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داروهای ضد قارچ  ANTIFUNGAL DRUGS  


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آمفوتريسين‌ Amphoericin B

کلوتريمازول‌‌ Clotrimazole

فلوکونازول‌‌ Fluconazole

فلوسيتوزين‌‌ Flucytosine

گريزئوفولوين‌‌ Griseofulvin

کتوکونازول‌‌‌ Ketoconazole

نيستاتين‌‌‌ Nystatin

 

 

 

 

 

 


آمفوتريسين

 

• موارد مصرف‌: آمفوتريسين‌ B در درمان ‌آسپرژيلوز ، بلاستوميکوز ، کانديدياز منتشر ، کوکسيديوئيدو ميکوز ، کريپتوکوکوز ، اندوکارديت‌ قارچي ‌، کانديدياز داخلي‌ چشم ، هيستوپلاسموز ، سالک ‌، مننژيت‌ قارچي‌، موکورميکوز،سپتي‌ سمي‌ قارچي‌، اسپوروتريکوزمنتشر، عفونتهاي‌ قارچي‌ دستگاه‌ ادراري‌و مننگوآنسفاليت‌ آميبي‌ اوليه‌ مصرف‌مي‌شود.

• مکانيسم‌ اثر: اين‌ دارو با اتصال‌ به‌استرولهاي‌ غشاي‌ سلولي‌ قارچ‌ و تغيير درقابليت‌ نفوذ اين‌ غشاء و در نتيجه‌ از دست‌رفتن‌ پتاسيم‌ و ملکولهاي‌ کوچک‌ از درون‌سلول‌، اثر ضد قارچي‌ خود را اعمال‌مي‌کند.

• فارماکوکينتيک‌: آمفوتريسين‌ B در ريه‌، کبد،طحال‌، کليه‌، غده‌ فوق‌ کليوي‌ و عضلات‌توزيع‌ شده‌ و غلظت‌ آن‌ در مايعات‌ جنب‌،صفاقي‌ و پرده‌ سينوويال‌ و مايع‌ زلاليه ‌تقريبا ۷۵% غلظت‌ پلاسمايي‌ آن‌ است‌. دفع‌اين‌ دارو از راه‌ کليه‌ بسيار آهسته‌ بوده‌ وتقريبا ۴۰% دارو در مدت‌ هفت‌ روز دفع‌شده‌ و حداقل‌ تا ۷ هفته‌ پس‌ از قطع‌ مصرف‌در ادرار يافت‌ مي‌شود.

• هشدارها: ۱ ـ در صورت‌ وجود عيب‌ کارکليه‌ بايد با احتياط فراوان‌ مصرف‌ شود. ۲ ـ مقدار مصرف‌ تام‌ بيش‌ از ۴g/day ممکن‌است‌ منجر به‌ بروز عيب‌ دايمي‌ کار کليه ‌گردد.

• عوارض‌ جانبي‌: از عوارض‌ شايع‌آمفوتريسين‌ B کم‌ خوني‌، کاهش‌ پتاسيم‌خون‌، تب‌ و لرز و تهوع‌ و استفراغ‌، دردمعده‌، سردرد، کمي‌ فشار خون‌، اختلال‌ کارکليه‌، درد عضله‌ و مفصل‌، کم‌ خوني‌،مسموميت‌ کليوي‌، اختلالات‌ نورولوژيک‌ و خوني‌، بثورات‌ جلدي‌ و ترومبوفلبيت‌ مي‌باشند.

• تداخل‌هاي‌ دارويي‌: مصرف‌ همزمان ‌آمفوتريسين‌ B با داروهاي‌ تضعيف‌ کننده ‌فعاليت‌ مغز استخوان ‌، گليکوزيدهاي‌ ديژيتال‌ ، مدرهاي‌ کاهنده‌ پتاسيم‌ و داروهاي‌ با سميت‌ کليوي‌ باعث‌ تشديدعوارض‌ سمي‌ دارو مي‌شود.

• نکات‌ قابل‌ توصيه‌:

۱ ـ در صورتيکه‌ وقفه‌درمان‌ بيش‌ از يک‌ هفته‌ باشد، درمان‌ مجددبايد با حداقل‌ مقدار مصرف‌ شروع‌ وبتدريج‌ تا مقدار مصرف‌ مطلوب‌ افزايش‌يابد.

۲ ـ با تزريق‌ وريدي‌ مقادير کم‌ کورتيکواستروئيدها قبل‌ و در طي‌انفوزيون‌ وريدي‌ آمفوتريسين‌ B احتمال‌بروز واکنش‌هاي‌ تب‌زا کاهش‌ مي‌يابد.همچنين‌ مصرف‌ استامينوفن ‌، آنتي‌هيستامين‌ها و يا فنوتيازين‌ها قبل‌ ازانفوزيون‌ آمفوتريسين‌ B عوارضي‌ چون‌تب ‌، تهوع‌ و لرز ناشي‌ از دارو را کاهش ‌مي‌دهند.

۳ ـ انفوزيون‌ وريدي‌ آمفوتريسين‌ B بايدطي‌ ۴ ـ ۲ ساعت‌ انجام‌ شود.

۴ ـ مصرف‌ مقادير کامل‌ اين‌ دارو حتي‌ دربيماران‌ مبتلا به‌ عيب‌ کار کليه‌ ضروري‌است‌. با اين‌ وجود در صورت‌ پيشرفت‌عيب‌ کار کليه‌ بيمار بايد تحت‌ مراقبت‌پزشکي‌ قرار گيرد.

۵ ـ نشت‌ دارو به‌ بافتهاي‌ اطراف‌ رگ‌ ممکن‌است‌ سبب‌ بروز تحريک‌ شديد محل‌ تزريق‌گردد.

