Macazid
Macazid Uses, Dosage, Side Effects, Food Interaction and all others data.
Macazid stimulates the release of insulin from pancreatic beta-cells by facilitating Ca++ transport across the beta-cell membranes. It lowers blood glucose by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets. Extrapancreatic effects also may play a part in the mechanism of action of oral sulfonylurea hypoglycemic drugs. Two extrapancreatic effects shown to be important in the action of Macazid are an increase in insulin sensitivity and a decrease in hepatic glucose production. The anti-oxidant, platelet inhibiting and fibrinolytic actions of Macazid involve processes which have been implicated in the pathogenesis of vascular complications of type 2 diabetes.
Based on the pharmacological properties, 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.
| Trade Name | Macazid |
| Generic | Gliclazide |
| Gliclazide Other Names | Gliclazida, Gliclazide, Gliclazidum |
| Weight | 80mg |
| Type | Tablet |
| Formula | C15H21N3O3S |
| Weight | Average: 323.41 Monoisotopic: 323.130362722 |
| Protein binding | 94%, highly bound to plasma proteins |
| Groups | Approved |
| Therapeutic Class | Sulfonylureas |
| Manufacturer | Macter International (pvt) Ltd, |
| Available Country | Pakistan |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Macazid is used for control of blood glucose in patients with non-insulin dependent diabetes mellitus (Type-II, maturity onset diabetes mellitus) whose hyperglycemia cannot be controlled by diet alone.
Macazid is also used to associated treatment for these conditions: Type 2 Diabetes Mellitus
How Macazid works
Macazid 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.
Dosage
Macazid dosage
Adult: The usual initial dose of Macazidis 40 to 80 mg daily, gradually increased, if necessary up to 320 mg daily until adequate control is achieved. A single dose should not exceed 160 mg. When higher doses are required it should be taken twice daily, according to the main meals of the day. For extended release tablet the initial recommended dose is 30 mg daily, even in elderly patients (>65 years); the daily dose may vary from 30 to 120 mg taken orally, once daily.
Macazid extend release tablet should be taken with food because there is increased risk of hypoglycemia if a meal is taken late. It is recommended that the medication be taken at breakfast time. If a dose is forgotten, the dose taken on the next day should not be increased. Dose titration should be carried out in steps of 30 mg, according to the fasting blood glucose response. Each step should last for at least two weeks. Macazid extend release tabletshould be neither broken nor chewed. Macazid extend release tablet30 mg, can replace Macazid 80 mg tabletsfor doses of 1 to 4 tablets per day.
Elderly: Plasma clearance of Macazid is not altered in the elderly and steady state plasma levels are similar to those in adults under 65 years. Clinical experience in the elderly shows that it is effective and well tolerated.
Children: Macazid as with other sulfonylureas is not indicated for the treatment of juvenile onset diabetes mellitus.
Side Effects
Hypoglycemia may occur in concurrent conditions such as hepatic & renal diseases, alcohol intoxication and adrenal and pituitary insufficiency. Mild gastro-intestinal disturbances including nausea, dyspepsia, diarrhea, and constipation have been reported but these types of adverse reactions can be avoided if Macazid is taken during a meal. Allergic dermatological reactions including rash, prurits, erythema, bullous eruption have been reported during treatment with the drug but are not known to be directly attributable to it. More serious reactions like leucopenia, thrombocytopenia, agranulocytosis, pancytopenia, hemolytic anemia, cholestatic jaundice, GI hemorrhage have not been reported with Macazid.
Toxicity
LD50=3000 mg/kg (orally in mice). Macazid 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.
Precaution
Macazid should be used carefully in patients with hepatic impairment. If there is definite hepatic disease then gliclazide should not be used. Consucon (Macazid) can be used safely in patients with renal insufficiency as it is extensively metabolized. Consucon has less sudden hypoglycaemic episode than other sulfonylurea group of drugs.
Interaction
The hypoglycemic effect of Macazid may be potentiated by NSAID (in particular aspirin), phenylbutazone, sulfonamides, coumarin derivatives, MAOIs, beta-adrenergic blockers, tetracyclines, chloramphenicol, clofibrate, cimetidine and miconazole tablets. Ingestion of alcohol may also increase the hypoglycemic effect of Macazid. Some drugs may on the contrary, reduce its activity e.g. barbiturates, corticosteroides, thiazide diuretics, thyroid hormones, laxatives and oral contraceptives.
Food Interaction
- Avoid alcohol.
- Take with or without food. Consistent food intake reduces the risk of hypoglycemia.
Elimination Route
Rapidly and well absorbed but may have wide inter- and intra-individual variability. Peak plasma concentrations occur within 4-6 hours of oral administration.
Half Life
10.4 hours. Duration of action is 10-24 hours.
Elimination Route
Metabolites and conjugates are eliminated primarily by the kidneys (60-70%) and also in the feces (10-20%).
