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: If you're dealing with chronic stable angina, doctors usually start treatment with beta-blockers. But if you're still having symptoms even after taking beta-blockers, they might add a calcium channel blocker like felodipine. Sometimes, if you can't take beta-blockers because of certain issues or if they cause bad side effects, felodipine could be used instead, based on recommendations from the American College of Cardiology and the American Heart Association in 2012.
- Starting Dose: Typically, the treatment begins with 5 to 10 mg taken orally once a day.
- Adjusting the Dose: If you start with 5 mg daily, your doctor may increase the dose to 10 mg daily after 2 to 4 weeks, depending on how well you tolerate the medication.
Felodipine (Plendil) Dose in the treatment of Hypertension:
- Starting Dose: The initial dosage of felodipine usually ranges between 2.5 mg and 5 mg, taken orally once daily.
- Adjustment: Depending on how you respond to the treatment, your doctor might adjust the dose. This adjustment typically occurs every 1 to 2 weeks.
- Usual Dosing Range: Over time, most patients stabilize on a daily dose ranging from 2.5 mg to 10 mg.
When to Combine Felodipine with Other Medications:
- High Blood Pressure Far Above Goal (≥20/10 mm Hg above target): Felodipine might be used in combination with another antihypertensive agent, such as an ACE inhibitor, an ARB, or a thiazide diuretic, right from the start.
- Mildly Above Goal (<20/10 mm Hg above target): It might be reasonable to start with felodipine alone. However, many patients will eventually need a combination of drugs to achieve optimal blood pressure control.
This strategy allows for flexibility based on how far your blood pressure is from your target goal and how your body responds to the medication.
Felodipine (Plendil) Dose in Children
Felodipine (Plendil) Dose in the treatment of Hypertension:
For treating hypertension in children aged 6 years and older, and in adolescents:
- Initial Dose: The starting dose is 2.5 mg, taken orally once daily.
- Dose Adjustments: If needed, the dose may be increased at 2-week intervals.
- Maximum Dose: The dose should not exceed 10 mg per day.
This dosing regimen is guided by recommendations and data from sources such as the American Academy of Pediatrics (AAP) and the National Heart, Lung, and Blood Institute (NHLBI).
Pregnancy Risk Factor "C"
- Felodipine falls into Pregnancy Risk Factor C, meaning there's a possibility of adverse effects observed in animal studies.
- It's crucial to manage hypertension during pregnancy to avoid risks to both the mother and the baby.
- However, if medication is necessary, other options are preferred over felodipine, as recommended by the American College of Obstetricians and Gynecologists (ACOG) in 2013.
- Additionally, Canadian labeling advises against the use of felodipine in women of childbearing potential and during pregnancy due to potential risks.
Felodipine use during breastfeeding:
- Since it's uncertain whether felodipine passes into breast milk, caution is advised for breastfeeding mothers.
- The manufacturer suggests considering the importance of treatment for the mother's health versus the potential risks to the breastfeeding infant.
- If felodipine is deemed necessary, alternatives like discontinuing breastfeeding or stopping the medication should be carefully evaluated, taking into account the potential for serious adverse reactions in the infant.
Felodipine Dose in Kidney Disease:
- No dosage adjustment is typically required for felodipine in individuals with renal impairment.
Felodipine Dose in Liver disease:
- The typical starting dose of felodipine is 2.5 mg taken once daily.
- During the adjustment period, it's important to monitor blood pressure closely to ensure it's effectively controlled without causing any adverse effects.
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):
- If you have a known hypersensitivity to felodipine or any component of its formulation, its use is contraindicated, meaning it should be avoided.
- Additionally, Canadian labeling specifies further contraindications not found in US labeling, including hypersensitivity to other dihydropyridines and avoiding its use in women of childbearing potential, during pregnancy, and while breastfeeding.
Warnings and precautions
Angina/MI
- Starting or adjusting the dosage of dihydropyridine calcium channel blockers like felodipine can sometimes lead to more angina (chest pain) or even heart attacks.
- This might happen because these medications can cause the heart to beat faster, which can make angina worse or trigger a heart attack, especially in people with blocked heart arteries.
- This risk is higher if you're not taking a beta-blocker at the same time.
Hypotension/syncope
- In rare cases, felodipine can cause low blood pressure, which may lead to symptoms like feeling dizzy or fainting (syncope).
- It's essential to lower blood pressure at a pace that's safe for the individual's overall health.
