Antidiabetic Drugs Flashcards
In which type of diabetes does the patient not secrete insulin?
Type 1
Which type of diabetes is an autoimmune disease?
Type 1
In which form of diabetes are the insulin receptors desensitized?
Type 2
Which form of diabetes is genetic?
Type 2
Which form of diabetes is associated with obesity?
Type 2
In which form of diabetes is the patient prone to ketogenesis?
Type 1
Hyperglycemia causes vascular, neural, and ocular damage. The neural and ocular damages are caused by an accumulation of what?
Sorbitol
Concerning canine (porcine) insulin, A = ___ aa.
A = 21 aa
Concerning canine (porcine) insulin, B = ____ aa.
B = 30 aa
How are the A and B chains connected in canine (porcine) insulin?
Via 2 disulfide bonds
What is proinsulin?
Insulin + C-peptide
What are the 3 stimulators of insulin secretion?
- Glucose
- Calcium, cyclic AMP
- GI hormones (gastrin, secretin, cholescystokinin, glucagon)
What are the inhibitors of insulin secretion?
Somatostatin and alpha-adrenergic agonists
How do beta2 adrenergic agonists affect insulin secretion?
Stimulate secretion
How do alpha2 adrenergic agonists affect insulin secretion?
Inhibit secretion
How do cholinergic agonists affect insulin secretion?
Stimulate secretion
How does glucose stimulate insulin release?
Glucose –> ATP –> blocks K+ channels –> decreased K+ efflux –> increased intracellular K+ –> depolarization –> open Ca2+ channels –> influx of Ca2+ –> increase in insulin exocytosis
In addition to glucose, what else blocks K+ channels?
Sulfonylurea
What are the 2 actions of insulin?
- To conserve energy
2. To increase glucose transport into cells
What are the 4 effects of insulin on carbohydrate metabolism?
- Decreased gluconeogenesis
- Decreased glycogenolysis
- Increased glucagon synthesis
- Increased glucose transport into striated muscle and adipose tissue
What is the effect of insulin on lipid metabolism?
Increased lipid synthesis, decreased lipolysis
What is the effect of insulin on protein metabolism?
Increased uptake of amino acids into cells, increased protein synthesis
What is the effect of insulin of K+ metabolism?
Increases Na+/K+ - ATPase activity, leading to increased K+ intracellularly
What is the half life of insulin in the plasma?
9 minutes
Where is insulin destroyed?
- Liver
2. Kidney
What is closest to feline insulin?
Bovine insulin
True or False: Canine and porcine insulin are identical.
TRUE
What is the term used to describe the following: not crystallized?
Amorphous
What is the term used to describe the following: large crystals slowing down absorption, and thus increasing the duration of action?
Crystalline
What is the term used to describe the following: an aid in crystallization?
Zinc
What is the term used to describe the following: a basic protein to form an insulin complex?
Protamine
What is a diluted protamine solution?
Isophane
What is the time of onset for rapid-acting insulin preparations?
5-15 minutes
What is the duration of action of rapid-acting?
2-4 hours
What is the onset of action of short-acting?
> 1 hour
What is the duration of action of short-acting?
5-8 hours
What is the onset of action of intermediate-acting?
2 hours
What is the duration of action of intermediate-acting?
18-24 hours
What is the onset of action of long-acting?
2-7 hours
What is the duration of action of long-acting?
36 hours
Into which class would you place “Insulin Injection (Regular)” such as HumulinR?
Short-acting
Into which class would you place “Insulin Lispro”?
Rapid-acting
Insulin Lispro:
B___ = ___
B28 = Lys
Insulin Lispro:
B___ = ___
B29 = Pro
Into which class would you place “Insulin Aspart”?
Rapid-acting
Insulin Aspart:
B___ = ___
B28 = Asp
Into which class would you place “Isophane insulin suspension” such as HumulinN?
Intermediate-acting
Into which class would you place “Insulin zinc suspension” such as Vetsulin?
Intermediate-acting
What are the 4 classes of long-acting insulin preparations?
- Protamine zinc insulin
- Insulin extended zinc suspension (HumulinU)
- Insulin glargine
- Insulin detemir
With Insulin Glargine, where are Gly and Arg located?
Gly = A21
Arg = B31, B32
With Insulin Detemir, where is Lysine located?
B29
How are Insulin Glargine and Insulin Detemir administered?
SQ
Which is bound to albumin upon SQ injection, Insulin Glargine or Insulin Detemir?
Insulin Detemir
What are the 5 causes of false insulin resistance?
- Owner can’t give injection
- Injected into the same spot
- Over eating
- Inactive insulin
- Insulin overdose
How do Sulfonylureas stimulate insulin secretion?
Block K+ channels –> increased intracellular K+ –> depolarization –> open Ca2+ channels –> increased intracellular Ca2+ –> insulin exocytosis
What is Biguanide?
An anti-hyperglycemic agent
What is the mechanism of action of Biguanide?
- Decreased gut glucose absorption
- Decreased hepatic glucose output
- Increased glucose utilization by increasing sensitivity to insulin
What is the mechanism of action of pioglitazone?
- Increased insulin receptor sensitivity by activating nuclear receptors (PPARs)
- Increase proteins and enzymes involved in insulin actions (GLUT4)
What is the mechanism of action of SGLT2 inhibitors?
Block reabsorption of glucose from proximal tubules by Na-glucose transporter 2
What is an example of one SGLT2 inhibitor?
Gliflozins
What are the 2 advantages of Glifozins?
- Oral administration
2. No hypoglycemia
What are the 3 disadvantages of Glifozins?
- Increased PU/PD
- Sodium loss
- UTIs