Like other phenylisopropanolamines, small amounts of the drug are slowly metabolized in the liver to an active hydroxylated metabolite. About 80-90% of a dose of phenylpropanolamine is excreted unchanged in the urine within 24 hours. /Phenylpropanolamine hydrochloride/
来源:Hazardous Substances Data Bank (HSDB)
毒理性
相互作用
使用安非他明、非那西丁和三环类抗抑郁药时，甲基多巴的抗高血压作用会减弱。
With amphetamines, phenylpropanolamine, and the tricyclic antidepressants, the antihypertensive effects of methyldopa are lessened.
Concomitant use /of/ phenylpropanolamine and indomethacin was associated with severe hypertension in one patient; hypertension did not occur when either drug was used alone. /Phenylpropanolamine hydrochloride/
Administration of phenylpropanolamine to patients who have received cyclopropane or halogenated hydrocarbon general anesthetics may result in arrhythmias. Arrhythmias, if they occur, may respond to administration of propranolol, a beta-adrenergic blocking agent. /Phenylpropanolamine hydrochloride/
The effects of caffeine and phenylpropanolamine are mediated through activation of the central and sympathetic nervous systems. Severe, life threatening, and occasionally fatal hypertensive reactions have been reported after their combined use. This study examined the possible pharmacokinetic interaction of phenylpropanolamine and caffeine. Sixteen normal subjects received combinations of caffeine, phenylpropanolamine, and placebo. In subjects receiving 400 mg caffeine plus 75 mg phenylpropanolamine, the mean (+ or - SEM) peak plasma caffeine concentration of 8.0 + or - 2.2 ug/mL was significantly greater than after 400 mg caffeine alone (2.1 + or - 0.3 ug/mL; t(24) = 2.4; p < 0.01). Physical side effects were more frequent after the phenylpropanolamine-caffeine combination than after either drug alone or after placebo. Greater increases in both systolic and diastolic blood pressures occurred after the combination than after either drug alone. These data indicate that phenylpropanolamine may enhance absorption or inhibit elimination of caffeine and may explain increased side effects reported after their combined use.
... This may be produced by reversing the effect of phenylpropanolamine on cardiac output. Atropine is useful for bradycardia states, and lidocaine in the presence of ventricular ectopic activity. Bradycardia: atropine sulfate ... . Ventricular tachycardia or frequent premature ventricular contractions: Lidocaine ... . If no response from lidocaine, then use propranolol ... . CNS toxic effects (agitation, disorientation, increased motor activity, hallucinations, hyperventilation, tachypnea) should be treated symptomatically. Seizures: intravenous diazepam ... .
Phenylpropanolamine is well absorbed orally, and the peak blood concentration is attained within one to two hours. ... The drug is principally excreted unchanged; the major route of excretion is renal. Since phenylpropanolamine is a weak base, elimination is enhanced in acid urine.
Phenylpropanolamine is readily absorbed from the GI tract. Nasal decongestion reportedly occurs within 15-30 minutes after oral administration of 25 mg of phenylpropanolamine hydrochloride and appears to persist for 3 hours. Plasma concentrations of the drug required for a therapeutic effect are not known. In one study, peak plasma concentrations of 100 ng/mL were reached in 1-2 hours and concentrations remained greater than 60 ng/ml for 6 hours following oral administration of 50 mg of phenylpropanolamine hydrochloride to fasting adults. Following administration of 150 mg of an extended-release preparation of the drug, peak plasma concentrations of 300 ng/mL occurred after 3.5 hours and phenylpropanolamine concentrations remained greater than 180 ng/mL for 12 hours. /Phenylpropanolamine hydrochloride/
来源:Hazardous Substances Data Bank (HSDB)
吸收、分配和排泄
动物研究表明，苯丙醇胺分布到各种组织和体液中，包括脑脊液和大脑。/盐酸苯丙醇胺/
Animal studies indicate that phenylpropanolamine is distributed into various tissues and fluids, including /cerebrospinal fluid/ and brain. /Phenylpropanolamine hydrochloride/
The bioavailability and pharmacokinetics of phenylpropanolamine hydrochloride from a controlled release caplet and solution were studied in 12 male subjects, aged 18 to 36 yr, who received either a 75 mg caplet once daily or a 25 mg solution 3 times daily for 4 days. Maximum plasma concentrations, time to maximum concentration, and areas under the concentration-time curves are reported for both caplet and solution. The mean first order absorption rate constant, elimination half-life and lag time for the drug from the caplet were 0.488 ngxhr/mL, 5.84 hr, and 0.394 hr, respectively, and 2.87 ngxhr/mL, 3.73 hr, and 0.325 hr, respectively, from the solution. The smaller apparent mean first order absorption rate constant and longer elimination half-life from the caplet is due to the slow release of drug, thereby slowing its absorption and producing sustained plasma drug concentrations.
N,N′-Dialkylated 1,2-diamine derivatives as new efficient ligands for RuCl2(PPh3)3 catalyzed asymmetric transfer hydrogenation of aromatic ketones
摘要：
Chiral N,N'-dialkylated cyclohexanediamine derivatives ligands have been synthesized and used in an asymmetric transfer hydrogenation of aryl ketones. Optically active alcohols with up to 93% enantiomeric excess were obtained in high yield. (C) 2002 Published by Elsevier Science Ltd.
[EN] METHYL OXAZOLE OREXIN RECEPTOR ANTAGONISTS<br/>[FR] MÉTHYLOXAZOLES ANTAGONISTES DU RÉCEPTEUR DE L'OREXINE
申请人：MERCK SHARP & DOHME
公开号：WO2016089721A1
公开（公告）日：2016-06-09
The present invention is directed to methyl oxazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
The present invention relates to compounds of formula I
wherein R
1
to R
4
and G are as defined in the description and claims and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
The present invention relates to compounds of formula I
wherein A and R
1
to R
4
are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
BENZOFURAN AND BENZOTHIOPHENE-2-CARBOXYLIC ACID AMIDE DERIVATIVES
申请人：Mohr Peter
公开号：US20090029976A1
公开（公告）日：2009-01-29
The present invention relates to compounds of formula I
wherein X, A and R
1
to R
4
are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
[EN] NOVEL CYCLIC BENZIMIDAZOLE DERIVATIVES USEFUL ANTI-DIABETIC AGENTS<br/>[FR] NOUVEAUX AGENTS ANTIDIABÉTIQUES UTILES AVEC DES DÉRIVÉS DE BENZIMIDAZOLE CYCLIQUES
申请人：MERCK SHARP & DOHME
公开号：WO2010051176A1
公开（公告）日：2010-05-06
Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
