Mechanism Flashcards by LL Cool G

replaces clotting factors, fibrinogen, protein S, protein C, and antithrombin

Fresh frozen plasma

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disrupt DNA and RNA synthesis, converted to 5-fluorouracil, by fungi

Flucytosine

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chlorinated to form nitrenium ion; toxic to bone marrow precursors

clozapine

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These drugs form a ternary complex with topoisomerase II and DNA

Doxorubicin, daunorubicin - anthracyclines

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inhibits dihydroorotate dehydrogenase, leading to inhibition of pyrimidine synthesis

Leflunomide

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Direct Factor Xa inhibitor not requiring antithrombin

Rivaroxaban

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inhibits the re-ligation of the broken DNA strands, leading to apoptosis

Doxorubicin, daunorubicin - anthracyclines

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concentrates in parasite food vacuoles; increases free heme and toxicity to parasite

Chloroquine

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monoclonal to T cells

Alemtuzumab

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monoclonal to B cells

rituximab

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competitive inhibitors of dihydrofolate reductase

Trimethoprim and pyrimethamine

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binds to both the active site and a second site on the thrombin molecule

Lepirudin

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Incorporates into the growing viral DNA chain results in premature chain termination due to inhibition of binding with the incoming nucleotide, cytosine

Lamivudine (nucleoside analog of cytosine), Emtricitabine (fluorinated analog of lamivudine)

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complex of ferric oxyhydroxide with polymerized dextran; The complex must be phagocytized by (1) cells before iron becomes available

Iron dextran 1. reticuloendothelial

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inhibit incorporation of PABA into dihydropteroic acid interfering with folate metabolism

Sulfonamides: sulfamethoxazole and sulfadiazine

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binds DNA and chelates iron, leading to formation of free radicals that cause single- and double-strand DNA breaks

Bleomycin

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bind to antithrombin and accelerate the rate at which it inhibits various coagulation proteases, but less effective in inhibiting thrombin

Enoxaparin: low molecular weight heparin

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Delivered to transferrin more readily

Sodium Ferric gluconate and iron sucrose

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active triphosphate derivative inhibits DNA polymerase, DNA primase, DNA ligase, and ribonucleotide reductase, and is incorporated into DNA and RNA

Fludarabine (antimetabolite, purine analog)

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drugs bind β-tubulin blocking its ability to polymerize with α-tubulin into microtubules

Antimitotic drugs - Vincristine and vinblastine (vinca alkaloids)

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concentrates in parasite food vacuoles; increases free heme and toxicity to parasite

Amodiaquine

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Active drug = Cycloguanil, a triazine metabolite

Proguanil

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inhibits vitamin K epoxide reductase which is the enzyme that regenerates reduced vitamin K; action occurs in liver

warfarin

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inhibits synthesis of phosphoribosylamine by inhibiting phosphoribosylpyrophosphate synthetase and phosphoribosylpyrophosphate aminotransferase

Mercaptopurine (antimetabolite, purine analog)

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bind only to the active site of thrombin

Argatroban and dabigatran

bind competitively to plasminogen blocking the binding of plasminogen to fibrin and subsequent conversion fo plasmin

Aminocaproic acid; Tranexamic acid

The false nucleotide also causes DNA damage upon intercalation

Mercaptopurine (antimetabolite, purine analog)

"Erythrocytic forms of all four human malarial species Folate synthesis blockade ‐ selective ↓ of plasmodial dihydrofolate reductase activity"

Pyrimethamine Proguanil

displaces the repressor, activating the differentiation program, and promoting degradation of the PML-RAR- fusion gene

Tretinoin

"Active against hepatic-stage schizonts Gametocidal "

Primaquine

Blocks IL-1-induced metalloproteinase release from synovial fluid; used for RA patients

Anakinra

block the enzyme lanosterol 14-α-demethylase inhibiting the conversion of lanosterol to ergosterol

azoles

incorporation into RNA inhibits RNA function, RNA processing, and mRNA translation

Fludarabine (antimetabolite, purine analog)

Alkaloid from bark of cinchona tree Rapid-acting, highly effective schizonticide against all four human malaria parasites Gametocidal against P. vivax and P. ovale but not P. falciparum

Quinine and Quinidine

blocks calcineurin and inhibits IL-2, IL-3; IL-4, IFN-γ synthesis

Tacrolimus (FK506)

Incorporates into the growing viral DNA chain results in premature chain termination due to inhibition of binding with the incoming nucleotide, adenosine

Tenofovir (nucleotide analog of adenosine)

increases drug exposure, thereby prolonging the drug's half-life and allowing reduction in frequency; in addition, thegenetic barrier to resistance is raised

Ritonavir

reduced to tetrahydrofolic acid which acts as an acceptor of one-carbon units

folate

causes release of factor VIII and vWF from endogenous endothelial storage site

DDAVP (desmopressin)

inhibits fungal mitosis by interacting with polymerized microtubules

Griseofulvin

potent inhibitor of DNA polymerase, both in replication and repair; the triphosphate form competes with the physiological substrate deoxycytidine 5'-triphosphate (dCTP) for incorporation into DNA by DNA polymerases.

