3. Learning outcome
• Define the terms
• Pharmacology
• Pharmacokinetics
• Pharmacodynamics
• List the various routes of administration of drugs.
• Advantages & disadvantages
• Onset of effect
4. Definition of Pharmacology
• What is Pharmacology?
• Greek words
PHARMACON + LOGOS
(Drugs/ medicine) (Study of)
PHARMACOLOGY
The study of substance (drug) that interact with living
systems through chemical processes, especially by binding to
regulatory molecules & activating or inhibiting normal body
processes (Katzung et al., 2009)
4
5. What the human body do to the
drugs
(dose-concentration)
What the drugs do to the human
body
(concentration- effect)
the kinetics of drug
Absorption, Distribution, Metabolism
and Elimination (excretion)
study of the action or effect of
drugs on living organism and their
mechanism of action in the body
Major areas of study in
Pharmacology
5
6. Major areas of study in Pharmacology
Drug indications and application
Drug interactions
Unwanted (adverse) effects
6
8. • Medication: substance administered for diagnosis, cure, treatment,
mitigation or prevention.
• Pharmaceutics: large scale manufacture of drugs, drug dosage,
formulation
• Therapeutic effect: primary effect intended that is the reason the drug
is prescribed such as morphine sulfate is analgesia
• Side effect: secondary effect of the drug is one that unintended, side
effects are usually predictable and may be either harmless
9. • Drug toxicity: deleterious effect of the drug on an organism or tissue, result
from overdose or external use.
• Drug allergy: immunological reaction to a drug.
• Drug interaction: occur when administration of one drug before or after
alter effect of one or both drug.
• Drug abuse: inappropriate intake of substance either continually or
periodically.
• Drug dependence: persons reliance on or need to take drug or substance
10. • Illicit drug/street drug: Those drugs that sold illegally.
• Pharmacotherapeutics: clinical using of drug for therapeutic.
• Adverse drug reactions (ADR): harmful or unpleasant reaction,
resulting from an intervention related to the use of a medicinal
product
• Pharmacognosy: study of natural (plant and animal) drug sources.
11.
12. What is
DRUG?
“ Drug is any substance or product
that is used or is intended to be used
to modify physiological systems or
pathological states for the benefit of
the recipient .”
What is consider as a drug?
Hormones
Neurotransmitters
Growth factors
Drugs (Pharmaceuticals)
Toxic agents in the environment
13. THINK: A drug with potent cytotoxic,
can it become a good medicine? Why?
"Poisons in small doses are the best
medicines, and the best medicine in too
large doses are poisonous,"- William
Withering.
.
23. Drug Nomenclature
Naming system
At least THREE names
Chemical
•Scientific name
•Long name – atomic &
molecular structure (for chemist)
•Not used by general public/
prescribing
Proprietary
Brand name (manufacturer)
1 type of drug may have several
brand names with ® symbol
Manufacturers property
Non-proprietary
Generic name
A standard name accepted
around the world with an
agreement from WHO
(International Non-proprietary
Name (INN)
Remains the same worldwide
24. Fepril ® and Panamol® : two branded products containing paracetamol produced by different
manufacturer
25. Generic name is usually written below the brand name
of the drug package
26. Universal
harmonizatio
n with
common root
name or
ending
Standardized drug affixes
Stem Drug class Example
-cillin Penicillin-derived
antibiotics
Penicillin, carbenicillin,
oxacillin
-oxacin Quinolone-derived
antibiotics
Levofloxacin
-prazole Proton-pump inhibitor Omeprazole
-sartan Angiotensin receptor
antagonist
Valsartan
-vastatin HMG-CoA reductase
inhibitor (Statin)
Atorvastatin
-vir Antiviral drugs Indinavir
28. Dose and
dosage
• Quantity of drug administered
at 1 time
• 500mg of Paracetamol (PCM)
Dose
• Size and frequency
• The amount of drug that
should be given over time
• 500mg of PCM for 3 days
Dosage
29. Drug Dosage
forms
Dosage forms are the means ( or the form ) by
which drug molecules are delivered to sites of
action within the body.
