DIT Drugs and UWorld Drugs Flashcards
How symp drugs work
short preganglionic - AcH, long postganglionic - NE (into SC - then to multiple organs at once) NE R = Adrenergic R’s
A1
“aggressive alpha 1”
vascular smooth muscle contraction
Inc TPR/BP/bladder sphincter contraction, mydriasis
A2
Negative feedback of NE (onto presynaptic R)
Found: B cells (pancreas), some smooth muscle
decrease NE/insulin release
Tx - some HTN
B1
“think heart increase”
Tachycardia / Inc HR / Inc myocardial contract
B2
“Dilate everything!”
vasodilation (w resulting inc HR), bronchodilation
dec uterine tone
1 R type predominates body location:
vascular smooth muscle, heart, lungs
VSM: B2 > A1
Heart: B1
Lungs: B2
Sympathomimetics - Direct/Indirect
Direct - bind adrenergic R
Indirect - release of catecholamines from presynaptic
- inhibit uptake of catecholamines
E, NE, Albuterol/Levalbuterol/Salmeterol, DA, Dobutamine, Phenylephrine, Terbutaline
Epinephrine
Direct
A1, A2, B1, B2
Tx: anaphylaxis, severe croup, hypotension
NE
Direct
A1, A2, B1
Tx: hypotension, (#1 for) septic/cardiogenic shock (stop vasodilation)
Albuterol/Levalbuterol/Salemterol
Direct
B2 (strong), weak B1
asthma
DA
Direct
low dose - blood vessels, kidneys
med dose - B1, B2
high dose - A1, A2 “aggressive alpha”
Dobutamine
Direct
B1 > B2
stress test
tx: HF
Phenylephrine
Direct
A1 > A2
Pupillary dilation
Tx: Nasal decongestion
Terbutaline
Direct
B2 (strong), weak B1
(sometimes given subQ for asthma)
tx: bronchospasm, tocolysis (stop premature uterine contraction)
Amphetamines
Indirect - release cats
tx: narcolepsy, obesity, ADHD
Ephedrine
Indirect - release cats
tx: oral and nasal decongestion, urinary incontinence
Cocaine
Indirect - inhibit reuptake of cats
tx: ENT nasal decongestion, local anesthetic
Isoproterenol
B1, B2
Causes:
-increase CO
-increase dilation (decrease vascular resistance)
Clonidine
Direct
A2
tx: malignant HTN, sedative
SFx = sudden stop - rebound HTN
Sympathetic blockers
A nonselective, A1 selective, B nonselective, B1 selective, B1B2 weak agonists, A1/B1 blockers
Prazosin, Doxazosin, Terazosin
A1 selective blocker
tx: BPH (#1), HTN
Sfx: Postural hypotension, Reflex tachycardia,
Rebound HTN
Tamsulosin
A1(A,D) selective blocker (R only found in prostate)
tx: BPH without HTN
Phenoxybutamine (irrev binds), Phentolamine
non-selective A-blocker
tx: acute pheochromcytoma
Propanolol, Timolol, Nadolol
nonselective B blocker
Timolol, Nadolol (topical) - tx: Glaucoma
Propanolol - anxiety
Metoprolol, Atenolol, Esmolol, Nebivolol
Selective B1
(N)ebivolol - (N)O action, vasodilation of the periphery
Acebutolol, Pindolol
Weak B1B2 agonists (so weak = blockers)
treat patients with HTN + bradycardia
Carvedilol, Labetalol
A1/B1 blockers
tx: HTN + tachycardia
B blocker uses
HTN, CHF?, angina, MI, coronary artery disease, hyperthyroidism, thyroid storm, migraine prophylaxis, anxiety, SVT, glaucoma (vs aqueous humor),
- *Tx Aortic Dissection (dec HTN and BP pulse)
- don’t give to CHF exacerbation patients
- don’t give for cocaine OD pts
B blocker SFx
Bronchospasm - asthma/COPD
Block hypoglycemic Sx - DM
Increase BP - cocaine user
Decrease myocardial contractility, AV block, bradycardia - CHF
abrupt stop: rebound tachycardia, rebound HTN, arrhythmia
*does not cause ED
A-methyldopa
tx: pregnancy induced HTN
Hemicholinium
Inhibit choline into pre-synapse for Ach
Vesamicol
Inhibit choline acetyltransferase / packaging
