Delorazepam

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Delorazepam
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150px
Systematic (IUPAC) name
7-Chloro-5-(2-chlorophenyl)-1,3-dihydro-1,4-benzodiazepin-2(2H)-one
Clinical data
Pregnancy
category
  •  ?
Routes of
administration		 Oral
Legal status
Legal status
  •  ?
Pharmacokinetic data
Bioavailability 87%
Metabolism Hepatic
Biological half-life [60-140]
Excretion Renal
Identifiers
CAS Number 2894-67-9
ATC code none
PubChem CID 17925
DrugBank ?
Chemical data
Formula C15H10Cl2N2O
Molar mass 304.02[[Script error: No such module "String".]]
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Delorazepam also known as chlordesmethyldiazepam is a drug which is a benzodiazepine and a derivative of desmethyldiazepam.[1] It is marketed in Italy, where it is available under the trade name EN and Dadumir.[2] Delorazepam (chlordesmethyldiazepam) is also an active metabolite of the benzodiazepine drug cloxazolam.[3] Adverse effects may include hangover type effects, drowsiness, behavioural impairments[4][5] and short-term memory impairments.[6] Similar to other benzodiazepines delorazepam has anxiolytic,[7] skeletal muscle relaxant,[8] hypnotic[4] and anticonvulsant properties.[9]

Indications

Delorazepam is mainly used as an anxiolytic because of its long elimination half life; showing superiority over the short-acting drug lorazepam.[10] In comparison with the antidepressant drugs, paroxetine and imipramine, delorazepam was found to be more effective in the short-term but after 4 weeks the antidepressants showed superior anti-anxiety effects.[11]

Delorazepam is also used as a premedication for dental phobia for its anxiolytic properties.[12]

Delorazepam has also demonstrated effectiveness in treating alcohol withdrawal.[13]

Availability

Delorazepam is available in tablet and liquid drop formulations. The liquid drop formulation is absorbed more quickly and has improved bioavailibility.[14]

Pharmacology

Delorazepam is well absorbed after administration, reaching peak plasma levels within 1 – 2 hours. It has a very long elimination half life and can still be detected 72 hours after dosing.[15] Bioavailability is about 77 percent. Peak plasma levels occur at just over one hour after administration. Significant accumulation occurs of delorazepam due to its slow metabolism; the elderly metabolise delorazepam and its active metabolite slower than younger individuals. The elderly also have a poorer response to the therapeutic effects and a higher rate of adverse effects. The elimination half life of delorazepam is 80–115 hours. The active metabolite of delorazepam is lorazepam and represents about 15 - 24 percent of the parent drug (delorazepam).[14][16][17] The pharmacokinetics of delorazepam are not altered if it is taken with food, except for some slowing of absorption.[18] The potency of delorazepam is probably 1 mg delorazepam equals 10 mg diazepam.[citation needed]

Special cautions

People with renal failure on haemodialysis have a slow elimination rate and a reduced volume of distribution of the drug.[19] Liver disease has a profound effect on the elimination rate of delorazepam, resulting in the half-life almost doubling to 395 hours, where as healthy patients showed an elimination half life of 204 hours on average. Caution is recommended when using delorazepam in in patients with liver disease.[20]

See also

References

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Benzodiazepine derivatives (N05BA, N05CD)
1,4-Benzodiazepines

Bromazepam · Camazepam · Carburazepam · Chlordiazepoxide · Cinolazepam · Clonazepam · Clorazepate · Cyprazepam · Delorazepam · Demoxepam · Devazepide* · Diazepam · Doxefazepam · Elfazepam · Ethyl carfluzepate · Ethyl dirazepate · Ethyl loflazepate · Fletazepam · Fludiazepam · Flunitrazepam · Flurazepam · Flutemazepam · Flutoprazepam · Fosazepam · Gidazepam · Halazepam · Iclazepam · Ketazolam · Lorazepam · Lormetazepam · Meclonazepam · Medazepam · Menitrazepam · Metaclazepam · Motrazepam · Nimetazepam · Nitrazepam · Nitrazepate · Nordazepam · Nortetrazepam · Oxazepam · Phenazepam · Pinazepam · Pivoxazepam · Prazepam · Proflazepam · Quazepam · QH-II-66 · Reclazepam · Ro5-2904 · Sulazepam · Temazepam · Tetrazepam · Tifluadom* · Tolufazepam · Tuclazepam · Uldazepam

