me-SAL-a-meen

Therapeutic Classification: gastrointestinal anti-inflammatories

Delzicol, Lialda, and Pentasa:

• Treatment and maintenance of remission of mildly-to-moderately-active ulcerative colitis.

Apriso:

• Maintenance of remission of ulcerative colitis.

Canasa:

• Treatment of active ulcerative proctitis.

Rowasa:

• Treatment of active mild-to-moderate distal ulcerative colitis, proctosigmoiditis, or proctitis.

• Locally acting anti-inflammatory action in the colon, where activity is probably due to inhibition of prostaglandin synthesis.

• Reduction in the symptoms of ulcerative colitis, proctosigmoiditis, and proctitis.

Absorption: 28% absorbed following oral administration; 10–30% absorbed from the colon, depending on retention time, following rectal administration.

Distribution: Unknown.

Metabolism/Excretion: Some metabolism occurs, site unknown; mostly eliminated unchanged in the feces.

Half-life: Oral: 12 hr (range 2–15 hr); Rectal: 0.5–1.5 hr.

(clinical improvement)

Contraindicated in:

• Hypersensitivity reactions to sulfonamides, salicylates, mesalamine, or sulfasalazine
• Cross-sensitivity with furosemide, sulfonylureas, or carbonic anhydrase inhibitors may exist
• Hypersensitivity to bisulfites (mesalamine enema only)
• Urinary tract or intestinal obstruction
• Porphyria.

Use Cautiously in:

• Renal impairment
• Hepatic impairment
• Atopic dermatitis or atopic eczema (↑ risk of photosensitivity)
• Phenylketonuria (Apriso contains phenylalanine)
• OB: Use tablets only if potential benefits justify potential fetal risks (enteric coating contains dibutyl phthalate, which has been shown to cause congenital malformations in animals)
• Lactation: Use while breastfeeding only if potential maternal benefits justify potential risk to infant
• Geri: Older adults may have ↑ risk of agranulocytosis, neutropenia, and pancytopenia.

CV: pericarditis.

Derm: ACUTE GENERALIZED EXANTHEMATOUS PUSTULOSIS, DRUG REACTION WITH EOSINOPHILIA AND SYSTEMATIC SYMPTOMS (DRESS), hair loss, photosensitivity, rash, STEVENS-JOHNSON SYNDROME, TOXIC EPIDERMAL NECROLYSIS.

EENT: pharyngitis, rhinitis.

GI: diarrhea, eructation (PO), flatulence, HEPATOTOXICITY, nausea, pancreatitis, vomiting.

GU: interstitial nephritis, nephrolithiasis, renal impairment.

Local: anal irritation (enema, suppository).

MS: back pain, myalgia.

Neuro: headache, dizziness, malaise, weakness.
Misc: acute intolerance syndrome, fever, (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA)HYPERSENSITIVITY REACTIONS .

Drug-Drug:

• May ↑ myelosuppressive effects of mercaptopurine or azathioprine; avoid concurrent use, if possible.
• Concurrent use with NSAIDs may ↑ risk of nephrotoxicity.

Treatment of Ulcerative Colitis

• PO (Adults): 1.6 g (two 800-mg tablets) 3 times daily for 6 wk; Delzicol: 800 mg (two 400-mg capsules) 3 times daily for 6 wk; Lialda: 2.4–4.8 g (two to four 1.2-g tablets) once daily for up to 8 wk; Pentasa: 1 g (four 250-mg capsules or two 500-mg capsules) 4 times daily for up to 8 wk.
• Rect (Adults): Rowasa: 4-g enema (60 mL) at bedtime, retained for 8 hr for 3–6 wk.
• PO (Children 12 yr and 54–90 kg): Delzicol: 27–44 mg/kg/day in 2 divided doses (max dose = 2.4 g/day) for 6 wk.
• PO (Children 12 yr and 33–53 kg): Delzicol: 37–61 mg/kg/day in 2 divided doses (max dose = 2 g/day) for 6 wk.
• PO (Children 12 yr and 17–32 kg): Delzicol: 36–71 mg/kg/day in 2 divided doses (max dose = 1.2 g/day) for 6 wk.
• PO (Children >50 kg): Lialda: 4.8 g (four 1.2-g tablets) once daily for 8 wk, then 2.4 g (two 1.2–g tablets) once daily.
• PO (Children 36–50 kg): Lialda: 3.6 g (three 1.2-g tablets) once daily for 8 wk, then 2.4 g (two 1.2–g tablets) once daily.
• PO (Children 24–35 kg): Lialda: 2.4 g (two 1.2-g tablets) once daily for 8 wk, then 1.2 g once daily.

Maintenance of Remission of Ulcerative Colitis

• PO (Adults): Apriso: 1.5 g (four 375-mg capsules) once daily in the morning; Delzicol: 800 mg (two 400-mg capsules) 2 times daily; Lialda: 2.4 g (two 1.2-g tablets) once daily; Pentasa: 1 g (four 250-mg capsules or two 500-mg capsules) 4 times daily.

Treatment of Ulcerative Proctosigmoiditis

• Rect (Adults): Rowasa: 4-g enema (60 mL) at bedtime, retained for 8 hr (treatment duration = 3–6 wk).

Treatment of Ulcerative Proctitis

• Rect (Adults): Rowasa: 4-g enema (60 mL) at bedtime, retained for 8 hr (treatment duration = 3–6 wk); Canasa: Insert a 1-g suppository at bedtime, retain for at least 1–3 hr (treatment duration = 3–6 wk).

