Mecolzine
Mecolzine Uses, Dosage, Side Effects, Food Interaction and all others data.
Although the mechanism of action of mesalazine is not fully understood, it appears to be topical rather than systemic. Mucosal production of arachidonic acid metabolites, both through the cyclooxygenase pathways, i.e., prostanoids, and through the lipoxygenase pathways, i.e., leukotrienes and hydroxyeicosatetraenoic acids, is increased in patients with chronic inflammatory bowel disease, and it is possible that mesalazine diminishes inflammation by blocking cyclooxygenase and inhibiting prostaglandin production in the colon.
Mecolzine is one of the two components of sulphasalazine, the other being sulphapyridine. It is the latter which is responsible for the majority of the side effects associated with sulphasalazine therapy whilst mesalazine is known to be the active moiety in the treatment of ulcerative colitis .
The pharmacodynamic actions of mesalazine occur in the colonic/rectal mucosae local to the delivery of drug from mesalazine tablets into the lumen . There is information suggesting that the severity of colonic inflammation in ulcerative colitis patients treated with mesalazine is inversely correlated with mucosal concentrations of mesalazine . Plasma concentrations representing systemically absorbed mesalazine are not believed to contribute extensively to efficacy .
| Trade Name | Mecolzine |
| Generic | Mesalazine |
| Mesalazine Other Names | 5-aminosalicylic acid, 5-ASA, m-Aminosalicylic acid, Mesalamine, Mesalazina, Mésalazine, Mesalazine, Mesalazinum, p-Aminosalicylsaeure |
| Type | |
| Formula | C7H7NO3 |
| Weight | Average: 153.1354 Monoisotopic: 153.042593095 |
| Protein binding | Mesalazine is approximately 43% bound to plasma proteins , . |
| Groups | Approved |
| Therapeutic Class | Anti-Tubercular Chemotherapeutics, Ulcerative Colitis |
| Manufacturer | |
| Available Country | Chile |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
This medication is used to treat a certain bowel disease (ulcerative colitis). It helps to reduce symptoms of ulcerative colitis such as diarrhea, rectal bleeding, and stomach pain. Mesalamine belongs to a class of drugs known as aminosalicylates.This medication may also be used to treat Crohn's disease.
Mecolzine is also used to associated treatment for these conditions: Crohn's Disease (CD), Proctitis, Ulcerative, Proctosigmoiditis, Ulcerative Colitis
How Mecolzine works
Although the mechanism of action of mesalazine is not fully understood, it is believed to possess a topical anti-inflammatory effect on colonic epithelial cells . Mucosal production of arachidonic acid metabolites, both through the cyclooxygenase pathways, i.e., prostanoids, and through the lipoxygenase pathways, i.e., leukotrienes and hydroxyeicosatetraenoic acids, is increased in patients with chronic inflammatory bowel disease, and it is possible that mesalazine diminishes inflammation by blocking cyclooxygenase and inhibiting prostaglandin production in the colon .
Furthermore, mesalazine also has the potential to inhibit the activation of Nuclear Factor kappa B (NKkB) and consequently the production of key of pro-inflammatory cytokines . It has been proposed that reduced expression of PPAR gamma nuclear receptors (gamma form of peroxisome proliferator-activated receptors) may be implicated in ulcerative colitis . There is evidence that mesalazine produces pharmacodynamic effects through direct activation of PPAR gamma receptors in the colonic/rectal epithelium as well .
Moreover, since increased leukocyte migration, abnormal cytokine production, increased production of arachidonic acid metabolites, particularly leukotriene B4, and increased free radical formation in the inflamed intestinal tissue are all present in patients with inflammatory bowel disease it is also believed that mesalazine has in-vitro and in-vivo pharmacological effects that inhibit leukocyte chemotaxis, decrease cytokine and leukotriene production and scavenge for free radicals .
Dosage
Mecolzine dosage
Adult:
- Acute attack: Initially, up to 4 gm/day in 2-3 divided doses
- Maintenance of remission: Initially, 1.5 gm/day in 2-3 divided doses, adjust subsequently based on response.
Child (5-15 year):
- Acute attack: 15-20 mg/kg (max: 1 gm) tid
- Maintenance of remission: 10 mg/kg (max: 500 mg) 2-3 times daily.
Should be taken on an empty stomach: Take 1 hr before meals. Swallow whole, do not chew/crush.
Side Effects
Abdominal pain, diarrhea, flatulence, nausea, vomiting. Tab: Renal impairment, acute & chronic interstitial nephritis, renal insufficiency; exanthema, drug fever, bronchospasm, pericarditis & myocarditis, pancreatitis, allergic & fibrotic lung reactions including dyspnoea, cough, alveolitis, pulmonary eosinophilia, lung infiltration, pneumonitis, butterfly rash (lupus erythematosus syndrome), pancolitis; myalgia, arthralgia; aplastic anaemia, agranulocytosis, pancytopenia, neutropenia, leucopenia, thrombocytopenia; raised transaminase & parameters of cholestasis, hepatitis, cholestatic hepatitis; alopecia; reversible oligospermia. Enema: Allergic exanthema, drug fever; bronchospasm; lupus erythematosus-like syndrome. Granules: Headache, dizziness; pericarditis. Supp: Allergic skin rash, fever, breathing difficulty.
