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Properties of an Ideal Drug
The Big 3
Effectiveness
Safety (cannot produce harmful effects even if admin in very high doses)
Selectivity (elicits only the response for which it is given)
ideally = localized effect
What is the most important property of a drug?
Effectiveness
What other drugs should you not take if you are taking a potassium-sparing diuretic?
other drugs that raise K
What are normal K+ levels?
3.5-5.0 mEq/L
What foods should you avoid if taking potassium-sparing diuretics?
potassium rich foods
salt substitutes
What drug properties enhance patient adherence?
ease of administration
a simple generic name
How to promote patient adherence to medications?
teach the pt WHY they are taking the drug and the SYMPTOMS of the medication
How does albumin affect drug distribution?
drugs attach to albumin → can’t reach site of action (not effective) → therapeutic failure
What are pharmacokinetic changes regarding drug therapy in older adults?
Absorption: slowed
Distribution: less albumin → DRUG ACCUMULATION
Metabolism: slowed, prolonged effects → DRUG ACCUMULATION
requires less frequent dosing
Excretion: declined → DRUG ACCUMULATION
What test should you use to assess the renal function of older adults? Why?
Creatinine clearance
serum creatinine is influenced by lean muscle mass (variable at older age)
creatinine levels may be normal even though kidney function is greatly reduced
Pharmacokinetics
What is the path/movement of drug distribution?
blood → interstitial space of tissues → cells
What are 3 major factors that determine drug distribution?
blood flow to tissues, adequate BP
ability of drug to exit the vascular system
ability of drug to enter cells
Pharmacokinetics
the movement of drugs through the body
what the body does to the drug
What lifestyle changes can a pt make if they have hypertension?
maintenance of potassium and calcium intake
sodium restriction (lowers BP)
DASH diet
alochol restriction
aerobic exercise
smoking cessation
Beta2 Agonists
SABA
LABA
What are factors that cause individual variation in drug responses?
pathologic variables → diminished function of kidneys (excrete) & liver (metabolize)
physiologic variables (age, sex, weight)
genetic predisposition (can alter the metabolism of drugs → unique/uncommon interactions)
drug interactions
PMHx
drug interactions (mult drugs interacting with e/o)
What much a LABA always been taken with?
glucocorticoid
What is the therapeutic levels of Theophylline?
10-20mcg/mL
What are s/sx of Theophylline plasma levels between 20-25mcg/mL?
n/v, diarrhea, insomnia, restlessness
**generally very sick
What are s/sx of Theophylline plasma levels above 30 mcg/mL?
severe dysrhythmias (v fib) and convulsions
**heart becomes affected
What should the nurse do when a pt is experiencing theophylline toxicity?
STOP theophylline
activated charcoal together with a cathartic
dysrhythmias respond to lidocaine
IV diazepam may help control seizures
Anticholinergic Drugs (Bronchodilators)
Ipratropium
Tiotroprium
Onset of therapeutic effect of ipratropium
therapuetic effects begin within 30 secs
reach 50% of max in 3 mins
persist ~6 hrs
Onset of therapeutic effect of tiotroprium
therapeutic effects begin about 30 mins after inhalation
peak in 3 hrs
persist ~24 hrs
reaches a plateau after 8 consecutive days
What is a half-life?
What is the dosing interval of a drug with a short half-life? Long-half life
the time required for the amount of drug in the body to decrease by 50%
short half-life → short dosing interval
long half-life → long dosing interval
How many half lives does it take for a drug to leave the body?
4
What is the normal range for digoxin?
0.5-0.8 ng/mL
What are signs of digoxin toxicity?
visual disturbances → halos around lights
n/v, diarrhea
Nursing considerations for digoxin administration
check HR before administration
hold & notify provider if levels are above range
Antihistamine pharmacodynamics
block H1 receptors to PREVENT action of histamine at these sites
Basic mechanisms by which neuropharmacological agents act
sites of action
steps in synaptic transmission
effects of drugs on the steps of synaptic transmission
What is one of the most desirable qualities a drug can have?
selectivity
can alter a disease process while leaving other physiologic processes largely unaffected (↑ processes affected = ↓ selective)
Stimulant Laxatives
Bisacodyl [Dulcolax]
Senna
Castor oil
What drug helps with opioid-induced constipation?
stimulant laxatives
How do stimulant laxatives work?
