anti-diabetic medication - wikipedia, the free encyclopedia
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Anti-diabetic medicationFrom Wikipedia, the free encyclopedia
Anti-diabetic medications treat diabetes mellitus by lowering glucose levels in the blood. With the exceptions
of insulin, exenatide, liraglutide and pramlintide, all are administered orally and are thus also called oral
hypoglycemic agents ororal antihyperglycemic agents. There are different classes of anti-diabetic drugs,
and their selection depends on the nature of the diabetes, age and situation of the person, as well as other
factors.
Diabetes mellitus type 1 is a disease caused by the lack of insulin. Insulin must be used in Type I, which must be
injected.
Diabetes mellitus type 2 is a disease of insulin resistance by cells. Treatments include (1) agents that increase the
amount of insulin secreted by the pancreas, (2) agents that increase the sensitivity of target organs to insulin, and
(3) agents that decrease the rate at which glucose is absorbed from the gastrointestinal tract.
Several groups of drugs, mostly given by mouth, are effective in Type II, often in combination. The therapeutic
combination in Type II may include insulin, not necessarily because oral agents have failed completely, but insearch of a desired combination of effects. The great advantage of injected insulin in Type II is that a well-
educated patient can adjust the dose, or even take additional doses, when blood glucose levels measured by the
patient, usually with a simple meter, as needed by the measured amount of sugar in the blood.
Contents
1 Insulin
2 Comparison
3 Sensitizers
3.1 Biguanides
3.2 Thiazolidinediones
4 Secretagogues
4.1 Sulfonylureas
4.2 Nonsulfonylurea secretagogues
5 Alpha-glucosidase inhibitors
6 Peptide analogs
6.1 Injectable Incretin mimetics6.2 Injectable Amylin analogues
7 Natural substances
7.1 Plants
7.2 Elements
8 Generic
9 References
10 Further reading
Insulin
Main article: insulin
https://en.wikipedia.org/wiki/Insulinhttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Referenceshttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Plantshttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Injectable_Incretin_mimeticshttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Alpha-glucosidase_inhibitorshttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Nonsulfonylurea_secretagogueshttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Secretagogueshttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Thiazolidinedioneshttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Biguanideshttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Sensitizershttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Insulinhttps://en.wikipedia.org/wiki/Diabetes_mellitus_type_2https://en.wikipedia.org/wiki/Diabetes_mellitus_type_1https://en.wikipedia.org/wiki/Exenatidehttps://en.wikipedia.org/wiki/Liraglutidehttps://en.wikipedia.org/wiki/Pramlintidehttps://en.wikipedia.org/wiki/Insulinhttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Further_readinghttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Referenceshttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Generichttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Elementshttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Plantshttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Natural_substanceshttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Injectable_Amylin_analogueshttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Injectable_Incretin_mimeticshttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Peptide_analogshttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Alpha-glucosidase_inhibitorshttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Nonsulfonylurea_secretagogueshttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Sulfonylureashttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Secretagogueshttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Thiazolidinedioneshttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Biguanideshttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Sensitizershttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Comparisonhttps://en.wikipedia.org/wiki/Anti-diabetic_medication#Insulinhttps://en.wikipedia.org/wiki/Diabetes_mellitus_type_2https://en.wikipedia.org/wiki/Diabetes_mellitus_type_1https://en.wikipedia.org/wiki/Pramlintidehttps://en.wikipedia.org/wiki/Liraglutidehttps://en.wikipedia.org/wiki/Exenatidehttps://en.wikipedia.org/wiki/Insulinhttps://en.wikipedia.org/wiki/Glucosehttps://en.wikipedia.org/wiki/Diabetes_mellitus -
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Insulin is usually given subcutaneously, either by injections or by an insulin pump. Research of other routes of
administration is underway. In acute-care settings, insulin may also be given intravenously. In general, there are
three types of insulin, characterized by the rate which they are metabolized by the body. They are rapid acting
insulins, intermediate acting insulins and long acting insulins. Examples of rapid acting insulins include
Regular insulin (Humulin R, Novolin R)
Insulin lispro (Humalog)
Insulin aspart (Novolog)Insulin glulisine (Apidra)
Prompt insulin zinc (Semilente, Slightly slower acting)
Examples of intermediate acting insulins include
Isophane insulin, neutral protamine Hagedorn (NPH) (Humulin N, Novolin N)
Insulin zinc (Lente)
Examples of long acting insulins include
Extended insulin zinc insulin (Ultralente)
Insulin glargine (Lantus)
Insulin detemir (Levemir)
Comparison
The following table compares some common anti-diabetic agents, generalizing classes, although there may be
substantial variation in individual drugs of each class. When the table makes a comparison such as "lower risk"
or "more convenient" the comparison is with the other drugs on the table.
