药品名称
伊曲康唑
英文名：itraconazole
主要成份：伊曲康唑

药理毒理　　
药效学　　
伊曲康唑系三唑类衍生物，具有广谱的抗菌活性。　　
体外试验结果显示：伊曲康唑在药物浓度≤0.025~0.8ug/mL小时，可抑制人多种病原性真菌的生长，包括白念珠菌、非白念珠菌属、典霉菌属、毛孢子菌属、地霉菌属，新型隐球菌，皮肤癣菌和多数暗色孢科真菌如产色芽生菌属、组织胞浆菌属、波伊德假霉样真菌和马尔尼非青霉菌属。　　
伊曲康唑不能抑制的主要真菌有接合菌纲（如：根霉菌属、根毛菌属、毛霉属和犁头霉属）、镰刀菌属、足放线病菌属和帚霉菌属。　　
体外试验证明曲康唑可阻碍真菌细胞中麦角固醇的合成，而麦角固醇则是真菌细胞膜的重要组成部分，影响其合成最终产生了抗真菌的作用。
毒理学　　
用小鼠、大鼠,鼠和狗对伊曲康唑的急性毒性和慢性毒性进行了研究，结果显示伊曲康唑的耐受性良好。　　
在妊娠的大鼠和小鼠中使用大剂量的伊曲康唑（分别为40mg/日和80mg/kg日，或更高）时，发现伊曲康唑会增加动物胎仔异常的发生率，并对动物胚胎产生不良影响。　　
在九项致突变试验中，伊曲康唑未显示致突变性。　　
在致癌性研究中，对小鼠给药剂量升至最高80mg/kg时，未显示至癌性，对雄性大鼠剂量升至20mg/kg和对雌性大鼠剂量升至40mg/kg时，未显示致癌性，对雌性大鼠剂量达40mg/kg时，软组织肉瘤的发生率轻微增加，这可能人是由于结缔组织的非肿瘤性、慢性炎症反应增加而致。这些纤维黄样变化被认为与脂类和胆固醇代谢的系统性紊乱有关。此紊乱在大鼠长期毒性研究中的高毒性剂量中也有出现，这也可能与血清胆固醇水平升高有关。

药代动力学　　
空腹服用本品，伊曲康唑的生物利用度量最大。连续给药1-2周后，可达稳态。口服给药2小时（禁食至少2小时后服药）至5小时（与食物同服）血药浓度达峰。连续每日空腹服用单剂量200mg伊曲康唑，稳态血药浓度在1ug/ml（谷值）-2ug/ml（峰值）间波动。本品若与食物同服，则伊曲康唑的稳态浓度约下降25%。　　
伊曲康唑的血浆蛋白结合率为99.8%。伊曲康唑广泛分布于易受真菌感染的组织，肺、肾、肝、胃、脾和肌肉中的药物浓度为相应血药浓度的2-3倍。　　
伊曲康唑经肝脏代谢为多种代谢产物，其中羟基伊曲康唑的体外抗真菌活性与伊曲康唑相当。血浆中羟基伊曲康唑的浓度约为伊曲康唑的2倍。　　
重复口服给药后，伊曲康唑从血浆中双相消除，半衰期为1.5天。经粪便排泄的原药量为3-18%，尿液中原药占0.03%以下。一周内约有35%的剂量以代谢物的形成经尿液排泄。

适应症　　
治疗HIV阳性或免疫系统损害患者口腔和/或食道念珠菌病。　　
对血液系统肿瘤、骨髓移植患者和预期发生中性粒细胞减少症（亦即＜500细胞/UL＝的患者，可预防深部真菌感染的发生。　　
对于伴有发热的中性粒细胞减少症患者，疑为系统性真菌病时，对作为伊曲康唑注射液经验治疗的序贯疗法。

