Felodipine

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Cat Number

API72509763

CAS Number

72509-76-3

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CAS Number

72509-76-3

EINECS

620-472-7

Storage

Store at 2-8°C

Synonyms

Plendil; Flodil; Modip; Felodipina; Preslow; Felodipinum

Molecular Formula

C18H19Cl2NO4

Molecular Weight

384.2

Smiles

CCOC(=O)C1=C(NC(=C(C1C2=C(C(=CC=C2)Cl)Cl)C(=O)OC)C)C

Appearance

White to light orange powder to crystal

Melting Point

142-145°C

Boiling Point

471.5±45.0°C at 760 mmHg

Relative Density

1.3±0.1

General Description

Felodipine is a synthetic dihydropyridine derivative, a calcium channel blocker, with a dichlorophenyl group. Its chemical structure is 3,5-pyridinedicarboxylic acid, 4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-, ethyl methyl ester. Felodipine is a yellow crystalline powder, practically insoluble in water but soluble in organic solvents. It is a potent vasodilator with high vascular selectivity.

Mechanism of Action

Felodipine acts as a calcium channel blocker by binding to the L-type calcium channels in the smooth muscle cells of the arterial wall, reducing calcium influx and causing vasodilation. This leads to a decrease in peripheral vascular resistance and a reduction in blood pressure. The drug has minimal effect on cardiac contractility and conduction at therapeutic doses.

Application

Felodipine is indicated for the treatment of hypertension, either as monotherapy or in combination with other antihypertensive agents. It is also used for the treatment of chronic stable angina. The drug is effective in lowering blood pressure and improving exercise tolerance, and it is generally well-tolerated.

Felodipine, a dihydropyridine Ca²⁺ channel blocker, inhibited TGF‑β1‑induced collagen production in fibroblasts and prevented bleomycin‑induced pulmonary fibrosis in mice when given intratracheally, even after fibrosis developed. Other dihydropyridines (nifedipine, benidipine) showed similar effects. Ca²⁺ channel blockers may be therapeutically beneficial for idiopathic pulmonary fibrosis.

Fig. 1 Effect of felodipine on bleomycin-induced pulmonary fibrosis, alteration of lung mechanics, and respiratory dysfunction. (Tanaka KI, et al., 2017)

References

Tanaka KI, et al. Protective and therapeutic effect of felodipine against bleomycin-induced pulmonary fibrosis in mice. Sci Rep. 2017;7(1):3439.

In a crossover study of 12 healthy Chinese subjects, co‑administration of enalapril and felodipine did not affect enalapril pharmacokinetics but altered felodipine exposure (AUC ratio 1.14, Cmax ratio 0.80). No severe adverse events occurred. While statistically significant, the pharmacokinetic changes are unlikely to be clinically meaningful given the safety profile observed.

Fig. 2 Study design and disposition of subjects. (Li D, et al., 2017)

References

Li D, et al. Pharmacokinetics and drug-drug interaction between enalapril, enalaprilat and felodipine extended release (ER) in healthy subjects. Oncotarget. 2017;8(41):70752-70760.

Does Felodipine require protection from light and heat during storage?

Yes, it is highly sensitive to light and heat. Light causes photodegradation and heat accelerates oxidation of the 1,4-dihydropyridine ring. Store in light-resistant containers at 2–8°C.

Is Felodipine stable in extended-release tablet formulations?

Yes, when formulated with antioxidants and moisture-protective packaging.

What is the recommended packaging for Felodipine to prevent degradation?

Use amber glass or opaque containers with tight closures, filled to minimize headspace. Protect from light and store in refrigerated conditions during transport.

How is the impurity felodipine pyridine (an oxidation product) monitored?

This primary degradation product is specifically quantified using a stability-indicating HPLC method, ensuring it remains within pharmacopoeial limits.