Delving into the Latest Updates on Carteolol Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Carteolol, Carteolol hydrochloride (JP17/USP)

+ [13]

Target

β1-adrenergic receptor x β2-adrenergic receptor x β3-adrenergic receptor

Mechanism

β1-adrenergic receptor antagonists(Beta-1 adrenergic receptor antagonists), β2-adrenergic receptor antagonists(Beta-2 adrenergic receptor antagonists), β3-adrenergic receptor antagonists(Beta-3 adrenergic receptor antagonists)

Therapeutic Areas

Nervous System DiseasesCardiovascular DiseasesEye Diseases

Active Indication

GlaucomaCataractOcular Hypertension+ [3]

Inactive Indication-

Originator Organization

Otsuka Pharmaceutical Co., Ltd.

Active Organization

Otsuka Pharmaceutical Co., Ltd.

China Otsuka Pharmaceutical Co., Ltd.

Inactive Organization

Novartis Pharmaceuticals Corp.

AbbVie, Inc.

Drug Highest PhaseApproved

First Approval Date

JP (25 Oct 1980),

Angina PectorisArrhythmias, CardiacHypertension

Regulation-

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Structure

Molecular FormulaC16H24N2O3

InChIKeyLWAFSWPYPHEXKX-UHFFFAOYSA-N

CAS Registry51781-06-7

View All Structures (2)

AbstractBeta blockers are a class of drugs commonly used to treat heart‐related diseases; they are also regulated under the World Anti‐Doping Agency. Tandem mass spectrometry is often used in the pharmaceutical industry, clinical analysis laboratory, and antidoping laboratory for detection and characterization of drugs and their metabolites. A deeper chemical understanding of dissociation pathways may eventually lead to an improved ability to predict tandem mass spectra of compounds based strictly on their chemical structure (or vice versa), which is especially important for characterization of unknowns such as emerging designer drugs or novel metabolites. In addition to providing insights into dissociation pathways, the use of energy‐resolved breakdown curves can produce improved selectivity and lend insights into optimal fragmentation conditions for liquid chromatography‐tandem mass spectrometry LC–MS/MS workflows. Here, we perform energy‐resolved collision cell and multistage ion trap collision‐induced dissociation‐mass spectrometry (CID‐MS) experiments, along with complementary density functional theory calculations, on five beta blockers (acebutolol, atenolol, bisoprolol, carteolol, and labetalol), to better understand the details of the pathways giving rise to the observed MS/MS patterns. Results from this work are contextualized within previously reported literature on these compounds. New insights into the formation of the characteristic product ion m/z 116 and the pathway leading to characteristic loss of 77 u are highlighted. We also present comparisons of breakdown curves obtained via qToF, quadrupole ion trap, and in‐source CID, allowing for differences between the data to be noted and providing a step toward allowing for improved selectivity of breakdown curves to be realized on simple instruments such as single quadrupoles or ion traps.

01 Nov 2023·Japanese Journal of Ophthalmology

Persistence of the carteolol hydrochloride/latanoprost fixed-combination ophthalmic solution, compared with the other β-blocker/prostanoid FP receptor agonist fixed-combination ophthalmic solutions

Article

Author: Kashiwagi, Kenji ; Shibasaki, Yoshiyuki ; Suginaka, Masaki ; Ouchi, Kentaro

PURPOSETo investigate the treatment persistence of carteolol hydrochloride/latanoprost fixed-combination ophthalmic solution (CAR/LAT) and other β-blocker/prostanoid FP receptor agonist fixed-combination ophthalmic solutions (BB/FP) in the treatment of glaucoma.STUDY DESIGNRetrospective observational cohort study.METHODSA retrospective observational cohort study using JMDC Claims Database. Patients aged 20 years or older diagnosed with glaucoma between February 1, 2017, and March 31, 2020, and prescribed CAR/LAT or another BB/FP were included.RESULTSA total of 16,612 patients (7423 in the CAR/LAT group and 9189 in the other BB/FP group) were included. The cumulative treatment persistence rate at the end of follow-up was 42.0% (64.9% at 1 year, 53.4% at 2 years, 45.0% at 3 years, and 42.0% at 4 years) in the CAR/LAT group and 34.7% (54.8% at 1 year, 43.6% at 2 years, 37.1% at 3 years, and 34.7% at 4 years) in the other BB/FP group. Treatment persistence was significantly longer in the CAR/LAT group compared to that in the other BB/FP group (hazard ratio 0.747, p < 0.0001). Over the treatment period, the number of patients who discontinued treatment was 3281 (44.2%) in the CAR/LAT group and 4926 (53.6%) in the other BB/FP group; the median duration of treatment was 135 days and 97 days, respectively.CONCLUSIONThe study results suggest that persistence rates vary depending on the BB/FP and CAR/LAT appears to be more persistent than other BB/FP.

01 Sep 2023·Internal Medicine

Life-threatening Vasospastic Angina Induced by Carteolol Eye Drops

Article

Author: Maemura, Koji ; Kawano, Hiroaki ; Suzuki, Ayaka ; Akashi, Ryohei ; Ikeda, Satoshi ; Eto, Ryo

Vasospastic angina (VSA) can be worsened by oral nonselective beta-blockers. Ophthalmic carteolol eye drops are nonselective beta-blockers and effective against glaucoma and ocular hypertension. Systemic effects of ophthalmic beta-blockers on VSA have not yet been reported. We herein report a case of VSA that developed after a patient started carteolol eye drops for ocular hypertension. Even though benidipine, a calcium channel blocker, was started, a VSA attack with incessant non-sustained ventricular tachycardia occurred. Once the carteolol eyedrops were discontinued, the VSA resolved. This case demonstrates that carteolol eye drops can induce life-threatening VSA.

100 Deals associated with Carteolol Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
D00599	Carteolol Hydrochloride	S01ED05 C07AA15	DB00521

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Glaucoma	CN	China Otsuka Pharmaceutical Co., Ltd.	01 Jan 1995
Cataract	JP	Otsuka Pharmaceutical Co., Ltd.	15 Feb 1984
Ocular Hypertension	JP	Otsuka Pharmaceutical Co., Ltd.	15 Feb 1984
Angina Pectoris	JP	Otsuka Pharmaceutical Co., Ltd.	25 Oct 1980
Arrhythmias, Cardiac	JP	Otsuka Pharmaceutical Co., Ltd.	25 Oct 1980
Hypertension	JP	Otsuka Pharmaceutical Co., Ltd.	25 Oct 1980