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Euthanasia
Published in Michele Barletta, Jane Quandt, Rachel Reed, Equine Anesthesia and Pain Management, 2023
Barbiturates or barbituric acid derivatives Pentobarbital 100 mg/kg IV alone or in combination with other agents is the euthanasia method of choice. Due to the large volume required, administration through an intravenous (IV) catheter placed in the jugular vein is recommended. The use of acepromazine, α2 adrenergic receptor agonists and/or opioids may facilitate restraint in fractious patients, but may also prolong the time to loss of consciousness due to effects on cardiac output.
Sedative and Hypnotic Drugs
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Arup Kumar Misra, Pramod Kumar Sharma
Alkyl or aryl group added barbituric acid at fifth position increases its depressive action on CNS, thus confers sedative–hypnotic activity. At position C2, replacement of sulphur with oxygen confers increase in lipophilicity and thus accelerates its sedative–hypnotic action, increases its potency, and increases metabolic degradation (Brunton et al., 2018).
Barbiturates And Minor Tranquilizers
Published in S.J. Mulé, Henry Brill, Chemical and Biological Aspects of Drug Dependence, 2019
As previously mentioned, the hexahydro-pyrimidine nucleus of barbituric acids contains three carbonyl groups which are capable of undergoing tautomeric transformations with an equilibrium existing between the lactam (keto) and lactim (enol) moieties (Figure 3).2 In solution monosubstitued and disubstituted barbituric acid derivatives are considered to undergo only single enolization. For example, 1, 3 disubstituted barbituric acid may exist in the following moieties (Figure 4).7 “9 The lactam moiety, stable in acidic solutions, is in equilibrium with lactim A and B, which are stable in an alkaline medium.8 In the crystalline state, barbituric acid is in the lactam form. This was based on infrared spectral data which showed no absorption bands indicative of a -C=C-or-C=N- linkage, whereas an intense absorption band occurred for carbonyl groups.1
The effect of acidic beverage versus mineral water on the change in serum phenobarbital concentrations: a randomized clinical trial on children with seizure
Published in International Journal of Neuroscience, 2021
Morteza Tavasolizadeh, Kazem Hasanpour, Milad Nazarzadeh, Davood Mahdian, Omid Gholami
Phenobarbital, the eldest modern anti-epileptic medication discovered in 1912, is a derivation of barbituric acid that increase binding to inhibitory gamma-aminobutyric acid receptors. It also inhibits glutamate induced depolarizations and regulate chloride currents through receptor channels [1]. One of the most common antiepileptic drugs used in neonates and children is phenobarbital [2]. One of the most important determination for oral bioavailability of drugs is absorption [3] and Phenobarbital has a weak acidity nature (pH at which the drug is 50% ionized (pKa) = 7.3). Absorption of a drug is influenced by the ionization state of drug, and ionization process is depends on the pH of the environment [4]. In an unionized state, permeability through the lipid bilayers of the intestinal mucosa is higher [4]. Based on Henderson–Hasselbalch equation, weak acidic drugs are predominantly in the unionized state and will thereby permeate more readily [4]. Therefore, based on the previous pharmacokinetics evidence, we hypothesized that intake of Phenobarbital with an acidic beverage such as Orange juice may increase Phenobarbital oral absorption.
Xanthine oxidase inhibitors: patent landscape and clinical development (2015–2020)
Published in Expert Opinion on Therapeutic Patents, 2020
Jatinder Vir Singh, Preet Mohinder Singh Bedi, Harbinder Singh, Sahil Sharma
The recent patent survey clearly indicates that the majority of efforts have been made toward the discovery of nonpurine and natural XO inhibitors. The literature has highlighted the number of small molecules with extreme potency against the enzyme with IC50 values in nanomolar range. Particularly, selenazole-based molecules patented by Atom Bioscience and Pharmaceutical Co, Ltd., showed excellent inhibition against XO with the IC50 value of 1.32 nM [83]. Teijin Pharma Limited patented azole benzene derivatives showed IC50 values below 5 nM against the enzyme with substantial hypouricemic effect in animal models [84]. A significant contribution was also made by Warrel research group by the discovery of small barbituric acid-based molecules with dual XO and URAT1 inhibitory potential [86,87]. Many of these reports also claimed that the compounds are safer than current drug therapy for hyperuricemia. These properties would enable them worthwhile to use in clinical studies for the treatment of hyperuricemia and gout.
Synthesis and characterisation of thiobarbituric acid enamine derivatives, and evaluation of their α-glucosidase inhibitory and anti-glycation activity
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
M. Ali, Assem Barakat, Ayman El-Faham, Hessa H. Al-Rasheed, Kholoud Dahlous, Abdullah Mohammed Al-Majid, Anamika Sharma, Sammer Yousuf, Mehar Sanam, Zaheer Ul-Haq, M. Iqbal Choudhary, Beatriz G. de la Torre, Fernando Albericio
Barbituric acid (BA) derivatives have been reported to have potential anti-hypertensive13, anti-cancer14, anti-convulsant15, anti-inflammatory16, anti-psychotic17, and antitumor properties18–21. Recently, these derivatives have also been reported as anti-diabetic agents22. On the other hand, thiobarbituric acid (TBA) analogues has been described to exert anti-inflammatory16,23, immunotropic24, anticonvulsant25, and anti-hypnotic25,26, anti-neoplastic27, and antitumor activities28. De Belin et al.29 reported a number of TBA derivatives as inhibitors of hypoxia-inducible factor 1 (HIF-1). Recently, Barakat et al.30 described the synthesis of a new series of diethylammonium salts of aryl substituted TBA derivatives as α-glycosidase inhibitors. Therefore, given the relevance of TBA derivatives in medicinal chemistry, the design of new molecules containing the thiobarbituric moiety is an inspiring goal.