AdrenocorticalHormones
Adrenocortical Hormones
IntroductionsteroidsAdrenocorticalhormonesareadrenal cortex.The secretionsecreted fromisofcontrolledby the pituitaryreleasecorticotropin (ACTH) and renin-angiotensin-system (RAS)
Introduction Adrenocortical hormones are steroids secreted from adrenal cortex. The secretion is controlled by the pituitary release of corticotropin (ACTH) and renin-angiotensinsystem (RAS)
ClassificationGlucocorticoids(fromzonafasciculata)-cortisone,hydrocortisoneMineralocorticoids(fromzonaglomerulosa)--aldosterone,desoxycorticosteroneSexhormones (fromzona reticularis)福androgen
Classification ➢ Glucocorticoids (from zona fasciculata) - cortisone, hydrocortisone ➢ Mineralocorticoids (from zona glomerulosa) - aldosterone, desoxycorticosterone ➢ Sex hormones (from zona reticularis) - androgen
HypothalamusstressCorticotropinreleasingfactorAnteriorpituitaryCorticotropin(ACTH)zonaAidosteroneglomerulosaZonaCortisolfasciculataZonaAndrogensreticularisAdrenalmedulla
SecretedRateandBloodConcentrationof TypicalAdrenocorticalHormonesAldosteroneHydrocortisone10 mg/d0.125 mg/dSecretedrate at normal conditionPeripheral plasma concentration8AM16 μg/100ml0.1 μg/100ml4 PM4 μg/100ml0.1μg/100ml
Secreted Rate and Blood Concentration of Typical Adrenocortical Hormones Hydrocortisone Aldosterone Secreted rate at normal condition 10 mg/d 0.125 mg/d Peripheral plasma concentration 8 AM 16 μg/100ml 0.1 μg/100ml 4 PM 4 μg/100ml 0.1 μg/100ml
Chemical StructureThe basic structures of adrenocorticalhormonesare steroids,which consistof fourrings: A, B, C and D.The ketonegroup at C3,doublebondsbetween C4 and Cs as well as the carbonylgroup at C2oareessential groups to maintainthebiological activity
Chemical Structure The basic structures of adrenocortical hormones are steroids, which consist of four rings: A, B, C and D. The ketone group at C3 , double bonds between C4 and C5 as well as the carbonyl group at C20 are essential groups to maintain the biological activity
ChemicalStructuresofSeveralAdrenocorticalHormones21CHOHCH2OH20 CO20C0H3C18OHOHD1619LeH3Chydrocortisonedesoxycorticosterone
Chemical Structures of Several Adrenocortical Hormones desoxycorticosterone hydrocortisone
ChemicalStructuresofSeveralAdrenocorticalHormonesCH,OHHOCH,OHC=0HCH3COHHOHH3CHHaldosteroneprednisolone
Chemical Structures of Several Adrenocortical Hormones aldosterone prednisolone
GlucocorticoidsPharmacokinetics·Rapid absorptionafteroral,intramuscularorintravenousadministration.1-2hoursofpeaktimeand8~12hoursofduration·80%withofbindingcirculatinghormonescorticosteroid bindingglobulin(CBG),10%bindingwithalbuminand10%free
Glucocorticoids Pharmacokinetics • Rapid absorption after oral, intramuscular or intravenous administration • 1~2 hours of peak time and 8~12 hours of duration • 80% of circulating hormones binding with corticosteroid binding globulin (CBG), 10% binding with albumin and 10% free
GlucocorticoidsPharmacokineticsInactivation in liver by reduction of double bondsbetweenC4andCsofringAMostmetabolitesexcretedinurine
Glucocorticoids Pharmacokinetics • Inactivation in liver by reduction of double bonds between C4 and C5 of ring A • Most metabolites excreted in urine