Risperidone | Risolept Konsta bottle, 37.5 mg
Special Price
$147.44
Regular Price
$159.00
In stock
SKU
BID463179
Release form
Powder for preparing a suspension for intramuscular administration of prolonged action
Powder for preparing a suspension for intramuscular administration of prolonged action
Release form
Powder for preparing a suspension for intramuscular administration of prolonged action
packaging
1 bottle complete with solvent
Pharmacological Action
Risperidone is a selective monoaminergic antagonist. It has high affinity for serotonergic 5-HT2 receptors and dopaminergic D2 receptors. In addition, risperidone binds to β 1 -adrenergic receptors and, to a lesser extent, with H1-histaminergic and 2-adrenergic receptors. Risperidone does not bind to cholinergic receptors. Despite the fact that risperidone is a powerful antagonist of D2 receptors, due to which it improves the positive symptoms of schizophrenia, this drug, compared with typical antipsychotics, inhibits motor activity to a lesser extent and less often causes catalepsy. Due to the balanced central antagonism of serotonin and dopamine receptors, risperidone is less likely to cause extrapyramidal side effects and has a therapeutic effect on the negative and affective symptoms of schizophrenia.
Pharmacokinetics
Risperidone is metabolized by the isoenzyme CYP2D6 to 9-hydroxyrisperidone, which has the same pharmacological activity as risperidone itself. Risperidone and 9-hydroxyrisperidone form an active antipsychotic fraction. Another route of risperidone metabolism is N-dealkylation.
For fast metabolizers, the clearance of the active antipsychotic fraction and risperidone is 5 and 13.7 l / h, respectively, and for weak metabolizers - 3.2 and 3.3 l / h, respectively.
General characteristics of risperidone after injection to patients of Rispolept Konsta®
With a single i / m administration of Rispolept Konsta®, the risperidone release profile consists of a small initial phase.
The combination of risperidone release profile and dosing regimen (intramuscular injection once every 2 weeks) ensures maintenance of therapeutic risperidone concentrations in plasma. Therapeutic concentrations persist until the 4th - 6th week after the last injection of Rispolept Konsta®. The elimination phase ends approximately 7-8 weeks after the last injection.
Risperidone is completely absorbed from Rispolept Consta® suspension. Risperidone is rapidly distributed in body tissues. Vd is 1-2 l / kg. In plasma, risperidone binds to albumin and 1-acid glycoprotein. Communication with plasma proteins of risperidone is 90%, and 9-hydroxyrisperidone is 77%. After intramuscular injections of the Rispolept Konsta® preparation in doses of 25 or 50 mg once every 2 weeks, the average values of Cmin and Cmax in the plasma of the active antipsychotic fraction are 9.9–19.2 and 17.9–45.5 ng / ml, respectively. With this dosing regimen, the pharmacokinetics of risperidone is linear. In long-term use (12 months) in patients which once every 2 weeks were injected with Rispolept Konsta® in doses of 25-50 mg, cumulation of risperidone was not observed. A study of the use of a single dose of the oral form of risperidone showed higher plasma concentrations and reduced clearance of the active antipsychotic fraction by 30% in elderly patients and by 60% in patients with renal failure. The concentration of risperidone in plasma in patients with liver failure was normal, but the average value of the free fraction in plasma increased by 35%.
Indications
Treatment and prevention of schizophrenia and schizoaffective disorder.
Contraindications
- lactation (breastfeeding)
- children and adolescents under 18
- hypersensitivity to the drug Risolept Konsta.
Due to the alpha-adrenergic blocking activity of risperidone, patients may experience orthostatic hypotension, especially during the initial period of treatment, and therefore risperidone should be used with caution in patients with cardiovascular diseases (for example, heart failure, myocardial infarction, cardiac muscle conduction / e.g. AV block, dehydration, hypovolemia, or cerebrovascular disorder). In such patients, the dose must be increased gradually. With the continuation of clinically significant hypotension, it is necessary to assess the risk / benefit indicator of further treatment with Risolept Konsta.
Caution should be exercised when administering Risolept Konst to patients with Parkinson's disease (since, theoretically, risperidone can exacerbate this disease), as well as to patients with epilepsy.
Use during pregnancy and lactation
Safety of the drug Risolept Konst during pregnancy in humans has not been studied.
In experimental animal studies, risperidone did not have a direct toxic effect on the reproductive system, but caused some indirect effects mediated through prolactin and central nervous system. In none of the studies did risperidone have a teratogenic effect.
Thus, Risolept Konsta can be used during pregnancy only if the expected benefit of the therapy for the mother outweighs the potential risk to the fetus.
