The Diabetes Pharmacology Ontology contains the classes needed to describe antihyperglycemic therapies.
A circumstance influencing the treatment of a disease through the use or recommendation of one or more drugs.
Therapy-related factors identified include: route of administration, treatment complexity, duration of treatment period, medication side effects, degree of behavioral change required, taste of medication and requirement for drug storage. [Definition Source: url:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2503662/ ]
A circumstance influencing the dianosis of a disease.
A biological, physiological, behavioral, or molecular indicator of the presence or predisposition towards development of a specific disease. [Definition Source: NCI]
The distinguishing qualities or prominent aspect of a person. [Definition Source: NCI]
An action or administration of therapeutic agents to produce an effect that is intended to alter or stop a pathologic process. [Definition Source: NCI]
A finding or categorization surmised from recorded measurements.
Annotation used to indicate the size or magnitude of something that was determined by comparison to a standard. [Definition Source: NCI]
A symptom is a perceived change in function, sensation, loss, disturbance or appearance reported by a patient indicative of a disease. [ url:https://link.springer.com/chapter/10.1007/978-1-4615-4789-1_5 url:https://www.nature.com/subjects/signs-and-symptoms url:https://www.merriam-webster.com/dictionary/symptom ][Definition Source: SYMP:0000462]
Nutrition Metabolism and Development Symptom
A symptom involving the nutrition, metabolism, and/or development system.
Symptoms concerning nutrition metabolism and development [include:] A disorder characterized by a loss of appetite; An abnormal loss of the appetite for food. Anorexia can be caused by cancer, aids, a mental disorder (i.e., anorexia nervosa), or other diseases; Clinical manifestation consisting of a physiopathological lack or loss of appetite accompanied by an aversion to food and the inability to eat; Loss of appetite; The lack or loss of appetite accompanied by an aversion to food and the inability to eat. It is the defining characteristic of the disorder anorexia nervosa. [Definition Source: url:http://www.icd9data.com/2013/Volume1/780-799/780-789/783/default.htm ]
Polydipsia is a nutrition, metabolism, and development symptom characterized by an excessive or abnormal thirst. [ url:http://www2.merriam-webster.com/cgi-bin/mwmednlm?book=Medical&va=polydipsia ][Definition Source: SYMP:0000560]
Polyphagia is a nutrition, metabolism, and development symptom characterized by an excessive appetite or eating. [ url:http://www2.merriam-webster.com/cgi-bin/mwmednlm?book=Medical&va=polyphagia ][Definition Source: SYMP:0000524]
The result of a body mass index measurement. [Definition Source: NCI]
A quantitative measurement for assessing the amount of glucose present in a blood sample. [Definition Source: NCI]
The determination of the amount of total cholesterol present in a sample. [Definition Source: NCI]
A quantitative measurement of the amount of triglyceride present in a sample. [Definition Source: NCI]
The quantification of weight/height relationships below a certain threshold that classes an individual as underweight. This threshold may vary based on an individual's ethnicity but is commonly considered in European populations to correspond to a BMI < 18. [Definition Source: EFO:0005936]
