Nifedipine (Adalat, Procardia) belongs to the class of dihydropyridine calcium channel blockers. It works by relaxation of the muscles of the heart and blood vessels.
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.
Nifedipine: Drug Interaction
Note: Drug Interaction Categories:
- Risk Factor C: Monitor When Using Combination
- Risk Factor D: Consider Treatment Modification
- Risk Factor X: Avoid Concomitant Use
Risk Factor C (Monitor therapy) |
|
| Alcohol (Ethyl) | May increase the serum concentration of NIFEdipine. |
| Alfuzosin | May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
| Alpha1-Blockers | May enhance the hypotensive effect of Calcium Channel Blockers. |
| Amphetamines | May diminish the antihypertensive effect of Antihypertensive Agents. |
| Antipsychotic Agents (Second Generation [Atypical]) | Blood Pressure Lowering Agents may enhance the hypotensive effect of Antipsychotic Agents (Second Generation [Atypical]). |
| Aprepitant | May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
| Atosiban | Calcium Channel Blockers may enhance the adverse/toxic effect of Atosiban. Specifically, there may be an increased risk for pulmonary edema and/or dyspnea. |
| Barbiturates | May increase the metabolism of Calcium Channel Blockers. Management: Monitor for decreased therapeutic effects of calcium channel blockers with concomitant barbiturate therapy. Calcium channel blocker dose adjustments may be necessary. Nimodipine Canadian labeling contraindicates concomitant use with phenobarbital. |
| Barbiturates | May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
| Benperidol | May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
| Beta-Blockers | NIFEdipine may enhance the hypotensive effect of Beta-Blockers. NIFEdipine may enhance the negative inotropic effect of Beta-Blockers. |
| Bosentan | May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
| Brigatinib | May diminish the antihypertensive effect of Antihypertensive Agents. Brigatinib may enhance the bradycardic effect of Antihypertensive Agents. |
| Brimonidine (Topical | May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
| Calcium Channel Blockers (Nondihydropyridine) | Calcium Channel Blockers (Dihydropyridine) may enhance the hypotensive effect of Calcium Channel Blockers (Nondihydropyridine). Calcium Channel Blockers (Nondihydropyridine) may increase the serum concentration of Calcium Channel Blockers (Dihydropyridine). |
| Calcium Salts | May diminish the therapeutic effect of Calcium Channel Blockers. |
| Cisapride | May increase the serum concentration of NIFEdipine. Reported with sustained release nifedipine product. |
| Clofazimine | May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
| Clopidogrel | Calcium Channel Blockers may diminish the therapeutic effect of Clopidogrel. |
| CycloSPORINE (Systemic) | Calcium Channel Blockers (Dihydropyridine) may increase the serum concentration of CycloSPORINE (Systemic). CycloSPORINE (Systemic) may increase the serum concentration of Calcium Channel Blockers (Dihydropyridine). |
| CYP3A4 Inducers (Moderate) | May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
| CYP3A4 Inhibitors (Moderate) | May decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors). |
| Dapoxetine | May enhance the orthostatic hypotensive effect of Calcium Channel Blockers. |
| Deferasirox | May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
| Dexmethylphenidate | May diminish the therapeutic effect of Antihypertensive Agents. |
| Diazoxide | May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
| Digoxin | NIFEdipine may increase the serum concentration of Digoxin. |
| DULoxetine | Blood Pressure Lowering Agents may enhance the hypotensive effect of DULoxetine. |
| Duvelisib | May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
| Efavirenz | May decrease the serum concentration of Calcium Channel Blockers. |
| Erdafitinib | May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
| Erdafitinib | May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
| Fluconazole | May increase the serum concentration of Calcium Channel Blockers. |
| FLUoxetine | May enhance the adverse/toxic effect of NIFEdipine. |
| Fosaprepitant | May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
| Fosnetupitant | May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
| Herbs (Hypertensive Properties) | May diminish the antihypertensive effect of Antihypertensive Agents. |
| Herbs (Hypotensive Properties) | May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
