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1. Pharmacology HMROBNS@aol.com
Phone Number: (203) 467-0094
2. Pharmacokinetics & Pharmacodynamics Injected Drugs
3. Pharmacokinetics What the body does to a drug
Absorption
Distribution
Metabolism
Excretion
4. Pharmacodynamics What the drug does to the body
Drug effect on receptors
5. Two Compartmental Model Central Compartment: Intravascular fluid and any highly perfused tissues. Highly perfused tissue receive 75% of CO, but only equal 10% of total body mass. Peripheral Compartments:
Not actual area but calculated.
6. Plasma Concentration Curves a graphic plot of the range of plasma concentrations after an injected drug is given. Plots plasma [ ] against time.
Alpha Phase distribution phase
This begins immediately after injection and reflects the drugs movement from the central compartment (circulation) to the peripheral (tissue) compartment.
Beta Phase elimination phase
Follows the Alpha phase and is a more gradual decline in plasma concentrations.
7. Plasma Concentration Slide...
8. Terms Elimination half time: The time necessary for the plasma concentration to fall 50% during the elimination phase (beta phase)
Context-sensitive half time: Measures half time after an infusion is stopped.
Elimination half-life: the time needed eliminate 50% of the drug from the body.
Effect-site equilibrium: delay between IV administration and desired effect.
Bioavailability- fraction of the administered drug available for absorption
9. Distribution Uptake
Volume of Distribution
Degree of Ionization
Protein Binding
10. Metabolism A. First order kinetics- Constant fraction broken down in a standard time. Independent of plasma concentrations.
B. Zero order kinetics- Constant amount is metabolized- constant amount each unit of time. example: alcohol
11. Metabolism: Pathways Hepatic microsomal enzymes
Non-microsomal enzymes
Oxidative
Reduction
Hydrolysis
Conjugation
12. Clearance Hepatic clearance:
Perfusion dependent
Capacity dependent
Biliary excretion:
Renal clearance:
Glomerular filtration
Tubular secretion
Tubular reabsorption
13. View Dose Response Curves....(See Slide and Handout)
14. Dose response Curves ED 50
Effective Dose in 50%
of the population
LD 50
Lethal Dose in 50%
of the population Therapeutic Index
LD 50/ED 50
15. Pharmacodynamics Receptors
Plasma Levels
16. Terms Sensitivity
Tolerance
Tachyphalaxis
Immunity
Agonist/Anatagonist
17. Any Questions ???????????????????
18. Pharmacokinetics & Pharmacodynamics Inhaled Anesthetics
19. Pharmacokinetics Absorption
Distribution
Metabolism
Elimination
20. PA=Pa=Pbr PA: Alveolar partial pressure of the gas
Pa: Arterial blood partial pressure
Pbr: Brain partial pressure
21. MAC: Minimum Alveolar Concentration The minimum alveolar concentration that will prevent movement to a surgical stimulus in the 50% of the population
22. Distribution:Solubility Coefficients
Blood: Gas Solubility
Oil: Gas Solubility
Tissue: Blood Solubility
23. Factors that Affect MAC Increases
Hyperthermia
Increases in CNS catecholamines
Hypernatremia
Decreases
Hypothermia
Alpha 2 agonists
Pregnancy
Alcohol ingestion
Lithium
Decreases in CNS catecholamines
Hyponatremia
24. No Change in MAC...
Metabolism
Chronic alcohol abuse
Gender
Length of anesthesia
Hyperkalemia or hypokalemia
25. Pharmacodynamics Meyer-Overton Theory
Protein Receptor Theory
GABA Suppression Theory
26. Lecture Finished Go home........