strength amount of the drug needed to achieve the intended effect Efficacy Emax

Strength amount of the drug needed to achieve the

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strength, amount of the drug needed to achieve the intended effect Efficacy (Emax): the ability of a drug to produce the desired therapeutic effect Pharmacokinetics Absorption: movement of drugs from its site of administration into blood 1. Variables that influence absorption o Nature of cell membrane o Blood flow at site of administration o Solubility of drug o pH o Molecular weight o Drug concentration o Dosage form 2. How to determine drug dose o Dose-response relationship A. Dose-response curve: depicts the relation btw drug dose and magnitude of effect B. Does below curve/above curve don’t produce a pharmacological response/much additional response (toxicity) o Therapeutic index: Minimum toxic concentration (MTC) to minimum effective concentration (MEC-no therapeutic effect) o Plasma level profile A. Onset of action B. Peak: Max concentration (point at which amount of drug absorbed and distributed is equal to amount metabolized and excreted) C. Duration: Cont’d entry of drug into body w/ levels above MEC D. Termination o Half-life : the time period over which the drug concentration will decrease by half; as a general rule, drugs tend to be administrated at dosing interval that are closed to their half-life o Bioavailability : a percentage of the administrated dose that enters the blood stream and reach the target tissues (oral is lower than IV-> higher dose needed, first-pass metabolism ) Distribution: movement of absorbed drug in bodily fluids throughout body to target tissues (requires adequate blood supply and distribute to areas of high blood flow first) 1. Tissue Distribution o Fat o Lipid-soluble fats have a high affinity for adipose tissue. o Adipose tissue has low blood flow. o Bone: Some drugs have affinity for bone ex) tetracyclines deposit in bones and teeth.
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o Blood-brain barrier: the blood-brain barrier is relatively impenetrable, Usually protective, Only lipid-soluble drugs cross barrier. o Placental barrier: many drugs pass barrier & low molecular weight drugs pass easier. Metabolism (Biotransformation) : chemical change of drug structure 1. Enhance excretion, Inactivate the drug, increase therapeutic action, activate a prodrug, Increase or decrease toxicity, & Excretion 2. Influential factors: o Age o Genetically determined differences o Pregnancy o Liver disease o Time of day o Environment o Diet o Alcohol o Drug interactions 3.
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  • Spring '14
  • Henrikson,J
  • Pharmacology, U.S. Drug Enforcement Administration

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