Pharmacology I - Introduction
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What is the definition of pharmacology, as stated in Goodman & Gilman's The Pharmacological Basis of Therapeutics?

The subject of pharmacology is a broad one and embraces the knowledge of the source, physical and chemical properties, compounding, physiological actions, absorption, fate, and excretion, and therapeutic uses of drugs.

The word "pharmacology" is derived from the Greek words "pharmakon" and "logos", meaning "active principle" and "a discourse or treatise", respectively.

True

What is the primary focus of pharmacodynamics?

Pharmacodynamics examines the relationship between drug concentrations in the blood and the desired and adverse effects it produces in the body.

What are the key areas of study within pharmacokinetics?

<p>Pharmacokinetics focuses on the time course of absorption, distribution, metabolism, and excretion (ADME) of a drug within the body, considering its behavior as a function of time.</p> Signup and view all the answers

What are the four main disciplines that pharmacology links together?

<p>Chemistry, Biochemistry, Physiology, Pathology</p> Signup and view all the answers

What is the definition of a drug?

<p>A drug is the active chemical entity present in a prescribed medicine, used for diagnosis, prevention, treatment, or cure of a disease.</p> Signup and view all the answers

What are the common sources for drugs?

<p>Drugs can be derived from natural sources (plants, animals, microbiota, minerals), semi-synthetic sources (modified natural compounds), or synthetic sources (exclusively laboratory-produced).</p> Signup and view all the answers

The term "drug" is derived from the French word "drogue", meaning "dried herb".

<p>True</p> Signup and view all the answers

Which of the following names refers to the drug's chemical nature?

<p>A</p> Signup and view all the answers

What is the purpose of the International Non-proprietary Name (rINN)?

<p>The rINN, adopted by WHO member nations, aims to standardize the generic name of a drug, ensuring a single, unambiguous name across different countries.</p> Signup and view all the answers

What is a proprietary or brand name of a drug?

<p>A proprietary or brand name is a name owned and designated by the manufacturer, used to market the drug under a unique and identifiable label.</p> Signup and view all the answers

Most drugs before the advent of recombinant DNA technology were primarily small organic molecules, typically smaller than 500 Da.

<p>True</p> Signup and view all the answers

What was the defining event that led to the passage of the Federal Food, Drug, and Cosmetic Act in 1938 in the US?

<p>The tragic death of over 100 individuals in the US due to the use of sulfanilamide elixir, contaminated with diethylene glycol as a solvent, prompted the enactment of the Food, Drug, and Cosmetic Act in 1938.</p> Signup and view all the answers

What was the major adverse effect of thalidomide, which led to stricter drug control in the 1960s?

<p>Thalidomide, initially marketed for morning sickness, caused phocomelia, a severe birth defect characterized by deformed or shortened limbs in thousands of babies.</p> Signup and view all the answers

What is the key requirement introduced by the Kefauver-Harris Amendment of 1962?

<p>The Kefauver-Harris Amendment mandated that drug manufacturers provide proof of their drug's effectiveness and safety before seeking approval for marketing.</p> Signup and view all the answers

Which of the following is NOT a stage of drug development?

<p>Manufacturing and Distribution</p> Signup and view all the answers

On average, developing and gaining approval for a new medicine can take at least 10 years and costs over 2.5 billion US dollars.

<p>True</p> Signup and view all the answers

Less than 10% of drug candidates that reach Phase I clinical trials are ultimately approved by regulatory bodies like the FDA.

<p>True</p> Signup and view all the answers

What is a generic drug product?

<p>A generic drug product is comparable to an innovator drug product in terms of dosage form strength, route of administration, quality, performance, and intended use.</p> Signup and view all the answers

What is a bioequivalence study, and what is its purpose?

<p>A bioequivalence study compares the bioavailability of a generic drug to its innovator counterpart, ensuring that both drugs reach the bloodstream and produce the same therapeutic effect. It is conducted to establish that the generic drug is equivalent to its innovator counterpart in terms of its therapeutic effect.</p> Signup and view all the answers

Study Notes

Pharmacology I - Introduction

  • Course instructor: Roger K. Verbeeck, Ph.D. and D.F Chuma
  • Institution: UNAM (School of Pharmacy)
  • Contact: [email protected]

Contents

  • Definitions
  • History of pharmacology
  • Development of a new drug

Pharmacology

  • Broad subject encompassing the source, physical and chemical properties, compounding, physiological actions, absorption, fate, excretion, and therapeutic uses of drugs. (Goodman & Gilman The Pharmacological Basis of Therapeutics, 1st edition, 1941)
  • Studies how drugs work (pharmacodynamics) and their processing by the body (pharmacokinetics).
  • Crucial for: discovering new drugs, improving drug effectiveness, reducing side effects, and understanding patient response differences.

What is a Drug?

