pharmacopeia
GET
/api/v1/drug/felodipine
2D structure
5-O-ethyl 3-O-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate
SMILES CCOC(=O)C1=C(NC(=C(C1C2=C(C(=CC=C2)Cl)Cl)C(=O)OC)C)C
InChIKey RZTAMFZIAATZDJ-UHFFFAOYSA-N

Mechanism of action

Sourced from openFDA

Felodipine is a member of the dihydropyridine class of calcium channel antagonists (calcium channel blockers). It reversibly competes with nitrendipine and/or other calcium channel blockers for dihydropyridine binding sites, blocks voltage-dependent Ca ++ currents in vascular smooth muscle and cultured rabbit atrial cells, and blocks potassium-induced contracture of the rat portal vein.

Calcium ChannelL-Calcium Channel Receptor

Indications

Sourced from openFDA
  • Felodipine extended-release tablets, USP are indicated for the treatment of hypertension, to lower blood pressure. Lowering blood pressure lowers the risk of fatal and non-fatal cardiovascular events, primarily strokes and myocardial infarctions.ICD-10: I10

Contraindications

Sourced from openFDA
  • Felodipine extended-release tablets, USP are contraindicated in patients who are hypersensitive to this product.contraindicated

Dosage & administration

Sourced from openFDA

The recommended starting dose is 5 mg once a day. Depending on the patient's response, the dosage can be decreased to 2.5 mg or increased to 10 mg once a day. These adjustments should occur generally at intervals of not less than 2 weeks. The recommended dosage range is 2.5 to 10 mg once daily. In clinical trials, doses above 10 mg daily showed an increased blood pressure response but a large increase in the rate of peripheral edema and other vasodilatory adverse events (see ADVERSE REACTIONS ). Modification of the recommended dosage is usually not required in patients with renal impairment. Felodipine extended-release tablets, USP should regularly be taken either without food or with a light meal (see CLINICAL PHARMACOLOGY, Pharmacokinetics and Metabolism ). Felodipine extended-release tablets, USP should be swallowed whole and not crushed or chewed. Geriatric Use Patients over 65 years of age are likely to develop higher plasma concentrations of felodipine (see CLINICAL PHARMACOLOGY ). In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range (2.5 mg daily). Elderly patients should have their blood pressure closely monitored during any dosage adjustment.

Adverse reactions

Sourced from openFDA

In controlled studies in the United States and overseas, approximately 3000 patients were treated with felodipine as either the extended-release or the immediate-release formulation. The most common clinical adverse events reported with felodipine extended-release administered as monotherapy at the recommended dosage range of 2.5 mg to 10 mg once a day were peripheral edema and headache. Peripheral edema was generally mild, but it was age and dose related and resulted in discontinuation of therapy in about 3% of the enrolled patients. Discontinuation of therapy due to any clinical adverse event occurred in about 6% of the patients receiving felodipine extended-release, principally for peripheral edema, headache, or flushing. Adverse events that occurred with an incidence of 1.5% or greater at any of the recommended doses of 2.5 mg to 10 mg once a day (felodipine extended-release, N = 861; Placebo, N = 334), without regard to causality, are compared to placebo and are listed by dose in the table below. These events are reported from controlled clinical trials with patients who were randomized to a fixed dose of felodipine extended-release tablets, USP or titrated from an initial dose of 2.5 mg or 5 mg once a day. A dose of 20 mg once a day has been evaluated in some clinical studies. Although the antihypertensive effect of felodipine extended-release tablets, USP is increased at 20 mg once a day, there is a disproportionate increase in adverse events, especially those associated with vasodilatory effects (see DOSAGE AND ADMINISTRATION ).

Use in specific populations

Sourced from openFDA

Pregnancy Pregnancy Category C Teratogenic Effects Studies in pregnant rabbits administered doses of 0.46, 1.2, 2.3 and 4.6 mg/kg/day (from 0.8 to 8 times 1 the maximum recommended human dose on a mg/m 2 basis) showed digital anomalies consisting of reduction in size and degree of ossification of the terminal phalanges in the fetuses. The frequency and severity of the changes appeared dose related and were noted even at the lowest dose. These changes have been shown to occur with other members of the dihydropyridine class and are possibly a result of compromised uterine blood flow. Similar fetal anomalies were not observed in rats given felodipine. In a teratology study in cynomolgus monkeys, no reduction in the size of the terminal phalanges was observed, but an abnormal position of the distal phalanges was noted in about 40% of the fetuses. Nonteratogenic Effects A prolongation of parturition with difficult labor and an increased frequency of fetal and early postnatal deaths were observed in rats administered doses of 9.6 mg/kg/day (8 times 1 the maximum human dose on a mg/m 2 basis) and above. Significant enlargement of the mammary glands, in excess of the normal enlargement for pregnant rabbits, was found with doses greater than or equal to 1.2 mg/kg/day (2.1 times the maximum human dose on a mg/m 2 basis).

