USMLE (Fach) / Pharmacology - Hematology and Oncology (Lektion)
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- Heparin Mechanism: Activates antithrombin, which ↓ the activity of IIa (thrombin) and factor Xa.- Short half-life. Clinical use:- Immediate anticoagulation for pulmonary embolism (PE)- Acute coronary syndrome, ...
- Bivalirudin Mechanism: Direct thrombin inhibitor Clinical use: - Venous thromboembolism- Atrial fibrillation- can be used in HIT Adverse effects: Bleeding; no specific reversal agent.
- Warfarin Interferes with γ-carboxylation of vitamin K-dependent clotting factors II, VII, IX, and X, and proteins C and S. Metabolism affected by polymorphisms in the gene for vitamin K epoxide reductase complex ...
- Apixaban Mechanism: Direct factor Xa inhibitor Clinical use:- Treatment and prophylaxis for DVT and PE- Stroke prophylaxis in patients with atrial fibrillation - Oral agents do not usually require coagulation ...
- Rivaroxaban Mechanism: Direct factor Xa inhibitor Clinical use:- Treatment and prophylaxis for DVT and PE- Stroke prophylaxis in patients with atrial fibrillation - Oral agents do not usually require coagulation ...
- Thrombolytics Alteplase (tPA), reteplase (rPA), streptokinase, tenecteplase (TNK-tPA) Mechanism: Aid conversion of plasminogen to plasmin, which cleaves thrombin and fibrin clots.↑ PT, ↑ PTT, no change in platelet ...
- ADP receptor inhibitors Clopidogrel, prasugrel, ticagrelor (reversible), ticlopidine Mechanism: Inhibit platelet aggregation by irreversibly blocking ADP (P2Y12) receptors. Prevent expression of glycoproteins IIb/IIIa on platelet ...
- Cilostazol Mechanism: Phosphodiesterase III inhibitor; ↑ cAMP in platelets, resulting in inhibition of platelet aggregation; vasodilator. Clinical use: - Intermittent claudication- Coronary vasodilation- Prevention ...
- Glycoprotein IIb/IIIa inhibitors Abciximab, eptifibatide, tirofiban Mechanism: Bind to the glycoprotein receptor IIb/IIIa on activated platelets, preventing aggregation. - Abciximab is made from monoclonal antibody Fab fragments. Clinical ...
- Vemurafenib Small molecule inhibitor of BRAF oncogene ⊕ melanoma V600E-mutated BRAF inhibition Clinical use: Metastatic melanoma
- Trastuzumab (Herceptin) Monoclonal antibody against HER-2 (c-erbB2), a tyrosine kinase receptor. Helps kill cancer cells that overexpress HER-2 through inhibition of HER-2 initiated cellular signaling and antibody-dependent ...
- Tamoxifen, raloxifene Selective estrogen receptor modulators (SERMs) – receptor antagonists in breast and agonist in bone. Block the binding of estrogen to ER ⊕ cells. Clinical use: Breat cancer treatment (tamoxifen only) ...
- Rituximab Monoclonal antibody against CD20, which is found on most B-cell neoplasms Clinical use: Non-Hodgkin lymphoma, CLL, ITP, rheumatoid arthritis Adverse effects: ↑ risk of progressive multifocal leukoencephalopathy ...
- Imatinib Tyrosine kinase inhibitor of BCR-ABL (Philadelphia chromosome fusion gene in CML) and c-kit (common in GI stromal tumors) Clinical use: CML, GI stromal tumors Adverse effects: Fluid retention
- Cetuximab Monoclonal antibody against EGFR. Clinical use: Stage IV colorectal cancer (wild-type KRAS), head and neck cancer Adverse effects:- Rash- Elevated LFTs- Diarrhea
- Erlotinib EGFR tyrosine kinase inhibitor Clinical use: Non-small cell lung carcinoma Adverse effects: Rash
- Bevacizumab Monoclonal antibody against VEGF. Inhibits angiogenesis. Clinical use: Solid tumors (colorectal cancer, renal cell carcinoma), wet age-related macular degeneration. Adverse effects:- Hemorrhage- Blood ...
