Pharm - Rami Flashcards
penicillin MOA
binds PBPs thereby blocking peptidoglycan cross linking
what 3 penicillins are more susceptible to beta lactamases?
penicillin, ampicillin, piperacillin
general side effect of penicillins
allergic reaction
side effect of penicillin
drug induced coombs positive hemolytic anemia
drugs that cause drug induced coombs positive hemolytic anemia
penicillin, alpha methyldopa, and cephalosporins
side effect of ampicillin/amoxicillin
non-allergenic skin rash
side effect of methicillin
interstitial nephritis
drugs that cause interstitial nephritis
methicillin, NSAIDs, furosemide (“buy meth in dollars instead of euros”)
what form is pen V given
oral
what form is pen G given
IV
aztreonam structure
monocyclic beta lactam ring
blocks peptidoglycan cross-linking as well
why give aztreonam
renally insufficient patient;
allergic to penicillin
side effect of aztreonam
elevated LFTs
imipenem side effect
seizures in renally impaired patients
what do you give with imipenem
cilastin - inhibits renal dihydropeptidase I (enzyme that inactivates drug in renal tubules)
antibiotic you do not want to give to renally insufficient patient that aztreonam might be great for
aminoglycosides
gen 1 cephalosporins
gram positive
CEFAZOLIN, CEPHALEXIN
gen 2 cephalosporins
gram positive, anaerobes, H flu
CEFACLOR, CEFUROXIME
gen 3 cephalosporins
gram negative
CEFTRIAXONE
gen 4 cephalosporins
gram positive and negative
pseudomonas, CEFEPIME
gen 5 cephalosporins
MRSA,
CEFTAROLINE
cephalosporin side effects
hypersensitivity reaction (10% of patients with penicillin allergy with be allergic),
disulfiram-like reaction,
nephrotoxicity
drugs that cause disulfiram like reactions
“Sorry pals, can’t go mingle”
1st gen sulfonylureas, procarbazine, cephalosporins, griseofulvin. metronidazole
50S inhibitors
"50 cent - I'm a CMLC" chloramphenicol, macrolides, linezolid, clindamycin,
30S inhibitors
aminoglycosides,
tetracyclines
chloramphenicol MOA
reversibly binds 50S to inhibit peptidyl transferase
clindamycin MOA
inhibits formation of initiation complex
aminoglycosides MOA
inhibits formation of initiation complex and causes mRNA misreading
tetracyclines MOA
blocks AMINOACYL tRNA from binding to the ribosome
chloramphenicol side effects
aplastic anemia,
gray baby syndrome (vomiting, flaccidity, gray skin hue, shock in newborns due to lack of UDP-glucuronyl transferase in liver)
drugs that cause aplastic anemia
"Cant Make New Blood Cells Properly" (carbamazepine, methimazole, NSAIDs, benzene, chloramphenicol, PTU)
side effects of macrolides
erythromycin, clarithromycin, azithromycin
acute cholestatic hepatitis (jaundice)
uses of clindamycin
anaerobic infections above the diaphragm
side effects of clindamycin
pseudomembranous colitis (c. diff)
linezolid treats…
VRE, MRSA
VRE: vancomycin resistant enterococcus
uses of metronidazole
anaerobic infections below the diaphragm
side effects of aminoglycosides
nephrotoxicity (especially with cephalosporin),
ototoxicity (especially with loop diuretic),
teratogenicity
aminoglycosides are ineffective against…
anaerobes because they require oxygen to be taken up into bacterial cells
tetracycline side effects
teeth discoloration, bone deformity in kids, fanconi syndrome (aminoaciduria, phosphaturia, acidosis, glycosuria), photosensitivity
how is doxycycline eliminated
fecally –>
so it can be used in renally insufficient patients
uses of demeclocycline
treats SIADH (competitive antagonist at V2 receptor)
name all of the anti mycobacterial agents
rifampin, isoniazid pyrazinamide ethambutol dapsone
rifampin MOA
inhibits bacterial DNA-dependent RNA polymerase
side effects of rifampin
orange urine, hepatitis
isoniazid MOA
inhibits synthesis of mycolic acids
side effects of isoniazid
peripheral neuropathy (due to Vitamin B6 depletion),
G6PD-hemolytic anemia,
drug induced lupus,
hepatitis
dapsone MOA
PABA antagonist, inhibits folic acid synthesis
dapsone side effects
G6PD hemolytic anemia
ethambutol MOA
inhibits mycobacterial arabinosyl transferase
ethambutol side effects
retrobulbar neuritis (decreased visual acuity and red green color blindness)
pyrazinamide side effects
hepatotoxicity,
hyperuricemia (gout)
drugs that are hepatotoxic
“Patron is FIRSt fun, then hepatotoxic”
pyrazinamide, fibrates, isoniazid, rifampin, statins,
drugs that cause SLE like syndrome
“Having lupus is Mega SHIPP-E”
methyldopa, sulfa, hydralazine, isoniazid, procainamide, phenytoin, etanercept
drugs that cause hyperuricemia/gout
“Painful Tophi in Feet Need Care”
pyrazinamide, thiazide, furosemide, niacin, cyclosporine
drugs that cause G6PD hemolytic anemia
“Hemolysis IS D PAIN”
isoniazid, sulfonamides, dapsone, primaquine, aspirin, ibuprofen, nitrofurantoin
isoniazid causes peripheral neuropathy because…
it depletes the body of vitamin B6
trimethoprim- sulfamethoxazole MOA
DNA synthesis disruption
trimeth - blocks dihydrofolate reductase
sulfameth - blocks dihydropteroate synthase
bactrim (TMP-SMX) side effects
stevens johnson syndrome,
hemolytic anemia,
kernicterus in newborns,
(BAK)
sulfa drugs
“Popular FACTSSS”
probenecid, furosemide, acetazolamide, celecoxib, thiazides, sulfonamide antibiotics, sulfasalazine, sulfonylureas
fluoroquinolones MOA
inhibits bacterial DNA topoisomerase II –>
DNA strand breaks –> cell death
fluoroquinolones side effects
tendonitis,
tendon rupture,
contraindicated in pregnant women and kids (damages cartilage)
fluoroquinolones coverage
gram negative
vancomycin MOA
binds D-ala D-ala, inhibits transglycosylase, weakens cell wall and causes cell lysis
vancomycin uses
MRSA, C. diff pseudomembranous colitis orally
side effects of vancomycin
“NOT” + red man
nephrotoxicity,
ototoxicity,
thrombophlebitis,
and red man syndrome
side effects of metronidazole
metallic taste,
disulfiram-like rxn
nucleoside reverse transcriptase inhibitors
zidovudine,
didanosine,
lamivudine,
abacavir
non nucleoside reverse transcriptase inhibitors
nevirapine,
efavirenz,
delavirdine
NRTI side effects
zidovudine - megaloblastic anemia
didanosine - pancreatitis
NNRTI side effects
efavirenz - CNS disturbances
nevirapine - stevens johnson syndrome, hepatitis
what NRTI is used on pregnant women?
