Cholinergic Drugs Flashcards
Cholinergic drugs
AKA cholinergic agonists or Parasympathmimetics
- Stimulate the parasympathetic
- Mimic effects of the PSNS neurotransmitter acetylcholine (ACh)
What are the two difference types of cholinergic receptors?
Nicotinic and Muscarinic
Cholinergic Drug MOA
- 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
Reversible category
Indirect acting
-bind to cholinesterase for a short period of time
Irreversible
Indirect acting
- 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
MOA and Drug Effect
Cholinergic Drugs
- 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
At recommended doses what does cholinergic primarily affect?
muscarininc
At high doses what does cholinergic stimulate
nicotinic
Direct-acting drugs
cholinergic
- reduce intraocular pressure
- useful for glaucoma and intraocular surgery
- Topical application because of poor oral absorption
Bethanechol
- increases tone and motility of bladder/GI tract
- relaxes sphincters in bladder/GI tract
- Helpful for postsurgical atony of the bladder/GI tract
Indirect- acting drugs
cholinergic
- 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)
Indirect-acting anticholinesterase drugs
used for treatment of mild to moderate Alzheimers disease
-Donepezil, Galantamine, Rivastigmine, Memantine
Adverse Effects: cholinergic drugs
-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
Toxicity for cholinergic
-circulatory collapse, hypotension, bloody diarrhea, shock, cardiac arrest
Early signs of toxicity
abdominal cramps, salivation, flushing of skin, N/V, transient syncope, transient complete heart block, dyspnea, Ortho hypotension