ATI Pharmacology 3.0 Pain & Inflammation Drugs

Types of Analgesics
NSAID’s-interfere with prodiction of prostoglandins
Opiods-stimulate opiod receptors

Types of Anti-inflammatories
Glucocorticoids
Uricosurics

Drugs for pain
Nonopioid analgesics
Opioid analgesics
Opioid antagonists

NSAIDs (Cox-1 and Cox-2 Inhibitors)
Aspirin, ibuprofen (Advil, Motrin)
Naproxen (Naproxen, Aleve)
Indomethacin (Indocin)
Ketorolac

NSAIDs (Cox-1 and Cox-2 Inhibitors)
Expected actions
Inflammation suppression
Analgesia for mild/moderate pain
Fever reduction
Dysmenorrhea
Inhibition of platelet aggregation (aspirin)

NSAIDs (Cox-1 and Cox-2 Inhibitors)
Side/adverse effects
GI upsets (heartburn, nausea & gastric ulceration)
Bleeding (less with non-aspirin NSAIDs
Kidney dysfunction
Salicylism (aspirin-aspirin toxicity)
Reye’s syndrome (aspirin: vomiting, confusion, seizures, LOC, liver/brain damage & death)
Thromboembolic events (non-aspirin NSAIDs)

NSAIDs (Cox-1 and Cox-2 Inhibitors)
Interventions
Test for & tx helicobacter pylori
Recommend PPI during NSAID tx
Monitor I&O, BUN, & creatinine
Monitor for salicylism (tinnitus)
Recommend acetaminophen for children
Non-aspirin NSAID’s: monitor s/s of embolism events
Recommend low dose aspirin to prevent embolism events

NSAIDs (Cox-1 and Cox-2 Inhibitors)
Administration
Swallow enteric-coated or SR whole-do not crush/chew
D.C. Aspirin 1 wk before surgery
Monitor initial & continued therapeutic effects
Prophylactic use aspirin to inhibit platelet aggregation usually 81mg/day

NSAIDs (Cox-1 and Cox-2 Inhibitors)
Pt instructions
Take w/food, milk or 8oz Water; avoid ETOH
Report GI irritation
Report changes in urine output, wt gain or fluid retention
Do not give aspirin to children/adolescents <19 Non-aspirin NSAIDS: report s/s embolic event; low dose aspirin Report tinnitus, sweating, HA, & dizziness:stop aspirin

NSAIDs (Cox-1 and Cox-2 Inhibitors)
Contraindications/precautions
Contraindications:
Pregnancy risk cat D, lactation
Hypersensitivity to aspirin; NSAIDS
PUD; bleeding
Children/adolescents
Prior to surgery
Precautions:
Older adults
Cigarettes smoking, ETOH use disorder
Helicobacter pylori infection
HF, advanced kidney dz
Htn (non-aspirin NSAIDs)

NSAIDs (Cox-1 and Cox-2 Inhibitors)
Interactions
Anticoagulants, glucocorticoids, and alcohol increase risk of bleeding
Ibuprofen decreases antiplatelet effects of low-dose aspirin
ACE Inhibitors & Angiotensin receptor blockers increase risk of kidney failure
Antihypertensive effects of ACE Inhibitors decrease
Risk of lithium carbonate (Lithobid) and methotrexate toxicity increases

NSAIDs (Cox-2 Inhibitors)
Celecoxib (Celebrex)

NSAIDs (Cox-2 Inhibitors)
Expected actions
Analgesia for Mild to mod pain
Inflammation suppression
Fever reduction
Dysmenorrhea

NSAIDs (Cox-2 Inhibitors)
Side/adverse effects
GI upset, diarrhea, heartburn, nausea, gastric ulceration (less than Cox-1 inhibitors)
Renal dysfunction
Cardiovascular & cerebrovascular events

NSAIDs (Cox-2 Inhibitors)
Interventions
Monitor/report GI upset/bleeding
Test/treat Helicobacter pylori prior to long term therapy
Recommend PPI for high risk of GI bleeding
Monitor I&O; watch for low urine output & fluid retention
Monitor for rapid rises in BUN & creatinine
Recommend drug for short periods & low doses only
Recommend low-dose aspirin to prevent these events
Monitor s/s MI and CVA

