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Pharmacology 1 choefsho > Drugs acting on the parasympathetic NS > Flashcards

Drugs acting on the parasympathetic NS Flashcards

1
Q

Which of the following are not indirect-acting parasympathomimetics (reversible anticholinesterases)?

  1. Physostigmine (opthalmic)
  2. Carbamate insecticides
  3. Pyridostigmine
  4. Acetylcholine
  5. Neostigmine
  6. Demecarium (opthalmic)
  7. Edrophonium
A
  1. Endogenous acetylcholine is a direct-acting parasympathomimetic

(know neostigmine, pyridostigmine, and edrophonium)

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1
Q

This indirect-acting parasympathomimetic (reversible) is available as an injection (1:4000) or as oral tablets (1:1000, 1:2000).

  1. Neostigmine (Prostigmin)
  2. Pyridostigmine (Mestinon)
  3. Edrophonium (Tensilon, Enlon)
A
  1. Neostigmine (Prostigmin)
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1
Q

A patient suspected of having myasthenia gravis (flaccid paralysis and cannot stand) was treated with Pyridostigmine at a high dose and was doing well, but now he has flaccid paralysis again. He is given Edrophonium IV and it worsens the muscle weakness. This is a:

  1. Myasthenic crisis
  2. Cholinergic crisis
A

Cholinergic crisis (decrease dose anticholinesterase)

Cholinergic crisis- treatment with excess doses of cholinesterase inhibitor

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2
Q

This indirect-acting parasympathomimetic (reversible) is very fast acting with onset at 1 minute and lasts about 10 minutes.

  1. Neostigmine (Prostigmin)
  2. Pyridostigmine (Mestinon)
  3. Edrophonium (Tensilon, Enlon)
A
  1. Edrophonium (Tensilon, Enlon)
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2
Q

A patient suspected of having myasthenia gravis (flaccid paralysis and cannot stand) is given Edrophonium IV and improves his muscle function. This is a:

  1. Myasthenic crisis
  2. Cholinergic crisis
A
  1. Myasthenic crisis (increase dose anticholinesterase)
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3
Q

This is an autoimmune neuromuscular disorder which causes immune destruction of nicotinic receptors at motor end plates.

A

Myasthenia gravis

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4
Q

Which direct-acting parasympatholytic is a quaternary ammonium compound?

  1. Aminopentamide
  2. Atropine
  3. Pyridostigmine
  4. Glycopyrrolate
  5. Oxybutynin
  6. Propantheline
A

4. Glycopyrrolate

(compared to atropine, it has a slower onset of action and longer duration; it does not absorb well orally and does not cross the BBB)

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5
Q

What type of drug affecting the PSNS blocks autonomic effects to get sympathetic signs?

A

Parasympatholytics

  • Direct acting
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7
Q

T or F. Direct-acting parasympatholytics can be called anticholinergics, antimuscarinics, and anitnicotinics.

A

False, only anticholinergics and anitmuscarinics (Atropine, Glycopyrrolate, Oxybutynin, Propantheline, Aminopentamide)

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8
Q

Which type of drug affecting the PSNS stimulates (mimics) autonomic effects to get parasympathetic signs?

A

Parasympathomimetics

  • Direct acting (acts on a receptors)
  • Indirect acting (acts somewhere close to a receptor)
    • Reversible anticholinesterases
    • Irreversible anticholinesterases
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8
Q

Which indirect-acting parasympathomimetic (reversible) is used to treat rumen atony, to stimulate GI motility, for bladder emptying, and for the reversal of competitive neuromuscular blockers (NKBs)?

  1. Neostigmine (Prostigmin)
  2. Pyridostigmine (Mestinon)
  3. Edrophonium (Tensilon, Enlon)
A
  1. Neostigmine (Prostigmin)

(also used to treat myasthenia gravis in dogs, but Pyridostigmine is used more often because it is longer acting)

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9
Q

Which of the following is not a direct-acting parasympatholytic?

  1. Aminopentamide
  2. Atropine
  3. Pyridostigmine
  4. Glycopyrrolate
  5. Oxybutynin
  6. Propantheline
A
  1. Pyridostigmine is an indirect-acting parasympathomimetic (reversible)
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10
Q

Which indirect-acting parasympathomimetic (reversible) is used to test for myasthenia gravis, to differentiate myasthenic crisis from cholinergic crisis, and for the reversal of nondepolarizing NMBs?

