Description overdue on 11/18/2014
- Latin name: Clopixol
- ATC code: N05AF05
- Active substance: Zuclopenthixol (Zuclopenthixol)
- Manufacturer: H. Lundbeck A / S (Denmark)
- Composition
- Product form
- Pharmacological action
- Pharmacodynamics and pharmacokinetics
- Indications
- Contraindications
- Side effects
- Instructions for use klopiksol (method and dosage)
- Overdose
- Cooperation
- Terms of sale
- Storage conditions
- Shelf life
- Reviews
- Price, where to buy
Composition
Klopiksol It contains as active component zuclopenthixol hydrochloride .
Additional ingredients: potato starch, MCC, glycerol , Hydrogenated castor oil, hypromellose, titanium dioxide, lactose, kopolividon, talc, magnesium stearate, macrogol, iron oxide red.
Klopiksol-akufaz It is as active substance zuclopenthixol acetate , a Klopiksol Depot - zuclopenthixol decanoate . Additional components in these drugs - Argon RM1137 and medium-chain triglycerides .
Product form
- Klopiksol sold in the form of tablets contained in plastic bottles.
- Klopiksol Depot and Klopiksol-akufaz available as a solution for injection.
Pharmacological action
This drug is neuroleptic . It has antipsychotic and inhibitory action.
Pharmacodynamics and pharmacokinetics
Drug forms in all blocks dopamine receptors in the brain. It is considered an effective corrector Psychopathic behavior. Increases content prolactin .
The active substance medications helps stop nuclear symptoms of schizophrenia : hallucinations , Thought disorder, mania. In addition, it causes sedative effect and reduces the manifestation of associated symptoms: hostility, alarm , Suspicion and aggression. Getting used to the nonspecific sedative effect rapidly.
The maximum content of active substance in tablets serum is observed after 4 hours. The drug can be taken regardless of meals. Bioavailability about 44%. The degree of connection with plasma proteins about 99%. Half-life - about 20 hours. Excreted in the feces and urine.
The active substance in a quantity penetrates placenta . A small amount of it is released into breast milk.
The equilibrium concentration is reached after about 4 days.
When using injection pronounced effect could be observed after 4 hours. Several larger effect is seen after 1-3 days after the internal administration. Then it is reduced.
One shot zuclopenthixol acetate It promotes pronounced and rapid reduction of symptoms psychotic symptoms . Drug action lasts 2-3 days. It is usually sufficient injection of 1-2 to the desired effect was achieved. Then you can take Oral or another depot .
After injection zuclopenthixol acetate begins transient dose-dependent sedation . Usually it is done in the initial phase psychosis As it calms the patient to establish antipsychotic effect . After internal administration sedative effect is fast enough and becomes pronounced after 2 hours. The maximum is reached after 8 hours. Then the action starts to weaken, even if they were repeated injections.
After drug administration zuclopenthixol acetate split. Half-life - about 32 hours. The maximum content in blood serum - after 1-2 days. The degree of coupling to plasma proteins is high. The minor extent through placenta . In some amounts excreted into breast milk. Excreted in the feces and urine.
Action klopiksol Depot and klopiksol-akufaz longer compared to oral forms.
Zuclopenthixol decanoate has sedative effect depends on the dosage. But the transition to klopiksol depot injection zuclopenthixol acetate or tablets zuclopenthixol probability Sedation decreases. The addiction develops quickly.
Zuclopenthixol decanoate splits when ingested. The maximum drug content in blood serum is observed in the first week. Half-life - 3 weeks. Equilibrium concentration in the re-introduction is set for 3 months.
The high degree of association with plasma proteins when administered drug in the form of injections. To a small extent of their active substances pass through placenta . A small amount is allocated to breast milk. Excreted in the feces and urine.
Indications
The drug is prescribed for chronic and acute forms Schizophrenia As well as other psychotic disorders Accompanied by hallucinations , Disturbances in thinking, paranoia. In addition, he was appointed to the disappearance of the state agitation , Hostility, the manic phase of manic-depressive psychosis , Increased anxiety, aggression, mental retardation in conjunction with psychomotor agitation and other behavioral disorders. Also, the drug is used for senile dementia Accompanied by paranoid ideas, behavior disorders, disorientation, confusion.
Klopiksol Depot provides continuous treatment. Its active ingredient prevents relapses, which may arise due to the discontinuation of the tablets.
Klopiksol-akufaz used to treat acute psychoses . chronic psychoses in acute and mania.
Contraindications
The drug is contraindicated in acute alcohol intoxication And acute intoxication opioid analgesics and barbiturates . coma . hypersensitivity to the drug.
