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MDSC 1206 > Cholinergic & Anti-Cholinergic Mechanisms& Drugs > Flashcards

Cholinergic & Anti-Cholinergic Mechanisms& Drugs Flashcards

1
Q

Two types of cholinergic receptors

A

Nicotinic

Muscarinic

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2
Q

Synthesis of ACH

A

choline acetyl transferase

Choline + Acetyl CoA ——————> Acetyl Choline

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3
Q

Degradation of Ach

A
  • Ach is broken down by Acetyl choline esterase

- to form choline + acetic acid

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4
Q

Which drugs are direct acting cholinergic agonist

A

Acetylcholine
Methacholine
Bethanecol
Pilocarpine

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5
Q

ACETYLCHOLINE MOA & Therapeutic Use

A

MOA :
binds to muscarinic/nicotinic AChR → direct AChR agonism

Therapeutic use:
to produce MIOSIS during ophthalmic surgery

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6
Q

BETHANECOL MOA & Therapeutic Use

A

MOA :

Bind to muscarinic AChR → direct AChR agonism
-Shows mild nicotinic agonism

Therapeutic Use:
↑ intestinal motility postoperatively

-Treat urinary retention ( inability to empty the bladder) by causing the detrusor muscle to contract during micturition.

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7
Q

METHACHOLINE MOA & Therapeutic Use

A

MOA:
binds to muscarinic AChR → direct AChR agonism

Therapeutic Use: Diagnosis of asthma and bronchial hypersensitivity

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8
Q

PILOCARPINE MOA & Therapeutic Use

A

MOA:
Binds to muscarinic AchR -> direct receptor agonism

Therapeutic uses:

Good stimulator of miosis
Good at stimulating opening of trabecular meshwork around canal of Sclemn ► used treatment of glaucoma.

Adverse Effects:

Crosses the BBB -> hallucinations, convulsions & generalized cholinergic stimulation

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9
Q

PILOCARPINE MOA & Therapeutic Use

A

MOA:
binds to muscarinic AChR → direct AChR agonism

Therapeutic Use:

  • Good stimulator of miosis
  • Good at stimulating the the opening of the trabecular network around the canal of sclemn in the treatment of glaucoma.

Adverse Effects:

  • can cross the BBB
  • causing hallucinations, convulsions & generalized cholinergic stimulation
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10
Q

Which drugs are indirect acting cholinergic agonist ( aka ACHE inhibitors)

A

Physostigmine
Neostigmine
Pyridostigmine
Edrophonium

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11
Q

Physostigmine MOA , Therapeutic Use &

Adverse Effects

A

MOA:

Inhibit AchE → ↓ breakdown of ACh → ↑ ACh levels in synapse

Therapeutic Use:

Use to treat Atropine, phenothiazine & tricyclic antidepressants overdose.

Adverse Effects:
Convulsions
Muscle paralysis secondary to overstimulation
Generalized cholinergic stimulation

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12
Q

Neostigmine MOA , Therapeutic Use &

Adverse Effects

A

MOA:
Inhibit AchE → ↓ breakdown of ACh → ↑ ACh levels in synapse

Therapeutic Use:
Treatment of:
-Myasthenia gravis
-Postoperative and paralytic ileus and urinary retention
-Postoperative reversal of neuromuscular blockade

Adverse Effects:
- Excessive cholinergic stimulation

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13
Q

Endophonium MOA , Therapeutic Use &

Adverse Effects

A

MOA:
Inhibit AchE → ↓ breakdown of ACh → ↑ ACh levels in synapse

Therapeutic Use:
Used to diagnose myasthenia gravis
Used to differentiate MG from cholinergic crisis (excessive Ach)

Adverse Effects:
Excessive cholinergic stimulation

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14
Q

Pyridostigmine MOA , Therapeutic Use &

Adverse Effects

A

MOA:
Inhibit AchE → ↓ breakdown of ACh → ↑ ACh levels in synapse

Therapeutic Use:

  • Used for long term treatment of myasthenia gravis
  • Longer action compared to neostigmine

Adverse Effects
Excessive cholinergic stimulation

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15
Q

What are organophosphates

A

IRREVERSIBLE anticholinesterases

  • irreversibly inhibits AchE
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16
Q

Cholinoesterase inhibitor

A

PRAILDOXIME

17
Q

Drug used to sea skickness

A

SCOPOLAMINE

18
Q

Therapeutic uses of atropine

A

Treatment of bradycardia

Mydriasis

Cycloplegia -A loss of lens accommodation due to paralysis of the ciliary muscle

Gastrointestinal spasms

Organophosphate poisoning

19
Q

TOXIC EFFECTS OF ATROPINE

A 
Mydriasis 
Delirium
Flushing
Hyperthermia
Decreased secretions and dry skin
Paralytic ileus and urinary retention
Tachycardia
20
Q

Pharmacologic actions of atropine

A

CNS- restlessness, hallucinations, delusions

CVS- Low doses – reduces heart rate through central stimulation of vagus nerve
High doses- blocks M2 receptors of heart→ tachycardia

GIT- Reduces salivary gland secretion & GI motility

Pulmonary - Reduces bronchial secretions & stimulates bronchodilation

Sweat glands- Suppresses sweating

Eye- Causes paralysis of sphincter m of iris & ciliary m of lens → mydriasis and cycloplegia

Urinary system- Blocks M receptors in bladder wall → bladder wall relaxation

21
Q

Adverse effects of ACHResult from excessive generalized cholinergic stimulation

Diarrhoea & decreased blood pressure

Urination

Miosis

Bronchoconstriction & bradycardia

Excitation of skeletal muscle

Lacrimation

Salivation & sweating

A

MDSC 1206 (2 decks)

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