Pharmacokinetics Strychnine




1 pharmacokinetics

1.1 absorption
1.2 distribution
1.3 metabolism
1.4 excretion





pharmacokinetics

absorption

strychnine may introduced body orally, inhalation, or injection. potently bitter substance, , in humans has been shown activate bitter taste receptors tas2r10 , tas2r46. strychnine rapidly absorbed gastrointestinal tract.


distribution

strychnine transported plasma , erythrocytes. due slight protein binding, strychnine leaves bloodstream , distributes tissues. approximately 50% of ingested dose can enter tissues in 5 minutes. within few minutes of ingestion, strychnine can detected in urine. little difference noted between oral , intramuscular administration of strychnine in 4 mg dose. in persons killed strychnine, highest concentrations found in blood, liver, kidney , stomach wall. usual fatal dose 60–100 mg strychnine , fatal after period of 1–2 hours, though lethal doses vary depending on individual.


metabolism

strychnine rapidly metabolized liver microsomal enzyme system requiring nadph , o2. strychnine competes inhibitory neurotransmitter glycine resulting in excitatory state. however, toxicokinetics after overdose have not been described. in severe cases of strychnine poisoning, patient dies before reaching hospital. biological half-life of strychnine 10 hours. half-life suggests normal hepatic function can efficiently degrade strychnine when quantity ingested high enough cause severe poisoning [citation needed].


excretion

a few minutes after ingestion, strychnine excreted unchanged in urine, , accounts 5 15% of sublethal dose given on 6 hours. approximately 10 20% of dose excreted unchanged in urine in first 24 hours. percentage excreted decreases increasing dose. of amount excreted kidneys, 70% excreted in first 6 hours, , 90% in first 24 hours. excretion virtually complete in 48 72 hours.








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