Table 57-11 Oral Agents for the Treatment of Type 2 Diabetes Mellitus
Drug Namea
Brand Name
Dose
Recommended Starting
Dosage
Nonelderly
Elderly
Usual/Maximal
Dose
Other
Sulfonylureas
250 mg/day
125–250
mg/day
1,500 mg/day
40 mg/day
Metabolized in liver; metabolite potency
equal to parent compound; renally
eliminated
Metabolized in liver; also excreted
unchanged renally
Metabolized in liver; metabolite less active
than parent compound; renally eliminated
Metabolized in liver to inactive metabolites
that are renally excreted
Metabolized in liver to inactive metabolites
20 mg/day
Slow-release form; do not cut tablet
20 mg/day
Metabolized in liver; elimination one half
renal, one half feces. two active metabolites
Better absorption from micronized
preparation
Metabolized in liver to inactive metabolites
Acetohexamide (Y)
Dymelor
250, 500
mg
Chlorpropamide (Y)
Diabinese
250 mg/day
100 mg/day
500 mg/day
Tolazamide (Y)
Tolinase
1,000 mg/day
Orinase
Glucotrol
Glipizide (Y)
Glucotrol XL
5 mg/day
Glyburide (Y)
DiaBeta,
Micronase
Glynase
2.5, 5, 10,
20 mg
1.25, 2.5,
5 mg
1.5, 3, 6
mg
1, 2, 4 mg
500–1,000
mg/day
2.5–5
mg/day
2.5–5
mg/day
1.25–2.5
mg/day
1.5–3
mg/day
0.5–1
mg/day
3,000 mg/day
Glipizide (Y)
100–250
mg/day
1,000–2,000
mg/day
5 mg/day
100 mg/day
Tolbutamide (Y)
100, 250
mg
100, 250,
500 mg
250, 500
mg
5, 10 mg
Glyburide,
micronized (Y)
Glimepiride (Y)
Amaryl
5 mg/day
3 mg/day
1–2 mg/day
1
12 mg/day
8 mg/day
Drug Namea
Brand
Name
Dose
Nateglinide
(Y)
Starlix
60, 120
mg
Usual/Maximal
Dose
Short-acting insulin secretagogues
120 mg/day with 120 mg/day
120 mg three times
meals
with meals
a day
Repaglinide
(N)
Prandin
0.05, 1, 2
mg
0.5–1 mg/day
with meals
Metformin (Y)
Glucophage
Metformin ER
(Y)
Glucophage
XR
500, 850,
1,000 mg
500, 750,
1,000 mg
Metformin
solution
Riomet
500 mg/5
mL
500 mg twice a
day
500–1,000 mg
with evening
meal
500 mg daily
Pioglitazone
(Y)
Actos
15, 30,
45 mg
15 mg/day
Assess renal
2,000 mg/day
function
Thiazolidinediones
15 mg/day
45 mg/day
Rosiglitazone
(N)
Avandia
2, 4, 8
mg
2–4 mg/day
2 mg/day
Acarbose (Y)
Precose
25, 50,
100 mg
Miglitol (N)
Glyset
25, 50,
100 mg
Nonelderly
Elderly
0.5–1 mg/day 16 mg/day
with meals
Biguanides
Assess renal
2,550 mg/day
function
Assess renal
2,550 mg/day
function
8 mg/day or 4 mg
twice a day
α-Glucosidase inhibitors
25 mg one to
25 mg one to
25–100 mg three
three times a day three times a
times a day
day
25 mg one to
25 mg one to
25–100 mg three
three times a day three times a
times a day
day
2
Other
Metabolized by cytochrome P450 (CYP450)
2C9 and 3A4 to weakly active metabolites;
renally eliminated
Caution with gemfibrozil or trimethoprim—
potential hypoglycemia
No metabolism; renally secreted and excreted
Take full dose with evening meal or may split
dose; may consider trial if intolerant to
immediate release
Metformin is indicated in children ≥10 years
old
Metabolized by CYP2C8 and 3A4; two active
metabolites have longer half-lives than parent
compound
Limited availability. Continuation of therapy
or unable to take pioglitazone.
