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利他能methylphenidate

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利他能methylphenidate
药品名称:利他能methylphenidate
药品别名:
英 文 名:
药品价格:$ 美国市场售价 50.48 美元
研发公司:
适 用 症:用于过动儿症候群,发作性嗜睡症
型号规格:每粒含有效成份10mg/20mg/30mg/40mg/60mg几种规格,每瓶100粒装
药品详情:

【利他能methylphenidate 简述】
 
    利他能methylphenidate是一种大脑兴奋药。


利他能methylphenidate_香港济民药业

 
 
【利他能methylphenidate 适应症】
 
    本品用于过动儿症候群,发作性嗜睡症。
 
【利他能methylphenidate 规格】
 
    本品为胶囊装,每粒含有效成份10mg/20mg/30mg/40mg/60mg几种规格,每瓶100粒装。
 
【利他能methylphenidate 服用方法】
 
    本品以口服投予,最好在饭前30~45分前服药。每日2次,推荐剂量为儿童每日5mg,成年人每日10mg。
 
【利他能methylphenidate 注意事项】
 
    1.盐酸右哌醋甲酯缓释制剂可引起静止心率和血压的轻度升高,使用升压药物的患者慎用,高血压、心衰、近期发生心肌梗死及甲状腺功能亢进患者慎用。盐酸右哌醋甲酯生殖毒性分级为C,只有当可能的受益高于潜在的危险时方可用于孕妇。尚不知盐酸右哌醋甲酯是否经乳汁分泌,哺乳期妇女慎用。
 
    2.哌醋甲酯能降低有癫痫病史患者、无癫痫病史但有脑电图异常患者、无癫痫病史也无脑电图异常患者(罕见)的癫痫域,出现癫痫时应停用盐酸右哌醋甲酯。
 
    3.使用盐酸右哌醋甲酯缓释制剂的患者,特别是高血压患者应监测血压。
 
    4.长期治疗期间应定期检查血细胞记数、血小板记数。
 
    5.哌醋甲酯过量的急性中毒症状主要是由于中枢神经系统过度兴奋和拟交感作用过强,可引起呕吐、激动、震颤、反射亢进、肌肉抽搐、欣快、混乱、幻觉、精神错乱、出汗、脸红、头痛、高烧、心动过速、心悸、心律失常、高血压、瞳孔散大、黏膜干燥。可采用洗胃清除胃内残留药物,如果有精神激动和癫痫,洗胃前应首先控制症状并保护呼吸道。其他解毒方法包括给予活性炭和导泻。注意保持循环和呼吸畅通,高热患者可进行降温。
 
    6.15~30℃室温密闭保存。
 
【利他能methylphenidate 不良反应】
 
    1. 抽搐,食欲减退,失眠,心动过速。
 
    2.使用盐酸右哌醋甲酯缓释制剂的儿童病例中,发生率超过5%的不良反应包括:消化系统疾病(消化不良、食欲减退),神经系统疾病(头痛),精神疾病(焦虑)。
 
    3.在成年病例中,10.7%使用盐酸右哌醋甲酯缓释制剂的患者因药物不良反应而停药,主要有失眠、紧张不安、食欲减退、焦虑。
 
    4.使用盐酸右哌醋甲酯缓释制剂的成年病例中,发生率超过5%的不良反应包括:消化系统疾病(口干、消化不良),神经系统疾病(头痛),精神疾病(焦虑),呼吸系统疾病(咽喉痛)。
 
    5.盐酸右哌醋甲酯能加重精神病患者的行为紊乱及思维障碍。

Ritalin(methylphenidate)

 
Methylphenidate, sold under the trade names Ritalin among others, is a stimulant medication used to treat attention deficit hyperactivity disorder (ADHD) and narcolepsy.[1] It is a first line medication for ADHD.[1] It is taken by mouth or applied to the skin.[1] Different formulations have different durations of effect.[1]
 
Common side effects include trouble sleeping, anxiety, and weight loss.[1] More serious side effects may include psychosis, allergic reactions, prolonged erection, abuse, and heart problems.[1] Methylphenidate is believed to work by improving the action of catecholaminesin the brain.[4] It achieves this by blocking dopamine and norepinephrine reuptake by neurons.[5][4] Methylphenidate is a central nervous system (CNS) stimulant of the phenethylamine and piperidine classes.[6][1]
 
Methylphenidate was first made in 1944 and was approved for medical use in the United States in 1955.[1][7] It was originally sold by CIBA, now Novartis Corporation.[7] It is estimated that in 2013 2.4 billion doses of methylphenidate were taken worldwide.[8] About 80% of this was taken by people in the United States making it the 47th most prescribed medication in that country.[8][9] It is available as a generic medication.[1] In the United States the wholesale cost of the immediate release formulation is less than US$0.30 per dose as of 2018.[10]
 
