卡比沙明是一种轻度镇静抗组胺药，数年来已被证明安全有效。2006年之前卡比沙明被广泛使用，已有100多个上市的含卡比沙明产品，包括缓释固体剂和复合药。但是，几乎所有这些老产品都没有通过FDA的严格审批程序。继2006年实施药效研究（DESI）审查后，FDA取消了所有基于卡比沙明的产品，除外两个已被审查的即释制剂，为有利于病人和医生的缓释制剂创造了机会。
美国儿科医生Laura Garabedian博士说，“我已经发现卡比沙明治疗儿童过敏症非常有效，但一般不作为一线治疗。因为现有的即释制剂必须每天多次给药，包括儿童在上学时给药一次，所以其依从性差。我期待着一个测试良好的12小时制剂。该新产品特性应向依从性的改善和更好结果进行转化。”
Tris总裁兼首席执行官Ketan Meht说：“这是基于Tris的OralXR+技术平台的第四份NDA提交，包括Nexiclon?XR，即最近推出的首个每24小时液体缓释混悬剂。Tris的流水线包括一些针对呼吸系统市场的产品，例如咳嗽、感冒、过敏治疗，并预定在未来两年提交申请。Tris计划在2012年推出卡比沙明缓释混悬剂，目前其方案正在评估，包括与其他专业制药公司的合作。”
药物名称：卡比沙明 　　
药物别名：氯苯吡醇胺，POLISTIN，ALLERGEFON，HISTEX 　 　
英文名称：Carbinoxamine 　　
说　明： 4mg。 　　
功用作用：
为乙醇类抗组胺药，
作用快，持续短。常配于复方中应用。 　　
用法用量：
口服：2～4mg/次，1日3～4次。 　　
注意事项：
（1）较多见的副作用为头晕、头痛、嗜睡、口干、恶心、倦乏，停药或减药后，即自行消失。
（2）有头晕、嗜睡等副作用，故驾驶员在工作时不宜使用。 　　
（3）偶可引起皮疹、粒细胞减少，长期应用（6个月以上），可引起贫血。
GASTROCROM  - cromolyn sodium solution, concentrate 
Azur Pharma, Inc.
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Gastrocrom®
(cromolyn sodium, USP)
Oral Concentrate
For Oral Use Only – Not for Inhalation or Injection.
DESCRIPTION
Each 5 mL ampule of GASTROCROM contains 100 mg cromolyn sodium, USP, in purified water. Cromolyn sodium is a hygroscopic, white powder having little odor. It may leave a slightly bitter aftertaste. GASTROCROM (cromolyn sodium, USP) Oral Concentrate is clear, colorless, and sterile. It is intended for oral use.
Chemically, cromolyn sodium is disodium 5,5’-[(2-hydroxytrimethylene)dioxy]bis[4-oxo-4H-1-benzopyran-2-carboxylate]. The empirical formula is C23H14Na2O11; the molecular weight is 512.34. Its chemical structure is:
Pharmacologic Category: Mast cell stabilizer
Therapeutic Category: Antiallergic
CLINICAL PHARMACOLOGY
In vitro and in vivo animal studies have shown that cromolyn sodium inhibits the release of mediators from sensitized mast cells. Cromolyn sodium acts by inhibiting the release of histamine and leukotrienes (SRS-A) from the mast cell.
Cromolyn sodium has no intrinsic vasoconstrictor, antihistamine, or glucocorticoid activity.
Cromolyn sodium is poorly absorbed from the gastrointestinal tract. No more than 1% of an administered dose is absorbed by humans after oral administration, the remainder being excreted in the feces. Very little absorption of cromolyn sodium was seen after oral administration of 500 mg by mouth to each of 12 volunteers. From 0.28 to 0.50% of the administered dose was recovered in the first 24 hours of urinary excretion in 3 subjects. The mean urinary excretion of an administered dose over 24 hours in the remaining 9 subjects was 0.45%.
CLINICAL STUDIES
Four randomized, controlled clinical trials were conducted with GASTROCROM in patients with either cutaneous or systemic mastocytosis; two of which utilized a placebo-controlled crossover design, one utilized an active-controlled (chlorpheniramine plus cimetidine) crossover design, and one utilized a placebo-controlled parallel group design. Due to the rare nature of this disease, only 36 patients qualified for study entry, of whom 32 were considered evaluable. Consequently, formal statistical analyses were not performed. Clinically significant improvement in gastrointestinal symptoms (diarrhea, abdominal pain) were seen in the majority of patients with some improvement also seen for cutaneous manifestations (urticaria, pruritus, flushing) and cognitive function. The benefit seen with GASTROCROM 200 mg QID was similar to chlorpheniramine (4 mg QID) plus cimetidine (300 mg QID) for both cutaneous and systemic symptoms of mastocytosis.
