Prazepam
Also called Centrac, Centrax, Demetrin, Lysanxia, Pozapam, Prasepine, Prazene, Reapam, Trepidan, Verstran, Sedapran, Settima
Part of the metabolic pathway of Prazepam. See the timeline on the metabolic highway.
Dosage
Oral
TripSit dose text
TripSit's factsheet also states its doses as text.
Light: 5-10mg Common: 10-20mg Strong: 20-40mg. TS
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Duration
TripSit factsheet
Mixing
For best safety practice, don't mix this drug with other depressants.
Why: respiratory depression. PsychonautWiki says:
- “Respiratory depression (also known as hypoventilation) can be described as a reduced urge to breathe that can be fatal depending on its intensity.” (PsychonautWiki, Respiratory depression, revision 150612)
- “... otherwise safe dosages of these compounds can become fatal when combined with even small amounts of other classes of depressant. For example, benzodiazepines combined with opioids are an extremely common cause of fatal respiratory depression. It is therefore strongly discouraged to combine these depressants at any dosage range.” (PsychonautWiki, Respiratory depression, revision 150612)
- “The most common cause of substance-related deaths is the combination of depressants (such as opiates, benzodiazepines, or alcohol) with other depressants.” (PsychonautWiki, Responsible drug use, revision 168206)
- “This combination potentiates the muscle relaxation, amnesia, sedation, and respiratory depression caused by one another. At higher doses, it can lead to a sudden, unexpected loss of consciousness along with a dangerous amount of depressed respiration.” (PsychonautWiki, dangerous interactions table, "Depressants" row, revision 156847)
Quotes from PsychonautWiki, CC BY-SA 4.0.
Acute combinations: what happens when these are taken close together. Entries backed by a medical journal or agency are listed first.
Backed by medical journals
TripSit combination chart
TripSit rates each pairing. Only pairings with a number carry a citation from TripSit. See the whole chart; TripSit's own notes are on combo.tripsit.me.
Caution
Risks and toxicity
TripSit factsheet
- Avoid
- All other CNS depressants, and Cimetidine TS
Testing
Effects
Overview
Benzodiazepine dervative. Has all the normal benzodiazepine-like quality (Anxiolytic/anticonvulsant/sedative/Skeletal muscle relaxant) It is also a prodrug for Desmethyldiazepam which is responsible for most if not all of the effects of Prazepam. TS
Prazepam is a benzodiazepine derivative drug developed by Warner-Lambert in the 1960s. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Prazepam, (Elimination half-life 29-224h), is a prodrug for desmethyldiazepam, (Elimination half-life 36-200h), which is responsible for the therapeutic effects of prazepam.[1]
History
Legal status
Pharmacology
Mechanism of action
Prazepam exerts its therapeutic effects primarily via modulating the benzodiazepine site which in turn enhances GABA function in the brain. Prazepam like other benzodiazepines has anticonvulsant properties, but its anticonvulsant properties are not as potent as other benzodiazepines when tested in animal studies.[4–8] WP
Pharmacokinetics
Prazepam is metabolised into descyclopropylmethylprazepam (also known as desmethyldiazepam) and 3-hydroxyprazepam which is further metabolised into oxazepam. Prazepam is a prodrug for descyclopropylmethylprazepam/desmethyldiazepam (also known as norprazepam or nordazepam) which is responsible for most of the therapeutic activity of prazepam rather than prazepam itself.[4]
Chemistry
- Formula
- C19H17ClN2O PC
- CAS number
- 2955-38-6 PC
- Molar mass (g/mol)
- 324.8 PC
- IUPAC name (computed by PubChem)
- 7-
chloro- PC1- (cyclopropylmethyl) - 5- phenyl- 3H- 1, 4- benzodiazepin- 2- one - SMILES
- C1CC1CN2C(=O)
CN=C(C3=C2C=CC(=C3) PCCl) C4=CC=CC=C4 - InChIKey
- MWQCHHACWWAQLJ-
UHFFFAOYSA- PCN - PubChem CID
- 4890
- IUPAC name
- 7-
Chloro- WP1- (cyclopropylmethyl) - 5- phenyl- 1, 3- dihydro- 2H- 1, 4- benzodiazepin- 2- one
