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Pharmacology II > cholinergic agonists and antagonists > Flashcards

cholinergic agonists and antagonists Flashcards

1
Q

sympathetic postganglionic neurons act on what type of receptors

A

adrenergic receptors

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2
Q

in cholinergic transmission, Ach can stimulate what two types of receptors

A
  • muscarinic
  • nicotinic
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3
Q

hemicholinium has what effect on cholinergic transmission

A

inhibits transporter that would take up choline into nerve terminal

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4
Q

botulinum toxin has what effect on cholinergic transmission

A

inhibits the release of ACh

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5
Q

List the Direct-Acting Cholinergic Agonists

A
  • acetylcholine
  • methacholine
  • carbachol
  • bethanechol
  • pilocarpine, Cevimeline
  • nicotine
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6
Q

define direct acting drugs

A

Drugs that bind to and activate the receptor are direct-acting, and most will discriminate between muscarinic and nicotinic receptors

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7
Q

define indirect acting drugs

A

Cholinesterase inhibitors are considered “indirect-acting”; they amplify the effects of ACh, and increase its effectiveness at both nicotinic and muscarinic receptors.

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8
Q
  • what cholinergic agonist
    • will act at both muscarinic and nicotinic receptors
    • is rapidly hydrolyzed by AChE
A

acetylcholine

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9
Q

which cholinergic agonist is

  • resistant to AChE
  • selective for muscarinic receptors
  • does not enter brain
A

Bethanechol

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10
Q

which cholinergic agonist/muscarinic agonist is

  • an alkaloid
  • selective for muscarinic receptors
  • easily absorbed orally
A

Pilocarpine

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11
Q

sweat and salivary glands are very sensitive to what cholinergic agonist

A

pilocarpine

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12
Q

which muscarinic agonist is selective for M3 receptors

A

Cevimeline

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13
Q

define muscarinic receptor agonist

A

is an agent that activates the activity of the muscarinicacetylcholine receptor.

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14
Q

MOA of muscarinic receptor agonists

A

Muscarinic agonists interact with specific G-proteins to increase DAG and IP3 vua Gq/11, M1 and M3 receptors), or inhibit adenylate cyclase and open K+ channels (Gi, M2 receptors)

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15
Q

Effects of Muscarinic Agonists in the Eye

A
  • constrict pupil
  • facilitate accomodation for near vision
  • decrease intraocular pressure
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16
Q

what class of drugs are used to treat glaucoma

A

Muscarinic Agonists

  • pilocarpine : decrease intraocular pressure
  • use for reversal of narrow-angle glaucoma attack
  • will cause blurred vision so drug of last choice
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17
Q

side effects of using Muscarinic Agonists like Pilocarpine in the eye

A

blurred vision

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18
Q

effects of muscarinic agonists on cardiovascular function

A

muscarinic agonists used clinically have very few cardiovascular effects: HOWEVER, vagal stimulation can have profound effects on the heart, so injecting acetylcholine can have effects on CV function

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19
Q

Muscarinic receptors are located on smooth muscle, and the effect of stimulation of muscarinic receptors resembles that of ?

A

parasympathetic activation

20
Q

Vagal inputs releasing acetylcholine (cholinergic agonist) has what effects on cardiovascular system

A
  • bradycardia
    • The effect of cholinergic stimulation in the heart is primarily on the atrium
    • slows conduction through AV node
  • vasodilation
    • stimulation of cholinergic receptors on endothelial cells releases nitric oxide
21
Q

Effects of Muscarinic Agonists on respiratory function

A

Bronchoconstriction can be quite striking in asthmatics exposed to cholinergic agonists.

