Vikipediya

Bromocriptine

Bromokriptin dastlab Parlodel nomi ostida sotilgan keyinchalik koʻplab brend nomlari ostida sotuvga chiqarilgan.[1] Ergolin hosilasi dofamin agonisti boʻlib, u gipofiz oʻsmalari, Parkinson kasalligi, giperprolaktinemiya, neyroleptik malign sindrom va 2-turdagi qandli diabetni davolashda qoʻllanadi.

Bromokriptin 1968-yilda patentlangan va 1975-yilda tibbiy foydalanishga ruxsat berilgan.[2]

Tibbiy maqsadlarda foydalanish

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Bromokriptin akromegaliya va amenoreya, bepushtlik, gipogonadizm va prolaktin ajraladigan adenoma kabi giperprolaktinemiya bilan bog'liq kasalliklarni davolash uchun foydalaniladi. Shuningdek, u tuxumdonlar giperstimulyatsiyasi sindromining oldini olish uchun[3][4] va Parkinson kasalligini davolash uchun ishlatiladi.

1980-yillarning oxiridan beri u kokain alomatlarini kamaytirish uchun ishlatilgan, ammo bu usulda foydalanish uchun isbotlar kam.[5]

Bromokriptinning formulasi, sikloset ham 2-toifa diabetni davolash uchun ishlatiladi.[6][7] Uyg'onganidan keyin 2 soat ichida qo'llanilganda, u gipotalamusdagi dofamin darajasini oshiradi va natijada jigarda glyukoza ishlab chiqarishni kamaytiradi. Shuning uchun u glyukemik nazoratni yaxshilash uchun parhez va jismoniy mashqlar uchun qo'shimcha sifatida iste'mol qilinishi mumkin.[8]

Nojo‘ya ta'sirlari

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Eng ko'p uchraydigan nojo'ya ta'sirlarga ko'ngil aynishi, ortostatik gipotenziya, bosh og'rig'i va qusish markazini stimulyatsiya qilish orqali qayt qilishdir.[9] Miyokard infarkti va insult kabi jiddiy oqibatlarga olib keladigan vazospazmlar tug'ruq davri bilan bog'liq bo'lib, juda kam uchraydigan hodisalardir.[10] Periferik vazospazm (barmoqlar yoki oyoq barmoqlari) Raynaud fenomeniga olib kelishi mumkin. Bromokriptinni qo'llash psixotik simptomlarni keltirib chiqarishi yoki yomonlashishi bilan bog'liq (uning mexanizmi ko'pchilik antipsikotiklarga qarama-qarshidir, ularning mexanizmlari odatda dopamin retseptorlarini bloklaydi).[11] Bromokriptin Parkinson kasalligini davolash uchun yuqori dozalarda qo'llanilganda o'pka fibrozi haqida xabar berilgan.[12]

Tuqqandan keyin sut ishlab chiqarishni to'xtatish uchun foydalanish 2014-yilda ko'rib chiqildi va bu kontekstda jiddiy yurak-qon tomir, nevrologik yoki psixiatrik hodisalar bilan sababiy bog'liqlikni istisno qilib bo'lmaydi, degan xulosaga keldi, umumiy insidans 0,005% dan 0,04% gacha. Ma'lumotlarga asoslanib, qo'shimcha xavfsizlik choralari va qat'iyroq retseptlash qoidalari taklif qilindi.[13][14] Bu safro tuzining eksport pompasi inhibitori.[15]

Dofamin agonistlarini uzoq muddat qabul qilgandan keyin, dozani kamaytirish yoki qabul qilishni to'xtatish paytida quyidagi nojo'ya ta'sirlar kelib chiqadi : tashvish, vahima hurujlari , disforiya, depressiya, qo'zg'alish, asabiylashish, o'z joniga qasd qilish fikri, charchoq, ortostatik gipotenziya, ko'ngil aynishi, qusish., diaforez, umumiy og'riq va giyohvand moddalarga bo'lgan ishtiyoq. Ba'zi odamlar uchun bu nojo'ya ta'sirlar qisqa muddatli bo'lib, ular to'liq tuzalib ketadi, boshqalar uchun uzoq davom etadigan nojo'ya ta'sirlar paydo bo'lishi mumkin, bu bu nojo'ya ta'sirlar oylab yillab davom etishi mumkin.[16]

