Olanzapine-canon pills coated 10 mg n28
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Description
Antipsychotic drug
Composition
olanzapine 10 mg
Excipients: low substituted hyprolosis - 3.5 mg, calcium hydrogen phosphate - 58 mg, croscarmellose sodium - 1.5 mg, mannitol - 75.5 mg, magnesium stearate - 1.5 mg.
The composition of the film shell: opadry II yellow 5 mg, including polyvinyl alcohol 2 mg, macrogol 1.01 mg, talc 0.74 mg, titanium dioxide 1.175 mg, iron dye yellow oxide 0.075 mg.
Excipients: low substituted hyprolosis - 3.5 mg, calcium hydrogen phosphate - 58 mg, croscarmellose sodium - 1.5 mg, mannitol - 75.5 mg, magnesium stearate - 1.5 mg.
The composition of the film shell: opadry II yellow 5 mg, including polyvinyl alcohol 2 mg, macrogol 1.01 mg, talc 0.74 mg, titanium dioxide 1.175 mg, iron dye yellow oxide 0.075 mg.
Pharmacological effect
Antipsychotic (neuroleptic). Possesses affinity for serotonin 5-HT2A / C-, 5-НТ3-, 5-НТ6-receptors, dopamine D1-, D2-, D3-, D4-, D5-receptors, M1-5-cholinergic receptors, α1-adrenergic receptors and histamine H1 receptors. Shows antagonism against serotonin 5-NT-, dopamine and cholinergic receptors.
In vitro and in vivo, it has a more pronounced affinity and activity for serotonin 5-HT2 receptors, compared with dopamine D2 receptors. According to electrophysiological studies, olanzapine selectively reduces the excitability of mesolimbic (A10) dopaminergic neurons and, at the same time, has little effect on striatal (A9) nerve pathways involved in the regulation of motor functions. Olanzapine reduces the conditioned defense reflex (a test that characterizes antipsychotic activity) at lower doses than is required to achieve catalepsy (a disorder reflecting a side effect on motor function). Unlike other neuroleptics, olanzapine increases the anti-anxiety effect when conducting anxiolytic test.
With the use of olanzapine, both productive (including delusions, hallucinations) and negative disorders are reduced.
In vitro and in vivo, it has a more pronounced affinity and activity for serotonin 5-HT2 receptors, compared with dopamine D2 receptors. According to electrophysiological studies, olanzapine selectively reduces the excitability of mesolimbic (A10) dopaminergic neurons and, at the same time, has little effect on striatal (A9) nerve pathways involved in the regulation of motor functions. Olanzapine reduces the conditioned defense reflex (a test that characterizes antipsychotic activity) at lower doses than is required to achieve catalepsy (a disorder reflecting a side effect on motor function). Unlike other neuroleptics, olanzapine increases the anti-anxiety effect when conducting anxiolytic test.
With the use of olanzapine, both productive (including delusions, hallucinations) and negative disorders are reduced.
Pharmacokinetics
After oral administration, olanzapine is well absorbed from the gastrointestinal tract, plasma Cmax is reached after 5-8 hours. Plasma concentrations of olanzapine are linearly dose-dependent (ranging from 1 to 20 mg). Eating does not affect the absorption of olanzapine.
At plasma concentrations from 7 to 1000 ng / ml, plasma protein binding is about 93%.
Olanzapine is metabolized in the liver by conjugation and oxidation. The major circulating metabolite is 10-N-glucuronide, which theoretically does not penetrate the BBB. CYP1A2 and CYP2D6 isoenzymes are involved in the formation of N-desmethyl and 2-hydroxymethyl metabolites of olanzapine.Experimental studies in animals have shown that these metabolites have a significantly less pronounced pharmacological activity in vivo than olanzapine. The main pharmacological activity is due to unchanged olanzapine.
CYP2D6 isoenzyme activity does not affect the level of olanzapine metabolism.
In healthy volunteers after oral administration, T1 / 2 of olanzapine is 33 h (21-54 h), and the average plasma clearance is 26 l / h (12-47 l / h).
About 57% of olanzapine labeled with radioisotopes is excreted in the urine, mainly in the form of metabolites.