Peripheral edema
- The most common side effect of felodipine is peripheral edema, which means swelling in the legs or ankles.
- This side effect can happen within 2 to 3 weeks of starting the medication and is usually related to the dose you're taking.
- If you notice swelling in your legs or ankles while taking felodipine, let your doctor know.
- They can help manage this side effect or adjust your treatment if needed.
Aortic stenosis
- In patients with severe aortic stenosis, using felodipine requires extreme caution.
- Felodipine might lower blood flow to the heart's arteries, which can lead to a condition called ischemia, where the heart muscle doesn't get enough oxygen.
- This caution is essential to prevent potential complications and ensure the safety of individuals with this heart condition.
Heart failure:
- According to the American College of Cardiology (ACC) and the American Heart Association (AHA) guidelines for heart failure, it's advised to avoid using felodipine in patients with heart failure.
- This recommendation stems from findings suggesting that calcium channel blockers, including felodipine, may not provide significant benefits and could potentially lead to worse outcomes in individuals with heart failure.
Hepatic impairment
- In patients with hepatic impairment (liver problems), it's important to use felodipine cautiously.
- Depending on the severity of the impairment, a lower starting dose may be necessary to ensure safety and effectiveness.
- The liver plays a crucial role in metabolizing medications like felodipine, so impairment can affect how the drug is processed in the body.
Hypertrophic cardiomyopathy with outflow tract obstruction (HCM)
- In patients with hypertrophic cardiomyopathy (HCM) and outflow tract obstruction, it's important to use felodipine with caution.
- Felodipine works by reducing the workload on the heart, which can potentially worsen symptoms in individuals with HCM and outflow tract obstruction.
- This caution is necessary to avoid exacerbating the condition.
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
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Risk Factor C (Monitor therapy) |
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The hypotensive effects of blood pressure-lowering medications may be strengthened. |
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Alpha1-Blockers |
The hypotensive effects of calcium channel blockers may be strengthened. |
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Amphetamines |
May lessen the effectiveness of antihypertensive agents. |
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Antipsychotic Agents (Second Generation [Atypical]) |
Antipsychotic drugs' hypotensive effects may be enhanced by blood pressure-lowering medications (Second Generation [Atypical]). |
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May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors). |
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ARIPiprazole |
ARIPiprazole's serum levels may rise in response to CYP2D6 Inhibitors (Weak). Management: Keep an eye out for enhanced pharmacologic effects of aripiprazole. Depending on the concurrent therapy and/or the indication, aripiprazole dosage modifications may or may not be necessary. For detailed advice, refer to the complete interaction monograph. |
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Atosiban |
Calcium channel blockers may intensify Atosiban's harmful or hazardous effects. Particularly, pulmonary edoema and/or dyspnea may be at higher risk. |
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Barbiturates |
Calcium Channel Blockers' metabolic rate might be increased. Management: Keep an eye out for any diminished therapeutic effects of barbiturate medication when concurrently using calcium channel blockers. There may need to be dose modifications with calcium channel blockers. The concurrent use of phenobarbital and nimodipine is not recommended. |
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Barbiturates |
The hypotensive effects of blood pressure-lowering medications may be strengthened. |
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Benperidol |
The hypotensive effects of blood pressure-lowering medications may be strengthened. |
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Brimonidine (Topical) |
The hypotensive effects of blood pressure-lowering medications may be strengthened. |
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Calcium Salts |
.Calcium Channel Blockers' therapeutic impact can be lessened. |
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Clofazimine |
May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors). |
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Clopidogrel |
Calcium channel blockers may reduce Clopidogrel's therapeutic efficacy. |
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CycloSPORINE (Systemic) |
The serum concentration of CycloSPORINE may rise when Calcium Channel Blockers (Dihydropyridine) are taken (Systemic). |
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CYP3A4 Inducers (Moderate) |
Calcium Channel Blockers' serum levels may rise when CycloSPORINE (Systemic) is used (Dihydropyridine). |
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CYP3A4 Inhibitors (Moderate) |
May lower the serum level of CYP3A4 substrates (High risk with Inducers). |
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Dapoxetine |
May intensify calcium channel blockers' orthostatic hypotensive effects. |
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May lower the serum level of CYP3A4 substrates (High risk with Inducers). |
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Dexmethylphenidate |
Can lessen an antihypertensive drug's therapeutic impact. |
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The hypotensive effects of blood pressure-lowering medications may be strengthened. |
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The hypotensive impact of DULoxetine may be enhanced by blood pressure lowering medications. |
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May lower the serum level of CYP3A4 substrates (High risk with Inducers). |
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Calcium Channel Blockers' serum concentration can drop. |
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May lower the serum level of CYP3A4 substrates (High risk with Inducers). |
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May lower the serum level of CYP3A4 substrates (High risk with Inducers). |
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Fluconazole |
Calcium Channel Blockers' serum levels can rise. |
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May lower the serum level of CYP3A4 substrates (High risk with Inducers). |
