Invega

Invega is an antipsychotic drug.

[1]

Indications of the invega

It is used to treat schizophrenia in adolescents from the age of 15, and in addition to this in adults. Also, he is prescribed to adults for the treatment of schizoaffective disorders.

Release form

Release in tablets, 7 pieces inside a blister pack. In a pack - 4 blisters with tablets.

Pharmacodynamics

The drug contains a racemic mixture of paliperidone.

Paliperidone is a selective blocking agent with a monoamine effect. Its medicinal effect is different from the standard antipsychotics. The substance is strongly synthesized with the receptors of serotonin (type 5-HT2), as well as dopamine (D2). Together with this, it acts as an antagonist of α1-adrenergic receptors, as well as histamine (H1) and α2-adrenegraic conductors (in respect of the latter two, it acts less actively). The medicinal activity of (+), as well as (-) - enantiomers of the active substance is similar in both quantity and degree of effect.

Paliperidone is not synthesized with acetylcholine receptors. Although the substance acts as a powerful antagonist of D2 conductors, which implies a reduction in the positive signs of schizophrenia, it contributes to the development of catalepsy, as well as the weakening of the motor effect is not as strong as the standard antipsychotics. Since the drug has a predominant antagonism against serotonin against the central type of action, it can weaken the property of the active ingredient to cause extrapyramidal etiology side effects.

[2]

Pharmacokinetics

The pharmacokinetics of the drug is proportional to the dosage sizes within the range of the available range.

With the use of a single dosage of drugs, a gradual increase in the rate of its release is observed, and therefore the plasma index of paliperidone steadily increases. Peak values of the drug are noted after a lapse of 24 hours. In many patients, stable indicators of the substance were observed after 4-5 days of daily disposable tablets.

Paliperidone is the active product of the disintegration of risperidone. Invegi release parameters are the result of a slight peak fluctuation in comparison with the immediate release of risperidone (the fluctuation index is 38%, compared to 12.5%).

The indicators of bioavailability of drugs with oral use reach 28%.

In the case of the use of tablets in combination with high-calorie or fatty foods, the peak values and the level of AUC of paliperidone increase by 50-60% in comparison with the use of drugs on an empty stomach.

The drug undergoes rapid distribution within the fluids with tissues. The distribution volume is 487 liters. The degree of protein binding inside the plasma reaches up to 74%. The substance is synthesized mainly with albumins, as well as with the α1-acid glycoprotein.

With a single use of 1 mg of labeled 14C-paliperidone after 7 days, 59% of the dose used is excreted - the unchanged substance is excreted in the urine. This demonstrates that the drug is not subject to intensive hepatic metabolism. About 80% of the labeled substance is found inside the urine, and about 11% is found in the feces.

Dosing and administration

Adults with schizophrenia.

It is recommended to take the drug in an amount of 6 mg once a day (taking in the morning). Titrating the dose at the initial stage of treatment is not necessary. In some patients, the drug effect of drugs is observed when using the smallest or large dose (within the range that is allowed to take - 3-12 mg once a day). To change the size of the dose is allowed, if there are such indications, and also after a careful reassessment of the state of health. If you want to increase the dose, this increase should be done according to this scheme: 3 mg / day with interruptions of at least 5 days.

Adults with schizoaffective disorders.

It is required to take the medicine in the morning at a rate of 6 mg once a day. In individual patients, therapeutic effectiveness develops after applying a large dosage (within the permissible range - 6-12 mg once per day). If it is necessary to increase the dose, it is necessary to increase it, adding 3 mg / day with intervals of at least 4 days.

People with functional renal impairment.

Persons who have a mild form of the disease (CC level ≥50 / <80 ml / minute) should take the medicine once a day at a rate of 3 mg. It is permitted to increase the dose to a single dose of 6 mg per day, but only after assessing the patient's drug tolerance, as well as its drug efficacy.

People with an average or severe form of the disorder (CC score ≥10 / <50 ml / minute) should drink a medicine in the amount of 1.5 mg, once a day. Portions may be increased to 1-fold intake of not more than 3 mg per day after clinical assessment of the health status.

Using Invega in individuals with a CC level <10 ml / minute was not performed, therefore, it is not recommended to prescribe a drug to this group of patients.

Children with schizophrenia.

Adolescents over 15 years old are recommended to take the medicine at a dosage of 3 mg - a single dose in the morning.

Children, whose weight is <51 kg, per day can take no more than 6 mg of the drug.

For children weighing ≥51 kg, a maximum of 12 mg of the drug can be taken per day.

You can change the dose if you have appropriate indications. Increase to perform according to the following scheme: 3 mg per day with intervals of at least 5 days.

The efficacy of the use and safety of the drug in the treatment of schizophrenia in adolescents 12-14 years old have not been studied.

The medicine is taken orally - swallowing the whole tablet, not chewing and grinding, and also washed down with water. The shell of the tablet is insoluble, and the active ingredient is gradually released from under it. The shell, together with the insoluble elements of the nucleus, is excreted completely from the body.

The use of drugs depends on eating. It is required to tell the patient that you need to take the pill all the time either on an empty stomach, or with breakfast, without alternating these methods of admission during the period of treatment.

Use of the invega during pregnancy

There is insufficient data on the use of paliperidone in pregnancy. The substance did not have teratogenic effects in animal tests, but other types of reproductive toxicity were noted.

