Sevoflurane resources


DRUG INFO
Sevoflurane

Drug Name: Sevoflurane

Indication: Used for induction and maintenance of general anesthesia in adult and pediatric patients for inpatient and outpatient surgery



Pharmacology: Sevoflurane is a general inhalation anesthetic used for induction and maintenance of general anesthesia. It induces muscle relaxation and reduces pains sensitivity by altering tissue excitability. It does so by decreasing the extent of gap junction mediated cell-cell coupling and altering the activity of the channels that underlie the action potential.

Mechanism Of Action: Sevoflurane induces a reduction in junctional conductance by decreasing gap junction channel opening times and increasing gap junction channel closing times. Sevoflurane also activates calcium dependent ATPase in the sarcoplasmic reticulum by increasing the fluidity of the lipid membrane. Also appears to bind the D subunit of ATP synthase and NADH dehydogenase. Sevoflurane also binds to the GABA receptor, the large conductance Ca2+ activated potassium channel, the glutamate receptor and the glycine receptor.

Drug Category: Anesthetics; General Anesthetics; ATC:N01AB08

Brand Names/Synonyms: Bax 3084; CHEMBANK2842; MR6S4; Sevofluran; Sevoflurane; Sevoflurane [Usan:Ban:Inn:Jan]; Sevoflurano [Inn-Spanish]; Sevofluranum [Inn-Latin]; Sevorane; Ultane; [Inn-Latin]

Dosage Forms: LIQUID

Absorption: Rapidly absorbed into the circulation via the lungs

Interactions: DrugBank: Interactions for Sevoflurane

Interactions for Sevoflurane:


In clinical trials, no significant adverse reactions occurred with other drugs commonly used in the perioperative period, including: central nervous system depressants, autonomic drugs, skeletal muscle relaxants, anti-infective agents, hormones and synthetic substitutes, blood derivatives, and cardiovascular drugs.

Intravenous Anesthetics: Sevoflurane administration is compatible with barbiturates, propofol, and other commonly used intravenous anesthetics.

Benzodiazepines and Opioids: Benzodiazepines and opioids would be expected to decrease the MAC of sevoflurane in the same manner as with other inhalational anesthetics. Sevoflurane administration is compatible with benzodiazepines and opioids as commonly used in surgical practice.

Nitrous Oxide: As with other halogenated volatile anesthetics, the anesthetic requirement for sevoflurane is decreased when administered in combination with nitrous oxide. Using 50% N2O, the MAC equivalent dose requirement is reduced approximately 50% in adults, and approximately 25% in pediatric patients.

Neuromuscular Blocking Agents: As is the case with other volatile anesthetics, sevoflurane increases both the intensity and duration of neuromuscular blockade induced by nondepolarizing muscle relaxants. When used to supplement alfentanil-N2O anesthesia, sevoflurane and isoflurane equally potentiate neuromuscular block induced with pancuronium, vecuronium or atracurium. Therefore, during sevoflurane anesthesia, the dosage adjustments for these muscle relaxants are similar to those required with isoflurane.

Potentiation of neuromuscular blocking agents requires equilibration of muscle with delivered partial pressure of sevoflurane. Reduced doses of neuromuscular blocking agents during induction of anesthesia may result in delayed onset of conditions suitable for endotracheal intubation or inadequate muscle relaxation.

Among available nondepolarizing agents, only vecuronium, pancuronium and atracurium interactions have been studied during sevoflurane anesthesia. In the absence of specific guidelines:

1. For endotracheal intubation, do not reduce the dose of nondepolarizing muscle relaxants.

2. During maintenance of anesthesia, the required dose of nondepolarizing muscle relaxants is likely to be reduced compared to that during N2O/opioid anesthesia. Administration of supplemental doses of muscle relaxants should be guided by the response to nerve stimulation.

The effect of sevoflurane on the duration of depolarizing neuromuscular blockade induced by succinylcholine has not been studied.

Hepatic Function

Results of evaluations of laboratory parameters (e.g., ALT, AST, alkaline phosphatase, and total bilirubin, etc.), as well as investigator-reported incidence of adverse events relating to liver function, demonstrate that sevoflurane can be administered to patients with normal or mild-to-moderately impaired hepatic function. However, patients with severe hepatic dysfunction were not investigated.

Occasional cases of transient changes in postoperative hepatic function tests were reported with both sevoflurane and reference agents. Sevoflurane was found to be comparable to isoflurane with regard to these changes in hepatic function.

Very rare cases of mild, moderate and severe post-operative hepatic dysfunction or hepatitis with or without jaundice have been reported from postmarketing experiences. Clinical judgement should be exercised when sevoflurane is used in patients with underlying hepatic conditions or under treatment with drugs known to cause hepatic dysfunction.





Chemical IUPAC Name: 1,1,1,3,3,3-hexafluoro-2-(fluoromethoxy)propane

Chemical Formula: C4H3F7O

Half Life: 15-23 hours

Drug Type: Approved Drug

# Accession No: APRD00219

CAS Registry Number: 28523-86-6



Sevoflurane News
(When available)


Baxter moves ahead with drug despite fight  Jan 2, 2006
Chicago Sun-Times, In September, a US District Court judge ruled Baxter's sevoflurane doesn't infringe a patent on Abbott's inhaled anesthetic agent, Ultane. ...

Fitch Affirms Abbott Laboratories 'AA-'; Outlook Stable  Dec 22, 2005
Business Wire (press release), Potential patent exclusivity losses in the intermediate term include an extended-release formulation of Biaxin, Ultane/sevoflurane, and Depakote. ...


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