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CPR Pharmacology > Cholinergic drugs > Flashcards

Cholinergic drugs Flashcards

1
Q

What are the direct-acting cholinomimetics?

A

ACh
Bethanechol
Carbachol
Cevimeline
Methacholine
Pilocarpine
Varenicline (Chantix)

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2
Q

What are the common cholinesterase inhibitors?

A

Ambenonium
Donepezil
Echothiphate
Edrophonium
Galantamine
Neostigmine
Pyridostigmine
Rivastigmine
Tacrine

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3
Q

What is the common cholinesterase regenerator?

A

Pralidoxime

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4
Q

What antimuscarinic drugs are used for motion sickness?

A

Scopolamine

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5
Q

What antimuscarinic drugs are used for tx of GI disorders?

A

Atropine
Dicyclomine
Glycopyrrolate
Hyoscyamine

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6
Q

What antimuscarinic drugs are used for tx of respiratory disorders (asthma and COPD)?

A

Ipratropium
Tiotropium

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7
Q

What antimuscarinic drugs are used for tx of urinary disorders?

A

Darifenacin
Feoterodine
Oxybutynin
Solifenacin
Tolterodine
Trospium

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8
Q

What antimuscarinic drugs are used for tx of cholinergic poisoning?

A

Atropine (+ pralidoxime)

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9
Q

What antimuscarinic drugs are used for tx of movement disorders?

A

Benztropine
Biperiden
Orphenadrine
Procyclidine
Trihexyphenidyl

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10
Q

What is the common ganglion blocker?

A

Mecamylamine

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11
Q

What is the overarching MOA of cholinergic agonists?

A

They mimic the actions of ACh on mAChR OR nAChR

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12
Q

What is specific about choline esters (ACh, bethanechol, carbachol) that results in poor absorption and distribution in the CNS?

A

These drugs have a charged quarternary ammonium group

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13
Q

All choline esters (ACh, bethanechol, carbachol) are hydrolyzed by cholinesterasem but at varying rates resulting in _____.

A

Varying durations of action

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14
Q

What is specific about cholinoreceptor alkaloid agents (muscarine, nicotine, pilocarpine) that allow for them to be well absorbed at most sites of administration?

A

They are uncharged tertiary amines (except for muscarine, which is a quarternary amine)

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15
Q

Effects of direct-acting cholinergic agonists on skeletal muscle

A

only nAChR are present on skeletal m.

Agents that activate nAChR will produe muscle contraction

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16
Q

Effects of direct-acting cholinergic agonists on the eye

A

Contraction of the iris sphincter and ciliary m. leading to drainage of the anterior chamber

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17
Q

Effects of direct-acting cholinergic agonists on the heart

A

Reduction in PVR and changes in HR through M2 mAChR

Usually results in decrease in BP and increase in HR with minimally effective doses of ACh agonist

Large doses of ACh agonist leads to bradycardia, decreased AV node conduction velocity and HoTN

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18
Q

Effects of direct-acting cholinergic agonists on GI/GU tracts

A

Increase in glandular sections, primarily salivary and gastric glands

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19
Q

What type of mAChR is required for direct activation of smooth m. contraction in GI/GU tracts?

A

M3

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20
Q

What type of mAChR is required to reduce relaxation caused by adrenergic effects in GI/GU tracts?

A

M2

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21
Q

What type of mAChR is involved in increased cognitive function and seizure activity?

A

Excitatory

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22
Q

What type of mAChR plays a role in tremors, hypothermia and analgesia?

A

inhibitory

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23
Q

What are the effects of nicotine on the CV system?

A

Sympathomimetic (HTN, alternating tachycardia and bradycardia)

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24
Q

What are the major clinical uses of direct-acting cholinomimetics?

A

Glaucoma

Accommodative esotropia

Post-operative atony

Neurogenic bladder

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25
Q

What direct acting cholinomimetic is the most widely used choline ester for GI/GU disorders?

A

Bethanechol

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26
Q

What direct-acting cholinomimetics are used to increase salivary secretions (typically in patients with Sjogrens disease)?

A

Pilocarpine

Cevimeline

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27
Q

What drug is used when a suspected direct-acting cholinomimetic toxicity is suspected?

A

Atropine

28
Q

What are the contraindications to using mAChR agonists that are distributed systemically?

A

Patients with asthma, hyperthyroidism, coronary insufficiency, or acid-peptic disease

29
Q

What are symptoms corresponding to acute nicotine toxicity?

A

Convulsions –> coma and respiratory arrest

Respiratory paralysis

HTN

Cardiac arrhythmias

30
Q

What are symptoms corresponding to chronic nicotine toxicity?

