Xeplion

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Xeplion: instructions for use and reviews

1. Release form and composition
2. Pharmacological properties
3. Indications for use
4. Contraindications
5. Method of application and dosage
6. Side effects
7. Overdose
8. Special instructions
9. Application during pregnancy and lactation
10. Use in childhood
11. In case of impaired renal function
12. For violations of liver function
13. Use in the elderly
14. Drug interactions
15. Analogs
16. Terms and conditions of storage
17. Terms of dispensing from pharmacies
18. Reviews
19. Price in pharmacies

Latin name: Xeplion

ATX code: N05AX13

Active ingredient: paliperidone (Paliperidone)

Manufacturer: Janssen Pharmaceuticals N. V. (Janssen Pharmaceutica NV) (Belgium); Cilag (Switzerland)

Description and photo update: 2018-27-11

Prices in pharmacies: from 25,973 rubles.

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Suspension for intramuscular administration of prolonged action Kseplion

Xeplion is a neuroleptic drug used to treat schizophrenia and schizoaffective disorders.

Release form and composition

Dosage form - suspension for intramuscular (intramuscular) administration of prolonged action: white or almost white, without foreign inclusions (in a cardboard box 1 plastic pallet containing 1 syringe of 0.25; 0.5; 0.75; 1; 1, 5 ml complete with two needles for intramuscular injections into the deltoid and gluteus muscles, as well as instructions for using Xeplion).

Composition of 1 ml of suspension:

active substance: paliperidone - 100 mg (paliperidone palmitate - 156 mg);
auxiliary components: sodium hydrogen phosphate - 5 mg; sodium hydroxide - 2.84 mg; polysorbate 20 - 12 mg; polyethylene glycol 4000 - 30 mg; sodium dihydrogen phosphate monohydrate - 2.5 mg; citric acid monohydrate - 5 mg; water for injection - up to 1 ml.

Pharmacological properties

Pharmacodynamics

Paliperidone palmitate is the active substance of Xeplion, hydrolyzed to paliperidone, which is a centrally active antagonist of mainly serotonin 5-HT _2A receptors, as well as dopamine D ₂ receptors, histamine H ₁ receptors, α ₁ - and α ₂ -adrenergic receptors.

Paliperidone does not bind with β ₁ - and β ₂ -adrenoreceptors and m-cholinergic receptors. The pharmacological activity of the (+) and (-) enantiomers of paliperidone is qualitatively and quantitatively the same.

There is an assumption that the therapeutic efficacy of paliperidone in schizophrenia is associated with the combined blockade of D ₂ and 5-HT _2A receptors.

Pharmacokinetics

Due to its extremely low solubility in water, paliperidone palmitate after i / m administration in the systemic circulation is absorbed and dissolves slowly. After a single application, the plasma concentration of paliperidone increases gradually, and reaches a maximum for 13-14 and 13-17 days after injection into the deltoid and gluteal muscles, respectively. The release of the substance is detected on the first day and persists for at least 126 days. The release characteristics of the active substance and the dosage regimen of Xeplion ensure long-term maintenance of its therapeutic concentration.

With _max (maximum concentration) after a single application of 25–150 mg into the deltoid muscle is more than after injection into the gluteal muscle, on average by 28%. When the drug is injected into the deltoid muscle at the beginning of therapy (on the first day - 150 mg, on the eighth day - 100 mg), the therapeutic concentration of paliperidone is achieved faster than when injected into the gluteus muscle. Further on, the difference in exposure is less obvious.

The average ratio of C _max and C _ss (equilibrium concentration) of paliperidone after four doses of 100 mg in the gluteal and deltoid muscles are 1.8 and 2.2, respectively. AUC (area under the concentration-time curve) at doses of paliperidone in the range of 25 to 150 mg changed in proportion to the dose, and C _max at doses from 50 mg increased to a lesser extent than in proportion to the dose.

Median T _1/2 (half-life) of 25–150 mg paliperidone is in the range of 25–49 days.

