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Pharmacology SP2018 Exam 1 > Lectures 9 and 10- Adrenergic pharm > Flashcards

Lectures 9 and 10- Adrenergic pharm Flashcards

1
Q

what is the minor component of establishment of resting potential (electrochemical gradient)?

A

ion flux from Na/K ATPase pump activity

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2
Q

what is the major component of establishment of resting potential (electrochemical gradient)?

A

potential arising from different membrane permeabilities of Na and K (K channels leaky)

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3
Q

K is … more permeable than Na

A

100x

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4
Q

excitable cells have special membrane proteins that are specific channels for Na and K. These proteins are called …. channels because they can be open or closed based on potential difference across the membrane.

The channel for Na responds … to changes in voltage and the K channel responds …

A

voltage gated

faster

slower

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5
Q

APs in cardiac tissue are much … than in nerve or skeletal muscle

A

slower

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6
Q

simplified timeline of AP

A
  1. Na enters through ligand gated channels. cell begins to depolarize
  2. threshold depolarization is reached causing voltage sensitive Na channels to open
  3. depolarization spreads
  4. K channels open (slower)
  5. Na and K close. system back to hyperpolarized resting state
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7
Q

synaptic transmission timeline

A
  1. Ap in nerve terminal opens calcium channels
  2. calcium entry causes vesicle fusion and transmitter release
  3. receptor channels open, Na enters the postsynaptic cell and AP resumes
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8
Q

the ganglia in the sympathetic system are close to the … in a chain

A

spinal cord

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9
Q

the ganglia in the parasympathetic system are close to

A

the target organ

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10
Q

sympathetic innervation comes from which part of the spinal cord?

A

thoracolumbar

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11
Q

parasympathetic innervation comes from which part of the spinal cord?

A

craniosacral

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12
Q

postganglionic fibers in the sympathetic system are

A

long

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13
Q

postganglionic fibers in the parasympathetic system are

A

short

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14
Q

is there more branching in the symp or parasymp system

A

sympathetic

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15
Q

alpha1 (some alpha2) receptors on … cells increase calcium, increase activity of a MLCK, increase myosin light chain phosphorylation and increase muscle contractility

A

smooth muscle

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16
Q

phosphorylated … is essential for muscle contraction

A

MLC

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17
Q

… receptors are most important at presynaptic termini, they inhibit epi and norepi release (CNS and PNS)

A

alpha2

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18
Q

alpha2 … enhance CNS response

A

antagonists

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19
Q

alpha2 … attenuate CNS response

A

agonists

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20
Q

alpha2 antagonists … HR

alpha2 agonists … HR

A

increase

decrease

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21
Q 
vasoconstrictor or vasodilator?
a1 agonist
a1 antagonist
a2 agonist
a2 antagonist
A

vasoconstrictor
vasodilator
vasodilator
vasoconstrictor

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22
Q

… receptors on smooth muscle cells increase PKA, phosphorylate and inhibit MLCK, diminish calcium levels and inhibit MLCK, diminish phosphorylation of MLC and decrease muscle contractility

A

beta2

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23
Q

cAMP activates … which in turn inhibits MLCK

A

PKA

24
Q

PKA mediated phosphorylation also activates … which leads to hyperpolarization leading to reduction in cellular calcium producing smooth muscle relaxation because MLCK activity is attenuated

A

K channels

25
Q

… receptors on cardiac muscle cells activate PKA, activate L type calcium channels, increase calcium levels and increase muscle contractility

A

b1

26
Q

the … receptor is the dominant receptor in cardiac muscle. drugs that activate this receptor improve contractility of heart, increase HR and excess stimulation can results in arrythmias

A

b1

27
Q

activation of the … receptor leads to vascular and non vascular smooth muscle relaxation. (reduce BP, broncodilation, reduce uterine contraction)

A

b2

28
Q

there are a large number of … receptors relative to … receptors on vascular smooth muscle. activation of these will lead to vasoconstriction

A

a1

b2

29
Q

epi’s actions in an emergent situation

A

stim alpha: increase BP
stim b1: positive cardiac effects
stim. b2: bronchodilation

30
Q

methoxamine, phenylephrine, levonordefrin, midodrine, oxymetazoline, metaraminol are all

A

alpha1 receptor agonists (increase BP)

31
Q

denopamine, dobutamine, xamoterol, isoprenaline are all

A

b1 receptor agonists (treat heart failure)

32
Q

albuterol, pirbuterol, isoprenaline, formoterol, clenbuterol are all

A

b2 receptor agonists (smooth muscle relax)

33
Q

… is used to reverse soft tissue numbness after administration of local anesthetics with vasoconstrictors. injected when pain relief is no longer needed

A

phentolamine

34
Q

beta blockers will …. renin release from kidney

A

diminish

35
Q

ISA stands for

A

intrinsic sympathomimetic activity (partial agonist)

36
Q

beta blockers without ISA…

A

decrease HR, decrease renin activity, decrease CO

37
Q

beta blockers with ISA

A

do not depress cardiac fxn or renin activity but do attenuate agonist driven increases

38
Q

beta blockers can also reduce vitreous production to treat …

A

glaucoma

39
Q

beta blockers that get into the CNS can be used to treat … and …

A

migraine

tremor associated anxiety

40
Q

2 blockers that are alpha receptor and beta receptor antagonists

A

labetalol

carvedilol

41
Q

…. is 7x more potent as a beta blocker, ISA activity, used in long term management of HTN

A

labetalol

42
Q

…. no ISA activity, effective in tx of CHF, antioxidant activity

A

carvedilol

43
Q

clonidine causes

A

xerostomia

44
Q

cholinergic receptors comes in 2 types:

A

nicotinic and muscarinic

45
Q

odd numbered muscarinic receptors (M1,M3,M5) are linked to …

A

Gaq (activate DAG and IP3 signaling)

46
Q

even numbered muscarinic receptors (M2, M4) are linked to ….

A

Gai (inhibit adenylate cyclase)

47
Q

cholinergic agonists can either be … or …

A

direct acting

indirect acting

48
Q

direct cholinergic agonists bind to ….

A

muscarnic or nicotinic AcCH receptor or both

49
Q

indirect acting cholinergic agonists are ….

A

cholintesterase inhibitors (acetylcholine will stick around longer)

50
Q

hydrolysis by cholinesterase has a profound effect on the duration of action of ….

A

cholinergic agonists

51
Q

acetylcholine is hydrolyzed …. and has the … duration of action

A

rapidly

shortest

52
Q

methacholine is hydrolyzed…. somewhat …duration of action (compared to acetylcholine)

A

slower

longer

53
Q

carbachol is … hydrolyzed so longer duration of action

A

not

54
Q

which are more clinically relevent? muscarinic or nicotinic agonists?

A

muscarinic

55
Q

does acetylcholine affect muscarinic or nicotinic specificity ?

A

non selective

56
Q

does carbachol favor muscarinic or nicotinic receptors

A

nicotinic

57
Q

does methacholine favor muscarinic or nicotinic receptors

A

muscarinic

Pharmacology SP2018 Exam 1 (8 decks)

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