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1
Binds with GABA
receptors
Leaded to hyperpolarization of the cell by
opening Chloride Channels
Binding of GABA is enhanced
Muscle Relaxant
(α2-GABAA)
Anticonvulsant
(α1-GABAA)
Sedative/Hypnotic
(α1-GABAA)
Reduction of anxiety
(α1-GABAA)
Anterograde amnesia
(α1-GABAA)
Muscle
Spasm
Cerebral palsy
Multi Sclerosis
Diazepam
Seizure Disorders
Clonazepam
Lorazepam
Diazepam
Anxiety Disorders
Clonazepam
Lorazepam
Diazepam
Alcoholic
withdrawal
syndrome Clonazepam
Lorazepam
Diazepam
Chlordiazepoxide m
Sleep Disorders
Trizolam
Temazepam
Flurazepam
Amnesia
(Pre-anesthetic
medication)
Midazolam
Absorption
&
distribution
Duration of
action
Fate
Rapidly &
completely
(they are
lipophilic)
Divided into 3
groups
1 (long time)
2(intermediate)
3 (Short Time)
Metabolized
In hepatic
microsomal
System
Drowsiness Amnesia Confusion
Early morning insomnia
Day time anxiety
Trizolam
Patients with liver disease
Acute angle closer glaucoma
Alcohol
Sedative Drugs
Sedative effects
Is a GABA receptor antagonist which rapidly revers the effects of benzodiazepine
available for IV administration only it’s unset is rapid but its half-life is short about 1hr?
Convulsion Diazepam
Addiction = yes
2
NOTE: they have been largely replaced by the benzodiazepines, because 1) induce tolerance, 2) physical dependence,
3) very severe withdrawal symptoms, 4) increases drug metabolizing enzymes in liver
Enhances the action of GABA
Decreases the action of Glutamate
Respiratory Depression
CNS Depression
At High Dose
Hypnosis
Anastasia
Coma
Death
At low Dose
Anxiolytic
Hypnotic
Sedative
At low Dose
Suppressthehypoxicand
chemoreceptorresponsetoCO2
At High Dose
Respiratory depression
DeathLiver Enzyme Induction
Anxiety Disorders Phenobarbital
Amnesia
(induction, maintaining
& Recovery)
Thiopenthal
Convulsion
Fibril convulsion
Tonic-Clonic con-- Phenobarbital
Status Epilepticus
Absorption
&
distribution
Duration of
action
Fate
Rapidly &
completely
(they are
lipophilic)
Divided into 3
groups
1 (long time)
2(intermediate)
3 (Short Time)
Metabolized
In hepatic
microsomal
System
Patients with liver disease
Acute intermediate Porphyria
Drugs which are metabolized in liver
Due to Induction of Cytochrome-P450
CNS
Drowsiness
Impaired concentration
Felling fatigue
Nausea
Drug Hang
over
Mental and Physical sluggishness
Dizziness
After
Sleep
Tremors, anxiety, weakness,
Restlessness, nausea and vomiting,
seizures, delirium, and cardiac arrest.
Addiction = yes
3
Liver disease
Pregnancy
Neurological Disease
Renal Disease
Epilepsy
Respiratory disease
Acute Respiratory filliure
Porphyria
Erythromyc
Rifampin
Serotonin Receptor antagonist
Neither muscle relaxant nor
anticonvulsant
headache
Dizziness
Light-headedness
Nausea
Nervousness
Zoleplon
Eszo-piclon
Zolpidin 30min
30min
30minRamelton
20min
5hr
3hr
7hr
7hr

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Axiomatic and hypnotic drugs

  • 1. 1 Binds with GABA receptors Leaded to hyperpolarization of the cell by opening Chloride Channels Binding of GABA is enhanced Muscle Relaxant (α2-GABAA) Anticonvulsant (α1-GABAA) Sedative/Hypnotic (α1-GABAA) Reduction of anxiety (α1-GABAA) Anterograde amnesia (α1-GABAA) Muscle Spasm Cerebral palsy Multi Sclerosis Diazepam Seizure Disorders Clonazepam Lorazepam Diazepam Anxiety Disorders Clonazepam Lorazepam Diazepam Alcoholic withdrawal syndrome Clonazepam Lorazepam Diazepam Chlordiazepoxide m Sleep Disorders Trizolam Temazepam Flurazepam Amnesia (Pre-anesthetic medication) Midazolam Absorption & distribution Duration of action Fate Rapidly & completely (they are lipophilic) Divided into 3 groups 1 (long time) 2(intermediate) 3 (Short Time) Metabolized In hepatic microsomal System Drowsiness Amnesia Confusion Early morning insomnia Day time anxiety Trizolam Patients with liver disease Acute angle closer glaucoma Alcohol Sedative Drugs Sedative effects Is a GABA receptor antagonist which rapidly revers the effects of benzodiazepine available for IV administration only it’s unset is rapid but its half-life is short about 1hr? Convulsion Diazepam Addiction = yes
  • 2. 2 NOTE: they have been largely replaced by the benzodiazepines, because 1) induce tolerance, 2) physical dependence, 3) very severe withdrawal symptoms, 4) increases drug metabolizing enzymes in liver Enhances the action of GABA Decreases the action of Glutamate Respiratory Depression CNS Depression At High Dose Hypnosis Anastasia Coma Death At low Dose Anxiolytic Hypnotic Sedative At low Dose Suppressthehypoxicand chemoreceptorresponsetoCO2 At High Dose Respiratory depression DeathLiver Enzyme Induction Anxiety Disorders Phenobarbital Amnesia (induction, maintaining & Recovery) Thiopenthal Convulsion Fibril convulsion Tonic-Clonic con-- Phenobarbital Status Epilepticus Absorption & distribution Duration of action Fate Rapidly & completely (they are lipophilic) Divided into 3 groups 1 (long time) 2(intermediate) 3 (Short Time) Metabolized In hepatic microsomal System Patients with liver disease Acute intermediate Porphyria Drugs which are metabolized in liver Due to Induction of Cytochrome-P450 CNS Drowsiness Impaired concentration Felling fatigue Nausea Drug Hang over Mental and Physical sluggishness Dizziness After Sleep Tremors, anxiety, weakness, Restlessness, nausea and vomiting, seizures, delirium, and cardiac arrest. Addiction = yes
  • 3. 3 Liver disease Pregnancy Neurological Disease Renal Disease Epilepsy Respiratory disease Acute Respiratory filliure Porphyria Erythromyc Rifampin Serotonin Receptor antagonist Neither muscle relaxant nor anticonvulsant headache Dizziness Light-headedness Nausea Nervousness Zoleplon Eszo-piclon Zolpidin 30min 30min 30minRamelton 20min 5hr 3hr 7hr 7hr