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Pharmacology
study of drugs that alter functions of living organisms
Pharmacotherapy
use of drugs to prevent, diagnose, or treat signs, symptoms, and diseases
Pharmacodynamics
drugs mechanism of action and effect on an organism, target cells
Ligand-gated ion channel
G protein-coupled receptors
Enzyme-linked receptors
Intracellular receptors
Medications
Drugs given for therapeutic purposes, can be given for local or systemic effects
Where do drugs come from?
Plants, animals, minerals, laboratories
Synthetic drugs are less likely to have allergic reactions, semisynthetic (antibiotics) are naturally occurring but chemically modified
Effects of medication
Local: at site of application (local anesthesia, sunscreen)
Systemic: taking into the body, circulated through bloodstream to sites of action and will be eliminated from body (most drugs given!!)
Drug classification
Classified by specific body systems (bronchodilator), therapeutic uses (anti-inflammatory), chemical characteristics (sulfa drug)
Many drugs fit into multiple
Prescription vs. non
Controlled vs. noncontrolled substances
Prototype
Individual drug that represents groups of drugs (usually first/original drug in class, most effective)
Similar drugs are compared
Drug names
Generic: original designation, lower case, law requires generic Rx to decrease cost (not absolutely chemically identical to trade)
Trade/brand: pharmaceutical company, capital letter
Patent: protects pharmaceutical manufacturer, expensive and time consuming, but others cannot manufacture drug
Chemical name: reflects chemical structure
DAW dispensed as written do not substitute
Properties of an ideal drug
Effectiveness (most important)
Safety: cannot produce harmful effects
Selectivity: only the response for which it is given
Pharmacoeconomics vs. Pharmacogenomics
Pharmacoeconomics
Costs of drug and effects (is it beneficial, storage, dispensing, administration, lab testing)
Identify drug therapy to provide benefits at lowest costs
Pharmacogenomics
Study of how one’s genetic makeup, or genome, affects the body’s response to drugs
Helps providers choose drugs and doses that work best for an individual
Prescription vs. Non-prescription drugs
Prescription
Written by provider
OTC
Do not require prescription, still regulated by law
Can mask the symptoms of underlying diseases, inaccurate self diagnosis, may result in drug interactions (adverse drug reactions), can lead to overdoses/toxicity
FTC suppresses misleading
FDA regulates manufacture, distribution, ads, and labeling of drugs
Controlled substances
Categorized according to therapeutic usefulness and abuse potential
Classes:
Schedule I: high abuse potential, psychological effects, no accepted medical use, only dispensed for research (heroin, LSD, X)
Schedule II: high abuse, severe dependence ability (opioid, codeine, morphine, hydromorphone, methadone, oxycodone) locked and no refills
Schedule III: less abuse, prescription expires in 6 months
Schedule IV: less abuse (antianxiety, benzodiazepines)
Schedule V: limited abuse, 18, must be recorded
Drug approval processes
Phase 0: chemicals tested on lab animals (3.5-4yr)
Phase 1: chemicals tests on healthy human volunteers (1-3yr)
Phase 2: drug tried on informed 100-300 patients w/ disease (2-3yr)
Phase 3: drug tested in vast clinical market patients with disease/diaries/placebo (2-3yr)
Phase 4: obtain FDA approval, continual evaluation(2-3yr)
1 in 10,000 are approved
Black box warning
Withdrawal of approved and marketed drugs: serious adverse effects that become evident only when drugs are used in large, diverse populations
Ex. antidepressants (suicide)
Rights of medication administration
Right drug
Right dose (how much?)
Right patient (correctly identified)
Right assessment (do they need it?)
Right route
Right time
Right reason
Right documentation
Right patient education
Right evaluation (check to see if it worked)
Right to refuse
3 medication checks : read label after selecting container, after take medication and compare to MAR, right before giving dose to pt
Pharmacokinetics
How the body interacts with administered substances for the duration of exposure
ADME (absorption, distribution, metabolism, excretion)
Absorption
How the drug enters bloodstream
Orally: has to get into stomach/intestine and get absorbed into blood
First-pass effect: drug is reduced in concentration before reaching bloodstream
Distribution
Transport of drug molecules within the body
Protein binding: combines with protein for complex, and only the free/unbound portion acts on cells
BBB: controls substances from passing through
Metabolism
Body chemically alters drugs into water-soluble, so that it can be excreted (biotransformation) LIVER!!!
