Drilldown: Medicines

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Medicines (732)

Medicines > classes

: Anticonvulsant

or Sedative-Hypnotic

or [[:Category:Barbiturates|Barbiturate (parent compound)]]

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None (9)

None (2) · AMPA receptor antagonist (1) · Extremely potent GABAA positive allosteric modulator (1) · GABA enhancer; sodium channel blocker; histone deacetylase inhibitor (1) · GABA reuptake inhibitor (GAT-1 blocker) (1) · GABAA positive allosteric modulator (16) · GABAA positive allosteric modulator (non-benzodiazepine) (3) · GABAA positive allosteric modulator; lactate dehydrogenase inhibitor (1) · GABAA positive allosteric modulator; very long half-life (1) · GABAA potentiator (1) · GABAA potentiator and direct activator (3) · GABAB agonist; GHB receptor agonist (1) · Irreversible GABA-T inhibitor (1) · Melatonin receptor agonist (2) · Multiple mechanisms; GPR55 antagonist; TRPV1 agonist (1) · NMDA antagonist; GABAA potentiator (1) · Positive allosteric modulator of the GABAA receptor at the benzodiazepine binding site; increases frequency of Cl− channel opening, producing anxiolytic, sedative, hypnotic, anticonvulsant, and skeletal-muscle relaxant effects. (1) · Prodrug of phenytoin; sodium channel blocker (1) · Selective GABAA agonist (extrasynaptic delta subunit) (1) · Serotonin releaser; sigma-1 agonist (1) · Slow-inactivation sodium channel enhancer; CRMP-2 ligand (1) · Sodium channel blocker (2) · Sodium channel blocker; GABAA positive allosteric modulator (1) · Sodium channel modulator (1) · Sodium/T-type calcium channel blocker; carbonic anhydrase inhibitor (1) · SV2A ligand (higher affinity than levetiracetam) (1) · T-type calcium channel blocker (1) · '"`UNIQ--vote-00000013-QINU`"' Strong CYP3A4 induction via the phenobarbital metabolite produces many interactions (reduces oral contraceptives, warfarin, many psychotropics). Essential-tremor efficacy is the unique pharmacological selling point'"`UNIQ--ref-00000014-QINU`"'. (1)

None (48) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-00000015-QINU`"', '"`UNIQ--vote-00000016-QINU`"' (1)

None (48) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1) · Seizures: 100-125 mg PO at bedtime x 3 days, then BID, then TID, escalating to 750-1500 mg/day. Essential tremor: 25-50 mg PO at bedtime, titrate slowly to 250-750 mg/day (1)

None (48) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1) · Tablets 50, 250 mg (1)

None (48) · 2 g/day (seizures); typically much lower for essential tremor (1) · N/A (never approved) (1)

None (48) · intranasal; rectal and IV reported. (1) · Oral (2) · sublingual (1)

None (48) · Anticonvulsant effect emerges with slow titration over weeks; tremor effect over weeks (1) · ~20–40 min PO; faster sublingual/intranasal. (1)

None (48) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · BID-TID dosing (1)

None (48) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · Primidone 5-15 hours; '''phenobarbital active metabolite 50-150 hours'''; PEMA (phenylethylmalonamide) active metabolite 16 hours'"`UNIQ--ref-00000017-QINU`"' (1)

None (48) · Not formally characterized in humans. (1) · ~90% (oral)'"`UNIQ--ref-00000018-QINU`"' (1)

None (48) · 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) · Substantial teratogenic signal (barbiturate class effects including neonatal withdrawal and hemorrhagic disease of newborn).[[[Pharmacopedia:Citation needed|citation needed]]] (1)

None (49) · [[USLegal:Prescription only|Rx-only]] in US. '''Federally non-controlled despite being a barbiturate''', a paradoxical situation given that its primary active metabolite phenobarbital is Schedule IV'"`UNIQ--ref-00000019-QINU`"' (1)

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