  • Active chemical entity in a prescribed medicine
  • Used for diagnosis, prevention, treatment, or curing a disease.
  • Derived from the French word "drogue," meaning "dried herb".
  • WHO defined it as any substance or product used or intended to modify or explore physiological systems or pathological states for recipient benefit (1966)

Nomenclature of Drugs

  • Every drug has three names:
    • Chemical name: Describes the drug's chemical nature (e.g., (RS)-2-(4-(-2-methylpropyl) phenyl) propanoic acid (Ibuprofen))
    • Non-proprietary/Generic name: Authoritatively accepted by a scientific body. All WHO member nations use a single recommended International Non-proprietary Name (rINN). (e.g., Ibuprofen)
    • Proprietary/Brand name: Owned and designated by the manufacturer (e.g., Brufen®, Combiflam®, Unafen®, Advil®, etc.)

Pharmacodynamics and Pharmacokinetics

  • Pharmacodynamics: Relationship between drug's blood concentration, and desired/adverse (toxic) effects in the body.
  • Pharmacokinetics: Time course of drug absorption, distribution, metabolism, and excretion (ADME) as a function of time.

History of Pharmacology

  • Started mid-19th century with increasing knowledge of normal/abnormal body function.
  • First department of pharmacology established in Dorpat (Estonia) in 1847.
  • Oswald Schmiedeberg (1838-1921), a student of Rudolph Buchheim, is considered the founder of modern pharmacology.
  • Concept of receptors proposed by John Newport Langley (1852-1925) in 1905.
    • Paul Ehrlich (1854-1915) further refined this concept in 1907.
  • Key discoveries: Penicillin (1928), Sulfonamides (1935), etc.
  • 20th century saw major developments in drug classes.
  • History timeline includes discoveries and developments from ancient times (e.g., Sumeria, 2000 BC - aspirin).
  • Including morphine discovery and synthesis dates.

Sources of Drugs

  • Natural Sources: Plants, Animals, Microbiota, Minerals
  • Key examples of plant-derived drugs include:
    • Leaves: Digoxin, digitoxin, atropine
    • Flowers: Vincristine, vinblastine
    • Fruits: Physostigmine
    • Seeds: Strychnine, morphine
    • Roots: Emetine, reserpine
    • Bark: Quinine, atropine
    • Stem: Tubocurarine
  • Animal Sources: Whole animals (leeches, etc.), organs (cod liver oil, insulin), glandular products (vaccines, sera).
  • Microbiota Sources: Penicillin, chloramphenicol, streptomycin
  • Mineral Sources: Ferrous sulfate, magnesium sulfate, potassium iodide, iodine, radioisotopes of iodine and other minerals.
  • Semi-synthetic Sources: Alteration of the chemical structure of a natural drug (e.g., homatropine, heroin, ampicillin).
  • Synthetic Sources: Chemical synthesis; altered structure, not naturally occurring (pure chemicals, better cost-effectiveness, improved safety).

Drug Development

  • Historical: Discovering active ingredients in traditional remedies or through accidental discoveries.
  • More recently: High-throughput screening and rational drug design (targeting receptors and biological processes).
  • Computer-aided drug design: Predicting whether a molecule binds to a target.
  • Small organic molecules: Primary drug type until recent advancements in DNA technology.
  • Recombinant DNA technology: Enables the synthesis of proteins by various organisms, including biopharmaceuticals like human insulin.
  • Regulatory aspects:
    • 1937: Sulfanilamide elixir disaster leads to the Federal Food, Drug, and Cosmetic Act (FD&C Act) of 1938.
    • 1956: Thalidomide disaster leads to more structured drug regulations (Kefauver-Harris Amendment).
  • Clinical development: Preclinical (physicochemical, cell cultures), clinical trials (Phase I, II, III, IV) and regulatory review for marketing authorisation.
  • Post marketing Surveillance: Pharmacovigilance to monitor the safety and efficacy of drugs after approval.

Drug Development (Regulatory Aspects)

  • Price considerations: Patient prices, wholesale prices.
  • Specific examples: Omeprazole, Eculizumab.

Bioequivalence Study

  • Comparing generic and reference drug formulations (using Acyclovir as an example) - similar blood concentration profiles.

Principles and Modes of Drug Administration

  • Principles: "Do No Harm" as primary, with five rights (patient, drug, dose, time, route).
  • Modes (Routes): Oral, sublingual, rectal, application to mucous membranes, inhalation, injection (various types).

Preparations of Drugs and Dosage Forms

  • Dosage Forms: Tablet, capsule, caplet, syrup, cream, ointment, lotion, liniment, gel/jelly, paste, lozenge, troche, solution (aqueous/suspension), aerosol, elixir, extract, powder, suppository; tincture, transdermal patch.

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This quiz covers the foundational concepts of pharmacology, including definitions, historical context, and the drug development process. Explore essential pharmacological principles, such as pharmacodynamics and pharmacokinetics, which are vital for understanding drug interactions and therapeutic applications.

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