sketchy pharm Flashcards
What type of receptor is the one for the adrenal medulla?
NICOTINIC acetylcholine (for producing Epi/Norepi and shit)
M1
CNS, Enteric (GI) nervous system—Gq (IP3/DAG)
M2
Heart—namely decreasing (Atria, SA, AV)—it is Gi after all
M3
Glands, bladder, smooth muscles, smooth muscle of eye
Also VESSELS—-causes release of Nitric oxide from endothelial cells and you get more cGMP and muscarinic effects. So you vasodilate
Nicotinic vs Muscarinic receptors
Nicotinic: Ion channels
M1: Gq (IP3/DAG)
M2: Gi (lowering cAMP)
M3: Gq (IP3/DAG)
What happens to M3 in atherosclerosis
the vascular epithelial damage from atherosclerosis stimualtes muscarinic receptors and you get VASOCONSTRICTION (instead of dilation)
Bethanechol
Cholemimetic. Mostly used for secretion and motor activation of gut
(eg neurogenic ileus, post op ileus–NONobstructive GI)
Or to increase urinary secretion (again NONobstructive)
Pilocarpine
Increases salivation
Treat glaucoma (reduce IOP by contracting ciliary body—relaxing it and accomodating lens—so muscle basedi t sounds like)
also causes miosis (activating sphincter pupil muscle in acute angle closure glaucoma)
Carbachol
both muscarinic and nicotinic
Methacholine
muscarinic stimulant; contracts bronchial smooth muscle tree-> exacerbate COPD and asthma
Vareniciline
partial nicotinic agonist used for smoking cessation (provides some degree of stimulation to get rid of craving Im guessing)
Tertiary vs Quatenary Acetylcholine esterase inhibitors and significance
Quatenary can’t cross the BBB (pyrido,neo,edrophonium)
Tertiary can (Physostigmine)
Long term management of MG
Pyridostigmine
Neostigmine less used
Edrophonium for the challenge aka tensilon test
Nondepolarizing neuromuscular blocking agents
curare compounds
tubocurarine, pancuronium, cistracurium
Reverse effects with acetylcholinesterase inhibitors afterwards.
Depolarizing NM block agent
Succinylcholine (doesn’t get metabolized, aggressively binds)—PHASE S1 block of depolarizing blockade. IRREVERSIBLE (cholinesterase inhibitors wont do shit)
phase 2 it will
Neostigmine post surgery
Neostigmine for post op bladder and urinary retention
Physosigmine use
used for atropine overdose (Jimson weed, or belladonna flower)—competitive block so can be overcome
Type of paralysis in acetylcholine esterase inhibitor overdose
flaccid paralysis (BB SLUDGE guy, could be frmo organophosphates for example)
Use of pralidoxime & atropine
regeneration of choline esterase; affects NICOTINIC components, CANT CROSS BBB
Atropine: CAN cross BBB, but can’t affect nicotinic receptors (so can’t affect paralysis)
Why do you need to traet organopsophate-choliensterase complex fast?
“Aging” effect where the bond becomes irreversible
Galnatime, Rivasgmine, Donepezil
all acetylcholinesterase inhibitors that can treat Alzheimers
Antimuscarinic blockers
Atropine Ipratropium Tiotropium Oxybutynin Tolterodine Scoloplamine Benzotropine Trihexylphenidyl obviously side effects for shit like TCAs too
Major side effects of TMP-SMX (or at least unique)
Pancytopenia, megaloblastic anemia, teratagogenic (neural tube defects), interstital nephritis, Renal tubular acidosis (type IV), CYP450 inhibitor, photosensitivity, kernicterus, SJS, hemolytic anemia g6pd
major side effect Ethambutol
optic neuritis (red green colorblindness)
major sideeffect pyrazinamide
tb drug, hyperuricemia
major side effect dapsone
leprosy drug; agranulocytosis, also hemolytic anemia with g6pd
mycobacter avium tx
macrolide and ethambutol
rifampin big side effects
CYP450 inducer, orange red body fluid
isonazide big side effects
b6 deficiency (so give pyrixodine, this is what give hte peripheral neuropathy), worse side effects in slow acetylators, anion gap metabolic acidosis, drug induced lupus, CYP450 inhibitor
rifampin prophylaxis uses
n meningi, h influ
drugs for myco leprae
dapsone, rifampin, maybe add clofazamine if its the major leprosy
major side effects aminoglycoside and major resistance
ototoxicity, nephrotoxicity, ATN, neuromusc blockade (avoid in mg), teratogen (ototoxicity)
resistance is acetylation enzyme
of note it is the only ribosome guy that is bacteriocidal, IV
Linezolid major side effects
neutropenia, serotonin syndrome (minor MAOi effect), optic neuropathy, peripheral neuropathy
major Chloramphenicol side effects
gray baby syndrome, aplastic anemia, regular anemia
marcolide big side effects
cyp450 inhibitor, prolong qt, hepatitis and jaundice
tetracycline big side effects and resistance
resistance: efflux pumps and altering the ribosome
adverse rxn is teeth skin discoloration (binding to calcium, tertaogenic) fanconi syndrome (esp expired tetracyclines; type II renal tubular acidosis)
daptomycin use and major side effects, moa
can use for VRE. Can’t use for pneumonia (surfactant destroys it)
moa is inserting its tail into bacterial cell wall/membrane?