Clinical improvement occurred within 2-6 weeks of treatment initiation and persisted for 2-3 weeks after treatment withdrawal. GASTROCROM did not affect urinary histamine levels or peripheral eosinophilia, although neither of these variables appeared to correlate with disease severity. Positive clinical benefits were also reported for 37 of 51 patients who received GASTROCROM in United States and foreign humanitarian programs.
INDICATIONS AND USAGE
GASTROCROM is indicated in the management of patients with mastocytosis. Use of this product has been associated with improvement in diarrhea, flushing, headaches, vomiting, urticaria, abdominal pain, nausea, and itching in some patients.
CONTRAINDICATIONS
GASTROCROM is contraindicated in those patients who have shown hypersensitivity to cromolyn sodium.
WARNINGS
The recommended dosage should be decreased in patients with decreased renal or hepatic function. Severe anaphylactic reactions may occur rarely in association with cromolyn sodium administration.
PRECAUTIONS
In view of the biliary and renal routes of excretion of GASTROCROM, consideration should be given to decreasing the dosage of the drug in patients with impaired renal or hepatic function.
Carcinogenesis, Mutagenesis, and Impairment of Fertility
In carcinogenicity studies in mice, hamsters, and rats, cromolyn sodium had no neoplastic effects at intraperitoneal doses up to 150 mg/kg three days per week for 12 months in mice, at intraperitoneal doses up to 53 mg/kg three days per week for 15 weeks followed by 17.5 mg/kg three days per week for 37 weeks in hamsters, and at subcutaneous doses up to 75 mg/kg six days per week for 18 months in rats. These doses in mice, hamsters, and rats are less than the maximum recommended daily oral dose in adults and children on a mg/m2 basis.
Cromolyn sodium showed no mutagenic potential in Ames Salmonella/microsome plate assays, mitotic gene conversion in Saccharomyces cerevisiae and in an in vitro cytogenetic study in human peripheral lymphocytes.
In rats, cromolyn sodium showed no evidence of impaired fertility at subcutaneous doses up to 175 mg/kg in males (approximately equal to the maximum recommended daily oral dose in adults on a mg/m2 basis) and 100 mg/kg in females (less than the maximum recommended daily oral dose in adults on a mg/m2 basis).
Pregnancy
Pregnancy Category B
In reproductive studies in pregnant mice, rats, and rabbits, cromolyn sodium produced no evidence of fetal malformations at subcutaneous doses up to 540 mg/kg in mice (approximately equal to the maximum recommended daily oral dose in adults on a mg/m2 basis) and 164 mg/kg in rats (less than the maximum recommended daily oral dose in adults on a mg/m2 basis) or at intravenous doses up to 485 mg/kg in rabbits (approximately 4 times the maximum recommended daily oral dose in adults on a mg/m2 basis). There are, however, no adequate and well controlled studies in pregnant women.
Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.
Drug Interaction During Pregnancy
In pregnant mice, cromolyn sodium alone did not cause significant increases in resorptions or major malformations at subcutaneous doses up to 540 mg/kg (approximately equal to the maximum recommended daily oral dose in adults on a mg/m2 basis). Isoproterenol alone increased both resorptions and major malformations (primarily cleft palate) at a subcutaneous dose of 2.7 mg/kg (approximately 7 times the maximum recommended daily inhalation dose in adults on a mg/m2 basis). The incidence of major malformations increased further when cromolyn sodium at a subcutaneous dose of 540 mg/kg was added to isoproterenol at a subcutaneous dose of 2.7 mg/kg. No such interaction was observed in rats or rabbits.
Nursing Mothers
It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when GASTROCROM is administered to a nursing woman.
