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acetylcholine
direct acting cholinergic agonist
indication: injected into eye during surgery
MoA: binds to M2/M3 receptors on iris
effects: miosis
very limited clinical uses b/c it doesn’t pass through membranes easily & is rapidly broken down
B12
vitamin ____ deficiency can lead to pernicious anemia
bethanech
direct acting cholinergic agonist
indication: urinary retention
MoA: binds M3/M2 receptors on bladder
adverse effects:
sweating
increased GI motility
miosis
increased accommodation
increased tearing
retinal detachment
decreases IOP
contraindications: bradycardia & asthma/COPD
pilocarpine, cevimeline
direct acting cholinergic agonist
indication: Sjogren’s syndrome
MoA: binds & stimulates M2/M2 receptors on lacrimal & salivary gland
adverse effects:
sweating
increased urination
increased GI motility
miosis
increased accommodation
retinal detachment
decreases IOP
contraindications: bradycardia & asthma/COPD
edrophonium
reversible, indirect acting cholinergic agonist
indication: diagnosis of myasthenia gravis
MoA: binds & inhibits acetylcholinesterase
adverse effects:
sweating
increased salivation
increased urination
increased GI motility
miosis
increased accommodation
retinal detachment
decreases IOP
contraindications: bradycardia, asthma/COPD
can’t cross BBB
pyridostigmine, neostigmine
reversible, indirect acting cholinergic agonist
indication: long-term tx of myasthenia gravis
MoA: binds & inhibits acetylcholinesterase
adverse effects:
sweating
increased salivation
increased urination
increased GI motility
miosis
increased accommodation
retinal detachment
decreases IOP
contraindications: bradycardia, asthma/COPD
can’t cross BBB
physostigmine
reversible, indirect acting cholinergic agonist
indication: myasthenia gravis tx
MoA: binds & inhibits acetylcholinesterase
adverse effects:
sweating
increased salivation
increased urination
increased GI motility
miosis
increased accommodation
retinal detachment
decreases IOP
contraindications: bradycardia, asthma/COPD
can cross BBB
echothiophate
irreversible, indirect acting cholinergic agonist
indication: decrease IOP in glaucoma (not really used)
MoA: covalently binds & inhibits acetylcholinesterase
adverse effects:
sweating
increased salivation
increased urination
increased GI motility
miosis
increased accommodation
retinal detachment
decreased IOP
skeletal muscle cramps or weakness (if OD)
contraindications: bradycardia, asthma/COPD
atropine
cholinergic antagonist
indication: emergent cardiac or respiratory issues
MoA: binds & inhibits M1/2/3 receptors on heart & lungs & brain (crosses BBB)
adverse effects:
dry mouth
decreased sweating
tachycardia
urinary retention
constipation
mydriasis
dry eye
hallucinations
ataxia
delirium
coma
scopolamine
cholinergic antagonist
indication: motion sickness or nausea/vomiting conditions
MoA: binds & inhibits M1/2/3 receptors in brain (crosses BBB)
adverse effects:
dry mouth
decreased sweating
tachycardia
urinary retention
constipation
mydriasis
dry eye
hallucinations
ataxia
delirium
coma
contraindications:
ipratropium, tiotropium, umeclidinium
cholinergic antagonist
indication: asthma/COPD
MoA: binds & inhibits M2/M3 receptors on lungs
adverse effects:
dry mouth
tachycardia
mydriasis (M3 inhibition at iris sphincter)
dry eye (M2/M3 inhibition at lacrimal gland)
increased IOP (M2/M3 inhibition on ciliary muscle)
reduced accommodation (M2/M3 inhibition on ciliary muscle
oxybutynin, tolterodine, solifenacin, hyoscyamine
cholinergic antagonist
indication: overactive bladder
MoA: binds & inhibits M2/M3 receptors on bladder
adverse effects:
dry mouth
decreased sweating
tachycardia
urinary retention
constipation
mydriasis
dry eye
hallucinations
ataxia
delirium
coma
glycopyrrolate
cholinergic antagonist
indication: hyperhidrosis
MoA: binds & inhibits M2/M3 receptors on sweat glands
adverse effects:
dry mouth
tachycardia
urinary retention
constipation
mydriasis
dry eye
hallucinations
ataxia
delirium
coma
physostigmine
what is the antidote for atropine overdose?
