ATI Pharmacology Medications for Pain & Inflammation

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Pain and 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

• Aspirin • Ketorolac (Toradol)
• Celecoxib (Celebrex) • Valdecoxib (Bextra)
• Ibuprofen • Indomethacin
• Naproxen •

NSAIDs General Information

Proto: aspirin, ibuprofen, ketorolac, celecoxib
Expected action: Cyclooxygenase inhibition - COX 2 decreases inflammation, COX 1 which leads to decreased platelet aggregation
Therapeutic Uses:
• Inflammation suppression / analgesia / decreased 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 decreased risk of ulceration)
• Renal dysfunction
• Reye syndrome (in kids with viral illnesses) • Salicylism (tinnitus, resp. alkalosis, dizziness)
Contraindications/Precautions:
• Peptic ulcers / bleeding disorders / hypersensitivity / pregnancy / kids ĉ viral inf.
Interactions: • Glucocorticoids (increased gastric bleeding) - use antiulcer prophylactic like misoprostol (Cytotec) to prevent
• Warfarin (increased bleeding)
• EtOH ( increased bleeding) • Ibuprofen (decreased antiplatelet effects of low-dose aspirin)
• Give with food or milk to reduce GI discomfort.
• If can't tolerate 1st generation, give 2nd generation (celecoxib)

Ketorolac Toradol - 1st Generation NSAID

Expected Action: decreased 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 (increased bleeding)
Education : Usually started parenteral and then transition to oral dose

Acetaminophan

Expected Action: Slows production of prostaglandins
Therapeutic Uses: Analgesic and antipyretic
Adverse Effects: • Max 4 g daily
• Acute liver toxicity • Antidote: acetylcysteine (Mucomyst)
Interactions : • EtOH leads to increased risk to liver / Warfarin leads to increased levels of warfarin

Opoid Agonist Information

Therapeutic Uses:
• Moderate to severe pain / Sedation / decreased bowel motility / Cough suppression
Adverse Effects: • Respiratory depression • Sedation
• 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 equipment available.
• Infuse IV slowly over 4-5 minutes

Opoid Agonist drugs

morphine, fentanyl, meperidine, methadone, codeine, oxycodone

Opoid Antagonist information

Prototype: naloxone (Narcan), naltrexone, nalmefene
Expected Action: 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
Education:
• Naloxone has extensive first-pass modification
• Observe for w/d symptoms or abrupt onset of pain

Adjuvant Pain Meds

• 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 Pain Meds information

Expected Action: • Enhance opioid effects thereby permitting lower opioid doses
• Alleviate other symptoms that aggravate pain • Treat neuropathic pain
Adverse Effects:
• TCAs (neuropathic pain) leads to Orthostatic hypotension, sedation, anticholinergic effects
• Anticonvulsants (neuropathic pain) leads to Bone marrow suppression
• CNS stimulants leads to Weight loss, insomnia
• Antihistamines leads to Sedation
• Glucocorticoids (increased ICP, nerve compression) leads to Adrenal insufficiency, Glucose intolerance, Hypokalemia, Osteoporosis, GI Ulcers
• Bisphosphonate (CA bone pain) leads to Flu-like symptoms and Injection site irritation

Antigout Medications

Prototype: Colchicine, indomethacin, allopurinol, probenecid
• Colchicine/Indomethacin:
Expected Action: 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: decreased η probenecid
• Warfarin: decreased warfarin metabolism in liver  bleeding risk
Education: Avoid EtOH, purines. Adequate hydration.

Migraine Medications

• 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 Medications

Expected: 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

Serotonin Receptor Antagonists

Prototype: Sumatriptan (Imitrex), almotriptan (Axert)
Expected Action: 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 leads to spastic reaction of blood vessels
• MAOIs leads to Concurrent use leads to MAOI toxicity (space 2 weeks apart)

Beta Blockers (Atenolol, Metapropolol)

Expected Action: Prevent inflammation and dilation of the intracranial blood vessels
Adverse Effects:
• Tiredness, fatigue
• Asthma exacerbation
* Depression

Anticonvulsants

Prototype: Divalproex (Depakote)
Expected Action: Prevent inflammation and dilation of the intracranial blood vessels
Adverse Effects: Neural tube defects

TCAs

Prototype: Amitriptyline (Elavil)
Expected Action: Prevent inflammation and dilation of the intracranial blood vessels
AE: Anticholinergic effects: dry mouth, constipation, urinary retention, tachycardia

Calcium Channel Blockers

Prototype: Verapamil
Expected Action: Prevent inflammation and dilation of the intracranial blood vessels
Adverse Effects:
• Orthostatic hypotension
• Constipation

Medications for Rheumatoid Arthritis

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 Information

• Cytotoxics: --> Hepatic fibrosis / Marrow suppression / GI ulceration / fetal death or abnormality
• Gold salts: --> Toxicity, renal toxicity, blood dyscrasias, hepatitis, GI 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

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