Farmakologiya

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Farmakodinamikasi

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Dopamin retseptorlari bilan bog'langan konformatsiyada bormokriptin

Bromokriptin dofamin D <sub id="mwXg">2</sub> retseptorining qisman agonistidir.[17] Bundan tashqari, boshqa dofamin retseptorlari va turli xil serotonin va adrenergik retseptorlari bilan o'zaro ta'sir qiladi. Bromokriptin qo'shimcha ravishda GLT1 glutamat tashuvchisini teskari o'zgartirib, glutamatning tarqalishini ingibatsiya qilgani aniqlangan.[18]

Serotonin 5-HT <sub id="mweA">2B</sub> retseptorlarining antagonisti sifatida bromokriptin yurak valvulopatiyasi bilan bog'liq emas.[19] Bu kabergolin va pergolid kabi 5-HT 2B retseptorlari agonistlari vazifasini bajaradigan boshqa ergolinlardan farqli o'laroq, lekin xuddi shunday tarzda 5-HT 2B retseptorlari antagonisti vazifasini bajaradigan lizuridga o'xshaydi.[19]

Activities of bromocriptine at various sites[20][21][22][23]
Site Affinity (Ki [nM]) Efficacy (Emax [%]) Action
D<sub id="mwmw">1</sub> 692 ? ?
D<sub id="mwpA">2S</sub> 5.0 41 Partial agonist
D<sub id="mwqw">2L</sub> 15 28 Partial agonist
D<sub id="mwsg">3</sub> 6.8 68 Partial agonist
D<sub id="mwuQ">4</sub> 372 0 Silent antagonist
D<sub id="mwwA">5</sub> 537 ? ?
5-HT<sub id="mwyQ">1A</sub> 13 72 Partial agonist
5-HT<sub id="mw0A">1B</sub> 355 66 Partial agonist
5-HT<sub id="mw1w">1D</sub> 11 86 Partial agonist
5-HT<sub id="mw3g">2A</sub> 107 69 Partial agonist
5-HT<sub id="mw5Q">2B</sub> 56 0 Silent antagonist
5-HT<sub id="mw7A">2C</sub> 741 79 Partial agonist
5-HT<sub id="mw8w">6</sub> 33 ? ?
5-HT<sub id="mw_A">7</sub> 11–126 ? ?
α<sub id="mwAQU">1A</sub> 4.2 0 Silent antagonist
α<sub id="mwAQw">1B</sub> 1.4 ? ?
α<sub id="mwARU">1D</sub> 1.1 ? ?
α<sub id="mwAR4">2A</sub> 11 0 Silent antagonist
α<sub id="mwASU">2B</sub> 35 0 Silent antagonist
α<sub id="mwASw">2C</sub> 28 0 Silent antagonist
α<sub id="mwATM">2D</sub> 68 ? ?
β<sub id="mwATw">1</sub> 589 ? ?
β<sub id="mwAUU">2</sub> 741 ?
H<sub id="mwAU4">1</sub> >10,000 – –
M<sub id="mwAVU">1</sub> >10,000 – –

Kimyo

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Barcha ergopeptidlar singari, bromokriptin ham sikloldir ; uning tripeptid qismining ikkita peptid guruhi o'zaro bog'langan bo'lib, amid funksionalligi bilan ikkita halqa o'rtasida >NC(OH)< birikmasini hosil qiladi.

Bromokriptin - N -bromosuksid yordamida ergokriptinni bromlash yo'li bilan sintez qilinadigan tabiiy ergot alkaloidi, ergokriptin (lisergik kislota hosilasi) ning yarim sintetik hosilasi hisoblanadi.

