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Neuro Exam 2 > Cholinergic Drugs > Flashcards

Cholinergic Drugs Flashcards

1
Q

All choline esters and natural alkaloids activate ___, ___and ____receptors

A

All choline esters and natural alkaloids activate M1, M2 and M3 receptors

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2
Q
  • Activation of postsynaptic receptors alters the ____ of ____ organs.
  • Activation of presynaptic receptors _____ the release of various ______
A
  • Activation of postsynaptic receptors alters the function of effector organs.
  • Activation of presynaptic receptors inhibits the release of various neurotransmitters
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3
Q

Initial activation on N-receptors (nicotinic receptors) causes ______of the ____-_______ cell membrane which triggers the ____ ______ and therefore the response of the effector organ.

A

Initial activation on N-receptors (nicotinic receptors) causes depolarization of the post-junctional cell membrane which triggers the action potential and therefore the response of the effector organ.

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4
Q

Prolonged activation of N-receptors causes a persistent _____of post-junctional cell membrane which prevents the _____to the _____ state, and the _____membrane is resistant to further _____ and the response of the effector organ is ______(known as depolarization blockade).

A

Prolonged activation of N-receptors causes a persistent depolarization of post-junctional cell membrane which prevents the return to the resting state, and the depolarized membrane is resistant to further depolarization and the response of the effector organ is blocked (known as depolarization blockade).

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5
Q

muscarinic effects= _____ effects

A

parasympathetic

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6
Q

cholinergic agonists have a _____ effect, activating the ______ nervous system responses.

A

muscarinic, parasympathetic

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7
Q

Acetylcholine is highly susceptible to ____ while carbachol and bethanechol are not.

A

cholinesterases

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8
Q

Do choline esters cause increased or decreased heart rate?

A

decreased

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9
Q

Generalized vasodilation is caused by what receptor?

A

M3

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10
Q

Increased tone, amplitude of contractions, peristaltic activity and secretions of GI tract is caused by what receptor?

A

M3

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11
Q

Contraction of the lower esophageal sphincter is caused by what receptor?

A

M3

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12
Q

Increased ureteral peristalsis is caused by what receptor?

A

M1

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13
Q

Contraction of detrussor muscle in GU system is caused by what receptor?

A

M3

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14
Q

Relaxation of trigone and internal sphincter of urethra is caused by what receptor?

A

M3

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15
Q

Erection in male is caused by what receptor?

A

M3

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16
Q

Bronchial smooth muscle contraction is caused by what receptor?

A

M3

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17
Q

Increased tracheobronchial secretions is caused by what receptor?

A

M3

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18
Q

Increased secretion of sweat glands is caused by what receptor?

A

M3

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19
Q

Pupil constriction and lacrimal glands are activated by what receptor?

A

M3

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20
Q

Choline ester absorption by oral route is _____; hydro____.

A

Choline ester absorption by oral route is poor; hydrophilic.

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21
Q

Choline esters are distributed to _____ ____ only, quaternary state drugs do not enter the ______.

A

Choline esters are distributed to peripheral tissues only, quaternary state drugs do not enter the CNS.

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22
Q

Carbachol and bethanechol are _____to hydrolysis by _____

A

Carbachol and bethanechol are resistant to hydrolysis by cholinesterases

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23
Q

Is acetylcholine resistant to cholinesterases?

A

no

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24
Q

Choline esters are excreted by the ____

A

kidney

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25
Q

Acetylcholine and carbachol are administered by _____ _____ on the _______.

A

Acetylcholine and carbachol are administered by topical instillation on the conjunctiva.

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26
Q

Bethanechol is administered by ______or_____\_

A

Bethanechol is administered by mouth or subcutaneously.

