英文药名: CABASER Tab(cabergoline)

中文药名: 卡麦角林片

生产厂家: 辉瑞公司
药品简介
通用名称：卡麦角林
药品英文名：Cabergoline
英文别名：Dostinex ,CABASER
药物剂型
片剂：0.25mg，1mg。
药理作用
本品为麦角衍生物。本品具有DA-受体激动作用，其特点是强力、长效并有选择性，与D2-受体有高度亲和力。作用与临床应用基本同溴隐亭。用于高催乳素血症。给予卡麦角林后，由于DA-受体受到刺激，可抑制泌乳素达2周。本品也有试用于乳腺癌。近年来，还用于治疗震颤麻痹。、一些神经学家将其用于早期治疗以延缓左旋多巴的应用，而另一些人则将本品留待左旋多巴不再有效或不能耐受时使用。本品与左旋多巴同用时，对改善“开关”现象中的“关”期有较好效果。据报道，每天给卡麦角林1次就可显著改善患者的日常生活能力和UPDRS运动检查评分，并减少DA的需量达18%，呈“开”状态的时间也明显增加。
药动学
本品口服后可被吸收，达峰时间为0.5～4h，消除t1/2约为6h。该药被广泛代谢成失活代谢物后，随尿和粪便排出。
适应证
1.用于治疗帕金森病。
2.用于高催乳素血症。
3.试用于乳腺癌。
禁忌证
1.参见溴隐亭。
2.哺乳者禁用。
 注意事项
1.参见溴隐亭。
2.有的患者不能耐受溴隐亭，却能耐受本品。
3.在停止本品治疗至少一个月后方可怀孕。
不良反应
1.参见溴隐亭。
2.文献报道1例使用本品后16个月发生胸膜肺病，另2例发生胸腔积液和肺纤维化。
用法用量
开始治疗时，每周0.25mg，以后每周增加0.5mg。直至每周4.5mg。
Brand name: Cabaser 1mg, 2mg and 4mg
Active ingredient (generic name): Caberguline
Manufacturer: Pfizer
Importer: Behestan Darou
Pharmacotherapeutic group: dopamine agonists
Pharmaceutical form: 1 mg, 2mg and 4mg Tablet
Pharmacodynamic: 
Cabaser is a dopaminergic ergoline derivative endowed with potent and long-lasting dopamine D2 receptor agonist properties.
The effect is prompt (within 3 hours of administration) and persistent (up to 7-28 days). The PRL-lowering effect is dose-related both in terms of degree of effect and duration of action.
Cabaser is used to treat the symptoms of Parkinson’s disease. The tablets contain the active ingredient Cabergoline which acts in a similar way to a chemical in the body called dopamine. Patients with Parkinson’s disease do not have enough of this chemical.
Pharmacokinetic:
The pharmacokinetic and metabolic profiles of Cabaser have been studied in healthy volunteers of both sexes, in female hyperprolactinemic patients and in parkinsonian patients. After oral administration of the labelled compound, radioactivity was rapidly absorbed from the gastrointestinal tract as the peak of radioactivity in plasma was between 0.5 and 4 hours. Ten days after administration about 18/20% and 55/72% of the radioactive dose (3H-cabergoline/14C-cabergoline) was recovered in urine and faeces, respectively.
The low urinary excretion of unchanged Cabaser has been confirmed also in studies with non-radioactive product. The elimination half-life of Cabaser, estimated from urinary excretion rates, is long (63-68 hours in healthy volunteers, 79-115 hours in hyperprolactinemic patients).
Food does not appear to affect absorption and disposition of Cabaser. Since the tolerability of dopaminergic agents is improved when administered with food, it is recommended that Cabaser be taken with meals.
Therapeutic indication:
If treatment with a dopamine agonist is being considered, cabergoline is indicated as second line therapy in patients who are intolerant or fail treatment with a non-ergot compound, as monotherapy, or as adjunctive treatment to levodopa plus dopa-decarboxylase inhibitor, in the management of the signs and symptoms of Parkinson's disease.
