Introduction to Pharmacology

Introduction to Pharmacology

• Pharmacology is the science of medicines, focusing on interactions between substances and living organisms at all levels.
• Pharmakon (φάρμακον) is a Greek word meaning medicine, poison, or active principle (later drug).
• Logos (Λόγος) is a Greek word meaning reason, speech, word, or science.
• Pharmacology focuses on the effective and safe use of drugs for medicinal purposes.

Pharmacology vs. Pharmacy

• Pharmacy is a medical field dealing with drug research, production, distribution, storage, control, and dispensing, including patient advice.
• Pharmaceutical sciences include pharmacology, pharmacognosy, pharmaceutical chemistry, drug control and analysis, pharmaceutical technology, social and clinical pharmacy, and pharmaceutical practice.
• A pharmacist is a professional in the field of pharmacy.

Content of Pharmacology

• Pharmacology encompasses general and special branches

General Pharmacology

• Studies the universally valid laws of substance and organism interactions
• Includes pharmacodynamics and pharmacokinetics

Special Pharmacology

• Focuses on specific drug groups and individual substances
• Examples include neuro-pharmacology, cardiovascular pharmacology, gastrointestinal pharmacology, and immuno-pharmacology

General Pharmacology: Pharmacodynamics

• Explores what the drug does to the body
• Drug-receptor complex and signal transduction are key concepts.
• Insight into the drug’s effects at the macro level, indications, contraindications, and side effects is gained.

General Pharmacology: Pharmacokinetics

• Examines what the body does to a drug
• ADME (Absorption, Distribution, Metabolism, Excretion) is a central concept.
• Optimal drug regimens, including administration route, dosage form, dose, frequency, and treatment duration, are determined.

Other Disciplines of Pharmacology

• Pharmacogenetics studies genetic influences on drug responses.
• Pharmacogenomics uses genetic information to guide drug therapy on an individual basis, known as personalized medicine, where individual responses to drugs are predicted from their genetic makeup.
• Pharmacoeconomics is a branch of health economics quantifying the costs and benefits of drugs in economic terms, identifying the "health gap."
• Toxicology studies the poisonous effects of drugs and other chemicals and emphasizes detection, prevention, and treatment of poisonings.
• Clinical pharmacology focuses on clinical trials, therapeutic drug monitoring, rational drug usage, and applying pharmacological principles in real-world settings.
• Pharmacovigilance involves the science and activities relating to the detection, assessment, understanding, and prevention of adverse drug effects or other drug-related problems.
• Pharmacoepidemiology studies drug effects at the population level, focusing on variability of drug effects among individuals and populations.
• Regulatory authorities use pharmacoepidemiology to decide whether to license new drugs for therapeutic use.

Nomenclature of Drugs

• Drugs can be identified by several names
• Drugs have three different names: chemical name, international non-proprietary name (INN), and proprietary name

Drug Names: Chemical Name

• Assigned when a new chemical entity (NCE) is developed.
• Follows chemical nomenclature rules established by the International Union of Pure and Applied Chemistry (IUPAC).
• Provides the precise arrangement of atoms and atomic groups in the molecule for chemists or technical personnel.
• This name is not used in clinical or marketing settings

Drug Names: International Non-Proprietary Name (INN)

• A short name for a drug not subject to proprietary rights.
• INNs should be concise and meaningful.
• Used in discussions and textbooks
• INNs can be either Approved Name or Official Name

Drug Names: Approved Name

• Given to a drug by bodies like the United States Adopted Name Council (USAN) and British Approved Name (BAN) soon after its introduction.
• Sometimes called a generic name, designating a chemical or pharmacological class of drugs (e.g., Sulphonamide, Penicillin).