atropine
what is the antidote for a pyridostigmine or neostigmine overdose?
pralidoxime
what is the antidote for an echothiophate overdose?
nicotine
ganglionic agonist
indication: smoking cessation
MoA: binds nicotinic receptors in sympathetic & parasympathetic ganglia
adverse effects of smoking it:
dry eye (smoke irritation)
worsens TED
worsens AMD
progresses cataracts
affects the dominant system at the time
epinephrine
adrenergic agonist
indication: anaphylaxis, cardiac arrest, respiratory emergency
MoA: binds & stimulates a1, a2, B1, B2
adverse effects:
mydriasis (a1 stimulation on dilator)
dry eye (a1 stimulation on lacrimal gland)
decreased accommodation (B2 stimulation on ciliary muscle)
eyelid raise (a1 stimulation on Mueller’s muscle)
decreased eye redness (a1 stimulation on vessels)
increased IOP (B1 & B2 stimulation increasing aqueous humor production)
norepinephrine
adrenergic agonist
indication: shock, cardiac arrest
MoA: binds & stimulates a1, a2, B1
adverse effects:
mydriasis (a1 stimulation on dilator)
dry eye (a1 stimulation on lacrimal gland)
decreased accommodation (B2 stimulation on ciliary muscle)
eyelid raise (a1 stimulation on Mueller’s muscle)
decreased eye redness (a1 stimulation on vessels)
increased IOP (B1 & B2 stimulation increasing aqueous humor production)
isoproterenol
non-selective beta agonist
indication: shock, cardiac arrest
MoA: binds & stimulates B1, B2
adverse effects:
decreased accommodation (B2 stimulation on ciliary muscle)
increased IOP (B1 & B2 stimulation increases aqueous humor production)
albuterol, levalbuterol, salmeterol, formoterol, vilanterol
selective beta agonist
indication: asthma & COPD
MoA: binds & stimulates B2
adverse effects:
decreased accommodation (B2 stimulation on ciliary muscle)
increased IOP (B2 stimulation increases aqueous production)
phenylephrine, oxymetazoline
selective alpha agonist
indication: nasal congestion
MoA: binds & stimulates a1
adverse effects:
HTN
mydriasis (a1 stimulation on dilator)
dry eye (a1 stimulation on lacrimal gland)
eyelid raise (a1 stimulation on Mueller’s muscle)
decreased eye redness (a1 stimulation on conjunctival vessels)
cocaine
indirect adrenergic agonist
indication: severe nosebleeds
MoA: blocks NE reuptake
adverse effects:
HTN
mydriasis (a1 stimulation on dilator)
dry eye (a1 stimulation on lacrimal gland)
decreased accommodation (B2 stimulation on ciliary muscle)
eyelid raise (a1 stimulation on Mueller’s muscle)
decreased eye redness (a1 stimulation on vessels)
increased IOP (B1 & B2 stimulation increasing aqueous humor production)
crack cornea (if smoked)
corneal ulcers (if smoked)
pseudoephedrine
mixed acting adrenergic agonist
indication: nasal decongestion
MoA: binds & stimulates a1, a2, B1, B2
adverse effects:
HTN
tachycardia
urinary retention
mydriasis (a1 stimulation on dilator)
dry eye (a1 stimulation on lacrimal gland)
decreased accommodation (B2 stimulation on ciliary muscle)
eyelid raise (a1 stimulation on Mueller’s muscle)
decreased eye redness (a1 stimulation on vessels)
increased IOP (B1 & B2 stimulation increasing aqueous humor production)
tamsulosin, terazosin, doxazosin, prazosin
alpha blockers
indication: BPH, HTN tx
MoA: inhibits a1
adverse effects:
IFIS
propranolol
non-selective beta blocker
indications: CV disease-HTN, angina, heart failure
MoA: binds & blocks B1, B2
adverse effects:
