Drugs to Know Flashcards
Acetominophen
- Normally GSTs catalyze reaction of transferring GSH (glutathione) to NAPQI -> inactive form that gets eliminated
- If OD –> deplete glutathione and accumulate NAPQI which kills liver and kidney cells (TOXIC)
- Tylenol
- Fever and pain reducer
Acetylcholine
- Nicotinic and muscarinic receptors
- Can be used to reduce pupil size in eye (inc miosis in ocular surgery); give intra-ocularly NOT systemically
- LOCAL EFFECTS
- Can give local infusion - will work on muscarinic receptors on vessels –> local vasodilation to inc blood flow tot hat area w/o systemic dec in BP
Albuterol
Beta 2 agonist
-bronchodilator (for asthma)
Alpha Methyl Dopa
central alpha 2 agonist –> dec central symp outflow (vasomotor center) bu inc inhibitory effect of these alpha 2 receptors–> dec BP
safe in pregnancy; so anti-hypertensive for pregnant women
Alpha Methyl Tyrosine
Sympatholytic
Inhibits tyrosin hydroxylase - dec in catecholamine synthesis
Synthetic tyrosine analogue
Amphetamine
- Leads to inc NE release –> extracellular fluid
- How? by inc exocytosis and inc release of NE from vesicle
- Crosses BBB so CNS effects
Atracurium
- Neuromuscular blocking agent
- Non-depolarizing, competitive
- Intermediate duration
In general…- Bind at same site at acetylcholine - only need to bind one of two alpha sites
- Dec frequency of channel opening
- Progression: motor weakness —> small rapidly moving muscles like eyes and jaw go first —> limbs/trunk —> intercostals —> diaphragm
- **Regained in reverse order
Atropine
Muscarinic antagonist (no effect on nicotinic receptors)
- Inhibit cholinesterase inhibitor toxicity (nerve gas exposure)
- good at .5-1 mg then bad CNS effects (because it crosses the BBB)
- at low dose it slows heart by M2 inhibitory receptors
- balance cardio effects of neostigmine in surgery, dilate eye, reduce bronchial contraction and secretion in lungs,
- side effects= dry mouth urinary retention
- Crosses BBB so also causes sleepiness
Carbachol
- MIOSTAT
- Used to close eye for protection in surgery (but slower onset and longer duration than local acetylcholine infusion)
Clonidine
Central alpha 2 agonist
Treats hypertension by dec symp tone (from vasomotor center)
Dec both cardiac output and TPR
Useful in hypertensive emergency- quick effect
Cocaine
- Blocks dopamnie and serotonin receptors for termination (blocks SERT, DAT and NET)
- Dec transport of NE back into cell –> more NE at receptors
- Overdose can lead to adrenergic crisis
- Crosses BBB so CNS effects
Diazepam
VALIUM
- benzo
- Inc GABA affinity for GABA A receptor –> inc Cl- into cell (so need GABA present to work); inc frequency of opening NOT duration of opening
- Anti-anxiety, treats seizures, treats alcohol withdrawal and insomnia
Dopamine
- Catecholamine
- DA > B1»_space; a1
- @ low dose DI induced inc in blood flow (vasodilation)- including inc blood flow to kidneys
- @ medium dose…beta 1 -induced in contractility w/o effect on BP
- @ high dose …alpha 1 -induced inc in BP (used for SHOCK)
-Also mixed acting (both inc release of catecholamines and works right on receptors)
Edrophonium
- Used to diagnose m. gravis (because short onset and short duration)
- If temporary relief of symptoms then pos diagnosis
- Cholinesterase inhibitor
Ephedrine
Non-selective adrenergic agonist (alpha and beta)
Mixed acting (so can inc NE release or act right on adrenergic receptor)
Inc BP, decongestant and bronchodilator
Epinephrine
- @ low dose … beta 2 agonist … inc contraction and heart rate while dec in peripheral resistance (beta 2 vasodilation)
- @ high dose… alpha agonist …inc vascular resistance and thus inc BP; also dec renal blood flow while inc muscle blood flow (beta 2 vasodilation is now offset by alpha vasoconstriction)
Flumazenil
- Used for benzo overdose
- GABA A receptor antagonist; binds to same spot on receptor as benzos; short half-life (30-60 min) so must monitor closely
- If too much can lea to withdrawal seizures
Ganacurium
Non-depolarizing neuromuscular block
In general…- Bind at same site at acetylcholine - only need to bind one of two alpha sites
- Dec frequency of channel opening
- Progression: motor weakness —> small rapidly moving muscles like eyes and jaw go first —> limbs/trunk —> intercostals —> diaphragm
- **Regained in reverse order
May replace succinylcholine b/c also ultra-short onset and duration but is non-depolarizing
Glycopyrrolate
Muscarinic Antagonist
Used to block sinus or nodal bradycardia (reverse effects of neostigmine) AKA inc HR
Does not cross BBB (unlike atropine) so does not cause sleepiness and other CNS effects
Also decreased secretions
Charged molecule
Guanethidine
- Sympatholytic
- Replace NE n vesicles/prevent NE release from storage vesicles
- Antihypertensive
- Uses Uptake 1 to get into pre-synaptic terminal where it can then act on NE neurotransmission
Ipratropium
ATROVENT
Used to treat COPD
Muscarinic antagonist
Charged
Does not cross BBB
Isoproterenol
beta agonist (B1»B2)
-inc HR w/o changing BP; bronchodilator; inc cardiac output (BUT HIGH O2 DEMAND)
Ionotropic and vasodilator (works on beta 2 on vessels)
Lidocaine
amine LA (long lasting; more stable)
- Stabilize inactive form of ion channels…inability to produce action potential
- DO NOT BLOCK CHANNEL ITSELF
- Bind to the wall of the channel pore —> conformational change
Aniline or benzoic acid linked to tertiary amine via amide bond
Methacholine
Direct muscarinic agonist
- Used to diagnose airway hypersensitivity (people w/ asthma will have response w/ lower dose of drug than normal person)
- Non-selective
Modanifil
PROVIGIL “wake promoting agent”
- psychostim (inc sleep vigilance and dec need for sleep)
- For narcolepsy, sleep disorder due to shift work or sleep apnea)
Amphetamine-like sympathomimetic
Central alpha1 agonist??
