Aktaparoxetine - instructions for use, doses, side effects, contraindications

Excipients: magnesium stearate 2255 4.5 mg, sodium carboxymethyl starch 6 mg, mannitol DC 133.64 mg, cellulose microcrystalline 133,64 mg; methyl methacrylate dimethylaminoethyl methacrylate and butyl methacrylate copolymer (Eudragit E 100) 1.8 mg; Dropped AMB white (water solution); polyvinyl alcohol partially hydrolyzed 5.46 mg, titanium dioxide (E 171) 3.84 mg, talc 2.4 mg; lecithin soy (E 322) 0.24 mg, xanthan gum (E 415) 0.06 mg;

1 tablet, coated, 30 mg contains:

active substance: paroxetine hydrochloride 33,33 mg corresponding to 30,00 mg of paroxetine;

Excipients: Magnesium stearate 2255 6.75 mg, sodium carboxymethyl starch 9 mg, mannitol DC 200.46 mg, cellulose microcrystalline 200.46 mg; methyl methacrylate, dimethylaminoethyl methacrylate and butyl methacrylate copolymer (Eudragit E 100) 2.7 mg; Opadry AMW blue (water solution): polyvinyl alcohol partially hydrolyzed 8.19 mg, titanium dioxide (E 171) 4.93 mg, talc 3.6 mg, indigocarmine (E 132) 0.83 mg, soy lecithin (E 322) 0.36 mg, xanthan gum (E 415) 0.086 mg; dye sunset yellow (E 110) 0.002 mg, dye quinoline yellow (E 104) 0.002 mg.

Description:

Producer of JSC "Aktavis", Iceland.

Tablets 20 mg: round biconvex tablets, covered film shell of white or almost white color with a risk on one side and the inscription "P20" on the other hand.

Tablets 30 mg: round biconvex tablets, covered film shell of blue color with a risk on one side and an inscription "P30" on the other hand.

Manufacturer "Aktavis Ltd.", Malta.

Tablets 20 mg: round biconvex tablets,Covered with a film shell of white or almost white color with a risk on both sides and lateral risks, the inscription "Р", with one side and the inscription "20" with the other side.

Tablets 30 mg: round biconvex tablets, covered with a film shell of blue color with a risk on one side and the inscription "P30" on the other hand.

Pharmacotherapeutic group:Antidepressant

ATX: & nbsp

N.06.A.B Selective serotonin reuptake inhibitors

N.06.A.B.05 Paroxetine

Pharmacodynamics:

Paroxetine is a potent and selective inhibitor of the capture of 5-hydroxytryptamine (5-HT, serotonin) by neurons of the brain, which determines its antidepressant effect and effectiveness in the treatment of obsessive-compulsive (OCD) and panic disorder.

The main metabolites of paroxetine are polar and conjugated products of oxidation and methylation, which are rapidly excreted from the body, have weak pharmacological activity and do not affect its therapeutic effect. In the metabolism of paroxetine, the selective uptake of 5-HT neurons due to its action is not impaired.

Paroxetine has a low affinity for muscariniccholinergic receptors. Having selective action, in contrast to tricyclic antidepressants, paroxetine showed a low affinity for α-1, α-2, β-adrenoreceptors, as well as for dopamine, 5-HT) -like, 5-HTr-like and histamine (Hi) receptors. Paroxetine does not violate psychomotor functions and does not potentiate the inhibitory effect of ethanol on them.

According to the behavioral and EEG studies, paroxetine reveals weak activating properties when it is administered at doses higher than those required to inhibit 5-HT capture. In healthy volunteers, it does not cause a significant change in blood pressure, heart rate and EEG.

In contrast to antidepressants, which inhibit the seizure of norepinephrine, paroxetine much weaker suppresses the antihypertensive effects of guanitidine.

Pharmacokinetics:

Paroxetine is well absorbed after ingestion and is metabolized first pass through the liver. The excretion of unchanged paroxetine in the urine is usually less than 2% of the dose, with metabolites accounting for about 64% of the dose. The intestine excretes about 36% through bile, in which the unchanged paroxetine is less than 1% of the dose. In this way, paroxetine is excreted mainly as a result of metabolism.

Excretion of metabolites of paroxetine from the body is biphasic, first as a result of the metabolism of the first passage through the liver, and then it is controlled by systemic elimination. The half-life period varies, but usually is about one day. Stable systemic levels are reached by 7-14 days after the start of treatment, and pharmacokinetics during prolonged treatment does not change. The clinical effects of paroxetine (side effect and efficacy) do not correlate with its concentration in the plasma.

