Pharma- Non Opioid Analgesics

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Characteristics of non opioid class

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3 A's-

analgesia

antipyresis

antiinflammatory

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Cardinal signs of inflammation

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redness

edema

warmth

pain

loss of function

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Prostaglandins

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Mediators of inflammatory response

Parent of all prostaglandins- arachidonic acid, a fatty acid

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formation of arachidonic acid inhibited by what?

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Steroidal antiinflammatory substances (cortisol, hydrocortisone, prednisone)

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cyclooxygenase (COX) enzymes inhibited by?

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NSAIDs

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COX

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cyclooxygenase, family of enzymes that produce prostaglandins

2 types identified-

COX-1

COX-2

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NSAIDs

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ease symptoms associated w/inflammation, inhibit prostaglandin synthesis in many different tissues in inflammation pathway

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NSAIDs indications

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mild to moderate pain where opioids not indicated or warranted

local inflammatory responses including

headache, dental extraction

soft tissue injury, sunburn

musculoskeletal, joint overexertion and strain,

dysmenorrhea, controlling signs/symptoms of osteo and RA

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NSAID examples

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Sulindac (Clinoril)

Tolmetin (Tolectin)

meclofenamic acid (Ponstel)

Meclofenamate (Meclomen)

piroxicam (Feldene)

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RA

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degenerative joint disease, associated w/inflammation of joint cartilage

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DOC for treatment osteoarthritis, spondylitis (inflammation of vertabrae), gout

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aspirin (can be)

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4 ways non opioid analgesics differ from opioid analgesics

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1. not chemically, structurally related to morphine

2. not effective against sharp (visceral) pain

3. produce analgesia through both CNS, peripheral site of injury mechanism of action

4. No tolerance, physical dependency w/chronic use

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3 groups non opioid analgesics

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1. salicylates and aspirin (original NSAIDs)

2. acetaminophen

3. synthetic NSAIDs such as ibuprofen, indomethacin, ketoprofen

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largest class of non opioid analgesics

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NSAIDs

3 groups:

salicylates

traditional NSAIDs

COX-2 selective inhibitors

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Salicylates natural product of?

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willow tree bark

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Salicylates taken today?

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sodium salicylate

aspirin (acetylsalicylic acid)

salicylamide

methyl salicylate- only salicylate poisonous when taken orally. taken topically (creams)

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non opioid analgesics mech of action

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analgesia and antipyresis- selectively affecting hypothalmic centers, reducing elevated but not affecting normal body temp. Increased vasodilation and sweating, promoting greater loss excess heat from body

Synthesis of prostaglandins inhibited, bradykinins prevented from stimulating pain receptors

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antiinflammatory action

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salicylates excellent antiinflammatory drugs

prohibit primary pathway in prostaglandin synthesis, inhibit COX-1 and COX-2

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GI effect of COX-1 blockage

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In stomach, prostaglandins integral part of cytoprotective mechanisms.

When COX-1 blocked, protective environment altered, leading to gastric distress, ulcers

vomiting can result

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Anticoagulent, CV benefit

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aspirin, salicylamide irreversibly inhibit platelet aggregation. Low aspirin doses increase bleeding time. Aspirin reduces risk of death, reinfarction following MI. aspirin therapy reduces 1st stroke risk in women (not men).

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salicylates metabolism and excretion

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salicylates readily bind to plasma proteins (80-90%), distributed to various tissues, esp. in CNS, joint fluids, kidneys

Plasma levels of salicylates affected by PH of urine

Acidic urine- more reabsorbed

Alkaline urine- more excreted

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salicylism

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condition in which large amounts salicylates ingested, resulting in nausea, tinnitus, delirium

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hypersensitivity to aspirin produces?

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skin rashes

laryngeal edema

asthma

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aspirin resistance

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non aspirin NSAIDs like ibuprofen, celecoxib w/chronic low-dose aspirin therapy reduces (antagonizes) beneficial CV effects of aspirin.

NSAIDs used 60+ days per year w/daily aspirin also contributes to aspirin resistance.

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Salicylate poisoning

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involves respiratory depression, acidosis. Renal function impaired, other acids build up in body

Acute lethal dose- 10-30 g for adults, 4 g children.

