- Approval Id
- 1895066a430e7e40
- Drug Approval Emc Name
- Prednisolone 20 mg/100 ml Rectal Solution
- Drug Name
- Prednisolone 20 mg/100 ml Rectal Solution
- Company Name
- Chemidex Pharma Ltd
- Company Address
- 7 Egham Business Village, Crabtree Road, Egham, Surrey, TW20 8 RB, UK
- Company Website
- http://www.chemidex.co.uk
- Company Telephone
- +44 (0)1784 477 167
- Company Medical Info Direct Line
- +44 (0)1784 477167
- Company Medical Info Email
- MedicalInformation-UK@essentialpharmagroup.com
- Legal Category
- Pharmacy
- Authorisation Holder
- Chemidex Pharma Ltd.
T/A Essential Generics 8a
Crabtree Road.
Egham
Surrey TW20 8RN
United Kingdom
- Authorisation Number
- PL 17736/0102
- Authorisation Date
- January 1986 \*I\* January 1996
- Instruction Authorisation Holder
- Chemidex Pharma Ltd.
T/A Essential Generics 8a
Crabtree Road.
Egham
Surrey TW20 8RN
United Kingdom
- Instruction Authorisation Number
- PL 17736/0102
- Instruction Authorisation Date
- January 1986 \*I\* January 1996
- Instruction Composition
- Each 100ml enema contains 35mg prednisolone metasulphobenzoate sodium equivalent to prednisolone 20mg.
- Instruction Dosage Form
- Rectal Solution
- Instruction Clinical Particulars
- 4.1 Therapeutic indications
Local treatment of ulcerative colitis.4.2 Posology and method of administration
| | |
| --- | --- |
| Adults (including the elderly): | One dose (20 mg) each night for 2-4 weeks, the course may be extended when a good response is obtained. |
| Children (under 12): | Not recommended. |
For rectal administration only.4.3 Contraindications
In local conditions where use might mask infection or impair healing, such as peritonitis, sinus infection, fistulae, intestinal obstruction, perforation of the bowel. Hypersensitivity to any of the ingredients.4.4 Special warnings and precautions for use
Symptoms of adrenal insufficiency have not been reported, but prolonged therapy should be carefully monitored. Prolonged continuous use is not recommended. Use with caution in patients with intestinal obstruction.
\*\*Scleroderma renal crisis\*\*
Caution is required in patients with systemic sclerosis because of an increased incidence of (possibly fatal) scleroderma renal crisis with hypertension and decreased urinary output observed with a daily dose of 15 mg or more prednisolone. Blood pressure and renal function (s-creatinine) should therefore be routinely checked. When renal crisis is suspected, blood pressure should be carefully controlled.
\*\*Visual disturbance\*\*
Visual disturbance may be reported with systemic and topical corticosteroid use. If a patient presents with symptoms such as blurred vision or other visual disturbances, the patient should be considered for referral to an ophthalmologist for evaluation of possible causes which may include cataract, glaucoma or rare diseases such as central serous chorioretinopathy (CSCR) which have been reported after use of systemic and topical corticosteroids.4.5 Interaction with other medicinal products and other forms of interaction
Co-treatment with CYP3A inhibitors, including cobicistat-containing products, is expected to increase the risk of systemic side-effects. The combination should be avoided unless the benefit outweighs the increased risk of systemic corticosteroid side-effects, in which case patients should be monitored for systemic corticosteroid side-effects.4.6 Pregnancy and lactation
Topical administration of corticosteroids to pregnant animals can cause abnormalities of foetal development. The relevance of this finding to human beings has not been established.
However, physicians should be aware of the possibility of teratogenic effects, and also of potential suppression of the HPA axis, and should weigh up the risk/benefit ratio before using the medicinal product n pregnancy.
If treatment is instituted, the minimum dosage and frequency of administration required for clinical control should be employed, and prolonged usage should be avoided.4.7 Effects on ability to drive and use machines
None stated.4.8 Undesirable effects
Administration of prednisolone via this route, for this indication, is seldom associated with adverse effects. The consequence of systemic absorption (e.g. suppression of the HPA axis) should be considered if the medicinal product is used extensively over prolonged periods. As with all rectal corticosteroids, prolonged continuous use is undesirable. Possible adverse events include osteoporosis, peptic ulceration, ocular hypertension, subcapsular cataract, pancreatic disturbances and myopathy.
