Felodipine Er (felodipine)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Felodipine is a 1,4-dihydropyridine-derivative calcium-channel blocking agent (calcium-channel blocker).
Felodipine is a 1,4-dihydropyridine-derivative calcium-channel blocking agent that is structurally related to nifedipine and nicardipine. The principal physiologic action of felodipine is to inhibit the transmembrane influx of extracellular calcium ions across the membranes of myocardial cells and vascular smooth muscle cells. Felodipine is a peripheral arterial vasodilator; the drug acts directly on vascular smooth muscle causing a reduction in peripheral vascular resistance and blood pressure.
The hypotensive effect is principally a consequence of a dose-related reduction in peripheral vascular resistance, with a modest reflex increase in heart rate. The effects of felodipine are more selective to vascular smooth muscle than cardiac muscle; no substantial effect on cardiac conduction (PR, PQ, and HV intervals) has been observed in clinical and electrophysiologic studies. During the first week of therapy, a reflex increase in heart rate may occur; however, this increase attenuated over time.
Following chronic dosing, heart rate increases of 5-10 beats per minute may be observed; such changes are inhibited by beta-adrenergic blocking agents.
The onset of the blood pressure lowering effect following administration of felodipine extended-release tablets generally occurs within 2-5 hours. The antihypertensive effect is dose dependent and during chronic administration, substantial blood pressure control lasts for 24 hours, with trough reductions in diastolic blood pressure approximately 40-50% of peak reductions.
Felodipine is almost completely absorbed following oral administration but the drug undergoes extensive first-pass metabolism. The systemic bioavailability of felodipine is approximately 20%. Mean peak felodipine concentrations occur within 2.5-5 hours following administration of felodipine extended-release tablets.
Peak concentrations of the drug were increased by 60% when felodipine (extended-release formulation) was administered with a high-fat or high-carbohydrate meal and no changes in pharmacokinetics were observed when the drug was administered with a light meal (e.g., orange juice, toast, and cereal); AUC was unchanged. When administered with grapefruit juice, felodipine bioavailability increased approximately 2-fold. Felodipine is highly protein bound (>99%); the drug is known to cross the blood-brain barrier and the placenta in animals.
Felodipine is metabolized in the liver by cytochrome P-450 (CYP) 3A4; none of the 6 metabolites identified to date has substantial vasodilating activity. Felodipine is eliminated as metabolites, mainly in urine and to a lesser extent in feces; a negligible amount (<0.5%) of intact drug is recovered in urine and feces. The mean terminal half-life is approximately 11-16 hours following administration of felodipine as an immediate-release formulation.
In elderly individuals, mean felodipine clearance is 45% of that observed in young individuals; mean felodipine AUC at steady-state in young individuals was 39% of that observed for elderly individuals. Felodipine clearance in patients with hepatic disease may be decreased to about 60% of that observed in young healthy individuals.
USES: This medication is used to treat high blood pressure. Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. Felodipine belongs to a class of drugs known as calcium channel blockers.
It works by relaxing blood vessels so blood can flow more easily.
Generic name: felodipine
Pronunciation: (fell-OH-dih-peen)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Felodipine Er
Indications
The following indications are listed for Felodipine Er:
- Hypertension
Also known as: Elevated Blood Pressure, Essential Hypertension, Hyperpiesia, Hyperpiesis, Hypertensive Disorder, Systemic Arterial Hypertension.
Dosing
No dosing information is available for this tab.
Felodipine is administered orally as extended-release tablets. The tablets should be swallowed intact and should not be chewed or crushed. Since peak concentrations of the drug were increased by 60% when felodipine was administered with a high-fat or high-carbohydrate meal and no changes in pharmacokinetics were observed when the drug was administered with a light meal (e.g., orange juice, toast, and cereal), the manufacturer states that felodipine should be taken either without food or with a light meal. However, the bioavailability of felodipine as determined by AUC was not affected when the extended-release tablets containing felodipine were administered with a high-fat or high-carbohydrate meal.
Concomitant administration with grapefruit juice has been shown to increase oral bioavailability of felodipine 2-fold compared with concomitant administration with orange juice or water. Concomitant oral administration of grapefruit juice usually should be avoided since potentially clinically important increases in hemodynamic effects can result.
Store extended-release tablets in a tightly closed container at 20-25degreesC; protect from light.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
Felodipine is metabolized by cytochrome P-450 (CYP) isoenzyme 3A4.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Known hypersensitivity to felodipine or any ingredient in the formulation.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
The most common adverse reactions to oral felodipine are peripheral edema, headache, and flushing.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Although safety and efficacy are not established in children younger than 18 years of age, some experts have recommended oral pediatric dosages+ for hypertension based on clinical experience.
Animal studies indicate felodipine crosses the placenta.
Digital anomalies consisting of reduction in size and degree of ossification of the terminal phalanges have been observed in pregnant rabbits administered oral felodipine dosages from 0.46 to 4.6 mg/kg daily (from 0.8 to 8-times the maximum recommended human dose (MRHD) on a mg/m2 basis and patient body weight of 50 kg); the frequency and severity of such changes appear to be dose-related and noted even at the lowest dose. Similar anomalies were not observed in rats, however an abnormal position of the distal phalanges, but not a reduction in size, was noted in 40% of the fetuses when cynomolgus monkeys received felodipine during a teratology study.
Rats administered felodipine >=9.6 mg/kg daily (8-times MRHD on a mg/m2 basis and patient body weight of 50 kg) experienced prolonged parturition with difficult labor and increased frequency of fetal and postnatal death.
Rabbits administered felodipine >=1.2 mg/kg daily (2.1-times MRHD on a mg/m2 basis and patient body weight of 50 kg) experienced significant mammary gland enlargement in excess of the normal expected enlargement; this effect regressed during lactation and was not observed in rats or monkeys.
There are no adequate and well-controlled studies using felodipine in pregnant women. Women taking felodipine during pregnancy, or who become pregnant while taking felodipine, should be advised of the potential hazards to the fetus (e.g., digital anomalies of the infant), effects on labor and delivery, and on the woman's mammary glands.
It is not known whether felodipine is distributed into human milk. Because of the potential for serious adverse reactions in the infant, a decision should be made to discontinue nursing or the drug, taking into account the importance of the drug to the woman.
Dosage of felodipine should be adjusted carefully and blood pressure response should be closely monitored with each adjustment in geriatric patients; the usual initial dosage is 2.5 mg daily. In clinical trials, the risk of peripheral edema was increased substantially in geriatric patients receiving dosages exceeding 10 mg daily.
Clinical studies did not include sufficient numbers of patients 65 years of age and older to determine whether geriatric patients respond differently than younger adults. Compared to younger individuals, felodipine clearance is decreased and AUC increased in geriatric subjects; felodipine plasma concentrations increase with age following a single dose or at steady-state.
While other clinical experience generally has not revealed age-related differences in response or tolerance, drug dosage generally should be titrated carefully in geriatric patients, usually initiating therapy at the low end of the dosage range (2.5 mg daily) and adjusting as necessary based on patient response. The greater frequency of decreased hepatic, renal, and/or cardiac function and of concomitant disease and drug therapy observed in the elderly also should be considered.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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