Etomidate (AMIDATE®) is an imidazole derivative anesthetic and hypnotic with little effect on blood gases, ventilation, or the cardiovascular system. It is intended for the induction of general anesthesia by intravenous injection. Etomidate (AMIDATE®) is also indicated for the supplementation of subpotent anesthetic agents, such as nitrous oxide in oxygen, during maintenance of anesthesia for short operative procedures such as dilation and curettage or cervical conization. It also produces a unique toxicity among anesthetic drugs - inhibition of adrenal steroid synthesis that far outlasts its hypnotic action and that may reduce survival of critically ill patients. The major molecular targets mediating anesthetic effects of etomidate (AMIDATE®) in the central nervous system are specific gamma-aminobutyric acid (GABA) type A receptor subtypes. The R(+) isomer of etomidate is 10 times more potent than its S(-) isomer at potentiating GABA-A receptor activity.

Aminoglutethimide, marketing as Cytadren has been used in the treatment of advanced breast and prostate cancer. It was formerly used for its weak anticonvulsant properties. Cytadren is indicated for the suppression of adrenal function in selected patients with Cushing’s syndrome. Morning levels of plasma cortisol in patients with adrenal carcinoma and ectopic ACTH producing tumors were reduced on the average to about one half of the pretreatment levels, and in patients with adrenal hyperplasia to about two thirds of the pretreatment levels, during 1-3 months of therapy with Cytadren. Data available from the few patients with adrenal adenoma suggest similar reductions in plasma cortisol levels. Measurements of plasma cortisol showed reductions to at least 50% of baseline or to normal levels in one third or more of the patients studied, depending on diagnostic groups and time of measurement. Because Cytadren does not affect the underlying disease process, it is used primarily as an interim measure until more definitive therapy such as surgery can be undertaken or in cases where such therapy is not appropriate. Only small numbers of patients have been treated for longer than 3 months. A decreased effect or “escape phenomenon” seems to occur more frequently in patients with pituitary dependent Cushing’s syndrome, probably because of increasing ACTH levels in response to decreasing glucocorticoid levels. Cytadren blocks several other steps in steroid synthesis, including the C-11, C-18, and C-21 hydroxylations and the hydroxylations required for the aromatization of androgens to estrogens, mediated through the binding of Cytadren to cytochrome P-450 complexes. A decrease in adrenal secretion of cortisol is followed by an increased secretion of pituitary adrenocorticotropic hormone (ACTH), which will overcome the blockade of adrenocortical steroid synthesis by Cytadren. The compensatory increase in ACTH secretion can be suppressed by the simultaneous administration of hydrocortisone. Since Cytadren increases the rate of metabolism of dexamethasone but not that of hydrocortisone, the latter is preferred as the adrenal glucocorticoid replacement. Although Cytadren inhibits the synthesis of thyroxine by the thyroid gland, the compensatory increase in thyroid-stimulating hormone (TSH) is frequently of sufficient magnitude to overcome the inhibition of thyroid synthesis due to Cytadren. In spite of an increase in TSH, Cytadren has not been associated with increased prolactin secretion. At low doses, aminogluthethimide is only an effective inhibitor of aromatase (Cytochrome P450 11A1), but at higher doses, it effectively blocks Cytochrome P450 11A1 (P450scc) as well. Citadel was marketed previously as an anticonvulsant but was withdrawn from marketing for that indication in 1966 because of the effects on the adrenal gland.

Metomidate is a non-barbiturate imidazole which produces a sleepy condition of 20-60 minutes duration without substantial analgesia. Since the beginning of 1997 the use of the hypnotic drug metomidate (Hypnodil) in swine is nor longer allowed. This ban caused a substantial therapeutic deficit for anesthesia in swine. 11C-metomidate may be used with positron emission tomography which can differentiate adrenocortical from nonadrenocortical tumors and a suspected adrenocortical cancer may be characterized and staged before surgery. Metomidate hydrochloride is for the sedation and anesthesia of aquarium and non-food fish species. Aquacalm has been granted Indexed status by the FDA for this purpose.

Etomidate (AMIDATE®) is an imidazole derivative anesthetic and hypnotic with little effect on blood gases, ventilation, or the cardiovascular system. It is intended for the induction of general anesthesia by intravenous injection. Etomidate (AMIDATE®) is also indicated for the supplementation of subpotent anesthetic agents, such as nitrous oxide in oxygen, during maintenance of anesthesia for short operative procedures such as dilation and curettage or cervical conization. It also produces a unique toxicity among anesthetic drugs - inhibition of adrenal steroid synthesis that far outlasts its hypnotic action and that may reduce survival of critically ill patients. The major molecular targets mediating anesthetic effects of etomidate (AMIDATE®) in the central nervous system are specific gamma-aminobutyric acid (GABA) type A receptor subtypes. The R(+) isomer of etomidate is 10 times more potent than its S(-) isomer at potentiating GABA-A receptor activity.

Etomidate (AMIDATE®) is an imidazole derivative anesthetic and hypnotic with little effect on blood gases, ventilation, or the cardiovascular system. It is intended for the induction of general anesthesia by intravenous injection. Etomidate (AMIDATE®) is also indicated for the supplementation of subpotent anesthetic agents, such as nitrous oxide in oxygen, during maintenance of anesthesia for short operative procedures such as dilation and curettage or cervical conization. It also produces a unique toxicity among anesthetic drugs - inhibition of adrenal steroid synthesis that far outlasts its hypnotic action and that may reduce survival of critically ill patients. The major molecular targets mediating anesthetic effects of etomidate (AMIDATE®) in the central nervous system are specific gamma-aminobutyric acid (GABA) type A receptor subtypes. The R(+) isomer of etomidate is 10 times more potent than its S(-) isomer at potentiating GABA-A receptor activity.

Metomidate is a non-barbiturate imidazole which produces a sleepy condition of 20-60 minutes duration without substantial analgesia. Since the beginning of 1997 the use of the hypnotic drug metomidate (Hypnodil) in swine is nor longer allowed. This ban caused a substantial therapeutic deficit for anesthesia in swine. 11C-metomidate may be used with positron emission tomography which can differentiate adrenocortical from nonadrenocortical tumors and a suspected adrenocortical cancer may be characterized and staged before surgery. Metomidate hydrochloride is for the sedation and anesthesia of aquarium and non-food fish species. Aquacalm has been granted Indexed status by the FDA for this purpose.