Zoloft is an effective antidepressant

Release form, composition and packaging

Film-coated tablets	1 tab.
zolpidem (as hemitartrate)	10 mg

15 pcs.
— cellular contour packages (1) — cardboard packs. 15 pcs. — contour cell packaging (2) — cardboard packs. pharmachologic effect

Zolpidem is an imidazopyridine hypnotic and is a selective agonist of the omega-1 benzodiazepine receptor subclass. It has a sedative effect, but when used in normal doses it does not have an anxiolytic, central muscle relaxant or anticonvulsant effect. Excites benzodiazepine receptors (omega) in the alpha subunit of GABA receptor complexes localized in the region of the IV plate of the sensory-motor zones of the cortex, reticular sections of the substantia nigra, visual hillocks of the ventral thalamic complex, pons, globus pallidus, etc. Interaction with omega receptors leads to to the opening of neuronal ionoform channels for chloride ions.

Shortens the time to fall asleep, reduces the number of night awakenings, increases the total duration of sleep and improves its quality. Extends stage II sleep and stages of deep sleep (III and IV). Does not cause drowsiness during the day.

Composition and form of the product

The active ingredient in the product is sertraline hydrochloride. The component has a powerful antidepressant effect, but does not have a sedative effect, and also does not have anticholinergic or stimulating properties.

Zoloft is produced in tablet form. One biconvex film-coated tablet contains 50 mg or 100 mg of active substance. Distinctive features of the tablets are their oval shape, white color, and the presence of “Pfizer” and “ZLT-50” engravings on different sides.

Other ingradienites are also used to produce the medicine. Their list is indicated in the instructions for use.

Pharmacokinetics

Zolpidem is rapidly absorbed from the gastrointestinal tract. The time to reach Cmax in blood plasma after oral administration is 0.5-3 hours. Bioavailability is 70%, binding to plasma proteins is 92%. There is a linear relationship between the dose of the drug and its plasma concentrations. Metabolized in the liver to form three inactive metabolites, which are excreted by the kidneys (56%) and through the intestines (37%). The average T1/2 is 2.4 hours. Vd is 0.5±0.02 l/kg. Does not induce liver enzymes. In elderly people, plasma clearance may decrease without a significant increase in T1/2 (average 3 hours), while Cmax increases by 50%. In patients with severe renal impairment, clearance increases slightly. In patients with impaired liver function, bioavailability increases, T1/2 increases to 10 hours. It is excreted in small quantities in breast milk.

INSOMNIA

Insomnia is characterized not only by a lack of sleep, but also by an inability to get enough sleep, and may also include difficulty falling asleep, not getting enough sleep, or waking up early and then being unable to get back to sleep.

Pharmacological properties of the drug Zolpidem

Zolpidem has a hypnotic and sedative effect, belongs to the group of imidazopyridines, and is used for short-term relief of insomnia. Zolpidem is a potent, highly active ω-subtype agonist, also called the benzodiazepine receptor subtype 1 (BZ1) γ-aminobutyric acid type A (GABA A) chlorionophore-related receptor. It is believed that the ω1 subtype of the GABA A receptor is localized in the central nervous system mainly in the cerebellum, sensory-motor zone of the cerebral cortex, substantia nigra, superior colliculus, olfactory bulb, ventral part of the thalamic complex, pons and globus pallidus. The receptor complex is located on the membranes of neurons and functions by opening chloride channels, allowing chloride ions to pass through the membrane into the neuron. The result of this is hyperpolarization, which suppresses the neuron's firing. Unlike benzodiazepines, which non-selectively bind to GABA A receptors, ω1-, ω2- and ω3-subtype, zolpidem has pronounced selectivity for the ω1-subtype of GABA A receptors. Such selectivity is likely responsible for the relatively weak anticonvulsant, muscle relaxant and anxiolytic effects zolpidem when used in therapeutic doses and overall preservation of the structure of sleep phases. Absorbed quickly and completely, but bioavailability due to primary passage through the liver is 70%. The maximum concentration in blood plasma is achieved 30–120 minutes after oral administration. Concomitant use with food reduces the rate and extent of absorption. The volume of distribution in healthy volunteers after intravenous administration at a dose of 8 mg was 0.54 l/kg. It passes into breast milk in small quantities: 3 hours after oral administration at a dose of 20 mg, the amount of zolpidem in milk is 0.004–0.019% of the dose taken. 92% of zolpidem is bound to plasma proteins. Biotransformed in the liver with the formation of several inactive metabolites. The half-life is 2.6 hours (1.4–4.5 hours), may increase in the elderly and in patients with impaired liver or kidney function. 48–67% of zolpidem taken is excreted in urine, and 29–42% in feces. It is excreted in the form of metabolites; traces of unchanged zolpidem are detected in urine and feces. Safety and effectiveness in children have not been established.