zidovudine
what is the suffix of the protease inhibitors
-navir
MOA of protease inhibitors
inhibit HIV protease enzyme
side effects of protease inhibitors
altered distribution of fat (buffalo hump, increased truncal obesity), insulin resistance = hyperlipidemia, neuropathy
what disease causes buffalo hump
cushing syndrome (increased cortisol)
what drug besides protease inhibitors leads to fat redistribution
glucocorticoids (fat PIG)
acyclovir MOA
phosphorylated by viral thymidine kinase into analog of dGTP (inhibits DNA synthesis)
acyclovir side effects
neurotoxicity (tremor, delirium),
nephrotoxicity
ganciclovir MOA
inhibit CMV DNA polymerase,
especially useful for CMV retinitis
“I Gan Ci”
amantidine MOA
binds M2 surface protein on influenza A, blocking uncoating of viral RNA,
can also stimulate release of dopamine from neurons of nigra striatum
amantidine side effect
CNS symptoms
zanamivir MOA
inhibits neuraminidase,
treats influenza A and B
ribavirin MOA
inhibits viral RNA polymerase –> inhibits viral replication
ribavirin side effect
teratogenicity
Contraindicated in pregnancy, and in renally insufficient patients
amphotericin MOA
tears holes,
binds ergosterol,
alters permeability of fungal cell membrane,
leads to cell death
amphotericin side effects
“Ampho-Terrible”
infusion related reaction,
nephrotoxicity
does amphotericin cross the BBB
no
flucytosine MOA
inhibits thymidylate synthease - inhibits fungal DNA and RNA synthesis
flucytosine side effect
bone marrow suppression
caspofungin MOA
inhibits B(1,3)-D-glucan synthase
β(1,3)-d-glucan is an essential component of the fungal cell wall
griseofulvin MOA
interferes with microtubule formation and inhibits fungal cell replication
name an allylamine and the enzyme it blocks
terbinafine,
blocks squalene epoxidase,
tx: onychomycosis
what enzyme do azoles block
lanosterol 14 alpha demethylase
ketoconazole, miconazole, clotrimazole side effect
gynecomastia (because they disrupt gonadal and adrenal steroid synthesis)
can be used to treat cushing syndrome because of this
quinine side effects
cinchonism (tinnitus, headache, dizziness, nausea)
coombs positive hemolytic anemia
fetal toxicity
mefloquine side effect
mental status change
primaquine side effects
G6PD hemolytic anemia,
fetal toxicity
alpha 1 receptor secondary messenger
PLC,
increased IP3 and DAG –>
increased intracellular calcium
alpha 2 and D2 secondary messenger
Gi - inhibition of AC leads to decreased cAMP
beta 1 and 2 and D1 secondary messenger
Gs - AC activation leading to increased cAMP
direct sympathomimetics - uses
emergency shock,
anaphylaxis
(fast decrease in BP)
epinephrine - receptors
alpha agonist at high doses,
beta agonist at low doses
uses of epinephrine
anaphylaxis,
bronchospasm
epinephrine SE
hypertension,
pulmonary edema
norepinephrine - receptors
alpha 1, alpha 2, beta 1 (increased contractility)
dopamine - receptors
alpha agonist at high doses
beta agonist at low doses
D1 agonist at even lower doses
dobutamine - receptors
beta 1 agonist
selective = B for BRAT
uses of dobutamine
cardiac stress test,
cardiogenic shock
side effect of dobutamine
hypotension (via rebound)
direct sympathomimetics
“Duplicate sympathetic END point”
dobutamine,
epinephrine,
norepinephrine,
dopamine
indirect sympathomimetics - stimulate the release of…
direct sympathomimetics
ephedrine stimulates release of…
norepinephrine,
also stimulates beta 2 receptors and the CNS
effect of ephedrine
increased contractility (same as NE), bronchodilation (beta 2)
uses of ephedrine
nasal decongestant (pseudoephedrine),
athletic enhancement drug
(since it is a CNS stimulant)
cocaine MOA
blocks Na/K ATPase pump responsible for reuptake of NE, serotonin, and dopamine
results in euphoria, vasoconstriction
also blocks voltage-gated Na channels
results in anesthesia
cocaine side effects
hypertension,
cardiac ischemia,
cardiac arrhythmias
indirect sympathomimetics
amphetamines,
cocaine,
ephedrine
use of phenylephrine
mydriasis (eye exam)
“would you like me to dilate your Pupils?”
phenylephrine MOA
alpha 1 agonist
midodrine MOA
alpha 1 agonist
midodrine uses
used in patients with advanced hepatic disease,
orthostatic hypotension
Think: Me go faint & M1dodr1ne
side effect of midodrine
supine hypertension
clonidine uses
treats hypertension by inhibiting release of sympathetic neurotransmitters
clonidine side effect
rebound hypertension if withdrawn quickly
Think: “Clonidine clones itself” - goes from treating HTN to causing it!
