|
Pronunciation |
|
(me
SAL a
meen) |
|
|
U.S. Brand
Names |
|
Asacol® Oral; Pentasa® Oral;
Rowasa®
Rectal |
|
|
Generic
Available |
|
No |
|
|
Synonyms |
|
5-Aminosalicylic Acid; 5-ASA; Fisalamine; Mesalazine |
|
|
Pharmacological Index |
|
5-Aminosalicylic Acid Derivative |
|
|
Use |
|
Oral: Remission and treatment of mildly to moderately active ulcerative
colitis
Rectal: Treatment of active mild to moderate distal ulcerative colitis,
proctosigmoiditis, or proctitis |
|
|
Pregnancy Risk
Factor |
|
B |
|
|
Contraindications |
|
Known hypersensitivity to mesalamine, sulfasalazine, sulfites, or
salicylates |
|
|
Warnings/Precautions |
|
Pericarditis should be considered in patients with chest pain; pancreatitis
should be considered in any patient with new abdominal complaints. Elderly may
have difficulty administering and retaining rectal suppositories. Given renal
function decline with aging, monitor serum creatinine often during therapy. Use
caution in patients with impaired hepatic function. |
|
|
Adverse
Reactions |
|
>10%:
Central nervous system: Headache, malaise
Gastrointestinal: Abdominal pain, cramps, flatulence, gas
1% to 10%: Dermatologic: Alopecia, rash
<1%: Anal irritation, acute intolerance syndrome (bloody diarrhea, severe
abdominal cramps, severe headache), pericarditis, fatal myocarditis,
hypersensitivity pneumonitis, allergic reactions, pancreatitis, nephrotic
syndrome, interstitial nephritis, hepatitis, aplastic anemia, pancytopenia,
leukopenia, agranulocytosis, anemia, elevated transaminases, LDH, alkaline
phosphatase, or bilirubin, jaundice, cholestatic jaundice, liver
necrosis/failure, Kawasaki-like syndrome |
|
|
Overdosage/Toxicology |
|
Symptoms of overdose include decreased motor activity, diarrhea, vomiting,
renal function impairment
Treatment is supportive; emesis, gastric lavage, and follow with activated
charcoal slurry |
|
|
Drug
Interactions |
|
Decreased effect: Decreased digoxin bioavailability |
|
|
Stability |
|
Unstable in presence of water or light; once foil has been removed, unopened
bottles have an expiration of 1 year following the date of
manufacture |
|
|
Mechanism of
Action |
|
Mesalamine (5-aminosalicylic acid) is the active component of sulfasalazine;
the specific mechanism of action of mesalamine is unknown; however, it is
thought that it modulates local chemical mediators of the inflammatory response,
especially leukotrienes; action appears topical rather than
systemic |
|
|
Pharmacodynamics/Kinetics |
|
Absorption: Rectal: ~15%; variable and dependent upon retention time,
underlying GI disease, and colonic pH
Metabolism: In the liver by acetylation to acetyl-5-aminosalicylic acid
(active) and to glucuronide conjugates; intestinal metabolism may also occur
Half-life: 5-ASA: 0.5-1.5 hours; Acetyl 5-ASA: 5-10 hours
Time to peak serum concentration: Within 4-7 hours
Elimination: Most metabolites are excreted in urine with <2% appearing in
feces |
|
|
Usual Dosage |
|
Adults (usual course of therapy is 3-6 weeks):
Capsule: 1 g 4 times/day
Tablet: 800 mg 3 times/day
Retention enema: 60 mL (4 g) at bedtime, retained overnight, approximately 8
hours
Rectal suppository: Insert 1 suppository in rectum twice daily
Some patients may require rectal and oral therapy concurrently
|
|
|
Mental Health: Effects
on Mental Status |
|
Malaise is common |
|
|
Mental Health:
Effects on Psychiatric
Treatment |
|
None reported |
|
|
Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
|
No information available to require special precautions |
|
|
Dental Health:
Effects on Dental Treatment |
|
No effects or complications reported |
|
|
Patient
Information |
|
Take as directed. Oral: Do not chew or break tablets. Enemas: Shake well
before using, retain for 8 hours or as long as possible. Suppository: After
removing foil wrapper, insert high in rectum without excessive handling (warmth
will melt suppository). You may experience flatulence, headache, or hair loss
(reversible). Report abdominal pain, unresolved diarrhea, severe headache, or
chest pain. Breast-feeding precautions: Consult prescriber if
breast-feeding. |
|
|
Nursing
Implications |
|
Provide patient with copy of mesalamine administration
instructions |
|
|
Dosage Forms |
|
Capsule, controlled release (Pentasa®): 250 mg
Suppository, rectal (Rowasa®): 500 mg
Suspension, rectal (Rowasa®): 4 g/60 mL (7s)
Tablet, enteric coated (Asacol®): 400 mg
|
|
|
References |
|
Grand RJ, Ramakrishna J, and Calenda KA,
"Inflammatory Bowel Disease in the Pediatric Patient," Gastroenterol Clin
North Am, 1995, 24(3):613-32.
|
|
Copyright © 1978-2000 Lexi-Comp Inc. All Rights Reserved
|