Desyrel 100 mg Tablets

Brand name

The trade name of the drug is Desyrel. This is the registered name under which the drug is known in medical practice and is available for purchase in pharmacies.

International Nonproprietary Name (INN)

The international nonproprietary name is trazodone. It indicates the active ingredient and is used in pharmacology at the global level.

Form of release

Desirel is available as tablets with dosages of 50 mg, 100 mg and 150 mg, packed in blisters of 10 or 20 pieces. Tablets have a white or slightly yellowish color, round shape and a risk for easy division. In some countries, the drug is available in the form of prolonged-release capsules (Desirel XR) of 150 mg and 300 mg, and as a solution for injection (25 mg/mL), although the latter form is less common and is used in hospitals.

Composition

Active substance

The main active ingredient is trazodone hydrochloride. One tablet contains 50 mg, 100 mg or 150 mg of trazodone hydrochloride, XR capsule contains 150 mg or 300 mg, and 1 ml of solution for injection contains 25 mg.

Auxiliary Components

Tablets include substances such as lactose monohydrate, microcrystalline cellulose, sodium starch glycolate, povidone, magnesium stearate. Capsules contain gelatin, titanium dioxide, microcrystalline cellulose and polymers for prolonged release. The solution for injection consists of sodium chloride, water for injection, and hydrochloric acid to stabilize the pH.

Pharmacologic Properties

Pharmacodynamics

Trazodone, the active ingredient of Desirel, has a complex mechanism of action that distinguishes it from other antidepressants. It is a serotonin 5-HT2A receptor antagonist and at the same time a weak serotonin reuptake inhibitor. Blockade of 5-HT2A receptors reduces excessive serotonin stimulation associated with anxiety and insomnia, whereas inhibition of serotonin reuptake increases its concentration in the synaptic cleft, improving mood and emotional stability. In addition, trazodone has antagonistic action on alpha-1-adrenoreceptors and histamine H1-receptors, which accounts for its pronounced sedative effect.

Sedative effect is faster than antidepressant effect: improvement of sleep is noticeable in the first days of use, while the full antidepressant effect develops after 2-4 weeks. The drug has no significant effect on the dopamine system and does not have anticholinergic properties, which reduces the risk of side effects such as dry mouth or constipation, typical for tricyclic antidepressants. Desyrel is particularly effective for depression with severe insomnia and anxiety, making it the preferred choice for patients with these symptoms.

Pharmacokinetics

Absorption

Trazodone is well absorbed from the gastrointestinal tract after oral administration. Maximum plasma concentration is reached in 1-2 hours for conventional tablets and in 4-6 hours for prolonged-release capsules. Bioavailability is about 65-80%, and food intake increases the degree of absorption by 20%, which allows to take the drug with food for better tolerability.

Distribution

Distribution

The drug actively binds to blood plasma proteins (89-95%), mainly to albumin. The volume of distribution is about 0.8-1.5 L/kg, indicating moderate penetration into tissues, including the central nervous system. Trazodone crosses the blood-brain barrier, ensuring its action at the level of the brain.

Metabolism

Trazodone is metabolized in the liver by cytochrome P450 enzymes, predominantly CYP3A4, to form the active metabolite, meta-chlorophenylpiperazine (mCPP). This metabolite has weak serotoninergic activity and may contribute to the sedative effect. Metabolism proceeds through several steps, including hydroxylation and conjugation.

Excretion

The elimination half-life of trazodone is 5-9 hours for conventional tablets and up to 12 hours for prolonged-release forms. The drug is excreted mainly through the kidneys (about 75% in the form of metabolites) and through the intestine (about 20%). Complete excretion takes about 24-48 hours.

Indications for Use

Desirel is prescribed for the treatment of the following conditions:

• Depressive disorders of various etiologies with or without anxiety;
• insomnia associated with depression or chronic stress;
• Anxiety conditions, including generalized anxiety disorder;
• Complex therapy for chronic pain with a depressive component;
• Sleep disorders in patients with emotional instability.

The drug is effective for both short-term symptom relief and long-term treatment.

Contraindications

The use of Desirel is prohibited in:

• Hypersensitivity to trazodone or auxiliary components;
• Acute myocardial infarction;
• Severe hepatic insufficiency;
• A history of priapism (prolonged painful erection);
• Simultaneous intake of MAO inhibitors (a break of 14 days is required);
• Pregnancy and lactation;
• Children under 6 years of age.

Cautiously prescribe in epilepsy, glaucoma, hypotension or moderate renal insufficiency.

Method of Administration and Dosage

How to take

Desirel tablets are taken orally, drinking water (100-150 ml), preferably after meals to reduce gastric irritation and increase absorption. Capsules with prolonged release are taken whole, without chewing. The solution for injection is administered intramuscularly or intravenously only by medical personnel.

Dosages for adults and children

Adults

The initial dose is 50-100 mg before bedtime or 150 mg/day divided into 2-3 doses. After 1-2 weeks, the dose is increased to 150-300 mg/day. The maximum daily dose is 600 mg (in hospital).

Children from 6 to 18 years of age

Dosage - 0.5-2 mg/kg body weight per day, divided into 2 receptions, with a maximum of 150 mg/day.

Dose adjustment for certain conditions

In moderate renal or hepatic impairment, the initial dose is reduced to 25-50 mg/day with a gradual increase under medical supervision. In severe hepatic insufficiency the drug is contraindicated.

Side Effects

Possible adverse reactions include:

• Nervous system: drowsiness, dizziness, confusion, insomnia;
• Cardiovascular system: orthostatic hypotension, tachycardia;
• Gastrointestinal system: nausea, dry mouth, constipation;
• Genitourinary system: priapism (rare), decreased libido;
• Allergic reactions: rash, itching, swelling;
• Other: headache, sweating, tremor.

Effects usually diminish with adaptation to the drug.

Overdose

Symptoms of overdose

Doses above 600-1000 mg may cause drowsiness, hypotension, convulsions, arrhythmias, in severe cases - coma.

First aid measures

Stop taking, call an ambulance. Before the arrival of the doctor, wash the stomach and give activated charcoal.

Drug Interactions

Influence on the effect of other drugs

Desirel increases the effect of sedatives, antihistamines and alcohol. CYP3A4 inhibitors (ketoconazole) increase the concentration of trazodone, and inducers (carbamazepine) decrease its effectiveness.

Compatibility with alcohol and food

Alcohol increases sedation and hypotension. Food improves absorption and tolerability.

Special Precautions

Use in pregnancy and breastfeeding

Desirel is contraindicated in pregnancy and lactation because of the risk to the fetus and penetration into milk.

Effect on driving and driving mechanisms

The drug causes drowsiness and dizziness, so driving and working with machinery is prohibited.

Particularities of use in the elderly and children

In the elderly, the initial dose is 25-50 mg/day due to the risk of hypotension. In children, use with caution, starting with the lowest doses.