increased accommodation (B2 blocked on ciliary muscle)
decreased IOP (B1 & B2 blocked on NPCE which decreases aqueous production)
dry eye (lower proteins in lacrimal gland)
contraindications: bradycardia, bronchoconstriction
labetalol, carvedilol
non-selective beta & alpha blockers
indications: CV disease-HTN, angina
MoA: binds & inhibits B1, B2, a1
adverse effects:
miosis (a1 blocked on dilator)
decreased accommodation (B2 blocked on ciliary muscle)
decreased IOP (B1 & B2 block on NPCE ciliary body which decreases aqueous production)
dry eye (lower proteins in lacrimal gland)
contraindications: bradycardia, bronchoconstriction
metoprolol, atenolol
cardio selective beta blockers
indications: CV disease- HTN, angina, arrythmia
MoA: binds & inhibits B1
adverse effects:
decreased eye pressure (B1 blocked on NPCE ciliary body which decreases aqueous production
dry eye (lower proteins in lacrimal gland)
contraindications: bradycardia
succinylcholine
direct acting NMJ desensitizing drug
indication: muscle relaxation/paralysis during surgery
MoA: binds nicotinic receptors in NMJ causing an initial twitch then makes receptor stop working
onabotulinumtoxin A, incobotulinumtoxin A
NMJ indirect antagonist
indication: blepharospasm, strabismus, sweating, wrinkles, HA
MoA: blocks pre-synaptic release of ACh at NMJ which inhibits skeletal muscle contractions
decreased sweating, dry mouth, thirst, tachycardia, blurry vision, urinary retention, hot & dry skin, restlessness, fatigue, rapid/weak pulse, hallucinations, ataxia, delirium, coma
what are the signs of atropine OD?
diarrhea, urination, miosis, bradycardia, emesis, lacrimation, lethargy, salivation
what are the signs of indirect cholinergic agonist OD?
clonidine
centrally acting a2 agonist
indication: HTN
MoA: stimulates a2 receptors in the brain → decreased HR/contraction & vasodilation
adverse effects:
decreased IOP (a2 stimulated on ciliary body which constricts vessels & decreases aqueous humor production)
miosis (a2 stimulated on pre-synaptic neurons of dilator, less NE release, less NE to bind to a1 receptors)
dry eye (anti-cholinergic SE)
stimulation of a2 on ciliary body causes vasoconstriction and decreased aqueous production
describe the MoA of clonidine decreasing IOP
a2 stimulation on presynaptic neurons in iris dilator inhibits NE release & there is less NE available to bind to iris dilator a1 receptors
describe the MoA of clonidine causing miosis
amlodipine, felodipine, nifedipine
dihydropyridine Ca channel blocker
indication: HTN, angina
MoA: inhibit L-type Ca channels → decreases Ca influx into blood vessel smooth muscle → vasodilation
diltiazem, verapamil
non-dihydropyridine Ca channel blocker
indication: HTN, angina, arrythmia
MoA: inhibit L-type Ca channels → decreasing influx of Ca into cardiac cells → decreases HR/contraction
less effective on BV (very slight vasodilation)
watch for pt on these, should not be given further beta blocker drops due to increased risk for bradycardia
hydrochlorothiazide, chlorothiazide, chlorthalidone
thiazide diuretics
indication: HTN, heart failure
MoA: inhibit Na/Cl transporter in DCT → increase Na & H2O excretion → decreased blood volume → decreased BP
adverse effects: idiosyncratic drug rxn (bilateral acute transient myopia & acute angle closure glaucoma), dry eye
furosemide
loop diuretic
indication: HTN, heart failure
