Gout Dx

Use: Acute Gout Attack (terminates inflammation of acute attack), NO ANALGESIC EFFECT, no effect on urate excretion; effective prophylactic

Mechanism: Binds tubulin, inhibiting microtubule formation inhibiting leukocyte migration and phagocytosis (causes gout symptoms); Inhibits Leukotrine B4 formation. 

Pharmacokinetics: acute use; liver metabolism, biliary and fecal excretion

Dx interactions:

Toxicities: Diarrhea, nausea, vomiting, abdominal pain, may limit the use of the drug

NSAID

Use: Primary NSAID for gout; Terminates the inflammatory process of acute gouty attack

NSAID for gout

anti-inflammatory in acute gouty attack

Uricosuric agent: Gout

Mechanism: Increases urinary excretion of uric acid; Decrease excretion of many acidic compoud metabolites

Give with Colchicine to decrease chance of gouty attack

NOT for gouty attack, maybe prescribe 3 weeks later

Dx interactions: decreases excretionon of acidic drugs i.e. penicillin, methotrexate, clofibrate, glucoronides of NSAIDS

Mechanism: Decrease excretion of many acidic compoud metabolites

inhibits platelet aggregation; strong plasma protein binding

Dx interaction: inhibits liver metabolism of warfarin

Give with Colchicine to decrease chance of gouty attack

NOT for gouty attack, maybe prescribe 3 weeks later

interferes with renal excretion of many acidic compounds

Gout

Decreases formation of uric acid; not for acute gout

Mechanism: inhibits xanthine oxidase enzyme blocking metabolism of oxypurines (hypoxanthine, xanthine) to uric acid

Colchisine prophylaxis as allopurinol can precipitate a gouty attack

Side effects: serious, vasculitis, agranulocytosis, hypersensitivity rxns; 

Dx interactions: aluminum hydroxide decreases absorption, increases effect of chemo and cyclophosphamide, inhibits elimination of chloprpropamide, inhibitis the metabolism of warfarin and probenacid; inhibits activation of fluorouracil (5-FU) thus reducing its therapeutic effect

Gout dx; Non-human enzyme

Mechanism: Catalyzes enzymatic oxidation of uric acid into readily excreted metabolite (recombinant form of urate oxidase); uric acid converted to allantoin then excreted

Pharmacokinetics: IV administration, but can only give once

Adverse rxns: severe hypersensitivity/anaphylactic shock; nausea, vomiting, fever, headache etc. 

Use: Migraine

Mechanism: 5-HT Agonists (triptans), binds 5-HT receptors in intracranial vessels and arteriovenous anasomoses; phase 1, vasoconstrict intracranial arteries; not analgesic, decrease in pain from vasoconstriction

PHK: metabolism in liver to inactive product, excreted in urine; oral or subq

Side effects: vasospasms, Peripheral vascular ischemia (Bowel too), abd pain, dizziness etc.

contraindications: breast feeding, cardiac disease, cerebrovascular disease, coronary artery disease, DM, HTN, IV administration, PVD, pregnancy, renal impairment, seizures, tobacco smoking

Zolmitriptan (Zomig)

Naratriptan (Amerge)

Rizatriptan (Maxalt)

Eletriptan (Relpax)

Frovatriptan (Miguard)

Almotriptan (Axert)

Use: migraine acute attack, maybe cluster headache

Mechanism: partial agonists/antagonists for 5-HT in clood vessels (like triptans but not specific)

Adverse rxns: vasoconstriction, diarrhea, nausea vomiting, CV tox; ergotism (chronic)

Contraindications: vascular problems, allergies, renal, hepatic disease

Use: migraine acute attack, maybe cluster headache

Mechanism: partial agonists/antagonists for 5-HT in clood vessels (like triptans but not specific)

Given IV

Ergot alkaloid

Use: Migrain prophylaxis, vascular headache prophylaxis

Mechanism: partial agonist of 5-HT, weak vasoconstrictor

Prolonged use = can lead to ergotism, dependence and or rebound headaches

Urography should be done periodically to keep track of retroperitoneal fibrosis

PHK: High first pass metabolism (13% get bioavailable); shouldn't be used for more than 6 months w/o 3-4 week drug vacay; 

Adverse: retroperitoneal fibrosis, pleuropulmonary fibrotic changes, angina, inhibits lactation CNS stim, nausea, vomiting, abd pain, alopecia, arthralgia, myalgia, localized edema