Invega, 6 mg, extended-release film-coated tablets, 28 pcs.

Invega (tablet form) belongs to the psycholeptic group. Important features of the medicine from the instructions for use:

How to dissolve vascular plaques, normalize blood circulation, blood pressure and forget the way to the pharmacy

• Sold only with a doctor's prescription
• During pregnancy: with caution
• When breastfeeding: contraindicated
• In childhood: contraindicated
• For liver dysfunction: you can
• If renal function is impaired: with caution
• In old age: with caution

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

Antagonist of dopamine D2 receptors and serotonin 5-HT2. The antipsychotic effect is associated with blockade of D2-dopamine receptors. Compared to classical antipsychotics, it suppresses motor activity less and provokes catalepsy.

Eliminates negative and productive symptoms of schizophrenia, while causing almost no extrapyramidal adverse reactions. It affects sleep: it reduces the period before falling asleep, the number of awakenings, and increases the duration and quality of sleep. Causes an increase in prolactin levels in the blood. Has a moderate antiemetic effect.

Pharmacokinetics

When taking one dose, the concentration of the active substance in the blood increases and reaches a maximum after 24 hours. Equilibrium concentrations are achieved after 4–5 days of regular use. Paliperidone is an active metabolite of risperidone. Its release characteristics provide less variation in paliperidone concentrations.

It is quickly distributed in tissues, 74% binds to blood proteins. A week after taking one tablet, 59% is excreted in the urine. It is not metabolized in the liver and is therefore excreted unchanged. In vitro studies have shown that cytochrome P450 isoenzymes play a certain role in metabolism, but not a significant one. The half-life is 23 hours.

Since the active substance is not metabolized in the liver, there is no need to reduce the dose in patients with moderate liver dysfunction. However, the dose should be reduced in severe renal impairment. The pharmacokinetics of paliperidone in adolescents is comparable to that in adults.

Side effects

Common adverse reactions:

• nasopharyngitis;
• insomnia, mania;
• weight gain;
• headache;
• muscle pain;
• nausea, abdominal discomfort, diarrhea or constipation, increased appetite;
• akathisia, dysarthria;
• parkinsonism, increased muscle tone;
• drowsiness;
• salivation.

Uncommon adverse reactions:

• cystitis;
• ear infections, bronchitis, sinusitis, tonsillitis;
• anaphylactic reaction;
• anemia, neutropenia, leukopenia;
• hyperprolactinemia;
• anorexia, hypoglycemia and hyperglycemia;
• diabetes;
• sleep disturbances, “nightmare” dreams;
• convulsions, impaired attention, paresthesia, psychomotor hyperactivity;
• conjunctivitis, dry eyes, lacrimation;
• pain and ringing in the ears;
• bradycardia, AV block, increased QT interval, increased or decreased blood pressure;
• flatulence, fecal incontinence, gastroenteritis;
• arthralgia, joint swelling and stiffness;
• dysuria, urinary incontinence;
• decreased libido, nipple discharge, gynecomastia,
• sexual dysfunction, changes in the menstrual cycle;
• peripheral edema, thirst, fever, hypothermia.

Adverse reactions

Invega causes drowsiness, dyspepsia, and dizziness much less frequently than its predecessor risperidone.

Dry mouth, tremors, headaches, increased blood pressure, orthostatic drop in pressure, increased QT interval - occur with a frequency of less than 5%. Tachycardia is much more common.

Extrapyramidal effects from taking the drug (akathisia, hypersalivation, rigidity, hypokinesia, acute dystonia) depend on the dose.

When using up to 6 mg of the drug, side effects occur with the same frequency as when taking placebo (up to 13%).

When taking 9 – 12 mg/day, about 26% of patients have side effects. The severity of extrapyramidal symptoms is mild.

The possibility of their occurrence increases in patients:

• with severe brain failure;
• in people who have previously taken typical antipsychotics for a long time.

Extrapyramidal disorders are most pronounced in the first three days of treatment. They decrease within 1-3 months, and then disappear completely.

