Chemical formula: C₇H₇NO₃ Molecular mass: 153.135 g/mol PubChem compound: 4075
Mesalazine interacts in the following cases:
Caution is recommended for the concomitant use of mesalazine with known nephrotoxic agents, including non-steroidal anti-inflammatory drugs (NSAIDs) and azathioprine as these may increase the risk of renal adverse reactions.
Reports of renal impairment, including minimal change nephropathy, acute/chronic interstitial nephritis and renal failure have been associated with preparations containing mesalazine and pro-drugs of mesalazine. Mezavant should be used with caution in patients with confirmed mild to moderate renal impairment. It is recommended that all patients have an evaluation of renal function prior to initiation of therapy and at least twice a year, while on treatment.
Administration with coumarin-type anticoagulants e.g. warfarin, could result in decreased anticoagulant activity. Prothrombin time should be closely monitored if this combination is essential.
Mesalazine inhibits thiopurine methyltransferase. In patients receiving azathioprine or 6-mercaptopurine, caution is recommended for concurrent use of mesalazine as this can increase the potential for blood dyscrasias.
Patients with chronic lung function impairment, especially asthma, are at risk of hypersensitivity reactions and should be closely monitored.
In case of existing gastric or duodenal ulcers treatment should begin with caution based on theoretical grounds.
Limited experience with mesalazine in pregnancy does not indicate an increased risk of drug induced congenital malformations. Mesalazine crosses the placental barrier, but provides foetal concentrations much lower than those seen with adult therapeutic use. Animal studies do not indicate harmful effects of mesalazine in pregnancy, embryonal/foetal development, parturition or postnatal development. Mesalazine should be used during pregnancy only when clearly indicated. Caution should be exercised when using high doses of mesalazine.
There is no adequate data on the use of mesalazine in pregnant women. However, data on a limited number of exposed pregnancies indicate no adverse effect of mesalazine on the pregnancy or on the health of the fetus/newborn child. To date no other relevant epidemiologic data are available.
In one single case after long-term use of a high dose of mesalazine (2-4 g, orally) during pregnancy, renal failure in a neonate was reported.
Blood disorders (leucopenia, thrombocytopenia, anaemia) have been reported in new-borns of mothers being treated with mesalazine.
Mesalazine should only be used during pregnancy if the potential benefit outweighs the possible risk.
N-acetyl-5-aminosalicylic acid and to a lesser degree mesalazine is excreted in breast milk. The mesalazine concentration in breast milk is lower than in maternal blood, whereas the metabolite, acetyl mesalazine appears in similar or increased concentrations. There is limited experience of the use of oral mesalazine in lactating women available to date.
No controlled studies with mesalazine during breast-feeding have been carried out. Hypersensitivity reactions such as diarrhoea in the infant cannot be excluded. Therefore, mesalazine should only be used during breast-feeding, if the potential benefit outweighs the possible risk.
If the infant develops diarrhoea, breast-feeding should be discontinued.
Data on mesalazine show no sustained effect on male fertility.
No studies on the effects on the ability to drive and use machines have been performed. Mesalazine is considered to have negligible influence on these abilities.
No effects on the ability to drive and use machines have been observed.
The most frequently reported adverse drug reactions (ADRs)within the pooled safety analysis of clinical studies with Mezavant, including 3,611 patients, were colitis (including ulcerative colitis) 5.8%, abdominal pain 4.9%, headache 4.5%, liver function test abnormal, 2.1%, diarrhoea 2.0%, and nausea 1.9%.
Adverse reactions are listed by System Organ Class (see list below). Within each system organ class, adverse reactions are listed under headings of frequency using the categories: very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1,000 to <1/100); rare (≥1/10,000 to <1/1,000); not known (cannot be estimated from the available data).
