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Medicines (732)

Medicines > classes

: Benzodiazepine

or [[:Category:Anticonvulsants|Anticonvulsant]]

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Alprazolam (1) · Bromazepam (1) · Carbamazepine (1) · Chlordiazepoxide (1) · Clobazam (1) · Clonazepam (1) · Clonazolam (1) · Clorazepate (1) · Diazepam (1) · Diclazepam (1) · Estazolam (1) · Flualprazolam (1) · Flubromazepam (1) · Flubromazolam (1) · Flunitrazepam (1) · Flunitrazolam (1) · Flurazepam (1) · Gabapentin (1) · Lamotrigine (1) · Levetiracetam (1) · Lormetazepam (1) · Midazolam (1) · Nifoxipam (1) · Nitrazepam (1) · Oxazepam (1) · Oxcarbazepine (1) · Pregabalin (1) · Primidone (1) · Pyrazolam (1) · Quazepam (1) · Temazepam (1) · Topiramate (1) · Triazolam (1)

None (9) · Dalmane (1) · Doral (1) · Halcion (1) · Keppra (IR), Keppra XR, Spritam (3D-printed orally disintegrating), Roweepra (1) · Klonopin (1) · Lamictal (IR), Lamictal XR, Lamictal ODT (1) · Lexotan (1) · Librium (1) · Lyrica (IR), Lyrica CR (1) · Mogadon (1) · Mysoline (1) · Neurontin (IR), Gralise (ER), Horizant (gabapentin enacarbil ER) (1) · Onfi (1) · ProSom (1) · Restoril (1) · Rohypnol (1) · Serax (1) · Tegretol (IR, XR, suspension), Carbatrol (ER), Equetro (ER for bipolar), Epitol (1) · Topamax (IR), Trokendi XR, Qudexy XR, Eprontia (oral solution); component of Qsymia (with phentermine) (1) · Tranxene (1) · Trileptal (IR), Oxtellar XR (1) · Valium (oral, IV/IM, rectal), Diastat (rectal gel for breakthrough seizures), Valtoco (nasal spray for breakthrough seizures), Libervant (buccal film) (1) · Versed (1) · Xanax (1)

None (9) · Extremely potent GABAA positive allosteric modulator (1) · GABA-A positive allosteric modulator'"`UNIQ--ref-00000067-QINU`"' '"`UNIQ--vote-00000068-QINU`"' (1) · GABAA positive allosteric modulator (18) · GABAA positive allosteric modulator; low sedation (1) · GABAA positive allosteric modulator; prodrug of desmethyldiazepam (1) · GABAA positive allosteric modulator; very long half-life (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 (23) · 0.25 mg (1) · 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 monotherapy: 300 mg PO BID, titrate by 300 mg every 3 days. Pediatric: weight-based titration starting 8-10 mg/kg/day divided BID (1) · Adult: 500 mg PO BID, titrate by 1000 mg/day every 2 weeks. Pediatric: 10-20 mg/kg/day divided BID, weight-titrated (1) · Anxiety: 0.25 mg PO BID, titrate by 0.125-0.25 mg every 3 days to target 1-4 mg/day divided. Seizures: 1.5 mg/day divided TID, titrate by 0.5-1 mg every 3 days (1) · Anxiety: 2-10 mg PO 2-4 times daily. Alcohol withdrawal: 10-20 mg PO/IV every 4-6 hours, symptom-triggered. Status epilepticus: 5-10 mg IV. Breakthrough seizures: Diastat rectal 0.2-0.5 mg/kg or Valtoco intranasal 5-20 mg (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) · 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) · 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) · Seizures: 200 mg PO BID, titrate by 200 mg/week to 800-1200 mg/day. Trigeminal neuralgia: 100-200 mg BID, titrate to 200-400 mg TID. Bipolar: 200 mg BID, titrate to 1600 mg/day (1)

