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Pharmacology 1
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Pharmacology
Undergraduate 1
09/20/2014

Additional Pharmacology Flashcards

 


 

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Term
what are the 3 branches of pharmacology
Definition
pharmacodynamics
pharmacokinetics
toxicology
Term
pharmacology
Definition
study of substances that interact with living systems through chemical processes, especially by biinding to regulatory molecules and activating or inhibiting normal body processes
Term
pharmacodynamics
Definition
drugs effect on the body
pharmacologic effect
clinical response
toxicity
therapeutic benefit
Term
pharmacokinetics
Definition
body's effects on drugs
drug administration (absorption)
blood, tissues and other extravascular sites
drug target site (distribution)
drug metabolism and excretion (elimination)
Term
toxicology
Definition
undesirable effects of a drug
Term
ibuprofen pharmacodynamics
Definition
non seroidal anti-inflammatory drug inhibition of the COX pathway which decreases production of inflammatory mediators biological response - decreased pain
Term
ibuprofen pharmacokinetics
Definition
PO - rapidly absorbed
Cmax - 1-2 hours
half life 1.5-2 hours
metabolized by liver
primarily excreted in urine
Term
generic name of Advil or Motrin
Definition
ibuprofen
Term
Drug
Definition
any substance that brings about a change in biologic function through its chemical actions
(ibuprofen, herbal medicines)
any chemical that affects a living process
Term
what chemical states are drugs in
Definition
solid
liquid
gas
Term
what are drugs made up of
Definition
organic compounds and inorganic elements
acids and bases
Term
what do drugs needs so they can easily be absorbed in the GI system
Definition
acids and bases
Term
what are the 4 different types of drugs
Definition
natural
synthetic
endogenous
exogenous
Term
natural drug
Definition
caffiene
nicotene
from a plant
Term
synthetic drug
Definition
made by a chemist
gravol
Term
endogenous drug
Definition
made within the body
acetylcholine, hormones
Term
exogenous drug
Definition
made outside the body
drugs
Term
what do drugs generally act on
Definition
receptors altering physiological function
Term
what are drug receptor interactions based on
Definition
physiochemical properties
(structural and chemical)
lock and key model
Term
enantiomer
Definition
mirror image stereoisomers that are non-superposable (not identical)
Term
diastereomer
Definition
when two or more stereoismoers of a compound have different configuration at one or more (but not all) of the equivalent seterocenters
not mirror images of each other
Term
racemic mixture
Definition
equal amount of left- and right-handed enantiomers of a chiral molecule
Term
what is the danger of isomers and racemic mixtures
Definition
sometimes one isomer is more active than the other, sometimes more toxic
thalidamide
Term
what are chemical interactions of drugs with molecules important for
Definition
pH dependence - causes the drug to become ionized
protein binding - keeps drugs going where they need to go
receptor interactions (binding) - drug only causes an effect when it properly interacts
Term
what type of molecular interactions are important in drug-receptor associations
Definition
weaker intermolecular bonds:
hydrogen bonds
vanderwalls
ionic bond

**covalent bonds are unbreakable
Term
how does the tertiary structure influence drug receptor binding
Definition
shape/ inherent structure - lock and key
hydrophobicity (where in the receptor this occurs)
orientation and type of binding with a receptor - special links must be formed
Term
affinity equation
Definition
D-R = sum of interactions
Term
What determines the relationship between drug dose and pharmacological effect
Definition
receptors - high doses, more drugs, binds to more receptors, larger pharmacological effect (beneficial / toxic)
Term
In drug receptor binding, receptors are responsible for
Definition
selectivity of drug action - some are specific and some are broad
Term
receptor definition
Definition
a protein molecule that a drug can interact with
causes some conformational change to alter its activity
Term
where are receptors located
Definition
found on the plasma membrane of a cell - biological changes
found intracellular on nuclear proteins - interact with transcription factors (slow acting)
Term
what type of binding to drugs to with target molecules
Definition
selective binding
but sometimes they can cause effects where it's not planned (negative side effects)
Term
affinity
Definition
favourability of drug-receptor interaction
Term
EC 50
Definition
[drug] required to produce 50% of the maximum response
measures potency
Term
Kd
Definition
dissociation constant
[drug] required to produce 50% of drug-receptor binding
measure of affinity
Term
what 3 things does the binding of drugs to receptors result in?