Uncommon: Thrombocytopenia
Rare: Agranulocytosis
Not known: Aplastic anaemia, Leukopenia, Neutropenia, Pancytopenia
Uncommon: Face oedema
Not known: Hypersensitivity, Anaphylactic shock, Angioedema, Stevens-Johnson syndrome, Drug rash with eosinophilia and systemic symptoms (DRESS)
Common: Headache
Uncommon: Dizziness, Somnolence, Tremor
Not known: Intracranial pressure increased, neuropathy
Uncommon: Ear pain
Uncommon: Tachycardia
Not known: Myocarditis, Pericarditis
Common: Hypertension
Uncommon: Hypotension
Uncommon: Pharyngolaryngeal pain
Not known: Hypersensitivity pneumonitis (including interstitial Pneumonitis, allergic alveolitis, eosinophilic pneumonitis), Bronchospasm
Common: Abdominal distension, Abdominal pain, Colitis, Diarrhoea, Dyspepsia, Vomiting, Flatulence, Nausea
Uncommon: Pancreatitis, Rectal polyp
Common: Liver Function Test abnormal (e.g. ALT; AST, Bilirubin)
Not known: Hepatitis, Cholelithiasis
Common: Pruritus, Rash
Uncommon: Acne, Alopecia, Urticaria
Rare: Photosensitivity
Common: Arthralgia, Back pain
Uncommon: Myalgia
Not known: Systemic-lupus erythematosus-like syndrome, Lupus-like syndrome
Rare: Renal failure
Not known: Interstitial nephritis, Nephrotic syndrome
Not known: Oligospermia (reversible)
Common: Asthenia, Fatigue, Pyrexia
Cases of increased intracranial pressure with papilledema (pseudotumor cerebri or benign intracranial hypertension) have been reported with the use of mesalamines. If undetected, this condition may result in restriction of the visual field and may progress to permanent loss of vision. Mesalamine should be discontinued, if this syndrome occurs.
More severe reactions are reported in patients with pre-existing skin conditions such as atopic dermatitis and atopic eczema.
Following rectal administration local reactions such as pruritus, rectal discomfort and urge may occur.
Frequency of adverse effects, based on clinical trials and reports from post-marketing surveillance: Common ≥1/100 to <1/10, Rare ≥1/10,000 to ≤1/1,000, Very rare ≤1/10,000.
Very rare: Altered blood counts (aplastic anaemia, anaemia, agranulocytosis, pancytopenia, neutropenia, leukopenia, thrombocytopenia), and eosinophilia (as part of an allergic reaction).
Rare: Headache, dizziness
Very rare: Peripheral neuropathy
Rare: Myocarditis*, Pericarditis*
Very rare: Allergic and fibrotic lung reactions (including dyspnoea, cough, bronchospasm, alveolitis pulmonary eosinophilia, lung infiltration, pneumonitis)
Rare: Abdominal pain, diarrhoea, flatulence, nausea, vomiting, increased amylase
Very rare: Acute pancreatitis*
Very rare: Impairment of renal function*** including acute and chronic interstitial nephritis*, nephrotic syndrome, urine discolouration and renal insufficiency
Common: Rash (incl. urticaria, erythematous rash)
Rare: Photosensitivity**
Very rare: Alopecia (reversible), Erythema multiforme, and Stevens-Johnson Syndrome (SJS)
Very rare: Myalgia, arthralgia
Very rare: Hypersensitivity reaction such as allergic exanthema, drug fever, lupus erythematosus syndrome, pancolitis
Very rare: Changes in liver function parameters (increase in transaminases, and cholestasis parameters), hepatitis*, cholestatic hepatitis, cirrhosis, hepatic failure
Very rare: Oligospermia (reversible)
* The mechanism of mesalazine-induced myo- and pericarditis, pancreatitis, nephritis and hepatitis is unknown, but it might be of allergic origin.
** Photosensitivity: More severe reactions are reported in patients with pre-existing skin conditions such as atopic dermatitis and atopic eczema.
*** Renal failure has been reported. Mesalazine-induced nephrotoxicity should be suspected in patients developing renal dysfunction during treatment.
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