Products
Sedatives are commercially available in the form of tablets, melting tablets, drops, as injectables and tinctures, among others.
Structure and properties
Sedatives do not have a uniform chemical structure.
Effects
The active ingredients have sedative properties. Some are additionally antianxiety, sleep-inducing, antipsychotic, antidepressant, and anticonvulsant. The effects are due to promotion of inhibitory mechanisms in the central nervous system, for example, by binding to the GABA-A receptor.
Indications
For the treatment of states of excitement and tension, nervousness, and restlessness.
Dosage
According to the professional information. Dosage depends on the active ingredients.
Abuse
Sedatives can be used as depressant intoxicants. The benzodiazepines are abused as so-called “date rape drugs.” The barbiturates can cause death if overdosed and have therefore been used for suicides and for homicides.
Agents
1st-generation antihistamines:
- Doxylamine (Sanalepsi).
- Diphenhydramine
Benzodiazepines:
- E.g. Lorazepam (Temesta).
- Alprazolam (Xanax)
Antidepressants:
- E.g., mirtazapine (Remeron, generic, off-label).
- Trimipramine (Surmontil, generic, off-label).
Neuroleptics:
- E.g. Haloperidol (Haldol).
- Promazine (Prazine)
Barbiturates:
- Are rarely used today because an overdose is life-threatening.
Thiazoles:
- Clomethiazole (Distreneurin).
Beta-blockers:
- Propranolol (Inderal, generic).
Phytopharmaceuticals (herbal medicines):
- Valerian
- Cannabis
- Melissa
- Hops
- St. John’s wort
- California poppy
- Kava
- Lavender
- Orange blossom
- Passionflower
Minerals:
- Magnesium
Contraindications
Full precautions can be found in the drug label.
Interactions
Centrally depressant drugs, such as anxiolytics, opioids, neuroleptics, or antidepressants, as well as alcohol, may increase adverse effects. The combination of multiple depressant agents may be life-threatening in some circumstances. Alcohol should be avoided. Some sedatives interact with CYP450 isoenzymes.
Adverse effects
Possible adverse effects of sedatives include (selection, depending on active ingredient):
- Central disturbances such as fatigue, cognitive disturbances, and drowsiness, headache, dizziness, impaired responsiveness
- Psychiatric disorders and paradoxical reactions.
- Dry mouth, gastrointestinal disorders.
- Anterograde amnesia
The benzodiazepines and barbiturates can lead to psychological and physical dependence and can cause withdrawal symptoms if discontinued quickly.
