Exam 1 Flashcards
what immunoglobulin mediates type 1 reaction?
IgE
immediate-type hypersensitivity characterizes what type of ADR?
type 1
anaphylaxis characterizes what type of drug reaction?
type 1
antibody-dependent cytotoxicity, what type of drug reaction?
type 2
heparin-induced thrombocytopenia is an example of which drug reaction type?
type 2
graft rejection is an example of which drug reaction type?
type 2
heparin-induced thrombocytopenia and graft rejection, examples of which drug reaction type?
type 2
immune complex hypersensitivity- which drug reaction type?
type 3
arthus reaction to tetanus vaccine- which drug reaction type?
type 3
lupus is an example of which drug reaction type?
type 3
cell-mediated or delayed hypersensitivity- which drug reaction type?
type 4
rash, eosinophilia, PPD test, poison ivy- which drug reaction type?
type 4
eosinophilia- which drug reaction type?
type 4
what is the term for drugs that produce receptor site stimulation?
agonists
agonists, think WHAT?
act
what do agonists produce?
receptor site stimulation
antagonists, think WHAT?
block
what type of drugs block receptor site stimulation?
antagonists
what do antagonists block?
receptor site stimulation
what do antagonists do?
block receptor site stimulation
parasympathetic nervous system is part of what system?
autonomic nervous system
what NT does parasympathetic nervous system release?
acetylcholine
acetylcholine is released by what system?
parasympathetic nervous system
what system counterbalances sympathetic activity?
parasympathetic nervous system
what two types of receptors does acetylcholine activate?
muscarinic and nicotinic
what are the two cholinergic receptors?
muscarinic and nicotinic
muscarinic and nicotininc receptors are activated by what?
acetylcholine
what effect does parasympathetic nervous system have on pupils?
constriction
what effect does PNS have on salivation?
stimulates salivation
what effect does PNS have on heart rate?
decreases HR
what effect does PNS have on contractility?
decreases contractility
what effect does PNS have on bronchi?
bronchial constriction
what effect does PNS have on digestion?
stimulates digestion
what effect does PNS have on gallbladder?
stimulates gallbladder
what effect does PNS have on bladder?
contracts bladder
what effect does PNS have on rectum?
relaxes rectum
what effect does PNS have on peripheral vascular system?
peripheral vasodilation
what do most postganglionic neurons release? (NT)
norepinephrine
what do adrenal medullary neurons release? (NT)
mix of epinephrine and norepinephrine
sympathetic nervous system is under which nervous system?
autonomic nervous system
what are the three types of receptors activated by epinephrine and norepinephrine?
alpha, beta, dopamine
what are the three types of adrenergic receptors?
alpha, beta, dopamine
alpha, beta, and dopamine are what type of receptors?
adrenergic
what effect does SNS have on pupils?
dilates pupils
what effect does SNS have on salivation?
inhibits salivation
what effect does SNS have on bronchi?
bronchial dilation
what effect does SNS have on heart rate?
increased heart rate
what effect does SNS have on digestion?
inhibits digestion
what effect does SNS have on contractility?
increases contractility
what effect does SNS have on glucose release?
stimulates glucose release by liver
what effect does SNS have on bladder?
relaxes bladder????
what effect does SNS have on rectum?
contracts rectum
what effect does SNS have on peripheral vascular system?
peripheral vasoconstriction
what type of drug is clonidine?
central acting adrenergic agonists
can you stop taking central acting adrenergic agonists abruptly? (e.g. clonidine)
no
what type of receptors are found in the eyes, salivary glands, arterioles, GI and GU tract?
alpha 1 receptors
where are alpha 1 receptors located?
eyes, salivary glands, arterioles, GI and GU tract
what happens when alpha 1 receptors are stimulated?
cause vascular and GI smooth muscle contraction
what effect do alpha 1 agonists have on peripheral vascular resistance?
increased peripheral vascular resistance
what effect do alpha 1 agnosists have on contractility?
increased contractility
what effect do alpha 1 agonists have on blood pressure?
increased blood pressure
alpha 1 agonists- vasoconstriction or vasodilation?
vasoconstriction
phenylephrine is an example of what type of drug?
alpha 1 agonists
methoxamine is an example of what type of drug?
alpha 1 agonists
what are two examples of alpha 1 agonists?
phenylephrine and metoxamine
what are the side effects of alpha 1 agonists?
headache, bradycardia, excitability, and restlessness
headaches, bradycardia, excitability, restlessness- side effects of what drug class?
alpha 1 agonists
what type of medication should be avoided with alpha 1 antagonists?
NSAIDS
doxazosin/cardura- what drug class?
alpha 1 antagonist
prazosin (for PTSD) what drug class?
alpha 1 antagonist
terazosin- what drug class?
alpha 1 antagonist
alpha 1 antagonists are often given for what condition?
BPH
what do alpha 1 antagonists do in the context of BPH?
block contraction of the GU smooth muscle so patients can urinate
what do alpha 1 antagonists do in the context of HTN?
help lower blood pressure through vasodilation as it inhibits norepinephrine
what NT do alpha 1 antagonists inhibit?
norepinephrine
alpha 1 antagonists cause vasoconstriction or vasodilation?
vasodilation
reflex tachycardia- SE of what drug class?
alpha 1 antagonist
orthostatic hypotension- seen with what drug class?
alpha 1 antagonist
fluid retention- seen with what drug class?
alpha 1 antagonist
peripheral edema- seen with what drug class?
alpha 1 antagonist
nasal congestion- SE what drug class?
alpha 1 antagonist
blurred vision- SE what drug class?
alpha 1 antagonist
dry mouth- SE what drug class?
alpha 1 antagonist
syncope- SE what drug class?
alpha 1 antagonist
impotence- SE what drug class?
alpha 1 antagonist
what is heart rate trying to compensate for as SE of alpha 1 antagonists?
hypotension (blood vessels become bigger when relaxed)
increased HR is compensating for what with alpha 1 antagonists?
hypotension (blood vessels become bigger when relaxed)
where are alpha 2 receptors located?
presynaptic nerve terminal of the smooth muscles, platelets, and lipocytes
what receptors are located in the presynaptic nerve terminal of the smooth muscles, platelets, and lipocytes?
alpha 2
what effect do alpha 2 agonists have on NE?
decreases NE
what effect do alpha 2 agonists have on peripheral vascular system?
cause vasodilation
what effect do alpha 2 agonists have on peripheral vascular resistance?
decreased PVR
what effect do alpha 2 agonists have on renal vascular resistance?
decreased renal vascular resistance
what effect do alpha 2 agonists have on HR?
decrease HR
what effect do alpha 2 agonists have on sympathetic response?
blocks body’s sympathetic response
what effect do alpha 2 agonists have on cardiac output/blood flow?
decreased cardiac output/blood flow
clonidine is an example of what drug class?
alpha 2 agonist
methyldopa is an example of what drug class?
alpha 2 agonist
clonidine and methyldopa are examples of what drug class?
alpha 2 agonist
what drug class should be avoided with coronary insufficiency, CVD, MI, renal function impairment and reacts with beta blockers?
alpha 2 agonist
what are the side effects of alpha 2 agonists?
hypotension, dry mouth/mucous membranes, bradycardia, impotence, nightmares, sedation
hypotension, dry mouth/mucous membranes, bradycardia, impotence, nightmares, sedation- SE what drug class?
alpha 2 agonist
what drug class increases release of norepinephrine?
alpha 2 antagonist
what drug class increases NE release and can be used in some cases to treat sexual dysfunction?
alpha 2 antagonist
what are two examples of alpha 2 antagonists?
yohimibine and idazoxan
yohimbine and idazoxan- what drug class?
