Zalasta

Zalasta is an antipsychotic whose active ingredient is olanzapine.

Indications Zalasta

Antipsychotic drug, which has the appropriate indications for the application of Zalast:

• Schizophrenia (in adult patients). Includes treatment for exacerbation of the disease; supportive therapy; preventive use, directed to prevent recurrence of the disease.
• A wide range of psychological disorders:
  • Automatism.
  • Hallucinations.
  • The decline of social activity.
  • Emotional impoverishment.
  • Narrowing of the verbal stock of words.
• Manic-depressive syndrome.

[1], [2]

Release form

The drug is widely represented in the pharmacy market. There is a form of output of this nature:

• tablets coated with a coating at a dosage of 2.5 - 5.0 - 7.5 - 10 - 15 and 20 mg of the drug, respectively.
• lyophilizate, a product obtained as a result of the lyophilization process (drying the sample in a vacuum under strong cooling), used hereinafter as the base for the preparation of injection solutions (for intramuscular administration).

[3]

Pharmacodynamics

Active active substance olanzapine is an excellent neuroleptic. Pharmacodynamics Zalasta differs developed pharmacologically active zone of sensitivity. The drug Zalasta, due to its antipsychotic effects on the patient's body, blocks the work of metabotropic receptors (namely, dopamine), which play one of the most important roles in the adequate functioning of the central nervous system. Also, the medication in question has sedative properties that allow the killing of receptors causing adrenaline bursts of brain stem cell cell formations. Zalasta effectively blocks the function of the receptors of the hypothalamus, the zone of the vomiting center, and also affects some serotonin receptors.

Due to active action on the corresponding receptor cells, olanzapine effectively removes such symptoms of psychosis as: the appearance of hallucinations in the patient, suspicion, social autism, delirium, emotional alienation and hostility.

Pharmacokinetics

Suction characteristics. Pharmacokinetics Zalasta has a high adsorption capacity. His characteristics are not related to the time and amount of food taken. When taken orally, the peak amount of active ingredient in the plasma is formed in five to eight hours (after taking the drug), falling within the range of 7 to 1000 ng of the drug per ml of blood, while the ability of olanzapine to bind the protein is 93%, which, you will agree, a sufficiently high level of penetration.

Metabolism and excretion of the drug from the body. Zalasta is easily metabolized in the liver, while not forming active metabolites. A noticeable effect on half-life and plasma clearance (an indicator of the rate of purification of blood plasma from foreign substances) has the sex of the patient, his age qualification and such negative habits as smoking:

• if the patient falls below the age of 65 years, the half-life of the drug is 51.8 hours, with a plasma clearance of 17.5 liters / hour.
• in persons younger than 65 years, the half-life is 33.8 hours, the clearance is 18.2 l / h.

The numerical value of plasma clearance is also decreasing in patients suffering from impaired liver function. However, the effect of these factors on half-life and clearance is less noticeable, in contrast to the individual characteristics of the patient's body.

Approximately 60% of the injected Zalasta preparation is excreted by the kidneys with urine in the form of metabolites.

[4], [5]

Dosing and administration

The recommended starting dosage of the drug Zalasta is 10-15 mg. In the future, the daily dose of the drug is calculated for each patient purely individually (depending on the condition of the patient and general clinic of the disease). The average therapeutic dosage taken is between 5 mg and 20 mg daily. When clinically necessary, after a thorough examination, the dose can be raised relative to the starting dose by 10-15 mg (per day). The growth of the dosage is carried out gradually, maintaining the time intervals before the next rise in 24 hours.

The mode of administration and dose for elderly patients, especially if they suffer from hepatic or renal insufficiency, in acute or moderate manifestation, are somewhat different. The starting dosage corresponds to 5 mg per day.

If there is a possibility of a decrease in the patient's metabolic processes, the total daily dosage of Zalast should be reduced. If you walk through the symptoms, then the recommended daily dosage looks like this:

• In schizophrenia, the amount of olanzapine is 10 mg.
• with manic-depressive syndrome: starting dose - 15 mg (once with monotherapy) and 10 mg (as part of complex treatment). Prophylactic dosage is 10 mg at a time in a day.

Also, women need a dose of Zalasta slightly less than the representatives of the stronger sex. Changes in the amount of the drug to a non-smoking patient, compared to a patient who has this bad habit, is not required.