Comparison of anti-diabetic medication[1][2]
agent[2] mechanism[3] advantages[2] disadvantages[2]
Sulfonylurea
(glyburide,
glimepiride,
glipizide)
Stimulating insulin release by
pancreatic beta cells by inhibiting
the KATP channel
Inexpensive
Fast onset of
action
No effect on
bloodpressure
No effect on
low-density
lipoprotein
inexpensive
lower risk of
gastrointestinal
problems than
with
metformin
more
convenient
dosing
causes an average of 5
10 pounds weight gainIncreased risk of
hypoglycemia
Glyburide has increases
risk of hypoglycemia
slightly more as
compared with
glimepiride and glipizide
Higher risk of death
compared with
metformin[4]
https://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-news.yahoo-4https://en.wikipedia.org/wiki/Hypoglycemiahttps://en.wikipedia.org/wiki/Weight_gainhttps://en.wikipedia.org/wiki/Human_gastrointestinal_tracthttps://en.wikipedia.org/wiki/Low-density_lipoproteinhttps://en.wikipedia.org/wiki/Blood_pressurehttps://en.wikipedia.org/wiki/ATP-sensitive_potassium_channelhttps://en.wikipedia.org/wiki/Beta_cellhttps://en.wikipedia.org/wiki/Glipizidehttps://en.wikipedia.org/wiki/Glimepiridehttps://en.wikipedia.org/wiki/Glyburidehttps://en.wikipedia.org/wiki/Sulfonylureahttps://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-BBDdiabetesM2-2https://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-BBDdiabetesM2-2https://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-agabegi2nd-185-3https://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-BBDdiabetesM2-2https://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-BBDdiabetesM2-2https://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-1https://en.wikipedia.org/wiki/Insulin_pumphttps://en.wikipedia.org/wiki/Subcutaneous_tissue -
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MetforminActs on liver to cause decrease in
insulin resistance
not associated
with weight
gain
low risk of
hypoglycemia
as compared
to alternatives
Good effect
on LDL
cholesterol
Decreases
triglycerides
no effect on
blood
pressure
inexpensive
increased risk of
gastrointestinal problems
Contraindicated for
people with moderate orsevere kidney disease or
heart failure because of
risk of lactic acidosis
increased risk of Vitamin
B12 deficiency[3]
less convenient dosing
Metallic taste[3]
Alpha-
glucosidase
inhibitor
(acarbose,
miglitol,
voglibose)
Reduces glucose absorbance by
acting on small intestine to cause
decrease in production of enzymes
needed to digest carbohydrates
slightly
decreased risk
of
hypoglycemia
as compared
to sulfonylurea
not associatedwith weight
gain
decreases
triglycerides
no effect on
cholesterol
less effective than most
other diabetes pills in
decreasing glycated
hemoglobin
increased risk of GI
problems than other
diabetes pills except
metformin
inconvenient dosing
expensive
Thiazolidinediones
(Pioglitazone,
Rosiglitazone)
Reduce insulin resistance by
activating PPAR- in fat and
muscle
Lower risk of
hypoglycemia
Slight increase
in high-densitylipoprotein
Actos linked
to decreased
increased risk of heartfailure
causes an average of 5
10 pounds weight gain
associated with higher
risk of edema
associated with higher
risk of anemia
increases low-density
lipoprotein
Avandia linked to
increased triglycerides
and risk of heart attack
Actos linked to
https://en.wikipedia.org/wiki/Anemiahttps://en.wikipedia.org/wiki/Edemahttps://en.wikipedia.org/wiki/Weight_gainhttps://en.wikipedia.org/wiki/Heart_failurehttps://en.wikipedia.org/wiki/High-density_lipoproteinhttps://en.wikipedia.org/wiki/Peroxisome_proliferator-activated_receptor_gammahttps://en.wikipedia.org/wiki/Rosiglitazonehttps://en.wikipedia.org/wiki/Pioglitazonehttps://en.wikipedia.org/wiki/Thiazolidinedioneshttps://en.wikipedia.org/wiki/Glycated_hemoglobinhttps://en.wikipedia.org/wiki/Small_intestinehttps://en.wikipedia.org/wiki/Voglibosehttps://en.wikipedia.org/wiki/Miglitolhttps://en.wikipedia.org/wiki/Acarbosehttps://en.wikipedia.org/wiki/Alpha-glucosidase_inhibitorhttps://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-agabegi2nd-185-3https://en.wikipedia.org/wiki/Metallic_tastehttps://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-agabegi2nd-185-3https://en.wikipedia.org/wiki/Vitamin_B12_deficiencyhttps://en.wikipedia.org/wiki/Lactic_acidosishttps://en.wikipedia.org/wiki/Heart_failurehttps://en.wikipedia.org/wiki/Kidney_diseasehttps://en.wikipedia.org/wiki/Human_gastrointestinal_tracthttps://en.wikipedia.org/wiki/Triglycerideshttps://en.wikipedia.org/wiki/LDL_cholesterolhttps://en.wikipedia.org/wiki/Insulin_resistancehttps://en.wikipedia.org/wiki/Metformin -