30. Pharmaceutical Dosage Form/ Drug Delivery System (according to its physical
properties)
Gases
• Gases,
Aerodispersion
• Solid particles (e.g:
inhalation,
antiasthmatics)
• Liquid particles
(inhalation,
antiasthmatics or
sprays
Liquids
• Solution
• Oral, sterile
solution
(injections)
• Emulsions
• Suspensions
• Syrups
Semisolid
• Unshaped (no
specific physical
shaped)
• Gels
• Creams
• Ointments
• Pastes
• Shaped
• Suppositories (for
rectal
administration)
• Pessaries (vaginal
suppositories)
Solid
• Unshaped
• Powders for
external/internal
use
• Shaped
• Tablets
• Capsules
• Implantates
• Transdermal
patches
31. Ingredients in dosage forms
• Active ingredients
• Paracetamol 500mg –
acetaminophen 500mg
• Inactive substances (excipients)
• Binding agents
• stick and clump powder
• Lactose, cellulose, gelatine
• Disintegrating agents – expand
when exposed to damp spaces
• Drugs to break up – release of
active ingredients for absorption, if
not straight go to stools
• Coating agents – cellulose,
gelatine
• Protect content from moisture
• Reduce the taste of bitterness
• Lubricants
• Tablets or capsule so they didn’t
stick to each other
• Silica, vegetable fat, talcum powder
(magnesium silicate)
• Filler
• Add bulk to pills and capsule for
easy manufacturing
• Flavouring agent
• Preservatives
• Vit A, C, E, selenium (antioxidants
act as natural preservatives)
• Paraben, methylparaben
32. Route of administration
The way through drug is
administered into the body for
the treatment of various
diseases and disorders
34. Route of Administration (ROA)?
Chosen ROA will have a
profound effect upon the
speed and efficiency with
which the drug acts
Influence bioavailability
Bioavailability -
measurement of the
rate and extent of active
drug that becomes
available at the site of
action (the
completeness of
absorption into the
systemic circulation).
Drug must enter the blood
circulation for them to
exert a systemic effect
Drug must be unchanged and
active in target site
Unbound with any other
molecules
possible routes of drug
entry
Enteral
• Through alimentary canal
or digestive system
Parenteral
• Other than through
alimentary canal or
digestive system
• Injections
Others
• Topical/ local
• Inhalation
35. ROA : ORAL
• most common
• Advantage:
• • inexpensive
• • convenient
• • Safe, does not break the skin
• • Conscious, able to swallow
• Disadvantage:
• • inappropriate for nausea and vomiting
• • unpleasant taste.
• • irritation of gastrointestinal tract
36. ROA : SUBLINGUAL
• a drug placed under the tongue, where it dissolved.
• Advantage:
• • rapidly absorbed into blood stream. • More potent than
oral.
• • Effect faster than oral
• Disadvantage:
• • swallowed may be inactive. • must remain under the
tongue until dissolved.
• WHY FASTER THAN ORAL ROA?
37. ROA : BUCCAL
• Between the gums or inner lining of the cheek.
• Absorbed by buccal mucosa.
• Advantage:
• • Avoid first pass effect • Rapid absorption • Drug
stability
• Disadvantage: • swallowed may be inactive. •
Inconvenient • Small dose limit
38. ROA: RECTAL
• solid or liquid dosage forms (suppository or enema)
• either local or systemic drug delivery.
• Advantage: • Used in children • Little or no first pass effect •
Used in vomiting or unconscious • Higher concentration drug
• Disadvantage: • Slow absorption • Inconvenient • Irritation or
inflammation of rectal mucosa
39. Parenteral (Par-beyond enteral-intestine)
• directly to target tissues
• across body barriers
• straight to systemic circulations
• Used for
• drugs that are poorly absorbed (e.g. Heparin) and unstable in
GIT (e.g insulin)
• treatment of unconscious patient
• under circumstances that require rapid onset of action
• highest bioavailability
• No first pass metabolism or harsh GIT environments
• most controlled of the drug dosages – ADMINISTERED = ABSORBED
• Disadvantage – dosages of the drug administered are not
reversible and may cause pain, fear and infections
• 4 major types :
40. 1. Intravenous (IV)
• Injection directly into the vein
• three ways
• IV push/bolus – injecting a single dose of drug
directly into the vein
• IV drip – mixing the drug with fluid in an IV bag or
bottle
• IV piggyback- mixing the drug in a very small IV
bag
• advantage: • Bioavailability 100% • Large
quantities • for vomit and nausea patient •
Emergency, fast onset desired
• Disadvantage: • Technical assistance required •
Danger and infection • Less convenient and painful
41. 2. Intramuscular (IM)
• injected into a muscle mass - well supplied with blood vessels
• Incorrect method leads to blood vessel nerve damage.
