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Brand Name :
Diastat, Diastat AcuDial, Valium
Synonyms :
diazepam
Class :
Anxiolytics; Benzodiazepines
Brand Name :
Diastat, Diastat AcuDial, Valium
Synonyms :
diazepam
Class :
Anxiolytics; Benzodiazepines
Dosage forms & Strengths
Oral solution:
1 mg/ml
5 mg/ml
Schedule IV tablet:
2 mg
5 mg
10 mg
Injectable solution:
5 mg/ml
Rectal gel:
2.5 mg
10 mg
20 mg
2 - 10
mg
Tablet
Orally
every 6 hrs
Alcohol Withdrawal Syndrome (AWS)
10
mg
Tablet
Orally
every 8 hrs
2 - 10
mg
Tablet
Orally
every 8 hrs
2 - 10
mg
Tablet
Orally
every 8 hrs
5 - 10
mg
Solution
Intramuscular (IM)
Every 10 minutes
2 - 10
mg
Orally
every 6 hrs
Alcohol Withdrawal Syndrome (AWS)
Orally
every 8 hrs
2 - 10
mg
Orally
every 6 hrs
Dosage forms and strengths
Muscle spasm
0.12-0.8 mg/kg/day orally every 6-8 hours
Status epilepticus
0.2 mg/kg every 4-12 hours
Anxiety
2-2.5 mg orally each day or every 12 hours
2 - 2.5
mg
Tablet
Orally
every 12 hrs
12
hrs
2 - 2.5
mg
Orally
every 12 hrs
The interaction may increase the risk of sedation, respiratory depression, and coma
The interaction may increase the risk of sedation, respiratory depression, and coma
The interaction may increase the risk of sedation, respiratory depression, and coma
lemborexant may enhance the CNS depressant effect of CNS depressants
may increase the CNS depressant effect of CNS Depressants
may have an increased CNS depressant effect when combined with buprenorphine
may have an increased CNS depressant effect when combined with CNS depressants
may have an increased CNS depressive effect when combined with CNS depressants
may have an increased CNS depressive effect when combined with CNS depressants
may have an increased CNS depressive effect when combined with methotrimeprazine
may have an increased CNS depressive effect when combined with oxycodone
may have an increased CNS depressant effect when combined with flunitrazepam
may have an increased CNS depressant effect when combined with CNS depressants
calcium, magnesium, potassium and sodium oxybate
may have an increased CNS depressant effect when combined with oxybate salt products
suvorexant: they may increase the CNS depressant effect of CNS Depressants
Ropeginterferon Alfa-2b: they may increase the adverse effect of CNS Depressants
nitrazepam: they may increase the CNS depressant effect of CNS Depressants
tiotropium: they may increase the CNS depressant effect of CNS Depressants
oxychlorosene: they may increase the CNS depressant effect of CNS Depressants
It may enhance the effect when combined with pharmacodynamic synergism
CYP3A strong enhancers of the small intestine may reduce the bioavailability of diazepam
may increase the CNS depressant effect
may increase the CNS depressant effect
CNS depressants increase the effect of CNS depression of thalidomide
CNS depressants increase the efficacy of cannabinoid products
CNS depressants increase the efficacy of cannabinoid products
may increase the CNS depressant effect of bromperidol
may have an increased CNS depressive effect when combined with flunarizine
it increases the effect of CNS depressants
may have an increased CNS depressant effect when combined with orphenadrine
may have an increased CNS depressant effect when combined with CNS depressants
may have an increased CNS depressant effect when combined with paraldehyde
may increase the CNS depressant effect of flibanserin
eluxadoline: they may increase the CNS depressant effect of CNS Depressants
ipratropium: they may increase the CNS depressant effect of CNS Depressants
glycopyrrolate: they may increase the CNS depressant effect of CNS Depressants
chlorthalidone: they may increase the CNS depressant effect of CNS Depressants
chloral hydrate: they may increase the CNS depressant effect of CNS Depressants
may enhance the adverse/toxic effect of antipsychotic agents
may enhance the adverse/toxic effect of antipsychotic agents
may enhance the adverse/toxic effect of antipsychotic agents
may enhance the adverse/toxic effect of antipsychotic agents
may enhance the adverse/toxic effect of antipsychotic agents
may enhance the risk of adverse/toxic effect of antipsychotic agents
may enhance the risk of adverse/toxic effect of antipsychotic agents
may enhance the risk of adverse/toxic effect of antipsychotic agents
may enhance the risk of adverse/toxic effect of antipsychotic agents
may enhance the risk of adverse/toxic effect of antipsychotic agents
may enhance the risk of adverse/toxic effect of antipsychotic agents
may enhance the risk of adverse/toxic effect of antipsychotic agents
may enhance the risk of adverse/toxic effect of antipsychotic agents
