Klopiksol

Клопиксол Drug photo

The description is actual on 18.11.2014

  • Latin name: Clopixol
  • ATH code: N05AF05
  • Active ingredient: Zuklopentiksol (Zuclopenthixol)
  • Producer: Lundbek X. A/S (Denmark)

Structure

Klopiksol contains a hydrochloride in quality of the operating component of a zuklopentiksol.

Additional components: potato starch, MKTs, glycerin, the hydrogenated castor oil, a gipromelloz, the titan dioxide, lactose, kopolividon, talc, magnesium stearate, a macrogoal, ferrous oxide red.

Klopiksol-Akufaz has as active agent of a zuklopentiksol acetate, and Klopiksol Depoa zuklopentiksola dekanoat. Additional components in these drugs – RM1137 argon and triglycerides of an average chain.

Release form

  • Klopiksol is on sale in the form of the tablets which are contained in plastic bottles.
  • Klopiksol Depo and Klopiksol-Akufaz are issued as solution for injections.

Pharmacological action

This medicine is a neuroleptic. It has the antipsychotic and braking effect.

Pharmacodynamics and pharmacokinetics

Drug in all forms blocks dopamine receptors in a brain. He is considered the effective proofreader of psychopatholike behavior. Increases the content of prolactin.

Active ingredient of medicine promotes the termination of nuclear symptoms of schizophrenia: hallucinations, the broken thinking, mania. Besides, it causes sedation and reduces manifestation of the accompanying symptoms: hostility, alarm, suspiciousness and aggression. Accustoming to nonspecific sedation quickly develops.

The maximum content of active ingredient of tablets in blood serum is observed 4 hours later. Medicine can be taken it is not dependent on food. Bioavailability about 44%. Extent of communication with proteins of plasma of about 99%. Semi-removal time – about 20 hours. It is brought out of an organism with a stake and urine.

Active agent in a quantity gets through a placental barrier. Its small amount is allocated in breast milk.

Equilibrium concentration is reached approximately 4 days later.

When using injections the expressed effect can be observed in 4 hours. A little bigger effect is swept up 1-3 days later after internal introduction. Then it decreases.

One prick of a zuklopentiksol of acetate promotes the expressed and fast decrease in manifestations of psychotic symptoms. Effect of medicine lasts 2-3 days. As a rule, 1-2 pricks that the necessary effect was reached are enough. Then it is possible to take the peroral or other deposited forms.

After an injection of a zuklopentiksol of acetate there comes tranzitorny dozozavisimy sedation. Usually it is done in an initial phase of psychosis as it calms the patient before establishment of antipsychotic effect. After internal introduction sedative action is shown quickly enough and becomes expressed 2 hours later. The maximum is reached in 8 hours. Then action begins to weaken even if there were repeated pricks.

After introduction of medicine of a zuklopentiksol acetate is split. Semi-removal time – about 32 hours. The maximum content in blood serum – 1-2 days later. Extent of communication with proteins of plasma high. In insignificant degree passes through a placental barrier. In a quantity it is allocated in breast milk. It is removed with a stake and urine.

Action Klopiksol Depo and Klopiksol-Akufaz longer in comparison with peroral forms.

Zuklopentiksola dekanoat renders the sedation depending on a dosage. But upon transition on Klopiksol Depo from injections of a zuklopentiksol of acetate or tablets of a zuklopentiksol the probability of sedation decreases. Accustoming develops quickly.

Zuklopentiksola dekanoat is split at hit in an organism. The maximum maintenance of medicine in blood serum is observed at the end of the first week. Semi-removal time – 3 weeks. Equilibrium concentration at repeated introduction is established for 3 months.

High extent of communication with proteins of plasma at introduction of medicine in the form of injections. In insignificant degree their active agents pass through a placental barrier. A small amount is allocated in breast milk. Are removed with a stake and urine.