Medical uses
 
Methylphenidate is most commonly used to treat ADHD and narcolepsy.[11]
Attention deficit hyperactivity disorder
Methylphenidate is used for the treatment of attention deficit hyperactivity disorder.[12] The addition of behavioural modification therapy can have additional benefits on treatment outcome.[13][14] The dosage may vary and are titrated to effect.[15]
The short-term benefits and cost effectiveness of methylphenidate are well established.[16][17]A number of reviews have established the safety and effectiveness of the stimulants for individuals with ADHD over several years.[18][19][19][20] A 2018 review found that it may cause both serious and non-serious adverse effects in children and adolescents.[21] The precise magnitude of improvements in ADHD symptoms and quality of life that are produced by methylphenidate treatment remains uncertain as of November 2015.[22]
 
Approximately 70% of those who use these stimulants see improvements in ADHD symptoms.[23][24] Children with ADHD who use stimulant medications generally have better relationships with peers and family members,[18][23] generally perform better in school, are less distractible and impulsive, and have longer attention spans.[18][23] People with ADHD have an increased risk of substance use disorders, and stimulant medications reduce this risk.[25][26] Some studies suggest that since ADHD diagnosis is increasing significantly around the world, using the drug may cause more harm than good in some populations using methylphenidrate as a "study drug".[27] This applies to people who potentially may be experiencing a different issue and are misdiagnosed with ADHD.[27] People in this category can then experience negative side-effects of the drug which worsen their condition, and make it harder for them to receive adequate care as providers around them may believe the drugs are sufficient and the problem lies with the user.[27] Methylphenidate is not approved for children under six years of age.[28][29]
Narcolepsy
Narcolepsy, a chronic sleep disorder characterized by overwhelming daytime drowsiness and uncontrollable sleep, is treated primarily with stimulants. Methylphenidate is considered effective in increasing wakefulness, vigilance, and performance.[30] Methylphenidate improves measures of somnolence on standardized tests, such as the Multiple Sleep Latency Test (MSLT), but performance does not improve to levels comparable to healthy controls.[31]
Other medical uses
Methylphenidate may also be prescribed for off-label use in treatment-resistant cases of bipolar disorder and major depressive disorder.[32] It can also improve depression in several groups including stroke, cancer, and HIV-positive patients.[33] However, the use of stimulants such as methylphenidate in cases of treatment-resistant depression is controversial.[34]
Stimulants may have fewer side-effects than tricyclic antidepressants in the elderly and medically ill.[35] In individuals with terminal cancer, methylphenidate can be used to counteract opioid-induced somnolence, to increase the analgesic effects of opioids, to treat depression, and to improve cognitive function.[36]
Enhancing performance
In 2015, review found that therapeutic doses of amphetamine and methylphenidate result in modest yet unambiguous improvements in cognition, including working memory, episodic memory, and inhibitory control, in normal healthy adults;[37][38] the cognition-enhancing effects of these drugs are known to occur through the indirect activation of both dopamine receptor D1 and adrenoceptor α2 in the prefrontal cortex.[37] Methylphenidate and other ADHD stimulants also improve task saliency and increase arousal.[39][40] Stimulants such as amphetamine and methylphenidate can improve performance on difficult and boring tasks[41][39][40] and are used by some students as a study and test-taking aid.[42][27] Based upon studies of self-reported illicit stimulant use, performance-enhancing use, rather than use as a recreational drug, is the primary reason that students use stimulants.[43]
 
Excessive doses of methylphenidate, above the therapeutic range, can interfere with working memory and cognitive control.[39][40] Like amphetamine and bupropion, methylphenidate increases stamina and endurance in humans primarily through reuptake inhibition of dopamine in the central nervous system.[44] Similar to the loss of cognitive enhancement when using large amounts, large doses of methylphenidate can induce side effects that impair athletic performance, such as rhabdomyolysis and hyperthermia.[45] While literature suggests it might improve cognition, most authors agree that using the drug recreationally as a study aid when ADHD diagnosis is not present does not actually improve GPA.[27]Moreover, it has been suggested that students who use the drug for studying may be self-medicating for potentially deeper underlying issues.[27]
 
Contraindications
 
Methylphenidate is contraindicated for individuals using monoamine oxidase inhibitors (e.g., phenelzine and tranylcypromine), or individuals with agitation, tics, or glaucoma, or a hypersensitivity to any ingredients contained in methylphenidate pharmaceuticals.[46]
 
The US FDA gives methylphenidate a pregnancy category of C, and women are advised to only use the drug if the benefits outweigh the potential risks.[47] Not enough animal and human studies have been conducted to conclusively demonstrate an effect of methylphenidate on fetal development. In 2007, empirical literature included 63 cases of prenatal exposure to methylphenidate across three empirical studies.[48]
 
