Felodipine

Dihydropyridine Calcium Channel Blocker — CARDIOVASCULAR SYSTEM

Key facts

Felodipine is an ofp drug in the Dihydropyridine Calcium Channel Blocker class catalogued in DrugCentral. It was first approved by the FDA in 1991. Its mechanism of action is classified as Calcium Channel Antagonists. DrugCentral lists 9 molecular targets, including CFTR, AOX1 and ADORA3. Recorded indications include Hypertensive disorder.

• Approval status: ofp (first approved 1991 by the FDA).
• Drug class: Dihydropyridine Calcium Channel Blocker.
• Mechanism of action: Calcium Channel Antagonists.
• Molecular targets: CFTR, AOX1, ADORA3 and CYP2C9 (9 listed in DrugCentral).
• Indications: Hypertensive disorder.
• ATC code: C07FB02 (Beta blocking agents and calcium channel blockers).
• Molecular formula: C18H19Cl2NO4; molecular weight 384.25 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Hypertensive disorder

Off-label uses (3)

• Angina pectoris
• Prinzmetal angina
• Raynaud's phenomenon

Contraindications (23)

• Acute cerebrovascular insufficiency
• Angioedema
• Aortic valve stenosis
• Bone marrow depression
• Chronic heart failure
• Chronic idiopathic constipation
• Coronary arteriosclerosis
• Disease of liver
• Disorder of connective tissue
• Hemodialysis with High-Flux Membrane
• Hereditary angioneurotic edema
• Hyperkalemia
• Hypertrophic cardiomyopathy
• Hyponatremia
• Immunosuppression
• Kidney disease
• Low blood pressure
• Myocardial infarction
• Neutropenic disorder
• Peripheral edema
• Pregnancy, function
• Renal artery stenosis
• Transplantation

Mechanism & targets

• Mechanism of action (MoA): Calcium Channel Antagonists
• Established pharmacologic class: Dihydropyridine Calcium Channel Blocker

Molecular targets (9)

Target	Gene	Action	Activity
Cystic fibrosis transmembrane conductance regulator	CFTR	activator	Ki 8.40
Aldehyde oxidase	AOX1	unknown	IC50 6.52
Adenosine receptor A3	ADORA3	unknown	Ki 6.22
Cytochrome P450 2C9	CYP2C9	unknown	IC50 5.34
Bile acid receptor	NR1H4	unknown	IC50 5.30
Voltage-dependent T-type calcium channel subunit alpha-1H	CACNA1H	unknown	Ki 5.17
Sodium channel alpha subunits; brain (Types I, II, III)	SCN1A|SCN2A|SCN3A	unknown	IC50 4.43
Voltage-dependent L-type calcium channel subunit alpha-1C	CACNA1C	blocker	—
Voltage-dependent L-type calcium channel subunit alpha-1D	CACNA1D	blocker	—

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1991-07-25	FDA	—	ASTRAZENECA

ATC classification

ATC code	Therapeutic hierarchy
C07FB02	CARDIOVASCULAR SYSTEM › BETA BLOCKING AGENTS › BETA BLOCKING AGENTS, OTHER COMBINATIONS › Beta blocking agents and calcium channel blockers
C08CA02	CARDIOVASCULAR SYSTEM › CALCIUM CHANNEL BLOCKERS › SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS › Dihydropyridine derivatives
C09BB05	CARDIOVASCULAR SYSTEM › AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM › ACE INHIBITORS, COMBINATIONS › ACE inhibitors and calcium channel blockers

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Cardiospasm	746.1
Palmoplantar keratoderma	717.5
Pruritus genital	678.1
Sleep terror	658.3
Carotid artery occlusion	623.3
Tension headache	612.6
Atrial tachycardia	610.2
Tinnitus	559.2
Anosmia	537.7
Facial pain	508.2
Immunisation	479.5
Pain of skin	466.8

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Felodipine is on its molecule page.

• Molecular formula: C₁₈H₁₉Cl₂NO₄
• Molecular weight: 384.25 g/mol
• CAS number: 72509-76-3
• InChIKey: RZTAMFZIAATZDJ-UHFFFAOYSA-N
• PubChem CID: 3333

CCOC(=O)C1=C(C)NC(C)=C(C1C1=C(Cl)C(Cl)=CC=C1)C(=O)OC

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Felodipine used for?

DrugCentral lists the following indications for Felodipine: Hypertensive disorder.

How does Felodipine work?

Felodipine is classified as Calcium Channel Antagonists; its molecular targets in DrugCentral include CFTR (activator), AOX1, ADORA3 and CYP2C9.

When was Felodipine first approved?

Felodipine was first approved by the FDA in 1991.

What drug class does Felodipine belong to?

Felodipine is in the Dihydropyridine Calcium Channel Blocker class.

What is the chemical formula of Felodipine?

Felodipine has the molecular formula C18H19Cl2NO4 and a molecular weight of 384.25 g/mol.

Sources

• DrugCentral drug card 1142 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1480 — compound record and bioactivity
• PubChem CID 3333 — chemical identifiers
• DrugBank DB01023 — drug record
• FDA UNII OL961R6O2C — substance identity
• DailyMed: FDA labels for Felodipine — current prescribing information (label search)
• UniProt P13569 (CFTR) — target protein
• UniProt Q06278 (AOX1) — target protein
• UniProt P0DMS8 (ADORA3) — target protein
• UniProt P11712 (CYP2C9) — target protein
• UniProt Q96RI1 (NR1H4) — target protein
• UniProt O95180 (CACNA1H) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.