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triglycerides
Convenient
dosing
increased risk of bladder
cancer
slower onset of action
requires monitoring for
hepatoxicity
associated with
increased risk of limb
fracturesexpensive
Most anti-diabetic agents are contraindicated in pregnancy, in which insulin is preferred.[3]
Sensitizers
Insulin sensitizers address the core problem in Type II diabetesinsulin resistance.
Biguanides
Main article: Biguanide
Biguanides reduce hepatic glucose output and increase uptake of glucose by the periphery, including skeletal
muscle. Although it must be used with caution in patients with impaired liver or kidney function, metformin, a
biguanide, has become the most commonly used agent for type 2 diabetes in children and teenagers. Among
common diabetic drugs, metformin is the only widely used oral drug that does not cause weight gain.
Typical reduction in glycated hemoglobin (A1C) values for metformin is 1.52.0%
Metformin (Glucophage) may be the best choice for patients who also have heart failure, [5] but it should
be temporarily discontinued before any radiographic procedure involving intravenous iodinated contrast,
as patients are at an increased risk of lactic acidosis.
Phenformin (DBI) was used from 1960s through 1980s, but was withdrawn due to lactic acidosis risk. [6]
Buformin also was withdrawn due to lactic acidosis risk.[7]
Metformin is usually the first-line medication used for treatment of type 2 diabetes. In general, it is prescribed at
initial diagnosis in conjunction with exercise and weight loss, as opposed to in the past, where it was prescribedafter diet and exercise had failed. There is an immediate release as well as an extended-release formulation,
typically reserved for patients experiencing GI side-effects. It is also available in combination with other oral
diabetic medications.
Thiazolidinediones
Main article: Thiazolidinedione
Thiazolidinediones (TZDs), also known as "glitazones," bind to PPAR, a type of nuclear regulatory protein
involved in transcription of genes regulating glucose and fat metabolism. These PPARs act on peroxysome
proliferator responsive elements (PPRE).[8] The PPREs influence insulin-sensitive genes, which enhance
production of mRNAs of insulin-dependent enzymes. The final result is better use of glucose by the cells.
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Typical reductions in glycated hemoglobin (A1C) values are 1.52.0%. Some examples are:
rosiglitazone (Avandia): the European Medicines Agency recommended in September 2010 that it be
suspended from the EU market due to elevated cardiovascular risks.[9]
pioglitazone (Actos)
troglitazone (Rezulin): used in 1990s, withdrawn due to hepatitis and liver damage risk[10]
Multiple retrospective studies have resulted in a concern about rosiglitazone's safety, although it is establishedthat the group, as a whole, has beneficial effects on diabetes. The greatest concern is an increase in the number
of severe cardiac events in patients taking it. The ADOPT study showed that initial therapy with drugs of this
type may prevent the progression of disease,[11] as did the DREAM trial.[12]
Concerns about the safety of rosiglitazone arose when a retrospective meta-analysis was published in the New
England Journal of Medicine.[13] There have been a significant number of publications since then, and a Food
and Drug Administration panel[14] voted, with some controversy, 20:3 that available studies "supported a signal
of harm," but voted 22:1 to keep the drug on the market. The meta-analysis was not supported by an interim
analysis of the trial designed to evaluate the issue, and several other reports have failed to conclude the
controversy. This weak evidence for adverse effects has reduced the use of rosiglitazone, despite its importantand sustained effects on glycemic control.[15] Safety studies are continuing.
