Doxepin capsules 25 mg, 30 pcs.

Pharmacological properties of the drug Doxepin

Tricyclic antidepressant, dibenzoxepin derivative. Effective in the treatment of psychoneurotic disorders with manifestations of anxiety and/or depression, psychosomatic disorders, sleep disorders accompanying depressive states. It has anxiolytic and sedative activity. Inhibits the reuptake of monoamines (adrenaline and norepinephrine) by presynaptic nerve endings, promoting their accumulation in the synaptic cleft and the manifestation of their neurotransmitter effect. Doxepin has antihistamine, anticholinergic and α1-adrenergic blocking effects. Well absorbed in the digestive tract. The maximum concentration in blood plasma is observed 1–3 hours after oral administration. Therapeutic concentration in the blood is usually achieved 2 weeks after the start of the course of use. Doxepin is metabolized in the liver mainly by demethylation and excreted in the urine as metabolites. The half-life is 8–24 hours. Doxepin crosses the placenta and blood-brain barrier, as well as into breast milk.

* Attention! Product packaging may differ from that shown in the photo.

Product description

Composition
active ingredient: doxepin; 1 capsule contains Doxepin 10 mg or 25 mg in the form of Doxepin hydrochloride, excipients:

corn starch lactose magnesium stearate sodium lauryl sulfate;
capsule shell:
indigo (E 132) titanium dioxide (E 171) gelatin erythrosine (E 127) for 10 mg capsules, patented blue V (E 131) is added.

Dosage form

Capsules.

Pharmacological group

Antidepressants. Non-selective inhibitors of neuronal monoamine reuptake. ATC code N06A A12.

Indications

Neurotic disorders with symptoms of depression or anxiety. Organic neuroses associated with insomnia. Depressive and anxiety states in alcoholism. Depression and anxiety associated with somatic disorders and diseases. Depression is accompanied by fear and anxiety against the background of psychoses, including involutional depression and the depressive phase of bipolar disorders.

Contraindications

Hypersensitivity to the drug; cross-sensitivity to other dibenzoxepins. Manic syndrome, severe liver dysfunction, glaucoma, urinary retention, simultaneous use with MAO inhibitors or their use 2 weeks before starting Doxepin treatment. Hypersensitivity to tricyclic antidepressants. Tendency to retain urine.

Directions for use and doses

Apply internally. The doctor selects the dose individually depending on the severity of the symptoms and the therapeutic effect.

The dose of Doxepin is 30-300 mg per day. Doses up to 100 mg can be used as a single dose or divided doses. Doses exceeding 100 mg should be administered in 3 divided doses. The maximum single dose is 100 mg (use before bedtime).

For moderate to severe symptoms, the starting dose is 75 mg daily.

For most patients, this dose is satisfactory. In severe forms of the disease, the dose is increased to 300 mg (in 3 doses).

In patients with insomnia, the total dose should be distributed so that the larger dose is administered in the evening. In cases where insomnia is reported as an adverse reaction, this dosage regimen can be used or the dose should be reduced.

After achieving a satisfactory therapeutic effect, the dose of the drug should be adjusted to the minimum maintenance level.

Reduction of anxiety symptoms when taking Doxepin is achieved earlier than the antidepressant effect. The antidepressant effect appears after 2-3 weeks of treatment.

For elderly patients with moderate symptoms, half the usual recommended dose of Doxepin (10-50 mg daily) is recommended. Satisfactory clinical effects were obtained after using Doxepin at a dose of 30-50 mg per day. The dose of the drug should be adjusted individually depending on the patient's clinical response to the drug.

Patients with impaired liver function should reduce doses.

Adverse reactions

Doxepin is generally well tolerated. Most side effects of moderate severity occur at the beginning of treatment and disappear after discontinuation of the drug or reduction in its dose. Some of the adverse reactions listed below are not specific to Doxepin; however, the possibility of these reactions should be taken into account due to the similarity of its pharmacological properties with other tricyclics.

Adverse reactions are distributed according to the frequency of manifestations: very often (> 1/10); common (> 1/100 <1/10) uncommon (> 1/1000 <1/100) rare (> 1/10000 <1/1000) very rare (> 1/10,000) unknown (frequency cannot be determined according to available information).

From the nervous system and mental disorders.

