Anesthetics, Intravenous

Ultrashort-acting anesthetics that are used for induction. Loss of consciousness is rapid and induction is pleasant, but there is no muscle relaxation and reflexes frequently are not reduced adequately. Repeated administration results in accumulation and prolongs the recovery time. Since these agents have little if any analgesic activity, they are seldom used alone except in brief minor procedures. (From AMA Drug Evaluations Annual, 1994, p174)
DrugDrug NameDrug Indication
DB00292EtomidateUsed in the induction of general anesthesia.
DB00474MethohexitalMethohexital is indicated for use as an intravenous anaesthetic. It has also been commonly used to induce deep sedation.
DB00599ThiopentalFor use as the sole anesthetic agent for brief (15 minute) procedures, for induction of anesthesia prior to administration of other anesthetic agents, to supplement regional anesthesia, to provide hypnosis during balanced anesthesia with other agents for analgesia or muscle relaxation, for the control of convulsive states during or following inhalation anesthesia or local anesthesia, in neurosurgical patients with increased intracranial pressure, and for narcoanalysis and narcosynthesis in psychiatric disorders.
DB00708SufentanilThe indications for this drug are as follows: 1. As an analgesic adjunct in the maintenance of balanced general anesthesia in patients who are intubated and ventilated. 2. As a primary anesthetic agent for the induction and maintenance of anesthesia with 100% oxygen in patients undergoing major surgical procedures, in patients who are intubated and ventilated, such as cardiovascular surgery or neurosurgical procedures in the sitting position, to provide favorable myocardial and cerebral oxygen balance or when extended postoperative ventilation is anticipated. 3. For epidural administration as an analgesic combined with low dose (usually 12.5 mg per administration) bupivacaine usually during labor and vaginal delivery 4. The sublingual form is indicated for the management of acute pain in adults that is severe to warrant the use of an opioid analgesic in certified medically supervised healthcare settings, including hospitals, surgical centers, and emergency departments. [FDA label]
DB00802AlfentanilFor the management of postoperative pain and the maintenance of general anesthesia.
DB00813FentanylFor the treatment of cancer patients with severe pain that breaks through their regular narcotic therapy.
DB00818PropofolUsed for induction and/or maintenance of anaesthesia and for management of refractory status epilepticus.
DB00829DiazepamIn general, diazepam is useful in the symptomatic management of mild to moderate degrees of anxiety in conditions dominated by tension, excitation, agitation, fear, or aggressiveness such as may occur in psychoneurosis, anxiety reactions due to stress conditions, and anxiety states with somatic expression [F3160]. Moreover, in acute alcoholic withdrawal, diazepam may be useful in the symptomatic relief of acute agitation, tremor, and impending acute delirium tremens [F3160]. Furthermore, diazepam is a useful adjunct for the relief of skeletal muscle spasm due to reflex spasm to local pathologies, such as inflammation of the muscle and joints or secondary to trauma; spasticity caused by upper motor neuron disorders, such as cerebral palsy and paraplegia; athetosis and the rare "stiff man syndrome" [F3160]. Particular label information from the United Kingdom also lists particular age-specific indications, including for adults: (1) The short-term relief (2-4 weeks) only, of anxiety which is severe, disabling, or subjecting the individual to unacceptable distress, occurring alone or in association with insomnia or short-term psychosomatic, organic or psychotic illness, (2) cerebral palsy, (3) muscle spasm, (4) as an adjunct to certain types of epilepsy (eg. myoclonus), (5) symptomatic treatment of acute alcohol withdrawal, (6) as oral premedication for the nervous dental patient, and (7) for premedication before surgery [L5188]. In the same UK label information, diazepam is indicated in children for: (1) control of tension and irritability in cerebral spasticity in selected cases, (2) as an adjunct to the control of muscle spasm in tetanus, and for (3) oral premedication [L5188].
DB00899RemifentanilFor use during the induction and maintenance of general anesthesia.
DB01154ThiamylalUsed for the production of complete anaesthesia of short duration, for the induction of general anaesthesia, and for inducing a hypnotic state.
DB01221KetamineKetamine is indicated as an anesthetic agent for recommended diagnostic and surgical procedures. If skeletal muscle relaxation is needed, it should be combined with a muscle relaxant. If the surgical procedure involves visceral pain, it should be supplemented with an agent that obtunds visceral pain. Ketamine can be used for induction of anesthesia prior other general anesthetic agents and as a supplement of low potency agents.[L1336, FDA label] Reports have indicated a potential use of ketamine as a therapeutic tool for the management of depression when administered in lower doses.[A31873] These reports have increased the interest for ketamine in this area and several clinical trials are launched for this indication.[L1337, A31874]
DB01440gamma-Hydroxybutyric acidUsed as a general anesthetic, to treat conditions such as insomnia, clinical depression, narcolepsy, and alcoholism, and to improve athletic performance.