MoA: inhibit Na/K/Cl transporter in TAL of LoH → increase Na & H2O excretion → decreased blood volume → decreased BP
adverse effects: idiosyncratic drug rxn (bilateral acute transient myopia & acute angle closure glaucoma), dry eye
spironolactone
potassium sparing diuretic
indication: HTN, heart failure
MoA: inhibit aldosterone’s actions on Na/K/H pump in DCT → increases Na & H2O excretion → decreases blood volume → decreases BP
adverse effects: dry eye
triamterene
potassium sparing diuretic
indication: HTN, heart failure
MoA: directly inhibits Na/K/H pump in DCT → increases Na & H2O excretion → decreases blood volume → decreases BP
adverse effects: dry eye
hydralazine
vasodilator
indication: HTN, angina, heart failure
MoA: unclear
adverse effects: Lupus-like syndrome (w/ photosensitivity), conjunctivitis, tearing
quinapril, captopril, benazepril, lisinopril, enalapril
ACE inhibitors
indication: HTN, heart failure
MoA: inhibits ACE → prevents formation of angiotensin II → vasodilation & Na & H2O excretion → decreased BP
losartan, valsartan
ARBS
indication: HTN
MoA: inhibit angiotensin II from binding to AT1 receptors → vasodilation, increased Na & H2O excretion → decreased BP
nitroglycerin, isosorbide
nitrodilators
indication: angina, heart failure
MoA: turns into NO in body → activates cGMP in blood vessels → blocks Ca entry → strong vasodilation in coronary arteries
digoxin
positive inotrope
indication: heart failure, arrythmias
MoA: inhibits Na/K/ATPase on heart → increases intracellular Ca2+ → increased force of contraction & decreases HR
adverse effects: visual snow, xanthopsia, retrobulbar optic neuritis, flickering lights
amiodarone
K channel blocker
indication: arrhythmia
MoA: blocks K, Na, Ca channels
adverse effects: whorl keratopathy, anterior subcapsular lens deposits and/or cataracts, NAION, torsades des pointes
lidocaine
Na channel blocker
indication: emergency cardiac arrest (arrythmia)
MoA: blocks Na channels
aspirin
anti-platelet
indication: clots
MoA: inhibits cox-1 → inhibits thromboxane A2 → irreversibly inhibits platelet aggregation
adverse effects: subconj heme (easy bleeding)
clopidogrel, ticlopidine
anti-platelet
indication: clots
MoA: inhibits ADP P2Y12 receptors → irreversibly inhibits platelet aggregation
adverse effects: subconj heme (easy bleeding)
dipyridamole, cilostazol
anti-platelet
indication: clots
MoA: inhibits PDE → increases cAMP → inhibits platelet aggregation & adhesion to blood vessel walls & vasodilates coronary arteries
adverse effects: subconj heme (easy bleeding)
warfarin
anti-coagulant
indication: clots
MoA: inhibits vitamin K → decreases production of vitamin K-dependent clotting factors (7, 10, 2, 9) → reduces clot formation
must follow a consistent vitamin K diet, so watch in AMD pt
apixaban, rivaroxaban
direct acting oral anti-coagulants
indication: clots
MoA: directly inhibits factor 10
adverse effects: subconj heme (easy bleeding)
heparin
anti-coagulant
indication: clots
MoA: potentiates anti-thrombin III → inhibits factor 10 & thrombin → inhibits clotting factors
adverse effects: subconj heme (easy bleeding)
protamine
what is the antidote for heparin toxicity?
tissue plasminogen factor
thrombolytic
indication: clots
MoA: convert plasminogen to plasmin → plasmin breaks down fibrin → breaks up clot
aminocaproic acid
what is the antidote to tPA toxicity?
vitamin K
what is the antidote to warfarin toxicity?