After the introduction of Xeplion, the (-) - enantiomer of paliperidone is partially transformed into the (+) - enantiomer, the ratio of AUC (+) - and (-) - enantiomers is about 1.6 ÷ 1.8.

The apparent Vd (volume of distribution) of paliperidone in a population analysis is 391 L; the substance binds to plasma proteins by 74%.

After a single oral dose of 1 mg of ¹⁴ C-paliperidone with immediate release within 7 days, 59% of the administered dose (unchanged) is excreted in the urine. Thus, the drug is not significantly metabolized in the liver. In urine, about 80% of the introduced radioactivity is found, in feces - 11%.

None of the four known metabolic pathways of a substance - dehydrogenation, dealkylation, hydroxylation, cleavage of the benzisoxazole group - causes metabolism to exceed 6.5% of the administered dose. In the metabolism of paliperidone, a certain participation of CYP3A4 and CYP2D6 isoenzymes can be assumed, but there is no information confirming a significant effect of these isoenzymes on its metabolism. Population pharmacokinetic analysis after oral administration of the drug in patients with active / weak metabolism of CYP2D6 did not reveal a noticeable difference in clearance of paliperidone. Xeplion does not significantly inhibit the biotransformation of drugs by isoenzymes CYP3A4, CYP3A5, CYP1A2, CYP2A6, CYP2E1, CYP2D6.

During the research, it was found that paliperidone exhibits the properties of a P-glycoprotein substrate, and when using high concentrations, the properties of a weak inhibitor of P-glycoprotein. The clinical significance of this information has not been clarified, there are no corresponding data.

Plasma concentration of paliperidone, in general, during the period of loading after i / m administration of Xeplion is in the same range as after oral administration of prolonged-action drugs with the release of the active ingredient in a dose of 6-12 mg. Thanks to such a load scheme, the maintenance of the concentration of paliperidone in this range is ensured even at the end of the interdose interval (on the 8th and 36th day). Individual variability of pharmacokinetic processes after administration of Xeplion in different patients is less than after oral administration of prolonged-release paliperidone.

In patients with severely impaired liver function, the use of paliperidone has not been studied.

Features of the use of Xeplion in patients with impaired renal function:

mild: the dose should be reduced;
moderate and severe: Xeplion is not recommended to use.

The distribution was studied after a single oral dose of 3 mg of prolonged-release paliperidone. The excretion of the substance with a decrease in CC (creatinine clearance) was weakened:

50-80 ml / min: 32%;
30-50 ml / min: 64%;
10-30 ml / min: 71% increase.

As a result, the AUC _0-∞ in comparison with healthy volunteers increased by 1.5; 2.6 and 4.8 times, respectively. The recommended loading dose of paliperidone for such patients on the first and eighth days is 75 mg; after that, once every 4 weeks, 50 mg is administered.

In elderly patients, correction of the dosage regimen may be associated with an age-related decrease in CC.

Indications for use

schizophrenia: treatment and prevention of relapse;
schizoaffective disorders: as monotherapy or in combination with antidepressants and normotimics.

Contraindications

Absolute:

impaired renal function of moderate or severe degree (with CC <50 ml / min);
lactation period;
established hypersensitivity to risperidone (paliperidone is its active metabolite);
individual intolerance to the components of the drug.

Relative (Xeplion is prescribed under medical supervision):

cardiovascular diseases (heart failure, myocardial infarction or ischemia, cardiac conduction disorders), cerebrovascular accidents or conditions that predispose to a decrease in blood pressure (decrease in circulating blood volume, dehydration, antihypertensive therapy);
aggravated history of seizures or other conditions in which the seizure threshold may decrease;
conditions in which an increase in body temperature is possible, including severe physical exertion, dehydration, exposure to high ambient temperatures, drugs with m-anticholinergic activity;
aggravated history of arrhythmia or congenital prolongation of the QT interval or combination therapy with drugs that prolong the QT interval;
combined use with other drugs that affect the central nervous system and alcohol; paliperidone may weaken the effect of dopamine and levodopa agonists;
dementia, Parkinson's disease, or Lewy body dementia;
the alleged presence of prolactin-dependent tumors;
impaired renal (with CC 50–80 ml / min) and hepatic function;
dementia in elderly patients;
pregnancy.

