摘要:

Abstract:Rat sarcolemma preparations were incubated with some membranes stabilizers to study their effects on the (Na+,K+)‐ and Ca2+‐ATPase activity. The drugs inhibited the enzymes with the same order of potency as in the earlier observed muscle contractures: chlorpromazine>dibucaine>propranolol>tetracaine>procaine (range 0.1–3.6 mM) (Røed&Brodal 1979). The contracture inducing effect of the stabilizers is suggested to be caused by a membrane depolarization due to the (Na+,K+)‐ATPase inhibition. Ouabain inhibited the (Na+,K+)‐ATPase activity in purified plasma membrane, but did not inhibit the sarcolemma located ATPases or induce any c

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1981.tb01589.x

出版商:Blackwell Publishing Ltd    

年代:1981

数据来源: WILEY

摘要:

Abstract:Ten former ergotamine abusers were given ergotamine tartrate 0.5 mg/70 kg intravenously. The arterial response was followed by measuring systolic blood pressures with strain gauge on arm, fingers, ankles and toes. Distal systolic blood pressures were significantly reduced relative to the arm level for 22 hours. The arterial response in these 10 patients was compared to the response in 17 migraine patients tested with the same technique. No differences were found. We conclude that hypersensitivity or tolerance to ergotamine tartrate is not observed in previous ergotamine abusers. Previous abuse is a relative contraindication to the use ofergotamine.But if ergotamine is the only effective drug, normal dosage can be used according to the present results.

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1981.tb01590.x

出版商:Blackwell Publishing Ltd    

年代:1981

数据来源: WILEY

摘要:

Abstract:Bisacodyl (BIS), the parent diphenol (DES) and its sulphuric acid di‐ester (picosulphate = PICO) were given by stomach tube to fasted rats at a dose of 3.1 μmol/100 g rat. Bile was sampled in the periods 0–6, 6–12 and 12–18 hrs after drug administration, and assayed for total diphenol (= free + conjugated) by HPLC. Mean fractions (% of dose±S.E.M.) excreted in 5 rats per compound and period were: BIS 74.0±4.7, 51.9±7.9 and 30.8±2.5; DES 41.2±4.3, 46.8±4.7 and 25.1±2.5; PICO 9.0±0.9, 26.0±5.4 and 19.6±3.1. Only minor amounts were excreted as free diphenol. Urine samples taken by bladder puncture and assayed as above furthermore showed that the renal excretion of total diphenol was insignificant compared to the amounts excreted in bile. Practically no diphenol was present in urine 0–6 hrs after the administration of PICO. In experiments with BIS and DES at 0.85 μmol/100 g, total diphenol excreted in bile during 0–6 hrs was: BIS 67.1±2.6 (n = 5); DES: 55.4±3.0 (5). ‐ The latency time for laxative effect was studied in groups of 10 unfasted rats per compound. Cumulative time response curves showed that PICO caused diarrhoea more promptly at 0.85 μmol/100 g than either BIS or DES. In most rats, this delayed action of BIS and DES persisted also at 1.7 μmol/100 g. At 3.1 μmol/100 g, however, the majority of the rats reacted as promptly to these two compounds as to PICO. These results are discussed in relation to the biliary excretion experiments, and interpreted in terms of the relative importance at the different dose levels of: 1. The enterohepatic recirculated fraction, and 2. The non‐absorbed fraction, which passes directly to the large intestine. For PICO, the latter fraction is the single determinant of the effect, which is triggered when the di‐ester is being hydrolyzed to active dip

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1981.tb01591.x

出版商:Blackwell Publishing Ltd    

年代:1981

数据来源: WILEY