• Advantage: • Absorption uniform • Rapid onset of effect > subcutaneous • No first
pass effect
• Disadvantage: • Infection • Painful • Less volume compared to IV
42. 3. Subcutaneous (SC)
Injection
• Injection of a liquid into the
fatty layer of tissue just below
the dermis of the skin but
above the muscle layer
• Example : insulin injection for
the management of diabetes
• Advantage: • Slow onset of
action • Effect faster than oral
• Self administered
• Disadvantage: • Slow
absorption, slow onset • Small
volume 0.5-1.0 mL
43. 4. Intradermal
Injection
• Injection of a liquid into the dermis, just below the epidermis;
when correctly administered the tip of the needle is still visible
through the skin
• Example : Mantoux screening test for TB consists of an intradermal
injection of one-tenth of a milliliter (ml) of PPD tuberculin
OPC20102
44. 5. Intrathecal Injection
• Directly into the cerebrospinal fluid, injection
into the spinal canal
• Provides access to the central nervous system
• drugs that are normally excluded by the blood
brain barrier
• Useful in spinal anesthesia, chemotherapy, or
pain management applications.
• Example: administration of amphotericin B for
the treatment of cryptococcal meningitis
• * involves a very high risks of neurotoxicity and
this route should never be used without
adequate training
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45. Others:
1.Inhalation
• inhaling a drug in gas or liquid form;
• drug absorbed through alveoli of the lungs
• gases or aerosol forms
• for patients with respiratory problems such as asthma or COPD
• Advantages:
• Rapid absorption and rapid onset of activity (as rapid as IV
injections) (e.g. Bronchodilators)
• Avoidance of first-pass effects of metabolism prior to
systemic absorption
• Localization of drug activity to the lung and systemic side
effects are minimized
• Disadvantages
• Difficulties in regulating the exact amount of dosage.
• Patient having difficulties giving themselves a drug by inhaler
46. 2. Topical
• Applied directly to the skin or the mucous membranes of the eye, ear,
nose or mouth
• When a local effect of the drug is desired (not systemic effect)
• Example:
• Timoptic eye drops
• Tropicamide – used drop by drop directly into the eye to dilate the
pupil and permit measurement of refractive errors
OPC20102
47. 3. Transdermal
• Transdermal administration delivers a drug into the patient’s
systemic circulation through the skin for systemic activity.
• Rate of absorption can vary markedly, depending on the
physical characteristics of the skin and the site of application
• Most often used for sustained drug delivery (drug is delivered
over several hours or days without the discomforts of GIT side
effects or 1st pass effects
• Example:
• Nitroglycerin transdermal patch for relieving angina attack
• Scopolamine – delivered through the skin of the ear for relief of motion
sickness
48. 4. Intranasal
• Administration of drug directly into
the nose
• Example:
• nasal decongestant such as anti-
inflammatory corticosteroids
50. Which route of administration can
by pass the FIRST PASS
EFFECT?
PARENTERAL
51. Fast absorption means the area
of administration must be
nourish/supply with …..
BLOOD VESSEL
52. Which route of administration has
slow absorption?
Orally
Topical
Intradermal
rectally
53. Which route of administration has
fast absorption?
Intravenous
Intramuscular
Intraperitoneal
Inhalation
54. Ingestion of drugs with food or in combination with other drugs can influence absorption.
Some drugs are destroyed by stomach acid
Presence of food delayed absorption
Editor's Notes
Pharmacology has been defined as an experimental science that studies changes brought about in vivo and in vitro by chemically acting substances, whether
used for therapeutic purposes or not.
May and may not. Because they might cause intolerable side-effects or death
Antiarrhythmic - suppress abnormal rhythms of the heart (cardiac arrhythmias)
William Withering FRS (17 March 1741 – 6 October 1799) was an English botanist, geologist, chemist, physician and the discoverer of digitalis.
Morphine was first derived from opium by a 20-year-old German pharmacist assistant name Friedrich Setürner in 1806. He named the drug morphium after Morpheus, the Greek god of dreams, and ran experiments on himself, describing the curative, euphoric and "terrible" aspects of the drug
The power, potency and agony of morphine, and later heroin, was dramatically increased with introduction of the hypodermic needle.
In 19th century United States and Europe, morphine was legal and easy to get a hold of .
Increase pupil size, beautiful lady, rennasaince (14th -17th century)
During the Renaissance, Italian women put drops made from Belladonna in their eyes. The drops made their pupils dilate, which they believed made them more alluring.
Drugs are compound into various types of preparations depending upon the physical characteristics of the drugs, the purpose for which intended, and the method by which they are to be administered. Some drugs are prepared in more than one form and may therefore be administered in several ways.
Solid Preparations. (1) Powder. A drug that is ground up and used in powder form. (2) Capsule. A drug placed in a gelatin container. (3) Tablet. A molded or compressed solid mass of one or more medicinal
substances, often diluted and bound together by other ingredients. The shape, usually discoid, may vary considerably from one tablet to another. Caplet : A caplet is shaped like a capsule but has the form of a tablet. The shape and film-coated covering make swallowing easier. Powder A drug that is dried and ground into fine particles is called a powder. Granule A small pill, usually accompanied by many others most commonly encased within a gelatin capsule is called a granule.
