Ciproheptadin

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Ciproheptadin
Cyproheptadine.svg
Cyproheptadine-Spartan-PM3-3D-balls.png
IUPAC ime
4-(5H-dibenzo [a,d]ciklohepten-5-iliden)-1-metilpiperidin hidrohlorid
Klinički podaci
Prodajno ime Periaktin
Drugs.com Monografija
MedlinePlus a682541
Kategorija trudnoće
  • US: B (Bez rizika u ispitivanjima na životinjama)
Način primene Oralno
Pravni status
Pravni status
  • UK: Samo u apoteci
Farmakokinetički podaci
Vezivanje proteina 96 do 99%
Metabolizam Hepatički i renalno
Poluvreme eliminacije 8,6 sata[1]
Izlučivanje Fekalno i renalno
Identifikatori
CAS broj 129-03-3 ДаY 969-33-5 (hidrohlorid)
ATC kod R06AX02 (WHO)
PubChem CID 2913
IUPHAR/BPS 277
DrugBank DB00434 ДаY
ChemSpider 2810 ДаY
UNII 2YHB6175DO ДаY
KEGG D07765 ДаY
ChEBI CHEBI:4046 ДаY
ChEMBL CHEMBL516 ДаY
Hemijski podaci
Formula C21H21N
Molarna masa 287,398 g/mol
  (verify)

Ciproheptadin (Periaktin) je prva generacija antihistamina sa dodatnim antiholinergičnim, antiserotinergičnim, i lokalno anestetičkim svojstvima.[2][3]

Farmakologija[уреди]

Ciproheptadin deluje kao antagonist (ili inverzni agonist u zavisnosti od aktivnog mesta) na sledećim receptorima:

On ima slab, i verovatno zanemarljiv, afinitet za sledeća mesta vezivanja (Ki):

Pored toga, ciproheptadin poseduje osobine blokatora kalcijumskog kanala[14] i lokalnog anestetika.[15]

Reference[уреди]

  1. Gunja N, Collins M, Graudins A (2004). „A comparison of the pharmacokinetics of oral and sublingual cyproheptadine”. Journal of Toxicology. Clinical Toxicology. 42 (1): 79—83. PMID 15083941. 
  2. Hardman JG, Limbird LE, Gilman AG (2001). Goodman & Gilman's The Pharmacological Basis of Therapeutics (10 изд.). New York: McGraw-Hill. doi:10.1036/0071422803. ISBN 0071354697. 
  3. Pdr Staff (2009). PDR: Physicians Desk Reference 2010 (Physicians' Desk Reference (Pdr)). Rozelle, N.S.W: Thomson Reuters. ISBN 1-56363-748-0. 
  4. Moguilevsky N; Varsalona F; Noyer M; et al. (1994). „Stable expression of human H1-histamine-receptor cDNA in Chinese hamster ovary cells. Pharmacological characterisation of the protein, tissue distribution of messenger RNA and chromosomal localisation of the gene”. European Journal of Biochemistry / FEBS. 224 (2): 489—95. PMID 7925364. doi:10.1111/j.1432-1033.1994.00489.x. 
  5. 5,0 5,1 Peroutka SJ (1988). „Antimigraine drug interactions with serotonin receptor subtypes in human brain”. Annals of Neurology. 23 (5): 500—4. PMID 2898916. doi:10.1002/ana.410230512. 
  6. 6,0 6,1 Bonhaus DW; Weinhardt KK; Taylor M; et al. (1997). „RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist”. Neuropharmacology. 36 (4–5): 621—9. PMID 9225287. doi:10.1016/S0028-3908(97)00049-X. 
  7. Stanton T, Bolden-Watson C, Cusack B, Richelson E (1993). „Antagonism of the five cloned human muscarinic cholinergic receptors expressed in CHO-K1 cells by antidepressants and antihistaminics”. Biochemical Pharmacology. 45 (11): 2352—4. PMID 8100134. doi:10.1016/0006-2952(93)90211-E. 
  8. 8,0 8,1 8,2 8,3 8,4 Toll L; Berzetei-Gurske IP; Polgar WE; et al. (1998). „Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications”. NIDA Research Monograph. 178: 440—66. PMID 9686407. 
  9. 9,0 9,1 F. S. Dukhovich (15. 8. 2005). Pharmacological aspects of molecular recognition. Nova Publishers. стр. 117. ISBN 978-1-59454-676-1. Приступљено 27. 11. 2011. 
  10. Kohen R; Metcalf MA; Khan N; et al. (1996). „Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor”. Journal of Neurochemistry. 66 (1): 47—56. PMID 8522988. doi:10.1046/j.1471-4159.1996.66010047.x. 
  11. 11,0 11,1 Bard JA, Zgombick J, Adham N, Vaysse P, Branchek TA, Weinshank RL (1993). „Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase”. The Journal of Biological Chemistry. 268 (31): 23422—6. PMID 8226867. 
  12. Hoyer D, Neijt HC (1988). „Identification of serotonin 5-HT3 recognition sites in membranes of N1E-115 neuroblastoma cells by radioligand binding”. Molecular Pharmacology. 33 (3): 303—9. PMID 3352595. 
  13. Runyon SP, Savage JE, Taroua M, Roth BL, Glennon RA, Westkaemper RB (2001). „Influence of chain length and N-alkylation on the selective serotonin receptor ligand 9-(aminomethyl)-9,10-dihydroanthracene”. Bioorganic & Medicinal Chemistry Letters. 11 (5): 655—8. PMID 11266163. doi:10.1016/S0960-894X(01)00023-3. 
  14. Lowe DA, Matthews EK, Richardson BP (1981). „The calcium antagonistic effects of cyproheptadine on contraction, membrane electrical events and calcium influx in the guinea-pig taenia coli”. British Journal of Pharmacology. 74 (3): 651—63. PMC 2071752Слободан приступ. PMID 6271323. 
  15. Riccioppo Neto F (1979). „The local anesthetic effect of cyproheptadine on mammalian nerve fibres”. European Journal of Pharmacology. 54 (3): 203—7. PMID 428422. doi:10.1016/0014-2999(79)90078-5. 

Literatura[уреди]

Spoljašnje veze[уреди]

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