Gout/Migraines

Question 1

Colchine

Answer 1

1. Alkaloid, anti-inflammatory effective only against gouty arthritis. Provides relief as well as prohpyhlactic against future attacks. Oral admin, liver metabolism, biliary/fecal excretion.
2. No analgesia, no effect on COX enzymes, no effect on urate excretion, binds to tubulin and inhibits the assembly of microtubules. Anti-inflammatory effects by inhibiting leukocyte migration and phagocytosis, inhibits formation of leukotriene B4.
3. SE produced by inhibition of tubulin polymerization.
4. Used along with uricosuric agents.
6. D/N/V, abdominal pain all may limit use of drug.

Question 2

Sumatriptan

Answer 2

1. Migraine Symptomatic treatment
   use: vasoconstriction to dec. migraine pain
2. Highly selectively agonist for 5HT D subtypes in the intracranial vessels (causes constriction)
   - oral, and sq, some plasma protein binding, metabolized in liver to inactive metabolites
3. Side Effects
   - coronary artery vasospasm, cardiac arrythmias, angina, transient myocardial ischemia, MI, cardiac arrest
   - cerebral vasospasm, peripheral vascular ishcemia, bowel ischemia,

CI in everyone who ever had heart, head, and vascular problems or with a baby

Question 3

Ergotamine Tartrate

Answer 3

1. Ergot Alkaloid
   use: migraine, cluster headache
2. partial agonist of 5HT on certain BV, antagonist on SM, partial agonist on alpha receptors
   administered orally or inhalation or sublingual
3. side effects due to vasoconstrictin (more potent than -triptans)
   - vomiting nausea diarrhea
   - chronic: vasoconstrition adn CNS

CI in PVD, and other things, see list

Question 4

Dihydroergotamine

Answer 4

1. ergot alkaloid
   use: tx migraines
2. IV administration,
3. nausea is a common adverse side effect

Question 5

Indomethacin

Answer 5

Primary NSAID used in Gout, naproxen and sulindac are also often used. ASA, salicylates are contraindicated as they decrease Urate excretin in usual analgetic doses.

Question 6

Probenecid

Answer 6

1. Uricosuric agent, increase uric acid secretion by blocking reabsorption in proximal tubule. Oral admin.
2. Do not start therapy until 2-3. wks after acute attack. Decreases excretion of many acidic compounds or metabolites (penicillin, methotrexate, clofibrate, glucuronides of NSAIDS).
3. SE: large amts of uric acid secreted may trigger kidney stones-maintain large volume of urine (pH >6.0, alkali administration) to minimize stones, initial admin may trigger acute attack: give colchine prophylacticly. Also may cause GI irritation.
5. Not effective in acute attacks and may actually aggravate them.

Question 7

Allopurinol

Answer 7

1. Inhibits synthesis of uric acid by inhibiting xanthine oxidase. Oral or IV
2. Effective in both primary and secondary forms of gout. Rapidly metabolized by hepatic oxidation to give oxipurinol (active compound). Initial therapy may precipitate acute attack, give prophylactic colchine.
3. SE: vasculitis, agranulocytosis, hypersensitivity rxns
4. Interactions: aluminum hydroxide, mercaptopurines, azathioprine, cyclophosphamide, chlorpropamide, warfarin, probenacid, fluorouracil.

Question 8

Rasburicase

Answer 8

1. Recombinant form of urate oxidase, will convert uric acid to allantoin. IV infusion administration.
2. Catalyzes oxidation of uric acid into allantoin which is readily excreted. Effective in Pts w/hematological malignancies or solid tumors are at particular risk for tumor lysis syndrome and thus hyperuricemia and related complications especially after chemotherapy.
3. Adverse effects: Severe hypersensitivity rxns including anaphylactic shock and anaphylactoid rxns. N/V, fever, HA, abdominal pain, constipation, diarrhea.