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Diazepam is chiefly the anxiolytic preparation (or tranquilizer) from the benzodiazepine row. This medication possesses by the expressed anxiolytic, hypnosedative, anti-convulsive and muscular relaxing action. The effect of this drug is usually conditioned by the capability of this medicant to potentate the central activity of the main mediator in the nervous system of patient. Diazepam 100mg 90 pills are the broadly-taken realizing form of this medicament. It is usually applied for monotherapy or complex treating of patients with neurotic conditions (including in combination with anxious syndromes, hysteria, mitochondria, neurasthenia and reactive depression), psychosis, dysphoria and organic illnesses of the central nervous system. The drug is also prescribed under the insomnia and in complex with other medical preparations with alcohol abstinent syndrome (including accompanied by the anxiety, uneasiness, nervous tension, transitory reactive state and psychoneurosis). This officinal agent is also used in the therapy of sick individual with some spasms of the skeletal muscles under the local traumas and also ill persons with spastic conditions which are generally tied together with some lesions of the spinal cord or brain. The medical remedy can be allocated in complex treatment of the patients with myositis, arthritis, bursitis, arthrosis, rheumatoid spondylitis and progressing chronic polyarthritis which are mainly accompanied by the tension of the skeletal muscles. You can buy Diazepam online without any prescriptions from physicians or other medical specialists in this area of medicine. We also suggest the cheapest costs of this officinal product all over the United States.
Generic name: Diazepam
Brand name: Apaurin, Valium, Seduxen, Relanium, Sibazone, Relium
Diazepam - instructions, indications, composition, side effects
- Composition
- Official form
- Pharmacological group
- Pharmacological properties
- Indications
- Contra-indications
- Interaction with other officinal remedies and other views of interaction
- Specifics of applying
- Application under the pregnancy and breast-feeding
- Capability to influence on the reaction speed under control by motor transport or other mechanisms
- Applying ways and dosing
- Overdose
- Side effects
- Keeping time
- Keeping conditions
- Package
- Analogs
Composition
Active ingredient: Diazepam.
1 tablet contains Diazepam 5 mg (0.005 g) or 10 mg (0.01 g).
Excipients: lactose, potato starch, gelatin, calcium stearate.
Official form
Tablets of white color, a flat-cylindrical form, with a facet and risky.
Pharmacological group
Anxiolytics. Benzodiazepine derivatives. ATC code N05B A01.
Pharmacological properties
Pharmacological. Diazepam is one of the main benzodiazepine tranquilizers. It has anxiolytic, central muscle relaxant, anticonvulsant, sedative and moderate hypnotic effect. It shows insignificant vegetative activity.
The mechanism of action of medication is associated with GABA, which is an inhibitory mediator in the central nervous system. It is known that GABAergic neurons inhibit the activity of other types of neurons. The drug reduces the activity of the enzyme GABA transaminase, thereby increasing the content of GABA in the brain. On the other hand, the sensitivity of membranes to GABA increases. All this enhances the inhibitory effect of GABAergic neurons on other types of neurons. Inhibition of noradrenergic and dopaminergic neurons is due to the sedative and hypnotic effects of diazepam and other benzodiazepines. Anticonvulsant and muscle relaxant actions are caused by inhibition of the corresponding neurons of the cortical centers and the spinal cord. Inhibition of excitation processes in the ladder reticular system leads to the development of an anxiolytic effect.
Pharmacokinetics:
absorption
Diazepam is rapidly and completely absorbed in the digestive tract, the maximum concentration in plasma is reached 30 to 90 minutes after oral administration.
distribution
Diazepam and its metabolites are largely associated with plasma proteins (diazepam 98%), penetrate the blood-brain and placental barriers, pass into breast milk at a concentration that is about 1/10 of the concentration of diazepam in the mother’s blood plasma. The volume of distribution is 1 – 2 l / kg.
metabolism
Diazepam is predominantly metabolized to pharmacologically active metabolites (N-desmethyldiazepam, temazepam and oxazepam). Oxidative metabolism of diazepam is carried out with the participation of CYP3A and CYP2C19 isoenzymes. Subsequently, oxazepam and temazepam are conjugated with glucuronic acid.
