部分中文磷苯妥英钠处方资料（仅供参考）
英文药名: Cerebyx (Fosphenytoin Injections)
中文药名: 磷苯妥英钠注射液
用法用量
按本品75mg相当于苯妥英钠50mg等效剂量计算，在非紧急情况时静注或肌注苯妥英钠10～20mg/kg，最初苯妥英钠维持剂量为4～6mg/(kg.d)。静注治疗癫痫发作的苯妥英钠剂量15～20mg/kg。静脉输注前以5%葡萄糖液或0.9%氯化钠注射液稀释本品制剂，稀释后本品浓度范围为1.5～25mg/ml（苯妥因钠），稀释液置室温8h或2～8℃24h是稳定的。
药理作用
本品是在全世界第一个被批准上市的苯妥英钠前体药，具有高效抗惊厥作用。通过小鼠抗电休克试验测得本品腹腔注射或口服给药的抗惊厥作用（抗最大电休克发作）半数有效剂量ED50（mg/kg）各为10.3、11.8，苯妥英的腹腔注射或口服给药ED50（mg/kg）各为9.5、0.4，表明本品与苯妥英具有同等程度的抗惊厥作用。但是小鼠腹腔注射给红色的旋转毒性TD50(mg/kg)本品为42.1苯妥英为65.4，本品旋转毒性较苯妥英大些，这是由于本品是苯妥英的前体，容易被机体吸收所致。给大鼠腹腔注射高半胱氨酸5.5mmol/kg引起大鼠癫发作，将动物分组，每组9只大鼠，分别腹腔给本品130mg/kg和苯妥英120mg/kg，用脑电图监察给药结果。给药后30min，本品在大鼠脑内浓度几乎与苯妥英相同，60min时未测得本品血药浓度峰值，但是在给药后1~2h期间苯妥英给药组大鼠的血药浓度及脑内浓度变化较本品组显著接收本品的大鼠没有1只中止癫发作，而苯妥英组大鼠有4只中止发作，此结果差异在于本品注射后转化为苯妥英需要一定时间。
本品与苯妥英相似具有抗心律失常作用。本品为苯妥因前体药，在豚鼠动脉的体外试验中，因本品未转化为苯妥因而无抗心律失常作用，而苯妥英显示抗心律失常作用。可是在动物体内本品与苯妥英等效地拮抗哇巴因引起的心律失常。以麻醉狗进行试验评价本品对心血管作用。分别静注本品27mg/kg、苯妥英18mg/kg（两药为等分子剂量）。迅速静注苯妥英的狗立即发生及明显降低左心室压力增高率、降低平均动脉压和心率，然后反射性地加快心率。而本品仅引起较小的血流动力学变化。这与本品不引起临床上明显的心血管系统的不良反应是一致的。
适应症
本品用于控制原发性癫痫病人的痉挛症状，预防并治疗神经外科手术中惊厥的发作。
不良反应
常见不良反应为眼球震颤、眩晕、瘙痒、感觉异常、头痛、嗜睡和运动失调。除了感觉异常和瘙痒外，其余的不良反应静注较肌注为常见。按折算为苯妥英钠剂量计，以150mg/min速率静注，剂量为≥15mg/kg时约有2/3病人发生不舒适感。
注意事项
对本品或其制剂成分、苯妥英或其他乙内酰脲药物过敏者禁用，心功能异常者禁用。紫质症病人慎用本品，因苯妥英可使其症状加重。与苯妥英有相互作用的药物也可与本品发生作用，如影响血浆蛋白结合或细胞色素P450酶系统的药物，使用时需注意。
抗癫痫药物苯妥英和磷苯妥英钠可能导致患者严重皮肤不良反应.
近日，FDA发布抗癫痫药苯妥英（Phenytoin）和磷苯妥英钠（Fosphenytoin
Sodium）可能导致相同严重皮肤不良反应的信息。2007年度，FDA曾发布的药物信息中指出携带HLA-B*1502等位基因的患者在服用抗癫痫药卡马西平（Carbamazepine）时可能导致致命的皮肤反应，包括史蒂文斯-约翰逊综合征（Stevens Johnson syndrome，SJS）和中毒性表皮坏死松解症（toxic epidermal necrolysis，TEN），这一特殊基因大多出现在亚裔人群中。
磷苯妥英钠是一个前体药物，在体内转化为苯妥英，因此任何与苯妥英相关的信息都适用于磷苯妥英钠。而苯妥英与卡马西平均属于二苯并氮卓类抗癫痫药物，结构相近，作用机理也类似。目前的数据显示，苯妥英与SJS/TEN之间的关联性已被证实，而HLA-B*1502等位基因与苯妥英导致SJS/TEN之间可能存在某种关联，证实这一关联性的研究尚在进行。在这项研究结束以前，FDA建议医护人员在为携带HLA-B*1502等位基因的患者提供苯妥英和磷苯妥英钠时应充分考虑使用该药的风险利益信息，同时应避免为这类患者提供苯妥英和磷苯妥英作为卡马西平的替代药物。
GENERIC NAME: FOSPHENYTOIN - INJECTION (foss-fen-eh-TOE-in)
BRAND NAME(S): Cerebyx
USES: Fosphenytoin is an anticonvulsant, it is used to treat or
prevent seizures.
