Flashcards in Pancreatic Hormones & Diabetic Drugs Deck (57)
Loading flashcards...
1
Which diabetes has more of a genetic predisposition
Type II
2
Which diabetes has insulin deficiency
Type 1
3
Which diabetes has a loss of beta cells
Type 1
4
Which diabetes is more prone to ketoacidosis
Type 1
5
Which diabetes is prone to a non-ketototic hyperosmolar coma
Type II
6
K+/ATP and Insulin:
Open state of K+/ATP channel
hyperpolarize the cell by causing outflow of K+ and inhibit insulin release
7
K+/ATP and Insulin:
Closed state of K+/ATP channel
depolarize the cell and insulin released.
8
Insulin Receptor signaling:
insulin binding to alpha subunit regulates beta subunit activity -->
autophosphorylation of beta subunit -->
increase tyrosine kinase activity -->
phosphorylation of other substrates -->
activation of phosphoinositide 3-kinase
9
Effects of insulin on the liver
Stimulates:
- glycogen synthesis
- triglyceride synthesis
Inhibits:
- glycogenolysis
- ketogenesis
- gluconeogenesis
10
Effects of insulin on skeletal muscle
Stimulates:
- glucose uptake
- protein synthesis
- glycogen synthesis
Inhibits:
- Protein degradation
- Glycogenolysis
11
Effects of insulin on adipose tissue
Stimulates:
- Glucose uptake
- Triglyceride storage
Inhibits:
- lipolysis
12
Overall, insulin stimulates ____and inhibits ____
Promotes anabolic processes and
Inhibits catabolic processes
13
advantages to recombinant DNA insulin
• Less insulin resistance
• Less allergy
• Less lipodystrophy
14
Rapid/ short-acting insulin:
onset and duration
Onset: 5-15 min
Duration: 3-5 h
15
Rapid insulin
• Insulin lispro, aspart, glulisine given s.c
• Inhaled human insulin - Indicated only in adults,
• Contraindicated- children, asthma, bronchitis, smokers
16
short-acting insulin
• duration
• what? method given?
• use?
• Duration: 5-8h
• Regular insulin given s.c and i.v.
• Use in diabetic ketoacidosis and other emergency situations
17
intermediate-acting insulin:
• onset
• duration
• what?
•
• onset: 2-5h
• duration: 4-12h
• Lente insulin, NPH insulin (Neutral protamine Hagedorn or isophane) mixture of insulin with protamine (basic substance obtained from fish sperm)
18
Ultra-long acting insulin
• onset
• duration
• what?
• onset: slow
• duration: 20-24h
• Ultra lente, Insulin glargine, Insulin detemir
• Peakless, given once daily
19
Hypoglycemia
• S/Sx
• Tx
• Sympathetic signs (tachycardia, sweating, palpitations, tremors) parasympathetic signs (nausea, hunger)
• Treatment : Glucose or glucagon treatment
20
Allergy and resistance to insulin
• Local cutaneous reactions or systemic
• Human insulin are less antigenic than insulin from animal sources
21
lipodystrophy
• Atrophy of fatty tissue at the site of injection
• Never seen since the development of highly purified insulin
22
Treatment of Type II DM includes
• Diet
• Exercise
• Wt reduction
• Step wise approach to drug treatment
• Patient education
➢ Oral drugs for reduction of blood glucose
• Used only in the Rx of Type II DM
• Oral medication is initiated when 2-3 months of diet and exercise alone are unable to achieve or maintain their optimal plasma glucose levels
23
Insulin secretogogues
• Sulfonyureas
• Meglitinides
24
Oral Hypoglycemics
1. Insulin secretogogues
• Sulfonyureas
• Meglitinides
2. Biguanides
3. Thiazolidinediones
4. Alpha glucosidase inhibitors
25
First Generation Sulfonylurea
• Chlorpropramide
• Tolbutamide
• Tolazamide
26
2nd Generation Sulfonuylurea
• Glipizide
• Glyburide
• Glimepiride
27
Mechanism of action of Sulfonylurea
• Block ATP sensitive K+ channels in pancreatic beta cells --> Inhibits the efflux of K+ resulting in depolarization
• Opening of voltage gated Ca influx --> release of preformed insulin -->
• Increase the sensitivity to insulin by increasing number of insulin Receptors
28
Chloropropamide (Diabinese)
• Long acting for 32 hours
• Can cause prolonged hypoglycemia in elderly patients (contraindicated age)
• Slowly metabolised in liver, so Contraindicated in patients with hepatic disease
29
Tolbutamide (Orinase)
• Rapidly metabolised in liver
• Short half life - safest SU in elderly
30