alpha 2 antagonist
three common side effects of alpha 2 antagonists?
dizziness, headaches, and reflex tachycardia
dizziness, headaches, reflex tachycardia- common SE of what drug class?
alpha 2 antagonist
beta 1 antagonist- what effect on heart rate?
decrease heart rate
beta 1 antagonist- what effect on contractility?
decrease contractility
beta 1 antagonist- what effect on conduction velocity?
decrease conduction velocity
three examples of beta 1 antagonists?
atenolol, metoprolol, esmolol
atenolol, metoprolol, esmolol- what drug class?
beta 1 antagonist
mild bronchoconstriction, bradycardia, hypotension, impotence- commone SE what drug class?
beta 1 antagonist
common SE of beta 1 antagonists?
mild bronchoconstriction, bradycardia, hypotension, impotence
why do you want to avoid beta 1 antagonists in asthmatic patient?
fear of bronchoconstriction
what happens if you stop beta 1 antagonists abruptly? (CV)
cardiac spasms that may potentially lead to MI
location of beta 2 agonist receptors?
smooth muscle of eye, arterioles, venules, bronchioles, liver, pancrease, GI and GU
what receptors are located in the smooth muscle of the eye, arterioles, venules, bronchioles, liver, pancreas, GI and GU tracts?
beta 2 agonist
what drug class- acts as a bronchodilator that can treat bronchospasms?
beta 2 agonist
what drug class- decreases GI tone and motility?
beta 2 agonist
what drug class- relaxes uterine contractions?
beta 2 agonist
what drug class- activates gluconeogenesis in the liver to inrease blood sugar?
beta 2 agonist
what effect does beta 2 agonist have on bronchi?
bronchodilator
what effect does beta 2 agonist have on GI tone and motility?
decreased GI tone and motility
what effect does beta 2 agonist have on uterine contractions?
relaxes uterine contractions
albuterol and terbutaline- examples what drug class?
beta 2 agonist
what are two examples of beta 2 agonists?
albuterol and terbutaline
what class SE- trembling, nervous tension, palpitations, muscle cramps?
beta 2 agonist
common SE of beta 2 agonists?
trembling, nervous tension, palpitations, muscle cramps
what class- cause bronchoconstriction on beta 2 receptors, oppose vasodilation, increase PVR?
beta 2 antagonists
what effect do beta 2 antagonists have on bronchi?
bronchoconstriction
what effect do beta 2 antagonists have on PVR?
increase PVR
what effect do beta 2 antagonists have on vasodilation?
oppose vasodilation
what class- used for angina, HTN, post-MI, migraines, glaucoma?
beta 2 antagonists
what are uses for beta 2 antagonists?
angina, HTN, post-MI, migraines, glaucoma
common SE what class? Tachycardia, tremors, anxiety, depression, hypotension, sexual dysfunction, arrhythmias
beta 2 antagonists
what are common SE of beta 2 antagonists?
tachycardia, tremors, anxiety, depression, hypotension, sexual dysfunction, arrhythmias
beta 2 antagonists- avoid giving this med to who? (more than B1)
asthmatics
beta 2 antagonists should be avoided more than B1 in asthmatic patients why?
bronchoconstriction
beta 2 antagonists- use caution in what patient popultion?
diabetic patients
why should beta 2 antagonists be used cautiously in diabetic patients?
block symptoms of hypoglycemic episoes
what is an example of a beta 2 antagonist?
propranolol
propranolol- what drug class?
beta 2 antagonists
where is sodium bicarbonate most likely to be absorbed?
intestines
what is the most frequent category of drug-WHAT interaction?
food
why is drug-food interaction the most common?
food affects the GI absorption of drugs
how should oral enteric-coated tablets be taken?
to achieve the best effect take the tablet with at least 8 oz of fluid
how much fluid should be taken orally with EC tablets?
8 oz
food in the GI tract affects drug absorption by?
altering gastric emptying time
food can alter the Ph of the stomach leading to…?
altered drug bioavailability
lipid solubility of the drug affects what?
drug absorption
a rich blood supply to the area of absorption leads to what?
better drug absorption
term- the fraction of a drug that reaches the systemic circulation?
bioavailability
what is the definition of bioavailability?
the fraction of drug that reaches the system circulation
what factors (5) affect bioavailability?
solubility, chemical structure, size, polarity, pre-systemic biotransformation
solubility, chemical structure, size, polarity, pre-systemic biotransformation affect what?
bioavailability
what (4) things do drug absorption depend on?
first pass metabolism, food, surface area, drug size
first pass metabolism, food, surface area, drug size- affect what?
drug absorption
fasting for an extended period of time can do what to absorption?
cause vasoconstriction which leads to decreased drug absorption
a low-carb, high-protein diet may what?
increase drug metabolizing enzymes
why do you not crush a sustained-release capsule?
if you crush the capsule the coated beads of drug can lead to toxicity
why is medroxyprogesterone/depo provera given IM?
to create a storage reservoir
what does the storage reservoir create (depo)?
increased length of time the drug is available and can be actively distributed
the ability of the body to excrete drugs via the renal system would be increased by…?
unbinding a nonvolatile drug from the plasma protein
until drugs are changed or excreted they continue to what?
act in the body
what is the difference in drug effects between men and women? (pharmacokinetics)
percentage of fat differs between the genders
nurse practitioner prescriptive authority is regulated by what?
state board of nursing
three facets of therapeutic goals when prescribing medications?
curative, palliative, and preventative measures
patient education regarding prescription medication should include discussion of what?
expected adverse drug reactions
assessment to determine diagnosis is what type of factor in prescribing medication?
factor associated with clinical judgement
review of potential alternative therapies is what type of factor in prescribing medication?
factor associated with clinical judgement
least invasive, least expensive, and least likely to cause an adverse reaction- what type of factor in prescribing medication?
factor associated with clinical judgement
assessment of other medications and supplements the patient is taking- what type of factor in prescribing medication?
factor associated with clinical judgement
what are the four factors associated with clinical judgement in prescribing medication?
(1) assessment to determine diagnosis (2) review of potential alternative therapies (3) least invasive, least expensive, least likely to cause an adverse reaction, (4) assessment of other medications and supplements that the patient is taking
what criteria should be followed for choosing an effective drug?
consulting nationally recognized guidelines for disease management
what are three cultural factors that must be considered when prescribing medications?
(1) who is the decision maker in the family for health-care decisions (2) patient’s view of health and illness (3) attitudes regarding use of drugs to treat illness
pharmacodynamic considerations in prescribing with different ethnicities?
ethnic differences have been found in drugs in regard to hepatic metabolism
what are patient benefits to having an APRN prescriber?
nurses care for the patient from a holistic approach and include patient in decision making regarding their care
why may NP thrive under healthcare reform?
the demonstrated ability of nurse practitioners to control costs and improve patient outcomes
what are the four clinical influences affecting how providers make decisions?
(1) competing demands (2) knowledge of and agreement with clinical guidelines (3) organizational issues- ancillary support; follow-up appointments (4) assessment of patient adherence
(1) competing demands (2) knowledge of and agreement with clinical guidelines (3) organizational issues- ancillary support; follow-up appointments (4) assessment of patient adherence are WHAT?
four clinical influences affecting how providers make decisions
what are the five medication-related factors affecting how providers make decisions?
