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MTC 3- Immunology > 10.18 NS drugs > Flashcards

10.18 NS drugs Flashcards

1
Q

M1 receptor (G protein):

A

Gq

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2
Q

M2 receptor (G protein):

A

Gi

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3
Q

M3 receptor (G protein):

A

Gq

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4
Q

α1 receptor (G protein):

A

Gq

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5
Q

α2 receptor (G protein):

A

Gi

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6
Q

β1 receptor (G protein):

A

Gs

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7
Q

β2 receptor (G protein):

A

Gs

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8
Q

Gq signaling involves (cAMP and PKA / PLC and calcium)

A

Gq signaling involves PLC –> Ca2+ (activation)

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9
Q

Gs signaling involves (cAMP and PKA / PLC and calcium)

A

Gs signaling involves AC –> cAMP –> PKA (activation)

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10
Q

Gi signaling involves (cAMP and PKA / PLC and calcium)

A

Gi signaling involves inhibition of AC –> decreased cAMP

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11
Q

Most organs are innervated by both the sympathetic and parasympathetic divisions; the exception is vascular smooth muscle which is only controlled by _

A

Most organs are innervated by both the sympathetic and parasympathetic divisions; the exception is vascular smooth muscle which is only controlled by sympathetic nervous system

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12
Q

Sympathetic receptor in the pupil

A

Sympathetic receptor in the pupil:
α1

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13
Q

Sympathetic receptor in the salivary glands

A

Sympathetic receptor in the salivary glands:
β2

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14
Q

Sympathetic receptor in the bronchioles

A

Sympathetic receptor in the bronchioles:
β2

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15
Q

Sympathetic receptor in the heart

A

Sympathetic receptor in the heart:
β1

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16
Q

Sympathetic receptor in the vascular SM

A

Sympathetic receptor in the vascular SM:
α1, β2

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17
Q

Sympathetic receptor in the GI tract

A

Sympathetic receptor in the GI tract:
β2

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18
Q

Sympathetic receptor in the uterus

A

Sympathetic receptor in the uterus:
β2

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19
Q

Sympathetic receptor in the urethra

A

Sympathetic receptor in the urethra:
α1

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20
Q

Sympathetic receptor in the bladder

A

Sympathetic receptor in the bladder:
β2

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21
Q

Parasympathetic receptor in the pupil

A

Parasympathetic receptor in the pupil:
M3

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22
Q

Parasympathetic receptor in the salivary glands

A

Parasympathetic receptor in the salivary glands:
M3

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23
Q

Parasympathetic receptor in the heart

A

Parasympathetic receptor in the heart
M2

24
Q

Parasympathetic receptor in the bronchioles

A

Parasympathetic receptor in the bronchioles:
M3

25
Q

Parasympathetic receptor in the GI tract

A

Parasympathetic receptor in the GI tract:
M3

26
Q

Parasympathetic receptor in the bladder

A

Parasympathetic receptor in the bladder:
M3

27
Q

Parasympathetic receptor in the urethra:

A

Parasympathetic receptor in the urethra:
none

28
Q

What is the general rule for selectivity of parasympathetic drugs for the M receptors?

A

Most parasympathetic drugs tend to affect both M2 and M3 equally
* Why we see toxicity

29
Q

α2 receptors are located _

A

α2 receptors are located on the presynaptic neuron and functions as a regulator; inhibits the release of too much NE/E

30
Q

What are three synonyms for drug classes that stimulate the parasympathetic NS?

A

Stimulate parasympathetic:
Parasympathomimetic =
Cholinomimetic =
Muscarinic receptor agonist

31
Q

Direct parasympathetic agonists work by _

A

Direct parasympathetic agonists work by activating the receptor just like Ach does

32
Q

Indirect parasympathetic agonists work by _

A

Indirect parasympathetic agonists work by inhibiting acetylcholinesterase (breakdown of Ach)

33
Q

Drugs (2) that can reverse bradycardia

A

To reverse bradycardia we need to inhibit M2

Atropine
Glycopyrrolate

34
Q

What are the effects of an M2 antagonist like atropine/ glycopyrrolate?

A

M2 agonist: decreases depolarization at the SA/AV node –> decreases heart rate –> decreases cardiac output

M2 antagonist: reverses the bradycardia; increases SA/AV node firing to increase HR

35
Q

What do M3 agonists do in the bronchioles?

