Week 1 - Anesthesia Pharm Flashcards
Roles of the Anesthesia Provider
Perform and document a thorough preanesthesia assessment and evaluation
Obtain/document informed consent for planned anesthetic
Formulate a pt-specific plan for anesthesia care
Implement and adjust plan based on pt’s physiologic response… intervene to maintain optimal physiologic condition
Monitor: oxygenation, ventilation, CV, temp, NMBs, positioning
Define Pharmacodynamics
The action of the drug on the body
“Relationship between the concentration of drug and the magnitude of effect”
Nature of the drug, receptors/receptor sites, inert binding sites, MOA, therapeutic/toxic effect
Define Pharmacokinetics
The effect of the body on the drug
“Relationship between the drug dose and the time course of drug levels in the bloodstream” - at the receptor site of desired action
Binding, permeability, henderson-hasselbach, distribution, elimination
Agonists vs Antagonists
Agonists: cause desired action at receptor
Antagonists: have affinity for receptor but NO efficacy (no action at receptor)
Competitive Antagonist vs Non-Competitive Antagonist
Competitive: antagonism shifts agonist concentration effect curve to the right (binds to same site as agonists - effect is which ever has higher concentration)
Non-Competitive: antagonists may bind irreversibly to the receptor. Lowers number of active receptors available, less effect seen, tend to bind to another site which changes the desired receptor site
ED/C50 and ED/C95
The dose (concentration) of drug needed to obtain 50% and 95% of maximal effect
Lower ED50 = more potent drug
During anesthesia induction we frequently give 2-3x the ED95 to achieve rapid onset
Define Potency of a Drug
A function of affinity for the receptor and function at the receptor
High affinity with low potency = low potency
Low affinity with high potency = HIGH potency
Define Therapeutic Index
Toxic Dose (TD50) divided by Effective Dose (ED50)
High TI indicates relative safety of a drug – the higher the TI the safer the drug
Define Dissociation Constant
Describes the propensity for a drug-receptor complex to break apart
Define Clearance
Rate of Elimination divided by Plasma Drug Concentration
Clearance by an organ = extraction capability of the organ X blood flow to the organ
Zero Order Kinetics vs First Order Kinetics
Zero Order: clearance of drug is constant and NOT dependent upon plasma concentration (Unit/Time)
First Order: clearance of drug is proportional to the plasma concentration (% Eliminated/Time) - basis of the half-life model of drug metabolism
How does half-life vary with Volume of Distribution and Clearance?
Directly with Vd and inversely with clearance
Higher Vd takes longer to clear
High clearance = shorter half-life
What are the phases of metabolism?
Phase I: converts parent drug to more polar (hydrophobic –> hydrophilic)
Phase II: conjugate drug with polar moiety making it more water soluble and excretable
CYP iso’s: P450, P2D P3A(4,5), (50% CYP rxn) responsible for most drug metabolism
Enzyme Induction: stimulation of drug metabolizing enzymes in the liver; usually phase I enzymes
Metabolism - Phase I Reactions
Oxidation, Reduction, Hydrolysis
Metabolism - Phase II Reactions
Makes drugs water soluble for excretion
Glucuronidation, Acetylation, Glutathione Conjugation, Glycine Conjugation, Sulfation, Methylation