NSAIDs (Cox-2 Inhibitors)
Administration
2 hr before or after magnesium- or aluminum-based antacids
Monitor for initial/continued therapeutic effects

NSAIDs (Cox-2 Inhibitors)
Pt instructions
Take low dose aspirin once daily reduce MI & CVA
Avoid ETOH
Report persistent GI upset/bleeding
Report changes inutile output, wt gain, signs of fluid retention such as edema or bloating
Report CO or heaviness, SOB, sudden/severe HA, numbness, weakness, visual disturbances, or confusion

NSAIDs (Cox-2 Inhibitors)
Contraindications/precautions

NSAIDs (Cox-2 Inhibitors)
Interactions
Diuretic effects of furosemide decreased
Fluconazole (Diflucan) increases celecoxib levels
Anticoagulant effects of warfarin (Coumadin) increase
Glucocorticoids & alcohol increase the risk of bleeding
Antihypertensive effects of ACE Inhibitors decrease
Risk of lithium carbonate (Lithobid) toxicity increases

Acetaminophen
Acetaminophen (Tylenol)

Acetaminophen
Expected actions
No anti-inflammatory effects
No anticoagulant effects

Acetaminophen
Side/Adverse effects
Liver damage (overdose)
Htn (with daily use-particularly women)

Acetaminophen
Interventions
Monitor for early s/s overdose/poisoning (abd discomfort, nausea, vomiting, sweating, diarrhea); liver damage results in 48-72 hrs following overdose
Admin acetylcysteine (Mucamyst, Acetadote) orally or IV to counteract overdose and reduce liver injury
Monitor BP, esp women who take regularly

Acetaminophen
Administration
Orally/rectally
No more the 4gm/day (>12yrs)
Give manufacturer’s recommended dose based on age (infants/children)
Caution it’s that the drug is available in many combination products as well as formulations; read labels carefully

Acetaminophen
Pt instructions
Do not exceed 4g/day for >12 yrs
Report abd discomfort, N/v/d/sweating immediately
Have BP checked regularly

Acetaminophen
Contraindications/precautions
Contraindications:
Alcoholism
Precautions:
Anemia
Immunosuppressive
Hepatic/kidney dz

Acetaminophen
Interactions
ETOH increases liver injury w/high doses of acetaminophen
Warfarin (Coumadin) increases risk of bleeding
Cholestyramine (Questran) reduces absorption

Centrally Acting nonopioids
Tramadol (Ultram)

Centrally Acting nonopioids
Expected actions
Moderate/severe pain
Binds to selected opioid receptors
Blocks uptake of norepinephrine & serotonin in CNS

Centrally Acting nonopioids
Side/adverse effects
Rare:
Sedation,ndizziness
HA, n/v/constipation, urinary retention
Respiratory depression (rare)
Seizures (rare)

Centrally Acting nonopioids
Interventions
Monitor pt when ambulating
Recommend lowest dose effective dose & short term only
Give w/food
Recommend antiemetic if n/v occur frequently
Measure baseline VS; monitor respirations
Resp rate <12 stimulate breathing Administer opioid antagonist, naloxone, to restore Resp rate Monitor for seizures, Institute precautions as needed Monitor for urinary retention

Centrally Acting nonopioids
Administration
Be aware it takes 1hr for analgesic effect to begin
Make sure patients swallow XR whole, do not crush or chew

Centrally Acting nonopioids
Pt instructions
Do not take prior to activities requiring mental alertness
Sit/lie down if lightheaded
Change positions slowly
Increase fiber intake
Increase activity & exercise
Take drug only when needed & short term
Report urinary retention to provider

Centrally Acting nonopioids
Contraindications/ precautions
Contraindications:
Acutely intoxicated w/ETOH, opioid, psychotropic drugs
Seizures disorders
Resp depression
Children <16 Precautions: Substance abuse hx Liver/kidney dz Increased ICP Older adults

