Aprobarbital

210.22976

210.23

200-997-4

Q0YKG9L6RF

2100

120769

DTXSID8022616

CRYSTALS|Fine, white, crystalline powder

N - Nervous system

75.27000

1.22850

Solid

1.086 g/cm3

140-141.5 °C

1.476

4.121g/L(25 ºC)

2-8°C

Peritoneal-rat LDL0: 100 mg/kg; peritoneal-mouse LD50: 200 mg/kg

Flammable; burning produces toxic nitrogen oxide fumes

SLIGHTLY BITTER

A SATURATED AQUEOUS SOLN IS ACID TO LITMUS

7.99(at 25 °C)

7.99 (at 25 °C)|pKa 7.99

OPTIC SIGN: -; EXTINCTION: INCLINED

11-23/25-36/38

16-24-45

F,T

Treasury is ventilated, low temperature and dry; stored separately from food materials

STABLE IN AIR

P264, P270, P301+P310, P321, P330, P405, P501

H301

Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended; 21 U.S.C. 321-392).|5-Allyl-5-isopropylbarbituric acid is a chemical derivative of barbituric acid, named in section 502(d) of the Federal Food, Drug, and Cosmetic Act, and is hereby designated as habit forming.|Warning and caution statements for 5-allyl-5-isopropylbarbituric acid specifically required by law. PREPARATIONS CONTAINING HABIT-FORMING DERIVATIVES OF SUBSTANCES NAMED IN SECTION 502(d) OF THE FEDERAL FOOD, DRUG, AND COSMETIC ACT ... The statement "Warning-May be habit forming" is required to appear on the labels of all drugs containing derivatives designated in 21 CFR 329.1 ... as habit forming.|Schedules of controlled substances are established by section 202 of the Controlled Substances Act (21 U.S.C. 812). Schedule III includes any substance which contains any quantity of a derivative of barbituric acid or any salt thereof. DEA Code #2100; Drug class: Depressant. /Derivatives of barbituric acid or any salt thereof/|For more FDA Requirements (Complete) data for APROBARBITAL (6 total), please visit the HSDB record page.

|Danger|H301 (100%): Toxic if swallowed [Danger Acute toxicity, oral]|P264, P270, P301+P310, P321, P330, P405, and P501|Aggregated GHS information provided by 39 companies from 1 notifications to the ECHA C&L Inventory.

highly toxic

IN CAT CEREBRAL CORTEX, BARBITURATES IN ANESTHETIC DOSES SELECTIVELY ABOLISH EXCITATION BUT NOT INHIBITION ELICITED BY NOREPINEPHRINE APPLIED DIRECTLY TO VARIOUS SYNAPSES... /BARBITURATES/|AT SKELETAL NEUROMUSCULAR JUNCTIONS BLOCKING EFFECTS OF BOTH D-TUBOCURARINE & DECAMETHONIUM ARE ENHANCED BY BARBITURATES. /BARBITURATES/|BOTH CARDIAC GLYCOSIDES & BETA-ADRENERGIC AGONISTS ANTAGONIZE MYOCARDIAL DEPRESSANT ACTION /OF BARBITURATES/. /BARBITURATES/|INTENSITY OF CNS DEPRESSION CAN BE INCR BY ACIDIC DRUGS SUCH AS ASPIRIN ... WHICH DISPLACE BARBITURATES FROM PLASMA PROTEINS. /BARBITURATES/|For more Interactions (Complete) data for APROBARBITAL (14 total), please visit the HSDB record page.

BARBITURATES MAY BE USED FOR PREANESTHETIC MEDICATION & TO PRODUCE BASAL ANESTHESIA. ... BARBITURATES ARE EMPLOYED AS DIAGNOSTIC & THERAPEUTIC AIDS IN PSYCHIATRY, IN NARCOANALYSIS & NARCOTHERAPY. /BARBITURATES/|ONE OF THE INTERMEDIATE-ACTING BARBITURATES ...|Aprobartital has been used for the short-term treatment /2 weeks or less/ of insomnia; however, it generally has been replaced by benzodiazepines. ... Has also been used for routine sedation to relieve anxiety, tension, and apprehension; however, barbiturates generally have been replaced by benzodiazepines for daytime sedation. /Uses are included in the labeling approved by the US Food and Drug Administration/.|The primary Medication Classification of the Veterans Administrations is CN301: Barbituric Acid Derivatives, Sedatives/Hyponotics.

