Antidiabetic Medications Gizi
-
Upload
mustikaarum -
Category
Documents
-
view
230 -
download
0
Transcript of Antidiabetic Medications Gizi
-
8/12/2019 Antidiabetic Medications Gizi
1/29
-
8/12/2019 Antidiabetic Medications Gizi
2/29
Normal Glucose
-
8/12/2019 Antidiabetic Medications Gizi
3/29
High blood glucose
1. Defective beta cell function Diminished phase 1 insulin release
Delayed phase 2 insulin release2. Overproduction of glucagon
Impaired GI motility
1. Tissues less sensitive to insulin
2. 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
http://professional.diabetes.org/UserFiles/What%20happens%20in%20Type%202%20Diabetes.wmvhttp://professional.diabetes.org/UserFiles/What%20happens%20in%20Type%202%20Diabetes.wmv -
8/12/2019 Antidiabetic Medications Gizi
4/29
ORAL ANTI DIABETICS
Metformin Glucophage 500, 850, 1000 mg tablets
(Glucophage XR) 500, 750 mg XR tablets
Pharmacokinetics
Given orally, Not bind to plasma proteins, Not metabolized, Excreted
unchanged in urine, t 1/2 2 hr
Indication
Type II Diabetes Mellitus,
MOA
Decreasehepatic glucose production, decrease intestinal absorptionof
glucose and increase insulin sensitivity therefore increasing peripheral
glucose uptake
Biguanides
-
8/12/2019 Antidiabetic Medications Gizi
5/29
Biguanides (cont)
SIDE EFFECT
N/V/D Upset stomach/dyspepsiatake with food
Metallic taste
Minimal Weight Loss Alcohol may increase likelihood of lactic
acidosis
Does not cause hypoglycemia
-
8/12/2019 Antidiabetic Medications Gizi
6/29
Biguanides (cont)
Special Population Considerations:
Geriatric:limited data suggests starting doses should be33% 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 notifypractitioner if: myalgia, malaise, hyperventilation, unusual
somnolence. Alcohol potentiates this reaction. Advise
patients not to consume excessive amounts of alcohol.
-
8/12/2019 Antidiabetic Medications Gizi
7/29
Biguanides (cont)
CONTRAINDICATIONS
Renal disease or renal dysfunction (Scr > 1.5 mg/dL
in males, >1.4 mg/dL in females)
Abnormal Scr (serum creatinin) from any cause
including: shock, acute MI, or septicemia
Metabolic acidosis (including diabetic ketoacidosis
(DKA)
Heart failure requiring pharmacologic therapy;
active liver failure
-
8/12/2019 Antidiabetic Medications Gizi
8/29
Sulfonylureas
Glimepiride (Amaryl) 1, 2, 4 mg tablets
Glipizide (Glucotrol,
Glucotrol XL)
(2.5), 5, 10 mg
(XL)
tablets
Glyburide
(Glibeclamide)
(DiaBeta) 1.25, 2.5, 5 mg tablets
Pharmacokinetics
Well absorp from GIT, metab.by hepar,, excr urine
glucose lowering effect: 30 minutes with peak at 1.5-3 hours lasting 24 hours,
duration 10-24h
MOA
Stimulating insulin release from beta-cells of pancreatic islets
Indications
Adjuncts to diet and exercise to lower blood glucose in patients w/ type IIdiabetes mellitus
-
8/12/2019 Antidiabetic Medications Gizi
9/299
Sulfonylureas (Oral Hypoglycemic drugs)
Tolbutamide Acetohexamide
Tolazamide
Chlorpropamide GlipizideGlyburide
(Glibenclamid
Glimepiride
Short
acting
First generation
Intermediate
acting
Long
acting
Long
acting
Short
acting
Second generation
-
8/12/2019 Antidiabetic Medications Gizi
10/29
Sulfonylureas (cont)
Side Effects Hypoglycemia
GI upset/abdominal pain
Dizziness
Weight gain
Heartburn/epigastric fullness
Possible disulfiram-like reaction with alcohol (mainly w/glyburide)
-
8/12/2019 Antidiabetic Medications Gizi
11/29
Sulfonylureas (cont)
Special Population Considerations:
Pediatric:safety and efficacy not established for px under age 16
Hepatic/Renal Dysfunction:conservative dosing and titrationrecommended.
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)
-
8/12/2019 Antidiabetic Medications Gizi
12/29
12
Meglitinides
e.g. Repaglinide, NateglinidePHARMACOKINETICS
Taken orally, Rapidly absorbed ( Peak approx. 1hr )
Metabolized by liver, t1/2= 1 hr, Duration of action 4-5 hr
MECHANISM of ACTION
as do Sulfonylureas, to cause insulin release from -cells.
CLINICAL USE
Approved as monotherapy and in combination with metformin in type 2 DM
SIDE EFFECTS:
Hypoglycemia
Wt gain ( less than SUs )
Caution in px with renal & hepatic impairement.
-
8/12/2019 Antidiabetic Medications Gizi
13/29
13
-Glucosidase Inhibitors
e.g. Acarbose
Pharmacokinetics
Given orallyNot absorbed from intestine except small amount
t1/2 3 - 7 hr
Excreted with stool
Mechanism of ActionInhibits intestinal alpha-glucosidases and
delays carbohydrate absorption,
reducing postprandial increase in blood glucose
-
8/12/2019 Antidiabetic Medications Gizi
14/29
14
Side Effects
Flatulence, Loose stool or diarrhea, Abdominal painAlone does not cause hypoglycemia
-Glucosidase Inhibitors(Contd.)
Indications
Patients with Type II inadequately controlled bydiet with or without other agents( SU, Metformin)
Can be combined with insulin
may be helpful in obese Type II patients
(similar to metformin)
-
8/12/2019 Antidiabetic Medications Gizi
15/29
Thiazolidinediones (TZD)
Pioglitazone (Actos) 15, 30, 45 mg tablets
Rosiglitazone (Avandia) 2, 4, 8 mg 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 inthe liver.
Glucose uptake , gluconeogenesis
-
8/12/2019 Antidiabetic Medications Gizi
16/29
TZD (cont)
Side Effects
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
-
8/12/2019 Antidiabetic Medications Gizi
17/29
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
-
8/12/2019 Antidiabetic Medications Gizi
18/29
TZD (cont)
Special Populations Considerations:
Congestive Heart Failure:should be initiated at
lowest approved dose with longer intervals between
dose increases for class II. Use is not recommended
in patients with Class III or IV CHF
CONTRAINDICATIONS
Class III-IV heart failure
Active liver disease (ALT > 2.5 upper limit of
normal)
I li
-
8/12/2019 Antidiabetic Medications Gizi
19/29
Insulin
Indications
Type I diabetes mellitus, type II diabetes mellitus
(+pregnant), hyperkalemia, DKA/diabetic coma
MOA
Stimulating peripheral glucose uptake and
inhibitinghepatic glucose production
Side Effects
Hypoglycemia (BG < 70 mg/dL) esp with higherdoses
Anxiety, blurred vision, palpitations, shakiness,
slurred speech, sweating
Weight gain
-
8/12/2019 Antidiabetic Medications Gizi
20/29
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)
-
8/12/2019 Antidiabetic Medications Gizi
21/29
Insulin Action
Rapid/immediate
Fast
Intermediate
Slow
0 2 4 6 8 10 12 14 16 18 20 22 24
Bloodco
ncentration
Time (hr)
-
8/12/2019 Antidiabetic Medications Gizi
22/29
Insulin (cont)
Cautions/Severe Adverse Reactions
Severe hypoglycemia (seizure/coma) (BG