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Pharmacology > cholinergic drugs (agonists and antagonists) > Flashcards

cholinergic drugs (agonists and antagonists) Flashcards

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

A

crosses BBB (tertiary amine)

20
Q

Pyridostigmine - BBB

A

No BBB (quaternary amine)

21
Q

Pyridostigmine - clinical use

A
  1. Myasthenia Gravis (long acting)
22
Q

with cholinomimetics agents using, be careful with

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

A

organophosphates, such as parathion, that IRREVERSIBLY inhibit AChE

24
Q

organophosphates are often components of …

A

insecticides

25
Q

organophosphates poisoning is often seen in

A

farmers

26
Q

direct vs inderct cholinomimetics agents toxicity

A

similar, but because indirect influence the nicotinic as the muscarinic actions, more nicotinic manifestations may be observed

27
Q

cholinommetics agents - adverse effects

A 
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
Q

organophosphates poisoning - antidote (and mechanism of action

A

atropine (competitive inhibitor) + pralidoxime (regenerates AChE if give early, NOT in BBB)

29
Q

cholinomimetic agents - drugs (all)

A

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
Q

Muscarinic antagonists - drugs

A
  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
Q

Muscarinic antagonists - drugs of the eye

A
  1. atropine
  2. homotropine
  3. tropicamide
32
Q

Muscarinic antagonists - drugs of the CNS

A
  1. benzotropine

2. scopolamine

33
Q

Muscarinic antagonists - drugs of GI/respiratory

A

glycopyrrolate

34
Q

Muscarinic antagonists - drugs of GI

A
  1. hyoscyamine

2. dicyclomine

35
Q

Muscarinic antagonists - drugs of GU

A
  1. oxybutynin
  2. solifenacin
  3. tolterodine
36
Q

Muscarinic antagonists - drugs of eye and clinical use

A
  1. atropine 2. homotropine 3. tropicamide

produce mydriasis and cycloplegia

37
Q

Muscarinic antagonists - drugs of the CNS

A
  1. benzotropine –> parkinson, acute dystonia

2. scopolamine –> motion sickness

38
Q

Muscarinic antagonists - drugs of GI/respiratory and mechanism of action

A

glycopyrrolate :

oral: drooling, peptic ulcer
parental: preoperative use to reduce airway secretions

39
Q

Muscarinic antagonists - drugs of GI and clinical use

A
  1. hyoscyamine 2. dicyclomine

antispasmodics for irrtavle bowel syndrome

40
Q

Muscarinic antagonists - drugs of Respiratory and clinical use

A
  1. Ipratropium 2. tiotropium

- -> COPD, ASTHMA

41
Q

Muscarinic antagonists - drugs of GU and mechanism of action

A
  1. oxybutynin 2. solifenacin 3. tolterodine

reduce bladder spasms and urge urinary incontinence (overactive bladder)

42
Q

Atropine - clinical use

A
  1. bradycardia

2. opthalmic applications (produce mydriasis and cycloplegia)

43
Q

action of atropin in different organ systems

A

eye –> produce mydriasis and cycloplegia
airway –> decreases secretion
stomach –> decreases acid secretion
gut –> decreases motility
bladder –> decreases urgency in cystitis

44
Q

general action of Atropine

A

blocks DUMMBBeLSS of cholinesterase inhibitor poisoning

does not block skeletal muscles and CNS because are nicotinic receptor mediated

45
Q

Aropine - adverse effects

A
  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
Q

plant with atropine

A

Jimson weed (Datura) –> gardner’s pupil (mydriasis due to plant alkaloids

Pharmacology (9 decks)

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