Term
| what are the 3 branches of pharmacology |
|
Definition
pharmacodynamics
pharmacokinetics
toxicology |
|
|
Term
|
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
|
Definition
drugs effect on the body
pharmacologic effect
clinical response
toxicity
therapeutic benefit |
|
|
Term
|
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
|
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
|
|
Term
|
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
|
|
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
|
|
Term
| what are the 4 different types of drugs |
|
Definition
natural
synthetic
endogenous
exogenous |
|
|
Term
|
Definition
caffiene
nicotene
from a plant |
|
|
Term
|
Definition
|
|
Term
|
Definition
made within the body
acetylcholine, hormones |
|
|
Term
|
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
|
Definition
| mirror image stereoisomers that are non-superposable (not identical) |
|
|
Term
|
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
|
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
|
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
|
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
|
Definition
| favourability of drug-receptor interaction |
|
|
Term
|
Definition
[drug] required to produce 50% of the maximum response
measures potency |
|
|
Term
|
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
|
Definition
molecule that binds to a receptor and stabilizes the receptor conformation
activates the receptor to cause a response |
|
|
Term
|
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
|
Definition
| stabilizes the inactive conformation of a receptor if there is baseline activity |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| brings it back to base line |
|
|
Term
|
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
|
Definition
| competitive and non competitive |
|
|
Term
|
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
|
Definition
neutralize stomach acid
TUMS |
|
|
Term
|
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
|
|
Term
| high [non-competitive antagontists] all spare receptors will be bound and ______ will be effected |
|
Definition
|
|
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
|
Definition
| effective dose for 50% of the population |
|
|
Term
|
Definition
| toxic dose for 50% of the population |
|
|
Term
|
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
|
Definition
| dose that provides therapeutic efficacy while remaining within safe limits |
|
|
Term
|
Definition
|
|
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
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
ion channels
PI3K
phospholipases
adenylylayclases
receptor kinases |
|
|
Term
|
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
|
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
|
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
|
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
|
Definition
|
|
Term
|
Definition
|
|
Term
| what are the two types of administration of drugs |
|
Definition
|
|
Term
|
Definition
enteral (PO)
parenteral:
sucutaneous (sc)
intramuscular (im)
intravenous (iv) |
|
|
Term
|
Definition
topical
inhaled
dermal
ocular |
|
|
Term
|
Definition
enteral
through the mouth, stomach, GI system |
|
|
Term
|
Definition
parenteral
subcutaneous under the skin |
|
|
Term
|
Definition
| parenteral into the muscle |
|
|
Term
|
Definition
|
|
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
|
|
Term
| example of a drug that uses transdermal administration |
|
Definition
|
|
Term
| example of a drug that uses transmucousal administration |
|
Definition
|
|
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
|
|
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
|
Definition
any agent that can disturb the development of an embryo or fetus
birth defect
halt pregnancy |
|
|
Term
|
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
|
Definition
conception to day 17
teratogenic exposure often causes miscarrage |
|
|
Term
|
Definition
days 18-60
exposure causes ireparable damage and significant anatomical deformities |
|
|
Term
|
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
|
Definition
folate metabolism inhibitors
CNS defects, craniofacial anomalies, mental retardation |
|
|
Term
|
Definition
ACE inhibitor
fetal renal and cardiovascular damage |
|
|
Term
| drugs considered safe in pregnancy |
|
Definition
diphenhydramine
penicillin
heparin
insulin
topical drugs |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
| which drug tend to cause withdrawl symptoms after birth (development of dependence) |
|
Definition
|
|
Term
|
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
|
|
Term
|
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
|
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
