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Transcript
Journal
Athaar Yosuef Jaha
User 4263
Sedative /Hypnotics/Anxiolytics drug (Barbiturates)
Introduction
According to what I studied about (Barbiturates). I will write a journal
about it. Barbiturate is one of the most famous drug , using for several reasons as,
sedative, anxiolytics to relief the feeling of Distress or uneasiness of mind caused
by fear of danger or misfortune, and as hypnotics for people who suffering from
insomnia . these disorders are belong to psychological situations or to defect in
body functions. I will also remind it is mechanism of action, types , (SAR) Structure
–activity relationship. To get simple,interesting, and benefit information about this
drug.
Body
Barbiturates are drugs that act on central nervous system as depressant
and it's one of the older drug choice. And can cause relaxation and sleeping in
relatively low doses .
Barbiturate bind to specific sites on gamma-aminobutyric acid (GABA) heteromultimeric structure contain α,β,δ,ε,γ,π polypeptide subtypes. And they
work on (β) .it's sensitive ion channels found in the central nervous system
(CNS),where they allow an influx of chloride into cell membranes and subsequently
hyper polarize the post synaptic neuron .
Their types :1-long duration barbiturate
barbital (5,5diethylbarbituric acid), phenobarbital (5-ethyl-5-phenyl barbituric
acid).
e.g (Phenobarbital)
2-Intermediate duration of action
Amobarbital(5-ethyl 5-isopentile barbituric acid), butabarbital(5-secbutyl 5
ethylbarbituric acid).
e.g (Amobarbital)
3- Short duration barbiturates
pentobarbital(5-ethyl 5-secpentyl barbituric acid), secobarbital (5-allyl5-secpentyl •
barbituric acid)
e.g Pentobarbital
(SAR) Structure activity relationship :In order to possess good hypnotic activity, a barbiturate must
be a weak acid and must have a lipid /water partition coefficient between certain
limit.
In position number (5) , R1 and R2 may be : alkayl group ,arayl group, or Benzen
ring.
In position number (1) ,(H)N may it be R3 as H,CH3 and the last is more
lipophilicity.
In position number (3), NH give the acidity .
After reading about Barbiturate, I knew different types of it ,their mechanism of
action ,and the structure activity relationship,I had a correlation between the
information that I study it in pharmacology and now in medicinal chemistry, and I
though it's big benefit for me to remember the information and make it stuck in
my mind.
Conclusion
At the end of my writing about barbiturates, I realized that the comparing
between different types of barbiturates it's depend on their Potency ,not on their
efficacy .because they all give the same effects but in different durations and
potency.
And they work as depressant agent on central nervous system on GABA receptor ,
for several reasons as, sedative ,anxiolytics ,and hypnotics . and you must know
that ,It's an important kind of the drugs that people may can't live with out it . just
by taking the cautions and follow the instruction.