: calcium channel blocker; action: inhibits calcium ion influx across cell membrane during cardiac depolarization; produces relaxation of coronary vascular smooth muscle, dilates coronary arteries; increases myocardial oxygen delivery in patients with vasospastic angina; dilates peripheral arteries; uses: chronic stable angina pectoris, vasospastic angina, hypertension.

Brand names: Adalat®Adalat® CCAfeditab™ CRNifediac™ CCNifedical™ XLProcardia XL®Procardia®

Chemical formula:

Drug Forms:
• Nifedipine Oral tablet, extended-release (below)
• Nifedipine Oral capsule

Español:
• Nifedipina, Tableta oral de liberación prolongada
• Nifedipina, Cápsula oral

Nifedipine Oral tablet, extended-release

What is this medicine?

NIFEDIPINE is a calcium-channel blocker. It affects the amount of calcium found in your heart and muscle cells. This relaxes your blood vessels, which can reduce the amount of work the heart has to do. This medicine is used to treat high blood pressure and chest pain caused by angina.

This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
•heart problems, low blood pressure, slow or irregular heartbeat
•kidney disease
•liver disease
•previous heart attack
•an unusual or allergic reaction to nifedipine, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding

How should I use this medicine?

Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. Do not cut, crush or chew. Take your doses at regular intervals. Do not take your medicine more often then directed. Do not suddenly stop taking this medicine. Your doctor will tell you how much medicine to take. If your doctor wants you to stop the medicine, the dose will be slowly lowered over time to avoid any side effects.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What may interact with this medicine?

•barbiturates, like phenobarbital
•cimetidine
•diuretics
•grapefruit juice
•local or general anesthetics
•medicines for high blood pressure or heart problems
•warfarin

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Visit your doctor or health care professional for regular check ups. Check your blood pressure and pulse rate regularly. Ask your doctor or health care professional what your blood pressure and pulse rate should be and when you should contact him or her.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol may interfere with the effect of this medicine. Avoid alcoholic drinks.

If you are taking Procardia XL, you may notice the empty shell of the tablet in your stool.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
•blood in the urine
•difficulty breathing
•fast heartbeat, palpitations, irregular heartbeat, chest pain
•redness, blistering, peeling or loosening of the skin, including inside the mouth
•reduced amount of urine passed
•skin rash
•swelling of the legs and ankles

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•constipation
•facial flushing
•headache
•weakness or tiredness

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store at room temperature below 30 degrees C (86 degrees F). Protect from moisture and humidity. Keep container tightly closed. Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

A calcium channel blocker used principally as a vasodilator.

Nifedipine
Systematic (IUPAC) name
3,5-dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
Identifiers
CAS number	21829-25-4
ATC code	C08CA05
PubChem	4485
DrugBank	APRD00590
ChemSpider	4330
Chemical data
Formula	C17H18N2O6
Mol. mass	346.335 g/mol
Physical data
Melt. point	173 °C (343 °F)
Pharmacokinetic data
Bioavailability	45-56%
Protein binding	92-98%
Metabolism	Gastrointestinal, Hepatic
Half life	2 hours
Excretion	Renal: >50%, Biliary: 5-15%
Therapeutic considerations
Pregnancy cat.	C: (USA)
Legal status
Routes	Oral

Nifedipine (brand name Adalat, Nifedical, and Procardia) is a dihydropyridine calcium channel blocker. Its main uses are as an antianginal (especially in Prinzmetal's angina) and antihypertensive, although a large number of other uses have recently been found for this agent, such as Raynaud's phenomenon, premature labor, and painful spasms of the esophagus in cancer and tetanus patients. It is also commonly used for the small subset of pulmonary hypertension patients whose symptoms respond to calcium channel blockers.

Contents 1 Dosing 2 Uses 2.1 Approved uses 2.2 Off-label uses 3 History 4 References 5 External links

Dosing

Nifedipine rapidly lowers blood pressure, and patients are commonly warned they may feel dizzy or faint after taking the first few doses. Tachycardia (fast heart rate) may occur as a reaction. These problems are much less frequent in the sustained-release preparations of nifedipine (such as Adalat OROS). A more novel release system is GITS (Gastro-Intestinal Therapeutic System), which - according to Bayer - provides 24-hour continuous release through an osmotic push system. Recent trials with GITS include INSIGHT (for blood pressure)^[1] and ACTION (for angina).^[2]

Extended release formulations of nifedipine should be taken on an empty stomach, and patients are warned not to consume anything containing grapefruit or grapefruit juice, as they raise blood nifedipine levels. There are several possible mechanisms, including the lowering of CYP3A4 activity.^[3]

Uses

Approved uses

The approved uses for nifedipine are the long-term treatment of hypertension (high blood pressure) and angina pectoris. In hypertension, recent clinical guidelines generally favour diuretics and ACE inhibitors, although calcium channel antagonists are still favoured as primary treatment for older black patients.^[4]

Sublingual nifedipine has previously been used in hypertensive emergencies. This was found to be dangerous, and has been abandoned.^[5][6]

Off-label uses

Nifedipine has been used frequently as a tocolytic (agent that delays premature labor). A Cochrane review has concluded that it is comparable with magnesium sulfate and beta-agonists (such as ritodrine) with fewer side-effects.^[7] Its role vis à vis atosiban is not established.

