10.18 NS drugs Flashcards

(57 cards)

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
Parasympathetic receptor in the **GI tract**
Parasympathetic receptor in the **GI tract**: **M3**
26
Parasympathetic receptor in the **bladder**
Parasympathetic receptor in the **bladder**: **M3**
27
Parasympathetic receptor in the **urethra**:
Parasympathetic receptor in the **urethra**: **none**
28
What is the general rule for selectivity of parasympathetic drugs for the M receptors?
Most parasympathetic drugs tend to affect **both M2 and M3 equally** * Why we see toxicity
29
α2 receptors are located _
α2 receptors are located **on the presynaptic neuron** and functions as a **regulator; inhibits the release of too much NE/E**
30
What are three synonyms for drug classes that stimulate the parasympathetic NS?
Stimulate parasympathetic: **Parasympathomimetic** = **Cholinomimetic** = **Muscarinic receptor agonist**
31
*Direct* parasympathetic agonists work by _
*Direct* parasympathetic agonists work by **activating the receptor just like Ach does**
32
*Indirect* parasympathetic agonists work by _
*Indirect* parasympathetic agonists work by **inhibiting acetylcholinesterase** (breakdown of Ach)
33
Drugs (2) that can *reverse* bradycardia
To *reverse* bradycardia we need to *inhibit M2* **Atropine** **Glycopyrrolate**
34
What are the effects of an M2 antagonist like atropine/ glycopyrrolate?
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
What do M3 agonists do *in the bronchioles*?
**M3 agonists**: found throughout the body besides the heart (pupil, salivary gland, bronchioles, GIT, bladder, uterus) * In bronchioles: **Induce bronchoconstriction** * Ex: methacholine
36
Name 3 types of M3 antagonists that can act in the bronchioles:
**Ipratropium** **Tiotropium** **Aclidinium** *These M3 antagonists will trigger bronchodilation to treat things like COPD*
37
Drugs to treat gastrointestinal motility include _ and _ which target _ receptor in the GIT
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
M3 receptors can be found in the glands (regulate secretions); Agonists include: Antagonists include:
M3 receptors can be found in the glands (regulate secretions); Agonists include: **pilocarpine** Antagonists include: **glycopyrrolate**
39
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
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
What is the effect of an M3 antagonist in the bladder?
**M3 antagonist** in the bladder would cause *urinary retention* * Ex: use **oxybutynin** and **tolterodine** to treat an overactive bladder
41
_ is a M3 agonist that causes the pupils to constrict
**Carbachol** is a M3 agonist that causes the pupils to constrict
42
_ is an M3 antagonist that causes the pupils to dilate
**Atropine** is an M3 antagonist that causes the pupils to dilate
43
Miosis means _
Miosis means **pupil constriction**
44
Mydriasis means _
Mydriasis means **dilation**
45
β1 agonists do what?
β1 agonists: stimulate AV/SA node --> increase HR --> increase CO
46
β1 antagonists are indicated for treatment of _ and _
β1 antagonists are indicated for treatment of **hypertension** and **angina**
47
β2 agonists do what?
β2 agonists: bronchodilation * ex: **albuterol, salmeterol, formoterol**
48
What does antagonizing the alpha1 receptor in the urethra do?
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
_ drug is an alpha1 agonist that leads to pupil dilation
**Phenylephrine** drug is an alpha1 agonist that leads to pupil dilation
50
Ritodrine and terbutaline are drugs used to stop preterm labor; they work by _
**Ritodrine** and **terbutaline** are drugs used to stop preterm labor; they work by **agonizing B2 receptors in the uterus** * Uterine relaxation
51
Vascular smooth muscle contains both **α1** and **β2** but the effect of _ usually dominates
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
**Clonidine** is an α2 agonist which is used to treat _
**Clonidine** is an α2 agonist which is used to treat **hypertension**
53
Side effects of pilocarpine:
Intended to increase salivation * Side effects: pupil constriction, diarrhea * All are M3 targets
54
Side effects of atropine:
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
Toxicities of parasympathomimetics:
DUMBBELS: **Diarrhea** **Urination** **Miosis** **Bradycardia** **Bronchoconstriction** **Emesis** **Lacrimation** **Salivation**
56
Side effects of tamsulosin:
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
Side effects of nadolol:
Nadolol is a beta blocker that is intended to block beta1 to decrease BP * Side effects: blocks B2 as well and can cause bronchoconstriction