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Benzodiazepines |
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The tables below contain a sample list of benzodiazepines and benzodiazepine analogs that are commonly prescribed, with their basic pharmacological characteristics, such as half-life and equivalent doses to other benzodiazepines, also listed, along with their trade names and primary uses. The elimination half-life is how long it takes for half of the drug to be eliminated by the body. "Time to peak" refers to when maximum levels of the drug in the blood occur after a given dose. Benzodiazepines generally share the same pharmacological properties, such as anxiolytic, sedative, hypnotic, skeletal muscle relaxant, amnesic, and anticonvulsant effects. Variation in potency of certain effects may exist amongst individual benzodiazepines. Some benzodiazepines produce active metabolites. Active metabolites are produced when a person's body metabolizes the drug into compounds that share a similar pharmacological profile to the parent compound and thus are relevant when calculating how long the pharmacological effects of a drug will last. Long-acting benzodiazepines with long-acting active metabolites, such as diazepam and chlordiazepoxide, are often prescribed for benzodiazepine or alcohol withdrawal as well as for anxiety if constant dose levels are required throughout the day. Shorter-acting benzodiazepines are often preferred for insomnia due to their lesser hangover effect.[1][2][3][4][5]
It is fairly important to note that elimination half-life of diazepam and chlordiazepoxide, as well as other long half-life benzodiazepines, is twice as long in the elderly compared to younger individuals. Due to increased sensitivity and potentially dangerous adverse events among elderly patients, it is recommended to avoid prescribing them as specified by the 2015 American Geriatrics Society Beers Criteria.[6] Individuals with an impaired liver also metabolize benzodiazepines more slowly. Thus, the approximate equivalent of doses below may need to be adjusted accordingly in individuals on short acting benzodiazepines who metabolize long-acting benzodiazepines more slowly and vice versa. The changes are most notable with long acting benzodiazepines as these are prone to significant accumulation in such individuals and can lead to withdrawal symptoms.[citation needed] For example, the equivalent dose of diazepam in an elderly individual on lorazepam may be half of what would be expected in a younger individual.[7][8] Equivalent doses of benzodiazepines differ as much as 20 fold.[9][10][11]
Pharmacokinetic properties of various benzodiazepines
Equivalency data in the table below is taken from the Ashton "Benzodiazepine Equivalence Table".[4][12][13][14]
Drug Name | Common Trade Names[a] | Year Approved
(US FDA) |
Typical Oral Dosage Formulations
(mg) |
Approx. Equivalent Oral Dose to 10 mg Diazepam[b] (mg) | Peak Onset of Action
(hours) |
