Xeplion
In patients who have never taken paliperidone orally or risperidone orally or parenterally, before starting treatment with Xeplion, it is recommended to check the tolerability of paliperidone or risperidone when taken orally for 2-7 days.
It is recommended to begin treatment with Xeplion with a dose of 150 mg on day 1 and 100 mg after 1 week (both injections into the deltoid muscle). In the future, a dose of 75 mg once a month is recommended. The dose may be increased or decreased in the range of 25-150 mg depending on individual tolerability and/or effectiveness. After the second dose, subsequent injections can be given to the deltoid or gluteal muscle.
The maintenance dose can be adjusted monthly. In this case, the long-term release of the active component from paliperidone palmitate should be taken into account, since The effect of a dose change may take several months to become fully apparent.
Missing a dose
A second loading dose of paliperidone is recommended to be administered 1 week after the first dose. If this is not possible, then it can be introduced 2 days earlier or later. Likewise, the third and subsequent doses are recommended to be administered monthly, but if this is not possible, the injection can be given 7 days earlier or later.
If the second injection of Xeplion was not given on time (1 week ± 2 days), resumption of treatment is recommended depending on the time that has passed since the date of the first injection.
Missing the second initial dose (less than 4 weeks).
If less than 4 weeks 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 of Xeplion at a dose of 75 mg should be given into the deltoid or gluteal muscle 5 weeks after the first injection (not taking into account the time of the second injection). In the future, follow a monthly course of injections in a dose of 25 mg to 150 mg into the deltoid or gluteal muscle, depending on individual tolerance and/or effectiveness.
Missing the second initial dose (4 to
7
weeks).
If 4 to 7 weeks have passed since the first injection of Xeplion, treatment is resumed with 2 injections at a dose of 100 mg according to the following scheme: 1st injection into the deltoid muscle is given as soon as possible; after 1 week, a second injection is made into the deltoid muscle, then a monthly course of injections into the deltoid or gluteal muscle is continued in a dose of 25 mg to 150 mg, depending on individual tolerability and/or effectiveness.
Missing the second initial dose (more than 7 weeks).
If more than 7 weeks have passed since the first injection of Xeplion, treatment begins in the same way as in the case of initiation of treatment with Xeplion.
Missing a maintenance dose (from 1 month to 6 weeks).
After starting treatment, it is recommended to inject Xeplion monthly. If less than 6 weeks have passed since the last injection, then the next dose should be administered as soon as possible, equal to the previous one. After this, administer the drug monthly.
Missing a maintenance dose (> 6 weeks to 6 months).
If more than 6 weeks have passed since the last injection of Xeplion, the following is recommended.
For patients whose condition is stabilized using the drug at a dose of 25 mg to 100 mg:
1) inject the drug into the deltoid muscle as soon as possible at the dose at which the patient’s condition was stabilized before missing the injection;
2) the next injection is given into the deltoid muscle (the same dose) a week later on the 8th day;
3) then resume the monthly course of injections into the deltoid or gluteal muscle in a dose of 25 mg to 150 mg, depending on individual tolerability and/or effectiveness.
For patients whose condition is stabilized using the drug at a dose of 150 mg:
1) inject a dose of 100 mg into the deltoid muscle as soon as possible;
2) after 1 week, another dose of 100 mg is administered (day 8) into the deltoid muscle;
3) then resume the monthly course of injections into the deltoid or gluteal muscle in a dose of 25 mg to 150 mg, depending on individual tolerability and/or effectiveness.
Missing a maintenance dose (> 6 months).
If more than 6 months have passed since the last injection of Xeplion, then treatment is started again, as described above for starting treatment.
Transfer from other antipsychotics
Data on the transfer of patients with schizophrenia from other antipsychotics to Xeplion or its use simultaneously with other antipsychotics are not systematized. For patients who have never received oral paliperidone or oral or injectable risperidone, tolerability with oral paliperidone or oral risperidone should be assessed before initiating treatment with Xeplion. At the beginning of treatment with Xeplion, previously used orally administered antipsychotics can be discontinued. For patients receiving long-acting injectable antipsychotics, treatment with Xeplion begins immediately with a maintenance dose at the time of the next scheduled injection. Treatment with Xeplion should be continued once a month. An initial dose is not required in the first week of treatment.
In patients whose condition has been stabilized with various doses of the drug Rispolept Konsta®, a suspension for intramuscular administration of prolonged action, the Css of the active substance can reach similar values during maintenance therapy with the drug Xeplion 1 time/month according to the following scheme:
| Last dose of Rispolept Consta® | Initial dose of Xeplion |
| 25 mg every 2 weeks | 50 mg 1 time/month |
| 37.5 mg every 2 weeks | 75 mg 1 time/month |
| 50 mg every 2 weeks | 100 mg 1 time/month |
Cancellation of the previous antipsychotic should be carried out in accordance with the instructions for medical use. When discontinuing the drug Xeplion, the prolonged release of the active component should be taken into account. As with other antipsychotics, the need for continued use of agents to prevent the development of extrapyramidal disorders should be periodically assessed.
Concomitant use of paliperidone palmitate and oral paliperidone or oral or parenteral risperidone has not been studied. Since paliperidone is the main active metabolite of risperidone, the possibility of additive effects of paliperidone should be considered when using these drugs simultaneously with Xeplion.
