Antineoplastic Drugs Flashcards
1
Q
Methotrexate
A
Folic Acid Analogue (Antimetabolite)
- Hepatotoxicity, category X “teratogenic”.
- PPIs increase plasma concentrations of MTX.
2
Q
6-Mercaptopurine
A
Purine Analogue (Antimetabolite)
- Pharmacogenomics: screen for Thiopurine S-Methyltransferase. (Responsible for metabolism)
*For Azathioprine as well.
- 6MP dose should be reduced by 75% when used with Allopurinol.
3
Q
Fludarabine
A
- Purine analogue, antimetabolite.
- Potent immunosuppressant (+++ w/ glucocorticoids)
- increased risk for opportunistic infections e.g. pneumocystis jirovecii pneumonia (PCP)
- co-trimoxazole at least 3 times a week, and continue for few weeks/up to a year after d.c.
4
Q
5-Fluorouracil
A
- pyrimidine analogue, antimetabolite.
- pharmacogenomics: screen for Dihydro-pyrimidine Dehydrogenase (DPD) enzyme. (Absence = toxicity)
5
Q
Cytarabine
A
- cytidine analogue, antimetabolite
- cytarabine syndrome: chemical conjunctivitis
6
Q
Cyclophosphamide & Ifosfamide
A
- alkylating agents, nitrogen mustard
- hemorrhagic cystitis and bladder fibrosis, reduced by:
- Slow IV infusion
- Adequate hydration
- Mesna (w/ Ifosfamide)
7
Q
Carmustine, Lomustine and Streptozocin
A
- alkylating agents, nitrosoureas
- highly lipid soluble, effective in the treatment of brain tumors
8
Q
Busulfan
A
- alkylating agent, alkylsulfonate
- pulmonary fibrosis (busulfan lung)
- antiepileptic used as prophylaxis from Busulfan-induced seizures
9
Q
Cisplatin, Carboplatin and Oxaliplatin
A
- alkylating agents, platinum analogues
- severe persistent vomiting, nephrotoxicity, ototoxicity ‘tinnitus’ and neurotoxicity. (Optic neuritis and peripheral neuropathy)
10
Q
Doxorubicin/Daunorubicin
A
- cytotoxic antibiotics, anthracyclines — DNA Function, Topoisonerase I and II inhibitors.
- the red devil ‘doxorubicin,’ due to the dark red color of the veins
- irreversible dose-dependent cardiotoxicity
- dexrazoxane is a cardioprotective against anthracyclines cardiotoxicity
11
Q
Bleomycin
A
- cytotoxic antibiotic
- pulmonary toxicity (bleomycin lung)
- skin toxicity (hyperpigmentation of hands)
12
Q
Vincristine, Vinblastine and Vinorelbine
A
- vinca alkaloids (microtubule inhibitors) — mitotic spindle
- neurotoxic
- only IV, fatal if given intrathecally
13
Q
Paclitaxel, Docetaxel and Cabazitaxel
A
- Taxanes, microtubule inhibitors — mitotic spindle
- Used in lung cancers
- Hypersensitivity reactions
- Neurotoxic (peripheral neuropathy)
14
Q
Tamoxifen
A
- SERM — Endocrine Therapy
- Prodrug (activated by CYP2D6), slow metabolizers and CYP2D6 inhibitors will suffer lowered efficacy.
- Most potent metabolite is Endoxifen.
- Increased risk of Thromboembolism (DVT, PE and stroke) and endometrial cancer.
- Used in Estrogen Receptor Positive Breast Cancer.
15
Q
Fulvestrant
A
- SERD ‘degrader, — Endocrine Therapy.
- Used in ER-positive breast cancer.
- Pure antagnoist, no partial agonist effects. No endometrial cancer risk.
16
Q
Anastrozole, Letrozole and Exemestane
A
- Aromatase Inhibitors — Endocrine Therapy.
- Letrozole & Anastrozole (non-steroidal) are ‘reversible,’ while Exemestane (steroidal) is irreversible.