lovastatin, simvastatin, atorvastatin, fluvastatin, rosuvastatin, pravastatin
HMG CoA reductase inhibitors
indication: high cholesterol
MoA: inhibits HMG CoA reductase → reduces LDL in liver & pulls more LDL into liver, increases HDL secretion
adverse effects: jaundice/icterus (from hepatotoxicity)
fenofibrate, gemfibrozil
fibric acid derivatives
indication: high cholesterol
MoA: binds & activates PPAR-a → increases lipoprotein lipase activity to breakdown triglycerides & VLDL to be used for energy → decreases amount of VLDL & triglycerides in blood
adverse effects: jaundice/icterus (from hepatotoxicity)
cholestyramine
bile-acid binding resins
indication: high cholesterol
MoA: binds bile acid in gut → prevents chylomicron absorption → chylomicrons excreted in feces
ezetimibe
indication: high cholesterol
MoA: blocks transport of dietary cholesterol in small intestines, so don’t get transport in body
omega-3 acid ethyl esters
indication: high cholesterol
MoA: unknown
decrease triglycerides, may increase LDL
niacin
indication: high cholesterol
MoA: inhibits VLDL formation & secretion in liver → reduces LDL & triglycerides in blood, also increases HDL
adverse effects: jaundice/icterus (from hepatotoxicity), cystoid macular edema
alprazolam, clonazepam, diazepam, lorazepam, midazolam
benzodiazepines
indication: anxiety, sleep disorders
MoA: bind & activate GABA receptor → decreases neurotransmission by opening Cl- channel
adverse effects: anti-cholinergic SE
mydriasis (M3 inhibition at sphincter)
increased IOP (M3 inhibition on ciliary muscle)
reduced accommodation (M3 inhibition on ciliary muscle)
dry eye (M2/3 inhibition on lacrimal gland)
fatal if combined w/ alcohol or opioids
phenobarbital
barbiturate
indication: anxiety, sleep disorders, epilepsy
MoA: binds & activates GABA receptor → decreases neurotransmission by opening Cl- channel
adverse effects: respiratory depression, anti-cholinergic SE
mydriasis (M3 inhibition at sphincter)
increased IOP (M3 inhibition on ciliary muscle)
reduced accommodation (M3 inhibition on ciliary muscle)
dry eye (M2/3 inhibition on lacrimal gland)
fatal if ODed (no antidote), fatal if combined w/ alcohol or opioids
zolpidem, eszopiclone
z drugs
indication: insomnia
MoA: bind & activate GABA receptor → decreases neurotransmission by opening Cl- channel
adverse effects: anti-cholinergic SE
mydriasis (M3 inhibition at sphincter)
increased IOP (M3 inhibition on ciliary muscle)
reduced accommodation (M3 inhibition on ciliary muscle)
dry eye (M2/3 inhibition on lacrimal gland)
diphenhydramine, hydroxyzine, meclizine, promethazine
anti-histamines
indication: mild insomnia, mild anxiety disorders, vomiting, motion sickness, nausea
MoA: inhibits H1 receptors in brain
adverse effects: anti-cholinergic SE
mydriasis (M3 inhibition at sphincter)
increased IOP (M3 inhibition on ciliary muscle)
reduced accommodation (M3 inhibition on ciliary muscle)
dry eye (M2/3 inhibition on lacrimal gland)
melatonin, tasimelteon
melatonin receptor agonists
indication: non-24-hr sleep-wake disorder in total blindness
MoA: stimulate melatonin receptors involved in control of circadian rhythms to promote sleep
phenytoin
indication: epilepsy
MoA: blocks voltage sensitive Na+ channels → decreases firing rate
adverse effects:
nystagmus
diplopia
EOM palsies
divalproex, valproic acid
indication: epilepsy
MoA: inhibits voltage-gated Na channels & T-type Ca2+ channels, enhances GABA by increasing its synthesis & decreasing its breakdown
adverse effects: subconj heme (low platelets)
topiramate
indication: epilepsy, migraines, weight loss
MoA: blocks voltage gated Na channels, GABA agonist, blocks glutamate kainite & AMPA receptors
adverse effects: idiosyncratic drug rxn (bilateral transient myopic shift & bilateral angle closure), nystagmus, diplopia
gabapentin
indication: epilepsy, post-herpetic neuralgia, restless leg syndrome, diabetic neuropathy
