部分中文酚妥拉明处方资料（仅供参考）
短效类a肾上腺素受体阻断药
酚妥拉明（phentolamine），又名立其丁，瑞吉亭（regitine）
【体内过程】
生物利用度低，口服效果仅为注射给药的20%。
口服后30分钟血药浓度达峰值，作用维持约3～6小时；肌内注射作用维持30～45分钟。
大多以无活性的代谢物从尿中排泄。          
【药理作用】选择性地阻断a受体，拮抗肾上腺素的a型作用，但作用较弱。
1. 扩血管、降血压：静脉注射给药能使血管舒张，血压下降，肺动脉压和外周血管阻力降低。其机制主要是：
1）阻断血管平滑肌上的a-受体，有舒血管作用；
2）本药的直接舒张血管的作用，使血管明显扩张，外周阻力降低，血压下降；
3）大剂量也出现阻断b受体的作用。
2. 兴奋心脏作用：兴奋心脏，使心肌收缩力增加，心率加快，心输出量增加。其机制主要是：
1）扩张血管，降低血压，反射性地兴奋心脏的功能； 
2）药物阻断去甲肾上腺素能神经末梢突触前膜的a2-受体（已知a2-受体对递质释放具有负反馈调节作用），减弱负反馈，从而促进神经末梢释放NA，间接兴奋b1-受体，加强心肌功能。偶可致心律失常。
注意：本药对心血管的作用与心血管当时的机能状态有关。当交感神经张力增加时，此降压和快心率的作用更明显。
3．其他:
1)拟胆碱作用，使胃肠平滑肌兴奋，增加胃肠蠕动；
2)拟组胺样作用，使胃酸分泌增加，皮肤潮红等。       
【临床应用】
1．用于外周血管痉挛性疾病及血栓闭塞性脉管炎：如雷诺氏症状--手足发绀、肢端感觉异常、灼痛等，以及冻疮后遗症，栓塞性脉管炎。
2．在静脉滴注去甲肾上腺素发生外漏，可用本品5mg溶于10～20ml生理盐水中，作皮下浸润注射，可改善NA造成的血管高度收缩，皮肤苍白等现象。也用于肾上腺素等拟交感胺过量所致高血压。
3．用于肾上腺嗜铬细胞瘤的诊断和此病骤发高血压危象以及手术前的准备，能使嗜铬细胞瘤所致的高血压下降。
嗜铬细胞瘤90%位于肾上腺髓质嗜铬组织中，促进NA、肾上腺素大量释放。
对于此病的诊断可用本药快速静脉注射5mg,注射后血压在2分钟内迅速下降35/25mmHg并持续5分钟者为阳性。（利用其对肾上腺素升压作用的反转作用）。
作诊断试验时，曾有致死的报告，故应特别慎重。
4．用于抗休克：用于感染性、出血性、心源性休克的治疗。
能使心搏出量增加，血管舒张，外周阻力降低，从而改善休克状态时的内脏血液灌注，解除微循环障碍。
并能降低肺循环阻力，防止肺水肿的发生，但给药前必需补足血容量。
有人主张合用去甲肾上腺素，目的是对抗去甲肾上腺素的a型收缩血管的作用，保留其b型加强心肌收缩力的作用。
5．用酚妥拉明等血管扩张药可治疗其他药物无效的急性心肌梗塞及充血性心脏病所致的心力衰竭。
心力衰竭时，因心输出量不足，交感张力增加，外周阻力增高，肺充血和肺动脉压力升高，易产生肺水肿。
应用酚妥拉明兴奋心脏、舒张小血管的作用，解除心功能不全时的小A小V的反射性收缩作用，降低外周阻力，使心脏后负荷明显降低，左室舒张末期压与肺动脉压下降，心搏出量增加，使心功能不全时的肺水肿、全身性水肿得到改善，心力衰竭得以减轻。      
【不良反应】
常见的反应有低血压，胃肠道平滑肌兴奋所致的腹痛、腹泻、呕吐和诱发溃疡病（可能与其胆碱受体激动作用有关）。
静脉给药有时可引起严重的心率加速，心律失常和心绞痛，因此须缓慢注射或滴注。
胃炎，胃、十二指肠溃疡病，冠心病患者慎用。
Regitine
Generic Name: phentolamine mesylate
Dosage Form: for Injection, USP
Regitine®
C98-25
Regitine®
phentolamine mesylate for injection, USP
DESCRIPTION
Regitine, phentolamine mesylate for injection, USP, is an antihypertensive, available in vials for intravenous and intramuscular administration. Each vial contains phentolamine mesylate USP, 5 mg, and mannitol USP, 25 mg, in sterile, lyophilized form.
