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2nd Year - Pharmacology > Antimuscarinics > Flashcards

Antimuscarinics Flashcards

1
Q

Dicyclomine hydrochloride acts on

A

M3 receptors as an intestinal antispasmodic agent; spastic colon

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2
Q

Tropicamide produces

A

Short-acting mydriasis and cycloplegia

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3
Q

Used to treat overactive bladder

A

Oxybutinin chloride
Tolterodine
Darifenacin
Solifenacin

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4
Q

Benztropine and Biperiden

A

Centrally acting

Adjunct in the therapy of all forms of Parkinsism and control of EPS

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5
Q

Ipratropium and Tiotropium

A

Used exclusively for effect on respiratory tract; bronchodilator; COPD and bronchial asthma except in acute conditions

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6
Q

Glycopyrrolate is used for

A

reducing secretions in the mouth, throat, airway, and stomach before surgery

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7
Q

Propantheline bromide

A

used for hyperhidrosis

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8
Q

Quaternary amine derivatives of synthetic and semi-synthetic antimuscarinics

A

Ipratropoium
Tiotropium
Glycopyrrolate
Propantheline bromide

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9
Q

Tertiary amine derivatives of synthetic and semi-synthetic antimuscarinics

A 
Dycyclomine
Tropicamide
Oxybutinin chloride
Tolterodine
Darifenacin
Solifenacin
Scopolamine
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10
Q

Tissues most sensitive to atropine

A

Salivary, bronchial, and sweat glands

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11
Q

Tissues least sensitive to atropine

A

Gastric parietal cells

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12
Q

Selectivity of atropine

A

Non-selective, does not distinguish among M1, M2, and M3

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13
Q

Selectivity of quaternary ammonium derivatives of atropine

A

Generally potent at muscarinic receptors and greater degree of nicotinic blockade

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14
Q

Hierarchy of relative senstivities to atropine in decreasing order

A

Salivary and sweat glands (xerostomia, anhydrosis, atropine fever)
Heart and eyes (tachycardia and blurred vision, mydriasis, cycloplegia, and reduced lacrimal secretion)
Smooth muscles (constipation, and urinary retention)
Gastric parietal glands (LAST)
CNS (TOXIC–> excitation)

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15
Q

Prominent difference in clinical manifestation between atropine and scopolamine

A

Scopolamine crosses BBB and may cause depression, drowsiness, amnesia, fatigue, dreamless sleep, reduced REM sleep, euphoria, and excitation

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16
Q

Antimuscarinic effect in the HEART

A

Modest tachycardia, blocks vagal effects on M2 receptors on SA node

17
Q

At low doses, what is the effect of antimuscarinics on the heart

A

Bradycardia due to central effect via inhibition of the secretions of the medulla (decreased catecholamines)
At higher doses, murscarinic receptors are blocked, producing modest tachycardia

18
Q

Antimuscarinic effect in the GIT

A

M3 block: Decrease tone and propulsive movements
Relaxed GIT walls
Prolonged gastric emptying time

M1 block: (by Pirenzepine and Telenzepine) inhibit gastric acid secretion

19
Q

Pirenzepine and Telenzepine action

A

M1 blockade: inhibit gastric acid secretion at lower doses without affecting the gastric walls
Acid Peptic Disease

20
Q

Dicyclomine is used in the GIT to

A

M3 block: reduce intestinal spasm

21
Q

Antimuscarinic effect in the GUT

A

M3 block: smooth muscles of the bladder and ureters are relaxed, sphincters are contracted
Slows voiding
Treatment of urgency, frequency, and overactive bladder, urinary retention in BPH

22
Q

Effective in overactive bladder and urinary incontinence

A

Selective M3 blockade:
Solifenacin
Darifenacin
Fesoteridine

23
Q

Antimuscarinic effect in the ocular system

A

Unopposed sympathetic dilator activity in the pupillary constrictor muscle –> mydriasis
Weakened contraction of the ciliary muscle (cycloplegia)–> cannot accommodate
Reduced lacrimation or sandy eyes

24
Q

Antimuscarinic effect on the respiratory tract

A

Bronchodilation
Reduced bronchial secretions
Decreased mucociliary clearance–> mucous plug
Dry mouth

25
Q

Ipratropium selectivity

A

Blocks all muscarininc receptor subtypes

26
Q

Tiotropium selectivity

A

Some selectivity in blocking M1 and M3 receptors

27
Q

Antimuscarinic effect on exocrine glands

A

Suppresses thermoregulatory sweating
Atropine fever
Dry mouth and mucous membranes (xerostomia)

28
Q

Antimuscarinic effect in the CNS

A

Drowsiness

Prevention of motion sickness (vestibular disturbances)

29
Q

ADRs of antimuscarinic drugs

A

Atropine fever (impaired thermoregulatory sweating)
Xerostomia (no secretion of sweat glands, dryness)
Atropine flush (vasodilation)
Cycloplegia (impaired accommodation)
Delirium (cortical stimulation and CNS excitation)

30
Q

If ingested orally, treatment of toxicity is done by

A

gastric lavage with activated charcoal

31
Q

First choice in antimuscarinic poisoning

A

Physostigmine IV (tertiary, can traverse the CNS)

32
Q

Anti-curare drugs

A

Neostigmine
Pyridostigmine
Ambenonium

33
Q

If poisoning due to quaternary ammonium compounds, treatment is via adminstration of

A

Neostigmine (quaternary compound)

Sympathomimetic (to reverse hypotension)

34
Q

Contraindications to the use of antimuscarinics

A

Narrow angle glaucoma
Caution in men with history of BPH
Obstructive conditions: GIT, GUT
Gastric ulcer (slows gastric emptying time)

35
Q

Used as adjunct to levodopa in Parkinsons disease

A

Benztropine
Biperiden
Trihexyphenidyl

2nd Year - Pharmacology (18 decks)

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