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Drugs reference index «Diclofenac Sodium/Misoprostol»

Diclofenac Sodium / Misoprostol

Pronunciation: (dye-KLOE-fen-ak SOE-dee-um MYE-soe-PROST-ol)Class: Nonnarcotic analgesic combination

Trade Names:Arthrotec- Tablets Diclofenac sodium 50 mg/Misoprostol 200 mcg- Tablets Diclofenac sodium 75 mg/Misoprostol 200 mcg

Pharmacology

Diclofenac, an NSAID, decreases inflammation, pain, and fever, probably through inhibition of cyclooxygenase activity and prostaglandin synthesis. Misoprostol, a prostaglandin E 1 analog, provides gastric antisecretory and mucosal protective properties.

Indications and Usage

Treatment of signs and symptoms of osteoarthritis (OA) and rheumatoid arthritis (RA) in patients at high risk of developing NSAID-induced gastric and duodenal ulcers and their complications.

Contraindications

Pregnancy; sensitivity to aspirin or any NSAID; sensitivity to misoprostol or other prostaglandins; history of asthma, urticaria, or other allergic-type reactions after taking aspirin or other NSAIDs; treatment of perioperative pain in the setting of coronary artery bypass graft (CABG) surgery.

Dosage and Administration

OAAdults

PO Diclofenac 50 mg/misoprostol 200 mcg (50/200) 3 times daily. For patients experiencing intolerance, 50/200 or diclofenac 75 mg/misoprostol 200 mcg (75/200) twice daily can be used, but they are less effective at preventing ulcers. Administer with meals.

RAAdults

PO 50/200 three or 4 times daily. For patients experiencing intolerance, 50/200 or 75/200 twice daily can be used, but they are less effective at preventing ulcers. Administer with meals.

General Advice

  • Administer tablet whole; do not crush or dissolve.
  • Administer the lowest effective dose for the shortest duration consistent with treatment goals.

Storage/Stability

Store tablets at or below 77°F. Protect from moisture.

Drug Interactions

ACE inhibitors

Antihypertensive effect may be decreased by diclofenac.

Antacids

Bioavailability of misoprostol may be reduced and absorption of diclofenac may be delayed. Magnesium-containing antacids increase risk of misoprostol-associated diarrhea.

Aspirin

Risk of serious GI complications, including bleeding, may be increased.

Cyclosporine

Risk of cyclosporine toxicity, including nephrotoxicity, may be increased.

Digoxin

Diclofenac may elevate digoxin levels, increasing risk of toxicity.

Diuretics

The natriuretic effect of furosemide and thiazide diuretics may be reduced. Coadministration of potassium-sparing diuretics may increase serum potassium levels.

Hypoglycemic agents, oral

Both hypo- and hyperglycemia may occur, necessitating a change in hypoglycemic dosage.

Lithium

Lithium levels may be elevated, increasing risk of toxicity.

Methotrexate

May increase methotrexate levels.

Phenobarbital

Phenobarbital toxicity has been reported following the initiation of diclofenac therapy.

Warfarin

May increase risk of gastric erosion and bleeding.

Adverse Reactions

GI

Abdominal pain (21%); diarrhea (19%); dyspepsia (14%); nausea (11%); flatulence (9%).

Genitourinary

Postmenopausal vaginal bleeding.

Precautions

Warnings

Misoprostol can cause abortion, premature birth, and birth defects in women who are pregnant. Uterine rupture has been reported when misoprostol was given to pregnant women to induce labor or abortion beyond the eighth week of pregnancy. Ensure that misoprostol is not be used by women of childbearing potential unless the patient requires NSAID therapy and is at high risk of developing gastric ulcers associated with NSAID use. Such patients must have a negative serum pregnancy test within 2 wk prior to beginning therapy; be capable of complying with effective contraceptive measures; receive both oral and written warnings of the hazards of misoprostol, risk of contraception failure, and danger to other women of childbearing potential if they take the medication by mistake; and begin drug only on second or third day of next normal menstrual period.

CV risk

NSAIDs may cause an increased risk of serious CV thrombotic events, MI, and stroke, which can be fatal. This risk may increase with length of therapy. Patients with CV disease or risk factors for CV disease may be at greater risk. Arthrotec is contraindicated for treatment of perioperative pain in the setting of CABG surgery.

