📌CHEMO DRUGS Flashcards
Cause cross-linking and abnormal base-pairing of DNA strands
ALKYLATION
Inhibit DNA replication
ALKYLATION
Nitrogen mustard used as a chemical warfare agent
Mechlorethamine
Cytotoxic, mutagenic, carcinogenic
Mechlorethamine
Metabolized in the P450 system
Cyclophosphamide
For breast CA, ovarian CA, Hodgkins and nonHodgkins lymphoma, all leukemias
Cyclophosphamide
For organ transplantation
Cyclophosphamide
Adverse effects of CYCLOPHOSPHAMIDE
Hemorrhagic cystitis
GI effects
Alopecia
Bone marrow suppression
Hemorrhagic cystitis
MESNA
Neurotoxicity
Ifosfamide
Ethylenimenes or amethylmelamines
Thiotepa, Altretamine (hexamethylmelamine)
Nitrosoureas
Carmustine, Lomustine, Semustine, Stretozocin
For brain tumors
Carmustine, Lomustine
Specially toxic to beta cells of islets of Langerhans
Streptozocin
For brain tumors, melanoma, GI cancer
Lomustine, Carmustine, Semustin, Streptozocin
Adverse effects of Nitroureas
CNS toxicityy
Nausea and vomiting
Bone marrow suppression
Skin flushing
Triazenes or Triazines
Dacarbacine
Melanoma
Dacarbacine
Platinum coordination complex
Carboplatin, Cisplatin
Platinum coordination complex -> cross links DNA -> prevents DNa synthesis
Cisplatin
For testicular, bladder, lung, ovarian CA
Cisplatin
Adverse effects of Cisplatin
Nephrotoxicity
Ototoxicity
Paresthesias
Axonal neuropathy
Cisplatin
Severe persistent vomiting
Nephrotoxicity
Cisplatin
Mild nausea and vomiting
Not nephro, neuro or ototoxic
Myelosuppression
Carboplatin
Intercalation (slides in between the DNA)
Antitumor antibiotics
Anthracyclines
Daunorubicin, Doxorubicin, Epirubicin, Idarubicin
Binds to sugar-phosphate backbone of DNA -> blocks synthesis
Doxorubicin, Daunorubicin
Adverse effects of Doxorubicin, Daunorubicin
Cardiotoxicity
Alopecia
Cardiotoxicity
Dexrazoxane
Anthracendiones
Metixantrone
Binds to double helix of DNA and for complex with it
Inhibits RNA polymerase
Dactinomycin
For Wilms tumor, rhabdomyosarcoma, choriocarcinoma, Kaposi sarcoma
Dactinomycin
Adverse effects of Dactinomycin
Bone marrow suppression
Skin reaction
GI irritation
Cell cycle specific (G2 phase)
Bleomycin
Generates free radicals, binds to DNA, causes strand breaks and inhibits DNA synthesis
Bleomycin
For testicular CA and Hodgkins disease
Bleomycin
Adverse effects of Bleomycin
Pulmonary toxicity
Fever and chills
Allergy
Adverse effects of Bleomycin
Pumonary fibrosis
Unusual: Myelosuppression is rare
Drugs causing pulmonary fibrosis
Bleomycin/Busulfan
Amiodarone
Nitrofurantoin
Methotrexate
Structural analogs of naturally occurring substrates for biochemical reactions
Antimetabolites
Inhibit DNA synthesis
Antimetabolites
Folic acid antagonist that prevents conversion of dihydrofolate to tetrahydrofolate that decreeases synthesis of thymidilate, amino acids, purine nucleotides
Methotrexate
Folinic acid
Leucovorin
DMARDs
Methotrexate
Renal damage
Abortifacient
Hepatotoxicity
Common: stomatitis, myelosuppression, erythema, rash, urticaria, alopecia, vomiting, diarrhea
Methotrexate
For chorioCA, lung CA, ALL, NHL, breast CA
Methotrexate
Also used for psoriasis, RA
Methotrexate
To minimize toxic effects of methotrexate
Leucovorin rescue
Adverse effects: neurotoxicity, macrovesicular fatty change in the liver, pulmonary infiltration and fibrosis, vomiting, nausea
Methotrexate
Purine analogs
Mercaptopurine, athioguanine, azathioprine
Alkylation
Mechlorethamine