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Heme/Onc Drugs
Heme/Onc Drugs
77
Medical
Graduate
11/15/2009

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Term
This drug may cause immune destruction of platelets
Definition
Unfractionated Heparin can cause HIT (Heparin Induced Thrombocytopenia)
Term
This anti-coagulant has a very negative charge
Definition
Heparin has a very negative charge
Term
What test do you use to measure the effectiveness of Heparin?
Definition
Measure unfractionated Heparin activity with the aPTT test
Term
What is the mechanism of Heparin?
Definition
Heparin accelerates the activity of anti-thrombin (a serine protease), which blocks the intrinsic pathway
Term
How would you treat a Heparin overdose?
Definition
Protamine sulfate
Term
What is the mechanism of Warfarin?
Definition
Warfarin is a Vitamin K antagonist that prevents activation of factors II, VII, IX and X (as well as protein C and S). It blocks carboxylation of glutamate residues, specifically be blocking the enzyme Vitamin K Epoxide Reductase (VKOR)
Term
What do you use the INR to measure?
Definition
Use INR (a normalized version of the PT test) to measure Warfarin activity
Term
Can pregnant patients receive Warfarin?
Definition
No, warfarin crosses the placenta and is teratogenic
Term
What fibrinolytic drug must be given within 3 hours of thromboembolism?
Definition
t-PA (tissue plasminogen activator) is a serine protease. Contraindicated in people with hypertension, recent GI bleeding or CVA.
Term
What is the anti-platelet mechanism of ASA?
Definition
ASA inhibits thromboxane formation by irreversibly acetylating COX. It is better at blocking arterial thrombus than venous thrombus.
Term
This drug specifically blocks the activity of the BCR-ABL tyrosine kinase
Definition
Imatinib (Gleevac) blocks the TK enzyme produced by the Philadelphia Chromosome, seen in CML.
Term
What is side effect of Bleomycin?
Definition
Bleomycin can cause pulmonary fibrosis
Term
What is a side effect of Busulfan?
Definition
Busulfan can cause pulmonary fibrosis
Term
What is a side effect of Doxorubicin?
Definition
Doxorubicin can cause cardiac toxicity. Increased skin pigmentation also seen.
Term
What is a side effect of cisplatin?
Definition
Cisplatin is nephrotoxic and can cause peripheral neuropathy
Term
What is a side effect of cyclophosphamide?
Definition
Cyclophosphamide can cause hemorrhagic cystitis - must take with lots of water to dilute these effects
Term
What is a side effect of Vincristine?
Definition
Vincristine can cause neurotoxicity, and possibly an aplastic crisis
Term
What is a side effect of cytarabine?
Definition
Cytarabine can cause cerebral damage
Term
What is the mechanism of the alkylating agents? (Ex. cyclophosphamide, busulfan or the nitrogen mustards?)
Definition
Alkylating agents bind guanine and cross link DNA. They often have chloroethyl functional groups.
Term
Name four alkylating agents.
Definition
4 alkylating agents are: cyclophosphamide, busulfan, nitrogen mustards and chlorambusil.
Term
How is carboplatin unique?
Definition
Carboplatin is unique in that dosing is based on the glomerular filtration rate. It works by forming reactive groups with DNA
Term
Name 4 anti-metabolites
Definition
4 anti-metabolite drugs are: methotrexate (blocks DHFR), 6-mercaptopurine (metabolized by xanthine oxidase), florouracil, and cytarabine
Term
How does Tamoxifen work?
Definition
Tamoxifen binds to, and inactivates, estrogen receptors. Maximum use is 5 years. 50% reduction in breast cancer, but increase in uterine cancer.
Term
What are anti-androgen drugs used for?
Definition
Anti-androgens are used for prostate cancer
Term
What is the mechanism of thalidomide?
Definition
Thalidomide blocks angiogenesis
Term
What is the mechanism of Bortezomib?
Definition
Bortezomib is a protease inhibitor and is used for Multiple Myeloma
Term
How does Bleomycin work?
Definition
Bleomycin breaks DNA
Term
How does the anti-cancer Abx Doxorubycin wokr?
Definition
Doxorubycin intercalates DNA and stops RNA synthesis. Active in G2/M phase
Term
How does Vincristine function?
Definition
Vincristine stops cellular division by blocking microtubules
Term
How does Paclitaxel function?
Definition
Paclitaxel works by blocking cell division by inhibiting microtubule synthesis. Works in G2/M phase
Term
What is the primary target of LMWH?
Definition
LMWH targets factor Xa
Term
Mechlorethamine
Definition
Nitrogen mustard that alkylates DNA. Targets proliferating cells. Can cause immunosuppresion
Term
What alkylating agent can penetrate the blood-brain barrier?
