Mesalazine oral modified release
- Drugs List
- Therapeutic Indications
- Dosage
- Contraindications
- Precautions and Warnings
- Pregnancy and Lactation
- Side Effects
- Monograph
Presentation
Oral modified release formulations of mesalazine.
Drugs List
Therapeutic Indications
Uses
Crohn's disease - maintenance of remission
Ulcerative colitis: induction of remission
Ulcerative colitis: maintenance of remission
Dosage
Not all brands are licensed for all indications.
The release characteristics of different modified release formulations of mesalazine may vary; these preparations should not be considered interchangeable.
Dosage should be individually determined on the clinical requirements of the patient.
Dosage recommendations vary according to brand: consult product literature for more information.
Adults
Ulcerative colitis
Active disease
1.5g to 4.8g daily, given in one single or in two to four divided doses.
When using the highest dose (4.8g), the effect of the treatment should be evaluated at eight weeks.
Maintenance treatment
1.2g to 2.4g daily, given in one single or in divided doses.
Up to 3g given as a single daily dose, preferably in the morning, can be given for patients that have an increased risk of relapse due to medical reasons or have difficulties with a three daily doses schedule.
Crohn's ileo-colitis
Maintenance of remission
1.2g to 2.4g daily in divided doses.
Children
Not all available brands are recommended to use in children or in all ages.
Children aged 10 years and older and weighing more than 50kg (gastro-resistant prolonged release 1200mg tablets)
Ulcerative colitis
Active disease: 2.4g to 4.8g once daily. When using the highest dose (4.8g), the effect of the treatment should be evaluated at eight weeks.
Maintenance of remission: 2.4g once daily.
Children aged 6 to 18 years (gastro-resistant modified release granules, modified release granules, modified release tablets)
Ulcerative colitis
Active disease: 30mg/kg to 50mg/kg should be given once daily, preferably in the morning or in three divided doses.
Maximum dose: 75mg/kg daily or 4g daily.
Maintenance of remission: 15mg/kg to 30mg/kg daily may be given in divided doses.
Maximum dose: 2g daily.
It is generally recommended that half the adult dose may be given to children up to a body weight of 40kg, and the full adult dose to those over 40kg body weight.
Crohn's ileo-colitis
Maintenance of remission: 15 to 30mg/kg/day in divided doses.
Maximum dose: 2g daily.
It is generally recommended that half the adult dose may be given to children up to a body weight of 40kg, and the full adult dose to those over 40kg body weight.
The following alternative dosing schedules may be suitable:
Active disease
Children aged 5 to 18 years and body weight over 40kg: Up to 3g once daily or in divided doses, or up to 4g in two to three divided doses.
Children aged 5 to 18 years and body weight under 40kg: 10mg/kg to 20mg/kg three times daily.
Alternatively, in children aged 12 to 18 years: 800mg three times a day.
Maintenance of remission
Children aged 5 to 18 years and body weight over 40kg: 2g once daily or 500mg three times daily.
Children aged 5 to 18 years and body weight under 40kg: 7.5mg/kg to 15mg/kg twice daily. Total dose may alternatively be given in three divided doses.
Alternatively, in children aged 12 to 18 years: 400mg to 800mg two to three times daily.
Crohn's ileo-colitis
Maintenance of remission in children aged 6 to 18 years and body weight over 40kg: 1.2g to 2g once a day or in divided doses.
Alternatively, in children aged 12 to 18 years: 400mg to 800mg two to three times daily.
Additional Dosage Information
In the treatment of both acute inflammatory episodes and remission mesalazine should be used on a regular basis and consistently in order to achieve the desired therapeutic effects.