CYP 450 inhibitors - inhibit drug metabolism, CYP 450 inducers - accelerates drug metabolism
Excretion
Kidney, urine
Bile, saliva, sweat, feces, milk, exhaled air
Serum drug levels
amount of a drug in the blood at a particular time
Ligand-gated ion channel
When specific drug attaches to channel’s receptor, specific ions can pass through (GATE)
Membranes of neurons
GABA receptors, nicotinic ach
Lorazepam, ketamine
G Protein-coupled receptors
In cell membrane
When substances bind, signals are sent to a G protein which seperates
Dopamine receptors, etc.
Antihistamines, beta blockers
Enzyme-linked receptors
When a ligand binds to the binding site, the receptor changes, and the change activates an enzyme, which triggers reactions to change gene expression
Insulin, growth factors
Intracellular receptors
Drugs are hydrophobic and lipid-soluble
When drugs combine with receptor, transcription occurs and desired actions
Steroids
Agonist vs. Antagonist drugs
Agonist: activate receptors (oxycodone)
Antagonist: block action of other drugs by blocking (Naloxone)
Drug-related variable that affect drug actions
Dosage: reason for use, potency, route
Loading dose: initial higher dose to be given before given a lower maintenance dose
Route: oral is slow, IV is fastest, transdermal is very slow, inhalation/IM is fast
Drug-diet: tyramine / antidepressants, vitamin K / anticoag, calcium / antibiotics, grapefruit / statins
Drug-drug: altered drug metabolism
Age
Body weight
Ethnicity
Pre-exisiting conditions, psychological factors
Gender
Drug toxicity
Goal of treatment: start treatment ASAP, stable ABCs, reduce absorption/increase elimination, antidotes
Opioids: Narcan (naloxone)
Warfarin: Vit K
Heparin: Protamine sulfate
Digoxin: Digoxin Immune Fab
Acetaminophen: Acetylcystein
Activated charcoal if poison ingestion/overdose (do not use if aspiration risk or obstruction)
Med errors
Risks: incorrect dose, incorrect diagnosis/meds, undetected reaction, not following guide, interactions
Nurses need to have enough drug knowledge to recognize an error in an order
Changes to prevent medication errors
Computerized provider order entry (order isn’t on paper, less issues)
Bar coding (can give error message and alarm, records drug/dose/time)
Point of care (Time)
Less abbreviations
Accurate med history, avoids errors, updated list given to next provider and patient
Electronic prescribing
Medication orders
Full name of pt. drug, dose, route, frequency, date, time, signature of prescriber
Orders: typed or written into record
Verbal orders: written on order sheet, signed by person taking order, later cosigned by prescriber
Drug prep and dosage forms
Enteric-coated tablets are coated with a substance insoluble in stomach acid
Controlled-release: long-acting
Transdermal formulation: absorbed clonidine, estrogen, fent, nitroglycerin (over period of time)
Pump: external or implanted under skin, refillable or long acting w/o refill
Solution/ointment/cream/supp: topically or mucous membrane
Injections
Sterile needles and syringes: measure and administer parenteral meds
usually 25 gauge (small) is used for sub q injections, and 22-20 (bigger) is for IM
S/C: upper arm, abdomen, back, thigh
IM: deltoid, ventrogluteal, vastus lateralis
IV: veins on back of hands and forearm
Children implications
Faster toxic level, as there are less receptors so molecules are roaming
Slower gastric emptying, delayed intestinal mobility, different routes, more water so more water-soluble, immature liver and kidneys
Safety: always check with another nurse, use weight-based doses, Leur lock syringes for IV, use pumps, teach caregivers, be safe with storage/access/administration
