奎奴普汀—达福普汀(Quinupristin-Dalfoprisdn)的复合制剂，商品名Synercid，在欧美已正式上市，两者均来源于Streptomycespristinaspiralis，单独应用时均为抑菌药，联合应用具有协同杀菌作用，通过被动扩散作用进入细菌，不可逆地与核糖体50S亚基结合，达福普汀与核糖体结合后，可使核糖体变构，增加其与奎奴普汀的亲和力，奎奴普汀—达福普汀使蛋白质的合成停止于转肽阶段，阻断核糖体合成的蛋白质的外排，使细菌死亡。本药对MSSA、MRSA、甲氧西林敏感的凝固酶阴性葡萄球菌(MSCNS)、MRCNS、链球菌属、屎肠球菌(包括万古霉素耐药菌)均有较强的杀灭作用，对厌氧菌、军团菌及支原体也有良好的抗菌作用，但对粪肠球菌作用差，对多数革兰阴性菌无作用。半衰期为1.5小时，主要经胆汁从肠道排出，少量经尿排出，在各种组织和胆汁中浓度高，但难以透过血脑屏障和胎盘。
有效成份：达福普汀(dalfopristin),喹努普丁(quinupristin)。
剂型：复方冻干粉针剂
本剂为半合成链阳性菌素复方制剂，适用于由多重耐药的革兰阳性菌引起的严重感染，尤其是医院内获得性感染。本剂含有两个普那霉素(Pristinamycin)的半合成衍生物达福普汀与喹努普丁，可与细菌70 s核糖体的50s亚基不可逆地结合，从而抑制细菌蛋白质的合成。达福普汀与细菌核糖体结合后引起核糖体构象改变，使喹努普丁与细菌核糖体的亲和力提高。与达福普汀和喹努普丁单独作用时具有的抑菌作用相比，本剂的杀菌性更能体现出药物的协同作用。
本剂中喹努普丁和达福普汀的血浆半减期分别为3和1小时；血浆Cmax分别为2.56和6.91mg/ml；血浆AUC分别为3.92和43.5mg/ml。两者体内清除率大体相同，表现组织浓度则完全一致，本剂主要经由粪便排泄。
在欧洲进行的Ⅲ期临床研究表明，443例皮肤及软组织感染病人，使用本品7.5mg/kg静脉注射4次，治愈率为71.2%，对金黄色酿脓葡萄球菌的根除率为66.7%。而头孢唑啉及万古霉素对照组的细菌根除率分别为72.5%和75%。298例医院内获得性肺炎病人静脉注射本剂7.5mg/kg，静脉注射4次，治愈率56.3%，万古霉素对照组为58.3%。在欧洲，以色列和美国，针对严重革兰阳性菌感染且使用其它抗菌素治疗无效的690例病人的研究表明，使用本剂7.5mg/kg静脉注射4次治愈率为75%。对401例万古霉素耐药的金黄色葡萄球菌感染病人，使用本剂7.5mg/kg静脉注射4次，治愈率为65.8%。与对照组头孢三嗪相仿。
Quinupristin, Dalfopristin Solution for injection
What is this medicine?
DALFOPRISTIN; QUINUPRISTIN (dal FOE pris tin; kwi NYOO pris tin) is a streptogramin antibiotic. It is used to treat certain kinds of bacterial infections. It will not work for colds, flu, or other viral infections.
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.
What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:
•liver disease
•other chronic illness
•an unusual or allergic reaction to dalfopristin, quinupristin, pristinamycin, virginiamycin, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding
How should I use this medicine?
This medicine is for infusion into a vein. It is usually given by a health care professional in a hospital or clinic setting.
If you get this medicine at home, you will be taught how to prepare and give this medicine. Use exactly as directed. Take your medicine at regular intervals. Do not take your medicine more often than directed. Do not skip doses or stop your medicine early.
It is important that you put your used needles and syringes in a special sharps container. Do not put them in a trash can. If you do not have a sharps container, call your pharmacist or healthcare provider to get one.
Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.
Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.
What may interact with this medicine?
Do not take this medicine with any of the following medications:
•cisapride
•ranolazine
This medicine may also interact with the following medications:
•carbamazepine
•cyclosporine
•dofetilide
•medicines for anxiety or sleep like diazepam, midazolam
•medicines for cholesterol like lovastatin
•medicines for HIV like delavirdine, indinavir, nevirapine, ritonavir
•steroid medicines like methylprednisolone
•tacrolimus
•some medicines for cancer like docetaxel, paclitaxel, vinblastine
•some medicines for irregular heart beat like disopyramide, quinidine, lidocaine
•some medicines for heart disease like diltiazem, nifedipine, verapamil
This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.
What should I watch for while using this medicine?
Your condition will be monitored carefully while you are receiving this medicine.
Do not treat diarrhea with over the counter products. Contact your doctor if you have diarrhea that lasts more than 2 days or if it is severe and watery.
What side effects may I notice from receiving this medicine?
Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•breathing problems
•fast, irregular heartbeat
•feeling faint or lightheaded, falls
•fever or chills
•flushing, reddening of the face and neck
•muscle or joint pain
•numb, tingling pain
•pain at site where injected
•swelling of the arms, hands, legs, or feet
•unusually tired or weak
•yellowing of the eyes or skin
•vomiting
Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•constipation
•difficulty sleeping
•headache
•diarrhea
•nausea
•upset stomach
This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Where should I keep my medicine?
Keep out of the reach of children.
If you are using this medicine at home, you will be instructed on how to store this medicine. Throw away any unused medicine after the expiration date on the label.
