Glustazon Dosage

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Dosage of Glustazon in details

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Glustazon Dosage

Generic name: Glustazon HYDROCHLORIDE 15mg

Dosage form: tablet

The information at Drugs.com is not a substitute for medical advice. Always consult your doctor or pharmacist.

Recommendations for All Patients

Glustazon should be taken once daily and can be taken without regard to meals.

The recommended starting dose for patients without congestive heart failure is 15 mg or 30 mg once daily.

The recommended starting dose for patients with congestive heart failure (NYHA Class I or II) is 15 mg once daily.

The dose can be titrated in increments of 15 mg up to a maximum of 45 mg once daily based on glycemic response as determined by HbA1c.

After initiation of Glustazon or with dose increase, monitor patients carefully for adverse reactions related to fluid retention such as weight gain, edema, and signs and symptoms of congestive heart failure.

Liver tests (serum alanine and aspartate aminotransferases, alkaline phosphatase, and total bilirubin) should be obtained prior to initiating Glustazon. Routine periodic monitoring of liver tests during treatment with Glustazon is not recommended in patients without liver disease. Patients who have liver test abnormalities prior to initiation of Glustazon or who are found to have abnormal liver tests while taking Glustazon should be managed as described under Warnings and Precautions.

Concomitant Use with an Insulin Secretagogue or Insulin

If hypoglycemia occurs in a patient co-administered Glustazon and an insulin secretagogue (e.g., sulfonylurea), the dose of the insulin secretagogue should be reduced.

If hypoglycemia occurs in a patient co-administered Glustazon and insulin, the dose of insulin should be decreased by 10% to 25%. Further adjustments to the insulin dose should be individualized based on glycemic response.

Concomitant Use with Strong CYP2C8 Inhibitors

Coadministration of Glustazon and gemfibrozil, a strong CYP2C8 inhibitor, increases Glustazon exposure approximately 3-fold. Therefore, the maximum recommended dose of Glustazon is 15 mg daily when used in combination with gemfibrozil or other strong CYP2C8 inhibitors.

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What other drugs will affect Glustazon?

Tell your doctor if you use insulin. Taking Glustazon while you are using insulin may increase your risk of serious heart problems.

Tell your doctor about all medicines you use, and those you start or stop using during your treatment with Glustazon, especially:

This list is not complete and many other medicines may increase or decrease the effects of Glustazon on lowering your blood sugar. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide.

Glustazon interactions

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Oral Contraceptives:

Co-administration of Glustazon (45 mg once daily) and an oral contraceptive (norethindrone 1 mg plus ethinyl estradiol 0.035 mg once daily) resulted in 11% and 11-14% decrease in ethinyl estradiol AUC and Cmax, respectively. Clinical significance of a high variability on ethinyl estradiol pharmacokinetics is unknown.

Insulin or Insulin Secretagogues: The dose of insulin and insulin secretagogues (eg, sulfonylurea) should be reduced since concomitant administration may result in hypoglycemia.

Midazolam: Administration of Glustazon for 15 days followed by a 7.5 mg single dose of midazolam syrup resulted in a 26% reduction in midazolam Cmax and AUC.

Strong CYP2C8 Inhibitors: Gemfibrozil (an inhibitor of CYP450 2C8) resulted in a 3-fold increase in the plasma concentration of parent Glustazon and also inhibited the further metabolism of M-III and M-IV. Careful blood glucose monitoring and dosage adjustments are suggested during co-administration of Glustazon and gemfibrozil. If used in combination with gemfibrozil or other strong CYP2C8 inhibitors, a maximum dose of Glustazon 15 mg should be used.

CYP2C8 Inducers: Co-administration of Glustazon with rifampicin (an inducer of CYP450 2C8) resulted in a 54% reduction in Glustazon's AUC. The dose of Glustazon may need to be increased when rifampicin is co-administered and glycemic control closely monitored.

If an inducer of CYP2C8 is started or stopped during treatment with Glustazon, the maximum recommended dose of 45 mg should not be exceeded and changes in diabetes treatment may be needed based on the patient's clinical response.

Drugs Metabolized via Cytochrome P-450: The cytochrome P-450 isoform, CYP3A4, is partially responsible for the metabolism of Glustazon. Potential pharmacokinetic interaction (reduction in Cmax and AUC) with CYP3A4 substrates (eg, atorvastatin, nifedipine). Clinical significance of this finding is unknown.

Peak plasma concentration and area under the AUC of Glustazon may increase when taken concomitantly with CYP3A4 inhibitors eg, ketoconazole. However, pharmacokinetic interaction is unlikely with ranitidine which is a relatively weak CYP3A4 inhibitor.

In vitro studies have shown no inhibition of any subtype of cytochrome P-450. Interactions with substances metabolized by these enzymes are unlikely: Ciclosporin, calcium channel blockers, and HMGCoA reductase inhibitors.

Co-administration of Glustazon with the following drugs did not show pharmacokinetic interactions: Metformin, glipizide, digoxin, phenprocoumon, fexofenadine, CYP2C9 substrates (eg, warfarin), CYP1A2 substrates (eg, theophylline).


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References

  1. MeSH. "Hypoglycemic Agents". https://www.ncbi.nlm.nih.gov/mesh/68... (accessed September 17, 2018).
  2. European Chemicals Agency - ECHA. "5-[4-[2-(5-Ethyl-2-pyridyl)ethoxy]benzyl]thiazolidine-2,4-dione: The information provided here is aggregated from the "Notified classification and labelling" from ECHA's C&L Inventory. ". https://echa.europa.eu/information-o... (accessed September 17, 2018).
  3. PubMed Health. "Duetact: This section provide the link out information of drugs collectetd in PubMed Health. ". http://www.ncbi.nlm.nih.gov/pubmedhe... (accessed September 17, 2018).

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Information checked by Dr. Sachin Kumar, MD Pharmacology

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