PRAM - instructions for use, dose, side effects, contraindications

Excipients: mannitol 66,275 / 132,55 / 265,1 mg, cellulose microcrystalline 8,9425 / 17,885 / 35,77 mg, silicon colloidal dioxide 0,3125 / 0,625 / 1,25 mg, magnesium stearate 1,975 / 3,95 / 7,9 mg;

shell: hypromellose 1,095 / 2,19 / 4,38 mg, titanium dioxide 0,44 / 0,88 / 1,76 mg, macrogol 6000 0,265 / 0,53 / 1,06 mg.

Description:

Round, biconvex tablets, covered with a film coating of white color; for dosages of 20 mg, 40 mg with a risk.

On the cross section, the core of the tablet is white or almost white in color.

Pharmacotherapeutic group:antidepressant

ATX: & nbsp

N.06.A.B.04 Citalopram

Pharmacodynamics:

Citalopram is an antidepressant from the group of selective serotonin reuptake inhibitors (SSRIs).

Citalopram, possessing a pronounced ability to inhibit the reuptake of serotonin, does not or has a very weak ability to bind to a variety of receptors, including histamine, muscarinic and adrenoreceptors. Citalopram only to a very small extent inhibits the isoenzyme CYP2D6 and, therefore, does not interact with drugs metabolized by this isoenzyme. Thus, side effects and toxic effects are manifested in significantly less than other drugs inhibiting the isoenzyme CYP2D6.

The antidepressant effect usually develops after 2-4 weeks of treatment.

Has no effect on body weight, hematological parameters, liver and kidney function, reproductive function, does not have a teratogenic effect.

Normalizes the emotional sphere, improves the pathologically changed mood, eliminates melancholy, melancholy.

Stimulates motor activity and accelerates the processes of thinking in depression.

Pharmacokinetics:

Bioavailability of citalopram with oral intake is about 80% and is practically independent of food intake. The maximum concentration in plasma is reached in 2-4 hours after administration. Binding to plasma proteins is below 80%. The plasma is present unchanged. At doses of 10-60 mg / day pharmacokinetic parameters have a linear dependence. The volume of distribution is 12 l / kg. The equilibrium concentration with a daily single dose is established after 7-14 days. Penetrates into breast milk.

Metabolized by demethylation, deamination and oxidation involving cytochrome P450 (isozymes CYP3A4 and CYP2C19) to form pharmacologically less active metabolites.

The half-life of citalopram is 1.5 days. Excretion is performed by the kidneys and with feces.

Patients over the age of 65 years

There is a longer biological half-life (1.5-3.75 days) and lower clearance values compared with patients younger than 65 years. Concentrations that were observed in the equilibrium state in elderly patients were almost twice as high as those observed in younger patients who received the same dose.

Lack of liver function

In patients with reduced liver function citalopram output more slowly. The biological half-life of citalopram is almost doubled and the equilibrium concentrations of citalopram in plasma are almost twice as high as in patients with normal liver function after administration of the same dose.

Lack of kidney function

The excretion of citalopram proceeds more slowly in patients with a small and moderate degree of renal dysfunction without a significant effect on the pharmacokinetics. At present, the experience of treating patients with severe renal function deficiency (creatinine clearance below 20 ml / mol) is insufficient.

Indications:

Treatment of depressive disorders and prevention of relapse.

Treatment of panic disorder with or without agoraphobia.

Treatment of obsessive-compulsive disorder (obsessive-compulsive disorder).

Contraindications:

Hypersensitivity to citalopram or to any component that is part of the drug.

Simultaneous use with sumatriptan and other serotonergic drugs.

Simultaneous use with pimozide.

Children's age (efficacy and safety of use not established).

The drug should not be used in combination with monoamine oxidase (MAO) inhibitors, and also within 14 days after discontinuation of their administration. Treatment with MAO inhibitors can be started no earlier than 7 days after stopping citalopram.

Carefully:

The drug should be used with caution in the presence of drug dependence (including in history), with insufficient liver and / or kidney function, with mania, hypomania, in the presence of convulsive disorders in the history, in the elderly, during pregnancy and lactation .

