Anticancer Drugs Flashcards by Desiree Namou

Alkylating Agents

6 CLASSES (Form ‘alkyl radicals’ that form covalent linkages with nucleophilic moieties)
Not cell cycle _____ but principle effect is during ____ synthesis
Most are ______ (two alkylating groups) – cross link two _______ sites
Cause intra and inter chain cross-linking
Interfere with transcription and replication

specific
DNA
bifunctional

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OTHER ORAL COMPLICATIONS

_______ INFECTIONS –
-Damaged lining in the mouth and weakened immune system
-Risk is raised by xerostomia during radiation therapy
-Managed with antibiotics (_______ or ______ with _______ antifungal and antiviral drugs
Rarely, the progression of the infection may cause cavernous sinus thrombosis and Ludwig angina –
–Immediate transfer to the nearest hospital and aggressive therapy with antibiotics are crucial and may save patients life
-_______ DISEASE
-_________
-_________ – Due to decreased platelet count, small red spots on lips, soft palate or bottom of the mouth) or severe at the gum line and from ulcers in the mouth

PERIAPICAL 
Clindamycin
Amoxicillin
Clauvulanic acid
PERIODONTAL
SIALADENTITIS
BLEEDING

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DRUG TREATMENT FOR MOUTH AND JAW STIFFNESS

ASA
IBUPROFEN
BENZODIAZAPENES such as diazepam
muscle relaxants: Methocarboamol (Robaxin), Cyclobenzaprine (Flexeril), Carisoprodal (Soma), Metaxalone (Skelaxin), Tizanidine (Zanaflex), Baclofen, Oxazepam

Methocarboamol (Robaxin), Cyclobenzaprine (Flexeril), Carisoprodal (Soma), Metaxalone (Skelaxin), Tizanidine (Zanaflex), Baclofen, Oxazepam

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MONOCLONAL ANTIBODIES - _______

________ produced by cell culture selected to react with antigen specifically expressed on cancer cells
_______– Hybrids of human antibodies
They attach to specific antigen with __ portion of the molecule and __ is left jutting out – this activates host’s immune mechanisms and cancer cell is killed by complement mediated lysis
Monoclonal abs can attach to and inactivate growth factor receptors on cancer cells

RITUXIMAB
immunoglobulins
Humanised
Fab
Fb

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ENZYMES

\_\_\_\_\_\_\_\_ –
-Isolated from bacteria
-Inhibit protein synthesis in tumor cells by depriving them of amino acid \_\_\_\_\_\_\_
-G phase specific
Use – \_\_\_\_
SE – \_\_\_\_\_\_\_ reactions,\_\_\_\_\_\_, \_\_\_\_\_\_\_ increased bleeding risk
\_\_\_\_\_ ASPARAGINASE –
To decrease immunogenicity

ASPARAGINASE
tumor
asparignase
ALL
hypersensitivty 
hepatitis, 
pancreatitis ***
PEG-L

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DRUGS AFFECTING SEX HORMONES

______,_______

Synthetic analogues of _____
agonistsduring short term /pulsatile therapy
Long term administration – _____ feedback loop with _____ gland (Inhibit ______ secretion, ovarian and testicular steroidogenesis)
SE – Initial tumor flare (pain at tumor site and hypercalcemia)
Hot flashes, erectile dysfunction, gynecomastia, hypercholesterolemia, hyperglycemia

LEUPROLIDE, GOSERELIN
GnRH
agonists
negative 
pituitary
gonadotropin
tumor

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DIFFERENTIATION AGENTS

RETINOIDS
-Can inhibit cell growth, induce differentiation and apoptosis
\_\_\_\_\_\_\_
Use – Acute promyelocytic leukemia
\_\_\_\_\_\_\_\_\_\_
Childhood neuroblastoma
\_\_\_\_\_\_\_\_\_ has revolutionized the treatment of APL (acute promyelocytic leukemia)
SE – QTc prolongation

