Usmle - Heme Drugs

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Ticlopidine

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Inhibits platelet aggregation by irreversibly blocking ADP receptors. Inhibits fibrinogen binding by preventing glycoprotein IIb/IIIa expression.

Used for acute coronary syndrome; coronary stenting; decreased incidence or recurrence of thombotic stroke.

Toxicity includes neutropenia.

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Clopidogrel

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Inhibits platelet aggregation by irreversibly blocking ADP receptors. Inhibits fibrinogen binding by preventing glycoprotein IIb/IIIa expression.

Used for acute coronary syndrome; coronary stenting; decreased incidence or recurrence of thombotic stroke

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Abciximab

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Monoclonal antibody that binds to the glycoprotein receptor IIb/IIIa on activated platelets, preventing aggregation.

Clinically used for non-ST elevated acute coronary syndromes, percutaneous transluminal coronary angioplasty.

Toxicity includes bleeding and thrombocytopenia.

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Tirofiban

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Monoclonal antibody that binds to the glycoprotein receptor IIb/IIIa on activated platelets, preventing aggregation.

Clinically used for non-ST elevated acute coronary syndromes, percutaneous transluminal coronary angioplasty.

Toxicity includes bleeding and thrombocytopenia.

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Eptifibatide

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Monoclonal antibody that binds to the glycoprotein receptor IIb/IIIa on activated platelets, preventing aggregation.

Clinically used for non-ST elevated acute coronary syndromes, percutaneous transluminal coronary angioplasty.

Toxicity includes bleeding and thrombocytopenia.

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Streptokinase

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Directly or indirectly aid conversion of plasminogen to plasmin, which cleaves thrombin and fibrin clots. Increases PT, PTT, but no change in platelet count.

Clinically used for early MI (ST elevated only), early ischemic stroke.

Toxicity includes bleeding; contraindicated in patients with active bleeding, history of intracranial bleeding, recent surgery, known bleeding diatheses, or severe hypotension. Treat toxicity with aminocaproic acid, an inhibitor of fibrinolysis.

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Urokinase

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Directly or indirectly aid conversion of plasminogen to plasmin, which cleaves thrombin and fibrin clots. Increases PT, PTT, but no change in platelet count.

Clinically used for early MI (ST elevated only), early ischemic stroke.

Toxicity includes bleeding; contraindicated in patients with active bleeding, history of intracranial bleeding, recent surgery, known bleeding diatheses, or severe hypotension. Treat toxicity with aminocaproic acid, an inhibitor of fibrinolysis.

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tPA (alteplase)

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Directly or indirectly aid conversion of plasminogen to plasmin, which cleaves thrombin and fibrin clots. Increases PT, PTT, but no change in platelet count.

Clinically used for early MI (ST elevated only), early ischemic stroke.

Toxicity includes bleeding; contraindicated in patients with active bleeding, history of intracranial bleeding, recent surgery, known bleeding diatheses, or severe hypotension. Treat toxicity with aminocaproic acid, an inhibitor of fibrinolysis.

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APSAC (anistreplase)

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Directly or indirectly aid conversion of plasminogen to plasmin, which cleaves thrombin and fibrin clots. Increases PT, PTT, but no change in platelet count.

Clinically used for early MI (ST elevated only), early ischemic stroke.

Toxicity includes bleeding; contraindicated in patients with active bleeding, history of intracranial bleeding, recent surgery, known bleeding diatheses, or severe hypotension. Treat toxicity with aminocaproic acid, an inhibitor of fibrinolysis.

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Aminocaproic acid

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Inhibitor of fibrinolysis; used to treat toxicity of streptokinase, urokinase, tPA, or APSAC.

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Methotrexate

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Antineoplastic - antimetabolite; folic acid analog that inhibits dihydrofolate reductase, decreasing dTMP, and decreasing DNA and protein synthesis.

Used to treat cancers (leukemias, lymphomas, choriocarinoma, and sarcomas) and also used in abortion, ectopic pregnancy, rheumatoid arthritis, and psoriasis.

Toxicity includes myelosuppression, which is reversible with leucovorin (folinic acid) "rescue", macrovesicular fatty change in liver, mucositis, teratogenic, and can cause a fibrotic lung disease.

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5-fluorouracil (5-FU)

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Antineoplastic - antimetabolite; pyrimidine analogue bioactivated to 5F-dUMP, which covalently complexes folic acid. This complex inhibits thymidylate synthase, decreasing dTMP, decreasing DNA and protein synthesis.

Used for colon cancer and other sold tumors, basal cell carcinoma (topical), and actinokeratosis. Has synergy with methotrexate.

Toxicity includes myelosuppression (not reversible with leucovorin); overdose is "rescued" with thymidine; photosensitivity.

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6-mercaptopurine (6-MP)

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Antineoplastic - antimetabolite; purine (thiol) analog; decreases de novo purine synthesis. Activated by HGPRTase. Inhibits PRPP synthesis.

