First Aid Hematology and Oncology-Pharmacology

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Heparin MOA
Cofactor for activation of antithrombin. Decreases thrombin and factor Xa.
Clinical use, heparin
Immediate anticoagulation for PE, acute coronary syndrome, MI, DVT. Used during pregnancy (doesn’t cross placenta). Follow PTT.
Toxicity, heparin
Bleeding, thrombocytopenia (HIT), osteoporosis, drug-drug interactions.
Antidote, heparin?
Antidote=protamine sulfate (positively-charged, binds negatively-charged drug)
Enoxaparin, dalteparin
Low weight molecular heparins
Low molecular weight heparins (enoxaparin, dalteparin)
Heparins that act more on factor Xa, have better bioavailability and longer half life. Can be given subQ and no lab monitoring necessary. Not easily reversible.
Heparin induced thrombocytopenia (HIT)
Development of IgG abs against heparin bound to platelet factor 4 (PF4). Antibody-heparin PF4 complex activates platelets–>thrombosis and thrombocytopenia
Lepirudin, bivalirudin
Derivatives of hirudin, the anticoagulant used by leeches; inhibit thrombin. Alternative to heparin for anticoagulating patients with HIT.
Warfarin MOA
Interferes with normal synthesis and gamma carboxylation of vitamin K dependent clotting factors II, VII, IX and X and proteins C and S. Metabolized by cytochrome P-450 pathway. In lab, has effect on extrinsic pathway and increases PT (The EX-PresidenT went to war(farin)).
Use, warfarin
Used in chronic anticoagulation. Not used in pregnant women because can cross the placenta.
PT/INR values, warfarin
What labs should be followed during warfarin ttmt?
Toxicity, warfarin
Bleeding, teratogenic, skin/tissue necrosis, drug-drug interactions
Reversal of warfarin
Reversal: vitamin K
Rapid reversal of severe overdose: fresh frozen plasma
Alteplase
A thrombolytic, tPA
Reteplase
A thrombolytic, rPA
Tenecteplase
Thrombolytic, TNK-tPA
Alteplase, reteplase, tenecteplase
Name the thrombolytics
Thrombolytics
Directly or indirectly aid conversion of plasminogen to plasmin, which cleaves thrombin and fibrin clots. Increased PT and PTT, no change in platelet count.
Uses of thrombolytics?
Uses: Early MI, early ischemic stroke, direct thrombolysis of severe PE
Toxicity, thrombolytics?
Toxicity=bleeding
Contraindicated in pts with active bleeding, hx of intracranial bleeding, recent surgery, known bleeding diatheses, or severe hypertension.
Ttmt of toxicity, thrombolytics?
Ttmt of toxicity=aminocaproic acid (an inhibitor of fibrinolysis)
Aspirin, MOA
Irreversibly inhibits COX1 and 2 via covalent acetylation. Platelets can’t make new enzyme, so effect lasts until new platelets are made. Increases bleeding time, decreases TXA2 and prostaglandins. No effect on PT or PTT.
Clinical use, aspirin
Use: antipyretic, analgesic, anti-inflammatory, antiplatelet (decreased aggregation).
Toxicity, aspirin
Toxicity: gastric ulceration, tinnitus (CN VIII). Chronic use can lead to acute renal failure, interstitial nephritis, and upper GI bleeding. Reye’s syndrome in children with viral infection.
What does OD on aspirin cause
OD causes respiratory alkalosis and metabolic acidosis
ADP receptor inhibitors?
Clopidogrel, ticlopidine, prasugrel, ticagrelor
MOA, ADP receptor inhibitors?
Inhibit platelet aggregation by irreversibly blocking ADP receptors (ADP its receptor on surface of platelet causes GP IIb/IIIa insertion on the membrane, receptor for fibrinogen). Inhibits fibrinogen binding by preventing glycoprotein IIb/IIIa from binding to fibrinogen.
Toxicity, ADP receptor inhibitors (ticlopidine)
Toxicity: neutropenia
Phosphodiesterase inhibitors
Cilostazol is what type of drug?
ADP receptor inhibitor
Ticlopidine=?
ADP receptor inhibitor
Prasugrel=?
ADP receptor inhibitor
Clopidogrel=?
ADP receptor inhibitor
Ticagrelor=?
Phosphodiesterase III inhibitor
Dipyridamole=?
Phosphodiesterase III inhibitors
Cilostazol, dipyridamole are this type of drug
GP IIb/IIIa inhibitor
Abciximab is what type of drug?
GP IIb/IIIa inhibitor
Eptifibatide=?
GP IIb/IIIa inhibitor
Tirofiban=?
GP IIb/IIIa inhibitors
Abciximab, eptifibatide, tirofiban=what type of drugs?
Cilostazol, dipyridamole MOA
Phosphodiesterase III inhibitor, increase cAMP in platelets, thus inhibiting platelet aggregation; vasodilators.
Clinical use, cilostazol, dipyridamole?
Use: Intermittent claudification, coronary vasodilation, prevention of stroke or TIAs (combined with aspirin), angina prophylaxis
Toxicity, cilostazol, dipyridamole?
Tox: nausea, headache, facial flushing, hypotension, abdominal pain.
