Mesalamine 4gm Kit( 7 X 60ml)

Manufacturer PERRIGO PHARMACEUTICALS Active Ingredient Mesalamine Rectal Enema(me SAL a meen) Pronunciation me SAL a meen
It is used to treat mild to moderate disease at the far end of the colon.It may be given to you for other reasons. Talk with the doctor.
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Drug Class
Anti-inflammatory agent
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Pharmacologic Class
5-aminosalicylic acid (5-ASA) derivative
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Pregnancy Category
Category B
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FDA Approved
Jul 1987
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Mesalamine rectal enema is a medication used to treat inflammation in the lower part of your large intestine (colon) and rectum, a condition called ulcerative proctosigmoiditis. It works by reducing inflammation directly where it's needed.
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How to Use This Medicine

Proper Use of This Medication

To use this medication correctly, follow your doctor's instructions and read all the information provided. This medication is designed for rectal use only and should not be taken by mouth. You may be prescribed both an oral tablet or capsule and a rectal product to use simultaneously.

Continue using this medication as directed by your doctor or healthcare provider, even if you start feeling well. It is recommended to use this medication at bedtime. Before using, make sure you understand the proper technique. If you have any questions, consult your doctor or pharmacist.

For the suspension form, shake the container well before use. Retain the suspension in your rectum for as long as possible. Note that the enema may darken slightly over time after opening the foil pouch, but it can still be used if the color change is minimal. However, do not use the enema if it has turned dark brown. If you are unsure about the enema's viability, consult your doctor or pharmacist.

Storage and Disposal

Store this medication at room temperature. Keep the rectal suspension in its foil packaging until you are ready to use it, and avoid refrigeration. Protect the rectal suspension from heat sources.

Missed Dose

If you miss a dose, take it as soon as you remember. However, if it is close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to compensate for a missed dose.
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Lifestyle & Tips

  • Administer the enema at bedtime, if possible, to allow the medication to remain in the rectum for several hours.
  • Lie on your left side with your lower leg extended and your upper leg bent forward for administration, or in a knee-chest position.
  • Try to retain the enema for at least 1-3 hours, or preferably overnight (8 hours), for best results.
  • Maintain adequate hydration.
  • Follow your doctor's dietary recommendations for ulcerative colitis.

Dosing & Administration

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Adult Dosing

Standard Dose: 4 grams (one 60 mL enema) rectally once daily at bedtime
Dose Range: 4 - 4 mg

Condition-Specific Dosing:

ulcerativeProctosigmoiditis: 4 grams (one 60 mL enema) rectally once daily at bedtime for 3 to 6 weeks.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established
Adolescent: Not established (safety and efficacy not established in pediatric patients)
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Dose Adjustments

Renal Impairment:

Mild: Use with caution; monitor renal function.
Moderate: Use with caution; monitor renal function. Consider dose reduction or discontinuation if renal impairment worsens.
Severe: Contraindicated in patients with severe renal impairment.
Dialysis: Not recommended; systemic absorption occurs, and accumulation may lead to toxicity. Avoid use.

Hepatic Impairment:

Mild: Use with caution; monitor liver function.
Moderate: Use with caution; monitor liver function. Consider dose reduction.
Severe: Use with caution; monitor liver function. Avoid if possible due to potential for hepatotoxicity.

Pharmacology

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Mechanism of Action

Mesalamine (5-aminosalicylic acid) is thought to exert its anti-inflammatory effect locally in the colon. Its exact mechanism is unknown but is believed to involve inhibition of prostaglandin and leukotriene synthesis in the colon, scavenging of free radicals, and inhibition of inflammatory cell migration.
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Pharmacokinetics

Absorption:

Bioavailability: Low systemic absorption (approximately 10-30% from rectal administration)
Tmax: Systemic Tmax is variable, typically 4-12 hours for parent drug and metabolite after rectal administration.
FoodEffect: Not applicable for rectal administration.

Distribution:

Vd: Not precisely determined for rectal administration due to low systemic absorption; primarily acts locally.
ProteinBinding: Mesalamine: approximately 43%; N-acetyl-5-aminosalicylic acid (Ac-5-ASA): approximately 78-83%.
CnssPenetration: Limited

Elimination:

HalfLife: Mesalamine: 0.5-1.5 hours (systemic); Ac-5-ASA: 5-10 hours (systemic). Local half-life in colon is longer.
Clearance: Primarily renal clearance of parent drug and metabolite.
ExcretionRoute: Renal (primarily as metabolite), fecal (unabsorbed drug).
Unchanged: Less than 10% of absorbed mesalamine is excreted unchanged in urine.
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Pharmacodynamics

OnsetOfAction: Clinical improvement typically seen within 3-21 days.
PeakEffect: Peak therapeutic effect often observed within 3-6 weeks of daily use.
DurationOfAction: Maintained with continued daily administration for the duration of treatment course (e.g., 3-6 weeks).