(1) side effects (2) contraindication (3) cost (4) convenience/complexity/dosing (4) patient/provider medication knowledge
diabetes-related knowledge is part of what consideration?
patient attitudes and values (how providers make decisions)
what factors are considerations involving patient attitudes and values? (3) (how providers make decisions)
(1) perceived risk (2) belief in treatment efficacy (3) health goals/values
cognitive skills (memory) affect what?
how providers make decisions- patient influences
health literacy affects what?
how providers make decisions- patient influences
autonomous motivation affects what?
how providers make decisions- patient influences
self-efficacy affects what?
how providers make decisions- patient influences
social support- affects what?
how providers make decisions- patient influences
environmental barriers- affects what?
how providers make decisions- patient influences
general adherence affects what?
how providers make decisions- patient influences
symptom burdon affects what?
how providers make decisions- patient influences
comorbidities affect what?
how providers make decisions- patient influences
diabetes-specific emotional distress affects what?
how providers make decisions- patient influences
drugs with a significant WHAT are rapidly metabolized by the liver and may have little, if any, desired action?
first pass effect
drugs with a significant first pass effect are what?
rapidly metabolized by the liver
drugs with a signifcant first pass effect that are rapidly metabolized by the liver may have what?
little if any desired action
what percentage of drugs are eliminated in the liver at first?
0.5
50% of drugs are eliminated in the liver at first and then go where?
systemic circulation
how many half lives are required to eliminate a drug? (significant FPE)
4-5 half lives
drugs are metabolized mainly by the liver in what two reactions?
phase I and phase II
phase I and phase II reactions change drug molecules into…?
a form that an excretory organ can excrete
WHAT may be more active, less active, or totally deactivated compared to parent drug?
metabolites
metabolies may be WHAT (3 things) than parent drug?
more active, less active, or totally deactivated
term? The proportion of a drug which enters the circulation when introduced into the body and so is able to have an active effect
bioavailability
bioavailability is what?
the proportion of a drug which enters the circulation when introduced into the body so is able to have an active affect
when are bioavailability issues especially important?
drugs with narrow therapeutic ranges or sustained-release mechanisms
term? The time it takes for the concentration of the drug in the body to fall by halg/50%
half-life
what is the half life?
the time it takes for the concentration of the drug in the blood to fall by half/50%
term? The amount of drug needed to get the concentration in the plasma to a therapeutic level quicker
loading dose
what is the loading dose?
the amount of drug needed to get the concentration in the plasma to a therapeutic level quicker
Example of what? Z-pack with 2 pills the first day to achieve a therapeutic range
loading dose
term? The time between drug administration and the minimum concentration of a drug to produce an effect
onset of action
what is the onset of action?
the time between drug administration and the minimum concentration of a drug to produce an effect
how is the onset of action seen on drug concentration curve?
first sign of therapeutic effect
term? The time between drug administration and the maximum concentration of a drug in the blood stream
peak of action
another term for peak of action
best therapeutic effect
what is the definition of peak of action?
the time between drug administration and the maximum concentration of a drug in the blood stream
what is the definition of best therapeutic effect?
the time between drug administration and the maximum concentration of a drug in the blood stream
term? The time between the onset of action and metabolism of the drug below the minimum needed for an effect
duration of action
what is the definition of duration og action?
the time between the onset of action and metabolism of the drug below the minimum needed for an effect
the length of time you have the drug in your system reflects what?
duraction of action
duration of action reflects what?
the length of time you have the drug in your system
term? The ability of a drug to produce a maximum effect at any dosage
efficacy
what is the definition of efficacy?
the ability of a drug to produce a maximum effect at any dosage
term? The expression of the maximum effect a drug can produce
efficacy
efficacy example- asians are known to be fast WHAT- meaning that they require higher doses of drugs to achieve efficacy?
acetylators
effects of tylenol versus morphine is an example of what?
efficacy- morphine is much stronger than tylenol as it produces more pain blocking power
what levels are used to determine therapeutic level of drugs?
peak/trough
peak/trough levels are used to determine what?
therapeutic level of drugs
if a lab result indicates the peak level of a drug is above the WHAT, this means that this will produce an adverse response?
minimum toxic concerntration
if a lab result indicates the peak level of a drug is above the minimum toxic concentration, this means that this will produce an ….
adverse response
examples of meds with peak/trough (2)?
phenytoin; vancomycin
term? The amount of drug in the body that remains constant
steady state
steady state definition?
the amount of drug in the body that remains constant
term? The rate of drug intake that is equal to the rate of drug elimination; attained after approximately four, occasionally five half-lives
steady state
when is steady state attained?
after approximately four, sometimes five half-lives
what does lipophilic mean?
lipid loving
term? Lipid loving
lipophilic
lipophilic drugs generally have a high WHAT?
high volume of distribution
lipophilic drugs are primarily cleared by what organ?
liver
lipophilic drugs have what two properties?
non-ionized, uncharged
lipophilic drugs are small or large in size?
small in size?
do lipophilic drugs cross the membranes easily?
yes
term? Water loving
hydrophilic
hydrophilic definition?
water loving
hydrophilic drugs generall have a low WHAT?
low volume of distribution
lipophilic drugs generally have a LOW or HIGH volume of distribution?
high
hydrophilic drugs generally have a LOW or HIGH volume of distribution?
low
organ that primarily clears hydrophilic drugs?
kidneys
kidneys or liver primarily clear lipophilic drugs?
liver
kidneys or liver primarily clear hydrophilic drugs?
kidneys
hydrophilic drugs- small or large in size?
large
hydrophilic drugs cross membranes easily?
no
hydrophilic or lipophilic drugs cross membranes easily?
lipophilic
ionized/charged or non-ionized uncharged- lipophilic?
non-ionized, uncharged
ionized/charged or non-ionized uncharged- hydrophilic?
ionized/charged
term? Moving from an area of high concentration to an area of low concentration
passive diffusion
passive diffusion- definition?
moving from an area of high concentration to an area of low concentration
what type of drugs can cross the membrane through passive diffusion?
lipid-soluble drugs
what type of drugs have to be filtered through the aqueous pore/paracellular space?
non-lipid soluble drugs
passive diffusion involves moving from an area of WHAT concentration to an area of WHAT concentration?
high to low
hypoalbuminemia affects what?
distribution of drugs to target tissues
what condition? If not enough protein available to bind with the drug
hypoalbuminemia
what condition causes too much free drug to build up in the system and become toxic?
hypoalbuminemia
what happens when drugs are bound to albumin?
they stay in the system longer and are not eliminated
what should you do if giving two protein bound drugs?
consider giving them at different times
what kind of diseases can affect production of albumin?
liver diseases
what are three examples of liver diseases that can affect production of albumin?
AIDS, cancer, cirrhosis
AIDS, cancer, cirrhosis can affect what?
production of albumin
what term? Protects the brain from substances that may harm the brain,
blood brain barrier
term? Protects the brain from hormones and neurotransmitters that are in the rest of the body?
blood brain barrier
blood brain barrier protects brain from what two things in the rest of the body?
hormones and neurotransmitters
WHAT helps maintain a constant environment for the brain?
blood brain barrier
do large molecules pass through BBB easily?
no
low lipid (fat) soluble molecules cross BBB fast or slow?
fast
molecules with a high or low electrical charge cross BBB fast or slow?
slow
typically, only meds that are WHAT cross the BBB?
lipid-soluble
WHAT slows the entry of many drugs into and from brain cells?
BBB
term? Lipid membrane that allows passage of drugs by simple diffusion
fetal placental barrier
smaller molecule or larger molecule drugs pass more easily across fetal placental barrier?
smaller molecule drugs
simultaneous use of several different drugs (drug-drug interactions) increase risk for what?
adverse drug reactions
age groups (2) at risk for ADRs?
young or old
pregant pts are at risk for what?
ADRs
breast feeding patients are at risk for what?
ADRs
hereditary factors play a role in the risk for what?
ADRs
disease states with may affect drug absorption, metabolism, and/or elimination increase risk for what?
