anti diabetic medications
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Antidiabetic Medications
High blood glucose
1. Defective beta cell functionDiminished phase 1 insulin releaseDelayed phase 2 insulin release
2. Overproduction of glucagon
Impaired GI motility
1. Tissues less sensitive to insulin2. Liver produces excess glucose
Type 2 Diabetes
Image Obtained From: Diabetes 101: Overview of Drug Therapy by Jennifer Danielson, RPh, CDE Type 2 Video from diabetes.com
Metformin
Biguanides
Biguanides
Metformin Glucophage 500, 850, 1000 mg tablets
Glucophage XR 500, 750 mg XR 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
Depends upon Presence of insulin
Power Decreases HbA1c 1% to 2%
Dosing One to three times daily
Biguanides
Patient InfoN/V/DUpset stomach/dyspepsia – take with foodMetallic tasteMinimal Weight LossAlcohol may increase likelihood of lactic acidosisDoes 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 ReactionsBlack 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
CONTRAINDICATIONSRenal 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 septicemiaMetabolic acidosis (including diabetic ketoacidosis (DKA))Heart failure requiring pharmacologic therapy; active liver failure
Sulfonylureas
Tolbutamide Acetohexamide
ChlorpropamideTolazamide
Glyburide
Glimepiride
Glipizide
Sulfonylureas
Glimepiride Amaryl 1, 2, 4 mg tablets
Glipizide Diamicrom, Diamicrom XL)
(2.5), 5, 10 mg (XL)
tablets
Glyburide (DiaBeta) 1.25, 2.5, 5 mg tablets
Indications Adjuncts to diet and exercise to lower blood glucose in patients w/ type II diabetes mellitusMOAStimulating insulin release from beta-cells of pancreatic isletsOnset glucose lowering effect: 30 minutes with peak at 1.5-3 hours lasting 24 hours
Sulfonylureas
Sulfonylureas
SU
SU
sulphonylurea receptor
KATP channel
KATP channel closes
membrane depolarisation
calcium entryinsulin secretion
Ca2+
Ca2+
insulin
insulin
insulin
pancreaticbeta cell
SU
Sulphonylureas allow for insulin release at lower glucose threshold
Adverse Effects– Hypoglycemia– Nausea and
vomiting– Cholestatic jaundice– Agranulocytosis– Anemia– Hypersensitivity– Dermatological rxns– Drug interactions– Dizziness– Weight gain
Contraindications– Type I diabetes– Pregnancy/
lactation– Hepatic/renal
failure– Diabetes
complicated by ketoacidosis
Sulfonylureas
Special Population Considerations:Pediatric: safety and efficacy not established for pts under age 16Hepatic/Renal Dysfunction: conservative dosing and titration recommended.
Caution/Severe Adverse ReactionsSyndrome of Inappropriate Anti-diuretic Hormone (SIADH)
Sulfonylureas
Dipeptidyl Peptidase-4 (DPP-4) Inhibitors
Vildagliptin Galvus 50 mg tablets
Vildagliptin/metformin Galvusmet 50/500, 50/1000 mg
tablets
Sitagliptin (Januvia) 25, 50, 100 mg tablets
Sitagliptin/metformin (Janumet) 50/500, 50/1000 mg
tablets
Saxagliptin (Onglyza) 2.5, 5 mg tablets
Saxagliptin/metformin (Kombiglyze XR)
2.5/1000, 5/500, 5/1000 mg
Tablets
Dipeptidyl Peptidase-4 (DPP-4) Inhibitors
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
Patient InfoN/VHypoglycemiaWeight neutralNasopharyngitis/URIHeadacheOnset: Reduction in postprandial serum glucose: 60 minutes
Dipeptidyl Peptidase-4 (DPP-4) Inhibitors
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
dailyGeriatric: caution due to age related renal function decreases
Cautions/Severe Adverse ReactionsAcute pancreatitisRash (Stevens-Johnson syndrome)
Dipeptidyl Peptidase-4 (DPP-4) Inhibitors
GLP-1 receptor agonist
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
Liraglutide Victoza Once daily Injection
Exenatide Byetta Once daily Injection
GLP-1 receptor agonist
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 (Actos) 15, 30, 45 mg tablets
Rosiglitazone (Avandia) 2, 4, 8 mg tablets
IndicationsAs adjunct to diet and exercise for type II diabetes MOAIncrease insulin sensitivity by affecting PPAR-γ (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 InfoWeight gainEdemaHypoglycemia esp. when used with other antidiabetic medications and insulin (not w/ metformin)May cause or exacerbate heart failure with risk of fluid retentionURI, sinusitis, pharyngitisMyalgiaHeadache
TZD (cont)
Cautions/Severe Adverse ReactionsBlack Box: Heart Failure (for all thiazolidinediones, mainly due to rosiglitazone)Hepatic failureAnemiaBone lossOvulation in premenopausal womenPregancy 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
CONTRAINDICATIONSNYHA Class III-IV heart failureActive 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 injectionRotate siteCheck blood sugars regularly
Storage:Refrigerate until useOnce 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 dosesAdjust according to fasting (premeal) blood glucose of 80-130 mg/dL and peak postprandial blood glucose < 180 mg/dLProvide 50% as long acting insulin and 50% as prandial insulin1 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
Exercise??? ---- Acute Stress???
Insulin Action
Rapid/immediate
Fast
Intermediate
Slow
0 2 4 6 8 10 12 14 16 18 20 22 24
Blo
od c
once
ntra
tion
Time (hr)
Insulin Dosing
Normal insulin secretion
Long-acting
Long-acting &Short-acting
70/30 pre-mixed
Insulin Administration
Pharmacology for Technicians by Ballington, Lauglin. EMC Paradigm 2006, Fig. 14.9
Insulin (cont)
Cautions/Severe Adverse ReactionsSevere hypoglycemia (seizure/coma) (BG < 40 mg/dL)EdemaLipoatrophy or lipohypertropy at injection site
CONTRAINDICATIONSSevere hypoglycemiaAllergy or sensitivity to any ingredient of the product
Insulin Comparison Chart
courses.washington.edu/pharm504/Insulin%20Chart.pdf
Adjunctive Therapy in Diabetes Mellitus Type II
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,
½ can of soda (NOT diet!)– Treatment: glucagon injection
Dose: 1 mg IM, IV, SQ; may repeat in 20 minutes if needed
Adjunctive Therapy (cont)
Energy balance, diet, exercise– Low-carb, low-fat, calorie-restricted diet is recommended
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
Adjunctive Therapies (cont)
Dislipidemia– Patients with type II diabetes have an LDL goal < 100
mg/dL– Weight loss– First line therapy: statins (i.e. atorvastatin, simvastatin,
rosuvastatin etc.)– Fiber, omega-3 fatty acids (fish oils) can be used as adjunct
therapy
Antiplatelet agents– Consider starting daily low dose aspirin (81 mg) to prevent
ischemic events
Adjunctive Therapies (cont)
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– Fastidious foot care– Regular foot exams (annually)
Eye exams Monitor kidney function
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