Phentolamine mesylate is 4,5-dihydro-2-[N-(m-hydroxyphenyl)-N-(p-methylphenyl) aminomethyl]-1H-imidazole 1:1 methanesulfonate, and its structural formula is
Phentolamine mesylate for injection, USP, is a white or off-white, odorless crystalline powder with a molecular weight of 377.46. Its solutions are acid to litmus. It is freely soluble in water and in alcohol, and slightly soluble in chloroform. It melts at about 178ºC.
CLINICAL PHARMACOLOGY
Regitine produces an alpha-adrenergic block of relatively short duration. It also has direct, but less marked, positive inotropic and chronotropic effects on cardiac muscle and vasodilator effects on vascular smooth muscle.
Regitine has a half-life in the blood of 19 minutes following intravenous administration. Approximately 13% of a single intravenous dose appears in the urine as unchanged drug.
INDICATIONS AND USAGE
Regitine is indicated for the prevention or control of hypertensive episodes that may occur in a patient with pheochromocytoma as a result of stress or manipulation during preoperative preparation and surgical excision.
Regitine is indicated for the prevention or treatment of dermal necrosis and sloughing following intravenous administration or extravasation of norepinephrine.
Regitine is also indicated for the diagnosis of pheochromocytoma by the Regitine blocking test.
CONTRAINDICATIONS
Myocardial infarction, history of myocardial infarction, coronary insufficiency, angina, or other evidence suggestive of coronary artery disease; hypersensitivity to phentolamine or related compounds.
WARNINGS
Myocardial infarction, cerebrovascular spasm, and cerebrovascular occlusion have been reported to occur following the administration of Regitine, usually in association with marked hypotensive episodes.
For screening tests in patients with hypertension, the generally available urinary assay of catecholamines or other biochemical assays have largely replaced the Regitine and other pharmacological tests for reasons of accuracy and safety. None of the chemical or pharmacological tests is infallible in the diagnosis of pheochromocytoma. The Regitine blocking test is not the procedure of choice and should be reserved for cases in which additional confirmatory evidence is necessary and the relative risks involved in conducting the test have been considered.
PRECAUTIONS
General
Tachycardia and cardiac arrhythmias may occur with the use of Regitine or other alpha-adrenergic blocking agents. When possible, administration of cardiac glycosides should be deferred until cardiac rhythm returns to normal.
Drug Interactions
See DOSAGE AND ADMINISTRATION, Diagnosis of pheochromocytoma, Preparation.
Carcinogenesis, Mutagenesis, Impairment of Fertility
Long-term carcinogenicity studies, mutagenicity studies, and fertility studies have not been conducted with Regitine.
Pregnancy Category C
Administration of Regitine to pregnant rats and mice at oral doses 24-30 times the usual daily human dose (based on a 60-kg human) resulted in slightly decreased growth and slight skeletal immaturity of the fetuses. Immaturity was manifested by increased incidence of incomplete or unossified calcanei and phalangeal nuclei of the hind limb and of incompletely ossified sternebrae. At oral doses 60 times the usual daily human dose (based on a 60-kg human), a slightly lower rate of implantation was found in the rat. Regitine did not affect embryonic or fetal development in the rabbit at oral doses 20 times the usual daily human dose (based on a 60-kg human). No teratogenic or embryotoxic effects were observed in the rat, mouse, or rabbit studies.
There are no adequate and well-controlled studies in pregnant women. Regitine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Nursing Mothers
It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from Regitine, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Pediatric Use
See DOSAGE AND ADMINISTRATION.
ADVERSE REACTIONS
Acute and prolonged hypotensive episodes, tachycardia, and cardiac arrhythmias have been reported. In addition, weakness, dizziness, flushing, orthostatic hypotension, nasal stuffiness, nausea, vomiting, and diarrhea may occur.
OVERDOSAGE
Acute Toxicity
No deaths due to acute poisoning with Regitine have been reported.
Oral LD50’s (mg/kg): mice, 1000; rats, 1250.
Signs and Symptoms
Overdosage with Regitine is characterized chiefly by cardiovascular disturbances, such as arrhythmias, tachycardia, hypotension, and possibly shock. In addition, the following might occur: excitation, headache, sweating, pupillary contraction, visual disturbances; nausea, vomiting, diarrhea; hypoglycemia.
Treatment
There is no specific antidote.
A decrease in blood pressure to dangerous levels or other evidence of shocklike conditions should be treated vigorously and promptly. The patient’s legs should be kept raised and a plasma expander should be administered. If necessary, intravenous infusion of norepinephrine, titrated to maintain blood pressure at the normotensive level, and all available supportive measures should be included. Epinephrine should not be used, since it may cause a paradoxical reduction in blood pressure.
