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Terms in this set (57)

Prostaglandin Analog Drugs
- Misoprostol
- Iloprost
- Latanoprost
- Travaprost
- Bimatoprost
NSAIDs drugs
- Aspirin

Acetic and Propionic Acids
- Indomethacin
- Ibuprofen
- Diclofenac
- Naproxen
- Ketorolac

Oxicams:
- Meloxicam
- Piroxicam

COX-2 Specific
- Celexocib

Acetaminophen
Drugs for arthritis
- Abatacept
- Adalimumab
- Anakinra
- Certolizumab
-Chloroquine/hydroxychloroquine
- Ethercept
- Golimumab
- Infliximab
- Leflunomide
- Methotrexate
- Tocilizumab
- Tofacitinib
What are prostaglandins? What are they also called? Inflammatory effect?
Lipid compounds that have hormone-like effects

Also called eicosanoids

pro-inflammatory effect
What is the primary precursor for the synthesis of prostaglandins?
Arachidonic acid
What are the 2 different pathways for prostaglandin synthesis?
- Cyclooxygenase pathway
- Lipoxygenase pathway
What are the products of Cyclooxygenase pathway?
Cyclooxygenase pathway-1 (COX-1): produces prostanoids which regulates a bunch of stuff

Cyclooxygenase pathway-2 (COX-2): inflammatory products
What are the products of Lipoxygenase Pathway?
Leukotrienes: good for treatment of asthma
What is the major role/action of prostaglandins?
- regulate pain, inflammation, and fever
What is the MOA of misoprostol?
Prostaglandin Analog (anti-inflammatory drugs)

MOA: interacts with prostaglandin receptor on parietal cells to reduce gastric acid secretion and stimulate mucus and bicarbonate production
What is the clinical use of misoprostol?
- protects mucosal lining of stomach during chronic NSAID treatment
- Decreases incidence of gastric and duodenal ulcers
- can also be used to treat constipation
What is the "Anti-inflammatory" drug that protects stomach lining of stomach during chronic NSAID treatment?
Misoprostol
What are the adverse effects of Misoprostol?
- potential risk to induce abortion

- diarrhea, abdominal pain, HA
What is MOA of Iloprost?
activates prostacyclin receptors and increases cAMP

Pulmonary vasodilator to treat pulm. HTN via inhalation
What is the clinical use of Iloprost?
A pulmonary dilator used to treat pulmonary hypertension (increased BP in arteries of the lungs)
What are the side effects of Iloprost?
Dizziness, headache, and flushing
What is the MOA of Latanoprost?
binds to prostaglandin FP receptors and increases uveoscleral outflow--> reduces IOP
What are the side effects of Latanoprost, Travoprost, Bimatoprost?
Blurred vision, increased iris pigmentation, increased number and pigment of eyelashes, eye redness and irritation
What is the MOA of Travoprost?
- specific a pro-drug
- binds to prostaglandin FP receptors and increases uveoscleral outflow--> reduces IOP
What is the MOA of Bimatoprost?
- specifically mimics endogenous prostamides

- binds to prostaglandin FP receptors and increases uveoscleral outflow--> reduces IOP
How do NSAIDs work?
inhibit cyclooxygenase (COX) enzymes which leads to decreased prostaglandin synthesis
What are the 4 common effects of NSAIDs?
- analgesic
- anti-inflammatory
- antipyretic
-gastric and intestinal ulceration
What is the action of aspirin on the respiratory system?
Increases alveolar ventilation by elevating CO2 -> inc respiration
What is the action of aspirin on platelets?
- Platelet aggregation is inhibited by aspirin
- Low dose aspirin decreases TXA production in platelets
What is pharmacokinetics of aspirin?
Good oral absorption
Avoid in children and teenagers with viral infections
Cross BBB and placenta
Absorbed through intact skin
Eliminated via first-order kinetics (low dose)
Eliminated via zero order at anti-inflammatory doses
Liver metabolism
Kidney excretion
What is the MOA of Aspirin?
IRREVERSIBLY inactivates cyclooxygenase -> break down into salicylate -> has anti-inflammatory, antipyretic, and analgesic properties
What is the MOA of indomethacin?
reversible inhibition of COX-1 and COX-2.
What is the ocular effects of long term doses of Indomethacin?
blurry vision
- corneal opacities
- macular pigment changes

