Transcript Rectodelt 100 mg suppositories

GmbH
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Unter den Eichen 5, Gebäude F Officio II, 3. OG, 65195 Wiesbaden, Germany
Biotech GmbH Hungarian Branch
www.rectodelt.net
Rectodelt 30, 100 mg suppositories
30, 100mg prednison micronised per suppositroy
The active pharmaceutical ingredient (API) in Rectodelt suppositories is
Prednison , which is a very well established glucocorticoid that has
been successfully used in the standard therapy similarly to
Prednisolone since many decades, despite the presence of numerous
other synthetic products.
The glucocorticoids are applied for their following actions:
Anti-inflammatory, anti-exudative, anti profilerative, anti-toxic, antiallergic and immunosuppresive actions.
In standard glucocorticoid therapy the oral and rectal routs of
administration are usually the most preferrable.
The advantage of Rectodelt over orally administered prednisone
preparations, is that it has a faster rate of absorption, and at the same
time any irritations of the gastric mucous membrane are totally
avoided, making it an excellent treatment especially for sensitive
individuals.
Rectodelt has proven to be a favorite choice amongst many pediatricians,
E.N.T specialists and pulmonologists.
Rectodelt is very successfully applied, not only in emergency cases, but
also in other fields of treatments.
• Amongst the different possible routs of administration for corticoids
Rectodelt is especially favored in the treatment of little children and
infants due to the following facts:
- It is quickly absorbed
- It has a fast onset of action.
- It does not cause fear in children.
- The therapy can be accurately followed.
The Rectodelt therapy is characterized by the favorable balance between
efficacy and unwanted side-effects.
Rectodelt 30mg is a green-colored,torpedo shaped suppository with the
active ingredient prednisone in lipophilic suppository base.
Composition of a Rectodelt 30 mg suppository
Ingredient
API:
Prednisone, micronized (Ph.Eur)
Content per
suppository
(mg)
30
Other ingredients:
- Hard fat (Ph.Eur)
- Colour coating green E104/132
Declared weight
1093.50
2,50
1126 mg
± 5%
Rectodelt 100mg is a blue-colored, torpedo shaped suppository with the
active ingredient prednisone in lipophilic suppository base.
Composition of a Rectodelt 100mg suppository
Ingredient
API:
Prednisone, micronized (Ph.Eur)
Content per
suppository
(mg)
100
Other ingredients:
- Hard fat (Ph.Eur)
- Aluminium hydroxide type 211 (USP)
- Colour lacquer indigotine E 132.
Declared weight
1040
1.00
0.23
1141.23 mg
± 5%
Indications for use in children
Respiratory tract disorders
• Croup syndrome
• obstructive bronchitis
• asthma brinchiale
Allergic conditions
• Anaphylactic reactions
Rheumatic conditions
Autoimmune diseases
Neoplatic disorders
• for palliative management of acute leukemia of childhood.
Indications for use in adults
Allergic conditions
• Bronchial asthma
• Seasonal or perennial allergic rhinitis, Hey fever
• Urticaria
• Drug hypersensitivity reactions
Rheumatic conditions
• Polyarthritis
• Rheumatic fever
• Rheumatic carditis
Gastro-intestinal diseases
• ulcerative colitis
Skin diseases
• Acute dermatitis
• Chronic dermatitis
Liver diseases
• Acute hepatitis
• Chronic hepatitis
Pulmonary diseases
• Chronic bronchitis with emphysema
• Pulmonary fibrosis
• Symptomatic sarcoidosis
• TBC, concurrently used with the appropriate antituberculous chemotherapy
Hematological diseases
• Autoimmune diseases
Toxic conditions of infectious diseases
• As a specific complement to chemotherapy
Neoplastic diseases
• for palliative management of: leukemias and lymphomas in adults
Chemistry
Under normal physiological conditions cortisol is produced in the body by
the adrenal glands cortex.
Cortisone which was synthesized by Reichstein in 1939 is considered as
the active metabolite of cortisol.
The first synthetic glucocorticoids to be introduced were prednisone and
prednisolon, which chemicaly only slightly differ from cortison and
cortisol.
Prednison is quickly metabolized in the liver to form prednisolone, and
thus both of these glucocorticoids are considered to be equivalent from
a pharmacodynamic point of view.
When comparing physiologically produced glucocorticoids with their
synthetic derivatives, the later are found to have a lower Na retention
and edema forming property, with simultaneously a 4 to 5 times
increased anti-inflammatory action.
Pharmacology
• Pharmacodynamic properties
ATC: H02A B07
INN: Prednisone
A glucocorticoid with an anti-exudative, anti-proliferative, antiinflammatory, immunsuppressiv and anti-allergic properties
The main actions of prednisone are:
1. Membrane stabilizing action
- Reduces the increased capillary and membrane permeability caused
by inflammation.
- stabilizes the lysomic membranes.
2. Inhibits the migration of macrophages and lymphocytes.
3. Metabolic actions:
- Stimulates gluconeogenesis from amino acids, thereby enhances
breakdown of protein.
- Decreases glucose tolerance and sensitivity to insuline.
- inhibits the absorption of Kalcium from the intestines.
4. Effect on salt and water balance:
- Increases Sodium re-absorption
- Decreases potassium retention
Pharmacokinetic properties:
• Absorption: Glucocorticoid plasma level can be measured shortly
after administration. A peak level is achieved in 5 hours.
• Metabolism: Prednisone is metabolized in liver, primarily to its active
metabolite prednisolone. In the body, prednisone and prednisolone are
reversibly converted to into each other, with prednisolone being the
dominant..