Suppository. A drug that is molded into shape for insertion in a body opening and which melts or dissolves at body temperature.
Ointment. A drug suspended in lard, Vaseline, lanolin, or other solid or semisolid base, intended for external application
Fluid Preparations. Fluid drugs for oral and external use are packaged in bottles; those for injection are packaged sterile in vials or ampules. (1) Fluidextracts. Alcoholic or hydroalcoholic solutions of the active constituents of vegetable drugs. They are usually prepared so that each milliliter of the finished preparation contains the extractive from 1 gm of the crude drug. These drugs should be kept in dark bottles because many of them precipitate in light. They are not to be used if precipitate has formed. (2) Spirit. An alcoholic solution of volatile substances. (3) Elixir. A solution containing alcohol, sugar, and flavoring substance in which one or more drugs may be dissolved. (4) Tincture. Alcoholic or hydroalcoholic solution or obstruction of a drug. Tinctures of potent drugs are 10 percent in strength; of most other drugs, 20 percent in strength. (5) Emulsion. A mixture of two liquids, usually oil and water, one of which is dispersed as droplets in the other. Any emulsion should have a "SHAKE WELL" label
on the container. (6) Suspension. A liquid preparation containing un-dissolved material. A "SHAKE WELL" label is applied to the container. (7) Syrup. A highly concentrated sugar solution containing a flavoring agent
into which a drug may be incorporated. (8) Liniment. A solution of drugs in a soapy, oily, or alcoholic base,
intended for external application with friction. (9) Lotion. An aqueous preparation, usually containing suspended insoluble matter, to be applied externally. A "SHAKE WELL" label should be on the container.
Suppository
A bullet-shaped dosage form intended to be inserted into a body orifice is called a suppository. Suppositories contain medication usually intended for a local effect at the site of insertion. Suppositories maintain their shape at room temperature but melt or dissolve when inserted. The most common sites of administration for suppositories are the rectum, vagina, and urethra.
Ointment
An ointment is a semisolid, greasy medication intended for external
application, usually by rubbing . Medications that may be administered in ointment form include anti-inflammatory drugs, topical anesthetics, and antibiotics. Examples are zinc oxide ointment and Ben-Gay®ointment.
Tincture
A tincture is an alcoholic preparation of a soluble drug, usually from plant sources. In some cases, the solution may also contain water (e.g., iodine tincture, digitalis tincture).
Elixir
A drug vehicle that consists of water, alcohol, and sugar is known as an elixir. It may or may not be aromatic and may or may not have active
Syrup
A drug dosage form that consists of a high concentration of a sugar in water is called a syrup. It may or may not have medicinal substances added (e.g., simple syrup, ipecac syrup).
Solution
A solution is a drug or drugs dissolved in an appropriate solvent. An example of a solution is normal saline, which is salt dissolved in water.
Spirit
An alcohol-containing liquid that may be used pharmaceutically as a solvent is called a spirit. It is also known as essence (e.g., essence of peppermint, camphor spirit).
Enteric - relating to or occurring in the intestines.
Injected into the vein. This allows for immediate adsorption. Intravenous includes IV push, IV piggyback and IV infusion or drip
Different muscle tissues have different blood flow. For example, blood flow to the deltoid (shoulder) muscle is higher than blood flow to the gluteus (bum) muscle.
Intramuscular injections may be formulated to have a faster or slower drug release by changing the vehicle of the injection preparation.
Aqueous, viscous, oily, or suspension vehicle may affect drug release and drug absorption. A change in a parenteral drug product from a solution to an emulsion, liposome, etc, will alter the drug's distribution and pharmacokinetic profile.
Injected into the fatty layer under the skin.
injected into the top layer of the skin at a slight angle.
This intradermal injection is termed the Mantoux technique. A person who has been exposed to the bacteria is expected to mount an immune response in the skin containing the bacterial proteins.
The reaction is read by measuring the diameter of induration (palpable raised, hardened area) across the forearm (perpendicular to the long axis) in millimeters. If there is no induration, the result should be recorded as "0 mm". Erythema(redness) should not be measured.
Injected into the space surrounding the spinal cord.
Inhalation routes of administration are inhaled through the mouth or the nose and usually act directly on the respiratory system before entering into the bloodstream. They are often used to treat respiratory diseases, but gases are inhaled for general anesthesia as well.
