摘要:

Fenoterol (hydroxyphenylorciprenaline) is chemically closely related to metaproterenol (orciprenaline). It has a higher bronchodilating potency than metaproterenol, albuterol (salbutamol in Europe) or terbutaline. The β2selectivity of fenoterol at normal oral and inhaled doses is the same as for albuterol and terbutaline. Its pharmacodynamic effects are similar to those of other selective β2‐adrenoceptor agonists. It has a high first‐pass metabolism. The long half‐life previously reported in the literature (7 hours) is mainly the half‐life of inactive fenoterol metabolites. The duration of action at equipotent bronchodilating doses seems to be the same as for albuterol and terbutaline, and not longer, as previously reported. Inhalation of β‐adrenoceptor agonists is the superior route of administration. Side effects do not usually occur at normal therapeutic doses. One puff of fenoterol (200 μg) is about equipotent to 2 puffs of albuterol (2 × 100 μg) or 2 puffs of terbutaline (2 × 250 μg) with the same duration of effect. In patients who overdose with the metered‐dose inhaler (MDI), side effects occur at half the number of puffs with fenoterol. Dosage for an acute attack in children is 1 puff (200 μg), repeated within 5 minutes if necessary; in adults 1–3 puffs can be given. For maintenance therapy, the dose in adults is 1–2 puffs 2–4 times daily, while in children 1 puff at night and 1 in the morning may be sufficient. The usual oral dosage has

ISSN:0277-0008    

DOI:10.1002/j.1875-9114.1985.tb03409.x

出版商:Blackwell Publishing Ltd    

年代:1985

数据来源: WILEY

摘要:

Bitolterol, (3–4 diester colterol) is a new β2‐adrenergic agonist. Since it in itself is biologically inactive, bitolterol is considered a pro‐drug. When administered it is activated within the lung by esterase hdyrolysis to the active compound colterol catecholamineN‐t‐butyl‐arterenol). In preclinical and clinical studies to date, bitolterol has proved to be an effective bronchodilator for adult and pediatric patients with chronic stable asthma and for some with chronic obstructive pulmonary disease.Bitolterol has been compared with other β2agents, including isoproterenol, metaproterenol and albuterol. There is no evidence for cardiotoxicity when bitolterol is used in combination with theophylline in human studies. It is effective for control of exercise

ISSN:0277-0008    

DOI:10.1002/j.1875-9114.1985.tb03410.x

出版商:Blackwell Publishing Ltd    

年代:1985

数据来源: WILEY

摘要:

Midazolam is a 1,4‐benzodiazepine derivative with a unique chemical structure: depending on environmental pH, the drug can produce highly water‐soluble salts (pH4). This characteristic contributes to rapid onset of action and to good local tolerance after parenteral administration. After both oral and parenteral administration, midazolam has a fast absorption rate and is rapidly excreted, with a half‐life of only about 2 hours. A reasonably good correlation has been found between plasma levels and clinical effects, indicating a fast but brief response. As a hypnotic, midazolam is mainly indicated in insomniac patients with difficulties in falling asleep or having a pathologic sleep pattern during the first half of the night. No marked hangover effects are present the next morning. In anesthesiology, midazolam appears to be a useful, short‐acting, sedative‐anxiolytic and amnesic premedicant after both oral and parenteral administration. In minor surgery, however, the slow, unpredictable onset and variable duration of action, as compared with thiopental, may inhibit its routine use as an induction agent, especially in young patients, without heavy premedication. In major surgery, midazolam is an alternative to thiopental for induction of anesthesia in spite of its slow, variable induction time. Its advantages include good cardiovascular stability, transient and mild respiratory depression, low frequency of venous irritation, production of anterograde amnesia and short duration of action in comparison with other benz

ISSN:0277-0008    

DOI:10.1002/j.1875-9114.1985.tb03411.x

出版商:Blackwell Publishing Ltd    

年代:1985

数据来源: WILEY

摘要:

Cromolyn is a white crystalline powder which is poorly absorbed from the gastrointestinal tract. Its therapeutic value lies in its functions as an inhaled or topically applied agent.Cromolyn has been approved in the United States for asthma therapy since 1973. It was marketed at that time as a drug to reduce the corticosteroid requirements of severe asthmatics. It clearly did not live up to that claim. Initial enthusiasm for cromolyn was replaced by disillusionment.In the last few years, investigators have taken another look at cromolyn and have a renewed interest in it. Cromolyn's mechanisms of action remain only partially understood. It appears to block allergic mediator release from certain mast cells. It may also decrease bronchial hyperreactivity.The frequency of drug toxicity at customary dosages is extremely low. Adverse effects tend to be mild, short‐lived and without sequelae.Currently, cromolyn is a first line therapy for mild to moderate asthma requiring chronic treatment. It is also of proven efficacy in the treatment of allergic rhinitis, allergic conjunctivitis and vernal keratoconjunctiviti

ISSN:0277-0008    

DOI:10.1002/j.1875-9114.1985.tb03412.x

出版商:Blackwell Publishing Ltd    

年代:1985

数据来源: WILEY

摘要:

Sodium valproate has been in clinical use for the treatment of epilepsy in Great Britain since 1973 and in the United States since 1978. It is chemically quite different from the existing antiepileptic drugs. Although most authorities concentrate on its modification of GABAergic inhibitory transmission in the central nervous system, its mechanism of action remains obscure. It has been shown to be an effective antiepileptic drug in a wide variety of seizure types, but clinically, its major use to date has been in generalized seizures. It is particularly effective in photosensitive epilepsy and myoclonus. Most adverse reactions to sodium valproate are mild and reversible, but with increasing experience, the drug's rare, idiosyncratic, adverse effects are becoming apparent, particularly hepatotoxicity and teratogenicity. The role of therapeutic drug monitoring in the management of patients taking sodium valproate is controversial.

ISSN:0277-0008    

DOI:10.1002/j.1875-9114.1985.tb03413.x

出版商:Blackwell Publishing Ltd    

年代:1985

数据来源: WILEY

ISSN:0277-0008    

DOI:10.1002/j.1875-9114.1985.tb03414.x

出版商:Blackwell Publishing Ltd    

年代:1985

数据来源: WILEY