TRETINOIN
ISOTRETINOIC ACID
ARSENIC TRIOXIDE

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TAXANES
___________
-Bark of yew tree
-MOA – cell replication in __ phase by promoting ________ and stabilization of ______ (inhibiting depolymerization)
-Formulated in Cremophor E1 and alcohol – infusion reactions
-Premedicated with steroids and antihistaminics
-Albumin bound drug (novel formulation)
-Use – Metastatic cancers of ____ and _____, NSCLC, Pancreatic adenocarcinoma with Gemcitabine

PACLITAXEL
M
polymerization
microtubules
ovary, breasts

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STEVEN JOHNSON SYNDROME

-Toxic epidermal necrolysis TEN – (different forms but same entity)
-Rare, life-threatening conditions involving both the cutaneous and mucosal membranes.
-Exfoliation implies a positive _______ sign (epidermal detachment caused by slight rubbing of the skin) –
–Destruction of ________ by apoptosis.
Management –
-_______
-_______
-________

nikolsky
keratinocytes
cyclosporine
corticosteroids
infliximab

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LASER THERAPY (wavelength about 650 nm, power setting 40 mW and a dose of 2 J/cm2at each square centimeter of tissue)
_________ favors ______ healing –
Preservation of _____ tissue integrity,
Increases re-epithelialization
Acts against ________and bacterial development

ZINC SULFATE
wound
epithelial
inflammation

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SIDE EFFECTS CONTD

Reactivation of _______
______ complications (seizures, peripheral and cranial neuropathy, myelopathy, aseptic meningitis, cerebellar syndrome, stroke, encephalitis)
-________ (hyper-excitability, ataxia of the extremities)
-______ in the mouth and throat
Hypothyroidism
Anemia is not common

hepatitis B
neurologic
neurotoxicity
parasthesias

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IV immunoglobulins and histamine gels for prevention
_______ (cytoprotective drug suppresses ROS)
VITAMIN E (antioxidant against ROS)
GLUTAMINE
________ causes hypo-salivation, thus reducing mucosal exposure to agents in saliva, _______ drug
XYLOCAINE AND LIDOCAINE solutions

AMIFOSTINE
VITAMIN E
GLUTAMINE
PROPANTHELINE
antimuscarinic drug **
XHYLOCAINE, LIDOCAINE

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DRUGS AFFECTING SEX HORMONES
_________–
Nonsteroidal reversible inhibitor of _______ enzyme
Use – Postmenopausal hormone receptor positive breast cancer
SE – Arthralgia, myalgia, hot flashes, osteoporosis (add calcium and vitamin D supplementation, ________ )

ANASTRAZOLE
aromatase
bisphosphonates

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CLINICAL USES OF CYTOKINES

Aldesleukin (IL2) – Increase lymphocyte differentiation and increase NK Cells, used in renal cell carcinoma and metastatic melanoma
Interleukin 11 – Increase platelet formation, used in thrombocytopenia
_______ (G-CSF) – Increase ______, used for _____ recovery
__________ (GM-CSF) – Increase granulocytes and ______, used for marrow recovery
Erythropoietin – To treat anemias, especially associated with renal failure
Thrombopoietin – Thrombocytopenia

FILGRASTIM
SARGRAMOSTIM
granulocytes
marrow
macrophages

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DRUGS AFFECTING SEX HORMONES
__________
_______ antiandrogen that directly competes with _______ binding site in ______ cells
Use – Combination with GnRH agonist to prevent the flare and in castration resistant _____ cancer
SE – Hot flashes, decreased libido, gynecomastia

FLUTAMIDE
nonsteroidal
testosterone
prostate
prostrate

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Antimetabolites -METHOTREXATE

Drug interactions –
-____________ binding (displaced by ________,_________, _________)
-Salicylates, Probenecid and Penicillins compete for tubular secretion
-NSAIDS reduce renal blood flow and increase nephrotoxicity
-PPIs delay clearance
Side effects –
______, ________

high plasma protein binding
salicylates, Sulfonamides, phenytoin
pneumonitis
nephrotoxicity *