用法用量　　
为达到最佳吸收，本品不应与食物同服。服药后至少1小时内不要进食。　　
对口腔和/或食道念珠菌病，应将本口服液在口腔内含漱约20秒后再吞咽，吞咽后不可用其它液体漱口。
[治疗口腔或食道念珠菌病] 　　
每日口服200mg（2量杯或20ml）分1-2次服用，连服1周。服药1周后若无效，则应再连续用1周。
[预防真菌感染] 　　
每日5mg/kg，分2次服用。在临床试验中，预防治疗开始于细胞抑制治疗前和移植手术一周前，治疗一直持续至嗜中性粒胞数恢复正常（即＞1000个细胞/uI）。
[对于伴有发热的中性粒细胞减少症患者，疑为系统性真菌病时的经验治疗] 首先应给予伊曲康唑注射液进行治疗，推荐剂量为每次200mg、每日2次。给药4次后，改为每次200mg，每日]1次。共使用14日。每剂的输液时间均应1小时上。然后使用伊曲康唑口服液每次200mg（2量杯或20ml）每日2次进行治疗，直至临床意义的嗜中性粒细胞减少症消除。对疑为系统性真菌病发热患者超过28日经验治疗的安全性和有效性尚未明确。
任何疑问，请遵医嘱！
不良反应　　
使用斯皮仁诺口服液时会出现以下不良反应：最常见于胃肠道系统，如：消化不良、恶心、呕吐、腹泻、腹痛和便秘。　　
其次有头痛、可逆性的肝酶升高、肝炎、月经异常、眩晕和过敏反庆（如：瘙痒、皮疹、荨麻疹和血管性水肿）、外周神经系统疾病、Stevens-Johnson综合征、脱发、低血钾、水肿、充血性心力衰和肺水肿。　　
极罕见包括致命的急性肝脏衰竭在内的严重肝脏毒性病例。

禁忌　　
禁用于已知对本品或其赋形剂过敏者。　　
对于孕妇，只有在疾病危及生命且潜在利益大于对胎儿的潜在危害时，方可使用本品。服用本品的育龄妇女，应采取适当的避孕措施，直至治疗结束后的下一次月经后期。　　
禁与以下药物合用：特非那丁、阿司咪唑、咪唑斯汀、西沙必利、三唑化、咪达唑仑口服制剂、多非利特、奎尼丁、匹莫齐特、经CYP3A4酶抑制剂如辛伐他汀和洛伐他汀。
注意事项
1、在一项健康志愿者的研究中，用伊曲康唑注射液治疗，观察到一过性无症状的左室射血分数下降，在下一次输液前消失。这一发现的临床相关性尚不明确。　　
2、伊曲康唑显示有负性肌力作用，与充血性心力衰竭的报告有一定的相关性。伊曲康唑不应用于患有充血性心力衰竭或有充血性心力衰竭病史的患者，除非利明显大于弊评估应考虑的因素有：病症的严重程度、给药方案和充血性心力衰竭的个体危险因素。这些危险期包括心脏疾病，如缺血性或瓣膜性心脏病：严重肺部疾病，如慢性阻塞性肺病，肾功能衰竭和其它水肿性疾病。医生应告知此类患者有关充血性心力衰竭的体征和症状，并谨慎用药，且在治疗期间监测其充血性心力衰竭的体征和症状。如果在治疗期间出现体征和症状，则应停止伊曲康唑的治疗。　　
3、钙通道阻滞剂具到有负性肌力作用，从而会加伊曲康唑的这一作用。伊曲康唑可抑制钙通道阻滞剂的代谢，所以合并使用伊曲康唑和钙通道阻滞剂时需加注意。　　
4、本品有发生药物相互相作用的可能性（参见药的物相互作用项），这些相互作用具有重要的临床意义。　　
5、囊性纤维化：在囊性纤维化患者中观察到，服用本品每次2.5mg/kg、每日2次，达稳态时的伊曲康唑血药浓度存在个体差异。在16岁以上患者中，药50%患者的稳态血药浓度＞250ng/ml，16岁以下患者未达到此血药药浓度。如果患者口服本品无效，应考虑改用伊曲康唑注射液其它方法治疗。　　
6、在使用本品时，极罕见包括可致命性的急性肝脏衰竭在内的严重肝脏毒性的病例。这些患者大多数以前曾患者有肝脏疾病，在使用本品治疗系统性疾病的同时还明显患有一些疾病和/或合用了其它具有肝脏毒性的药物。也有一些患者无明显的肝病危险因素。其中某些病例出现于开始治疗的一个月内，个别病例出现于开始治疗的一周内。接受本品治疗的患者可酌情考虑进行肝功能监测。应指导患者及时向医生报告包括食欲减退、恶心、呕吐、疲劳、腹痛或尿色加深在内的有关肝炎的体征和症状。对于出现这些症状的患者应立即停药，并进行肝功能检查。　　
7、对于肝酶升高，患者有活动性肝病或受到过其它药物肝毒性损伤的患者不应使用本品，除非利益超过对肝脏损害的风险。对这些病例应进行肝酶监测。　　
8、伊曲康唑绝大部分在肝脏代谢。在伊曲康唑胶囊的使用中，观察到肝硬化患者服药后的生物利用度降低，且伊曲康唑的消除半衰期延长。推测伊曲康唑口服液也可能发生此现象。肝功能不全的患者用药可考虑调剂量。　　
9、对肾功能不全的患者，在伊曲康口供胶囊的使用中，观察到伊曲康唑的口服生物利用度降低。推测伊曲康唑口服液也可能发生此现象。此类患者用药可考虑调整剂量。　　
10、当发生可能由本品导致的神经系统症状时应终止治疗。　　
11、尚无有关伊曲康唑和其它类抗真菌药之刘交叉过敏的资料，因此对其它唑类过敏的患者在使用本品时应慎重　
12、本品不影响驾驶及使用机器的能力。　　
13、请置于儿童不易拿到处。
孕妇及哺乳期妇女用药　　
尚未进行伊由康唑对妊娠妇女的研究。对于孕妇，只有在疾病危及生命且潜在利益大于对胎儿的潜在危害时，方可使用本品。服用本品的育龄妇女，应采取适当的避孕措施，直至治疗结束后的下一次月经周期。　　
伊曲康唑经母乳的分泌量很少。对哺乳期妇女使用本品时应权权衡利弊。如有疑问时，应停止母乳喂养。