major side effects: myopathy, rhabdomyolysis (monitor CK)
major side effects panems
skin rash, GI, reduce seizure threshold (esp imipeneum with renal failure). good drugs for penicilin allergies
Vancomycin major side effects
red man syndrome (histamine mediated)
can increase risk of ototoxicity with aminoglycosides
thrombophelitis
major side effects griseofulvin, moa
grnaulocytopenia, CYP450 inducer—bind microtubule and halt mitosis.
major side effects Echniocandins (what are these), moa
these are the fungins that alter B2 glucan. ONLY CELL WALL GUYS. adverse rxn is histamine release in IV
teribafine moa, adverse rxn
inhibit fungal sequeale epoxidase, get squalene accumulation (is toxic)
hepatotoxicity
moa major side effects of azoles, what one can you use for PCOS/Cushing/hirsutism shit
inhibit ergesterol synthesis
adverse rxn is CYP450 inhibitor (esp voriconazole, this guy also causes blurry flashes of light and color blindness)
fluconazole is your crypt meningitis guy
voriconazole is your invasive aspergillis and candida esophagitis guy
itraconazole is more systemic dimorphics and tinea
Ketoconazole: Hirsutism guy. inhibits 1720 desmolase (anti androgen effect, 1st step in steroid syn)
major side effects of flouroquinolones, name a use or two
complicated pseudomonas; osteomyeloitis sickle cell, pyelonephritis, anthrax
can fuck up absorption with antacids
adverse: long qt, tendon rupture (kids, elderly, steroids, pregnancy)
major side effect amphotericin
infusion related headache, hypotension, fever, chills, thrombophelitis cns admin (intrathecal): fever, seizure, neuro damage Renal damage (prerenal azotemia, hypokalemic type 1 tubualr injury, can manage with magnesium I think also do volume expansion with saline before admin). anemia from epo issues
Nystatin moa
same as amphotericin; binds to ergesterol and forms pores to induce electrolyte leakage
metronidazole main sx, moa
forms free radicals-> damgae bact dna
disulfram rxn
interferon beta use
relapsing remiting ms
interferon gamma usage
treats CGD, or diseases with deficiecny in it
interferon alpha usage, adverse rxn
hep B and C, hairy cell leuekmia, malig melanoma, Kaposis sarcoma, Condyloma accumuinatica, RENAL CELL CARCINOMA (also in general pegylated version lasts longer)
adverse: myelosuppression, flu symp, tinnitus, mood disorders, drug induced lupus
entry and fusion inhibitors for HIV, names, moa, adverse rxn
maraviroc (block CCR5): so gotta genotype. (gp120)
enfurvitide; binds gp41 (fusion)
Can fuck both thse up with an env mutation (processed in host ER normally)
integrase inhibitors (pol gene)—eg is raltegravir. adverse rxn of rhabdomyolysis. Pol mutation fucks these up (as well as NRTIs, NNRTIs)
Ribavirin moa, adverse rxn
Guanosine nucleoside naalog; needs to be phosphorylated 3 times (inhibits rna activity)
used in HCV with interferon alpha
adverse rxn are dose dependent hmeolytic anemia, tertaogen (must be on contraceptive)
Sineprevir moa, use
NS3,4 protease inhibitors
can be used in HCV
adverse rxn are photosensitivity and cyp450inhibitor
sofosbuvir moa, adverse rnx
direct poylmerase inhibitor; stop NS5B RNA production (I think this is for HCV as well), fatigue, nausea
NRTIs unique side effects, qualities
tenofovir: nucleotide, does not need phosphorylation
stauvidine, lamivudine, zidouvine: lipodystrophy
lamivudine, stavudine, didenosine: periph neuropathy
didenosine: pancreatitis
Abacavir: HLAB57 allele issues (type IV hypersensitivity)
emtricabine: hyperpigmenting palms and soles
Zimivudine is your pregnancy guy, but it also can cause myelosuppression (in addition to lipodystrophy….periph neuropathy
in general names is “-dine”
NNRTIs names and uses, adverse rxn
Efavirenz, Nevirapine, Delavirdine (watch the dine on the last one, I guess it sounds elvish), doesnt need phosphorylation, doesnt incoporate into DNA strand
adverse rxn: liver fialure (often fast within 6 weeks), CNS side effects (weird ones like nightmares and insomnia), tertaogenic
Nevirapine is a CYP450 inducer
Efa nad dela induce and inhibit cyp450
also SJS TEN
Protease inhibitor name, adverse rxn
-navir
adverse rxn: hyperglycemia (insulin resistance), hyperlipiedemia, lipodystrophy, nephrolithiasis (esp indinavir, make sure htey have adequate hydration)
CYP450 inhibition (esp ritonavir, can be used theopetically)
HSV, VZV tx
acyclovir/clovir guys in general.
