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Pharm-Drugs (Exam 2)

QuestionAnswer
Chlorpheniramine H1 Histamine Receptor Antagonist (1st generation) -mild sedative effects -in OTC "cold" drugs -rapidly absorbed orally -ineffective in bronchial ashthma TX: seasonal allergic rhinitis/urticaria
Diphenhydramine H1 Histamine Receptor Antagonist (1st generation) -strong sedative -widely used for oral and paraenteral administration SEs: ototoxicity-not in newborns or w/ antibiotics TX: motion sickness, Parkinsonism, sedation, allergies
Promethazine H1 Histamine Receptor Antagonist (1st generation) SEs: ototoxicity-not in newborns or w/ antibiotics TX: motion sickness, vestibular disturbances, allergies
Terfenadine H1 Histamine Receptor Antagonist (1st generation) -cardiac toxicity when taking in combo with antimicrobial drugs -metabolized to fexofenadine, if CYP3A4 is inhibited -> terfenadine accumulates TX: allergies
Desloratadine H1 Histamine Receptor Antagonist (2nd generation)
Fexofenadine H1 Histamine Receptor Antagonist (2nd generation) -active metabolite of terfenadine (not cardiotoxic) -no sedative effects -lower risk of arrythmia/cardiac effects TX: allergies
Loratadine H1 Histamine Receptor Antagonist (2nd generation) -no sedative effects -longer action -no significant SEs TX: allergies
Cetirizine H1 Histamine Receptor Antagonist (2nd generation)
Cromolyn sodium -inhibit immunologically triggered degranulation of mast cells -used in prophylaxis of bronchial asthma
Nedocromil -inhibit immunologically triggered degranulation of mast cells -used in prophylaxis of bronchial asthma
PGF2α -dec. intraocular pressure; vasoconstriction/bronchoconstriction (inc. Ca2+ or IP3/DAG); inc. contractions (inc. oxytocin) DRUGS: latanoprost
PGI -dec. intraocular pressure; dec. plt aggreg; vasodilation/bronchodilation (inc. cAMP); GI: dec. acid, inc. mucus, inc. blood flow; reprod: dec. tone; kidney: incr. blood flow, inc. diuresis, dec. ADH; inc. temp, dec. NE DRUGS: misoprostil, alprostadil
Dinoprostone synthetic PGE2 administered vaginally for oxytotic effects, collagenase activity -approved for 2nd trimester use as abortifacient -produces uterine contractions (used to induce labor)
Latanoprost stable, long acting PGF2α derivative-treat open angle glaucoma -dec. intraocular pressure -stimulate eyelash growth
Misoprostol PGE1 analog -can be used in combination with meifeprestone (RU486) or methotrexate -> inc. contractions -> abortifacient -provide protection for NSAID induced ulcers (cytoprotective at low dose and inhibits gastric acid secretion at higher doses)
Alprostadil PGE1 analog -administered as a urethral suppository or intracavernous injection to aid in producing erections -maintainence of patent ductus arteriosus -> until surgical correction
Treprostinil PGI2 analog -treatment of pulmonary arterial hypertension -administered using continuous sub-Q delivery
Montelukast leukotriene receptor antagonist -treating asthma by preventing bronchoconstriction and inhibiting bronchial mucal secretions
Acetaminophen not an NSAID because not anti-inflammatory or anti-coagulant -antipyretic and analgesic -inhibits COX-1 and COX-2 -less gastric irritation/bleeding like other NSAIDs -substitute where aspirin is contraindicated -liver toxicity TX: RA, chronic infla
Aspirin (acetylsalicylic acid) NSAID -irreversible inhibitor of COX-1 and 2 -potent anti-coagulant -substantial GI irritation SEs: aspirin-induced asthma (hypersensitivity), Reyes syndrome, salicylism TX: RA, chronic inflamm. -prevent transient ischemic attacks
Ibuprofen non-salicylic NSAID -COX-1 and 2 inhibitor -anti-inflammatory like ASA but less GI irritation -short half-life (2h) and liver metabolized -low dose: analgesic -high dose: analgesic/anti-inflamm SEs: GI, rash, hepatitis... TX: RA, chronic inflam
