Introduction to Pharmacology
‣ By the early 1900’s, there were an estimated 250,000
Pharmacology
- Study of substances that interact with living systems through
chemical processes.
- Medical Pharmacology: To prevent, diagnose, & treat
diseases.
toxicology
- Undesirable effects of drug.
drug
- Chemicals obtained from plants or animals, or products of
genetic engineering.
medicine
- Chemical preparation, which contains one or more drugs,
administered with the intention of producing a therapeutic effect.
History of Pharmacology
stone ages
‣ Alcohol - Nutrition, medicine & rituals.
‣ Primitive men - Recognized the benefits/toxic effects of
plants & animal materials.
ancient times
‣ Hippocrates - Inorganic salts as medications.
‣ Galen - Dogmatic approach to medicine.
Middle ages
‣ Medical care taken over by the Church
‣ Medicine became a matter of faith & prescriptions became
prayers.
‣ Reason for failure of Medicine:
➡ Poor knowledge of functioning of the body.
➡ Lack of experimentations and observations.
➡ Close relationship between religion and treatment of
diseases (drugs were thought to be magical!)
renaissance
‣ Paracelsus - Challenged Galenic medicine. He also
promoted use of chemicals & minerals (zinc) in medicine.
➡ Recognized the Dose-response Concept
“Poison is in everything, & no thing is without
poison. The dosage makes it either a poison or a
remedy” - Paracelsus
18th century
‣ Francois Magendie & Claude Bernard - Experimental
Physiology & Pharmacology.
‣ Simultaneous developments in botany, zoology, chemistry &
physiology.
19th century
‣ American Civil War – Usage of Morphine.
‣ Morphine, laudanum, cocaine, & heroin were
completely unregulated and prescribed freely by the
physicians for a wide variety of ailments.
* Scurvy happens where there is absence of vitamin C.
** During those times, people having type 1 DM only have 1-2 years
life span.
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20th century
addicts in the United States.
‣ Various US laws has been established to address drug
addiction.
‣ Nutritional deficiencies has been addressed.
‣ Numerous vaccine discoveries.
21st century
‣ Rapid growth of information and understanding of the
molecular basis for drug action.
‣ Fetal Alcohol Syndrome brought warning tablets to alcohol
products.
‣ Currently, modern pharmacology uses genetics,
molecular biology, biochemistry, & other
advanced tools to transform information about molecular
mechanisms & targets into therapies directed against
disease, defects or pathogens, & create methods for
preventive care, diagnostics, & ultimately personalized
medicine.
- Surgeon General Warning made people aware of the
addictive nature of nicotine.
- The addictive nature of prescription drugs such as Diazepam
(valium) became known, & caffeine came under scrutiny as
well.
oswald schmiedeberg (1838-1921)
- Founder of Modern Pharmacology
carl koller
- Clinical pharmacologist that introduced cocaine as a local
anesthetic into surgical procedures.
pure food & drug act of 1906
- First national drug law in the US, which required accurate
labeling of patient medicines containing opium & certain other
drugs.
harrison narcotic act of 1914
- Forbade sale of substantial doses of opiates or cocaine
except by licensed doctors & pharmacies.
comprehensive drug abuse prevention & control act of 1970
- Repealed, replaced, & updated all previous federal concerned
with narcotics & all other dangerous drugs.
anti-drug abuse acts of 1986 & 1988
- Increased funding for treatment & rehabilitation of drug
addiction.
Drug Laws & Regulation in the
Philippines
RA 9165 (Comprehensive dangerous drugs act of 2002)
- Safeguard the integrity of its territory & the well-being of its
citizenry from the harmful effects of dangerous drugs.
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eo 218 (creation of the philippine drug enforcement agency (pdea)
- EO = Executive Order
- By virtue of the RA 9165, the PDEA was created for effective
law enforcement agency responsible for preventing, investigating
& combating any of all dangerous drugs &/or precursors &
essential chemicals within the Philippines.
ra 10640 (Strengthening of section 21 of the ra 9165)
- The PDEA shall have custody of all dangerous drugs, plant
sources, essential chemicals, as well as instruments/
paraphernalia &/or laboratory equipments.
Ra 6675 (generics act of 1988)
- An act to promote, require & ensure the production of an
adequate supply, distribution, use & acceptance of drugs &
medicines identified by their generic names.
- ra 9502 (cheaper medicine act of 2008)
- An act providing for cheaper & quality medicines,
amending RA 6675
- Started having price ceiling; required to write the
generic name of the drug.
➡ Government Hospital: Generic name only
➡ Private Hospital: Generic name or Generic name +
brand name
Ex. Levothyroxine (Euthyrox) 25 mcg/tab
Pharmacologic Principles
3 Phases of Drug Action
‼ Remember:
• Food in the GI tract may interfere with dissolution
• Some drugs may be gastric irritant, so food may be
necessary to dilute drug concentration
• Liquid form are more rapidly available for
absorption
• Drugs are better absorbed in acidic pH
- Young & elderly have less gastric acidity.
pharmacokinetics
- Process of drug movement to achieve drug action.
‣ What the body does to the drug. (Body → Drugs)
1. Liberation
- AKA Dissolution
- Dissolving drugs into smaller particles to be absorbed
by the body
2. Absorption
- Movement of a drug into the bloodstream after
administration
- Affects bioavailability
➡ Fraction/Percentage of administered dose that
reaches the systemic circulation.
➡ Proportion of a drug or other substance which
enters the circulation when introduced into the
body & so is able to have an active effect.

