1 CONCHEM 4TH QUARTER
MEDICINE
PROPERTIES OF MEDICINE AND ITS
MAJOR CLASSIFICATIONS
WHAT IS DRUG?
- From French term ‘drogue”
- Induce form stupefaction > stupefies
one’s line of thought and state of mental
well-being
- Any chemical compound (synthesized in
lab/plant/animal/marine origin) that
brings change in normal physiological
functions of body
- Habit-forming substances, can lead to
serious adverse effects
WHAT IS MEDICINE
- Any preparation meant for
treating/preventing illnesses/discomfort
- Field of study about the clinical
assessment, making diagnoses, treating
diseases and preventing them
- Won’t lead to addiction; won’t stupefy
the mind
- Latin word “medicina”
PROPERTIES OF MEDICINE
1. Activity of Medicine*
2. Solubility
3. Shell life
4. Selectivity *
5. Distribution inside*
6. Excretion
7. Bioavailability
8. Side effects/Toxicity
9. Oral Absorption*
10. Metabolism*
1. ACTIVITY OF MEDICINE
 Ability to produce a therapeutic
effect in the body
 Factors that can influence:
 Chemical Structure
 Pharmacokinetics
 Pharmacodynamics
 Dosing
 Measured by Potency
**TM – THERAPEUTIC MEDICINE
o Amount of medicine
required to produce a
certain level of effect
o More potent medicines
require less medicine to
produce the same effect as
less potent medicines
 Efficacy of a Medicine related to its
activity
 Efficacy is how well medicine
produces a desired effect
compared to other medicines
 Medicines with high activity
tend to have higher efficacy
2. Selectivity
 Degree to which a drug can bind to
a specific target/receptor and
produce a desired effect without
affecting other targets/receptors
 Degree of selectivity is determined
by:
 Chemical structure
 How well it fits into the active
site of its target receptor
 Factors that influence:
 Chemical structure
 Active site of its target receptor
 Use of targeted drug delivery
systems
 Can be improved by modifying
chemical structure/through the use
of targeted drug delivery systems
that deliver the drug directly to its
intended target
 Important in drug development to
determine drug’s effectiveness and
potential side effects
3. ORAL ADSORPTION
 Process by which a drug is
ABSORBED into the
BLOODSTREAM AFTER
INGESTED ORALLY
 Factors that influence:
 Chemical properties of the drug
 Presence of food/other drugs in
the stomach
 2 CONCHEM 4TH QUARTER

 pH of the stomach & small

intestine
 surface area and blood flow of
the intestinal flow
 First-pass metabolism
 Metabolic breakdown of a drug
 Occurs in the lived before
entering the blood circulation
 REDUCES amount of drugs that
enters the bloodstream, impacts
DRUG ABSORPTION AND
EFFICACY  Factors that influence drug
4. DRUG DISTRIBUTION distribution:
 Process by which drugs move from  Drug’s chemical properties
the bloodstream to various tissues  Route of administration
and organs  Body’s physiological
characteristics
 Presence of other drugs
 Molecular weight
 Lipophilicity
 Ionization

