| Methods of Drug Discovery | 1 Random Screening
2 Molecular manipulation
3 Molecular designing
4 Drug metabolites
5 Serendipity |
| testing of synthetic organic compounds for biologic activity | Random Screening |
| Chemical alteration of previously characterized organic compound to enhance its usefulness. | Molecular manipulation |
| To design a drug that interferes specifically with known or suspected biochemical pathway or mechanism of disease process. | Molecular designing |
| for Prodrugs | Drug metabolites
ex. Enalaprilat as metabolite of enalapril |
| by good chance | Serendipity |
| What steps are involved in developing a new drug? | 1 In vitro studies (0-2 years)
2 Animal Testing (IND)
3 Clinical Testing (NDA)
4 Marketing (20 years) |
| it is a summary of the entire drug development process; contains
1 Essential chemistry, pcol, toxi
2 I, C/I for use
3 A/E
4 Formulation composition
5 Dosage
6 Storage requirements | Package Insert |
| Drug Sources | 1 Plants
2 Animals
3 Mineral / Earth Sources
4 Synthetic / Semi-synthetic sources
5 Microbiological sources
6 Genetic Engineering |
| Drugs of Plant Sources | 1 Reserpine from Rauwolfia serpentina
2 Vinca rosea – Periwincle, Rosas de baybayon |
| Techniques which influence cells’ ability to produce proteins
__, __
Common to each technique is the ability to manipulate and produce __ | 1 rDNA
2 mAb
3 proteins |
| genetic material is transplanted from higher species (humans) into a lowly bacterium; induce the lower organism to make proteins it would not supposedly have. | Gene-splicing |
| Gene Splicing products | 1 Human insulin
2 Human growth hormone
3 HepaB vac
4 epoetin alfa
5 interferon. |
| 1st FDA approved mAb | Muromonab |
| Production process usually starts with generation of mAb-producing cells (i.e. hybridomas) by fusing myeloma cells with desired antibody-producing splenocytes (e.g. B cells), typically sourced from animals, usually mice. | Monoclonal antibodies (mAb) |
| Used to prevent, treat, cure, diagnose, or mitigate human diseases caused by genetic disorders.
Medical intervention is based on the modification of the genetic material of the living cells. | Human Gene Therapy |
| the branch of medicine concerned with the uses, effects, and modes of action of drugs. | Pharmacology |
| 2 major branches of Pharmacology | 1 Pharmacokinetics
2 Pharmacodynamics |
| refers to the absorption, distribution, metabolism, and excretion of drugs. | Pharmacokinetics |
| which physiological effects of drugs, including drug mechanism of action. | Pharmacodynamics |
| LADME Process | Input
1 Liberation
2 Absorption
3 Distribution
Output
4 Metabolism
5 Excretion |
| 1 The release of drug from its dosage form
2 The movement of drug from the site of administration to the blood circulation | 1 Liberation
2 Absorption |
| 1 The chemical conversion or transformation of drugs into compounds which are easier to eliminate
2 The elimination of unchanged drug or metabolite from the body via renal, biliary, or pulmonary processes
3 The action of the body to the drug administered | 1 Metabolism
2 Excretion
3 Response |
| The LADMERT system is key to the following tasks: | 1 Development of new active compounds, analogs, or derivatives;
2 Development of dosage forms with desired release characteristics;
3 Determination of pharmacokinetic parameters and pharmacokinetic drug product profiles;
4 Determination and evaluation of bioavailability;
5 Selection of the most appropriate route of administration;
6 Determination of effective dose sizes; and
7 Adjustment of dosage regimen to achieve a desired therapeutic concentration of drug in the body based on physiologic (e.g., body weight, age, sex) and pathologic (e.g., renal, hepatic, or heart failure; obesity; malnutrition) factors. |
| involves the study of the adverse effects of chemical substances on living organisms and the practice of diagnosing and treating exposures to toxins and toxicants.
As part of the IND application, FDA requires an integrated summary of toxicological effects of the drug in animals and in vitro. | Toxicology |
