Drugs Flashcards
Acetylecholine
Nicotinic and muscarinic receptors
“Chief parasympathetic NS NT –> contracts smooth muscle, dilates blood vessels, increases secretions, slows heart rate
Additionally involved in muscle contraction (ex. Myasthenia gravis “
Donepezil (Acetylcholinesterase inhibitor)
Increased ACh. Used in alzheimers
improves memory function, attention, ability to ineract with others in CNS diseases “
Neostigmine (Acetylcholinesterase inhibitor)
Neo CNS = No CNS penetration (quaternary
amine).
Postoperative and neurogenic ileus and urinary retention, myasthenia gravis, reversal of neuromuscular junction blockade (postoperative).
Physostigmine (Acetylcholinesterase inhibitor)
Increases ACh. Phreely (freely) crosses blood-brain
barrier = CNS (tertiary amine).
“Can reduce pressure in the eye by decreasing fluid (treatment for glaucoma)
Antidote for anticholinergic toxicity; physostigmine “phyxes” atropine overdose.
Edrophonium (Acetylcholinesterase inhibitor)
increase in the ACh
Historically used to diagnose myasthenia gravis
Pyridostigmine (Acetylcholinesterase inhibitor)
Increased ACh. Increased muscle strength. Preferred use for MG (long acting). does not penetrate CNS (quaternary amine).
Pilocarpine (Cholinomemetic)
Potent stimulator of sweat, tears, and saliva Open-angle and closed-angle glaucoma,
xerostomia (Sjögren syndrome)
resistant to AChE, can cross blood- brain barrier (tertiary amine). “You cry, drool, and sweat on your ‘pilow.’ ”
Bethanechol
Cholinomemetic
muscarinic and nictonic receptors
Activates bowel and bladder smooth muscle; resistant to AChE. No nicotinic activity. “Bethany, call (bethanechol) me to activate your bowels and bladder.”
Nicotine (stimulant of nicotinic acetylcholine receptors in autonomic ganglia)
nicotinic receptors
increase HR, heightened mood, elevated BP, increased alertnes, better memory
Atropine (anti-muscarinic)
Used to dilate the pupil.
Blocks DUMBBeLSS in cholinesterase inhibitor poisoning. Does not block excitation of skeletal muscle and CNS (mediated by nicotinic receptors).
Side effects:
Hot as a hare Dry as a bone Red as a beet Blind as a bat Mad as a hatter Full as a flask
Darifenacin (Anti-muscarinic)
inhibiton of muscarinic receptors
typically used to treat overactive bladder or urgency incontinance (by relaxing bladder muscles)
Botulinum toxin (Anti-cholinomemtic )
SNARE proteins in motor neurons causing inhibition of release of ACh
“Causes decending flaccid paralysis
Affects PNS only (can’t break BBB)”
Glycopyrrolate (muscarinic antagonist)
M1 and M3 specific antagonist both are Gq
typically used preoperatively to reduce drooling and to reduce airway secretions
Ipratropium (Inhaled M3 antagonist)
M3 in the lungs
COPD, asthma (“I pray I can breathe soon!”).
Oxybutynin (Oral M3 antagonist)
Reduce bladder spasms and urge urinary
incontinence (overactive bladder).
Scopolamine (M1 antagonist)
CNS M1 antagonist
can be used in a transdermal patch to treat motion sickenss
Pralidoxime (Cholinesterase reactivator)
AChE
“antidote to organophosphate
adminstered after atropine in organophosphate poisoning “
Hexamethonium (non-depolarizing nicotinic receptor blocker)
especially blood vessel nAChR
used for chronic hypertension
A compound that activates the M3 receptor would do what?
PNS: Rest and digest: M1-M5
Bronchoconstriction, vasodilation, urination, defecation, pupil constriction, bradycardia
ACH injection would cause what symptoms?
Bradycardia, miosis, bronchoconstriction, urination, defecation, vasodilation
Pilocarpine would increase saliva secretion and what else? What receptor is activated?
It would induce miosis (pupil constriction) and would act on the M2
Blocking nicotinic receptors at PNS and SNS ganglia would cause what symptom?
Urinary retention
Loss of basal autonomic tone (mainly PNS)
Vasculature + sweat glands are under SNS control
An overdose of pyridostigmine would cause what symptoms?
Bradycardia
pyridostigmine= ACHE inhibitor, increase ASH = increase PNS
DUMBELLS
What medication is used for COPD and is a muscarinic receptor inhibitor?
Ipratropium (induces bronchodilation)
What medication is used to test for MGr?
Edrophonium
Nicotine overdose may cause convulsions and tachycardia. Why?
Nicotine activates the autonomic ganglia of the CNS
A medication given to treat urinary retention would stimulate what receptor and cause what 2nd messenger?
M3(q) which would increased IP3 + DAG
Hexamethonium does what to pupil, blood pressure, and HR?
Decreases blood pressure (hypotension), dilate eyes (SNS), and cause tachycardia (SNS)
Hexamethonium is a ganglionic blocker, basal autonomic tone will be reversed
Eye dilation can be caused by what cholinergic antagonist?
Scopolamine (motion -sickness, dilation)
What side effect would be brought on by atropine?
Atropine is a muscarinic antagonist so you get bronchodilation
Darifenacin does what? What receptor does it inhibit?
Darifenacin treats urinary incontinence. It works on the M3 receptor
How does scopolamine transdermal patch work?
it produces a steady blood level that inhibits M1, M4, and M5 receptors
transdermal = steady