PHA6125 - Unit 1: Introductory Concepts in Drug Discovery and Development

Vocabulary flashcards covering medicinal chemistry principles, stereochemistry models, and stages of drug discovery and development.

Crude drugs

Plant extracts containing a mixture of potentially active molecules that have had their solvents evaporated.

Small molecules

Organic or inorganic drug compounds characterized by a molecular weight of less than 500 ($MW < 500$).

Biopharmaceuticals

Large biomolecules such as peptides, nucleic acids, and monoclonal antibodies with molecular weights in the tens of thousands.

Me-too drugs

Improved versions of existing drugs with a known target, designed with altered R-groups to lessen toxicity or optimize effects.

Agonist

A ligand or drug molecule that binds to a specific receptor target and possesses intrinsic action.

Antagonist

A ligand or drug molecule that binds to a receptor target but lacks intrinsic action, thereby inhibiting or blocking response.

Nalorphine (n-allylnormorphine)

A morphine derivative designed to displace morphine from the miu receptor; it lacks intrinsic activity and serves as an antidote for morphine.

Easson-Stedman Model

A model demonstrating drug chirality where an active drug-receptor complex requires at least three correct binding interactions between defined points on the drug ($A, B, C$) and corresponding points on the receptor ($a, b, c$).

Chiral Carbon

A central carbon atom attached to four different substituents, giving rise to optical isomers or enantiomers.

Chiral Resolution

The process of separating enantiomers in order to isolate and formulate the desired active isomer.

S-Ibuprofen

The more potent enantiomer of ibuprofen that acts as an anti-inflammatory and analgesic agent.

Quinidine

An antiarrhythmic stereoisomer of the antimalarial compound quinine that differs in its hydrogen and oxygen spatial arrangement.

Cisplatin

The active isomer used as an anticancer drug, in contrast to its inactive isomer, transplatin.

R-Thalidomide

The enantiomer of thalidomide that functions as an antiemetic for pregnant women.

S-Thalidomide

The teratogenic enantiomer of thalidomide that causes phocomelia (birth defects leading to limbless infants).

Codeine

A methylated morphine derivative used as an antitussive that is more soluble than morphine and precipitates in $NaOH$ solution.

Heroin

An illicit recreational opioid produced by the acetylation of morphine.

Apomorphine

A central emetic and dopaminergic agonist produced through the dehydration of morphine.

Drug Discovery

The initial stage of pharmaceutical research lasting about 3 to 6 years, involving lead identification, in silico studies, in vitro assays, and initial animal studies.

Drug Development

The stage of bringing a drug to market lasting roughly 12 to 21 years, encompassing preformulation, preclinical ADME/toxicity testing, clinical trials (Phases I-III), and regulatory review.

Pharmacovigilance (PV)

The post-marketing process of ongoing monitoring and evaluation of side effects and adverse drug reactions in broad patient populations.

Erythromycin (Ilosone)

An antibiotic isolated from Streptomyces erytheus, a member of the actinomycetes family discovered in Iloilo.

Ephedrine

A nasal decongestant isolated from the plant Ephedra (Ephedra sinica).

Digoxin

A cardiac glycoside derived from Digitalis (Digitalis lanata) used to treat congestive heart failure (CHF).