Mikelan (carteolol) / Senju - LARVOL DELTA

Predicting compounds that interact with the 2 known agonist-induced conformations of the human β1-adrenoceptor. (PubMed, Mol Pharmacol) - "Using a structure-activity hypothesis built on the predicted poses CGP12177 and 3 biphasic agonists (alprenolol, oxprenolol, and bucindolol), predictions based on ligand similarity and structural compatibility reasoning were made about 11 other β1-ligands not yet tested for secondary conformation interaction and examined in radioligand binding and functional assays using human β1- and β2-adrenoceptors...Carteolol (related to CGP12177) and bunitrolol (similar to alprenolol) activated both conformations with biphasic concentration responses...In a β1-adrenoceptor mutant (β1-V189T-L195Q-W199Y) where secondary site CGP12177 and pindolol interaction is lost, the 3 novel secondary-site compounds were also no longer able to stimulate secondary conformation responses, suggesting that there is a common TM4 secondary conformation-inducing interaction site. SIGNIFICANCE STATEMENT: The β1-adrenoceptor exists in 2 agonist-stabilized, pharmacologically distinguishable conformations...."

Journal

Efficacy of Topical 2% Carteolol in the Treatment of Infantile Hemangiomas: A Dermoscopic and Clinical Evaluation (EADV 2025) - "While systemic propranolol is the first-line treatment, its potential for systemic side effects raises interest in topical therapies. Topical 2% carteolol is an effective and safe treatment for IH. Dermoscopic monitoring provides valuable insights into treatment progression, showing significant changes in erythema, clod, and vascular patterns. The presence of dotted vessels at baseline may serve as a predictor of a favorable treatment response."

Clinical • Dermatology

Association of Gut Microbiota and Metabolites With Thalidomide-Induced Antiemetic Efficacy in Small Cell Lung Cancer Patients (IASLC-WCLC 2025) - P3 | "A previous study (CLOG1302 study, NCT02203253) confirmed that thalidomide (THD) combined with palonosetron and dexamethasone could significantly improve the complete response rate of delayed CINV after hyperemetogenic chemotherapy with good safety...Metabolomic profiling identified higher levels of Hydrogenated MDI ( P <0.05), Carteolol ( P <0.05), Becocalcidiol ( P <0.05), B-Octylglucoside ( P <0.05), and Azelaic acid ( P <0.05) in the C group. KEGG pathway analysis highlighted significant differences in Neomycin, kanamycin, and gentamicin biosynthesis and Tryptophan metabolism. Conclusions : These findings suggest that THD may alleviate CINV in SCLC patients by modulating gut microbiota and associated metabolites. Gut microbiota composition and metabolite profiles may correlate with THD antiemetic efficacy, positioning them as potential predictive biomarkers and therapeutic targets for optimizing CINV management in SCLC patients treated with THD."

Clinical • Gut Microbiota • Chemotherapy-Induced Nausea and Vomiting • Lung Cancer • Oncology • Small Cell Lung Cancer • Solid Tumor

Atrioventricular Block Caused by Carteolol Eye Drops Administered to Unilateral Eye or Bilateral Eyes: A Case Report. (PubMed, Cureus) - "The pacemaker implantation was deferred, and he is currently under close follow-up. Depending on the amount administered to a unilateral eye or bilateral eyes, topical carteolol eye drops can cause second- or third-degree AV block."

Journal • Cardiovascular • Diabetes • Hypotension • Metabolic Disorders • Ophthalmology • Type 2 Diabetes Mellitus

0.01% atropine combined with carteolol hydrochloride can inhibit the scleral remodeling in guinea pigs with form-deprivation myopia. (PubMed, Sci Rep) - "We found that 0.01% atropine combined with carteolol hydrochloride refined mitochondrial dysfunction-induced extracellular matrix degradation by activating the PGC-1α/NRF2/HO-1 signaling pathway, thereby suppressing scleral remodeling and the progression of form-deprivation myopia in guinea pigs. In conclusion, 0.01% atropine combined with carteolol hydrochloride may be an effective strategy for the treatment of myopia."

Journal • Metabolic Disorders • Ophthalmology

Drugs for open-angle glaucoma. (PubMed, Med Lett Drugs Ther) - No abstract available

Journal • Glaucoma • Ophthalmology

Efficacy of topical 2% carteolol in the treatment of infantile hemangiomas: a dermoscopic and clinical evaluation. (PubMed, Arch Dermatol Res) - "While systemic propranolol is the first-line treatment, its potential for systemic side effects raises interest in topical therapies. The presence of dotted vessels at baseline may serve as a predictor of a favorable treatment response. Further studies with longer follow-up are needed to validate these findings."