Indications to use

Drug is appointed at chronic and acute forms of schizophrenia, and also the other psychotic frustration which are followed by hallucinations, disturbances in thinking, paranoia. Besides, it is appointed for disappearance of a condition of agitation, hostility, a maniacal phase of maniac-depressive psychosis, the increased concern, by aggressions, mental retardation in combination with psychomotor excitement and other frustration in behavior. Also drug is used at senile weak-mindedness, followed by paranoid ideas, behavior disorders, a disorientation, confusion of consciousness.

Klopiksol Depo provides continuous treatment. Its active ingredient interferes with emergence of recurrence which can arise because of interruption of reception of tablets.

Klopiksol-Akufaz is used for treatment of acute psychoses, chronic psychoses in the period of an aggravation and maniacal states.

Contraindications

This medicine is contraindicated at an acute drunkenness, and also acute intoxication opioid analgetics and barbiturates, a coma, hypersensitivity to drug components.

Besides, it is not desirable to appoint it at pregnancy and a lactation.

Side effects

At drug intake, as a rule, there can be following side effects:

  • Nervous system: dizziness, emergence of extrapyramidal disturbances (for their disappearance it is possible to lower a dose or to accept protivoparkinsonichesky drugs), drowsiness, accommodation disturbance, at prolonged treatment is possible dyskinesia, an akathisia, a hypokinesia, a hyperkinesia, a tremor, a hyper tone, a headache, disturbances of attention and gait, dystonia, paresthesias, amnesia, a syncope, alalias, spasms, a hyperreflexia, parkinsonism, an ataxy, a hypotone, migraine, a sleep disorder, an alarming state, pathological and dreadful dreams, a depression, nervousness, apathy, confusion of consciousness.
  • Alimentary system: dryness in an oral cavity, a lock, the raised salivation, vomiting, diarrhea, dyspepsia, pains in a stomach, a meteorism, nausea.
  • CCC: arterial hypotension, orthostatic hypotension, tachycardia.
  • Visual system: vision disorder, mydriasis.
  • Respiratory system: bunged-up nose, asthma.
  • Acoustic organs: hypersensitivity, a ring in ears.
  • Integuments: hyperhidrosis, skin itch, dermatitis, rash, photosensitivity, pigmentation disturbance, seborrhea, purpura.
  • Skeletal and muscular system: mialgiya, muscular rigidity, wryneck, lockjaw.
  • Exchange processes: the increased or reduced appetite, a set or a degrowth of a body.
  • Urinary system: ischuria, frustration of an urination, polyuria.
  • Liver and zhelchevyvodyashchy system: disturbance of functional tests.
  • Reproductive system: lack of an ejaculation, orgastichesky frustration (women), erectile dysfunction, decrease/strengthening of a libido, dryness of a vulvovaginal site.
  • General frustration: adynamy, indisposition, fatigue, pain, thirst, pyrexia, hypothermia.

In rare instances perhaps:

  • Alimentary system: passing change of hepatic tests.
  • CCC: a venous trobmoyembolizm, lengthening of an interval of QT on an ECG.
  • Hemopoietic and lymphatic system: thrombocytopenia, leukopenia, neutropenia, agranulocytosis.
  • Endocrine system: the increased prolactin level.
  • Exchange processes: a hyperglycemia, a lipidemia, problems with tolerance to glucose.
  • Immune system: hypersensitivity reactions, anaphylactic reactions.
  • Reproductive system and mammary glands: gynecomastia, amenorrhea, galactorrhoea, priapism.
  • Liver and zhelchevyvodyashchy system: cholestatic hepatitis, jaundice.
  • Nervous system: malignant antipsychotic syndrome.

Side effects, as a rule, depend on a dose. They can be more expressed in an initiation of treatment and gradually decrease.

Effects of use of medicine by pregnant women and during feeding by a breast are thoroughly not studied.

Unexpected interruption of a course of treatment can cause cancellation symptoms. As a rule, this dizziness, nausea, anorexia, a rhinorrhea, mialgiya, sleeplessness, a condition of excitement, vomiting, diarrhea, the increased perspiration, paresthesias, concern, a tremor, alarm, variable caumesthesias or cold weather.

These symptoms can be shown within 1-4 days after the termination of administration of drug and gradually decrease for 1-2 weeks.

