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Medicines > routes: Oral & pregnancy : Category C or Limited data; avoid

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mechanism:
None (2) · Cardioselective β1-adrenergic antagonist. Selectivity is dose-dependent and partially lost at higher doses. (1) · Competitive antagonist at OX1R and OX2R. Faster receptor association/dissociation kinetics than suvorexant (~16 sec dissociation vs ~57 sec) hypothesized to support sleep onset, with sufficient duration for maintenance. (1) · Competitive antagonist at OX1R and OX2R. First-in-class DORA. Receptor dissociation slower than lemborexant or daridorexant. (1) · High-affinity D2 receptor antagonist (1) · Highly β1-selective adrenergic antagonist. Greater selectivity than metoprolol or atenolol. (1) · Non-selective competitive antagonist at β1 and β2 adrenergic receptors. Lipophilic; significant blood–brain barrier penetration, accounting for its CNS effects. (1) · Norepinephrine–dopamine reuptake inhibition (DAT, NET), d-threo enantiomer of methylphenidate (1) · Selective alpha-1 adrenergic receptor antagonist. Lowers peripheral vascular resistance via vasodilation; in the CNS, blunts noradrenergic hyperarousal thought to drive trauma-related nightmares. (1) · Selective inverse agonist at 5HT2A receptors with weaker activity at 5HT2C. Has no significant dopamine D2 affinity, unique among approved antipsychotics. Inverse agonism (rather than antagonism) reduces constitutive 5HT2A receptor activity below baseline. (1) · Serotonin–norepinephrine reuptake inhibition (balanced) (1) · TAAR1 agonism, VMAT2 substrate, DAT/NET reverse transport, net release of dopamine and norepinephrine (1) · The d-enantiomer is a highly β1-selective antagonist; the l-enantiomer triggers endothelial nitric-oxide–mediated vasodilation. Unique among beta blockers for this NO mechanism. (1)
uses:
Depression, anxiety, neuropathic pain, fibromyalgia, chronic musculoskeletal pain (1) · Hallucinations and delusions associated with Parkinson's disease psychosis (PDP). Investigational for psychosis in other dementias and as augmentation for depression. (1) · Insomnia (sleep onset and/or maintenance) in adults (FDA-approved August 2014). Also studied for insomnia in mild-moderate Alzheimer disease. (1) · Insomnia (sleep onset and/or maintenance) in adults (FDA-approved Dec 2019) (1) · Insomnia (sleep onset and/or sleep maintenance) in adults (FDA-approved Jan 2022) (1) · Major depressive disorder in adults (FDA-approved August 2022) (1) · Schizophrenia, acute psychosis, agitation, delirium, Tourette syndrome, severe nausea (1) · '"`UNIQ--vote-00000150-QINU`"', '"`UNIQ--vote-00000151-QINU`"' (1) · '"`UNIQ--vote-000004F5-QINU`"', '"`UNIQ--vote-000004F6-QINU`"', '"`UNIQ--vote-000004F7-QINU`"', '"`UNIQ--vote-000004F8-QINU`"', '"`UNIQ--vote-000004F9-QINU`"' (1) · '"`UNIQ--vote-00000562-QINU`"', '"`UNIQ--vote-00000563-QINU`"', '"`UNIQ--vote-00000564-QINU`"', '"`UNIQ--vote-00000565-QINU`"', '"`UNIQ--vote-00000566-QINU`"' (1) · '"`UNIQ--vote-0000059D-QINU`"' (1) · '"`UNIQ--vote-000005D0-QINU`"', '"`UNIQ--vote-000005D1-QINU`"', '"`UNIQ--vote-000005D2-QINU`"' (1) · '"`UNIQ--vote-000005E7-QINU`"', '"`UNIQ--vote-000005E8-QINU`"', '"`UNIQ--vote-000005E9-QINU`"', '"`UNIQ--vote-000005EA-QINU`"', '"`UNIQ--vote-000005EB-QINU`"' (1) · '"`UNIQ--vote-00000636-QINU`"', '"`UNIQ--vote-00000637-QINU`"', '"`UNIQ--vote-00000638-QINU`"' (1)
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