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153 Cards in this Set

  • Front
  • Back
  • 3rd side (hint)
heparin
p. 305
Heparin catalyzes activation of ____________, decreases ________ and __________. It has a ____t1/2. check PTT
catalyzes the activation of antithrombin III, decreases thrombin and Xa. It has a short t1/2
p. 305
Heparin s used for immediated anticoagulation for pulmonary embolism,_______, _______, MI, and ________. Follow PTT
used for pulmonary embolism, stroke, angina, MI, and DVT.
p. 305
T/F: Heparin is used during pregnancy
true: it is used during pregnancy because it does not cross the placenta.
p. 305
Heparin can cause bleeding,___________, and drug-drug interactions.
thrombocytopenia
p. 305
___________ is used for rapid reversal of heparization (it is a _______ charged molecule that binds the ________ charged heparin)
protamine sulfate is used for rapid reversal of heparinization (it is a positively charged molecule that binds the negatively charged heparin).
p. 305
Newer________________-heparins(enoxaparin) act more on _____, have better bioavailability and 2-4 times longer t1/2. Can be administered subcut and (with/without) lab monitoring.
lower-molecular-weight heparins (enoxaparin) act more on Xa, have better bioavailabitlity and 2-4 times longer half-life. Can be adm. Subcut and without lab monitoring.
p. 305
Warfarin interferes with normal synthesis and gamma-carboxylation of vitamin K-dependent factors ___, ___, ___, and ___, also, ___ and ___ via ______ antagonism.
Interferes with normal synthesis and gamma-carboxylation of vitamin K-dependent clotting factors II, VII, IX, and X, protein C and S via vitamin K antagonism.
p. 305
What is the t1/2 (short/long) of warfarin?
long
p. 305
Warfarin is used for _______ anticoagulation. Follow PT
WEPT - Warfirin affects the Extrinsic pathway and prolongs PT
p. 305
T/F: warfarin is used during pregnacy
False! (warfarin, unlike heparin, can cross the placenta).
p. 305
Warfarin Toxicity: bleeding, _________, drug-drug interactions
teratogenic
p. 305
Heparin is a (large/small) _____charged acicid polymer while Warfarin is (large/small) (charged/neutral) molecule
Heparin is a large negatively charged acidic polymer while Warfarin is a small neutral charged lipid-soluble molecule
p. 305
T/F: Heparin is given orally while warfarin is given SC/IV
False! Heparin is given IV/SC and warfarin is give oral
p. 305
Site of action: heparin _________, warfarin ______
heparin's site of action is the blood; warfarin's site of action is the liver (synthesises clotting factors)
p. 305
Onset of action of _________ is slow; the onset of action of ______ is rapid
onset of action of heparin is rapid (secs) and the onset of action of warfarin is slow, limitd by t1/2 of normal clotting factors.
p. 305
Warfarin works by imparing the synthesis of _______ dependent factors __, ___, ___, and ___ also _____, and ____; heparin activates _____, ____ and ___
Warfarin works by imparing the synthesis of vitamin K dependent factors II, VII, IX, and X also protein S and protein C; heparin activates ATIII, Iia (thrombin) and Xa.
p. 305
Heparin 's duration of action is (acute/chronic); warfarin's duration of action is (actue/chronic)
Heparin's duration of action is actute and warfarin's duration of action is chronic.
p. 305
Tx of acute OD: Heparin = _________; warfarin=______
Tx of heparin OD is protamine sulfate; Tx of warfarin= IV vit. K and fresh frozen plasma.
p. 305
Warfarin is monitored by _________ while Heparin is monitored by ___________.
Warfrin is monitored by PT (extrinsic pathway) (WEPT) and heparin is monitored by PTT (intrinsic pathway)
p. 305
plasmin is the major ___________ enzyme. It breaks down both _______ and _______
fibrinolytic enzyme. It accelerates breaks down of both fribin and fibrinogen yielding fibrin splip products and degradation products, respectively.
p. 306
Fibrinogen is converted to fibrin by _________
thrombin
p. 306
tPA and urokinase promote the converson of ______ to ________ thereby increasing fibrinolysis.
plasminogen to plasmin
p. 306
Various stimuli activate a blood proactivator to a blood activator that promotes conversion of _________ to blank thereby increasing fibrinolysis
plasminogen to plasmin
p. 306
Streptokinase and anistreplase both activate ____, which increases convesion of plasminogen to plasmin.
