Biomedical subjects
Publications and source records attributed to J J Brennan.
The rule of anticoagulation therapy in the setting of an acute myocardial infarction has been debated for decades. The role of such therapy in reducing mortality, preventing deep venous thrombosis and pulmonary emboli, and in reducing the frequency of left ventricular thrombus formation and subsequent systemic embolization is discussed.
Eighteen lame boars were equally assigned to two treatment groups based on initial bodyweight and leg soundness. The boars were injected intramuscularly with an aqueous solution of glycosaminoglycan polysulfate or saline on day 0, 5, 10, 15, 20 and 25 and killed on day 27. The glycosaminoglycan polysulfate treatment significantly (P less than 0.05) improved leg soundness score, and resulted in an increase (P less than 0.06) in the hyaluronic acid concentration of the cubitus joint synovial fluid, and an increase (P less than 0.05) in the proportion of aggregated proteoglycans in the articular cartilage of the medial femoral condyle. Feed intake, growth rate and articular cartilage soundness score for the cubitus and stifle joints were not significantly (P greater than 0.10) affected by the treatment.
The effects of the anticonvulsants ethosuximide and valproate on the excitable Na and K channels of the squid giant axon are evaluated and compared. The drugs are highly specific in their effects on channel gating and ion permeability with regard to the membrane side of application. Both drugs when applied internally affect Na activation gating in ways that lead to the conclusion that they do not act as channel blockers. However, external ethosuximide is clearly a voltage-independent Na channel blocker with no effect on channel gating. On the K channel, ethosuximide appears to have a mixed action affecting both gating and the ion flux through open channels. However, valproate slows K channel gating without effect on the flux through open channels. The dose-response curve of the effects has a shape similar to that for ethanol. The implications for paroxysmal discharge and synchronous impulse generation are discussed in a preliminary way.
The major metabolite of sulpiride, N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-sulfamoyl-2-anisamide (I), in the monkey is N-[(1-ethyl-5-oxo-2-pyrrolidinyl)methyl]-5-sulfamoyl-2-anisamide (II). It is also a metabolite in other laboratory animal species and possibly at very low levels in humans. Treatment of the urine from a monkey dosed orally with 14C-I by dry column chromatography and high-pressure liquid chromatography (HPLC) produced the major metabolite in pure form. Characterization of the purified 14C-radiolabeled metabolite by proton NMR, TLC, HPLC, and chemical ionization mass spectroscopy, along with subsequent comparison of a synthetically prepared sample, gave unequivocal structural confirmation.
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The metabolism of 14C-carbonyl-sulpiride (form A) and of 14C-3, 4 pyrrolidine-sulpiride (form B) was studied in the rhesus monkey and man. In the monkey, the metabolites in both the urine and the bile were the same with form A and form B: 60-80% sulpiride, 10-30% 5-oxopyrrolidine sulpiride and 3-8% an unidentified metabolite (ME-X). In four human volunteers given a single oral dose of either 108 mg form A or 100 mg form B, more than 95% of the 14C recovered in the urine and feces was unchanged sulpiride. Sulpiride levels in plasma reached maximum in 3 hr and ranged from 232 to 403 ng/ml. The plasma t1/2 was 8.3 hr. Pharmacokinetic analyses indicated little or no biliary excretion of sulpiride in man.
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