Felodipine (Plendil) is a calcium channel blocker like amlodipine and nicardipine that primarily acts on the vascular smooth muscles. It is used in the treatment of patients with hypertension.
Felodipine Uses:
-
Hypertension:
- Management of hypertension
-
Off Label Use of Felodipine in Adults:
- Chronic stable angina
- Management of angina
Felodipine (Plendil) Dose in Adults
Felodipine (Plendil) Dose as an alternative agent in the treatment of chronic stable angina (off-label):
Note: A beta-blocker is the preferred therapy; a calcium channel blocker (typically a dihydropyridine [eg, felodipine]) may be added if symptoms are uncontrolled on beta-blockers or as an alternative therapy if there are contraindications or side effects with beta-blockers.
- Oral: Initial: 5 to 10 mg once daily;
- if started at 5 mg, increase the dose to 10 mg once daily according to tolerance, after 2 to 4 weeks.
Felodipine (Plendil) Dose in the treatment of Hypertension:
Note: For initial treatment in patients with blood pressure ≥20/10 mm Hg above goal, use in combination (eg, ACE inhibitor, ARB, or thiazide diuretic).
- Oral: Initial: 2.5 to 5 mg once daily;
- Titrate the dose every 1 to 2 weeks as required based on patient response;
- The usual dose range: 2.5 to 10 mg once daily.
Felodipine (Plendil) Dose in Childrens
Felodipine (Plendil) Dose in the treatment of Hypertension:
-
Children ≥6 years and Adolescents:
- Oral: Initial: 2.5 mg once daily;
- The dose may be increased as needed at 2-week intervals to a maximum daily dose:
- 10 mg/day as tolerated after 2 to 4 weeks.
Pregnancy Risk Factor "C"
- It is possible for adverse events to occur in the mother, infant and fetus. It is not recommended during pregnancy.
- You can also use other agents during pregnancy.
Felodipine use during breastfeeding:
- Potential harm to the infant
- Before starting therapy during lactation, assess the risks and benefits.
Dose in Kidney Disease:
No dose adjustment needed
Dose in Liver disease:
Initial: 2.5 mg once daily; monitor blood pressure closely during titration.
Common Side Effects of Felodipine (Plendil):
-
Cardiovascular:
- Peripheral edema
-
Central nervous system:
- Headache
Less Common Side Effects of Felodipine (Plendil):
-
Cardiovascular:
- Flushing
- Tachycardia
-
Other Side effects:
- Gingival hyperplasia
- Rash
- Upper respiratory tract infection
Contraindications to Felodipine (Plendil):
- Hypersensitivity to felodipine and any component of the formulation
- Women with reproductive potential
- Pregnancy
- Breastfeeding
Warnings and precautions
-
Angina/MI
- Reflex tachycardia can occur, which may cause angina or MI in patients with obstructive heart disease.
-
Hypotension/syncope
- Rarely, symptoms of hypotension can develop with or without syncope.
-
Peripheral edema
- Peripheral edema is the most common side effect (dose-dependent).
-
Aortic stenosis
- It reduces coronary perfusion, which can lead to ischemia.
-
Heart failure:
- Do not use calcium channel blockers to treat heart disease according to ACC/AHA guidelines.
-
Hepatic impairment
- Hepatic dysfunction: Dose adjustment required.
-
Hypertrophic cardiomyopathy with outflow tract obstruction (HCM)
- Patients with HCM or outflow tract obstruction may experience a decrease in afterload, which can worsen their symptoms.
Felodipine: 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) |
|
| 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). |
| ARIPiprazole | CYP2D6 Inhibitors (Weak) may increase the serum concentration of ARIPiprazole. Management: Monitor for increased aripiprazole pharmacologic effects. Aripiprazole dose adjustments may or may not be required based on concomitant therapy and/or indication. Consult full interaction monograph for specific recommendations. |
| 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. |
| Bitter Orange | May increase the serum concentration of Felodipine. |
| 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. |
| 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. |
| 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. |
| 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. Risk C: Monitor therapy |
| 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. |
| Perhexiline | CYP2D6 Inhibitors (Weak) may increase the serum concentration of Perhexiline. |
| 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. |
| 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). |
| 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. |
| CarBAMazepine | May increase the metabolism of Calcium Channel Blockers (Dihydropyridine). Management: Consider calcium channel blocker (CCB) dose adjustments or alternative therapy in patients receiving concomitant carbamazepine. Nimodipine Canadian labeling contraindicates concurrent use with carbamazepine. |
| 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. |
| CYP3A4 Inducers (Strong) | May increase the metabolism of CYP3A4 Substrates (High risk with Inducers). Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. |
| 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). |
