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Oral Hypoglycemic Agents

Oral Hypoglycemic Agents

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Published by Hassan.shehri
Oral hypoglycemic agents
Oral hypoglycemic agents

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Published by: Hassan.shehri on Apr 30, 2010
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01/22/2014

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Hassan Mohammad AlShehri ID#2051040006
Oral Hypoglycemic AgentsSULFONYLUREAS
Accidentally discovered following the observation that sulfa antibiotics(sulfonamides) caused hypoglycemia in experimental animalsThey are divided into two groups or generations of agents.Structural Formulas of the SulfonylureasFirst Generation:Tolbutamide, Tolazamide, Acetohexamide
Second Generation 
:
Glyburide, Glipizide, GliclazideSecond genertion are non-polar and minimally bound to albumin which reducesincidence of certain types of drug interaction seen with first generationsulfonylureas.Mechanism of Sulfonylurea Actiona. Stimulate the release of insulin from pancreatic
β
cells.Sulfonylureas bind to SUR and block ATP-dependent K
+
channels- This reduces K
+
efflux leading to: 
β
cell depolarization, calcium influx and secretion of insulin.b. May also increase the sensitivity of peripheral tissues to insulin.Therapeutic Uses of SulfonylureasOf value only in the management of type 2 diabetic patients that have notdemonstrated ketosis and have not responded adequately to dietary therapy andweight control."
patient must have functional beta cells 
"Side Effects of Sulfonylureas1. May cause hypoglycemia2. Weight gain, allergic reactions, pruritus, rash, hepatotoxicity, andphotosensitivity are possible3. Hyponatremia and water retention - non
β
cell effects4.Therapeutic effect may be antagonized by thiazide diuretics, estrogens or anyagents that inhibit insulin release or antagonize peripheral action.
MEGLITINIDES
Repaglinide (Prandin®/NovoNorm®) 
Repaglinide (Prandin®/NovoNorm®)- an insulinotropic agent: stimulates insulin secretion by pancreatic beta cells-fast acting - short duration, administered before meals - from 30 min prior, rightup to meal time - unlike sulfonylureas (30 min)
 
Mechanism of Action:causes closure of ATP-dependent K
+
-channels.Side effects of Meglitinides:
In general, these are minimal, can cause hyperglycemia, hypoglycemia
Repaglinide has recently been contraindicated in patients taking gemfibrozil dueto the risk of severe/prolonged hypoglycemia
Also can occur with Clarithromycin, itraconazole, ketoconazole, MAOIs due toCYP2C8 and CYP3A4 interactions
BIGUNANIDES
Not marketed in US from 1977-1994 due to lactic acidosis1. Phenformin was associated with lactic acidosis2. Metformin (Glucophage®) introduced in the US in 1994 Several mechanisms of action have been proposed:increases liver, muscle and fat cell sensitivity to insulin- enhances peripheral glucose uptake and utilizationreduces hepatic glucose outputincreased muscle glycogen synthesisMetformin Side Effects:G.I. Disturbances - nausea, diarrhea, and flatulencelactic acidosis (rare) - risk where clearance of metformin is reduced i.e., patientswith renal or hepatic impairment
*
No significant hypoglycemia - does not stimulate insulin secretionshould be avoided in patients with alcohol abuse, severe hepatic impairment, andsevere congestive heart failureNotes:Particularly useful in patients with refractory obesityReduces a number of cardiac risk factorsCo-administered with a sulfonylurea, it can lower HbA1c values by 1% to 2%
EXENATIDE
- (Byetta®) 
Glucagon-like peptide-1 (GLP-1), a member of the incretin family
exendin-4 is a 39 amino acid peptide in salivary secretions of Gila monsterMechanism of Action:* exhibits 53% sequence similarity to GLP-1; protease resistant-enhances glucose-dependent insulin secretion
 
-suppresses elevated glucagon secretion-slows gastric emptyingimproves glycemic control by reducing fasting and postprandial glucoseconcentrations in patients with type 2 diabetesadministered twice daily, (subcutaneously) alone or in combination withmetformin, a sulfonylurea or both - significantly reduces HbA1cSide Effects:hypoglycemia, when taken in conjunction with a sulfonylureaGI disturbances – nausea, vomiting, diarrhea
Dipeptidyl Peptidase-4 (DPP-4) Inhibitors
Sitagliptin - (Januvia®) 
Mechanism of action:Sitagliptin (Januvia®) blocks DDP-4, a cell surface peptidase that cleaves a widerange of protein/peptide substrates This resultsin elevated levels of endogenous GLP-1 and GIP. This increases insulin anddecreases glucagon secretion, leading to better glycemic control.*It is used as an adjunct monotherapy to diet and exercise, to improve glycemiccontrol in patients with type 2 diabetes mellitus May be used incombination with metformin or a thiazolidinedione (TZD).- Sitagliptin should not be used in patients with type 1 diabetes or for thetreatment of diabetic ketoacidosis.- Recommended dose is 100 mg once daily, with or without food, asmonotherapy, as combination therapy with metformin or a TZD or as anadjunct to diet and exercise.Side Effects:include respiratory tract infection, nasopharyngitis (cold symptoms) andheadache
.ACARBOSE
Acarbose (Precose®) 
Mechanism of Action:

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