gliclazide | apollo | +9191 46 950 950 gliclazide · description: gliclazide is an oral...
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Gliclazide | apollo | +9191 46 950
950
Gliclazide | apollo | +9191 46 950 950
Gliclazide
CAS Number : 21187-98-4
Molecular Weight : 323.411 g/mol
Molecular Formula : C15H21N3O3S
Systematic (IUPAC) : 1-[(4-methylbenzene)sulfonyl]-3-{octahydrocyclopenta[c]pyrrol-2-yl}urea
Type : small molecule
Description : Gliclazide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent
diabetes mellitus (NIDDM). It belongs to the sulfonylurea class of insulin secretagogues, which act by
stimulating β cells of the pancreas to release insulin. Sulfonylureas increase both basal insulin secretion and
meal-stimulated insulin release. Medications in this class differ in their dose, rate of absorption, duration of
action, route of elimination and binding site on their target pancreatic β cell receptor. Sulfonylureas also
increase peripheral glucose utilization, decrease hepatic gluconeogenesis and may increase the number and sensitivity of insulin receptors. Sulfonylureas are
associated with weight gain, though less so than insulin. Due to their mechanism of action, sulfonylureas may
cause hypoglycemia and require consistent food intake to decrease this risk. The risk of hypoglycemia is
increased in elderly, debilitated and malnourished individuals. Gliclazide has been shown to decrease
fasting plasma glucose, postprandial blood glucose and glycosolated hemoglobin (HbA1c) levels (reflective of the
last 8-10 weeks of glucose control). Gliclazide is extensively metabolized by the liver; its metabolites are
excreted in both urine (60-70%) and feces (10-20%).
Categories :
Hypoglycemic Agents
Sulfonylureas
Antidiabetic
Taxonomy
Kingdom : Organic
Classes : Sulfonylureas
Substructures
Sulfonylureas
Sulfonyls
Pyrrolidines
Benzene and Derivatives
Benzenesulfonamides
Heterocyclic compounds
Aromatic compounds
Sulfonamides
Semicarbazides
Hydrazine Derivatives
Pharmacology
Indication : For the treatment of NIDDM in
conjunction with diet and exercise.
Pharmacodynamics : Gliclazide is a second
generation sulphonylurea which acts as a hypoglycemic agent. It stimulates β cells of the islet of Langerhans in
the pancreas to release insulin. It also enhances peripheral insulin sensitivity. Overall, it potentiates
insulin release and improves insulin dynamics.
Mechanism of action : Gliclazide binds to the β cell
sulfonyl urea receptor (SUR1). This binding subsequently blocks the ATP sensitive potassium
channels. The binding results in closure of the channels and leads to a resulting decrease in potassium efflux
leads to depolarization of the β cells. This opens voltage-
dependent calcium channels in the β cell resulting in calmodulin activation, which in turn leads to exocytosis
of insulin containing secretorty granules.
Absorption : Rapidly and well absorbed but may have wide inter- and intra-individual variability. Peak plasma
concentrations occur within 4-6 hours of oral administration.
Protein binding : 94%, highly bound to plasma
proteins
Metabolism : Extensively metabolized in the liver. Less
than 1% of the orally administered dose appears unchanged in the urine. Metabolites include oxidized and hydroxylated derivates, as well as glucuronic acid
conjugates.
Route of elimination : Metabolites and conjugates are eliminated primarily by the kidneys (60-70%) and
also in the feces (10-20%).
Half life : 10.4 hours. Duration of action is 10-24 hours.
Toxicity : LD50=3000 mg/kg (orally in mice).
Gliclazide and its metabolites may accumulate in those with severe hepatic and/or renal dysfunction. Symptoms
of hypoglycemia include: dizziness, lack of energy, drowsiness, headache and sweating.
Uses
This medication is used in conjunction with diet and exercise regimens to control high blood sugar in non-insulin dependent diabetic patients. Controlling high
blood sugar helps prevent heart disease, strokes,kidney disease, circulation problems, and blindness.
How To Use?
This is best taken with meals. Try to take this medication at the same time(s) each day.
Side Effects
Nausea, stomach upset or diarrhea may occur as your body adjusts to the medication. If any of these effects continue or become bothersome, inform your doctor. Notify your doctor if you develop a skinrash, itching,
easy bruising or bleeding, fever, weakness, trembling or chills while taking this medication. This medication may cause low blood sugar (hypoglycemia) which manifests as dizziness, weakness, drowsiness,headache, sweating,
nervousness, shaking, tingling of the hands or feet, hunger, fast heartbeat. Should these symptoms occur, drink a glass of orange juice or non-diet soda or eat a piece of candy to raise your blood sugar level quickly.
Report the incident to your doctor. To help prevent low blood sugar, eat meals on a regular schedule and do not
skip meals. Symptoms of high blood sugar (hyperglycemia) include confusion, drowsiness,
flushing, rapid breathing or fruity breath odor. Notify your doctor if you experience any of these symptoms. If you notice other effects not listed above, contact your
doctor or pharmacist.
