Understanding drugs & medicines
• is a word derived from a French word ‘Drogue’ which means dry herb.
• Any substance that brings about a change in biologic
function through its chemical action
• Alters state in the body
• can’t create new function but alter existing function
• Are poisons if they used irrationally
Nutrition
• The process of taking in food and using it for
growth, metabolism, and repair. Nutritional
stages are ingestion, digestion, absorption,
transport, assimilation, and excretion
DRUG NAMES
• Every drug has at least three names—a chemical
name, a generic (nonproprietary or official) name,
and a trade (proprietary or brand) name.
• The chemical name describes the atomic or molecular
structure of the drug. This name is usually too
complex and cumbersome for general use.
• So an official body assigns a generic name to a drug.
The generic names for drugs of a particular type
(class) usually have the same ending.
• For example, the names of all beta-blockers, which
are used to treat such disorders as high blood
pressure, end in "lol."
The trade name/proprietary name is chosen by the
pharmaceutical company that manufactures or
distributes the drug.
Patented drugs are usually sold under a trade name.
Generic versions of trade-name drugs—manufactured
after expiration of the pharmaceutical company's
patent—may be sold under the generic name (for
example, ibuprofen) or under the manufacturer's own
trade name (for example, Advil).
• Active ingredient- chemical component that
gives a medicine its action.
• Drug interaction- when a drug reacts with
another drug, food, or dietary supplement such
that the effect of one of the substances is
greater or smaller
DRUG GROUPS
Understanding what group a drug belongs to is also
useful.
Broadly, drugs are classified by therapeutic group—that
is, by what disorder or symptom they are used to treat.
For example, drugs used to treat
high blood pressure are called antihypertensive, and
drugs used to treat nausea are called antiemetic (emesis is
the medical term for vomiting).
Within each therapeutic group, drugs are categorized by
classes. Some classes are based on how the drugs work
in the body to produce their effect.
For example, diuretics, calcium channel blockers, beta-
blockers, and angiotensin-converting enzyme (ACE)
inhibitors are all classes of antihypertensives that work
differently.
DRUG USAGES
• Drugs have 3 medical uses.
• Therapeutic use: Drugs are used to control, improve
or cure symptoms, conditions or diseases of a
physiological or psychological nature. E.g of the
therapeutic use of drugs include the following:
Antibiotics to kill the bacteria that cause an infection
Analgesics to control the pain and inflammation of
arthritis
Hormone replacement therapy for the symptoms of
menopause
• Preventive use: Drugs are used to prevent the
occurrence of symptoms, conditions or diseases. e.g
of the preventive use of drugs include the following
• Vaccination for immunization against childhood
diseases.
• Drugs taken to prevent motion sickness prior to flying
on an aeroplane.
• Diagnostic use: Drugs are used by themselves or in
conjunction with radiological procedures and other
types of medical tests to provide evidence of a disease
process.
e.g. Radiopaque dyes used during x-ray procedures
• Drugs given to stimulate cardiac exercise in patients
who cannot undergo regular exercise stress testing
Sources of drugs.
• Drugs are obtained from various sources. According to sources they are:-
1. Natural drugs
A/ Plants
E.g. .Digoxin from Digitalis purpurea
.Atropine from Atropa belladonna
.Quinine from Cinchona officinalis
B/ Animals
[Link] liver oil from Cod fish liver.
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C/ Minerals
E.g.. Iron, Iodine, Potassium salts.
D/ Micro – organisms
E.g. .Penicillin from penicillium
notatum.
.Chloramphenicol from Streptomyces
venezuelae (Actinomycetes).
2. Synthetic drugs
- prepared by chemical synthesis in pharmaceutical
laboratories
E.g.. Sulphonamides, quinolones,
barbiturates
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3. Semisynthetic drugs
- prepared by chemical modification of natural drugs.
E.g.. Ampicillin from penicillin G.
.Dihydroergotamine from ergotamine.
4. Biosynthetic drugs
- prepared by cloning of human DNA in to the bacteria
like [Link].
E.g.. Human insulin.
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Pharmacokinetics
Pharmacokinetics and Dosage Regimens Determine:
How much drug is in the body at any given time
How long it takes to reach a constant level of drug in the body
during chronic drug administration.
