Nifedipine

 

Generic name: nifedipine (nye FED i peen)

Brand name: Adalat CC, Afeditab CR, Nifediac CC, Nifedical XL, Procardia, Procardia XL, Adalat
Drug class: Calcium channel blocking agents

What is nifedipine?

Nifedipine is in a group of drugs called calcium channel blockers. It works by relaxing the muscles of your heart and blood vessels.

Nifedipine is used to treat hypertension (high blood pressure) and angina (chest pain).

Nifedipine may also be used for purposes not listed in this medication guide.

What is the most important information I should know about nifedipine?

You should not use nifedipine if you have severe coronary artery disease, or if you have had a heart attack within the past 2 weeks.

Before taking nifedipine, tell your doctor if you have kidney or liver disease, a blockage in your digestive tract (stomach or intestines), a history of stomach surgery, coronary artery disease, underactive thyroid, diabetes, or congestive heart failure.

If you need surgery, tell the surgeon ahead of time that you are using nifedipine. You may need to stop using the medicine for a short time.

Do not stop taking nifedipine without first talking to your doctor, even if you feel fine. Stopping suddenly may make your condition worse. High blood pressure often has no symptoms. You may need to use blood pressure medication for the rest of your life.

Nifedipine Uses

• Angina:

  • It is indicated for the treatment of chronic stable/vasospastic angina.

• Hypertension:

  • It is used for controlling blood pressure

• Off Label Use of Nifedipine in Adults:

  • Anal fissure
  • High-altitude pulmonary edema
  • Hypertensive emergency in pregnancy or postpartum (including acute-onset hypertension in preeclampsia and eclampsia)
  • Group 1 Pulmonary arterial hypertension
  • Raynaud phenomenon
  • Tocolysis

Nifedipine dosage in adults:

Note:

• Nifedipine sublingually is not recommended due to safety concerns.
• Dosage forms include immediate-release capsules (typically given thrice daily) and extended-release (ER) tablets (prescribed once daily).
• The dose remains unchanged when switching from immediate-release to extended-release form.

Nifedipine dose for the treatment of Anal fissure:

Note:

Topical application as a local vasodilator in addition to supportive measures. Ointment and gel are not commercially available and must be prepared by a licensed compounding facility.

• Intra-anal: 0.2% to 0.3% ointment or gel should be applied on or around fissures 2 to 4 times daily for one month.

Nifedipine treatment dose for the treatment of Angina pectoris:

• Chronic stable angina (alternative agent):

Note:

• If symptoms are not controlled with initial beta-blocker therapy, long-acting dihydropyridine calcium channel blocker (eg, nifedipine) may be added.
• Extended-release nifedipine is considered as an alternative therapy if there are contraindications to beta-blockers.
• Use of immediate-release nifedipine (oral /sublingual) is not usually prescribed due to increased adverse effects such as hypotension and reflex tachycardia particularly in absence of a beta-blocker.

• Extended-release nifedipine tablets:

  • The initial dose is 30 or 60 mg per oral once daily
  • The dose should be increased accordingly to an effective antianginal dose over 7-14 days.
  • Doses >90 mg/day are rarely required
  • The maximum dose is 120 mg/day per oral.

• Vasospastic angina:

Note: May be used as a single agent or concurrently with nitrates.

• Extended-release:

  • The dose is the same as for chronic stable angina.

Nifedipine dose for the treatment of High-altitude pulmonary edema (adjunctive therapy):

• For the prevention of high-altitude pulmonary edema:

Note: Adjunct to gradual ascent in higher-risk individuals (e.g. history of high altitude pulmonary edema or other predisposing factors).

• Extended-release:

  • 30 mg per oral every 12 hours starting 24 hours before the ascent.
  • It should be continued for 5 days after reaching maximal altitude.
  • The therapy can be extended beyond 5 days in high-risk circumstances (eg, descent impossible).

• For the Treatment of high-altitude pulmonary edema:

Note: Adjunctive therapy to nonpharmacologic measures such as oxygen supply/portable hyperbaric chamber/gradual descent to lower altitude or as a single agent if nonpharmacologic measures are not available.

