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英文药名: Dibenzyline(Phenoxybenzamine Hcl)
中文药名: 盐酸酚苄明胶囊
药品名称
药物名称：盐酸酚苄明胶囊
英文名称：Phenoxybenzamine
中文别名: 苯苄胺、苯氧苄胺、酚苄胺、双苄胺、氧苯苄胺、盐酸酚苄明
英文别名: Bensylyt、Dibenyline、Dibenzylin、Dibenzyline、Dibenzyran、Phenoxybenz
药物类别：神经系统用药/抗肾上腺素药
药理作用
前列腺增生组织的平滑肌及前列腺腺体外膜均有大量的α受体，受交感神经的兴奋刺激引起前列腺腺体收缩，从而使前列腺段尿道关闭压增大，形成梗阻。膀胱括约肌α受体兴奋引起括约肌收缩，但膀胱逼尿肌主要为β受体支配，不受α受体阻滞药的影响。酚苄明为肾上腺素α受体阻滞药，可松弛前列腺平滑肌及膀胱括约肌，缓解尿道梗阻，使排尿困难症状得以改善。此外，本品还能抑制5α还原酶的活性，使双氢睾丸酮生成减少，阻止前列腺增生的进一步发展。
药动学
口服吸收不完全，因局部刺激强，不作皮下或肌内注射，采用静脉注射。口服后数小时开始作用，持续3～4天。静脉注射后1小时作用达高峰。半衰期约为24小时。在肝内代谢, 多数在24 小时从肾及胆汁排出, 少量在体内保留数天。
适应症
用于周围血管痉挛疾病、休克及嗜铬细胞瘤的治疗。
本品用于前列腺增生症引起的非机械性梗阻所致的排尿困难，如昼夜尿频尿急、尿线细、尿滴沥、排尿等待等症。服药后症状在12～72h内得到改善。也可用于防止尿潴留的发生，对尿潴留已下导管患者也有效。
用法用量
1．成人常用量
①静脉滴注，用于心力衰竭或休克，按体重1mg/kg加于200—500ml氯化钠注射液中滴注1小时以上，用于嗜铬细胞瘤术前应用3天，必要时麻醉诱导时给药一次；
②口服，开始10mg，每日2次，以后隔日增加10mg，直至取得疗效，以20—40mg，每日2次维持，用于治疗周围血管病和嗜铬细胞瘤术前准备或非手术治疗。
2．小儿常用量口服，开始按体重0.2mg/kg，每日2次，或按体表面积6～10mg／平方米，每日1次，以后每隔4日增量一次，直至疗效出现；维持量一日按体重0.4—1.2mg／kg或按体表面积12—36mg／平方米，分3—4次服。
任何疑问，请遵医嘱！
不良反应
主要为直立性低血压，还有鼻塞、口干、瞳孔缩小、反射性心跳加快；神志模糊、倦怠、头痛、阳萎、易睡则较少见。如因逾量而引起了低血压，应立即使病人平卧，腿抬高；常用的升压药无效，需静注去甲肾上腺素，肾上腺素可能加剧低血压，应禁用。
体位性低血压,心动过速, 鼻塞, 口干, 瞳孔缩小。性功能障碍(或性欲下降)。
部分患者可出现轻度口干、鼻塞、头晕、乏力，停药或改服每日1次后症状即可消失，个别患者有心悸或心脏早搏。
严重的不良反应是意料不到的低血压及伴有心动过速的晕厥。心肌梗死患者用此药来改善循环时，可导致或加重肺水肿。常见的不良反应是射精受抑制及鼻塞。此药可致瞳孔缩小、疲劳及胃肠不适。如皮内注射或静注时漏到血管外，可发生严重的坏死反应及过敏反应。
药物相互作用
①与拟交感胺类药同用，升压效应减弱或消失；
②与胍乙啶同用，体位性低血压易发生；
③与二氮嗪同用时二氮嗪的抑制胰岛素释放作用被拮抗。
注意事项
(1)动物试验证明，长期口服可引起胃肠道癌。
(2)本品对妊娠的影响尚未充分研究。
(3)本品在哺乳期妇女应用未发现问题。
(4)本品在小儿应用未经充分研究。
(5)在老年人中本品的研究不充分，但老年人对本品的降压作用敏感，且易发生低温，老年人肾功能较差，用时须注意。
(6)下列情况应慎用：
①脑血供不足时用本品须注意血压下降有可能加重脑缺血；
②代偿性心力衰竭，降压可引起反射性心跳加快，心功能失代偿；
③冠心病可因心跳反射性加速而致心绞痛；
④肾功能不全时可因降压和肾缺血而加重；
⑤上呼吸道感染时可因鼻塞而症状加重。
肾、冠脉功能不全及脑血管病患者慎用。近期有严重心血管疾病或脑血管意外者禁用。
DIBENZYLINE - phenoxybenzamine hydrochloride 10 mg capsules
Wellspring Pharmaceutical Corporation
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DIBENZYLINE
(Phenoxybenzamine hydrochloride)
10 mg capsules
adrinergic, α-receptor blocker
DESCRIPTIONEach Dibenzyline capsule with red cap and body, is 001 Indian policewomen and 10 mg, and containing phenoxybenzamine hydrochloride 10 mg USP. Non-active ingredients D & C Red No. 33, FD & C Red No. 3, FD & C Yellow No. 6 composed of gelatin factor, lactose factor, sodium lauryl sulfate NF, and silicon dioxide NF.
