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苯巴比妥Phenobarbital

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苯巴比妥Phenobarbital
药品名称:苯巴比妥Phenobarbital
药品别名:
英 文 名:
药品价格:$ 美国市场售价 9.82 美元
研发公司:
适 用 症:镇静,催眠,抗惊厥,抗癫痫
型号规格:每片含有效成份15mg/30mg/60mg/100mg,每瓶100片装
药品详情:

【苯巴比妥Phenobarbital 简述】
 
    苯巴比妥Phenobarbital为一类精神科药品。

苯巴比妥Phenobarbital_香港济民药业


 
 
【苯巴比妥Phenobarbital 适应症】
 
    用于:①镇静:如焦虑不安、烦躁、甲状腺功能亢进、高血压、功能性恶心、小儿幽门痉挛等症;
 
    ②催眠:偶用于顽固性失眠症,但醒后往往有疲倦、嗜睡等后遗效应;
 
    ③抗惊厥:常用其对抗中枢兴奋药中毒或高热、破伤风、脑炎、脑出血等病引起的惊厥;
 
    ④抗癫痫:用于癫痫大发作和部分性发作的治疗,出现作用快,也可用于癫痫持续状态;
 
    ⑤麻醉前给药;
 
    ⑥与解热镇痛药配伍应用,以增强其作用;
 
    ⑦治疗新生儿高胆红素血症。
 
【苯巴比妥Phenobarbital 规格】
 
    本品为片剂,每片含有效成份15mg/30mg/60mg/100mg,每瓶100片装。
 
【苯巴比妥Phenobarbital 服用方法】
 
    由于剂型及规格不同,用法用量请仔细阅读药品说明书或遵医嘱。
 
【苯巴比妥Phenobarbital 注意事项】
 
    (1)长期用于治疗癫痫时不可突然停药,以免引起癫痫发作,甚至出现癫痫持续状态。
 
    (2) 一般应用5~10倍催眠量时可引起中度中毒,10~15倍则重度中毒,血药浓度高于8~10mg/100ml时,有生命危险。急性中毒症状为昏睡,进而呼吸浅表,通气量大减,最后呼吸衰竭而死亡。
 
    (3)慎用于严重贫血、心脏病、糖尿病、高血压、甲状腺功能亢进、老年人、妊娠期妇女和哺乳期妇女。
 
    (4)静脉注射速度不应超过每分钟60mg,过快可引起呼吸抑制。
 
    (5)妊娠期服用本品,新生儿可发生低凝血酶原血症和出血。维生素K有治疗或预防作用。
 
    (6)本品或其他巴比妥类药物中毒的急救:口服本品未超过3小时者,可用大量温生理盐水或1: 2000的高锰酸 钾溶液洗胃(注意防止液体流入气管内,以免引起吸入性肺炎)。洗毕,再以10~15g硫酸钠(忌用硫酸镁)导泻。并给碳酸氢钠或乳酸钠碱化尿液,减少在肾小管中的重吸收,加速 药物排泄。亦可用甘露醇等利尿剂增加尿量,促进药物排出。又因呼吸抑制所致的呼吸性酸中毒时,可促进药物进入中枢,加重中毒反应,因此保证呼吸道通畅尤为重要,必要时行气管切开或气管插管,吸氧或人工呼吸。亦可适当给予中, 枢兴奋药。血压偏低时,可静脉滴注葡萄糖盐水或低分子右旋糖酐。
 
【苯巴比妥Phenobarbital 不良反应】
 
    (1)用药后可出现头晕、困倦等后遗效应,久用可产生耐受性及依赖性。多次连用应警惕蓄积中毒。
 
    (2)少数患者可出现皮疹、药热、剥脱性皮炎等过敏反应。

Phenobarbital

 
Phenobarbital, also known as phenobarbitone or phenobarb, is a medication recommended by the World Health Organization for the treatment of certain types of epilepsy in developing countries.[4] In the developed world, it is commonly used to treat seizures in young children,[5]while other medications are generally used in older children and adults.[6] It may be used intravenously, injected into a muscle, or taken by mouth.[2] The injectable form may be used to treat status epilepticus.[2] Phenobarbital is occasionally used to treat trouble sleeping, anxiety, and drug withdrawal and to help with surgery.[2] It usually begins working within five minutes when used intravenously and half an hour when administered orally.[2] Its effects last for between four hours and two days.[2][3]
 
Side effects include a decreased level of consciousness along with a decreased effort to breathe.[2] There is concern about both abuse and withdrawal following long-term use.[2] It may also increase the risk of suicide.[2] It is pregnancy category B or D (depending on how it is taken) in the United States and category D in Australia, meaning that it may cause harm when taken by pregnant women.[2][7] If used during breastfeeding it may result in drowsiness in the baby.[8] A lower dose is recommended in those with poor liver or kidney function, as well as elderly people.[2] Phenobarbital is a barbiturate that works by increasing the activity of the inhibitory neurotransmitter GABA.[2]
 
Phenobarbital was discovered in 1912 and is the oldest still commonly used anti-seizure medication.[9][10] It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.[11] It is the least expensive anti-seizure medication at around US$5 a year in the developing world.[12] Access, however, may be difficult as some countries label it as a controlled drug.[12]
 
