Pharm 2 Block 7

sbentley's version from 2016-02-14 23:08

Section 1

Question Answer
First line for preventing/reducing chronic allograft vaculophathy in cardiac transplant pts.Mycophenolate Mofetil
Lymphopenia may be significant, so monitoring blood counts must be done regularly and drug is withheld if active infection is present.DMF: Dimethyl fumurate AE and complications
Toxicities: elevation of liver enzymes with risk of liver and kidney damage. TERATOGENICDMF: Dimethyl fumurate AE and complications
Antimalarial with immunosuppressant propertiesHydroxychloroquine
Suppresses intracellular antigen processing and loading of peptides onto MHC2 by increasing the pH of lysosomal and endosomal components, increasing T cell activationHydroxychloroquine
Used to tx and prevent GVH after allogenic stem cell transplantationHydroxychloroquine
Alkylating agent • Destroys proliferating lymphoid cells by targeting DNA, but also alkylated resting cells. • High doses can cause pancytopenia • MOST EFFECTIVE immunosuppressant Cyclophosphamide AE, MOA
When using methotrexate, can use folinic acid to “rescue” the normal cells.Leucovorin Therapy
Give the drug given as an antidote to cyclophosphamide caused hemorrhagic cystitis.MESNA
Describe p-glycoprotein as an energy-dependent efflux pump for anti-tumor agents.p-glycoprotein = has two binding sites for ATP and one binding site involved in drug transport. This efflux pump allows cells to expel drugs and thus contributes to multidrug resistance of cancer cells. This protein comes from MDR1 gene.
is the dose-limiting factor in use of vincristineNeurotoxicity
MOPPUsed for Hodgkin’s dz.  mechlorethamine, vincristine, procarbazine, prednisone.
First line agent for SCLC (small cell lung carcinoma)Etoposide
Blocks G1 phase, as well as block replication of DNA (S-phase) Mainly for tx of testicular cancer.Etoposide
Triphosphate metabolite that interferes with DNA synthesis by inhibiting DNA polymerase alpha and beta. It also induces apoptosisFludarabine
acts on dihydrofolate reductase → blocks DNA synthesis and proliferation= MOA  Anemia –megoblatic anemia (Rx with folate and b12)  myelosuppression, GI toxicity, nephrotoxicity= 3 dose limiting AEMethotrexate
Bleomycin dose limiting AE?Pulmonary Toxicity= pulmonary fibrosis
Binds tubulin that prevents cells from forming spindles needed to move chromosomes during metaphase.Vincristine
Neurotoxicity= dose limiting AE, CI in pts with neuromuscular disordersVincristine
Anaphylaxis, Neurotoxicity (hearing loss)? is a dangerous side effect. Nephrotoxicity is a dose-limiting AE. Cisplatin
Platinum analog • Reacts with N7 of guanine • Crosslinks DNACisplatin
DNA topoisomerase II inhibitor (crucial for replication and transcription) • Intercalates btw base pairs of DNA (inhibits DNA-dependent RNA synthesis) • Generates free radicals (causing membrane damage and DNA strand breaks) Doxorubicin MOA
Prolonged use = megaloblastic anemia • 5-FU = acts on thymidylate synthase → blocks DNA synthesis and proliferation5FU (SE and MOA)
Why don’t we use alkylating agents for multiple myelomathey destroy fast growing cells and destroy regenerative bone marrow.
Apply one level 1 treatment in the maintenance phase of multiple myeloma treatment to a clinically-relevant case scenarioThalidomide (1) • Lenalidomide (1)

Section 2

Question Answer
(-gravir) • Dolutegravir, Elvitegravir, RaltegravirIntegrase inh
Integrase MOA:Inhibitors stop integration of viral and host cell DNA
(-navir) • Atazanavir, darunavir, fosamprenavir, indinavir, lopinavir, ritonavirProtease inh
Cleaves viral polyprotein into active viral enzymes • Inhibitors bind to active site of HIV protease.Protease MOA:
bind reversibly to the active site of the HIV protease o Viral particles become immature and noninfectious o PI inhibits viral replication in any infected cellsProtease Inh
Give the three drugs in the one PI-based ART regimen recommended for naïve HIV patientsDarunavir/ ritonavir (DRV/r) plus tenofovir (TDF) + emtricitabine (FTC)
Regimens that contain full-dose ritonavir or ritonavir as the sole HIV protease inhibitor (PI) are not recommended for initial treatment
not recommended in initial ARTFusion inhibitor, CCR5 antagonist
Osteopenia/osteoporosis • Hepatotoxicity= monitor enzymes AST/ALT= objective • Lipodystrophy, lipid abn. • HyperglycemiaProtease AE
CCR5 antagonist. Binds to allosteric site of the receptor and inhibits HIV viral entryMaravorac
Inhibits the early essential step of HIV replication (reverse transcriptase) by incorporating false nucleic acids into newly produced proviral DNA. The nucleic acids lack 3’-OH group, thus incorporation into DNA terminates chain elongation.Nucleoside reverse transcriptase
Apply a unique indication for enfuvirtide to a clinically-relevant case scenario.Advanced HIV-1 infection patients o Ongoing viral replication despite antiretroviral therapy
risk factor for multiple myelomaold age
Which of the following is often seen in the cytoplasm of acute myelocytic leukemia cells?Auer Rods

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