Chapter 20 Flashcards
analgesia
inhibition of the perception of pain
anaphylaxis
condition in which the body develops a severe allergic response; this is a medical emergency
anemia
condition in which the number of red blood cells or the amount of hemoglobin inside the red blood cells is less than normal
anti-inflammatory
minimizing or stopping the response to tissue injury by reducing the pain, localized swelling and chemical substances released at the site of injury
- known as NSAIDs (nonsteroidal anti-inflammatory drugs)
- Decrease inflammation by inhibiting prostaglandin synthesis
- Not structurally related to cortisone
- NSAIDs selectively inhibit the cyclooxygenase enzymes further along the pathway, while cortisone inhibit the formation of arachidonic acid
- Groups
- Original NSAIDs salicylates & aspirin
- Non-NSAIDs acetaminophen
- Synthetic NSAIDs ibuprofen and celecoxib
- All NSAIDs are nonopioid analgesics.
- Relieve mild to moderate pain associated with inflammation
- Do not affect consciousness or mental function
- Not related to morphine and do not produce tolerance or physical dependency
- Not effective against severe, sharp pain
- Produce analgesia through a central and a peripheral mechanism of action
antipyresis
reducing an elevated body temperature
arthralgia
joint pain
arthritis
inflammation of the joints
cyclooxygenase(COX)
- cyclooxygenase, a family of enzymes that produce prostaglandins from arachidonic acid
- Known as prostaglandin synthetase, but COX is the newer terminology
- Subtypes - COX-1 and COX-2
- COX-1 – believed to always be available in the cells
- COX-2 – manufactured in activated macrophages in response to injury or damage to local tissues
dysmenorrhea
difficult or painful
-mensuration
erythema
abnormal redness of the skin, caused by capillary congestion
inflammation
condition in which tissues have been damaged, characterized by swelling, pain, heat and sometimes redness
intoxicaiton
state in which a substance has accumulated to potentially harmful levels in the body
ischemia
reduction in blood supply and oxygen to localize area of the body or tissue
lavage
washing with fluids or flushing of a cavity such as the stomach
leukopenia
condition in which the total number of white blood cells circulating in the blood is less than normal
megaloblastic anemia
condition for which there is a large, immature form of the red blood cell, which does not function as efficiently as the mature form
myalgia
pain associated with muscle injury
petechia
small area of the skin or mucous membranes that is discolored because of localized hemorrhages
phagocyte
circulating cell ( such as a leukocyte) that ingests waste products or bacteria in order to remove them from the body
prophylaxis
treatment of drug given to prevent a condition or disease
prostalglandins (PG)
- Mediators of inflammatory response
- substance naturally found in certain tissues of the body; can stimulate urterine and intestinal muscle contractions and may cause pain by stimulating nerve endings; can elevate body tempurature (In conjunction with histamine and bradykinin)
- Formed in the cell membranes of organs
- Involved in erythema, edema, and pain
rhemumatic fever
condition in which pain and inflammation of the joints or muscles are accompanied by evaluated body temperature usually a complication of untreated strep throat
salicylism
condition in which toxic doses of salicylates are ingested, resulting in nausea, tinnitus, and delirium
selectiv COX-2 inhibitors
drugs that only interact with one of the enzymes in the cyclooxygenase family
What is the process of inflammation?
Substances are released.
-Produce vasodilation and increase permeability in the capillary walls
Pain receptors are stimulated.
Phagocytes migrate to destroy harmful substances.
Results in the cardinal signs of inflammation:
-redness, swelling, warmth, pain, and loss of function
inflammation is good until…
It becomes exaggerated or prolonged
Will result in further tissue damage
It becomes the disease itself
Clinical indications of Anti-inflammatory Analgesics
- Headache, dental extraction, soft tissue injury, sunburn, musculoskeletal, joint overexertion, and strain
- Chronic treatment of dysmenorrhea
-Tendinitis, bursitis, osteoarthritis, and rheumatoid arthritis
Aspirin is used in the treatment of osteoarthritis, spondylitis, and gout
Actions of Nonopioid anti-inflammatory analgesics
Salicyclates and NSAIDs
-Salicylates include aspirin, salicylic acid, and methyl salicylate.
- Produce antipyresis
- Affect the hypothalamic centers in the brain to reduce elevated body temperature
- Mechanism of the central action - Block prostaglandin stimulation of the central nervous system (CNS)
- Produce Analgesia
- Inhibit the synthesis of prostaglandins and prevent bradykinin from stimulating pain receptors
- Inhibit pain centrally and peripherally
Anti-inflammatory Action
- Inhibit a primary pathway in prostaglandin synthesis
- Drugs vary in in their ability to reduce all types of inflammation.
Produce gastrointestinal effects
- Blockage of COX-1 results in gastric ulcers and distress.
- Gastrointestinal (GI) irritation and CNS stimulation cause vomiting.
Aspirin is a useful anticoagulant.
-Inhibit the aggregation of platelets necessary for blood clot formation
Cardiovascular benefit is associated with aspirin.
Reduces risk of death and re-infarction post myocardial infarction
Prevents heart disease
NSAIDs like ibuprofen and celecoxib act as antagonists.
Prevents the formation of thromboemboli
Drug preparations of aspirin and NSAIDs
Aspirin and salicylates are available in oral formulations.
Other NSAIDs are primarily for oral administration.
