antimalignant, antimetabolite

CCS of S phase

solid tumors such as choriocarcinoma

osteogenic sarcoma

ALL

inhibit dihydrofolate reductase, responsible for reduction of THF which carries one carbon units responsible for synthesis of purines and pyrimidines

competitive inhibitor

oral, IV, intrathecal

not metabolized except at very high doses, then its cytP450 enzymes

potentially nephrotoxic

50% bound to plasma protein

can be displaced by sulfonamide, salicylate, tetracycline, chloramphenical, phenytoin

nephrotoxicity

myelosuppression

pulmonary toxicity

hepatotoxicity

GIT-mucositis

Leucovorin, folinic acid residue

antimetabolite

metastatic carcinoma of breast

carcinoma of GIT

hepatoma

carcinoma of ovary

CRC

bladder

prostate

pancreas

oropharyngeal cancers

interferes with RNA function by misincorporation of fluorodinated uridine in to RNA resulting in dysfunctional RNA

inhibits DNA synthesis

anorexia, nausea, alopecia, stomatitis, diarrhea, myelosuppression

cancer cells develop resistance to inhibitors of thymidylate synthase by changing sensitivity of enzyme to anticancer drug

this reduces drugs effectiveness

antimalignant, alkylating agent

CCNS

CLL

solid tumors i.e. breast cancer

NHL

ovarian carcinoma

neuroblastoma

immunosuppressive to prevent graft rejection

treatment of SLE

strong electrophile

prodrug that is converted to active nitrogen mustard

interferes with transcription and translation

dose levels which hit DNA are insufficient to effect RNA and protein synthesis

oral, IV

not IT because needs metabolic activation

cytP450 to active mustard form and acrolein which causes chemical cystitis

given with high water load, alkaline urine prevents reabsorption of parent drug in metabolite

Mesna

reduces chemical cystitis

myelosuppression

permanent amenorrhea

azoospermia

leukemogenic

cardiotoxic in high doses

has renal and bladder toxicity

water intoxication leading to hyponatremia

cytotoxic antibiotic

solid tumors of breast, endometrium, testes, lung

osteogenic sarcoma, Ewing's sarcoma

metastatic carcinoma of thyroid

intercalates with DNA and binds helical groove

prevents topoisomerase II from resealing helical breaks

causes free radical formation (highly destructive)

development of abnormal transport proteins - controls "in" traffic

mdr gene will overexpress glycoprotein regulating "out" traffic

single IV fast running infusion

repeated after 21 days

severe local vesicant if extravasation occurs

local vesicant if extravasation occurs

Dimethyl sulfoxide swabbed onto vesicants

serious cardiomyopathy

with repeated doses - supraventricular arrhythmia may occur

cytotoxic antibiotic

CCNS

testicular cancer

squamous carcinomas of head, neck, lungs

lymphomas

fragmentation of DNA by free radical formation

will also cause chromosomal fragmentation

cell will accumulate in G2 phase of cell cycle

pulmonary toxicity manifests as dry cough

pulmonary fibrosis

hyperthermia

skin blisters

antimalignant antimitotic

CCS

pediatric leukemia

Hodgkins diseases

rhabdomyosarcoma

lymphomas

neuroblastomas

mdr gene mutation

spindle poisons

bind to tubulin and prevent assembly of microtubules

act in M phase of cell cycle

peripheral neuropathy

sensory and motor parasthesia

autonomic neuropathy

highly neurotoxic

IV

antimalignant antimitotic

CCS

Hodgkins diseases

testicular CA

binds to tubulin and prevents assembly of microtubules

acts in M phase of cell cycle

associated with mdr gene mutation

reversible

myelosuppression

leukopenia

alopecia

fecal and bile

fecal and bile

fecal and bile

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