Centrally Acting nonopioids
Interactions
MAOIS pose risk for htn crisis
Selective serotonin norepinephrine reuptake inhibitors, tricyclic antidepressants, MAOIS, and Triprans pose risk for serotonin syndrome
Response to CNS depressants increase
Carbamazepine (Tegretol) decreases levels
St. John’s wort increases sedative effects

Opioid agonists
Morphine
Fentanyl (Sublimaze)
Meperidibe (Demerol)
Methadone (Dolophine)
Codeine
Oxycodone (OxyContin, Percodan)
Hydrocodone (Vicodin, Lortab)

Opioid Agonists
Expected Effects
Analgesic moderate_severe pain
Preoperative Sedation & reduction of anxiety

Opioid agonists
Side/adverse effects
Resp depression
Sedation, dizziness, lightheadedness, drowsiness
Constipation, N/V
Orthostatic hypotension
Urinary retention
Cough suppression
Potential for abuse
Tolerance w/continued use & cross tolerance with other opioids

Opioid agonists
Interventions
Naloxone for <12/min Encourage urination every 4 hrs Prepare to insert urinary catheter to drain bladder

Opioid agonists
Administration
Measure baseline VS before administration & monitor throughout tx
Swallow XR whole, do not crush or chew
Administer IV by diluting as recommended & admin slowly over 4-5 mins; have naloxone & resuscitation equipment available
Monitor PCA use & pump settings carefully
Administration to cancer patients on a fixed schedule, around-the-clock, not PRN

Opioid agonists
Pt instructions
Take w/food or milk (oral)
Report inability/difficulty voiding
Cough regularly to clear secretions from throat & chest

Opioid agonists
Contraindications/precautions
Contraindications:
Pregnancy risk cat D (long-term use, high doses, near term, otherwise cat C)
Kidney failure
Increased ICP
Biliary colic, Biliary tract surgery
Preterm labor
Precautions:
Schedule II controlled substance
Older adults, infants
Reduced respiratory reserve
Head injury
Inflammatory bowel disease
Prostatic enlargement
Hypotension
Hepatic/kidney dz

Opioid agonists
Interactions
Anticholinergics (antihistamines, TCA) increase Anticholinergic effects (constipation, urinary retention)
MAOIs can cause hyperpyrexic coma (excitation, seizures, respiratory depression) with meperidine (Demerol)
Antihypertensives increase hypotension effects
St. John’s wort can increase sedation

Opioid agonists-antagonists
Butorphanol, pentazocine (Talwin)
Buprenorphine (Buprenex)

Opioid agonists-antagonists
Expected actions
Analgesia for mod to severe pain
Anesthesia adjunct
Fewer Resp depression, euphoria, dependence
Milder analgesic effects than opioids
Can precipitate withdrawal in pts addicted to opioids

Opioid agonists-antagonists
Side/adverse effects
Resp depression (limited)
Sedation, dizziness, lightheadedness, drowsiness
HA
Nausea
Increased cardiac workload (butorphenol & pentazocine)
Abstinence syndrome (less severe than that experienced by opioid-dependent pts)

Opioid agonists-antagonists
Interventions
Measure baseline VS & monitor respirations
RESP <12, withhold drug & stimulate breathing Monitor pts when ambulating Recommend alternative drug if nausea does not resolve Do not admin with MI or cardiac insufficiency Ask pts about opioid use before administration

Opioid agonists-antagonists
Administration
Pentazocine (Talwin) orally
Measure vs before administration, monitor respirations, do not give for respirations <12 Have naloxone (Narcan) & resuscitation equipment available For intranasal administration, give one spray & repeat every 60-90 min as needed Preoperative I'M, give 30-90 min before surgery Monitor therapeutic effects Do not DC drug abruptly

Opioid agonists-antagonists
Pt instructions
Take only when needed, short term
Do not use for angina pain
Do not take opioids while taking antagonists

Opioid agonists-antagonists
Contraindications/precautions
Contraindications:
Acute MI
Opioid dependence
Precautions:
Schedule IV controlled substance
Hx substance abuse
Head injury, increased ICP
Hepatic/kidney dz
Cardiac insufficiency
Htn

