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ASSIGNMENT

General u WHAT IS THE CONNECTION BETWEEN PHARMACOLOGY AND MEDICAL

TECHNOLOGY?
Principle of u HOW CAN LABORATORY RESULTS IMPROVE TREATMENT OUTCOMES?

Pharmacology u HOW CAN LABORATORY RESULTS EVALUATE THE EFFECTS OF DRUGS?

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OBJECTIVES
Pharmacology – a study of a substances that interact with
living systems through chemical processes, especially by
u DEFINE IMPORTANT TERMS ASSOCIATED IN PHARMACOLOGY binding to regulatory molecules and activating or inhibiting
u DISCUSS THE HISTORY OF PHARMACOLOGY, ITS CONCEPT ON THE NATURE OF normal body processes.
DRUGS AND ITS PHYSICAL AND CHEMICAL PROPERTIES
u APPRECIATE THE IMPORTANCE OF PHARMACOLOGY IN MEDICAL TECHNOLOGY Introduction Medical Pharmacology – a science of substances used to
prevent, diagnose, and treat diseases.

Toxicology – a branch of pharmacology that deals with the

undesirable effects of chemicals on living systems, form
individual cells to humans to complex ecosystem.

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Areas of the study History of Pharmacology

of Pharmacology u Materia medica (17 th century)– the science of drug
preparation and the medical use of the drug.

Pharmacokinetics – deals with ADME u Experimental physiology and pharmacology (18 th to

early 19 th century) – Francois Magendie and his
(Absorption, Distribution,
student Claude Bernard – develop the method.
Metabolism, & Excretion) of the
chemical/drug. u Controlled clinical trials was introduced at the same
time because of too many worthless patented
medication.
Pharmacodynamics – concerns the
u At the same time, research have found new concept
action of the chemical on the
and techniques that support pharmacology.
organism.
u Drug receptor concept
u Pharmacogenomics

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The Nature of Drugs Drug/Chemical Interactions

u Drug molecule interacts as:

u Agonist (activator) u Chemical antagonist – mostly affects by inactivating a chemical (drug
Plays a regulatory role (hormones,
agonist/ hormones/ neurotransmitter, etc…)
u Antagonist (Inhibitor) neurotransmitters ion channels,
etc..) u Poisons – most of the drugs may have a harmful effects (Side effects, Adverse
effect, Toxic effect, etc…)
Drug molecule/
Drug Receptor - a protein hormones/ “The dose makes the poison.” – Paracelsus (1493-1541)
that receives signal from a neurotransmitters, etc…
u Toxins – poisons of biologic origin. (e.g. spores, bacterial waste, venoms,
chemical or a drug etc…)
molecule. Receptor (violet); the
rest are part of the cell
membrane
Formation of drug-receptor
complex requires appropriate Pharmacologic Effect –
qualifications such as size, shape, production of protein,
elec. Charges. And atomic metabolism, release of
composition.
hormones/ neutrasmitter,
etc..

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The Physical Nature of Drugs

Drug Reactivity &
Drug-Receptor
Bonds
Three major types of chemical forces/ Bonds
u Solid ( aspirin, amoxicillin) The matter of the drug 1. Covalent – very strong and irreversible (e.g.
DRUGS u Liquid (nicotine, ethanol) identifies the Route of aspirin – cyclooxygenase complex)
Electrostatic – common in drug-receptor
u Gas (nitrous oxide) Administration. 2.
bonding. It vary from relatively strong
linkages between permanently charged
ionic molecules to weaker hydrogen bonds
and very weak induced dipole interactions
such as van der Waals forces. Weaker than
covalent bonds.
3. Hydrophobic –quite weak and important
interaction of highly lipid-soluble drugs with
the lipids of cell membrane.

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Drug Size and Shape

Rational Drug Design
u Drug Size – the molecular drug size should be enough
to fit within the receptor site to achieve biological
effect.
Definition: The ability to predict the appropriateness molecular structure of a
u Drug molecular weigh (MW) – 100-1000 - ideal drug on the basis of information about the biologic receptor.
size.

