펜토바비탈

Water spray, dry chemical, carbon dioxide, or foam as appropriate for surrounding fire and materials.

As with all fires, evacuate personnel to a safe area. Firefighters should use self-contained breathing equipment and protective clothing.

Store in tight, light-resistant container as defined in the USP-NF. This material should be handled and stored per label instructions to ensure product integrity.

Pentobarbital sodium injection should be stored at room temperature; freezing and exposure of the injection to extreme heat should be avoided. Brief exposure to temperatures up to 40 °C will not adversely affect the injection.

SRP: Expired or waste pharmaceuticals shall carefully take into consideration applicable DEA, EPA, and FDA regulations. It is not appropriate to dispose by flushing the pharmaceutical down the toilet or discarding to trash. If possible return the pharmaceutical to the manufacturer for proper disposal being careful to properly label and securely package the material. Alternatively, the waste pharmaceutical shall be labeled, securely packaged and transported by a state licensed medical waste contractor to dispose by burial in a licensed hazardous or toxic waste landfill or incinerator.

SRP: At the time of review, regulatory criteria for small quantity disposal are subject to significant revision, however, household quantities of waste pharmaceuticals may be managed as follows: Mix with wet cat litter or coffee grounds, double bag in plastic, discard in trash.

This material is assumed to be combustible. As with all dry powders, it is advisable to ground mechanical equipment in contact with dry material to dissipate the potential buildup of static electricity.

As a general rule, when handling USP Reference Standards avoid all contact and inhalation of dust, mists, and/or vapors associated with the material. Wash thoroughly after handling.

/Use/ safety goggles /and/ protect exposed skin.

Engineering controls such as exhaust ventilation are recommended.

Use a NIOSH-approved respirator, if it is determined to be necessary by an industrial hygiene survey involving air monitoring. In the event that a respirator is not required, an approved dust mask should be used.

Treatment of overdosage is mainly supportive and consists of maintaining an adequate airway, with assisted respiration and oxygen administration as necessary, monitoring of vital signs and fluid balance, and fluid therapy and other standard treatment for shock, if needed. If renal function is normal, forced diuresis may aid in the elimination of the barbiturate. Alkalinization of the urine increases renal excretion of some barbiturates, especially phenobarbital, also aprobarbital and mephobarbital (which is metabolized to phenobarbital). Although not recommended as a routine procedure, hemodialysis may be used in severe barbiturate intoxications or if the patient is anuric or in shock. The patient should be rolled from side to side every 30 minutes and antibiotics should be given if pneumonia is suspected. Appropriate nursing care to prevent hypostatic pneumonia, decubiti, aspiration, and other complications of patients with altered states of consciousness. (L1712)

Acute dosage of mice with DDT prolonged pentobarbitone sleeping time, with inhibition of barbiturate metabolism, but chronic dosage of mice or rats shortened sleeping time because of enzyme induction.

Pentobarbital & streptomycin interact to induce vasodilation in the perfused kidney & other vessels of the dog.

During evaluations of a vaccine of killed suspensions of Corynebacterium parvum, iv injections of Corynebacterium parvum in mice rendered them lethally sensitive to normal safe anesthetic doses of pentobarbitone. Caution was recommended when both preparations might be used in man.

Therapeutic effects of acetaminophen may be decreased when the medication is used concurrently in patients receiving chronic barbiturate therapy because of increased metabolism resulting from induction of hepatic microsomal enzymes; risk of hepatotoxicity with single toxic doses or prolonged use of high doses of acetaminophen may be increased in alcoholics or in patients regularly using hepatic enzyme inducers such as barbiturates. /Barbiturates/

For more Interactions (Complete) data for Pentobarbital (42 total), please visit the HSDB record page.

TERRESTRIAL FATE: Based on a classification scheme(1), an estimated Koc value of 28(SRC), determined from a log Kow of 2.10(2) and a regression-derived equation(3), indicates that pentobarbital is expected to have very high mobility in soil(SRC). The pKa of pentobarbital is 7.8(4), indicating that this compound will exist partially in the anion form in the environment and anions generally do not adsorb more strongly to soils containing organic carbon and clay than their neutral counterparts(5). Volatilization of the neutral species from moist soil surfaces is not expected to be an important fate process(SRC) given an estimated Henry's Law constant of 8.4X10-13 atm-cu m/mole(SRC), using a fragment constant estimation method(6). Pentobarbital is not expected to volatilize from dry soil surfaces(SRC) based upon an estimated vapor pressure of 3.0X10-10 mm Hg at 25 °C(SRC), determined from a fragment constant method(7). Biodegradation data were not available(SRC, 2009).