- Aromatization (Testosterone —to— Estrogen in adipose tissues)
17
Q
Leuprorelin, Goserelin and Triptorelin
A
- GnRH Analogues — Endocrine Therapy.
- They are used in hormone-dependent breast cancer and endometriosis.
18
Q
Cyproterone Acetate (Androcur)
A
- Antiandrogen — Endocrine Therapy.
- Synthetic steroidal antiandrogen, used in prostate cancer.
- Flutamide, Nilutamide and Bicalutamide are synthetic antiandrogens for the same use.
19
Q
Rituximab
A
- Anti-CD20 (CD20 is found on normal and malignant B lymphocytes)
- Used in blood cancers:
- non-Hodgkin’s Lymphoma
- Chronic Lymphocytic Leukemia
- Autoimmune diseases and organ transplantation.
— Severe infusion reactions. FATAL.
— RISK FOR PML (If JCV-positive)
20
Q
Trastuzumab and Pertuzumab
A
- Anti-HER2 (Human Epidermal Growth Factor Receptor 2)
- HER2-positive breast cancer.
- Risk for HF (worsened w/ anthracyclines)
21
Q
Cetuximab and Panitumumab
A
- EGFR Inhibitor.
- Used in Metastatic Colorectal Cancer Wild-Type RAS ONLY. Doesn’t work in mutations.
- Cetuximab is also used in head and neck cancer.
22
Q
Bevacizumab
A
- Anti-VEGF (Vascular Endothelial Growth Factor) — inhibits angiogenesis.
- Used in:
- Colorectal Cancer
- Lung Cancer
- Renal-cell Carcinoma
— USED IN EYE DISEASES SUCH AS AGE-RELATED MACULAR DEGENERATION.
23
Q
Daratumumab
A
- ANTI-CD38 — CD38 is expressed at relatively low levels on normal lymphoid and myeloid cells, over expressed in multiple myeloma cells.
- Used in Multiple Myeloma (in combination with Bortezomib)
24
Q
Sunitinib
A
- Tyrosine Kinase Inhibitor
- Used in:
- Renal cell carcinoma
- Gastrointestinal Stromal Tumor
- Pancreatic Neuroendocrine Tumors
25
Sorafenib
- Tyrosine Kinase Inhibitor
- Used in:
1. Advanced Renal Cell Carcinoma
2. Primary Liver Cancer
3. Radioactive Iodine Resistant Advanced Thyroid Carcinoma
26
Imatinib, Nilotinib, Dasatinimb and Ponatinib
- Tyrosine Kinase Inhibitors
- Specific inhibitors for BCR-ABL Tyrosine Kinase produced by Philadelphia Chromosome in:
1. Chronic Myelogenous Leukemia (CML)
2. Acute Lymphoblastic Leukemia (ALL)
— Used in Philadelphia positive (Ph+) CML/ALL.
27
Crizotinib, Osimertinib, Afatinib, Gefitinib and Erlotinib
- Specific Tyrosine Kinase Inhibitors for EGFR
- Used in Non-small Cell Lung Cancer (NSCLC) with EGFR-positive mutations
— Erlotinib is used in NSCLC and Pancreatic Cancer.
28
Pegaptanib
- ANTI-VGEF TKI
- Used in age-related macular degeneration.
29
Palbociclib, Ribociclib and Abemaciclib
- Cyclin-dependent Kinase (CDK) Inhibitors — CDK4/CDK6.
- HR-positive and HER2-negative breast cancer. (Combination w/ Fulvestrant)
30
Etoposide, Teniposide, Topotecan and Irinotecan
- Plant alkaloids—Topoisomerase II inhibitors.
- Solid Cancers.
31
L-Asparaginase
- Used in childhood Acute Lymphocytic Leukemia.
32
Abiraterone Acetate
Steroidal CYPA17A1 inhibitor—Androgen Synthesis inhibitor.
In combination w/ Prednisone in metastatic castration-resistant Prostate Cancer.
33
Enzalutamide
Oral synthetic non-steroidal antiandrogen.
Used in metastatic castration-resistant Prostate Cancer.
