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88 Cards in this Set
- Front
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Time it takes for amount of drug to fall to half of its value; this is a constant in first order kinetics (majority of drugs)
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Half-life (T1/2)
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Relates the amount of drug in the body to the plasma concentration
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Volume of distribution (VD)
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Plasma concentration of a drug at a given time
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Cp
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The ratio of the rate of elimination of a drug to its plasma concentration
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Clearance (CL)
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The elimination of drug that occurs before it reaches the systemic circulation
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First pass effect
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The fraction of administered dose of a drug that reaches the systemic circulation
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Bioavailability (F)
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When the rate of drug input equals the rate of drug elimination
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Steady state
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Metabolism
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This step of metabolism makes a drug more hydrophilic and hence augments elimination
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Phase I
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Different steps of Phase I
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Oxidation, reduction, hydrolysis
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Inducers of Cytochrome P450 (CYP450)
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Barbiturates, phenytoin, carbamazepine, rifampin, St. John's Wort
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Inhibitors of CYP450
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Amiodarone, Diltiazem, Verapamil, Cimetidine, ketoconazole, erythromycin, isoniazid and grapefruit
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Products of Phase II conjugation
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Glucuronate, acetic acid, and glutathione sulfate
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Type of kinetics when a constant percentage of substrate is metabolized per unit time
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First order kinetics
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Drug elimination with a constant amount metabolized regardless of drug concentration
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Zero order kinetics
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Target plasma concentration times (volume of distribution divided by bioavailability)
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Loading dose (Cp*(Vd/F))
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Concentration in the plasma times (clearance divided by bioavailability)
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Maintenance dose (Cp*(CL/F))
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Pharmacodynamics
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Strength of interaction between drug and its receptor
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Affinity
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Selectivity of a drug for its receptor
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Specificity
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Amount of drug necessary to elicit a biologic effect; refers to the drug's strength
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Potency
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Maximum response achieveable from a drug
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Efficacy
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Ability of a drug to produce 100% of the maximum response regardless of the potency
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Full agonist
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Ability to produce less than 100% of the response
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Partial agonist
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Ability to bind reversibly to the same site as the drug and without activating the effector system
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Competitive antagonist
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Class of drugs with ability to decrease the maximal response to an agonist
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Noncompetitive antagonist
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A hormone whose mechanism of action (MOA) utilizes intracellular receptors
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Thyroid and steroid hormones
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A hormone whose MOA utilizes transmembrane receptors
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Insulin
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Class of drugs whose MOA utilizes ligand gated ion channels
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Benzodiazepines and calcium channel blockers
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Median effective dose required for an effect in 50% of the population
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ED50
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Median toxic dose required for a toxic effect in 50% of the population
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TD50
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Dose which is lethal to 50% of the population
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LD50
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Window between therapeutic effect and toxic effect
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Therapeutic index
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Term for a high margin of safety
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High therapeutic index
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Term for a narrow margin of safety
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Low therapeutic index
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Antidotes and agents used in drug overdose
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Antidote used for lead poisoning
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Dimercaprol, EDTA
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Antidote used for cyanide poisoning
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Nitrites
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Antidote used for anticholinergic poisoning
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Physostigmine
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Antidote used for organophosphate/anticholinesterase poisoning
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Atropine, pralidoxime (2-PAM)
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Antidote used for iron salt toxicity
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Deferoxamine
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Antidote used for acetaminophen (APAP) toxicity
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N-acetylcysteine (Mucomyst)
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Antidote for arsenic, mercury, lead, and gold poisoning
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Dimercaprol
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Antidote used in poisonings: copper (Wilson's disease), lead, mercury, and arsenic
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Penicillamine
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Antidote used for heparin overdose
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Protamine
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Antidote used for warfarin toxicity