AQUATIC FATE: Based on a classification scheme(1), an estimated Koc value of 28(SRC), determined from a log Kow of 2.10(2) and a regression-derived equation(3), indicates that pentobarbital is not expected to adsorb to suspended solids and sediment(SRC). Volatilization from water surfaces is not expected(4) based upon an estimated Henry's Law constant of 8.4X10-13 atm-cu m/mole(SRC), developed using a fragment constant estimation method(5). According to a classification scheme(6), an estimated BCF of 11(SRC), from its log Kow(2) and a regression-derived equation(7), suggests the potential for bioconcentration in aquatic organisms is low(SRC). Biodegradation data were not available(SRC, 2009).

ATMOSPHERIC FATE: According to a model of gas/particle partitioning of semivolatile organic compounds in the atmosphere(1), pentobarbital, which has an estimated vapor pressure of 3.0X10-10 Hg at 25 °C(SRC), determined from a fragment constant method(2), is expected to exist solely in the particulate phase in the ambient atmosphere. Particulate-phase pentobarbital may be removed from the air by wet or dry deposition(SRC). Pentobarbital does not contain chromophores that absorb at wavelengths >290 nm(3) and therefore is not expected to be susceptible to direct photolysis by sunlight(SRC).

The main adverse reactions surrounding pentobarbital use are CNS effects, including altered mental status, agitation, confusion, drowsiness, respiratory depression, bradycardia, hypotension, cardiovascular collapse, and syncope. Other significant adverse effects to be aware of include hallucinations, headache, insomnia, nausea, vomiting, hepatoxicity, megaloblastic anemia, angioedema, local injection site reactions, laryngospasm, bronchospasm, apnea, and hyperkinesia. At high doses of pentobarbital, total loss of neurological function is observed.

Pediatric neurotoxicity is reported with the use of pentobarbital. Barbiturates, including pentobarbital, can increase GABA activity, leading to increased neuronal apoptosis and impaired cognition when used for more than 3 hours. Treatment of pentobarbital toxicity involves supportive care, as no antidote exists. Overdose can lead to airway compromise, cardiovascular collapse, coma, and death. Treatment often requires intubation, hemodynamic support with vasopressors, and maintaining body temperature with warmers, commonly in an intensive care unit (ICU) setting. In mild or early cases of toxicity, activated charcoal and alkaline diuresis have been added but show minimal benefits. Always contact poison control if poisoning or overdose is suspected.

Pentobarbital binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged. All of these effects are associated with marked decreases in GABA-sensitive neuronal calcium conductance (gCa). The net result of barbiturate action is acute potentiation of inhibitory GABAergic tone. Barbiturates also act through potent (if less well characterized) and direct inhibition of excitatory AMPA-type glutamate receptors, resulting in a profound suppression of glutamatergic neurotransmission.

The Koc of pentobarbital is estimated as 28(SRC), using a log Kow of 2.10(1) and a regression-derived equation(2). According to a classification scheme(3), this estimated Koc value suggests that pentobarbital is expected to have very high mobility in soil. The pKa of pentobarbital is 7.8(4), indicating that this compound will exist partially in the anion form in the environment and anions generally do not adsorb more strongly to soils containing organic carbon and clay than their neutral counterparts(5). The pK values of the hypnotically active barbituric acids range between 7.78 and 8.30. Disubstituted barbituric acids exist in the undissociated form at pH 7.4 and the degree of dissociation is strongly influenced by slight alterations in pH(4).

/HUMAN EXPOSURE STUDIES/ To investigate the effect of sedative agents on visual processing in humans, /investigators/ analysed the BOLD contrast signal response to a visual stimulation paradigm in 15 healthy, adult volunteers using functional magnetic resonance imaging. The subjects were tested during alert state and under sedation following intravenous administration of pentobarbital. The injection of pentobarbital not only significantly reduced the response signal strength but the reduction in BOLD contrast signal was related to the ratio of amount of sedative administered and the subject's body weight. The three subjects with the highest relative sedative dosage even displayed an inverted (negative) BOLD contrast signal. A significant reduction in the number of positively correlating pixels was found 15 min after administration of pentobarbital. All measured parameters returned to near pre-sedative levels by the end of the experimental session. The relative dosage dependence of the strength of the BOLD signal the negative BOLD signal in the three subjects with the highest relative sedative dosage indicates that pentobarbital had a more pronounced effect on cerebral blood flow than on cerebral oxidative metabolism.