MoA: increase GABA release & inhibits L-type Ca2+ channels
pregabalin
indication: epilepsy, diabetic neuropathy, postherpetic neuralgia, restless-leg syndrome
MoA: inhibits voltage-gated Ca2+ channels
nitrous oxide gas
inhaled general anesthetic
indication: surgery
MoA: GABA agonist, Na & Ca inhibition
no respiratory depression
isoflurane
inhaled general anesthetic
indication: surgery
MoA: GABA agonist, Na & Ca inhibition
adverse effects: respiratory depression
midazolam
general anesthetic, parenteral
indication: surgery, cataract surgery
MoA: GABA agonist
respiratory depression
propofol
general anesthetic, parenteral
indication: surgery
MoA: GABA agonist
respiratory depression
haloperidol
typical antipsychotics
indication: schizophrenia, depression, BPD, autism, nausea
MoA: block DA receptor → reduce effects of DA
adverse effects: oculogyric crisis, anti-cholinergic SE
mydriasis (M3 inhibition at sphincter)
increased IOP (M3 inhibition on ciliary muscle)
reduced accommodation (M3 inhibition on ciliary muscle)
dry eye (M2/3 inhibition on lacrimal gland)
thioridazine, chlorpromazine
typical antipsychotics
indication: schizophrenia, depression, BPD, autism, nausea
MoA: block DA receptor → reduce effects of DA
adverse effects: oculogyric crisis, pigmentation on cornea, anterior stellate cataracts, pigment disruption of RPE, anti-cholinergic SE
mydriasis (M3 inhibition at sphincter)
increased IOP (M3 inhibition on ciliary muscle)
reduced accommodation (M3 inhibition on ciliary muscle)
dry eye (M2/3 inhibition on lacrimal gland)
aripiprazole
atypical antipsychotic
indication: schizophrenia, depression, BPD
MoA: block DA receptor → reduce effects of DA
adverse effects: anti-cholinergic SE
mydriasis (M3 inhibition at sphincter)
increased IOP (M3 inhibition on ciliary muscle)
reduced accommodation (M3 inhibition on ciliary muscle)
dry eye (M2/3 inhibition on lacrimal gland)
citalopram, escitalopram, fluoxetine, fluvoxamine, paroxetine, sertraline
SSRIs
indication: affective disorders
MoA: inhibit reuptake of serotonin → increases serotonin in the brain
adverse effects:
serotonin syndrome
subconj heme (due to platelet inhibition)
anti-cholinergic SE
mydriasis (M3 inhibition at sphincter)
increased IOP (M3 inhibition on ciliary muscle)
reduced accommodation (M3 inhibition on ciliary muscle)
dry eye (M2/3 inhibition on lacrimal gland)
mydriasis, mental status changes, increased BP, increased pulse, increase temp, sweating, tremors, hypereflexia
what are the symptoms of serotonin syndrome?
venlafaxine, duloxetine
SNRIs
indication: affective disorders
MoA: inhibit NE & serotonin reuptake → increase NE & serotonin in brain
adverse effects:
serotonin syndrome
subconj heme (due to low platelets)
anti-cholinergic SE
mydriasis (M3 inhibition at sphincter)
increased IOP (M3 inhibition on ciliary muscle)
reduced accommodation (M3 inhibition on ciliary muscle)
dry eye (M2/3 inhibition on lacrimal gland)
amitriptyline, imipramine
TCAs
indication: affective disorders
MoA: inhibit NE & serotonin reuptake → increase NE & serotonin in brain
adverse effects:
OD is fatal
serotonin syndrome
subconj heme (due to low platelets)
STRONG anti-cholinergic SE
mydriasis (M3 inhibition at sphincter)
increased IOP (M3 inhibition on ciliary muscle)
reduced accommodation (M3 inhibition on ciliary muscle)
dry eye (M2/3 inhibition on lacrimal gland)
phenelzine
MAOI
indication: affective disorders
MoA: inhibit monoamine oxidase → increases NE, serotonin, & DA in brain
adverse effects:
excessive HTN can be fatal (if taken w/ tyramine containing food/drinks)
nystagmus
photophobia
STRONG anti-cholinergic SE
mydriasis (a1 stimulation at iris dilator)
increased IOP (M3 inhibition on ciliary muscle)
reduced accommodation (M3 inhibition on ciliary muscle)
dry eye (M2/3 inhibition on lacrimal gland)
bupropion
anti-depressant
indication: affective disorders, smoking cessation