May be habit forming.|AS WITH ETHANOL ... SEDATIVE DOSES THAT EXERT NO EFFECTS OBVIOUS TO UNTRAINED OBSERVER OR PATIENTS CAN CAUSE IMPAIRMENT IN LEARNING, JUDGEMENT, SHORT-TERM MEMORY, DRIVING PERFORMANCE ... /BARBITURATES/|... IMPORTANT IN USE ... DURING LABOR IS ... POSSIBLE RESP DEPRESSANT EFFECT ON INFANT, SINCE PLACENTA OFFERS NO SIGNIFICANT BARRIER ... /BARBITURATES/|CAPACITY OF BARBITURATES TO INCR SYNTHESIS OF PORPHYRINS IS RESPONSIBLE FOR ONE ... BIZARRE & DANGEROUS SIDE EFFECT. IN PT SUFFERING FROM ACUTE INTERMITTENT PORPHYRIA, DRUGS MAY PPT SEVERE ATTACK, POSSIBLY ... PARALYSIS & DEATH. /BARBITURATES/|For more Drug Warnings (Complete) data for APROBARBITAL (15 total), please visit the HSDB record page.

EFFECT OF THE BIOTRANSFORMABLE BARBITURATES TO INCR RATE OF THEIR OWN METAB ACCOUNTS FOR PART OF TOLERANCE TO THE DRUGS. ... PHARMACODYNAMIC TOLERANCE INVOLVES ADAPTATION OF NERVOUS TISSUE TO PRESENCE OF THE DRUG. ... CNS MAY BECOME RESISTANT ... DURING A SINGLE ADMIN ... KNOWN AS "ACUTE TOLERANCE." /BARBITURATES/

RATE OF DECLINE OF BLOOD CONCN AFTER A LARGE DOSE FOR ... ALURATE ... IS 25-40% /PER 24 HR/ ... RATE OF DECLINE IS A FUNCTION OF ACCUMULATION IN LIVER, METAB OF DRUG & URINARY EXCRETION.|AS MUCH AS 50% OF HYPNOTIC DOSE OF ... APROBARBITAL MAY BE EXCRETED UNCHANGED BY KIDNEY. ... APROBARBITAL ... ELIMINATED SLOWLY, OVER A PERIOD OF SEVERAL DAYS.|A FRACTION OF BARBITURATE IN BLOOD IS REVERSIBLY BOUND TO PLASMA PROTEIN, CHIEFLY ALBUMIN. ... THE CEREBROSPINAL FLUID IS VIRTUALLY PROTEIN FREE. ACCORDINGLY, THE MAXIMAL CONCN OF BARBITURATES ATTAINED IN CEREBROSPINAL FLUID IS LESS THAN THE PLASMA CONCN, BEING IN MOST CASES SLIGHTLY LESS THAN THE CONCN IN AN ULTRAFILTRATE OF PLASMA. THE CONCN IN OCULAR FLUID IS SIMILAR TO THAT OF CEREBROSPINAL FLUID. IN TISSUES, THE BARBITURATE CONCN IS GENERALLY AS HIGH AS OR SLIGHTLY HIGHER THAN IN PLASMA. /BARBITURATES/|... SODIUM SALTS ARE MORE RAPIDLY ABSORBED THAN FREE ACIDS ... FOOD IN STOMACH DECR RATE OF ABSORPTION BUT NOT AMT ABSORBED. THERE EXISTS NO IMPENETRABLE BARRIER TO ... BARBITURATES IN BODY ... IF SOJOURN OF DRUG IN PLASMA IS SUFFICIENTLY LONG, IT WILL BE DISTRIBUTED TO ALL TISSUES & FLUIDS. /BARBITURATES/|For more Absorption, Distribution and Excretion (Complete) data for APROBARBITAL (10 total), please visit the HSDB record page.