In contrast, at least one large prospective study, PROactive 05, has shown that pioglitazone may decrease the
overall incidence of cardiac events in people with type 2 diabetes who have already had a heart attack.[16]
Secretagogues
These are the drugs that increase Insulin output from Pancreas.
Sulfonylureas
Main article: Sulfonylurea
Sulfonylureas were the first widely used oral anti-hyperglycaemic medications. They are insulin secretagogues,
triggering insulin release by inhibiting the KATP channel of the pancreatic beta cells. Eight types of these pills
have been marketed in North America, but not all remain available. The "second-generation" drugs are now
more commonly used. They are more effective than first-generation drugs and have fewer side-effects. All may
cause weight gain. A 2012 study found sulfonylureas raise the risk of death compared with metformin. [4]
Sulfonylureas bind strongly to plasma proteins. Sulfonylureas are useful only in Type II diabetes, as they work
by stimulating endogenous release of insulin. They work best with patients over 40 years old who have had
diabetes mellitus for under ten years. They cannot be used with type I diabetes, or diabetes of pregnancy. They
can be safely used with metformin or -glitazones. The primary side-effect is hypoglycemia.
Typical reductions in glycated hemoglobin (A1C) values for second-generation sulfonylureas are 1.02.0%.
First-generation agents
tolbutamide (Orinase brand name )
acetohexamide (Dymelor)
tolazamide (Tolinase)
chlorpropamide (Diabinese)
Second-generation agents
https://en.wikipedia.org/wiki/Chlorpropamidehttps://en.wikipedia.org/wiki/Tolazamidehttps://en.wikipedia.org/wiki/Acetohexamidehttps://en.wikipedia.org/wiki/Tolbutamidehttps://en.wikipedia.org/wiki/Glycated_hemoglobinhttps://en.wikipedia.org/wiki/Hypoglycemiahttps://en.wikipedia.org/wiki/Plasma_proteinhttps://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-news.yahoo-4https://en.wikipedia.org/wiki/Beta_cellhttps://en.wikipedia.org/wiki/ATP-sensitive_potassium_channelhttps://en.wikipedia.org/wiki/Secretagoguehttps://en.wikipedia.org/wiki/Sulfonylureahttps://en.wikipedia.org/wiki/Sulfonylureahttps://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-16https://en.wikipedia.org/wiki/Pioglitazonehttps://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-Ajjan-15https://en.wikipedia.org/wiki/Glycemic_controlhttps://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-14https://en.wikipedia.org/wiki/Food_and_Drug_Administrationhttps://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-13https://en.wikipedia.org/wiki/The_New_England_Journal_of_Medicinehttps://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-12https://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-11https://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-10https://en.wikipedia.org/wiki/Hepatitishttps://en.wikipedia.org/wiki/Troglitazonehttps://en.wikipedia.org/wiki/Pioglitazonehttps://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-9https://en.wikipedia.org/wiki/European_Medicines_Agencyhttps://en.wikipedia.org/wiki/Rosiglitazonehttps://en.wikipedia.org/wiki/Glycated_hemoglobin -
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glipizide (Glucotrol)
glyburide or glibenclamide (Diabeta, Micronase, Glynase)
glimepiride (Amaryl)
gliclazide (Diamicron)
glycopyramide
gliquidone
Nonsulfonylurea secretagogues
Meglitinides
Main article: Meglitinide
Meglitinides help the pancreas produce insulin and are often called "short-acting secretagogues." They act on the
same potassium channels as sulfonylureas, but at a different binding site.[17] By closing the potassium channels o
the pancreatic beta cells, they open the calcium channels, thereby enhancing insulin secretion. [18]
They are taken with or shortly before meals to boost the insulin response to each meal. If a meal is skipped, the
medication is also skipped.
