Basic Pharmacology HND100 Evening

NUS 122: GENERAL PHARMACOLOGY AND DRUG ADMINISTRATION 2023/2024
AHIBTS DOUALA
GENERAL PHARMACOLOGY AND

DRUG ADMINISTRATION
Course Facilitator
NGU SANDRA LEM
Student’s Name:
Matricule Number:
Campus:
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CHAPTER ONE
INTRODUCTION
1.1 BRIEF HISTORICAL DEVELOPMENT OF PHARMACOLOGY
 The oldest writings of medicinal agents belonged to Ancient India, closely followed by
Chinese and Egyptian literatures.
 Rigveda, the oldest records of civilization (3000 BC) describes the value of medicinal
herbs.
 Ayurveda, the oldest system of medicine, which is very popular in these days also,
recommends herbal remedies and animal origin products for treatment of disease in man
and animals. Charaka, Sushruta and Vaghbata pioneered in Ayurveda. Nakula, one of the
Pandavas followed sound principles of animal husbandry and veterinary science.
 The earliest written compilation of drugs is the Chinese Herbal Formulary (Materia
Medica) “Pen Tsao” which was written by Emperor Shen Nung (2700 BC). It contains
many vegetables, metallic and animal products as remedies.
 The oldest record of Egyptian drug codification is the Kahun Papyrus (2000 BC). It
deals with veterinary medicine and uterine disease of women and contains a number of
prescriptions. The Ebers Papyrus (1550 BC) is a compilation of number of disease
conditions and 829 prescriptions for medicaments employed in Egyptian medicine.
 Hippocrates (460 – 375 BC), a Greek physician and a great teacher of medicine
advocated little use of drugs, maintained very high ethical standards of practice (“Above
all, do no harm”) and attempted to treat diseases based on four elements of nature i.e.
water, fire, air and earth. Combination of these elements gave rise to four humours of the
body related to a scale of life from most alive to dead. They are – Blood (Sanguine
temperament), Phlegm (Phlegmatic), Yellow Bile or Urine (Bilious) and Black Bile
(Melancholic). Treatment consisted of attempting to balance these humours by
replenishment of deficiencies or removing excesses. Thus arose the practices of bleeding,
purging and sweating.
 Aristotle (384 – 322 BC) gave scientific basis for medicine who recorded numerous
observations on animals.
 Theophrastus (380 – 287 BC), a pupil of Aristotle, classified systematically medicinal
herbs on the basis of their individual characteristics rather than their recommended use in
treatment.
 Dioscorides (77), a surgeon, compiled and improved the work of Theophrastus and wrote
the First Materia Medica which consisted of 6 volumes and described 600 plants. Drugs
were discussed from the standpoint of name, source, identification, test for adulteration,
preparation of dosage form, what it would do and for what conditions it would be used.
 Following the fall of Roman Empire, Europe entered the dark ages, during which time
there was little advancement in intellectual development. Custodian of knowledge and
medical thought during this period were found in Muslims. An intellectual Persian writer,
Geber Ibn Hajar (702-765) classified drugs and poisons of his time and stated that
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difference between a drug and a poison was just a matter of dosage. Any drug can be
toxic if given in large enough amounts.
 The spirit of enquiry was re-established in Europe during Renaissance. A German person
Valerius Cordus (1514 - 1544) compiled First Pharmacopoeia.
 During 17th and 18th centuries, drug trade flourished and medical experimentation
began. Drugs like cinchona (Quinine), coffee, tea, cocoa (methylxanthines), curare,
digitalis and a variety of alkaloids were discovered.
 William Withering (1741 - 1799) worked on digitalis in the treatment of dropsy (due to
congestive heart failure, CHF).
 Edward Jenner (1749 - 1823) gave principle of prophylactic immunization against small
pox and first described anaphylaxis.
 William Harvey (1578 - 1657) discovered circulation of blood and indicated that drugs
were distributed to various body parts via blood.
 Christopher Wren (1632 - 1723) made first intravenous injection in a dog.
 Alexander Wood (1817 - 1884) devised hypodermic syringe and needle.
 Friedrich Surtner (1783 - 1841) isolated morphine from opium and named it after the
Roman God of sleep, “Morpheus”.
 Claude Bernard (1813 - 1878) and James Blake (1814 - 1893) established the
foundations of modern pharmacology. They worked on dose response relationship, drug
disposition in the body, mechanism of action of drugs and structure activity relationship
(SAR).
 Rudolph Buchheim (1820 - 1879) established the first laboratory for pharmacology at
University of Dorpat, Estonia.
 John J. Abel (1857 - 1938) who is regarded as the Father of Pharmacology in USA,
established Departments of Pharmacology at University of Michigan and at John Hopkins
University. He also founded reputed journals like Journal of Biological Chemistry and
Journal of Pharmacology and Experimental Therapeutics.
 During 20th Century, the science of Pharmacology flourished in the medical and
pharmacy schools, and focus of leadership shifted from Europe to USA (due to two world
wars and emergence of USA as industrial power). The science of Pharmacology
developed exponentially thereafter due to emergence of Organic Chemistry.
QUESTIONS
What about the history of Pharmacology in Africa? How did our early folks treat diseases?
What is the origin of our famous “African Healers”?
What is the historical development of Pharmacology, medicine and drug therapy in your
own culture?
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1.2 THE NURSING PROCESS AND DRUG THERAPY

Nursing Process
This is an organizational framework for the practice of nursing. It encompasses all steps taken by
the nurse in caring for a patient i.e. assessment, nursing diagnoses, planning and establishing
Goals for nursing care (Statements that are time specific and describe generally),
implementation of the plan (with patient teaching), and evaluation.
1-Assessment
Objective Data
Objective data include information available through the senses, such as what is seen, felt, heard,
and smelled. Among the sources of data are the chart, laboratory test results reports of diagnostic
procedures, physical assessment, and examination findings Examples of specific data are age,
height, weight, all allergies, medication profile, and health history.
Subjective Data
Subjective data include all spoken information shared by the patient, such as complaints
problems, or stated needs (e.g., patient complains of "dizziness, headache, vomiting, and feeling
hot for 10 days")
2-Nursing Diagnoses
Once the assessment phase has been completed, the nurse analyses objective and subjective data
about the patient and the drug and formulates nursing diagnoses. The following is an example of
a nursing diagnosis statement: "Deficient knowledge related to lack of experience with
medication regimen and second-grade reading level as an adult as evidenced by inability to
perform a return demonstration and inability to state adverse effects to report to the prescriber.
This statement of the nursing diagnosis can be broken down into three parts, as follows
Part 1-Deficient knowledge: This is the statement of the human response of the patient to illness,
injury, medications, or significant change. This can be an actual response, an increased risk, or
an opportunity to improve the patient health status. Nursing diagnosis related to knowledge may
be identifying as either deficient or readiness for enhanced.
Part 2-"Related to lack of experience with medication regimen and second-grade reading level
as an adult; This portion of the statement identifies factors related to the response; it often
includes multiple factors with some degree of connection between them. The nursing diagnosis
statement does not necessarily claim that there is a cause-and-effect link between these factors
and the response, only that there is a connection.
Part 3-As evidenced by inability to perform a return demonstration and inability to state adverse
effects to report to the prescriber; This statement lists clues, cues, evidence, and/or data that
support the nurse's claim that the nursing diagnosis is accurate.
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Nursing diagnoses are prioritized in order of criticality based on patient needs or problems.
The ABCs of care (airway, breathing, and circulation) are often used as a basis for prioritization.
Prioritizing always begins with the most important, significant, or critical need of the patient.
Nursing diagnoses that involve actual responses are always ranked above nursing diagnoses that
involve only risks (potential responses).
3-Planning Goals and Outcome Criteria

The planning phase includes the identification of goals and outcome criteria, provides time
frames, and is patient oriented. Goals are objective, realistic, and measurable patient-centred
statements with time frames and are broad, whereas outcome criteria are more specific
descriptions of patient goals.
4-Implementation
In the implementation phase, the nurse intervenes on behalf of the patient to address specific
patient problems and needs. This is done through independent nursing actions; collaborative
activities such as physical therapy, occupational therapy, and music therapy, and implementation
of medical orders. Family, significant others, and caregivers assist in carrying out this phase of
the nursing care plan. Specific interventions that relate to particular drugs (e.g. giving a
particular cardiac drug only after monitoring the patient's pulse and blood pressure), non-
pharmacologic interventions that enhance the therapeutic effects of medications, and patient
education are major components of the implementation phase.
5-Evaluation
Evaluation is the part of the nursing process that includes monitoring whether patient goals and
outcome criteria related to the nursing diagnoses are met. Monitoring includes observing for
therapeutic effects of drug treatment as well as for adverse effects and toxicity. Many indicators
are used to monitor these aspects of drug therapy as well as the results of appropriately related
non pharmacologic interventions. If the goals and outcome criteria are met, the nursing care plan
may or may not be revised to include new nursing diagnoses; such changes are made only if
appropriate. If goals and outcome criteria are not met, revisions are made to the entire nursing
care plan with further evaluation.
CASE STUDY
Dollie, a 27-year-old social worker, is visiting the clinic today for a physical examination. She
states that she and her husband want to "start a family." but she has not had a physical for several
years: She was told when she was 22 years of age that she had "anaemia" and was given iron
tablets, but Dollie states that she has not taken them for years: She said she "felt better" and did
not think she needed them. She denies any use of tobacco and illegal drugs: she states that she
may have a drink with dinner once or twice a month. She uses tea tree oil on her face twice a day
to reduce acne breakouts. She denies using any other drugs.
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1. What other questions does the nurse need to ask during this assessment phase?
2. After laboratory work is performed, Dollie is told that she is slightly anaemic. The prescriber
recommends that she resume taking iron supplements as well as folic acid. She is willing to try
again and says that she is "all about doing what's right to stay healthy and become a mother."
What nursing diagnoses would be appropriate at this time?
3. Dollie is given a prescription that reads as follows: "Ferrous sulfate 325 mg PO for anaemia."
When she goes to the pharmacy, the pharmacist tells her that the prescription is incomplete.
What is missing? What should be done?
4. After 4 weeks, Dollie's latest laboratory results indicate that she still has anaemia. However,
Dollie states, "I feel so much better that I'm planning to stop taking the iron tablets. I hate to take
medicine." How should the nurse handle this?
CURRENT NANDA-I-APPROVED NURSING DIAGNOSES MOST RELEVANT TO

DRUG THERAPY
 Activity intolerance and risk for

 Knowledge (deficient, readiness)
 Adverse reaction to iodinated contrast
 Lattes any response risk Lifestyle Sedentary"
 Airway clearance, ineffective
 Allergy response latex and ik for
 Liver function is for impaired
 Aspiration, risk, for
 Loneliness, risk for Memory,
 Body image disturbed
 Mobility impaired, impaired physical,
 Nutrition, imbalanced (les thin body has body
 Self-care deficit (bathing, dressing) etc
GO TO THE YOUR WORK BOOK AND ANSWER QUESTIONS
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CHAPTER TWO
CHAPTER THREE
DEFINITION OF TERMS USED IN PHARMACOLOGY
 Additive effects: Drug interactions in which the effect of a combination of two or more
drugs with similar actions is equivalent to the sum of the individual effects of the same drugs
given alone. For example, 1+1=2 (compare with synergistic effects).
 Adverse drug event: Any undesirable occurrence related to administering or failing to
administer a prescribed medication.
 Adverse drug reaction: Any unexpected, unintended, undesired, or excessive response to a
medication given at therapeutic dosages (as opposed to overdose).
 Adverse effects: A general term for any undesirable effects that are a direct response to one
or more drugs.
 Agonist: A drug that binds to and stimulates the activity of one or more receptors in the
body.
 Allergic reaction: An immunologic hypersensitivity reaction resulting from the unusual
sensitivity of a patient to a particular medication; a type of adverse drug event.
 Antagonist: A drug that binds to and inhibits the activity of one or more receptors in the
body. Antagonists are also called inhibitors.
 Antagonistic effects: Drug interactions in which the effect of a combination of two or more
drugs is less than the sum of the individual effects of the same drugs given alone (1+1 equals
less than 2); it is usually caused by an antagonizing (blocking or reducing) effect of one drug
on another.
 Bioavailability: A measure of the extent of drug absorption for a given drug and route (from
0% to 100%).
 Biotransformation: One or more biochemical reactions involving a parent drug.
Biotransformation occurs mainly in the liver and produces a metabolite that is either inactive
or active. Also known as metabolism.
 Blood-brain barrier: The barrier system that restricts the passage of various chemicals and
microscopic entities (e.g. bacteria, viruses) between the bloodstream and the central nervous
system. It still allows for the passage of essential substances such as oxygen.
 Compliance: Implementation or fulfilment of a prescriber's or caregiver's prescribed course
of treatment or therapeutic plan by a patient.
 Noncompliance: An informed decision on the part of the patient not to adhere to or follow a
therapeutic plan or suggestion
 Chemical name: The name that describes the chemical composition and molecular structure
of a drug.
 Chemotherapy: It’s the effect of drugs upon microorganisms, parasites and neoplastic cells
living and multiplying in living organisms.
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 Contraindication: Any condition, especially one related to a disease state or patient

