Save
Busy. Please wait.
Log in with Clever
or
show password
Forgot Password?
Don't have an account?  Sign up 
Sign up using Clever
or
Username is available taken
show password


Make sure to remember your password. If you forget it there is no way for StudyStack to send you a reset link. You would need to create a new account. Your email address is only used to allow you to reset your password. See our Privacy Policy and Terms of Service.

Already a StudyStack user? Log In

Reset Password
Enter the associated with your account, and we'll email you a link to reset your password.
focusNode
Didn't know it?
click below
 
Knew it?
click below
Don't Know
Remaining cards (0)
Know
0:00
edit
Embed Code - If you would like this activity on your web page, copy the script below and paste it into your web page.

  Normal Size     Small Size show me how

Anticancer Drugs

Blood and Lymph Medical Pharmacology Anticancer Drugs

QuestionAnswer
Major categories of alkylating agents Nitrogen Mustards Nitrosoureas
Nitrogen Mustards (Drug Names) Cyclophosphamide Mechlorethamine Melphalan
Nitrosoureas (Drug Names) Carmustine Lomustine
Platinum complexes (Drug Names) Cisplatin
Major Categories of Antimetabolites Antifolates Pyrimidine antimetabolites Purine antimetabolites
Major Categories of Natural Product Anticancer Drugs Antimitotic drugs Epipodophyllotoxins Camptothecins Antibiotics Enzymes
Major Categories of Hormones and Antagonists Glucocorticoids Anti-estrogens Aromatase inhibitors
Targeted Agents (Drug Names) Bortezomib Hydroxyurea Imatnib Trastuzumab Bevacizumab
Alkylating Agents: Primary Mechanism of Antitumor Action Alkylation of DNA
The major site of action for Alkylating Agents N7 position of Guanine
Alkylating agents form highly reactive alkyl groups by binding _______________ to nucleophilic targets. Covalently
Effects of Alkylation on DNA Excessive Cross Linking (bifunctional) DNA Strand Breaks (monofunctional) Miscoding of DNA
General Toxicities of Alkylating Agents Potentially Carcinogenic, Mutagenic, Teratogenic Reproductive system toxicity Veno-Occlusive Disease of the liver from vascular endothelial damage. Strong Vesicant Properties-->damaged veins
Unique feature of Nitrogen Mustards Clothes pin structure crosslinks DNA
Cyclophosphamide is a __________________ that is activated in the ____________________. prodrug; liver
The dose-limiting effect of cyclophosphamide is _________________, which allows for cyclophosphamide to also be used as a(n)____________________ Bone marrow depression; immunosuppressant
Acute dose-limiting effect of Cyclophosphamide. Hemorrhagic cystitis
______________________is the metabolite that causes Hemorrhagic cystitis. Acrolein
Treatment/prevention of hemorrhagic cystitis caused by cyclophosphamide. -Aggressive hydration -Mesna (2-mercaptoethane sodium sulfonate) -N-acetylcysteine (NAC)
Action of Mesna and N-acetylcysteine Scavenge for acrolein molecules.
Hemhorrhagic cystitis is _________ ___________ of the bladder that leads to hemorrhage. diffuse inflammation
Nitrosorueas major site of action O6 Guanine (Attack the DNA!)
Nitrosoureas, because they are highly lipophilic, are able to _____________ which makes them UNIQUELY useful in treating _________________. cross the BBB; brain tumors
Major toxicities of Nitrosoureas -Profound and delayed bone marrow depression -Multiple dose limiting toxicities (CNS, renal, hepatic, pulmonary)
Nitrosoureas are so toxic, you must track a patient's ____________________. lifetime cumulative dose
Platinum Complexes (Drug Names) Cisplatin
Cisplatin range of antitumor activity (major organs/tissue) Testicular Ovarian Bladder
Cisplatin mechanism of action Causes inter- and intra- strand DNA crosslinks.
How Cisplatin is modified in order to act. Water replaces chloride in structure, creating a reactive molecule.
Environment for Cisplatin modification Low chloride concentrations (occurs inside cells as well as in the urine which can lead to bladder problems)
Cisplatin Toxicity -Severe Nausea and Vomiting -Anaphylactic like Reactions -Nephrotoxicity -Neurotoxicity
