DIABETES MEDICATION COMPARISON CHART GENERIC/ NAMES BRAND DOSAGE KINETIC FORMS S DRUG INTERACTION S SIDE EFFECTS COMMENTS

DOSAGE RANGE

SULFONYLUREAS - stimulate insulin release from cell; increase peripheral glucose utilization ( sensitivity of insulin receptor) reduce hepatic gluconeogenesis Glimepiride (Amaryl) Glipizide (Glucotrol) Glipizide XL (Glucotrol XL) 2.5,5,10 mg 1,2,4mg D=24h P=2-3h -Blockers NSAIDs Niacin Hypoglycemia: most seen w/ chlorpropamide & elderly)

Reduce dose if

hypoglycemia or renal/hepatic dysfxn

I: 1-2mg/d

Mt: 1-4mg/d Mx: 8mg/d I: 5mg/d Mt: 5-20mg/d Mx: 40mg/d I: 5mg/d

5,10mg

P=1.5-2h Rifampin ( D=12-24h effect)

glyburide (caution in Wt gain, (caution in obese) ; 1 choice option for lean patient
st

Dose titration q1-2 weeks

MAO

Require consistent food intake to avoid hypoglycemia

P=612h

inhibitors

Probenecid Salicylates

Mt: 5-10mg/d Mx: 20mg/d

D=24hr

Glyburide

(Diabeta) Glyburide micronized (Glynase Prestab)

1.25, 2.5, 5mg

P=2-4h

D=12-24h Diuretics

Ethanol Azole

HA, Dizziness

Sulfa skin reaction (rash/photosensitivit y

Effects on Cholesterol and weight:

I: 1.25-2.5mg qd Mt: 5mg bid Mx: 10mg bid I: 1.5-3.0 mg/d Mt: 6-10mg/d Mx: 12mg/d

1.5, 3, 5, P= 26mg 3H

antifungals Chloramphe

No effect on Cholesterol May increase weight

D=12-24h nicol

BIGUANIDES - increase insulin sensitivity and cellular glucose uptake & utilization; reduce hepatic glucose production Metformin (MF) 500, 850, P=3h

D=8-12h cimetidine Effect

EtOH and

in

~1%) GI side effects 1-3%;

hypoglycemia by itself

Does not cause

I: 250-500mg/s Mx: 2500mg/s I: 2.5/250mg

Mt: 500-1000mg/d

Glucophage 1000mg Metaglip

MF + Glipizide 2.5/250mg P=1-3h Decreased 2.5/500mg D=See

5/500mg Metformin nicotinic

To avoid GI S/E, Start low & titrate up Anemia

60mL/min;

Caution if ClCr Elderly dose may be

effects:

Q2-4wk

required

Mt: 5-10/1000mg/d Mx: 20/2000mg

acid, & Glipizide

MF +

Rosiglitazone ,2,4mg Avandamet 2mg, 4mg MF Ext. 500,

500mg/1 Similar tocorticosteroid MF & e s, estrogens, isoniazid, thyroid 1000mg/ Rosiglitazon phenytoin, given

malabsorption)

6-8: 100(due to B12

dysfx/CHF or hepatic disease (lactic Avoid if SrCr acidosis 1:10,000)

Avoid if severe renal

I: 4/1000mg/d

Mt: 4-8/1000mg Mx: 8/2000mg

separately products P= 4-8 h Increased D= Up to effects: 24hr digoxin,

>1.5,men; >1.4, women

Release(NF) Glucophage XR

750mg

Metformin is DOC for

I: 500mg qd

furosemide,

obese!

Mt: 500-1000mg qd Mx: 2000mg qd

MF+

Glyburide

1.25/250 P= 2.75h ranitidine, mg, g,

D=10-12h triamterene

Effects on Cholesterol and weight:

I: 1.25/250mg w/meal qd Mx: 10/2000mg

Glucovance 2.5/500m 5/500mg

LDL, HDL, and TG.

