Autonomous Nervous Sys. Drugs Flashcards
what are the types of cholinergic receptors?
nicotinic receptors (“smoker”)
muscarinic receptors (“motorcycle parking spots”)
where are n-ACHR found ?
-autonomic ganglia
(“ganglia like transformers”)
-skeletal muscle motor end plate
(“electric outlet near smoker”)
-adrenal glands
(“adrenal beanie on smoker”)
what type of receptor is n-ACHR ?
act as ion channels where influx of + ions occur
(“ion channel news behind smoker”)
What type of receptor is m-ACHR ? what are the subtypes ? where are they found ?
G-coupled receptors
M1 (Gq) - nerves , CNS
(“Brain helmet on 1st rider” , “3 DAGS”)
M2 (Gi) - SA node , AV node , atria
(“2nd rider shirt showing heart with jewels”)
M3 (Gq) - found on glands and smooth muscle (“glandular sponge with 3rd rider “ “3 DAGS”)
M3 stimulation effect on vessels ?
M3→ Gq→ IP3/DAG→ Ca+2 increase→ NO release → cGMP increase → VASODILATION →drop in BP
(“Dilated NO Exhaust on 3rd motorcycle”)
Name the Direct Cholinomimetics
Bethanecol (“Beth with Cola”)
Pilocarpine (“Pile of Carps”)
Carbachol (“constricted hood blocking carbon”)
Methacholine (“Marathon challenge”)
Varenicline
(“1-800 very-clean sign on pole next to smoker” )
Bethanecol (“Beth with Cola”)
-increases secretions and gastric motility
(“cement pouring out from colon”)
-to treat neurogenic ileus/bladder due to spinal cord injury / post operation/ post pregnancy
*non obstructive*
(“Beth holding Bladder hose”)
Pilocarpine
(“Pile of Carps”)
-increase Salivation -treat sjorgen
(“dripping carps mouths”)
-meiosis -activates sphincter pupilae muscle
(“constricted hood”)
- for treatment of acute angle Glaucoma
- contracts cilliary muscle (“smooth muscle crane”) causing accomodation and relaxation of zonular fibers (“fish net zonules”) as well as increasing the outflow of AQ.H
- treatment of Glaucoma
Carbachol
(“constricted hood blocking carbon fumes”)
-agonist of both muscarinic and nicotinic receptors
(“carbon fumes from smoker”)
-causes pupillary constriction
(“constricted hood”)
- to treat acute angle glaucoma
Methacholine
(“marathon challenge”)
- induce bronchoconstriction and may worsen asthma / COPD (“Wheezing Man”)
- may be used to intiate asthma for pulmonary testing
*Bronchial challenge test* Asthmatics react to lower doses .. then give Bronchodilator as a “reversibility test” to distinguish between ASTHMA/ COPD
Varenicline
(“1800-Very-clean sign on pole”)
-nicotinic **partial agonist
-**
for smoking cessation
(“smoking cessation hotline 1800-Very-clean” sign on pole)
indirect cholinomimetics do so by …
reversible/irreversible inhibition of Acetylcholine- Esterase therefore increasing Ach at the synapse
(dumpster spilling cola bottles with “Anti-Establishment” /”STIGMA” - suffix for these drugs )
what is the use of indirect cholinomimetics ?
- 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
how can we classify indirect cholinomimetics ?
Tertiary or Quaternary
(“Quarters only in phone booth”)
mention all the Quaternary indirect cholinomimetics
Edrophonium
(“phone booth”)
Pyridostigmine
(“community pride t-shirt on blacky”)
Neostigmine
(“neon sign stigma”)
Edrophonium
(“phone booth”)
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
Pyridostigmine
(“community PRIDE shirt on blacky “)
used for long term treatment of Myasthenia Gravis by outcompeting with MG antibodies
(“community PRIDE blacky removing GRAVIS graffiti from electric outlet “)
Neostigmine
(“neon sign STIGMA”)
-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”)
Physostigmine
(“PHYS ED center”)
-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
-
Organophosphates
(“THIOL spray”)
- 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” )
name the acetylcholine esterase inhibitors that are used in treatment of Alzheimer’s Disease
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”)
anti -muscarinic drugs are good for ..
blocking “DUMBBLLSS” symptoms
(“two dumb-fucks sitting on motorcycle and squeezing dumbells”)
name the anti-muscarinic drugs
Muscarinic antagonists
Atropine
(“alice in wonderland”)
Scopolamine
(“seasick seal sailor outfit holding telescope”)
M3 Antagonists
Ipratropium /Tiotropium
(“cat-ipa-tio tropillar” caterpillar sitting on mushroom”)
Oxybutynin
(“Ox butler”)
Tolterodine
(“Turtle butler”)
M1 Antagonists
Benztropine
(“BENZ Parked in M1”)
Trihexyphenidyl
(“car with 3 hexagons parked in M1”)
Atropine
(“alice in wonderland”)
from Belladona flower (“alice holding pink flower”) or Jimms weed(“Jimms weed tea bag incup next to alice”)
-antimuscarinics block M2 therefore block Parasympathetic activity on heart leading to elevated HR and AV conduction
(“crazy queen holding heart with jewel nodes “)
- increases heart rate (anti-M) and useful for bradycardia (“bunny elevates heart watch”)
- increase AV conduction (anti-M) and is useful for treatment of AV blocks
(“heart shield” resembels block “falling heart shields because of anti-M effect”)
- can cross BBB and and has CNS effects
(“CNS hat on sick sea sailor”)
Scopolamine
(“Sea Sick Seal sailor holding telescope “)
-can cross BBB (Anti-M) and has CNS effects
(“Sick Seal Sailor’s hat says CNS on it “)
- to treat motion sickness/ vestibular nausea
(“sea sick sailor”)
-administered in for of transdermal patch
(“sea sick seal sailor has eyepatch on”)
-antimuscarinics cause mydriasis and *cycloplegia
(“sea sick sailor holding telescope with dilated pupil”)
Ipratropium/Tiotropium-M3 antagonists
(“Cat-ipa-tio-tropillar” blue caterpillar smoking hookah sitting on mushroom)
- inhaled antimuscarinic bronchoDILATORS (“Caterpiller inhaling Shisha smoke”)
- useful in management of COPD since they act as bronchodilators as well as reduce secretions
(blue bloater- “blue caterpillar “ pink puffer -“pink shisha”)
-Tiotropium dissociates slower therefore is used as a long lasting bronchodilator
(“long lasting TIOoo smoke rings”)
Oxybutynin/Tolterodine-M3 antagonists
(“Ox butler / Turtle butler”)
-useful in treatment of Bladder spasms as well as Urinary incontinence
(“ox butler Turning off Bladder”)
Benztropine - M1 antagonist
(“BENZ car parked in M1)
Trihexyphenidyl-M1 antagonist
(“Car with 3 hexagons parked in M1”)
-M1 receptors are found in nerves and CNS
(M1 Parking spots below “Parking Center” sign)
-useful in treatment of tremors and rigidity seen in Parkinson’s disease
(BENZ and TRIHEX cars parked under the sign “PARKING CENTER” having “Shakey Antenas” to resemble tremors and rigidity of parkinson’s)
-antimuscarinics are useful in treatment of extrapyramidal side effects caused by antipsychotic drugs such as
- Dystonia
- Akathisia
- Parkinsonism
(falling cone next to M1 cars saying “EXTRA PARKING”)