HOW TO USE: This medication is injected into a vein (IV) or a muscle(IM). This medication will be used until you can take an oral form of the drug. Follow all instructions for correct mixing and dilution with IV fluids. Consult your pharmacist.
Learn how to store and discard needles and medical supplies safely. Consult your pharmacist. Before using, check this product visually for particles or discoloration. If either is present, do not use the liquid. Do not discontinue this medication, or any other seizure medication, without your doctor's approval.
SIDE EFFECTS: Burning/tingling sensations, groin pain, itching, nausea, dizziness, or drowsiness may occur. If any of these effects persist or worsen, contact your doctor or pharmacist promptly.
Tell your doctor immediately if any of these serious side effects occur: mental/mood changes, loss of coordination, rash, eye/vision problems. Tell your doctor immediately if any of these unlikely but serious side effects occur: seizures, difficulty speaking, muscle
twitching/tremors, severe headache. Tell your doctor immediately if any of these highly unlikely but very serious side effects occur: chest pain, changes in hearing, increased thirst/urination, unusually fast/slow/irregular pulse, unusual fatigue, unusual bruising, severe stomach pain, joint/muscle pain, swollen glands, change in the amount of urine. An allergic reaction to this drug is unlikely, but seek medical attention immediately. Symptoms of an allergic reaction include: itching, rash, swelling, dizziness, yellowing skin/eyes, dark urine, fever, trouble breathing.
If you notice other effects not listed above, contact your doctor or pharmacist.
PRECAUTIONS: Tell your doctor your medical history, especially: any alcohol use, low blood pressure, blood disorders (e.g., anemia, porphyria), thyroid problems (hypothyroid), diabetes, immune disorders (systemic lupus erythematosus), liver or kidney problems, any allergies (especially to phenytoin, phenobarbital, ethosuximide, or carbamazepine). This medication is not recommended for use if you have the following conditions: heart problems (e.g., sinus bradycardia, second and third degree A-V block). This drug may make you dizzy or drowsy; use caution engaging in activities requiring alertness such as driving or using machinery.
Avoid alcoholic beverages. Caution is advised when using this drug in the elderly because they may be more sensitive to the effects this drug may have on the heart. This medication is not recommended for use during pregnancy.
Consult your doctor for more details. It is not known if this medication passes into breast milk. Consult your doctor before breast-feeding.
DRUG INTERACTIONS: Tell your doctor or pharmacist of all prescription and nonprescription drugs you may use, especially: other seizure drugs (e.g., carbamazepine, valproic acid, phenobarbital), "blood thinners" (e.g., warfarin), corticosteroids(e.g., prednisone), hormone replacement therapy (e.g., estrogens), rifamycin antibiotics (e.g., rifampin, rifabutin), heart drugs(e.g., quinidine, amiodarone, nifedipine, digoxin, dopamine), vitamin supplements (e.g., vitamin D, folic acid), azole antifungal drugs (e.g., ketoconazole, itraconazole), anti-ulcer drugs (e.g., cimetidine, omeprazole, sucralfate), antidepressant drugs (e.g., amitriptyline, trazodone, fluoxetine), NSAIDs (e.g., ibuprofen, phenylbutazone), certain diabetes medications (e.g., diazoxide, tolbutamide), sulfa drugs (e.g., sulfamethoxazole), trimethoprim, chloramphenicol, disulfiram, doxycycline, anti-cancer drugs, methadone, chlordiazepoxide, metyrapone, pyrimethamine, xanthines(e.g., theophylline, aminophylline), levodopa, cyclosporine, isoniazid, capecitabine. Also, tell your doctor if you use any of the following drowsiness-causing drugs: sleep aids, sedatives,
tranquilizers, anti-anxiety drugs like diazepam, narcotic pain relievers like codeine, psychiatric medicines, muscle relaxants, antihistamines like diphenhydramine. Check the labels carefully on all your medicines (e.g., cough- and-cold preparations) because they may contain drowsiness- causing ingredients. Ask your pharmacist about safe use of those products.
This medication may interfere with the effectiveness of birth control pills. Consult your doctor or pharmacist about other forms of birth control.
This drug may interfere with certain laboratory tests. Make sure laboratory personnel and your doctors know you use this drug. Do not start or stop any medicine without doctor or pharmacist approval.
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. Canadian residents should call their local poison control center directly. Symptoms of overdose may include nausea, vomiting, unconsciousness; unusually fast or slow heartbeat; muscle weakness or aches; severe dizziness, drowsiness, or stomach pain; fainting, or rapid breathing.
NOTES: Laboratory and/or medical tests may be performed to monitor your progress.
MISSED DOSE: If you miss a dose, contact your doctor or pharmacist promptly to establish a new dosing schedule.
STORAGE: Store vials in the refrigerator between 36 and 46 degrees F(2 to 8 degrees C) away from light and moisture. After proper mixing with correct IV fluids (consult your pharmacist for details), this medication is stable at room temperature for 8 hours and for 24 hours when refrigerated. Discard any unused liquid.
MEDICAL ALERT: Your condition can cause complications in a medical emergency. For enrollment information call MedicAlert at 1-800-854-1166 (USA), or 1-800-668-1507 (Canada).
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