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77 Cards in this Set
- Front
- Back
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rivastigmine
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- pseudo-irreversible AcHE inhibitor
- short half life but long inhibition |
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donepezil
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- reversible AChE inhibitor -
- short enzyme inhibition - long halflife = long duration |
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galantamine
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- reversible AChEI - (tertiary alkaloid)
- allosteric effect on nicotinic receptors to enhance effect on ACh |
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tacrine
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- very short acting AChE inhibitor
- rarely used |
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memantine
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- use dependent NDMA blocker
- excitotoxic NMDA transmission is thought to worsen AD |
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drugs which cause mast cell degranulation (3)
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- polymyxin B
- vancomycin - radiocontrast media |
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lodoxamide tromethamine
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- ophthalmic mast cell stabilizer
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pemirolast potassium
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- ophthalmic mast cell stabilizer
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combination H1 antagonists/mast cell stabilizers
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- ketotifen fumarate (ophth)
- olpatadine (ophth, nasal) |
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buspirone
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- 5-HT1A agonist - anxiolytic
- only affects raphie nucleus/hippocampus |
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sumatriptan (and congeners)
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- 5-HT 1d/1b agonists
- brain, substantia nigra, globus pallidus, basal ganglia |
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tegaserod
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- partial 5-HT4 agonist
- Tx of constipation predominant IBS |
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cyproheptadine
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- phenothiazine antihistamine
- 5-HT2 antagonist (anti-inflammation, anti-gut movement) |
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ondansetron
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- 5-HT3 antagonist
- anti-emetic - also dolasetron - granisetron - palonosetron |
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metaproterenol
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- specific B2 agonist
- resistant to COMT - sustained bronchodilation |
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tertbutaline
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- specific B2 agonist
- resistant to COMT |
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bitolterol
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- prodrug of colterol
- specific B2 agonist - resistant to COMT |
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zileuton
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- 5-lipoxygenase inhibition throughout body
- hepatotoxicity, GI upset, headache |
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liclofelone
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- phase III trials for inhibition of COX AND LIPOXYGENASE
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zafirlukast
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- competitive inhibitor of CysLT1 (normal substrates LTD4 and LTE4)
- inhibits migration of basophils and lymphocytes to the area - synthetic peptide |
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montelukast
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- competitive CysLT1 inhibitor
- take without regard to food - does not interfere with warfarin metabolism |
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omalizumab
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- monoclonal antibody (IgG) that locks IgE receptor and decreases hypersensitivity type 1 reactions
- Tx steroid resistant astma |
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methylxanthine interactions
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- phenytoin, barbiturates, rifampin, oral contraceptives increase elimination
- cimetidine, macrolides, some fluoroquinolones decrease rate of elimination |
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antipyretic effect of NSAIDS occurs in the ______ via ______
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- hypothalamus
- PGE2 inhibition |
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indomethacin
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- indole derivative
- similar to salicylate - inhibit PMN motility - tx: patent ductus arteriosis - high GI effects and thrombocytopenia |
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suldinac
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- indole derivateve
- fewer adv effects to indomethacin |
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etodolac
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- indole derivative
- slightly more cox2 selective (not specific) - fewer side effects than indomethacin |
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meclofenamate, mefenamic acid
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- NSAID's (fenamates)
- Tx of dysmenorrhea - both high incidence of GI upset |
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phenylbutazone
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- pyrazolon derivative NSAID
- similar action to salicylates - significat ADV effects - removed |
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propionic acid NSAIDS
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- "fens" plus naproxen, oxaprozin
- lower GI upset - protein binding - inhibit clotting - reduced efficacy of antihypertensives |
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enolic acids
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- oxicams
- piroxicam causes Stevens-Johnson syndrome - meloxicam slightly cox-2 selective |
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tolmetin
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- miscellaneous NSAID
- better tolerated than aspirin - 99% protein bound but doesn't interfere with warfarin |
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diclofenac
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- NSAID
- leads to hepatotoxicity much like acetaminophen |
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celecoxib
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- NSAID (cox 2 specific)
- metabolized by CYP 2C9 (fluconazole inhibits) - still causes GI upset |
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gold
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- inhibits maturation and function of mononuclear phagocytes and T cells
- immune suppression - minimal effect in conditions other than RA |
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leflunomide
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- dihydroorate dehydrogenase inhibitor
- inhibits pyrimidine synthesis in lymphocytes - induces p53 tumor supressor protein - cell cycle arrest in lymphocytes |
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etanercept
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- recombinant soluble receptor for TNF-a
- tx chron's disease, RA |
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adalimumab
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- monoclonal antibody to TNF-a
- binds and neutralizes circulating TNF - tx refractory RA |
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anakinra
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- recombinant human interleukin 1 receptor antagonist
- TX refractory RA |
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abatacept
