Mechanism of action of oral antidiabetic drugs. (1/3)The fall in blood sugar with carbutamide (BZ55) 24 hr. after the maintenance dose of insulin (28.1%+/-2.9 s.e) in rabbits made severely diabetic with alloxan was significantly different from the change in the blood sugar with the same drug given 72 hr. (6.8%+/-2.0) or distilled water given 24 hr. (7.7%+/-1.3) respectively after the last dose of insulin. It is postulated that the drug acts by liberating bound insulin in the plasma. (+info)
Characterization of acetohexamide reductases purified from rabbit liver, kidney, and heart: structural requirements for substrates and inhibitors. (2/3)The structural requirements of acetohexamide reductases purified from rabbit liver, kidney, and heart for substrates and inhibitors were examined. Acetohexamide, an oral antidiabetic drug with a ketone group, and analogs of it with various alkyl groups instead of the cyclohexyl group were used as substrates for these three enzymes. The results obtained as to substrate specificity suggested that the nature of the substrate-binding region of the heart enzyme is markedly different from those of the substrate-binding regions of the liver and kidney enzymes. Tolbutamide, which has no ketone group within its chemical structure, strongly inhibited the heart enzyme, whereas it had little ability to inhibit the liver or kidney enzyme. The inhibition of the heart enzyme by tolbutamide was competitive with respect to acetohexamide and uncompetitive with respect to NADPH. Furthermore, tolbutamide analogs with n-pentyl and n-hexyl groups instead of the n-butyl group exhibited very pronounced inhibition of only the heart enzyme. Therefore, it is reasonable to postulate that the heart enzyme, unlike the liver and kidney ones, has a cleft of a strongly hydrophobic nature near its substrate-binding region, and that this hydrophobic cleft plays a critical role in the interaction of the heart enzyme with the cyclohexyl group of acetohexamide. (+info)
Interaction of N-benzoyl-D-phenylalanine and related compounds with the sulphonylurea receptor of beta-cells. (3/3)1. The structure activity relationships for the insulin secretagogues N-benzoyl-D-phenylalanine (NBDP) and related compounds were examined at the sulphonylurea receptor level by use of cultured HIT-T15 and mouse pancreatic beta-cells. The affinities of these compounds for the sulphonylurea receptor were compared with their potencies for K(ATP)-channel inhibition. In addition, the effects of cytosolic nucleotides on K(ATP)-channel inhibition by NBDP were investigated. 2. NBDP displayed a dissociation constant for binding to the sulphonylurea receptor (K(D) value) of 11 microM and half-maximally effective concentrations of K(ATP)-channel inhibition (EC50 values) between 2 and 4 microM (in the absence of cytosolic nucleotides or presence of 0.1 mM GDP or 1 mM ADP). 3. In the absence of cytosolic nucleotides or presence of GDP (0.1 mM) maximally effective concentrations of NBDP (0.1-1 mM) reduced K(ATP)-channel activity to 47% and 44% of control, respectively. In the presence of ADP (1 mM), K(ATP)-channel activity was completely suppressed by 0.1 mM NBDP. 4. The L-isomer of N-benzoyl-phenylalanine displayed a 20 fold lower affinity and an 80 fold lower potency than the D-isomer. 5. Introduction of a p-nitro substituent in the D-phenylalanine moiety of NBDP did not decrease lipophilicity but lowered affinity and potency by more than 30 fold. 6. Introduction of a p-amino substituent in the D-phenylalanine moiety of NBDP (N-benzoyl-p-amino-D-phenylalanine, NBADP) reduced lipophilicity and lowered affinity and potency by about 10 fold. This loss of affinity and potency was compensated for by formation of the phenylpropionic acid derivative of NBADP. A similar difference in affinity was observed for the sulphonylurea carbutamide and its phenylpropionic acid derivative. 7. Replacing the benzene ring in the D-phenylalanine moiety of NBDP by a cyclohexyl ring increased lipophilicity, and the K(D) and EC50 values were slightly lower than for NBDP. Exchange of both benzene rings in NBDP by cyclohexyl rings further increased lipophilicity without altering affinity and potency. 8. This study shows that N-acylphenylalanines interact with the sulphonylurea receptor of pancreatic beta-cells in a stereospecific manner. Their potency depends on lipophilic but not aromatic properties of their benzene rings. As observed for sulphonylureas, interaction of N-acylphenylalanines with the sulphonylurea receptor does not induce complete inhibition of K(ATP)-channel activity in the absence of inhibitory cytosolic nucleotides. (+info)
... (brand name Glucidoral) is an anti-diabetic drug of the sulfonylurea class, developed by Servier. It is classified ...