Medical uses
 
Phenobarbital is used in the treatment of all types of seizures, except absence seizures.[13][14] It is no less effective at seizure control than phenytoin, however phenobarbital is not as well tolerated.[15] Phenobarbital may provide a clinical advantage over carbamazepine for treating partial onset seizures. Carbamazepine may provide a clinical advantage over phenobarbital for generalized onset tonic-clonic seizures.[16] Its very long active half-life (53–118 hours) means for some people doses do not have to be taken every day, particularly once the dose has been stabilized over a period of several weeks or months, and seizures are effectively controlled.[citation needed]
The first-line drugs for treatment of status epilepticus are benzodiazepines, such as lorazepam or diazepam. If these fail, then phenytoin may be used, with phenobarbital being an alternative in the US, but used only third-line in the UK.[17] Failing that, the only treatment is anaesthesia in intensive care.[14][18] The World Health Organization (WHO) gives phenobarbital a first-line recommendation in the developing world and it is commonly used there.[4][19]
 
Phenobarbital is the first-line choice for the treatment of neonatal seizures.[20][21][22]Concerns that neonatal seizures in themselves could be harmful make most physicians treat them aggressively. No reliable evidence, though, supports this approach.[23]
 
Phenobarbital is sometimes used for alcohol detoxification and benzodiazepine detoxification for its sedative and anti-convulsant properties. The benzodiazepines chlordiazepoxide (Librium) and oxazepam (Serax) have largely replaced phenobarbital for detoxification.[24]
 
While phenobarbital has been used for insomnia, such use is not recommended due to the risk of addiction and other side affects.[25]
Other uses
Phenobarbital properties can effectively reduce tremors and seizures associated with abrupt withdrawal from benzodiazepines.
 
Phenobarbital is a cytochrome P450 inducer, and is used to reduce the toxicity of some drugs.
 
Phenobarbital is occasionally prescribed in low doses to aid in the conjugation of bilirubin in people with Crigler-Najjar syndrome (Type II),[26] or in patients with Gilbert syndrome.[citation needed]
Phenobarbital can also be used to relieve cyclic vomiting syndrome symptoms.
 
Phenobarbital is a commonly used agent in high purity and dosage for lethal injection of "death row" criminals.
 
In infants suspected of neonatal biliary atresia, phenobarbital is used in preparation for a 99mTc-IDA hepatobiliary (HIDA; hepatobiliary 99mTc-iminodiacetic acid) study that differentiates atresia from hepatitis or cholestasis.
 
Phenobarbital is used as a secondary agent to treat newborns with neonatal abstinence syndrome, a condition of withdrawal symptoms from exposure to opioid drugs in utero.
 
In massive doses, phenobarbital is prescribed to terminally ill patients to allow them to end their life through physician-assisted suicide.[27]
 
Like other barbiturates, phenobarbital can be used recreationally,[28] but this is reported to be relatively infrequent.[29]
 
Contraindications
 
Acute intermittent porphyria, hypersensitivity to any barbiturate, prior dependence on barbiturates, severe respiratory insufficiency (as with chronic obstructive pulmonary disease), severe liver failure, pregnancy, and breastfeeding are contraindications for phenobarbital use.[30]
 
Overdose
 
Phenobarbital causes a depression of the body's systems, mainly the central and peripheral nervous systems. Thus, the main characteristic of phenobarbital overdose is a "slowing" of bodily functions, including decreased consciousness (even coma), bradycardia, bradypnea, hypothermia, and hypotension (in massive overdoses). Overdose may also lead to pulmonary edema and acute renal failure as a result of shock, and can result in death.
 
The electroencephalogram (EEG) of a person with phenobarbital overdose may show a marked decrease in electrical activity, to the point of mimicking brain death. This is due to profound depression of the central nervous system, and is usually reversible.[33]
 
Treatment of phenobarbital overdose is supportive, and mainly consists of the maintenance of airway patency (through endotracheal intubationand mechanical ventilation), correction of bradycardia and hypotension (with intravenous fluids and vasopressors, if necessary), and removal of as much drug as possible from the body. Depending on how much time has elapsed since ingestion of the drug, this may be accomplished through gastric lavage (stomach pumping) or use of activated charcoal. Hemodialysis is effective in removing phenobarbital from the body, and may reduce its half-life by up to 90%.[33] No specific antidote for barbiturate poisoning is available.[34]
 
British veterinarian Donald Sinclair, better known as the character Siegfried Farnon in the "All Creatures Great and Small" book series by James Herriot, committed suicide at the age of 84 by injecting himself with an overdose of phenobarbital. Activist Abbie Hoffman also committed suicide by consuming phenobarbital, combined with alcohol, on April 12, 1989; the residue of around 150 pills was found in his body at autopsy.[35] Also dying from an overdose in 1996 was actress/model Margaux Hemingway. The Japanese officers aboard the German submarine U-234 killed themselves with phenobarbital while the German crew members were on their way to the US to surrender (but before Japan had surrendered).
 
Thirty-nine members of the Heaven's Gate UFO religious group committed mass suicide in March 1997 by drinking a lethal dose of phenobarbital and vodka "and then lay down to die" hoping to enter an alien spacecraft.[36]
 
Mechanism of action
 
Through its action on GABAA receptors, phenobarbital increases the flow of chloride ions into the neuron which decreases the excitability of the post-synaptic neuron. Hyperpolarizing this post-synaptic membrane leads to a decrease in the general excitatory aspects of the post-synaptic neuron. By making it harder to depolarize the neuron, the threshold for the action potential of the post-synaptic neuron will be increased. Phenobarbital stimulates GABA to accomplish this hyperpolarization.[37] Direct blockade of excitatory glutamate signaling is also believed to contribute to the hypnotic/anticonvulsant effect that is observed with the barbiturates.[38]
 
 




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