Drug Names: Official Name

• The National Pharmacopeia Commission approves a drug's official name.
• It is included in the official book, i.e., Pharmacopeia.
• It must be identical with the approved name

Drug Names: Proprietary Name

• Given to a drug by the pharmaceutical company that sells it, also known as the brand/trade name.
• A single drug can be sold under multiple proprietary names by different firms.
• Written with a capital initial letter, often with a superscript R in a circle (®).
• Clinicians commonly use proprietary names to describe drugs

Drug Name Example: Paracetamol

• Chemical Name: N-(4-hydroxyphenyl)acetamide
• International Non-Proprietary Name:
  • British Approved Name (BAN): paracetamol
  • United States Adopted Name (USAN): acetaminophen
• Official Name: Acetaminophen
• Proprietary Names: Panadol, Calpol, Adol, Tylenol

Drug Name Examples (INN, Chemical, Brand)

• Nimesulide
  • Chem Name: 4'-nitro-2'-phenoxymethansulphoanilid
  • Brand Names: Aulin, Mesulid, Nimed
• Ibuprofen
  • Chem Name: 2-(4-isobutylfenyl)propionic acid
  • Brand Names: Ibalgin, Brufen, Motrin, Nurofen, Apsifen, Fenbid, Ebufac, Ibular, Lidifen, Paxofen, Dolgit, Pabiprofen, Solpaflex
• Diazepam
  • Chem Name: 7-chloro-1,3-dihydro-1-methyl-5-fenyl-2H-1,4-benzodiazepin-2-on
  • Brand Names: Apaurin, Seduxen, Valium, Vival, Alupram, Atensine, Diazemuls, Evacalm, Solis, Stesolid, Tensium, Valrelease

Common INN Prefixes and Suffixes

• Cef- : Cephalosporins (antibiotics)
• Pam- : Benzodiazepines
• Lam- : Benzodiazepines
• Olol- : Betablockers
• Pril- : ACEI
• Sartan- : ARB
• Vastatin- : HMG CoA reductase inhibitors (statins)
• Dipine- : Calcium channel blockers
• Profen- : NSAIDS (anti-inflammatory)
• Mab- : Monoclonal antibodies
• Triptan- : Antimigraine (triptans)
• Xaban : Anticoagulatns (xabans)

Classification of Drugs

• Essential to reduce thousands of drugs into manageable groups
• No uniform or homogenous system of classification exists.
• Drugs are classified based on the convenience of the person discussing them (chemist, pharmacologist, pharmacist, clinician).

Drug Classification: Bases

Drugs are classified based on

• Chemical Nature
• Source
• Target organ/Site of Action
• Mode of Action
• Therapeutic Uses
• Physiological system
• Physical Effects

Drug Classification: Chemical Nature

• Inorganic drugs include metals, their salts (Ferrous Sulphate, Zinc Sulphate, Magnesium Sulphate), and non-metals like Sulphur.
• Organic drugs include alkaloids (atropine, morphine, strychnine), glycosides (digitoxin, digoxin), proteins (insulin, oxytocin), esters, amide, alcohol, and glycerides.

Drug Classification: Source

• Natural sources include plants (morphine, atropine, digitoxin), animals (insulin), micro-organisms (penicillin), and minerals (sodium chloride).
• Synthetic sources include, (Sulphonamide, Procaine).
• Semi-synthetic sources include amoxicillin, ampicillin, and doxycycline.

Drug Classification: Target Organ

• CNS: Diazepam, Phenobarbital
• Respiratory System: Salbutamole
• Cardiovascular System: Digitoxin, Digoxin
• GIT: Omeprazole
• Urinary System: Mannitol, Spironolactone
• Reproductive System: Oxytocin, Estrogen

Drug Classification: Mode of Action

• Inhibitor of bacterial cell wall synthesis (penicillin)
• Inhibitor of bacterial protein synthesis (tetracycline)
• Calcium Channel blocker (verapamil, nifedipine)