Geriatric implications
Older adults are more prone to antibiotic-resistant infections, more drug-drug interactions, slowed body systems (increased toxicity)
More fat, prolonged half-life, less receptors
Beers criteria: inappropriate medications for adult populations, need to be adjusted, ANTICHOLINERGICS (benadryl)
More likely to be dehydrated, decreased gastric acidity (more basic), increased infections
POLYPHARMACY, (slow and low), altered mental and visual status, always consult the provider before stopping a medication
Pregnancy implications
No drug is considered safe during pregnancy
Folic acid for neural tube abnormalities (spinabifida)
Physiologic changes: more blood volume/output/flow/weight/fat/kidney flow/hormones
Drugs are more diluted, and dosage may need to increase, more excretion in kidney until 3rd trimester
Lactation: many drugs reach milk, use alcohol in moderation, caffeine, smoking, drugs
Fetal therapeutics: digoxin (fetal tachy/heart failure), levothyroxine (hypothyroid), penicillin (syphilis), corticosteroids (decrease resp. distress)
estrogen, progestin, Ortho-Novum
Estrogen: BATS (antibiotics, alcohol, smoking, seizure meds (inc preg)) St. John’s lowers effectiveness (inc. risk of endo cancer, thrombo, dementia, breast cancer) teach about ACHES
Progestin: increased CV risk, bone loss (If HRT, test liver function)
Ortho-novum: prevent pregnancy, acne
MOA: inhibit ovulation, prevent follicle from forming, thin endometrium, thicken mucus
Interactions: Do not take while pregnant, breastfeeding, smokers 35 years or older, reproductive cancers, abnormal kidney/liver function (STOP if jaundice), diabetes, high BP, migrane
Adverse: gallbladder disease, thromboembolism
Drug interactions: (dec.) anticonvulsant, barbs, benzo, St. John, Topiramate, succinimides
Teaching: assess knowledge, adherance, lowest dose/shortest duration, VTE signs, intact uterus only
sildenafil (Viagra)
Class: PDE5 Inhibitors
MOA: vasodilate smooth muscle
Use: ED (po), pulmonary arterial hypertension for males
Adverse: irreversible loss of vision, sudden hearing loss, priaprism
Side effect: priaprism, headache, flushed
Interactions: NITRATES (they already dilate), (inc) alcohol, antihypertensives, grapefruit juice, saw palmento (dec) fatty foods
Teaching: no more than once a day
finasteride (Proscar)
Class: 5-Alpha Reductase Inhibitors
Use: BPH, male pattern baldness (po)
MOA: reduce enlargement (shrink) prostate
Adverse: impotence, gynecomastia, reduced libido, ejaculatory disorders, decreased sperm
Side: hypotension
Interactions: (dec) testosterone, anticholinergics (inc) saw palmetto
Teaching: 3 TO 6 MONTHS, females do not take, esp if pregnant or lactating do not stay near, no abnormal kidney function pt, no regard to food once per day, check for improved urinary function, unable to void (pass urine, fever) call provider, DIZZINESS, do not give blood
tamulosin (Floxmax)
Class: Alpha 1-Adrenergic Blockers
MOA: RELAX muscles in prostate/bladder neck
Use: BPH, female urethral calculi expulsion
Adverse effects: POSTURAL HYPOTENSION
Side effects: Ejaculation failure/retrograde/decreased, weakness, sleepy, insomnia, stuffy/runny nose, sore throat, vision blurry
Contraindications: Cimetidine, alpha blocker (antihypertensives), anticoagulants, PDE5 (inc. orthostatic hypotension)
Teaching: immediate effects!, enzyme system is essential, take 30 after eating same time, DO NOT OPEN/CLOSE/CHEW, assess for decreased frequency/hesitancy/urgency/dribble/nocturia/improved force, pain, assess for OH/insomnia, vision, congestion, etc.