pharmaceutics
- The study how various dosage forms influence the way which ‣ Parenteral medication has higher
drug affects the body. concentration that oral
- Formulation of drugs to their delivery & disposition in the body medications.
to help them achieve therapeutic effects at their sites of
action. ‣ Parenteral is faster than oral
‣ Enteral & Parenteral Drugs
➡ 80% of drugs are taken orally (enteral)
➡ Oral meds must be disintegrated & combined with a
solution to be absorbed by the GI tract & into the ➡ Factors affecting Bioavailability:
bloodstream 1. Drug Form: tablets, capsule, liquid,
➡ Parenteral drugs do not pass the GI tract.
transdermal patch, suppository, inhalation
‣ Disintegration VS. Dissolution
2. Route of Administration: enteral, topical,
➡ Disintegration: Breakdown of tablet into smaller or parenteral
particles. ‣ First-Pass Metabolism: A fraction of
➡ Dissolution: Dissolving of smaller particles in the GI the drug can be metabolized in the liver
tract. before it even reaches the systemic
circulation. Makes the bioavailability of
the drug reduced. Oral & Rectal route.
✓ Oral drugs have lower plasma
concentration; Rectal drugs are
suppository.
‣ Enteric-coated drugs
➡ Polymer barrier applied on oral medication that ✓ Sublingual & Buccal route won’t
prevents its dissolution or disintegration in the gastric Hepatic First-Pass Metabolism
environment, causing delayed onset/sustained release. (HFPM); not all drugs can be
➡ Don’t crush; designed not to be dissolved immediately sublingual.
3. GI Mucosal Integrity & Motility
4. Administration With Food or Other
Drugs

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 5. Disease: Change in liver metabolism due to • Drugs that dissolve in fat
liver dysfunction or decrease in hepatic blood • EX: Anti-anxiety drug, Clorazepate, tends to
flow concentrate in fatty tissues.
‣ Protein Binding
- Drug Absorption Through GI Membrane:
➡ Degree to which medications attach to proteins
within the blood.
➡ Common Blood Proteins that Drug Bind:
• Albumin
‣ Abundant protein in the body
‣ Mainly synthesized in the liver
‣ Responsible for the oncotic (“pulls water”)
pressure inside the cell.
• Lipoprotein
• Glycoprotein
• α, β‚ & γ Globulins
➡ Free drugs
• AKA Unbound drug
• An active drug or other compound that is not
bound to a carrier protein.
‣ Active Absorption: energy department (ATP)
➡ Requires an enzyme or protein - may be from
low to high concentration ‼ Remember:
‣ Passive Absorption: no energy • The less bound a drug is, the more efficiently it can traverse cell
➡ Diffusion - high to low concentration membranes or diffuse.
➡ Facilitated Diffusion - rely on carrier protein
from high to low concentration - Volume of Drug Distribution (Vd)
‣ Pinocytosis: ‣ Volume at which drug would need to be uniformly
➡ Cells carry drug across membrane by distributed to produce an observed blood
engulfing drug particles concentration
- Factors Affecting Drug Absorption: ‣ Calculated as the ration of the dose present in the
> Blood flow > Fasting body & its plasma concentration.

> Pain > Food

> Stress > pH
> Hunger

‼ Remember:
• Certain drugs need acid for better absorption (thus taken ‣ Interstitial Fluid can be
after meals) penetrated by water-soluble
& low molecular weight
3. Distribution
drugs

‣ Lipid-soluble & other

low molecular weight
drugs targets the cell.

- Blood-brain Barrier (BBB)

‣ Highly selective semipermeable border of
- Process wherein drug reversibly leaves the bloodstream endothelial cells that protects the brain from
& enters the target organs. foreign substances (98% of drugs) & prevents
- Affected by: solutes in the circulating blood from non-
‣ Size of Organ selectively crossing into the extracellular
‣ Blood Flow
fluid of the central nervous system where neurons
➡ Ex:
reside.
• Uncontrolled DM in patient’s blood is viscous ✓ Brain is highly sensitive to changes.
• When patient is hypotensive, they need to be
hydrated first so drugs would go to the tissues
‣ Some drugs that are highly lipid soluble & low
faster. molecular weight are able to cross BBB through
‣ Solubility diffusion & transport protein.
➡ Water-soluble Drugs 4. Metabolism (Biotransformation)
• Drugs that dissolve in water - Chemical alteration of chemicals such as nutrients,
• EX: Anti-hypertensive drug, Atenolol, tends to amino acids, toxins, & drugs in the body.
stay within the blood & the fluid that - Liver is the primary site; metabolizes lipid-soluble drugs
surrounds cells (interstitial space). into water-soluble drugs for excretion.
➡ Lipid-solube Drugs

