药动学专业知识讲座.pptxVIP

Object;pharmacokineticsinclude:;drug;biomembranestructure;§1Transmembranetransportationofdrug;药动学专业知识讲座;I.Passivetransport;Mostdrugs;PenicillinGsodium(青霉素G钠)

penicillin-+Na+------water-solubility?

ionization(解离型)

∴Un-ionization(非解离型)------lipo-solubility?;Un-ionizationdegreedependon:

pKa(解离指数)ofthedrug

pHoftheenvironment;bytheHenderson-Hasselbalchequation:;Forexample:;Clinicalsignificance:;II.carrier-mediatedtransport;characteristicsoffacilitateddiffusion:;§2Theprocessofdruginthebody;Routsofadministration;Firstpasselimination(首关消除)

药品经胃肠道吸收后第一次经过肝脏被代谢一部分,使进入血循环有效药量降低,此作用称～.;2.Parenteraladministration(胃肠道外)

1)Inhalation(吸入)

2)Localadministration

includeskin,ear,noseoreyedrops……s;药动学专业知识讲座;2.Distribution;Factoraffectingdistribution:;D+P;药动学专业知识讲座;distributionandredistribution(再分布);combinewithtissue;;Barrier(屏障)phenomenon

Blood-brainbarrier（血脑屏障）BBB;Placentabarrier（胎盘屏障）

Thepermeabilityofplacentabarrierisnotespecial.;药动学专业知识讲座;3.Biotransformation

(metabolism);Phasesofmetabolicreactions;Enzymesforbiotransformation:;Characteristicsoftheenzymes;Enzymerevulsant(药酶诱导剂)

somedrugs??activityofcertainenzyme??metabolism(ownorotherdrug).

e.gphenobarbital(苯巴比妥)……

Enzymeinhibitor(药酶抑制剂)

somedrugs??activityofcertainenzyme??metabolismoftheotherdrug.

e.gcimetidine(西米替丁)……

;+药酶诱导剂;4.Excretion;①Renalexcretion;Clinicalsignificance:;②Biliaryexcretion（胆汁）;others;§3Compartmentmodel(房室模型);Twocompartmentopenmodel;§4Eliminationkineticsofdrugs;§4Eliminationkineticsofdrugs;§4Eliminationkineticsofdrugs;I.Firstordereliminationkinetics

(一级消除动力学)

单位时间内药品消除百分比是恒定.;T1/2;Halflife(半衰期,t?);II.zeroordereliminationkinetics

(零级消除动力学)

单位时间内药品消除量是恒定.;III.mixedeliminationkinetics

(混合消除动力学)