• Very often drowsiness.
• Uncommon: headache dizziness insomnia nightmares confusion disorientation anxiety numbness or paresthesia tremor (usually moderate). When using high doses (especially in elderly patients), extrapyramidal symptoms including tardive dyskinesia may occur.
• Rarely, hallucinations, ataxia (only if several drugs acting on the central nervous system are used), convulsions (in patients prone to seizures, the cause of which may be brain damage or alcohol use and substance abuse).
• Unknown: Suicidal thoughts and behavior.
• Cases of suicidal thoughts and behavior have been reported during treatment with Doxepin or immediately after its discontinuation.
• Psychiatric manifestations including mania and paranoid hallucinations may be exacerbated by treatment with tricyclic antidepressants. Tinnitus has been reported occasionally.

From the organs of vision.

• Very rare: visual disturbances (blurredness).

From the vascular system.

• Rarely, orthostatic hypotension and facial flushing.

From the cardiovascular system.

• Very rarely, tachycardia ECG abnormalities (widening of the QRS complex, prolongation of the PR interval).

From the immune system.

• Uncommon: allergic reactions including skin rashes, swelling of the face, photosensitivity, itching, urticaria.
• During treatment with tricyclic antidepressants, exacerbation of bronchial asthma is possible.

From the skin and subcutaneous tissue.

• Rarely: increased sweating, allergic skin reactions listed above.
• Very rarely alopecia.

From the blood and lymphatic systems.

• Rarely: eosinophilia and bone marrow dysfunction with symptoms such as agranulocytosis, leukopenia, thrombocytopenia purpura and hemolytic anemia.

From the gastrointestinal tract.

• Very often there is dryness of the mucous membranes of the mouth and nose and constipation.
• Rarely: nausea, vomiting, dyspepsia, disturbance of taste, diarrhea, anorexia, stomatitis.

From the endocrine system.

• Rarely: impaired secretion of ADH, gynecomastia, enlargement of the mammary glands, galactorrhea in women.
• Isolated cases of changes in libido, testicular swelling, increased or decreased blood glucose levels.

From the kidneys and urinary system.

• Rarely, urinary retention (complaints may intensify in men with prostate hypertrophy).

From the digestive system.

• Rarely jaundice.

General violations.

• Very common: fatigue, weakness, weight gain, chills, hyperpyrexia (in patients taking chlorpromazine at the same time).

Cancel Doxepin.

• If tricyclic antidepressants are stopped suddenly, withdrawal symptoms may occur including insomnia, irritability and excessive sweating. Withdrawal symptoms in newborns of mothers taking tricyclic antidepressants during the third trimester include: depression of respiratory function, convulsions and hyperreflexia.

Overdose

Symptoms:

drowsiness anxiety dry mouth stupor blurred vision arrhythmia. If such symptoms occur, the drug should be discontinued and the patient examined.

In case of severe overdose, there may be a decrease/increase in blood pressure, dilation of the pupils, tachycardia, urinary retention (bladder atony), ileus, hyperthermia/hypothermia, respiratory depression, increased sweating, convulsions, coma.

Treatment:

discontinuation of the drug, gastric lavage, artificial ventilation, control of the cardiovascular system, use of sleeping pills. If necessary, administer physostigmine salicylate 1-3 mg. Features of application. Hemodialysis and forced diuresis are ineffective.

Use during pregnancy and lactation

Animal reproductive studies did not reveal any adverse effects on the fetus; There have been no adequate and well-controlled studies in pregnant women. Thus, during pregnancy, the drug is used only in cases where the expected benefit to the mother outweighs the potential risk to the fetus.

Doxepin passes into breast milk, so breastfeeding should be discontinued during treatment.

Children

The safety and effectiveness of Doxepin in children have not been established.

Features of application

Patients with concomitant diseases or patients taking other medications should use a single dosage regimen. This also applies to patients who are taking drugs with anticholinergic effects.

Elderly patients should also use this dosage regimen and adjust it with caution. These patients are prone to developing adverse reactions such as anxiety, confusion and orthostatic hypotension. Therefore, the initial dose should be prescribed with caution and under close monitoring of the patient's condition and response to the drug. For an appropriate clinical effect, half the dose of Doxepin may be sufficient.

Patients should be advised that drowsiness may occur during treatment and drinking alcohol may enhance the effect of the drug.

If the symptoms of psychosis or manic episodes worsen during treatment with Doxepin, it may be necessary to reduce the dose of Doxepin or add drugs from the group of tranquilizers (neuroleptics) to the treatment regimen.

Although the use of Doxepin has less effect on the vascular system than other tricyclic antidepressants, it should be used with caution in patients with severe cardiovascular disease (heart block, cardiac arrhythmia and recent myocardial infarction).

