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What are some important properties of an ideal drug other than safe, effective, and selective? (7)
reversible action, predictable, easy administration, free of interaction, affordable, chemically stable, simple generic name
What is a chemical name?
precise description of the chemical composition and molecular structure of the drug
What drugs would we be concerned about switching for a generic to a brand name?
low therapeutic indexes (warfarin)
What are the six rights of medication administration?
medication, patient, dose, route, time, documentation
What information should you give the patient about their prescription?
drug name, therapeutic category, dosage size, dosing schedule, route of adminisration, technique of administration, non-pharmacologic measures, expected response, duration of treatment, method of storage, major adverse side effects, drug-drug interaction, drug-food interaction, contact person
What is a randomized controlled trial?
RCTs are the most reliable way to objectively assess drug therapies. Subjects in an RCT are either given a experimental drug or a control (standard or placebo) for comparison.
Why is randomization important?
to prevent allocation bias which results when subjects in the experimental group are different from those in the control group
What is a blinded study?
one in which the people involved do not know to which group - control or experiment - individual subjects have been randomized
What is a double blind study?
the researchers as well as the subjects do not know to which group - control or experiment - subjects have been placed
What is the order of new drug development? (5)
preclinical testing, clinical testing phase I, II, III, and IV
Which phase of new drug development is drug metabolism, pharmacokinetics, and biologic effects assessed?
Which phase(s) of new drug development assess(es) therapeutic effects, dosage range, safety, and effectiveness?
phase II and III
Drug development has historically excluded which groups of people?
women, children, those with co-morbidities
What are the two main components of the pharmaceutical phase of drug activity?
disintegration of dosage form, dissolution of drug
What are the four main components of the the pharmacokinetic phase of drug activity?
absorption, distribution, metabolism, excretion
Arrange the following oral dosage forms from slowest to fastest absorbing. (powders, tablets/capsules, liquids/elixirs/syrups, EC tablets, suspension solutions, coated tablets)
EC tablets, coated tablets, tablets/capsules, powders, suspension solutions, liquids/elixirs/syrups
What is a p-glycoprotein?
transport system that moves drugs form one side of a cell membrane to another
What drugs cannot directly penetrate cell membranes? (3)
polar molecules, ions, those that are too large to pass through channels or pores
What is absorption?
process involving the movement of drug molecules from the site of entry into the body to the circulating fluids
What is Vd?
volume of distribution; relates the amount of drug in the body to the concentration of drug in the blood
What is metabolism?
the process of chemically inactivating a drug by converting it into a more water-soluble compound or metabolite that can be excreted from the body
What is a prodrug?
a compound that is pharmacologically inactive as administered and then undergoes conversion to its active form within the body
Describe the process of Tylenol poisoning.
Tylenol (acetaminophen) is converted into a hepatoxic metabolite following metabolism in the liver; it is this product of metabolism, and not acetaminophen itself, that causes toxicity
Would you except to see increased or decreased metabolism in a malnourished patient? Why?
decreased; not as many CYPs due to insufficient protein intake
The following parenteral routes are ordered from fastest to slowest or from slowest to fastest absorptive rate? SC, IM, IV
slowest to fastest
Why is the pulmonary route of drug administration great for absorption? (2)
large surface area, rich capillary network
What is the hepatic first-pass effect?
a significant amount of drug is metabolized by the liver before reaching systemic circulation
If the dosage of PO morphine was doubled, would its half-life increase, decrease, or stay the same?
stay the same
If a patient has hepatic or renal dysfunction, you should expect the half-life to be longer or shorter?
What is the effective dose (ED)?
dose required to produce therapeutic effect in 50% of a similar population
What is physical dependence?
a stage in which the body has adapted to drug exposure in such a way that an abstinence syndrome will result if the drug use is discontinued
If a drug is supposed to be given "with food," when do you give it in relation to meal time?
with or shortly after meals
If a drug is supposed to be given "on an empty stomach," when do you given it in relation to meal time?
