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KLINIK TREATMENT WITH

SULFONYLUREAS 1-2
KESIHATAN
For new patients to be
PENAMPANG initiated on sulfonylureas
(SU), the immediate release
(IR) formulation should be
PHARMACY UNIT started first, not the modified
(DRUG INFORMATION release (MR) formulation.
CENTRE) Gliclazide IR can be taken
NEWSLETTER once daily as a single dose up
Issue 1/2019 to 320mg, with higher doses
to be divided in a day
(standard practice of BD
dosing).
HIGHLIGHTS:
This treatment with MR
➢ Gliclazide MR 30mg = formulation should only be
Gliclazide IR 80mg prescribed if the patient is
likely to have a regular food
➢ Recommended vildagliptin intake (including breakfast).
dose as add-on combination The single daily dose of the
therapy with SU: 50 mg OD MR formulation may be
between 30 mg and 120 mg.

In any case, the maximum dose of gliclazide MR should not exceed 120
mg/day.
The hydrophilic matrix of hydromellose-based polymer in the new
formulation brings about a progressive release of the drug which parallels
the 24-hour glycemic profile in untreated patients with type 2 diabetes
mellitus. The formulation shows high bioavailability and its absorption
profile is unaffected by coadministration with food.
Prepared by CLL02/19
EQUIVALENT DOSES BETWEEN GLICLAZIDE IR AND MR
FORMULATIONS 3

Gliclazide modified release (MR) 30mg is therapeutically


equivalent to gliclazide immediate release (IR) 80mg.
This is not a brand specific recommendation and hence, it can be
applied to the generic versions of gliclazide tablets.

INITIATING A GLIPTIN AND GLIPTIN-SWITCHING 4-7


The mechanism of dipeptidyl If initiating a gliptin to SU/insulin therapy, one
peptidase-4 inhibitors may consider decreasing the SU/insulin dose,
(Gliptins) differs from to reduce hypoglycemia risk.
peptidomimetics Renal impairment
(vildagliptin, saxagliptin) ▪ CrCl <50 mL/min or with ESRD, the
compared to non- recommended dose of vildagliptin is 50 mg
peptidomimetics i.e. OD.
sitagliptin, linagliptin).
The peptidomimetics have THE SWITCH:
lesser selectivity toward DPP- From saxagliptin 5mg OD (maximum daily
4, whereby its inhibition dose)→ vildagliptin 50g BD (maximum daily
occurs in a manner that dose)
involves formation of a Factor to consider: Recommended vildagliptin
reversible covalent enzyme– dose as add-on combination therapy with SU:
inhibitor complex. 50 mg OD (in the morning) (Rule of thumb; to
Gliptins are weight-neutral, reduce hypoglycemia risk); or; may be
thus may be an attractive gradually titrated after assessing the adequacy
option for some patients. of therapeutic response.
References:
1. Rojanasthien N, Autsavakitipong T, Kumsorn B, Manorot M, Teekachunhatean S. Bioequivalence study of modified-release gliclazide tablets in healthy
volunteers. ISRN Pharmacology. 2012;2012:6.
2. Diamicron MR 30mg. Medicines Compendium [updated 31 Jan 2017. Available from: https://www.medicines.org.uk/emc/product/1321/smpc#
3. Joint Formulary Committee. British National Formulary (online) London: BMJ Group and Pharmaceutical Press. Available at http://www.medicinescomplete.com
4. Gupta V, Kalra S. Choosing a gliptin. Indian journal of endocrinology and metabolism. 2011;15(4):298-308.
5. Novartis Pharmaceuticals Australia Pty Ltd. Galvus Product Information. 7 June 2010. 2010. Available from: http://www.novartis.com.au/PI_PDF/gal.pdf
6. Trevisan R. The role of vildagliptin in the therapy of type 2 diabetic patients with renal dysfunction. Diabetes therapy: research, treatment and education of
diabetes and related disorders. 2017;8(6):1215-26.
7. Vildagliptin: a new treatment for type 2 diabetes. 2018. Best Practice Advocacy Centre New Zealand. Available from: https://bpac.org.nz/2018/vildagliptin.aspx
Prepared by CLL02/19

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