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BIOM*3090 > cholinergic drugs > Flashcards

cholinergic drugs Flashcards

(42 cards)

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1
Q

What are cholinomimetics?

A

Drugs that mimic the action of acetylcholine (ACh)

Cholinomimetics include direct receptor agonists and indirect acting AChE inhibitors.

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2
Q

What are the two categories of cholinomimetics?

A
  1. Direct (receptor agonists)
  2. Indirect (AChE inhibitors)
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3
Q

What is the effect of cholinergic antagonists?

A

Reduce the action of acetylcholine (ACh)

Cholinergic antagonists can be further classified into antimuscarinic and antinicotinic.

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4
Q

What direct acting agonists are susceptible to AChE?

A

Acetylcholine

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5
Q

What are the 2 classes of cholinergic antagonists?

A
  1. antimuscarinic
  2. antinicotinic.
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6
Q

What are the characteristics of indirect acting agonists?

A

They are AChE inhibitors that increase local ACh concentration by reducing hydrolysis.

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7
Q

What is the duration of action for reversible AChE inhibitors like physostigmine?

A

intermediate-acting

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8
Q

What is the duration of action for AChE inhibitor, physostigmine?

A

30min - 6h (intermediate-acting)

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9
Q

What is the duration of action for AChE inhibitor, echothiophate?

A

long-acting

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10
Q

What is the mechanism of irreversible AChE inhibitors?

A

Covalent bond formation with AChE, stabilizing the bond

Examples include organophosphates like echothiophate.

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11
Q

What are the symptoms of muscarinic excess?

A
  • Diarrhea
  • Urination
  • Miosis
  • Bradycardia
  • Bronchoconstriction
  • Excitation (CNS)
  • Lacrimation
  • Sweating and salivation
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12
Q

What is the fatal dose of nicotine?

A

40 mg, approximately 2 cigarettes

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13
Q

What is the primary effect of nicotine on the nervous system?

A

Activates both the PSNS and SNS (Nn) at ganglia, whoch increases release of ACh and NE in tissue and adrenal gland

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14
Q

What is the role of atropine in organophosphate poisoning?

A

Atropine is used to block muscarinic effects and has equal affinity for M receptor subtypes.

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15
Q

What type of drug is trimethaphan?

A

Ganglionic blocker

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16
Q

What are the effects of pilocarpine in the eye?

A

Reduces intraocular pressure, used to treat glaucoma

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17
Q

Fill in the blank: Most cholinergic receptor agonists used clinically are not receptor subtype _______.

18
Q

True or False: Muscarinic receptor activation leads to vasodilation.

19
Q

What is the primary action of AChE inhibitors?

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A

Increase ACh levels at synapses

20
Q

What are the two types of cholinergic receptors?

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A
  • Muscarinic
  • Nicotinic
21
Q

What neurotransmitter is primarily released by the PSNS?

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A

Acetylcholine (ACh)

22
Q

What are the main effects of nicotine on the cardiovascular system?

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A
  • muscarinic excess
  • CNS induced convulsions/coma/respiratory depression
  • skeletal muscle contraction followed by paralysis
  • Increased heart rate and blood pressure
23
Q

What are the effects of ACh at ganglia in the PSNS?

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A

Increased ACh levels

24
Q

What is the effect of organophosphates on the nervous system?

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A

Initial symptoms of muscarinic excess followed by CNS stimulation Nn and Nm activation)

25
What is the pharmacokinetics of atropine?
Well absorbed and distributed, half-life of 2 hours
26
What is the historical significance of Atropa Belladonna?
Used in the Italian renaissance for dilating pupils, considered beautiful | (Plant version of Atropine)
27
What are antinicotine drugs?
Antinicotine drugs inhibit the effect of ACh at specific sites. ## Footnote They include ganglionic blockers and neuromuscular blockers.
28
What is an example of a ganglionic blocker?
Trimethaphan ## Footnote It can be used for hypertensive crisis or dissecting aortic aneurysm.
29
What kind of drug is D-Tubocurarine? What is it used for?
- A neuromuscular blocker - Use to reduce skeletal muscle contraction in surgical procedures. ## Footnote It is a neuromuscular blocker.
30
What condition is characterized by increased ocular pressure?
Glaucoma ## Footnote It is a condition that can lead to vision loss if untreated.
31
Which drugs are used to treat glaucoma?
Pilocarpine, physostigmine, echothiophate ## Footnote These drugs help decrease ocular pressure.
32
How do pilocarpine and physostigmine differ in their mechanism of action?
Pilocarpine primarily stimulates muscarinic receptors while physostigmine inhibits acetylcholinesterase. ## Footnote This leads to different physiological effects.
33
The PNS releases ____ at the ganglion, and ____ at the neuroeffector junction. This activates ____ receptors.
ACh, ACh, M2/M3
34
The SNS releases ____ at the ganglion, and ____ at the neuroeffector junction. This activates ____ receptors.
ACh, NE, a1/b1/b2
35
The PSNS is made up of 2 axons: a ____ pregalglionic axon, and a ____ postganglionic axon.
cholinergic, cholinergic
36
The SNS is made up of 2 axons: a ____ pregalglionic axon, and a ____ postganglionic axon.
cholinergic, adrenergic
37
Esters of Choline and Alkaloids are...
Direct-Acting Cholinergic Agonists
38
What are the 2 types of choline esters? Describe their absorbtion/distribution.
1. acetylcholine 2. bethanechol (not absorbed/distributed well)
39
What are the 3 types of alkaloids? Describe their absorbtion/distribution.
1. muscarine 2. nicotine 3. pilocarpine (absorbed/distributed well, even in the CNS)
40
M3 receptors are found where in the body?
- eye - glands (salivary, sweat, etc.) - bladder - genitals - intestines/colon - stomach - bronchi - endothelial cells
41
M2 receptors are found where in the body?
- heart
42
M5 receptors are found where in the body?
- endothelial cells

BIOM*3090 (13 decks)

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