1 hour before or 2 hours after
What are the two major components of the peripheral nervous system? Which is voluntary? Which is involuntary?
somatic (voluntary) and autonomic nervous system (involuntary)
What are the two divisions of the ANS?
parasympathetic nervous system (PNS) and sympathetic nervous system (SNS)
What is innervated by both the PNS and SNS and produces complementary effects?
male reproductive function; PNS erection, SNS ejaculation
What is the result of alpha2 activation?
in the CNS, reduced sympathetic outflow to heart and blood vessels and relief of severe pain
What is the response of alpha1 activation for the following? (eye, arterioles, veins, male sex organs, prostate capsule, bladder)
mydriasis (dilation), constriction, constriction, ejaculation, contraction, contraction (sphincter)
What are three clinically significant actions of alpha1 agonists?
mydriasis (dilation), increased BP, nasal decongestion
What are two clinically significant actions of alpha1 antagonists?
decreased BP, decreased urinary symptoms associated with enlarged prostate
What is the response of beta1 activation for the following? (heart, kidney)
increased HR, increased AV node conduction, increase force of contraction; renin release
What are three clinically significant actions of beta1 agonists?
increase HR, increase cardiac output; increased BP with renin release
Where do beta2 receptors act? (4)
bronchi, uterus, liver, select arterioles (heart, lungs, skeletal muscle)
What is the response of beta2 activation for the following? (bronchi, uterus, liver, select arterioles)
dilation, relaxation (to avoid labor), glycogenolysis, dilation
What are two clinically signficant actions of beta2 agonists?
bronchial dilation; relaxation of uterine smooth muscle
Where do muscarinic receptors act? (6)
eye, heart, lung, bladder, GI tract, male sex organs, sweat glands
What is the response of muscarinic activation for the following? (eyes, heart, lung, bladder, GI tract, male sex organs)
miosis (near vision focus), decreased rate, bronchial constriction, voiding, salivation/increased motility/gastric secretions/defecation, erection
What drug would need to be avoided when using prazosin (Minipress), an alpha1 anatgonist?
PDE5 inhibitors like Viagra
What are the adverse effects of atropine?
blurred vision, photophobia, urinary retention, xerostomia (dry mouth), constipation, elevation of intraocular pressure, anhidrosis (absence of sweat), tachycardia, asthma (plugging secretions)
What do laxatives do?
soften stool, increase stool volume, hasten fecal passage through the intestine, facilitate evacuation from the rectum
What are the actions of bulk-forming laxatives? What group are they? What is their response time?
swell in water to soften and increase the bulk of fecal mass; group III; 1-3 days
What are the actions of surfactant laxatives? What group are they? What is their response time?
lower surface tension to facilitate the movement of water into the stool; group III; 1-3 days
What are the actions of stimulant laxatives? What group are they? What is their response time?
stimulate intestinal motility and increase water and electrolytes within the intestine; group II; 6-12 hours
Name two examples of stimulant laxatives.
bisacodyl (Correctol, Dulcolax, Feen-a-mint), senna (Ex-Lax, Senokot)
What are the actions of osmotic laxatives? What group are they? What is their response time?
osmotic action draws water into the intestine to the poorly absorbed compounds; group I; 2-6 hours
Name three examples of osmotic laxatives.
milk of magnesia, polyethylene glycol (Miralax), sodium phosphate (Fleet Phospho-Soda)
Where are H2 receptors located? What is their function?
parietal cells; activation promotes gastric acid secretion
What is the function of H2 blockers?
suppress acid secretion by blocking the receptors that promote acid secretion
What are the uses for cimetidine (Tagamet)?
