Name Glyburide

Accession DB01016 (APRD00233)

Number

Type Small Molecule

Groups Approved

Description Glyburide is an oral antihyperglycemic agent used for the treatmen

class of insulin secretagogues, which act by stimulating β cells of t
and meal-stimulated insulin release. Medications in this class differ
site on their target pancreatic β cell receptor. Sulfonylureas also in
increase the number and sensitivity of insulin receptors. Sulfonylur
mechanism of action, sulfonylureas may cause hypoglycemia and r
increased in elderly, debilitated and malnourished individuals. Glyb
glucose and glycosolated hemoglobin (HbA1c) levels (reflective of t
metabolized, likely in the liver. Although its metabolites exert a sma
thought to be clinically unimportant. Glyburide metabolites are exc
glyburide appears to be unaffected in those with a creatinine clear

Synonyms 1-((P-(2-(5-chloro-O-Anisamido)ethyl)phenyl)sulfonyl)-3-cyclohexylurea

International
Brands
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Name

Daonil
Delmide
Micronase
Novo-Glyburide
Semi-Daonil
Brand mixtures

Show entries

Name

Glucovance

Glyburide (micronized) and Metformin Hydrochloride

Glyburide and Metformin

Glyburide and Metformin Hydrochloride

Glyburide-metformin Hydrochloride

Categories
 Hypoglycemic Agents

 Anti-Arrhythmia Agents

 Antidiabetic Agents

 Drugs Used in Diabetes

 Alimentary Tract and Metabolism

  Blood Glucose Lowering Drugs, Excl. Insulins

 Sulfonylureas

 Cytochrome P-450 CYP2C9 Inhibitors

 Cytochrome P-450 CYP2C9 Inducers

 Cytochrome P-450 CYP2C19 Inducers

 CYP3A4 Inhibitors

 BSEP/ABCB11 Inhibitors

 Combined Inhibitors of CYP3A4 and P-glycoprotein

Indication
Indicated as an adjunct to diet to lower the blood glucose in pat
alone.

Pharmacodynam
ics Glyburide, a second-generation sulfonylurea antidiabetic agent,
pancreas, an effect dependent upon functioning beta cells in
blood glucose lowering effect persists despite a gradual decl
involved in the mechanism of action of oral sulfonyl-urea hypo
synergistic effect, since both agents act to improve glucose t
glucose lowering actions, glyburide produces a mild diuresis
related second-generation agent glipizide.

Mechanism of
action Sulfonylureas such as glyburide bind to ATP-sensitive potassium
causing depolarization of the membrane. Depolarization stimu
intracellular concentrations of calcium ions, which induces th

Absorption
Significant absorption within 1 hour and peak plasma levels are
Volume of
distribution Steady state Vd=0.125 L/kg; Vd during elimination phase=0.155 L

Protein binding
Unchanged drug is ~99% bound to serum proteins; 4-trans-hydro
primarily nonionic making glyburide and is less likely to displ

Metabolism
Primarily hepatic (mainly cytochrome P450 3A4). The major met
derivative, also occurs. These metabolites do not contribute c
however, retention of 4-trans-hydroxyglyburide may prolong th

Route of
elimination Glyburide is excreted as metabolites in the bile and urine, appro
from that of other sulfonylureas, which are excreted primarily

Half life
1.4-1.8 hours (unchanged drug only); 10 hours (metabolites inclu

Clearance
78 ml/hr/kg in healthy adults. Clearance may be substantially dec

Toxicity
Oral rat LD50: > 20,000 mg/kg. Oral mouse LD50: 3250 mg/kg.

