Trazodone use. Trazodone - instructions, use, indications, contraindications, action, side effects, analogues, composition, dosage

Formula: C19H22ClN5O, chemical name: 2-propyl]-1,2,4-triazolopyridin-3(2H)-one (as hydrochloride).
Pharmacological group: neurotropic drugs / antidepressants.
Pharmachologic effect: antidepressant.

Pharmacological properties

The mechanism of action of trazodone has not been fully elucidated. Trazodone has a strong affinity for some of the serotonin receptor subtypes. Trazodone selectively inhibits the reuptake of serotonin by synapses in the brain, potentiates the effects of 5-hydroxytryptophan (which is a precursor of serotonin), reduces the sensitivity of beta-adrenergic receptors and slightly affects the neuronal uptake of dopamine and norepinephrine and alpha-adrenergic receptors, MAO does not inhibit. Trazodone has almost no anticholinergic effect, but may suppress or reduce salivation (especially in elderly and middle-aged patients). The antidepressant effect of trazodone is combined with anxiolytic and sedative effects. Trazodone relieves manifestations of anxiety, both mental (fear, affective tension, insomnia) and somatic ( headache, palpitations, myalgia, increased sweating, frequent urination). Trazodone increases the duration and depth of sleep in depressed patients, restores the physiological structure of sleep. Trazodone reduces the craving for alcohol. With withdrawal syndrome in patients with benzodiazepine dependence, trazodone eliminates sleep disturbances and anxiety-depressive state (benzodiazepines can be completely replaced by trazodone during remission). Trazodone helps restore potency and libido. Trazodone can be used for concomitant cognitive impairment, prostatic hypertrophy, glaucoma, and in elderly patients, but the latter are more likely to have hypotensive and sedative effects. Trazodone is not addictive. Therapeutic effects in some patients (according to clinical trials) were observed by the end of the first week of therapy, in 75% of patients - at the end of the second week, in 25% - after 2-4 weeks.

Trazodone is well absorbed from the gastrointestinal tract. After 1 hour, the maximum concentration in the blood plasma is reached. Taking the drug during or immediately after a meal increases its absorption, but reduces the maximum concentration, lengthening the time to reach it up to 2 hours. Trazodone is 89-95% bound to plasma proteins. Trazodone passes through tissue barriers (including the blood-brain barrier). Trazodone is metabolized in the liver to form the active metabolite m-chlorophenylpiperazine. The half-life of trazodone has two phases: the duration of the early phase is 3–6 hours, the late phase is 5–9 hours; some patients may accumulate trazodone. The drug is excreted within 98 hours after its administration with urine (75%, including 70% in the form of inactive metabolites) and bile (20%). There is information about the effectiveness of trazodone in kleptomania, bulimia, panic attacks, phobias (including agoraphobia), acute withdrawal syndrome in alcoholism, pain in diabetic neuropathy and other types of chronic pain and for the prevention of migraine.

Indications

Depressive states of various origins (psychotic, endogenous, somatogenic, neurotic and others) with severe tension, anxiety; agoraphobia, neuralgia pain syndrome, benzodiazepine drug dependence, alcohol withdrawal state, impotence, decreased libido.

Route of administration of trazodone and dosage

Trazodone is taken by mouth. Adults: the initial dose is once at bedtime 50-100 mg, the dose is increased, if necessary, by 50 mg every 3-4 days until a therapeutic effect is achieved. The maximum daily dose on an outpatient basis is 450 mg, in hospitals it is 600 mg. For debilitated and elderly patients, the initial dose is up to 100 mg per day, which can be increased, if necessary, up to 300 mg per day. Children 6 - 18 years old: 1.5 - 2 mg / kg per day, the dose is increased, if necessary, to 6 mg / kg per day.

Libido disorders: 50 mg per day. Impotence: 200 mg per day with monotherapy, 50 mg per day as part of complex treatment. Benzodiazepine dependence: stepwise reducing the dose of benzodiazepines by 0.25 or 0.5 tablets, add 50 mg of trazodone together for 3 weeks, then continue to reduce the dose of benzodiazepines until complete withdrawal, then reduce the dose of trazodone by 50 mg per day every 3 weeks.
During therapy with trazodone, it is necessary to regularly carry out general analysis blood (for the timely detection of blood changes), ECG monitoring is desirable in patients with diseases of the circulatory system. Careful monitoring of patients with suicidal tendencies is necessary, especially in the first weeks of therapy. With the development of severe neutro - and leukopenia, priapism, treatment is immediately canceled; in other cases, the abolition of trazodone should be carried out gradually. Alcohol should be avoided during treatment with trazodone. Use trazodone with caution for drivers of vehicles during work and for people whose activities are associated with increased concentration of attention.

Contraindications for use

Hypersensitivity, ventricular arrhythmia, myocardial infarction (early recovery period), tachycardia, extrasystole, renal and/or liver failure, age up to 6 years.

Application restrictions

History of priapism, arterial hypertension (adjustment of doses of antihypertensive drugs may be required), age up to 18 years.
Etc

changes during pregnancy and lactation

Do not use trazodone in women during pregnancy. Animal studies have shown that trazodone at doses 30 to 50 times the MRDH increases fetal resorption and causes congenital malformations. During therapy with trazodone, breast-feeding should be discontinued. Trazodone with its metabolites is found in the milk of lactating rats. It is not known whether trazodone is excreted in breast milk in women.

