Intro To Pharmacology
Intro To Pharmacology
WHAT IS PHARMACOLOGY?
Pharmacology includes:
1. Pharmacokinetics: the study of the characteristics of the time course and extent of drug exposure in
individuals and populations and deals with the absorption, distribution, metabolism and excretion
(ADME) of drugs. It has been described as “what the body does to the drug.”
2. Pharmocodynamics: is the study of the biochemical and physiological effects of drugs, their modes
of action and the relationship between drug concentration and effect. It has been described as ‘what
the drug does to the body’. An understanding of pharmacodynamics forms the foundation of rational
therapeutic drug use and provides insights into improved dosage regimens and possible drug
interactions as well as the design of new drugs.
3. Toxicology: is the branch of pharmacology that deals with the undesirable effects of chemicals on
living systems, from individual cells to humans to complex ecosystems; study of poisons, including
their chemical properties and biological effects
4. Pharmacotherapeutics: refers to the application of drugs for use in the diagnosis, prevention, and
treatment of diseases, induction of anesthesia and synchronization of uterus in farm animals. It
includes drug of choice,, route of administration, forms of drugs and frequency of administration.
5. Pharmacy: the art and science of preparing, compounding and dispensing of drugs
a. Pharmacognosy: study of source of drugs; study of medicinal drugs obtained from plants or
other natural sources
b. Posology: study of drug dosage
c. Metrology: deals with weight and masses as applied to preparation and administration of drugs
• Dose: quantity of medicine to the administered at one time; amount of drug received per
animal.
• Dosage: amount of drug per unit of animal mass of weight; can also be expressed as the
amount ofdrug per unit of mass or weight per unit of time (example, 50 mg/kg/day for one
week)
Categories of Pharmacology
1. Molecular Pharmacology: concerned with the study of basic mechanism of drug action in biological
system aims to determine and interpret the relationship between biologic activity and the structure of
molecules or group of molecules .
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2. Clinical Pharmacology: concerned with the rational development, effective use,and then proper
evaluation of drugs for the diagnosis, prevention and care of diseases also deals with the safe use of
drugs in any animal species including human being; devoted to the study of the clinical effects of drugs on
patients with a goal of optimizing therapeutic dosage regimens.
Clinical pharmacology in the veterinary setting is the clinical discipline devoted to the optimal use of drugs
in veterinary patients, maximizing their prophylactic or therapeutic benefi ts while ensuring that the
adverse consequences of drug use are minimized.
3. Veterinary Pharmacology: concerned with drugs as they are used in the diagnosis and treatment of
animal disease, and in the intention alteration of animal physiology. The range of animal species in which
drugs are used and studied distinguishes Veterinary Pharmacology from, medical (human) Pharmacology
4. Pharmacogenomics: the relation of the individual’s genetic makeup to his or her response to specific
drugs
Since the dawn of humankind, mixtures of animal parts, plants and minerals to treat wounds, sores
and ailments evolved from rudimentary pharmacological compounds into more sophisticated experiments to
create medical treatments. Egypt first documented herbal amalgams for healing. Archives of ancient Greek
texts reveal the extent of their medicinal knowledge of herbal mixtures. Chinese and Arab peoples advanced
pharmacology research of herbal and mineral benefits for medical treatments as well. Early in the 20th
century, modern pharmacology emerged with the first synthetic compound created in Europe.
Prehistoric: Knowledge of pharmacology practiced by humans before the Egyptian and Greek writings
comes from archaeological findings. Because prehistoric humans had no understanding of the inner workings
of the human body, pharmacology was a rational application of what they could see. These early people
treated wounds, burns and broken bones with plants and locally gathered materials to assist in the healing.
The Medical Book of Thoth: Ancient Egyptian life evolved around their many gods. Thoth, the
Egyptian Goddess of knowledge, left 42 books directing how Egyptians should live. Among these records, one
specifically provides cures from plant and animal mixtures for human ailments. Court records from Egypt's
18th Dynasty (1550 to 1292 B.C.E.) are the first known reference to this tome.
Ebers Papyrus: The Ebers papyrus, the world's oldest preserved medical and pharmacological
record, is believed to be a copy of the book of Thoth. It measures nearly 20.23 m in length and 30 cm in
height. The 110-page scroll from 1552 B.C.E. contains 700 medical and pharmacological recipes for
treatments from crocodile bites to intestinal afflictions as well as diabetes and arthritis.
China: Shen Nong recorded hundreds of Chinese medicinal herbs over 4,000 years ago. Included in
China's Shen Nong's "The Divine Farmer's Herb-Root Classic" are 365 medicine compounds made from
minerals, plants and animals. Shen Nong personally tested the properties of hundreds of medical herbs he
identified around 2000 B.C.E. His experiments and documentation are the forerunner to the development of
traditional Chinese (herbal) medicine still used today.