۶ ـ براي‌ به‌ حداقل‌ رساندن‌ بروزترومبوفلبيت‌ موضعي‌ ناشي‌ از انفوزيون‌وريدي‌ اين‌ دارو، مي‌توان‌ هپارين‌ را به‌محلول‌ تزريقي‌ اضافه‌ کرد و ياآمفوتريسين‌ B را يک‌ روز در ميان‌ تجويزکرد. همچنين‌ مصرف‌ يک‌ روز در ميان‌آمفوتريسين‌ B احتمال‌ بي‌اشتهايي‌ راکاهش‌ مي‌دهد.

۷ ـ مقدار مصرف‌ اين‌ دارو به‌صورت‌ يک‌روز در ميان‌ نبايد بيش‌ از ۱/۵mg/kg باشد.

• مقدار مصرف‌:

بزرگسالان‌: آمفوتريسين‌ Bبه‌عنوان‌ ضدقارچ‌ سيستميک‌ در ابتدا ۵ ميلي‌گرم‌ در ۲۰ ـ ۱۰ ميلي‌ليتر از محلول‌ تزريقي‌دکستروز ۵% طي‌ ۵ ـ ۳ دقيقه‌ در حفرات‌بدن‌ چکانده‌ مي‌شود. سپس‌ ۵۰ ميلي‌گرم‌اين‌ دارو در ۲۰ ـ ۱۰ ميلي‌ليتر از محلول‌تزريقي‌ دکستروز ۵% طي‌ ۵ ـ ۳ دقيقه‌ هرروز مصرف‌ مي‌شود. از راه‌ تزريق‌ داخل‌نخاعي‌ ابتدا ۰/۱ ـ ۰/۰۱ ميلي‌گرم‌ هر ۷۲ ـ ۴۸ ساعت‌ تزريق‌ مي‌شود. اين‌ مقدار بر حسب‌ تحمل‌ بيمار بتدريج‌ تا ۰/۵ميلي‌گرم‌ افزايش‌ مي‌يابد.

به‌صورت‌انفوزيون‌ وريدي‌، ابتدا مقدار ۱ ميلي‌گرم‌به‌عنوان‌ مقدار آزمايشي‌ بعد از رقيق‌ شدن‌با ۵۰ ـ ۲۰ ميلي‌ليتر از محلول‌ تزريقي‌دکستروز ۵% طي‌ ۳۰ ـ ۱۰ دقيقه‌ تزريق‌مي‌شود. به‌ اين‌ مقدار برحسب‌ تحمل‌ بيمارو شدت‌ عفونت‌ ۱۰ ـ ۵ ميلي‌گرم‌ در هر نوبت‌مي‌توان‌ افزود. در اين‌ صورت‌ حداکثرمقدار مصرف‌ ۵۰mg/day طي‌ دوره‌ ۶ ـ ۲ساعته‌ مي‌باشد.

شستشوي‌ مثانه‌ با مقدار ۵ ميلي‌گرم‌آمفوتريسين‌ B در ۱۰۰۰ ميلي‌ليتر آب‌استريل‌ در روز با سرعت‌ ۴۰ml/h با يک‌کاتتر به‌ مدت‌ ۱۰ ـ ۵ روز ادامه‌ مي‌يابد. کودکان‌: به‌عنوان‌ ضد قارچ‌ سيستميک‌مقدار اوليه‌ ۰/۲۵mg/kg/day در محلول‌تزريقي‌ دکستروز ۵% طي‌ شش‌ ساعت‌انفوزيون‌ وريدي‌ مي‌شود که‌ به‌ اين‌ مقدارمي‌توان‌ برحسب‌ تحمل‌ بيمار بتدريج‌۰/۲۵mg/kg ـ ۰/۱۲۵ هر روز يا يک‌ روز درميان‌ در هر نوبت‌ افزود.

• اشکال‌ دارويي‌: For Injection: 50mg

 

 


کلوتريمازول

 

• موارد مصرف‌: کلوتريمازول‌ در درمان‌کانديدياز ناشي‌ از کانديدا آلبيکنس‌ و سايرگونه‌هاي‌ کانديدا، کچلي‌ بدن‌ و ران‌ و پاناشي‌ از تريکوفيتون‌ روبروم‌ ، تريکوفيتون ‌منتاگروفيس ‌، اپيدرموفيتون‌ فلوکوزوم‌ وميکروسپوروم‌ کانيس ‌، تيناورسيکالر (ناشي‌ از پيتي‌روسپوروم‌) ، اريپکولار (مالاسزيا فورفور) و در درمان‌ عفونت‌قارچي‌ اطراف‌ ناخن‌ و کچلي‌ ريش‌ و سرمصرف‌ مي‌شود.

• مکانيسم‌ اثر: کلوتريمازول‌ ساخت‌ارگوسترول‌ را مهار کرده‌ و با آسيب‌رساندن‌ به‌ غشاء سلولي‌ قارچ‌ و تغيير درنفوذپذيري‌ آن‌، باعث‌ خروج‌ عناصرضروري‌ داخل‌ سلولي‌ مي‌گردد. اين‌ داروهمچنين‌ ساخت‌ تري‌گليسيريدها وفسفوليپيدها را توسط قارچ‌ مهار مي‌کند.کلوتريمازول‌ باعث‌ افزايش‌ غلظت‌هيدروژن‌ پراکسايد داخل‌ سلول‌ قارچ‌ شده‌که‌ باعث‌ نکروز سلولي‌ و از بين‌ رفتن‌عناصر داخل‌ سلولي‌ مي‌شود. اين‌ دارومانع‌ تبديل‌ بلاستوسپورها به‌ شکل‌ ميسلي‌فعال‌ در کانديدا آلبيکنس‌ مي‌شود.

• فارماکوکينتيک‌: جذب‌ سيستميک‌ اين‌ داروبعد از مصرف‌ پوستي‌ کم‌ است‌ ولي‌ بعد ازمصرف‌ از راه‌ مهبل‌ به‌ ميزان‌ ۱۰ ـ ۳ درصدجذب‌ مي‌شود.

