Oxazepam: instructions for use, analogues, price and reviews

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Active ingredients

Oxazepam

Disease class

Mental and behavioral disorders caused by alcohol consumption - dependence syndrome
Phobic anxiety disorders
Panic disorder [episodic paroxysmal anxiety]
Other neurotic disorders
Disturbances in falling asleep and maintaining sleep [insomnia]
Anxiety and agitation
State of emotional shock and stress, unspecified

Clinical and pharmacological group

Not indicated. See instructions

Pharmacological action

Anxiolytic
Tranquilizing

Pharmacological group

Anxiolytics

Chemical properties

The substance is classified as an anxiolytic of the benzodiazepine series. According to its physical properties, Oxazepam is a white or white with a yellowish tint powder that is insoluble in water, poorly soluble in ethanol , ether , chloroform , and highly soluble in dimethylformamide . Molecular weight = 286.7 grams per mole.

The molecular structure of the drug is similar to diazepam and chlordiazepoxide . The drug is less toxic, has a less pronounced muscle relaxant effect and anticonvulsant effect. Available in the form of 10 mg tablets.

Oral tablets Oxazepam (Oxazepam)

Instructions for medical use of the drug

Description of pharmacological action

Excites benzodiazepine receptors and increases the sensitivity of GABA receptors to the mediator, enhancing the inhibitory effect of GABA on the central nervous system. It has a sedative, hypnotic, muscle relaxant and anticonvulsant effect. In neurotic syndromes, obsessive fear has a stronger effect on the mental than on the autonomic component of fear.

Indications for use

Neuroses; states of anxiety, tension, fear, excitability (with chronic alcoholism); sleep disorders.

Release form

tablets 10 mg; blister 20 box (box) 1;

Pharmacodynamics

Use during pregnancy

Contraindicated during pregnancy. Breastfeeding should be stopped during treatment.

Contraindications for use

Hypersensitivity, myasthenia gravis, liver and kidney diseases, respiratory failure, pregnancy, breastfeeding.

Side effects

Weakness, feeling of fatigue, drowsiness, anxiety, paradoxical reactions (psychomotor agitation, etc.), headache and dizziness, ataxia, decreased blood pressure, urinary disorders, decreased libido, allergic skin reactions.

Directions for use and doses

Inside. Adults: 1–2 tablets. 2-3 times a day, for older people - 1-2 tablets. 2 times a day. Children: 1–3 tablets. per day in 2-3 doses. For inpatient treatment - up to 120 mg/day (maximum daily dose).

Interactions with other drugs

Strengthens the effect of sedatives, hypnotics, psychotropic, antiepileptic drugs, alcohol and anticholinergics. May alter the effect of indirect anticoagulants.

Precautions for use

It should be kept in mind that drug dependence may develop. Use with caution in elderly people with cardiac disorders. With long-term treatment, monitoring of liver function and the composition of cellular elements in peripheral blood is necessary. While taking it, you should not drink alcohol, drive vehicles, operate machinery or engage in activities that require increased attention.

Special instructions for use

Treatment is discontinued gradually, reducing daily doses.

Storage conditions

In a place protected from light.

Best before date

36 months

ATX classification:

N Nervous system

N05 Psycholeptics

N05B Anxiolytics

N05BA Benzodiazepine derivatives

N05BA04 Oxazepam

Pharmacodynamics and pharmacokinetics

Oxazepam acts on specific benzodiazepine receptors, which are located in the postsynaptic gamma-aminobutyric acid of the limbic system of the brain. The substance increases the sensitivity of receptors to gamma-aminobutyric acid . The balance in the cytoplasmic membrane shifts towards chloride ion channels. There is inhibition of neuronal activity due to membrane hyperpolarization. The CNS inhibitory effect of GABA .

The medicine has anxiolytic, sedative and hypnotic effects. After taking the pills, emotional stress decreases, anxiety and fear, and the feeling of restlessness disappear, and patients with insomnia can finally fall asleep. The substance relieves symptoms of alcohol withdrawal . Oxazepam also has an anticonvulsant and central muscle relaxant effect.

