إريثرومايسين
إريثرومايسين Erythromycin هو مضاد حيوى ماكروليدي، ويتميز بمجال طيفي يشبه أو يزيد قليلا عن البنسيلين، ولذلك يستعمل لمن يعاني أو لديه حساسية للبنسيلين, بالنسبة لعدوى الجهاز التنفسي، فإن لديه تغطية أفضل للميكروبات الغير شائعة مثل mycoplasma وLegionellosis. وقد سوق أول الأمر بواسطة شركة شركة إلاي ليلي، ما يخثص بالتركيب الكيمائى، فهذا المركب الماكروليدى يحتوى على 14-membered lactone ring مع عشرة مراكز غير متماثلة ونوعين من السكر L-cladinose and D-desoamine مما يجعل هذا المركب عصياً على التخليق.
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| البيانات السريرية | |
|---|---|
| فئة السلامة أثناء الحمل |
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| مسارات الدواء | oral, iv, im, topical |
| رمز ATC | |
| الحالة القانونية | |
| الحالة القانونية | |
| بيانات الحركية الدوائية | |
| التوافر الحيوي | 100% |
| ارتباط الپروتين | 90% |
| الأيض | liver (under 5% excreted unchanged) |
| Elimination half-life | 1.5 hours |
| الإخراج | bile |
| المعرفات | |
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| رقم CAS | |
| PubChem CID | |
| DrugBank | |
| ChemSpider | |
| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.003.673  |
| Chemical and physical data | |
| التركيب | C37H67NO13 |
| الكتلة المولية | 733.93 g/mol |
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التاريخ
الصور المتاحة
تأثيرات جانبية
.[1] Erythromycin used for feeding intolerance in young infants has not been associated with hypertrophic pyloric stenosis.[1]
can also affect the central nervous system, causing psychotic reactions and nightmares and night sweats.[2]
May also alter the effectiveness of combined oral contraceptive pills.
نظرية العمل
Erythromycin may possess bacteriocidal activity, particularly at higher concentrations[3]. The mechanism is not fully elucidated however. By binding to the 50s subunit of the bacterial 70s rRNA complex, protein synthesis and subsequently structure/function processes critical for life or replication are inhibited[4]. Erythromycin interferes with aminoacyl translocation, preventing the transfer of the tRNA bound at the A site of the rRNA complex to the P site of the rRNA complex. Without this translocation, the A site remains occupied and thus the addition of an incoming tRNA and its attached amino acid to the nascent polypeptide chain is inhibited. This interferes with the production of functionally useful proteins and is therefore the basis of antimicrobial action.
الحراك الدوائى
تمثيل الدواء
مضادات الإستعمال
Erythromycin inhibits the cytochrome P450 system, particularly the CYP3A4 isozyme, which can cause it to affect the metabolism of many different drugs. If CYP3A4 substrates—drugs that are broken down by CYP3A4, such as simvastatin (Zocor), lovastatin (Mevacor), or atorvastatin (Lipitor)—are taken concomitantly with erythromycin, levels of the substrates will increase, often causing adverse effects. A noted drug interaction involves erythromycin and simvastatin, resulting in increased simvastatin levels and the potential for rhabdomyolysis. Another group of CYP3A4 substrates are drugs used for migraine such as ergotamine and dihydroergotamine; their adverse effects may be more pronounced if erythromycin is associated.[2] Earlier case reports on sudden death prompted a study on a large cohort that confirmed a link between erythromycin, ventricular tachycardia, and sudden cardiac death in patients also taking drugs that prolong the metabolism of erythromycin (like verapamil or diltiazem) by interfering with CYP3A4.[5] Hence, erythromycin should not be administered to people using these drugs, or drugs that also prolong the QT interval. Other examples include terfenadine (Seldane, Seldane-D), astemizole (Hismanal), cisapride (Propulsid, withdrawn in many countries for prolonging the QT time) and pimozide (Orap). Theophylline (which is mostly used in asthma) is also contraindicated.
المراجع
- ^ أ ب Maheshwai N (2007). "Are young infants treated with erythromycin at risk for developing hypertrophic pyloric stenosis?". Arch. Dis. Child. 92 (3): 271–3. doi:10.1136/adc.2006.110007. PMID 17337692.
{{cite journal}}: Unknown parameter|month=ignored (help) - ^ أ ب Erythromycin. Belgian Center for Pharmacotherapeutical Information. Retrieved July 20, 2008.
- ^ Katzung PHARMACOLOGY, 9e Section VIII. Chemotherapeutic Drugs Chapter 44. Chloramphenicol, Tetracyclines, Macrolides, Clindamycin, & Streptogramins
- ^ Katzung PHARMACOLOGY, 9e Section VIII. Chemotherapeutic Drugs Chapter 44. Chloramphenicol, Tetracyclines, Macrolides, Clindamycin, & Streptogramins
- ^ Ray WA, Murray KT, Meredith S, Narasimhulu SS, Hall K, Stein CM. Oral Erythromycin and the Risk of Sudden Death from Cardiac Causes. N Engl J Med 2004;351:1089-96.
- British National Formulary "BNF 49" March 2005.
- Mims C, Dockrell HM, Goering RV, Roitt I, Wakelin D, Zuckerman M. Chapter 33: Attacking the Enemy: Antimicrobial Agents and Chemotherapy: Macrolides. In: Medical Microbiology (3rd Edition). London: Mosby Ltd; 2004. p 489