Exam 1 Drugs Compilation Flashcards
Cimetidine
Imidazole
Inhibitor of CYP enzymes (Phase 1), competitive inhibitor of OCT
n/a for now
Decrease metabolism / increase drug level
Phenobarbital
Barbiturate
Activator of CYP enzymes (Phase 1)
n/a for now
Increase metabolism, decrease drug level
Probenecid
n/a
competitive inhibitor of OAT
n/a
Decreases secretion of anions
Ethanol
n/a
Activator of CYP enzymes
Increase metabolism, decrease drug level
Proadifen
n/a
Only known role is as inhibitor of CYPs
Decrease metabolism / increase drug level
Bethanechol
Muscarinic Receptor Agonist Muscarinic receptor selective Long acting Used to stimulate smooth muscle post-op (Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)
Carbachol
Muscarinic Receptor Agonist
Long acting
Corneal Application for Wide Angle Glaucoma (Increase drainage)
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)
Methacholine
Muscarinic Receptor Agonist
Muscarinic receptor selective
Used to test muscarinic receptor function, slow HR and test bronchial hyperactivity
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)
Muscarine
Muscarinic Receptor Agonist
Muscarinic Receptor selective
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)
Pilocarpine
Muscarinic Receptor Agonist (Natural Alkaloid)
Corneal Application for Wide Angle Glaucoma (increase drainage)
Muscarinic Receptor selective, sweat glands sensitive
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)
Nicotine
Nicotinic Receptor Agonist
Competitive Nicotinic Receptor Agonist
Can cause Autonomic hyperactivity (convulsions, coma, death, respiratory arrest)
Varenicline
Nicotinic Receptor Agonist
Agonist
Used to quit smoking
Ambemonium
Competitive AChE inhibitor
Used to treat myasthenia gravis
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)
Edrophonium
Quaternary Simple Alcohol
Competitive AChE inhibitor
Used to diagnose Myesthenia Gravis
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)
Neostigmine
Carbamate
Competitive AChE inhibitor
Increases smooth muscle motility, treat paralytic ileus and atony of bladder, treatment and diagnosis of myasthenia gravis, reversal of neuromuscular block
** Used to compete off N2 receptor blockers **
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)
Physostigmine
Carbamate
Competitive AChE inhibitor
Topical treatment for wide angle glaucoma
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)
Pyridostigmine
Carbamate
Competitive AChE inhibitor
Treatment of myesthenia gravis, pretreatment for nerve gas exposure, reversal of neuromuscular blockade
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)
diisopropylfluorophosphate
Organophosphate Derivative
Non - Competitive AChE inhibitor
No clinical use
SLUD
echothiophate
Organophosphate Derivative
Non - Competitive AChE inhibitor
Treatment of glaucoma
SLUD
Carbaryl
Insecticide Carbaryl
Non - Competitive AChE inhibitor
No clinical use
SLUD
Malathion
Insecticide Organophosphate Derivative
Non - Competitive AChE inhibitor
Least toxic – used for head lice
SLUD
Parathion
Organophosphate Derivative
Non - Competitive AChE inhibitor
No clinical use
SLUD
Tetraethylpyrophosphate
Insecticide Organophosphate Derivative
Non - Competitive AChE inhibitor
No clinical use
SLUD
Sarin
Nerve Gas - Organophosphate Derivative
Non - Competitive AChE inhibitor
No clinical use
SLUD
Soman
Nerve Gas - Organophosphate Derivative
Non - Competitive AChE inhibitor
No clinical use
SLUD
Pralidoxime
AchE reactivator
Releases phosphoryl moiety to restore AChE activity
Needs to be admin with Atropine, before Aging
Atropine
Muscarinic (selective) Antagonist (Long lasting)
Treatment of insecticide poisoning, anti-parkinson, cause mydriasis and cycloplegia, anti-motion sickness, decreased bronchial secretions, slow smooth muscle, Increase HR, Preanesthetic
Can cause hallucinations and amnesia
Atropine fever, dry mouth
Homatropine
Muscarinic antagonist (Intermediate lasting)
Used to cause mydriasis and cycloplegia
Can cause hallucinations and amnesia, dry mouth, sedation / excitement
Scopolamine
Muscarinic antagonist
Anti-motion sickness, Amnesia before surgery
Can cause hallucinations and amnesia, dry mouth, sedation / excitement
Methscopolamine
Muscarinic antagonist
Slow GI tract
Trihexyphenidyl
Muscarinic antagonist
Antiparkinson therapy, reduce uncoord. Movt.