(Generic available)

• Delayed-release tablets: 400 mg; 500 mg; 800 mg; 1 g; 1.2 g (Lialda);
• Delayed-release capsules (Delzicol): 400 mg;
• Extended-release capsules (Apriso) (contain phenylalanine): 375 mg;
• Extended-release capsules (Pentasa): 250 mg; 500 mg;
• Rectal enema (Rowasa): 1 g/100 mL; 2 g/60 mL; 4 g/60 mL; 4 g/100 mL;
• Rectal foam: 1 g/actuation;
• Rectal suppository (Canasa): 500 mg; 1 g;

• Assess abdominal pain and frequency, quantity, and consistency of stools at the beginning of and during therapy.
• Assess for allergy to sulfonamides and salicylates. Patients allergic to sulfasalazine may take mesalamine or olsalazine without difficulty, but therapy should be discontinued if rash or fever occurs.
• Monitor intake and output ratios. Fluid intake should be sufficient to maintain a urine output of at least 1200–1500 mL daily to prevent crystalluria and stone formation.
• Monitor for signs and symptoms of acute intolerance syndrome (cramping, acute abdominal pain and bloody diarrhea, sometimes fever, headache, rash) during therapy; may be difficult to distinguish from an exacerbation of ulcerative colitis. If syndrome occurs, promptly discontinue therapy.

• Monitor urinalysis, BUN, and serum creatinine prior to and periodically during therapy. Mesalamine may cause renal toxicity. Discontinue mesalamine if renal functions declines.
  • Mesalamine may cause ↑ AST and ALT levels, serum alkaline phosphatase, GGT, LDH, amylase, and lipase.

• PO: Administer with a full glass of water. DNC: Swallow tablets whole; do not break the outer coating, which is designed to remain intact. Take Lialda tablets with a meal. Take Apriso capsules in the morning without regard to meals. Do not coadminister with antacids; may affect dissolution of the coating of the granules in Apriso capsules. Intact or partially intact tablets may occasionally be found in the stool. If this occurs repeatedly, advise patient to notify health care professional. DNC: Swallow Delzicol capsules whole; do not break, crush, or chew. Administer without regard to meals. If unable to swallow capsules, may open capsule and swallow inner tablets. Intact or partially intact tablets may occasionally be found in the stool. If this occurs repeatedly, advise patient to notify health care professional. Two Delzicol 400-mg capsules are not equal to one Asacol HD (mesalamine) delayed-release 800-mg tablet. Pentasa capsules may be swallowed whole or opened and sprinkled onto applesauce or yogurt. Consume entire contents immediately. DNC: Avoid crushing or chewing capsules and capsule contents.
• Rect: Patient should empty bowel prior to administration of rectal dose forms.
  • Avoid excessive handling of suppository. Remove foil wrapper and insert pointed end first into rectum with gentle pressure. Do not cut or break suppository. Retain suppository for 1–3 hr or more for maximum benefit.
  • Administer 60-mL retention enema once daily at bedtime. Solution should be retained for approximately 8 hr. Prior to administration of rectal suspension, shake bottle well and remove the protective cap. Have patient lie on left side with the lower leg extended and the upper leg flexed for support or place the patient in knee-chest position. Gently insert the applicator tip into the rectum, pointing toward the umbilicus. Squeeze the bottle steadily to discharge most of the preparation.

• Instruct patient on the correct method of administration. Advise patient to take medication as directed, even if feeling better. Take missed doses as soon as remembered unless almost time for next dose. Advise patient to read Patient Information before starting therapy and with each Rx refill in case of changes.
• Advise patient not to change brands of mesalamine without consulting health care professional.
• Encourage patient to drink an adequate amount of fluids to minimize risk of kidney stones and to notify health care professional if signs and symptoms of kidney stones (severe side or back pain, blood in urine) occur.
• May cause dizziness. Caution patient to avoid driving or other activities that require alertness until response to medication is known.
• Advise patient to notify health care professional if skin rash, sore throat, fever, mouth sores, unusual bleeding or bruising, wheezing, fever, or hives occur.
• Advise patient to avoid sun exposure, wear protective clothing, and use a broad-spectrum sunscreen when outdoors to decrease risk of photosensitivity.
• Instruct patient to notify health care professional if symptoms do not improve after 1–2 mo of therapy.
• Instruct patient to notify health care professional if symptoms worsen or do not improve. If symptoms of acute intolerance (cramping, acute abdominal pain, bloody diarrhea, fever, headache, rash) occur, discontinue therapy and notify health care professional immediately.
• Inform patient that proctoscopy and sigmoidoscopy may be required periodically during treatment to determine response.
• Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected, or if breastfeeding. Monitor breastfed infants for diarrhea.
• Rect: Instruct patient to use rectal suspension at bedtime and retain suspension all night for best results.

• Decrease in diarrhea and abdominal pain.
• Return to normal bowel pattern in patients with inflammatory bowel disease. Effects may be seen within 3–21 days. The usual course of therapy is 3–6 wk.
• Maintenance of remission in patients with inflammatory bowel disease.

Apriso, Asacol, Asacol HD, Canasa, Delzicol, Lialda, Pentasa, Rowasa

Mezavant, Mezera, Octasa, Salofalk, Teva 5–ASA