Cholinergic Drugs Flashcards

1
Q

Cholinergic drugs

AKA cholinergic agonists or Parasympathmimetics

A
  • Stimulate the parasympathetic

- Mimic effects of the PSNS neurotransmitter acetylcholine (ACh)

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2
Q

What are the two difference types of cholinergic receptors?

A

Nicotinic and Muscarinic

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3
Q

Cholinergic Drug MOA

A
  • mimic effect of acetylcholine
  • Direct-acting cholinergic agonists
  • Indirect-acting cholinergic agonists
    • cholinesterase inhibitors
    • inhibit the enzyme acetylcholinesterase, which breaks down ACh
    • Results in more ACh available at the receptors
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4
Q

Reversible category

Indirect acting

A

-bind to cholinesterase for a short period of time

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5
Q

Irreversible

Indirect acting

A
  • bind to cholinesterase for a long period of time
  • Bind to cholinesterase and form a permanent covalent bond
  • The body must make new cholinesterase to break these bonds
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6
Q

MOA and Drug Effect

Cholinergic Drugs

A
  • after binding, permeability of the cell changes allowing flow of calcium and sodium into the cells
  • results in depolarization of cell membrane and stimulation of the effector organ
  • The PNS in the “rest and digest” system
  • Stimulate intestine and bladder
  • stimulate pupils-miosis
  • increased salivation and sweating
  • cardiovascular effects
  • Respiratory effects
  • SLUD
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7
Q

At recommended doses what does cholinergic primarily affect?

A

muscarininc

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8
Q

At high doses what does cholinergic stimulate

A

nicotinic

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9
Q

Direct-acting drugs

cholinergic

A
  • reduce intraocular pressure
  • useful for glaucoma and intraocular surgery
  • Topical application because of poor oral absorption
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10
Q

Bethanechol

A
  • increases tone and motility of bladder/GI tract
  • relaxes sphincters in bladder/GI tract
  • Helpful for postsurgical atony of the bladder/GI tract
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11
Q

Indirect- acting drugs

cholinergic

A
  • increased ACh concentrations at the receptor sites, which leads to stimulation of the effector cells
  • cause skeletal muscle contractions
  • used for diagnosis and treatment of myashtenia gravis
  • used to reverse neuromuscular blocking drugs
  • used to reverse anticholinergic poisoning (antidote)
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12
Q

Indirect-acting anticholinesterase drugs

A

used for treatment of mild to moderate Alzheimers disease

-Donepezil, Galantamine, Rivastigmine, Memantine

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13
Q

Adverse Effects: cholinergic drugs

A

-Adverse effects are a result of overstimulation of PSNS
-Cardiovascular: brady, hypo, syncope, conduction abnormals
CNS: HA, dizzy, convulsions, ataxia
GI: abdomen cramps, secretions, N/V
Respiratory: bronchial secretions and spasms
Other: lacrimation, sweating, salivation, miosis

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14
Q

Toxicity for cholinergic

A

-circulatory collapse, hypotension, bloody diarrhea, shock, cardiac arrest

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15
Q

Early signs of toxicity

A

abdominal cramps, salivation, flushing of skin, N/V, transient syncope, transient complete heart block, dyspnea, Ortho hypotension

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16
Q

Treatment in early phase of Toxicity

A

atropine

17
Q

Treatment of severe cardiovascular reactions or bronchoconstriction

A

epinephrine

18
Q

Muscarinic Poisoning

A
  • caused by certain mushrooms
  • Overdose of direct-acting muscarinic agonists and indirect-acting cholinomimetics
  • Symptoms-result from excessive activation of muscarinic receptors
  • Treatment-Atropine
19
Q

Bethanechol (Urecholine)

A
  • Direct-acting cholinergic agonist
  • Uses: acute postop and postpartum nonobstructive urinary retention and management of urinary retention associated with neurogenic atony of the bladder
  • Contraindications: known drug allergy, hyperthyroidism, peptic ulcer, active bronchial asthma, cardiac disease or coronary artery disease, epilepsy, and parkinsonism
20
Q

Donepezil (Aricept)

A
  • cholinesterase inhibitor that works centrally in the brain to increase levels of ACh by inhibiting acetylcholinesterase
  • used in the treatment of mild to moderate Alzheimers disease
  • similar cholinesterase inhibitor include galantamine and rivastigmine
  • Adverse effects: GI upset, drowsiness, dizziness, insomnia, muscle cramps. Cardiovascular effects may include brady, syncope, hypotension with refelx tachycardia, or HTN
  • interacting drugs: anticholinergics and NSAIDS
21
Q

Memantine (Namenda)

A
  • not a cholinergic drug
  • NMDA receptor antagonist
  • used for treatment of Alzheimers disease
  • improves cognitive function and quality of life
22
Q

Neostigmine, Pyridostigmine, and Physostigmine

A

-used: reversing the effects of nondepolarizing neuromuscular blocking drugs; treating severe overdoses of tricyclic anttidepressants; and antidote after toxic exposure to nondrug anticholinergic agents, including those used in chemical warfare

23
Q

Pyridostigmine (Mestinon)

A
  • Indirect-acting cholinergic drugs that work to increase ACh by inhibiting acetylcholinesterase
  • use: myasthenia gravis
24
Q

Edrophonium (Tensilon)

A

indirect-acting cholinergic drug that is used to diagnose myasthenia gravis. It can also be used to differentiate between myasthenia gravis and cholinergic crisis

25
Q

Herbal Products: Gingko

A

Common uses: prevent memory loss, vertigo, tinnitus

  • may cause GI upset, HA, bleeding
  • potential interactions: aspirin, NSAIDs, anticoagulants, anticonvulsants
26
Q

What is the antidote for cholinergic drugs?

A

Atropine