• Distribution: 50 to 90% of prednizolon becomes bound to plasma
proteins, especially to transcortin and albumin. Clearence is approx.
1.5 ml/min/kg.
• Elimination: it is excreted through the kidney, about 2-5 % as
prednisone, 11-24 % as prednisolone and remaining part in the form of
other metabolites.
Posology
• General considerations:
The human body produces cortison according to a circadian rhythm.
If the patient receives the entire daily dose in the morning hours (6:00 to
8:00AM), then the inhibition of the adrenal gland function can be
avoided, and the unwanted side-effects are hence reduced.
• For Adults: The starting dose in hyper acute and emergency cases is
100 – 200 mg Rectodelt daily.
In acute inflammatory conditions a 50mg to 100mg dose is given.
In case of chronic diseases the daily dose is 30 to 50mg.
• For Children: In emergency conditions it is much easier to apply
Rectodlet compared to other methods of administration. The usual
daily dose is 100mg. However, depending on the severity of the given
condition the dose can may be varied from 5mg up to 15mg per kg of
body weight.
If necessary, the high starting dose may be repeated with 24 hours. The
high dose should be consequently reduced as soon as the clinical state
of the patient improves.
The human body produces 15 to 40mg of cortisol daily.
This production follows a circadian rhythm, where the peak concentration
of cortisol is reached between 2:00 and 8:00 AM, while the lowest
concentrations can be measured around 4:00 PM and 12:00 AM.
The synthesis of corticoids in the hypothalamus and the secretion into the
blood is controlled by a feed back mechanism.
Therefore when a single dose of Rectodelt is given early in the morning, it
hardly influences the body’s own circadian rhythm in producing cortisol.
Latest studies showed that in the case of long term treatments, alternateday administration should he considered.
Doubling the dosage and administering the drug every other day in the
morning more closely mimics the endogenous corticosteroid circadian
rhythm. This form of administration enables the patient to experience
the therapeutic effects while side effects are minimized, because the
least suppresion of adrenocortical activity occurs, when corticoids are
given at the time of maximal activity.
Treatment in children
The rectal administration of Rectodelt in children and specially in infants,
has a great advantage, is it can be easily applied even with the lack of
patient’s cooperation.
The production of cortisol in children is 20-25mg daily per square meter of
body surface area.
Examinations showed that when correlating the dose to the child’s average
body weight, higher doses where needed in children than in adults,
while when correlating the doses to the body’s surface area, then
children and adult doses completely corresponded to each other.
Once a noticeable improvement is shown, then the amount of corticoids
given every other day must be gradually reduced until it reaches the
maintenance dose.
The maximum daily maintenance doses are as follows:
• Under the age of 1 year: 2.5 –5 mg per body kg
• 1 – 10 years old: 5 –10 mg per body kg
• 10 – 14 years old: 5 – 15 mg per body kg
For infants a maximum daily dose of 100mg can be given.
For children of school age, a maximum daily dose of 500mg may be
given, while keeping always in mind the 5 – 20 mg/ kg body wt. rule.
The dose should be reduced to its half on the following day, and
subsequently reduced until the maintenance dose of 2.5 –5 mg/kg body
weight is reached.
Croup syndrome
• It is a respiratory disease which afflicts infants and young children,
typically common in infants and children from 3 months to 3 years of
age. However older children may get croup. The respiratory symptoms
are caused by inflammation of the larynx and upper airways, with
resultant narrowing of the airway and a harsh 'barking' cough with
noisy breathing.
Croup is most often caused by parainfluenza virus, primarily types 1
and 3, but other viral and possibly bacterial infections can also cause it.
It is most common in the autumn but can occur year-round, with a
slight predilection for males.
• Treatment:
Treatment of croup syndrome is done with Rectodelt 100mg
suppositories, with a starting dose of 5-20mg/ kg body weight, which
maybe repeated once or twice a day depending on the severity of the
case.
Improvment of the condition is usually noticable within 1and½ hour.
The breathing difficulties usually stop within 24 hours of the
adminstration.
Side-effects
• For short-term therapies that last from 1 to 3 days, a high daily doses
of corticoids can be well tolerated by patients.
• However, if a high dose is continued for a long term, then the well
known side-effects of steroid therapy will become present.
These include: Cushing syndrome, myasthenia gravis, hypertension,
osteoporosis, acne, decreased glucose tolerance, adrenal gland atrophy,
ventricular ulcer, glaucoma, growth retardation in children, weakening
of the immune system, and slow wound healings.
Contraindications
In emergency cases, there is no absolute contraindication to shortterm therapy.
Absolute contraindications otherwise:
Known hypersensitivity reactions to the active ingredient or to any of the
other components of the preparation.
Relative contraindications: In case of long-term therapy, as with other
glucocorticoids the following contraindications are known:
Stomach or duodenal ulcers, sever osteoporosis, sever hypertension,
before and immediately after vaccinations. Viral infections: herpes
simplex, herpes zoster, varicella. Systemic mycosis, amoebiasis,
glaucoma, poliomyelitis (except the bulbar encephalitic form). Lymph
adenitis following following BCG vacination. Like all glucocorticoids
therapies, Rectodelt should only be used after carefull assesment of
benefit/risk ratio.
Drug Interactions
• Simultaneous adminstration of cardiac glycosides may potentiate their
activity, due to steroid-induced excretion of potassium.
• Hypoglycemic effect of anti diabetic agents, and the anti coagulant
properties of coumarin derivatives may be impaired.
• Salicylates and other NSAIDs may increase gastrointestinal
hemorrhage.
• Rifampicine , phenytoin and barbiturates decrease the corticoids
action.