Toxicity
Oral, mouse: LD50 = 3370 mg/kg; Oral, rat: LD50 = 2800 mg/kg; Skin, rabbit: LD50 = >5 gm/kg .
There have been no documented reports of serious toxicity in man resulting from massive overdosing with mesalamine. Under ordinary circumstances, mesalazine absorption from the colon is limited. Although there is little to no clinical experience with mesalazine overdosage . Mecolzine is an aminosalicylate, and symptoms of salicylate toxicity may be possible, such as tinnitus, vertigo, headache, confusion, drowsiness, sweating, hyperventilation, vomiting, and diarrhea . Severe intoxication with salicylates can lead to disruption of electrolyte balance and blood-pH, hyperthermia, and dehydration .
Precaution
Use with caution, usually starting at the low end of the dosage range, because of the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant diseases or other drug therapy.
Hypersensitivity: Some patients who have experienced a hypersensitivity reaction to sulfasalazine may have a similar reaction to mesalamine.
Renal Function: Patients with history of renal function impairment or disease may have worsening of renal function.
Hepatic Function: Use with caution. There have been reports of hepatic failure in patients with preexisting liver disease.
Sulfite Sensitivity: Some products may contain sulfites, which may cause allergic reactions in susceptible individuals.
Interaction
Antacids: Because the dissolution of the coating of Apriso granules depends on pH, do not administer with antacids.
Nephrotoxic agents (including NSAIDs): Increased risk of renal adverse reactions.
Thiopurines (eg, azathioprine, mercaptopurine): Risk of leukopenia may be increased.
Warfarin: Decreased anticoagulant effect of warfarin has been reported in 1 patient.
Laboratory Test Interactions: None well documented.
Food Interaction
- Take with or without food. The absorption is unaffected by food.
Volume of Distribution
The apparent volume of distribution (Vd) of the drug in adults is approximately 0.2 L/kg .
Elimination Route
Depending on the formulation administered, prescribing information for orally administered delayed-released tablets of 2.4g or 4.8g of mesalazine given once daily for 14 days to healthy volunteers was to found to be about 21% to 22% of the administered dose while prescribing information for an orally administered controlled-release capsule formulation suggests 20% to 30% of the mesalazine in the formulation is absorbed . In contrast, when mesalamine is administered orally as an unformulated 1-g aqueous suspension, mesalazine is approximately 80% absorbed .
Half Life
The apparent elimination half-life documented for oral delayed-release mesalazine tablets is 7 to 12 hours . The elimination half-life recorded for the active N-acetyl-5-aminosalicylic acid metabolite generated from the administration of oral delayed-release mesalazine tablets is 12 to 23 hours .
Clearance
The mean (SD) renal clearance in L/h for mesalazine following the single dose administration of mesalazine delayed-release tablets 4.8g under fasting conditions to young and elderly subjects was documented as 2.05 (1.33) in young subjects aged 18 to 35 years old, 2.04 (1.16) in elderly subjects aged 65 to 75 years old, and 2.13 (1.20) in elderly subjects older than 75 years .
Elimination Route
Elimination of mesalazine is mainly via the renal route following metabolism to N-acetyl-5-aminosalicylic acid (acetylation) . However, there is also limited excretion of the parent mesalazine drug in the urine .
After the oral administration of the extended-release formulation of mesalazine, of the approximately 21% to 22% of the drug absorbed, less than 8% of the dose was excreted unchanged in the urine after 24 hours, compared with greater than 13% for N-acetyl-5-aminosalicylic acid .
When given the controlled-release formulation, about 130 mg free mesalazine was recovered in the feces following a single 1-g dose, which was comparable to the 140 mg of mesalazine recovered from the molar equivalent sulfasalazine tablet dose of 2.5 g F3001]. Elimination of free mesalazine and salicylates in feces increased proportionately with the dose given. N-acetylmesalazine was the primary compound excreted in the urine (19% to 30%) following the controlled-release dosing .
Pregnancy & Breastfeeding use
Pregnancy Category B. 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).
Lactation: Excreted in breast milk.
Contraindication
Hypersensitivity to salicylates, aminosalicylates, or any component of the product.
Special Warning
Renal Impairment: CrCl <20 Dosage Avoid.
Hepatic Impairment: Avoid in severe impairment.
Acute Overdose
Products are salicylates; symptoms of salicylate toxicity may include confusion, deafness, dehydration, diarrhea, drowsiness, dyspnea, electrolyte and blood pH imbalance, headache, hematemesis, hyperpnea, hyperthermia, hyperventilation, lethargy, seizures, sweating, tachypnea, tinnitus, vertigo, vomiting.
