Friday, March 1, 2013

MESALAMINE


MESALAMINE is also known as Mesalazine.  or 5-aminosalicylic acid (5-ASA), is an anti-inflammatory drug used to treat inflammatory bowel disease, such as ulcerative colitis and mild-to-moderate Crohn's disease. Mesalazine is a bowel-specific aminosalicylate drug that acts locally in the gut and has its predominant actions there, thereby having few systemic side effects.

5-amino-2-hydroxybenzoic acid

As a derivative of salicylic acid, mesalazine is also thought to be an antioxidant that traps free radicals, which are potentially damaging byproducts of metabolism.
Mesalazine is considered the active moiety of sulfasalazine, which is metabolized to sulfapyridine and mesalazine.

Mesalamine is used to treat ulcerative colitis (a condition in which part or all of the lining of the colon [large intestine] is swollen or worn away). Mesalamine delayed-release tablets and controlled-release capsules may be used to treat ulcerative colitis that affects any part of the colon. Mesalamine suppositories and enemas should only be used to treat inflammation of the lower part of the colon. Mesalamine is in a class of medications called anti-inflammatory agents. It works by stopping the body from producing a certain substance that may cause pain or inflammation.


Mesalamine comes as a delayed-release tablet and a controlled-release capsule to take by mouth and as a suppository and an enema to use in the rectum. The delayed-release tablet is usually taken three times a day, and the controlled-release capsule is usually taken four times a day. The suppository is usually used one to three times a day, and the enema is usually used once a day at bedtime. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take or use mesalamine exactly as directed. Do not take or use more or less of it or take or use it more often than prescribed by your doctor.

Swallow the tablets whole; do not split, chew, or crush them. Be careful not to break the protective coating on the tablets.

If you are unable to swallow the capsules, you may mix the contents of the capsules with water. Open a capsule and sprinkle all of the beads it contains in a small glass of water. Stir the beads into the water and drink the mixture right away. Do not store mixtures of beads and water for later use.

The enema and suppositories are for rectal use only.

You should begin to feel better during the first few days or weeks of your treatment with mesalamine. Continue to take or use mesalamine until you finish your prescription, even if you feel better at the beginning of your treatment. Do not stop taking or using mesalamine without talking to your doctor.

Mesalamine suppositories and enemas may stain clothing, flooring, fabric and other surfaces. Take precautions to prevent staining when you use these medications.

If you are to use the enema, follow these steps:
Try to have a bowel movement. The medication will work best if your bowels are empty.

Use scissors to cut the seal of the protective foil pouch that holds seven bottles of medication. Be careful not to squeeze or cut the bottles. Remove one bottle from the pouch.

Look at the liquid inside the bottle. It should be off-white or tan colored. The liquid may darken slightly if the bottles are left out of the foil pouch for a time. You may use liquid that has darkened a little bit, but do not use liquid that is dark brown.

Shake the bottle well to make sure the medication is mixed.

Remove the protective cover from the applicator tip. Be careful to hold the bottle by the neck so that the medication will not leak out of the bottle.

Lie on your left side with your lower (left) leg straight and your right leg bent toward your chest for balance. You can also kneel on a bed, resting your upper chest and one arm on the bed.

Gently insert the applicator tip into your rectum, pointing it slightly toward your navel (belly button). If this causes pain or irritation, try putting a small amount of personal lubricating jelly or petroleum jelly on the tip of the applicator before you insert it.

Hold the bottle firmly and tilt it slightly so that the nozzle is aimed toward your back. Squeeze the bottle slowly and steadily to release the medicine.

Withdraw the applicator. Remain in the same position for at least 30 minutes to allow the medicine to spread through your intestine. Try to keep the medicine inside of your body for about 8 hours (while you sleep).

Throw away the bottle in a trash can that is out of the reach of children and pets.Each bottle contains only one dose and should not be reused.

If you are to use the suppository, follow these steps:
Try to have a bowel movement just before using the suppository. The medication will work best if your bowels are empty.

Separate one suppository from the strip of suppositories. Hold the suppository upright and use your fingers to peel off the plastic wrapper. Try to handle the suppository as little as possible to avoid melting it with the heat of your hands.

You may put a small amount of personal lubricant jelly or Vaseline on the tip of the suppository so that it will be easier to insert.

Lie down on your left side and raise your right knee to your chest. (If you are left-handed, lie on your right side and raise your left knee.)

Using your finger, insert the suppository into the rectum, pointed end first. Use gentle pressure to insert the suppository completely. Try to keep it in place for 1 to 3 hours or longer if possible.

Wash your hands thoroughly before you resume your normal activities.