How long it takes for the body to rid itself of drug once intake
of drug has stopped
Pk principles
In practical therapeutics, a drug should be able to reach its
intended site of action after administration by some convenient
route. So,drug should be
absorbed into the blood from its site of administration
distributed to its site of action, permeating through the various
barriers that separate these compartments
After bring about its effect, a drug should be eliminated at a
reasonable rate
-by metabolic inactivation or
-by excretion from the body, or by a combination of these processes
Drug at site of
administration
Absorption
Distribution Metabolism
Drug in Drug /
plasma metabolites
in tissues
Liver
Drug /
metabolites in
urine, feces, bile
Kidney
Elimination
Conc
1,000
Half-life (plural half-lives)
t1/2
500
What is the percentage of drug left after 4.5
hours if its half-life is 1.5 hours?
250
125
1 2 3
Half-life
absorption
• The transfer of substances from sites of
administration to sc.
• Drugs get absorbed to systemic circulation after
crossing different barriers
-orally mucous membrane of gut
capillary membrane of BV
-injections capillary membrane of BV
Mechanisms by which Drugs Cross
Biological Membranes……..Cont
Passive Diffusion:
• Vast majority of drugs cross membranes by passive
diffusion
• Most lipid soluble drugs readily move across
membranes (lipid diffusion)
• Drug moves across membranes according to
concentration gradient
• No carrier is involved
• Not saturable
• Low structural specificity
Mechanisms by which Drugs Cross
Biological Membranes……..Cont
Passive Diffusion…cont:
• Water-soluble drugs (MW 20,000 – 30,000) cross
membrane through aqueous channels or pores
(Aqueous diffusion)
• Drugs bound to large molecules such as albumin do
not penetrate aqueous pores.
• The capillaries of the brain and testes are
characterized by absence of pores that permit
aqueous diffusion of many drug molecules into the
tissues (protection)
Mechanisms by which Drugs Cross
Biological Membranes……..Cont
Active transport:
• Involves specific carrier protein
• A few drugs that closely resemble the structure of
naturally occurring metabolites (structural
specificity)
• Involves energy expenditure
• Drugs can move against concentration gradient
• Saturable
Mechanisms by which Drugs Cross
Biological Membranes……..Cont
Endocytosis and Exocytosis:
• For large molecules
• Substance is engulfed by the cell membrane and
carried into the cell by pinching off of the newly
formed vesicle inside the membrane
• The substance can then be released inside the cytosol
by breakdown of the vesicle membrane
• Iron and vitamin B12
• Exocytosis is a reverse process for the excretion of
some substances outside the cell
ROUTES OF DRUG
When does a drug exert its
pharmacological effect?
Reach the site of action
Major routes
Enteral Parenteral Topical
Conjunctival,Nasal
Oral Injections ,Auditory
,Mucosal
Sublingual Inhalation Vaginal and
Urethral
Inunction and
Rectal Transdermal
Dermal
Commonly Used Routes of Drug
Administration
FACTORS GOVERNING CHOICE OF
ROUTE
• Physical & chemical properties of drug
• Rate & extent of absorption from
various routes
• Effect of digestive juices & first pass
effect
• Site of desired action
• Rapidity of the desired response
• Accuracy of dosage
• Condition of the patient
Enteral
• Enteron -intestine
• Placement of drug into any
part of GIT
ORAL=MOUTH
ADVANTAGES DISADVANTAGES
•Safe •Slow absorption
•Convenient •Slow action
•Economical •Irritable and
•Usually good unpalatable drugs
absorption •Unco-operative and
•Can be self unconscious patients
administered •Some drugs
•Painless destroyed
•First-pass effect
First pass effect:
Examples
• Solid- Tablet, Capsule, Powder
• Liquid- Syrup, Elixir, Mixture
Sublingual and Buccal
Sublingual :beneath the tongue
Buccal: Crushed and spread over buccal
mucosa
SUBLINGUAL ROUTE
ADVANTAGES DISADVANTAGES
•Economical •Unpalatable &
•Drug absorption is bitter drugs
quick •Irritation of oral
•First-pass avoided mucosa
•Quick termination- •Large quantities
Spit off not given
•Can be self •HMW drugs not
absorbed
administered
Example
• Systemic use
–Isosorbide dinitrate
–Nitroglycerine
–Nifedipine
• Local
–Antispetic lozenge
RECTAL ROUTE-RECTUM
ADVANTAGES DISADVANTAGES
Used in children Embarrassing
Little or no first pass Inconvenient
effect Absorption is
Used in slow and erratic
vomiting/unconscious Irritation or
Higher inflammation of
concentrations rapidly rectal mucosa can
achieved occur
Can use gastric
irritants
Prepackaged enema container
Example
• Local Effects
– Dulcolax, Glycerine suppository, enema,
ointment
• Systemic Effects
– Aminophylline, Indomethacin, suppositories
Gastric Tube Administration
• Gastric tubes provide access directly
to the GI system.
