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39 Cards in this Set

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PK / MOA: AGENTS ARE NOT CELL CYCLE-SPECIFIC ; REPLICATING CELLS ARE SUSCEPTIBLE TO AKLYLATION IN LATE G1 AND S PHASES OF THE CELL CYCLE AND EXPRESS BLOCK IN G2
; ALKYLATING AGENTS
PK / MOA: ORAL ; IV ; CYP TO ACTIVE METABOLITE AND UROTOXIC METABOLITE ; HEPATIC ELIM
NITROGEN MUSTARDS ; CYCLOPHASPHAMIDE
PK / MOA: IV ; ACTIVE METABOLITE AND UROTOXIC METABOLITE
; ISOSFAMIDE
PK / MOA: IV ; RENAL ELIM ; HIGHLY REACTIVE ; Pt > 90% PROTEIN BOUND (COVALENT) ; RAPIDLY TAKEN UP BY TUMOR AND OTHER TISSUES ; POOR CNS PENETRATION ; NONENZYMATIC INACTIVATION (UNBOUND FRACTION) ; COVALENT BINDING TO GLUTATHIONE, THIOSULFAT ; SECONDARY t1/2 UP TO 5 DAYS
PLATINUM ANALOGS ; CISPLATIN
PK / MOA: IV ; RENAL ELIM ; LESS REACTIVE ; MAJORITY OF DRUG UNBOUND
; CARBOPLATIN
PK / MOA: IV ; RENAL ELIM ; HIGHLY REACTIVE ; SIMILAR TO CISPLATIN
; OXLIPLATIN
PK / MOA: A SUBSTANCE THAT IS SIMILAR IN STRUCTURE TO A METABOLITE OR ENZYMATIC SUBSTRATE, BUT INTERFERES WITH THE NORMAL DIVISION AND FUNCTION OF CELLS ; S PHASE OF CELL CYCLE
; ANTIMETABOLITES
PK / MOA: PARENTERAL ; ORAL (SATURABLE) ; -50% PLASMA PROTEIN BOUND --> NARROW THERAPEUTIC WINDOW --> DRUGS THAT DISPLACE METHOTREXATE FROM ALBUMIN --> INCR. RISK OF SEVERE MYELOSUPPRESSION ; DISTRIBUTES IN BODY WATER ; POOR PENETRATION OF CSF, HIGH DOSE MTX ACHIEVES CYTOTOXIC LEVELS ; ENTER CELLS VIA REDUCED FOLATE TRANSPORTER --> POLYGLUTAMATED (RETENTION IN CELL) ; RENAL EXCRETION ; MAINLY UNCHANGED DRUG BY GLOMERULAR FILTRATION AND TUBULAR SECRETION ; IT IS A SUBSTRATE OF PgP AND OATP1B1 ; COMPETITIVE BINDING TO DHFR --> INHIBITS FH4 FORMATION --> SHUTS DOWN ONE-ARBON TRANSFER RXNS --> DECR. DE NOVO SYNTHESIS OF PURINE NUCLEOTIDES AND THYMIDYLATE --> DECR. DNA AND RNA SYNTHESIS AND ULTIMATELY IMPAIRS THE SYNTHESIS OF THYEMIDYLATE AND PURINE NUCLEOTIDES ; IT INDUCES p53 AND CELL-CYCLE ARREST
FOLATE ANTAGONISTS ; METHOTREXATE
PK / MOA: IV ; DISTRIBUTES TO BODY FLUIDS AND CSF ; ENZYMATIC RIBOSYLATION AND PHOSPHORYLATION TO THE ACTIVE NUCLEOTIDE ; METABOLISM OF DRUG --> DPD (FOUND IN LIVER, INTESTINAL MUCOSA, TUMOR AND OTHER TISSUES) ; PARTIALLY METABOLIZED TO CO2 (EXCRETED BY LUNGS) ; RENAL ELIMINATION (5% UNCHANGED DRUG) ; t1/2 (PLASMA) 6-20 MINUTES ; IT HAS PROLONGED t1/2 DEPENDING ON THE TISSUE