ADRs
dry mouth, dry eyes, decreased urine output, increased stomach acid- examples of what?
anticholinergic effects
cannot see, cannot pee, cannot spit, cannot shit—- memory device for what?
anticholinergic effects
anticholinergic prototype drug?
atropine
atropine- drug prototype?
anticholinergic
two types of adverse reactions?
intrinsic and idiosyncratic
term? Predictable and dose-related adverse reaction
intrinsic
term? Unpredictable and not dose-related advserse reaction
idiosyncratic
example of idiosyncratic adverse reaction?
rash
rash is an example of what type of ADR? Intrinsic or idiosyncratic
idiosyncratic
term? Using an FDA approved drug for an indication not on the label
off label prescribing
what is the definition of off label prescribing?
using an FDA approved drug for an indication not on the label
example of off label prescribing?
trazodone (antidepressant) used for sleep
what medications (think patient population) are often used off label?
pediatric medications
term? Types of drug effects- valued response (BP, HR, Pain, coma score)
graded effect
valued response? Term
graded effect
yes/no response (seizure, pregnancy, rash) term?
quantal effect
graded effect definition?
valued response
quantal effect definition?
yes/no response
examples of quantal effect?
seizure, pregnancy, rash
seizure, pregnancy, rash are examples of what drug effect?
quantal effect
examples (4) of graded effect?
BP, HR, Pain, coma score
which will predominate in combined alpha and beta?
alpha
example (two drugs) of combined alpha and beta?
coreg and labetalol
3 uses of combined alpha and beta drugs?
(1) hypertension (2) decreased CHF progression (3) left ventricular dysfunction after MI
(1) hypertension, (2) decreased CHF progression (3) left ventricular dysfunction after MI- what type of drugs used?
combined alpha and beta
hypotension, bradycardia, bronchospasm exacerbation, dizzy, drowsy, mask low blood sugar- SE of what drugs?
combined alpha and beta
common SE of combined alpha and beta?
hypotension, bradycardia, bronchospasm exacerbation, dizzy, drowsy, mask low blood sugar
another term for cholinergic agonists?
parasympathomimetics
another term for parasympathomimetics?
cholinergic agonists
where do cholinergic agonists act? (7)
eyes, heart, blood vessels, lungs, GIT, bladder, sweat glands
what drugs work on eyes, heart, blood vessels, lungs, GIT, bladder, sweat glands?
cholinergic agonists
what are the two types of cholinergic agonists?
muscarinic and nicotinic
two drug examples of muscarinic agonists?
carbachol and pilocarpine
carbachol and pilocarpine are examples of what drug class?
muscarinic agonists
what type of poisoning can occur with poison mushrooms?
muscarinic poisoning
what is the antidote for muscarinic poisoning?
atropine
what three things are muscarinic agonists used for?
treats glaucoma, improves GI tone, and urinary bladder tone
what class? Treats glaucoma, improves GI tone, urinary bladder tone
muscarinic agonists
what class? Metabolize acetylcholinesterase to metabolize and break down acetylcholine at synapses
cholinesterase inhibitor
what class? Use for myasthenia gravis (against nicotinic receptors)
cholinesterase inhibitor
neostigmine and pyridostigmine help what?
swallow, raise eyelids, treat Alzheimers
when should cholinesterase inhibitors be avoided?
if GI/GU obstruction present
side effects of cholinesterase inhibitors?
excess GI stimulation, increased salivation, miosis
excess GI stimulation, increased salivation, miosis- SE of what class?
cholinesterase inhibitor
donepezil drug class?
cholinesterase inhibitor
pesticides? (some) drug class
cholinesterase inhibitor
donepezil side effects reversible?
yes
pesticide SE reversible?
cholinesterase inhibitor SE not reversible
class? Selective blockage specific to organ being targeted
anticholinergics
another name for cholinergic blockers?
anticholinergics
another name for anticholinergics?
cholinergic blockers
how to anticholinergics work?
blocks acetylcholine at muscarinic receptors
where to anticholinergics block acetylcholine?
muscarininc receptors
class? Decreases heart rate, bronchodilation, salivary glands, sweat glands, treats urinary spasms, excitation, and dilates eyes
anticholinergices
anticholinergics dilate or constrict pupils?
dilates
anticholinergics increase or decrease HR?
decrease
effect of anticholinergics on bronchi?
bronchodilation
treats urinary spasms- what class?
anticholinergics
examples (4) of anticholinergics?
atropine, scopolamine, oxybutynin, carbidopa/levodopa
atropine, scopolamine, oxybutynin, carbidopa/levodopa- what class?
anticholinergics
atropine- drug class?
anticholinergic
scopolamine- drug class?
anticholinergic
oxybutynin- drug class?
anticholinergic
carbidopa/levodopa- drug class?
anticholinergic
SE of what drug class- tachycardia, relaxed respiratory muscles, dry mouth, constipation, urinaty retention, dilated eyes, dizziness, confusion?
anticholinergics
SE of anticholinergics?
tachycardia, relaxed respiratory muscles, dry mouth, constipation, urinary retention, dilated eyes, dizziness, confusion
term? Referred to as biotransformation/how drug is broken down
metabolism
drugs with high WHAT will not be given orally?
first pass effect
CYP450 is what?
an oxidative reaction that can vary with genetics
an oxidative reaction that can vary with genetics
CYP450
CYP34A
responsible for metabolism of many drugs
responsible for metabolism of many drugs? (enzyme)
CYP34A (enzyme)
Zithromax has a long or short half life?
long
penicillin has a long or short half life?
short
drug that is inactive until metabolized?
prodrug
prodrug is what?
inactive until metabolized
there is a lack of studies in safety and efficacy for what population?
pediatric
distribution in what population? Less protein binding sites due to less albumin, immature BBB, and increased total body water and lower fat content
infants
there are less WHAT type or binding sites in infants?
less protein binding sites
why are there less protein binding sites in infants?
less albumin
BBB is WHAT in infants?
immature
lower or higher fat content in infants?
lower
increased or decreased TBW in infants?
increased
(metabolism) what organ is immature in infants?
liver
there are not enough WHAT (in metabolism) in infants?
enzymes
older children may require more meds with WHAT metabolism?
higher
less stomach acid until what age?
3 years
there is less what until 3 years of age?
stomach acid
gastric emptying is slowed until what age range?
6-8 months
WHAT is slowed until 6-8 months of age?
gastric emptying
immature kidney function- what population?
infants
immature GFR- what population?
infants
decreased kidney perfusion and renal clearance/urine output until what age?
2 years
higher risk for toxicity until what age?
2 years
first WHO step in prescribing?
define the patient’s problem/make a diagnosis
define the patient’s problem/make a diagnosis (WHO prescribing)- which step?
first step
specify the therapeutic objective and approach- (WHO prescribing)- which step?
second step
choose a drug class, generic med, dose, and suitability- (WHO prescribing)- which step?
third step
start the treatment/write the script- (WHO prescribing)- which step?
fourth step
educate the patient- (WHO prescribing)- which step?
fifth step
monitor effectiveness and for adverse effects (WHO prescribing)- which step?
sixth step
alter the prescription if necessary- (WHO prescibing)- which step?
seventh step
what entity- regulates the labeling of all prescriptions, over the counter medications, and medical devices?
FDA
what entity- collect information and monitor safety of human drugs, animal drugs, biological products, medical devices, food, cosmetics, and radiation emission?
FDA
what entity? Protecting and promoting publich health through regulation
FDA
food safety, tobacco products, RX and OTC, vaccines, biopharmeceuticals, blood transfusions, cosmetics, electromagnetic imaging devices, animal food feeds, veterinary products- regulated by what entity?
FDA
post-marketing surveillance- what entity?