Raynaud's phenomenon is often treated with nifedipine. A 2005 meta-analysis showed modest benefits (33% decrease in attack severity, 2.8-5 reduction in absolute number of attacks per week); it does conclude that most included studies used low doses of nifedipine.^[8]

Topical nifedipine has been shown to be as effective as topical nitrates for anal fissures.^[9]

Nifedipine is also used in high-altitude medicine to treat high altitude pulmonary edema.^[10]

History

Nifedipine (initially BAY a1040) was developed by the German pharmaceutical company Bayer, with most initial studies being performed in the early 1970s.^[11]

The use of nifedipine and related calcium channel antagonists was much reduced in response to 1995 trials that mortality was increased in patients with coronary artery disease who took nifedipine.^[12] This study was a meta-analysis, and demonstrated harm mainly in short-acting forms of nifedipine (that could cause large fluctations in blood pressure) and at high doses of 80 mg a day and more.^[13]

References

1. ^ Brown MJ, Palmer CR, Castaigne A, et al. (2000). "Morbidity and mortality in patients randomised to double-blind treatment with a long-acting calcium-channel blocker or diuretic in the International Nifedipine GITS study: Intervention as a Goal in Hypertension Treatment (INSIGHT)". Lancet 356 (9227): 366–72. doi:10.1016/S0140-6736(00)02527-7. PMID 10972368. 
2. ^ Poole-Wilson PA, Kirwan BA, Vokó Z, de Brouwer S, van Dalen FJ, Lubsen J (2006). "Safety of nifedipine GITS in stable angina: the ACTION trial". Cardiovas Drugs Ther 20 (1): 45–54. doi:10.1007/s10557-006-6312-4. PMID 16552473. 
3. ^ Odou P, Ferrari N, Barthélémy C, et al. (2005). "Grapefruit juice-nifedipine interaction: possible involvement of several mechanisms". Journal Clinical Pharm Ther 30 (2): 153–8. doi:10.1111/j.1365-2710.2004.00618.x. PMID 15811168. 
4. ^ Hypertension: management of hypertension in adults in primary care. Clinical guideline CG34. National Institute for Health and Clinical Excellence (NICE), June 2006. Fulltext index. ISBN 1-86016-285-1.
5. ^ Grossman E, Messerli FH, Grodzicki T, Kowey P (1996). "Should a moratorium be placed on sublingual nifedipine capsules given for hypertensive emergencies and pseudoemergencies?". JAMA 276 (16): 1328–31. doi:10.1001/jama.276.16.1328. PMID 8861992. 
6. ^ Varon J, Marik PE (2003). "Clinical review: the management of hypertensive crises". Critical care (London, England) 7 (5): 374–84. doi:10.1186/cc2351. PMID 12974970. 
7. ^ King JF, Flenady VJ, Papatsonis DN, Dekker GA, Carbonne B (2003). "Calcium channel blockers for inhibiting preterm labour". Cochrane database of systematic reviews (Online) (1): CD002255. doi:10.1002/14651858.CD002255. PMID 12535434. 
8. ^ Thompson AE, Pope JE (2005). "Calcium channel blockers for primary Raynaud's phenomenon: a meta-analysis". Rheumatology (Oxford, England) 44 (2): 145–50. doi:10.1093/rheumatology/keh390. PMID 15546967. 
9. ^ Ezri T, Susmallian S (2003). "Topical nifedipine vs. topical glyceryl trinitrate for treatment of chronic anal fissure". Dis. Colon Rectum 46 (6): 805–8. doi:10.1097/01.DCR.0000070044.62336.1D (inactive 2008-06-21). PMID 12794583. 
10. ^ Ali, Mir Omar and Qazi, Samia (2007-09-19). "Pulmonary Edema, High-Altitude". eMedicine. http://www.emedicine.com/med/topic1956.htm. Retrieved on 2007-11-25. 
11. ^ Vater W, Kroneberg G, Hoffmeister F, et al. (1972). "[Pharmacology of 4-(2'-nitrophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid dimethyl ester (Nifedipine, BAY a 1040)]" (in German). Arzneimittel-Forschung 22 (1): 1–14. PMID 4622472. 
12. ^ Furberg CD, Psaty BM, Meyer JV (1995). "Nifedipine. Dose-related increase in mortality in patients with coronary heart disease". Circulation 92 (5): 1326–31. PMID 7648682. 
13. ^ Opie LH, Messerli FH (1995). "Nifedipine and mortality. Grave defects in the dossier". Circulation 92 (5): 1068–73. PMID 7648646. 

External links

• Official site (Bayer)
• MedlinePlus DrugInfo medmaster-a684028

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