Zalasta

Zalasta is a neuroleptic drug whose active ingredient is olanzapine.

Indications Zalasta

Antipsychotic drug that has the corresponding indications for use of Zalasta:

• Schizophrenia (in adult patients). Includes treatment during an exacerbation of the disease; maintenance therapy; prophylactic use aimed at preventing relapses of the disease.
• A wide range of psychological disorders:
  • Automatism.
  • Hallucinations.
  • Decline in social activity.
  • Emotional impoverishment.
  • Narrowing of vocabulary.
• Manic-depressive syndrome.

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Release form

The drug is widely represented on the pharmacy market. It is available in the following forms:

• film-coated tablets in dosages of 2.5 – 5.0 – 7.5 – 10 – 15 and 20 mg of the drug, respectively.
• lyophilisate, a product obtained as a result of the lyophilization process (drying a sample in a vacuum with strong cooling), used subsequently as a basis for the preparation of injection solutions (for intramuscular administration).

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Pharmacodynamics

The active ingredient olanzapine is an excellent neuroleptic. Pharmacodynamics Zalasta is characterized by an expanded pharmacologically active sensitivity zone. The drug Zalasta, due to its antipsychotic effect 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 drug in question has sedative properties that allow you to stop the receptors that cause adrenaline surges in the cellular formations of the brain stem. Zalasta allows you to effectively block the function of the hypothalamus receptors, the vomiting center zone, and also affects some serotonin receptors.

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

Pharmacokinetics

Absorption characteristics. Pharmacokinetics Zalasta is characterized by high adsorption capacity. Its characteristics are not related to the time and amount of food taken. When taken orally, the peak amount of the active substance 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 protein is 93%, which, you will agree, is a fairly high figure for the level of penetration.

Metabolism and elimination of the drug from the body. Zalasta is easily metabolized in the liver, without forming active metabolites. The half-life and plasma clearance (an indicator of the rate of blood plasma purification from foreign substances) are significantly affected by the patient's gender, age, and such negative habits as smoking:

• If the patient is over 65 years of age, the half-life of the drug is 51.8 hours, while the plasma clearance is 17.5 l/hour.
• in people under 65 years of age, the half-life is already 33.8 hours, clearance is 18.2 l/hour.

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

Approximately 60% of the administered Zalasta is excreted in the urine as metabolites.

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Dosing and administration

The recommended starting dose of Zalasta is 10-15 mg. The daily dose is then calculated for each patient individually (depending on the patient's condition and the general clinical picture of the disease). The average therapeutic dose is taken within the range of 5 mg to 20 mg daily. If clinically necessary, after a thorough examination, the dose can be increased relative to the starting dose by 10-15 mg (per day). The dose is increased gradually, maintaining time intervals of 24 hours before the next increase.

The method of administration and dosage for elderly patients, especially if they suffer from liver or kidney failure, in acute or moderate form of manifestation, are somewhat different. The starting dosage is 5 mg per day.

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

• For schizophrenia, the amount of olanzapine is 10 mg.
• for manic-depressive syndrome: starting dose - 15 mg (once for monotherapy) and 10 mg (as part of complex treatment). Preventive dosage - 10 mg once a day.

Women also need a slightly smaller dosage of Zalasta than men. A non-smoking patient does not need to change the amount of the drug compared to a patient who has this bad habit.

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Use Zalasta during pregnancy

Based on limited experience, the use of Zalast during pregnancy and breastfeeding should be limited as much as possible. Only the attending physician has the right to prescribe it for treatment and only in cases where the expected effect of taking the medication clearly outweighs the negative impact that the drug has on the young woman or her child. Therefore, the expectant mother must necessarily notify the doctor about her "interesting situation" or planned pregnancy.

There are known isolated cases where a pregnant woman or a newborn baby had some abnormalities:

• Arterial hypertension.
• Slight tremor.
• Drowsiness in babies born to mothers taking Zalasta in the last trimester of pregnancy.
• Lethargy.

Due to the ease with which olanzapine is absorbed into the tissue and fluid forms of the body, it, accordingly, also gets into breast milk, therefore, during the course of treatment with Zalasta, breastfeeding should be discontinued.

Contraindications

Any medical drug should be taken with great caution. There are also contraindications to the use of Zalasta:

• Individual hypersensitivity to active substances, including olanzapine, or other components of the medication.
• The period of pregnancy and breastfeeding.
• Children and teenagers up to 18 years old.
• Risk of developing angle-closure glaucoma.
• Not so often, but still there is a hereditary pathology expressed in galactose intolerance.

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

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

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Side effects Zalasta

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

Side effects of Zalasta 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 stuttering.
• Coma.
• And others.

Cardiovascular system:

• Tachycardia and bradycardia.
• Hemorrhagic syndrome.
• Cardiac arrest.
• Shift in electrocardiogram readings.
• Leukocytosis.
• And other pathology.