Clinician/patient sign that known risk of MI
Eliminated in bile. Slow titration key for
tolerability. With meals
Eliminated renally
Drug Namea
Brand
Name
Dose
Sitagliptin (N)
Januvia
100, 50, 25
mg
Saxagliptin (N)
Onglyza
2.5, 5 mg
5 mg daily
Linagliptin (N)
Tradjenta
5 mg
Alogliptin (N)
Nesina
25, 12.5,
6.25 mg
Colesevelam (N)
Bromocriptine
mesylate (N)
a
Welchol
Cycloset
Nonelderly
Elderly
Usual/Maximal
Dose
Dipeptidyl peptidase-4 inhibitors (DPP-4 inhibitors)
100 mg daily
25–100 mg
100 mg daily
daily based on
renal function
5 mg daily
5 mg daily
2.5–5 mg daily
based on renal
function
5 mg daily
25 mg daily
25 mg
25 mg
5 mg daily
Bile acid sequestrants
- 625-mg tablet - 6 tablets daily or
- 6 tablets daily or
3.75 g/day
- 1.875- and
3.75-g oral
suspension
0.8-mg
tablets
three tablets twice a
day
- 1.875 g twice a day
or 3.75 g daily
1.6–4.8 mg
daily
three tablets twice
a day
- 1.875 g twice a
day or 3.75 g daily
Dopamine agonist
1.6–4.8 mg
4.8 mg daily
daily
Generic version available? Y, yes; N, no.
3
Other
50 mg daily if estimated creatinine clearance
>30 to <50 mL/min (>0.50 to <0.83 mL/s); 25
mg if creatinine clearance <30 mL/min (<0.50
mL/s)
2.5 mg daily if creatinine clearance <50
mL/min (<0.83 mL/s) or if on strong inhibitors
of CYP3A4/5
Not substantially eliminated by renal, found in
feces. Do not use with strong inducer of
CYP3A4/p-glycoprotein
˜75% eliminated unchanged in urine. 12.5 mg
CrCl <60 mL/min (<1 mL/s), 6.25 mg <30–15
mL/min (<0.50–0.25 mL/s)
Constipation may occur. Take with meal.
Drug–drug absorption interactions present,
may increase triglycerides; contraindicated if
TG >500 mg/dL (>5.65 mmol/L)
Take within 2 hours of rising with food.
Significant nausea, other side effects, and
drug–drug, drug–disease interactions may
occur
Table 57-14 Drug Monitoring for Diabetes Mellitus Medications
Medication
Class
α-Glucosidase
inhibitors
Bile acid
sequestrants
Biguanides
DPP-4
inhibitors
Dopamine
agonists
Adverse Drug Reaction
Monitoring Parameters
Comments
GI upset
Gas, bloating, loose stools
Titrate, take in less carbohydrate
Constipation
Bowel movement frequency
Do not use if history of bowel obstruction
Raises triglycerides
Triglycerides
GI upset
Lactic acidosis
Reflux, nausea, vomiting, stomach
upset, loose stools
Hypoxic states, renal function
Hypersensitivity/angioedema and
exfoliating dermatologic skin reactions
Skin rash, signs/symptoms of
angioedema
Pancreatitis
Amylase, lipase, abdominal pain with
nausea/vomiting
Syncopal symptoms
Not recommended TG >500 mg/dL (>5.65
mmol/L)
Take with food and titrate dose; split doses;
consider extended release
Lactate levels usually not measured, but can if
suspected toxicity
Risk factors, such as history of angioedema,
possibly ACE inhibitor use, and past history of
severe dermal drug reactions, should be explored
Discontinue; look for underlying causes
Hypotension
Worsening psychiatric issues
CNS effects
Gastrointestinal side effects
Signs/symptoms of underlying mental
illness
Mental
alertness/asthenia/fatigue/headache
Nausea
4
Stop antihypertensives
Avoid use with antipsychotics
Titrate slowly
Titrate slowly
Medication Class
Adverse Drug Reaction
Monitoring Parameters
Comments
Thiazolidinediones
Heart failure/pulmonary
edema
Peripheral edema
Weight gain
Peripheral fractures
Hypoglycemia
Hypoglycemia
GI
Pancreatitis
Discontinue
C-cell tumors of thyroid
Signs/symptoms of heart failure, BNP,
weight
Peripheral edema measures
Weight
None except fracture
Self-monitored blood glucose
Self-monitored blood glucose
Nausea/vomiting
Amylase, lipase, abdominal pain with
nausea/vomiting
None recommended, calcitonin
GI upset
Hypoglycemia
Nausea/vomiting
Self-monitored blood glucose
Sulfonylureas
Meglitinides
GLP-1 receptor
agonists
Amylinomimetic
Insulin
5
Limit dose, consider diuretic (see text), or discontinue
Consider if weight is fluid or likely caloric intake
Avoid use in osteoporosis and osteopenia
Titrate slowly; avoid in gastroparesis
Discontinue; look for underlying causes
Calcitonin could be measured if suspected, has not
occurred in humans to date
Titrate slowly; avoid in gastroparesis