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90 Cards in this Set

  • Front
  • Back
Time it takes for drug to fall to half its value; this is constant in first order kinetics (majority of drugs)
Half life (T1/2)
Relates to 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)
Elimination of a drug that occurs before it reaches systemic circulation
First pass effect
Fraction of administered dose of a drug that reaches systemic circulation
bioavailability
When rate of drug input equals the rate of drug elimination
Steady state
This step of metabolism makes a drug more hydrophilic and hence augments elimination
Phase 1
Different steps of Phase I
hydrolysis, oxidation, reduction
Inducers of Cytochrome P450
rifampin, barbiturates, phenytoin, carbamazepine
Inhibitors of CYP450
grapefruit juice, ketaconazole, cimetidine, erythromycin
Products of Phase II conjugation
glucoronate, acetic acid, glutathione sulfate
Type of kinetics when a constant percentage of substrate is metabolized per unit
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 plasma times (clearance divided by bioavailability)
Maintenance dose (Cp * (Cl/F)
Strength of interaction between a 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 achievable from a drug
Efficacy
Ability of 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 utilizes intracellular receptors
Thyroid hormones
steroid hormones
A hormone whose MOA utilizes transmembrane receptors
Insulin
Class of drugs whose MOA utilizes ligand gated ion channels
Benzodiazepines
calcium channel blockers
Median effective dose required for an effect in 50% of 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 high margin of safety
High therapeutic index
Term for narrow margin of safety
Low therapeutic index
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, arsenic
Penicillamine
Antidote used for heparin overdose
Protamine
Antidote used for warfarin toxicity
Vitamin K
Fresh Frozen Plasma
Antidote for tissue plasminogen activator (t-PA), streptokinase
Aminocaproic acid
Antidote used for methanol and ethylene glycol
Ethanol
Fomepizol
Antidote used for opiod toxicity
Naloxone (IV)
Naltrexone (oral)
Antidote used for benzodiazepine toxicity
Flumanezil
Antidote used for tricyclic antidepressants (TCA)
sodium bicarbonate
Antidote used for carbon monoxide poisoning
100% Oxygen (O2)
Hyperbaric O2
Antidote used for digitalis toxicity
Digibind (also need to d/c digoxin, normalize potassium, and lidocaine is patient is arrhythmic).
Antidote 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)
Constant proporation of cell population killed rather than a constant number
log-kill hypothesis
Treatment with cancer chemotherapy at high doses every 3-4 weeks, too toxic to be used continuously
Pulse therapy
Toxic effect of anticancer drug can be lessened by rescue agents
rescue therapy
Drug used concurrently with toxic anticancer agents to reduce renal precipitation of urates
Allopurinol
Pyrimidine analog that causes "thymine-less death" given with leucovorin rescue
5-flouracil (5-FU)
Drug used in cancer therapy causes Cushing-like symptoms
Prednisone
Side effect of mitomycin
SEVERE myelosuppresion
MOA of cisplatin
Alkylating agent
Common toxicities of cisplatin
Nephrotoxicity
Ototoxicity
Analog of hypoxanthine, needs HGPRTase for activation
6-mercaptopurine (6-MP)
interaction with drug requires dose reduction of 6-MP
Allopurinol
May protect against doxorubicin toxicity by scavenging free radicals
Dexrazoxane
Blows DNA (breaks DNA strands) limiting SE is pulmonary fibrosis
Bleomycin
Bleomycin + vinblastine + etoposide + cisplatin produce almost a 100% response when all agents are used for this neoplasm
Testicular cancer
ABVD regimen for HD, but appers less likely to cause sterility and secondary malignancies than MOPP
Adriamycin (Doxorubicin)
Bleomycin
Vinblastine
Dacarbazine
Regimen used for non-Hodgkin's lymphoma
CDVP (cyclophosphamide, doxorubicin, vincristine, and prednisone) plus rituximab
Regimen used for breast cancer
CMF (cyclophosphamide, methotrexate, and flourouracil)
Alkylating agent, vesicant that causes tissue damage with extravasation
Meclorethamine
Anticancer drug also used in RA, produces acrolein in urine that leads to hemorrhagic cystitis
Cyclophosphamide
Prevention of cyclophosphamide induced hemorragic cystitis
Hydration
mercaptoethanesulfonate (MESNA)
Microtubule inhibitor that causes peripheral neuropathy, foot drop (eg. ataxia), and "pins and needles" sensation
Vincristine
Interact with microtubules (but unlike vinca whch prevent disassembly tubules), it stabilizes tubulin and cells remain frozen in metaphase
Paclitaxol (taxol)
Toxicities include nephrotoxicity and ototoxicity, leading to severe interaction with aminoglycosides
Cisplatin
Agent similar to cisplatin, less nephrotoxic, but greater myelosuppresion
Carboplatin
Converts asparagine to aspartate and ammonia, denies cancer cells of essential AA (asparagine)
L-asparaginase
Used for hairy cell leukemia; it stimulates NK cells
interferon alpha
Anti-androgen used for prostate cancer
Flutamide (eulexin)
Anti-estrogen used for esterogen receptor + breast cancer
Tamoxifen
Aromatase inhibitor used in breast cancer
Letrozole
Anastrozole
Newer estrogen receptor antagonist used in advanced breast cancer
Toremifene (Fareston)
Some cell cycle specific anti-cancer drugs
Bleomycin
Vinca alkaloids
Antimetabolites: 5-FU, 6-MP, methotrexate, etoposide
Soem cell cycle non-specific drugs
Alkylating agents: meclorethamine, cyclophosphamide
Antibiotics: doxorubicin, daunorubicin
Cisplatin
Nitrosourea
Anti-emetics used in assocation with anti-cancer drugs that are 5-HT3 (serotoning receptor subtype) antagonists
Odansetron
Granisetron
Nitrosoureas with high lipophilicity, used for brain tumors
Carmustine (BCNU)
Lomustine (CCNU)
Produces disulfarim-like reaction with ethanol
Procarbazine