PARTLY METABOLIZED IN LIVER BY OXIDN OF C-5 SUBSTITUENT(S) (ALLYL &/OR ISOPROPYL GROUPS) ... ALLYL GROUP ... MAY ALSO /BE REMOVED/. RESULTING /IN/ INACTIVE METABOLITES /HUMAN, ORAL/.|Hepatic biotransformation, primarily by the hepatic microsomal enzyme system. /barbiturates/|Partially metabolized in the liver by oxidation of the C5 substituent(s) (allyl and/or isopropyl groups). Removal of the allyl group at C5 may also occur. The resulting inactive metbolites, which have not been identified are excreted in the urine.|With the exception of the less lipid-soluble aprobarbital and phenobarbital, nearly complete metabolism and/or conjugation of barbiturates in the liver precedes their renal excretion. The oxidation of radicals at C5 is the most important biotransformation responsible for termination of biological activity. Oxidation results in the formation of alcohols, ketones, phenols, or carboxylic acids, which may appear in the urine as such or as glucuronic acid conjugates. In some instances (eg, phenobarbital), N-glucosylation is an important metabolic pathway. Other biotransformations include N-hydroxylation, desulfuration of thiobarbiturates to oxybarbiturates, opening of the barbituric acid ring, and N-dealkylation of N-alkylbarbiturates to active metabolites (eg, mephobarbital to phenobarbital).

APROBARBITAL DOSE 0.75 G ORAL REACHED CONCN 2.3 MG% IN 3-9 HR; T/2 WAS 24-36 HR. /FROM TABLE/|Plasma half-life is about 14 fto 40 hours.

Aprobarbital (like all barbiturates) works by binding to the GABAA receptor at either the alpha or the beta sub unit. These are binding sites that are distinct from GABA itself and also distinct from the benzodiazepine binding site. Like benzodiazepines, barbiturates potentiate the effect of GABA at this receptor. This GABAA receptor binding decreases input resistance, depresses burst and tonic firing, especially in ventrobasal and intralaminar neurons, while at the same time increasing burst duration and mean conductance at individual chloride channels; this increases both the amplitude and decay time of inhibitory postsynaptic currents. In addition to this GABA-ergic effect, barbiturates also block the AMPA receptor, a subtype of glutamate receptor. Glutamate is the principal excitatory neurotransmitter in the mammalian CNS. Aprobarbital also appears to bind neuronal nicotinic acetylcholine receptors.|... REVERSIBLY DEPRESS ACTIVITY OF ALL EXCITABLE TISSUES. ... CNS IS ... SENSITIVE, SO ... IN SEDATIVE OR HYPNOTIC DOSES, VERY LITTLE EFFECT ON SKELETAL, CARDIAC, OR SMOOTH MUSCLE OCCURS. ... PROBABLE THAT EXCITABILITY IN EACH TISSUE IS DEPRESSED BY AN ACTION ON OR IN A MEMBRANE & THAT ... MECHANISMS ... ARE ... SIMILAR. /BARBITURATES/|AS DOSE ... INCR, HYPOXIC & CHEM DRIVES TO RESP ARE DIMINISHED ... HOWEVER, HYPOXIC DRIVE PERSISTS @ LEVELS OF INTOXICATION CAUSING ... INSENSITIVITY OF RESP CENTERS TO CO2. ... AS INTOXICATION /INCR/ ... THERE IS SHIFT IN CONTROL OF RESP FROM CO2-SENSITIVE AREAS OF MEDULLA TO MORE PRIMITIVE ... CAROTID & AORTIC ... /BARBITURATES/|WHATEVER ... THE EFFECTS OF BARBITURATES ELSEWHERE IN CNS, IT IS EFFECT ON RETICULAR SYSTEM ... RESPONSIBLE FOR INABILITY TO MAINTAIN WAKEFULNESS UNDER INFLUENCE OF A BARBITURATE. /BARBITURATES/|BARBITURATES DECR TURNOVER OF 5-HYDROXYTRYPTAMINE & CATECHOLAMINES IN BRAIN OF EXPTL ANIMALS, BUT WHETHER THIS IS CAUSE OR EFFECT OF ANESTHESIA IS CONJECTURAL. /BARBITURATES/|For more Mechanism of Action (Complete) data for APROBARBITAL (10 total), please visit the HSDB record page.

