Drug intelligence / Profile preview

melatonin + nicotine + bupropion + repaglinide + losartan + omeprazole + chlorzoxazone + midazolam + dextromethorphan

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular, Transdermal, Inhalation, Intranasal, Sublingual, Buccal
01

Overview

This is a combination of eight active pharmaceutical ingredients and one dietary supplement, each with distinct mechanisms of action and clinical uses: - **Melatonin** is an endogenous hormone used as a dietary supplement for sleep disorders. It acts primarily on melatonin receptors in the brain to regulate circadian rhythms. - **Nicotine** is a stimulant and parasympathomimetic alkaloid found in tobacco, used therapeutically for smoking cessation. It acts as an agonist at nicotinic acetylcholine receptors. - **Bupropion** is an antidepressant and smoking cessation aid that inhibits norepinephrine and dopamine reuptake (NDRI) and antagonizes nicotinic acetylcholine receptors[3][4]. - **Repaglinide** is an oral antidiabetic agent (meglitinide class) that stimulates insulin release from pancreatic beta cells by inhibiting ATP-sensitive potassium channels[7]. - **Losartan** is an angiotensin II receptor blocker (ARB) used to treat hypertension by blocking the angiotensin II type 1 receptor. - **Omeprazole** is a proton pump inhibitor that suppresses gastric acid secretion by inhibiting the H+/K+ ATPase enzyme system in gastric parietal cells[8]. - **Chlorzoxazone** is a centrally acting muscle relaxant, believed to act at the level of the spinal cord or subcortical areas of the brain. - **Midazolam** is a short-acting benzodiazepine with anxiolytic, amnestic, hypnotic, anticonvulsant, sedative, and muscle relaxant properties; it enhances GABAergic transmission via GABA-A receptors. - **Dextromethorphan** is an antitussive agent acting as an NMDA receptor antagonist. There are no known approved pharmaceutical products containing this exact combination. The mixture would present significant risks due to potential drug-drug interactions affecting CNS depression, metabolism (notably CYP450 enzymes), cardiovascular effects, glycemic control, blood pressure regulation, sedation levels, respiratory function, and more.

02

Targets

MTNR1A (MT1)α4β2 nAChR (Nicotinic acetylcholine receptor alpha4 beta2 subtype)DAT (Dopamine plasma membrane transport protein)SUR1 (Sulfonylurea receptor 1)NET (Norepinephrine Transporter)MTNR1B (Melatonin Receptor 2)

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