A-Z Drug Facts > Nifedipine

Nifedipine

Pronouncation: (nye-FED-ih-peen)
Class: Calcium channel blocking agent

Trade Names:
Adalat CC
- Tablets, extended-release 30 mg
- Tablets, extended-release 60 mg
- Tablets, extended-release 90 mg

Trade Names:
Afeditab CR
- Tablets, extended-release 30 mg
- Tablets, extended-release 60 mg

Trade Names:
Nifediac CC
- Tablets, extended-release 30 mg
- Tablets, extended-release 60 mg
- Tablets, extended-release 90 mg

Trade Names:
Nifedical XL
- Tablets, extended-release 30 mg
- Tablets, extended-release 60 mg

Trade Names:
Procardia
- Capsules 10 mg

Trade Names:
Procardia XL
- Tablets, extended-release 30 mg
- Tablets, extended-release 60 mg
- Tablets, extended-release 90 mg

Adalat XL (Canada)
Apo-Nifed (Canada)
Apo-Nifed PA (Canada)
Novo-Nifedin (Canada)
Nu-Nifed (Canada)
Nu-Nifedipine (Canada)

Pharmacology

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Inhibits movement of calcium ions across cell membrane in systemic and coronary vascular smooth muscle and myocardium. Decreases peripheral vascular resistance. Reduces myocardial oxygen demand; relaxes and prevents coronary artery spasm.

Pharmacokinetics

Absorption

Nifedipine is rapidly and fully absorbed (100%). T _max is about 30 min (immediate-release) and 2.5 to 5 h (extended-release). Bioavailability is 84% to 89% (extended-release) and 45% to 75% (immediate-release).

Distribution

Nifedipine protein binding is 92% to 98%.

Metabolism

Nifedipine is metabolized extensively in the liver to inactive metabolites.

Elimination

Nifedipine is eliminated in urine (0.1% unchanged) and in small amounts in feces. The t _½ is about 7 h (extended-release) and 2 h (immediate-release). 60% to 80% excreted in urine and the remainder in feces in metabolized form.

Special Populations

Hepatic Function Impairment

Longer t _½ , higher bioavailability, and reduced protein binding may occur in patients with liver cirrhosis.

Elderly

Mean C _max is 36% higher and plasma concentration is 70% greater in elderly patients.

Indications and Usage

Chronic stable angina (except Adalat CC , Afeditab CR , Nifediac CC ); vasospastic angina (except Adalat CC , Afeditab CR , Nifediac CC ); hypertension (except Procardia ).

Contraindications

Standard considerations.

Dosage and Administration

Capsules
Adults

PO Start with 10 mg 3 times daily and titrate dose over 7- to 14-day period (usual dose range, 10 to 20 mg 3 times daily). Some patients (eg, coronary artery spasm) respond only to higher doses and/or more frequent administration (eg, 20 to 30 mg 3 to 4 times daily; max, 180 mg/day). In hospitalized patient, under close observation, dose may be increased in 10 mg increments over 4- to 6-h periods as required to control pain and arrhythmias caused by ischemia. A single dose rarely exceeds 30 mg.

Extended-release tablets
Adults Procardia XL and Nifedical XL

PO 30 or 60 mg once daily, titrated over 7- to 14-day period (max, 120 mg/day). Administer on an empty stomach. Swallow whole. Do not crush, chew, cut, or break extended-release tablets.

Adalat CC , Afeditab CR , and Nifediac CC (hypertension)

PO Start with 30 mg once daily and titrate dose over 7- to 14-day period (max, 90 mg/day). Administer on an empty stomach. Swallow whole. Do not crush, chew, cut, or break extended-release tablets.

Storage/Stability

Store immediate-release capsules at controlled room temperature (59° to 77°F). Protect from light and moisture. Store extended-release tablets below 86°F). Protect from light, moisture, and freezing.

Drug Interactions

Acarbose

Coadministration may lead to loss of glucose control.

Anticoagulants (eg, warfarin)

May increase PT during coadministration.

Antiviral agents, azole antifungal agents, cisapride, diltiazem, erythromycin, nefazodone, quinupristin/dalfopristin, valproic acid, verapamil

May elevate nifedipine levels, increasing the risk of side effects.

Barbiturates, carbamazepine, nafcillin, rifampin, St. John's wort

May reduce nifedipine levels, decreasing the therapeutic effect.

Cimetidine

May increase bioavailability of nifedipine.

Digitalis

Reports are conflicting; however, digoxin levels may be increased.

Fentanyl, parenteral magnesium

Hypotension may occur.

Grapefruit juice

Nifedipine plasma levels may be elevated, increasing the pharmacologic and adverse reactions. Avoid coadministration.

Melatonin

May interfere with the antihypertensive effects of nifedipine.

Micafungin

Nifedipine plasma levels may be elevated by micafungin, increasing the pharmacologic and adverse reactions.

Phenytoin

Phenytoin plasma levels may be increased.

Quinidine

May decrease quinidine plasma levels during coadministration.

Tacrolimus

Tacrolimus trough concentrations may be elevated, increasing the risk of toxicity.

Other hypertensive agents

May have additive effects.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Peripheral edema (10%); palpitation (7%); transient hypotension (5%); asthenia, fatigue, insomnia (less than 3%).

CNS

Dizziness, lightheadedness, giddiness (27%); headache (23%); weakness (12%); nervousness, mood changes (7%); paresthesia, vertigo (3% or less); fatigue, asthenia, insomnia (less than 3%); shakiness, jitteriness, sleep disturbances, difficulty in balance, somnolence (2% or less).

Dermatologic

Rash, pruritis (3% or less); urticaria, sweating, dermatitis (2% or less); exfoliative or bullous skin reactions including erythema multiforme, Steven-Johnson syndrome, toxic epidermal necrolysis (postmarketing).