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Fosnetupitant |
May lower the serum level of CYP3A4 substrates (High risk with Inducers). |
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Herbs (Hypertensive Properties) |
May lessen the effectiveness of antihypertensive agents. |
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Herbs (Hypotensive Properties) |
The hypotensive effects of blood pressure-lowering medications may be strengthened. |
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Hypotension-Associated Agents |
May lessen the effectiveness of antihypertensive agents. |
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May lower the serum level of CYP3A4 substrates (High risk with Inducers). |
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May lower the serum level of CYP3A4 substrates (High risk with Inducers). |
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Levodopa-Containing Products |
The hypotensive action of hypotension-associated agents may be strengthened by blood pressure lowering medications. |
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Lormetazepam |
The hypotensive effects of blood pressure-lowering medications may be strengthened. |
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Magnesium Salts |
Levodopa-Containing Products' hypotensive effects may be strengthened by blood pressure-lowering medications. |
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Melatonin |
May reduce the effectiveness of calcium channel blockers as an antihypertensive (Dihydropyridine). |
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May lessen the effectiveness of antihypertensive agents. |
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Molsidomine |
The hypotensive effects of blood pressure-lowering medications may be strengthened. |
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Naftopidil |
The hypotensive effects of blood pressure-lowering medications may be strengthened. |
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Netupitant |
May lower the serum level of CYP3A4 substrates (High risk with Inducers). |
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Neuromuscular-Blocking Agents (Nondepolarizing) |
The neuromuscular-blocking impact of neuromuscular-blocking agents may be enhanced by calcium channel blockers (Nondepolarizing). |
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Nicergoline |
Blood pressure-lowering medicines may strengthen their hypotensive effects. |
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Nicorandil |
The hypotensive effects of blood pressure-lowering medications may be strengthened. Risk C: Follow-up treatment |
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Nitroprusside's hypotensive impact may be strengthened by blood pressure-lowering medications. |
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May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
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Blood pressure-lowering medicines may strengthen their hypotensive effects. |
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Perhexiline |
The quantity of perhexiline in the serum may rise in response to CYP2D6 Inhibitors (Weak). |
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Pholcodine |
Pholcodine's hypotensive impact may be strengthened by blood pressure lowering medications. |
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Phosphodiesterase 5 Inhibitors |
The hypotensive effects of blood pressure-lowering medications may be strengthened. |
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Prostacyclin Analogues |
The hypotensive effects of blood pressure-lowering medications may be strengthened. |
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The hypotensive effects of blood pressure-lowering medications may be strengthened. |
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May lower the serum level of CYP3A4 substrates (High risk with Inducers). |
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May lower the serum level of CYP3A4 substrates (High risk with Inducers). |
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May lower the serum level of CYP3A4 substrates (High risk with Inducers). |
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Tacrolimus (Systemic) |
Tacrolimus serum levels may rise when Calcium Channel Blockers (Dihydropyridine) are used (Systemic). |
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May lower the serum level of CYP3A4 substrates (High risk with Inducers). |
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Yohimbine |
May lessen the effectiveness of antihypertensive agents. |
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Risk Factor D (Consider therapy modification) |
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Amifostine |
Amifostine's hypotensive impact may be strengthened by blood pressure lowering medications. Treatment: Blood pressure-lowering drugs need to be avoided for 24 hours before amifostine is administered when used at chemotherapeutic doses. Amifostine should not be given if blood pressure lowering treatment cannot be stopped. |
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Antifungal Agents (Azole Derivatives, Systemic) |
Calcium Channel Blockers' harmful or toxic effects could be exacerbated. In particular, itraconazole may make verapamil or diltiazem's unfavourable inotropic effects worse. Calcium Channel Blockers' metabolism may be slowed down by antifungal agents (systemic azole derivatives). Fluconazole and isavuconazonium, which are covered in different monographs, probably have less powerful effects than those of other azoles. Treatment: Itraconazole should not be used concurrently with felodipine or nisoldipine. With any such combination, regular monitoring is advised; calcium channel blocker dose decreases might be necessary. |
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Calcium Channel Blockers' metabolism could be accelerated (Dihydropyridine). In individuals receiving concurrent carbamazepine, consider adjusting the dosage of calcium channel blockers (CCBs) or switching to an alternative form of treatment. The Canadian labelling for nimodipine expressly forbids taking it alongside carbamazepine. |
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Calcium Channel Blockers' serum levels can rise. Management: Take cimetidine substitutes into consideration. If there is no suitable substitute, watch for increased calcium channel blocker effects after starting or increasing the dosage of cimetidine and decreased effects after stopping or decreasing the dosage. |
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CYP3A4 Inducers (Strong) |
