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182 Cards in this Set

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Aspirin:
NSAID. tox: GI bleed/ulcer/perf, asthma, Reye's syn.
Ibuprofen:
NSAID. tox: GI bleed/ulcer/perf. Propionic acid class.
Naproxen:
NSAID. tox: GI bleed/ulcer/perf. Propionic acid class.
Indomethacin:
NSAID. tox: GI bleed/ulcer/perf. Acetic acid class.
Celecoxib:
Cox2 inh. tox: Inc stroke/MI.
Misoprostol:
PGE1 analog. Vasodilator. Abortifacient. Cytoprotective (NSAIDs).
Etanercept:
TNFa inh. Recomb TNFR. RA. also binds TNF-B
SE: potential activ of latent TB (true of all TNF-a inhibitors)
Infliximab:
TNFa inh. mouse TNFa Ab. RA, Crohn's.
Adalimumab:
fully humanized anti TNFa mAb. RA
Anakinra:
recombinant human IL1 R
Methotrexate:
dihydrofolate reductase inh. S-phase-specific antimetabolite. RA, cancer.
Levodopa:
dopamine precursor
Carbidopa:
aromatic L-aa decarboxylase inhibitor (so Levodopa can --> brain)
Bromocriptine:
d R agonist (2,3,4; partial 1,5 antagonist)
Pergolide:
Parkinsons. d R agonist (1-5)
None
Pramipexole:
d2/d3 selective agonist
Ropinerol:
d2/d3 selective agonist
Entacapone:
inhibit peripheral COMT, prevent levodopa brkdn
Selegiline:
irrev inhibit MAO-B. Selective at dose (tyramine ok) Met to amphetamine, methamphetamine.
Chlorpromazine:
d R antagonist. (Typical) antipsychotic. Extrapyramidal effects.
Haloperidol:
d R antagonist. (Typical) antipsychotic. Extrapyramidal effects.
Amitriptyline:
TCA. block NET and 5HTT. Tox: sedation, ortho hypoT, anticholinergic Convulsions, Coma, Cardiotoxicity. Nortriptyline for elderly.
Fluoxetine:
SSRI. Tox: GI distress, anorgasmia. + MAOi serotonin syn (hyperthermia,  rigidity, cv collapse)
Bupropion:
~ amphetamine. Tox: tachycardia, insomnia, h/a, seizure (bulimic), !sexual
Tranylcypromine:
irrev MAOi. Tyramine tox. Seratonin syndrome (+SSRI/ßagonist)
Lithium:
Bipolar. Inhibit IP3 regen --> dec CNS adrenergic, muscarinic, serotonergic signaling. Tox: tremor, hypothyroid, nephro DI, teratogen. narrow TI.
Midazolam:
Benzodiazepine. Anxiety, IVGA.
Tox: dependence, exacerbate EtOH CNS dep. Tx OD w/ flumazenil.
Diazepam:
Benzodiazepine. Anxiety, status epilepticus, spasticity, EtOH detox IVGA. Tox: dependence, exacerbate EtOH CNS dep. Tx OD w/ flumazenil.
Flumazenil:
compet GABAa R antag. benzodiazepine OD (!barbiturate).
Phenytoin:
"Na+ channel blocker (maintain inactivation). Use dependent (specific for channels involved with Paroxysmal Depolarizing Shift and avoids side affects of non-use dep GABA agonists). Stabilizes focus and prevents generalization. Partial + tonic clonic seizures. NOT absence.Tox:
Fosphenytoin:
Anticonvulsant. Affects Na chan; mech unk. Prodrug for phenytoin. Less tox b/c solvent.
Carbamazepine:
Anticonvulsant. Same mech as phenytoin. Use instead of phenytoin for pt w/ complications or drug interactions. Partial seizures.
Phenobarbital:
Barbiturate (hypnotic, anesthetic, anticonvulsant). Increases GABA-mediated Cl conduction. Metabolized to Phenobarbital (active barbiturate). Tx overdose with Sx amangement (respiratory, bp)
Primidone:
Barbiturate (hypnotic, anesthetic, anticonvulsant). Increases GABA-mediated Cl conduction. Metabolized to Phenobarbital (active barbiturate). Tx overdose with Sx amangement (respiratory, bp)
Valproic acid:
Anticonvulsant.Na+ channel blocker (maintain inactivation), T-type Ca2+ channel blocker, increases GABA availability. Partial and Generalized. Note: can be used for absence seizures (after ethosuximide)
Prednisone:
inh expression of pro-inflam gene prod. CLL, Hodgkin (MOPP), autoimmune.
Cyclosporine:
bind cyclophilin --| calcineurin => inh IL2 prod by *Tcell. Tplant. Tplant, autoimmune.
