INSULIN &OTHER GLUCOSE LOWERING DRUGS

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Diabetes Mellitus

Heterogenous group of syndromes characterizes by elevated Blood Glucose level caused by relative or absolute deficiency of INSULIN.

Pancreas is an Endogenous gland, produces Insulin, Glucagon, Somatastatin…
Pancreas is also an exogenous gland produce digestive enzymes…β-cells produce
insulin, α-cells Glucagon, δ-cells produce Somatostatin…

Type-1 Diabetes Mellitus

 young individual, Autoimmune destruction of β-cells, Pancreas fail to respond Glucose……..required Exogenous Insulin to avoid Catabolic state characterized by Hyperglycemia & Ketoacidosis…..

Insulin deficiency symptoms Polydipsia, Polyphagia, Polyuria, weight loss

Type-2 Diabetes Mellitus


 by Genetic factor, obesity, aging, peripheral insulin resistance older patients...β-cells become resistance to insulin...infection lead to
Amputation

Gestational Diabetes Mellitus

 abnormality ofglucose in first term of Pregnancy
Insulin & its analogue
Diabetes , sugar lowering drugs insulin pharmacology mechanism of action


MOA

insulin secretion triggered by High Glucose…Glucokiase act as Glucose sensor...
Glucose taken up into the β-cell...phosphorylated by Glucokinase…products of Glucose met.

 Enter in Mitochondria…generate ATP….increase ATP block K+ channel…depolarization…influx of Ca++…..insulin exocytosis…

Sources of insulin=recombinant DNA from Escherichia or yeast 

Short/Rapid Acting Insulin


Regular insulin, Insulin Lispro, Insulin Aspart pregnancy category B…….., Insulin Glulisine pregnancy category C…..insulin lispro 30-90min
peak level…Insulin Aspart & Glulisine ara Rapid acting

Intermediate-Acting Insulin


NPH (Neutral Protamine Hagedorn) suspension of crystalline zinc insulin at neutral pH +Ve charged……

Long –Acting Insulin

 Insulin Glargine isoelectric point lower than human insulin... no peak effect
Insulin Detemir
 has fatty acid side chain...bind to Albumin..
Amylin Analogue
Pramlintide synthetic amylin analogue...an adjunct to mealtime insulin…delay gastric
emptying…decrease postprandial Glucagon secretion...imporve satiety….used in
diabetic gastroparesis (delay stomch emptying)…..
not mixed with any insulin prep in
syringe…
S.E; Anorexia, vomiting,, nausea..

Insulin Sectretagogue; 

Sulfonylurea

MOA same to insulin…useful in Diabetes type-2…classified secretagogue bcz produce
Insulin from β-cells….orally...12-24hr duration...

S.E;weight gain, hypoglycemia...safe in
preganancy...caution in hepatic & renal impair
Glinides

Rapaglinide & Nateglinide

MOA like insulin…have rapid onset & short duration of action called Postprandial Glucose Regulator bcz early release of insulin after
meal…

S.E
Hypoglycemia, weight gain ...used with caution in hepatic impair…use with Gemfibrozil is contraindicated

Insulin sensitizer

Biguanides

Metformin only currently used…does not promote insulin secretion

MOA : reduction of hepatic glucose output…inhibit Gluuconeognesis…slow intestinal
abs. of sugars...improve peripheral glucose uptake & utilization…
reduce hyperlipidemia... decrease insulin resistance…increase HDL…
used in pregnancy
T.E
used in Diabetic Ketooacidosis, DOC in type-2 Diabetes, Polysystic ovarydisease
S.E
 GIT disturbance, contraindicated in pt.with lver/renal impair, M.I, CHF, Lactic
acidosis….interfere with vit B12 Abs.

Glitazone/Thiazolidinediones TZDs

Traglitazine withdraw due to hepatotxicity…

MOA= bind to PPARγ….Peroxisome-Proliferator-activated receptor-γ …regulate
Adipocyte production….secretion of fatty acid…glucose met…insulin sensitivity in liver,
adipose tissue, skeletal muscle…Hyperglycemia,Hyperinsulinemia,Elevated HbA1c,
hypertricglycemia….HDL level incrase

S.E
weight gain, Osteopenia, increased Fracture risk, anemia...cause Ovulation in postmenopausal women so take Contraceptive while taking TZDs....not used in lactation

α-Glucosidase Inhibitors

Acarbose & Miglitol=used in Diabetes type-2

MOA= used in beginning of meal...inhibit α-Glucosidase….enzyme responsible
hydrolysis of Oligosacharide to glucose & other sugar…..delay digestion of C.H.O…
decrease postprandial glucose level…also inhibit α-amylase...inhibit breakdown of Starch into Oligosacchaaride

S.E= diarrhea, cramps, Flatulance…contra in ulcer & intestinal obstruction 

Dipeptidyl Peptidase-IV inhibitor

Sitagliptin & Saxagliptin

inhibit DPP-IV...responsible for inactivation of Incretin hormone…result increase Incretin...increase Insulin.

S.E= Pancreatitis, Headache, Nasopharyngitis,
Incretin mimetics
Exenatide & Liraglutide=analogue of GLP-1(Glucagon like peptide)…increase
Glucose dependent Insulin secretion …Slow Gastric emptying…decrease postprandial Glugagon
Secretion, promote β-cell Proliferation…Liraglutide O.D used...
Exenatide twice inj...Weight gain reduced.

S.E=Constipation, Pancreatitis, Abdominal pain

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