Opioid agonists-antagonists
Interactions
CNS depressants increase CNS depression & increase risk of resp depression
Opioid effects decrease

Opioid Antagonists
Naloxone
Methylnatrexone (Relistor-reverses constipation)
Naltrexone (ReVia, Vivitrol-reverses euphoria)

Opioid Antagonist
Expected actions
Reversal of opioid effects
Reversal of neonatal Resp depression (from maternal analgesia)

Opioid Antagonist
Side/adverse effects
Increased respiratory rate, BP, heart rate
Abstinence syndrome (htn, vomiting, tremors in opioid-dependent pts)

Opioid Antagonist
Interventions
Monitor vs, esp BP
Monitor rhythm for s/s ventricular tachycardia
Have O2 & resuscitation equipment available
Expect symptoms in opioid-dependent pts

Opioid Antagonist
Administration
IM, IV, SC
Titration dose carefully
Monitor vs
Be aware drug may increase pain & precipitate withdrawal
Prepare to admin every 2-3 min until reversal of undesirable effects
Prepare to begin admin again as effects of opioids might persist beyond the reversal agent
Observe for n/v tachycardia and diaphoresis (indications of opioid reversal)

Opioid Antagonist
Pt instructions
If awake, inform Pt of need for drug
Warn Pt of possible side effects & return of pain

Opioid Antagonist
Contraindications/precautions
Contraindications:
Opioid dependence
Resp depression due to nonopioids drug
Precautions: cardiac irritability
Head injury, increased ICP
Brain tumor
Seizures disorder

Opioid Antagonist
Interactions
Opioid effects decrease

Uricosurics
Allopurinol (Zyloprim)
Febuxostat (Uloric)
Probenecid

Uricosurics
Expected actions
Hyperglycemia that causes gout
Gout occurs secondary to cancer chemotherapy & blood dyscrasias

Uricosurics
Side/adverse effects
Hypersensitivity syndrome (fever, rash, eosinophilia, liver/kidney dysfunction)
GI disturbances
Drowsiness, headache, vertigo
Agranulocytosis, aplastic anemia, bone marrow depression
Metallic taste
Cataracts (>3 years of tx)

Uricosurics
Interventions
Monitor symptoms of hypersensitivity syndrome
Stop drug immediately for signs of hypersensitivity syndrome
Monitor worsening GI effects
For vomiting, ensure adequate hydration
Give after meals
Monitor for drowsiness/vertigo when ambulating
Monitor CBC, liver, kidney function & uric acid levels
Monitor for unusual taste
Recommend regular ophthalmic examinations

Uricosurics
Administration
Orally or IV
Monitor uric acid levels (initially & q1-2 was to establish appropriate dose)
Obtain baseline CBC, liver, kidney function tests before therapy & monitor periodically thereafter
Allow crushing tabs & mixing with food or fluid
Administration IV using recommended dilution & infuse over 30 to 60 mins
Make sure pts drink at least 3L/day

Uricosurics
Pt instructions
Report fever, rash, abdominal pain, swelling, low urine output immediately
Drink 3L/day
Report bleeding, easy bruising, or sore throat
Report blurred vision and/or loss of color acuity
Minimize exposure of eyes to sunlight
Obtain periodic eye exams

Uricosurics
Contraindications/precautions
Contraindications:
Hypersensitivity to allopurinol
Precautions:
Bone marrow suppression
Liver/kidney dysfunction
PUD
Lower GI dz

Uricosurics
Interactions
Warfarin (Coumadin) requires lower dosages
Risk of mercaptopurine (Purinethol), theophylline (Theolair), and azathioprine (Imuran) toxicity increases
Ampicillin (Principen) increases the risk for rash

Glucocorticoids
Prednisone (Deltasone)
Hydrocortisone sodium succinate (Solu-Cortef)
Methylprednisolone (Solu-Medrol)