• هشدارها: از تماس‌ دارو با چشم‌ خودداري‌شود.

• نکات‌ قابل‌ توصيه‌:

۱ ـ رعايت‌ نکات‌ بهداشتي‌مانند استفاده‌ از لباس‌ زيرنخي‌ و يا استفاده‌از کاندوم‌ در هنگام‌ مقاربت‌ به‌ درمان‌ کمک‌مي‌کند.

۲ ـ در صورت‌ مصرف‌ دارو براي‌ درمان ‌کانديدياز ، از به‌ کار بردن‌ پانسمان‌ بسته‌ در موضع‌ خودداري‌ شود. ۳ ـ در صورت‌ عدم‌ پاسخ‌ به‌ درمان‌ بعد ازاطمينان‌ از عدم‌ وجود ساير پاتوژنها، دوره‌درمان‌ ممکن‌ است‌ مجددا تکرار شود.

• مقدار مصرف‌: موضعي‌ ـ روزي‌ ۲ بار صبح‌و عصر از محلول‌ يا کرم‌ بر روي‌ موضع‌ ماليده‌ شود.

قرص‌ واژينال‌ ـ در بيماران‌ غير حامله ‌۲۰۰mg/day ترجيحا قبل‌ از خواب‌ به‌ مدت ‌۳ روز يا ۱۰۰mg/day به‌ مدت‌ ۷ روزاستعمال‌ مي‌گردد. کرم‌ واژينال‌ ـ مقدار ۵۰mg/day (يک‌اپليکاتور از کرم‌ يک‌ درصد) ترجيحا قبل‌ ازخواب‌ به‌ مدت‌ ۱۴ ـ ۶ روز استعمال‌مي‌شود.

• اشکال‌ دارويي‌: Topical Cream: 1% Topical Solution: 1% Vaginal Cream: 1% Vaginal Tablet: 100mg

 

 


فلوکونازول‌

 

• موارد مصرف‌: فلوکونازول‌ در درمان‌ عفونتهاي‌ قارچي‌ دهان‌ و حلق ‌، مري ‌، واژن‌ و عفونت هاي‌ سيستميک‌ ناشي‌ از کانديداآلبيکنس‌ و در درمان‌ عفونتهاي‌ قارچي‌پوست‌ مصرف‌ مي‌شود. اين‌ دارو ممکن ‌است‌ به‌ عنوان‌ جايگزين‌ آمفوتريسين‌ در درمان‌ عفونتهاي‌ کريپتوکوکي‌ نيز مصرف‌ شود. فلوکونازول‌ همچنين‌ براي‌ پيشگيري ‌از عود مننژيت‌ کريپتوکوکي‌ در بيماران ‌مبتلا به‌ ايدز و پيشگيري‌ از بروز عفونت هاي‌قارچي‌ در بيماران‌ تحت‌ درمان‌ با پرتو درماني‌ يا داروهاي‌ سيتوتوکسيک‌ مصرف‌ مي شود.

• مکانيسم‌ اثر: فلوکونازول‌ در قارچهاي‌حساس‌ به‌ دارو، آنزيم‌هاي‌ وابسته‌ به‌ راسيتوکروم‌ بيوسنتز p-450 مهار مي‌نمايد وديواره‌ سلولي‌ را مختل‌ مي‌کند.

• فارماکوکينتيک‌: اين‌ دارو از راه‌ خوراکي‌بخوبي‌ جذب‌ مي‌شود. پس‌ از جذب‌ به‌طورگسترده‌ در مايعات‌ بدن‌ منتشر مي‌شود،اوج‌ غلظت‌ سرمي‌ دارو ۲ ـ ۱ ساعت‌ پس‌ ازمصرف‌ خوراکي‌ بدست‌ مي‌آيد. نيمه‌ عمردفع‌ دارو ۳۰ دقيقه‌ است‌ که‌ در بيماران‌مبتلا به‌ عيب‌ کار کليه‌ ممکن‌ است‌ افزايش‌يابد. دفع‌ اين‌ دارو عمدتا کليوي‌ است‌.

• موارد منع‌ مصرف‌: در صورت‌ ابتلاي‌ بيماربه‌ عيب‌ کار کبد يا پورفيري‌، اين‌ دارو نبايدمصرف‌ شود.

• هشدارها:

۱ ـ در صورت‌ نياز به‌ درمان‌طولاني‌ مدت‌ (بيش‌ از ۱۴ روز) با اين‌ دارو،وضعيت‌ کار کبد به‌طور باليني‌ وبيوشيميايي‌ حتما بايد قبل‌ از شروع‌درمان‌، دو هفته‌ پس‌ از شروع‌ درمان‌ و پس‌از آن‌ به‌طور ماهانه‌ پيگيري‌ شود.

۲ ـ در صورت‌ ابتلاي‌ بيمار به‌ عيب‌ کارکليه‌، اين‌ دارو بايد با احتياط فراوان‌مصرف‌ شود.

• عوارض‌ جانبي‌: عوارض‌ گزارش‌ شده‌ براي‌فلوکونازول‌ عبارتند از: تهوع‌، استفراغ‌، دردشکم‌، سردرد، بثورات‌ جلدي‌، کهير وخارش‌، بندرت‌ کاهش‌ پلاکتهاي‌ خون‌،پاراسترني‌، ترس‌ بيمار از نور، سرگيجه‌،آلوپس‌، ژينکوماستي‌، و کاهش‌ مقدار اسپرم‌.همچنين‌ در صورت‌ مصرف‌ طولاني‌ مدت‌دارو (بيش‌ از ۱۴ روز) احتمال‌ بروز هپاتيت‌يا آسيب‌کشنده‌ کبدي‌ وجود دارد.

• تداخل‌هاي‌ دارويي‌: در صورت‌ مصرف‌همزمان‌ ريفامپين‌ با فلوکونازول‌ به‌ دليل‌افزايش‌ پتاسيم‌، غلظت‌ سرمي‌ فلوکونازول‌کاهش‌ مي‌يابد.

