Pharmacology of the Autonomic Drugs Flashcards

1
Q

Which division of ANS has long preganglionic neurons?

A

Psymp

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2
Q

Preganglionic symp nt?

A

ACh

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3
Q

Preganglionic psymp nt?

A

ACh

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4
Q

Postganglionic symp nt?

A

NE

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5
Q

Postganglionic psymp nt?

A

ACh

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6
Q

Symp effects on eye

A
  • Far focus
  • Contraction of radial m→mydriasis (dilation)
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7
Q

Psymp effects on eye

A
  • Contraction of circ. sphincter m→miosis (constriction)
  • Contraction of ciliary m→ short focus
  • More tear production
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8
Q

Symp effects on Digestive system

A
  • Less secretion and motility
  • More sphincter tone
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9
Q

Psymp effects on digestive system

A
  • More secretion and motility
  • Less sphincter tone
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10
Q

Symp effects on heart

A
  • Increase HR
  • Increase contraction force
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11
Q

Psymp effects on heart

A
  • Decrease HR
  • Decrease force
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12
Q

Symp effects on blood vessels

A
  • Muscle vessels relax
  • Skin and gut vessels constrict
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13
Q

Psymp effects on blood vessels

A
  • Relaxes most
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14
Q

Symp effects on lungs

A

Relaxes bronchial smooth m

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15
Q

Psymp effects on lungs

A

Constricts bronchial smooth m

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16
Q

Symp effects on reproductive organs

A
  • Relaxes blader
  • Ejaculation (symp=shoot)
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17
Q

Psymp effects on reproductive organs

A
  • Contracts bladder
  • Erection (Psymp=point)
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18
Q

Symp effects on metabolism

A

Increase in blood glucose

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19
Q

Psymp effects on metabolism

A

Decrease in blood glucose

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20
Q

ACh removal

A

AChE

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21
Q

NE removal

A
  1. Reuptake
  2. COMT (catecholomethyltransferase)
  3. MAO (monoamine oxidase)
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22
Q

Subtypes of cholinergic receptors and what they alter

A

Nicotinic receptor: Alterted ion channel (ionotropic)

Muscarinic receptor: altered metabolism (metabotropic)

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23
Q

What branch of the ANS do cholinergic agents affect and what are their effects??

A

Primarily Psymp

Miosis

Increased in tear, sweat, and saliva

Decrease in bronchiole smooth m and HR

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24
Q

Muscarine

A

Direct muscarinic agonist

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25
Q

Pilocarpine

A

Direct muscarinic agonist

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26
Q

Bethanechol

A

Direct muscarinic agonist

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27
Q

Nicotine

A

Direct nicotinic agonist

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28
Q

Varenicline

A

Direct partial nicotinic agonist

Binds to receptor but does not fully activate it. Thus prevents others from binding.

Anti-smoking drug b/c binds but does not have effects of nicotine

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29
Q

What are the two agonists that act on nicotinic and muscarinic receptors?

A

ACh

Carbachol

30
Q

How do indirect acting cholinergic agonists work and what are their effects?

A

Inhibit AChE

Similar to direct cholinergic agonists:

Miosis

Increased in tear, sweat, and saliva

Decrease in bronchiole smooth m and HR

But also affect muscle

31
Q

Physostigmine

A

Indirect cholinergic agonist

Lasts for several hours

Inhibit AChE

32
Q

Neostigmine

A

Indirect cholinergic agonist

Lasts for several hours

Inhibit AChE

33
Q

Demecarium

A

Indirect cholinergic agonist

Lasts for several hours

Inhibit AChE

34
Q

Echothiophate

A

Indirect cholinergic agonist

Lasts for 100s hours

Phosphorylates AChE

35
Q

Edrophonium

A

Indirect cholinergic agonist

Doesn’t last very long

Inhibit AChE

36
Q

What are indirect cholinergic agents used to treat?

