Anti-cholinergic drugs Flashcards

1
Q

atropine is classified as a _____ drug and a ___ ___

A

anti-muscarinic; tertiary amine

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2
Q

scopolamine is classified as a ____ drug and a ____ ___

A

anti-muscarinic; tertiary amine

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3
Q

homatropine is classified as a ____ drug and a ____ ____

A

anti-muscarinic; tertiary amine

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4
Q

Dariferain is classified as a _____ drug and a ____ ____

A

anti-muscarinic; tertiary amine

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5
Q

Benztropine is classified as a ____ drug and a ____ ____

A

Anti-muscarinic, tertiary amine

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6
Q

Glycopyrrolate is classified as a _____ drug and a ____ ____ ___

A

anti-muscarinic; quaternary ammonium compound

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7
Q

Ipratropium is classified as a ______ drug and a ____ ___ ___

A

anti-muscarinic; quaternary ammonium compound

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8
Q

Nicotine is classified as a ____ _____

A

Ganglionic stimulant

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9
Q

Mecamylamine is classified as a ____ ___

A

ganglionic blocker

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10
Q

Nicotine at lower doses has a _____ effect

A

agonist effect

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11
Q

Nicotine at higher doses has a ____ ____

A

depolarizing blockade

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12
Q

Atropine and scopolamine are ____ ______ found in several plants

A

Atropine and scopolamine are natural alkaloids found in several plants

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13
Q

M1, M2, and M3 receptors have a ____ affinity for atropine

A

high

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14
Q

M3 has ____ affinity and M1 and M2 have ____ affinity for Darifenacin

A

high;little to no

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15
Q

M1, M2, and M3, have a ____ affinity for Glycopyrrolate, Ipratropium

A

high

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16
Q

Nicotinic receptors have a ____ affinity for Glycopyrrolate, Ipratropium

A

moderate

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17
Q

Tolterodine, M3-selective antimuscarinic, to treat overactive _____

A

Tolterodine, M3-selective antimuscarinic, to treat overactive bladder

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18
Q
  • All antimuscarinic drugs ______ _____ muscarinic receptors
  • The effectiveness of this blockade (the affinity for the receptor) varies with the antagonist and with the _____ of the tissue.
A
  • All antimuscarinic drugs competitively block muscarinic receptors
  • The effectiveness of this blockade (the affinity for the receptor) varies with the antagonist and with the sensitivity of the tissue.
19
Q

Atropine and scopolamine block ______subgroups of M receptors

A

•Atropine and scopolamine block all subgroups of M receptors

20
Q

Tertiary antimuscarinic drugs have ______blocking activity at ganglionic Nn receptors.

A

Tertiary antimuscarinic drugs have negligible blocking activity at ganglionic Nn receptors.

21
Q

Quaternary compounds mainly block ______ receptors but also exhibit a significant blocking activity at _____ ____receptors

A

Quaternary compounds mainly block muscarinic receptors but also exhibit a significant blocking activity at ganglionic Nn receptors

22
Q

Oral bioavailability: variable (atropine _____; ipratropium >____)

A

Oral bioavailability: variable (atropine 50%; ipratropium >1%)

23
Q

Distribution

  • Tertiary amines distribute in _____tissues.
  • Quaternary derivatives do not enter the _____.
A

Distribution

  • Tertiary amines distribute in all tissues.
  • Quaternary derivatives do not enter the CNS.
24
Q

Biontransformation

•~ 50% of atropine and 90% of scopolamine are metabolized by the _________

A

Biontransformation

•~ 50% of atropine and 90% of scopolamine are metabolized by the liver.

25
Q

Excretion

  • About 60% of atropine is excreted by the ______.
  • Half-lives: Atropine and scopolamine: ~____ hours; Glycopyrrolate: ~ ___ hours
A

Excretion

  • About 60% of atropine is excreted by the kidney.
  • Half-lives: Atropine and scopolamine: ~3 hours; Glycopyrrolate: ~ 10 hours
26
Q

•When atropine is used to treat diarrhea, the appearance of ______is considered a side effect, but when the same drug is used to counteract sinus bradycardia, the appearance of _____ is regarded as a side effect.

A

•When atropine is used to treat diarrhea, the appearance of tachycardia is considered a side effect, but when the same drug is used to counteract sinus bradycardia, the appearance of constipation is regarded as a side effect.

27
Q

•Atropine has a good therapeutic index in adults, but a dose of ____ mg can be lethal for children.

A

•Atropine has a good therapeutic index in adults, but a dose of 5 mg can be lethal for children.

