Cytotoxic Antica Drugs Flashcards
Adverse effects of Anti Ca Drugs
(present in all anticancer drugs)
BM Suppression
Alopecia
Mucositis -Diarrhea
Hyperuricemia
Secondary Leukemia
Sterility
Alkylating Agents
MC site of alkylation -N7 of Guanine
If -Ifosfamide
Bus -Busulfan
Not -Nitrosoureas
present -Procarbazine
(Disulfiram like reaction)
Take -Temozolomide (DOC- Glioma)
My -Melphalan (used -MM)
Mechlorethamine
Cycle -Cyclophosphamide
Nitrosoureas
Carmustine (BCNU)
Lomustine (CCNU)
Semustine (Methyl CCNU)
•Cross BBB, Used -Brain Tumors
•S/E -Delayed BM Suppression &
Neutropenia
Ifosfamide & Cyclophosphamide
Metibolized by - Acrolein
Cause - Hemorrhagic Cystitis
Prevention of HC - MESNA
Tx of HC - Steroids
Platinum Compounds
Cisplatin
Carboplatin
Oxaliplatin (Colorectal Ca -FOLFOX)
MOA & S/E - same as Alkylating Agents
Cisplatin
-Most emetogenic anti Ca drug
•Early vomiting (<24hr) -Ondansetron,
-Granisetron
•Delayed vomiting (>24hr) -Neurokinin
-Aprepitant
-Nephrotoxicity (reversible)
•Slow IV infusion of cisplatin
•Saline loading
•Amifostine (also prevent radiation
induced Xerostomia)
-Ototoxicity (irreversible)
Antimetabolites - Drugs effecting Purine
Metabolism
(S- phase specific)
•6-Mercaptopurine
-Hepatotxic
-active metabolite of Azathioprine
-Metbolised by Xanthine oxidase
(Dec dose with Allopurino
combination)
•6-Thioguanine - Hepatotoxic
•Cladribine; DOC -HCL
•Fludarabine: DOC -CLL
Antimetabolites - Drugs effecting
pyrimidine Metabolism
(S- phase specific)
•5-Fluorouracil (5-FU]; causes Hand &
Foot syndrome
•Capecitabine; cause Hand & Foot sydrm
Given orally.
(Metabolism to 5-FU )
•Gemcitabine: DOC-Pancreatic
carcinoma
•Cytarabine: Causes cerebellar S/E
[MC S/E of 5-FU is Diarrhea]
Antimetabolites - Drugs effecting
Folic acid Metabolism
(S- phase specific)
DHFR
•Methotrexate
•Pemetrexed (used in mesothelioma)
•Pralatrexate-(used for peripheral T-cell
lymphoma)
-All cause; Megaloblastic Anemia
Methotrexate
•DHFR# (S-phase specific)
Uses;
C: Choriocarcinoma (DOC)
A: Acute leukemias (ALL,AML]
N: Non-Hodgkin’s lymphoma
C: Crohn’s disease
E: Ectopic pregnancy
R: Rheumatoid arthritis (DOC)
S/E; -megaloblastic anemia
-Hepatotoxic
DOC; -Chorio- carcinoma
-RA (MC used DMARD)
Methotrexate Poisoning - Folinic Acid (Leucovorin/ Citrovorum)
Drugs acting on Mitotic spindle
-M-phase specific
•Spindle formation #
Vincristine (marrow sparring)
Vinblastine
-S/E : peripheral neurophathy
SIADH
•Spindle breakdown #
Paclitaxel
-S/E : Allergy
•Newdrugs which act on mitotic spindle:
Eribulin - #tubules - Breast Ca
Ixabepilone. -Breast Ca
Estramustine -Prostate Ca
Topoisomerase #
Toposiomerase =#-ve coiling=#replictn
•Topoisomerase 1 #
Irinotecan -colorectal carcinoma
S/E: cholinergic (diarrhea, sweating)
•Topoisomerase 2#
Etoposide
- cause 2° Leukemia [Early in onset]
Absence of myelodysplastic stage
Anthracyclines
-Doxorubicin
-Daunorubicin
S/E : -Radiation Recall Syndrome
-Cardiotoxicity (Prevented by;
Dexrazoxane)
Miscellaneous Drugs
•Bleomycin
-Marrow sparing
-metabolized by bleomycin hydrolase
which is deficient at (cause-S/E)
Lungs- pulmonary fibrosis
Skin - Flagellated pigmentation
•L-Asparaginase
-Marrow sparing
-Used for ALL
S/E -Allergy
- Acute Pancreatitis
•As2O3 (Arsenic trioxide)
-Used in Acute Promyelocytic leukemia
(M3-AML)
(All-Trans Retinoic Acid can also be
used)
-Acts as maturation agent
•Thalidomide
-Used; multiple myeloma (acts
by # angiogenesis)
-C/l in pregnancy (Teratogenic:-
phocomelia)
-Powerful immunosuppressant
drug (inhibits TNF-)
S/E- peripheral neuropathy
- constipation
Adverse effects of important Anti Ca drugs
Thalidomide -PN, Constipation
Vincristine -PN, SIADH
Vinblastine -PN, SIADH
Cisplatin -Max vomiting
Ototoxicity
Nephrotoxicity
Bleomycin -Pulmonary fibrosis
Busulfan -Pulmonary fibrosis
Cyclophosphamide
-Pulmonary fibrosis
Doxorubicin -Cardiotoxicity
Daunorubicin -Cardiotoxicity
6-MP -Hepatotxicity
6-TG -Hepatotxicity
Cyclophosphamide
-Hemorrhagic Cystitis
Ifosfamide -Hemorrhagic Cystitis
Anthracycline -Radiation Recall Syndrm
Marrow Sparring Cytotoxic Drugs
•Bleomycin
•Vincristine
•L-Asparginase