may enhance the risk of adverse/toxic effect of antipsychotic agents
may enhance the risk of adverse/toxic effect of antipsychotic agents
may enhance the risk of adverse/toxic effect of antipsychotic agents
may enhance the risk of adverse/toxic effect of antipsychotic agents
may enhance the risk of adverse/toxic effect of antipsychotic agents
may enhance the risk of adverse/toxic effect of antipsychotic agents
may enhance the risk of adverse/toxic effect of antipsychotic agents
may enhance the risk of adverse/toxic effect of other CNS depressants
may enhance the risk of adverse/toxic effect of other CNS depressants
may enhance the risk of adverse/toxic effect of other CNS depressants
may enhance the risk of adverse/toxic effect of other CNS depressants
may enhance the risk of adverse/toxic effect of other CNS depressants
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may enhance the adverse/toxic effect of antipsychotic agents
may enhance the adverse/toxic effect of antipsychotic agents
may enhance the adverse/toxic effect of antipsychotic agents
may enhance the adverse/toxic effect of antipsychotic agents
may enhance the adverse/toxic effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may have an increased CNS depressive effect when combined with cannabinoid-containing products
may have an increased CNS depressive effect when combined with cannabinoid-containing products
may increase the risk of adverse effect
may increase the risk of adverse effect
may increase the risk of adverse effect
may increase the risk of adverse effect
may increase the risk of adverse effect
may increase the CNS depressant effect
may increase the CNS depressant effect
may increase the CNS depressant effect
may increase the CNS depressant effect
may increase the CNS depressant effect
may increase the CNS depressant effect
diazepam: they may diminish the serum concentration of CYP3A4 Inducers
diazepam: they may diminish the serum concentration of CYP3A4 Inducers
diazepam: they may diminish the serum concentration of CYP3A4 Inducers
diazepam: they may diminish the serum concentration of CYP3A4 Inducers
diazepam: they may diminish the serum concentration of CYP3A4 Inducers
It may enhance the effect when combined with miconazole vaginal by affecting CYP3A4 metabolism
It may enhance sedation when combined with oxycodone
Combining diazepam with pranlukast may cause a reduction in the diazepam’s metabolism
The potential for increased CNS depression risk or seriousness occurs when diazepam is used together with pinazepam
The potential for increased CNS depression risk or seriousness occurs when diazepam is used together with pipecuronium
When diazepam is used together with bromisoval, the risk or seriousness of CNS depression is enhanced
diazepam has the potential to reduce the rate of excretion of idebenone, leading to an elevation in levels of serum
When diazepam is used together with medazepam, the risk or seriousness of CNS depression is enhanced
The potential for CNS depression may enhanced when diazepam is used together with fencamfamin
Combining tegafur with diazepam can reduce tegafur’s metabolism
When diazepam is used together with niaprazine, the risk or seriousness of CNS depression is enhanced
When diazepam is used together with levosulpiride, the risk or seriousness of CNS depression is enhanced
may have an increased CNS depressant effect when combined with alcohol
When alprazolam and diazepam is used together, this leads to reduction in the alprazolam’s metabolism
When dexrabeprazole and diazepam is used together, this leads to reduction in the dexrabeprazole’s metabolism
When diazepam is used together with chlordiazepoxide, this leads to enhanced risk or seriousness of CNS depression
When diazepam is used together with norelgestromin, this leads to a rise in norelgestromin’s metabolism
When diazepam is used together with melitracen, this leads to enhanced risk or seriousness of CNS depression
When emylcamate is used together with diazepam, this leads to enhanced risk or seriousness of CNS depression
When acepromazine is used together with diazepam, this leads to enhanced risk or seriousness of CNS depression
may have an increasingly adverse effect when combined with sodium phosphates
may have an increasingly adverse effect when combined with sodium phosphates
may have an increasingly adverse effect when combined with sodium phosphates
may have an increasingly adverse effect when combined with sodium phosphates
may have an increasingly adverse effect when combined with sodium phosphates
nafcillin will decrease the effect of action of diazepam by affecting enzyme CYP3A4 metabolism.