FLUROPYRIMIDINES ; FLUORORURACIL (5-FU)
PK / MOA: ORAL PRODRUG CONVERTED IN TISSUE TO 5-FU
; CAPECITABINE
PK / MOA: PARENTERAL ; CLEARED RAPIDLY, EXTENSIVE HEPATIVE DEGRADATION BY CYTIDINE DEAMINASE TO INACTIVE COMPOUND ; RENAL EXCRETION PRIMARILY ; ELIM t1/2 1-3 HOURS ; CYTIDINE DEAMINASE ACTIVITY IS HIGH IN MANY NORMAL TISSUES BUT LOWER IN AML CELS AND OTHER HUMAN TUMORS
DEOXYCYTIDIDINE ANALOGS ; CYTARABINE (ARA-C)
PK / MOA: DRUG GETS INCORPORATED INTO RNA AND DNA --> STRAND BREAKS AND BASE MISPAIRING ; TIMP (SUBSTRATE) INHIBITS NEW FORMATION OF RIBOSYL-5-PHOSPHATASE AND CONVERSION OF IMP TO PURINE NUCLEOTIDES
PURINE ANALOGS ; 6-MERCAPTOPURINE (6-MP)
PK / MOA: IV ; WIDELY DISTRIBUTED (RAPID UPTAKE OF DRUG BY HEART, KIDNEYS, LUNGS, LIVER AND SLEEN ; THEY DO NOT PENETRATE BBB OR TESTES ; HEPATIC METABOLISM TO AN ACTIVE ALCOHOL INTERMEDIATE (DOSE REDUCTION IS REQUIRED IN PT'S WITH ABNORMAL BILIRUBIN LEVELS) ; MAINLY BILIARY EXCRETION AND SOME URINARY EXCRETION ; MULTIPHASIC ELIMINATION HALF-LIVES
; ANTICANCER ANTIBIOTICS
PK / MOA: IV ; WIDELY DISTRIBUTED (RAPID UPTAKE OF DRUG BY HEART, KIDNEYS, LUNGS, LIVER AND SLEEN ; THEY DO NOT PENETRATE BBB OR TESTES ; HEPATIC METABOLISM TO AN ACTIVE ALCOHOL INTERMEDIATE ; TURNS URINE RED
ANTHRACYCLINES ; DAUNORUBICIN
PK / MOA: HEPATIC METABOLISM TO AN ACTIVE ALCOHOL INTERMEDIATE: CYP2D6, 3A4 AND PgP ; WEAK TO MODERATE INHIBITOR OF CYP2B6, 2D6, CYP3A4 ; INDUCER OF PgP ; TURNS URINE RED
; DOXORUBICIN
PK / MOA: BIND TO BETA-TUBULIN AND BLOCK POLYMERIZATION WITH ALPHA-TUBULIN ; CELLS BLOCKED IN MITOSIS --> APOPTOSIS
MICROTUBULE INHIBITORS ; VINBLASTINE (VINKA ALKALOIDS)
PK / MOA: BIND TO BETA-TUBULIN AND BLOCK POLYMERIZATION WITH ALPHA-TUBULIN ; CELLS BLOCKED IN MITOSIS --> APOPTOSIS
; VINCRISTINE (VINCA ALKALOIDS)
PK / MOA: IV ; WIDELY DISTRIBUTED BUT DO NOT PENETRATE CNS ; EXTENSIVE CYP-MEDIATED HEPATIC METABOLISM ; BILIARY SECRETION ; FECAL EXCRETION ; CLEARANCE IS NON-LINEAR (MAY BE RELATED TO THE ETHANOL-POLYOXYETHYLATED CASTOR OIL DILUTENT) ; HEPATIC CYP2C8, 3A4 METABOLISM ; ALSO A SUBSTRATE OF PgP ; PRIMARILY FECAL EXCRETION OF METABOLITES ; t1/2 DOSE-DEPENDENT, MEAN TERMINAL t1/2 13-52 HOURS ; ENHANCE TUBULIN POLYMERIZATION AND ANTAGONIZED MICROTUBULE DISASSEMBLY
