Zolpidem

Psycholeptic drug, produced by the Slovenian pharmaceutical company Lek, working purposefully as a hypnotic - Sanvall - has the international name Zolpidemum.

It would seem that such a small fact as a bad dream can bring to life and health of a person a lot of unpleasant sensations and pathological changes. If insomnia appears from case to case, then it is much easier to transfer and a healthy organism is able to quickly restore its strength. But if the problems with sleep go to the chronic plane, then the growing fatigue begins to manifest itself with increasingly severe negative symptoms. In such a situation, Sanvale can come to help a person - a highly effective medicine with sedative and hypnotic characteristics. It should only be remembered that the appointment should be prescribed by the attending or district doctor. Only a specialist is able to correctly assess the pattern of pathological changes and to prescribe an adequate therapeutic dosage capable of quickly and effectively solving the problem.

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

Indications Zolpidem

Due to their pharmacological characteristics, indications for the use of Sanvall are reduced to such pathological changes that are associated with disturbances in the process of falling asleep. This drug is also intended as a medicine that effectively relieves the patient from the problem of early awakening, as well as repeated spills throughout the night.

Release form

The main active substance of the drug is zolpidem tartrate, which, in order to maintain its high pharmacological efficacy, is combined with some other excipients.

Together with zolpidem, 55 mg of lactose monohydrate, 42.4 mg of microcrystalline cellulose, 4.8 mg of sodium carboxymethyl starch, 1.8 mg of povidone, 0.4 mg of colloidal silicon dioxide and 0.6 mg of magnesium stearate are present in tableted form.

The protective shell is represented by such chemical compounds as macrogol, giprolose, hypromellose, titanium dioxide, carnauba wax and special dyes.

The form of release of a medicinal product is one - the tablets covered with a dense protective cover. The tablet has a slightly convex, two-sided shape, on one side of the plane of which, the dividing risk is discernible.

Depending on the concentration of zolpidem tartrate in the medicamentous unit, the final form of Sanvall is divided into two different medicinal representations.

1. The tablet of a light pinkish hue contains active substance concentration of 5 mg. In a cardboard packaging box, two blisters are provided with ten tablets each.
2. A tablet of almost white color contains active substance concentration of 10 mg. On the pharmacological market, two graduating options are proposed:

• In a cardboard packaging box, two blisters are provided with ten tablets each.
• In a cardboard box there is one blister with ten tablets.

Pharmacodynamics

The drug in question is a pharmacological group of imidazopyridines. Pharmacodynamics Sanvall shows sedative properties, with persistent hypnotic characteristics. However, against the background of the drug, there is no significant anxiolytic effect, that is, Sanvale is not a serious antidepressant. Not strongly expressed anticonvulsant characteristics. Sanval has no significant effect on the decrease in the tone of the skeletal muscles with a decrease in motor activity until complete immobilization (central muscle relaxant syndrome).

Zolpidem irritates the benzodiazepine ω - receptors in the alpha structure of the GABA - complex of nerve endings that are located in the moto - sensory and other areas of the human cerebral cortex.

The tandem of the ω-receptors and the active active substance of the drug SANVAL provokes neural structural channels intended for the movement of ionoforms to open. In this case - for the passage of chloride ions.

Thanks to this effect, the process of falling asleep is accelerated, the number of situations when a person wakes up at night is reduced. Against this background, and the morning awakening becomes more pleasant, as the time of sleep increases, and the body manages to regain its strength.

Sanvall makes it possible to extend the second phase of sleep and increase the time and quality of deep sleep (phases three and four). Sleeping effect occurs in a short time after taking the drug and does not bring a sensation of drowsiness throughout the next day.

Pharmacokinetics

Not the least in the pharmacological characteristics of any drug is its ability to rapidly enter pathologically altered tissues, as well as the ability of the patient's body to utilize and excrete the constituents of the drug and its metabolites.

Pharmacokinetics Sanvall shows high parameters for its adsorption. This process is actively flowing through the mucosa of the gastrointestinal tract. Depending on the individual characteristics of the patient's body, the time interval through which zolpidem reaches its maximum concentration in blood plasma can reach from half an hour to three hours. The ratio of the administered dosage of the drug in question and the amount of zolpidem accumulating in the blood is linear.

The bioavailability of the active active substance Sanvall is about 70%. A sufficiently high index and binding capabilities of zolpidem with protein structures of blood plasma. This figure is close to 92%.

