Nykob 5mg Genepharm SA tablets treat schizophrenia (4 blisters x 7 tablets)

In preclinical studies, olanzapine has affinity (KI;

olanzapine has a stronger affinity with the receptor of Serotonin SHT2 on in vitro compared to D2 and the activity of 5HT2 on in Vivo is stronger than D2 activity. Physiological electrophoresis studies have shown that olanzapine selectively reduces the activation of dopaminergic nerve cells in Mesolimbic (A10), but has little effect on movement (49) in motor function.

olanzapine reduces conditional avoidance response, is a test that determines the anti -psychotic effect when taking lower doses than the dose that causes the remedy, is a side effect on motor function.

Unlike some other anti -psychotic drugs, olanzapine causes an increase in response in a test that reduces anxiety. "

In a single oral dosage study (10 mg) using a Positron (PET) method of healthy volunteers, Olanzapine occupies the SHT2A receptor than the Dopamine D2 receptor.

Moreover, an image study uses a method of cutting a single phroton transmission (specter) in schizophrenic mental illness showing that people who respond to olanzapine occupy the D2 of the body is still less than those who respond to Risperidone and some other anticonvol drugs, but equivalent to those who respond to clozapine.

Both of the two verified tests and two of the three tests are verified by the comparative substance over 2,900 schizophrenia patients with both positive and negative symptoms, seeing olanzapine significantly improved positive as well as negative symptoms.

in children

Experience treatment in teenagers (from 13-17 years old) is limited to treatment for less than 200 patients and only data on short-term effectiveness with schizophrenia (6 weeks) and Hung Cam have bipolar disorder (3 weeks).

olanzapine is used in flexible dose from 2.5 to 20mg/day.

During treatment, patients of adolescents gain weight faster than adults. Changes in total cholesterol index, ldl cholesterol, triglycerides and prolactin in teenagers are more than changes in adults. No effective and safe data when long -term treatment.

Pharmacokinetics

absorption

olanzapine absorbs well when drinking, reaching the top concentration of plasma within 5 to 8 hours.

Food does not affect absorption. The absolute oral use has not been determined compared to the vein. Olanzapine concentration in plasma is linear and proportional to the dose in research tests with the dose of 1 to 20mg.

Distribution

About 93% olanzapine connects to plasma proteins when concentrations from 7 - 1000ng/ml.

olanzapine is mainly linked to albumin and al-acid-glycoprotein.

Metabolism

olanzapine is metabolized in the liver through a conjugate and oxidative mechanism. The main metabolite is 10-N-Glucuronide, and does not pass through the brain barrier. Cytochrom P450- CYP1A2 and P450-CYP2D6 are involved in the creation of N-Destrethyl and 2-Hydroxylylyl metabolites.

Both of these metabolites have a much lower pharmacological activity on Vivo.

compared to olanzapine in animal studies. Pharmacological effects are mainly caused by mother medicine.

Elimination

After oral use, the average selling time in healthy people varies depending on age and gender. After drinking in healthy people, the average selling time is 33 hours (21 - 54 hours for the 5th to 95th branch) and the average plasma clearance of olanzapine is 26L/hour (12 to 47L/hour for the 5th to 95th branch).

In the elderly (65 and higher) healthy compared to young people, the average selling time is extended (51.8 compared to 33.8 hours) and reduced clearance (17.5 compared to 18.2 l/hour).

Pharmacokinetic changes in the elderly are still within the scope of changes of young people. In 44 people with schizophrenia (65 years), the dose is from 5 - 20mg/day there is no difference in side effects.

In women compared to men, the average selling time is extended (36.7 compared to 32.3 hours) and the clearance decreases (18.9 compared to 27.3 l/hour). However, the safety of olanzapine (5 - 20mg) is similar in female patients (n = 467) and men (n = 869).

Renal failure: There is no significant difference in the average selling time (37.7 compared to 32.4) or clearance (21.2 compared to 25.0L/hour) of olanzapine between kidney failure (creatinine clearance

olanzapine is not prescribed treatment in children and minors under 18 years of age. Although no clinical studies are designed to compare teenagers with adults, data from teenagers tested has been compared to these large data.