Other side effects:

• memory impairment, decreased speed of thinking and reaction to external stimuli, etc.;
• cerebrovascular deficiency.

Article on the topic: Nordic walking - the benefits and harms of a newfangled hobby

Increased risk:

• deterioration of carbohydrate metabolism;
• expansion of the QT interval on the cardiogram, which is manifested by severe arrhythmia leading to death.

Patients' weight increases within 2 months of treatment, by an average of 700 grams. Significant weight gain (more than 7% of the original) occurs rarely and is associated with the dosage of the drug. There is no need to prescribe higher doses to control weight gain.

People prone to obesity are additionally prescribed diet and exercise.

An increase in prolactin levels in the blood is detected in 67% of patients by the end of the 2nd week of treatment with paliperidone. Then this indicator remains at the same level. Possible manifestations of hyperprolactinemia:

• nipple discharge;
• cessation of menstruation;
• gynecomastia;
• sexual dysfunction, etc.

But they occur in only 2% of patients who use the drug. This sets it apart from risperidone and other classical antipsychotics.

Invega, instructions for use (Method and dosage)

The drug is taken orally in the morning, regardless of meals. The dosage of Inveg depends on the severity of the disease and the age of the patients.

For schizophrenia, adults are prescribed Invega 6 mg once a day. If an increase in dose is required, it is recommended to increase it by 3 mg every 5 days. In some patients, the effect occurs at lower or higher doses - in the range of 3-12 mg per day. Adolescents are recommended 3 mg per day. However, higher doses may be required, increasing them every 5 days.

For schizoaffective disorders, the recommended dose is 6 mg per day, in the morning. It is also possible to increase the dose to 12 mg per day, which is carried out gradually.

For moderate liver dysfunction, there is no need to reduce the dose. For severe cases, the dose is no more than 3 mg per day. In elderly patients, the dose depends on renal function. The safety of the drug in the treatment of schizophrenia in children under 12 years of age has not been studied. When transferring patients from paliperidone to other antipsychotics, you need to monitor the patient's condition.

Rules for administration and dosage

The drug is taken in the morning. The time of administration is not related to food consumption. The whole capsule must be swallowed; the integrity of the tablet must not be damaged!

When choosing a dose, the person’s weight must be taken into account. For people weighing up to 50 kg, the dosage of the drug is usually no higher than 6 mg/day. For patients weighing 50–70 kg, the average dose of the drug is 9 mg.

For people of average weight who have not previously taken antipsychotics, or if they used this group of drugs during the treatment of an exacerbation of schizophrenia (lasting no more than 2 months), treatment should begin with 6 mg / day.

Patients weighing more than 85 kg, as well as people who have had therapeutic results in the past only from taking high doses of antipsychotics, should start taking 9 mg.

Sometimes, in patients weighing more than 70 kg, the “working” dose is 12 mg.

The effective concentration of paliperidone in the blood develops after 4 - 5 days from the start of taking the drug. Then the best antipsychotic effect appears. Therefore, you need to think about increasing the dosage no earlier than 5 days from the start of therapy.

Almost always, the individually selected dosage of the drug does not need to be subsequently increased. The medication is effective for the treatment of schizophrenia during exacerbation and as maintenance treatment.

Article on the topic: Complications after hip replacement

With proper therapy, the full anti-productive effect of the antipsychotic medication appears within 4–6 weeks from the start of administration, and the anti-deficiency effect by 8–12 months of continuous treatment.

That is, if the drug is well tolerated, even after leaving the exacerbation zone, the dose does not need to be reduced.

The reason for reducing the dosage is the occurrence and persistence of side effects longer than 7 days, such as:

• dizziness;
• drowsiness;
• mild dyspeptic disorders.

If intolerance occurs or in case of severe complications, the medicine is immediately discontinued. But such situations are quite rare.

The question of a possible replacement of the drug, if there are no serious side effects, should be raised no earlier than after 3–4 weeks. from the start of therapy.

