Transcript File
Mechanism of action
It interacts with specific receptors in the CNS,
particularly in the cerebral cortex.
Benzodiazepine-receptor binding enhances the
inhibitory effects of various neurotransmitters. ( GABA
Facilitatory)
Flumazenil (an imidazolebenzodiazepine) is a specific
benzodiazepine-receptor antagonist that reverses most
of the CNS effects of benzodiazepines. (Dose: 0.20.5mg IV to a maximum of 3mg)
DIAZEPAM
MIDAZOLAM
LORAZEPAM
Routes
Oral, IM, IV
IM, IV
Oral, IM, IV
Onset of action
IV: 30-60 sec
Oral: 1-2 hrs
IM: 30 min
IV: 30-60 sec
IM: 30 min
IV: 1-2 min
Oral: 1-2 hrs
IM: 30 min
Preparation (IV)
Oil based so
injection is
painful
Water based so
injection is not
painful
---------------
Elimination Half
Life
30-60 hrs
2-3 hrs
15 hrs
Dose of Sedation
0.05-0.2mg/kg
0.01-0.1mg/kg
0.03-0.04mg/kg
Diazepam
It is a colorless crystalline compound, insoluble in
water and has a molecular weight of 284.74.
Each mL contains 5 mg diazepam compounded with
40% propylene glycol, 10% ethyl alcohol, 5% sodium
benzoate and benzoic acid as buffers, and 1.5% benzyl
alcohol as preservative.
Indications
Diazepam is indicated for the management of anxiety
disorders or for the short-term relief of the symptoms
of anxiety.
In acute alcohol withdrawal.
Diazepam Injection is a useful adjunct in status
epilepticus and severe recurrent convulsive seizures.
Diazepam is a useful premedication (the IM route is
preferred) for relief of anxiety and tension in patients
who are to undergo surgical procedures.
To prevent hallucination caused by Ketmaine.
DOSAGE AND ADMINISTRATION
Dosage should be individualized for maximum beneficial effect.
The usual recommended dose in adults ranges from 2 mg to 20
mg IM or IV, depending on the indication and its severity.
Anxiety Disorders and Symptoms of Anxiety: 2 mg to 5 mg,
IM or IV
Acute Alcohol Withdrawal
The usual dose is 10 mg---- 3 or 4 times during the first 24 hours,
then 5 mg---- 3 or 4 times daily as needed.
Relief of Muscle Spasm
The usual dose is 2mg to 10 mg----- 3 or 4 times daily.
Convulsive Disorders
The usual dose is 2 mg to 10 mg------- 2 to 4 times daily
Systemic Effects
CNS: Mainly acts on RAS and amygdala ( limbic
system) producing sedation, anxiolysis and amnesia.
Also acts on medulla producing muscle relaxation and
on cerebellum producing ataxia.
No any analgesic effects.
Produce Muscle relaxation by acting on medullary and
spinal cord (central action) and not at neuromuscular
junction.
Reduces cerebral metabolic rate, brain oxygen
consumption and Intracranial pressure.
Respiratory system:
At higher dose cause respiratory depression and may
lead to death.
It is maximum seen with midazolam.
Cardiovascular System
Minimal reduction in blood pressure , heart rate and
cardiac output.
Hypotension is maximum with midazolam.
Metabolism
Metabolized in Liver.
The major active metabolite of diazepam is des-methyl
diazepam.
Metabolites are excreted in Gut and Urine.
Side effects
Fatigue and ataxia; venous thrombosis and phlebitis at
the site of injection
CNS: confusion, depression, dysarthria, headache,
slurred speech, syncope, tremor, vertigo.
GI: constipation, nausea.
GU: incontinence ,libido, urinary retention.
Cardiovascular: bradycardia, cardiovascular collapse,
hypotension.
OTHERS : blurred vision, diplopia,
nystagmus,urticaria, skin rash, jaundice.
Contraindications and Precautions
Valium Injection is contraindicated in patients
with a known hypersensitivity to this drug.
Valium Injection should not be administered to
patients in shock, coma.
Should be used with precautions in patients with
pulmonary and cardiovascular diseases.
Usage in Pregnancy: An increased risk of
congenital malformations associated with the use
of diazepam during the first trimester of
pregnancy has been suggested in several studies.