Arabic Pharmacology: The first pharmacological medicine written in Arabic provided formulas
organized by preparation--powders, tablets, ointments and syrups. This work, written by al-Agrabadhin tly
Sabur bin Sahl in 869 C.E. provides recipes with methods and techniques to create pharmacological
preparations along with the dosages.
Modern Pharmacology
Pharmacology is one of the cornerstones of the drug discovery process. The main tasks of
pharmacologists in the search for and development of new medicines are:
• screening for desired activity,
• determining mode of action, and
• quantifying drug activity when chemical methods are not available.
Synthetic organic chemistry was born in 1828, when Friedrich Wohler synthesized urea from inorganic
substances and thus demolished the vital force theory.
The birth date of pharmacology is not as clear-cut. In the early 19th century, physiologists performed
many pharmacologic studies. Thus, François Magendie studied the action of nux vomica (a strychnine-
containing plant drug) on dogs, and showed that the spinal cord was the site of its convulsant action. His work
was presented to the Paris Academy in 1809.
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In 1842, Claude Bernard discovered that the arrow poison curare acts at the neuromuscular junction
to interrupt the stimulation of muscle by nerve impulses.
Nevertheless, pharmacology is held to have emerged as a separate science only when the first
university chair was established.
According to Walter Sneader, this occurred in 1847, when Rudolf Buchheim was appointed professor
of pharmacology at the University of Dorpat in Estonia (then a part of Russia).
Lacking outside funding, Buchheim built a laboratory at his own expense in the basement of his
home. Although Buchheim is credited with turning the purely descriptive and empirical study of medicines into
an experimental science, his reputation is overshadowed by that of his student, Oswald Schmiedeberg.
In 1869, Schmiedeberg showed that muscarine evoked the same effect on the heart as electrical
stimulation of the vagus nerve. In 1878, he published a classic text, Outline of Pharmacology, and in 1885, he
introduced urethane as a hypnotic.
In his 46 years at Strassburg, Schmiedeberg trained most of the men who became professors at other
German universities and in several foreign countries. He was largely responsible for the preeminence of the
German pharmaceutical industry up to World War II.
In the United States, the first chair in pharmacology was established at the University of Michigan in
1890 under John Jacob Abel, an American who had trained under Schmiedeberg.
In 1893, Abel went to Johns Hopkins University in Baltimore, where he had a long and brilliant career.
His major accomplishments include the isolation of epinephrine from adrenal gland extracts (1897–1898),
isolation of histamine from pituitary extract (1919), and preparation of pure crystalline insulin (1926).
Today, there is a pharmacology department in colleges offering medical courses (i.e, human
medicine, veterinary medicine, dental medicine, nursing, pharmacy)
Pharmacology depends largely on experiments conducted in laboratory animals, but even the human
animal may be used as a test subject.
Friedrich Serturner, the German pharmacist who isolated the first alkaloid from opium in 1805,
administered a whopping dose (100 mg) to himself and three friends. All experienced the symptoms of severe
opium poisoning for several days. The alkaloid was named morphine, for Morpheus, the Greek god of sleep.
An interesting example of the use of humans for testing occurred in the 1940s. Although digitalis had
been a standard medication for heart disease for more than a century, there were still no reliable methods for
evaluating its potency. Biological assays (bioassays) were performed on frogs, pigeons, and cats, but none
were totally satisfactory.
In 1942, a group of cardiologists published “a method for bioassay of digitalis in humans”. The assay
was based on quantitative changes in the electrocardiogram (ECG) of patients in the cardiac clinics of two
New York City hospitals. It was hard to find patients whose ECGs could be standardized. Of 97 patients in
whom calibration of the ECG was tried, only 18 proved to be satisfactory assay subjects. Fortunately,
chemical research on the active glycosides of digitalis, and development of analytical methods, soon rendered
all digitalis bioassays obsolete.
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Although humans are no longer used as ad hoc laboratory animals, they are essential in clinical
pharmacology.
When a new drug compound has gone through sufficient preclinical testing to show potential
therapeutic action and reasonable safety on short-term administration, and the data have been reviewed by
the FDA, the compound is administered to a small number of human volunteers under closely controlled and
monitored conditions.
These Phase I clinical trials provide information about dosage and the most common side effects to
be expected. The animals most frequently used in pharmacologic studies are mammals. Mice are preferred
because of their small size, ease of breeding, and short generation time. Rats, guinea pigs, rabbits, and dogs
are also used; each has special characteristics that make it optimal for certain types of tests.