Decreased therapeutic efficacy of diazepam.
the effect of diazepam is decreased by lorlatinib, by altering intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect of CNS depressants
it increases the effect of CNS depressants
it increases the effect of CNS depressants
CNS depressants increase the effect of sedation of ropinirole
may increase the CNS depressant effect
may enhance the risk of adverse/toxic effect of other CNS depressants
may enhance the risk of adverse/toxic effect of other CNS depressants
may enhance the risk of adverse/toxic effect of other CNS depressants
may enhance the risk of adverse/toxic effect of other CNS depressants
may enhance the risk of adverse/toxic effect of other CNS depressants
may have an increased CNS depressive effect when combined with brexanolone
may have an increased CNS depressive effect when combined with CNS depressants
may have an increased CNS depressive effect when combined with CNS depressants
may have an increased CNS depressive effect when combined with CNS depressants
it increases the effect of CNS depressants
it increases the effect of CNS depressants
may have an increased CNS depressant effect when combined with CNS depressants
may have an increased CNS depressant effect when combined with Cyproheptadine
may increase the toxic effect of CNS depressants
may have an increased hepatotoxic effect when combined with diazepam
may increase the toxic effect of antipsychotics
may increase the adverse effect of CNS Depressants
doxylamine: they may increase the CNS depressant effect of CNS Depressants
perampanel: they may increase the CNS depressant effect of CNS Depressants
valerian: they may increase the CNS depressant effect of CNS Depressants
it increases the effect of CNS depressants
may increase the serotonergic effects
may increase the serotonergic effects
may increase the serotonergic effects
may increase the serotonergic effects
may increase the serotonergic effects
may increase the serotonergic effects
acetaminophen/doxylamine/dextromethorphan
may increase the CNS depressant effect of Doxylamine
metoclopramide increases the effect of CNS depressants
may increase the toxic effect of Seizure Threshold, Lowering Potential agents
may enhance the serum concentration of CYP3A4 Inhibitors
pramipexole: they may increase the sedative effect of CNS Depressants
mianserin: they may increase the CNS depressant effect of CNS Depressants
seizure lowering agents increase the toxic or adverse effects of iomeprol
trimeprazine: they may increase the CNS depressant effect of CNS Depressants
piribedil: it may increase the CNS depressant effect of CNS Depressants
ceritinib: they may increase the CNS depressant effect of CNS Depressants
halofantrine: they may increase the CNS depressant effect of CNS Depressants
lomitapide: they may increase the CNS depressant effect of CNS Depressants
methadone: they may increase the CNS depressant effect of CNS Depressants
pilsiicainide hydrochloride: they may increase the CNS depressant effect of CNS Depressants
mirabegron: they may increase the CNS depressant effect of CNS Depressants
dapoxetine: they may increase the CNS depressant effect of CNS Depressants
sacubitril: they may increase the CNS depressant effect of CNS Depressants
pholcodine: they may increase the CNS depressant effect of CNS Depressants
adenosine: it may increase the risk or severity of CNS depression
ajmaline: it may increase the risk or severity of CNS depression
alprazolam: it may increase the risk or severity of CNS depression
benazepril: it may increase the risk or severity of CNS depression
bufexamac: it may increase the risk or severity of CNS depression
butabarbital: it may increase the risk or severity of CNS depression
cefaclor: it may increase the risk or severity of CNS depression
carvedilol: it may increase the risk or severity of CNS depression
alosetron: it may increase the risk or severity of CNS depression
ampicillin: it may increase the risk or severity of CNS depression
anagrelide: it may decreased the serum concentration of CNS depressants
antipyrine: it may decreased the serum concentration of CNS depressants
arbutamine: it may decreased the serum concentration of CNS depressants
binimetinib: it may increase the metabolism of CNS depressants
chlorpromazine: it may increase the metabolism of CNS depressants
