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76 Cards in this Set
- Front
- Back
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When are antimetabolites active?
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S-phase
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Which antimetabolite is used at high doses with a leucovorin rescue? Why does this work?
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methotrexate. Rapidly proliferating tumor cells are more dependent on folate metabolism than normal cells.f
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Name 2 pyrimidine analogues.
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5-FU
ara-C |
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This chemotherapeutic agent was first isolated from a sponge.
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Cytosine arabinoside (ara-C)
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Which antimetabolite(s) interfere with both RNA and DNA synthesis?
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5-FU
6- mercaptourine |
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Which chemotherapeutic agents cross the BBB?
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Cytosine arabinoside (ara-C)
Cyclohexylchloroethylnitrosourea (a nitrosourea) ________ |
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What phase of the cell cycle do vinca alkaloids affect?
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Mostly M
Also G1, S |
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Which chemotherapeutics are phase-dependent?
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Antimetabolites
Vinca alkaloids Taxanes Bleomycin |
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What are the 2 vinca alkaloids most used in veterinary medicine?
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Vincristine
Vinblastine |
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Which chemotherapeutic agent concentrates in pulmonary tissues and is particularly useful against lung tumors?
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Vinorelbine
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Which group of chemotherapeutics induce sustained mitotic block at metaphase?
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Taxanes
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These were the first non-hormonal drugs to show signigficant antineoplastic activity in people?
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Alkylating agents
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Which chemotherapeutics' activity on DNA resembles that of radiation?
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Alkylating agents
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What is the mechanism of alkylating agents?
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Miscoding of DNA strands
incomplete repair of DNA segments inhibition of strand separation at mitosis due to excessive cross-linking |
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True/False. Alkylating agents are typically affected by p-glycoprotein-mediated multidrug resistance.
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False.
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Which nitrogen mustards require hepatic activation?
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cyclophosphamide, ifosamide
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Which agents need to be administered with proper hydration because of lower urinary tract irritation?
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Metabolites of cyclophosphamide, ifosfamide
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This agent binds covalents to all bases.
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Cisplatin
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This agent causes significant nausea due to serotonin release and nephrotoxicity due to drug-protein interactions in renal tubules.
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Cisplatin
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Which antineoplastics cannot be given to cats?
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5-FU
Cisplatin |
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What drug is an alternative to cisplatin without nephrotoxic activity?
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Carboplatin
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Which enzyme do the anthracyclines inhibit topoisomerase? What does this result in?
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Topoisomerase II
Inhibit re-ligation of DNA cleaved by topoisomerase II and induce protein-linked breaks. |
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Which agents is one of the most widely used chemotherapeutic agents in both veterinary and human oncology?
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Doxyrubicin
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Which group of chemotherapeutic agents also have membrane effects that affect signal transduction?
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Anthracyclines
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What are agents that can be used if doxyrubicin is contraindicated?
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Mitotoxane
Dactinomycin |
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Which chemotherapeutics are phase nonspecific?
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Alkylators
Platinum Compounds Anthracyclines |
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Resistance to alkylating agents is often associated with increased levels of what?
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glutathione-S-transferase and glutathione
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Common features of drugs with multidrug resistance?
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small
lipophilic |
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To what can multidrug resistance of tumor cell be ascribed?
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increased levels of p-glycoprotein, which plays a role in excretion of xenobiotics from the body.
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Some effects of biological response modifiers?
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Decreased angiogenesis
Enhance immune recognition of cancer cells Inhibit metabolic pathways inhibit invasion and metastasis mechanisms |
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True/False. The flattening of the cancer growth curve is due to cell death due to overcrowding.
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False. Decreased proliferation.
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True/False. Larger tumors are more sensitive to chemotherapy.
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False. A larger proportion of cells are quiescent, and therefore less sensitive.
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What type of administration pattern is best for cell-cycle nonspecific drugs?
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Larger intermittent doses (their effects are concentration dependent)
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What type of administration pattern is best for phase-specific drugs?
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Maintain cytotoxic levels for a period of time (schedule dependent).
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About how many cycles of chemotherapy would theoretically eliminate tumor cells?
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6
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Why is cure of a gross tumor rare?
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Delay in therapy to allow normal tissues to recover
tumor heterogeneity |
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Which healthy tissues are most affected by chemotherapy?
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bone marrow
GI mucosa hair follicles gonads |
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Which synthetic glucocorticoid has the greatest anti-inflammatory activity?
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Dexamethasone
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Which glucocorticoid has the most mineralocorticoid activity?>
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Prednisolone
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What is the basic chemical structure of glucocorticoids?
