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Musculoskeletal
FA complete review part 4 Pharmacology
| Question | Answer |
|---|---|
| Which are the anti-inflammatory type of drugs that inhibit Phospholipase A2 in the Arachidonic acid pathway? | Glucocorticoids (corticosteroids) |
| Which enzyme is inhibited by glucocorticoids in the AA pathway? | Phospholipase A2 |
| Membrane phospholipids are converted into Arachidonic acid via which enzyme? | Phospholipase A2 |
| Leukotriene synthesis stopped by inhibiting which enzyme? | 5-Lipoxygenase |
| Inhibition of 5-lipoxygenase causes the inhibition what type product synthesis? | Leukotrienes |
| What is a common drug that works by inhibiting 5-Lipoxygenase? | Zileuton |
| Which enzyme is inhibited by Zileuton? | 5-Lipoxygenase |
| What process is inhibited with the use of Zileuton? | Leukotriene synthesis |
| Which leukotrienes are inhibited ty Leukotriene receptor antagonists? | LTC-4, LTD-4, and LTE-4 |
| What are some common Leukotriene Receptor antagonists? | Montelukast and Zafirlukast |
| LTC4, LTD4, LTE4 cause: | Increased bronchial tone |
| What is the function of LTB4? | Incrase neutrophil chemotaxis |
| Which is precursor of leukotrienes from Arachidonic acid? | 5-HPETE |
| What enzyme converts Arachidonic acid into 5-HPETE? | 5-Lipoxygenase |
| Which Leukotriene (LT) subtype is NOT inhibited by Leukotriene receptor antagonists? | LTB-4 |
| What is a common COX-2 only inhibitor? | Celecoxib |
| What is the irreversible COX-1 & COX-2 inhibitors? | Aspirin |
| Which COX is inhibited by Celecoxib? | COX-2 |
| List of reversible NSAIDs: | - Diclofenac - Ibuprofen - Indomethacin - Ketorolac - Naproxen |
| What process is inhibited by inhibiting COX? | Endoperoxidase synthesis |
| What are the roles of PGI2? | - Decreased platelet aggregation - Decreased vascular tone |
| Which prostaglandin decreases vascular tone? | PGE-1 |
| What are the products of Cyclic endoperoxides? | Prostacyclin, Prostaglandins, and Thromboxane |
| Which prostaglandins work by increased uterine tone? | PGE2 and PGF-2 alpha |
| What is the functions of TXA2? | - Increased platelet aggregation - Increased vascular tone |
| What is the mechanism of action of Acetaminophen? | Reversibly inhibits cyclooxygenase, mostly in CNS |
| Where does acetaminophen has the most efficacy? | CNS |
| What are clinical uses for Acetaminophen? | Antipyretic, analgesic, but not anti-inflammatory |
| True or False. Acetaminophen has no anti-inflammatory properties. | True. Acetaminophen is not an anti-inflammatory |
| What medication should be used instead to aspirin in children to avoid Reye syndrome? | Acetaminophen |
| What does OD on acetaminophen causes? | Hepatic necrosis |
| What is the acetaminophen metabolite? | NAPQI |
| What causes NAPQI? | Depletes glutathione and foresm toxic tissue byproducts in liver |
| What is used to treat acetaminophen overdose? | N-acetylcysteine |
| How does N-acetylcysteine works to treat acetaminophen overdose? | Regenerates glutathione |
| What is MOA of Aspirin? | Irreversibly inhibits cyclooxygenase-1/-2, by covalent acetylation leading to decreased synthesis of TXA2 and prostaglandins |
| What hematologic lab result in increased by the use of Aspirin? | Bleeding time |
| How long do the effects of Aspirin last? | Until new platelets are produced |
| What is the clinical cause for a low dose of Aspirin? | Decrease platelet aggregation |
| What is considered a low dose of aspirin? | < 300 mg/day |
| What is a intermediate dose of aspirin? | 300-2,400 mg/day |
