Index of drugs

Treatment of schizophrenia in adults. Treatment of psychotic or manic symptoms in schizoaffective disorder in adults. The effects on depressive symptoms have not been demonstrated.

1 tabl sustained release contains 3 mg, 6 mg, 9 mg or 12 mg paliperidone; 3 mg tablets contain lactose.

Paliperidone is a selective blocking agent of monoamines. It binds strongly to 5-HT serotoninergic receptors₂ and dopaminergic D₂. It also blocks α adrenergic receptors₁ and slightly weaker histamine H-receptors₁ and α-adrenergic receptors₂. The preparation contains a racemic mixture of paliperidone. The pharmacological activity of both enantiomers is similar in qualitative and quantitative terms. Paliperidone is not associated with cholinergic receptors. Although it is a potent D-receptor antagonist₂, thus relieving positive symptoms of schizophrenia, it causes catalepsy to a lesser extent and weakens motor functions than traditional neuroleptics. Dominating central serotonin antagonism may reduce the propensity of paliperidone to cause extrapyramidal symptoms. After a single dose of the preparation, paliperidone levels in the blood increase continuously until the maximum value is reached (C_max) about 24 hours after administration of the drug. When dosing once a day, steady-state concentrations are achieved within 4-5 days. The bioavailability of paliperidone after oral administration is 28%. A high-calorie meal increases the C value_max and Paliperidone AUC by 50-60% compared to fasting. Paliperidone binds to plasma proteins 74%. Paliperidone is the active metabolite of risperidone. It is slightly metabolised in the liver. T_0,5 It is about 23 hours. It is mainly excreted in the urine. Elimination of paliperidone decreases with decreased renal function.

Hypersensitivity to paliperidone, Risperidone or to any of the excipients.

It is not recommended for use in children <12 years. The safety and efficacy of paliperidone in children from 12 to 17 years have not been studied. Patients with schizoaffective disorder treated with paliperidone should be closely monitored for possible change from manic to depressive symptoms. The use of paliperidone in elderly patients with dementia has not been studied, but experience with risperidone is considered: in elderly patients with dementia, using atypical antipsychotics (including risperidone), increased mortality and an increased incidence of cerebrovascular accidents have been observed. Paliperidone should be used with caution in elderly patients with dementia and risk factors for stroke. When prescribing paliperidone to patients with Lewy body disease or Parkinson's disease, the risk / benefit ratio should be considered because of the risk of neuroleptic malignant syndrome, as well as increased sensitivity to antipsychotic drugs (manifested by confusion, impaired consciousness, and postural instability falls). Paliperidone should not be used in patients with creatinine clearance (CCr) <10 ml / min. Use with caution in patients with: renal impairment with CCr ≥ 10 ml / min (adjust the dosage); with severe hepatic impairment - Child-Pugh class C (no data on these patients); with diabetes or risk factors for the development of diabetes (regularly control glycaemia); with an interview for potentially prolactin-dependent tumors (eg breast cancer) and for patients with prolactin-dependent tumors; with heart failure, myocardial infarction or ischemia, conduction abnormalities, with cerebrovascular disease or with disorders predisposing to hypotension, e.g. dehydration and hypovolemia (risk of orthostatic hypotension in these groups of patients); with cardiovascular disease,prolongation of family QT interval or during concomitant use of other QT prolonging agents (risk of arrhythmia); with a history of convulsions or other conditions that may lower the seizure threshold; with haematological disorders - with clinically significant leukopenia or drug-induced leucopenia / neutropenia (observe patients for the first few months of treatment, discontinuation of the drug at the first symptom of clinically significant decrease in leukocyte count, in the absence of other causative factors), with clinically significant neutropenia (observe patients, if they have a fever or other signs or symptoms of infection, and take immediate treatment if these symptoms occur, in patients with absolute neutrophil count <1 x 10⁹/ l the use of paliperidone should be discontinued and the leukocyte count should be investigated until the result returns to normal); with the risk of increasing the basic body temperature (eg those performing intense physical exercise, exposed to extremely high temperatures, taking concomitantly with anticholinergic or dehydrated drugs). Because of the frequent acquired risk factors for the development of venous thromboembolism in patients treated with antipsychotics, risk factors should be determined before and during treatment and appropriate preventive measures should be taken. Due to the risk of intraoperative flaccid iris syndrome (IFIS), an ophthalmologist should be informed about the use of paliperidone now or in the past before cataract surgery; a cautious approach to the procedure is recommended; If the IFIS team is suspected, it may be necessary to take measures to stop the iris before falling out during the procedure. All patients treated with any atypical antipsychotic drug, including paliperidone, should be observed for symptoms of hyperglycaemia (such as polydipsia, polyuria, excessive appetite and weakness) and regularly control body weight. Risperidone should be discontinued in the event of tardive dyskinesia or symptoms of a neuroleptic malignant syndrome. Patients should be advised to see a doctor immediately if symptoms of priapism persist within 3-4 hours. Antiemetics of paliperidone may mask the signs and symptoms of drug overdose or conditions such as intestinal obstruction, Reye's syndrome and brain tumor . Due to the fact that the tablets of the preparation do not deform and do not change their shape in the digestive tract in a significant way, they usually should not be administered to patients with pre-existing severe gastrointestinal stenosis (pathological or iatrogenic), or patients with dysphagia or severe difficulties. swallowing tablets - there is a risk of obstruction symptoms. The preparation can only be used in patients who are able to swallow the tablet whole. Conditions leading to shortened gastrointestinal transit time, e.g. diseases associated with chronic severe diarrhea, may result in reduced absorption of paliperidone. Due to the lactose content, 3 mg tablets should not be used in patients with rare hereditary galactose intolerance, lactase deficiency (Lappa type) or malabsorption of glucose-galactose.

