Pancreatic hormones and anti diabetic drugs Flashcards
(115 cards)
0
Q
insulin dependent DM
A
Type 1
1
Q
4 categories if Diabetes Mellitus
A
Type1 insulin dependent
Type 2 non insulin dependent
Type 3 juvenile
Type 4 Gestational DM
2
Q
non insulin dependent DM
A
Type 2
3
Q
juvenile DM
A
Type 3
4
Q
Gestational DM
A
Type 4
5
Q
4 main cell types in pancreas
A
glucagon
insulin
somatostatin
pancreatic polypeptide
6
Q
alpha pancreatic cells secrete
A
glucagon
7
Q
beta pancreatic cells secrete
A
insulin
8
Q
gamma pancreatic cells secrete
A
somatostatin
9
Q
effects of insulin on liver
A
inhibit glycogenolysis
inhibit conversion of AA and FA to keto acids
inhibit AA to glucose
anabolic action
10
Q
effects of insulin on muscle
A
increase CHON. synthesis, AA transport, ribosomal synthesis
increase glycogen synthesis, glucose trasport
inhibits phosphorylase
11
Q
effects of insulin on adipose tissue
A
increase triglyceride stores
lipoprotein lipase induced
glucose transport into cells
inhibits intracellular lipase
12
Q
rapidly acting insulin
A
Lispro
Aspart
Glulisine
13
Q
rapidly acting insulin (1) onset of action and (2) peak
A
ONSET: 15 minutes
PEAK: 30-90minutes
taken before meals
14
Q
duration of action is 3-5 hours
A
rapidly acting insulin
15
Q
crystalline zinc insulin that is now made by recombinant DNA techniques
A
short acting insulin
16
Q
short acting insulin onset of action
A
within 30 min
17
Q
peak of short acting insulin
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2-4 hours after SQ
18
Q
short acting insulin duration of action
A
5-8 hours
19
Q
regular insulin / short acting insulins
A
Novolin
Humulin
20
Q
regular insulin should be administered within
A
30-45 mins
21
Q
intermediate acting insulin which combines insulin and protamine
A
Neutral Protamine Hagedorn or isophane insulin
22
Q
intermediate acting insulin onset of action
A
1-2 hours
23
Q
intermediate acting insulin peak
A
8 hours
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duraton of action is 12-16 hours
intermediate acting insulin
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usually mixed with regular, lispro, aspart, or glulisine insulin
NPH or isophane intermediate acting insulin
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duration of action >24 hours
| onset of actin 1-2 hrs
DETEMIR long acting insulin
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soluble "peakless" insulin given once daily
GLARGINE Long acting insulin
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insulin glargine onset of action
slow onset of action 1-1.5 hrs
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insulin lispro, aspart, glusine acutely mixed with NPH
Pre-mixed insulin (doesnt affect rapid absorption)
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available concentration of insulin
100 U/ml
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external open loop pump for insulin delivery
Continuous SQ insulin infusion device (abdomen, flank, thighs)
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most recently developed long scting insulin
| DOSE dependent
DETEMIR insulin
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insulin therapy formula
(wt in lbs) / (4) or
| 0.55) x (wt in kg
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conventional insulin therapy
for DM type 2
fixed dose of intermediate or long acting
vary dos of short or rapidly acting
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condition caused by inadequate or absent insulin replacement
Diabetic Ketoacidosis (DKA)
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Tx for DKA
regular insulin IV 0.1IU/kg/h + IV hydration
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DM type 2 characterized by HYPERGLYCEMIA and DEHYDRATION
Hyperosmolar Hyperglycemic Syndrome (HHS)
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Tx for Hyperosmolar Hyperglycemic Syndrome (HHS)
aggressive rehydration and restoration of glucose
| LOW DOSE Insulin therapy
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most common complication of insulin therapy
HYPOGLYCEMIA
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2 major disorders of insulin therapy
insulin allergy
| immune insulin resistance
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immediate type hypersensitivity, rare condition
insulin allergy
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disorder where low titer IgG anti insulin antibodies neutralize the action of insulin
immune insulin resistance
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abnormal or degenerative conditionof the body's adipose tissue
Lipodystrophy
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oral anti diabetic agents
```
Secretagogues
BIGuanides
Thiazolidinediones
Alpha-glucosidase inhibitors
Incretin based therapies
Amylin analogs
```
46
insulin secretagogues
Sulfonylureas
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sulfonylureas MOA
increase insulin release
reduce serum glucagon levels
closure of K channels in extrapancreatic tissure
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first generation of Sulfonylureas
Tolbutamide
Chlorpropamide
Tolazamide
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safest sulfonylureas for elderly diabetics, short halflife
TOLBUTAMIDE
| rapidly metabolized in liver
50
first gen sulfonylurea prolonged hypoglycemic reactions
Chlorpropamide
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ADR of CHLORPROPAMIDE if given >500mg daily
Jaundice
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more slowly absorbed than other sulfonylureas
half life: 7hours
duration: 10-14 hours
TOLAZAmide
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Second generation sulfonylureas
Glyburide (aka Glibenclamide)
gLIPizide
gLIMEpiride
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Second gen sulfonylureas used with caution on Px with CV DISEASE and the ELDERLY
gLIMEpiride
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2nd gen sulfonylurea with very loew hypoglycemic effect
Glyburide (aka Glibenclamide)
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dose of Glyburide (aka Glibenclamide)
starting dose: 2.5mg/day
| maintainance: 5-10 mg/day
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contraindicated in Glyburide (aka Glibenclamide) therapy
hepatic and renal impairment
| alcohol intake
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ADR of Glyburide (aka Glibenclamide) with alcohol intake
Flushing
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2nd gen sulfonylurea with delayed absorption when taken with food (take 20min before breakfast)
gLIPizide
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2nd gen sulfonylurea single dose 1mg use as MONOTHERAPY or in combination with insulin
gLIMEpiride
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1st member of MEGLITINIDE group of insulin secretagogue
REPAglinide
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Used for controlling pstprandial glucose excursion
REPAGLINIDE
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latest insulin secretagogue available clinically
NATEGLINIDE
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insulin secretagogue D phenylalanine derivative
NATEGLINIDE
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stimulates very rapid insulin release from beta cells thru CLOSURE of ATP-sensitive K channel
NATEGLINIDE
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Nateglinide metabolism
via liver CYP2C9 and CYP3A4
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reduces glucose production thru AMPK
BIGuanides
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BIGuanide minor MOA
IMPAIR renal gluconeogenesis, SLOWS GIT glucose abs
direct stimulation of glycolysis in tissues
INCREASE glucose removal in blood
REDUCE glucagon
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first line therapy for DM type 2
METFORMIN
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insulin sparing drug
METFORMIN
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METFORMIN dosage
500mg to 2.55g daily
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METFORMIN toxicity
```
GIT disorders (anorexia, NV, abd pain, diarrhea)
DECREASE vit B12 abs
```
73
METFORMIN contraindication
renal, hepatic disease, alcoholism
| predispose to ANOXIA ( bec inc risk of LACTIC ACIDOSIS)
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they act to decrease insulin resistance
THIAZOLIDINEDIONE
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major site of THIAZOLIDINEDIONE
adipose tissue
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In, THIAZOLIDINEDIONE ligands of peroxisomes proliferatior activates what receptor?