فلوکونازول‌ ممکن‌ است‌ درمتابوليسم‌ بعضي‌ از داروها، از جمله‌فني‌توئين‌ و داروهاي‌ سولفونيل‌ اوره‌ پايين‌آورنده‌ قند خون‌، تداخل‌ کند و غلظت‌سرمي‌ اين‌ داروها را افزايش‌ دهد.

همچنين‌افزايش‌ غلظت‌ سرمي‌ سيکلوسپورين‌،نورتريپتيلين‌ و ترفنادين‌ در صورت‌مصرف‌ همزمان‌ با اين‌ دارو گزارش‌شده‌اند که‌ در مورد ترفنادين‌ احتمال‌ بروزواکنشهاي‌ غيرعادي‌ در ECGوجود دارد.فلوکونازول‌ ممکن‌ است‌ اثر وارفارين‌ راافزايش‌ دهد.

• مقدار مصرف‌:

بزرگسالان‌: مقدار مصرف‌ اين‌ دارو درکانديدياز واژينال‌ ۱۵۰ ميلي‌گرم‌ به‌صورت‌دوز واحد است‌. در ساير عفونتهاي‌مخاطي‌ ناشي‌ از کانديدا به‌ غير از کانديديازتناسلي‌، ۵۰mg/day (در عفونتهاي‌ سخت‌۱۰۰mg/day) براي‌ ۱۴ ـ ۷ روز مصرف‌مي‌شود. در برخي‌ از عفونتهاي‌ مخاطي‌مانند التهاب‌ مرکزي‌، کانديدوري‌،عفونتهاي‌ ناي‌ ـ ريوي‌ غيرتهاجمي‌ اين‌مقدار براي‌ ۳۰ ـ ۱۴ روز مصرف‌ مي‌شود.

مقدار مصرف‌ فلوکونازول‌ در درمان‌عفونتهاي‌ قارچي‌ پوست‌ ۵۰mg/day براي‌۴ ـ ۲ هفته‌ تا حداکثر ۶ هفته‌ مي‌باشد. درعفونتهاي‌ تهاجمي‌ کانديديايي‌ ياکريپتوکوکي‌، ابتدا مقدار ۴۰۰ ميلي‌گرم‌ وپس‌ از آن‌ ۲۰۰mg/day که‌ در صورت‌ نيازتا ۴۰۰mg/day افزايش‌ مي‌يابد، مصرف‌مي‌شود. طول‌ دوره‌ درمان‌ به‌ پاسخ‌ بيماربستگي‌ دارد (در مورد مننژيت‌کريپتوکوکي‌ طول‌ دوره‌ درمان‌ حداقل‌ ۸ ـ ۶هفته‌ مي‌باشد).

براي‌ پيشگيري‌ از عود مننژيت‌کريپتوکوکي‌ در بيماران‌ مبتلا به‌ ايدز بعداز تکميل‌ درمان‌ اوليه‌، به‌ مقدار۲۰۰mg/day ـ ۱۰۰ مصرف‌ مي‌شود.همچنين‌ براي‌ پيشگيري‌ از بروز عفونتهاي‌قارچي‌ در بيماران‌ تحت‌ درمان‌ با پرتودرماني‌ يا داروهاي‌ سيتوتوکسيک‌ به‌مقدار ۴۰۰mg/day ـ ۵۰ بسته‌ به‌ احتمال‌بروز عفونت‌ مصرف‌ مي‌شود که‌ درصورت‌ احتمال‌ بروز عفونتهاي‌ سيستميک‌اين‌ مقدار ۴۰۰mg/day خواهد بود.

شروع‌ درمان‌ در اين‌ بيماران‌ قبل‌ از بروزنوتروپني‌ خواهد بود و درمان‌ تا ۷ روزپس‌ از آنکه‌ شمارش‌ نوتروفيلها به‌ حدمطلوب‌ رسيد، ادامه‌ خواهد يافت‌.

در درمان‌کچلي‌ پا، سر، پيتي‌ ريازيس‌ ورسيکالر وکانديدياي‌ پوستي‌، ۵۰mg/day به‌ مدت‌ ۴ ـ ۲هفته‌ (تا حداکثر ۶ هفته‌ در کچلي‌ پا) مصرف‌مي‌شود.

کودکان‌: مقدار مصرف‌ اين‌ دارو در درمان‌عفونتهاي‌ قارچي‌ مخاطي‌ (غير از عفونت‌واژن‌) ۶mg/kg ـ ۳ در روز اول‌ درمان‌ وسپس‌ روزانه‌ ۳mg/kg (هر ۷۲ ساعت‌ درنوزادان‌ با سن‌ کمتر از دو هفته‌ و هر ۴۸ساعت‌ در نوزادان‌ با سن‌ ۴ ـ ۲ هفته‌)مي‌باشد. مقدار مصرف‌ فلوکونازول‌ دردرمان‌ عفونتهاي‌ قارچي‌ پوست‌ درکودکان‌ مانند بزرگسالان‌ است‌. در درمان‌عفونتهاي‌ تهاجمي‌ کانديديايي‌ ياکريپتوکوکي‌ به‌ مقدار ۱۲mg/kg/day ـ ۶(هر ۷۲ ساعت‌ در نوزادان‌ با سن‌ کمتر ازدو هفته‌ و هر ۴۸ ساعت‌ در نوزادان‌ با سن‌۴ ـ ۲ هفته‌) مصرف‌ مي‌شود.

براي ‌پيشگيري‌ از بروز عفونتهاي‌ قارچي‌ ، مقدار مصرف‌ فلوکونازول‌ ۱۲mg/kg/day ـ ۳ (هر ۷۲ ساعت‌ در نوزادان‌ با سن‌ کمتر از دو هفته‌ و هر ۴۸ ساعت‌ در نوزادان‌ با سن‌ ۴ ـ ۲ هفته‌) مي‌باشد.