Metformin improves In combination with Increase or decrease

other agents may

weight. carbohydrates

GLUCOSIDASE INHIBITORS - inhibit -glucosidase in brush border of small intestine; prevent hydrolysis & delay digestion of

Acarbose

(Precose)

50mg

100mg

Mealtime dosing ; may take l

Thiazides diuretics

and other Corticostero ids

GI

intolerance: flatulence >41% >28%

Administer with first bite of each meal Does not cause

I:

M: 50mg tid

25mg tid

hypoglycemia by itself

Max: 100mg tid

severa weeks to work

Estrogens Phenytoin Thyroid CCB's products

diarrhea

Liver enzymes=3% w/Acarbose; monitor

>21%

abdominal pain (Caution: may accumulate in chronic renal failure) Maximal effect takes weeks; ROLE: useful in pts with PPBG;

dose q4-8 weeks.

Minim ally ed absorb

SU, MF

Effects on Cholesterol and Weight:

Miglitol

(Glyset)

25,mg 50mg, 100mg

Well absorbed

May decrease TG and Weight I: Neutral on LDL and HDL

M: 100mg tid

25mg tid

THIAZOLIDINEDIONES (TZDs) - insulin sensitizers: hepatic output of glucose & peripheral insulin uptake; ~ 4 weeks before effec (adjust dose at ~3 months) Pioglitazone (Actos) 15, 30, 45mg Onset~ several weeks

Cholestyra mine

Edema (4.8%)

Does not cause hypoglycemia by itself

I: 15-30mg qd Mx: 45mg qd

Rosiglitazone 2, 4, (Avandia) 8mg

Max effect in absorption~ 8-16 weeks70%

HA, fatigue, diarrhea Wt gain URI

Resumption of ovulation in women (increased risk of pregnancy)

anovulatory premenopausal

I: 4mg qd

Mx: 8mg qd

Hepatic

CYP2C8 inhibitors and inducers

Mild anemia

Monitor AST/ALT yr

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)

q2mo in 1

st

Effects on Cholesterol and Weight:

Both TZDs improve HDL and

MEGLITINIDES- short-acting insulin secretagogue; bind to cell to stimulate insulin release at different site than SUs; (adjust dose at ~7 days) Nateglinide (Starlix) 60, O= CYP3A4 effect Hypoglycemi a

120mg <20m P=60120m D=~4h

inhibitors

Restores 1 phase insulin release- ( PPBG) Rapid, short duration risk of hypoglycemia vs. SUs

st

I: 60mg tid ac

M: 120mg tid ac Mx: 180mg tid ac

HA

N/V Constipation

Repaglinide (Prandin)

0.5, 1, 2mg

O= 1560m 90m 6h P=60-

CYP3A4 effect

inducers

Muscle aches Chest pain Dyspepsia

Flexibility with food intake: extra dose if add meal}

skip dose if skip meal; take ROLE: alone or + MF, TZD, or insulin Effects on Cholesterol and Weight:

I: 0.5mg tid ac

M:0.5 - 4mg ac Mx: 4mg qid ac

NSAIDs Sulfonamide s Oral nts

D= ~4-

anticoagula Salicylates

No change in HDL panel May increase weight

AMYLIN AGONISTS- synthetic analog of human amylin (hormone made in pancreatic cells; reduction of postprandial glucagon secretion; regulation of gastric emptying

Pramlintide (Symlin)

15,30, 50 & 90 mcg

P=20m D=3h

Acetaminop hen

Hypoglycemi a Dizziness N/V Stomach pain

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

Tiredness appetite

Decreased Ingestion

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 l

mcg/m h

O=1-2 P=2.1h D=10h

Digoxin

Lovastatin Lisinopril hen Acetaminop 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 for < 6 mo

5 mcg BID within 60m prior to meal After 1 mo, may be

increase to 10 mcg BID

Can increase dose after 4 weeks

have discontinued smoking Poorly-controlled or unstable lung disease DIPEPTIDYL PEPTIDASE-4-INHIBITOR (dpp-4)- Enhances incretin system by inhibiting DPP-4 (breaks down GLP-1); helps regulate glucose ( & cells)