Pregnancy and lactation:

Do not assign citalopram pregnant and breastfeeding women, unless the potential clinical benefit prevails over theoretical risk.

Citalopram penetrates into breast milk. It should either stop breastfeeding, or stop using the drug during breastfeeding.

Dosing and Administration:

The drug is taken orally once a day at any time of the day, regardless of food intake.

Depression

The recommended daily dose is 20 mg of citalopram for once-daily administration. Depending on the patient's individual response to treatment and the severity of the disease, the dose can be increased to a maximum of 60 mg per day.

Panic disorders

It is recommended that 10 mg of citalopram be used once a day during the first week of treatment, after which the dose is increased to 20 mg per day. Depending on the patient's individual response to treatment and the severity of the disease, the dose can be increased to a maximum of 60 mg per day.

Obsessive-compulsive disorder

The recommended daily dose is 20 mg of citalopram for once-daily administration. Depending on the patient's individual response to treatment, the dose can be increased by 20 mg to a maximum of 60 mg per day.

Patients aged 65 years and over

The recommended initial dose can be increased to 40 mg per day.

Lack of kidney function

Patients with mildly or moderately impaired renal function may apply the drug in normal doses. Information on citalopram treatment in patients with severe renal insufficiency (creatinine clearance up to 20 ml / min) is not available.

Lack of liver function

Patients with impaired liver function should not be administered more than 30 mg per day.

Duration of treatment

Usually, the antidepressant effect of the drug is observed after 2-4 weeks of treatment.Treatment with antidepressants is symptomatic and should be carried out for a long time. Usually, to prevent recurrence, treatment should be carried out for 6 months or even a longer period of time. In the case of patients with recurrent depression, maintenance treatment should be carried out for several years to prevent the onset of subsequent phases of the disease. If the treatment is completed, the drug should be withdrawn gradually within a few weeks.

In the treatment of panic disorder, the maximum effect of citalopram is observed after 3 months of treatment. This effect persists throughout the period of maintenance therapy.

In the treatment of obsessive-compulsive disorder, the effect of the drug appears after 2-4 weeks of treatment; With further continuation of treatment, further improvement can be observed.

Side effects:

Co hand nervous system: dizziness, headache, tremor, drowsiness, insomnia, agitation, nervousness, migraine, paresthesia; sleep disturbance, impaired concentration, amnesia, anxiety, decreased libido,increased appetite, anorexia, apathy, suicidal attempts, confusion of thoughts, asthenia, mood changes, aggressive behavior, emotional lability, agitation, mania, hypomania, panic behavior, paranoid reaction, psychosis, excessive fatigue, anxiety, extrapyramidal disorders, convulsions, euphoria, serotonin syndrome (agitation, confusion, diarrhea, hyperthermia, hyperreflexia, ataxia, increased sweating, uncontrolled behavior), hallucinations, depersonalization.

From the cardiovascular system: atrial flutter (heart rhythm disturbance), tachycardia, bradycardia, orthostatic hypotension, increase or decrease in blood pressure, supraventricular and ventricular arrhythmias.

From the gastrointestinal tract: nausea, dry mouth, constipation, diarrhea, indigestion, vomiting, abdominal pain, flatulence, anorexia, increased salivation, an increase in the activity of liver enzymes.

From the side of the urinary system: frequent urination, polyuria.

Metabolic disorders: decrease or increase in body weight.

From the respiratory system: rhinitis, sinusitis, cough, shortness of breath.

From the side reproductive system: ejaculation disorders, increased or decreased libido, female anorgasmia, dysmenorrhea, impotence, menstrual irregularities, galactorrhea.

Co hand leather: increased sweating, rash, itching, photosensitivity, epidermal necrolysis, angioedema.

From the side of the organ of vision: violation of accommodation, impaired vision, mydriasis.

From the sense organs: a taste disorder.

From the side of the auditory and vestibular apparatus: noise in ears.

From the side of the musculoskeletal system: myalgia, arthralgia.