Cisplatin Dose-Limiting Toxicity Nephrotoxicity
Nephrotoxicity by cisplatin is abrogated by _______________, __________________, and _________________. Hydration; Chloride Diuresis; Amifostine
Major Categories of Antimetabolites Antifolates Pyrimidine Antimetabolites Purine Antimetabolites
Antifolates (Drug Names) Methotrexate
Methotrexate inhibits ___________________, which means that ____________________ is not converted into ____________________. The overall meaning of this is that methotrexate interrupts ____ ___________ synthesis of _______ and purine nucleotides. Dihydrofolate Reductase (as well as other enzymes) Dihydrofolate Tetrahydrofolate de novo TMP
Methotrexate is often given with _______________ in a process called "_________________ _______________"to reduce toxicity in normal cells. Leucovorin Leucovorin Rescue
Pyrimidine Analogs (Drug Names) 5-Fluorouracil Capecitabine Cytarabine Gemcitabine
Cytarabine is also known as ____________. ara-C
5-Fluorouracil is one of the most widely used agents for ____________, _____________, and ___________________. Basal Cell Carcinoma Breast Cancer Colorectal Cancer
Two main things that 5-FU does Incorporates into nucleic acid Prevents generation of TTP
Target cells convert 5-FU to ______________, which covalently binds to the enzyme _________________. 5F-dUMP Thymidylate synthetase
Dose limiting toxicities of 5-FU GI mucositis Bone marrow depression
Effect of leucovorin when used with 5-FU Enhances cytotoxic effects and toxicities
Prodrug that is converted to ara-CTP Cytarabine
Cytarabine competes with this to inhibit DNA synthesis. dCTP
Cytarabine is unstable in the blood so it requires this type of delivery. Constant infusion over 5-7 days.
Cytarabine uses Hematological (AML, ALL, non-Hodgkin's lymphoma)
Cytarabine toxicities Bone Marrow Depression Hyperuricemia
Deoxycytidine analog used in breast, nonsmall cell lung, pancreatic, and ovarian cancer Gemcitabine
Deoxycytidine analog used in breast, nonsmall cell lung, pancreatic, and ovarian cancer Gemcitabine
Three major mechanisms of action of Gemcitabine Inhibits ribonucleotide reductase, inhibits DNA polymerase, incorporates into DNA
Gemcitabine dose limiting toxicity Myelosuppression
Ribonucleotide reductase function Takes ribonucleotides and makes them deoxyribonucleotide.
Purine Analogs (Drug Names) 6-Mercaptopurine (6-MP), 6 Thioguanine (6-TG)
Uses of 6-MP and 6-TG ALL; AML; CML Acute lymphocytic leukemia; Acute myelogenous leukemia; Chronic myelogenous leukemia
Enzyme that activates Purine analogs from inactive parent form HGPRT (hypoxanthine-guanine phosphoribosyltransferase)
Purine analogs Mechanisms of Action Inhibit synthesis of purine nucleotides Incorporate into RNA and DNA
Enzyme that metabolizes 6-Mercaptopurine Xanthine Oxidase
Drug that is given to protect kidneys against uric acid damage. Allopurinol
Mechanism by which allopurinol inhibits uric acid production Inhibition of Xanthine Oxidase
The dose of ________ must be lowered when allopurinol is used concurrently (and why) 6-MP because allopurinol inhibits xanthine oxidase which also helps breakdown 6-MP. 6-MP could build up.
Purine analog side effects Bone marrow depression; Hyperuricemia; Hepatotoxicity
Substance that can make a tumor resistant to all Natural Products drugs. P-glycoprotein
Vincristine and Vinblastine mechanism of action Inhibit microtubule polymerization
Vincristine Treatment of Choice Induce remissions in Lymphocytic Leukemia
Vincristine Dose Limiting Tox Neurological Toxicity: Peripheral Sensory neuropathy
Vinblastine Dose Limiting Tox Myelosuppression (vinBlastine= Bone marrow)
Paclitaxel and Docetaxel mechanism of action hyperstabilizes polymerized microtubules by binding to tubulin. Mitotic spindle can't breakdown inducing apoptosis.
Paclitaxel Dose Limiting Tox Peripheral Neuropathy; Bone marrow depression.
Docetaxel Toxicities Neurotoxicity (neurosensory and neuropathy);Bone marrow depression; Fluid Retention
Etoposide mechanism of action Inhibits topoisomerase II
