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Tipepidine

Chemical compound

Summary

Chemical compound

| Drugs.com =

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Tipepidine (INN; also known as tipepidine hibenzate (JAN); brand names Asverin, Antupex, Asvelik, Asvex, Bitiodin, Cofdenin A, Hustel, Nodal, and Sotal) is a synthetic, non-opioid antitussive and expectorant of the thiambutene class. It acts as an inhibitor of G protein-coupled inwardly-rectifying potassium channels (GIRKs). The drug was discovered in the 1950s, and was developed in Japan in 1959. It is used as the hibenzate and citrate salts.

The usual dose is 20 mg every 4–6 hours. Possible side effects of tipepidine, especially in overdose, may include drowsiness, vertigo, delirium, disorientation, loss of consciousness, and confusion.

Tipepidine has been investigated as a potential psychiatric drug. It is being investigated in depression, obsessive-compulsive disorder, and attention-deficit hyperactivity disorder (ADHD). 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.

References

References

  1. (21 November 1996). "Dictionary of Pharmacological Agents". CRC Press.
  2. (January 2000). "Index Nominum 2000: International Drug Directory". Taylor & Francis.
  3. (December 2009). "The centrally acting non-narcotic antitussive tipepidine produces antidepressant-like effect in the forced swimming test in rats". Behavioural Brain Research.
  4. "Procedure for the preparation of a new piperidine derivative of anti-nutritional activity".
  5. (October 2011). "Tipepidine hibenzate intoxication". Pediatrics International.
  6. (May 2010). "[Novel antidepressant-like action of drugs possessing GIRK channel blocking action in rats]". Yakugaku Zasshi.
  7. (2014). "Tipepidine in adolescent patients with depression: a 4 week, open-label, preliminary study". Neuropsychiatric Disease and Treatment.
  8. (January 2011). "The potent inhibitory effect of tipepidine on marble-burying behavior in mice". Behavioural Brain Research.
  9. (2014). "Tipepidine in children with attention deficit/hyperactivity disorder: a 4-week, open-label, preliminary study". Neuropsychiatric Disease and Treatment.
  10. (February 2015). "Old drug tipepidine as new hope for children with ADHD". The Australian and New Zealand Journal of Psychiatry.
  11. (November 2019). "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.
  12. (November 2013). "Tipepidine activates VTA dopamine neuron via inhibiting dopamine D₂ receptor-mediated inward rectifying K⁺ current". Neuroscience.
  13. (May 2015). "Tipepidine increases dopamine level in the nucleus accumbens without methamphetamine-like behavioral sensitization". Behavioural Brain Research.
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antitussives expectorants piperidines potassium-channel-blockers thiophenes
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