Dibenzyline is N - (2 - chloroethyl) - N, - (1 - methyl - 2 - phenoxyethyl) benzylamine hydrochloride:
Phenoxybenzamine hydrochloride is a colorless, has a molecular weight of 340.3, between 136 ° and 141 ° C the melting of its crystalline powder soluble in water, alcohol and chloroform, insoluble in ether.
Clinical PHARMACOLOGYDibenzyline (phenoxybenzamine hydrochloride) is a long-acting, α-adrenergic receptor blocker, can produce and maintain "chemical sympathectomy" oral. It increases blood flow to the skin, mucous membranes, and abdominal viscera, and lowers both supine and upright blood pressure. It is not the parasympathetic nervous system.
20 to 30 per cent of oral phenoxybenzamine appears to be actively absorbed form.1
Half-life of oral phenoxybenzamine hydrochloride life is not known, but intravenous drug half life of about 24 hours. And to prove the effect of intravenous injection for at least 3 to 4 days, and daily management of the cumulative impact of nearly week.1
Display and USAGEDibenzyline is indicated in the treatment of pheochromocytoma, control high blood pressure and sweating attacks. If excessive tachycardia, you may need to use β-blockers followed.
CONTRAINDICATIONSConditions such as decrease in blood pressure may be undesirable, drug allergy or any of its components.
WARNINGDibenzyline α-adrenergic blockade induced by β-adrenergic receptor leaves opposition. Compounds, to stimulate both types of receptors, which can produce hypotension and tachycardia exaggerated.
Notes
Universal Management, in marked cerebral or coronary atherosclerosis, or used with caution in patients with impaired renal function. Receptor blocking effect may aggravate symptoms of respiratory tract infection.
Drug Interactions2 Dibenzyline (phenoxybenzamine hydrochloride) compounds, which may stimulate both α-and β-adrenergic receptor (ie adrenaline) produced hypotension and tachycardia exaggerated. (See WARNINGS.)
Dibenzyline blocks production levarterenol high temperature, low temperature and block the reserpine production.
Carcinogenic and mutagenic case reports have been reported after long-term and phenoxybenzamine treatment of human cancer. Therefore, the long-term use is not recommended.3 phenoxybenzamine, 4 carefully weighed before the prescription drug benefits and risks.
Phenoxybenzamine hydrochloride showed that in vitro Ames test and mouse lymphoma assay mutagenic activity, it did not show mutagenic activity in vivo mouse micronucleus test. In rats and mice, repeated intraperitoneal injection of phenoxybenzamine hydrochloride (three times per week for up to 52 weeks), resulting in peritoneal sarcoma. Chronic oral administration (up to 2 years) produced malignant intestinal and non-glandular stomach, as well as ulcerative and / or erosive gastritis proventriculus. Since non-glandular squamous cell carcinoma of the dose in all tests was observed phenoxybenzamine hydrochloride, there is a no-observed effect level of 10 mg of small intestine / kg of the tumor (carcinoma and sarcoma). The dose is based on the body surface area, about twice the maximum recommended human dose of 20 mg bid
Pregnancy
Teratogenic effects - Pregnancy Category C Animal reproduction studies have not been enough to complete and Dibenzyline (phenoxybenzamine hydrochloride). It is also not known whether Dibenzyline cause fetal harm when administered to a pregnant woman. Dibenzyline should be given to pregnant women only when really needed.