A

Glaucoma

Myasthenia Gravis

Sjrogens Syndrome

Alzheimers (not very effective)

37
Q

Donepezil

A

Indirect cholinergic agonist

Alzheimer’s tx

38
Q

Tacrine

A

Indirect cholinergic agonist

Alzheimer’s tx

39
Q

Pralidoxime

A

If given early can reduce any perm. damage caused by organophosphate AChE inhibitors

40
Q

Malathion

A

Insecticide-cholinergic agonist

Irreversible AChE inhibitors

41
Q

Sarin

A

Nerve gas-direct cholinergic agonist

Irreversible AChE inhibitors

42
Q

Toxicities of cholinergic agonist

A

Diarrhea

Urination

Miosis

Bradycardia

Bronchoconstriction

Excitation of CNS*

Lacrimation

Salivation

*Paralysis, seizures, atoxia, amnesia

43
Q

Atropine

A

Antimuscarinic agent

Blocks muscarinic receptor

Lasts 7-10 days

44
Q

Scopolamine

A

Antimuscarinic agent

Blocks muscarinic receptor

Lasts 3-7 days

45
Q

Homatropine

A

Antimuscarinic agent

Blocks muscarinic receptor

Used to dilate pupils

46
Q

Cyclopentolate

A

Antimuscarinic agent

Blocks muscarinic receptor

Used to dilate pupils

47
Q

Tropicamide

A

Antimuscarinic agent

Blocks muscarinic receptor

Used to dilate pupils

48
Q

Ipratropium

A

Antimuscarinic agent

Blocks muscarinic receptor

49
Q

Side effects of antimuscarinic agents

A

Mydriasis

Inhibits ciliary m→loss of accomodation→virtually blind

Less tear production

Bronchodilation

Dry mouth

Less gastric motility and secretion (constipation)

Urinary retention

Less sweating

Higher HR

Psychosis

“Mad, blind, dry, red, hot”

50
Q

Succinylcholine

A

Direct nicotinic agonist

Antinicotinic agent-Depolarizing neuromuscular blocker

Long duration of action compared to acetylcholine

Initially activates receptor, eventually muscle hyperpolarization then paralysis

51
Q

Non-depolarizing neuromuscular blockers that are antinicotinic agents are derived from?

A

curare

52
Q

Pancuronium

A

Antinicotinic agent

non-depolarizing neuromuscular blockers

53
Q

atracurium

A

Antinicotinic agent

non-depolarizing neuromuscular blockers

54
Q

Rocuronium

A

Antinicotinic agent

non-depolarizing neuromuscular blockers

Most common one

55
Q

Sugammadex

A

Reverses block by rocuronium by binding directly

56
Q

Botulinum toxin type A

A

Inhibitor of ACh release

Cosmetically now

Originally for muscle spasms:

  • Tics
  • Strabismus
  • Nystagmus
57
Q

Sympathetic adrenoceptor subtypes

A

alpha 1: contract vascular smooth m–increase HR

alpha 2: activate presynaptic nerve terminals in CNS

Beta 1: increase HR and contraction force

Beta 2: relaxation of resp. vascular smooth m.

58
Q

Epinephrine

A

Works on all adrenergic receptors

Causes increased HR, etc. etc.

59
Q

Phenylephrine

A

Adrenergic agonist

Activates alpha1 receptors

Tx: congestion

Taken intranasally

60
Q

Tetrahydrozoline (Visine)

A

Adrenergic agonist

Activates alpha1 receptors

Tx: congestion

Taken intranasally

61
Q

Naphazoline

A

Adrenergic agonist

Activates alpha1 receptors

Tx: congestion

Taken intranasally

62
Q

Clonidine

A

Adrenergic agonist

Activates alpha2 receptors

Decrease symp outflow from CNS

Tx: hypertension

Other analogs used for glaucoma (Decrease pressure)

63
Q

alpha-methyl NE

A

Adrenergic agonist

Activates alpha2 receptors

Decrease symp outflow from CNS

Tx: hypertension

Other analogs used for glaucoma (Decrease pressure)

64
Q

Agents that activate beta1 receptors

A

NE

Dobutamine

65
Q

Agents that activate B2 receptors

A

“Nols and rols”

Metaproterenol

Terbutaline

Fenoterol

Albuterol

Tx: asthma

Causes bronchodilation

66
Q

What induces the release of NE from nerve terminals?

A

Indirect acting amines:

Amphetamine, methamphetamine

Tyramine

Phenylpropanolamine

Pseudoephedrine

67
Q

Prazosin

A

Adrenergic antagonist

alpha1 receptor blocker

Tx: hypertension

68
Q

Alpha 1 receptor blockers are used to treat?

A

Hypertension

Benign prostatic hypertrophy

69
Q

Specific B1 receptor blockers

A

“olol”s

Metoprolol

Acebutolol

Nebivolol

Atenolol

Esmolol

Alprenolol

These decrease HR

70
Q

Non specific B1 and B2 blockers

A

Propanolol

Timolol

Levobunolol

Certeolol

Metipranolol

71
Q

Phenoxybenzamine

A

Adrenergic antagonist

alpha1 receptor blocker

Tx: hypertension