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Old Pharmacology test 2 > Muscarinic/Cholinergic Agents > Flashcards

Muscarinic/Cholinergic Agents Flashcards

1
Q

Nicotinic Ach receptor agonist

A

Nicotine

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2
Q

Nicotinic Ach receptor antagonist

A

Mecamylamine, Curare(will kill you)

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3
Q

Muscarinic ACh receptor agonist(s)?

A

Muscarine, Pilocarpine(glaucoma), Bethanechol(GI Bloating)

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4
Q

Muscarinic ACh receptor antagonist?

A

Atropine (for bradycardia)

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5
Q

Drug that blocks the choline transporter(HAChT)

A

hemicholium-3

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6
Q

Drug that blocks Ach uptake into vesicles

A

vesamicol

-inhibits effects of ACH

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7
Q

Drugs that block vesicular release(exocytosis)

A

Botulinum toxin or tetanus toxin

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8
Q

Anti-AChE (AChE Inhibitors) Drug Names & (Categories)

A

Edrophonium (simple alcohol) aka Tensilon
Physostigmine & Neostigmine (Carbamate)
Echothiophate & Sarin Gas (Organophosphate)

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9
Q

Where are cholinergic receptors found in the autonomic nervous system?

A

ALL autonomic preganglionic terminals

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10
Q

Sympathetic postganglionic terminals

A

Sweat glands

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11
Q

dominant tone is usually controlled by which division of the ANS?

A

Parasympathetic nervous system

-cholinergic control

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12
Q

What organ is under cholinergic sympathetic control?

A

sweat glands

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13
Q

What organ has sympathetic(adrenergic) dominant tone?

A

Blood vessels

-control of blood pressure

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14
Q

major physiologic effects of Ach on Parasympathetic nervous system

A 
"SLUDGE"
S- salivation
L- lacrimation
U- Urinary incontinence
D- Diarrhea
G- Gastrointestinal cramps
E- Emesis

“Rest & Digest”

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15
Q

Agonist

A

A drug that mimics the effects of a neurotransmitter

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16
Q

Antagonist

A

A drug that opposes or blocks the effects of a neurotransmitter

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17
Q

Prototypic muscarinic agonist

A

Muscarine

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18
Q

Prototypic muscarinic antagonist

A

Atropine

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19
Q

What activates nicotinic and muscarinic (cholinergic) receptors?

A

Binding of ACH

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20
Q

How do nicotinic and muscarinic receptors differ?

A
  • Pharmacology
  • Receptor structure
  • Signal transduction mechanism
  • tissue localization
21
Q

nicotinic receptor

A
  • Ligand gated Ion channel, -Always excitatory

- Ach

22
Q

muscarinic receptor

A
  • GPCR(metabotropic)
  • excitatory or inhibitory
  • Ach
23
Q

Muscarinic receptor subtypes M1,M3, M5

A

mediate excitation responses through the activation of the enzyme phospholipase C

24
Q

M2 and M4 Muscarinic receptor subtypes

A

mediate inhibition of cellular activity

25
Q

M1,M3,M5 Muscarinic subtype responses

A

Formation of IP3(second messenger inositol triphosphate and DAG(diacylglycerol); inreased intracellular calcium

26
Q

M2 & M4 Muscarinic subtype responses

A
  • Opening of potassium channels

- Inhibition of adenylyl cyclase, which decreases production of cyclic AMP, thereby decreasing cellular activity

27
Q

Where are nicotinic receptors located in the peripheral nervous system?

A
  • neuromuscular junction
  • all autonomic preganglionic terminals
  • adrenal medulla
28
Q

Where are muscarinic receptros found in the peripheral nervous system?

A

parasympathetic post-ganglionic smooth muscle, cardiac muscle * gland cells
-sympathetic post ganglionic sweat glands

29
Q

What type of receptor is concentrated in the brain stem?

A

Muscarinic>nicotinic

subtypes in the brain: M4(inhibitory), M5(excitatory)

30
Q

What are parasympathomimetics?

