Asentra^® (Tablets) Instructions for Use

Marketing Authorization Holder

Krka d.d., Novo mesto (Slovenia)

ATC Code

N06AB06 (Sertraline)

Active Substance

Sertraline (Rec.INN registered by WHO)

Dosage Forms

	Asentra®	Film-coated tablets, 50 mg: 28 pcs.
		Film-coated tablets, 100 mg: 28 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white, round, biconvex, with a bevel, with a score on one side.

Excipients : calcium hydrogen phosphate dihydrate, microcrystalline cellulose, sodium carboxymethyl starch, hypromellose, talc, magnesium stearate.

Film coating composition Opadry 03H28758 white (hypromellose, titanium dioxide (E171), talc, propylene glycol).

7 pcs. – blisters (4) – cardboard packs.

Film-coated tablets white, round, slightly biconvex, with a bevel, with a score on one side.

Excipients : calcium hydrogen phosphate dihydrate, microcrystalline cellulose, sodium carboxymethyl starch, hypromellose, talc, magnesium stearate.

Film coating composition Opadry 03H28758 white (hypromellose, titanium dioxide (E171), talc, propylene glycol).

7 pcs. – blisters (4) – cardboard packs.

Clinical-Pharmacological Group

Antidepressant

Pharmacotherapeutic Group

Antidepressant

Pharmacological Action

Antidepressant, a naphthylamine derivative. Selective blocker of neuronal serotonin reuptake in the brain. It has practically no effect on neuronal norepinephrine and dopamine reuptake. Does not possess specific affinity for adreno- and m-cholinergic receptors, GABA receptors, dopamine, histamine, serotonin, or benzodiazepine receptors. Does not inhibit MAO. Causes anorexia, effective for obsessive-compulsive states.

Pharmacokinetics

When taken orally in doses of 50-200 mg once daily for 14 days, C_max in blood plasma is reached after 4.5-8.4 hours. The mean T_1/2 in young and elderly men and women is 22-36 hours. Corresponding to the half-life, approximately a twofold accumulation of the active substance is observed until steady state is reached after 1 week of treatment. Plasma protein binding is about 98%, V_d – 20 L/kg. It is extensively metabolized during the first pass through the liver. The main metabolite found in plasma is N-desmethylsertraline, which has weak pharmacological activity.

T_1/2 of N-desmethylsertraline varies within 62-104 hours. It is excreted mainly through the intestines and in urine in equal amounts as metabolites; less than 0.2% is excreted unchanged in the urine.

Indications

Treatment of depressive states of various origins in patients with mono- and bipolar affective disorders. Prevention of relapse of depressive episodes.

ICD codes

Dosage Regimen

Administer orally once daily, in the morning or evening, with or without food.

Initiate treatment for adults at a dose of 50 mg once daily.

If clinically indicated after one week, increase the dose in increments of 50 mg.

The maximum recommended daily dose is 200 mg.

For most patients, the therapeutic dose range is 50 mg to 100 mg daily.

When discontinuing treatment, gradually reduce the dose to minimize potential withdrawal symptoms.

In patients with hepatic impairment, use a lower initial dose or increase the dose more gradually.

No dosage adjustment is typically required for elderly patients or those with renal impairment.

The full antidepressant effect may take 2 to 4 weeks to develop.

For long-term treatment, use the lowest effective dose to maintain remission.

Adverse Reactions

From the nervous system dizziness, drowsiness, headache, insomnia, feeling of tiredness, weakness, tremor; rarely – manic or hypomanic state, anxiety, restlessness, visual disturbances.

From the cardiovascular system rarely – skin redness with a sensation of heat or warmth, palpitations.

From the digestive system: decreased appetite, diarrhea, dry mouth, nausea, stomach or intestinal cramps, flatulence; rarely – constipation, vomiting.

From metabolism increased sweating.

From the reproductive system rarely – decreased potency.

Allergic reactions: rarely – fever, skin rash, hives or itching.

Contraindications

Concomitant use with MAO inhibitors, hypersensitivity to sertraline.

Use in Pregnancy and Lactation

Adequate and well-controlled studies on the safety of sertraline during pregnancy have not been conducted, so use is possible only in cases where the expected benefit to the mother outweighs the potential risk to the fetus.

It is not known whether Sertraline is excreted in breast milk, so its use during lactation is not recommended. Individual studies have shown that in breastfed infants whose mothers received Sertraline during feeding, its level in blood plasma is insignificant or undetectable, while concentrations in breast milk exceed concentrations in maternal blood.

Women of childbearing age during treatment with sertraline should use reliable methods of contraception.

In experimental studies, no teratogenic or mutagenic effects of sertraline were identified. However, in doses approximately 2.5-10 times higher than the maximum daily clinical doses, Sertraline caused delayed ossification of fetal bone tissue, possibly as a result of an effect on the maternal organism. When sertraline was administered in doses approximately 5 times higher than the maximum clinical doses, a decrease in newborn survival was observed.

Use in Hepatic Impairment

Use with caution in cases of impaired liver function.

Use in Renal Impairment

Use with caution in cases of impaired renal function.

Pediatric Use

The safety of use in pediatrics has not been established.

Special Precautions

Use with caution in cases of a history of drug abuse or dependence, impaired liver function, impaired renal function, epileptic seizures, weight loss.

Should not be used in patients undergoing electroconvulsive therapy. Use of sertraline is possible no earlier than 14 days after discontinuation of MAO inhibitors.

Avoid alcohol consumption during treatment.

The safety of use in pediatrics has not been established.

Effect on ability to drive vehicles and operate machinery

During the treatment period, activities requiring increased attention and high speed of psychomotor reactions should be avoided.

Drug Interactions

When used concomitantly with coumarin derivative anticoagulants, prothrombin time is significantly increased.

When used concomitantly, Sertraline may displace other drugs from plasma protein binding, resulting in an increased plasma concentration of the corresponding active substance and an increased risk of adverse effects.

When used concomitantly with drugs whose metabolism involves the CYP2D6 isoenzyme, an increase in the plasma concentration of these drugs is possible due to inhibition of the CYP2D6 isoenzyme under the influence of sertraline.

When used concomitantly with MAO inhibitors (including selegiline, moclobemide), the development of serotonin syndrome (hyperthermia, muscle rigidity, myoclonus, as well as manifestations of instability of the mental and physiological state of the body, up to the development of delirium and coma) is possible.

When used concomitantly with lithium salts, tremor may be enhanced. When used concomitantly with desipramine, an increase in the plasma concentration of desipramine is possible; with cimetidine – a significant decrease in the clearance of sertraline.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.