Ibuprofen, indomethacin, and ketorolac tromethamine can be administered parenterally
Drug disposition
Salicylates and NSAIDs are rapidly absorbed from the stomach and small intestine
Possess a 4- to 6-hour duration of action
Metabolized in the liver, excreted into urine
Clinical Indications of NSAIDs
Fever reduction, mild to moderate pain, and inflammation contributing to headache and to muscle and joint pain
Clinical Indications of Aspirin
Treatment and prevention of cardiovascular disease and management of adenomatous polyps, and colorectal cancer
Clinical Indications of Salicylates
Management of ulcerative colitis
Acetaminophen
Analgesic and antipyretic
- Does NOT have anti-inflammatory properties
- Directly acts on heat regulation centers in the hypothalamus to reduce body temperature
- Relieves headaches by inhibiting prostaglandin synthetase within the CNS
- Does not produce GI irritation or ulceration
Clinical indications
- Indicated for patients allergic to aspirin
- Fever, headache, minor musculoskeletal pain, and discomfort associated with the common cold and flu
- Recommended for patients who experience GI upset from aspirin or NSAIDs
Available as OTC products in a variety of formulations
Toxicity may develop from chronic use
-People that consume more than 3 alcoholic beverages daily have potential hepatic sensitivity that becomes compromised with increased exposure to acetaminophen
Adverse effects of hepatotoxity
-Nausea and vomiting, hepatic damage, acidosis, respiratory complications, and death
Treatment for overdose
- Gastric aspiration and lavage
- Maintenance of fluid balance
- Activated charcoal
- Liver transplantation
- N-acetylcysteine
Adverse effects and Boxed warnings of NSAIDs
Common effects
- Vertigo, vomiting, mental confusion, and headaches due to CNS stimulation
- NSAIDs and aspirin - Nausea, GI distress, and ulceration
Gastrointestinal effects of NSAIDs
- Mucosal irritation
- Ulceration, GI bleeding, and perforation of the stomach or intestines
Boxed warning
-Every OTC NSAID product includes a bolded warning, advising about the potential risks
Cardiovascular effects
- Boxed warning
- NSAIDs can cause fatal cardiovascular thrombotic events, myocardial infarction, and stroke.
NSAIDs and COX-2 inhibitor drugs
-Sodium and water retention
Hypersensitivity and allergic effects of NSAIDs
- Mild rashes, fever, hepatic damage, respiratory distress
- Serious side effects of NSAIDs - Exfoliative dermatitis, and Steven’s Johnson syndrome
- Acetaminophen - Reddening of the skin, blisters, and detachment of the upper surfaces of the skin
Hematological effects of NSAIDs
Megaloblastic anemia – larger than normal RBC that are structurally abnormal and immature
iron deficiency anemia – due to blood loss through hemorrhage
Bone marrow suppression – leads to blood disorders
Idiopathic hemolytic anemia – RBC are destroyed faster than they are produced
Acute toxicity and overdose
Acetaminophen
- Causes hepatic damage, acidosis, and respiratory complications
- Antidote - N-acetylcysteine
Salicylates and NSAIDs
- Respiratory depression and acidosis
- Dehydration, cardiovascular depression, vasodilation, and hypotension
- Treatment for aspirin poisoning - Administration of sodium bicarbonate and infusion of fluid and electrolytes
Chronic toxicity
Nausea, vomiting, and salicylism
-Salicylism – series of symptoms that include:
-nausea, ringing in the ears, HA, delirium, and
hyperventilation
-Hyperglycemia
-Signs of overdose in elderly patients
-Ringing in the ears (tinnitus), gastric upset, and GI bleeding
Salicylates Contraindications
Produce Reye’s syndrome
When aspirin is given to children (ages 1-4 & 10-14) as treatment to a viral illness, symptoms include N/V, HA, excitability, delirium, and combativeness, which may progress to coma and death
Aspirin and ibuprofen Contraindications
Not be used during pregnancy
Can cause premature closure of vessels in the baby’s heart and aspirin may induce bleeding
nonaspirin NSAIDs Contraindications
Contraindicated for the treatment of perioperative pain
Gout
Caused by the deposition of uric acid in joint fluid and soft tissue
-May occur due to overproduction or uric acid and/or an inefficient excretion of uric acid
Characteristics
- Acute gout - Edema, redness, and severe pain
- Chronic gout - Deposition of uric acid in soft tissue, causing tophi
- Hypouricemic agents
- Allopurinol – inhibits the enzyme that is necessary to make uric acid
- Febuxostat - used for chronic management of hyperuricemia in gout patients
Uricosuric agents
-Probenecid - used for the chronic management of gout; inhibits renal reabsorption by of uric acid so it passes through the urine
Modified Enzyme
-Pegloticase – converts uric acid to a water-soluble metabolite that can be excreted in the urine
Adverse effects
Colchicine
(Gout Medication)
Nausea, vomiting, diarrhea, abdominal cramps, and blood in the urine (hematuria)
Adverse effects
Allopurinol
(Gout Medication)
ever, rash, and leukopenia
Adverse effects
Febuxostat
(Gout Medication)
Dizziness, rash, nausea, and temporary elevation in liver enzymes
Adverse effects
Probenecid
(Gout Medication)
GI disturbances, including nausea and vomiting, arthralgias, skin rash, and fever
Adverse effects
Pegloticase
(Gout Medication)
Anaphylaxis, infusion reactions, nausea, vomiting, and constipation
Clinical Indications and preffered treatment for Gout
Lifelong process including diet adjustment and medication
Colchicine, specific NSAIDs, and sodium thiosalicylate
-Used in the treatment of acute gout attacks, relief of pain, and interruption of the inflammatory process
Probenecid
- Used to treat hyperuricemia associated with gout and gouty arthritis
- Used as an adjunct to antibiotic therapy
Allopurinol
- Manages primary and secondary gout, acute gout attacks, tophi, nephropathy, joint destruction, or uric acid stones
- Reduces serum and urinary uric acid resulting from the treatment of malignancies, leukemia, and lymphoma