MOA, abciximab, eptifibatide, tirofiban
MOA: bind to glycoprotein receptor IIb/IIIa on activated platelets, preventing aggregation. Abciximab made from monoclonal Ab Fab fragments.
Clinical use, abciximab, eptifibatide, tirofiban?
Use: acute coronary syndromes, percutaneous transluminal coronary angioplasty.
Toxicity, abciximab, eptifibatide, tirofiban?
Toxicity: bleeding, thrombocytopenia
Act on S phase, antimetabolites
Antimetabolites act at what phase in the cell cycle?
Act on S phase, G2 phase
Etopiside acts on which phases on cell cycle?
G2 phase
Bleomycin acts on which phase of the cell cycle?
M phase
Vinca alkaloids and taxols work at which phase of the cell cycle?
Methotrexate, MOA
MOA:Folic acid analog that inhibits dihydrofolate reductase
-v dTMP, v DNA, and v protein synthesis
Methotrexate, clinical use
Cancers: leukemias, lymphomas, choriocarcinoma, sarcomas
Non-neoplastic: abortion, ectopic pregnancy, rheumatoid arthritis, psoriasis
MTX, toxicity
Toxicity: myelosuppression reversible with leucovorin (folinic acid) rescue)
-Macrovesicular fatty change in liver
-Mucositis
-Teratogenic
5-fluorouracil MOA
Pyrimidine analog bioactivated to 5F-dUMP, which covalently complexes folic acid. This complex inhibits thymidylate synthase–> vdTMP–>v DNA and v protein synthesis
5-fluorouracil uses
Uses: Colon cancer, basal cell carcinoma
5-fluorouracil toxicity
Myelosuppresion which isn’t reversible via leucovorin.
Photosensitivity
Antidote for 5-FU OD?
Antidote=thymidine
MOA, cytarabine (arabinogfuranosyl cytidine)
MOA: pyrimidine analog–>inhibition of DNA polymerase
Clinical use, cytarabine
Clinical use: leukemias, lymphomas
Tox, cytarabine
Toxicity: leukopenia, thrombocytopenia, megaloblastic anemia
MOA, azathioprine, 6-mercaptopurine (6-MP), and 6-thioguanine (6-TG)
MOA: purine (thiol) analogs–>v de novo purine synthesis. Acitvated by HGPRT.
Clinical use, azathioprine, 6-mercaptopurine (6-MP) and 6-thioguanine (6-TG)
Use: Leukemias
Azathioprine, 6-mercaptopurine, and 6-thioguanine toxicity
Tox: bone marrow, GI, liver
Metabolized by xanthine oxidase; thus increases toxicity with allopurinol
Antitumor antibiotics
What do dactinomycin (actinomycin D), doxorubicin, daunorubicin, and bleomycin have in common?
Dactinomycin MOA
Antitumor abx that intercalates in DNA
Dactinomycin clinical use
Use: wilm’s tumor
-Ewing’s sarcoma
-Rhabdomyosarcoma
-Used for childhood tumors (children ACT out)
Dactinomycin, toxicity
Tox: myelosuppression
Doxorubicin, daunorubicin MOA
MOA: generate free radicals. Noncovalently intercalate in DNA–>breaks in DNA–>decrease replication
Doxorubicin, daunorubicin use
Use: solid tumors, leukemias, lymphomas
Doxorubicin, daunorubicin tox
Tox: cardiotoxicity (dilated cardiomyopathy)
-Myelosuppression
-Alopecia
-Toxic to tissues following extravasation
Doxorubicin, daunorubicin antidote
Dexrazoxane (iron chelating agent), used to prevent cardiotoxicity
Bleomycin MOA
MOA: induces free radical formation, which causes breaks in DNA strands
Bleomycin uses
use: testicular cancer, lymphoma
Bleomycin tox
Tox: pulmonary fibrosis, skin changes. Minimal myelosuppression.
Alkylating agents
Cyclophosphamide
Ifosfamide
Nitrosureas (carmustine, lomustine, semustine, streptozocin)
Busulfan
Cyclophosphamide, ifosfamide MOA
MOA: covalently X-link (interstrnad) DNA @ guanine N-7. Require bioactivation by liver.
Uses, cyclophosphamide, ifosfamide
Uses: solid tumors, leukemia, lymphomas, and some brain cancers.
Tox, cyclophosphamide, ifosfamide
Tox: myelosuppression
-Hemorrhagic cystitis
Mesna (thiol group binds toxic metabolite)
Substance that can be used to prevent hemorrhagic cystitis caused by cyclophosphamide, ifosfamide
Nitrousoureas
Carmustine, lomustine, semustine, streptozocin are?
MOA, nitrousureas
MOA: require bioactivation, cross BBB–>CNS
Uses, nitrousureas
Uses: brain tumors (including glioblastoma multiforme)
Toxicity, nitrousureas?
Tox: CNS toxicity (dizziness, ataxia)
MOA, busulfan
MOA: alkylates DNA
Uses, busulfan
Uses: CML, also used to ablate pt’s bone marrow before bone marrow transplantation.
Toxicity, busulfan:
Tox: pulmonary fibrosis, hyperpigmentation
Microtubule inhibitors
Vincristine, vinblastine
Paclitaxel, other taxols
MOA: vincristine, vinblastine
MOA: alkaloids that bind to tubulin in M phase and block polymerization of microtubules so that mitotic spindle cannot form “Microtbules are the VINes of your cells
Tox, vincristine
Tox: neurotoxicity (areflexia, peripheral neuritis), paralytic ileus
Tox, vinblastine