Definition
conformational changes in receptor
transduction of the signal via alterations in cytosolic metabolism (signal is passed down)
changes in cell function/ gene transcription
Term
hat is conformational selection
Definition
receptors move from inactive to active spontaneously
increase ligand increases level of receptors in active state
Term
agonist
Definition
molecule that binds to a receptor and stabilizes the receptor conformation
activates the receptor to cause a response
Term
antagonist
Definition
binds to the active site on the receptor or to an allosteric site to prevent the agonist biing and stabilization of the R-L signaling complex
blocker/ inhibitor
blocks receptor activation
Term
inverse agonist
Definition
stabilizes the inactive conformation of a receptor if there is baseline activity
Term
full agonist
Definition
increases response
Term
partial agonist
Definition
causes partial response
Term
antagonist
Definition
brings it back to base line
Term
inverse agonist
Definition
inhibits a process that is already happening
Term
what happens to the concentration of a full agonist when the concentration of a partial agonist increases
Definition
concentration of partial agonist decreases, decreasing body's response to the drug
Term
type of antagonists
Definition
competitive and non competitive
Term
competitive antagonist
Definition
reversible
interacts with same binding site as agonist
increasing [agonist] displaces antagonist
Term
non-competitive antagonist
Definition
non-reversible
binds to same site as agonist with covalent bond
binds to allosteric site
Term
what do drugs without receptors do
Definition
alter physiological state - antacids
alter action of endogenous modulatos
Term
what do antacids do
Definition
neutralize stomach acid
TUMS
Term
herceptin
Definition
trastuzumab
monolonal antibodies taht bind to HER2
this prevents EGF from binding to the EGF receptor
HER2 is up-regulated in some breast cancers
Term
low [non-competitive antagonists] will decrease _______ but not effect ______
Definition
potency
efficacy
Term
high [non-competitive antagontists] all spare receptors will be bound and ______ will be effected
Definition
efficacy
Term
quantal dose-response curves
Definition
used for determining the amount of the population which a dose will respond to with respect to efficacy
can also be used for toxicology analysis with toxicity and lethality
ED50
Term
ED50
Definition
effective dose for 50% of the population
Term
TD50
Definition
toxic dose for 50% of the population
Term
LD50
Definition
lethal dose for 50% of the population
Term
what is the difference between side effects and adverse effects
Definition
side effects - alternative effects of drug; can be useful in some cases
adverse effects - toxic or harmful effects
Term
on target adverse effects intended tissue
Definition
dose too high
chronic activation or inhibition effects
Term
off target adverse effects intended tissue
Definition
incorrect receptor is activated/ inhibited
Term
on target adverse effects unintended tissue
Definition
correct receptor, incorrect tissue
dose too high
chronic activation or inhibition effects
Term
off target adverse effects unintended tissue
Definition
incorrect receptor is activated/ inhibited
Term
therapeutic window
Definition
dose that provides therapeutic efficacy while remaining within safe limits
Term
therapeutic index
Definition
TD50/ED50
Term
the larger the therapeutic index the _____ the drug the smaller the TI the ______ a drug is
Definition
safer
less safe (increase monitoring)
Term
signal transduction cascade
Definition
receptor activation by ligands
coupling to intracellular proteins
generation of second messengers
enzme regulation by phosphorylation
changes in cell activity and gene expression
Term
ligand-gated ion channels
Definition
ionotropic receptors
fast synaptic transmission in neurons
ligand binding occur on a millisecond timescale
can be composed of 3-5 subunits around a central aqueous channel
Term
G- protein coupled receptors
Definition
work in sec to min
7 transmembrane serpentine structure
ligand binds to extra-cellular side of receptor
receptor/ligand complex associates with a G protein
interactions with the G protein stabilize the active confirmation of the receptor and allow regulation of effector molecules
Term
Gi alpha
Definition
inhibits
Term
Gs alpha
Definition
stimulates
Term
Gq alpha
Definition
increase DAG
IP3
Term
G12 14 alpha
Definition
activates Rho
Term
G beta
Definition
ion channels
PI3K
phospholipases
adenylylayclases
receptor kinases
Term
downregulation
Definition
process by which a cell decreases teh number of a cellular component, such as RNA or protein in response to external variable
(negative feedback mechanism)
Term
desensitization
Definition
loss of responsiveness to the continuing or increasing dose of a drug
Term
down regulation vs desensitization
Definition
Desensitization is where the receptors become phosphorylated and therefore inactive but remain on the plasma membrane.

