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108 Cards in this Set

  • Front
  • Back
What is the mechanism of Heparin?
Catalyzes the activation of AT3 which decreases Fx 2 and Xa
Half life of Heparin:
SHORT
What is heparin used for clinically?
IMMEDIATE anticoagulation for
-PE
-Stroke
-Angina
-MI
-DVT
When can heparin be used/why?
Pregnancy - does not cross placenta
How is Heparin therapy monitored?
PTT
3 toxic side effects of heparin:
-Bleeding
-Thrombocytopenia (HIT)
-Drug interactions
Antidote for rapid reversal of Heparin; mechanism?
Protamine sulfate - pos charged molecule; binds highly neg charged Heparin
What is a LMWH?
Enoxaparin, Daltaparin
How do the LMWH's act differently from Heparin?
More action on Xa than Thrombin; better bioavailability and 2-4 times longer half life
How can LMWH's be administered?
Subcutaneously instead of only IV
What is the good thing about better bioavailability and half life of LMWH's?
Don't require lab monitoring with PTT
What is Warfarin's clinical use?
CHRONIC longterm anticoagulation
When CAN'T Warfarin be used?
Pregnancy - teratotenic
Site of action of
-Heparin
-Warfarin
Heparin - blood
Warfarin - Liver
Onset of action of:
-Heparin
-Warfarin
Heparin - seconds
Warfarin - takes several days until the pre-existing clotting fxs are removed - half lives limit
4 Thrombolytic agents
Streptokinase
Urokinase
tPA
APSAC
Mechanism of thrombolytics:
Help convert Plasminogen to Plasmin to cleave Fibrin clots
2 clinical uses of thrombolytic agents:
-Early MI
-Early ischemic stroke
Toxicity of Thrombolytics:
Bleeding
What is the antidote for Thrombolytic TOXICITY?
Aminocaproic acid - fibrinolysis inhibitor
What is the rec on platelets for
-collagen
-vWF
-Fibrinogen
-TxA2/ADP/5-HT
Collagen is GP1a
vWF is GP1b
Fibrinogen is GP2b3a
Txa2/ADP/5HT all bind GP's
What 2 drugs inhibit platelet synthesis of thromboxane?
Aspirin
What drug blocks GP2b/3a to prevent Fibrinogen crosslinking the platelet plug?
Abciximab
What drugs irreversibly block ADP receptors on platelets?
Clopidogrel and Ticlopidine
What effect does blocking ADP receptors on Platelets have?
It inhibits the expression of GP2b/3a hence no fibrinogen crosslinking!
What are 2 clinical uses of Ticlopidine and Clopidogrel?
Acute coronary syndorme
Cardiac stenting
What toxic side effect does Ticlopidine have?
Neutropenia
What are the 3 antimetabolite cancer drugs?
-Methotrexate
-5-Fluorouracil
-6-Mercaptopurine
How do MTX and 5-FU work?
Synergistically
What cell cycle phase are MTX and 5-FU both specific for?
S-phase - DNA synthesis
What is the mechanism of MTX?
-Folate analog
-Inhibits Di-HF reductase, inhibits dTMP synth, DNA synth, and protein synthesis
What 4 cancers is MTX used for?
-Lymphomas
-Leukemias
-Choriocarcinoma
-Sarcomas
What are 4 other clinical uses of Methotrexate?
PEAR
-Psoriasis
-Ectopic pregnancy
-Abortion
-Rheumatoid arthritis
What are 2 toxic side effects of MTX and how is one treated?
-Macrovesicular Fatty Liver
-Myelosuppression - rescued with Leucovorin
What is the mechanism of 5-FU?
-Pyrimidine analog; bioactivated to 5F-Dump; covalently complexes Folate which inhibits Thymidylate Synthase.
And what is the effect of inhibiting thymidylate synthease?
Inhibits dTMP synth, DNA, and protein synthesis.
And what does giving MTX and 5-FU together allow for?
Synergistic inhibition of the same biochemical pathway
What are 3 cancers that 5-Fluorouracil is used for?
-Colon cancers
-Other solid tumors
-Cream for Basal cell carcinoma
What are 2 side effects of 5-Fluorouracil?
-Photosensitivity
-Irreversible myelosuppression
What has to be given to 'rescue' the myelosuppression due to 5-FU?
Thymidine
What is the other antimetabolite?
6-Mercaptopurine
How is 6-MP activated and what is its effect?
-Activated by HGPRTase
-Blocks de Novo Purine synthesis
What cancers can/can't 6-MP be used for treating?
CAN treat Leukemia/Lymphoma