Cidofuvir does not need phosphorylation
Foscarnet does not need any activaiton (inhibits viral DNA polymerase at pyrophosphate site)
Acyclovir is your only IV guy (so good for encephalitis and neonates)
Adverse rxn acyclovir: interstital nephritis/nephrolithiasis, be sure to hydrate
foscartnet has those hypo
acyclovir adverse rxn (maybe other clovir too)
interstital nephritis/nephrolithiasis, be sure to hydrate, all drugs have CNS side effects
CMV tx
oral vanciclovir/ganciclovir to prevent reactivation in HIV/transplant 9also CMV retinitis concern)
UL97 mutation, use foscarnet (this does first step of phosphorylation normally), cidofovir can be alright too
adverse rxn ganciclovir and valciclovir
myelosuppression
adverse rxn for fascarnet
hypocalcemia, hypomansium, renal toxiciity->hypokalemia, seizures
What do you need to pair cidofovir with
probenicid; block its nephrotoxici effects (blocking the renal secrvetion)
how could you be resistant to foscarnet or cidofovoir
dna polymerase mutation
benzotropine
centrally acting M1 antagonist
scolpamine
m1 antagonist crossing BBB for motion sicknes
antimuscarnic heart effects
block parasymp effects of M2 on SA and AV nodes (increase HR and AV nodal conduction)—so can be useful in heart block (eg atropine)
ipratroprium and tiotropium
M3 antagonists useful in COPD (bronchodilate, decrease secretions). tiotropium is longer lasting, dissociates more slowly
oxybuytin, tolterodine
m3 antagonists use to treat incontinence (specifically urge incontinence htat occurs at night caused by detrusor overstimulation). relaxes smooth muscle in ureter and bladder wall.
trihexyphenidryl, benzotropine
both m1 antagonists; can be used in parkinsons; (excess m1 linked to cog wheel rigidity, again this disease is increased Ach decreased dopamine). can also be used to tx extrapyramidal side effects from antipsychs
antimuscarinic side effects
dry eyes and mouth
inhibit m3 sweat glands-> hyperthermia
blurred vision
acute angle closure glaucoma (due to mydriasis- dilation)
sedation, confusion,agitation, hallucination (m1, esp elderly)
alpha 1 effects
Gq-> so increase IP3 and DAG (more Ca2+)
increase periph art tone (vasoconstrict), also venoconstrict, increase MAP
activate pupillary dilator muscle (pup dilation aka mydriasis)
urethral sphincter, prostatic muscle contraction (urinary retention)
alpha 2 effects
basically decrease sympathetic tone (sympatholytics)
coupled to gi, decrease camp
inhibit NT release
decrease insulin release
inhibit lipolysis and release of fatty acids
decrease aqueous humor production at ciliary body
brimonidine
alpha 2 agonist for open angle glaucoma (decrease AH prod at ciliary body)
beta 1 agonist
Gs->increase cAMP and intracell calcium
SA and AV node: increase cardiac contractility, HR, CO
increase renin release
beta 2 agonists
gs increase camp activate pka
coronary and skeletal muscle VASODILATION, decrease SVR
bronchodilation (look for -rol suffix eg albuterol)
act at ciliary body increase ah production
stimulates lipolysis and release of free fatty acids
increase insulin release (beta 2 islet cells) (can cause hypokalemia as a result)
gluconeogenesis at liver
relax uterine smooth muscle
phenylephrine
alpha 1 agonist
treat nasal congestion (due to vasoconstriction)
increase MAP and systolic pressure (vasoconstrict) and diastolic (venoconstrict)
causes mydriasis
REFLEX BRADYCARDIA
Norepinephrine
alpha agonist and beta 1 (more alpha)
increase map, systolic and diastolic
reflex bradycardia
increase cardiac contractility (beta 1 mediated)
widens pulse pressure (systolic and diastolic increase, but beta 1 makes more systolic)
