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Cytotec (Misoprostol)
Diclofenac inhibits COX-1/COX-2 to reduce prostaglandins; misoprostol is PGE1 analog protecting gastric mucosa.
Diclofenac sodium and misoprostol delayed-release tablets combine an NSAID with a prostaglandin analog for treating osteoarthritis and rheumatoid arthritis in patients at high risk of NSAID-induced ulcers. Diclofenac inhibits COX-1/COX-2 to reduce inflammation and pain, while misoprostol protects gastric mucosa by increasing bicarbonate and mucus secretion. The combination is contraindicated in pregnancy, active GI bleeding, CABG surgery, and patients with NSAID hypersensitivity or allergic reactions. Significant drug interactions exist with anticoagulants, antiplatelet agents, and serotonergic drugs, requiring careful monitoring for bleeding complications.
At a glance
| Generic name | Misoprostol |
|---|---|
| Sponsor | Pfizer |
| Drug class | NSAID combined with prostaglandin analog |
| Target | Cyclooxygenase (COX-1 and COX-2); Prostaglandin receptors |
| Modality | Small molecule |
| Therapeutic area | Immunology |
| Phase | FDA-approved |
| First approval | 1988 |
Mechanism of action
Diclofenac, an NSAID, inhibits cyclooxygenase (COX-1 and COX-2) enzymes, reducing prostaglandin synthesis in peripheral tissues. Prostaglandins sensitize afferent nerves and potentiate bradykinin-induced pain; they also mediate inflammation. By decreasing prostaglandins, diclofenac provides analgesic, anti-inflammatory, and antipyretic effects. Misoprostol is a synthetic PGE1 analog that counteracts NSAID-induced gastric damage by increasing bicarbonate and mucus secretion in the gastric and duodenal mucosa. Misoprostol binds to specific prostaglandin receptors with high affinity and saturable, reversible, stereo-specific binding. The combination addresses both the therapeutic benefit of NSAID activity and the protective effect against NSAID-induced ulceration through complementary mechanisms.
Approved indications
- Osteoarthritis in Patients at High Ulcer Risk
- Postpartum hemorrhage
- Prevention of CMV Disease After Organ Transplant
- Prevention of NSAID-Induced Gastric Ulcer
- Rheumatoid Arthritis in Patient at High Ulcer Risk
Common side effects
- Abdominal pain
- Diarrhea
- Dyspepsia
- Nausea
- Flatulence
Drug interactions
- Anticoagulants (e.g., warfarin)
- Antiplatelet drugs (e.g., aspirin)
- SSRIs and SNRIs
- ACE Inhibitors, Angiotensin Receptor Blockers, and Beta-Blockers
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
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