Sufentanil, sold under the brand names Sufenta among others, is a
synthetic
Synthetic may refer to:
Science
* Synthetic biology
* Synthetic chemical or compound, produced by the process of chemical synthesis
* Synthetic elements, chemical elements that are not naturally found on Earth and therefore have to be created in ...
opioid
Opioids are a class of Drug, drugs that derive from, or mimic, natural substances found in the Papaver somniferum, opium poppy plant. Opioids work on opioid receptors in the brain and other organs to produce a variety of morphine-like effects, ...
analgesic drug approximately 5 to 10 times as
potent as its
parent drug,
fentanyl
Fentanyl is a highly potent synthetic piperidine opioid primarily used as an analgesic (pain medication). It is 30 to 50 times more Potency (pharmacology), potent than heroin and 50 to 100 times more potent than morphine. Its primary Medici ...
, and 500 to 1,000 times as potent as
morphine
Morphine, formerly also called morphia, is an opiate that is found naturally in opium, a dark brown resin produced by drying the latex of opium poppies (''Papaver somniferum''). It is mainly used as an analgesic (pain medication). There are ...
. Structurally, sufentanil differs from fentanyl through the addition of a methoxymethyl group on the piperidine ring (which increases potency but is believed to reduce duration of action
), and the replacement of the
phenyl ring by
thiophene
Thiophene is a heterocyclic compound with the formula C4H4S. Consisting of a planar five-membered ring, it is aromatic as indicated by its extensive substitution reactions. It is a colorless liquid with a benzene-like odor. In most of its reacti ...
. Sufentanil first was synthesized at
Janssen Pharmaceutica
Johnson & Johnson Innovative Medicine (formerly Janssen Pharmaceuticals) is a Belgian pharmaceutical company headquartered in Beerse, Belgium, and wholly owned by Johnson & Johnson. It was founded in 1953 by Paul Janssen.
In 1961, Janssen Ph ...
in 1974.
Medical uses
Sufentanil offers properties of sedation and can be used as analgesic component of
anesthetic
An anesthetic (American English) or anaesthetic (British English; see spelling differences) is a drug used to induce anesthesia — in other words, to result in a temporary loss of sensation or awareness. They may be divided into t ...
regimen during an operation.
Because of its extremely high potency, it is often used in surgery and post-operative pain management for patients that are heavily opioid dependent/opioid tolerant because of long term opiate use for chronic pain or illicit opiate use. It is also used in surgery and post-operative pain control in people that are taking high dose
buprenorphine for chronic pain because it has the potency and binding affinity strong enough to displace buprenorphine from the opioid receptors in the central nervous system and provide analgesia.
In 2018, the
Food and Drug Administration (FDA) approved Dsuvia, a sublingual tablet form of the drug, that was developed in a collaboration between AcelRx Pharmaceuticals and the
United States Department of Defense
The United States Department of Defense (DoD, USDOD, or DOD) is an United States federal executive departments, executive department of the federal government of the United States, U.S. federal government charged with coordinating and superv ...
for use in battlefield settings where intravenous (IV) treatments may not be readily available. The decision to approve this new potent synthetic opioid came under criticism from politicians and from the chair of the FDA advisory committee, who fear that the tablets will be easily diverted to the illegal drug market. Dsuvia has since been withdrawn from the market due to "unresolvable manufacturing constraints."
Overdose
Management
Because sufentanil is very potent, practitioners must be prepared to reverse the effects of the drug should the patient exhibit symptoms of overdose such as
respiratory depression
Hypoventilation (also known as respiratory depression) occurs when ventilation is inadequate (''hypo'' meaning "below") to perform needed respiratory gas exchange. By definition it causes an increased concentration of carbon dioxide (hypercapni ...
or
respiratory arrest
Respiratory arrest is a serious medical condition caused by apnea or respiratory dysfunction severe enough that it will not sustain the body (such as agonal breathing). Prolonged apnea refers to a patient who has stopped breathing for a long period ...
. As for all other opioid-based medications,
naloxone
Naloxone, sold under the brand name Narcan among others, is an opioid antagonist, a medication used to reverse or reduce the effects of opioids. For example, it is used to restore breathing after an opioid overdose. Effects begin within two ...
(trade name Narcan) is the definitive antidote for overdose. Depending on the amount administered, it can reverse the respiratory depression and, if enough is administered, completely reverse the effects of sufentanil.
Society and culture
Brand names
Sufentanil is marketed under various brand names including Dsuvia, Dzuveo, Sufenta, and Sufentil.
Veterinary use
In cats sufentanil's half-life is longer than that of fentanyl and
alfentanil. In dogs sufentanil produces a better anaesthetic recovery with similar analgesic and respiratory depression than fentanyl. One report suggest that for post-operative pain
bupivacaine
Bupivacaine, marketed under the brand name Marcaine among others, is a medication used to decrease sensation in a specific small area. In nerve blocks, it is injected around a nerve that supplies the area, or into the spinal canal's epidural ...
and sufentanil provides greater analgesia than fentanyl and bupivacaine in dogs. There is little information on sufentanil's use in large animals. Due to the greater risk of cardiovascular and respiratory depression sufentanil is rarely used in practice.
References
{{Authority control
Anilides
Belgian inventions
Ethers
Fentanyl
General anesthetics
Janssen Pharmaceutica
Mu-opioid receptor agonists
Opioids
Piperidines
Propionamides
Thiophenes