Xeplion, instructions for use: method and dosage

If the patient has never taken oral paliperidone or oral / parenteral risperidone, it is recommended to determine the tolerance of oral paliperidone or risperidone for 2-7 days before the appointment of Xeplion.

In patients with mild to moderate severity of psychotic conditions, who previously had a response to therapy with paliperidone / risperidone in oral forms, Xeplion can be used without prior stabilization with oral drugs of this group.

It is recommended to start treatment with the introduction of a dose of 150 mg into the deltoid muscle. A week later, a dose of Xeplion of 100 mg is also injected into the deltoid muscle. Subsequently, supportive injections can be given into the gluteus or deltoid muscle.

The recommended maintenance dose for schizophrenia is 75 mg once a month.

In schizophrenia and schizoaffective disorder, the maintenance dose is determined by individual tolerance and / or efficacy and may be in the range of 25–150 mg. The 25 mg dose has not been studied in schizoaffective disorder.

The maintenance dose of Xeplion can be adjusted monthly. In this case, it is necessary to take into account the prolonged release of the active substance from paliperidone palmitate, since the effect of changing the dose can fully manifest itself only after a few months.

When the second loading dose cannot be administered 7 days after the first, it is possible to do so 4 days earlier / later. Similarly, in the future, if it is impossible to inject Xeplion monthly, the injection can be done 7 days earlier / later.

In cases where the second injection was not done on time (7 ± 4 days), it is recommended to resume therapy depending on the time that has passed since the first injection of Xeplion.

If less than 28 days have passed since the first injection, the patient should receive a second injection of 100 mg into the deltoid muscle as soon as possible. The third injection at a dose of 75 mg is injected into the gluteus or deltoid muscle 5 weeks after the first (excluding the time of the second injection). In the future, you should follow the monthly course of injections.

If 4-7 weeks have passed since the day of the first injection, therapy should be resumed by introducing two injections of 100 mg of Xeplion into the deltoid muscle, according to the following scheme:

first: introduced as soon as possible;
second: introduced after 7 days.

Then the therapy is carried out according to the standard scheme.

When more than 7 weeks have passed since the first injection, treatment should be started over.

If less than 6 weeks have passed since the last maintenance injection, the next injection should be given as soon as possible at the same dose as the previous one. After that, the drug is administered monthly.

If more than 6 weeks have passed since the last maintenance injection, Xeplion is administered according to one of two schemes:

Patients stabilized with a dose of 25-100 mg: Xeplion is injected into the deltoid muscle as soon as possible at the dose at which the patient's condition was stabilized before the injection was missed. The next injection into the deltoid muscle at the same dose is given a week later on the eighth day. The therapy is continued according to the standard scheme.
Patients stabilized with a 150 mg dose: Xeplion is injected into the deltoid muscle as soon as possible at a dose of 100 mg. The next injection into the deltoid muscle at a dose of 100 mg is given a week later on the eighth day. The therapy is continued according to the standard scheme.

If it is missed more than 6 months after the last maintenance injection, the therapy is restarted.

Xeplion can only be used intramuscularly (deep into the muscle). Only a medical professional should carry out the procedure. The entire dose is administered at one time, it cannot be divided into several injections.

The size of the needle for insertion into the deltoid muscle depends on the patient's body weight:

≥ 90 kg: long needle with gray body from the kit;
<90 kg: short needle with blue barrel from the kit.

Xeplion should be injected alternately into the right and left deltoid muscles.

