Pain and Inflammation

(General Key Points)

N203
ATI (Unit 4)
Pain & Inflammation -
 Analgesics relieve pain
 Narcotics / NSAIDs / Antimigraine agents

 Anti-inflammatory medications relieve inflammation

 Salicylates / Glucocorticoids / Antigout / Disease-modifying
antirheumatics drugs (DMARDs)
 Some are antipyretic (salicylates, ibuprofen)

 Salicylates and NSAIDs reduce platelet aggregation

 Salicylates, NSAIDs, and glucocorticoids pose risk for ulceration

 Acetaminophen has analgesic and antipyretic properties but not anti-

inflammatory. It poses a risk for liver injury
 NSAIDs
(Medication List)

N203
ATI (Unit 4)
Pain & Inflammation -
 Aspirin  Ketorolac (Toradol)
 Celecoxib (Celebrex)  Valdecoxib (Bextra)
 Ibuprofen  Indomethacin
 Naproxen 
 
NSAIDs

N203
ATI (Unit 4)
Pain & Inflammation -
Expected Action: Proto: aspirin, ibuprofen, ketorolac, celecoxib

 Cyclooxygenase inhibition – COX 2  inflammation, COX 1   platelet agg.

Therapeutic Uses:  Inflammation suppression / analgesia /  fever
 dysmenorrhea / suppression of platelet aggregation
Adverse Effects:
 GI discomfort, aspirin induced ulceration and bleeding (use misoprostol as
prophylaxis, and/or PPI and/or H2-receptor agonist  risk of ulceration)
 Renal dysfunction  Salicylism (tinnitus, resp.
 Reye syndrome (in kids with viral illnesses) alkalosis, dizziness)
Contraindications/Precautions:
 Peptic ulcers / bleeding disorders / hypersensitivity / pregnancy / kids ĉ viral inf.
Interactions:  Glucocorticoids ( gastric bleeding) – use antiulcer
 Warfarin ( bleeding) prophylactic like misoprostol (Cytotec) to prevent
 EtOH ( bleeding)  Ibuprofen ( antiplatelet effects of low-dose aspirin)
Education:  Give with food or milk to reduce GI discomfort.
 If can’t tolerate 1st generation, give 2nd generation (celecoxib)
Ketorolac (Toradol)

N203
ATI (Unit 4)
Pain & Inflammation -
Expected Action: Proto: ketorolac (Toradol) – 1st generation NSAID

  pain without anti-inflammatory effect

Therapeutic Uses:
 Short-term treatment of moderate to severe pain (post-op)
 Enhances opioid analgesia without opioid adverse effects
Adverse Effects:
 Can occur when used with other NSAIDs.
 GI bleeding / blood dyscrasias
Contraindications/Precautions:
 Give no more than 5 days
Interactions:
 Other NSAIDs / anticoagulants ( bleeding)
Education:
 Usually started parenteral and then transition to oral dose
Acetaminophen

N203
ATI (Unit 4)
Pain & Inflammation -
Expected Action:
 Slows production of prostaglandins
Therapeutic Uses:
 Analgesic and antipyretic
Adverse Effects:  Max 4 g daily
 Acute liver toxicity  Antidote: acetylcysteine (Mucomyst)
Contraindications/Precautions:

Interactions:
 EtOH   risk to liver / Warfarin   levels of warfarin
Education:

Opioid Agonists

N203
ATI (Unit 4)
Pain & Inflammation -
 Proto: morphine, fentanyl, meperidine, methadone, codeine,
Therapeutic Uses: oxycodone
 Moderate to severe pain / Sedation /  bowel motility / Cough suppression
 Respiratory
Adverse Effects:  Sedation
depression
 Constipation  Orthostatic Hypotension  Urinary retention
 Biliary colic  Cough suppression  Emesis
Contraindications/Precautions:  Increases cardiac workload
 Meperidine metabolites are neurotoxic  (< 600 mg/24hr, < 48 hours)
Interactions:
 CNS depressants (barbiturates, phenobarbital, benzodiazepines, EtOH)
 Anticholinergics, antihistamines, tricyclic antidepressant  anticholinergic effects
 MAOIs (hyperpyrexia, seizures)  Antihypertensives
Education:  Withhold if RR<12  Have naloxone (Narcan) and resuscitation
 Infuse IV slowly over 4-5 minutes equipment available.
Opioid Antagonists

