DIABETES MEDICATION COMPARISON CHARTGENERIC/
BRAND NAMES
DOSAGE FORMS
KINETICS
DRUG INTERACTION
SSIDE EFFECTS COMMENTS DOSAGE RANGE
SULFONYLUREAS - stimulate insulin release from β cell; increase peripheral glucose utilization (↑ sensitivity of insulin receptor) reduce hepatic gluconeogenesis
Glimepiride (Amaryl)
1,2,4mg P=2-3hD=24h
• β -Blockers• NSAIDs• Niacin• Rifampin (↓
effect)• MAO inhibitors
• Probenecid• Salicylates
• ↑ Hypoglycemia : most seen w/ chlorpropamide & glyburide (caution in elderly)
• Wt gain, (caution in obese) ; 1st choice option for lean patient
• Reduce dose if hypoglycemia or renal/hepatic dysfxn
• Dose titration q1-2 weeks
• Require consistent food intake to avoid hypoglycemia
I: 1-2mg/dMt: 1-4mg/dMx: 8mg/d
Glipizide (Glucotrol®)
5,10mg P=1.5-2hD=12-24h
I: 5mg/dMt: 5-20mg/dMx: 40mg/d
Glipizide XL (Glucotrol XL®)
2.5,5,10mg
P=6-12hD=24hr
I: 5mg/dMt: 5-10mg/dMx: 20mg/d
Glyburide(Diabeta®)
1.25, 2.5,5mg
P=2-4hD=12-24h
• Ethanol• Diuretics• Azole antifungals
• Chloramphenicol
• HA, Dizziness• Sulfa skin reaction (rash/photosensitivity
Effects on Cholesterol and weight:• No effect on Cholesterol
• May increase weight
I: 1.25-2.5mg qdMt: 5mg bidMx: 10mg bid
Glyburide micronized(Glynase Prestab)
1.5, 3, 5, 6mg
P= 2-3HD=12-24h
I: 1.5-3.0 mg/dMt: 6-10mg/dMx: 12mg/d
BIGUANIDES - increase insulin sensitivity and cellular glucose uptake & utilization; reduce hepatic glucose productionMetformin (MF)Glucophage®
500, 850,1000mg
P=3hD=8-12h
• EtOH and cimetidine ↓
EffectDecreased effects: • nicotinic acid,
• ~1%) GI side effects in • 1-3%;• To avoid GI S/E, • Start low & titrate up Q2-4wk• Anemia
• Does not cause hypoglycemia by itself • Caution if ClCr ≤
60mL/min; • Elderly dose may be required
I: 250-500mg/s Mt: 500-1000mg/dMx: 2500mg/s
MF + GlipizideMetaglip®
2.5/250mg2.5/500mg5/500mg
P=1-3hD=SeeMetformin& Glipizide
I: 2.5/250mgMt: 5-10/1000mg/dMx: 20/2000mg
corticosteroids, estrogens, phenytoin, isoniazid, thyroid products• Increased effects: digoxin, furosemide,
• 6-8: 100(due to B12 malabsorption)
• Avoid if severe renal dysfx/CHF or hepatic disease (lactic acidosis 1:10,000)• Avoid if SrCr >1.5,men; >1.4, women• Metformin is DOC for obese!
MF + RosiglitazoneAvandamet®
500mg/1,2,4mg1000mg/2mg, 4mg
Similar to MF &Rosiglitazonegivenseparately
I: 4/1000mg/dMt: 4-8/1000mgMx: 8/2000mg
MF Ext. Release(NF)Glucophage XR®
500, 750mg
P= 4-8 hD= Up to 24hr
I: 500mg qdMt: 500-1000mg qdMx: 2000mg qd
ranitidine, triamterene
Effects on Cholesterol and weight:• Metformin improves LDL, HDL, and TG.• In combination with other agents may • Increase or decrease weight.
