Situations where rapid action is needed and intravenous administration is not possible or contraindicated: epileptic fever and febrile seizures; relieving muscle contraction caused by tetanus; as a sedative agent in small surgical and dental procedures; initial treatment of anxiety and agitation, when the disorders are severe, impair the patient's activities or cause a very high psychological burden. The drug is particularly useful in the immediate treatment of convulsions in children.
Composition:
2.5 ml solution contains 5 mg or 10 mg diazepam. The preparation contains benzyl alcohol.
Action:
A long-acting benzodiazepine derivative. It has anti-anxiety, anticonvulsant, miorelaxis, sedative and hypnotic properties. Enhances the inhibitory effect of GABAergic transmission at o.u.n. After administration of the solution via rectal administration, diazepam is rapidly and almost completely absorbed through the rectal mucosa. The beginning of the action occurs within a few minutes. Cmaxis reached 10-30 min after administration. In 95-99% it is bound to plasma proteins. It penetrates quickly into the cerebrospinal fluid. It penetrates the placental barrier and is excreted into breast milk. Diazepam is metabolized in the liver. Metabolites (N-desmethylodiazepam - nordiazepam, temazepam, oxazepam) are pharmacologically active. Diazepam has a biphasic half-life with an initial rapid distribution phase followed by an elimination phase of the final elimination lasting 1-2 days. The drug is excreted mainly via the kidneys, partly with bile. The excretion of diazepam may be prolonged in newborns, in elderly patients and in people with liver or kidney disease.
Contraindications:
Hypersensitivity to diazepam, other benzodiazepines or any of the excipients. Myasthenia gravis. Severe respiratory failure. Sleep apnea syndrome. Severe hepatic failure. The product contains benzyl alcohol - do not use in premature babies.
Precautions:
Diazepam is not recommended for the primary treatment of mental illness. It should not be used in patients with phobia or obsessions or in monotherapy in patients with depression or anxiety associated with depression (increased risk of suicide in this group of patients). Particularly cautiously use in patients with personality disorders or revealing aggressive behaviors, including autoaggressive ones, as well as in patients who abuse alcohol or medications in history. Use with caution in patients with impaired renal or hepatic function, chronic lung insufficiency, angle-closure glaucoma, organic brain disorders, especially atherosclerosis. In children, it should only be used if necessary and as short as possible. It is not recommended to use the drug in children with an <10 kg. Caution should be exercised when changing the formulation to a benzodiazepine with short duration of action, as withdrawal symptoms may occur.
Pregnancy and lactation:
The drug should not be used during pregnancy, especially during the first and third trimester, unless the benefits for the mother outweigh the potential risk to the fetus. Diazepam administered during pregnancy may increase the risk of congenital malformations and the onset of mental impairment in a child. Administering the medicine in the third trimester or during delivery is associated with a risk of flaccid assembly (floppy infant syndrome) in a newborn, characterized by: hypothermia, hypotonia, respiratory depression, arrhythmias and sucking reflex. In newborns of mothers who chronically took benzodiazepines later in pregnancy, physical dependence may occur. There is a risk of withdrawal symptoms at birth in these newborns. In addition, the preparation contains benzyl alcohol that can pass through the placenta. After administration of the preparation before or during delivery, any toxic effects of benzyl alcohol on premature babies and newborns should be considered. Diazepam is excreted in human milk. Use during breastfeeding is not recommended.
Side effects:
Common: double vision, muscle weakness, impaired concentration, dullness of emotions, confusion, postmortem disorder, sedative action, drowsiness, headache, dizziness (with the risk of falling in the elderly), discomfort, blurred speech, tremors, tiredness , "hangover". Rare: hypotension, bradycardia, chest pain, hematological disorders (including thrombocytopenia), visual disturbances, dry mouth, nausea, vomiting, epigastric pain, constipation, diarrhea, congestive jaundice, jaundice, urinary retention, disorder libido, menstrual disorders, laryngeal spasm, respiratory depression, apnea, increased appetite. Very rare: cutaneous hypersensitivity reactions (including urticaria and angioneurotic edema). During treatment (especially in children and elderly patients), paradoxical reactions may occur, such as anxiety, agitation, irritability, emotional instability, aggressiveness, fits, hallucinations, nightmares, psychosis symptoms, delusions, inappropriate behavior). Paradoxical reactions should be discontinued. Dacepam may reveal latent depression. Long-term use may lead to a reduction in the effectiveness of hypnotics. Even after therapeutic doses, physical dependence may occur, and discontinuation of diazepam may result in withdrawal symptoms and "rebound" reactions. Mental addiction may occur.
Dosage:
Rectally. The dose is determined individually depending on age, body weight and individual tolerance to the drug. The usual dose is 0.25-0.5 mg / kg. The lowest effective dose should be used. Treatment should last as short as possible. Children: mc. 10-15 kg - 1 tube of 5 mg; mc. > 15 kg - 1 tube of 10 mg. Adults: 2 tubes of 10 mg. In the absence of a therapeutic effect after 10 min children can be repeated dose, while adults can be given an additional 1 tube of 10 mg. The dose can be repeated every 12 hours. If the seizures do not improve despite using the medicine, other anticonvulsants should be used. Elderly people and people in poor general condition should not be given more than half of the dose usually used in adults. Dose reduction is recommended in patients with chronic respiratory failure and in patients with impaired liver or kidney function. Regularly assess the patient's condition and check if further treatment is necessary. Tubes are intended for single use.
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