With the drug, compared to other benzodiazepine derivatives, there is a large difference between the effective dosage and the dose that causes unwanted side effects. During animal studies, the ability of the drug to cause the growth of benign tumors was discovered. However, in humans, no such pattern was identified during clinical trials.

After taking the tablets, they are absorbed quite slowly in the digestive tract. Oxazepam reaches its maximum concentration in the blood after 60 - 120 minutes, up to 4 hours. The substance has a high degree of binding to plasma proteins (about 98%). To achieve equilibrium concentration in the blood, several days must pass. The drug is well distributed throughout the tissues of the body, overcomes the blood-brain barrier, the placental barrier, and is excreted in breast milk.

Metabolism ( glucuronidation ) occur in the liver tissues; all metabolites formed are inactive. The half-life is from 6 to 10 hours. The medicine is excreted through the kidneys in the form of metabolites. The medicine practically does not accumulate in the body.

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Apo-Lorazepam Oral tablets
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** The Drug Directory is intended for informational purposes only. For more complete information, please refer to the manufacturer's instructions. Do not self-medicate; Before starting to use Oxazepam, you should consult a doctor. EUROLAB is not responsible for the consequences caused by the use of information posted on the portal. Any information on the site does not replace medical advice and cannot serve as a guarantee of the positive effect of the drug.

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Indications for use

Oxazepam is prescribed:

for the treatment of neuroses , neuropathy , conditions accompanied by anxiety, irritability, insomnia and fear;
for senesto-hypochondriacal disorders and obsessive states (if other anxiolytics are poorly tolerated);
for the treatment of autonomic disorders in women during menopause ;
with severe premenstrual syndrome;
as part of a complex treatment of reactive depression ;
during abstinence in alcoholics (combination with other drugs).

Side effects

During treatment with Oxazepam the following are observed:

drowsiness , especially in the initial stages of treatment;
dizziness , general weakness, lethargy, fatigue;
headaches , memory loss, tremors , difficulty speaking;
paradoxical reactions (anxiety, central nervous system excitement);
dry mouth, indigestion , leukopenia ;
liver failure, allergies , decreased and increased libido, fainting;
addiction, withdrawal syndrome , drug dependence.

Rarely occur:

euphoria , numbness, depression , fear, suicidal thoughts and behavior, hallucinations , insomnia ;
agranulocytosis , anemia , constipation, urinary incontinence, and kidney disease;
dysmenorrhea , decreased blood pressure , bulimia , tachycardia .

Oxazepam

From the hematopoietic organs: leukopenia, neutropenia, agranulocytosis (chills, hyperthermia, sore throat, excessive fatigue or weakness), anemia, thrombocytopenia.

From the digestive system: dry mouth or drooling, heartburn, nausea, vomiting, loss of appetite, constipation or diarrhea; liver dysfunction, increased activity of liver transaminases and alkaline phosphatase, jaundice.

From the genitourinary system: urinary incontinence, urinary retention, renal dysfunction, increased or decreased libido, dysmenorrhea.

Allergic reactions: skin rash, itching.

Effect on the fetus: teratogenicity, central nervous system depression, respiratory impairment and suppression of the sucking reflex in newborns whose mothers used the drug.

Other: addiction, drug dependence; decrease in blood pressure; rarely - depression of the respiratory center, visual impairment (diplopia), bulimia, weight loss, tachycardia, anterograde amnesia. If the dose is sharply reduced or taken is stopped - withdrawal syndrome (irritability, headache, anxiety, excitement, agitation, fear, nervousness, sleep disturbances, dysphoria, spasm of smooth muscles of internal organs and skeletal muscles, depersonalization, increased sweating, depression, nausea, vomiting, tremor, perception disorders, including hyperacusis, paresthesia, photophobia, tachycardia, convulsions, hallucinations, rarely - acute psychosis).Overdose. Symptoms: drowsiness (with a single dose exceeding 10 times the therapeutic dose, sleep occurs, from which the patient recovers on his own), confusion, paradoxical arousal, decreased reflexes, stunnedness, decreased response to painful stimuli, deep sleep, dysarthria, ataxia, visual impairment (nystagmus ), tremor, bradycardia, shortness of breath or difficulty breathing, severe weakness, decreased blood pressure, collapse, depression of cardiac and respiratory activity, coma.

