Lercanidipine

JFDA label: Lercadip

Indications

Approved

• Cardiovascular Diseases — cardiovascular disease

Off-label

• Essential Hypertension
• Hypertension

Adverse Reactions

Cardiac disorders (3)

Common Palpitations · Tachycardia

Rare Angina pectoris

Vascular disorders (3)

Very Common Hypotension · Orthostatic hypotension

Common Flushing

Nervous system disorders (4)

Very Common Dizziness · Headache

Rare Gynaecomastia · Somnolence

Hepatobiliary disorders (4)

Common Foetor hepaticus · Hepatocellular injury · Liver disorder

Rare Hepatic failure

Renal and urinary disorders (2)

Uncommon Urinary tract disorder

Rare Polyuria

Blood and lymphatic system disorders (2)

Uncommon Anaemia

Rare Neutropenia

Metabolism and nutrition disorders (3)

Very Common Hyperkalaemia

Uncommon Diabetes mellitus · Hypoglycaemia

Gastrointestinal disorders (5)

Very Common Diarrhoea · Nausea

Uncommon Ileus

Rare Aphthous stomatitis · Stomatitis

Skin and subcutaneous tissue disorders (4)

Very Common Dermatitis · Rash

Uncommon Hyperhidrosis

Rare Erythema multiforme

Musculoskeletal and connective tissue disorders (3)

Uncommon Muscle spasms

Rare Musculoskeletal discomfort · Myalgia

Psychiatric disorders (1)

Uncommon Confusional state

Eye disorders (1)

Very Common Vision blurred

Reproductive system and breast disorders (1)

Uncommon Erectile dysfunction

Infections and infestations (1)

Uncommon Nasopharyngitis

Investigations (4)

Common Gamma-glutamyltransferase increased

Uncommon Blood urea increased · Feeling abnormal

Rare Urine output increased

General disorders and administration site conditions (8)

Very Common Angiopathy · Asthenia · Fatigue

Common Oedema peripheral

Uncommon Urethral disorder

Rare Glossitis · Mediastinal disorder · Oliguria

Respiratory, thoracic and mediastinal disorders (4)

Very Common Cough · Dyspnoea

Uncommon Rhinorrhoea

Rare Lung infiltration

Pregnancy & Lactation

Chemistry & Properties

Formula	C36H41N3O6
Molecular weight	611.74 g/mol
IUPAC name	5-O-[1-[3,3-diphenylpropyl(methyl)amino]-2-methylpropan-2-yl] 3-O-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
CAS	100427-26-7
PubChem CID	65866
InChIKey	ZDXUKAKRHYTAKV-UHFFFAOYSA-N
logP	6.48 (XLogP 6.9)
Polar surface area	111.01 Ų
H-bond acceptors / donors	8 / 1
Drug-likeness (QED)	0.14
Lipinski violations	2

SMILES

COC(=O)C1=C(C)NC(C)=C(C(=O)OC(C)(C)CN(C)CCC(c2ccccc2)c2ccccc2)C1c1cccc([N+](=O)[O-])c1

Biology & Pharmacokinetics

Pharmacokinetics

BBB penetrant	No

Enzyme interactions

Enzyme	Role	Detail
CYP1A2	Substrate	—
CYP2B6	Inhibitor	—
CYP2C19	Inhibitor	—
CYP2C19	Substrate	—
CYP2C8	Inhibitor	—
CYP2C9	Inhibitor	—
CYP2D6	Inhibitor	—
CYP2D6	Substrate	—
CYP3A4	Inhibitor	—
CYP3A4	Substrate	—

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Registered Products (4)

Brand	Form / strength	Pack	Agent	Citizen (JOD)
Trolin 10mg F.c Tab	Film-Coated Tablet 10 mg	30 tab	UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN	6.880
Lercadip	Tablet 10 mg	30 tab	Adatco Drug Store	7.640
Trolin 20mg F.C Tab	Film-Coated Tablet 20 mg	30 tab	UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN	8.220
Lercadip	Tablet 20 mg	30 tab	Adatco Drug Store	9.130