Pharmacokinetic indicators of olanzapine vary depending on gender, age, and smoking addiction:
Characteristics of patients T1 / 2 (h) Plasma clearance (l / h)
Nonsmoking 38.6 18.6
Smokers 30.4 27.7
Women 36.7 18.9
Men 32.3 27.3
Elderly (65 years and older) 51.8 17.5
Younger than 65 years old 33.8 18.2
However, the degree of changes in T1 / 2 and plasma clearance under the influence of each of these factors is significantly inferior to the degree of individual differences of these indicators.
Significant differences between the mean T1 / 2 and plasma clearance of olanzapine in patients with severe impaired renal function, compared with those with normal renal function, have not been established.
In smokers with minor hepatic impairment, plasma clearance of olanzapine is lower than in non-smokers without such disorders.
At plasma concentrations from 7 to 1000 ng / ml, plasma protein binding is about 93%.
Olanzapine is metabolized in the liver by conjugation and oxidation. The major circulating metabolite is 10-N-glucuronide, which theoretically does not penetrate the BBB. CYP1A2 and CYP2D6 isoenzymes are involved in the formation of N-desmethyl and 2-hydroxymethyl metabolites of olanzapine.Experimental studies in animals have shown that these metabolites have a significantly less pronounced pharmacological activity in vivo than olanzapine. The main pharmacological activity is due to unchanged olanzapine.
CYP2D6 isoenzyme activity does not affect the level of olanzapine metabolism.
In healthy volunteers after oral administration, T1 / 2 of olanzapine is 33 h (21-54 h), and the average plasma clearance is 26 l / h (12-47 l / h).
About 57% of olanzapine labeled with radioisotopes is excreted in the urine, mainly in the form of metabolites.
Pharmacokinetic indicators of olanzapine vary depending on gender, age, and smoking addiction:
Characteristics of patients T1 / 2 (h) Plasma clearance (l / h)
Nonsmoking 38.6 18.6
Smokers 30.4 27.7
Women 36.7 18.9
Men 32.3 27.3
Elderly (65 years and older) 51.8 17.5
Younger than 65 years old 33.8 18.2
However, the degree of changes in T1 / 2 and plasma clearance under the influence of each of these factors is significantly inferior to the degree of individual differences of these indicators.
Significant differences between the mean T1 / 2 and plasma clearance of olanzapine in patients with severe impaired renal function, compared with those with normal renal function, have not been established.
In smokers with minor hepatic impairment, plasma clearance of olanzapine is lower than in non-smokers without such disorders.
Indications
Treatment of exacerbations, supportive and long-term anti-relapsing therapy for schizophrenia and other psychotic disorders with pronounced productive (including delusions, hallucinations, automatism) and / or negative (including emotional flattening, decrease in social activity, impoverishment of speech) symptoms, as well as concomitant affective disorders.
Treatment of acute manic or mixed episodes in bipolar affective disorder with / without psychotic manifestations and with / without rapid phase change.
Treatment of acute manic or mixed episodes in bipolar affective disorder with / without psychotic manifestations and with / without rapid phase change.
Contraindications
Hypersensitivity to olanzapine.
Precautionary measures
Application for violations of the liver
In case of insufficiency of the liver function of moderate severity, the initial dose is 5 mg / day.
Application for violations of kidney function
In severe renal failure, the initial dose is 5 mg / day.
Use in children
The safety and efficacy of olanzapine in patients under the age of 18 years have not been studied.
Use in elderly patients
For elderly patients, the initial dose is 5 mg / day.
In case of insufficiency of the liver function of moderate severity, the initial dose is 5 mg / day.
Application for violations of kidney function
In severe renal failure, the initial dose is 5 mg / day.
Use in children
The safety and efficacy of olanzapine in patients under the age of 18 years have not been studied.
Use in elderly patients
For elderly patients, the initial dose is 5 mg / day.
Dosage and administration
The method of application and the dosage regimen of a particular drug depend on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly observe the compliance of the used dosage form of a particular preparation with the indications for use and the dosage regimen.
The initial dose is 10-15 mg / day. The daily dose must be selected individually depending on the clinical condition of the patient. Therapeutic doses - 5-20 mg / day. Increasing the dose over the standard component (depending on the evidence) 10-15 mg / day is recommended only after an appropriate clinical examination of the patient. The dose should be increased gradually, at intervals of at least 24 hours.