Side effects of trazodone

Sense organs and nervous system: fatigue, headache, weakness, dizziness, drowsiness, insomnia, agitation, hypomania, psychosis, hallucinations, muscle twitches, tremors, aphasia, grand mal seizures, akathisia, ataxia, dyskinesia, confusion, paresthesia, syncope, diplopia, blurred vision;
blood and circulatory system: arterial hypotension (including orthostatic), arrhythmias (including ectopic ventricular rhythms, tachy - and bradycardia), atrial fibrillation, congestive heart failure, leukopenia or leukocytosis, neutropenia (usually minor), methemoglobinemia, hemolytic anemia;
digestive system: increased appetite, unpleasant taste and dry mouth, caries, hypersalivation, diseases of the periodontal tissues, nausea, oral candidiasis, vomiting, diarrhea, flatulence, constipation, increased levels of amylase and bilirubin in the blood plasma, cholestasis, jaundice;
urinary system: urinary retention, hematuria, increased urination, premature menstruation, increased libido, hirsutism, priapism, retrograde ejaculation, impotence;
allergic reactions: urticaria, skin rash;
others: chest pain, myalgia, alopecia, edema, psoriasis.

Interactions of trazodone with other substances

Trazodone, unlike typical antidepressants, does not reduce the depriming effects of reserpine, it weakens the peripheral effect of norepinephrine and the central effect of amphetamine. Trazodone enhances the effects of drugs that depress the central nervous system (including tricyclic antidepressants, barbiturates, clonidine, antihistamines, alcohol), as well as muscle relaxants and anticholinergics. With the joint use of trazodone with antihypertensive drugs, the possibility of developing orthostatic hypotension increases. Trazodone reduces the effects of psychostimulants. Trazodone increases plasma levels of phenytoin and digoxin. Do not use trazodone in conjunction with MAO inhibitors. Co-administration of ritonavir and trazodone may require a dose reduction of the latter. Patients who take trazodone and carbamazepine together should be under close medical supervision. When trazodone is combined with potent CYP3A4 inhibitors, the dose should be reduced.

Overdose

With an overdose of trazodone, nausea, drowsiness, vomiting, dizziness, impaired coordination, lowering blood pressure, priapism, epileptiform seizures, respiratory arrest, changes in the ECG, worsening of adverse reactions develop. Necessary: ​​gastric lavage, activated charcoal intake, forced diuresis, maintenance of vital functions, symptomatic treatment; there is no specific antidote.

Trade names of drugs with the active ingredient trazodone

Azona
Trittiko

Content

Depression is a common problem in modern people. Psychiatrists treat the disease by prescribing special medical preparations. Trazodone is one of the effective means from the class of antagonists/inhibitors recapture serotonin (AIOS). Before you start using the medicine, it is important to read the instructions, contraindications, side symptoms.

Composition and form of release

Trazodone is a drug that is widely used to treat depressive disorders. It differs from traditional antidepressants in that it does not belong to tetracyclic and tricyclic structures. The drug is produced in the form of capsules for oral administration, which contain 25, 50 or 150 mg of the active substance. You can also purchase Trazodone injectable solution.

The effectiveness of the drug is explained by the components that it contains. Substances included in 1 capsule are presented in the table below:

Chemical properties

According to the instructions for use, the drug is a derivative of thiazolopyridine. Trazodone is a mild antidepressant, anxiolytic, serotonin reuptake antagonist. The substance has the form of a crystalline white powder, readily soluble in water (hydrochloride), has no specific odor. The molecular weight of the drug components is about 371.9 g/mol.

Pharmacological properties

Scientists have not fully studied the action of Trazodone. According to the instructions for use, the drug provides a pronounced anxiolytic, antidepressant, tranquilizing effect. According to the pharmacological properties, this remedy differs from similar drugs. The components of Trazodone do not stimulate the central nervous system (central nervous system) and do not inhibit monoamine oxidase (do not affect the process of amino acid catabolism nervous system enzymes). The drug blocks alpha1-adrenergic receptors.

In addition, the drug has the ability to selectively inhibit the reuptake of serotonin by the brain. Trazodone acts as a 5-HT2A/2C receptor antagonist. The active substance eliminates insomnia, headache, myalgia, affective tension, helps fight arrhythmia, eliminates anxiety, and reduces sweating. Against the background of Trazodone treatment, patients' sleep improves, the physiological processes of the body are restored.

After taking the capsule inside, the maximum concentration of the substance in the blood is reached after 30-120 minutes. Parallel ingestion of food with the drug reduces the rate of absorption of the drug, due to which it is longer excreted from the patient's body. It is important to consider that the agent easily overcomes all histohematic barriers, is able to penetrate into saliva, bile, and breast milk. For this reason, Trazondol is not prescribed during pregnancy and lactation.

The drug has a high degree of binding to plasma proteins (up to 96%). The substance is metabolized by the liver, forming the active metabolite 1-m-chlorophenylpiperazine. Depending on whether the patient took the drug once or takes it systematically, the half-life is 3-9 hours. About 75% of the drug is excreted by the kidneys with urine, 20% with bile unchanged. Fully human body removes the antidepressant in 98 hours.

Indications for use

Before starting the use of the drug, it is important to study the instructions and familiarize yourself with the indications. An antidepressant helps fight many ailments, it can be prescribed in the following cases:

  • neurotic, endogenous, psychotic, somatogenic depression (in the presence of symptoms such as anxiety, loss of appetite, suicidal thoughts, poor sleep, decreased libido, lethargy, agitation, severe fatigue);
  • bulimia;
  • phobias;
  • anxiety;
  • kleptomania;
  • panic attacks;
  • alcohol withdrawal in an acute form;
  • benzodiazepine drug dependence;
  • migraine (for the purpose of prevention);
  • impotence;
  • diabetic neuropathy (to eliminate pain syndrome).