The active substance is actively transformed into the liver into three metabolites, which are not particularly active. The process of inducing enzymes, produced by the liver, is not observed.

Metabolized zolpidem derivatives, for the most part, about 56%, are excreted through the kidneys and urinary tracts together with urine, a smaller part of the metabolites is utilized together with the calves.

The half-life of the drug is on average three hours. In elderly patients, without increasing the duration of T _1/2, the parameter of the maximum concentration in the blood can increase by one and a half times, while the creatinine clearance significantly decreases.

In patients who have a history of significant disorders in the functioning of the kidney system, such a criterion as clearance increases its value insignificantly.

In patients with severe or moderate level of liver dysfunction, the bioavailability of Sangwal increases, while the half-life of the drug (T _1/2 ) increases its index and can last up to ten hours.

Dosing and administration

The medicine Sanval is taken orally (inside through the mouth). To get the expected effectiveness, the medicine should be drunk immediately before going to bed, a little after the meal. Zolpidem is washed down with water.

It should immediately be stipulated that after taking the medication, the patient is guaranteed a normal sleep within the next seven to eight hours after Sanaval administration. If a person does not plan so long to rest - Sanaval is better not to drink.

Before starting treatment, you need to make an appointment with a doctor: it is he who is able to correctly describe the treatment, the way of application and the dosage of Sanaval, which are necessary to obtain therapeutic effectiveness of treatment.

For adult patients, the recommended daily amount of the drug administered should not exceed 10 mg taken before going to bed. In rare cases, the maximum dosage may be 20 mg.

If the patient refers to patients who are already 65 years of age, the recommended dosage is halved and is 5 mg taken according to the schedule described above.

The same dose (5 mg) is prescribed for persons who have a history of liver failure or the patient's body is severely weakened. Such quantity is the starting one and its number can be gradually increased, but this procedure should be under the constant control of the attending doctor. If the patient's body has a good tolerability of zolpidem, but at the same time the desired clinical effectiveness is not obtained, the dosage of Sanvala can be gradually increased to 10 mg.

The duration of therapeutic treatment, as a rule, is no more than a month (or four weeks). If insomnia is not chronic, and it worries from case to case, it is recommended to take the drug in question for two to five days. If insomnia is situational, then the course of treatment can be stretched for two to three weeks.

The shortness of the therapeutic course does not require gradualness in the abolition of Sanvala. If the medicine was taken for a long time, in order to avoid a "ricochet" situation (the return of insomnia), zolpidem should be canceled gradually, reducing its dosage.

[7], [8]

Use Zolpidem during pregnancy

Due to their pharmacological characteristics of the impact on the human body, the use of Sangwal during pregnancy is contraindicated. Especially such categorical concerns the first trimester of embryo-bearing, since in this time there is a laying of all the organs and systems of the future person.

During the second and third period of pregnancy, the ban on the introduction of zolpidem is not so categorical, but its appointment requires significant medical indications. Sanvall is entered into the treatment protocol only when the real need for medical therapy for the health of the expectant mother far outweighs the possible negative consequences that may affect and affect the natural process of fetal formation.

Previously, before the drug was delivered to the pharmacological market, test studies were conducted on animals. The results of these analyzes showed the absence of any embryotoxic (unfavorable effect, not related to an organogenesis disorder in the first three months of pregnancy) or teratogenic abnormalities (occurrence of developmental defects under the influence of environmental factors).

It is also necessary to inform the representatives of the weaker sex of the reproductive age who are taking Sanvall that in the case of planning or the onset of conception, it is necessary to inform the treating doctor. Against the background of therapeutic therapy zolpidem, a woman should use reliable methods of contraception (prevent pregnancy).

If the clinical picture of the disease forced a specialist to appoint a woman Sanaval in the period immediately before childbirth or during delivery (even in minor dosages), a newborn baby can expect the appearance of hypothermia symptoms. Reducing the temperature of the child's body gradually can lead to problems with the respiratory system, until it stops. This situation can develop in hypertension (high blood pressure) or, conversely, in axial hypotension (low blood pressure), as well as problems with suckling activity of the baby.

There are also cases when, against the background of prolonged use of a pregnant woman on the last terms of zolpidem bearing, a newborn was diagnosed with a developed physical and psychological dependence on the drug, which subsequently, in the perinatal period, led to an increase in the likelihood of withdrawal syndrome.

Soporific and sedative drug freely penetrates into the mother's milk during the onset of the young mother lactation. Therefore, if a woman feeds her newborn with her milk, but there is a need to take a medication, breastfeeding of the baby should be discontinued. Transferring it to artificial food.