Elimination Half-life of Active Metabolite (hours) | Primary Therapeutic Use |
---|---|---|---|---|---|---|---|
Adinazolam | Deracyn | Research chemical | 1–2 | 3 | anxiolytic, antidepressant | ||
Alprazolam | Xanax, Helex, Xanor, Trankimazin, Onax, Alprox, Misar, Restyl, Solanax, Tafil, Neurol, Frontin, Kalma, Ksalol, Farmapram | 1981 | 0.25, 0.5, 1, 2 | 0.5 | 1–3[16] | 11-13 [16] | anxiolytic, antidepressant[17] |
Bentazepam[c] | Thiadipona | 25 | 1–3 | 2–4 | anxiolytic | ||
Bretazenil[18] | 2.5 | anxiolytic, anticonvulsant | |||||
Bromazepam | Lexotanil, Lexotan, Lexilium, Lectopam, Lexaurin, Lexatin, Bromam | 1981 | 1.5, 3, 6 | 6 | 1–5 | 20–40 | anxiolytic, |
Bromazolam | Research chemical | 2 , 4 | 2 | anxiolytic | |||
Brotizolam[d] | Lendormin, Dormex, Sintonal, Noctilan | 0.25 | 0.5 | 0.5–2 | 4–5 | hypnotic | |
Camazepam | Albego, Limpidon | 40[19] | 1–3 | 6–11 | anxiolytic | ||
Chlordiazepoxide | Librium, Risolid, Elenium | 1960 | 5, 10, 25 | 25 | 1.5–6 | 36–200 | anxiolytic |
Cinazepam | Levana | 0.5, 1, 2 | 2–4 | 60 | hypnotic, anxiolytic | ||
Cinolazepam | Gerodorm | 40 | 0.5–2 | 9 | hypnotic | ||
Clobazam | Onfi, Frisium, Urbanol | 2011 | 5, 10, 20 | 20 | 1–5 | 8–60 | anxiolytic, anticonvulsant |
Clonazepam | Rivatril, Rivotril, Klonopin, Iktorivil, Paxam | 1975 | 0.5, 1, 2 | 0.5-1 | 1–5 | 19.5–50 | anticonvulsant, anxiolytic |
Clonazolam | Research chemical | 0.25, 0.5 | 0.2 | 0.5-1 | 3-4[20] | hypnotic, anticonvulsant | |
Clorazepate | Tranxene, Tranxilium | 1972 | 3.75, 5, 7.5 | 15 | Variable | 32–152 | anxiolytic, anticonvulsant |
Clotiazepam[c] | Veratran, Clozan, Rize | 5, 10 | 10 | 1–3 | 4 | anxiolytic | |
Cloxazolam | Cloxam, Sepazon, Olcadil | 1, 2, 4 | 1.5[19] | 2–5 | 55–77[19] | anxiolytic, anticonvulsant | |
Delorazepam | Dadumir | 0.5, 1, 2 | 1-1.5 | 1–2 | 79<[21] | anxiolytic, amnesic | |
Deschloroetizolam[d] | Research chemical | 1, 2 | 4 | anxiolytic | |||
Diazepam | Antenex, Apaurin, Apzepam, Apozepam, Diazepan, Hexalid, Normabel, Pax, Stesolid, Stedon, Tranquirit, Valium, Vival, Valaxona | 1963 | 2, 5, 10 | 10 | 1–1.5 | 32–205 | anxiolytic, anticonvulsant, muscle relaxant, amnesic |
Diclazepam[22] | Research chemical | 1, 2 | 2 | 1.5–3 | 42 | anxiolytic, muscle relaxant | |
Estazolam | ProSom, Nuctalon | 1990 | 1, 2 | 2[19] | 3–5 | 10–24 | hypnotic, anxiolytic |
Ethyl carfluzepate | Not approved | 2 | 1–5 | 11–24 | hypnotic | ||
Etizolam[d] | Etilaam, Etizest, Pasaden, Depas | Often sold as a research chemical, but is approved for human use in many countries. Controlled substance in some US states, Canada, Germany, Austria, and others.[23][24] | 1 | 2 | 1–3 | 5-7 | anxiolytic, muscle relaxant, anticonvulsant |
Ethyl loflazepate | Victan, Meilax, Ronlax | 2[19] | 2.5–3 | 73–119 | anxiolytic | ||
Flualprazolam | Research chemical | 0.5, 1 | 0.25 | 1-2 | 12-22 | anxiolytic, hypnotic | |
Flubromazepam[25] | Templex | Research chemical | 4, 8, 12 | 4 | 1.5–8 | 100–220 | anxiolytic, hypnotic, amnesic, muscle relaxant, anticonvulsant |
