diazepam buccal

Action and Spectrum

Actions and Spectrum 

Diazepam works by enhancing the effect of a neurotransmitter called gamma-aminobutyric acid (GABA) in the brain.  

GABA is an inhibitory neurotransmitter, and increasing its activity can produce a calming effect, helping to alleviate anxiety.

Drug Interaction

Adverse Reaction

Frequency not defined  

None

Black Box Warning

Black Box Warning 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Individuals with a known hypersensitivity or allergy to diazepam should not use diazepam buccal. 
• Diazepam contraindicated in individuals with severe respiratory insufficiency and acute respiratory distress. 

Caution: 

• Caution should take while using diazepam in individuals with impaired respiratory function. 
• Diazepam is advised to use cautiously in individuals with severe hepatic and renal impairment. 

Pregnancy / Lactation

Pregnancy consideration: 

Pregnancy category: N/A 

Lactation: Excretion into human milk is unknown  

Pregnancy Categories:         

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.  

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women. 

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 

Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology  

Diazepam has muscle relaxant properties and is used to treat muscle spasms. It acts on the central nervous system, reducing the activity of certain neurons that cause muscle contractions. 

Pharmacodynamics 

Diazepam enhances the effect of GABA by binding to a specific site on the GABA-A receptor, distinct from the GABA binding site. This binding increases the frequency of chloride channel opening, leading to an increased inhibitory effect.  

Pharmacokinetics 

Absorption   

When diazepam is administered buccally, it is absorbed through the oral mucosa. 

The buccal route provides rapid absorption, leading to a quicker onset of action. 

Distribution 

It can cross the blood-brain barrier, leading to its effects on the CNS. 

Diazepam is extensively bound to plasma proteins.  

Metabolism 

Diazepam undergoes extensive metabolism in the liver through the cytochrome P450 enzyme. 

Elimination and excretion 

Diazepam is excreted occurs primarily through the kidneys.  

Adminstartion

Administration 

The administration of diazepam through the buccal route involves placing the drug in film form between the gum and cheek. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: diazepam buccal 

Why do we use diazepam buccal? 

Diazepam buccal is used in the management of seizure clusters in paediatrics.   

Diazepam is also indicated to manage symptoms of anxiety disorders.