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PHRM 825 > ANS-5 > Flashcards

ANS-5 Flashcards

1
Q

Antimuscarinic agents are selective for ___, ___, and ___ receptors

A

M1, M2, M3

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2
Q

Antimuscarinic agents have little effect on ___

A

nicotinic receptors

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3
Q

Antimuscarinic agents are ____ antagonists

A

competitive

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4
Q

What is the problem with antimuscarinic agents such as Atropine?

A

lack of selectivity

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5
Q

Only ___ doses of Atropine can cause a partial block (M1) of the CNS

A

high

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6
Q

What are the 2 general classes of antimuscarinics?

A

tertiary amines and quarternary amines

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7
Q

antimuscarinic tertiary amines are mainly used on ___ and ___ applications

A

ocular, CNS

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8
Q

antimuscarinic quarternary amines are mainly used on ___ and ___ applications

A

GI tract, peripheral

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9
Q

What is this?

A

Atropine

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10
Q

What is this?

A

Anisotropine

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11
Q

T or F: Tertiary amines have good access to the CNS

A

True

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12
Q

Tertiary amines: Belladonna alkaloids (long acting)

A

Atropine and Scopolamine (Maldemar)

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13
Q

Tertiary amines: short acting derivatives

A

Homatropine and Tropicamide

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14
Q

Tertiary amines: Antiparkinson use

A

Benztropine (Cogentin) and Trihexyphenidyl (Artane)

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15
Q

Quaternary amines: Belladonna alkaloid derivatives

A

Ipratropium (Atrovent) and Tiotropium (Spiriva)

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16
Q

What is this?

A

Scopolamine (Maldemar)

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17
Q

Atropine and Scopolamine treat ___, ___, and ___

A

GI conditions, urinary conditions, and motion sickness

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18
Q

Compared to Atropine, Scopolamine has ___ CNS penetration

A

higher

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19
Q

Scopolamine is more ___philic than Atropine

A

lipo

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20
Q

Side effects of Scopolamine

A

dry mouth, blurred vision, and sedation

High doses: confusion and psychosis

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21
Q

Homatropine and Tropicamide are used in optical applications such as ___ and ___ because of the ___ duration of action

A

cycloplegia, mydriasis, short

Cycloplegia = paralysis of the ciliary muscle of the eye

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22
Q

Homatropine is ___ toxic; Tropicamide has a ___ duration of action

A

less, shorter

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23
Q

What is this?

A

Homatropine

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24
Q

What is this?

A

Tropicamide

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25
Q

Tertiary amines used for Parkinsons Disease have ___ activity

26
Q

___ is used as an adjunct therapy with L-DOPA in PD patients (to achieve better balance between dopaminergic and cholinergic neurotransmission)

A

Benztropine (Cogentin)

27
Q

What is this?

A

Benztropine (Cogentin)

28
Q

Ipratropium (Atorvent) clinical use

A

M3 antagonist used for COPD treatment (blocks bronchoconstriction). Occasionally used for asthma. Enhances effect of B-adrenergic agoinst in COPD

29
Q

Combivent/Duoneb is a combo of which two medications? (used to treat COPD)

A

ipratropium and albuterol

30
Q

What is this?

A

Ipratropium

31
Q

Quaternary amines for GI disorders

A

Glycopyrrolate amd Propantheline Bromide

Propantheline Bromide is not available in the US

32
Q

___ is often used pre-op to reduce secretions

A

Glycopyrrolate

33
Q

Why are quaternary amines good for GI?

A

positive charge makes it difficult to escape the gut

34
Q

What is this?

A

Glycopyrrolate

35
Q

Tolterodine (Detrol) is a antimuscarinic used for ____

A

overactive bladder (OAB)

36
Q

What is this?

A

Propantheline Bromide

37
Q

Tolterodine has no apparent selectivity for different muscarinic receptor subtypes; however therapeutically seems to act somewhat selectively on the ___ receptor

38
Q

What is this?

A

Tolterodine (Detrol)

39
Q

Proposed advantages of newer M3 receptor-selective muscarinic antagonists used to treat OAB

A

Lower incidence of constipation and confusion

40
Q

Examples of newer M3 drugs for OAB

A

Solifenacin (Vesicare) and Darifenacin (Enablex)

41
Q

What is this?

A

Solifenacin (Vesicare)

42
Q

What is this?

A

Darifenacin (Enablex)

43
Q

Antimuscarinic Poisoning Treatment

A
  • change medicine or decrease dose
  • supportive care (sodium bicarbonate for QRS/arrhythmias, benzodiazepines for agitation/delirium)
  • physostigmine (AChE inhibitor)
44
Q

Neuromuscular blocking agents look like ___

45
Q

What is this?

A

Succinylcholine

46
Q

What is this?

A

Tubocurarine

47
Q

Blocking the Nicotinic Receptor: What drug has a non-depolarizing blockade and acts as a “normal” antagonist?

A

Tubocurarine

48
Q

Blocking the Nicotinic Receptor: What drug has a depolarizing blockade? (First activates, then blocks)

A

Succinylcholine

49
Q

Depolarizing Blockade definition (nicotinic)

A

agonist remains bound to receptor. Persistent depolarization means fast Na+ channels cannot reset to active state.

50
Q

Tubocurarine (Curare) mechansim

A

competitive antagonist for nicotinic receptors producing a non-depolarizing blockade

51
Q

Tubocurarine (Curare)
clinical use

A

skeletal muscle relxation during anesthesia (useful for intubation)

52
Q

Succinylcholine (Suxamethonium = SUX) mechanism

A

At first, acts as an nicotinic receptor agonist (initial depolarization). But it doesnt dissociate from the receptor and the presistent depolarization does not allow receptor to reset.

53
Q

What metabolizes Succinylcholine?

A

Plasma Butyrylcholinesterase

slower than AChE breaking down ACh

54
Q

T or F: Choline increases BP

55
Q

Succinylcholine (SUX) clinical use:

A

skeletal muscle relaxation during anesthesia (useful for intubation and electro-convulsant therapy)

56
Q

Problems with Succinylcholine (SUX)

A

muscle soreness (avoid in hyperkalemia - cardiac arrest), malignant hyperthermia, atypical cholinesterases (prolonged cholinesterases)

57
Q

____ inhibits the release of ACh

A

Botulinum Toxin

58
Q

Botulinum Toxin clinical use

A

uncontrolled muscle spasms (dystonias), cerebral palsy, ocular muscle spasms, anal fissures, excessive sweating (hyperhidrosis)

59
Q

Problems with Botulinum Toxin

A

spreads from injection site

60
Q

Hexamethonium mechanism

A

Antagonist at nicotinic receptors in autonomic ganglia thus blocking all SNS and PSNS activity

61
Q

What was the original use of Hexamethonium and why is it no longer used?

A

hypertension, but no longer used due to adverse effects

PHRM 825 (49 decks)

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