; PACLITAXEL (TAXANES)
PK / MOA: IV ; WIDELY DISTRIBUTED BUT DO NOT PENETRATE CNS ; EXTENSIVE CYP-MEDIATED HEPATIC METABOLISM ; BILIARY SECRETION ; FECAL EXCRETION ; LINEAR CLEARANCE ; HEPATIC CYP3A4 METABOLISM ; ALSO A SUBSTRATE OF PgP ; PRIMARILY FECAL EXCRETION OF METABOLITES ; TERMINAL t1/2 - 11 HOURS ; ENHANCE TUBULIN POLYMERIZATION AND ANTAGONIZED MICROTUBULE DISASSEMBLY
; DOCETAXEL (TAXANES)
PK / MOA: IV ; HEPATIC METABOLISM VIA CARBOXYLESTERASE TO ACTIVE CLOSED-RING METABOLITES SN-38 AND TOPOTECAN LACTONE ; IN BIOLOGIC FLUIDS, SN-38 AND TOPOTECAN LACTONE ARE HYDROLYZED TO INACTIVE OPEN RING CARBOXYLATE FORMS ; A DYNAMIC EQUILIBRIUM EXISTS BETWEEN THE LACTONE RING AND THE CARBOXYLATE FORM ; ACIDIC pH FAVORS THE LACTONE FORM AND BASIC pH FAVORING FORMATION OF THE INACTIVE, OPEN RING CONFIGURATION ; SN-38 (UGT1A1) --> GLUCURONIDE METABOLITE (INACTIVE) - DOSE REDUCTION IS RECOMMENDED IN PT'S WITH HOMOZYGOUS UGT1A1*28 ALLELE (DECR. UGT ACTIVITY --> INCR. TOXICITY)
TOPOISOMERASE I INHIBITORS ; IRINOTECAN (CAPTOTHECINS)
PK / MOA: ORAL, IV, HIGHLY BOUND TO PLASMA PROTEINS AND WIDELY DISTRIBUTED ; EXTENSIVE HEPATIVE METABOLISM (CYP3A4, PgP) ; RENAL EXCRETION (UNCHANGED DRUG) ; ARREST IN LATE S OR EARLY G2 PHASE
TOPOISOMERASE II INHIBITORS ; ETOPOSIDE (EPIPODOPHYLLOTOXINS)
PK / MOA: INHIBITION OF THE TYROSINE KINASE DOMAIN OF THE BCR-ABL ONCOPROTEIN (9:22 TRANSLOCATION) ; OCCUPY ATP BINDING POCKET --> PREVENT SUBSTRATE PHOSPHORYLATION AND DOWNSTREAM ACTIVATION OF SIGNALS
; PROTEIN TYROSINE KINASE INHIBITORS
PK / MOA: BINDS TO A SEGMENT OF THE KINASE DOMAIN THAT FIXES THE ENZYME IN A CLOSED STATE
BCR-ABL KINASE INHIBITORS ; IMATINIB (GLEEVAC)
PK / MOA: BINDS TO BOTH OPEN AND CLOSED CONFIGURATIONS OF THE BCR-ABL KINASE
; DASATINIB (SPRYCEL)
PK / MOA: BINDS TO A SEGMENT OF THE KINASE DOMAIN THAT FIXES THE ENZYME IN A CLOSED STATE
; NILOTINIB (TASIGNA)
PK / MOA: ORAL, HEPATIC CYP3A4 METABOLISM, TERMAL t1/2 - 40 HOURS ; COMPETITIVELY INHIBITS ATP BINDING AT ACTIVE SITE OF THE KINASE --> INHIBITION OF TYROSINE KINASE AND ITS SIGNALING CASCADE
EPIDERMAL GROWTH FACTOR INHIBITORS ; ERLOTINIB (TARCEVA)