On the part of the organs of hematopoiesis: it is rarely possible to develop bleeding (eg, bleeding due to gynecological causes, gastrointestinal bleeding, ecchymosis), thrombocytopenia.

Other: asthenia, fatigue, allergic reactions, fainting, malaise, hyperthermia, mastodonia, yawning, gnashing of teeth, hyponatremia, anaphylactoid reaction.

Overdose:

Symptoms: dizziness, tremor, agitation, increased sweating, drowsiness, depression of consciousness of varying severity, convulsions, sinus tachycardia,changes in the ECG (ST segment and T wave changes, QRS extension, QT interval prolongation), arrhythmia, ventricular arrhythmia, cyanosis, respiratory depression, vomiting, rhabdomyolysis, metabolic acidosis, hypokalemia, very rarely acute renal failure.

Treatment: symptomatic and supportive - gastric lavage, adequate oxygenation. Monitoring the function of the cardiovascular and respiratory systems.

There is no specific antidote.

Interaction:

MAO inhibitors

In patients taking SSRIs with MAO inhibitors, or in patients who start taking MAO inhibitors immediately after SSRI therapy, serious adverse reactions may occur.

The drug should not be used simultaneously with MAO inhibitors.

Treatment with citalopram should be started 14 days after discontinuation of MAO inhibitors. Treatment with citalopram should be discontinued 7 days before treatment with MAO inhibitors.

Serotonergic drugs

Simultaneous use with serotonergic drugs (eg with tramodol, sumatriptan, etc.) can lead to the development of serotonin syndrome.

Drugs that reduce the threshold of convulsive readiness

The drug can reduce the threshold of convulsive readiness. Therefore, care should be taken when using other medications that reduce the threshold of convulsive readiness (antidepressants (tricyclics and SSRIs), neuroleptics (phenothiazines, thioxanthenes, butyrophenones), mefloquine, bupropion and tramadol).

Lithium, tryptophan

The drug enhances the pharmacological effects of tryptophan (amplification serotonergic effect) and toxic effects of lithium preparations.

Hypericum perforatum (Hypericum perforatum)

The simultaneous use of SSRIs and preparations containing St. John's Wort, can lead to an increase in the number of side effects.

Anticoagulants and other drugs that affect blood coagulability

Violation of blood clotting can occur with the simultaneous use of citalopram with oral anticoagulants and other drugs that affect blood clotting (for example, atypical antipsychotics and phenothiazines, most tricyclic antidepressants, acetylsalicylic acid and non-steroidal anti-inflammatory drugs (NSAIDs),ticlopidine and dipyridamole). In such cases, control of blood clotting parameters is necessary.

Ethanol

The drug does not enter with pharmacodynamic or pharmacokinetic interaction with ethanol. However, as in the case of other psychotropic drugs, simultaneous use of citalopram and ethanol is not recommended.

Digoxin

In persons who received citalopram for 3 weeks, a single dose of digoxin (1 mg) did not significantly affect the pharmacokinetics of both citalopram and digoxin.

Theophylline

Simultaneous use of citalopram for 3 weeks and theophylline (single dose 300 mg) did not significantly affect the pharmacokinetics of theophylline.

The effect of other drugs on the pharmacokinetics of citalopram

Caution should be exercised when used simultaneously with inhibitors of the isoenzyme CYP2C19 (omeprazole, esomeprazole, fluvoxamine, lansoprazole, tikpopidine) or with cimetidine. Also, caution should be given to high doses of the drug at the same time with high doses of cimetidine. It may be necessary to reduce the dose of the drug depending on adverse reactions.

Effect of citalopram on the pharmacokinetics of other drugs

To an insignificant degree inhibits the isoenzyme CYP2D6, in connection with which it practically does not interact with drugs, however caution should be exercised while using the drug and drugs metabolized by isoenzyme CYP2D6 and have a small therapeutic index, for example, flecainide, propafenone and metoprolol (in cases of heart failure) or drugs, mainly metabolized by the isoenzyme CYP2D6 and acting on the central nervous system, for example, antidepressants - desipramine, clomipramine, nortriptyline, or antipsychotic funds - risperidone, thioridazine, haloperidol. In these cases, a dose adjustment may be required.