BMI greater than or equal to 18.5 to 24.9 kg/m^2 [Definition Source: url:https://www.ncbi.nlm.nih.gov/books/NBK541070/ ]
The quantification of weight/height relationships above a certain threshold that classes an individual as overweight. This threshold may vary based on an individual's ethnicity but is commonly considered to correspond in European populations to a 25<BMI<30. [Definition Source: EFO:0005935]
Having a high amount of body fat (body mass index [BMI] of 30 or more). [Definition Source: NCI]
The quantification of weight/height relationships above a certain threshold that classes an individual as overweight. This threshold may vary based on an individual's ethnicity but is commonly considered to correspond in European populations to a BMI > 30. [Definition Source: EFO:0007041]
FPG 100 mg/dL (5.6 mmol/L) to 125 mg/dL (6.9 mmol/L). [Definition Source: url:https://doi.org/10.2337/dc22-S002 ]
FPG ≥126 mg/dL (7.0 mmol/L). [Definition Source: url:https://doi.org/10.2337/dc22-S002 ]
Prediabetes Two Hour Blood Glucose Level
2-h PG during 75-g OGTT 140 mg/dL (7.8 mmol/L) to 199 mg/dL (11.0 mmol/L). [Definition Source: url:https://doi.org/10.2337/dc22-S002 ]
Prediabetes Two Hour Blood Glucose Range
2-h PG ≥200 mg/dL (11.1 mmol/L) during OGTT. [Definition Source: url:https://doi.org/10.2337/dc22-S002 ]
A1C 5.7–6.4% (39–47 mmol/mol). [Definition Source: url:https://doi.org/10.2337/dc22-S002 ]
A1C ≥6.5% (48 mmol/mol). [Definition Source: url:https://doi.org/10.2337/dc22-S002 ]
Symptoms of urinary disorders vary from person to person and based on the cause of the disorders. Common urinary symptoms include: Abdominal cramping; Abdominal, pelvic or back pain that can be severe; Bloody or pink-colored urine (hematuria); Cloudy urine; Fever and chills; Foul-smelling urine; Frequent urination; General ill feeling; Leaking of urine; Pain during sexual intercourse; Pain or burning with urination (dysuria); Unexplained weight loss; Urgent need to urinate. [Definition Source: url:https://www.healthgrades.com/right-care/kidneys-and-the-urinary-system/urinary-disorders ]
A urinary system symptom that is characterized by the excessive secretion of urine. [ url:http://www2.merriam-webster.com/cgi-bin/mwmednlm?book=Medical&va=polyuria ][Definition Source: SYMP:0000565]
A urinary system symptom that is characterized by the difficult, or painful, discharge of urine. [ url:http://www2.merriam-webster.com/cgi-bin/mwmednlm?book=Medical&va=dysuria ][Definition Source: SYMP:0000485]
A bacterial infectious process affecting any part of the urinary tract, most commonly the bladder and the urethra. Symptoms include urinary urgency and frequency, burning sensation during urination, lower abdominal discomfort, and cloudy urine. [Definition Source: NCI]
Increased frequency of urination. [Definition Source: HP:0100515]
A deviation from the normal odor of the urine. [Definition Source: HP:0012088]
A vision symptom that is characterized by a decreased clarity or sharpness in vision, which can be caused by eye conditions myopia or hyperopia. [Definition Source: SYMP:0000012]
Fatigue is a neurological and physiological symptom characterized by a weariness or exhaustion from labor, exertion, or stress. [ url:http://www2.merriam-webster.com/cgi-bin/mwmednlm?book=Medical&va=fatigue ][Definition Source: SYMP:0019177]
A symptom involving the musculoskeletal system.