/HUMAN EXPOSURE STUDIES/ /Investigators/hypothesized that pentobarbital would improve upper airway mechanics based on an increase in: a) latency to arousal, b) amplitude of the phasic genioglossus electromyogram, and decrease in: c) the active upper-airway critical closing pressure (Pcrit).Twelve healthy subjects received pentobarbital 100 mg or placebo in a double-blind, cross-over protocol. During wakefulness, /investigators/ measured the genioglossus reflex response to negative-pressure pulses. During sleep, carbon dioxide was insufflated into the inspired air. Airway pressure was then decreased in a stepwise fashion until arousal from sleep.With basal breathing during sleep, flow-rate was lower in volunteers given pentobarbital, end-tidal carbon dioxide concentration and upper airway resistance were greater, and Pcrit was unaffected (pentobarbital: -11.7+/-4.5 vs. placebo: -10.25+/-3.6 cm H2O, p=0.11). Pentobarbital increased the time to arousal (297+/-63s vs. 232+/-67s p<0.05), at which time phasic genioglossus EMG was higher (6.2+/-4.8 %max vs. 3.1+/-3%, respectively, p<0.05) as were carbon dioxide levels. The increase in genioglossus electromyogram after carbon dioxide administration was greater after pentobarbital vs. placebo. Pentobarbital did not affect the genioglossus negative pressure reflex.Pentobarbital increases the time to arousal and stimulates genioglossus muscle activity, but it increases upper airway resistance during sleep.

/SIGNS AND SYMPTOMS/ Complications such as pneumonia, pulmonary edema, cardiac arrhythmias, congestive heart failure, and renal failure may occur. Uremia may increase CNS sensitivity to barbiturates.

/SIGNS AND SYMPTOMS/ In extreme overdose, all electrical activity in the brain may cease, in which case a "flat" EEG normally equated with clinical death cannot be accepted. This effect is fully reversible unless hypoxic damage occurs. Consideration should be given to the possibility of barbiturate intoxication even in situations that appear to involve trauma.

The Approved Drug Products with Therapeutic Equivalence Evaluations List identifies currently marketed prescription drug products, including pentobarbital, approved on the basis of safety and effectiveness by FDA under sections 505 of the Federal Food, Drug, and Cosmetic Act.

The Generic Animal Drug and Patent Restoration act requires that each sponsor of an approved animal drug must submit to the FDA certain information regarding patents held for the animal drug or its method of use. The Act requires that this information, as well as a list of all animal drug products approved for safety and effectiveness, be made available to the public. Pentobarbital is included on this list.

The Generic Animal Drug and Patent Restoration act requires that each sponsor of an approved animal drug must submit to the FDA certain information regarding patents held for the animal drug or its method of use. The Act requires that this information, as well as a list of all animal drug products approved for safety and effectiveness, be made available to the public. Pentobarbital sodium is included on this list. /Pentobarbital sodium/

Sodium pentobarbital injection. ... The drug is indicated for use as a general anesthetic in dogs and cats. Although it may be used as a general surgical anesthetic for horses, it is usually given at a lower dose to cause sedation and hypnosis and may be supplemented with a local anesthetic. It may also be used in dogs for the symptomatic treatment of strychnine poisoning. /Sodium pentobarbital/

For more FDA Requirements (Complete) data for Pentobarbital (7 total), please visit the HSDB record page.

This is a controlled substance.

THERAPEUTIC CATEGORY: Sedative, hypnotic

THERAPEUTIC CATEGORY (VET): Anesthetic (intravenous); for euthenasia

MEDICATION

MEDICATION (VET)

For the short-term treatment of insomnia.

Ethyl cyanoacetate + methyl propyl ketone + ethyl bromide + dicyandiamide (Cope reaction/hydrogenation/dehydrobromination/cyclisation/nitrile hydrolysis/decarboxylation).

It is prepared by boiling ethyl-1-methylbutylcyanoacetic ester with guanidine in sodium ethoxide solution and saponifying the product with dilute sulfuric acid.

The 5,5-disubstituted barbituric acids are still synthesized by the classical condensation of substituted malonic esters, malonic amides, or cyanoacetic esters with urea, thiourea, guanidine, or dicyanodiamide, followed by the hydrolysis of the resulting imino- or cyanobarbiturate. /5,5-Disubstituted barbituric acids/

Pentobarbital sodium preparations: (AHFS, 2009)

Pentobarbital sodium, soluble pentobarbital, Carbrital, Narcoren, Nembutal, Pentone, Praecicalm, Somnopentyl, Sopental. /Sodium pentobarbital/.

Pentobarbital calcium, Repocal