the _________ leads to the effect we're looking for

ligand that binds to a receptor and thereby results in a biological response

ligand that produces less than maximal response

ligand that diminishes the response of the receptor

ligand that binds to the same receptor site as the agonist, but reverses the activity of the receptor

an antagonist

morphine is an example of a(n)

codeine is an example of a(n)

naloxone is an example of a(n)

in the pharmacodynamic sigmoid Emax model, the E is ____

in the pharmacodynamic sigmoid Emax model, the Emax is ____

in the pharmacodynamic sigmoid Emax model, the EC50 is ____

in the pharmacodynamic sigmoid Emax model, the C is ____

in the pharmacodynamic sigmoid Emax model, the n is ____

select all that are true

_____ is an effect, _____ is a concentration

in PK we look at _____. in PD we look at _____

this pharmacodynamic response occurs on a scale or continuum

this pharmacodynamic response cannot be continuously correlated with drug concentration

what are some reasons that it's clinically difficult to determine the "true" Emax

in dichotomous responses we evaluate the response from

____ measures the activity of a ligand in terms of the concentration required to produce the defined effect

____ describes the way by which agonists vary in response, even when occupying the same number of receptors

______ is displayed when a lower drug concentration is required to achieve the same response

______ is displayed when you get a larger response with the same drug concentration as another compound

what factors affect the relationship between plasma concentration and physiologic response

in a direct pharmacodynamic link/response

in an indirect pharmacodynamic link/response

counter-clockwise hysteresis (the time delay between the measured plasma concentration and the observed effect) is

clockwise hysteresis (the time delay between the measured plasma concentration and the observed effect) is

in counter-clockwise hysteresis

what are some reasons that sensitization (counter-clockwise hystereisis) can occur

clockwise hysteresis (proteresis)

what are some reasons tolerance can occur

how do we prevent tachyphylaxis from occuring

PK vs. PD drug and disease interactions: enzyme inhibition

PK vs. PD drug and disease interactions: enzyme induction

PK vs. PD drug and disease interactions: changes in metabolism

PK vs. PD drug and disease interactions: changes in organ function

PK vs. PD drug and disease interactions: CNS depressants

PK vs. PD drug and disease interactions: Anticoagulants

PK vs. PD drug and disease interactions: Anticonvulsants

PK vs. PD drug and disease interactions: QT-prolonging agents

PK vs. PD drug and disease interactions: drug concentration changed

t/f: dosage form/route of administration does not have a significant effect on onset and duration of analgesia

t/f: changes in dosing regimens are driven primarily by efficacy and tolerability

t/f: onset and duration of analgesia will be a result of combined PK, MOA, receptor location, dosage form, and patient factors

t/f: PD is sometimes related to the side effects of a class of drugs where the side effects become the targeted pharmacologic outcome

n-acetyl-cysteine

which is expressed in response to insult/injury

t/f: must functions, including GI protection, renal function, and inflammation are impacted by at least two prostaglandins

there is no ____ in platelets

COX-2 selective drugs were developed in order to

because platelets do not have a nucleus, they cannot inhibit platelet aggregation. when you inhibit with COX-2...

what are you at risk for if children use ASA

what patients should not use ASA

t/f: gralise and horizant are interchangeable with other gabapentin products

which chemical mediator increases vascular permeability, and increases blood flow to the injured area

which chemical mediator(s) is (are) involved in pain response, vascular permeability, and chemotaxis

which chemical mediator(s) increase capillary blood flow and vascular permeability

what is the only NSAID that irreversibly covalently modifies COX by acetylating Ser530 of COX-1 and SER516 of COX-2.

salicylates are more potent against ___ than ___ which is why we see so many side effects with ASA

ASA should be avoided in patients with

as effective as ASA but few side effects. does not cause GI bleeds and can be given to ASA sensitive patients

has an amide group instead of a carboxylic acid. it is not acidic which means there's a lack of gastric irritation. this one can be used in patients with ASA hypersensitivity. has minimal anti-inflammatory activity

longer-acting, slower onset. more potent and more effective than ASA but fewer side effects. this one is also much more expensive

one of the most potent NSAIDS in use. more potent than ASA and acetaminophen (10x analgesic potency of ASA)

has way too many side effects to be used long term

a non-nitrogenous analog of indomethacin

can be used long-term because there are limited side effects

there is a sulfoxide group on the compound. when it is reduced to sulfide, we get the active form of the drug. when it's oxidized to sulfone, we get the inactive form

if the R group is a hydrogen it's _____. if the R group is a methyl it's _____.