May speed up CYP3A4 substrate metabolism (High risk with Inducers). Management: Take into account a substitute for one of the interfering medications. Specific contraindications may apply to some combinations. the relevant manufacturer's label. |
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CYP3A4 Inhibitors (Strong) |
May slow down CYP3A4 substrate metabolism (High risk with Inhibitors). |
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Dabrafenib |
May lower the serum level of CYP3A4 substrates (High risk with Inducers). Management: When possible, look for substitutes for the CYP3A4 substrate. If concurrent therapy cannot be avoided, pay special attention to the substrate's clinical consequences (particularly therapeutic effects). |
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May lower the serum level of CYP3A4 substrates (High risk with Inducers). Treatment: Enzalutamide should not be used concurrently with CYP3A4 substrates that have a limited therapeutic index. Enzalutamide use, like with the use of any other CYP3A4 substrate, should be done cautiously and under close observation. |
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Calcium channel blockers may raise the level of fosphenytoin in the blood. Monitoring for phenytoin toxicity while using a calcium channel blocker (CCB) at the same time or reduced phenytoin effects while stopping the CCB are the two management options. |
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Grapefruit Juice |
Could raise the serum level of felodipine. Treatment: In patients who drink grapefruit juice, closely monitor the hemodynamic response to felodipine. It might be necessary to modify how much grapefruit juice is consumed while taking felodipine. The Canadian labelling for felodipine advises against drinking grapefruit juice. |
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Lorlatinib |
May lower the serum level of CYP3A4 substrates (High risk with Inducers). Management: Avoid taking lorlatinib at the same time as any CYP3A4 substrates for which even a small drop in serum levels of the substrate could result in therapeutic failure and negative clinical outcomes. |
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Macrolide Antibiotics |
Calcium Channel Blockers' metabolic rate might be decreased. Use a noninteracting macrolide as a possible management strategy. The Canadian labelling for felodipine expressly advises against using it in conjunction with clarithromycin. Azithromycin (Systemic), Fidaxomicin, Roxithromycin, and Spiramycin are exceptions. |
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May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors). Management: During and two weeks after mifepristone treatment, reduce doses of CYP3A4 substrates and keep an eye out for elevated amounts or toxicity. Fentanyl, pimozide, quinidine, sirolimus, and tacrolimus should all be avoided. Cyclosporine should also be avoided. |
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May lower the serum level of CYP3A4 substrates (High risk with Inducers). Treatment: When administered in individuals receiving mitotane, doses of CYP3A4 substrates may need to be significantly modified. |
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The hypotensive effects of blood pressure-lowering medications may be strengthened. Management: Take into account temporarily stopping blood pressure-lowering drugs 12 hours before the start of the obinutuzumab infusion and keeping them off until 1 hour after the infusion is finished. |
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The serum levels of phenytoin may rise when calcium channel blockers are used. Calcium Channel Blockers' serum levels may be reduced by phenytoin. Avoid combining nimodipine or nifedipine with phenytoin for management. With any concurrent use, keep an eye out for phenytoin toxicity and/or diminished calcium channel blocker effects. |
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May lower the serum level of CYP3A4 substrates (High risk with Inducers). Management: Pitolisant should not be used in conjunction with a CYP3A4 substrate that has a limited therapeutic index. When administered with pitolisant, other CYP3A4 substrates need to be checked more carefully. |
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Rifamycin Derivatives |
Calcium Channel Blockers' serum concentration can drop. This predominantly affects calcium channel blockers used orally. Management: Using rifampin with certain calcium channel blockers is not advised according to the labelling in the US and Canada. Look up the relevant labelling. |
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The therapeutic benefit of Sincalide may be reduced by medications that affect gallbladder function. Prior to using sincalide to induce gallbladder contraction, you should think about stopping any medications that can impair gallbladder motility. |
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St John's Wort |
May lower the serum level of CYP3A4 substrates (High risk with Inducers). Management: Take into account a substitute for one of the interfering medications. Specific contraindications may apply to some combinations. the relevant manufacturer's label. |
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May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors). Management: Due to the increased potential for side effects and toxicity, stiripentol should not be used with CYP3A4 substrates that are thought to have a narrow therapeutic index. Use of stiripentol with any CYP3A4 substrate necessitates closer observation. |
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Risk Factor X (Avoid combination) |
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Bromperidol |
May lessen blood pressure lowering agents' hypotensive effects. The hypotensive impact of bromperidol may be enhanced by blood pressure lowering medications. |
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Conivaptan |
May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors). |
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Fusidic Acid (Systemic) |
May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors). |
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Idelalisib |
May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors). |
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Could raise the serum level of felodipine. |
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Ketoconazole (Systemic) |
Could raise the serum level of felodipine. |
Monitoring parameters:
Blood Pressure Goals:
- Confirmed Hypertension with Known Cardiovascular Disease (CVD) or High ASCVD Risk (ACC/AHA [Whelton 2017]):
- Target Blood Pressure: <130/80 mm Hg is recommended.
