get into brain

Question 1

what are 3 examples of drugs that result in several dose-dependent responses and how are these multiple responses possible

Answer 1

• Phenothiazines
• Antihistamines
• CNS depressants

multiple responses due to presence of multiple receptors being activated at different dose levels

Question 2

examples of dose dependent toxicities

Answer 2

Excessive hypotension
arrhythmias
hypoglycemia
hemorrhage

Question 3

chloramphenicol causes what toxicity

Answer 3

aplastic anemia

Question 4

what drug causes retardation of bone growth

Answer 4

tetracycline

Question 5

what toxicities are caused by aminoglycosides

Answer 5

renal + ototoxicity

Question 6

type of antagonism that decreases the agonists max response

Answer 6

non competitive

Question 7

type of antagonism where antagonist binds irreversibly to receptor so that the agonist can’t bind OR binds to secondary site so agonist can’t act

how rude!

Answer 7

Non competitive

Question 7

type of antagonism that decreases affinity (Kd or EC50)

Answer 7

Competitive antagonists

Question 7

type of antagonism that DOESN’T affect max response

Answer 7

competitive

Question 8

type of antagonism that shifts the curve to the right in a parallel fashion

Answer 8

competitive

Question 9

if the agonist concentration is high enough, the effect of this kind of antagonist can be overcome

Answer 9

competitive

Question 10

what type of agonist is Buprenophine

Answer 10

partial
response caused is less than that produced by full agonist

Question 11

naloxone is an…

Answer 11

antagonist
binds to receptor
does NOT initiate response
will block response of agonist

Question 12

morphine is an…

Answer 12

agonist
causes max shift of receptors to the activated state

Question 13

if potency of a drug decreases, which direction does the curve shift

Answer 13

right

Question 14

efficacy of a drug is dependent on what

Answer 14

drug receptor interaction and intrinsic activity

Question 15

what is Kd

Answer 15

concentration needed to produce half max binding

Question 16

activation of _____ by NE and E leads to activation of Gq

Answer 16

α1

Question 17

activated Gq leads to activated phospholipase _____which leads to the release of ____+_____

Answer 17

phospholipase C
IP3 and DAG

Question 18

IP3 stimulates ____ release

Answer 18

Ca+
increased calcium can activate Ca dependent protein kinases which phosphorylate their substrates

Question 19

what does DAG activate

Answer 19

PKC

Question 20

what is the loading dose of a drug dependent on

Answer 20

Vd (volume of distribution)

Question 21

equation for loading dose

Answer 21

LD = Vd x target concentration (Css)

Question 22

is a loading dose dependent on half life or clearance?

Answer 22

naur

Question 23

if a drug has a High Vd, will it require a high or low loading dose

Answer 23

HIGH b/c the drug plasma concentration is low

Question 24

what needs to be considered in patients with decreased renal or hepatic clearance and maintenance doses

Answer 24

maintenance doses need to be decreased or change the dosing interval to cause a lower concentration of the drug

they cannot eliminate the drug as well

Question 25

when steady state condition has been achieved, the dosing rate is equal to what

Answer 25

elimination rate

Question 26

what is a maintenance dose

Answer 26

dose needed to maintain steady state concentration

Question 27

equation for maintenance dose

Answer 27

maintenance dose = (CL * TC / F) * dosing interval

Question 28

what has a large role in maintenance dose

Answer 28

Clearance (elimination)

Question 29

what is the effect of shortening the dosing interval on steady state concentration

Answer 29

causes a higher steady state concentration

Question 30

what is the effect of lengthening the dosing interval on steady state [ ]

Answer 30

gradual decrease of the plasma level of drug and a lower steady state

Question 31

type of elimination in which the rate of elimination is proportional to the [drug]

Answer 31

first order
if drug [ ] increases so does rate of elimination

Question 32

what type of elimination do aspirin, fentanyl and phenytoin undergo

Answer 32

zero order elim

Question 33

explain enterohepatic recirculation

Answer 33

drugs get metbolized in liver (get conjugated) then are excreted in bile where they are metabolized back into free drug that gets reabsorbed into plasma and returned back to liver

Question 34

what are the consequences of drugs that undergo enterohepatic circulation? Give a drug example

Answer 34

lower doses of the drugs can be therapeutically effected since elimination is reduced by the recycling of the drug

ex: opioids, benzodiazepines

Question 35

Steady state concentrations and conditions can only develop for __________ order eliminations

Answer 35

first

Question 36

what kind of tolerance is seen with morphine

Answer 36

Pharmacodynamic tolerance
same [drug] but effect decreases

Question 37

what effect does meningitis & encephalitis have on drug metabolism

Answer 37

increased penetration into the CNS

Question 38

what does a large Kd mean in regards to receptor - ligand affinity
what about a small Kd

Answer 38

large Kd: receptor binds ligand poorly
small Kd: high affinity of ligand for receptor