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PHARMACOLOGY
- Greek: pharmakon + logos
- Study of drugs and their actions
- Study of biologic effect of chemicals
DRUGS
- Dutch: droog meaning dry
- Chemical substances that have an effect on living organisms
- Therapeutic drugs
PHARMACOTHERAPEUTICS
- Clinical pharmacology
- Branch of pharmacology involving drugs used to treat, prevent or diagnose disease
MEDICINES
- Therapeutic drugs
- Sources
o Plants
o Animal products
o Inorganic compounds
o Synthetic sources
1. PREVENTION
- First level
- Health impact of environment
- Health aspects of social, medicinal and illegal drug abuse
PHARMACOLOGY IN RESEARCH
- Drug research
- Considerations in drug research
o Nurse
Fully informed
o Information available to physician
o Research and pharmacist
o Recommended dosage
o Route of administration
o Desired therapeutic effects
o Adhere to the study protocol
ETHICAL PRINCIPLES
- Respect for person
o Individuals are independent meaning they are capable of making decisions
- BENEFICENCE – duty to do no harm
- JUSTICE – social benefits can be allocated objectively and that those with equivalent circumstances should be
treated equally
1. FLOOR STOCK
- All medications are stocked at nursing station
- Except dangerous drugs
- Utilized in small hospitals, government hospitals
DRUG ORDERS
STAT
- emergency doses
- Meds given ASAP but ONCE only
SINGLE ORDER
- Administration at a certain time only but once
STANDING ORDER
- Meds given for a specific number of doses
PRN (pro re nata)
- For the thing born
- As needed
- Allows nurse to practice judgement to when a medication should be administered
VERBAL ORDERS
- Should be avoided
- Physician should co-sign and date the order in 24 hours
RIGHT
1. Patient
2. Drug
3. Time
4. Dose
5. Route
6. Administration
PATIENT’S CHART
- Primary source of information
ASSESSMENT
- Subjective and objective
- Prescriptions
- OTCs
- Herbals
- Responses to medications
NURSING DIAGNOSIS
- Decision about the needs/problems of patient
- Critical thinking, creativity and accurate data
PLANNING
- Goals and outcome criteria
- Specific and measurable
- Patient-centered
- Time-frame
- Prioritization
IMPLEMENTATION
- Initiation and completion of nursing plans
2. FEDERAL LEGISLATION
- Public protected from drugs that are impure, toxic, ineffective or not tested prior to public use
LEGAL REGULATIONS
LEGAL TERM
1. MISFEASANCE
a. Negligence
b. Nonfeasance
c. Omission
2. MALFEASANCE
a. Giving right drug by wrong route
PHILIPPINE LAWS
ADVANTAGES
- Decreases prices
- Ensures adequate drug supply
- Promote safety
- For scientific basis use of drugs
DISADVANTAGES
- Some have inert fillers and binders that may result in differences in effectiveness
- May have some variation in action or response
- Too long and difficult to pronounce
PHARMACEUTIC PHASE
- Dissolution- drugs in solid form must disintegrate into small particles to dissolve into a liquid
- Excipients – fillers and inert substances; used in drug preparation to take on a particular size and shape and to
enhance drug dissolution
- Disintegration- breakdown of a tables into smaller particles
- Dissolution – dissolving of the smaller particles in the GI fluid before absorption
- Rate limiting- the time it takes the drug to disintegrate and dissolve to become available for the body to absorb it
** drugs are both disintegrated and absorbed faster in acidic fluids with a pH of 1 or 2 rather than alkaline fluids
- Enteric-coated drugs- resist disintegration in the gastric acid of the stomach, so the disintegration does not occur
until the drug reaches the alkaline environment of the small intestine; should not be crashed
PHARMACOKINETIC PHASE
- The process of drug movement to achieve drug action
1. ABSORPTION
- Movement of drug particles from the GI tract to body fluids by passive absorption, active absorption or
pinocytosis
- Most oral drugs are absorbed into the surface area of the small intestine through the action of the
extensive mucosal villi
- Dec. number of villi = dec. absorption
- Protein-based drugs- ( insulin and growth hormones) destroyed in the s.intestine by digestive enzymes
- PASSIVE ABSORPTION- occurs mostly by diffusion
- ACTIVE ABSORPTION- requires a carrier such as an enzyme or protein to move the drug against a
concentration gradient
- PINOCYTOSIS- process by which cells carry drug across their membrane by engulfing the drug particles
** drugs that are fat soluble pass rapidly through the GI membrane
** weak acid drugs such as aspirin are less ionized in the stomach and they pass through the stomach lining
easily and rapidly
***calcium carbonate and many of the antifungals need an acidic environment to achieve greater
absorption
- FIRST-PASS EFFECT or HEPATIC FIRT PASS- process in which the drug passess to the liver first; example:
Coumadin, morphine
- BIOAVAILABILITY- subcategory of absorption; percentage of the administered drug that reaches the systemic
circulation
- FACTORS THAT ALTER BIOAVAILABILITY
o Drug form
o Route of administration
o GI mucosa and motility
o Food and other drugs
o Changes in liver metabolism
2. DISTRIBUTION
- Process by which the drug becomes available to body fluids and body tissues
- Influenced by blood flow, its affinity to the tissue and protein-binding effect
- VOLUME OF DRUG DISTRIBUTION- dependent on drug dose and its concentration in the body
- Larger Vd = longer half-life
- FREE DUGS- portion of drug that is bound is inactive because it is not available to receptors, and the portion
that remains unbound; are active and can cause pharmacologic effect
- Two highly protein bound drugs = drug accumulation and possible drug toxicity
3. METABOLISM OR BIOTRANSFORMATION
-LIVER – primary site of metabolism
*** Most drugs are inactivated by liver enzymes and are then converted or transformed by hepatic
enzymes to inactive metabolites or water-soluble substances for excretion
- HALF LIFE- the time it takes for one half of the drug concentration to be eliminated
- SHORT HALF-LIFE= 4 to 8 hours
- LONG HALF-LIFE= 24 hours or longer
- Administration of the drug for three to five half-lives saturates the biologic system to the extent that the
intake of drugs equals the amount metabolized and excreted
- STEADY-STATE SERUM CONCENTRATION is the predictive of therapeutic effect
4. EXCRETION or ELIMINATION
- Main route of elimination is through the kidneys
- KIDNEYS filter free, unbound drugs; water soluble drugs and drugs hat are unchanged
- LUNGS eliminate volatile drugs substances and products metabolized to CO2 and H2O
- ACID URINE promotes elimination of weak base drugs
- ALKALINE URINE promotes elimination of weak acid drugs
- ASPIRIN a weak acid; excreted rapidly in alkaline urine
- SODIUM BICARBONATE – antidote for aspirin
- CRANBERRY JUICE- can decrease urine pH
- CREATININE CLEARANCE- most accurate test to determine renal function; varies with age and gender; lower
in elderly and female clients
- CREATININE- metabolic byproduct of muscles that is excreted by the kidneys
- CREATININE CLEARANCE TEST – 12 or 24 hour urine collection
- NORMAL CREATININE CLEARANCE- 85 to 135ml/min
- AGING- decreases muscle mass and results in a decrease in functioning nephrons
PHARMACODYNAMIC PHASE
- PHARMACODYNAMICS- the study of drug concentration and its effects on the body
- Primary effect may be desirable; secondary effect may be desirable or undesirable
- DOSE RESPONSE- relationship between the minimal versus the maximal amount of drug dose needed to produce
the desired drug response
- ONSET OF ACTION- time it takes to reach the minimum effective concentration after a drug is administered
- PEAK ACTION- occurs when the drug reaches its highest blood or plasma concentration
- DURATION OF ACTION- the length of time the drug has a pharmacologic effect
- RECEPTORS- protein in structure; found on cell membranes
- LIGAND-BINDING- the site on the receptor in which drugs bind
- FOUR RECEPTOR FAMILIES
o CELL MEMBRANE-EMBEDDED ENZYMES – LIGAND BINDING DOMAIN- on the cell surface; the drug
activates the enzyme and a response is initiated
o LIGAND-GATED ION CHANNELS – the drug spans the cell membrane and with this receptor, the channel
opens, allowing for the flow of ions into and out of the cells. The ions are primarily sodium and calcium.
o G PROTEIN-COUPLE RECEPTOR SYSTEMS
Receptor
G protein than binds with guanosine triphosphate
Effector that is either an enzyme or an ion channel
o TRANSCRIPTION FACTORS – on the DNA in the cell nucleus and not on the surface of the cellmembrane
Drugs act through receptors by binding to the receptor to produce a response or to block a
response
Activity of many drugs is determined by the ability of the drug to bin to a specific receptor
- AGONISTS- drug that produce a response
- ANTAGONISTS- drugs that block a response
- CHOLINERGIC RECEPTORS- located in the bladder, heart, blood vessels, lungs and eyes
- NON SELECTIVE DRUGS- drugs that affect various sites
- FOUR CATEGORIES OF DURG ACTION
o STIMULATION OR DEPRESSION
STIMULATION- the rate of cell activity or secretion from a gland increases
DEPRESSION-cell activity and function of a specific organ are reduced
o REPLACEMENT- replace essential body compounds
o INHIBIT OR KILL- interfere with bacterial cell growth
o IRRITATION
- THERAPEUTIC INDEX- estimates the margin of safety of a drug through the use of a ratio that measure the
effective dose and the lethal dose
o LOW THERAPEUTIC INDEX- have a narrow margin of safety
o HIGH THERAPEUTIC INDEX- wide margin of safety and less danger of a producing toxic effects
- THERAPEUTIC RANGE- between the minimum effective concentration in the plasma for obtaining desired drug
action and the minimum toxic concentration in the plasma for obtaining desired drug action and the minimum
toxic concentration
- PEAK DRUG LEVEL- highest plasma concentration of drug at a specific time
o Orally- 1 to 3 hours
o IV- 10 minutes
- TROUGH LEVEL- lowest plasma concentration of a drug and it measures the rate at which the drug is eliminated
- LOADING DOSE- initial dose
- DIGITALIZATION- the process by which the minimum effective concentration level for digoxin is achieved in the
plasma within a short time
- SIDE EFFECTS- physiologic effects not related to desired drug effects
- ADVERSE REACTIONS- more severe than side effects; a range of untoward effects that cause mild to severe side
effects including anaphylaxis
- TOXIC EFFECTS or TOXICITY- can be identified by monitoring plasma therapeutic range of the drug
- PHARMACOGENICS- effect of a drug action that varies from a predicted drug response because of genetic factors
or hereditary influence
- TACHYPHYLAXIS- drug tolerance to a frequently repeated administration of a certain drug
- PLACEBO EFFECT- psychologic benefit from a compound that may not have the chemical structure of a drug
effect
PHARMACEUTIC PHARMACOKINETICS PHARMACODYNAMICS
ABSORPTION DRUG ACTION
DISTRIBUTION RECEPTORS
SOLID FORM METABOLISM OR
LIQUID FORM BIOTRANSFORATION ENZYMES
EXCRETION HORMONES
UNIT FIVE
ADRENERGICS AND ADRENERGIC BLOCKERS
AUTONOMIC NERVOUS SYSTEM AGENTS
- CENTRAL NERVOUS SYSTEM- body’s primary nervous system that consists of the brain and spinal cord
- PERIPHERAL NERVOUS SYSTEM- located outside the brain and spinal cord
- AUTONOMIC NERVOUS SYTEM- acts on smooth muscles and glands; control and regulation of heart, respiratory
system, gastrointestinal tract, bladder, eyes and glands; an involuntary nervous
- AUTONOMIC COMPONENTS OF THE PNS
o AFFERENT NEURONS- sends impulses to the CNS where they are interpreted
o EFFERENT NEURONS- receive the impulses from the brain and transmit those impulses through the
spinal cord to the effector organ cells
- EFFERENT PATHWAYS
o SYMPATHETIC NERVOUS SYSTEM- also known as the ADRENERGIC NERVOUS SYSTEM
At one time it was believed that adrenaline was the neurotransmitter that innervated the
smooth muscle NOREPINEPHRINE – the actual neurotransmitter
o PARASYMPATHETIC NERVOUS SYSTEM- called the CHOLINERGIC SYSTEM
Neurotransmitter at the end of the neuron that innervates the muscle is ACETYLCHOLINE
Cholinergic receptors are either NICOTINIC or MUSCARINIC
- Drugs that mimic the neurotransmitters norepinephrine and acetylcholine produces response opposite to each
other in the same organ
CNS PNS
SYMPATHETIC PARASYMPATHETI
C
SYMPATHOLYTICS PARASYMPATHOLYTICS
- Adrenergic blockers, adrenolytics or - Anticholinergics, cholinergic
adrenergic antagonists antagonists or anti spasmodic
ANS
NOREPINEPHRINE adrenergic NS
ACETYLCHOLINE cholinergic NS
ADRENERGIC- stimulate the sympathetic nervous system; located throughout the body, alpha and beta receptors
CHAPTER 17
ADRENERGICS AND ADRENERGIC BLOCKERS
ALPHA1 RECEPTOR
INCREASED BP
ALPHA2 RECEPTOR
INC. CONTRACTIBILITY
OF THE HEART
BLOOD VESSELS SMOOTH MUSCLES
GI TRACT
BETA1 RECEPTOR
SMOOTH
DEC.
INC.INC.
HEART
GI TONE
MUSCLE
CONTRACTION
ANDRATE
HEART
HEART BRONCHODILATION
INC.
LUNGS
INC.
ANGIOTENSIN
KIDNEY
INC
RENIN RELAXATION
BP BETA2 RECEPTOR UTERUSOF UTERINE INC.
ACTIVATION
BLOOD
LIVER SUGAR
OF
GI
MOTILITY
TRACT SMOOTH MUSCLE GLYCOGENOLYSIS
INACTIVATION OR NEUROTRANSMITTERS
- Caused by
o Reuptake of the transmitter back into the neuron (nerve terminal)
o Enzymatic transformation or degradation
o Diffusion away from the receptor
- MECHANISM OF NOREPINEPHRINE UPTAKE plays more important role in inactivation of the enzymatic action