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PHARMACOLOGY > CHOLINERGIC DRUG > Flashcards

CHOLINERGIC DRUG Flashcards

1
Q

When does we use adrenaline and acetylcholine?

A

Adrenaline - during sympathetic (fight or flight)

Acetylcholine - during parasympathetic (rest and digest)

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2
Q

State the locations of cholinergic neurons.

A
  1. Basal forebrain
  2. Nucleus basalis
  3. Medial septal nucleus and nucleus of the diagonal band
  4. Pedunculopontine nucleus and laterodorsal tegmental nucleus
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3
Q

State the types of cholinergic receptors.

A
  1. Nicotinic acetylcholine receptors (Ionotropic)

2. Muscarinic acetylcholine receptors (Metabotropic) - G protein coupled

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4
Q

What is the fx of acetylcholinsterase?

A

Breaks ACh down into acetate and choline.

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5
Q

State 1 fx of acetylcholine.

A

Used at NMJ to cause muscle contraction

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6
Q

What is the subtypes of nicotinic receptors and where is the location of the subtypes?

A
  1. Nm - NMJ
  2. Nn
    - Can be found in the peripheral:autonomic ganglia & adrenal medulla
    - Can be found in the central: CNS
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7
Q

List the subtypes of muscarinic receptors and its location.

A
  1. M1
    - CNS neurons
    - Sympathetic postganglionic cell bodies
  2. M2
    - Myocardium
    - Smooth muscled organs
  3. M3
    - Glands
    - Smooth muscle
    - Endothelium
    - Eyes
  4. M4
    - CNS
  5. M5
    - CNS
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8
Q

In muscarinic agonist, which one will stimulate excitatory?

A

M1,M3,M5

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9
Q

In muscarinic agonist, which one will produce inhibitory effect?

A

M2, M4

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10
Q

Classify cholinergic drugs into direct and indirect acting drugs

A

Directly acting

  • ACh
  • Pilocorpine
  • Bethanecol
  • Methacoline

Indirectly acting

  • Reversible: Neostigmine, edrophonium, physostigmine
  • Irreversible: Organophosphate, malathion
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11
Q

State the therapeutic uses of pilocarpine

A
  • Medical management of glaucoma
  • Dry mouth treatment
  • Sjogren’ syndrome - an autoimmune disease - body’s immune system attacks glands that secrete fluid including lacrimal and salivary glands
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12
Q

State the adverse effect of pilocarpine.

A
  • Excessive sweating (diaphoresis)
  • Excessive tearing
  • Blurred vision
  • Increased need to urinate (frequency)
  • Bradycardia
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13
Q

State other therapeutic uses of cholinergic stimulants.

A
  1. Bethanicol - urinary bladder disorder
  2. Methacholine - diagnosis of bronchial hyperactivity
  3. Acetylcholine/ carbachol - miotic agents
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14
Q

What is the causes of muscarinic toxicity?

A
  • Overdose of medications
  • Mushroom poisoning
  • Organophosphate poisoning
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15
Q

What is the sign and symptoms of muscarinic toxicity?

A

D- Diarrhoea
U- Urination
M- Miosis : contraction of the pupil of the eye.
B- Bradycardia : a slower than normal heart rate
B- Bronchospasm : a tightening of the muscles that line the airways (bronchi) in your lungs
E- Emesis : vomit
L- Lethargy : drowsiness
L- Lacrimation : abnormal or excessive secretion of tears due to local or systemic disease
S- Salivation/ seizure

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16
Q

What is treatment of muscarinic toxicity?

A
  • Blockade of muscarinic activity with muscarinic cholinergic blockers such as atropine
  • Reversal of acetylcholinesterase inhibition such as pralidoxime
17
Q

What is the effect of muscarinic receptor in the eye?

A
  • In the eye, the muscarinic receptor is M3 receptor. It is a Gq.
  • In the eye, the M3 will causes the sphinter to contract.
  • This will lead to miosis.
  • M3 will also causes the ciliary muscle to contract
  • Hence, it will accomodate near vision.
18
Q

What is the mechanism of action of pilocarpine?