Down regulation is any scenario where there are less numbers of receptors on the plasma membrane. So this can include internalization.
Term
enzyme linked receptors
Definition
work on second to min
single polypeptide chains with extracellular ligand binding domain, a transmembrane domain and an intracellular kinase domain
cross linking of the receptors is essential for activation
downstream signaling occurs through phosphorylation and dephosphorylation of substrate proteins
Term
intracellular receptors
Definition
hours to days
change transcription - DNA and RNA slow acting
ligands taht are lipophillic or very small diffuse through the cellular membrane
ligands can also be transported via facilitated diffusion or active transport
ligands bind to receptors
receptors can then act to increase or decrease transcription of a gene or alter rate of transcription
Term
ACE inhibitors
Definition
decreases blood pressure
Term
COX inhibitors
Definition
decrease inflammation
Term
what are the two types of administration of drugs
Definition
systemic
local
Term
systemic administration
Definition
enteral (PO)
parenteral:
sucutaneous (sc)
intramuscular (im)
intravenous (iv)
Term
local administration
Definition
topical
inhaled
dermal
ocular
Term
po
Definition
enteral
through the mouth, stomach, GI system
Term
sc
Definition
parenteral
subcutaneous under the skin
Term
IM
Definition
parenteral into the muscle
Term
iv
Definition
parenteral
into the vein
Term
what is the most common route of administration
Definition
oral - it's easy but it's less effective
Term
what are the limitations to oral administration
Definition
acid liable (acid can break down drug)
can cause GI irritation
Metabolism - first pass effect (concentration of a drug is decreased due to metabolism upon administration)
Term
what is first pass metabolism
Definition
the concentration of the drug is reduced before it reaches systemic circulation during the process of absorption in the liver or gut wall
Term
how does IV administration avoid first pass metabolism
Definition
drug enters directly into the system circulation and has direct access to the rest of the body
IV drugs are not broken by by enterocytes or liver
Term
what are the limitations of parenteral administration
Definition
professional administration
needs sterile preparation
Term
what are the benefits of parenteral administration
Definition
100% bioavailability
Term
example of a drug that uses transdermal administration
Definition
nicotine patch
Term
example of a drug that uses transmucousal administration
Definition
buccal (nitroglycerine)
Term
pros of oral administration
Definition
easy
preferred by patients
slow release - available to extend duration of action
drugs can be formulated to protect them from digestive enzymes and acids etc.
Term
cons of oral administration
Definition
unsuitable in patients who are uncooperative,
nil by mouth patients
patients who vomit profusely or have ileus
absorbed slowly
unpredictable absorption due to degradation by stomach acid and enzymes
Term
pros of rectal administration
Definition
good absoroption - avoid hepatic first pass metablism
Term
cons of rectal administration
Definition
not suitable after recatal or anal surgery
some patients dislike suppositories
Term
pros of subcutaneous or intramuscular administration
Definition
good absorption
onset is more rapid
can have very long duration depending on the formulation
Term
cons of subcutaneous or intramuscular administration
Definition
absorption may still be unpredictable if peripheries are poorly perfused
injections hurt, cause bruises and frighten children and needle phobics
Term
pros of IV administration
Definition
dependable and reproducible effects
does can be accurately titrated against response
Term
cons of IV administration
Definition
requires a functioning cannula
more expensive and labour intensive
cannulation is distressing
cannulae are prone to infection
IV injection of drugs may cuase local reactions
Term
pros of topical administration
Definition
easy
non-invasive
high levels of patient satisfaction
Term
cons of topical administration
Definition
most drugs have a high molecular weight and are poorly lipid soluble,
most drugs cannot be absorbed via skin or mucous membranes
