Drugs List

Therapeutic Indications

Uses

Ulcerative colitis involving rectal and recto-sigmoid disease

Administration

Rectal foam:
The canister is first fitted with an applicator and then shaken for about 15 seconds before the applicator is inserted into the rectum as far as comfortable. The dose is only sufficiently accurate when the pump dome is held downwards as vertically as possible. To administer a dose of budesonide rectal foam, the pump dome is fully pushed down and very slowly released. Following activation the applicator should be held in position for 10 to 15 seconds before being withdrawn from the rectum.

Rectal enema:
Reconstitute the enema immediately before use, ensuring that the tablet is completely dissolved.

Contraindications

Children under 12 years
Hepatic cirrhosis

Precautions and Warnings

Children aged 12 to 18 years
Transfer from other steroid therapy
Hepatic impairment
History of severe affective disorders
Pregnancy

Exposure to measles may require prophylaxis with normal immunoglobulin
May mask symptoms or signs of infections
Systemic corticosteroids may be needed during periods of stress
Some formulations contain hydroxybenzoate
Some formulations contain propylene glycol
Consider adrenal suppression when transferring from systemic steroid
If visual disturbances occur, perform ophthalmic evaluation
Prolonged or high dose may lead to adrenal suppression
Antibody response to vaccines may be reduced
During transfer from oral steroids allergic conditions may be unmasked
May affect results of some laboratory tests
Treatment period should not exceed 8 weeks
If exposed to chickenpox or Herpes zoster seek urgent medical attention

Treatment with budesonide rectal formulations results in lower systemic steroid levels than oral therapy with systemically acting corticoids. Transfer from other steroid therapy may result in symptoms relating to the change in systemic steroid levels.

If a patient suffers from symptoms such as tiredness, headache, nausea and vomiting during the withdrawal phase then a insufficient glucocorticosteroid effect is likely and a temporary increase in the dose of systemic glucocorticosteroids may be necessary.

Deterioration of bacterial, fungal, amoebic, and viral infections during glucocorticoid treatment should be considered. The clinical presentation may often be atypical and serious infections such as septicaemia and tuberculosis may be masked and may reach an advanced stage before being recognised.

In patients with severe liver function disorders, the elimination of glucocorticoids including budesonide rectal formulations will be reduced, and their systemic bioavailability will be increased.

False results (low values) may occur in an ACTH stimulation test for diagnosing pituitary insufficiency because adrenal function may be suppressed.

Pregnancy and Lactation

Pregnancy

Use with caution in pregnancy.

Administration during pregnancy should be prescribed only when the expected benefits to mother and child outweigh the risks. When use of budesonide is essential, patients with normal pregnancies should be treated as though they were not pregnant.

In pregnant animals, budesonide has been shown to cross the placenta. Administration of corticosteroids to pregnant animals causes abnormalities of foetal development, including intra-uterine growth retardation. Hypoadrenalism may in theory occur in the neonate following prenatal exposure to corticosteroids but usually resolves spontaneously following birth.

The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14-17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Lactation

Budesonide is secreted in small amounts in breast milk. At therapeutic doses of budesonide exposure to the suckling infant is anticipated to be low, as shown in pharmacokinetic studies, and is unlikely to cause systemic effects.

Infants of mothers taking higher than recommended dose of budesonide may have a degree of adrenal suppression.

When taken orally, budesonide is only about 9% bioavailable; bioavailability in the infant is likely to be similarly low for any budesonide that enters the breast milk.

These data support continued use of budesonide, oral and rectal administrations during breastfeeding.

Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
Specialist advice is available from the UK Drugs in Lactation Advisory Service at https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1

Side Effects

Abdominal pain
Accelerated erythrocyte sedimentation
Acne
Adrenal cortex insufficiency
Aggression
Agitation
Amenorrhoea
Anaemia
Anal fissure
Anaphylactic reaction
Anxiety
Aphthous stomatitis
Asthenia
Blurred vision
Bone necrosis
Cataracts
Cholestatic liver changes
Constipation
Contact dermatitis
Cushing's syndrome
Decreased glucose tolerance
Depression
Diabetes mellitus
Diarrhoea
Dizziness
Duodenal ulcer
Dyspepsia
Ecchymosis
Euphoria
Exanthema
Faecal urgency
Flatulence
Gastro-intestinal disturbances
Glaucoma
Growth retardation (children)
Haemorrhoids
Headache
Hirsutism
Hypertension
Impotence
Increase of liver transaminases
Increased amylase secretion
Increased appetite
Increased I.C.P. with papilloedema in children (pseudotumour cerebri)
Increased susceptibility and severity of infections
Increased sweating
Insomnia
Irritability
Leukocytosis
Malaise
Moon face
Muscle pain
Muscle weakness
Nausea
Oedema
Osteoporosis
Pancreatitis
Paraesthesia
Petechiae
Potassium loss
Psychomotor hyperactivity
Rectal bleeding
Rectal pain/discomfort
Skin reactions
Smelling disturbances
Sodium retention
Steroid acne
Striae
Thrombosis
Tiredness
Truncal obesity
Urinary tract infections
Urticaria
Vasculitis
Visual disturbances
Weight gain
Wound healing retarded

Presentation

Budesonide rectal formulations.

Drugs List

Therapeutic Indications

Uses

Ulcerative colitis involving rectal and recto-sigmoid disease

Dosage

The attending physician determines the duration of use. An acute episode generally subsides after 2 to 8 weeks.

The best results are obtained when the intestine is evacuated prior to administration.