Tox: bone marrow suppress

Vinblastine BLASTS Bone marrow

MOA, paclitaxel, other taxols
MOA: hyperstabilize polymerized microtubules in M phase so that mitotic spindle cannot break down (anaphase cannot occur). “it is TAXing to stay polymerized”
Toxicity, paclitaxel and other taxols
Tox: myelosuppression and hypersensitivity
MOA, cisplatin and carboplatin
MOA: cross-link DNA
Tox, cisplatin and carboplatin
Tox: nephrotoxicity and acoustic nerve damage.
Amifostine (free radical scavenger) and chloride diuresis
How to prevent nephrotoxicity with cisplatin and carboplatin?
MOA, etopiside, teniposide
MOA: inhibit topoisomerase II–>increase DNA degradation
Tox, etopiside, teniposide
Tox: myelosuppression, GI irritation, alopecia
MOA, hydroxyurea
MOA: inhibits ribonucleotide reductase–>v DNA Synthesis (S phase specific)
Tox, hydroxyurea
TOx: bone marrow suppression, GI upset
MOA, prednisone, prednisolone
MOA: may trigger apoptosis, may even work on non-dividing cells
Toxicity, prednisone, prednisolone
Tox: Cushing-like sx, immunosuppression, cataracts, acne, osteoporosis, htn, peptic ulcers, hyperglycemia, psychosis
MOA: tamoxifen, raloxifene
MOA: SERMs, receptor antagonists in breast and agonists in bone. Block the binding of estrogen to estrogen receptor-positive cells.
Toxicity, tamoxifen
Tox: partial agonist in endometrium, which increases the risk of endometrial cancer; hot flashes
Tox, raloxifene
Tox: no increase in endometrial CA because it’s an endometrial antagonist
Trastuzumab (Herceptin) MOA
MOA: monoclonal Ab vs HER-2 (c-erb B2), a tyrosine kinase. Helps kill breast cancer cells that overexpress HER-2, possibly through antibody-dependent cytotoxicity.
Toxicity, trastuzumab
Tox: cardiotoxicity
MOA, Imatinib (gleevec)
MOA: Philadelphia chromosome bcr-abl tyrosine kinase inhibitor
Uses, imatinib
Use: CML, GI stromal tumors
Tox, imatinib
Fluid retention=tox
Rituximab MOA
MOA: monoclonal Ab vs. CD20, which is found on most B cell neoplasms
Vemurafenib MOA
MOA: small molecule inhibitor of forms of the B-Rag kinase with the V600E mutation.
Vemurafenib use
Use: metastatic melanoma
Bevacizumab MOA
MOA: monoclonal ab vs VEGF. Inhibits angiogenesis.

We use cookies to give you the best experience possible. By continuing we’ll assume you’re on board with our cookie policy Enzyme inhibited by methotrexate dihydrofolate reductase ↓ dTMP → ↓ DNA and ↓ protein synthesis List 3/4 cancers treated …

We use cookies to give you the best experience possible. By continuing we’ll assume you’re on board with our cookie policy Antibiotics that block cell wall synthesis by inhibition of peptidoglycan CROSS-LINKING Beta lactams. Penicillin, methicillin, ampicillin, piperacillin, cephalosporins, aztreonam, …

We use cookies to give you the best experience possible. By continuing we’ll assume you’re on board with our cookie policy Antibiotics that block cell wall synthesis by inhibition of peptidoglycan CROSS-LINKING Beta lactams. Penicillin, methicillin, ampicillin, piperacillin, cephalosporins, aztreonam, …

We use cookies to give you the best experience possible. By continuing we’ll assume you’re on board with our cookie policy Neutropenia A common side effects of Interferon (INF) treatment is? TMP-SMZ Antimicrobial prophylaxis for a history of recurrent UTIs …

We use cookies to give you the best experience possible. By continuing we’ll assume you’re on board with our cookie policy Anethetists often administer midazolam (Versed) during induction of anesthesia because of which of the pharmacologic actions? causes amnesia adverse …

We use cookies to give you the best experience possible. By continuing we’ll assume you’re on board with our cookie policy The nurse working on a bone marrow unit knows that it is a priority to monitor which of the …

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