• Extended-release:

  • 30 mg per oral every 12 hours.

Nifedipine dose for the treatment of Hypertension:

Note:

It can be used in combination with another agent such as ACE inhibitor, angiotensin receptor blocking agents or thiazide diuretic for initial treatment when blood pressure ≥20/10 mmHg above goal.

For patients <20/10 mm Hg above goal, it can be given as a single agent, however, over time, many patients will need combination therapy.

•  Extended-release formulation:

  • The initial dose is 30 or 60 mg per oral once daily.
  • The dose should be increased dose based on response and tolerability every 7-14 days.
  • The usual dosage range is 30 to 90 mg once daily.

Nifedipine dose for the treatment of Hypertensive emergency in pregnancy or postpartum (including acute-onset hypertension in preeclampsia/ eclampsia):

• Extended-release:

  • The initial dose of 30 mg per oral repeat 30 mg after 1 to 2 hours if target blood pressure is not achieved.
  • If the systolic and diastolic blood pressure remains above the threshold after the second dose, another class of agents should be considered.

• Immediate-release (alternative agent):

Note:

Generally reserved for use when intravenous access is not available.

Some experts avoid the use of immediate-release formulations as it can result in dropping blood pressure in some women.

Do not puncture capsule or give sublingually.

• • The initial dose of 10 mg per oral once with fetal heart rate monitoring.
  • If systolic or diastolic blood pressure remains above target at 20 minutes, another dose of 10 or 20 mg per oral should be given depending on the initial response.
  • If blood pressure remains above target after 40 minutes, give another dose of 10 or 20 mg depending on the previous response.
  • If target blood pressure is not achieved after three doses, another class of agents should be considered.

Nifedipine dose for the treatment of Group 1 Pulmonary arterial hypertension:

Note:

It is only recommended for rigorously selected group 1 pulmonary arterial hypertension patients having a positive vasodilator testing and under the care of a pulmonary hypertension specialist.

European guidelines recommend a 12-hour, sustained-release formulation that is not available in the United States.

Dosing is provided empirically for the extended-release formulation.

• Extended-release formulation:

  • 60 mg per oral every 2 hours.
  • Titrate gradually and with close hemodynamic monitoring
  • The reported dose range is 120 to 240 mg/day per oral.
  • Some experts initiate therapy at 30 mg per oral once daily.

Nifedipine dose for the treatment of Raynaud phenomenon:

• Extended-release:

  • The initial dose of  30 mg per oral once daily
  • The dose may be increased gradually once every month if required, but not more frequently than once every 7 to 10 days.
  • Close BP monitoring with each dose increase should be done
  • The usual effective dose: 30 to 120 mg/day.

• Immediate release:

Note:

Only for short-term use in closely monitored hospitalized patients with severe digital ischemia who haven”t received first-line therapy.

• • The initial dose of 10 mg per oral thrice daily titrated by 10 mg increments every 4 to 6 hours if required up to 30 mg thrice daily, a transition to an extended-release formulation for maintenance therapy.

Nifedipine treatment dose as a tocolytic agent:

• Immediate-release:

  • An initial dose of 20 to 30 mg as a loading dose, followed by 10 to 20 mg every 3 to 8 hours for up to 48 hours.
  • The maximum dose is 180 mg/day.

 

Nifedipine dosage in children:

Nifedipine dose for the treatment of severe Hypertension:

Note:

It should be used under the supervision of a specialist for pediatric hypertension in the inpatient tertiary setting and used only after other drugs are ineffective.

Current pediatric blood pressure guidelines do not recommend nifedipine for the management of acute severe hypertension, as other safe/ effective drugs are available for instance hydralazine and isradipine.

• Immediate-release tablets in Children and Adolescents:

  • Oral dose of 0.04 to 0.25 mg/kg.
  • The maximum single dose is 10 mg/dose.
  • The dose may be repeated if required every 4 to 6 hours to the maximum daily dose of 1 to 2 mg/kg/day with careful monitoring.