Early in the development of pharmacologic techniques, it was found that an isolated organ or tissue
remained functional for several hours in a bath containing a physiologic solution of salts through which oxygen
was bubbled.
Henrick Magnus (1802–1870) first applied this method to a strip of small intestine, Jean-François
Heymans (1904) worked with the mammalian heart, and Claude Bernard experimented with isolated nerve–
muscle preparations.
The organ or tissue is so suspended that the contraction or relaxation of the muscle is mechanically
transmitted to a stylet. The stylet writes on a drum covered with smoked paper rotated by clockwork at a
constant speed. This device, called a kymograph, graphically records motion or pressure. The effects of drug
substances added to the bath can thus be visualized. The kymograph is a relatively crude device. In modern
laboratories, organ and tissue movements are transmitted by force transducers to polygraph machines, which
produce similar tracings. Or the polygraph is replaced by computerized equipment that issues a digital record.
The surgical preparation of animals is illustrated by the following examples. As early as 1849, the
German anatomist Arnold Berthold transplanted testicular tissue into a capon (a castrated rooster) and
showed that this induced growth of the comb. This basic method was used in the 20th century to isolate and
study the male sex hormones.
Similarly, in 1924, Americans Edgar Allen and Edward Doisy used ovariectomized rats to test the
action of estrogenic hormones. To study anti-inflammatory agents, rats can be made arthritic by injection of an
oily suspension of killed bacteria (Freund’s adjuvant).
Drugs affecting gastric secretion may be studied in animals by forming a Heidenhain pouch—a small
sac of the stomach, vagally denervated and closed off from the main cavity, but with an opening through the
abdominal wall.
Screening of candidate compounds and mode-of-action studies may focus on specific tissues,
organs, or systems or on actions, such as antihistaminic or anticonvulsant.
As knowledge of human biochemistry and molecular biology advances, pharmacology zeroes in more
often on enzymatic action and receptors.
Captopril (Capoten), developed by M. Ondetti and co-workers at Squibb in the 1970s, exemplifies a
molecule that was rationally designed to fit the active site of an enzyme—angiotensin converting enzyme
(ACE). This drug, and subsequent ACE inhibitors, reduces blood pressure.
Knowledge of cell receptors is now on the cutting edge of pharmacology and drug discovery. The
concept was first proposed about a hundred years ago by Paul Ehrlich, the great bacteriologist and chemist
who synthesized salvarsan (also known as “606”) for the treatment of syphilis.
On the basis of his research on bacterial toxins, Ehrlich postulated that the body’s cells possess a
great many “receptors” by which they combine with the food substances in the body fluids. He theorized that
the metabolic products of certain bacteria combine with the receptors of some cells, thus injuring the cells.
Ehrlich visualized receptors as unsatisfied chemical side chains.
This is not far from the modern idea of receptors as domains in enzymes or other proteins, with which
drugs of appropriate structure can combine.
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Illustrating the importance of receptor research are drugs that act on the adrenergic (sympathetic)
nervous system. This system has both - and -receptors. Propranolol (Inderal) was the first specific -
adrenergic receptor blocking agent. Marketed in 1964, it ended a long drought in new heart medicines and
soon became a major therapy for angina pectoris, cardiac arrhythmias, hypertension, and essential tremor.
However, all -adrenergic receptors are not identical, and propranolol is nonselective.
Second-generation drugs such as atenolol (Tenormin) and metoprolol (Lopressor), developed in the
late 1970s, have a preferential effect on l receptors, which are chiefly located in heart muscle. At higher
doses, they also inhibit 2 receptors, which are found mainly in the bronchial and vascular musculature.
There are also blockers of the -adrenoreceptors, such as prazosin (Minipress; early 1980s), and
1-blockers, such as terazosin (Hytrin; 1987). And there are / -blockers: Labetolol (Normodyne) and
carvedilol (Coreg), developed in the mid-1990s, exhibit selective 1 and non-selective -blocking action.
The methods and approaches mentioned are merely a sampling. Pharmacology is similar to medicinal
chemistry in that it has developed a vast array of techniques, both general and specialized.
Building on its past, the ongoing progress of pharmacology supports its critical role in modern drug
discovery and augurs (predicts) well for the future.
