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cholinergic drugs (agonists and antagonists) Flashcards

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1
Q

Cholinomimetics agents are divided to

A
  1. direct agents

2. indirect agonists (anticholinesterases)

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2
Q

direct cholinominetics agents - drugs

A
  1. Bethanechol
  2. Carbachol
  3. Metacholine
  4. Pilocarpine
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3
Q

Bethanechol - clinical use

A
  1. Postoperative ileus
  2. neurogenic ileus
  3. urinary retention
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4
Q

Bethanechol - action

A

cholinomimetic agents (direct agonist) –> activates bowel and bladder smooth muscle (reistant to AChE)

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5
Q

Carbahol - clinical use

A

constricts pupil and relieves intraocular pressure in open-angle glaucoma

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6
Q

Carbahol - mechanism of action

A

cholinomimetic agents (direct agonist)

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7
Q

Metacholine - clinical use

A

challange test for diagnosis of asthma

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8
Q

Metacholine - mechanism of action

A

cholinomimetic agents (direct agonist) –> stimulates M receptors in airway when inhaled (M3)

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9
Q

pilocarpine - clinical use

A
  1. Potent stimulator of sweat tears, and saliva - xerostomia (Sjogren syndrome)
  2. open angle and closed angle glaucoma (1st line in acute)
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10
Q

pilocarpine - mechanism of action

A 
cholinomimetic agents (direct agonist) --> contracts ciliary muscle of eye (open-angle glaucoma), pupillary sphincter 
Resistant to AChE)
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11
Q

direct cholinominetics agents - drugs and which is AChE resistant

A
  1. Bethanechol –> resistant
  2. Carbachol
  3. Metacholine
  4. Pilocarpine –> resistant
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12
Q

Indirect antagonists (anticholinesterases) - drugs

A
  1. Donepezil
  2. galantamine
  3. rivastigmine
  4. Edrophonium
  5. Neostigimine
  6. Physostigmine
  7. Pyridostigmine
  8. tacrine
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13
Q

anticholinesterases used in Alzheimer

A
  1. Donepezil
  2. galantamine
  3. rivastigmine
  4. tacrine
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14
Q

Edrophonium - clinical use

A

historically, diagnosis of myasthenia gravis (extremely short acting)

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15
Q

diagnosis of myasthenia gravis

A
  1. historically: Edrophonium –> extremely short acting

2. NOW: anti AChR Ab test

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16
Q

Neostigmine - BBB

A

No BBB (quaternary amine)

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17
Q

Neostigmine - clinical use

A
  1. postoperative and neurogenic ileus
  2. urinary retention
  3. Myasthenia gravis
    4 . Reversal of NMJ blockade (postoperative)
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18
Q

Physostigmine - clinical use

A
  1. anticholinergic toxicity
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19
Q

Physostigmine - BBB

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A

crosses BBB (tertiary amine)

20
Q

Pyridostigmine - BBB

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A

No BBB (quaternary amine)

21
Q

Pyridostigmine - clinical use

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A
  1. Myasthenia Gravis (long acting)
22
Q

with cholinomimetics agents using, be careful with

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A

exacerbation of 1. asthma and 2. COPD
3. peptic ulcers
(when giving to susceptible patients)

23
Q

Cholinesterase inhibitor poisoning is often due to

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A

organophosphates, such as parathion, that IRREVERSIBLY inhibit AChE

24
Q

organophosphates are often components of …

25
organophosphates poisoning is often seen in
farmers
26
direct vs inderct cholinomimetics agents toxicity
similar, but because indirect influence the nicotinic as the muscarinic actions, more nicotinic manifestations may be observed
27
cholinommetics agents - adverse effects
``` DUMBBELLSS (M:muscarinic, N: nicotinic) Diarrhea (M) Urination (M) Miosis (M) Bronchospasm (M) Bradycardia (M) Excitation of skeletal muscle and CNS (N) Lacrimation (M) Sweating (M) Salivation (M) ```
28
organophosphates poisoning - antidote (and mechanism of action
atropine (competitive inhibitor) + pralidoxime (regenerates AChE if give early, NOT in BBB)
29
cholinomimetic agents - drugs (all)
Direct: 1. Bethanechol 2. Carbachol 3. Metacholine 4. Pilocarpine Indirect: 1. Donepezil 2. galantamine 3. rivastigmine 4. Edrophonium 5. Neostigimine 6. Physostigmine 7. Pyridostigmine 8. tacrine
30
Muscarinic antagonists - drugs
1. Atropine 2. Homatropine 3. tropicamide 4. Benzotropine 5. Glycopyrrolate 6. Hyoscyamine 7. dicyclomine 8. ipratropium 9. tiotropium 10. Oxybutunin 11. solifenaxin 12. tolterodine 13. Scopolamine
31
Muscarinic antagonists - drugs of the eye
1. atropine 2. homotropine 3. tropicamide
32
Muscarinic antagonists - drugs of the CNS
1. benzotropine | 2. scopolamine
33
Muscarinic antagonists - drugs of GI/respiratory
glycopyrrolate
34
Muscarinic antagonists - drugs of GI
1. hyoscyamine | 2. dicyclomine
35
Muscarinic antagonists - drugs of GU
1. oxybutynin 2. solifenacin 3. tolterodine
36
Muscarinic antagonists - drugs of eye and clinical use
1. atropine 2. homotropine 3. tropicamide | produce mydriasis and cycloplegia
37
Muscarinic antagonists - drugs of the CNS
1. benzotropine --> parkinson, acute dystonia | 2. scopolamine --> motion sickness
38
Muscarinic antagonists - drugs of GI/respiratory and mechanism of action
glycopyrrolate : oral: drooling, peptic ulcer parental: preoperative use to reduce airway secretions
39
Muscarinic antagonists - drugs of GI and clinical use
1. hyoscyamine 2. dicyclomine | antispasmodics for irrtavle bowel syndrome
40
Muscarinic antagonists - drugs of Respiratory and clinical use
1. Ipratropium 2. tiotropium | - -> COPD, ASTHMA
41
Muscarinic antagonists - drugs of GU and mechanism of action
1. oxybutynin 2. solifenacin 3. tolterodine | reduce bladder spasms and urge urinary incontinence (overactive bladder)
42
Atropine - clinical use
1. bradycardia | 2. opthalmic applications (produce mydriasis and cycloplegia)
43
action of atropin in different organ systems
eye --> produce mydriasis and cycloplegia airway --> decreases secretion stomach --> decreases acid secretion gut --> decreases motility bladder --> decreases urgency in cystitis
44
general action of Atropine
blocks DUMMBBeLSS of cholinesterase inhibitor poisoning | does not block skeletal muscles and CNS because are nicotinic receptor mediated
45
Aropine - adverse effects
1. increased body Q (decreased sweating) 2. rapid pulse 3. dry mount 4. dry, flushed skin 5. cycloplegia 6. constipation 7. disorientation 8. acute agle-closure glaucoma in elederly (mydriasis) 9. urinary retention in men with BOH 10. hypertermia in infants
46
plant with atropine
Jimson weed (Datura) --> gardner's pupil (mydriasis due to plant alkaloids

Pharmacology (9 decks)

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