indirect cholinomimetics

Question 1

indirect cholinomimetics do so by …

Answer 1

reversible/irreversible inhibition of Acetylcholine- Esterase therefore increasing Ach at the synapse

(dumpster spilling cola bottles with “Anti-Establishment” /”STIGMA” - suffix for these drugs )

Question 2

what is the use of indirect cholinomimetics ?

Answer 2

• to treat myasthenia gravis which is an autoimmune diseasei in which anti-n-ACHR antibodies are generated (“gravis graffiti” on electric outlet)
• symptoms (“Gravis Graffiti” covers electric outlet)
• muscle weakness
• diplopia
• ​ptosis

Question 3

how can we classify indirect cholinomimetics ?

Answer 3

Tertiary or Quaternary

(“Quarters only in phone booth”)

Question 4

mention all the Quaternary indirect cholinomimetics

Answer 4

Edrophonium
(“phone booth”)

Pyridostigmine
(“community pride t-shirt on blacky”)

Neostigmine
(“neon sign stigma”)

Question 5

Edrophonium

(“phone booth”)

Answer 5

Reverses muscle weakness in MG but not used for therapy only for diagnosis due to short half life used in Tensilon test (“phone wire tension”)

• Symptoms relieved (+ tensilon) → undertreated MG
• Symptoms not relieved,or even worsen ( - tensilon )→ cholinergic crisis

Question 6

Pyridostigmine

(“community PRIDE shirt on blacky “)

Answer 6

used for long term treatment of Myasthenia Gravis by outcompeting with MG antibodies

(“community PRIDE blacky removing GRAVIS graffiti from electric outlet “)

Question 7

Neostigmine

(“neon sign STIGMA”)

Answer 7

-can reverse non-depolarizing neuromuscular agents that are called CURARE-like
(tubocurarine ,pancuronium,cisatracurium)

(“Crayons stuck in electric outlet put by the asshole kid and neon sign store owner tells him to fuck off”)

-also used for treatment of Urinary retention
(“neon sign store owner holding bladder hose”)

-can reverse depolarizing neuromuscular agents such as Succinylcholine (“SUCKS graffiti”) but not during phase 1 which is irreversible
( “phase-1 cleanup guy get shocked”)

Question 8

Physostigmine

(“PHYS ED center”)

Answer 8

-a tertiary indirect cholinomimetic that can cross BBB and has CNS effects
(“PHYS ED CENTER” / “YOUR BRAIN ON DRUGS SIGN IN PHYS ED GYM”)

-Physostigmine (AchEst inhibitors toxicity) causes the DUMBBLESS symptoms as well as flaccid paralysis due to nicotinic overstimulation.

(“weak kid smoking cigarette trying to lift dumbells” )

• Diarrhea
• ​Urination
• ​Miosis
• ​Bronchospasm
• ​Bradycardia
• ​Lacrimation
• ​Salivation
• ​Sweating

-Can reverse Atropine overdose both peripherally and centrally

(“PHYS gym instructor dragging the asshole atropine in wonderland graffiti kid” )

-Atropine comes from belladona flower /Jimms weed→”gardneres midriasis”
(“GYM SIGN below phys ed center”)

-

Question 9

Organophosphates

(“THIOL spray”)

Answer 9

• found in insecticides (e.g. echothiophate)
• major cause of acute cholinergic toxicity

(“green fumes from THIOL spray aiming towards weak smoking kid”)

-Pralidoxime can reverse Organophosphates overdose (“DUMBBLSS) by hydrolyzing covalent bonds and regenerate m/n-ACHRs ***Peripheral only***

(dumpster saying “ PUT A LID on TOXIC waste “ / “closing LID on TOXIC spray”)

-Atropine can cross BBB and has CNS effects therefore used as an antidote for Organophosphates overdose to treat both peripheral and CNS symptoms

(“atropine alice black graffiti on Open toxic dumpster”)

-Aging of Organophosphates creates irreversible binding complex and Pralidoxime is ineffective at that point

(“Old Pesticides control man spray and Corrodes the ACH dumpster” )

Question 10

name the acetylcholine esterase inhibitors that are used in treatment of Alzheimer’s Disease

Answer 10

Galantamine
(“Alzheimer’s GALA” on the sign)

Rivastigmine
(“Reverse the Stigma” on the sign)

Donepezil
(“old farts done with their puzzle”)

*ALL OF THESE PENETRATE THE CNS (“brain puzzle”)