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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
which muscarinic receptor agonist has the most bladder effect
Bethanechol
26
muscarinic receptor agonist effect on urinary bladder
* tone and peristalsis increase * void pressure increases * bladder capacity decreases * detrusor contracts * tirgone and sphincter relax
27
muscarinic receptor agonist effect on glands
* increased secretion * sweat * lacrimal * nasopharyngeal * tracheobronchial
28
which muscarinic receptor agonist has the most effect on sweat glands
pilocarpine
29
effect of muscarinic receptor agonist on brain activity
* improvement of memory * alertness and arousal * used for treatment of alzheimer's disease
30
which muscarinic receptor agonist is used to increase GI motility
* Bethanechol (urecholine) * treats postoperative abdominal distension * treats gastric atony
31
which muscarinic receptor agonist is used to treat urinary retention and inadequate emptying
Bethanechol (Urecholine)
32
which muscarinic receptor agonist is used to treat Xerostomia: dry mouth due to Sjogren's syndrome or head and neck radiation
* pilocarpine * sweating will be common side effect * Cevimeline (Evoxac): selective M3 agonist * long lasting action and fewer side effects
33
Side Effects of Muscarinic Agonists
* Nausea, vomiting, **diarrhea** * **Abdominal cramps**, belching * **Salivation and sweating** * Cutaneous vasodilation * Bronchoconstriction * Bladder tightness * Blurred vision
34
contraindications of muscarininc receptor agonists
* peptic ulcer * increases GI acid production * Asthma/COPD * bowel obstruction * increases peristalsis
35
mushrooms contain muscarine thus a person can get muscarine toxicity. What is the treatment for this patient
* treat with atropine (antagonist) * albuterol (to reverse bronchoconstriction)
36
Nicotinic receptors are located where?
* the autonomic ganglia (NN) * the brain (NM) * skeletal muscle (NM)
37
what type of receptors are nicotinic receptors
ligand-gated ion channels * Nicotinic agonists cause an immediate activation, followed by a rapid desensitization if the receptors continue to be stimulated
38
effects of nicotinic stimulation on the brain
* Low doses of nicotine: increase alertness and attention * Higher doses: tremor, vomiting and increased respiration. * toxic doses: convulsions
39
peripheral effects of nicotinic stimulation are similar to which autonomic pathway
Effects of nicotine may be similar to discharge of both parasympathetic and sympathetic neurons, due to stimulation of autonomic ganglia.
40
nicotinic effects on CV and GU function
* **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
Nicotinic agonists effects on neuromuscular junction
* 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
Nicotine toxicity
* vomiting * CNS stimulation * convulsions, coma, respiratory arrest * skeletal muscle depolarization * NMJ block and paralysis * CV * HTN, cardiac arrhythmia
43
treatment of nicotine toxicity
* with atropine to block muscarinic receptors * with anticonvulsants to decrease seizures * with mechanical respiration
44
what is Varenicline (Chantix)
* partial agonist on nicotinic receptor subtype in brain * prevents craving from nicotine withdrawal but also blocks effect of nicotine if smoke cigarettes
45
Varenicline (Chantix) side effects
* nausea, vomiting * constipation, flatulence * sleep, psychiatric disturbance
46
MOA of Cholinesterase Inhibitors
* increase duration of time that ACh is available to activate receptors in the synaptic cleft
47
Name the Cholinesterase Inhibitors
* Neostigmine * Physostigmine * Edrophonium * Organophosphates

Pharmacology II (9 decks)

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