22
Q

which muscarinic receptor agonist is used to diagnose asthma

A

Methacholine

23
Q

muscarinic receptor agonist effect on GI tract

A
  • motility and peristalsis is increased in the GI tract
  • sphincters are relaxed
  • salivary and gastric secretions increase
24
Q

which muscarinic receptor agonist has the most GI effect

A

Bethanechol

25
Q

which muscarinic receptor agonist has the most bladder effect

A

Bethanechol

26
Q

muscarinic receptor agonist effect on urinary bladder

A
  • tone and peristalsis increase
  • void pressure increases
  • bladder capacity decreases
  • detrusor contracts
  • tirgone and sphincter relax
27
Q

muscarinic receptor agonist effect on glands

A
  • increased secretion
    • sweat
    • lacrimal
    • nasopharyngeal
    • tracheobronchial
28
Q

which muscarinic receptor agonist has the most effect on sweat glands

A

pilocarpine

29
Q

effect of muscarinic receptor agonist on brain activity

A
  • improvement of memory
  • alertness and arousal
    • used for treatment of alzheimer’s disease
30
Q

which muscarinic receptor agonist is used to increase GI motility

A
  • Bethanechol (urecholine)
    • treats postoperative abdominal distension
    • treats gastric atony
31
Q

which muscarinic receptor agonist is used to treat urinary retention and inadequate emptying

A

Bethanechol (Urecholine)

32
Q

which muscarinic receptor agonist is used to treat Xerostomia: dry mouth due to Sjogren’s syndrome or head and neck radiation

A
  • pilocarpine
    • sweating will be common side effect
  • Cevimeline (Evoxac): selective M3 agonist
    • long lasting action and fewer side effects
33
Q

Side Effects of Muscarinic Agonists

A
  • Nausea, vomiting, diarrhea
  • Abdominal cramps, belching
  • Salivation and sweating
  • Cutaneous vasodilation
  • Bronchoconstriction
  • Bladder tightness
  • Blurred vision
34
Q

contraindications of muscarininc receptor agonists

A
  • peptic ulcer
    • increases GI acid production
  • Asthma/COPD
  • bowel obstruction
    • increases peristalsis
35
Q

mushrooms contain muscarine thus a person can get muscarine toxicity. What is the treatment for this patient

A
  • treat with atropine (antagonist)
  • albuterol (to reverse bronchoconstriction)
36
Q

Nicotinic receptors are located where?

A
  • the autonomic ganglia (NN)
  • the brain (NM)
  • skeletal muscle (NM)
37
Q

what type of receptors are nicotinic receptors

A

ligand-gated ion channels

  • Nicotinic agonists cause an immediate activation, followed by a rapid desensitization if the receptors continue to be stimulated
38
Q

effects of nicotinic stimulation on the brain

A
  • Low doses of nicotine: increase alertness and attention
  • Higher doses: tremor, vomiting and increased respiration.
  • toxic doses: convulsions
39
Q

peripheral effects of nicotinic stimulation are similar to which autonomic pathway

A

Effects of nicotine may be similar to discharge of both parasympathetic and sympathetic neurons, due to stimulation of autonomic ganglia.

40
Q

nicotinic effects on CV and GU function

A
  • Cardiac effects are mostly sympathetic
    • hypertension and increased heart rate, which may alternate with vagal bradycardia
  • Gastrointestinal and urinary effects are parasympathetic
    • ​vomiting, diarrhea and urination.
41
Q

Nicotinic agonists effects on neuromuscular junction

A
  • initially cause stimulation of the muscle depending on the size of the stimulus, which may range from twitches to a strong contraction
  • Long-lasting stimulation which is not rapidly hydrolyzed, will then desensitize the NMJ
    • resulting in loss of strength and flaccid paralysis.
42
Q

Nicotine toxicity

A
  • vomiting
  • CNS stimulation
    • convulsions, coma, respiratory arrest
  • skeletal muscle depolarization
    • NMJ block and paralysis
  • CV
    • HTN, cardiac arrhythmia
43
Q

treatment of nicotine toxicity

A
  • with atropine to block muscarinic receptors
  • with anticonvulsants to decrease seizures
  • with mechanical respiration
44
Q

what is Varenicline (Chantix)

A
  • partial agonist on nicotinic receptor subtype in brain
  • prevents craving from nicotine withdrawal but also blocks effect of nicotine if smoke cigarettes
45
Q

Varenicline (Chantix) side effects

A
  • nausea, vomiting
  • constipation, flatulence
  • sleep, psychiatric disturbance
46
Q

MOA of Cholinesterase Inhibitors

A
  • increase duration of time that ACh is available to activate receptors in the synaptic cleft
47
Q

Name the Cholinesterase Inhibitors

A
  • Neostigmine
  • Physostigmine
  • Edrophonium
  • Organophosphates

Pharmacology II (9 decks)

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