最近的临床研究报告显示:Carter-Wallace公司的抗癫痫新药Felbamate商品名Felbamyl是治疗顽固发作癫痫突发的安全而有效的单方药物,同时也对Lennox-Gastaut氏综合症有增效作用。目前,Felbamate已提请美国FDA审批。
本品为氨基甲酸酯的衍生物。合成本品由2-苯基-1,3-丙二醇与氨甲酸甲酯进行酯交换反应而制得[J MedChem 1969,12(3)∶462]。药理本品为低毒性的具独特的抗惊厥作用谱的抗癫痫药.

中文别名：  非尔氨酯、非巴马特
药品类别：  镇静、催眠药

药理药动
	Classification: Anticonvulsant, miscellaneous (second-line therapy) Action/Kinetics: Mechanism not known. Felbamate may reduce seizure spread and increase seizure threshold. Has weak inhibitory effects on both GABA and benzodiazepine receptor binding. Well absorbed after PO use. Terminal t1/2: 20-23 hr. Trough blood levels are dose dependent. From 40% to 50% excreted unchanged in the urine.

适 应 症
	Alone or as part of adjunctive therapy for the treatment of partial seizures with and without generalization in adults with epilepsy. As an adjunct in the treatment of partial and generalized seizures associated with Lennox-Gastaut syndrome in children. The drug should be used only as second-line therapy.

用法用量

Suspension, Tablets Monotherapy, initial therapy. Adults over 14 years of age, initial: 1,200 mg/day in divided doses t.i.d.-q.i.d. The dose may be increased in 600-mg increments q 2 weeks to 2,400 mg/day based on clinical response and thereafter to 3,600 mg/day, if needed. Conversion to monotherapy. Adults: Initiate at 1,200 mg/day in divided doses t.i.d.-q.i.d. Reduce the dose of concomitant antiepileptic drugs by 1/3 at initiation of felbamate therapy. At week 2, the felbamate dose should be increased to 2,400 mg/day while reducing the dose of other antiepileptic drugs up to another 1/3 of the original dose. At week 3, increase the felbamate dose to 3,600 mg/day and continue to decrease the dose of other antiepileptic drugs as indicated by response. Adjunctive therapy. Adults: Add felbamate at a dose of 1,200 mg/day in divided doses t.i.d.-q.i.d. while reducing current antiepileptic drugs by 20%. Further decreases of concomitant antiepileptic drugs may be needed to minimize side effects due to drug interactions. The dose of felbamate can be increased by 1,200-mg/day increments at weekly intervals to 3,600 mg/day. Lennox-Gastaut syndrome in children, aged 2-14 years. As an adjunct, add felbamate at a dose of 15 mg/kg/day in divided doses t.i.d.-q.i.d. while decreasing present antiepileptic drugs by 20%. Further decreases in antiepileptic drug dosage may be needed to minimize side effects due to drug interactions. The dose of felbamate may be increased by 15-mg/kg/day increments at weekly intervals to 45 mg/kg/day.

不良反应

May differ depending on whether the drug is used as monotherapy or adjunctive therapy in adults or for Lennox-Gastaut syndrome in children. CNS: Insomnia, headache, anxiety, somnolence, dizziness, nervousness, tremor, abnormal gait, depression, paresthesia, ataxia, stupor, abnormal thinking, emotional lability, agitation, psychologic disturbance, aggressive reaction, hallucinations, euphoria, suicide attempt migraine. GI: Dyspepsia, vomiting, constipation, diarrhea, dry mouth, nausea, anorexia, abdominal pain, hiccoughs, esophagitis, increased appetite. Respiratory: Upper respiratory tract infection, rhinitis, sinusitis, pharyngitis, coughing. CV: Palpitation, tachycardia, SVT. Body as a whole: Fatigue, weight decrease or increase, facial edema, fever, chest pain, pain, asthenia, malaise, flu-like symptoms, anaphylaxis. Ophthalmologic: Miosis, diplopia, abnormal vision. GU: Urinary incontinence, intramenstrual bleeding, UTI. Hematologic: Aplastic anemia purpura, leukopenia, lymphadenopathy, leukocytosis, thrombocytopenia, granulocytopenia, positive antinuclear factor test, agranulocytosis qualitative platelet disorder. Dermatologic: Acne, rash, pruritus, urticaria, bullous eruption, buccal mucous membrane swelling, Stevens-Johnson syndrome. Miscellaneous: Otitis media, acute liver failure taste perversion, hypophosphatemia, myalgia, photosensitivity, substernal chest pain, dystonia, allergic reaction.

注意事项
	Pregnancy Category: C Contraindications: History of hepatic dysfunction or blood dyscrasia. Hypersensitivity to carbamates. Special Concerns: Aplastic anemia and acute liver failure have been observed in a few clients. Use with caution during lactation. Safety and efficacy have not been established in children other than those with Lennox-Gastaut syndrome.

药物相互作用

Carbamazepine / ↓ Carbamazepine steady-state levels and ↑ steady-state carbamazepine epoxide (metabolite) levels. Also, drug → 50% ↑ in felbamate clearance Methsuximide / ↑ Normethsuxide levels; decrease methsuximide dose Phenobarbital / ↑ Phenobarbital plasma levels and ↓ in felbamate levels Phenytoin / ↑ Phenytoin steady-state drug levels necessitating a 40% decrease in drug dose. Also, drug ↑ felbamate clearance Valproic acid / ↑ Steady-state valproic acid levels

FELBATOL (Felbamate)

 Epilepsy Medication

Felbamate is an antiepileptic drug used to treat seizures. Felbamate is effective in reducing the number and severity of partial, and secondarily generalized tonic/clonic seizures in adults and for children with seizures caused by the Lennox Gastaut syndrome. Felbamate can be taken as a single drug therapy.

What side effects can be caused by Felbamate?

Just like other drugs, felbamate can cause side effects. If you experience any side effects please report them to your doctor. (There is a risk of serious side effects, including death, with all medications that are used to treat seizures. However, this risk is exceedingly small.)

Common Side Effects

Decreased appetite resulting in weight loss
Insomnia (difficulty sleeping)
Nausea
Vomiting
Headache
Burping
Constipation
Abdominal pain
Change in taste
Nervousness
Depression or mood swings
Rare but Serious Side Effects

Skin rash
Unusual bleeding or bruising
Sore throat
Fever
Women who plan to have children should consult with their doctor about the possible effects on the fetus.

How should I take my medicine?

It is important that you take the total daily dose of felbamate. Felbamate is normally taken three times a day. A convenient dosing is breakfast, lunch, and dinner. If you have difficulty in falling asleep, contact your doctor to readjust the dosage of your felbamate. Do not stop this medication without the advice of your doctor. Doing so may result in an increase in seizures.

What should I do if I miss a dose?

Try to take the correct total dose each day. If you forget to take a dose early in the day, take it as soon as you remember, then spread the rest of your doses out throughout the rest of the day. If you wake up and realize you forgot the dose of felbamate the night before, continue your regular medication schedule that day and take your morning doses as soon as you remember. DO NOT make up the medicine from the day before. It is important that you not run out of medication. Always have at least one week's supply of medication on hand. You or your pharmacist may call your doctor's office in order to obtain refills.

Can I take Felbamate with food or other medications?

Yes, felbamate can be taken with meals. Felbamate interacts with many other medications. For example, if you are taking Dilantin, Tegretol, Depakene or Depakote (phenytoin, carbamazepine, valproic acid or divalproex sodium), felbamate will increase the blood levels of these medications. Felbamate may also increase the blood levels of many other medications including Coumadin. Prior to beginning any other medication, please contact your doctor.