objective 2.4 Flashcards
- Work together to provide support and movement for the body
- Skeletal system is composed of bones, cartilage, and joints. This system protects,
supports, and allows body movement, produces blood cells in the long bones,
and stores minerals
MSK system
Act to relieve pain associated with skeletal muscle spasms
muscle relaxants
Site of action: CNS
* Similar in structure and action to other CNS depressants
centrally acting muscle relaxants
- Act directly on skeletal muscle and decreases response to stimuli
- Closely resemble GABA
direct acting muscle relaxants
what are the AE of muscle relaxants?
Extension of effects on CNS and skeletal muscles
* Dizziness, Drowsiness, Lightheadedness, Euphoria, Fatigue, Confusion, Muscle
weakness, others
what are the common muscle relaxants?
- Baclofen (Lioresal®)
- Cyclobenzaprine (Flexeril®)
- Dantrolene sodium (Dantrene®)*
- Tizanidine hydrochloride
- Localized protective response stimulated by
injury to tissues, which serves to destroy,
dilute, or wall off (sequester) both the
injurious agent and the injured tissue - Pain, fever, loss of function, redness,
and swelling - Endogenous compounds, including
proteins of the complement system,
histamine, serotonin, bradykinin,
leukotrienes, and prostaglandins
inflammation
- A large and chemically diverse group of drugs that have:
- Analgesic activities
- Anti-inflammatory activities
- Antipyretic activities
- aspirin-platelet inhibition
NSAIDs
why might one use NSAIDs?
Relief of mild to moderate headache, myalgia, neuralgia, arthralgia, Relief of
postoperative pain, Relief of pain associated with arthritic disorders such as
rheumatoid arthritis, juvenile arthritis, ankylosing spondylitis, and
osteoarthritis, Treatment of gout and hyperuricemia
what is the MOA of NSAIDs?
- Inhibition of the leukotriene pathway, the prostaglandin pathway, or both
- Blocking the chemical activity of the enzyme COX
- COX-1 has a role in maintaining the gastrointestinal (GI) mucosa.
- COX-2 promotes synthesis of prostaglandins involved in the inflammatory process.
what are the contraindications of NSAIDs?
- Known drug allergy
- Conditions that place the patient at risk for bleeding
- Rhinitis, Vitamin K deficiency, Peptic ulcer disease
- Recommended that NSAIDs be stopped 1 week prior to surgery.
- Avoid NSAIDS after 32 weeks gestation.
what are the AE of NSAIDs?
- Heartburn to severe GI bleeding, Acute kidney injury, Noncardiogenic
pulmonary edema, Altered hemostasis (stopping of flow of blood),
Hepatotoxicity, Skin eruption, sensitivity reaction, Tinnitus, hearing
loss - GI: Dyspepsia, heartburn, epigastric distress, nausea, vomiting,
anorexia, abdominal pain - GI irritation and bleeding*
- Mucosal lesions* (erosions or ulcerations)
what are the interactions of NSAIDs?
Alcohol, Angiotension Converting Enzyme Inhibiors (ACEIs), Angiotension Receptor inhibitors
(ARBs), Anticoagulants, acetylsalicylic acid (ASA), Biphosphonates, Corticosteroids and other
ulcerogenic medications, Protein-bound drugs, Diuretics
what are the categories of NSAIDs?
- Salicylates (ie. Aspirin)
- Acetic Acid Derivatives (ie. Ketorolac (Toradol), diclofenac sodium
(voltaren) - Cox-2 Inhibitors (ie. Celebrex)
- Enolic Acid Derivatives (ie. Mobicox)
- Propionic Acid Derivatives (ie. Ibuprofen/Advil; Naproxen/ Aleve)
- Inhibits platelet aggregation
- Antithrombotic effect: used in the treatment of MI and other
thromboembolic disorder
acetylsalicylic acid
what are examples of salicylates?
- acetylsalicylic acid (aspirin) the most common
- Oral (tablets, capsules), topical cream (Aspercreme®), oral liquids, rectal
suppositories - aspirin–antacid combinations (Alka-Seltzer®)
- Enteric-coated aspirin (Praxis ASA EC®)
what is the MOA of aspirin?
- Irreversible inhibitor of COX-1 receptors within the platelets themselves
- Reduced formation of thromboxane A2, a substance that normally promotes
platelet aggregation (also known as antiplatelet activity) - Prolongs bleeding time
- Other NSAIDs lack these antiplatelet effects.
what are the uses of aspirin?