Indomethacin non-salicylic NSAID -COX-1 and 2 inhibitor -very potent -30% patients have rxns TX: RA, chronic inflamm
Naproxen non-salicylic NSAID -COX-1 and 2 inhibitor -long half life (12h) -free fraction higher in females than males TX: RA, chronic inflamm
Non-acetylated salicylates -no irreversible acetylation of COX enzymes -> less effective than ASA -major advantages: lack of renal toxicity and don't produce NSAID asthma TX: RA, chronic inflamm
Celecoxib Cox-2 selective inhibitor -least potent of these agents, less cardiovascular risks -fewer GI effects, does not effect platelet aggregation -SE: interfere with anti-hypertensive med -> edema, do not give to patients with GI ulcer TX: RA, chronic infla
N-Acetylcysteine for acetaminophen overdose -maintain liver glutathione stores by binding to reactive metabolite as it is produced -can be given 36h after OD, most effective if administered within 8-10h if possible
Cyclosporin A immunosuppressent (T cell inhib.) -inhib. calcineurin phosphatase -> dec. cytokines and impairs response of T cells to antigens TX: GVH, aplastic anemia, organ transplants; autoimmune diseases TOX: rev. nephrotoxicity, neurotoxicity, vasoconstx -> HTN
Tacrolimus (FK506) immunosuppressant (cytotoxic), 100 times more potent than cyclosporin A (similar MOA, USES, TOXICITY, and DRUG INTERACTIONS as cyclosporin A)
Azathioprine immunosuppressant (cytotoxic) -purine antimetabolite (S phase inhibitor), inhibits T and B cell cell cycle/proliferation SEs: myelosupp., coadm. with allopurinal is TOXIC TX: transplant rejection, RA
Mycophenolate mofetil (MOA, USES) immunosuppressant (cytotoxic) -inhibits inosine monophosphate dehydrogenase -> inhibit proliferation of T and B lymphocytes -coadm. cyclosporine or CSs -no coadm. antacids USE: trasplantation rejection (renal)
Prednisone (corticosteroid) (MOA and USES) immunosuppress. and anti-inflamm MOA: regulates of genes with glucocorticoid response elements USE: combo with immunosuppresents for treatment of allograft rejection, autoimmmune disorders, hypersensitivity rxns that produce hives
Inteferons USES: hairy cell leukemia, kaposi's sarcoma, malignant melanomas; IFN-beta used to treat MS TOXICITY: fever, chills, myelosuppression, neurotoxicity
Filgastrim (Granulocyte-macrophage colony stimulating factor, GM-CSF) MOA: cytokine that stimulates clonal expansion and differentiation of hematopoietic cells USES: accelerate recovery of WBC in patients with depressed hematopoiesis (cancer, congential) TOXICITY: hypersensitivity rxns
Epoetin alfa recombinant human erythropoetin MOA: given IV USES: treat anemia resulting from AIDS, renal failure, cancer chemo, prematurity, chronic inflammation TOXICITY: patients may need anticoagulants (hemodialysis), hypertensive patients need readjustment of d
Sirolimus (MOA and USES) -inhibit T cell activation/proliferation USE: transplant rejection (when used in combo with calcineurin inhibitor and GCs), GVHD, autoimmune disease -may produce tolerance
FTY720 (MOA) sphingosine 1-phosphate receptor agonist MOA: reversibly sequesters lymphocytes in lymph nodes and peyer's patches and keeps them out of circulation so that graft is protected form T cell-mediated attack
Infliximab/Etanercept (ENEBREL) Ig against TNF-alpha MOA: prevent cytokine from binding to its receptor USES: combo with methotrexate for RA who do no respond to methotrexate alone, crohn's disease (Infliximab) TOXICITY: serious infections
Muromonab-CD3 Ig against CD3 (mouse monoclonal antibody) -binds to CD3 on T cell and alters CMI -> blocks antigen binding site -> no transplant rejection TOXICITY: cytokine release syndrome-fever, chills, vomiting, headache, weakness