1,5-Benzodiazepines
2,3-Benzodiazepines *
Triazolobenzodiazepines
Imidazobenzodiazepines
Oxazolobenzodiazepines
Thienodiazepines
Pyridodiazepines
Pyrazolodiazepines
Pyrrolodiazepines
Tetrahydroisoquinobenzodiazepines
Benzodiazepine prodrugs
 * atypical activity profile (not GABAA receptor ligands)


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  1. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  2. ↑ "Benzodiazepine Names". non-benzodiazepines.org.uk. Retrieved 2008-12-29. 
  3. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  4. ↑ 4.0 4.1 Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  5. ↑ Cesco, G.; Giannico, S.; Fabbruci, I.; Scaggiante, L.; Montanaro, N. (1977). "Single-blind evaluation of hypnotic activity of chlordesmethyldiazepam in No-placebo-reactor medical patients". Arzneimittelforschung. 27 (1): 146–8. PMID 322671. 
  6. ↑ Scarone, S.; Strambi, LF.; Cazzullo, CL. (1981). "Effects of two dosages of chlordesmethyldiazepam on mnestic-information processes in normal subjects". Clin Ther. 4 (3): 184–91. PMID 6796270. 
  7. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  8. ↑ Kostowski, W.; Płaźnik, A.; Puciłowski, O.; Trzaskowska, E.; Lipińska, T. (1981). "Some behavioral effects of chlorodesmethyldiazepam and lorazepam". Pol J Pharmacol Pharm. 33 (6): 597–602. PMID 6127668. 
  9. ↑ Curatolo, P.; Cusmai, R.; Trasatti, G.; Sciarretta, A. (1985). "[Effects of intravenous administration of chlordesmethyldiazepam on paroxysmal intercritical activity in various electroclinical forms of infantile epilepsy]". Riv Neurol. 55 (6): 377–86. PMID 3938567. 
  10. ↑ Bertin, I.; Colombo, G.; Furlanut, M.; Benetello, P. (1989). "Double-blind placebo cross-over study of long-acting (chlordesmethyldiazepam) versus short-acting (lorazepam) benzodiazepines in generalized anxiety disorders". Int J Clin Pharmacol Res. 9 (3): 203–8. PMID 2568350. 
  11. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  12. ↑ Manani, G.; Baldinelli, L.; Cordioli, G.; Consolati, E.; Luisetto, F.; Galzigna, L. (1995). "Premedication with chlordemethyldiazepam and anxiolytic effect of diazepeam in implantology" (PDF). Anesth Prog. 42 (3-4): 107–12. PMC 2148912 Freely accessible. PMID 8934975. 
  13. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  14. ↑ 14.0 14.1 Bareggi, SR.; Truci, G.; Leva, S.; Zecca, L.; Pirola, R.; Smirne, S. (1988). "Pharmacokinetics and bioavailability of intravenous and oral chlordesmethyldiazepam in humans". Eur J Clin Pharmacol. 34 (1): 109–12. doi:10.1007/BF01061430. PMID 2896126. 
  15. ↑ Dal Bo, L.; Marcucci, F.; Mussini, E.; Perbellini, D.; Castellani, A.; Fresia, P. (1980). "Plasma levels of chlorodesmethyldiazepam in humans". Biopharm Drug Dispos. 1 (3): 123–6. doi:10.1002/bdd.2510010306. PMID 6778522. 
  16. ↑ Bareggi, SR.; Nielsen, NP.; Leva, S.; Pirola, R.; Zecca, L.; Lorini, M. (1986). "Age-related multiple-dose pharmacokinetics and anxiolytic effects of delorazepam (chlordesmethyldiazepam)". Int J Clin Pharmacol Res. 6 (4): 309–14. PMID 2875955. 
  17. ↑ Bareggi, SR.; Pirola, R.; Leva, S.; Zecca, L. (1986). "Pharmacokinetics of chlordesmethyldiazepam after single-dose oral administration in humans". Eur J Drug Metab Pharmacokinet. 11 (3): 171–4. doi:10.1007/BF03189844. PMID 3102240. 
  18. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
  19. ↑ Sennesael, J.; Verbeelen, D.; Vanhaelst, L.; Pirola, R.; Bareggi, SR. (1991). "Pharmacokinetics of intravenous and oral chlordesmethyldiazepam in patients on regular haemodialysis". Eur J Clin Pharmacol. 41 (1): 65–8. doi:10.1007/BF00280109. PMID 1782980. 
  20. ↑ Bareggi, SR.; Pirola, R.; Potvin, P.; Devis, G. (1995). "Effects of liver disease on the pharmacokinetics of intravenous and oral chlordesmethyldiazepam". Eur J Clin Pharmacol. 48 (3-4): 265–8. PMID 7589052. 
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