Etoposide use Testicular Tumors; Small Cell Lung Cancer "Lance Armstrong Used This so that 'E TOP the world of cycling"
Topotecan use Ovarian and Small Cell Lung Cancer
Irinotecan use Metastatic Colon Carcinoma
Topotecan and Irinotecan inhibit this Topoisomerase I
Irinotecan dose limiting toxicity Diarrhea; Bone Marrow Depression
Anticancer drugs that cause something to go wrong with neuro system
Dactinomycin mechanism of action. Intercalates in DNA to block DNA/RNA synthesis.
Doxorunbin and Daunorubicin mechanisms of action (3) 1. Intercalate into DNA 2. Inhibit topoisomerase II 3. Free radical formation because Fe complex is very reactive.
Daunorubicin Use Acute Lymphocytic Leukemia (ALL); Acute Non-Lymphocytic Leukemia (ANLL)
Doxorubicin and Danorubicin Toxicity Cardiotoxicity- chronic, cumulative, dose related, often irreversible
Bleomycin mechanism of action DNA Strand Breakage by oxidative damage by DNA-bleomycin-Fe(II) complex.
Bleomycin toxicity Pulmonary toxicity; Cutaneous toxicity "Lance Armstrong Didn't Use This because he didn't want to Bleo his chances"
Bleomycin pulmonary toxicity stages Nonspecific pneumonitis-->Life threatening pulmonary fibrosis
Bleomycin pulmonary toxicity is _____________over a lifetime Cumulative
Bleomycin pulmonary toxicity risk factors Total Dose; Age>70; Underlying lung disease; High doses; High [Oxygen]
L-Asparaginase use Standard for all Lymphocytic leukemia including ALL
L-Asparaginase Mechanism Hydrolyzes circulating L-asparagine. For tumor cells that can't make L-asparagine, this depletes cells of it.
Hormones and Antagonists: Major Classes Glucocorticoids; Anti-Estrogens; Aromatase Inhibitors
Prednisone (glucocorticoid) used for suppressing this. Lymphocytes
Tamoxifen (Anti-Estrogen) Mechanism Competitively binds to estrogen receptor
Tamoxifen Use Brest tumors that are Estrogen Receptor Positive (ER+)
Risk reduction setting for tamoxifen use. Women with Ductal Carcinoma in Situ; Women at High Risk for Breast Cancer
Anastrozole mechanisms of action Inhibits: 1. Adrenal synthasis of steroids 2. Aromatase conversion of androgens to estrogens in peripheral tissues.
Anastrozole key use Cases in which tamoxifen is no longer effective.
Bortezomib Use Multiple Myeloma
Bortezomib mechanism 1.Inhibits 26S proteasome which prevents degradation of proteins (initiating apoptosis). 2. Disrupts cell signaling pathways
Imatinib mechanism Inhibits Bcr-Abl tyrosine kinase
Imatinib use Chronic Myelogenous Leukemia
Trastuzumab mechanism Block HER-2 receptor
Description of HER-2 receptor Extremely aggressive pathway, cranks up metastasis, turns down apoptosis
Associated with HER-2 Estrogen Receptor Negative Breast Cancer
Bevacizumab mechanism Blocks vascular endothelial growth factor (VEGF) for anti-angiogenic action.
Hydroxyurea mechanism Inhibits ribuncleotide reductase which is important for salvaging ribodiphos-->deoxyribodiphos
Created by: sdave
Popular Pharmacology sets

 

 



Voices

Use these flashcards to help memorize information. Look at the large card and try to recall what is on the other side. Then click the card to flip it. If you knew the answer, click the green Know box. Otherwise, click the red Don't know box.

When you've placed seven or more cards in the Don't know box, click "retry" to try those cards again.

If you've accidentally put the card in the wrong box, just click on the card to take it out of the box.

You can also use your keyboard to move the cards as follows:

If you are logged in to your account, this website will remember which cards you know and don't know so that they are in the same box the next time you log in.

When you need a break, try one of the other activities listed below the flashcards like Matching, Snowman, or Hungry Bug. Although it may feel like you're playing a game, your brain is still making more connections with the information to help you out.

To see how well you know the information, try the Quiz or Test activity.

Pass complete!
"Know" box contains:
Time elapsed:
Retries:
restart all cards