Contraindications

In the light of the above and on the basis of the results of the conducted studies, contraindications to the use of Sanvall were revealed.

1. Individual intolerance to the body of a patient with zolpidem, lactose or one of the additional substances that make up the medicinal product.
2. Severe form of respiratory failure.
3. If a history of a patient is diagnosed with a severe degree of hepatic dysfunction. This applies to both acute and chronic stage of the disease.
4. Lack of lactose in the patient's body.
5. Syndrome of sudden respiratory arrest (apnea), which can occur during sleep.
6. The first trimester of pregnancy.
7. Breastfeeding time of a newborn.
8. Do not prescribe medication until the patient is under 18 years of age, as the validity of the excess of therapeutic effectiveness over the relative safety of the drug is not proven.
9. Syndrome of glucose - galactose malabsorption.

It should be noted that with special care it is necessary to prescribe and take medicine if the patient suffers from drug addiction, alcoholism and other pathological dependencies.

Also, under the constant supervision of physicians, there must be a patient with a history of:

• Insufficiency of liver function with mild and moderate severity.
• Diseases of a mental nature.
• Second, third trimester of pregnancy.
• Respiratory dysfunction with mild and moderate severity of pathology.
• Myasthenia gravis is a pathological change in the human body of an autoimmune nature, as a result of which antibodies destroy and / or damage receptors to acetylcholine in the striated muscle. This restriction applies to the severe stage of the disease.

Side effects Zolpidem

According to the World Health Organization, the pathological manifestations of the use of pharmacological drugs are divided according to the degree of their frequency: multiple - more than one case of a hundred; not very frequent symptoms - more than one case of a thousand; rare - more than one case out of ten thousand and single cases - less than one case out of ten thousand. Moreover, it is proved that the side symptomatology affects more and more the representatives of the weaker sex than men, and the frequency of their occurrence directly depends on the quantitative component of the drug administered.

Side effects of Sangwal are manifested by this symptomatology:

• Multiple cases of pathological discomfort:
  • Drowsiness.
  • There is a partial loss of memory.
  • Diarrhea.
  • Both visual and auditory hallucinations.
  • Feeling tired.
  • Pain affecting the head region.
  • Increased sleep problems, the appearance of nightmares in dreams.
  • Dizziness of varying intensity.
  • Feeling of intoxication.
  • Motion coordination disorder.
  • High excitability.
  • Emotional instability.
• Not very frequent symptoms:
  • Paresthesia - a violation of the sensitivity of the skin.
  • Tremor of the lower and upper extremities.
  • Nausea, sometimes passing into vomiting.
  • Gastroenteritis.
  • Irritability.
  • Difficulty in swallowing solid foods or liquids.
  • Euphoric state.
  • Hiccough.
  • Abdominal pain.
  • Confusion of consciousness.
  • Flatulence.
  • Appearance of signs of impaired concentration.
• Rarely manifested symptoms:
  • Delirium.
  • Febrile state.
  • Increased sweat production by the corresponding glands.
  • Appearance in the muscles of weakness.
  • Puffiness.
  • Appearance of signs of somnambulism.
  • Aggressiveness and other manifestations of inadequate behavior. More often such symptomatology is shown in the elderly.
  • Frequent falls and injuries in persons of retirement age.
  • Increase in activity of liver enzymes.
  • Symptomatic of allergy.
• Single cases:
  • Unreasonable attacks of anger.
  • Sharp weight loss. Disorder of the cerebrovascular system.
  • Pale skin.
  • Bronchitis.
  • Drug dependence, addiction.
  • Appearance of cough and shortness of breath.
  • Increased contraction of the heart muscle.
  • Orthostatic hypotension.
  • The withdrawal syndrome. Edema of the Quincke.
  • Decreased sexual desire.
  • Hyperglycemia - a failure in carbohydrate metabolism, which is characterized by a high content of glucose in the blood.
  • Paradoxical reactions from the psyche.
  • Arthritis.
  • A sharp drop or, conversely, an increase in blood pressure.
  • Diplopia - the appearance of problems with eyesight.

In case of occurrence of any undesirable symptomatology, given above, it is necessary to inform the expert who has appointed the given medicine. He will assess the situation and give the necessary recommendations, up to the cancellation of Sanvala and the appointment of symptomatic therapy. An effective antidote, capable of stopping the problem that has arisen, does not exist today.