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cyclopentanoperhydro phenanthrene ring
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What are some short-acting glucocorticoids?
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hydrocortisone, cortisone
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What are some intermediate-acting glucocorticoids?
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prednisone, prednisolone
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What are some long-acting glucocorticoids?
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dexamethasone, betamethasone, paramethasone
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Which elements does the glucocorticoid-receptor complex bind to activate transcription?
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GRE
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Which elements does the glucocorticoid-receptor complex bind to inhibit transcription?
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NF-kB or AP1
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Which cytokines are released with infection that stimulates cortisol release?
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IL-1
IL-6 TNF-a |
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Name the 3 mechanisms of inhibition of prostaglanding synthesis by glucocorticoids?
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Inhibit PLA2
Induce MAPK-phosphatase Inhibit NF-kB mediated transcription of COX2 |
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Effect of glucocorticoids on formed blood elements?
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impede neutrophil migration
inhibit phagocytosis decrease lymphocyte response decrease circulating lymphocytes, eosinophils, monocyes, basophils |
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Contraindications for glucocorticoid use?
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Pancreatitis
Fungal and viral infection osteoporosis late pregnancy corneal ulcers DM Undernourished animals |
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Which esters of glucocorticoids are very soluble and used when a rapid effect is desirable?
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Hemisuccinate
Phosphate |
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Which esters can be used intra-articularly?
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Acetate
Diacetate Tebutate Hexacetonide |
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Which glucocorticoid is given during treatment of shock and why?
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Hydrocortisone because of the mineralocorticoid activity
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Why might you administer glucocorticoids in a shock patient?
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restores vascular sensitivity to NE
increases blood glucose reverses weakness and depression |
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When might intensive short-term glucocorticoid therapy be indicated?
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acute pulmonary edema
acute adrenal insufficiency shock accompanying adrenal insufficiency |
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Which anabolic steroids are approved for horses?
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Stanozolol
Boldenone undecylenate |
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Pharmacological effects of anabolic steroids.
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Nitrogen retention
Ca++, PO4--- retention normalize electrolyte balance stimulate muscle protein production |
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What structural element of testosterone imparts adnrogenic activity?
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The oxygen at C3
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What class of drugs might be given for anemia and why?
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Anabolic steroids stimulate erythropoiesis by unknown mechanism
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What class of drugs may be used in immune-mediated thrombocytopenia?
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Anabolic steroids.
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Why are anabolic steroids contraindicated in congestive heart failure?
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Na+ and H2O retention
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Major mechanism of action of NSAIDs.
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Inhibit COX and therefore prostaglandin synthesis?
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True/False. NSAIDs block COX1 and COX2 and therefore inhibit prostaglandin, thromboxane, prostacylin and leukotriene synthesis.
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False. Does not affect leukotrienes.
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What mediates the analgesic effects of NSAIDs?
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Decrease of prostaglandins, which sensitize pain receptors to bradykinin.
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Which product of COX is involved in fever?
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PGE
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What advantages do NSAIDs have over opiods as analgesics?
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Do not produce respiratory depression, sedation, constipation, tolerance or dependence.
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True/False. NSAIDs may be used in the treatment of cancer.
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True- COX2 is unusually active in many cancers, though COX2 inhibitors are only shown to be helpful with colon cancers.
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What useful effects of COX2 are blocked by NSAIDs?
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maintain gastric mucosa
regulage gastric acid secretion maintain renal blood flow maintain coagulability status |
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What could be one side effect of targeting COX2 as an inhibitor?
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increased clotting/stroke.
also constitutively expressed in the heart. |
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Deficiency of glucuronyl transferase in cats is problematic with which NSAID?
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Acetominophen
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What are consequences of aspirin overdoes?
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Respiratory alkalosis (hyperventilation)
Respiratory acidosis (CNS depression) Metabolic acidosis (acidic drug) Hyperthermia (uncoupling of oxidative phosphorylation) Dehydration |
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What are effects mediated by the H1 receptor?
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Vasodilation
increase capillary permeability contract bronchial smooth muscle contract GI smooth muscle urticarial response |
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What effects are mediated by the H2 receptor?
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Increase gastric acid secretion
vasodilation |
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MOA of H1
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IP3 and DG release
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MOA of H2
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Increase adenylate cyclase activity
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What effects of H1-antagonists are not mediated by the H1 receptor?
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sedation
anti-motion sickness anticholinergic effect anti-serotonin effect local anesthetic teratogenic effects |
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Which antihistamine particularly has drug-drug interactions that prolong the half life of many other drugs?
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Cimetidine
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