A

M3 agonists: found throughout the body besides the heart (pupil, salivary gland, bronchioles, GIT, bladder, uterus)
* In bronchioles: Induce bronchoconstriction
* Ex: methacholine

36
Q

Name 3 types of M3 antagonists that can act in the bronchioles:

A

Ipratropium
Tiotropium
Aclidinium

These M3 antagonists will trigger bronchodilation to treat things like COPD

37
Q

Drugs to treat gastrointestinal motility include _ and _ which target _ receptor in the GIT

A

Drugs to treat gastrointestinal motility include dicyclomine and hyoscyamine which target M3 receptor in the GIT
* They will inhibit smooth muscle contraction in the gut to decrease peristalsis rate
* Used in IBS

38
Q

M3 receptors can be found in the glands (regulate secretions);
Agonists include:
Antagonists include:

A

M3 receptors can be found in the glands (regulate secretions);
Agonists include: pilocarpine
Antagonists include: glycopyrrolate

39
Q

To treat urinary retention we can either activate _ parasympathetic receptor in the detrusor muscle of the bladder (squeezes the bladder)

Or we can cause urethral smooth muscle to relax which means we want _ sympathetic receptor to be inhibited

A

To treat urinary retention we can either activate M3 parasympathetic receptor in the detrusor muscle of the bladder (squeezes the bladder)
* Agonist: bethanechol

Or we can cause urethral smooth muscle to relax which means we want alpha1 sympathetic receptor to be inhibited
* alpha1 antagonists: alfuzosin, silodosin, tamsulosin

40
Q

What is the effect of an M3 antagonist in the bladder?

A

M3 antagonist in the bladder would cause urinary retention
* Ex: use oxybutynin and tolterodine to treat an overactive bladder

41
Q

_ is a M3 agonist that causes the pupils to constrict

A

Carbachol is a M3 agonist that causes the pupils to constrict

42
Q

_ is an M3 antagonist that causes the pupils to dilate

A

Atropine is an M3 antagonist that causes the pupils to dilate

43
Q

Miosis means _

A

Miosis means pupil constriction

44
Q

Mydriasis means _

A

Mydriasis means dilation

45
Q

β1 agonists do what?

A

β1 agonists: stimulate AV/SA node –> increase HR –> increase CO

46
Q

β1 antagonists are indicated for treatment of _ and _

A

β1 antagonists are indicated for treatment of hypertension and angina

47
Q

β2 agonists do what?

A

β2 agonists: bronchodilation
* ex: albuterol, salmeterol, formoterol

48
Q

What does antagonizing the alpha1 receptor in the urethra do?

A

alpha1 antagonists: alfuzosin, silodosin, tamsulosin

Normally sympathetic NS will lead to retention of urine –> so normally SM of urethra is contracted –> if we add alpha 1 antagonist is causes relaxation and allows urination

49
Q

_ drug is an alpha1 agonist that leads to pupil dilation

A

Phenylephrine drug is an alpha1 agonist that leads to pupil dilation

50
Q

Ritodrine and terbutaline are drugs used to stop preterm labor; they work by _

A

Ritodrine and terbutaline are drugs used to stop preterm labor; they work by agonizing B2 receptors in the uterus
* Uterine relaxation

51
Q

Vascular smooth muscle contains both α1 and β2 but the effect of _ usually dominates

A

Vascular smooth muscle contains both α1 and β2 but the effect of α1 usually dominates
* Meaning we see constriction of vessels when sympathetic system is active
* α1 agonists will cause vasoconstriction and increase in BP

52
Q

Clonidine is an α2 agonist which is used to treat _

A

Clonidine is an α2 agonist which is used to treat hypertension

53
Q

Side effects of pilocarpine:

A

Intended to increase salivation
* Side effects: pupil constriction, diarrhea
* All are M3 targets

54
Q

Side effects of atropine:

A

Intended to target M2 to increase heart rate
* Side effects: pupil dilation, dry mouth, constipation
* Not very selective so it inhibits M3 and M2

55
Q

Toxicities of parasympathomimetics:

A

DUMBBELS:
Diarrhea
Urination
Miosis
Bradycardia
Bronchoconstriction
Emesis
Lacrimation
Salivation

56
Q

Side effects of tamsulosin:

A

Tamsulosin is intended to inhibit alpha1 in the bladder to relax the urethra
* Side effects: inhibits alpha1 in the eyes and vascular smooth muscle –> miosis, hypotension

57
Q

Side effects of nadolol:

A

Nadolol is a beta blocker that is intended to block beta1 to decrease BP
* Side effects: blocks B2 as well and can cause bronchoconstriction

MTC 3- Immunology (8 decks)

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