The safety of the medicine during pregnancy has not been established. It should not be used during pregnancy unless clearly necessary. Newborns exposed to paliperidone during the third trimester of pregnancy are at risk for extrapyramidal disorders and / or withdrawal symptoms of varying severity and duration after delivery - therefore neonates should be carefully monitored. If you need to stop treatment during pregnancy, do not stop your treatment suddenly. Paliperidone is excreted in breast milk in such an amount that the effect on the fed baby is likely if the breast-feeding mother takes therapeutic doses. Do not use the product during breast-feeding.

Very often: insomnia, parkinsonism, akathisia, sedation, drowsiness, headache. Common: bronchitis, upper respiratory tract infection, sinusitis, urinary tract infection, influenza, weight gain, increased appetite, weight loss, decreased appetite, mania, agitation, depression, anxiety, dystonia, dizziness, dyskinesia, tremor,blurred vision, conduction abnormalities, prolonged QT interval in ECG, bradycardia, tachycardia, orthostatic hypotension, hypertension, sore throat and larynx, cough, nasal congestion, abdominal pain, abdominal discomfort, vomiting, nausea, constipation, diarrhea, indigestion, dry mouth, toothache, transaminase elevation, pruritus, rash, musculoskeletal pain, back pain, joint pain, amenorrhea, fever, weakness (asthenia), fatigue. Uncommon: pneumonia, respiratory tract infection, cystitis, ear infection, tonsillitis, anemia, decreased hematocrit, diabetes, hyperglycemia, anorexia, increased triglycerides in the blood, sleep disturbances, confusion, decreased libido, anorgasmia, nervousness , nightmares, fits, fainting, psychomotor hyperactivity, dizziness dependent on body posture, concentration disorders, dysarthria, taste disturbances, hypoesthesia, paraesthesia, conjunctivitis, dry eye, labyrinthine dizziness, tinnitus, ear pain, block atrio-ventricular, sinus arrhythmia, abnormal ECG, palpitations, hypotension, dyspnea, wheezing, nosebleeds, tongue edema, gastroenteritis, dysphagia, bloating, increased GGT, increased liver enzymes, urticaria, alopecia, acne , increase one concentration of phosphocreatine kinase in the blood, muscle spasms, stiffness of the joints, swelling of the joints, muscle weakness, neck pain, incontinence, pollakiuria, urinary stasis, dysuria, erectile dysfunction, ejaculation disorders, menstrual disorders, galactorrhea, sexual dysfunction, breast pain, breast discomfort, swelling of the face, swelling, chills, increased body temperature, abnormal walking, thirst, chest pain, feeling unwell, falling. Rare: eye infection, onychomycosis, cellulitis, dermal acarosis, agranulocytosis, neutropenia, leukopenia, thrombocytopenia, increased eosinophils, anaphylactic reaction, hypersensitivity, abnormal secretion of antidiuretic hormone, urinary Glucose, hyperprolactinemia, water intoxication, diabetic ketoacidosis , hypoglycemia, polydipsia, increased cholesterol in the blood, demented affect, neuroleptic malignant syndrome, tardive dyskinesia, cerebrovascular incident, cerebral ischemia, lack of response to stimuli, loss of consciousness, decreased level of consciousness, diabetic coma, balance disorders, improper coordination, head nodding, glaucoma, eye movement disorders, rotational eye movements, photophobia, increased tearing, ocular congestion, atrial fibrillation, orthostatic