Journal • Dermatology • Oncology

Toward a personalized chronotherapy of blood pressure. (PubMed, Biomed J) - "Personalized optimization of treatment timing to best match a healthy circadian BP pattern is recommended, guided by chronobiological analyses of ABPM data collected over several days in view of the large day-to-day variability in all features of the 24-hour BP rhythm."

Journal

Adrenaline enhances nociceptive and motor blockades by intrathecal carteolol and oxprenolol in rats. (PubMed, Fundam Clin Pharmacol) - "Carteolol and oxprenolol are more effective than propranolol on spinal blockades, while other beta-blockers are relatively ineffective. Compared to propranolol, the duration of action of carteolol and oxprenolol is longer or the same. Epinephrine enhances spinal blockades of carteolol, oxprenolol, and propranolol, suggesting that alpha-adrenergic receptors may play an important role in enhancing the anti-nociceptive effects of beta-blockers."

Journal • Preclinical

Genotypic and phenotypic analysis of an oculocutaneous albinism patient: a case report and review of the literature. (PubMed, J Med Case Rep) - "We report a patient with oculocutaneous albinism combined with cataract and secondary angle closure, and whole-exome sequencing suggested that he harbored TYR gene variants. Comprehensive examinations were important for identifying the causes of angle closure and making proper treatment strategies. Genetic testing enabled precise diagnosis and genetic counseling."

Journal • Review • Achromatopsia • Cardiovascular • Cataract • Glaucoma • Ophthalmology

A national analysis of systemic adverse events of beta-blockers used for glaucoma therapy. (PubMed, Cutan Ocul Toxicol) - "To evaluate systemic complications for timolol, carteolol, levobunolol, and/or betaxalol by using an FDA Federal Adverse Event Reporting System (FAERS). No allergic, endocrine, constitutional, or gastrointestinal symptoms generated positive signals. β-blocker use in glaucoma therapy can be rarely associated with serious systemic and life-threatening complications."

Adverse events • Journal • Cardiovascular • Gastrointestinal Disorder • Glaucoma • Ophthalmology • Pulmonary Disease

Timing and Efficacy Evaluation of 755-nm Long Pulse Alexandrite Laser and 2% Carteolol Hydrochloride Eye Drops Co-Treatment for Thicker Superficial Infantile Hemangioma. (PubMed, Clin Cosmet Investig Dermatol) - "Compared with the 3-12M group, ≤ 3 months can achieve better efficacy, requires a shorter treatment time, less likely to leave permanent skin lesions such as scars. Moreover, patients with no proliferation can be observed to 1 month."

Journal

Effect of treatment with carteolol and latanoprost in newly diagnosed primary open-angle glaucoma on peripapillary vessel density. (PubMed, Biomed Pap Med Fac Univ Palacky Olomouc Czech Repu) - "Carteolol had a better effect on vessel density than latanoprost."

Journal • Glaucoma • Ophthalmology

Further exploration of the collision-induced dissociation of select beta blockers: Acebutolol, atenolol, bisoprolol, carteolol, and labetalol. (PubMed, J Mass Spectrom) - "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."

Journal

Persistence of the carteolol hydrochloride/latanoprost fixed-combination ophthalmic solution, compared with the other β-blocker/prostanoid FP receptor agonist fixed-combination ophthalmic solutions. (PubMed, Jpn J Ophthalmol) - "The study results suggest that persistence rates vary depending on the BB/FP and CAR/LAT appears to be more persistent than other BB/FP."

Journal • Glaucoma • Ophthalmology

Carteolol triggers senescence via activation of β-arrestin-ERK-NOX4-ROS pathway in human corneal endothelial cells in vitro. (PubMed, Chem Biol Interact) - "The excess ROS also impair DNA to activate the DNA damage response (DDR) pathway of ATM-p53-p21 with diminished poly(ADP-Ribose) polymerase (PARP) 1, a NAD-dependent enzyme for DNA damage repair, resulting in cell cycle arrest and subsequent DDR-mediated senescence. Taken together, carteolol induces excess ROS to trigger HCEnC senescence via metabolic disturbance and DDR pathway."

