Depressant: Difference between revisions

[[File:Somadril Comp.JPG|thumb|upright|[[Carisoprodol]] tablets]][[Carbamate]]s are a class of depressants or "[[tranquilizer]]s" that are synthesized from [[urea]].<ref>{{Cite journal |last1=Jordan |first1=Allan M. |last2=Khan |first2=Tariq H. |last3=Malkin |first3=Hugh |last4=Osborn |first4=Helen M. I. |date=August 2002 |title=Synthesis and analysis of urea and carbamate prodrugs as candidates for melanocyte-directed enzyme prodrug therapy (MDEPT) |journal=Bioorganic & Medicinal Chemistry |volume=10 |issue=8 |pages=2625–2633 |doi=10.1016/s0968-0896(02)00097-4 |issn=0968-0896 |pmid=12057651}}</ref> Carbamates have [[anxiolytic]],<ref name="Conermann 2022">{{Citation |last1=Conermann |first1=Till |title=Carisoprodol |url=http://www.ncbi.nlm.nih.gov/books/NBK553077/ |work=StatPearls |place=Treasure Island (FL) |date=2022 |publisher=StatPearls Publishing |pmid=31971718 |access-date=2022-11-30 |last2=Christian |first2=Desirae}}</ref> [[muscle relaxant]],<ref name="Conermann 2022"/> [[anticonvulsant]],<ref>{{Cite journal |last1=Kulig |first1=Katarzyna |last2=Malawska |first2=Barbara |date=October 2007 |title=Carisbamate, a new carbamate for the treatment of epilepsy |journal=IDrugs: The Investigational Drugs Journal |volume=10 |issue=10 |pages=720–727 |issn=1369-7056 |pmid=17899491}}</ref> [[hypnotic]],<ref name="Conermann 2022"/> [[Antihypertensive drug|antihypertensive]],<ref>{{Cite journal |last1=Kavelman |first1=D. A. |last2=Lewis |first2=J. A. |title=Clinical Evaluation of a New Antihypertensive Agent: W583 (Mebutamate) |date=1963-11-09 |journal=Canadian Medical Association Journal |volume=89 |issue=19 |pages=993–995 |issn=0008-4409 |pmc=1921904 |pmid=14076168}}</ref> and [[analgesic]] effects. It has other uses like [[Tremor|muscle tremors]], [[Psychomotor agitation|agitation]], and [[Alcohol withdrawal syndrome|alcohol withdrawal]]. Its muscle relaxant effects are useful for [[Strain (injury)|strains]], [[sprain]]s, and muscle injuries together with rest, physical therapy, and other measures.<ref name="Conermann 2022"/> The effects, synthesis and mechanism of action of Carbamates are very similar to [[barbiturate]]s.<ref>{{Cite journal |last1=Rho |first1=J. M. |last2=Donevan |first2=S. D. |last3=Rogawski |first3=M. A. |date=March 1997 |title=Barbiturate-like actions of the propanediol dicarbamates felbamate and meprobamate |journal=The Journal of Pharmacology and Experimental Therapeutics |volume=280 |issue=3 |pages=1383–1391 |issn=0022-3565 |pmid=9067327}}</ref> There are many different types of Carbamates, some only produce anxiolytic effects and hypnotic effects while some only have anticonvulsant effects.

 

 

[[Meprobamate]] which metabolizes to ''[[Carisoprodol]]'' was launched in 1955. It quickly become the first blockbuster psychotropic drug in America becoming popular in Hollywood and gaining fame for its seemingly miraculous effects. It has since been marketed under more than 100 trade names, from Amepromat through Quivet to Zirpon. [[Carisoprodol]], which is still used today mainly for its muscle relaxant effects has high abuse potential. Its mechanism of action is very similar to [[barbiturate]]s, [[Alcohol (drug)|alcohol]], [[methaqualone]] and [[benzodiazepine]]s. Carsidoprodol [[Allosteric modulator|allosterically modulates]] and directly [[Agonist|activates]] the human [[GABAA receptor|α1β2γ2 GABAAR]] ([[GABAA receptor|GABA_A]]) in the [[central nervous system]] in a [[Barbiturate|barbiturate-like manner]]. This causes [[chloride channel]]s to open, allowing [[chloride]] to flood into the neuron, slowing down [[Neurotransmission|communication between neurons]]; thus slowing down the [[nervous system]].<ref>{{Cite journal |last1=Gonzalez |first1=Lorie A. |last2=Gatch |first2=Michael B. |last3=Taylor |first3=Cynthia M. |last4=Bell-Horner |first4=Cathy L. |last5=Forster |first5=Michael J. |last6=Dillon |first6=Glenn H. |date=May 2009 |title=Carisoprodol-Mediated Modulation of GABAA Receptors: In Vitro and in Vivo Studies |journal=The Journal of Pharmacology and Experimental Therapeutics |volume=329 |issue=2 |pages=827–837 |doi=10.1124/jpet.109.151142 |issn=0022-3565 |pmc=2672873 |pmid=19244096}}</ref> Unlike [[Benzodiazepine|benzodiazpines]] which increase the frequency of the chloride channel opening, Carisoprodol increase the duration of channel opening when GABA is bound.<ref>{{Cite journal |last1=Twyman |first1=Roy E. |last2=Rogers |first2=Carl J. |last3=Macdonald |first3=Robert L. |date=March 1989 |title=Differential regulation of ?-aminobutyric acid receptor channels by diazepam and phenobarbital |url=https://onlinelibrary.wiley.com/doi/10.1002/ana.410250302 |journal=Annals of Neurology |language=en |volume=25 |issue=3 |pages=213–220 |doi=10.1002/ana.410250302 |pmid=2471436 |hdl=2027.42/50330 |s2cid=72023197 |issn=0364-5134}}</ref><ref>{{Cite journal |last1=Twyman |first1=R. |last2=Rogers |first2=C. J. |last3=Macdonald |first3=R. |date=1989 |title=Differential regulation of γ‐aminobutyric acid receptor channels by diazepam and phenobarbital |journal=Annals of Neurology |volume=25 |issue=3 |pages=213–220 |url=https://www.semanticscholar.org/paper/Differential-regulation-of-%CE%B3%E2%80%90aminobutyric-acid-by-Twyman-Rogers/24b0d9bd86fce40b1d24c9ddf281706af949a21c |doi=10.1002/ANA.410250302 |pmid=2471436 |hdl=2027.42/50330 |s2cid=72023197 |language=en}}</ref> [[Γ-Aminobutyric acid|GABA]] is the main [[Inhibitory postsynaptic potential|inhibitory]] [[neurotransmitter]] in the [[nervous system]], which causes its depressant effects.