Musculoskeletal symptoms are defined as pain in the muscles, tendons, and nerves arising from repetitive, continuous, and unnatural movements. These symptoms can be expressed in various areas of the body and affect the quality of life by causing difficulties in performing occupational tasks and activities of daily living (ADL). [Definition Source: url:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3567324/ ]
Arthritis is a musculoskeletal system symptom characterized as an inflammation of joints due to infectious, metabolic, or constitutional causes. [ url:http://www2.merriam-webster.com/cgi-bin/mwmednlm?book=Medical&va=arthritis ][Definition Source: SYMP:0019169]
Peripheral neuropathy refers to the many conditions that involve damage to the peripheral nervous system, the vast communication network that sends signals between the central nervous system (the brain and spinal cord) and all other parts of the body. [Definition Source: url:https://www.ninds.nih.gov/peripheral-neuropathy-fact-sheet ]
A state of being, such as a state of health. [Definition Source: NCI]
Elevated levels of lipids in the blood. [Definition Source: NCI]
Blood pressure that is abnormally high. [Definition Source: NCI]
The aggregate of past events; the continuum of events occurring in succession leading from the past to the present; a record or narrative description of past events. [Definition Source: NCI]
A record of a patient's background regarding health and disease events of blood relatives. A patient's family medical history may be important in diagnosing existing conditions. [Definition Source: NCI]
A record of a patient's background regarding health and the occurrence of disease events of the individual. In addition, personal medical history may be a variable in epidemiologic studies. [Definition Source: NCI]
Family History of Coronary Artery Disease
History of a first-degree relative (less than 55 years for male relatives or less than 65 years for female relatives) having had any of the following: coronary artery disease, myocardial infarction, coronary artery bypass graft surgery, percutaneous coronary intervention, or sudden cardiac death without obvious cause. [Definition Source: NCI]
Having at least one-first-degree relative with diabetes. [Definition Source: url:https://doi.org/10.1111/jdi.12033 ]
Personal History of Gestational Diabetes
Gestational diabetes mellitus (GDM), defined as glucose intolerance that is first recognized during pregnancy, is associated with maternal obesity and confers a 4‐ to 7‐fold greater risk of incident type 2 diabetes (DM), and increased risk of developing the metabolic syndrome (MetS) in midlife. In addition, a history of GDM among nondiabetic women is characterized by elevations in fasting glucose and insulin concentrations, as well as dyslipidemia and greater inflammation in the absence of the MetS. [Definition Source: url:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4187501/ ]
Febrile seizures are defined as events in infancy or childhood that usually occur between three months and five years of age and are associated with a fever, but without evidence of intracranial infection or a defined cause for the seizure. [Definition Source: url:https://www.aafp.org/pubs/afp/issues/2008/1115/p1199.html ]
Bilateral Lower Extremity Burning Sensation
Occasional Burning Sensation in Bilateral Lower Extremities
Any abnormal condition of the body or mind that causes discomfort, dysfunction, or distress to the person affected or those in contact with the person. The term is often used broadly to include injuries, disabilities, syndromes, symptoms, deviant behaviors, and atypical variations of structure and function. [Definition Source: NCI]
Narrowing of the coronary arteries due to fatty deposits inside the arterial walls. The diagnostic criteria may include documented history of any of the following: documented coronary artery stenosis greater than or equal to 50% (by cardiac catheterization or other modality of direct imaging of the coronary arteries); previous coronary artery bypass surgery (CABG); previous percutaneous coronary intervention (PCI); previous myocardial infarction. (ACC) [Definition Source: NCI]
A metabolic disorder characterized by abnormally high blood sugar levels due to diminished production of insulin or insulin resistance/desensitization. [Definition Source: NCI]
Disease associated with kidneys, typically chronic kidney disease.
A neoplastic or non-neoplastic condition affecting the kidney. Representative examples of non-neoplastic conditions include glomerulonephritis and nephrotic syndrome. Representative examples of neoplastic conditions include benign processes (e.g., renal lipoma and renal fibroma) and malignant processes (e.g., renal cell carcinoma and renal lymphoma). [Definition Source: NCI]
A non-neoplastic or neoplastic disorder affecting the heart or the vessels (arteries, veins and lymph vessels). Representative examples of non-neoplastic cardiovascular disorders are endocarditis and hypertension. Representative examples of neoplastic cardiovascular disorders are endocardial myxoma and angiosarcoma. [Definition Source: NCI]
A sudden loss of neurological function secondary to hemorrhage or ischemia in the brain parenchyma due to a vascular event. [Definition Source: NCI]
Stroke is a nervous system symptom characterized by a sudden diminution or loss of consciousness, sensation, and voluntary motion caused by rupture or obstruction (as by a clot) of a blood vessel of the brain. [ url:http://www2.merriam-webster.com/cgi-bin/mwmednlm?book=Medical&va=stroke ][Definition Source: SYMP:0000734]
A sensation perception where there is an unpleasant sensation that usually indicates the body is threatened or damaged. The sensation may be sharp or dull, short-lived or chronic, intermittent or continual, confined to one area or spread over the entire body. [ url:http://www.nationalpainfoundation.org/MyTreatment/articles/Cancer_PainDefinitions.asp ][Definition Source: SYMP:0000576]
An unpleasant sensation characterized by physical discomfort (such as pricking, throbbing, or aching) localized to the chest. [Definition Source: HP:0100749]
The actions or reactions of an object or organism, usually in relation to the environment or surrounding world of stimuli. [Definition Source: NCI]
A type of lifestyle that lacks physical exercise, characterized by sitting, reading, watching television or using a computer for much of the day without vigorous physical exertion. [Definition Source: NCI]
A description of an individual's current and past experience with alcoholic beverage consumption. [Definition Source: NCI]
A description of an individual's current and past use and/or abuse of drugs and chemicals. This includes prescription medication, illicit drugs and recreational substances. [Definition Source: NCI]
The principal activity that a person does to earn money. [Definition Source: NCI]
A physical demand level described as the exertion of up to 10 pounds of force occasionally, negligible amount of work frequently, and a negligible amount of force constantly to move objects. [Definition Source: url:https://medical-dictionary.thefreedictionary.com/sedentary+work ]
Treatment designed to lower blood sugar levels.