Daclizumab Ig against IL-2 receptor (mouse/human monoclonal antibody) MOA: blocks IL-2 receptor on T cells USE: prevents acute renal transplant rejection, coadmin. with cyclosporine and CSs TOXICITY: well tolerated
Rho (d) immune globulin Ig against anti-D antibodies MOA: block response of an Rh-neg mother to a RH-positive baby USE: prevent hemolytic disease of newborn
Bacillus Calmette-Guerin strain of byobacterium bovis MOA: stimulates T cells and NK cells USES: used for bladder cancer patients TOXICITY: severe hypersensitivity and shock
Interleukin-2 (Aldeslleukin) -promotes T and B cell proliferation, differentiation, recruitment of NK cells, thymocytes USES: AIDS and cancer patients TOXICITY: fever, nausea, vomiting, malaise
Cyclosporin A (DRUG INTERACTIONS) DRUG INTERACT.: erythomycin, ketoconazole, amphotericin B inhibit metabolism in liver -> increase in drug's toxicity; drugs that accelerate clearance -> transplant rejection -do not give cyclosporine and sirolimus at same time (increase other drug's S
Mycophenolate mofetil (TOXICITY, DRUG INTERACTIONS) TOXICITY: diarrhea, leukopenia, CMV infection, GI hemmorage DI: coadm. w/ antacids containing magnesium and aluminum hydroxides decreases absorption
Prednisone (corticosteroid) (TOXICITY) TOXICITY: chronic use (beyond 2 weeks) associated with increased infections, formation of ulcers, induction of hyperglycemia and osteroperosis
Sirolimus (TOXICITY and DRUG INTERACTIONS) TOXICITY: dose-dependent thrombocytopenia, leukopenia, hyperlipidemia DI: substrate for CYP3A4 -> affected by any drug that inhibit/induces this enzyme -should not be given with cyclosporine or ketoconazole
FTY720 (USES and TOXICITY) USES: used with cyclosporine and prednisone for prevention of acute organ rejection in transplant patients TOXICITY: reversible lymphopenia and increased heart rate
Indomethacin NSAID -immediate relief of pain and inflammation -not mandatory in tx of RA, adjuvant
Naproxen NSAID -immediate relief of pain and inflammation -not mandatory in tx of RA, adjuvant
Celecoxib NSAID -immediate relief of pain and inflammation -not mandatory in tx of RA, adjuvant
Prednisone glucocorticoid, corticosteroid -fast action for severe inflammation when NSAIDs are contraindicated, serious systemic manifestations (vasculitis, pericarditis), bridge therapy, when all other medical means are exhausted
Azathioprine traditional DMARD -for refractory RA or systemic involvement
Cyclosporine traditional DMARD -limited use
Methotrexate traditional DMARD MOA: inhibits dihydrofolate reductase -standard of care for early therapy of RA -> response in 4-6 weeks -low doses decrease symptoms, preserve joints, improve outcome
Sulfasalazine traditional DMARD -antimalarial: anti-inflammatory, immunomodulator -moderately effective for mild RA -used in combo with methotrexate -may require 2-3 months for response -more toxic than hydroxychloriquine -use during pregnancy is safe
Etarnercept biological DMARD (TNF-alpha inhibitor) -fusion protein-contains ligand-binding sequence of human TNF-alpha receptor fused to human IgG1 -binds TNF-alpha, prevents it from activating its receptors -monotherapy or combo with methotrexate -numerous SEs
Adalimunab biological DMARD (TNF-alpha inhibitor) -humanized anti-TNF-alpha monoclonal antibody -does not contain non-humna or artificial sequences -monotherapy or combo with methotrexate -numerous SEs
Infliximab biological DMARD (TNF-alpha inhibitor) -chimeric anti-TNF-alpha monoclonal antibody -combo with mexotrexate for patients that do no respond to methotrexate alone -numerous SEs
Anakinra biologic DMARD (IL-1 inhibitor) -competitively inhibits pro-inflammatory effects of IL-1 -monotherapy or combo with methotrexate -not given with TNF inhibitor -modest improvements in signs/symptoms -considered least effective DMARD -infrequently use
