Anticholinergics Flashcards

1
Q

2 types of anticholinergics

A

antimuscarinics and ganglionic blockers

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2
Q

action of muscarinic AChR antagonists ( antimuscarinics)

A

interrupts parasympathetics influence in various tissues

  • predominant autonomic tone is parasympathetic ( except: vasculature and sweat glands)
  • blocking mAChR-> premits sympathetic influence to become predominant
  • effects will be typical of sympathetic activity
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3
Q

how do ganglionic blockers act

A

antagonising the neuronal nAChRs present on the primary ganglionic cell in all autonomic ganglia ( but arent all antagonists)
- effects are sympathetic-like ( not sweat glands or vasculature) due to blocking all autonomic influence

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4
Q

pharm effects of prototypical anti-muscarinic atropine - on ocular a

A

ocular-> 1. relaxes iris sphinicter, symp tone predominates on radial muscle

  1. blocks accommodation -relaxes ciliary muscle-> increases tension on ligaments -> flattens lens
  2. inhibits lacrimation
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5
Q

pharm effects of prototypical anti-muscarinic atropine - on cardiac

A
  1. standard dose increase heart rate and atrioventricular conduction by blocking vagal input
  2. very low doses may initially decrease hr by first blocking presynaptic receptors
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6
Q

pharm effects of prototypical anti-muscarinic atropine - on respiratory

A
  1. bronchial smooth muscle relaxation and dilation

2. inhibit secretions

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7
Q

pharm effects of prototypical anti-muscarinic atropine - on GI

A
  1. decreases lower esophageal muscle tone
  2. relaxes GI tones, prolonging intestinal transit time
  3. inhibits gastric acid secretions
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8
Q

pharm effects of prototypical anti-muscarinic atropine - on urinary

A
  1. relaxes detrusor muscle of the bladder causing urinary retention
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9
Q

pharm effects of prototypical anti-muscarinic atropine - on CNS

A

1, atropine and scopolamine are tertiary amines

  1. scopolamine is more sedating than atropine
  2. atropine-> 1st stimulation followed by sedating effect
  3. high doses can cause confusion and or hallucinations

other: inhibits sweating and could possibly lead to hyperthermia-> causes cutaneous vasodilation

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10
Q

major clinical uses of atropine

A

long lasting mydriasis, pharm path to treat amblyopia, cycloplegia , sinus bradycardia and av block, decrease of salivary and respiratory secretions -> prevents airway obstruction
, intestinal spasms and pain , decrease gastric acid secretions, reversal of muscarinic or AChE inhibitor poisoning, prevention of muscarinic side effects in pts receiving AChE inhibitors and neostigmine to reverse nerve block, mixed with diphenoxylate (opioid agonist) its an anti-diarrheal

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11
Q

scopolamine

A

anti-mus

motion sickness, side effect - drowsiness

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12
Q

tropicamide , cyclopentolate, homatropine

A

anti-mus
fast but short acting mydriatic agent
may be combined with alpha adrenergic agonist

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13
Q

ipratropium

A

anti-mus
quaternary amine-> inhalled
bronchodilator
COPD

TIOTROPIUM- similar but longer acting

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14
Q

tolterodine

A

ant-mus
managment of overactive bladder ( increased freq, nocturia, incontinence)
-fewer side effects_> dry mouth and blurred vision
contraindicated for individuals w/ narrow-angle glaucoma

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15
Q

dicyclomine

A

anti-mus
releaxes intestinal smooth muscle
IBS-> symptoms

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16
Q

glycopyrrolate

A

anti-mus

  • low doses preferentially inhibit secretions for preop
  • prevents excessive generalized sweating
  • prevention of muscarinic side effect in pt receiving neostigmine to reverse neuromuscular block
17
Q

benztropine

A

relieve extrapyramidal symptoms in parkinson’s or in pt taking antipsychotics

18
Q

adverse actions of anti-mus

A

dry mouth , blurred vision (mydriasis and cycloplegia) , hot, flushed skin( anhidrosis and cutaneous vasodilation) constipation difficulty in urinating, tachycardia , CNS effects : confusion, sedation, delirium