- Confirmed Hypertension without Increased ASCVD Risk (ACC/AHA [Whelton 2017]):
- Target Blood Pressure: <130/80 mm Hg may be reasonable.
Diabetes and Hypertension (ADA 2019):
- Patients 18 to 65 years without ASCVD and <15% ASCVD risk:
- Target Blood Pressure: <140/90 mm Hg is recommended.
- Patients 18 to 65 years with known ASCVD or >15% ASCVD risk:
- Target Blood Pressure: <130/80 mm Hg may be appropriate if safely attainable.
- Patients >65 years (healthy or complex/intermediate health):
- Target Blood Pressure: <140/90 mm Hg is recommended.
- Patients >65 years (very complex/poor health):
- Target Blood Pressure: <150/90 mm Hg is recommended.
These guidelines provide tailored blood pressure targets based on various factors such as age, presence of cardiovascular disease, and overall health status.
How to administer Felodipine (Plendil)?
- Swallow Whole: Felodipine tablets should be swallowed whole and should not be divided, crushed, or chewed.
- Food Intake: Felodipine may be taken without food or with a small meal that is low in fat and carbohydrates.
Mechanism of action of Felodipine (Plendil):
- Felodipine works by blocking calcium ions from entering certain areas of vascular smooth muscle and heart muscle during depolarization.
- This action specifically targets "slow channels" or voltage-sensitive regions.
- By doing so, it causes relaxation of the smooth muscles in the coronary blood vessels, leading to dilation (widening).
- This dilation improves blood flow to the heart muscle, increasing the delivery of oxygen.
- This effect is particularly beneficial for patients with vasospastic angina, a condition characterized by spasms in the coronary arteries, as it helps to prevent and relieve symptoms by improving blood flow to the heart.
Onset of Action (Antihypertensive):
- It typically takes 2 to 5 hours for felodipine to start lowering blood pressure.
Duration of Antihypertensive Effect:
- The antihypertensive effect of felodipine lasts for about 24 hours.
Absorption:
- Felodipine is completely absorbed when taken orally, but only about 20% of the drug reaches the bloodstream due to the first-pass effect (metabolism in the liver before entering systemic circulation).
Protein Binding:
- More than 99% of felodipine in the bloodstream is bound to proteins.
Metabolism:
- Felodipine is primarily metabolized in the liver, mainly by the enzyme CYP3A4. It undergoes extensive first-pass metabolism.
Half-life (Elimination):
- The half-life of immediate-release felodipine is around 11 to 16 hours.
Time to Peak:
- It takes approximately 2.5 to 5 hours for felodipine to reach its peak concentration in the bloodstream after oral administration.
Excretion:
- Felodipine and its metabolites are primarily excreted in the urine (about 70%) and to a lesser extent in the feces (about 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:
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Felodipine Tablets 5 mg in Pakistan |
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Felpine |
Navegal Laboratories |
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Plendil |
Barrett Hodgson Pakistan (Pvt) Ltd. |
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Felodipine Tablets 10 mg in Pakistan |
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Felpine |
Navegal Laboratories |
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Plendil |
Barrett Hodgson Pakistan (Pvt) Ltd. |