clonidine MOA
alpha 2 agonist
isoproterenol uses
treats torsades de pointes (long QT) - given with magnesium for this,
can also treat cardiac arrest/heart block
isoproterenol MOA
beta 1 and 2 agonist
fenoldopam use
produces renal vasodilation for severe hypertension
albuterol uses
produces bronchodilation (treats asthma), treats hyperkalemia by causing transcellular shift of K into the cell
beta 2 agonists
“Beta 2 agonist needed for SAT-induced asthma!”
salmeterol,
albuterol,
terbutaline,
salmeterol uses
long acting treatment for COPD and asthma;
used with inhaled corticosteroids
analogue of albuterol
terbutaline MOA
beta 2 agonist;
relaxes smooth muscle in lungs and uterus
by directly-acting on the receptor
terbutaline use
delay preterm labor by reducing uterine contractions
Think: “TERM-butaline”
side effects of terbutaline
tachycardia,
tremor
methyldopa MOA
alpha 2 agonist
methyldopa uses
treats moderate hypertension
using adrenergic neurotransmitters
methyldopa side effects
positive coombs test,
orthostatic hypotension
phenoxybenzamine MOA
irreversible alpha receptor antagonist
phenoxybenzamine side effect
inhibition of ejaculation
phenoxybenzamine use
treats pheochromocytoma
both are 16 letters
phentolamine MOA
SHORT-ACTING
reversible alpha receptor antagonist
phentolamine use
diagnose pheochromocytoma
prazosin (-zosin) and tamulosin MOA
selective alpha 1 antagonist
prazosin (-zosin) and tamulosin uses
decrease prostatic and bladder neck contraction,
decrease blood pressure,
treatment for hypertension and BPH
prazosin (-zosin) and tamulosin side effect
first dose syncope (severe orthostatic hypotension –> syncope)
timolol MOA
beta 1 and 2 antagonist
timolol uses
ophthalmic solution - decreases aqueous humor secretion;
used to treat glaucoma
pindolol MOA
weak beta receptor agonist,
beta receptor antagonist,
intrinsic sympathomimetic properties
pindolol uses
treats: HTN, bradycardia
propranolol MOA
beta 1 and 2 antagonist
propranolol uses
tachycardia associated with hyperthyroidism and chronic migraines
side effects of propranolol
bronchoconstriction, fasting hypoglycemia (decreased glycogenolysis)
esmolol MOA
short acting beta 1 antagonist
“es small” = short acting
esmolol uses
treats critically ill patients with arrhythmias, hypertension, and MI
carvedilol MOA
alpha 1 and beta receptor blocker
carvedilol uses
decreases HR and contractility;
bronchoconstriction,
treats CHF (given with ACEi and diuretics),
treats hypertension
metoprolol MOA
selective beta 1 antagonist
metoprolol uses
decreases HR and contractility,
treats hypertension, tachycardias, CAD, especially in patients with diabetes
M1 and M3 receptors
Gq (increased IP3 and DAG –> increased intracellular calcium)
(same mechanism as alpha1 from adrenergics)
M2 receptor
Gi (AC is inhibited –> decreased cAMP),
also an increase in K+ conductance
same mechanism as alpha2 from adrenergics
Nm and Nn
activation of Na/K channels
pilocarpine and carbachol uses
applied topically to eye (ophthalmic solution);
treats glaucoma;
Think: piloCRYpine and CRYbachol
pilocarpine/carbachol MOA
M3 muscarinic agonist
methacholine uses
bronchial challenge test (inhalation);
diagnoses asthma
methacholine MOA
smooth muscle contraction of bronchi,
M1, M2, M3 muscarinic agonist (*use targets M3)
methacholine side effects
bradycardia, hypotension;
minimally seen because it is inhaled
bethanechol MOA
M2, M3 agonist (use related to M3)
bethanechol uses
promotes urination,
treats neurogenic ileus (urinary retention), especially postpartum or postop
bethanechol side effect
diarrhea
M3 agonists (3 of them)
pilocarpine,
methacholine,
bethanechol
atropine MOA
competitive M1-M3 antagonist
atropine use
antidote for cholinesterase inhibitor poisoning (nerve gas, insecticide)
treatment for atropine poisoning
physostigmine
cholinesterase inhibitor
atropine side effects
characteristic of muscarinic block:
hyperthermia (flushing), decreased salivation, cycloplegia (blurred vision), psychosis, tachycardia
tropicamide and homatropine uses
ophthalmic solutions,
retinal examinations,
temporary cycloplegia and mydriasis
tropicamide and homatropine MOA
atropine analogs,
antimuscarinic M1-M3
benztropine MOA
M1-M3 antagonist, M1 receptors (brain) in corpus striatum (PD)
benztropine use
treats parkinson’s by improving tremor and rigidity;
no effect on bradykinesia
benztropine contraindication
patients with glaucoma
scopolamine MOA
competitive M1-M3 antagonist;
action at MI for usage
scopolamine use
treats motion sickness,
crosses BBB to interact between vestibular ear and vomiting center of brain
think: “scopukeamine”
ipratropium MOA
M3 receptor antagonist
ipratropium uses
inhaled form causes bronchodilation;
treats COPD and asthma
(especially in those who are unable to take adrenergic agents)
think: “i pray to breathe”
oxybutynin MOA
M1-M3 receptor antagonist (action at M3)
oxybutynin uses
treats urinary incontinence and hyperhidrosis
cholinesterase inhibitors (anticholinesterases) have what effects
parasympathetic/muscarinic,
increased ACh
neostigmine MOA
reversibly inhibits acetylcholinesterase,
increased stimulation of nicotinic and muscarinic receptors
does neostigmine cross the BBB
no
neostigmine uses
treats myasthenia gravis,
overcomes nondepolarizing neuromuscular blockade (caused by pancuronium or vecuronium)