 

• اشکال‌ دارويي‌: Capsule or Tablet: 50mg, 100mg, 150mg

 

 

 


فلوسيتوزين‌

 

• موارد مصرف‌: فلوسيتوزين‌ در درمان‌عفونتهاي‌ قارچي‌ و مخمري‌ سيستميک‌،همراه‌ با آمفوتريسين‌ يا فلوکونازول‌ دردرمان‌ مننژيت‌ کرپيتوکوکي‌، کانديديازشديد و سيستميک‌ ناشي‌ از کانديداآلبيکنس‌ (اندوکارديت‌، پنوموني‌، سپتي‌سمي‌ و عفونتهاي‌ مجاري‌ ادرار) و همراه‌ باآمفوتريسين‌ در درمان‌ ساير عفونتهاي‌طولاني‌ مدت‌ و شديد مصرف‌ مي‌شود.

• مکانيسم‌ اثر : فلوسيتوزين‌ پس‌ از نفوذ در سلول هاي‌ قارچي‌ ، به‌ فلوئورواوراسيل‌ که‌ يک‌ آنتي‌متابوليت‌ است‌، تبديل‌ مي‌شود. اين‌ترکيب‌ به‌ نوبه‌ خود در متابوليسم‌پيريميدن‌ وارد مي‌گردد و بيوسنتزاسيدهاي‌ نوکلئيک‌ و پروتئين‌ها را مختل‌مي‌سازد.

• فارماکوکينتيک‌: اين‌ دارو بخوبي‌ و بسرعت ‌از مجراي‌ گوارش‌ جذب‌ مي‌شود و پس‌ ازجذب‌ به ‌طور گسترده‌ در تمام‌ بدن‌ منتشر مي‌گردد. غلظت‌ سرمي‌ دارو ۲ ـ ۱ ساعت‌پس‌ از مصرف‌ به‌ اوج‌ خود مي‌رسد. نيمه ‌عمر دارو ۶ ـ ۲/۵ ساعت‌ است‌ که‌ در صورت‌ عيب‌ کار کليه‌ ممکن‌ است‌ به‌ ۲۵۰ ـ ۱۲ ساعت‌ افزايش‌ يابد. دفع‌فلوسيتوزين‌ عمدتا کليوي‌ است‌.

• هشدارها:

۱ ـ اين‌ دارو در موارد زير بايد بااحتياط فراوان‌ مصرف‌ شود: عيب‌ کار کبد و عيب‌ کار کليه‌ (ممکن‌ است‌ به‌کاهش‌ مقدار مصرف‌ و اندازه‌گيري‌ غلظت‌خوني‌ دارو نياز باشد)، بيماران‌سالخورده‌، اختلالهاي‌ خوني‌ (از جمله‌ضعف‌ ـ مغز استخوان‌) و بيماراني‌ که‌ قبلاتحت‌ درمان‌ با داروهاي‌ سيتوتوکسيک‌ ياپرتو درماني‌ بوده‌اند.

۲ ـ در طول‌ مصرف‌ اين‌ دارو، به‌ويژه‌ درصورت‌ ابتلاي‌ بيمار به‌ عيب‌ کار کليه‌ يااختلالهاي‌ خوني‌، ممکن‌ است‌ انجام‌آزمونهاي‌ کار کليه‌ و شمارش‌ خون‌ضروري‌ باشد.

• عوارض‌ جانبي‌: عوارض‌ گزارش‌ شده‌ ناشي‌از مصرف‌ اين‌ دارو عبارتند از کم‌ خوني‌،هپاتيت‌ يا يرقان‌، واکنش‌هاي‌ حساسيت‌مفرط (شامل‌ بثورات‌ جلدي‌، قرمزي‌ ياخارش‌)، کاهش‌ گلبولهاي‌ سفيد و پلاکتهاي‌خون‌، اختلالهاي‌ گوارشي‌ (شامل‌ درد شکم‌،اسهال‌، کاهش‌ اشتها، تهوع‌ و استفراغ‌)،اغتشاش‌ شعور، توهم‌، افزايش‌ حساسيت‌پوست‌ به‌ نور و اثرات‌ CNS(شامل‌ سرگيجه‌يا منگي‌، خواب‌آلودگي‌ و سردرد).

• تداخل‌هاي‌ دارويي‌: فلوسيتوزين‌ ممکن‌است‌ اثر ساير داروهاي‌ تضعيف‌ کننده‌ مغزاستخوان‌ و پرتودرماني‌ را در کاهش‌فعاليت‌ مغز استخوان‌ تشديد نمايد.

• نکات‌ قابل‌ توصيه‌:

۱ ـ احتمال‌ بروزواکنشهاي‌ ناشي‌ از حساسيت‌ پوست‌ به‌نور وجود دارد. از اين‌ رو بيمار نبايد درمعرض‌ نور مستقيم‌ خورشيد قرار گيرد.

۲ ـ در صورت‌ بروز سرگيجه‌، منگي‌ ياخواب‌آلودگي‌ بايد احتياط کرد.

• مقدار مصرف‌:

بزرگسالان‌ و کودکان‌: اين‌ دارو به‌ مقدار۳۷/۵mg/kg ـ ۱۲/۵ هر ۶ ساعت‌ مصرف‌مي‌شود. در بيماران‌ مبتلا به‌ عيب‌ کار کليه‌مي‌توان‌ فواصل‌ مصرف‌ دارو را افزايش‌ داد.

• اشکال‌ دارويي‌: Scored Tablet: 500mg

 

 


گريزئوفولوين

 

• موارد مصرف‌: گريزئوفولوين‌ در درمان‌کچلي‌هاي‌ ريش‌، مو، سر، بدن‌، ران‌، پاها،ناخن‌ و اندام‌ تحتاني‌ ناشي‌ از تريکوفيتون‌،ميکروسپوروم‌ و اپي‌درموفيتون‌فلوکوزوم‌ مصرف‌ مي‌شود.گريزئوفولوين‌ در عفونت‌هاي‌ جزيي‌ که‌تنها با ضد قارچهاي‌ موضعي‌ قابل‌ درمان‌است‌، مصرف‌ نمي‌شود.