Withdrawal
After taking the drug, the decrease in the concentration of diazepam in the blood plasma takes place in two phases: the initial phase of rapid distribution changes the prolonged elimination phase (half-life of 48 hours). The half-life of the active metabolite of N-desmethyldiazepam can reach 100 hours. Diazepam and its metabolites are mainly excreted in the urine in conjugated forms. The clearance of diazepam is 20 – 30 ml / min.
Metabolites of diazepam can remain intact for up to 2 weeks.
The half-life may be lengthened in newborns, the elderly and patients with impaired liver function. Reduced renal function does not affect the half-life of diazepam.
Indications
Adults.
- Anxiety disorders.
- Insomnia (benzodiazepines are indicated only for severe disorders, especially for patients with critical pathological conditions).
- Elimination of muscle spasms associated with cerebral etiology spasms.
- In the complex treatment of epilepsy.
Contra-indications
Hypersensitivity to benzodiazepines or to any of the components of the drug. Myasthenia gravis, severe respiratory failure, sleep apnea syndrome, severe liver failure, phobic or obsessive states, chronic psychosis, alcohol and drug addiction (with the exception of acute withdrawal syndrome).
Interaction with other officinal remedies and other views of interaction
Pharmacokinetics of the interaction. Oxidative metabolism of diazepam is carried out with the participation of CYP3A and CYP2C19 isoenzymes. Oxazem and temazepam are further conjugated with glucuronic acid.
Substances that are CYP3A and / or CYP2C19 modulators may alter the pharmacokinetics of diazepam. Medicines cimetidine, ketoconazole, fluvoxamine, fluoxetine and omeprazole inhibit CYP3A and CYP2C19, which can lead to increased and prolonged sedation. There is evidence that the metabolic elimination of phenytoin affects diazepam.
Cisapride can lead to a temporary increase in sedation with oral administration of benzodiazepines due to rapid absorption.
Pharmacological interactions
An increase in sedation, respiration, and hemodynamics can occur with simultaneous use of diazepam with centrally acting depressants such as antipsychotics, tranquilizers / sedatives, antidepressants, hypnotics, antiepileptic drugs, narcotic analgesics, anesthetics, and sedative antihistamines or alcohol.
Do not drink alcohol during benzodiazepine treatment.
Specifics of applying
Simultaneous use of alcohol / depressants of the central nervous system (CNS)
Alcohol and / or CNS depressants should not be consumed during treatment with diazepam. This combination enhances the clinical effects of benzodiazepines, including severe sedation, clinically associated with the treatment of respiratory and / or cardiovascular depression.
Diazepam is with caution prescribed to patients with the history of abuse of alcohol or narcotic drugs. It is not recommended for patients who are dependent on the use of antidepressants of the central nervous system or alcohol, except for the period of exacerbation of withdrawal symptoms.
tolerance
The use of diazepam for several weeks may lead to a weakening of its hypnotic effects due to the development of tolerance.
addiction
When taking benzodiazepines (even in therapeutic doses) addiction, the formation of mental and physical dependence may appear. The risk of addiction increases with the use of large doses and with an increase in the duration of treatment, as well as in patients with alcohol or drug addiction in history, personality disorders. Regular monitoring is necessary for such patients. Repeated administration of the drug should be avoided, treatment should be stopped gradually.
withdrawal syndrome
Sudden cessation of benzodiazepine use is accompanied by withdrawal syndrome. Symptoms of withdrawal syndrome: headache, muscle pain, increased anxiety, tension, agitation, confusion, irritability. In severe cases, there can be derealization (perception of the surrounding world), depersonalization, numbness and tingling in the extremities, increased sensitivity to light, noise and physical contact, hallucinations or epileptic seizures.
Recovery of insomnia and anxiety symptoms
Abrupt cessation of Diazepam treatment can trigger the rebound phenomenon, which is manifested by an exacerbation of the condition with subsequent rapid reduction of symptoms (mood changes, anxiety or sleep disturbance, anxiety). To prevent the rebound / withdrawal syndrome phenomenon, it is recommended to gradually lower the dose of the preparation.
duration of treatment
The duration of treatment should be as short as possible depending on the indication, but should not exceed 4 weeks for insomnia, anxiety states 8 to 12 weeks, including a period of gradual reduction of the drug dose. The duration of treatment is increased only after a thorough assessment of the patient’s condition.
