Pilsicainide

This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification

Generic Name
Pilsicainide
DrugBank Accession Number
DB12712
Background

Pilsicainide has been investigated for the treatment of Paroxysmal Atrial Fibrillation.

Type
Small Molecule
Groups
Investigational
Structure
Thumb
Weight
Average: 272.392
Monoisotopic: 272.188863401
Chemical Formula
C17H24N2O
Synonyms
  • Pilsicainida
  • Pilsicainide
  • Pilsicaïnide
  • Pilsicainidum
  • Pilzicainide

Pharmacology

Indication

Not Available

Pharmacology
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Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Not Available

Mechanism of action
Not Available
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
Adverseeffects
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AcebutololAcebutolol may increase the arrhythmogenic activities of Pilsicainide.
AcetyldigitoxinAcetyldigitoxin may increase the arrhythmogenic activities of Pilsicainide.
AcrivastineThe risk or severity of QTc prolongation can be increased when Acrivastine is combined with Pilsicainide.
AdenosineAdenosine may increase the arrhythmogenic activities of Pilsicainide.
AjmalineAjmaline may increase the arrhythmogenic activities of Pilsicainide.
AlfuzosinThe risk or severity of QTc prolongation can be increased when Alfuzosin is combined with Pilsicainide.
AlimemazineThe risk or severity of QTc prolongation can be increased when Alimemazine is combined with Pilsicainide.
AmantadineThe risk or severity of QTc prolongation can be increased when Amantadine is combined with Pilsicainide.
AmifampridineThe risk or severity of QTc prolongation can be increased when Pilsicainide is combined with Amifampridine.
AmiodaroneThe risk or severity of adverse effects can be increased when Amiodarone is combined with Pilsicainide.
Interactions
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Food Interactions
Not Available

Products

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Product Ingredients
IngredientUNIICASInChI Key
Pilsicainide hydrochloride03C8I9296V88069-49-2NZOSVDHCTCLGEB-UHFFFAOYSA-N
International/Other Brands
Sunrythm

Categories

Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as beta amino acids and derivatives. These are amino acids having a (-NH2) group attached to the beta carbon atom.
Kingdom
Organic compounds
Super Class
Organic acids and derivatives
Class
Carboxylic acids and derivatives
Sub Class
Amino acids, peptides, and analogues
Direct Parent
Beta amino acids and derivatives
Alternative Parents
Anilides / m-Xylenes / Pyrrolizidines / N-arylamides / N-alkylpyrrolidines / Trialkylamines / Secondary carboxylic acid amides / Azacyclic compounds / Organopnictogen compounds / Organic oxides
show 2 more
Substituents
Amine / Anilide / Aromatic heteropolycyclic compound / Azacycle / Benzenoid / Beta amino acid or derivatives / Carbonyl group / Carboxamide group / Hydrocarbon derivative / M-xylene
show 16 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available
Affected organisms
Not Available

Chemical Identifiers

UNII
AV0X7V6CSE
CAS number
88069-67-4
InChI Key
BCQTVJKBTWGHCX-UHFFFAOYSA-N
InChI
InChI=1S/C17H24N2O/c1-13-6-3-7-14(2)16(13)18-15(20)12-17-8-4-10-19(17)11-5-9-17/h3,6-7H,4-5,8-12H2,1-2H3,(H,18,20)
IUPAC Name
N-(2,6-dimethylphenyl)-2-(hexahydro-1H-pyrrolizin-7a-yl)acetamide
SMILES
CC1=CC=CC(C)=C1NC(=O)CC12CCCN1CCC2

References

General References
Not Available
KEGG Drug
D08377
PubChem Compound
4820
PubChem Substance
347828910
ChemSpider
4654
BindingDB
50413638
ChEBI
135127
ChEMBL
CHEMBL163238
ZINC
ZINC000049925459
Wikipedia
Pilsicainide

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
Not AvailableUnknown StatusTreatmentParoxysmal Atrial Fibrillation (PAF)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Not Available
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.389 mg/mLALOGPS
logP2.36ALOGPS
logP3.16ChemAxon
logS-2.8ALOGPS
pKa (Strongest Acidic)14.44ChemAxon
pKa (Strongest Basic)10.46ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area32.34 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity83.77 m3·mol-1ChemAxon
Polarizability31.16 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Transporter activity
Specific Function
Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
Gene Name
ABCB11
Uniprot ID
O95342
Uniprot Name
Bile salt export pump
Molecular Weight
146405.83 Da
References
  1. Pedersen JM, Matsson P, Bergstrom CA, Hoogstraate J, Noren A, LeCluyse EL, Artursson P: Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43. doi: 10.1093/toxsci/kft197. Epub 2013 Sep 6. [Article]

Drug created on October 20, 2016 23:45 / Updated on February 21, 2021 18:53