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Hemotologic Drugs

Anemia Theraputics

Oral preparations

Ferrous sulfate

Ferrous gluconate

Ferrous fumarate

* Iron is absorbed in the duodenum and proximal ileum,

so it is important that these supplements be taken on

an empty stomach, and not given in enteric-coated

preparations!

Parental preparations

Iron dextran -- used to treat iron def. after GI resections

in IBD involving the proximal bowel.

Iron Chelator

Desferal -- used in iron toxicity

Drugs which alter Folate Metabolism

Dihydrofolate reductase inhibitors

Trimethoprim

Pyrimethamine

Methotrexate

Inhibitors of folate absorption

Anticonvulsants

Oral contraceptives

Isoniazid

Coagulation Basics

Platelet aggregators

Collagen

Thromboxane

Thrombin

* Prostacyclin (PGI

2

) is an inhibitor of platelet

aggregation

* White thrombi form in arteries (platelets and fibrin)

* Red thrombi form in veins (mainly fibrin, w/ trapped

platelets and RBCs)

* PTT is used to measure integrity of the intrinsic pathway

* PT is used to measure integrity of the extrinsic pathway

* Intrinsic pathway begins with activation of factor XII

by collagen

* Extrinsic pathway begins with activation of factor VII

by tissue thromboplastin

Protease inhibitors

1

2

-antitrypsin

-macroglobulin

2

-antiplasmin antithrombin III

Antithrombogenics

Platelet inhibitors

Aspirin -- irreversible inhibitor of cyclooxygenase

Ticlopidine -- inhibits ADP-induced platelet aggregation

Dipyridamole -- potentiates the effects of Prostacyclin

Sulfinpyrazone

Anticoagulants

Heparin -- NOT administered IM; only IV or SQ; binds to

antithrombin III & increases its actions; use

to prolong PTT; does not cross placenta

Warfarin -- can be give orally; inhibits Vit. K epoxide

reductase; use to prolong PT; will cross the

placenta

Dextran -- used to prevent postop venous thrombosis

* Heparin overdose is treated with protamine sulfate

* Warfarin overdose is treated with Vitamin K

Drugs that alter Warfarin’s effects

P-450 inducers(attenuate): P-450 inhibitors(potentiate):

Barbiturates

Glutethimide

Griseofluvin

Phenytoin

Amiodarone

Cimetidine

Chloramphenicol

Cotrimoxazole

Disulfiram

Metronidazole

Miconazole

Phenylbutazone

Sulfinpyrazone

Trimethoprim/sulfa

Rifampin

Thrombolytic agents

Tissue plasminogen activator (TPA) -- preferentially

activates plasmin in thrombi, and not

free plasmin

Streptokinase -- activates plasma plasmin

Anistreplase -- also activates plasmin in thrombi and

not free plasmin; longer 1/2-life than the

others

Urokinase -- activates plasma plasmin

Fibrinolytic inhibitors

Antiplasmins

Aminocaproic acid

Tranexamic acid

Hemophilia drugs

Desmopressin acetate

Danazol -- both of these increase factor VIII activity

Immunopoietic Drugs

Immunosuppressive Drugs

Corticosteroids

Prednisone -- these are non-toxic to marrow stem cells

Dexamethasone

Cytotoxic agents

Azathioprine -- an antimetabolite; toxicity is augmented

by renal disease and inhibitors of Xanthine oxidase;

will suppress marrow function; used in kidney

transplants

AZT

Cyclophosphamide -- alkylating agent; used in bone

marrow transplantation

Cytarabine

Dactinomycin

Methotrexate -- used in prophylatic treatment of GVH disease

Vincristine

Macrolide antibiotics

Cyclosporin A -- blocks the differentiation & activation rejection;

of T-cells; used to suppress organ

metabolism is blocked by erythromycin

or ketoconazole

Tacrolimus (FK-506) -- used when cyclosporin is too toxic

or ineffective

Immunosuppressive Antibodies

Anti-T-cell antibody (OKT3) -- used in kidney transplants

Antithymocyte globulin -- used to treat idiopathic aplastic anemia

Antilymphocyte globulin -- activates complement-

Rh

0 mediated destruction of lymphocytes; used in organ transplantation and GVH disease

(D) immune globulin -- Used in prophylactic treatment of Rh hemolytic disease (Erythroblastosis fetalis)

Immunomodulating Agents

Thymosin -- produced by thymus; induces the maturation

of T-cells; thymosin levels decrease w/ age

Levamisole -- enhances cellular immunity; potential uses

include Hodgkin’s disease and rheumatoid

arthritis

Inosiplex -- enhances T-cell and monocyte cytotoxicity;

may be useful in treatment of AIDS

Interleukins -- work in different ways to stimulate and

suppress leukocyte proliferation and function

Interferons (  ,  ,  ) -- display antiviral properties; IFN has been approved for the treatment of hepatitis and hematologic neoplasms

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