Nifedipine dose for the chronic treatment of Hypertension:

• Children and Adolescents who are able to swallow the whole tablet:

  • Extended-release:

    • The initial dose of 0.25 to 0.5 mg/kg once daily or divided into 2 doses every 12 hours.
    • The initial adult daily dose should not exceed 30 to 60 mg/day titrated to an effective dose.
    • The maximum daily dose is 3 mg/kg/day up to 120 mg/day.
    • Some centers use a higher maximum dose: 3 mg/kg/day up to 180 mg/day.

Note: Doses are usually titrated upward over one to two weeks may increase over 3 days if clinically necessary.

Nifedipine (Procardia, Adalat) dose for the treatment of High altitude pulmonary edema in children and adolescents:

Note: Treatment with Nifedipine should be considered for an unsatisfactory response to oxygen and/or altitude descent

• Immediate-release formulation:

  • 5 mg/kg/dose per oral every 8 hours
  • The maximum dose is 20 mg/dose

• Extended-release (preferred):

  • 5 mg/kg/day per oral given once daily or divided into 2 doses per day
  • The maximum dose is 40 mg/dose.
  • The usual adult dose is 30 mg every 12 hours.

 

Pregnancy Risk Category: C

• Nifedipine can cross the placenta.
• It can increase perinatal asphyxia and C-section, prematurity, intrauterine growth retardation, and perinatal asphyxia.
• Actual fetal/neonatal risk depends on how severe and long-lasting maternal hypertension is.
• Untreated hypertension may increase the risk of gestational diabetes and other complications such as MI, preeclampsia or stroke.
• Oral nifedipine, one of the most preferred treatments for chronic antenatal hypertension, is also available.
• For the treatment of severe, acute-onset hypertension in pregnant or postpartum women (including those with preeclampsia and eclampsia), oral immediate-release nifedipine can also be recommended.
• Preterm labor can be treated with Nifedipine.
• Tocolytics can be used to prolong pregnancy for a short time (48 hours) to allow for administration of antenatal steroids. They should not be administered before fetal viability, or when the risk to the mother or foetus is greater than the risk to preterm birth.
• For the maintenance of tocolytic treatment, Nifedipine will not be effective.

Nifedipine use during breastfeeding:

• Breast milk contains Nifedipine.
• According to the manufacturer the decision to continue breastfeeding while on therapy is based on the risks of infant exposure/the benefits to breastfeeding and the benefits to the mother.
• The Academy of Breastfeeding Medicine recommends that nifedipine be used to treat Raynaud phenomenon of nipple in breastfeeding mothers.

 

Nifedipine dose adjustment in renal disease:

There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied).

The pharmacokinetics of nifedipine is not significantly influenced by the degree of renal impairment (only trace amounts of unchanged drug are found in urine).

Hemodialysis and peritoneal dialysis:

The supplemental dose is not necessary.

 

Nifedipine dose adjustment in liver disease:

There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied).

Use with caution. The clearance of nifedipine is decreased in cirrhosis, which may lead to increased systemic exposure.

Close monitoring for adverse effects/toxicity and dose adjustments should be done.

 

Common Side Effects of Nifedipine:

• Cardiovascular:

  • Flushing
  • Peripheral Edema

• Central Nervous System:

  • Dizziness
  • Headache

• Gastrointestinal:

  • Heartburn
  • Nausea

Side Effects of Nifedipine (Uncommon):

• Cardiovascular:

  • Palpitations
  • Transient Hypotension
  • Cardiac Failure

• Central Nervous System:

  • Mood Changes
  • Nervousness
  • Fatigue
  • Chills
  • Disturbed Sleep
  • Equilibrium Disturbance
  • Jitteriness
  • Shakiness

• Dermatologic:

  • Dermatitis
  • Diaphoresis
  • Pruritus
  • Urticaria

• Gastrointestinal:

  • Gingival Hyperplasia
  • Sore Throat
  • Abdominal Cramps
  • Constipation
  • Diarrhea
  • Flatulence

• Genitourinary:

  • Sexual Difficulty

• Neuromuscular & Skeletal:

  • Muscle Cramps
  • Tremor
  • Weakness
  • Joint Stiffness

• Ophthalmic:

  • Blurred Vision

• Respiratory:

  • Cough
  • Nasal Congestion
  • Wheezing
  • Chest Congestion
  • Dyspnea

• Miscellaneous:

  • Fever
  • Inflammation

 

Contraindication to Nifedipine (Adalat, Procardia):

• • • Contraindications include hypersensitivity to nifedipine or any component of the formulation, hypersensitivity to other dihydropyridine calcium antagonists/concurrent use with rifampicin.

