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Gout/Emesis
Pharm
64
Medical
Kindergarten
04/27/2010

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Cards

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