Interaction

Use caution when prescribing with drugs that prolong the QT interval. Paliperidone does not cause clinically significant interactions with drugs that are metabolized by the cytochrome P450 system. In vitro studies have shown that paliperidone does not cause inhibition or induction of isoenzymes of this cytochrome.

The drug should be used with caution in combination with other centrally acting drugs. Do not co-administer with drugs that cause orthostatic hypotension. Neutralizes the effect of levodopa. An interaction between this drug and lithium is unlikely.

Simultaneous administration with sodium valproate - the concentration of both drugs did not change. There was also no significant interaction with paroxetine. Use with risperidone has not been studied, but with carbamazepine it caused a decrease in the concentration of paliperidone in the blood by 37%, and therefore the dose of the latter needs to be adjusted. Use with trimethoprim did not affect the pharmacokinetic characteristics of paliperidone.

Invega, 6 mg, extended-release film-coated tablets, 28 pcs.

ZNS. It is known that antipsychotic drugs, including paliperidone, can cause NMS, which is characterized by hyperthermia, muscle rigidity, instability of the autonomic nervous system, depression of consciousness, and increased serum concentrations of CPK. Myoglobinuria (rhabdomyolysis) and acute renal failure may also occur in patients with NMS. If a patient experiences objective or subjective symptoms of NMS, all antipsychotic medications, including paliperidone, should be immediately discontinued.

Tardive dyskinesia. Drugs with dopamine receptor antagonist properties can cause tardive dyskinesia, which is characterized by rhythmic involuntary movements, mainly of the tongue and/or facial muscles. If a patient experiences objective or subjective symptoms indicating tardive dyskinesia, the advisability of discontinuing all antipsychotic drugs, including paliperidone, should be considered.

Prolongation of the QT interval. As with other antipsychotics, caution should be exercised when prescribing Invega ® to patients with a history of cardiac arrhythmias, congenital prolongation of the QT interval, and concomitant use with drugs that prolong the QT interval.

Hyperglycemia and diabetes mellitus. Hyperglycemia, diabetes mellitus and exacerbation of existing diabetes mellitus were observed during treatment with Invega ®. Establishing a relationship between the use of atypical antipsychotic drugs and disorders of glucose metabolism is complicated by the increased risk of developing diabetes mellitus in patients with schizophrenia and the prevalence of diabetes mellitus in the general population. Given these factors, the relationship between the use of atypical antipsychotic drugs and the development of adverse effects associated with hyperglycemia is not fully established. In patients diagnosed with diabetes mellitus, glucose levels should be regularly monitored. Patients with risk factors for diabetes mellitus (eg, obesity, family history of diabetes) should have fasting blood glucose levels monitored at the start of treatment and periodically during treatment. All patients should be clinically monitored for symptoms of hyperglycemia and diabetes mellitus. Patients who develop symptoms of hyperglycemia while being treated with atypical antipsychotics should have their blood glucose levels monitored. In some cases, symptoms of hyperglycemia have resolved with discontinuation of atypical antipsychotic medications, but some patients require antidiabetic treatment despite discontinuation of the drug.

Increase in body weight. Significant weight gain was observed during treatment with atypical antipsychotics. It is necessary to monitor patients' body weight.

Hyperprolactinemia. Like other D2-dopamine receptor antagonists, paliperidone increases prolactin levels, and this increase persists throughout drug administration. The effects of paliperidone are comparable to those of risperidone, the drug that has the greatest effect on prolactin levels among other antipsychotic drugs. Hyperprolactinemia, regardless of etiology, can suppress the expression of GnRH in the hypothalamus, which leads to a decrease in the secretion of gonadotropins by the pituitary gland. This in turn can suppress reproductive function, weakening sexual steroidogenesis in women and men. Galactorrhea, amenorrhea, gynecomastia and impotence have been reported in patients taking drugs that increase prolactin levels. Long-term hyperprolactinemia associated with hypogonadism can lead to decreased bone density in women and men.

