Anticancer and Immunosuppressants Flashcards
Process of altered cell differentiation and growth
Uncoordinated
Autonomous
Lacks normal regulatory control
Neoplasia
Disease resulting from altered cell differentiation and growth
Cancer
Loss of differentiation
Anaplasia
Arise from the cells that cover external and internal body surfaces such as lung,
pancreatic, breast, and colon
Carcinoma
Arise from cells found in the supporting tissues of the body such as bone, cartilage,
fat, connective tissue, and muscle
Sarcoma
Arise in lymph nodes and tissues of the body’s immune system
Lymphoma
Cancers of the immature blood cells that grow in the bone marrow
Leukemia
__% of breast cancer pts develop bone metastases
70%
If the drug ends in -dronate, what kind of drug is it?
Bisphosphonate
Inhibit osteoclast
Attach to bony surfaces undergoing
active resorption
released during
resorption by osteoclasts impairs
ability of osteoclasts to form the
ruffled border, to adhere to the
bony surface
Reduce osteoclast genesis and
recruitment
Promoting osteoclast apoptosis
Bisphosphonates
Inhibit osteoclast activation
RANKL is secreted by bone
marrow cells and osteoblasts
RANKL binds to the RANK receptor on
osteoclasts and promotes osteoclast
differentiation and activity.
a fully human
monoclonal antibody that binds to
RANKL
Bound RANKL cannot attach to RANK
receptors (i.e. inhibiting activation of
osteoclast)
Denosumab
Denosumab
Osteoporosis treatment
60mg every 6months
Prolia
Denosumab:
Bone cancer treatment - same prevalence as bisphosphonate
120mg every 4weeks
Xgeva
Profound and prolonged inhibition of bone resorption with
oversuppression of bone remodeling (ie, low bone turnover), and
infection are the main mechanisms
MRONJ
Used in solid tumor cancers
Specifically recognize and bind to VEGF.
Once bound, the complex is unable to activate the
VEGF receptor.
Most effective when combined with additional
therapies, especially chemotherapy.
Do not necessarily kill tumors; they instead may
prevent tumors from growing.
Reduce formation of new blood vessels; reduce
nutrient delivery
Increases in bleeding and reduced wound healing
Bevacizumab
Directly damage cell DNA
Impairs replication & transcription= cell death
Work in all phases of the cell cycle
Can be used in many different cancers
Due to affect on DNA, big impact on bone marrow
Bone Marrow Suppression – reduce blood cell
production
Highly immunosuppressant
Toxicity related to cumulative dose
Mucosal damage – oral mucosal ulceration
GI disturbance
Sterility
Acute non-lymphocytic leukemia
Alkylating agents
Drugs enter into the dorsal root ganglion
and binds to DNA, causing apoptosis.
Regardless of the mechanism, apoptosis
results in secondary damage to peripheral
nerves.
pain triggered by
exposure to cold liquids
Cold-induced perioral paresthesias – 95%
Cold-induced pharyngolaryngeal dysesthesia – 92%
Dyspnea – 40%
Muscle cramps – 34%
Jaw stiffness – 34%
Dysphagia – 30%
Visible fasciculations – 30%
Voice changes – 6%
Ocular changes – 0.7%
Platinum compounds
Oxaliplatin
are structurally related to normal compounds that exist
within the cell
interfere with DNA and RNA growth by substituting for
or competing with the normal building blocks of DNA and RNA
i.e. the availability of normal purine or pyrimidine nucleotide precursors
May either by inhibiting the synthesis of normal nucleotides or compete with them in
the formation of DNA or RNA
Their maximal cytotoxic effects are in S-phase
Synthesis – DNA replicates, yielding two separate sets
Antimetabolites
Antimetabolites are specific to what phase of cell cycle
S phase
Folate antagonist
Antineoplastic; immunosuppressant (psoriasis; RA)
Target S-phase (DNA replication), inhibit rapid proliferating cells
Bone marrow and intestinal epithelium
Myelosuppression risk for hemorrhage and infection
Dental Note: oral mucositis
Oral pain; Erythema; Difficulty opening the mouth
DNA cycle specific agents are most stomatotoxic
Methotrexate, etoposide known to be secreted into the saliva
further increasing stomato toxicity potential
Can also be used for psoriasis and Rheumatoid arthritis
Methotrexate
Bind to and break DNA inside cancer cell to keep them from growing
and multiplying
Groups:
Anthracyclines: Doxorubicin, daunorubicin, epirubicin, idarubicin.
Other: bleomycin, plicamycin, mitomycin.
Oral Mucositis
Cytotoxic antibiotics
Work in M-Phase to prevent cell division
Groups include:
Vinca Alkaloids: Vincristine, Vinblastine
Taxanes: Paclitaxel, Docetaxel
Mitotic inhibitors
Mitotic inhibitor
Derived from Madagascar periwinkle
MOA: bind β tubulin & block its polymerization with α tubulin into
microtubules
Cell division arrests in metaphase
Absence of intact mitotic spindle, chromosomes
cannot align, disperse throughout the cytoplasm
Apoptosis
Toxicity-
Peripheral neuropathy-numbness, tingling
Neurotoxicity may also be persistent, deep aching and burning pain that mimics
a toothache
Vincristine
Interfere with topoisomerase which is responsible for unwinding double
-stranded DNA
Epipodophyllotoxins: Etoposide
Camptothecins: Irinotecan, topotecan
Topoisomerase Inhibitors