in most racemic arylacetic acid derivatives, the ____ is the only isomer with anti-inflammatory activity

in this med, caution use with hydantoins, sulfonamides, and sulfonylureas. this drug displaces the drugs listed from their binding sites and can cause toxicity

an arylacetic acid derivative that is NOT sold as a racemic mixture. Only the S(+) isomer is obtained and marketed

not recommended for pregnant or lactating women

not recommended for children under 16

has more anti-inflammatory activity than phenylbutazone but less than indomethacin. it's COX-2 selective analog was removed from the market due to anaphylaxis, particularly in patients with ASA sensitivity

instead of inhibiting COX, this drug inhibits the synthesis of leukotrienes and leukocyte migration into inflamed joints in addition to inhibiting the biosynthesis of prostaglandins

mainly used as 1% ophthalmic solution for prevention of surgically induced miosis during cataract extraction

oral dosage forms have been discontinued due to renal effects

this is NOT an arylacetic acid. it is a ketone. it is non-acidic which decreases GI side effects. the active metabolite IS an acetic acid.

a propionic acid derivative with an a-methyl group

1st topical NSAID indicated for ophthalmic use in the US

inhibits intraoperative miosis induced by prostaglandins in cataract surgery

a cyclized heteroaryl propionic acid derivative with a-methyl group fused to the pyrrole ring. this is done for rigidity.

relatively more effective as an analgesic than as an anti-inflammatory

relief of ocular itching caused by seasonal allergies

contraindicated in patients receiving ASA or NSAIDs due to cumulative risk of inducing serious side effects

belongs to arylacetic acid derivatives, but is also considered a homolog of n-arylanthranillic acid

it inhibits COX but also inhibits the lipooxygenase pathway, resulting production of leukotrienes. it also inhibits arachidonic acid release and stimulation of it's uptake, resulting in a reduction of arachidonic acid availability.

highly selective for COX-2. has a high safety profile.

not strictly an arylacetic acid derivative

cannot be used safely for more than 7 days

can treat primary dysmenorrhea

can use for chronic treatment. does have a high incidence of severe diarrhea

do not have a COOH but instead have an enolic acid

which oxicam is considered a selective COX-2 inhibitor

first marketed selective COX-2 inhibitor

side effects include increased risk of serious CV thrombotic events, MI, and stroke

29 year old man drinking 3 shots of whiskey daily

64 year old taking warfarin for blood clot

MM is on warfarin. disregarding all other factors, what could you select for your patient

CK is on heparin. disregarding all other factors, what could you select for your patient

JT is on antiplatelets. disregarding all other factors, what could you select for your patient

PH is on NOACs/DOACs. disregarding all other factors, what could you select for your patient

NS is on ASA. disregarding all other factors, what could you select for your patient

76 year old taking gabapentin

58 year old with heart failure

54 year old with history of GI bleeds

50 year old taking 40mg lisinopril daily

26 year old woman in her third trimester of pregancy

26 year old woman in her third trimester of pregancy

46 year old woman receiving chemotherapy for metastatic breast cancer

what is safe to use in patients with thrombocytopenia

34 year old man with aspirin-sensitive asthma

72 year old woman taking aspirin and sertraline

t/f: bleeding can occur with low-dose ASA alone

44 year old s/p roux-en y gastric bypass

32 year old woman taking 20mg prednisone daily

32 year old woman taking 20mg prednisone daily

found in the skin, subcutaneous tissue, and mucous membranes

due to external mechanical, chemical, or thermal events

found in muscles, tendons, joints, and bones.

due to overuse, strain, mechanical injury, cramping, or inflammation

carries proprioceptive signals, it is myelinated, the largest, and has the quickest conduction speed

carries touch signals. it is myelinated, the second largest, and has the second quickest conduction speed

not involved in pain signals unless there is a change in the nervous system. this is called allodynia.

carries pain signals. it is myelinated. it carries the faster, more sharp-feeling pain. it has mechanoreceptors

carries pain signals. it is not myelinated. it carries the slower pain which manifests as burning, aching, and gnawing. it is responsive to changes in temperature

carries pain signals. it is not myelinated. it carries the slower pain which manifests as burning, aching, and gnawing. it is responsive to changes in temperature. it is chemically activated

peripheral stimulus to dorsal root ganglion

action potential from dorsal root ganglion to dorsal horn of the spinal cord

dorsal horn of the spinal cord

thalamus to reach somatic/sensory cortex and premotor cortex

brainstem to spinal cord

transduction

conduction

perception

chemical to electrical

chemical and electrical

incredibly complex GCPRs that are cell surface bound and set off a cascade of secondary messenger systems once a drug is bound that reduce the depolarization that is occuring

presynaptic channels on the peripheral nociceptor

there are two endogenous purine synthesis genetic enzyme abnormalities. which one is superactivity

there are two endogenous purine synthesis genetic enzyme abnormalities. which one is deficiency