FDA
determines the official labeling for all Rx and OTC medications?
FDA
does FDA have regulation over herbal supplements?
no
definition of off label use?
use of prescription drugs for unapproved indications, age groups, dose, route of administration
term? Use of prescription drugs for unapproved indications, age groups, dose, route of admin
off-label
what two types of drugs can be used in off label ways?
prescription and OTC
off label prescribing is legal unless what?
violates ethical or safety guidelines
drug development- phase 1?
drug is tested on healthy volunteers
drug development- phase 2?
trials with people who have the disease for which the drug is thought to be effective
drug tested on healthy volunteers- what phase?
phase 1
trials with people who have the disease for which the drug is thought to be effective- what phase?
phase 2
drug development- phase 3?
large number of patients in medical research centers receive the drug in phase 3
large numbers of patients in medical research centers receive the drug- which phase?
phase 3
larger sampling provides information about infrequent or rare adverse effects- which phase?
phase 3
when will the FDA approve a new drug application?
if phase 3 studies are satisfactory
what is the minimum number of drug trials?
two
which phase- confirms clinical doses, frequency, and timing of administration for approval?
phase 3
single maximal tolerated dose/several dose levels are tested on the target population- which phase?
phase 2
adverse effects are collected to assess benefit-risk potential- which phase?
phase 3
designed to test the hypothesis of efficacy- which phase?
phase 3
which phase- voluntary and involves postmarket surveillance of the drug’s therapeutic effects?
phase 4
what population- less physiologically tolerate medication error d/t developing renal, immune, and hepatic functions?
infants/children
age-related differences and medication metabolism and mechanisms of action don’t necessarily apply to what population?
pediatric population
why are kids at high risk for toxicity and ADRs?
immature liver and renal function
what is dosing based on in infants/children?
weight (mg/kg)
infants have more or less water?
more
infants have more or less fat?
less
immature liver makes fewer what?
serum proteins
at what age is renal function fully developed?
30 months
when does gastric ph reach adult level?
1 year
acidic environment needed to absorb medication- so MORE or LESS medication will be absorbed by infant?
less
children have a larger or smaller body surface area?
greater
greater body surface area in children leads to greater absorption of what type of medication?
topical
why do infants have greater absorption of topical medication?
skin more permeable
what anatomical/physio features lead to increased absorption of topical medications in infants?
increased hydration; thinner stratum corneum
WHAT will prevent the absorption of IM or SQ medications? (infants)
immature peripheral circulation
less albumin and fewer plasma proteins- what age group?
0-6 months
fewer WHAT in pediatric patients result in higher blood conceptrations of two or more drugs or less affinity for one of the drugs?
fewer BINDING SITES in pediatric patients
BBB not fully developed in infants leading to greater risk of what?
CNS toxicity
cytochrome P-450 3A enzymes play a major role in what?
drug metabolism
what enzyme is low in neonates and doesn’t reach adult levels until about 6-12 months?
34A
when does CYP 34A reach adult levels in babies?
6-12 months
what is the earliest isoenzyme to show activity and present in utero (declines rapidly after birth)?
CYP3A7
what enzyme decreases throughout the first 6 months?
CYP3A7
what enzymes INCREASE after the decrease of CYP3A7?
CYP3A4 and CYP3A5
what enzyme is absent in neonates and does not reach adult levels until 3-5?
2D6
2D6 is relevant in what type of medication?
cold medicine
what is the pathway that metabolizes Robitussin and some of the other ingredients in OTC medications?
Cytochrome P-450 2D6
2d6 reaches adult levels when?
about age 5
neonates and preterm infants have reduced WHAT 3 things re: kidneys?
reduced GFR, reduced tubular secretion, reduced reabsorption
renal function does not reach adult levels until what age?
at least 6 month
decreased renal function in neonates leads to extended WHAT?
half life
medication errors in pediatrics- top two?
1 immunizations; #2 antibiotics
two reasons for drug therapy in pregnang women?
(1) treat pre-existing medical condition (2) treat pregnancy related conditions
five classes of pregnancy/lactation meds?
A B C D X
which class of meds can be used during pregnancy?
B
what hormone decreases gastric tone and motility in pregnancy?
progesterone
what is the effect of progesterone on stomach emptying?
prolonged stomach emptying time
what hormone in pregnancy alters pharmacokinetics of oral medications?
progesterone
what hormone in pregnancy promotes respiratory changes?
progesterone
what effect does progesterone have on tidal volume?
increased tidal volume
what effect does progesterone have on pulmonary vasodilation?
increased pulmonary vasodilation
what effect does progesterone have on inhaled drug absorption?
inhaled drug absorption increased
how much does HR increase in pregnancy?
10-15 beats per minue
how much does blood volume increase in pregnancy?
0.5
what does the increase in blood volume during pregnancy cause?
hemodilution of plasma albumin
plasma levels of what increase during pregnancy?
lipid
what is the result of increased plasma lipid levels in pregnancy?
more unbound and free drug
why is there more unbound and free drug during pregnancy?
drugs compete for receptor site occupied by hormones
what kind of drugs enter fetal circulation?
drugs that are not lipophilic
is drug metabolism altered by pregnancy or lactation?
no
what are the two properties of drugs that allows them to pass easily into breast milk?
increased lipid solubility and low protein binding (e.g. CNS agents)
drugs with low or high molecular weight pass into breast milk?
low molecular weight
drugs during lactation with LOW ph produce low or high concentrations?
high concentrations
changes in what in geriatric patients lead to increased reisk for orthostatic hypotension and falls?
baroreceptor responsiveness
what happens to renal and hepatic blood flow in geriatric patient?
decreased renal/hepatic blood flow (stiffer vessels/atherosclerosis)
term? Gradual deterioration of the immune system
immunosenescence
immunosenescence in geriatric patient leads to increased risk for what two things?
infection and malignancy
what is the #1 cause of morbidity in the elderly?
pneumonia
gastric acid increased or decreased in elderly?
decreased
systemic availability of drug increased or decreased in elderly?
decreased
why is there decreased drug absorption with IM or SQ route in elderly?
decreased blood flow at injection site
decreased GI motility, decreased gastric acidity, reduced blood flow in elderly lead to what?
overall slow drug absorption
what are the three most problematic drugs (decreased drug distribution) in the elderly?
warfarin, dilantin, SSRIs
body mass is increased or decreased in elderly?
decreased
body fat is increased or decreased in elderly?
increased
increased body fat leads to what type of meds having greater time to excretion?
lipophilic (e.g. benzodiazepines)
albumin is increased or decreased in elderly?
decreased
BBB is more or less effective in elderly?
less
cardiac output is increased or decreased in elderly?
decreased
body water is increased or decreased in elderly?
decreased
decreased body water in elderly leads to increased levels of what kind of meds?
hydrophilic
decreased blood flow in elderly results in less what? (metabolism)
drug clearance
what happens to size of liver in elderly?
declines
what happens to hepatocytes in elderly?
decreased
what happens to first pass effect in elderly?
reduced
aging effects the efficiency of what phase of metabolism?
phase 1
phase 1 metabolism involves which enzyme?
cytochrome P450
what two enzyme systems are slowed in elderly?
34A and 2D6
what happens to oxidation in drug metabolism in elderly?
reduced
what is the effect of reduced oxidation on half life in elderly?
extended half life
is phase 1 or phase 2 metabolism affected more in elderly?
phase 1
what is the effect of aging on renal function?
decreased
what is the effect of aging on glomerular filtration?
decreased
what is the effect of aging on renal tubule excretion?
decreased
caution with GFR less than what?
60
patient is asymptomatic until GFR is less than what?