characteristic, including current or recent drug therapy, which renders a particular form of
treatment improper or undesirable.
 Cytochrome P-450: The general name for large class of enzymes that play a significant role
in drug metabolism and drug interactions.
 Dependence: A state in which there is a compulsive or chronic need, as for a drug
Dissolution: The process by which solid forms of drugs disintegrate in the gastrointestinal
tract and become soluble before being absorbed into the circulation.
 Drug: Any chemical that affects the physiologic processes of a living organism.
 Drug actions: The processes involved in the interaction between a drug and body cells (eg,
the action of a drug on a receptor protein); also called mechanism of action.
 Drug classification: A method of grouping drugs; may be based on structure or therapeutic
use.
 Drug effects: The physiologic reactions of the body to a drug. They can be therapeutic or
toxic and describe how the body is affected as a whole by the drug. The terms onset, peak,
and duration are used to describe drug effects (most often refer- ring to therapeutic effects).
 Drug-induced teratogenesis: The development of congenital anomalies or defects in the
developing fetus caused by the toxic effects of drugs
 Drug interaction: Alteration in the pharmacologic or pharmacokinetic activity of a given
drug caused by the presence of one or more additional drugs it is usually related to effects on
the enzymes required for metabolism of the involved drugs
 Duration of action: The length of time the concentration of a drug in the blood or tissues is
sufficient to e licit a response.
 Enzymes: Protein molecules that catalyze one or more of a variety of biochemical reactions,
including those related to the body's physiologic processes as well as those related to drug
metabolism.
 Excipient: substances included in the pharmaceutical dosage form, with no therapeutic
action but protects, supports and enhance stability of the active ingredient
 First-pass effect: The initial metabolism in the liver of a drug absorbed from the
gastrointestinal tract before the drug reaches systemic circulation through the bloodstream.
 Generic name: The name given to a drug by the United States Adopted Names Council.
Also called the nonproprietary name. The generic name is much shorter and simpler than the
chemical name and is not protected by trademark.
 Glucose-6-phosphate dehydrogenase (G6PD) deficiency: A hereditary condition in which
red blood cells break down when the body is exposed to certain drugs
 Half-life: In pharmacokinetics, the time required for half of an administered dose of drug to
be eliminated by the body, or the time it takes for the blood level of a drug to be reduced by
50% (also called elimination half-life).
 Idiosyncratic reaction: An abnormal and unexpected response to a medication, other than
an allergic reaction, that is peculiar to an individual patient.
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 Incompatibility: The characteristic that causes two parenteral drugs or solutions to undergo
a reaction when mixed or given together that results in the chemical deterioration of at least
one of the drugs.
 Indication: it is a disease or a situation for which a drug is used.
 Contraindications: this is the situation where the taking of the medicine may prove to be
dangerous. The latter must therefore not be given.
We distinguish the relative contraindications where in some cases the benefit-risk ratio of the
taking of the molecule remains acceptable and the absolute contraindications where the drug
should not be taken, whatever the expected benefit.
o Association not recommended: to avoid, except after evaluation of the
benefit/risk ratio; need for close monitoring.
o Usage precaution: this is the most frequent case; possible Association in
accordance with the recommendations.
o Facts to be considered: risk reporting; the practitioner to assess the
appropriateness of the Association; no specific conduct to be held.
 Intra-arterial: Within an artery (e.g., intra-arterial injection).
 Intra-articular: Within a joint (e.g., intraarticular injection).
 Intrathecal: Within a sheath (e.g., the theca of the spinal cord, as in an intrathecal injection
into the subarachnoid space).
 Medication error: Any preventable adverse drug event (see above) involving inappropriate
medication use by a patient or health care professional; it may or may not cause patient harm.
 Medication use process: The prescribing, dispensing, and administering of medications, and
the monitoring of their effects.
 Metabolite: A chemical form of a drug that is the product of one or more biochemical
(metabolic) reactions involving the parent drug (see later).
 Active metabolites: are those that have pharmacologic activity of their own, even if the
parent drug is inactive (see prodrug). Inactive metabolites lack pharmacologic activity and
are simply drug waste products awaiting excretion from the body (e.g., via the urinary,
gastrointestinal, or respiratory tract).
 Onset of action: The time required for a drug to elicit a therapeutic response after dosing.
 Outcome criteria: Descriptions of specific patient behaviours or responses that demonstrate
meeting of or achievement of goals related to each nursing diagnosis. These statements, as
with goals, are verifiable, framed in behavioural terms, measurable, and time specific.
Outcome criteria are considered to be specific, whereas goals are broad.
 Prescriber: Any health care professional licensed by the appropriate regulatory board to
prescribe medications.
 Parent drug: The chemical form of a drug that is administered before it is metabolized by
the body's biochemical reactions into its active or inactive metabolites (see metabolite). A
parent drug that is not pharmacologically active itself is called a prodrug. A prodrug is then
metabolized to pharmacologically active metabolites.
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 Peak effect: The time required for a drug to reach its maximum therapeutic response in the
body.
 Peak level: The maximum concentration of a drug in the body after administration, usually
measured in a blood sample for therapeutic drug monitoring.
 Pharmaceutics: The science of preparing and dispensing drugs, including dosage form
design.
 Pharmacodynamics: The study of the biochemical and physiologic interactions of drugs at
their sites of activity. It examines the physicochemical properties of drugs and their
pharmacologic interactions with body receptors.
 Pharmacoeconomics: The study of economic factors impacting the cost of drug therapy.
 Pharmacogenomics: The study of the influence of genetic factors on drug response,
including the nature of genetic aberrations that result in the absence, overabundance, u
insufficiency of drug metabolizing enzymes (also called
 Pharmacognosy: The study of drugs that are obtained from natural plant and animal sources.
 Pharmacokinetics: The study of what happens to a drug from the time it is put into the body
until the parent drug and all metabolites have left the body. Pharmacokinetics represent the
drug absorption into, distribution and metabolism within, and excretion from the body.
 Pharmacology: The broadest term for the study or science of drugs.
 Pharmacotherapeutics: The treatment of pathologic conditions through the use of drug
 Prodrug: An inactive drug dosage form that is converted to an active metabolite by various
biochemical reactions once it is inside the body.
 Posology or Dosage: this is the usual dose of the drug used. It depends on the disease, the
age of the patient, its weight and certain factors: renal function, hepatic function. It should
naturally not be altered without medical advice or possibly the pharmacist.
 Receptor: A molecular structure within or on the outer surface of a cell. Receptors bind
specific substances (e.g., drug molecules), and one or more corresponding cellular effects
(drug actions) occurs as a result of this drug-receptor interaction. Steady state The
physiologic state in which the amount of drug removed via elimination is equal to the amount
of drug absorbed with each dose.
 Substrates: Substances (e.g., drugs or natural biochemical in the body) on which an enzyme
acts.
 Synergy: this corresponds to the interaction between two drugs with an identical
pharmaceutical activity. The intensity of the activity of the Association is greater than that
which one could obtain with one of the drugs administered alone.
 Synergistic effects: Drug interactions in which the effect of a combination of two or more
drugs with similar actions is greater than the sum of the individual effects of the same drugs
given alone. For example, 1+1 is greater than 2 (compare with additive effects).
 Therapeutic drug monitoring: The process of measuring drug levels to identify a patient's
drug exposure and to allow adjustment of dosages with the goals of maximizing therapeutic
effects and minimizing toxicity.
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 Therapeutic effect: The desired or intended effect of a particular medication.

 Therapeutic index: The ratio between the toxic and therapeutic concentrations of a drug.
 Tolerance: Reduced response to a drug after prolonged use.
 Toxic: The quality of being poisonous (i.e., injurious to health or dangerous to life).
 Toxicity: The condition of producing adverse bodily effects due to poisonous qualities.
 Toxicology: The study of poisons, including toxic drug effects, and applicable treatments.
 Trade name: The commercial name given to a drug product by its manufacturer; also called
the proprietary name.
 Trough level: The lowest concentration of drug reached in the body after it falls from its
peak level, usually measured in a blood sample for therapeutic drug monitoring.
GO TO THE YOUR WORK BOOK AND ANSWER QUESTIONS
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CHAPTER THREE
SOURCES OF DRUGS, DRUG SCHEDULES AND NOMENCLATURE
2.1 SOURCES OF DRUGS
Drugs have different sources namely:
Minerals: Liquid paraffin, magnesium sulfate, magnesium trisilicate, kaolin, etc.
Animals: Insulin, thyroid extract, heparin and antitoxin sera, etc.
Plants: Morphine, digoxin, atropine, castor oil, etc.
Synthetic source / semi synthetic: Aspirin, sulphonamides, paracetamol, zidovudine, etc.
Microorganisms: Penicillin, streptomycin and many other antibiotics.
Genetic engineering: Human insulin, human growth hormone etc. Out of all the above sources,
majority of the drugs currently used in therapeutics are from synthetic source.
1. Plant Sources: Plant source is the oldest source of drugs. Most of the drugs in ancient times
were derived from plants. Almost all parts of the plants are used i.e. leaves, stem, bark, fruits and
roots.
Leaves:
 The leaves of Digitalis Purpurea are the source of Digitoxin and Digoxin, which are
cardiac glycosides.
 Leaves of Eucalyptus give oil of Eucalyptus, which is important component of cough
syrup. Tobacco leaves give nicotine.
 Atropa belladonna gives atropine.
Flowers:
 Poppy papaver somniferum gives morphine (opoid)
 Vinca rosea gives vincristine and vinblastine
 Rose gives rose water used as tonic.
Fruits:
 Senna pod gives anthracine, which is a purgative (used in constipation)
 Calabar beans give physostigmine, which is cholinomimetic agent.
Seeds:
 Seeds of Nux Vomica give strychnine, which is a CNS stimulant.
 Castor oil seeds give castor oil.
Roots:
 Ipecacuanha root gives Emetine, used to induce vomiting as in accidental poisoning. It
also has amoebicidal properties.
 Rauwolfia serpentina gives reserpine, a hypotensive agent. Reserpine was used for
hypertension treatment.
Bark:
 Cinchona bark gives quinine and quinidine, which are antimalarial drugs. Quinidine also
has antiarrythmic properties.
 Atropa belladonna gives atropine, which is anticholinergic.
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Stem:
 Chondrodendron tomentosum gives tuboqurarine, which is skeletal muscle relaxant used
in general anesthesia.
2. Animal Sources:
 Pancreas is a source of Insulin, used in treatment of Diabetes.
 Urine of pregnant women gives human chorionic gonadotropin (hCG) used for the
treatment of infertility.
 Sheep thyroid is a source of thyroxin, used in hypertension.
 Cod liver is used as a source of vitamin A and D.
 Anterior pituitary is a source of pituitary gonadotropins, used in treatment of infertility.
 Blood of animals is used in preparation of vaccines.
3. Mineral Sources:
i. Metallic and Non-metallic sources:
 Iron is used in treatment of iron deficiency anemia.
 Mercurial salts are used in Syphilis.
 Zinc is used as zinc supplement. Zinc oxide paste is used in wounds and in eczema.
 Iodine is antiseptic. Iodine supplements are also used.
ii. Miscellaneous Sources:
 Fluorine has antiseptic properties.
 Borax has antiseptic properties as well.
 Selenium as selenium sulphide is used in anti-dandruff shampoos.
i. Synthetic Sources:
 When the nucleus of the drug from natural source as well as its chemical structure is
altered, we call it synthetic.
 Examples include Emetine Bismuth Iodide
ii. Semi Synthetic Source:
 When the nucleus of drug obtained from natural source is retained but the chemical
structure is altered, we call it semi-synthetic.
 Examples include Apomorphine, Diacetyl morphine, Ethinyl Estradiol, Homatropine,
Ampicillin and Methyl testosterone.
 Most of the drugs used nowadays (such as antianxiety drugs, anti convulsants) are
synthetic forms.
5. Microbiological Sources:
 Penicillium notatum is a fungus which gives penicillin.
 Actinobacteria give Streptomycin.
 Aminoglycosides such as gentamicin and tobramycin are obtained from streptomyces and
micromonosporas.
6. Recombinant DNA technology:
Recombinant DNA technology involves cleavage of DNA by enzyme restriction endonucleases.
The desired gene is coupled to rapidly replicating DNA (viral, bacterial or plasmid). The new
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genetic combination is inserted into the bacterial cultures which allow production of vast amount
of genetic material.
Advantages:
 Huge amounts of drugs can be produced.
 Drug can be obtained in pure form.
 It is less antigenic.
Disadvantages:
 Well-equipped lab is required.
 Highly trained staff is required.
 It is a complex and complicated technique.
2.2 DRUG SCHEDULES (CATEGORIES OF CONTROLLED SUBSTANCES)

Schedule I
 Drugs that are not approved for medical use and have high abuse potentials: heroin,
lysergic acid diethylamide (LSD), peyote, mescaline, tetrahydrocannabinol, marijuana.
Schedule II
 Drugs that are used medically and have high abuse potentials: opioids analgesics (e.g.
codeine, hydromorphone, methadone, meperidine, morphine, oxycodone, oxomorphone),
central nervous system (CNS) stimulants (e.g. cocaine, methamphetamine,
methylphenidate), and barbiturate sedative-hypnotics (amobarbital, pentobarbital,
secobarbital)
Schedule III
 Drugs with less potential for abuse than those in schedules I and II, but abuse may lead to
psychological or physical dependence:androgens and anabolic steroids, some CNS
stimulants (e.g. benzphetamine), and mixtures containing small amounts of controlled
substances (e.g. codeine, barbiturates not listed in other schedules).
Schedule IV
 Drugs with some potential for abuse: benzodiazepines (e.g. diazepam. Lorazepam,
temazepam), other sedative-hypnotics (e.g. phenobarbital, chloral hydrate) and some
prescription appetite suppressants (e.g. mazindol, phentermine).
Schedule V
 Products containing moderate amounts of controlled substances. They may be dispensed
by the pharmacist without a physician’s prescription but with some restrictions regarding
amount, record keeping and other safeguards. Included are antidiarrheal drugs such as
diphenoxylate and atropine (lomotil).
2.3 DRUG NOMENCLATURE
Every drug has at least three names
 A chemical name (e.g. 6-dimethylamino-4,4-diphenyl-3heptanone hydrochloride),
 A generic name (e.g., methadone hydrochloride)
 A proprietary (or trade) name (e.g., Dolophine)
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CHAPTER FOUR
PHYSICO-CHEMICAL PROPERTIES OF DRUGS
The ability of a chemical compound to elicit a pharmacological/ therapeutic effect is related to
the influence of various physical and chemical (physicochemical) properties of the chemical
substance on the bio molecule that it interacts with.
1) Physical Properties: Physical property of drug is responsible for its action
2) Chemical Properties: The drug reacts extracellularly according to simple chemical reactions
like neutralization, chelation, oxidation etc.
Physical Chemical
Solubility and permeability Partition coefficient
Physical state Isomerization
Polarity Intermolecular forces
Particle size Ionization
Melting point Ph.
Functional group
Requirements for a drug to exert its biological effect
The drug must
 Pass via barriers
 Survive alternate sites of attachment/storage
 Avoid metabolic destruction before it reaches the site of action
 Allow favourable binding characteristics
 Dissociate from receptor and re-enter the systemic circulation to be excreted
Dosage form
Dosage forms are the means (or the form) by which drug molecules are delivered to sites of
action within the body.
The need for dosage forms:
 Accurate dose: To provide for the safe and convenient delivery of accurate dosage.
Examples: Tablets, Capsules, syrups
 Protection: For the protection of a drug substance from the destructive influence of
atmospheric oxygen or moisture. Examples: coated tablets, sealed ampoules
 For the protection of a drug substance from the destructive influence of gastric acid after oral
administration. Example: enteric coated tablets
 To provide liquid preparations of substances that are either insoluble or unstable in the
desired vehicle. Example: suspension
 To provide liquid dosage forms of substances soluble in desired vehicle. Example: solution
 To provide extended drug action through controlled release mechanisms Examples:
controlled release tablets, capsules, suspensions
 To provide optional drug action from topical administration sites. Examples: ointments,
creams, ophthalmic, ear and nasal preparations
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 To provide for insertion of a drug into one of the body’s orifices. Examples: rectal and
vaginal suppositories
 To provide for the placement of drugs within body tissues. Examples: Implants
 To provide for the optimal drug action through inhalation therapy. Examples: inhalants and
inhalation In addition, many dosage forms permit ease of drug identification through
distinctiveness of color, shape, or identifying markings
Factors that influence drug dosage and action

