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Medicines > legal : Leaves legal in Bolivia, Peru, Colombia; cocaine internationally controlled or Rx, Schedule IV (US) or Rx-only in US

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mechanism:
None (1) · 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) · Donepezil: reversible AChE inhibitor, increases synaptic acetylcholine. Memantine: uncompetitive low-affinity NMDA receptor antagonist, dampens pathological glutamate overactivation while preserving normal synaptic signaling. Targets two distinct mechanisms in Alzheimer's. (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) · Primary alkaloid is cocaine, a tropane that blocks reuptake of dopamine and norepinephrine (and serotonin). At low oral doses from leaf chewing, the slow release favors NE-mediated alertness over DA-mediated euphoria. (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 dopamine and norepinephrine reuptake inhibitor (DAT and NET inhibition). Unlike amphetamine, does not significantly release monoamines, pure reuptake inhibition. (1) · Selective inhibitor of PDE5 with a substantially longer half-life than other PDE5 inhibitors, allowing once-daily continuous dosing. (1) · Selective inhibitor of PDE5. Slightly higher PDE5/PDE6 selectivity vs sildenafil (less visual side effect) but more PDE1 cross-activity (occasional QT effects at high doses). (1) · Selective inhibitor of phosphodiesterase type 5 (PDE5), preventing cGMP breakdown in vascular smooth muscle. In the corpus cavernosum, potentiates the NO/cGMP cascade triggered by sexual stimulation. (1) · Selective inhibitor of phosphodiesterase type 5 (PDE5); increases cGMP in cavernous smooth muscle, producing erection in response to sexual stimulation. (1) · Synthetic neuroactive steroid (an analog of allopregnanolone), bioavailable orally unlike brexanolone. Positive allosteric modulator at GABA-A receptors including extrasynaptic δ-containing subtypes. (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) · TrkB/BDNF'"`UNIQ--ref-00000084-QINU`"' '"`UNIQ--vote-00000085-QINU`"' (1)
uses:
None (1) · Excessive daytime sleepiness in adults with narcolepsy or obstructive sleep apnea (OSA) (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) · Postpartum depression (PPD) in adults (FDA-approved 2023) (1) · '"`UNIQ--vote-0000000C-QINU`"', '"`UNIQ--vote-0000000D-QINU`"', '"`UNIQ--vote-0000000E-QINU`"', '"`UNIQ--vote-0000000F-QINU`"' (1) · '"`UNIQ--vote-00000040-QINU`"' (1) · '"`UNIQ--vote-00000468-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-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) · '"`UNIQ--vote-00000669-QINU`"' (1) · '"`UNIQ--vote-00000705-QINU`"', '"`UNIQ--vote-00000706-QINU`"' (1) · '"`UNIQ--vote-00000738-QINU`"', '"`UNIQ--vote-00000739-QINU`"', '"`UNIQ--vote-0000073A-QINU`"' (1)
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