Stimulate the intestinal muscles to contract → increased bowel movements
What are adverse effects of nitroglycerin?
headache
orthostatic hypotension **make sure pt is sitting when taking
reflex tachycardia
What o
life-threatening hypotension
Nursing considerations for discontinuing nitro
discontinue gtt SLOWLY
How do you administer emergency nitroglycerin?
take 1st dose, wait 5 mins
if no sx resolution, take 2nd dose and call 911
take 3rd dose is still no sx resolution
How should you store nitrates?
light sensitive, original container
dry
room temp
What is the common ending for benzodiazepine drugs?
“-pam”
Sx of benzodiazepine oral overdose (toxicity)
drowsiness
lethargic
confusion
Sx of benzodiazepine IV toxicity
profound hypertension
cardiac arrest
respiratory depression (moderate unless combined with other CNS depressants)
**life threatening reactions
Pharmacologic effects of benzodiazepines
CNS depressant
reduce anxiety
promote sleep
induce muscle relaxation
What is the antidote for benzodiazepine toxicity?
FLUMAZENIL
I “flu” in my mercedes “benz”
Extrapyramidal symptoms (EPS)
(serious movement disorders)
pseudoparkinsonism
acute dystonia
akathisia
tardive dyskinesia
What atypical antipsychotic (SGA) would a pt use only if 2 other psychotics have been tried and failed?
Clozapine
What is the pneumonic for anticholinergic side effects?
can’t SEE
can’t PEE
can’t SPIT
can’t SHIT
What is the normal plasma levels of Lithium?
0.8-1.4 mEq/Lin the treatment of bipolar disorder.
What drug class does Lithium belong in?
mood stabilizers
What drug class does Fluoxetine belong in?
SSRI
At what time of the day should you take Fluoxetine?
morning (can cause insomnia)
Side effects of fluoxetine
withdrawal syndrome
teratogenesis
sexual dysfunction
weight gain
bleeding disorders
insomnia
What should be done if serotonin syndrome is suspected?
d/c drug immediately
What are the two potassium sparing diuretics?
Spironolactone (aldosterone antagonists)
Triamterene (nonaldosterone antagonists)
Adverse reactions to potassium sparing diuretics
hyponatremia (increased secretion of sodium)
hyperkalemia
benign and malignant tumors
endocrine effects
hypotension
What are the role of spacers for inhalers?
increases delivery of drug into the lungs
What drugs are bronchodilators?
SABA & LABA
Theophylline
Ipratropium & Tiotropium
How long should you wait in between puffs when using a MDI?
Between puffs if using 2 different meds/inhalers?
at least 60 sec
3-5 mins
What is the preferred method of administering inhalation drug therapy?
nebulizers
better absoption than MDI
preferred when in the hospital
Is ipratropium a fast or slow acting anticholinergic drug?
faster acting
often administered w/ albuterol
relieves broncospasm
Is tiotropium a fast or slow acting anticholinergic drug?
slower acting
will take about ~1 week before seeing full benefits
What drug do you administer when managing an acute severe exacerbation of asthma?
albuterol
How would you manage an acute severe exacerbation of asthma?
admin albuterol immediately (PRIORITY)
in the meantime:
sit pt up 90 degrees
supplemental O2
nebulized ipratropium
How would you manage a COPD exacerbation?
treat cause to treat exacerbation
SABAs
systemic glucocorticoids (for inflammation)
antibiotics
supplemental O2 (maintain sat of 88% to 92%)
Pharmacodynamics
what the drug does to the body
What drugs are used for allergic rhinitis?
glucocorticoids
antihistamines (oral and intranasal)
sympathomimetics (oral and intranasal)
What is the first choice drug to prevent rhinitis?
intranasal glucocorticoidsare the first-line treatment.