PUD, GERD, Zollinger-Ellison syndrome, aspiration pneumonitis, heartburn
What two drugs are preferred over cimetidine (Tagamet)? Why? (3)
ranitidine (Zantac), famotidine (Pepcid); more potent, fewer side effects, fewer interactions
What characteristic of cimetidine (Tagamet) causes other drug levels to rise? What drugs agents should not be used with cimetidine? (4)
inhibits metabolic enzymes; warfarin, phenytoin, theophylline, lidocaine
What is the action of a proton pump inhibitor?
suppresses gastric acid secretion by inhibiting the enzyme, H+, K+-ATPase, which makes gastric acid
What PPI is a prodrug? Where is it converted to an active form?
omeprazole (Prilosec); parietal cells
What is rebound acid hypersecretion?
when symptoms of PUD, GERD, Zollinger-Ellison, etc. get worse when a PPI is stopped
Name four antacids.
aluminum hydroxide, magnesium hydroxide (Milk of Magnesia), calcium carbonate (TUMS), sodium bicarbonate (Baking Soda)
Which antacid(s) should be used cautiously with renal impairment?
magnesium hydroxide (Milk of Magnesia)
What two characteristics of antacids make them prone to drug interactions?
raise gastric pH thereby influencing the dissolution and absorption of many other drugs; akalinizes urine thereby accelerating excretion of acidic drugs and delaying excretion of basic drugs
What should you do to minimize the interaction of antacids and other drugs?
administer drugs at least 1 hour apart
What is the mechanism of action for ondansetron (Zofran)?
blocks 5-HT3 in the CTZ and on afferent vagal neurons in upper GI
What are the uses of ondansetron (Zofran)?
chemo-induced and post-operative nausea and vomiting; acute emesis
What is the mechanisms of action for promethazine (Phenergan)?
blocks dopamine in CTZ; also blocks ACh, histamine 1, NE
What are the adverse side effects of promethazine (Phenergan)?
sedation, hypotension, anticholinergic, extrapyramidal (EPS)
Increased drug sensitivity in infants is due to what five immature pharmacokinetic processes?
absorption (prolonged gastric emptying), protein binding of drugs (albumin levels low), blood-brain barrier (not fully developed), hepatic metabolism (not fully developed), renal drug excretion (not fully developed)
Describe the variable course of drug metabolism with relation to age.
Drugs metabolism is markedly faster than adults until 2 years of age, then gradual declines until puberty
How is dosing of a drug determined in the pediatric patient?
most commonly based on body surface area; initial dosing is, at best, an approximation; subsequent doses need to be adjusted
Why are geriatric patients more sensitive to drugs than younger adults?
system degeneration; altered pharmacokinetics; multiple pathologies
How does absorption of drugs change with age?
delayed gastric emptying and reduce splanchnic blood flow slows absorption
How does distribution of drugs change with age? (3)
increased body fat allows for storage of lipid-soluble drugs; decreased total body water concentrates drugs and causes a more intense effect; reduced serum albumin causes increase in levels of free drugs
How does metabolism of drugs change with age?
hepatic metabolism declines thereby prolonging some drug effects
How does excretion of drugs change with age?
renal function undergoes progressive decline beginning in early adulthood (reduced blood flow, GFR, active tubular secretion, number of nephrons)
What is the most common cause of adverse drug reactions in the elderly?
drug accumulation secondary to reduced renal excretion
What CV drug class is less effective in the elderly? Why?
beta blockers; reduced number of beta receptors; reduced receptor affinity
Nonspecific symptoms in the elderly, such as dizziness and cognitive impairment, can be indicative of what?
adverse drug reactions
What percent of nonadherence cases are intentional? Why?
