Short-term hypnotics

Clomethiazole is used as a hypnotic for older patients because of its lack of hangover effect but it can still produce dependence. It should be used as a hypnotic only in the short-term. Hypnotics generally should be avoided in older people because of the risk of confusion, ataxia and falls as a consequence. 

A barbiturate with a hydroxy group in the side chain (XXXV) (ipronal) was reported to have tranquiilising activity in a clinical study when given orally for a 2 to 3 week period [182]. Its short-term hypnotic effect was found to be very weak, and it was reported not to be an anticonvulsant. However, it markedly potentiates the hypnotic effect of phenobarbitone and barbitone. This effect is not produced with non-barbiturate hypnotics, such as chloral hydrate or ether. 

Ideally limit hypnotic therapy to short-term use, and reevaluate after 2 to 3 weeks of therapy. 

Transient and short-term insomnia should be treated with good sleep hygiene and careful use of sedative-hypnotics if necessary. 

Acute Phase Treatment. Hypnotic medications are useful for short-term treatment of insomnia, but they should always be accompanied by behavioral and psychoeducational treatments, including a review of good sleep hygiene practices. It may also include more aggressive measures such as relaxation training, sleep restriction therapy, and stimulus control therapy. 

Timing of drug administration Take zaleplon immediately before bedtime or after going to bed and experiencing difficulty falling asleep. As with all sedatives/hypnotics, taking zaleplon while ambulatory may result in short-term memory impairment, hallucinations, impaired coordination, dizziness, and lightheadedness. 

Hypnotic Short-term treatment of insomnia, because barbiturates appear to lose their effectiveness in sleep induction and maintenance after 2 weeks. If insomnia persists, seek alternative therapy (including nondrug) for chronic insomnia. Preanesthetic Used as preanesthetic sedatives. 

Estazolam (Prosom) [C-IV] [Hypnotic/Benzodiazepine] Uses Short-term management of insomnia Action Benzodiazepine Dose 1-2 mg PO qhs PRN -1- in hqjatic impair/elderly/debilitated Caution [X, -] t Effects w/ CNS d ressants Contra PRG Disp Tabs SE Somnolence, weakness, palpitations, anaphylaxis, angioedema, amnesia Interactions t Effects W7 amoxicillin, clarithromycin T effects OF diaz am, phen5rtoin, warfarin X effects W7 food X effects OF azole antifungals, digoxin EMS Use caution w/ other benzodiazepines, may need a reduced dose concurrent EtOH and caffeine use can t CNS effects OD May cause alt ed reflexes, drowsiness, CNS depression, slurred speech, and Szs flumazenU can be used as an antidote... 

Zolpidem (1) is an effective hypnotic agent indicated for the short-term treatment of insomnia. Zolpidem interacts with the GABAa receptor, and its pharmacological effect is blocked by the benzodiazepine-receptor antagonist fiumazenil (Sanger and Depoortere, 1998). Zolpidem displaces benzodiazepines more selectively from the cerebellum than the hippocampus or spinal cord, consistent with preferential interaction with the ajGABAA receptor subtype (sometimes referred to as the benzodiazepine coi receptor). Studies... 

It does not cause cognitive impairment and has a low potential for abuse. It does not show withdrawal reactions and has no anticonvulsive, hypnotic, muscle relaxant and sedative effects. The anxiolytic effect gradually evolves over 1-3 weeks, it does not potentiate the sedative effects of alcohol and is indicated for the short-term management of generalized anxiety disorder. 

Geriatric Considerations - Summary Benzodiazepines are effective anxiolytic agents, and hypnotics. These drugs should be reserved for short-term use. SSRls are preferred for long-term management of anxiety disorders in older adults, and sedat-... 

Some patients may experience jitteriness, restlessness, muscle tension, and disturbed sleep. These side effects typically occur early in treatment, before the antidepressant effect. All patients should be informed of the possibility of these side effects and be reassured that if they develop, they tend to be transient. In patients with preexisting anxiety, therapy should be started at low doses, with subsequent titration as tolerated. If overstimulation occurs with this approach, it will be less likely to be severe enough to result in nonadherence with therapy. The short-term use of a benzodiazepine also may help the patient cope with overstimulation in the early stages of treatment until tolerance to this side effect occurs. Despite these common transient stimulating effects, SSRIs are clearly effective in patients with anxiety or agitated depression. Similarly, insomnia that commonly occurs early in treatment may be tolerable if the patient is reassured that the side effect will be transient. Symptomatic, short-term treatment with a hypnotic at bedtime is reasonable. 