 

Tarix

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Bromokriptin 1965-yilda Sandoz tomonidan kashf etilgan va birinchi marta 1968-yilda patentlangan birinchi marta Parlodel brendi ostida sotuvga chiqarilgan.[24][25]

Bromokriptinning formulasi 2009-yilda FDA tomonidan tasdiqlangan[26]

Jamiyat va madaniyat

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Brend nomlari

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2017-yil iyul oyidan boshlab bromokriptin butun dunyo bo'ylab ko'plab brendlar ostida sotildi, jumladan Abergin, Barlolin, Brameston, Brocriptin, Brom, Broma-Del, Bromergocryptine, Bromergon, Bromicon, Bromocorn, Bromocriptin, Bromocriptina, Bromocriptine, Bromocriptina, Bromocriptine, Bromocriptina, Bromocriptine, Bromocriptine, Bromocriptine, Bromocriptemes, metansulfonat, bromokriptin mesilas, bromokriptinmesilat, bromodel, bromokriptin, bromolac, bromotin, bromtin, brotin, butin, korpadel, kripsa, kriptin, kriten, sikloset, degala, demil, deparo, deprolak, dokriptin, kiriptin, diakriptin,, Kriptonal, Laktodel, Medokriptin, Melen, Padoparin, Palolactin, Parlodel, Pravidel, Proktinal, Ronalin, Yarim Brom, Serokriptin, Serokriptin, Suplac, Sintokriptin, Umprel, Unew, Updopa, Upnol B va Volbro.[1]

2017-yil iyul oyidan boshlab u Diakriptin-M sifatida metformin bilan kombinatsiyalangan dori sifatida va Pseudogravin brendi ostida veterinariya preparati sifatida sotilgan.[1]

