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(MUL) Pharmacology > Autonomic Drugs (Cholinergic) > Flashcards

Autonomic Drugs (Cholinergic) Flashcards

1
Q

Define Cholinergic

A

Cholinergic agents are compounds which mimic the action of acetylcholine and/or butyrylcholine.

choline is a primary component of the neurotransmitter acetylcholine and functions with inositol as a basic constituent of lecithin.

Choline also prevents fat deposits in the liver and facilitates the movement of fats into cells.

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2
Q

Parasympathetic nervous system uses which Neuro Transmitter to send its messages?

Parasympathetid NS is said to be almost entirely ______…

Provide 5 exmaples

A

acetylcholine almost exclusively to send its messages, is said to be almost entirely cholinergic. Ex:

  1. Neuromuscular junctions,
  2. preganglionic neurons of the sympathetic nervous system,
  3. the basal forebrain,
  4. brain stem complexes ,
  5. the receptor for the merocrine sweat glands.
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3
Q

Cholinergic affects

A

decrease HR/AV conduction
Bronchoconstriction/inc. secretions
increase GI/GU
Eye miosis, ciliary muscle contration (near vision)

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4
Q

Direct acting cholinergic drugs:

Action-Name 4

Also known as?

A

Directly bind to muscarinic receptors
Bethanachol

carbachol

methacholine
Pilocarpine

Known as: Cholinomimetics (direct)

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5
Q

direct acting Nicotinics

name…

A

Nicotine

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6
Q

Bethanachol: indications

A

Urinary retention,

postoperative ileus

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7
Q

ACh: indications

A

Miotic in ophthalmology

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8
Q

Pilocarpine: indications

A

Treatment of glaucoma

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9
Q

Bethanachol: actions

A

Stimulates the detrussor muscle and relaxes trigone and sphincter

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10
Q

Bethanachol: Effects of actions

A

increases voiding pressure and decreases bladder capacity to cause expulsion of urine, lasts a few hours

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11
Q

Bethanachol: Therapeutic application

A

stimulates atonic bladder mostly in postpartum or postoperative , non obstructive urinary retention, also treats neurogenic atony and megacolon

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12
Q

Bethanachol: Adverse effects

A

sweating, salivation, flushing, decreased blood pressure, nausea, abdominal pain, diarrhea, and bronchospasm

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13
Q

ACh: actions

A

decrease in HR and cardiac output, decrease in BP, increase in salivary secrestions, intestinal secresions, GI motility, increases tone of detrusor muscle, enhances bronchiolar secretions, stimulates ciliary muscle contratction, constriction of pupillae sphincter muscle

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14
Q

ACh: therapeutic application

A

lacks therapeutic importance because of its multiplicity of actions and its rapid inactivation by the cholinesterases

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15
Q

Pilocarpine: Actions

A

Rapid miosis and contraction of ciliary muscle when applied topically to cornea, one of most potent stimulator of secretions like sweat, tears and saliva, is effective at opening schlemms canal

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16
Q

Pilocarpine: Therapeutic applications

A

promotes slaivation in patients with xerostomia sjogrens syndrome,used to treat glaucoma and is the drug of choice in the emergency lowering of intraoccular pressure of narrow and wide angle glaucoma. Useful in reversing mydriasis

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17
Q

Pilocarpine: Adverse effects

A

Because pilocarpine can cross the BBB it can be a poisoning agent causing exaggerated parasympatheic effects like profuse sweating and salivation. Atropine can revers the toxic effects

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18
Q

Name 6

(Indirect-reversible)

Cholinergic Drug

A

physostigmine

neostigmine

pyridostigmine

edrophonium

rivastigmine

donepezil

19
Q

Indirect acting cholinergic drugs

ex:

A

inhibit acetylcholinesterase to allow the accumulation of ACh at all 3 cholinergic receptor sites
Physostigmine, Neostigmine, donepezil

20
Q

Physostigmine: Action

A

stimulates muscarinic and nicotinic sites of ANS and nicotinic receptors of the NMJ, it can also penetrate BBB to stimulate cholinergic sites in CNS

21
Q

Physostigmine: Time duration

A

lasts about 2-4 hours

22
Q

Physostigmine: Therapeutic uses

A

increases intestinal and bladder motility to treat atony of either organ, topically it produces miosis and spasm of accommodation, as well as decreasing intraocular pressure, can be used to treat glaucoma but pilocarpine is more effective.

23
Q

Physostigmine: Treatment for overdose

A

used to treat overdoses of drugs with anticholinergic actions like atropine, phenothiazines, and tricyclic antidepressants

24
Q

Physostigmine: Adverse effects

A

convulsions (with high doses) bradycardia, fall in cardiac output, paralysis of skeletal muscle

25
Q

Neostigmine: duration

A

usually last 30 min to 2 hours

26
Q

Neostigmine: therapeutic uses

A

Stim. bladder and GI, treats myasthenia gravis, stimulates a greater # of ACh receptors at muscle endplate

27
Q

Neostigmine: As an antidote

A

For tubocurarie and competitive neuromuscular blocking agents

28
Q

Neostigmine: Adverse effects

A

salivation, flushing, decreased BP, nausea, abdominal pain, diarrhea, bronchospasm

29
Q

Neostigmine: contraindications

A

intestinal or urinary bladder obstruction, pts with peritonitis, or inflammatory bowel disease

30
Q

Donepezil

A

an anticholinesterase remedy for the loss of cognitive function in alzheimers patients (alzheimers pts have deficient cholinergic neurons in CNS)

31
Q

Donepezil: adverse effects

A

primarily GI distress

32
Q

Pilodoxene

A

antidote for indirect cholinergic agonists (reactivates AChE)

33
Q

name 3

(indirect-irreversible) Cholinergic Drugs

A

Malathion

parathion

echothiophate

34
Q

Malathione

A

(house hold insecticides)
ANS Parasympathomimetic
MOA: Irreversible cholinesterase inhibitor
-tertiary ammonium compound
-binds covalently to esterase enzymes
-not hydrolyzed by esterase enzymes
-rapidly absorbed, multiple sites

  • causes SLUD/other ANS things
  • CNS disturbance
  • not therapeutic
  • similar agent as chemical weapon
  • atropine is antidote (plus supportive)
35
Q

Name 3

Ganglionic Blockers

type of drug

A

hexamethonium

mecamylamine

trimethaphan

Type: Cholinergic Drug

36
Q

name 1 Depolarizing

NMJ Blocker

A

Syccinylcholine

37
Q

Name 6

Non-depolarizing NMJ Blockers

A

tubocurarine

atracurium

doxacurium

pancuronium

vecuronium

mivacurium

38
Q

name 1 Nicotinic Blocker

A

Alpha-Bungarotoxin

39
Q

name 8 Muscarinic Blockers

A

atropine

tropicamide

ipratropium

scopolamine

glycopyrrolate

pirenzepine

benztropine

trihexyphenidyl

40
Q

prevents release of Ach

A

Botulinus toxin

41
Q

ACh: actions

A

decrease in HR and cardiac output, decrease in BP, increase in salivary secrestions, intestinal secresions, GI motility, increases tone of detrusor muscle, enhances bronchiolar secretions, stimulates ciliary muscle contratction, constriction of pupillae sphincter muscle

42
Q

ACh: therapeutic application

A

lacks therapeutic importance because of its multiplicity of actions and its rapid inactivation by the cholinesterases

43
Q

for excessive Ach release

name 2 drugs

A

latrotoxin

B-bungarotoxin

44
Q
A

(MUL) Pharmacology (18 decks)

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