“dry as a bone, red as a beet, hot as a hare, blind as a bat, mad as a hatter”

19
Q

classes of drugs which some members have antimus activity

A

antihistamines - diphenhydramine
antidepressants - tricyclics - amitriptyline
phenothiazine antipsychotics- chlorpromazine

20
Q

depolarizing ganglionic blockers

A

nicotinic agonist

  • act by initially activating the ganglionic nACh receptors - followed by receptor blockade resulting from persistent depolarization
  • organophosphate cholinesterase inhibitors may cause some degree of depolarizing ganglionic block
21
Q

nicotine

action, basic pharm effects

A
  1. stimulation of autonomic ganglia followed by ganglionic blockade ( dose-dependent)
  2. stim of adrenal medulla (possible significant secretion of epi)
  3. stim of CNS: altering response, change in respiration
22
Q

symptoms of nicotine toxicity

A

GI-> nausea, vomiting, salivation, diarrhea
cardio-> tachy/brady, hypo/hypertension, arrhythmia
CNS-> lethargy, confusion, seizures, coma
peripheral nervous system-> diaphoresis
muscles-> tremors, fasciculations, weakness, paralysis
endocrine-> increase epi release

23
Q

non-depolarizing ganglionic blockers

A

act by blocking nACh receptors in all autonomic ganglia

  • reduce the most prominent autonomic tone in each organ
  • curare compounds use in the past as NM blockers cause non-depolarizing ganglionic blocks as well
24
Q

hexamethonium (C6)

A

antagonist at nAChR at ganglion

  • 1st effective antihypertensive (not used anymore)
  • poor absorption and autonomic side effects led to discontinuation of its use
25
Q

mecamylamine

A

antagonist at nAChR at ganglion

  • can be used to improve GI absorption
  • recent interest in its use for tourette syndrome
26
Q

effects of ganglionic blockade on and predom tone

  1. arterioles
  2. veins
  3. heart
  4. iris
  5. ciliary muscle
  6. GI tract
  7. urinary bladder
  8. salivary glands
  9. sweat glands
A
  1. arterioles -s-vasodilation and increase peripheral blood flow
  2. veins -s- dilation, peripheral pooling , decrease return decrease CO
  3. heart- p- tachy
  4. iris-p- mydriasis
  5. ciliary muscle-p-cycloplegia (loss of accomodation)
  6. GI tract-p-decrease tone and motility, constripation
  7. urinary bladder- p- urinary retention
  8. salivary glands -p-xerostomia
  9. sweat glands -s- anhidrosis ( cholinergic)
27
Q

atropine
action
selected uses

A

antagonist at all mAChRs

revere muscarinic or AChE inhibitor poisoning, long lasting pupil dilation and antidiarrheal

28
Q

scopolamine

action and uses

A

antagonist to all mAChRs

motion sickness

29
Q

tropicamide
cyclopentolate
homatropine

A

antagonist to all mAChRs - hort acting

pupil dilation

30
Q

Ipratropium
tiotropium
action and uses

A

antagonist at mAChRs

quaternary amine ; local action
newer alt: tiotropium
COPD

31
Q

tolterodine

action and uses

A

antagonist at bladder mAChRs

overactive bladder

32
Q

dicyclomine

action and uses

A

antagonist at GI mAChRs

irritable bowel

33
Q

Glycopyrrolate

action and uses

A

antagonist at mAChR

secretion, sweating, muscarinic overshoot after cholinesterase inhibition

34
Q

benztropine

action and uses

A

lipid soluble mAChR antagonist

extra pyramidal effects of parkinsons

35
Q

mecamylamine

action and uses

A

antagonist at nAChR at ganglion

improves GI absorption , tourette syndrome

36
Q

hexamethonium

action and uses

A

antagonist at nAChR at ganglion

prevents baroreceptor reflex