Storage Condition
Tablet: store at below 25° C.
Capsule: protect from light and store at 15-30° C.
Innovators Monograph
You find simplified version here Mecolzine
Mecolzine contains Mesalazine see full prescribing information from innovator Mecolzine Monograph, Mecolzine MSDS, Mecolzine FDA label
FAQ
What is Mecolzine used for?
Mecolzine is used to treat ulcerative colitis and Crohn's disease and other types of inflammatory bowel disease. Mecolzine is a medication used to treat inflammatory bowel disease, including ulcerative colitis and Crohn's disease. It is generally used for mildly to moderately severe disease.
How safe is Mecolzine?
With these precautions in mind, Mecolzine can be used safely with excellent benefit in many patients with inflammatory bowel disease. High-dose Mecolzine appears to have similar safety profile as low dose, and is not associated with greater risk of adverse events.
How does Mecolzine work?
No one knows exactly how Mecolzine works. It is thought to act on the inflamed lining of the gut (intestine) by stopping the body producing chemicals that cause inflammation. Mecolzine helps by reducing the redness and swelling (inflammation) in your intestine. This improves your symptoms.
What are the common side effects of Mecolzine?
Common side effects of Mecolzine are include:
- muscle or joint pain, aching, tightness or stiffness
- back pain
- nausea
- vomiting
- heartburn
- burping
- constipation
- gas
- dry mouth
- itching
- dizziness
- sweating
- acne
- slight hair loss
- decreased appetite
Is Mecolzine safe during pregnancy?
The use of Mecolzine in pregnancy is safe. They are safe to continue during pregnancy.
Is Mecolzine safe during breastfeeding?
Small amounts of Mecolzine have been found in breast milk, and in most cases where it has been used, there have not been any problems with the infants.
Can I drink alcohol with Mecolzine?
You can drink alcohol while taking Mecolzine. However, alcohol can irritate your gut so may make symptoms worse. It's best to stick to the national guidelines of no more than 14 units a week.
When should be taken of Mecolzine?
You will usually use Mecolzine enemas once a day before you go to bed.
Can I take Mecolzine on an empty stomach?
You may take this Mecolzine with or without food.
How much Mecolzine can I take daily?
Adults, 800 milligrams (mg) 3 times a day. Children 5 years of age and older. Dose is based on body weight and must be determined by your doctor. The dose is usually not more than 2400 mg per day, divided in 2 doses.
How long does Mecolzine take to work?
There is usually an improvement in 3 to 21 days. You may need about 6 weeks of treatment to get good results.
How long does Mecolzine stay in my system?
The medicine needs to remain in your body for 1 to 3 hours or longer, depending on your doctor's advice.
Can I take Mecolzine on an empty stomach?
Mecolzine can be taken long term.
How long can I take Mecolzine?
Mecolzine may take up to a few months for your symptoms to be completely treated if they are severe. Mecolzine can be used at a higher dose for a short time to treat flare-ups.
Who should not take Mecolzine?
You should not use Mecolzine if you are allergic to Mecolzine.Tell your doctor if you have ever had:a kidney stone or kidney disease; liver disease; a blockage in your stomach or intestines (such as pyloric stenosis); or a skin condition such as eczema.
When should I stop taking Mecolzine?
Stop using Mecolzine and call your doctor at once if you have severe stomach pain, stomach cramping, bloody diarrhea (may occur with fever, headache, and skin rash).
What happens if I miss a dose?
Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.
Can I overdose on Mecolzine?
Mecolzine containing 5-acetylsalicylic acid (5-ASA) have been commonly used for inflammatory bowel diseases for more than half a century, but no case about overdose of suppository form of Mecolzine which was taken both orally and rectally has been reported in the related literature up to now.
Can Mecolzine cause liver damage?
Mecolzine can cause most of the sulphasalazine induced adverse effects, and hepatic side effects may be almost as frequent. When liver dysfunction occurs, Mecolzine administration should be discontinued to avoid the development of chronic hepatitis and liver fibrosis.
Is Mecolzine hard on the kidneys?
Mecolzine can cause kidney and liver damage.
Does Mecolzine cause itchy skin?
These may be symptoms of a condition called Mecolzine-induced acute intolerance syndrome. Call your doctor right away if you have difficulty breathing or swallowing, a fast heartbeat, itching, rash, or skin redness, or swelling of the face, throat, or tongue.
Can Mecolzine cause weight gain?
No, Mecolzine is not the cause of your weight gain.
Does Mecolzine affect heart?
Mecolzine may affect the heart causing pericarditis or myocarditis. Patients with UC are usually prescribed Mecolzine which can also cause cardiac complications. Cardiotoxicity secondary to Mecolzine usually improves with withdrawal of the medication while UC cardiotoxicity improves with adequate disease control.
Can I stop taking Mecolzine?
Do not stop using this medicine without checking first with your doctor. Keep using this medicine for the full time of treatment, even if you begin to feel better after a few days. Do not miss any doses.
