Hypnotics Flashcards
The major classes of neurotransmitters are
Small molecules gag gaa and histamine, serotonin and noradrenaline
Gaseous molecules
CO and NO
Neuropeptides
Endocannabinoids
The major classes of neurotransmitters are
Small molecules gag gaa and histamine, serotonin and noradrenaline
Gaseous molecules
CO and NO
Neuropeptides
Endocannabinoids
The actions of glutamate and aspartate include
Increased proteinase activity
Increased intracellular NO build up
Increased calcium build up and free radical
The receptors which glutamate binds to include
NMDA
Kainate
AMPA ( a amino 3 hydroxy 5methyl 4isoxazolepropionic acid)
Aspartate and glutamate are found majorly in …..
Cerebrum
Spinal cord
Cerebellum
The major inhibitory neurotransmitters in the brain and spinal cords are ……. and ……. respectively
GABA
Glycine
GABA is formed from ……….
Decarboxylation of glycine
Barbiturates works on ………… receptors
Benzodiapine receptors BDZ
The nomenclature of the benzodiazepine ring is……
A benzene ring fused to a 1,4 diazepine ring
All clinically important benzodiazepine contains……… group
5 aryl substituent ring
Benzodiazepines can be administered through ……….. routes
Enteral and paraenteral
All orally administered benzodiazepine are …………… absorbed except
Completely absorbed except clorazepate
Clorazepate is rapidly carboxylated to ………….. in the gastric juice
Nordazepam
BZD are highly protein bound T/F
True
Alprazolam is has ………. % of protein binding
70%
Diazepam has ……… % of protein binding
99%
BDZ are metabolised in the ………..
Liver
The BDZ are metabolised first to their ……….. forms
Active
The active forms of BDZ are cleared rapidly than their parent drugs T/F
False
The back bone of barbiturates are
Barbiturates acid
Trioxohexahydropyrimidine
The back bone of barbiturates are
Barbiturates acid
Trioxohexahydropyrimidine
The two forms of barbiturates are and what makes them different
Oxabarbiturates O2 at position II
Thiobarbiturates O2 is replaced by sulfur
Clinically active barbiturates contains ……….. functional group
5 alkyl or aryl group
Contrast Thiobarbiturates and oxabarbiturates
Thiobarbiturates are more lipophillic due to the substitution
Easily absorbed
Early onset of action
Increase hypnotic potency
But quick degradation which leads to a lesser duration of action.
Barbiturates are usually administered through ………. route
Orally
Barbiturates can be administered through ……….. and ……… routes
Oral and parenteral route
Barbiturates readily cross the placenta and are secreted in breast milk with the exceptions of ….
Aprobarbital
Phenobarbital
All barbiturates are completely metabolised in …………… and excreted in …………..
Liver and excreted in the kidney
What is the peculiarity in the excretion of barbiturates
~Quater of phenobarbital and almost all the aprobarbital are excreted unchanged
Rxn of metabolism of barbiturates in the liver include
C oxidation at C5
N hydroxylation
N dealkylation
N glycosylation
Desulfuration
The three stages of metabolism of benzodiazepene are
Modification or removal of substituent
Alpha hydroxylation
Glucuronidation
The first two stages of bzd metabolism results in active metabolites T/F
True