very slow absorption
Term
pros of inhaled administration
Definition
very rapid absorption due to the huge surface area of the respiratory endothelium
bronchodilators and inhaled steroids can be targeted to lungs with low levels of systemic absorption
Term
cons of inhaled administration
Definition
bioavailabiliy depends on patient's inhaler technique and size of drug particles generated by the delivery technique
Term
what are the physiological barriers of absorption
Definition
epithelial lining
mucus membranes
blood -brain barrier
Term
what are the biological barriers of absorption
Definition
lipid bilayers
Term
what factors affect physiological oral drug absorption
Definition
GI motility
Metabolism
changes in pH of GI tract
Term
how does GI motility affect oral drug absorption
Definition
decreased stomach emptying slows onset or rate of drug absorption
can be decreased by food, disease or drugs
Term
how does metabolism affect oral drug absorption
Definition
enzymes in the intestinal cells
first pass effect
Term
how do changes in the pH of GI affect administration
Definition
affects ionization of acid and base drugs
can be altered by food, diseases and drugs
Term
what are physiochemical factors that affect oral drug absorption
Definition
concentration gradients across membranes
size
polarity
ionization
Term
teratogen
Definition
any agent that can disturb the development of an embryo or fetus
birth defect
halt pregnancy
Term
thalidomide
Definition
treatment for sleep distrubances and nausea in pregnant women
Term
what factors need to be considered for drugs during pregnancy
Definition
physiochemical properties of teh drug
rate and amount of drug reaching fetus
distribution of the drug in fetal tissues
duration of fetal exposure
stage of fetal development during drug exposure
Term
all or none period
Definition
conception to day 17
teratogenic exposure often causes miscarrage
Term
embryonic period
Definition
days 18-60
exposure causes ireparable damage and significant anatomical deformities
Term
fetal phase
Definition
>60 days
exposure typically causes organ dysfunction
developmental and behavioural problems
Term
examples of drug category X
Definition
folate metabolism inhibitors ACE inhibitors
Term
methotrexate
Definition
folate metabolism inhibitors
CNS defects, craniofacial anomalies, mental retardation
Term
ramipril
Definition
ACE inhibitor
fetal renal and cardiovascular damage
Term
drugs considered safe in pregnancy
Definition
diphenhydramine
penicillin
heparin
insulin
topical drugs
Term
diphenhydramine
Definition
antihistamine
Term
penicillin
Definition
antibiotic
Term
heparin
Definition
anticoagulant
Term
insulin
Definition
antihyperglycemic
Term
which drug tend to cause withdrawl symptoms after birth (development of dependence)
Definition
opioids
Term
acetaminophen
Definition
non-antiinflammatory analgesic
category B
compatible in breast feeding
Term
high doses and long term use during pregnancy of this drug causes hepatorenal toxicity in the fetus
Definition
acetaminophen
Term
codeine
Definition
opioid analgesic
pregnancy category C
long term use/ high dose - category D
risk of dependence and withdrawal after birth
compatible in breastfeeding - must monitor infant
Term
ibuprofen
Definition
non -steroidal antiinflammatory analgesic
category D
risk of hemorrhage, teratogenic effects
highest risk in 1st and 3rd trimester
not recommended during breast feeding - interfere with platelet function
Term
what is phase 1 of clinical trials
Definition
is it safe
pharmacokinetics
20-100 subjects
young adult, male, average build
no underlying disease conditions
monitor side effects
adjust dosages of other propulations
Term
how does renal failure alter the PK of many drugs
Definition
decreases clearance and elimination
Term
how does obesity/ anorexia alter the PK of many drugs
Definition
unpredictable volume of distribution
Term
which is more accurate adjustments based on age or weight or body surface
Definition
body surface
Term
describe the normal GI function of elderly people and neonates
Definition
irregular and may be slow
Term
how is absorption altered with oral administration in different populations
Definition
nutrition and other drugs can influence absorption (antacids and laxatives)