Since risperidone and 9-hydroxy-risperidone pass into breast milk, if you need to use the drug during lactation, you should stop breastfeeding.
Special instructions
In patients who have not previously received risperidone, it is recommended to determine the tolerance of oral dosage forms before proceeding with treatment with Risolept Konsta.
When using drugs that have the properties of antagonists of dopamine receptors, the occurrence of tardive dyskinesia, characterized by involuntary rhythmic movements (mainly of the tongue and / or face), was noted. When symptoms of tardive dyskinesia appear, consideration should be given to the abolition of Rispolept Konst, as well as all antipsychotic drugs used simultaneously.
When using classical antipsychotics, cases of the appearance of malignant antipsychotic syndrome (NSS) are described, which are characterized by hyperthermia, muscle rigidity, instability of the peripheral nervous system function, impaired consciousness and an increase in the level of CPK. In the case of the development of ZNS, it is necessary to cancel all antipsychotic drugs, including Risolept Konst (it should be borne in mind that after the last injection risperidone is present in the blood plasma for another 6 weeks).
Effect on the ability to drive vehicles and control mechanisms
Risperidone can reduce the speed of mental and physical reactions, therefore, during treatment, patients should avoid driving vehicles and other activities that require a high concentration of attention and speed of psychomotor reactions.
Composition
Active substance: risperidone (as extended release microgranules) 37.5 mg
Aux ogatelnye matter: lactic and glycolic acid copolymer - 619 mg (per 1 g of microbeads)
Solvent: sodium carmellose (40 MPa נs) - 22.5 mg polysorbate 20 - 1 mg sodium hydrogen phosphate dihydrate - 1.27 mg anhydrous citric acid - 1 mg sodium chloride - 6 mg sodium hydroxide - 0.54 mg water for injection - up to 1 ml
Dosage and administration
Rispolept Konsta is administered once every 2 weeks deeply in oil using a sterile needle attached to the syringe. Injections should be done alternately in the right and left buttocks. The drug can not be entered in / in!
Adults Risolept Konsta is administered at a dose of 25 mg IM once every 2 weeks. Some patients need higher doses - 37.5 mg or 50 mg. The maximum dose should not exceed 50 mg once every 2 weeks.
Within 3 weeks after the first administration of the Rispolept Konsta drug (i.e., prior to the onset of the drug), the patient should take an effective antipsychotic.
The dose of the drug can be increased no more than 1 time in 4 weeks. The effect of such a dose increase should be expected no earlier than 3 weeks after the first injection of the increased dose.
In elderly patients, the recommended dose is 25 mg IM once every 2 weeks. Within 3 weeks after the first administration of the Rispolept Konsta drug (i.e., before the drug begins), the patient should take an effective antipsychotic.
There is currently no data on the use of the Risolept Konsta in patients with impaired liver or kidney function. If you still need to use Risolept Konst in this category of patients, then in the first week it is recommended to take inside 500 μg of risperidone 2 times / day in the form of tablets or oral solution. During the second week, the patient can take 1 mg 2 times / day or 2 mg 1 time / day. If the patient tolerates an oral dose of at least 2 mg well, then 25 mg of the Rispolept Konsta drug can be administered IM once every 2 weeks.
Side effects of
Resolept Konsta in therapeutic doses causes the following adverse events:
Often (> 1/100) - weight gain (2.7 kg or more in 1 year), depression, increased fatigue and extrapyramidal symptoms. Against the background of taking Rispolept Konsta (in doses up to 50 mg), the incidence of extrapyramidal symptoms is similar to that in patients receiving placebo.
Rarely (> 0.1 / 100) - weight gain, increased irritability, sleep disturbances, apathy, decreased attention span, tardive dyskinesia, seizures, antipsychotic malignant syndrome, visual impairment, hypotension, tachycardia, fainting, skin rash, itching , peripheral edema, reaction at the injection site.
Symptoms of hyperprolactinemia, such as non-labor lactation, amenorrhea, gynecomastia, menstrual irregularities, sexual dysfunction, impaired ejaculation, decreased libido and impotence.
Hematologic disorders: increase or decrease in the number of leukocytes or platelets, increased activity of liver enzymes.
In addition, the following adverse events are possible: insomnia, agitation, anxiety, headache, constipation, abdominal pain, rhinitis, urinary incontinence, priapism, drowsiness, dizziness, dyspepsia, nausea, vomiting, disturbances in thermoregulation, as well as hypervolemia caused by polydipsia or ADH secretion syndrome. During treatment with Rispolept Konsta, cerebrovascular accident sometimes occurs. When treating with Rispolept Konsta, hyperglycemia or worsening of diabetes mellitus is very rarely observed.