When is it best to take intranasal glucocorticoids for seasonal rhinitis?
2-3 weeks before allergy season (before onset of sx)
What is the preferred route of administration for allergy drugs?
intranasal
What drugs are used for coughs?
antitussives
expectorants
Pharmacodynamics of antitussives
supress cough
Pharmacodynamics of expectorants
make cough more productive (stimulates flow of secretions)
What is an example of an expectorant drug for cough?
Guaifenesin
What are examples (2) of opioid antitussive drugs for cough?
Codeine
Hydrocodone
What are examples (2) of non-opioid antitussive drugs for cough?
Dextromethorphan
Benzonatate
H1 Antagonists
1st gen vs. 2nd gen
1st generation
highly sedating (“i am so tired by 1am”)
2nd generation
less sedation than 1st gen (“i always get a second wind at 2”)
Therapeutic uses of antihistamine drugs
mild allergy
severe allergy (sx management only)
motion sickness
insomnia
common cold
Therapeutic use of drugs for diabetes mellitus
prevent long term complications
tighten blood glucose control
control blood pressure and blood lipids
What are the basic mechanisms by which neuropharmacological agents act?
sites of action (axons vs synapses)
steps in synaptic transmission
effects of drugs on the steps of synaptic transmission
Axonal conduction
conducting an action potential down the axon of the neuron
Synaptic transmission
information is carries across the gap between the neuron and the postsynaptic cell
What happens to the receptor activation when there is a block in reuptake?
increased receptor activation (more available)
Steps in synaptic transmission
transmitter synthesis
transmitter storage
transmitter release
What drug is contraindicated with nitroglycerin? Why?
Sildenafil
severe hypotension
What is the application procedure for transdermal contraceptive patches?
put on once a week for 3 weeks, followed by 1 week off (to permit normal menstruation)
Adverse effects of the transdermal contraceptive patch
breast discomfort
headache
local irritation
nausea
menstrual cramps
What location should you avoid placing a transdermal contraceptive patch? Why?
breast (risk for breast cancer)
What is the application process of a vaginal contraceptive ring?
one ring inserted each month
left in place for 3 weeks, then removed
withdrawal bleeding occurs during ring-free week
new ring inserted 1 week later
What should you do if a vaginal contraceptive ring is expelled in the following time frames:
< 3 hrs
> 3 hrs
< 3 hrs → wash with warm water and reinsert
> 3 hrs → wash and reinsert AND use backup contraception for 7 days
What oral drugs can be taken for erectile dysfunction?
sildenafil
tadalafil
What priapism?
What drug is it an adverse effect for?
an erection lasting longer than normal
seek medical attention if erection lasts > 4 hrs
Sildenafil
Sildenafil vs. Tadalafil (difference in timing aspect of med)
sildenafil → HAS timing aspect, peaks in 1 hr
tadalafil → DON’T need to time, effects last up to 36 hrs (“long acting viagra”)
What drugs are used to treat PUD?
Histamine 2 receptor antagonists
What ending do H2 receptor antagonist drugs have in their name?
-dine
How do H2 receptor antagonists work?
promote healing by suppressing secretion of gastric acid
What are H2 receptor antagonists used to treat?
gastric and duodenal ulcers
What is an example of a H2 receptor antagonist drug? What are its adverse effect?
Famotidine [Pepcid]
condusion
hallucinations
CNS depression (lethargy, somnolence)/excitation (restlessness, seizures)
increased risk of pneumonia (d/t elevation of gastric pH)
What are 3 antidiarrheal agents?
Which ones are opioids and which ones are non-specific antidiarrheals?
Diphenoxylate [Lomotil] → opioid
Loperamide [Imodium] → opioid
Subsalicylate [Pepto-Bismol] → nonspecific antidiarrheal
What is a notable adverse effect of Subsalicylate [Pepto Bismol]?
may blacken stools and tongue
don’t confuse with GI bleed and worry