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- soluble fusion protein consisting of extracellular domain of cytotoxic T lymphocyte associated antigen 4 (CTLA-4) linked to IgG1
- inhibits T-activation, proliferation and production of TNF-a, interferon-y, interleukin-6 and 2 |
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penicillamine
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- metal chelator
- TX RA (reduces Cu) - may cause blood disorders |
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hydroxychloroquine
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- antimalarial for RA
- high rate of ocular toxicity |
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colchicine
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- binds tubulin, interferes with function of mitotic spindles in granulocytes
- TX gout |
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probenacid
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- uricosuric agent
- inhibits renal tubular secretion of a variety of drugs (B-lactams) - inhibits reabsorption of uric acid (only) |
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somatropin
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- recombinant human growth hormone
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mecasermin
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- recombinant IGF-1
- also contains IGF binding protein to increase halflife |
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octreotide/lanreotide
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- somatostatin receptor angonist
- inhibits GH production - lesser inhibition of glucagon, insulin, gastrin - TX acromegaly |
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pegvisomant
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- pegylated rhGH-variant, with mutations to increase affinity at GHR without stimulaion
- (GH antagonist) - tx: acromegaly |
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FSH analogs (3)
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- Follitropin alfa
- follitropin beta - urofolitropin - uses: ovulation stimulation (women) - TX: infertility due to hypogonadism in men |
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LH analogs (3)
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- human chorionic gonadotropin (hCG)
- choriogonadotropin alfa - lutropin - use: initiation of ovulation |
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GnRH analogs (2)
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- leuprolide
- others (elins) - tx: central precocious puberty - ovarian supression in COH - advanced prostate cancer |
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GnRH antagonists for COH
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- ganirelix
- cetrorelix - reduces endogenous LH and FSH |
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degarelix
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- GnRH receptor antagonist
- TX: advanced prostate cancer |
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bromocriptine, cabergoline
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- ergots (D2 agonists)
- tx: hyperprolactinemia (and PD) |
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oxytocin
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- TX: induction of labor
- control of uterine hemorrhage after delivery |
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desmopressin
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- V2 agonist more than V1
- TX: pituitary diabetes insipidus - hemophilia A - von Willebrand disease |
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vasopressin
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- TX: diabetes insipidus
- control of bleeding from esophageal varices |
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conivaptan
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- V1a and V2 antagonist
- tx: hyponatremia |
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tolvaptan
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- more V2 selective antagonist
- Tx: hyponatremia |
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perchlorate
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- inhibits Iodide transport into the thyroid
- TX: hyperthyroidism - rarely due to aplastic anemia |
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iodide
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- in high concentrations inhibits uptake of iodide
- also shrinks thyroid prior to surgery |
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propylthiouracil
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- inhibits thyroid peroxidase (organification)
- inhibits 5-deiodinase) conversion of T4 to T3 - TX: hyperthyroidism - has fewer side effects |
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methimazole
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- inhibits thyroid peroxidase (organification)
- PTU is preferred to further inhibition of T4 to T3 - Tx: hyperthyroidism |
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mitotane
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- medical adrenalectomy
- structural analog of DDT - compassionate care |
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aminoglutethimide
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- tx: cushings (due to adrenal carcinoma)
- inhibits production of all hormonally active steroids (aromatase as well) - breast cancer (largely replaced) |
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metyrapone
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- inhibits 11B-hydroxylation (cortisol synthesis_
- Tx: cushings - diagnosis of HPA axis (ACTH will increase if pituitary is normal) |
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spironolactone
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- aldosterone antagonist
- weak inhibitor of androgen receptors - decreases levels of testosterone and androstenedione - Tx: aldosteronism |
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dehydroepiandrosterone (DHEA)
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- TX: hypoaldosteronism
- chronic fatigue |
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cyproterone acetate
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- androgen receptor antagonist
- orphan drug - prostate cancer |
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flutamide, bicalutamide, nilutamide
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- androgen receptor antagonists
- prostate cancer - hirsutism |
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trilostane
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- inhibits 3B-hydroxysteroid synthesis
- inhibits cortisol and aldosterone synthesis - Tx: cushing's syndrome |
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leuprolide
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- GnRH receptor agonist
- long term administration desensitizes pituitary to GnRH effects, FSH, and LH release is inhibited - intermittent treatment increases FH, LSH |
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estrogen receptor partial agonists (antagonists) (4)
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- tamoxifen
- toremifine - raloxifene - clomiphene (most used to stimulate LH and FSH resulting in multiple follicle development and ovulation) |
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mifepristone (2 uses)
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- prosgesterone receptor competitive antagonist
- USE: abortion - also glucocorticoid receptor antagonist, useful in ectopic ACTH syndrome |
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danazol
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- weak progesterone, testosterone, glucocorticoid receptor agonist (androgen agent)
- used to suppress ovarian function (mid-cycle FSH LH surge) |
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aromatase inhibitors
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- anastrozole, letrozole (non-steroidal)
- exemestane - steroidal irreversible inhibitor |
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fluvestrant
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- pure estrogen receptor antagonist
- little use outside breast cancer |
