Pharmacology Flashcards

1
Q

competitive inhibitors

A
  • resemble substrate
  • can be overcome by increasing substrate
  • binds active site
  • does not affect Vmax
  • increases Km
  • less potent
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

competitive inhibitors, irrersible

A
  • resembles substrate
  • cant be overcome by increasing substrate
  • binds active site
  • lowers Vmax
  • unchanged Km
  • less efficacious
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

noncompetitive inhibitors

A
  • doesn’t resemble substrate
  • cant by overcome by increasing substrate
  • does not bind active site
  • lowers Vmax
  • does not affect Km
  • less efficacious
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

bioavailability (F)

A

fraction of drug that reaches the systemic circulation

- IV dose = 100%

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

volume of distribution

A

volume occupied by total amount of drug in body relative to plasma concentration

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Vd equation

A

Vd = amount of drug/concentration (mg/mg/ml=ml)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

low Vd

A

stays in IV space, large/charged molecules, protein bound

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

high Vd

A

in all tissues, small lipophilic molecules

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

clearance

A

volume of drug clear per unit time

- can change based on organ function

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

clearance equation

A

Cl = rate of elimination / drug concentration (mg/min / mg/ml)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

half life equation

A

t1/2 = Vd*0.693/Cl

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

loading dose equation

A

Cp * Vd / F

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

maintenance dose equation

A

Cp *CL * dose interval / F

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

additive drug interaction

A

A + B = sum of effects

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

permissive drug interactions

A

A is required for full B effects

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

synergistic drug interactions

A

A + B = greater than sum of parts

17
Q

tachyphylactic drug interactions

A

acute decrease in response after administation

18
Q

zero order elimination

A

eliminated independent of concentration (constant amount)

19
Q

zero order drugs

A

phenytoin, ethanol, aspirin

20
Q

first order elimination

A

eliminated dependent on concentration (constant fraction)

21
Q

weak acids in urine

A

deprotonated form is ionized
will dissociate and stay trapped in urine
- in case of overdose, add base to remove H+ and keep drug in urine

22
Q

weak bases in urine

A

protonated is ionized

- in case of overdose, add acid to increase protonated form

23
Q

phase I drug metabolism

A

reduction, oxidation, hydrolysis with P450, yield slightly polar, water soluble metabolites

24
Q

phase II drug metabolism

A

conjugation (methylation, glucuronidation, acetylation, sulfation), very polar inactive metabolites
- slow acetylators have increased side effects

25
Q

efficacious drug

A

high Vmax, unrelated to potency

26
Q

potent drug

A

lowest dose that still causes symptoms

- unrelated to efficacy

27
Q

competitive antagonist curve

A

shift curve right, does not change efficacy, can be overcome

28
Q

noncompetitive antagonist curve

A

lowers curve (efficacy), doesn’t change potency

29
Q

partial agonist

A

acts at the same site, lower efficacy, potency is independent

30
Q

sweat glands

A

are part of sympathetic pathway but are innervated by cholinergic fibers

31
Q

nicotinic receptors

A

ligand gated Na/K channels

  • Nn = autonomic
  • Nm = neuromuscular junction
32
Q

muscarinic receptors

A

G protein coupled receptors

- use Ach

33
Q

alpha 1 effects

A

increase vascular smooth muscle, pupillary dilator muscle contraction, intestinal and bladder contraction

34
Q

Gq pathway

A

receptor binding, phospholipase C converts PIP2 to IP# and DAG, activated PKC and increasing calcium

35
Q

Gs pathway

A

receptor binding, increase in adenylyl cyclase, increase cAMP, protein kinase A, increase in calcium and blocks myosin light chain

36
Q

Gi pathway

A

receptor binding, decrease in adenylyl cyclase, decrease cAMP, protein kinase A, decrease in calcium and activates myosin light chain

37
Q

tetrodotoxin

A

puffer fish toxin

- binds voltage gated sodium channels preventing depolarization

38
Q

ciguatoxin

A

reef fish toxin

- opens sodium channels causing depolarization