Pediatric Use
In adult rats no adverse effects of cromolyn sodium were observed at oral doses up to 6144 mg/kg (approximately 25 times the maximum recommended daily oral dose in adults on a mg/m2 basis). In neonatal rats, cromolyn sodium increased mortality at oral doses of 1000 mg/kg or greater (approximately 9 times the maximum recommended daily oral dose in infants on a mg/m2 basis) but not at doses of 300 mg/kg or less (approximately 3 times the maximum recommended daily oral dose in infants on a mg/m2 basis). Plasma and kidney concentrations of cromolyn after oral administration to neonatal rats were up to 20 times greater than those in older rats. In term infants up to six months of age, available clinical data suggest that the dose should not exceed 20 mg/kg/day. The use of this product in pediatric patients less than two years of age should be reserved for patients with severe disease in which the potential benefits clearly outweigh the risks.
Geriatric Use
Clinical studies of GASTROCROM did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
ADVERSE REACTIONS
Most of the adverse events reported in mastocytosis patients have been transient and could represent symptoms of the disease. The most frequently reported adverse events in mastocytosis patients who have received GASTROCROM during clinical studies were headache and diarrhea, each of which occurred in 4 of the 87 patients. Pruritus, nausea, and myalgia were each reported in 3 patients and abdominal pain, rash, and irritability in 2 patients each. One report of malaise was also recorded.
Other Adverse Events
Additional adverse events have been reported during studies in other clinical conditions and from worldwide postmarketing experience. In most cases the available information is incomplete and attribution to the drug cannot be determined. The majority of these reports involve the gastrointestinal system and include: diarrhea, nausea, abdominal pain, constipation, dyspepsia, flatulence, glossitis, stomatitis, vomiting, dysphagia, esophagospasm.
Other less commonly reported events (the majority representing only a single report) include the following:
Skin: pruritus, rash, urticaria/angioedema, erythema/ burning, photosensitivity
Musculoskeletal: arthralgia, myalgia, stiffness/weakness of legs
Neurologic: headache, dizziness, hypoesthesia, paresthesia, migraine, convulsions, flushing
Psychiatric: psychosis, anxiety, depression, hallucinations, behavior change, insomnia, nervousness
Heart Rate: tachycardia, premature ventricular contractions (PVCs), palpitations
Respiratory: pharyngitis, dyspnea
Miscellaneous: fatigue, edema, unpleasant taste, chest pain, postprandial lightheadedness and lethargy, dysuria, urinary frequency, purpura, hepatic function test abnormal, polycythemia, neutropenia, pancytopenia, tinnitus, lupus erythematosus (LE) syndrome
DOSAGE AND ADMINISTRATION
NOT FOR INHALATION OR INJECTION. SEE DIRECTIONS FOR USE.
The usual starting dose is as follows:
Adults and Adolescents (13 Years and Older)
Two ampules four times daily, taken one-half hour before meals and at bedtime.
Children 2-12 Years
One ampule four times daily, taken one-half hour before meals and at bedtime.
Pediatric Patients Under 2 Years
Not recommended.
If satisfactory control of symptoms is not achieved within two to three weeks, the dosage may be increased but should not exceed 40 mg/kg/day.
Patients should be advised that the effect of GASTROCROM therapy is dependent upon its administration at regular intervals, as directed.
Maintenance Dose
Once a therapeutic response has been achieved, the dose may be reduced to the minimum required to maintain the patient with a lower degree of symptomatology. To prevent relapses, the dosage should be maintained.
Administration
GASTROCROM should be administered as a solution at least 1/2 hour before meals and at bedtime after preparation according to the following directions:
Break open ampule(s) and squeeze liquid contents of ampule(s) into a glass of water.
Stir solution.
Drink all of the liquid.
HOW SUPPLIED
GASTROCROM Oral Concentrate is an unpreserved, colorless solution supplied in a low density polyethylene plastic unit dose ampule with 8 ampules per foil pouch. Each 5 mL ampule contains 100 mg cromolyn sodium, USP, in purified water.
NDC 18860-678-70     96 ampules x 5 mL
GASTROCROM Oral Concentrate should be stored between 15°-30°C (59°-86°F) and protected from light. Do not use if it contains a precipitate or becomes discolored. Keep out of the reach of children.

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产地国家: 美国
原产地英文商品名:
GASTROCROM 100 MG/5 ML CONCENTRATION 96 X 5MLS PER BOX
原产地英文药品名:
CROMOLYN SODIUM
中文参考商品译名:
卡比沙明口服缓释混悬剂 100毫克／5毫升 96X5毫升／盒
中文参考药品译名:
氯苯吡醇胺
生产厂家中文参考译名:
MEDA PHARMS
生产厂家英文名:
MEDA PHARMS