INTRODUCTION TO PHARMACOLOGY 1

What is Pharmacology?

The study of drugs and their effects on living organisms.

What do pharmacologists study?

Drug absorption, distribution, metabolism, excretion, and interactions.

What is medical pharmacology?

The science of substances used to prevent, diagnose, and treat disease.

What is the primary method by which drugs affect biological systems?

By binding to regulatory molecules and activating or inhibiting processes.

What does toxicology study?

The harmful effects of drugs on living organisms.

Where does pharmacology originate from?

Ancient civilizations like Mesopotamians, Egyptians, Chinese, and Greeks.

What is Paracelsus known for?

Introducing the concept "The dose makes the poison."

Who is the father of modern pharmacology?

Oswald Schmiedeberg.

When was the first pharmacology lab established?

In 1846 by Rudolf Buchheim at the University of Dorpat.

Name one key 20th-century drug milestone.

Discovery of penicillin by Alexander Fleming in 1928.

What is the general principle regarding drug toxicity?

All substances can be toxic under certain conditions.

How do botanical chemicals compare to synthetic drugs?

They are chemically similar but often contain more impurities.

What is a drug?

A chemical substance (not a nutrient) that produces a biological effect when administered.

What is a medicine?

A preparation containing one or more drugs aimed at therapeutic effect.

What are excipients?

Inactive substances in a drug formulation like solvents or stabilizers.

What is a receptor in pharmacology?

A regulatory molecule that a drug binds to as an agonist or antagonist.

What are chemical antagonists?

Drugs that interact directly with other drugs.

What are osmotic agents?

Drugs that interact primarily with water molecules.

What are xenobiotics?

Foreign chemicals not synthesized in the body.

How do toxins differ from poisons?

Toxins are of biological origin; poisons may be inorganic.

What determines drug interaction with receptors?

Size, charge, shape, and atomic composition.

Why must drugs be transportable?

Because they’re usually administered at a different site than their target.

What physical forms can drugs take at room temperature?

Solid, liquid, or gaseous.

What compound classes do drugs belong to?

Carbohydrates, proteins, lipids, and small organic molecules.

What is an ideal property of a drug?

It should be inactivated or excreted at a suitable rate.

What is the usual molecular weight range for drugs?

Between 100 and 1000 daltons.

Why must drugs be a certain size?

To ensure specificity in binding to a unique receptor.

What is the role of drug charge and shape?

To prevent nonspecific binding and allow selective receptor interaction.

What does specificity of action refer to?

A drug’s ability to affect only its intended receptor or pathway.

What example is given for a very large drug?

Alteplase (t-PA), MW 59,050.

What types of bonds exist between drugs and receptors?

Covalent, electrostatic, and hydrophobic bonds.

Which bond type is strongest?

Covalent bonds.

Which bond type is most common in drug-receptor interaction?

Electrostatic (e.g., hydrogen bonds, van der Waals).

What do weak bonds indicate about a drug?

High selectivity due to the need for a precise receptor fit.

Why are hydrophobic bonds important?

They help lipid-soluble drugs interact with cell membranes.

How does drug shape affect binding?

Shape must be complementary to the receptor site.

What is chirality in pharmacology?

The property of having non-superimposable mirror images (enantiomers).

How many diastereomers exist for a drug with two asymmetric centers?

Four.

What’s the usual difference between drug enantiomers?

One is typically more potent due to better receptor fit.

What is a racemic mixture?

A drug mixture containing both enantiomers.

What is rational drug design?

Predicting drug structure based on receptor structure.

What helped improve drug design in recent decades?

Characterization of receptor 3D structures.

What tool aids in rational drug design?

Computer-based modeling and simulations.

What is the benefit of molecular modeling?

It enables targeted drug development instead of random screening.

What is an example of iterative optimization?

Refining a known drug to enhance its fit and effectiveness.

What is the primary goal of pharmacology in drug development?

To understand and optimize drug effects on the body.

What happens during drug discovery?

Pharmacologists identify and test potential therapeutic compounds.

What is preclinical testing?

Testing drug safety and efficacy in animals.

What are excipients used for?

To aid in drug formulation and administration.

Why are pharmacokinetics and pharmacodynamics important?

They determine how the drug acts and how the body processes it.

