1 CONCHEM 4TH QUARTER

MEDICINE o Amount of medicine

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

**TM – THERAPEUTIC MEDICINE

 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 - Better, safe, and effective treatments for
to be eliminated) patients
 Important because it can impact 2. Potential benefits of highly selective
EFFECTIVENESS AND SAFETY medicine
OF DRUGS, as well as their - More effective and safer
potential for drug interactions and - Treatment of wide ranges of diseases
adverse effects 3. Presence of food in the stomach and oral
 MAIN PHASES OF DRUG absorption
METABOLISM - Presence of food/other drugs can alter
 Factors that affect drug pH and transit time of the drug
metabolism: - Binding to the drug and reducing its
 Age
 Genetics
 Disease
Other drugs and substances that may

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
induce/inhibit metabolic enzymes 5. Knowledge of drug metabolism in
clinical practice (drug dosing and
QUESTIONS TO ASK monitoring)
1. Why is understanding activity of - Informing drug dosing and monitoring
medicine important for drug strategies
development
- Optimize drug design, dosing regimens, DRUG RECEPTORS
treatment strategies 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

**TM – THERAPEUTIC MEDICINE

 4 CONCHEM 4TH QUARTER

- Any changes/dysfunctions can cause  Epidermal growth factor

DRUG RESISTANCE, TOXICITY, AND receptor inhibitors (Treating
REDUCED EFFICACY cancer)
DRUG AFFINITY LIGAND
- Drug’s ability to affect a given receptor - Molecules that binds to a receptor
is related to DRUG AFFINITY - 2 types of ligands
(probability of drug to occupy a 1. Agonist
receptor) AND INTRINSIC EFFICACY 2. Antagonist
(degree to which a ligand activates
receptors and leads to cellular
response)
3 MAIN TYPES OF DR CLASSIFICATION OF LIGANDS
1. G protein-coupled receptors 1. Agonist
(GPCRs)  Activator
 Largest most diverse family of  Promotes activity of a specific
receptors in the body regulatory system/body process
 Found in cell membrane  ACTIVATES RECEPTORS TO
 Wide range of physiological PRODUCE DESIRED RESPONSE
processes (i.e vision, taste,  Mimic similar response to the
regulation of heart rate)\ intended chemical and receptor
 Ex. BETA BLOCKERS (to treat  INCREASE DRUG EFFICACY BY
high blood pressure and heart PRODUCING A BIOLOGICAL
disease > ACE INHIBITOR) RESPONSE
 Ex. ANTIHISTAMINES (treat
allergies) 2. Antagonist
2. Ligand-gated ion channels  Inhibitor
 Cell membrane
 Opposite effect of agonist
 Transmission of nerve impulses
 PREVENT RECEPTOR
 When a ligand (i.e drug) binds
ACTIVATION
to the channels, causes channel
 Stops/blocks receptor from making
to open and allowing ions to
a response
flow into/out of the cell
 Ex. BENZODIAZEPINES (treat  DECREASES DRUG EFFICACY
anxiety and insomnia) BY BLOCKING BIOLOGICAL
 Ex. NICOTINE (tobacco RESPONSE
products)  Improves safety by blocking
3. Enzyme-linked receptors harmful biological responses that
 Found on surface of cells may be caused by agonists
 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

 5 CONCHEM 4TH QUARTER

to be able to move within the

body
CHARACTERISTICS OF AN EFFECTIVE  Drugs larger than 1000MW do
PHARMACOLOGICAL DRUG not diffuse readily > most drugs
1. A drug must have a very specific size, are below 1000MW
shape, atomic config. And electrical  Large drug sizes may reduce
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 drug efficacy
 Formulation b. Drug Reactivity and Drug bonds
 Route of administration  Short-acting effect – drug must have
3. Must be easily inactivated/excreted from low reactivity
the body once used for its purpose  Powerful and long-lasting effect –
CHARACTERISTICS OF DRUGS higher reactivity
**Note: high reactivity can reduce
efficacy and cause unwanted side
effects
I. Covalent
 Strong bonds, not easily broken
 Ex. ASPIRIN, forms covalent
a. Physical and Chemical Nature of Drugs bond with target enzyme
I. Drug Size cyclooxygenase
 Drug must be a certain size to II. Electrostatic
bind to a receptor  More common type of bond in
 This size is approx. 100MW > drug receptor interactions
LOWER LIMIT OF DRUG  Weaker than covalent (i.e ionic)
SIZE > determined by the need III. Hydrophobic
for the drug to be sufficiently fit  Quite weak
for the receptor  Found in highly lipid-soluble
 ALL DRUGS MUST BE ABLE drugs and lipids in the cell
TO CARRY OUT DIFFUSION membranes interaction
TO MOVE WHERE THEY
ARE NEEDED
 Upper limit of drug size

THERAPEUTIC MEDICINE
- Medications for treating/managing
specific medical conditions
- Many start with the prefix “anti”
(against) > describe what the drug is
working AGAINST
depends on the need of the drug **Antipsychotics, antidepressants,
anticonvulsants, analgesics, antibiotics,