use for agonists in septic shock
phenylephrine, norepinephrine increase SVR and venosu return
dobutamine
B1>b2
increase HR, cardiac contractility, CO—USE IN CARDIOGENIC SHOCK
moderate vasodilation (beta 2, decrease SVR)
increase systolic pressure (beta1)
decrease diastolic pressure (alpha 2 arterial dilation)
increase in pulse pressure (due to b1 effects)
terbutaline, ritodrine
beta 2 agonist used to relax uterus and prevent premature labor
Epinephrine
beta, alpha activity LOW doses (beta>alpha): bronchodilate (b2), decrease diastolic pressure (b2), increase HR (b1)
HIGH doses (alpha>beta): increase MAP (alpha1) increase systolic pressuer (alpha1), increase pulse pressure (alpha 1 but beta 1 contractility increase) decrease diastolic (beta2)
Great in anaphylactic shock (bronchodilate, increase SVR)
metyrosine
prevent conversion of tyrosine to L-DOPA
cocaine
inhibit NET DAT
agitatino, dilation ,tachycardia, hypertension, mucosal atrophy, myocardial ischemia, coronary vasospasm (and thus angina)
what to avoid in cocaine tx
dont give them a beta blocker (unopposed alpha action), severe hypertension
atomoxetine
ADHD tx (serratra)
reserpine
block VMAT, deplete NT Stores
VMAT
vesicular monoamine transporter; moves catecholamines into presynaptic vesicle
amphetamine
displace catecholamines into synapse
ADHD tx
appetite suppression
modafinil
narcolepsy tx
Dopamine
D1 (Gs), D2 (Gi) low dose D1 increase renal blood flow medium dose: acts on beta 1 to affect cardiac receptors (has those effects of increase contractility, HR, CO) D2 is your cns guy
clonidine
alpha 2 agonist
inhibits symp tone, reduc bp
treats hypertension, hypertensive urgency, can be used for ADHD
alpha methyldopa
a2 agonist
htn tx, ESP GESTATIONAL HTN
tizanidine
a2 agonist
muscle relaxant
phentolamine
reversible alpha 1 and alpha 2 antagonist
vasodilates
cocaine tox, preop pheo
can cause reflex tachy
phenoxybenzamine
IRREVERSIBLE alpha 1 and alpha 2 antaognist
tx for cocaine toxicity (phentolamine probs works too), preop pheo
can cause reflex tachy
-osin suffix
alpha 1 antagonists (prazosin, doxazosin, tamulosin, terazosin)
treat BPH (relax smooth muscle prostate and urethra)
vasodilation
prazosin has unique use in PTSD
mirtazapine
alpha 2 antagonist, atypical antidepression
enhances serotonin release
why beta blockers relieve angina
decrease myocardial oxygen demand (decrease contractility and HR)
beta blockers A-M
more beta1>beta 2, mostly cardioselective
beta blockers and mortality rate
decrease it; dont forget they modify cardiac remodeling effects
carvedilol
beta block and alpha 1 block, also mortality reducing for heart stuff
timolol
beta block for glaucoma; (antagonize beta 2, reduce AH production at ciliary epithelium)
beta block adverse effects
worsen asthma, COPD (esp nonselective N-Z, antagonize bronchodilate)
impotence
heart block
acebutolol, pindolol
a beta 1 antagonist with some agonist activity—avoid in HF patients or MI patients
Hypertensive emergency
labetalol or esmolol
Labetalol
other beta block and alpha 1 block
use to treat HTN in pregnany
good for hypertensive emergency
good for htn in general
unique beta block uses
thyroid storm
migrane prophylaxis
essential tremor
aortic disseciton (including labetolol)
tx beta blocker toxicity
glucagon
fenolodopam
d1 agonist for hypertension
isoproternolol
b1 and b2 agonist for heart block
advantage clonidine and methyldopa for htn
dont reduce kidney blood flow
midodrine
selective alpha 1 guy; good for orthostatic HTN
ephendrine
like amphetamines; release stored catecholamines
nasal decongest, urinary retention, hypotension
