Term
What is the chemoreceptor trigger zone? |
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Definition
area postrema, in the caudal medulla |
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Term
What is important to keep in mind about area postrema? |
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Definition
circulation reaches it becasue no BBB and it controls vomiting |
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Term
What are the inputs to the emetic region? |
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Definition
vestibular inputs, vagal input, solitatry taste inputs |
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Term
What is the efferent component of the emetic center? |
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Definition
DMX nucleus of the Vagus Nerve, which is responsible for the physiological response of vomiting |
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Term
What is the connection between the CTZ and the emetic center carried by? (neurotransmitter) |
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Definition
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Term
What blockers would be useful in blocking emesis from CTZ-triggered emesis (Opioid |
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Definition
D2, H1, M, Serotonin- indcued)?,Substance P block. However, higher cetner inputs go directly to emetic cneter, so a Subastance P block would not effect emesisi induced by vision taste and thought. |
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Term
Which 2 drugs induce emesis? |
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Definition
Syrup of Ipecac and Apomorphine |
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Term
What is the MOA of Syrup of Ipecac? |
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Definition
local irritatnt in the intestines and direct effects ofn the CTZ |
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Term
When is Syrup of Ipecac given? |
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Definition
only used in CONSCIOUS patients to indcue emesis in 15-20 minutes |
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Term
What is the time of onset of Apormorphine? |
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Definition
very rapid; more rapid than SYrup of Ipecac |
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Term
What is the MOA of Apomorphine? |
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Definition
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Term
What are the 5HT3 antagonists used for chemo patients and pregos to block emesis? |
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Definition
Ondansentron, Granisetron, palonosetron |
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Term
What are the therapeutic uses of the 5HT3 antagonists? |
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Definition
Chemo-indcued nausea, Hyperemesis of pregnancy |
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Term
what are the adverse effects of 5HT3 antagonists? |
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Definition
constipation and headache, but generally well-tolerated |
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Term
What are the D2 receptor antagonists? |
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Definition
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Term
What receptor overlap does Promethazine have? |
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Definition
also blocks cholinergic and histaminergic receptors |
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Term
What are the therapeutic uses of D2 antagonists used for anti-emesis |
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Definition
Gastroenteritis, drug-induced nausea, motion sickness |
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Term
What are the adverse effects of D2 antagonists? |
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Definition
drowsiness, diarrhea, extrapyramidal side effects |
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Term
What are the antihistamines used for anti-emesis? |
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Definition
Dimenhydrinate, Diphenhydramine, Meclizine |
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Term
What are the therapeutic uses of Antihistamines? |
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Definition
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Term
What are the adverse effects of Antihistmaines? |
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Definition
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Term
What is the M-antagonist used for motion sickness /anti-emesis? |
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Definition
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Term
How is Scopolamine administered? |
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Definition
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Term
What is the therapeutic use of Scopolamine? |
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Definition
drug of choice for motion sickness |
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Term
What are the adverse effects of Scopolamine? |
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Definition
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Term
What anti-emetic is a Cannabinoid? |
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Definition
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Term
What is the use of Dronabinol? |
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Definition
prophylactic agent in cancer chemo, appetite stimulant in AIDsS patients or anorexics |
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Term
What are the adverse effects of Dronabinol? |
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Definition
central sympathetic stimulation leading to tachycardia; upon withdrawl, irritability |
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Term
What drugs are anti-nausea drugs in chemo patients that have anti-inflammatory effects to inhibit PG synthesis? |
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Definition
Synthetic Glucocorticoids |
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Term
What are the side effects of Systemic Glucocorticoids? |
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Definition
Hypoglycemia and Mood change; among other systemic side effects. |
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Term
What is the MOA of Aprepitant? |
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Definition
Substance P rceptor antagonist |
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Term
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Definition
in combo wiht Dexamethasone and 5HT3 antagonist for acute and delayed emesis a/w chemotherapy |
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Term
What combination of drugs is very good for pretreatment of chemo-induced emesis? |
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Definition
Aprepitant (substance P blocker), Dexamethasone, 5HT3 antagonist |
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Term
what depositis in joints with gout? |
