كلوفازيمين

كلوفازيمين
البيانات السريرية
أسماء أخرى	N,5-bis(4-chlorophenyl)-3-(1-methylethylimino)-5H-phenazin-2-amine
رمز ATC	J04BA01 (WHO) ;
بيانات الحركية الدوائية
Elimination half-life	70 days
المعرفات
	IUPAC name N,5-bis(4-chlorophenyl)-3-(propan-2-ylimino)-3,5-dihydrophenazin-2-amine;
رقم CAS	2030-63-9;
PubChem CID	2794;
DrugBank	APRD00278;
CompTox Dashboard (EPA)	DTXSID7022839 ;
ECHA InfoCard	100.016.347
Chemical and physical data
التركيب	C27H22Cl2N4
الكتلة المولية	473.396 g/mol

كلوفازيمين كلوفازيمين,هو صبغة قابلة للذوبان في الدهون من نوع riminophenazine تستعمل مع rifampicin و dapsone كعلاج متعدد (MDT) لعلاج الجذام leprosy , وقد استعمل هذا العقار بحثيا بالإشتراك مع أدوية أخرى من نوعية antimycobacterial لعلاج Mycobacterium avium في مرضى ال AIDS , Mycobacterium avium paratuberculosis في عدوى مرض Crohn's disease و كلوفازيمين له تأثيرات مضادة للإلتهابات , يعطى لمجابهة تفاعلات مرض الجذام مثل erythemanodosum leprosum وهو مايطلق عليه (ENL) From AMA Drug Evaluations Annual, 1993, p1619 .

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التاريخ

الإمداد

تمثيل الدواء

التأثيرات الجانبية

تأثيرات كبح المناعة

إن تأثيرات كبح المناعة للكلوفازيمين سرعان ماظهرت حينما طبقت على نموذج حيواني فقد سجلت تقارير أن المكروفاج قد Macrophages inhibitedعطل نتيجة ثبات lysosomal membrane بواسطة كلوفازيمين .^[1] Clofazimine also showed a dosage-dependent inhibition of neutrophil motility, lymphocyte transformation ^[2], mitogen-induced PBMC proliferation ^[3] and complement-mediated solubilization of pre-formed immune complexes in vitro ^[4]. A systematic mechanistic studying of clofazimine in human T cells revealed that this drug actually is a Kv1.3 (KCNA3) channel blocker ^[5]. This indicates that clofazimine will be potentially used for treatment of multiple sclerosis, rheumatoid arthritis and type 1 diabetes. Because the Kv1.3-high effector memory T cells (T_EM) are actively involved in the development of these diseases ^[6], and Kv1.3 activity is essential for stimulation and proliferation of T_EM by regulating calcium influx in the T cells ^[7].

المراجع

^ Conalty ML, Barry VC, Jina A (1971). "The antileprosy agent B.663 (Clofazimine) and the reticuloendothelial system". Int J Lepr Other Mycobact Dis. 39 (2): 479–92. PMID 4948088. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
^ Gatner EM, Anderson R, van Remsburg CE, Imkamp FM. (1982). "The in vitro and in vivo effects of clofazimine on the motility of neutrophils and transformation of lymphocytes from normal individuals". Lepr Rev. 53 (2): 85–90. PMID 7098757. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
^ van Rensburg CE, Gatner EM, Imkamp FM, Anderson R. (1982). "Effects of clofazimine alone or combined with dapsone on neutrophil and lymphocyte functions in normal individuals and patients with lepromatous leprosy". Antimicrob Agents Chemother. 21 (5): 693–7. PMID 7049077. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
^ Kashyap A, Sehgal VN, Sahu A, Saha K. (1992). "Anti-leprosy drugs inhibit the complement-mediated solubilization of pre-formed immune complexes in vitro". Int J Immunopharmacol. 14 (2): 269–73. PMID 1624226. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
^ Ren YR, Pan F, Parvez S, Fleig A, Chong CR, Xu J, Dang Y, Zhang J, Jiang H, Penner R, Liu JO. (2008). "Clofazimine inhibits human Kv1.3 potassium channel by perturbing calcium oscillation in T lymphocytes". PLoS ONE. 3 (12): e4009. PMID 19104661. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
^ Beeton C, Wulff H, Standifer NE, Azam P, Mullen KM, Pennington MW, Kolski-Andreaco A, Wei E, Grino A, Counts DR, Wang PH, LeeHealey CJ, S Andrews B, Sankaranarayanan A, Homerick D, Roeck WW, Tehranzadeh J, Stanhope KL, Zimin P, Havel PJ, Griffey S, Knaus HG, Nepom GT, Gutman GA, Calabresi PA, Chandy KG. (2006). "Kv1.3 channels are a therapeutic target for T cell-mediated autoimmune diseases". Proc Natl Acad Sci U S A. 103 (46): 17414–9. PMID 17088564. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
^ Wulff H, Calabresi PA, Allie R, Yun S, Pennington M, Beeton C, Chandy KG. (2003). "The voltage-gated Kv1.3 K(+) channel in effector memory T cells as new target for MS". J Clin Invest. 111 (11): 1703–13. PMID 17088564. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)

