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Methotrexate
Folic acid analog that inhibits dihydrofolate reductase; decrease in dTMP


Toxicity: Myelosuppresion (reversed with leucovorin); macrovesicaulr fatty change; mucositis; teratogenic
5FU
Pyrimidine Analog that binds to folic acid and inhibits thymidylate synthesis resulting in decrease in dTMP

Toxicity: Mywlosuppresion (can't reverse with leucovorin, rescuse with thymidine); photosensitivity
6MP
Purine analog that inhibits purine synthesis


Toxicity: Bone marrow, GI, liver; metabolized by xanthine oxidase so allopurinol increases toxicity
6TG
Purine analog that inhibits purine synthesis


Toxicity: Bone marrow, liver; can be given with allopurinol
Cytarabine
Pyrimidine antagonist inhibits DNA polymerase


Toxicity: Leukopenia, thromocytopenia, megaloblastic anemia
Dactinomycin
intercalates with DNA

Toxicity: myelosupression
Doxorubicin
Generates free radicals and creates breaks in strand through non-covalent intercalation

Toxicity: cardiotoxicity, myelosupression and alopecia. Toxic to tissues with extravasation
Bleomycin
induces free radical formation causes DNA breaks


Toxicity: pulmonary fibrosis, skin cahnges, minimal myelosupression
Etoposide
topoisomerase inhibitor increase DNA degradation


Toxicity: myelosupression, GI irriation, alopecia
Cyclophosphamide
covalently X link DNA at guanine nitrogen; needs to be bioactivated


Toxicity: myelosupression, hemorrhagic cystitis (can be prevented with mesna which binds toxic metabolites)
Nitrosoureas
carmustine, lomustine, semustine, streptozocin

require activation and cross CNS

Toxicity: CNS - dizziness and ataxia
Busulfan
alkylates DNA

Toxicity: pulomary fibrosis and hyperpigmentation
Vincristine
binds tubulin and blocks polymerization


Toxicity: neurotoxicity and paralytic ileus
Vinblastine
binds tubulin and blocks polymerization

Toxicity: bone marrow suppression
Paclitaxel and taxol
hyperstabilizes polyermized microtubules so can't break down mitotic spindle

Toxicity: myelosupression and hypersensitivity
Heparin
ATIII cofactor to decrease thrombin and Xa, short half life

follow PTT
Use: PE, MI, ACS, stroke, DVT, can be used during pregnancy

Toxicity: bleeding, throbocytopenia (HIT-binds factor IV and leads to hypercoaguable state), osteoporosis, drug-drug

Antidote:protamine
Lepirudin
directly inhibit thrombin
alternative to heparin for pts with HIT
warfarin
intereferes with synthesis and gamma carboxylation of vit K dependent factors. metabolized by P450 monitor PT
use: chronic anticoagulation, do not use in pregnant women can cross placenta

toxicity: bleeding, teratogenic, skin/tissue necrosis, drug-drug
Antidote: vit K or FFP
Aspirin
irreversible cox inhibitor so Tx2 can't be produced. increase bleeding time
Use: antipyretic, anti-inflammatory, anti-platelet, analgesic

Toxicity: castric ulceration, bleeding, hyperventilation, Reye's syndrome, tinnitus
Clopidogrel
inhibit platelet aggregation by irreversibly blockin ADP receptors. Inhibits fibringoen by blocking gpIIb/IIIa receptors
Use: ACS, coronary stenting, decreased incidence of thrombotic stroke
ticlopidine
inhibit platelet aggregation by irreversibly blockin ADP receptors. Inhibits fibringoen by blocking gpIIb/IIIa receptors
Use: ACS, coronary stenting, decreased incidence of thrombotic stroke

Toxicity: neutropenia
Abciximab
monoclonal antibody that binds to the glycoprotein receptor on active platelets and prevents aggregation
Use: ACS, percutaneous transluminal coronary angioplasty

Toxicity: bleeding, thrombocytopenia
cisplatin, carboplatin
cross link DNA
nephrotoxicity ad acoustic nerve damage
hydroxyurea
inhibits ribonucleotide reductase leading to a decrease in DNA synthesis
bone marrow suppression and GI upset
prednisone
may trigger apoptosis
cushing like syndrome, immunosuppression, cataracts, acne, osteoporosis, hypertension, peptic ulcers, hyperglycemia, psychosis
tamoxifen
SERM; breast antagonist and agonist in bone
may increase risk of endometrial cancer via partial agonist effect, hot flashes
raloxifene
SERM; breast antagonist and agonist in bone
hot flashes
trastuzumab
monoclonal antibody against HER 2 and can kill cells overexpression Her 2
cardiotoxicity
imatinib
bcr-abl tyrosine kinase inhibitor
fluid retention
rituximab
monoclonal antibody against CD20