For insertion into the gluteus maximus, it is recommended to use the long, gray-bodied needle from the kit. The drug should be injected alternately into the upper outer quadrant of the right and left gluteus muscles.

For patients with CC 50-80 ml / min, it is recommended to start using Xeplion with a dose of 100 and 75 mg on the first and eighth days, respectively (in the deltoid muscle). After 1 month, 50 mg is applied (in the gluteus or deltoid muscle). Further maintenance dose is in the range of 25–100 mg.

There is no systematic record of the transfer of patients with schizophrenia or schizoaffective disorder from other antipsychotics to paliperidone or about its combined use with other antipsychotics. Previously used oral antipsychotics at the beginning of the use of Xeplion can be gradually canceled.

If the patient has received injectable long-acting neuroleptics, they begin immediately with the use of a maintenance dose of paliperidone at the time of the next scheduled injection (the initial dose is not required in the first week of therapy).

For patients who have been stabilized with different doses of the suspension for intramuscular administration of prolonged action Rispolept Konsta, the equilibrium concentrations of the active ingredient can reach similar values during maintenance therapy with Xeplion once a month. If the last dose of Rispolept Konst administered every 2 weeks was 25; 37.5 and 50 mg, then Xeplion should be administered once a month at a dose of 50, 75 or 100 mg, respectively.

Cancellation of the previous antipsychotic is carried out in accordance with the instructions for use. When canceling Xeplion, the prolonged release of the active ingredient should be taken into account. As with the use of other antipsychotics, the need to continue therapy with the prevention of extrapyramidal disorders should be periodically assessed.

The suspension syringe is intended for single administration only. Before the procedure, it must be shaken for 10 seconds.

Side effects

During clinical studies, it was found that most often due to the use of Xeplion, drowsiness, sedation, constipation, nausea, abdominal pain, diarrhea, vomiting, dizziness, reactions at the injection site, anxiety, insomnia, headache, upper respiratory tract infections, parkinsonism develop, akathisia, weight gain, agitation, tachycardia, tremor, dystonia, fatigue, musculoskeletal pain. Dose-dependent of these disorders are drowsiness and sedation.

Most side effects were moderate or mild.

Possible adverse reactions [> 10% - very common; (> 1% and 0.1% and 0.01% and <0.1%) - rarely; <0.01% - very rare]:

immune system: infrequently - hypersensitivity; rarely - anaphylactic reactions;
hepatobiliary system: often - increased activity of hepatic transaminases; infrequently - an increase in the activity of liver enzymes and gamma-glutamyl transferase; rarely, jaundice;
respiratory system: often - nasal congestion, cough; infrequently - wheezing, pain in the pharyngeal-laryngeal region, dyspnea, epistaxis, pulmonary congestion; rarely - sleep apnea syndrome, aspiration pneumonia, dysphonia, hyperventilation, airway congestion;
cardiovascular system: often - tachycardia, bradycardia, increased blood pressure; infrequently - orthostatic hypotension, decreased blood pressure, conduction disturbance, atrioventricular block, abnormalities on the ECG, postural orthostatic tachycardia syndrome, increased QT interval on the ECG, palpitations, atrial fibrillation; rarely - sinus arrhythmia, hot flashes, ischemia, pulmonary embolism, deep vein thrombosis;
digestive system: often - nausea, dyspepsia, pain in the upper abdomen, diarrhea, constipation, toothache, vomiting; infrequently - gastroenteritis, flatulence, discomfort in the abdomen, dryness of the oral mucosa; rarely - intestinal obstruction, pancreatitis, fecal incontinence, dysphagia, cheilitis, fecal stones, tongue edema;
nervous system: very often - headache; often - drowsiness, dyskinesia, sedation, dystonia, tremor, parkinsonism, dizziness, akathisia, extrapyramidal symptoms; infrequently - psychomotor hyperactivity, dysgeusia, seizures (including epileptic seizures), paresthesia, distraction of attention, dysarthria, fainting, postural dizziness, hypesthesia, severe dyskinesia; rarely - loss of consciousness, diabetic coma, head tremors, imbalance, cerebral ischemia, neuroleptic malignant syndrome, decreased level of consciousness, lack of response to stimuli, impaired coordination;
reproductive system: infrequently - irregularities / delayed menstruation, amenorrhea, gynecomastia, vaginal discharge, galactorrhea, sexual / erectile dysfunction, ejaculation disorders; rarely - discharge from the mammary glands, enlargement / engorgement of the mammary glands, pain in the mammary glands, priapism, discomfort in the mammary glands;
urinary system: infrequently - urinary incontinence, pollakiuria, dysuria; rarely - delayed urinary excretion;
musculoskeletal system: often - pain in the limbs, back, musculoskeletal pain; infrequently - muscle spasms, arthralgia, neck pain, joint stiffness; rarely - postural disorder, increased creatine phosphokinase activity, muscle weakness, joint swelling, rhabdomyolysis;
psychiatric disorders: very often - insomnia; often - agitation, depression, anxiety; infrequently - sleep disturbance, decreased libido, nightmares, nervousness, mania, a state of confusion; rarely - emotional flattening, anorgasmia;
infections: often - influenza, infections of the upper respiratory tract and urinary system; infrequently - bronchitis, ear infections, eye infections, tonsillitis, sinusitis, subcutaneous abscess, cystitis, respiratory tract infections, pneumonia, inflammation of the subcutaneous fat, acarodermatitis; rarely - onychomycosis;
circulatory / lymphatic system: infrequently - a decrease in the number of white blood cells, an increase in the number of eosinophils, anemia, a decrease in hematocrit; rarely - neutropenia, thrombocytopenia, agranulocytosis;
endocrine system: often - hyperprolactinemia; rarely - inadequate secretion of antidiuretic hormone; with an unknown frequency - glucose in the urine;
metabolism: often - weight loss / gain, hyperglycemia, increased plasma triglyceride concentration; infrequently - diabetes mellitus, hyperinsulinemia, increased blood cholesterol concentration, anorexia, increased / decreased appetite; rarely - diabetic ketoacidosis, polydipsia, water intoxication, hypoglycemia;
senses: infrequently - conjunctivitis, blurred vision, vertigo, dry eyes, tinnitus, ear pain; rarely - rotatory nystagmus, involuntary movement of the eyeball, redness of the eyes, photophobia, glaucoma, increased lacrimation;
skin: often - skin rash; infrequently - urticaria, alopecia, erythema, acne, dry skin, eczema, itching; rarely - seborrheic dermatitis, drug rash, dandruff, skin discoloration, angioedema, hyperkeratosis;
others: often - asthenic disorders, weakness, fever, local reactions (in the form of pain, itching, induration at the injection site); infrequently - induration at the injection site, malaise, facial edema, chest pain, chest discomfort, gait disturbance, edema (including mild, peripheral and / or generalized edema), fall; rarely - hypothermia, chills, withdrawal syndrome in newborns, fever, decreased body temperature, thirst, cyst at the injection site, withdrawal syndrome, inflammation of the subcutaneous tissue, abscess and / or hematoma at the injection site.

Side effects reported with risperidone therapy (may occur when using Xeplion in addition to the above):

nervous system: impaired cerebral circulation;
respiratory system: wheezing;
organ of vision: intraoperative sagging iris syndrome;
violations at the injection site (observed when using the injectable form of risperidone) and general disorders: necrosis, ulcer at the injection site.

Most often, mild to moderate pain develops at the injection site. The frequency and intensity of pain syndrome decreases over time. Deltoid injections are a little more painful compared to gluteus injections. Other disorders at the injection site were mostly mild and included: often induration; infrequently - itching; rarely nodules.