Safety & Warnings

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Side Effects

Urgent Side Effects: Seek Medical Help Right Away

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor immediately or seek emergency medical attention:

Signs of an allergic reaction, such as:
+ Rash or hives
+ Itching or red, swollen, blistered, or peeling skin (with or without fever)
+ Wheezing or tightness in the chest or throat
+ Difficulty breathing, swallowing, or talking
+ Unusual hoarseness or swelling of the mouth, face, lips, tongue, or throat
Signs of kidney problems, including:
+ Inability to urinate or changes in urine output
+ Blood in the urine or significant weight gain
+ Back pain, abdominal pain, or blood in the urine (which may indicate a kidney stone)
Chest pain or pressure, rapid or irregular heartbeat
Fever, chills, sore throat, unexplained bruising or bleeding, or feeling extremely tired or weak
Rectal bleeding or pain
Symptoms that may resemble ulcerative colitis, such as:
+ New or worsening stomach pain or cramps
+ Bloody stools
+ Fever
+ Headache
+ Itching or rash
+ Red or pink eyes
+ General feeling of illness
Signs of liver problems, which can be rare but potentially life-threatening:
+ Dark urine
+ Fatigue
+ Decreased appetite
+ Nausea or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Signs of heart problems, which can be rare but potentially life-threatening:
+ Shortness of breath
+ Significant weight gain
+ Swelling in the arms or legs
Severe skin reactions, including:
+ Stevens-Johnson syndrome (SJS)
+ Toxic epidermal necrolysis (TEN)
+ Other serious reactions that can affect body organs and be life-threatening
+ Symptoms may include:
- Red, swollen, blistered, or peeling skin
- Red or irritated eyes
- Sores in the mouth, throat, nose, eyes, genitals, or skin
- Fever
- Chills
- Body aches
- Shortness of breath
- Swollen glands

Other Possible Side Effects

Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects, contact your doctor if they bother you or do not resolve:

Constipation
Diarrhea
Stomach pain or upset stomach
Vomiting
Heartburn
Gas
Burping
Nose or throat irritation
Dizziness or headache
Back pain
Cough
* Rectal irritation

This is not an exhaustive list of possible side effects. If you have questions or concerns, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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Seek Immediate Medical Attention If You Experience:

  • Worsening of abdominal pain or bloody diarrhea (may indicate acute intolerance syndrome)
  • New or worsening kidney problems (e.g., decreased urination, swelling in legs/feet)
  • New or worsening liver problems (e.g., yellowing of skin/eyes, dark urine, severe nausea/vomiting)
  • Signs of an allergic reaction (e.g., rash, hives, difficulty breathing, swelling of face/lips/tongue)
  • Unexplained bleeding, bruising, fever, sore throat, or unusual tiredness (signs of blood problems)
  • Chest pain, shortness of breath, or new onset of fever (rare heart inflammation)
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Before Using This Medicine

Before Taking This Medication: Important Information to Share with Your Doctor

It is essential to inform your doctor about the following:

Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
Existing health conditions, including:
+ Kidney disease or liver disease
+ Stomach or bowel ulcers
+ Narrowing of the stomach valve or other types of stomach blockages
+ Blockages in the urinary tract (consult with your healthcare provider)
Other medications you are taking, including:
+ Prescription and over-the-counter (OTC) drugs
+ Natural products
+ Vitamins
Any health problems you have, as this is not an exhaustive list of potential interactions with this medication.

To ensure your safety, it is crucial to verify that it is safe to take this medication with all your existing medications and health conditions. Never start, stop, or change the dosage of any medication without consulting your doctor.
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Precautions & Cautions

It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Regular blood tests will be necessary, as directed by your doctor, to monitor your condition. Be sure to discuss any concerns or questions with your doctor.

This medication may interfere with certain laboratory tests, so it is crucial to notify all your healthcare providers and laboratory personnel that you are taking this drug.

To stay hydrated, drink plenty of non-caffeinated fluids, unless your doctor advises you to limit your fluid intake. If you have a sulfite allergy, consult your doctor, as some products may contain sulfites.

While taking this medication, you may notice that your urine turns reddish-brown when it comes into contact with surfaces or water that have been treated with bleach, such as in a toilet. However, if you observe that your urine is reddish-brown before it comes into contact with any surfaces or water, monitor your urine flow and contact your doctor if necessary.

You may be more susceptible to sunburn while taking this medication. To minimize this risk, avoid exposure to the sun, sunlamps, and tanning beds, and use sunscreen and protective clothing and eyewear when going outside.

If you are 65 years or older, use this medication with caution, as you may be more prone to side effects.

Not all formulations of this medication are suitable for children, so it is essential to consult your doctor before giving it to a child. Additionally, do not give this medication to children or teenagers who have or are recovering from flu symptoms, chickenpox, or other viral infections, as this may increase the risk of Reye's syndrome, a condition that can cause severe brain and liver damage.

Be aware that this medication may stain certain surfaces, including fabric, flooring, painted surfaces, marble, granite, vinyl, and enamel.

If you are pregnant, plan to become pregnant, or are breastfeeding, inform your doctor, as they will need to discuss the potential benefits and risks of this medication to you and your baby.
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Overdose Information

Overdose Symptoms:

  • Nausea
  • Vomiting
  • Abdominal pain
  • Headache
  • Drowsiness
  • Vertigo
  • Tinnitus
  • Confusion
  • Hyperventilation (rare, with very high systemic absorption)

What to Do:

There is no specific antidote. Treatment is symptomatic and supportive. Contact a poison control center immediately or seek emergency medical attention. Call 1-800-222-1222.

