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Medicines > classes : Neuroleptic or Research material or [[:Category:Antiemetics|Antiemetic]]

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generic:
brand:
None (130) · (none, never marketed) (1) · Antivert (Rx), Bonine (OTC), Dramamine Less Drowsy (OTC) (1) · Benadryl (oral, injectable, topical), Banophen, Sominex (sleep aid), ZzzQuil, Aler-Dryl (1) · Clozaril (1) · Fanapt (1) · Geodon (1) · Inapsine (1) · Invega (1) · Latuda (1) · Loxitane (1) · Mellaril (1) · Moban (1) · Navane (1) · O-DSMT (1) · Orap (1) · Phenergan, Promethegan (suppositories) (1) · Prolixin (1) · Reglan, Gimoti (intranasal), Metozolv ODT (1) · Saphris (1) · Stelazine (1) · Thorazine (1) · Trilafon (1) · Zofran, Zofran ODT (1)
classes: (Click arrow to add another value)
mechanism:
5-HT2A agonist (26) · Monoamine releasing agent (9) · GABAA positive allosteric modulator (8) · CB1/CB2 agonist (7) · Dopamine/norepinephrine reuptake inhibitor (5) · Potent 5-HT2A agonist (5) · LSD analogue; 5-HT2A agonist (4) · Phenothiazine D2 antagonist (4) · Prodrug of LSD; 5-HT2A agonist (4) · None (3) · Serotonin/norepinephrine/dopamine releasing agent (3) · Cathinone analogue; monoamine reuptake inhibitor (2) · Dopamine and norepinephrine reuptake inhibitor (2) · NMDA antagonist (2) · Prodrug of GHB (2)
uses:
None (147) · 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`"', '"`UNIQ--vote-00000017-QINU`"' (1) · '"`UNIQ--vote-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"', '"`UNIQ--vote-0000001F-QINU`"', '"`UNIQ--vote-00000020-QINU`"', '"`UNIQ--vote-00000021-QINU`"' (1) · '"`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-00000374-QINU`"', '"`UNIQ--vote-00000375-QINU`"', '"`UNIQ--vote-00000376-QINU`"', '"`UNIQ--vote-00000377-QINU`"' (1) · '"`UNIQ--vote-00000EF4-QINU`"', '"`UNIQ--vote-00000EF5-QINU`"', '"`UNIQ--vote-00000EF6-QINU`"', '"`UNIQ--vote-00000EF7-QINU`"', '"`UNIQ--vote-00000EF8-QINU`"' (1)
starting dose:
None (147) · 10 mg PO/IV/IM QID, '''not to exceed 12 weeks''' (tardive dyskinesia risk); intranasal Gimoti 15 mg BID (1) · 4-8 mg PO or IV every 8 hours as needed; 16 mg single dose preoperatively for PONV prevention (1) · Allergy: 25 mg PO BID-QID. Nausea/vomiting: 12.5-25 mg PO/IM/IV/PR every 4-6 hours. Motion sickness: 25 mg PO 30-60 minutes before travel. '''Pediatric <2 years: contraindicated''' (1) · Allergy: 25-50 mg PO every 4-6 hours. Insomnia: 25-50 mg PO at bedtime. IV (acute dystonia, severe allergic reaction): 25-50 mg slow IV push (1) · Motion sickness: 25-50 mg PO 1 hour before travel, repeat every 24 hours as needed. Vertigo: 25-100 mg/day divided (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)
preparations:
None (147) · 4 mg, 8 mg, 24 mg tablets; 4 mg, 8 mg orally disintegrating tablets; 4 mg/5 mL oral solution; IV (2 mg/mL) (1) · 5, 10 mg tablets; 5 mg/5 mL solution; 5 mg/mL IV; 15 mg/spray intranasal (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1) · Tablets 12.5, 25 mg; chewable tablets 25 mg (1) · Tablets 12.5, 25, 50 mg; oral syrup 6.25 mg/5 mL; suppositories 12.5, 25, 50 mg; injection 25 mg/mL and 50 mg/mL (1) · Tablets 25, 50 mg; capsules; liquid; chewable; topical cream/gel; injection 50 mg/mL (1)
fda max:
None (147) · 100 mg/day (adult) (1) · 100 mg/day (vertigo) (1) · 300 mg/day (oral) (1) · 40 mg/d (1) · N/A (never approved) (1) · Single doses ≤16 mg (FDA 2012 advisory withdrew the 32 mg single IV dose for QT-prolongation risk); 24-32 mg/d divided (1)
routes:
None (147) · IM (4) · intranasal (1) · intranasal; rectal and IV reported. (1) · IV (3) · IV (with caution) (1) · Oral (6) · rectal (1) · sublingual (1) · topical (1)
onset:
None (147) · 15-30 minutes (oral); 1-2 minutes (IV) (1) · 20 minutes (oral); 5 minutes (IV) (1) · 30 minutes PO; minutes IV (1) · IV/IM 1-3 minutes; PO 30-60 minutes (1) · ~1 hour (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (147) · 12-24 hours (long for an antihistamine) (1) · 4-12 hours (1) · 4-6 hours (3) · 6–10 h subjective; full pharmacologic effect considerably longer. (1)
halflife:
None (147) · 12-15 hours'"`UNIQ--ref-00000022-QINU`"' (1) · 3-6 hours (longer in hepatic impairment)'"`UNIQ--ref-00000378-QINU`"' (1) · 4-8 hours (longer in elderly, 9-13 hours)'"`UNIQ--ref-00000026-QINU`"' (1) · 5-6 hours'"`UNIQ--ref-00000EF9-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~6 hours'"`UNIQ--ref-00000018-QINU`"' (1)
bioavailability:
None (147) · Not formally characterized in humans. (1) · ~25% (oral)'"`UNIQ--ref-00000019-QINU`"' (1) · ~25% (oral, with extensive first-pass)'"`UNIQ--ref-00000023-QINU`"' (1) · ~40-60% (oral, with significant first-pass)'"`UNIQ--ref-00000027-QINU`"' (1) · ~60% (oral)'"`UNIQ--ref-00000379-QINU`"' (1) · ~80% (oral; reduced by significant first-pass)'"`UNIQ--ref-00000EFA-QINU`"' (1)
pregnancy:
None (148) · 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) · Older agent with substantial use experience, including in hyperemesis gravidarum; broadly reassuring observational data'"`UNIQ--ref-00000024-QINU`"' (1) · Older agent with substantial use experience; broadly considered safe in pregnancy'"`UNIQ--ref-00000028-QINU`"' (1) · Older agent with substantial use experience; observational signals reassuring for first-trimester exposure.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Widely used for hyperemesis gravidarum; reassuring data.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)
legal:
None (149) · [[USLegal:Over-the-counter|OTC]] as Bonine and Dramamine Less Drowsy; [[USLegal:Prescription only|Rx-only]] as Antivert (1) · [[USLegal:Over-the-counter|OTC]] for most oral and topical formulations; [[USLegal:Prescription only|Rx-only]] for injectable (1) · [[USLegal:Prescription only|Rx-only]] in US (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries a '''Boxed Warning''' for '''tardive dyskinesia''' (irreversible movement disorder), driving the 12-week chronic-use limit'"`UNIQ--ref-00000EFB-QINU`"' (1)

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