Lecture Notes Review: Drug Development and Prodrug Concepts

These flashcards cover key concepts related to drug development, prodrugs, pharmacology, and therapeutic strategies discussed in the lecture.

Aqueous Solubility

The ability of a drug to dissolve in water to facilitate injection in small volumes.

Absorption and Distribution

The processes to improve drug absorption and bio-distribution in the body.

Site Specificity

Targeting a drug to a specific organ or tissue to minimize toxicity.

Instability

The tendency of a drug to undergo rapid metabolism or elimination, necessitating modification.

Prolonged Release

A drug formulation that allows for a gradual and steady release of the drug.

Poor Patient Acceptability

Unpleasant properties of a drug, like taste or odor, that hinder patient compliance.

Conversion of Gas to Solid

The formulation challenge of changing a gaseous or volatile drug into a solid form for administration.

Imine

A functional group containing a carbon-nitrogen double bond; prodrugs can be structured as imines.

LDOPA

A prodrug of dopamine that facilitates its transport across cell membranes.

Mitomycin C Activation

The process where reduction activates the prodrug Mitomycin C, facilitating its therapeutic effects.

Prodrug of Prodrug

A compound converted into another prodrug before being activated into the active drug form.

Sentry Drugs

Drugs that protect other drugs from undesired enzymatic action.

Auxiliary Drugs

Drugs that enhance the action of a primary drug, such as MAO inhibitors protecting dopamine.

Azathioprine

A prodrug that provides a sustained effect of its active form, 6-mercaptopurine, on the immune system.

Preventing Hydrolysis

Strategies like creating sterically hindered esters to make drugs more resistant to hydrolysis.

Salicylic Acid Usage

A painkiller replaced by aspirin to avoid gastric bleeding caused by its phenolic -OH group.

Lysine Ester of Oestrone

Improves oral bioavailability and solubility of oestrone compared to its parent compound.

Photodynamic Therapy

Utilizes light-activated agents like Foscan to target and destroy cancerous cells.

Unstable Ampicillin

Ampicillin's instability is due to its chemical structure, which can be modified by creating derivatives like Hetacillin.

Taste Masking of Clindamycin

Clindamycin palmitate is introduced to mask the bitter taste associated with the drug.

Controlling Drug Metabolism

Techniques like removing functional groups that are metabolized rapidly to prolong drug action.

L-lysozyme Example

Illustrates how a drug can be converted into a prodrug to reduce toxicity until it reaches the target site.

Enzyme-Prodrug Therapy

A strategy using enzymes to convert a prodrug into an active drug form selectively.

ADEPT

Antibody-directed enzyme prodrug therapy; targets drugs specifically to diseased cells.

Abzyme

An artificial antibody that catalyzes specific reactions, potentially in prodrug activation.

GDEPT and VDEPT

Gene-Directed and Virus-Directed Enzyme Prodrug Therapy; approaches for targeted cancer treatment.

Hard Drugs

Drugs with essential structural characteristics for activity but are less susceptible to metabolism.

Soft Drugs

Drugs designed to be active but are safely inactivated into non-toxic products.

Pharmacokinetics (PK)

The study of how the body affects a drug over time, including absorption, distribution, metabolism, and excretion.

Pharmacodynamics (PD)

The study of the effects and mechanisms of action of a drug on the body.

Drug Distribution Parameters

Factors affecting drug distribution include protein binding, disease state, and cardiac output.