Affected
organisms  Humans and other mammals

Drug
Interactions
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Drug

Acetohexamide Acetohexamide may increase the hypoglycemic activit

Acetylsalicylic acid Acetylsalicylic acid may increase the hypoglycemic ac
 Drug
Alogliptin Alogliptin may increase the hypoglycemic activities of
Amitriptyline Amitriptyline may increase the hypoglycemic activitie
Amodiaquine The serum concentration of Amodiaquine can be increa
Aripiprazole The therapeutic efficacy of Glyburide can be decreased
Arsenic trioxide The therapeutic efficacy of Glyburide can be decreased
Articaine The therapeutic efficacy of Glyburide can be decreased
Asenapine The therapeutic efficacy of Glyburide can be decreased
Atazanavir The therapeutic efficacy of Glyburide can be decreased

Food
Interactions  Avoid alcohol.

 Take 30-60 minutes before breakfast.

Name METFORMIN

Accession DB00331 (APRD01099)

Number

Type Small Molecule

Groups Approved

Description Metformin is a biguanide antihyperglycemic agent used for treating

by decreasing hepatic glucose production, decreasing glucose abso
weight loss and is the drug of choice for obese NIDDMpatients. Use
does not cause hypoglycemia; however, it may potentiate the hypog
nausea and diarrhea. Dose titration and/or use of smaller divided do
compromised renal function (creatinine clearance < 30 ml/min), acu
of iodinated contrast dyes due to the risk of lactic acidosis. Lower
Metformin decreases fasting plasma glucose, postprandial blood gl
8-10 weeks of glucose control. Metformin may also have a positive
 hydrochloride was marketed under the name Jentadueto for use in

Synonyms 1,1-Dimethylbiguanide
Dimethylbiguanid

Prescription
Products
Show entries

Name Dosage

Act Metformin tablet

Act Metformin tablet

Auro-metformin tablet

Auro-metformin tablet

Ava-metformin tablet

Ava-metformin tablet

Bci Metformin tablet

Bci Metformin tablet

Bio-metformin tablet

Bio-metformin tablet

Brand mixtures

Show entries

Name

Actoplus Met
Name

Actoplus Met XR

Appformin

Appformin-D

Avandamet

Glipizide and Metformin HCl

Glipizide and Metformin Hydrochloride

Glucovance
 Name

Glyburide (micronized) and Metformin Hydrochloride

Glyburide and Metformin

Indication For use as an adjunct to diet and exercise in adult patients (18 year
reproductive abnormalities associated with polycystic ovary syndro
andMETFORMIN is appropriate.

Pharmacodynam Metformin is an oral antihyperglycemic agent that improves glucos

ics glucose. Metformin is not chemically or pharmacologically related t
does not produce hypoglycemia in either patients with NIDDM or he
insulin secretion.

Mechanism of METFORMIN'S mechanisms of action differ from other classes of o

action decreasing hepatic glucose production, decreasing intestinal absor
uptake and utilization. These effects are mediated by the initial act
plays an important role in insulin signaling, whole body energy bala
metformin's inhibitory effect on the production of glucose by liver c
binding to insulin receptors. Metformin administration also increase
the plasma membrane, resulting in insulin-independent glucose upt
uptake of serum lactate, one of the substrates of gluconeogenesis.
those with severe renal impairment may accumulate clinically sign
acidosis include severe hepatic disease and acute/decompensated

Absorption Absorbed over 6 hours, bioavailability is 50 to 60% under fasting co

indicates that the level of absorption is not dose-related, suggestin
human cell cultures indicate that absorption occurs through a pass
 occurs 3 hours after oral administration.

Volume of 654 L for metformin 850 mg administered as a single dose. The volu
distribution in the GI tract and/or different methods used to determine volume o

Protein binding Metformin is negligibly bound to plasma proteins.

Metabolism Metformin is not metabolized.

Route of Intravenous single-dose studies in normal subjects demonstrate th

elimination metabolism (no metabolites have been identified in humans) nor bil
healthy renal function. Renal clearance of metformin is approximat
primary mode of metformin elimination.

Half life 6.2 hours. Duration of action is 8-12 hours.

Clearance 718-1552 mL/minute following single oral dose of 0.5-1.5 g. Metform

hemodynamic conditions.