A

Muscarinic receptor agonists

31
Q

systemic effects of muscarinic receptor agonists

A

“SLUDGE”

eye:pupillary constriction,ciliary muscle contraction for near vision

Lungs:bronchoconstriction

Heart: Decreased HR and conduction

GI, GU: Increased motility, secretion, contraction of bladder, relaxation of sphincter

Increased sweat/salivation

Vasodilation

32
Q

How do muscarinic receptor agonists cause vasodilation without parasympathetic innervation?

A
  • M3 indirectly caues vasodilation
  • Paradoxical effect
  • Activation of M3 receptors on endothelial cells by acetylcholine releases Nitric Oxide which activates Guanyl cyclase, resulting in an increase of cyclic GMP which causes relaxation of vascular smooth muscle (or vasodilation)
33
Q

Therapeutic uses of muscarinic agonists

A
  • Glaucoma: Decreases intraocular pressure
  • Post-op/post-partum abdominal distention & gastric atony: stimulates smooth muscle of th GI tract and urinary bladder
  • Used to test for antimuscarinic drug poisoning(atropine intoxiation,tricyclic antidepressant OD)
34
Q

Muscarinic agonist contraindications

A
  • asthma(bronchoconstriction)
  • acid-peptic dz(^gastric secretion)
  • hyperthyroidism(Afib)
  • Coronary insufficiency
35
Q

Prototypical muscarinic receptor antagonists

A
  • Atropine

- Scopolamine (scopolamine has prominent CNS effects)

36
Q

what type of antagonism are muscarinic receptor antagonists?

A

Competitive antagonists

  • compete with Ach for muscrinic receptors @ target organs and in CNS
  • prevent Ach from binding
37
Q

Systemic effects of muscarinic receptor antagonists

A
  • opposite of agonists
  • “sympathomimetic effects”
  • block parasympathetic effects
  • pupillary dilation
  • paralysis of accomodation
  • decreased tone/sphincter constriction
  • transient decrease in HR- no change in BP( by reflex action of baroreceptors)
  • blocks salivary/bronchial/gastric secretions/sweating
  • decrease parkinsonian tremor and prevent motion sickness
38
Q

Organs most sensitive to atropine?

A

salivary glands
bronchial glands
sweat glands

39
Q

Muscarinic antagonist therapeutic uses

A

-motion sickness
-GI disorders(hypermotility & peptic ulcer dz)
-used to dilate pupils
-COPD/Asthma
-Overactive bladder
-parkinsonian tremors
-

40
Q

muscarinic antagonist contraindications

A

glaucoma, elderly males(bph)

41
Q

symptoms of anticholinergic syndrome

A 
"Dry as a bone"
"Red as a beet"
"Blind as a bat"
"Hot as a furnace"
"mad as a hatter"
42
Q

treatment for anticholinergic syndrome

A

Physostigmine

43
Q

Depolarizing Neuromuscular Blocker Drugs

A

Succinylcholine (could decrease HR)

Any Anti-AChE at High Doses could Cause this effect.

44
Q

Non-Depolarizing Neuromuscular Blocker Drugs (competitive nicotinic antagonists)

A 
D-Tubocurarine (prototype) (may increase histamines)
Mivacurium (may increase histamines)
Rocuronium
Cisatracurium (no histamine effect)
Doxacurium (no histamine effect)
Pancuronium (may increase HR)
Gallamine (may increase HR)
45
Q

Benztropine

A

Tx Parkinsons, passes BBB, Musc. Antagonist

46
Q

Pralodoxime (2-Pam)

A

Sarin Gas Antidote, give Atropine at the same time for antiparasympathetic effects.

47
Q

Myesthenia gravis Dx & Tx

A

Tensilon, physostigmine, remove thymus

48
Q

Procanimide

A

High Lupus Rates with 80% early blood work markers.

49
Q

Physostigmine(Category & uses)

A

Anti-AChE, Carbamate, Alzheimer’s, BBB, M.G., Glaucoma, Atropine Toxicity.

Old Pharmacology test 2 (2 decks)

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