Active ingredient: Isoflurane - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

• Anesthetics
• General Anesthetics

Dosage Forms

• Liquid

Brands / Synonyms

Aerrane; Ethane; Forane; Forene; Isoflurane [Usan:Ban:Inn:Jan]; Isofluranum [Inn-Latin] ; Terrell

Indications

For induction and maintenance of general anesthesia.

Pharmacology

Isoflurane 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

Isoflurane induces a reduction in junctional conductance by decreasing gap junction channel opening times and increasing gap junction channel closing times. Isoflurane 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. Isoflurane also binds to the GABA receptor, the large conductance Ca²⁺ activated potassium channel, the glutamate receptor and the glycine receptor.

Absorption

Not Available

Toxicity

LC50=15300 ppm/3 hrs (inhalation by rat)

Biotrnasformation / Drug Metabolism

Minimal

Contraindications

Known sensitivity to Isoflurane, USP or to other halogenated agents.

Known or suspected genetic susceptibility to malignant hyperthermia.

Drug Interactions

Isoflurane potentiates the muscle relaxant effect of all muscle relaxants, most notably nondepolarizing muscle relaxants, and MAC (minimum alveolar concentration) is reduced by concomitant administration of N2O. See CLINICAL PHARMACOLOGY.