Drug Interactions

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Major Interactions

  • Azathioprine
  • Mercaptopurine (6-MP)
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Moderate Interactions

  • Nonsteroidal Anti-inflammatory Drugs (NSAIDs)
  • Nephrotoxic agents (e.g., tacrolimus, cyclosporine)

Monitoring

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Baseline Monitoring

Renal function (BUN, serum creatinine)

Rationale: To establish baseline and identify pre-existing renal impairment, as mesalamine can cause renal toxicity.

Timing: Prior to initiation of therapy.

Liver function tests (ALT, AST, bilirubin)

Rationale: To establish baseline and identify pre-existing hepatic impairment, as mesalamine can cause hepatotoxicity.

Timing: Prior to initiation of therapy.

Complete Blood Count (CBC) with differential

Rationale: To establish baseline and monitor for blood dyscrasias (rare).

Timing: Prior to initiation of therapy.

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Routine Monitoring

Renal function (BUN, serum creatinine)

Frequency: Periodically during treatment, especially in patients with known renal disease or those receiving concomitant nephrotoxic drugs. Annually for long-term use.

Target: Within normal limits or stable from baseline.

Action Threshold: Significant increase in creatinine or BUN; consider dose adjustment or discontinuation.

Liver function tests (ALT, AST, bilirubin)

Frequency: Periodically during treatment, especially if symptoms of hepatic dysfunction develop. Annually for long-term use.

Target: Within normal limits or stable from baseline.

Action Threshold: Significant elevation of liver enzymes; consider discontinuation.

Complete Blood Count (CBC) with differential

Frequency: Periodically during treatment, especially if unexplained bleeding, bruising, fever, or sore throat occur.

Target: Within normal limits.

Action Threshold: Significant decrease in blood counts (e.g., leukopenia, thrombocytopenia); consider discontinuation.

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Symptom Monitoring

  • Worsening of ulcerative colitis symptoms (e.g., increased rectal bleeding, diarrhea, abdominal pain)
  • Signs of renal dysfunction (e.g., decreased urine output, swelling in ankles/feet)
  • Signs of liver dysfunction (e.g., yellowing of skin/eyes, dark urine, persistent nausea/vomiting, abdominal pain)
  • Signs of hypersensitivity reaction (e.g., rash, fever, difficulty breathing, chest pain)
  • Signs of acute intolerance syndrome (e.g., cramping, acute abdominal pain, bloody diarrhea, fever, headache, rash)
  • Signs of blood dyscrasias (e.g., unexplained bruising, bleeding, persistent sore throat, fever)

Special Patient Groups

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Pregnancy

Generally considered safe for use during pregnancy. Studies in pregnant women have not shown an increased risk of fetal abnormalities. However, use only if clearly needed and potential benefits outweigh risks.

Trimester-Specific Risks:

First Trimester: Low risk; no increased risk of major birth defects observed.
Second Trimester: Low risk.
Third Trimester: Low risk; some reports of renal dysfunction in newborns with prolonged high-dose exposure, but rare with rectal administration.
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Lactation

Mesalamine and its metabolite are excreted in breast milk in small amounts. Generally considered compatible with breastfeeding, but monitor breastfed infant for diarrhea.

Infant Risk: Low risk; rare reports of diarrhea in breastfed infants. Monitor for changes in stool consistency.
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Pediatric Use

Safety and efficacy have not been established in pediatric patients. Use in children is off-label and typically reserved for specific cases under specialist supervision.

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Geriatric Use

Use with caution in elderly patients, as they are more likely to have decreased renal function. Monitor renal function closely. Start at the lower end of the dosing range.

Clinical Information

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Clinical Pearls

  • Mesalamine rectal enema is designed for local action in the rectum and sigmoid colon, making it highly effective for proctosigmoiditis with minimal systemic side effects.
  • Instruct patients to administer the enema at bedtime and try to retain it overnight for optimal efficacy.
  • Patients should be advised that the enema may stain clothing or bedding.
  • Monitor renal function, especially in patients with pre-existing kidney disease or those on concomitant nephrotoxic medications.
  • Acute intolerance syndrome (cramping, abdominal pain, bloody diarrhea, fever, headache, rash) is a rare but important adverse effect; if suspected, discontinue therapy immediately.
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Alternative Therapies

  • Mesalamine suppositories (for proctitis)
  • Oral mesalamine formulations (e.g., tablets, capsules)
  • Corticosteroid enemas or foams (e.g., hydrocortisone, budesonide)
  • Immunomodulators (e.g., azathioprine, mercaptopurine) for more severe or extensive disease
  • Biologic agents (e.g., infliximab, adalimumab) for moderate to severe disease
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Cost & Coverage

Average Cost: Varies widely, typically $100-$300+ per 7 enemas (4gm/60ml)
Generic Available: Yes
Insurance Coverage: Tier 2 or 3 (often preferred generic)
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General Drug Facts

If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it occurred.