Sitagliptin (Januvia)

25, 50, 100 mg

P=1-4h D=24h

Digoxin

Runny or

stuffy nose

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 renal impairment

25-50 mg once daily,

Sore throat URI HA

Comb o avail:S itaglipt ormin met): 00 in/Metf (Janu 50/10 mg,

BRAND NAMES

IC/

DOSAGE KINETIC FORMS S

INTERACTIO NS

DRUG

SIDE EFFECTS

COMMENTS

DOSAGE RANGE

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 INSULIN (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

Hypoglycemia Weight gain reactions Injection site Lipodystrophy Pruritis Rash

Except when adjusting for hypoglycemia,

Initial dosing may be: Type 2: Single dose Intermediate

Corticoster oids Diuretics Atypical ics antipsychot

primary step in insulin titration should be to 120 first correct FBS to <

or long acting (glargine) Slender type 2 patients: at HS to facilitate 5-10 units daily (preferably 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) R

10

mg/ml

O= -1 m P= 2-4 h D=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

Insulin regular =

Rapid-acting (Humalog)

Insulin aspart 100 U/mL

O=510m P=1-3h

Refer to In general

Refer to In general

More rapid onset of ketoacidosis Teratogenicity Higher cost injections Multiple daily

Initially 0.2-0.6 unit/kg/day in divided doses Titrate to response

D=3-5h O=1/4h

(Novolog)

Insulin lispro 100

U/mL Flexpe n Penfill 100

P=0.51.5h D=4-5h O=0.20.5h 90m P=30D=3-4h

Insulin glulisine (Apidra)

U/mL OptiCli k

Intermediateacting

100

O=1-2h D=24% O=1-3h D=24%

P=6-14h

Refer to In general

Refer to In general

Up to 80% of day in BG response due to intermediate-

to day fluctuations

Initially 0.2-0.6 unit/kg/day in divided doses Titrate to response

Insulin NPH = N U/mL

Insulin lente = L

P=6-14h

acting insulins

Long-acting (basal) Lantus

Insulin glargine100 = U/ml (3mL cartrdri ge) (10 ml vial)

O=1.5h P=flat D=24h O=3-4h P=flat

Refer to In general

Refer to In general

Do not mix with other insulins Lower incidence oaf nocturnal hypoglycemia

In switching from NPH given twice a day to insulin glargine (Lantus) given once daily, the reduce the insulin recommendation is to glargine dose by 20%

Less weight gain compared with NPH

D=6-23h

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%.

Insulin detemir = Levemir 100

O=6h P=1824h D=36%

Pen available in Lantus and Levemir

U/mL Insulin ultralente filled =U syringe (3mL) Pre-

Levemir can be adjusted 1:1 with Lantus

Inhaled insulin, kit, short -acting Exubera

Starter combo pack 15), (12 or 1mg, 3mg O=1020m P=2h

Corticoster oids

Cough Dry mouth Chest

Basal insulin still needs to be given TY1DM still need longer acting insulin Should be given

Inhaler Initial dose: BW(kg) x 0.05 mg/kg=pre-meal dose (round down to Titrate to response

Diuretics Atypical ics antipsychot

D=6h

discomfort

Decrease in pulmonary function Dyspnea

nearest whole number)

Albuterol e

Epinephrin

10m before meal

Glucagon Thyroid hormones

Otitis media

Not recommended with chronic lung disease, smokers or quit smoking < 6 mo Not for < 18 yo 1mg=3U 3mg=8U

Estorgens ens

Progestog Protease

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 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 Decreased renal function Glipizide Medications to Use products. Beta blockers minimal risk of altering glucose control but may alter/mask hypoglycemic response. Pregnancy:

Glimepiride Tolazamide or tolbutamide Insulin

Repaglinide/nategli ndie Decreased liver function Pts gaining weight TZDs Insulin Repaglinde Miglitol Acarbose Miglitol Irregular eating patterns Metformin Acarbose Metformin Repaglinide/nategli nide TZDs