Dosing and uses of Dipentum (olsalazine)
Adult dosage forms and strengths
capsule
- 250mg
Ulcerative Colitis
Maintenance: 1g PO qDay in 2 divided doses
Administration
Take with food
Other Indications & Uses
Maintenance of remission of ulcerative colitis in patients who are intolerant of sulfasalazine
Pediatric dosage forms and strengths
Safety & efficacy not established
Dipentum (olsalazine) adverse (side) effects
>10%
Diarrhea (17%)
Abdominal pain (11%)
1-10%
Nausea/vomiting (6%)
Headache (5%)
Arthralgia (4%)
Dyspepsia (4%)
Joint pain (4%)
Rash/itching (3.6%)
Fatigue (1.8%)
Bloating (1.5%)
Depression (1.5%)
Upper respiratory infection (1.5%)
Anorexia (1.3%)
Dizziness (1%)
Warnings
Contraindications
Hypersensitivity to salicylates
Cautions
Kidney disease, hepatic impairment
Pregnancy and lactation
Pregnancy category: C
Lactation
Not known whether drug distributed into breast milk, use caution
5-ASA is excreted in breast milk & may cause diarrhea in infant
However little is absorbed from oral olsalazine
Avoid
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Dipentum (olsalazine)
Absorption: ~2.4% of a single 1 g dose
Peak Plasma (single 1 g dose)
Olsalazine: 1.6-6.2 umol/L
5-aminosalicylic acid (5-ASA): 0-4.3umol/L
N-acetyl-5-ASA: 1.7-8.7 umol/L
Half-Life
Olsalazine: 0.9 hr
5-ASA: 45 min
N-Ac-5-ASA: 80 min
Olsalazine-S (~0.1%): 7 d
Metabolism
>90% converted to 5-ASA in the gut
5-ASA is deactivated to N-Ac-5-ASA in colonic epithelium & liver
Approx. 0.1% converted to olsalazine-O-sulfate (Olsalazine-S) in liver
Excretion
Urine: 20% (mostly N-Ac-5-ASA)
Feces: 80% (both 5-ASA & N-Ac-5-ASA)
Other Information
Protein Bound: 99%
Mechanism of action
Converted to 5-aminosalicylic acid (mesalamine) by gastrointestinal flora which is thought to be the therapeutically active component; works topically rather tha systemically