Not recommended for patients suffering from ST-elevation myocardial Infarction.

• • • Heart attack/ severe hypotension

Notice: The SOGC and ACOG guidelines recommend that nifedipine be used as a preferred agent to treat maternal hypertension (Extended release only).

• • • Kock pouch (ileostomy following a proctocolectomy).
    • Moderate or severe liver impairment, severe intestinal obstruction disorders.

Warnings and precautions

• • Angina or MI

    • Reflex tachycardia can occur when patients have dihydropyridine calciumchannel blockers. This is especially true if there are no concurrent beta-blockers.
    • Patients with unstable angina/nonST elevation myocardial injury should not be prescribed immediate-release nifedipine, except in combination with beta-blockade

  • Syncope and hypotension:

    • It is rare to have hypotension symptoms with or without syncope. The patient’s clinical condition dictates that blood pressure be maintained at a level appropriate to their needs.
    • In hypertensive situations, immediate-release nifedipine can cause serious adverse events, including death, cerebrovascular infarction, stroke, syncope, hypotension, acute myocardial injury, and fetal distress.
    • In acute blood pressure reduction, it is best to avoid immediate-release nifedipine.
    • There are guidelines for when immediate-release, nifedipine must be used to treat acute conditions in pregnant or postpartum mothers.

  • Peripheral edema

    • Peripheral edema is the most common side effect within 2 to 3 week of starting therapy.

  • Aortic stenosis

    • Nifedipine can reduce coronary perfusion, resulting in myocardial infarction in aortic narrowing.

  • Restrictions on GI:

    • Extended-release nifedipine can cause bezoar formation when there are alterations to the gastrointestinal anatomy (e.g., severe GI narrowing, GI Malignancy, obstruction, bowel resection), and underlying hypomotility disorders.

  • Heart failure:

    • According to the ACC/AHA guidelines for heart failure, patients with heart disease should not use calcium channel blockers. This is because they are likely to have worse outcomes and/or no benefit.

  • Hypertrophic cardiomyopathy with outflow tract obstruction (HCM)

    • Patients with hypertrophic cardiomyopathy or outflow tract obstruction should be cautious. Reduced afterload could worsen the symptoms.

 

Monitoring parameters:

These include pulse, Blood pressure, signs, and symptoms of heart failure, and peripheral edema.

Hypertension:

The 2017 Guideline for the Prevention, Detection, Evaluation, and Management of High Blood Pressure in Adults.

Confirmed hypertension and known CVD (cardiovascular disease) or 10-year atherosclerotic cardiovascular disease (ASCVD) risk ≥10%:

• Target blood pressure <130/80 mm Hg is recommended

Confirmed hypertension without markers of increased ASCVD risk:

• Target blood pressure <130/80 mm Hg may be reasonable

Diabetes and hypertension:

• Patients 18 to 65 years of age, without ASCVD, and 10-year ASCVD risk <15%:

  • Target blood pressure <140/90 mm Hg is recommended

• Patients 18 to 65 years of age and known ASCVD or 10-year ASCVD risk >15%:

  • Target blood pressure <130/80 mm Hg may be appropriate if it can be safely attained

• Patients >65 years of age (healthy or complex/intermediate health):

  • Target blood pressure <140/90 mm Hg is recommended

• Patients >65 years of age (very complex/poor health):

  • Target blood pressure <150/90 mm Hg is recommended

 

How to administer Nifedipine (Procardia, Adalat)?

Immediate-release formulation:

In general, it may be given orally with or without food.

Extended-release formulation:

Tablets should be swallowed whole without crushing, splitting, or chewing.

Adalat CC, Afeditab CR:

Administer on an empty stomach (per manufacturer).

Other extended-release products may not have this recommendation.

Consult product labeling.

