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Medical Pharmacology > Cholingergics > Flashcards

Cholingergics Flashcards

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USMLE® Step 1 flashcards
1
Q
  • Cimetidine (OAT)
  • Proadifen (OCT)
  • Probenecid
A
  • Drug metabolism inhibitor
  • Decrease metabolism by direct enzyme inhibitor
  • Common site of drug-drug interaction
  • Increase circulating drug level
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2
Q
  • Ethanol

- Phenobarbital

A
  • Drug metabolism activators
  • Increase metabolism by enhanced synthesis, reduced degradation, and direct enzyme action
  • Increase toxicity
  • Decrease circulating drug level
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3
Q

Bethanechol

A
  • Cholinergic agonist – synthetic choline ester
  • M receptors– CH3 and NH2 groups – para activation – especially GI tract
  • Para hyperactivity
  • Stimulate smooth muscle post-operatively – increased GI motility, sphincters relax, stimulate secretions
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4
Q

Carbachol

A
  • Cholinergic agonist – synthetic choline ester
  • M receptors –NH2 is poor substrate for AchE (prolongs drug action) - para activation
  • Para hyperactivity
  • Wide-angle glaucoma (constrict ciliary muscle)
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5
Q

Methacholine

A
  • Cholinergic agonist – synthetic choline ester
  • M receptors – CH3 group decreases interaction with N receptors - para activation
  • Para hyperactivity
  • Slow heart in severe tachycardia`
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6
Q

Pilocarpine

A

*Cholinergic agonist – natural alkaloid
*M receptor selective -
Para activation - sweat and salivary glands (increase secretions)
*Para hyperactivity
*Glaucoma (short term treatment of acute angle-closure), treat dry mouth

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7
Q

Ambenonium

A
  • Competitive cholinesterase inhibitor - carbamate
  • Reversible – short acting- indirect para activation (keeping ACh in synapse)
  • Paralysis, respiratory failure, sweating, GI cramps, salivation, miosis, tearing
  • Myasthenia gravis
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8
Q

Edrophonium

A
  • Competitive cholinesterase inhibitor - simple alcohol with quartenary ammonium
  • Reversible – short acting- indirect para activation (keeping ACh in synapse)
  • Paralysis, respiratory failure, sweating, GI cramps, salivation, miosis, tearing
  • Paralysis, respiratory failure, sweating, GI cramps, salivation, miosis, tearing
  • Myasthenia gravis, ileus, arrhythmias, reversal of neuromuscular blockade (short)
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9
Q

Neostigmine

A

*Competitive cholinesterase inhibitor – carbamate with quartenary ammonium
*Reversible – short acting
indirect para activation (keeping ACh in synapse)
*Paralysis, respiratory failure, sweating, GI cramps, salivation, miosis, tearing
*Myasthenia gravis, ileus, arrhythmias, reversal of neuromuscular blockade (Long)

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10
Q

Physostigmine

A

*Competitive cholinesterase inhibitor – carbamate with tertiary amine
*Reversible – short acting
indirect para activation (keeping ACh in synapse)
*Paralysis, respiratory failure, sweating, GI cramps, salivation, miosis, tearing
*Paralysis, respiratory failure, sweating, GI cramps, salivation, miosis, tearing
*Myasthenia gravis

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11
Q
  • Diisopropyl-fluorophosphate
  • Echothiopate
  • Carbaryl
  • Malathion
  • Parathion
  • Tetraethyl-pyrophosphate
A

*Noncompetitive cholinesterase inhibitor – OP insecticie
*Reacts more with PChE – irreverislbe – long acting, very toxic - indirect para activation (keeping ACh in synapse)
*Paralysis, respiratory failure, sweating, intestinal cramps, salivation, miosis, tearing
*Echothiopate for glaucoma
Malathion for head lice

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12
Q
  • Sarin

- Soman

A
  • Noncompetitive cholinesterase inhibitor – nerve gas
  • Reacts more with PChE – irreverislbe – long acting, very toxic - indirect para activation (keeping ACh in synapse)
  • Paralysis, respiratory failure, sweating, GI cramps, salivation, miosis, tearing
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13
Q

Pralidoxime

A
  • AchE reactivator – cholinesterase inhibitor
  • Reactivates AChE (must occur before AChE aging)
  • Little CNS effects
  • Step 2 following OP intoxication
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14
Q

Atropine

A

*Cholinergic antagonist – highly muscarinic selective (low potency at nicotinic), no M subtype selectivity – 3 amine
*Quickly distributed in CNS 30-60 minutes – salivary, bronchial, and sweat glands are most sensitive
Parasympathetic inhibition - long-acting eye effects (mydriasis and cycloplegia), decreases gastric secretions, therapeutic doses only mild vagal stimulation
*Increased body temperature due to impaired ability to sweat (atropine fever), hallucinations, amnesia, sedation, excitement, dry mouth
*OP and cholinergic agonist toxicity, elicit tachycardia following brady from MI, anti-parkinson, relieves urinary incontinence, mydriasis (7-10 days), anti-motion sickness

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15
Q

Homatropine

A
  • Cholinergic antagonist – muscarinic selective - 3 amine
  • Parasympathetic inhibition - intermediate length eye effects (mydriasis and cycloplegia)
  • Hallucinations, amnesia, sedation, excitement, dry mouth
  • Mostly used for eye effects (topical agent) – mydriasis (1-3 days)
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16
Q

Scopolamine

A

*Cholinergic antagonist – very muscarinic selective – 3 amine
*Quickly distributed after administration, primarily central effects
Parasympathetic inhibition - short acting eye effects (mydriasis and cycloplegia)
*Sedation and dry mouth, hallucinations, amnesia, sedation, excitement
*Anti-motion sickness, amnesia (pre-anesthetic), mydriasis (3-7 days), induction of amnesia

