马来酸卡比沙明（氯苯吡醇胺）    英文名称： Carbinoxamine Maleate(Clistin,Histex,Lergefin,Polistin) 性状： 白色无臭晶体，溶于水(1:1)、乙醇(1:1.5)、氯仿(1:1.5)，微溶于乙醚(1:8300)。1％的水溶液pH为4.6-5.1，避光密闭保存。具有抗组胺、抗胆碱、中枢镇静作用，常用于缓解过敏反应症状、感冒和咳嗽。口服4-8mg/次，3-4次/d；儿童：1-3岁2mg/次，3-6岁2-4mg/次，大龄儿童4mg/次，3-4次/d。可加入止咳糖浆的制剂中应用。 片剂：4mg。 作用与作用机制： 丙胺类包括溴苯那敏，二甲茚定，非尼拉敏，曲普利啶，具有强H1受体拮抗剂，具镇静作用。乙醇胺类包括曲美苄胺，卡比沙明，多西拉敏，具有显著的镇静作用与抗胆碱作用，胃肠道副作用较低。乙二胺类包括美吡拉敏，氯吡啉，安他唑林，希司洛啶，具有中度镇静活性，可致肠紊乱和光敏反应。酚噻嗪类包括帕拉塞嗪、异丙嗪、丙酰马嗪、美喹他嗪，具有显著的抗胆碱作用与止吐作用，可致镇静和光过敏反应。哌嗪类包括西替利嗪、布克利嗪、美克洛嗪，具有止吐作用。其他还有阿斯咪唑、阿扎他啶、特非那啶、阿伐司丁、巴米品、氯雷他定，是高选择性H1受体拮抗剂。NULL 药动学： 注意事项： 抗组胺药是一类能对抗组胺引起的各种病理反应的药物。本类药物可逆性占领组胺受体，竞争性阻断组胺与受体结合，从而表现抗组胺作用。组胺受体有H1和H2两种类型，激动时产生不同的效应。H1受体激动时可引起支气管及胃肠道平滑肌收缩，血管平滑肌舒张，心房肌收缩加强，房室传导减慢等。H2受体激动时可引起胃壁细胞分泌胃酸增加等。这两类效应各被不同的药物所拮抗。H1受体拮抗剂取代了机体中的组胺，竞争性拮抗其作用，它不能灭活组胺，也不抑制其合成与释放。故主要用于缓解过敏反应的症状，如荨麻疹、血管神经性水肿、鼻炎、结膜炎，也可缓解皮肤病所致瘙痒；一些传统的H1受体拮抗剂可拮抗乙酰胆碱、5-HT、肾上腺素，并具有局麻作用；H1受体拮抗剂如苯海拉明、茶苯海明、异丙嗪等因具镇吐作用，可用于治疗梅尼埃病及相关疾病的恶心、呕吐、腹泻症状。一些药物还具有抗眩晕作用及镇静作用，异丙嗪因具镇静作用可用于术前麻醉及短期治疗失眠。H1受体拮抗剂可加强乙醇、巴比妥、催眠药、止痛药、抗焦虑药、安定药等中枢抑制药的作用。单胺氧化酶抑制剂可增强其抗胆碱作用。该药还可协同阿托品、三环类抗抑郁药的作用。可掩蔽氨基糖苷类等的耳毒性，使皮试呈假阳性而提前停药。在使用抗组胺药前，应充分了解其配伍禁忌。NULL 临床应用： 本类药物不良反应主要有中枢神经系统抑制，表现为乏力、头昏、困倦，嗜睡等。本药还有锥体外系反应、胃肠道功能紊乱及光敏性皮炎、血相紊乱等反应。注意事项：本药忌用于早产儿和新生儿。这个年龄段的婴儿对其抗胆碱作用敏感，年纪稍大的儿童对其抗胆碱作用、镇静、低血压也十分敏感。抗组胺药因其嗜睡副作用，用药后病人不宜驾驶车辆、操纵机器，也不宜饮酒。因其阿托品样作用，伴发闭角型青光眼、尿潴留、前列腺肥大、幽门十二指肠梗阻的患者，慎用H1受体拮抗剂。癫痫、严重心血管或重度肝脏疾病使用吩噻嗪类药的患者的哮喘患者，在服用抗组胺药时，应注意其他副作用。孕期服用，可能致婴儿畸形，但缺乏充分证据。NULL 适应症 常用于缓解过敏反应症状、感冒和咳嗽。 药理作用 具有抗组胺、抗胆碱、中枢镇静作用。 用法用量 口服4～8mg/次，3～4次/d ；儿童：1～3岁2mg/次，3～6岁2～4mg/次，大龄儿童4mg/次，3～4次/d。可加入止咳糖浆的制剂中应用。 规格 片剂：4mg。 DESCRIPTION Carbinoxamine maleate is a histamine-H1 receptor blocking agent. Each tablet contains 4 mg carbinoxamine maleate and the following inactive ingredients: anhydrous lactose, magnesium stearate, microcrystalline cellulose, and sodium starch glycolate. Each 5 mL (teaspoonful) of oral solution contains 4 mg carbinoxamine maleate and the following inactive ingredients: artificial bubble gum flavor, citric acid (anhydrous), glycerin, methylparaben, propylene glycol, propylparaben, purified water, sodium citrate (hydrous) and sorbitol solution. Carbinoxamine maleate is freely soluble in water. Its structure is: 2-[(4-chlorophenyl)-2-pyridinylmethoxy]-N, N-dimethylethanamine (Z)-2-butenedioate (1:1) C16H19CIN2O• C4H4O4                                                                    MW = 406.86 CLINICAL PHARMACOLOGY Carbinoxamine maleate is an antihistamine with anticholinergic (drying) and sedative properties. Antihistamines appear to compete with histamine for receptor sites on effector cells. The pharmacological effects of carbinoxamine maleate after oral absorption have been shown to last approximately 4 hours. Interactions of carbinoxamine maleate with food or with other drugs and the possibility of cardiac conduction effects on the QT interval have not been studied. INDICATIONS AND USAGE Carbinoxamine maleate is effective for the symptomatic treatment of: Seasonal and perennial allergic rhinitis. Vasomotor rhinitis. Allergic conjunctivitis due to inhalant allergens and foods. Mild, uncomplicated allergic skin manifestations of urticaria and angioedema. Dermatographism. As therapy for anaphylactic reactions adjunctive to epinephrine and other standard measures after the acute manifestations have been controlled. Amelioration of the severity of allergic reactions to blood or plasma. CONTRAINDICATIONS Carbinoxamine maleate is contraindicated in children younger than 2 years of