Pharmacokinetics

Sourced from openFDA
Metabolism
and Metabolism Following oral administration, felodipine is almost completely absorbed and undergoes extensive first-pass metabolism. The systemic bioavailability of felodipine is approximately 20%.

Overdosage

Sourced from openFDA

Oral doses of 240 mg/kg and 264 mg/kg in male and female mice, respectively, and 2390 mg/kg and 2250 mg/kg in male and female rats, respectively, caused significant lethality. In a suicide attempt, one patient took 150 mg felodipine together with 15 tablets each of atenolol and spironolactone and 20 tablets of nitrazepam. The patient's blood pressure and heart rate were normal on admission to hospital; he subsequently recovered without significant sequelae. Overdosage might be expected to cause excessive peripheral vasodilation with marked hypotension and possibly bradycardia. If severe hypotension occurs, symptomatic treatment should be instituted. The patient should be placed supine with the legs elevated. The administration of intravenous fluids may be useful to treat hypotension due to overdosage with calcium antagonists. In case of accompanying bradycardia, atropine (0.5 to 1 mg) should be administered intravenously. Sympathomimetic drugs may also be given if the physician feels they are warranted. It has not been established whether felodipine can be removed from the circulation by hemodialysis.

Approval history

Sourced from openFDA
  • Dec 17, 2010ANDAANDA090365Glenmark Pharms Ltd
  • Oct 28, 2011ANDAANDA200815Ph Health
  • Nov 28, 2011ANDAANDA202170Torrent Pharms Ltd
  • Jan 17, 2013ANDAANDA203417Aurobindo Pharma Ltd
  • Nov 8, 2013ANDAANDA201964Heritage
  • Oct 26, 2018ANDAANDA210847Yiling
  • Apr 29, 2019ANDAANDA204800Yung Shin Pharm

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
11,135 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Fatigue1,0669.6%
  2. 2Dyspnoea9678.7%
  3. 3Dizziness9598.6%
  4. 4Diarrhoea8537.7%
  5. 5Nausea8537.7%
  6. 6Headache8347.5%
  7. 7Pain8067.2%
  8. 8Pyrexia7416.7%
  9. 9Vomiting7016.3%
  10. 10Malaise6706.0%
  11. 11Arthralgia6565.9%
  12. 12Off Label Use6505.8%
  13. 13Palpitations6425.8%
  14. 14Pruritus6285.6%
  15. 15Abdominal Discomfort5905.3%

Literature

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Recent PubMed references pinned to Felodipine as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 28 ClinicalTrials.gov registrations naming Felodipine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Structural analogs

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Ranked by 2D fingerprint (Tanimoto) similarity over PubChem structures. Structural proximity only — not a claim of therapeutic equivalence.

Frequently asked questions

How does Felodipine work?
Felodipine is a member of the dihydropyridine class of calcium channel antagonists (calcium channel blockers). It reversibly competes with nitrendipine and/or other calcium channel blockers for dihydropyridine binding sites, blocks voltage-dependent Ca ++ currents in vascular smooth muscle and cultured rabbit atrial cells, and blocks potassium-induced contracture of the rat portal vein.
What is Felodipine used for?
According to FDA labeling, Felodipine carries indications including: Felodipine extended-release tablets, USP are indicated for the treatment of hypertension, to lower blood pressure. Lowering blood pressure lowers the risk of fatal and non-fatal cardiovascular events, primarily strokes and myocardial infarctions.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Felodipine?
Felodipine is classified as Dihydropyridine derivatives, Dihydropyridine Calcium Channel Blocker, Calcium Channel Antagonists, L-Calcium Channel Receptor Antagonists, Coronary Arterial Vasodilation, Decreased Blood Pressure.
What are the contraindications for Felodipine?
Felodipine labeling lists contraindications including: Felodipine extended-release tablets, USP are contraindicated in patients who are hypersensitive to this product.. Always consult the full prescribing information and a clinician.
Note. Data for felodipine is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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