Use in special patient groups
In patients with impaired liver function
the use of Xeplion has not been studied.
Based on the results of the oral paliperidone study,
no dosage adjustment is required
patients with mild to moderate hepatic impairment The use of Xeplion in patients with severe liver dysfunction
has not been studied.
The use of Xeplion in patients with impaired renal function has not been systematically studied. In patients with mild renal impairment (creatinine clearance ≥ 50 to < 80 ml/min)
It is recommended to start using Xeplion with a dose of 100 mg on day 1 and 75 mg after 1 week (both injections into the deltoid muscle).
After this, after 1 month, 50 mg is administered monthly into the deltoid or gluteal muscle, and then the dose is changed from 25 mg to 100 mg depending on individual tolerability and/or effectiveness. Xeplion is not recommended for use in patients with moderate or severe renal impairment (creatinine clearance <50 ml/min).
Elderly patients
with normal renal function, the same dose of Xeplion is recommended as for younger patients with normal renal function. In elderly patients, renal function may be reduced, and the above recommendations for patients with impaired renal function apply to such patients.
Safety and effectiveness of the drug Xeplion in children and adolescents under 18 years of age
has not been studied.
No dose adjustment of Xeplion is required depending on gender, race of patients and smoking.
Rules for using the drug
Xeplion is intended for intramuscular administration only. The drug is slowly injected deep into the muscle. Injections should only be administered by a medical professional. The entire dose is administered at one time; Do not administer the dose in multiple injections. The drug should not be injected into blood vessels or subcutaneously. Accidental entry into a blood vessel should be avoided. To do this, before starting to administer the drug, the syringe plunger is pulled back to check whether the needle has entered a large blood vessel. If blood enters the syringe, the needle and syringe should be removed from the muscle and disposed of.
The recommended needle size for administering Xeplion into the deltoid muscle is determined by the patient's body weight. For patients weighing ≥90 kg, the long, gray barrel needle included in the kit is recommended. For patients weighing <90 kg, the short needle with the blue body from the kit is recommended. The drug should be injected alternately into the right and left deltoid muscles.
To inject Xeplion into the gluteal muscle, a long needle with a gray body from the kit is recommended. Injections should be made into the upper outer quadrant of the buttock. The drug should be injected alternately into the right and left gluteal muscles.
Administration of the drug
The syringe is intended for single administration only.
1. Shake the syringe vigorously for 10 seconds to obtain a homogeneous suspension.
2. Select the appropriate needle.
For insertion into the deltoid muscle,
patients weighing <90 kg
use a short needle (blue body), and
patients weighing > 90 kg
use a long needle (gray body).
For injection into the gluteal muscle
use a long needle (with a gray body).
3. Holding the syringe vertically, remove the rubber cap by gently rotating it clockwise.
4. Open the safety needle package halfway, grasp the needle cap through the package and insert the syringe into the luer lock needle cap by gently rotating clockwise.
5. Remove the cap from the needle by pulling it along the needle. Do not rotate the cap, because this may loosen the connection between the needle and the syringe.
6. Point the syringe with the needle upward and squeeze the air out of the syringe by lightly pressing the plunger.
7. Inject the entire contents of the syringe into the selected muscle (deltoid or gluteal). Do not inject the drug into a blood vessel or subcutaneously.
8. After completing the injection, bring the needle guard into working position with your thumb or forefinger or by pressing the syringe against a hard surface. The needle guard should click into place. The syringe with needle should be destroyed in accordance with the requirements.
Contraindications
Contraindications to the use of the drug Xeplion are: hypersensitivity to paliperidone or any component of the drug; patients with known hypersensitivity to risperidone (since paliperidone is an active metabolite of risperidone).
With caution: - Orthostatic hypotension. Having alpha-blocker activity, paliperidone can cause orthostatic hypotension in some patients. Xeplion should be used with caution in patients with cardiovascular diseases (for example, heart failure, myocardial infarction or ischemia, cardiac conduction disorders), cerebrovascular accidents, or conditions predisposing to a decrease in blood pressure (for example, dehydration, a decrease in blood volume, the use of antihypertensive drugs). - Cramps. Like other antipsychotics, Xeplion should be used with caution in patients with a history of seizures or other conditions that may lower the seizure threshold. - Regulation of body temperature. The use of antipsychotics is associated with a deterioration in the body's ability to reduce body temperature. It is recommended to exercise caution when prescribing Xeplion to patients who may be exposed to exposures that increase body temperature, such as intense physical activity, high ambient temperatures, exposure to drugs with m-anticholinergic activity, and dehydration. - QT interval. As with other antipsychotics, caution should be exercised when prescribing Xeplion to patients with a history of arrhythmia or congenital prolongation of the QT interval, or taking drugs that prolong the QT interval. - Given the effect of paliperidone on the central nervous system, Xeplion should be used with caution in combination with other drugs acting on the central nervous system and alcohol. Paliperidone may reduce the effect of levodopa and dopamine agonists. - Caution should be exercised when prescribing Xeplion to elderly patients with dementia, patients with Parkinson's disease or dementia with Lewy bodies.
Directions for use and dosage