Dosage

Orally (immediately before bedtime) in a single dose of 10 mg.

In elderly
or debilitated patients with impaired liver function
treatment begins with a dose of 5 mg.
If necessary (insufficient clinical effect) and the drug is well tolerated, the dose can be increased to 10 mg. The maximum daily dose is 10 mg. The course of treatment should not exceed 4 weeks. For transient insomnia,
the recommended course of treatment is 2-5 days, for
situational
insomnia - 2-3 weeks.

Very short periods of treatment do not require gradual withdrawal of the drug. In case of long-term use of the drug, to reduce the possibility of developing rebound insomnia, zolpidem should be discontinued gradually (first reducing the daily dose and then discontinuing the drug).

Use of the drug Zolpidem

In order to minimize the possibility of developing anterograde amnesia and other undesirable effects, zolpidem is taken only if it is possible to obtain 7-8 hours of sleep after its use. To promote sleep onset more quickly, zolpidem should be taken on an empty stomach. Usually prescribed at a dose of 10 mg orally at bedtime. The maximum daily dose for adults is up to 20 mg. Weakened patients, patients with impaired liver or kidney function, and elderly people are prescribed a reduced initial dose - 5 mg at bedtime, the dose is adjusted taking into account individual tolerance.

Overdose

Symptoms:

impaired consciousness (from confusion and lethargy to coma), ataxia, decreased blood pressure, respiratory depression.

Treatment:

induction of vomiting within 1 hour after an overdose, activated charcoal, if more than 1 hour has passed since the overdose (if conscious, by mouth, if unconscious, by tube), gastric lavage, symptomatic therapy. Flumazenil (a benzodiazepine receptor antagonist) is recommended as an antidote, but it should be remembered that antagonism with benzodiazepine receptors can lead to the development of seizures, especially in patients with epilepsy. Dialysis is ineffective.

Rules of application

The effectiveness of the drug is not affected by food intake. The medicine is taken once a day, the initial dose for treatment is:

• Depressive conditions and obsessive-compulsive disorders are 50 mg.
• Panic disorders, post-traumatic stress disorders and social phobias – 25 mg.

During therapy, the dosage of the medicine can be increased according to the doctor’s recommendation. In this way, the optimal treatment regimen is selected.

A noticeable positive effect from taking the drug is observed after about a week. But in most cases, a course of treatment lasting 2-4 weeks is required to obtain a lasting result. For major depressive episodes, therapy can be continued for six months or more to prevent relapses.

The drug can also be prescribed for maintenance therapy. In this case, the minimum dose is prescribed, which provides the desired effect. This requires periodic dosage adjustments depending on the therapeutic effect.

Drug interactions

Not recommended combinations:

ethanol enhances the sedative effect of zolpidem.

Combinations that require caution when used:

- drugs that depress the central nervous system (neuroleptics, barbiturates, other hypnotics, anxiolytics/sedatives, antidepressants with sedative action, narcotic analgesics, antitussives of central action), antiepileptics, drugs for general anesthesia, antihistamines with sedative effect, hypotensive drugs of central action; baclofen; thalidomide; pizotifen - increased inhibitory effect on the central nervous system and risk of respiratory depression;

- buprenorphine - risk of respiratory depression;

- ketoconazole (a powerful inhibitor of CYP3A4) at a dose of 200 mg 2 times / day increases T1/2, AUC and reduces the clearance of zolpidem (possibly increasing the sedative effect of zolpidem);

- itraconazole (CYP3A4 inhibitor) - a slight, clinically insignificant change in the pharmacokinetics and pharmacodynamics of zolpidem.