None (22) · 0.25 mg, 0.5 mg, 1 mg, 2 mg tablets (immediate-release and orally disintegrating); 0.5 mg, 1 mg, 2 mg, 3 mg extended-release tablets; 1 mg/mL oral concentrate (1) · 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) · IR tablets 150, 300, 600 mg; oral suspension 60 mg/mL; XR tablets 150, 300, 600 mg (Oxtellar) (1) · IR tablets 200 mg; chewable 100 mg; oral suspension 100 mg/5 mL; XR tablets 100, 200, 400 mg (Tegretol XR); ER capsules 100, 200, 300 mg (Carbatrol, Equetro) (1) · IR tablets 25, 100, 150, 200 mg; chewable dispersible tablets 2, 5, 25 mg; ODT 25, 50, 100, 200 mg; XR tablets 25, 50, 100, 200, 250, 300 mg (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) · IR tablets 250, 500, 750, 1000 mg; XR tablets 500, 750 mg; oral solution 100 mg/mL; injection 100 mg/mL; Spritam ODT 250, 500, 750, 1000 mg (1) · Tablets 0.5, 1, 2 mg; orally disintegrating tablets 0.125, 0.25, 0.5, 1, 2 mg (1) · Tablets 2, 5, 10 mg; oral solution 1, 5 mg/mL; injection 5 mg/mL; Diastat rectal gel 2.5, 5, 10, 20 mg; Valtoco nasal spray 5, 7.5, 10 mg/dose; Libervant buccal film (1) · Tablets 50, 250 mg (1)

None (22) · 10 mg/d (1) · 1200 mg/day (adult seizures); 1600 mg/day (bipolar mania) (1) · 1600 mg/day (theoretical seizure dosing); practical use 400 mg/day for seizures, 100-200 mg/day for migraine prophylaxis (1) · 2 g/day (seizures); typically much lower for essential tremor (1) · 20 mg/day (seizures); commonly limited to 4 mg/day for anxiety in current practice (1) · 2400 mg/day (adult) (1) · 3000 mg/day (1) · 3600 mg/day; off-label doses higher are common but bioavailability saturates well below this (1) · 40 mg/day (oral, anxiety) (1) · 400 mg/day (bipolar monotherapy); 700 mg/day (epilepsy with enzyme-inducing comedication) (1) · 600 mg/day (seizures); 450 mg/day (fibromyalgia and neuropathic pain) (1)

None (22) · buccal (1) · IM (1) · intranasal (1) · intravenous (1) · IV (1) · Oral (11) · rectal (1)

None (22) · 1-2 weeks for neuropathic pain and anxiolytic effect; anticonvulsant effect at therapeutic plasma level (1) · 15-60 minutes (oral); 1-5 minutes (IV); 4-10 minutes (rectal or intranasal) (1) · 20-60 minutes (1) · 30-60 min (immediate-release); 1-2 h (extended-release) (1) · Anticonvulsant effect emerges with slow titration over weeks; tremor effect over weeks (1) · Anticonvulsant effect within days at therapeutic level; migraine prophylaxis effect emerges over 2-3 months (1) · Anticonvulsant effect within days at therapeutic plasma level (1) · Anticonvulsant effect within days at therapeutic plasma level; rapid titration possible (1) · Anticonvulsant effect within days; trigeminal neuralgia relief 24-72 hours; mood-stabilizing effect over weeks (1) · Antiepileptic effect within days at therapeutic level; mood-stabilizing effect emerges over weeks (1) · Neuropathic pain and fibromyalgia effect emerges over 1-2 weeks (1)

None (22) · 12-24 hours (IR BID); 24 hours (ER once-daily) (1) · 24 hours (often divided BID at higher doses) (1) · 6 h (immediate-release); ~11 h (extended-release) (1) · 6-12 hours (long-acting among benzodiazepines) (1) · 6-24 hours (parent); much longer when accounting for the long-lived active metabolites (1) · BID dosing (IR); once-daily (XR) (2) · BID-QID dosing (IR); BID for ER formulations (1) · BID-TID dosing (1) · BID-TID dosing for IR; once-daily for CR (1) · TID dosing for IR; once-daily for ER formulations (1)

None (22) · '''Autoinduction''': 25-65 hours initially, falling to 12-17 hours after 2-3 weeks of dosing as carbamazepine induces its own CYP3A4 metabolism. Major clinical implication: doses require re-titration after the autoinduction period'"`UNIQ--ref-0000001D-QINU`"' (1) · 11-13 h (immediate-release); 11-16 h (extended-release) (1) · 30-40 hours (long; accumulates with chronic dosing)'"`UNIQ--ref-00000026-QINU`"' (1) · 5-7 hours'"`UNIQ--ref-00000029-QINU`"' (1) · 6-8 hours'"`UNIQ--ref-0000001F-QINU`"' (1) · 6.3 hours'"`UNIQ--ref-00000026-QINU`"' (1) · Diazepam 20-50 hours; '''N-desmethyldiazepam (nordazepam) 30-200 hours''' is the major active metabolite and accumulates substantially with chronic dosing'"`UNIQ--ref-00000026-QINU`"' (1) · Oxcarbazepine 2 hours; '''10-monohydroxy active metabolite (MHD) ~9 hours''' (the agent that produces essentially all of the clinical effect)'"`UNIQ--ref-0000001A-QINU`"' (1) · Primidone 5-15 hours; '''phenobarbital active metabolite 50-150 hours'''; PEMA (phenylethylmalonamide) active metabolite 16 hours'"`UNIQ--ref-00000017-QINU`"' (1) · ~21 hours'"`UNIQ--ref-00000028-QINU`"' (1) · ~25-33 hours alone; ~15 hours with enzyme inducers; '''≥60 hours with valproate''' (UGT inhibition)'"`UNIQ--ref-00000025-QINU`"' (1)