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 - Half-life (t1⁄2) ‣ Antagonists: Prevent receptor activation; drugs that
‣ Time it takes for one-half of the drug concentration “block” a response.
to be eliminated.
‣ Takes approximately six half-lives for a drug to be
eliminated around 98%
‣ Almost all drugs, not all drugs are applicable to
half-life
‣ EX: 12pm 100mg (every 4 hours)
4pm 50mg
8pm 25mg
12am 12.5mg
- Loading Dose: Initial higher dose of a drug that may
be given at the beginning of a course of treatment
before dropping down lower maintenance dose.
- Enzyme Inducers VS. Enzyme Inhibitors
‣ Inducer = increases metabolism -> increase ‼ Remember:
elimination -> decrease drug concentration
• The drug agonist that has an exact fit with a receptor
‣ Inhibitor = decreases metabolism -> decrease is a strong agonist & is more biologically active.
elimination -> increase drug concentration
➡ Ex: Drug A = Warfarin (Blood Thinner)
Drug Response
Drug B = Enzyme Inhibitor (Inducer)
————————————————————————————————- 1. Tachyphylaxis
Bleeding (Clotting) ‣ Rapidly diminishing response to successive dosage of a
drug, rendering it less effective.
5. Excretion
- Most drugs, particularly water-soluble drugs & their 2. Placebo Effect

metabolites, are eliminated by the kidneys in urine.

‣ Beneficial effect that cannot be attributed to the properties
of the placebo itself, & must therefore be due to the
- Others: sweat, feces, saliva, bile, & breast milk
patient’s belief in that treatment.
- Therefore, drug dosing depends largely on kidney
function. 3. Therapeutic Index
- Creatinine Clearance: ‣ Margin of safety of a drug through the use of a ration that
measures the effective (therapeutic concentration) dose (ED)
in versus the lethal dose (LD)
‣ Measures renal
function
‣ Normal: 85-135 mL/
min
‣ ↓Renal Function
↑Excretion

‼ Remember:
• Drugs should be metabolized to water-soluble
for it to be excreted.

pharmacodynamics 4. Side Effect VS. Adverse Effect

- Branch of pharmacology concerned with the effects of drugs &
the mechanism of their action.
- Study of drug concentration & its effects in the body
- What the drugs does to the body (Drugs → Body)
- Receptor Theory:
‣ A specialized target macromolecule that binds a drug &
mediates its pharmacological action.
➡ Ex: Enzymes, nucleic acids, or specialized membrane-
bound proteins.
‣ The formation of the drug-receptor complex leads to a
biological response.
- Receptor Site:
‣ Proteins that are on the surface of each cell that act as
receivers of chemical messenger molecules in the
intercellular fluid surrounding every cell.
- Agonists VS. Antagonists
‣ Agonists: Activate receptors to produce the desired
response; drugs that produce a similar response. “Helps”
‣ Side Effect: Physiological effects not related to desired
drug effects, which can be desirable or undesirable.
‣ Adverse Effects: Range of untoward effects of drugs that
may cause mild to severe side effects, these are always
undesirable.
5. Toxic Effect
‣ Level of damage that a compound can cause to an
organism.
‣ When the drug level exceeds the therapeutic range of the
drug.
Dose-response & maximal effect
- Relationship between minimal & maximal amount of drug dose
needed to produce the desired drug response.
pharmacotherapeutics
- The use of drugs & the clinical indications for drugs to prevent &
treat diseases.

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onset, peak, & duration of action
- Onset: Time it takes to reach the minimum effective
concentration (MEC) after a drug is administered.
- Peak Action: Occurs when the drug reaches its highest blood
or plasma concentration.
- Duration of Action: Length of time the drug has a
pharmacological effect.
Therapeutic Window
- Range of doses that produces therapeutic response without
causing any significant adverse effect in patients.
- Between the minimum effective concentration (MEC) & the
minimum toxic concentration (MTC) non-specific drug effect
- Safe range for drug dosage

Therapeutic failure
- Failure to achieve or maintain desired therapeutic effect of a
drug.
non-specific drug effect - Causes of Therapeutic Failure:
> Poor Compliance > Quality of Drugs
> Factors affecting Biotransformation > Drug Tolerance
> Factors affecting Bioavailability > Inappropriate
Indication
> Drug Interactions > Untoward effects

Categories of drug action

> Stimulation/Depression > Inhibition/Killing of organisms
> Replacement > Irritation

Non-selective drug effect

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