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Medicines > classes : Research material or [[:Category:Migraine prophylactics|Migraine prophylactic]]

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generic:
brand:
None (130) · (none, never marketed) (1) · Elavil (US brand discontinued; generic widely available), Endep, Tryptizol (1) · O-DSMT (1) · Pamelor (US brand discontinued; generic widely available), Aventyl (1) · Timoptic (ophthalmic), Timoptic-XE (gel-forming once-daily), Istalol (once-daily 0.5%), Betimol; Blocadren (oral, discontinued in many markets); combination eye drops Combigan (with brimonidine), Cosopt (with dorzolamide) (1) · Topamax (IR), Trokendi XR, Qudexy XR, Eprontia (oral solution); component of Qsymia (with phentermine) (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) · 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 (131) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-00000017-QINU`"', '"`UNIQ--vote-00000018-QINU`"', '"`UNIQ--vote-00000019-QINU`"', '"`UNIQ--vote-0000001A-QINU`"' (1) · '"`UNIQ--vote-0000001B-QINU`"', '"`UNIQ--vote-0000001C-QINU`"', '"`UNIQ--vote-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"', '"`UNIQ--vote-0000001F-QINU`"' (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`"' (1)
starting dose:
None (131) · Depression (rarely used now): 25-75 mg PO at bedtime, titrate to 150 mg/day. Neuropathic pain / migraine prophylaxis: 10-25 mg at bedtime, titrate by 10-25 mg weekly to 50-100 mg/day. Elderly: 10 mg at bedtime (Beers-list cautions apply) (1) · Depression: 25 mg PO TID-QID or 75 mg at bedtime, titrate to 75-150 mg/day. Neuropathic pain: 10-25 mg at bedtime, titrate to 50-100 mg/day. Elderly: 10 mg at bedtime (Beers-list cautions, though less than amitriptyline) (1) · Migraine: 25 mg PO at bedtime, titrate by 25 mg weekly to target 100 mg/day divided BID. Seizures: 25-50 mg/day, titrate weekly to 200-400 mg/day divided BID (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1) · Ophthalmic: 1 drop 0.5% in affected eye(s) BID (or once daily for XE / Istalol). Oral hypertension: 10 mg PO BID, titrate to 60 mg/day. Migraine prophylaxis: 10 mg BID, titrate to 30 mg/day (1)
preparations:
None (131) · Capsules 10, 25, 50, 75 mg; oral solution 10 mg/5 mL (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1) · IR tablets 25, 50, 100, 200 mg; sprinkle capsules 15, 25 mg; Trokendi XR capsules 25, 50, 100, 200 mg; Qudexy XR capsules; Eprontia oral solution 25 mg/mL (1) · Tablets 10, 25, 50, 75, 100, 150 mg (1) · Tablets 5, 10, 20 mg; ophthalmic solution 0.25%, 0.5%; ophthalmic gel-forming solution 0.25%, 0.5% (Timoptic-XE) (1)
fda max:
None (131) · 150 mg/day; therapeutic plasma-level monitoring recommended (target 50-150 ng/mL window) (1) · 1600 mg/day (theoretical seizure dosing); practical use 400 mg/day for seizures, 100-200 mg/day for migraine prophylaxis (1) · 300 mg/day (historical hospitalized inpatient depression); 150 mg/day outpatient typical ceiling (1) · 60 mg/day (oral, hypertension); 0.5% BID (ophthalmic) (1) · N/A (never approved) (1)
routes:
None (131) · intranasal; rectal and IV reported. (1) · ophthalmic (1) · Oral (5) · sublingual (1)
onset:
None (131) · Anticonvulsant effect within days at therapeutic level; migraine prophylaxis effect emerges over 2-3 months (1) · BP effect within hours (oral); IOP reduction within 30 minutes, full effect 1-2 weeks (ophthalmic) (1) · Pain and migraine prophylaxis effect 1-4 weeks; antidepressant effect 4-6 weeks (1) · Sleep effect from first dose; analgesic and migraine-prophylaxis effect 1-4 weeks; antidepressant effect 4-6 weeks (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (131) · 12 hours (oral BID); 24 hours (Timoptic-XE) (1) · 12-24 hours (IR BID); 24 hours (ER once-daily) (1) · 24 hours (HS dosing) (2) · 6–10 h subjective; full pharmacologic effect considerably longer. (1)
halflife:
None (131) · 18-44 hours'"`UNIQ--ref-00000020-QINU`"' (1) · Amitriptyline 10-50 hours (highly variable); nortriptyline active metabolite 18-44 hours'"`UNIQ--ref-00000026-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~21 hours'"`UNIQ--ref-00000028-QINU`"' (1) · ~4 hours (oral)'"`UNIQ--ref-0000001B-QINU`"' (1)
bioavailability:
None (131) · Not formally characterized in humans. (1) · ~50% (oral); systemic absorption from ophthalmic application is clinically meaningful via nasolacrimal drainage'"`UNIQ--ref-0000001C-QINU`"' (1) · ~50% (oral)'"`UNIQ--ref-00000021-QINU`"' (1) · ~50% (oral)'"`UNIQ--ref-00000027-QINU`"' (1) · ~80% (oral)'"`UNIQ--ref-00000029-QINU`"' (1)
pregnancy:
None (131) · '''Substantial teratogenic risk''' including cleft lip/palate, hypospadias, and growth restriction (pregnancy registry data clear); effective contraception and pre-pregnancy counseling are required in reproductive-age patients'"`UNIQ--ref-0000002A-QINU`"' (1) · 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) · Limited human data; β-blocker class effects include fetal growth restriction and neonatal bradycardia/hypoglycemia.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Older agent with substantial use experience; observational signals not clearly causal.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · TCA class signal; limited human data specific to nortriptyline.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)
legal:
None (132) · [[USLegal:Prescription only|Rx-only]] in US (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries the antidepressant '''Boxed Warning''' for suicidality in children, adolescents, and young adults'"`UNIQ--ref-00000022-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries the antidepressant '''Boxed Warning''' for suicidality in children, adolescents, and young adults'"`UNIQ--ref-00000028-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Not a controlled substance'"`UNIQ--ref-0000002B-QINU`"' (1)

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