Typical reductions in glycated hemoglobin (A1C) values are 0.51.0%.
repaglinide (Prandin)
nateglinide (Starlix)
Adverse reactions include weight gain and hypoglycemia.
Alpha-glucosidase inhibitors
Main article: Alpha-glucosidase inhibitor
Alpha-glucosidase inhibitors are "diabetes pills" but not technically hypoglycemic agents because they do not
have a direct effect on insulin secretion or sensitivity. These agents slow the digestion of starch in the small
intestine, so that glucose from the starch of a meal enters the bloodstream more slowly, and can be matched
more effectively by an impaired insulin response or sensitivity. These agents are effective by themselves only in
the earliest stages of impaired glucose tolerance, but can be helpful in combination with other agents in type 2
diabetes.
Typical reductions in glycated hemoglobin (A1C) values are 0.51.0%.
miglitol (Glyset)
acarbose (Precose/Glucobay)
voglibose
These medications are rarely used in the United States because of the severity of their side-effects (flatulence
and bloating). They are more commonly prescribed in Europe. They do have the potential to cause weight loss
by lowering the amount of sugar metabolized.
Research has shown that the culinary mushroom maitake (Grifola frondosa) has a hypoglycemic
effect,[19][20][21][22][23][24] possibly due to the mushroom acting as a natural alpha glucosidase inhibitor.[25]
https://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-25https://en.wikipedia.org/wiki/Alpha_glucosidase_inhibitorhttps://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-pmid11349892-24https://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-pmid11874441-23https://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-pmid18457360-22https://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-pmid7820117-21https://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-pmid17430642-20https://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-pmid11903406-19https://en.wikipedia.org/wiki/Blood_sugarhttps://en.wikipedia.org/wiki/Grifola_frondosahttps://en.wikipedia.org/wiki/Voglibosehttps://en.wikipedia.org/wiki/Acarbosehttps://en.wikipedia.org/wiki/Miglitolhttps://en.wikipedia.org/wiki/Glycated_hemoglobinhttps://en.wikipedia.org/wiki/Type_2_diabeteshttps://en.wikipedia.org/wiki/Impaired_glucose_tolerancehttps://en.wikipedia.org/wiki/Alpha-glucosidase_inhibitorhttps://en.wikipedia.org/wiki/Alpha-glucosidase_inhibitorhttps://en.wikipedia.org/wiki/Nateglinidehttps://en.wikipedia.org/wiki/Repaglinidehttps://en.wikipedia.org/wiki/Glycated_hemoglobinhttps://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-diabetespancreasbeta-18https://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-17https://en.wikipedia.org/wiki/Meglitinidehttps://en.wikipedia.org/wiki/Meglitinidehttps://en.wikipedia.org/wiki/Gliquidonehttps://en.wikipedia.org/w/index.php?title=Glycopyramide&action=edit&redlink=1https://en.wikipedia.org/wiki/Gliclazidehttps://en.wikipedia.org/wiki/Glimepiridehttps://en.wikipedia.org/wiki/Glibenclamidehttps://en.wikipedia.org/wiki/Glipizide -
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Overview of insulin secretion
Peptide analogs
Injectable Incretin mimetics
Incretins are insulin secretagogues. The two main
candidate molecules that fulfill criteria for being an
incretin are glucagon-like peptide-1 (GLP-1) and gastric
inhibitory peptide (glucose-dependent insulinotropic
peptide, GIP). Both GLP-1 and GIP are rapidly
inactivated by the enzyme dipeptidyl peptidase-4 (DPP-
4).
Injectable Glucagon-like peptide analogs and
agonists
Glucagon-like peptide (GLP) agonists bind to a
membrane GLP receptor.[18] As a consequence, insulinrelease from the pancreatic beta cells is increased.
Endogenous GLP has a half-life of only a few minutes, thus an analogue of GLP would not be practical.
Exenatide (also Exendin-4, marketed as Byetta) is the first GLP-1 agonist approved for the treatment of
type 2 diabetes. Exenatide is not an analogue of GLP but rather a GLP agonist.[26][27] Exenatide has only
53% homology with GLP, which increases its resistance to degradation by DPP-4 and extends its half-
life.[28] Typical reductions in A1C values are 0.51.0%.
