Analgesics and Anti-inflammatory

Ibuprofen (Motrin/Advil/Caldador)

NSAID – Reversible Non-Selective Cyclooxygenase

• Inhibition of

  ·         COX-1: but does not lead to protection against thrombotic events)

  COX-2: leads to reduction of inflammation, pain and fever

• For 

  • pain, fever, inflammation

Ketorolac (Toradol)

NSAID – Reversible Non-Selective Cyclooxygenase Inhibitor

• Inhibition of

  ·         COX-1: but does not lead to protection against thrombotic events)

  COX-2: leads to reduction of inflammation, pain and fever

• For

  • acute and severe pain

  • similar to morphine

Celecoxib (Celebrex)

2^nd Generation Selective Cyclooxygenase Inhibitor

• inhibition of COX-2 à

  • ↓ inflammation & pain

Acetaminophen (Tylenol/Ofirmev)

CNS COX inhibitor to reduce fever and pain

• MOA

  • Reduces prostaglandin synthesis in the CNS

Glucocorticoids

·         High doses: suppressing inflammation

MOA

• ·         binding to intracellular glucocorticoid receptors (GRs)

FOR - RA

Sulfasalazine (Azulfidine)

Non-Biologic (Conventional) DMARD

• ·         5-aminosalicyclic acid to modulate local chemical mediators of inflammatory response, including leukotrienes

• For 

  • RA

Etanercept (Enbrel)

·         Biologic DMARD

·         Tumor Necrolysis Factor (TNF) antagonist

MOA

• ·         Inhibits inflammation through neutralization of tumor necrosis factor (TNF) by preventing TNF from interacting with natural receptors in synovium

For

• Moderate to severely active RA

Rituximab (Rituxan)

·         Biologic DMARD

·         B-Lymphocyte-depleting agent

• MOA

  • Monoclonal antibody that targets CD20 proteins to deplete positive B cells via cell lysis and apoptosis

• FOR

Abatacept (Orencia)

• Class

  • ·         Biologic DMARD

    ·         T-Cell activation inhibitor

• MOA

  • ·         Selectively binds with receptors on antigen-presenting cells to prevent T cell activation to:

    o    Reduce T-cell proliferation

    o    Reduce production of

    §  interferon gamma

    §  interleukins

    TNF

• FOR

  • moderately to severely active RA in adults

Colchicine (Colcrys)

• MOA

  • Inhibits leukocyte infiltration by disrupting microtubules required for cellular motility and cell division

• FOR

  • ·         Acute gout attack

    ·         Prophylaxis of future gout attacks

Allopurinol (Zyloprim)

Xanthine Oxidase Inhibitor

• For 

  • ·         Chronic management of gout

    ·         Nephrolithiasis

• MOA

  • Inhibits oxidase enzyme that decrease uric acid production

Probenecid

Uricosuric

• For gout prevention

• MOA

  • ·         Acts on renal tubules to inhibit reabsorption of uric acid

    o    helps ↑ excretion of uric acid by the kidneys and reduce hyperuricemia

Pegloticase (Krystexxa)

Recombinant Uric Acid Oxidase

• if patients are not responsive to PO urate lowering therapies gout

• MOA

  • ·         Converts uric acid to allantoin, which is water soluble & readily excreted by the kidneys

Sumatriptan (Imitrex)

Serotonin Receptor Agonist

• For

  • acute (mod-severe migraines and cluster)

• MOA

  • ·         Binds to receptors on intracranial blood vessels causes

    o    Vasoconstriction

    Diminishes perivascular inflammation

Ergotamine (Ergomar)

Ergot alkaloids

MOA

• unknown but ·         Suppresses release of CGRP to block inflammation; selectively binds & activates serotonin receptors located on intracranial blood vessels

  o    à vasoconstriction & ↓ blood flow in cerebral arteries

For - ·         2^nd line for migraine attacks in patients who have not responded to triptans

Baclofen (Lioresal)

Centrally Acting Muscle Relaxer for Muscle Spasticity

• MOA·         Acts within spinal cord to suppress hyperactive reflexes involved in regulation of muscle movement

  may mimic GABA on spinal neurons

Cyclobenzaprine (Flexeril, Fexmid)

Centrally Acting Skeletal Muscle Relaxer for Muscle Spasm

• MOA

  • Acts primarily within brainstem to reduce tonic somatic motor activity

• For 

  • localized muscle spasm(s), such as musculoskeletal injury

Morphine

Pure Agonist Opioid Analgesic

• MOA

  • ·         Acts primarily on mu receptors to mimic endogenous opioid peptide actions

    Mu and Kappa receptors

Fentanyl

Pure Agonist Opioid Analgesic

• MOA

  • Acts primarily on mu and kappa receptors to mimic endogenous opioid peptide actions

Codeine

PURE Opioid Agonist

• MOA

  • ·         Acts primarily on Mu and Kappa receptors to mimic endogenous opioid peptide actions

Naloxone (Narcan)

Competitive Antagonist

• MOA

  • Antagonist at opioid receptors that blocks opioid action

• For 

  • Opioid overdose (respiratory depression, etc.)

Tramadol (Ultram)

Opioid/Non-opioid

• Pain relief achieved through

  •  weak mu agonist activity

  • block of NE and serotonin reuptake

treatment of moderate to severe pain

Methadone

Long-Acting Pure Agonist

• MOA

  • ·         Acts primarily on mu receptors to mimic endogenous opioid peptide actions

• FOR

  • ·         Pain relief

    ·         Maintenance treatment for opioid use disorder

    Short-term supervision of opioid withdrawal

Buprenorphine/Naloxone (Suboxone)

Agonist-Antagonist Opioid Analgesic

• MOA

  • ·         both agonist & antagonist actions at mu receptors

    and

    antagonist action at kappa receptors

• FOR

  • Acute and chronic pain relief

  • Opioid use disorder & opioid withdrawal