Drug interaction
Risolept Konsta increases the severity of the inhibitory effect on the central nervous system of opioid analgesics, hypnotics, anxiolytics, tricyclic antidepressants, agents for general anesthesia, ethanol.
Konsta Resolept may weaken the effect of levodopa and other dopamine agonists.
It was found that carbamazepine reduces the plasma content of the active antipsychotic fraction of risperidone. Similar effects can cause other inducers of liver enzymes. After the cancellation of carbamazepine or other inducers of liver enzymes, the dose of Risolept Consta should be reviewed and, if necessary, reduced.
Phenothiazines, tricyclic antidepressants, and certain beta-blockers may decrease plasma risperidone concentrations.
With the simultaneous use of fluoxetine can increase the concentration of risperidone in plasma, but to a lesser extent the concentration of the active antipsychotic fraction.
Pharmaceutical Interactions
Risolept Konst should not be mixed or diluted with any other drugs or liquids other than the special solvent contained in the package.
Overdose
Overdosage with risperidone is less likely than with oral doses. When using oral forms, the following symptoms are possible: severe drowsiness, tachycardia, arterial hypotension, extrapyramidal symptoms in rare cases - an increase in QT interval.
Treatment: The airway should be kept open to maintain adequate oxygen supply and ventilation. ECG monitoring should be started immediately to identify possible cardiac arrhythmias.
The specific antidote is unknown. It is necessary to conduct symptomatic therapy aimed at maintaining the function of the CNS and cardiovascular system, as well as detoxification therapy. In case of severe extrapyramidal symptoms, anticholinergic drugs should be prescribed. Continuous medical monitoring and monitoring should continue until symptoms of overdose have disappeared.
Storage conditions
The product should be stored at 2 ° to 8 РC in a dark place away from children.
Shelf life
3 years.
Deystvuyushtee substance
Risperidone
Terms and conditions
prescription
dosage form
injection
Possible product names
Rispolept Konsta vial, 37.5 mg
RISPOLEPT KONSTA 0.0375 POR D / SUSP
RISPOLEPT DUST KONSTRUCT DISTANCE 075 INF + RAS-
RISPOLEPT KONSTA 0.0375 POR D / SUSP + DEVICE ALARIS
RISPOLEPT Konsta 37.5 mg No. 1 vial + solution (syringe 2 ml) +
Janssen Pharmaceutical N.V., Belgium
Powder for preparing a suspension for intramuscular administration of prolonged action
packaging
1 bottle complete with solvent
Pharmacological Action
Risperidone is a selective monoaminergic antagonist. It has high affinity for serotonergic 5-HT2 receptors and dopaminergic D2 receptors. In addition, risperidone binds to β 1 -adrenergic receptors and, to a lesser extent, with H1-histaminergic and 2-adrenergic receptors. Risperidone does not bind to cholinergic receptors. Despite the fact that risperidone is a powerful antagonist of D2 receptors, due to which it improves the positive symptoms of schizophrenia, this drug, compared with typical antipsychotics, inhibits motor activity to a lesser extent and less often causes catalepsy. Due to the balanced central antagonism of serotonin and dopamine receptors, risperidone is less likely to cause extrapyramidal side effects and has a therapeutic effect on the negative and affective symptoms of schizophrenia.
Pharmacokinetics
Risperidone is metabolized by the isoenzyme CYP2D6 to 9-hydroxyrisperidone, which has the same pharmacological activity as risperidone itself. Risperidone and 9-hydroxyrisperidone form an active antipsychotic fraction. Another route of risperidone metabolism is N-dealkylation.
For fast metabolizers, the clearance of the active antipsychotic fraction and risperidone is 5 and 13.7 l / h, respectively, and for weak metabolizers - 3.2 and 3.3 l / h, respectively.
General characteristics of risperidone after injection to patients of Rispolept Konsta®
With a single i / m administration of Rispolept Konsta®, the risperidone release profile consists of a small initial phase.
The combination of risperidone release profile and dosing regimen (intramuscular injection once every 2 weeks) ensures maintenance of therapeutic risperidone concentrations in plasma. Therapeutic concentrations persist until the 4th - 6th week after the last injection of Rispolept Konsta®. The elimination phase ends approximately 7-8 weeks after the last injection.