35
levels of WHAT may remain normal despite GFR changes?
creatinine
what happens to muscle mass in elderly?
decreases
there is less or more overall creatinine in elderly?
less
five classes of drugs in elderly at risk for ADR?
HTN, CAD, analgesics/anti-inflammatory, sedatives, GI meds
what meds are often the cause of accidental overdose in elderly?
pain meds
how much is hepatic blood flow decreased in elderly?
nearly one-half
what percentage is hepatic flow decreased by in elderly?
0.4
what percentage of elderly have chronic kidney disease?
0.5
what percentage of elderly are affected by heart failure? (over age 80)
0.4
what effect does aging have on the first pass effect?
decreases
what are the four medications that cause 2/3 of hospitalizations in the elderly?
(1) warfarin, (2) insulin, (3) oral antiplatelet, (4) oral hypoglycemic (sulfonylureas)
what ratio is decreased in elderly affecting distribution to body compartments?
lean body weight to body fat
what happens to level of serum protein in the elderly?
decrease
drug metabolism can be affected by what two types of substance abuse in elderly?
alcohol, polypharmacy
what are two examples of medication factors- ADRs in elderly?
drug to drug or drug to food
what are two examples of physiological aging changes- ADRs in elderly?
cant hear instructions; can’t see label
what are patient-related errors in ADRs in elderly?
cognitive; sensory
polypharmacy is an example of what type of ADR/error in elderly?
system error
what age group (elderly) is at high risk for ADR?
> 85
what BMI (elderly) is at high risk for ADR?
<22
what creatinine clearance is at high risk for ADR (elderly)?
<50 ml/min
how many comorbid disorders place elderly at risk for ADR?
> 6
how many meds place elderly at risk for ADR?
> 9 meds
how many daily doses place elderly at risk for ADR?
> 12 daily doses
previous adverse drug effect place elderly at risk for what?
ADR
what does STOPP stand for?
screening tool of older persons’ potentially inappropriate
what does START stand for?
screening tool to alert doctors to right reatment
what is the BBB a barrier to?
drug distribution
what blocks many types of drugs from getting into or getting access to the brain?
BBB
what other three things does BBB block?
toxins, pathogens (viruses and bacteria), some inflammatory cells
what provides protection for the CNS?
BBB
what does the BBB help transport? (two things)
nutrients and oxygen
what does the BBB help get rid of? (two things)
metabolites and waste products (from cellular function within the brain)
what two types of drugs are able to cross the BBB?
highly lipid soluble and non-ionized
what does the fetal placental barrier operate by?
simple diffusion
what must drugs be to cross fetal placental barrier?
lipid soluble
is the fetal placental barrier a perfect barrier?
no
why is the fetal placental barrier not perfect?
many substances a mother takes into her body will reach the fetus
what three things does fetal placental barrier help transport to fetus?
nutrients, oxygen, fluids
what two things does fetal placental barrier remove?
waste and CO2
does fetal placental barrier protect against infection?
yes
what does IV med administration take effect?
immediate
does IV administration bypass first pass?
yes
does IM bypass first pass?
yes
does SQ bypass first pass?
yes
which is faster- SL or PO?
SL
can SL bypass first pass?
yes
does topical admin produce systemic absorption?
yes
is inhalation systemic?
yes
what isoenzyme? Convert a drug that is less lipid soluble to more water soluble to be excreted
CYP450
where is CYP450 located?
liver
what phase of biotransformation? Oxidation metabolites are still able to act in the body (bioactive)
phase 1
what phase of biotransformation? Conjugation of the drug molecule metabolites are not able to act in the body are water soluble
phase 2
if two drugs are metabolized by the same metabolic pathway they will what?
compete for the site of metabolism
term? Adverse effects that appear unpredictably
idiosyncratic ADRs
which hypersensitivity? Results from production of IgE after exposure to an antigen (most severe)
type 1
which hypersensitivity? Allergic reaction provoked by re-exposure to a specific type of antigen referred to as allergen
type 1
which hypersensitivity? Urticaria, wheezing, rhinitis, anaphylaxis
type 1
which hypersensitivity? Occurs when drug binds to cells and is recognized by an antibody
type 2
which two antibodies are involved in type 2 hypersensitivity?
IgG and IgM
which hypersensitivity? Complement and cytotoxic T cells are activated
type 2
which hypersensitivity is rare?
type 2
which hypersensitivity? ABO blood incompatibility
type 2
which hypersensitivity? Occurs when antibodies (IgG and IgM) are formed against soluble antigens
type 3
which hypersensitivity? Antigen-antibody complexes are deposited in tissues like joints and lungs
type 3
which hypersensitivity? Reaction takes hours, days, or weeks to develop
type 3
which hypersensitivity? Causes serum sickness
type 3
which hypersensitivity? Ceclor
type 3
what antibodies are involved in type 3 hypersensitivity?
IgG and IgM
which hypersensitivity? Cytotoxic t cells are activated, cell mediated
type 4
which hypersensitivity? Poison ivy and latex
type 4
which hypersensitivity? Contact dermatitis
type 4
which hypersensitivity? Repeated exposure to drugs causes a cytokine storm
type 4
which hypersensitivity? Delayed-type hypersensitivity
type 4
which hypersensitivity? Rash
type 4
term? Drugs dissolve and cross the cell membrane following concentration gradient
passive diffusion
term? Moving passively with no energy required from a higher to lower concentration area until equilibrium achieved
passive diffusion
passive diffusion moves from an area of WHAT to WHAT concentration?
higher to lower
what type of molecules move by passive diffusion?
small, mainly lipid soluble, uncharged
small or large molecules- passive diffusion?
small
charged or uncharged molecules- passive diffusion?
uncharged
ionized or unionized- passive diffusion?
unionized
stomach- acidic or basic?
acidic
intestine- acidic or basic?
basic
term? Moves against concentration gradient; requires energy
active transport
another term for active transport?
carrier mediated transport
carrier mediated transport is another term for what?
active transport
term? Involves specific membrane transport proteins that carrier the drug across the membrane
active transport
what carries drugs across the membrane in active transport?
specific membrane transport proteins
does active transport cross entire cell membrane?
yes
does active transport require energy?
yes
most drugs are weak WHATs or WHATs?
acids or bases
term? Characteristic of a drug- the ph at which half the molecules are ionized and the other half is unionized
pka
henderson-hasselbach equation is involved with what?
pka
the ionization of drugs may markedly reduce their ability to what?
permeate membranes
what two factors determine degree of ionization of drugs?
ph and pka
drus that are weak WHAT are uncharged in an acidic environment?
weak acids
drugs that are WHAT are uncharged in a basic environment?
basic
term? Transfer of a drug from its site of administration to the blood stream
absorption
most absorption occurs through what?
passive diffusion
what favors charged species?
solubility
solubility favors what?
charged species
permeability favors what?
neutral species
some molecules have what two things to facilitate movement from the lumen into circulation?
exchange proteins and channels
what is the fastest route of absorption?
inhalation
the GIT is lined with what?
epithelial cells
drugs must permeate through what cells to be absorbed into the circulatory system?
GI epithelial cells
does IV medication need absorption?
no- direct to circulation
which has greater predictability of absorption? IM/SQ or PO
IM/SQ
what is drug property is reduced by liver metabolism of drugs?
bioavilability
term? Before the drug reaches the systemic circulation significant portion of the drug can be metabolized by the liver
first pass
first pass causes what to be decreased?
concentration of drug in systemic circulation
what is the pathway of first pass?
portal vein
does rectal route bypass FPE?
yes
does buccal route bypass FPE?
yes
does SL route bypass FPE?
yes
term? A measure of an amount of administered dose of a drug that actually reaches the systemic circulation in unchanged form
bioavilability
what is the bioavailability of IV administration?