physostigmine MOA
reversibly inhibits Acetylcholinesterase
does physostigmine cross BBB
yes - used as antidote for atropine overdose
uses of physostigmine
antidote for atropine overdose,
ophthalmic solution - treats glaucoma
edrophonium and pyridostigmine MOA
reversibly inhibit Acetycholinesterase –>
increased stimulation of both nicotinic and muscarinic receptors
edrophonium use
diagnosis of myasthenia gravis (short acting)
think: “a drop lasts a moment, but a stigma lasts forever”
pyridostigmine use
treats myasthenia gravis (long acting)
tacrine MOA
reversibly inhibits AChE –>
increased stimulation of both nicotinic and muscarinic receptors
tacrine use
treats alzheimers
Think: “Tacrine (taking) care of Alzheimer’s patients”
tacrine side effect
hepatotoxicity
drugs similar to tacrine
Think: “Tacrine RDG”
rivastigmine,
donezepil,
galantamine,
echothiophate MOA
inhibits AChE by covalently binding to the enzyme –>
increased stimulation of both nicotinic and muscarinic receptors
drugs similar to echothiophate
isoflurophate,
malathion,
parathion
think: “echothiophate - IMP”
echothiophate and isoflurophate use
ophthalmic ointments, treat glaucoma (M3)
side effects of echothiophate
seizures, bradycardia, flaccid paralysis, and muscarinic activation SEs
due to persistent nicotinic activation resulting in NM blockade - depolarizing)
echothiophate overdose treatment
atropine,
pralidozime
pralidoxime MOA
cholinesterase reactivator,
reverses cholinesterase inhibitor binding to AChE
(so it opposes acetylcholinesterase inhibitors)
pralidoxime effects are similar to what other drug
atropine
pralidoxime uses
used with atropine to treat nerve gas or organophosphate poisoning,
treats overdose of neostigmine or pyridostigmine
hexamethonium, mecamylamine, trimethphan MOA
competitive inhibition of Nn receptors on postsynaptic neurons of autonomic ganglia,
block outflow to sympathetic and parasympathetic neurons,
anti-nicotinic
hexamethonium use
treats hypertensive emergencies
hexamethonium side effect
hypotension
how long does it take for antidepressants to work
3-4 weeks
SSRIs
fluoxetine, fluvoxamine, paroxetine, escitalopram, citalopram, sertraline
Think: “Fun Fabulous PECS”
SSRI uses
treat depression and OCD
SSRI side effect
sexual dysfunction
SSRIs and MAOIs cannot be given together due to
serotonin syndrome - changes in mental status, muscle stiffness, autonomic instability, hyperthermia
fluoxetine inhibits what enzyme
cytochrome P450
TCAs
Think: “ANTI-Depressant”
amitriptyline, nortriptyline, trazodone (tetracyclic anti depressant or SARI), imipramine, doxepin
TCA MOA
block norepinephrine and serotonin reuptake,
also inhibit muscarinic, histamine, and alpha adrenergic receptors (side effects)
TCA uses
treats depression, enuresis (bed wetting), chronic pain syndromes
given together, TCAs and MAOIs cause
seizures
trazodone use
insomnia
think: “trazodone makes you zone out”
trazodone side effect
priapism
prolonged erection
amitriptyline use
neuropathic pain
think: “am i tripping?”
imipramine use
enuresis
think: “promise me to stop wetting the bed”
buproprion use
smoking cessation,
anti-depressant
histamine blockade
sedation
adrenergic blockade
postural hypotension, cardiac arrhythmias
muscarinic blockade
urinary retention,
blurred vision,
constipation,
dry mouth
heterocyclic anti depressants
nefazodone,
venlafaxine,
mitrazapine,
maprotiline
think: “NVM, Man”
nefazodone, venlafaxine, maprotiline MOA
block reuptake of norepinephrine and serotonin
mirtazapine MOA
inhibits activation at alpha 2 adrenergic receptors and at 5HT2 receptors,
increases release of NE and serotonin
mirtazapine side effects
sedation,
increased appetite,
weight gain
venlafaxine side effects
elevated BP and HR
MAOIs
tranylcypromine,
isocarboxazid,
phenelizine
think: “MAO TIP”
MAOa
NE and serotonin
MAOb
dopamine
MAOI use
atypical depression
side effect of MAOI
cheese effect:
MAO metabolizes tyramine- increased tyramine stimulates release of epi and NE
causes hypertensive crisis (HA, HTN, cardiac arrhythmias)
avoid tyramine-containing foods
selegiline MOA and use
MAOI for MAOb (dopamine),
treats parkinsons with levodopa,
and major depressive disorder
lithium use
bipolar disorder
lithium side effects
tremor,
hypothyroidism,
nephrogenic diabetes insipidus (ADH antagonism),
teratogen
drugs that cause hypothyroidism
lithium,
amiodarone,
sulfonamide
think: “LASs with hypothyroidism”
drugs that cause nephrogenic diabetes insipidus
lithium,
demeclocycline
typical antipsychotics MOA
block dopamine D2 receptors,
inhibit histamine, cholinergic, and alpha adrenergic receptors
typical antipsychotics
fluphenazine,
thioridazine,
chlorpromazine,
haloperidol
think: “antipsychotics For Typical, Crazy, Humans”
typical antipsychotics side effects
galactorrhea and amenorrhea (due to hyperprolactinemia),
neuroleptic malignant syndrome,
blockade symptoms,
extrapyramidal side effects
think: typicals treat tourette’s syndrome
typical antipsychotics are effective against
positive symptoms
antidote for neuroleptic malignant syndrome
dantrolene (muscle relaxant)
atypical antipsychotics
olanzapine, clozapine, quetiapine, risperidone, aripiprazole, ziprasidone,
think: (its) ATYPICAL (for) OLd CLOSets (to) QUIETly RISPER (from) A (to) Z.