GI risk

NSAIDs cause an increased risk of serious GI adverse reactions, including bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal. These reactions can occur at any time during use, with or without warning symptoms. Elderly patients are at greater risk of serious GI events.

Monitor

Monitor Hgb and Hct in patients on long-term therapy exhibiting signs or symptoms of anemia. Monitor liver enzymes within 4 to 8 wk after starting therapy. Monitor for signs and symptoms of GI bleeding. Check CBC and chemistry profile periodically in patients receiving long-term treatment.

Pregnancy

Category X .

Lactation

Diclofenac

Excreted in breast milk.

Misoprostol

Undetermined.

Children

Safety and efficacy in patients younger than 18 yr of age not established.

Elderly

Increased risk of adverse reactions. Select dose with caution because elderly patients are more likely to have decreased renal function.

Renal Function

NSAIDs may cause a further decrease in renal function in patients with preexisting renal function impairment. Use is not recommended in patients with advanced renal disease.

Hepatic Function

Diclofenac can cause abnormal LFTs, often within the first 2 mo of therapy.

Anaphylactoid reactions

May occur in patients without known prior exposure to diclofenac. Do not administer this product to patients with the aspirin triad. Severe, potentially fatal bronchospasm may occur.

Anemia

Has been reported and may be caused by fluid retention, occult or gross GI blood loss, or incompletely described effect on erythropoiesis.

Aseptic meningitis

Aseptic meningitis with fever and coma may occur and may be more likely in patients with systemic lupus and related connective tissue diseases.

Asthma

NSAIDs may precipitate bronchospasm in some patients with asthma.

CHF

Fluid retention and edema may occur; use with caution in patients with fluid retention or heart failure.

Hematologic disorders

NSAIDs interfere with platelet function and vascular response to bleeding; use with caution in patients with coagulation disorders or those who are receiving anticoagulants.

Hypertension

Onset of new hypertension or worsening of preexisting hypertension may occur, increasing the risk of CV reactions.

Porphyria

Avoid use in patients with hepatic porphyria.

Renal effects

Long-term administration of diclofenac may cause renal injury, including renal papillary necrosis. Renal toxicity may occur in patients in whom renal prostaglandins have a compensatory role in maintaining renal perfusion.

Skin reactions

Serious and sometimes fatal skin adverse reactions, including exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis, may occur.

Overdosage

Symptoms

Diclofenac

Aspiration pneumonitis, confusion, death, drowsiness, GI complaints, hypotonia, increased intracranial pressure, loss of consciousness, vomiting.

Misoprostol

Abdominal pain, bradycardia, convulsions, diarrhea, dyspnea, fever, GI discomfort, hypotension, palpitations, sedation, tremor.

Patient Information

  • Advise patient to read the patient information leaflet before using product the first time and with each refill.
  • Advise patients of the abortifacient property and not to share this drug with others.
  • Caution women not to take this medicine if pregnant and to take measures to prevent pregnancy while on this drug. If a patient suspects she is pregnant, advise her to stop taking the drug and to contact health care provider immediately.
  • Advise women who become pregnant or intend to become pregnant during therapy to notify health care provider.
  • Instruct patient to report any signs or symptoms of GI ulceration or bleeding, skin rash, swelling, or weight gain to health care provider.
  • Instruct patient not to take drug and to seek immediate medical attention if signs of liver toxicity occur, including fatigue, flu-like symptoms, itching, jaundice, lethargy, nausea, or right upper quadrant tenderness.
  • Caution breast-feeding mothers to discontinue breast-feeding because of potential harm to the baby.
  • Instruct patient to seek immediate medical attention if difficulty breathing or swelling of the face or throat occurs.
  • Tell patient that abdominal pain, diarrhea, nausea, and upset stomach may develop during first few weeks of therapy and usually stop after approximately 1 wk of continued treatment. To minimize diarrhea, advise patient to take with meals and avoid antacids containing magnesium. If symptoms persist for more than 7 days or if symptoms become severe, instruct patient to notify health care provider.
  • Instruct patients to swallow tablet whole, and not to crush, chew, or dissolve.

Copyright © 2009 Wolters Kluwer Health.

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