Benzodiazepine equivalence - Biblioteka.sk

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Benzodiazepine equivalence
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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]

Zdroj:https://en.wikipedia.org?pojem=Benzodiazepine_equivalence
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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,

hypnotic, muscle relaxant

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