Olanzapine: Difference between revisions

(7 intermediate revisions by 2 users not shown)

Line 1:

{{MedTemplate

| generic = Olanzapine

| brand = Zyprexa

| brand = Zyprexa (oral, IM acute), Zyprexa Zydis (ODT), Zyprexa Relprevv (LAI), Lybalvi (with samidorphan)

| classes = ~~Antipsychotic~~, ~~Neuroleptic~~

| structure =

| mechanism = Multi-receptor antagonist (D1-4, 5-~~HT2~~, H1, muscarinic)

| classes = [[:Category:Neuroleptics|Neuroleptic]], [[:Category:Atypical neuroleptics|Atypical neuroleptic (second-generation)]], [[:Category:Thienobenzodiazepines|Thienobenzodiazepine]], [[:Category:Mood stabilizers|Mood stabilizer]]

| uses = <vote slug="schizophrenia-use">Schizophrenia (FDA)</vote>, <vote slug="bipolar-mania-mixed-use">Bipolar I mania and mixed episodes (FDA)</vote>, <vote slug="bipolar-maintenance-use">Bipolar I maintenance (FDA)</vote>, <vote slug="bipolar-depression-combination-use">Bipolar depression (FDA, in combination with fluoxetine as Symbyax)</vote>, <vote slug="acute-agitation-im-use">Acute agitation in schizophrenia or bipolar disorder (FDA, IM)</vote>, <vote slug="treatment-resistant-depression-adjunct-use">Treatment-resistant depression adjunct (off-label)</vote>, <vote slug="anorexia-nervosa-use">Anorexia nervosa (off-label, evidence-supported)</vote>

| starting_dose = Schizophrenia / acute mania: 5-10 mg PO once daily, target 10-15 mg/day. Acute agitation IM: 10 mg, may repeat in 2 hours. Relprevv LAI: 150-300 mg every 4 weeks after oral overlap

| preparations = Tablets 2.5, 5, 7.5, 10, 15, 20 mg; ODT (Zydis) 5, 10, 15, 20 mg; acute IM injection 10 mg/vial; Relprevv LAI 210, 300, 405 mg vials

| fda_max = 20 mg/day (oral)

| pill_id =

| routes = Oral, intramuscular (acute and long-acting)

| onset = Sedation from first dose; neuroleptic effect emerges over days to weeks

| duration = 24 hours (oral); 2-4 weeks (LAI)

| halflife = 21-54 hours<ref name="zyprexa-label">FDA Prescribing Information, Zyprexa (olanzapine), Eli Lilly, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/020592s062,021086s041,021253s048lbl.pdf</ref>

| bioavailability = ~60% (oral); ~100% (IM)<ref name="zyprexa-label" />

| pregnancy = Signal for gestational diabetes and metabolic syndrome with maternal exposure; the metabolic load can be substantial during pregnancy.{{citation needed}}

| legal = [[USLegal:Prescription only|Rx-only]] in US. Carries the atypical-neuroleptic '''Boxed Warning''' for increased mortality in elderly patients with dementia-related psychosis. '''Zyprexa Relprevv LAI''' additionally carries a Boxed Warning for '''post-injection delirium/sedation syndrome''' requiring 3-hour monitored observation after each injection<ref name="zyprexa-label" />

| mechanism = <vote slug="olanzapine-mech-claim">Multi-receptor antagonist with broad activity at D1, D2, D3, D4 dopamine receptors (D2/D3 mediating the neuroleptic effect), 5-HT2A and 5-HT2C serotonin receptors (the atypical-neuroleptic feature, reducing extrapyramidal burden), H1 histamine (mediating sedation and weight gain), M1-M5 muscarinic (anticholinergic effects), and α1-adrenergic (orthostatic hypotension) receptors.</vote> The marquee tolerability concern is '''severe metabolic burden''': weight gain often exceeding 10 kg in the first year, insulin resistance, hyperlipidemia, and elevated type 2 diabetes risk, among the worst in the second-generation class. Routine metabolic monitoring (weight, fasting glucose, lipid panel) is standard. The Lybalvi formulation combines olanzapine with samidorphan, an opioid antagonist, to mitigate weight gain<ref name="zyprexa-label" />.

}}

== References ==

[[Category:Neuroleptics]]

[[Category:Atypical neuroleptics]]

[[Category:Thienobenzodiazepines]]

[[Category:Mood stabilizers]]

MDElliottMD (talk | contribs)