Method of application and dosage

Before starting a course of taking the tablets, it is recommended to consult a doctor. The course of therapy and the regimen for the use of the drug is determined individually in each case. Self-use of the drug can adversely affect the health of the patient. Instructions for use Trazodone provides for oral administration of tablets. It is recommended to take the medicine at bedtime. In some cases, the dose is divided into 3 doses.

Start using the drug with 100 mg per day. Gradually increase the dose every 3 days by 50 mg until the desired therapeutic effect. The maximum daily amount of the drug for outpatient treatment is 450 mg. In a hospital under the supervision of doctors, the patient can receive up to 0.6 g of Trazodone daily. Maintenance therapy for moderate or mild depression involves the use of 0.15 g of the drug every day.

According to the instructions, the drug can be used as an anxiolytic (anti-anxiety, sedative). In this case, the patient is prescribed 75 mg of the drug, which is divided into 3 doses. Patients over 65 years of age are allowed to use no more than 0.3 g of the drug daily. For children, the dosage is calculated by body weight: 1.5-2 mg per 1 kg. In extreme cases, babies are prescribed up to 6 mg of the drug per 1 kg of weight.

special instructions

In addition to following the instructions for use medicinal product, it is important to take into account the special instructions of specialists. To avoid the occurrence of neutro-, leukopenia (decrease in the level of neutrophilic granulocytes / leukocytes in plasma), it is worth regularly donating blood for analysis. In patients with a high risk of developing arrhythmias (disturbances in the process of normal heartbeat), during treatment with Trazodone, an ECG (electrocardiogram) of the heart is periodically done.

Particular attention should be paid to patients with suicidal tendencies, especially in the early stages of therapy for depressive syndrome. It is forbidden to drink alcohol together with the tablets. If the patient develops neutropenia, leukopenia or priapism (painful erection in men, not associated with sexual arousal) during the use of the drug, the therapy is stopped. In other cases, the abolition of Trazodone is carried out gradually.

According to the instructions, during the course of the drug, patients are prohibited from driving or performing work that requires increased concentration. The tablets often cause pupillary dilation, which can lead to angle-closure glaucoma in people with an anatomically narrow anterior chamber angle. It is important to consider that the antidepressant increases the risk of developing ventricular tachycardia, bleeding, sudden death of the patient, so treatment should be carried out under the supervision of doctors.

drug interaction

Before starting the use of the medicine, it is important not only to read the instructions, but also to inform the doctor about other means used. In combination with Trazodone, medications can provoke the following negative reactions:

  1. Pseudoephedrine causes panic, clouding of reason, anxiety.
  2. Amiodarone reduces the anticoagulant activity of Warfarin, causing cardiac arrhythmias.
  3. Digoxin causes cardiac glycoside intoxication.
  4. The concentration of Carbamazepine, Thioridazine in blood plasma increases.
  5. Lithium salts cause neurotoxic effects, tremor of the extremities.
  6. CYP3A4 inhibitors (Erythromycin, Itraconazole, Nefazodone) inhibit the metabolism of Trazodone, increase its concentration in the blood.
  7. Alcohol and any preparations containing ethanol increase CNS depression.
  8. Tryptophan causes hypomania, psychosis, aversion to food.
  9. The risk of developing side effects of Phenytoin, Fluoxetine increases.
  10. Trifluoperazine, Chlorpromazine increase arterial hypotension.

Side effects

The antidepressant is a prescription drug and should only be used when prescribed by a doctor. The fact is that Trazodone has a huge number of side effects. According to the instructions for use, tablets can provoke the following:

  • headaches;
  • drowsiness;
  • psychosis;
  • hallucinations;
  • increased fatigue;
  • confusion;
  • insomnia;
  • dizziness;
  • increased salivation;
  • dry mucous membranes;
  • heart arrhythmia;
  • bad breath;
  • decrease in blood pressure (blood pressure);
  • bradycardia;
  • congestive heart failure;
  • tachycardia;
  • convulsions;
  • dyskinesia;
  • tremor of the limbs;
  • paresthesia (disturbance of sensitivity);
  • damage to the oral cavity by the Candida fungus;
  • diplopia (double vision);
  • caries;
  • jaundice;
  • increased levels of amylase and bilirubin in the blood;
  • liver disease;
  • increased sexual activity;
  • leukocytosis;
  • impotence in men;
  • priapism;
  • leukopenia;
  • flatulence;
  • hemolytic anemia;
  • neutropenia;
  • diarrhea;
  • vomiting;
  • constipation;
  • violation of the menstrual cycle in women;
  • cholestasis;
  • hematuria (presence of blood in the urine);
  • hirsutism (the growth of coarse dark hair on the body in women according to the male pattern);
  • alopecia;
  • allergic skin rashes;
  • puffiness;
  • painful urination;
  • urticaria;
  • myalgia (muscle pain caused by cell hypertonicity);
  • psoriasis.

Overdose

Failure to follow the instructions for use of the drug can cause vomiting, dizziness, drowsiness, convulsions, seizures similar to epilepsy. In addition, exceeding the dose of Trazodone provokes changes in the electrocardiogram, an increase in the occurrence of side effects, up to respiratory arrest. If signs of an overdose are detected, the patient is given activated charcoal or another enterosorbent, forced diuresis is performed, and symptomatic therapy is prescribed. Trazodone has no specific antidote.

