CHAPTER 1: DRUG ACTIONS

Drugs maybe synthetic chemicals, chemical obtained from plants,

➢ Medicines - drugs that are used to treat or prevent disease or other conditions
➢ Drugs - substances other than food that change the structure or function of the body or mind
○ All medicines are drugs, but not all drugs are medicines
Difference between Drugs and Medicine
➢ Drugs
○ Substances that cause a change in a person’s physical and/or psychological state
○ Single chemical substance in a medicine that alters the structure or function of some of the body’s biological processes
➢ Medicine
○ Drug or combination of drugs that is intended to prevent illness, cure disease, and pain relievers
○ Used to cure, prevent or treat discomfort
○ Must have 3 of these characteristics:
■ effectiveness - good at carrying out its task
■ safety - safe when used as directed
■ minor side effects
○ Medicines usually contain other substance besides the active drug to make them more convenient to use
○ Only antibiotics are tested to ensure side effects are only minor and not significantly damaging to one’s health

Definitions of Terms
➢ Pharmacology - deals with the study of drugs, their sources, appearances, chemistry, their actions and uses on living organisms
➢ Pharmacy - practice of preparing and dispensing drugs
➢ Posology - the branch of pharmacology and therapeutics concerned with the determination of the doses of remedies
➢ Pharmacotherapeutics - the study of how drugs may be best used in the treatment of disease
○ Ie which drug would be the most or least appropriate for a patient
➢ Pharmacotherapy - the treatment of disease by means of drugs
➢ Pharmacodynamics - study of the biochemical and physiological effects of drugs as well as their mechanism of action or study
of the action of drugs on living organisms
➢ Pharmacokinetics - deals with liberation, absorption, distribution, biotransformation and excretion of drugs
 ➢ Pharmacognosy - branch of pharmacology concerned with physical characteristics and botanical sources of crude drugs
➢ Chronopharmacology - study of the relationship between the time of drug administration and the pharmacological effects
produced
➢ Toxicology - science of poisons, their sources, chemical composition, action, tests and antidotes or study of poisons and
poisoning
➢ Therapeutic agents - drugs used in treating patient’s illness
➢ Pharmaceutic phase - first phase of drug action
➢ Pharmacokinetic phase - process of drug movement to achieve drug action
○ Drug absorption process by which drug is made available to body fluids for distribution
➢ Drug distribution - refers to the ways in which drugs are transported by the circulating body fluids to the sites of action
(receptors), metabolism and excretion
➢ Drug excretion - elimination of metabolites of drugs, and in some cases, active drug itself from the body
➢ Onset of action - time it takes to reach the minimum effective concentration (MEC) after a drug is administered
➢ Peak action - occurs when the drug reaches its highest blood plasma concentration
➢ Duration of action - length of time the drug has a pharmacologic effect
➢ Critical concentration - amount of drug needed to cause a therapeutic effect
➢ Half life - measure of time required for elimination of half the drug from the body

Sources of Drugs
● Plants ● Mineral (inorganic compounds)
○ Digitalis products ○ Aluminum
○ Opiates ○ Fluoride
○ Ergotrates ○ Iron
● Animals ○ Gold
○ Insulin ● Synthetic drugs
○ Thyroid drugs ○ Produced in the lab
○ Growth hormone preparations ○ Synthetic chemicals/genetically engineered
Examples of Mineral Based Drugs ● Ferrous sulfate - anemia
 ● Magnesium sulfate - purgative
● Sodium bicarbonate - antacid
● Aluminum hydroxide - antacid

Examples of Animal Based Drugs

● Heparin - leech
● Insulin - pork pancreas
● Thyroxin - thyroid
● Vitamin B12 - liver extract
● Cod liver oil
● Anti toxic care

Drug Laws
● All drugs must meet certain rigid standards
● Approval of new drugs through
○ US FDA
○ FDA of the Philippines (formerly BFAD)
● RA 6675
○ Generic Act of 1988
○ An act to promote, require and ensure the production of an adequate supply, distribution, use and acceptance of drugs
and medicines identified by their generic names
● RA 6425
○ Dangerous Drugs Act of 1972
○ Includes prohibited drugs such as opium, heroin, etc. and restricted drugs
● RA 9165
○ Dangerous Drugs Act of 2002
○ Repeals RA 6425
○ Objectives
 ■ To safeguard the integrity of the territory of the state and the well-being of its citizenry particularly the youth
from harmful effects of unregulated drugs
■ To provide effective mechanisms or measure to reintegrate into society individuals who have fallen victims to
drug abuse or dangerous drug dependence through sustainable programs of treatment and rehabilitation
● RA 953
○ Narcotic Drug Law
○ Approved: June 20, 1953
● RA 9502
○ Universally Accessible Cheaper and Quality Medicines Act of 2008

Standardizing Drugs
● References on Drug Standards
○ Main section - contain essential medicines for primary care facilities
○ PIMS - Philippine Index of Medical Specialties
○ MIMS - Medimedia Index of Medical Specialties
○ Pharmacopoeia (United States - USP) - includes detailed monographs on drug substances and dosage forms
○ Formulary (National Formulary) - contains monographs on pharmaceutic ingredients
○ Essential Drugs List (EDL)
■ Derived from the Philippine National Drug Formulary (PNDF)
■ Intended for used in the RHUs for primary medical care
■ It contains list of drugs useful in meeting the immediate therapeutic needs of the great majority of the
population

Drug Nomenclature
● Chemical name - describes the drug’s chemical structure
○ First name to be applied to drug during its early stages of development
● Generic name - the official nonproprietary name for the drug
○ Not owned by any drug company
○ Universally accepted
 ○ Given before the drug becomes official
● Brand (trade) name - chosen by the drug company
○ Also known as proprietary name
○ Usually registered trademark owned by that specific \\oompany
○ Drug companies market a compound using its brand name
● Official name - name under which the drug is listed
○ Also known as the generic name

3 Phases of Drug Action

1. Pharmaceutic phase - also termed as the dissolution phase
a. Dissolution - the first phase of drug action; the disintegration of solid form of a drug into a liquid form
i. Need to be in a solution so they can be absorbed in the GI tract
ii. Drugs in solid form must disintegrate into small particles to dissolve into liquid
iii. Drugs in liquid form are already in solution
b. Excipients - fillers and inert substances used in drug preparation to allow the drug to take on a particular size and shape
and to enhance drug dissolution
c. Additives - can increase its absorbability
d. Disintegration - the breakdown of a tablet into smaller particles
e. Rate limiting - time it takes the drugs to disintegrate and dissolve to become available for the body to absorb it
i. Enteric-coated drugs - resist disintegration in the gastric acid of the stomach
1. Disintegration does not occur until drug reaches alkaline environment of small intestine
2. Remain in the stomach for a long time thus, effect may be delayed in onset
3. Should not be crushed
ii. Rate of Dissolution - time it take the drug to disintegrate and dissolve to become available for the body to
absorb it**
1. Generally drugs are both disintegrated and absorbed faster in acidic fluids with a ph 1 or 2 rather than in
alkaline fluids
2. Liquid form drugs are more rapidly available for GI absorption than are solids
2. Pharmacokinetic phase
a. Process of drug movement to achieve drug action - includes absorption, distribution, metabolism, and excretion
b. Absorption - process by which a drug is made available to the body fluids for distribution
i. First step in the passage of a drug through the body, unless it is introduced directly into the bloodstream by IV
administration
ii. Movement of drug particles:
1. Passive - occurs mostly by diffusion
2. Active - requires a carrier such as an enzyme or protein to move the drug against a concentration
gradient
3. Pinocytosis - process by which cells carry a drug across their cell membrane by engulfing drug particles
iii. Rate of absorption depends on:
1. Route of drug administration
2. Blood flow through the tissue at the point of drug administration
3. Solubility of the drug
iv. Lipid soluble and nonionized drugs are absorbed faster than water soluble or ionized drugs
v. First pass effect (Hepatic first pass) - process in which the drug passes to the liver first
1. Large percentage of oral doses will be destroyed by liver enzymes and sometimes not reaching the site
intended for the drug
vi. Bioavailability - subcategory of absorption; the percentage of the administered drug dose that reaches systemic
circulation
1. Oral route = < 100%
2. IV route = 100 %
3. Factors that alter bioavailability
a. Drug form
b. Route of administration
c. GI mucosa and motility
d. Food and other drugs
e. Changes in liver metabolism
c. Distribution - process by which the drug becomes available to body fluids and body tissues
 i. Involves movement of drug to the bodies tissues the portion of the drug that gets through the first pass effect is
delivered to criculation for transport throughout the body
ii. Factors that affect distribution:
1. Drug lipid solubility and ionization (blood flow)
2. Perfusion of the reactive tissue (drug’s affinity to the tissue)
3. Protein binding - many drugs are bound to proteins
a. Highly protein-bound - drugs greater than 89% bound to protein
b. Moderately highly protein-bound - drugs 61-89% bound to protein
c. Moderately protein-bound - drugs 30-60% bound to protein
d. Low protein-bound - less than 30% bound to protein
e. Free drugs - drugs not bound to protein
i. The ONLY active part of the drug because there is an available receptor site
ii. Causes pharmacologic response
iii. Protein-drug complex is relatively large and cannot enter into the capillaries and then into tissue to react drug
must be freed from protein binding site at the tissues
1. Some drugs are tightly bound and are released slowly = long duration of action
2. Some drugs are loosely bound and disperse faster = shorter duration of action
3. Portion of the drug that is bound is inactive because it is not available to receptors
4. Portion that remain unbound is free, active drug and causes pharmacologic response
d. Metabolism or biotransformation - process by which body inactivates drugs
i. Factors that affect metabolism:
1. Age
2. Nutrition
3. Insufficient amounts of major body hormones
ii. Large percentage of drugs are lipid soluble thus, the liver metabolizes the lipid-soluble substances to a water
soluble substance for renal excretion
iii. Some drugs are transformed into active metabolites = increased pharmacologic response
iv. Half-life - (t1/2) drug is the time it takes for one half of the drug concentration to be eliminated
 1. By knowing half life, you will know the time it takes for a drug to reach a steady state of serum
concentration can be computed
e. Excretion or elimination - elimination of metabolites of drugs and, sometimes, the active drug itself
i. The skin, saliva, lungs, bile and feces are some of the routes used to excrete drugs
ii. Kidneys - main route of drug elimination
iii. Factors that affect elimination:
1. Renal excretion
2. Drugs can affect elimination of other drugs
3. Blood concentration levels
4. Half-life of a drug
3. Pharmacodynamic phase
a. Effect occurs
b. Drug-receptor interaction
c. Drug is available for action
i. Maximal efficacy - all drugs have a maximum drug effect

Receptor Theory
● Many drugs are thought to act on specific areas on cell membrane called receptor sites
● Drug binding sites are primarily on proteins, glycoproteins, proteolipids and enzymes
● Four receptor families:
○ Kinase-linked receptors - ligand-binding domain for drug binding is on the cell surface
■ Drug activates enzyme inside the cell and response is initiated
○ Ligand-gated ion channels - channel spans the cell membrane, this receptor then opens the channel which allows for
flow of ions into and out of cells
■ Ions are primarily sodium and calcium
○ G protein-coupled receptor systems - 3 components
■ Receptor
■ G protein that binds to GTP
■ Effector (either enzyme or ion channel)
 Drug (activates) → Receptors (activates) → G protein (activates) → Effect/Pharmacological Response
○ Nuclear receptors - found in cell nucleus (not on surface) of cell membrane
■ Activation of receptors through transcription factors is prolonged compared to first 3 receptor groups
(activation is rapid)
● The better the drug fits into receptor site = more biologically reactive the drug is
● Agonist - produce an effect
● Antagonist - block an effect
● How drug acts/works in the body:
○ According to purpose/use/action:
■ Prophylactic - prevent occurrence of a disease or to lessen its severity if it does occur
● Ie rabies vaccine or dengue vaccine
■ Palliative or symptomatic - relieve distressing symptoms
● Ie acetaminophen/Tylenol/Ibuprofen
■ Curative or specific - eliminate disease
● Ie antibiotics
■ Supportive - sustain the patient until measures can be instituted that will either cure or other treatments can be
given
■ Substitute or replacement - replace substance normally found in the body but which are absent or diminished in
amount
● Ie blood transfusion, IVF, PNSS
■ Supplementary - added as a supplement or something that supplies a deficiency
● Ie vitamins, B-complex supplements
■ Chemotherapeutic - uses of certain chemical or drugs in the treatment of certain disease
■ Restorative - drugs that help return the body to its normal state
■ Diagnostic - help the physician determine whether a disease is present
○ According to:
■ Prescription - require an order from a healthcare professional for a specific medicine
■ Nonprescription - does not need an order from a healthcare professional and can be bought over-the-counter
Effects of Drugs
● Major type of drug responses
○ Local or topical - drugs whose major effect takes place at the point of contact with the body or the desired site of action
○ Systemic - result from the entrance of the drug into the circulatory system and its subsequent transport
■ Selective action - systemic drugs that affect a specific organ/organs
■ General action - drugs appear to affect the body as a whole
○ Therapeutic index - estimates margin of safety of a drug through use of ratio that measures the effective dose (ED) in
50% of people and the other 50% lethal dose (LD)
○ Therapeutic effect - primary effect intended; the reason the drug is intended or the desired effect
○ Side effect - secondary effects; unintended
○ Adverse or toxic effect - implies abnormal, undesirable or harmful effects
○ Idiosyncratic effect - unexpected peculiar response to drug; either over or under response of the body to the drug
○ Allergic effect - hypersensitivity reaction or immunologic reaction to a drug
○ Drug tolerance - decreased physiologic response to repeated administration of a drug
○ Drug interaction - effect of one drugs are modified by prior or concurrent administration of another drug
■ Synergistic - increase potency or reduce the undesirable effects of the drugs
■ Antagonistic - counteracts effects
○ Anaphylactic reaction - severe life-threatening allergic reaction
○ Cumulative effect - when a drug is excreted slowly, it tends to accumulate in the system, giving rise to toxic symptoms
○ Drug tolerance - developing resistance to the effects of a drug; needing increased dose or frequency of drug
administration
○ Drug abuse/dependence
■ Physical drug dependency - body becomes accustomed to the drug and cannot function without the presence of
the drug
■ Psychological dependency - drug is the center of the person’s thoughts
○ Therapeutic range or window - drug concentration in the plasma between the minimum effective concentration in the
plasma for obtaining the
● Peak and Trough drug levels
 ○ Requested for drugs with narrow therapeutic index and are considered toxic
○ Time-response curve - evaluates 3 parameters of drug action
■ Onset of action - time it takes to reach minimum effective concentration (MEC) after administration of drug
■ Peak action - occurs when drug reaches its highest blood or plasma concentration
■ Duration of action - length of time the drug has pharmacologic effect
○ Peak drug level - highest plasma concentration of a drug at a specific time; it also indicates the rate of absorption
○ Trough drug level - lowest plasma concentration which measures the rate of elimination
■ Example:
● Vancomycin is a glycopeptide antibiotic. Time dependent killer which means it can become toxic over
time
● Side effect, adverse reactions, and toxic effects
○ All drugs have side effects, desirable or undesirable, even with correct drug dosages
○ They are predictable
○ Side effects occur with drugs which lack specificity
○ Toxic effect or toxicity - harmful effects which can be identified by monitoring the plasma in the therapeutic effect of
the drug
○ Pharmacogenetics - effects of drug action that varies from a predicted drug response because of genetic factor or
hereditary influence
○ Tachyphylaxis - rapid decrease in response to the drug
■ Otherwise known as “acute response”
■ Rapid development of tolerance
■ When some drugs are administered repeatedly at short intervals, tolerance develops rapidly
■ Due to depletion of norepinephrine stores
○ Placebo effect - psychological benefit from a compound that may not have the chemical structure of a drug effect
■ A substance or treatment with no active therapeutic effect
■ Effect is solely due to the patient’s belief of the treatment