Sedatives and hypontics are the most desired drugs.
Decreased responsiveness to a constant level of stimulation.(Psychomotor retardation)
Reduced excitation, calming and relaxing effect, without excessive drowsiness.
These drugs exert a calming effect and reduce excitement in hyperactive individuals, with little or no effect on motor or mental functions.
Increased sedation –> increased drowsiness –> induction of state of sleep
The drugs which produce drowsiness & encourage the onset & maintenance of a state of sleep.
Hypnotics produce drowsiness and facilitate the onset of sleep, resembling normal sleep pattern, causing psychomotor slowing.
Sleep consists of REM and non-REM sleep. REM is for 20-30% of time. 80-100 minute cycle is repeated.
It is further divided into four stages:
|Stages of sleep||Wave pattern|
||a, b theta|
||Theta, delta, K complexes sleep spindles|
||Delta (high voltage)|
|Delta||< 4/sec||50 µ v|
|Theta||4-7/sec||May vary from 0-300 µv|
|K complex||brief high voltage activity|
|Sleep spindles||10-14/sec||50 µv interspersed with delta wave|
The drug should resemble normal sleep pattern. Normal architecture should not be disturbed. Large number of drugs are available.
Actually all drugs are depressants of CNS. Some non-selective, like barbiturates cause non-selective depression of CNS.
- Depress CNS –graded depression
- Sedative in small dose,
As dose is increased moderately, there is hypnosis,
Further higher dose produces general anesthesia.
As concentration is further increased, coma or even death may occur.
Dose should not exceed the level of hypnosis.
These drugs are also used for anxiety treatment, thus are anxiolytic drugs. All sedatives relieve anxiety, by causing sedation and drowsiness.
A subjective feeling , fear or apprehension, with or without any obvious cause, usually accompanied by autonomic disturbance, manifested by sympathetic over activity.
Symptoms are of sympathetic over activity.
Mild anxiety is common and needs no treatment. If symptoms become severe, interfering with normal routine of life, only then drugs are prescribed.
These are also known as minor tranquilizers.
Major tranquilizers are called neuroleptics.
|Normal anxiety||Pathological anxiety|
|Same drug in smaller dose, acts as sedative5mg dose of diazepam to produce anti-anxiety effects and sleep||Higher dose is required|
Normal or physiological (Adaptive)
i.e. in interviews, examinations
Loss of sleep, deprivation of sleep. Varying from children (GH secretion) to elderly.
Normal adult requires 6-8 hours sleep.
Insomnia may be:
- Transient insomnia
Normal individual undergoing emotional disturbances (family, work, etc.) 1-2 doses of hypnotics are indicated to help cope with situation.
- Short term insomnia
Also related to emotional disturbances but may reoccur (psychiological disturbance) subjective to feeling. 5-10 day hypnotic with some missing doses.
As continuous use of hypnotics leads to:
- Rebound insomnia
- Chronic insomnia
Rarely benefited by hypnotics. Routine ingestion of hypnotics may produce mild dependence.
Underlying cause needs to be seen, whether psychiatric problem, depression or pain.
Insomnia secondary to underlying cause has to be treated, if pain analgesic is prescribed along with hypnotic.
Sedatives and hypnotics are not prescribed to children and elderly.
Only sometimes given when someambolism (walking at night) occurs, involving hyperactive situations, night terrors, only if lack of sleep is detrimental.
Unjustified use leads to greater risk of person becoming ataxic and confused. May produce rebound insomnia, especially if drug is discontinued suddenly.
1. Non – Pharmacological
– Comfortable/conducive environment
– Stimulants like caffeine
– Comfortable environment, milk (tryptophan has soothing effect)
– Timing of sleep –fixed routine, better sleep habits
Benzodiazepines –small dose during day, higher dose at night,
Some tolerance does develop
Treatment of allied diseases
- Difficulty in falling a sleep ( Latency)
- Interrupted Sleep (Frequent awakenings)
- Early Morning wakening
- Non- Refreshing sleep
Sedatives are also used in hypertension, for short term and also for bronchoscopy and diagnostic procedures.
- Diazepam (Valium)
- Nitrazepam (Mogadon)
- Clonazepam (Pintril)
- Chlorazepate (Tranxene)-prodrug
- Bromazepam (lexatonel)
- Alprazolam (Xanax)
- Lorazepam (Ativan)
- oxazepam (Serax)
- Temazepam (Restoril)
- Midazolam (Versed)
- Triazolam (Halcion)
1. Imidazo pyridine derivative
2. Pyrazolo pyrimidine Derivative
3. Cyclo pyrrolone Derivatives
4. Melatonin Receptor Agonist
Long Acting (10-12 hrs)
Not preferred because of long hang overs
Intermediate Acting (6-8 hrs)
Short Acting (3-6 hrs)
– Chloral hydrate –dental extraction in children
Diphenhydramine & Promethazine
Helpful in pruritis and allergic rhinitis.
Flumazenil -Benzodiazepines Antagonist
Buspirone, Zolpidem, Zaleplon and other Sedative/Hypnotic Drugs