Liraglutide, a once-daily human analogue (97% homology), has been developed by Novo Nordisk under
the brand name Victoza. The product was approved by the European Medicines Agency (EMEA) on
July 3, 2009, and by the U.S. Food and Drug Administration (FDA) on January 25,
2010.[29][30][31][32][33][34]
Taspoglutide is presently in Phase III clinical trials with Hoffman-La Roche.
These agents may also cause a decrease in gastric motility, responsible for the common side-effect of nausea,
and is probably the mechanism by which weight loss occurs.
Gastric inhibitory peptide analogs
None are FDA approved
Dipeptidyl Peptidase-4 Inhibitors
Main article: Dipeptidyl peptidase-4 inhibitors
GLP-1 analogs resulted in weight loss and had more gastrointestinal side-effects, while in general DPP-4
inhibitors were weight-neutral and increased risk for infection and headache, but both classes appear to present
an alternative to other antidiabetic drugs. However, weight gain and/or hypoglycaemia have been observed
when DPP-4 inhibitors were used with sulfonylureas; effect on long-term health and morbidity rates are stillunknown.[35]
Dipeptidyl peptidase-4 (DPP-4) inhibitors increase blood concentration of the incretin GLP-1 by inhibiting its
degradation by dipeptidyl peptidase-4.
https://en.wikipedia.org/wiki/Dipeptidyl_peptidase-4https://en.wikipedia.org/wiki/Incretinhttps://en.wikipedia.org/wiki/Dipeptidyl_peptidase-4_inhibitorshttps://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-nps01-35https://en.wikipedia.org/wiki/Dipeptidyl_peptidase-4_inhibitorshttps://en.wikipedia.org/wiki/Hoffman-La_Rochehttps://en.wikipedia.org/wiki/Taspoglutidehttps://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-34https://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-33https://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-32https://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-31https://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-30https://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-29https://en.wikipedia.org/wiki/U.S._Food_and_Drug_Administrationhttps://en.wikipedia.org/wiki/European_Medicines_Agencyhttps://en.wikipedia.org/wiki/Victozahttps://en.wikipedia.org/wiki/Novo_Nordiskhttps://en.wikipedia.org/wiki/Liraglutidehttps://en.wikipedia.org/wiki/Glycated_hemoglobinhttps://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-pmid17428109-28https://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-27https://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-26https://en.wikipedia.org/wiki/Type_2_diabeteshttps://en.wikipedia.org/wiki/Glucagon-like_peptide-1https://en.wikipedia.org/wiki/Exenatidehttps://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-diabetespancreasbeta-18https://en.wikipedia.org/wiki/Dipeptidyl_peptidase-4https://en.wikipedia.org/wiki/Gastric_inhibitory_peptidehttps://en.wikipedia.org/wiki/Glucagon-like_peptide-1https://en.wikipedia.org/wiki/Secretagoguehttps://en.wikipedia.org/wiki/Incretinhttps://en.wikipedia.org/wiki/File:Incretins_and_DPP_4_inhibitors.svg -
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Examples are:
vildagliptin (Galvus) EU Approved 2008
sitagliptin (Januvia) FDA approved Oct 2006
saxagliptin (Onglyza) FDA Approved July 2009
linagliptin (Tradjenta) FDA Approved May 2, 2011
allogliptin
septagliptin
DPP-4 inhibitors lowered hemoglobin A1C values by 0.74%, comparable to other antidiabetic drugs. [36]
A result in one RCT comprising 206 patients aged 65 or older (mean baseline HgbA1c of 7.8%) receiving
either 50 or 100 mg/d of Sitagliptin was shown to reduce HbA1c by 0.7% (combined result of both doses).[37]
A combined result of 5 RCTs enlisting a total of 279 patients aged 65 or older (mean baseline HbA1c of 8%)
receiving 5 mg/d of Saxagliptin was shown to reduce HbA1c by 0.73%.[38] A combined result of 5 RCTs
enlisting a total of 238 patients aged 65 or older (mean baseline HbA1c of 8.6%) receiving 100 mg/d of
Vildagliptin was shown to reduce HbA1c by 1.2%.[39] Another set of 6 combined RCTs involving Alogliptin
(not yet approved, might be released in 2012) was shown to reduce HbA1c by 0.73% in 455 patients aged 65or older who received 12.5 or 25 mg/d of the medication.[40]
Injectable Amylin analogues
Amylin agonist analogues slow gastric emptying and suppress glucagon. They have all the incretins actions
except stimulation of insulin secretion. As of 2007, pramlintide is the only clinically available amylin analogue.