Contraindications

To reduce the risk of developing side symptoms, you should familiarize yourself with the contraindications before using the tablets. According to the instructions, Trazodone is not prescribed in the following cases:

  • children under 6 years of age;
  • with an allergy to the components of the drug;
  • with intoxication with alcohol or sleeping pills;
  • during pregnancy;
  • with lactation;
  • after myocardial infarction;
  • with arterial hypotension;
  • with AV-blockade of the heart;
  • with ventricular arrhythmias;
  • with severe diseases of the liver and kidneys.

Terms of sale and storage

Trazodone is an antidepressant drug that can only be purchased with a prescription from a doctor. So that the tablets do not lose their effectiveness, it is important to observe the storage conditions. According to the instructions for use, Trazodone must be consumed within 5 years from the date of manufacture. The manufacturer recommends keeping the medicine away from children and direct sunlight. The air temperature in the room where the tablets are stored should not exceed 25 degrees.

Trazodone's analogs

If the drug is not available in pharmacies, you can replace it with a similar drug in composition or action. The main analogues of Trazodone are presented below:

  1. Trittiko is a medicine with a similar composition, produced in Italy. Available in a dosage of 75 or 150 mg. It has a moderate antidepressant, anti-anxiety, sedative effect.
  2. Azona is a synthetic antidepressant based on trazodone, manufactured in Finland. Tablets are available in dosages of 25, 50 and 100 mg. The tool is used to treat depression and nervous disorders.

Price of Trazodone

The cost of an antidepressant depends on the manufacturer, outlet, and other factors. Trazodone is currently only available under other brand names. Below is a table with prices in Moscow:

Video

Are there pregnancy restrictions?

Prohibited at breastfeeding

Forbidden for children

Has restrictions for the elderly

Has limitations for liver problems

Has limitations for kidney problems

Antidepressants are prescribed for various mental disorders to relieve negative symptoms. Trazodone is especially popular among such drugs, which, according to the instructions for use, is most effective in depressive states that have arisen as a result of exposure to external or internal factors.

The active substance of the drug trazodone is a thiazolopyridine derivative. It has a special chemical structure, therefore it does not belong to any group of antidepressants (tri- or tetracyclic). Trazodone itself is a chemical found in many medications. In Russia, the full analogue of the foreign drug Trazodone - Trittiko pilyule_nervi-521 (Italy) and Azona (Finland) is especially common.

Drugs with trazodone belong to a large group of drugs - antidepressants. Such funds are intended for the treatment of mental disorders - depressions of various origins.

The international non-proprietary name is determined by the content of the active ingredient in the drug, which has one or another effect on the body. In this case, the INN is trazodone (Trazodone). The scope of the medicinal substance is psychiatry. Trazodone-based drugs are used to treat depressive disorders in adults and the elderly.

Description of the drug

Release forms, cost

Trazodone hydrochloride is a white crystalline powder. It is odorless and dissolves well in water. On its basis, tablets, capsules or injections are produced. Such pharmacological forms have their own characteristics:

  1. Tablets with a slow release of the active substance. They are oblong in shape and white-yellow in color. Packed in aluminum blisters of 10 pieces. The carton box contains 20 or 30 tablets.
  2. Capsules for oral administration. Packed in plastic blisters of 10 pieces. The cardboard box contains 30 or 100 capsules.
  3. Injection. It is a colorless or yellowish odorless transparent liquid. It is contained in glass ampoules with a volume of 5 ml (in 1 ampoule 50 mg of trazodone).

On the this moment Trazodone is not available in Russian pharmacies, and the cost of drugs with trazodone under the trade name Trittiko is presented below.

Composite Components

The composition of the drug is somewhat different depending on the dosage form:

  • a regular-acting capsule may contain 25, 50, or 100 mg of trazodone;
  • 5 ml of solution for intravenous or intramuscular administration contains 50 mg of the active substance, as well as additionally water for injection;
  • 1 tablet of prolonged action contains 75 or 150 mg of trazodone and auxiliary components - carnauba wax, sucrose, magnesium stearate and povidone.

Pharmacodynamics and pharmacokinetics

The mechanism of action of trazodone is not fully understood. Studies show that this substance is able to selectively inhibit the reuptake of serotonin by specific receptors in the brain. It is also an alpha1-adrenergic receptor antagonist. At the same time, trazodone does not inhibit MAO and has no effect on the stimulation of the central NS.

Mechanism of action of antidepressants

In addition to antipsychotic (eliminating manifestations of depression, fear), it has a slight sedative and hypnotic effect, improves the quality of sleep. It also tends to eliminate the somatic manifestations of anxiety:

  • cardiopalmus;
  • increased sweating;
  • frequent urination;
  • pain in the head and muscles.

Pharmacokinetic features of trazodone:

  • rapidly absorbed from the digestive organs;
  • the rate of absorption decreases when the substance is taken with or immediately after food;
  • the highest concentration is observed half an hour after ingestion (when taken with food - after 2 hours);
  • high connection with blood proteins (more than 90%);
  • able to penetrate the blood-brain and placental barriers;
  • the metabolic process occurs in the liver with the release of the active metabolite m-chlorophenylpiperazine;
  • excreted mainly by the kidneys (about 75%) and together with bile (20%);
  • the half-life takes 2 phases: the early one lasts up to 6 hours, the late one - from 5 to 9 hours;
  • complete elimination from the body occurs 98 hours after application.

Indications and contraindications for taking Trazodone

As a rule, the main indications for prescribing the drug are depressive states of various origins (neurotic, somatic, psychotic, depression due to external factors). They are often accompanied by emotional and physical tension, feelings of fear and anxiety.

