1. Name Of The Medicinal Product
Stesolid® rectal tubes 5 mg.
2. Qualitative And Quantitative Composition
Diazepam 2 mg/ml.
3. Pharmaceutical Form
Enema.
4. Clinical Particulars
4.1 Therapeutic Indications
Diazepam has anticonvulsant, sedative, and muscle relaxant properties. It is used in the treatment of severe anxiety and tension states, as a sedative and premedication, in the control of muscle spasm, and in the management of alcohol withdrawal symptoms.
Stesolid rectal tubes 5 mg may be used in acute severe anxiety and agitation, epileptic and febrile convulsions, tetanus, as a sedative in minor surgical and dental procedures, or in other circumstances in which a rapid effect is required but where intravenous injection is impracticable or undesirable.
Stesolid rectal tubes 5 mg may be of particular value for the immediate treatment of convulsions in infants and children.
4.2 Posology And Method Of Administration
Sensitivity to diazepam varies with age.
Children above 1 year of age: 0.5 mg/kg body weight
Adults: 0.5 mg/kg body weight
Elderly patients: 0.25 mg/kg body weight
A maximum dose of 30 mg diazepam is recommended, unless adequate medical supervision and monitoring are available.
4.3 Contraindications
Myasthenia gravis, hypersensitivity to benzodiazepines, severe respiratory insufficiency, sleep apnoea syndrome, severe hepatic insufficiency and porphyria.
4.4 Special Warnings And Precautions For Use
Tolerance
Some loss of efficacy to the hypnotic effects of diazepam may develop after repeated use for a few weeks.
Dependence
Use of benzodiazepines may lead to development of physical and psychic dependence upon these products. The risk of dependence increases with dose and duration of treatment; it is also greater in patients with a history of alcohol or drug abuse.
Once physical dependence has developed, abrupt termination of treatment will be accompanied by withdrawal symptoms. These may consist of headaches, muscle pain, extreme anxiety, tension, restlessness, confusion and irritability. In severe cases the following symptoms may occur: derealisation, depersonalisation, hyperacusis, numbness and tingling of the extremities, hypersensitivity to light, noise and physical contact, hallucinations or epileptic seizures.
Rebound insomnia and anxiety: a transient syndrome whereby the symptoms that led to treatment with a benzodiazepine recur in an enhanced form may occur on withdrawal of treatment. It may be accompanied by other reactions including mood changes, anxiety or sleep disturbances and restlessness. Since the risk of withdrawal phenomena/rebound phenomena is greater after abrupt discontinuation of treatment, it is recommended that the dosage is decreased gradually.
Psychiatric and paradoxical reactions
Reactions like restlessness, agitation, irritability, aggressiveness, delusion, rages, nightmares, hallucinations, psychosis, inappropriate behaviour and other adverse behavioural effects are known to occur when using benzodiazepines. Should this occur, use of the medicinal product should be discontinued.
They are more likely to occur in children and the elderly.
Specific patient groups
Benzodiazepines should not be given to children without careful assessment of the need to do so; the duration of treatment must be kept to a minimum. Elderly should be given a reduced dose (see posology). A lower dose is also recommended for patients with chronic respiratory insufficiency due to the risk of respiratory depression. Benzodiazepines are not indicated to treat patients with severe hepatic insufficiency as they may precipitate encephalopathy.
Benzodiazepines are not recommended for the primary treatment of psychotic illness.
Benzodiazepines should not be used alone to treat depression or anxiety associated with depression (suicide may be precipitated in such patients).
In common with other benzodiazepines, the use of diazepam may be associated with amnesia and should not be used in cases of loss or bereavement as psychological adjustment may be inhibited.
Stesolid rectal tubes 5 mg should not be used in phobic or obsessional states, as there is insufficient evidence of efficacy and safety in such conditions.
Benzodiazepines should be used with extreme caution in patients with a history of alcohol or drug abuse.
4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction
- Not recommended: concomitant intake with alcohol.
The sedative effects may be enhanced when the product is used in combination with alcohol. This affects the ability to drive or use machines.
- Take into account: combination with CNS depressants.
Enhancement of the central depressive effect may occur in cases of concomitant use with antipsychotics (neuroleptics), hypnotics, anxiolytics/sedatives, antidepressant agents, narcotic analgesics, anti-epileptic products, anaesthetics and sedative antihistamines.