The use of antipsychotic drugs (here includes paliperidone) in the 3rd trimester increases the likelihood of negative effects, among which extrapyramidal manifestations or withdrawal syndrome in newborns. These symptoms may be different in duration of exposure and severity. There is information about the development of hyper and hypotension, agitation, drowsiness and tremor, as well as respiratory insufficiency and problems with infant feeding. Because of this, the state of the newborn should be constantly and very carefully monitored.

The medicine can not be administered to pregnant women (except for special life indications). If it is necessary to stop taking Invega during pregnancy, it is necessary to perform the abolition of drugs gradually.

Paliperidone passes inside the mother's milk, so you can expect the effect of the medication on the baby who is breast-fed. In this regard, it is forbidden to prescribe a medicine for lactation.

Contraindications

Major contraindications: hypersensitivity to paliperidone, risperidone, as well as any other additional elements of the drug. It is forbidden to appoint children under the age of 15.

[3],

Side effects of the invega

The most common side effects are:

• rhinopharyngitis;
• a state of mania or insomnia;
• weight gain;
• headache or muscle pain;
• abdominal discomfort, nausea, constipation or diarrhea, as well as increased appetite;
• dysarthria or akathisia;
• an increase in muscle tone, and in addition a tremor paralysis;
• feeling drowsy;
• hypersalivation.

Negative reactions that develop more rarely:

• cystitis;
• ear infections, tonsillitis with bronchitis, and also sinusitis;
• anaphylactic symptoms;
• leuko- or neutropenia, as well as anemia;
• hyperprolactinemia;
• hyper- or hypoglycemia, and in addition to this anorexia;
• development of diabetes mellitus;
• sleep disorders, nightmares;
• problems with concentration of attention, the emergence of paresthesia or seizures, as well as hyperactivity of the psychomotor type;
• dryness of the eye mucous membranes, conjunctivitis, and also lacrimation;
• ear call or pain;
• increase or decrease in blood pressure, bradycardia, prolongation of the QT-interval, AV blockade;
• incontinence, bloating, and gastroenteritis;
• swelling and stiffness in the joints, as well as arthralgia;
• urinary incontinence or dysuria;
• the appearance of discharge from the nipples, the weakening of the libido and the development of gynecomastia;
• problems with sexual function, menstruation cycle disorders;
• thirst, hypothermia, peripheral puffiness, and fever.

[4]

Overdose

In general, it is expected that the symptoms of drug intoxication will manifest in the form of potentiation of the medicinal effect of the drug. Among these symptoms: sedation, a feeling of drowsiness, lower blood pressure, tachycardia, extrapyramidal signs and prolongation of the QT-interval. As a result of poisoning, ventricular tachycardia of bi-directional type was also noted, and in addition ventricular fibrillation.

In the process of assessing the patient's condition, it must be remembered that the drug has a prolonged effect. Also he does not have a special antidote. Supportive procedures of a general nature are required. It is necessary to provide permeability to respiratory ducts and adequate ventilation with oxygenation, and to maintain these functions. It is also necessary to constantly monitor the work of the CAS (this includes the ECG procedure) to determine the possible presence of arrhythmias. Reduction of pressure along with circulatory collapse is treated with IV injections of fluid or sympathomimetics. Sometimes gastric lavage may be required (if the victim is unconscious, after the intubation procedure), taking activated charcoal and laxatives. In the case of development of extrapyramidal disorders, it is necessary to introduce cholinolytic drugs in a severe degree. Constant monitoring of the victim, as well as monitoring of vital physiological functions, is required until all the overdose manifestations disappear.

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Interactions with other drugs

It is necessary to prescribe with caution the drug with drugs prolonging the QT interval.

The active component of drugs does not cause drug-significant interactions with drugs, the metabolism of which occurs through the hemoprotein system P450. In vitro tests, it was found that paliperidone does not have an inhibitory or inductive effect on the isoenzymes of this hemoprotein.

Caution is required when combined with other drugs that have a central effect.

It is forbidden to combine with medications that cause hypotension of orthostatic type.

Invega neutralizes the effect of levodopa.

The probability of drug interaction with lithium is very low.

When combined with sodium valproate, there was no change in the concentrations of both drugs. There was no significant interaction of the drug with paroxetine.

Combined use of carbamazepine with the substance provoked a 37% reduction in the indices of paliperidone within the blood. Because of this, it is necessary to adjust the dose size of Invega with this combination.

Simultaneous admission with trimethoprim did not affect the pharmacokinetics of the drug.

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Storage conditions

Invega medicine must be kept out of reach for young children. The temperature level should not rise above 30 ° C.

[9], [10],

Special instructions

Reviews

Invega effectively fights against productive manifestations of schizophrenia (such as agitation with hallucinations, as well as delirium). Psychiatrists point out that the drug demonstrates the greatest effectiveness in the treatment of schizophrenia, against which there is an apatoabulic syndrome (with indications such as indifference and indifference, as well as a lack of pathological character, a sense of detachment and a lack of desire to do anything). Drug use has a resocializing effect - the feeling of apathy disappears towards what is happening around, there is a desire to act.

The patient's feedback shows that the drug, in addition to high efficiency, has a lot of side effects.

Invega is considered a safer means compared to risperidone, but it must be taken into account that it can be administered exclusively to adolescents and adults.

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Shelf life

Invega can be used in the period of 2 years from the date of manufacture of the medicament.

[12], [13]