Like insulin, it is administered by subcutaneous injection. The most frequent and severe adverse effect of
pramlintide is nausea, which occurs mostly at the beginning of treatment and gradually reduces. Typical
reductions in A1C values are 0.51.0%.
Natural substances
Plants
A number of medicinal plants have been studied for the treatment of diabetes, however there is insufficient
evidence to determine their effectiveness.[41] Cinnamon has blood sugar-lowering properties, however whether
or not it is useful for treating diabetes is unknown.[42] Researchers from Australia's Swinburne University have
found extracts from Australian Sandalwood and Indian Kino tree slows down two key enzymes in carbohydratemetabolism. [43] Bioassay-directed fractionation techniques led to isolation of isoorientin as the main
hypoglycemic component in Gentiana olivieri.[44]
Elements
While chromium supplements have no beneficial effect on healthy people, there might be an improvement in
glucose metabolism in individuals with diabetes, although the evidence for this effect remains weak.[45] Vanadyl
sulfate, a salt of vanadium, is still in preliminary studies.[46] There is tentative research that thiamine may prevent
some diabetic complications however more research is needed.[47]
Generic
https://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-47https://en.wikipedia.org/wiki/Thiaminehttps://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-46https://en.wikipedia.org/wiki/Vanadiumhttps://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-45https://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-44https://en.wikipedia.org/wiki/Gentiana_olivierihttps://en.wikipedia.org/wiki/Isoorientinhttps://en.wikipedia.org/wiki/Bioassay-directed_fractionationhttps://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-43https://en.wikipedia.org/wiki/Indian_Kino_treehttps://en.wikipedia.org/wiki/Australian_Sandalwoodhttps://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-42https://en.wikipedia.org/wiki/Cinnamonhttps://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-41https://en.wikipedia.org/wiki/Nauseahttps://en.wikipedia.org/wiki/Subcutaneous_injectionhttps://en.wikipedia.org/wiki/Pramlintidehttps://en.wikipedia.org/wiki/Glucagonhttps://en.wikipedia.org/wiki/Amylinhttps://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-40https://en.wikipedia.org/wiki/Alogliptinhttps://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-39https://en.wikipedia.org/wiki/Vildagliptinhttps://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-38https://en.wikipedia.org/wiki/Saxagliptinhttps://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-37https://en.wikipedia.org/wiki/Sitagliptinhttps://en.wikipedia.org/wiki/Anti-diabetic_medication#cite_note-pmid17622601-36https://en.wikipedia.org/wiki/Glycated_hemoglobinhttps://en.wikipedia.org/wiki/DPP-4_inhibitorshttps://en.wikipedia.org/w/index.php?title=Septagliptin&action=edit&redlink=1https://en.wikipedia.org/w/index.php?title=Allogliptin&action=edit&redlink=1https://en.wikipedia.org/wiki/Linagliptinhttps://en.wikipedia.org/wiki/Saxagliptinhttps://en.wikipedia.org/wiki/Sitagliptinhttps://en.wikipedia.org/wiki/Vildagliptin -
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Many anti-diabetes drugs are available as generic. It are:[48]
Sulfonylureas - Glimepiride, Glipizide, Glyburide
Biguanides - Metformin
Thiazolidinediones (Tzd) - Pioglitazone, Actos generic
Alpha-glucosidase inhibitors - Acarbose
Meglitinides - Nateglinide
Combination of Sulfonylureas plus Metformin - known by generic names of the two drugs
No generic for Dipeptidyl peptidase-4 inhibitors (Januvia, Onglyza) and Others Combinations
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Further reading
Lebovitz, Harold E. (2004). Therapy For Diabetes Mellitus and Related Disorders (4th ed.). Alexandria, VA:
American Diabetes Association. ISBN 1-58040-187-2.
Adams, Michael Ian; Holland, Norman Norwood (2003). Core Concepts in Pharmacology. Englewood Cliffs,
NJ: Prentice Hall. ISBN 0-13-089329-3.
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