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Cholinergic drugs Flashcards

(67 cards)

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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
What direct acting cholinomimetic is the most widely used choline ester for GI/GU disorders?
Bethanechol
26
What direct-acting cholinomimetics are used to increase salivary secretions (typically in patients with Sjogrens disease)?
Pilocarpine Cevimeline
27
What drug is used when a suspected direct-acting cholinomimetic toxicity is suspected?
Atropine
28
What are the contraindications to using mAChR agonists that are distributed systemically?
Patients with asthma, hyperthyroidism, coronary insufficiency, or acid-peptic disease
29
What are symptoms corresponding to acute nicotine toxicity?
Convulsions --\> coma and respiratory arrest Respiratory paralysis HTN Cardiac arrhythmias
30
What are symptoms corresponding to chronic nicotine toxicity?
Increased risk of vascular disease Sudden coronary death Ulcers
31
Clinical use of ACh
Used during ocular surgery to induce miosis (pupillary constriction)
32
Clinical use of Methacholine
Used to diagnose bronchial airway hyperreactivity
33
Clinical use of Bethanechol
It is a selective mAChR agonist that can be used to tx patients with urinary retention and heart burn
34
Clinical use of Carbachol
Used to tx glaucoma Used to produce miosis during ocular surgery
35
Clinical use of Cevimeline
Tx xerostomia
36
Clinical use of Pilocarpine
Tx xerostomia Induce miosis during ophthalmic procedures Topical tx for glaucoma
37
Clinical use of Varenicline
Smoking cessation
38
What are the three subgroups of AChE inhibitors?
Alcohols Carbamic acid esters (carbamates) Organophosphates
39
The group of alcohol AChE inhibitors function by binding to AChE nonconvalently and thus reversibly. Give an example of a drug in this class.
Edrophonium
40
What drugs are considerd to be carbamates?
Neostigmine Pyridostigmine Physostigmine Carbaryl
41
What specific features of organophosphates allow them to induce CNS toxicity?
They are charge-neutral and highly lipid soluble, thus they can cross the BBB
42
What type of bonding to organophosphates have with AChE?
Covalent and irreversible
43
Describe the pharmacokinetics of quaternary and charged AChE inhibitors
insoluble in lipids absorption is poor No CNS distribution duration of effect is dtermined by the stability of the inhibitor-enzyme complex
44
Describe the pharmacokinetics of tertiary and uncharged AChE inhibitors
Well absorbed from all sites CNS distribution More toxic
45
Duration of action of alcohol AChE inhibitors
2-10 minutes
46
Duration of action of carbamate AChE inhibitors
30 min to 6 hours
47
Duration of action of organophosphate AChE inhibitors
Hundreds of hours (very slow!!!)
48
What are the effects of AChE inhibitors on the CNS?
At high concentrations: convulsions
49
What are the effects of AChE inhibitors on the eye, respiratory tract, GI tract, urinary tract?
* *Eye:** contraction of ciliary m. and iris sphincter * *GI/GU tract:** increased glandular secretions
50
What are the effects of AChE inhibitors on the CV system?
Decreased cardiac output Bradycardia Increased BP
51
What are the effects of AChE inhibitors on the NMJ?
Increased strength of contraction Fasciculations
52
What are common clinical uses of AChE inhibitors?
Reversal of pharmacologic paralysis Glaucoma Dementia Antidote
53
What are the signs and symptoms of acute AChE inhibitor toxicity?
Miosis Salivation Sweating Bronchial constriction Vomiting and diarrhea
54
How can you diagnose an acute AChE inhibitor toxicity?
Measure AChE activity in erythrocytes and plasma
55
What drug is used as prophylaxis against AChE inhibitor poisoning?
Pyridostigmine
56
What are the most clinically useful cholinergic antagonists?
mAChR antagonists
57
What is the prototype antimuscarinic compound?
Atropine
58
What tissues are most sensitive to atropine?
Salivary glands Bronchial glands Sweat glands
59
Effects of mAChR-blocking drugs on CNS
Slow, long-lasting sedative effect on the brain
60
Effects of mAChR-blocking drugs on the eye
Mydriasis Cycloplegia and loss of accommodation Reduced lacrimal secretions
61
Effects of mAChR-blocking drugs on the CV system
can cause tachycardia
62
Effects of mAChR-blocking drugs on respiratory tract
Bronchodilation and reduced secretions
63
Effects of mAChR-blocking drugs on GI tract
Reduced salivary secretions Prolonged gastric emptying Lengthened intestinal transit time
64
Effects of mAChR-blocking drugs on GU tract
Relaxes smooth m. and subsequently slows voiding (i.e. useful in tx of urinary incontinence) No significant effect on the uterus
65
What clinical conditions are cholinergic antagonists (mAChR-blocking drugs) used for?
Parkinson disease Motion sickness Prevent synechia in uveitis and iritis Asthma and COPD​ Travelers diarrhea Urinary urgency
66
Overdoses of mAChR antagonists should be treated with what drug type?
Cholinesterase inhibitor (physostigmine) and seizure control (with diazepam)
67
Contraindications of muscarinic antagonists such as atropine
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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