Valium

Valium is an anxiolytic-type medicine, a tranquilizer.

Indications of the valium

It is used to eliminate such violations:

• anxiety disorders;
• insomnia;
• caused by local trauma spasm in the musculature of the skeleton;
• spastic disorders due to cerebrospinal or cerebrospinal lesions. Among them are cerebral palsy, as well as athetosis and tetanus;
• arthritis with myositis and bursitis, and in addition, rheumatic spondylitis and progressive polyarthritis (chronic form);
• vertebral syndrome, tension, headaches and angina pectoris, as well as arthrosis, in which the tension of skeletal muscles is observed;
• an abstinent condition that manifests itself in the form of sensation of tension, anxiety and excitation, and also in the form of tremors and transient reactive conditions.

As an adjunct for combined treatment, they are used for such problems:

• dystrophy;
• increased blood pressure;
• disorders of psychosomatic nature in obstetrics and gynecology (among them menopause, menstrual disorders, and gestosis);
• ulcers inside the duodenum a gut or a stomach;
• an epistatus;
• eczema and other dermatological diseases, in which irritability with itching is observed;
• Meniere's syndrome;
• intoxication with drugs.

In addition, Valium is used before endoscopic procedures, general anesthesia and surgical operations (as a means of premedication).

[1], [2], [3], [4]

Release form

Release in tablets with a volume of 2, 5 or 10 mg. Inside the pack - 30 or 500 tablets 2 mg; 25, 100 or 500 tablets 5 mg; 25, 100, 500 tablets with a volume of 10 mg.

[5], [6], [7], [8], [9], [10]

Pharmacodynamics

Diazepam is an active component of Valium. It has a powerful sedative, hypnotic and anticonvulsant effect, as well as a central muscle relaxant effect. The anxiolytic properties of drugs manifest themselves in the form of a relief of a feeling of inner fear, anxiety, and anxiety and tension.

The degree of drug exposure to the central nervous system depends on the size of the daily dosage of diazepam: when administered in small amounts (within 2-15 mg), it has a stimulating effect, but at high doses (more than 15 mg) it causes sedation.

The central muscle relaxant effect is due to the fact that diazepam is able to slow down the spinal reflexes of the polysynaptic type. In addition, the drug also has weak sympatholytic properties - it helps to lower the blood pressure a little. The drug increases the pain threshold, increases the stability of the brain with respect to hypoxia, as well as the expansion of coronary vessels.

The drug has powerful anticonvulsant and anticonvulsant properties, manifested in the form of oppression of paroxysms (sympathoadrenal and parasympathetic type).

[11], [12], [13], [14], [15], [16]

Pharmacokinetics

After oral administration of the pill, the substance is quickly absorbed and begins to act on the body. Duration of peak indices of the drug is 15-60 minutes. Level of bioavailability for oral administration is 100%. Inside the plasma, the peak values of the component are noted after 0.5-1.5 hours after taking the tablet inside. Diazepam has a high degree of synthesis with protein - 96-99%.

The half-distribution time is 2-13 minutes. Diazepam is a fat-soluble component, it is quickly distributed within the body, passes through the placental barrier and BBB, and is excreted with the mother's milk. After absorption, the drug is redistributed within the fat, as well as muscle tissue. In the case of a permanent daily intake of drugs, it quickly accumulates inside the body (mainly inside fatty tissues), reaching an index that significantly exceeds the size of the actual dosage. Cumulation of matter is carried out mainly within individual organs, among which the heart.

The drug passes oxidative metabolic processes - hydroxylation with demethylation, as well as glucuronization inside the liver (as part of the enzyme system of the hemoprotein P450). Diazepam has several pharmacoactive decay products, the main one being desmethyldiazepam (it is also called nordiazepam or Nordazepam). Other active breakdown products include weak elements of oxazepam with temazepam. These degradation products undergo conjugation with glucuronide, and are excreted mainly along with urine.

Diazepam has a two-stage half-life, lasting 1-3 days, and in desmethyldiazepam it is 2-7 days. Metabolism is exposed to most of the drug, only a small amount of it is excreted unchanged.

The half-life of diazepam and desmethyldiazepam is significantly increased in patients in old age, which can lead to prolonged exposure to drugs, and additionally to cumulation in the case of repeated administration.

[17], [18], [19], [20]

Dosing and administration

The size of the dose and duration of Valium use can be prescribed only by a specialist, taking into account the type of pathology and severity of its clinical manifestations. The standard recommended doses are often:

• during treatment of phobias with neuroses, as well as angina pectoris, hypochondriacal or hysterical disorders, neurological pathologies of degenerative type and disturbance of BP parameters, it is required to take the medication 2-3 times a day in an amount of 5-10 mg;
• When eliminating polyarthritis, arthritis or arthrosis, as well as other joint diseases, 5 mg of medication should be taken 1-4 times per day (a more accurate number of procedures is determined by the doctor);
• with alcohol withdrawal syndrome it is required to take 5 mg of Valium 3-4 times a day;
• for the treatment of vertebral syndrome take a medicine in the amount of 10 mg 4 times a day (while you need to adhere to bed rest);
• to eliminate menopausal, menstrual or psychosomatic disorders, as well as gestosis tablets drink in the amount of 2-5 mg, 3 times a day.