الروابط الخارجية

الكلمات الدالة:

كلوفازيمين

[pmid4948088-1] Conalty ML, Barry VC, Jina A (1971). "The antileprosy agent B.663 (Clofazimine) and the reticuloendothelial system". Int J Lepr Other Mycobact Dis. 39 (2): 479–92. PMID 4948088. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)

[pmid7098757-2] Gatner EM, Anderson R, van Remsburg CE, Imkamp FM. (1982). "The in vitro and in vivo effects of clofazimine on the motility of neutrophils and transformation of lymphocytes from normal individuals". Lepr Rev. 53 (2): 85–90. PMID 7098757. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)

[pmid7049077-3] van Rensburg CE, Gatner EM, Imkamp FM, Anderson R. (1982). "Effects of clofazimine alone or combined with dapsone on neutrophil and lymphocyte functions in normal individuals and patients with lepromatous leprosy". Antimicrob Agents Chemother. 21 (5): 693–7. PMID 7049077. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)

[pmid1624226-4] Kashyap A, Sehgal VN, Sahu A, Saha K. (1992). "Anti-leprosy drugs inhibit the complement-mediated solubilization of pre-formed immune complexes in vitro". Int J Immunopharmacol. 14 (2): 269–73. PMID 1624226. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)

[pmid19104661-5] Ren YR, Pan F, Parvez S, Fleig A, Chong CR, Xu J, Dang Y, Zhang J, Jiang H, Penner R, Liu JO. (2008). "Clofazimine inhibits human Kv1.3 potassium channel by perturbing calcium oscillation in T lymphocytes". PLoS ONE. 3 (12): e4009. PMID 19104661. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)

[pmid17088564-6] Beeton C, Wulff H, Standifer NE, Azam P, Mullen KM, Pennington MW, Kolski-Andreaco A, Wei E, Grino A, Counts DR, Wang PH, LeeHealey CJ, S Andrews B, Sankaranarayanan A, Homerick D, Roeck WW, Tehranzadeh J, Stanhope KL, Zimin P, Havel PJ, Griffey S, Knaus HG, Nepom GT, Gutman GA, Calabresi PA, Chandy KG. (2006). "Kv1.3 channels are a therapeutic target for T cell-mediated autoimmune diseases". Proc Natl Acad Sci U S A. 103 (46): 17414–9. PMID 17088564. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)

[pmid12782673-7] Wulff H, Calabresi PA, Allie R, Yun S, Pennington M, Beeton C, Chandy KG. (2003). "The voltage-gated Kv1.3 K(+) channel in effector memory T cells as new target for MS". J Clin Invest. 111 (11): 1703–13. PMID 17088564. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)

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v t e مضادات المتفطرات (J04)
السل/ علاج السل	حمض الأمينو ساليسيليك (Calcium aminosalicylate, Sodium aminosalicylate) Antibiotics (Amikacin, Capreomycin, Cycloserine, Kanamycin, Rifabutin, Rifampicin, Rifamycin, Rifapentin, Streptomycin) hydrazides (Isoniazid) thiocarbamides (Ethionamide, Protionamide, Tiocarlide) Others (Ethambutol, Morinamide, Pyrazinamide, Terizidone)
الجذام	Aldesulfone sodium • Clofazimine • Dapsone • Rifampicin