| Hypotension-Associated Agents | Blood Pressure Lowering Agents may enhance the hypotensive effect of Hypotension-Associated Agents. |
| Ivosidenib | May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
| Larotrectinib | May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
| Levodopa-Containing Products | Blood Pressure Lowering Agents may enhance the hypotensive effect of Levodopa-Containing Products. |
| Lormetazepam | May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
| Magnesium Salts | Calcium Channel Blockers may enhance the adverse/toxic effect of Magnesium Salts. Magnesium Salts may enhance the hypotensive effect of Calcium Channel Blockers. |
| Melatonin | May diminish the antihypertensive effect of Calcium Channel Blockers (Dihydropyridine). |
| Methylphenidate | May diminish the antihypertensive effect of Antihypertensive Agents. |
| Molsidomine | May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
| Naftopidil | May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
| Netupitant | May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
| Neuromuscular-Blocking Agents (Nondepolarizing) | Calcium Channel Blockers may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents (Nondepolarizing). |
| Nicergoline | May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
| Nicorandil | May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
| Nitroprusside | Blood Pressure Lowering Agents may enhance the hypotensive effect of Nitroprusside. |
| Palbociclib | May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
| Pentoxifylline | May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
| Pholcodine | Blood Pressure Lowering Agents may enhance the hypotensive effect of Pholcodine. |
| Phosphodiesterase 5 Inhibitors | May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
| Prostacyclin Analogues | May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
| Quinagolide | May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
| QuiNIDine | Calcium Channel Blockers (Dihydropyridine) may decrease the serum concentration of QuiNIDine. Calcium Channel Blockers (Dihydropyridine) may increase the serum concentration of QuiNIDine. QuiNIDine may increase the serum concentration of Calcium Channel Blockers (Dihydropyridine). |
| Sarilumab | May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
| Siltuximab | May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
| Simeprevir | May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
| Tacrolimus (Systemic) | Calcium Channel Blockers (Dihydropyridine) may increase the serum concentration of Tacrolimus (Systemic). |
| Tocilizumab | May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
| VinCRIStine | NIFEdipine may increase the serum concentration of VinCRIStine. |
| VinCRIStine (Liposomal) | NIFEdipine may increase the serum concentration of VinCRIStine (Liposomal). |
| Yohimbine | May diminish the antihypertensive effect of Antihypertensive Agents. |
Risk Factor D (Consider therapy modification) |
|
| Amifostine | Blood Pressure Lowering Agents may enhance the hypotensive effect of Amifostine. Management: When amifostine is used at chemotherapy doses, blood pressure lowering medications should be withheld for 24 hours prior to amifostine administration. If blood pressure lowering therapy cannot be withheld, amifostine should not be administered. |
| Antifungal Agents (Azole Derivatives, Systemic) | May enhance the adverse/toxic effect of Calcium Channel Blockers. Specifically, itraconazole may enhance the negative inotropic effects of verapamil or diltiazem. Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Calcium Channel Blockers. Fluconazole and isavuconazonium likely exert weaker effects than other azoles and are addressed in separate monographs. Management: Concurrent use of felodipine or nisoldipine with itraconazole is specifically contraindicated. Frequent monitoring is warranted with any such combination; calcium channel blocker dose reductions may be required. Exceptions: Fluconazole; Isavuconazonium Sulfate. |
| Cimetidine | May increase the serum concentration of Calcium Channel Blockers. Management: Consider alternatives to cimetidine. If no suitable alternative exists, monitor for increased effects of calcium channel blockers following cimetidine initiation/dose increase, and decreased effects following cimetidine discontinuation/dose decrease. |
