Principles of Pharmacology.pdf - Pharmacokinetics R.A Rabin Jacobs School 3rd Floor Room 3222(Sherman 105 [email protected] Material presented and

Principles of Pharmacology.pdf - Pharmacokinetics R.A Rabin...

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PharmacokineticsR.A. RabinJacobs School, 3rdFloor, Room 3222(Sherman 105)[email protected]Material presented and made available for this course is for the educational purposes of students enrolled in PMY 311 for the Spring 2020 semester at University at Buffalo. The material is subject to U.S. copyright law (Title 17, U.S. Code) and is not for further reproduction or transmission.
Learning Objectives & Knowledge PointsBe able to explain the concept of the central compartment and the role of drug concentration in the systemic circulationBe able to explain how drugs cross cell membranesBe able to discuss diffusion and Fick’s law including the factors regulating diffusionBe able to explain and apply the Henderson-Hasselbalch equation including how to calculate % ionizationBe able to discuss the role of pH and pKa on drug ionization and solubility Be able to discuss pH trappingBe able to discuss the properties of carrier-mediated active transportBe able to explain passive vs. carrier-mediated diffusionBe able to discuss the different active transporter classes and how they workBe able to discuss the role of the SLC and ABC transporters in drug absorption and distributionBe able to discuss what happens to a drug once it enters a cell2
Supplemental readingFor overview of Pharmacokinetics see posting from Lippincott Pharmacology on UBLeransApplied Bipopharmaceutics & Pharmacokinetics 7thed by L. Shargel and A.B.C. Yu is available online through the UB Health Sciences Library via HUBNET ( go to “Resources by Subject” and click on Pharmacology and Toxicology”)
Ultimate goal is to achieve this
Pharmacokinetics: movement of a drug into, around & out of the body[Drug]target= f[drug]systemiccirculation(i.e., central compartment)[drug]freeis the critical specie
Drug release & dissolutionDrug in systemic circulationDrug in tissuesExcretion & MetabolismBiologicaleffectabsorptioneliminationdistributionProcesses of Absorption, Distribution, Metabolism & Excretion are occurring simultaneouslyStep 1: Getting the drug into Systemic Circulation (i.e., central compartment)
Common Routes of Drug AdministrationEnteral administration (involving any part of GI tract): Oral (PO)Sublingual (SL)BuccalRectal (PR)Parenteral administration (route Not involving GI tract):Intravenous (IV)Intramuscular (IM) Subcutaneous (SC)Intrathecal (IT)Epidural (ED)IntranasalInhalationTopical/Transdermal (TD)Injectable routes
ParacellulartransportPassive diffusionFacilitated diffusionActive transportDrug TransportersAll route of administration, except for IV, require drugs to pass through cell membrane.

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