Chemical name, Chemical structure (compounds marked with*) Uses, Stability and storage conditions, different types of formulations and their popular brand names of:
1. Metformin *
2. Glibenclamide *
3. Glimepiride
4. Pioglitazone
5. Repaglinide
6. Gliflozins
7. Gliptins
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ORAL HYPOGLYCAEMIC AGENTS - PART 2.pptx
1. ORAL HYPOGLYCAEMIC AGENTS
PHARMACEUTICAL CHEMISTRY
D. Pharm 1st year
2023-2024
MISS NIKITA J. BHUTE
Assistant professor
Nagpur college of Pharmacy, Wanadogri,
Hingna road, Nagpur 441110.
2. INDEX
• Chemical name, Chemical structure (compounds
marked with*) Uses, Stability and storage conditions,
different types of formulations and their popular
brand names of:
1. Metformin *
2. Glibenclamide *
3. Glimepiride
4. Pioglitazone
5. Repaglinide
6. Gliflozins
7. Gliptins
3. 1. Metformin
• Structure:
• Chemical name:
1,1-dimethylguanidine.
• Uses:
1) It is used as first-line medication for the treatment of type 2 diabetes.
2) It is also used as a second line agent for the treatment of infertility in patient
with polycystic ovary syndrome (PCOS).
3) It is used as an adjunct to diet and exercise in NIDDM patients older than
18years.
4) It can also be used with a sulphonylurea or insulin to improve glycaemic
control in adults.
4. • Stability and Storage Conditions:
1) This medication should be kept in the tightly closed container and out of
reach of children.
2) It should be stored at room temperature and kept away from light, excess
heat and moisture.
3) It should not be stored in the bathroom.
• Formulations:
1) Solution
2) Suspension
3) It is available in the form of tablet and is administered with dose of 500 mg
orally twice a day or 850 mg orally once a day.
• Popular brand names:
1) Glucophage
2) Fortamet
3) Glumetza
4) Riomet
5) Glucophage XR
5. 2. Glibenclamide
• Structure:
• Chemical name:
5-chloro-N-[2-[4- (cyclohexylcarbamoylsulfamoyl) phenyl]
ethyl] -2-methoxybenzamide
• Uses:
1) It is used to treat patients with impairment of hepatic function.
2) It acts as a hypoglycaemia and hematologic agent.
3) It is recommended that it should be taken along with diet and exercise for
the treatment of type 2 diabetes.
6. • Stability and Storage Conditions:
1) It can be stored at a temperature of more than 40°C or at 40°C for at
least 90 days.
2) It is sensitive to light. It is stored in tightly closed container.
3) It is found to be stable when stored at ambient temperature (25±1°C) as
well as under refrigeration (4 ± 0.5°C).
• Type of Formulation:
1) It is available as tablet with dose of 1.25 mg, 2.5 mg or 5 mg.
• Popular Brand Names:
1) Diabeta
2) Flycron
3) Glyburide
4) Afdiex
5) Aviglen
6) Betanase
7) Bionil
8) Diabeta
7. 3. Glimepiride
• Chemical Name:
4-ethyl-3-methyl-N-[2- [4-[(4-methylcyclohexyl) carbamoyl
sulfamoyl] phenyl]ethyl]-5-oxo-2H-pyrrole-1-carboxamide.
• Uses:
1) It is used with insulin for treating the non-insulin-dependent (type 2)
diabetes mellitus.
2) It is used with a proper diet and exercise to control high blood glucose
level.
• Stability and Storage Conditions:
1) It is stored in a cool, dry place at room temperature and kept away from
light and moisture.
2) The temperature should be kept between 68°F and 77°F (20°C and 25°
C). It should not be refrigerated.
8. • Types of Formulations:
1) The recommended starting dose or initial dose is 1 to 2 mg orally
once a day whereas in case of maintenance dose, there is increase in
1 or 2 mg increments based on glycemic response. Similarly,
maximum dose is 8 mg per day.