| What is the clinical use of intermediate aspirin dose? | Antipyretic and analgesic |
| What is consider a high dose of Aspirin? | 2,400-4,000 mg/day |
| What is the clinical use of high-dose of Aspirin? | Anti-inflammatory |
| What does toxic doses of Aspirin can provoke? | Respiratory alkalosis early, but transition to mixed metabolic acidosis-respiratory alkalosis |
| What reh the acute adverse effects of Aspirin? | Gastric ulceration, tinnitus (CN VII),and allergic reactions |
| What are some adverse effects of chronic aspirin administration? | Acute renal failure, interstitial nephritis, and GI bleeding |
| What is a severe adverse effect of treating a child's fever with Aspirin? | Reye syndrome |
| Which conditions lead to higher risk to develop allergic reaction to aspirin? | Asthma and/or nasal polyps |
| What is used to treat Aspirin overdose? | NaHCO3 (sodium bicarbonate) |
| What is the acid base profile of Aspirin toxicity? | 1st: Respiratory alkalosis (early) 2nd: Transitions to mixed metabolic acidosis <--> Respiratory alkalosis |
| MOA of Celecoxib | Reversibly and selectively inhibits the cyclooxygenase (COX) isoform 2 |
| COX-2 receptors are found in: | Inflammatory cells and vascular endothelium and mediates inflammation and pain |
| Why is Celecoxib used to treat pain in PUD patients? | Spares COX-1, which helps maintains gastric mucosa, thus not affect PUD patients |
| Spares platelet function as TXA2 productions is dependent on COX-1. Drug? | Celecoxib |
| What conditions are often treated with Celecoxib? | Rheumatoid arthitirts and Osteoarthritis |
| What are the significant adverse effects associated with Celecoxib? | 1. Increase risk of thrombosis 2. Sulfa allergy |
| What are some examples of NSAIDs? | Ibuprofen, naproxen, indomethacin, ketorolac, diclofenac, meloxicam, and piroxicam. |
| What is the MOA of NSAIDs? | Reversibly inhibit COX-1 and COX-2; blocking prostaglandin synthesis. |
| What is the clinical use for NSAIDs? | Antipyretic, analgesic, anti-inflammatory |
| What is an specific use for Indomethacin? | Close a PDA |
| Which NSAID is used to close a PDA? | Indomethacin |
| What are the associated adverse effects of NSAIDs? | 1. Interstitial nephritis 2. Gastric ulcer 3. Renal ischemia 4. Aplastic anemia |
| How does usage of NSAIDs for a prolonged time cause a Gastric ulcer? | Prostaglandins protect gastric mucosa |
| Which type of analgesics are contraindicated in persons with PUD or risk of any gastric ulcer? | NSAIDs |
| How does NSAID therapy may cause renal ischemia? | Prostaglandin vasodilation afferent arteriole of the nephron |
| MOA of Leflunomide: | Reversibly inhibits dihydroorotate dehydrogenase, preventing pyrimidine synthesis |
| What are the common uses for Leflunomide? | Rheumatoid arthritis and Psoriatic arthritis |
| Associated adverse effects of Leflunomide: | Diarrhea, HTN, Hepatotoxicity, and Teratogenicity |
| Which enzyme is inhibited by Leflunomide? | Dihydroorotate dehydrogenase |
| Common Bisphosphonates: | Alendronate, Ibandronate, Risedronate, and Zoledronate |
| Pyrophosphate analogs used in bone diseases? | Bisphosphonates |
| MOA of Bisphosphonates: | Bind hydroxyapatite in bone, inhibiting osteoclast activity |
| What are common clinical uses of Bisphosphonates? | Osteoporosis, hypercalcemia, Paget disease of bone, metastatic bone disease, and osteogenesis imperfecta |
| What are the associated adverse effects of Bisphosphonates? | 1. Esophagitis 2. Osteonecrosis of jaw 3. Atypical femoral stress fractures |
| How is Esophagitis due to bisphosphonates intended to prevented? | Patients are advised to take with water and remain upright for 30 minutes |