Both zolpidem and zaleplon are available in 5- and 10-mg tablets for oral administration. The maximum recommended dose for adults is 10 mg/day and 20 mg/day, respectively, administered at night. The initial dose for elderly persons should not exceed 5 mg. Caution is advised in patients with hepatic dysfunction. In general, hypnotics should be limited to short-term use, with reevaluation for more extended therapy (see below under Treatment of Specific Conditions ). 

This is an extension of the crossover design that applies in situations where more than two treatment conditions are being evaluated. Each subject receives each treatment successively but in a different sequence. This design can be used in the case of single-dose experimental trials, such as studies of cognitive function, psychomotor performance, psyehophysiological responses, etc. in healthy volunteers (Chapter 3) but also in therapeutic short-term trials of hypnotics or anxiolytics. 

It is a novel hypnotic belonging to cyclopyrrolone derivative. It is useful in short term management of insorrmia and has low abuse potential. 

Dyssomnias consist of problems associated with the amount, quality or timing of sleep, whereas parasomnias involve pathological, behavioral, or psychological events that occur with sleep, specific sleep stages, or sleep-wake transitions (see also Chapter 11). The other two categories usually require treatment of the mental or physical condition that has created the sleep disturbance. For all categories, the short-term use of hypnotics may play a role. 

BZDs may offer temporary symptomatic relief for transient and short-term insomnia. They generally are not recommended as a long-term primary treatment for chronic insomnia or in patients with sleep apnea. Several of these agents are currently marketed in the United States or elsewhere for use as hypnotics ( Table 12-5), but other BZDs can also serve the same purpose. 

This non-BZD hypnotic, cyciopyrroione, is indicated for short-term management of insomnia. Zopiclone has a BZD-like profile, a short half-life of 3.5 to 6.5 hours, no active metabolites, minimal rebound effects, and less abuse potential than BZDs. The usual therapeutic dose is oral 7.5 mg administered 30 to 60 minutes before bedtime. Zopiclone has a well-documented capacity to reduce sleep latency, improve quality and duration of sleep, and reduce the frequency of nighttime awakenings. In clinical trials, 7.5 mg doses of zopiclone have been found to be as effective as triazolam 0.5 mg, temazepam 20 mg, flurazepam 15-30 mg, and nitrazepam 5 to 10 mg for the short-term treatment of insomnia (136). 

Zopiclone is relatively well tolerated (137). The most common adverse reaction is taste alteration. A postmarketing analysis of 10,000 cases revealed that zopiclone has a relatively low incidence of side effects (about 8%) (138). Like BZDs, zopiclone has a dose-related hangover effect (139). Rebound insomnia has occurred after short-term use (5 to 14 days) but does not appear to be as severe, even after abrupt withdrawal (140, 141). Abuse, tolerance, and physical and psychological dependence have been reported with zopiclone (142). Zopiclone has been shown to be as effective a hypnotic as triazolam in the elderly ( 143). More comparisons with short to medium half-life BZDs for the treatment of insomnia are needed to show that zopiclone has an advantage over the BZDs. 

This newest non-BZD hypnotic is a pyrazolopyrimidine derivative with a fuii agonist activity on centrai BZD receptors B2 type. It is an effective hypnotic for the short-term treatment of insomnia. Because of its very short half-life (almost an hour), it may be useful for patients experiencing difficulty falling asleep and in those who wake up at night and who have trouble falling back to sleep. Zaleplon is rapidly absorbed after oral administration and its mean, apparent elimination half-life is similar to that obtained after i.v. infusion. Zaleplon is extensively metabolized in the liver by aldehyde oxidase, and to a lesser extent by CYP3A4. This drug is excreted in the urine (156). 

Small doses of trazodone (25 to 50 mg) at bedtime may be useful as a sedative-hypnotic. More data are required on pain control and analgesia using low-dose opioids on a short-term basis, which may also benefit anxiety. For example, the use of morphine in patients with advanced disease has been found to be particularly helpful in decreasing their associated anxiety. 

With the use of major tranquillisers, for example, thioridazine, chlorpromazine, or perphenazine, it is possible to withdraw opiate dependents who are highly motivated. The dosages can be titrated to the degree of clinical symptoms and this can be monitored with key carers through an out-patient clinic. The use of hypnotics should be restricted to short-term use due to their own dependency problems, but they can be a useful addition, particularly in the early phases of the treatment programme. 

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