TREATMENT: Stabilization: Respiratory arrest is the major cause of early death. Assess the patency of the airway and the adequacy of ventilation first. Appropriate corrective measures include supplemental oxygen, head tilt-chin lift, intubation, and assisted ventilation. Establish an iv line with Ringer's lactate and give a fluid challenge up to 2 l for patients who are hypotensive. Cardiac dysrhythmias are rare but were reported. ... Be sure to give glucose, naloxone, and thiamine to all patients with depressed mental status. /Barbiturates/|Gut Decontamination: Because of decr gastrointestinal mobility and delayed gastric emptying, gut decontamination is indicated 6-8 hr postingestion in obtunded patients. Barbiturates are well absorbed by charcoal; 10 times the ingested dose (or 1 g/kg body weight) should be given together with a cathartic (sorbitol, magnesium citrate) to all patients. /Barbiturates/|Elimination Enhancement: Most overdose patients respond to supportive care and require no special measures. ... Alkaline diuresis is ineffective for short and intermediate acting barbiturates. ... Hemoperfusion: This measure is more effective than dialysis for short and intermediate acting barbiturates. ...|Antidotes: No effective antidotes are available. Respiratory and central nervous stimulants incr complications and should be avoided. /Barbiturates/

... BARBITURATES REDUCE AMT OF TIME SPENT IN REM PHASE SLEEP, &, IN THIS ... BARBITURATE-INDUCED SLEEP DIFFERS FROM PHYSIOLOGICAL SLEEP. ... CLAIMED ... THAT DEPRIVATION OF THIS PHASE ... MAY HAVE DELETERIOUS EFFECTS. SUBJECTS DEPRIVED OF REM ... EXHIBIT REBOUND INCR IN ... TIME SPENT IN REM SLEEP FOLLOWING ... DEPRIVATION. /BARBITURATE/|PROLONGED USE OF BARBITURATES INCR RESTLESSNESS DURING LATE STAGES OF SLEEP, CAUSES ANXIETY, & INCR PLASMA CONCN OF GROWTH HORMONE BUT DECR THOSE OF ADRENOCORTICOIDS. ... IN SMALL DOSES, BARBITURATES MAY INCR REACTION TO PAINFUL STIMULI. /BARBITURATES/|OXYBARBITURATES TEND TO DECR TONUS OF GI MUSCULATURE & AMPLITUDE OF RHYTHMIC CONTRACTIONS. /OXYBARBITURATES/|SEVERE OLIGURIA OR ANURIA MAY OCCUR IN ACUTE ... POISONING, LARGELY AS RESULT OF MARKED HYPOTENSION. /BARBITURATES/|For more Human Toxicity Excerpts (Complete) data for APROBARBITAL (17 total), please visit the HSDB record page.

allylpropymal

Aprobarbital|Alurate|2100|Schedule III - Substances in the DEA Schedule III have a potential for abuse less than substances in Schedules I or II and abuse may lead to moderate or low physical dependence or high psychological dependence.|No

Alurate Elixir, oral solution with aprobarbital 40 mg/5 ml and alcohol 20%.|Oral solution: 40 mg/5 ml, Alierate on Elixis (C-III with 20% alc)