diarrhea can decrease the amount of drug absorbed
Term
how is absorption altered with subcutaneous administration
Definition
depends on blood flow to/from site of injection
Term
premature infant considerations with absorption (IM or subcu administration)
Definition
little muscle mass and low body fat, absorption may be altered
Term
obesity considerations with absorption (IM or subcu admin)
Definition
high adipose can affect absorption from site of injection
Term
geriatric considerations with absorption (IM or subcu admin)
Definition
reduced muscle mass may alter absorption of drug
Term
in comparison to an average adult neonates and infants body make up is
Definition
higher in body water %
premature babies have lower body fat%
Term
in comparison to an average adult, geriatrics
Definition
have less body water% and higher body fat%
Term
what enzymes metabolize drugs in the liver
Definition
CYP450 enzymes
conjugating enzymes (glucuronide enzymes)
Term
in terms of metabolism what % of the capacity of the liver enzymes of an adult liver do neonates have
Definition
50-70%
slowed metabolism = slowed elimination
Term
how does the half life of acetaminophen in young children compare to adults
Definition
longer half life but the dosing interval is often the same
neonates 2.2 -5 hours
adults 0.9-2.2 hours
Term
how is elimination affected in neonates and infants
Definition
slower glomerular filtration rate 60-70% less than adults
slower clearance of drug from teh body
by 6-12 months of age, rate is similar to adults
young children - faster filtration rate = faster clearance
Term
how is elimination affected in geriatrics
Definition
renal impairment or disease = slower clearance
observed in about 2/3 of the geriatric population
Term
what are three major organ dysfunctions in geriatrics that affect PK
Definition
glomerular filtration - greatest effect on altered PK in geriatrics
cardiac index - impacts renal function (decreases blood flow)
max breathing capacity - greater sensitivity to respiratory depression (decreases delivery of inhaled drugs)
Term
what are some special considerations for children before administering drugs
Definition
adverse effects - children may not be able to communicate side effects
many drugs are not studied in children
interference with other systems (growth hormones, development of bones and teeth)
Term
which polymorphism leads to clinical difference in response to drugs
Definition
CYP2D6
Term
what does CYP2D6 do
Definition
liver enzyme
metabolizes antidepressants, antipsychotics and beta blockers
activates pro-drugs(codine to morphine)
Term
extensive metabolizers
Definition
CYP2D6*1
majority of population
Term
ultra rapid metabolizers
Definition
CYP2D6*2
rapid removal of drugs metabolized by CYP2D6
Term
poor metabolizers
Definition
CYP2D6*3
very slow removal of drugs metabolized by CYP2D6
10% of caucasian population
2% of asian population
little to no expression of functional enzyme
Term
pain
Definition
a basic bodily sensation that is induced by a noxious stimulus
characterized by physical discomfort
leads to evasive action
very subjective
Term
what causes pain
Definition
painful stimulus sends signal via action potential to the brain
brain returns signals that generate the response
Term
adaptive pain
Definition
painful stimulus with a physiological purpose
nociceptive
inflammatory
Term
maladaptive pain
Definition
painful stimulus has no physiological responseneuropathic
choronic/ excessive inflammation
Term
after surgery ____% of patietns are left experiencing moderate-severe pain, only ____% of ordered pain medication is given
Definition
50%
30%
Term
____/____ canadian adults suffer from chronic pain
Definition
1/5
Term
__-___% of children experience recurrent or chronic pain
Definition
15-30%
Term
two methods of pain management
Definition
opioid analgesics
non-opioid analgesics
Term
non-opioid analgesics
Definition
acetaminophen
antiinflammatory agents (steroids, non-steroidal antiinflammatory agents NSAIDS)
Term
1-3 on the pain scale - pharmacologic management?
Definition
ibuprofen
acetaminophen
Term
4-6 on the pain scale (moderate) - pharmacologic management?
Definition
codeine, oxycodone
+/- acetaminophen or ibuprofen
Term
7-10 on the pain scale (sever)- pharmacologic management?
