Class
They belong
to the class of drugs anxiolytics (Sedatives) and hypnotics. Cause sedation
with the concomitant relief from anxiety.
Type of Effects
Include sedation when taken in low to moderate
dose. At high dose they cause hypnosis and further at very high dose impair the
brain function by severely depressing its electrical activity.
Benzodiazepines
are the most widely used anxiolytics, by replacing barbiturates and meprobamate.
Effects on the body: -
1) Sedation:- They cause calming effect
with concomitant anxiolytic effect. This response is due the effect on the
central nervous system, By decreasing the electrical activity. Sedative and
anxiolytic effect is some time accompanied with depressive effect on
psychomotor and cognitive functions.
2) Hypnosis :- hypnosis is also
centrally mediate function of benzodiazepines, which occur on high doses. They
cause hypnosis by decreasing latency of sleep (time to fall a sleep), increase
Non-Rapid eye moment sleep, and decrease Rapid Eye movement sleep.
3) Anesthesia:- As shown previously at
higher doses then required for hypnosis they depress central nervous system to
a point of stage 3 general anesthesia.
4) Anticonvulsant effect:- Many benzodiazepines
have ability to prevent the generation of epileptiform electrical activity in
the CNS. Selective agent having this
tendency include lorazepam, diazepam, clonazepam and Nitrazepam.
5) Muscles Relaxation:- at high doses
they my inhibit transmission at muscular level by locally affecting neurons
there. And also mediated by presynaptic inhibition of spinal cord.
6) Effect on Respiration and CVS:- This
respiratory depression is due to the medullary
respiratory center suppression. Even at normal dose it may impair
respiratory functions in susceptible and respiratory patient. In contrast to Respiratory functions CVS
function are no announced in normal people even at hypnotic dose. But may
affect people with hypovolemic status, CVS diseases and Heart failure. This
action is due to suppression of medullary vasomotor area of the hind brain.
7) Anterograde amnesia:- Short term
memory loss is due to the effect on CNS by alpha1 GABA sub type. In this
duration of maintained dose individual become un-aware of environment.
Addiction
If used in a high doses for prolong time they can cause
dependency ( fall in Schedule 4 of controlled substances having a low potency
to cause dependency and Addiction). This dependency is due to the effect on
reward pathway. Where it the drugs cause increase in the level of
neurotransmitters particularly dopamine (causing euphoria, state of relaxation
and calmness). This stimulation of reward pathway lead to Psychological
dependency. Dependency is also due to prevent the with drawl effects associated
with benzodiazepines like insomnia, anxiety and central nervous system
excitability that may lead to convulsion.
Tolerance to
Benzodiazepines
Tolerance to benzodiazepines is not likely to be contributed
by metabolic induction. Here increase metabolism play little to no role in
tolerance. Benzodiazepines tolerance is due to down regulation of receptors.
Tolerance to benzodiazepines is not vary abrupt and take long time to be
generated.
With drawl of
benzodiazepines include symptoms like
Anxiety, depression, increased heart rate, insomnia, high
blood pressure, excessive sweeting, tremors, hallucination, seizures and
convulsions.
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