Stimulates benzodiazepine receptors located in the allosteric center of postsynaptic GABA receptors ascending activating reticular formation of the brain and the neurons of the lateral horn of the spinal cord, reduces the excitability trenbolone enanthate of the subcortical structures of the brain (the limbic system, thalamus, hypothalamus), inhibits polisinapticheskie spinal reflexes.
The anxiolytic effect is due to the influence on the amygdala of the limbic system and manifests itself in the reduction of emotional stress, anxiety, weakening, fear, anxiety. The sedative effect is due to the influence on the reticular formation of the brain stem and the nonspecific thalamic nuclei and manifested a decrease in symptoms of neurotic origin (anxiety, fear).
The main mechanism of hypnotic action is inhibition of the reticular formation cells brainstem. It reduces the impact of emotional, autonomic and motor stimuli that disturb sleep.
Anticonvulsant action is realized by increasing presynaptic inhibition. It suppresses the spread of epileptogenic activity, but does not eliminate the excited state of the hearth.
The central muscle relaxant effect is due to inhibition of polysynaptic spinal afferent inhibitory ways (to a lesser extent and monosynaptic). Perhaps, and direct inhibition of motor nerve and muscle function.
In the productive psychotic symptoms genesis (acute delusional, hallucinatory, affective disorders) has practically no effect, it is rarely observed decrease in affective intensity, delusional disorders.
After intake of rats is slow but complete. Relationship to plasma proteins – 97%. The time required to reach maximum concentration -. 4.1 h maximum concentration of 450 ng / mL after administration of a dose of 30 mg. It penetrates through the blood-brain barrier (BBB), the placenta, into breast milk.
Neurotic and neurosis-like states (including in patients with severe medical conditions, as well as in elderly patients) occurring with irritability, fatigue, sleep disorders, autonomic disorders.
Neuroses (anxiety, nervous tension, anxiety, sleep disorders); reactive depression (in combination with antidepressants); anxiety associated with depression (in the complex therapy); withdrawal symptoms;vegetative lability (women – menopause, preklimaks).
Hypersensitivity, coma, shock, acute alcohol intoxication with the weakening of vital functions, acute intoxication of drugs, causing a dampening effect on the central nervous system (including narcotic analgesics and hypnotics drugs), myasthenia gravis, angle-closure glaucoma trenbolone enanthate (acute onset or predisposition) severe chronic obstructive pulmonary disease (progression of the degree of respiratory failure), acute respiratory failure, severe depression (suicidal tendencies may be observed), pregnancy (especially I trimester), lactation, children under 18 years.
Precautions : Hepatic and / or renal failure, cerebral and spinal ataxia, hyperkinesis, drug dependency history, the propensity to abuse drugs, organic brain disease, psychosis (possible paradoxical reactions), hypoproteinemia, sleep apnea (or suspected) , elderly age.
Dosing and Administration
Inside, regardless of meals, at an initial dose of 10 mg 2-3 times a day; outpatient treatment, the mean dose – 30-50 mg / day, with inpatient treatment, especially in acute and severe conditions – up to 120 mg / day.
Insomnia -. 10-30 mg for 1 h before bedtime
Alcohol withdrawal – 10-30 mg 3 . -4 times daily
in elderly initially – 10 mg three times a day, if necessary, taking into account increased tolerability of dose to 20 mg three times a day; You can take one 10 mg twice a day; patients older than 65 years -. not more than 40 mg / day
Duration of treatment is determined individually, on average it is 2-4 weeks.
Abolition of the drug or the end of a course of therapy is carried out gradually.