Treatment: gastric lavage, forced diuresis, activated charcoal. Symptomatic therapy (maintaining breathing and blood pressure). Flumazenil is used as a specific antagonist (in a hospital setting). Hemodialysis is ineffective.

Overdose

There is an increase in adverse reactions, depression of the central nervous system, up to coma , confusion , drowsiness , lethargy , ataxia , arterial hypotension .

As therapy, it is recommended to lavage the stomach, monitor vital signs, and administration of norepinephrine , an antidote (inpatient), is indicated. Hemodialysis is ineffective.

Interaction

The effectiveness of the drug is reduced when combined with oral contraceptives.

The medicine reduces the bioavailability of zidovudine headaches develop more often .

Combination with phenytoin leads to a decrease in the concentration of Oxazepam.

The medicine cannot be combined with other drugs that depress the central nervous system, MAO inhibitors phenothiazine derivatives .

special instructions

Particular care should be taken when treating patients with arterial hypotension , elderly people, and patients who have previously suffered from drug addiction with Oxazepam.

It is not recommended to treat with the drug for a long time (4 or more weeks). If treatment is necessary over several months, intermittent therapy is used. The pills are discontinued gradually to avoid the development of withdrawal syndrome ( convulsions , tremors , vomiting, spasms and pain, sweating ).

Also, during long-term treatment, it is necessary to monitor liver function and peripheral blood picture.

The drug should not be taken by drivers or if it is necessary to perform work with increased concentration.

NOZEPAM

Dosage form:

pills

Pharmachologic effect:

Anxiolytic drug (tranquilizer) of the benzodiazepine series. It has a sedative-hypnotic, anticonvulsant and central muscle relaxant effect. Strengthens the inhibitory effect of GABA (a mediator of pre- and postsynaptic inhibition in all parts of the central nervous system) on the transmission of nerve impulses. Stimulates benzodiazepine receptors located in the allosteric center of postsynaptic GABA receptors of the ascending activating reticular formation of the brain stem and interneurons of the lateral horns of the spinal cord; reduces the excitability of subcortical structures of the brain (limbic system, thalamus, hypothalamus), inhibits polysynaptic spinal reflexes. The anxiolytic effect is due to the influence on the amygdala complex of the limbic system and manifests itself in a decrease in emotional stress, easing anxiety, fear, and restlessness. The sedative effect is due to the influence on the reticular formation of the brain stem and nonspecific nuclei of the thalamus and is manifested by a decrease in symptoms of neurotic origin (anxiety, fear). The main mechanism of hypnotic action is the inhibition of cells of the reticular formation of the brain stem. Reduces the impact of emotional, vegetative and motor stimuli that disrupt the mechanism of falling asleep. The anticonvulsant effect is realized by enhancing presynaptic inhibition. Suppresses the spread of epileptogenic activity, but does not relieve the excited state of the focus. The central muscle relaxant effect is due to inhibition of polysynaptic spinal afferent inhibitory pathways (to a lesser extent, monosynaptic ones). Direct inhibition of motor nerves and muscle function is also possible. The productive symptoms of psychotic origin (acute delusional, hallucinatory, affective disorders) are practically not affected; a decrease in affective tension and delusional disorders is rarely observed.

Indications:

Neurotic and neurosis-like conditions (including in patients with severe somatic diseases, as well as in elderly patients and children), occurring with irritability, increased fatigue, sleep disturbances, and autonomic disorders. Neuroses (anxiety, nervous tension, fear, sleep disorders); reactive depressive state (in combination with antidepressants); anxiety associated with depression (as part of complex therapy); withdrawal syndrome; vegetative lability (in women - menopause, premenopause).

Contraindications:

Hypersensitivity, coma, shock, acute alcohol intoxication with weakening of vital functions, acute intoxication with drugs that have a depressant effect on the central nervous system (including narcotic analgesics and hypnotic drugs), myasthenia gravis, angle-closure glaucoma (acute attack or predisposition); severe COPD (progression of the degree of respiratory failure), acute respiratory failure, severe depression (suicidal tendencies may be noted), pregnancy (especially the first trimester), lactation period, children (up to 6 years). With caution. Hepatic and/or renal failure, cerebral and spinal ataxia, hyperkinesia, history of drug dependence, tendency to abuse psychoactive drugs, organic brain diseases, psychosis (paradoxical reactions are possible), hypoproteinemia, sleep apnea (established or suspected), advanced age, children age 6-12 years (safety and effectiveness have not been determined).