In addition, it is not advisable to appoint pregnancy and Lactation .
Side effects
When you receive the medication as a rule, may experience the following side effects:
- Nervous system : dizziness Appearance extrapyramidal disorders (for their disappearance is possible to reduce the dose or take ANTIPARKINSONISM preparations) drowsiness , Violation accommodation , Long-term treatment is possible dyskinesia . akathisia . hypokinesia . hyperkinesia . tremor . gipertonus . headache , Attention disorders and gait, dystonia . paresthesia . amnesia . syncope , Speech disorders, convulsions, hyperreflexia . Parkinsonism . ataxia . gipotonus . migraine . sleep disturbance , Anxiety, abnormal dreams and nightmares, depression , Nervousness, apathy . confusion .
- Digestive system : Dryness of the mouth, constipation , Increased salivation, vomiting, diarrhea . dyspepsia , Abdominal pain, flatulence Nausea.
- CCC : hypotension . orthostatic hypotension . tachycardia .
- The visual system : Blurred vision, mydriasis .
- Respiratory system : Stuffy nose, breathlessness .
- Hearing Hypersensitivity, ringing in the ears.
- Skin : hyperhidrosis . itching . dermatitis , Rash, photosensitivity, pigmentation disorders, seborrhea . purpura .
- Musculoskeletal System : myalgia . muscle rigidity . torticollis . lockjaw .
- Metabolic processes : Increase or decrease appetite Set or decrease in body weight.
- The urinary system : Urinary retention, urinary disorders, polyuria .
- Liver and biliary system : Violation of functional tests.
- Reproductive system : Lack of ejaculation, orgasmic disorder (women) erectile dysfunction , Decreased / increased libido, dryness, vulvovaginal area.
- General disorders : asthenia , Malaise, fatigue, pain, thirst, pyrexia . hypothermia .
In rare cases it is possible:
- Digestive system : Transient changes in liver function tests.
- CCC : Venous trobmoembolizm Lengthening the interval QT on ECG .
- Blood and lymphatic system : thrombocytopenia . leukopenia . neutropenia . agranulocytosis .
- Endocrine system : Increased prolactin .
- Metabolic processes : hyperglycemia . hyperlipidemia Problems with glucose tolerance.
- The immune system : Hypersensitivity reactions anaphylactic reaction.
- Reproductive system and breast : gynecomastia . amenorrhea . galactorrhea . priapism .
- Liver and biliary system : cholestatic hepatitis . jaundice .
- Nervous system : Malignant neuroleptic syndrome .
Side effects are usually dose-dependent. They may be more pronounced at the beginning of treatment and decreases gradually.
The consequences of the use of medications during pregnancy and breast-feeding not thoroughly studied.
The sudden interruption of treatment may cause withdrawal symptoms. Typically, this dizziness , Nausea, anorexia, rhinorrhea . myalgia . insomnia , The state of excitation, vomiting, diarrhea , Increased Sweating . paresthesia . anxiety . tremor , Anxiety, variable sensations of heat or cold.
These symptoms may occur for 1-4 days after discontinuation of the drug and gradually reduced over 1-2 weeks.
Instructions for use klopiksol (method and dosage)
The tablets are administered orally in divided doses. The first dose of the drug during therapy should be small, then they gradually increased in view of the patient's response to treatment.
In the case of an acute attack Schizophrenia and other acute psychotic disorders, mania, severe agitation Instructions for use klopiksol recommends daily dosage of 10-50 mg.
Patients with chronic schizophrenia and other chronic psychosis dose a day - 20-40 mg.
With senile disorders that are accompanied by agitation and confusion drug per day by taking 2-6 mg, if needed, the dose may be increased to 10-20 mg. It is desirable to take the tablets in the evening.
In the case of moderate to severe psychotic disorders the initial dose - 20 mg per day. It may be gradually increased every 2-3 days to 10-20 mg as a daily dose of 75 mg is reached.
With agitation when mental retardation daily dose - 6-20 mg. If necessary, it increased to 25-40 mg.
After applying the injection klopiksol-akufaz prescribed pills klopiksol after 2-3 days.
Instructions on klopiksol Depot and klopiksol-akufaz reported that their dosage is selected individually depending on the patient's condition. Intramuscular injection. Medicine is injected into the upper outer quadrant of the buttocks.
As a general rule, appoint 1-3 ml klopiksol-akufaz. If more than 2 ml dose distributed to twice inject at different locations. If you want to make the second stab in 2-3 days. In some cases, it is administered within 1-2 days.