5. DRUG METABOLISM
 Process by which the body breaks
down drugs and other foreign

**TM – THERAPEUTIC MEDICINE

 3 CONCHEM 4TH QUARTER
substances (such as toxins for them
to be eliminated)
 Important because it can impact
EFFECTIVENESS AND SAFETY
OF DRUGS, as well as their
potential for drug interactions and
adverse effects
 MAIN PHASES OF DRUG
METABOLISM
 Factors that affect drug
metabolism:
 Age
 Genetics
 Disease
Other drugs and substances that may
induce/inhibit metabolic enzymes
QUESTIONS TO ASK
1. Why is understanding activity of
medicine important for drug
development
- Optimize drug design, dosing regimens,
treatment strategies
**TM – THERAPEUTIC MEDICINE
- Better, safe, and effective treatments for
patients
2. Potential benefits of highly selective
medicine
- More effective and safer
- Treatment of wide ranges of diseases
3. Presence of food in the stomach and oral
absorption
- Presence of food/other drugs can alter
pH and transit time of the drug
- Binding to the drug and reducing its
availability for absorption
4. Drugs in the body and drug distribution
- Other drugs can affect drug distribution
by competing for binding sites
- Inhibiting the activity of drug-
metabolizing enzymes in the liver
5. Knowledge of drug metabolism in
clinical practice (drug dosing and
monitoring)
- Informing drug dosing and monitoring
strategies
DRUG RECEPTORS
Drugs will not work unless it is bound. They are
bounded by RECEPTORS. They can be
proteins, lipids, or DNA
- Macromolecular component of cell with
which a drug interacts with to produce
a response
- Molecule in the body that recognizes
and binds to specific drugs
- Drug binds to receptor > produces
specific effect in the body/specific
physiological response
 4 CONCHEM 4TH QUARTER
- Any changes/dysfunctions can cause
DRUG RESISTANCE, TOXICITY, AND
REDUCED EFFICACY
DRUG AFFINITY
- Drug’s ability to affect a given receptor
is related to DRUG AFFINITY
(probability of drug to occupy a
receptor) AND INTRINSIC EFFICACY
(degree to which a ligand activates
receptors and leads to cellular
response)
3 MAIN TYPES OF DR
1. G protein-coupled receptors
(GPCRs)
 Largest most diverse family of
receptors in the body
 Found in cell membrane
 Wide range of physiological
processes (i.e vision, taste,
regulation of heart rate)\
 Ex. BETA BLOCKERS (to treat
high blood pressure and heart
disease > ACE INHIBITOR)
 Ex. ANTIHISTAMINES (treat
allergies)
2. Ligand-gated ion channels
 Cell membrane
 Transmission of nerve impulses
 When a ligand (i.e drug) binds
to the channels, causes channel
to open and allowing ions to
flow into/out of the cell
 Ex. BENZODIAZEPINES (treat
anxiety and insomnia)
 Ex. NICOTINE (tobacco
products)
3. Enzyme-linked receptors
 Found on surface of cells
 Involved in signal transduction
pathways
 When drugs bind to this
receptor, can either
activate/inhibit certain enzymes
inside the cell, leading to a
variety of effects
 Ex. Insulin (Treating diabetes)
**TM – THERAPEUTIC MEDICINE
 Epidermal growth factor
receptor inhibitors (Treating
cancer)
LIGAND
- Molecules that binds to a receptor
- 2 types of ligands
1. Agonist
2. Antagonist
CLASSIFICATION OF LIGANDS
1. Agonist
 Activator
 Promotes activity of a specific
regulatory system/body process
 ACTIVATES RECEPTORS TO
PRODUCE DESIRED RESPONSE
 Mimic similar response to the
intended chemical and receptor
 INCREASE DRUG EFFICACY BY
PRODUCING A BIOLOGICAL
RESPONSE
2. Antagonist
 Inhibitor
 Opposite effect of agonist
 PREVENT RECEPTOR
ACTIVATION
 Stops/blocks receptor from making
a response
 DECREASES DRUG EFFICACY
BY BLOCKING BIOLOGICAL
RESPONSE
 Improves safety by blocking
harmful biological responses that
may be caused by agonists
 5 CONCHEM 4TH QUARTER
CHARACTERISTICS OF AN EFFECTIVE
PHARMACOLOGICAL DRUG
1. A drug must have a very specific size,
shape, atomic config. And electrical
charge to be able to interact with the
receptor
2. Drug size must have the necessary
properties to travel to its site of
action/receptor from its site of
administration
 Drug physiochemical properties
 Formulation
 Route of administration
3. Must be easily inactivated/excreted from
the body once used for its purpose
CHARACTERISTICS OF DRUGS
a. Physical and Chemical Nature of Drugs
I. Drug Size
 Drug must be a certain size to
bind to a receptor
 This size is approx. 100MW >
LOWER LIMIT OF DRUG
SIZE > determined by the need
for the drug to be sufficiently fit
for the receptor
 ALL DRUGS MUST BE ABLE
TO CARRY OUT DIFFUSION
TO MOVE WHERE THEY
ARE NEEDED
 Upper limit of drug size
depends on the need of the drug
**TM – THERAPEUTIC MEDICINE
to be able to move within the
body
 Drugs larger than 1000MW do
not diffuse readily > most drugs
are below 1000MW
 Large drug sizes may reduce
drug efficacy
b. Drug Reactivity and Drug bonds
 Short-acting effect – drug must have
low reactivity
 Powerful and long-lasting effect –
higher reactivity
**Note: high reactivity can reduce
efficacy and cause unwanted side
effects
I. Covalent
 Strong bonds, not easily broken
 Ex. ASPIRIN, forms covalent
bond with target enzyme
cyclooxygenase
II. Electrostatic
 More common type of bond in
drug receptor interactions
 Weaker than covalent (i.e ionic)
III. Hydrophobic
 Quite weak
 Found in highly lipid-soluble
drugs and lipids in the cell
membranes interaction
THERAPEUTIC MEDICINE
- Medications for treating/managing
specific medical conditions
- Many start with the prefix “anti”
(against) > describe what the drug is
working AGAINST
**Antipsychotics, antidepressants,
anticonvulsants, analgesics, antibiotics,
 6 CONCHEM 4TH QUARTER