[8]

Use Zalasta during pregnancy

Based on a small experience, the use of Zalast during pregnancy and during breastfeeding should be minimized as much as possible. It is only the doctor who is entitled to prescribe him in the treatment and only in cases when the expected effect of taking the drug clearly outweighs the negative impact that the drug has on a young woman or her child. Therefore, the future mother must necessarily warn the doctor about his "interesting situation" or planned pregnancy.

There are some cases when some deviations were observed in a pregnant or newborn baby:

• Arterial hypertension.
• A small tremor.
• Drowsiness in children who were born to mothers who take Zalasta in the last trimester of pregnancy.
• Lethargy.

Due to the ease with which olanzapine is absorbed into the body and fluid forms of the body, it also falls into the breast milk, therefore, during the period of treatment with the drug Zalasta, it is necessary to stop breastfeeding the baby.

Contraindications

Any medical drug must be taken with great care. Has also contra-indications to application of Zalasta:

• Individual hypersensitivity to active substances, including olanzapine, or other components of the drug.
• The period of pregnancy and breast-feeding.
• Babies and teenagers under 18 years.
• Risk of occlusive glaucoma.
• Not so often, but nevertheless there is a hereditary pathology, expressed in intolerance of galactose.

It is necessary to take with special caution the Zalasta with its active substance olanzapine, in case the patient has a history: •

• Epilepsy.
• Neutropenia (decrease in the level of neutrophils in the blood).
• Pathology of kidney function.
• Leukopenia (decrease in the content of leukocytes in peripheral blood).
• Liver failure.
• Pathology of the prostate gland.
• Intestinal obstruction.
• Congestive heart failure.
• Old age.
• Arterial hypotension.
• And some other diseases.

[6]

Side effects Zalasta

The use of the drug in question is associated with a fairly wide range of abnormalities.

Side effects of Zalast are represented by such manifestations as:

Central nervous system:

• Severe headaches and migraines.
• Decreased general vitality and dizziness.
• Insomnia or drowsiness.
• Hostility and anxiety.
• Depersonalization.
• Hemorrhage and stroke.
• Neuralgia.
• Tremor and stammering.
• Coma.
• And others.

The cardiovascular system:

• Tachycardia and bradycardia.
• Hemorrhagic syndrome.
• Cardiac arrest.
• Shift in the indication of the electrocardiogram.
• Leukocytosis.
• And another pathology.

Allergic manifestations - hives.

Respiratory system:

• Voice defects.
• The cough becomes more strained.
• Laryngitis and pharyngitis.
• Rhinitis and bronchial asthma.
• And others.

Gastrointestinal tract:

• Inadequate appetite growth, often leading to bulimia.
• Activation of the salivary glands.
• Dryness of the oral mucosa and thirst.
• Gastritis.

Gingivitis and stomatitis.

• Nausea, resulting in vomiting.
• Bleeding rectal.
• Diarrhea, problems with retention of feces and constipation.
• And other manifestations.

Genitourinary system:

• Cystitis (inflammation of the bladder).
• Pathology of urination.
• Pain in the mammary glands.
• Urinary tract infection.
• Fibrosis of the uterus.
• Premenstrual syndrome.
• Impotence in men and ejaculation in women.
• And other violations.

Exchange processes:

• Diabetes.
• Coma of a diabetic genesis.
• Struma (an increase in the size of the thyroid gland or as it is also called - goiter).
• Growth, less often a decrease, the body weight of the patient.
• And other changes.

Skin system:

• Dryness of the epidermis.
• Ulcerative lesion of the epidermis.
• Contact dermatitis.
• Change of skin color.
• Eczema and seborrhea (violation of the secretory function of sebaceous glands).
• And others.

Musculoskeletal system:

• Arthritis (inflammation in the joints).
• Pain in the bones.
• Appearance of cramps in the calf muscles.
• Bursitis (inflammation of the synovial bag).
• Arthralgia (the appearance of pain in the joint).

Myasthenia gravis and myopathy.

Other systemic manifestations:

• Fever and chills.
• Pain in the abdomen and chest.
• Symptoms similar to influenza.
• Lymphadenopathy (lymph node enlargement).
• Puffiness.
• And many others.

