Professional Documents
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Anti Diabetic Medications
Anti Diabetic Medications
Anti Diabetic Medications
Type 2 Diabetes
High blood glucose Impaired GI motility
2. Overproduction of glucagon 1. Tissues less sensitive to insulin 2. Liver produces excess glucose
Image Obtained From: Diabetes 101: Overview of Drug Therapy by Jennifer Danielson, RPh, CDE
Biguanides
Metformin
Biguanides
Metformin Indication Type II Diabetes Mellitus, Antipsychotic-induced weight gain MOA Decrease hepatic glucose production, decrease intestinal absorption of glucose and increase insulin sensitivity therefore increasing peripheral glucose uptake Depends upon Power Dosing Presence of insulin Decreases HbA1c 1% to 2% One to three times daily Glucophage Glucophage XR 500, 850, 1000 mg 500, 750 mg XR tablets tablets
Biguanides
Patient Info N/V/D Upset stomach/dyspepsia take with food Metallic taste Minimal Weight Loss Alcohol may increase likelihood of lactic acidosis Does not cause hypoglycemia
Biguanides
Special Population Considerations: Geriatric: limited data suggests starting doses should be 33% lower for geriatric patients than that of an adult dose. Titration should also to a lower limit. Cautions/Severe Adverse Reactions Black Box Lactic Acidosis: D/C immediately and notify practitioner if: myalgia, malaise, hyperventilation, unusual somnolence. Alcohol potentiates this reaction. Advise patients not to consume excessive amounts of alcohol.
Biguanides
CONTRAINDICATIONS Renal disease or renal dysfunction (Scr > 1.5 mg/dL in males, >1.4 mg/dL in females) Abnormal Scr from any cause including: shock, acute MI, or septicemia Metabolic acidosis (including diabetic ketoacidosis (DKA)) Heart failure requiring pharmacologic therapy; active liver failure
Sulfonylureas
Tolbutamide
Acetohexamide
Tolazamide
Chlorpropamide
Sulfonylureas
Glyburide
Glipizide
Glimepiride
Sulfonylureas
Glimepiride Glipizide Glyburide Amaryl Diamicrom, Diamicrom XL) (DiaBeta) 1, 2, 4 mg (2.5), 5, 10 mg (XL) 1.25, 2.5, 5 mg tablets tablets tablets
Indications Adjuncts to diet and exercise to lower blood glucose in patients w/ type II diabetes mellitus MOA Stimulating insulin release from beta-cells of pancreatic islets Onset glucose lowering effect: 30 minutes with peak at 1.5-3 hours lasting 24 hours
Sulfonylureas
SU
sulphonylurea receptor
KATP channel
pancreatic beta cell insulin
SU
membrane depolarisation
SU
Ca2+ calcium entry Ca2+ insulin insulin secretion insulin
Sulfonylureas
Adverse Effects
Contraindications
Hypoglycemia Nausea and vomiting Cholestatic jaundice Agranulocytosis Anemia Hypersensitivity Dermatological rxns Drug interactions Dizziness Weight gain
Sulfonylureas
Special Population Considerations: Pediatric: safety and efficacy not established for pts under age 16 Hepatic/Renal Dysfunction: conservative dosing and titration recommended. Caution/Severe Adverse Reactions Syndrome of Inappropriate Anti-diuretic Hormone (SIADH)
Indications Diabetes Mellitus Type II MOA Inhibits the breakdown of GLP-1 by DPP-4 therefore increasing GLP-1 levels resulting in increased glucose-dependent insulin release and decreased level of circulating glucagon and hepatic glucose production
Dipeptidyl Peptidase-4 (DPP-4) Inhibitors Patient Info N/V Hypoglycemia Weight neutral Nasopharyngitis/URI Headache Onset: Reduction in postprandial serum glucose: 60 minutes
It is 97% similar to endogenous GLP-1 (7-37). It provides powerful and sustained reductions in A1C for adults with type 2 diabetes and has direct and indirect effects in multiple organ systems that affect glucose homeostasis
It slows gastric emptying It reduces glucagon secretion, helping to lower hepatic glucose output from the liver It impacts beta-cell function and improves insulin secretion in the pancreas Structural modifications increase the stability against DPP-4 and promote plasma protein binding. 13-hour half-life because an amino acid substitution and a fatty acid attachment make it stable against degradation by DPP-4. suitable for once-daily administration.