antihistamine, antinauseants, and many Anticoagulants – prevent blood clots

more
- Some don’t start with this prefix
**Decongestants, hallucinogens,
sedatives, stimulants
- Can have potential risks and side
effects; varies on the medication

PHARMACOLOGICAL DRUG
- Categorizes drug based on chemical
composition, mechanism of action, how
the affect the body’s physiological
functions
- Ex.
 Atenolol – beta-blocker that reduces
DEFINITION OF TERMS heart rate and blood pressure
MODE OF ACTION  Lisinopril – ACE (angiotensin-
 How medication works in the body to converting enzyme) inhibitor that
produce a therapeutic effect works by relaxing blood vessels,
EFFICACY reducing blood pressure, improving
 How well the medication works blood flow
- Factors to be considered:  Fluoxetine – SSRI (Selective
Patient’s medical history, severity of condition, Serotonin Reuptake Inhibitor) that
potential side effects/interactions that can impact works by increasing serotonin in the
efficacy of treatment/medicine brain
EXAMPLES OF TM
Antidepressants - depression and other mood
disorders
Antibiotics - bacterial infections
Antihypertensive –High blood pressure
Analgesics - used to relieve pain

- Helps healthcare professionals in

determining the most appropriate
medication for a particular health

**TM – THERAPEUTIC MEDICINE

 7 CONCHEM 4TH QUARTER

condition based on the DRUG’S

SPECIFIC PROPERTIES
DIFFERENCE BETWEEN THERAPEUTIC
AND PHARMACOLOGICAL
CLASSIFICATION
THERAPEUTIC
 Based on primary therapeutic
use/intended effect on the body
 What the drug is used to treat, rather
than drug’s specific properties
PHARMACOLOGICAL
 Based on chemical composition,
mode of action, and atomic
configuration

**More examples of a drug’s pharmacological

and therapeutic class.

OVER THE COUNTER AND

PRESCRIPTION MEDICINE

**TM – THERAPEUTIC MEDICINE

 8 CONCHEM 4TH QUARTER
OVER-THE-COUNTER DRUGS
- Do not require a prescription
- Bought off-the-shelf of stores
- Regulated by FDA > OTC Drug
Monographs
- TEMPORARY RELIEF ONLY
- NOT FOR LONG-TERM
USE/TREATMENT OF CHRONIC
CONDITIONS
DEFINITION OF TERMS
CHEMICAL COMPOSITION OF OTCs
Active ingredients & other components that
make up the medication
PHYSICAL PROPERTIES
Refers to the FORM IN WHICH THE
MEDICATION IS PRESENTED
- Tablets, capsules, liquids, dissolvable
tablets
- Packaging
THERAPEUTIC EFFECTS
Intended purpose of medication (i.e. relieving
pain, reducing fever, etc.)
EXAMPLES
1. Acetaminophen
 For fever
 Minor aches and pains,
especially for people who can’t
tolerate anti-inflammatory meds
like ibuprofen/aspirin
2. Non-steroidal Anti-inflammaroty
Drugs (NSAIDs)
 Inflammation, fever, pain
3. Dextromethrophan
 Controls cough
 Usually found in cough syrups
and cold medications
 Indicated as DM (ex.
Robitussin DM)
4. Guaifenisin
 Loosens mucus in the
bronchi/large breathing tubes
 Causes more coughing but
decreases cough intensity and
frequency to clear out mucus
5. Oral Decongestants (OD)
 Pill/liquid form
**TM – THERAPEUTIC MEDICINE
 Shrinking engorged blood
vessels in nasal and sinus
passages
6. Nasal Spray Decongestants
 Similar to OD
 Acting only in the area applied
 Usually without the stimulat
side effects
7. Diphenhydramine
 Antihistamine
 Treats sneezing, runny nose,
watery eyes
8. Calcium Carbonate
 Antacids that work
immediately to relieve acid
indigestion and heartburn
 Chewable tablets and liquid
forms
 HOWEVER, aluminum-based
antacids may cause constipation
and magnesium based products
can cause diarrhea
9. Medications for Constipation
 Relieve constipation
 Include glycerin suppositories
that help in bulking-up and
lubricating stool
10. Loperamide
 Treatment for diarrhea
 HOWEVER, if constipation,
ileus, fever, or bleeding occurs
> STOP THE USE OF THIS
OTC