Adults

Children

Administration

Rectal foam:
The canister is first fitted with an applicator and then shaken for about 15 seconds before the applicator is inserted into the rectum as far as comfortable. The dose is only sufficiently accurate when the pump dome is held downwards as vertically as possible. To administer a dose of budesonide rectal foam, the pump dome is fully pushed down and very slowly released. Following activation the applicator should be held in position for 10 to 15 seconds before being withdrawn from the rectum.

Rectal enema:
Reconstitute the enema immediately before use, ensuring that the tablet is completely dissolved.

Contraindications

Children under 12 years
Hepatic cirrhosis

Precautions and Warnings

Children aged 12 to 18 years
Transfer from other steroid therapy
Hepatic impairment
History of severe affective disorders
Pregnancy

Exposure to measles may require prophylaxis with normal immunoglobulin
May mask symptoms or signs of infections
Systemic corticosteroids may be needed during periods of stress
Some formulations contain hydroxybenzoate
Some formulations contain propylene glycol
Consider adrenal suppression when transferring from systemic steroid
If visual disturbances occur, perform ophthalmic evaluation
Prolonged or high dose may lead to adrenal suppression
Antibody response to vaccines may be reduced
During transfer from oral steroids allergic conditions may be unmasked
May affect results of some laboratory tests
Treatment period should not exceed 8 weeks
If exposed to chickenpox or Herpes zoster seek urgent medical attention

Treatment with budesonide rectal formulations results in lower systemic steroid levels than oral therapy with systemically acting corticoids. Transfer from other steroid therapy may result in symptoms relating to the change in systemic steroid levels.

If a patient suffers from symptoms such as tiredness, headache, nausea and vomiting during the withdrawal phase then a insufficient glucocorticosteroid effect is likely and a temporary increase in the dose of systemic glucocorticosteroids may be necessary.

Deterioration of bacterial, fungal, amoebic, and viral infections during glucocorticoid treatment should be considered. The clinical presentation may often be atypical and serious infections such as septicaemia and tuberculosis may be masked and may reach an advanced stage before being recognised.

In patients with severe liver function disorders, the elimination of glucocorticoids including budesonide rectal formulations will be reduced, and their systemic bioavailability will be increased.

False results (low values) may occur in an ACTH stimulation test for diagnosing pituitary insufficiency because adrenal function may be suppressed.

Pregnancy and Lactation

Pregnancy

Use with caution in pregnancy.

Administration during pregnancy should be prescribed only when the expected benefits to mother and child outweigh the risks. When use of budesonide is essential, patients with normal pregnancies should be treated as though they were not pregnant.

In pregnant animals, budesonide has been shown to cross the placenta. Administration of corticosteroids to pregnant animals causes abnormalities of foetal development, including intra-uterine growth retardation. Hypoadrenalism may in theory occur in the neonate following prenatal exposure to corticosteroids but usually resolves spontaneously following birth.

The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14-17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Lactation

Budesonide is secreted in small amounts in breast milk. At therapeutic doses of budesonide exposure to the suckling infant is anticipated to be low, as shown in pharmacokinetic studies, and is unlikely to cause systemic effects.

Infants of mothers taking higher than recommended dose of budesonide may have a degree of adrenal suppression.

When taken orally, budesonide is only about 9% bioavailable; bioavailability in the infant is likely to be similarly low for any budesonide that enters the breast milk.

These data support continued use of budesonide, oral and rectal administrations during breastfeeding.

Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
Specialist advice is available from the UK Drugs in Lactation Advisory Service at https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1

Side Effects

Abdominal pain
Accelerated erythrocyte sedimentation
Acne
Adrenal cortex insufficiency
Aggression
Agitation
Amenorrhoea
Anaemia
Anal fissure
Anaphylactic reaction
Anxiety
Aphthous stomatitis
Asthenia
Blurred vision
Bone necrosis
Cataracts
Cholestatic liver changes
Constipation
Contact dermatitis
Cushing's syndrome
Decreased glucose tolerance
Depression
Diabetes mellitus
Diarrhoea
Dizziness
Duodenal ulcer
Dyspepsia
Ecchymosis
Euphoria
Exanthema
Faecal urgency
Flatulence
Gastro-intestinal disturbances
Glaucoma
Growth retardation (children)
Haemorrhoids
Headache
Hirsutism
Hypertension
Impotence
Increase of liver transaminases
Increased amylase secretion
Increased appetite
Increased I.C.P. with papilloedema in children (pseudotumour cerebri)
Increased susceptibility and severity of infections
Increased sweating
Insomnia
Irritability
Leukocytosis
Malaise
Moon face
Muscle pain
Muscle weakness
Nausea
Oedema
Osteoporosis
Pancreatitis
Paraesthesia
Petechiae
Potassium loss
Psychomotor hyperactivity
Rectal bleeding
Rectal pain/discomfort
Skin reactions
Smelling disturbances
Sodium retention
Steroid acne
Striae
Thrombosis
Tiredness
Truncal obesity
Urinary tract infections
Urticaria
Vasculitis
Visual disturbances
Weight gain
Wound healing retarded

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: January 2013

Reference Sources

Summary of Product Characteristics: Budenofalk 2mg/dose rectal foam. Dr. Falk Pharma GmgH. Revised September 2012.

Summary of Product Characteristics: Entocort Enema. Tillotts Pharma UK Limited. Revised January 2017.

NICE Evidence Services Available at: www.nice.org.uk Last accessed: 21 June 2017

US National Library of Medicine. Toxicology Data Network. Drugs and Lactation Database (LactMed).
Available at: https://toxnet.nlm.nih.gov/cgi-bin/sis/htmlgen?LACT
Budesonide; Last revised: November 01, 2010
Last accessed: January 10, 2013