Clinically used for leukemias, lymphomas (not CLL or Hodgkin's).

Toxicity includes bone marrow, GI, and liver. Metabolized by xanthine oxidase; thus increased toxicity with allopurinol.

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6-thioguanine (6-TG)

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Antineoplastic - antimetabolite; same mechanism as 6-MP; purine (thiol) analog; decreases de novo purine synthesis. Activated by HGPRTase. Inhibits PRPP synthesis.

Clinically used for acute lymphoid leukemia.

Toxicity includes bone marrow depression and liver; can be given with allopurinol.

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Cytarabine (ara-C)

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Antineoplastic - antimetabolite; pyrimidine antagonist which inhibits DNA polymerase.

Used for AML, ALL, high grade non-Hodgkin's lymphoma.

Toxicity includes leukopenia, thrombocytopenia, and megaloblastic anemia.

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Dactinomycin

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Antineoplastic - antitumor; intercalates in DNA.

Used for Wilms' tumor, Ewing's sarcoma, rhabdomyosarcoma. Used for childhood tumors (children ACT out).

Toxicity includes myelosuppression.

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Doxorubicin

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Antineoplastic - antitumor; generates free radicals. Noncovalently intercalate in DNA, breaks DNA, and decreases replication.

Used for Hodgkin's lymphoma, myelomas, sacromas, and solid tumors (breast, ovary, lung).

Toxicity includes cardiotoxicity (dilated cardiomyopathy), myelosuppression, alopecia. Toxic to tissues with extravasation.

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Daunorubicin

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Antineoplastic - antitumor; generates free radicals. Noncovalently intercalate in DNA, breaks DNA, and decreases replication.

Used for Hodgkin's lymphoma, myelomas, sacromas, and solid tumors (breast, ovary, lung).

Toxicity includes cardiotoxicity (dilated cardiomyopathy), myelosuppression, alopecia. Toxic to tissues with extravasation.

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Bleomycine

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Antineoplastic - antitumor; G2 phase specific. Induces formation of free radicals, which cause breaks in DNA strands.

Used for testicular cancer, Hodgkin's lymphoma.

Toxicity includes pulmonary fibrosis, skin changes, but minimal myelosuppression.

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Etoposide (VP-16)

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Antineoplastic - antitumor; late S to G2 phase specific; inhibits topoisomerase II, causing increased DNA degeneration.

Clinically used for small cell carcinoma of the lung and prostate, testicular carcinoma.

Toxicity includes myelosuppression, GI irritation, and alopecia.

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Teniposide

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Antineoplastic - antitumor; late S to G2 phase specific; inhibits topoisomerase II, causing increased DNA degeneration.

Clinically used for small cell carcinoma of the lung and prostate, testicular carcinoma.

Toxicity includes myelosuppression, GI irritation, and alopecia.

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Cyclophosphamide

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Antineoplastic - alkylating; covalently X-linked (interstrand) DNA at guanine N-7; require bioactivation by liver.

Used clinically for non-Hodgkin's lymphoma, breast and ovarian carcinomas. Also immunosuppressant.

Toxicity includes myelosuppression, HEMORRHAGIC CYSTITIS (prevented with MESNA).

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Mesna

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Used to prevent hemorrhagic cystitis caused by cyclophosphamide or ifosfamide.

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Ifosfamide

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Antineoplastic - alkylating; covalently X-linked (interstrand) DNA at guanine N-7; require bioactivation by liver.

Used clinically for non-Hodgkin's lymphoma, breast and ovarian carcinomas. Also immunosuppressant.

Toxicity includes myelosuppression, HEMORRHAGIC CYSTITIS (prevented with MESNA).

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Carmustine

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Antineoplastic - alkylating; nitrosurea; require bioactivation. Cross blood-brain barrier - CNS activity.

Clinically used for brain tumors (including glioblastoma multiforme).

Toxicity includes CNS issues (dizziness, ataxia).

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Lomustine

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Antineoplastic - alkylating; nitrosurea; require bioactivation. Cross blood-brain barrier - CNS activity.

Clinically used for brain tumors (including glioblastoma multiforme).

Toxicity includes CNS issues (dizziness, ataxia).

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Semustine

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Antineoplastic - alkylating; nitrosurea; require bioactivation. Cross blood-brain barrier - CNS activity.

Clinically used for brain tumors (including glioblastoma multiforme).

Toxicity includes CNS issues (dizziness, ataxia).

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Streptozocin

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Antineoplastic - alkylating; nitrosurea; require bioactivation. Cross blood-brain barrier - CNS activity.

Clinically used for brain tumors (including glioblastoma multiforme).

Toxicity includes CNS issues (dizziness, ataxia).

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Busulfan

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Antineoplastic - alkylating; alkylates DNA.

Clinically used for CML; also used for ablating bone marrow in hematopoietic stem cell transplants.

Toxicity includes pulmonary fibrosis and hyperpigmentation.