 

Nifedipine (Procardia, Adalat) Mechanism of action:

During depolarization, the nifedipine inhibits calcium ion’s entry to the “slow channel” or selected voltage-sensitive areas in vascular smooth muscles and myocardium. This results in relaxation of coronary smooth muscle and coronary vasodilation.

Patients with vasospastic and reduced peripheral resistance have higher myocardial oxygen delivery, which leads to lower arterial blood pressure.

The onset of action of the Immediate-release tablets is about 20 minutes

Protein binding (concentration-dependent): 92% to 98%. Note: Protein-binding may be significantly decreased in patients with renal or hepatic impairment.

Metabolism: Hepatic via CYP3A4 to inactive metabolites.

Bioavailability:

• Capsule: 40% to 77%;
• Extended-release: 65% to 89% relative to immediate-release capsules;
• The bioavailability is increased with significant hepatic disease

Half-life elimination in healthy adults: 2 to 5 hours, in cirrhosis: 7 hours, and in the elderly: 7 hours (extended-release tablet)

Excretion: Urine (60% to 80% as inactive metabolites); feces

 

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.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What should I avoid?

Grapefruit and grapefruit juice may interact with nifedipine and lead to unwanted side effects. Discuss the use of grapefruit products with your doctor.

Avoid getting up too fast from a sitting or lying position, or you may feel dizzy. Get up slowly and steady yourself to prevent a fall.

Nifedipine Brand Names (International):

• Adalat CC
• Afeditab CR
• Nifedical XL
• Procardia
• Procardia XL
• Adalat XL
• APO-Nifed PA
• DOM-NIFEdipine
• MYLAN-NIFEdipine
• PMS-NIFEdipine
• PMSNIFEdipine ER Adalat
• Adalat 10
• Adalat 20
• Adalat CC
• Adalat CR
• Adalat Crono
• Adalat GITS
• Adalat GITS 30
• Adalat L
• Adalat LA
• Adalat LP
• Adalat Oros
• Adalat Retard
• Adalat XL
• Adalate
• Addos XR
• Adefin
• Adefin XL
• Adifen SR
• Adipine XL
• Alonix-S
• Altapres
• Ampine
• Aprical
• Atanaal Softcap
• Calcibloc
• Calcibloc OD
• Calcicor
• Calcigard
• Calcigard Retard
• Cardifen
• Cardiiopine
• Chronadalate LP
• Citilat
• Coracten
• Coral
• Cordaflex
• Cordilat
• Cordipen
• Cordipen Retard
• Cordipin
• Cordipin Retard
• Cordipin XL
• Corinfar
• Corinfar Retard
• Corotrend
• Depin
• Depin-E Retard
• Dignokonstant
• Dipinkor
• Duranifin
• Ecodipin
• Epilat
• Fenamon
• Glopir
• Hexadilat
• Huma-Nifedin
• Hypan
• Jutadilat
• Kin Ran
• Myogard
• Nedipin
• Nelapine
• Nepin SR
• Nicardia
• Nicardia CD
• Nicardia Retard
• Nicardia XL
• Nidipin
• Nifa
• Nifadil
• Nifangin
• Nifar
• Nifar-GB
• Nifdemin
• Nifebene
• Nifecap
• Nifecard
• Nifecard XL
• Nifecor
• Nifedepat
• Nifedicor
• Nifedigel
• NIfedilat
• Nifedilong
• Nifedin
• Nifedine
• Nifedipin
• Nifedipin AL
• Nifedipin Pharmavit
• Nifedipin Stada
• Nifedipin-ratiopharm
• Nifedipresc MR
• Nifedix SR
• Nifehexal
• Nifehexal 30 LA
• Nifelan
• Nifelat
• Nifelat Q
• Nifelat-Q
• Nifensar
• Nifensar Retard
• Niferon CR
• Nifeslow
• Nifestad
• Nifezzard
• Nificard
• Nifin
• Nifipen
• Nipen
• Noviken LP
• Nyefax Retard
• Odipin
• Orix
• Osmo-Adalat
• Pidilat
• Pressolat
• Sepamit
• Servidipine
• Slow-Nifine
• Unidipin
• Vasonipine
• Zenusin

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