Extrapyramidal symptoms include the following terms:

dyskinesia: dyskinesia, choreoathetosis, muscle twitching, myoclonus, athetosis;
parkinsonism: parkinsonian tremor at rest, hypokinesia, muscle rigidity, glabellar reflex disturbance, hypersalivation, musculoskeletal stiffness, parkinsonism, salivation, muscle tension, mask-like face, parkinsonian gait, bradykinesia, akinesia of the occipital muscles, rigidity of the occipital muscles, rigidity
dystonia: involuntary muscle contractions, convulsive clenching of the jaws, tongue spasm, dystonia, blepharospasm, tongue paralysis, facial spasm, laryngospasm, opisthotonus, pleurototonus, oropharyngeal spasm, myotonia, myogenic contracture, hypertension, torticollis, movement of the eyeball;
akathisia: hyperkinesia, restless legs syndrome, akathisia, restlessness;
tremor.

The list includes a wider range of symptoms that may not have an extrapyramidal etiology.

Weight gain is dose-dependent. When using placebo and doses of 25, 100 and 150 mg of Xeplion, this violation was noted with a frequency of 5, 6, 8 and 13%, respectively.

With antipsychotic therapy, prolongation of the QT interval, the occurrence of ventricular arrhythmias (ventricular fibrillation and tachycardia), tachycardia such as pirouette, cardiac arrest, and sudden unexplained death are possible. There is also evidence of cases of venous thromboembolism (with an unknown frequency), including deep vein thrombosis and pulmonary embolism.

Overdose

The likelihood of Xeplion overdose by patients is small, since the drug is administered by health workers.

The main symptoms are: an increase in the known pharmacological effects of paliperidone, including drowsiness, prolongation of the QT interval, tachycardia, lethargy, decreased blood pressure, extrapyramidal disorders. Overdose of oral paliperidone has been associated with ventricular fibrillation and polymorphic ventricular tachycardia such as pirouette.

In the event of an acute overdose, the likelihood of receiving multiple drugs must be considered.

To assess the need for therapy and recovery, the sustained release of the active substance and the prolonged T _{1/2 of} paliperidone should be taken into account.

Therapy: there is no specific antidote. It is shown to carry out general supportive measures, to ensure and maintain airway patency, sufficient ventilation of the lungs and oxygenation of the blood. Immediate monitoring of cardiovascular function is required, including continuous monitoring of the electrocardiogram (ECG), to detect possible arrhythmias. In case of circulatory collapse and a decrease in blood pressure, appropriate measures should be taken, for example, intravenous administration of sympathomimetics and / or solutions. In the case of severe extrapyramidal symptoms, anticholinergics are prescribed. Careful monitoring of the patient's condition is required until his full recovery.

special instructions

Xeplion is not recommended for patients with acute psychomotor agitation or in a severe psychotic state, when immediate control of symptoms is required.

Care must be taken when prescribing the drug against the background of cardiovascular diseases or prolongation of the QT interval in history, as well as when used in combination with drugs that can lead to prolongation of the QT interval.

There is information about the development of NMS (neuroleptic malignant syndrome) during the period of use of paliperidone. It is characterized by an increase in body temperature, muscle rigidity, instability of the autonomic nervous system, an increase in serum creatine phosphokinase concentration and impaired consciousness. It is also possible to develop myoglobinuria (rhabdomyolysis) and acute renal failure. If symptoms appear that suggest NMS, Xeplion is canceled.

The appearance of symptoms of tardive dyskinesia, which is characterized by rhythmic, involuntary movements, mainly of the facial muscles and / or tongue, require the abolition of Xeplion.

During post-registration observation, rare cases of the development of anaphylactic reactions were recorded in patients who had previously tolerated oral forms of paliperidone or risperidone. When hypersensitivity reactions appear, Xeplion must be canceled and the necessary supportive clinical measures must be taken. The condition is monitored until symptoms disappear.