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27
Q

Adverse effects of choline esters when given locally on the conjunctiva (Carbachol, Ach):

  • Visual difficulty on _____ vision or in ___ _____.
  • Reddening, stinging and burning of the conjunctiva.
  • Postoperative ______.
  • ____ (rare, with long term use!!)
  • ______detachment (with long term use!!)
A

Adverse effects of choline esters when given locally on the conjunctiva (Carbachol, Ach):

  • Visual difficulty on far vision or in dim light.
  • Reddening, stinging and burning of the conjunctiva.
  • Postoperative iritis.
  • Cataract (rare, with long term use!!)
  • Retinal detachment (with long term use!!)
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28
Q

Adverse effects of choline esters when given systemically (Bethanechol):

  • Nausea and vomiting, abdominal pain, diarrhea
  • _______ cough
  • Sweating, lacrimation, ______
  • ____ and _____of the skin
  • Urinary _____
  • ______ (M3 via NO)
A

Adverse effects of choline esters when given systemically (Bethanechol):

  • Nausea and vomiting, abdominal pain, diarrhea
  • Bronchospasm, cough
  • Sweating, lacrimation, salivation
  • Flushing and warmth of the skin
  • Urinary urgency
  • Hypotension (M3 via NO)
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29
Q

Contraindications and precautions of choline esters given systemically:

  • Asthma, ____ ____ ___disease.
  • Cardiac _____, coronary artery disease, _____ disease, hypotension.
  • Peptic ulcer disease, GI obstruction, irritable bowel disease, inflammatory bowel disease, peritonitis.
  • Urinary tract _____.
  • ____thyroidism.
A

Contraindications and precautions of choline esters given systemically:

  • Asthma, chronic obstructive pulmonary disease.
  • Cardiac arrhythmias, coronary artery disease, myocardial disease, hypotension.
  • Peptic ulcer disease, GI obstruction, irritable bowel disease, inflammatory bowel disease, peritonitis.
  • Urinary tract obstruction.
  • Hyperthyroidism.
30
Q
  • Pilocarpine is a ____ ____ contained in ____ of the genus Pilocarpus.
  • Muscarine is a _____ ______compound contained mainly in ______ of the genus Inocybe and Clitocybe.
A
  • Pilocarpine is a tertiary amine contained in plants of the genus Pilocarpus.
  • Muscarine is a quaternary ammonium compound contained mainly in mushrooms of the genus Inocybe and Clitocybe.
31
Q
  • Peripheral effects of natural alkaloids are very similar to those of ____ _____. Stimulation of ____and ______ is particularly prominent.
  • Central effects include _____, excitation, _____ and tremors
A
  • Peripheral effects of natural alkaloids are very similar to those of choline esters. Stimulation of salivation and sweating is particularly prominent.
  • Central effects include arousal, excitation, headache and tremors
32
Q

Adverse effects of natural alkaloids:

  • Most adverse effects are very similar to those of ___ _____
  • Poisoning produced by mushrooms is called ____.
  • Symptoms of mycetism from muscarine containing mushrooms develop within _______minutes of ingestion and include salivation, lacrimation, sweating, nausea and vomiting, visual disturbances, abdominal colic, bronchospasm, bradycardia, hypotension, headache, tremors, confusion, convulsions and coma.
  • Contraindications and precautions: Very similar to those of ____ _____
A

Adverse effects of natural alkaloids:

  • Most adverse effects are very similar to those of choline esters.
  • Poisoning produced by mushrooms is called mycetism.
  • Symptoms of mycetism from muscarine containing mushrooms develop within 30-60 minutes of ingestion and include salivation, lacrimation, sweating, nausea and vomiting, visual disturbances, abdominal colic, bronchospasm, bradycardia, hypotension, headache, tremors, confusion, convulsions and coma.
  • Contraindications and precautions: Very similar to those of choline esters.
33
Q

Symptoms of muscarine mushroom toxicity typically occur within 1 hour of ingestion, last for _____hours.

Symptoms resolve in most cases without drug therapy or with a dose of ____ when excessive bronchial secretions compromise_______or bradycardia

A

Symptoms of muscarine mushroom toxicity typically occur within 1 hour of ingestion, last for 4-24 hours.