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Definition
monosodium urate and uric acid crystals |
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Term
What is the pathophys of gout? |
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Definition
urate cyrstals phagocytosed by synoviocytes, PG release, PMN migrate and amplify respoknse further, Macrophages ingest urate crystals, amplifying the response further. |
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Term
What is the prototype NSAID used for Gout and what are 2 others? |
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Definition
Indomethacin, Naproxen, Etoricoxib |
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Term
What things do NSAIDs use to relieve gout? |
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Definition
inhibit PG synthesis, inhibit urate crystal phagocytosis |
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Term
What is the MOA of corticosteroids used for gout? |
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Definition
Inhibit COX, reducing inflammatory mediators. ALso inhibit PLA2. Inhibiting production of PG's and AA |
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Term
HOw are corticosteroids administered for gout? |
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Definition
orally or by local injection for single joint involvement; local injection avoids systemic side effects |
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Term
Why is Colchicine now 2nd line? |
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Definition
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Term
How is Colchicine administered? |
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Definition
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Term
How effective is Colchicine? |
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Definition
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Term
What is the MOA of Colchicine? |
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Definition
binds tubulin, preventing polymeriazatoin into tubules, ultimately inhibiting leukocyte migration and proinflammatroy release |
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Term
What is the Major side effect of Colchicine? |
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Definition
Terrible diarrhea in most patients; actually can be used as a laxative |
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Term
Whati interactions are a/w Colchicine? |
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Definition
It is a substrate for CYP3A4 and P-glycoprotien efflux transporter |
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Term
What antibiotic inhibits CYP3A4 and causes Colchicine toxicity? |
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Definition
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Term
What drug inhibits P-glycoprotein and leads to Colchicine toxicity? |
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Definition
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Term
What 2 drugs are contraindicated when a patient is taking Colchicine? |
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Definition
Clarithromycin and Cyclosporine |
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Term
What is the MOA of Probenecid and Sulfinpyrazone? |
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Definition
enhance uric acid excretion by inhibiting renal reabsorption in the proximal tubule |
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Term
What must be maintained in patients on Probenecid and Sulfinpyrazone? |
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Definition
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Term
What is a risk with Probenecid/Sulfinpyrazone use? |
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Definition
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Term
When are Probenecid and Sulfinpyrazone contraindicated? |
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Definition
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Term
Do Probenecid and Sulfinpyrazone work acutely? |
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Definition
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Term
What is the MOA of allopurinol and Febuxostat? |
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Definition
Xanthine Oxidase inhibitors; lower serum uric acid by inhibiting xanthine oxidase |
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Term
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Definition
Hypoxanthine-->xanthine by xanthine oxidase. Xanthinde--->uric acid by xanthine Oxidase |
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Term
Are the xanthine oxidase inhibitors effective acutely/short term? |
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Definition
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Term
In what situations are xanthine oxidase inhibitors used? |
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Definition
patients with high urine uric acid levels, impaired kidney funtin, or allergies to probenecid or sulfinpyrazone |
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Term
What are the adverse effects of Xanthine Oxidase inhibitors? |
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Definition
Hypersensitivity Reactions and liver enzyme abnormalities. |
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Term
What is a significant drug interaction with allopurinol? |
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Definition
Allopurinol and 6-Mercaptopurine (immunomodulator for IBS tx); 6-Mercaptopurine is inactivated by xanthine Oxidase, so a Xanthine Oxidase inhibitor increases the levels of 6-Mercaptopurine leading to serious leukopenia |
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Term
What are the 2 xanthine oxidase inhibitors? |
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Definition
ALlopurinol and Febuxostat |
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Term
What is the net effect of 6-Mercaptopurine / Allopurinol co-administration? |
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Definition
Leukopenia. 6 Mercaptopurine is broken down by Xanthine Oxidase, so if you inhibit XO with Allopurinol, 6-Mercaptopurine levels skyrocket |
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Term
What dosage must be evaluated with Allopurinol use? |
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Definition
6-mercaptopurine dose must be decreased by 50% |
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Term
Uncle Bob has gout. He has diabetes and his kidney function is poor. After initial treatment with Indomethacin |
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Definition
hea has been placed on long term drug that does not require fully functioning kidneys. What drug is it?,Allopurinol |
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Term
In What gout situations are Xanthine oxidase Inhibitors given? |
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Definition
effective in recurrence of acute gouty arthritis and treating urate neprhrolithiasis. It is safe for LONG TERM |
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