|
|
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
|
|
Term
|
Definition
liver enzyme
metabolizes antidepressants, antipsychotics and beta blockers
activates pro-drugs(codine to morphine) |
|
|
Term
|
Definition
CYP2D6*1
majority of population |
|
|
Term
|
Definition
CYP2D6*2
rapid removal of drugs metabolized by CYP2D6 |
|
|
Term
|
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
|
Definition
a basic bodily sensation that is induced by a noxious stimulus
characterized by physical discomfort
leads to evasive action
very subjective |
|
|
Term
|
Definition
painful stimulus sends signal via action potential to the brain
brain returns signals that generate the response |
|
|
Term
|
Definition
painful stimulus with a physiological purpose
nociceptive
inflammatory |
|
|
Term
|
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
|
|
Term
| ____/____ canadian adults suffer from chronic pain |
|
Definition
|
|
Term
| __-___% of children experience recurrent or chronic pain |
|
Definition
|
|
Term
| two methods of pain management |
|
Definition
opioid analgesics
non-opioid analgesics |
|
|
Term
|
Definition
acetaminophen
antiinflammatory agents (steroids, non-steroidal antiinflammatory agents NSAIDS) |
|
|
Term
| 1-3 on the pain scale - pharmacologic management? |
|
Definition
|
|
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
|
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
|
|
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
|
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
|
Definition
full agonist at mu receptor
available in many formulations
oral:immediate, sustained, and controlled release
parenteral: SC 2D6 or IV |
|
|
Term
|
Definition
partial agonist @ mu-receptor
metabolized to morphine by CYP2D6 |
|
|
Term
|
Definition
full agonist at mu-receptor
more potent than morphine
inactivates metabolites via CYP2D6 |
|
|
Term
|
Definition
oxycodone
crushed to give very high doses of immediate release oxycodone
problems with abuse |
|
|
Term
|
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
|
|
Term
|
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
|
|
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
|
Definition
tylenol
reduces fever and pain
maximum dose- children: <65mg/kg/24 hours ; adults: <4g/24 hours |
|
|
Term
|
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
|
|
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
|
|
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
|
Definition
corticosteroid
acute use of low dose to reduce or prevent post-operative pain and inflammation |
|
|
Term
|
Definition
corticosteroid
topical/ local
reduce inflammation related to asthma, dermatitis and allergies |
|
|
Term
|
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
|
Definition
| treatment of inflammatory pain |
|
|
Term
|
Definition
active in tissues to produce prostoglandins (gastric epithelial cell production)
involved in platelet aggregation |
|
|
Term
|
Definition
induced during inflammation to produce more prostoglandins - increase inflammation
role in cardiovascular system |
|
|
Term
| which COX pathway does this drug inhibit: ibuprofen |
|
Definition
|
|
Term
| which COX pathway does this drug inhibit: naproxen |
|
Definition
|
|
Term
| which COX pathway does this drug inhibit: celecoxib |
|
Definition
|
|
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
|
Definition
advil
reversibly inhibits COX 1 and 2
half life: 1-2 hours
OTC |
|
|
Term
|
Definition
aleve
reversibly inhibits COX 1 and 2
half life: 15-17 hours
OTC, higher doses need Rx |
|
|
Term
|
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
|
|
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
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
oral anti-diabetic
insulin secretagogue |
|
|
Term
|
Definition
bronchodilator
beta agonist |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
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
|
|
Term
| target receptor omeprazole |
|
Definition
|
|
Term
| target receptor propanolol |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
| receptor class salbutamol |
|
Definition
|
|
Term
|
Definition
|
|
Term
| receptor class omeprazole |
|
Definition
|
|
Term
| receptor class propanolol |
|
Definition
|
|
Term
|
Definition
|
|
Term
| drug-receptor interaction glyburide |
|
Definition
|
|
Term
| drug-receptor interaction salbutamol |
|
Definition
|
|
Term
| drug-receptor interaction celecoxib |
|
Definition
|
|
Term
| drug-receptor interaction omeprazole |
|
Definition
| non-competitive antagonist |
|
|
Term
| drug-receptor interaction propanolol |
|
Definition
|
|
Term
| drug-receptor interaction levodopa |
|
Definition
|
|
Term
| what is the maximum daily dose of acetaminophen in adults recommended by health canada |
|
Definition
|
|
