Drilldown: Medicines
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mechanism:
None (2) ·
Active metabolite of tramadol; mu-opioid agonist (1) ·
Extremely potent GABAA positive allosteric modulator (1) ·
Extremely potent mu-opioid receptor agonist (1) ·
GABAA positive allosteric modulator (15) ·
GABAA positive allosteric modulator (non-benzodiazepine) (3) ·
GABAA positive allosteric modulator; very long half-life (1) ·
GABAA potentiator (1) ·
GABAA potentiator and direct activator (2) ·
GABAB agonist; GHB receptor agonist (1) ·
Highly potent mu-opioid receptor agonist (1) ·
Kappa agonist; mu antagonist (1) ·
Kappa agonist; mu partial agonist (1) ·
Kappa agonist; mu partial agonist/antagonist (1) ·
Melatonin receptor agonist (2) ·
Mitragynine/7-hydroxymitragynine; mu-opioid partial agonist (1) ·
Mu-opioid agonist; modulates glutamate AMPA receptors (1) ·
Mu-opioid agonist; norepinephrine reuptake inhibitor (1) ·
Mu-opioid receptor agonist (4) ·
Mu-opioid receptor agonist; fentanyl analogue (1) ·
Mu-opioid receptor agonist; NMDA antagonist (1) ·
Mu-opioid receptor agonist; prodrug (metabolized to morphine) (1) ·
Mu-opioid receptor agonist; sodium channel blocker (1) ·
Mu/kappa/delta agonist; NMDA antagonist (1) ·
Opioid receptor partial agonist/antagonist; toxic alkaloid (1) ·
Partial agonist at D2 and 5HT1A. Antagonist at 5HT2A, α1A, α1B, α2C. More potent 5HT2A antagonism, 5HT1A partial agonism, and α1 antagonism (relative to D2 partial agonism) than aripiprazole, proposed to reduce akathisia and enhance affective/cognitive effects. (1) ·
Partial mu-opioid agonist; kappa antagonist (1) ·
Partial mu-opioid receptor agonist; alpha-2 agonist (1) ·
Phosphodiesterase inhibitor; calcium channel blocker (1) ·
Positive allosteric modulator of the GABA<sub>A</sub> receptor at the benzodiazepine binding site; increases frequency of Cl<sup>−</sup> channel opening, producing anxiolytic, sedative, hypnotic, anticonvulsant, and skeletal-muscle relaxant effects. (1) ·
Potent mu-opioid receptor agonist (6) ·
Prodrug of morphine; mu-opioid receptor agonist (1) ·
Prodrug; converted to [[Morphine|morphine]] by [[Enzyme:CYP2D6|CYP2D6]] for analgesic action. (1) ·
Selective GABAA agonist (extrasynaptic delta subunit) (1) ·
Selective mu-opioid receptor agonist (1) ·
Ultra-short-acting mu-opioid agonist (1)
uses:
None (60) ·
Mild to moderate pain; cough suppression (low-dose). (1) ·
No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) ·
Schizophrenia (FDA-approved 2015). Adjunctive treatment of major depressive disorder (2015). '''Agitation associated with dementia due to Alzheimer disease''' (FDA-approved May 2023, first agent specifically approved for this problem). Investigational for PTSD (combined with sertraline). (1)
starting dose:
None (60) ·
Adult: 15–60 mg every 4 hours as needed. (1) ·
No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1) ·
Schizophrenia: 1 mg PO daily × 4 days, then 2 mg daily × 3 days, then 4 mg daily. MDD adjunct: 0.5-1 mg daily, increase to 2 mg max. AD agitation: 0.5 mg daily, titrate to 2-3 mg daily. (1)
preparations:
fda max:
routes:
onset:
duration:
halflife:
bioavailability:
pregnancy:
None (60) ·
Avoid. Benzodiazepines are associated with neonatal sedation, floppy-infant syndrome, and withdrawal; teratogenic signal weak but non-zero. Designer benzo with no safety data, assume worst-case. (1) ·
Avoid; risk of neonatal opioid withdrawal with chronic use; UM-mother breastfeeding contraindicated. (1) ·
Limited data; National Pregnancy Registry available (1)
Showing below up to 63 results in range #1 to #63.