Metabolism and nutrition:

Be cautious when used

The accompanying diseases: Olanzapine has anti -anti -anti -Vitro, but in clinical trials, relevant symptoms appear at a low rate. Due to the clinical experience using olanzapine in patients with the accompanying diseases is small, carefully when indicating olanzapine for patients with prostate hypertrophy, intestinal obstruction, or related conditions.

Mental disorders are related to behavioral disorders

olanzapine is not approved to treat mental disorders related to memory loss or behavioral disorder due to an increase in mortality and the risk of stroke.

Parkinson's disease

The use of olanzapine in the treatment of mental disorders associated with dopamine agents in patients with Parkinson's disease is not recommended,

Hyperglycemia and diabetes

Need to monitor clinical indicators in accordance with the instructions for anti -psychotic drugs, for example: measuring blood sugar at the beginning of treatment, 12 weeks after treatment with olanzapine and each year later.

Patients treated with any anti -psychotic agent, including olanzapine, should be checked for signs and symptoms of hyperglycemia (or thirst, urination, eating a lot and fatigue) and patients with diabetes or there are risk factors for diabetes to be monitored regularly to control blood sugar.

Need to monitor weight regularly, for example: at the beginning of treatment, 4, 8 and 12 weeks after the beginning of olanzapine treatment and every 4 months later.

Lipid metabolic disorders

Lipid metabolism disorders have been observed in Planzapine treatment patients in placebo clinical trials. Lipid changes should be monitored in an appropriate way, especially in patients with dyslipidemia and in patients with risk factors for the development of lipid disorders.

Patients treated with any anti -psychotic drugs, including olanzapine, should be monitored regularly in the lipid index in accordance with the instructions for anti -psychotic drugs, for example at the beginning of treatment, 12 weeks after treatment with olanzapine and every 5 years later.

Liver function

The liver enzymes Transaminase, ALT, AST sometimes increase fleeting, no symptoms, especially in the early stages of the treatment. Be careful to monitor patients with an increase in ALT or/and AST, patients with signs and symptoms of liver failure, patients have limited liver function status and patients taking drugs that are toxic to the liver.

In case of increasing ALT and/or AST during treatment, it is necessary to monitor and consider reducing the dose.

leukopenia

Like other anti -psychotic drugs, be careful when taking olanzapine in patients with low number of white blood cells and/or neutrophils due to any causes, patients with a history of inhibiting bone marrow poisoning due to drugs, patients with bone marrow inhibitors due to accompanying diseases, radiation therapy or chemotherapy, and patients with eosinatic hypernage or osteoporosis.

Malignant neuropular syndrome

Malignant neuroleptic syndrome is a potentially life -threatening condition, related to anti -psychotic drug treatment. Rarely report on cases of malignant neuron syndrome related to olanzapine.

The clinical manifestations of malignant neuropular syndrome are high fever, muscle stiffness, mental status that changes, and has an unstable manifestation of plant nervous systems (circuits or uneven blood pressure, tachycardia, sweating, arrhythmia). Other signs include increased creatinine phosphokinase, myoglobin urine (pattern pepper), and acute renal failure.

Need to stop all anti -psychotic drugs, including olanzapine, when the patient has symptoms and symptoms of malignant neurolithic syndrome or when there is no high fever of unknown cause without the light of the malignant neuroleptic syndrome.

epilepsy

Be careful when using olanzapine in patients with a history of epilepsy or have factors that reduce epilepsy threshold, epilepsy rarely occur in patients when treated with planzapine. Most of these patients have a history of epilepsy or risk factors for epilepsy.

Late movement

In comparative studies for 1 year or less, the rate of dysplasia complications in patients when treating olanzapine lower statistical significance.

However, the risk of dysplasia wants to increase when taking anti -psychotic drugs for a long time, so it is necessary to reduce the dose or stop the drug when there are signs or symptoms. Symptoms of late dysplasia may worsen over time or even appear after treatment.

Central nervous system activity

micro olanzapine has the main effect on the central nervous system, so be careful when used in combination with other drugs that also act on the central nervous system and alcohol. Because olanzapine represents antagonism with dopamine on in vitro, olanzapine may be opposed to the effect of indirect and direct dopamine agents.