In vitro tissue culture studies have shown that approximately one third of human breast cancers are prolactin-dependent. This should be taken into account when prescribing drugs that increase prolactin levels to patients with previously diagnosed breast cancer. Clinical and epidemiological studies conducted to date have shown no association between atypical antipsychotic drugs and tumor formation in humans. However, the available data are too limited to draw definitive conclusions.

Orthostatic hypotension. Paliperidone has α-blocking activity and may therefore cause orthostatic hypotension in some patients. Paliperidone should be used with caution in patients with cardiovascular disease (for example, heart failure, myocardial infarction or ischemia, cardiac conduction disorders), cerebrovascular disease, and with conditions that contribute to arterial hypotension (for example, dehydration, hypovolemia and therapy with antihypertensive drugs).

Regulation of body temperature. Antipsychotic drugs are associated with such undesirable effects as disruption of the body's ability to regulate temperature. Caution should be exercised when prescribing paliperidone to patients with conditions that may contribute to an increase in core body temperature, including intense exercise, dehydration, exposure to high external temperatures, or concomitant use of drugs with anticholinergic activity.

Antiemetic effect. Preclinical studies have demonstrated the antiemetic effect of paliperidone. This effect, when observed in humans, may mask objective and subjective symptoms of overdose of some drugs, as well as diseases such as intestinal obstruction, Reye's syndrome, and brain tumors.

Priapism. Drugs with α-adrenergic blocking effects can cause priapism. Priapism has been reported in post-marketing studies of paliperidone.

Suicidal attempts. The possibility of suicide attempts is characteristic of mental illness, so treatment of patients at high risk should be carried out under close supervision. In these cases, Invega ® should be prescribed in a minimum number of tablets to reduce the risk of overdose.

Leukopenia, neutropenia, agranulocytosis. Leukopenia, neutropenia and agranulocytosis were observed with the use of antipsychotics, incl. when using the drug Invega ® . Agranulocytosis has been observed very rarely during post-marketing surveillance. In patients with a history of clinically significant decreases in white blood cell count or drug-dependent leukopenia/neutropenia, a complete blood count is recommended during the first months of therapy; Discontinuation of treatment with Invega should be considered at the first clinically significant decrease in the white blood cell count in the absence of other possible causes. Patients with clinically significant neutropenia are advised to be monitored for fever or symptoms of infection and to initiate treatment immediately if such symptoms occur. Patients with severe neutropenia (absolute neutrophil count less than 1·10 9 /l) should stop using Invega ® until the white blood cell count returns to normal.

Venous thromboembolism. Cases of venous thromboembolism have been reported with the use of antipsychotic drugs. Since patients taking antipsychotic drugs are often at risk of developing venous thromboembolism, all possible risk factors should be identified before and during treatment with Invega ® and preventive measures taken.

Intraoperative floppy iris syndrome (ISID). ISDR was observed during surgery for the presence of cataracts in patients receiving therapy with drugs from the group of α 1 -adrenergic receptor antagonists. ISDR increases the risk of complications associated with the organ of vision during and after surgery. The doctor performing such an operation must be informed in advance that the patient has taken or is currently taking drugs that have α 1-adrenergic receptor antagonist activity. The potential benefit of discontinuing α 1 -adrenergic antagonist therapy before surgery has not been established and should be weighed against the risks associated with discontinuing antipsychotic therapy.

Pregnancy and child care. The patient should notify his or her physician of pregnancy or planning to become pregnant during treatment with Invega ® . Caution should be exercised when prescribing Invega ® to nursing mothers (see “Use during pregnancy and lactation”).

Alcohol consumption. Patients should avoid drinking alcohol during treatment with Invega ® .

Conditions leading to a decrease in the presence of the drug in the gastrointestinal tract. Conditions that reduce the presence of the drug in the gastrointestinal tract, such as diseases associated with chronic diarrhea, may cause a decrease in the absorption of paliperidone.

