Cholinergics Flashcards
Nicotinic Antagonist
Competitive Nn blocker
Use - lowers blood pressure
This drug was introduced in the 50’s and there are way better anti-hypertensives
MECAMYLAMINE
TACRINE, DONEPZIL, RIVASTIGMINE, GALANTAMINE
Long acting AChE-inhibitors used to treat DEMENTIA
BETHANACHOL
Half-life - long, not a substrate for acetylcholinesterase
Use - Nonobstructive GI Disorders or URINARY RETENTION
Stimulate GI motility and bladder emptying
d-Tubocurarine
Muscle relaxant
Active component in curare, hypotension
Rarely used due to tendency to release histamine and cause bronchospasm
Some cross reactivity with Nn
CARBACHOL
Half-life - long, not a substrate for acetylcholinesterase
Pupillary constriction
Use - limited, because nicotinic activity stimulates all autonomic ganglia
Some application in treating glaucoma
More selective for M1, which lessens side effects
Less tendency for dry mouth/blurred vision
Peptic Ulcer Disease - suppresses acid secretion via action on parietal cells
PIRENZIPINE
TIOTROPIUM
Bronchodilation
Supposedly more bronchoselective than ipratropium
Has less affinity for M2 receptors (doesn’t cause cardiac side effects)
Increase exercise tolerance
Spasmolytic
Stimulates presynaptic GABA-B receptors, suppressing excitatory transmissions
BACLOFEN
Similar to neostigmine but with a longer duration
MYASTHENIA GRAVIS — primary drug
PYRIDOSTIMINE
Inhibits calcium release from sarcoplasmic reticulum
Treat malignant hypertherima
DANTROLENE
Muscle relaxant
Active component in curare, hypotension
Rarely used due to tendency to release histamine and cause bronchospasm
Some cross reactivity with Nn
d-Tubocurarine
Chronic Asthma/COPD - induces bronchodilation but does not inhibit ciliary motility
Note for acute asthma attacks (beta-2 agonists are much better)
Rhinorrhea — stops runny nose
IPRATROPIUM
MECAMYLAMINE
Nicotinic Antagonist
Competitive Nn blocker
Use - lowers blood pressure
This drug was introduced in the 50’s and there are way better anti-hypertensives
ATROPINE
M1, M2, and M3 receptors
Eyes - causes MYDRIASIS & CYCLOPLEGIA
Promotes BRONCHODILATION and reduces secretions
Initial bradycardia, but in general causes TACHYCARDIA
TREAT AV-blocks and post-MI bradycardia
GI - antispasmodic, can be used to treat IBS
Use for OVERACTIVE BLADDER
Anti-AchE poisoning
BACLOFEN
Spasmolytic
Stimulates presynaptic GABA-B receptors, suppressing excitatory transmissions
PYRIDOSTIMINE
Similar to neostigmine but with a longer duration
MYASTHENIA GRAVIS — primary drug
TOLTERODINE, OXYBUTYNIN, DARIFENACIN, SOLIFENACIN
Slightly more selective for the M3 receptors
Used to treat OVERACTIVE BLADDER and incontinence
Neurologic problems
SUCCINYLCHOLINE
Depolarizing blocker Hyperkalemia Myalgia Ganglionic Stimulation Malignant Hyperthermia
Eyes - causes MYDRIASIS & CYCLOPLEGIA
Promotes BRONCHODILATION and reduces secretions
Initial bradycardia, but in general causes TACHYCARDIA
TREAT AV-blocks and post-MI bradycardia
GI - antispasmodic, can be used to treat IBS
Use for OVERACTIVE BLADDER
Anti-AchE poisoning
ATROPINE
Prophylactic for MOTION SICKNESS
Can be used as a patch
SCOPOLAMINE
Depolarizing blocker Hyperkalemia Myalgia Ganglionic Stimulation Malignant Hyperthermia
SUCCINYLCHOLINE
PIRENZIPINE
More selective for M1, which lessens side effects
Less tendency for dry mouth/blurred vision
Peptic Ulcer Disease - suppresses acid secretion via action on parietal cells
Partial nicotinic agonist that reduces nicotine craving
Causes nightmares
VARENCICLINE
Covalently bind and inactivate AChE, undergo aging (irreversible)
SLUDGEM symptoms - Bradycardic, Excessive Tearing, Can’t breathe
Parathion, Malathion, Echothiophate
Use — DIAGNOSIS of myasthenia gravis via injection Cholinergic Crisis (Tensilon Test) - identify if they are OVER or UNDER treated
EDROPHONIUM
IPRATROPIUM
Chronic Asthma/COPD - induces bronchodilation but does not inhibit ciliary motility
Note for acute asthma attacks (beta-2 agonists are much better)