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Fluorouracil

IV bolus or continuous infusion (half life of 10 -20 mins) over 96 hours
Topical – Actinic keratosis and noninvasive skin cancers
Intra-arterial – Metastasis to liver and head and neck _cancers

MOA: inhibits _________ which converts dUMP to dTMP

thymidilate synthetase

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BLOOD LEUKEMIAS - COMBINATION THERAPIES

ALL – _______, _______, _______
AML – __________, _______
CML – _________( tyrosine kinase inhibitor - produced by ________)
CLL – ______, _____ (CD20 expression)

– Daunorubicin, Vincristine, Prednisone
Cytosine arabinoside, Daunorubicin
Imatinib
philedelphia chromosome
Fludarabine, Rituximab

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TISSUE AND BONE LOSS

Destruction of very small _______within the bone resulting in bone death/fractures/infection
Destruction of tissue inside the ______can result in loss of ______

blood vessels
mouth
feeling

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PODOPHYLLOTOXINS
_________
-Mandrake plant
-MOA – Induce DNA strand breaks by inhibiting ________
-Use – First line treatment for small cell lung cancer and refractory testicular cancer
-SE – _______, hypotension and ______ intoxication (dissolved in ethanol)

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ETOPOSIDE
topoisomerase II
lung, testicular
myelosuppression
alcohol

MISC AGENTS
_________, __________
-MOA – Complex and misunderstood, _________ and immune system modulation, inhibits TNF production, stimulates T cell proliferation, IL-2 and interferon release
-Uses – _________ (pre-leukemic syndrome), Multiple myeloma with Dexamethasone, HIV related aphthous ulcers, Rheumatoid arthritis, CGVHD
-SE – Sedation, rash, neuropathy, constipation and venous thrombosis (anticoaglulation therapy)

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thalidomide, lenalidomide
antiangiogenesis
TNF
T
myelodysplastic syndrome

GENERAL SIDE EFFECTS OF CYTOKINES

-_________ after 10-14 days
-_____ loss
-Nausea, vomiting, diarrhea and fatigue (most frequent)
-Defects in ________
-Hand-foot syndrome
-_________(left ventricular impairment or CHF leading to hypertension), thromboembolism, pericardial thickening or arrhythmias
-Bleomycin induced pulmonary fibrosis (_______ is contraindicated)
Hepatic toxicity (Jaundice)

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thrombocytopenia
hair
spermatogenesis
cardiotoxicity
nitrous

MISC AGENTS
_______
-MOA – Inhibits DNA synthesis by blocking action of ribonucleoside _________
-Uses – ___, ______ disorders, to reduce rapidly increasing blast cells in acute leukemias, Polycythemia vera
-In sickle cell anemia to reduce pain crisis and reduce the need for blood transfusions
-SE – myelosuppression and megaloblasgtic anemia

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hydroxyurea
diphosphate reductase
CML
myeloproliferative

Bleomycin

MOA – DNA _____ and fragmentation with inhibition of ____ repair, inhibit ____and _____ synthesis
Cell cycle specific – __ and __ phase
Use – head and neck cancers, testicular cancers and Hodgkin’s lymphoma
Malignant pleural infusion – Direct instillation into pleural space
Minimal nausea and vomiting, no myelosuppression, or local tissue toxicity
Combination protocols
SE – Major dose limiting __________ progressing to pulmonary _____ and pulmonary insufficiency
Caution – Exacerbation/precipitation of pulmonary ____ caused by supplemental oxygen administration (general anesthesia)

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scission
DNA
RNA
protein
G2, M
interstitial pneumonitis
fibrosis
toxicity