  1. Neostigmine (Prostigmin)
  2. Pyridostigmine (Mestinon)
  3. Edrophonium (Tensilon, Enlon)
A
  1. Edrophonium (Tensilon, Enlon) “Tensilon Test”
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11
Q

This indirect-acting parasympathomimetic (reversible) has gastrointestinal effects in 10-30 minutes and lasts for 4 hours.

  1. Neostigmine (Prostigmin)
  2. Pyridostigmine (Mestinon)
  3. Edrophonium (Tensilon, Enlon)
A
  1. Neostigmine (Prostigmin)
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12
Q

Which of the following is not an effect of Atropine?

  1. Slows gut
  2. Increased urination
  3. Bronchodilation
  4. Blurred vision (cycloplegia)
  5. Tachycardia
  6. Mydriasis (dilates pupil)
  7. Reduces salivation
  8. Dries secretions
  9. Difficulty with urination
A
  1. Increased urination

(Have to be careful of cycloplegia in horses! They will freak the fuck out!)

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13
Q

This indirect-acting parasympathomimetic (reversible) is available only as an injection (10 mg/mL solution).

  1. Neostigmine (Prostigmin)
  2. Pyridostigmine (Mestinon)
  3. Edrophonium (Tensilon, Enlon)
A
  1. Edrophonium (Tensilon, Enlon)
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14
Q

Which of the following is not an indirect-acting parasympathomimetics (irreversible anticholinesterase)?

  1. Echothiophate (opthalmic)
  2. Edrophonium
  3. Organophosphate insecticides (toxicity)
A
  1. Edrophonium is an indirect-acting parasympathomimetic REVERSIBLE anticholinesterase
14
Q

All of the following are nicotinic effects of organophosphate toxicity, except:

  1. CNS effects
  2. Bronchospasm
  3. Muscle tremors
  4. Muscle weakness
  5. Muscle paralysis
  6. Tachycardia
  7. Mydriasis
A
  1. Bronchospasm is a muscarinic effect

(Tachycardia and mydriasis due to stimulation of sympathetic ganglia and release of [nor]epinephrine)

  • *Nicotinic/ionotropic receptors affect the neuromuscular junction, autonomic ganglia, CNS, and the adrenal medulla*
  • *Muscarinic/metabotropic receptors affect smooth muscles, glands, the heart, and CNS*
16
Q

All of the following are muscarinic effects of organophosphate toxicity, except:

  1. Bronchospasm
  2. Bradycardia
  3. Emesis
  4. Muscle paralysis
  5. Lacrimation
  6. Diarrhea
  7. Urination
  8. Miosis
  9. Salivation
A
  1. Muscle paralysis is a nicotinic effect

Don’t forget DUMBBELS!

  • Diarrhea
  • Urination
  • Miosis
  • Bronchospasm
  • Bradycardia
  • Emesis
  • Lacrimation
  • Salivation
  • *Nicotinic/ionotropic receptors affect the neuromuscular junction, autonomic ganglia, CNS, and the adrenal medulla*
  • *Muscarinic/metabotropic receptors affect smooth muscles, glands, the heart, and CNS*
17
Q

Which direct-acting parasympatholytic is available as an injectable solution and oral tablets?

  1. Aminopentamide
  2. Atropine
  3. Pyridostigmine
  4. Glycopyrrolate
  5. Oxybutynin
  6. Propantheline
A

2. Atropine sulfate (Atroject), systemic

(usually used as an injection)

18
Q

Which direct-acting parasympatholytics treat incontinence due to detrusor muscle instability (hyperactive bladder)?

  1. Aminopentamide
  2. Atropine
  3. Pyridostigmine
  4. Glycopyrrolate
  5. Oxybutynin
  6. Propantheline
A

5. Oxybutynin (Ditropan)

6. Propantheline (Pro-banthine)

These are urinary and gastrointestinal antispasmodic agents that allows the bladder to fill (relaxes the detrusor muscle)

(does the opposite of what Bethanochol does)

20
Q

This indirect-acting parasympathomimetic (reversible) is available as oral tablets, ER tablets, oral syrup, and injectable.

  1. Neostigmine (Prostigmin)
  2. Pyridostigmine (Mestinon)
  3. Edrophonium (Tensilon, Enlon)
A
  1. Pyridostigmine (Mestinon)
21
Q

This indirect-acting parasympathomimetic (reversible) has an onset of 1 hour after oral dosing and lasts longer than Neostigmine.