Contraindications
Children under 5 years
Haemorrhagic diathesis
Renal impairment - glomerular filtration rate below 20ml/minute
Severe hepatic impairment
Precautions and Warnings
Children aged 5 to 18 years
Restricted sodium intake
Asthma
Breastfeeding
Duodenal ulcer
Galactosaemia
Glucose-galactose malabsorption syndrome
Hepatic impairment
Hereditary fructose intolerance
History of myocarditis
History of pericarditis
Lactose intolerance
Peptic ulcer
Phenylketonuria
Pregnancy
Pulmonary disease
Renal impairment - glomerular filtration rate 20-50ml/minute
Some formulations contain aspartame - caution in phenylketonuria
Some formulations contain more than 1mmol (23mg) sodium per dose
Not all available brands are licensed for all indications
Not all available brands/formulations are licensed for use in children
Restore electrolyte & fluid balance in case of dehydration
Some formulations contain lactose
Some formulations contain sucrose
Delivery characteristics of e-c preps may vary and are not interchangeable
Ensure patient has adequate fluid intake
Blood counts should be performed before and periodically during treatment
Monitor hepatic function before treatment and regularly during treatment
Monitor renal function prior to initiating treatment
Elderly: Monitor renal function and consider dose modification
Monitor for signs of blood dyscrasias eg fever, sore throat, malaise etc
Monitor patients with bronchial asthma
Monitor renal function especially during the initial phase of treatment
Advise patient to report unexplained fever, sore throat, bruising, bleeding
Drug-induced cardiac hypersensitivity[myocarditis & pericarditis] may occur
Suspect drug-induced nephrotoxicity if renal impairment occurs with therapy
May affect results of some laboratory tests
Discontinue if myocarditis or pericarditis occurs
Discontinue if renal function deteriorates
Discontinue if severe hypersensitivity reactions occur
Discontinue if severe skin reaction occurs
Discontinue immediately if suspicion of a blood dyscrasia
Avoid concurrent use of lactulose
Advise patients that empty tablet/capsule may be observed in stools
Haematological investigations are generally recommended within 14 days of initiation of therapy and with 2 to 3 repeat tests at 4 week intervals. If the results are normal, tests are recommended quarterly.
It is recommended that renal function is tested initially, at three months and annually thereafter.
Pregnancy and Lactation
Pregnancy
Use mesalazine with caution during pregnancy.
The manufacturers recommends mesalazine is not used in pregnancy unless the potential benefit to the mother outweighs the potential risk to the foetus. One manufacturer states that blood disorders (leucopenia, thrombocytopenia, anaemia) have been reported in neonates of mothers being treated with mesalazine and recommends use with caution.
Although mesalazine acts within the gastrointestinal tract, systemic absorption occurs with up to 50% of the dose being absorbed after oral administration.
In inflammatory bowel disease, symptoms and activity are linked to pregnancy outcomes, active disease being associated with low birth weights, higher rates of spontaneous abortion, prematurity and perinatal complications. Most authors conclude that mesalazine does not further increase the risk of adverse pregnancy outcomes. There is one report of renal insufficiency in an infant exposed after long term use of a high dose (2g to 4g, orally) of mesalazine.
Schaefer states that mesalazine is the drug of choice for chronic inflammatory bowel disease during pregnancy. Inflammatory markers and haematology should be monitored regularly. Dosage should be as required for optimal disease control.
Lactation
Use mesalazine with caution during breastfeeding.
The manufacturer advises that mesalazine is excreted in breast milk in small quantities while its metabolite N-acetyl-5-aminosalicyclic acid is excreted in larger amounts. There have been a number of reported cases of diarrhoea in the nursing infant which were considered to be due to a possible hypersensitivity reaction. The manufacturer recommends that if the infant develops diarrhoea, breast feeding should be discontinued.