Abatacept biological DMARD (selective costimulation) -fusion protein-homologue of CD28 (T cell receptor for B7) -> binds B7 with higher affinity than CD28 -> interferes with T-cell activation -> inhibits production of TNF-alpha, IFN-gamma, IL-2
Rituximab biological DMARD (CD20 antibody) -chimeric monoclonal antibody against CD20 on surface of B cells -combination with methotrexate -no combo with other biologic DMARD -fatal infusion rxns -increased risk of infection, reactivation of Hep B infection
Prednisone (TOXICITY) high doses: mineralcorticoid effects -increased susceptibility to infection, inhibits growth, induces myopathy, osteroporosis, acute adrenal insufficiency
Methotrexate (TOXICITY) adverse SEs even at low doses -bone marrow suppression: leukopenia, thrombocytopenia, anemia -hypersensitivity pnemonia -teratogenic -avoid alcohol -> hepatic toxicity
Abatacept (TOXICITY) -not given with another biologic DMARD -infusion rxs: hypertension, headache, anaphylaxis (rare) -increased risk of serious infections
Cancer Regimens (MOPP) mechloretamine, oncovin, prednisone, procarbazine TX: hodgkin's disease (lymphoma)
Cancer Regimens (CVPP) cyclophosphamide, vincristine, prednisone, procarbazine TX: hodgkin's disease, non hodgkin's disease
Cancer Regimens (CMF) cyclophosphamide, methotrexate, 5-fluorouracil TX: breast cancer (in post-menopausal women with no estrogen receptors)
Cancer Regimens (ABVD) adriamycin, bleomycin, vinblastine, dacarbazine TX: lymphomas, sarcomas
Cancer Regimens (FAM) 5-fluorouracil, adriamycin, mitomysin TX: colon cancer
Cancer Regimens (CMV) cisplatin, methotrexate, vinblastine
Cancer Regimens (FAC) 5-fluorouracil, adriamycin, cyclophosphamide
mechlorethamine (nitrogen mustards) phase non-specific -affects DNA synthesis and cell cycle -bifunctional agents produce cross-linking b/w DNA strands or b/w DNA and protein resulting in cytotoxicity TX: MOPP -> hodgkin's disease TOXICITIY: bone marrow and GI
cyclophosphamide, ifosfamide (nitrogen mustards) phase non-specific -crosslinks DNA/RNA strands TX: non-hodgkin's lymphona, breast/ovarian cancer (CMF, CVPP), RA TOXICITY: tall lean cyclist has bladder problems and goes to the men's (MENSA) room (acrolein->hemmorhagic cystitis), immunosupp and alope
melphalan (nitrogen mustards) phase non-specific TX: multiple myeloma and ovarian cancer TOXICITY: nausea and bone marrrow suppression
carmustine, loumustine (nitrosoureas) phase non-specific -alkylate DNA, produce strand breaks and inhibit protein syn. TX: brain tumors (highly lipophilic) TOXICITY: severe myelosuppression, long-term use -> renal failure
busulfan phase non-specific -crosslinks strands of DNA TX: CML TOXICITY: high doses -> pulmonary fibrosis
procarbazine phase non-specific -inhibits DNA/RNA/protein synthesis TX: hodgkin's (MOPP, CVPP), non-hodgkin's, small cell lung cancer, malignant melanoma, brain tumors TOX: bone marrow depress, acetaldehyde accum, inhib. MO and cytochrome P450 (no drugs or drinkin
dacarbazine (triazenes) phase non-specific -methylate DNA TX: hodgkin's
cisplatin, carboplatin (platinum complexes) phase non-specific -form intra/interstrand DNA crosslinks -> dec DNA/RNA synth, produce DNA breaks TX: testicular tumors (coadm. vinblastine and bleomycin), ovarian CA (coadm. cyclophosphamide), SCLC, bladder CA TOX: ototoxic, nephrotox, electrolyte di
methotrexate (folic acid analogs)-antimetabolite -inhib DHFR (S phase specific) TX: cures osteosarcoma, choriocarcinoma; tx ALL, burkitts, non-hodgkin's, bladder CA, breast CA (CMF); low dose-RA and psoriasis TOX: myelosupp, nausea/diarr/fatigue, neurotoxic, chronic adm.-> hepatic fib -leucovorin res