75%; expense, side effects, patient's conviction that the drug is unnecessary or the dosage is too high
What response is expected when Mu opioid receptors are activated? (5)
analgesia, respiratory depression, euphoria, sedation, physical dependence
Describe agonist-antagonist opioids.
when given alone produce analgesia (opioid naive patient); antagonist effect when already taking an opioid
Name the six strong opioid agonists.
morphine, fentanyl, meperidine, hydromorphone, methadone, heroin
What is the action of morphine sulfate?
mimics actions of various types of "endorphins" (endogenous morphine)
What are the adverse effects of morphine sulfate? (16)
respiratory depression, sedation, orthostatic hypotension, urinary retention, cough suppression, biliary colic, constipation, nausea, vomiting, increased ICP, euphoria, dysphoria, miosis, neurotoxicity, itching, flushing
What two topics would you be sure to educate your patient about regarding the pharmacokinetics of morphine sulface?
avoid abrupt discontinuation (tapering required); first pass effect is large with oral route (explains difference between large oral dose and relatively small IV dose)
Precautions for opioid use should be taken with patients with what conditions? (7)
hypersensitivity, head injury, acute asthma, decreased respiratory reserve (sleep apnea), biliary tract disease, BPH, chronic opioid users
What six categories of drugs interact with opioids?
CNS depressants, anti-cholinergic, anti-hypertension, MAO-I, agonist antagonist opioid, opioid antagonist
Can you give naloxone (Narcan) to a patient that isn't on an opioid if you suspect opioid toxicity?
You observe your patient on a opioid with pinpoint pupils of <2mm. What should you suspect?
morphine sulfate toxicity (overdose)
What can be used to treat constipation that may result with opioid usage?
stool softeners, stimulant laxatives
What can be used to treat sedation that may result with opioid usage?
stimulants such as caffeine and amphetamines
What can be used to treat the nausea and vomiting that may result with opioid usage?
promethazine (Phenergen) or ondansetron (Zofran)
Does the sedation side effect of opioid usage get better? Does the constipation side effect?
yes (2-3 days); no
What is Actiq? What question should we ask a patient who is using Actiq?
fentanyl lozenges on a stick; are their children in the home?
Why is meperidine (Demerol) use declining? (3)
frequent dosing, interactions, neurotoxic metabolite (confusion, seizure)
What is the major adverse side effect of methadone?
prolonged QT that may lead to fatal dysrhythmias
What is the difference between the OxyContin and Percocet preparation of oxycodone?
OxyContin is long acting, Percocet is short aciting
What is drug abuse?
use that is inconsistent with medical or social norms (may vary in different cultures)
What is addiction?
behavior pattern characterized by continued use of a psychoactive drug despite harm to family, friends, career, etc.
In what specific settings are opioids commonly used? (6)
postoperative pain, obstetric analgesia, myocardial infarction, head injury (caution), cancer-related pain, chronic noncancer pain
What is the action of NSAIDs?
blockade of the production of prostaglandins by inhibiting cyclooxygenase (COX) at the site of injury in the periphery, thus decreasing the formation of mediators of pain in the peripheral nervous system
What are the three major uses of cyclooxygenase inhibitors?
suppress inflammation, relieve pain, reduce fever
What are the three major adverse effects of cyclooxygenase inhibitors?
gastric ulceration, bleeding, renal impairment
Ketoralac (Toradol) is given as an injection and is restricted to 5 days or less because of this risk.
Which NSAID(s) cause renal impairment?
first-generation (aspirin, others), second-generation (coxibs)
What are the five major therapeutic uses of aspirin?
analgesic, antipyretic, anti-inflammatory, suppression of platelet aggregation (protects against MI and stroke), dysmenorrhea
Is inhibition of COX-1 and COX-2 reversible or irreversible with first-generation NSAID use?
Compared to aspirin, first-generation NSAIDs have fewer _____? (3)
GI, renal, and hemorrhagic effects
Name three first-generation NSAIDs.
ibuprofen (Advil, Motrin), naproxen (Aleve), ketoralac (Toradol)
Why do most inadvertent overdoses of acetaminophen (Tylenol) occur?