Symptoms resolve in most cases without drug therapy or with a dose of atropine when excessive bronchial secretions compromise breathing or bradycardia

34
Q

Pilocarpine

  • Used locally in case of ____-_____ _______
  • Sometimes used _____ in case of ______due to radiation therapy or associated with ______ syndrome
A

Pilocarpine

  • Used locally in case of open-angle glaucoma
  • Sometimes used orally in case of xerostomia due to radiation therapy or associated with Sjögren’s syndrome
35
Q

Cholinesterase inhibitors can be:

  • Reversible:_____ (physostigmine and neostigmine), _____ (edrophonium), others (donepezil)
  • Irreversible: _______ (organophosphorus derivatives)
A

Cholinesterase inhibitors can be:

  • Reversible: carbamates (physostigmine and neostigmine), alcohols (edrophonium), others (donepezil)
  • Irreversible: organophosphates (organophosphorus derivatives)
36
Q

Mechanism of action for cholinesterase inhibitors:

  • Are ______ for both acetylcholinesterase and butyrylcholinesterase.
  • The ____ of these enzymes for Anti-ChE is _____Xs higher than that for Ach. and the drugs are able to ____ both enzymes.
  • Most effects of Anti-ChEs of are due to _____of ________
A

Mechanism of action for cholinesterase inhibitors:

  • Are substrates for both acetylcholinesterase and butyrylcholinesterase.
  • The affinity of these enzymes for Anti-ChE is 1000Xs higher than that for Ach. and the drugs are able to inhibit both enzymes.
  • Most effects of Anti-ChEs of are due to inhibition of acetylcholinesterase
37
Q

Edrophonium reversibly binds to the ____ ____of the enzyme so preventing _____access. The bond is short-lived (_____minutes)

A

Edrophonium reversibly binds to the active site of the enzyme so preventing Ach access. The bond is short-lived (2-10 minutes)

38
Q

Carbamates undergo a ___-____ _____similar to that of Ach. However the carbamoylated enzyme is more ______ to hydrolysis and the second step is more______ (____hours).

A

Carbamates undergo a two-step hydrolysis similar to that of Ach. However the carbamoylated enzyme is more resistant to hydrolysis and the second step is more prolonged (1-6 hours).

39
Q

Some quaternary carbamates (neostigmine) also can directly activate _____receptors at the ______ _____.

A

Some quaternary carbamates (neostigmine) also can directly activate nicotinic receptors at the neuromuscular junction.

40
Q

Irreversible inhibitor mechanism of action:

  • Organophosphates bind to the ______ site.
  • The phosphorylated enzyme is extremely _____.
  • The phosphorus-enzyme bond is further strengthened with time by the loss of one ____ ____, a process called ____.
A

Irreversible inhibitor mechanism of action:

  • Organophosphates bind to the esteratic site.
  • The phosphorylated enzyme is extremely stable.
  • The phosphorus-enzyme bond is further strengthened with time by the loss of one alkyl group, a process called aging.
41
Q

Cholinesterase inhibitors that can enter the CNS may cause:

  • After moderate doses: increased _____, stimulation of various _____activities.
  • After high doses: confusion, _____, loss of r_____, generalized convulsions, coma and central respiratory _____.
A

Cholinesterase inhibitors that can enter the CNS may cause:

  • After moderate doses: increased alertness, stimulation of various central activities.
  • After high doses: confusion, ataxia, loss of reflexes, generalized convulsions, coma and central respiratory paralysis.
42
Q

Cholinesterase inhibitor effects in eye, respiratory, GI, urinary systems:

•______tone is the predominant tone in these systems and the effects of Anti-ChE are similar to those of ____ ___ ______.

A

Cholinesterase inhibitor effects in eye, respiratory, GI, urinary systems:

•Parasympathetic tone is the predominant tone in these systems and the effects of Anti-ChE are similar to those of direct acting cholinomimetics.

43
Q

The net effects of cholinesterase inhibitors on cardiovascular system depend on the dose:

  • After moderate doses: _______ and no change or a modest fall in ____ ______.
  • After high doses: marked bradycardia and ______.
A

The net effects of cholinesterase inhibitors on cardiovascular system depend on the dose:

  • After moderate doses: bradycardia and no change or a modest fall in blood pressure.
  • After high doses: marked bradycardia and hypotension.
44
Q

Effects of cholinesterase inhibitors at the neuromusclar junction:

  • After moderate doses: _____ strength of ____.
  • After high doses: _____, neuromuscular _____.
A

Effects of cholinesterase inhibitors at the neuromusclar junction:

  • After moderate doses: increased strength of contraction.
  • After high doses: fasciculations, neuromuscular blockade.
45
Q

Absorption of cholinesterase inhibitors:

Oral bioavailability:

  • good for ____ _____
  • low for ____ ______ compounds
  • very good for _______
  • Organophosphates are absorbed by ____ ____including the _____
A

Absorption of cholinesterase inhibitors:

Oral bioavailability:

  • good for tertiary amines
  • low for quaternary ammonium compounds
  • very good for organophosphates
  • Organophosphates are absorbed by all routes including the skin.
46
Q

Distribution of cholinesterase inhibitors:

  • ____ ____ enter the CNS.
  • Quaternary compounds distribute only in ____ ____.
  • Organophosphates distribute in ____ _____.
A

Distribution of cholinesterase inhibitors:

  • Tertiary amines enter the CNS.
  • Quaternary compounds distribute only in peripheral tissues.
  • Organophosphates distribute in all tissues.
47
Q

biotransformation of cholinesterase inhibitors:

  • Carbamates are hydrolyzed by ____ _____.
  • Organophosphates are hydrolyzed by enzymes found in _____ and ____ called _____.
A

biotransformation of cholinesterase inhibitors:

  • Carbamates are hydrolyzed by plasma esterases.
  • Organophosphates are hydrolyzed by enzymes found in plasma and liver, called paraoxonases.
48
Q

Excretion of cholinesterase inhibitors:

  • _____are excreted by the ______.
  • Half-lives: edrophonium, _____ physostigmine, neostigmine ______
A

Excretion of cholinesterase inhibitors:

  • Metabolites are excreted by the kidney.
  • Half-lives: edrophonium, 1-10 minutes physostigmine, neostigmine 1-2 hours
49
Q

Acute poisoning from cholinesterase inhibitors:

Symptoms and signs appear within _____minutes after ____, or within _____minutes after _____ or ______absorption.

A

acute poisoning from cholinesterase inhibitors:

Symptoms and signs appear within 5-10 minutes after inhalation, or within 30-60 minutes after gastrointestinal or percutaneous absorption.

50
Q

adverse effect of cholinesterase inhibitors:

When given locally for the treatment of glaucoma _____ is a frequent adverse effect (treated for more than _____months!!)

A

adverse effect of cholinesterase inhibitors

When given locally for the treatment of glaucoma cataract is a frequent adverse effect (treated for more than 6 months!!)

51
Q

Treatment of adverse effects of cholinesterase inhibitors:

  • Alleviation of convulsion with ______
  • Administration of _____
  • Administration of a ______ ______
A

Treatment of adverse effects of cholinesterase inhibitors:

  • Alleviation of convulsion with diazepam
  • Administration of atropine
  • Administration of a cholinesterase re-activator
52
Q

Chemistry of cholinesterase reactivators:

  • All compounds are _____ (R-CH=NOH).
  • Pralidoxime is a _______oxime.
  • Obidoxime is a _____ oxime.
A

Chemistry of cholinesterase reactivators:

  • All compounds are oximes (R-CH=NOH).
  • Pralidoxime is a monoquaternary oxime.
  • Obidoxime is a biquaternary oxime.
53
Q

Mechanism for Cholinesterase Reactivators:

  • Spontaneous hydrolytic regeneration of _______AchE is exceedingly long.
  • Oximes have high affinity for the _______ atom and can rapidly regenerate the enzyme if the complex did not undergo aging.
  • Oximes themselves have weak _____ activity and are not able to regenerate _____ blocked by ______.
A

Mechanism for Cholinesterase Reactivators:

  • Spontaneous hydrolytic regeneration of phosphorylated AchE is exceedingly long.
  • Oximes have high affinity for the phosphorus atom and can rapidly regenerate the enzyme if the complex did not undergo aging.
  • Oximes themselves have weak AchE activity and are not able to regenerate AchE blocked by carbamates.
54
Q

Pharmacological effects of cholinesterase reactivators:

  • The reactivating action of oxides is:
  • most pronounced at the _____ _____
  • less striking at ____ _____sites
  • insignificant in the _____.
A

Pharmacological effects of cholinesterase reactivators:

  • The reactivating action of oxides is:
  • most pronounced at the neuromuscular junction;
  • less striking at autonomic effector sites
  • insignificant in the CNS.
55
Q

Pharmacokinetics of cholinesterase reactivators:

  • Oral bioavailability: < 1%. Vd: ~ 15 L.
  • The drug does not enter the ______
  • Half-life: _______ hours
A

Pharmacokinetics of cholinesterase reactivators:

  • Oral bioavailability: < 1%. Vd: ~ 15 L.
  • The drug does not enter the brain
  • Half-life: 1-1.5 hours
56
Q

Cholinesterase reactivators can be therapeutically used for poisoning by _______insecticides

A

Cholinesterase reactivators can be therapeutically used for poisoning by organophosphate insecticides

57
Q

Contraindications of cholinesterase inhibitors:

  • GI and urinary tract obstruction, inflammatory bowel disease, peritonitis.
  • Cholinergic crisis in the ______ patient.
  • Asthma, chronic obstructive pulmonary disease.
  • _____tension, cardiac arrhythmias, coronary artery disease, myocardial disease.
  • Peptic ulcer disease.
  • ______thyroidism.
  • Seizure disorder.
  • _______disease.
A

Contraindications of cholinesterase inhibitors:

  • GI and urinary tract obstruction, inflammatory bowel disease, peritonitis.
  • Cholinergic crisis in the myasthenic patient.
  • Asthma, chronic obstructive pulmonary disease.
  • Hypotension, cardiac arrhythmias, coronary artery disease, myocardial disease.
  • Peptic ulcer disease.
  • Hyperthyroidism.
  • Seizure disorder.
  • Parkinson disease.
58
Q

Therapeutic uses of cholinesterase inhibitors in neuromuscular system:

Myasthenia gravis diagnosis

  • ________ is used:
  • to confirm the clinical diagnosis: the test is positive when a brief ______ in muscular ______ is observed;
  • to distinguish between cholinergic crisis and myasthenic crisis

Myasthenia gravis treatment

  • Neostigmine, pyridostigmine, ambenonium (PO).
  • ______ is generally co-administered to control _____effects.
A

Therapeutic uses of cholinesterase inhibitors in neuromuscular system:

Myasthenia gravis diagnosis

  • Edrophonium IV is used:
  • to confirm the clinical diagnosis: the test is positive when a brief improvement in muscular strength is observed;
  • to distinguish between cholinergic crisis and myasthenic crisis

Myasthenia gravis treatment

  • Neostigmine, pyridostigmine, ambenonium (PO).
  • Atropine is generally co-administered to control muscarinic effects.
59
Q

Therapeutic uses of cholinergic drugs:

-_____ angle glaucoma

  • ________ (pilocarpine, bethanechol)
  • Postoperative nonobstructive _____ (bethanechol, neostigmine)
  • Postoperative and postpartum urinary _____ (bethanechol, neostigmine)
  • Neurogenic ______(bethanechol, neostigmine
A

Therapeutic uses of cholinergic drugs:

-open angle glaucoma

  • Xerostomia (pilocarpine, bethanechol)
  • Postoperative nonobstructive ileus (bethanechol, neostigmine)
  • Postoperative and postpartum urinary retention (bethanechol, neostigmine)
  • Neurogenic bladder (bethanechol, neostigmine
60
Q

Pralidoxime is a ______

A

cholinesterase reactivator

61
Q

Parathion is a _____

A

cholinesterase irreversible inhibitor

62
Q

Edrophonium is a _____

A

cholinesterase reversible inhibitor

63
Q

Physostigmine is a _____

A

cholinesterase reversible inhibitor

64
Q

Neostigmine is a ____

A

cholinesterase reversible inhibitor

65
Q

Donepezil is a _______

A

cholinesterase reversible inhibitor

66
Q

Pilocarpine is a ____-

A

natural alkaloid

67
Q

Muscarine is a _____

A

natural alkaloid

68
Q

Acetylcholine is a _____

A

choline ester

69
Q

Carbachol is a _____

A

choline ester

70
Q

Bethanechol is a _____

A

choline ester

Neuro Exam 2 (18 decks)

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