leucovorin (folate antagonist rescue agent)-antimetabolite used to reverse effects of methotrexate by bypassing the blocked DHFR
6-mercaptopurine (6-MP) (purine analogs) S phase specific -decrease purine synthesis TX: ALL TOX: bone marrow depression, gout (treat with allopurinol)
6-thioguanine (6-TG) (purine analogs) S phase specific -inhibit purine synthesis TX: coadmin. cytarabine and daunorubicin for acute ganulocytic leukemia TOX: bone marrow immunosuppression
5-fluorouracil, capecitabine (5-FU) (pyrimadine analogs) S phase specific -inhibit thymidylate synthase -> dec DNA synthesis and cell death TX: breast CA (CMF), colon or rectum CA (FAM), colon CA pts on cimetidine (hrtburn)have inc rate of survival TOX: myelosuppress, GI tract toxicity
cytarabine (AraC) (pyrimadine analogs) S phase specific -incorporate into DNA and terminates chain elongation TX: acute leukemia (coadm. 6-TG) TOX: severe myelosuppression
gemcitabine (pyramidine analogs) NOT S phase specific -inhibits DNA polymerase and ribonucleotide reductase (terminates elongation) TX: metastatic pancreatic CA (1st line) and non-small cell lung CA TOX: myelosupp, flu-like syndrome, mild elevation in liver transaminases
vincristine (vinca alkaloids) M phase-specific -reversibly bind tubulin and blocks polymerization into MT TX: childhood ALL (1st line), hodgkin's (MOPP), acute myelogenous leuk, hodgkin's, pediatric solid tumors, some adult solid tumors TOX: peripheral neuropathy
vinblastine (vinca alkaloids) M phase-specific -reversibly bind tubulin and blocks polymerization into MT TX: cures testicular tumors (coadm. bleomycin, cisplatin); hodgkin's, non-hodgkin's, choriocarcinoma TOX: bone marrow suppression
paclitaxel, docetaxel (taxanes) M phase-specific -promotes MT formation and stabilization TX: ovarian and breast CA TOX: neutropenia (give G-CSF), hypersensitivity (give dexamethasone/diphenhydramine/H2 blocker)
etoposide (podophyllotoxins) S/G2 phase-specific -inihibits topoisomerase II -> block DNA replication TX: testicular tumors (coadm. bleomycin and cisplatin), SCLC (coadm. cisplatin and ifosfamide) TOX: dose-limiting myelosuppression
topotecan, irinotecan (camptothecins) -inihibit topoisomerase I -> block DNA replication TX: colorectal CA (after 5-FU treatment), ovarian and advanced SCLC TOX: myelosupp, alopecia, nausea, vomiting, cholinergic sym, mucositis, bronzing of skin
bleomycin G2 phase-specific -binds DNA, generates free rad and produces strand breaks, inhib ATP-dependent DNA ligase -> prevent DNA repair, cells accumulate in G2 TX: cures testicular CA (coadm. cisplatin and vinblastine); squamous carcinomas and lymphomas
bleomycin (TOXICITY) TOX: pneumonitis and pulmonary fibrosis (may be fatal); hyperpigmentation, stomatitis, alopecia, LEAST MYELOSUPP ACTIVITY
Actinomycin D (Dactinomycin) (DNA-binding antibiotics) inhibits DNA/RNA synthesis TX: cures Wilm's tumor and rhabdomyosarcoma (coadm. vincristine and cyclophosphamide after surgery/radiotherapy); methotrextae-resistant choriocarcinoma TOX: myelosupp
Adriamycin (Doxorubicin) (anthracyclines) -intercalate with DNA and blocks DNA/RNA synthesis TX: myelomas, sarcomas, lymphomas (ABVD, FAM) TOX: cardiotoxicity, myelosupp, severe alopecia
Daunorubicin (anthracyclines) -intercalate with DNA and blocks DNA/RNA synthesis TX: acute leukemias TOX: cardiotoxicity, myelosupp, severe alopecia
Hydroxyurea (miscellaneous antineoplastic agents) ?
L-asparaginase (miscellaneous antineoplastic agents) -metabolizes L-asparagine required by tumor cells and dec levels of asparagine synthetase TX: ALL (coadm. vincristine and prednisone) TOX: hypersensitivity resulting from its antigenicity
Thalidomide (miscellaneous antineoplastic agents) ?
Vorinostat (miscellaneous antineoplastic agents) ?
