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Delorazepam
Systematic (IUPAC) name
(7-Chloro-5-(o-chlorophenyl) -1,3-dihydro-2H-1,4-benzodiazepin-2-one)
Identifiers
CAS number 2894-67-9
ATC code none
PubChem 17925
DrugBank ?
Chemical data
Formula C 15H10Cl2N2O 
Mol. mass 304.02
Pharmacokinetic data
Bioavailability 87%
Metabolism Hepatic
Half life [60-140]
Excretion Renal
Therapeutic considerations
Pregnancy cat.  ?
Legal status  ?
Routes Oral

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]

Contents

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]

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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).[16][17][14] 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.

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

  1. ^ Govoni, S.; Fresia, P.; Spano, PF.; Trabucchi, M. (Nov 1976). "Effect of desmethyldiazepam and chlordesmethyldiazepam on 3',5'-cyclic guanosine monophosphate levels in rat cerebellum.". Psychopharmacology (Berl) 50 (3): 241–4. doi:10.1007/BF00426839. PMID 188062.  
  2. ^ "Benzodiazepine Names". non-benzodiazepines.org.uk. http://www.non-benzodiazepines.org.uk/benzodiazepine-names.html. Retrieved 2008-12-29.  
  3. ^ Oliveira-Silva, D.; Oliveira, CH.; Mendes, GD.; Galvinas, PA.; Barrientos-Astigarraga, RE.; De Nucci, G. (Dec 2009). "Quantification of chlordesmethyldiazepam by liquid chromatography-tandem mass spectrometry: application to a cloxazolam bioequivalence study.". Biomed Chromatogr 23 (12): 1266–75. doi:10.1002/bmc.1249. PMID 19488979.  
  4. ^ a b Zimmermann-Tansella, C.; Tansella, M.; Lader, M. (Oct 1976). "The effects of chlordesmethyldiazepam on behavioral performance and subjective judgment in normal subjects.". J Clin Pharmacol 16 (10 Pt 1): 481–88. PMID 977791.  
  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. ^ Andreoli, V.; Maffei, F.; Montanaro, N.; Morandini, G. (Feb 1977). "Double-blind cross-over clinical comparison of two 2'-chloro benzodiazepines: 7-chloro-5-(2-chlorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one (chlordesmethyldiazepam) versus 7-chloro-5-(o-chlorophenyl)-1,3-dihydro-3-hydroxy-2H-1,4-benzodiazepin-2-one (lorazepam) in neurotic anxiety.". Arzneimittelforschung 27 (2): 436–9. PMID 16622.  
  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. ^ Rocca, P.; Fonzo, V.; Scotta, M.; Zanalda, E.; Ravizza, L. (May 1997). "Paroxetine efficacy in the treatment of generalized anxiety disorder.". Acta Psychiatr Scand 95 (5): 444–50. doi:10.1111/j.1600-0447.1997.tb09660.x. PMID 9197912.  
  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. PMID 8934975. PMC 2148912. http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2148912/pdf/anesthprog00243-0044.pdf.  
  13. ^ Cazzato, G.; Gioseffi, M.; Torre, P.; Coppola, N. (Nov-Dec 1982). "[Prevention and therapy of delirium tremens with tiapride and chlordesmethyldiazepam]". Riv Neurol 52 (6): 331–42. PMID 6130594.  
  14. ^ a b 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. PMID 3102240.  
  18. ^ Bareggi, SR.; Pirola, R.; Truci, G.; Leva, S.; Smirne, S. (Apr 1988). "Effect of food on absorption of chlordemethyldiazepam.". Arzneimittelforschung 38 (4): 561–2. PMID 2900012.  
  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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