Thiazolidinediones (TZD)
Pioglitazone Rosiglitazone (Actos) (Avandia) 15, 30, 45 mg 2, 4, 8 mg tablets tablets
Indications As adjunct to diet and exercise for type II diabetes MOA Increase insulin sensitivity by affecting PPAR- (peroxisome proliferators-activated receptor) at adipose tissue, skeletal muscle and in the liver. Special Alert February 2011: Addition of Risk Evaluation and Mitigation Strategy to rosiglitazone. The medication is restricted to those patients already on rosiglitazone for fails pioglitazone or cannot be managed by other oral antidiabetic medications.
TZD (cont)
Patient Info Weight gain Edema Hypoglycemia esp. when used with other antidiabetic medications and insulin (not w/ metformin) May cause or exacerbate heart failure with risk of fluid retention URI, sinusitis, pharyngitis Myalgia Headache
TZD (cont)
Cautions/Severe Adverse Reactions Black Box: Heart Failure (for all thiazolidinediones, mainly due to rosiglitazone) Hepatic failure Anemia Bone loss Ovulation in premenopausal women Pregancy Cat: C
TZD (cont)
Special Populations Considerations: Congestive Heart Failure: should be initiated at lowest approved dose with longer intervals between dose increases for NYHA class II. Use is not recommended in patients with NYHA Class III or IV CHF CONTRAINDICATIONS NYHA Class III-IV heart failure Active liver disease (ALT > 2.5 upper limit of normal)
Insulin
Indications Type I diabetes mellitus, type II diabetes mellitus, hyperkalemia, DKA/diabetic coma MOA Stimulating peripheral glucose uptake and inhibiting hepatic glucose production Patient Info Hypoglycemia (BG < 70 mg/dL) esp with higher doses Anxiety, blurred vision, palpitations, shakiness, slurred speech, sweating Weight gain
Insulin (cont)
Administration: Subcutaneous injection Rotate site Check blood sugars regularly Storage: Refrigerate until use Once vial is punctured, it is good for 28 days and can be left at room temperature (except for glargine which is 90 days)
Insulin (cont)
Dosing: Starting daily dose: 0.5-1 unit/kg/day in divided doses Adjust according to fasting (premeal) blood glucose of 80-130 mg/dL and peak postprandial blood glucose < 180 mg/dL Provide 50% as long acting insulin and 50% as prandial insulin 1 unit of can account for 30 grams of carbohydrate (14-50) 1 unit can lower 50 mg/dL blood glucose (10-100) Special Population Consderations: Renal dysfunction
CrCl 10-50 mL/min: 75% of normal dose CrCl < 10 ml/min: 25-50% of normal dose; monitor closely
Insulin Action
Rapid/immediate
Blood concentration
Intermediate
Fast Slow
10
12
14
16
18
20
22
24
Time (hr)
Insulin Dosing
Long-acting
Insulin Administration
Pharmacology for Technicians by Ballington, Lauglin. EMC Paradigm 2006, Fig. 14.9
Insulin (cont)
Cautions/Severe Adverse Reactions Severe hypoglycemia (seizure/coma) (BG < 40 mg/dL) Edema Lipoatrophy or lipohypertropy at injection site CONTRAINDICATIONS Severe hypoglycemia Allergy or sensitivity to any ingredient of the product
courses.washington.edu/pharm504/Insulin%20Chart.pdf
Hypoglycemia
Complication of treatment! Make sure patients inform the people around them of these symptoms and what to do! Symptoms: Anxiety, blurred vision, palpitations, shakiness, slurred speech, sweating Treatment: glucose/simple sugars: 3-4 glucose tablets, can of soda (NOT diet!) Treatment: glucagon injection
Smoking cessation Regular Screening for Cardiovascular Diseases and Coronary Artery Disease Depression/Stress/Anxiety/Other psychosocial conditions need to be screen for regularly Diabetic neuropathies especially in extremities need to be screened for on a regular basis