Confirm proper tube placement.
Withdraw the plunger while observing for the
presence of gastric fluid or contents.
Instill the medication into the gastric tube.
Gently inject the saline.
Clamp off the distal tube.
Parenteral Routes
Routes
other than
enteral are
called
parenteral
Administration of drugs by
the parenteral route
Intradermal
• Intradermal- outer layers
• Amount of drug small, slow
absorption
• Tuberculin syringe
• Example: BCG vaccine, diagnostic
tests, allergic sensation testing
Subcutaneous administration
Site: Injection under skin
Merits Demerits
• Smooth but slow • small volume(1 ml)
absorption • irritant drugs-
• depot sloughing and
injections/implants necrosis
• Examples • not suitable in shock
– Local-local
anaesthetic
– Systemic-Insulin
Intramuscular Injections
• Site-Deltoid muscle, Gluteus, Vastus
Intramuscular route
ADVANTAGES DISADVANTAGES
•Absorption •Only up to 10ml drug
reasonably uniform given
•Rapid onset of •Local pain and
action abscess
•Mild irritants can •Expensive
be given •Infection
•First pass avoided •Nerve damage
•Gastric factors can
be avoided
Intravenous Administration
Merits Demerits
• Bypass first pass • Antiseptic conditions
metabolism(100%) • Depend on others
• Quick onset of action • Painful and risky-cant be
• In uncooperative and recalled
unconscious patients • Embolism
• those with nausea and • Suspensions/oily
drugs/depots cant be
vomiting
given
• hypertonic solutions and • Venous thrombosis and
irritants phlebitis
• large volumes • Necrosis due to
• amount of drug can be extravasation
controlled accurately
Examples
• IV infusion- Ringer, Dextrose
5%,DNS,Dopamine
• IV bolus- Diazepam, Adenosine,
Insulin
Intra-arterial
• Site: Lumen of artery
• Merits: Greater concentration of the
drug can be delivered
• Demerits: Expertise and asepsis
• Examples: Radiopaque contrast for
coronary angiography and cerebral
angiography
Intraperitoneal
• Site-Peritoneal space
• Merits-Rapid absorption-large surface
area
• Demerits-
Painful,Risky,Adhesions,Peritonitis
• Example: Dialysing fluid-poisoning and
renal failure
• In lab animals
Intrathecal (Intraspinal)
• Site: Subarachanoid space
• Merits: Bypass blood brain barrier and
blood CSF barrier-acts directly on
meninges and spinal cord
• Demerits- Asepsis, Expertise, Painful,
Risky
• Example: Radioopaque contrast media,
Xylocaine injection
Epidural
• Through vertebral interspace
between dura and lining of spinal
canal
• Example: Xylocaine injection
Intramedullary
Site: Tibial or Sternal bone marrow
Merits: onset of action very fast
Demerits: Strict aseptic conditions,
expertise and skill required
Painful and risky
Examples: Bone Marrow
transplantation
Intraarticular
• Site: Injection directly into the joint space
• Merit: High concentration in localised area
• Demerits: Asepsis, Joint damage, Pain
• Examples: Hydrocortisone, Gold chloride for
rheumatoid arthritis
Intracardiac injection
• Left fourth intercostal space into
heart muscle
• Eg Adrenaline injection-cardiac arrest
Inhalation
• Site: Inspiration nose/mouth
• Merits: fast, quick-large surface
area, self
• Demerits: increased bronchial and
salivary secretions
• Examples: Salbutamol ,Na
cromoglycate –Metered dose
inhalers
Intranasal
• drugs directly into the nose.
•Desmopressin is administered
intranasally in the treatment of
diabetes insipidus
•Salmon calcitonin- osteoporosis
•GnRH aanalogues
TOPICAL OR LOCAL ROUTE
• Mucous membrane of eye, ear, nose throat, mouth
urinary bladder, vagina and rectum
• Ointments, creams ,lotions and powders used
Topical
• Conjunctival, Nasal ,Auditory Mucosal
– drops, sprays
• Vaginal and urethral
– Solutions, ointment ,emulsions, suppositories,
pessary,pencil shaped bougie
• Inunction and dermal
– Rubbing into skin
– Dust/spray