Mobenol , Novobutamide , Orinase
Classifications: hormone; sulfonylurea antidiabetic; Therapeutic: antidiabetic, sulfonylurea
Pregnancy Category: C
500 mg tablets; 1 g vial
Short-acting sulfonylurea that lowers blood glucose concentration by stimulating pancreatic beta cells to synthesize and
release insulin. No action demonstrated if functional beta cells are absent.
Lowers blood glucose concentration by stimulating pancreatic beta cells to synthesize and release insulin.
Management of mild to moderately severe, stable type 2 diabetes that is not controlled by diet and weight reduction alone.
Also used in treatment of patients who are unresponsive to other sulfonylureas and adjunctively with insulin to stabilize
certain cases of labile diabetes. Used as diagnostic agent to rule out pancreatic islet cell adenoma or diabetes.
Hypersensitivity to sulfonylureas or to sulfonamides; history of repeated episodes of diabetic ketoacidosis (with or without
coma); type 1 diabetes as sole therapy; diabetic coma; severe stress, infection, trauma, or major surgery; severe renal
insufficiency, liver or endocrine disease; pregnancy (category C). Safe use in children is not established.
Cardiac, thyroid, pituitary, or adrenal dysfunction; severe hepatic disease, renal disease, renal impairment, renal failure;
history of peptic ulcer; alcoholism; infection; older adults, debilitated, malnourished, or uncooperative patient; lactation.
Route & Dosage
|Type 2 Diabetes
Adult: PO 250 mg to 3 g/d in 12 divided doses
Diagnosis of Functioning Insulinoma
Adult: IV 1 g over 23 min
- Give total dose before breakfast but preferably in divided doses after meals.
- Crush tablet and give with full glass of water if patient desires.
- Do not give at bedtime because of danger of nocturnal hypoglycemia, unless specifically prescribed.
- Discontinue at least 2 wk before the expected delivery date to prevent prolonged severe hypoglycemia (410 d) in the
neonate if used during pregnancy.
- Store below 40° C (104° F), preferably between 15°30° C (59°86° F) in well-closed
container. Avoid freezing.
Adverse Effects (≥1%)GI:
Nausea, epigastric fullness, heartburn, anorexia, constipation
, cholestatic jaundice
(rare). Hematologic: Agranulocytosis, thrombocytopenia
, hemolytic anemia
, aplastic anemia, pancytopenia
. Metabolic: Hepatic
porphyria, disulfiram-like reactions, SIADH, hypoglycemia
without loss of consciousness or neurologic symptoms
, tremulousness, hunger, drowsiness, GI distress, sweating, anxiety, headache) severe hypoglycemia
ataxia, paresthesias, confusion, tachycardia, seizures, coma
Allergic skin reactions: pruritus, erythema
, urticaria, morbilliform or maculopapular eruptions; porphyria cutanea tarda,
photosensitivity. Special Senses:
Taste alterations. CNS:
Diagnostic Test Interference
The sulfonylureas may produce abnormal thyroid function test results and reduced RAI uptake (after long-term administration). A tolbutamide metabolite may cause false-positive urinary protein values when turbidity procedures are used (such as heat and acetic acid or sulfosalicylic acid); Ames reagent strips reportedly not affected.
increases hypoglycemic effects; thiazide diuretics
may attenuate hypoglycemic effects; alcohol
may produce disulfiram
reaction; beta blockers
may mask symptoms
of a hypoglycemic reaction. Herbal: Ginseng, karela
may potentiate hypoglycemic effects.
Readily from GI tract. Peak:
35 h. Distribution:
Into extracellular fluids. Metabolism:
Principally in liver. Elimination:
7585% in urine; some in feces. Half-Life:
Assessment & Drug Effects
- Supervise closely during initial period of therapy until dosage is established. One or 2 wk of therapy may be required before
full therapeutic effect is achieved.
- Give low initial dose before breakfast to older adults, who may be hyperresponsive to oral antidiabetic therapy. If blood
and urine glucose tests are negative during first 24 h of therapy, initial dose may be continued on a daily basis.
- Monitor closely during adjustment period, watching for S&S of impending hypoglycemia (see Appendix F). Detection of a hypoglycemic
reaction in a diabetic patient also receiving a beta blocker, especially older adults, is difficult.
- Evaluate nondefinitive vague complaints; hypoglycemic symptoms may be especially vague in older adults. Observe patient
carefully, especially 23 h after eating, check urine for sugar and ketone bodies and capillary blood glucose.
- Lab tests: Baseline liver and kidney function tests; periodic HbA1C, serum electrolytes, CBC with differential, and platelet counts.
- Report repetitive complaints of headache and weakness a few hours after eating; may signal incipient hypoglycemia.
- Be aware that pruritus and rash, frequently reported adverse effects, may clear spontaneously; if these persist, drug will
Patient & Family Education
- Understand need to inform physician promptly of symptoms of hyperglycemia and ketoacidosis: flushed, dry skin, weight loss,
fatigue, Kussmaul respiration, double or blurred vision, soft eyeballs, irritability, fruity-smelling breath, abdominal cramps,
nausea, vomiting, diarrhea, dyspnea, polydipsia, polyphagia, polyuria, headache, hypotension, weak and rapid pulse, positive
ketonuria and glycosuria.
- Hypoglycemia is frequently caused by overdosage of hypoglycemic drug, inadequate or irregular food intake, nausea, vomiting,
diarrhea, and added exercise without caloric supplement or dose adjustment. Its occurrence indicates need for immediate
reevaluation of patient's diet, medication regimen, and compliance. It is most likely to appear in patients >50 y of age.
- Report any illness promptly. Physician may want to evaluate need for insulin.
- Do not self-medicate with OTC drugs unless approved or prescribed by physician.
- Be aware that alcohol, even in moderate amounts, can precipitate a disulfiram-type reaction (see Appendix F). A hypoglycemic
response after ingesting alcohol requires emergency treatment.
- Protect exposed skin areas from the sun with a sunscreen lotion (SPF 1215) because of potential photosensitivity (especially
in the alcoholic).
- Weigh at least weekly and report a progressive gain, especially if edema is present. These signs indicate the necessity to
- Be alert to added danger of loss of control (hyperglycemia) when a drug that affects the hypoglycemic action of sulfonylureas
(see DRUG INTERACTIONS) is withdrawn or added to the tolbutamide regimen. Monitor blood glucose carefully.
- Use or add barrier contraceptive if using hormonal contraceptives.
- Carry medical identification at all times. It needs to indicate medical diagnosis, medication(s) and doses, patient's and
physician's names, addresses, and telephone numbers.
- Potential for hypoglycemia in breast fed infants presents the necessity to decide whether to discontinue breast feeding or
temporarily transfer to insulin (if diet alone is inadequate for blood sugar control).