Principles of Chemotherapy GOAL – Eradicate every viable ___ cell without significantly damaging the ___ cell CLASSIC CHEMOTHERAPY AGENT – - Not tumor cell _____ - Kills all actively _____ cell - Unintended destruction of gastrointestinal, bone marrow, hair follicles,

tumor host specific dividing

CYTARABINE (Cytosine Arabinoside) – Crosses ____ (40-50% conc than in plasma) Most active single drug for ____ in adults – 25% complete remission, given as combination therapy AraC + Daunorubicin AML – ___ cells, _____ cells Progresses rapidly and is typicall fatal within ____ or _____ if left untreated

``` BBB AML stem white blood weeks, months ```

PLATINUM AGENTS _______ - An atom of platinum surrounded by 2 chlorides - Produces ______ and _______ cross-links in DNA causing ____ - Not cell cycle _____ - _______ when used concurrently with radiotherapy - Uses – Carcinoma testis, ovary, transitional bladder cancer, small and non small cell lung cancer and head and neck cancers - SE – ________ is dose limiting, ototoxic - Concurrent AMIFOSTINE and saline hydration is given to reduce renal toxicity - ________, _________

``` CISPLATIN interstrand intrastrand breaks specific radiosensitizer nephrotoxicity AMIFOSTINE CARBOPLATIN, OXALIPLATIN ```

Alkylating Agents - _______ – Chlorambucil, Cyclophosphamide, Estramustine, Ifosfamide, Mechlorethamine, Melphalan - ________ – Busulfan - ________ – Thiotepa - _____ – Dacarbazine - _______ – Carmustine, Lomustine, Streptozocin SE – All cause _________ and _______ disturbance Long term use – ______ (suppression of gametogenesis), increased risk of acute non-lymphocytic leukemia, other malignancies

``` Nitrogen mustards alkyl sulfonates ethylenimines triazenes nitrosoureas myelosuppression gastrointestinal ```

Dactinomycin ``` _____ tumor (Wilms, Ewing, Embryonal rhabdomyosarcoma) -Intercalates in the minor groove between adjacent guanine-cytosine pairs, interfering with movement of --_______ along the gene – preventing transcription Also act on ________ ```

pediatric RNA polymerase topoisomerase II

VINCA ALKALOIDS ______, ________ -Arrest cell division in metaphase by binding to _______ proteins that form mitotic spindle -Use – ___, Hodgkin’s -SE – _______ (peripheral and autonomic), constipation, ileus, paresthesias, neutropenia -Caution – Never intrathecal (Ascending fatal paralysis) -Liposomal formulation – Relapsed ___ (pts who do not have philedelphia chromsome mutation) --Increases duration and decrease toxicity (neurotoxicity)

``` Vinblastine, Vincristine microtubular proteins ALL neurotoxicity ALL philedelphia chromsome ```

ANTITUMOR ANTIBIOTICS -Produced by streptomycetes species -Intercalate with ___ to form irreversible complexes that inhibit cell division -______ specific ANTHRACYCLINES – -_____ (___,____), doxorubicin (Broad range) -_________ inhibitors (double stranded DNA breaks during DNA replication) -SE – ______ -liposomal encapsulated forms – Provide increased _____ circulation time and decreased cardiomyopathy, different indications (Karposi sarcoma related to AIDS etc)

``` DNA non phase Danurubicin AML, ALL Topoisomerase II cardiac toxicity liposomal plasma ```

MISC AGENTS __________ - MOA – Prevents __ and ____ synthesis - Use – CNS malignancies and Hodgkin’s - For Multiple myeloma in combination with alkylating agents and Vinca alkaloids - SE – ________ toxicity (leukopenia, thrombocytopenia), _____ toxicity - Is a ____ inhibitor, warn against tyramine rich foods and antidepressants - has ______ like reaction (avoid alcohol)

