Benzodiazepines short-acting

Breimer DD, Jochemsen R and von Albert HH (1980) Pharmacokinetics of benzodiazepines. Short-acting versus long-acting. Arzneimittelforschung 30 875-881. 

As noted, the barbiturates once were used extensively as sedative-hypnotic drugs, but except for certain specialized uses they now have been replaced by the safer benzodiazepines. Short-acting barbiturates still are used to produce anesthesia. Other current uses include emergency treatment of convulsions and prevention of seizures in persons with certain types of epilepsy (Perrine, 1996). 

Midazolam (Versed), a short-acting benzodiazepine CNS depressant, is used as a preanesthetic drug to relieve anxiety for induction of anesthesia for conscious sedation before minor procedures, such as endoscopic procedures and to supplement nitrous oxide and oxygen for short surgical procedures. When the drug is used for induction anesthesia, the patient gradually loses consciousness during a period of 1 to 2 minutes. 

A rebound sleep disturbance has been found after only 7—10 days of treatment with therapeutic doses of triazolam (Greenblatt et al. 1987). Others have described a withdrawal syndrome after substitution of a short-acting benzodiazepine for a long-acting benzodiazepine (Conell and Berhn 1983). Rebound insomnia may occur with zolpidem. 

Cocaine or stimulant intoxication may require administration of a small dose of a short-acting benzodiazepine (e.g., lorazepam 1 to 2 mg) for agitation or severe anxiety. Antipsychotics (e.g., haloperidol 2 to 5 mg) should be used only if psychosis is present. If hyperthermia is present, initiate cooling measures. 

Secobarbital exhibits the same pharmacologic properties as other members of the barbiturate class. Most nonmedical use is with short-acting barbiturates, such as secobarbital. Although there may be considerable tolerance to the sedative and intoxicating effects of the drug, the lethal dose is not much greater in addicted than in normal persons. Tolerance does not develop to the respiratory effect. The combination of alcohol and barbiturates may lead to fatalities because of their combined respiratory depressive effects. Similar outcomes may occur with the benzodiazepines. Severe withdrawal symptoms in epileptic patients may include grand mal seizures and delirium. 

Non-motor signs of the disorder are also treatable with symptomatic medications. The frequent mood disorder can be treated with standard antidepressants, including tricyclics (such as amitryptiline) or serotonin reuptake inhibitors (SSRIs, such as fluoxetine or sertraline). This treatment is not without risks in these patients, as it may trigger manic episodes or may even precipitate suicide. Anxiety responds to benzodiazepines, as well as to effective treatment of depression. Long-acting benzodiazepines are favored over short-acting ones because of the lesser abuse potential. Some of the behavioral abnormalities may respond to treatment with the neuroleptics as well. The use of atypical neuroleptics, such as clozapine is preferred over the typical neuroleptics as they may help to control dyskinesias with relatively few extrapyramidal side-effects (Ch. 54). 

The use of benzodiazepines should be avoided. There are other safer pharmacological alternatives. Benzodiazepine withdrawal may play a role in the occurrence of delirium in the elderly. Other withdrawal symptoms include tremor, agitation, insomnia and seizures (Turnheim 2003). Thus, when there is long-term use of benzodiazepines abrupt discontinuation might be difficult. Discontinuation should however not be withheld but done slowly and step-wise. If benzodiazepines are used in the elderly, short-acting benzodiazepines such as oxazepam are preferred, because they do not accumulate in the elderly to the same extent (Kompoliti and Goetz 1998). If short-acting benzodiazepines are used they should be prescribed with caution, at low doses, and for short periods. As with all pharmacotherapy the effects should be evaluated. Benzodiazepines are sometimes used as a behavioural control. One should always ask if this use is for the benefit of staff or the benefit of the patient. The presence of staff may be sufficient for behavioural control. 

Medications may be necessary for patients with delirium especially in patients with severe behavioural disturbances and agitation. Any medications used may however be hazardous and actually lengthen the condition. A continuous reassessment of the need for theses kind of drugs should be done. Antipsychotic drugs may be needed especially if vision hallucinations and agitated behaviour are predominant. Short-acting benzodiazepines may be used for a limited time. There is no... 

Substance-Induced Anxiety Disorder. Numerous medicines and drugs of abuse can produce panic attacks. Panic attacks can be triggered by central nervous system stimulants such as cocaine, methamphetamine, caffeine, over-the-counter herbal stimulants such as ephedra, or any of the medications commonly used to treat narcolepsy and ADHD, including psychostimulants and modafinil. Thyroid supplementation with thyroxine (Synthroid) or triiodothyronine (Cytomel) can rarely produce panic attacks. Abrupt withdrawal from central nervous system depressants such as alcohol, barbiturates, and benzodiazepines can cause panic attacks as well. This can be especially problematic with short-acting benzodiazepines such as alprazolam (Xanax), which is an effective treatment for panic disorder but which has been associated with between dose withdrawal symptoms. 

Benzodiazepines. Like the barbiturates, benzodiazepines bind to the GABA receptor and are therefore cross-tolerant with alcohol. As a result, they also make suitable replacement medications for alcohol and are widely used for alcohol detoxification. Theoretically, any benzodiazepine can be used to treat alcohol withdrawal. However, short-acting benzodiazepines such as alprazolam (Xanax) are often avoided because breakthrough withdrawal may occur between doses. Intermediate to long-acting benzodiazepines including chlordiazepoxide (Librium), diazepam (Valium), oxazepam (Serax), lorazepam (Ativan), and clonazepam (Klonopin) are more commonly utilized. 

Anxiolytics. The use of anxiety-reducing medications has not been systematically assessed in the treatment of AN. Nevertheless, many clinicians anecdotally report that the use of short-acting benzodiazepine such as lorazepam (Ativan) prior to mealtime diminishes anticipatory anxiety and thereby facilitates refeeding. 

Q80 Lorazepam may be used for short-term relief of severe anxiety. Lorazepam is a short-acting benzodiazepine. 

Lorazepam is a short-acting benzodiazepine indicated for use in relieving anxiety and insomnia. Lorazepam may also be administered perioperatively to alleviate pain and in status epilepticus. Imipramine is a tricyclic antidepressant, paroxetine is a selective serotonin re-uptake inhibitor, venlafaxine is a serotonin and adrenaline re-uptake inhibitor and moclobemide is a reversible monoamine oxidase inhibitor. Imipramine, paroxetine, venlafaxine and moclobemide are all classified as antidepressants. 

Discontinuation of a hypnotic after a month of continued use can cause a rebound of REM (rapid eye movement) sleep. The duration of action of a hypnotic is determined not only by the half-life of the mother substance but especially by their biological half-life determined by the half-life of the mother substance and the biological active metabolites. On this basis the benzodiazepines can be divided in four different groups ultra short-acting with a half-life < 6 hours such as midazolam and triazolam, short-acting with half-lives between 6 and 12 hours like lormetazepam, loprazolam, oxazepam and temazepam. Alprazolam, bromazepam... 

Opioids play an important role in anesthetic practice. Opioid analgesics potentiate the efficacy of anesthetics. They can be given as part of the premedication as well as during the operation. Examples of short acting agents with high potency are fentanyl, sufentanyl, alfentanil and remifentanil. Because of their hemodynamic stability these agents can be used for patients with compromised myocardial function. Respiration must be maintained artificially and may be depressed into the postoperative period. They are usually supplemented with inhalation anesthetic, benzodiazepines or propofol. 

---