Interactions to consider:

- rifampicin (CYP3A4 inducer) - accelerates metabolism, reduces the concentration and, as a consequence, the effectiveness of zolpidem.

Zolpidem drug overdose, symptoms and treatment

Manifested by severe ataxia, dysfunction of the cardiovascular system (bradycardia), visual impairment (diplopia), severe dizziness, drowsiness, nausea, respiratory failure, uncontrollable vomiting, inappropriate behavior, convulsions, loss of consciousness. Symptomatic and supportive treatment is carried out: monitoring of respiratory function and cardiovascular systems, neurological status, induction of vomiting or gastric lavage, administration of activated charcoal, refusal to use sedatives, even in a state of excitement. Flumazenil can be used to reverse the sedative effect of zolpidem and its depressant effect on breathing. Zolpidem is not eliminated by hemodialysis.

List of pharmacies where you can buy Zolpidem:

• Moscow
• Saint Petersburg

Side effects

Zolpidem is generally well tolerated.

Frequency of occurrence of adverse reactions: very often - more than 10%, often - more than 1% and less than 10%, infrequently - more than 0.1% and less than 1%), rarely - more than 0.01% and less than 0.1%, very rarely - less than 0.01% ( including isolated cases), the frequency is unknown (it is not possible to establish the frequency of occurrence based on the available data).

From the nervous system:

often - drowsiness, feeling of intoxication, headache, dizziness, increased insomnia, anterograde amnesia (the effects of amnesia may be associated with behavioral reactions), the risk of which increases in proportion to the dose, hallucinations, agitation, nightmares; infrequently - confusion, irritability; frequency unknown - disturbance of consciousness, dysphoria, aggressiveness, visual and auditory hallucinations, increased excitability, behavioral reactions, somnambulism, drug dependence (can develop even when using therapeutic doses), when discontinuing the drug - withdrawal syndrome or rebound insomnia, decreased libido, gait disturbance , ataxia, falls (mainly in elderly patients), addiction to the drug (decreased sedative and hypnotic effects when used for several weeks). Most mental side effects are paradoxical reactions.

From the digestive system:

often - diarrhea, nausea, vomiting, abdominal pain; frequency unknown - increased activity of liver enzymes.

From the musculoskeletal system:

frequency unknown - muscle weakness.

From the skin:

frequency unknown - rash, itching, urticaria, hyperhidrosis.

Allergic reactions:

frequency unknown - angioedema.

Other:

often - feeling tired; infrequently - diplopia.

Contraindications

- acute and/or severe respiratory failure;

- severe acute or chronic liver failure;

— night apnea (including suspected);

- due to the presence of lactose in the composition: hereditary lactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome;

- pregnancy;

- lactation period;

- children's age (up to 18 years);

- hypersensitivity to zolpidem or other components of the drug.

Carefully :

myasthenia gravis, respiratory failure, mild to moderate liver failure, depression, alcoholism, drug addiction and other types of addiction.

special instructions

The persistence of insomnia for 7-14 days of treatment indicates the presence of primary mental disorders and/or disorders of the nervous system. Therefore, to identify these disorders, it is necessary to regularly reassess the patient's condition.

To reduce the risk of developing anterograde amnesia, patients should have conditions for uninterrupted 7-8 hours of sleep.

When using zolpidem, mental and behavioral (including paradoxical) reactions may occur (the risk of development is higher in elderly patients). If such reactions occur, zolpidem should be discontinued. After a course of taking it for several weeks, there may be some reduction in the sedative and hypnotic effects of zolpidem.

Use of zolpidem (especially long-term use) may lead to the formation of physical and/or mental dependence, the risk of which increases with increasing dose and duration of treatment, as well as in patients with a history of abuse of alcohol or other drugs and non-drug substances. Such patients should be closely monitored during treatment. However, dependence (extremely rarely) can also occur when using therapeutic doses and/or in patients without individual risk factors.

The combination of zolpidem with benzodiazepines increases the risk of developing drug dependence.