It is important for the nurse to be oriented of the characteristic that modify cell conditions and
therefore modify the activity of a drug. These characteristics include the following:
1- Age:
 Children and elderly persons are highly responsive to drug.
 Infants often have immature hepatic and renal systems and therefore incomplete
metabolic & excretory mechanisms.
 N.B.: Aged individuals may demonstrate different responses to drug therapy because of
deterioration of hepatic and renal function which is often accompanied by concurrent
disease process such as C.V.D. (cardiovascular disease).
2- Weight:
 The greater the weight, the greater must be the dose.
 However, body weight due to fat or edema fluid should not be taken into consideration.
 For very lean and very obese individuals, drug dosage is frequently determined on the
basis of drug/kg of body weight or body surface area.
3-Sex:
 Females don’t always respond to the action of drug in the same manner as do men.
 Women are usually smaller than men, which lead to high drug concentration if dosage is
prescribed indifferently.
 Female’s body is composed of higher % of adipose tissue than males, absorption rate of
drug are slower in fatty tissue than in skeletal muscle, so the effect of drug will be more
pronounced and prolonged.
N.B: During pregnancy, lactation, and menstruation, many drugs are stopped:
 Aspirin: not used during menstruation as it increase blood fluidity.
 Drugs excreted in milk aren’t given during lactation as penicillin.
 Uterine stimulant should be avoided during pregnancy as they may produce abortion such
as prostaglandin.
 Drugs that might affect foetus and placenta should not be given during pregnancy.
4-Time of administration:
 Drug is more rapidly absorbed when the GIT is free of food, while irritating drugs are
more tolerated if there is food in stomach.
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 Body resistant to drug is generally greater in the early morning when the body is at its
lowest point of physiologic functioning and conversely, the body is more sensitive to
drugs effect during time of maximal activity.
5-Pathologic state:
 Diseases alter the functional activity and accordingly its response to drug. e.g. sever pain
tends to increase patient’s requirement to opiates.
 The presence of circulatory, hepatic and/ or renal dysfunction will interfere with the
physiologic process of drug action.
6-Environmental Milieu:
 Drugs affecting mood & behaviour are particularly susceptible to the influence of the
patient’s environment.
 With such drugs one has to consider effects in light of 4
o The drug itself.
o The personality of the user.
o The environment of the user.
o The interaction of these 3 components.
o Heat relaxes peripheral blood vessels while cold has the opposite effect.
7-Genetic factors
Dosage forms depend on:

 The route of administration
o Rectal
o Parenteral
o Gaseous
o Vaginal
o Inhaled
o Ophthalmic
o Otic
 Their physical form
o Solid
o Semisolid
o Liquid
o Gaseous
2.4.1 Physical Dosage Forms
In physical form, there are 4 main dosage forms
 Solid
 Semisolid
 Liquid
 Gaseous
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TYPES OF DOSAGE FORM: PHYSICAL

Solid dosage forms
Shaped Tablets, capsules, implants, transdermal patches
unshaped Powders for external/internal use
Semi solid dosage forms
Shaped Suppositories (for rectal administration)
Pessaries (vaginal suppositories)
Unshaped Gels, creams, ointments, pastes

Liquid dosage forms
Monophasic Solutions (syrup, spirits, elixir, tinctures)
Biphasic Emulsions, suspensions
External solutions Lotions, liniments, collodions
Gaseous dosage forms/
Medicinal gases Aerosols: inhalation/volatile anaesthetics
Aerodispersions Antiasthmatic sprays
Route of administration
A route of administration in pharmacology and toxicology is the path by which a drug, fluid,
poison, or other substance is taken into the body.
 Routes of administration are generally classified by the location at which the substance is
applied. Common examples include oral and intravenous administration.
Routes can also be classified based on where the target of action is.
 Action may be topical (local), enteral (system wide effect, but delivered through the
gastrointestinal tract) or parenteral (systemic action, but delivered by routes other than
the GI tract).
 Routes of administration can also basically be classified whether the effect is local (in
topical administration) or systemic (in enteral or parenteral administration):
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TYPES OF DOSAGE FORM: ROUTE OF ADMINISTRATION

Enteral
oral Tablets, capsules, syrups, suspensions, emulsions etc. dry powder inhaler
(DPI), pressurized metered dose inhaler (pMDI), nebulizer, vaporizer
Sublingual Orally disintergrating tablets (ODT), lozenges, chewing tablets, mouthwash,
buccal toothpaste, ointments, oral spray
Rectal Ointment, suppository, enema, Nutrient enema
Parental, (injections and infusions)
Intravenous, Intra-arterial, Intramuscular, Intradermal, Intraosseous, intracardiac.
Intraperitoneal, Intrathecal, subcutaneous
Topical
Dermal Ointments, liniments, paste, creams, lotion, lip balm, medicated shampoo,
dermal patch.
mucosal Ear drops, eye drops, nasal sprays, ointment, hydrogel, nanosphere
suspension, mucoadhesive microdisc, pessaries
Percutaneous Transdermal patches
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ROUTE OF DRUG ADMINISTRATION AND RELATED NURSING CONSIDERATION

ROUTE ADVANTAGES DISADVANTAGES NURSING CONSIDERATION
Intravenous (IV) Provides rapid onset (drug Higher cost, inconvenience leg, Continuous intravenous infusions require frequent
delivered immediately to not self-administered), monitoring to be sure that the correct volume and
bloodstream); allows more direct irreversibility of drug action in amount are administered and that the drug reaches
control of drug level in blood, most cases and inability to safe, therapeutic blood levels. Intravenous drugs
gives option of larger fluid retrieve medication risk of fluid and solutions must be checked for compatibilities
volume, therefore diluting overload, greater likelihood of Intravenous sites are to be monitored for redness,
irritating drugs; avoids first-pass infection possibility of swelling, heat, and drainage-all indicative of
metabolism embolism complications, such as thrombophlebitis If
intermittent intravenous infusions are used,
clearing or flushing of the line with normal saline
before and after is generally indicated to keep the
intravenous site patent and minimize
incompatibilities,
Intramuscular (IM), Intramuscular injections are good Discomfort of injection Using landmarks to identify correct intramuscular
for poorly soluble drugs, which inconvenience, bruising slower and subcutaneous sites is always required and
are often given in "depot onset of action compared to recommended as a nursing standard of care. For
preparation form and are then intravenous although quicker adults, the intramuscular site of choice is the
absorbed over a prolonged period, than oral in most situations ventral gluteal muscle with use of a 15-inch
onsets of action differ depending (sometimes 1-inch in very thin or emaciated
on route patients) and 20- to 25-gauge needle for aqueous
solutions and 18- to 25-gauge needle for viscous
Subcutaneous (Sc) or oil-based solutions.
Subcutaneous injections are recommended to be

given at a 90-degree angle with a proper size
syringe and needle (- to -inch) in emaciated or
very thin patients, the subcutaneous angle is at 45
degrees. Subcutaneous injections require a 26- to
30-gauge, 3-inch needle inserted at a 90-degree
angle, Selection of correct size of syringe and
needle is key to safe administration by these
Page 20
routes and is based on thorough assessment of the

patient as well as the characteristics of the drug.
Oral Usually easier, more convenient, Variable absorption, inactivation Enteral routes include oral administration and
and less expensive safer than of some drugs by stomach acid involve a variety of dosage forms (e.g.. liquids,
injection, dosing more likely to be and/or pH. problems with first- solutions, tablets, and enteric-coated pills or
reversible in cases of accidental pass effect or pre-systemic tablets) Some medications are recommended to be
ingestion e.g. through induction metabolism, greater dependence taken with food, while others are recommended
of emesis, administration of of drug action on patient not to be taken with food: it is also suggested that
activated charcoal) variables oral dosage forms of drugs be taken with at least 6
to 8 oz. of fluid, such as water. Other factors to
consider include other medicines being taken at
the same time and concurrent use of dairy
products or antacids. If oral forms are given via
nasogastric tube or gastrostomy tube, tube
placement in stomach must be assessed prior to
giving the medication and the patient's head is to
remain elevated; flushing the nasogastric tube
with at least 30 to 60 ml of water before and after
the drug has been given is recommended to help
maintain tube patency and prevent clogging
Sublingual, buccal Absorbed more rapidly from oral Patients may swallow pill Drugs given via the sublingual route are to be
subtypes of oral, but mucosa and leads to more rapid instead of keeping under tongue placed under the tongue; once dissolved, the drug
more parenteral than onset of action; avoids breakdown until dissolved, pills often may be swallowed. When using the buccal route,
enteral) of drug by stomach acid; avoids smaller to handle medication is placed between the cheek and gum,
first-pass metabolism because Both of these dosage forms are relatively non-
gastric absorption is bypassed irritating, the drug usually is without flavour and
water-soluble
Rectal Provides relatively rapid Possible discomfort and Absorption via this route is erratic and
absorption, good alternative when embarrassment to patient often unpredictable, but it provides a safe alternative
oral route not feasible; useful for higher cost than oral route when nausea or vomiting prevents oral dosing of
local or systemic drug delivery. drugs. The patient must be placed on his or her
usually leads to mixed first-pass left side so that the normal anatomy of the colon
and non-first-pass metabolism allows safe and effective insertion of the rectal
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dosage form. Suppositories are inserted using a

gloved hand and/or gloved index finger and
water-soluble lubricant. Drug must be
administered exactly as ordered.
Topical Delivers medication directly to Sometimes awkward 10 self- Most dermatologic drugs are given via topical
affected area, decreases administer (e.g. eye drops) can route in form of a solution, ointment, spray, or
likelihood of systemic drug be messy. usually higher cost drops. Maximal absorption of topical drugs is
effects than oral route enhanced with skin that is clean and free of
debris; if measurement of ointment is necessary-
such as with topical nitro-glycerine-application
must be done carefully and per instructions (e.g.,
apply 1 inch of ointment) Gloves help minimize
cross-contamination and prevent absorption of
drug into the nurse's own skin. If the patient's skin
is not intact, sterile technique is needed.
Transdermal (subtype Provides relatively constant rate Rate of absorption can be Transdermal drugs should be placed on alternating
of topical) of drug absorption; one patch can affected by excessive sites and on a clean, non-hairy non-imitated area,
last 1 to 7 days, depending on perspiration and body and only after the previously applied patch has
drug; avoids first-pass temperature; patch may peel off; been removed and that area cleansed and dried.
metabolism cost is higher; used patches must Transdermal drugs generally come in a single-
be disposed of safely dose adhesive backed drug application
Inhalation Provides rapid absorption; drug Rate of absorption can be too Inhaled medications are to be used exactly as
delivered directly to lung tissues rapid, increasing the risk of prescribed and with clean equipment Instructions
where most of these drugs exert exaggerated drug effects; need to be given to the patient/family/caregiver
their actions requires more patient education regarding medications to be used as well as the
for self-administration; some proper use, storage, and safe of inhalers, spacers,
patients may have difficulty and nebulizers
with administration technique
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Factors governing Choice of routes of drug administration

The reasons for choice of routes of drug administration are governed by various factors. Such as:
 Physical and chemical properties of the drug. Here there physical properties of drug
are solid, liquid and gas. And chemical properties of drug are solubility, stability, pH,
irritancy etc.
 Site of desired action. Here the action of drug may be localized and approachable or
generalized and non-approachable.
 Rate of extent of absorption of the drug from different routes.
 Effect of digestive juices and first phase of metabolism.
 Condition of the patient.
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CHAPTER FIVE
PHASES IN PHARMACOLOGICAL PROCESS AND DRUG ACTION
A tablet or capsule taken by mouth goes through three phases—pharmaceutic,
pharmacokinetic, and pharmacodynamics—as drug actions occur.
In the pharmaceutic phase, the drug becomes a solution so that it can cross the biologic
membrane.
When the drug is administered parenterally by subcutaneous (Sc), intramuscular (IM), or
intravenous (IV) routes, there is no pharmaceutic phase.
The second phase, the pharmacokinetic phase, is composed of four processes: absorption,
distribution, metabolism (or biotransformation), and excretion (or elimination).
In the pharmacodynamics phase, a biologic or physiologic response result.
5.1-PHARMACEUTIC
Approximately 80% of drugs are taken by mouth. The pharmaceutic phase (dissolution) is the
first phase of drug action. In the gastrointestinal (GI) tract, drugs need to be in solution so they
can be absorbed.
A drug in solid form (tablet or capsule) must disintegrate into small particles to dissolve into a
liquid, a process known as dissolution. Drugs in liquid form are already in solution.
Tablet disintegration dissolution
Tablets are not 100% drug. Fillers and inert substances, generally called excipients, are used in
drug preparation to allow the drug to take on a particular size and shape and to enhance drug
dissolution. Some additives in drugs, such as the ions potassium (K) and sodium (Na) in
penicillin potassium and penicillin sodium, increase the absorbability of the drug.
Penicillin is poorly absorbed by the GI tract because of gastric acid. However, by making the
drug potassium or sodium salt, penicillin can then be absorbed.
 Disintegration is the breakdown of a tablet into smaller particles.
 Dissolution is the dissolving of the smaller particles in the GI fluid before absorption.
Rate of dissolution is the time it takes the drug to disintegrate and dissolves to become available
for the body to absorb it. Drugs in liquid form are more rapidly available for GI absorption than
are solids.
Generally, drugs are both disintegrated and absorbed faster in acidic fluids with a pH of 1 or 2
rather than in alkaline fluids. Alkaline drugs would become ionized and have difficulty crossing
cell membrane barriers.
Both the very young and older adults have less gastric acidity; therefore, drug absorption is
generally slower for those drugs absorbed primarily in the stomach.
Enteric-coated drugs resist disintegration in the gastric acid of the stomach, so disintegration
does not occur until the drug reaches the alkaline environment of the small intestine.
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Enteric-coated tablets can remain in the stomach for a long time; therefore, their effect may be
delayed in onset.
Enteric-coated tablets or capsules and sustained-release (beaded) capsules should not be
crushed. Crushing would alter the place and time of absorption of the drug.
Food in the GI tract may interfere with the dissolution of certain drugs.
Some drugs irritate the gastric mucosa, so fluids or food may be necessary to dilute the drug
concentration and to act as protectants.
5.2-PHARMACOKINETICS
Pharmacokinetics is defined as ‘what does the body do with the drug’. The body directs the
drug to the receptor site and then eliminates the drug from the site of action.
Most often the drugs are administered orally (per os).
Following administration, two main pharmacokinetic events determine the route of a drug:
invasion and evasion.
 Invasion involves the absorption and distribution,
 Evasion involves biotransformation and excretion of the drug.
 Instead of evasion, the term ‘elimination’ is more frequently used in the literature.
The four processes are absorption, distribution, metabolism (or biotransformation), and excretion
(or elimination).
The nurse applies knowledge of pharmacokinetics when assessing the patient for possible
adverse drug effects.
The nurse communicates assessment findings to members of the health care team in a timely
manner to promote safe and effective drug therapy for the patient.
1. Absorption
Absorption is the process by which the drug enters in to the systemic circulation from the site of
administration through biological barrier.
Absorption is the movement of drug particles from the GI tract to body fluids by passive
absorption, active absorption, or pinocytosis (Biotransport of drug: It is translocation of a solute
from one side of the biological barrier to the other).
In case of intravenous or intra-arterial administration the drug bypasses absorption processes and
it enters into the circulation directly.
Structure of biological membrane: The outer surface of the cell covered by a very thin
structure known as plasma membrane. It is composed of lipid and protein molecules. The
membrane proteins have many functions like
 contributing structure to the membrane acting as enzyme
 acting as carrier for transport of substances
 Acting as receptors.
The plasma membrane is a semipermeable membrane allowing certain chemical substances to
pass freely e.g. it allows water, glucose, etc. but it won’t allow sucrose until it is converted into
glucose and fructose.
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Passage of drug across membrane