• مکانيسم‌ اثر: گريزئوفولوين‌ از ميتوزسلول‌ قارچ‌ جلوگيري‌ کرده‌ و با اين‌ عمل‌تقسيم‌ سلولي‌ را در مرحله‌ متافاز متوقف‌مي‌کند. اين‌ دارو با مقادير متفاوت‌ درسلولهاي‌ پيش‌ساز کراتين‌ پوست‌، مو وناخنها رسوب‌ مي‌کند و اين‌ سلولها را درمقابل‌ تهاجم‌ قارچ‌ مقاوم‌ مي‌سازد و بدين‌ترتيب‌ با ريزش‌ کراتين‌ آلوده‌ بافت‌ سالم‌جانشين‌ آن‌ مي‌شود.

• فارماکوکينتيک‌: جذب‌ خوراکي‌گريزئوفولوين‌ ميکروسايز بين‌ ۷۰ ـ ۲۵درصد در هر نوبت‌ مصرف‌ است‌. مصرف‌همزمان‌ يا متعاقب‌ غذاهاي‌ چرب‌ با اين‌دارو جذب‌ آن‌ را به‌طور قابل‌ توجهي‌افزايش‌ مي‌دهد. اين‌ دارو با مقادير متفاوت‌در لايه‌ کراتيني‌ پوست‌، مو و ناخنها رسوب‌مي‌کند. متابوليسم‌ آن‌ کبدي‌ است‌ و نيمه‌عمر آن‌ تقريبا ۲۴ ساعت‌ است‌. دفع‌ آن‌کليوي‌ است‌.

• هشدارها:

۱ ـ مصرف‌ گريزئوفولوين‌ درنارسايي‌ کبدي‌ و وجود پورفيري‌ بايد بااحتياط فراوان‌ صورت‌ گيرد.

۲ ـ احتمال‌ بروز حساسيت‌ به‌ نور بامصرف‌ اين‌ دارو وجود دارد. از تماس‌ نورخورشيد يا لامپهاي‌ خورشيدي‌ با پوست‌بايد اجتناب‌ شود.

• عوارض‌ جانبي‌: اين‌ دارو ممکن‌ است‌ باعث‌سردرد، تهوع‌، استفراغ‌، بثورات‌ جلدي‌حساسيت‌ به‌ نور، سرگيجه‌، کسالت‌،آگرانولوسيتوز ولکوپني‌ شود.

• تداخل‌هاي‌ دارويي‌: اين‌ دارو باعث‌ افزايش‌متابوليسم‌ داروهاي‌ ضد انعقادي‌کوماريني‌ و داروهاي‌ خوراکي‌ جلوگيري‌کننده‌ از بارداري‌ حاوي‌ استروژن‌مي‌شود.

• نکات‌ قابل‌ توصيه‌:

۱ ـ براي‌ جلوگيري‌ ازعود بيماري‌ درمان‌ بايد تا حذف‌ کامل‌ارگانيسم‌ عامل‌ بيماري‌ ادامه‌ يابد. دوره‌ درمان‌ پيشنهادي‌ براي‌ کچلي‌ سر ۱۰ ـ ۸هفته‌، کچلي‌ بدن‌ ۴ ـ ۲ هفته‌، کچلي‌ پاها ۸ ـ ۴ هفته‌ ، کچلي‌ ناخنهاي‌ دست‌ حداقل‌ ۴ ماه‌ و کچلي‌ ناخن‌هاي‌ پا حداقل‌ ۶ ماه‌است‌. با اين‌ وجود ميزان‌ عود کچلي‌ناخنهاي‌ پا خيلي‌ زياد است‌.

۲ ـ از آنجا که‌ مخمرها و باکتري‌ها مانند قارچ‌ ممکن‌ است‌ در بعضي‌ از اشکال‌بيماري‌ قارچي‌ ورزشکاران‌ وجود داشته‌باشند، معمولا مصرف‌ يک‌ داروي‌ موضعي‌مناسب‌ در درمان‌ کچلي‌ پا مورد نياز است‌.

۳ ـ بمنظور کاهش‌ تحريک‌ گوارشي‌ وافزايش‌ جذب‌ گريزئوفولوين‌، اين‌ دارو بايدهمراه‌ غذا (به‌ويژه‌ غذاهاي‌ چرب‌) و شير ياپس‌ از آن‌ مصرف‌ شود.

۴ ـ در صورت‌ مصرف‌ داروهاي‌ خوراکي‌جلوگيري‌ کننده‌ از بارداري‌ حاوي‌استروژن‌ همزمان‌ با اين‌ دارو، طي‌ مصرف‌ اين‌ دارو و تا يک‌ ماه‌ بعد از آن‌ از ساير روشهاي‌ جلوگيري‌ کننده‌ نيز بايد استفاده‌ شود.

• مقدار مصرف‌:

بزرگسالان‌: در درمان‌ کچلي‌ ناخن‌ و پاهامقدار ۵۰۰ ميلي‌گرم‌ هر ۱۲ ساعت‌ مصرف‌مي‌شود و در درمان‌ کچلي‌ سر و بدن‌ و ران‌مقدار ۲۵۰ ميلي‌گرم‌ هر ۱۲ ساعت‌ يا۵۰۰mg/day تجويز مي‌شود.