 9 CONCHEM 4TH QUARTER
PRESCRIPTION DRUGS
- Prescribed by a doctor
- Bought at pharmacys
- Intended for one person only
- Regulated by FDA through the New
Drug Application (NDA) process
EXAMPLES OF PD
1. Vicodin
 Popular drug for treating
acute/chronic moderate to
moderately severe pain
2. Simvastatin
 One of the first “statins” (HMG-
CoA reductase inhibitors)
approved for:
 TREATS HIGH
CHOLESTEROL AND
REDUCING RISK OF
STROKE, DEATH FROM
HEART DISEASE, AND RISK
OF HEART ATTACKS
3. LISINOPRIL
 ACE inhibitor
 Treats high blood pressure,
congestive heart failure,
 Prevents kidney failure from
blood pressure and diabetes
 Can be taken with or without
food as prescribed by the doctor
and has to be used regularly to
take full effect
4. Levothyroxine
 Man-made version of thyroid
hormone
 Treats hyperthyroidism
o Condition wherein the
thyroid gland does not
produce enough thyroid
hormones for the body
o Thyroid is inactive
 Brand names: Levoxyl,
Synthroid, Unithroid
 Available in Oral
tablet, oral capsule,
injectable solution
5. Azithromycin
 Antibiotic
**TM – THERAPEUTIC MEDICINE
 Treats ear, throat, sinus
infections, pneumonia,
bronchitis, and some STDs
6. Metformin
 Used alone or in combo with
other drugs
 Treats type 2 diabetes in adults
and children
 Side effects: nausea, vomiting,
gas, bloating, loss of apetite
7. Lipitor
 Treats high cholesterol
 Prevents chest pain, stroke,
heart attack in individuals with
Coronary artery disease
 THESE ARE NOT FOR
EVERYONE
o People who are allergic to
Lipitor
o Women who are
nursing/pregnant
 Side effects: diarrhea, upset
stomach, muscle, and joint pain
8. Amlodipine
 Calcium channel blocker
 Treats high blood pressure and
prevention of chest pain
 Lowers BP by Relaxes blood
vessels so that the heart does not
have to work too much
 Controls chest pain by
increasing blood supply to the
heart
 Comes in tablet and
suspension(liquid)
 Side effects: head aches and
swelling of lower extremities
9. Amoxicillin
 Penicillin type antibiotic
 Treats bacterial infections like
ear, tonsils, throat, larynx,
urinary tract, and skin infections
 WILL NOT WORK for VIRAL
INFECTIONS (cold, flu etc)
 Using antibiotics when not
needed will cause drug
resistance
 1
0 CONCHEM 4TH QUARTER

10. Hydrochlorothiazide
 Diuretic (Water pill)
 Used alone or combo with other
drugs to treat HBP
 Eliminates extra salts and water
in the body
 Reduces excess fluids in the
body (edema) caused by
conditions like heart failure,
liver disease, etc.
 Lessens symptoms like
shortness of breath/sweeling of
ankles

MEANING OF Rx
 imperative form
of the verb “to
receive”
 a command,
meaning in
effect “take
this”