Adverse effects
 
Methylphenidate is generally well tolerated.[50][51] The most commonly observed adverse effects with a frequency greater than placebo include appetite loss, dry mouth, anxiety/nervousness, nausea, and insomnia. Gastrointestinal adverse effects may include abdominal pain and weight loss. Nervous system adverse effects may include akathisia (agitation/restlessness), irritability, dyskinesia (tics), lethargy(drowsiness/fatigue), and dizziness. Cardiac adverse effects may include palpitations, changes in blood pressure and heart rate (typically mild), tachycardia (rapid resting heart rate), and Raynaud's phenomenon(reduced blood flow to the hands and feet).[52] Ophthalmologic adverse effects may include blurred vision and dry eyes, with less frequent reports of diplopia and mydriasis.[53] Other adverse effects may include depression, emotional lability, confusion, and bruxism. Hyperhidrosis (increased sweating) is common. Chest pain is rarely observed.[54]
 
There is some evidence of mild reductions in growth rate with prolonged treatment in children, but no causal relationship has been established and reductions do not appear to persist long-term.[55] Hypersensitivity(including skin rash, urticaria, and fever) is sometimes reported. The Daytrana patch has a much higher rate of dermal reactions than oral methylphenidate.[56]
 
Methylphenidate can worsen psychosis in psychotic patients, and in very rare cases it has been associated with the emergence of new psychotic symptoms.[57] It should be used with extreme caution in patients with bipolar disorder due to the potential induction of mania or hypomania.[58] There have been very rare reports of suicidal ideation, but evidence does not support a link.[55] Logorrhea is occasionally reported. Libido disorders, disorientation, and hallucinations are very rarely reported. Priapism is a very rare adverse event that can be potentially serious.[59]
 
USFDA-commissioned studies from 2011 indicate that in children, young adults, and adults there is no association between serious adverse cardiovascular events (sudden death, heart attack, and stroke) and the medical use of methylphenidate or other ADHD stimulants.[60]
 
Because some adverse effects may only emerge during chronic use of methylphenidate, a constant watch for adverse effects is recommended.[61]
 
Overdose
 
The symptoms of a moderate acute overdose on methylphenidate primarily arise from central nervous system overstimulation; these symptoms include: vomiting, agitation, tremors, hyperreflexia, muscle twitching, euphoria, confusion, hallucinations, delirium, hyperthermia, sweating, flushing, headache, tachycardia, heart palpitations, cardiac arrhythmias, hypertension, mydriasis, and dryness of mucous membranes.[45][62] A severe overdose may involve symptoms such as hyperpyrexia, sympathomimetic toxidrome, convulsions, paranoia, stereotypy (a repetitive movement disorder), rapid muscle breakdown, coma, and circulatory collapse.[45][62][63] A methylphenidate overdose is rarely fatal with appropriate care.[63] Severe toxic reactions involving abscess and necrosis have been reported following injection of methylphenidate tablets into an artery.[64]
 
Treatment of a methylphenidate overdose typically involves the application of benzodiazepines, with antipsychotics, α-adrenoceptor agonists, and propofol serving as second-line therapies.[63]
Addiction and dependence
Pharmacological texts describe methylphenidate as a stimulant with effects, addiction liability, and dependence liability similar to amphetamine, a compound with moderate liability among addictive drugs;[67][68] accordingly, addiction and psychological dependence are possible and likely when methylphenidate is used at high doses as a recreational drug.[68][69] When used above the medical dose range, stimulants are associated with the development of stimulant psychosis.[70] As with all addictive drugs, the overexpression of ΔFosB in D1-type medium spiny neurons in the nucleus accumbens is implicated in methylphenidate addiction.[69][71]
 
Methylphenidate has shown some benefits as a replacement therapy for individuals who are addicted to and dependent upon methamphetamine.[72] Methylphenidate and amphetamine have been investigated as a chemical replacement for the treatment of cocaine addiction[73][74][75][76] in the same way that methadone is used as a replacement drug for physical dependence upon heroin. Its effectiveness in treatment of cocaine or psychostimulant addiction or psychological dependence has not been proven and further research is needed.[77]
Biomolecular mechanisms
Methylphenidate has the potential to induce euphoria due to its pharmacodynamic effect (i.e., dopamine reuptake inhibition) in the brain's reward system.[71] At therapeutic doses, ADHD stimulants do not sufficiently activate the reward system, or the reward pathway in particular, to the extent necessary to cause persistent increases in ΔFosB gene expression in the D1-type medium spiny neurons of the nucleus accumbens;[68][71][78]consequently, when taken as directed in doses that are commonly prescribed for the treatment of ADHD, methylphenidate use lacks the capacity to cause an addiction.[68][71][78] However, when methylphenidate is used at sufficiently high recreational doses through a bioavailable route of administration (e.g., insufflation or intravenous administration), particularly for use of the drug as a euphoriant, ΔFosB accumulates in the nucleus accumbens.[68][71] Hence, like any other addictive drug, regular recreational use of methylphenidate at high doses eventually gives rise to ΔFosB overexpression in D1-type neurons which subsequently triggers a series of gene transcription-mediated signaling cascades that induce an addiction.[71][78][79]
 
 




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