کودکان‌: مقدار ۱۰mg/kg ـ ۵ هر ۱۲ ساعت‌يا ۱۰mg/kg/day مصرف‌ مي‌شود. براي‌کودکان‌ با وزن‌ ۲۳ ـ ۱۴ کيلوگرم‌ مقدار ۲۵۰mg/day ـ ۱۲۵ يا ۱۲۵ ـ ۶۲/۵ميلي‌گرم‌ هر ۱۲ ساعت‌ مصرف‌ مي‌شود.در کودکان‌ با وزن‌ ۲۳ کيلوگرم‌ به‌ بالا۵۰۰mg/day ـ ۲۵۰ يا ۲۵۰ ـ ۱۲۵ ميلي‌گرم‌هر ۱۲ ساعت‌ مصرف‌ مي‌شود.

• اشکال‌ دارويي‌: Scored Tablet: 500mg Tablet: 125mg

 

 


نيستاتين

 

• موارد مصرف‌: نيستاتين‌ در درمان‌کانديدياز ناشي‌ از کانديدا آلبيکانس‌ وساير گونه‌هاي‌ کانديدا مصرف‌ مي‌شود.نيستاتين‌ در درمان‌ کچلي‌ ريش‌ و سر هم‌مصرف‌ مي‌شود.

• مکانيسم‌ اثر: نيستاتين‌ با اتصال‌ به‌استرول‌هاي‌ موجود در غشاء سلولي‌ قارچ‌باعث‌ تغيير در نفوذپذيري‌ غشاء شده‌ وباعث‌ مي‌شود که‌ محتويات‌ ضروري‌ داخل‌سلولي‌ قارچ‌ از آن‌ خارج‌ شوند.

• فارماکوکينتيک‌: نيستاتين‌ از مجراي‌ گوارش‌ و يا پوست‌سالم‌ و غشاهاي‌ مخاطي‌ جذب‌ نميشود. تقريبا تمام‌ دارو بعد از مصرف‌خوراکي‌ به‌صورت‌ تغيير نيافته‌ از طريق‌مدفوع‌ دفع‌ مي‌شود. • عوارض‌ جانبي‌: تحريک‌ پوستي‌ که‌ قبل‌ ازدرمان‌ وجود نداشته‌ است‌، از عوارض‌جانبي‌ دارو است‌.

• نکات‌ قابل‌ توصيه‌:

۱ ـ قرص‌ واژينال‌ اين‌ دارو به‌ عنوان‌ قرص‌ مکيدني‌ به‌ جاي‌ سوسپانسيون‌ خوراکي‌ براي‌ درمان ‌کانديدياز دهان‌ نيز قابل‌ مصرف‌ است‌.

۲ ـ در صورت‌ مصرف‌ موضعي‌ دارو ازپانسمان‌ بسته‌ در موضع‌ بايد خودداري‌شود و در صورت‌ مصرف‌ آن‌ در نوزادان‌از پيچيدن‌ سفت‌ پاي‌ بچه‌ و يا استفاده‌ ازشلوارک‌ پلاستيکي‌ نيز بايد اجتناب‌ شود.

• مقدار مصرف‌: خوراکي‌:

بزرگسالان‌: مقدار ۶۰۰,۰۰۰ ـ ۴۰۰,۰۰۰واحد از سوسپانسيون‌ خوراکي‌ ۴ بار درروز يا ۱۰۰۰,۰۰۰ ـ ۵۰۰,۰۰۰ واحد ازقرص‌ ۳ بار در روز مصرف‌ مي‌شود.

کودکان‌: در نوزادان‌ نارس‌ و کم‌ وزن‌ مقدار۱۰۰,۰۰۰ واحد ۴ بار در روز و در نوزادان‌بزرگتر ۲۰۰,۰۰۰ واحد ۴ بار در روزمصرف‌ مي‌شود. مقدار مصرف‌ قرص‌ درکودکان‌ بالاي‌ ۵ سال‌، ۵۰۰,۰۰۰ واحد ۴ باردر روز است‌.

موضعي‌: بزرگسالان‌ و کودکان‌: ۲ يا ۳ بار در روزبر روي‌ پوست‌ ماليده‌ مي‌شود. واژينال‌: مقدار ۱۰۰,۰۰۰ واحد، يک‌ يا دو بار در روزبه‌ مدت‌ ۲ هفته‌ مصرف‌ مي‌شود.

• اشکال‌ دارويي‌: Vaginal Tablet: 100,000 U Coated Tablet: 500,000 U For Suspension Drops: 100,000 U/ml Topical Ointment: 100,000 U/g

 

 


کتوکونازول

 

• موارد مصرف‌: کتوکونازول‌ در درمان‌بلاستوميکوزيس‌ ريوي‌ و منتشر،کانديدياز مري‌، حلق‌ و دهان‌، عفونت‌هاي‌کانديدايايي‌ دستگاه‌ ادراري‌، پنوموني‌،کانديدياز شديد مزمن‌ مخاط پوستي‌ وکانديدياز مهبلي‌ ـ فرجي‌ مصرف‌ مي‌شود . کتوکونازول‌ در درمان‌ پيتي‌ريازيس ‌ورسيکالر ، کچلي‌ بدن‌ ، کروموميکوزيس‌ وکوکسيديوايد و ميکوزيس‌ شديد به ‌عنوان ‌انتخاب‌ دوم‌، کچلي‌ اندامهاي‌ تحتاني‌ و پاي ‌مقاوم‌ به‌ گريزئوفولوين‌ ، ليشمانيوز جلدي ‌عفونت‌هاي‌ قارچي‌ ناخن‌ و اطراف‌ آن‌ وپنوموني‌ قارچي‌، سپتي‌ سمي‌ قارچي‌ واسپوروتريکوزيس‌ منتشر مصرف‌مي‌شود.