1
why is oral drug bioavailability lower?
incomplete absorption; first pass metabolism
term? Passage of a drug from the circulation to the tissue and its site of action
distribution
what are the six factors that affect drug distribution?
(1) lipid solubility (2) drug ph (pka) (3) blood flow to tissues (4) plasma protein binding (5) specialized barriers (6) disease state
what are these? (1) lipid solubility (2) drug ph (pka) (3) blood flow to tissues (4) plasma protein binding (5) specialized barriers (6) disease state
factors that affect distribution
term? Hypothetical volume of fluid into which the drug is distributed
volume of distribution
what are the functional water compartments in the body?
intracellular fluid, extracellular fluid, plasma, interstitial volume ?
what is the only form of a drug that is pharmacologically active?
free/unbound drug
what is the only form of a drug able to cross membranes?
free/unbound drug
what happens when a drug travels through the body and comes in contaact with a protein?
can remain free or bind to the protein
the portion of a drug that is bound to a protein is what?
inactive
the portion of a drug that is not bound to a protein is what?
active (free)
a drug is said to be highly protein-bound if more than what percent of the drug is bound to protein?
0.8
what is the primary serum protein responsible for drug binding?
albumin
albumin has a strong affininty for what?
weak acids
drugs that are minimally bound to protein penetrate the tissue BETTER/WORSE than drugs who are highly bound?
better
drugs that are minimally bound to protein are excreted FASTER/SLOWER?
faster
if drugs are bound to protein they stay in the plasma to get where they need to go but cannot bind to receptor until WHAT?
unbound
low albumin= more WHAT?
free drug
low albumin = more/less free drug?
more
low albumin= more free drug= more what?
adverse effects
two drugs that are highly protein bound do what?
compete
when two highly protein bound drugs compete what happens?
can cause increase concentration of the free drug
example of highly protein bound competing and increasing free drug concentration?
aspirin and sulfa
to penetrate the CNS, drugs need to penetrate what?
BBB
what kind of drugs penetrate the BBB?
only highly lipid-soluble ionized drugs are going to penetrate
term? Highly selectively permeable barrier that separates the circulating blood from the brain and extracellular fluid on the CNS
BBB
what kind of cells form the BBB?
brain endothelial cells
what connects brain endothelial cells in BBB?
tight junctions
in BBB- brain endothelial cells are connected by tight junctions with extremely high what?
electrical resistivity
water, some gases, lipid soluble molecules move across BBB by what process?
passive diffusion
BBB allows passage of what three things by passive diffusion?
water, some gases, lipid soluble molecules
glucose and amino acids, crucial to neuro function, move across BBB by what?
selective transport molecules
is the placental membrane a complete barrier?
no (incomplete barrier)
how do molecules move across placental membrane?
simple diffusion
what type of molecules move across placental membrane?
lipid soluble
term? Impedes certain molecules although allows most fat soluble chemicals to cross
placental membrane
what are the two properties of drugs that tend to make it unlikely to cross placental membrane?
drugs that are more water soluble and have a higher molecular weight
drugs that are more water soluble and have a higher molecular weight DO/DO NOT as readily cross placental membrane?
do not
if a drug binds to a large molecule like blood protein/albumin it is MORE/LESS likely to contact fetus?
less likely
term? Lipid bilayer, semipermeable
cell membrane
pure lipid bilayers are generally permeable only to what?
small and uncharged solutes
ionic molecules are charged/uncharged?
charged
whether or not a molecule is ionized will affect its what?
absorption
term? Irreversible biochemical transformation of drug into metabolites to increase excretion from body via kidney
metabolism
where does metabolism mainly occur?
liver
metabolites are usually more or less ionized?
more ionized
metabolites are usually more or less lipid soluble?
less lipid soluble
why are metabolites not absorbed by renal tubule?
less lipid soluble
non-synthetic reactions, which phase of metabolism?
phase 1
oxidation- which phase of metabolism?
phase 1
what is the most important metabolizing reaction?
oxidation
term? Adds oxygen or a charged radical/involves cytochrome P450 isoenzymes
oxidation
reduction- which phase of metabolism?
phase 1
hydrolysis- which phase of metabolism?
phase 1
metabolite may be active or inactive- which phase of metabolism?
phase 1
metabolies are only inactive- which phase of metabolism?
phase 2
synthetic reactions- which phase of metabolism?
phase 2
glucuronidation- which phase of metabolism?
phase 2
what enzyme- convert drugs to more water soluble forms?
CYP450
what enzyme? The major enzymes involved in drug metabolism
CYP450
what percentage of total metabolism does CYP450 account for?
0.75
grapefruit is an inducer or inhibitor of CYP450?
inhibitor
grapefruit will increase/decrease metabolism of drugs?
decrease
where is CYP450 primarily located within liver cells?
endoplasmic reticulum
aside from liver, what other organs house CYP450?
kidney and intestine
what are the 3 CYP enzymes that carry out largest number (50%) of biotransformation?
3A, 4, and 5
term? Some drugs can induce or stimulate the production of one or more isoforms of the enzymes to increase drug metabolism or decrease amount of one of the drugs
enzyme induction
what is the result of enzyme induction?
decrease the therapeutic effect of one of the other drugs because the enzymes have been induced
term? Drugs will inhibit the production of CYP enzymes and decrease drug metabolism to the effect is increased plasma concentration of concurrently used drugs
enzyme inhibition
enzyme inhibition- what kind of interaction?
drug to drug interaction
interacting CYP enzymes equates to what?
enzyme inhibition
five factors that affect metabolism?
age (small kids, elderly), genetics, gender, diet and environmental factors, disease state
acetylation is involving what metabolism factor?
genetics
term? Elimination of drugs from the body unchanged or as a metabolite
excretion
what is the most common organ of elimination?
kidney
via what route does elimination occur?
urine
what is the primary organ of excretion?
kidney
term? To produce drug metabolites that are more water soluble and more easily removed by the kidneys
excretion
what lab used to monitor renal function in the clinical setting?
serum creatinine
variability of excretion lies in the WHAT of the patient?
renal function
patients with poor renal function have LOWER/HIGHER levels of drugs secondary to decreased excretion of metabolites?
higher
what is the hepatic route of excretion?
bile
what is the mechanism of lung excretion?
exhalation
does excretion occur via breast milk?
yes
does excretion occur via skin?
yes
what type of compounds can be easily excreted?
hydrophilic compounds
why are hydrophilic compounds easily excreted?
body keeps from being reabsorbed
what is the most common method of excretion?
renal excretion
are protein bound drugs filtered in excretion?
no
what is normal GFR?