PUBLIUS VEGETIUS Complied a treatise that included prescriptions for farm animal
GEBER IBN HAJAR (702-765 AD) An influential Persian who classified drugs and poisons
MUHAMMAD IBN ZAKARIYA AL-RAZI Introduced the use of mercurial ointments and developed
(865-925 AD) mortars, flasks, spatulas and phials
MATHIEU JOSEPH BONAVENTURE
Published “Toxicologie Generale”
ORFILA (1787–1853)
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JOHN GAMGEE Published “The Veterinarians Vade Mecum”
KENELM WINSLOW Authored “Veterinary Material Medica and Therapeutics”
VALERIUS CORDUS(1514-1544 AD) Compiled the 1st pharmacopeia; pioneered the synthesis of ether
Discovered the circulation of blood and indicated that drugs were
WILLIAM HARVEY
distributed to various parts of the body by this means
CHRISTOPHER WREN 1630, make the 1st I.V. of drug into a dog (opium)
ALEXANDER WOOD 1850, devised the 1st hypodermic needle and syringe
HINDS, HAWTHORNE, WILLERSON Studied hemodynamics of dobutamine in dog
THEOPRASTUS BOMBASTUS VON Introduced the clinical uses of opium or laudanum; also called
HOHENHEIM himself Phillipus Aureolus Paracelsus or just Paracelsus
Isolated the narcotic substance from opium and called it
morphine, after Morpheus
• Nyx – goddess of night, mother of Hypnos
• Thanatos – god of death, brother of Hypnos
• Hypnos/Sommus – goddess of sleep
FREDRICH SERTURNER (1783-1841)
• Live in a dark cave, where the river Lether flowed
through, known as the
– River of forgetfulness
• Morpheus – one of the hundred sons of Hypnos, god of
dream
EDWARD JENER Discovered the vaccine against small pox
First to prove that chemical can be absorbed into the vascular
system
FRANCOIS MAGENDIE
• Established the foundation for modern pharmacology
(drug action, d-12relationship, drug disposition)
FRANÇOIS MAGENDIE AND PIERRE
Made I.V injection of ipecac, morphine and strychnine
JOSEPH PELLETIER (1788-1842)
WILLIAM WITHERING Observed the use of foxglove in the Tx of dropsy
Showed the active ingredient of foxglove and called it digitalis
CLAUDE BERNARD
• Demonstrated that curare prevent muscle contractio
Studied evidence-based pharmacology, which requires that
chemical be term a drug only if the specific action in living tissue
is demonstrated
RUDOLF BUCHHEIM
• Established the 1st independent laboratory devoted
exclusively to the study of pharmacology
• “Father of Pharmacology”
“Father of pharmacology in U.S.”
JOHN ABEL • Isolated adrenalin
• Prepared and crystallized insulin
“Father of Modern Veterinary Pharmacology”
L. MEYER JONES (1913-2002 ) Authored the 1st edition of Veterinary Pharmacology &
Therapeutics in 1954
JESUIT PRIEST Use bark of cinchona tree for treatment of malaria
The term pharmacology (pharmakologie) was applied to the study
of material medica by Dale
HENRY HALLETT DALE
Report that prevent hemodynamic effect of epinephrine
Led in establishing pharmacology as an independent science
OSWALD SCHMIEDEBERG based on experimental methodology
“Father of modern pharmacology”
Pioneer in the field of experimental pharmacology of indigenous
COL.SIR RAM NATH CHOPRA plants of India
“Father of Indian Pharmacology”
1910, reported the synthesis of arsphenamine which in an anti-
syphilitic drug
– Anti-trypanosomal drug
PAUL EHRLICH
– 1st antibacterial drug processing specific it for
invading pathogens
– “father of chemotherapy”
ALEXANDER FLEMING 1928, isolated penicillin
GERHARD DOMAGK 1935, isolated estrogenic activity
RAYMOND P. AHLQUIST Designated adrenergic receptors
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Placed neuromuscular blocking agent (muscle relaxant into 2
DANIEL BOVET
categories)
DANIEL BOVET AND ANNE-MARIE
Demonstrated 2 types of antihistamine activity (H1 and H2)
STAUB
GILES MERKEL AND EDMOND I Described the standard index of anesthetic potency for inhalant
EGER II anesthetics
ADOLPH VON BAEYER Synthesized barbituric acid
MAURICE M. RAPPORT Isolated serotonin
Characterized the first 4 cardinal signs of inflammation (heat, red,
AULUS CORNELIUS CELSUS
swell, pain)
RUDOLF VIRCHOW Added the 5th sign (loss of function)
FELIX HOFFMAN Synthesize acetyl ester of salicyclic acid (aspirin)
EDGAR ALLEN 1st to determined estrogenic activity
EDWARD ADELBERT DOISY AND
ADOLF FRIEDRICH JOHANN Isolated estrone from female urine
BUTENANDT
ADOLF FRIEDRICH JOHANN
BUTENANDT, (MARCH 24, 1903 - Isolated aldosterone from male urine
JANUARY 18, 1995)
KARL HEINRICH SLOTTA Discovered the steroid structure of progesterone
EDWARD CALVIN KENDALL (MARCH
Isolated thyroxine
8, 1886 – MAY 4, 1972)
MARIA C. R. HARRINGTON Established the chemical structure of thyroxine
OSKAR MINKOWSKI AND JOSEF
Produced diabetes by total pancreatectomy in dog
VON MERING
FREDERICK BANTING AND Extracted the active compound from pancreas and able to control