PK / MOA: ORAL, HEPATIC CYP3A4 METABOLISM, TERMAL t1/2 - 40 HOURS ; COMPETITIVELY INHIBITS BINDING OF EPITHELIAL GROWTH FACTOR TO ITS RECEPTOR, EGFR --> BLOCKS RECEPTOR DIMERIZATION AND PHOSPHORYLATION AND LIGAND-DEPENDENT SIGNALING --> INHIBITS CELL GROWTH --> APOPTOSIS
; CETUXIMAB (ERBITUX)
PK / MOA: IV ; DOSE-DEPENDENT PK ; SS LEVLS ACHIEVED IN 16-32 WEEKS ; HIGH AFFINITY SELECTIVE BINDING TO EXTRACELLULAR DOMAIN OF HER2 ; INHIBITS HOMO- AND HETERODIMERIZATION OF THE RECEPTOR --> PREVENTS TYROSINE KINASE ACTIVATION AND DOWNSTREAM SIGNALING ; BLOCKS ANGIOGENIC EFFECTS OF HER2 SIGNALING ; INDUCES ANTIBODY-DEPENDENT CELL-MEDIATED CYTOTOXICITY (ADCC)
HER2 / NEU INHIBITORS ; TRASTUZUMAB (HERCEPTIN)
PK / MOA: IV ; DOSE-DEPENDENT PK ; SS LEVLS ACHIEVED IN 16-32 WEEKS ; REVERSIBLY BINDS TO AN INTERNAL SITE ON THE RTK (USUALLY ATP BINDING POCKET) --> BLOCKS PHOSPHORYLATION AND ACTIVATION OF DOWNSTREAM SECOND MESSENGERS ; ALSO INHIBITS A TRUNCATED FORM OF HER2R (LACKS A TRASTUZUMAB-BINDING DOMAIN)
; LAPATINIB (TYKERB)
PK / MOA: IV EVERY 2-3 WKS ; MEAN PLASMA t1/2 - 4 WKS ; BINDS TO AND NEUTRALIZES VEGF, PREVENTING IT FROM ASSOCIATING ITS ENDOTHELIAL RECEPTORS
ANGIOGENESIS INHIBITORS ; BEVACIZUMAB (AVASTIN)
PK / MOA: ORAL ; METABOLIZED BY CYP3A4 TO ACTIVE METABOLITE (SU12662) AND INACTIVE PRODUCTS ; SUBSTRATE OF PgP ; INHIBITS PgP AND OTHER EFFLUX TRANSPORTERS, t1/2 80-110 HOURS ; ONCE DAILY DOSE x4 WKS THEN 2 WEEKS OFF ; SMALL MOLECULAR MULTIKNASE INHIBITORS --> COMPETITIVE INHIBITION OF ATP BINDING TO THE TYROSINE KINASE DOMAIN OF TYROSINE KINASES
; SUNITINIB (SUTENT)
PK / MOA: IV ; MOST TISSUES (EXCEPT TESTES, EYES AND CNS) ; SEVERAL CYP ENZYMES ; EXCRETED IN BILE AND URINE t1/2 - 9-15 HOURS ; SPECIFIC / SELECTIVE REVERSIBLE INHIBITOR OF THE 26S PROTEASOME ; BORONIC ACID GROUP OF FORMS A COMPLEX WITH THE THREONINE HYDROXYL GROUP IN THE CHYMOTRYPSIN-LIKE ACTIVE SITE --> INHIBITING PROTEOLYSIS --> CELL CYCLE ARREST AND APOPTOSIS
PROTEASOME INHIBITOR ; BORTEZOMIB
PK / MOA: (MURINE-HUMAN CHIMERIC MONOCLONAL ANTIBODY THAT TARGETS CD20 ANTIGEN) IV (RAPID AND SUSTAINED DEPLETION OF CIRCULATING AND TISSUE-BASED B CELLS ; DETECTABLE IN SERUM 3-6 MONTHS AFTER COMPLETION OF THERAPY - B CELL RECOVERY BEGINS IN 6 MONTHS POST THERAPY ; MEDIAN B CELL LEVELS ARE NORMAL 12 MONTHS LATER ; ELIM UNCERTAIN
ANTI-CD20 MONOCLONAL ANTIBODY ; RITUXIMAB