SEDATIVE & HYPNOTIC

DRUGS

BY
SHAHZAD TAHIR
M.phil Chemistry
Sedative & Hypnotic Drugs
A sedative is a substance that induces sedation by reducing irritability [1] or excitement.[2]
They are CNS depressants and interact with brain activity causing its deceleration. Various kinds
of sedatives can be distinguished, but the majority of them affect the neurotransmitter gamma-
aminobutyric acid (GABA). In spite of the fact that each sedative acts in its own way, most
produce relaxing effects by increasing GABA activity.[3]
Hypnotic (from Greek Hypnos, sleep[1]), or soporific drugs, commonly known as sleeping pills,
are a class of psychoactive drugs whose primary function is to induce sleep[2] (or surgical
anesthesia and to treat insomnia (sleeplessness).
This group of drugs is related to sedatives. Whereas the term sedative describes drugs that
serve to calm or relieve anxiety, the term hypnotic generally describes drugs whose main
purpose is to initiate, sustain, or lengthen sleep. Because these two functions frequently
overlap, and because drugs in this class generally produce dose-dependent effects (ranging
from anxiolysis to loss of consciousness), they are often referred to collectively as sedative-
hypnotic drugs.[3]
This group is related to hypnotics. The term sedative describes drugs that serve to calm or
relieve anxiety, whereas the term hypnotic describes drugs whose main purpose is to initiate,
sustain, or lengthen sleep. Because these two functions frequently overlap, and because drugs
in this class generally produce dose-dependent effects (ranging from anxiolysis to loss of
consciousness) they are often referred to collectively as sedative-hypnotic drugs.[4]
Sedatives can be used to produce an overly-calming effect (alcohol being the most common
sedating drug). In the event of an overdose or if combined with another sedative, many of
these drugs can cause deep unconsciousness and even death.[5]
Hypnotic effects involve more pronounced depression of the central nervous system than
sedation, and this can be achieved with most sedative drugs simply by increasing the dose.
Graded dose-dependent depression of central nervous system function is a characteristic of
sedative-hypnotics.
Benzodiazepines not to lead general anesthesia, rarely death. Barbiturates the older sedative-
hypnotics, general depression of central nervous system. With such drugs, an increase in dose
above that needed for hypnosis may lead to a state of general anesthesia. At still higher doses,
it may depress respiratory and vasomotor centers in the medulla, leading to coma and death.
Other classes of drugs chloral hydrate, Proudfoot H, et al. [6]
Doctors often administer sedatives to patients in order to dull the patient's anxiety related to
painful or anxiety-provoking procedures. Although sedatives do not relieve pain in themselves,
they can be a useful adjunct to analgesics in preparing patients for surgery, and are commonly
given to patients before they are anaesthetized, or before other highly uncomfortable and
invasive procedures like cardiac catheterization, colonoscopy or MRI.[7]
The first benzodiazepine, chlordiazepoxide, was synthesised by accident in 1961. Derivative of
1,4- benzodiazepines. carboxamide group in the 7-membered heterocyclic ring structure. A
substituent in the 7 position, such as a halogen or a nitro group, about 20 are available for
clinical use. They are basically similar in their pharmacological actions, though some degree of
selectivity has been reported. It is possible that selectivity with respect to two types of
benzodiazepine receptor may account for these differences. From a clinical point of view,
difference in pharmacokinetic behavior are more important than difference in profile of activity.
[8]
When we talk about pharmacological affects, its Reduction of anxiety and aggression, affects
the hippocampus and nucleus amygdalae, Sedation and induction of sleep, The latency of sleep
onset is decreased, The duration of stage 2 NREM sleep is
increased, The duration of slow-wave sleep is decreased. Anticonvulsant and antiseizure,
Muscle relaxation (relax contracted muscle in joint disease or muscle pasm). Other effects
includes lead to temporary amnesia, decrease the dosage of anesthetic, and depress
respiratory and cardiovascular function.[9]
Reasons for their extensive clinical use includes Great margin of safety, Little effect on REM
sleep, Little hepatic microsomal drug-metabolizing enzymes, Slight physiologic and psychologic
dependence and withdrawal syndrome, Less adverse effects such as residual drowsiness and
incoordination movement.[10]
Benzodiazepines act very selectively on GABAA-receptors, which mediate the fast inhibitory
synaptic response produced by activity in GABA-ergic neurons. The effect of benzodiazepines is
to enhance the response to GABA, by facilitating the opening of GABA-activated chloride
channels (an increase in the frequency of channel opening, but no change in the conductance
or mean open time). Benzodiazepines bind specifically to a regulatory site on the receptor,
distinct from the GABA binding site, and enhanced receptor affinity for GABA.[11] The GABAA-
receptors is a ligand-gated ion channel consisting of a pentameric assembly of subunits.
Some sedatives can cause psychological and physical dependence when taken regularly over a
period of time, even at therapeutic doses. [6][7][8] Dependent users may get withdrawal
symptoms ranging from restlessness and insomnia to convulsions and death. When users
become psychologically dependent, they feel as if they need the drug to function, although
physical dependence does not necessarily occur, particularly with a short course of use. In both
types of dependences, finding and using the sedative becomes the focus in life. Both physical
and psychological dependence can be treated with therapy.
Many sedatives can be misused, but barbiturates and benzodiazepines are responsible for most
of the problems with sedative use due to their widespread recreational or non-medical use.
People who have difficulty dealing with stress, anxiety or sleeplessness may overuse or become
dependent on sedatives. Some heroin users may take them either to supplement their drug or
to substitute for it. Stimulant users may take sedatives to calm excessive jitteriness. Others take
sedatives recreationally to relax and forget their worries.[12] Barbiturate overdose is a factor in
nearly one-third of all reported drug-related deaths. These include suicides and accidental drug
poisonings. Accidental deaths sometimes occur when a drowsy, confused user repeats doses, or
when sedatives are taken with alcohol.[13]

References:

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2. Smith, Rebecca (25 October 2010). "'Chemical cosh' will be cut for dementia
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