MoA: inhibit NE & DA reuptake → increases NE & DA levels in brain
adverse effects: anti-cholinergic SE
mydriasis (M3 inhibition at sphincter)
increased IOP (M3 inhibition on ciliary muscle)
reduced accommodation (M3 inhibition on ciliary muscle)
dry eye (M2/3 inhibition on lacrimal gland)
mirtazapine
anti-depressant
indication: affective disorders
MoA: uncertain; increases NE & serotonin release & blocks histamine
adverse effects: anti-cholinergic SE
mydriasis (M3 inhibition at sphincter)
increased IOP (M3 inhibition on ciliary muscle)
reduced accommodation (M3 inhibition on ciliary muscle)
dry eye (M2/3 inhibition on lacrimal gland)
trazodone
anti-depressant
indication: affective disorders
MoA: blocks reuptake of serotonin, blocks serotonin from binding to 5HT receptors, blocks histamine from binding to histamine receptors
adverse effects: anti-cholinergic SE
mydriasis (M3 inhibition at sphincter)
increased IOP (M3 inhibition on ciliary muscle)
reduced accommodation (M3 inhibition on ciliary muscle)
dry eye (M2/3 inhibition on lacrimal gland)
lithium
mood stabilizer
indication: mania
MoA: unknown, reduces NE & DA in brain
adverse effects: IIHTN → papilledema
amphetamine, dextroamphetamine, lisdexamphetamine
CNS stimulants, indirect adrenergic agonists
indication: ADHD, narcolepsy, obesity
MoA: enters DA & NE neurons → gets packaged into vesicles with DA & NE → enhances effects of NE & DA
adverse effects:
mydriasis (a1 stimulation on dilator)
dry eye (a1 stimulation on lacrimal gland)
methylphenidate
CNS stimulant, indirect adrenergic agonist
indication: ADHD, narcolepsy, obesity
MoA: inhibits DA & NE reuptake → increasing DA & NE in brain
adverse effects:
mydriasis (a1 stimulation on dilator)
dry eye (a1 stimulation on lacrimal gland)
carbidopa-levodopa
indication: Parkinson’s disease
MoA: increase DA synthesis
adverse effects: mydriasis (a1 stimulation on dilator)
amantadine
indication: Parkinson’s disease
MoA: increases DA release
adverse effects: mydriasis (a1 stimulation on dilator)
bromocriptine
indication: pituitary adenomas
MoA: DA agonist
adverse effects: mydriasis (a1 stimulation on dilator)
donepezil
indirect, reversible cholinergic agonist
indication: Alzheimer’s disease
MoA: inhibits acetylcholinesterase → increases effects of ACh
adverse effects:
miosis (M3 stimulation at sphincter)
tearing (M2/3 stimulation at lacrimal gland)
increased accommodation (M2/3 stimulation at ciliary muscle)
cyclobenzaprine
muscle relaxant
indication: skeletal muscle spasms
MoA: uncertain, increases NE, serotonin, DA & anti-histamine/anti-cholinergic effects in CNS → causes sedation
adverse effects: STRONG anti-cholinergic SE
mydriasis (M3 inhibition at sphincter)
increased IOP (M3 inhibition on ciliary muscle)
reduced accommodation (M3 inhibition on ciliary muscle)
dry eye (M2/3 inhibition on lacrimal gland)
ergotamine
serotonin receptor agonist
indication: migraine
MoA: serotonin 5-HT1 receptor agonist → vasoconstriction, inhibit release of peptides & other pain mediators, inhibit trigeminal nerves
adverse effects:
NAION
retinal artery & vein occlusions
sumatriptan, zolmitriptan
serotonin receptor agonist
indication: migraine
MoA: serotonin 5-HT1 receptor agonist → vasoconstriction, inhibit release of peptides & other pain mediators, inhibit trigeminal nerves
adverse effects:
NAION
retinal artery & vein occlusions
idiosyncratic drug rxn (bilateral transient myopic shift & angle closure)
morphine, meperidine, oxycodone, hydrocodone, fentanyl, codeine
opioids
MoA: full opioid mu receptor agonists
adverse effects:
respiratory depression
miosis (direct stimulation of EW nucleus of CN3 → parasympathetic stimulation of sphincter)
contraindications: alcohol, benzodiazepines, barbiturates, other opioids, muscle relaxants, sleep aids/hypnotics, first gen antihistamines, asthma, COPD, sleep apnea, kidney or liver disease, closed head injury, history of addiction