[5], [6]

Overdose

If, for any reason, an overdose of the drug occurred, it is necessary to give the patient first aid, washing his stomach and causing vomiting, then give a drink of any adsorbent, for example, activated charcoal.

If the patient's condition is bad, or after taking a large dosage for more than an hour, in parallel with his assistance activities, it is necessary, depending on the patient's condition, to call an ambulance (in the unconscious state of the patient) or inform the treating doctor if a mild degree of poisoning.

Symptoms of increased use of zolpidem:

• Inhibition of the reaction of the central nervous system, various degrees of manifestation of pathology.
• Confusion of consciousness.
• At serious displays - a coma.
• Ataxia is a disorder of coordination of movements.
• The inhibition of thinking.
• A sharp drop in blood pressure.
• Problems with breathing.
• A condition dangerous to the life of the patient.

When symptoms of an overdose appear, the doctor in a hospital conducts symptomatic treatment, as well as maintenance therapy. Especially it concerns the cardiovascular system and respiratory organs. It should be remembered that in such a situation it is not necessary to administer sedatives, even if the symptomatology requires it.

If the patient is experiencing all manifestations of severe intoxication of the body, the question may arise of introducing flumazenil, an active antagonist of benzodiazepine receptors. All reanimating measures are carried out in a hospital, because the oppression of this group of receptors can trigger various deviations of the neurological nature. For example, convulsions, which are especially dangerous for patients with epileptic seizures in the anamnesis.

To resuscitation measures do not connect hemodialysis, because it is not able to help in the withdrawal of excess zolpidem from the patient's body.

Interactions with other drugs

If, in the light of treatment of pathology, one drug therapy is used, it is necessary to clearly know the pharmacodynamic characteristics of the medicine used to prevent the appearance of various negative symptoms. But if the drug is injected into complex therapy, the specialist must necessarily know how each drug affects each other. In fact, ignorance of the results of the joint introduction of a different combination of complex chemical compounds can lead to irreversible pathological consequences.

Interactions with other drugs show that when combined with opioid analgesics, as well as other drugs that inhibit the receptors of the central nervous system, CNS is even more oppressed.

A similar situation is observed with the parallel introduction of zolpidem and neuroleptics, as well as drugs used to stop coughing attacks. 

Oppressively acts on the central nervous system and tandem entry with barbiturates (drugs with hypnotics).

To a lesser extent, but to inhibit the work of the central nervous system receptors and joint intake of sanguine and antihistamines, as well as drugs that belong to the pharmacological group of antidepressants and / or tranquilizers. This combination also increases the likelihood of drug dependence.

Copes the hypnotics of the drug in question, his tandem reception, together with flumazenil.

On the contrary, the pharmacodynamics of zolpidem is strengthened by such drugs as chlorpromazine and imipramine. This combination also increases the half-life of chlorpromazine, as well as the concentration of the active active substance imipramine in the patient's blood. Chlorpromazine is able to strengthen the state of drowsiness. At his joint reception with Sanvall, it is often possible to observe manifestations of anterograde amnesia.

Due to the fact that ritonavir and ketoconazole reduce Sanvan's clearance and the ability of zolpidem to metabolize, in the clinical picture one can observe an increase in the sedative potential of the drug in question.

It is able to reduce the amount of cumulative amount of zolpidem in the patient's blood rifampicin, which reduces the effectiveness of Sanvall.

Do not take alcoholic beverages, against the background of therapeutic therapy zolpidem. Alcohol inhibits the effect of the drug in question on the central nervous system receptors.

[9], [10], [11]

Storage conditions

After the acquisition of Sanaval, the patient should be sure to familiarize himself with those recommendations that are prescribed in the medication attached to the medicine for its storage.

If the patient meets all the requirements, you can be sure that the degree of effectiveness of the drug will remain at a high pharmacological level, which will last for the entire admissible period of admission.

The storage conditions of Sanvall do not differ much from the classic set of recommendations:

1. The drug should be stored throughout the period of permissible use in a cool place, where the temperature does not exceed + 25 degrees.
2. Keep Sanvall in a place inaccessible to small children.
3. The medicine should not be exposed to direct sunlight.
4. The humidity of the room where the drug is stored should be reduced.

[12], [13]

Shelf life

When buying any medication, first of all it is necessary to pay attention to its expiration date. On the packaging of the medicinal product, both the production date and the recommended end-of-course time are necessarily reflected. For Sanvall, the period of effective work is three years. If the end date of use on the package has already passed, then such a drug is not recommended for further use.

[14]