Chemo Pharm Flashcards
Ondansetron
- serotonin antagonist
- acute antiemetic
- blocks serotonin at CTZ 3 receptor
- QT prolongation
- headaches, hiccups, constipation, cardiotoxicity
aprepitant
- NK-1 antagonist
- acute and delayed antiemetic
- blocks substance P
- drug interactions (CYP inducer)
- hiccups, fatigue
lorazepam
- benzodiazepine
- anticipatory antiemetic
- GABA mediated
-sedation, retrograde amnesia
dexamethasone
- glucocorticoid
- delayed antiemetic
- hormone
- reduces number of lymphocytic cells
- lymphocytic leukemias/lymphomas
- ALL, NHL
-glucose intolerance, insomnia, agitation, HTN
Prochlorperazine
Metoclopramide
- dopaminergic antagonists
- acute and delayed antiemetic
-extrapyramidal, sedation
alkylators
- cell cycle non specific
- form DNA cross links that inhibit replication
side effects:
- bone marrow suppression
- N/V, diarrhea
- sterility
- amenorrhea
- secondary malignancy
cyclophosphamide
- nitrogen mustard
- alkylator
- prodrug, needs liver activation
- binds to nucleophiles/purines
- breast CA, leukemia, lymphoma
- immunosuppressant
- cardiac NECROSIS
- delayed N/V
- hemorrhagic cystitis (ACROLEIN)
- neutropenia, lymphopenia, cardiotoxicity, SIADH
ifosfamide
- nitrogen mustard
- alkylator
- isomer to cyclophosphamide, with longer half life
- crosses BBB
- prodrug, needs liver activation
-sarcomas, lymphomas, uterine CA
- nephrotoxicity
- neurotoxicity
- hemorrhagic cystitis (ACROLEIN)
mesna
- counteracts ifosfamide induced hemorrhagic cystitis caused by acrolein
- binds acrolein in bladder
chlorambucil
- nitrogen mustard
- alkylating agent
AML
NHL
CLL
melphalan
- nitrogen mustard
- alkylating agent
- multiple myeloma
- primary myelofibrosis
- AML
cisplatin
- platinum analog
- alkylator
-testicular, ovarian, lung CAs
- severe acute and delayed N/V
- nephrotoxicity
- neurotoxicity (peripheral neuropathies, auditory impairment)
carboplatin
- platinum analog
- alkylator
-use if resistance develops to other analogs
- neuropathies
- increased toxicity if given before taxane
oxaliplatin
- platinum analog
- alkylating agent
- DNA adducts between bases
- colorectal, GI
- if resistance to other platinum analogs
- neurotoxicity triggered by COLD
- electrolyte abnormalites, myelosuppression, hepatotoxicity
dacarbazine
procarbazine
- triazenes
- alkylator
ABVD/MOPP regimens for Hodgkin’s
antimetabolics/analogs
- S phase specific
- block formation of DNA components
methotrexate
-antimetabolic
-S phase specific
-reversibly binds to dihydrofolate reductase
(no THF formed, no dTMP formed, no DNA synthesis)
-polyglutaminated form has higher efficacy
- nephrotoxicity, GI toxicity, hepatotoxicity, mucositis, myelosuppression
- methotrexate induced lung injury
- leucovorin rescue
- drain 3rd spaces
5-FU
- antimetabolic
- inhibits thymidylate synthase
- S phase specific
-breast, colorectal, head/neck, basal cell carcinoma
- myelosuppression
- mucositis/diarrhea, hand-foot syndrome
- CORONARY VASOSPASM (EKG changes)
- neurotoxicity
- PHOTOSENSITIVITY
- synergistic with leucovorin
hydroxyurea
- antimetabolic
- inhibits ribonucleotide reductase
- decreases WBC and platelet count
- S phase specific
- used for leukostasis in acute leukemia, sickle cell
- myelosuppression
cytrabine (Ara-C)
- pyrimidine analog
- inhibits DNA polymerase