CHARLES BEST hyperglycemia in dog and human
JOHN JACOB ABEL Prepared and crystallized insulin
FREDERICK SANGER Sequenced the amino acid of insulin
1968, a pioneer of veterinary pharmacology, was elected to a
personal chair in veterinary pharmacology at Edinburgh
FRANK ALEXANDER University, he delivered an inaugural lecture entitled: ‘Materia
Medica to veterinary pharmacology: a transition’ (Alexander,
1969)
MEYENHOFER AND KATSOYANNIS Synthesized insulin
Discovered that insulin was synthesize as a larger molecule
DONALD F. STEINER
called preproinsulin
KIMBALL AND MURLIN Postulated a pancreatic hyperglycemic hormone
A. STAUB Succeed in purifying glucagon
WILLIAM W. BROMER Sequenced the amino acid of glucagon
GIROLAMO FRACASTORO Postulated that germ caused infection
ANTONIE VAN LEEUWENHOEK Discovered microorganism through lenses
Introduced the scientific approach to the field of medical
ROBERT KOCH
microbiology
LOUIS PASTEUR Indentified infective agent as caused of diseases
Demonstrated the beneficial effect of hand washing between
patients
IGNAZ SEMMELWEIS
• Demonstrated antiseptic effect of chlorine (chlorinated
lime)
Suggested the used of antiseptic in the field of surgery
• Used carbolic lotion
JOSEPH LISTER
• Initiated chemical sterilization of bandage, dressing and
surgical instruments
HENRY DRYSDALE DAKIN (12 Introduced chlorine - containing solution (sodium hypochlorite) for
MARCH 1880 – 10 FEBRUARY 1952) disinfecting
WILLIAM CAMPBELL AND SATOSHI Discovered avermectin; 2015 Nobel Prize in Physiology or
OMURA Medicine
• Dr. Abelardo Aguilar – discovered erythromycin (brand name: Ilosone) in 1949 in Iloilo
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• Dr. Lourdes Jansuy Cruz – discovered conotoxins (or toxins) from marine snails during the 1970s to
80s
• Lagundi cough medicine – launched in the market in 1994, developed by the National Integrated
Research Program on Medicinal Plants, Philippines (NIRPROMP of UPManila) and Philippine Council
for Health Research and Development
• Dr. Teodulo M. Topacio, Jr. (Doctor of Veterinary Medicine); National Scientist for Veterinary Medicine
2009; helped in the development of antibacterial regimen for leptospirosis among domesticated
animals (with an important discovery that pigs could also be infected with leptospirosis and could then
infect humans)
• Anti-Dengue Drug –Phase 1 Preclinical Testing in 2019, Pharmalytics and De La Salle Medical and
Health Sciences Institute
• Tulkas Lunas Program of DOST
3. PHARMACOGNOSY
WHAT IS DRUG?
1. In a broad sense, is any chemical agent other than food that affects living organisms
2. Any substance which is capable of modifying a biological activity
3. Includes any chemical agent (other than food) used in the treatment, cure, prevention or diagnosis of
disease or the control of physiological processes.
4. Definition from R.A. 9502 Universally Accessible Cheaper and Quality Medicines Act of 2008:
Drugs and medicines refers to any chemical compound or biological substance, other than food,
intended for use in the treatment, prevention or diagnosis of disease in humans or animals, including
but not limited to:
(1) any article recognized in the official United States Pharmacopoeia-National Formulary
(USP-NF), official Homeopathic Pharmacopoeia of the United States, Philippine
Pharmacopoeia, Philippine National Drug Formulary, British Pharmacopoeia, European
Pharmacopoeia, Japanese Pharmacopoeia, Indian Pharmacopoeia, any national
compendium or any supplement to any of them;
(2) any article intended for use in the diagnosis, cure, mitigation, treatment, or prevention of
disease in humans or animals;
(3) any article other than food intended to affect the structure or any function of the human
body or animals;
(4) any article intended for use as a component of any articles specified in clauses (1), (2),
and (3) not including devices or their components, parts, or accessories; and
(5) herbal and/or traditional drugs which are articles of plant or animal origin used in folk
medicine which are:
(i) recognized in the Philippine National Drug Formulary;
(ii) intended for use in the treatment or cure or mitigation of disease symptoms, injury
or body defects in humans;
(iii) other than food, intended to affect the structure or any function of the human
body;
(iv) in finished or ready-to-use dosage form; and
(v) intended for use as a component of any of the articles specified in clauses (i), (ii),
(iii), and (iv);
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• New animal drug (NAD): “any drug intended for use in animals other than man, not generally
recognized as safe and effective for the use under the conditions prescribed, recommended, or
suggested in the labeling of the drug.”
