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tolbutamide (Rx)Brand and Other Names:Orinase

 
 
 

Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

tablet

  • 500mg
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Type 2 Diabetes

250 mg-2 g PO qDay or q8-12hr; not to exceed 3 g/day; maintenance dose >2 g/day seldom required

Divided doses may minimize gastrointestinal side effects

Renal Impairment

Dose adjustment not necessary

Hepatic Impairment

May require a lower dose (monitor)

Safety and efficacy not established

250 mg PO qDay or q8-12hr; not to exceed 3 g/day; maintenance dose >2 g/day seldom required

Divided doses may minimize gastrointestinal side effects

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Interactions

Interaction Checker

tolbutamide and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            Frequency Not Defined

            Hypoglycemia

            Dermatologic recations

            Disulfiram-like reactions

            Agranulocytosis

            Hyponatremia

            Aplastic anemia

            Thrombocytopenia

            Heartburn

            Nausea/vomiting

            Cholestatic jaundice and hepatitis may occur rarely which may progress to liver failure

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            Warnings

            Contraindications

            Hypersensitivity, sulfa allergy

            Type I diabetes, diabetic ketoacidosis

            Cautions

            Patients with hypoglycemia, when caloric intake is decreased or there is increased stress due to infection, fever, trauma, or surgery (may need to discontinue treatment)

            Risk of cardiovascular mortality increases with oral hypoglycemic drug treatments compared to treatment with diet alone or diet plus insulin

            Risk of sulfonylurea-induced hemolytic anemia may increase in patients iwth glucose-6-phosphate dehydrogenase deficiency

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            Pregnancy & Lactation

            Pregnancy Category: C

            Lactation: Controversial, avoid

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Initial effect is to increase beta-cell insulin secretion

            May also decrease rate of hepatic glucose production, increases insulin receptor sensitivity, and increases number of insulin receptors

            Pharmacokinetics

            Half-Life: 4.5-6.5 hr

            Duration: 6-24 hr

            Onset: 1hr

            Max Effect: 5-8 hr

            Time to peak, serum: 3-4 hr

            Protein Bound: 80-99%

            Vd: 0.15 L/kg

            Metabolism: extensively, in liver to inactive metabolites by hepatic P450 enzyme CYP2C9

            Metabolites: carboxytolbutamide, hydroxymethyltolbutamide (inactive)

            Excretion: mainly in urine 70-80%

            Dialyzable

            • Hemodialysis: No
            • Peritoneal dialysis: No data
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            Images

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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