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TERMS TO LEARN

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Abortifacient An agent that causes an abortion.
Dysmenorrhea Painful menstruation.
Orthostatic Hypotension Low blood pressure in the standing position.
Tinnitis Ringing in the ears.

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I. PROSTAGLANDIN ANALOGS

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PROSTAGLANDIN ANALOGS: DRUG FACTS

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Drug Pharmacokinetics Clinical Uses Side Effects
PGE1 Analogs
Alprostadil (Prostin, Muse, Caverject)
  • A: IV, intracavernosal injection, and intraurethral suppository

  • M: Metabolized in the lungs

  • E: Metabolites excreted in urine

  • Maintains patent ductus arteriosus in infants with this condition or with congenital heart defects until surgical repair (Prostin)

  • Erectile dysfunction (Caverject—penile injection; Muse—suppository)

  • Flushing

  • Bradycardia/tachycardia

  • Hypotension

  • Diarrhea

  • May result in gastric obstruction secondary to antral hyperplasia in neonates

Misoprostol (Cytotec)
  • A: PO

  • M: Hepatic

  • E: Majority of metabolites excreted in urine; remainder in feces

  • Treatment and prophylaxis of NSAID-induced gastric ulcer

  • Abortifacient

  • Cervical ripening and induction of labor

  • GI effects (abdominal pain, diarrhea, constipation, and dyspepsia)

  • Headache

  • Vaginal bleeding

PGE2 Analog
Dinoprostone (Prepidil, ProstinE2, Cervidil)
  • A: Vaginal gel and suppository

  • M: Metabolized in lungs, kidneys, spleen, and other tissues

  • E: Majority of parent drug and metabolites excreted in urine; remainder in feces

  • Vaginal suppository to ripen cervix and induce labor (Prepidil—gel)

  • Induce abortion (Prostin E2—vaginal suppository)

  • Both indications (Cervidil)

  • Chills/shivering

  • GI effects (abdominal pain, diarrhea, nausea, and vomiting)

  • Headache

PGI2 Analog
Epoprostenol (Flolan)
  • A: IV

  • M: Hydrolyzed in plasma

  • E: Majority of metabolites excreted in urine; remainder in feces

  • Pulmonary hypertension (drug of last resort, not very effective)

  • Flushing

  • GI effects (abdominal pain, diarrhea, nausea, and vomiting)

  • Headache

  • Hypotension

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II. DRUGS USED IN THE TREATMENT OF GOUT

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MANAGING GOUT: DRUG FACTS

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Drug Pharmacokinetics Mechanism of Action Clinical Uses Drawbacks and Side Effects
Indomethacin (Indocin)
  • A: PO, IV, or rectal

  • M: Hepatic (P450 minor)

  • E: Metabolites primarily excreted in urine

  • NSAID that inhibits COX

  • Reduces production of prostaglandins

  • Inhibits phagocytosis of uric acid crystal by macrophages

  • Acute treatment of gouty arthritis

  • GI effects (irritation, bleeding, and ulceration)

  • Renal effects (dysuria, interstitial nephritis, and renal failure)

  • CNS effects (headache, dizziness)

  • Hepatic effects (jaundice, cholestatic hepatitis)

  • Hematologic effects (thrombocytopenia, leukopenia)

  • Inhibits P450 enzymes

Colchicine
  • A: PO and IV

  • M: Hepatic (P450)

  • E: Parent drug and metabolites primarily excreted in urine

  • Disrupts the inflammatory cycle, which inhibits leukocyte migration and phagocytosis of uric acid crystals

  • Acute treatment of gouty arthritis

  • Low doses useful for chronic treatment of gout

  • Narrow therapeutic window so must be carefully titrated to effective dose in each individual

  • Overdose can lead to nephrotoxicity, hepatotoxicity, or death

  • Long t1/2 in the white blood cells leading to systemic accumulation (must wait 3–4 days between uses)

  • IV dose must be administered in an indwelling catheter due to irritation

  • GI side effects (nausea, abdominal discomfort, ...

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