Risperidone is completely absorbed from Rispolept Consta® suspension. Risperidone is rapidly distributed in body tissues. Vd is 1-2 l / kg. In plasma, risperidone binds to albumin and 1-acid glycoprotein. Communication with plasma proteins of risperidone is 90%, and 9-hydroxyrisperidone is 77%. After intramuscular injections of the Rispolept Konsta® preparation in doses of 25 or 50 mg once every 2 weeks, the average values of Cmin and Cmax in the plasma of the active antipsychotic fraction are 9.9–19.2 and 17.9–45.5 ng / ml, respectively. With this dosing regimen, the pharmacokinetics of risperidone is linear. In long-term use (12 months) in patients which once every 2 weeks were injected with Rispolept Konsta® in doses of 25-50 mg, cumulation of risperidone was not observed. A study of the use of a single dose of the oral form of risperidone showed higher plasma concentrations and reduced clearance of the active antipsychotic fraction by 30% in elderly patients and by 60% in patients with renal failure. The concentration of risperidone in plasma in patients with liver failure was normal, but the average value of the free fraction in plasma increased by 35%.
Indications
Treatment and prevention of schizophrenia and schizoaffective disorder.
Contraindications
- lactation (breastfeeding)
- children and adolescents under 18
- hypersensitivity to the drug Risolept Konsta.
Due to the alpha-adrenergic blocking activity of risperidone, patients may experience orthostatic hypotension, especially during the initial period of treatment, and therefore risperidone should be used with caution in patients with cardiovascular diseases (for example, heart failure, myocardial infarction, cardiac muscle conduction / e.g. AV block, dehydration, hypovolemia, or cerebrovascular disorder). In such patients, the dose must be increased gradually. With the continuation of clinically significant hypotension, it is necessary to assess the risk / benefit indicator of further treatment with Risolept Konsta.
Caution should be exercised when administering Risolept Konst to patients with Parkinson's disease (since, theoretically, risperidone can exacerbate this disease), as well as to patients with epilepsy.
Use during pregnancy and lactation
Safety of the drug Risolept Konst during pregnancy in humans has not been studied.
In experimental animal studies, risperidone did not have a direct toxic effect on the reproductive system, but caused some indirect effects mediated through prolactin and central nervous system. In none of the studies did risperidone have a teratogenic effect.
Thus, Risolept Konsta can be used during pregnancy only if the expected benefit of the therapy for the mother outweighs the potential risk to the fetus.
Since risperidone and 9-hydroxy-risperidone pass into breast milk, if you need to use the drug during lactation, you should stop breastfeeding.
Special instructions
In patients who have not previously received risperidone, it is recommended to determine the tolerance of oral dosage forms before proceeding with treatment with Risolept Konsta.
When using drugs that have the properties of antagonists of dopamine receptors, the occurrence of tardive dyskinesia, characterized by involuntary rhythmic movements (mainly of the tongue and / or face), was noted. When symptoms of tardive dyskinesia appear, consideration should be given to the abolition of Rispolept Konst, as well as all antipsychotic drugs used simultaneously.
When using classical antipsychotics, cases of the appearance of malignant antipsychotic syndrome (NSS) are described, which are characterized by hyperthermia, muscle rigidity, instability of the peripheral nervous system function, impaired consciousness and an increase in the level of CPK. In the case of the development of ZNS, it is necessary to cancel all antipsychotic drugs, including Risolept Konst (it should be borne in mind that after the last injection risperidone is present in the blood plasma for another 6 weeks).
Effect on the ability to drive vehicles and control mechanisms
Risperidone can reduce the speed of mental and physical reactions, therefore, during treatment, patients should avoid driving vehicles and other activities that require a high concentration of attention and speed of psychomotor reactions.
Composition
Active substance: risperidone (as extended release microgranules) 37.5 mg
Aux ogatelnye matter: lactic and glycolic acid copolymer - 619 mg (per 1 g of microbeads)
Solvent: sodium carmellose (40 MPa נs) - 22.5 mg polysorbate 20 - 1 mg sodium hydrogen phosphate dihydrate - 1.27 mg anhydrous citric acid - 1 mg sodium chloride - 6 mg sodium hydroxide - 0.54 mg water for injection - up to 1 ml
Dosage and administration
Rispolept Konsta is administered once every 2 weeks deeply in oil using a sterile needle attached to the syringe. Injections should be done alternately in the right and left buttocks. The drug can not be entered in / in!
Adults Risolept Konsta is administered at a dose of 25 mg IM once every 2 weeks. Some patients need higher doses - 37.5 mg or 50 mg. The maximum dose should not exceed 50 mg once every 2 weeks.
Within 3 weeks after the first administration of the Rispolept Konsta drug (i.e., prior to the onset of the drug), the patient should take an effective antipsychotic.
The dose of the drug can be increased no more than 1 time in 4 weeks. The effect of such a dose increase should be expected no earlier than 3 weeks after the first injection of the increased dose.