atypical antipsychotic MOA
blocks serotonin and dopamine receptors
side effects of atypical antipsychotics
mild weight gain,
parkinsonism
atypical antipsychotics treat what symptoms
positive and negative
clozapine side effects
leukopenia,
agranulocytosis
drugs that cause agranulocytosis
ganciclovir, clozapine, carbamazepine, colchicine, methimazole, PTU
think: “Gangs CCCrush Myeloblasts and Promyelocytes”
benzodiazepines (-lam, -pam, chlordiazepoxide) MOA
enhances GABAa activity, increased chloride ion influx, hyperpolarization, decreased CNS neuronal activity
benzo uses
anxiety, seizures, status epilepticus, alcohol withdrawal,
midazolam and diazepam are anesthetics
treatment for benzo overdose
flumazenil
competitive antagonist of benzodiazepines
barbiturates uses
thiopental - induction of anesthesia,
phenobarbital - management of seizures, treats neonatal hyperbilirubinemia
CC: crigler najjar syndrome
congenital syndrome where babies have difficulty conjugating bilirubin;
jaundice, encephalopathy
zolpidem use
short term tx for insomnia
think: “Zolpidem for Zzz”
zolpidem MOA
binds GABAa like benzos
zolpidem side effects
mild anterograde amnesia,
hallucinations
phenytoin MOA
decrease flow of Na and Ca ions
phenytoin uses
anti-epileptic,
partial seizures,
status epilepticus,
phenytoin side effects
nystagmus,
gingival hyperplasia,
drug-induced lupus,
teratogen (fetal hydantoin syndrome)
drugs that cause drug induced lupus (SHIPP-E)
sulfa, hydralazine, isoniazid, procainamide, phenytoin, etanercept
lamotrigine MOA
blocks fast voltage activated Na channels;
anti-epileptic
lamotrigine side effect
stevens johnson syndrome
drugs that cause stevens johnson syndrome
sulfa,
penicillin,
allopurinol,
lamotrigine
valproic acid uses
mania,
seizures
valproic acid side effects
hepatotoxic,
teratogen (neural tube defects)
ethosuximide use
treats absence seizures
think: “it sux to be absent”
MOA: is not well-understood
carbamazepine MOA
inhibits flow of Na ions
carbamazepine uses
first line for simple seizures, complex partial seizures, generalized tonic-clonic seizures (grand mal),
treats trigeminal neuralgia
topiramate uses
migraines, seizures
think: “top of head hurts”
topiramate MOA
inhibits Na ion flow
tiagabine MOA
inhibits reuptake of GABA
tiagabine use
partial seizures as adjunct tx
vigabatrin MOA
irreversibly inhibts GABA transaminase
vigabatrin uses
infantile spasm in kids,
refractory complex partial seizures
think: “Vi-GABA-trin - “Visual” - “GABA transaminase”
side effects of vigabatrin
visual field constriction, visual loss in 30% of patients
levetiracetam uses
anti-epileptic, treats neuropathic pain
side effects of levetiracetam
drowsiness, depression
succinylcholine MOA
depolarizing neuromuscular blocker, competes with ACh to reversibly bind to nicotinic receptors
continuous depolarization at NMJ leads to fasciculations and eventual desensitization (NM blockade)
succinylcholine antidote
physostigmine
cholinesterase inhibitor
succinylcholine use
muscle paralysis for endotracheal intubation
succinylcholine contraindicated with halothane because
malignant hyperthermia (antidote = dantrolene)
pancuronium MOA
non-depolarizing neuromuscular blocker,
does not activate nicotinic receptor but just blocks ACh binding to it,
no skeletal muscle contraction can occur
pancuronium antidote
neostigmine
cholinesterase inhibitors
pancuronium use
adjunct to general anesthesia induction
ester local anesthetics duration of action
shorter than amides
side effects of local anesthetics
seizures
general inhaled anesthetics (-fluranes and halothane) uses
GA induction and maintenance
inhaled general anesthetic side effects
myocardial/respiratory depression,
halothane - fulminant hepatic necrosis,
methoxyflurane/enflurane - nephrotoxic
drugs that cause fulminant hepatic necrosis (HAVAc)
halothane,
amanita phalloides (death cap mushroom),
valproic acid,
acetaminophen
think: “Liver HAVAc”
bupivacaine side effects
myocardial depression,
hypotension
IV general anesthetics
propofol, etomidate, ketamine, benzos, barbiturates
propofol uses and side effect
induction and maintenance of GA
conscious sedation;
hypotension
etomidate MOA and use
prolongs GABA activity;
induction of anesthesia and conscious sedation
ketamine MOA and side effects
NMDA receptor antagonist; decrease neuronal conduction
hallucinations, cardiac and resp depression
uses of codeine and dextromethorphan
cough suppressant
butorphanol
opioid agonist and antagonist (mixed)
treats pain, manages migraines via intranasal formulation
tramadol
opioid agonist,
moderate to severe pain,
side effect is seizures
dantrolene MOA
inhibits calcium release from SR of myocytes to relax muscle –>
muscle relaxants
dantrolene uses
malignant hyperthermia;
neuroleptic malignant syndrome
dantrolene side effect
hepatotoxic
levodopa crosses the BBB and then becomes
dopamine
levodopa use
first line tx for parkinsonism
levodopa side effects
dyskinesia, cardiac arrhythmias
levodopa is given with
carbidopa,
carbidopa inhibits dopa-decarboxylase peripherally so levodopa can act on the brain
sumatriptan MOA
stimulates presynaptic serotonin receptors –> inhibits vasodilation and inflammation of dura
sumatriptan uses
treats migraines and cluster headaches
sumatriptan side effect
coronary vasospasm (CI in CAD patients)
memantine MOA
NMDA antagonist
memantine use
moderate to severe alzheimers
buproprion MOA
inhibits reuptake of NE and dopamine,
nicotinic antagonist
buproprion side effects
psychosis, seizures, dry mouth
varenicline MOA
partial agonist and antagonist (mixed) at a4B2 nicotinic ACh receptors in the brain
varenicline use and side effect
smoking cessation,
suicidal ideation
pregabalin (lyrica) uses
treats neuropathic pain and fibromyalgia
gabapentin (neurontin) MOA
GABA analog
gabapentin uses
treats postherpetic neuralgia, neuropathic pain, partial seizures
gabapentin side effect
peripheral edema
buspirone MOA
acts on 5-HT1a as partial agonist
buspirone use
treats anxiety when used with SSRIs
goals of treating systolic heart failure
increase contractility - inotropes (dobutamine, milrinone), digoxin,
optimize HR - beta blockers,
optimize preload - diuretics, venodilators,
reduce afterload - arteriolar vasodilators, mixed vasodilators
which phases of the cardiac myocyte action potential are missing from the SA node action potential?
