DrugInfoSys

Felodipine

Drug #299

Felodipine is a calcium channel blocker. It lowers the blood pressure by blocking calcium, relaxes the heart muscle and dilates the heart blood vessels. It has been known since the late 1800s that calcium influx was necessary for the contraction of muscle. The discovery of calcium channel in a cardiac muscle was followed by the finding of several diffent type of calcium channel in diffrent tissues. These discoveries provided the necessary mechanisms for the triggering of cardiac and smooth muscle contraction. The discovery of these channels also made possible the developemnet of clinically useful blocking drugs.

Primary Characteristics

It is of Synthetic origin and belongs to Dihydropyridine.

It belongs to Calcium L-channel antagonist pharmacological group on the basis of mechanism of action.

Molecular Weight: 384.2 · pKa: <1 · Solubility in Water: <1 in 10000000 · Solubility in Alcohol: high · Non-proprietary name: Felodipine.

Molecular structure of Felodipine

Pharmacokinetics

Absorption: Felodipine has an oral bioavailability is 100%, pre-systemic (first-pass) metabolism accounts for 85%.

Distribution: Felodipine has a volume of distribution is 10 l/kg. plasma protein binding is >99%.

Elimination: it is metabolised via complete, plasma half-life is 25 hr, renal excretion is major.

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Indications

Felodipine is primarily indicated in conditions like Angina, Hypertension, Prophylaxis of angina.

Contraindications

None recorded.

Dosage

Felodipine's dosage details are as follows:

DoseSingle DoseFrequencyRouteInstructions
Adult Dosage
2.5 – 20 mgEvery 24hPOMaintenance
5 mg5 mgEvery 24hPOInitial
Paediatric Dosage (20kg)
0 – 0Not Recommended in this Age Group
Neonatal Dosage (3kg)
0 – 0Not recommended in this age group

Drug Interactions

Unknown7 interactions
3 interactions
Major2 interactions
Moderate1 interaction

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

The signs and symptoms that are produced after acute overdosage of Felodipine are Bradycardia, Hypotension, Excessive peripheral vasodilation.

Felodipine is known to cause more or less tolerable side effects which are usually transient. These include Ankle swelling, dizziness, Fatigue, Flushing, Headache, Palpitation, Pruritus , Rashes .

Warnings / Precautions

Felodipine should be used with caution in patients with pre-existing heart disease or liver disease.This drug should be used only if clearly needed during pregnancy or lactation. Limit alcohol while taking this medication because it can enhance dizziness. Avoid drinking grapefruit juice at the same time when take this medication.This medication may cause enlargement of the gums, this can be minimized by maintaining good oral hygiene with regular brushing, flossing and massaging of the gums.

Interference in Pathology

Felodipine may interfere in the diagnosis of Increased in Serum Aminotransferase.

Available Brands

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Single Ingredient

Storage Conditions

Felodipine should be stored Tab.

Drug Classification

  1. 1.12.3.2Calcium antagonists

Manufacturers

Manufacturers of Felodipine in Pakistan: