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Pharmocology Chap.1-3
N/A
107
Nursing
Undergraduate 3
09/21/2010

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Term
Generic name
Definition
the original designation that the drug was given when the drug company applied for the approval process.
Term
Brand name (trade name)
Definition
given to an approved drug by the pharmaceutical company that developed it.
Term
Chemical names
Definition
name that reflect the chemical structure of a drug.
Term
Preclinical trials
Definition
chemicals id-ed that might have therapeutic activity tested on animals
-Fail = inactive, too toxic, teratogenic, narrow safety margins
Term
Phase I
Definition
Human volunteers that are young, healthy, males
-Fail = inactive, too toxic, teratogenic, too many adverse effects
Term
Phase II
Definition
human volunteers who have target disease or conditions
-Fail = less effective, too toxic, too many adverse effects, low benefit to risk ratio
Term
Phase III
Definition
use clinically with prescribers. Info collected by drug company and shared w/FDA
→ Begin Phase IV which is continual monitoring by prescribers with reporting to FDA.
Term
Category A
Definition
adequate studies in pregnant women with no demonstrated risk to fetus (best)
→ Ferrous sulfate (iron)
Term
Category B
Definition
Animal studies have not demonstrated risk to fetus, but no studies in pregnancy or animal studies adverse, but studies in pregnant woman okay
→ Claritin (Loratidin), Amoxicillin
Term
Category C
Definition
Animal studies have shown an adverse effect on fetus but no adequate human studies
→ Albuterol (Proventil)
Term
Category D
Definition
Evidence of human fetal risk of benefits to pregnant women may be acceptable
→ phenytoin (Dilantin)
Term
Category X
Definition
all risk no benefit (never use during pregnancy/ breastfeeding)
→ Accutane (Isoretinoin), Zocor
Term
Controlled Substances Act of 1970
Definition
classified drugs by abuse potential with shared control over coding and enforcement to the DEA; how likely they are to be abused & cause dependability
Term
Schedule I
Definition
High abuse potential and no acceptable medical use
→ Heroin
Term
Schedule II
Definition
High abuse potential w/ severe dependence liability
→ morphine, meperidine, oxycotin
Term
Schedule III
Definition
less abuse potential than schedule II w/ moderate dependence liability
→ Tylenol-3 (codeine 30 mg)
Term
Schedule IV
Definition
Less abuse potential than Sched. II with limited dependence liability
→ Xanax (alprazoiam)
Term
Schedule V
Definition
Limited abuse potential and dependence liability
→ cough medicines with codeine (dextromethorphan hydrobromide
Term
Reliable sources
Definition
PDR (Physician's Desk Reference)
- Package inserts
- Medical Letter
- Journal Reviews
- Drug Facts and Comparisons
- Pharmacist
- Internet sources
Term
Generic Drugs
Definition
chemicals that are produced by companies involved solely in the manufacturing of drugs (legend drugs) these drugs do not have the research the advertising, or quality control depts. the that pharmaceutical companies have so they cost much less than the brand names. (Example: the binders used in a generic drug might be different so it might break down differently in the body)
Term
Orphan Drug
Definition
drugs that have been discovered but are not financially viable and therefore have not been “adopted” by any drug company; may be useful in treating a rare disease or may have potentially dangerous adverse effects; often abandoned after preclinical trials or phase I studies. The Orphan Drug Act of 1983: provided tremendous financial incentives to drug companies to adopt these drugs and develop them. This puts the drugs through the rest of the process despite the small market for the drug.
Term
Over the Counter Drugs
Definition
products that are available w/o prescription for self-treatment of a variety of complaints. Some of these agents were approved for prescription use but later found to be very safe and useful for patients without the need of a Rx. Some were not screened and tested by the current drug protocols b/c they were developed and marketed before the current laws were put into effect.**Problems with OTC use: could mask signs and symptoms of underlying disease, making diagnosis difficult, taking these drugs w/ Rx could result in drug interactions, not taking them as directed could result in overdoses.
Term
Pharmacodynamics
Definition
study of the processes by which a drug alters the physiology of the cell; how the drug exerts its actions
Term
Drugs act by...(4)
Definition
1. replacing or acting as subs for missing chems (Prozac replaces missing serotonin)
2. increasing or stimulating certain cellular activities (digestion/circulation)
3. depressing or slowing cellular activities (acid production)
4. interfering with the function of foreign cells (chemotherapeutic; sinus antibiotics)
→ This effect is achieved by the opening or closing of ion channels, activating biochemical messengers, inhibiting cellular processes, turning on a cellular function.
Term
Receptor Theory of Drug Action: Agonist Interaction
Definition
Agonist interaction with receptor site on cell. *Drug A reacts with specific receptor sites on cells activity.
Term
Receptor Theory of Drug interactions: Competitive Antagonism
Definition
Drug A and Drug C have an affinity for the same receptor sites and compete for the sites; drug C has a great affinity, so it occupies more of the sites and antagonizes drug A.
Term
Receptor Theory of Drug Interaction: Noncompetitive antagonism
Definition
Drug D reacts with a receptor site that is different from the receptor site for drug A but still somehow prevents drug A from binding with its receptor sites. Drugs that act by inhibiting enzymes can be picturing as acting similarily to the receptor site antagonists in B and C. Enzyme inhibitors block the binding of molecules of normal substrate to active sites on the enzyme.
Term
Pharmacokinetics
Definition
the way the body processes drugs and includes absorption, distribution, metabolism (biotransformation), and excretion. Level of drug in the body based on the functioning of these four activities.
Term
Critical Concentration
Definition
level in bloodstream that drug needs to reach to be effective (cause a therapeutic effect) ; therapeutic range
Term
Loading Dose
Definition
“a big kick”- trying to increase activity (in beginning) if effects are needed immediately (emergency) then this is recommended.
Term
Dynamic equilibrium
Definition
simultaneous absorption, distribution, metabolism, excretion
Term
Absorption
Definition
drug moves from site of administration into venous or lymphatic circulation. Affected by dosage from and route of administration and patient charac. Drug transported by vascular system to site of activity. Can stay bloodstream and be reversibly bound to protein or circulate unbound.
Term
Bioavailability
Definition
escribes how much of what is administered makes it into circulation to produce effects. **Oxycotin: long release, if crushed, absorption is changed.
Term
Absorption processes
Definition
passive diffusion (most important), active transport (carriers that
form complex w/drug and carry through membrane and then dissociate), filtration (through pores- very small)
Term
route of admin: oral
Definition
cheapest, less invasive, safest but affected by GI contents (acidity) and emptying time
Term
Off label use
Definition
Drug is used for purposes different than those FDA approved; Example: Prozac was used for depression; later found that it helped with anxiety and OCD. Physicians now use it this way but it has been added to the label.
Term
Pharmacodynamics
Definition
study of the processes by which a drug alters the physiology of the cell. How the drug exerts its actions.
Term
Drug Effect
Definition
relationship btw the concentration of the drug & response of the patient
Term
Potency
Definition
measure of concentration of drug
Term
Efficacy
Definition
maximum response a drug can produce
Term
Receptor Theory
Definition
Receptors are most likely proteins or nucleic acids on cell wall or in cytoplasm that regulate normal cell function. drugs interact with receptors (binding) to produce a response- can bind or bind to BLOCK
Term
Agonist
Definition
binds at the receptor the SAME way the natural chemical would, enhances activity ; Albuterol (opens airways)
Term
Antagonist
Definition
binds at the receptor to BLOCK natural chemicals; decreases activity; Benadryll
Term
Therapeutic Range
Definition
range of plasma levels between the minimal effective concentration and the minimal toxic concentrations
Term
Steady State Concentration
Definition
maintaining the drug level in therapeutic range; example: thyroid problem --> take Sinroid, no problems
Term
Selective Toxicity
Definition
characteristic of a drug to attack only those systems found in foreign cells. often cells that rapidly reproduce (hair, skin, mucous membranes) Example: chemotherapy and antibiotics
Term
Route of Admin: SL
Definition
Sublingual (under tongue) 2nd fastest after IV; Example: NTG (Nitrogylcerin for chest pain) goes directly into bloodstream
Term
Route of Admin: SL
Definition
Sublingual (under tongue) 2nd fastest after IV; Example: NTG (Nitrogylcerin for chest pain) goes directly into bloodstream
Term
Route of Admin: IM and SQ
Definition
Intramuscular and Subcutaneous: more directly absorbed into circulation, but dependent on circulation and site where given, more painful and expensive
Term
Route of Admin: Pulmonary
Definition
large surface area of lung, rich capillary bed, conveyed as fine mist inhaled (or rectally,, vaginally, or patches)
Term
First pass effect
Definition
Oral; from gastric absorption, po meeds go to portal venous system into liver where transformed by enzymes, so increased doses needed as compared to parental where some of dose reaches reactive tissue before going to liver; goes into portal circulation, altering dosage before reaching destination.
Term
Factors affecting absorption
Definition
1-nature of absorbing surface
2- blood flow to site
3- solubility of drug
4- Ph and effect of ionization (more highly ionized less absorbable)
5- drug concentration
6-dosage form
Term
Distribution
Definition
drug movement from bloodstream to the site of action and to storage sites; move first into organs with rich blood supply (heart, kidney, liver, brain) then into muscle and fat
Term
Factors affecting distribution
Definition
tissue perfusion, lipid solubility, protein binding
Term
Protein binding
Definition
most drugs protein bound in blood to be carried in circ. can't diffuse into capillaries due to size. drugs are variably bonded and can be released slowly or quickly which affects onset of action. protein bound drugs are inactive. dissociate-free drug is active. another drug can cause loss of protein binding or low protein levels may result in more toxicity.
Term
It is more difficult for drugs to be distributed into...
Definition
CNS, intrathecal
Term
Drugs can be distributed more easily into...
Definition
placenta to fetus or in breast milk.
Term
Cytochrome P450 enzyme system
Definition
In liver; People without this enzyme cannot metabolize anesthesia, their temp goes up to about 104-108; If 2 drugs are taken, one can effect this system and allow the other drug to become toxic.
Term
Metabolism (biotransformation)
Definition
conversion of compounds to less toxic or nontoxic substances and prepare for excretion (transforming the blood) besides metab. drugs and preparing them for excretion, may actually convert an active prodrug to an active compound
Term
Metabolism: Phase I
Definition
oxidation, reduction, , or hydrolysis of drug in cytochrome P450 system (most abundant in liver) alters drug to more polar and water soluble form to aid excretion
Term
Metabolism: Phase II
Definition
conjugation of compound to inactivate and then eliminate. (union of polar group of drug with another substance in body)
Term
Enzyme induction
Definition
occurs when one compound increases the activity of the enzyme system. this increased enzyme act. hastens the breakdown of other drugs that use the same pathway (genetics also factor since certain subsets of C-P450 system may be missing in some populations
Term
Where does metabolism occur?
Definition
Liver, skin, mucous (saliva), lungs, bile and feces
Term
What factor can effect both metabolism and excretion?
Definition
abnormalities in renal, hepatic systems or CHF affects both
Term
Excretion
Definition
removal of drug or its metabolites from the body
Term
What are the 4 modes of excretion?
Definition
1.Occurs through skin, saliva, lungs, bile (from liver to bile to duodenum to feces), feces
2. Kidneys play the major role with passive glomerular filtration and active tubular secretion or partial reabsorption
3. acidity of urine may have a effect
4. half-life: time it takes for the drug in serum to go from peak concentration to half its concentration (only inside body)
Term
Tolerance
Definition
decreased response to drug- may be due to more rapid metabolism, fewer receptors
Term
Dependence
Definition
needs drug to have normal function (can be physical or psychological)
Term
Withdrawal
Definition
symptoms resulting from decrease in drug in dependent individual
Term
Cross dependence
Definition
tolerance to different drug due to chemical similarities
Term
What are the 4 half-life factors?
Definition
Immunological, psychological, environmental, tolerance
Term
Half life factors: Immunological
Definition
allergic reactions
Term
Half life factors: psychological factors
Definition
how you present the medicine is emphasized or patients might know other patients who have taken the meeds and had certain symptoms
Term
Half Life factors: environmental factors
Definition
nitroglycerin deactivates by light/heat
Term
Tolerance
Definition
more you take, higher chance of med-interactions, higher doses to be effective. cumulation (more to be taken)
Term
What are the 8 factors influencing drug effects?
Definition
Weight, age, gender, physiological factors (diurnal rhythm, electrolyte balance, pH balance, hydration), pathological factors (disease, hepatic illness), immunological, psychological, environmental, drug tolerance, cumulation effects, interactions
Term
Adverse effects
Definition
undesired, unintended, and at times unpredictable; other affects of the drug besides the therapeutic; patient may be taking too little or too much; patient may be more sensitive to the effects
Term
Primary action
Definition
extension of the desired effect (overdosage) which can be due to individ. differences in response, increase or decreased body weight, pathology
Term
Secondary Action
Definition
effects that occur in addition to primary action; example: bendryll has add'l side effects
Term
Hypersensitivity
Definition
excessively responsive to the drug
Term
Allergy
Definition
occurs after 1st exposure; development of antibodies; re-exposure will result in immune response; when patient says they're allergic, ask for details
Term
What are the 4 types of allergic reactions?
Definition
Anaphylaxis, cytotoxic, serum sickness, delayed hypersensitivity
Term
Anaphylaxis
Definition
antibody response w/immune reactivity and release of histamine w/resulting signs and symptoms; most dangerous
Term
Cytotoxic
Definition
circulating antibodies attach the drug on cell sites and cause cell death. See drop in HCT , WBC and elevated LFT, elevated BUN/Creat. tends to be delayed and seen over a few days
Term
Serum Sickness
Definition
immune complexes deposit in blood vessels. cause rash, fever, lymphadenopathy, swollen joints, impaired renal function, spleenomegaly (enlarged), occurs 1-3 wks after exposure
Term
Delayed hypersensitivity
Definition
with reaction of sensitized T lymphocytes and macrophages; Example: Steven-Johnson's syndrome- burns w/tissue sloughing, can be fatal.
Term
What are some common high risk drugs? (PINCH)
Definition
Potassium: will cause cardiac standstill, Insulin: narrow therapeutic index, Narcotics: esp.IV, respiratory depression, Chemotherapy: any cancer med, Heparin/related
Term
The risk of drug therapy on a fetus depends on what 3 factors?
Definition
drug type, concentration, fetal age
Term
5 pregnancy categories are based on what ratio?
Definition
risk to benefit ratio
Term
What are the physiological changes in pregnancy that impact pharmacokinetics?
Definition
Delayed gastric emptying and decreased motility, increased pulmonary ventilation and increased blood flow and surface area, increase GFR (globular filtration rate) and renal blood flow, decreased hepatic enzyme activity, change in body mass and fluid distribution
Term
What does drug transfer across placenta depend on?
Definition
lipid solubility, protein binding, and other drug propeties
Term
Compare fetal serum levels to maternal serum levels
Definition
majority of drugs pass by simple diffusion with fetal serum levels equal to maternal levels but may be higher
Term
When are the critical periods for drug effects on fetus?
Definition
1st 2 weeks of rapid cell proliferation and weeks 3-12 during organogenesis
Term
Why are neonates (birth-1 month) a separate category than pediatrics?
Definition
This is due to thin permeable skin, lack of stomach acid, poor temperature regulation, propensity for dehydration, immature liver and kidneys and lungs
Term
How do breastfed infants receive drugs?
Definition
almost all forms of drugs are received that are in maternal circulation although usually at lower doses b.c of maternal biotransformation; water soluble drugs may be admin. in larger doses to infants
Term
Describe how breast-fed infants receive high lipid soluble drugs
Definition
these drugs will be more concentrated in breast milk, low serum protein results in more free drug, slower metabolic reactions by liver, delayed drug excretion due to immature kidneys
Term
By what age are most pharmacokinetic patterns similar to those in adults and except for which system?
Definition
by age 1 and except hepatic; Liver enzymes are increased due to larger liver size in proportion to body wt. drugs eliminated by hepatic mechanisms need more freq. dosing or change in dosage. liver function advances rapidly with ability to excrete medication mature @ about 1 yr.
Term
Describe the renal system in relation to drug therapy during late childhood.
Definition
renal system may excrete more rapidly than adults. due to increased percentages of body water and less fat.
Term
How does thick skin and large surface area in proportion to weight affect drug therapy?
Definition
This will enhance action of topical medications.
Term
What are examples drug induced or organ specific damage?
Definition
dermatologic, stomatitis (inflammation of epithelial cells, lining), superinfections, blood dyscrasias (blood disease), toxicity w/liver or renal, poisoning, altered glucose metab., electrolyte imbalance, sensory (ocular and auditory), neuro. (cns, atropine like, parkinson-like, neuroleptic malignant syndrome), teratogenicity
Term
Why is drug research in children limited?
Definition
Due to use of protected population, costs of randomized controlled trials and their dominance in evaluation, limited research infrastructure
Term
What is common with the elderly and their med use?
Definition
usually taking many drugs at once, polypharmacy
Term
What can effect pharmacokinetics in the elderly?
Definition
mult chronic conditions including deficits in hepatic and renal systems that affect pharamcokinetics
Term
What would necessitate use of children's dosage in the elderly?
Definition
lower body weights
Term
Describe factors that effect drug therapy in the elderly
Definition
reduced gastric acidity and motility alters absorption, incr body fat w/resulting incr. in fat storage of meds, less total body water so more risk of toxicity in water soluble drugs, decreased serum albumin results in less protein binding and more free drug, alteration in blood flow due to CHF impacts functioning of liver and kidneys as well as transport of drug from site
Term
Overall changes in elderly may result in...(drug therapy)
Definition
higher blood and tissue levels of drug with increased adverse effects and likelihood of toxicity
Term
Altered number or sensitivity of receptors may occur with what age group pertaining to drug therapy?
Definition
the elderly
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