Special instructions:

The use of antidepressants, incl. citalopram, especially in children, adolescents and young people under the age of 24, can lead to increased suicidal behavior. For this reason, especially at the beginning of the course of treatment and during the first months of treatment, with a change in the doses of the drug, both upwards,and in the direction of diminishing or abolishing the drug, patients should be carefully monitored for the detection of suicidal behavior or other changes, such as agitation and / or irritability.

Paradoxical anxiety

In some patients with panic disorders, anxiety may occur at the onset of antidepressant treatment. In most of cases, these paradoxical reactions take place within 2 weeks after initiation of therapy. To reduce the likelihood of an anxiogenic effect, it is recommended to use low initial doses.

Convulsions

In the case of convulsive seizures, the drug should be immediately withdrawn. SSRIs should not be administered to patients with uncontrolled epilepsy; with controlled seizures careful monitoring is necessary. With an increase in the frequency of convulsive seizures of SSRIs, including citalopram, should be canceled.

Mania and Hypomania

SSRIs should be used with caution in patients with manic disorders in history. With the development of the manic state citalopram should be canceled.

Diabetes

In patients with diabetes mellitus, the treatment of SSRIs can alter the glucose level in the blood. Therefore, it may be necessary to adjust the dosages of insulin and / or oral hypoglycemic drugs.

Hyponatremia

When SSRIs were used, there were cases of development of hyponatremia, which is probably associated with a violation of the secretion of antidiuretic hormone. Therefore, SSRIs should be used with caution in patients at risk of developing hyponatremia: elderly, with cirrhosis of the liver and taking drugs that can cause hyponatraemia.

Pathological bleeding

With the use of SSRIs, a case of development of cutaneous hemorrhages was observed: ecchymosis and purpura. It is necessary to use SSRIs with caution in patients with a tendency to bleeding, and also taking oral anticoagulants and drugs that affect blood clotting (for example, atypical antipsychotics and phenothiazine, most tricyclic antidepressants, acetylsalicylic acid and NSAIDs).

Electroconvulsive therapy

Since the clinical experience of the simultaneous use of SSRIs and electroconvulsive therapy is limited, caution should be exercised in such cases.

Reversible selective inhibitors of MAO type A

Combine citalopram and MAO type A inhibitors are not recommended because of the risk of developing a serotonin syndrome. See section "Interaction with other drugs".

Serotonin syndrome

Caution should be exercised while using citalopram and serotonergic drugs, such as sumatriptan, other substances of the triptane group, tramadol, tryptophan. However, the development of serotonin syndrome in patients receiving both serotonergic drugs and SSRIs was extremely rare. The development of this syndrome may indicate such signs as agitation, tremor, myoclonus, hyperthermia. In this case, simultaneous reception of SSRIs and serotonergic drugs should be stopped immediately and symptomatic therapy should be started.

Malignant neuroleptic syndrome

At simultaneous, application atypical antipsychotics and antidepressants of group SIOZS, incl. citalopram, the risk is increased development of malignant neuroleptic syndrome.

Effect on the ability to drive transp. cf. and fur:

Although citalopram does not affect the psychomotor activity, during the period of treatment, care must be taken when driving vehicles and engaging in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated, 10 mg, 20 mg and 40 mg.

Packaging:

For 10 tablets in PVC / PVDC / Al blister.

1 blister with instructions for use in a cardboard box.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

4 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LS-001780

Date of registration:29.07.2011

The owner of the registration certificate:Lannacher Heilmittel GmbHLannacher Heilmittel GmbH Austria

Manufacturer: & nbsp

LANNACHER HEILMITTEL, GmbH Austria

Representation: & nbspLANNACHER HILMITTEL GmbHLANNACHER HILMITTEL GmbHAustria

Information update date: & nbsp27.09.2015

Illustrated instructions

Instructions

PRAM® (Pram®)