What is the role of pharmacology in the drug industry?

It helps in understanding how drugs work, interact with the body, and how they treat or prevent disease.

What are the key stages of drug development?

Drug discovery, preclinical testing, clinical trials, and regulatory approval.

What happens during drug discovery?

Pharmacologists identify potential drug candidates using screening and modeling.

What is preclinical testing?

Testing of drug compounds in animals to assess safety and efficacy.

Why is pharmacology important in regulatory approval?

It provides scientific evidence of safety, mechanism, and effectiveness needed by authorities.

What is the first step in drug discovery?

Target identification.

What is hit-to-lead optimization?

Refining initial compounds to improve potency and drug-like properties.

What does lead validation involve?

Demonstrating biological activity of a compound in disease models.

Give an example of hit optimization in cancer therapy.

Improving a tyrosine kinase inhibitor by enhancing potency and stability.

What is high-throughput screening?

Testing thousands of compounds rapidly to find active ones.

What does mechanism of action research focus on?

How a drug works at molecular and cellular levels.

What are binding studies used for?

Determining drug-receptor affinity and kinetics.

What is SAR analysis?

Relating chemical structure to biological activity.

What does propranolol block?

β1- and β2-adrenergic receptors.

How does propranolol reduce heart rate?

By decreasing cyclic AMP levels in heart cells.

What is assessed in safety and toxicity studies?

Cytotoxicity, genotoxicity, lethal doses, and long-term effects.

What is NOAEL?

No Observed Adverse Effect Level.

What is LD₅₀?

Dose lethal to 50% of animals tested.

What caused thalidomide’s historical tragedy?

Inadequate species-specific teratogenic testing.

What is the purpose of drug–drug interaction studies?

To predict harmful metabolic effects when drugs are combined.

What does pharmacokinetics study?

How drugs are absorbed, distributed, metabolized, and excreted.

What does pharmacodynamics study?

How drug concentration affects the body.

What are key PK parameters?

Half-life, AUC, clearance, and volume of distribution.

What does PK/PD modeling help with?

Predicting optimal dosing regimens.

What influences warfarin dosing?

Genetic polymorphisms (CYP2C9, VKORC1) and PK/PD variables.

What is drug optimization?

Improving drug properties like potency, selectivity, and bioavailability.

What is a prodrug?

An inactive compound that is metabolized into an active drug.

Why is lipophilicity important?

It affects drug absorption and cell membrane penetration.

What is SAR used for in drug design?

To guide chemical modifications for better effects.

What role does ritonavir play?

Inhibits CYP3A4 to enhance plasma levels of other HIV drugs.

What does regulatory compliance involve?

Meeting standards set by FDA, EMA, NAFDAC, etc.

What is an IND application?

A submission for approval to begin human clinical trials.

What is a REMS?

A strategy to manage serious drug risks post-approval.

What is pharmacovigilance?

Monitoring drug safety after approval.

What is the NDA process?

A full regulatory submission to market a new drug.

What is personalized medicine?

Tailoring drug treatment based on individual genetic makeup.

What is pharmacogenomics?

Studying how genes affect drug metabolism and response.

What is TDM?

Therapeutic Drug Monitoring — adjusting doses based on blood levels.

What are companion diagnostics?

Tests used to determine patient eligibility for specific drugs.

How is trastuzumab therapy guided?

By HER2 testing (IHC or FISH) to ensure HER2 overexpression.

What is the focus of pharmacology in research?

Exploring new drug modalities, delivery systems, and repurposing.

What are antibody–drug conjugates?

Targeted drugs that deliver toxins directly to cancer cells.

What is an example of repurposed drug research?

Using metformin for potential cancer treatment.

How did mRNA vaccines succeed?

Due to lipid nanoparticles enabling mRNA delivery.

What is an example of cross-disciplinary innovation?

Immunologists and pharmacologists developing vaccine adjuvants.

What is the pharmacologist’s role in clinical trials?

Designing studies, selecting doses, and interpreting PK/PD data.

What is Phase I focused on?

Safety and PK/PD in healthy volunteers.

What happens in Phase II trials?

Assessing efficacy and safety in a patient group.

What is the purpose of Phase III trials?

Large-scale comparisons with standard care for regulatory submission.