Black widow spider toxic
causes Ach release - spastic paralysis
Botulinum toxin
inhibits Ach release - flaccid paralysis (top down)
Metyrosine
Inhibits Tyrosine hydroxylase
Guanethidine, Bretylium (K+chan blocker vs arrhythmia)
Blocks NE release
Amphetamines, Ephedrine, Tyramine
causes NE release
Cocaine, TCAs, SNRIs
inhibit NE reuptake
ex: Amitriptyline (TCA)
Angiotensin R
causes NE release via presynaptic R
A2 agonist, M2 agonist
inhibits NE release via presynaptic R
Reserpine
inhibits NE packaging
Acetazolimide
tx: idiopathic intracranial hypertension, glaucoma, altitude sickness
Fomepizole
Inhibits - Alcohol dehydrogenase
Cure for methanol and ethylene glycol poisioning
Methanol is converted to formaldehyde (metabolic acidosis, retinal damage, blindness)
Ethylene glycol -> oxalic acid (metabolic acidosis, kidney dmg due to oxalate stones, CNS, heart, lung)
Disulfram
inhibits - acetylaldehyde dehydrogenase
Stop alcoholics from drinking (hypotension, flush, sweat, headache, n/v)
Disfulfram-like reactions
metronidazole some cephalosporins sulfonureals procarbazine (CA drug to treat HL) **avoid alcohol while taking
P450 inducers
Guiness, Corona, PRBrs induce Chronic alcoholism
P450 inhibitors
CRACK AMIGOS
Treat acidic drug OD with…?
NaCO3 -> traps acidic drug (as proton) in urine
ex: salicylates) (ex: ASA - a weak acid
Treat basic drug OD with…?
NH4Cl -> traps basic drug (as proton) in urine
ex: amphetamines - a weak base
Indomethacin
Treat PDA (blocks PG synthesis)
Anti-arrhythmics: overall mnemonic
"No Bad Boy KeepsClean" C1 = Na blockers mnemonic C2 = B-blockers "-olol" C3 = K blockers *other* C4 = Ca channel blockers "only 2 D/V"
AA - C1 - Na channel blockers - mnemonic
“Double Quarter Pounder, Mayo, Lettuce, Tomato, Fries, Please
myocytes, Phase 0, inc EPR and inc QT interval
1A: disopyramide, quinidine (SFx cinchonism, thrombocytopenia, torsades), procainamide (WPW, SFx SHIPP)
1B: mexiletine, tocainide, lidocaine (tx: acute VTach, digitalis arrhythmias, tachys-post MI)
1C: flecainide, propafenone (tx: VTach going to AFib, SFx: pro-arrhythmogenic)
AA - C2 - B blockers
“-olol”
mech: dec cAMP, dec calcium currents
pacemaker cells, decrease phase 4 slope
propranolol, esmolol, metoprolol, atenolol, timolol
Tx: VTach, SVT, A-fib/A-flutter
SFx: exac CHF/asthma, bradycardia, AV block, mask hypoglycemia
Tx OD -olol = glycogen
AA - C3 - K blockers
phase 3, inc ERP, in QT interval
sotalol, ibutilide, bretylium, dofetilide, amiodarone
Tx: rhythmic control w/ AFib
SFx: Torsades
Amiodarone SFx: “check PFTs (pulm fibrosis), LFTs (hepatotoxicity), TFTs (drug is 40% iodine), sight (SAT for photo), CV
AA - C4 - CCB
pacemaker cells, phase 0, inc ERP
2 types CCB: (not here = dihydropyridine)
here: non-dihydropyridine (heart)
verapamil, diltiazem
SFx: flushing, edema, CV: sinus node depression, ablocks, HF, torsades
be careful mixing with giving to HF pts -> H block
Adenosine – anti-arrhythmic
increase K efflux (keep baseline/hyperpolarize)
Tx: SVT
SFx/toxic: flushing, hypotension, chest pain
toxic tx: theophylline (3rd line asthma tx)
Digitalis toxic tx
optimize K (4), Mg (2-nrm lvl) (Mg also for torsades)
Methotrexate
inhibits dihydrofolate reductase
Tx: Cancers: leukemias (ALL), lymphomas, choriocarcinoma, sarcomas. Non-neoplastic: ectopic pregnancy, medical abortion (with misoprostol), rheumatoid arthritis, psoriasis, IBD, vasculitis.