儿童用药　　
由于斯皮仁诺口服液用于儿童治疗的临床资料有限，因此，不推荐儿童使用本品，儿童只有在利大于弊时，方可使用本品。
老年患者用药　　
由于本品用于老年人的资料有限，老年患者只有在利大于弊时，方可使用本品。
药物相互作用
1．影响伊曲康唑代谢的药物　　
诱酶药物如：利福平、利福布丁和苯妥英可明显降低伊曲康唑的口服生物利用度，而导致疗效降低。因此，本品不应与强效酶诱导药物合用。尚无有关其它酶诱导剂，如卡马西平，苯巴比妥和异烟肼的正式研究，如卡马西平，苯巴比妥和异烟肼的正式研究，但预期的作用相似。　　
由于伊曲康唑主要通过CYP3A4酶代谢。因此，此酶的强抑制剂可增加伊曲康唑的生物利用度如；利托那韦、克拉霉素和红霉素。
2．伊曲康唑对其它药物代谢的影响
2.1伊曲康唑会抑制由细胞色素3A酶代谢的药物的代谢，这会导致药物作用的增加和/或延期长（包括副作用）。停用伊曲康唑治疗后，伊曲康唑血浆浓度逐渐下降，其下降速度取决于用药量和用药时间（参见药代动力学项），当考虑伊曲康唑和用药对同服药物的抑制作用时，应考虑此特点。
例如：在使用本品治疗期间不应使用的药物：　　
特非那丁、阿司咪唑、咪唑斯汀、西沙必利、三唑化、咪达唑仑口服制剂、多非利特、奎尼丁、匹莫齐特、经CYP3A4酶代谢的羟甲基戊二酰辅酶A（HMG-COA）还原酶抑制剂如辛伐他汀和洛伐他汀。　　
钙通道阻滞剂具有负性肌力作用。从而会加强伊曲康唑的这一作用。伊曲康唑可抑制钙通道阻滞剂的代谢，所以合并使用伊曲康唑和钙通道阻滞剂时需加注意。　　
若与本品同服，需监测血浆浓度、药物作用及副作用，必要时应减少剂量的药物：
口服抗凝剂　　
抗艾滋病病毒的蛋白酶抑制剂如：利托那韦、茚地那韦和沙奎那韦。　　
一些抗肿瘤药物如：长春生物碱、白消安、多烯紫杉醇和三甲曲沙。　　
CYP3A4酶代谢的钙通道阻断剂如二氢吡啶和维拉帕米。　　
一些免疫抑制剂如：环孢霉素、他克莫司、雷帕霉素（亦称sirolimus）。　
其它：地高辛、卡马西平、丁螺环酮、阿芬太尼、阿普唑仑、溴替唑仑，咪仑注射剂、利福布丁，甲基泼尼松龙，依巴斯汀、瑞波西汀。
2.2尚未观察到伊曲康唑与齐多夫定（AZT）和氟伐他汀的相互作用。尚未观察到伊曲康唑对炔雌醇和炔诺酮代谢的诱导效应。
3. 对蛋白结合的影响 　　
体外研究表明：在血奖蛋白结合方面伊曲康唑与丙咪嗪、普萘洛尔、安定，西咪替丁，引哚美辛、甲苯磺丁脲和磺胺二甲基嘧喧之间无相互作用。