Trazodone may also be used to treat the following conditions:


  • individual intolerance to the active substance;
  • severe violations of the functioning of the liver or kidneys;
  • priapism in men (prolonged painful erection that is not associated with arousal);
  • period of acute infarction;
  • violation of the heart rhythm;
  • severe poisoning from alcohol or certain drugs (for example, sleeping pills).

It is not recommended to use the drug for the treatment of children and adolescents until they reach the age of majority. They are much more likely than adults to develop suicidal tendencies while taking antidepressants.

During pregnancy, trazodone can be used, since clinical trials have not shown any negative effects on the fetus, its growth and development. Therapy is carried out with caution and only if the expected benefit to the mother is higher than the possible risk to the fetus. If a pregnant woman takes medication immediately before childbirth, then the newborn should be monitored in order to diagnose withdrawal syndrome in time.

Trazodone passes into breast milk in very small amounts. It is not known for certain how much this substance affects the child, so breastfeeding should be stopped while taking it.

Instructions for use of the drug Trazodone

The method of application and dosage regimen of the drug depends on the form of its release:


Maximum per day you can take no more than 600 mg of trazodone. The duration of therapy and dosage is determined by the attending physician individually for each patient.

Side effects

The drug can provoke various side effects. Often, when using it, thoughts of suicide arise (as with other antidepressants). Reactions that are characteristic of depression are also possible. Among side effects allocate:


Overdose

With a sharp discontinuation of the drug, a withdrawal syndrome may develop. As a rule, overdose symptoms appear on the first day after taking too high a dose. It can be:

  • bouts of nausea and vomiting;
  • dizziness;
  • drowsiness;
  • increased heart rate;
  • lowering blood pressure;
  • convulsions;
  • violation of respiratory activity;
  • coma.

Treatment of overdose is aimed at stopping the poisoning effect of trazodone. To do this, the patient's stomach is washed and sorbents are given (such actions are effective for 1 hour after poisoning). Next, symptomatic therapy is prescribed. At the same time, it is important to control the vital functions of the body (activity of the cardiovascular system, respiratory activity).

Analogues of the drug Trazodone

You can find many antidepressants on drugstore shelves. The most popular analogues of Trazodone:


Any antidepressant is prescribed only by the attending physician. Before prescribing a medicine, he takes into account the characteristics of the patient, his general condition and the severity of the symptoms.

It's no secret that the state of erection, the degree of libido, the general sexual capabilities of a man directly depend on his psychological state. It is experiences, stress, depression that lead not only to erectile dysfunction, but also to the complete suppression of normal sexuality. Therefore, it is imperative to begin treatment precisely with the stabilization of the neuropsychic state of the stronger sex, as well as with the fight against depression. Trazodone successfully fights these kinds of problems, which we will discuss below.

Instructions for use of Trazodone indicate that the drug belongs to the group of antidepressants that do not have an effect on MAO, that is, it does not stimulate the central nervous system (central nervous system). The mechanism of therapeutic action is still being studied to the end, however, antidepressant efficacy has been proven. The action of the drug is due to the fact that it selectively prevents the reuptake of serotonin by special synaptosomes of the brain. Trazodone is able to eliminate two groups of negative manifestations:

  1. Somatic, manifested by palpitations, increased sweating, headache, muscle pain (myalgia), frequent urination.
  2. Mental, a vivid example of which can be all sorts of fears, insomnia, a feeling of tension.

Studies have shown that Trazodone is metabolized in the liver and completely eliminated from the body after 98 hours. The drug is well absorbed from gastrointestinal tract.

In the pharmacy network, you can also find Trazodone analogues. The following are the most popular:

  1. Trittiko.
  2. Azona.

The active substance and dosage in all medicines are the same, so the indications, contraindications and method of use for the original will not differ from those that have analogues.

Usage details

Indications for the use of Trazodone are not limited to disorders of the sexual sphere in men. The instruction indicates the following diseases for which therapy with this drug is possible:

  • Decreased libido against the background of a depressive state.
  • Erectile dysfunction due to depression and other psychological problems.
  • Various forms of depression (involutional, psychogenic, alcoholic).
  • Depressive manifestations in organic diseases of the central nervous system, that is, in Alzheimer's disease, dementia, atherosclerosis of cerebral vessels.

In any case, the final indications are determined by the doctor, therefore, before using Trazodone, consultation with a specialist is required. In some cases, men tend not to take depression, depression seriously, attributing impotence to anything but the deplorable state of their own nervous system. Therefore, self-medication is strictly prohibited. The specialist will determine true reason erectile dysfunction, which means he will prescribe the right treatment.

Unfortunately, not everyone can prescribe Trazodone and analogues. The instructions contain the following contraindications for use:

  1. Pathology of the heart and blood vessels: recent myocardial infarction, rhythm and conduction disturbances (atrioventricular blockade, ventricular arrhythmias). Patients with arterial hypertension may need to change the selected dosages of antihypertensive drugs.
  2. Gastrointestinal diseases: liver failure.
  3. Kidney disease, accompanied by a violation of the normal function of the kidneys and renal failure.
  4. Priapism. If a man has previously had an episode of a prolonged, painful erection that required medical intervention, Trazodone is categorically contraindicated.
  5. Age limit: under 18 years of age and in childhood, you can not prescribe the medicine.