Since the metabolism of paroxetine involves the stage of the first passage through the liver, its quantity, determined in the systemic circulation, is less than that absorbed from the gastrointestinal tract. With an increase in the dose of paroxetine or with multiple dosing, when the load on the body increases, a partial absorption of the effect of the first passage through the liver and a decrease in the plasma clearance of paroxetine occur. As a result, an increase in paroxetine concentration in the plasma and fluctuations in the pharmacokinetic parameters are possible, which can be observed only in those patients,which, when taking low doses, reach low levels of the drug in plasma.

Paroxetine is extensively distributed in tissues, and pharmacokinetic calculations show that only 1% of it is present in the plasma, and at therapeutic concentrations 95% is associated with plasma proteins.

In elderly patients, as well as those who suffer from severe renal and hepatic insufficiency, the concentration of paroxetine in plasma is increased, and the range of plasma concentrations in them almost coincides with the range of healthy adult volunteers.

Indications:

- Depression of all types, including reactive, severe endogenous depression and depression, accompanied by anxiety;

- obsessive-compulsive disorder (OCD);

- panic disorder, including agoraphobia;

- social anxiety disorder / social phobia;

- generalized anxiety disorder;

treatment of post-traumatic stress disorder

Contraindications:

- Hypersensitivity to the components of the drug;

- simultaneous reception with MAO inhibitors and within 14 days after their cancellation;

- simultaneous reception of thioridazine;

- unstable epilepsy;

- pregnancy and lactation;

- children's age (under 18 years).

Carefully:

Liver failure; kidney failure; angle-closure glaucoma; hyperplasia of the prostate; mania; pathology of the heart; epilepsy; convulsive conditions; the appointment of electropulse therapy; taking drugs that increase the risk of bleeding; presence of risk factors for increased bleeding and diseases that increase the risk of bleeding, elderly age.

Pregnancy and lactation:Contraindicated.

Dosing and Administration:

Inside, 1 time per day, in the morning, while eating. The tablet is swallowed whole, washed down with water. The dose is selected individually during the first two to three weeks after the start of therapy and is subsequently adjusted if necessary.

With depression - 20 mg once a day. If necessary, the dose is gradually increased by 10 mg / day, the maximum daily dose should not exceed 50 mg.

In obsessive-compulsive disorders the initial therapeutic dose is 20 mg / day followed by a weekly increase of 10 mg. The recommended average therapeutic dose is 40 mg / day, if necessary, the dose may be increased to 60 mg / day.

In panic disorders the initial dose is 10 mg / day (to reduce the possible risk of developing panic symptoms), followed by a weekly increase of 10 mg. The average therapeutic dose is 40 mg / day. The maximum dose is 50 mg / day.

Socially-disturbing disorders / social phobia: the initial dose is 20 mg per day, in the absence of effect for at least two weeks, an increase in the dose to a maximum of 50 mg per day is possible. The dose should be increased by 10 mg at intervals of at least a week in accordance with the clinical effect.

Post-traumatic disorders of the psyche: for the majority of patients, the initial and therapeutic doses are 20 mg per day. In some cases, an increase in the dose of paroxetine to a maximum of 50 mg per day is recommended. The dose should be increased by 10 mg every week in accordance with the clinical effect.

Generalized anxiety disorders: the initial and recommended dose is 20 mg per day.

With renal and / or liver failure the recommended dose is 20 mg per day.

For elderly patients daily dose should not exceed 40 mg.

In order to prevent the development of withdrawal syndrome, the discontinuation of taking the drug is carried out gradually.

Side effects:

From the nervous system: drowsiness, tremor, asthenia, insomnia, dizziness, fatigue, seizures, extrapyramidal disorders, serotonin syndrome, hallucinations, mania, confusion, agitation, anxiety, depersonalization, panic attacks, increased nervous excitability, paresthesia, decreased ability to concentrate.

From the side of the musculoskeletal system: arthralgia, myalgia, myasthenia gravis, myoclonia, myopathic syndrome.

From the sense organs: visual impairment, taste change.

From the genitourinary system: violations of sexual function, including impotence and ejaculation disorders, urinary retention, hyperprolactinaemia / galactorrhea, anorgasmia, increased frequency of urination.