17
Q

Methscopolamine

A
  • Cholinergic antagonist – muscarinic selective – 4 ammonium
  • PNS activity only - parasympathetic inhibition
  • Dry mouth, tachycardia, red skin, excess mydriasis, cycloplegia, dry eyes, urinary retention
  • Mostly GI diseases
18
Q

Trihexyphenidyl

A
  • Cholinergic antagonist – muscarinic selective – 3 amine
  • Parasympathetic inhibition
  • Hallucinations, amnesia, sedation, excitement
  • Decrease uncoordinated movement and excess salivation for parkinsons
19
Q

Tropicamide

A
  • Cholinergic antagonist – muscarinic selective – 3 amine
  • Parasympathetic inhibition - very short acting eye effects (mydriasis and cycloplegia)
  • Hallucinations, amnesia, sedation, excitement
  • Mostly used as topical ocular treatment – mydriasis (6 hours)
20
Q

Cyclopentolate

A
  • Cholinergic antagonist – muscarinic selective
  • Parasympathetic inhibition
  • Dry mouth, tachycardia, red skin, excess mydriasis, cycloplegia, dry eyes, urinary retention
  • Mydriasis – 1 day
21
Q

Ipratropium

A
  • Cholinergic antagonist – muscarinic selective – 4 ammonium
  • Parasympathetic inhibition – bronchodilation, tachycardia, decreased salivation
  • Dry mouth, tachycardia, red skin, excess mydriasis, cycloplegia, dry eyes, urinary retention
  • Topical - minimizes mucociliary clearance issues (pts with airway problems – COPD)
22
Q

Tiotropium

A
  • Cholinergic antagonist – muscarinic selective
  • Parasympathetic inhibition – longer acting
  • Dry mouth, tachycardia, red skin, excess mydriasis, cycloplegia, dry eyes, urinary retention
  • Topical - targets bronchodilation and minimizes mucociliary clearance issues
23
Q
  • Darifenacin
  • Solifenacin
  • Tolterodine
A
  • Cholinergic antagonist – M3 selective
  • Parasympathetic inhibition – longer acting relaxation of smooth muscle in GU system
  • Excessive urinary retention
  • Urinary urgency, bladder spasms
24
Q

Mecamylamine

A

*Cholinergic antagonist – nicotinic selective – 2 amine – nondepolarizing competitive antagonists
*Inhibit neurotransmission by N1 receptors in both para and symp ganglia
Parasympathetic and sympathetic inhibition – very broad effects
*Tremors, confusion, seizures, mania, depression
*Improve absorption from GI tract (oral – 12 hours), adjunct therapy for hypertension and peripheral vascular disease

25
Q

Trimethaphan

A

*Cholinergic antagonist – nicotinic selective – sulfonium- nondepolarizing competitive antagonists
*Inhibit neurotransmission by N1 receptors in both para and symp ganglia
Parasympathetic and sympathetic inhibition – very broad effects
*Excessive hypotension and possible brain anoxia
*IV infusion use (lasts minutes), adjunct therapy for hypertension and peripheral vascular disease, short-acting IV to minimize blood loss in surgery

26
Q

Succinylcholine

A

*Cholinergic antagonist – depolarizing, noncompetitive receptor agonist for ACh action
*Systemic activity is very short-lived (rapid hydrolysis by plasma ChE)
Parasympathetic inhibition
*Don’t use with CHF, burns, trauma, or neuromuscular disease patients
*Muscle relaxation for surgery, tracheal intubation, control of ventilation, convulsions

27
Q

Curare

A
  • Cholinergic antagonist – non-depolarizing – long acting, benzylisoquinoline
  • Compete with ACh for binding to N2 receptor sites - motor weakness – total flaccid paralysis
  • Check respirations and ventilation, bronchial airway obstruction
  • Muscle relaxation for surgery, tracheal intubation, control of ventilation, convulsions
28
Q

Atracurium

A
  • Cholinergic antagonist – non-depolarizing
  • Compete with ACh for binding to N2 receptor sites - motor weakness – total flaccid paralysis
  • Check respirations and ventilation, bronchial airway obstruction
  • Muscle relaxation for surgery, tracheal intubation, control of ventilation, convulsions
29
Q

Cisatracurium

A
  • Cholinergic antagonist – non-depolarizing – intermediate length, benzylisoquinoline
  • Compete with ACh for binding to N2 receptor sites - motor weakness – total flaccid paralysis
  • Check respirations and ventilation, bronchial airway obstruction
  • Muscle relaxation for surgery, tracheal intubation, control of ventilation, convulsions
30
Q

Mivacurium

A
  • Cholinergic antagonist – non-depolarizing – short acting, benzylisoquinoline
  • Compete with ACh for binding to N2 receptor sites - motor weakness – total flaccid paralysis
  • Check respirations and ventilation, bronchial airway obstruction
  • Muscle relaxation for surgery, tracheal intubation, control of ventilation, convulsions
31
Q

Pancuronium

A
  • Cholinergic antagonist – non-depolarizing – long acting, ammonio steroid
  • Compete with ACh for binding to N2 receptor sites - motor weakness – total flaccid paralysis
  • Check respirations and ventilation, bronchial airway obstruction
  • Muscle relaxation for surgery, tracheal intubation, control of ventilation, convulsions
32
Q

Vecuronium

A
  • Cholinergic antagonist – non-depolarizing – intermediate length, ammonio steroid
  • Compete with ACh for binding to N2 receptor sites - motor weakness – total flaccid paralysis
  • Check respirations and ventilation, bronchial airway obstruction
  • Muscle relaxation for surgery, tracheal intubation, control of ventilation, convulsions

Medical Pharmacology (26 decks)

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