In elderly patients or with impaired liver function, a significant increase in T1/2 of zolpidem is possible, which can lead to accumulation of the drug when it is repeated. Based on the pharmacokinetics of zolpidem, drug accumulation is not expected in chronic renal failure.

When using zolpidem in elderly people, caution must be exercised due to the risk of developing pronounced sedative and/or muscle relaxant effects.

Impact on the ability to drive vehicles and operate machinery

During the treatment period, you should refrain from engaging in potentially hazardous activities that require increased concentration (driving a car, working with machinery) and the speed of psychomotor reactions.

Modern life in a metropolis is associated with chronic persistent stress, unfavorable ecology, disruption of diet, sleep and rest. These unfavorable factors are the cause of the development of many pathological conditions. Often their first and only manifestations are symptoms of a sleep disorder.

The most common complaints encountered in various sleep disorders:

• difficulty falling asleep,
• intermittency of sleep,
• superficial nature of sleep,
• early awakening with inability to fall back to sleep,
• early awakening from sleep,
• poor quality of sleep,
• lack of feeling of rest after sleep.

When many patients visit doctors of various specialties, complaints about sleep disturbances are quite common, although they are not a reason to visit a doctor. Complaints about sleep disturbances come to the fore much less often. Many doctors in their practice, without establishing the true cause of sleep disturbance, easily prescribe sleeping pills. However, it is known that sleep disturbance can be one of the manifestations of various diseases, physiological and pathological conditions, as well as a consequence of drug exposure. This must be taken into account when choosing a method of corrective therapy. At the same time, one should also take into account the high frequency of self-medication and over-the-counter dispensing of some sleeping pills, which not only can aggravate the clinical situation, but also contribute to the risk of developing serious adverse reactions.

The indication for pharmacotherapy of sleep disorders is the persistence and duration of these disorders, which significantly worsen the quality of life. Drug therapy is carried out when recommendations for adherence to the regimen and general hygiene measures are ineffective.

Recently, patients with sleep disorders are often prescribed Zolpidem by doctors of various specialties. However, as practice shows, data concerning its safety are not always taken into account.

The main problem in the drug treatment of insomnia with Zolpidem at present is not so much its lack of effectiveness as the insufficient safety of treatment with this drug if it is used in violation of the instructions.

Compliance with the requirements for the prescription and use of Zolpidem should help not only reduce the risk associated with the drug, but also prevent its discredit.

FC MBLS considered it appropriate to inform the medical community, as well as consumers, about measures to prevent possible negative consequences associated with the use of this drug, which are presented below in the form of recommendations.

In Russia, the drug Zolpidem is registered under the trade names Hypnogen, Zolpidem tartrate, Zonadin, Nitrest, Sanval, Snovitel, Ivadal, Zolsana.

It is advisable for physicians prescribing Zolpidem and patients to read these recommendations before using Zolpidem.

This information does not replace the patient's consultation with a physician on issues related to treatment with this drug.

Contents of recommendations

I. What is Zolpidem?

II.
What is important to know before you start using Zolpidem?
III.
Who should not take Zolpidem and when?
IV.
How should I take Zolpidem?
V.
What adverse side effects may occur while taking Zolpidem?
VI.
Minimizing the risks associated with taking Zolpidem
VII.
How to store Zolpidem.
VIII.
Composition of Zolpidem.
I.
What is Zolpidem?
Zolpidem is a short-acting hypnotic drug. Improves the ability to fall asleep, increases the duration and improves the quality of sleep. It has sedative, slightly expressed anxiolytic, central muscle relaxant and anticonvulsant effects.

II.
What is important to know before you start using Zolpidem?
When taking Zolpidem, symptoms of somnambulism may appear - the patient may get out of bed in a sleepy state and perform various actions that he does not remember in the morning. The combined use of Zolpidem with hypnotics, drugs that depress the function of the central nervous system, as well as in doses exceeding the maximum recommended, increases the risk of developing sleepwalking.

Activities that a patient can perform in a sleepy state: drive a car (drowsy driving), cook and eat food, talk on the phone, have sex, walk, etc.