Rhinorrhea — stops runny nose
Anti-Cholinergic Toxicity
Hot dry skin, Dry mouth, Dry eyes
Mydriasis and Cyclopegia —> Blurred vision (Blind as a bat)
Narrowing of anterior chamber and diminished outflow of aqueous humor
Sedation, Agitation, Hallucination, Coma (Mad as a Hatter)
PILOCARPINE
Half-life - long, not a substrate for acetylcholinesterase
Glaucoma - contracts ciliary muscle and increases outflow of aqueous humor
Xerostomia - stimulates salivary glands, useful in Sjorgen’s syndrome
Can cause Diaphoresis
GI atony - used in cases of post-operative paralysis of the GI tract
GU atony - used in post-operative dysuria
Glaucoma - miosis, lowers IOP
Myasthenia Gravis - most common treatment in the US, increases Ach concentration @ NMJ
NM blockade reversal - reverses paralysis from competitive NM blockade agents (eg Curare and related drugs)
NEOSTIGMINE
Act on GABA receptors in the CNS
DIAZEPAM
Long acting AChE-inhibitors used to treat DEMENTIA
TACRINE, DONEPZIL, RIVASTIGMINE, GALANTAMINE
Half-life - long, not a substrate for acetylcholinesterase
Use - Nonobstructive GI Disorders or URINARY RETENTION
Stimulate GI motility and bladder emptying
BETHANACHOL
Slightly more selective for the M3 receptors
Used to treat OVERACTIVE BLADDER and incontinence
Neurologic problems
TOLTERODINE, OXYBUTYNIN, DARIFENACIN, SOLIFENACIN
METHACHOLINE
No effect in normal patients, but will provoke airway constriction in asthmatics
Used to diagnose bronchial hyperreactivity (asthma) WHEEZING
SCOPOLAMINE
Prophylactic for MOTION SICKNESS
Can be used as a patch
No effect in normal patients, but will provoke airway constriction in asthmatics
Used to diagnose bronchial hyperreactivity (asthma) WHEEZING
METHACHOLINE
EDROPHONIUM
Use — DIAGNOSIS of myasthenia gravis via injection Cholinergic Crisis (Tensilon Test) - identify if they are OVER or UNDER treated
Parathion, Malathion, Echothiophate
Organophosphates
Covalently bind and inactivate AChE, undergo aging (irreversible)
SLUDGEM symptoms - Bradycardic, Excessive Tearing, Can’t breathe
Tx: Pralidoximine, Atropine
Half-life - long, not a substrate for acetylcholinesterase
Glaucoma - contracts ciliary muscle and increases outflow of aqueous humor
Xerostomia - stimulates salivary glands, useful in Sjorgen’s syndrome
Can cause Diaphoresis
PILOCARPINE
Bronchodilation
Has less affinity for M2 receptors (doesn’t cause cardiac side effects)
Increase exercise tolerance
TIOTROPIUM
VARENCICLINE (“Chantix”)
Partial nicotinic agonist that reduces nicotine craving
Causes nightmares
1-800-VERY CLEAN
Sometimes used in ophthalmic surgery to constrict pupil (Miochol)
Acetylcholine
Acetylcholine
Half-life - very short, rapidly metabolized by acetylcholinesterase
Use - Limited clinical use due to potential side effects, sometimes used in ophthalmic surgery to constrict pupil (Miochol)
NEOSTIGMINE
GI atony - used in cases of post-operative paralysis of the GI tract
GU atony - used in post-operative dysuria
Glaucoma - miosis, lowers IOP
Myasthenia Gravis - most common treatment in the US, increases Ach concentration @ NMJ
NM blockade reversal - reverses paralysis from competitive NM blockade agents (eg Curare and related drugs)
DIAZEPAM
Spasmolytic
Benzodiazepines act on GABA receptors in the CNS
Rocuronium
Muscle relaxant for surgery
Nm selective, no CV side effects
Muscle relaxant for surgery
Nm selective, no CV side effects
Rocuronium
DANTROLENE
Inhibits calcium release from sarcoplasmic reticulum
Treat malignant hyperthermia
Half-life - long, not a substrate for acetylcholinesterase
Pupillary constriction
Use - limited, because nicotinic activity stimulates all autonomic ganglia
Some application in treating glaucoma
CARBACHOL
Hot dry skin, Dry mouth, Dry eyes
Mydriasis and Cyclopegia —> Blurred vision (Blind as a bat)
Narrowing of anterior chamber and diminished outflow of aqueous humor
Sedation, Agitation, Hallucination, Coma (Mad as a Hatter)
Anti-Cholinergic Toxicity