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Vincristine

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Antineoplastic - microtubule inhibitor; alkaloid that binds to tubulin in M phase and BLOCKS POLYMERIZATION OF MICROTUBULES so that mitotic spindle cannot form. Microtubules are the vines of your cells.

Clinically used for Hodgkin's lymphoma, Wilm's tumor, and choriocarcinoma.

Toxicity includes neurotoxicity (areflexia, peripheral neuritis), paralytic ileus.

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Vinblastine

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Antineoplastic - microtubule inhibitor; alkaloid that binds to tubulin in M phase and BLOCKS POLYMERIZATION OF MICROTUBULES so that mitotic spindle cannot form. Microtubules are the vines of your cells.

Clinically used for Hodgkin's lymphoma, Wilm's tumor, and choriocarcinoma.

BLASTs the Bone marrow.

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Paclitaxel

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Antineoplastic - microtubule inhibitor; hyperstablizes polymerized microtubules in M phase so that mitotic spindle cannot break down (anaphase cannot occur).

Used for ovarian and breast carcinomas.

Toxicity includes myelosuppression and hypersensitivity.

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Cisplatin

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Antineoplastic; cross links DNA.

Clinically used for testicular, bladder, ovary, and lung carcinomas.

Toxicity includes nephrotoxicity and acoustic nerve damage.

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Carboplatin

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Antineoplastic; cross links DNA.

Clinically used for testicular, bladder, ovary, and lung carcinomas.

Toxicity includes nephrotoxicity and acoustic nerve damage.

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Hydroxyurea

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Antineoplastic; inhibits ribonucleotide reductase; decreases DNA synthesis (S phase specific).

Clinically used for melanoma, CML, and sickle cell disease (increases HbF).

Toxicity includes bone marrow suppression, GI upset.

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Prednisone

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Antineoplastic; may trigger apoptosis. May even work on nondividing cells.

Most commonly used glucocorticoid in cancer chemotherapy. Used in CLL, Hodgkin's lymphomas. Also an immunosuppressant used in autoimmune diseases.

Toxicity includes Cushing like symptoms; immunosuppression, cataracts, acne, osteoporosis, hypertension, peptic ulcers, hyperglycemia, and psychosis.

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Tamoxifen

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Antineoplastic; SERM - selective antagonist in breast, agonist in bone; block the binding of estrogen to estrogen receptor positive cells.

Clinically used in breast cancer (if estrogen receptor positive). Also useful to prevent osteoporosis.

May increase the risk of endometrial via partial agonist effects; "hot flashes".

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Raloxifene

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Antineoplastic; SERM - selective antagonist in breast, agonist in bone; block the binding of estrogen to estrogen receptor positive cells.

Clinically used in breast cancer (if estrogen receptor positive). Also useful to prevent osteoporosis.

Does not cause endometrial carcinoma because it is an endometrial antagonist.

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Trastuzumab

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Antineoplastic; monoclonal antibody against HER-2 (erb-B2). Helps kill breast cancer cells that overexpress HER-2, possibly through antibody dependent cytotoxicity.

Clinically used for metastatic breast cancer.

Toxicity includes cardiotoxicity.

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Imatinib

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Antineoplastic; Philadelphia chromosome bcr-abl tyrosine kinase inhibitor.

Clinically used for CML, GI stromal tumors, and any Phl + tumors (some ALL, etc).

Toxicity includes fluid retention.

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What drugs interfere with microtubules?

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Bendazoles, taxols, griseofulvin, vincristine, vinblastine, and colchicine

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What drugs are nephrotoxic and ototoxic?

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Cisplastin, carboplatin, vancomycin, aminoglycosides, and loop diuretics

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Heparin

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Cofactor for the activation of antithrombin; decreases thrombin and Xa. Short half life.

Used for immediate anticoagulation for pulmonary embolism, stroke, acute coronary syndrome, MI, DVT. Used during pregnancy (does not cross placenta). Follow PTT.

Toxicity includes bleeding, HIT, osteoporosis, drug-drug interactions. Use protamine sulfate to reverse heparinization.

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Lepirudin

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Hirudin derivatives; directly inhibit thrombin. Used as an alternative to heparin for anticoagulating patients with HIT.

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Bivalirudin

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Hirudin derivatives; directly inhibit thrombin. Used as an alternative to heparin for anticoagulating patients with HIT.

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Argatroban

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Directly inhibit thrombin. Used as an alternative to heparin for anticoagulating patients with HIT.

Not a hirudin derivative

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Warfarin

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Interferes with normal synthesis and gamma-carboxylation of vitamin K dependent clotting factors 2, 7, 9, 10, and protein C and S. Metabolized by cytochrome P-450. In laboratory assay, has effect on extrinsic pathway and increases PT. Long half life.

Use for chronic anticoagulation. Not used in pregnancy. Follow PT/INR values.

Toxicity includes bleeding, teratogenic, skin/tissue necrosis, drug-drug interactions.