Doxepin should be used with caution in patients with hepatic renal impairment and in patients with a history of epileptic seizures.

Suicide/suicidal ideation or clinical deterioration.

Patients with severe depression are at risk of developing suicidal thoughts and actions that may persist until significant remission is achieved. If improvement does not occur within the first few weeks of treatment or even more, patients require careful monitoring until improvement occurs. It is known from general clinical practice that the risk of suicidal thoughts or actions may increase in the early stages of treatment.

Other psychiatric conditions for which doxepin is prescribed also have an increased risk of suicide. Therefore, special safety measures must be observed for such patients.

Careful monitoring is required throughout treatment for patients with a history of suicidal ideation or suicide attempts.

Careful monitoring of patients, especially at high risk, should be combined with the administration of appropriate medications, especially in the early stages, followed by dose adjustments if necessary. Patients (and those caring for them) should be informed of the need to monitor for any clinical worsening of suicidal thoughts or unusual changes in behavior and to seek immediate medical attention if these symptoms occur.

A meta-analysis of placebo-controlled studies of antidepressants in adult patients with mental disorders showed an increased risk of suicidal behavior in patients under 25 years of age compared with placebo.

In patients with moderate prostatic hypertrophy, urinary retention may increase.

Doxepin contains lactose; therefore, patients with rare hereditary forms of galactose intolerance, glucose-galactose malabsorption syndrome, and Lapp lactase deficiency are not recommended to prescribe it.

Patients with hypersensitivity or gluten intolerance should not use this drug as its excipients include corn starch.

The ability to influence the reaction rate when driving vehicles or other mechanisms

During treatment with Doxepin, it is prohibited to drive vehicles or operate complex mechanisms that require concentration, since Doxepin can lead to drowsiness and other negative reactions from the central nervous system.

Interaction with other drugs and other types of interactions.

With the simultaneous use of ethanol, antidepressants, barbiturates, benzodiazepines and general anesthetics, a significant increase in the inhibitory effect on the central nervous system, respiratory depression and a hypotensive effect is possible. Doxepin enhances the anticholinergic effect of amantadine. Phenothiazines antiparkinsonian drugs atropine biperiden antihistamines increase the risk of side effects from the central nervous system vision of the intestines of the bladder. When used simultaneously with antihistamines, clonidine increases the inhibitory effect on the central nervous system; with atropine - the risk of paralytic intestinal obstruction increases; with drugs that cause extrapyramidal reactions - body weight and the frequency of extrapyramidal effects increase. With the simultaneous use of Doxepin with indirect anticoagulants (coumarin or indadione derivatives), the anticoagulant activity of the latter may increase. Doxepin may increase depression caused by corticosteroids. When used together with anticonvulsants, it is possible to enhance the inhibitory effect on the central nervous system, reduce the threshold of convulsive activity (when used in high doses) and reduce the effectiveness of the latter. Drugs used to treat thyrotoxicosis increase the risk of developing agranulocytosis. Reduces the effectiveness of phenytoin and a-blockers. Inhibitors of microsomal oxidation (cimetidine) prolong the half-life, increase the risk of developing toxic effects of Doxepin (a 20-30% dose reduction of Doxepin may be required), inducers of microsomal liver enzymes (barbiturates carbamazepine phenytoin nicotine and oral contraceptives) reduce plasma concentrations and reduce the effectiveness of doxepin. Fluoxetine and fluvoxamine increase plasma concentrations of Doxepin (a 50% reduction in Doxepin dose may be required). When used simultaneously with anticholinergic phenothiazines and benzodiazepines, there is a mutual enhancement of the sedative and central anticholinergic effects and an increased risk of epileptic seizures (lowering the threshold of convulsive activity); Phenothiazines may also increase the risk of neuroleptic malignant syndrome. With simultaneous use of Doxepin with clonidine, guanethidine, betanidine, reserpine and methyldopa, the hypotensive effect of the latter is reduced; with cocaine - the risk of developing cardiac arrhythmias. Estrogen-containing oral contraceptives and estrogens may increase the bioavailability of Doxepin; antiarrhythmic drugs (quinidine) increase the risk of developing rhythm disturbances (possibly slowing down the metabolism of Doxepin). Concomitant use with disulfiram and acetaldehydrogenase inhibitors provokes delirium. Incompatible with MAO inhibitors (possible increase in the frequency of periods of hyperpyrexia, severe convulsions, hypertensive crises and death of the patient). Pimozide and probucol can increase cardiac arrhythmias, which is manifested by prolongation of the QT interval on the ECG. The effect on the cardiovascular system of epinephrine, norepinephrine, isoprenaline, ephedrine and phenylephrine is enhanced (including when these agents are part of local anesthetics) and the risk of developing heart rhythm disturbances, tachycardia, and severe arterial hypertension increases. The simultaneous use of a-adrenergic receptors for intranasal administration or for use in ophthalmology (with significant systemic absorption) may enhance the vasoconstrictor effect of the latter. When used together with thyroid hormones, there is a mutual enhancement of the therapeutic effect and toxic effects (including cardiac arrhythmias and stimulating effects on the central nervous system). M-anticholinergics and antipsychotics increase the risk of developing hyperpyrexia (especially in hot weather).