A drug which lowers the blood glucose level. [Definition Source: CHEBI]
The probability of benefit to individuals in a defined population from a medical technology applied for a given medical problem under ideal conditions of use. Efficacy is a measure of effect of therapy among appropriate patients in whom treatment is tolerated and effectively administered, under the condition of sufficient patients' compliance, usually determined in randomized trials. [Definition Source: NCI]
A high capacity to bring about a desired effect.
An intermediate capacity to bring about a desired effect.
A low capacity to bring about a desired effect.
The lack of expected or desired effect related to a therapy. [Definition Source: NCI]
The capacity for an increase or decrease in the weight of an individual.
The capacity for a decrease in the weight of an individual.
The capacity for an increase in the weight of an individual.
The lack of an effect on the capacity for an increase or decrease in the weight of an individual.
The possiblility of lowering blood sugar below the normal range.
The most important risk factor for the occurrence of hypoglycemia is the aggressiveness of therapy applied to achieve glycemic control. [Definition Source: url:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3784865/ ]
No known association with the lowering of blood sugar below the normal range.
A known association with the lowering of blood sugar below the normal range.
A pharmacotherapy factor related to the heart or blood vessels.
Cardiovascular effects are defined as any uncomfortable physical effect that relates to the heart and blood vessels. [Definition Source: url:https://effectindex.com/categories/cardiovascular-effects ]
Atherosclerotic Cardiovascular Disease Risk
Risk of cardiovascular disease resulting from atherosclerosis.
Potential to reduce the risk of cardiovascular disease resulting from atherosclerosis.
Potential to increase the risk of cardiovascular disease resulting from atherosclerosis.
Minimal effect on reducing or increasing the risk of cardiovascular disease resulting from atherosclerosis.
Potential to decrease the risk of heart failure.
Potential to increase the risk of heart failure.
Minimal effect on reducing or increasing the risk of heart failure.
The amount paid, charged, or engaged to be paid, for purchasing goods, services and financial instruments. [Definition Source: NCI]
A pharmacotherapy factor related to the kidneys.
The progression of diabetic kidney disease.
Defined by the presence of diabetes and reduced estimated glomerular filtration rate (eGFR) to <60/ mL/min/1.73 m2, increased albuminuria (>300 mg/24 hours) or both, diabetic kidney disease (DKD) is a progressive disease that affects one in seven individuals worldwide eventuating renal replacement therapy (RRT) and premature death secondary to cardiovascular causes. [Definition Source: url:https://www.ncbi.nlm.nih.gov/books/NBK571719/ ]
Drug dosage considerations related to the effect on the kidneys.
Potential Diabetic Kidney Disease Benefit
Potential to decrease the risk or progression of diabetic kidney disease.
Potential to increase the risk or progression of diabetic kidney disease.