Activator
p. 306
Aminocaproic acid:____________ fibrinolysis.
inhibits fibrinolysis by inhibition of plasminogen conversion to plasmin.
p. 306
4 examples of thrombolytics include: ________, _________, _____________, and ___________
Streptokinase, urokinase, tPA(altepalse), APSAC (anistreplase)
p. 306
Thrombolytics work by directly or indirectly aiding the conversion of ___________ to __________, which cleaves ______ and ________ clots. tPA specifically coverts _______________ to plasmin
Directly or indirectly aid conversion of plaminogen to plasmin, which cleaves thrombin and fribrin clots. It is claimed that tPA specifically coverts fribrin-bound plasminogen to plasmin.
p. 306
T/F: Thrombolytic clinical use is for DVTs
False: used for early MI and early ischemic stroke
p. 306
pts. receiving thrombolytics are at most risk for: ______
bleeding
p. 306
mechanism of antiplatelet interaction
p. 306
questions from diagram at top of page
p. 306
When a break in the endothelium occurs _________ and _________ are exposed.
collagen and vWF
p. 306
Platelets are activated by binding to the above macromolecules. The two structures expressed by the platelets involved in this process are __________ and _________ and they bind to _________ and __________, repectively
Platelets bind to collagen and vWF. The two structures expressed by platelets that are involved in this process are GP 1a and GP 1b. GP 1a and GP 1b bind to collagen and vWF, respectively.
p. 306
After platelet activation _________ is expressed on their surface. What is the role of this structure?
after platelets are activated they express GP IIb/IIIa. This molecule is important in platlelet-platelet aggregation.
p. 306
_________ and _________ interaction is needed in order for platelet aggregation to occur.
GP IIb/IIIa and fribinogen
p. 306
5-HT, _______, and ________ are molecules that play a role in the glycoprotein expression of activated platelets.
5-HT, ADP, and TxA2 are molecules that play a role in the glycoprotein expression of activated platelets.
p. 306
Aspirin acts by inhibiting production of ________ that in turn inhibits glycoprotein expression in activated platelets.
TxA2
p. 306
ADP production is inhibited by the drug _________.
ticlopidine
p. 306
This antibody drug targets the _______ on platelets.
Abciximab
p. 306
What drug inhibits platele aggregation by irreversibly inhibiting the ADP pathway involved in the binding of fibrinogen
Clopidogrel, ticlopidine
p. 307
Clopidogrel, ticlopidine is used for ______ ________ syndrome, coronary _______, and it has been shown to decrease the incidence or recurrence of___ ____.
it is used for acute coronary syndrome, coronary stenting. Decreases incidence or recurrence of thrombotic stroke
p. 307
Ticlopidine is associated with_________ as a side effect.
Ticlopidine causes neutropenia and it is reserved for those who cannot tolerate aspirin.
p. 307
What drug is a monoclonal antibody that binds to __________ on activated platelets.
Abciximab, gp IIb/Iia
p. 307
Abciximab is used for ___________ and ________ _________ ___________ ___________
acute coronary syndromes and percutanous transluminal coronary angioplasty
p. 307
Toxiciites of abciximab are _______ and ________
bleeding and thrombocytopenia
p. 307
Asparin ________ and (reversibly/irreversibly) inhibits COX1 and COX2 to prevent the conversion of _______ to prostaglandins.
acetilates and irreversably inhibits COX-1 and COX-2
p. 307
T/F: aspirin has an effect of PT, PTT
false it has no effect but increases bleeding time
p. 307
What are the 4 A's of aspirin and NSAIDS in general
Antipyretic, Analgesic, Anti-inflam, antiplatelet
p. 307
Important toxicities of Aspirin include _________, bleeding, hyperventilation, __________- in children, and CN ____ toxicity
gastric ulceration, bleeding, hyperventilation, Reyes syndrome and tinnitus (CNVIII).
p. 307
What are the cell cycle specific oncologic drugs (6)
antimetabolites (MTX, 5-FU, 6-MP), vinca alkaloids, stroid hormones, bleomycin, paclitaxel, etoposide
p. 307
What are the cell cycle Nonspecific oncologic drugs?
alkylating agents and antibiotics (dactinomycin, doxorubicin, bleomycin)
p. 307
What class of drugs inhibits with cell division by interfering with the S phase (DNA synthesis)
Antimetabolites (MTX, 5-FU)
p. 308
What drug acts on boht the S phase and the G2 phase of the cell cycle?
Etoposide
p. 308
What drug specifically acts on the G2 phase of the cell cycle?
Bleomycin
p. 308
What two classes of drugs interfere with the M phase of the cell cycle?
