-
Heparin
- - increases AT-III activity==> b/d of IXa, XIIa, XIIa, Xa and IIa
- - inhibit platelet aggregation
- - venous thrombosis, Pulm embolism, unstable angina, acute MI, ballon angioplasty
-
LMWH
- - Xa inihibitor
- - no effect on platelets
-
Fondaparinux
- - synthetic LMWH
- - Xa inhibitor
- - no effect on platelets
-
Lepirudin
- thrombin (IIa) inhibitor
-
Warfarin
- - VKOR (Vit K epoxide reductase inhibitor
- - inhibits formation of II, VII, IX and X
- - APC inhibitor (necrosis?)
- - highly protein bound
-
Drotecogrin- alpha
- - rAPC
- - Va and VIIIa inactivator
- - reduce mortality in septic pts
-
Dabigatran etixilate
- - competative thrombin (IIa) inhibitor
- - no antidote
- - prevents thrombin induced platelet aggregation and clot formation
-
Atelpase
- - plasminogen activator (to plasmin)
- - leads to fibrin degradation
- - MI and Ichemic stroke (within 3 hours) and pulmonayry thromboembolism
-
ASA
- - irreversible inactivation of COX1
- - inhibits synthesis of TXA2
-
Clopidigrel
- blocks ADP-r on platelets, so fibrin cannot bind, inhibitig aggregation
-
Abciximab
- Fab fragment against glucoprotein IIb/IIIa
-
Vitamin K
- - cofactor for VKOR
- - counteract warfarin toxicity, hemorrhagic disease of the newborn, hypoprothrombinemia
-
Thrombin
- - rIIa (rThrombin)
- - intraocular surgeries to control hemorrhaging
-
EACA/ Aminocaproic acid/ epsilon aminocaproic acid
- - competatively inhibits plasminogen activation
- - inhibits fibrinolysis
- - reduce hemorrhage in CABG
- - TOTAL C/I: DIC
-
protamine sulfate
- - binds heparin tightly, reversing its effect
- - after cardiac surgery
-
Proguanil
- sporontocidal produg
- effective against hepatic preerythrocytic forms of P falciparum and P vivax
- used with atovaquone for MDR faaciparum and vivax
-
Primaquine
- used for latent tissue (hyponozoite) forms of vivax and ovale with chloroquine, gametocytic.
- can also be used a prophylactic
- **C/I in G6PD deficiency (==>acute IV hemolysis and methemoglobinuria)**
-
chloroquine
- effective against INTRAerythrocytic forms of plasmodia by preventing heam (parasitic waste product) conversion
- inhibits actions of TNF-alpha, gametocytic (v, o, m)
- **A/E: convulsions and, at high doses, retinopathy and ototoxicity**
- safe prophylaxis for prego
-
Quinine
- prototypical blood schizonticide and gametocytic (vivax and malariae)
- prevent haem conversion (like chloroquine)
- **A/E: cinchonism, hypogly, hypoTN, thrombocytopenia**
- NO PREGO
-
pyrimethamine and sulfadioxine
3 uses
MOA
- prophylaxis of falciparum, combo with quinine to tx MDR falciparum, 2 doses for prego with chloro-R falciparum
- inhibits pDHFR
-
drugs that act on asexual erythrocytic stage of malarial infection to interrupt erythrocytic schizogony, thus terminating clinical attacks
6
- chloroquine, quinine, quinidine, mefloquine, doxycycline, artermisinin
- MADQCQ
-
Metronidazole
- tx of certain protozoa- amebiasis, trichomniasis, giadiasis, balantdiasis and hepatic abscess
- deprive anaerobe of reducing equivalents
- amplifies warfarin
- **metallic aftertaste, No EtOH (disulfiram- like effects) **
-
Nifurtimox
- tx of acute Chagas disease (prolonged therapy req'd)
- **seizures and polyneuritis**
- no early prego
-
Stibogluconate
- tx for leishmaniasis
- becomes highly toxic during therapy (cardiac toxicity!!)
