Term
| 1.) Discovery and characterization of a new drug |
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Definition
*isolate or sythisize a new drug.
*determine chemcial and pharmaceutical properties of the new drug. |
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Term
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Definition
*Determine pharmacokinetic and pharmacodynamic properties of the drug.
*Test animals for toxicity (acute, subacute, and chronic), teratogenesis, mutagenesis, and carcinogenesis. |
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Definition
*Outline properties of the drug.
*Report results of studies to date.
*Propose clinical studies (sites, investigators, protocols, and methods of data analysis) |
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Term
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Definition
*PHASE 1- gather data on drug safety and pharmacokinetics in healthy volunteers.
*PHASE 2- Gather data on efficacy, safey, and proper dosage in a small group of pt's.
*PHASE 3- Obtain statistical evidence of drug safety and efficacy. |
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Term
| 4.) PHASE 1 of clinical studies |
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Definition
Gather data on drug safety and pharmacokinetics in healthy volunteers.
Seek to determine the pharmacokinetic and safety of an IND in healthy human subjects. The subjects typically undergo physical examination, imaging studies, and chemical and pharmacokinetic analyses of samples of blodd and other body fluids. The pharmacokinetic analyses provide a basis for estimating doses to be employed in the next phase of studies and the other examinations seek to determine if the drug is safe for use in humans. |
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Term
| 4.) PHASE 2 of clinical studies |
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Definition
Gather data on efficacy, safey, and proper dosage in a small group of pt's.
The first studies to be performed in human subjects who have the particular disease for which the IND is to be used. These studies use a small number of pt's to obtain a preliminary assessment of the drugs efficacy and safety in diseased individuals and to establish a dosage range for further clinical studies. |
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Term
| 4.) PHASE 3 of clinical studies |
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Definition
Obtain statistical evidence of drug safety and efficacy.
Are conducted to compare the safety and efficacy of the IND with that of another substance or treatment approach. Employs a larger group of subjects, 100s or even 1000s ppl large. Phase 3 are often double blind and placebo controlled. Phase three trials often involve crossover studies in which the pt's recieve one medication of placebo for a period of time and then are switched, after a washout period, to the other medication or placebo. A clinical study is topped if an IND has been found to cause a significant increase in rate of mortality or serious toxicity. |
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Term
| 5.) Submission of the NDA |
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Definition
*Outline properties of the drug.
*Report results of all experimental and clinical studies.
*Propse labeling of drug and clinical indications for use. |
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Term
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Definition
| New drug application. The FDA often requires a number of months to review the NDA before deciding whether to permit the drug to be marketed. Approved drugs are labeled for specific indications based on the data submitted to the FDA. Some drugs are found to have other clinical uses after the drug has been marketed. These indications are known as unlabeled or "off label" uses. |
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Term
| 7.) Postmarketing surveillance |
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Definition
| Gather and analyze voluntary reports of adverse effects submitted by health care professionals. |
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Term
| 3.) IND (investigational new drug) |
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Definition
| FDA must approve an application for an investigational new drug before the drug can be distributed for the purpose of conducting studies in human subjects. The IND application includes a complete description of the drug, the results of all experimental studies completed to date, and a description of the design and methods of the proposed clinical studies and the qualifications of the investigators. |
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Term
OXIDATIVE RXN:
Aliphatic hydroxylation
adding an OH group. |
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Definition
| examples- ibuprofen, pentobarbital, and tolbutamide |
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Term
OXIDATIVE RXN:
Aromatic hyroxylation
adding an OH group onto aromatic ring |
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Definition
| examples- phenbarbital, phenytoin, & propranolol. |
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Term
OXIDATIVE RXN:
N-Dealkylation
Carbon group off Nitrogen |
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Definition
| examples- codeine, imipramine, & theophylline |
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Term
OXIDATIVE RXN:
O-Dealkylation
Carbon group off Oxygen |
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Definition
| examples- Codeine, dextromethacin, and indomethacin |
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Term
OXIDATIVE RXN:
Deamination
taking away an amine group |
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Definition
| examples- amphetamine and diazepam |
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Term
OXIDATIVE RXN:
N-Oxidation
adding oxygen to nitrogen group |
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Definition
| examples- Chlorpheniramine |
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Term
OXIDATIVE RXN:
S-Oxidation
Adding oxygen to sulfur group |
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Definition
| examples- chlorpromazine & cimetidine |
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Term
HYDROLYTIC RXN:
Amide hydrolysis
adding H2O to amide |
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Definition
| examples- lidocaine and procainamide |
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Term
HYDROLYTIC RXN:
Ester hydrolysis
adding H20 to ester group |
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Definition
| examples- aspirin, esmolol, and procaine |
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Term
REDUCTIVE RXNS:
Nitro reduction |
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Definition
| examples- chloramphenicol |
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Term
REDUCTIVE RXNS:
Reductive hydrolysis |
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Definition
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Term
| The ratio of the ionized and non-ionized form of drugs at a particular site influences the rate of drug absorption, distribution, or elimination. |
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Definition
The protonated form of a weak acid is nonionized, whereas the protonated form of a weak base is ionized.
eg: he's a pro (tonated) at taking acid, so he's NOt(non-ionized) going anywhere.-- WAPN
eg: he's a pro (tonated) at BASEball so he's ionized.-- WBPI |
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Term
| The log ratio of non-ionized acidic drug to it's ionized form. |
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Definition
| Hendersson-Hasselbalch equation. |
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Term
| Henderson-Hasselbalch equation |
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Definition
| log* [protonated form]/[non-protonated form]= pKa-pH |
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Term
if it's acid protonated goes before non protonated or non-ionized goes before ionized- eg:
the log ratio of the non-ionized acidic drug to it's ionized form. |
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Definition
if it's basic, non protonated goes before protonated or ionized goes before non-ionized- eg:
the log ratio of the ionized basic drug to it's non-ionized form |
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Term
| Most drugs are absorbed by _____________ _______________ across a biologic barrier and into the circulation. |
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Definition
| Most drugs are absorbed by passive diffusion across a biologic barrier and into the circulation |
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Term
| The rate of absorption is __________ to the drug concentration gradient across the barrier and the surface area available for absorption. |
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Definition
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Term
| When drugs are administered orally, distribution occurs ______________ with absorption, and the rate of distribution can't be determine from the plasma drug concentration curve. |
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Definition
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Term
| Almost all drugs are__________ bound to plasma proteins, primarily ___________. |
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Definition
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Term
| The extent of drug binding depends on the _____________ of a particular drug for protein-binding sites and ranges from less than __________ to as high as _________ of the plasma concentration. |
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Definition
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Term
| Plasma protein binding is saturable and a drug can be displaced from binding sites by other drugs that have a higher affinity for such sites. This causes a temporary increase in the __________ ________________ of the displaced drug and can lead to an __ |
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Definition
free concentration; increased
increased in the free concentration of the displaced drug and can lead to an increased tissue concentration and pharmacologic effect. |
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Term
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Definition
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Term
| Phase 1 biotransformation |
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Definition
| incules oxidative, hydrolytic, and reductive reactions. Oxidative rxns are the most common type. They're catalyzed by enzymes isolated in the microsomal fraction of liver homogenates & by cytoplasmic enzymes. |
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