Vinca alkaloids and taxols
p. 308
What is an S-phase-specific antimetabolite that is a folic acid analog that inhibits dihydrofolate reductase, resulting in a decrease dTMP (thymidine and purines) and therefore decreased DNA and protien synthesis
Methotrexate
p. 308
What is the mechanism of action of Methotrexate
Methotrexate is an S-phase-specific antimetabolite. Folic acid analog that inhibits dihydrofolate reductase, resulting in a decrease dTMP (thymidine and purines) and therefore decreased DNA and protien synthesis
p. 308
What anti-cancer drug is a folic acid analogue?
Methotrexate
p. 308
Methotrexate effects what part of the cell cycle?
S-phase
p. 308
What anti-cancer drug inhibits dihydrofolate reductase?
Methotrexate (folic acid analogue)
p. 308
Used to treat leukemias, lymphomas, choricarcinoma, sacromas, rheumatoid arthritis, psoriasis, and can be an abortifacient; it may lead to myelosuppression
Methotrexate
p. 308
What is Methotrexate used for (7)
Used to treat leukemias, lymphomas, choricarcinoma, sacromas, rheumatoid arthritis, psoriasis, and can be an abortifacient; it may lead to myelosuppression
p. 308
What are the toxicities of Methotrexate?
meylosuppression, which is reversbiel by leucovorin (folinic acid) "rescue." Macrovesicular fatty chage in the liver.
p. 308
What is the effect of Methotrexate on the liver?
Macrovesicular fatty chage in the liver.
p. 308
____is an S-phase-specific anti-metabolite that is a pyrmidine analog which complexed to folic acid, inhibiting thymidylate synthase, decreasing dTMP and decreasing DNA/protein synthesis
5-Fluorouracil (5-FU)
p. 308
What is the mechanism of action of 5-Fluorouracil (5-FU)
5-Flourouacil (5-FU) is an S-phase-specific anti-metabolite BIOACTIVATED TO 5F-dUMP that is a pyrmidine analog which complexed to folic acid, inhibiting thymidylate synthase, decreasing dTMP and decreasing DNA/protein synthesis
p. 308
Myelosuppression by methotrexate is reversible with ____
leucovorin (folinic acid) rescue
p. 308
What is the clinical use for 5-Flourouracil?
Colon cancer and other solid tumors, basal cell carcinoma (topical).
p. 308
What drug works well on solid tumors?
5-Flourouracil (5-FU)
p. 308
What drug works synergistically with 5-FU?
Methotrexate (MTX)
p. 308
What drug is works welll in colon cancer?
5-Flourouracil (5-FU)
p. 308
Leucovorin (folinic acid) is counteract what drug side-effect
meylosuppression due to methotrexate
p. 308
What are the toxicities of 5-Flourouracil?
myelosuppression (NOT reversible with leucovorin) and photosensitivity
p. 308
What drug inhibits thymiylate synthase?
5-Flourouracil (5-FU)
p. 308
Used to treat colon cancer and other solid tumors, basal cell carcinoma (topically)
5-Fluorouracil (5-FU)
p. 308
Myelosuppression by 5-FU is ______
Not reversible
p. 308
Which drug blocks purine synthesis and is used to treat leukemias, lymphomas (not CLL or Hodgkins)
6-mercaptopurine (6-MP)
p. 309
What is the mechanism of 6-mercaptopurine?
Blocks de novo purine synthesis. Activated by HGPRTase.
p. 309
What drug is commonly used to treat leukemias and lymphomas (not CLL or Hodgkin's)?
6-mercaptopurine (6-MP)
p. 309
6-mercaptopurine (6-MP) is used for what cancers?
leukemias and lymphomas (not CLL or Hodgkin's)?
p. 309
What drug increases the toxicity of allopurinol and how?
6-mercaptopurine (6-MP) because it is metabolized by xanthine oxidase
p. 309
What are the side effects of 6-mercaptopurine (6-MP)?
Bone marrow, GI, liver, increased tox of allopurinol
p. 309
This drug used to treat Leukemias and Lymphomas is metaboilized by xanthine oxidase
6-mercaptopurine (6-MP)
p. 309
Which drug inhibits DNA polymerase and is used to treat AML?
cytarabine (ara-C)
p. 309
This drug used to treat AML may lead to leukopenia, thrombocytopenia, megaloblastic anemia?
cytarabine (ara-C)
p. 309
What are the side effects of cytarabine (ara-C)
Leukopenia, thrombocytopenia, megaloblastic anemia
p. 309
What cancer drug inhibits DNA polymerase?
cytarabine (ara-C)
p. 309
These alkylating agents can cause myelosuppression and hemorhagic cystitis
cyclophosphamide, ifosfomide
p. 309
What drugs are alkylating agents?
cyclophosphamide, ifosfomide
p. 309
What is the mechanism of action of alkylating agents (cyclophosphamide and ifosfomide)?