age. Carbinoxamine maleate is contraindicated in nursing mothers. Carbinoxamine maleate is contraindicated in patients who are hypersensitive to the drug or on monoamine oxidase inhibitor therapy. (See Drug Interactions section.) WARNINGS Deaths have been reported in children less than 2 years of age who were taking antihistamines, including carbinoxamine-containing drug products, therefore, carbinoxamine maleate is contraindicated in children younger than 2 years of age (see CONTRAINDICATIONS). Antihistamines should be used with considerable caution in patients with: narrow angle glaucoma, stenosing peptic ulcer, symptomatic prostatic hypertrophy, bladder neck obstruction, pyloroduodenal obstruction. PRECAUTIONS As many other antihistamines, carbinoxamine maleate has an atropine-like action and, therefore, should be used with caution in patients with: increased intraocular pressure, hyperthyroidism, cardiovascular disease, hypertension. Antihistamines such as carbinoxamine maleate should not be used to treat lower respiratory tract symptoms, including asthma. Carbinoxamine maleate may diminish mental alertness in children. In the young child, particularly, they may produce excitation. Carbinoxamine maleate is more likely to cause dizziness, sedation, and hypotension in elderly patients (approximately 60 years or older). Information for Patients Carbinoxamine maleate may cause drowsiness; alcohol, sedatives, and tranquilizers may increase the drowsiness effect. Avoid alcoholic beverages while taking this product. Do not take this product if you are taking sedatives or tranquilizers, without first consulting your doctor. Use caution when driving a motor vehicle or operating machinery. Drug Interactions Monoamine oxidase inhibitors prolong and intensify the anticholinergic (drying) effects of antihistamines. Carbinoxamine maleate has additive effects with alcohol and other CNS depressants (hypnotics sedatives, tranquilizers, etc.). Carcinogenesis, Mutagenesis, Impairment of Fertility No long-term studies in animals have been performed to determine the possible effects of carbinoxamine maleate on carcinogenesis, mutagenesis, and fertility. Pregnancy  Pregnancy Category C Animal reproductive studies have not been conducted with carbinoxamine maleate. It is also not known whether carbinoxamine maleate can cause fetal harm when administered to a pregnant woman or can affect reproductive capacity. Carbinoxamine maleate should be given to a pregnant woman only if clearly needed. Nursing Mothers Because of the higher risk of antihistamines for infants generally and for newborns and prematures in particular, use of carbinoxamine maleate is contraindicated in nursing mothers (see CONTRAINDICATIONS section). Pediatric Use Carbinoxamine maleate is contraindicated in children younger than 2 years of age (see CONTRAINDICATIONS). Geriatric Use Sedating drugs may cause confusion and over-sedation in the elderly; elderly patients generally should be started on lower doses of carbinoxamine maleate and observed closely. ADVERSE REACTIONS The most frequent adverse reactions are underlined: Body as a Whole: Urticaria, drug rash, anaphylactic shock, photosensitivity, excessive perspiration, chills, dryness of mouth, nose and throat. Cardiovascular: Hypotension, headache, palpitations, tachycardia, extrasystoles. Hematologic: Hemolytic anemia, thrombocytopenia, agranulocytosis. Central Nervous