Plant Alkaloids Flashcards
Extracts from Catharanthus roseus
Vincristine
Vinblastine
Vinrosidine
Vinorelbine
Vinleurosine
Cancer treated by Vincristine and Vinblastine
Leukemia, Lymphoma, Testicular Cancer
Vinca Alkaloids mechanism is common as
Colchicine, Podophyllotoxin, Taxanes , epothilones,.
Block cell proliferation in metastasis
How Vincristine and Vinblastine act
Bind to tubulin, no microtubules, mitotic arrest, dissolution of Mitotic Spindle and interference with chromosome segregation
Most important use Vincristine and Vinblastine
With bleomycin, Cisplatin for testicular therapy
Other clinical uses of Vincristine and Vinblastine
Kaposi sarcoma, Hodgkin’s lymphoma neuroblastoma, breast and chorio carcinoma
Toxicities of Plant alkaloids
Leukopenia, alopecia, GIT , dermatitis, myelo toxicity and neurotoxicity
Gene responsible for resistance in plant alkaloids
MDR gene… And it’s glycoprotein…
Paclitaxel is obtained from
Bark of western yew tree
Anti tumor activity of paclitaxel is due to
Taxane ring as it’s nucleus
MOA of paclitaxel
Antagonize the disassembly of microtubules by binding with the B-tubulin…
Resistance to paclitaxel occur due to
Mdr-1 and p-glycoprotein…
Therapeutic use of paclitaxel
Metastatic ovarian and breast cancer
Toxicities of Paclitaxel
Bone marrow suppression, neutropenia, peripheral neuropathy, etoposide
Etoposide blocks cell division in which phase
S and G 2 phase
MOA of etoposide
Drug form tertiary complex with topoisomerase 2 and DNA…
Double strand DNA breakage
Clinical use of etoposide
With bleomycin and Cisplatin
Testicular Cancer, non Hodgkin’s lymphoma, small cell lung cancer…
Toxicities of Etoposide
Hypotension, bronchospasm,
What is dactinomyocin
1st crystalline antibiotic species obtained from streptomyces
MOA of dactinomyocin
Drug DNA complex inhibit transcription of DNA by blocking DNA dependent RNA polymerase
How dactinomyocin is used for treatment of Wilm tumor and rhabdomyosarcoma
In combination with Vincristine and Cyclophosphamide
Dactinomyocin toxicities
Hematopoietic suppression, pancytopenia, ulceration
What is bleomycin
DNA Cleaving Group
Mixture of 2 copper chelating peptides
A2 and B2….
MOA of bleomycin
Bind to DNA through it’s amino terminal peptide and activated free radicals cause DNA breakage
Explain the mechanism of bleomycin
Oxidation of DNA-Bleomycin iron complex which act as ferrous oxidase..
It transfer electrons to molecular oxygen which lead to chromosomal aberrations
Bleomycin effects which phase
G2
Clinical use of bleomycin
Germ cell tumors of testis and ovaries with Cisplatin and Vinblastine
WHAT IS ABVD
Adriamycin, bleomycin, Vinblastine, Dacarbazine
ABVD is used for
Carcinoma of head, neck, Hodgkin’s and non Hodgkin’s, esophagus,
Toxicities of ABVD
Hyperpigmentation, Hyperkeratosis, pulmonary toxicities and anorexia
