Parasympathetic Agents Flashcards
What Type of Nervous System is;
▪️Biosynthesis: Metyrosine
▪️Storage: Reserpine
RELEASE (Exocyte)
□ Stimulators: TEAM
□ Inhibitors: GGB
TERMINATION
□ Reuptake: RIs
□ Metabolism: MAOs, COMT Inh.
Sympathetic
What Type of Nervous System is;
▪️Biosynthesis: Hemicholium (rate-limiting step)
▪️Storage: Vesamicol
RELEASE (Exocyte)
□ Stimulators: alpha-latrotoxin
□ Inhibitors: Botolinum toxin
TERMINATION
□ Reuptake: N/A
□ Metabolism: AChaE Inh.
Parasympathetic
What type of cholinoceptors
▪️GIT
▪️Parietal cells
▪️(+) Proton Pump=HCl production
M1 (Muscarinic)
What type of cholinoceptors
▪️Heart (atria)
▪️↓ cAMP
▪️Bradycardia, Dromotropic
M2 (Muscarinic)
What type of cholinoceptors
▪️Organs & Glands
▪️Exocrine Glands: (Wetness) Salivation, Lacrimation, Sweating
▪️Smooth Muscles: Qontraction
• Eyes: Circular (pupils) & Ciliary=Contraction Miosis
• Bronchi: Bronchoconstriction
• GIT: Tae= Bowel Mvmt.
• Urinary Bladder: Ihi=Urination
M3 (Muscarinic)
What type of cholinoceptors
▪️Ganglion=Synaptic Neurotransmission
▪️Adrenal Medulla=Epi release
▪️Stimulation
Nn (neural)
What type of cholinoceptors
▪️Nueromuscular End Plates
▪️Skeletal Muscle: Contraction
Nm (muscular)
Parasympathomimetics Agonist
Drug use for Mgt. of Glaucoma (CDE)
Carbachol - (Direct Acting)
Demecarium - (Indirect Acting)
Echothiopate - (Indirect Acting)
Direct Acting Cholinergic Agonist (Parasympathomimetics)
Drug use for Mgt. of Atropine Toxicity
Neostigmine
Direct Acting Cholinergic Agonist (Parasympathomimetics)
Drug use for Mgt. of Non-Obstructive Ileus (reduced peristalsis)
Physostigmine, Pilocarpine
Direct Acting Cholinergic Agonist (Parasympathomimetics)
Drug use for Smoking Cessation
Varenicline
Nicotine
Direct Acting Cholinergic Agonist (Parasympathomimetics)
Drug use for Pulmonary Challenge Test
Methacholine (bronconstrictor)
DIRECT ACTING or INDIRECT ACTING
Agonists: Cholinomimetics
▪️bind to stimulate receptors (M,N)
▪️cholinoceptors activation (Drug)
Direct Acting
DIRECT ACTING or INDIRECT ACTING
Agonists: Cholinomimetics
▪️inhibit ACh metabolism =↑ ACh
▪️Aka: Anticholinesterases
Indirect Acting Cholinergic Agonist
What Drug are under;
Parasympathetic Direct Agonist
a. Choline Esters
• Non-Selective: M & N
Mnemonics: ABCM
Acetylcholine
Bethanechol - M Selective
Carbachol
Methacholine
Parasympathetic Direct Agonist
a. Choline Esters
▪️Mgt. of Urine Retention
Bethanechol (urecholine)
What Drug are under;
Parasympathetic Direct Agonist
a. Cholinergic Alkaloids
• Non-Selective: binds to M&N (A)
• M-Selective: (PM)
• N-Selective: (LVN)
• Non-Selective: Arecoline
• M-Selective: Pilocarpine, Muscarine
• N-Selective: Lobeline, Varenicline, Nicotine
Areca Catechu; betel nut, nga nga
Arecoline (Non-Selective)
Parasympathetic Direct Agonist
a. Cholinergic Alkaloids
▪️Mgt. of Glaucoma & GI Atony
Pilocarpine (M-Selective)
Parasympathetic Drug
Indirect Acting Cholinergic Agonist
▪︎ Classes
1. Reversible: (?)
2. Irreversible: (?)
3. CNS-acting: (?)
- Reversible: safer
- Irreversible: toxic
- CNS-acting: Anti-Alzheimer’s
What Classes belongs the ff. drugs?
[Reversible, Irrreversible, CNS-acting]
▪️Aminialcohol: Edrophonium (Tensilon)
▪️Carbamates: (-stigmine)
▪︎ Physostigmine
▪︎ Pyridostigmine
▪︎ Neostigmine
▪️Others:
▪︎ Ambenonium
▪︎ Demecarium
Reversible
What Classes belongs the ff. drugs?