aclidinium: it may increase the risk of CNS depression
baclofen: it may increase the risk of CNS depression
balsalazide: it may increase the risk of CNS depression
benorilate: it may increase the risk of CNS depression
boceprevir: it may increase the risk of CNS depression
bosentan: it may increase the risk of CNS depression
bretylium: it may increase the risk of CNS depression
brexpiprazole: it may increase the risk of CNS depression
carisoprodol: it may increase the risk of CNS depression
carprofen: it may increase the risk of CNS depression
the sedative property of hyoscine may be increased
diazepam might lead to a reduction in the rate of excretion of telavancin, potentially leading to elevated levels of serum
it increases the effect of CNS depressants
it increases the effect of CNS depressants
it increases the effect of CNS depressants
CNS depressants increase the effect of oxycodone
it increases the toxicity of CNS depressants
CNS depressants increase the effect of zolpidem
CNS depressants increase the effect of opioid agonists
CNS depressants increase the effect of opioid agonists
CNS depressants increase the effect of opioid agonists
CNS depressants increase the effect of opioid agonists
Actions and Spectrum:
Action:
Gamma-aminobutyric acid (GABA) neurotransmitter action at the GABA-A receptor is amplified by diazepam. The brain’s main inhibitory neurotransmitter is GABA. Diazepam enhances the affinity of GABA for its receptor by binding to the benzodiazepine site on the GABA-A receptor. This increases the amount of chloride ions that enter the cell.
Frequency defined
1-10%
Rash
Euphoria
Incoordination
Diarrhea
Somnolence
Frequency not defined
Hypotension
Fatigue
Headache
Incontinence
Dysarthria
Muscle weakness
Respiratory depression
Urinary retention
Depression
Changes in salivation
Incontinence
Blurred vision
Skin rash
Black Box Warning
The drug should be used in caution as it will cause habit-forming potential effects.
Contraindication /Caution:
Diazepam is contraindicated in patients hypersensitive to the formulation’s active ingredient and other excipients.
Myasthenia Gravis
Severe Hepatic Insufficiency
Pregnancy and breastfeeding
Pregnancy/Lactation
Pregnancy consideration:
Pregnancy category: Category D
Breastfeeding warnings:
The drug is secreted in breastmilk, hence not recommended during breastfeeding
Pregnancy category:
Pharmacology:
Diazepam is a benzodiazepine derivative with a wide range of pharmacological effects.
Pharmacodynamics:
Gamma-aminobutyric acid (GABA) neurotransmitter action at the GABA-A receptor is amplified by diazepam. The brain’s main inhibitory neurotransmitter is GABA. Diazepam enhances the affinity of GABA for its receptor by binding to the benzodiazepine site on the GABA-A receptor. This increases the amount of chloride ions that enter the cell.
Pharmacokinetics
Absorption
Peak plasma concentrations of diazepam are reached in 1 to 1.5 hours after oral administration. The drug is efficiently absorbed from the gastrointestinal system.
Distribution
Because of its high lipophilicity, it can penetrate the central nervous system rapidly. It is also extensively dispersed throughout the body and can pass across both the placental and blood-brain barriers.
Metabolism
In the liver, cytochrome P450 enzymes, specifically, CYP3A4 and CYP2C19 metabolize diazepam extensively.
Excretion and Elimination
Diazepam and its metabolites are excreted primarily in the urine.
Diazepam’s elimination half-life varies, however it usually lasts 48 hours. Longer half-lives of its metabolites add to the drug’s sustained effects.
Administration:
The drug can be taken in form of oral tablets and liquid.
The drug is also administered through Intravenous (IV) or Intramuscular (IM) Injection
Patient Information Leaflet
Generic Name: diazepam
Pronounced: dia-zeh-pam
Why do we use diazepam?
It is used to treat anxiety, seizure and muscle spasms and in withdrawal alcohol addicts.
Diazepam is intended for the treatment of anxiety disorders, or as a short-term treatment of anxiety symptoms that are present.
It is prescribed for the treatment of conditions like anxiety, increased muscle activity, and severe alcohol withdrawal states like tremor, agitation and hallucinations.
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