Tox limits use: nephro, neuro, hepato (CsA -->TGF-B --> ECM --> fibrosis). prevent nephrotox with mannitol diuresis
Tacrolimus:
FK506. bind FKBP --| calcineurin => inh IL2 prod by *Tcell (50-100x more potent than CsA). Tplant.
Sirolimus:
aka Rapamycin. bind FKBP => inh mTOR/FRAP/RAFT = > inh intracellular resp to IL2 (blocks IL2 signalling). **binds to FKBP like tacrolimus, but does not inhibit calcineurin** Tplant. Inh stent stenosis: inh cell cycle at G1.
Azathioprine(AZA):
Cytotoxic. prodrug for mercaptopurine (6-MP) => inh nuc acid synth. Prodrug ==> slow release ==> used in immunosuppression (6-MP given directly for chemotherapy) Tplant, autoim.
Mycophenolate (MPA):
Cytotoxic. MMF = Mycophenolate mofetil, prodrug for MPA, activated by plasma esterases. inhibits IMPDH (RLS purine synthesis). *primary activity = lymphocytes*
None
Leflunomide:
Cytotoxic. --| de novo pyramidine synth ==> --| lymphocyte prolif. RA, SLE, MG, WG.
Cyclophosphamide:
"Cytotoxic. Alkylating agent: xlink DNA @ guanine N-7. activated in liver. **Main effect on B cell proliferation**
ATG:
"Anti-thymocyte globulin. mouse anti-human T cell pAb. Inactivates peripheral lymphocytes
OKT3:
Mouse anti-human CD3 mAb. tx acute tplant rej.
5-fluorouracil:
inhibit thymidylate synthase => inh dTMP synth. metabolite FdUMP incorp into mRNA
6-mercaptopurine:
converted to T-IMP => inh AMP, GMP synth
Cytosine arabinoside: Cytarabine. Cytidine analog. Met to AraCTP, incorporates into DNA => termination and death. Synergy with cyclophosphamide.
Bleomycin:
binds DNA, chelates iron => ssb + dsb via free radicals. R: drug efflux.
Vincristine:
bind tubulin prevent extension (dynamic instability). Mitotic spindle. M phase. MOPP
Vinblastine:
bind tubulin prevent extension (dynamic instability). Mitotic spindle. M phase.
Taxol:
Hyperstabilize MT.
Nitrogen mustard:
alkylate DNA.
Cyclophosphamide:
bis-alkylate (x-link) DNA. * by P450.
Procarbazine:
nonclassical alkylating agent. MOPP. Tox: met to MAOI.
Cis-platinum:
Cisplatin. x-link DNA. Tox: nephrotoxicity.
Methotrexate:
Folate analog. Competitively inhibit DHFR. Inh purine synth. S phase. Nonselective. Trimethoprim: bacterial isoform. Pyrimethamine: malrial.
Leukovorin:
Folinic acid rescue post lethal dose of MTX.
Doxorubicin:
Adriamycin. intercalates into DNA => scission.
L-asparaginase:
Removes exogenous asparagine. ALL req exog asp.
Folate:
Leukovorin. Wtih 5-flurouracil (complex). Folinic acid rescue w/MTX.
Prednisone:
Glucocorticoid R agonist. Trigger apoptosis. MOPP
Penicillin:
Pen tpeptidase inh.
 
S. pyogenes, N. meningitides, Clostridium, T. pallidum, Leptospira
Methicillin:
Pen tpeptidase inh. S. aureus
Nafcillin:
Pen tpeptidase inh. S. aureus
Ampicillin:
Pen tpeptidase inh. GP cocci.
Cefazolin:
Cephalosporin tpeptidase inh. Proteus mirabilis. E coli. K. pneumoniae
Sulbactam:
Beta-lactamase inh
Clavulanic acid:
Beta-lactamase inh
Imipenem-cilastin:
Monobactam tpeptidase inh. Cilastin inh renal dihjydropeptidase I.
Vancomycin:
Transglycosidase inh (polymerization). MRSA sepsis. C diff.
 
Gentamicin:
Aminoglycoside (inh 30S). Bacteriocidal. GN rod infections, !anaerobes.
Streptomycin:
Aminoglycoside (inh 30S). Bacteriocidal. GN rod infections, !anaerobes.
Tetracycline:
30S inh. Bstatic. Divalent cations inh abs. VACCUM THe BedRoom: Vibrio cholerae, Acne, Chlamydia, Ureaplasma Urealyticum, Mycoplasma  pneumoniae, Tularemia, H. pylori, Boreelia burgdorferi, Rickettsia.