Can cause hallucinations and amnesia, dry mouth, sedation / excitement
Tropicamide
Muscarinic antagonist (Short acting) Used to cause mydriasis and cycloplegia
Cyclopentolate
Muscarinic antagonist
Used to cause mydriasis and cycloplegia
Ipratropium
Muscarinic antagonist (Quaternary)
Bronchodilation, Decreased bronchial secretions,
Shorter acting for COPD
Tiotropium
Muscarinic antagonist (Quaternary)
Bronchodilation, Decreased bronchial secretions
Longer acting for COPD
Darifenacin
Muscarinic antagonist (M3 Specific)
Slow Smooth muscle, over active bladder (GI / Genitourinary)
Longer Duration of action
Solifenacin
Muscarinic antagonist (M3 Specific)
Slow Smooth muscle, over active bladder (GI / Genitourinary)
Longer Duration of action
Tolterodine
Muscarinic antagonist (M3 Specific)
Slow Smooth muscle, over active bladder (GI / Genitourinary)
Longer Duration of action
Mecamylamine
Ganglionic Blocker
Non-depolarizing competitive antagonist
Good GI absorption
Adjunct for peripheral vascular disease – relieve vasoconstriction and increase perfusion
CNS side effects including tremors, confusion, seizures, mania, depression
Trimethaphan
Ganglionic Blocker
Non-depolarizing competitive antagonist
Used IV in OR to decrease BP to control bleeding, adjunct anti-hypotensive
Succinylcholine
Non-Competitive Nicotinic N2 blocker
Depolarizing – Prevent Depolarization
Causes muscle relaxation, e.g. before surgery
Hydrolyzed by plasma cholinesterase
Curare (t-tubocurarine)
benzylisoquinolines
Competitive Nicotinic N2 blocker (N2 Specific)
Non-depolarizing – Prevent Depolarization
Causes muscle relaxation, e.g. before surgery
* Long acting *
Histamine Release (hypotension) is side effect
Reversed by edrophonium, neostigmine
Atracurium
benzylisoquinolines
Competitive Nicotinic N2 blocker (N2 Specific)
Non-depolarizing – Prevent Depolarization
Causes muscle relaxation, e.g. before surgery
* Intermediate acting *
Histamine Release (hypotension) is side effect
Reversed by edrophonium, neostigmine
Cisatracurium
benzylisoquinolines
Competitive Nicotinic N2 blocker (N2 Specific)
Non-depolarizing – Prevent Depolarization
Causes muscle relaxation, e.g. before surgery
* Intermediate acting *
Histamine Release (hypotension) is side effect
Reversed by edrophonium, neostigmine
Mivacurium
benzylisoquinolines
Competitive Nicotinic N2 blocker (N2 Specific)
Non-depolarizing – Prevent Depolarization
Causes muscle relaxation, e.g. before surgery
* Short acting *
Histamine Release (hypotension) is side effect
Reversed by edrophonium, neostigmine
Pancuronium
Ammonio Steroids
Competitive Nicotinic N2 blocker
Non-depolarizing – Prevent Depolarization
Causes muscle relaxation, e.g. before surgery
* Long acting *
Cross react with Muscarinic and N1 – Tachycardia
Reversed by edrophonium, neostigmine
Vecuronium
Ammonio Steroids
Competitive Nicotinic N2 blocker
Non-depolarizing – Prevent Depolarization
Causes muscle relaxation, e.g. before surgery
* Intermediate acting *
Cross react with Muscarinic and N1 – Tachycardia
Reversed by edrophonium, neostigmine
Metaraminol
Alpha-1 Selective Agonist
Long acting beta 1 and alpha 1 stimulant
Displaces NE
Methoxamine
Alpha-1 Selective Agonist (less alpha 2)
treat hypotensive crisis
Phenylephrine
Alpha-1 Selective Agonist (less alpha 2)
Vasoconstriction, prevent shock, nasal decongestant, treat hypotensive crisis, reduce drug diffusion, reduce mucus membrane congestion, mydriasis
Long acting
Alpha methyldopa
Alpha-2 Selective Agonist
Decrease NT in synapse – replaces DOPA in synthetic pathway to yield Alpha-methyl norepinephrine (false neurotransmitter)
Used to treat hypertension – acts at brainstem vasomotor center
Side effects diminish over time – sedation, xerostomia, anorexia, fluid retention, vivid dreams, impotence, CNS stimulation
Clonidine
Alpha-2 Selective Agonist (less alpha 1)
Decrease NT in synapse (inhibit NE release)
Side effects diminish over time – sedation, xerostomia, anorexia, fluid retention, vivid dreams, CNS stimulation
Guanabenz
Alpha-2 Selective Agonist
Decrease NT in synapse (inhibit NE release)
Side effects diminish over time – sedation, xerostomia, anorexia, fluid retention, vivid dreams, CNS stimulation
Amphetamine
Alpha and beta adrenergic agonist Releasing agent (increases NE release), also releases intraneuronal NE – reverse transport
Ephedrine
Alpha and beta adrenergic agonist
Releasing agent, Stimulant of most adrenergic receptors
Increase CO and arterial pressure, treat orthostatic hypotension, reduce mucus membrane congestion, stress incontinence
Long acting – Displaces NE
Epinephrine
Alpha and beta adrenergic agonist
Binds all adrenergic receptors equally
Potent vasoconstrictor and cardiac stimulant, hemostasis during surgery, reduce drug diffusion, anaphylaxis
Norepinephrine
Alpha and beta adrenergic agonist (except beta 2)
IV infusion for shock, increase CO and cause vasoconstriction (increase BP, treat hypotensive crisis), reduce drug diffusion
Binds Beta-2 a lot less than all other adrenergics
Dobutamine
Beta 1 Selective agonist (Less beta-2)
Cardiogenic shock, heart failure
Isoproterenol
Beta 1 and 2 agonist
Used for relaxation of bronchial smooth muscle, also cardiac stimulation (potent vasodilator)