Receptor GAMMA
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current available THIAZOLIDINEDIONE
PIOglitazone
| ROSIglitazone
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other THIAZOLIDINEDIONEs pulled from the market due to LIVER TOXICITY
TROglitazone
| REZULIN
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insulin sensitizer THIAZOLIDINEDIONE
PIOglitazone
80
attaches to insulin receptors throughout the body
PIOglitazone (insulin sensitizer!)
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rapidly absorbed and highly protein bound THIAZOLIDINEDIONE
ROSIglitazone
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not recommended for type 1 DM
| MONOTHERAPY for type 2 DM
ROSIglitazone
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ROSIglitazone adverse effects
```
Fluid retention (presented as MILD ANEMIA, EDEMA)
Bone fracture (decrease osteoblast formation)
```
84
alpha glucosidase inhibitors
ACARBOSE
| MIGLITOL
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competitive inhibitors of of intestinal Alpha GLUOSIDASES
ACARBOSE
| MIGLITOL
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Alpha GLUOSIDASES moa
reduces post meal glucose excursions
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sugars that can only be transported out of the GIT
glucose and fructose
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Alpha GLUOSIDASES with side effect of FLATULENCE and DIARRHEA
ACARBOSE
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Synthetic analog of AMYLIN
PRAMLINTIDE
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hyperglycemic agent modulates POST PRANDIAL GLUCOSE LEVEL
| rapidly absorbed SQ admin
PRAMLINTIDE
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synthetic analog of Glucagon-like polypeptide 1 (GLP-1 agonist)
Exenatide
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1st INCRETIN therapy for Diabetes
EXENATIDE
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Adjunctive therapy in persons with type 2 DM
EXENATIDE
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EXENATIDE moa
```
potentiation of INSULIN SECRETION
supression of POSTPRANDIAL GLUCAGON release
DECREASE gastric emptying
REDUCE appetite
REDUCES liver fat content
```
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EXENATIDE adr
Nausea, vomiting, diarrhea
| risk for THYROID CA, ACUTE PANCREATITIS
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inhibitor of dipeptidyl petidase 4 (DPP-4)
SITAglipin
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SITAglipin MOA
increase GLP-1 and GIP
| decreases post prandial glucose excusion
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SITAglipin common side effects
Nasopaharyngitis, URTI, headaches
99
other DPP4 inhibitors
SAXAgliptin
LINAgliptin
ALOgliptin
VILDAgliptin
100
What do you give in combination therapy?
Initial therapy: BIGuanide
| 2nd line: Sulfonylureas or insulin (cost-efficient) ; EXENATIDE (aggressive control)
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for concurrent mealtime administration in type 2 DM for early post prandial glucose excursion
combination therapy with PRAMALINTIDE
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for adjunct to oral anti diabetic therapy in type 2 DM
Bedtime insulin
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NOT approved for Tx of type 1 DM
insulin secretagogues, Tzds, biguanides, alpha glucosidase and incretin
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insulin secretagogues
Sulfonylureas, Meglitidines, D phenylalanine derivatives
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For concurrent meal time administration with type 1 DM who have POOR control despite optimal insulin therapy
Combination therapy with PRAMLINTIDE
106
synthesized in alpha cells of pancreas, degraded in liver and kidney
Glucagon
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GLUCAGON is a precursor intermmediate of 69 AA peptide called
GLUCENTIN
108
Glucentin immuno reactivity found in small intestine and alpha cells
Gut Glucagon
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predominant form of GLP in human intestine
glucagon like peptide GLP-1
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potential therapeutic agent in type 2 D
GLP-1 aka INSULINOTROPIN
111
Metabolic effects of glucagon
increase gluconeogenesis and ketogenesis
112
clinical uses of glucagon
```
severe hypoglycemia (for emergency)
endocrine diagnosis
beta adrenoceptor blocker overdose
radiation of bowel
```
113
glucagon adverse reactions
NV
114
drug interaction with glucagon which result to greater risk of bleeding
WARFARIN
115
standard mode of insulin therapy
SQ