Against the background of the use of the drug, there were cases of hyperglycemia, diabetes mellitus and exacerbation of existing diabetes mellitus. It is difficult to establish the relationship between the use of Xeplion and impaired glucose metabolism, which is associated with a high risk of diabetes mellitus in patients with schizophrenia and schizoaffective disorder, as well as with a wide prevalence of diabetes mellitus in the general population. All patients should be monitored for symptoms of diabetes mellitus and hyperglycemia.

There is information about a significant increase in weight during the period of use of Xeplion, and therefore control over the patient's body weight should be established.

When using paliperidone against the background of possible prolactin-dependent tumors, care must be taken, despite the fact that, so far, in epidemiological and clinical studies, a direct relationship between Xeplion therapy and breast tumor growth has not been demonstrated.

Paliperidone, possessing the activity of an α-blocker, in some patients can lead to the development of orthostatic hypotension. In this regard, Xeplion in patients with cardiovascular diseases, cerebrovascular accidents or conditions predisposing to a decrease in blood pressure should be prescribed with caution.

The use of Xeplion in elderly patients with dementia has not been studied. Paliperidone is an active metabolite of risperidone, therefore, the experience of therapy with these drugs should be taken into account. Among elderly patients with dementia taking risperidone, there was an increased mortality in patients taking furosemide and risperidone, compared with the group that took these drugs as monotherapy. The pathophysiological mechanisms explaining this observation have not been established. However, special care must be taken when prescribing Xeplion in such cases. The increase in mortality in patients simultaneously taking other diuretics together with risperidone was not found. Regardless of therapy, dehydration is a common risk factor for mortality, and elderly patients with dementia require careful monitoring.

When conducting placebo-controlled studies, it was found that the frequency of cerebrovascular accidents (transient and stroke), including fatal ones, in comparison with placebo, increased threefold in elderly patients with dementia who received some atypical antipsychotics, including risperidone, olanzapine, and aripiprazole. The mechanism of this phenomenon is unknown.

During the period of therapy, the development of leukopenia, neutropenia, agranulocytosis was noted. Agranulocytosis occurred in very rare cases during post-registration observations. For patients with a clinically significant decrease in the number of leukocytes in history or drug-dependent neutropenia / leukopenia during the first months of therapy, a complete blood count is recommended. In the absence of other possible causes, withdrawal of Xeplion should be considered at the first clinically significant decrease in the number of leukocytes. Patients with clinically significant neutropenia should be monitored for fever or symptoms of infection. If such signs occur, treatment should be started immediately. Patients with severe neutropenia (with an absolute neutrophil count of less than 1 × 10 ⁹/ l) until the number of leukocytes is normalized, Xeplion is canceled.

There is information about the development of venous thromboembolism. Since patients taking Xeplion often have a high likelihood of developing venous thromboembolism, all possible risk factors must be taken into account before and during therapy, and preventive measures should be taken if necessary.

Before prescribing Xeplion in patients with Parkinson's disease or dementia with Lewy bodies, the physician should assess the relationship between the benefits and risks of developing NMS, and the presence of hypersensitivity to antipsychotics. Possible manifestations of hypersensitivity: extrapyramidal symptoms, instability of posture with frequent falls, dullness of pain sensitivity, confusion.

There is information about the ability of Xeplion to induce priapism. Priapism was registered during post-marketing control of the drug use. If the symptoms of priapism do not disappear on their own within 3-4 hours, the patient should see a doctor.

Deterioration in the body's ability to lower body temperature may be associated with the use of Xeplion. Therefore, caution should be exercised in patients who may be exposed to an increase in body temperature.

In preclinical studies, paliperidone has been found to have antiemetic effects. This can mask the symptoms and signs of overdose of certain drugs or specific conditions, including bowel obstruction, brain tumor, or Reye's syndrome.

Care should be taken to avoid accidental ingestion of paliperidone into a blood vessel when using IM Xeplion.

The development of ISDR (intraoperative flabby iris syndrome) was noted during the operation for cataract in patients receiving Xeplion therapy. ISDR increases the risk of complications associated with the organ of vision during and after surgery. The potential benefit of canceling Xeplion before surgery has not been established. The physician should assess the risk associated with drug withdrawal.