From the nervous system: at the beginning of treatment (particularly in elderly patients) – drowsiness, dizziness, fatigue, decreased ability to concentrate, ataxia, unsteady gait and poor coordination of movements, lethargy, blunting of emotions, mental retardation and motor responses; rarely – headache, euphoria, depression, tremors, depressed mood, catalepsy, memory impairment, extra pyramidal dystonic reactions (uncontrolled movements including eye), asthenia, myasthenia gravis during the day, dysarthria, confusion; very rarely – paradoxical reaction (aggressive outbursts, agitation, anxiety, suicidal tendencies, muscle spasms, hallucinations, severe agitation, irritability, anxiety, insomnia). From the side of hematopoiesis: leukopenia, neutropenia, agranulocytosis (chills, pyrexia, sore throat , unusual tiredness or weakness), anemia, thrombocytopenia. From the digestive system: dry mouth or salivation, heartburn, nausea, vomiting, loss of appetite, constipation or diarrhea; abnormal liver function, increased activity of “liver” transaminases and alkaline phosphatase, jaundice. From the urogenital system: urinary incontinence, urinary retention, impaired function by check, increased or decreased libido, dysmenorrhea. Allergic reactions: skin rash, itching. The impact on the fetus : teratogenicity, central nervous system depression, respiratory failure and suppression of sucking reflex in infants whose mothers used the drug. Other: addiction, drug dependency; reduction of blood pressure (BP), rarely – depression of the respiratory center, blurred vision (diplopia), bulimia, weight loss, tachycardia, anterograde amnesia. With a sharp decrease in dose or cessation of reception – syndrome “cancel” (irritability, headache, anxiety, excitement, agitation, anxiety, nervousness, sleep disturbances, dysphoria, a spasm of smooth muscles of internal organs and skeletal muscles, depersonalization, increased sweating, depression, nausea, vomiting, tremors, disorders of perception, including hyperacusis, paresthesia, photophobia, tachycardia, convulsions, hallucinations, rare – acute psychosis).
Symptoms: drowsiness (with a single excess of the therapeutic dose of 10 times there comes a sleep from which the patient comes alone), confusion, paradoxical excitement, reduced reflexes, stupor, decreased response to pain stimuli, deep sleep, dysarthria, ataxia, blurred vision (nystagmus ), tremor, bradycardia, dyspnea or shortness of breath, severe weakness, decreased blood pressure, collapse, depression of cardiac and respiratory activity, coma. Treatment: gastric lavage, forced diuresis, administration of activated charcoal. Symptomatic therapy (maintenance of respiration and blood pressure). As a specific antagonist flumazenil is used (in a hospital). Hemodialysis is ineffective.
Interaction with other drugs
Reduces the effectiveness of levodopa in patients with Parkinson’s disease.
The mutual reinforcement of hypnotic action of antiepileptic drugs, antipsychotic drugs, drugs for general anesthesia, narcotic analgesics, indirect muscle relaxants, ethanol.
Drugs that block calcium secretion may increase the effects of oxazepam.
Inhibitors of microsomal oxidation extend T 1 / 2 , increase the risk of toxic effects.
Inductors microsomal liver enzymes decrease the efficiency.
Narcotic analgesics increase the euphoria, leading to an increase in psychological dependence.
cimetidine, disulfiram, estrogensoderzhaschie oral contraceptives and erythromycin increase the concentration and prolong the effect of the drug (due to inhibition of hepatic metabolism) to a lesser extent affect oxazepam binding to glucuronic acid.
Antihypertensive drugs may increase the severity of blood pressure lowering.
against the background of the simultaneous appointment of clozapine may increase the respiratory depression.
It may increase the toxicity of zidovudine.
monoamine oxidase inhibitors, strychnine, korazol and large doses of caffeine weaken the effects of oxazepam.
During treatment the patient strictly prohibited the use of ethanol.
In renal / hepatic failure and prolonged treatment is necessary to monitor the car mud peripheral blood and “liver” enzymes.
In elderly patients, those who are likely to abuse drugs, reduction of blood pressure in patients receiving the drug may cause to a violation of cardiac activity.
The risk of drug dependence increases when using large doses, a significant duration of treatment in patients who previously abused drugs or ethanol. Without specific instructions, should not be used for a long time.
It is unacceptable abrupt discontinuation of treatment because of the risk of the syndrome of “cancellation” (headache, myalgia, anxiety, tension, confusion, irritability, and in severe cases – derealization, depersonalization, hyperacusis, photophobia, paresthesia extremities, hallucinations and seizures).
If you have patients with such unusual reactions such as increased aggression, acute state of excitement, anxiety, suicidal thoughts, hallucinations, increased muscle cramps, difficult to fall asleep, shallow sleep, treatment should be discontinued.
In the period of pregnancy is used only in exceptional cases and only for the “life” readings. It has a toxic effect on the fetus and increase the risk of birth defects when used in the I trimester of pregnancy.Therapeutic dose in the later stages of trenbolone enanthate pregnancy can cause depression of the central nervous system of the newborn. The constant use during pregnancy may lead to physical dependence with the development of the syndrome of “cancellation” of the newborn.
Children, especially at a younger age, are very sensitive to central depressant action of benzodiazepines.
Using just before birth or during labor may cause neonatal respiratory depression, decreased muscle tone, hypotension, hypothermia and a weak act of sucking ( “floppy baby” syndrome).
In the period of treatment must be careful when driving and occupation of other potentially hazardous activities that require high concentration and psychomotor speed reactions. decaprime