During the treatment period, care must be taken when driving vehicles and other potentially dangerous activities that require increased concentration and speed of psychomotor reactions, as well as when drinking alcoholic beverages.

When prescribing the drug to patients with concomitant depressive conditions, it is necessary to take into account the possibility of increased suicidal tendencies.

Zolpidem is not intended for use in children under 18 years of age.

Exceeding the dosage of the drug is contraindicated, because this may be associated with a risk of developing serious negative consequences.

Zolpidem is addictive when taken over a long period of time.

Particular attention should be paid when prescribing Zolpidem to elderly patients, since the occurrence of adverse reactions in them is observed more often than in patients of other age groups.

You should not take Zolpidem for more than 4 weeks. If symptoms of sleep disturbance continue, the patient should consult a doctor, as these may be symptoms of various diseases.

III.
Who should not take Zolpidem and when?

• Patients with a history of allergic reactions to Zolpidem and its components.
• Patients with depressive disorders, mental illness, suicide attempts.
• Patients who use alcohol and drugs.
• For kidney and liver diseases.
• For diseases of the respiratory system.
• During pregnancy or when planning it.
• When breastfeeding.

The attending physician must be informed about all medications, vitamins and herbal preparations that the patient uses, as they can interact with each other, leading to undesirable consequences.

Zolpidem should not be taken with the following medications:

• Benzodiazepines, antidepressants, opiates, barbiturates, narcotic analgesics, antihistamines and sedatives, some antitussives, antipsychotics, clonidine.

Take Zolpidem with caution with the following medications:

• With some antibiotics (Erythromycin, Rifampicin, Clarithromycin).
• With antifungal drugs such as ketoconazole.

IV.
How to take Zolpidem?

• Zolpidem should be taken immediately before going to bed.
• You should not take Zolpidem if you cannot spend more than 7-8 hours in bed
• In order for Zolpidem to work faster, you should not take it during or immediately after a meal.

The patient should consult a doctor if:

• Insomnia symptoms have worsened or remained unchanged. Perhaps the occurrence of insomnia is associated with other factors.
• When using the drug in a larger dose than prescribed by the attending physician.
• Adverse side reactions appeared.

Zolpidem is not recommended for use without a doctor's prescription.

It is not recommended to share Zolpidem with others, even if they have similar symptoms of sleep disturbance. This may harm their health.

V. What adverse reactions (ADRs) may occur while taking Zolpidem?

In table No. 1 provides a list of possible ADRs for the drug Zolpidem.

Table No. 1 Possible adverse reactions that occur when taking Zolpidem.

Frequent CPD (>1/100)

Infrequent CPD (from 1/100 to 1/1000 )	Rare NPR (less than 1/1000)
Drowsiness Dizziness Diarrhea Asthenia Nausea, vomiting Ataxia Feeling drunk Euphoria Lethargy Sinusitis Diplopia Visual impairment Urinary tract infections Itchy skin	Orthostatic hypotension Syncope Chest pain Cerebrovascular disorders Agitation Emotional lability Decreased cognitive abilities Concentration problems Hallucinations Migraine Stupor Tremor Anorexia Gastroenteritis Liver dysfunction Menstruation disorders Bronchitis Cough Pain in the eyes	Impotence Glaucoma Anaphylactic shock Arrhythmias Angina pectoris Extrasystole Malignant hypertension Thinking disorders Neuroses Panic attacks Personality disorders Somnambulism Suicide attempts Tetany Gastritis Anemia Lymphadenopathy Thrombosis Hypercholesterolemia Corneal ulceration Acute renal failure Pyelonefitis
After completing a course of taking sleeping pills The following symptoms may persist for two days:
Inability to sleep Nausea, Tides, Dizziness, Uncontrollable crying Stomach cramps, Panic attacks, Nervousness, Abdominal pain. Vomit
Attention! When taking Zolpidem: Possible development of addiction to the drug Possible unusual and potentially dangerous sleep behavior. It is not recommended to use psychotropic drugs or alcohol, as serious adverse consequences may occur. You should not take Zolpidem for more than 4 weeks. The patient should immediately seek medical help if the above symptoms or any other symptoms that bother him appear while taking Zolpidem.