From the digestive system: decreased appetite, nausea, vomiting, dry mouth, constipation or diarrhea, in very rare cases - hepatitis.

From the side of the cardiovascular system: Orthostatic hypotension.

Other: increased sweating, allergic reactions (rash, urticaria, ecchymatosis, pruritus, angioedema), hyponatremia, violation of the secretion of antidiuretic hormone, withdrawal syndrome with abrupt withdrawal of the drug, rhinitis.

Overdose:

Symptoms: nausea, dilated pupils, fever, increased blood pressure, headache, involuntary muscular contractions, agitation, anxiety, sinus tachycardia, bradycardia, nodal rhythm.

In very rare cases, with simultaneous administration with other psychotropic drugs and / or alcohol, depression of consciousness is possible up to coma.

Treatment: gastric lavage, Activated carbon. If necessary, symptomatic therapy. There is no specific antidote.

Interaction:

The intake of food and antacid agents does not affect the absorption and pharmacokinetic parameters of the drug.

Paroxetine is incompatible with MAO inhibitors.

With simultaneous administration with paroxetine, the concentration of procyclidine increases.

During therapy with paroxetine, one should refrain from taking alcohol because of the increased toxic effect of alcohol.

In connection with paroxetine inhibition of cytochrome P450, the effect of barbiturates, phenytoin, indirect anticoagulants, tricyclic antidepressants, phenothiazine antipsychotics and antiarrhythmics of the class 1C, metoprolol and an increased risk of side effects with the simultaneous administration of these drugs.

At simultaneous appointment with the preparations, inhibiting enzymes of a liver, the dose of paroxetine can be required.

Paroxetine increases bleeding time against the background of taking warfarin, with the same prothrombin time.

With the simultaneous administration of paroxetine with. atypical antipsychotic agents, phenothiazines, tricyclic antidepressants, acetylsalicylic acid, non-steroidal anti-inflammatory agents, caution should be taken in connection with possible bleeding disorders.

Simultaneous administration with serotonergic agents (tramadol, sumatriptan) can lead to an increase in the serotonergic effect.

Mutual enhancement of the action of tryptophan, lithium and paroxetine preparations was noted.

With the simultaneous administration of paroxetine with phenytoin and other anticonvulsants, a decrease in paroxetine concentration in the plasma and an increase in the incidence of side effects are possible.

Special instructions:

To avoid the development of malignant neuroleptic syndrome with caution appoint patients receiving neuroleptics.

Paroxetine does not impair cognitive and psychomotor functions, however, as with other psychotropic medications, patients should be careful when driving and moving machinery.

Treatment with paroxetine is prescribed 2 weeks after the abolition of MAO inhibitors.

In elderly patients, hyponatremia is possible.

In some cases requires dose adjustment insulin and / or oral hypoglycemic drugs.

With the development of seizures, paroxetine treatment is discontinued.

At the first sign of mania, therapy with paroxetine should be discontinued.

During the first few weeks, the patient's condition should be carefully monitored in connection with possible suicidal attempts.

Effect on the ability to drive transp. cf. and fur:During the treatment period, one should refrain from using ethanol and from practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated 20 mg and 30 mg.

Packaging:

Tablets 20 mg: by 6, 7 or 10 tablets in blisters Aluminum Foil / PVC / Aluminum foil. 1 or 2 blisters for 6 tablets, 1, 2, 4, 8 or 14 Blisters for 7 tablets or 1, 2, 3, 5, 6 or 10 blisters of 10 tablets together with instructions for use in a cardboard box.

Tablets 30 mg: by 6, 7 or 10 tablets in blisters Aluminum foil / PVC / Aluminum foil. 1 blister for 6 tablets, 2 or 4 blisters for 7 tablets or 1, 3 or 10 blisters for 10 tablets together with instructions for use in a cardboard box.

For 20, 40, 60, 100 blisters, along with instructions for use in a cardboard box (for hospitals).

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children!

Shelf life:3 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-002868/08

Date of registration:18.04.2008

Expiration Date:Unlimited

The owner of the registration certificate:AKTAVIS GROUP, AO AKTAVIS GROUP, AO Iceland

Manufacturer: & nbsp

ACTAVIS, Ltd. Iceland

ACTAVIS hf. Iceland

Representation: & nbspACTAVIS GROUP AO ACTAVIS GROUP AO Iceland

Information update date: & nbsp04.07.2017

Illustrated instructions

Instructions

Aktaparoxetine (Actaparoxetin)