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Block 8 Cardiology Flashcards > Cholinergic Agonists > Flashcards

Cholinergic Agonists Flashcards

1
Q

Direct Acting Cholinergic Agonists MOA

A

1) muscarinic receptor agonists
- choline esters, pilocarpine
2) nicotinic receptor agonists
- nicotine

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2
Q

Indirect Acting Cholinergic Agonists MOA

A

1) Inhibitors of cholinesterases
- carbamates, organophosphates
2) Stimulators of ACh release
- Black Widow Spider venum, metoclopramide (GI drug)

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3
Q

Choline Esters

A

“the ABCs of cholinergics”
=direct acting structural analoges of ACTH
Acetylcholine (Miochol)- miotic eye surgery
Bethanechol (Urecholine)- bladder, paralytic ileum
Carbachol (Miostat)- constant miosis, glaucoma (long acting)
Methacholine (Provocholine)- used to access bronchial hypersensitivity in asthma

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4
Q

Choline Esters MOA

A

Direct activation of cholinergic receptors.

- muscarinic activity

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5
Q

Choline Esters Effects

A

DUMBELS

diarrhea, urination, miosis, bradycardia, excitation of SKM, lacrymation, salivation/sweating

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6
Q

Natural Alkaloids

A

Muscarine and Pilocarpine

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7
Q

Muscarine Intoxication

A

wild mushrooms!
-accidental intoxication- abdominal cramping, tightness in chest, over secretion
rx for intoxication: pump stomach, atropine (muscarinic antagonist)

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8
Q

Pilocarpine Uses

A

1) xerostomia
(dry mouth- to induce salivation) and
2) glaucoma
(to induce outflow of aqueous humor, thus, reducing intraocular pressure).

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9
Q

Uses of Muscarinic Agonists

A 
eye surgery
glaucoma
nonobstructive atony of the bladder
paralytic ileus
xerostomia
diagnosis of bronchial hyper-reactivity
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10
Q

Contraindications of Muscarinic Agonists

A

peptic ulcers - (stimulate acid secretion)
bronchial asthma- (worsens constriction)
hyperthyroidism- (can cause arrhythmia)

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11
Q

Cholinesterase Inhibitors MOA

A

Inhibit AChE and pChE -> prevents the destruction of ACh

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12
Q

Carbamate esters

A

Bind to active site of AChE enzyme -> preventing binding of ACh

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13
Q

Edrophonium

A

Binds reversibly to AChE -> preventing access by ACh

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14
Q

Organophosphates

A

“IRREVERSIBLE”
= phosphorylate AChE => extremely stable and hydrolyzed at very slow rate.
Undergoes AGING- (breaking of one of the oxygen-phosphorus bonds of the inhibitor) further strengthening the phosphorylated enzyme.

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15
Q

Name Four Reversible ChE-Inhibitors

A

Physostigmine- Crossed BBB
Edrophonium- short acting
Pyridostigmine- long acting
Neostigmine

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16
Q

Uses for Reversible ChE-Inhibitors

A

Paralytic ileum/neurogenic bladder
Glaucoma
Myasthenia Gravis
Reversal of N-M blockade (used by anesthesiologists)
Anti-muscarinic Drug Intoxication Rx
Alzheimer’s Disease- Donepezil (Aricept), Rivastigmine

17
Q

Name Three Organophosphates

A

Echothiophate- eye drops
Malathion/Parathion- agricultural pesticides
Soman/Sarin- warfare

18
Q

Toxicities of ChE Inhibitors

A 
DUMB BELS 
bronchoconstriction
miosis
excessive secretions
diarrhea
urinary incontinence, 
alterations in heart rate and blood pressure
tremors, convulsions
19
Q

Antidotes to organophosphates

A

1) Atropine- blocks muscarinic effects
2) Pralidoxime- cholinesterase reactivator. Must be used before aging takes place!
3) Benzodiazepines (lorazepam)- reduce or prevent seizure activity

20
Q

Nicotine MOA

A

Binds to α - subunits of nicotinic receptors -> increase in Na+ influx.

21
Q

Nicotine Effects

A

CNS- increased focus, tremors, seizures
CVS- sympathomimetic effects
GI- increased acid secretion and motility

22
Q

Nicotine Pharmacokinetics

A

HIGHLY LIPID Soluble

Well absorbed from all routes of administration

23
Q

Nicotine: Acute intoxication

A

ie. sprayed pesticide or too many nicotine patches.

- Respiratory failure, cardiovascular collapse, nausea, vomiting, headache, dizziness, palpitations, and convulsions

24
Q

Nicotine: Chronic intoxication

A
  • Tolerance and physical dependence.

- Respiratory disease, cardiovascular disease and cancer

25
Q

Nicotine Uses

A

Smoking cessation

Nicotine gum, inhaler, nasal spray, transdermal patch

26
Q

Drugs used for smoking cessation

A
  • Nicotine replacement (patches, gum, etc)
  • Bupropion (Zyban)= antidepressant
  • Varenicline (Chantix)= direct acting nicotinic partial agonist

Block 8 Cardiology Flashcards (6 decks)

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