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Definition
The rate and extent at which an active drug is absorbed from the product and become available at the site of drug action.
- measure blood urine concentration
- Assumes drug at site of action = drug in the blood |
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Definition
(F) fraction of dose reaching systemic circulation: 0-1.
Measure blood concentration / time |
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Definition
Compare formulations Cmax, Tmax, Auc
Cmax: maximum concentration
Tmax: time of Cmax
AUC (area under curve) |
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Term
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Definition
| Active ingredients of two products are the same, and rate and extent are the same |
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Definition
Two drugs are administered similarly w/ same effect.
- Bioequivalent should be equal to therapeutic effect |
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Definition
Comparing bioavailabilities
* 90% confidence interval
* 0.8-1.25 at 0.05 level of significance |
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Term
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Definition
| the measurement and analysis of an organism's time-dependent course of a pharmaceutical as it passes through the different fluids, tissues, and excreta of the body using compartmental or non-compartmental mathematical models |
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Term
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Definition
| the study of the biochemical and physiological effects of drugs and the mechanisms of their actions, including the correlation of their actions and effects with their chemical structure |
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Definition
| The study of how the actions of and reactions to drugs, cary with the patients' genes |
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Term
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Definition
| the analysis of the expression, localization, functions, and interactions of the proteins produced by the genes of an organism |
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Term
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Definition
| computerized automated delivery and manipulation of information to and by users of computer systems |
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Definition
| Area between MEC : minimum effective concentration and MTC: maximum toxic concentration. |
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Term
| Factors affecting therapeutic window |
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Definition
| patient compliance, pathophysiology, age, deit, drug interactions, physiology: gender/pregnancy |
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Term
| Therarpy of Parkinson's Disease |
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Definition
Dopamine generating cells of substantia nigra, symptoms: shaking, rigidity, slow movement.
Tablet therapy: initially sinemet 25/100 q6-8 hours
- sinement ER doesed in three divided doses daily
* Duopa enteral supsension
- levodopa-carbidopa intestinal gel delivered continuously via percutaneous endoscopic gastrojejunostomy tube |
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Term
| Overton's rule of membrane permeability |
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Definition
| entry of any molecule into a cell is the result of its "selective solubility" in the cell's boundary, and the more soluble in lipids the molecule is, the greater its permeability. |
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Term
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Definition
primary active transporter
Extensively distributed and expressed in the intestinal epithelium, hepatocytes, renal proximal tubular cells, adrenal gland and capillary endothelail cells comprising the blood-brain and blood testis barrier.
- implicated in multi-drug resistance
- an efflux transporter, moving substrates from cytosol into extracellular region |
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Term
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Definition
cystic fibrosis transmembrane conductance regulator, 1480 amino acids.
- chloride and thiocyanate transport |
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Term
| PepT1 intestinal peptide transporter |
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Definition
| Reabsorption and uptake from GI lumen into enterocytes |
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Term
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Definition
| e.g. sodium-calcium exchanger |
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Term
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Definition
| e.g. glucose transporter SGLT1, moves one glucose in with two sodium ions |
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Term
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Definition
| Absorption, Distriubution, Metabolism, Excretion |
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Term
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Definition
movement throughout the body
- blood perfusion, membrane permeability, tissue binding, partitioning
- Dispostion distribution and elimination
- Elimination: chemical transformation and/or physical removal of a drug |
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Term
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Definition
| Vd = total amount of drug in the body / drug blood plasma concentration |
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Term
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Definition
Lipophilic drugs are more efficiently deposited in cells and tissues, are readily reabsorbed across renal tubular cells, tend to be highly bound to plasma proteins
- mteabolites tned to be more polar, more hydrophilic, more readily exreted by the kindeys and liver |
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Term
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Definition
| cytochrome P450 microsomal enzymes, smooth endoplasmic reticulum of liver. Oxidation, reduction, and hydrolysis. HOR |
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Term
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Definition
conjugation generally increases hydrophilicity for excretion by kidney or bile. Methylation sulphation, acetylation, glucuronidation
MAGS |
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Term
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Definition
Transporters: liver, intestine, kidney, brain
P-gp, mutlidrug resistance protein, OAT2 |
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Term
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Definition
| After a drug is swallowed, it is absorbed by the digestive system and enters the hepatic portal system. It is carried through the portal vein into the liver before it reaches the rest of the body. The liver metabolizes many drugs, sometimes to such an extent that only a small amount of active drug emerges from the liver to the rest of the circulatory system. This greatly reduces the bioavailability of the drug. |
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Term
| Enzyme induction -- inhibition |
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Definition
Enzyme induction is a process in which a molecule (e.g. a drug) induces (i.e. intiates or enhances) the expression of an enzyme.
Inhibition: inhibition of enzyme expression by another molecule, inteference at the enzyme-level, basically with enzyme function. |
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Term
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Definition
Highly Active Anti-retroviral therapy, regimens to improve bioavailability of other drugs.
- Includes ritonavir an HIV protease inhibitor |
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Term
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Definition
Routes: urine, breath, feces, bile, milk, perspiration, saliva, tears and hair
- kidney most important organ
- feces: usually involve orally ingested unabsorbed drugs or metabolites excreted in the bile that are not reabsorbed from the intestinal tract
- pulmonary excretion is important as it pertains to the elimination of anesthetic gases and vapors as well as alcohol |
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Term
| Low bioavailability causes |
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Definition
| First-pass effect, drug chemical properties ( low water solubility, pka), insufficient time in GI tract , competing reactions, enzyme induction or inhibition, patient age, concomitant diseases |
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Term
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Definition
| Product ID and info, protection, convenience and compliance, containment during storage, attractive appearance. |
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Term
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Definition
sum of packaging components that together contain and protect the dosage form.
Primary: may be in contact with dosage form
Secondary: is not and will not be in direct contact with the dosage form |
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Term
| Plastic Packaging Materials |
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Definition
Advantages: light weight, reduced volume, no corrosion, good resistance to mold/bacteria, gnearlly inert (caution with solvents), good impact strength, wide design and decorative possibilities, wide range of manufacturing processes
* Disadvantages: gas permeability, stress cracking, leaching, heat sensitive |
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Term
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Definition
| 1998, EPO from outside us, Polysorbate 80 and uncoated rubber stoppers or prefilled syringes. Protein denaturation. |
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Term
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Definition
Protective properties change b/c thickness decreases. Good seal = 3mm from the edge of the blister cavity to the nearest edge or perforation is recommended
** Cold form foil is an extreme barrier for products that are moisture or light sensitive |
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Term
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Definition
drug degradation from moisture and oxidation
- stabilox a packaging to reduce moisture and oxygen levels |
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Term
| 671 Containers - Performance Testing |
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Definition
| Store at 75 +/- 3% relative humidity and a temperature of 23 + 2 degrees celcius |
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Term
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Definition
| no more than 1/10 exceed 100mg per day per L in moisture permeability, and none exceeds 200mg per day per L |
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Definition
| if not more than 1 of the 10 test containers exceeds 200mg per day per L in moisture permeability, and none exceeds 300 mg per day per L |
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