HA posture blood pressure

rarely occurs in older people in Olanzapine clinical experiences. As well as for other anti -psychotic drugs, blood pressure should be measured periodically in patients over 65 years old.

Disorders of OT

In clinical trials, olanzapine is not related to an absolute increase in QT interval.

There are only 8 out of 1685 subjects with an increase in QT in many cases. However, like other anti -psychotic drugs, it is careful to prescribe olanzapine along with known drugs to increase the QT range, especially in the elderly.

Stop taking medicine

Symptoms such as sweating, insomnia, tremor, anxiety, nausea, or vomiting appear at a dangerous rate ( thrombosis

Venous thrombosis related to the time of treatment has been reported at a common rate (≥ 0.1% and

Sudden cardiac arrest

In the after -sales report, when treating Planzapine, there were cases of a patient who sudden death due to the heart stopped working. In a pure observation, rescue study, the risk of sudden death due to heart occurred in patients treated with planzapine is twice as high as in patients without anti -psychotic drugs.

lactose

This drug contains lactose monohydrate. Patients with rare genetic problems are galactose intolerance, lactase deficiency or glucose-galactose tolerance should not be taken.

aspartame

This drug product contains aspartam. Can be harmful to patients with urinary phenylketon.

The ability to reproduce, pregnant and lactating

There is no adequate and accurate data on the effects of drugs on pregnant women. Patients should be recommended to consult a doctor if pregnant during the use of the drug. Because of the limited treatment experience, olanzapine should only be used if the benefits are superior to the risk of the fetus.

For babies that mothers use psychotic drugs during the third pregnancy, there is a risk of side effects including: extracurricular reactions at different levels. There have been reports of excitement, increasing tone, reducing tone, tremor, drowsiness, respiratory failure, eating disorders. Therefore, these babies should be carefully monitored.

breastfeeding:

In a healthy and lactating woman's study, olanzapine is excreted in breast milk. The level of contact with olanzapine (mg/kg) in children in a stable period is about 1.8% of the mother's doses. Therefore, patients are advised not to breastfeed during treatment with olanzapine.

The ability to drive and operate machinery

There has been no research on the effects of the drug on the ability to drive and operate machinery, but because Planzapine can cause dreamy and drowsiness, patients need to be careful when driving or operating machinery.

Interactive drug

drugs at risk of interaction

Because olanzapine is metabolized by CYP1A2, substances that have the ability to touch or inhibit the specific enzyme system are capable of affecting the pharmacokinetics of olanzapine.

CYPLA2 induction

Data on clinical consequences of interactions is limited, but clinical monitoring is recommended and may increase the dose of olanzapine if necessary.

CYP1A2 inhibitors

Fluvoxamin, a specific CYPIA2 inhibitor, has shown the ability to inhibit olan metabolism.

After using fluvoxamine, the average peak concentration of olanzapine increased by 54% in non -smoking male patients and 77% in male patients with smoking. Olanzapine's AUC increased by 52% in non -smoking people and 108% in smoking patients.

Patients are using flovoxamine or other CYP1A2 inhibitors, should use olanzapine at lower starting dose. Can reduce the dose if necessary.

Reduce bioavailability

Activated carbon reduces the bioavailability of oral olanzapine by 50 - 60% and should be used at least 2 hours before or after using olanzapine.

Ability to affect other drugs of olanzapine

olanzapine may be opposed to the enhanced effect of direct, indirect dopamine.

olanzapine does not inhibit the main enzyme of the CYP450 system on in vitro (for example, 1A2, 2D6, 2C9, 219, 3A4). Therefore, Olanzapine has no special interaction and does not inhibit the metabolic process of the following active substances: Triple -round antidepressants (mainly represented by CYP2D6), Warfarin (CYP2C9), Theophylline (CYP1A2), or diazepam (CYP3A4 and 2019).

There is no interaction when using olanzapine together with lithium or pitcher.

Monitoring of plasma valproate levels shows no need to adjust the valproate dose when used with olanzapine.

Central neurological inhibition activity

Be careful in patients with alcohol or are taking central neurological inhibitors.

Concomitance the use of olanzapine with anti -Parkinson drugs in Parkinson's patients and memory loss is not recommended.

About QT adjustment

Be cautious if olanzapine is being used simultaneously with drugs that can increase the adjustment range of QT.