Dosage and administration:
As expected for dopamine agonists, dose response for both efficacy and side effects appears to be linked to individual sensitivity. Optimization of dose should be obtained through slow initial dose titration, from starting doses of 1 mg daily. The dosage of concurrent levodopa may be gradually decreased, while the dosage of Cabaser is increased, until the optimum balance is determined. In view of the long half-life of the compound, increments of the daily dose of 0.5-1 mg should be done at weekly (initial weeks) or bi-weekly intervals, up to optimal doses.
The recommended therapeutic dosage is 2 to 3 mg/day for patients with signs and symptoms of Parkinson's disease. Cabaser should be given as a single daily dose.
Use in children
The safety and efficacy of Cabaser have not been investigated in children as Parkinson's disease does not affect this population.
Adverse reaction:
The most common adverse events are gastrointestinal disorders, peripheral edema, Constipation, dyspepsia, gastritis, vomiting,dizziness, dyskinesia Confusion, and hallucinations.
Contraindication:
Hypersensitivity to Cabaser, any excipient of the product, or any ergot alkaloid.
History of pulmonary, pericardial and retroperitoneal fibrotic disorders.
For long-term treatment: Evidence of cardiac valvulopathy as determined by pre-treatment echocardiography.
Pharmacokinetic interactions
As with other ergot derivatives, Cabaser should be given with caution to patients with severe cardiovascular disease, Raynaud's syndrome, peptic ulcer or gastrointestinal bleeding, or with a history of serious, particularly psychotic, mental disorders.
Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
Pregnancy and lactation:
In a twelve year observational study on pregnancy outcomes following cabergoline therapy, information is available on 256 pregnancies. Seventeen of these 256 pregnancies (6.6%) eventuated in major congenital malformations or abortion. Information is available on 23/258 infants who had a total of 27 neonatal abnormalities, both major and minor. Musculoskeletal malformations were the most common neonatal abnormality (10), followed by cardio-pulmonary abnormalities (5). There is no information on perinatal disorders or long-term development of infants exposed to intra-uterine cabergoline. Based on recent published literature, the prevalence of major congenital malformations in the general population has been reported to be 6.9% or greater. Rates of congenital abnormality vary between different populations. It is not possible to accurately determine if there is an increased risk as no control group was included.
Storage temperature:  keep in room temperature (15-25 C) away from sunlight and moisture.
注：日本上市的完整处方资料附件：http://www.info.pmda.go.jp/go/pack/1169011F1028_4_06/
-----------------------------------------   
产地国家:日本
原产地英文商品名:
CABASER TABLETS 0.25MG/Tablets 10Tablets/box 
原产地英文药品名:
cabergoline
中文参考商品译名:
CABASER片 0.25毫克/片 10片/盒
中文参考药品译名:
卡麦角林
生产厂家中文参考译名:
辉瑞公司
生产厂家英文名:
Pfizer
-----------------------------------------   
产地国家:日本
原产地英文商品名:
CABASER TABLETS（カバサール錠）0.25MG/Tablets 100Tablets/box 
原产地英文药品名:
cabergoline
中文参考商品译名:
CABASER片（カバサール錠）0.25毫克/片 100片/盒
中文参考药品译名:
卡麦角林
生产厂家中文参考译名:
辉瑞公司
生产厂家英文名:
Pfizer
-----------------------------------------   
产地国家:日本
原产地英文商品名:
CABASER TABLETS（カバサール錠）1.00MG/Tablets 100Tablets/box 
原产地英文药品名:
cabergoline
中文参考商品译名:
CABASER片（カバサール錠）1.00毫克/片 100片/盒
中文参考药品译名:
卡麦角林
生产厂家中文参考译名:
辉瑞公司
生产厂家英文名:
Pfizer
-----------------------------------------   
产地国家:土耳其
原产地英文商品名:
Dostinex TABLETS  0.5MG/Tablets 8Tablets/box 
原产地英文药品名:
Cabergoline
中文参考商品译名:
Dostinex片 0.5毫克/片 8片/盒
中文参考药品译名:
卡麦角林
生产厂家中文参考译名:
PHARMACIA
生产厂家英文名:
PHARMACIA