Parasympathetic / Cholinergic Flashcards
Cholinergic transmission steps
Synthesis Storage in vesicles Release Binding to receptor Degradation of acetylcholine Recycling of choline
Carries choline from extracellular to pre-synaptic region
Na-dependent transporter
Process in synthesis
Enzyme
Product
Acetylation
Choline acetyltransferase
Acetylcholine
Inhibits transporter, uptake of acetylcholine
Vesamicol
Inhibits transport of choline to the pre-synaptic region
Hemicholinum
Blocks release of acetylcholine
Decreased neurotransmitter
Decreased muscle contraction
Paralysis
Botulinum toxin
Cholinoceptors
Muscarinic
Nicotinic
M1
E - exocrine glands
A - autonomic glands
C - CNS
M2
HCSP Heart CNS Smooth muscle Peripheral nerve
M3
ESEBC Exocrine glands Smooth muscle Eye Blood vessel CNS
M4
CNS
Enhanced locomotion
M5
CSI
CNS
Salivary glands
Iris
NN
Ganglion - stimulation
CNS - neurotransmisson
NM
Skeletal muscle - contraction
Subtypes of cholinergic agonists
DIRECT
Indirect
DIRECT acting cholinergic agonists
Choline esters
Alkaloids
Choline esters
Acetylcholine
Bethanechol
Carbachol
Methacholine / provocholine
Most potent cholinergic agonist
Cause 10-Min miosis during cataract surgery
Lack of selectivity
Acetylcholine
Strong muscarinic activity
Increase intestinal motility after surgery
Bethanechol
Ester of carbamic acid
Carbachol
For open angle glaucoma that is resistant to pilocarpine
Carbachol
Weak nicotinic activity
Diagnosis of asthma
Methacholine
What should be given after the methacholine test
Rapid-acting bronchodilator
DOC for glaucoma
Can Cross blood brain barrier
Pilocarpine
No therapeutic use
Muscarine
Has muscarinic and nicotinic activity
Potential for Alzheimer’s
Arecholine
Indirect-acting cholinergic agonists /
Cholinesterase inhibitors
Organophosphates
Carbamates
Quaternary amines
DFP Keana
Diisopropylfluorophosphate
Organophosphates
Isofluorophate
Echothiophate
Malathion, parathion
Tabon, sarin, soman
Chronic treatment of open-angle glaucoma
Duration 1 week
Isofluorophate
Open angle glaucoma
3-7 days
Echothiophate
Insecticides / Pesticides
No clinical use
Active metabolites: malaoxon, paraoxon
Malathion, parathion
Phospholine Iodide
Echothiophate
Placed on soldiers to combat the spread of life threatening diseases on the Front lines typhus and Malaria
DDT
dichlrorodiphenyltrichloroethane
Nerve gases
Tabun
Sarin
Soman
Organophosphate toxicity
Cholinergic Crisis
Antidote for cholinergic Crisis
Pralidoxine chloride 2 PAM
Atropine
Carbamates
Physostigmine eserine
Neostigmine prostigmin
Pyridostigmine mestinon
Intestinal and bladder atony
Miotic agent for open angle glaucoma
6-12 hrs
Physostigmine
Treats MYASTHENIA GRAVIS
Paralytic ileus or atony of the urinary bladder
Antidote for TUBOCURARINE POISONING
3-6 hrs
Neostigmine
Carbamate insecticides
Carbaryl
Propoxur
Aldicarb
For tensilon test - diagnosis of myasthenia gravis
Edrophonium
Cholinergic antagonists
Muscarinic blockers
Ganglion blockers
Neuromuscular blockers
Prevents motion sickness
Blocks short-term memory
Scopolamine
Scopolamine, when given with atropine produces
Twilight sleep
Produce mydriasis and cycloplegia for ophthalmoscopic examination
Homatropine
Cyclopentolate
Tropicamide
For ASTHMA and COPD chronic obstructive pulmonary disease
More peripheral effects less CNS effects
Ipratropium bromide
Treatment for COPD
Tiotropium
For peptic ulcer
Selective for muscarinic receptor in the stomach
Pirenzepine
Pirenzepine decreases secretion of
Acid and pepsin
Parkinson’s disease
Extrapyramidal disorders
Benztropine
Trihexyphenidyl
Oxybutynin
Hypermotility of the bowel
Dicyclomine
Reduces GI smooth muscle spasms
Adjunct for peptic ulcer
Propantheline
Other drugs that have anticholinergic effects
Antihistamines
Antipsychotics
TCAs
Opioids
Block nicotinic receptors causing paralysis
Neuromuscular blockers /
Skeletal muscle relaxants
Subtypes of neuromuscular blockers
Competitive non-depolarizing
Competitive depolarizing
Compete with acetylcholine at nicotinic receptors
Prevent depolarization
Inhibit muscular contraction
Nondepolarizing blockers
Adjunct to anesthesia
For short surgical operations
Very little histamine release
Vecuronium
Mechanical ventilation for critically ill patients
Ideal for patients with kidney and liver failure
Atracurium
Cisatracurium
No histamine release
Cisatracurium
Has vagolytic actions
Used when elevated heart rate is desired
Pancuronium
Increase heart rate
No histamine release
Pancuronium
Prevents fasciculation associated with succinyl choline
Tubocurarine
Tubocurarine adverse effects
Hypotension:________
Bronchospasm:_________
Histamine
Ganglionic blockade
For short surgical procedures
Mivacurium
Mivacurium is hydrolyzed by
Plasma cholinesterase
Useful for tracheal intubation in patients with gastric contents
Rocuronium
Adjunct to anesthesia in long surgery cases
Long duration in patients with renal dysfunction
Pipecuronium
Doxacurium
DRUG INTERACTIONS of Nondepolarizing neuromuscular blockers
Cholinesterase inhibitors
Halogenated hydrocarbon anesthetics
Aminoglycoside antibiotics
Calcium channel blockers
Can overcome the action of nondepolarizing blockers
Cholinesterase inhibitors
Neostigmine, physostigmine, edrophonium
Enhance neuromuscular blockade by exerting a stabilizing action of nondepolarizing blockers
Halogenated hydrocarbon anesthetics
Inhibit ACh release from cholinergic nerves by competing with calcium ions
Aminoglycoside antibiotics
May increase the neuromuscular block of nondepolarizing and dep blockers
Calcium channel blockers
Muscle regidity and hyperpyrexia
Malignant hyperthermia
Treatment for malignant hyperthermia
DANTROLENE
- blocks release of calcium from the sarcoplasmic reticulum of muscle cells
Rapidly cooling the patient
Pre-reversal
Atropine
Glycopyrrolate
Reversal
Cholinesterase inhibitors
Block nicotinic receptors in both sympathetic and parasympathetic ganglia
Ganglionic blockers
Ganglionic blockers
Hexamethonium
Trimethaphan
Mecamylamine
Nicotine
First drug effective for hypertension
Hexamethonium
Treatment of hypertensive emergencies caused by pulmonary edema or dissecting aortic aneurysm
Trimethaphan
Treats moderately severe to severe hypertension
Mecamylamine
Nicotine
Low dose: _______
High dose: _______
Ganglionic stimulation
Ganglionic blockade