Patients should be informed of the beginning and duration of treatment and explained about the gradual reduction of the dose. In addition, the patient should be warned about the possible occurrence of withdrawal symptoms to reduce anxiety, especially when discontinuing therapy with the drug.
In the case of benzodiazepines with a short duration of action, withdrawal symptoms may occur between taking the drug, especially when the dose is high. Due to the risk of developing withdrawal symptoms, it is not recommended to change benzodiazepines with a long-term effect on benzodiazepines with a short duration of action.
amnesia
It should be borne in mind that benzodiazepines can cause anterograde amnesia. Anterograde amnesia can occur when therapeutic doses are applied, the risk increases with higher doses. Amnestic effects may be associated with inappropriate behavior. The condition manifests itself most often within a few hours after taking benzodiazepines internally, and therefore, in order to reduce the risk, patients should be given the option of continuous sleep 7 – 8:00.
Mental and paradoxical reactions
While taking benzodiazepines, reactions such as anxiety, agitation, irritability, aggressiveness, delirium, anger, nightmares, hallucinations, psychosis, inappropriate behavior and other behavioral disorders are possible. If these reactions occur, discontinue treatment with the medication. Such reactions are more often observed in children and the elderly.
Special groups of patients
Elderly patients and weakened patients need a dose reduction. In connection with the muscle relaxant effect, there is a risk of falls and fractures in this group of patients. Low doses are also recommended for patients with chronic pulmonary insufficiency due to the risk of respiratory depression.
Benzodiazepines are not prescribed to treat patients with severe liver failure, as they can provoke encephalopathy. For patients with chronic liver disease doses should be reduced. Drugs are not recommended for the primary treatment of psychosis. Benzodiazepines should not be used as monotherapy for the treatment of depression or anxiety related to depression, because of the possibility of suicidal behavior in these patients. Benzodiazepines should not be used only to treat depression or anxiety associated with depression, because of the possibility of suicidal behavior in these patients. Preparation can delay the psychological recovery of patients from the symptom complex caused by the severe loss of a loved one. During treatment with Diazepam drinking alcohol is unacceptable. Medication contains lactose, so it should not be prescribed to patients with rare hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome.
Application under the pregnancy and breast-feeding
It is not applicable during pregnancy. Diazepam passes into breast milk, so if you need drug treatment, you should stop breastfeeding. If the medicine is prescribed to women of reproductive age, it is necessary to inform the doctor about stopping the treatment if women become pregnant or suspect that they are pregnant.
Use in children
Benzodiazepines are used in children only in cases of urgent need only when it is not possible to take other alternative medicines.
The duration of treatment should be as short as possible.
Capability to influence on the reaction speed under control by motor transport or other mechanisms
During treatment, you should refrain from driving or working with machinery.
Applying ways and dosing
For optimal therapeutic effect, the doctor selects the dose individually for each patient. Treatment should begin with the minimum effective dose corresponding to a particular indication.
Tablets are taken orally.
Duration of treatment
The duration of treatment should be as short as possible depending on the indication. In the treatment of insomnia, the duration of the course should not exceed 4 weeks, and in states of anxiety, 8 to 12 weeks, including a period of gradual dose reduction.
At the beginning of treatment, it is necessary to inform the patient that the therapy will have a limited duration, and to explain the scheme of gradual dose reduction. In order to reduce anxiety due to the rebound phenomenon, the patient should be aware of the possibility of its occurrence during the treatment period. (See “Features of the application”).
It should be borne in mind that when using benzodiazepines with a short duration of action, symptoms of withdrawal symptoms may appear in the intervals between single doses, especially when using large doses. When using benzodiazepines with a long-term effect, they should not be replaced with short-acting benzodiazepines because of the possibility of the development of withdrawal syndrome.
adults
The doctor selects the dose individually, depending on the patient’s condition.
alarm states
The usual dose is 5 mg per day. The maximum dose is up to 30 mg per day in divided doses. The dosage regimen is determined by the doctor individually.