Cytarabine (antimetabolite, a cytidine analog)

bind directly to reverse transcriptase resulting in allosteric inhibition of RNA- and DNA-dependent DNA polymerase

Nonnucleoside: Efavirenz

vitamin K1 - found in green leafy vegetables

Phytonadione

causes a permanent conformational change in antithrombin

fondaparinux

block HIV-1 integrase activity, preventing viral DNA from integrating with cellular DNA

Integrase inhibitor: raltegravir

Binds specifically and selectively to CCR5

Penetration blocker: Maraviroc

competitively binds to the ATP binding site on the bcr-abl which inhibits phosphorylation of proteins involved in CML clone proliferation

Tyrosine kinase inhibitor - Imatinib

prodrug that is converted in the liver to MTIC which interrupts DNA replication by causing methylation of guanine

Dacarbazine

S-FKBP complex leads to inhibition of mTOR

sirolimus

inhibits dihydrofolate reductase

Methotrexate

have lympholytic effects and are able to suppress mitosis in lymphocytes

Glucocorticoids - Prednisone, Dexamethasone

inhibits reverse transcriptase by competing with endogenous deoxynucleotides (adenosine) for the catalytic site of the enzyme

Tenofovir (nucleotide analog of adenosine)

inosine monophosphate dehydrogenase (IMPDH) inhibitors, leading to inhibition of purine synthesis

MPA or MMF; (Mycophenolic Acid and Mycophenolate Mofetil)

oxidized to form reactive hydroxylamine; toxic to bone marrow precursors

dapsone

Also required for the active forms of proteins C and S

Phytonadione

"Disrupts plasmodia mitochondria electron transport Acts against Tissue/Erythrocytic schizonts"

"Atovaquone-proguanil aka Malarone"

Xa and IIa inhibitors

heparin and LMWH

production of free radicals following iron catalyzed cleavage of artemisinin endoperoxide bridge in the parasite’s food vacuole inhibition of parasite’s calcium ATPase

Artemisinin

Produced using recombinant DNA technology using cultured cells transfected with the human factor VIII/IX gene

Recombinant factor VIII/IX

catalyzes the hydrolysis of circulating asparagine to aspartic acid and ammonia depriving malignant cells of the asparagine necessary for protein synthesis, leading to cell death

Asparaginase

contain vitamin K-dependent factors II, VII, IX, and X, activated factor VII and IX

Prothrombin complex concentrate (PCC) and activated PCC (aPCC)

These drugs do not compete with nucleoside triphosphates nor require phosphorylation to be active

Nonnucleoside: Efavirenz

bind to antithrombin and accelerate the rate at which it inhibits various coagulation proteases

Unfractionated heparin and fondaparinux

biotransformed into false purine nucleotides which inhibit phosphoribosylpyrophosphate synthetase and phosphoribosylpyrophosphate aminotransferase

Mercaptopurine (antimetabolite, purine analog)

prevent post-translational cleavage of the Gag-Pol polyprotein by protease resulting in the production of immature, noninfectious viral particle

Protease inhibitors: Atazanavir, Darunavir, Ritonavir

potent CYP3A4 inhibitory properties used to "boost" the levels of other protease inhibitors when given in combination, thus acting as a pharmacokinetic enhancer rather than an antiretroviral agent

Ritonavir

Inhibits clot lysis for treatment of oral bleeding because of the high concentration of fibrinolytic enzymes found in saliva

Aminocaproic acid; Tranexamic acid

has a high affinity for ferric iron. Once bound with iron, it is excreted in the urine

Deferoxamine has a high affinity for ferric iron. Once bound with iron, feroxamine is excreted in the urine

Binds to the CD20 antigen on the surface of pre-B cells and mature B cells, resulting in the depletion of B cells from peripheral blood, lymph nodes, and bone marrow

Rituximab

highly reactive alkyl groups that forms covalent bonds between guanines resulting in cross-linking between two DNA strands. DNA cannot be replicated resulting in cell death

Cyclophosphamide

36 amino acid peptide which binds to gp41 inhibiting fusion of HIV with the target cell

Fusion inhibitor: Enfuvirtide

Antibodies against CD25 – the high affinity IL-2 receptor (CD25 – expressed only on activated T-cells)

Daclizumab and Basiliximab

selectively toxic because human cells do not contain β-(1,3)-D-glucan

echinocandins (capsofungin)

Antifibrinolytic

Aminocaproic acid; Tranexamic acid

Effective for patients with adequate endogenous stores of vWF

DDAVP (desmopressin)

selectively toxic because in human cells the major sterol is cholesterol rather than ergosterol

The polyenes, the azoles, and terbinafine

Directly interact with the thrombin molecule; Able to inhibit circulating and clotbound thrombin

Direct thrombin inhibitors: Lepirudin; Argatroban and dabigatran

Down-regulates expression of cytokines IL-1, IL-4 and TNF-α

Glucocorticoids

Binds to ergosterol in fungal cell membranes forming pores or channels

Polyenes: Amphotericin B

non-specific (binds TNF-α and TNF-β) and inhibits both – approved for rheumatoid arthritis

Etanercept

cell-cycle-specific agents blocking cells in mitosis (M phase). Cell division is arrested in metaphase.

Antimitotic drugs - Vincristine and vinblastine (vinca alkaloids)

↓Bacterial protein synthesis (also ↓Protein synthesis in plasmodial species)

Doxycycline

can form radical intermediates, which in turn can react with oxygen to produce superoxide anion radicals which attack DNA and oxidize DNA bases

Doxorubicin, daunorubicin - anthracyclines

integrase strand transfer inhibitor (INSTI)

Integrase inhibitor: raltegravir

blocks calcineurin and inhibits IL-2 synthesis

cyclosporine

inhibits reverse transcriptase by competing with endogenous deoxynucleotides (cytosine) for the catalytic site of the enzyme

Lamivudine (nucleoside analog of cytosine), Emtricitabine (fluorinated analog of lamivudine),

TNF-α-specific inhibitors - approved for rheumatoid arthritis, Crohn’s disease, ulcerative colitis

Infliximab and Adalimumab

Strong blood schizonticidal activity against P. falciparum and P. vivax

Mefloquine

Cofactor in the activation of factors II, VII, IX, and X

Phytonadione