Pharm Exam 1 Flashcards
Direct acting agonist
Class: Cholinomimetics
AChE inhibitors
Class: Cholinomimetics
Cholinergic antagonist
Class: Anticholinergics
Neuromuscular blockers
Class: Anticholinergic
Acetylcholine
direct acting Cholinergic Agonist
Muscarinic
Bethanechol
direct acting Cholinergic Agonist
Muscarinic
Pilocarpine
direct acting Cholinergic Agonist
Muscarinic
Nicotine
direct acting Cholinergic Agonist
Nicotinic
Varenicline
direct acting Cholinergic Agonist
Nicotinic
Neostigmine
AChe/Cholinesterase Inhibitor
Pyridostigmine
Ache/Cholinesterase Inhibitor
Physostigmine
Ache/Cholinesterase Inhibitor
Edrophonium
Ache/Cholinesterase Inhibitor
Donepezil
Ache/Cholinesterase Inhibitor
Organophosphates
Ache/Cholinesterase Inhibitor
Pralidozime
Poisoning tx
Cholinesterase Inhibitor
Atropine
Cholinergic Antagonist
Muscarinic
Diphenoxylate-atropine
Cholinergic Antagonist
Scopolamine
Cholinergic Antagonist
Tropicamide
Cholinergic Antagonist
Muscarinic
Ipratropium
Cholinergic Antagonist
Muscarinic
Tolterodine, Fesoterodine, Darifenacin, Solifenacin
Cholinergic Antagonist
Muscarinic
Oxybutynin
Cholinergic Antagonist
Muscarinic
Dicyclomine
Cholinergic Antagonist
Muscarinic
OnabotuliniumtoxinA
Botox
Cholinergic Antagonist
(Muscarinic)
Succinycholine
Depolarizing Nueromuscular Blocker
Direct Acting Agonists and Cholinesterase Inhibitors are what class:
Cholinomimetics
Cholinergic Antagonists and Neuromusc blockers are what class:
Anticholinergics
think “antagonist” and “blockers” are ANTIcholinergics
Muscarinic effects on the heart
stimulates M2 receptors in the SA node
effects primarily SA, AV, and Atrial
Slows conduction thru AV node
Acetylcholine
decreases HR and decreases BP
Ach
M3 receptors on endothelium increase NO –> increase cGMP –> vasodilation
experimentally driven
very short effect bc Ach has such a short half life
Ach
stimulates both Muscarinic and Nicotinic receptors
no clinical use (short half life)
Ach effect
IV infusion: similar to parasympathetic stimulation
EXCEPT: decrease BP
Ach pharmacokinetics
hydrolyzed by AchE (Very quickly)
Bethanechol (Urecholine)
Mechanism
Non specific Muscarinic agonist with highest effect in urinary bladder and GI tract
Bethanechol (Urecholine)
Use
Muscarinic DOC for: increasing GI motility, treating Urinary retention
Bethanechol (Urecholine)
Pharmacokinetics
Quart ammon ion (has charge) does not enter brain bc BBB does not allow any charged ions
Pilocarpine (IsoptoCarpine)
Mechanism
Non specific Muscarinic agonist
Pilocarpine (IsoptoCarpine)
Use
Topical: Acute angle glaucoma (last agent used)
Oral: Xerostomia (dry mouth)
Pilocarpine (IsoptoCarpine)
Adverse Effects
Topical: Blurred vision
Oral: Sweating
Both: HA/brow ache
Overall Adverse effects of Muscarinic Agonists
N/V/D, abd cramp, bladder tightness, sweating, salivation, bronchoconstriction, constricted pupils, blurred vision
Contraindications to Muscarinic Agonists
Asthma/COPD
Peptic Ulcer
Bowel Obstruction
Coronary insuff
Toxicity of Muscarinic Agonists
Mushroom poisoning : muscarine
SLUDGE
SLUDGE side effects of Mushroom poisoning
Salivation Lacrimation Urination Defecation Gastric distress Emesis
Bronchoconstriction d/t Muscarinic poisoning
Treat with atropine (antagonist) and albuterol (beta agonist) to reverse
Sympathetic effects of Nicotine
HTN, tachycardia alternating with vagal bradycardia
Parasymp effects of Nicotine
N/v/d, urination
Varenicline (Chantix)
Mechanism
Partial agonist on the nicotinic receptor
subtype that stimulates reward system in the brain by releasing Dopamine
Varenicline (Chantix)
Use
Smoking cessation (provide some nicotine stimulation to decrease craving)
Varenicline (Chantix)
Adverse Effects
Nightmares
Psychoses
Suicidal ideation
AChE inhibitors
all ganglia activated, so both Parasympathetic and Sympathetic . nerves are stimulated
Parasympathetic dominates the heart
effects of AChE Inhibitors
Ach release increased (ganglia) and prolonged (heart) cardiac M2 receptors are stimulated more
