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Sulfonylureas, Miglitinides
Insulin Secretagogues
Insulin Sentisizers
Biguanie, Thiazolidinediones
Glucagon, mobilizes glycogen stores
Produced hormone and fx of alpha
Insulin, Amylin, Storage and anabolic effects
Beta 75%
Beta 75%
Most common islet of langherhans cell
Somatostain, universal inhibitor of secretory cells
Delta (3-5%)
Ghrelin, (+) appetite
Epsilon (<1%)
Insulin
Catabolic is inhibited by what
Raised function in blood
Glucagon function
GLUT 1 → glycolysis → krebs → ETC → ATP
In the pancreatic beta cell, glucose enters through
Glucose
Most potent insulin stimulator
Glucagon
Increases blood sugar, gluconeogenesis, glycogenolysis
Heart force
Inotropic
Chronotropic
Heart rate
Type 1 DM
Complete absence of insulin
Type 1 DM
Destruction of pancreatic beta cell → severe or absolute insulin deficiency
Common in younger patients
200mg/dL
RBS
>126 mg/dL
FBS
6.5%
HBA1C
>200mg/dL
OGTT
Polyphagia, polydipsia, polyuria ( 4th is unintentional weight loss)
Common signs and symptoms of diabetes
gestational pregnancy
placenta and placental hormones creates insulin resistance
(Lispro, Aspart, Glusine)
Rapid Acting
5-15mins
Rapid Acting Onset of action
Short Acting
(Regular)
30-60 mins
Immediate Acting (NPH)
2-4Hrs OOA
Long acting
Gladgins, detemer, degludec
Rapid acting
Usually given sa ICI due to early peak of activity
True
T/F Rapid acting is given before meals
Rapid acting
Prepared for continuous SQ infusion devices
Short acting
Administered 1hr before meals
Short acting
Used in IV emergencies (DKA), SQ for ordinary maintenance therapy
Neutral Protamine Hagedorn
Intermediate acting
Intermediate acting (NPH)
Combination of regular insulin + protamine (hastens the absorption of insulin) +Zinc
Protamine
Hastens the absorption of insulin
Intermediate acting
It is rapidly combined with short and rapid acting
Peak less insulin
Long acting are
Glargine, deteme, degludec
Long acting insulins are
Chlorpropamide, Tolbutamide, Tolazamide
1st Gen sulfonyureas
Glimepiride, glipizide, glibenclamide, glaclazide (GLI and zide)
2nd gen sulfonyureas
2nd Gen
■ MOA: (+) Insulin release by (-) ATP dependent K+ channels in the pancreatic Beta cells (blocks ATP sensitive K+ channel)
■ USES: Type 2 DM
Hypoglycemia
Commin toxicity in 1st and 2nd gen
chocolate/ candy
rub coke
Rescue agent for hypoglycemia is _____ (if unconscious: ____ in the buccal area of the patient)
Disulfiram like effect
1st gen toxicity is like
Glibenclamide
Colestatic jaundice is a toxicity of what drug
Meglitinides (-nide)
MOA: (+) Insulin release by (-) ATP dependent K+ channels in the pancreatic Beta cells
■ USES: Type 2 DM
■ TOX:
● Hypoglycemia
● Headache
● Upper respiratory tract infection
Biguanide (Metformin)
MOA: (+) AMP-stimulated protein kinase →
inhibition of renal and hepatic gluconeogenesis; slows down glucose absorption in the GIT, reduces risk of DM in high-risk patients
T2DM, DM prevention, Polycystic Ovarian Syndrome, DOC for obese DM
Metformin is used for?
Ptx with hepatic and renal failure
Metformin
Thiazolidinediones (-tazone) Pioglitazone, Rosiglitazone, Troglitazone
○ MOA: (+) PPAR (Peroxisome proliferator-Activated receptor) γ → increase insulin sensitivity by regulating the transcription of genes encoding for protein involved in carbohydrate and lipid metabolism
Thiazolidinediones (tazones)
Used for T2DM, DM PREVENTION
○ TOX:
■ Weight gain
■ Fluid retention → CHF
■ ↑ risk for fractures
■ ↑ risk of MI and cardiovascular events
(Rosiglitazone)
■ Hepatotoxicity (Troglitazone)
■ ↑ risk of bladder CA (Pioglitazone)
Toxicity of thiazolidinediones
Rosiglitazone
↑ risk of MI and cardiovascular events
Troglitazone
Hepatotoxicity
Pioglitazone
↑ risk of bladder CA
GLP1 analogs (-Tide)
MOA: (+) GLP1 receptors → mimics incretin which (+) insulin release, (-) glucagon release, produce a feeling of satiety
○ USES: T2DM
○ TOX:
■ Hypoglycemia
■ Acute pancreatitis (inflamed pancreas)
■ Weight loss → however once stopped, will
result in rebound weight gain
DPP4 Inhibitors (-gliptin) Sitagliptin, Linagliptin, Vildagliptin
MOA: Prevents GLP1 degradation
○ USES: T2DM
○ TOX:
■ Headache
■ Nasopharyngitis
■ URTI
Alpha-Glucosidase (Acarbose, Voglibose, Miglitol)
● MOA: (-) Intestinal α glucosidase → ↓ conversion of
starch and disaccharides to monosaccharides
● USES: T2DM
● TOX:
○ GI disturbances (Flatulence, Abdominal Pain, Diarrhea)
Amylin (Pramlintide)
● MOA: (+) Amylin receptors → ↓ glucagon release,
slows gastric emptying time, reduces appetite
● USES: T2DM
● TOX:
○ Hypoglycemia
○ Nausea
SGLT2 Inhibitors (-flozin) Dapaglifozin, Empaglifozin, Canaglifozin
● MOA: (-) Sodium-Glucose co-Trasnporter 2 (SGLT2) → (-) renal glucose reabsorption
● USES: T2DM
● TOX:
○ Glucosuria (UTI, vulvovaginitis, vaginal candidiasis)