 Passive transfer by Simple diffusion and Filtration
 Specialized transport by Facilitated diffusion, Active transport, Endocytosis.
i) Simple diffusion: Movement of a solute through a biological barrier from the phase of higher
concentration to phase of lower concentration. No need of energy e.g. highly lipid soluble drugs.
ii) Filtration: Is the process by which water soluble drug of relatively low molecular weight
crosses the plasma membrane through pores as a result of hydrodynamic pressure gradient across
the membrane e.g. urea and ethylene glycol.
iii) Facilitated diffusion: It means the passage of drug across the biological membrane along the
concentration gradient by the protein carrier mediated system also called as carrier mediated
diffusion. It depends on number of carrier e.g. tetracycline, pyrimidine.
iv) Active transport: The process by which drugs pass across the biological membrane most
often against their concentration gradient with the help of carriers along with the expenditure of
energy e.g. alpha methyl dopa, levodopa, 5-fluoro-uracil, 5 bromouracil.
v) Endocytosis: It is the process by which the large molecules are engulfed by the cell
membrane and releases them intracellularly e.g. protein, toxins (botulinum, diphtheria)
The GI membrane is composed mostly of lipid (fat) and protein, so drugs that are lipid soluble
pass rapidly through the GI membrane. Water-soluble drugs need a carrier, either enzyme or
protein, to pass through the membrane. Large particles pass through the cell membrane if they
are non-ionized (have no positive or negative charge). Weak acid drugs such as aspirin are less
ionized in the stomach, and they pass through the stomach lining easily and rapidly.
An infant’s gastric secretions have a higher pH (alkaline) than those of adults; therefore, infants
can absorb more penicillin. Certain drugs such as calcium carbonate and many of the antifungals
need an acidic environment to achieve greater drug absorption; thus food can stimulate the
production of gastric acid. Hydrochloric acid destroys some drugs such as penicillin G; therefore
a large oral dosage of penicillin is needed to offset the partial dose loss. Drugs administered by
many routes do not pass through the GI tract or liver. These include parenteral drugs, eyedrops,
eardrops, nasal sprays, respiratory inhalants, transdermal drugs, and sublingual drugs.
Remember, drugs that are lipid soluble and non-ionized are absorbed faster than water-soluble
and ionized drugs.
Blood flow, pain, stress, hunger, fasting, food, and pH affect drug absorption. Poor circulation to
the stomach as a result of shock, vasoconstrictor drugs, or disease hampers absorption. Pain,
stress, and foods that are solid, hot, or high in fat can slow gastric emptying time, so the drug
remains in the stomach longer. Exercise can decrease blood flow
by causing more blood to flow to the peripheral muscle, thereby decreasing blood circulation to
the GI tract.
Drugs given IM are absorbed faster in muscles that have more blood vessels (e.g., deltoids) than
in those that have fewer blood vessels (e.g., gluteals). Subcutaneous tissue has fewer blood
vessels, so absorption is slower in such tissue.
Page 26
Some drugs do not go directly into the systemic circulation following oral absorption but pass
from the intestinal lumen to the liver via the portal vein. In the liver, some drugs may be
metabolized to an inactive form that may then be excreted, thus reducing the amount of active
drug. Some drugs do not undergo metabolism at all in the liver, and others may be metabolized
to drug metabolite, which may be equally or more active than the original drug. The process in
which the drug passes to the liver first is called the first-pass effect, or hepatic first pass.
Most drugs given orally are affected by first-pass metabolism. Lidocaine and some nitroglycerins
are not given orally because they have extensive first-pass metabolism and therefore most of the
dose would be destroyed.
Drug routes and first pass effects
First pass routes Non first pass routes
 Hepatic arterial  Aural (instilled into the ear)
 Oral  Buccal
 Portal venous  Inhaled
 Rectal  Intra-arterial
 Intramuscular
 Intranasal
 Intraocular
 Intravaginal Intravenous
 Subcutaneous
 Sublingual
 Transdermal
Site of absorption
Most oral drugs are absorbed into the surface area of the small intestine through the action of the
extensive mucosal villi. Absorption is reduced if the villi are decreased in number because of
disease, drug effect, or the removal of small intestine.
Protein-based drugs such as insulin and growth hormones are destroyed in the small intestine by
digestive enzymes. Passive absorption occurs mostly by diffusion (movement from higher
concentration to lower concentration). With the process of diffusion, the drug does not require
energy to move across the membrane. Active absorption requires a carrier such as an enzyme or
protein to move the drug against a concentration gradient. Energy is required for active
absorption. Pinocytosis is a process by which cells carry a drug across their membrane by
engulfing the drug particles.
Bioavailability
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Bioavailability is a subcategory of absorption. It is the percentage of the administered drug dose

that reaches the systemic circulation. For the oral route of drug administration, bioavailability
occurs after absorption and first-pass metabolism. The percentage of bioavailability for the oral
route is always less than 100%, but for the IV route it is 100%. Oral drugs that have a high first-
pass hepatic metabolism may have a bioavailability of only 20% to 40% on entering systemic
circulation. To obtain the desired drug effect, the oral dose could be higher than the drug dose for
IV use.
Factors affecting drug absorption and bioavailability:
 Physico-chemical properties of drug
 Nature of the dosage form
 Physiological factors
 Pharmacogenetic factors
 Disease states.
Other Factors that alter bioavailability include
1. the drug form (e.g., tablet, capsule, sustained-release, liquid, transdermal patch, rectal
suppository, inhalation),
2. route of administration (e.g., oral, rectal, topical, parenteral),
3. GI mucosa and motility,
4. food and other drugs, and
5. Changes in liver metabolism caused by liver dysfunction or inadequate hepatic blood
flow.
A decrease in liver function or a decrease in hepatic blood flow can increase the bioavailability
of a drug, but only if the drug is metabolized by the liver.
Fewer drugs are destroyed by hepatic metabolism in the presence of liver disorder. With some
oral drugs, rapid absorption increases the bioavailability of the drug and can cause an increase in
drug concentration. Drug toxicity may result. Slow absorption can limit the bioavailability of the
drug, thus causing a decrease in drug serum concentration.
a. Physico-chemical properties of drug:
 Physical state: Liquids are absorbed better than solids and crystalloids absorbed better than
colloids.
 Lipid or water solubility: Drugs in aqueous solution mix more readily than those in oily
solution. However at the cell surface, the lipid soluble drugs penetrate into the cell more
rapidly than the water soluble drugs.
 Ionization: Most of the drugs are organic compounds. Unlike inorganic compounds, the
organic drugs are not completely ionized in the fluid. Unionized component is predominantly
lipid soluble and is absorbed rapidly and an ionized is often water soluble component which
is absorbed poorly. Most of the drugs are weak acids or weak bases. It may be assumed for
all practical purposes, that the mucosal lining of the G.I.T is impermeable to the ionized form
of a weak organic acid or a weak organic base. These drugs exist in two forms.
o Acidic drugs: rapidly absorbed from the stomach e.g. salicylates and barbiturates
Page 28
o Basic drugs: Not absorbed until they reach to the alkaline environment i.e. small
intestine when administered orally e.g. pethidine and ephedrine.
 Particle size: Small particle size is important for drug absorption. Drugs given in a dispersed
or emulsified state are absorbed better e.g. vitamin D and vitamin A.
b. Disintegration time and dissolution rate.
 Disintegration time: The rate of breakup of the tablet or capsule into the drug granules.
 Dissolution rate: The rate at which the drug goes into solution.
 Formulation: Usually substances like lactose, sucrose, starch and calcium phosphate are
used as inert diluents in formulating powders or tablets. Fillers may not be totally inert but
may affect the absorption as well as stability of the medicament. Thus a faulty formulation
can render a useful drug totally useless therapeutically.
c. Physiological factors
 Gastrointestinal transit time: Rapid absorption occurs when the drug is given on empty
stomach. However certain irritant drugs like salicylates and iron preparations are deliberately
administered after food to minimize the gastrointestinal irritation. But sometimes the
presence of food in the G.I tract aids the absorption of certain drugs e.g. griseofulvin,
propranolol and riboflavin.
 Presence of other agents: Vitamin C enhances the absorption of iron from the G.I.T.
Calcium present in milk and in antacids forms insoluble complexes with the tetracycline
antibiotics and reduces their absorption.
 Area of the absorbing surface and local circulation: Drugs can be absorbed better from
the small intestine than from the stomach because of the larger surface area of the former.
Increased vascular supply can increase the absorption.
 Enterohepatic cycling: Some drugs move in between intestines and liver before they reach
the site of action. This increases the bioavailability e.g. phenolphthalein.
 Metabolism of drug/first pass effect: Rapid degradation of a drug by the liver during the
first pass (propranolol) or by the gut wall (isoprenaline) also affects the bioavailability. Thus
a drug though absorbed well when given orally may not be effective because of its extensive
first pass metabolism.
d. Pharmacogenetics factors:
Individual variations occur due to the genetically mediated reason in drug absorption and
response.
e. Disease states:
Absorption and first pass metabolism may be affected in conditions like malabsorption,
thyrotoxicosis, achlorhydria and liver cirrhosis.
2. Distribution of Drugs
Page 29
Definition: Penetration of a drug to the sites of action through the walls of blood vessels from
the administered site after absorption is called drug distribution. Drugs distribute through various
body fluid compartments such as
 plasma
 interstitial fluid compartment
 Trans-cellular compartment.
Distribution is the process by which the drug becomes available to body fluids and body tissues.
Drug distribution is influenced by blood flow, the drug’s affinity to the tissue, and the protein-
binding effect. In addition, volume of drug distribution (Vd) is dependent on drug dose and its
concentration in the body. Drugs with a larger volume of drug distribution have a longer half-life
and stay in the body longer.
Apparent Volume of distribution (VD): The volume into which the total amount of a drug in
the body would have to be uniformly distributed to provide the concentration of the drug actually
measured in the plasma. It is an apparent rather than real volume.
Factors determining the rate of distribution of drugs:

1. Protein binding of drug:
As drugs are distributed in the plasma, many are bound to varying degrees (percentages) with
protein (primarily albumin). The portion of the drug that is bound is inactive because it is not
available to receptors, and the portion that remains unbound is free, active drug.
Only free drugs (drugs not bound to protein) are active and can cause a pharmacologic response.
As the free drug in the circulation decreases, more bound drug is released from the protein to
maintain the balance of free drug
Drugs bound to proteins cannot leave the systemic circulation to get to the site of action. This is
why only free drug is active.
2. Plasma concentration of drug (PC):
It represents the drug that is bound to the plasma proteins (albumins and globulins) and the drug
in free form. It is the free form of drug that is distributed to the tissues and fluids and takes part
in producing pharmacological effects. The concentration of free drug in plasma does not always
remain in the same level e.g.
 After I.V. administration plasma concentration falls sharply
 After oral administration plasma concentration rises and falls gradually.
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Clearance: Volume of plasma cleared off the drug by metabolism and excretion per unit time.
Protein binding reduces the amount of drug available for filtration at the glomeruli and hence
delays the excretion, thus the protein binding reduces the clearance.
Physiological barriers to distribution:
There are some specialized barriers in the body due to which the drug will not be distributed
uniformly in all the tissues. These barriers are:
1-Blood brain barrier (BBB)

 Is a special anatomic arrangement that aims to distribute only lipid-soluble drugs into the
brain and CSF e.g. General anaesthesia
 Ionized drugs & poorly soluble in fat are not allowed to enter into the brain and CSF.
 Antibiotics that cross the BBB with difficulty can NOT be used for CNS Infections such
as meningitis and encephalitis.
 The instillation of the drug INTRATHECALY to bypass the BBB will provide direct
effect against bacterial brain infection.
2-Placental Barrier: (PB)
 Is the membrane layers that separate the blood vessels of the mother and foetus.
 N.B.: Tissue enzymes in the placenta have the ability to metabolize some agents (e.g.
catecholamines) by inactivating them as they travel from maternal circulation to the
embryo.
 Unlike BBB, the non-selective passage of drugs across the placenta to the foetus is well-
established fact.
3-Metabolism of Drugs
Drugs are chemical substances, which interact with living organisms and produce some
pharmacological effects and then, they should be eliminated from the body unchanged or by
changing to some easily excretable molecules. The process by which the body brings about
changes in drug molecule is referred as drug metabolism or biotransformation.
Enzymes responsible for metabolism of drugs:

1. Microsomal enzymes: Present in the smooth endoplasmic reticulum of the liver, kidney and
GIT e.g. glucuronyl transferase, dehydrogenase, hydroxylase and cytochrome P450
2. non-microsomal enzymes: Present in the cytoplasm, mitochondria of different organs. E.g.
esterases, amidase, hydrolase
Types of biotransformation:
The chemical reactions involved in biotransformation are classified as phase-I and phase – II
(conjugation) reactions.
In phase-I reaction the drug is converted to more polar metabolite. If this metabolite is
sufficiently polar, then it will be excreted in urine. Some metabolites may not be excreted and
further metabolised by phase –II reactions.
Phase-I: Oxidation, reduction and hydrolysis.
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Phase-II: Glucuronidation, sulfate conjugation, acetylation, glycine conjugation and methylation

reactions.
Phase - I reactions
1. Oxidation: Microsomal oxidation involves the introduction of an oxygen and/or the removal
of a hydrogen atom or hydroxylation, dealkylation or demethylation of drug molecule e.g.
conversion of salicylic acid into gentisic acid.
2. Reduction: The reduction reaction will take place by the enzyme reductase which catalyze the
reduction of azo (-N=N-) and nitro (NO2) compounds e.g. prontosil converted to sulfonamide.
3. Hydrolysis: Drug metabolism by hydrolysis is restricted to esters and amines (by esterases
and amidases) are found in plasma and other tissues like liver. It means splitting of drug
molecule after adding water e.g. pethidine undergoes hydrolysis to form pethidinic acid. Other
drugs which undergo hydrolysis are atropine and acetylcholine.
Phase - II reactions (conjugation reactions):

This is synthetic process by which a drug or its metabolite is combined with an endogenous
substance resulting in various conjugates such as glucoronide, ethereal sulfate, methylated
compound and amino acid conjugates.
1. Glucuronide conjugation: It is the most common and most important conjugation reaction
of drugs. Drugs which contain Hydroxyl, amino or carboxyl group undergo this process e.g.
phenobarbitone.
2. Sulfate conjugation: Sulfotransferase present in liver, intestinal mucosa and kidney, which
transfers sulfate group to the drug molecules e.g. phenols, catechols, etc.
3. Acetyl conjugation: The enzyme acetyl transferase, which is responsible for acetylation, is
present in the kupffer cells of liver. Acetic acid is conjugated to drugs via its activation by CoA
to form acetyl CoA. This acetyl group is then transferred to-NH2 group of drug e.g. dapsone,
isoniazid.
4. Glycine conjugation: Glycine conjugation is characteristic for certain aromatic acids e.g.
salicylic acid, isonicotinic acid, p-amino salicylic acid. These drugs are also metabolized by
other path ways.
5. Methylation: Adrenaline is methylated to metanephrine by catechol-o-methyl transferase.
Here the source of methyl group is s – adenosyl methionine.
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Example of conditions and drugs that affect drug metabolism

Category. Example. Increase. Decrease
Disease. Cardiovascular. X
dysfunction
Renal insufficiency X
Condition. Starvation. X
Obstructive jaundice X
Genetic constitution. X
Fast acetylation. X
Slow acetylation X
Drugs. Barbiturates. X
Rifampin p450 inducer. X
Phenytoin p450 inducer. X
Ketoconazole p-450 inhibitor. X
4. Excretion of Drugs
Excretion of drugs means the transportation of unaltered or altered form of drug out of the body.
The major processes of excretion include renal excretion, hepatobiliary excretion and pulmonary
excretion. The minor routes of excretion are saliva, sweat, tears, breast milk, vaginal fluid, nails
and hair.
The rate of excretion influences the duration of action of drug. The drug that is excreted slowly,
the concentration of drug in the body is maintained and the effects of the drug will continue for
longer period.
DRUG THERAPY DURING PREGNANCY

A foetus is exposed to many of the same substances as the mother, including any drugs that she
takes-prescription, non-prescription, or street drugs. The first trimester of pregnancy is generally
the period of greatest danger of drug-induced developmental defects. Transfer of both drugs and
nutrients to the foetus occurs primarily by diffusion across the placenta, although not all drugs
cross the placenta. Recall from chemistry that diffusion is a passive process based on differences
in concentration between different tissues. Active transport requires the expenditure of energy
and often involves some sort of cell-surface protein pump. The factors that contribute to the
safety or potential harm of drug therapy during pregnancy can be broadly broken down into three
areas: drug properties, foetal gestational age, and maternal factors. Drug properties that impact
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drug transfer to the foetus include the drug's chemistry, dosage, and concurrently administered
drugs. Examples of relevant chemical properties include molecular weight, protein binding, lipid
solubility, and chemical structure. Important drug dosage variables include dose and duration of
therapy.
Foetal gestational age is an important factor in determining the potential for harmful drug effects
to the foetus. The foetus is at greatest risk for drug-induced developmental defects during the
first trimester of pregnancy. During this period, the foetus undergoes rapid cell proliferation.
Skeleton, muscles, limbs, and visceral organs are developing at their most rapid rate. Self-
treatment of minor illness is strongly discouraged anytime during pregnancy, but especially
during the first trimester. Gestational age is also important in determining when a drug can most
easily cross the placenta to the foetus. During the last trimester, the greatest percentage of
maternally absorbed drug gets to the foetus.
Although exposure of the foetus to drugs is most detrimental during the first trimester, drug
transfer to the foetus is more likely during the last trimester. This is the result of enhanced blood
flow to the foetus, increased foetal surface area, and increased amount of free drug in the
mother's circulation. It’s important to use drugs judiciously during pregnancy; however, there
are certain situations that require their use. Without drug therapy, maternal conditions such as
hypertension, epilepsy, diabetes, and infection could seriously endanger both the mother and the
foetus, and the potential for harm far out weight the risks of appropriate drug therapy
The FDA classifies drugs according to their safety for use during pregnancy. This system of drug
classification is based primarily on animal studies and limited human studies. This is due in part
to ethical dilemma surrounding the study of potential adverse effects on foetus.
DRUG THERAPY DURING BREASTFEEDING

Breastfed infants are at risk for exposure to drugs consumed by the mother. A wide variety of
drugs easily cross from the mother's circulation into the breast milk and subsequently to the
breastfeeding infant. Drug properties similar to those discussed in the previous section influence
the exposure of infants to drugs via breastfeeding. The primary drug characteristics that increase
the likelihood of drug transfer via breastfeeding include fat solubility, low molecular weight,
non-ionization, and high concentration.
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Fortunately, breast milk is not the primary route for maternal drug excretion. Drug levels in
breast milk are usually lower than those in the maternal circulation. The actual amount of
exposure depends largely on the volume of milk consumed. The ultimate decision as to whether
a breastfeeding mother takes a particular drug depends on the risk/benefit ratio. The risks of drug
transfer to the infant in relation to the benefits of continuing and the therapeutic benefits to the
mother must be considered on a case-by-case basis
PREGNANCY SAFETY CATEGORIES

CATEGORY DESCRIPTION
Category A Studies indicate no risk to the human foetus.
Category B Studies indicate no risk to the animal foetus but information for humans
is not available
Category C Adverse effects reported in the animal foetus, information for humans is
not available
Category D Possible foetal risk in humans has been reported; however, in selected
cases consideration of the potential benefit versus risk may warrant use
of these drugs in pregnant women
Category x Foetal abnormalities have been reported, and positive evidence of foetal
risk in humans is available from animal and/or human studies. These
drugs are not be used in pregnant women
Pharmacokinetic Changes in the Neonate and Paediatric Patient

Absorption
 Gastric pH is less acidic because acid-producing cells in the stomach are immature until
approximately 1 to 2 years of age.
 Gastric emptying is slowed because of slow or irregular peristalsis.
 First pass elimination by the liver is reduced because of the immaturity of the liver and
reduced levels of microsomal enzymes.
 Intramuscular absorption is faster and irregular
Distribution
 Total body water is 70% to 80% in full-term infants, 85% in premature new-borns, and
64% in children 1 to 12 years of age.
 Fat content is lower in young patients because of greater total body water.
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 Protein binding is decreased because of decreased production of protein by the immature

liver,
 More drugs enter the brain because of an immature blood-brain barrier.
Metabolism
 Levels of microsomal enzymes are decreased because the immature liver has not yet
started producing enough.
 Older children may have increased metabolism and require higher dosages once
hepatic enzymes are produced.
 Many variables affect metabolism in premature infants, infants, and children,
including the status of liver enzyme production, genetic differences. and substances to
which the mother was exposed during pregnancy.
Excretion
 Glomerular filtration rate and tubular secretion and resorption are all decreased in
young patients because of kidney immaturity.
 Perfusion to the kidneys may be decreased, which results in reduced renal function,
concentrating ability, and excretion of drugs.
PATIENT-CENTERED CARE: LIFESPAN CONSIDERATIONS FOR THE ELDERLY

PATIENT
Pharmacokinetic Changes
Absorption
 Gastric pH is less acidic because of a gradual reduction in the production of hydrochloric
acid in the stomach.
 Gastric emptying is slowed because of a decline in smooth muscle tone and motor
activity
 Movement throughout the gastrointestinal tract is slower because of decreased muscle
tone and motor activity
 Blood flow to the gastrointestinal tract is reduced by 40% to 50% because of decreased
cardiac output and decreased perfusion
 The absorptive surface area is decreased because the aging process blunts and flattens
villi
Distribution
 In adults 40 to 60 years of age, total body water is 55% in males and 47% in females, in
those older than 60 years of age, total body water is 52% in males and 46% in females.
 Fat content is increased because of decreased lean body mass.
 Protein (albumin) binding sites are reduced because of decreased production of proteins
by the aging liver and reduced protein intake.
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Metabolism
 The levels of microsomal enzymes are decreased because the capacity of the aging liver to
produce them is reduced.
 Liver blood flow is reduced by approximately 1.5% per year after 25 years of age, which
decreases hepatic metabolism.
Excretion
 Glomerular filtration rate is decreased by 40% to 50%, primarily because of decreased blood
flow.
 The number of intact nephrons is decreased.
5.3-PHARMACODYNAMICS
In general, drugs bind to macromolecules in tissues and cells, and drugs act following binding to
receptors. The binding is a prerequisite for the biological effects of drugs (latin:’Corpora non
agunt nisi fixata’-a particle does not act without binding). Exceptions:
 Those drugs that exert physical effect on the body, e.g. osmotically acting diuretic drugs
 Those drugs that neutralize other compounds chemically, e.g. basic protamine neutralizes
acidic heparin or desferroxamine chelate complex with ferric compounds
Receptors for drugs
Receptors are macromolecules (e.g. lipo-or glycoproteins) that, in the majority of cases, couple
with effector systems generating biological signals.
A. Agonists
The drug that binds to the receptor and produces an effect is called: agonist. When the drug binds
to receptor and inhibits the binding of another drug or hormone (neurotransmitter) the drug is
called: antagonist. The antagonist alone has no effect, that is, an antagonist by itself does not
generate a biological signal.
B. Antagonist
 Antagonists –by definition-have potency but lack of efficacy.
 Competitive antagonists reversibly bind to the receptor and the enhancement of the dose
of agonists displaces the antagonists from the receptor.
 Non-competitive antagonists bind strongly- in a partly or completely irreversible manner-
to the receptor. In the presence of a non-competitive antagonist even the higher doses of
an agonist are not able to produce maximum effects.
1. Receptor and Non-Receptor Mechanisms
Most of the drugs act by interacting with a cellular component called receptor. Some drugs act
through simple physical or chemical reactions without interacting with any receptor.
 Receptors are protein molecules present either on the cell surface or with in the cell e.g.
adrenergic receptors, cholinoceptors, insulin receptors, etc.
 The endogenous neurotransmitters, hormones, autacoids and most of the drugs produce
their effects by binding with their specific receptors.
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 Aluminium hydroxide and magnesium trisilicate, which are used in the treatment of
peptic ulcer disease act by non-receptor mechanism by neutralizing the gastric acid
Many drugs are similar to or have similar chemical groups to the naturally occurring chemical
and have the ability to bind onto a receptor where one of two things can happen- either the
receptor will respond or it will be blocked.
A drug, which is able to fit onto a receptor, is said to have affinity for that receptor.
Efficacy is the ability of a drug to produce an effect at a receptor.
An agonist has both an affinity and efficacy whereas antagonist has affinity but not efficacy or
intrinsic activity.
When a drug is able to stimulate a receptor, it is known as an agonist and therefore mimics the
endogenous transmitter. When the drug blocks a receptor, it is known as antagonist and therefore
blocks the action of the endogenous transmitter (i.e. it will prevent the natural chemical from
acting on the receptor).
However, as most drug binding is reversible, there will be competition between the drug and the
natural stimulus to the receptor.
The forces that attract the drug to its receptor are termed chemical bonds and they are
 hydrogen bond
 ionic bond
 covalent bond
 Vander waals force.
Covalent bond is the strongest bond and the drug-receptor complex is usually irreversible.
When first messengers like neurotransmitters, hormones, autacoids and most of drugs bind with
their specific receptors, the drug receptor complex is formed which subsequently causes the
synthesis and release of another intracellular regulatory molecule termed as second messengers
e.g. cyclic AMP, calcium, cyclic GMP, inositol triphosphate (IP3), diacylglycerol and
calmodulin which in turn produce subcellular or molecular mechanism of drug action.
2. Site of drug action:

A drug may act:
a. Extracellularly e.g.: osmotic diuretics, plasma expanders.
b. On the cell surface e.g.: digitalis, penicillin,
c. Inside the cell e.g.: anti-cancer drugs, steroid hormones.
3. Dose Response relationship
The exact relationship between the dose and the response depends on the biological object under
observation and the drug employed. When a logarithm of dose as abscissa and responses as
ordinate are constructed graphically, the “S” shaped or sigmoid type curve is obtained
The lowest concentration of a drug that elicits a response is minimal dose, and the largest
concentration after which further increase in concentration will not change the response is the
maximal dose.
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 Graded dose effect: As the dose administered to a single subject or tissue increases, the
pharmacological response also increases in graded fashion up to ceiling effect. It is used for
characterization of the action of drugs. The concentration that is required to produce 50 % of
the maximum effect is termed as EC50 or ED50.
 Quantal dose effect: It is all or none response, the sensitive objects give response to small
doses of a drug while some will be resistant and need very large doses. The quantal dose-
effect curve is often characterized by stating the median effective dose and the median lethal
dose.
o Median lethal dose or LD50: This is the dose (mg/kg), which would be expected to kill
one half of a population of the same species and strain.
o Median effective dose or ED50: This is the dose (mg/kg), which produces a desired
response in 50 per cent of test population.
o Therapeutic index: It is an approximate assessment of the safety of the drug. It is the
ratio of the median lethal dose and the median effective dose. Also called as therapeutic
window or safety.
LD 50
o Therapeutic index (T. I) =
ED 50
The larger the therapeutic index, the safer is the drug. Penicillin has a very high therapeutic
index, while it is much smaller for the digitalis preparation.
Formulae
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4. Structural activity relationship

The activity of a drug is intimately related to its chemical structure. Knowledge about the
chemical structure of a drug is useful for:
 Synthesis of new compounds with more specific actions and fewer adverse reactions
 Synthesis of competitive antagonist and Understanding the mechanism of drug action
 Slight modification of structure of the compound can change the effect completely.
5.4 PHARMACOTHERAPEUTICS
5.5 TOXICOLOGY
Before drug therapy is initiated, an end point or expected outcome of therapy needs to be
established. This desired therapeutic outcome is patient-specific, established in collaboration
with the patient, and, if appropriate, determined with other members of the health care team.
Outcomes need to be clearly defined and must be either measurable or observable by monitoring.
Outcome goals must be realistic and prioritized so that drug therapy begins with interventions
that are essential to the patient's well-being. Examples include curing a disease, eliminating or
reducing a pre-existing symptom, arresting or slowing a disease process, preventing a disease or
other unwanted condition, or otherwise improving quality of life. These goals and outcomes are
not the same as nursing goals and outcomes.
Patient therapy assessment is the process by which a practitioner integrates his or her knowledge
of medical and drug- related facts with information about a specific patient's medical and social
history. Items to be considered in the assessment are drugs currently used (prescription, over-the-
counter, herbal, and illicit or street drugs), pregnancy and breastfeeding status, and concurrent
illnesses that could contraindicate initiation of a given medication. A contraindication for a
medication is any patient condition, especially a disease state that makes the use of the given
medication dangerous for the patient. Careful attention to this assessment process helps to ensure
an optimal therapeutic plan. The implementation of a treatment plan can involve several types
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and combinations of therapies. The type of therapy can be categorized as acute, maintenance,
supplemental (or replacement), palliative, supportive, prophylactic, or empiric
Acute Therapy
Acute therapy often involves more intensive drug treatment and is implemented in the acutely ill
(those with rapid onset of illness) or the critically ill. It is often needed to sustain life or treat
disease. Examples are the administration of vasopressors to maintain blood pressure and cardiac
output after open heart surgery, the use of volume expanders for a patient who is in shock, and
intensive chemotherapy for a patient with newly diagnosed cancer.
Maintenance Therapy
Maintenance therapy does not eradicate problems the patient may already have but will prevent
progression of a disease or Condition. It is used for the treatment of chronic illnesses such as
hypertension. In the latter case, maintenance therapy maintains he patient's blood pressure within
given limits, which prevents certain end-organ damage. Another example of maintenance
Therapy is the use of oral contraceptives for birth control.
Supplemental Therapy
Supplemental (or replacement) therapy supplies the body with a substance needed to maintain
normal function. This substance may be needed either because it cannot be made by the body or
because it is produced in insufficient quantity. Examples are the administration of insulin to
diabetic patients and of iron to patients with iron-deficiency anaemia.
Palliative Therapy
The goal of palliative therapy is to make the patient as comfort- able as possible. Palliative
therapy focuses on providing patients with relief from the symptoms, pain, and stress of a serious
illness. The goal is to improve quality of life for both the patient and the family. It is typically
used in the end stages of an illness when attempts at curative therapy have failed; however, it can
be provided along with curative treatment. Examples are the use of high-dose opioid analgesics
to relieve pain in the final stages of cancer.
Supportive Therapy
Supportive therapy maintains the integrity of body functions while the patient is recovering from
illness or trauma. Examples are provision of fluids and electrolytes to prevent dehydration in a
patient with influenza who is vomiting and has diarrhoea. and administration of fluids, volume
expanders, or blood products to a patient who has lost blood during surgery,
Prophylactic Therapy and Empiric Therapy
Prophylactic therapy is drug therapy provided to prevent illness or other undesirable outcome
during planned events. A common example is the use of preoperative antibiotic therapy for
surgical procedures. The antibiotic is given before the incision is made, so that the antibiotic can
kill any potential pathogens. Another example is the administration of disease-specific vaccines
to individuals traveling to geographic areas where a given disease is known to be endemic.
Empiric therapy is based on clinical probabilities. It involves drug administration when a certain
pathologic condition has an uncertain but high likelihood of occurrence based on the patient's
initial presenting symptoms. A common example is use of antibiotics active against the organism
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most commonly associated with a specific infection before the results of the culture and
sensitivity reports are available.
Monitoring
Once the appropriate therapy has been implemented, the effectiveness of the therapy-that is, the
clinical response of the patient to the treatment-must be evaluated. Evaluating the clinical
response requires familiarity with both the drug's intended therapeutic action (beneficial effects)
and its unintended possible adverse effects (predictable adverse drug reactions). Examples of
monitoring include observing for the therapeutic effect of reduced blood pressure following
administration of antihypertensive drugs and observing for the toxic effect of leukopenia after
administering antineoplastic (cancer chemotherapy) drugs. Another example is performing a pain
assessment after giving pain medication. It should be noted that this text generally highlights
only the most common adverse effects of a given drug; however, the drug may have many other
less commonly reported adverse effects. Always keep in mind that patients may sometimes
experience less common and less readily identifiable adverse drug effects. Consult
comprehensive references, pharmacists, or poison and drug information centre staff when there is
uncertainty regarding adverse effects that a patient may be experiencing.
All drugs are potentially toxic and can have cumulative effects. Recognizing these toxic effects
and knowing their manifestations are integral components of the monitoring process. A drug can
accumulate when it is absorbed more quickly than it is eliminated or when it is administered
before the previous dose has been metabolized or cleared from the body. Knowledge of the
organs responsible for metabolizing and eliminating a drug combined with knowledge of how a
particular drug is metabolized and excreted enables the nurse to anticipate problems and treat
them appropriately if they occur.
Therapeutic Index
The ratio of a drug's toxic level to the level that provides therapeutic benefits is referred to as the
drug's therapeutic index. The safety of a particular drug therapy is determined by this index. A
low therapeutic index means that the difference between a therapeutically active dose and a toxic
dose is small. A drug with a low therapeutic index has a greater likelihood than other drugs of
causing an adverse reaction, and therefore its use requires closer monitoring. Examples of such
drugs are warfarin and digoxin. In contrast, a drug with a high therapeutic index, such as
amoxicillin, is rarely associated with overdose events
Drug Concentration
All drugs reach a certain concentration in the blood. Drug concentrations can be an important
tool for evaluating the clinical response to drug therapy. Certain drug levels are associated with
therapeutic responses, whereas other drug levels are associated with toxic effects. Toxic drug
levels are typically seen when the body's normal mechanisms for metabolizing and excreting
drugs are compromised. This commonly occurs when liver and kidney functions are impaired or
when the liver or kidneys are immature (as in neonates). Dosage adjustments should be made in
these patients to appropriately accommodate their impaired metabolism and excretion.
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Patient's Condition
Another patient-specific factor to be considered is the patient's concurrent diseases or other
medical conditions. A patient's response to a drug may vary greatly depending on physiologic
and psychological demands. Disease of any kind, infection, cardiovascular function, and GI
function are just a few of the physiologic elements that can alter a patient's therapeutic response.
Stress, depression, and anxiety can also be important psychological factors affecting response.
Tolerance and Dependence
To provide optimal drug therapy, it is important to understand and differentiate between
tolerance and dependence. Tolerance is a decreasing response to repeated drug doses.
Dependence is a physiologic or psychological need for a drug. Physical dependence is the
physiologic need for a drug to avoid physical withdrawal symptoms (e.g., tachycardia in an
opioid-addicted patient). Psychological dependence is also known as addiction and is the
obsessive desire for the euphoric effects of a drug. Addiction typically involves the recreational
use of various drugs such as benzodiazepines, opioids, and amphetamines.
Interactions
Drugs may interact with other drugs, with foods, or with agents administered as part of
laboratory tests. Knowledge of drug interactions is vital for the appropriate monitoring of drug
therapy. The more drugs a patient receives, the more likely that a drug interaction will occur.
This is especially true in older adults, who typically have an increased sensitivity to drug effects
and are receiving several medications. In addition, over-the-counter medications and herbal
therapies can interact significantly with prescribed medications. Food also can interact
significantly with certain drugs. See Table 2for the most common food and drug interactions.
Alteration of the action of one drug by another is referred to as drug interaction. A drug
interaction can either increase or decrease the actions of one or both of the involved drugs Drug
interactions can be either beneficial or harmful. Numerous drug interactions can occur and have
been reported. Please note that only those drug interactions that are considered to be significant
with at least a good probability of occurring and/or those that require dosage therapy adjustment
are discussed in this textbook. An authoritative resource may be used as a means of exploring all
possible drug interactions.
Concurrently administered drugs may interact with each other and alter the pharmacokinetics of
one another during any of the four phases of pharmacokinetics: absorption, distribution,
metabolism, or excretion. Most commonly drug interactions occur when there is competition
between two drugs for metabolizing enzymes, such as the cytochrome P-450 enzymes listed in
Table . As a result, the speed of metabolism of one or both drugs may be enhanced or reduced.
This change in metabolism of one or both drugs can lead to sub therapeutic or toxic drug actions.
Many terms are used to categorize drug interactions. When two drugs with similar actions are
given together, they can have additive effects (1+1=2). Examples are the many combinations of
analgesic products, such as antihistamine and opioid combinations (e.g. promethazine and
codeine) for treatment of cold symptoms, and acetaminophen and opioid combinations (e.g.,
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acetaminophen and oxycodone) for treatment of pain. Often drugs are used together for their
additive effects so that smaller doses of each drug can be given.
Synergistic effects occur when two drugs administered together interact in such a way that their
combined effects are greater than the sum of the effects for each drug given alone (1+1=greater
than 2). The combination of hydrochlorothiazide with lisinopril for the treatment of hypertension
is an example.
Antagonistic effects are said to occur when the combination of two drugs results in drug effects
that are less than the sum of the effects for each drug given separately (1 + 1 = less than 2). An
example of this type of interaction occurs when the antibiotic ciprofloxacin is given
simultaneously with antacids, vitamins, iron, or dairy products. These drugs reduce the
absorption of ciprofloxacin and lead to decreased effectiveness of the antibiotic.
Incompatibility is a term most commonly used to describe 1 parenteral drugs. Drug

incompatibility occurs when two parenteral drugs or solutions are mixed together and the result
is a chemical deterioration of one or both of the drugs or the formation of a physical precipitate.
The combination of two such drugs usually produces a precipitate, haziness, or colour change in
the solution. Before administering any intravenous medication, the nurse must always inspect the
bag for precipitate. If the solution appears cloudy or if visible flecks are seen, the bag must be
discarded and not given to the patient. An example of incompatible drugs is the combination of
parenteral furosemide and heparin.
COMMON FOOD AND DRUG INTERACTIONS

FOOD DRUG (CATEGORY) RESULT
Leafy green warfarin (anticoagulant) Decreased anticoagulant effect from
vegetables warfarin
Dairy products tetracycline, levofloxacin, ciprofloxacin, Chemical binding of the drug leading
moxifloxacin (antibiotics) to decreased effect and treatment
failures
Grapefruit juice amiodarone (antidysrhythmic). buspirone Decreased metabolism of drugs and
(antianxiety).carbamazepine increased effects
(antiseizure), cyclosporine, tacrolimus
(immunosuppressants), felodipine,
nifedipine, nimodipine, nisoldipine
(calcium channel blockers), simvastatin,
atorvastatin (anticholesterol drugs)
Aged cheese, wine Monoamine oxidase inhibitors Hypertensive crisis
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EXAMPLES OF DRUG INTERACTIONS AND THEIR EFFECTS ON

PHARMACOKINETICS
PHARMACOKINETIC DRUG MECHANISM RESULT
PHASE COMBINATION
Absorption Antacid with Antacids bind to the Decreased

levofloxacin levofloxacin effectiveness
preventing adequate of
absorption levofloxacin,
resulting from
decreased
blood levels
(harmful)
Distribution warfarin with Both drugs compete Higher levels
amiodarone for protein-binding of free
sites (unbound)
warfarin and
amiodarone,
which
increases
actions of both
drugs
(harmful)
Metabolism erythromycin with Both drugs compete Decreased
cyclosporine for the same hepatic metabolism of
enzymes cyclosporine,
possibly
resulting in
toxic levels of
cyclosporine
(harmful)
Excretion amoxicillin with Inhibits the secretion Elevation and

probenecid of amoxicillin into the prolongation of
kidneys plasma levels
of amoxicillin
(can be
beneficial)
Page 45
Adverse Drug Events

The recognition of the potential hazards and detrimental effects of medication use is a topic that
continues to receive much attention in the literature. This focus has contributed to an increasing
body of knowledge regarding this topic as well as the development of new terminology. Health
care institutions are under increasing pressure to develop effective strategies for preventing
adverse effects of drugs.
Adverse drug event (ADE) is a broad term for any undesirable occurrence involving
medications. A similarly broad term also seen in the literature is drug misadventure. Patient
outcomes associated with adverse drug events vary from no effects to mild discomfort to life-
threatening complications, permanent disability, disfigurement, or death. Adverse drug events
can be preventable or non-preventable. Fortunately, many adverse drug events result in no
measurable patient harm. Adverse drug events can be both external and internal. The most
common causes of adverse drug events external to the patient are errors by caregivers (both
professional and nonprofessional) and mal- functioning of equipment (e.g., intravenous infusion
pumps). An adverse drug event can be internal, or patient induced, such as when a patient fails to
take medication as prescribed or drinks alcoholic beverages that he or she was advised not to
consume while taking a given medication. An impending adverse drug event that is noticed
before it actually occurs is considered a potential adverse drug event (and appropriate steps must
be taken to avoid such a "near miss" in the future). A less common situation, but one still worth
mentioning, is an adverse drug withdrawal event. This is an adverse outcome associated with
discontinuation of drug therapy, such as hypertension caused by abruptly discontinuing blood
pressure medication or return of infection caused by stopping antibiotic therapy too soon.
The two most common broad categories of adverse drug event are medication errors and
adverse drug reactions. A medication error is a preventable situation in which there is a
compromise in the "Six Rights" of medication use: right drug, right dose, right time, right route,
right patient, and right documentation. Medication errors are more common than adverse drug
reactions. Medication errors occur during the prescribing, dispensing, administering, or
monitoring of drug therapy. These four phases are collectively known as the medication use pro
cess.
TOXICOLOGY
The study of poisons and unwanted responses to both drugs and other chemicals is known as
toxicology. Toxicology is the science of the adverse effects of chemicals on living organisms.
Clinical toxicology deals specifically with the care of the poisoned patient. Poisoning can result
from a variety of causes, ranging from drug overdose to ingestion of household cleaning agents
to snakebite. Poison control centres are health care institutions equipped with sufficient
personnel and information resources to recommend appropriate treatment for the poisoned
patient.
Effective treatment of the poisoned patient is based on a system of priorities, the first of which
is to preserve the patient's vital functions by maintaining the airway, ventilation, and circulation.
The second priority is to prevent absorption of the toxic substance and/or speed its elimination
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from the body using one or more of the variety of clinical methods available. Several common
poisons and their specific antidotes are listed in the Table below;
COMMON POISON AND THEIR ANTIDOTES*

SUBSTANCE ANTIDOTE
Acetaminophen Acetylcysteine Atropine
Organophosphates (e.g, insecticides) Ateopine
Tricyclic antidepressants, quinidine Sodium bicarbonate
Calcium channel blockers Intravenous calcium
Iron salt Deferoxamine
Digoxin and other cardiac glycosides Digoxin antibodies
Ethylene glycol (eg. automotiveantifreeze Ethanol (same as alcohol used for drinking).
solution), methanol given intravenously
Benzodiazepines Flumazenil
Beta blockers Glucagon
Opiates, opioid drugs Naloxone
Carbon monoxide (by inhalation] Oxygen (at high concentration). known as
bariatric therapy
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CHAPTER SIX
DRUG DOSAGE CALCULATION
A. Factors modifying the dosage and action of drugs:
Individuals differ both in the degree and the character of the response that a drug may elicit and
therefore the optimum dose of a drug which produces the desired therapeutic effect varies from
person to person. The important factors which influence the effect of a drug are:
1. Drug intolerance: It is a quantitative deviation from the anticipated response to a given dose
of a drug. Thus drug intolerance is inability of the individual to tolerate a drug. It is also called as
hyper susceptibility.
2. Sex difference: Special care should be exercised when drugs are administrated during
menstruation, pregnancy and lactation.
3. Menstruation: Drugs producing pelvic congestion should be avoided during menstruation e.g.
drastic purgatives.
4. Pregnancy: During pregnancy, the use of all drugs except those essential to maintain
pregnancy should be used with caution. Drugs which may stimulate the uterine smooth muscle
are contraindicated during pregnancy. Further, many drugs administered to mother are capable of
crossing the placenta and affecting the foetus. Most of drugs can produce teratogenicity when
they are used in pregnancy. Teratogenicity means congenital malformation
i) Drugs known to produce teratogenicity e.g. thalidomide, cyclophosphamide,
methotexate, tetracyclines, phenytoin, carbamazepine and progestogens.
ii) Drugs may be teratogenic e.g. Warfarin, lithium, quinine, primaquine, trimethoprim,
rifampicin, anaesthetic agents.
5. Breast feeding: Nearly all agents received by mother are likely to be found in her milk and
could theoretically harm the infant. Most of the lipid soluble drugs get into breast milk.
Therefore the drugs, which are excreted in the milk and harm the infant health should be,
avoided by breast-feeding mothers e.g. sulphonamides, tetracyclines, nalidixic acid, isoniazid,
diazepam, lithium, Indomethacin, aspirin, etc.
6. Body Weight: The average dose is mentioned either in terms of mg per kg body weight or as
the total single dose for an adult weighing between 50-100kg. However, dose expressed in this
fashion may not apply in cases of excessively obese individuals or those suffering from oedema
or dehydration nutritional factors can sometimes alter drug metabolizing capacity and this should
be kept in mind in malnourished patients.
7. Age: The pharmacokinetics of many drugs changes with age. Thus gastric emptying is
prolonged and the gastric pH fluctuates in neonates and infant, further the liver capacity to
metabolize drugs is low, renal function is less developed and the proportion of body water is
higher in the new-born and the neonates. Hence children may not react to all drugs in the same
fashion as young adults. With a few exceptions, drugs are more active and more toxic in the new
born than the adults.
The paediatric doses are expressed in terms of body weight (mg/kg per dose or day) or in terms
of body surface area (mg/m2per day). The body surface area can be calculated from the height
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and weight of the child. Like children, old people also present problems in dosage adjustment
and this may vary widely with different people. The metabolism of drugs may diminish in the
elderly and the renal function declines with age. Elderly are sensitive to the drugs like hypnotics,
tranquilizers, phenylbutazone, drugs in the same fashion as young
8. Disease state: Some antimicrobial agents penetrate the cerebrospinal fluid well across the
normal meninges while other antimicrobials penetrate well only when the meninges are
inflammed (meningitis) e.g. sulphonamides, metronidazole, chloramphenicol, isoniazid and
rifampicin penetrate well through the normal meninges and other antimicrobial agents like
benzyl penicillin, ampicillin, tetracycline, streptomycin, gentamicin and cephalosporin penetrate
only when the meninges are inflammed.
Acute or chronic liver diseases markedly modify the rate and extent of biotransformation of
drugs. The t1/2 of chlordiazepoxide and diazepam in patients with liver cirrhosis is greatly
increased with corresponding prolongation of their effects.
Cardiac disease by limiting blood flow to the liver may impair disposition of those drugs whose
biotransformation is flow limited e.g. imipramine, isoniazid, lignocaine, morphine and
propranolol.
Similarly renal and pulmonary diseases may modify the biotransformation of drugs like insulin
or isoprenaline. Excretion of drug is impaired in chronic renal disease.
SEE SLIDES FOR CALCULATIONS
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CHAPTER SEVEN
DRUG DEVELOPMENT AND EVALUATION
The ultimate aim of pharmacological studies in animals is to find out a therapeutic agent suitable
for clinical evaluation in man. No doubt, animal studies provide analogies and serve as useful
models. The administration of biologically active agent to human beings is associated with an
element of risk, which cannot be predicted by even the most careful and exhaustive animal
experiments. Scientists all over the world are in a continuous effort to develop new drugs
although drug development is an extremely technical and enormously expensive operation.
Among the contributors to new drug development, pharmacologists are more concerned in
evaluating ―new chemical entities‖ (NCE). Synthesis and evaluation of thousands of NCEs are
usually necessary for new drugs to be introduced in the market.
Research and development of new drugs have been done under strict government regulations
which have greatly increased over the past couple of decades. Drug development comprises of
two steps.
 Preclinical development and
 Clinical development
a. Preclinical development: Synthesis of new chemical entities is done as per research policy
decision which is based on:
(i) Random synthesis
(ii) Structure activity relationship (SAR)
(iii) Biochemical and pharmacological insight and
(iv)Chance finding
The aim of the preclinical development phase for a potential new medicine is to explore the
drug’s efficacy and safety before it is administrated to patients. In this preclinical phase, varying
drug doses are tested on animals and/or in vitro systems.
If active compounds are found, then studies on animals are done which include
pharmacodynamics, pharmacokinetics, toxicology and special toxicological studies
(mutagenicity and carcinogenicity) have to be done.
In this study single dose is used for acute toxicity and repeated doses for sub chronic and chronic
toxicity studies. Most of the preclinical tests have to be conducted in accordance with the
standards prescribed
b. Clinical development: About one in 1000 NCEs reach this stage.

The steps to be studied in this stage include:
 Pharmaceutical study
 Pharmacological study
 Clinical trial.
1. Pharmaceutical study covers stability of formulation and compatibility of the NCEs with other
tablet or infusion ingredients.
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2. Pharmacological study includes further chronic toxicological study in animal, initially animal
metabolic and pharmacokinetic study. When studies in animals predict that a NCE may be useful
medicine i.e. effective and safe in relation to its benefits, then the time has come to put it to the
test in man i.e. clinical trial.
3. Studies on human or Clinical Trial: Clinical trial is a means by which the efficacy of drug is
tested on human being. It may also give some idea about the risk involved. It is divided into 4
phases. With each phase, the safety and efficacy of the compound are tested progressively.
Phase - I: This is the first exposure of the new drug on man which is usually conducted in
healthy volunteers and which is designed to test the tolerable dose, duration of action. This phase
is usually carried out in only one centre on 20 to 50 subjects.
Phase - II: This phase comprises small scale trials on patients used to determine dose level and
establish that the treatment offers some benefit. It usually involves 100-500 patients and is
usually conducted in several centres.
Phase - III: Full scale evaluation of treatment comparing it with standard treatment is done in
this phase. It involves randomised control trials on 250 to 2000 patients and is done in multiple
centres. Information from all studies are received by the ―Committee of safety of medicines‖
(CSM). If the drug is satisfied by the CSM, the product license is issued then the drug is
marketed.
Phase - IV: It is also called as phase of post marketing surveillance. Reports about efficacy and
toxicity are received from the medical practitioners and reviewed by the committee of review of
medicines. Renewal or cancellation of the product license depends on the comment of the review
committee.
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CHAPTER EIGHT
CLASSIFICATION OF DRUGS
Pharmacologic Classification
 Similar Characteristics
Similar Chemical Makeup – examples: Penicillins, Beta Blockers
 Therapeutic Classification
Used for similar effect
May not have similar chemical make up – Examples: Antihypertensives, Antibiotics
Allopathic Drugs: The term "Allopathy" refers to the principle of curing a disease by
administering substances that produce the opposite effect of the disease when given to a healthy
human.
Allopathic drugs can be further classified as:
Non Prescription Drugs: Non Prescription Drugs are the drugs, which can be purchased from a
pharmacy without the prescription of a doctor. Non-prescription drugs are also called as Over-
the-counter drugs (OTC drugs).
i. Anti-Haemorrhoid Drugs
 Anti-Haemorrhoid Drugs are medicines that reduce the swelling and relieve the
discomfort of haemorrhoids.
 Anti-haemorrhoid drugs are available as creams, ointments and suppositories.
 Most can be bought without a physician's prescription.
ii. Topical Antibiotics
 Topical Antibiotics are medicines applied to the skin to kill bacteria.
 Topical Antibiotics helps in preventing infections caused by bacteria that get into minor
cuts, scrapes, and burns.
 Treating minor wounds with Antibiotics allows quicker healing.
 If the wounds are left untreated, the bacteria will multiply, causing pain, redness,
swelling, itching, and oozing.
iii. Cough-Suppressants
 Cough Suppressants are medicines that prevent or stop coughing.
 Cough Suppressants act on the center in the brain that controls the cough reflex.
 They are meant to be used only to relieve dry, hacking coughs associated with colds and
flu.
 They should not be used to treat coughs that bring up mucus or the chronic coughs
associated with smoking, Asthma, Emphysema or other lung problems.
iv. Anti-acne Drugs
 Anti-acne drugs are medicines that help clear up pimples, black heads, white heads, and
more severe forms of acne.
 Different types of anti-acne drugs are used for different purposes.
 For example, lotions, soaps, gels, and creams containing benzoyl peroxide or tretinoin
may be used to clear up mild to moderately severe acne.
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v. Non-steroidal Anti-inflammatory Drugs

 Non-steroidal Anti-inflammatory Drugs are medicines that relieve pain, swelling,
stiffness, and inflammation.
 Non-steroidal Anti-inflammatory Drugs (NSAIDs) are prescribed for a variety of painful
conditions, including Arthritis, Bursitis, Tendinitis, Gout, sprains, strains, and other
injuries.
 Non-steroidal Anti-inflammatory Drugs relieve pain, stiffness, swelling, and
inflammation, but they do not cure the diseases or injuries responsible for these problems.
vi. Antiseptics
 Antiseptics are medicines that slow or stop the growth of germs and help prevent
infections in minor cuts, scrapes, and burns.
 Antiseptics are applied to the skin to keep bacteria from getting into wounds and causing
infection.
 Although Antiseptics do not usually kill bacteria, they do weaken them and slow their
growth. Simply applying an Antiseptic to a wound is not adequate treatment.
 The wound should be cleaned first and in most cases it should be covered with a bandage
or other type of dressing to keep it clean and moist while it heals.
 However, some Antiseptics, such as Phenol, can damage the skin if the wound is covered
after they are applied.
vii. Analgesics
 Analgesics are medicines that relieve pain.
 Analgesics are prescribed to relieve pain of all sorts - headaches, backaches, joint pain, sore
muscles and pain that results from surgery, injury or illness.
 Among the most common Analgesics are Aspirin, Choline Salicylate, Magnesium Salicylate
and Sodium Salicylate.
viii. Salicylates Drug Classifications
 Ibuprofen, Naproxen Sodium and Ketoprofen are all in the general category known as Non-
Steroidal Anti- Inflammatory Drugs (NSAIDs).
 NSAIDs relieve pain and also reduce inflammation.
 Another common analgesic, Acetaminophen provides pain relief but does not reduce
inflammation.
ix. Vasodilator
 Vasodilators are medicines that act directly on muscles in blood vessel walls to make
blood vessels widen (dilate).
 Vasodilators are used to treat high blood pressure (hypertension).
 By widening the arteries, these drugs allow blood to flow through more easily, reducing
blood pressure.
x. Antacids: Antacids are medicines that neutralize stomach acid.
 Antacids are used to relieve acid indigestion, upset stomach, sour stomach, and heartburn.
 Some antacid products also contain the ingredient Simethicone to relieve gas.
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 Antacids are taken by mouth and work by neutralizing excess stomach acid.
 Antacids contain ingredients such as Aluminum Hydroxide, Calcium Carbonate,
Magnesium Hydroxide, and Sodium Bicarbonate, alone or in various combinations.
xi. Expectorants
 Expectorants are drugs that loosen and clear mucus and phlegm from the respiratory tract.
 Guaifenesin is an ingredient in many cough medicines, such as anti--Tuss, Dristan Cold
& Cough, Guaifed, GuaiCough, and some Robitussin products.
 Some products that contain guaifenesin are available only with a physician's prescription;
others can be bought without a prescription.
 They come in several forms, including capsules, tablets, and liquids.
xii. Anti-fungal Drugs
 Many fungi are harmless, some cause minor and irritating infections while a few can
cause much more severe infections.
 People with compromised immune systems, such as AIDS and cancer patients, may be
more susceptible to fungal infections than others.
 Anti-fungal drugs are used to treat fungal infections.
xiii. Anti-Histamines
 Antihistamines are drugs that block the action of histamine (a compound released in
allergic inflammatory reactions) at the H1 receptor sites, responsible for immediate
hypersensitivity reactions such as sneezing and itching.
 By inhibiting the activity of histamine, they can reduce capillary fragility, which
produces the erythema, or redness, associated with allergic reactions.
 They will also reduce histamine-induced secretions, including excessive tears and
salivation
xiv. Antigas Agents
 Antigas Agents are medicines that relieve the uncomfortable symptoms of too much gas
in the stomach and intestines.
 Antigas agents help relieve the symptoms by preventing the formation of gas pockets and
breaking up gas that already is trapped in the stomach and intestines.
 Antigas agents are sold as capsules, liquids, and tablets (regular and chewable) and can
be bought without a physician's prescription.
xv. Smoking Cessation Drugs
 Smoking-cessation Drugs are medicines that help people stop smoking cigarettes or using
other forms of tobacco.
 People who smoke cigarettes or use other forms of tobacco often have a difficult time
when they try to stop.
 Most Smoking-Cessation products contain nicotine, but the Nicotine is delivered in
small, steady doses spread out over many hours.
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 Smoking Cessation Drugs that contain Nicotine are also called Nicotine Substitution
products or Nicotine Replacement therapy. • Smoking Cessation Drugs come in four
forms- chewing gum, skin patch, nasal spray, and inhaler.
 Another type of Smoking Cessation drug, Bupropion (Zyban) also reduces craving and
withdrawal symptoms, but it contains no Nicotine.
xvi. Anti-Histamines
CHAPTER NINE
DRUG ADMINISTRATION AND MEDICATION ERRORS
9.1-GUIDELINES FOR THE USE OF MEDICATIONS

1. When preparing or giving medicines, concentrate your whole attention on what you are doing.
2. Make certain that you have a written order for every medication you will administer.
3. Read the label before taking, while using, and returning the drug to its place.
4. All medicines should be labelled and the label should be clear.
5. Never give medicine from unlabelled container.
6. Never give a put a drug in a bottle that has a different label. For example, if you have kefex
that you need to put it in a bottle, and you have empty bottle that was used to contain ampecillin,
don’t put the keflex in that bottle.
7. Measure quantities and calculate doses as ordered in proper way
8. Handling tablets, capsules and pills properly and DO’NOT touch with fingers. Use the cap of
the container to guide or from the container to the cup directly.
9. Avoid wastage of medicine.
10. Never administer medications prepared by another person; otherwise you will bear the
responsibility of any mistake.
11. Some preparations as insulin, vaccines & suppositories need to be kept in the refrigerator 2-
8º C.
12. Stay with the patient until he takes his medicine.
13. All mixtures should be made immediately before use.
14. NEVER return unused drug to a stock bottle.
15. Don’t add any drug to the blood; interactions may occur without visible changes.
16. Don’t use any sterile article that gets unsterile by any way.
17. Don’t use clear solutions which have become cloudy or have sediment.
18. Don’t use a drug that is out date.
19. Don’t use a drug that has changes its color.
20. Don’t use a drug which arise doubt in mind.
21. All medicines should be kept in cupboard, NARCOTICS in a locked one.
22. Narcotics have a rule controlling their ordering, giving, and their registration.
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23. Many liquids should be diluted with water or other liquids. ―This is especially when
medicine has a bad taste.
24. Exceptions to this rule, cough medicines are not diluted, or the patient not allowed drinking
water after taking cough syrup.
25. Don’t leave a tray of medicines unattended. If you are in a patient’s room and must leave,
take the tray with you.
26. Never chart a medicine as having been given, until it has been administered.
27. Follow up the rights of medication administration (14 rights)
1. Right patient.
2. Right drug.
3. Right dose.
4. Right route of administration.
5. Right time
6. Right documentation
7. Right personnel
8. Right diagnosis
9. Right assessment
10. Right refusal
11. Right technique
12. Right evaluation
13.
14.
Tolerance: Decrease physiologic response to the repeated administration of a drug or chemically
related substances which necessities increase in dosage to maintain a given therapeutic effect e.g.
morphine.
Dependence (addiction): When the body is getting used to function in the presence of a certain
drug. The body will not perform its normal functions in the absence of that drug.
Substitute: these are many different drugs which may use to treat a single disease. From these
drugs, always present a drug of choice, if not available the others are considered as the substitute.
Antidote: a drug used to antagonize the toxic effect of another drug and to neutralize its
symptoms.
9.2-SIX FUNDAMENTAL RIGHTS OF MEDICATION ADMINISTRATION

Right Drug
The "right drug" begins with the registered nurse's valid license to practice. Some states allow
currently licensed practical nurses to administer medications with specific guidelines. The
registered nurse is responsible for checking all medication orders and/or prescriptions. To ensure
that the correct drug is given, you must check the specific medication order against the
medication label or profile three times before giving the medication. Conduct the first check of
the right drug/drug name while you prepare the medication for administration. At this time,
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consider whether the drug is appropriate for the patient and, if doubt exists or an error is deemed
possible, contact the prescriber and/pharmacist immediately.
All medication orders or prescriptions are required by law se, right time, to be signed by the
prescriber involved in the patient's care. If a verbal order is given, the prescriber must sign the
order within 24 hours or as per facility protocol. Verbal and/or telephone orders are often used in
emergencies and time-sensitive patient care situations. To be sure that the right drug is given,
information about the patient and drug (see previous discussion of the assessment phase) must be
obtained to make certain that all variables and data have been considered. Approved, current
authoritative references (see earlier discussion) are the reliable sources of information about
prescribed drugs. Avoid relying upon the knowledge of peers as this is unsafe nursing practice.
Remain current in your knowledge of generic (nonproprietary) drug names as well as trade
names (proprietary name that is registered by a specific drug manufacturer); however, use of the
drug's generic name is now preferred in clinical practice to reduce the risk of medication errors.
A single drug often has numerous trade names, and drugs in different classes may have similarly
spelled names, increasing the possibility of medication errors. Therefore, when it comes to the
"right drug" phase of the medication administration process, use of a drug's generic name is
recommended to help avoid a medication error and enhance patient safety.
Right Dose
Whenever a medication is ordered, a dosage is identified from the prescriber's order. Always
check the dose and confirm that it is appropriate for the patient's age and size. Also, check the
prescribed dose against the available drug stocks and against the normal dosage range. Recheck
all mathematical calculations, and pay careful attention to decimal points, the misplacement of
which could lead to a tenfold or even greater overdose, Leading zeros, or zeros placed before a
decimal point, are allowed. but trailing zeros, or zeros following the decimal point, are to be
avoided. For example, 0.2 mg is allowed, but 2.0 mg is not acceptable, because it could easily be
mistaken for 20 mg, especially with unclear penmanship, Patient variables (eg, vital signs, age,
gender, weight, height) require careful assessment because of the need for dosage adjustments in
response to specific parameters. Pediatric and elderly patients are more sensitive to medications
than younger and middle-age adult patients; thus, use extra caution with drug dosage amounts for
these patients.
Right Time
Each health care agency or institution has a policy regarding routine medication administration
times; therefore, always check this policy. However, when giving a medication at the prescribed
time, you may be confronted with a conflict between the timing suggested by the prescriber and
specific pharmacokinetic or pharmacodynamic drug properties, concurrent drug therapy,
dietary influences, laboratory and/or diagnostic testing, and specific patient variables. For
example, the prescribed right time for administration of antihypertensive drugs may be four
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times a day, but for an active, professional 42-year-old male patient working 14 hours a day,
taking a medication four times daily may not be feasible, and this regimen may lead to
noncompliance and subsequent complications. Appropriate actions include contacting the
prescriber and inquiring about the possibility of prescribing another drug with a different dosing
frequency (eg, once or twice daily)
Right Route
As previously stated, you must know the particulars about each medication before administering
it to ensure that the right drug, dose, and route are being used. A complete medication order
includes the route of administration. If a medication order does not include the route, be sure to
ask the prescriber to clarify it. Never assume the route of administration.
Right Patient
Checking the patient's identity before giving each medication dose is critical to the patient's
safety. Ask the patient to state his or her name, and then check the patient's identification band to
confirm the patient's name, identification number, age, and allergies. With paediatric patients, the
parents and/or legal guardians are often the ones who identify the patient for the purpose of
administration of prescribed medications. With new-borns and in labour and delivery situations,
the mother and baby have identification bracelets with matching numbers, which must be
checked before giving medications. With elderly patients or patients with altered sensorium or
level of consciousness, ask- ing the patient his or her name or having the patient state his or her
name is neither realistic nor safe. Therefore, checking
the identification band against the medication profile, medication order, or other treatment or
service orders is crucial to avoid errors.
Right Documentation
Documentation of information related to medication administration is crucial to patient safety.
Recording patient observations and nursing actions has always been an important ethical
responsibility, but now it is becoming a major medical-legal consideration as well. Because of its
significance in professional nursing practice, correct documentation is becoming known as the "6
right of medication administration Always assess the patient's chart for the presence of the
following information date and time of medication adm name of medication, dose, route, and site
of administration
 Documentation of drug action may also be made in the regularly schedule assessments
for changes in symptoms the patient is experiencing adverse effects, toxicity, and any
other drug related physical and/or psychosocial symptoms.
 Documentation must also reflect any improvement in the patient's condition, symptoms,
disease process as well as no change or lack of improvement. You must not only
document these observations, but report them to the prescriber promptly in keeping with
your critical thinking and judgment.
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 Document any teaching, as well as an assessment of the degree of understanding

exhibited by the patient
9.3-MEDICATION ERRORS
When the Six Rights (and other rights) of drug administration are discussed, medication errors
must be considered. Medication errors are a major problem for all of health care, regardless of
the setting. The National Coordinating Council for Medication Error Reporting and Prevention
defines a medication error as any preventable event that may cause or lead to inappropriate
medication use or patient harm while the medication is in the control of the health care
professional, patient, or consumer. Such events may be related to professional practice, health
care products, procedures, or systems, including prescribing order communication; product
labelling, packaging, and nomenclature; compounding: dispensing: distribution; administration;
education; monitoring; and use. Both patient-related and system-related factors must always be
considered when the medication administration process and the prevention of medication errors
are being examined.
How to Prevent Medication Errors
 As the first step to defend against errors, assess information about drug allergies, vital
signs, and laboratory test results
 Use two patient identifiers before giving medications
 Never give medications that you have not drawn up or prepared yourself
 Minimize the use of verbal and telephone orders, be sure to repeat the order to confirm
with the prescriber Speak slowly and clearly, and spell the drug name aloud
 List the reason for use of each drug on the indication administration record and any
educational materials
 Avoid abbreviations, medical shorthand and any because they can lead to confusion,
miscommunication, and risk of error
 Never assume anything about any drug order or prescription, including route.
 If a medication order is questioned for any reason (e.g. dose, drug, and indication), never
assume that the prescriber is correct Always be the patient's advocate and investigate the
matter until all ambiguities are resolved.
 Do not try to decipher illegibly written orders; instead, contact the prescriber for
clarification. Illegible orders fall below applicable standards for quality medical care and
endanger patient safety. If in doubt about any part of an order, always check with the
prescriber. Compare the medication order against what is on hand by checking for the
Right Drug. Right Dose, Right Time, Right Patient, and Right Route.
 Never use trailing zeros (e.g. 1.0 mg) in writing and/or transcribing medication orders
Use of trailing zeros is associated with increased occurrence of overdose. For example,
1.0 mg warfarin sodium could be misread as "10 mg warfarin, a tenfold dose increase
Instead, use "1 mg" or even "one mg.
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 “Failure to use leading zeros can also lead to overdose. For example, 25 mg digoxin
could be misread as 25 mg digoxin, a dose that is 100 times the dose ordered. Instead,
write "0.25 mg"
 Carefully read all labels for accuracy, expiration dates, dilution requirements, and
warnings (e.g., black box warnings).
 Remain current with new techniques of administration and new equipment. Encourage
the use of generic names to avoid medication errors due to many sound-alike trade
names. .
 Listen to and honour any concerns expressed by patients. If the patient voices a concern
about being allergic to a medication or states that a pill has already been taken or that the
medication is not what he or she usually takes-then STOP, listen, and investigate
 Strive to maintain your own health to remain alert, and never be too busy to stop, learn,
and inquire, In addition, engage in ongoing continuing education.
 Become a member of professional nursing organizations to network with other nursing
students or professional nurses to advocate for improved working conditions and to stand
up for the rights of nurses and patients.
 Know where to find the latest Information on which dosage forms can or should not be
crushed or opened (e.g. capsules), and educate patients. Accordingly, Safeguard any
medications that the patient had on admission or transfer so that additional doses are not
given or taken by mistake. In such situations, Safeguarding is accomplished by compiling
a current medication history and resolving any discrepancies rather than ignoring them.
 Always verify new medication administration records if they have been rewritten or re-
entered for any reason, and follow policies and procedures about this action.
 Make sure the weight of the patient is always recorded before carrying out a medication
order to help decrease dosage errors.
 •Provide for mandatory recalculation of every drug dosage for high-risk drugs (e.g.,
highly toxic drugs) or high-risk patients (e.g. paediatric or elderly patients) because there
is a narrow margin between therapeutic serum drug levels and toxic levels (e.g., for
chemotherapeutic or digitalis drugs, or in the presence of altered liver or kidney function
in a patient).
 Always suspect an error whenever an adult dosage form is dispensed for a paediatric
patient. Sook translators when appropriate-never guess what patients are trying to say
 Educate patients to take an active role in medication error prevention, both in the hospital
setting and at home
 Involve yourself politically in advocating for legislation that improves patient safety
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NUS 122: GENERAL PHARMACOLOGY AND DRUG ADMINISTRATION 2023/2024

GENERAL PHARMACOLOGY AND

NGU SANDRA LEM

1.2 THE NURSING PROCESS AND DRUG THERAPY

3-Planning Goals and Outcome Criteria

CURRENT NANDA-I-APPROVED NURSING DIAGNOSES MOST RELEVANT TO

 Activity intolerance and risk for

GO TO THE YOUR WORK BOOK AND ANSWER QUESTIONS

 Contraindication: Any condition, especially one related to a disease state or patient

 Therapeutic effect: The desired or intended effect of a particular medication.

GO TO THE YOUR WORK BOOK AND ANSWER QUESTIONS

2.2 DRUG SCHEDULES (CATEGORIES OF CONTROLLED SUBSTANCES)

Factors that influence drug dosage and action

Dosage forms depend on:

TYPES OF DOSAGE FORM: PHYSICAL

Unshaped Gels, creams, ointments, pastes

TYPES OF DOSAGE FORM: ROUTE OF ADMINISTRATION

ROUTE OF DRUG ADMINISTRATION AND RELATED NURSING CONSIDERATION

Subcutaneous injections are recommended to be

routes and is based on thorough assessment of the

dosage form. Suppositories are inserted using a

Factors governing Choice of routes of drug administration

Tablet disintegration dissolution

Passage of drug across membrane

Bioavailability is a subcategory of absorption. It is the percentage of the administered drug dose

Factors determining the rate of distribution of drugs:

1-Blood brain barrier (BBB)

Enzymes responsible for metabolism of drugs:

Phase-II: Glucuronidation, sulfate conjugation, acetylation, glycine conjugation and methylation

Phase - II reactions (conjugation reactions):

Example of conditions and drugs that affect drug metabolism

DRUG THERAPY DURING PREGNANCY

DRUG THERAPY DURING BREASTFEEDING

PREGNANCY SAFETY CATEGORIES

Pharmacokinetic Changes in the Neonate and Paediatric Patient

 Protein binding is decreased because of decreased production of protein by the immature

PATIENT-CENTERED CARE: LIFESPAN CONSIDERATIONS FOR THE ELDERLY

2. Site of drug action:

4. Structural activity relationship

Incompatibility is a term most commonly used to describe 1 parenteral drugs. Drug

COMMON FOOD AND DRUG INTERACTIONS

EXAMPLES OF DRUG INTERACTIONS AND THEIR EFFECTS ON

Absorption Antacid with Antacids bind to the Decreased

Excretion amoxicillin with Inhibits the secretion Elevation and

Adverse Drug Events

COMMON POISON AND THEIR ANTIDOTES*

SEE SLIDES FOR CALCULATIONS

b. Clinical development: About one in 1000 NCEs reach this stage.

v. Non-steroidal Anti-inflammatory Drugs

9.1-GUIDELINES FOR THE USE OF MEDICATIONS

9.2-SIX FUNDAMENTAL RIGHTS OF MEDICATION ADMINISTRATION

 Document any teaching, as well as an assessment of the degree of understanding

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