``` procarbizine haematological pulmonary MAO disulfram ```

Methotrexate -Very ______, third space fluid accumulation (ascitic, pleural, peritoneal), drug reservoir – increased toxicity ________ acid rescue – bypasses the blockage of ____________ in normal cells (reduced severity of mucositis and myelosuppression) MOA: For the conversion of ____ to _____, there is a cofactor required. The cofactor is ________ which is formed from dihydrofolate methotrexate inhibits function of that cofactory and ____ is not converted to ____

``` hydrophilic FOLINIC dihydrofolate reductase dUMP, dTMP tetrahydrafolate dump, dtmp ```

BIOLOGIC RESPONSE MODIFIERS -Interferons, Interleukins, Hematopoietic growth factors, Monoclonal antibodies Example – _________ – -A monoclonal antibody specifically used for breast cancer that is ____ receptor positive -Used alone or with other chemotherapy medications

trastuzumab | HER2

HORMONE AGONISTS AND ANTAGONISTS GLUCOCORTICOIDS -Combination therapy(___, ____, Lymphomas, Multiple Myeloma) Supportive care – --Reduce ________ (bone metastasis) --_______ compression --______ --____management Dexamethasone, Prednisone, Methylprednisone SE – _____, gastritis, elevated blood glucose Prolonged use – ______ appearance, hypertension, osteoporosis, immune suppression

``` ALL, CLL hypercalcemia spinal cord antiemetic pain insomnia Cushingoid ```

Antimetabolites - Marked structural resemblance to ______, _____ and ________bases - _______ substrates for biochemical reactions - Effect on __ Phase (DNA synthesis phase) - Interferes with growth of rapidly proliferating cells (oral mucosa toxicity) - Folic acid analogues – ________ (Folate antagonist) - Purine analogues – Mercaptopurine, Thioguanine, Fludarabine - Pyrimidine analogues – __________, ________ Floxuridine, Gemcitabine

``` folic acid purine pyrimidine fraudulent S phase Methotrexate Cytarabine Fluorouracil ```

mouth and jaw stiffness MANAGE: - Medical devices (bite openers made from acrylic resin, metal) - Pain treatment - Muscle relaxants - Jaw exercises - __________(Tri-cyclics like Amitriptyline, SSRIs) - ________ drugs (BENZODIAZEPINES)

anti-depressants | anti-anxiety

Hallmark of Cancer Cells ``` CANCER CELLS VERSUS NORMAL CELLS – -Uncontrolled ______ -________ and loss of function -Invasiveness -Metastasis GENESIS OF CANCER CELLS – -Genetic change --Activation of ________ to oncogenes --Inactivation of _________genes -Hormonal action -Co-carcinogens -Tumor promoter effects ```

proliferation dedifferentation proto oncogenes tumor suppressor

___________ -Zoledronic acid, Pamidronate MOA – inhibit ______ activity, and promote _____ -Bone pain associated with metastasis arising from breast, prostate, lung carcinoma and multiple myeloma -SE – Fever, flu like syndrome, decreased renal function, hypocalcemia and ______ (anti-resorptive agent induced osteonecrosis of jaw)

bisphosphonates osteoclast apoptosis ARONJ

SEVERE PAIN –______ and changes in _____ -Pain medications, muscle relaxants, anti anxiety drugs and antidepressants ________ – Protocols recommend dental intervention before chemotherapy -Dental floss and oral rinses (Sterile water or physiologic saline solution are more effective than chlorhexidine) -Povidone iodine rinses

opioids diet ORAL HYGIENE

ANTHRACENEDIONE-anti tumor _________ - anthraquinone antibiotic (antibiotic, antiviral, antiprotozoal and immunomodulating) - MOA – ___ strand breaks - free radicalgeneration is low (low risk of cardiotoxicity) - SE – Bluish green discoloration of urine and sclera - Effective against resistant cancers

mitoxantrione

-___________ (Diphenhydramine, viscous lidocaine, bismuth subsalicylate, and corticosteroids) -_________ 5-30 mins before chemotherapy (local vasoconstriction, reducing mucosal blood flow and thus the exposure) -Cryotherapy is contraindicated in patients treated with _______, to eliminate neurological side effects such as mandibular stiffness. Granulocyte-colony stimulating factor (G-CSF) – ________ ________ IV – Mucocutaneous epithelial human growth factor