Pregnancy & Breastfeeding use
Pregnant Women: Macazid should not be used in pregnant women although animal studies of Macazid have not shown any teratogenic effect.
Nursing Mothers: This drug is contraindicated when breast feeding.
Contraindication
Hypersensitivity to sulfonylurea, diabetes complicated by ketoacidosis with coma, as a sole therapy of insulin-dependent (Type-1) diabetes mellitus, diabetes when complicated by pregnancy & breast-feeding.
Special Warning
Elderly: Plasma clearance of Macazid is not altered in the elderly and steady state plasma levels are similar to those in adults under 65 years. Clinical experience in the elderly shows that it is effective and well tolerated.
Children: Macazid as with other sulfonylureas is not indicated for the treatment of juvenile onset diabetes mellitus.
Acute Overdose
Symptoms: Hypoglycaemia with or without coma, convulsions or other neurological disorders.
Management: Carbohydrate intake, dosage adjustment and/or change of diet may be helpful. Admin rapid IV inj of concentrated glucose soln for hypoglycaemic coma.
Storage Condition
Store in a cool and dry place, below 30° C and away from light.
Innovators Monograph
You find simplified version here Macazid
Macazid contains Gliclazide see full prescribing information from innovator Macazid Monograph, Macazid MSDS, Macazid FDA label
FAQ
What is Macazid used for?
Macazid is a sulfonylurea type of anti-diabetic medication, used to treat type 2 diabetes. It is used when dietary changes, exercise, and weight loss are not enough.
How safe is Macazid?
Macazid is safe to take for a long time. There's no evidence it harms your pancreas or your general health. But Macazid may stop working properly after a while. Your doctor may then want to stop it or add a different medicine to help keep your blood sugar level stable.
How does Macazid work?
Macazid works by increasing the amount of insulin your body makes.
What are the common side effects of Macazid?
Common side effects of Macazid are include:
- stomach ache or indigestion.
- feeling sick (nausea)
- being sick (vomiting) or diarrhoea.
- constipation.
Is Macazid safe during pregnancy?
Macazid is not generally recommended in pregnancy and while breastfeeding. It's not clear whether Macazid harms an unborn baby. For safety, your doctor will probably change your medicine to insulin before you become pregnant or as soon as you find out you're pregnant.
Is Macazid safe during breastfeeding?
Macazid is not generally recommended in pregnancy and while breastfeeding.
Can I drink alcohol with Macazid?
Yes, you can drink alcohol while taking Macazid, but it's best for men and women to drink no more than 2 units a day. Drinking more than this can increase the risk of low blood sugar.
Can I drive after taking Macazid?
If your blood sugar levels are stable, your ability to drive, cycle or use machines or tools should not be affected by Macazid. But if your blood sugar levels become too low, this can reduce your concentration. If this happens to you, do not drive, cycle or use machines or tools until you feel better.
When should be taken of Macazid?
If you take Macazid once a day, it's best to take it in the morning with breakfast. Macazid can sometimes make your blood sugar level too low . Carry some sweets or fruit juice with you to help when this happens.
Can I take Macazid on an empty stomach?
Macazid tablets should be taken before food , either with breakfast or the first main meal of the day.
How long does Macazid take to work?
When taken 30 minutes before breakfast, Macazid produced a peak of IRI 30 minutes after the meal; taken immediately before or after, it took twice to three times as long to produce an IRI peak.
How long does Macazid last in the body?
Macazid is more effective when administered about 30 minutes before a meal. Blood sugar control persists for up to 24 hours following a single dose, even though levels of Macazid in the blood are barely detectable.
How often can I take Macazid?
For standard-release Macazid, the maximum daily dose is 320mg. If you need to take more than 160mg a day, take the tablets twice a day with your morning and evening meals.
Who should not take Macazid?
Macazid is only for adults. Do not give this medicine to children under 18 years.
What happen If I missed Macazid?
If you missed a dose of Macazid, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose. Do not take two doses together to make up for a missed dose.
What happen if I overdose of Macazid?
Never take more than the prescribed dose of Macazid. If you suspect that you might have taken an overdose of this medicine, go to the nearest emergency medical department/hospital.
Can Macazid affects my heart ?
If you have problems with the heart and blood vessels, use Macazid with caution as it can increase the risk of heart failure.
Will Macazid affect my fertility?
There's no firm evidence to suggest that taking Macazid will reduce fertility in either men or women.
Does Macazid affect kidney function?
Macazid can be considered in renal impairment if appropriate attention is paid to the dose.
Can Macazid cause liver damage?
This case strongly suggests that Macazid can induce acute icteric liver necro-inflammation which may be misdiagnosed clinically as acute viral hepatitis. In patients who show abnormal liver function tests, the immediate discontinuation of Macazid is recommended.
