Ch 16 -Anti-inflammatory, Antiarthritis,

Question 1

What are anti-inflammatory, antiarthritis

Answer 1

There are a couple different drugs 1. Corticosteroids are used to systemically to block the inflammatory and immune systems but can lead to adverse effects including dec resistance to infection and neoplasms, can be used topically for local effect without as much adverse effects.
Antihistamines are used to block the release of histamine in the initiation of the inflammatory response.
Many of both of these drugs are bought OTC

Question 2

What are salicylates? Therapeutic, Pharmcokinetics, adverse effects, drug-drug.

Answer 2

Are popular anti-inflammatory agents not only because of their ability to block the inflammatory response, but also because of their antipyretic and analgesic properties.
Aspirin
Indications: Treatment of mild to moderate pain, fever, inflammatory conditions; reduction of risk of transient ischemic attack or stroke; reduction of risk of myocardial infarction.
Action: Inhibits the synthesis of prostaglandins, blocks the effect of pyrogens at the hypothalamus; inhibits platelet aggregation by blocking thromboxane A2.
Pharmacokinetics; Route PO, rectal Onset 5-30 min, 1-2 h Peak 0.25-2h, 4-5h, Duration 3-6h, 6-8 h
T1/2: 15 min to 12 h; metabolized in the liver and excreted in the urine
Adverse Effects: Nausea, vomiting, heartburn, epigastric discomfort, occult blood loss, dizziness, tinnitus, acidosis.
Drug-drug: interact with many other drugs, primarily because of alterations in absorption, effects on the liver, or extension of the therapeutic effects of the salicylate.

Question 3

What is NSAIDS? Therapeutic, pharmcokinetic, adverse effects, drug-drug.

Answer 3

This group of drugs includes propionic acids, acetic acids, fenamates, oxicam derivatives, and cyclooxygenase -2 inhibitors.
Ibuprofen (propionic). Diclofenac (acetic acids) Meclofenamate (fenamates), celecoxib (cyclooxygenate-2 inhibitors)
Indications: Relief of the signs and symptoms of rheumatoid arthritis and osteoarthritis; relief of mild to moderate pain; treatment of primary dysmenorrhea; fever reduction.
Actions: Inhibits prostaglandin synthesis by blocking COX-1 and COX-2 receptor sites, leading to an anti inflammatory effect, analgesia, and antipyretic effects.
Pharamacokinetics: Route PO IV, Onset 30 min, start of infusion, Peak 1-2 h, minutes, Duration 4-6h, 4-6 h.
T1/2: 1.8-2.5 h; metabolized in the liver and excreted in the urine.
Adverse Effects: Headache, dizziness, somnolence, fatigue, rash, nausea, dyspepsia, bleeding, constipation.

Question 4

What is acetaminophen? Therapeutic, pharmacokinetics, adverse effects, drug-drug.

Answer 4

Is used. To treat moderate to mild pain and fever and often is used in place of the NSAIDs or salicylates.
Indications: Treatment of mild to moderate pain, fever, or signs and symptoms of the common cold or flu; musculoskeletal pain associated with arthritis and rheumatic disorders.
Actions: Acts directly on the hypothalamus to cause vasodilation and sweating, which will reduce fever; mechanism of action as an analgesic is not understood.
Pharmacokinetics; Route PO Onset Varies Peak 0.5-2h Duration 3-6h
T1/2: 1 - 3 h; metabolized in the liver and excreted in the urine.
Adverse effects: Rash, fever, chest pain, liver toxicity and failure, bone marrow suppression.

Question 5

What are antiarthritis agents? Gold compounds?

Answer 5

That block the inflammatory process. Arthritis is a potentially debilitating inflammatory process in the joints that causes pain and bone deformities.
Gold compounds
Auranofin
Indications: Treatment of selected adults with rheumatoid arthritis, who have insufficient response to or intolerance to NSAIDs
Actions: Taken up by macrophages, which inhibits phagocytosis and release of lysosomal enzymes that cause damage associated with inflammation.
Pharmacokinetics; Route PO Onset Slow Peak 4-6h
T 1/2: 3-7 days; excreted in the urine and feces.
Adverse Effects: Bone marrow suppression, renal toxicity, dermatitis, nausea, vomiting, stomatitis. Kick

Question 6

What is tumor necrosis factor? Therapeutic, pharmacokinetics, adverse effects, drug-drug.

Answer 6

Are often the first class used with progressing arthritis, act to deck the local effects of TNF, a locally released cytokines that can cause the death of tumor cells and stimulate a wide range of pro inflammatory activities.
Adalimumab
Indications: Reduction of signs and symptoms, and improvement of function with rheumatoid arthritis, psoriatic arthritis, ankylosis spondylitis, plaque psoriasis, crohn disease, ulcerative colitis, hidradenitis suppurativa, uveitis,
Actions: Specifically binds to TNF-a and blocks its interaction with cell surface TNF receptors.
Pharmacokinetics: Route SC
Adverse effects: injection site pain, URTI, inc creative phosphokinase, headache, rash, sinusitis

Question 7

What is other antiarthritis drugs? Leflunomide

Answer 7

It directly inhibits an enzyme, dihydroorotate dehydrogenase, that is active in the autoimmune process that leads to rheumatoid arthritis, reliving signs and symptoms of inflammation and blocking the structural damage this inflammation can cause, slowing disease progression.
Is slowly absorbed from the GI tract, reaching peak levels in 6- 12 h. It undergoes hepatic metabolism and excretion in the urine. Half life is 14-18 days.
Adverse effects: local irritation at injection site, pain with injection, and inc risk of infection. Is associated with potentially fatal hepatic toxicity, hence the pt liver function needs to be monitored closely.
Drug-drug: can cause severe liver dysfunction if it is combined with other hepatotoxic drugs.