Lactating women is not clear whether this is excreted in human milk drugs. Because many drugs are excreted in human milk, because the potential of phenoxybenzamine hydrochloride and serious adverse reactions, should be made to decide whether to terminate nursing or discontinue drug, taking into account the importance of the drug to the mother.
Pediatric Use Safety and effectiveness in pediatric patients has not been established.
The following adverse reactions have been bad REACTIONSThe found, but not enough data to support their frequency estimates.
Autonomic Nervous System 1: orthostatic hypotension, tachycardia, inhibition of ejaculation, nasal congestion, miosis.
Miscellaneous: gastrointestinal discomfort, drowsiness, fatigue.
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A
These so-called "side effects", is actually evidence of adrenergic blockade and under different degrees of blockade.
To report 1-866-337-4500 or FDA at 1 - 800 - U.S. FDA - 1088 or www.fda.gov / MedWatch reporting system for suspected adverse reactions, drug companies to contact the source.
Excess
Symptoms, which is largely sympathetic nervous system and the result of blocking the cycle of adrenaline. They may include postural hypotension, resulting in dizziness or fainting, tachycardia, particularly postural, vomiting, lethargy, shock.
Treatment, symptoms and signs over there, stop drugs. The treatment of circulatory failure, if present, is a prime consideration. Slight excess in the case of supine with legs elevated cerebral circulation is usually restored. In more serious cases, the usual measures to combat shock should be institutionalized. Usual vasopressor effect is not ideal. Epinephrine is contraindicated, because it not only stimulate the α-and β-receptor, since the α-receptor blocker, the net effect of epinephrine vasodilation and blood pressure (epinephrine reversal) to decline further.
Patients may have to remain flat, 24 hours or more, in the case of excess, as the long-term effects of drugs. Legs and abdomen adhesive bandages may shorten the period of persons with disabilities.
Intravenous infusion of levarterenol bitartrate2 can be used to combat severe hypotension, because it stimulates α-receptor-based. Although Dibenzyline (phenoxybenzamine hydrochloride) is an α-receptor blocker, tartaric acid adequate doses of levarterenol will overcome this effect.
The oral LD50 phenoxybenzamine hydrochloride is approximately 2000 mg / kg, rat, and about 500 mg / kg in guinea pigs.
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2
As Levophed ® tartrate (norepinephrine tartrate brand) from Abbott Laboratories.
Dosage ADMINISTRATIONThe dose should be adjusted to fit each patient's needs. Small initial dose should be increased slowly until you get the desired results, or block the side effects of a trouble. In each increase, the patient should follow to increase the level before the implementation. Dose should be a relief to the symptoms and / or objectives are to improve, but not so high, side effects from blockade become troublesome point.
At first, 10 Dibenzyline (phenoxybenzamine hydrochloride) twice a day mg. Dose should be increased every day, usually 20 to 40 mg 2 or 3 times a day, until a best dose, such as blood pressure control judgments.
Long-term use of phenoxybenzamine is not recommended (see PRECAUTIONS Carciongenesis and mutation)
Save stored in 25 ℃ (77 ℉); allowed to visit the 15 ° -30 ℃ (59 ° -86 ° F) [see USP controlled room temperature].
How SUPPLIEDDibenzyline (phenoxybenzamine hydrochloride) capsules, 10 mg bottles of 100 (State 65197-001-01).
REFERENCESWeiner, all: drugs that inhibit adrenergic nerves and block Goodman Lake, and Gilman, A, pharmacology, adrenergic receptor-based treatment, the Education Department. 6, New York, Macmillan Publishing Company, 1980, p. 179 182.
Vaidyanathan seconds, Mansour P, Riley bone marrow, Hilst, etc., Singh G: chronic lymphocytic leukemia, small cell carcinoma and squamous synchronous bladder cancer paraplegic man in the long-term phenoxybenzamine therapy. Spinal cord. 2006, 44 (3): 188 - 91.
Release Date March 2009
© source, 2009
Manufacturer
Wellspring Pharmaceutical Corporation
Sarasota, Florida 34243 United States
By Wellspring Pharmaceutical
Canada
Oakville, Ontario L6H 1M5
Product PHOTONOTE: These photos can only shape, color, and print identification. They do not depict actual or relative size.
Product samples shown here has been provided by the manufacturer and reproduced in full color People's Democratic Republic as a quick reference in the identification of assistance. Although every effort has been made to ensure the accurate reproduction, please remember that any visual identification should be considered preliminary. In the case of food poisoning or suspected overdose, drug identification, subject to chemical analysis.
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