Invega ® tablets are manufactured using osmotic release technology, in which osmotic pressure releases paliperidone at a controlled rate. The system, which looks like a capsule-shaped tablet, consists of an osmotically active three-layer core surrounded by an intermediate shell and a semi-permeable membrane. The three-layer core consists of two medicinal layers containing the drug substance and excipients, as well as an ejector layer containing osmotically active components. On the dome side of the drug layers there are two outlet holes made using a laser. In the gastrointestinal tract, the colored shell quickly dissolves, and water begins to flow into the tablet through a semi-permeable control membrane. The membrane controls the level of water intake, and this in turn controls the level of drug release.

The hydrophilic polymers in the tablet core absorb water and swell into a gel containing paliperidone, which is then expelled through holes in the dome. The insoluble components of the tablet are excreted from the body in the stool. Patients should not worry if they notice something that looks like a pill in their stool.

Influence on driving a car and working with machinery. Paliperidone may interfere with activities requiring rapid mental response and may also have visual effects, so patients should avoid driving or operating machinery until their individual sensitivity to paliperidone has been established.

Reviews about Invega

This drug eliminates productive symptoms (delusions, hallucinations, agitation) in schizophrenia. According to the observation of psychiatrists, the drug is more effective in schizophrenia, accompanied by apatoabulic syndrome (indifference, indifference, detachment from everything, pathological lack of will, reluctance to perform any actions). Taking the drug gives a resocializing effect - apathy towards everything that happens disappears and the potential for action appears. In their reviews, patients note the effectiveness of the drug and the presence of side effects.

• “... I took 12 mg for two months. The negative symptoms went away - he became sociable and became interested in life. Prolactin increased greatly and I was switched to Rispolept.”
• “... The general condition on Inveg is much better than on others. A desire for creativity, which disappeared 14 years ago, and creative vigor appeared.”
• “... I take 12 mg - the condition has returned to normal, but in order to consolidate the effect, they told me to drink at this dosage for another 1.5 months and a half, and then reduce it to 9 mg.”
• “... The most unpleasant side effect for me is hormonal disorders. I’m gaining a lot of weight, my periods have completely disappeared, there’s discharge from the mammary glands and my breasts are growing.”
• “... I take the medicine Invega, I tolerate it well. The doctor said that the tablet should not be divided, since its shell ensures a gradual release and long-term effect of the active substance.”
• “... As the dose increases, flu-like symptoms appear: aching joints, muscle pain, nasal congestion, thirst, rapid breathing - a condition similar to a temperature over 40.”

This drug is safer than risperidone, but is approved for use only in adults and adolescents.

General information about the drug

Invega is a popular drug used to treat psychosis. It is produced by a pharmaceutical company (USA).

Drug group, INN, application

The drug belongs to a special drug group - antipsychotic drugs. They are also called antipsychotics. Such drugs affect the central nervous system.

The international nonproprietary name of a drug depends on the active substance that is included in its composition and determines its effect on the body. The INN of the drug Invega is Paliperidone. The scope of application of the drug is psychiatry. It is prescribed for the treatment of various psychotic disorders in adults and adolescents from 12 years of age.

Release form and cost

The drug is available in the form of extended-release tablets. They have a capsule-like shape. Their color and markings differ depending on the content of the active substance:

• 3 mg – white tablets marked PAL 3;
• 6 mg – yellowish color and the inscription PAL 6;
• 9 mg – pinkish and gray tint labeled PAL 9;
• 12 mg – yellow-brown color with the inscription PAL 12.

Advantages of the Invega drug molecule

All tablets are packaged in cell blisters of 7 pieces. A cardboard box contains 28 or 56 tablets. Invega is available with a prescription; its price depends on the content of the active ingredient in 1 tablet and their quantity in the package. Also, the cost may vary depending on where it was purchased. Examples of prices for medicine in different pharmacies in Russian cities:

This remedy is one of the vitally important drugs. It can only be purchased with a special prescription from the attending psychiatrist.