Bortezomib (proteasome inhibitors) -reversible inhibitor of 26 S proteosome and prevents activation of NF-kB TX: multiple myeloma TOX: nausea, diarrhea, muscle weakening, myelosupp, peripheral neuropathy, fever, anorexia, anemia, constipation
Imatinib mesylate (GLEEVEC) (protein tyrosine kinase inhibitors) blocks Bcr-Abl kinase -phosphorylates proteins that cause cell proliferation (blocks this) TX: CML; GI stromal sarcoma TOX: nausea, edema, muscle cramps, rash, diarrhea, myelosupp DI: inc warfarin, itraconz and erythro -> inc IM, phenytoin -> dec I
Gefitinib (protein tyrosine kinase inhibitors) blocks EGFR kinase TX: non small cell lung CA TOX: well tolerated, diarrhea, acne-like rash -works best in asian nonsmokers DI: inducers of P450 decrease serum conc of drug
Erlotinib (protein tyrosine kinase inhibitors) ?
Sunitinib (protein tyrosine kinase inhibitors) blocks VEGFR and PDGFR kinase TX: RCC, GI stromal tumors TOX: fatigue, anorexia, nausea, diarrhea, mucositis, stromatitis DI: ketoconz -> inc drug, rifampin -> dec drug
Sorafenib (protein tyrosine kinase inhibitors) blocks cell surface and intracellular kinases TX: RCC TOX: fatigue, diarrhea, dermatologic hypertension, neutropenia, bleeding
Lapatinib (protein tyrosine kinase inhibitors) ?
Trastuzumab (monoclonal antibodies) blocks HER2/neu receptor TX: breast CA TOX: very few-fever and chills, cardiotoxicity when coadm. adriamycin
Rituximab (monoclonal antibodies) blocks CD20 receptor TX: low grade non-hodgkin's B cell lymphoma TOX: fever, chills, nausea on first infusion
Cetuximab (monoclonal antibodies) blocks EGFR receptor (EGFR overexpressed in colorectal CA) TX: colorectal CA TOX: acne-like skin rash
IFN-alpha (bilogical response modifiers) TX: hairy cell leukemia, kaposi's sarcoma, melanoma (malignant) TOX: fever and chills, myelosupp, neurotoxicity
IL-2 (biological response modifiers) -induces a T cell response cytolytic for tumor cell TX: melanoma (malignant), renal cell CA TOX: hypotension, arrythmias, peripheral edema, elevated liver function, anemia, thrombocytopenia, nausea, diarrhea, fever
G-CSF (biological response modifiers) -expands pop of neutrophil granulocyte precursors and augments granulocyte function TX: prophylaxis of chemotherapy-induced neutropenia TOX: bone pain in lower back, sternum, pelvis
Tamoxifen (selective estrogen receptor modulators) estrogen antagonist -inhibits expression of TGF and IGF-1 and inhibits breast CA growth TX: breast CA (post-men, in ER+ tumors) TOX: nausea, hot flashes, vaginal bleeding, skin rases, hypercalcemia, incresed risk of endometrial CA
aminoglutethimide (aromatase inhibitors) inhibits desmoloase and aromatase -> dec estradiol TX: breast cancer (post-men, in ER+ tumors) TOX: CNS depression (drowsiness, visual blurring, ataxia)
anastrozole (aromatase inhibitors) TX: breast CA (post-men, in ER+ tumors) TOX: GI disturbanes, lack of bodily strength, headaches, bone and back pain -reduced incidence of developing blood clotting and vaginal bleeding compared to Tamoxifen
prednisone (GCs) -converted to prednisolone, binds receptor TX: pt of MOPP and CVPP regimens for hodgkins/non-hodgkin's lymphomas TOX: cushing's syndrome; immunosupp
Leuprolide, Goserelin (long-acting gonadotropin releasing hormone analogs) cause testosterone and estrogen production to drop TX: prostate cancer TOX: not very toxic, sexual dysfunction, transient flare of disease after initial dose prevented by coadm. flutamide,
Flutamide (antiandrogens) blocks DHT binding to receptors TX: prostate CA TOX: GI distress
Tamoxifen (benefits) dec osteoporosis, decreased serum and LDL cholestrol, increased apolipoprotein A1 (prevent heart disease)
Created by: 8403333
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