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Lormetazepam

Lormetazepam
Identificare
Număr CAS848-75-9[1][2]  Modificați la Wikidata
PubChem13314[3]  Modificați la Wikidata
DrugBankDB13872  Modificați la Wikidata
ChemSpider12750[4]  Modificați la Wikidata
UNIIGU56C842ZA[2]  Modificați la Wikidata
KEGGD01657  Modificați la Wikidata
ChEMBLCHEMBL22097[5]  Modificați la Wikidata
Cod ATCN05CD06  Modificați la Wikidata
SMILES
CN1C2=C(C=C(C=C2)Cl)C(=NC(C1=O)O)C3=CC=CC=C3Cl[3]  Modificați la Wikidata
InChI
InChI=InChI=1S/C16H12Cl2N2O2/c1-20-13-7-6-9(17)8-11(13)14(19-15(21)16(20)22)10-4-2-3-5-12(10)18/h2-8,15,21H,1H3[3]  Modificați la Wikidata
Date chimice
FormulăC₁₆H₁₂Cl₂N₂O₂[3]  Modificați la Wikidata
Masă molară334,027583 u.a.m.[6]  Modificați la Wikidata
Modifică date / text Consultați documentația formatului

Lormetazepamul este un medicament din clasa 1,4-benzodiazepinelor, derivat de temazepam,[7] fiind utilizat în tratamentul insomniilor.[8][9] Calea de administrare disponibilă este cea orală.[8]

Prezintă efecte anxiolitice, hipnotice și sedative, anticonvulsivante și miorelaxante.

Molecula a fost patentată în 1961 și a fost aprobată pentru uz medical în 1980.[10]

Utilizări medicale

Lormetazepamul este indicat în tratamentul de scurtă durată al tulburărilor de somn de etiologie variată, care sunt moderate sau severe. Prezintă un timp de acțiune scurt, de aceea este utilizat la pacienții care prezintă probleme de adormire sau de menținere a somnului.[11]

Farmacologie

Ca toate benzodiazepinele, lormetazepamul acționează ca modulator alosteric pozitiv al receptorului de tip A pentru acidul gama-aminobutiric (R GABAA), reducând excitabilitatea neuronilor.[9][12] Prezintă o biodisponibilitate de 80%.[13]

Note

  1. ^ a b CAS Common Chemistry, accesat în  
  2. ^ a b c d lormetazepam (în engleză), Global Substance Registration System, accesat în  
  3. ^ a b c d e f g h i j k l „Lormetazepam”, Lormetazepam (în engleză), PubChem, accesat în  
  4. ^ a b Lormetazepam (în engleză), ChemSpider, accesat în  
  5. ^ a b LORMETAZEPAM (în engleză), ChEMBL, accesat în  
  6. ^ a b „Lormetazepam”, Lormetazepam (în engleză), PubChem, accesat în  
  7. ^ Nicholson AN, Stone BM (martie 1982). „Hypnotic activity and effects on performance of lormetazepam and camazepam--analogues of temazepam”. British Journal of Clinical Pharmacology. 13 (3): 433–9. doi:10.1111/j.1365-2125.1982.tb01398.x. PMC 1402107 Accesibil gratuit. PMID 6120717. 
  8. ^ a b „Lormetazepam”. The American Society of Health-System Pharmacists. Arhivat din original la . Accesat în . 
  9. ^ a b „Lormetazepam”. DrugBank - Canadian Institutes of Health Research. Accesat în . 
  10. ^ Fischer J, Ganellin CR (). Analogue-based Drug Discovery (în engleză). John Wiley & Sons. p. 537. ISBN 9783527607495. 
  11. ^ Rickels K (). „The clinical use of hypnotics: indications for use and the need for a variety of hypnotics”. Acta Psychiatrica Scandinavica. Supplementum. 332 (S332): 132–41. doi:10.1111/j.1600-0447.1986.tb08990.x. PMID 2883820. 
  12. ^ Kurowski M, Ott H, Herrmann WM (mai 1982). „Relationship between EEG dynamics and pharmacokinetics of the benzodiazepine lormetazepam”. Pharmacopsychiatria. 15 (3): 77–83. doi:10.1055/s-2007-1019513. PMID 6124982. 
  13. ^ Hümpel M, Stoppelli I, Milia S, Rainer E (). „Pharmacokinetics and biotransformation of the new benzodiazepine, lormetazepam, in man. III. Repeated administration and transfer to neonates via breast milk”. European Journal of Clinical Pharmacology. 21 (5): 421–5. doi:10.1007/BF00542330. PMID 6122580. 

Vezi și


v • d • m
Benzodiazepine (ATC N05BA)
1,4-benzodiazepine
Bromazepam  • Camazepam  • Clordiazepoxid  • Cinolazepam  • Clonazepam  • Delorazepam  • Clorazepat  • Diazepam#  • Fenazepam  • Flubromazepam  • Fludiazepam  • Flunitrazepam  • Flurazepam  • Halazepam  • Ketazolam  • Loflazepat  • Lorazepam#  • Lormetazepam  • Medazepam  • Nimetazepam  • Nitrazepam  • Nordazepam  • Oxazepam  • Pinazepam  • Prazepam  • Quazepam  • Sulazepam  • Temazepam  • Tetrazepam
1,5-benzodiazepine
Triazolobenzodiazepine
Imidazobenzodiazepine
Tienotriazolodiazepine
Tienobenzodiazepine
Altele
v • d • m
Terapia sistemului nervos central: psiholeptice - hipnotice și sedative (ATC N05C)
Modulatori ai
R GABAA
Alte clase
Antagoniști ai
R H1
ISRS (Etoperidonă  • Nefazodonă  • Trazodonă)  • ATC (Amitriptilină  • Doxepină, etc)  • ATeC (Mianserină  • Mirtazapină, etc)
Tipice (Clorpromazină  • Tioridazină, etc)  • Atipice (Olanzapină  • Quetiapină  • Risperidonă, etc)
Antagoniști ai
R 5-HT2A
ISRS (Trazodonă)  • ATC (Amitriptilină  • Doxepină  • Trimipramină, etc)  • ATeC (Mianserină  • Mirtazapină, etc)
Tipice (Clorpromazină  • Tioridazină, etc)  • Atipice (Olanzapină  • Quetiapină  • Risperidonă, etc)
Altele
Modulatori ai
R GABAB
Agoniști ai
R α2
Gabapentinoide
Melatonină
Orexină
Altele

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