• Extra-label drug: when the drug is used in a manner not in accordance with approved label
directions
• Compounded preparation/drugs: constitutes extra-label drug use; undergoes no regulatory
assessment or approval; includes any manipulation of the drug beyond that stipulated on the label
• Generic products/drugs (nonproprietary) drugs that contain the same active ingredient as the
proprietary drug and also meet bioequivalence standards; can be dispensed by the pharmacist
Drug product or medicine is the finished form that contains the active ingredient (s) generally, but not
in association with inactive ingredients.
• Prescription or ethical drugs are pharmaceutical products or drug preparations that are to be
dispensed only upon written order of a validly registered licensed physicians, dentist or
veterinarian for the management or treatment of a condition disease.
• Non-prescription or over-the counter drugs are pharmaceutical products or drug preparations
that can be dispensed even without the written order of a validly-registered licensed physician,
dentist, or veterinarian, for the use of consumer for the prevention of symptomatic relief of minor
or self-limiting ailments.
Dangerous drugs refer to either prohibited drugs or regulated drugs which require a special prescription
form, the use of which is monitored by the Dangerous Drug Board.
• Prohibited drugs include “Opium and its active components and derivatives such as heroin and
morphine; coca leaf and its derivatives, principally cocaine, alpha and beta Eucaine,
hallucinogenic drugs such as mescaline, lysergic acid diethylamide (LSD) and other substances
producing similar effects; Indian hemp and its derivatives; all preparation made derivatives; all
preparation made from any of the foregoing; and other drugs, whether natural or synthetic, with
the physiological effects of a narcotic drug.”
• Regulated drugs includes sleep-inducing sedatives, such as secorbarbital, phenobarbital,
barbital, amobarbital and other drugs which contain a salt or derivative of a salt of barbituric acid;
any salt, isomer or salt of an isomer, of amphetamine such as benzedrine or dexedrine, or any
drug which produces a pharmacological action similar to amphetamine; and hypnotic drugs such
as methaqualone, or any other compound producing similar pharmacologic effects.
SOURCES OF DRUGS
Most drugs currently used in veterinary practice are synthesized by the organic chemist, screened
and tested by pharmacologist and toxicologist, prepared in suitable dosage forms by the pharmaceutical
chemist, evaluated by the clinical investigator, and marketed by pharmaceutical company
• Mineral source:
• Antacids - Magnesium oxide (ex. MAALOX Antacid)
• Purgatives - Magnesium sulfate
• Hematinics - Ferrous sulfate
• Electrolyte - Sodium Chloride
EFFECTS OF DRUGS
• Physiological Effect
• Effect that maintains normal body function
o Water is normally taken in as part of food and is essential in the normal function of
the body.
o Insulin, a hormone essential to glucose uptake and giving of sufficient amount to
reduce blood glucose concentration.
• Pharmacological Effect
• Produces exaggerated effects on the animal when administered in excess
o Ex. Too much ingestion of water causes the volume of plasma to increase while
osmolarity (concentration of osmotically active particles) decreases in relation to the
ECF swelling and disruption of cellular function overdose of insulin cause
hypoglycemia (lowered blood glucose concentration)
1. Solid Dosage Forms: most common medicinal preparation for oral administration
Advantages:
• Ease of administration
• Stability (provides a long shelf life)
• Uniformity with respect to drug contents
a) Powder
• Simplest solid oral dosage from
• Employed by adding the powder to drinking water (soluble
powder) or feeds
d) Capsules
• Hardened containers made up of a mixture of gelatin and
glycerin
• Suitable for drug in powdered forms and certain liquid drugs
o Advantage: drugs with very unpalatable taste, does
not contact the oral mucosa prior to swallowing
o Disadvantage: dose cannot be fractionalized for smaller animals
e) Bolus
• Large compressed tablets, rectangular in shape
• Used for horses and cattle to provide a larger amount of drug required
in the dose without increasing the cross sectionalized size of the
dosage to a dimension that cannot be easily swallowed
f) Suppositories
• Intended for rectal, uretheral or vaginal use
• Made of medicinal substances incorporated in a base
glycinerated gelatin, which melt at body temperature
o rectal suppositories – usually cone shape
o vaginal suppositories – globular
o urethral suppositories – pencil shaped
g) Lozenges
• Oblong, circular, or rectangular medicated candies composed of
the active substance, sugar and mucilage, which are then air dried
• Intended for mouth and throat medication (pastilles)
a) Mixture
• Aqueous solution or suspension intended for oral administration
• Aromatic water (aqueous solution of a volatile oil such as peppermint or cinnamon)
is frequently employed as vehicles but probably add little to the preparation for animal use
