Prozac^® (Capsules) Instructions for Use

Marketing Authorization Holder

Swix Healthcare LLC (Russia)

Manufactured By

Patheon France (France)

ATC Code

N06AB03 (Fluoxetine)

Active Substance

Fluoxetine (Rec.INN WHO registered)

Dosage Form

Prozac®

Capsules 20 mg: 14 or 28 pcs.

Dosage Form, Packaging, and Composition

Capsules hard gelatin, size No. 3, opaque, with a green cap and a yellow body; the capsules are marked with the identification code “LILLY 3105”; the capsule contents are a white powder.

Excipients: starch (bulk powder), dimethicone.

Composition of the capsule cap patent blue V (E131), yellow iron oxide (E172), titanium dioxide (E171), gelatin, pharmaceutical food ink.
Composition of the capsule body yellow iron oxide (E172), titanium dioxide (E171), gelatin, pharmaceutical food ink.

14 pcs. – blisters (1) – cardboard packs.
14 pcs. – blisters (2) – cardboard packs.

Cardboard packs may have a sticker/stickers (first opening control).

Clinical-Pharmacological Group

Antidepressant

Pharmacotherapeutic Group

Selective serotonin reuptake inhibitors

Pharmacological Action

Antidepressant, a propylamine derivative. The mechanism of action is associated with the selective blockade of neuronal serotonin reuptake in the CNS. Fluoxetine is a weak antagonist of cholinergic, adrenergic, and histamine receptors. Unlike most antidepressants, fluoxetine apparently does not cause a reduction in the functional activity of postsynaptic beta-adrenergic receptors. It helps improve mood, reduces feelings of fear and tension, and eliminates dysphoria. It does not cause a sedative effect. When taken in average therapeutic doses, it has virtually no effect on the functions of the cardiovascular and other systems.

Pharmacokinetics

Absorbed from the gastrointestinal tract. Weakly metabolized during the first pass through the liver. Food intake does not affect the extent of absorption, although it may slow its rate. C_max in plasma is reached after 6-8 hours. Steady-state concentration in plasma is achieved only after continuous administration for several weeks. Protein binding is 94.5%. Easily penetrates the blood-brain barrier. Metabolized in the liver by demethylation to form the main active metabolite, norfluoxetine.

T_1/2 of fluoxetine is 2-3 days, of norfluoxetine – 7-9 days. Excreted by the kidneys 80% and through the intestine – about 15%.

Indications

Depressions of various origins, obsessive-compulsive disorders, bulimic neurosis.

ICD codes

Dosage Regimen

Initiate treatment at 20 mg once daily, administered in the morning.

For insufficient clinical response after 3-4 weeks, consider a dose increase.

Divide the total daily dosage into two or three administrations when using higher doses.

The maximum recommended daily dose for adult patients is 80 mg.

Adjust the dosage for elderly patients and those with hepatic or renal impairment; initiate at the lower end of the dosing range.

In patients with compromised renal function, use with particular caution; it is contraindicated in severe impairment.

For bulimia nervosa, administer 60 mg once daily; this higher dose may also be used for obsessive-compulsive disorder.

Swallow the capsule whole; do not chew or crush.

Take with or without food; food may delay absorption without affecting overall bioavailability.

Adhere strictly to the prescribed regimen; do not discontinue abruptly.

Adverse Reactions

From the central nervous system anxiety, tremor, nervousness, drowsiness, headache, sleep disturbances are possible.

From the digestive system diarrhea, nausea are possible.

From the metabolism increased sweating, hypoglycemia, hyponatremia (especially in elderly patients and with hypovolemia) are possible.

From the reproductive system decreased libido.

Allergic reactions skin rash, itching are possible.

Other joint and muscle pain, difficulty breathing, increased body temperature.

Contraindications

Glaucoma, bladder atony, severe renal impairment, benign prostatic hyperplasia, concurrent use of MAO inhibitors, convulsive syndrome of various origins, epilepsy, pregnancy, lactation, hypersensitivity to fluoxetine.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and lactation.

Use in Hepatic Impairment

Use with particular caution in patients with impaired liver function.

Use in Renal Impairment

Contraindicated in severe renal impairment. Use with particular caution in patients with moderate and mild renal impairment.

Pediatric Use

The safety of fluoxetine use in children has not been established.

Geriatric Use

Dosage adjustment is required for elderly patients.

Special Precautions

Use with particular caution in patients with impaired liver and kidney function, with a history of epileptic seizures, cardiovascular diseases.

In patients with diabetes mellitus, changes in blood glucose levels are possible, which requires adjustment of the dosage regimen of hypoglycemic drugs. When used in debilitated patients, the likelihood of epileptic seizures increases when taking fluoxetine.

With the simultaneous use of fluoxetine and electroconvulsive therapy, prolonged epileptic seizures may develop.

Fluoxetine can be used no earlier than 14 days after discontinuation of MAO inhibitors. The period after discontinuation of fluoxetine before starting therapy with MAO inhibitors should be at least 5 weeks.

Dosage adjustment is required for elderly patients.

The safety of fluoxetine use in children has not been established.

Do not consume alcohol during treatment.

Effect on ability to drive vehicles and operate machinery

During the treatment period, one should refrain from potentially hazardous activities that require increased attention and rapid psychomotor reactions.

Drug Interactions

With simultaneous use with drugs that have a depressant effect on the central nervous system, with ethanol, a significant enhancement of the depressant effect on the central nervous system, as well as an increase in the likelihood of seizures, is possible.

With simultaneous use with MAO inhibitors, furazolidone, procarbazine, tryptophan, the development of serotonin syndrome (confusion, hypomanic state, motor restlessness, agitation, convulsions, dysarthria, hypertensive crisis, chills, tremor, nausea, vomiting, diarrhea) is possible.

With simultaneous use, fluoxetine inhibits the metabolism of tricyclic and tetracyclic antidepressants, trazodone, carbamazepine, diazepam, metoprolol, terfenadine, phenytoin, which leads to an increase in their serum concentration and an enhancement of their therapeutic and side effects.

With simultaneous use, inhibition of the biotransformation of drugs metabolized with the participation of the CYP2D6 isoenzyme is possible.

With simultaneous use with hypoglycemic agents, an enhancement of their effect is possible.

There are reports of enhanced effects of warfarin with its simultaneous use with fluoxetine.

With simultaneous use with haloperidol, fluphenazine, maprotiline, metoclopramide, perphenazine, periciazine, pimozide, risperidone, sulpiride, trifluoperazine, cases of extrapyramidal symptoms and dystonia have been described; with dextromethorphan – a case of hallucinations has been described; with digoxin – a case of increased digoxin concentration in blood plasma.

With simultaneous use with lithium salts, an increase or decrease in the concentration of lithium in blood plasma is possible.

With simultaneous use, an increase in the concentration of imipramine or desipramine in blood plasma by 2-10 times is possible (may persist for 3 weeks after discontinuation of fluoxetine).

With simultaneous use with propofol, a case was described in which spontaneous movements were observed; with phenylpropanolamine – a case was described in which dizziness, weight loss, hyperactivity were observed.

With simultaneous use, an enhancement of the effects of flecainide, mexiletine, propafenone, thioridazine, zuclopenthixol is possible.

Storage Conditions

Store at 2°C (36°F) to 30°C (86°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.