Before taking or using mesalamine,you should follow the special precautions -
tell your doctor and pharmacist if you are allergic to mesalamine, balsalazide (Colazal); olsalazine (Dipentum); salicylate pain relievers such as aspirin, choline magnesium trisalicylate, choline salicylate (Arthropan), diflunisal (Dolobid), magnesium salicylate (Doan's, others), and salsalate; sulfasalazine (Azulfidine) or any other medications. If you will be using mesalamine enemas, tell your doctor if you are allergic to sulfites (substances used as food preservatives and found naturally in some foods) or any foods, dyes, or preservatives. Also tell your doctor if you are allergic to any of the ingredients in the type of mesalamine you will be using. Ask your pharmacist for a list of the ingredients.
tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following: aspirin or other nonsteroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen (Advil, Motrin) and naproxen (Aleve, Naprosyn); digoxin (Lanoxicaps, Lanoxin); or other medications for ulcerative colitis such as balsalazide (Colazal), olsalazine (Dipentum), or sulfasalazine (Azulfidine). Your doctor may need to change the doses of your medications or monitor you more carefully for side effects.
tell your doctor if you have or have ever had pancreatitis (swelling of the pancreas), pericarditis (swelling of the sac around the heart), or liver or kidney disease. If you will be taking the delayed-release tablets, tell your doctor if you have or have ever had pyloric stenosis (condition in which the stomach does not empty normally). If you will be using the enemas, tell your doctor if you have asthma or allergies.
tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking or using mesalamine, call your doctor.
you should know that mesalamine may cause a serious reaction. Many of the symptoms of this reaction are similar to the symptoms of ulcerative colitis, so it may be difficult to tell if you are experiencing a reaction to the medication or a flare (episode of symptoms) of your disease. Call your doctor if you experience some or all of the following symptoms: stomach pain or cramping; bloody diarrhea; fever; headache; weakness; rash; or red, irritated eyes.

If you forgot one dose  -  Take or use the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take or use a double dose to make up for a missed one.

In case of overdose, call your local poison control center at 1-800-222-1222. If the victim has collapsed or is not breathing, call local emergency services at 911.






GIT Regulators, Antiflatulents & Anti-Inflammatories

Dose indications    -    Adult: PO Ulcerative colitis Dose is dependant on preparation and brand used. Pentasa® tab: Acute attack: Initially, up to 4 g/day in 2-3 divided doses; maintenance of remission: Initially, 1.5 g/day in 2-3 divided doses, adjust subsequently based on response. Pentasa® granules: Acute attack: Initially, up to 4 g/day in 2-4 doses; maintenance of remission: 2 g/day in 2 divided doses. Asacol® tab: Acute attack: Initially, 2.4 g/day in divided doses; maintenance of remission: 1.2-2.4 g/day in divided doses. Salofalk® tab: Acute attack: Initially, 1.5 g/day in 3 divided doses; maintenance of remission: 0.75-1.5 g/day in divided doses. Salofalk® granules: Acute attack: Initially, 1.5-3 g/day in 1-3 divided doses; maintenance of remission: 1.5 g/day in 3 divided doses. Rectal Ulcerative proctitis Pentasa® supp or suspension enema: 1 g/day. Asacol® supp: 0.75-1.5 g/day in divided doses; Asacol ® foam enema: 1 or 2 g/day depending on the disease location. Salofalk® supp: 0.5-1 g 2-3 times/day; Salofalk® foam or suspension enema: 2 g/day.
Oral
Ulcerative colitis
Adult: Dose is dependant on preparation and brand used. Pentasa® tablets: Acute attack: Initially, up to 4 g daily in 2-3 divided doses; maintenance of remission: Initially, 1.5 g daily in 2-3 divided doses, adjust subsequently based on response. Pentasa® granules: Acute attack: Initially, up to 4 g daily in 2-4 doses; maintenance of remission: 2 g daily in 2 divided doses. Asacol® tablets: Acute attack: Initially, 2.4 g daily in divided doses; maintenance of remission: 1.2-2.4 g daily in divided doses. Salofalk® tablets: Acute attack: Initially, 1.5 g daily in 3 divided doses; maintenance of remission: 0.75-1.5 g daily in divided doses. Salofalk® granules: Acute attack: Initially, 1.5-3 g daily in 1-3 divided doses; maintenance of remission: 1.5 g daily in 3 divided doses.
Child: Dose is dependant on preparation and brand used. Pentasa® tablets: 5-15 yr: Acute attack: 15-20 mg/kg (max: 1 g) tid; maintenance of remission: 10 mg/kg (max: 500 mg) 2-3 times daily. Pentasa® granules: 5-12 yr: Acute attack: 15-20 mg/kg (max: 1 g) tid; maintenance of remission: 10 mg/kg (max: 500 mg) 2-3 times daily. Asacol® tablets: 12-18 yr: Acute attack: Initially, 2.4 g daily in divided doses; maintenance of remission: 1.2-2.4 g daily in divided doses. Salofalk® tablets: 12-18 yr: Acute attack: Initially, 1.5 g daily in 3 divided doses; maintenance of remission: 250-500 mg 2-3 times daily. Salofalk® granules: 6-12 yr: Acute attack: 10-15 mg/kg (max: 1 g) tid; maintenance of remission: 7.5-15 mg/kg (max: 500 mg) bid or 250 mg tid for patients weighing <40 kg.="" p="">