MF+ GlyburideGlucovance®
1.25/250mg,2.5/500mg, 5/500mg
P= 2.75h D=10-12h
I: 1.25/250mg w/meal qdMx: 10/2000mg
α GLUCOSIDASE INHIBITORS - inhibit α -glucosidase in brush border of small intestine; prevent hydrolysis & delay digestion of carbohydrates
Acarbose (Precose®)
50mg100mg
• Meal-time dosing; may take several weeks to work
• Minimally absorbed
• Thiazides and other diuretics
• Corticosteroids
• Estrogens• Phenytoin• Thyroid products
• CCB's
• GI intolerance: flatulence >41% diarrhea >28%
• abdominal pain >21%
• Administer with first bite of each meal
• Does not cause hypoglycemia by itself
• ↑ Liver enzymes=3% w/Acarbose; monitor
• (Caution: may accumulate in chronic renal failure)
• Maximal effect takes weeks; ↑
dose q4-8 weeks.• ROLE: useful in pts with ↑ PPBG; SU, MF
Effects on Cholesterol and Weight:
I: 25mg tidM: 50mg tidMax: 100mg tid
• May decrease TG and Weight• Neutral on LDL and HDL
Miglitol (Glyset®)
25,mg50mg, 100mg
Well absorbed
I: 25mg tidM: 100mg tid
THIAZOLIDINEDIONES (TZDs) - insulin sensitizers: ↓ hepatic output of glucose & ↑ peripheral insulin uptake; ~ 4 weeks before effect (adjust dose at ~3 months)
Pioglitazone (Actos)®
15, 30, 45mg
Onset~ several weeks
• Cholestyramine ↓
• Edema (4.8%)
• Does not cause hypoglycemia by itself
I: 15-30mg qdMx: 45mg qd
Max effect in 8-16 weeks
absorption~70%
• Hepatic CYP2C8 inhibitors and inducers
• HA, fatigue, diarrhea
• Wt gain • Mild anemia• URI• Monitor AST/ALT q2mo in 1st
yr
• Resumption of ovulation in anovulatory premenopausal women (increased risk of pregnancy)
• Use with caution in patients with elevated AST/ALT
• Pioglitazone may have more + lipid effect
• Avoid in patients with NYHA class 3 or 4 heart failure
• Role: Alone + MF; SU; Insulin (but ↑ HF risk)
Effects on Cholesterol and Weight:• Both TZDs improve HDL and
Rosiglitazone (Avandia)
2, 4, 8mg
I: 4mg qdMx: 8mg qd
MEGLITINIDES- short-acting insulin secretagogue; bind to β cell to stimulate insulin release at different site than SU’s; (adjust dose at ~7 days)Nateglinide (Starlix®)
60, 120mg
O= <20mP=60-120mD=~4h
• CYP3A4 inhibitors ↑
effect
• Hypoglycemia
• HA• N/V• Constipation
• Restores 1st phase insulin release- (↓PPBG)
• Rapid, short duration ⇒↓ risk of hypoglycemia vs. SUs
I: 60mg tid ac M: 120mg tid acMx: 180mg tid ac
• CYP3A4 inducers ↓
effect• NSAIDs• Sulfonamides
• Oral anticoagulants
• Salicylates
• Muscle aches
• Chest pain • Dyspepsia
• Flexibility with food intake: skip dose if skip meal; take extra dose if add meal}
• ROLE: alone or + MF, TZD, or insulin
Effects on Cholesterol and Weight:• No change in HDL panel• May increase weight
Repaglinide (Prandin®)
0.5, 1, 2mg
O= 15-60mP=60-90mD= ~4-6h