Definition
oxycodone, morphine, fentanyl
Term
opioid receptors
Definition
mu-opioid receptor
delda- opioid receptor
kappa-opioid receptor
Term
what is the main opioid receptor involved in analgesic effects and side effects
Definition
mu0opioid receptor
target for clinically used opioids
Term
what is the mode of action for opioids
Definition
GPCR
Gi coupled receptor
mu receptor closes calcium channels and opens potassium channels
reduced neuronal transmission of pain signal
Term
what detects the pain stimulus in the opioid MOA to inhibit pain signal transmmission
Definition
detected by the peripheral neuron
Term
what are some side effects/adverse effects of opioids in the CNS
Definition
sedation
respiratory depression
cough supression
nausea and vomiting
Term
what are some side effects/adverse effects of opioids in the cardiac
Definition
hypotensive effect
additive with antihypertensives
Term
what are some side effects/adverse effects of opioids in the GI tract
Definition
decrease motility leading to constipation
Term
how is the bio availability in opioids
Definition
varied but 100% via IV
Term
how is the distribution in opioids
Definition
high distribution to tissue with high blood perfusion (brain, liver, lungs, kidneys)
most are very lipophilic, accumulate in adipose tissue
Term
how is the metabolism of opioids completed
Definition
converted to polar metabolites (glucuronides) - prolongs duration
CYP2D6 metabolism to more potent compounds (codeine to morphine)
Term
morphine 6 glucuronide
Definition
10% of morphine dose metabolizes to M6G
which is 4-6x more potent than morphine
Term
how are opioids eliminated
Definition
kidneys to urine
so renal dysfunction must be considered
Term
what are some drug-drug interactions associated with opioids
Definition
many
consider effects of opioids and avoid drugs with similar effects or similar metabolic pathways
Term
what are the most common clinically used opioids
Definition
morphine
codeine
oxycodone
fentanyl
Term
morphine
Definition
full agonist at mu receptor
available in many formulations
oral:immediate, sustained, and controlled release
parenteral: SC 2D6 or IV
Term
codeine
Definition
partial agonist @ mu-receptor
metabolized to morphine by CYP2D6
Term
oxycodone
Definition
full agonist at mu-receptor
more potent than morphine
inactivates metabolites via CYP2D6
Term
oxycontin
Definition
oxycodone
crushed to give very high doses of immediate release oxycodone
problems with abuse
Term
oxyNeo
Definition
new controlled release fomulation in canada
very difficult to crush
does not dissolve easily so it can't be injected
Term
codeine or oxycodone can be used in combination with which analgesic
Definition
acetaminophen, better analgesia at lower doses
two different Mechanism of action
Term
what is added to combinations of analgesics to reduce abuse
Definition
caffeine
excitatory effects of caffeine counteract sedative effects of opioid
Term
what is an example of an opioid with caffeine
Definition
tylenol 1
Term
fentanyl
Definition
full agonist at mu receptor
very high potency
only indicated in severe chronic pain (cancer)
Term
how is fentanyl usually administered
Definition
transdermal patch formulation
continuous controlled release 12-100 micrograms/ hr over 72 hour release
Term
how does fentanyl compare to morphine
Definition
>60mg/day morphine
Term
how does fentanyl affect opioid-naive individuals
Definition
analgesia ! 1-2 ng/ mL blood
surgical anasthesisa and profound respiratory depression @10-20ng/mL blood
Term
acetominophen
Definition
tylenol
reduces fever and pain
maximum dose- children: <65mg/kg/24 hours ; adults: <4g/24 hours
Term
ADME of acetaminophen
Definition
A - orally: high bioavailabiliy - onset 1 hour duration 1-4 hours, half life 2 hours
metabolism and excretion - hepatic and renal
metabolized to toxic metabolite, effective excretion is essential to prevent fatal hepatotoxicity
Term
what increases production of toxic metabolite when taken with acetaminophen
Definition
alcohol
Term
what is the MOA of acetaminophen
Definition
unclear
not anit-inflammatory
involves reduciton of prostaglandins in CNS
Term
what are 4 theoretical drug targets or pathways for acetaminophen
Definition
inhibition of COX 1 and 2 (CNS)
COX3 enzyme only expressed in CNS
activates 5HT3 receptors
active metabolite increases endocannavinoid production (antiinflammatory effects)
Term
How do cannavinoids aid pain management
Definition
GPCRs - Gi coupled, evidence of heterodimerization with opioid receptors
has significant analgesic and antiinflammatory effects
typically granted after other agents have failed or have adverse effects
Term
2 types of antiinflammatory agents
Definition
steroidal
non steroidal
Term
steroidal antiinflammatory agents
Definition
corticosteroids - mimic actions of endogenously released cortisol
used to treat inflammatory disease or cause immunosuppression
Term
non-steroidal antiinflammatory agents (NSAID)
Definition
interfere with the production of inflammatory mediators
typically used to treat inflammatory pain
Term
what do corticosteroids do
Definition
cause cahgnes in gene transcription, affecting metabolism, fluid electrolyte balance etc.