Minimal effect on reducing or increasing the risk or progression of diabetic kidney disease.
Any antidiabetic agent with the biguanide base structure or phenformin derivatives with antihyperglycemic activity. Biguanide antidiabetic agents activate AMP-activated protein kinase (AMPK) resulting in decreased glucose production in the liver, increased peripheral glucose uptake and improved utilization of glucose. Biguanide-based antidiabetic agents do not cause hypoglycemia. In addition, biguanide antidiabetics decrease absorption of glucose from the gastrointestinal tract. [Definition Source: NCI]
An agent belonging to the biguanide class of antidiabetics with antihyperglycemic activity. Metformin is associated with a very low incidence of lactic acidosis. This agent helps reduce LDL cholesterol and triglyceride levels, and is not associated with weight gain, and prevents the cardiovascular complications of diabetes. Metformin is not metabolized and is excreted unchanged by the kidneys. [Definition Source: NCI]
Any inhibitor of the sodium-glucose co-transporter subtype 2 (SGLT2) with antihyperglycemic activity. By binding to and blocking SGLT2, these inhibitors suppress reabsorption of glucose in the proximal tubule within the kidneys and thereby enhancing urinary excretion of glucose. This eventually normalizes blood glucose levels. SGLT2, a transport system exclusively expressed in the proximal renal tubules, mediates about 90% of renal glucose reabsorption from tubular fluid. [Definition Source: NCI]
An orally available competitive inhibitor of sodium-glucose co-transporter 2 (SGLT2; SLC5A2) with antihyperglycemic activity. Upon oral administration, empagliflozin selectively and potently inhibits SGLT2 in the kidneys, thereby suppressing the reabsorption of glucose in the proximal tubule. Inhibition of SGLT2 increases urinary glucose excretion by the kidneys, resulting in a reduction of plasma glucose levels in an insulin-independent manner. Inhibition of SGLT2 in the kidneys also suppresses the renal reabsorption of 1,5-anhydroglucitol (1,5AG). This lowers serum 1,5AG and neutrophil 1,5-anhydroglucitol-6-phosphate (1,5AG6P) levels, which may improve neutropenia and neutrophil dysfunction in patients with glycogen storage disease type Ib (GSD Ib). SGLT2, a transport protein exclusively expressed in the proximal renal tubules, mediates approximately 90% of renal glucose reabsorption from tubular fluid. [Definition Source: NCI]
A C-glucoside with a thiophene ring that is an orally available inhibitor of sodium-glucose transporter 2 (SGLT2) with antihyperglycemic activity. Canagliflozin is also able to reduce body weight and has a low risk for hypoglycemia. [Definition Source: NCI]
A selective sodium-glucose co-transporter subtype 2 (SGLT2) inhibitor with antihyperglycemic activity. Dapagliflozin selectively and potently inhibits SGLT2 compared to SGLT1, which is the cotransporter of glucose in the gut. [Definition Source: NCI]
Ertugliflozin is in a class of medications called sodium-glucose co-transporter 2 (SGLT2) inhibitors. It lowers blood sugar by causing the kidneys to get rid of more glucose in the urine. Ertugliflozin is not used to treat type 1 diabetes (condition in which the body does not produce insulin and, therefore, cannot control the amount of sugar in the blood) or diabetic ketoacidosis (a serious condition that may develop if high blood sugar is not treated). [Definition Source: https://medlineplus.gov/druginfo/meds/a618011.html]
Any of the analogues of the endogenous gastrointestinal hormone glucagon-like peptide-1 (GLP-1) with antihyperglycemic activity. GLP-1 mimetics mimic the activity of GLP-1 and thereby stimulate glucose-dependent secretion of insulin from pancreatic beta cells, suppress glucagon secretion from alpha cells, increase insulin sensitivity and inhibit gastric emptying thereby slowing absorption of nutrients and creating a satiating effect. Altogether, this lowers blood glucose levels. GLP-1 is rapidly inactivated by the enzyme dipeptidyl peptidase-4 (DPP-4). [Definition Source: NCI]