[7]

Overdose

At vital indications to introduction in an organism of the patient of antipsychotic preparation Zalasta, it is necessary precisely to maintain a dose of reception and intervals between them. Overdose of the drug is fraught with many dangerous consequences.

• Severe tachycardia.
• Falling blood pressure.
• Delirium (darkened state of consciousness).
• A surge of excitement and aggression.
• Convulsions.
• The inhibition of the patient's consciousness, in the worst of its manifestations - a coma.
• Dysarthria (disorder of articulate speech).
• Less common malignant neuroleptic syndrome (CNS).
• It is rare, but nevertheless there is a lack of cardiopulmonary activity.

Clinical observations revealed the lowest dosage of olanzapine, which can lead to death - this corresponds to 450 mg daily, although a maximum overdose of the Zalasta drug was also recorded, at which the patient managed to survive - this figure corresponds to 1500 mg.

The sequence of treatment for an overdose of the drug in question is as follows:

• It is urgently necessary to carry out measures for gastric lavage, it is not recommended to initiate a gag reflex in this situation.
• Take activated charcoal at the rate of one tablet per ten kilograms of the patient's weight. This procedure will reduce the bioavailability of the active substance of the drug Zalast by approximately 60%.
• It is impossible in this situation to introduce into the patient's body various sympathomimetics, since they can worsen a patient's condition and cause arterial hypotension.
• It is necessary to constantly control the breath, up to the artificial ventilation of the lungs.
• Constant monitoring of all vital organs.
• Then there is a direct treatment of the symptoms, which is manifested due to the intake of a large amount of olanzapine.
• Until the patient completely leaves this condition, the patient must be under constant supervision of the attending physician.
• The only antidote that would have coped with all the overdose manifestations does not exist.

[9]

Interactions with other drugs

At any use of combined treatment, it is necessary to remember that interactions of Zalast with other drugs are ambiguous and can give both a positive therapeutic effect and negative consequences.

The rate of withdrawal of the active substance olanzapine increases if the patient smokes, and with simultaneous admission and carbamazepine, the activation of the isoenzyme CYP1A2 is observed, which can significantly affect the metabolism of Zalast.

As already mentioned above, the use of activated carbon significantly blocks the bioavailability of the antipsychotic. The joint administration of olanzapine and ethanol is fairly neutral and does not significantly affect the pharmacokinetics of the drugs, only a positive effect of ethanol on sedative abilities of Zalast is observed.

If, in parallel with the drug in question, 60 mg is administered once, or in the same dosage daily for eight days of fluoxetine, then physicians observe approximately a 16% increase in the maximum concentration of the active substance of plasma gelatine. At the same time, by the same 16%, the clearance decreases, which does not significantly affect the clinical picture of treatment and does not require correction of the amount of the drug administered.

Joint use of Zalast with fluvoxamine decreases the clearance of olanzapine, increasing its maximum concentration in the blood. At the same time, the figures obtained by monitoring the situation are quite impressive: for non-smokers, the increase is 54%, for non-smokers this figure is even higher - 77%. In such patients, the growth of AUC olanzapine is also observed at 5 and 108%, respectively. For obvious reasons, in this case, it is necessary to reduce the dosage of olanzapine.

Valproic acid has no significant effect on olanzapine metabolism, while Zalasta inhibits, albeit insignificantly, the processes of reproduction of valproic acid, glucuronide, which is the basis of metabolic processes in the body.

With a joint protocol for taking the medication in question and biperidene or lithium-containing drugs, there was no significant change in the clinical picture. It is necessary to apply the preparation Zalast very carefully and with preparations having the characteristics of the central action.

Despite the fact that the influence of small doses of alcohol on the work of olanzapine has not been revealed, it is still worthwhile to abstain from its consumption during the period of Zalasta intake (depending on the individual characteristics of the patient's organism, a depressive symptom may be manifested).

[10], [11]

Storage conditions

Olanzapine should be located in a place that would not be accessible to young children and adolescents, otherwise the storage conditions of Zalasta are simple: the temperature in the room should not exceed 25 ° C.

[12],

Shelf life

A five-year shelf life is a fairly good period of effective work of the drug. This shelf life is on Zalast packs with a dosage of 5 mg and 10 mg. Tablets with a dose of 2.5 mg, 7.5 mg, 15 mg and 20 mg do not waste their medicinal qualities for three years.