Alkylating agents ; covalentsly x-link (interstrand) DNA at guanin N-7. Require bioactivation by the liver.
p. 309
Where is cyclophosphamide and ifosfonide activated?
liver
p. 309
What drug can be used to prevent the side effects of alkylating agents (cyclophosphamide and ifosfomide)?
mesna
p. 309
What are cyclophosphamide and ifosfamide used for?
Non-Hodgekin's lymphoma, breast and ovarian carcinomas. Also immunosuppressants?
p. 309
What drugs are used to treat Non-Hodgekin's lymphoma, breast and ovarian carcinomas.
cyclophosphamide, ifosfomide
p. 309
What cancer agents can be used as immunosuppressants
cyclophosphamide, ifosfomide
p. 309
What drugs alkylate DNA after bioactivation and can cross the BBB and treats brain tumors (glioblastoma multiforme)
Nitrosoureas (Carmustine, lomustine, semustine, streptozocin)
p. 309
Name 4 Nitrosoureases
Carmustine, lomustine, semustine, streptozocin
p. 309
What class of drugs are Carmustine, lomustine, semustine, streptozocin
Nitrosoureas
p. 309
What class of drugs is used to treat brain tumors (including gioblastoma maltiforme)
Nitrosoureas (Carmustine, lomustine, semustine, streptozocin)
p. 309
What anti cancer drugs causes CNS toxicity (dizziness and ataxia)
Nitrosoureas (Carmustine, lomustine, semustine, streptozocin)
p. 309
What are the side effects of Nitrosoureas (Carmustine, lomustine, semustine, streptozocin)
CNS toxicity (dizziness and ataxia)
p. 309
What 2 drugs act like an alkylating agent, x-linking via hyrdolysis of Cl and platinum; used to treat testicular, bladder, lung carcinomas
Cisplatin, carboplatin
p. 309
What are the toxicities of cisplatin and carboplatin?
nephrotoxicity and acoustic nerve damage
p. 309
What 2 drugs are used to treat testicular, bladder, ovary, and lung carcinomas
Cisplatin, carboplatin
p. 309
Cisplatin and carboplatin are used to treat what 4 cancers
testicular, bladder, ovary, and lung carcinomas
p. 309
Which drug alkylates DNA and is used to treat CML?
Busulfan
p. 309
This drugs used to treat CML may lead to pulmonary fibrosis and hyperpigmentation?
Busulfan
p. 309
What are the toxicities of Busulfan?
pulmonary fibrosis and hyperpigmentation
p. 309
This combination of drugs is used to treat Hodgkin lymphoma
ABVD: Adriamycin (Doxorubicin), Bleomycin, Vinblastine, Dacarbazine
p. 309
What 2 drugs create free radicals and noncovalently intercalates in DNA, creating breaks to decrease replication and transcription
Doxorubicin (adriamycin) and Daunorubicin
p. 309
What are the uses of Doxorubicin (andriamycin) and Daunorubicin?
Hodgkin's, myelomas, sarcomas and solid tumors (breast, ovary, lung)
p. 309
What are the 4 toxicities of Doxorubicin (andriamycin) and Daunorubicin?
Cardiotoxicity, myelosupression and marked alopecia. Toxic extravasation.
p. 309
What is the mechanism of action of Dactinomycin (actinomycin D)
Intercalates in DNA
p. 309
What is Dactinomycin (actinomycin D) used for? (3)
Wilm's tumor, Ewing's sarcoma, rhabdomyosarcoma (Children ACT out)
p. 309
What drug is used for Wilm's tumor, Ewing's sarcoma and rhabdomyosarcoma?
Dactinomycin (actinomycin D)
p. 309
What drug induces formation of free radicals which cause breaks in DNA strands and is used to treat testicular cancer and lymphomas?
Bleomycin
p. 309
What chemo drug causes pulmonary fibrosis, skin changes but minimal myelosuppression?
Bleomycin
p. 309
What are 3 side effects of bleomycin?
pulmonary fibrosis, skin changes and minimal myelosuppression
p. 309
What is Bleomycin used to treat?
testicular cancer and lymphomas (part of ABVD Hodgkin's regimen)
p. 309
What 4 chemo drugs are given for testicular cancer?