Insulin basics
Rapid acting (Lispro): 5-15 minutes onset, peak 1-2 hrs
Short acting (Regular): 30-60 min, peak 2-3 hrs, can be given IV
Intermediate acting (NPH): 2-4 hrs, peak 4-12 hrs, can be combined with short
Long acting: 24 hr, steady control, CANNOT MIX, NO PEAK
MUST ROLL CLOUDY INSULIN
Insulins
Reg: short-acting, peak 2-3 hrs, can wait 30 min to eat, IV use, DKA, hospital, GIVE BEFORE REG (clear before cloudy)
NPH: intermediate, 4-12 hrs peak, eat immediately, pumps/meals, GIVE AFTER REG (clear before cloudy)
Class: Insulins
Use: Hyperglycemia, treating type 1 and 2 DM, and GDM
Adverse effects: hypokalemia, hypoglycemia, lipodystrohy, allergic rxn, edema
Side effects: weight gain, injection site reaction, mild hypoglycemia
Contraindications: Beta-blockers (inc. effects), corticosteroids and diuretics (dec. effects)
Teaching: Rotate injections, avoid problem areas, balanced diet/exercise, clean skin, carry sugar with you, can use open vial for up to 28 days, safe for pregnancy/lactation
glyburide (glynase)
Class: sulfonylureas (oral)
MOA: stimulate beta cells to release insulin (hypoglycemia effect)
Use: insulin for those with some beta-cells, type 2 DM
Adverse effects: hypoglycemia (common), GI upset, sunburn
Contraindications: Type 1, sulfa allergy, severe renal/hepatic impairment, PREGNANCY (macrosomia)
Teaching: Elder pt. have higher hypoglycemia risk, 30 minutes before meals
metformin
Class: biguanide
MOA: reducing the production of glucose from liver
Use: can be taken alone or with others, type 2 diabetes (no weight gain!)
Adverse effects: LACTIC ACIDOSIS (sob)
Side effects: GI issues, metallic taste, vitamin B12 deficiency
Contraindications: steroids, thyroids, oral contra, antipsychotics, pseudophedrine, dye, nsaids, ace inhibitors, diuretics, alcohol
Teaching: discontinue 48 hrs before and after contrast test, take with meals, do not skip meals
sitagliptin (Januvia)
Class: dipeptidyl peptidase 4 (DPP-4) inhibitor
MOA: increases incretin hormones
Use: lowers blood sugar levels
Adverse effects: pancreatitis, severe joint pain, heart failure risk
Teaching: 30 min before meals, refrigerate, discuss herbal supplements with provider, drink fluids, seek attention if level is above 250
glucagon
Class: anti-hyperglycemics
Use: severe hypoglycemia, patient is unconscious and unable to swallow
Adverse effects: vomit, avoid with tumor, increase HR and BP, headache, itchy
Contraindications: warfarin (+ anticoag effect), anticholingerics, indomethacin, allergy to glucagon
Teaching: cannot take oral meds, if IV, use dextrose over glucagon, POSITION ON SIDE, assess LOC, check blood glucose, can be given IM SQ IV
Diabetic tests
Hba1c: percentage of glycated hb in blood for 2-3 months, explain it doesn’t replace daily test, low Hb may have low A1c, iron deficiency may have high A1c
normal: below 5.7%
pre: 5.7%-6.4%
diabetes: 6.5% or higher
Fasting blood sugar: glucose after 8hr fast, water is permitted
normal: less than or equal to 100 mg/dL (to 125 can be pre, higher is diabetes)
epoetin alfa
Class: erythropoiesis-stimulating agents
MOA: helps produce more RBCs
Use: anemia w/ CKD, anemia w/ HIV, below 10 g/dL
Adverse effects: HTN, increased risk of MI and STROKE
Contraindications:
age: retinopathy for infants, do not give in multi-dose vial
be careful with people with existing HTN
chemo-meds (lenalidomide) → thrombus formation
Teaching: Do not shake, freeze, or dilute; iron supplments, discard after 21 days, check HB, HC, goal is no more than 12 g/dL, check BP, make sure clean and healthy lifestyle, take foods with vitamin C for absorption
filgrastim
Class: colony-stimulating factors
MOA: stimulate WBC by bone marrow
Use: patients with bone marrow transplant or chemo-induced neutropenia, neutropenia
Adverse effects: flu-like symptoms, bone pain, splenic rupture (L upper quad, L shoulder)
Contraindications:
age: peds: spleen enlargement, pregnancy: preservative-free solution
known sensitivity, e. coli
Teaching: Do not shake, use once, do not give w/i 24 hrs of chemo infusion, take tylenol for bone pain, isolation, RECOGNIZE ISSUE IF WBC IS MORE THAN 100,000 cells/mm3
immunizations
Adults have 1 dose in older age of MMR, Tdap every 10 years, pneumococcal at 65 yrs, no live vaccines during pregnancy, flu for children over 6 years
Flu
IM injections for everyone, only nasal if they can have live
New vaccine every year, strains change each year (protection 2 wks after injection) does not cause flu
Do not give is GBS, allergic rxn, severe egg allergy
Wait if someone is mod-severe sick to give vaccine
MMR
Live virus
1st dose: 12-15 months, 2nd dose: 4-6 yrs, 1 dose if born after 1957
No for pregnancy, immunocompromised, hx of allergy to neomycin/gelatin, thrombocytopenia, seizure hx
Lifelong immunity, tylenol not aspirin
cyclophosphamide
Class: Alkylating agent
MOA: treat cancer by decreased DNA synthesis
Use: Cancer, autoimmune
Adverse effects: myelosuppresion, hemorrhagic cystitis, alopecia, GI distress, anemia, bleeding, fatigue, mucositis, N/V, neutropenia, myelosuppression, thrombocytopenia, nephrotoxic, hepatotoxic
Contraindications: active infections, pregnancy/lactation, azole antifungal, erythromycins, protease inhibitors, CYp3A4, myelosuppression
Teaching: drink 2-3q of water, urinate frequently, avoid crowds, neutropenic precautions, iron foods
hemorrhagic cystitis
methotrexate
Class: Antimetabolite/antifolate
MOA: Antineoplastic, intereferes with DNA synthesis, ectopic pregnancy
Use: Treatment of cancer, chemotherapy, autoimmune
Adverse effects: Bleeding, fatal opportunistic infection, change in mental status, nephrotoxic, photosensitivity, hepatotoxicity, alopecia, anemia, bleeding, fatigue
Contraindications: pregnancy/breastfeeding, blood dyscarias, immunocompromised, alcoholism, azole antifungal, erythromycins, protease inhibitors, CYp3A4 inducers
Teaching: Immunocompromised, avoid crowds, wear masks, get vaccinated but not live vaccines, once a week, folic acid, iron-rich foods, schedule/route/dosage are important, leak around tissue (extravasation), free flow of IV fluid into the vein and assess
avoid aspirin, alcohol, BC before and after 6 months
infliximab
Action: TNF alpha blocking
Use: autoimmune
Adverse effects: serious infections/malignancies, infusion reactions, hepatotoxicity, CV, neutropenia, leukopenia, thrombocytopenia, auto-immune diseases, rash, HTN, skin injection site rxn, chills, dyspnea, chest pain
Contraindications: active infections, heart failure, hypersensitivity, methotraxate, echnacea, live virus
Teaching: infections prevention, TB tests, infusion monitor, cancer risks, vaccines (no live), delayed reactions
cyclosporine
Class: Immunosuppressant
MOA: Inhibits T-lymphocyte activation, reduces Interleukin-2 (IL-2)
Use: Transplant rejection, autoimmune disorders
Adverse effects: Nephrotoxicity, HTN, infection risk, high risk of malignancy,hyperlipidemia, hirsutism, hyperkalemia
Contraindications: grapefruit, don’t mix with other antirejections, antibiotics/fungals, st johns
Teaching: Avoid crowds, live vaccines/fresh flowers/raw food, test WBC, can increase risk of infection, do not crush/chew, sun safety, don’t take hrs prior to transplant, do not give in plastic/Styrofoam, dilute neoral w/ orange/apple juice, drink all immediately, infection risk, no other drugs, same time everyday, don’t rinse syringe, same time every day, do not miss dose
Radiation
- Can cause DNA damage, long exposure is harmful (non-ionized)
- EBRT - external, avoid putting things on site, loose clothes, sun protection
- Brachytherapy - private room, time/dis/shield principles, cluster care, limit visitors, use lead shielding, radiation badges
- Side effects: pruritis, erythema, burning, sloughing, anorexia, N/V, diarrhea, bone marrow depression