Olanzapine: palliative medicine update
American Journal of Hospice and Palliative Medicine, 04/19/2012
Prommer E – The purpose of this article is to outline the pharmacodynamics, pharmacology, and evidence for the use of olanzapine in palliative care.
- Olanzapine is an atypical antipsychotic agent of the thienobenzodiazepine class.
- Olanzapine blocks multiple neurotransmitter receptors, including dopaminergic (D1, D2, D3, and D4), serotonergic (5–hydroxytryptamine 2A [5–HT2A], 5–HT2C, 5–HT3, and 5–HT6), adrenergic (α1), histaminic (H1), and muscarinic (M1, M2, M3, and M4) receptors.
- Olanzapine has a high affinity for the 5HT2A receptor, which is up to 5 times greater than the dopamine receptor, resulting in less propensity to the development of extrapyramidal side effects.
- The affinity of olanzapine for multiple receptors has lead to the identification of olanzapine as an important agent in the treatment of delirium, nausea, and vomiting.
- Olanzapine has been demonstrated to have opioid–sparing properties.
- Olanzapine is principally metabolized by glucuronidation, with a smaller metabolic contribution from the cytochrome oxidase system.
- Adverse effects of olanzapine include somnolence, postural hypotension, constipation, dizziness, restlessness, and weight gain.