(possibilities of contamination by bacteria or molds and to remedy this, preservative such
as benzoic or chlorobutanol are added to inhibit such growth)
• Aqueous suspension of solid (magmas) which are insoluble or nearly insoluble
substances generally contain a dispersing agent (tragacanth or methylcellulose) to delay
settling has label “ shake well before using to insure uniformity of dosage
b) Syrup
• Dense sugar solution in water containing the medicinal substances
• Solution of medicinal agents, flavoring and coloring agents in an 85% sucrose solution
• Employed as cough remedies
c) Elixir
• Hydro-alcoholic solution of medicinal substances that have been sweetened and flavored
characterized by pleasant taste and stability and capable of masking bitter taste
• Usually contained 25% alcohol (better keeping qualities than mixture)
d) Emulsion
• Suspension of minute globules of oily drugs permanently dispersed in aqueous medium,
usually containing flavoring
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e) Gargles
• Watery solutions of a medicament which may or may not be flavored
• Used for rinsing the mouth and throat
f) Extraction
• Infusion (warm or cold water is used)
• Decoction (boiling of water is used)
b) Repository/suppositories
• Designed to prolonged effective drug concentration in the body by providing sustained
release from the dosage form thus delaying absorption
c) Implants
• Very hard, sterile pellets inserted under the skin where they dissolve very slowly
a) Liniments/Braces
• Liquid or semi-solid preparation applied to the skin with inunction (i.e. the rubbing of ointment
or oil into the skin)
• Contains counter-irritant to relieve muscles or tendon pains
b) Lotions
• Solutions of suspensions of soothing substances to be applied to the without friction
c) Ointment
• Semi-solid greasy preparation in which the drug is dissolved or dispersed in a suitable base
(petrolatum, lanolin, or polyethylene glycol)
• Left in consistency and intended for inunction
d) Cream
• Incorporate a drug in a water oil emulsion
• Water will evaporate following application, leaving the drug and a thin film of oil in the skin
e) Dusting Powder
• Mixture of drug in powder form for application to external surfaces
o Adsorbent (e.g. corn starch)
o Lubricant (Talcom)
b) Spirit/Essences
• Alcoholic solution of volatile substances, especially oils, containing 90% volume of alcohol
c) Tinctures
• Alcoholic or mildly alcoholic solution of the extract of the crude drug
ROUTES OF ADMINISTRATION
• Entry points of drugs into the body
• Administration of Drug
o Produces reactions on gross mammalian physiology, attempt shall be made to clearly
visualize:
a) Primary action of drugs on specific cell –receptors
b) Unit structures of tissues their membrane and specific enzymes system
o Depends upon the intention of the veterinarian, which may be either a strictly local action
or a more widely distributed systemic effect or a combined local and systemic
manifestation
• Local Application
o Protection of the surface upon which drug is applied or production of some reflex action
• Local antiseptic
• Local anesthetic
• Systemic Application
o Either parenterally or enterally
o Absorbed into the blood and transported to the different organs or tissues and where they
exert their main actions, thus they manifest their systemic effects
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a) Qualitative type of response desired
• Magnesium sulfate solution given IV will cause muscle relaxation or paralysis but given per os
may produce purgation
• Gentamycin injected: control systemic infection; given per os it modifies the bacterial flora of
the intestinal tract
b) Chemical Properties of drugs
• Procaine penicillin: insoluble in water and available as suspension; injected IM not IV
• Acid labile drugs: destroyed by gastric enzyme when given orally (e.g. insulin, heparin)
d) Therapeutic indication
A. ENTERAL ROUTE
• Through the digestive tract
Reasons:
a) Drugs diluted in the rumen and reticulum maybe rendered
ineffective
b) Metabolically attacked and inactivated by ruminal
microorganism
c) Antibiotic (especially) may kill or inhibit ruminal
microorganism which may lead to digestive disturbance
Advantages:
a) generally safe
b) most economical
c) sterility not a requirement
d) danger of acute drug reaction is not great
e) most practical in medicating a large herd or flock of animal
Disadvantages:
a) Slower onset of action → rate of absorption from the gut is generally slow
b) Drugs may be inactivated in the digestive tract of monogastric animal (exposed to low pH)
e.g. Penicillin G is inactivated by Gastric acid and food in the stomach delays in
absorption
c) Required large dose
d) Irritant drugs may cause vomition
e) Transit time may be modified by GIT disturbances
f) Unpredictability and inconsistency of absorption
g) Procedure may be difficult in uncooperative and vicious animal
h) Poor technique or presence of dysphagia may lead to intra-tracheal delivery and
subsequent bronchopneumonia
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o generally, the rate and extent of absorption of a given drug will be greater in carnivorous