  1. Pyridostigmine (Mestinon)
  2. Edrophonium (Tensilon, Enlon)
A
  1. Pyridostigmine (Mestinon)

(because it lasts longer, it can be given 2-3 times a day; good for patients taking the drug home)

22
Q

Which indirect-acting parasympathomimetic (reversible) is used to treat myasthenia gravis in dogs?

  1. Neostigmine (Prostigmin)
  2. Pyridostigmine (Mestinon)
  3. Edrophonium (Tensilon, Enlon)
A
  1. Pyridostigmine (Mestinon)
24
Q

T or F. Direct-acting parasympatholytics are muscarinic antagonists.

A

True

25
Q

Which direct-acting parasympatholytic is an antispasmodic for colic in horses?

  1. Aminopentamide
  2. Atropine
  3. Pyridostigmine
  4. Glycopyrrolate
  5. N-Butylscopolammonium Bromide
  6. Propantheline
A

5. N-Butylscopolammonium Bromide (Buscopan); it is also used to treat bradycardia

(not used much anymore)

26
Q

Which two direct-acting parasympatholytics are not available as an injectable?

  1. Aminopentamide
  2. Atropine
  3. Pyridostigmine
  4. Glycopyrrolate
  5. Oxybutynin
  6. Propantheline
A

5. Oxybutynin (Ditropan)

6. Propantheline (Pro-banthine)

These are available as oral tablets, ER tablets, syrup, and topicals for human use; Oxybutynin is widely distributed but Propantheline does not readily cross the BBB

27
Q

Which direct-acting parasympatholytic treats just like Atropine (bradyarrhythmias), but has slower kinetics?

  1. Aminopentamide
  2. Atropine
  3. Pyridostigmine
  4. Glycopyrrolate
  5. Oxybutynin
  6. Propantheline
A

4. Glycopyrrolate (Robinul), onset 30-45 minutes and can last hours (remember this is a quaternary ammonium compound)

(has also been used as a pre-med in anasthesia and to reduce hypersialism [drooling])

28
Q

CAUTION! Match the drug to its caution:

A. Neostigmine (Prostigmin)

B. Pyridostigmine (Mestinon)

C. Edrophonium (Tensilon, Enlon)

  1. Cholinergic signs (mild urination, defecation, lacrimation) or more severe cholinergic crisis (bronchoconstriction/secretions, bradycardia or tachycardia, hypotension, cardiac arrest)
  2. Anything contraindicating use of cholinergic agents
  3. Contraindicated in peritonitis, GI obstruction, late pregnancy, presence of other cholinesterase inhibitors
A

A. Neostigmine (Prostigmin) - 3. Contraindicated in peritonitis, GI obstruction, late pregnancy, presence of other cholinesterase inhibitors

B. Pyridostigmine (Mestinon) - 2. Anything contraindicating use of cholinergic agents

C. Edrophonium (Tensilon, Enlon) - 1. Cholinergic signs (mild urination, defecation, lacrimation) or more severe cholinergic crisis (bronchoconstriction/secretions, bradycardia or tachycardia, hypotension, cardiac arrest)

29
Q

All of the following describe Neostigmine (Prostigmin), except:

  1. Indirect acting parasympathomimetic (reversible)
  2. Anticholinesterase
  3. Cholinergic
  4. Cholinesterase
  5. Cholinesterase inhibitor
A
  1. Cholinesterase
30
Q

Which of the following is not a direct-acting parasympathomimetic drug?

  1. Carbachol
  2. Muscarine (poisoning)
  3. Pilocarpine (opthalmic)
  4. Bethanechol (PO)
  5. Endogenous acetylcholine
  6. Pyridostigmine
A
  1. Pyridostigmine (this is an indirect-acting parasympathomimetic drug); the rest are all muscarinic agonists
31
Q

T or F. Bethanechol (Urecholine) is a direct acting parasympathomimetic drug given orally to increase bladder contractility (treats detrusor m. atony).

A

True.

  • It is a muscarinic agonist that has some selectivity for M3 receptors; it usually has minimal nicotinic activity
  • Drug approved for humans that come in 5, 10, 25, 50 mg tabs (off-label use)
  • Other functions are to increase GI motility [treat ileus], treat dysautonomia [uncommon], and for reproductive cases [stimulate uterine contraction]
32
Q

What are some cautions for taking Bethanechol (Urecholine)?

