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CMBM Exam 2 > Anticholinergics > Flashcards

Anticholinergics Flashcards

1
Q

Muscarinic blockers belladonna alkaloid drugs

A
  • Atropine

- Scopolamine

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2
Q

Muscarinic blockers tertiary amines drugs

A
  • Tolterodine and Oxybutynin (Antispasmodics)
  • Tropicamide (Mydriatics)
  • Benztropine and Diphenhydramine (Antiparkinsonian)
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3
Q

Muscarinic blockers quarternary amines drugs

A
  • Glycopyrrolate
  • Ipratropium
  • Tiotropium
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4
Q

Ganglionic Blocking Agent drugs

A
  • Nicotine (Depolarizing)
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5
Q

ANTICHOLINERGIC DRUGS MOA

A
  • Block action of ACh at cholinergic receptors throughout body
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6
Q

Anticholinergic drugs subdivisions

A
  • Muscarinic blockers
  • Ganglionic blockers
  • Neuromuscular blockers
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7
Q

Muscarinic blockers MOA

A

(e. g., atropine, propantheline)
- Inhibit cholinergic transmission at postganglionic parasympathetic receptor sites, e.g., on smooth muscle, cardiac muscle, and exocrine glands: M (muscarinic) receptors

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8
Q

Ganglionic blockers MOA

A

e. g., mecamylamine, trimethaphan
- Block cholinergic transmission at autonomic ganglia in both parasympathetic and sympathetic nerve fibers: N (nicotinic) I sites

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9
Q

Neuromuscular blockers MOA

A

e. g., pancuronium
- Reduce action of ACh at synapses between nerves and skeletal muscles (neuromuscular junction): N (nicotinic) II receptors.

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10
Q

Major pharmacologic actions of anticholinergic drugs

A
  • GI
    ↓ motility (reduced smooth muscle tone) —> constipation
    ↓ secretions
  • CV
    Tachycardia (small doses of atropine can produce bradycardia)
  • Urinary Tract
    Contraction of sphincter muscle; relaxation of detrusor muscle —> urinary retention
    -Eye
    Relaxes ciliary muscle: cycloplegia (paralysis of
    accomadation)
  • Exocrine Glands
    ↓ sweating, salivation and mucous formation (e.g., nasal)
  • Smooth Muscle
    Relaxation of non-vascular smooth muscle (e.g., biliary, bronchiolar, intestinal, uterine)
  • CNS
    Decreased sensitivity to motion
    Drowsiness, disorientation, possible hallucinations
    Decreased skeletal muscle activity (e.g., decreased tremor)
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11
Q

Belladonna alkaloid MOA

A
  • Atropine and scopolamine are the principal naturally occurring anticholinergic drugs
  • Rapidly absorbed after p.o. administration
  • Relatively selective blocking action at M receptor sites Readily enter the CNS
  • Blockade (via competitive antagonism) of acetylcholine at postsynaptic muscarinic receptor sites
  • Large doses block cholinergic transmission at autonomic ganglia and the neuromuscular junction
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12
Q

Belladonna alkaloids major therapeutic uses

A
  • Production of mydriasis and cycloplegia to facilitate eye exam
  • Preop to reduce excess salivation and preventbradycardia
  • Reduction of GI motility
  • Reduce muscarinic side effects
  • Relief of nasopharyngeal and bronchial secretions
  • Relief of bronchoconstriction
  • Prevention and relief of motion sickness
  • Treatment of enuresis
  • Treatment of sinus bradycardia
  • Sedation and amnesia
  • Antidote to overdosage with cholinergic agents
  • Relief of symptoms of parkinsonism
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13
Q

Belladonna alkaloids ADR’s

A 
GI
- Dry mouth, constipation, paralytic ileus
Cardiovascular
- Tachycardia
Ocular
- Blurred vision, increased intraocular tension
GU
- Urinary retention
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14
Q