药物过量　　
一旦发生意外过量，应采取支持疗法。在摄入后1小时内可采取洗胃法。若有必要，可给予活性炭。　　
本品不能经过血液透析清除。本品无特殊的解救药。

【原产地英文商品名】ITRACONAZOLE CAPSULE 100mg/cap 28caps/box
【原产地英文药品名】ITRACONAZOLE
【中文参考商品译名】
注：以下产品不同规格和不同价格，购买时请以电话咨询为准！
·伊曲康唑胶囊 100毫克/胶囊 30胶囊/盒
·伊曲康唑胶囊 100毫克/胶囊 28胶囊/盒
【中文参考药品译名】伊曲康唑

Sporanox
Generic Name: itraconazole (IT ra KON a zole)
Brand Names: Sporanox
What is Sporanox?
Sporanox is an azole antifungal medicine. It kills sensitive fungi by interfering with the formation of the fungal cell membrane.
Sporanox is used to treat three types of serious fungal infections (blastomycosis, histoplasmosis, and aspergillosi) which can invade any part of the body including the lungs, mouth or throat, toenails, or fingernails.

Sporanox may also be used for other purposes not listed in this medication guide.
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Important information about Sporanox
Do not take Sporanox if you are allergic to itraconazole or similar medications such as fluconazole (Diflucan) or ketoconazole (Nizoral), if you have ever had congestive heart failure, or if you are pregnant or may become pregnant during treatment.
You should not take Sporanox together with cisapride (Propulsid), dihydroergotamine (D.H.E. 45, Migranal), dofetilide (Tikosyn), ergonovine (Ergotrate), ergotamine (Ergomar), lovastatin (Altocor, Altoprev, Mevacor), methylergonovine (Methergine), midazolam (Versed), nisoldipine (Sular), pimozide (Orap), quinidine (Quinaglute, Quinidex, Quin-Release), simvastatin (Zocor), or triazolam (Halcion).
Other drugs that should not be taken together with Sporanox include astemizole (Hismanal), or levomethadyl Orlaam) (these drugs are no longer available in the U.S.).
There are many other medicines that can interact with Sporanox. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor. Keep a list with you of all the medicines you use and show this list to any doctor or other healthcare provider who treats you.
Before taking Sporanox, tell your doctor if you have heart disease, a history of stroke, a heart rhythm disorder, kidney or liver disease, a breathing disorder, cystic fibrosis, or a history of "Long QT syndrome."
Sporanox capsules should not be used in place of Sporanox oral solution (liquid) if that is what your doctor has prescribed. Make sure you have received the correct type of this medication at the pharmacy and ask the pharmacist if you have any questions. Take this medication for the entire length of time prescribed by your doctor. Your symptoms may get better before the infection is completely treated. Call your doctor if your symptoms do not improve.
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Before taking Sporanox
Do not take Sporanox if you are allergic to itraconazole or similar medications such as fluconazole (Diflucan) or ketoconazole (Nizoral), if you have ever had congestive heart failure, or if you are pregnant or planning to become pregnant during treatment. The following drugs should not be taken together with Sporanox:cisapride (Propulsid);
dofetilide (Tikosyn);
nisoldipine (Sular);
pimozide (Orap);
quinidine (Quinaglute, Quinidex, Quin-Release);
lovastatin (Altocor, Altoprev, Mevacor) or simvastatin (Zocor);
midazolam (Versed) or triazolam (Halcion);
ergot medicines such as dihydroedrgotamine (D.H.E. 45, Migranal), ergonovine (Ergotrate), ergotamine (Ergomar, Cafergot, Ercaf, Migergot), or methylergonovine (Methergine); or
(these drugs are no longer available in the U.S.) astemizole (Hismanal), or levomethadyl Orlaam).
If you have any of the following conditions, you may need a dose adjustment or special tests to safely take Sporanox:
heart disease, a heart rhythm disorder, circulation problems, or a history of stroke;
chronic obstructive pulmonary disease (COPD) or other breathing disorder;
kidney disease;
liver disease;
cystic fibrosis; or
a personal or family history of "Long QT syndrome."
FDA pregnancy category C. It is not known whether Sporanox is harmful to an unborn baby. Before taking this medication, tell your doctor if you are pregnant or plan to become pregnant during treatment. Itraconazole passes into breast milk and can harm a nursing baby. Do not use Sporanox without telling your doctor if you are breast-feeding a baby.
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How should I take Sporanox?
Take Sporanox exactly as it was prescribed for you. Do not take the medication in larger amounts, or take it for longer than recommended by your doctor. Follow the directions on your prescription label.
The Sporanox capsule should be taken after a full meal. Take Sporanox oral solution (liquid) on an empty stomach, at least 1 hour before or 2 hours after a meal. Swish the liquid in your mouth for several seconds before swallowing it.