User reports
Erowid erowid.org
ListingsBluelight bluelight.org
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References
- Other US Patent 3192199 – Process for the production of I-CYCLO- ALKYL derivatives of I,X-BENZODIAZEPINE
- Journal / agency Shader RI, Greenblatt DJ. Ciba Foundation Symposium 74 - Drug Concentrations in Neuropsychiatry. Ciba Foundation Symposium. 1979. doi:10.1002/9780470720578.ch9 · PMID 45081
- Journal / agency Jacqmin P, Ansseau M. Comparison of sublingual and oral prazepam in normal subjects. II. Pharmacokinetic and pharmacodynamic data. Neuropsychobiology. 1988. doi:10.1159/000118458 · PMID 2854609
- Journal / agency Quast U. Molecular mechanism of action of benzodiazepines. Fortschritte der Medizin. May 1981. PMID 6114911
- Journal / agency De Sarro G, Gitto R, Rizzo M, Zappia M, De Sarro A. 1,4-Benzodiazepine derivatives as anticonvulsant agents in DBA/2 mice. General Pharmacology. September 1996. doi:10.1016/0306-3623(95)02147-7 · PMID 8909973
- Journal / agency De Sarro G, Chimirri A, Zappala M, Guisti P, Lipartiti M, De Sarro A. Azirino[1, 2-d][1, 4]benzodiazepine derivatives and related 1,4-benzodiazepines as anticonvulsant agents in DBA/2 mice. General Pharmacology. October 1996. doi:10.1016/S0306-3623(96)00049-3 · PMID 8981061
- Journal / agency De Sarro G, Chimirri A, McKernan R, Quirk K, Giusti P, De Sarro A. Anticonvulsant activity of azirino[1,2-d][1,4]benzodiazepines and related 1,4-benzodiazepines in mice. Pharmacology, Biochemistry, and Behavior. September 1997. doi:10.1016/S0091-3057(96)00565-5 · PMID 9264104
- Journal / agency Fukinaga M, Ishizawa K, Kamei C. Anticonvulsant properties of 1,4-benzodiazepine derivatives in amygdaloid-kindled seizures and their chemical structure-related anticonvulsant action. Pharmacology. November 1998. doi:10.1159/000028247 · PMID 9742288
- Journal / agency Viau JP, Epps JE, Di Carlo J. Prazepam metabolism after chronic administration to humans. Xenobiotica; the Fate of Foreign Compounds in Biological Systems. September 1973. doi:10.3109/00498257309151546 · PMID 4763144
- Journal / agency Valavani P, Atta-Politou J, Panderi I. Development and validation of a liquid chromatographic/electrospray ionization mass spectrometric method for the quantitation of prazepam and its main metabolites in human plasma. Journal of Mass Spectrometry. April 2005. doi:10.1002/jms.824 · PMID 15712230
- Journal / agency Lu XL, Guengerich FP, Yang SK. Stereoselective metabolism of prazepam and halazepam by human liver microsomes. Drug Metabolism and Disposition. 1991. doi:10.1016/S0090-9556(25)07201-0 · PMID 1680631
- Journal / agency Greenblatt DJ, Shader RI. Prazepam, a precursor of desmethyldiazepam. Lancet. April 1978. doi:10.1016/S0140-6736(78)90834-6 · PMID 76260
- Journal / agency Nau H, Liddiard C, Jesdinsky D, Wittfoht W. Quantitative analysis of prazepam and its metabolites by electron capture gas chromatography and selected ion monitoring. Application to diaplacetal passage and fetal hepatic metabolism in early human pregnancy. Journal of Chromatography. September 1978. doi:10.1016/S0378-4347(00)81889-7 · PMID 701422
- Journal / agency Shader RI, Greenblatt DJ. The use of benzodiazepines in clinical practice. British Journal of Clinical Pharmacology. 1981. doi:10.1111/j.1365-2125.1981.tb01832.x · PMID 6133535 · PMC1401641
- Journal / agency Kölle EU. Pharmacokinetics of oral prazepam. Fortschritte der Medizin. June 1981. PMID 6790396
- Journal / agency Ochs HR, Greenblatt DJ, Verburg-Ochs B, Locniskar A. Comparative single-dose kinetics of oxazolam, prazepam, and clorazepate: three precursors of desmethyldiazepam. Journal of Clinical Pharmacology. October 1984. doi:10.1002/j.1552-4604.1984.tb01817.x · PMID 6150943
Text and values on this page are quoted from Wikipedia (CC BY-SA 4.0), TripSit factsheets, PubChem (public domain). Each value links to the exact revision it came from.