SFx: Myelosuppression, which is reversible with leucovorin “rescue.” Hepatotoxicity. Mucositis (eg, mouth ulcers). Pulmonary fibrosis.
Drugs that prolong QT
macrolides, chloroquine haloperidol, risperidone methadone -navirs (anti-protease HIV) antiarrhythmics: Class 1A, Class 3
N-Acetylcysteine
acetaminophen OD
mucolytic (intubated pts)
prevent contrast neuropathy
Cholinergic Direct Agonists (bind musc R) - Parasympathetic activation (receptor 2)
"-chol" bethenachol - urinary retention carbachol - glaucoma pilocarpine - sweat, tear, saliva methacholine - asthma Dx test bc causes bronchospasm
Cholinergic Indirect Agonists (anti-acetylcholinesterases)
“-stigmine”
neogstigmine - postop, urinary retention
edrophonium - myasthenia gravis Dx test (auto-Ab)
pyridostigmine - LT MG tx
physostigmine - antichol or atropine toxicity
echothiophate - glaucoma
donepezil - AD
AD drugs - mnemonic
“Grandma Can’t Remember”
galatamine, donepezil, rivastigmine
Cholinergic direct antagonists (competitive inhibitors) (muscarinic R 2 antagonists)
atropine - bradycardia, organophosphate poisoning
tropicamide “topical” - pupil dilation/mydriasis
benztropine - PD, decrease anti-psych SFx
glycopyrrolate - dec mucosal secretions (anesthesia)
hyoscyamine, dicyclome - “help digest”, antispasmotics vs IBS
scopolamine - motion sickness, dec secretions
ipratropium, triotropium - bronchodilators
“triumph” = bronchod”i”la”t”or
*psych drugs have anticholinergic effects (benadry, TCA) + amandadine
Regenerate AchE
parlidoxine
anticholinergics for urge urinary incontinence - mnemonic
"Off The Darn Toilet Seat" oxybutynin tolterodine darifenacin trospium solifenacin
atropine
tx - bradycardia, organophosphate poisoning
- don’t give to BPH, hyperthermic, GI obstruction, Eldery
- *never acute angle glaucoma
tacrolimus, pimecrolimus
calcineurin inhibitors
inhibits secretion of IL-2 and other cytokines
result: blocks T-cell activation and B-cell differentiation
Skin tx - Vit A derivatives “noin”
hyperkeratosis
skin tx sebum overproduction
isotretinonin, spironolactone, OCPs
skin tx P acnes
abx - “mycin” “cyclin”, benzoylperoxide
Danazol
synthetic androgen - neg feedback to AP and hypothal, dec FSH and LH
tx - endometriosis, fibrocystic breast Dz, hereditary angioedema
Sfx - masculine effects
leuprolide
mech: GnRH analog - continued use (non-pulsatile) causes neg feedback AP = dec FSH, LH
tx: leiomyomas, endometriosis, central precocious puberty, advanced prostate CA, infertility
Tertbutaline
tocayltic, asthma, secretions destroy
selective B2 agonist - also found in uterus, causes muscle to relax
mifepristone (RU-486) and Methotrexate
Progestin R antagonist, Glucocorticoid antagonist
abortion -necrosis of the uterine decidua
give with misoprostol
MTX - used for abortion of ectopic pregnancy - folic acid antagonist
misoprostol
prostaglandin E1 agonist
causes cervical softening and uterine contractions
(early - abortion, late - induce labor)
Tamoxifen
SERM
Estrogen R antagonist - breast tissue
agoinst - endometrial tissue (CA risk)
Raloxifine
SERM
estrogen antagonist - breast (*no risk endometrial CA)
