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Therapeutics > Anticholinergics: Antimuscarinics > Flashcards

Anticholinergics: Antimuscarinics Flashcards

1
Q

Anticcholinergics

A

-bind to receptor and disrupt acetylcholine binding
-competitive ANTAgonists
-reversible

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2
Q

Effects of antimuscarinic agents

A

-block muscarinic receptor
-ganglia: little effect on actions of ACh at the NICOTINIC receptor
-CNS: widespread distribution of muscarinic receptors throughout brain

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3
Q

Atropine

A

-oldest antimuscarinic agent
-antagonist at M1, M2, M3
-can produce partial block (M1) only at relatively high doses

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4
Q

Antimuscarinics

A

-muscarinic receptor ANTAgonists
-competitive and reversible
-block ACh from binding

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5
Q

Atropine effect on exocrine glands

A

-decreased sweating and secretions
-preanesthetic

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6
Q

Atropine effect on eye

A

-mydriasis
-dilation

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7
Q

Atropine effect on cardiovasc

A

-increase heart rate
-no effect on BP
-treat arrhythmia

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8
Q

atropine effect on respiratory tract

A

-block of vagal bronchoconstriction

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9
Q

Atropine effect on bladder

A

-decrease tone
-constricted sphincter
-reduce frequency

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10
Q

Atropine effect on GI smooth muscle

A

-decrease motility and tone
-treat hypermobility

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11
Q

Atropine effect on CNS

A

-block all muscarinic receptors
-anti-motion sickness
-anti-parkinsons

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12
Q

Antimuscarinic classes

A

-tertiary amines
-quarternary amines

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13
Q

tertiary amine antimuscarinics

A

-atropine
-mainly used in ocular and CNS applications

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14
Q

Quarternary amine antimuscarinics

A

-anisotropine
-mainly used in GI tract and PERIPHERAL applications

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15
Q

Tertiary amine antimuscarinic classes

A

-belladonna alkaloids (long last)
-tertiary amine derivatives (short acting)
-tertiary amine derivatives (antiparkinson)

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16
Q

belladonna alkaloid drugs

A

-long lasting
-atropine
-scopolamine

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17
Q

tertiary amine derivative drugs (short acting)

A

-homatropine
-tropicamide

18
Q

tertiary amine derivative drugs (antiparkinson)

A

-benztropine (cogentin)
-trihexyphenidyl (artane)

19
Q

Quarternary derivatives of belladonna alkaloids drugs

A

-Ipratropium (atrovent)
-tiotropium (spiriva)

20
Q

belladonna alkaloids

A

-long lasting tertiary amines
-M1/M2/M3 non-selective
-treat GI and motion sick
-can affect CNS
-naturally occuring
-little bit of hallucinations

21
Q

need to know

A

acetylcholine structure

22
Q

Scopolamine

A

-3’ belladonna alkaloid
-higher CNS penetration than atropine= more drowsy and hallucinations
-highly lipophillic

23
Q

Scopolamine clinical use

A

-motion sickness
-oral or transdermal
-dry mouth, blurred vision, sedation side effects
-confusion and psychosis at high doses

24
Q

Short acting tertiary amines

A

-homatropine and tropicamide
-optical applications
-cycloplegia and mydriasis

25
Q

Homatropine

A

-short acting 3’ amine
-less toxic than tropicamide

26
Q

tropicamide

A

-short acting 3’ amine
-shorter duration than homatropine

27
Q

Benztropine (congentin)

A

-treat parkinson
-sedative activity
-combo therapy with L-DOPA in patients
-similar potency to atropine

28
Q

Ipratropium

A

-4’ amine
-M3 ANTAgonist
-block ACh-mediated constriction = open airways

29
Q

Ipratropium clinical use

A

-treat COPD sometimes asthma
-enhances therapeutic effect of B-adrenergic AGonists in COPD

30
Q

Combivent or Duoneb

A

-brand name for Ipratropium
-treat COPD

31
Q

Ipratropium problems

A

-few bc poor absorption
-toxic doses may cause hypotension (ganglionic block) or muscle weakness (neuromuscular block)

32
Q

tiotropium

A

-longer acting analog of Ipratropium

33
Q

antimuscarinic 4’ Amines for GI disorders

A

-glycopyrrolate
-propantheline bromide
-treat spasms and ulcers

34
Q

glycopyrrolate

A

-4’ amine
-pre-op to reduce secretions
-charged N makes crossing gut difficult

35
Q

Antimuscarinics for overactive bladder

A

-tolterodine
-“fenacin” (M3 selective)

36
Q

Tolterodine

A

-non-selective but favors M3 receptor
-treat overactive bladder

37
Q

“fenacin”

A

-newer M3 selective antagonists
-treat overactive bladder
-lower constipation and confusion

38
Q

Mirabegron

A

also a B3 agonist ?

39
Q

Antimuscarinic poisoning

A

-over 600 meds with antimuscarinic effects
-diphenhydramine, chlorprozamine, amitriptyline
-dry mouth

40
Q

Antimuscarinic poisoning treatment

A

-change meds/decrease dose
-sodium bicarb for QRS
-Benzos for delirium
-physostigmine (AChase inhibitor)

41
Q

physostigmine

A

-AChASE inhibitor
-treat antimuscarinic poisoning

Therapeutics (78 decks)

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