Cholinergic Antagonist Flashcards

0
Q

Scopolamine

A

Isopto Hyoscine/ transderm scop. Also a tertiary I mean plant alkaloid produces Peru Friel effect similar to those of atropine although has greater action on CNS. Anti-motion sickness produces sedation but at higher doses produces excitement

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1
Q

Atropine

A

Isopto atropine. Tertiary a mean belladonna alkaloid with high affinity for muscarinic receptors. Binds competitively and prevents ACH from binding to sites. Block muscarinic activity and I resulting in mydriasis. Reduce his activity in G.I. tract low doses is a slight decrease in heart rate at higher doses causes increase in heart rate. Produces dryness of mouth

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2
Q

Ipatropium and tiotropium

A

Atrovent, spiriva handi haler. Quaternary derivatives of atropine these agents are use for bronchodilators. For treatment of bronchospasm associated with COPD. Tiotropium has the advantage of one daily dose

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3
Q

Tropicamide and cyclopentolate

A

Midryacyl/tropicacyl, ak-pentolate/cyclogyl. Ophthalmic solution for my dryasis and cycloplegia.

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4
Q

Benzotropine and trihexyphenidyl

A

Cogentin,artane. Parkinson’s disease

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5
Q

Darfenacin,fesoterodine,oxybutnin,solifenacin,tolterodine,trospiumchloride

A

Enablex,toviaz,ditropan,vesicare,detrol,sanctuary. Synthetic atropine like drugs used to treat overactive bladder blocks muscarinic receptors in bladder

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6
Q

Ganglionic blockers

A

Block nicotinic receptors of both parasympathetic and sympathetic autonomic ganglia some also block I am channels show no selectivity toward parasympathetic or sympathetic ganglia. not effective as neuromuscular antagonist

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7
Q

Nicotine

A

Depolarizes ganglia resulting in stimulation then paralysis of ganglia.

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8
Q

Neuromuscular blocking agents

A

Block cholinergic transmission between motor nerve endings and nicotinic receptors on skeletal muscle. Act as either antagonists (nondepolarizing type) Or as agonist (depolarizing type).

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9
Q

Neuromuscular blockers (non de polarizing competitive drugs)

A

Cisatracurium(nimbex), pancuronium (pavulon), rocuronium (zemuron), vecoronium.

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10
Q

Nondepolarizing competitive blockers drug interactions cholineesterase inhibitors

A

Choline esterase inhibitor’s reverse action of nondepolarizing neuromuscular blockers. However with increased dosage cholinesterase inhibitor’s can cause a depolarizing block as a result of elevated acetylcholine concentrations.

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11
Q

Halogenated hydrocarbon anesthetics

A

Drugs like desflurane enhance neuromuscular blockade by stabilizing NMJ

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12
Q

Aminoglycoside antibiotics

A

Gentamicin and tobramycin inhibit acetylcholine release from cholinergic nerves by competing with calcium ions.

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13
Q

Calcium channel blocker’s

A

Increase neuromuscular blockade of competitive blockers

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14
Q

Depolarizing neuromuscular blocking agents

A

People arrive plasma membrane of muscle fiber similar to acetylcholine. However these agents are more resistant to degradation by acetylcholine esterase. Succinylcholine is only depolarizing muscle relaxant used today.

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16
Q

Succinylcholine

A

Anectine, quelicin. Attaches to nicotinic receptor and Acts like acetylcholine to depolarize Junction. Remains in synaptic little longer than acetylcholine. Useful for endotracheal intubation

17
Q

glycopyrrolate

A

robinul

18
Q

propantheline

A

hyperhydrosis

19
Q

trimethophan

A

arfonad. ganglionic blocker (only one)

20
Q

typical dose for atropine

A

.4-1.0mg For bradycardia, repeat q 3-5 minutes up to 3X

21
Q

robinul dose

A

.2-.6 mg

22
Q

how do we use these drugs

A
Patients with (advanced) heart disease often have increased parasympathetic tone (what does that do?)
-Used most commonly for symptomatic bradycardia (what’s this?), pulseless electrical activity/electromechanical dissociation (what’s this?), and AV block (what’s this?)
23
Q

side effects of antimuscarinics

A

tachycardia,dry mouth,

24
Q

What are the effects of ganglionic blockers?”

A

PROFOUND hypotension via loss of sympathetic tone to the vasculature and histamine release.

  • Predictably…Negative chronotrope, negative inotrope (with no reflex tachycardia…why?)
  • Profound constipation
25
Q

doses for trimethophan (arfonad)

A

Given IV

  • Very short duration of action (5-15 mins) -Typical adult dose:
  • 1.0-3.0 mg bolus -0.5-6.0 mg/min
26
Q

therapeutic uses of neuromuscular blockers

A

Used extensively in surgery to prevent patient movement.

• Does NOT sedate, tranquilize, or anesthetize the patient!!!!

27
Q

Depolarizing Neuromuscular Blocker Logic

A

phase 1:membrane depolarizes which causes transient contractions, followed by flaccid paralysis
phase 2:membrane repolarizes but is desensitized to ach
short acting less than 8 minutes

28
Q

glycopyrrolate

A

robinul