Bleomycin, cicsplaitn, carboplatin, etoposide (VP-16),
p. 309
What 6 drugs are used to treat breast cancer?
cyclophosphamide, ifosfomide, tamoxifen, raloxifene, trastuzumab (herceptin), taxols (parlitaxel)
p. 309
What is the mechanism of action of Etoposide (VP-16)?
G2 phase specific agent that inhibits topoisomerase II and increases DNA degradation.
p. 310
What drug works by inhibiting topoisomerase II and increases DNA degradation in G2 of the cell cycle?
Etoposide
p. 310
What are the indications for Etoposide? (3)
Small cell carcinoma of the lung and prostate, testicular carcinoma
p. 310
What G2 phase drug is used to treat small cell carcinoma of the lung and prostate, testicular carcinoma?
Etoposide
p. 310
What drug causes myelosuppresssion, GI irritation and alopecia?
Etoposide
p. 310
What are the side effects of Etoposide?
myelosuppression, GI irritation and alopecia
p. 310
This drugs used as an immunosuppressant and in lymphomas may cause acne, osteoporosis, hypertension, peptic ulcers, hyperglycemia, psychosis?
Prednisone
What is the mechanism of action of Prednisone?
May trigger apoptosis. May even work on non-dividing cells
p. 310
What is the most commonly used glucocorticoid in cancer chemo. Used in CLL, Hodgkin's lymphomas (mopP regimen). Also an immunosuppressant used in auto-immune diseases
Prednisone
What chemo agent is used in CLL and Hodgkin's lymphoma
Prednisone
p. 310
Name 9 side effects of prednisone
Cushing-like symptoms, immunosuppresion, cataracts, acne, osteoporosis, hypertenstion, peptic ulcers, hyperglycemia, psychosis.
p. 310 O CHIP CHAP
What are 2 estrogen receptor mixed agonist/antagonists that blocks the binding of estrogen to ER+ cells.
Tomoxifen/Raloxifene
What two SERM's are used in breast cancer chemo and osteoperosis?
Tomoxifen/Raloxifene
What are the negative side effects of Tomoxifen?
May increase the risk of endometrial carcinoma via partial agonist effects; also hot flashes.
p. 310
What drugs is used to treat breast cancer, but may increas the risk of endometrial carcinomas and hot flashes
Tomoxifen
p. 310
What is the mechanism of action of Trastuzumab (Herceptin)?
Monoclonal antibody against Her-2 (erb-B2). Helps kill breast cancer cells that over-express HER-2, possibly through antibody dependent cytotoxicity.
p. 310
What drug is used to treat HER-2 positive metastatic breast cancer
Trastuzumab (Herceptin)
p. 310
What is the toxicity of Trastuzumab (Herceptin)?
Cardiotoxicity.
p. 310
What 3 drugs used in cancer treatment have cardiotoxicity?
Trastuzumab (Herceptin), Doxorubicin, daunorubicin
p. 310
What is the mechanism of action of Imatinib (Gleevac)?
Monoclonal antibody againt the Philadelphia chromosomem brc-abl tyrosine kinase
p. 310
What is Imatinib (Gleevac) used for?
CML and GI stromal tumors (Philadelphia chromosome +)
p. 310
What drug is used for CML and GI stromal tumors?
Imatinib (Gleevac)
p. 310
What three chemo drugs are used for CML?
Imatinib (Gleevac), 6-mercaptopurine, Busulfan
p. 310
What is the side effect of Imatinib (Gleevac)?
Fluid retention
p. 310
____is n M-phase-specific alkaloid that binds to tubulin and blocks polymerization of microtubules, preventing spindle formation
Vincristine and Vinblastine
p. 310
____is an M-phase-specific agen that binds to tubulin and hyperstabilizes the polymerized microtubules, so that the mitotic spindle cannot break down
Paclitaxel
p. 310
What drug is used to treat lymphoma, Wilms' tumor and choriocarcinoma?
Vincristine, Vinblastine
p. 310
4 Side-effects of Vinblastine include….
VinBASTine BLASTs Bone Morraow, causing myelosuppression, as well as perepheral neuritis, areflexia and paralytic ileus.
p. 310
Side effects of Paclitaxel include….
Myelosuppression and hypersensitivity
p. 310
What drugs are used to treat ovarian and breast carcinomas and act during the M phase of the cell cycle
Taxols (paclitaxel)
p. 310
What 3 drugs are used to treat Wilms' tumor
Vincristine, Vinblastine, Dactinomycin
p. 310