DOSAGE AND ADMINISTRATION
The reconstituted solution should be used upon preparation and should not be stored.
Note: Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.
1. Prevention or control of hypertensive episodes in the patient with pheochromocytoma.
For preoperative reduction of elevated blood pressure, 5 mg of Regitine (1 mg for children) is injected intravenously or intramuscularly 1 or 2 hours before surgery, and repeated if necessary.
During surgery, Regitine (5 mg for adults, 1 mg for children) is administered intravenously as indicated, to help prevent or control paroxysms of hypertension, tachycardia, respiratory depression, convulsions, or other effects of epinephrine intoxication. (Postoperatively, norepinephrine may be given to control the hypotension that commonly follows complete removal of a pheochromocytoma.)
2. Prevention or treatment of dermal necrosis and sloughing following intravenous administration or extravasation of norepinephrine.
For Prevention: 10 mg of Regitine is added to each liter of solution containing norepinephrine. The pressor effect of norepinephrine is not affected.
For Treatment: 5-10 mg of Regitine in 10 mL of saline is injected into the area of extravasation within 12 hours.
3. Diagnosis of pheochromocytoma — Regitine blocking test.
The test is most reliable in detecting pheochromocytoma in patients with sustained hypertension and least reliable in those with paroxysmal hypertension. False-positive tests may occur in patients with hypertension without pheochromocytoma.
a. Intravenous
Preparation
The CONTRAINDICATIONS, WARNINGS, and PRECAUTIONS sections should be reviewed. Sedatives, analgesics, and all other medications except those that might be deemed essential (such as digitalis and insulin) are withheld for at least 24 hours, and preferably 48-72 hours, prior to the test. Antihypertensive drugs are withheld until blood pressure returns to the untreated, hypertensive level. This test is not performed on a patient who is normotensive.
Procedure
The patient is kept at rest in the supine position throughout the test, preferably in a quiet, darkened room. Injection of Regitine is delayed until blood pressure is stabilized, as evidenced by blood pressure readings taken every 10 minutes for at least 30 minutes.
Five milligrams of Regitine is dissolved in 1 mL of Sterile Water for Injection. The dose for adults is 5 mg; for children, 1 mg.
The syringe needle is inserted into the vein, and injection is delayed until pressor response to venipuncture has subsided.
Regitine is injected rapidly. Blood pressure is recorded immediately after injection, at 30-second intervals for the first 3 minutes, and at 60-second intervals for the next 7 minutes.
Interpretation
A positive response, suggestive of pheochromocytoma, is indicated when the blood pressure is reduced more than 35 mmHg systolic and 25 mmHg diastolic. A typical positive response is a reduction in pressure of 60 mmHg systolic and 25 mmHg diastolic. Usually, maximal effect is evident within 2 minutes after injection. A return to preinjection pressure commonly occurs within 15-30 minutes but may occur more rapidly.
If blood pressure decreases to a dangerous level, the patient should be treated as outlined under OVERDOSAGE.
A positive response should always be confirmed by other diagnostic procedures, preferably by measurement of urinary catecholamines or their metabolites.
A negative response is indicated when the blood pressure is elevated, unchanged, or reduced less than 35 mmHg systolic and 25 mmHg diastolic after injection of Regitine. A negative response to this test does not exclude the diagnosis of pheochromocytoma, especially in patients with paroxysmal hypertension in whom the incidence of false-negative responses is high.
b. Intramuscular
If the intramuscular test for pheochromocytoma is preferred, preparation is the same as for the intravenous test. Five milligrams of Regitine is then dissolved in 1 mL of Sterile Water for Injection. The dose for adults is 5 mg intramuscularly; for children, 3 mg. Blood pressure is recorded every 5 minutes for 30-45 minutes following injection. A positive response is indicated when the blood pressure is reduced 35 mmHg systolic and 25 mmHg diastolic, or more, within 20 minutes following injection.
HOW SUPPLIED
Vials— each containing 5 mg of phentolamine mesylate for injection, USP, and 25 mg of mannitol, USP, in lyophilized form.
Cartons of 2…………………………………………………………….NDC 0083-6830-02
The reconstituted solution should be used upon preparation and should not be stored.
Store between 15ºC and 30ºC (59ºF-86ºF).
附件:

201241022533140.PDF   
201241022532310.pdf   
201241022525416.PDF
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产地国家: 加拿大
原产地英文商品名:
REGITINE(also called OraVerse) 10mg/ml/amp 5amps/box
原产地英文药品名:
PHENTOLAMINE
中文参考商品译名:
瑞吉亭(也叫OraVerse) 10毫克/毫升/安醅 5安醅/盒
中文参考药品译名:
酚妥拉明
生产厂家中文参考译名:
诺华
生产厂家英文名:
NOVARTIS