Sleeping Pills: Effects, Side Effects, Dosage and Uses

Products

Sleeping pills are most commonly taken in the form of tablets (“sleeping pills“). In addition, melting tablets, injectables, drops, teas and tinctures are also available, among others. The technical term hypnotics is derived from Hypnos, the Greek god of sleep.

Structure and properties

Within the sleeping pills, groups can be identified which have a common structure (see below).

Effects

Sleeping pills have sleep-inducing and sleep-promoting (hypnotic) properties. They may additionally be antianxiety, sedative, narcotic, anticholinergic, and anticonvulsant. The effects are due to attenuation of the central nervous system by promoting centrally inhibitory mechanisms, for example, by binding to the postsynaptic GABA-A receptor.

Indications

For short-term treatment of sleep onset and sleep maintenance disorders.

Dosage

According to the professional information. The correct dosage depends on the active ingredient used. For example, tablets containing valerian are taken up to one hour before bedtime. Zolpidem, on the other hand, should be administered immediately before bedtime or in bed, according to the professional information. The maximum dose should not be exceeded. Repeated administration during the night is not allowed with some medications. It should be started with a low dose. The duration of treatment should usually be kept short because many sleep medications can be addictive, especially the benzodiazepines, the Z-drugs, and the barbiturates. From our experience, the 1st generation antihistamines can also cause habituation. Discontinuation should be gradual to avoid withdrawal symptoms. Before using sleeping pills, nonpharmacologic therapy methods should be tried (see below, Checklist).

Abuse

The benzodiazepines are abused as depressant intoxicants and as so-called “date rape drugs.” The barbiturates can cause death if overdosed and have therefore been used for suicides and for homicides.

Agents

Herbal medicines (phytopharmaceuticals):

  • Valerian roots
  • Bryophyllum
  • Orange blossom
  • Melissa leaves
  • Passionflower herb
  • Hop cone
  • California poppy
  • Kavarhizome
  • See also under sleeping teas

1st generation antihistamines:

Alcohols:

  • Ethanol (not approved as a medicinal product for this indication).

Amino acids:

  • Tryptophan

Benzodiazepines:

Z-Drugs:

Antidepressants:

Neuroleptics:

  • Quetiapine (Seroquel, off-label).
  • Promethazine (off-label)

Melatonin and melatonin receptor agonists:

  • Melatonin (Circadin, melatonin is available over-the-counter in some countries).
  • Agomelatine (not approved for this indication).
  • Ramelteon (Rozerem, USA).

Orexin receptor antagonists:

Aldehydes:

  • Chloral hydrate (Nervifene)
  • Paraldehyde (out of trade)

Thiazole derivatives:

Barbiturates:

  • Are rarely used today

Quinazolines:

Contraindications

Full precautions can be found in the drug label.

Interactions

Centrally depressant drugs, such as sedatives, anxiolytics, opioids, neuroleptics, or antidepressants, as well as alcohol, may increase adverse effects. The combination of several depressant agents can be life-threatening under certain circumstances. Alcohol should be avoided. Some sleeping pills interact with CYP450 isoenzymes.

Adverse effects

Possible adverse effects of sleep aids include (selection):

  • Central disorders such as fatigue, cognitive impairment, and next-day sleepiness (“hangover”), headache, dizziness, impaired responsiveness
  • Psychiatric disorders and paradoxical reactions
  • Dry mouth, gastrointestinal disorders.
  • Anterograde amnesia

Many sleeping pills can lead to psychological and physical dependence and can cause withdrawal symptoms if stopped quickly. Depending on the duration of action, sleeping pills can still cause fatigue the next day (see above). This can lead to impaired concentration and increase the risk of car accidents and falls.