Precautions
Tell your doctor if you have: liver problems, kidney problems, any allergies. This medication may make you more sensitive to the sun's effects. Avoid prolonged sun exposure. Wear protective clothing and use an effective
sunscreen when outdoors. Notify your doctor if you become ill, are injured or acquire a severe infection. This
medication is not recommended for use during pregnancy and should be used only if clearly needed
while breast-feeding. Discuss the risks and benefits with your doctor.
Before taking gliclazide
Before taking gliclazide make sure your doctor or pharmacist knows:
If you are pregnant, trying for a baby or breast-feeding.
If you are over 65 years of age.
If you have liver or kidney problems.
If you have a blood condition called porphyria.
If you have experienced ketosis (where the body converts fat into energy) or acidosis (an accumulation of
acid in the body).
If you are about to undergo surgery, or if you have had a severe trauma or have an infection.
If you have juvenile onset diabetes.
If you are taking other medicines, including those available to buy without a prescription, herbal or
complementary medicines.
If you have ever had an allergic reaction to this or to any other medicine.
How to take gliclazide?
Before beginning treatment, read the manufacturer's printed information leaflet.
Take gliclazide exactly as directed by your doctor.
Taking your dose after food may ease any indigestion side-effects.
Try to take gliclazide at the same time each day to avoid missing any doses. Gliclazide is usually taken once a day with breakfast, although if you are taking higher doses
you may be asked to take a dose twice daily.
If you forget to take a dose, take it as soon as you remember unless it is nearly time for your next dose, in which case leave out the missed dose. Do not take two
doses together to make up for a missed dose.
How does it work?
Diamicron tablets contain the active ingredient gliclazide, which is a type of medicine called a
sulphonylurea. (NB. Gliclazide is also available without a brand name, ie as the generic medicine.) Gliclazide is used to help control blood sugar levels in people with
type 2 diabetes.
People with type 2 diabetes (non-insulin dependent diabetes) have a deficiency of a hormone called insulin.
Insulin is produced by the pancreas and is the main hormone responsible for controlling sugar levels in the blood. It normally makes the cells of the body remove
excess sugar from the blood. In type 2 diabetes insulin is produced inefficiently in response to surges of blood sugar, such as following a meal. The cells of the body also become resistant to the action of insulin that is produced, which means that blood sugar levels can
become too high.
Gliclazide works mainly by stimulating the cells in the pancreas that produce insulin. These cells are called beta
cells. Gliclazide causes the beta cells to produce more
insulin. This helps to decrease the amount of sugar in the blood of people with type 2 diabetes.
Gliclazide improves insulin production immediately after eating. This is called early or first phase insulin
secretion. The enhanced insulin production results in a blood sugar lowering effect in response to meals or
glucose, as occurs naturally in people without diabetes.
Gliclazide is used when dietary measures, weight loss and physical exercise are not enough to control blood
sugar levels in people with type 2 diabetes.
Gliclazide also has effects in the blood vessels. It has been shown to prevent blood cells called platelets from
clumping together in the blood. It also increases the breakdown of blood clots that form within the blood
vessels. This may help prevent the long-term complications of diabetes, which may be partly due to
changes in the blood vessels caused by these mechanisms.
What is it used for?
Type 2 (non-insulin dependent) diabetes, when diet, exercise and weight loss have failed to fully control blood
sugar.
Can gliclazide cause problems?
Along with their useful effects, all medicines can cause unwanted side-effects although not everyone
experiences them. These usually improve as your body adjusts to the new medicine, but speak with your doctor
or pharmacist if any of the following side-effects continue or become troublesome.
Gliclazide Interactions
Your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you
for them. Do not start, stop, or change the dosage of any medicine before checking with them first.
Before using this medication, tell your doctor or pharmacist of all prescription and non-
prescription/herbal products you may use, especially of:
salicylates (aspirin),
phenylbutazone (used to treat arthritis),
sulphonamides,
coumarin drugs (used to thin the blood),
MAOIs (a type of antidepressant),
beta blockers (used to treat high blood pressure),
tetracycline compounds (a type of antibiotic),
chloramphenicol (a type of antibiotic),
disopyramide (used to treat irregular heart beat),
miconazole (an oral treatment for fungus infection),
clofibrate (used to reduce fat),
cimetidine (used to treat stomach ulcers),
oral contraceptives,
steroids,
thiazide diuretics (water tablets),
phenothiazine derivatives (a type of sedative),
thyroid hormone,
laxatives.
This information does not contain all possible interactions. Therefore, before using glicazide, tell your
doctor or pharmacist of all the products you use.
Gliclazide Overdose
In the event of an overdose, contact your doctor or nearest hospital casualty department immediately.
The symptoms to be expected of overdose are those of hypoglycaemia (low blood suger) - sweating, pale skin
colour, hunger pangs, fast heart beat. They can be helped by taking glucose or sweet drinks.
Missed Dose
If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose
and resume your usual dosing schedule. Do not double the dose to catch up.
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