System:Sedation, sleepiness, dizziness, disturbed coordination, fatigue, confusion, restlessness, excitation, nervousness, tremor, irritability, insomnia, euphoria, paresthesia, blurred vision, diplopia, vertigo, tinnitus, acute labyrinthitis, hysteria, neuritis, convulsions. Gastrointestinal:Epigastric distress, anorexia, nausea, vomiting, diarrhea, constipation. Urogenital: Urinary frequency, difficult urination, urinary retention, early menses. Respiratory:Thickening of bronchial secretions, tightness of chest and wheezing, nasal stuffiness. OVERDOSAGE Manifestations Antihistamine overdosage reactions may vary from central nervous system depression to stimulation. Stimulation is particularly likely in children. Atropine-like signs and symptoms - dry mouth; fixed, dilated pupils; flushing; and gastrointestinal symptoms may also occur. Especially in infants and children, antihistamine overdosage may cause hallucinations, convulsions, or death. The oral LD50 of carbinoxamine maleate in guinea pigs is 411 mg/kg. Treatment The treatment of overdosage with carbinoxamine maleate is essentially symptomatic and supportive. Vital signs (including respiration, pulse, blood pressure, and temperature) and EKG should be monitored. Induction of vomiting is not recommended. Activated charcoal should be given and gastric lavage should be considered after ingestion of a potentially life-threatening amount of drug. In the presence of severe anticholinergic effects, physostigmine may be useful. Vasopressors may be used to treat hypotension. DOSAGE AND ADMINISTRATION Carbinoxamine maleate is contraindicated in children younger than 2 years of age (see CONTRAINDICATIONS). Carbinoxamine maleate tablets should be taken on an empty stomach with water. DOSAGE SHOULD BE INDIVIDUALIZED ACCORDING TO THE NEEDS AND THE RESPONSE OF THE PATIENT. Carbinoxamine maleate dosage should be based on the severity of the condition and the response of the patient. The drug is well tolerated in doses as high as 24 mg daily, in divided doses, over prolonged periods. On the other hand, some patients respond to as little as 4 mg daily. Clinical experience suggests the following dosage schedules: Tablets Usual Adult Dosage: 1 or 2 tablets (4 to 8 mg) 3 to 4 times daily Usual Child’s Dosage: Over six years – 1 to 1½ tablets (4 to 6 mg) 3 or 4 times daily. Oral Solution Usual Adult Dosage: 1 or 2 teaspoonfuls (4 to 8 mg) 3 to 4 times daily Usual Child’s Dosage (approximately 0.2 – 0.4 mg/kg/day): Two to three years –½ teaspoonful (2 mg) 3 or 4 times daily. Three to six years –½ teaspoonful to 1 teaspoonful (2 to 4 mg) 3 or 4 times daily Over six years - 1 to 1½ teaspoonfuls (4 to 6 mg) 3 or 4 times daily. HOW SUPPLIED Carbinoxamine Maleate Tablets, USP 4 mg are supplied as white, round, scored tablets, debossed “PAL” on one side and score “4” on the other side, and are supplied in bottles of 100 tablets, NDC 0525-6748-01 and bottles of 500 tablets, NDC 0525-6748-05. Carbinoxamine Maleate Oral Solution, 4 mg/5 mL is supplied as clear, colorless liquid with a bubble gum aroma, and is supplied in 4 oz bottles NDC 0525-6752-04 and 16 oz bottles NDC 0525-6752-16. Store at controlled room temperature, 15°C to 30°C (59°F to 86°F) [See USP]. Arbinoxa片剂和口服液对过敏可用治疗 山楂制药宣布Arbinoxa（carbinoxamine）片剂和口服液为过敏性（季节性和常年）和血管运动性鼻炎，结膜炎，荨麻疹，血管性水肿，以及治疗血液反应可用。 Arbinoxa也表示，作为一个辅助过敏和对dermatographism治疗。 Arbinoxa片剂，口服液剂AA级泛型Palgic（PamLab）片剂和口服液。 Arbinoxa可作为4毫克片剂和口服液为4mg/5mL。