Drug Classification: Therapeutic Use

• Antimicrobials/Antibacterials: Penicillin, Streptomycin, Quinolones, Macrolides
• Antihypertensive: Clonidine, hydralazine, Enalpril
• Antidiarrheals: Lopramide, Kaoline
• Antiemetics: Domperidone, Meclizine and Metoclopramide
• Physicians & Pharmacologists typically perform classification based on mode of action

Drug Classification: Physiological System

• Sympathomimetics: Adrenaline, Noradrenaline
• Parasympathomimetics: Carbachol, Pilocarpine, Neostigmine
• Neuromuscular blockers: Suxamethonium, Gallamine

Drug Classification: Physical Effects

• Emollients: Lanolin, Vaseline
• Caustics: Silver nitrate
• Demulcents: Zinc Oxide, Tannic Acid

ATC Classification of Drugs

• The Anatomical-Therapeutic-Chemical (ATC) classification system is designed for PC data processing
• It is international
• Drugs are classified into groups, including anatomical, therapeutic, and chemical subgroups

Anatomical Therapeutic Chemical (ATC) Codes

• The first level is anatomical, indicated by a letter
• The second level is the main therapeutic group, indicated by a two-digit number
• The third level is the therapeutic subgroup, indicated by a letter

AISLP

• The Automated Information System of Medicinal Products (AISLP)
• AISLP is always up to date
• AISLP contains information on SPC, package leaflets (PIL), composition, method of issue, prices and payments, and prescription and indication restrictions available for each MP

Act No. 378/2007 Coll.

• Act on Pharmaceuticals sets conditions for research, manufacturing, preparation, distribution, control, and disposal of medicinal products and active substances.
• Act No. 378/2007 Coll. also addresses registration, post-authorization monitoring, prescription, supply and sale of products, and international cooperation for public health protection.

Basic Terms: Active Substance (AS)

• Any substance or mixture intended for use in manufacturing a medicinal product
• After manufacturing, the active substance functions to exert a pharmacological, immunological, or metabolic action for the purpose of restoring, correcting, or modifying physiological functions or for medical diagnosis.

Original vs. Generic Drugs

• Original medicine (reference drug) includes active substances and "know-how" that are patented, and is the first authorized medicine with a specific active substance.
• Generic drug contains the same quantity of the same active drug as the original product drug with the same dosage and biological activity, but may differ in the type and ratio of excipients used.

Basic Terms: Excipient

• Any component of a medicinal product that is not an active substance or packaging material.
• Basic excipients include fillers, binders, sliding substances, loosening agents, dyes, solvents, antimicrobials, and taste and smell correctors.

Basic Terms: Medicinal Product (MP)

• Substance or combination presented as having therapeutic or preventive properties for human or animal diseases.
• Can be used or administered to humans or animals to restore, correct, or modify physiological functions through pharmacological, immunological, or metabolic action, or for medical diagnosis.
• Active substance, a mixture of active substances, or a medicinal product intended for administration to humans or animals

Medicinal Preparation

• Medicinal preparations are the most strictly regulated
• They have control and surveillance before market entry
• And have the most expensive fees
• Medicinal preparations treat human diseases and have strict advertising regulations

Types of Medicinal Products

• Humane
• Veterinary
• Homeopathy
• Radiopharmaceuticals
• Transfusion products
• Blood derivatives
• Vegetable preparations

Classification of Medicinal Products: Method of Production

• RMP (Industrially Produced)
  • Produced in larger volumes in batches outside medical facilities
  • Subject to registration with SÚKL(State Institute for Drug Control) or EMA(European Medicines Agency)
  • Can include products not registered in the Czech Republic
  • Can be part of specific treatment programmes
• IPP: extemporaneously prepared (prepared in a pharmacy according to an individual doctor's prescription)

Medicinal Products: According to Supply

• Prescription only
  • Issued by a pharmacist only against a doctor's prescription
  • OTC (over the counter)
    • Dispensed without a prescription where pharmaceutical care is available
  • OTC with restrictions
    • With limited quantity/strength packages, and identity card to be handled by a pharmacist.
    • MP containing pseudoephedrine
  • Reserved
    • Sold also outside the pharmacies (teas, disinfectants, medicines for the treatment of mild pain)

Product Info: SPC & PIL

• A summary of product characteristics (SPC) provides a written summary, is part of the marketing authorization, essential for proper use, and serves as an obligatory public document.
• A patient information letter (PIL) contains information for users and is part of a medicinal product (package leaflet).