A
  • Pilocarpine bind to muscarinic receptor.
  • This will causes phospholipase C to be activated.
  • The activation of phospholipase C will causes the PIP2 to cleave to IP3 and DAG.
  • DAG undergoes phosphorylation and is catalysed by PKC.
  • Hence, the channel for Ca+ is opened and this lead to muscle contraction d/t high amount of Ca+
19
Q

List the effect of pilocarpine in the eye.

A
  • Contraction of ciliary muscle
  • Fixed near vision
  • Lower the intraocular pressure
  • Increase the glandular secretion
20
Q

TRUE/FALSE
MANAGEMENT OF ORGANOPHOSPHATE POISONING INCLUDES:
A. ATROPINE TO COUNTERACT THE NICOTINIC RECEPTOR OVERSTIMULATION
B. PILOCARPINE TO THE MUSCARINIC RECEPTOR OVERSTIMULATION
C. PRALIDOXIME TO REGENERATE ACETYLCHOLINESTERASE.
D. EDROPHONIUM FOR THE DIAGNOSIS
E. SUCCINYLCHOLINE TO REDUCE SEIZURES

A

A. FALSE (THE AMOUNT OF ACETYLCHOLINE IS HIGH ATROPINE IS A CHOLINERGIC BLOCKER (ANTICHOLINERGIC) - REDUCE THE AMOUNT OF ACETYCHOLINE BUT IT BINDS TO THE MUSCARINIC RECEPTOR NOT NICOTINIC RECEPTOR)
B. FALSE (PILOCARPINE IS A CHOLINERGIC DRUG. IT WILL INCREASE THE AMOUNT OF ACETYLCHOLINE.)
C. TRUE (ATROPINE AND PRALIDOXIME IS CONSUMED DURING MUSCARINIC TOXICITY/ ORGANOPHOSPHATE POISONING)
D. FALSE (EDROPHONIUM IS USED TO DIAGNOSED MG AS IT IS AN ANTICHOLINESTERASE. IT WILL INCREASE THE AMOUNT OF ACETYLCHOLINE)
E. FALSE (SUCCINYLCHOLINE IS A DEPOLARISING MUSCLE RELAXANT.)

21
Q

TRUE/FALSE
PILOCARPINE:
A. IS AN ANTICHOLINERGIC DRUG
B. MIOSIS
C. CYCLOPLEGIA
D. IS USED FOR THE TREATMENT OF GLAUCOMA
E. ANTAGONIST BY PHYSOSTIGMINE

A

A. FALSE (CHOLINERGIC DRUG. ANTICHOLINERGIC DRUG = ATROPINE)
B. TRUE (DECREASED THE INTRAOCULAR PRESSURE. SAME LIKE ANTICHOLINESTERASE)
C. FALSE (CYCLOSPASM. CYCLOPLEGIA = ATROPINE)
D. TRUE (AS IT CAN DECREASED THE INTRAOCULAR PRESSURE AND INCREASE THE LACRIMINAL SECRETION)
E. FALSE (PHYSOSTIGMINE IS AN ANTICHOLINESTERASE -> INCREASE OF ACETYLCHOLINE -> SAME F(X) AS PILOCARPINE)

22
Q

TRUE/FALSE
WHICH OF THE FOLLOWING DRUGS AND THEIR THERAPEUTIC USES ARE CORRECTLY MATCHED?
A. NEOSTIGMINE: MG
B. ATROPINE: GLAUCOMA
C. IPRATROPIUM BROMIDE: BRONCHIAL ASTHMA
D. SCOPOLAMINE: MOTION SICKNESS
E. PILOCARPINE: ORGANOPHOSPHATE POISONING

A

A. TRUE (NEOSTIGMINE IS AN ANTICHOLINESTERASE. IT WILL INCREASE THE ACETYLCHOLINE)
B. FALSE (ATROPINE WILL INCREASE THE INTRAOCULAR PRESSURE. PILOCARPINE AND NEOSTIGMINE CAN DECREASE THE INTRAOCULAR PRESSURE -> TREAT GLAUCOMA)
C. TRUE (SAME GRP AS ATROPINE - ANTICHOLINERGIC -> INCREASE THE AMOUNT OF ACETYLCHOLINE)
D. TRUE
E. FALSE (PILOCARPINE IS THE CAUSED OF ORGANOPHOSPHATE POISONING)

PHARMACOLOGY (9 decks)

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