| What is the mode of action of Teriparatide? | Increase osteoblastic activity when administered in pulsatile fashion |
| Important Recombinant PTH analog used for Osteoporosis. | Teriparatide |
| What is the clinical use of Teriparatide? | Osteoporosis; causes increase bone growth compared to antiresorptive therapies |
| What is the adverse effect of Teriparatide? | Increase risk of Osteosarcoma and transient hypercalcemia |
| What are the chronic gout drugs (preventive)? | Probenecid, Allopurinol, Pegloticase, and Febuxostat |
| List of Acute Gout drugs: | 1. NSAIDs 2. Glucocorticoids 3. Colchicine |
| MOA of Probenecid: | Inhibits reabsorption of uric acid in PCT |
| What is a common adverse of Probenecid? | Precipitate uric acid calculi |
| What are two common Gout (preventive) drugs that inhibit XO? | Allopurinol and Febuxostat |
| What is the mode of action of Allopurinol | Competitive inhibitor of XO leading to a decrease conversion of hypoxanthine and xanthine to urate |
| Other than in Gout, Allopurinol, is also a preventive measure for: | Tumor lysis-associated urate nephropathy in Leukemia and lymphoma patients |
| The use of Allopurinol leads to increase concentrations of: | Xanthine oxidase active metabolites, azathioprine, and 6-MP. |
| High levels of 6-MP and Azathioprine are often seen in patient with long Hx of Gout, because: | Allopurinol use |
| MOA of Febuxostat: | Inhibits xanthine oxidase |
| What is the MOA of Pegloticase? | Recombinant uricase catalyzing uric acid to allantoin |
| What is more water soluble, uric acid or allantoin? | Allantoin |
| Which Gout-treating medication is known to convert uric acid into allantoin? | Pegloticase |
| In which part of the nephron does Probenecid act upon? | PCT |
| What is an added effect of Probenecid? | Inhibition of the secretion of penicillin |
| Which drugs can inhibit (decrease) uric acid excretion/secretion? | Diuretics and low-dose salicylates |
| How does high-dose salicylates help in treating acute gout flares? | Inhibit tubular reabsorption of Uric acid |
| Does high-dose or Low-dose salicylates, help in treating acute gout events? | High-dose salicylates |
| What is the MOA of Colchicine? | Binds and stabilizes tubulin to inhibit microtubule polymerization, impairing neutrophil chemotaxis and degranulation |
| To what protein does Colchicine bind in order to work in acute gout? | Tubulin |
| What is the result of Colchicine--Tubulin binding? | Microtubule polymerization which leads to impairing neutrophil chemotaxis and degranulation |
| What type of side effects are associated with Colchicine? | GI and Neuromyopathic side effects |
| List of common TNF-alpha inhibitors: | 1. Etanercept 2. Infliximab, 3. Adalimumab, 4. Certolizumab, 5. Golimumab |
| What is the mechanism of action of Etanercept? | TNF-alpha inhibitor |
| Fusion protein, produced by recombinant DNA | Etanercept |
| What drug is a decoy receptor for TNF-alpha + IgGi Fc? | Etanercept |
| What conditions are often treated with Etanercept? | Rheumatoid arthritis, psoriasis, and ankylosing spondylitis |
| List of Anti-TNF-alpha monoclonal antibody medications: | Infliximab, Adalimumab, Certolizumab, and Golimumab |
| Which conditions are treated with infliximab? | Inflammatory bowel disease, rheumatoid arthritis, ankylosing spondylitis, and psoriasis |
| What are the most significant adverse effect of TNF-alpha inhibitors? | Predisposition to infection, including reactivation of latent TB and drug-induced lupus. |
Created by:
rakomi
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