Frequency 'unknown': Scleroderma renal crisis\\*, bradycardia\\*\\* , vision, blurred (see also section 4.4).
\\*see section c) \\*\\*following high doses
c) Scleroderma renal crisis
Amongst the different subpopulations the occurrence of scleroderma renal crisis varies. The highest risk has been reported in patients with diffuse systemic sclerosis. The lowest risk has been reported in patients with limited systemic sclerosis (2%) and juvenile onset systemic sclerosis (1%).
\*\*Reporting of suspected adverse reactions\*\*
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the Yellow Card Scheme at: www.mhra.gov.uk/yellowcard.4.9 Overdose
Overdose is not likely with this route of administration.
- Instruction Pharmacology
- 5.1 Pharmacodynamic properties
Prednisolone 21-sodium metasulphobenzoate has the general properties of prednisolone as a potent anti-inflammatory agent with immuno-suppressant glucocorticoid properties. Esterification of prednisolone at the 21 position increases the topical activity of the drug.5.2 Pharmacokinetic properties
Following rectal administration of prednisolone 21-sodium metasulphobenzoate in the form of an enema, the action of the drug is predominantly local. The peak plasma levels obtained following this treatment are significantly lower than those obtained following treatment with prednisolone 21-phosphate.
Following absorption, the drug is hydrolysed to m-sulphobenzoic acid (and salts) and free prednisolone.
At the low plasma levels obtained, following rectal administration of prednisolone 21-sodium metasulphobenzoate the precautions generally applied to the use of prednisolone are considered to be unnecessary.5.3 Preclinical safety data
There are no pre-clinical data of relevance to the prescriber which are additional to that already included in other sections of the SPC.
- Instruction Pharmaceutical Particulars
- 6.1 List of excipients
Disodium Edetate Ph.Eur., Nipostat and Purified Water Ph.Eur.6.2 Incompatibilities
None stated.6.3 Shelf life
12 months6.4 Special precautions for storage
Store below 25°C, protected from light.6.5 Nature and contents of container
Presentation: a ready to use, single dose, disposable plastic bag or EVA bottle, with prelubricated PVC nozzle, containing 100ml of solution. A version with an extension tube is available for those patients who may find it helpful.6.6 Special precautions for disposal and other handling
Before use the patient should lie in bed on their side with knees drawn up.
The product may be administered at room temperature, or warmed in warm water before use.
Bag: Hold the bag with tube upwards, squeeze base of tube where it joins the bag. Remove cap and lubricate tube before inserting into rectum. Squeeze gently until fluid is dispelled, and discard bag hygienically.
Bottle: Keeping bottle upright, remove blue protective cap. Insert nozzle into rectum and squeeze bottle gently until fluid is dispelled. Discard bottle hygienically. For the 'long-tube' version first carefully remove the bottle cap, screw on the applicator and then administer as above.
After administration the patient should lie face down for a few minutes to retain the fluid before going to sleep in their usual position.
- Instruction Content
- ## Composition
Each 100ml enema contains 35mg prednisolone metasulphobenzoate sodium equivalent to prednisolone 20mg.
## Pharmaceutical Form
Rectal Solution
## Clinical Particulars
4.1 Therapeutic indications
Local treatment of ulcerative colitis.4.2 Posology and method of administration
| | |
| --- | --- |
| Adults (including the elderly): | One dose (20 mg) each night for 2-4 weeks, the course may be extended when a good response is obtained. |
| Children (under 12): | Not recommended. |
For rectal administration only.4.3 Contraindications
In local conditions where use might mask infection or impair healing, such as peritonitis, sinus infection, fistulae, intestinal obstruction, perforation of the bowel. Hypersensitivity to any of the ingredients.4.4 Special warnings and precautions for use
Symptoms of adrenal insufficiency have not been reported, but prolonged therapy should be carefully monitored. Prolonged continuous use is not recommended. Use with caution in patients with intestinal obstruction.
\*\*Scleroderma renal crisis\*\*
Caution is required in patients with systemic sclerosis because of an increased incidence of (possibly fatal) scleroderma renal crisis with hypertension and decreased urinary output observed with a daily dose of 15 mg or more prednisolone. Blood pressure and renal function (s-creatinine) should therefore be routinely checked. When renal crisis is suspected, blood pressure should be carefully controlled.