N203
ATI (Unit 4)
Pain & Inflammation -
Expected Action: Proto: naloxone (Narcan), naltrexone, nalmefene

 Competitively interfere with opioid actions

Therapeutic Uses:
 OD treatment  Reversal of opioid effects
Adverse Effects:
 Tachycardia / Tachypnea  Abstinence syndrome (cramping, hypertension)
Contraindications/Precautions:
 Hypersensitivity  Dependency  Pregnancy: B
Interactions:

Education:
 Naloxone has extensive first-pass modification
 Observe for w/d symptoms or abrupt onset of pain
Adjuvant Pain Medications
(Medication List)

N203
ATI (Unit 4)
Pain & Inflammation -
 Tricyclic Antidepressants (TCA).........................Amitriptyline (Elavil)
 Anticonvulsant..............................................Carbamazepine (Tegretol)
 .............................................................................................................
Gabapentin (Neurontin)
 .............................................................................................................
Phenytoin (Dilantin)
 CNS Stimulants.............................................Methylphenidate (Ritalin)
 .............................................................................................................
Dextroamphetamine (Dexedrine)
 Antihistamines....................................................Hydroxyzine (Vistaril)
 Glucocorticoids...........................................Dexamethasone (Decadron)
 .............................................................................................................
Prednisone (Deltasone)
 Bisphosphonates...................................................Etidronate (Didronel)
 .............................................................................................................
Pamidronate (Aredia)
Adjuvant Medications

N203
ATI (Unit 4)
Pain & Inflammation -
 Proto: TCAs, Anticonvulsants, CNS stimulants, Antihistamines,
Therapeutic Uses:
Glucocorticoids, Bisphosphonates
 Enhance opioid effects thereby permitting lower opioid doses
 Alleviate other symptoms that aggravate pain  Treat neuropathic pain
Adverse Effects:
 TCAs (neuropathic pain)  Orthostatic hypotension, sedation, anticholinergic
effects
 Anticonvulsants (neuropathic pain)  Bone marrow suppression
 CNS stimulants  Weight loss, insomnia
 Antihistamines  Sedation
 Glucocorticoids ( ICP,  Adrenal insufficiency  Glucose intolerance
nerve compression)  Hypokalemi  Osteoporosi  GI Ulcers
a s
 Bisphosphonate (CA bone  Flu-like symptoms  Injection site irritation
pain)
Antigout Medication

N203
ATI (Unit 4)
Pain & Inflammation -
Expected Action: Proto: Colchicine, indomethacin, allopurinol, probenecid

 Colchicine/Indomethacin:  inflammation by preventing leukocyte infiltration

 Allopurinol: Inhibits production of uric acid
 Probenecid: Inhibits reabsorption of uric acid by renal tubules
Therapeutic Uses:  Colchicine/Indomethacin: Acute gout attacks
 Allopurinol/Probenecid: Hyperuricemia
 Probenecid: Prolongs effects of penicillins and cephalosporins
Adverse Effects:  Colchicine: GI toxicity  Others: GI discomfort
 Probenecid: Renal injury (get 2-3L fluid/day)
Contraindications/Precautions:  Colchicine: Pregnancy (C/D), renal, cardiac, elderly
Interactions:  Salicylates: η probenecid
 Warfarin:  warfarin metabolism in liver  bleeding risk
Education: Avoid EtOH, purines. Adequate hydration.
Migraine Medications
(Medication List)

N203
ATI (Unit 4)
Pain & Inflammation -
 Ergot Alkaloids....................................................Ergotamine (Ergostat)
 Serotonin Receptor Agonists................................Sumatriptan (Imitrex)
 Beta-Blockers........................................................Propanolol, Atenolol
 Anticonvulsants..................................................Divalproex (Depakote)
 Tricyclic Antidepressants.....................................Amitriptyline (Elavil)
 Calcium Channel Blockers.....................................................Verapamil
 Estrogens.........................................................................Alora, Climara
 Triptans.....................................................Almotriptan, Naratriptan, etc