- Headache, neuralgia, myalgia, and arthralgia
- Pain syndromes resulting from inflammation: arthritis, pleurisy, and
pericarditis - Systemic lupus erythematosus: antirheumatic effects
- Antipyretic action
- Acute and potentially life-threatening condition involving progressive
neurological deficits that can lead to ICP, coma & liver damage. - Triggered by viral illnesses such as influenza, as well as by salicylate therapy itself
in the presence of a viral illness. - Survivors of this condition may or may not have permanent neurological damage.
reyes syndrome
- Analgesic, anti-inflammatory, antirheumatic, and antipyretic properties
- Uses: therapy for rheumatoid arthritis (RA), osteoarthritis (OA), acute bursitis
or tendonitis, ankylosing spondylitis, acute gouty arthritis - Oral and rectal routes
indomethacin
Some anti-inflammatory activity
* Used primarily for its powerful analgesic effects, which are comparable to
those of narcotic drugs such as morphine sulphate
* Indication: short-term use (up to 5 to 7 days) to manage moderate to severe
acute pain
* Adverse effects: kidney impairment, edema, GI pain, dyspepsia, and nausea
ketorolac tromethamine
- Most commonly used NSAID
- Uses: analgesic effects in the management of RA, OA, primary dysmenorrhea,
dental pain, musculoskeletal disorders; antipyretic actions - Doses over 2400mg/ day not recommended
ibuprofen
- Second most commonly used NSAID
- Somewhat better adverse effect profile than ibuprofen
- Fewer drug interactions with angiotensin-converting enzyme inhibitors given
for hypertension
naproxen
- First and only remaining COX-2 inhibitor
- Indicated for OA, RA, acute pain symptoms, ankylosing spondylitis, and
primary dysmenorrhea - Adverse effects include headache, sinus irritation, diarrhea, fatigue, dizziness,
lower-extremity edema, and hypertension - Little effect on platelet function
- Not to be used in patients with known sulpha allergy
celecoxib
Used to treat the pain of OA
* GI discomfort
* Drowsiness, headache, skin reactions
may increase insulin resistance
actions
glucosamine
Used to treat the pain of OA
GI discomfort (normally well tolerated)
Both herbs enhance the effects of warfarin
chondroitin
- OTC med used to decrease fever (antipyretic) and treat mild pain,
(analgesic) - Can be used in patients with gastric irritation with aspirin or NSAIDS
- Drug of choice for relief of minor pain in children
- No anti-inflammatory effect
- Antipyretic, effective for treating chronic pain both malignant and non
malignant, initial drug of choice for osteoarthritis - Fewer adverse effects than NSAIDS
- Linked to hepatotoxicity when dosage is increased
acetaminophen
what are the interactions of acetaminophen?
- Acetaminophen when used with the following meds may increase
risk of hepatotoxicity: barbiturates, hydantoin, carbmazepine,
rifampin, sulfinpyrazone, and ethanol - Activated charcoal reduces acetaminophen absorption. Mucomyst
is used as an antidote in overdosage
what are the AE of acetaminophen?
- Symptoms of hypersensitivity are skin eruptions, uritcaria, erythema, fever; Rare
hematologic reactions; hypoglycemia, liver toxicity, jaundice - Overdosage possible and can be fatal, particularly a problem in young
children - *Do not exceed < 4grams / day.
- A condition that results from inappropriate uric acid metabolism
- Underexcretion of uric acid
- Overproduction of uric acid
- Uric acid crystals are deposited in tissues and joints, resulting in pain and
inflammation. - Hyperuricemia
gout
what are the antigout drugs?
- allopurinol (Zyloprim®)
- febuxostat (Uloric®)
- colchicine
- probenecid (Benuryl®)
- Sulfinpyrazone
- Indication: Used to prevent uric acid
production and to prevent acute tumour lysis
syndrome - Used: for longer term treatment not acute
gout. - Adverse effects: agranulocytosis, aplastic
anemia and severe skin conditions such as;
exfoliative dermatitis, Stevens-Johnson
syndrome, and toxic epidermal necrolysis
allopurinol
- Best for patients with low urate clearance.
- Inhibits the reabsorption of uric acid in the kidneys and thus increases the excretion of
uric acid. - Contraindications: current peptic ulcer disease, blood dyscrasias, or kidney function
impairment
probenecid
- Oldest available therapy for gout
- Reduces the inflammatory response to the deposits of urate crystals in joint tissue
- Powerful inhibitor of cell mitosis, and can cause short-term leukopenia
- Short term use of 1 to 1.2mg (one time) is dose for acute gout followed by 0.6 mg on a
regime. Pg 797. - Can be used, for prophylaxis in dosages of 0.6 mg once or twice a day
- Works best on empty stomach, but can be given with food.
colchicine