Influence on the ability to drive vehicles and complex mechanisms

During the period of therapy, it is recommended to refrain from driving vehicles until the individual sensitivity to the action of Xeplion is determined.

Application during pregnancy and lactation

pregnancy: Xeplion can be used only in cases where the expected benefit outweighs the possible risk;
lactation period: the use of the drug is contraindicated.

The effect of Xeplion on labor and childbirth in humans has not been studied. If a woman took paliperidone in the third trimester of pregnancy, the newborn is likely to develop extrapyramidal disorders and / or varying degrees of severity of the withdrawal syndrome. Symptoms include hypertension, agitation, hypotension, drowsiness, tremors, breastfeeding, and respiratory distress.

It has been established that paliperidone passes into breast milk.

Pediatric use

Xeplion is not prescribed for patients under 18 years of age (safety profile has not been studied).

With impaired renal function

Application depending on QC:

50–80 ml / min: Xeplion is prescribed with caution;
<50 ml / min: therapy is not recommended.

For violations of liver function

The use of Xeplion in patients with severe hepatic impairment has not been studied, which requires caution when prescribing the drug.

Use in the elderly

Care should be taken when prescribing Xeplion to elderly patients with dementia.

Drug interactions

Paliperidone palmitate is hydrolyzed to paliperidone, therefore, when assessing the possibility of drug interactions, the results of studies of paliperidone for oral administration should be taken into account.

Possible interactions:

drugs that increase the QT interval, including antiarrhythmic drugs (procainamide, quinidine, amiodarone, disopyramide, sotalol), antihistamines, antipsychotic drugs (thioridazine, chlorpromazine); some medicines for malaria (mefloquine), antibiotics (moxifloxacin, gatifloxacin): the combination requires caution, since paliperidone can increase the QT interval;
centrally acting drugs, alcohol: increased effects on the central nervous system, the combination requires caution;
levodopa, dopamine receptor agonists: weakening of their effects, the combination requires caution;
drugs with the ability to cause orthostatic hypotension: an additive increase in this effect;
drugs that lower the seizure threshold (tramadol, mefloquine, butyrophenones, phenothiazines, selective serotonin reuptake inhibitors, tricyclic derivatives, etc.): the combination requires caution;
carbamazepine: decrease in average C _max and AUC of paliperidone; at the beginning of the use of carbamazepine, the dose of Xeplion should be reviewed and, if necessary, increased; when carbamazepine is canceled, the dose of paliperidone, on the contrary, may be increased;
divalproex sodium (in prolonged-release tablets): increase in C _max and AUC of paliperidone; when co-administered with valproate, based on the patient's clinical assessment, the possibility of reducing the dose of Xeplion may be considered;
risperidone, oral paliperidone: Long-term combined use requires caution.

There is limited information on the safety of the combined use of paliperidone and other antipsychotics.

Analogs

The analogues of Xeplion are: Invega, Trevikta, Risperidone Ozone, Rispolept, Risset, Torendo, etc.

Terms and conditions of storage

Store at temperatures up to 30 ° C. Keep out of the reach of children.

Shelf life is 2 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Xeplion

Reviews about Xeplion are few. Some patients are satisfied with both the effectiveness and tolerability of the drug. It has been reported to cause less sleepiness and less fatigue than other antipsychotics. In other cases, severe side effects are reported.

Price for Xeplion in pharmacies

The approximate price for Xeplion (1 syringe) is:

50 mg / ml - 9300-14,100 rubles;
75 mg / ml - 10,500–20,375 rubles;
100 mg / ml - 12,500-25,054 rubles;
150 mg / ml - 14,500–33,534 rubles.

Xeplion: prices in online pharmacies

Drug name

Price

Pharmacy

Xeplion 100 mg / ml suspension for intramuscular administration of prolonged action 1 ml 1 pc.

RUB 25,973

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Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!