-
Levamisole
- antiparasitic drug that stimulates maturation/proliferation of T cells- Dukes Stage C colon cancer
- **A/E: agranulocytosis**
-
BCG
non specific immunostimulant for the treatment of bladder cancer
-
Thalidomide
- used in leprosum and Chrons disease
- inhibits TNF-alpha production
-
INF- alfa
- enhances expression of MHC-I, decreases expression of MHC-II
- hairy cell leukemia, Hep B and C, HPV(imiquimod)
-
INF- beta
approved for MS
-
INF- gamma
- promotes CTL response
- tx CGD
- antiviral, proinflammatory, influences T cell subset differentiation
-
Aldesleukin
- r-IL-2
- promotes lymphoid cell differentiation-->CTLs and NK
- metastatic melanoma and metastatic renal cell carcinoma
-
Oprelvekin
- r- IL-11
- tx thrombocytopenia
-
Filgrastim
- G-CSF (granulocyte colony stimulating factor)
- increase n0 production
- stimulates bone marrow recovery during chemo
-
Sargramostim
- non lineage specific hematopoetic agent
- promotes myeloid recovery in high dose chemo patients:
- - Non-Hodgkins lymphoma
- - acute lymphoblastic leukemia (ALL)
- - Hodkins pts undergoing BM transplant
- - AIDS neutropenia
- **C/I in HF, pulm edema, yeast allergy**
-
-
Epoetin-alfa
- r- erythropoetin
- tx of anemia
- adequate Fe intake is required
-
Thrombopoetin
- selectively stimulates megakaryocytopoesis
- tx anemia, neutropenia and thrombocytopenia in high dose chemo and platelet recovery in hematopeitic stem cell transplant
-
Azathiprine
use
MOA
- antimetabolite of purine synthesis that is indiscriminately toxic to dividing cells, PRPP inhibitor
- tx to prevent graft rejection, AID (SLE, RA,etc), T4HS
- prevents clonal expansion (B and T), prevent de novo purine syn, inhibit S phase in all cells
- **interaction with allopurinol** (mercaptopurine accum)
-
mercaptopurine
- PRPP inhibitor
- tx some cancers and as an immunosuppressant
- utilizes XO, so concaminent use of allopurinol may result in toxic levels of MP
-
antilymphocytic globulin (ALG)
- anti-Tcell horse Ig
- used to treat acute rejection of kidney t/p, prevent rejection following kidney t/p, prevent GVHD in BM t/p, treat aplastic anemia
- **A/E: anaphylaxis (T1HS) and serum sickness: T3HS- fever, rash, joint pain
-
Rho (D) Ig
- prevention of hemolytic disease of the newborn
- given to Rh- pregos
-
Immune Globulin (IVIG)
- polyclonal human Ig (mostly IgG)
- tx Kawasaki's disease, subacute SLE, thrombocytopenic purpure
-
Muronab
- - anti-CD3 Ig of thymocytes and primed T-cells
- - use: acute renal allograft rejection, esp when corticosteroid therapy is not working
- **A/E: cytokine release syndrome, pulmonary edema (avoid in hypervolemic pt), blood dyscrasias**
-
cyclosporine
- calcineurin inhibitor (prevents activation (de-P of TF NF-AT-------X----> IL-2 t/s) (binds cyclophilin)
-
use: prevent t/p rejection (must be used before t/p performed), treat GVHD, uveitis, severe psoriasis - very hydrophobic and hard to solublize
- **nephrotoxic**
-
Tacrolimus
- -macrolide Abx that prevents IL-2 t/s
- - used as cyclosporine substitue to prevent transplant rejection, also used topically for atopic dermatitis
- **seizures, nephro/neuro-toxicity**
-
Sirolimus
- macrocytic lactone- immunosuppressive
- acts like cyclosporine by preventing IL-2 t/s
- inhibits mammalian kinase mTOR (molecular tgt of rapamycin)
- NOT nephroxic
-
mycophenolate
- prodrug converted to mycophenolic acid
- inhibitor of inosine monophosphate dehydrogenase (guanine synthese RLS)
- prevent allogenic graft rejection, SLE
- selectively inhibits T and B proliferation and function
- **A/E: leukopenia, neutropenia, cytomegalo sepsis
- used INSTEAD of azothoiprine in immunosuppression
-
Etanercept
- TNF-alpha FUSION PROTEIN (prevents action)
- tx: RA, cancer (with methotrexate), psoriasis, immunosupp
-
Infliximab
- anti-TNF-alpha Ig (prevents binding)
- tx: RA and Chrons
- **C/I: infections, sepsis, chronically immunosuppressed**
-
Daclizumab
- binds IL-2 receptor, preventing CD4 Tcell activation
- tx: acute transplant rejection
- **A/E: dyspnea, fever, GI distress, hypoTN, HTN, angina**
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