OTC preparations contain APAP, prescription opioid combinations contain APAP
What drug is used to treat an overdose of acetaminophen (Tylenol)?
acetylcysteine (Mucomyst) PO or IV
What are the two most common drugs that interact with acetaminophen (Tylenol)?
alcohol (increases risk of liver damage), warfarin (increases risk of bleeding by inhibiting the metabolism of warfarin)
How do antibiotics promote resistance?
the weakest microorganisms are killed and the stronger ones survive, reproduce and cause greater harm
What is a suprainfection or superinfection?
a new infection that appears during the course of treatment for a primary infection
What organisms are known to have drug resistance?
enterococcus faecalis, enterococcus faecium, staphylococcus aureus, staphylococcus epidermidis, streptococcus pneumonia, klebsiella pneumonia, HIV, TB, MRSA (HA and CA), VRE
What are the common side effects of antimicrobials? (7)
diarrhea, allergic reactions, phlebitis with IV, pain with IM; renal, liver, and bone marrow toxicity
Why are women who use OCP advised to use "back up" methods for up to 2 weeks after discontinuing antimicrobial therapies?
antimicrobials can inactivate OCPs
What is the action of penicillin+beta-lactamase inhibitors?
inhibit bacterial beta-lactamases to extend the antimicrobial activity of the penicillin
How should the nurse administer oral penicillin?
oral doses should be taken with a full glass of water 1 hour before or 2 hours after meals
What should the nurse avoid when administering IV penicillin?
mixing aminoglycosides (gentamicin) in the same IV; running two different antibiotics at the same time
Cephalosporins have four generations with increasing activity against microorganisms. Which is the preferred generation for therapy?
What four adverse effects are expected with cephalosporin use?
allergic reaction, thrombophlebitis with IV, pain with IM, bleeding
Yellow discoloration of teeth is an adverse side effect in children <8 years old seen with this drug.
What are the six major adverse effects of tetracyclines?
GI (burning, nausea, vomiting, diarrhea, cramps), yellow discoloration of teeth, photosensitivity, clostridium dfficile or candida infection, hepatotoxicity (high IV doses), renal toxicity
How should the nurse administer tetracyclines?
1 hour before or 2 hours after a meal; not with calcium, iron, magnesium, aluminum, or zinc
A patient with an atypical respiratory pneumonia or anaerobic agent will be treated with which class of antibiotics?
What adverse effects are expected with vancomycin? (5)
ototoxicity (tinnitus, decreased hearing), red man syndrome (flushed color - not true allergy), thrombophlebitis, thrombocytopenia, allergy
What are the two major adverse effects of aminoglycosides?
ototoxicity (cochlear and vestibular), nephrotoxicity
Which class of drug requires peak and tough levels to be drawn 30 minutes and 1 hour, respectively, after dosage?
Which class of antibiotics can result in tendon rupture, especially in the Achilles tendon?
What are two adverse effects of fluoroquinolones?
Candida infections (pharynx and vagina), phototoxcity
What reduces the absorption of fluoroquinolones?
aluminum, magnesium, iron, zinc, milk and diary products
What are five major adverse effects of glucocorticoids?
oralpharyngeal candidiasis, dysphonia, adrenal suppression, bone loss, slowed growth in children
What are the two actions of beta2-adrenergic agonists?
promote bronchodilation, suppress histamine release
Name two common glucocorticoid/LABA combinations.
fluticasone/salmeterol (Advair), budesonide/formoterol (Symbicort)
What occurs when histamine 1 receptors are activated?
vasodilation, increased capillary permeability, bronchoconstriction, itching, pain, secretion of mucus
If a patient presents with bronchoconstriction, hypotension, and edema of the glottis, should an antihistamine be used for drug therapy?
What is the main difference between the 1st generation and 2nd generation antihistamines?
the 1st generation is highly sedating and the 2nd generation is not
Name three common 2nd generation antihistamines.
fexofenadine (Allegra), cetririzine (Zyrtec), loratadine (Claritin)
What are the adverse effects of a therapeutic dose of antihistamine?
CNS depression (negligible in second-generation), anticholinergic
Should the nurse administer an antihistamine to a patient with a cold?
no (may provide minimal relief with anticholinergic property)
A patient with thin skin, alopecia, muscle wasting, and fragile bones may be on what drug regimen?
