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40 Cards in this Set

  • Front
  • Back
Alkylating agents are .............?
Meclorethamine
Melphalan
Cyclophosphamide
Chlorambiocil
Oral Alkylating agents ?
Chlorambiocil
Melphalan
Cyclophosphamide
Injected alkylating agents ?
Mechlorethamine
Cyclophasphamide
Alkylating agent with less side effects ( No alopecia - less nausea and vomiting ) ? and Why ?
Melphalan
It contain Phenyl alanine which is a natural amino acid ---> ++ active uptake by cancer cells that need it as it rapidly divides ---> ++ selectivity ---> -- S.E
Targeting in Cyclophasphamide ?
It is hydrolyzed by phosphoramidase enzyme and cancer cells is more rich than normal cells in this enzyme ---> assist targeting .
Cyclophosphamide act on cancer cells while it's not in normal ones ?
Cyclophosphamide --> Aldophosphamide which :
in normal cells ( Neutral PH ) : oxidized by aldehyde dehydrogenase to inactive metabolite

in cancer cells ( acidic PH ) : transformed to acrolin ( nephrotoxicity ) + phosphamide mustard ( Active )
Acetyl cysteine is co-administered with Cyclophosphamide ?
Bec Cyclophosphamide produce Acrolin which cause nephrotoxicity

Acetyl cysteine is a precurser for GSH ---> Detoxification
Aziridine used for brain cancers ?
Thiotepa
Alkyl sulphonate ?
Busulfan
Nitrosourea anticancer ?
Carmustine (BCNU)
Lomustine (CCNU)
Mech. of action of Nitrosourea ?
Dual Mechanism of action :
1- isocyanate ( react with ptn in cell giving carbamylated ptns )
2- Cloroethyl diazohydroxyl ( Bind to DNA )
Used for ovarian and testicular carcinoma ?
Cisplatin
Mannitol is co- administered with Cisplatin ?
90% of Cisplatin is bounded to plasma ptn leading to toxicity

Mannitol is an osmotic diuretic to ++ Excretion and -- Toxicity .
Nitrosourea anticancers are used for brain cancers ?
Lipophilic --> pass BBB
Antibiotic used for treatment of cancer ?
Mitomycin C
Anticancers forms Superoxide ?
Mitomycin C
Daunorubicin
Doxorubicin
Hormonal treatment of cancer ?
Prednisone ( used in combination with cyclophosphamide and Vincristine (CVP) )
Used for treatment of hairy cell leukemia ?
Interferon
L-asparginase is selective to cancer cells ?
It breakdown Aspargine in normal and cancer BUT:
normal cells contain (Aspargine synthase enzyme ) that regenerate aspargine
While cancer cells don't .
Used for chronic myloid leukemia ?
L-asparginase
Act by inhibition of Ribonucleotide diphospho Reductase enzyme ?
Hydroxy Urea
Mechanisms of action of Anti metabolites ?
1- Enzyme inhibitor .
2- Substrate analogue.
Or both.
A pyrimidine antagonist ?
5-Flourouracil
Mech. of action of 5-FU ?
5-FU + Ribose ---> Flourouracil monophosphate (FUMP) ---> False RNA ( Substrate analogue )


5-FU + Deoxyribose ---> Flourouracil deoxyuracil monophosphate (FdUMP) ---> inhibit Thymidilate synthase enzyme ---> inhibit DNA synthesis ( enzyme inhibitor )
Purine antagonists ?
6-Mercaptopurine
6-Thioguanine
HGPRtase stands for ?
Hypoxathine Guanine Phosphate Ribose Transferase .
Role of HGPRtase in 6-MP action ?
Transform 6-MP to the active form---> Monpphosphate MP ( Thioinosinic acid )
Mech. of action of Thioinosinic a' ?
inhibit transformation of monoinosinic a' to AMP ---> inhibit DNA synthesis
( Enzyme inhibitor )
Characters of HGPRtase ?
1- only in cancer cells ( selective )
2- not all cancer cells have the enzyme ( not broad spectrum )
3- cancer cells can develop resistance against the drug by stop producing HGPRtase .
Enzymes that metabolize 6-MP ?
1- Guanase ---> Thioxanthine
2- Xanthine Oxidase ---> Thiouric a'
Allopurinol is co-administered with anti cancers ?
Anticancer ---> cancer cells death ---> DNA breakdown ---> Purine (by xanthine oxidase ) ---> Uric a' ---> sever gout attack
Allopurinol ia oxidase xanthine inhibitor to avid formation of Uric a' .
Interaction bet . Allopurinol and 6-MP ?
Allopurinol inhibit the metabolism of 6-MP ---> accumulation of the drug and toxicity
need to reduce the dose by 60%-70%
6-Thioguanine M.O.A ?
1- substrate analogue ( transformed to triphosphate )
2- enzyme inhibitor .
M.O.A of Methotrexate ?
Enzyme inhibitor ---> inhibit Dihydrofolate reductase enzyme
Methotrexate have higher affinity to DHFR enzyme than DHF ?
Amino gp in methotrexate is protonated in the physiological PH and interact by ionic interaction .
Start materials of synthesis of Methotrexate ?
Tetra-amino pyrimidine
+
Methyl amino benzoyl glutamic
DNA interchalating agents ?
Daunorubicin
Doxorubicin
Dactinomycin
M.O.A of Anthracycline ?
1- DNA interchalating
2- Electron acceptor--->generate Superoxide
3- Metal chelation .
S.E of anthracycline ?
Cardiac toxicity
Used for Wilm's carcinoma ?
Dactinomycin