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40 Cards in this Set
- Front
- Back
Alkylating agents are .............?
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Meclorethamine
Melphalan Cyclophosphamide Chlorambiocil |
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Oral Alkylating agents ?
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Chlorambiocil
Melphalan Cyclophosphamide |
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Injected alkylating agents ?
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Mechlorethamine
Cyclophasphamide |
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Alkylating agent with less side effects ( No alopecia - less nausea and vomiting ) ? and Why ?
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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 |
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Targeting in Cyclophasphamide ?
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It is hydrolyzed by phosphoramidase enzyme and cancer cells is more rich than normal cells in this enzyme ---> assist targeting .
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Cyclophosphamide act on cancer cells while it's not in normal ones ?
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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 ) |
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Acetyl cysteine is co-administered with Cyclophosphamide ?
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Bec Cyclophosphamide produce Acrolin which cause nephrotoxicity
Acetyl cysteine is a precurser for GSH ---> Detoxification |
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Aziridine used for brain cancers ?
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Thiotepa
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Alkyl sulphonate ?
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Busulfan
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Nitrosourea anticancer ?
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Carmustine (BCNU)
Lomustine (CCNU) |
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Mech. of action of Nitrosourea ?
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Dual Mechanism of action :
1- isocyanate ( react with ptn in cell giving carbamylated ptns ) 2- Cloroethyl diazohydroxyl ( Bind to DNA ) |
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Used for ovarian and testicular carcinoma ?
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Cisplatin
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Mannitol is co- administered with Cisplatin ?
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90% of Cisplatin is bounded to plasma ptn leading to toxicity
Mannitol is an osmotic diuretic to ++ Excretion and -- Toxicity . |
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Nitrosourea anticancers are used for brain cancers ?
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Lipophilic --> pass BBB
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Antibiotic used for treatment of cancer ?
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Mitomycin C
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Anticancers forms Superoxide ?
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Mitomycin C
Daunorubicin Doxorubicin |
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Hormonal treatment of cancer ?
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Prednisone ( used in combination with cyclophosphamide and Vincristine (CVP) )
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Used for treatment of hairy cell leukemia ?
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Interferon
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L-asparginase is selective to cancer cells ?
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It breakdown Aspargine in normal and cancer BUT:
normal cells contain (Aspargine synthase enzyme ) that regenerate aspargine While cancer cells don't . |
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Used for chronic myloid leukemia ?
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L-asparginase
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Act by inhibition of Ribonucleotide diphospho Reductase enzyme ?
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Hydroxy Urea
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Mechanisms of action of Anti metabolites ?
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1- Enzyme inhibitor .
2- Substrate analogue. Or both. |
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A pyrimidine antagonist ?
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5-Flourouracil
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Mech. of action of 5-FU ?
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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 ) |
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Purine antagonists ?
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6-Mercaptopurine
6-Thioguanine |
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HGPRtase stands for ?
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Hypoxathine Guanine Phosphate Ribose Transferase .
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Role of HGPRtase in 6-MP action ?
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Transform 6-MP to the active form---> Monpphosphate MP ( Thioinosinic acid )
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Mech. of action of Thioinosinic a' ?
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inhibit transformation of monoinosinic a' to AMP ---> inhibit DNA synthesis
( Enzyme inhibitor ) |
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Characters of HGPRtase ?
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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 . |
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Enzymes that metabolize 6-MP ?
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1- Guanase ---> Thioxanthine
2- Xanthine Oxidase ---> Thiouric a' |
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Allopurinol is co-administered with anti cancers ?
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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' . |
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Interaction bet . Allopurinol and 6-MP ?
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Allopurinol inhibit the metabolism of 6-MP ---> accumulation of the drug and toxicity
need to reduce the dose by 60%-70% |
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6-Thioguanine M.O.A ?
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1- substrate analogue ( transformed to triphosphate )
2- enzyme inhibitor . |
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M.O.A of Methotrexate ?
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Enzyme inhibitor ---> inhibit Dihydrofolate reductase enzyme
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Methotrexate have higher affinity to DHFR enzyme than DHF ?
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Amino gp in methotrexate is protonated in the physiological PH and interact by ionic interaction .
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Start materials of synthesis of Methotrexate ?
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Tetra-amino pyrimidine
+ Methyl amino benzoyl glutamic |
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DNA interchalating agents ?
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Daunorubicin
Doxorubicin Dactinomycin |
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M.O.A of Anthracycline ?
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1- DNA interchalating
2- Electron acceptor--->generate Superoxide 3- Metal chelation . |
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S.E of anthracycline ?
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Cardiac toxicity
|
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Used for Wilm's carcinoma ?
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Dactinomycin
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