DB04827UrethaneNot Available
DB09072Sodium oxybateFor the treatment of cataplexy in narcolepsy and excessive daytime sleepiness (EDS) in narcolepsy.
DB11549TiletamineNot Available
DB13234PropanididNot Available
DrugDrug NameTargetType
DB00292EtomidateGamma-aminobutyric acid receptor subunit alpha-1target
DB00292EtomidateAlpha-2B adrenergic receptortarget
DB00292EtomidateSolute carrier family 2, facilitated glucose transporter member 1carrier
DB00292EtomidateCytochrome P450 11B1, mitochondrialenzyme
DB00292EtomidateCytochrome P450 11B2, mitochondrialenzyme
DB00292EtomidateCytochrome P450 19A1enzyme
DB00292EtomidateGABA-A receptor (anion channel)target
DB00474MethohexitalGamma-aminobutyric acid receptor subunit alpha-1target
DB00474MethohexitalCytochrome P450 2C19enzyme
DB00599ThiopentalGamma-aminobutyric acid receptor subunit alpha-1target
DB00599ThiopentalFatty-acid amide hydrolase 1target
DB00599ThiopentalGamma-aminobutyric acid receptor subunit alpha-2target
DB00599ThiopentalGamma-aminobutyric acid receptor subunit alpha-3target
DB00599ThiopentalGamma-aminobutyric acid receptor subunit alpha-4target
DB00599ThiopentalGamma-aminobutyric acid receptor subunit alpha-5target
DB00599ThiopentalGamma-aminobutyric acid receptor subunit alpha-6target
DB00599ThiopentalNeuronal acetylcholine receptor subunit alpha-4target
DB00599ThiopentalNeuronal acetylcholine receptor subunit alpha-7target
DB00599ThiopentalGlutamate receptor 2target
DB00599ThiopentalGlutamate receptor ionotropic, kainate 2target
DB00599ThiopentalCytochrome P450 2E1enzyme
DB00599ThiopentalCytochrome P450 3A4enzyme
DB00599ThiopentalMuscarinic acetylcholine receptor M3target
DB00599ThiopentalCytochrome P450 2C19enzyme
DB00708SufentanilMu-type opioid receptortarget
DB00708SufentanilDelta-type opioid receptortarget
DB00708SufentanilKappa-type opioid receptortarget
DB00708SufentanilCytochrome P450 3A4enzyme
DB00802AlfentanilMu-type opioid receptortarget
DB00802AlfentanilCytochrome P450 3A4enzyme
DB00802AlfentanilCytochrome P450 3A5enzyme
DB00802AlfentanilAlpha-1-acid glycoprotein 1carrier
DB00802AlfentanilSerum albumincarrier
DB00802AlfentanilCytochrome P450 3A7enzyme
DB00802AlfentanilMultidrug resistance protein 1transporter
DB00813FentanylMu-type opioid receptortarget
DB00813FentanylDelta-type opioid receptortarget
DB00813FentanylCytochrome P450 3A4enzyme
DB00813FentanylCytochrome P450 3A5enzyme
DB00813FentanylCytochrome P450 3A7enzyme
DB00813FentanylMultidrug resistance protein 1transporter
DB00813FentanylKappa-type opioid receptortarget
DB00813FentanylMultidrug resistance protein 1target
DB00818PropofolCytochrome P450 2B6enzyme
DB00818PropofolUDP-glucuronosyltransferase 1-1enzyme
DB00818PropofolUDP-glucuronosyltransferase 1-9enzyme
DB00818PropofolGamma-aminobutyric acid receptor subunit beta-2target
DB00818PropofolGamma-aminobutyric acid receptor subunit beta-3target
DB00818PropofolSerum albumincarrier
DB00818PropofolSodium channel protein type 4 subunit alphatarget
DB00818PropofolSodium channel protein type 2 subunit alphatarget
DB00818PropofolFatty-acid amide hydrolase 1enzyme
DB00818PropofolCytochrome P450 2C9enzyme
DB00818PropofolUDP-glucuronosyltransferase 1-8enzyme
DB00818PropofolCytochrome P450 2E1enzyme
DB00818PropofolCytochrome P450 1B1enzyme
DB00818PropofolCytochrome P450 1A1enzyme
DB00818PropofolCytochrome P450 1A2enzyme
DB00818PropofolCytochrome P450 2C18enzyme
DB00818PropofolCytochrome P450 2C19enzyme
DB00818PropofolCytochrome P450 2C8enzyme
DB00818PropofolUDP-glucuronosyltransferase 1-6enzyme
DB00818PropofolGABA-A receptor (anion channel)target
DB00829DiazepamTranslocator proteintarget
DB00829DiazepamGamma-aminobutyric acid receptor subunit alpha-1target