Flubromazolam | Remnon | Research chemical | 0.25, 0.5 | 0.075 | 0.5-5 | 10-20[26] | hypnotic |
Fluclotizolam[d] | Research chemical | 0.25-0.5 | anxiolytic | ||||
Flunitrazepam | Rohypnol, Hipnosedon, Vulbegal, Fluscand, Flunipam, Ronal, Rohydorm, Hypnodorm | 1972 | 1, 2 | 1.5 | 0.5–3 | 18–200 | hypnotic |
Flunitrazolam | Research chemical | 0.25, 0.5 | 0.1 | 0.5-1 | 5-13 | hypnotic | |
Flurazepam | Dalmadorm, Dalmane, Fluzepam | 1970 | 30 | 20-25 | 1–1.5 | 40–250 | hypnotic |
Flutazolam | Coreminal | 4 | 10 | 1-3 | 47-100 | hypnotic | |
Flutemazepam | Research chemical | 1 | 0.5-5 | 8-20 | hypnotic, anxiolytic, anticonvulsant, muscle relaxant[27] | ||
Flutoprazepam | Restas | 1984 | 1, 2 | 2.5 | 0.5–9 | 87[28] | hypnotic, anticonvulsant, muscle relaxant |
Halazepam | Alapryl, Paxipam | 1981 | 20, 40 | 40 | 3–6 | 15-35 | anxiolytic |
Ketazolam | Anxon, Sedotime | 1980 | 15, 30, 45 | 20 | 2.5–6 | 30-100 | anxiolytic |
Loprazolam | Dormonoct, Havlane | 1983 | 1, 2 | 1.5 | 2–5 | 6–20[29] | hypnotic |
Lorazepam | Ativan, Orfidal, Lorenin, Lorsilan, Temesta, Tavor, Lorabenz | 1977 | 0.5, 1, 2, 2.5 | 1 | 2–4 | 10–20 | anxiolytic, anticonvulsant, hypnotic, muscle relaxant[30][14][31] |
Lormetazepam | Loramet, Noctamid, Pronoctan | 1984 | 1, 2 | 1.5 | 0.5–2 | 10-12 | hypnotic, anxiolytic |
Meclonazepam | Research chemical | 6 | anxiolytic | ||||
Medazepam | Nobrium, Ansilan, Mezapam, Rudotel, Raporan | 10 | 10 | 4-8 | 36–200 | anxiolytic | |
Metizolam[d] | Research chemical | 1, 2, 4 | 2–4 | 12 | anxiolytic | ||
Mexazolam | Melex, Sedoxil | 0.5, 1 | 1–2 | anxiolytic | |||
Midazolam | Dormicum, Flormidal, Versed, Hypnovel, Dormonid | 1985 | 7.5, 15 | 10 (oral)
4 (IV) |
0.5–1 | 1.8-6 | hypnotic, anticonvulsant |
Nifoxipam | Research chemical | 0.5, 1, 2 | hypnotic | ||||
Nimetazepam | Erimin, Lavol | 1984 | 5 | 2.5-5 | 0.5–3 | 14–30 | hypnotic |
Nitemazepam | Research chemical | 2 | 0.5-5 | 10-27 | hypnotic, anticonvulsant | ||
Nitrazepam | Mogadon, Alodorm, Pacisyn, Dumolid, Nitrazadon | 1965 | 5, 10 | 5 | 0.5–7 | 17–48 | hypnotic, anticonvulsant |
Nitrazolam | Research chemical | 0.5, 1 | hypnotic | ||||
Nordazepam | Madar, Stilny | 5, 7.5, 15 | 10-15 | 30–150 | anxiolytic | ||
Norflurazepam | Research chemical | 5 | 47-100 | hypnotic | |||
Oxazepam | Seresta, Serax, Serenid, Serepax, Sobril, Oxabenz, Oxapax, Oxascand, Ox-Pam, Opamox, Alepam, Medopam, Murelax, Noripam, Purata | 1965 | 10, 15, 30, 50 | 30 | 3–4 | 4–11 | anxiolytic |
Phenazepam | Phenazepam, Phenzitat | Research chemical | 1.5–4 | 60 | anxiolytic, anticonvulsant | ||
Pinazepam | Domar, Duna | 5, 10 | 40–100 | anxiolytic | |||
Prazepam | Demetrin, Lysanxia, Prazene, Centrax | 1976 | 10, 20, 30 | 15-20 | 2–6 | 36–200 | anxiolytic |
Premazepam | Not approved | 15 | 2–6 | 10–13 | anxiolytic | ||
Pyrazolam | Research chemical | 0.25, 0.5, 1 | 1–1.5 | 16–18[32] | anxiolytic, amnesic | ||
Quazepam | Doral, Quiedorm | 1985 | 15 | 20 | 1–5 | Zdroj:https://en.wikipedia.org?pojem=Benzodiazepine_equivalence