Cholinoceptor-Blocking Drugs Flashcards

1
Q

M1 receptor subtype is located in?
M2?
M3?

A

M1 - CNS neurons, sympathetic postganglionic cell bodies, many presynaptic sites

M2 - Myocardium, smooth muscle organs

M3 - Effector cell membrane

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2
Q

Muscarinic Antagonist a.k.a

A
  • Parasympathetic

- Antimuscarinic

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3
Q

What drug is derived from plant atropa belladonna that are often use on their effects on the eye and CNS

A

Atropine (Hyosctamine)

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4
Q

Tissues most sensitive to atropine?

A

Salivary
Brochial
Sweat Glands

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5
Q

Which antimuscarinic drug has more marked central effects?

In your answer above, it produces what in recommended dose?
In toxic doses, produce what?

A
  • Scopolamine > Atropine
  • Drowsiness (Amnesia in sensitive individuals)
  • Excitement, agitation, hallucinations, and coma
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6
Q
  • Antimuscarinic effect on pupillary constrictor muscle.
A
  • unopposed sympthetic dilator activity and mydriasis

Additional effects:

  • weaken the contraction of the ciliary muscle or cycloplegia (loss of the ability to accommodate)
  • reduce lacrimal secretion(large doses)
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7
Q

SA node is very sensitive to muscarinic receptor blockade.

Moderate to high therapeutic doses of atropine causes what?

A
  • Tachycardia
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8
Q

True or False.

Ventricles are highly affected by anti-muscarinic drugs at therapeutic levels.

A

False.

Ventricles are less affected by anti-muscarinic drugs at therapeutic levels because of lesser degree of vagal control.

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9
Q

Certain vestibular disorders respond to anti-muscarinic drugs (and to antihistamine with anti-muscarinic effects). True or False. Name one example.

A

True. Scopolamine.

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10
Q

Antimuscarinic agents are administered topically as eye drops or ointment are not helpful in doing complete examination. True or false.

A

False

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11
Q

Atropine became part of routine preoperative medication when anesthetics such as ether were used. This would lead to what?

How to prevent?

A

Increased airway secretion and frequent laryngospasm.

Pre-anesthetic injection of atropine or scopolamine could prevent this hazardous effects.

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12
Q

This is a synthetic analog atropine used as inhalation drug for asthma or COPD.
How does is work?

A

Ipatropium.

Aerosol route has the advantage of maximal concentration At bronchial target tissue with reduced systemic effects.

(Also used in COPD.)

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13
Q

In the situation of marked reflex vagal discharge that sometimes accompanies the pain in MI, what is the drug of choice?

A

Parenteral Atropine

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14
Q

A person infected with trypanosoma cruzi has what disease?

It affects what receptor in the heart? And exert what action? This is prevented by what drug?

A

Chagas’ Disease.

M2 muscarinic receptors.
Parasympathomimetic action.
Atropine.

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15
Q

What muscarinic receptors are expressed predominantly in the human urinary bladder?

A

M3 and M2.

With M3 mediating direct activation of contraction.

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16
Q

Oxybutinin is used to relieve what?

It is somewhat selective to what receptor?

A

Bladder spasm.

M3 receptors.

17
Q

Alternative treatment for urinary incontinence refractory to antimuscarinic drugs?

A

Intrabladder injection of botulinum toxin A by interfering with the release of neuronal ACh.

18
Q

Antimuscarinic agents are administered topically as eye drops or ointment are not helpful in doing complete examination. True or false.

A

False

19
Q

Atropine became part of routine preoperative medication when anesthetics such as ether were used. This would lead to what?

How to prevent?

A

Increased airway secretion and frequent laryngospasm.

Pre-anesthetic injection of atropine or scopolamine could prevent this hazardous effects.

20
Q

This is a synthetic analog atropine used as inhalation drug for asthma or COPD.
How does is work?

A

Ipatropium.

Aerosol route has the advantage of maximal concentration At bronchial target tissue with reduced systemic effects.

(Also used in COPD.)

21
Q

In the situation of marked reflex vagal discharge that sometimes accompanies the pain in MI, what is the drug of choice?

A

Parenteral Atropine

22
Q

A person infected with trypanosoma cruzi has what disease?

It affects what receptor in the heart? And exert what action? This is prevented by what drug?

A

Chagas’ Disease.

M2 muscarinic receptors.
Parasympathomimetic action.
Atropine.

23
Q

What muscarinic receptors are expressed predominantly in the human urinary bladder?

A

M3 and M2.

With M3 mediating direct activation of contraction.

24
Q

Oxybutinin is used to relieve what?

It is somewhat selective to what receptor?

A

Bladder spasm.

M3 receptors.

25
Q

Alternative treatment for urinary incontinence refractory to antimuscarinic drugs?

A

Intrabladder injection of botulinum toxin A by interfering with the release of neuronal ACh.