Measure liquid medicine with a special dose-measuring spoon or cup, not a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist for one.
Sporanox capsules should not be used in place of Sporanox oral solution (liquid) if that is what your doctor has prescribed. Make sure you have received the correct type of this medication at the pharmacy and ask the pharmacist if you have any questions. Take this medication for the entire length of time prescribed by your doctor. Your symptoms may get better before the infection is completely treated. Call your doctor if your symptoms do not improve.
To be sure this medication is not causing harmful effects, your liver function may need to be checked with blood tests on a regular basis. Do not miss any scheduled appointments.
Store Sporanox at room temperature away from moisture, heat, and light.
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What happens if I miss a dose?
Take the missed dose as soon as you remember. If it is almost time for your next dose, skip the missed dose and take the medicine at your next regularly scheduled time. Do not take extra medicine to make up the missed dose.
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What happens if I overdose?
Seek emergency medical attention if you think you have used too much of this medicine. Symptoms of an Sporanox overdose are not known.
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What should I avoid while taking Sporanox?
Avoid taking antacids or stomach acid reducers (Tagamet, Pepcid, Axid, Zantac, and others) within 1 hour before or 2 hours after you take Sporanox. These medications can make it harder for your body to absorb Sporanox.
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Sporanox side effects
Get emergency medical help if you have any of these signs of an allergic reaction tp Sporanox: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Call your doctor at once if you have any of these serious side effects:
fever;
feeling short of breath, even with mild exertion;
swelling, rapid weight gain;
problems with hearing;
numbness or tingly feeling;
pain or burning when you urinate; or
nausea, stomach pain, low fever, loss of appetite, weakness, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes).
Less serious Sporanox side effects may include:
diarrhea, constipation, mild stomach pain;
mild itching or skin rash;
headache, dizziness; or
runny nose or other cold symptoms.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
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What other drugs will affect Sporanox?
Many drugs can interact with Sporanox. Below is just a partial list. Tell your doctor if you are using:
a blood thinner such as warfarin (Coumadin);
cancer medications;
cholesterol medications such as atorvastatin (Lipitor);
cyclosporine (Gengraf, Sandimmune, Neoral);
diabetes medication you take by mouth;
digoxin (digitalis, Lanoxin);
disopyramide (Norpace);
fentanyl (Actiq, Duragesic);
isoniazid (for treating tuberculosis);
rifabutin (Mycobutin), rifampin (Rifadin, Rimactane, Rifater, Rifamate), or rifapentine (Priftin);
sirolimus (Rapamune) or tacrolimus (Prograf);
an antibiotic such as clarithromycin (Biaxin), erythromycin (E.E.S., E-Mycin, Ery-Tab, Erythrocin), telithromycin (Ketek) or troleandomycin (Tao);
an antifungal medication such as clotrimazole (Mycelex Troche), ketoconazole (Nizoral), or voriconazole (Vfend);
an antidepressant such as nefazodone, paroxetine (Paxil), or sertraline (Zoloft);
a barbiturate such as amobarbital (Amytal), butabarbital (Butisol), mephobarbital (Mebaral), secobarbital (Seconal), or phenobarbital (Solfoton);
heart or blood pressure medications such as amlodipine (Norvasc), diltiazem (Tiazac, Cartia, Cardizem), felodipine (Plendil), nifedipine (Procardia, Adalat), verapamil (Calan, Covera, Isoptin, Verelan), and others;
HIV/AIDS medicine such as atazanavir (Reyataz), delavirdine (Rescriptor), efavirenz (Sustiva), etravirine (Intelence), indinavir (Crixivan), nelfinavir (Viracept), nevirapine (Viramune), saquinavir (Invirase, Fortovase), or ritonavir (Norvir);
a sedative such as alprazolam (Xanax), diazepam (Valium); or
seizure medication such as carbamazepine (Carbatrol, Tegretol), felbamate (Felbatol), oxcarbazepine (Trileptal), or phenytoin (Dilantin), or primidone (Mysoline).

This list is not complete and there are many other medicines that can interact with Sporanox. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor. Keep a list with you of all the medicines you use and show this list to any doctor or other healthcare provider who treats you.
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Where can I get more information?
Your pharmacist can provide more information about Sporanox.

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.
Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.