Term
what are the therapeutic effects of corticosteroids
Definition
inhibit production of Prostaglandins and Leukokins
Term
prednisone
Definition
corticosteroid
acute use of low dose to reduce or prevent post-operative pain and inflammation
Term
fluticasone
Definition
corticosteroid
topical/ local
reduce inflammation related to asthma, dermatitis and allergies
Term
dexamethasone
Definition
useful in organ transplant, cancer chemotherapy
chronic use of systemic high dose causes immunosupression
Term
how do dexamethasone and prednisone compare to cortisol
Definition
dexamethasone 30x > prednisone 4x > cortisol
Term
what are the adverse effects of corticosteroid therapy
Definition
immunosupression
growth retardation
impaired wound healing
acute adrenal crisis (with abrupt removal of drug)
osteoporosis
Term
how can you avoid adverse effects of corticosteroid therapy
Definition
use lowest possible dose adn potecy to control inflammation
use local/topical administration whenever possible
taper doses to stop therapy
Term
what is the MOA for NSAIDs
Definition
target COX pathway to reduce inflammation
doesn't have immunosuppressive or adrenal effects
Term
NSAIDs function
Definition
treatment of inflammatory pain
Term
COX 1
Definition
active in tissues to produce prostoglandins (gastric epithelial cell production)
involved in platelet aggregation
Term
COX 2
Definition
induced during inflammation to produce more prostoglandins - increase inflammation
role in cardiovascular system
Term
which COX pathway does this drug inhibit: ibuprofen
Definition
non-selective
both
Term
which COX pathway does this drug inhibit: naproxen
Definition
non-selective
both
Term
which COX pathway does this drug inhibit: celecoxib
Definition
selective
COX 2
Term
How do non selective COX inhibitors affect the COX pathways
Definition
reduces inflammation via COX2 inhibition
adverse effects associated with COX 1 inhibition: GI unceration, increased risk of bleeding
Term
ibuprofen
Definition
advil
reversibly inhibits COX 1 and 2
half life: 1-2 hours
OTC
Term
naproxen
Definition
aleve
reversibly inhibits COX 1 and 2
half life: 15-17 hours
OTC, higher doses need Rx
Term
celecoxib
Definition
10-20x more selective for COX 2 vs COX 1
less likely to cause GI problems
half life: 11-12 hours
only by Rx
*may increase incidence of cardiovascular events in patients already at risk
Term
why was Vioxx removed from the market
Definition
due to number of MIs
Term
what factors should you consider when choosing an NSAID
Definition
risk of GI bleed - COX2 selective, or one with mucosal protectant
adherence - choose one with longer lang life
cost
Term
glyburide pro-drug?
Definition
no
Term
salbutamol pro-drug?
Definition
no
Term
celecoxib pro-drug?
Definition
no
Term
omeprazole pro-drug?
Definition
yes
Term
propanolol pro-drug?
Definition
no
Term
levodopa pro-drug?
Definition
yes
Term
drug class glyburide
Definition
oral anti-diabetic
insulin secretagogue
Term
drug class salbutamol
Definition
bronchodilator
beta agonist
Term
drug class celecoxib
Definition
NSAID
COX 2 inhibitor
Term
drug class omeprazole
Definition
proton pump inhibitor
Term
drug class propanonol
Definition
beta blocker
Term
drug class levodopa
Definition
anti-parkinson
dopamine precursor
Term
target receptor glyburide
Definition
K-ATP channel
sulfonylurea receptor
Term
target receptor salbutamol
Definition
beta andrenergic receptor
Term
target receptor celecoxib
Definition
COX 2 enzyme
Term
target receptor omeprazole
Definition
H/K-ATPase pump
Term
target receptor propanolol
Definition
beta adrenergic receptor
Term
target receptor levodopa
Definition
dopamine receptor
Term
receptor class glycuride
Definition
ion channel
Term
receptor class salbutamol
Definition
GPCR
Term
receptor class celecoxib
Definition
enzyme
Term
receptor class omeprazole
Definition
ion channel
Term
receptor class propanolol
Definition
GPCR
Term
receptor class levodopa
Definition
GPCR
Term
drug-receptor interaction glyburide
Definition
antagonist
Term
drug-receptor interaction salbutamol
Definition
agonist
Term
drug-receptor interaction celecoxib
Definition
antagonist
Term
drug-receptor interaction omeprazole
Definition
non-competitive antagonist
Term
drug-receptor interaction propanolol
Definition
antagonist
Term
drug-receptor interaction levodopa
Definition
agonist
Term
what is the maximum daily dose of acetaminophen in adults recommended by health canada
Definition
4000mg/24 hrs
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