agonist at bone (vs osteoporosis)
Paget Dz of breast
see eczema on areola
HISTO - dark nuclei with perinuclear clearing “halo”
invasive lobular carcinoma
ER + PR +
signet ring cells, cells line up in single lines
inactivation of e-cadherin genes
invasive ductal CA
immobile, firm, hard
HISTO: “stellate” star-like border tumor
DCIS
eventually malignant/met
includes paget dz of breast
LCIS
signet ring cells
ER+ PR+
DONT HAVE TO TAKE OUT - low malignancy
phyllodes tumor
“leaf-like” HISTO
large, bulky
cromolyn
block mast cell degranulation
Filgrastin, Sargrastim
granulocyte stimulating factors
Rx INF alpha
tx: genitar warts, hep b and c, kaposisarcoma, hairy cell leukemia, melanoma
Rx INF B
tx MS
Rx INF y
chronic granulomatis Dz
stimulate macrophages to make NADPH oxidase
cyclosporin
binds cyclophilins in cytosol of T cells complex inhibits calcineurin -> no IL 2 Result: Blocks T-cell activation Tx - AI Ds (psoriasis, RA) Sfx - nephrotoxicity
tracolimus, primecrolimus
mech: bind FK binding prs -> dec calcineuria -> dec IL2
Sfx - hepatotoxicity
azathioprine
precursor 6-mercaptopurine
mech - interfere with synth of nucleic acids
Tx -txx, RA, AI dz
Sfx - metabolized by xanthine oxidase (don’t give to allopurinol pts), BM suppression
infliximab/adaliximab
bind TNF a
tx: seronegative spondylosying arthropathires
PAIR
enterecept
vs TNF a receptor
Rituximab
bind CD20 on b cells, lyse them
tx - NHL (most b cell)
omalizumab
vs IgE
tx - severe asthma pts
abliximab
vs IIbIIIa R on platelets
tx - angioplasty, stent, MI
trastuzimab
vs ERBB2 (HER2/neu) breast CA
sirolimus
binds FK binding pr-12 -> inhibits mTOR
blocks T cell response to IL 2
Sfx - NO nephrotoxicity
mycophenolate
inhibits inosine monophosphate dehydrogenase
-> inhibits guanine synthesis -> prev lymphocyte proliferation
tx - txx, SLE
sfx - teratogenic, HTN, high sugar, lymphoma
thalidomide
mech - suppress TNF a production, increases NK and IL2 –NK kills cells
tx - Hansen dz, multiple myeloma
sfx: phocomelia - teratogent
SJS -Rx SFx
Steve Jobs made APPLE PCs
Allopurinol Penicillin Phenytoin Lamotrigine Ethosuximide
Phenobarbital
Carbamazepine
Phenytoin SFx
"Phenytoin Has Given MDs Frustration" Hirisitism Gingival hyperplasia Megaloblastic anemia SJS Fetal hydentoin syndrome
+SHIPP
Rx that cause agranulocytosis
"C's" carbamazepine clozapine colchicine PTU miconazole
Haptotixic antiepileptics
valproic acid
carbamazepine
anti-seizure drugs
Block Na+ channels
phenytoin carbamazepine lamotrigine topirimate valproic
anti-seizure drugs
increase GABA activity
“barbital”
valproic acid
benzodiazepine
gabapentin
anti-seizure drugs
block T-type Ca2+ channels
gabapentin
ethosuximide
phenytoin
Levadopa / Carbidopa
Levadopa - cross BBB, precursor DA
Sfx - DA in periphery (HTN, hallucinations)
Carbidopa - stops peripheral conversion Levadopa
Other Rx to increase DA - BALSA
bromocriptine - inc DA and BP
Amantadine - enhance edogenous DA (& dec tremor)
Levodopa/Carbidopa
Selegiline - vs COMT/MAOB
**treat MPTP exposure
antimuscarinic (bc PD has inc Ach) - benztropine/trihexyphenidyl
dantrolene
blocks RYR
no Ca2+ release from sarcoplasmic ret.