Toxicity Acute oral toxicity (LD50): 350 mg/kg [Rabbit]. It would be expected
nausea, and vomiting followed by diarrhea, drowsiness, weakness,

Affected
organisms  Humans and other mammals

Drug
Interactions
Show entries

Drug

Acetazolamide The risk or severity of adverse effects can be increased

Acetylsalicylic acid Acetylsalicylic acid may increase the hypoglycemic ac
Aldesleukin The risk or severity of adverse effects can be increased
 Drug
Ardeparin Ardeparin may increase the hyperkalemic activities of
Aripiprazole The therapeutic efficacy of Metformin can be decrease
Arsenic trioxide The therapeutic efficacy of Metformin can be decrease
Articaine The therapeutic efficacy ofMETFORMIN can be dec
Asenapine The therapeutic efficacy of Metformin can be decrease
Atazanavir The therapeutic efficacy of Metformin can be decrease
Bendroflumethiazide The therapeutic efficacy of Metformin can be decrease

Showing 1 to 10 of 163 entries

Food
Interactions  Avoid alcohol.

 Take with food to reduce gastric irritation

Identification
Name Piroxicam

Accession DB00554 (APRD01187)

Number

Type Small Molecule

Groups Approved, Investigational

Description A cyclooxygenase inhibiting, non-steroidal anti-inflammatory agent

and used for musculoskeletal disorders, dysmenorrhea, and postop

Structure
MOLSDF3D-SDFPDBSMILESInChI View 3D Structure

Synonyms 4-Hydroxy-2-methyl-N-(2-pyridyl)-2H-1,2-benzothiazin-3-caboxyamid-1,1-dioxid
Feldene
Piroxicam
Piroxicamum
Pyroxycam

INTERNATIONAL
BRANDS
Show entries

Name

Bruxicam
Dolonex
Erazon
Geldène
Improntal
Roxam
Roxiden
 Name
Sasulen
Solocalm
Trast

Pharmacology

Indication For treatment of osteoarthritis and rheumatoid arthritis.

Pharmacodynami Piroxicam is in a class of drugs called nonsteroidal anti-inflammato

cs and pain in the body. Piroxicam is used to reduce the pain, inflamm

Mechanism of The antiinflammatory effect of Piroxicam may result from the rever
action synthesis. The prostaglandins are produced by an enzyme called Co
of prostaglandins. Piroxicam also inhibits the migration of leukocyt
aggregating agent, by the platelets.

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Absorption Well absorbed following oral administration.

Volume of
distribution  0.14 L/kg

Protein binding Not Available

Metabolism Renal

Substrate Enzymes

Piroxicam
 Cytochrome P450 2C9

Route of Piroxicam and its biotransformation products are excreted in urine

elimination Approximately 5% of a piroxicam dose is excreted unchanged. How
Piroxicam is excreted into human milk.

Half life 30 to 86 hours

Clearance Not Available

Toxicity Symptoms of overdose include drowsiness, nausea, stomach pain, a

Affected
organisms  Humans and other mammals

Interactions

Drug
Interactions
Show entries

Drug

Abciximab Piroxicam may increase the anticoagulant activities of

Acenocoumarol Piroxicam may increase the anticoagulant activities of
Acetylsalicylic acid The risk or severity of adverse effects can be increased
Aliskiren Piroxicam may decrease the antihypertensive activities
 Drug
Alteplase Piroxicam may increase the anticoagulant activities of
Amikacin Piroxicam may decrease the excretion rate of Amikacin
Amitriptyline Amitriptyline may increase the antiplatelet activities of
Anistreplase Piroxicam may increase the anticoagulant activities of
Apixaban The risk or severity of adverse effects can be increased
Arbekacin Piroxicam may decrease the excretion rate of Arbekaci
Showing 1 to 10 of 103 entries

Food
Interactions  Take with food. Avoid alcohol.