Manbalar

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  1. ↑ 1,0 1,1 1,2 „Bromocriptine international brand names“. Drugs.com. 6-avgust 2017-yilda asl nusxadan arxivlangan. Qaraldi: 13-iyul 2017-yil.
  2. ↑ Analogue-based Drug Discovery (en). John Wiley & Sons, 2006 — 533-bet. ISBN 9783527607495. 
  3. ↑ „Diagnosis and Treatment of Pituitary Adenomas: A Review“. JAMA. 317-jild, № 5. February 2017. 516–524-bet. doi:10.1001/jama.2016.19699. PMID 28170483.
  4. ↑ „Dopamine agonists for preventing ovarian hyperstimulation syndrome“. The Cochrane Database of Systematic Reviews. 14-Apr 2021-yil. doi:10.1002/14651858.CD008605.pub4. PMC 8092425. PMID 33851429.{{cite magazine}}: CS1 maint: date format ()
  5. ↑ „Dopamine agonists for the treatment of cocaine dependence“. The Cochrane Database of Systematic Reviews. № 5. May 2015. CD003352-bet. doi:10.1002/14651858.CD003352.pub4. PMC 6999795. PMID 26014366. {{cite magazine}}: Invalid |display-authors=6 (yordam)
  6. ↑ „The role of bromocriptine-QR in the management of type 2 diabetes expert panel recommendations“. Endocrine Practice. 19-jild, № 1. 2013. 100–6-bet. doi:10.4158/EP12325.OR. PMID 23337160.
  7. ↑ „Efficacy and Safety of Bromocriptine-QR in Type 2 Diabetes: A Systematic Review and Meta-Analysis“. Hormone and Metabolic Research. 47-jild, № 11. October 2015. 805–12-bet. doi:10.1055/s-0035-1559684. PMID 26332757. {{cite magazine}}: Invalid |display-authors=6 (yordam)
  8. ↑ „Bromocriptine: a sympatholytic, d2-dopamine agonist for the treatment of type 2 diabetes“. Diabetes Care. 34-jild, № 4. April 2011. 789–94-bet. doi:10.2337/dc11-0064. PMC 3064029. PMID 21447659.
  9. ↑ „The safety of bromocriptine in long-term use: a review of the literature“. Current Medical Research and Opinion. 10-jild, № 1. 1986. 25–51-bet. doi:10.1185/03007998609111089. PMID 3516579.
  10. ↑ „Bromocriptine related atypical vascular accidents postpartum identified through medicolegal reviews“. Medicine and Law. 15-jild, № 1. 1996. 127–34-bet. PMID 8691994.
  11. ↑ „Bromocriptine and psychosis: a literature review“. The Psychiatric Quarterly. 66-jild, № 1. 1995. 87–95-bet. doi:10.1007/BF02238717. PMID 7701022.
  12. ↑ „Pleuropulmonary fibrosis due to bromocriptine treatment for Parkinson's disease“. Clinical and Experimental Neurology. 27-jild. 1990. 79–82-bet. PMID 2129961.
  13. ↑ „European Medicines Agency - News and Events - CMDh endorses restricted use of bromocriptine for stopping breast milk production“. www.ema.europa.eu (2018-yil 17-sentyabr). 2014-yil 28-avgustda asl nusxadan arxivlangan.
  14. ↑ „EMA rät vom Abstillmittel Bromocriptin ab“ (2014-yil 25-avgust). 2015-yil 9-iyunda asl nusxadan arxivlangan. Qaraldi: 2014-yil 26-avgust. "EMA rät vom Abstillmittel Bromocriptin ab", article in Ärzteblatt
  15. ↑ „Flagging Drugs That Inhibit the Bile Salt Export Pump“ (PDF). Molecular Pharmaceutics. 13-jild, № 1. January 2016. 163–71-bet. doi:10.1021/acs.molpharmaceut.5b00594. PMID 26642869. {{cite magazine}}: Invalid |display-authors=6 (yordam)
  16. ↑ „Dopamine agonist withdrawal syndrome: implications for patient care“. Drugs & Aging. 30-jild, № 8. August 2013. 587–92-bet. doi:10.1007/s40266-013-0090-z. PMID 23686524.
  17. ↑ „The dopamine receptor D2 agonist bromocriptine inhibits glucose-stimulated insulin secretion by direct activation of the alpha2-adrenergic receptors in beta cells“. Biochemical Pharmacology. 79-jild, № 12. June 2010. 1827–36-bet. doi:10.1016/j.bcp.2010.01.029. PMID 20138024. {{cite magazine}}: Invalid |display-authors=6 (yordam)
  18. ↑ „Bromocriptine, an ergot alkaloid, inhibits excitatory amino acid release mediated by glutamate transporter reversal“. European Journal of Pharmacology. 643-jild, № 1. September 2010. 48–57-bet. doi:10.1016/j.ejphar.2010.06.007. PMID 20599932.
  19. ↑ 19,0 19,1 „Safety Pharmacology assessment of drugs with biased 5-HT(2B) receptor agonism mediating cardiac valvulopathy“. J Pharmacol Toxicol Methods. 69-jild, № 2. 2014. 150–61-bet. doi:10.1016/j.vascn.2013.12.004. PMID 24361689.
  20. ↑ Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A (November 2002). „Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes“. J Pharmacol Exp Ther. 303-jild, № 2. 791–804-bet. doi:10.1124/jpet.102.039867. PMID 12388666.
  21. ↑ Newman-Tancredi A, Cussac D, Audinot V, Nicolas JP, De Ceuninck F, Boutin JA, Millan MJ (November 2002). „Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. II. Agonist and antagonist properties at subtypes of dopamine D(2)-like receptor and alpha(1)/alpha(2)-adrenoceptor“. J Pharmacol Exp Ther. 303-jild, № 2. 805–14-bet. doi:10.1124/jpet.102.039875. PMID 12388667.
  22. ↑ Newman-Tancredi A, Cussac D, Quentric Y, Touzard M, Verrièle L, Carpentier N, Millan MJ (November 2002). „Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. III. Agonist and antagonist properties at serotonin, 5-HT(1) and 5-HT(2), receptor subtypes“. J Pharmacol Exp Ther. 303-jild, № 2. 815–22-bet. doi:10.1124/jpet.102.039883. PMID 12388668.
  23. ↑ National Institute of Mental Health. PDSP Ki Database (Internet). ChapelHill (NC): University of North Carolina. Available from: „Archived copy“. 2021-yil 12-aprelda asl nusxadan arxivlangan. Qaraldi: 2021-yil 12-aprel.
  24. ↑ Drug Discovery: A History (en). John Wiley & Sons, 2005 — 352-bet. ISBN 9780471899792. 
  25. ↑ „Fungal Metabolites as Pharmaceuticals“. Australian Journal of Chemistry. 67-jild, № 6. 2014. 827-bet. doi:10.1071/CH13639.
  26. ↑ „Bromocriptine: old drug, new formulation and new indication“. Diabetes, Obesity & Metabolism. 12-jild, № 12. December 2010. 1048–57-bet. doi:10.1111/j.1463-1326.2010.01304.x. PMID 20977575. 
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