phase 1 and 2
cardiac myocyte depolarizaton occurs with what ion
Na
SA node depolarization occurs with what ion
Ca
class IA anti arrhythmics
disopyramide,
quinidine,
procainamide
think: “Double Quarter Pounder”
class IA anti arrhythmic MOA
block activated Na channels (phase 0 depol prolonged, phase 3 repol prolonged)
prolonged QT interval
class IB anti arrhythmics
lidocaine,
tocainide,
mexiletine
think: “lettuce tomato mayo”
class IB anti arrhythmic MOA
block activated and inactivated Na channels (phase 3 repol shortened along with AP)
shortened QT interval
class IC anti arrhythmics
encainide,
flecainide,
propafenone
think: “extra fries please!”
class IC anti arrhythmic MOA
block flow of Na inside;
phase 0 depol prolonged
class III anti arrhythmics
bretylium -- amiodarone, ibutilide, dofetilide, sotalol
think: “Band-AIDS”
class III anti arrhythmic MOA
block flow of K channels out;
phase 3 repol prolonged (and AP)
prolonged QT interval
class IV anti arrhythmics
verapamil,
diltiazem
class IV anti arrhythmic MOA
block voltage gates Ca channels in SA and AV nodes;
slow phase 4 spontaneous depolarization
class I, 3, 4 - assoc. ions
class I - Na, class III - K, class IV - Ca
class IA anti arrhythmic uses
WPW syndrome,
a fib,
v tach
class IB anti arrhythmic uses
v tach,
v fib
class IC anti arrhythmic uses
supraventricular arrythmias (a fib)
class III anti arrhythmic uses
-tilides –> atrial arrhythmias,
sotalol and amiodarone –> atrial and ventricular arrhythmias
class IV anti arrhythmic uses
supraventricular tachycardia (a fib), also treat hypertension and angina
quinidine side effect
cinchonism (vertigo, headache, tinnitus, psychosis)
class IA anti-arrhythmic
procainamide side effect
drug induced lupus
class IA anti-arrhythmic
disopyramide side effects
urinary retention,
double vision,
constipation
class IA anti-arrhythmic
amiodarone side effects
pulmonary fibrosis, hepatotoxicity, thyroid dysfunction, cardiac arrhythmias, ataxia, photosensitivity
class III anti-arrhythmic; but has class I-IV actions
class IA and class III common side effect
torsades de pointes (prolonged QT interval, type of v tach)
how to treat torsades de pointes
isoproterenol and magnesium
adenosine use
anti arrhythmic used for cardiac stress testing
potassium uses
anti arrhythmic,
suppresses ectopic pacemakers,
treats digoxin toxicity
magnesium uses
anti arrhythmic,
treats torsades de pointes and digoxin toxicity
nitroglycerin use
treats angina
nitroglycerin MOA
–> becomes nitric oxide –>
smooth muscle relaxation of veins,
decreases preload (venous return)
nitroglycerin side effect
hypotension
nitroprusside MOA
mixed vasodilator,
smooth muscle relaxation of peripheral veins and arteries,
decreased preload (venous return) and afterload (blood pressure)
use of nitroprusside
treats hypertensive crisis
side effect of nitroprusside
cyanide toxicity (adminster nitroprusside IV)
uses of ACEi and ARBs
treat hypertension and CHF,
treat and prevent diabetic nephropathy
side effects of ACEi
cough,
angioedema
due to increased active bradykinin levels, while ARBs do not, since they simply block the angiotensin II receptor without inhibiting ACE
hydralazine MOA
direct relaxation of arteriolar smooth muscle;
arteriolar vasodilators
uses of hydralazine
hypertension,
heart failure,
decreases afterload,
first line treatment of hypertension in pregnancy
side effect of hydralazine
drug induced lupus
minoxidil MOA and use
arteriolar vasodilators,
anti hypertensive agent,
opens K channels in smooth muscle,
also used for hair growth
CCB use
treats hypertension,
verapamil and diltiazem treat supraventricular tachycardia
CCBs
nifedipine, diltiazem, verapamil, amlodipine, nicardipine
think: “ND VAN”
May need CCBs after eating at the ND VAN
side effect of amlodipine
peripheral edema
side effects of CCBs
hypotension,
heart block
carbonic anhydrase inhibitor
acetazolamide
osmotic diuretics
glycerin,
mannitol,
urea,
isosorbide
think: “GUMI”
loop diuretics
furosemide,
bumetanide,
ethacrynic acid
torsemide
think: “F BEaTs”
thiazide diuretics
metolazone,
indapamide,
thiazide,
thalidone
think: “MITT”
K sparing diuretics
aldosterone receptor antagonists- spironolactone, eplerenone,
Na channel blockers - triamterene, amiloride
carbonic anhydrase inhibitors act at which part of the nephron
PCT
think: “PaCeTazolamide”
osmotic diuretics act at which part of the nephron
thin descending loop of henle
think: “osmosis jones is a tall, thin man (mannitol)”
carbonic anhydrase inhibitors MOA
inhibit carbonic anhydrase,
less bicarbonate reabsorbed,
more Na lost in tubular lumen,
carbonic anhydrase also in the eye - involved in production of aqueous humor
carbonic anhydrase inhibitors uses
treats glaucoma,
alkalinize the urine,
prophylaxis for high altitude sickness
uses of osmotic diuretics
decrease intracranial or intraocular pressure
uses of loop diuretics
for volume overload states,
hypertension,
hypercalcemia (excretes calcium)
uses of thiazide diuretics
first line for hypertension,
nephrogenic diabetes insipidus,
recurrent kidney calcium stones (spares calcium) - decreased excretion of calcium
MOA of K sparing diuretics
Na channel blockers - spare K by specifically blocking Na channels;
aldosterone receptor antagonists - competitive
carbonic anhydrase inhibitor side effects
hyperchloremic metabolic acidosis,
hypokalemia,
neuropathy,
sulfa allergy
osmotic diuretics side effects
pulmonary edema,
contraindicated in CHF patients
loop diuretic side effects
ototoxicity,
hyperuricemia,
sulfa allergy (give ethacrynic acid instead),
hypokalemia
thiazide diuretics side effects
