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88 Cards in this Set

  • Front
  • Back
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)
Half-life (T1/2)
Relates the amount of drug in the body to the plasma concentration
Volume of distribution (VD)
Plasma concentration of a drug at a given time
Cp
The ratio of the rate of elimination of a drug to its plasma concentration
Clearance (CL)
The elimination of drug that occurs before it reaches the systemic circulation
First pass effect
The fraction of administered dose of a drug that reaches the systemic circulation
Bioavailability (F)
When the rate of drug input equals the rate of drug elimination
Steady state
Metabolism

This step of metabolism makes a drug more hydrophilic and hence augments elimination
Phase I
Different steps of Phase I
Oxidation, reduction, hydrolysis
Inducers of Cytochrome P450 (CYP450)
Barbiturates, phenytoin, carbamazepine, rifampin, St. John's Wort
Inhibitors of CYP450
Amiodarone, Diltiazem, Verapamil, Cimetidine, ketoconazole, erythromycin, isoniazid and grapefruit
Products of Phase II conjugation
Glucuronate, acetic acid, and glutathione sulfate
Type of kinetics when a constant percentage of substrate is metabolized per unit time
First order kinetics
Drug elimination with a constant amount metabolized regardless of drug concentration
Zero order kinetics
Target plasma concentration times (volume of distribution divided by bioavailability)
Loading dose (Cp*(Vd/F))
Concentration in the plasma times (clearance divided by bioavailability)
Maintenance dose (Cp*(CL/F))
Pharmacodynamics

Strength of interaction between drug and its receptor
Affinity
Selectivity of a drug for its receptor
Specificity
Amount of drug necessary to elicit a biologic effect; refers to the drug's strength
Potency
Maximum response achieveable from a drug
Efficacy
Ability of a drug to produce 100% of the maximum response regardless of the potency
Full agonist
Ability to produce less than 100% of the response
Partial agonist
Ability to bind reversibly to the same site as the drug and without activating the effector system
Competitive antagonist
Class of drugs with ability to decrease the maximal response to an agonist
Noncompetitive antagonist
A hormone whose mechanism of action (MOA) utilizes intracellular receptors
Thyroid and steroid hormones
A hormone whose MOA utilizes transmembrane receptors
Insulin
Class of drugs whose MOA utilizes ligand gated ion channels
Benzodiazepines and calcium channel blockers
Median effective dose required for an effect in 50% of the population
ED50
Median toxic dose required for a toxic effect in 50% of the population
TD50
Dose which is lethal to 50% of the population
LD50
Window between therapeutic effect and toxic effect
Therapeutic index
Term for a high margin of safety
High therapeutic index
Term for a narrow margin of safety
Low therapeutic index
Antidotes and agents used in drug overdose

Antidote used for lead poisoning
Dimercaprol, EDTA
Antidote used for cyanide poisoning
Nitrites
Antidote used for anticholinergic poisoning
Physostigmine
Antidote used for organophosphate/anticholinesterase poisoning
Atropine, pralidoxime (2-PAM)
Antidote used for iron salt toxicity
Deferoxamine
Antidote used for acetaminophen (APAP) toxicity
N-acetylcysteine (Mucomyst)
Antidote for arsenic, mercury, lead, and gold poisoning
Dimercaprol
Antidote used in poisonings: copper (Wilson's disease), lead, mercury, and arsenic
Penicillamine
Antidote used for heparin overdose
Protamine
Antidote used for warfarin toxicity
Vitamin K and Fresh frozen plasma (FFP)
Antidote for tissue plasminogen activator (t-PA), streptokinase
Aminocaproic acid
Antidote used for methanol and ethylene glycol
Ethanol or fomepizole
Antidote used for opioid toxicity
Naloxone (IV), naltrexone (PO)
Antidote used for benzodiazepine toxicity
Flumazenil
Antidote used for tricyclic antidepressants (TCA)
Sodium bicarbonate
Antidote used for carbon monoxide poisoning
100% O2 and hyperbaric O2
Antidote used for digitalis toxicity
Digibind (also need to d/c digoxin, normalize K+, and lidocaine if pt. Is arrhythmic)
Antidote used for beta agonist toxicity (eg. Metaproterenol)
Esmolol
Antidote for methotrexate toxicity
Leucovorin
Antidote for beta-blockers and hypoglycemia
Glucagon
Antidote useful for some drug induced Torsade de pointes
Magnesium sulfate
Antidote for hyperkalemia
sodium polystyrene sulfonate(Kayexalate)
Antidote for salicylate intoxication
Alkalinize urine, dialysis
Cancer Chemotherapy

Relationship of tumor cell number to time of diagnosis, symptoms, treatment and survival
Log-kill hypothesis
Pyrimidine analog that causes "thymineless death" given with leucovorin rescue
5-fluorouracil (5-FU)
Drug used in cancer therapy causes Cushing-like symptoms
Prednisone
Side effect of Mitomycin
SEVERE myelosuppression
MOA of cisplatin
Alkylating agent
Common toxicities of cisplatin
Nephro and ototoxicity, peripheral neuropathy
Analog of hypoxanthine, needs HGPRTase for activation
6-mercaptopurine (6-MP)
Interaction with this drug requires dose reduction of 6- MP
Allopurinol
Iron-chelating agent, protects against doxorubicin toxicity by scavenging free radicals
Dexrazoxane
Blows DNA (breaks DNA strands), limiting SE is pulmonary toxicity
Bleomycin
Platinum-based combination therapy for testicular cancer
Bleomycin+etoposide+cisplatin
ABVD regimen used for Hodgkin's, but appears less likely to cause sterility and secondary malignancies than MOPP
Adriamycin (doxorubicin) +bleomycin,,vinblastine +dacarbazine
Regimen used for non-Hodgkin's lymphoma
CHOP (cyclophosphamide, doxorubicin, vincristine, and prednisone) plus rituximab
Regimen used for breast cancer
CMF (cyclophosphamide, methotrexate, and fluorouracil) and tamoxifen if ER+
Alkylating agent, vesicant that causes tissue damage with extravasation
Mechlorethamine
Anticancer drug also used in RA, produces acrolein in urine that leads to hemorrhagic cystitis
Cyclophosphamide
Microtubule inhibitor that causes peripheral sensory neuropathy , foot drop (eg. ataxia), and SIADH
Vincristine
Interact with microtubules (but unlike vinca which prevent disassembly of tubules), it stabilizes tubulin and cells remain frozen in metaphase
Paclitaxel (taxol)
Agent similar to cisplatin, less nephrotoxic, greater myelosuppression, used to treat refractory hematologic malignancies
Carboplatin
Anti-androgen used for prostate cancer
Flutamide, bicalutamide, nilutamide
Anti-estrogen used for estrogen receptor + breast cancer
Tamoxifen
Aromatase inhibitor used in breast cancer
anastrozole
Newer biologic agent approved for metastatic melanoma, enhances T-cell immune responses
Ipilimumab
Some cell cycle specific anti-cancer drugs
Bleomycin, vinca alkaloids, antimetabolites (eg., 5-FU, 6-MP, methotrexate, etoposide)
Some cell cycle non-specific drugs
Alkylating agents (eg., mechlorethamine, cyclophosphamide), antibiotics (doxorubicin, daunorubicin), cisplatin
Regimen used for advanced colorectal cancer, stageII and III colon cancer
FOLFOX (oxaliplatin, 5-FU and leucovorin)
Nitrosoureas with high lipophilicity, used for brain tumors
lomustine
Anti-cancer agents that affect the VEGF-signaling pathway
Bevacizumab, Ziv-aflibercept, Sorafenib, Sunitinib, Pazopanib