get into brain Flashcards

1
Q

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

A
  • Phenothiazines
  • Antihistamines
  • CNS depressants

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

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2
Q

examples of dose dependent toxicities

A

Excessive hypotension
arrhythmias
hypoglycemia
hemorrhage

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3
Q

chloramphenicol causes what toxicity

A

aplastic anemia

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4
Q

what drug causes retardation of bone growth

A

tetracycline

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5
Q

what toxicities are caused by aminoglycosides

A

renal + ototoxicity

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6
Q

type of antagonism that decreases the agonists max response

A

non competitive

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7
Q

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!

A

Non competitive

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7
Q

type of antagonism that decreases affinity (Kd or EC50)

A

Competitive antagonists

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7
Q

type of antagonism that DOESN’T affect max response

A

competitive

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8
Q

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

A

competitive

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9
Q

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

A

competitive

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10
Q

what type of agonist is Buprenophine

A

partial
response caused is less than that produced by full agonist

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11
Q

naloxone is an…

A

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

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12
Q

morphine is an…

A

agonist
causes max shift of receptors to the activated state

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13
Q

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

A

right

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14
Q

efficacy of a drug is dependent on what

A

drug receptor interaction and intrinsic activity

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15
Q

what is Kd

A

concentration needed to produce half max binding

16
Q

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

A

α1

17
Q

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

A

phospholipase C
IP3 and DAG

18
Q

IP3 stimulates ____ release

A

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

19
Q

what does DAG activate

A

PKC

20
Q

what is the loading dose of a drug dependent on

A

Vd (volume of distribution)

21
Q

equation for loading dose

A

LD = Vd x target concentration (Css)

22
Q

is a loading dose dependent on half life or clearance?

A

naur

23
Q

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

A

HIGH b/c the drug plasma concentration is low

24
Q

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

A

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

25
Q

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

A

elimination rate

26
Q

what is a maintenance dose

A

dose needed to maintain steady state concentration

27
Q

equation for maintenance dose

A

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

28
Q

what has a large role in maintenance dose

A

Clearance (elimination)

29
Q

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

A

causes a higher steady state concentration

30
Q

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

A

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

31
Q

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

A

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

32
Q

what type of elimination do aspirin, fentanyl and phenytoin undergo

A

zero order elim

33
Q

explain enterohepatic recirculation

A

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

34
Q

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

A

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

ex: opioids, benzodiazepines

35
Q

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

A

first

36
Q

what kind of tolerance is seen with morphine

A

Pharmacodynamic tolerance
same [drug] but effect decreases

37
Q

what effect does meningitis & encephalitis have on drug metabolism

A

increased penetration into the CNS

38
Q

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

A

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