**TM – THERAPEUTIC MEDICINE

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1 CONCHEM 4TH QUARTER

CANCER APOPTOSIS > genetic information

DIFFERENTIATE CANCER FROM is broken down; cell is fragmented
to smaller pieces and is taken in by
CARCINOGENS
nearby cells (phagocytic cells)
CELL DIVISION
- Growth, repair, and replacement of
TUMOURS
damaged/dying cells
- Defined by the National Cancer Institute
CANCER
- Disease in which some of the body’s
cells grow uncontrollably and spread
to other parts of the body
NORMAL CELLS
Will not divide unless they receive an outside
signal

as “ABNORMAL MASS OF TISSUE

Normal tissue
 There is a balance between the
generation of new cells via cell
division and loss of cells
through cell death
 Old cells become damaged and
undergo apoptosis (form of
programmed cell death)
AS A RESULT OF
UNCONTROLLABLE CELL
DIVISION
- Can be cancerous (malignant) or
noncancerous (benign)
o Benign – cannot spread or
grow/very slowly growing
o Malignant – grow and
spread to the rest of the
body
METASTASIS
- Spread of cancer to diff. parts of the
body (usually to bones, liver, or lungs)
through the lymph system/bloodsystem

**TM – THERAPEUTIC MEDICINE

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2 CONCHEM 4TH QUARTER

- Metastatic cancer/metastatic tumour > MX: Metastasis cannot be measure

spread from the primary site of origin to M0: Cancer has not spread
other parts of the body M1: Cancer has spread
- New tumours form using the same kind
of cancer cells from the orig, tumour
CANCER STAGING
- Stage – extent of cancer depending on
largeness of tumor and metastasis of the
cancer
- Knowing this helps doctors

OTHER STAGING SYSTEMS FOR ALL

TYPES OF CANCER
In Situ – Presence of abnormal cells, has not
metastasized
Localized – Cancer is limited to primary site, no
signs of spreading
Regional – Cancer has spread to nearby lymph
nodes, tissues, and organs
STAGING SYSTEMS Distant – has spread to distant parts of the body
1. TNM STAGING SYSTEM Unknown – Not enough info to figure out the
 Most widely used cancer staging stage
system
 T – Size and Extent of main TYPES OF CANCER
tumor 1. CARCINOMA
 N - # of nearby lymph nodes - Originates from the skin
that have cancer - Can form solid tumors
 M – whether the cancer has 2. SARCOMA
metastasized - Starts from tissues that support and
i. Primary tumor (T) connect the body (i.e fat, muscles,
TX: Main tumor cannot be measured nerves, tendons, nerves, joints, blood
T0: Main tumor cannot be found vessels, bone, lymph vessels, or
T1, T2, T3, T4: Size &/ extent of main tumor cartilage)
(Higher number, larger/growth of tumor to 3. LEUKEMIA
nearby tissue - “Cancer of the Blood”
ii. Regional lymph nodes (N) - Cancer of the body’s blood-forming
NX: Cancer in nearby lymph nodes cannot be tissues (bone marrow and lymphatic
measured system)
N0: No cancer in lymph nodes 4. LYMPHOMA
N1, N2, N3: # and location of lymph nodes with - Cancer of the lymphatic system (part of
cancer (higher number, more infected lymph the body’s germ fighting system”)
nodes)
iii. Distant metastasis (M)

