Predominantly sedating are olanzapine, quetiapine immediate and extended release, ziprasidone, asenapine, and iloperidone. Agents that are neither activating nor sedating are paliperidone and brexpiprazole.
A study by Richelson and Souder7 of the binding profiles of antipsychotic medications found that olanzapine has the highest affinity for the histamine H1 receptors, followed by clozapine (Figure 1). This may explain why olanzapine has a relatively large sedative effect even though it is a high-potency medication.
Among agents indicated for schizophrenia treatment, lurasidone and cariprazine were found to be predominately activating, while olanzapine, quetiapine (both immediate and extended-release), ziprasidone, asenapine, and iloperidone were predominately sedating.
The main study findings, from this population-wide head-to-head comparison of thirty-seven antipsychotics, is that zuclopenthixol showed the strongest association with sedation and somnolence while prochloperazine resulted in the weakest association.
Mechanism of Action
Olanzapine is an atypical (second-generation) antipsychotic that exerts its action primarily on dopamine and serotonin receptors. It works on dopamine D2 receptors in the mesolimbic pathway as an antagonist, blocking dopamine from potential action at the post-synaptic receptor.
It is usually recommended to take olanzapine at bedtime because it can cause sleepiness as a side effect. However, it is important to choose a time of day to take it that you can easily remember, which could be bedtime, a mealtime, or when you brush your teeth.
Some of olanzapine's most common side effects are drowsiness, constipation, and dry mouth. Weight gain is also a frequent complaint. More serious side effects can also occur. If you notice symptoms like movement problems or abnormal changes in mood or behavior, contact your healthcare provider right away.
Olanzapine is associated with a lower incidence of extrapyramidal symptoms than typical and some atypical antipsychotics,93,94 an important cause of noncompliance and treatment discontinuation.
Olanzapine can make you feel sleepy. If this happens to you, do not drive, ride a bike or use tools or machinery until you feel better. Some people find it hard to concentrate while they are taking olanzapine.
Patients taking clozapine had more blood dyscrasias, hypersalivation, seizures, and sedation than those taking olanzapine, risperidone, or quetiapine.
Olanzapine is well absorbed and reaches peak concentrations in approximately 6 hours following an oral dose. It is eliminated extensively by first pass metabolism, with approximately 40% of the dose metabolized before reaching the systemic circulation. Food does not affect the rate or extent of olanzapine absorption.
Olanzapine augments the effect of selective serotonin reuptake inhibitors by suppressing GABAergic inhibition via antagonism of 5-HT₆ receptors in the dorsal raphe nucleus.
Olanzapine gave me that opportunity in a way. It gave me peace for the first time in months. It didn't stop the pain or the anxiety, but it gave me the ability to rest, sleep, and relax.
Of the SSRIs, Prozac (fluoxetine) is the most likely to cause activation. The latter is due to the effects Zoloft has on dopamine receptors. Although activation can be troublesome, it can be helpful for those with severe fatigue.
Olanzapine (OLZ), a second-generation antipsychotic, is efficacious in acute settings at dosages of 5 to 20 mg/d, and it can be considered a first-line treatment for patients with an acute episode of schizophrenia.
Olanzapine is used to treat schizophrenia. It may also be used alone or with other medicines (eg, lithium or valproate) to treat mania or mixed episodes that is part of bipolar disorder (manic-depressive illness).
Seroquel, Abilify, Geodon, Latuda, and Depakote are some olanzapine alternatives.
Olanzapine (Zyprexa) is considered a mood stabilizer, along with lithium (Lithotabs), certain anticonvulsants (anti-seizure medications), and some other antipsychotics. Olanzapine (Zyprexa) can also help to treat depression when combined with fluoxetine (Prozac).
Alcohol can increase the nervous system side effects of OLANZapine such as dizziness, drowsiness, and difficulty concentrating. Some people may also experience impairment in thinking and judgment. You should avoid or limit the use of alcohol while being treated with OLANZapine.
This is consistent with the reports from case studies. Two of the published case studies describe a euphoric feeling or a 'high' from olanzapine. A quarter of those who engaged in NMU of olanzapine used it to 'get stoned'.
Similar analyses in male C57BL/6 mice found that olanzapine treatment led to a similar increase in energy expenditure and a decrease in physical activity.
A person should never abruptly stop taking Zyprexa as the shock to the body can be severe and intolerable. Even with a slow taper, especially without proper support, withdrawals can tend to be long-lasting, and near to impossible to tolerate.
Atypical antipsychotics such as quetiapine, aripiprazole, olanzapine, and risperidone have been shown to be helpful in addressing a range of anxiety and depressive symptoms in individuals with schizophrenia and schizoaffective disorders, and have since been used in the treatment of a range of mood and anxiety disorders ...
Some improvements may be seen in as little as 1 to 2 weeks. However, it can sometimes take up to 6 weeks to see the full benefits of the medication.
It has a profoundly calming effect in many people. It can stop “racing thoughts” that can be one of the most severe symptoms of bipolar disorder, especially in Bipolar II — as well as the more obvious symptoms of paranoia or delusions as seen in Bipolar I.