Side Effects
Abdominal distension
Abdominal pain
Abnormal liver function tests
Acne
Agranulocytosis
Allergic alveolitis
Allergic lung reactions
Alopecia
Anaemia
Angioedema
Aplastic anaemia
Arthralgia
Asthenia
Back pain
Benign intracranial hypertension
Bloating
Bone marrow depression
Bronchospasm
Bullous reactions
Cholelithiasis
Cholestatic hepatitis
Cirrhosis
Cough
Diarrhoea
Discolouration of urine
Dizziness
Drug fever
Dyspepsia
Dyspnoea
Ear pain
Elevated amylase levels
Eosinophilia
Eosinophilic pneumonia
Erythema multiforme
Erythematous rash
Exacerbation of colitis
Exanthema
Facial oedema
Fatigue
Fibrosing alveolitis
Flatulence
Granulocytopenia
Headache
Hepatic failure
Hepatic impairment
Hepatitis
Hepatotoxicity
Hypersensitivity reactions
Hypertension
Hypotension
Increase of liver transaminases
Influenza-like syndrome
Interstitial nephritis
Interstitial pneumonia
Leucopenia
Lupus erythematosus-like syndrome
Methaemoglobinaemia
Myalgia
Myocarditis
Nausea
Nephrolithiasis
Nephrotic syndrome
Nephrotoxicity
Neutropenia
Oligospermia (reversible)
Pancolitis
Pancreatitis
Pancytopenia
Pericarditis
Peripheral neuropathy
Pharyngolaryngeal pain
Photosensitivity
Pleurisy
Pleuropericarditis
Pneumonitis
Polyps
Pruritus
Pulmonary eosinophilia
Pulmonary infiltration
Pyrexia
Quincke's oedema
Rash
Rectal disorders
Renal failure
Renal impairment
Respiratory tract infection
Rhinitis
Serum bilirubin increased
Sinusitis
Somnolence
Stevens-Johnson syndrome
Tachycardia
Thrombocytopenia
Toxic epidermal necrolysis
Tremor
Urticaria
Vertigo
Vomiting
Overdosage
It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.
The following number will direct the caller to the relevant local centre (0844) 892 0111
Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).
Further Information
Last Full Review Date: October 2019
Reference Sources
Drugs in Pregnancy and Lactation: A Reference Guide to Fetal and Neonatal Risk, 10th edition (2015) ed. Briggs, G., Freeman, R. Wolters Kluwer Health, Philadelphia.
Drugs During Pregnancy and Lactation: Treatment Options and Risk Assessment, 3rd edition (2015) ed. Schaefer, C., Peters, P. and Miller, R. Elsevier, London.
Summary of Product Characteristics: Asacol 400mg MR tablets. Allergan Ltd. Revised December 2020.
Summary of Product Characteristics: Asacol 800mg MR tablets. Allergan Ltd. Revised December 2020.
Summary of Product Characteristics: Mezavant XL 1200mg, gastro-resistant, prolonged release tablets. Shire Pharmaceuticals Contracts Limited. Revised June 2021.
Summary of Product Characteristics: Octasa 400mg modified-release tablets. Tillotts Pharma UK Ltd. Revised November 2019.
Summary of Product Characteristics: Octasa 800mg modified-release tablets. Tillotts Pharma UK Ltd. Revised November 2019.
Summary of Product Characteristics: Octasa 1600mg modified-release tablets. Tillotts Pharma UK Ltd. Revised November 2019.
Summary of Product Characteristics: Pentasa Sachet 1g prolonged release granules. Ferring Pharmaceuticals Ltd. Revised June 2018.
Summary of Product Characteristics: Pentasa Sachet 2g prolonged release granules. Ferring Pharmaceuticals Ltd. Revised June 2018.
Summary of Product Characteristics: Pentasa Sachet 4g prolonged release granules. Ferring Pharmaceuticals Ltd. Revised June 2018.
Summary of Product Characteristics: Pentasa Slow Release tablets 500mg. Ferring Pharmaceuticals Ltd. Revised January 2018.
Summary of Product Characteristics: Pentasa Slow Release tablets 1g. Ferring Pharmaceuticals Ltd. Revised January 2018.
Summary of Product Characteristics: Salofalk 500mg gastro-resistant prolonged-release granules. Dr Falk Pharma UK Ltd. Revised August 2019.
Summary of Product Characteristics: Salofalk 1000mg gastro-resistant prolonged-release granules. Dr Falk Pharma UK Ltd. Revised August 2019.
Summary of Product Characteristics: Salofalk 1.5g gastro-resistant prolonged-release granules. Dr Falk Pharma UK Ltd. Revised August 2019.
Summary of Product Characteristics: Salofalk 3g gastro-resistant prolonged-release granules. Dr Falk Pharma UK Ltd. Revised August 2019.
Summary of Product Characteristics: Zintasa 400mg EC tablets. Morningside Healthcare Ltd. Revised July 2019.
NICE Evidence Services Available at: www.nice.org.uk Last accessed: 11 October 2022
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