Mod 1 - Clinical Pharm 8/14 Flashcards
Quiz 1
Define pharmacokinetics.
what the body does to the drug
study of ADME
Define pharmacodynamics.
what the drug does to the body
Define clinical pharmacology.
study of drug effects on the body with an emphasis on the patient
Define ADME.
A = absorption
D = distribution
M = metabolism
E = excretion
why is it important to know the half-life of a drug?
to know when the patient will wake up and when you should redose
why is it important to know the clearance time of a drug?
to know when the patient will be fully recovered and when they will fully clear the drug from their body
the rate of absorption of a drug determines what?
how soon the drug effects will be seen after administration
the amount of drug absorbed determines what?
the intensity of the drug response (i.e., bioavailability; F)
drug distribution is determined by 1, 2, and 3.
- blood flow to tissues
- ability of drug to exit vascular system
- ability of drug to enter cells
why is metabolism an important part of drug pharmacokinetics?
it enzymatically alters the drug’s structure to more readily clear it from the body - biotransformation
what are 4 therapeutic consequences of drug metabolism?
- accelerated drug excretion
- drug inactivation
- activation of pro-drugs
- inc./dec. toxicity
what does phase 1 metabolism accomplish? (3)
- uses oxidoreductases and hydrolases to make a drug more water soluble
- oxidation/reduction/hydrolysis
- can make a drug more OR less biologically active
what does phase 2 metabolism accomplish? (3)
- uses transferases to attach endogenous polar compounds to the drug
- derivatives are highly polar & easily excreted
- makes compounds LESS biologically active
which phase of drug metabolism plays a role in drug toxicity?
phase 1
what are 5 ways drugs can be eliminated from the body?
- urine
- bile
- milk
- sweat
- expired air
what organ is the most important organ in drug elimination?
kidney
T/F - all of the drug is absorbed, distributed, metabolized, and excreted at the same time (there is no circulation of the drug).
False - continuous circulation of drug molecules until all has been metabolized and excreted
what is the AUC (area under the plasma drug concentration-time curve)?
units?
dependent on?
reflects actual body exposure to a drug post-administration
mg*h/L
dependent on rate of elimination & dose
define first-pass effect.
elimination of drug post-administration before reaching systemic circulation (e.g., during passage of gut wall, portal circulation, liver for drug given PO)
define steady state.
condition in which the average total amount of drug in the body doesn’t change over multiple dosing cycles
how many half-lives must you have to reach steady state when giving a drug?
3-5
define therapeutic index.
comparison of amount of therapeutic agent that causes therapeutic effect to the amount that causes toxicity.
define therapeutic range.
range of drug concentrations associated with reasonable probability of efficacy w/o undue toxicity in the majority of patients
define volume of distribution.
theoretic concept relating the amount drug in the body (dose) to the concentration (C) of drug measured
- AKA a drug’s propensity to either remain in plasma or redistribute to other tissue compartments
half-life is (directly/inversely) proportional to clearance and (directly/inversely) proportional to volume of distribution.
inversely
directly
with a larger volume of distribution, there is more drug distributed (to the tissues/in the plasma) compared to the opposite.
to the tissues
if the drug conc. in plasma is too low, the drug 1.
if the drug conc. in plasma is too high, the drug will cause 2.
- elicits no response
- toxicity
define permissible therapeutic range.
between the min effective conc. and the max. effective conc., above which toxicity occurs.
what is “balanced anesthesia”?
name 3 things we want in a properly anesthetized patient.
administering multiple drugs together to provide safe & effective anesthesia
- loss of consciousness
- analgesia
- muscle relaxation
Volume of distribution determines a drug’s what?
dose
Clearance is determined by what?
organ function
AUC is the ? of a drug formulation.
bioavailability
Distribution of a drug influences what?
volume of distribution
Absorption of a drug determines the time to what?
efficacy
Elimination of a drug determines the 1 and the time to 2.
- dosing interval
- steady-state
define sedation.
change in mental state of a patient, resulting in unconsciousness
Name 4 things about sedated animals that you must keep in mind.
- they are arousable
- they can hurt you
- they can hurt themselves
- they can remember what happened while sedated
define immobilization.
change in mental state characterized by:
1. inability to voluntarily move
2. amnesia of events while immobilized may occur
define anesthesia.
change in mental state characterized by:
1. loss of consciousness
2. muscle relaxation
3. analgesia (prevention of pain info transmission to brain)
T/F - administering multiple anesthetic drugs has a higher margin of safety compared to administering a single anesthetic drug.
True
what drug types are used to cause loss of consciousness in a patient for multimodal anesthesia? (2)
- IV anesthetics (like ketamine)
- inhalant anesthetics
what drug types are used to cause muscle relaxation in a patient for multimodal anesthesia? (2)
- benzodiazepines
- alpha-2 agonists
what drug types are used for analgesia in a patient for multimodal anesthesia? (2)
- opioids
- local anesthetics
T/F - SQ/IM administration has the fastest time to maximal plasma concentrations.
False - IV
IV > SQ/IM > PO
what are the 3 therapeutic objectives when administering a drug?
- therapeutic onset (how long does it take to work?)
- length of desired effect (how long will it stay effective?)
- local vs. systemic effect
briefly describe how anesthetic drugs affect the nervous system. (5)
- anesthetic drug activates ion channel
- hyperpolarization of neuron
- dec. NTM release
- inhibition of synaptic communication via inhibition of response of Ach receptors to NTM
- preferentially inhibit post-synaptic receptors
name the 3 parts to the chemical structure of a local anesthetic drug.
- lipophilic end
- hydrophilic end
- intermediate chain
local anesthetics tend to be (strong/weak) (acids/bases).
why?
weak bases
have both a lipid soluble end & a hydrophilic end
briefly describe the mechanism of action of local & regional anesthetics. (5)
- anesthetic binds to Na+ channels, blocking action potential in peripheral nerves
- anesthetic binds to AA residues at binding site
- non-ionized form of anesthetic enters axonal membrane - converted to ionized form
- ionized form binds to Na+ in open state - prolongs Na+ channel inactivation
- Na+ entry blocked during inactivation
what do local anesthetics do to nerve transmission?
reversible block
Higher potency means it takes (more/less) drug to reach the desired effect
less
drug lipid solubility determines drug what?
potency
a higher pKa means the drug has a (slower/faster) onset of action
slower
the higher the tissue vascularity, the (slower/faster) the drug is absorbed
faster
how are amides eliminated from the body?
biotransformed in liver
how are esters eliminated from the body?
enzymatic plasma hydrolysis
what are 4 toxic effects of local anesthetic associated with the CNS?
- depression
- coma
- excitement
- seizures
what are 3 toxic effects of local anesthetic associated with the cardiovascular system?
with rapid IV administration:
1. hypotension
2. bradycardia
3. dysrhythmias
can be direct or mediated by CNS