Cholinergic Pharmacology Flashcards
MoA of Direct acting cholinergic agonist (DACA)
Act directly on ACh receptos
Adverse effects of DACA
Muscarinic Toxicity:
1) increased salivation and sweating
2) Blurred vision
3) Decreased HR and Bp
4) shortness of breath
5) Urinary frequency
6) CNS stimulation
Nicotinic Toxicity:
1) CNS stimulation
2) Fasciculation- parylsis
3) Very addictive
what are the categories of DACA? give drug examples
Muscarinic
1) Pilocarpin (Glaucoma)
2) Bethanechol (Atonic bladder conditions)
Nicotinic
1) Nicotin
2) Varenciline (reduce nicotine craving)
Both
1) Acetylcholine
2) Carbachol
Category of Benthanechol
DACA - Choline ester
Indication of Benthanechol
-Atonic bladder conditions
- Postoperative/Postpartum urine retention
MoA of Benthanechol
Activate bladder SM
PK/PD Benthanechol
–> Resistant to AChE.
–> No nicotinic activity.
–> Used for urinary retention.
Category of Pilocarpin
DACA- Alkaloids
Indication Pilocarpin
Glaucoma/ Eye surgery
MoA of Pilocarpine
Decrease Intraocular pressure (IOP)
PK/PD of Pilocarpine
1) Contracts ciliary muscle of eye (open-angle glaucoma)
2) Pupillary sphincter (closed-angle
glaucoma)
3) Resistant to AChE.
4) Can cross blood-brain barrier
(BBB).
5) It is a potent stimulator of sweat,
tears, and saliva, open/closed angle glaucoma, xerostomia
(Sjögren syndrome).
Category of Varenicline
Nictotic Agonist
MoA of Varenicline
inhibit nicotinic receptors
Indication of Varenciline
used to reduce nicotinic cravinings
MoA of IAAC (Indirect Acting Anti-Cholinesterases)
Accumulation of Ach at the synaptic cleft —–> by inhibiting AchE
What are the 2 types of IAAC?
1) Reversible —> short-acting (min-hr)
end in -ium or igmine
2) Irreversible –> long acting (days-weeks)
e.g. insect /pesticides (Orangophosphates), chemical weapons
The effect of IAAC depend on?
1) Drug dose
2) Structure (tertiary or quaternary)
3) duration of action (Reversible/irreversible)
Indications of IAAC
Antidote to:
1)Anti-cholenergics
2) Tricyclic anti-depressants
3) Narcotics
List a few IAAC drugs
1) Physostigmine (glaucoma)
2) Neostigmine (Myasthenia gravis, urinary retention etc)
3) Donepezil (Mild/moderate Dementia & AD)
4) Edrophonium ( increase tone and parestalisis in GI)
Adverse effects of IAAC
DUMBBELSS
1) Diarrhea
2) Urination
3) Miosis (pupil constiction)
4) Bradychardia
5) Bronchoconstriction
6) Excitation (of Skeletal Muscles and CNS)
7) Lacrimation
8) Salivation
9) Sweating
MoA of Physostigmine
Antidote for anticholenergic toxicity
Indication of Physostigmine
Glaucoma eye surgery –> decreaes intracoular pressure
PK/PD of Physostigmine
Tertriay amine–> corsses the BBB –> enters the CNS
Indication of Neostigmine
1) Myasthenia Gravis
2) Urinary retention
3) Postoperative/ neurogenic ileus
4) Reversal NM blockade
MoA of Neostigmine
increase tone –> Atonic bladder condition
Indication of Edrophonium
1) To increase tone & peristalisis in GI disorders
2) Cholenergic crisis:
-salivation
-lacrimation
-urination
-defecation
MoA of Edrophonium
Increases ACh
PK/PD of Edrophonium
Used to diagnose Myasthenia gravis –> replaced by an anti-AChRAB test
Indication of Donepezil
Mild/Moderate Dementia and AD
MoA of Donepezil
to increase cognetion
PK/PD of Donepezil
- increases ACh
- Lipid soluble (CNS entery)
- 1st line for Alzehimer’s Disease