Glucocorticoids
Expected actions
Symptomatic relief of pain & inflammation for a wide variety of disorders: inflammatory disorders& autoimmune disorders
MGMT of many skin disorders; allergic reactions
Delay of progression of some disorders, rheumatoid arthritis
Prevention of organ rejection
adjunctive therapy for some cancers
Suppresses inflammation/immune response

Glucocorticoids
Aide/adverse effects
Suppress adrenal function
Hyperglycemia
Myopathy
PUD, GI discomfort
Infection
Fluid/electrolyte imbalance
Fat redistribution-truncal obesity with moon-face & buffalo hump(long-term therapy)
Bone loss
Cataracts (long-term therapy)

Glucocorticoids
Interventions
Larger doses during stress & illness
Monitor glucose levels, esp DM
Observe for GI bleeding
Give w/food or meals
Recommend analgesic substitute if NSAIDs prescribed
Observe signs of infection that may not include fever/inflammation
Recommend initiation of appropriate abx therapy & regular eye exams
Monitor I&O; watch for crackles in lungs, & unexplained wt loss (hypernatremia)
Monitor also for generalized weakness (hypokalemia) and Cushing-like effects (and fat, buffalo hump & moon face)
Recommend lowest possible effective dose and alternate-day dosing

Glucocorticoids
Administration
IV, IM, Sc, topically, intranasally, or inhalation
Short-term oral use the largest dose is given day 1 w/progressively smaller doses for each of next 8 days
Long-term use (10 days or more), take in am using alternate-day dosing
Give supplemental doses as needed in times of stress

Glucocorticoids
Pt instructions
Avoid taking NSAIDS
Taper drug before D.C.
Report polyphagia, poly dips is, & polyurireport muscle pain/weakness
Perform wt bearing exercise daily; consume adequate calcium & Vit D; minimize exposure of eyes to sunlight
Report signs of infection, wt gain, edema (hypernatremia)
Report blurred vision & loss of color acuity (cataract)
Obtain periodic eye exams

Glucocorticoids
Contraindications/precautions
Contraindications:
Systemic fungal infection
Cataracts
Precautions:
HF
PUD
DM
Htn
Kidney dysfunction
Myastheniangravis
Osteoporosis

Glucocorticoids
Interactions
Glucocorticoids prevent replaponse to vaccines
Live vaccines administration increases risk for developing that viral dx
Potassium-depleting diuretics, furosemide increase risk of hypokalemia
Risk of digoxin-induced dysrhythmias increase with digoxin
NSAIDs increase risk of GI bleed & ulceration
Effects of insulin & oral hypoglycemics decrease in its with DM

What are the pain mediating chemicals found in the body? Substance P, prostaglandins, bradykinins, and histamine What does the body produce and release in response to pain? Body releases serotonin and produces enkephalins and endorphins which bind to opioid receptors …

Therapeutic Use (NSAIDS: COX-1 & COX-2 INHIBITORS) – aspirin, ibuprofen (Advil, Motrin) • Inflammation suppression • Analgesia for mild to moderate pain • Fever reduction • Dysmenorrhea • Inhibition of platelet aggregation (aspirin) Administration (NSAIDS: COX-1 & COX-2 INHIBITORS) • …

Older adult patient about take prednisone for long-term treatment of rheumatoid arthritis. Monitor for what adverse effects? Bone loss prednisone (glucocorticoid) can cause osteoporosis esp with long-term use increase weight-bearing activity and report back pain. HCP must monitor bone density …

A health care professional should understand that naloxone can reverse the effects of an excessive dose of which of the following drugs? A) Aspirin B) Acetaminophen (Tylenol) C) Morphine D) Prednisone ANS: C Rationale: Naloxone, an opioid antagonist, reverses the …

A health care professional is caring for a patient who is opioid-dependent and is about to begin taking butorphanol (stadol). The health care professional should recognize the patient is at risk for developing a sundrome that causes which of the …

Naloxone reversea excessive dosage of: Morphine Naloxone, an opioid antagonist, reverses the effects of morphine, an opioid analgesic. HCPs should monitor respirations and reassess pts after the effects of naloxone have diminished (20-40 minutes) for recurrence of the adverse effects …

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