28
Q
  • In serious atropine poisoning symptoms and signs appears within ______minutes after ingestion and may last _____days.
  • Death due to _____ failure may follow a period of circulatory collapse/coma.
A
  • In serious atropine poisoning symptoms and signs appears within 30-60 minutes after ingestion and may last 2-7 days.
  • Death due to respiratory failure may follow a period of circulatory collapse/coma.
29
Q
  • Diagnosis of poisoning by anti-muscarinic drugs is easy in severe cases. An IM injection of ______ may be used for confirmation. If signs of _____ activation do not occur poisoning with antimuscarinic drug is almost certain.
  • The treatment is _____. Physostigmine is reserved for severe cases since drug can be more dangerous and no more effective than symptomatic treatment.
A
  • Diagnosis of poisoning by anti-muscarinic drugs is easy in severe cases. An IM injection of physostigmine may be used for confirmation. If signs of muscarinic activation do not occur poisoning with antimuscarinic drug is almost certain.
  • The treatment is symptomatic. Physostigmine is reserved for severe cases since drug can be more dangerous and no more effective than symptomatic treatment.
30
Q

symptomatic treatment of anti-muscarinic drug poisoning

  • Maintenance of vital signs
  • Alleviation of convulsion with _____
  • _____ control with ice bags and alcohol sponges.
A

symptomatic treatment of anti-muscarinic poisoning:

  • Maintenance of vital signs
  • Alleviation of convulsion with diazepam
  • Temperature control with ice bags and alcohol sponges.
31
Q

Poisoning with anticholinergics:

____: due to vasodilation (cause unknown)

____: due to vasodilation & hyperthermia

___: due to reduced sweating, reduced salivation, reduced fluid intake & developing dehydration

____: due to cycloplegia and mydriasis

____: due to delirium

A

Poisoning with anti-cholinergics:

RED: due to vasodilation (cause unknown)

HOT: due to vasodilation & hyperthermia

DRY: due to reduced sweating, reduced salivation, reduced fluid intake & developing dehydration

BLIND: due to cycloplegia and mydriasis

MAD: due to delirium

32
Q

Contraindications of anti-muscarinics:

–Glaucoma

–Prostatic ______

–Urinary tract obstruction

–Gastrointestinal tract obstruction

–Adynamic ileus

–Gastric ulcer

–Severe infectious _____

–_____esophagitis

–Ulcerative colitis, Crohn’ disease (toxic _____ can ensue)

–Tachyarrhythmias

–Coronary artery disease, cardiac failure

–_____thyroidism

–Children

–Elderly

A

contraindications of anti-muscarinics:

–Glaucoma

–Prostatic hypertrophy

–Urinary tract obstruction

–Gastrointestinal tract obstruction

–Adynamic ileus

–Gastric ulcer

–Severe infectious diarrhea

Reflux esophagitis

–Ulcerative colitis, Crohn’ disease (toxic megacolon can ensue)

–Tachyarrhythmias

–Coronary artery disease, cardiac failure

Hyperthyroidism

–Children

–Elderly

33
Q

Scopalamine is used for _____ sickness prevention and treatment

A

motion

34
Q

What drug do you use for these conditions?:

Visceral hypermolity and spasms

Excessive salivation

Cardiovascular disorders

Cholinesterase inhibitor overdose

Opthalmology

Preanesthetic medication

A

atropine

35
Q

What drug do you use for these conditions?

Motion sickness

Opthalmology

Preanesthetic medication

A

scopalamine

36
Q

What drug do you use for these conditions?

Opthalmology

A

homatropine

37
Q

What drug do you use for these conditions?

Neurogenic bladder

Urinary urge incontinence

A

Darifenacin

38
Q

what drug do you use for parkinson’s disease?

A

Benztropine

39
Q

What drug do you use for these conditions?

Visceral hypermotility and spasms

Cardiovascular disorders

Preanesthetic medication

A

glycopyrrolate

40
Q

What drug do you use for bronchospastic disorders?

A

Ipratropium

41
Q

ganglionic blocking drugs mechanism:

–_____blockade of nicotinic receptors (Nn) in:

a) ______ ganglia
b) adrenal medulla
c) ______ nerve terminals
d) central nervous system (mecamylamine)

A

ganglionic blocking drugs mechanism:

–Competitive blockade of nicotinic receptors (Nn) in:

a) autonomic ganglia
b) adrenal medulla
c) presynaptic nerve terminals
d) central nervous system (mecamylamine)

42
Q

Ganglionic blocking drugs cardio effects:

  • Moderate _____ in heart rate
  • _____cardiac output (in spite of the increase in heart rate, because the peripheral venous pooling decreases the preload).
  • Marked _____ in venous tone and peripheral vascular resistance (which leads to hypotension, mainly in the upright position).
  • Skin blood flow is ____, splanchnic and renal blood flow are ____.
A

Ganglionic blocking drugs cardio effects:

  • Moderate increase in heart rate
  • Decreased cardiac output (in spite of the increase in heart rate, because the peripheral venous pooling decreases the preload).
  • Marked decrease in venous tone and peripheral vascular resistance (which leads to hypotension, mainly in the upright position).
  • Skin blood flow is increased, splanchnic and renal blood flow are decreased.
43
Q
  • Hexamethonium is a ____ _____ (negligible oral absorption and access to the CNS).
  • Mecamylamine is a ___ ____ (it is active by oral route and enters the brain).
A
  • Hexamethonium is a quaternary ammonium (negligible oral absorption and access to the CNS).
  • Mecamylamine is a secondary amine (it is active by oral route and enters the brain).