- can cross BBB
- S phase specific
- AML, ALL, CML, NHL
- intrathecally to treat lymphomatous meningitis
- myelosuppression
- mucositis
- CNS toxicity (cerebellar, conjunctival)
- pulmonary edema
gemcitabine
- pyrimidine analog
- inhibits DNA polymerase, ribonucleotide reductase
- S phase specific
- Pacreatic, NSCLC, bladder CA, sarcoma
- myelosuppression, N/V, flu like sx, skin rash, proteinuria, hematuria
fludarabine
cladribine
- purine analogs
- interfere with DNA synthesis
- CLL
- immune damage to RBC causes hemolytic anemia
prednisone
- glucocorticoid
- homrone
- decreases lymphocytes
- lymphocytic leukemias/lymphomas
- glucose intolerance, insomnia, agitation, appetite, wight gain, fluid retention
Danazol
Dihydrotestosterone
- androgen hormone
- suppress pituitary output of FSH, LH
- used for bone marrow failure syndromes, myelodysplasia
- NHL, leukemia, testicular
-edema, flushing, HTN, hirsuitism, voice changes
flutamide
bicalutamide
- anti androgen (receptor antagonist)
- prostate cancer
- hot flashes, decr libido, gynecomastia
tamoxifen
raloxifene
competes with estrogen for binding to receptor
- breast CA
- menopausal sx, edema
- tumor flare
- DVT/PE
- endometrial hyperplasia
anastrozole
- aromatase inhibitor
- selective, reversible
- used in post menopausal women with breast CA
- hot flashes, tumor flare, edema, asthenia
letrozole
- aromatase inhibitor
- selective, reversible
-causes arthralgias, musculoskeletal pain, hot flashes, LFTs
leuprolide
-inhibits gonadotropin via negative feedback inhibition of the pituitary
-surge of estrogen, testosterone, then none
- premenopausal women with breast CA
- testicular CA
- tumor flare
- pain, flushing, peripheral edema, asthenia, hot flashes, gynecomastia, changes in serum lipids, bone loss long term
exemestane
- aromatase inhibitor
- IRreversible
-hot flashes, fatigue, headache
goserelin
-LHRH agonist
breast, prostate CA
danorubicin
- anti tumor antibiotic
- cell cycle non specific
- intercalates between DNA base pairs, breakage
- inhibits Topo II
- releases Fe to make free radicals
-leukemia
- myelosuppression
- alopecia
- N/V
- tissue necrosis (vesicant)
- cardiotoxicity (systolic HF)
- Fe release –> ROS
doxorubicin
- anti tumor antibiotic
- cell cycle non specific
- intercalates between DNA base pairs, breakage
- inhibits Topo II
- releases Fe to make free radicals
-lymphoma, solid tumors
- myelosuppression
- alopecia
- N/V
- tissue necrosis (vesicant)
- cardiotoxicity (systolic HF)
- Fe release –> ROS
bleomycin
- anti tumor antibiotic
- G2 phase specific
- binds to DNA
- free radical formation
-Hodgkins
- interstitial pneumonitis
- pulmonary fibrosis
- skin toxicity
vincristine
- vinca alkaloids
- inhibits microtubules
NHL, ALL
-neuropathies (paresthesias, decreased autonomic function –> constipation)
vinCristine = Constipation
vinblastine
- vinca alkaloids
- inhibits microtubules
Hodgkins, Testicular CA
-bone marrow suppression
vinBlastine = Bone marrow
vinorelbine
- vinca alkaloids
- inhibits microtubules
- NSCLC, breast CA
- bone marrow suppression
paclitaxel
- plant alkaloid
- Taxane
- enhances microtubule formation (cannot break down – stuck in metaphase)
-breast, lung, ovarian
- myelosuppression
- neuropathy (long nerves)
- hypersensitivity
- HAND FOOT syndrome
docetaxel