``` MAGIC MOUTHWASH CRYOTHERAPY Oxaliplatin FLIGRASTIM PALIFERMIN ```

Alklyating Agents ___________ – Broad spectrum (induction, maintenance, remission) Pronounced effect on _______ – --Conditioning for bone marrow transplant --Immunosuppressive (autoimmune disorders) -Two active metabolites – Phosphoramide mustard and Acrolein (Toxic to bladder – _________ and dysuria) -_____ (sodium 2 mercaptoethane sulfonate) or N-acetylcysteine, chemoprotectants ______ – -Directly instilled into bladder for superficial cancer

``` Cyclophosphamide lymphocytes hemorrhagic cystitis MESNA Thiotepa ```

DRUGS AFFECTING SEX HORMONE STATUS SEX HORMONES – ________ – Advanced prostatic cancer and postmenopausal breast cancer -TAMOXIFEN – ____ USES – ________ of breast with positive Estrogen or Progesterone receptor status --Endometrial and ovarian cancers -SE – intial flare, bone pain, hypercalcemia --hot flashes, thromboembolism Metabolized by cytochrome P450, _____inhibit hepatic metabolism TOREMIFENE _______ (________ for endometrial, breast and renal cell carcinoma)

``` ESTROGENS SERM adenocarcinoma initial flare hot flashes SSRIs TOREMIFENE MEGESTROL progesterone ```

XEROSTOMIA – -Dryness begins after 1 week and it takes around ___ months to recover (complete recovery may not be seen sometimes) -Saliva substitutes and medications that help make more saliva (_______ and _______) DYSGUESIA – Damage to ______ Most patients – Returns to normal in 6 to 8 wks, sometimes permanent with radiation therapy _______ supplements ________ AND FATIGUE – Liquid diet and feeding tube within 3 to 4 weeks Team – Speech and swallowing therapists, dietician, psychologist (risk of aspiration and pneumonia, constipation with opioids) + DENTAL SPECIALIST (Replace missing teeth and damaged area with artificial devices to help swallowing)

``` 2-3 PILOCARPINE, CVIMELINE taste buds Zinc sulfate MALNUTRITION ```

telomerase and angiogenesis Nutrition – 1-2 mm size by diffusion, blood supply through ________ (a response to growth factors - VEGF, PDGF, FGF, and TGF) ________ Expression – Confers _______ on a cancer cell

telomerase angiogenesis immortality

MONOCLONAL ANTIBODIES ______ -A ___________ inhibitor -Use – Adults and children who have been newly diagnosed with ________ positive chronic myeloid leukemia (Ph+ CML) in chronic phase -Dermatofibrosarcoma protuberans (DFSP), tissue under the ___ grows out of control -SE – ______ – Bluish-brown pigmentation on the hard palate, gingiva, teeth, and perioral region -Occurs with Imatinib therapy – effects c-kit, a tyrosine kinase receptor with regulatory action on ________ – --Overstimulation Dose related and reversible

``` IMATINIB protein tyrosine kinase philedelphia chromosome skin melanosis melanogenesis ```

Useful Application of Cancer Chemotherapy - Susceptible tumor cells - Resistant host cells - Intolerable local or systemic toxicity - Adequate concentration - Sufficient period - Cell burden (blood supply and debulking) - ___________ - _______between cycles - Combination - Resistance

first order kinetics | interval

ORAL SIDE EFFECTS - ________ - Most common painful inflammatory reaction of the oral mucosa - Infiltration of the inflammatory cells followed by epithelial disruption and ulceration (erythema, burning, odema and ulcers – impacting ____, ____ and ______) - Injured tissue releases reactive oxygen species (ROS) which damage ____ - Arises ___ days after the initiation of a high dose course and disappears ___ weeks after the treatment is completed - _______ and ______ are secreted in saliva (favors oral toxicity)

``` oral mucositis speech, eating, swallowing DNA 4-7 2-4 methotrexate, etoposide ```

Anticancer Drugs Flashcards

(49 cards)