• Popular Brand Names:
1) Amaryl
2) Azulix
3) Duetact
4) Tandemact
9. 4. Pioglitazone
• Chemical name:
5-[[4-[2-(5-ethylpyridin-2-yl) ethoxy] phenyl]methyl]-1,3-thiazolidine-2,4-dione
• Uses:
1) It is used as an adjunct to diet and exercise for improving glycaemic control
in individuals having type 2 diabetes mellitus.
2) It may be administered with metformin on insulin.
• Stability and Storage Conditions:
1) It is thermodynamically stable. It should be stored at a temperature of 25°C
(77°F) and excursion permission is 15°C - 30°C (59°F - 86°F)
2) Container should be tightly closed and protected from light, moisture and
humidity.
• Type of Formulation:
1) It is available as a tablet for oral administration containing 15 mg, 30 mg or
45 mg of pioglitazone.
• Popular Brand Names;
1) Actos 5) Duetact
2) Bioglita 4) Diavista
10. 5. Repaglinide
• Chemical name:
2-ethoxy-4-[2-[[(1R)-3-methyl-1-(2-piperidin-1-ylphenyl)butyl]amino]-
2-oxoethyl]benzoic acid.
• Uses:
1) It is used as an adjunct to diet and exercise for improving glycaemic
regulation in individuals having type 2 diabetes mellitus.
2) It has a rapid onset and short duration of action.
• Stability and Storage Conditions :
1) It should be stored at room temperature between 59-77°F (15-25°C) and
kept away from light and moisture.
2) It should not be stored in the bathroom.
3) All medicines should be kept away from the reach of children and pets.
4) Medications should not be flushed down in the toilet or poured into a
drain unless instructed to do so.
11. • Type of Formulation:
1) The starting dose of repaglinide tablet is 0.5-4 mg which is
administered before meals. The maximum daily dose should not
exceed 16 mg/day.
2) Capsules
• Popular Brand Names;
1) Eurepa
2) Novonorm
3) Prandin
4) Rapilin
5) Enyglid
6) Gluconorm
12. 6. Gliflozins
• Chemical name:
(1S)-1,5-anhydro-1-C-(3-{[5-(4- fluorophenyl)thiophen-2-
yl]methyl]}-4-methylphenyl)-D-glucitol
• Uses:
1) It is used for the treatment of type 2 diabetes mellitus. Sometimes
it can be used along with insulin to treat type-1 diabetes.
• Stability and Storage Conditions:
• It should be stored at room temperature
• It should be stored in a cool and dry place.
• The container is kept tightly closed and protected from light.
13. • Type of Formulation:
1) Tablets : The recommended starting dose is 5 mg orally once daily
and maintenance dose is 10-25 mg once daily.
• Popular Brand Names:
1) Canagliflozin
2) Dapagliflozin
3) Empagliflozin
4) Farxiga
5) Invokana
14. 7. Gliptins
• Uses:
1) Gliptins, i.e., DPP-4 inhibitors are a group of medications which is
used in the treatment of type 2 diabetes. Generally, DPP4 inhibitors are
prescribed when both proper diet and regular exercise cannot control
blood glucose levels.
• Stability and Storage Conditions:
1) Medicines may get damaged in direct contact with heat, air and light.
2) The medicine should be kept in a safe place and out of children's reach.
3) Mainly the drug should be kept at room temperature between 68°F and
77°F (20°C and 25°C).
15. • Type of Formulation:
1) The normal dosage vildagliptin tablet is 50 mg taken twice a day.
2) Sitagliptin: recommended dose is 25-100 mg once a day.
3) Saxagliptin: recommended dose is 2.5 or 5 mg once a day.
• Popular Brand Names:
1) Januvia (Sitagliptin)
2) Galvus (Vildagliptin)
3) Tradjenta
4) Onglyza (Saxagliptin)
5) Eucreas