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Pharm block 1 > 06,08,09 PNS, Adrenergics, Cholinergics > Flashcards

06,08,09 PNS, Adrenergics, Cholinergics Flashcards

(68 cards)

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1
Q

Bethanechol

A
  • direct acting cholinergic agonist
  • stimulate atonic bladder/bowel
  • “Bethany needs to activate Bowels and Bladder”
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2
Q

Pilocarpine

A
  • direct acting cholinergic agonist
  • ophthalmology: induce miosis, cycloplegia. Tx glaucoma
  • Effects: “You cry, sweat, and drool on your Pilo-carpine”
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3
Q

Neostigmine

A
  • AchE-I (indirect cholinergic agonist)
  • tx for Myasthenia gravis
  • no CNS access
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4
Q

Physostigmine

A
  • AchE-I (indirect cholinergic agonist)
  • tx for atonic bowel/bladder, glaucoma
  • yes, CNS access
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5
Q

Edrophorium

A
  • AchE-I (indirect cholinergic agonist)

- dx for Myasthenia gravis

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6
Q

Sarin

A
  • AchE-I (organophosphate–irreversible indirect cholinergic agonist)
  • Weaponized
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7
Q

Malathion

A
  • AchE-I (organophosphate–irreversible indirect cholinergic agonist)
  • insecticide
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8
Q

Pralidoxime

A
  • AchE-I (weak)
  • Used to reactivate AchE after organophosphate poisoning because it can dispace organophosphates from AchE before they undergo aging.
  • High doses: cholinergic side effects
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9
Q

Cholinergic side effects/toxicity

A

SLUDGE:

  • Salivation
  • Lacrimation
  • Urination
  • Defecation
  • GI upset
  • Emesis

Also: bradycardia, hypotension, blurry vision

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10
Q

Atropine

A
  • antimuscarinic
  • tx for spastic disorders of GI/urinary tract
  • mydriasis
  • decrease respiratory secretions before surgery
  • tx for organophosphate poisoning
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11
Q

Tropicamide

A
  • antimuscarinic

- mydriasis and glaucoma tx

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12
Q

Scopolamine

A
  • antimuscarinic

- tx motion sickness

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13
Q

Ipratropium

A
  • antimuscarinic

- tx COPD

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14
Q

Darifenacin

A
  • antimuscarinic

- tx overactive bladder

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15
Q

Oxybutynin

A
  • antimuscarinic

- tx overactive bladder

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16
Q

Glycopyrrolate

A
  • antimuscarinic

- used to block PS-mimetic effects of AchE-I when used to reverse NMJ blockade

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17
Q

Categories of cholinergic agonists

A
  1. Direct
  2. Indirect–reversible
  3. Indirect–irreversible (organophosphates)
  4. Reactivation of AchE
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18
Q

Categories of cholinergic antagonists

A
  1. Antimuscarinics
  2. Ganglionic blockers
  3. NMJ blockers (non-depol and depol)
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19
Q

Pancuronium

A
  • NMJ blocker (cholinergic anatagonist)
  • non-depol
  • muscle relaxant before surgery/intubation
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20
Q

Atacurium

A
  • NMJ blocker (cholinergic anatagonist)
  • non-depol
  • muscle relaxant before surgery/intubation
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21
Q

Rocuronium

A
  • NMJ blocker (cholinergic anatagonist)
  • non-depol
  • muscle relaxant before surgery/intubation
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22
Q

Vecuronium

A
  • NMJ blocker (cholinergic anatagonist)
  • non-depol
  • muscle relaxant before surgery/intubation
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23
Q

Succinylcholine

A
  • NMJ blocker (cholinergic anatagonist)
  • depolarizing
  • Rapid action means preferred muscle relaxant prior to intubation.

-worry about lack of pseudocholinesterase (genetic polymorphism), leads to side effects

