Diazepam

Effect on the body

The mechanism of action of diazepam is its stimulation of benzodiazepine receptors with simultaneous activation of GABA receptors and inhibition in synapses that regulate the emotional sphere, including the thalamus, hypothalamus, reticular formation and limbic system of the brain. Thanks to this effect, when using Diazepam, you can get several effects at once. Its ability to regulate the central nervous system gives the following results:

Soothing. The sedative effect is to relieve anxiety and restlessness, reduce the body’s reactivity to external stimuli, and drowsiness. When using the drug in maximum quantities, inability to concentrate and absent-mindedness may occur. Overdose causes amnesia.
Anxiolytic. A person’s anxiety level decreases, fears and tension go away.
Hypnotic. Inhibiting arousal in the brain and eliminating excessive arousal helps a person normalize sleep and ensures falling asleep quickly.
Anticonvulsant. The muscle relaxant effect of the substance blocks the conduction of impulses along interneurons located in the spinal cord. This allows you to stop seizures and reduce limb tremors.

The drug helps increase the pain threshold, reduces the need for peripheral tissues for oxygen, and eliminates syndromes caused by activation of the autonomic nervous system. All the main effects of Diazepam have a beneficial effect during the treatment of chronic alcoholism. It makes it much easier to survive the signs of withdrawal, stopping most of its symptoms. The medicine helps eliminate hand tremors, psychomotor agitation, anxiety, unmotivated aggression, convulsive syndrome, hallucinosis and reduces the severity of signs of alcoholic delirium.

Indications for use of "Diazepam"

To get the desired result, you need to take the drug as prescribed. You should not use the drug without the advice of a doctor, since Diazepam causes many negative effects and leads to addiction.

Recommended Dosages

According to the instructions, the dosage of Diazepam for an adult is from 4 to 15 mg per day. It is necessary to take the drug by dividing the total dosage into two doses. Parenteral administration is 10-20 mg, and its frequency is determined by a specialist. Withdrawal syndrome is relieved by using a tranquilizer 10 mg up to 4 times a day. After which it is recommended to switch to a maintenance dose of 5 mg 2-4 times a day.

Contraindications

The drug has many side effects. And in some cases its use is contraindicated. "Diazepam" is not recommended for treatment in the following situations and diseases:

glaucoma without aqueous outflow (angle-closure)
functional failure of the kidneys and liver
respiratory disorders
muscular asthenia
sudden drop in blood pressure, shock
loss of consciousness
organic changes in the brain
drug overdose and alcohol poisoning
treatment with drugs that have a depressant effect on the nervous system
intolerance to the active substance and additional components
pregnancy and breastfeeding

Side effects

Before starting treatment, you should carefully read the instructions. Some patients may experience side effects when using Diazepam:

severe drowsiness
weakness, lack of activity
myasthenia gravis
bronchospasm
drop in blood pressure
hiccups (with rapid intravenous administration)
dry mouth
breathing disorder
decreased potency in men (disappears after discontinuation of the drug)
paradoxical arousal
nausea, vomiting and intestinal upset
hyperprolactinemia

If, after taking or administering the drug, negative symptoms are observed or intolerance is detected, you should immediately consult a doctor. It may be necessary to reduce the dose or reconsider treatment in favor of another tranquilizer.

Interaction with alcohol and other drugs

Treatment should never be combined with alcohol. If you take strong drinks at the same time as Diazepam, the likelihood of developing an adverse reaction increases significantly even with a minimum dosage. Intoxication occurs faster, pronounced inhibition of brain structures leads to loss of consciousness and a life-threatening condition.

When using the drug, it is necessary to take into account the peculiarities of its interaction with other drugs. Otherwise, overdose symptoms and negative reactions may be increased or sharply decreased:

the likelihood of side effects increases with the use of anticoagulants and beta blockers
the use of sleeping pills increases drowsiness and lethargy
the use of muscle relaxants can lead to severe weakness and potentiation of the effect of the tranquilizer
joint treatment with antipsychotics increases their effectiveness
Taking antidepressants neutralizes the effects of anxiolytics

Instructions for use DIAZEPAM 2 mg, 5 mg, 10 mg

During the period of treatment with the drug and 3 days after its completion, you should not drink any alcoholic beverages!

Please note that anxiety or tension associated with everyday stress does not usually require treatment with anxiolytics.

Diazepam should be prescribed with extreme caution for severe depression, because the drug can be used to realize suicidal intentions.

If patients experience such unusual reactions as increased aggressiveness, acute states of agitation, anxiety, feelings of fear, thoughts of suicide, hallucinations, increased muscle cramps, difficulty falling asleep, shallow sleep, it is necessary to interrupt treatment with the drug.

The drug should not be used in states of shock, acute alcohol poisoning, coma and head injuries.