Allergic manifestations - urticaria.

Respiratory system:

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

Gastrointestinal tract:

• Inappropriate increase in appetite, often leading to bulimia.
• Activation of the salivary glands.
• Dryness of the oral mucosa and thirst.
• Gastritis.

Gingivitis and stomatitis.

• Nausea leading to vomiting.
• Rectal bleeding.
• Diarrhea, problems with stool retention and constipation.
• And other manifestations.

Urogenital system:

• Cystitis (inflammation of the bladder).
• Pathology of urination.
• Pain in the mammary glands.
• Urinary tract infection.
• Uterine fibrosis.
• Premenstrual syndrome.
• Impotence in men and ejaculatory dysfunction in women.
• And other violations.

Exchange processes:

• Diabetes mellitus.
• Coma of diabetic origin.
• Struma (enlargement of the thyroid gland or as it is also called - goiter).
• Increase, or less commonly, decrease, in the patient's body weight.
• And other changes.

Skin system:

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

Musculoskeletal system:

• Arthritis (inflammation of the joints).
• Bone pain.
• The appearance of cramps in the calf muscles.
• Bursitis (inflammation of the synovial bursa).
• Arthralgia (the appearance of pain in the joint).

Myasthenia and myopathy.

Other systemic manifestations:

• Fever and chills.
• Pain in the abdomen and chest.
• Flu-like symptoms.
• Lymphadenopathy (enlarged lymph node).
• Swelling.
• And many others.

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Overdose

In case of vital indications for the introduction of the antipsychotic drug Zalasta into the patient's body, it is necessary to strictly adhere to the dose and intervals between them. An overdose of the drug is fraught with many dangerous consequences.

• Severe tachycardia.
• Drop in blood pressure.
• Delirium (clouded state of consciousness).
• A surge of excitement and aggression.
• Convulsions.
• Inhibition of the patient's consciousness, in its worst manifestations - coma.
• Dysarthria (disorder of articulate speech).
• Less common is neuroleptic malignant syndrome (NMS).
• Quite rarely, but cardiopulmonary insufficiency still occurs.

Clinical observations have also revealed the lowest dosage of olanzapine that can lead to death - this corresponds to a daily dose of 450 mg, although the maximum overdose of the drug Zalasta was also recorded, in 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 gastric lavage; initiating the gag reflex in this situation is not recommended.
• Take activated carbon 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 Zalasta by approximately 60%.
• In such a situation, it is impossible to introduce various sympathomimetics into the patient’s body, as they can worsen the patient’s condition and cause arterial hypotension.
• It is necessary to constantly monitor breathing, up to and including artificial ventilation.
• Continuous monitoring of all vital organs.
• Next comes targeted treatment of the symptoms that have appeared as a result of taking large amounts of olanzapine.
• Until complete recovery from this condition, the patient must be under constant supervision of the attending physician.
• There is no single antidote that would stop all manifestations of an overdose.

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Interactions with other drugs

When using any combination therapy, it is important to remember that the interactions of Zalasta with other drugs are ambiguous and can have both a positive therapeutic effect and negative consequences.

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

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

If, in parallel with the drug under consideration, 60 mg is used once, or in the same dosage daily for eight days fluoxetine, then doctors observe an approximately 16% increase in the maximum concentration of the active substance Zalasta in the blood plasma. At the same time, clearance falls by the same 16%, which does not significantly affect the clinical picture of treatment and does not require adjustment of the amount of the administered drug.

The combined use of Zalast with fluvoxamine reduces 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: in non-smoking women, the increase is 54%, for non-smoking men, this figure is even higher - 77%. In such patients, an increase in AUC of olanzapine is also observed by 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 the metabolism of olanzapine, whereas Zalasta inhibits, albeit slightly, the processes of reproduction of valproic acid glucuronide, which is the basis of metabolic processes in the body.

With a combined protocol of taking the drug in question and biperiden or lithium-containing drugs, no significant change in the clinical picture was detected. It is necessary to use Zalasta very carefully with drugs that have central action characteristics.

Despite the fact that the effect of small doses of alcohol on the work of olanzapine has not been identified, it is still worth refraining from its consumption during the period of taking Zalasta (depending on the individual characteristics of the patient's body, depressive symptoms may appear).

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Storage conditions

Olanzapine should be kept in a place that is inaccessible to young children and adolescents, otherwise the storage conditions for Zalasta are simple: the room temperature should not exceed 25 °C.

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Shelf life

A five-year shelf life is a fairly good period of effective drug operation. This expiration date is on the packages of Zalasta with a dosage of 5 mg and 10 mg. Tablets with a dosage of 2.5 mg, 7.5 mg, 15 mg and 20 mg do not lose their medicinal properties for three years.