Zuclopenthixol acetate It can not be used for a long time. Maximum - 2 weeks. Total treatment dosage should not exceed 400 mg, and the number of shots - 4.
Maintenance therapy continued tablets or injections klopiksol Depot. The transition is performed as follows:
- Therapy tablets zuclopenthixol : 2-3 days after the last injection administered at a dose of 40 mg. It is recommended to divide it into several times. If needed, the dosage can be increased to 10-20 mg every 2-3 days up to 75 mg.
- On treatment Klopiksol Depot : After the last injection zuclopenthixol acetate introduces 1-2ml zuclopenthixol decanoate . Intramuscular injection of the latter continued every 2-4 weeks. If necessary, you can use higher dosages or make shorter intervals between injections.
In addition, klopiksol Depot and klopiksol-akufaz can be mixed in the same syringe, and to do as a single injection. Then use zuclopenthixol decanoate set individually.
For elderly patients at a dose can be reduced. The maximum single dose should not exceed 100 mg.
Preparation with zuclopenthixol decanoate It can cause irritation at the site where administered. Injections at a dosage of 2 ml are divided into two steps.
Switching from tablets to injections of course klopiksol Depot:
- A typical daily oral dosage, an increase of 8 times, is one prick zuclopenthixol decanoate every 2 weeks.
- A typical daily oral dosage increased to 16 times, is one prick zuclopenthixol decanoate every 4 weeks.
After the first injection continue to take pills for a week, but to a lesser dosage.
Patients in the elderly prescribed klopiksol Depot in the minimum dose.
If you have problems with the work of the liver appoint half the usual dose injection and control the content of the drug in the blood serum.
Overdose
The manifestations of an overdose of the drug in all its forms: drowsiness, extrapyramidal disorder . hypotension . hyperthermia . coma , Convulsions, shock, hypothermia .
As the therapy is prescribed gastric lavage. Then, treatment is symptomatic. Supportive therapy. Do not use adrenaline . Seizures can be prevented using the Diazepam , a extrapyramidal symptoms - Biperidenom .
An overdose of the drug by injection is considered unlikely. Possible changes in the ECG and QT-prolongation Also reported on Arrhythmia type Torsade de Pointes . ventricular arrhythmias , Cardiac arrest.
Treatment in this case, symptomatic and supportive. Measures should be taken to improve the functions of the respiratory system and CCC.
Cooperation
The medicament may increase Sedation acts of oppressive nervous system. You can not assign it together with Guanethidine and its analogs, as well as medicines, significantly prolongs QT interval . May decrease the effectiveness of adrenergic drugs for simultaneous use. It increases the likelihood of extrapyramidal symptoms in combination with Metoclopramide and Piperazine .
Together with lithium increases the likelihood neurotoxicity .
Tricyclic antidepressants in combination with neuroleptics mutually inhibit the biotransformation.
The use of drugs that inhibit the enzyme CYP2D6 , Slows down zuclopenthixol .
With careful use of the drug with the means that affect electrolyte balance.
Terms of sale
The drug is released under the prescription.
Storage conditions
Keep the drug should be out of the reach of small children. Store at 2 mg tablets and solutions for injections needed at temperatures up to 25 ° C. Means in tablets of 10 mg and 25 must be kept at a temperature of 30 ° C.
Shelf life
Klopiksol and klopiksol-akufaz should be stored no longer than two years. Shelf life klopiksol Depot - three years.
Reviews klopiksol
As a rule, patients leave reviews about klopiksol as a solution for injection. They note that the rate of use of this drug is very convenient, as the injections are made rarely. It's much easier than ever to take the pills.
Nevertheless, some of the benefits of the drug and in the case of point tablet form. For example, what it does not need to visit the doctor. The patient takes the medication on their own, so do not coordinate their activities with the schedule of injections.
Also reviews of klopiksol Depot and similar drugs in pill form, and note some unwanted effects. Usually, patients have reported apathy and decreased libido. Sometimes described extrapyramidal disorder .
However, the effectiveness of this means there is no doubt. The main thing is to take it exactly as prescribed by a doctor. As for any adjustments to the dose and changes in the state it is necessary to contact a specialist.
Price klopiksol where to buy
The cost of the drug is dependent on the release form. The average price klopiksol tablets is the following:
- Tablets 2 mg 50 pieces - 240 rubles;
- 25 mg tablets 100 pieces - 1550 rubles;
- Tablets 10 mg 50 pieces - 460 rubles.
Cost-klopiksol akufaz - about 2100 rubles.
Price klopiksol Depot one ampoule in the package - about 370 rubles, of 10 vials per pack - 3200 rubles.
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