ICL 4.2: Medical care and Pharmacological Agents of Diabetes Flashcards
(39 cards)
how do you diagnose diabetes?
AIc over 6.5
FPG over 126
casual plasma glucose over 200
2 hr plasma glucose over 200
how do you diagnose prediabetes?
A1c 5.7-6.4
impaired fasting glucose 100-125
impaired glucose tolerance
what int he genetic risk of DMI?
identical twins is 30-60%
risk in family members is 5% if a sibling has it, 3% if mom and 6% if dad
what int he genetic risk of DMII?
50-90% in twins
lifetime risk of DM2 is 40$ in offspring of one diabetic parents and 70% if both parents
what are the goals of therapy for DM in non pregnant adults?
A1c under 7%
fasting 70-130
postprandial under 180
what are the goals of therapy for DM in elders?
A1C under 8% but over 7
what are the goals of therapy for DM in GDM pregnant adults?
fasting less than 95
post prandial in 1 hr is under 140 and 2 hr is under 120
what is the goal in DM in the hospital?
critically ill surgical patients: 140-180 and treat with insulin
critically ill nonsurgical patients: 140-180 and also insulin treatment
noncritlcally ill patients: fasting under 140 but treat with insulin basal, nutritional and correct preferred
what are the classes of DM drugs?
- sensitizers
- insulin secretagogues
- insulin analogs
- others
which drugs are sensitizers?
- biguianides like metformin
2. TZs like glitazones
what is the MOA of biguanides?
biguanidesreducehepaticglucose output and increase uptake of glucose by the periphery, including skeletal muscle
reduces A1c 1.5-2%
among common diabetic drugs, metformin is the only widely used oral drug that does not cause weight gain
what caution do you have to take when giving biguanidse?
although it must be used with caution in patients with impaired liver or kidneyfunction,metformin a biguanide, has become the most commonly used agent for type 2 diabetes in children and teenagers
metformin(Glucophage) may be the best choice for patients who also have heart failure, but it should be temporarily discontinued before any radiographic procedure involving intravenousiodinatedcontrast, as patients are at an increased risk oflactic acidosis.
what is the first line medication for treating DMII?
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
there is an immediate release as well as an extended-release formulation, typically reserved for patients experiencinggastrointestinalside-effects
it is also available in combination with other oral diabetic medications
what is the MOA of thiazolidinediones?
TZDs also known as “glitazones,” bind toPPARγ, 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).
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
so basically they increase insulin sensitivity and also reduce A1c by 1.5-2% like metformin
what are the concerns with TZDs?
multiple retrospective studies have resulted in a concern about rosiglitazone’s safety, although it is established that 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
one large prospective study, PROactive, has shown thatpioglitazonemay decrease the overall incidence of cardiac events in people with type 2 diabetes who have already had a heart attack.
which drugs are KATP secretagogues?
aka K+ATP sulfonylureas
1st generation: Acetohexamide · Carbutamide · Chlorpropamide · Metahexamide · Tolbutamide · Tolazamide
2nd generation: Glibenclamide · Glyburide# · Glibornuride · Glipizide · Gliquidone · Glisoxepide · Glyclopyramide · Glimepiride · Gliclazide
what is the MOA of KATP secretagogues?
they areinsulinsecretagogues, triggering insulin release by inhibiting theKATPchannel of the pancreaticbeta cells
sulfonylureaswere the first widely used oral anti-hyperglycemic medications
sulfonylureas bind strongly toplasma proteins
reduce A1c by 1-2%
which type of DM are KATP secretagogues used in?
sulfonylureas are useful only in type 2 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 1 diabetes, or diabetes of pregnancy. They can be safely used with metformin or glitazones. The primary side-effect ishypoglycemia.
which drugs are KATP non-sulfa drugs?
Meglitinides/”glinides” Nateglinide · Repaglinide · Mitiglinide
what is the MOA of KATP non-sulfa drugs?
meglitinideshelp 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
by closing the potassium channels of the pancreatic beta cells, they open the calcium channels, thereby enhancing insulin secretion
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
.5-1% decrease in A1c
what is the side effects of KATP non-sulfa drugs?
weight gain and hypoglycemia
what are the GLP-1 agonist drugs?
Exenatide · Liraglutide · Taspoglutide† · Albiglutide† · Lixisenatide · Dulaglutide† · Semaglutide
what is the MOA of GLP-1 agonist drugs?
incretins are insulinsecretagogues – the two main candidate molecules that fulfill criteria for being an incretin areglucagon-like peptide-1(GLP-1) andgastric inhibitory peptide(glucose-dependent insulinotropic peptide, GIP)
noth GLP-1 and GIP are rapidly inactivated by the enzymedipeptidyl peptidase-4(DPP-4)
glucagon-like peptide (GLP) agonists bind to a membrane GLP receptor – therefore, insulin release 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
typical reductions inA1C values are 0.5–1.0%
what are GLP-1 agonists used to treat?
Exenatide(Byetta) was the firstGLP-1agonist approved for the treatment oftype 2 diabetes
Exenatide is not an analogue of GLP but rather a GLP agonist
Exenatide has only 53% homology with GLP, which increases its resistance to degradation by DPP-4 and extends its half-life
Liraglutide, a once-daily human analogue (97% homology), has been developed byNovo Nordiskunder the brand nameVictoza. Lixisenatide (Lyxumia) and Semaglutide (Ozempic) are now also available.