In the case of narcotic analgesics enhancement of the euphoria may also occur leading to an increase in psychic dependence.
Compounds which inhibit certain hepatic enzymes (particularly cytochrome P450) may enhance the activity of benzodiazepines. To a lesser degree this also applies to benzodiazepines that are metabolised only by conjugation.
4.6 Pregnancy And Lactation
In animal studies administration of benzodiazepines during gestation has lead to cleft palate, CNS malformation and permanent functional disturbances in the offspring.
There is no evidence as to the safety of diazepam in human pregnancy. It should not be used, especially during the first and last trimesters, unless the benefit is considered to outweigh the potential risk.
In labour, high single doses or repeated low doses have been reported to produce hypotonia, poor sucking, and hyperthermia in the neonate, and irregularities in the foetal heart.
If benzodiazepines are prescribed to a woman of childbearing potential, she should be warned to contact her physician regarding discontinuance of the product if she intends to become or suspects that she is pregnant.
If, for compelling medical reasons, the product is administered during the late phase of pregnancy, or during labour at high doses, effects on neonate, such as hypothermia, hypotonia and moderate respiratory depression, can be expected, due to the pharmacological action of the compound.
Infants born to mothers who took benzodiazepines chronically during the later states of pregnancy may have developed physical dependence and may be at some risk for developing withdrawal symptoms in the postnatal period.
Since benzodiazepines are found in breast milk, benzodiazepines should not be given to breast feeding mothers.
4.7 Effects On Ability To Drive And Use Machines
Sedation, amnesia, impaired muscular function may adversely affect the ability to drive or use machines. If insufficient sleep occurs, the likelihood of impaired alertness may be increased (see also Interactions).
4.8 Undesirable Effects
The side effects of diazepam are usually mild and infrequent.
The most common side effects are drowsiness, light-headedness, unsteadiness, and ataxia. Elderly patients are particularly susceptible to these effects.
Rare side effects include hypotension, apnoea, gastrointestinal and visual disturbances, skin rashes, urinary retention, headache, confusion, vertigo, changes in libido, blood dyscrasias, jaundice and respiratory depression.
Paradoxical reactions to the benzodiazepines, provoking excitement instead of sedation, have been reported.
4.9 Overdose
As with other benzodiazepines, overdose should not present a threat to life unless combined with other CNS depressants (including alcohol).
In the management of overdose with any medical product, it should be borne in mind that multiple agents might have been taken.
Overdose of benzodiazepines is usually manifested by degrees of central nervous system depression ranging from drowsiness to coma. In mild cases, symptoms include drowsiness, mental confusion and lethargy, in more serious cases, symptoms may include ataxia, hypotonia, hypotension, respiratory depression, rarely coma and very rarely death.
Emergency procedure is to secure adequate airway maintenance. Otherwise, the treatment is symptomatic. Intravenous fluids may be administered and Flumazenil may be useful as an antidote.
5. Pharmacological Properties
5.1 Pharmacodynamic Properties
Pharmacotherapeutic group: Diazepam has anticonvulsant, sedative, and muscle relaxant properties.
5.2 Pharmacokinetic Properties
Absorption: Diazepam is quickly absorbed from the rectal mucosa. The maximum serum concentration is reached within 17 minutes. Absorption is 100% compared with that of intravenous injection of diazepam.
5.3 Preclinical Safety Data
Not applicable.
6. Pharmaceutical Particulars
6.1 List Of Excipients
Benzoic acid
Ethanol
Propylene glycol
Sodium benzoate
Benzyl alcohol
Purified water.
6.2 Incompatibilities
None known.
6.3 Shelf Life
30 months at 25°C.
6.4 Special Precautions For Storage
The storage temperature must not exceed 25°C.
6.5 Nature And Contents Of Container
Carton containing sealed low density polyethylene tubes, single packed in aluminium laminated bags.
Package size: 5 x 2.5 ml
6.6 Special Precautions For Disposal And Other Handling
Not applicable.
Administrative Data
7. Marketing Authorisation Holder
Actavis Group PTC ehf.
Reykjavikurvegi 76-78
220 Hafnarfjordur
Iceland
8. Marketing Authorisation Number(S)
PL 30306/0040
9. Date Of First Authorisation/Renewal Of The Authorisation
01/06/2007
10. Date Of Revision Of The Text
31/07/2007
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