  
Ergot Alkaloids

N203
ATI (Unit 4)
Pain & Inflammation -
Expected Action: Proto: Ergotamine, ergotamine + caffeine

 Prevent inflammation and dilation of the intracranial blood vessels

Adverse Effects:
 GI discomfort  administer metoclopramide (Reglan)
 Ergotism (muscle pain, paresthesia)  stop medication
 Physical dependence
 Abortion
Contraindications/Precautions:
 Renal or liver dysfunction / sepsis / CAD / pregnancy
Interactions:
 Sumatriptan (Imitrex)  can lead to spastic rxn of blood vessels
Education:

Serotonin Receptor
Antagonists

N203
ATI (Unit 4)
Pain & Inflammation -
Expected Action: Proto: Sumatriptan (Imitrex), almotriptan (Axert)

 Prevent inflammation and dilation of the intracranial blood vessels

Adverse Effects:
 Chest symptoms (not dangerous, self-resolving)
 Coronary vasospasm/angina
 Teratogenic
Contraindications/Precautions:
 Pregnancy, hypertension, cardiac disease, CAD
Interactions:
 Triptans & Ergot Alkaloids  spastic reaction of blood vessels
 MAOIs  Concurrent use leads to MAOI toxicity (space 2 weeks apart)
Education:

Beta-Blockers

N203
ATI (Unit 4)
Pain & Inflammation -
Expected Action: Proto: Metoprolol, atenolol

 Prevent inflammation and dilation of the intracranial blood vessels

Adverse Effects:
 Tiredness, fatigue  Depression
 Asthma exacerbation 
Contraindications/Precautions:

Interactions:

Education:

Anticonvulsants

N203
ATI (Unit 4)
Pain & Inflammation -
Expected Action: Proto: Divalproex (Depakote)

 Prevent inflammation and dilation of the intracranial blood vessels

Adverse Effects:
 Neural tube defects
Contraindications/Precautions:

Interactions:

Education:

TCAs

N203
ATI (Unit 4)
Pain & Inflammation -
Expected Action: Proto: Amitriptyline (Elavil)

 Prevent inflammation and dilation of the intracranial blood vessels

Adverse Effects:
 Anticholinergic effects: dry mouth, constipation, urinary retention, tachycardia
Contraindications/Precautions:

Interactions:

Education:

Calcium Channel Blocker

N203
ATI (Unit 4)
Pain & Inflammation -
Expected Action: Proto: Verapamil

 Prevent inflammation and dilation of the intracranial blood vessels

Adverse Effects:
 Orthostatic hypotension
 Constipation
Contraindications/Precautions:

Interactions:

Education:

Medications for Rheumatoid
Arthritis
(Medication List)

N203
ATI (Unit 4)
Pain & Inflammation -
 DMARDs
 Cytotoxic medications.................................methotrexate (Rheumatrex)
 Gold salts.......................................................................aurothioglucose
 Antimalarial agents..............................hydroxychloroquine (Plaquenil)
 Sulfasalazine..........................................................................Azulfidine
 Biologic Response Modifiers...................................etanercept (Enbrel)
 .............................................................................................................
infliximab (Remicade)
 Penicillamine.............................................................Cuprimine, Depen
Others
 Glucocorticoids......................................................................prednisone
 Immunosuppressants..........................................................Cyclosporine
 NSAIDs....................................................................................naproxen
 .............................................................................................................
celecoxib
Rheumatoid Arthritis Meds
(Adverse Effects)

N203
ATI (Unit 4)
Pain & Inflammation -
  Hepatic fibrosis / Marrow suppression / GI ulceration / fetal
 Cytotoxics:
death or abnormality

 Toxicity, renal toxicity, blood dyscrasias, hepatitis, GI

 Gold salts:
discomfort

 Antimalarials:  Retinal damage

 Sulfasalazine:  GI discomfort / hepatic dysfunction / marrow suppression

 Bio Response Modifiers:  Injection-site irritation

 Penicillamine:  Marrow suppression

 Glucocorticoids:  Osteoporosis (vit D, Ca2+, bisphosphonate)
 Adrenal suppression  GI discomfort