I: 0.5mg tid acM:0.5 - 4mg acMx: 4mg qid ac
AMYLIN AGONISTS- synthetic analog of human amylin (hormone made in pancreatic β cells; reduction of postprandial glucagon secretion; regulation of gastric emptying
Pramlintide (Symlin)
15,30,50 & 90 mcg
P=20mD=3h
• Acetaminophen
• Hypoglycemia
• Dizziness• N/V• Stomach pain
• Tiredness• Decreased appetite
• Ingestion
• Do not mix with other insulins
• Greater medication error risk: drawn up in unit syringe and dosed in mcg
• Given 15m prior to meals
• Initially decrease current insulin dose by 50%
• Initial:15 mcg immediately prior to meals
• After 3-7d, increase to 30 mcg if no nausea
• Every 3-7d, increase by 15mcg to desired goal, max 60 mcg
INCRETIN HORMONES- Glucagon-like-peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) hormones; causes secretion oaf hormones; GLP-1 inhibits glucagon secretion, promotes saiety, inhibits gastric emptying; promotes glucose disposal
Exenatide (Byetta)
250 mcg/ml
O=1-2 hP=2.1hD=10h
• Digoxin• Lovastatin• Lisinopril• Acetaminophen
• Warfarin
• Nausea especially with 10 mg dose
• Do not need to be on insulin• Adjunctive therapy uncontrolled on metformin, sulfonylurea or combo
• Additional A1c decrease by 0.5%-1%
• Smokers or patients who have discontinued smoking for < 6 mo
• Poorly-controlled or unstable lung disease
• 5 mcg BID within 60m prior to meal
• After 1 mo, may be increase to 10 mcg BID
• Can increase dose after 4 weeks
DIPEPTIDYL PEPTIDASE-4-INHIBITOR (dpp-4)- Enhances incretin system by inhibiting DPP-4 (breaks down GLP-1); helps regulate glucose (α &β cells)
Sitagliptin (Januvia)
25, 50, 100 mg
Combo avail:Sitagliptin/Metformin (Janumet): 50/1000 mg,
P=1-4hD=24h
• Digoxin • Runny or stuffy nose
• Sore throat• URI• HA
• Not approved with insulin or sulfonylureas
• Not approved in DM Type 1 or diabetic ketoacidosis
• Monothearpy and as add-on to metformin or TZDs
• Does not cause weight gain• Less GI effects• A1C decrease of 2%
• 100 mg once daily• 25-50 mg once daily, renal impairment
IC/BRAND NAMES
DOSAGE FORMS
KINETICS
DRUG INTERACTIO
NSSIDE EFFECTS COMMENTS DOSAGE RANGE
INSULIN
General guidelines for Type 2 diabetic insulin dosing are presented below; however, the insulin dose must be individualized for each patient based on SMBG and patient life-style(ie, exercise patterns, diet, and stress). The primary activity of insulin is regulation of glucose metabolism. Insulin lowers blood glucose concentrations by stimulating peripheral glucose uptake by skeletal muscle and fat, and by inhibiting hepatic glucose production. Insulin inhibits lipolysis in the adipocyte, inhibits proteolysis, and enhances protein synthesis.