Bradycardia
AChe Inhibitors effect on BP
little effect no cholinergic (Ach) innervation
(BP is only stimulated by sympathetic system)
Myasthenia Gravis
Autoimmune
Antibodies bind to Nicotinic Ach receptors and REDUCE the receptor number able to respond to Ach
not enough Ach can be released to stimulate the low receptor number
Neostigmine and Pyridostigmine
Mechanism
Form covalent bond with AchE enzyme and BLOCK it
Neostigmine and Pyridostigmine
Pharmacokinetics
Hydrolyzed slowly
Quat ammon ion- meaning does NOT enter brain
Neostigmine and Pyridostigmine
Use
Most common used for Myasthenia Gravis
Reverse neuromuscular block after surgery
Postop/neurogenic ileus or atony of urinary bladder
Neostigmine and Pyridostigmine
Adverse Effects
Muscarinic SE, although pt generally becomes tolerant
Physotigmine
Pharmacokinetics
Tertiary amm compound- ENTERS CNS
Physotigmine
Use
systemic use rare: used in Muscarinic Antagonist poitoning (Atropine)
Edrophonium
Pharmacokinetics
VERY short acting (5-10 min), reversible, must be INJECTED
similar to Neo and Pyrido, but more short acting
Edrophonium
Use
to diagnose and determine tx dose for Myasthenia gravis
To reverse neuromuscular blockade after surgery
Donepezil
Pharmacokinetics
Well absorbed orally and CAN enter CNS
Donepezil
Use
Alzheimer’s dz
Finding the right dose of Neostigmine or Pyridostigmine by testing with Edrophonium
Add Edro on top of the Neo/Pyrido
If strength improves: need to increase Neo/Pyrido dose
If strength worsens: dose is too high, need to decrease
(if dose is too high, causing desensitization)
Predominant tone is usually parasympathetic under what receptor
M3
Muscarinic receptors work via:
G proteins
secondary cascade that we don’t need to know details about fo this exam
Nicotinic receptors work via
ligand gated Na+ channel
rapid desensitization
Muscarinic effects on eye
Miosis (contraction of circular muscle)
Accomodation for near vision
Opens angle, decrease pressure
Muscarinic agonists can help what in the eye?
Glaucoma, help decrease pressure
Muscarinic effects on the heart
slow conduction via SA node
M2 receptors
Ach
stimulates both M and N receptors
Decrease BP
Bethanechol (Urecholine)
highest effect on bladder and GI tract
used to: increase GI motility and treat Urinary retention
charged (no enter to brain)
Pilocarpine (IsoptoCarpine)
Applied topically for acute angle glaucoma (last resort though)
Treat Xerostomia (Dry mouth)
SE: blurred vision, sweating, HA
Contraindications to Muscarinic Agonists
Asthma, COPD, Peptic ulcer, Bowel obstruction, Coronary insufficiency/heart dz
Nicotine activates
both para and symp neurons
has para and symp effects
para: n/v/d, urination
symp: HTN, tachy alt with vagal brady
Varenicline (Chantix)
smoking cessation
PARTIAL agonist on Nicotinic receptor
Varenicline (Chantix) bad side effects
nightmare, psychose, SI
Neostigmine and Pyridostigmine
most common drug for Myasthenia Gravis
Also used to: reverse neuromuscular blockade post surgery, and for postop/neurogenic ileus or atony of bladder
Physostigmine
Used in Muscarinic antagonist poisoning
Edrophonium
test dose for Neo and Pyrid
short acting, injected
and to reverse neuro blockade
Donepezil
Alzheimer’s dz
Organophosphates
long lasting effect
soman, sarin, tabun, VX
AChE Inh Toxicity
SLUDGE
Salivation, lacrimation, urination, defecation, gastric distress, emesis
Miosis, sweating, bronchoconstrict, n/v/d
CNS: confusion, ataxia,s lurring, convulsions, coma
Neuromusc stimulation followed by blockade –> paralysis –> respiratory arrest –> Death
Tx of Organophosphate AcHe inh poisoning
Atropine until pupils dilate
2-PAM (Pralidozine) if less than 3-4 hrs since exposure
Diazepam (Valium) for convulsions
Many drugs block Muscarinic receptors:
Old antihistamine (Benadryl) Antidepressants Antipsychotics GI meds Eyedrops Plants
*poisoning fairly common
Nicotinic Receptor
Acetylcholine
Nondepolarizing blocker
Depolarizing blocker