Drugs and Cosmetics Rules, 1945
Examples of substances under this schedule: Testolactone, Hydroxyurea, Carbutamide, Primidone etc. Schedule H: The drug label ...
First-generation drugs include acetohexamide, carbutamide, chlorpropamide, glycyclamide (tolcyclamide), metahexamide, ...
Lilly pulled carbutamide and halted development, leaving the field open for Upjohn to market its new treatment. In 1956, Upjohn ... Upjohn discovered Eli Lilly had begun clinical trials for carbutamide, another oral hypoglycemic. Upjohn pushed for large-scale ...
Carbutamide (Glucidoral) Daflon 500 Fenspiride (Pneumorel) Fotemustine (Muphoran) Fusafungine (Locabiotal) Gliclazide ( ...
ATC code A10
A10BB01 Glibenclamide A10BB02 Chlorpropamide A10BB03 Tolbutamide A10BB04 Glibornuride A10BB05 Tolazamide A10BB06 Carbutamide ...
SIDE-EFFECTS IN THE ORAL TREATMENT OF DIABETES WITH SULFONYLUREAS] - PubMed
A quantum chemical study with special reference to the sulfamyl group of sulfonylureas - PubMed
Carbutamide Preferred Term Term UI T006531. Date01/01/1999. LexicalTag NON. ThesaurusID ... Carbutamide Preferred Concept UI. M0003414. Registry Number. E3K8P4869P. Related Numbers. 339-43-5. Scope Note. A sulfonylurea ... Carbutamide. Tree Number(s). D02.065.950.828.204. D02.886.590.795.204. Unique ID. D002271. RDF Unique Identifier. http://id.nlm ...
Drug Eruptions: Practice Essentials, Background, Pathophysiology
Carbutamide Preferred Term Term UI T006531. Date01/01/1999. LexicalTag NON. ThesaurusID ... Carbutamide Preferred Concept UI. M0003414. Registry Number. E3K8P4869P. Related Numbers. 339-43-5. Scope Note. A sulfonylurea ... Carbutamide. Tree Number(s). D02.065.884.060.010. D02.065.950.828.204. D02.455.426.559.389.085.010. D02.886.590.700.090.010. ...
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Oxcarbazepine - WikiProjectMed
Oxcarbazepine, sold under the brand name Trileptal among others, is a medication used to treat epilepsy and bipolar disorder. For epilepsy it is used for both focal seizures and generalized seizures. It has been used both alone and as add-on therapy in people with bipolar who have had no success with other treatments. It is taken by mouth. Common side effects include nausea, vomiting, dizziness, drowsiness, double vision and trouble with walking. Serious side effects may include anaphylaxis, liver problems, pancreatitis, suicide, and an abnormal heart beat. While use during pregnancy may harm the baby, use may be less risky than having a seizure. Use is not recommended during breastfeeding. In those with an allergy to carbamazepine there is a 25% risk of problems with oxcarbazepine. How it works is not entirely clear. Oxcarbazepine was patented in 1969 and came into medical use in 1990. It is available as a generic medication. A month supply in the ...
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Liver damage and estrogen therapy of prostatic cancer. Case report - PubMed
Liver damage and estrogen therapy of prostatic cancer. Case report - PubMed
Drug-Induced Bullous Disorders: Background, Pathophysiology, Etiology
- X. Binding of tolbutamide, chlorpropamide and carbutamide to human serum albumin, and the competition between tolbutamide or chlorpropamide and carbutamide or 4-sulfanilamido-2,6-dimethylpyrimidine for binding sites on human serum albumin. (nih.gov)