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"Approved Drug Products with Therapeutic Equivalence Evaluations" aka...: Orange Book
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Absolute Bioavailability: fraction of the administered dose that reaches systemic circulation relative to an intravenous dose
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Active Pharmaceutical Ingredient: The medicinal agent or active drug in a dosage form
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Active Transport: process using a "carrier" with the additional feature of the drug being moved across the membrane against a concentration gradient; from lower concentration to higher concentration
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ADME: Drug Absorption, Distribution, Metabolism, and Elimination
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Area under the serum concentration time curve (AUC): Measures the total amount of drug absorbed into systemic circulation following the administration of a single dose of drug
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As the drug at the absorption decreases...: the amount of drug excreted and the total amount of metabolites increase. The amount of drug in the body initially increases, but then decreases
8.
Bioavailability: the RATE and EXTENT to which an active drug ingredient or therapeutic moiety is absorbed from a drug product and becomes available at the site of action
9.
Bioavailability Data are required for...: New drug applications (NDA), abbreviated NDA, and supplemental applications if there is a change in manufacturing process, a new indication for use of the drug, or a new or additional dosage regimen for a special patient population
10.
Bioavailability Data are used to determine...: the amount of drug absorbed from a dosage form, the rate at which the drug was absorbed, the duration of the drug's presence in the biologic fluid or tissue, and the relationship between drug blood levels and clinical efficacy and toxicity
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Bioavailability Equation (F): F= (AUCpo DOSEiv)/(AUCiv DOSEpo)
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Bioequivalent drugs should...: have similiar AUC and Peak height concentration (have super-imposable concentration-time profiles)
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Biopharmaceutics: Area of study dealing with the relationship between physical, chemical, and biological aspects of drugs, dosage forms, and drug action
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Curves that have different peak height concentrations and time of peak.....: may have the same area under the serum concentration time curve (AUC)...meaning the dose of the drug absorbed into circulation are equal
15.
Degree of Drug Binding to Plasma Protein: Alpha = (Cb/(Cb + Cu)) Cb = Concentration bound to protein; Cu = Concentration not bound to protein
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Disc: Longest lasting dosage form
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Drugs that are weak acids are absorbed best where?: Stomach. because the stomach has a very acidic environment which allows the weak acid to be in its non-ionized form.
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Drugs that are weak bases are absorbed best where?: Small Intestines. because the small intestines have a more alkaline environment which allows the weak-base to be in its non-ionized form.
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Excipients: Any non-medicinal agent in a dosage form. (Diluents/Fillers, Binders, Disintegrants, Surfactant, Lubricants/Glidants)
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F= FA FI FH: FA = fraction of the administered dose that is not destroyed in the gut or lost in the feces; FI = the fraction of the dose that escapes metabolism in the intestinal wall; FH = the fraction of the dose that escapes metabolism on first-pass through the live
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Facilitated Diffusion: Specialized transport using a "carrier", but the drug is not moved against a concentration gradient
22.
Factors that affect drug absorption...: Physiology of the GI tract; Physiochemical characteristics of the drug; and dosage form
23.
Factors that affect ORAL bioavailability: Lipophilicity of the drug (Lipophilic drugs penetrate membrane easier); Surface area for absorption (microvilli); Intestinal blood flow; Gastric emptying time (any delay in drug reaching small intestines will slow the rate of absorption)
24.
FDA criteria for bioequivalence...: Ratio of AUC and Peak Height Concentration is calculated for each individual study (brand/generic); the average ratio is calculated; Study must be large enough to provide an 80% probability to detect a 20% difference in average bioavailability
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FDA may bioavailability data requirements if...: Solution is used solely for IV administration and it contains the same API in the same concentration and solvent as a previously approved product. And for topical preparations intended for local therapeutic effect.
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Fick's Law: dc/dt = P(C1-C2)
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Generic Drugs must...: Contain the same API; be identical in strength, dosage form, and route of administration; have the same indications and precautions for use and other labeling instructions; be bioequivalent; meet same batch-to-batch requirements for identity, strength, purity, and quality
28.
If equivalent doses of a drug in different formulations provide different AUC levels...: it means that there are differences in the extent of absorption
29.
In general, dissolution rate correlates better with absorption for drugs that are...: highly permeable (highly lipophilic)
30.
Increasing the dose of a particular drug will....: Increase the peak height concentration and the area under the serum curve
31.
MEC: Minimum Effective Concentration; drug concentration that must be achieved for the patient to exhibit adequate response
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Most drugs are...: Weak bases or weak acids
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MTC: Minimum Toxicity Concentration; drug concentrations should generally not exceed this level
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Noyes-Whitney Equation: dC/dT = kS(Cs-Ct) k = dissolution rate constant; S=surface area of particles; Cs = concentration of drug in the immediate proximity of the dissolving particle; Ct = concentration of drug in the bulk fluid
35.
Oral dosage strengths are based on...: considerations of the proportion of the dose administered that is expected to be absorbed
36.
Passive Diffusion: Passage of drug molecule(s) through a membrane that does not actively participate in the process. Calculated by Fick's Law
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Peak Height Concentration (Cmax): the rates of absorption and elimination are equal, and conventional dosage forms such as tablets only have one maximum of this. Also, expressed as a concentration (amount of drug/specific volume of blood)
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Pharmaceutical Equivalents: drug products that contain the same strength of amount of the active ingredient in the same dosage form to be given by the same route of administration
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Pharmaceutics: Area of study concerned with the formulation, manufacture, stability, and effectiveness of dosage forms
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Pharmocokinetics: Area of study that elucidates the time course of drug concentration in the blood and tissues
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Products are rate B if...: the FDA does not consider them to be therapeutically equivalent and should not be substituted with A rated products
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Products are rated A if...: the FDA considers them to be therapeutically equivalent
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Products are rated AA...: if the product is therapeutically equivalent on basis of in vitro testing
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Products are rated AB...: if the product is therapeutically equivalent on basis of in vivo testing
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Products that are bioequivalent are...: therapeutic equivalent
46.
Regardless, of a drug being a weak base or weak acid, the preferred site of drug absorption is where?: Small Intestines. the short residence time, small surface area, and low perfusion rate make the small intestines the preferred site of absorption for weak acids as well.
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Relative Bioavailability: fraction of the adminstered dose which reaches the systemic circulation relative to another dosage form or product
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Sublingual Dosage Form: Quickest route to get drug to the site of action
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Therapeutic Equivalents: pharmaceutical equivalents that are expected to produce the same clinical effects and safety profile
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Time of Peak (Tmax): reflects the rate of absorption from a formulation, which determines the time needed for the MEC to be reached and maintain it
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Types of Dosage Forms: Solids, Semi-Solids, Inserts, Liquids, Sterile Products, and Novel Delievery Systems
52.
What are the parameters for assessment of bioavailability: Peak Height Concentration (Cmax), Time of the peak concentration (Tmax), and the area under the blood concentration time curve (AUC)
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When (F) is less than 1: Oral dose must be larger than IV dose to provide the same concentration of drug in the plasma; variability from patient to patient increases at this point
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When dissolution is the rate-limiting step in in absorption...: faster in vitro dissolution may lead to faster absorption
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When rate of absorption is decreased..: the peak height concentration is lowered and the time of peak occurs later
56.
Why are dosage forms needed: Provide correct drug dose, Protect API during storage and from gastric acid, Conceal undesirable taste, Provide rate controlled drug action, Provide optimal drug action from topical sites