hyperuricemia, hypokalemia, hyperglycemia, hyperlipidemia, hypercalcemia, metabolic alkalosis, hypersensitivity reactions
Na channel blocker K sparing diuretic side effect
hyperkalemia
aldosterone receptor antagonist K sparing diuretic side effects
hyperkalemia,
gynecomastia (anti- androgen effect with spironolactone)
phosphodiesterase inhibitors
sildenafil (viagra),
milrinone
sildenafil MOA
selectively inhibits cGMP-specific PDE type 5 found in corpus cavernosum of the penis and smooth muscle of pulmonary vasculature
think: “sildenafive for type 5”
sildenafil uses
treats erectile dysfunction and pulmonary arterial hypertension
milrinone MOA
inhibits PDE type 3 (increased cAMP, open calcium channels, increased contractility)
milrinone use
treats acute decompensated heart failure
side effects of milrinone
nausea, thrombocytopenia
nesiritide MOA
synthetic human B type natriuretic peptide (hBNP),
binds guanylate cyclase - increased cGMP, smooth muscle relaxation, reduced preload and afterload
nesiritide use
treats acute decompensated heart failure
nesiritide side effect
hypotension
digoxin (cardiac glycoside - others are digitoxin and ouabain) MOA
inhibits Na/K pump - increased intracellular Na, decreased activity of Na/Ca exchanger, increased intracellular Ca, increased contractility
digoxin use
treats heart failure
digoxin side effects
GI upset,
blurry, yellow vision,
ECG changes (prolonged PR, decreased QT, ST segment scooping, T wave inversion),
increase in parasympathetic flow
digoxin side effects are made worse by:
hypokalemia (digoxin and K compete for binding site to ATPase),
quinidine (displaces digoxin from binding sites on albumin and increases serum levels of digoxin)
heparin MOA
activates antithrombin III,
short half life,
rapid onset
LMWHs (low molecular weight heparin)
(enoxaparin, dalteparin) duration of action
longer than heparin,
need less frequent dosing
warfarin MOA
inhibits vitamin K dependent g-carboxylation of factors 2, 7, 9, 10, protein C and protein S;
long half life,
slow onset
direct thrombin inhibitors (argatroban) MOA
directly inhibit thrombin
-rudin, -gatroban, & -gatran
fondaparinux MOA
accelerate selective action of antithrombin III by inhibiting factor Xa
does fondaparinux have HIT has a side effect?
Heparin Induced Thrombocytopenia (HIT)
no
because Fondaparinux is selective –> doesn’t have HIT as a side-effect
rivaroxaban MOA
direct inhibition of factor Xa
what do you give to a patient that is allergic to heparin?
fondaparinux or rivaroxaban
heparin uses
acute DVT,
pulmonary embolism
warfarin use
chronic anticoagulation
direct thrombin inhibitors (argatroban) uses
acute and chronic anticoagulation
argatroban use
treats HIT
bivalirudin use
treats acute coronary syndromes during cardiac catheterization
can be used by patients allergic to heparin
fondaparinux uses
acute DVT,
pulmonary embolism
rivaroxaban uses
DVT prophylaxis,
prevent thromboembolism in patients with A Fib
can be used by patients allergic to heparin
heparin side effects
bleeding (give protamine sulfate),
HIT
warfarin side effects
bleeding,
teratogen
aspirin MOA
irreversibly inhibits COX 1 and 2 to decrease prostaglandin synthesis –>
TXA2 inhibition provides decreased platelet aggregation
clopidogrel/prasurgel MOA
irreversibly inhibits binding of ADP to platelet P2Y receptor, blocking ADP mediated platelet aggregation;
no fibrinogen interaction with platelets so no platelet plug
cilostazol MOA
inhibits cAMP phosphodiesterase III;
inhibits TXA2 which decreases platelet aggregation
prasugrel is the same
dipyridamole MOA
inhibits uptake of adenosine into platelets,
inhibits platelet aggregation and thrombus formation
promotes vasodilation,
inhibits cGMP PDE
abciximab MOA
binds GP IIb/IIIa receptor complex,
inhibits binding of fibrinogen and vWF to the receptor
no platelet aggregation
think: “ABC it’s easy as GP-2,3”
aspirin overdose can lead to
respiratory or metabolic acidosis (must alkalinize urine to promote excretion - give sodium bicarbonate)
ticagrelor MOA
reversible allosteric inhibitor of P2Y12 receptor,
no platelet plug
aspirin indications
many uses, pain, fever, antiplatelet, antiinflammatory
clopidrogel uses
acute coronary syndrome (with aspirin),
patients undergoing placement of a coronary stent
prasugrel is the same
cilostazol use
claudication
dipyridamole uses
cardiac stress test,
used with aspirin for stroke prevention
abciximab use
acute coronary syndrome
aspirin side effects
bleeding in GI tract,
gastric ulcers/gastritis,
reye’s syndrome (fatal liver failure in kids with viral infections),
tinnitus
ticlopidine side effects
bleeding,
neutropenia,
thrombocytopenic purpura
prasugrel side effect
thrombocytopenic purpura
cilostazol side effects
headache,
palpitations
dipyridamole side effects
hypotension,
hepatotoxicity
abciximab side effects
bleeding,
thrombocytopenia,
diffuse alveolar hemorrhage
fibrinolytic agents
streptokinase,
urokinase,
alteplase,
reteplase
fibrinolytic agents MOA
promote conversion of plasminogen to plasmin
fibrinolytic agents indications
massive pulmonary embolism,
stroke,
acute MI,
most effective when given early on
fibrinolytic agents side effect
bleeding
aminocaproic acid (tranexamic acid) MOA
inhibits plasminogen activation,
inhibition of fibrinolysis,
promotes clotting
aminocaproic acid use
treats bleeding
aminocaproic acid side effect
thrombosis
synthetic erythropoietin (epoetin, darbepoetin) MOA
stimulates bone marrow to enhance erythroid proliferation and differentiation,
increases hematocrit
epoetin use
treats anemia
epoetin side effects
CV events and thrombotic complications,
teratogen
epoetin contraindications
renal patients
how is insulin secreted?