Trazodone and its analogues can be prescribed to women to treat depression, but only if the lady is not pregnant and not breastfeeding. The full range of contraindications can be found in the instructions for Trazodone. Also, you can not use the drug for people who are hypersensitive or allergic to any component of the drug. Reviews of doctors confirm that the potential harm to health in such cases significantly exceeds the expected benefits.

During clinical trials, the adverse effects that trazodone hydrochloride has on the body have been identified:

  • CNS and sense organs. Patients may complain of general weakness and fatigue, sleep disturbance, dizziness. More rare side effects were hallucinations, trembling of the limbs (tremor), impaired sensitivity, convulsions, etc.
  • Heart and blood vessels. Observed arterial hypotension, arrhythmias.
  • From the side of hematopoiesis. Perhaps a decrease or increase in leukocytes, neutropenia, rarely - hemolytic anemia.
  • Gastrointestinal tract. Increased appetite, a feeling of unpleasant aftertaste in the mouth, hypersalivation (increased salivation), dyspepsia, bloating, bile stasis. In some cases, an increase in liver parameters (bilirubin, amylase), jaundice was observed.
  • Urogenital system. Priapism, urinary disorders.
  • The immune system. Like all medicines, Trazodone can cause allergies.

More rare extrasystemic manifestations were alopecia (alopecia), skin diseases (psoriasis), chest pain without an appropriate diagnosis. Symptoms of an overdose resemble those of side effects, but are more clinically pronounced. For treatment, symptomatic therapy is used, since there are no specific antidotes.

special instructions

Given the characteristics of metabolism and the effects of the drug on the body, together with some other drugs, Trazodone should be administered with caution.

  • Ritonavir. In clinical trials in healthy patients, it was noted that Ritonavir slows down the half-life of Trazodone and increases the risk of side effects: nausea, syncope, hypotension.
  • Other inhibitors of CYP3A4 (fluoxetine, ketoconazole). They act like Ritonavir, which belongs to the same group.
  • Carbomazepine. Reduces the concentration of the drug in the blood, and therefore, Trazodone may not have the desired effect.
  • Warfarin. Currently, studies are underway on their combined use. There are already facts that both drugs mutually affect the concentration of active components in the blood serum, which is confirmed by the reviews of scientists published on specialized sites.
  • Antihypertensive drugs. Caution should be exercised when used together, as the risk of hypotension increases.

Reviews of researchers indicate that during treatment with Trazodone, it is necessary to monitor general blood counts (leukocytes, blood count), determine the level of liver enzymes, and do an ECG (electrocardiogram). During treatment, it is advisable to refrain from driving vehicles and working with precise mechanisms.

Method of use

The method of application may vary slightly in men of different groups. In some situations, single and daily doses should be slightly adjusted:

A tablet of the original drug or analogue is taken before meals or 3-4 hours after, since simultaneous use with food slows down the absorption of Trazodone. In the event that combined therapy for erectile dysfunction is prescribed, the dose of Trazodone is reduced to 50 mg / day.

Where to follow him

It is better to purchase the remedy in a pharmacy, which is confirmed by the reviews of doctors. The price of a medicine and its analogues may fluctuate in different regions:

When buying from online pharmacies, the price may include postage or courier fees. Check this information.

Be aware that Trazodone is a serious drug, which is undesirable to take without medical prescription. Therefore, no matter how much you want to quickly get rid of erectile dysfunction on the background of depression, you should not prescribe this medicine yourself.

Ivan, 32 years old:

Against the backdrop of depression, sexual desire disappeared. After a month of using Tradozon positive effect appeared to be good. I will definitely continue the treatment prescribed by the doctor.

Valery Sergeevich, 47 years old:

The erection disappeared along with any desire to have sex after severe stress, against the backdrop of depression that followed. I started taking Tradozon after consulting a doctor and have no regrets. Firstly, it really got better after a while sex life Secondly, the depression receded. Now I look at things positively.

Sergey Leonidovich, psychotherapist:

Indeed, Trazodone and its analogues are able to successfully deal with erectile dysfunction in men suffering from depression. The drug has long been adopted by the specialists of the clinic where I work. The main thing is the right approach to therapy, and then the sex life is getting better quickly.

INN: Trazodone

Manufacturer: Aziende Kimike Riunite Angelini Francesco A.K.R.A.F. S.p.A

Anatomical-therapeutic-chemical classification: Trazodone

Registration number in the Republic of Kazakhstan: No. RK-LS-5 No. 019504

Registration period: 06.04.2018 - 06.04.2023

Instruction

Tradename

Trittiko

International non-proprietary name

Trazodone

Dosage form

Extended release tablets, 150 mg

Composition

One tablet contains

active substance - trazodone hydrochloride 150 mg,

Excipients: sucrose, carnauba wax, povidone, magnesium stearate.

Description

Tablets are white or white with a yellowish tinge, oval-shaped with two parallel risks on both sides.

Pharmacotherapeutic group

Psychoanaleptics. Other antidepressants.

ATX code N06AX05

Pharmacological properties

Pharmacokinetics

Absorption of the drug from the gastrointestinal tract (GIT) after oral administration is high. Taking trazodone during or immediately after a meal slows down the absorption rate, reduces the maximum concentration of the drug in the blood plasma and increases the time to reach the maximum concentration (hereinafter referred to as TCmax). TCmax of the drug is reached after ½ - 2 hours after ingestion.

The drug penetrates through histohematic barriers, as well as into tissues and fluids (bile, saliva, breast milk).

Communication with plasma proteins - 89-95%.

