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Drugs for Diabetes Mellitus by Mind Map: Drugs for Diabetes Mellitus
0.0 stars - reviews range from 0 to 5

Drugs for Diabetes Mellitus

Meglitinides

Repaglinide

Nateglinide

MOA

Similar to Sulfonylreas, binds different site on the K channel

PK

Fast onset of action (15-30 min)

Short duration of action, Repa>Nate

Take before meal to control postprandial glycemia

Use

Type II DM

SE

Hypoglycemia

Sulfonylureas

Glimepiride

Glipizide

Glyburide

MOA

Antagonized K channel on pancreatic beta cell, Cause cell depolarization and allows efflux of Ca, Increased insulin release

Increases AMOUNT, not FREQUENCY of pulsatilue release of insulin, No effect on basal insulin levels!

Minor effect: Subsequently decreases glucagon release (b/c of increased insulin release), Possibly enhance by increased release of SMSTN w/ insulin

Use

Type II DM

Take 1/day

SE

Hypoglycemia, Both basal and postprandial

Weight gain, d/t high insulin levels

NV

Allergic skin rxns

Cholestatic jaundice

TCP, leukopenia, hemolytic anemia

Hyponatremia and SIADH

Thiazolidinediones (TZDs)

Pioglitazone

Rosiglitazone

MOA

Stimulate PPAR-gamma (intracellular receptor that increases transcription of GLUT-4), Found in fat and some muscle tissue

Increases glucose uptake in M and fat tissue

Decreased levels of free TGs

Inhibit GNG

Use

Type II D

Taken one/day, with food, Requires presence of insulin to work, GLUT-4 is an insulin sensitive receptor

SE

Weight gain, PPAR activation, collecting tubules, New node, Increased expression/activity of Na channels, Na resorption, edema, Weight gain, Differentiation of pre-adipocytes into mature adipose cells

Fluid retention, CI in pts with > Stage III CHF or acutely decompensated

Bone fracture, PPAR activated diverts stromal cells from osteoblasts to adipocyte lineage, fat deposition in bone, Women only!!

Anemia

Hepatotoxicity

Increased risk of CV events

Incretin (GLP-1) mimetics

GLP-1 agonist

Exanatide

Liraglutide

Admin - SQ injection

SE, Hypoglycemia, Pruritis, urtecaria, rash, Acute pancreatitis, Lira ONLY - risk of thyroid Ca, Black box warning!!!

DPP-IV inhibitors

Sitagliptin

Saxagliptin

Admin - oral

SE, Hypoglycemia, Allergic rxns, Stevens-Johnson Syndrome, angioedema, anaphyllaxis

MOA

GLP-1 is secreted by L-cells in ileum, Slows gastric emptying in stomach, Reduces postprandial spike in blood glucose levels, Promotes sense of satiety in brain, Increases glu-stimulated insulin and decreases glucagon secretion in pancreas, If target glu-stimulated insulin release, less chance of hypoglycemia

DPP-IV is the NZ that metabolizes GLP-1, GLP-1 1/2 life in circulation = 1-2 minutes

Use

Type II DM

Amylin analog

Primlintide

Use

Type I & II DM who inject insulin at meal times

SQ injection

MOA

Released w/ insulin from beta cells, Increases satiety, Delays gastric emptying, Inhibits glucagon release

Reduces postprandial glucose spike

SE

NVA

Headache

Hypoglycemia when combined w/ insulin

alpha-glucosidase inhibitors

Acarbose

Miglitol

MOA

Reversible inhibition of NZ on brush border that breaks down disaccharides into glucose, Slows absorption of glucose from gut, Reduces postprand insulin spike, No effect on fasting glucose levels

Use

Type II DM

Reduces risk of Type II DM in pts with impaired glucose tolerance

SE

Flatulence, bloating, abdominal discomfort

Diarrhea

Elevated liver NZs

Biguanides

Metformin

Use, Reduces insulin resistane in Type II, Decreases risk of Type II D in pts with insulin resistance, Not as effective as lifestyle changes!!!

Admin/PK, Ineffective in the absense of insulin, Must take with food, Also reduces GI SE, Excreted in urine, 1/2 life = 2 hrs

MOA, Improves glucose uptake in M and fat celss, Reduces hepatic glucose production - Major Action!!!, Ultimately decreases serum insulin and glucose levels, Decreases both fasting and postprandial hyperglycemia

SE, Positives, No risk of hypoglycemia, Not stimulating any insulin release from pancreas, Weight loss or stabilization, Prevent macrovascular complications, Decreased TG, total and LDL-C, Decreases VLDL synthesis, Cheap!!!, Negative, NVD (pretty common), anorexia - contributes to the weight loss, Metallic taste, Lactic acidosis (rare), Increases tissue hypoxia -> increased production of LA

CI, Pt predisposed to lactic acidosis, Renal Dz, Hepatic Dz, or alcoholics, Hx of LA, Decreased tissue perfusion or hemodynamic instability, MI, Left ventricular failut, Chronic hypoxic lung Dz, Septicemia, Discontinue prior to, Surgery, Compromised circulation, Use of IV contrast, Increased change of ARF

Insulin

Rapid Acting (4 hrs activity)

Insulin Lispro

Short Acting

Regular Humulin R

Intermediate Acting

NPH Humulin N

Long Acting (24 hrs activity)

Insulin Glargine

Use

Pt often on > 1 type, Ex - 1 LA dose/day for basal levels + RA injection before every meal to handle addition carb load

Insulin pump, maintains basal raid + gives a meal bolus, Only use RA insulin

Injection

SE

Lipohypertrophy, Occurs when you give the injection in the same spot

Hypoglycemia, Sx of activated sympathetics, Sx of brain not getting enough glucose

Glucagon

Use

Tx hypoglycemia

MOA

Made by alpha cells in pancreas; stimulate liver into GNG and glycogenolysis

Admin

SQ injection

Type II Diabetes causes

Insulin resistance

Failure of liver to decrease glucose production

Impaired glucose uptake in muscle and fat cells

Drugs that work here:, Metformin, TZDs

reduced GLP-1

Drugs that work here:, Incretins

Pancreatic Beta cell dysfuntion

reduced insulin secretion, Drugs that work here:, Sulfonylureas, Meglitinides

Reduced amylin secretion, Drugs that work here:, Pramlintide