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奥沙米特(Oxatimide, Tinest/PEPECIN DRY SYRUP 2％)

2012-10-23 23:42:20 作者：新特药房来源：中国新特药网天津分站浏览次数：378 文字大小：【大】【中】【小】

简介： 【中文品名】奥沙米特【药效类别】抗组胺药，平喘药【通用药名】OXATOMIDE【别　　名】Oxatimide, Tinest, Celtech, Dasten, Finsedy, MCN-JR-35443, R5443【化学名称】 2H-Benzimidazol-2-one, 1-[3- ...

关键字：奥沙米特(Oxatimide Tinest/PEPECIN DRY SYRUP 2％)

【中文品名】奥沙米特
【药效类别】抗组胺药，平喘药
【通用药名】OXATOMIDE
【别　　名】Oxatimide, Tinest, Celtech, Dasten, Finsedy, MCN-JR-35443, R5443
【化学名称】 2H-Benzimidazol-2-one, 1-[3-[4-(diphenylmethyl)-1-piperazinyl] propyl]-1,3-dihydro-
【CA登记号】[60607-34-3]
【结构式】

【分子式】C27H30N4O
【分子量】426.553
【收录药典】JP14
【开发单位】Janssen (比利时)
【首次上市】1981年，德国
【性　　状】白色粉末，溶于三氯甲烷、苯，不溶于水。mp153.6℃。
【用　　途】抗组胺药。用于治疗变应性鼻炎，荨麻疹，皮肤瘙痒症、湿疹、皮炎、痒疹，结膜炎和食物过敏以及滤泡性结膜炎等。

【药理作用】

本品为哌嗪的衍生物，能选择性的阻断H1受体，除具有较强的抗组胺作用外，还可拮抗血小板激活因子和白三烯，还具有炎性细胞稳定作用，可抑制肥大细胞、嗜酸细胞和巨噬细胞等炎性细胞释放炎性介质和细胞因子等。此外，还具有一定的抗毒蕈碱、胆碱作用。

