Benzodiazepine+Barbiturates CNS Flashcards
Benzodiazepine Ultra short acting ?
570
CloraZepate
570
Benzodiazepine short acting ?
- TriAzolam
- MidAzolam
- OxaZepam
570
Long acting benzodiazepine ??
- Diazepam
- Flurazepam
- Parazepam
- Quazepam
- Nitrazepam
570
Benzodiazepine intermediate acting ??
- AlprAzolam
- EstAzolam
- Lorazepam
- Temazepam
570
Major inhibutory Neurotransmitters in the CNS ?
GABA
571
GABA receptor which type of channel ??
Cl- ion channel
572
Structure of GABA receptor ??
Pentameric structure
Two binding site for GABA location ??
Between ALPHA – BETA
572
BZ binding site in GABA receptor ??
Between ALPHA–GAMA
572
Barbiturate binding site in GABA receptor >??
Between ALPHA – BETA
Different Site
572
Alpha-1 subunit binding drugs name ??
- Zolpidem
- 2.Zaleplon
3.Eszopiclone
572
Which sedative-hyptonics has low affinity for GABA ??
BZ
Anticonvulsant use of BZ ??
- Epilepsy / Status epilecticus
- Seizure
573
Anesthesia use of BZ»_space;??
Diazepam
Lorazepam
Midazolam
573
How to inc the affintiy ??
Baclofen
572
Effeccts of BZ on diff stages of NREM sleep ?
- Stage-2 NREM duration inc
- Stage-4 NREM duartion dec
NREM- Non Rapid Eye Movement
573
Sedation effects of BZ ??
- dec anxiety
- Euphoria
- Loss of self control
- Impaired judgment
- Anterograde amnesia
573
Drugs that enhance GABAergic action ??
- BZ
- Barbiturates-Phenobarbitone
- Valproate
- Vigabatrin
- GabaPentin
Mechanism of BZ shortly ??
My own way _____———–
- BZ binds with GABA-R
- inc affinity of GABA-R to GABA
- GABA binds with GABA-R
- inc frequency of opening Cl- channel
- inc influc of Cl- ions
- Hyperpolarization
- No Action Potential
- No excitability
- CNS depression / Sedation / Hypnosis
571
Metabolism of BZ ?? Location ??
Liver
Ultra short acting barbiturates /
- thiopental Na
- methohexital
short acting barbiturates ?
- pento + seco
- barbital
intermediate acting barbiturates ?
amo-apro-buto
barbital
long acting Bt ?
phenobarbitone/phenobarbital
M/A of Bt ?
same as BZ
but Inc duration of opening of Cl channel
indications of Bt ?
- GA-thiopental Na
- congenital hyperbilirubinemai - phenobarbitone ‘
- epilepsies
- partial seizure
- eclampsia
- GTCS
- Status epilepticus
- sedation
- hypnosis
- anticonvulsant
how congenital hyperbilirubinemia by Bt ?
- induce hepatic drug metabolizing enzyme
- inc conc of glucoronyl transferase
- inc conjugation of bilirubin
- in metabolism of bilirubin
- dec serum B level ``
Bt + Warferin = ?
inc metabolism of warferin
dec anti-coagulant effect
inc coagulation=thrombosis
Bt + OCP = ?
- inducre epatic microsomal enzyme
- inc metabolism of OCP
- Failure of contraception
A/E of Bt ?
- drowsiness
- hangover effect
- addiction
- tolerance
- enzyme induction’
- allergy
- skin lesion
- asthma
- oligurtia
- dependence
antidote of Bz ?
FLUMAZENIL
A/E of BZ ?
- hangover effect
- somnolence
- drowsiness
- anterograde amnesia
- impraired judegement
- lethaylethargy
- cardiac failure
- respiratory center depression
- memory loss
- rhabdo,yosis
why Bz»_space;> Bt ?
- high TI = need more dose
- have antidote=flumazenil
- donot induce drug metabolizing enzymes