57 Questions
What is the primary inhibitory neurotransmitter in the brain?
GABA
What does the efficacy of a drug refer to?
The maximal response when all receptor sites are occupied
How is the primary mechanism of termination of action of a bolus dose of an anesthetic induction agent achieved?
Redistribution to the vessel intermediate group
What does volume of distribution represent?
The dosage divided by the initial plasma concentration of the drug
Which type of drugs activate the GABAA receptor?
Sedative-hypnotics
Which measure is considered the best measure of renal function?
Glomerular filtration rate
What is the most reliable measure of glomerular filtration rate?
Creatinine clearance
What is a pharmacokinetic model that can adequately describe the pharmacokinetics of most anesthetic drugs?
Two or three compartment model
What does the lag between peak plasma concentration and peak effect represent from a pharmacodynamic standpoint?
Hysteresis effect
Which type of receptors bind an extracellular molecule (ligand) and convert this input into a change in intracellular behavior?
G protein-coupled receptors
Which family of receptors acts through activation or inhibition of an enzyme, ion channel, or other target?
G protein-coupled receptors
Which type of receptors are typically a tyrosine kinase that phosphorylates an intracellular second messenger?
Enzyme-linked transmembrane receptors
What is the best measure for determining proper bolus dosing for a drug?
$V_dpe$
Which type of drug is poorly absorbed from the GI tract?
Ionized
Where is the principle site of absorption for oral drug administration?
Small intestine
Which route of administration bypasses the liver?
Oral transmucosal
In which of the following does the slowest equilibration of a drug occur?
Bone
Which compartment is the slowly equilibrating compartment?
Vessel poor group
What is the primary mechanism of termination of action of a bolus dose of an induction agent?
Redistribution to other tissues
What is the function of the apparent volume of distribution (Vd)?
Model to explain drug concentration in blood following a given dose
Which of the following does not affect the volume of distribution of a drug?
Renal failure
'Only free drug can cross cell membranes' - this statement refers to which phenomenon?
Protein binding effect on drug distribution
'Most drugs are protein bound to some extent' - what reduces the concentration of plasma proteins?
Age
Which type of receptor consists of a protein linked to 7 transmembrane spanning domains?
G protein-coupled receptor
What results in a conformational change in the G protein-coupled receptor, allowing substitution of GTP for GDP on the Gα protein?
Ligand binding
Which neurotransmitter acts as the primary excitatory neurotransmitter in the central nervous system and is important in learning, memory, and central pain transduction?
Glutamate
Which ion channel opens when ions flow in or out based on their concentration gradients?
Ligand-gated ion channel
Entry of which ion inhibits the cell?
$Cl^-$
Which type of receptor is associated with rapid synaptic transmission, synaptic plasticity, and long-term potentiation?
NMDA receptors
What activates the Gα protein which then activates or inhibits an enzyme, ion channel, or other target?
$GTP$ binding
What characterizes an agonist according to the receptor theory?
Maximal response when all receptor sites are occupied
What is the defining factor for potency according to the receptor theory?
Defined by the dose needed to produce a defined effect
Which type of antagonist can be overcome by large doses of agonist?
Competitive antagonist
What is the main difference between partial and full agonists?
Partial agonists favor an active state less than full agonists
In pharmacokinetics, what does the term 'volume of distribution' refer to?
The distribution of a drug in various body tissues
Which type of drugs come in an acidic solution to render them more water soluble?
Basic drugs
What does $pKa - pH$ indicate when it's a negative number for weak bases?
Less than 50% of the drug is protonated (ionized)
Which enzyme is responsible for the metabolism of the majority of drugs?
CYP3A4
Which phase of drug metabolism increases the drugs polarity preparing it for phase II reactions?
Phase I reactions
What is the formula for hepatic extraction ratio (ER)?
ER = Q x (Cinflow - Coutflow)
Which type of drug metabolism is more affected by changes in liver blood flow?
Flow-limited metabolism
Which drug is categorized as a low hepatic extraction ratio (HER) drug?
Diazepam
Which process involves the passive reabsorption of water-soluble drugs from the tubules?
Tubular reabsorption
What is the formula for Calculated Creatinine Clearance?
(140-age) x lean body mass / Plasma creatinine concentration x 72
What is the main purpose of concentration-response relationships in pharmacodynamics?
To measure the dose required to produce a specific effect
Which term describes the maximum effect a drug can produce?
Efficacy
What is the therapeutic index of a drug?
The ratio of LD50/ED50
What is the main focus of response surface models?
The net effect of combining two drugs
What does ED50 stand for in pharmacology?
The dose required to produce a specific effect in 50% of patients
What is the time required for the drug concentration to decrease by 50% following termination of a steady state infusion?
Context-sensitive half-time
Which mathematical technique is sometimes labeled non-compartmental and may avoid some of the confusion related to trying to perceive a compartment as specific tissues?
Stochastic dosing
What do isoconcentration nomograms plot?
The plasma concentration achieved over time with various infusion rates
What is used to compensate for distribution to peripheral tissues in the BET dosing scheme?
Decreasing rate over time
What is the main consideration when determining the initial infusion rate in practice?
Clearance from the central compartment
What is the primary mechanism for patient controlled sedation with propofol?
An infusion rate is established and patient demand dose increases the rate by a small amount.
What is used to control drug delivery in closed-loop infusions for anesthetic purposes?
Output from the patient as processed EEG or auditory evoked potentials
What does hysteresis/biophase refer to in combined pharmacokinetic/pharmacodynamic models?
The distribution of drug from effect site to less well-perfused tissues, and then ultimately back to the central compartment for clearance.
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