nrsg351 agents to treat diabetes
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Civility Clause….Students are expected to behave toward lecturers and fellow students with courtesy and consideration. This means that talking and disruptive behavior will be kept to a minimum. Cell phones, pagers, and other electronic devices should be silenced in the classroom. I reserve the right to end a class at any time, for any reason, including the disruptive or rude behavior of anyone in the classroom.
Starting with insulin
Figure 3 The feedback loops of the insulin axis involve a number of different tissues.
Maloney C A , and Rees W D Reproduction 2005;130:401-410
© 2005 Society for Reproduction and Fertility
Goals of therapy in diabetes
• To normalize blood sugar levels to minimize risk of long-term complications
• To avoid instances of hypoglycemia• To promote normal carbohydrate, fat and
protein metabolism
Non-insulin drugsInsulins
Drugs for diabetes
biguanides
secretagogues
sulfonylureas meglitinides
-glucosidaseinhibitors
TZDs
amylinanalogues
incretinmodulators
GLP-1analogues
DPP-4inhibitors
Others
Therapy with insulin
• Insulin is the PRIMARY treatment for Type 1 diabetes – insulin administration replaces insulin that is not produced by B cells
• Also used in Type 2 as B cells fail and disease progresses
Therapy with insulin
• USED TO TREAT– Type I or type 2 diabetes
• CONTRAINDICATED IN– Allergy to a specific insulin product– hypoglycemia
Types of insulin
• Ultra short acting or rapid acting– Rapid onset, short duration
• Short-acting– Rapid onset
• Intermediate-acting• Long-acting
– Slow onset
Insulins Insulin aspart (Novolog®) - CInsulin lispro (Humalog®) - BInsulin glulisine (Apidra®) - C
Pharmacology (Mechanism of action)
Replaces insulin;
Promotes cellular uptake of glucose, fatty acids and amino acids;
Promotes storage of glycogen, triglycerides and proteins
Adverse Effects Pharmacokinetics
Insulins Regular insulin (Humulin-R®, Novolin-R®)
Pharmacology (Mechanism of action)
Replaces insulin;
Promotes cellular uptake of glucose, fatty acids and amino acids;
Promotes storage of glycogen, triglycerides and proteins
Adverse Effects Pharmacokinetics
Insulins Isophane insulin suspension (NPH®, Novolin-N®, Humulin-N)
Insulin zinc suspension (Lente) (Humulin-L®; Novolin-L®)
Pharmacology (Mechanism of action)
Replaces insulin;
Promotes cellular uptake of glucose, fatty acids and amino acids;
Promotes storage of glycogen, triglycerides and proteins
Adverse Effects Pharmacokinetics
Insulins Insulin glargine (Lantus®)Insulin detemir (Levemir®)
Pharmacology (Mechanism of action)
Replaces insulin;
Promotes cellular uptake of glucose, fatty acids and amino acids;
Promotes storage of glycogen, triglycerides and proteins
Adverse Effects Pharmacokinetics
Insulins - MixturesNPH70% + regular insulin 30% (Humulin 70/30 ®; Novolin 70/30®)NPH50% + regular insulin 50% (Humulin 50/50®)
Insulin lispro protamine suspension 75% + insulin lispro 25% (Humalog Mix 75/25®)
Pharmacology (Mechanism of action)
Replaces insulin;
Promotes cellular uptake of glucose, fatty acids and amino acids;
Promotes storage of glycogen, triglycerides and proteins
Adverse Effects Pharmacokinetics
http://forecast.diabetes.org/files/images/InsulinChart_4.pdf
Adverse Effects of Insulin
• Hypoglycemia– Sympathatic activation produces palpitations,
sweating, nervousness, weakness– Serious hypoglycemia produces CNS effects,
including mental confusion, incoherent speech, blurred vision, coma
• Weight gain
Role of the nurse (Abrams, pp. 726-730)
• Teach the patient how to administer insulin correctly– Choice of administration techniques– Using a syringe– Choice of injection sites– When and how often to inject– How to store
Non-insulin drugsInsulins
Drugs for diabetes
biguanides
secretagogues
sulfonylureas meglitinides
-glucosidaseinhibitors
TZDs
amylinanalogues
incretinmodulators
GLP-1analogues
DPP-4inhibitors
Others
SulfonylureasGlyburide (Diabeta®, Micronase®)Glipizide (Glucotrol®) Glimepiride (Amaryl®)
Pharmacology (Mechanism of action)
Stimulate insulin release from the pancreas;
Increases the number and sensitivity of insulin receptors;
Decreases glycogenolysis and gluconeogenesis
Adverse Effects Pharmacokinetics
K+
B cellbasal state
insulin
glucose
K+
Sulfonylureas
• Inhibits (closes) a K+-ATP channel, leading to• Decreased K+ efflux from B-cells which• Depolarizes the B-cell membrane, leading to• Increased Ca++ influx and• Increased exocytosis of insulin from B-cells
glipizide
sulfamethoxazole
Sulfonylureas
• Serious adverse effects– Hypoglycemia– Hematological effects (thrombocytopenia, aplastic
anemia, others)
• Common adverse effects– Weight gain– Rash– Hypoglycemia
Biguanidesmetformin (Glucophage®)
metformin / glipizide (Metaglip®) rosiglitazone / metformin (Avandamet®)Others….