Journal • Preclinical • Glaucoma • Metabolic Disorders • Ophthalmology • CCL27 • CDKN1A • CXCL8 • IL10 • IL6 • NOX4 • PARP1 • TGFB1 • TNFA

Further Characterization of a Spontaneous Glaucoma Model in Non-human Primates with Intraocular Pressure Lowering Agents (ARVO 2023) - "These animals were eye-drop dosed once a day for 7 days with either a negative control, a beta-adrenergic receptor blocking agent (carteolol hydrochloride or timolol maleate), a muscarinic agonist (pilocarpine nitrate), a selective alpha-2 adrenergic receptor agonist (brimonidine tartrate), a carbonic anhydrase inhibitor (brinzolamide), or a synthetic prostamide analog (bimatoprost or Travoprost) with a washout period of at least 7 days before cross-over. Describe the big picture and the implications of your findings, not the study itself and the associated details. Non-human primates spontaneous glaucoma model can be utilized for PK/PD studies of IOP lowering drugs"

Glaucoma • Ocular Inflammation • Ophthalmology • Optic Neuritis

A comparative study between a transscleral sustained-release device and eyedrops on intraocular distribution of carteolol hydrochloride. (PubMed, Heliyon) - "In conclusion, transscleral drug delivery may be a useful method for the reduction of IOP. Notably, the aqueous concentration must be equal to that delivered by the eyedrops, and this approach might be preferable for drug delivery to the posterior segment of the eye."

Journal

Frequent self-monitoring of intraocular pressure can determine effectiveness of medications in eyes with normal tension glaucoma: A case report. (PubMed, Medicine (Baltimore)) - "We conclude that frequent self-measurements of the IOP can determine that small changes of the IOPs are significant."

Journal • Glaucoma • Ophthalmology

Aqueous liquid chromatography with mobile phases of sodium dodecyl sulphate and ionic liquid. (PubMed, J Chromatogr A) - "In this work, the chromatographic behavior of six basic compounds of pharmaceutical interest, the β-adrenoceptor antagonists acebutolol, atenolol, carteolol, metroprolol, oxprenolol and propranolol, is examined. In order to assess the chromatographic behavior of the mixed mobile phases containing SDS and IL, changes in retention, peak profile and resolution of mixtures of the analytes were explored at varying concentration of the additives."

Journal

A Case of Life-threatening Vasospastic Angina Induced by Carteolol Eye Drops. (PubMed, Intern Med) - "Even though benidipine, a calcium channel blocker. Once the carteolol eyedrops were discontinued, the VSA resolved. This case demonstrates that carteolol eye drops can induce life-threatening VSA."

Journal • Cardiovascular • Glaucoma • Ophthalmology • Ventricular Tachycardia

Beta-blocker carteolol and oxprenolol produce cutaneous analgesia in response to needle pinpricks in the rat. (PubMed, Neurol Res) - "Using a rat model of infiltrative cutaneous analgesia, the effect of 5 beta-blockers (oxprenolol, carteolol, butaxamine, metoprolol, and acebutolol) and bupivacaine was compared and eventually combined with epinephrine. Oxprenolol produced a similar duration of action when compared to bupivacaine, while carteolol had a greater duration of action than bupivacaine. Cutaneous analgesia of oxprenolol (or carteolol) plus adrenaline was greater than that of bupivacaine plus adrenaline."

Journal • Preclinical • Anesthesia • Pain

Therapeutic potential of pupilloplasty combined with phacomulsification and intraocular lens implantation against uveitis-induced cataract. (PubMed, Int J Ophthalmol) - "PPI improves the visual gain and prevents the long-term recurrence of uveitis in patients with uveitis-induced cataract, including those with preoperative intraocular pressure abnormality (glaucoma) and inflammation (active uveitis). Uveitis presents stroma atrophy, pigment cell hyperplasia, and inflammatory cell infiltration, even in a quiet state."

Journal • Ankylosing Spondylitis • Cataract • Glaucoma • Hematological Disorders • Immunology • Inflammation • Inflammatory Arthritis • Ocular Inflammation • Ophthalmology • Rheumatology • Seronegative Spondyloarthropathies • Uveitis

Urinary excretion patterns and potential risks of beta-blocker ophthalmic drops in sports. (PubMed, Drug Test Anal) - "On the other hand, 36.36% (4/11) of urine samples were detected with beta-blockers higher than the MRL during the chronic administration of timolol and carteolol ophthalmic drops. In the context of receiving ophthalmic beta-blocker medications, the present study has highlighted the potential risk of constituting an AAF in specific sports and suggests strengthening athletes' awareness of therapeutic use exemptions."

Journal • Glaucoma • Ophthalmology

Comparison of the Effect on Vessel Density and RNFL between Carteolol and Latanoprost. (PubMed, J Clin Med) - "In contrast, the change in the VD parameter was statistically significant between groups (p < 0.05), with a greater difference observed in the carteolol-treated group of eyes. Carteolol had a better effect on the VD."

Journal • Glaucoma • Ophthalmology