Remimazolam and Oliceridine: Sedative and Analgesic Drugs Approved by FDA

injection sedation

Sedation is commonly performed in various medical areas, including dentistry and endoscopy. The specialists administering sedation are highly qualified and typically have a moderate sedation certification that allows them to perform these kinds of procedures. For many years, medications such as midazolam, propofol, ketamine, and dexmedetomidine have been widely used in sedation procedures. However, several recently approved medications, such as remimazolam and oliceridine, have been showing great results as well. This article will focus on these two medications and their use in sedation procedures.


Remimazolam is a drug used for sedation in medical procedures, particularly in endoscopy and surgery cases. It is a benzodiazepine drug that affects the central nervous system to induce sedation and reduce anxiety. It has a short duration of action and a rapid onset, which makes it particularly useful for procedures that require brief sedation, such as endoscopy procedures. Remimazolam was approved by the US Food and Drug Administration (FDA) in 2020.

How Does Remimazolam Work?

Remimazolam is one of the few drugs used for short-term sedation (around 30 minutes). It has a mild effect and can be used for endoscopies and colonoscopies.  This sedation drug acts as a positive allosteric modulator of the gamma-aminobutyric acid (GABA) type A receptor. It exerts its sedative effects by enhancing the inhibitory effects of GABA neurotransmission in the brain. 

To be more precise, GABA causes the opening of the chloride ion channel, leading to an influx of chloride ions into the neuron. It hyperpolarizes the neuron, making it less likely to fire an action potential and reducing neuronal activity — this results in sedation.


Since remimazolam is a generic component, its dosage depends on the exact prescription product it’s in, as well as a specific medical procedure and the patient’s condition. The recommended dosage ranges from 2.5 to 5 mg for intravenous administration, with an option to add 2.5 mg for sedation maintenance.

Side Effects

Remimazolam has minimal side effects and is generally safe. However, it should be used cautiously, even during sedation, especially if a patient has underlying conditions. The most common side effects include hypotension, headache, tachycardia, and injection site pain. Such side effects may not occur in all patients, and some people may experience other side effects like allergic reactions

Approval by FDA 

The FDA approved remimazolam, marketed as “BYFAVO,” after undergoing rigorous clinical trials involving around 1,000 patients. Its mode of action is similar to midazolam, commonly utilized in IV sedation dentistry to reduce anxiety while maintaining respiratory and cardiovascular stability. Compared to midazolam, studies have shown that remimazolam has a more consistent and brief effect, making it ideal for adult procedures that last no longer than 30 minutes, such as colonoscopies.

FDA Sign and Building 21 at Entrance – Photo by: The U.S. Food and Drug Aadministration – Source: Flickr Creative Commons

Oliceridine: Facts and Usage

Oliceridine is another powerful painkiller designed to manage moderate to severe acute pain in patients. It is an opioid agonist that is primarily administered intravenously when other forms of pain relief have proven inadequate.

How Does Oliceridine Work?

Oliceridine binds to the mu-opioid receptors in the brain, effectively blocking the pain sensations. The process causes inhibition of neuronal and neurotransmitter excitability, which leads to analgesia. This allows for prolonging the sedation effect, causing fewer side effects than other similar medications.  


The standard dosage of oliceridine depends on the needed sedation level and the patient’s condition. The lowest effective dose to me administered throughthough an IV is 1.5 mg, with possible dosage additions to maintain and prolong the effect. However, the maximum cumulative dose should not exceed 27 mg per day

Side Effects

Oliciderine, just like other sedation drugs, has its side effects. However, in most cases, they are relatively mild and pass quickly. Common side effects include nausea, dizziness, vomiting, and headaches. Compared to other previously used opioids like ketamine or morphine, these side effects are relatively insignificant. 

However, the drug should not be administered to patients with conditions like severe asthma or respiratory depression. It should also not be given to pregnant women, especially in the first trimester. Drug hypersensitivity can also cause serious side effects, that’s why it should only be introduced by a certified specialist.

Approval by FDA 

Oliceridine has been approved by the FDA in 2020 and is marketed under the brand name “OLINVYK.” It has undergone several clinical trials and changes since it initially raised some concerns. The approval process has taken around seven years since the first drug report was published in 2013. It has an improved safety profile compared to other opioid agonists, such as morphine. 


Both remimazolam and oliceridine have their benefits and side effects, and only a certified medical specialist can determine which drug should be introduced to the patient.

This article and other related articles on the Internet are not medical advice and cannot be used for self-prescription. The right sedation drugs must be selected based on the patient’s condition and treatment history. To make the right prescription, it’s necessary to study the patient’s medical history, possible drug side effects, and new medical protocols to ensure the sedation is safe.