VI.
Minimizing the risks associated with taking Zolpidem
Before prescribing Zolpidem, your doctor should:

• Warn the patient about all possible adverse reactions,
• Find out from the patient whether he is taking alcohol, drugs, and other medications. (see section IV
  ),
• Monitor the dynamics of changes in symptoms of sleep disorders,
• Discontinue the drug if it is ineffective and if adverse reactions occur,
• Systematically monitor the correctness of taking the drug and its dosage,
• Notify the FC MBLS about the NPR by filling out the NPR notification card (the NPR notification form is available on the website https://www.regmed.ru/ in the “Pharmacovigilance” section).

VII.
How to store Zolpidem?

• Store at room temperature (20-25C)
• Keep out of the reach of children.

VIII.
What does Zolpidem contain?
Active substance

: Zolpidem

Excipients

: hydroxypropyl methylcellulose, lactose, magnesium stearate, microcrystalline cellulose, polyethylene glycol, sodium glycolate, titanium dioxide, red steel color, polysorbate 80

Sources:

1. https://www.ambiencr.com/hcp/Dosing_Safety/Adverse-Reactions.aspx
2. https://www.drugs.com/pro/zolpidem.html
3. https://www.accessdata.fda.gov/scripts/cder/drugsatfda/index.cfm?fuseaction=Search.Label_ApprovalHistory
4. https://medact.ru/article/27/56/
5. https://www.sanofi-aventis.com.au/products/aus_cmi_stilnox.pdf

_____________________________________________________________________________

In accordance with the requirements of the Federal Law “On Medicines” dated June 22, 1998, all subjects of medicine circulation are required to report detected cases of adverse reactions to medicines in the prescribed form.
(see website www. regmed.ru section pharmacovigilance)
The Federal Center for Monitoring the Safety of Medicines (FCMBLS) calls on healthcare professionals to pay special attention to identifying adverse side reactions associated with taking Zolpidem and asks to report them in the prescribed form to the address:

123182, Moscow, st. Shchukinskaya, 6

Federal Center for Monitoring the Safety of Medicines (FCMBLS)

Tel. (495)2346104, ext.3093, 3128, 3091

Fax (495)1903461

Email

Source: Journal of drug safety and pharmacovigilance, 2008, No. 2, p. 23

For liver dysfunction

Contraindicated in acute or chronic liver failure.

With caution: mild to moderate liver failure.

In case of liver dysfunction

treatment begins with a dose of 5 mg.
If necessary (insufficient clinical effect) and the drug is well tolerated, the dose can be increased to 10 mg. The maximum daily dose is 10 mg. The course of treatment should not exceed 4 weeks. For transient insomnia,
the recommended course of treatment is 2-5 days, for
situational
insomnia - 2-3 weeks.

Use in old age

In elderly
patients,
treatment begins with a dose of 5 mg.
If necessary (insufficient clinical effect) and the drug is well tolerated, the dose can be increased to 10 mg. The maximum daily dose is 10 mg. The course of treatment should not exceed 4 weeks. For transient insomnia,
the recommended course of treatment is 2-5 days, for
situational
insomnia - 2-3 weeks.

Elderly patients may experience mental and behavioral (including paradoxical) reactions. If such reactions occur, zolpidem should be discontinued.

In elderly patients or with impaired liver function, a significant increase in T1/2 of zolpidem is possible, which can lead to accumulation of the drug when it is repeated.

When using zolpidem in elderly people, caution must be exercised due to the risk of developing pronounced sedative and/or muscle relaxant effects.

What does the drug treat?

Zoloft, the instructions for use confirm this, is indicated for the treatment and prevention of major depressive episodes. Such conditions are characterized by mental disorders with characteristic symptoms: loss of strength, increased fatigue, loss of interest in life, and a general deterioration in well-being.

In addition, the drug helps relieve:

• Obsessive-compulsive disorder, characterized by obsessive thoughts and actions.
• Panic attacks, which may be associated with various phobias.
• Post-traumatic stress disorders, which are caused by mental disorders against the background of a certain traumatic situation, which can be repeated or have an isolated character.
• The body's reactions to social phobias.