If it is necessary to use the drug in patients with liver and kidney diseases, the risk-benefit ratio of therapy should be assessed.

In case of renal or liver failure and long-term use, it is necessary to monitor the peripheral blood picture (morphology with smear) and the activity of liver enzymes.

If it is necessary to use the drug in patients with respiratory failure, sleep apnea syndrome, or coma, a careful assessment of the indications is necessary due to the possibility of respiratory depression in these categories of patients.

The risk of developing drug dependence increases when diazepam is used in high doses, with a significant duration of treatment in patients who have previously abused alcohol or drugs. To reduce the risk of drug dependence, the drug should not be used for a long time. Abrupt cessation of treatment is unacceptable due to the risk of “floppy baby syndrome”) and metabolic disorders in response to cold stress.

Diazepam is excreted in breast milk, so when using the drug during lactation, breastfeeding should be discontinued.

Impact on the ability to drive vehicles and work with dangerous mechanisms.

Diazepam can cause a slowdown in the speed of psychomotor reactions, therefore, during treatment with the drug and 5 days after its completion, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Application in the treatment of alcoholism

Indications for the use of Diazepam in the treatment of chronic alcoholism are the development of delirium and severe withdrawal syndrome. The person’s condition at this moment becomes severe, as there is a failure in the central regulatory system responsible for mood and emotions. Severe stimulation of brain structures is accompanied by life-threatening symptoms.

The mechanism of action of Diazepam is to reduce the excitability of nerve cells. This helps to relieve all the main symptoms and eliminates:

anxiety
psychomotor agitation
sleep disturbance

The drug helps increase the pain threshold, reduces the need for peripheral tissues for oxygen, and eliminates syndromes caused by activation of the autonomic nervous system. All the main effects of Diazepam have a beneficial effect during the treatment of chronic alcoholism. It makes it much easier to survive the signs of withdrawal, stopping most of its symptoms. The medicine eliminates hand tremors, unmotivated aggression, convulsive syndrome, and hallucinosis.

For acute psychotic manifestations in an alcoholic during the withdrawal period, the drug is best administered intravenously or intramuscularly. This allows you to quickly fix the problem. At home, it is recommended to use rectal administration. Oral administration is not always appropriate, especially when nausea and vomiting occur.

When used simultaneously with drugs that have a depressant effect on the central nervous system (including neuroleptics, sedatives, hypnotics, opioid analgesics, anesthetics), the depressant effect on the central nervous system, on the respiratory center, and severe arterial hypotension increases.

When used simultaneously with tricyclic antidepressants (including amitriptyline), it is possible to enhance the inhibitory effect on the central nervous system, increase the concentration of antidepressants and enhance the cholinergic effect.

In patients receiving long-term centrally acting antihypertensive drugs, beta-blockers, anticoagulants, cardiac glycosides, the degree and mechanisms of drug interaction are unpredictable.

When used simultaneously with muscle relaxants, the effect of muscle relaxants is enhanced and the risk of apnea increases.

When used simultaneously with oral contraceptives, the effects of diazepam may be enhanced. The risk of breakthrough bleeding increases.

When used simultaneously with bupivacaine, it is possible to increase the concentration of bupivacaine in the blood plasma; with diclofenac - increased dizziness is possible; with isoniazid - decreased excretion of diazepam from the body.

Drugs that cause induction of liver enzymes, incl. antiepileptic drugs (carbamazepine, phenytoin) can accelerate the elimination of diazepam.

When used simultaneously with caffeine, the sedative and possibly anxiolytic effect of diazepam is reduced.

When used simultaneously with clozapine, severe arterial hypotension, respiratory depression, and loss of consciousness are possible; with levodopa - it is possible to suppress the antiparkinsonian effect; with lithium carbonate - a case of the development of a coma has been described; with metoprolol - a decrease in visual acuity and worsening psychomotor reactions are possible.

When used simultaneously with paracetamol, it is possible to reduce the excretion of diazepam and its metabolite (desmethyldiazepam); with risperidone - cases of the development of NMS have been described.

When used simultaneously with rifampicin, the excretion of diazepam increases due to a significant increase in its metabolism under the influence of rifampicin.

Theophylline in low doses distorts the sedative effect of diazepam.

When used simultaneously in rare cases, diazepam suppresses metabolism and enhances the effect of phenytoin. Phenobarbital and phenytoin may accelerate the metabolism of diazepam.

When used concomitantly, fluvoxamine increases plasma concentrations and side effects of diazepam.

When used simultaneously with cimetidine, omeprazole, disulfiram, it is possible to increase the intensity and duration of action of diazepam.

When taking ethanol and ethanol-containing drugs simultaneously, the inhibitory effect on the central nervous system (mainly on the respiratory center) increases, and pathological intoxication syndrome may also occur.