Trazodone is metabolized in the liver, the active metabolite is 1-m-chlorophenylpiperazine. The half-life is 3-6 hours, in the second phase - 5-9 hours. Most of the metabolized drug is excreted through the kidneys, about 75% is excreted in the urine and is completely completed 98 hours after ingestion, about 20% is excreted in the bile.

Pharmacodynamics

Trittico, being a derivative of triazolopyridine, has a predominantly antidepressant effect, with some sedative and anxiolytic effects.

Quickly affects mental (affective tension, irritability, fear, insomnia) and somatic symptoms of anxiety (palpitations, headache, muscle pain, frequent urination, sweating, hyperventilation).

Trittiko is effective in sleep disorders in patients with depression, increases the depth and duration of sleep, restores its physiological structure and quality.

Trittiko stabilizes the emotional state, improves mood, reduces the pathological craving for alcohol in patients suffering from chronic alcoholism during the period of alcohol withdrawal syndrome, as well as in remission. With withdrawal symptoms in patients suffering from dependence on benzodiazepine derivatives, Trittiko is effective in the treatment of anxiety-depressive conditions and sleep disorders. During remission, benzodiazepines can be completely replaced by Trittiko.

Promotes the restoration of libido and potency both in patients with depression and in those who do not suffer from depression.

The mechanism of action of Trittiko is associated with the high affinity of the drug for certain subtypes of serotonin receptors, with which Trittiko enters into antagonistic or agonistic interaction depending on the subtype, as well as with the specific ability to cause inhibition of serotonin reuptake.

Neutral uptake of norepinephrine and dopamine is little affected.

Indications for use

Depressive disorders, with or without:

Anxiety

sleep disorder

Sexual dysfunctions of non-organic etiology

Dosage and administration

The drug is intended exclusively for adults.

adults

The drug should be taken orally 30 minutes before a meal or 2-4 hours after a meal. When taken after a meal, the development of undesirable effects is slowed down (re-absorption increases and peak plasma concentration decreases). Tablets should be taken without chewing, drinking plenty of water.

Tablets can be divided into 3 parts in order to select the optimal dose depending on the severity of the disease, age and general condition of the patient.

The initial dose of the drug is 50-100 mg, taken once at bedtime after meals. On the 4th day, you can increase the dose to 150 mg. Further increase in dosage in order to achieve the optimal therapeutic effect should be made by 50 mg / day every 3-4 days until the optimal dose is reached. A daily dose of more than 150 mg should be divided into 2 doses, with a smaller dose taken after dinner, and the main dose at bedtime.

The maximum daily dose for outpatients is 450 mg.

The maximum daily dose for inpatients is 600 mg.

elderly people

For the elderly and debilitated people, the initial dose is up to 100 mg / day in divided doses or once at bedtime. It can be increased under the supervision of a physician, depending on the effectiveness and tolerability of the drug. Doses in excess of 300 mg/day are usually not required.

Patients with liver failure

Trittiko undergoes intensive hepatic metabolism.

Patients with renal insufficiency

As a rule, individual dosage adjustment is required, however, it is recommended to exercise caution when taking Trittiko in patients with severely impaired renal function.

Trittiko should be used in therapeutic cycles of at least one month.

Children

The safety of Trittico in children under 18 years of age has not been established. Therefore, the use of the drug by children and adolescents is not recommended.

Side effects

Possible

Fatigue, weakness, drowsiness, agitation, headache, dizziness, decreased vigilance, disorientation, tremor, memory disorder, myoclonus, expressive aphasia, paresthesia, dystonia, epileptic seizures, narcoleptic malignant syndrome

Suicidal thoughts, or suicidal behavior, confused

states, mania, feeling of fear, nervousness, agitation (usually aggravated to delirium), delirium, aggressive reaction

Withdrawal withdrawal syndrome

Nasal congestion, dyspnea

Palpitations, decreased blood pressure, orthostatic hypertension

(especially in persons with vasomotor lability), due to the adrenolytic effect of the drug, arrhythmia, ventricular extrasystoles, tachycardia, including ventricular paroxysmal, conduction disturbance, bradycardia, ECG disturbances (increased QT interval)

Decreased or increased appetite, anorexia, dryness and bitterness in the mouth,

change in taste sensations, increased salivation, nausea, vomiting, diarrhea, abdominal pain, weight loss, gastroenteritis, paralytic ileus

Pain in limbs, back pain, myalgia, arthralgia

Urination disorder

Itching, erythematous rash

Flu-like syndrome, chest pain, fever

Leukopenia, neutropenia, agranulocytosis, thrombocytopenia,

eosinophilia (usually minor), anemia

Syndrome of inappropriate secretion of antidiuretic hormone

Increasing the content of liver enzymes

Hyperhidrosis

Eye irritation

Priapism (patients who experience this side effect,

should immediately stop taking the drug and consult a doctor)

Contraindications

Hypersensitivity to the active substance or any

excipient

Alcohol or hypnotic intoxication

Acute heart failure

Pregnancy and lactation

Drug Interactions

The sedative effects of antipsychotic, hypnotic, sedative, anxiolytic and antihistamine drugs may increase, in these cases it is necessary to reduce the dosage.

The hepatic effects of oral contraceptives, phenytoin, carbamazepine, and barbiturates accelerate the metabolism of antidepressants, while cimetidine and other antipsychotics inhibit it.

Cytochrome enzyme inhibitors

There is a potential pharmacological interaction with the simultaneous use of Trittiko and cytochrome inhibitors such as erythromycin, ketoconazole, itraconazole, ritonavir, indinavit and nefazadone. Cytochrome inhibitors can contribute to a significant increase in plasma concentrations of trazodone.