Tx - malignant hyperthermia (+succinyl choline)
Insomnia tx melatonin antihistamines antidepressents benzos zolpidem, zalepon eszopiclone ramelteon orexin R antagonists
melatonin antihistamines antidepressents benzos zolpidem, zalepon - sfx - sleep walk eszopiclone - sleep maintenance ramelteon orexin R antagonists - block RAS
narcolepsy, cataplexy tx
suppress REM
fluoxetine, venlafaxine, atomoxetine
Sleep stages:
including old and depressed pts
awake - open eyes = alpha, closed eyes = beta
N1 = theta
N2 = sleep spindles, k complexes
N3 = delta waves (sleep walk, night terrors, bed wet)
-decrease with benzos/alcohol
REM = beta waves, REM bc PPRF
old:
dec N3, dec REM, inc REM latency
depressed:
dec N3, inc REM, dec REM latency
Restless leg syndrome - check what major lab?
**check iron levels!!!
pramiprexole, porimvole
Inhaled anesthetics:
factors that effect potency
drugs
lipid soluble - increase = cross BBB = inc potency
blood soluble - dec = inc potency
Minimum alveolar concentration - MAC
-amt to get 50% pain response
NO: Low blood, low blood (rapid)
Halothane: hepatotoxicity
Sevoflurane, desflurane: low blood, high lipid #1 used
Isoflurane: mod blood, mod soluble
IV anesthetics: Propofol Ketamine Barbiturates Benzodiazepines Opioids
= sedation hypnotics, NO ANALGESIA
Propofol -inc GABA, fast, high triglyceride content
Ketamine - dissociative anesthetic, hallucinations, increase cerebral blood flow
Barbiturates
-“tol” “ital”
“don’t want to the bars to close early, less lines (CSF)”
work on GABA, Cl- channels =inc duration open
decreases cerebral BF (brain Sxx - Thiopental)
-phenobarbital = inc liver enzyme tx Crigler-Najjar
Benzodiazepines "azalam" "azapram" inc frq Cl- channels open midazolam - short procedures, conscious sedation chloridazopoxide - tx alcoholism *safe than Barbs Tx OD - flumazenil
Opioids - analgesia
mu - beta endorphin
delta - encephalin
kappa - dynorphin
1 - non-depolarizing competitive inhibitors nicotinic Ach Receptors, can reverse with ChE inhibitor
“curium” “curonium” “curarine”
2 - Depolarizing (binds Ach R, initial muscle but none after)
*succinylcholine
phase 1 - rapid onset/recovery, no reversal
phase 2 - large dose, can be reversed
**succinylcholine + inhaled anesthetic in RYR1 MT pt = malignant hyperthermia == TX with Dantrolene!
SFx succinylchole:
Brady or tachycardia
malignant hyperthermia
severe hyperkalemia
Local anesthetic
block Na+ channels
lidocaine
1 - worse with acid/inf
2 - small myelinated (sensory) > small unmyelinated (SNS) > large myelinated (motor)
size most important factor
3 - give with local vasoconstrictor (Epi)
-dec blood out, dec blood take away (not at closed areas*)
PD tx - direct agonists
bromocriptine - ergot derivative, inc DA and BP
sooo, give… nonergot derivatives
pramipexole and ropinirole
Nitrates
isosorbid dinitrate
tx - sx relief angina
sfx - headaches, cutaneous flushing, hypotension
DONT Give To: HCM, RVentricular infarct, PDE inhibs
Primary pulmonary HTN tx
Bonsentan (-sentan),
PG - prost
sildenafil
nifedipine (smooth muscle relaxor bc gene MT GMBRT MT proliferation of smooth muscle)
Theophylline
=methylxanthine like caffeine
Sfx - seizures and tachyarrythmias
antidote - charcoal, BB (arrhythmias), Benzodiazepines for seizures
Decrease cardiac demand in pt having an MI - Tx (3)
NO - reduce preload
ACEI/ARB - reduce afterload
BB - dec heart contractility
Digoxin - mechs of action
1 - direct inhibitor Na/K ATPase -> dec Na/Ca exchanger
2 - Inc intracellular Ca -> positive inotropy
3 - Stimulates vagus nerve -> dec HR
Used for VFib bc it decrease AV nodal conduction