**TM – THERAPEUTIC MEDICINE

 1
3 CONCHEM 4TH QUARTER
- Lymph nodes(lymph glands), spleen,
thymus gland, and bone marrow.
- Can affect all those areas as well as
other organs
CARCINOGENS
- Cancer causing agent
- Originates from the English word
carcinoma
- Depends on:
1. What you are exposed to?
2. How often you were exposed?
3. How much were ou exposed to?
TYPES OF CARCINOGENS
1. Chemicals/substances
2. Environmental radiation
3. Medical Radiation
4. Viruses
5. Lifestyle factors
1. CHEMICALS/SUBSTANCES
Three types are:
 Procarcinogen
 Chemical being changed during
embolism
 Cocarcinogen
 Acting with another chemical
 Direct acting Carcinogen
 Causes cancer as is
2. ENVIRONMENTAL RADIATION
 ULTRAVIOLET RADIATION(UV
RAYS – well known cause of skin
cancer
 Radon emitted can cause nroaml
decay of uranium in soil which
is then trapped in homes > 2nd
leading cause of lung cancer
3. MEDICAL RADIATION
 Both radiation used medically for
diagnostics and those used to treat
cancer are carcinogens
4. VIRUSES
 Human papillomaviruses – oral and
cervical cancer
 Hepatitis C – liver cancer
5. LIFESTYLE FACTORS
**TM – THERAPEUTIC MEDICINE
Smoking AND obesity are both
carcinogens > causes mutations that
may result to cancer
CARCINOGEN CLASSIFCATION
SYSTEM
- The Internation agency for Research on
Cancer (IARC devised a list of
carcinogens they have tested
i. Group 1: Carcinogenic to humans
– sufficient evidence of
carcinogenicity
Ex. Cigarettes, processed meat,
alcohol, radiation
ii. Group 2A: Probably carcinogenic
to humans – limited evidence of
carcinogenicity in humans and
sufficient evidence of
carcinogenicity in experimental
animal
Ex. Beef, fried food, beef
ii. Group 2B: Possibly carcinogenic –
Limited evidence of carcinogencity
in humans, less han sufficient
evidence in experimental animals
Ex. Caffeine, gas, pickled veggies,
vehicile smoke
iii. Group 3: Carcinogenicity not
Classifiable – evidence of
carcinogenicity is inadequate for
humans and limited/inadequate for
experimental animals
iv. Group 4: Probably not
Carcinogenic – Evidence suggests
no carcinogenicity
*Only one chemical was classified
in this group CAPROLACTUM
(used in manufacturing of
synthetic fibres
DETECTING CANCER
The earlier the diagnosis, the better chance of
survival
- MRI (Magnetic Resonance Imaging)
- (CT) Computerized Axial Tomography
Scan
- Prostatic ultrasound
- Regular self-exams and checkups
 1
4 CONCHEM 4TH QUARTER

ANTI CANCER DRUGS ALTERING THE FUNCTION OF

- Targets DNA structure/segregation of
DNA
- Conventional chemotherapy
RESPONSES TO ANTI-CANCER
MEDICINES
- Induce cancer cell death
- Tumor shrinkage & Increase patient
survival
- Increase time until disease progresses
- Induce cancer cell
differentiation/dormancy
- Combination of drugs is selected
through:
1. Efficacy ENZYMES FOR CELL
2. Toxicity METABOLISM AND PROTEIN
3. Optimum scheduling SYNTHESIS
4. Mechanism of interaction  Cell cycle specific: s-phase (acts on
5. Avoidance of arbitrary dose changes cells that are synthesizing new DNA for
new cells)
Dosage factors  Bone marrow suppression, GI
1. Dose escalation ulcerations, alopecia, and nausea and
2. Reducing interval between treatment vomiting
cycles  Ex. PURINE, PYRIMIDINE, FOLATE
3. Sequential scheduling of either ANTAGONISTS
agents/combination of regimens 3. PLANT ALKALOIDS
TYPES OF ANTI-CANCERS
 Anti-tumor agents derived from
1. ALKYLATOR/ALKYLATING
plants
DRUGS
 Blocks ability of cancer cells to
 First anti-cancer drug
divide
 ACTS DIRECTLY ON DNA
 S-phase and m-phase specific
 Prevents cell division by damaging
 Ex. Madagascar periwinkle plant
the DNA
**DRUGS DERIVED FROM
 Not cell cycle specific PLANTS – Eetoposide and teniposide
 Results to susceptibility to infection inhibit function of DNA
 Dose-limiting toxicity: bone marrow 4. HORMONE ANTAGONISTS
suppression  Female hormone estrogen > can be a
 Adverse effects – nausea, vomiting, factor in causing some types of
alopecia, ulcerations of FI tract & creast cancer
mucus membranes  TAMOXIFEN – estrogen receptor
 Works in 2 WAYS: blocker > inhibits growth of breast
2. ANTIMETABOLITE DRUGS cancer cells
 EFFECTIVE FOR Treatment of 5. ANTIBIOTIC DRUGS
LEUKEMIA  Cell-cycle nonspecific
 Replace natural substance as building
blocks in DNA molecules >

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5 CONCHEM 4TH QUARTER

 Binds with DNA and preventing

RNA synthesis (necessary for cell
survival)

**TM – THERAPEUTIC MEDICINE