120
what two things does GFR depend on?
plasma protein binding and renal blood flow
process? Transported by liver cells from blood to bile then enter GIT and excreted through feces
biliary excretion
enterohepatic reabsorption is part of what type of excretion?
biliary excretion
term? Action of a drug on the body
pharmacodynamics
what receptors do ligand-gated ion channels act on?
cholinergic nicotinic
cholinergic nicotinic receptors interact with what channels?
ligand gated ion channels
what receptors do g-protein-coupled receptors act on?
alpha and beta adrenoreceptors
alpha and beta adrenoreceptors act on what receptor?
g protein coupled receptor
what receptors interact with enzyme-linked receptors?
insulin receptors
insulin receptors interact with what receptors?
enzyme-linked receptors
intracellular receptors interact with what receptors?
steroid receptors
steroid receptors interact with what receptors?
intracellular receptors
term? The ability of the drug to bind to the receptor
affinity
term? How well a drug binds to its receptor
affinity
definition of affinity?
the ability of a drug to bind to the receptor (how well)
term? The ability of a drug to produce a pharmacological response once the drug attaches to the receptor
efficacy
another term for efficacy?
intrinsic activity
definition of efficacy?
ability of the drug to produce a pharmacological response once the drug attaches to the receptor
alternative definition of efficacy?
how well the drug works to exert its therapeutic effect
term? How well a drug exerts its therapeutic effect
efficacy
term? Drug that has affinity plus intrinsic activity
agonist
term? Binds to a receptor and produces a pharmacological response
agonist
term? Binds to receptor and will do something
agonist
term? Possess some intrinsic activity, but less than a full agonist
partial agonist
term? Measure of drug activity expressed in terms of the amount required to produce an effect
potency
term? Amount of drug required to produce an effect of given intensity
potency
term? The point in time on the drug concentration curve that indicates the first sign of therapeutic effect
onset of action
onset of action, definition?
the point in time on the drug concentration curve that indicates the first sign of therapeutic effect
first sign of therapeutic effect? Term?
onset of action
term? The point in time on the drug concentration curve that indicates the max therapeutic effect
peak action
peak action- definition?
maximal effect in the body
term? The length of time the drug shows any effect in the body
duration of action
term? Time between onset of action and metabolism of the drug
duration of action
term? Amount of drug needed in the body remains constant (five half lives)
steady state
how long is the steady state?
five half lives
term? The amount of drug going into the body is the amount of drug being eliminated
steady state
what is used to determine if a drug is in therapeuti range?
peak and trough
what is used to decide dosing schedule?
half life
term? The length of time for the concentration of the drug to decrease to half its starting concentration
half life
What is the term? What the drug does/action on the body
pharmacodynamics
What is the term? What the body does to the drug
pharmacokinetics
What is the term? Factors that affect prescribing- include bioavailability
pharmacokinetics
Term? Think Absorption, Distribution, Metabolism, Excretion
pharmacokinetics
ADME
Absorption, distribution, metabolism, excretion (pharmacokinetics)
Description of which route of absorption? Convenient, takes longer to reach blood stream, may be destroyed by stomach acid
oral
which route of absorption? May be destroyed by stomach acid
oral
Another term for IV administration route?
parenteral
which route of absorption? Faster than oral, more readily absorbed, avoids 1st pass effect
sublingual
route of absorption that avoids 1st pass effect?
sublingual
which route (absorption) faster than oral, absorbs directly through mucous membranes into blood stream?
rectal
which route (absorption) can be fast, like IV, but also unreliable?
inhalation
which route (absorption) must undergo absorption through injection site?
IM/SQ
which route (absorption), drugs cannot create action if they are not distributed in adequate concentrations?
IM/SQ
term? Creates equal amounts of un-iodized drug on both sides of the membrane, works best for small unbound, uncharged drugs?
passive diffusion
term? Creates equal amounts of un-iodized drug on both sides of the membrane
passive diffusion
passive diffusion works best on what drugs?
small, unbound, uncharged drugs
what works best on small, unbound, uncharged drugs?
passive diffusion
define plasma protein binding
drugs may compete for protein binring sites
two examples od drugs re: plasma protein binding?
coumadin, bactrim
hypoalbuminemia leads to what?
more free (unbound drug) in the blood stream
hypoalbuminemia leads to increased risk of what?
toxic effect
why does hypoalbuminemia have increased risk for toxic effect?
drug hanging in the bloodstream and not doing anything productive, less drug available to work in target tissues
term? Process in which drugs are transferred from inside the body to outside the body
excretion
what age group has less ability to excrete?
older adults
why do older adults have less ability to excrete?
decreased kidney function
slower excretion increases potential for what?
toxicity
what is the likely route of excretion of a volatile drug?
likely the lungs
where does excretion primarily take place?
kidneys
aside from kidneys, where are the three organs excretion also occurs?
liver, lungs, skin
what type of reaction is CYP 450?
oxidative
what can cause variation in CYP 450?
genetics
what drug? A nonspecific CYP 450 inducer that can induce the metabolism of drugs, like oral contraceptives, leading to therapeutic failure
rifampin
what type of drug is rifampin?
nonspecific CYP 450 inducer
what does rifampin induce?
metabolism of drugs
what enzyme? Drugs may compete for this enzyme, meaning one will not be metabolized?
CYP34A
term? Drug cannot be metabolized by enzymes properly; block or slow the enzyme
inhibitor
what does an inhibitor do?
block or slow the enzyme
what does an inducer do?
stimulate the enzyme
ter? Drug is metabolized too fast- make enzymes work better
inducer
what hormone? Decreases gastric tone and prolongs stomach emptying
progesterone
what are two effects of progesterone in pregnancy?
decreases gastric tone and prolongs stomach emptying
what special population? Hormones may occupy protein binding sites leading to more free drug in circulation
pregnancy
what kind of drugs pass through breast milk?
highly lipid soluble, low protein binding drugs
is drug metabolism changed in pregnancy?
no
what special population? Peak serum concentrations lower and delayed
elderly
what happens to peak serum concentrations in elderly?
lower and delayed
gastric acid increased or decreased in elderly?
decreased
drug absorption increased or decreased in elderly?
decreased
body water increased or decreased in elderly?
decreased
distribution of hydrophilic drugs increased or decreased in elderly?
decreased
why is there reduced distribution in elderly?
less albumin, less body mass, less plasma protein
why is there increased unbound active drug in elderly?
why is there slow metabolism in elderly?
what two changes to liver happen in the elderly?
what changes to the kidney happen in the elderly?
renal tubular secretion increased or decreased in elderly?
kidney size increased or decreased in elderly?
number of functioning nephrons increased or decreased in elderly?
increased fat stores in elderly lead to what?
what effect do increased fat stores have on volume distribution in elderly?
what increases volume distribution of lipophilic drugs in elderly?
first pass effect is increased or decreased in elderly?
why is 1st pass effect increased in elderly?
role of DEA?
schedule of drugs with no medical use?
two examples of schedule 1 drugs?
heroin and LSD are examples of which drug schedule?
what drugs have high potential for abuse and dependence?
refills and telephone orders permitted with schedule 2?
vicodin, oxycontin, adderall- what schedule?
what schedule- moderate potential for abuse and dependence?
scripts rewritten after 6 months for 5 refills- what schedule?
tylenol with codeine- what schedule?
ketamine- what schedule?
steroids- what schedule?
testosterone- what schedule?
tylenol with codeine, ketamine, steroids, testosterone? What schedule
what schedule- drugs with low potential for abuse and dependence?
xanax, clonazepam, valium, ativan- what schedule?
what schedule- xanax?
what schedule- valium?
what schedule, tramadol?
what schedule clonazepam?
what schedule- ativan?
what schedule- same as all prescrtipion drugs over the counter?
robitussin AC- what schedule?
lomotil- what schedule?
Lyrica- what schedule?
robitussin AC, lomotil, lyrica- what schedule?
type 1 reaction is mediated by what?
immediate type hypersensitivity, which type?
anaphylaxis- which type?
antibody-dependent cytotoxicity- which type?
heparin-induced thrombocytopenia- which type?
graft rejection- which type?
immune complex hypersensitivity- which type?
arthus reaction to tetanus vaccine- which type?
lupus- which type?
describe type 3 reaction?
describe type 2 reaction?
what do agonists do?
term? Receptor site stimulation?
term? Block receptor site stimulation?
what do antagonists do?
what do antagonists block?
which system? Releases acetylcholine and counterbalances sympathetic activity
which system? ACH activates muscarinic and nicotinic receptors
what are the two cholinergic receptors?
what two receptors does ACH activate?
parasympathetic nervous system is part of which system?
constricts pupils- which system?
stimulates salivation- which system?
decreases heart rate- which system?
decreases contractility- which system?
left off on page 3