CAN'T treat CLL/Hodgkin lymphoma
What are 3 tissues that 6-MP has toxic effects on?
-Bone marrow
-GI tract
-Liver
What metabolizes 6-MP to its inactive form?
Xanthine oxidase
So what can prevent 6-MP metabolism?
Allopurinol - careful!
Drug for treating AML:
Cytarabine; ara-C
What is the mechanism of Cytarabine?
INhibits DNA polymerase
What are 3 toxic side effects of Cytarabine?
-Leukopenia
-Thrombocytopenia
-Megaloblastic anemia
What type of agents are Cyclophosphamide and Ifosfamide?
Alkylating agents
What is the mechanism of Cyclophosphamide and Ifosfamide? How are they activated?
-X-link DNA (interstrand) at Guanine-7 - activated by liver bioactivation
What are the 4 clinical uses of Cyclophosphamide and Ifosfamide?
-NHL
-Breast cancer
-Ovarian cancer
-Immunosuppressant
What are 2 toxic side effects of Cyclophosphamide and Ifosfamide?
-Myelosuppression
-Hemorrhagic cystitis
How can the Hemorrhagic cystitis caused by Cyclophosph and Ifosfamide be prevented?
With MESNA
What are the Nitrosoureas? 4
-Carmustine
-Lomustine
-Semustine
-Streptozocin
What is the mechanism of the Nitrosoureas? What are they especially useful for?
-Alkylate DNA
-Cross the BBB - so treat BRAIN TUMORS!
What brain tumor do the nitrosoureas like Carmustine especially treat?
Glioblastoma multiforme
What are the main toxic side effects of the Nitrosoureas?
CNS - toxicity and Ataxia
How do Cisplatin and Carboplatin work?
LIKE alkylating agents
What are the 4 cancers treated by Cisplatin and Carboplatin?
OBLT
-Ovarian
-Breast
-Lung
-Testicular
What are 2 toxic side effects of Cisplatin and Carboplatin?
-Nephrotoxicity
-Acoustic nerve damage
What drug is used for treating CML?
Busulfan
What is the mechanism of Bulsulfan?
Alkylates DNA
What are 2 toxic side effects of Busulfan?
-Pigmentation
-PULMONARY FIBROSIS
So what are the 4 alkylating agents?
-Cyclophosphamide/Ifosfamide
-Nitrosoureas (Carmustine)
-Cisplatin/Carboplatin
-Busulfan
What is Doxorubicin aka?
Adriamycin
What is the mechanism of Doxorubicin and Daunorubicin? (3 steps)
-Generate FREE RADICALS
-INTERCALATE DNA
-CREATE BREAKS in DNA strand to inhibit replication
What is Adriamycin used for?
-ABVD regimen - Hodgkin lymphoma
-Sarcomas
-Myelomas
-Other solid tumors (brst/ovary)
What are 3 toxic side effects of Adriamycin/doxorubicin/daunorubicin?
-CARDIOtoxicity
-Marked Alopecia
-Myelosuppression
What intercalator just intercalates and doesn't cause strand breaks?
Dactinomycin
What is Dactinomycin used for clinically?
CHILDHOOD tumors
-Wilms tumor
-Ewing's sarcoma
-Rhabdomyosarcoma
What is the toxic side effect Dactinomycin can have?
Myelosuppression
What drug is the B in the ABVD regimen for Hodgkin lymphoma?
Bleomycin
What is Bleomycin's mechanism?
Induces formation of free radicals - causes DNA strand breaks!
What are 2 uses of Bleomycin then?
-Hodgkin lymphoma
-Testicular cancer
What are 2 toxic effects of Bleomycin?
-PULMONARY FIBROSIS (bab)
-Skin changes
What does Bleomycin cause MINIMALLY?
Myelosuppression
What cell cycle phase is Bleomycin specific for?
G2
What drug works on S and G2?
Etoposide
What is Etoposide's mechanism?
-Inhibits Topoisomerase II
-Increases DNA degradation
What are 3 cancers Etoposide is used for?
-SCC of lung
-SCC of prostate
-Testicular cancer
SE's of Etoposide?
Normal
-GI upset, myelosuppress, alopecia
What is the most commonly used Glucocorticoid in cancer therapy?
PREDNISONE
What is Prednisone's mechanism?
Triggers Apoptosis
What are 2 cancers Prednisone is used for treating?
-CLL
-Hodgkin's lymphoma
What are 9 side effects of Prednisone?
COACHH PIP
-Cushing's syndrome
-Osteoporosis, Acne, Cataracts
-Hypertension/Hyperglycemia
-Peptic ulcers, Immunosuppress, Psychosis
What are the main drugs for treating Estrogen receptor pos breast cancer?
Tamoxifen/Raloxifene
How do Tamoxifen and Raloxifene work on the breast? Bone?
Breast = Est antagonist