【药动学】

口服后tmax为4h，与血浆蛋白结合率高达91%，其半衰期约20h，主要经肝脏代谢，代谢产物自尿中排泄。本品大剂量可为胎盘吸收。

【适应证】

常用于荨麻疹、变应性鼻炎(过敏性鼻炎)或结膜炎和食物过敏，还可多途径阻断气道变应性炎症的过程，用于防治过敏性哮喘，尤其是儿童哮喘的防治效果更好。

【禁忌证】

对本品过敏者禁用，本品有嗜睡作用，驾驶车辆人员禁用。

【注意事项】

妊娠期和哺乳妇女慎用。

【不良反应】

常见嗜睡。少数有体重增加、头痛、恶心、胃肠不适、皮疹和口干等。

【用法用量】

口服：1.每次30～60mg，每天2次；2.5～14岁儿童，每次15～30mg，每天2次；3.5岁以下儿童可口服2%干糖浆：每次0.5mg/kg，每天2次。

【药物相应作用】

(尚不明确)与中枢镇静药合用可加强本药嗜睡作用。

专家点评

本品主要用来治疗过敏性鼻炎和过敏性结膜炎。在治疗哮喘方面主要用来预防儿童哮喘急性发作，疗效一般，对荨麻疹也有明显的治疗作用。
THERAPEUTIC INDICATIONS:
· Antihistamine.
· TINSET * is indicated for the prevention and treatment of allergic reactions, particularly rhinitis, extrinsic asthma, chronic urticaria, follicular conjunctivitis, food allergy and atopic dermatitis.
· If desired, other medications may be administered in combination with TINSET *, provided that its mechanism of action differs from that of TINSET *.
· TINSET * is not appropriate to stop allergic reactions such as acute asthmatic attack.
· TINSET * is indicated for skin allergies in general and in particular pruritus. Any kind of itching caused by viral rashes, chicken pox, measles, insect bites, senile pruritus, atopic dermatitis, stasis and biliary carcinomas.
IN HUMAN CLINICAL PHARMACOLOGY:
Pharmacodynamics: The oxatomide inhibits allergic hypersensitivity and decreased release and effects of different mediators. It is known to block or mitigate the effects mediated by histamine receptors (H1), serotonin (5-HT1), leukotrienes (LTC3, LTC4) and platelet aggregation factor (PAF).
The onset and intensity of the allergic reaction is slower as a result of the decrease in mediator release. Mast cells, which produce and store allergic mediators, being secreted by calcium mobilization. This process is inhibited by oxatomide.
At clinical doses no pharmacological effects of oxatomide to cause other anti-allergic effects.
Pharmacokinetics is virtually complete absorption of oxatomide by the gastrointestinal tract in humans.
The peak plasma concentration is reached within 2 hours post oral administration. Oxatomide is metabolized by the liver by aromatic hydroxylation, oxidative N-dealkylation and conjugation. Less than 0.5% of the dose is excreted unchanged. The stool is the main route of elimination of metabolites (60%), especially in bile and also via the urine. Oxatomide, which has a half life of 14 hours, reaching stable levels in plasma after 3 days (about 35 ng / ml with a dose of 30 mg twice daily). Protein binding is 98%.
Contraindications
Hypersensitivity to the active or formula components.
PRECAUTIONS:
Caution is recommended in children under 6 years by the phenomenon of overdose risk due to increased distribution in the CNS.
TINSET * not suitable for the rapid relief of allergic conditions like asthma attack.
When prescribing TINSET * patients with asthma, the existing treatment regimen should not be discontinued abruptly, but the dose should be decreased gradually. This is particularly important in patients treated with corticosteroids.
Due to its hepatic clearance, TINSET * should be administered with caution in patients with liver disorders. If necessary, treatment in these patients should preferably be started with half the normal dose, dosing intervals should be maintained.
Effects on ability to drive or operate machinery: Patients who drive or operate machinery should be warned of the possibility of drowsiness and impair alertness. The simultaneous intake of alcohol may potentiate these effects.
Use in Pregnancy and Lactation
Data in animal experiments suggest a limited step oxatomide through the placenta, but in pregnant women TINSET safety * has not been established. When necessary to administer during pregnancy TINSET * potential risks should be carefully weighed against the anticipated therapeutic benefit.
Oxatomide is excreted in the milk of lactating bitches. The concentration in milk is low and probably has no clinical relevance. It is not known if TINSET * is excreted in human milk. Therefore, you should exercise caution when TINSET * is administered to women who are breastfeeding.
ADVERSE REACTIONS:
Allergic reactions may occur such as rash, urticaria, angioedema and rarely anaphylaxis. At recommended doses are drowsiness and fatigue rare and usually transient in nature. If necessary, the dose may be reduced temporarily.
Can occur occasionally nausea, vomiting, abdominal discomfort, dizziness, muscle weakness and dry mouth. At high doses has been an increase in appetite.
In post-marketing experience has reported rare cases spontaneously TINSET * including seizures, elevated transaminases and hepatitis.
It has been observed exceptionally in infants and young children dyskinetic neurological reactions. These symptoms have disappeared completely and spontaneously within 24 hours after stopping treatment.
DRUG INTERACTIONS AND OTHER GENDER:
Patients should be cautioned that TINSET * may increase the sedative effects of CNS depressants including alcohol, barbiturates, hypnotics, narcotic analgesics, sedatives and tranquilizers.
CHANGES IN RESULTS OF LABORATORY TESTS:
Transaminase elevations.
PRECAUTIONS IN RELATION TO EFFECTS OF Carcinogenesis, Mutagenesis, Impairment of Fertility:
In animals have not noticed any direct embryotoxic effect or a direct toxic effect of peri-or postnatal. There is also no direct adverse effect on fertility and side effects were found only maternal toxic doses.
DOSAGE AND ADMINISTRATION:
TINSET * must be taken twice daily after breakfast and dinner.
Adults: Take one tablet every 12 hours.
Tablets:
· Between 15 to 35 kg (4 to 10 years): 15 mg (½ tablet) twice daily.
· Weight greater than 35 kg: 30 mg (1 tablet), twice daily.
The doses above may be doubled if there is insufficient improvement within a week.
REPRESENTATIONS AND MANAGEMENT Overdosage:
Symptoms: The symptoms most commonly reported after an overdose include drowsiness, stupor, and extrapyramidal symptoms such as dyskinesia, torticollis, oculogíria, dystonia and hypertonia. Less common are hyperexcitability and restlessness. Less frequently reported were dilated pupils, tachycardia and bradycardia, and generalized muscle spasms.
Treatment: No specific antidote is available. Treatment involves careful observation of vital signs and supportive measures. Within the first hour after ingestion, gastric lavage can be performed. If appropriate, may be given activated charcoal. Extrapyramidal symptoms have been successfully treated with anticholinergic agents.

Name of medicine: Tinset
Comparable patent medicine: Tinset
Active ingredient: Oxatomide
Presentation: Tablets
Concentration: 30mg
Extended-release tablets: No
Lab: Janssen-Cilag, SA de CV
Box of 20 pills
Made in: Mexico