Pharmacology (Mechanism of action)
Decrease hepatic glucose production;
Decrease glucose absorption from GI tract;
Increases insulin receptor sensitivity
Adverse Effects Pharmacokinetics
Biguanides
• USED TO TREAT– Type 2 diabetes
• CONTRAINDICATED IN– Hypersensitivity to biguanides– Hepatic or renal disease– Alcoholism– Cardiopulmonary disease
Biguanides
• Serious adverse effects– Lactic acidosis (due to the inhibition of
gluconeogenesis and the buildup of fatty acids) - rare
• Common adverse effects– Nausea, vomiting– Flatulence
Thiazolidinediones (Insulin Sensitizers; glitazones; TZDs)Rosiglitazone (Avandia®) - CPioglitazone (Actos®) - C
Pharmacology (Mechanism of action)
Enhances the effects of circulating insulin;
Stimulates peripheral glucose uptake and storage
Inhibits hepatic glucose production
NO increase in insulin levels
Adverse Effects Pharmacokinetics
http://www.fda.gov/Drugs/DrugSafety/ucm255005.htm
Thiazolidinediones (TZDs)• Serious adverse effects
– Congestive heart failure (new or exacerbated) due to increasing blood volume –
BLACK BOX WARNING– Hepatic dysfunction or failure
• Common adverse effects– Mild anemia– Moderate weight gain– Upper respiratory infection– Headache and myalgia
Secretagogues (meglitinides)Repaglinide (Prandia®)Nateglinide (Starlix®)Pharmacology (Mechanism of action)
Stimulates insulin release from B-cell through inhibition of ATP-sensitive K+ channels;
Adverse Effects Pharmacokinetics
Alpha-glucosidase inhibitorsAcarbose (Precose®)
Pharmacology (Mechanism of action)
Reversibly inhibit alpha glucosidase
Delays absorption of glucose in the intestine;
Blunts postprandial elevations in glucose
Adverse Effects Pharmacokinetics
Glucagon-like peptide 1 (GLP-1)Exenatide (Byetta®; Bydureon®) – CLiraglutide (Victoza®)Pharmacology (Mechanism of action)
Incretin mimetic that binds to GLP receptors;
Increases glucose-dependent secretion of insulin from pancreatic B cells
Adverse Effects Pharmacokinetics
Injected sc
Synthetic amylin analogpramlintide (Symlin®)
Pharmacology (Mechanism of action)
Amylin slows gastric emptying;
suppresses glucagon;
Modulates appetite in the CNS
Adverse Effects Pharmacokinetics
Injected sc
DPP-4 inhibitorSitagliptin (Januvia®)Saxagliptin (Onglyza®)Pharmacology (Mechanism of action)
Inhibits DPP-4, which slows inactivation of incretin hormones GLP-1 and GIP
Adverse Effects Pharmacokinetics
Oral
Figure 1. Key sites of action of diabetes medications.
Martin C L The Diabetes Educator 2007;33:6S-13S
Copyright © by American Association of Diabetes Educators; Published by SAGE Publications
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