For elderly patients, as well as severe renal failure or liver failure of moderate severity, the initial dose is 5 mg / day.
A reduction in the initial dose is recommended for patients with a combination of factors (female patients, senile patients, non-smokers) who may slow down the metabolism of olanzapine.
The initial dose is 10-15 mg / day. The daily dose must be selected individually depending on the clinical condition of the patient. Therapeutic doses - 5-20 mg / day. Increasing the dose over the standard component (depending on the evidence) 10-15 mg / day is recommended only after an appropriate clinical examination of the patient. The dose should be increased gradually, at intervals of at least 24 hours.
For elderly patients, as well as severe renal failure or liver failure of moderate severity, the initial dose is 5 mg / day.
A reduction in the initial dose is recommended for patients with a combination of factors (female patients, senile patients, non-smokers) who may slow down the metabolism of olanzapine.
Side effects
On the part of the central nervous system: disturbance of gait (in patients with dementia of the Alzheimer's type), drowsiness, akathisia, dizziness, rarely convulsive seizures, ZNS.
On the part of metabolism: weight gain, peripheral edema.
On the part of the endocrine system: an increase in prolactin content (clinical manifestations of hyperprolactinemia were rarely noted, in most cases, normalization of prolactin levels occurred without discontinuation of olanzapine), in rare cases - hyperglycemia, diabetic coma, diabetic ketoacidosis.
Since the cardiovascular system: orthostatic hypotension, rarely - bradycardia.
On the part of the digestive system: constipation, dry mouth, increased appetite, increased activity of ALT and AST, rarely - hepatitis.
Dermatological reactions: rarely - photosensitivity, rash.
From the genitourinary system: rarely - priapism.
On the part of the blood system: eosinophilia, rarely - leukopenia, thrombocytopenia.
Other: asthenia.
On the part of metabolism: weight gain, peripheral edema.
On the part of the endocrine system: an increase in prolactin content (clinical manifestations of hyperprolactinemia were rarely noted, in most cases, normalization of prolactin levels occurred without discontinuation of olanzapine), in rare cases - hyperglycemia, diabetic coma, diabetic ketoacidosis.
Since the cardiovascular system: orthostatic hypotension, rarely - bradycardia.
On the part of the digestive system: constipation, dry mouth, increased appetite, increased activity of ALT and AST, rarely - hepatitis.
Dermatological reactions: rarely - photosensitivity, rash.
From the genitourinary system: rarely - priapism.
On the part of the blood system: eosinophilia, rarely - leukopenia, thrombocytopenia.
Other: asthenia.
Interaction with other drugs
With simultaneous use with drugs that have a depressant effect on the central nervous system, with ethanol increases the inhibitory effect on the central nervous system, antihypertensive effect.
The metabolism of olanzapine can be altered by the action of inhibitors or inducers of the CYP1A2 isoenzyme. Plasma clearance of olanzapine is increased in smoking patients and in patients taking carbamazepine (due to increased activity of CYP1A2). Strong inhibitors of CYP1A2 can reduce the plasma clearance of olanzapine.
The simultaneous intake of activated carbon reduces the bioavailability of olanzapine by 50-60%.
With simultaneous use with fluvoxamine increases the concentration of olanzapine in the blood plasma.
Taking fluoxetine (60 mg once or 60 mg daily for 8 days) causes an increase in plasma Cmax of olanzapine by an average of 16% and a decrease in plasma clearance of olanzapine by an average of 16%.
The metabolism of olanzapine can be altered by the action of inhibitors or inducers of the CYP1A2 isoenzyme. Plasma clearance of olanzapine is increased in smoking patients and in patients taking carbamazepine (due to increased activity of CYP1A2). Strong inhibitors of CYP1A2 can reduce the plasma clearance of olanzapine.
The simultaneous intake of activated carbon reduces the bioavailability of olanzapine by 50-60%.
With simultaneous use with fluvoxamine increases the concentration of olanzapine in the blood plasma.
Taking fluoxetine (60 mg once or 60 mg daily for 8 days) causes an increase in plasma Cmax of olanzapine by an average of 16% and a decrease in plasma clearance of olanzapine by an average of 16%.