- Prednisone, prednisolone Clinical use:- most commonly used glucocorticoids in cancer chemotherapy- used in CLL, non-Hodgkin lymphoma- also used as immunosuppressants Adverse symptoms: Cushing-like symptoms, weight gain, central ...
- Hydroxyurea Inhibits ribonucleotide reductase → ↓ DNA synthesis Clinical use: Myeloproliferative disorders (eg, CML, polycythemia vera), sickle cell disease (HbF ↑) Adverse effects: Myelosuppression
- Irinotecan, topotecan Inhibit topoisomerase I and prevent DNA unwinding and replication. Clinical use: - Colon cancer (irinotecan)- Ovarian and small cell lung caners (topotecan) Adverse effects: Severe myelosuppression, diarrhea ...
- Etoposide, teniposide Inhibit topoisomerase II → ↑ DNA degradation Clinical use: Solid tumors (particularly testicular and small cell cancer), leukemias, lymphomas Adverse effects: Myelosuppression, alopecia
- Cisplatin, carboplatin Cross-link DNA Clinical use: Testicular, bladder, ovary, and lung carcinomas Adverse effects: Nephrotoxicity, peripheral neuropathy, ototoxicity.- Prevent nephrotoxicity with amifostine (free radical ...
- Paclitaxel, other taxols Hyperstabilize polymerized microtubules in M phase so that mitotic spindle cannot break down (anaphase cannot occur). Clinical use: Ovarian and breast carcinomas Adverse effects:- Myelosuppression- Neuropathy- ...
- Vincristine, vinblastine Vinca alkaloids that bind β-tubulin and inhibit its polymerization into microtubules → prevent mitotic spindle formation (M-phase arrest). Clinical use:- Solid tumors- Leukemias- Hodgkin (vinblastine) ...
- Bleomycin Antitumor antibiotic. Induces free radical formation → breaks DNA strands Clinical use: Testicular cancer, Hodgkin lymphoma Adverse effects: - Pulmonary fibrosis- Skin hyperpigmentation- Minimal myelosuppression ...
- Dactinomycin (actinomycin D) Antitumor antibiotic. Intercalates in DNA, preventing RNA synthesis. Clinical use: Used for childhood tumors.- Wilms tumor- Ewing sarcoma- Rhabdomyosarcoma Adverse effects: Myelosuppression
- Busulfan Alkylating agent. Cross-links DNA. Clinical use: Used to ablate patient's bone marrow before bone marrow transplantation. Adverse effects: Severe myelosuppression (vs bleomycin), pulmonary fibrosis, hyperpigmentation. ...
- Cyclophosphamide, ifosfamide Alkylating agent. Cross-link DNA at guanine. Require bioactivation by liver. A nitrogen mustard. Clinical use: Solid tumors, leukemia, lymphomas Adverse effects:- Myelosuppression- SIADH- Metabolized ...
- Nitrosoureas Carmustine, lomustine, semustine, streptozocin. Alkylating agent.Require bioactivation. Cross blood-brain barrier → CNS. Cross-link DNA. Clinical use: Brain tumors (including glioblastoma multiforme) ...
- Azathioprine, 6-mercaptopurine Purine (thiol) analogs → ↓ de novo purine synthesis. Activated by HGPRT. Azothioprine is metabolized into 6-MP. Clinical use:- Preventing organ rejection- Rheumatoid arthritis, IBD, SLE- Used to ...
- Cladribine Purine analog → inhibition of DNA polymerase, DNA strand breaks Clinical use: Hairy cell leukemia Adverse effects:- Myelosuppression- Nephrotoxicity- Neurotoxicity
- 5-fluorouracil Pyramidine analog bioactivated to 5-FdUMP, which covalently complexes with thymidylate synthase and folic acid. This complex inhibits thymidylate synthase → ↓ dTMP → ↓ DNA synthesis.- Capecitabine ...