Considerations:
1. Physical and Chemical Properties
• Drug Shape – it should be complimentary
with shape of the receptor site. 2. Functional group components (structural)
• Factors that influence binding with regards 3. Environment of the receptor
shapes.
• Actual shape 4. Drug release and activation (prodrug)
• Chirality (Stereoisomerism) – Symmetry (mirror- 5. Drug survival and passage (metabolism)
like enantiomers), rotation (dextro-/ levo-).
Example: Symmetry – ephedrine (sympathomimetic 6. Drug selectivity
drug), Rotation – levocetirizine, Levodopa,
Dextrometamorphan.

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Physicochemical Properties of the Drug 1. Solubility

u at given temperature, it is the concentration of the dissolved
solute. Where solute is in equilibrium with the solvent.

u The ability of a chemical compound to elicit a pharmacological/ therapeutic effect is u Factors affects solubility of the drug.
related to the influence of various physical and chemical (physicochemical) 1. Temperature
properties of the chemical substance on the bio molecule that it interacts with. 2. pH
1. Physical Properties - physical characteristics of drug that is responsible for its action. 3. Pressure
2. Chemical Properties - the drug react extracellularly according to simple chemical u “Likes dissolve likes”; “polar solute is soluble in polar solvents.”
reactions like neutralization, chelation, oxidation etc.
u Hydrophilicity – water-loving / Lipophobicity – fat-hating
u Hydrophobicity – water-hating / Lipophilicity – fat-loving

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2. Partition coefficient 3. Hydrogen Bond

Extracellular Intracellular

u influence the drug transport

and drug distribution to reach u a dipole-dipole interaction between hydrogen atom in a polar bond. The
the site of action. capability of forming water molecule.
PLASMA MEMBRNE

u It affects the drug transfer u Physical properties affected by H-bonding

characteristics Hydrophilic / Lipophobic 1. Boiling and Melting point
Ionized drugs
2. Water solubility
3. Strength of acids (pH)
4. Spectroscopic properties
5. Surface tension and viscosity
Hydrophobic / Lipophilic
6. Biological products (hormones, enzymes)
Unionized drugs
7. Drug-receptor interactions

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4. Chelation/ Complexation 5. Ionization of drug

u Ionization is the protonation or deprotonation resulting in charged molecule.
u It from imparts good water solubility to the drug which is required of binding of drug and
u complex (attachment) of drug molecule that can’t cross the natural
receptor interaction.
membrane and may result to ineffectivity.
u Unionized from helps the drug to cross the cell membrane.
Example:
Example: Barbituric acid – inactive because it’s a strong acid; 5,5 disubstituted Barbituric acid – CNS
Antidote for metal poisoning. depressant (weak acid)
u - Dimercaprol is a chelating agent. (+ Arsenic poisoning)

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6. Redox Potential 7. Surface Activity

u A quantitative expression of the tendency that a compound has to give or u Surfactant is defined as a material that can reduce the surface tension of
receive electrons water at very low concentration.
u Redox potential of the drug may greatly affect its activation for prodrugs and u Lower concentration of surfactant enhanced the rate of absorption.
metabolism of other drugs for elimination.
u Higher concentration of surfactant reduced the rate of absorption
Example:

1. Riboflavin (Vit B2) analogue

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8. Protein Binding 9. Stereochemistry of drugs

u Stereochemistry –study of the chiral molecules.

Protein + drug <-> Protein-Drug Complex u Roles in pharmacodynamics
1. Any change in stereo specificity of the drug will affect its
u The ability of the drug to bind to the protein may increase the concentration pharmacological activity.
of the drug within the body and the duration of action of the drug and may
Example: Dopamine – cannot pass through BBB; Levodopa – can pass
enhance toxicity.
through BBB
u Common protein: Albumin, Glycoprotein, Lipoproteins
Example: Albumin – NSAIDs, Barbiturates, Penicillins, Warfarin, tetracyclines. 2. The isomeric pairs have different physical properties (pH,
Alpha3-acid glycoprotein – Lidocaine, Quinidine, Metoprolol, verapamil solubility, etc.) and thus differ in pharmacological activity

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Thank you for listening!

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