Chloramphenicol:
50S inh. Bstatic. Rickettsia (eye inf, topical). Meningitis (H influ, N men, S pneumo). Rare b/x tox: (+/- aplastic) anemia, gray baby syndrome (UDP-glucuronyl tferase)
Erythromycin:
Macrolide. 50S inh. Bstatic. URI, pneumonias, STDs (GP cocci), Mycoplasma, Legionella, Chlamydia, Neisseria.
Azithromycin:
Macrolide. 50S inh. Bstatic. URI, pneumonias, STDs (GP cocci), Mycoplasma, Legionella, Chlamydia, Neisseria.
Ciprofloxacin:
Fluoroquinolone. Inh DNA gyrase (topoisomerase II). Bacteriocidal. GN rods (psedomonas), Neisseria
Isoniazid:
FAS2 inh (mycolic acid). M tuberculosis.
Rifampin:
DNA-dep RNA polymerase inh. M tuberculosis. Delay R to dapsone (leprosy). Meningoccal, HIB prophylaxis.
Morphine:
u opiod receptor agonist, inhibits substance P and other NT release from pre-syn neuron.  post syn neuron has inc. K+ conductance and hyperpolarize -> inhibition.  weak agonist at kappa and delta
Use: severe pain, cough suppressor, dec. GI motility (diarrhea), acute pulm. edema (venodilates to dec. preload/dyspnea)
Tox: resp. dep., biliary colic, N/V, pruritis, constipation/miosis, dependence (withdrawal Sx lacrimation, rhinorrhea, diaphoresis, piloerection, naus., inc. HR), overdose (triad of coma, pinpoint pupils and resp. depression)
  Meperidine:
trade name: Demerol, similar mechanism to morphine
used for rigors and mod-severe pain
Tox: metabolite build up can cause seizure
Codeine
methylated morphine, binds to u receptors - only a weak agonist (<morphine)
Use: mild-mod analgesia, antitussive (suppress cough), dec. GI motility
Oxycodone
potent oral opiod agonists, given with NSAIDs
long acting oxycodone (oxycontin) high abuse potential
same mech. as codeine
Fentanyl
same mech as morphine
short-acting IV agent used for general anesthesia, transderm fenatyl patch for cancer pain
Methadone
u agonist similar to morphine, used for Tx withdrawal Sx (good analgesic activity, oral, long t1/2 suppresses withdrawal, persistent effects with repeated administration)
Use: withdrawal Sx, analgesisa (esp. outpatient cancer palliation), antiperistaltic (rare)
Nalorphine
reverses effects of morphine and other narcotics
used for opiod overdose
side note: nalorphine causes withdrawal symptoms in addicts, it is administered to apparent ex-addicts to determine if they have returned to drug use
Naloxone
u receptor antagonist, reverse opiod effects (on resp., consciousness, pupil size, GI) in minutes (no effect without exogenous opiods)
use for acute opiod overdose (resp. dep, low BP, coma) - may need repeat dosing/2 minutes
Naltrexone
same mech as naloxone, given PO and dose lasts 48 hrs, used for outpatient mangement of alcohol/heroin dependence
Methylnaltrexone
peripheral opioid receptor antagonist (phase III clinical trials) for Tx of opioid-induced constipation in patients treated with narcotics for pain
does not cross BBB, reverses opiod side effects w/o eliminating analgesiathe blood-brain barrier in humans and reverses the opioid effects without interfering with pain relief
use for opiod induced: constipation, nausea/vomiting, cough suppression and urinary retention.