MICROCHEMICAL TEST|IDENTIFICATION OF APROBARBITAL & OTHER BARBITURATES BY CHEM IONIZATION & MASS ANALYZED ION KINETIC ENERGY SPECTROMETRY.|DIMETHYLFORMAMIDE DIMETHYLACETAL AS A DERIVATIZING AGENT FOR GAS LIQUID CHROMATOGRAPHY OF BARBITURATES.|A simple and reproducible method for the analysis of barbiturates, including apobarbital by GC/MS after derivatization with DMF di-Pr acetal is reported. The method is readily adapted to screening, confirmation, and quantitation.|An ion mobility detector was used for qualitative and quant determination of 5,5'-disubstituted barbiturates including apobarbital after capillary GC separation Using a recently developed time dispersive Fourier transform method for ion mobility spectrometry, complete ion mobility spectra could be obtained for each component in the chromatogram. This type of spectra can be used for providing qualitative information on unknown cmpd or for selecting the proper detector conditions needed when operating in the continuous mobility monitoring mode. Five barbiturates investigated produced a Fourier transformed ion mobility spectrum containing one major product ion. When drift times corresponding to those of the product ions measured in the Fourier transform mode were monitored continuously, selective chromatographic detection of the barbiturates was achieved. In one case even isomers were differentiated based on mobility characteristics.

With high doses and/or chronic daily doses, homogeneous enzyme immunoassay (EMIT) and radioimmunoassay (RIA) can be used effectively for screening /urine/. Gas liquid chromatography/flame ionization detector (GLC/FID) after derivatization, gas liquid chromatography /nitrogen-phosphorus detector (GLC/NPD) and gas liquid chromatography/mass spectrometry are reliable methods used for confirmation of the various barbiturates. /Barbiturates/|A GC/MS procedure is described for the identification and differentiation of sedative-hypnotics and their metabolites in urine. The following 24 barbiturates and 13 other hypnotics could be detected: acecarbromal, allobarbital, amobarbital, aprobarbital, barbital, brallobarbital, bromisoval, (sec)butabarbital, butalbital, butobarbital, carbromal, clomethiazole, crotylbarbital, cyclobarbital, cyclopentobarbital, diethylallylacetamide, dipropylbarbital, glutethimide, guaifenesin, ethinamate, heptabarbital, hexobarbital, meprobamate, methaqualone, metharbital, methohexital, methylphenobarbital, methyprylone, pentobarbital, phenobarbital, propallylonal, pyrithyldione, secobarbital, thiobutabarbital, thiopental, vinbarbital, and vinylbital. The procedure presented is integrated in a general screening procedure (general unknown analysis) for several groups of drugs detecting over 300 drugs and over 1000 of their metabolites. It includes cleavage of conjugates by acid hydrolysis, isolation by liq-liq extraction, derivatization by acetylation, separation by capillary GC, and identification by computerized MS. Using mass chromatography with the selected ions m/z 83, 117, 141, 167, 169, 207, 221, and 235, the presence of barbiturates, other hypnotics and/or their metabolites was indicated. The identity of pos signals in the reconstructed mass chromatograms was confirmed by a visual or computerized comparison of the stored full mass spectra with the ref. spectra. The sample preparation, mass chromatograms, ref. mass spectra and GC retention indexes are documented.|After extraction with Et2O clonazepam and the internal std were separated from plasma and urine by HPLC on a reversed-phase Nova Pak C18 column with MeCN-MeOH-6 mM phosphate buffer (pH 5.7) (30:10:60) as the mobile phase and detection at 242 nm. The urine samples were pretreated with beta-D-glucuronidase. The recovery of clonazepam from plasma samples of 0.2 mg/l was 89.3% at a plasma concn of 40 ug/l; the coefficients of variation were 6.2% for within-run precision and 7.4% for day-to-day precision. For pediatric samples, a minimum of 200 ul serum or urine can be analyzed without loss of precision. The method enables other benzodiazepines used in therapy or found in cases of intoxication to be resolved.|After extract from human blood plasma onto SEP PAK C18 reversed-phase columns, drugs of abuse can be separated by TLC and visualized and identified by UV light and various spray reagents. Data are presented comparing the discriminant powers of 11 such systems with respect to 16 common drugs of abuse, including apobarbital.|Barbiturates (aprobarbitone, amylobarbitone, barbitone, dial, pentobarbitone, phenobarbitone, quinalbarbitone, secobarbital, and talbutal), salicylic acid, caffeine, and theophylline can be identified in human blood plasma by extraction of samples on a SepPak C18 cartridge followed by UV spectroscopic characterization.