Lorazepam: Pharmacokinetics & Pharmacology

Instructor: Justine Fritzel

Justine has been a Registered Nurse for 10 years and has a Bachelor's of Science in Nursing degree.

Lorazepam is a medication that is used for different symptoms. In this lesson, we will learn how lorazepam works within your body to give you the desired results.

What Is Lorazepam?

Lorazepam is a prescription medication classified as a benzodiazepine. Ativan is the brand name for this medication. Lorazepam is used to relieve anxiety and to help a person sleep. It can be used as a sedative prior to medical procedures and is also effective for nausea from chemotherapy. It is also used for seizures.


Lorazepam is a prescription medication.
lorazepam


It is available in different forms for administration. Pills are available for oral use and a solution is available for intravenous (IV) or intramuscular (IM) use. To help us understand how lorazepam works, let's shrink ourselves and grab onto a lorazepam tablet to see what happens within the body.

The Adventures of Lorazepam

Bonnie has an anxiety disorder and she takes lorazepam when she starts feeling anxiety creep in. Picture yourself on the raft called lorazepam as Bonnie washes it down with a drink of water.

The tablet is swallowed and travels down into her stomach. Here, there is an ocean of contents where the raft floats around. As the tablet starts dissolving, your raft disintegrates and you grab onto debris to keep you afloat.

You travel along with your debris as it is absorbed in the GI tract and here it binds onto another raft called the plasma protein in the bloodstream. You travel along the red river until your debris finds the receptor that it was created for! The benzodiazepine receptor. This receptor inhibits the central nervous system and soon Bonnie is feeling less anxious and relaxed.

When lorazepam is administered, it is rapidly absorbed in the body. If a tablet is taken orally, it is absorbed in the gastrointestinal (GI) tract. It then binds to plasma proteins and is distributed to the tissues of the body. Lorazepam then binds to benzodiazepine receptors and enhances the effects of GABA. GABA inhibits the the central nervous system. Relaxation and sedation will reach their peak effect two hours after taking the pill.

Some medications have to be converted to an active metabolite within the body to work. Lorazepam does not have to be. When taken orally, its bioavailability is very high at 90%. Bioavailability refers to the amount of a medication that enters the bloodstream which is available for use.

Lorazepam administered IV or IM is absorbed more rapidly with a faster onset of action. IV lorazepam will have effects felt within 1-5 minutes and IM within 15-30 minutes.

Lorazepam is metabolized in the liver. Here it is converted to the inactive metabolite 3-0-phenolic glucuronide. This inactive metabolite is then eliminated from the body through the kidneys in urine.

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