script for

Hi, everyone,

I am going to present the first drug that hit 1 billion Doller. Diazepam, also is known by the brand name valium.

 

Diazepam is the number 1 prescription drug in 1975 and the sales peaked with more 2.3 million of pills sold that year in US.

Diazepam

 

 

Between 1968 and 1982, Diazepam had been prescribed to 59.3 million patients

  • Diazepam became a blockbuster drug in the United States
  • Diazepam was known as ” A MATHER LITTLE HELPERS” because of its alleged ability to help reduce motherhood pressures and other women’s problems.
  • In 1970, the drug enforcement agency (DEA) classified Diazepam as a controlled drug that make it illegal to access or even use the drug in the absence of a valid prescription.

In In 1985, Diazepam patent was expired which facilitied to other pharmaceutical companies to manufacture the drug on generic basis

 

Since then the diazepam prescriptions were down according to IMS Health,

The graph illustrates the number of diazepam’s prescription from 2007 to 2017

 

In 2017, there were more than five million prescriptions.

 

How diazepam works

Diazepam promotes the profound action of gamma-aminobutyric acid (GABA), which  produce calming effects that help reduce anxiety, relax the muscles, or stop seizures.

 

(GABA) is defined as an inhibitory neurotransmitter in the brain that blocks abnormal signals and decreases its activity in the nervous system.

 

Diazepam is bind to the Y subunite on GABA A receptor which result in opening GABA A receptor that leading to chlorides ion to inflex into neuron.

 

Diazepam increases the frequence of opening the GABA A receptor which can increase conductance of chloride ions. Consequensly, it leads to a hyperpolarization of the neuronal membrane and reduced excitability of the neuron.

 

Rout of administration

Diazepam is available in multiple formulations, including oral tablets, intramuscular injections (IM), intravenous injection (IV), or rectal gel

.

PK

  • Diazepam is acknowledged as a bio-available. Bioavailability ranges from 93 to 100% orally, and 90% rectally with high levels of plasma protein binding (96–99%).

 

Diazepam is highly lipid soluble and it is bound to plasma proteins at a high level of 98%, which allow its distribution through tissue and across the blood-brain barriers.

 

Metabolism

 

Diazepam is metabolized  in liver to either nordiazepam by CYP 2C19 or temazepam by CYP3A4. Nordiazepam and temazepam are hydroxylated and demethylated to oxazepam. Oxazepam is then glucuronidated and excreted in the urine.

 

 

Toxicity:

 

in cases of severe overdose, symptoms manifest as cardio-respiratory depression, and coma.

Also, the combination of diazepam with alcohol and opioids can lead to fatal events.

 

Conclusion

 

  • For more than 50 years, Diazepam has been witnessed a significant growth due to its applications in treating nervous system illnesses.
  • The effectiveness of the drug is experienced through its long duration actions, not to mention its fast-action effect.
  • Today, diazepam is still on market and its sales expected to reach 1.57 billion by 2027 according to Fior Markets ‘report.

 

 

 

 

 

 

 

 

 

 

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