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Allopathic Medicines
Published in Varma H. Rambaran, Nalini K. Singh, Alternative Medicines for Diabetes Management, 2023
Varma H. Rambaran, Nalini K. Singh
The literature has shown that the use of tolbutamide has been associated with increased mortality in its patients (Sola et al. 2015, Riddle 2017). Douros et al. compiled several clinical and research studies concerning the association of sulfonylureas with the increased risk of cardiovascular events. They found that short-acting sulfonylureas – gliclazide, glipizide, and tolbutamide – could increase the risk of adverse cardiovascular events, compared to the long-acting sulfonylureas – glyburide and glimepiride (Douros, Yin et al. 2017). This greatly tarnished the reputation of sulfonylureas and they were derided as the drugs associated with cardiovascular mortality, while their counterpart, metformin was known to mitigate that risk (Douros, Yin et al. 2017).
Endocrine Disorders, Contraception, and Hormone Therapy during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
The frequency of congenital anomalies was not increased among 42 women who were treated with tolbutamide during pregnancy, but only 12 of these women had been treated during the first trimester. Several clinical series have suggested that the frequency of congenital anomalies among infants born to women who took tolbutamide in pregnancy is no greater than would be expected among infants of diabetic mothers (Coetzee and Jackson, 1984; Dolger et al., 1969; Notelovitz, 1971). Rat and mouse studies show no increase in congenital anomalies with tolbutamide until the doses are maternally toxic. Tolbutamide does not seem likely to cause birth defects in exposed infants, but this is based on fewer than 50 exposed infants.
Drugs Affecting the Endocrine System
Published in Radhwan Nidal Al-Zidan, Drugs in Pregnancy, 2020
Risk Summary: It should be used with caution during the 1st and 2nd Trimesters. However, it is better to avoid the use of Tolbutamide during the 3rd Trimester because fetal toxicity has been associated with its use during the last Trimester.
Aldehyde oxidase at the crossroad of metabolism and preclinical screening
Published in Drug Metabolism Reviews, 2019
Narges Cheshmazar, Siavoush Dastmalchi, Mineko Terao, Enrico Garattini, Maryam Hamzeh-Mivehroud
As for the AOX-dependent metabolism of aldehyde-containing xenobiotics, the number of therapeutic agents characterized by an aldehyde functional group is extremely limited. Nevertheless, AOX is deemed to play an important role in the metabolism of aldehyde intermediates generated from the oxidation of xenobiotics containing alcohol and amine groups by other drug-metabolizing enzymes. The following xenobiotics are examples of direct and indirect substrates whose aldehyde function is oxidized into the corresponding carboxylic acid by AOX. AOX metabolizes vitamin A into retinoic acid (Lakshmanan et al. 1964; Terao et al. 2009) via its retinaldehyde intermediate, which is generated by another enzyme-like alcohol dehydrogenase. Vitamin B6 is transformed by AOX into 4-pyridoxic acid (Stanulovic et al. 1976; Merrill and Henderson 1990). Tolbutamide, an anti-diabetic drug, is biotransformed to an aldehyde intermediate by a CYP450-dependent monoxygenase (CYP450) and/or an alcohol dehydrogenase. The aldehyde metabolite is subsequently oxidized into carboxytolbutamide by AOX (Mcdaniel et al. 1969). AOX oxidizes Tamoxifen, a well-known anti-estrogen used in the treatment of breast cancer, following transformation into an aldehyde intermediate by monoamine oxidase (MAO) (Kücükgöze and Leimkühler 2018). Citalopram is a selective serotonin reuptake inhibitor (SSRI), which is oxidized into an aldehyde intermediate by CYP450 subsequently biotransformed into the corresponding carboxylic acid by AOX (Rochat et al. 1998).
The role of sulfonylureas in the treatment of type 2 diabetes
Published in Expert Opinion on Pharmacotherapy, 2022
Brian Tomlinson, Nivritti Gajanan Patil, Manson Fok, Paul Chan, Christopher Wai Kei Lam
The UGDP study randomized 1027 people with T2D to treatment arms of diet (placebo), tolbutamide, fixed-dose insulin or variable-dose insulin therapy and another treatment arm of phenformin was added later so there were just over 200 patients in each group [85]. The study began in 1961, and the tolbutamide treatment arm was discontinued in 1969 because of a greater than twofold increase in the risk of cardiovascular mortality (26 cases or 12.7%) compared to the placebo (10 cases or 4.9%) or insulin treated patients. The phenformin arm was also stopped early in 1971 because of a similar excess of cardiovascular deaths compared to placebo [87], whereas the two insulin arms continued to completion in 1975 and showed no difference from placebo in cardiovascular outcomes [88].
Altered tolbutamide pharmacokinetics by a decrease in hepatic expression of CYP2C6/11 in rats pretreated with 5-fluorouracil
Published in Xenobiotica, 2018
Shuhei Fukuno, Katsuhito Nagai, Keita Kasahara, Yuki Mizobata, Sachiko Omotani, Yasutoshi Hatsuda, Michiaki Myotoku, Hiroki Konishi
Tolbutamide (TB) is a sulfonylurea derivative used in clinical practice as a hypoglycemic agent in the management of type 2 diabetes mellitus. TB is metabolized to 4-hydroxytolbutamide (4-OH-TB) by CYP2C6 and CYP2C11 in rats (Bogaards et al., 2000; Soucek & Gut, 1992), and by CYP2C9 in humans (Lee et al., 2003). The aim of the present study was to investigate whether the pharmacokinetic profile of TB is altered in response to the change in the hepatic metabolic capacity for TB by a single intraperitoneal administration of 5-FU using rats. In addition, the effects of 5-FU treatment on the hepatic expression of transcripts for CYP2C6 and CYP2C11 were also examined.