An agonist that binds to and activates glucagon-like peptide-1 (GLP-1) receptors. [Definition Source: CHEBI]
A glucagon-like peptide-1 (GLP-1) receptor agonist that is 90% homologous to native human GLP-1 (7-37) and is composed of a dipeptidyl peptidase-IV-protected GLP-1 analog covalently linked to a human immunoglobulin G4 (IgG4)-Fc heavy chain, with antihyperglycemic activity. Upon administration, dulaglutide binds to and activates GLP-1 receptors, thereby increasing intracellular cyclic AMP (cAMP) in pancreatic beta cells. This increases glucose-dependent insulin release. Dulaglutide also reduces the elevated glucagon secretion by inhibiting alpha cells of the pancreas and slows gastric emptying. Altogether this lowers the postprandial glucose level. GLP-1 is normally secreted by L cells of the gastrointestinal (GI) mucosa in response to a meal to normalize blood glucose levels. [Definition Source: NCI]
A long-acting, fatty acylated glucagon-like peptide-1 (GLP-1) analog administered subcutaneously, with antihyperglycemic activity. Liraglutide's prolonged action and half-life of 11-15 hours are attributed to the attachment of the fatty acid palmitic acid to GLP-1 that reversibly binds to albumin. Albumin binding protects liraglutide from immediate degradation and elimination and causes GLP-1 to be released from abumin in a slow and consistent manner. This agent may cause thyroid C-cell tumors and increases the risk of acute pancreatitis. [Definition Source: NCI]
A polypeptide that contains a linear sequence of 31 amino acids joined together by peptide linkages. It is an agonist of glucagon-like peptide-1 receptors (GLP-1 AR) and used for the treatment of type 2 diabetes. [Definition Source: CHEBI]
A forty-four membered polypeptide consisting of L-His, Gly, L-Glu, Gly, L-Thr, L-Phe, L-Thr, L-Ser, L-Asp, L-Leu, L-Ser, L-Lys, L-Gln, L-Met, L-Glu, L-Glu, L-Glu, L-Ala, L-Val, L-Arg, L-Leu, L-Phe, L-Ile, L-Glu, L-Trp, L-Leu, L-Lys, L-Asn, Gly, Gly, LPro, L-Ser, L-Ser, Gly, L-Ala, L-Pro, L-Pro, L-Ser, L-Lys, L-Lys, L-Lys, L-Lys, L-Lys, and L-Lys-NH2 residues joined in sequence. Used as an adjunct to diet and exercise for the treatment of adults with type II diabetes. [Definition Source: CHEBI]
A 39 amino acid peptide and synthetic version of exendin-4, a hormone found in the saliva of the venomous lizard Gila monster, with insulin secretagogue and antihyperglycemic activity. Exenatide is administered subcutaneously and mimics human glucagon-like peptide-1 (GLP-1). Compared to GLP-1, exenatide has a longer half-life of 2.4 hours. [Definition Source: NCI]
A bioactive polypeptide of 39 amino acid residues isolated from the saliva of the Gila monster (Heloderma suspectum). High-affinity glucagon-like peptide 1 (GLP-1) receptor agonist (Kd = 136 pM); potently induces cAMP formation without stimulating amylase release in pancreatic acini; potentiates glucose-induced insulin secretion in isolated rat islets; protects against glutamate-induced neurotoxicity. A synthetic version is called exenatide. [Definition Source: CHEBI]
Any inhibitor of the proline-specific serine protease dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity. DPP-4 inhibitors bind to DPP-4 and inhibit the breakdown of the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). This prolongs incretin activity, increases postprandial insulin release, decreases glucagon release, delays gastric emptying and lowers blood glucose levels. The risk for hypoglycemia is negligible with the use of DPP-4 inhibitors. [Definition Source: NCI]
An EC 3.4.14.* (dipeptidyl- and tripeptidyl-peptidases) inhibitor that specifically inhibits dipeptidyl peptidase-4 (EC 3.4.14.5). [Definition Source: CHEBI]
