Drilldown: Medicines
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generic:
brand:
classes: (Click arrow to add another value)
mechanism:
None (4) ·
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 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) ·
'"`UNIQ--vote-0000001F-QINU`"', '"`UNIQ--vote-00000020-QINU`"', '"`UNIQ--vote-00000021-QINU`"', '"`UNIQ--vote-00000022-QINU`"', '"`UNIQ--vote-00000023-QINU`"', '"`UNIQ--vote-00000024-QINU`"', '"`UNIQ--vote-00000025-QINU`"' (1) ·
'"`UNIQ--vote-00000021-QINU`"', '"`UNIQ--vote-00000022-QINU`"', '"`UNIQ--vote-00000023-QINU`"', '"`UNIQ--vote-00000024-QINU`"', '"`UNIQ--vote-00000025-QINU`"', '"`UNIQ--vote-00000026-QINU`"', '"`UNIQ--vote-00000027-QINU`"', '"`UNIQ--vote-00000028-QINU`"' (1)
starting dose:
None (60) ·
300 mg PO at bedtime night 1, 300 mg BID day 2, 300 mg TID day 3; titrate to clinical effect, commonly 1800-3600 mg/day divided TID (1) ·
Adult: 15–60 mg every 4 hours as needed. (1) ·
Neuropathic pain: 75 mg PO BID, titrate to 150 mg BID after 1 week. Fibromyalgia: 75 mg PO BID, titrate to 150 mg BID. Anxiety (off-label): 75-150 mg/day divided BID-TID (1) ·
No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)
preparations:
None (60) ·
Capsules 100, 300, 400 mg; tablets 600, 800 mg; oral solution 250 mg/5 mL; Gralise ER tablets 300, 600 mg (once-daily); Horizant ER tablets 300, 600 mg (gabapentin enacarbil, an inactive parent compound metabolized to gabapentin in vivo) (1) ·
Capsules 25, 50, 75, 100, 150, 200, 225, 300 mg; oral solution 20 mg/mL; Lyrica CR tablets 82.5, 165, 330 mg (1) ·
Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1) ·
Tablet (15, 30, 60 mg); oral solution; combination products (with [[Acetaminophen|acetaminophen]] or ibuprofen). (1)
fda max:
routes:
onset:
duration:
halflife:
bioavailability:
None (60) ·
'''Saturable''' via the LAT-1 amino-acid transporter, producing nonlinear pharmacokinetics: ~60% at 300 mg single dose, falling to ~35% at 1200 mg single dose'"`UNIQ--ref-0000002A-QINU`"' (1) ·
Not formally characterized in humans. (1) ·
~50% (variable, CYP2D6-dependent for analgesic effect). (1) ·
≥90% (linear pharmacokinetics, distinguishing it favorably from gabapentin's saturable LAT-1 absorption)'"`UNIQ--ref-00000027-QINU`"' (1)
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 human data; some signal for cardiac malformations and developmental delay but confounded by maternal disease and polytherapy.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Some signal for major congenital malformations; limited human data.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1)
Showing below up to 64 results in range #1 to #64.