Olanzapine: What You Should Know About It

Due to the increased affinity to the serotonin and dopamine receptors, the active ingredient olanzapine can decisively improve the symptoms of schizophrenia.

The active ingredient olanzapine is one of the atypical neuroleptics. It is used to treat schizophrenia and the depressive episodes or obsessive-compulsive disorder caused by bipolar disorder.

The patent for the active ingredient, which the pharmaceutical company Eli Lilly & Company held until 2011, which made it the sole producer and distributor of the drug and thus dominant in the market, expired in 2011. Since then, olanzapine has been available from various suppliers around the world.

Interesting facts about schizophrenia

Schizophrenia is a chronic type of psychosis that manifests itself through thought disorders, hallucinations or delirium. These symptoms are known in specialist circles as positive symptoms. On the other hand, there are also the negative symptoms that the patient can suffer from. This includes:

• Antisociality
• apathy
• Flattening of affect

As for what triggers this disease, a number of factors contribute to schizophrenia. Some of these factors that the patient may have are listed below:

• Biochemical changes in the brain : Schizophrenia patients have high levels of dopamine and serotonin in the brain.
• Genetic factors : If there is a hereditary problem, i.e. parents or close relatives suffer from the disease, this increases the likelihood of developing it as well.

• Problems during pregnancy : if complications such as a lack of oxygen, infections or trauma of any kind occur, the baby can be so damaged that this increases the risk of developing schizophrenia or other problems.

Structure and mechanism of action: What is the effect on the organism?

The neuroleptic has a chemical composition similar to the benzodiazepines, more precisely the structure is similar to the active ingredients quetiapine and clozapine. Its psychopharmaceutical effects are due to the interaction with the serotonin receptors. This blocks the serotonin receptors 5-HT2 in the brain.

Olanzapine also reacts with the dopamine receptors D1 and D2, but with a lower affinity. There is also a certain affinity to the cholinergic muscarinic receptors, the alpha adrenoceptors and the H1 histamines.

Due to all of these interactions, a number of side effects are triggered, which we will discuss in more detail later. Due to its high affinity for the mentioned receptors, olanzapine can bring about a significant improvement in both the positive and negative symptoms of schizophrenia.

Finally, it is worth mentioning that there is also an active ingredient formula with long-term effects.

Pharmacokinetics: what happens to olanzapine in the organism?

Pharmacoconetics describes all processes of uptake, distribution and biochemical conversion and degradation. Olanzapine is given orally and processed quickly.

Once absorbed by the body, it reaches its maximum concentration in the blood plasma after 6 hours. It is important to know that food intake does not affect absorption, which is not the case with all drugs.

The bioavailability of the active ingredient, i.e. the maximum available concentration in the blood when it becomes effective, is not very high. This is because olanzapine is heavily metabolized in the liver. Only around 40% of the dose originally taken gets into the bloodstream.

Metabolism, a series of chemical reactions that increase the solubility of the drug and thus make it easier to break down, takes place in the liver.

After metabolism, the so-called metabolites, i.e. the converted substances, may or may not have an effect on the organism. In the case of olanzapine, the metabolites resulting from the chemical reactions have no pharmacological effect.

After conversion, 30% of both metabolites and drug are excreted in the urine and 55% in the stool.

Side effects of olanzapine

The most common side effects of this drug are:

• Weight gain
• Drowsiness
• Elevated prolactin levels
• Elevated cholesterol, glucose and triglyceride levels
• dizziness
• Orthostatic hypotension
• constipation
• Restlessness
• Disorders of the movement sequence

Conclusion

Olanzapine is a widely used drug in the treatment of schizophrenia. Due to its strong effect on the organism , the drug is only available on prescription. In any case, taking it without a doctor’s prescription is not recommended. Consult your doctor or pharmacist for all questions about the drug, risks and side effects.