This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.
Identification
- Summary
Landiolol is an ultra short-acting selective beta-blocker used for rapid ventricular rate control in cases of supraventricular tachycardia.
- Generic Name
- Landiolol
- DrugBank Accession Number
- DB12212
- Background
Landiolol is a rapid-acting beta-blocker used for rapid ventricular rate control.
- Type
- Small Molecule
- Groups
- Investigational
- Structure
Structure for Landiolol (DB12212)
- Weight
- Average: 509.6
Monoisotopic: 509.273715228 - Chemical Formula
- C25H39N3O8
- Synonyms
- Landiolol
- Landiololum
- External IDs
- AOP-200704
- AOP200704
- LDLL-600
- LDLL600
- ONO 1101
- ONO-1101
Pharmacology
- Indication
Not Available
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- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- 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
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbatacept The metabolism of Landiolol can be increased when combined with Abatacept. Abiraterone The metabolism of Landiolol can be decreased when combined with Abiraterone. Acebutolol Acebutolol may increase the arrhythmogenic activities of Landiolol. Aceclofenac Aceclofenac may decrease the antihypertensive activities of Landiolol. Acemetacin Acemetacin may decrease the antihypertensive activities of Landiolol. Acetaminophen The metabolism of Landiolol can be decreased when combined with Acetaminophen. Acetohexamide Landiolol may increase the hypoglycemic activities of Acetohexamide. Acetophenazine The serum concentration of Landiolol can be increased when it is combined with Acetophenazine. Acetylcholine The risk or severity of adverse effects can be increased when Landiolol is combined with Acetylcholine. Acetyldigitoxin Acetyldigitoxin may increase the arrhythmogenic activities of Landiolol. 
Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more - Food Interactions
- Not Available
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Landiolol hydrochloride G8HQ634Y17 144481-98-1 DLPGJHSONYLBKP-IKGOIYPNSA-N
Categories
- ATC Codes
- C07AB14 — Landiolol
- Drug Categories
- Adrenergic Agents
- Adrenergic Antagonists
- Adrenergic beta-Antagonists
- Agents causing hyperkalemia
- Amides
- Antiarrhythmic agents
- Antihypertensive Agents
- Beta Blocking Agents, Selective
- Bradycardia-Causing Agents
- Cardiovascular Agents
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 Substrates
- Neurotransmitter Agents
- Oxazines
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as morpholine carboxylic acids and derivatives. These are heterocyclic compounds containing a morpholine ring substituted by one or more carboxylic acid groups (or derivative thereof).
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Oxazinanes
- Sub Class
- Morpholines
- Direct Parent
- Morpholine carboxylic acids and derivatives
- Alternative Parents
- Phenoxy compounds / Phenol ethers / Ketals / Alkyl aryl ethers / Fatty acid esters / 1,3-dioxolanes / Ureas / Secondary alcohols / 1,2-aminoalcohols / Carboxylic acid esters show 10 more
- Substituents
- 1,2-aminoalcohol / Acetal / Alcohol / Alkyl aryl ether / Amine / Amino acid or derivatives / Aromatic heteromonocyclic compound / Azacycle / Benzenoid / Carbonic acid derivative show 26 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- 62NWQ924LH
- CAS number
- 133242-30-5
- InChI Key
- WMDSZGFJQKSLLH-RBBKRZOGSA-N
- InChI
- InChI=1S/C25H39N3O8/c1-25(2)35-18-22(36-25)17-34-23(30)8-5-19-3-6-21(7-4-19)33-16-20(29)15-26-9-10-27-24(31)28-11-13-32-14-12-28/h3-4,6-7,20,22,26,29H,5,8-18H2,1-2H3,(H,27,31)/t20-,22+/m0/s1
- IUPAC Name
- [(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl 3-{4-[(2S)-2-hydroxy-3-({2-[(morpholine-4-carbonyl)amino]ethyl}amino)propoxy]phenyl}propanoate
- SMILES
- CC1(C)OC[C@@H](COC(=O)CCC2=CC=C(OC[C@@H](O)CNCCNC(=O)N3CCOCC3)C=C2)O1
References
- General References
- BASG Product Information: Rapibloc (landiolol hydrochloride) for infusion [Link]
- External Links
- PubChem Compound
- 114905
- PubChem Substance
- 347828494
- ChemSpider
- 102855
- ChEBI
- 135809
- ChEMBL
- CHEMBL1742466
- ZINC
- ZINC000003929810
- Wikipedia
- Landiolol
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Recruiting Treatment Atrial Fibrillation / Surgery, Cardiac 1 3 Completed Diagnostic Coronary Artery Disease (CAD) 1 3 Completed Treatment Atrial Fibrillation 1 3 Not Yet Recruiting Treatment Septic Shock 1 3 Recruiting Prevention Atrial Fibrillation / Postoperative Complications 1 3 Recruiting Prevention Atrial Fibrillation / Surgery, Cardiac 1 2 Completed Diagnostic Coronary Artery Disease (CAD) 2 2 Completed Treatment Healthy Subjects (HS) / Pharmacokinetics/Dynamics Study 1 2 Completed Treatment Postoperative Supraventricular Tachyarrythmia 1 2, 3 Completed Treatment Postoperative Supraventricular Tachyarrythmia 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, powder, for solution Intravenous 600 MG Injection, solution, concentrate Intravenous 20 mg/2ml Injection, powder, for solution Intravenous 300 mg - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Not Available
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.334 mg/mL ALOGPS logP 0.44 ALOGPS logP 0.35 ChemAxon logS -3.2 ALOGPS pKa (Strongest Acidic) 14.04 ChemAxon pKa (Strongest Basic) 8.79 ChemAxon Physiological Charge 1 ChemAxon Hydrogen Acceptor Count 8 ChemAxon Hydrogen Donor Count 3 ChemAxon Polar Surface Area 127.82 Å2 ChemAxon Rotatable Bond Count 14 ChemAxon Refractivity 131.29 m3·mol-1 ChemAxon Polarizability 56.5 Å3 ChemAxon Number of Rings 3 ChemAxon Bioavailability 0 ChemAxon Rule of Five No ChemAxon Ghose Filter No ChemAxon Veber's Rule No ChemAxon MDDR-like Rule Yes ChemAxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- Sternieri E, Coccia CP, Pinetti D, Guerzoni S, Ferrari A: Pharmacokinetics and interactions of headache medications, part II: prophylactic treatments. Expert Opin Drug Metab Toxicol. 2006 Dec;2(6):981-1007. doi: 10.1517/17425255.2.6.981 . [Article]
- Brodde OE, Kroemer HK: Drug-drug interactions of beta-adrenoceptor blockers. Arzneimittelforschung. 2003;53(12):814-22. [Article]
- Iwaki M, Niwa T, Bandoh S, Itoh M, Hirose H, Kawase A, Komura H: Application of substrate depletion assay to evaluation of CYP isoforms responsible for stereoselective metabolism of carvedilol. Drug Metab Pharmacokinet. 2016 Dec;31(6):425-432. doi: 10.1016/j.dmpk.2016.08.007. Epub 2016 Sep 2. [Article]
Drug created at October 20, 2016 21:37 / Updated at May 21, 2021 10:28