tachycardia associated with a change in body position, venous thrombosis, embolism pulmonary disease, ischemia, fits of redness, sleep apnea syndrome, hyperventilation, aspiration pneumonia, respiratory congestion, dysphonia, pancreatitis, intestinal obstruction, faecal incontinence, fecal stones, lip inflammation, jaundice, angioedema, drug efflorescence, hyperkeratosis, eczema, dry skin, erythema, skin discoloration, seborrheic dermatitis, dandruff, rhabdomyolysis, abnormal posture, neonatal withdrawal syndrome, priapism, delayed menstruation, gynecomastia, breast swelling, breast enlargement, discharge from the breast, vaginal discharge, hypothermia, reduction body temperature, chest discomfort, induration, withdrawal syndrome. Not known: hyperinsulinaemia, lung stasis. Paliperidone is the active metabolite of Risperidone, which may result in side effects that have been observed with risperidone. When using antipsychotics may occur: QT prolongation, ventricular arrhythmia (ventricular fibrillation, ventricular tachycardia), sudden unexplained death, cardiac arrest andorsade de pointes. Cases of venous thromboembolism including cases of pulmonary embolism and deep vein thrombosis have also been reported - frequency unknown. There is a risk of intraoperative flaccid iris syndrome (IFIS) during cataract surgery in patients taking paliperidone.

Orally. Adults.Schizophrenia: 6 mg once a day, in the morning.It is not required to gradually increase the dose at the beginning of treatment. In some patients, it may be beneficial to use the drug in smaller or larger doses, in the range of 3-12 mg once a day. If dose adjustment is indicated, this should only be done after re-evaluating the patient's clinical condition. When the dose should be increased, it is recommended to increase it by 3 mg daily, at intervals of more than 5 days.Schizoaffective disorder: 6 mg once a day, in the morning. It is not required to gradually increase the dose at the beginning of treatment. Some patients may benefit from higher doses in the range of 6-12 mg once a day. If dose adjustment is indicated, this should only be done after re-evaluating the patient's clinical condition. When the dose should be increased, it is recommended to increase it by 3 mg daily, at intervals of more than 4 days. The persistence of clinical improvement has not been studied.Special groups of patients. There is no need to change the dosage in elderly patients if the kidney function is normal. The safety and efficacy of paliperidone in patients> 65 years with schizoaffective disorder has not been studied. No dose adjustment is required in patients with mild to moderate hepatic impairment; no data available for patients with severe hepatic impairment. In patients with mild renal impairment (CCr ≥50 to <80 ml / min), the recommended starting dose is 3 mg once a day and can be increased to 6 mg once a day based on clinical response and tolerability; in patients with moderate to severe renal impairment (CCr ≥ 10 to <50 ml / min), the recommended starting dose is 1.5 mg once a day and may be increased to 3 mg once a day after reassessment of the patient's clinical status; in patients with CCr <10 ml / min, paliperidone should not be used.
The tablets should be swallowed whole, they should not be chewed, divided or used. Drink with liquid. Take it in the morning and always in the same way: always on an empty stomach or always with breakfast.