**TM – THERAPEUTIC MEDICINE

 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  Shrinking engorged blood

- Do not require a prescription vessels in nasal and sinus
- Bought off-the-shelf of stores passages
- Regulated by FDA > OTC Drug 6. Nasal Spray Decongestants
Monographs  Similar to OD
- TEMPORARY RELIEF ONLY  Acting only in the area applied
- NOT FOR LONG-TERM  Usually without the stimulat
USE/TREATMENT OF CHRONIC side effects
CONDITIONS 7. Diphenhydramine
DEFINITION OF TERMS  Antihistamine
CHEMICAL COMPOSITION OF OTCs  Treats sneezing, runny nose,
Active ingredients & other components that watery eyes
make up the medication 8. Calcium Carbonate
PHYSICAL PROPERTIES  Antacids that work
Refers to the FORM IN WHICH THE immediately to relieve acid
MEDICATION IS PRESENTED indigestion and heartburn
- Tablets, capsules, liquids, dissolvable  Chewable tablets and liquid
tablets forms
- Packaging  HOWEVER, aluminum-based
THERAPEUTIC EFFECTS antacids may cause constipation
Intended purpose of medication (i.e. relieving and magnesium based products
pain, reducing fever, etc.) can cause diarrhea
EXAMPLES 9. Medications for Constipation
1. Acetaminophen  Relieve constipation
 For fever  Include glycerin suppositories
 Minor aches and pains, that help in bulking-up and
especially for people who can’t lubricating stool
tolerate anti-inflammatory meds 10. Loperamide
like ibuprofen/aspirin  Treatment for diarrhea
2. Non-steroidal Anti-inflammaroty  HOWEVER, if constipation,
Drugs (NSAIDs) ileus, fever, or bleeding occurs
 Inflammation, fever, pain > STOP THE USE OF THIS
3. Dextromethrophan OTC
 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

 9 CONCHEM 4TH QUARTER

PRESCRIPTION DRUGS  Treats ear, throat, sinus

- Prescribed by a doctor infections, pneumonia,
- Bought at pharmacys bronchitis, and some STDs
- Intended for one person only 6. Metformin
- Regulated by FDA through the New  Used alone or in combo with
Drug Application (NDA) process other drugs
EXAMPLES OF PD  Treats type 2 diabetes in adults
1. Vicodin and children
 Popular drug for treating  Side effects: nausea, vomiting,
acute/chronic moderate to gas, bloating, loss of apetite
moderately severe pain 7. Lipitor
2. Simvastatin  Treats high cholesterol
 One of the first “statins” (HMG-  Prevents chest pain, stroke,
CoA reductase inhibitors) heart attack in individuals with
approved for: Coronary artery disease
 TREATS HIGH  THESE ARE NOT FOR
CHOLESTEROL AND EVERYONE
REDUCING RISK OF o People who are allergic to
STROKE, DEATH FROM Lipitor
HEART DISEASE, AND RISK o Women who are
OF HEART ATTACKS nursing/pregnant
3. LISINOPRIL  Side effects: diarrhea, upset
 ACE inhibitor stomach, muscle, and joint pain
 Treats high blood pressure, 8. Amlodipine
congestive heart failure,  Calcium channel blocker
 Prevents kidney failure from  Treats high blood pressure and
blood pressure and diabetes prevention of chest pain
 Can be taken with or without  Lowers BP by Relaxes blood
food as prescribed by the doctor vessels so that the heart does not
and has to be used regularly to have to work too much
take full effect  Controls chest pain by
4. Levothyroxine increasing blood supply to the
 Man-made version of thyroid heart
hormone  Comes in tablet and
 Treats hyperthyroidism suspension(liquid)
o Condition wherein the  Side effects: head aches and
thyroid gland does not swelling of lower extremities
produce enough thyroid 9. Amoxicillin
hormones for the body  Penicillin type antibiotic
o Thyroid is inactive  Treats bacterial infections like
 Brand names: Levoxyl, ear, tonsils, throat, larynx,
Synthroid, Unithroid urinary tract, and skin infections
 Available in Oral  WILL NOT WORK for VIRAL
tablet, oral capsule, INFECTIONS (cold, flu etc)
injectable solution  Using antibiotics when not
5. Azithromycin needed will cause drug
 Antibiotic resistance

**TM – THERAPEUTIC MEDICINE

 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

 1
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

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
Normal tissue spread to the rest of the
 There is a balance between the body
generation of new cells via cell
division and loss of cells
through cell death
 Old cells become damaged and METASTASIS
undergo apoptosis (form of - Spread of cancer to diff. parts of the
programmed cell death) body (usually to bones, liver, or lungs)
through the lymph system/bloodsystem

**TM – THERAPEUTIC MEDICINE

 1
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, Smoking AND obesity are both

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

**TM – THERAPEUTIC MEDICINE

 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 >

**TM – THERAPEUTIC MEDICINE

 1
5 CONCHEM 4TH QUARTER

 Binds with DNA and preventing

RNA synthesis (necessary for cell
survival)

**TM – THERAPEUTIC MEDICINE