An orally available, competitive, beta-amino acid-derived inhibitor of dipeptidyl peptidase 4 (DDP-4) with hypoglycemic activity. Sitagliptin may cause an increased risk in the development of pancreatitis. [Definition Source: NCI]
A potent, selective and competitive, cyanopyrrolidine-based, orally bioavailable inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity. Saxagliptin is metabolized into an, although less potent, active mono-hydroxy metabolite. [Definition Source: NCI]
A monocarboxylic acid amide obtained by formal condensation of the carboxy group of (2S)-amino(3-hydroxyadamantan-1-yl)acetic acid with the amino group of (1S,3S,5S)-2-azabicyclo[3.1.0]hexane-3-carbonitrile. Used in its monohydrate form for the treatment of Type II diabetes. [Definition Source: CHEBI]
A selective, orally bioavailable, pyrimidinedione-based inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity. In addition to its effect on glucose levels, alogliptin may inhibit inflammatory responses by preventing the toll-like receptor 4 (TLR-4)-mediated formation of proinflammatory cytokines. [Definition Source: NCI]
A piperidine that is 3-methyl-2,4-dioxo-3,4-dihydropyrimidine carrying additional 2-cyanobenzyl and 3-aminopiperidin-1-yl groups at positions 1 and 2 respectively (the R-enantiomer). Used in the form of its benzoate salt for treatment of type 2 diabetes. [Definition Source: CHEBI]
A potent, orally bioavailable dihydropurinedione-based inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity. The inhibition of DPP-4 by linagliptin appears to be longer lasting than that by some other DPP-4 inhibitors tested. [Definition Source: NCI]
A xanthine that is 7H-xanthine bearing (4-methylquinazolin-2-yl)methyl, methyl, but-2-yn-1-yl and 3-aminopiperidin-1-yl substituents at positions 1, 3, 7 and 8 respectively (the R-enantiomer). Used for treatment of type II diabetes. [Definition Source: CHEBI]
Any antidiabetic agent with the glitazone (thiazolidinedione) base structure with antihyperglycemic activity. Glitazone antidiabetic agents selectively bind to and stimulate the nuclear receptor peroxisome proliferator-activated receptor (PPAR) gamma. This results in the selective transcription of a number of insulin-sensitive genes involved in glucose metabolism. This eventually enhances insulin sensitivity, reduces insulin resistance and decreases hepatic gluconeogenesis. PPARs function as transcription factors that regulate expressions of genes involved in cellular differentiation, development, and metabolism (carbohydrate, lipid, protein), as well as tumorigenesis; PPARgamma is expressed at high levels in adipose tissue. [Definition Source: NCI]
An orally-active thiazolidinedione with antidiabetic properties and potential antineoplastic activity. Pioglitazone activates peroxisome proliferator-activated receptor gamma (PPAR-gamma), a ligand-activated transcription factor, thereby inducing cell differentiation and inhibiting cell growth and angiogenesis. This agent also modulates the transcription of insulin-responsive genes, inhibits macrophage and monocyte activation, and stimulates adipocyte differentiation. [Definition Source: NCI]
A member of the class of thiazolidenediones that is 1,3-thiazolidine-2,4-dione substituted by a benzyl group at position 5 which in turn is substituted by a 2-(5-ethylpyridin-2-yl)ethoxy group at position 4 of the phenyl ring. It exhibits hypoglycemic activity. [Definition Source: CHEBI]
An agent belonging to the glitazone class of antidiabetic agents with antihyperglycemic and anti-inflammatory activities. In addition to its selective affinity for peroxisome proliferator-activated receptor (PPAR) gamma and its ability to lower blood glucose levels, rosiglitazone also exerts anti-inflammatory activity through its ability to inhibit nuclear factor-kappaB (NF-KB) activity and increase I-kappaB levels. In addition, rosiglitazone may cause fluid retention and may worsen congestive heart failure. This agent is also associated with an increased risk of heart attacks. [Definition Source: NCI]