None (22) · '''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) · 80-90% oral (1) · ~100% (oral)'"`UNIQ--ref-0000001B-QINU`"' (1) · ~100% (oral)'"`UNIQ--ref-00000020-QINU`"' (1) · ~80% (oral)'"`UNIQ--ref-0000001E-QINU`"' (1) · ~80% (oral)'"`UNIQ--ref-00000029-QINU`"' (1) · ~90% (oral)'"`UNIQ--ref-00000018-QINU`"' (1) · ~90% (oral)'"`UNIQ--ref-00000027-QINU`"' (1) · ~93% (oral); ~90% (rectal)'"`UNIQ--ref-00000027-QINU`"' (1) · ~98% (oral)'"`UNIQ--ref-00000026-QINU`"' (1) · ≥90% (linear pharmacokinetics, distinguishing it favorably from gabapentin's saturable LAT-1 absorption)'"`UNIQ--ref-00000027-QINU`"' (1)

None (22) · '''Among the safest mood stabilizers in pregnancy''' with reassuring monotherapy registry data, in sharp contrast to valproate. Estrogen-containing contraceptives accelerate lamotrigine metabolism, requiring dose adjustments at start and stop of contraception'"`UNIQ--ref-00000027-QINU`"' (1) · '''Considered one of the safest anticonvulsants in pregnancy''', with reassuring monotherapy registry data comparable to lamotrigine and in sharp contrast to valproate, topiramate, and carbamazepine'"`UNIQ--ref-00000021-QINU`"' (1) · '''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) · '''Substantial teratogenic risk''' including neural tube defects, craniofacial malformations, cardiac defects, and growth restriction; folic acid supplementation and effective contraception are required in reproductive-age patients'"`UNIQ--ref-0000001F-QINU`"' (1) · Category D'"`UNIQ--ref-0000006C-QINU`"' (1) · Limited human data; some signal for cardiac malformations and developmental delay but confounded by maternal disease and polytherapy.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Limited human data; some signal for cleft palate with first-trimester exposure (debated); neonatal sedation and withdrawal with third-trimester exposure.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Some signal for cleft palate with first-trimester exposure (debated); neonatal sedation and withdrawal with third-trimester exposure.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Some signal for major congenital malformations; limited human data.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Substantial teratogenic signal (barbiturate class effects including neonatal withdrawal and hemorrhagic disease of newborn).[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Teratogenic signal less than carbamazepine but present; folate supplementation and effective contraception are appropriate in reproductive-age patients'"`UNIQ--ref-0000001C-QINU`"' (1)

None (23) · '''[[USLegal:Schedule V|Schedule V controlled substance]] in US (federally)''', distinct from gabapentin which remains federally unscheduled'"`UNIQ--ref-00000028-QINU`"' (1) · Schedule IV (US) (1) · [[USLegal:Prescription only|Rx-only]] in US (2) · [[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) · [[USLegal:Prescription only|Rx-only]] in US. Carries the FDA '''Boxed Warning for serious skin reactions''' including Stevens-Johnson syndrome and toxic epidermal necrolysis, with the risk concentrated in the first 2-8 weeks of therapy and elevated by rapid titration'"`UNIQ--ref-00000028-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Not a controlled substance'"`UNIQ--ref-00000022-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Not a controlled substance'"`UNIQ--ref-0000002B-QINU`"' (1) · [[USLegal:Schedule IV|Schedule IV controlled substance]] in US. Carries the benzodiazepine class '''Boxed Warning''' for risk of fatal respiratory depression, coma, and death when combined with opioids'"`UNIQ--ref-00000028-QINU`"' (2)