Even before the synthetic, target-based, and selective medicinal agents, remedies were abundantly provided by various plant sources more commonly referred to as herbal remedies

Dating back to the cavemen following their instincts to survive or preserve their lives, drugs already exist in various forms.

The DISCOVERY phase includes synthesis, isolation, fermentation, screening, and SAR studies

Focusing on the financial return

Receptors, enzymes, and nucleic acids

an increasing number of new receptors and enzymes potential drug targets

inducing a clinical condition and treated with the test drug

In vivo and in vitro.

drugs activity is tested on isolated tissues, cells, enzymes.

A compound showing a desired pharmacological property which can be used to initiate a medicinal chemistry project

Ways of discovering a lead compound

vaccines (living or killed microorganisms)

Morphine

Cocoaine.

Quinine

Prewingkle

Reserpine.

Paclitaxel.

Penicillin.

Cephalosporin.

Tetracycline.

Aminoglycosides.

Lovastatin.

Protein.

Somatostatin. (protein)

Glucagon (Protein)

Heparin (Polysaccharide)

Bile acids.

Estrogens.

Large libraries of compounds are tested for their ability to modify the target capable of examining 15,000 chemical compounds a week using 10 – 20 bioassays.

A popular term for a generic drug with an identical formulation and stated indications as a drug previously approved by the FDA.

atoms and functional groups required for a specific pharmacological activity, and their relative positions in space

Science of the properties of the drugs and it's effect in the body.

The study of the interaction of the drugs with cells.

The handling of a drug within the body. it includes the adme process.

In. vitro and in vivo testing, determination of LD 50.

Chemical and physical characterization, pharmacology, pharmacokinetics, pharmacodynamics, pharmaceutics, analytical studies, toxicology

The general area of study concerned with the formulation, manufacturing, stability, and effectiveness of a pharmaceutical dosage form

Filed before drug may be given to human (clinical trials)

Filed before drug may be given to human (clinical trials)

Special consideration is given on Orphan drugs (treatment IND) • orphan drug is used to treat orphan disease, or disease that affects fewer than 200,000 people in the US

Submitted to FDA à Review by FDA for 30 days

20-80 healthy volunteer.

For safety

100-300 Suffer from the target illness

Safety and effectiveness

1000-3000 with the target illness.

Safety, effectiveness and dosage

These studies are designed to determine the metabolic and pharmacological actions of the drug in humans, the side effects associated with increasing doses, and, if possible, to gain early evidence of effectiveness

These studies also evaluate drug metabolism, structure-activity relationships, and the mechanism of action in humans.

This phase of testing also helps determine the common short-term side effects and risks associated with the drug.

• Failure during Phase II testing is common • After phase 2, sponsors meet with the FDA (True/False)

These studies are intended to gather the additional information about effectiveness and safety that is needed to evaluate the overall benefit-risk relationship of the drug.

These studies also provide an adequate basis for extrapolating the results to the general population and transmitting that information in the physician labeling

Generic drug . A company needs to show the FDA that the drug is bioequivalent to the innovator drug

submitted for review and approval after the completion of the clinical trials and requirements have been met

Permit to market drug product

Post-marketing studies and manufacturing scale-up activities take place

Modification of drug formulation as obtained from manufacturing scale-up and validation process may be done

Conduct short-term toxicity studies ranging from 2 weeks to 3 months.

Dynamic interactions between drug molecules and cellular components

Cell or group of cells specialized to detect changes in the environment and trigger impulses in the sensory nervous system

Protein in nature and embedded in the cell membrane

a molecule that binds to a receptor

Amphotericin B.

Used as molecular tag.

Used as receptors.

DNA and RNA acting as a drug target.

What is B2-adrenoceptors Agonist.

What is B2-adrenoceptors Antagonist

What is B1-adrenoceptors Agonist

What is B1-adrenoceptors Antagonist

What is the H1 and H2 receptors agonist

What is the H1 receptors antagonist

What is the H2 receptors antagonist

What is the opiate u receptors antagonist

What is the opiate u receptors agonist

Protein catalysts are produced by living cells by acting as a surface or focus for the reaction, bringing the substrate(s) together and holding them in the best position for the reaction.

completely complementary relationship between the drug molecule and a specific area on the surface of the receptor molecule

Complementary relationship between the drug molecule and its active site

the intensity of the pharmacologic activity of a structurally specific drug is directly proportional to the number of receptors occupied by the drug

measure of how strongly a drug binds to a receptor

maximum biological effect resulting from a drug binding to its target

Caused by continuous prolonged exposure of receptors to drugs that disrupt the homeostatic equilibrium and result in altered levels of the receptors.

Result of downregulation

The target cells become desensitized and the effect of subsequent exposure to the same concentration of the drug is reduced.

An increased-concentration of the drug is required to produce an effect of the same magnitude as the initial exposure with a smaller drug concentration (T/F)