| Enzalutamide | May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Concurrent use of enzalutamide with CYP3A4 substrates that have a narrow therapeutic index should be avoided. Use of enzalutamide and any other CYP3A4 substrate should be performed with caution and close monitoring. |
| Fosphenytoin | Calcium Channel Blockers may increase the serum concentration of Fosphenytoin. Management: Monitor for phenytoin toxicity with concomitant use of a calcium channel blocker (CCB) or decreased phenytoin effects with CCB discontinuation. Monitor for decreased CCB therapeutic effects. Nimodipine Canadian labeling contraindicates use with phenytoin. |
| Grapefruit Juice | May increase the serum concentration of Felodipine. Management: Monitor hemodynamic response to felodipine closely in patients who consume grapefruit juice. Felodipine dose adjustment and/or modification of grapefruit juice ingestion may be needed. Felodipine Canadian labeling recommends avoiding grapefruit juice. |
| 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. |
| Mitotane | May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Doses of CYP3A4 substrates may need to be adjusted substantially when used in patients being treated with mitotane. |
| 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. |
| Phenytoin | Calcium Channel Blockers may increase the serum concentration of Phenytoin. Phenytoin may decrease the serum concentration of Calcium Channel Blockers. Management: Avoid use of nimodipine or nifedipine with phenytoin. Monitor for phenytoin toxicity and/or decreased calcium channel blocker effects with any concurrent use. |
| Pitolisant | May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Combined use of pitolisant with a CYP3A4 substrate that has a narrow therapeutic index should be avoided. Other CYP3A4 substrates should be monitored more closely when used with pitolisant. |
| 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. |
| St John's Wort | May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. |
| 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 | May diminish the hypotensive effect of Blood Pressure Lowering Agents. Blood Pressure Lowering Agents may enhance the hypotensive effect of Bromperidol. |
| Conivaptan | May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
| Fusidic Acid (Systemic) | May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
| Idelalisib | May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
| Itraconazole | May increase the serum concentration of Felodipine. |
| Ketoconazole (Systemic) | May increase the serum concentration of Felodipine. |
Monitoring parameters:
- Blood pressure,
- heart rate
Hypertension:
- The 2017 Guideline for the Prevention, Detection, Evaluation, and Management of High Blood Pressure in Adults:
Confirmed hypertension and known CVD or 10-year atherosclerotic cardiovascular disease (ASCVD) risk ≥10%:
- Target blood pressure <130/80 mm Hg
Confirmed hypertension without markers of increased ASCVD risk:
- Target blood pressure <130/80 mm Hg may be reasonable.
Diabetes and hypertension: The American Diabetes Association (ADA) guidelines:
- 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 if it can be safely achieved.
- Patients >65 years of age (healthy or complex/intermediate health):
- Target blood pressure <140/90 mm Hg is advised.
- Patients >65 years of age (very complex/poor health):
- Target blood pressure <150/90 mm Hg is advised.
How to administer Felodipine (Plendil)?
- Oral: Swallow tablet whole do not chew or cut.
- Take an empty stomach or with a low-fat low carb meal.
Mechanism of action of Felodipine (Plendil):
- Felodipine blocks the influx extracellular Ca ions across myocardial and vascular smooth muscles cell membranes.
- This prevents cardiac & vasospastic patients from contracting their smooth muscle.
The onset of action:
- Antihypertensive: 2 to 5 hours
- Duration of antihypertensive effect: 24 hours
Absorption:
- 100%;
- Absolute: 20% due to the first-pass effect
Protein binding:
- >99%
Metabolism:
- Hepatic; CYP3A4 substrate (major); extensive first-pass effect
Half-life elimination:
- Immediate-release: 11 to 16 hours
Time to peak:
- 2.5 to 5 hours
Excretion:
- Urine (70% as metabolites);
- feces 10%
International Brand Names of Felodipine:
- APO-Felodipine
- Plendil
- SANDOZ Felodipine
- AGON SR
- Dilahex
- Dilofen ER
- Dilopin
- Fedil
- Fedil SR
- Felo ER
- Feloblock
- Felocor
- Felocor Retardtab
- Felodil ER
- Felodil XR
- Felodip
- Felodur ER
- Felogamma Retard
- Felogard
- Felogard-ER
- Felopine 5
- Felopine-SR
- Felostad 5 Retard
- Feloten
- Felpin
- Felpin E.R.
- Feltor
- Flodil LP
- Hidipine
- Hydac
- Keliping
- Keydipin ER
- Lodil
- Lodipin ER
- Lodistad MR
- Mibeplen
- Modip
- Munobal
- Munobal Retard
- Nirmadil
- Penedil
- Perfudal
- Phenodical
- Plendil
- Plendil Depottab
- Plendil ER
- Plendil PR
- Plendil Retard
- Plentopine
- Polo
- Presid
- Preslow
- Renedil
- Splendil
- Splendil ER
- Stapin ER
- Topidil
- Vascalpha
- Vaspine ER
- Versant XR
Felodipine Brand Names in Pakistan:
Felodipine Tablets 5 mg in Pakistan |
|
| Felpine | Navegal Laboratories |
| Plendil | Barrett Hodgson Pakistan (Pvt) Ltd. |
Felodipine Tablets 10 mg in Pakistan |
|
| Felpine | Navegal Laboratories |
| Plendil | Barrett Hodgson Pakistan (Pvt) Ltd. |