Sulfonamide urea derivatives with antihyperglycemic activity. Sulphonylurea antidiabetic agents bind to sulfonylurea receptor type 1 (SUR1), the subunit of ATP-sensitive inwardly-rectifier potassium (IKATP) channels on the membranes of pancreatic beta cells, thereby blocking the inward current flow (influx) of positively charged K+ ions into the cell. This results in tonic membrane depolarization, and induces a calcium ion influx through voltage-sensitive calcium channels; increased intracellular calcium ion levels trigger exocytosis of insulin-containing granules. This eventually induces secretion of insulin. The IKATP channels found in pancreatic islets are complexes of four IKATP 6.2 and four SUR1 subunits. In addition, some sulfonylureas of larger molecular size may increase the sensitivity of peripheral tissues to insulin mediated through peroxisome proliferator-activated receptor gamma (PPARgamma). [Definition Source: NCI]
A sulfonamide urea derivative with antihyperglycemic activity that can potentially be used to decrease cerebral edema. Upon administration, glyburide binds to and blocks the sulfonylurea receptor type 1 (SUR1) subunit of the ATP-sensitive inwardly-rectifying potassium (K(ATP)) channels on the membranes of pancreatic beta cells. This prevents the inward current flow of positively charged potassium (K+) ions into the cell, and induces a calcium ion (Ca2+) influx through voltage-sensitive calcium channels, which triggers exocytosis of insulin-containing granules. In addition, glyburide also inhibits the SUR1-regulated nonselective cation (NC) Ca-ATP channel, melastatin 4 (transient receptor potential cation channel subfamily M member 4; (TRPM4)), thereby preventing capillary failure and brain swelling. SUR1-TRPM4 channels are formed by co-assembly of SUR1 with TRPM4 in neurons, astrocytes, and capillary endothelium during cerebral ischemia. Upon ischemia-induced ATP depletion, channels open which results in sodium influx, cytotoxic edema formation, capillary fragmentation and necrotic cell death. SUR1-TRPM4 is not expressed in normal, uninjured tissues. [Definition Source: NCI]
An N-sulfonylurea that is acetohexamide in which the acetyl group is replaced by a 2-(5-chloro-2-methoxybenzamido)ethyl group. [Definition Source: CHEBI]
A short-acting, second-generation sulfonylurea with hypoglycemic activity. Glipizide is rapidly absorbed, has a very quick onset of action and a short half-life. This agent is extensively metabolized in the liver and the metabolites as well as the unchanged form are excreted in the urine. [Definition Source: NCI]
An N-sulfonylurea that is glyburide in which the (5-chloro-2-methoxybenzoyl group is replaced by a (5-methylpyrazin-2-yl)carbonyl group. An oral hypoglycemic agent, it is used in the treatment of type 2 diabetes mellitus. [Definition Source: CHEBI]
A long-acting, third-generation sulfonylurea with hypoglycemic activity. Compared to other generations of sulfonylurea compounds, glimepiride is very potent and has a longer duration of action. This agent is metabolized by CYP2C9 and shows peroxisome proliferator-activated receptor gamma (PPARgamma) agonistic activity. [Definition Source: NCI]
nutrition, metabolism, and development symptom
Abnormal Blood Chemistry and Hematology Test Result
Non-Neoplastic Endocrine Pancreas Disorder
sodium-glucose transport protein subtype 2 inhibitor
glucagon-like peptide-1 receptor agonist
EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor
metFORMIN [Moles/volume] in Serum or Plasma
Fasting glucose [Mass/volume] in Serum or Plasma
Glucose [Mass/volume] in Serum or Plasma --2 hours post 75 g glucose PO
Hemoglobin A1c/Hemoglobin.total in Blood by IFCC protocol
Cholesterol in LDL [Mass/volume] in Serum or Plasma
Triglyceride [Mass/volume] in Body fluid