Butorphanol
similar to pentazocine (stronger agent), mixed opiod agonist-antagonist
agonist at kappa (SC analgesia), patial agonist/weak antagonist at u receptors (supraspinal analgesia if no other agonists around, if others agonist then may reduced analgesia)
use for analgesia for moderate-severe pain
Nalbuphine
potent kappa agonist and complete u antagonist for moderate to severe pain (similar to mech. of butorphanol)
Buprenorphine
same mechanism as butophanol for mod-severe pain, also used for opiod dependence
Dextromethorphan
OTC antitussive, d-isomer of methlated opiod with no analgesic/addictive properties
Enkephalin
naturally occurring morphine like substance of CNS that functions as analgesic and sedative (effects on mood and motivation)
act on u and delta receptors
b-endorphin
endogenous opiod with role in pain perception via CNS action
act on u and delta receptors
Dynorphin
endogenous opiod in the CNS that acts on kappa receptors
Miscellaneous
Timolol
non-selective beta-blocker (comp. antagonist), same effects as propanolol
can be given to dec. aqueous humor production (eye drops) = Glaucoma
Acetazolamide
inhibits CA -> dec. absorption of HCO3 and diuresis and hyperchloremic metabolic acidosis
use: chronic glaucoma (dec. aq. humor production), alkalosis, alkalize urine for excretion of weak acids (cystine, uric acid, phenobarb overdose), high-altitude sickness
Prochlorperazine
typical antipsychotic , 10-20X more potent than chlorpromazine
rarely used for psychosis and mania, now more for N/V
D2 antagonist with anti-Ach and histamine effects
Metoclopramide
Antiemetics that are D2 antagonists and weak 5-HT3 anatagonists
accelerate gastric emptying -> Tx for gastroparesis
Ondansetron
Selective seratonin antagonist of 5-HT3 receptors in chemoreceptor trigger zone in CNS and GI tract
use: potent antiemetic (chemo and post-op nausea)
Acarbose
oligosaccharide that inhibits alpha-glucosidase and delays intestinal absorption of carbs
Tx: T2DM
contraindicated in IBD
Tolbutamide
first generation sulfonylurea (less potent) than glyburide
Glyburide
2nd generation sulfonylurea that inc. insulin release - inhibits ATP-sensitive K+ channel and dec. efflux -> depolarization and open Ca+2 channels and insulin release
(this is also used physiologically - fed state has lots of ATP which inhibits channel)
minor effects on dec. glucagon/periph. sens. to insulin
Tx: T2DM
Metformin 
oral biguanide that dec. hepatic GNG (likely via AMPK), may also stimulate glycolysis
Tx: T2DM
Rosiglitazone
thiazolidinedione (gliatoze) that is an insullin sensitizer - binds to PPAR-gamma which  inc. adipose uptake of Glu and dec. TG/FFA release and inc. adiponectin release; skeletal muscle: inc. Glu uptake and use, inc. FFA oxid. (direct & indirect); liver: dec. GNG
Tx: T2DM
Ergotamine
partial 5-HT agonist causes intracranial constriction and suppression of meningeal pain pathways
Tx: acute migraine
Sumatriptan
selective 5-HT agonist for 1B and 1D receptors -> vasoconst. of intracranial arteries and presyn. suppression of vasoactive/nociceptive pepetides -> prevents blood from being diverted by AV fistulas (which cause ischemia) and trigeminal nerve activ
Tx: acute migraine +/- aura
contraindic: vascular dz, HTN
Trimethoprim
inhibits DHFR (PABA analog) and blocks folic acid recycling -> dec. nucleotides (T&purines) in bacteria
resistance: impaire uptake, altered DHFR, increased DHFR production
use: works with SMX for UTI, COPD, Nocardia, Stenotrophomonas, Isospora, Toxo, MRSA, PCP
Sulfamethoxazole
PABA analog that block dihydropteroate synthetase, which makes folate from PABA
humans do not synthesize
resistance via mutation/increased expression of DHPS, destroy drug
see TMP for use
contraindic: pregnancy -> neonatal kernicterus
potentiates phenytoin, warfarin, and oral hypoglycemics
P-aminobenzoate
PABA converted to folic acid by bacteria, PABA analogs (TMP-SMX) uses as Abx
Thalidomide
glutamic acid analog, mech. unclear - suppresses TNFalpha and antitumor properties via inhibition of NF-KB and angiogenesis, and inc NK activity
Tx: erythema nodosum leprae, chronic inflamm. dz (cutaneous SLE, sarcoidosis, RA, chronic arthritis, undiff. CT dz), chemotx for multiple myeloma/myelodysplastic syndrome
DO NOT use in pregnancy -> shortened/absent limbs in 1st trimester
Folate
Vitamin used by humans and bacteria, deficiency can cause neural tube defects during pregnancy or megaloblastic anemia outside of pregnancy
can be used to treat B12 deficiency, but will NOT Tx neurological effects 
Leucovorin (folinic acid)
treat megaloblastic anemia side effects of TMP-SMX with folinic acid since bacteria cant use it
Phenytoin:
"Na+ channel blocker (maintain inactivation). Use dependent (specific for channels involved with Paroxysmal Depolarizing Shift and avoids side affects of non-use dep GABA agonists). Stabilizes focus and prevents generalization. Partial + tonic clonic seizures. NOT absence.Tox: Highly protein bound => displace Warfarin, Hypoglycemics, Methotrexate, NSAIDs. Saturation kinetics: small inc doses => large inc plasma concentration. Induce P450. gingival hyperplasia, hirsutism, teratogenesis, nystagmus, diplopia, ataxia, sedation, megaloblastic anemia, SLE-like snydrome
None
Mycophenolate (MPA):
Cytotoxic. MMF = Mycophenolate mofetil, prodrug for MPA. *primary activity = lymphocytes* --| IMP dehydrogenase (rate limiting enzyme for guanosine formation) ==> impaired de-novo synthesis, affects de novo dependent cells (e.g. lymphocytes, activated T-cells) also induces apoptosis S/E: pancytopenias, GI sx