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US Approved Rx

3

Possibly Marketed Outside US

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Primary Target

GABA-A receptor; alpha-6/beta-3/gamma-2

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Human herpesvirus 1

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Human herpesvirus 2

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Thymidine kinase

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1982

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Pain

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Herpes zoster infections

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Originator

Janssen Pharmaceutica

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Magat, J.

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ANESTHETICS, GENERAL

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DIRECT ACTING ANTIVIRALS

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ATC Level 4

Nucleosides and nucleotides excl. reverse transcriptase inhibitors

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Other general anesthetics

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Showing 1 - 4 of 4 results

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ETOMIDATE

Z22628B598

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Status:

US Approved Rx (2016)

First approved in 1982

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

GABA-A receptor; alpha-6/beta-3/gamma-2

GABA-A receptor; alpha-6/beta-3/gamma-2

Conditions:

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.

BRIVUDINE

2M3055079H

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Status:

Possibly Marketed Outside US

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Thymidine kinase

Human herpesvirus 1

Human herpesvirus 2

Conditions:

Herpes zoster infections

Brivudine (trade names Zostex, Mevir, Brivir, among others) is an antiviral drug used in the treatment of herpes zoster ("shingles"). Brivudine is an analog of the nucleoside thymidine. The active compound is brivudine 5'-triphosphate, which is forme...

d in subsequent phosphorylations by viral (but not human) thymidine kinase and presumably by the nucleoside-diphosphate kinase. Brivudine 5'-triphosphate works because it is incorporated into the viral DNA, but then blocks the action of DNA polymerases, thus inhibiting viral replication. Brivudine is used for the treatment of herpes zoster in adult patients. It is taken orally once daily, in contrast to aciclovir, valaciclovir, and other antivirals. A study has found that it is more effective than aciclovir, but this has been disputed because of a possible conflict of interest on part of the study authors. The drug is contraindicated in patients undergoing immunosuppression (for example because of an organ transplant) or cancer therapy, especially with fluorouracil (5-FU) and chemically related (pro)drugs such as capecitabine and tegafur, as well as the antimycotic drug flucytosine, which is also related to 5-FU. It has not been proven to be safe for children and pregnant or breastfeeding women. The drug is generally well tolerated. The only common side effect is nausea (in 2% of patients). Less common side effects (<1%) include a headache, increased or lowered blood cell counts (granulocytopenia, anemia, lymphocytosis, monocytosis), increased liver enzymes, and allergic reactions. Brivudine is approved for use in a number of European countries including Austria, Belgium, Germany, Greece, Italy, Portugal, Spain, and Switzerland.

ETOMIDATE HYDROCHLORIDE

ZUM3W5027S

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Status:

US Approved Rx (2016)

First approved in 1982

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

GABA-A receptor; alpha-6/beta-3/gamma-2

GABA-A receptor; alpha-6/beta-3/gamma-2

Conditions:

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 SULFATE

Y26131IQZI

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Status:

US Approved Rx (2016)

First approved in 1982

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

GABA-A receptor; alpha-6/beta-3/gamma-2

GABA-A receptor; alpha-6/beta-3/gamma-2

Conditions:

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.

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