Pharmacological properties

Pharmacological.

Doxepin belongs to the group of tricyclic antidepressants. The antidepressant effect is combined with anxiolytic and sedative.

Doxepin inhibits the reuptake of biogenic amines (norepinephrine and serotonin) in synaptic structures. It also has antihistamine cholinolytic and α1-adrenergic blocking effects. Does not cause euphoria of psychomotor agitation.

Pharmacokinetics

Doxepin is well absorbed from the digestive tract quickly (2-4 hours after administration) and reaches its maximum concentration in the blood serum. A stable therapeutic concentration in the blood is achieved 2 weeks after the start of treatment.

Doxepin is metabolized in the liver mainly by demethylation to form the main metabolite, desmethyldoxepin (nordoxepin). The binding of Doxepin and its metabolites to plasma proteins is about 76%. Distribution volume: about 20 l/kg. The half-life of Doxepin is 8-24 hours; the main active metabolite is 33-80 hours. Doxepin crosses the placenta and blood-brain barrier and passes into breast milk.

Basic physical and chemical properties

white powder in cylindrical capsules with rounded ends and size No. 4. For 10 mg capsules - body - blue; cap - cherry; for capsules of 25 mg - body - pink, cap - cherry.

Best before date

4 years.

Storage conditions

Store at a temperature not exceeding 25 ° C, protected from light and out of the reach of children.

Package

10 capsules in a blister, 3 blisters in a cardboard package.

Vacation category

On prescription.

Use of the drug Doxepin

Orally, usually at an initial dose of 30–75 mg/day in 3 divided doses. In patients with moderate or severe psychoneurotic symptoms, the dose can be gradually increased to 150 mg/day. To achieve a satisfactory result in severe depression, a maximum daily dose of 300 mg may be necessary. Once clinical effect is achieved, the dose can be reduced accordingly. Maintenance dose: 25–50 mg/day in 2–3 divided doses. Children over 12 years of age are prescribed at the rate of 0.5 mg/kg body weight per day in several doses. For sleep disorders, most of the daily dose is prescribed in the evening. An alternative method of treatment is to administer the entire daily dose (up to 150 mg) at bedtime (without reducing the effectiveness of treatment).

Drug interactions Doxepin

Incompatible with MAO inhibitors; doxepin is prescribed no earlier than 2 weeks after their discontinuation. Doxepin should not be used simultaneously with sulpiride, chlorpromazine, quinidine; Use with caution in combination with baclofen and digitalis glycosides. Doxepin potentiates the action of atropine and the central action of levodopa, as well as the toxic effects of barbiturates, morphine and pethidine. The combination of doxepin with antipsychotics requires a reduction in the dose of doxepin by 50%. The simultaneous use of lithium preparations and ethanol intake may potentiate the depressant effect of doxepin.

List of pharmacies where you can buy Doxepin:

• Moscow
• Saint Petersburg

Overdose

In clinical practice, an overdose of Doxepin can be provoked by taking doses of the drug that are more than recommended and manifest itself as a change in consciousness, in the form of drowsiness or stupor, decreased visual acuity, heart rhythm disturbances,

Severe drug poisoning can stimulate a sharp decrease in blood pressure, tachycardia, urinary retention, respiratory depression with the subsequent appearance of convulsive syndrome and coma.

Interaction

The combined internal use of Doxepin with barbiturates, morphine, atropine, chlorpromazine, quinidine is not recommended, since in some cases the action of the drug is potentiated, and in some its toxicity increases.

When combined with an antidepressant and a neuroleptic, the dosage of the latter should be reduced by 50%. Exercise caution and mandatory medical supervision when additionally prescribing digitalis medications.