Side effects:

From the nervous system: at the beginning of treatment (especially in elderly patients) - drowsiness, dizziness, increased fatigue, decreased ability to concentrate, ataxia, unsteady gait and poor coordination of movements, lethargy, dullness of emotions, slowed mental and motor reactions; rarely - headache, euphoria, depression, tremor, depressed mood, catalepsy, memory impairment, dystonic extrapyramidal reactions (uncontrolled movements including the eyes), asthenia, myasthenia during the day, dysarthria, confusion; extremely rarely - paradoxical reactions (aggressive outbursts, psychomotor agitation, fear, suicidal tendencies, muscle spasms, hallucinations, acute agitation, irritability, anxiety, insomnia). From the hematopoietic organs: leukopenia, neutropenia, agranulocytosis (chills, hyperthermia, sore throat, excessive fatigue or weakness), anemia, thrombocytopenia. From the digestive system: dry mouth or drooling, heartburn, nausea, vomiting, loss of appetite, constipation or diarrhea; liver dysfunction, increased activity of liver transaminases and alkaline phosphatase, jaundice. From the genitourinary system: urinary incontinence, urinary retention, renal dysfunction, increased or decreased libido, dysmenorrhea. Allergic reactions: skin rash, itching. Effect on the fetus: teratogenicity, central nervous system depression, respiratory impairment and suppression of the sucking reflex in newborns whose mothers used the drug. Other: addiction, drug dependence; decrease in blood pressure; rarely - depression of the respiratory center, visual impairment (diplopia), bulimia, weight loss, tachycardia, anterograde amnesia. With a sharp reduction in dose or cessation of administration, “hepatic enzyme” syndrome occurs. In elderly patients and people prone to drug abuse, a decrease in blood pressure while taking the drug can lead to cardiac dysfunction. The risk of developing drug dependence increases when using large doses, a significant duration of treatment, and in patients who have previously abused ethanol or drugs. Should not be used for a long time without special instructions. Abrupt cessation of treatment is unacceptable due to the risk of life-saving syndrome. It has a toxic effect on the fetus and increases the risk of birth defects when used in the first trimester of pregnancy. Taking therapeutic doses later in pregnancy may cause depression of the newborn's central nervous system. Chronic use during pregnancy can lead to physical dependence with the development of “flaccid baby” syndrome). During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Interaction:

Reduces the effectiveness of levodopa in patients with parkinsonism. Mutual enhancement of the effect of hypnotics, antiepileptic drugs, neuroleptics, drugs for general anesthesia, narcotic analgesics, indirect muscle relaxants, ethanol. Drugs that block tubular secretion may enhance the effect of oxazepam. Inhibitors of microsomal oxidation prolong T1/2 and increase the risk of developing toxic effects. Inducers of microsomal liver enzymes reduce effectiveness. Narcotic analgesics increase euphoria, leading to an increase in mental dependence. Cimetidine, disulfiram, estrogen-containing oral contraceptives and erythromycin increase the concentration and prolong the effect of the drug (due to inhibition of hepatic metabolism), and have a lesser effect on oxazepam, which binds to glucuronic acid. Antihypertensive drugs can increase the severity of the decrease in blood pressure. Increased respiratory depression may occur during concomitant administration of clozapine. May increase the toxicity of zidovudine. MAO inhibitors, strychnine, corazole and large doses of caffeine weaken the effect of oxazepam.

Drugs containing (Oxazepam analogues)

Level 4 ATC code matches:
Bromazepam

Helex

Rudotel

Relium

Nozepam

Tazepam

Xanax

Elenium

Valium Roche

Alprazolam

Tofisopam

Diazepam

Grandaxin

Mezapam

Sibazon

Seduxen

Relanium

Lorazepam

Analogues: Nozepam , Oxazepam tablets , Tazepam , Vaben , Nozepam tablets 0.01 g.