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Antidiabetic Medications: Pharm 585 February 15, 2011 Hy N Dang
Antidiabetic Medications: Pharm 585 February 15, 2011 Hy N Dang
Goal
To understand the use and side effects of antidiabetic medications and be able to educate patients.
Nine to Know
The minimum that every pharmacist must know about drugs!
Brand & Generic Name Mechanism of action Therapeutic effect Relevant pharmacokinetics and pharmacodynamics Dosing by route Adverse reactions and contraindications Monitoring parameters Drug-drug and drug food interactions Comparisons between agents w/in the same class of drugs
Contraindications/Cautions/Adver se Reactions
Adverse Reactions
Unwanted side effects: need to warn patient Warnings for clinicians to be aware when using medication. Conditions which will render the medication absolutely unusable in that patient population
Cautions
Contraindications
Type 2 Diabetes
High blood glucose Impaired GI motility
2. Overproduction of glucagon
Image Obtained From: Diabetes 101: Overview of Drug Therapy by Jennifer Danielson, RPh, CDE
Biguanides
Metformin Glucophage (Glucophage XR) 500, 850, 1000 mg 500, 750 mg XR tablets tablets
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
Image Obtained From: Diabetes 101: Overview of Drug Therapy by Jennifer Danielson, RPh, CDE
Biguanides (cont)
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 (cont)
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 (cont)
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
Saxagliptin/metformin
(Kombiglyze XR)
tablets
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
Image Obtained From: Diabetes 101: Overview of Drug Therapy by Jennifer Danielson, RPh, CDE
DPP-4 (cont)
Patient Info N/V Hypoglycemia Weight neutral Nasopharyngitis/URI Headache Onset: Reduction in postprandial serum glucose: 60 minutes
DPP-4 (cont)
Special Population Considerations: Renal Impairment: avoid combo drugs w/ metformin For sitagliptin: CrCl 30-50 mL/min : 50 mg daily CrCl < 30 mL/min: 25 mg daily End Stage Renal Disease Requiring dialysis: 25 mg daily Geriatric: caution due to age related renal function decreases Cautions/Severe Adverse Reactions Acute pancreatitis Rash (Stevens-Johnson syndrome)
Sulfonylureas
Glimepiride Glipizide Glyburide 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 (Amaryl) (Glucotrol, Glucotrol XL) (DiaBeta) 1, 2, 4 mg (2.5), 5, 10 mg (XL) 1.25, 2.5, 5 mg tablets tablets tablets
Image Obtained From: Diabetes 101: Overview of Drug Therapy by Jennifer Danielson, RPh, CDE
Sulfonylureas (cont)
Patient Info
Hypoglycemia GI upset/abdominal pain Dizziness Weight gain Heartburn/epigastric fullness Possible disulfiram-like reaction with alcohol (mainly w/ glyburide) Onset: glucose lowering effect: 30 minutes with peak at 1.5-3 hours lasting 24 hours
Sulfonylureas (cont)
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) CONTRAINDICATIONS Diabetes complicated by ketoacidosis Type I DM Diabetes w/ pregnancy. Pregnancy Cat: C (except glyburide: B)
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.
Image Obtained From: Diabetes 101: Overview of Drug Therapy by Jennifer Danielson, RPh, CDE
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
Image Obtained From: Diabetes 101: Overview of Drug Therapy by Jennifer Danielson, RPh, CDE
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
Cardiovascular disease/Hypertension Systolic blood pressure goal < 130 mm Hg Angiotensin Converting Enzyme II Inhibitor (ACE-I) is first line Renal protective Angiotensin Receptor Blockers (ARB) can be used if patient fails or is intolerant to ACE-I
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