\*\*Visual disturbance\*\*
Visual disturbance may be reported with systemic and topical corticosteroid use. If a patient presents with symptoms such as blurred vision or other visual disturbances, the patient should be considered for referral to an ophthalmologist for evaluation of possible causes which may include cataract, glaucoma or rare diseases such as central serous chorioretinopathy (CSCR) which have been reported after use of systemic and topical corticosteroids.4.5 Interaction with other medicinal products and other forms of interaction
Co-treatment with CYP3A inhibitors, including cobicistat-containing products, is expected to increase the risk of systemic side-effects. The combination should be avoided unless the benefit outweighs the increased risk of systemic corticosteroid side-effects, in which case patients should be monitored for systemic corticosteroid side-effects.4.6 Pregnancy and lactation
Topical administration of corticosteroids to pregnant animals can cause abnormalities of foetal development. The relevance of this finding to human beings has not been established.
However, physicians should be aware of the possibility of teratogenic effects, and also of potential suppression of the HPA axis, and should weigh up the risk/benefit ratio before using the medicinal product n pregnancy.
If treatment is instituted, the minimum dosage and frequency of administration required for clinical control should be employed, and prolonged usage should be avoided.4.7 Effects on ability to drive and use machines
None stated.4.8 Undesirable effects
Administration of prednisolone via this route, for this indication, is seldom associated with adverse effects. The consequence of systemic absorption (e.g. suppression of the HPA axis) should be considered if the medicinal product is used extensively over prolonged periods. As with all rectal corticosteroids, prolonged continuous use is undesirable. Possible adverse events include osteoporosis, peptic ulceration, ocular hypertension, subcapsular cataract, pancreatic disturbances and myopathy.
Frequency 'unknown': Scleroderma renal crisis\\*, bradycardia\\*\\* , vision, blurred (see also section 4.4).
\\*see section c) \\*\\*following high doses
c) Scleroderma renal crisis
Amongst the different subpopulations the occurrence of scleroderma renal crisis varies. The highest risk has been reported in patients with diffuse systemic sclerosis. The lowest risk has been reported in patients with limited systemic sclerosis (2%) and juvenile onset systemic sclerosis (1%).
\*\*Reporting of suspected adverse reactions\*\*
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the Yellow Card Scheme at: www.mhra.gov.uk/yellowcard.4.9 Overdose
Overdose is not likely with this route of administration.
## Pharmacological Properties
5.1 Pharmacodynamic properties
Prednisolone 21-sodium metasulphobenzoate has the general properties of prednisolone as a potent anti-inflammatory agent with immuno-suppressant glucocorticoid properties. Esterification of prednisolone at the 21 position increases the topical activity of the drug.5.2 Pharmacokinetic properties
Following rectal administration of prednisolone 21-sodium metasulphobenzoate in the form of an enema, the action of the drug is predominantly local. The peak plasma levels obtained following this treatment are significantly lower than those obtained following treatment with prednisolone 21-phosphate.
Following absorption, the drug is hydrolysed to m-sulphobenzoic acid (and salts) and free prednisolone.
At the low plasma levels obtained, following rectal administration of prednisolone 21-sodium metasulphobenzoate the precautions generally applied to the use of prednisolone are considered to be unnecessary.5.3 Preclinical safety data
There are no pre-clinical data of relevance to the prescriber which are additional to that already included in other sections of the SPC.
## Pharmaceutical Particulars
6.1 List of excipients
Disodium Edetate Ph.Eur., Nipostat and Purified Water Ph.Eur.6.2 Incompatibilities
None stated.6.3 Shelf life
12 months6.4 Special precautions for storage
Store below 25°C, protected from light.6.5 Nature and contents of container
Presentation: a ready to use, single dose, disposable plastic bag or EVA bottle, with prelubricated PVC nozzle, containing 100ml of solution. A version with an extension tube is available for those patients who may find it helpful.6.6 Special precautions for disposal and other handling
Before use the patient should lie in bed on their side with knees drawn up.
The product may be administered at room temperature, or warmed in warm water before use.
Bag: Hold the bag with tube upwards, squeeze base of tube where it joins the bag. Remove cap and lubricate tube before inserting into rectum. Squeeze gently until fluid is dispelled, and discard bag hygienically.
Bottle: Keeping bottle upright, remove blue protective cap. Insert nozzle into rectum and squeeze bottle gently until fluid is dispelled. Discard bottle hygienically. For the 'long-tube' version first carefully remove the bottle cap, screw on the applicator and then administer as above.
After administration the patient should lie face down for a few minutes to retain the fluid before going to sleep in their usual position.