A

Increased risk of vascular disease

Sudden coronary death

Ulcers

31
Q

Clinical use of ACh

A

Used during ocular surgery to induce miosis (pupillary constriction)

32
Q

Clinical use of Methacholine

A

Used to diagnose bronchial airway hyperreactivity

33
Q

Clinical use of Bethanechol

A

It is a selective mAChR agonist that can be used to tx patients with urinary retention and heart burn

34
Q

Clinical use of Carbachol

A

Used to tx glaucoma

Used to produce miosis during ocular surgery

35
Q

Clinical use of Cevimeline

A

Tx xerostomia

36
Q

Clinical use of Pilocarpine

A

Tx xerostomia

Induce miosis during ophthalmic procedures

Topical tx for glaucoma

37
Q

Clinical use of Varenicline

A

Smoking cessation

38
Q

What are the three subgroups of AChE inhibitors?

A

Alcohols

Carbamic acid esters (carbamates)

Organophosphates

39
Q

The group of alcohol AChE inhibitors function by binding to AChE nonconvalently and thus reversibly. Give an example of a drug in this class.

A

Edrophonium

40
Q

What drugs are considerd to be carbamates?

A

Neostigmine

Pyridostigmine

Physostigmine

Carbaryl

41
Q

What specific features of organophosphates allow them to induce CNS toxicity?

A

They are charge-neutral and highly lipid soluble, thus they can cross the BBB

42
Q

What type of bonding to organophosphates have with AChE?

A

Covalent and irreversible

43
Q

Describe the pharmacokinetics of quaternary and charged AChE inhibitors

A

insoluble in lipids

absorption is poor

No CNS distribution

duration of effect is dtermined by the stability of the inhibitor-enzyme complex

44
Q

Describe the pharmacokinetics of tertiary and uncharged AChE inhibitors

A

Well absorbed from all sites

CNS distribution

More toxic

45
Q

Duration of action of alcohol AChE inhibitors

A

2-10 minutes

46
Q

Duration of action of carbamate AChE inhibitors

A

30 min to 6 hours

47
Q

Duration of action of organophosphate AChE inhibitors

A

Hundreds of hours (very slow!!!)

48
Q

What are the effects of AChE inhibitors on the CNS?

A

At high concentrations: convulsions

49
Q

What are the effects of AChE inhibitors on the eye, respiratory tract, GI tract, urinary tract?

A
  • *Eye:** contraction of ciliary m. and iris sphincter
  • *GI/GU tract:** increased glandular secretions
50
Q

What are the effects of AChE inhibitors on the CV system?

A

Decreased cardiac output

Bradycardia

Increased BP

51
Q

What are the effects of AChE inhibitors on the NMJ?

A

Increased strength of contraction

Fasciculations

52
Q

What are common clinical uses of AChE inhibitors?

A

Reversal of pharmacologic paralysis

Glaucoma

Dementia

Antidote

53
Q

What are the signs and symptoms of acute AChE inhibitor toxicity?

A

Miosis

Salivation

Sweating

Bronchial constriction

Vomiting and diarrhea

54
Q

How can you diagnose an acute AChE inhibitor toxicity?

A

Measure AChE activity in erythrocytes and plasma

55
Q

What drug is used as prophylaxis against AChE inhibitor poisoning?

A

Pyridostigmine

56
Q

What are the most clinically useful cholinergic antagonists?

A

mAChR antagonists

57
Q

What is the prototype antimuscarinic compound?

A

Atropine

58
Q

What tissues are most sensitive to atropine?

A

Salivary glands

Bronchial glands

Sweat glands

59
Q

Effects of mAChR-blocking drugs on CNS

A

Slow, long-lasting sedative effect on the brain

60
Q

Effects of mAChR-blocking drugs on the eye

A

Mydriasis

Cycloplegia and loss of accommodation

Reduced lacrimal secretions

61
Q

Effects of mAChR-blocking drugs on the CV system

A

can cause tachycardia

62
Q

Effects of mAChR-blocking drugs on respiratory tract

A

Bronchodilation and reduced secretions

63
Q

Effects of mAChR-blocking drugs on GI tract

A

Reduced salivary secretions

Prolonged gastric emptying

Lengthened intestinal transit time

64
Q

Effects of mAChR-blocking drugs on GU tract

A

Relaxes smooth m. and subsequently slows voiding (i.e. useful in tx of urinary incontinence)

No significant effect on the uterus

65
Q

What clinical conditions are cholinergic antagonists (mAChR-blocking drugs) used for?

A

Parkinson disease
Motion sickness
Prevent synechia in uveitis and iritis
Asthma and COPD​
Travelers diarrhea
Urinary urgency

66
Q

Overdoses of mAChR antagonists should be treated with what drug type?

A

Cholinesterase inhibitor (physostigmine) and seizure control (with diazepam)

67
Q

Contraindications of muscarinic antagonists such as atropine

A

Moderate to high doses in children can cause death 2/2 hyperthermic effects

Contraindicated in patients with glaucoma and acid-peptic disease

Use with caution in men with prostatic hyperplasia

CPR Pharmacology (7 decks)

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