DB00829DiazepamGamma-aminobutyric acid receptor subunit alpha-2target
DB00829DiazepamGamma-aminobutyric acid receptor subunit alpha-3target
DB00829DiazepamCytochrome P450 3A4enzyme
DB00829DiazepamSerum albumincarrier
DB00829DiazepamCytochrome P450 2C9enzyme
DB00829DiazepamCytochrome P450 2C19enzyme
DB00829DiazepamCytochrome P450 3A5enzyme
DB00829DiazepamCytochrome P450 3A7enzyme
DB00829DiazepamGamma-aminobutyric acid receptor subunit alpha-5target
DB00829DiazepamGamma-aminobutyric acid receptor subunit beta-1target
DB00829DiazepamGamma-aminobutyric acid receptor subunit beta-2target
DB00829DiazepamGamma-aminobutyric acid receptor subunit beta-3target
DB00829DiazepamGamma-aminobutyric acid receptor subunit gamma-1target
DB00829DiazepamGamma-aminobutyric acid receptor subunit gamma-2target
DB00829DiazepamGamma-aminobutyric acid receptor subunit gamma-3target
DB00829DiazepamGamma-aminobutyric acid receptor subunit deltatarget
DB00829DiazepamGamma-aminobutyric acid receptor subunit epsilontarget
DB00829DiazepamGamma-aminobutyric acid receptor subunit pitarget
DB00829DiazepamGamma-aminobutyric acid receptor subunit rho-1target
DB00829DiazepamGamma-aminobutyric acid receptor subunit rho-2target
DB00829DiazepamGamma-aminobutyric acid receptor subunit rho-3target
DB00829DiazepamGamma-aminobutyric acid receptor subunit thetatarget
DB00829DiazepamMultidrug resistance protein 1transporter
DB00829DiazepamCytochrome P450 2B6enzyme
DB00829DiazepamProstaglandin G/H synthase 1enzyme
DB00829DiazepamCytochrome P450 2C18enzyme
DB00829DiazepamCytochrome P450 2C8enzyme
DB00829DiazepamCytochrome P450 2E1enzyme
DB00829DiazepamGABA-A receptor (anion channel)target
DB00899RemifentanilMu-type opioid receptortarget
DB00899RemifentanilDelta-type opioid receptortarget
DB00899RemifentanilKappa-type opioid receptortarget
DB01154ThiamylalGamma-aminobutyric acid receptor subunit alpha-1target
DB01154ThiamylalATP-sensitive inward rectifier potassium channel 8target
DB01154ThiamylalATP-sensitive inward rectifier potassium channel 11target
DB01154ThiamylalCytochrome P450 2C9enzyme
DB01154ThiamylalCytochrome P450 3A4enzyme
DB01154ThiamylalCytochrome P450 2E1enzyme
DB01221KetamineGlutamate receptor ionotropic, NMDA 3Atarget
DB01221KetamineSubstance-P receptortarget
DB01221KetamineCytochrome P450 2B6enzyme
DB01221KetamineCytochrome P450 2C9enzyme
DB01221KetamineCytochrome P450 3A4enzyme
DB01221KetamineD(2) dopamine receptortarget
DB01221KetamineProstaglandin G/H synthase 1enzyme
DB01221KetamineCytochrome P450 2C8enzyme
DB01221KetamineDelta-type opioid receptortarget
DB01221KetamineSodium-dependent noradrenaline transportertarget
DB01221KetamineKappa-type opioid receptortarget
DB01221KetamineMu-type opioid receptortarget
DB01221KetamineMuscarinic acetylcholine receptortarget
DB01221Ketamine5-hydroxytryptamine receptor 2target
DB01221Ketamine5-hydroxytryptamine receptor 1target
DB01221Ketamine5-hydroxytryptamine receptor 3Atarget
DB01221KetamineAlpha-7 nicotinic cholinergic receptor subunittarget
DB01221KetamineCholinesterasetarget
DB01221KetamineNitric oxide synthase, braintarget
DB01440gamma-Hydroxybutyric acidMonocarboxylate transporter 2transporter
DB01440gamma-Hydroxybutyric acidMonocarboxylate transporter 1transporter
DB01440gamma-Hydroxybutyric acidMonocarboxylate transporter 4transporter
DB01440gamma-Hydroxybutyric acidGamma-hydroxybutyrate (GHB) receptortarget
DB01440gamma-Hydroxybutyric acidGamma-aminobutyric acid receptor subunit beta-1target
DB04827UrethaneCytosolic phospholipase A2enzyme
DB04827UrethaneMyeloperoxidaseenzyme
DB04827UrethaneAldehyde oxidaseenzyme
DB09072Sodium oxybateSuccinate-semialdehyde dehydrogenase, mitochondrialenzyme
DB09072Sodium oxybateHydroxyacid-oxoacid transhydrogenase, mitochondrialenzyme