| Cladribine | Inhibitors of Equilibrative Nucleoside (ENT1) and Concentrative Nucleoside (CNT3) Transport Proteins may increase the serum concentration of Cladribine. Management: Avoid concomitant use of ENT1 or CNT3 inhibitors during the 4 to 5 day oral cladribine treatment cycles whenever possible. If combined, consider an ENT1 or CNT3 inhibitor dose reduction and separation in the timing of administration. |
| CYP3A4 Inhibitors (Strong) | May decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors). |
| Dabrafenib | May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Seek alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects). |
| Lorlatinib | May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Avoid concurrent use of lorlatinib with any CYP3A4 substrates for which a minimal decrease in serum concentrations of the CYP3A4 substrate could lead to therapeutic failure and serious clinical consequences. |
| Macrolide Antibiotics | May decrease the metabolism of Calcium Channel Blockers. Management: Consider using a noninteracting macrolide. Felodipine Canadian labeling specifically recommends avoiding its use in combination with clarithromycin. Exceptions: Azithromycin (Systemic); Fidaxomicin; Roxithromycin; Spiramycin. |
| MiFEPRIStone | May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Minimize doses of CYP3A4 substrates, and monitor for increased concentrations/toxicity, during and 2 weeks following treatment with mifepristone. Avoid cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus. |
| Nafcillin | May decrease the serum concentration of NIFEdipine. |
| Obinutuzumab | May enhance the hypotensive effect of Blood Pressure Lowering Agents. Management: Consider temporarily withholding blood pressure lowering medications beginning 12 hours prior to obinutuzumab infusion and continuing until 1 hour after the end of the infusion. |
| Rifamycin Derivatives | May decrease the serum concentration of Calcium Channel Blockers. This primarily affects oral forms of calcium channel blockers. Management: The labeling for some US and Canadian calcium channel blockers contraindicate use with rifampin, however recommendations vary. Consult appropriate labeling. |
| Sincalide | Drugs that Affect Gallbladder Function may diminish the therapeutic effect of Sincalide. Management: Consider discontinuing drugs that may affect gallbladder motility prior to the use of sincalide to stimulate gallbladder contraction. |
| Stiripentol | May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. |
Risk Factor X (Avoid combination) |
|
| Bromperidol | Blood Pressure Lowering Agents may enhance the hypotensive effect of Bromperidol. Bromperidol may diminish the hypotensive effect of Blood Pressure Lowering Agents. |
| Conivaptan | May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
| CYP3A4 Inducers (Strong) | May decrease the serum concentration of NIFEdipine. |
| Fusidic Acid (Systemic) | May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
| Grapefruit Juice | May increase the serum concentration of NIFEdipine. |
| Idelalisib | May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
| Phenytoin | NIFEdipine may increase the serum concentration of Phenytoin. Phenytoin may decrease the serum concentration of NIFEdipine. |
| St John's Wort | May decrease the serum concentration of NIFEdipine. |
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
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
Nifedipine Brand Names in Pakistan:
Nifedipine Tablets 10 mg |
|
| Nifelate | Siza International (Pvt) Ltd. |
Nifedipine Tablets 20 mg |
|
| Adalat Retard | Bayer Health Care |
| Anifed | Tread Pharmaceuticals Pvt Ltd |
| Nifecard Retard | Novartis Pharma (Pak) Ltd |
| Nifed | Unimark Pharmaceuticals |
| Nifedicor | Scharper Pharmaceuticals (Pvt) Ltd. |
Nifedipine Tablets 30 mg |
|
| Adalat La | Bayer Health Care |
| Adalat-Cc | Bayer Health Care |
| Nifecard Xl | Novartis Pharma (Pak) Ltd |
| Nifedil-Xl | Zafa Pharmaceutical Laboratories (Pvt) Ltd. |
| Nifine C.C | Tread Pharmaceuticals Pvt Ltd |
Nifedipine Tablets 60 mg |
|
| Adalat La | Bayer Health Care |
| Adalat-Cc | Bayer Health Care |
Nifedipine SR Tablets 20 mg |
|
| Anifed | Tread Pharmaceuticals Pvt Ltd |
Nifedipine Capsules 10 mg |
|
| Adalat | Bayer Health Care |
| Adipen | Lisko Pakistan (Pvt) Ltd |
| Caranta | Akhai Pharmaceuticals. |
| Nifedil | Zafa Pharmaceutical Laboratories (Pvt) Ltd. |
| Nifedil S.G | Zafa Pharmaceutical Laboratories (Pvt) Ltd. |
| Ronian | S. Ejazuddin & Company |
| Vasculine | Geofman Pharmaceuticals |
Nifedipine Capsules Sr 20 Mg |
|
| Cardipine | Phar-Man Laboratories |