Specific Use of Medicinal Products

• Use of Unregistered MP
  • Can be used if there's no adequate medicinal product that works
  • Should be authorized abroad
  • This method should be scientifically proven
  • The product cannot contain GMO
  • The patient should be aware of the treatment
  • Use of Non-registered MP
    • Can use if there treatment is specified by the Ministry Of Health, SZU and SUKL.
    • Public health insurance covers some
    • Must be reported to SUKL
  • Off Label
    • When a drug is used when not specified on SPC
    • If there is any application outside of indications
    • If a different dose or route of application is required by a patient
    • Must be legal

Rules for Drug Promotion

• Limited to only OTC products
• Includes information which must follow SPC regulations
• No drug product should
  • Be deceptive
  • Use motive of fear
  • Have a description of an erroneous diagnostic
  • Negatively be guaranteed if they affect health
  • Be implied as any other product that food or cosmetic
  • Specifically target under 15’s
  • Recommend from any non official authorities
  • Compare

Dietary Supplement

• A food that supplements food
• Contains minerals and or other nutrients
• Intended for direct consumption Is regulated by Decree No. 58/2018 Coll Has mild regulations Must include description of “dietary supplements” CANNOT claim to CURE HUMAN DISEASE

Pharmacopoeia

• It’s derived from the Green words pharmakon (drug), and poieo (prepare).
• Consists of aggregated data about medicinal substances and other compounds as well as any other information on the methods.

Key points Pharmacopoeia

• officinal drugs are substances used in pharmacopoeia and pharmacopoeial
• Non officinal drugs: Other medicines are not mentioned in pharmacopoeia
• Obsolete drugs: Are medicinal preparations that where already deleted from the current Pharmacopoeia
• May prescribe as justified
• Classify as drug.

European Pharmacopoeia (Ph. Eur)

• Serves as a single reference work for the best control of medicine
• Serves as the official standard document
• Standards are legally binding
• Every three years there is a new edition

European Pharmacopoeia Legal Framework

Several sections make it the European Pharmacopoeia law

• Developed by the Council of Europe on the Elaboration of European Pharmacopoeia
• A Protocol was adopted in 1994, and the convention prepare for the EU
• European Directives maintain the European Pharmacopedia monographs

European Pharmacopoeia Missions

• Promote public health
• Provide good quality medicine standards And facilitate movement of medicine

Eur. Pharm (Benefits)

• It’s legally binding in 39 countries on the EU, applicable to 120 + countries
• Provides new and revised test
• Delivers crucial markets
• Currently on 11th edition

S Eur. Pharm Volume 1-2

Volume one has 52 pages of the eighth edition Volume two page index is 3600

Regulatory Authorities

• The European Medicines Agency (EMA) - EU
• The Food and Drug Administration (FDA) - USA
• State Institute for Drug Control (SÚKL) – CR

European Medicines Agency (EMA)

• A European agency that evaluates product
• Is parallel to the U.S Food and Drug agencies
• The agency consists of committees for humans; veterinary, herbal, orphan drugs and advanced therapies
• Their responsibility is the protection and safety to the public through animal and human medicine

Food and Drug Administration (FDA)

• A U.S agency for the department of health
• Responsible to control drug to food and cosmetic and regulate the device of medicine in the U.S
• The website below has available information

State Institute for Drug Control (SUKL)

• Agency in the Czech Republic
• Pricing is implemented that the agencies
• MP registrations are kept at the agencies
• Monitoring implement drug control through information from websites.