Hepatic impairment: Avoid in severe impairment.
Rectal
Ulcerative proctitis
Adult: Pentasa® suppository or suspension enema: 1 g daily. Asacol® suppository: 0.75-1.5 g daily in divided doses; Asacol ® foam enema: 1 g daily if disease affects the rectosigmoid regions or 2 g daily if disease affects the descending colon. Salofalk® suppository: 0.5-1 g bid-tid; Salofalk® foam or suspension enema: 2 g daily.
Child: As suppository: Pentasa®: 12-18 yr: 1 g daily for 2-4 wk. Salofalk®: 12-18 yr: 0.5-1 g bid-tid according to respons

Contraindications             Hypersensitivity to mesalazine, salicylates and sulfasalazine. Severe impaired renal (CrCl < 20 ml/min) or hepatic function. Children <2 p="" yr.="">

Special Precautions         Mild to moderate impaired renal or hepatic function (test serum creatinine before treatment, every 3 mth for 1st yr, every 6 mth for next 4 yr, then annually). Elderly; active peptic ulcer; pregnancy, lactation; patients predisposed to pericarditis or myocariditis. Counsel patients to report any unexplained bleeding, bruising, purpura, sore throat, fever or malaise during treatment; perform blood count and stop treatment if blood dyscrasias suspected. Counsel patients taking delayed release tablets to report repeatedly unbroken or partially broken tablets in their faeces. Pyloric stenosis may delay release into colon.

Adverse Drug Reactions                Abdominal pain (if new abdominal pain - consider pancreatitis); headache, nausea; flu; fatigue; fever, rash; sore throat; diarrhoea; joint pain; dizziness; bloating; back pain; haemorrhoids; itching; rectal pain, constipation; hair loss; intolerance syndrome; peripheral oedema; UTI; myocarditis, pre-existing pericarditis; pancreatitis; nephritis; hepatitis; lupus-like syndrome; alopecia; myalgia, arthralgia; increased liver enzyme values.

Potentially Fatal: Blood dyscrasias, aplastic anaemia, agranulocytosis; renal toxicity.

Drug Interactions -   Do not give with lactulose or other drugs which lower pH for they prevent release of mesalazine. May decrease digoxin absorption.

PREGNANCY   -   Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

Storage                Oral: Tablets: store at below 25°C. Capsule: protect from light and store at 15-30°C. Rectal: Store <25 and="" be="" direct="" do="" freeze.="" from="" heat="" humidity.="" light="" may="" not="" p="" protect="" refrigerated="">

Mechanism of Action     Mesalazine is considered to be the active moiety of sulfasalazine. The mechanism of action is uncertain, but may be due to its ability to inhibit local chemical mediators of the inflammatory response especially leukotriene synthesis in the GI mucosa. Action may be topical in terminal ileum and colon rather than systemic.
Absorption: Absorption variable, depending on formulation and route of admin.
Distribution: Enters breast milk and crosses placenta (small amounts) after oral dosing; protein-binding: 40-80%. Distribution into other tissues: variable depending on route of admin.
Metabolism: Exact metabolism pathways not established. Main site of metabolism is probably liver with some N-acetylation occurring in the intestinal wall and/or lumen (where intestinal flora are involved in the acetylation).
Excretion: Dependant upon route of admin. Eliminated via urine <8 and="" as="" faeces="" metabolites="" p="" unchanged="">


UK: Asacol, Ipocal, Pentasa, Salofalk, Mezavant XL
Ireland: Asacolon, Pentasa, Salofalk, Mezavant XL
France: Asacol, Pentasa, Mezavant
US: Canasa, Rowasa, Pentasa, Asacol, Lialda, Apriso, Salofalk
Canada: Asacol, Pentasa, Salofalk, Mezavant
India: Mesacol, VEGAZ-OD.
Mexico: Salofalk
Serbia: Salofalk
Uruguay: Mesacron, Mesalazina
Brazil: Mesalazina, Mesalazina Enema, Mesacol, Mesacol MNX, Asalit,
Australia: Mesasal





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