[Reversible, Irrreversible, CNS-acting]
▪️Organophosphate
▪️Agricultural Poisons: Malathion, Parathion
▪️Nerve Gases: (Soman Tabun, Sarin)
▪️Echothiophate: medically useful
Irreversible (Long-Acting)
Parasympathetic (Indirect Acting Cholinergic Agonist)
- Diagnostic agent for Myasthenia Gravis
- Treatment for Myasthenia Gravis
- Dx: Edrophonium (Tensilon Test)
- Tx: Carbamates (Neostigmine, Pyridostigmine, Ambenonium)
Drugs for Alzheimer’s Disease (CNS -acting: ↑ ACh effects)
Mnemonics:
TAClesa at GALANTe si DONya RIVA
Tacrine
Galantamine
Donepezil
Rivastigmine
Parasympathetic
(Indirect-Acting Cholinergic Agonist)
Side effects/Toxicity [DUMBBELSS]
Diarrhea
Urination
Miosis
Bradycardia
Bronchoconstriction
Emesis
Lacrimation
Sweating
Salivation
Management of Cholinergic Toxicities:
Tx:
▪️Early (short): cholinesterase reactivators
▪️Late (long):
▪️Early (short): Pralidoxime,, Diacetylmonoxime (DAM)
▪️Late (long): Atropine
Cholinergic Antagonist
[Antimuscarinic/Aka: Anticholinergics]
▪️Prototype: (?)
Atropine - inhibits M1, M2, M3
What Drug is:
Effects: Peripheral
▪️M1: block HCl production ( ↓acid secretion)
▪️M2: tachycardia
▪️M3: Mydriasis, Cyclopegia
Uses:
▪️Tx. Symptomatic bradycardia
▪️Tx. Cholinometic Poisoning - Organophosphate: DUMBBELSS
▪️Given with Diphenoxylate as anti-diarrheal [Atropine + Diphenoxylate (Lomotil) ]
Atropine
Parasympathetic Antagonist
(Anticholinergics)
▪️CNS Acting
- Mgt. of Extrapyramidal Syndrome Parkinsonism
Mnemonics: BBT
Benztropine
Biperiden
Trihexyphenidyl
Parasympathetic Antagonist
(Anticholinergics)
▪️CNS Acting
- Mgt. of motion sickness
Scopolamine
Parasympathetic Antagonist
(Anticholinergics)
▪️Mydriatics-for eye exam
▪️Cycloplegics-tx of pain (eye injury)
What drug are under these? (ATCH)
Mydriatics/Cycloplegics
▪️ Anistropine
▪️ Tropicamide
▪️ Cyclopentolate
▪️ Homotropine
Parasympathetic Antagonist
(Anticholinergics)
▪️Bronchodilators (-tropium)
- Mgt. of BA & COPD
SAMA: Ipatropium, Oxytropium
LAMA: Tiotropium (1st Line Reliever in COPD)
▪️1st line reliever for BA
▪️1st line reliever in COPD
▪️SAMA
▪️LAMA (Tiotropium)
Parasympathetic Antagonist
(Anticholinergics)
▪️Selective M1-Blocker (-zepine)
- (-) HCl production
- Mgt. of hyperacidity
Pirenzepine
Telenzepine
Parasympathetic Antagonist
(Anticholinergics)
▪️Selective M3-Blocker
- act as GIT & urinary bladder
- For Urine incontinence & Hypermotility D/O
HNBB
Dicycloverine
Glycopyrrolate
Oxybutinin
Antinicotinics = Nn & Nm
What is Nn Blockers:
Nn Blockers: Ganglionic
Antinicotinics = Nn & Nm
What is Nm Blockers:
Nm Blockers: Nueromuscular Blockers
What drug belongs to:
▪️Nn Blockers: Ganglionic Blockers
- obsolete antiHTNsive
Hexamethonium
Trimethaphan
Mecamylamine
What are the 2 types lf Antinicotinics?
- Nn
- Nm
Use of each Antinicotinics
1. Nn
2. Nm
- For obsolete antihypertensive
- Skeletal muscle-Relaxants , anesthetic adjuncts, spastic D/O
2 Classes of Nm Blockers
- Depolarizing/Irreversible/Non-Comp.
- Non-depolarizing/Reversible/Competitive
What drug under?
Parasympathetic Antagonist
[Nm Blocker-Depolarizing]
Succinylcholine
-MOA: Irrevesible Nm activation
What drug under?
Parasympathetic Antagonist
[Nm Blocker-Non-Depolarizing]
-curare derivatives (2)
Isoquinolones (-curium) Tubocurarine
▪️Atracurium
▪️Cistracurium
Steroidal (-curonium)
▪️Pancuronium
▪️Vecuronium