Older or weakened people, as well as if the patient has atherosclerosis, drugs should be taken twice a day in an initial dose of 2 mg. Then it is gradually increased until the required drug effect is achieved.

In adults, therapy is usually done according to this scheme: taking 0.5 tablets 5 mg (that is, 2.5 mg of the drug) 1-2 times per knock or taking the evening of the first whole tablet (5 mg).

The sizes of children's doses are calculated taking into account the patient's age:

• for 1-3 years - a dose of 1 mg;
• for the age of 3-7 years - taking 2 mg;
• children over 7 years - a dose of 3-5 mg.

[27], [28], [29], [30], [31]

Use of the valium during pregnancy

Take Valium during pregnancy is prohibited.

Contraindications

The main contraindications:

• myasthenia gravis;
• obstructive pulmonary pathology of chronic type in severe form;
• glaucoma of the closed type;
• a state of coma or shock;
• respiratory insufficiency in acute form;
• acute poisoning with drugs that have an overwhelming effect on the function of the central nervous system;
• alcoholic poisoning in acute form, with the weakening of important for life functions of the body;
• hypersensitivity to diazepam or other additional elements of the drug;
• lactation period;
• infants less than 6 months of age.

Caution is required when appointing in such cases:

• people with epilepsy or having a history of epileptic seizures;
• with insufficiency of the liver or kidneys;
• available in the history of drug dependence;
• people with a tendency to abuse psychotropic substances;
• cerebrospinal pathologies of organic type;
• hyperkinesis;
• cerebral or spinal form of ataxia;
• hypoproteinemia;
• night apnea;
• aged people.

[21], [22]

Side effects of the valium

Taking medication can be accompanied by the development of many different side effects:

• increased fatigue, a feeling of sluggishness, disorientation, drowsiness;
• decreased attention;
• dizziness and slowing of psychomotor reactions;
• amnesia of retrograde type;
• motor coordination disorder.

In addition, there is information that Valium can cause tremors, muscle spasms, feelings of depression, irritability, euphoria and confusion, and in addition, the development of depression, tachycardia, dyspeptic manifestations, insomnia and thrombosis, as well as catalepsy and other abnormalities in the function of the NA and the psyche.

[23], [24], [25], [26]

Overdose

Among the manifestations of an overdose: a sensation of confusion, drowsiness, deafness, or severe weakness. In addition, areflexia or weakening of reflexes, paradoxical stimulation, weakening of reaction to pain, dysarthria, tremor, nystagmus and ataxia, as well as deep sleep are observed. Difficulty in the respiratory process, dyspnoea, bradycardia and apnea can develop, and in addition, collapse, a decrease in blood pressure, a coma and suppression of respiratory and cardiac function.

To eliminate the disorders, it is required to rinse the stomach, perform the forced diuresis procedure, and also take activated charcoal. There is also ventilation and support for blood pressure and respiratory function. Antidote is the substance flumazenil (application in the hospital). The effectiveness of hemodialysis is very small.

[32], [33]

Interactions with other drugs

The drug potentiates the suppressive effects on the central nervous system of substances such as antipsychotics (neuroleptics), ethyl alcohol, opioid analgesics, antidepressants, muscle relaxants and drugs used for general anesthesia.

Medications-inhibitors of oxidative microsomal processes (among them oral contraceptives, cimetidine with fluoxetine, as well as disulfiram, erythromycin with ketoconazole and propranolol, isoniazid with propoxyphene and metoprolol with valproic acid) prolong the half-life of Valium, and also potentiate its properties.

Inductors of microsomal hepatic enzymes weaken the effect of drugs.

Opiates potentiate a sense of euphoria, caused by Valium, because of which the psychological dependence on the medicine increases.

Antacids reduce the rate of absorption of drugs from the gastrointestinal tract, without affecting its degree.

Antihypertensive drugs are able to potentiate the severity of lowering blood pressure.

In the case of combination with clozapine, potentiation of respiratory function suppression is possible.

The combination of Valium and SG with a low polarity can increase their serum values, and also cause SG poisoning (due to competition for synthesis with plasma protein).

The drug weakens the effect of levodopa on individuals with Parkinson's disease.

The excretion time of Valium is prolonged when combined with omeprazole.

Restorative drugs, MAOI, as well as psychostimulants reduce the activity of the drug.

Premedication with Valium makes it possible to reduce the dosage of fentanyl, which is necessary for an initial general anesthesia, and also to shorten the time required to "turn off" consciousness with induction doses.

The drug is able to potentiate the toxic properties of zidovudine.

Potentation of valium excretion together with a decrease in its plasma level occurs when combined with rifampin.

Small dosages of theophylline can reduce or even distort the sedative effect of the drug.

[34], [35], [36]

Storage conditions

The medicine must be stored in a place that is closed from penetration of sunlight.

[37], [38], [39], [40]

Special instructions

Reviews

Valium is considered a very unsafe drug, and reviews about it are very ambiguous. Although it is quite effective for alcohol dependence, as well as for psychosomatic and post-traumatic disorders, it can not be abused, as it is capable of causing addiction, and also has a large number of negative effects. Therefore, you can take it only with the appointment of a doctor.

[41], [42], [43]

Shelf life

Valium can be used during 2-3 years from the moment of manufacturing of a medicine.

[44], [45], [46], [47], [48], [49], [50]