Term
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Definition
| administration of drug into the alimentary tract |
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Term
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Definition
| injection of drug into skin, muscle, or blood |
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Term
| Factors (chemical variable) affecting drug absorption |
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Definition
| Chemical structure, molecular weight, solubility, lipid solubility |
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Term
| Factors (physiological variable) affecting drug absorption |
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Definition
| Gastric motility, pH at absorption site, surface area at absorption site, blood flow, presence or absence of food |
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Term
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Definition
| Flux (molecules/unit of time)= (deltaC x A x Perm. coefficient)/Thickness |
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Term
| Henderson-Hasselbalch Equation |
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Definition
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Term
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Definition
| pH of bodily compartment similar to pH of unionized form of drug |
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Term
| Factors affecting bioavailability |
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Definition
1. drug metabolism by enzymes in the blood
2. binding to blood proteins |
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Term
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Definition
| 2 phase process that modifies the chemical structure of compounds, generally to inactivate and make more water-soluble. |
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Term
| Phase I of biotransformation |
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Definition
| chemical reactions that change molecule, can be oxidation, reduction, or hydrolysis. |
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Term
| Phase II of biotransformation |
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Definition
| addition of another molecule to modified drug, via conjugation. |
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Term
| Urine pH affect on drug excretion |
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Definition
| weak acids excreted more readily in alkaline urine; weak bases excreted more readily in acidic urine |
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Term
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Definition
relates the amount of drug in the body to the concentration of the drug in the blood or plasma
Vd= amount of drug in body/ concentration of drug in blood |
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Term
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Definition
factor that predicts the rate of elimination in relation to the drug concentration
CL= rate of elimination/ concentration of drug |
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Term
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Definition
Clearance is constant over the concentration range encountered in clinical settings
Rate of elimination= CL x concentration |
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Term
| Capacoty-limited elimination |
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Definition
CL=(Vmax x C)/(Km + C)
when C>>Km, elimination rate becomes independent of drug concentrations |
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Term
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Definition
| elimination of drug depends primarily on the rate of drug delivery to the organ |
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Term
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Definition
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Term
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Definition
the effect of first-pass hepatic elimination on bioavailability is expressed as the extraction ratio
ER=CLliver/Q, where Q=hepatic blood flow |
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Term
| Systemic bioavailability of drug equation |
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Definition
| F (systemic bioavail.)= f (extent of absorption) x (1-ER) (extraction ratio) |
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Term
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Definition
at a steady state, the dosing rate must equal the rate of elimination
DR=RE=CL x TC (target concentration) |
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Term
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Definition
when giving intermittent doses, the maintenance dose is calculated
MD=dosing rate x dosing interval |
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Term
| Dosing rate w/less than 100% bioavailability |
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Definition
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Term
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Definition
When using maintenance dosing, it may take 4-5 half-lives to reach steady-state, thus a fast onset can be achieved via loading
Loadin dose=Vd x TC |
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Term
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Definition
| important in controlling phase I reactions, particularly oxidation, enzymes especially abundant in liver |
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Term
| The Big Four of Pharmacokinetics |
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Definition
A-D-M-E
Absorption
Distribution
Metabolism
Excretion |
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Term
| Pediatric absorption differences |
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Definition
less muscle mass may impact absorption
GI function
irregular peristalsis and changes in bile production may lead to unpredictable absorption |
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Term
| Pediatric distribution differences |
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Definition
neonates can have up to 85% of total weight be water
lipid content can be greatly decreased in preterm neonate
protein binding may be diminished in neonates |
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Term
| Pediatric metabolism differences |
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Definition
| cytochrome P450 can be decreased in early life |
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Term
| Pediatric excretion differences |
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Definition
| GFR can be markedly lower in preterm and neonates |
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Term
| Drugs targeting opiod receptors |
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Definition
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Term
| Drugs targeting B receptors |
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Definition
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Term
| Drugs targeting estrogen receptors |
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Definition
| ethinyl estradiol, tamoxifen |
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Term
| Drugs targeting voltage-gated Na+ channels |
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Definition
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Term
| Drugs targeting acetylcholinesterase |
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Definition
| neostigmine, organophosphates |
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Term
| Drugs targeting cyclooxygenase |
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Definition
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Term
| Drugs targeting catecholamine reuptake |
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Definition
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Term
| Alpha part of heterotrimeric G receptor |
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Definition
| Involved in inhibition of adenylate cyclase |
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Term
| Quantal dose response curve |
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Definition
| Shows how many of a given population respond to a drug at a certain dose to elicit a certain response |
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Term
| Concentration response curve |
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Definition
| shows concentration (x) vs. effect/maximum effect (E/Em) (y) |
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Term
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Definition
| defined by the therapeutic effect that is sought, and is graphed as a y-axis |
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Term
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Definition
| amount of drug needed to garner a desired effect |
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Term
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Definition
| ratio of the dose of the drug lethal to 50% of the population to the dose of the drug therapeutically effective to 50% of the population |
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Term
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Definition
| shows effect in relation to dose, for individual patient |
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Term
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Definition
Drug A + Drug B= effect A + effect B
PREDICTABLE! |
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Term
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Definition
Drug A + Drug B= effect A2 + effect B2
UNPREDICTABLE! |
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Term
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Definition
| requires that agonist can be overcome |
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Term
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Definition
| decreased effectiveness of a drug that results from repeated drug exposure |
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Term
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Definition
| enzyme inducement following repeat exposure |
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Term
| Pharmacodynamic tolerance |
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Definition
| repeated administration of a drug produces changes to drug receptors and second messenger systems (affects drugs effect on body) |
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Term
| Pharmacodynamic tolerance |
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Definition
| repeated administration of a drug produces changes to drug receptors and second messenger systems (affects drugs effect on body) |
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Term
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Definition
| development of tolerance can be influenced by learning and conditioning processes |
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Term
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Definition
| A rapidly decreasing response to a drug following administration of the first dose |
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Term
| Effect of St. John's Wort on CYP450-3A4 |
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Definition
| CYP450-3A4 is a major liver enzyme, and SJW decreases serum concentration of some other important drugs via this enzyme |
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Term
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Definition
| Most popular herbal among all age groups and sexes, use to decrease cardiovascular disease risk |
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Term
| Sensitization or Reverse tolerance |
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Definition
| Continuing to take a drug leads to an increased effect |
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