In general • Induces CYP1A2
• Corticosteroids
• Diuretics• Atypical antipsychotics
• Hypoglycemia• Weight gain• Injection site reactions
• Lipodystrophy• Pruritis• Rash
• Except when adjusting for hypoglycemia, primary step in insulin titration should be to correct FBS to < 120 first
Initial dosing may be:Type 2: Single dose Intermediateor long acting (glargine)Slender type 2 patients: 5-10 units daily (preferably at HS to facilitate normalization of FBS).5.10 obese type 2
patients: 10-15 units HS
Alternative: 0.2 units/kg HS (Yale Diabetes Center Diabetes Facts & Guidelines. 2000)
Short-acting (bolus) Insulin regular = R
10 mg/ml
O= ½-1 mP= 2-4 hD=5-7h
Refer to “In general”
Refer to “In general”
• Bolus insulin for meal-time coverage 15 min. before or after meals
• Initially 0.2-0.6 unit/kg/day in divided doses
• Titrate to response
Rapid-acting Insulin aspart (Humalog)
Insulin lispro (Novolog)
Insulin glulisine (Apidra)
100 U/mL
100 U/mLFlexpenPenfill
100 U/mLOptiClik
O=5-10mP=1-3hD=3-5h
O=1/4h P=0.5-1.5hD=4-5h
O=0.2-0.5hP=30-90mD=3-4h
Refer to “In general”
Refer to “In general”
• More rapid onset of ketoacidosis
• Teratogenicity• Higher cost• Multiple daily injections
• Initially 0.2-0.6 unit/kg/day in divided doses
• Titrate to response
Intermediate-acting Insulin NPH = N
Insulin lente = L
100 U/mL
O=1-2hP=6-14hD=24%
O=1-3hP=6-14hD=24%
Refer to “In general”
Refer to “In general”
• Up to 80% of day to day fluctuations in BG response due to intermediate-acting insulins
• Initially 0.2-0.6 unit/kg/day in divided doses
• Titrate to response
Long-acting (basal) Insulin glargine = Lantus
Insulin detemir = Levemir
Insulin ultralente = U
100 U/ml (3mL cartrdrige)(10 ml vial)
100 U/mLPre-filled syringe (3mL)
O=1.5hP=flatD=24h
O=3-4hP=flatD=6-23h
O=6hP=18-24hD=36%
Refer to “In general”
Refer to “In general”
• Do not mix with other insulins
• Lower incidence oaf nocturnal hypoglycemia
• Less weight gain compared with NPH
• Pen available in Lantus and Levemir
• In switching from NPH given twice a day to insulin glargine (Lantus®) given once daily, the recommendation is to reduce the insulin glargine dose by 20%
• In switching from NPH given once daily to insulin glargine (Lantus®) given once daily, the recommendation is to reduce the insulin glargine dose by 10%.
• Levemir can be adjusted 1:1 with Lantus
Inhaled insulin, short -actingExubera
Starter kit, combo pack (12 or 15), 1mg, 3mg
O=10-20mP=2hD=6h
• Corticosteroids
• Diuretics• Atypical antipsychotics
• Albuterol• Epinephrine
• Glucagon• Thyroid hormones
• Estorgens• Progestogens
• Protease
• Cough• Dry mouth• Chest discomfort
• Decrease in pulmonary function
• Dyspnea• Otitis media
• Basal insulin still needs to be given
• TY1DM still need longer acting insulin
• Should be given 10m before meal
• Not recommended with chronic lung disease, smokers or quit smoking < 6 mo
• Not for < 18 yo• 1mg=3U• 3mg=8U
• Inhaler• Initial dose: BW(kg) x 0.05 mg/kg=pre-meal dose (round down to nearest whole number)
• Titrate to response
BP= blood pressure DOC= drug of choice dysfx= dysfunction EtOH= alcohol FPG= fasting plasma glucose GI= gastrointestinal HbA1C= glycosolated Hemoglobin A1C (reflects glycemic control over prior 8-10 weeks) HDL= high density lipoprotein HF= heart failure Ins.= Insulin KINETICS: O=onset P= peak D= duration; LDL= low density SE=side effects Wt= weight * Drugs that may cause hyperglycemia & loss of diabetic control: corticosteroids, diuretics (high-dose thiazides), estrogens, phenothiazines, phenytoin, sympathomimetics (decongestants) & thyroid products. Beta blockers minimal risk of altering glucose control but may alter/mask hypoglycemic response. Pregnancy: Encourage diet, moderate exercise; Avoid oral Hypoglycemics. Also consider: ASA, control of lipids, diet/exercise, ↓hypertension (ACE Inhibitor/ARB/thiazide) & DC smoking SMBG=Self monitored blood glucose.
Special Patient Characterics Medications to UseDecreased renal function
GlipizideGlimepirideTolazamide or tolbutamideInsulin
Repaglinide/nateglindieTZDs
Decreased liver function
Insulin RepaglindeMiglitol
Pts gaining weight AcarboseMiglitolMetformin
Irregular eating patterns
AcarboseMetforminRepaglinide/nateglinideTZDs
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