In elderly patients, the recommended dose is 25 mg IM once every 2 weeks. Within 3 weeks after the first administration of the Rispolept Konsta drug (i.e., before the drug begins), the patient should take an effective antipsychotic.
There is currently no data on the use of the Risolept Konsta in patients with impaired liver or kidney function. If you still need to use Risolept Konst in this category of patients, then in the first week it is recommended to take inside 500 μg of risperidone 2 times / day in the form of tablets or oral solution. During the second week, the patient can take 1 mg 2 times / day or 2 mg 1 time / day. If the patient tolerates an oral dose of at least 2 mg well, then 25 mg of the Rispolept Konsta drug can be administered IM once every 2 weeks.
Side effects of
Resolept Konsta in therapeutic doses causes the following adverse events:
Often (> 1/100) - weight gain (2.7 kg or more in 1 year), depression, increased fatigue and extrapyramidal symptoms. Against the background of taking Rispolept Konsta (in doses up to 50 mg), the incidence of extrapyramidal symptoms is similar to that in patients receiving placebo.
Rarely (> 0.1 / 100) - weight gain, increased irritability, sleep disturbances, apathy, decreased attention span, tardive dyskinesia, seizures, antipsychotic malignant syndrome, visual impairment, hypotension, tachycardia, fainting, skin rash, itching , peripheral edema, reaction at the injection site.
Symptoms of hyperprolactinemia, such as non-labor lactation, amenorrhea, gynecomastia, menstrual irregularities, sexual dysfunction, impaired ejaculation, decreased libido and impotence.
Hematologic disorders: increase or decrease in the number of leukocytes or platelets, increased activity of liver enzymes.
In addition, the following adverse events are possible: insomnia, agitation, anxiety, headache, constipation, abdominal pain, rhinitis, urinary incontinence, priapism, drowsiness, dizziness, dyspepsia, nausea, vomiting, disturbances in thermoregulation, as well as hypervolemia caused by polydipsia or ADH secretion syndrome. During treatment with Rispolept Konsta, cerebrovascular accident sometimes occurs. When treating with Rispolept Konsta, hyperglycemia or worsening of diabetes mellitus is very rarely observed.
Drug interaction
Risolept Konsta increases the severity of the inhibitory effect on the central nervous system of opioid analgesics, hypnotics, anxiolytics, tricyclic antidepressants, agents for general anesthesia, ethanol.
Konsta Resolept may weaken the effect of levodopa and other dopamine agonists.
It was found that carbamazepine reduces the plasma content of the active antipsychotic fraction of risperidone. Similar effects can cause other inducers of liver enzymes. After the cancellation of carbamazepine or other inducers of liver enzymes, the dose of Risolept Consta should be reviewed and, if necessary, reduced.
Phenothiazines, tricyclic antidepressants, and certain beta-blockers may decrease plasma risperidone concentrations.
With the simultaneous use of fluoxetine can increase the concentration of risperidone in plasma, but to a lesser extent the concentration of the active antipsychotic fraction.
Pharmaceutical Interactions
Risolept Konst should not be mixed or diluted with any other drugs or liquids other than the special solvent contained in the package.
Overdose
Overdosage with risperidone is less likely than with oral doses. When using oral forms, the following symptoms are possible: severe drowsiness, tachycardia, arterial hypotension, extrapyramidal symptoms in rare cases - an increase in QT interval.
Treatment: The airway should be kept open to maintain adequate oxygen supply and ventilation. ECG monitoring should be started immediately to identify possible cardiac arrhythmias.
The specific antidote is unknown. It is necessary to conduct symptomatic therapy aimed at maintaining the function of the CNS and cardiovascular system, as well as detoxification therapy. In case of severe extrapyramidal symptoms, anticholinergic drugs should be prescribed. Continuous medical monitoring and monitoring should continue until symptoms of overdose have disappeared.
Storage conditions
The product should be stored at 2 ° to 8 РC in a dark place away from children.
Shelf life
3 years.
Deystvuyushtee substance
Risperidone
Terms and conditions
prescription
dosage form
injection
Possible product names
Rispolept Konsta vial, 37.5 mg
RISPOLEPT KONSTA 0.0375 POR D / SUSP
RISPOLEPT DUST KONSTRUCT DISTANCE 075 INF + RAS-
RISPOLEPT KONSTA 0.0375 POR D / SUSP + DEVICE ALARIS
RISPOLEPT Konsta 37.5 mg No. 1 vial + solution (syringe 2 ml) +
Janssen Pharmaceutical N.V., Belgium
Submit your review to Earn 10 Reward Points click here to login
Write Your Own Review