- plant alkaloid: taxane
- enhances microtubule formation (cannot break down, stuck in metaphase)
-breast, lung, ovarian
- myelosuppression
- neuropathy
- hypersensitivity
- HAND FOOT syndrome
irinotecan
topotecan
- plant alkaloid
- camptothecin
- TOPO I INHIBITOR
- S to G2 phase specific
-colon, ovarian, prostate, esophageal, non Hodgkins
- myelosuppression, neutropenia, thrombocytopenia
- diarrhea (leads to vol depletion)
ATROPINE (anticholinergic) helps early onset SLUDD sx
LOPERAMIDE helps with late onset SLUDD Sx
atropine
- anticholinergic
- helps with early onset SLUDD (diarrhea) sx of camptothecans
loperamide
-helps with late onset SLUDD (diarrhea) sx of camptothecans
trastuzamab
- mAb
- anti HER2
-breast CA
- infusion related (bronchospasm, dyspnea, angioedema, hypotension) from cytokine release
- myelosuppression
- cardiotoxicity
bevacizumab
- mAb
- anti VEGF
- blocks angiogenesis
-solid tumors
- impaired wound healing
- hypertension
- thrombotic events
- bleeding episodes
- GI perf
rituximab
- mAb
- anti CD20
- apoptosis, ADCC, complement activation
-CD20+ NHL, CLL, autoimmune diseases
- immunosuppressive
- HEP B REACTIVATION
- infusion related (hypotension, SOB, diaphoresis) due to cytokines
- tumor lysis
- skin reactions
- N/V
cetuximab
- mAb
- anti EGFR (tyrosine kinase receptor)
- decreases cell growth/differentiation
-solid tumors
- acneiform rash
- N/V
- hepatotoxicity
eculizumab
- mAb
- anti complement C5
imatinib
- tyrosine kinase inhibitor
- BCR-ABL inhibitor
- limits cell proliferation
-CML
- edema
- cytopenia
- elevated LFTs
- cardiotoxicity
erlotinib
- tyrosine kinase inhibitor
- EGFR inhibitor
- limits cell growth/proliferation
-lung cancer
- acneiform rash
- diarrhea
- interstitial lung disease
thalidomide
- imid
- antiangiogenesis (inhibit VEGF)
- immunomodulatory (inhibits TNF, induces apoptosis)
-multiple myeloma
- teratogenic
- neurotoxicity
- sedation
- depression
lenalidomide
- imid
- unknown MOA
- more potent than thalidomide
-multiple myeloma
- cytopenia
- thrombotic events
- teratogenic?
azacytidine
- demethylating agent
- un silences tumor suppressor genes
-MDS
- myelosuppression
- N/V
- diarrhea
decitabine
- demethylating agent
- un silences tumor suppressor genes
-MDS
- myelosuppression
- N/V
- diarrhea
bortezomib
- protease inhibitor
- disrupts normal protein metabolism, downregulation of NF-kB
- multiple myeloma
- NHL
- fatigue, malaise
- myelosuppression
- peripheral neuropathy
ATRA
-vitamin A analog
- acute promyelocytic leukemia
- allows differentiation of RAR
- curative
ipilimumab
- immune checkpoint inhibitor
- blocks CTLA-4
- augments T cell activation/proliferation
-AE: immune related (every “itis”) Tx: corticosteroids
nivolumab
- mAb
- anti PD1
- allows immune system to recogniza and kill tumor
AE
-hepatitis, gastritis, nephritis, thyroidits (Tx: corticosteroids)
leucovorin
- rescue for methotrexate
- synergistic with 5 FU
glucarpidase
- enzyme
- cleaves MTX
- absurdly expensive
L-asparaginase
- decreases MTX toxicity
- prevents cells from entering S phase
intrathecal drugs
- methotrexate
- C Ara
- Thiotepa (alkylator)
dexrazoxane
- iron chelator
- limits cardiotoxicity
- w/i 30 min of daunorubicin/doxorubicin
atropine
-for acute N/V for irinotecan
loperamide
-for delayed N/V for irinotecan