EENT

Nasal congestion, sore throat (6%); blurred vision, epistaxis, rhinitis (3% or less).

GI

Nausea, heartburn (11%); diarrhea, constipation, flatulence (3% or less); abdominal pain, dry mouth, dyspepsia (less than 3%); cramps (2% or less).

Genitourinary

Impotence, polyuria, urinary frequency (3% or less); sexual difficulties (2% or less).

Musculoskeletal

Muscle cramps, tremor (8%); arthralgia, leg cramps (3% or less); inflammation, joint stiffness (2% or less).

Respiratory

Dyspnea, cough, wheezing (6%); shortness of breath (2% or less).

Miscellaneous

Flushing/heat sensation (25%); pain (less than 3%); chills, fever (2% or less).

Precautions

Monitor Frequently assess patient for response to treatment. Ensure that therapy is periodically reviewed to determine if it needs to be continued without change or if a dose change (eg, increase, decrease, discontinuation) is indicated. Frequently monitor BP during initial administration and following any dose escalation.

Pregnancy

Category C .

Lactation

Excreted in breast milk.

Children

Safety and efficacy not established.

Elderly

May experience greater hypotensive effects.

Renal Function

Absorption of nifedipine from extended-released form could be modified by renal disease. Use with caution.

Hepatic Function

Use drug with caution in patients with impaired hepatic function, reduced hepatic blood flow, or hepatic cirrhosis.

Acute hepatic injury

In rare instances, nifedipine has been associated with significant elevations in liver enzymes, symptoms consistent with acute hepatic injury, cholestasis with or without jaundice and allergic hepatitis.

Antiplatelet effects

Nifedipine decreases platelet aggregation and can increase bleeding time in some patients.

Beta-blocker withdrawal

Patients withdrawn from beta-blockers while taking nifedipine may experience increased angina.

CHF

Use drug with caution in patients with CHF. New onset CHF and worsening of preexisting CHF have been reported, usually in patients also receiving a beta-blocker.

Discontinuation

Decrease dose gradually. Abrupt withdrawal may cause increased frequency and duration of angina.

Edema

Nifedipine has been associated with edema in some cases and should be distinguished from fluid retention secondary to heart failure.

Excessive hypotension

Excessive and poorly tolerated hypotension has occurred. This appears to occur during initial titration or during upward dosage adjustment and may be more common in patients with concurrent beta-blocker use.

Fentanyl anesthesia

Severe hypotension occurred in patients receiving immediate-release nifedipine together with a beta-blocker and who underwent coronary artery bypass surgery using high-dose fentanyl anesthesia. If possible, withdraw nifedipine 36 h before surgery when using high-dose fentanyl.

GI narrowing

Use extended-release nifedipine with caution in patient with severe GI narrowing. Obstructive symptoms have been rarely reported in patients with known strictures in association with ingestion of extended-release nifedipine.

Increased angina

Occasional patients may have increased frequency, duration, or severity of angina at start of therapy or when dose is increased. Sublingual nitroglycerin may be used to control acute angina episodes.

Interchangeability

Two 30 mg Afeditab and Nifediac CC tablets may be interchanged with one 60 mg Afeditab or Nifediac CC tablets. Three 30 mg tablets are not considered interchangeable with a single 90 mg tablet.

Myocardial infarction

Immediate-release nifedipine should not be used within the first 2 weeks following MI, and should be avoided in the setting of acute coronary syndrome.

Overdosage

Symptoms

Hypotension, nausea, dizziness, second- or third-degree AV block, marked and prolonged hypotension and bradycardia, functional rhythms, loss of consciousness, metabolic acidosis, hypoxia, cardiogenic shock with pulmonary edema, palpitations, flushing, nervousness, vomiting, generalized edema, ECG abnormalities.

Patient Information

• Notify health care provider if condition does not appear to be improving or is worsening, or if bothersome side effects are noted.
• Advise patient that dose of medication may be adjusted to obtain max benefit.
• Advise patient taking immediate-release capsules to take 3 to 4 times daily as prescribed. Advise patient to swallow whole, without regard to meals, and not to chew or puncture capsule. Advise patient to take with food if stomach upset occurs.
• Advise patient taking extended-release tablets to take once daily as prescribed, on an empty stomach. Caution patient to swallow extended-release tablets whole and not to crush, chew, cut, or break.
• Advise patient using extended-release tablets that empty tablets may be seen in the stool but that these are are the empty matrix that released the nifedipine for absorption. Advise patient not to be concerned as the active drug has already been absorbed.
• Advise patient to try to take each dose at about the same time each day.
• Inform patient that drug controls, but does not cure, hypertension or angina and to continue taking as prescribed even when BP is not elevated or angina symptoms are not present.
• Caution patient not to change the dose or stop taking unless advised by health care provider.
• Instruct patient to continue taking other BP or angina medications as prescribed by health care provider.
• Instruct patient being treated for angina to notify health care provider if frequency or severity of chest pain or need for sublingual nitroglycerin appears to be increasing.
• Instruct patient in BP and pulse measurement skills.
• Advise hypertensive patient to monitor and record BP and pulse at home and to inform health care provider if abnormal measurements are noted. Also advise patient to take record of BP and pulse to each follow-up visit.
• Instruct patient to lie or sit down if experiencing dizziness or lightheadedness when standing.
• Advise patient to notify health care provider if any of the following occur: frequent episodes of dizziness when arising; swelling of lower legs or ankles; persistent fatigue; or any other unusual or unexplained symptom or sign.
• Emphasize to hypertensive patient importance of other modalities on BP: weight control, regular exercise, smoking cessation, moderate intake of alcohol and salt.

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