Treatment- admin of sodium bicarbonate to correct acidosis and increase excretion (increase urine PH). Fluids, electrolytes infused to correct acid-base balance. Treatment no always successful. Coma and death may result from dehydration, extensive CNS depression, renal failure

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Aspirin cornerstone of treatment for what?

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CV disease

Low dose 50-100 mg daily reduce risk of MI, TIAs stroke. Long term therapy reduces development of adenomayous polyps, colorectal cancer

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Salicylates related to or metabolized to 5-ASA (acetylsalicylic acid) used for management of what?

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ulcerative colitis

ex:

Balsalazide (Colozal)

mesalamine (Asacol, Pentasa, Rowasa)

olsalazine

sulfadiazine

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Reye's syndrome

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condition caused by aspirin use in children, including teenagers who have active viral infections or chickenpox

Symptoms-

vomiting, belligerence

delirium, coma

Death

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Acetaminophen

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Datril, Panadol, Tylenol

produces analgesia for relief of minor headache, antipyresis but has no proven antiinflammatory activity and doesnt supress stomach acid secretions. May act on COX-3, found in brain.

Does not produce GI irritation, ulceation in therapeutic doses

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Acetaminophen toxicity

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Chronic use of large doses (>4 g/day in adults, 75 mg/kg/day in children w/febrile ilnesses)

acute OD from single ingestion (>200 mg/km children, 6 g adults)

1st symptoms are flu-like, often ignored

hepatic damage may result 36 hours after toxic dose. Death is possible.

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Treatment for acetaminophen poisoning

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gastric aspiration/lavage

activated charcoal, increases absorption if administered within hours of ingested OD

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Approved antidote for Acetaminophen OD

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N-acetylcysteine (NAC, Acetadote)

given PO, foul odor, may be given IV

Oral dose repeated over 72 hours; IV completes effect in 1/2 the time

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Acetaminophen drug interaction with?

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Warfarin- increases anticoagulent effect

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selective COX-2 inhibitors

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drugs that interact with only 1 of the enzymes in cyclooxygenase family

celecoxib (Celebrex)

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NSAIDs available OTC

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ibuprofen (Advil)

naproxen (Aleve, Midol extended relief)

treatment for osteoarthritis

prescription needed for >300 mg ibuprofen, >250 mg naproxen

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NSAIDs available for parenteral admin

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ibuprofen (Neoprofen)

indomethacin (Indocin IV)

keterolac

Ibuprofen, indomethacin used for patent ductus arteriosis (closure of atrial opening) in infants

keterolac used for moderate/severe pain "at opioid level"

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NSAIDs adverse effects

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nausea, GI distress, ulceration

most serious complication of ulceration is massive hemorrhage leading to shock and death

vertigo, vomiting, mental confusion, headaches

megoblastic anemia

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Megoblastic anemia

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large immature RBCs, don't function as effectively as mature form

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Adverse effect more like in patients...

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receiving large doses in treatment of arthritis, especially RA

Bone marrow suppression possible

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Symptoms of NSAID OD

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tinnitus, gastric upset, GI bleeding (Black tarry stools)

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NSAIDs and COX-2 inhibitors promote...

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sodium and water retention

can result in peripheral edemaincrease stress on CV system in patients with HT, heart failure

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Celecoxib (Celebrex) contraindications

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patients w/history of sensitivity to sulfonamides

All selective COX-2 inhibitors associated w/exacerbating allergic reactions

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Special consideration NSAIDs

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BP should be monitored during therapy- ACE inhibitor effect on BP may be reduced for patients receiving certain anti-HT drugs

non-aspirin NSAIDs may increase risk of serious CV thrombotic events, MI, stroke, which can be fatal. Contraindicated treatment post-op pain (10-14 days) from coronary artery bypass graft (CABG) surgery

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NSAIDs adverse reactions GI tract

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serious reactions, including bleeding, ulceration, preforation of stomach, intestines, which can be fatal.

"severe stomach bleeding"

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Gout

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Inflammatory disease. Deposition uric acid in joint fluid (big toe, knees, elbows) soft tissue.

hyperuricemia- increased uric acid level in blood

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Drugs used to treat gout

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allopurinol

februxostat