Bone = Est agonist!
So what are the 2 useful effects of Tamox/Raloxifene?
-Slow Br cancer growth
-Slow osteoporosis!
What are 2 toxic side effects of Tamoxifen specifically?
-Hot flashes
-May increase risk of endometrial carcinoma - agonist properties in the uterus
Why doesn't Raloxifene have this risk?
It's an antagonist in the uterus
What is Herceptin and what is it aka?
Trastuzumab - anti Her-2 (erb-B2)
What is Trastuzumab used for?
HER-2 expressive Breast cancer
What is a possible side effect of Trastuzumab?
Cardiotoxicity
What is Imatinib aka?
Gleevac!
What is Gleevac used for?
Inhibition of the Ph' chromosome brc-abl fusion protein tyrosine kinase product
So what 2 cancers are treated with Gleevac?
-CML
-GI stromal tumors
What is a toxic side effect of Gleevac?
Fluid retention
What are the 'Vinca alkaloids'?
Vincristine and Vinblastine
What is the mechanism of Vincristine/blastine; what cell cycle phase are they specific for?
-Bind tubulin, block MT polymerization - mitotic spindle can't form!
-M-phase specific! Mitotic
What are 3 clinical uses of Vincristine/blastine?
-Wilm's tumor
-Lymphoma
-Choriocarcinoma
What are 2 side effects of:
-Vincristine

-Vinblastine
Cristine = Neurotoxic/Paralytic ileus

Blastine = Bone marrow suppression
What is Paclitaxel?
A Taxol!
What is the mechanism of Paclitaxel and other Taxols?
Bind tubulin and HYPERSTABILIZE polymerized MT's so the mitotic spindle can't BREAK DOWN!
What cell cycle phase are the taxols specific for?
M-phase - prevent progression to anaphase
What are 2 cancers for which the Taxols/Paclitaxel are used?
-Breast
-Ovarian
What are 2 side effects of the Taxols?
-Myelosuppresion
-Hypersensitivity
What are the drugs that act on MIcrotubules?
Maybe Taxes on Grease Vindicate Coalworkers!
-Mabendazole
-Taxols (Paclitaxel)
-Griseofulvin
-Vincristine/blastine
-Colchicine