Muscarine
acts on muscarinic receptors –> parasymp response
Toxic- mushroom poisoning
Neostigmine
Cholinesterase Inhibitor
- Reversible
- Treat m. gravis (because longer lasting than edrophonium but does not cross BBB so no CNS effects )
- In surgery… reverse paralysis from neuromuscular block (given w/ glycopyrrolate so no anti-muscarinic effects) and reverse anti-muscarinic effects of inc HR
Nicotine
acts on nicotinic receptors at ganglia and NMJ
addictive b/c desensitization
when it works on ganglia- enhances underlying tone (symp or parasymp) - tachycardia, inc BP, sweating
Norepinephrine
- catecholamine
- Mainly alpha effects (works on beta to inc HR but only transient b/c body compensates for now high BP from alpha effects –> slows HR back down via baroreceptors)
- Inc peripheral resistance/ inc BP
- dec renal, cutaneous and muscle blood flow (unlike dopamine - which inc renal blood flow)
Organophosphates
Cholinesterase Inhibitor
- Irreversible (ages the enzyme)
- Insecticides, nerve gas (serin, VG, VX), DFP (drug)
2-PAM
Treat cholinesterase inhibitor toxicity (esp in military)
Must use right away b/c only works b/f the receptor has aged
Pancuronium
Non-depolarizing neuromuscular block
Competitive inhibitor
Long duration
In general…- Bind at same site at acetylcholine - only need to bind one of two alpha sites
- Dec frequency of channel opening
- Progression: motor weakness —> small rapidly moving muscles like eyes and jaw go first —> limbs/trunk —> intercostals —> diaphragm
- **Regained in reverse order
Phenobarbital
LUMINAL
- barbiturate
- Directly activates GABA A receptor to keep Cl- channel open longer (but considered reversible)
- anti-seizure and sedative/hypnotic effects
- induces certain CYPs –> potential drug interactions
Phenylephrine
- Alpha 1 agonist (JUST ALPHA)
- Ocular/nasal vasoconstrictor (decongestant), acute vasopressor
Physostigmine
Cholinesterase Inhibitor
- Reversible
- Not used to treat m gravis b/c crosses BBB (CNS effects)
- Can cause seizures
- Can also reverse effects of atropine OD in CNS since both cross the BBB
Propanolol
non-slective beta agonist (BETA BLOCKER)
- INDERAL
- Can cause dec in exercise capacity b/c blocks the beta 2 receptors on vessels going to muscle - no vasodilation to inc blood flow to muscles when exercising
Prozosin
MINIPRESS
selective alpha 1 antagonist (blocks receptors directly)
antihypertensive b/c prevents alpha 1 vasoconstriction
Pyridostigmine
Cholinesterase Inhibitor
- Reversible
- Treat m. gravis b/c does not pass BBB
Reserpine
inhibit transport of NE into storage vesicles –> deplete vesicular NE –> subsequent destruction by MAO inside pre-synaptic cell
So overall has a sympatholytic effect
Blocks VMAT (enzymes that loads NE into vesicles for release into synapse)
Scopolamine
Muscarinic antagonist
Used to treat motion sickness (usually patch)
Dec vestibular muscarinic effects
Central- crosses BBB to have effects on CNS
Also causes euphoria —> abuse (“mad as a hatter”)
Succinylcholine
Depolarizing neuromuscular block
quick b/c degraded by cholinesterase (unless using cholinesterase inhibitor)
Short onset and ultra-short duration so used for quick procedure such as intubation
Eliminated by butylcholinesterase NOT acetylcholinesterase
If prolonged apnea after use - patient may have dec levels of plasma butyl cholinesterase
Tamsulosin
alpha 1 selective antagonist
Treat benign prostate hypertrophy
Blocks alpha 1 receptors in bladder smooth muscle and in prostate to enhance urine flow (b/c prostate hypertrophy inhibits urine flow)
Terbutaline
beta 2 agonist
delay labor (dec contractions in premature labor) and short-acting bronchodilator
Tolterodine
Muscarinic antagonist w/ partial receptor selectivity
Competitive antagonist - synthetic derivative to competes w/ acetylcholine at receptor site
For neuronal/urge urinary incontinence (not stress incontinence)
Tropicamide
Synthetic muscarinic antagonist
Short duration - short acting paralysis of eye muscles
Used by eye Dr for dilation of eye for procedures
Lose ability to see near-sight
Tyramine
- Indirect acting sympathomimetic
- Promote NE exocytosis or NE displacement from vesicles–> accumulation of NE at receptor sites (similar to amphetamines)
- In diet (aged cheese, poultry, fish, wine, beer, yeast, beans) but normally degraded by MAO in liver - so usually only a problem if taking MAO inhibitors (class of anti-depressants)