Iatrogenic hyperglycemia or glucose intolerance may be caused by which drug therapy?
What are some examples of intermediate acting GCs?
prednisone, prednisolone, methylprednisolone, triamicinolone
What is insulin?
a hormone secreted by the beta cells in the pancreas that works like a key to unlock cells so that blood glucose can enter and be used as fuel
Which drug classes sensitize the body to insulin and/or control hepatic glucose production?
thiazolidinediones (TZDs), biguanides
Can you give sulfonylureas (SFUs) to a type II diabetic? What about a type I? Why or why not?
yes, no (must have ability to secrete insulin)
Name three second generation sulfonylureas (SFUs).
glyburide (Micronase, Glynase, and DiaBeta), glimepiride (Amaryl), glipizide (Glucotrol, Glucotrol XL)
Who is at risk for lactic acidosis? (4)
patients with impaired liver function, severe infection, excessive alcohol use, heart failure
What should the nurse explain to a patient complaining that he wants to stop taking his metformin because if gives him diarrhea?
diarrhea tends to resolve over and week; improves if taken with food
Your patient has just come back from a CT scan procedure using IV contrast. Which postoperative drug should you hold?
Which oral diabetic agent does not have hypoglycemia or weight gain side effects?
Most diabetic patients will require multiple medications to achieve control. Which oral agents can be used in combination?
sulfonylureas (SFUs), thiazolidinediones (TZDs), biguanides
Name the three most common rapid acting insulins.
lispro (Humalog), aspart (Novolog), glulisine (Apidra)
What is a bolus of insulin?
rapid and short-acting insulin that targets post-prandial glucose levels and bring elevated glucose down
What is basal insulin?
intermediate and long-acting insulin that targets between meals and fasting glucose levels
What should you do before administering intermediate insulin?
roll vial in hands to mix the suspension prior to injection
What is premixed insulin?
preparations containing basal and bolus insulin (Novolin 70/30, Humulin 70/30, Novolog 70/30, Humalog 75/25)
What is the order to draw up rapid or short acting insulin with NPH?
insert air into cloudy then clear, draw up clear then cloudy; "cloudy, clear, clear, cloudy"
How should the nurse prepare for IV insulin administration?
prepare the bag and tubing 30 minutes prior to administration to allow binding to plastic
What is IV insulin used to treat?
diabetic ketoacidosis (DKA), hyperosmolar hyperglycemic state (HHS)
What are the adverse side effects of clonidine (Catapress)? (4)
sedation, dry mouth, rebound HTN if abrupt withdrawal, fetal harm
What is the action of calcium channel blockers (CCBs)?
prevent calcium ions from entering cells; inhibits the contractile process of peripheral arterioles/arteries and cardiac arterioles
What do nondihydrophyridines, such as verampil (Calan) and diltiazem (Cardizem), act on?
vascular smooth muscle (VSM), heart
What are the three most common adverse effects of verapamil (Calan) and diltiazem (Cardizem)?
constipation, lower extremity edema, gingival hyperplasia
What should the nurse teach a patient who is taking nondihydropyridines?
diet for constipation side effect
What are the three most common adverse side effects of dihydropyridines?
reflex tachycarida, lower extremity edema, gingival hyperplasia
What is the mechanism of action for beta antagonists?
prevent the binding of endogenous catecholamines (EPI and NE) to beta adrenergic receptors
What are the five conditions that beta blockers are commonly used to treat?
HTN, angina pectoris, dysrhythmias (tachycardias), MI (post-MI), heart failure
What is the mechanism of action for ACE-inhibitors?
decreases levels of angiotensin II and increase bradykinin by blocking ACE; vasodilation, reduced blood volume
What are the five most common adverse effects of ACE-inhibitors?
cough, angioedema, 1st dose hypotensions, hyperkalemia, fetal injury
What is the mechanisms of action for angiotensin receptor blockers?
block receptors for angiotensin II on blood vessels, the adrenals, arterioles, and veins
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