Application instruction of Klopiksol (Way and dosage)

Tablets are applied orally in stages. The first doses at therapy by drug have to be small, then they gradually raise taking into account reaction of the patient to a course of treatment.

In case of a bad attack of the schizophrenia and other acute psychotic diseases, maniacal states expressed to agitation the application instruction of Klopiksol recommends a day dosage in 10-50 mg.

To patients with chronic schizophrenia and other chronic psychoses a dosage in days – 20-40 mg.

At senile frustration which are followed by agitation and confusion of consciousness medicine is taken in day on 2-6 mg if it is necessary, it is possible to increase a dose to 10-20 mg. At the same time it is desirable to take a pill in the evening.

In case of the moderated and expressed psychotic diseases an initial dosage – 20 mg a day. It is possible to raise it gradually each 2-3 days on 10-20 mg until the day dose reaches 75 mg.

At agitation in case of an oligophrenia a daily dosage – 6-20 mg. If there is a need, it is increased to 25-40 mg.

After use of injections Klopiksol-Akufaz appoint tablets Klopiksol 2-3 days later.

The instruction on Klopiksol Depo and Klopiksol-Akufaz reports about what their dosages select individually taking into account a condition of the patient. Injections are intramuscular. Drugs are entered into an upper outside quadrant of a buttock.

As a rule, appoint 1–3 ml Klopiksol-Akufaz. If more than 2 ml are entered, the dose is distributed on two times, prick to different places. If necessary the repeated injection in 2-3 days is given. In certain cases it is appointed in 1-2 days.

Zuklopentiksol acetate cannot be applied it is long. At most – 2 weeks. For all the time of treatment the dosage should not exceed 400 mg, and quantity of pricks – 4.

The maintenance therapy proceeds tablets or pricks Klopiksol Depo. Transition is carried out according to the following scheme:

  • On therapy by tablets with zuklopentiksoly: in 2-3 days after the last prick appoint a dose in 40 mg. It is recommended to divide it on several times. If it is necessary, it is possible to raise a dosage on 10-20 mg each 2-3 days to 75 mg.
  • On therapy Klopiksol Depo: after the last prick of a zuklopentiksol of acetate enters 1-2 ml of a zuklopentiksol of a dekanoat. Intramuscular injections of the last proceed each 2-4 weeks. If necessary it is possible to apply higher dosages or to do shorter intervals between pricks.

Besides, Klopiksol Depo and Klopiksol-Akufaz it is possible to mix in one syringe and to do as one injection. Then use of a zuklopentiksol of a dekanoat is established in an individual order.

For patients at advanced age of a dose can be reduced. The maximum one-time dosage should not be more than 100 mg.

Drug from a zuklopentiksol dekanoaty can provoke irritation in the place where it is entered. Pricks in a dosage more than 2 ml are divided in two steps.

Transition from a course of tablets to pricks Klopiksol Depo:

  • The usual day peroral dosage increased by 8 times is equal to one prick of a zuklopentiksol of a dekanoat each 2 weeks.
  • The usual day peroral dosage increased by 16 times is equal to one prick of a zuklopentiksol of a dekanoat each 4 weeks.

After the first prick a pill continues to be taken within a week, but in a smaller dosage.

To patients at advanced age appoint Klopiksol Depo in the minimum dose.

At problems with work of a liver appoint a half of a usual dosage of injections and control the maintenance of medicine in blood serum.

Overdose

Overdose manifestations by medicine in all forms: drowsiness, extrapyramidal frustration, arterial hypotension, hyperthermia, coma, spasms, depressed case, hypothermia.

As therapy the gastric lavage is appointed. Then symptomatic treatment. Carry out a maintenance therapy. It is impossible to apply adrenaline. It is possible to prevent spasms Diazepam use, and extrapyramidal symptoms Biperiden.

Overdose by drug in the form of injections is considered improbable. Changes in an ECG and QT prolongation are possible, it is also reported about arrhythmia like Torsade de Pointes, ventricular arrhythmia, a cardiac standstill.

Therapy in this case symptomatic and supporting. It is necessary to take measures for improvement of functions of respiratory system and CCC.