animal than in herbivores due to differences in physiology and amount of indigestible bulk
contained in the GIT
3) Rectal route: seldom used in animals except in giving enema to constipated gut
Local Effect: not proceeded by drug absorption, administration enterally or parenterally drug is applied on
the site where its effect is wanted. These sites includes:
o Intradermal
o Intra-articular
o Oral or Rectal (for drug bot absorbed from GIT)
o Intrathecally (spinal Cord membrane)
o Intra-mammary
o Intra-uterine
o Topical (intra lesional → applied into the lesion)
Systemic Effect: requires the absorption of drug and distribution at its site of action
Method requires:
• Thorough asepsis
• The needle is introduced in the veins, the drug is released slowly except in certain cases
• To reduce the chances of causing drug reaction, allow at least one circulation time (about 1 to
2 minute) to complete an intravenous injection
• Some instances maybe longer than that in pentobarbital (sedative-anesthetic) to effect
• Drug preparation must be pure, sterile and exist as a true solution
• Remove the bubbles inside the syringe
• The usual barrier to absorption is by-passed, the actual rate of absorption is limited by the
rate of injection which is under the control of the injector
Disadvantages:
• Short duration of action
• Adverse effects usually are more severe
• There is no redress once injection had been made
• Difficulty in injecting the needle inside the veins in young animals
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• IV injection of particulate suspension may result in death from pulmonary embolism
Disadvantages:
a) Possibility of improper deposition of the drug preparation in nerves, blood vessels, fat or
between muscle bundles in connective tissue sheath
b) Moderately irritant drug may cause necrosis
3) Subcutaneous (SC)
• needle is inserted through the layers of the skin sand
the drug is deposited in the areolar tissue
• response is more prompt than that of the oral route
• usual dose is generally half that required for oral
administration
• generally employed for administration of relatively
large volume of non-irritating solution or medication
that may produce an moderate degree of muscular
soreness
• absorption is almost as fast as in the intravenous
SC site in dogs
route because the drug goes to the circulation easily
• chosen when a slow and continuous absorption of a
drug is required (provided that the formulation approaches body pH and tonicity is not irritant or
vasoconstricting; oily vehicles should be avoided
• rate of drug absorption from SQ site can be manipulated to some degree of application of:
a) Heat: increase rate of absorption
b) Cold: delayed the rate of absorption
c) Hyalurinadase: increase rate of absorption
d) Massaging the site of Injection: increase rate of absorption (enhances the dispersion)
Disadvantages of SC:
• Injection of irritant or unstable medicinal substances may lead to inflammation, abscess formation and
necrosis
• Danger of infection could be prevented by proper asepsis of the area and of the instrument used.
• Rate of absorption is unpredictable and depends upon:
o Blood flow (most important
o Presence of vasoconstrictor or vasodilator which substantially alter the rate of evaporation
4) Intrapleural (IP)
• A small aseptic opening is made on the abdominal wall through which a needle is passed to the
peritoneal cavity where the drug is deposited
o Peritoneum provides a larger surface area for absorption of drugs
• Important in large animal for the administration of large volume due to great absorbing surface and
rapid absorption rate
• Usually used in experimental animals
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Disadvantages of IP
• Must be careful to place the needle through an area of the abdominal wall within which there not be a
likelihood of penetrating a visceral organ
• Extremely irritating compounds may induce chemical peritonitis
• Seldom used clinically due to danger of infection of the peritoneum and adhesion of the same with
neighboring structures
Duration of Treatment
• It depends entirely on the nature of the disease and the number of doses will vary accordingly, but a
sufficient number to allow for wastage and flexibility of revisiting should be prescribed.
5. PHARMACOTHERAPEUTICS
An additional important responsibility is to make provision for the care, comfort, feeding and alleviation
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of pain or suffering of the affected animal. When medical treatment is deemed necessary, safe and effective,
pharmacological agents that possess the appropriate actions should be selected.
Following administration of selected agent, a complex series of events occur, which govern in large
measure the disposition of the drugs and the ultimate clinical success (or failure) of the regimen selected.
An understanding of the fundamental pharmacological principles involved, together with an
appreciation of the major attributes of each class of drug, form the basis of rational pharmacotherapeutic.
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