Autonomic Drugs (Cholinergic)

Question 1

Define Cholinergic

Answer 1

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.

Question 2

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

Parasympathetid NS is said to be almost entirely ______…

Provide 5 exmaples

Answer 2

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.

Question 3

Cholinergic affects

Answer 3

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

Question 4

Direct acting cholinergic drugs:

Action-Name 4

Also known as?

Answer 4

Directly bind to muscarinic receptors
Bethanachol

carbachol

methacholine
Pilocarpine

Known as: Cholinomimetics (direct)

Question 5

direct acting Nicotinics

name…

Answer 5

Nicotine

Question 6

Bethanachol: indications

Answer 6

Urinary retention,

postoperative ileus

Question 7

ACh: indications

Answer 7

Miotic in ophthalmology

Question 8

Pilocarpine: indications

Answer 8

Treatment of glaucoma

Question 9

Bethanachol: actions

Answer 9

Stimulates the detrussor muscle and relaxes trigone and sphincter

Question 10

Bethanachol: Effects of actions

Answer 10

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

Question 11

Bethanachol: Therapeutic application

Answer 11

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

Question 12

Bethanachol: Adverse effects

Answer 12

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

Question 13

ACh: actions

Answer 13

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

Question 14

ACh: therapeutic application

Answer 14

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

Question 15

Pilocarpine: Actions

Answer 15

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

Question 16

Pilocarpine: Therapeutic applications

Answer 16

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

Question 17

Pilocarpine: Adverse effects

Answer 17

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

Question 18

Name 6

(Indirect-reversible)

Cholinergic Drug

Answer 18

physostigmine

neostigmine

pyridostigmine

edrophonium

rivastigmine

donepezil

Question 19

Indirect acting cholinergic drugs

ex:

Answer 19

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

Question 20

Physostigmine: Action

Answer 20

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

Question 21

Physostigmine: Time duration

Answer 21

lasts about 2-4 hours

Question 22

Physostigmine: Therapeutic uses

Answer 22

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.

Question 23

Physostigmine: Treatment for overdose

Answer 23

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

Question 24

Physostigmine: Adverse effects

Answer 24

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

Question 25

Neostigmine: duration

Answer 25

usually last 30 min to 2 hours

Question 26

Neostigmine: therapeutic uses

Answer 26

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

Question 27

Neostigmine: As an antidote

Answer 27

For tubocurarie and competitive neuromuscular blocking agents

Question 28

Neostigmine: Adverse effects

Answer 28

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

Question 29

Neostigmine: contraindications

Answer 29

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

Question 30

Donepezil

Answer 30

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

Question 31

Donepezil: adverse effects

Answer 31

primarily GI distress

Question 32

Pilodoxene

Answer 32

antidote for indirect cholinergic agonists (reactivates AChE)

Question 33

name 3 (indirect-irreversible) Cholinergic Drugs

Answer 33

Malathion parathion echothiophate

Question 34

Malathione

Answer 34

(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)

Question 35

Name 3 Ganglionic Blockers type of drug

Answer 35

hexamethonium mecamylamine trimethaphan Type: Cholinergic Drug

Question 36

name 1 Depolarizing NMJ Blocker

Answer 36

Syccinylcholine

Question 37

Name 6 Non-depolarizing NMJ Blockers

Answer 37

tubocurarine atracurium doxacurium pancuronium vecuronium mivacurium

Question 38

name 1 Nicotinic Blocker

Answer 38

Alpha-Bungarotoxin

Question 39

name 8 Muscarinic Blockers

Answer 39

atropine tropicamide ipratropium scopolamine glycopyrrolate pirenzepine benztropine trihexyphenidyl

Question 40

prevents release of Ach

Answer 40

Botulinus toxin

Question 41

ACh: actions

Answer 41

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

Question 42

ACh: therapeutic application

Answer 42

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

Question 43

for excessive Ach release name 2 drugs

Answer 43

latrotoxin B-bungarotoxin