Belladonna alkaloids contraindications

A
  • Narrow-angle glaucoma
  • Myasthenia gravis
  • Asthma (atropine)
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15
Q

Belladonna alkaloids effects increased by

A

antihistamines, tricyclic anti- depressants, antipsychotics

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16
Q

Tertiary Amines MOA

A
  • Good lipid-solubility
  • Well absorbed after p.o.
  • Wide distribution into peripheral and central tissues
17
Q

Oxybutinin ADR’s

A
  • Tertiary amine

- Bladder instability (e.g., urinary leakage)

18
Q

Tolterodine ADR’s

A
  • Tertiary amine

- Bladder instability (e.g., urinary leakage)

19
Q

Antispasmodics major therapeutic uses

A
  • Oxybutinin and Tolterodine
  • Range from slight to no anticholinergic activity
  • minimal reduction of gastric secretion
  • Direct relaxant effect on smooth muscle (nonspecific)
20
Q

Mydriatics major therapeutic uses

A
  • Tropicamide

- To produce mydriasis and cycloplegia for eye exam; also employed in treatment of uveitis

21
Q

Mydriatics ADR’s

A
  • Danger of systemic absorption; possible toxic side effects include:
    ➢ disorientation
    ➢ retrograde amnesia
    ➢ hallucinations
    ➢ cardiac arrhythmias:
  • atrial fibrillation; supraventricular tachycardia
    ➢ death (in children)
22
Q

Antiparkinsonian Agents

A

Employed in clinical conditions related to imbalance between acetylcholine (Ach) and dopamine (DA)

  • Benztropine
  • Diphenhydramine
23
Q

Benztropine MOA

A
  • Blockade of DA sites allows greater action of ACh

- More selective than belladonna alkaloids.

24
Q

Diphenhydramine MOA

A
  • Blockade of DA sites allows greater action of ACh
  • More selective than belladonna alkaloids
  • Antihistamine with central antichol. activity
  • Appears to have less peripheral side effects than other agents
  • Sedative effect beneficial in pts with insomnia
25
Q

Quaternary Amines drugs

A
  • Glycopyrrolate
  • Tiotropium bromide
  • Umeclidinium
26
Q

Quaternary Amines MOA

A
  • Low degree of lipid solubility:
    ➢ poor and erratic absorption.
    ➢ limited systemic distribution; do not cross BBB
  • Duration of action&raquo_space; than that of tertiary amines
27
Q

Quaternary Amines major therapeutic uses

A
  • Reduce gastric acid secretion in treatment of peptic ulcer
    ➢ ↓ motility of GI and biliary tracts in spastic discord
    ➢ ↓ motility of urinary tract in hypertonic neurogenic bladder
28
Q

Glycopyrrolate

A
  • Quarternary amine
  • Also parenteral use as preanesthetic med to: decrease saliva, reduce secretions of GI and respiratory tracts, prevent bradycardia
29
Q

Ganglionic Blocking Agents

A
  • Nicotine
30
Q

Nicotine

A
  • An alkaloid
  • Stimulatory actions prominent during cigarette smoking:
    ➢ elevated BP (stim. of adrenal medulla –→ ↑ NE and E
    ➢ increased HR ( “ )
    ➢ increased GI motility –→ diarrhea
    ➢ CNS stimulation
    ➢ increased respiration
31
Q

Nicotine major therapeutic uses

A
  • Used therapeutically as a smoking deterrent
32
Q

Nicotine ADR’s

A
  • Blocking actions occur with extremely large (toxic) doses, e.g., systemic absorption from tobacco smoke (especially by children) or inadvertent ingestion of nicotine-containing insecticides. Rapid onset of effects including:
    ➢ reduced BP
    ➢ ↑ HR (compensatory tachycardia) / irregular & weak
    ➢ confusion
    ➢ convulsions
    ➢ respiratory failure

CMBM Exam 2 (13 decks)

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