Pain and Inflammation Management Agents Flashcards
Phases of Inflammation
Vascular phase
Delayed phase
a reaction to tissue injury caused by the release of chemical mediators that trigger both a vascular response and the migration of fluid and cells to the injured site
Inflammation
occurs 10-15 minutes after an injury
Vascular phase
vasodilation and increased capillary permeability 🡪 fluid shift to the injured site
Vascular phase
leukocytes infiltrate the inflamed tissue
Delayed phase
Chemical Mediators
Histamine
Kinin
Prostaglandin
first mediator
Histamine
causes dilation of the arterioles and increases capillary permeability 🡪 fluids shift to the injured area
Histamine
-increase capillary permeability and the sensation to pain
Kinins
increase in vasodilation, capillary permeability, pain, and fever
Prostaglandins
Antiinflammatory Agents aka
Prostaglandin Inhibitors
Relieve pain, reduce elevated body temperature, and inhibit platelet aggregation
Antiinflammatory Agents
Oldest anti-inflammatory drug
ASPIRIN
First used as analgesic and antipyretic
ASPIRIN
Aspirin and aspirin-like drugs that inhibit the COX enzyme
NONSTEROIDAL ANTIINFLAMMATORY DRUGS
Not suggested for use in alleviating mild headaches and mildly elevated temperature
NONSTEROIDAL ANTIINFLAMMATORY DRUGS
More appropriate for reducing swelling, pain, and stiffness in joints
NONSTEROIDAL ANTIINFLAMMATORY DRUGS
only OTC NSAIDs
Ibuprofen and naproxen
1st generation
- Salicylates
- Para-chlorobenzoic acid derivatives/ indoles
- Phenylacetic acids
- Propionic acid derivatives
- Fenamates
- Oxicams
Aspirin aka
acetylsalicylic acid (ASA)
Also considered as an antiplatelet drug for patients with cardiac or cerebrovascular disorders
Aspirin
a rare disorder that typically occurs after a viral illness that results in brain and liver damage.
Reye’s Syndrome
The proposed mechanism for aspirin contributing to the development of Reye’s syndrome is related to __________________________ that can be caused by salicylates, which may be intensified during viral illness by endotoxins and cytokines
mitochondrial damage
- used for rheumatoid arthritis, gouty arthritis an osteoarthritis
- potent prostaglandin inhibitor
- 90% protein-bound
- very irritating to the stomach, should be taken with food
Indomethacin
Similar to the analgesic and anti-inflammatory effects of aspirin, but minimal to no antipyretic effects
Diclofenac
first injectable NSAID
Ketorolac
used acute and chronic arthritis
Meclofenamate sodium and Mefenamic acid
- for long-term arthritis condition (RA and OA)
- lower incidence of ulceration and gastric distress
Piroxicam
- Prototype drug
- DOC for patients with severe arthritic conditions who need high doses of anti-inflammatory drug
Celecoxib
CORTICOSTEROIDS
Prednisone, prednisolone, dexamethasone
Controls inflammation by suppressing or preventing many of the components of the inflammatory process at the injured site
CORTICOSTEROIDS
- DOC when NSAIDs do not control immune-mediated arthritic disease sufficiently, however more toxic *
- Immunosuppressive agents, immunomodulators, antimalarials
DISEASE-MODIFYING ANTIRHEUMATIC DRUGS (DMARDs)
Immunosuppressive Agents
Azathioprine, Cyclophosphamide, Methotrexate
- used to treat refractory rheumatoid arthritis
- primarily used to suppress cancer growth and proliferation
- might be used to suppress the inflammatory process of rheumatoid arthritis when other treatments fail
Immunosuppressive Agents
Azathioprine, Cyclophosphamide, Methotrexate
are proinflammatory cytokines that contribute to synovial inflammation and joint destruction
IL-1 and TNF (Interleukin receptor (IL-1) agonists and Tumor necrosis factor(TNF))
- Treat moderate to severe rheumatoid arthritis by disrupting the inflammatory process and delaying disease progression
- Interleukin receptor (IL-1) agonists and Tumor necrosis factor(TNF) blockers
Immunomodulators
IL-1 receptor antagonist
Anakinra
Blocks TNF from attaching to TNF receptors on synovial cell surfaces
Infliximab
inflammatory condition that attacks joints, tendons, and other tissues
Gout
Gout aka
gouty arthritis
common site of Gout
Joint of the big toe
Uric acid metabolism disorder and a defect in purine metabolism resulting in increase in urates and accumulation of uric acid or an ineffective clearance of uric acid by the kidneys
Gout
May appear as bumps, or tophi, in the subcutaneous tissue of earlobes, elbows, hands, and base of large toe
Gout
first drug used to treat gout, 1936
Colchicine
- Inhibits the migration of leukocytes to the inflamed site
- Effective in alleviating acute symptoms of gout
- Does not inhibit uric acid synthesis and does not promote uric acid excretion
- Taken with food
Colchicine
Xanthine oxidase inhibitor
Allopurinol, Febuxostat
the level of stimulus needed to create a painful sensation
Pain threshold
Amount of pain a person can endure without having it interfere with normal functioning
Pain tolerance
Less potent that opioid analgesics
NONOPIOID ANALGESICS
Effective for dull, throbbing pain of headaches, dysmenorrhea, inflammation, minor abrasions, muscular aches, and pain, and mild to moderate arthritis
NONOPIOID ANALGESICS
- Nonprescription drug for the relief of pain, discomfort, and fever in infants, children, adults, and older adults
- Analgesic and antipyretic
- Does not have anti-inflammatory properties
- Little to no gastric distress and does not interfere with platelet aggregation
- Administered every 4hours as needed; max 4g/day
Acetaminophen (Paracetamol)
- Prototype
- An extraction from opium
- Effective against acute pain resulting from acute MI, cancer, and dyspnea from pulmonary edema
- May be used as a preoperative medication
Morphine
- One of the first synthetic opioids
- Schedule II drug
- Shorter duration of action than morphine
- Primarily effective in GI procedures
- No antitussive property; less constipation and urinary retention
- Preferred to morphine in pregnancy
Meperidine (Demerol)
- Semisynthetic opioid
- 6x more potent than morphine; fewer hypnotic effects and less GI distress
- Faster onset and shorter duration of action than morphine
Hydromorphone (Dilaudid)
Self-administered pain relief as needed
Patient-Controlled Analgesia
Provides a continuous around-the-clock pain control that is helpful to patients who suffer from chronic pain
Transdermal Opioid Analgesics
Postoperative pain will decrease overtime 🡪
downtitration
Cancer-related pain has continual increase in pain 🡪
uptitration
Developed for other purposes and later found to be effective for pain relief in neuropathy
ADJUVANT THERAPY
nonopioids with or without an adjuvant medication
Mild Pain
nonopioids and mild opioids with or without adjuvant medication
Moderate Pain
stronger opioid at higher drug dosage levels with our without an adjuvant medication
Severe Pain
- Act on the peripheral nerves and CNS by inhibiting neuronal firing
- Used for neuropathic pain and prevention of migraine headaches
Anticonvulsants (gabapentin)
- Prevent reuptake of serotonin and norepinephrine in the cells
- Effective in treating peripheral neuropathy
Tricyclic antidepressants (amitriptyline)
Reduce nociceptive stimuli
Corticosteroids
Blocks sodium channels to reduce pain
Antidysrhythmics (mexiletine)
Interrupts the transmission of pain signals to the brain
Local anesthetics (lidocaine)
first triptan drug; short duration of action
Sumatriptan