A
  • Must have patent urethra (make sure urethra is open, or else bladder will hyperdistend) and intact bladder wall
  • Do not use if GI obstruction present or if increased GI motility contraindicated
34
Q

CAUTION! Match the drug to its caution:

A. Atropine sulfate (Atroject), systemic

B. Glycopyrrolate

C. Oxybutynin

D Propantheline

  1. Potential to cause other parasympatholytic signs as for Atropine (so must avoid if glaucoma, tachycardia, ileus), however at normal doses bladder and GI tract appear to be most affected
  2. Contraindicated in glaucoma, tachycardia; certain GI diseases (e.g. paralytic ileus), obstructive uropathy, myathenia gravis; rabbits have endogenous atropinases (breaks the drug down very rapidly)
  3. Same as for Atropine, but less likely to cause CNS effects; generally less arrythmogenic than Atropine
A

A. Atropine sulfate (Atroject), systemic - 2. Contraindicated in glaucoma, tachycardia; certain GI diseases (e.g. paralytic ileus), obstructive uropathy, myathenia gravis; rabbits have endogenous atropinases (breaks the drug down very rapidly)

B. Glycopyrrolate - 3. Same as for Atropine, but less likely to cause CNS effects; generally less arrythmogenic than Atropine

C. Oxybutynin and D. Propantheline - 1. Potential to cause other parasympatholytic signs as for Atropine (so must avoid if glaucoma, tachycardia, ileus), however at normal doses bladder and GI tract appear to be most affected

35
Q

Do you know your cholinergic receptors?

Nicotinic/ionotropic receptors affect:

Muscarinic/metabotropic receptors affect:

A

Nicotinic/ionotropic receptors affect the neuromuscular junction, autonomic ganglia, CNS, and the adrenal medulla

Muscarinic/metabotropic receptors affect smooth muscles, glands, the heart, and CNS

36
Q

Which direct-acting parasympatholytic is an antispasmodic for the gastrointestinal tract of dogs and cats?

  1. Aminopentamide
  2. Atropine
  3. Pyridostigmine
  4. Glycopyrrolate
  5. Oxybutynin
  6. Propantheline
A

1. Aminopentamide (Centrine)

(not used much anymore)

37
Q

What will you see in a case of Bethanechol (Urecholine) overdose?

A

Salivation, urination, defecation (excessive muscarinic effects);

in very high doses, more life-threatening cholinergic signs can be seen (bradycardia, bronchospasm, etc.)

38
Q

Which direct-acting parasympatholytic treats bradyarrhythmia/bradycardia, toxicity of ogranophosphates and carbamates, and also treats cholinergic crisis/anticholinesterase overdose (‘safety net’ for edrophonium response test)?

  1. Aminopentamide
  2. Atropine
  3. Pyridostigmine
  4. Glycopyrrolate
  5. Oxybutynin
  6. Propantheline
A

2. Atropine sulfate (Atroject), systemic

39
Q

What do the PSNS postganglionic axons release and what type of receptors do they act on?

  1. ACh, muscarinic
  2. ACh, nicotinic
  3. NE, adrenergic
  4. NE, muscarinic
A
  1. ACh, muscarinic
40
Q

T or F. An indirect-acting parasympathomimetic inhibits acetylcholinesterase to decrease the concentration of ACh.

A

False, an indirect-acting parasympathomimetic doesn’t work on a receptor, but works on acetylcholinesterase (inhibits it) to INCREASE the concentration of ACh.

41
Q

Which of the following are not acetylcholine effects from drugs affecting the PSNS?

  1. Bradycardia
  2. Decrease blood pressure
  3. Increase GI motility and secretion
  4. Smooth muscle contraction in bladder, uterus, bronchioles, and iris
  5. Increased secretions
  6. Convulsions (if it gets to the CNS)
  7. Stimulation of autonomic ganglia and adrenal medulla
  8. Skeletal muscle relaxation
A
  1. Skeletal muscle relaxation; it should be skeletal muscle CONTRACTION
  • Bradycardia (negative chronotropy)
  • Decrease blood pressure (negative inotropy + vasodilation)
  • Increase GI motility and secretion
  • Smooth muscle contraction in bladder (micturition), uterus, bronchioles (bronchoconstriction), and iris (miosis)
  • Increased secretions (salivary, lacrimal, bronchial)
  • Convulsions (if it gets to the CNS)
  • Stimulation of autonomic ganglia and adrenal medulla (sympathetic effects from A2 receptor)
  • Skeletal muscle contraction

Pharmacology 1 choefsho (13 decks)

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