Interaction

This medicine can lead to increase of sedative action of the means oppressing a nervous system. It is impossible to appoint it together with Guanetidin and his analogs, and also with the drugs considerably extending QT interval. Reduction of efficiency of adrenergic drugs at simultaneous use is possible. The probability of emergence of extrapyramidal symptoms at a combination to Metoclopramidum and Piperazin increases.

Together with drugs of lithium the probability of a neurotoxicity increases.

Tricyclic antidepressants at a combination to neuroleptics mutually suppress biotransformation.

Use of drugs which suppress CYP2D6 enzyme slow down removal of a zuklopentiksol.

With care use this drug with means which influence electrolytic balance.

Terms of sale

Medicine is released according to the recipe of the doctor.

Storage conditions

It is necessary to hold drug in unavailable to small children the place. It is necessary to store tablets on 2 mg and solutions for pricks at a temperature up to 25 °C. Means in tablets on 10 and 25 mg needs to be held at a temperature up to 30 °C.

Period of validity

Klopiksol and Klopiksol-Akufaz it is necessary to store not longer than two years. A period of validity Klopiksol Depo – three years.

About Klopiksole

As a rule, patients leave About Klopiksole in the form of solution for injections. They note that the course of use of this drug is very convenient as injections are given seldom. It is much simpler, than to constantly take a pill.

Nevertheless, some advantages of this medicine note also in case of the tableted form. For example, the fact that at the same time it is not required to go to the doctor. The patient takes medicine independently therefore it is not necessary to agree on the plans with the schedule of injections.

Also About Klopiksol Depo and similar drug in the form of tablets note also some undesirable effects. As a rule, patients report about apathy and reduction of a libido. Extrapyramidal frustration are sometimes described.

However in efficiency of this means there are no doubts. The main thing to accept it strictly on doctor's orders. About any corrections of a dose and changes of a state it is necessary to address the specialist.

Klopiksol's price where to buy

The cost of this medicine depends on a release form. On average Klopiksol's price in tablets following:

  • tablets of 2 mg 50 pieces – 240 rubles;
  • tablets of 25 mg 100 pieces – 1550 rubles;
  • tablets of 10 mg 50 pieces – 460 rubles.

Cost Klopiksol-Akufaz – about 2100 rubles.

The price Klopiksol Depo on one ampoule in packaging – about 370 rubles, on 10 ampoules in packaging – 3200 rubles.

Zdravzona

  • Klopiksol of 2 mg No. 100 of a tablet p / about
  • Klopiksol of depot 200mgml solution for injections of 1 ml No. 10 of an ampoule
  • Klopiksol of 2 mg No. 50 of a tablet
  • Klopiksol-Akufaz 50mg/ml solution for injections of 1 ml No. 5 ampulylundbeck
  • Klopiksol of 25 mg No. 50 of a tablet

Drugstore of IFC

  • Klopiksol tbl p/pl/o 2 mg No. 50, Lundbeck N.Daniya
  • Klopiksol of depot solution for infection masl 200mg/ml 1 ml of amp No. 1, Lundbeck N.Daniya
  • Klopiksol tbl p/pl/o 25 mg No. 50, Lundbeck N.Daniya
  • Klopiksol of depot solution for infection masl 200mg/ml 1 ml of amp No. 10, Lundbeck N.Daniya
  • Klopiksol-Akufaz solution for infection masl 50mg/ml 1 ml of amp No. 5, Lundbeck N.Daniya
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Apteka24

  • Klopiksoln. Lundbeck (Denmark)
  • Klopiksol-depon. Lundbeck (Denmark)
  • Klopiksoln. Lundbeck (Denmark)
  • Klopiksol-akufazn. Lundbeck (Denmark)

Paniapteka

  • Klopiksol of depot solution masl. for infection. 200mg/ml No. 10lundbek
  • Klopiksol of depot solution masl. for infection. 200mg/ml No. 10lundbek
  • Klopiksol of depot solution masl. for infection. 200mg/ml No. 10lundbek
  • Klopiksol of depot solution masl. for infection. 200mg/ml No. 10lundbek
Section: For a nervous system
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