glucose enters cell, metabolizes to ATP, ATP binds K channel and closes it so K cannot flow out of the cell, depolarization, calcium release intracellularly, promotes exocytosis of insulin
thiazolidinediones (-glitazone) MOA
bind to PPAR-g which upregulates genes that lead to decrease in insulin resistance
rosiglitazone side effect
heart attacks
troglitazone side effect
liver damage
pioglitazone side effect
bladder cancer
thiazolidinediones (-glitazone) general side effects
edema, hypoglycemia
sulfonylureas MOA
inhibit K channel on beta cells
chlorpropamide side effect
disulfiram like reaction with alcohol
sulfonylurea general side effect
hypoglycemia
contraindication for sulfonylureas
pregnancy
1st generation sulfonylureas
chlorpropamide,
tolbutamide,
tolazamide
2nd generation sulfonylureas
glyburide,
glipizide
3rd generation sulfonylureas
glimepiride
think: M3
alpha glucosidase inhibitors (acarbose and miglitol) MOA
inhibt alpha glucosidase which breaks down carbs into monosaccharides for absorption (no more absorption of glucose)
acarbose and miglitol side effects
GI upset (flatulence, diarrhea)
metformin uses
diabetes,
treats polycystic ovarian syndrome (PCOS)
does metformin cause hypoglycemia?
no
metformin side effects
GI upset,
lactic acidosis
metformin contraindication
renal patients (this is how it is excreted)
metformin MOA
inhibits hepatic gluconeogenesis and helps make beta cells work better
(improves insulin sensitivity)
meglitinides (-glinide) - ex. repaglinide MOA
bind K channel (different channel from sulfonylureas but same effect essentially)
meglitinides side effects
weight gain,
hypoglycemia
DPP-4 inhibitors (sitagliptin, saxagliptin) MOA
DPP-4 degrades GLP-1,
GLP-1 increases insulin and decreases glucagon secretion,
inhibition of DPP-4 allows for more GLP-1 action
DPP-4 inhibitors side effect
nausea/vomiting
GLP-1 analogs (exenatide, liraglutide) MOA
mimic GLP-1 –> increase insulin and decrease glucagon secretion
GLP-1 analog side effects
pancreatitis,
hypoglycemia,
weight loss
bile acid resins
cholestyramine,
colestipol,
colesevelam
bile acid resins MOA
inhibit reabsorption of bile acids in jejunum and ileum,
decreases LDL levels
bile acid resins side effects
GI upset,
decreased fat soluble vitamin absorption (ADEK) and folic acid
statins MOA
HMG-coA reductase inhibitors,
decrease total cholesterol and LDL levels
statins side effects
myopathy,
abnormal LFTs
niacin MOA
increases HDL levels
niacin side effects
flushing (give aspirin to decrease),
hyperuricemia
fibrates (gemfibrozil, -fibrates) MOA
stimulates lipoprotein lipase (breaks down TG into VLDL and chylomicrons which are then removed from circulation),
decreases TG levels
fibrates side effect
gallstone formation
ezetimibe MOA
decreases absorption of cholesterol in small intestine,
decreases serum LDL
ezetimibe use
adjunct for hypercholesterolemia
ezetimibe side effects
steatorrhea (diarrhea),
myalgia,
elevated LFT
levothyroxine MOA
synthetic T4
think: “LeFOURthyroxine”
levothyroxine uses
hypothyroidism,
goiters (thyroid cancer) by suppressing TSH secretion
PTU and methamizole MOA
inhibit thyroid peroxidase,
inhibition of thyroid hormone synthesis and peripheral conversion of T4 to T3
PTU and methamizole use
hyperthyroidism
PTU and methamizole side effects
hepatotoxicity,
rash,
methamizole also is teratogen
symptoms of hyperthyroidism
tachycardia,
weight loss,
diarrhea
symptoms of hypothyroidism
bradycardia,
weight gain,
constipation
where is T4 secreted from?
follicular cells of the thyroid gland
prednisone (synthetic corticosteroid) MOA
synthetic glucocorticoids that mimic the action of endogenous glucocorticoids
prednisone uses
adrenocortical insufficiency, IBD, allergic reactions, SLE, RA, diagnosis of cushing's syndrome, immunosuppression in organ transplants
prednisone side effects
symptoms of cushing syndrome (osteoporosis, hyperglycemia, fat redistribution - buffalo hump and moon facies),
impaired wound healing
how do we diagnose cushing’s syndrome?
dexamethasone suppression test
beclomethasone use
inhaled corticosteroid used to treat chronic asthma
think: “B for Bronchial asthma and Beclomethasone”
bisphosphonates (-onate) - ex. alendronate MOA
decrease osteoclastic bone reabsorption