- Methotrexate Folic acid analog that competitively inhibits dihydrofolate reductase → ↓ dTMP → ↓ DNA synthesis. Clinical use:- Cancers: leukemias (ALL), lymphomas, choriocarcinoma, sarcomas- Non-neoplastic: ...
- Ticagrelor ADP receptor inhibitor (reversible)
- Ticlopidine ADP receptor inhibitor Adverse effect: Neutropenia
- Clopidogrel ADP receptor inhibitor
- Dipyridamole Mechanism: Phosphodiesterase III inhibitor; ↑ cAMP in platelets, resulting in inhibition of platelet aggregation; vasodilator. Clinical use: - Intermittent claudication- Coronary vasodilation- Prevention ...
- Abciximab Glycoprotein IIb/IIIa inhibitor - Made from monoclonal antibody Fab fragments Clinical use: - Unstable angina- Percutaneous transluminal coronary angioplasty Adverse effects:- Bleeding- Thrombocytopenia ...
- Eptifibatide Glycoprotein IIb/IIIa inhibitor Clinical use: - Unstable angina- Percutaneous transluminal coronary angioplasty Adverse effects:- Bleeding- Thrombocytopenia
- Tirofiban Glycoprotein IIb/IIIa inhibitor Clinical use: - Unstable angina- Percutaneous transluminal coronary angioplasty Adverse effects:- Bleeding- Thrombocytopenia
- Doxorubicin, daunorubicin Antitumor antibiotic.Generate free radicals. Intercalate in DNA → breaks DNA → ↓ replication. Interferes with topoisomerase II. Clinical use: Solid tumors, leukemias, lymphomas Adverse effects:- ...
- Argatroban Direct thrombin inhibitor Clinical use:- Venous thromboembolism- Atrial fibrillation- Can be used in HIT Does not require lab monitoring.
- Dabigatran Direct thrombin inhibitor Clinical use:- Venous thromboembolism- Atrial fibrillation- Can be used in HIT Does not require lab monitoring. Can be reversed with idarucizumab.
- Bortezomib Proteasome inhibitor, induce arrest at G2-M phase and apoptosis. Clinical use: - Multiple myeloma- Mantle cell lymphoma Adverse effects:- Peripheral neuropathy- Herpes zoster reactivation
- Carfilzomib Proteasome inhibitor, induce arrest at G2-M phase and apoptosis. Clinical use: - Multiple myeloma- Mantle cell lymphoma Adverse effects:- Peripheral neuropathy- Herpes zoster reactivation
- Rasburicase Recombinant uricase that catalyzes metabolism of uric acid to allantoin. Clinical use: Prevention and treatment of tumor lysis syndrome.
- Drugs that affect warfarin metabolism CYP-450 Inhibitors (↑ warfarin effect):- Antibiotics/antifungals- Acetaminophen, NSAIDs- Amiodarone- Cimetidine- Cranberry juice, vitamin E- Omeprazole- Thyroid hormone- SSRIs (eg, fluoxetine) CYP-450 ...
- Direct thrombin inhibitors Bivalirudin (related to hirudin, the anticoagulant used by leeches), argatroban, dabigatran (only oral agent in class). Directly inhibits activity of free and clot-associated thrombin. Clinical use:- ...
- Cytarabine (arabinofuranosyl cytidine) Pyrimidine analog → DNA chain termination. At higher concentrations, inhibits DNA polymerase. Use: Leukemias (AML), lymphomas Adverse effect: Myelosuppression with megloblastic anemia
- Procarbazine Cell cycle phase-nonspecific alkylating agent. Mechanism not yet defined. Mechanism: Hodgkin lymphoma, brain tumors. Adverse effects:- Bone marrow suppression- Pulmonary toxicity- Leukemia