*these patients should be monitored for vision changes
What is the MOA of Oxicams? (Piroxicam and meloxicam)
Preferential for COX-2 (but NOT COX-2 specific)

Non-selective at high doses
What are the adverse effects of Oxicams? (Piroxicam and meloxicam)
Similar adverse effects as other NSAIDs
- Rare instances of serious stomach and intestinal bleeding
Why does Celecoxib produce fewer side effects?
COX-2 specific, so still has COX-1 effects (protects GI)
Acetaminophen v. NSAID
Acetaminophen = analgesic and antipyretic

NSAID = analgesic, antipyretic, ANTI-INFLAMMATORY, ANTI-PLATELET
T/F. Acetaminophen has less effect on cyclooxygenase in peripheral tissues and is considered an NSAID
false, not an NSAID
What is the DOC for children with viral infections/chickenpox?
acetaminophen
What is a good substitute for NSAID?
acetaminophen
What are the adverse effects of NSAID?
- Free of significant adverse effects at normal doses
- Hepatic necrosis at high doses (CI in severe hepatic impairment)
What is the max ibuprofen dose available?
Ibuprofen available as high as 800 mg

- Max dose is 3200 mg/day
What are the available doses of acetaminophen?
available in 325 mg, 500 mg and 650 mg tablets
What is the clinical use of Disease-Modifying Antirheumatic Drugs (DMARDs)?
-Used in the treatment of RA and other chronic inflammatory conditions
What is rheumatoid arthritis?
autoimmune disease that causes chronic inflammation in around joints due to destruction of cartilage
What is the initial therapy for RA?
glucocorticoids and/or NSAIDS (chronic therapy limited by side effects)
What is the management of RA?
treatment of pain, reduction of inflammation, and inhibition of the immune system
What is the MOA of methotrexate?
- immunosuppresant--> inhibits dihydrofolate reductase (Impairs DNA synthesis)

oral med
What does methotrexate aid in?
effectiveness for autoimmune disease
What was Hydroxychloroquine originally developed as?
anti-malarial drug
Leflunomide
Arthritis Drug (anti-inflammatory Drugs)

MOA: decreases pyrimidine synthesis in lymphocytes (causes cell arrest)

oral absorption

contraindcated in pregnancy
What is the MOA of hydroxychloroquine?
Increases pH within inflammatory cells -> interference w/ antigen processing -> decreased stimulation of CD4 cells

BULLS-EYE MACULOPATHY BOYYYYY
What are the adverse effects of hydroxychloroquine?
low doses: GI, skin rashes, HA

decreased vision: "bulls-eye maculopathy" = permanent vision loss
What are the highest RF of bulls-eye maculopathy?
- Excessive daily dose by weight
- Duration of use
- Concomitant use of tamoxifen
- Retinal disease
What is the current recommendation of plaquenil?
Dose: < 5mg/kg body weight

Eye screening: baseline within 1 year, annual screening after 5 years of use
What are the pro-inflammatory cytokines involved in RA?
Interleukin-1 and TNF-α
What is the treatment that has been shown to decrease signs and symptoms of RA?
TNF inhibitors or IL-1 antagonists
T/F - TNF inhibitors can be combined with methotrexate for standard therapy
TRUE
What are the adverse effects of TNF Inhibitors?
- Increased risk of infection
- Do not administer live vaccinations while on therapy
- Can cause worsening of preexisting heart failure
- Increased risk of lymphoma and other cancers
What is anakinra?
IL-1 receptor antagonist
What can't anakinra be combined with?
TNF inhibitors
Why should you monitor pts on anakinra?
signs of infection
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