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24
Q

Categories of Adrenergic agonists

A
  1. Direct–catecholamines
  2. Direct–non-catecholamines
  3. Indirect
  4. Mixed
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25
Categories of Adrenergic Antagonists
1. alpha blockers--nonselective, selective 2. beta blockers--gen 1,2,3 3. Indirect
26
Epinephrine (Epi) - pulse - systolic - diastolic - peripheral resistance
- A1, A2, B1, B2 agonist - pulse up, BP up/down, peripheral down - tx for anaphylactic shock
27
Norepinephrine (NE) - pulse - systolic - diastolic - peripheral resistance
- A1, A2, B1 agonist - pulse down (b/c reflexive bradycardia from hypertension--vagal), BP up/up, peripheral up - tx for shock
28
Isoproterenol - pulse - systolic - diastolic - peripheral resistance
- B1, B2 agonist - pulse up, BP up/down, peripheral down - no clinical use
29
Dopamine (DA)
- A1, B1 agonist, also dopaminergic 1. renal dose, low--increase blood flow to kidneys (dopamine receptors) 2. cardiac dose, med--increase B1 effect 3. pressor dose, high--increase BP, A1 effect
30
Dobutamine
-B1 agonist
31
Methyldopa
- A2 agonist - acts on central CNS receptors, psychoactive - tx for HTN and gestational HTN
32
Why is dopamine better than NE in tx of shock?
Both increase BP which is important. However, DA increases blood flow to kidneys and splanchnic areas, while NE constricts blood flow there, risking renal problems.
33
Asthma attack in the ER: you have no Epi available. Can NE be used instead?
No. NE is poor B2 agonist.
34
Phenylephrine
- A1 agonist - nasal decongestant - induce mydriasis
35
Clonidine
- A2 agonist - acts on CNS receptors, psychoactive - tx for HTN, ADHD
36
Albuterol
- B2 agonist | - short acting bronchodilator
37
Salmeterol
- B2 agonist | - long acting bronchodilator
38
Amphetamine
- Indirect adrenergic agonist, with A,B, and CNS effects - induces NE release - tx for ADHD, narcolepsy
39
Tyramine
- Indirect adrenergic agonist, with A,B, and CNS effects - Dietary tyramine found in fermented foods (eg aged cheese) - If eaten, induces NE release in pts that are taking MAO-I. Give phentolamine to pts that eat tyramine-rich foods. -"tiramisu" -- food
40
Ephedrine
- Mixed adrenergic agonist - A, B, CNS effects - nasal decongestant
41
Pseudoephedrine
- Mixed adrenergic agonist - A, B, CNS effects (A1 major effect) - nasal decongestant
42
A1 receptors
- peripheral vasconstriction - mydriasis - increased closure of bladder internal sphincter
43
A2 receptors
- inhibition of NE release (negative feedback on presynaptic neuron) - inhibit Ach release - inhibit insulin release
44
B1 receptors
- Positive Inotropic effect - positive chronotropic effect - Kidneys--release renin - lipolysis
45
B2 receptors
- bronchodilation - Decrease peripheral resistance (skeletal m) - gluconeogenesis, glycogenolysis, glucagon release - relax uterine smooth m
46
Catecholamines vs non-catecholamines: - effect time - effect duration - oral? - CNS access
- Catecholamines: rapid effect, short duration, no oral, no CNS access (exception to last 2 is methyldopa) - non-catech: slower effect, long duration (not metab by COMT and MAO), yes oral, yes CNS access
47
Catecholamine synthesis pathway
``` Tyrosine ---(Tyr OHlase) DOPA ---(DOPA decarboxylase) DA ---(DA beta-OHlase) NE ```
48
Enzymes that metabolize catecholamines
1. MAO (monoamine oxidase). found within neuron, so NE must enter from synpase through NET first. 2. COMT (Catechol-O-methytransferase). found in synapstic space at postsynaptic membrane. Oxidizes catecholamines.
49
Phenoxybenzamine
- A1, A2 blocker, irreversible | - tx pheochromocytoma
50
Phentolamine
- A1, A2 blocker, reversible - tx pheochromocytoma - give to pts on MAO-I that eat tyramine rich foods
51
Prazosin
- A1 blocker | - tx HTN, also BPH
52
Tamsulosin
- A1 blocker | - tx BPH
53
Propranolol
-B1, B2 blocker. gen1
54
Timolol
- B1, B2 blocker. gen1 - tx for glaucoma -"Tim Wang with increased ocular pressure from climbing"
55
Atenolol
-B1 blocker, gen2
56
Metoprolol
-B1 blocker, gen2
57
Carvedilol
-A1, B1, B2 blocker, gen3
58
Labetalol
-A1, B1, B2 blocker, gen3
59
Reserpine
- Indirect adrenergic antagonist | - acts on VMAT-2, prevents NE from entering vesicle
60
Guandedrel
- Indirect adrenergic antagonist | - prevents NE release from vesicles
61
Guanethidine
- Indirect adrenergic antagonist | - prevents NE release from vesicles
62
Cocaine
- Indirect adrenergic agonist | - acts on NET so that NE cannot uptake into presynaptic cell
63
Botulinum
-Ach vesicle release inhibited.
64
VMAT2
- vesicular monoamine transporter 2 - transports NE into vesicles. - blocked by reserpine
65
NET
- NE transporter - allows uptake of NE in synapse back into presynaptic neuron. - inhibited by cocaine
66
ENT
- Extraneuronal transporter - allows uptake of NE into postsynaptic neuron - 5% of NE go this pathway
67
AchE
acetylcholinesterase: hydrolyzes Ach into acetate and choline. Choline uptake into presynaptic neuron.
68
Tyrosine hydroxylase
Catalyzes: Tyrosine to DOPA | -rate limiting step in catecholamine synthesis

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