• مکانيسم‌ اثر: کتوکونازول‌ بيوسنتزارگوسترول‌ يا ديگر استرول‌ها را مهارمي‌کند و باعث‌ آسيب‌ به‌ غشاء سلول‌ قارچ ‌شده‌ و نفوذ پذيري‌ آن‌ را تغيير مي‌دهد که‌ در نهايت‌ منجر به‌ از دست‌ رفتن‌ عناصرضروري‌ داخل‌ سلولي‌ مي‌گردد.کتوکونازول‌ همچنين‌ بيوسنتزتري‌گليسيريدها و فسفوليپيدها را مهارمي‌کند و فعاليت‌ آنزيم‌ اکسيداتيو وپراکسيداتيو را مختل‌ مي‌کند. کتوکونازول‌تبديل‌ بلاستوسپورها را به‌ شکل‌ ميسلي‌مهاجم‌ در کانديدا آلبيکنس‌ متوقف‌ مي‌کند.

• فارماکوکينتيک‌: فراهمي‌ زيستي‌ دارو حدود۷۵% است‌. متابوليسم‌ کتوکونازول‌ کبدي‌است‌ و راه‌ اصلي‌ دفع‌ آن‌ از طريق‌ صفرامي‌باشد.

• موارد منع‌ مصرف‌: کتوکونازول‌ درصورت‌ وجود حساسيت‌ شديد به‌داروهاي‌ ضد قارچ‌ آزولي‌ نبايد مصرف‌شود.

• هشدارها: مصرف‌ سيستميک‌ کتوکونازول‌در صورت‌ عيب‌ کار کبد، فقدان‌ يا کاهش‌اسيد معده‌ بايد با احتياط فراوان‌ صورت‌گيرد.

• عوارض‌ جانبي‌: خارش‌ و تحريکي‌ که‌ قبل‌ ازمصرف‌ کتوکونازول‌ وجود نداشته‌ است‌از عوارض‌ شايع‌ کتوکونازول‌ موضعي‌مي‌باشد. تهوع‌، استفراغ‌، درد شکم‌،سردرد، بثورات‌ جلدي‌، کهير و بندرت‌ترومبوسيتوپني‌، پارستزي‌، ترس‌ از نور،سرگيجه‌، طاسي‌ و ژينکوماستي‌ نيز بامصرف‌ اين‌ دارو گزارش‌ شده‌ است‌.

• تداخل‌هاي‌ دارويي‌: کتوکونازول‌ با داروهاي‌ هپاتوتوکسيک‌ ، آنتي‌اسيد ، آنتي ‌کولينرژيک‌ ، آنتي ‌اسپاسموديک ‌، آنتاگونيست‌هاي‌ گيرنده‌ H2، امپرازول‌،سوکرالفيت‌، استميزول‌، سيزاپرايد،سيکلوسپورين‌، ايزونيازيد، ريفامپين‌،فني‌توئين‌ و وارفارين‌ تداخل‌ دارد.

• نکات‌ قابل‌ توصيه‌:

۱ ـ کتوکونازول‌ بايدهمراه‌ با غذا مصرف‌ شود.

۲ ـ از تماس‌ اشکال‌ موضعي‌ دارو با چشم‌اجتناب‌ شود.

۳ ـ دوره‌ درمان‌ بايد کامل‌ شود.عفونت‌هاي‌ قارچي‌ ممکن‌ است‌ به‌ دوره‌درمان‌ طولاني‌ نياز داشته‌ باشند.

۴ ـ هنگام‌ مصرف‌ موضعي‌ دارو، مقدارکافي‌ از دارو بايد در موضع‌ مصرف‌ شودبه‌طوري‌ که‌ سطح‌ پوست‌ را بپوشاند.

• مقدار مصرف‌:

بزرگسالان‌: مقدار ۴۰۰mg/day ـ ۲۰۰به‌عنوان‌ ضد قارچ‌ مصرف‌ مي‌شود. براي‌درمان‌ پيتي‌ريازيس‌ ورسيکالر مقدار۲۰۰mg/day به‌ مدت‌ ۱۰ ـ ۵ روز، در درمان‌کانديدياز مهبلي‌ ـ فرجي‌ ۴۰۰mg/day ـ ۲۰۰به‌ مدت‌ ۵ روز، در عفونت‌ اطراف‌ ناخن‌۴۰۰mg/day ـ ۲۰۰، در پنوموني‌ و سپتي‌سمي‌ قارچي‌ ۴۰۰ ميلي‌ گرم‌ تا يک‌ گرم‌ درروز، مصرف‌ مي‌شود.

کودکان‌: در کودکان‌ در کانديدياز مهبلي‌ ـفرجي‌ ۱۰mg/kg ـ ۵ يکبار در روز به‌ مدت‌ ۵روز و در عفونت‌ اطراف‌ ناخن‌ و پنوموني‌ وسپتي‌ سمي‌ قارچي‌ ۱۰mg/kg ـ ۵ يکبار درروز مصرف‌ مي‌شود.

موضعي‌: مقدار مصرف‌ کرم‌ کتوکونازول‌در بزرگسالان‌ در درمان‌ کچلي‌ بدن‌، کچلي‌اندام‌ تحتاني‌، کچلي‌ پا و پيتي‌ ريازيس‌ورسيکالر و کانديدياز پوستي‌ يکبار درروز و در حالات‌ سبورئيک‌ پوستي‌، عفونت‌اطراف‌ ناخن‌، کچلي‌ ريش‌ و پوست‌ سر ۲ يا۳ بار در روز است‌. مقدار مصرف‌ شامپودر بزرگسالان‌ در درمان‌ شوره‌ سر هر ۴روز يکبار به‌ مدت‌ ۴ هفته‌ مي‌باشد که‌ اين‌مقدار مصرف‌ به‌ يکبار هر يک‌ يا دو هفته‌کاهش‌ مي‌يابد.

• اشکال‌ دارويي‌: Scored Tablet: 200mg Shampoo: 2% Topical Cream: 2%

 

 

 

هشدار!    تجويز و تعيين دوز دارو به عهده پزشک مي باشد
و مدفایلز هيچگونه مسئوليتي در خصوص مصرف خود سرانه دارو ندارد

 

 

 


 مدفایلز (بانک جامع فایل های پزشکی)


 

کارشناس پرستاری و علاقه مند به دنیای وب و کامپیوتر

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