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Vitamin K and Fresh frozen plasma (FFP)
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Antidote for tissue plasminogen activator (t-PA), streptokinase
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Aminocaproic acid
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Antidote used for methanol and ethylene glycol
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Ethanol or fomepizole
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Antidote used for opioid toxicity
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Naloxone (IV), naltrexone (PO)
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Antidote used for benzodiazepine toxicity
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Flumazenil
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Antidote used for tricyclic antidepressants (TCA)
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Sodium bicarbonate
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Antidote used for carbon monoxide poisoning
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100% O2 and hyperbaric O2
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Antidote used for digitalis toxicity
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Digibind (also need to d/c digoxin, normalize K+, and lidocaine if pt. Is arrhythmic)
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Antidote used for beta agonist toxicity (eg. Metaproterenol)
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Esmolol
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Antidote for methotrexate toxicity
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Leucovorin
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Antidote for beta-blockers and hypoglycemia
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Glucagon
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Antidote useful for some drug induced Torsade de pointes
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Magnesium sulfate
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Antidote for hyperkalemia
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sodium polystyrene sulfonate(Kayexalate)
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Antidote for salicylate intoxication
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Alkalinize urine, dialysis
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Cancer Chemotherapy
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Relationship of tumor cell number to time of diagnosis, symptoms, treatment and survival
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Log-kill hypothesis
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Pyrimidine analog that causes "thymineless death" given with leucovorin rescue
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5-fluorouracil (5-FU)
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Drug used in cancer therapy causes Cushing-like symptoms
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Prednisone
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Side effect of Mitomycin
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SEVERE myelosuppression
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MOA of cisplatin
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Alkylating agent
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Common toxicities of cisplatin
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Nephro and ototoxicity, peripheral neuropathy
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Analog of hypoxanthine, needs HGPRTase for activation
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6-mercaptopurine (6-MP)
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Interaction with this drug requires dose reduction of 6- MP
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Allopurinol
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Iron-chelating agent, protects against doxorubicin toxicity by scavenging free radicals
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Dexrazoxane
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Blows DNA (breaks DNA strands), limiting SE is pulmonary toxicity
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Bleomycin
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Platinum-based combination therapy for testicular cancer
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Bleomycin+etoposide+cisplatin
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ABVD regimen used for Hodgkin's, but appears less likely to cause sterility and secondary malignancies than MOPP
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Adriamycin (doxorubicin) +bleomycin,,vinblastine +dacarbazine
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Regimen used for non-Hodgkin's lymphoma
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CHOP (cyclophosphamide, doxorubicin, vincristine, and prednisone) plus rituximab
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Regimen used for breast cancer
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CMF (cyclophosphamide, methotrexate, and fluorouracil) and tamoxifen if ER+
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Alkylating agent, vesicant that causes tissue damage with extravasation
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Mechlorethamine
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Anticancer drug also used in RA, produces acrolein in urine that leads to hemorrhagic cystitis
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Cyclophosphamide
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Microtubule inhibitor that causes peripheral sensory neuropathy , foot drop (eg. ataxia), and SIADH
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Vincristine
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Interact with microtubules (but unlike vinca which prevent disassembly of tubules), it stabilizes tubulin and cells remain frozen in metaphase
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Paclitaxel (taxol)
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Agent similar to cisplatin, less nephrotoxic, greater myelosuppression, used to treat refractory hematologic malignancies
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Carboplatin
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Anti-androgen used for prostate cancer
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Flutamide, bicalutamide, nilutamide
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Anti-estrogen used for estrogen receptor + breast cancer
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Tamoxifen
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Aromatase inhibitor used in breast cancer
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anastrozole
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Newer biologic agent approved for metastatic melanoma, enhances T-cell immune responses
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Ipilimumab
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Some cell cycle specific anti-cancer drugs
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Bleomycin, vinca alkaloids, antimetabolites (eg., 5-FU, 6-MP, methotrexate, etoposide)
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Some cell cycle non-specific drugs
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Alkylating agents (eg., mechlorethamine, cyclophosphamide), antibiotics (doxorubicin, daunorubicin), cisplatin
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Regimen used for advanced colorectal cancer, stageII and III colon cancer
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FOLFOX (oxaliplatin, 5-FU and leucovorin)
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Nitrosoureas with high lipophilicity, used for brain tumors
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lomustine
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Anti-cancer agents that affect the VEGF-signaling pathway
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Bevacizumab, Ziv-aflibercept, Sorafenib, Sunitinib, Pazopanib
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