Chemistry:Tipepidine
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| Routes of administration | Oral |
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| Formula | C15H17NS2 |
| Molar mass | 275.43 g·mol−1 |
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Tipepidine (INN) (brand names Asverin, Antupex, Asvelik, Asvex, Bitiodin, Cofdenin A, Hustel, Nodal, Sotal), also known as tipepidine hibenzate (JAN), is a synthetic, non-opioid antitussive and expectorant of the thiambutene class.[1][2] It acts as an inhibitor of G protein-coupled inwardly-rectifying potassium channels (GIRKs).[3] The drug was discovered in the 1950s,[4] and was developed in Japan in 1959.[5] It is used as the hibenzate and citrate salts.[1][5]
The usual dose is 20 mg every 4–6 hours.[citation needed] Possible side effects of tipepidine, especially in overdose, may include drowsiness, vertigo, delirium, disorientation, loss of consciousness, and confusion.[5]
Tipepidine has been investigated as a potential psychiatric drug. It is being investigated in depression,[3][6][7] obsessive-compulsive disorder,[8] and attention-deficit hyperactivity disorder (ADHD).[9][10][11] Through inhibition of GIRK channels, tipepidine increases dopamine levels in the nucleus accumbens, but without increasing locomotor activity or producing methamphetamine-like behavioral sensitization, and this action appears to be at least partly responsible for its antidepressant-like effects in rodents.[12][13]
See also
- Cough syrup
- Noscapine
- Codeine; Pholcodine
- Dextromethorphan; Dimemorfan
- Racemorphan; Dextrorphan; Levorphanol
- Butamirate
- Pentoxyverine
- Cloperastine; Levocloperastine
- Guaifenesin
- Timepidium bromide
References
- ↑ 1.0 1.1 Dictionary of Pharmacological Agents. CRC Press. 21 November 1996. pp. 1988–. ISBN 978-0-412-46630-4. https://books.google.com/books?id=A0THacd46ZsC&pg=PA1988.
- ↑ Index Nominum 2000: International Drug Directory. Taylor & Francis. January 2000. pp. 1649–. ISBN 978-3-88763-075-1. https://books.google.com/books?id=5GpcTQD_L2oC&pg=PA1649.
- ↑ 3.0 3.1 "The centrally acting non-narcotic antitussive tipepidine produces antidepressant-like effect in the forced swimming test in rats". Behavioural Brain Research 205 (1): 315–318. December 2009. doi:10.1016/j.bbr.2009.07.004. PMID 19616036. https://kumadai.repo.nii.ac.jp/?action=repository_action_common_download&item_id=24712&item_no=1&attribute_id=21&file_no=1.
- ↑ "Procedure for the preparation of a new piperidine derivative of anti-nutritional activity" ES patent 272195, published 1 March 1962, assigned to Antonio Gallardo SA.
- ↑ 5.0 5.1 5.2 "Tipepidine hibenzate intoxication". Pediatrics International 53 (5): 779–781. October 2011. doi:10.1111/j.1442-200X.2010.03297.x. PMID 21955016.
- ↑ "[Novel antidepressant-like action of drugs possessing GIRK channel blocking action in rats]". Yakugaku Zasshi 130 (5): 699–705. May 2010. doi:10.1248/yakushi.130.699. PMID 20460867.
- ↑ "Tipepidine in adolescent patients with depression: a 4 week, open-label, preliminary study". Neuropsychiatric Disease and Treatment 10: 719–722. 2014. doi:10.2147/NDT.S63075. PMID 24833905.
- ↑ "The potent inhibitory effect of tipepidine on marble-burying behavior in mice". Behavioural Brain Research 216 (1): 308–312. January 2011. doi:10.1016/j.bbr.2010.08.010. PMID 20713091.
- ↑ "Tipepidine in children with attention deficit/hyperactivity disorder: a 4-week, open-label, preliminary study". Neuropsychiatric Disease and Treatment 10: 147–151. 2014. doi:10.2147/NDT.S58480. PMID 24493927.
- ↑ "Old drug tipepidine as new hope for children with ADHD". The Australian and New Zealand Journal of Psychiatry 49 (2): 181–182. February 2015. doi:10.1177/0004867414553952. PMID 25280911.
- ↑ "Efficacy and safety of tipepidine as adjunctive therapy in children with attention-deficit/hyperactivity disorder: Randomized, double-blind, placebo-controlled clinical trial". Psychiatry and Clinical Neurosciences 73 (11): 690–696. November 2019. doi:10.1111/pcn.12913. PMID 31294924.
- ↑ "Tipepidine activates VTA dopamine neuron via inhibiting dopamine D₂ receptor-mediated inward rectifying K⁺ current". Neuroscience 252: 24–34. November 2013. doi:10.1016/j.neuroscience.2013.07.044. PMID 23896570.
- ↑ "Tipepidine increases dopamine level in the nucleus accumbens without methamphetamine-like behavioral sensitization". Behavioural Brain Research 284: 118–124. May 2015. doi:10.1016/j.bbr.2015.02.012. PMID 25687844.
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