Definition
Nitrosureas pass the BBB. May cause pulmonary fibrosis and renal toxicity
Term
What are the side effects of carboplatin?
Definition
Unlike cisplatin, carboplatin does not have the serious side effects of renal toxicity and neurotoxicity, but does cause myelosuppresion
Term
When is Melphalan used?
Definition
Melphalan is an alkylating agent used for multiple myeloma
Term
What is the principle use of 6-mercaptopurine?
Definition
6-mercaptopurine is used to maintain remission in ALL
Term
Leucovorin (folinic acid)
Definition
Replenishes folate- given with 5FU or Methotrexate
Term
Aminoglutethimide
Definition
Anti-steroid, used for metastatic breast cancer. Blocks aromatase.
Term
Exemestane
Definition
Steroidal aromatase inhibitor, used for hormone responsive breast cancers
Term
Anastrozole
Definition
Aromatase inhibitor, used for breast cancer
Term
Letrozole
Definition
Non-steroidal aromatase inhibitor, for breast cancer
Term
Flutamide
Definition
Anti-androgen, for prostate cancer. Competes with DHT for androgen receptor binding sites.
Term
Rituximab
Definition
Chimerical Monoclonal Ab, binds B-cell CD20. Initiates ADCC.
Term
Trastuzumab
Definition
a.k.a Herceptin - binds HER2/Neu. Human monoclonal Ab. Side effect = congestive heart failure
Term
Gefitinib
Definition
Selective inhibitor of the tyrosine kinase, EGFR (epidermal growth factor receptor)
Term
L-Asparaginase
Definition
Destroys asparagine in the blood, depriving tumor cells of this amino acid
Term
Prednisone
Definition
Employed to induce remission in patients with ALL and in treatment of both HL and NHL
Term
Dexamethasone
Definition
Helps prevent nausea and vomitting from cancer chemotherapy
Term
Megestrol
Definition
Used to be used for estrogen receptor + breast and ovarian cancers (aromatase inhibitors are more frequent now)
Term
Dasanitib
Definition
Tyrosine Kinase inhibitor, for use in imatinib resistnat CML
Term
Bevacizumab
Definition
mAb used in colorectal cancer, targets VEGF, limits angiogenesis
Term
Bisphosphonates
Definition
Palliative use in multiple myeloma to prevent bone degradation
Term
Meperidine (demerol)
Definition
Avoid in cancer pain, short duration and addictive
Term
Nalbuphine
Definition
Avoid in cancer pain. Mu antagonist, K agonist (psychomimetic)
Term
Buprenorphine
Definition
Avoid in cancer pain. Used to treat opioid dependence
Term
Naloxone
Definition
Avoid in cancer pain- for emergency opioid overdose
Term
Naltrexone
Definition
Avoid in cancer pain- used to prevent relapse in chronice opioid addicts or alcoholics
Term
Pentazocine
Definition
Avoid in treatment of cancer pain (opioid antagonist)
Term
Butorphanol
Definition
Avoid in use of cancer pain, partial mu antagonist
Term
Morphine
Definition
Causes analgesia, miosis, respiratory depression, sedition, anti-tussis. Also causes constipation, urinary retention, pruritis, hypotension. Good for breathing distress.
Term
Methadone
Definition
Slightly more potent than MS. Slow and mild withdrawal.
Term
Oxycodone
Definition
For pain
Term
Fentanyl
Definition
100x more potent than morphine. Can give transdermal.
Term
Codeine
Definition
1/10 the strength of morphine. Anti-tussive
Term
Hydromorphone
Definition
For cancer pain. Strongest of the anti-tussive drugs.
Term
Fenoprofen
Definition
NSAID, for mild to moderate pain
Term
Ketoprofen
Definition
NSAID that inhibits the production of prostaglandin
Term
Ketorolac tromethamine (toradol)
Definition
NSAID, blocks COX. For moderate to severe pain
Term
Carbamazepine
Definition
Anti-convulsant. Good for trigeminal neuralgia. May cause aplastic anemia
Term
Valproate
Definition
Anti-convulsant. Inhibits T-type Ca channels and increases GABA, good for chronic pain
Term
Gabapentin
Definition
Anti-convulsant (GABA analog). Good for chronic pain
Term
Clonazepam
Definition
Anti-convulsant, muscle relaxant, anxiolytic.
Term
Amitriptyline
Definition
Tricyclic antidepressant and anxiolytic
Term
Desipramine
Definition
Tricyclic antidepressant, also used for neuropathic pain
Term
Duloxetine
Definition
Antidepressant and anxiolytic
Term
Naproxen
Definition
NSAID, inhibits COX1 and COX2 (same drug as Ibuprofen)
Term
Ibuprofen
Definition
NSAID, inhibits COX1 and COX2 (same drug as Naproxen)
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