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  • Title: [General pharmacology of cefoperazone, a new cephalosporin antibiotic (author's transl)].
    Author: Takai A, Hirai S, Watanabe I, Hiraiwa T, Abe N, Omori M, Muroda T, Nakajima S, Nakada Y, Tanada K, Senda N, Tanaka K, Makino H.
    Journal: Jpn J Antibiot; 1980 Oct; 33(10):994-1018. PubMed ID: 6451724.
    Abstract:
    General pharmacological properties of cefoperazone (CPZ) were studied in various experimental animals. CPZ showed the following effects with intravenous injection to experimental animals. On the central nervous system, CPZ caused vomiting in dogs at 500 mg/kg, pyrexia and slow waves in electroencephalogram in rabbits at 1,000 mg/kg. On the motor and sensory nervous systems, CPZ enhanced slightly the twitch tension of musculus gastrocnemius induced by electrical stimulation in rats at 500 mg/kg. On the respiratory, cardiovascular and autonomic nervous systems, CPZ increased transiently the respiratory rate and potentiated the depressor response to Ach at 125 mg/kg, increased femoral blood flow, potentiated the pressor response to Adr in dogs and decreased the contraction of nictitating membrane induced by electrical stimulation in cats at 500 mg/kg, and then raised the systolic blood pressure in rabbits at 1,000 mg/kg. On the blood, CPZ decreased ChE activity in rabbit plasma at 250 mg/kg, prolonged bleeding time in mice at 500 mg/kg and prothrombin time in rabbits at 1,000 mg/kg. On the smooth muscle organs, CPZ enhanced slightly gastric motility in rabbits and ileal motility in guinea pigs at 62.5 and 125 mg/kg respectively, and promoted gastrointestinal propulsion of BaSO4 meal in mice at 1,000 mg/kg. On the urinary organ, CPZ increased urine volume and electrolytes excretion in dogs at 500 mg/kg. Subcutaneous injection of CPZ scarcely showed any significant effect in experimental animals under the dose of 2,000 mg/kg. In the in vitro experiments, CPZ enhanced slightly the motility of isolated rabbit gastrointestinal tract at 10(-3) g/ml. Assuming the single clinical dose of CPZ should be 10 approximately 40 mg/kg, it is concluded that the occurrence of pharmacological effects observed in experimental animals seems to be very rare clinically.
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