Co-administration of Trittico and strong inhibitors of cytochromes should be avoided or a lower dose of the drug should be prescribed.

Carbamazepine

Plasma concentrations of trazodone are reduced by concomitant administration of carbamazepine. Concomitant use of carbamazepine resulted in a reduction in levels of trazodone and its active metabolite, metachlorphenylpiperazine, by 76% and 60%, respectively. Therefore, patients who take Trittiko and carbamazepine concomitantly should be closely monitored to assess the need for higher dosages.

Tricyclic antidepressants

The simultaneous use of Trittico and tricyclic antidepressants is not recommended, due to the possible risk of interaction. Perhaps the development of serotonergic syndrome and adverse reactions from the cardiovascular system.

fluoxetine

Rare cases of increased plasma levels of trazodone and the development of adverse reactions have been reported while taking Trittiko and fluoxetine. The mechanism of their pharmacokinetic interaction is unclear. Serotonin syndrome may result from this pharmacodynamic interaction.

Monoamine oxidase (MAO) inhibitors

The simultaneous appointment of Trittiko and monoamine oxidase inhibitors, as well as the appointment of Trittiko earlier than two weeks after the abolition of monoamine oxidase inhibitors, is strongly not recommended. It is also not recommended to prescribe monoamine oxidase inhibitors earlier than one week after discontinuation of the drug, since MAO inhibitors increase the risk of side effects of Trittiko.

Phenothiazines

With the simultaneous administration of Trittico with phenothiazines (chlorpromazine, fluphenazine, levomepromazine, perphenazine), severe orthostatic hypertension was observed.

Muscle relaxants and gaseous anesthetics

Trittico may enhance the effect of muscle relaxants and gaseous anesthetics.

Antihypertensive drugs

Trittico may enhance the effect of some antihypertensive drugs and usually requires a reduction in their doses.

Antihistamines and drugs with anticholinergic activity enhance the anticholinergic effect of Trittico.

When Trittiko is used with digoxin and phenytoin, the concentration of these drugs in the blood plasma increases.

Undesirable effects may be more frequent when taking Trittiko together with medicines containing certain medicinal plants such as St. John's wort.

In patients treated with Trittico and warfarin, cases of altered prothrombin time have been reported.

special instructions

Use by children and adolescents under the age of 18

As a general rule, Trittiko should not be taken by children and adolescents under 18 years of age.

In clinical studies conducted with the participation of children and adolescents, cases of suicidal behavior (suicide attempts, suicidal thoughts) and hostility (significant aggressiveness, conflict behavior and anger) occurred more often in those treated with antidepressants compared to those who took placebo.

Moreover, there are no data on the safety of long-term effects of Trittico in children and adolescents, including growth, maturation, cognitive and behavioral development.

Suicide/suicidal ideation or clinical deterioration

Depression associated with an increased risk of suicidal thoughts, self-harm and suicide. The risk exists until there is a significant weakening of the disease. Since improvement may not occur during the first few weeks of treatment or more, patients should be closely monitored until improvement occurs. Clinical experience shows that the risk of suicide may increase in the early stages of recovery.

To reduce the potential risk of suicide attempts, especially at the beginning of therapy, the dosage of Trittiko given at each patient visit should be gradually reduced.

The drug should be administered with caution to patients with AV blockade of varying severity, myocardial infarction (in the early recovery period), arterial hypertension (dose adjustment of antihypertensive drugs may be required), ventricular arrhythmia, a history of priapism, with renal and / or hepatic insufficiency.

Special attention to dosage and regular monitoring of elderly patients suffering from prostatic hypertrophy, urination disorders, angle-closure glaucoma, hyperthyroidism is recommended.

If you experience prolonged and inadequate erections, you should consult a doctor.

When using Trittiko, a slight decrease in the number of leukocytes is possible, which does not require specific treatment, except in cases of severe leukopenia. Developing agranulocytosis can manifest itself with symptoms characteristic of influenza. Therefore, it is recommended to conduct studies of peripheral blood, especially in the presence of pain in the throat when swallowing and the appearance of fever.

In patients with schizophrenia or various psychiatric disorders, antidepressants may exacerbate psychotic symptoms. Paranoid thoughts may develop more intensely. With Trittiko therapy, depressive episodes can range from manic-depressive to manic psychosis. In this situation, it is necessary to interrupt the treatment.

During treatment, you should refrain from drinking alcohol.

Trittiko contains sucrose, so patients with hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase deficiency should not take this medicine.

Features of the effect of the drug on the ability to drive vehicles and work with potentially dangerous mechanisms

You should refrain from engaging in potentially hazardous activities that require concentration and quick psychomotor reactions, as the drug has anxiolytic and sedative activity.

Overdose

Symptoms: drowsiness, dizziness, nausea, vomiting, increased frequency and severity of side effects. In more severe cases, tachycardia, arterial hypotension, hyponatremia, convulsions, respiratory failure, coma are possible.

Treatment: there is no specific antidote for the drug. In cases of overdose, administration of activated charcoal should be considered for those who have taken more than 1 g of trazodone within one hour. Alternatively, gastric lavage may be administered within one hour of overdosing.

In case of an overdose, the patient should be closely monitored for at least 6-12 hours after taking the drug. Control of pulse and arterial pressure is required.

Release form and packaging

10 or 20 tablets are placed in a blister pack made of PVC film and aluminum foil.

1 blister pack of 20 tablets or 2 blister packs of 10 tablets each, together with instructions for medical use in the state and Russian languages, is placed in a cardboard box.

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