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From miracle drug to risk medication

indication Adult dosage (mg / d) Half-life (h), active metabolites and their half-life (h) CYP metabolism Equivalent dose (mg) Alprazolam acute and chronic states of tension, excitement and anxiety 3 × 0.25 - 0.5, max. 4 12-15 hydroxyalprazolam (12-15) CYP3A4 0,5 Bromazepam acute and chronic states of tension, excitement and anxiety Start with 3 - 6 in 2 to 4 single doses, outpatient in individual cases up to 12, in the clinic until 18 15 - 28 hydroxybromazepam (unknown) CYP3A4 5 – 6 Brotizolam short-term treatment of problems falling and staying asleep 0,125 – 0,25 4 - 9 9-hydroxymethyl brotizolam (3 - 6)
6-hydroxymethyl brotizolam (3 - 6) 0,5 Clonazepam - Mainly as an additional therapy for epilepsy, especially absences including atypical absences, Lennox-Gastaut syndrome, myoclonic and atonic seizures
- Infantile seizures (including West syndrome) and tonic-clonic seizures (only as additional therapy or in the event of non-response to other drugs) orally: 0.5 - 4, maximum 8, intravenous: slow (0.5 to 1 ml / min) injection of 2 ml (1 mg) solution. The dose can be repeated if necessary, possibly as an i. v. Infusion. Maximum daily dose about 13 mg i.v. v. 18 - 50 no active metabolites CYP3A4, NAT2 0,5 Flunitrazepam Short-term treatment of sleep disorders 0.5 - 1, in exceptional cases 2 18-26 Desmethyl-Flunitrazepam (20-30) Desmethyl-Hydroxyflunitrazepam (9-25) CYP3A4 1 Lorazepam - Short-term treatment of anxiety, tension and excitement and the resulting sleep disorders
- Sedation before diagnostic and surgical procedures
- i.v./i.m. Ampoules: Calming (basic sedation) before and during surgical and diagnostic interventions
- Treatment initiation of severe neurotic anxiety symptoms and pronounced phobias (preferably IV)
- adjuvant short-term treatment of severe anxiety and agitation in psychoses and depression
- Status epilepticus orally: 0.5 - 2.5, divided into 2 to 3 single doses or as a single dose in the evening, maximum 7.5
- intramuscular / intravenous: 2 mg starting dose (0.05 mg / kg body weight), maximum 8 12-16 no active metabolites Glucuronidation via UGT2B15 1 Lormetazepam Short term treatment for insomnia Single dose: 1, for elderly patients 0.5, in individual cases: double the dose 10-12 lorazepam (12-16) Glucuronidation, renal elimination 1 – 2 Midazolam -peroral: sedation in premedication before diagnostic and surgical interventions
- i. v./i. m .: Analgesic sedation before and during diagnostic or therapeutic interventions with or without local anesthetics, anesthesia: premedication before induction of anesthesia, induction of anesthesia, sedating components of a combination anesthesia (only for adults), sedation in the intensive care unit 30 to 60 min before the diagnostic or surgical procedure orally: 7.5 - 15
intramuscular / intravenous: see product information 2 - 3 alpha-hydroxymidazolam (1) CYP3A4 10 Nitrazepam Short-term treatment of sleep disorders 2.5 - 5, maximum 10 18-30 no active metabolites CYP3A4 10 Oxazepam acute and chronic states of anxiety, tension and excitement, disorders of staying asleep 10 - 30, maximum 60 4-15 no active metabolites Glucuronidation via UGT2B15, UGT2B7, UGT1A9, renal elimination 20 Temazepam Short term treatment of sleep disorders in adults Maximum daily dose: 10 - 20, in exceptional cases: 30 - 40 8-22 oxazepam (4-15) CYP3A4, CYP3C19, glucuronidation via UGT2B7, UGT2B15 20 Triazolam Short-term treatment of sleep disorders 0.125-0.25 (adults), elderly: 0.125 2 - 5 hydroxytriazolam (2 - 4) CYP3A4 0,5