Synercid（喹奴普丁/达福普丁）复方冻干粉针剂

有效成份：达福普汀(dalfopristin),喹努普丁(quinupristin)。

剂型：复方冻干粉针剂

开发与上市厂商
(法)Rhone-Poulenc Rorer公司研制，1999年10月在英国首次上市。
作用

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。

临床评价
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。

适应证

本剂适用于革兰阳性菌引起的且使用其它药物治疗无效的皮肤及软组织感染，医院内获得性肺炎及粪肠球菌引起的感染。

不良反应：
常见的不良反应有注射部位不适，烦燥，头痛，关节疼痛及肌痛。

注意事项：

肝肾功能不全病人及孕妇禁用本剂。

用法与用量：

剂量为7.5mg/kg，以5%葡萄糖注射液输注，时间在60分钟以上。

规格与包装：

注射剂，每瓶含主药500mg。

Synercid（复方冻干粉针剂）获批准治疗肺炎有效

链阳性菌素类抗菌剂喹奴普丁/达福普丁（Synercid）对于革兰氏阳性球菌（屎肠球，金黄色葡萄球菌或肺炎链球菌）包括许多对目前所用药物耐药的阳性球菌有良好的活性。其活性可和万古霉素治疗医院获得性肺炎相比。在该研究中，喹双普丁、达福普丁（Synercid）和万古霉素接受者在治疗结束后7-13天的临床成功率无明显差异；在甲氧西林耐药苏金黄色葡萄球菌感染病人的亚组中也无明显差异。

喹奴普丁/达福普丁（Synercid）于1999年12月在EU批准治疗获得性肺炎，皮肤和软组织感染及由证明对其它所有合适的抗菌剂都耐药的耐万古霉素的屎肠球菌（VREF）引起的重要感染。

Important note
HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

Monograph title
QUINUPRISTIN/DALFOPRISTIN - INJECTION

Common brand name(s)
Synercid

Uses
This medication is a combination of 2 antibiotics. It is used to treat certain serious bacterial infections that have not responded to treatment with other antibiotics (resistant infections). This medication belongs to the class of antibiotics called streptogramins. Quinupristin/dalfopristin works by stopping the growth of bacteria.

How to use
This medication is given by injection into a vein as directed by your doctor, usually 2 to 3 times daily. It should be injected slowly over 1 hour. The dosage is based on your medical condition, body weight, and response to treatment.If you are giving this medication to yourself at home, learn all preparation and usage instructions from your health care professional. Before using, check this product visually for particles or discoloration. If either is present, do not use the liquid. Learn how to store and discard medical supplies safely.Antibiotics work best when the amount of the medicine in your body is kept at a constant level. Therefore, use this drug at evenly spaced intervals.Continue to use this medication for the full time prescribed, even if symptoms disappear after a few days. Stopping the medication too early may allow bacteria to continue to grow, which may result in a return of the infection.Tell your doctor if your condition persists or worsens.

Missed dose
For the best possible benefit, it is important to receive each scheduled dose of this medication as directed. If you miss a dose, contact your doctor or pharmacist immediately to establish a new dosing schedule. Do not double the dose to catch up.

Precautions
Before using quinupristin/dalfopristin, tell your doctor or pharmacist if you are allergic to it; or to other streptogramin antibiotics (e.g., pristinamycin, virginiamycin); or if you have any other allergies.

This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver problems, high levels of bilirubin in the blood (hyperbilirubinemia).During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.It is not known whether this drug passes into breast milk. Consult your doctor before breast-feeding.

Side effects
Nausea, vomiting, diarrhea, and headache may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including:joint/musclepain,redness/swelling/pain/warming of the skin at the injection site, yellowing eyes/skin, blood in the urine.Get medical help right away if you experience this rare but very serious side effect: chest pain.This medication may rarely cause a severe intestinal condition (Clostridium difficile-associated diarrhea) due to a type of resistant bacteria.

This condition may occur during treatment or weeks to months after treatment has stopped. Do not use anti-diarrhea products or narcotic pain medications if you have any of the following symptoms because these products may make them worse.

Tell your doctor immediately if you develop: persistent diarrhea, abdominal or stomach pain/cramping, blood/mucus in your stool.Use of this medication for prolonged or repeated periods may result in oral thrush or a new vaginal yeast infection. Contact your doctor if you notice white patches in your mouth, a change in vaginal discharge, or other new symptoms.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

Drug interactions
See also How to Use.Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug include: digoxin.This drug can slow down the removal of certain medications from your body by affecting certain liver enzymes.