Insomnia associated with anxiety in adults 5 to 15 mg at bedtime. It is necessary to apply the most effective doses to eliminate the symptoms of the disease. Do not continue treatment in a full dose for more than 4 weeks. Long-term use of the medicine is not recommended.
Withdrawal of the preparation should be carried out by gradually reducing the dosage. For patients who have been using benzodiazepines for a long time, a longer period may be required to reduce the dose. Only a doctor can reduce the dosing.
Muscle Spasms
Muscle spasms: 5 – 15 mg per day in divided doses. Spasms of cerebral etiology in some cases – 2 – 60 mg per day in divided doses.
Sedation
Adults – 5 to 20 mg. Children are prescribed 2 to 10 mg.
Benzodiazepines should not be given to children without a thorough assessment of the evidence. Duration of treatment should be kept to a minimum.
Overdose
Symptoms: drowsiness, ataxia, dysarthria and nystagmus. An overdosage of the medicine can rarely cause a threat to life, but can lead to a lack of reflexes, apnea, hypotension, depression of the cardio-respiratory system and coma. Coma usually lasts several hours, but can be long and cyclical, especially in elderly patients. Respiratory depression with benzodiazepines in patients with diseases of the respiratory system has a severe course.
Benzodiazepines enhance the effects of other central nervous system depressants, including alcohol.
Treatment: monitoring of the basic vital functions of the body. Symptomatic therapy is aimed at maintaining the functions of the cardiovascular, respiratory systems and the central nervous system.
Side effects
Most often there is increased fatigue, drowsiness, muscle weakness. In most cases, after several days of intake, they spontaneously disappear. They can also be avoided by lowering the dose of the medication.
Nervous system disorders: ataxia, dysarthria, speech disorder, headache, tremor, dizziness, worsening of mood, anger. With increasing therapeutic dose of the drug the risk of anterograde amnesia increases. Amnestic effects may be accompanied by abnormal behavior.
Mental disorders: anxiety, agitation, irritability, aggressiveness, delirium, hostility, nightmares, hallucinations, psychosis, behavioral changes and other adverse behavioral effects (mainly in children and the elderly, if they occur, the remedy should be discontinued) consciousness, emotional poverty, loss of attention, depression.
Prolonged use of the medicament (even at therapeutic doses) can lead to the development of physical dependence: cessation of therapy can cause withdrawal syndrome or rebound phenomenon. There have been reports of benzodiazepine abuse.
Injuries, poisoning, procedural complications: an increased risk of falls and fractures when using benzodiazepines was registered in elderly patients.
Digestive tract: nausea, dry mouth or hypersalivation, constipation and other gastrointestinal disorders.
Organ of vision: diplopia, blurred vision.
Cardiovascular system: arterial hypotension, circulatory failure, heart failure, including cardiac arrest.
Urinary system: incontinence or urinary retention.
Skin: skin reactions.
Hearing: vertigo.
Respiratory system: respiratory depression, including respiratory failure.
Digestive system: very rarely – jaundice.
Others: pain in the joints, changes in libido.
Laboratory indicators: disturbance of a cardiac rhythm; very rarely – increased levels of transaminases, alkaline phosphatase in the blood.
Keeping time
Three years.
Keeping conditions
Store in the original package at a temperature not higher than 25°C. Keep out of the reach of children.
Package
Tablets on 5 mg No. 20 (10 × 2) 10 mg No. 20 (10 × 2) in blisters in a pack.
Analogs
Valium, Vazepam, Diazepam Intensol, Diastat
- Composition
- Official form
- Pharmacological group
- Pharmacological properties
- Indications
- Contra-indications
- Interaction with other officinal remedies and other views of interaction
- Specifics of applying
- Application under the pregnancy and breast-feeding
- Capability to influence on the reaction speed under control by motor transport or other mechanisms
- Applying ways and dosing
- Overdose
- Side effects
- Keeping time
- Keeping conditions
- Package
- Analogs