These affected drugs include those that may affect the heart rhythm (QTc prolongation in the EKG), infrequently resulting in serious (rarely fatal) irregular heartbeat. Quinupristin/dalfopristin should not be used with the following medications because very serious interactions may occur: certain antiarrhythmic drugs (e.g., amiodarone, disopyramide, quinidine), cisapride, certain macrolide antibiotics (e.g., erythromycin, clarithromycin), certain antipsychotics (e.g., haloperidol, pimozide).If you are currently using any of these medications listed above, tell your doctor or pharmacist before startingquinupristin/dalfopristin.Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use, especially of: digoxin.This drug can also slow down the removal of other drugs from your body by affecting certain liver enzymes. Before taking quinupristin/dalfopristin, tell your doctor or pharmacist if you are taking any of the following medications: certain drugs to suppress the immune system (e.g., cyclosporine, sirolimus, tacrolimus), certain drugs to treat HIV (e.g., delavirdine, indinavir, nevirapine, ritonavir), certain anti-cancer drugs (e.g., docetaxel, paclitaxel, vinblastine, vincristine), calcium channel blockers (e.g., diltiazem, nifedipine, verapamil), certain "statin" drugs to lower cholesterol (e.g., atorvastatin, lovastatin, simvastatin), certain benzodiazepines (e.g., diazepam, midazolam), carbamazepine, corticosteroids (e.g., methylprednisolone), drugs to treat erectile dysfunction (e.g., sildenafil, tadalafil, vardenafil).Although most antibiotics probably do not affect hormonal birth control such as pills, patch, or ring, some antibiotics may decrease their effectiveness.

This could cause pregnancy. Examples include rifamycins such as rifampin or rifabutin. Be sure to ask your doctor or pharmacist if you should use additional reliable birth control methods while using this antibiotic.

Overdose
If overdose is suspected, contact your local poison control center or emergency room immediately. US residents can call the US National Poison Hotline at 1-800-222-1222. Canada residents can call a provincial poison control center.

Notes
Laboratory and/or medical tests (e.g., liver function tests) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

Storage
Consult the product instructions and your pharmacist for storage details. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

粉针
赛诺菲 - 安万特公司生产的

美国是KING PHARMS

SYNERCID达福普汀，奎奴普丁350MG/VIAL的;150MG/VIAL注射; IV（输液）

SYNERCID  DALFOPRISTIN; QUINUPRISTIN  350MG/VIAL; 150MG/VIAL  INJECTABLE; IV (INFUSION)

Generic Name for SYNERCID
Quinupristin/dalfopristin 500mg per vial (as 150mg quinupristin and 350mg dalfopristin); pwd for IV infusion after reconstitution; preservative-free.

Legal Classification:
Rx

Pharmacological Class for SYNERCID
Streptogramin.

Manufacturer of SYNERCID
King Pharmaceuticals, Inc.

Indications for SYNERCID
Treatment of serious or life-threatening susceptible infections associated with vancomycin resistant E. faecium (VREF) bacteremia. Complicated skin and skin structure infections due to S. aureus (methicillin-susceptible) or S. pyogenes.

Adult dose for SYNERCID
≥16 years: VREF bacteremia: 7.5 mg/kg every 8 hours; base duration of therapy on infection site and severity. Complicated skin and skin structure: 7.5 mg/kg every 12  hours for at least 7 days.

Children's dosing for SYNERCID
<16 years: not recommended; doses of 7.5 mg/kg every 8 or 12 hours have been used in a limited number of children under emergency-use conditions (see literature).

Warnings/Precautions for SYNERCID
Hepatic insufficiency. Pregnancy (Cat.B). Nursing mothers.

Interactions for SYNERCID
Avoid use with drugs that can cause QTc prolongation. Caution with these and with other drugs metabolized by CYP3A4 (e.g., cyclosporine, midazolam, calcium channel blockers, cisapride, vinca alkaloids, steroids, non-nucleoside reverse transcriptase inhibitors, statins, protease inhibitors); monitor appropriately.

Adverse Reactions for SYNERCID
Inj site reactions, arthralgia, myalgia, GI upset, thrombophlebitis, rash, headache, pruritus.

How is SYNERCID supplied?
Single-dose vials—10

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