Gliquidone

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Gliquidone

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Medically reviewed

Marina Burgos

Last updated on 10/01/2026

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Gliquidone

Property Description
Active Ingredient Gliquidone (INN)
Form Tablet
Pharmacological Class Second-Generation Sulfonylurea, Oral Hypoglycemic Agent
Common Therapeutic Goal Blood glucose control in Type 2 Diabetes Mellitus
Origin Synthetic (Isoquinoline derivative)

Gliquidone: Identity and Classification as a Sulfonylurea Agent

Gliquidone is a potent, synthetic, single-ingredient oral medication that belongs to the sulfonylurea class of antidiabetic agents, developed specifically for managing Type 2 Diabetes Mellitus. It is precisely classified as a second-generation sulfonylurea, a group widely recognized for its enhanced binding affinity and overall potency compared to earlier formulations in the same category. The medication is chemically identified as an isoquinoline derivative, with the molecular structure C27H33N3O6S. This classification confirms its role as an oral hypoglycemic agent.

Pharmaceutical Form and General Composition

This medication is presented as a tablet and is designated exclusively for oral intake. The product is a single-ingredient formulation, meaning the therapeutic activity is derived entirely from the substance Gliquidone itself. Gliquidone’s unique metabolism, involving predominantly biliary and fecal excretion, is a characteristic differentiating its use profile from sulfonylureas that rely heavily on renal elimination. The tablet also consists of solid pharmaceutical excipients, which are non-active components necessary for forming the dosage structure and ensuring stability of the oral preparation.

Primary Purpose and Therapeutic Goal

The primary therapeutic goal of Gliquidone is to facilitate better blood glucose control in adults with Type 2 Diabetes. It achieves this general purpose by encouraging the pancreas to stimulate insulin release from the pancreatic beta-cells. This fundamental action aids in regulating blood sugar levels, serving as an important measure to reduce chronically elevated glucose in the bloodstream, which is the defining metabolic challenge in this condition.

What side effects are possible with Gliquidone?

Possible Side Effects and Safety Information: Gliquidone

The official safety documentation for Gliquidone, a sulfonylurea agent, is structured around the identification and classification of adverse reactions primarily within the context of metabolic control. The most frequent and clinically significant reaction documented is Hypoglycemia (low blood glucose), which is officially classified as a Common adverse effect.

Documented Adverse Reaction Groupings

Adverse reactions are officially reported across several System-Organ Classes (SOCs), which classify effects according to the body system affected. These include:

  • Metabolism and Nutrition Disorders: Primarily Hypoglycemia and associated weight gain.
  • Gastrointestinal Disorders: Such as nausea, vomiting, abdominal pain, and diarrhea.
  • Hepatobiliary Disorders: Reports of elevated liver enzymes have been noted.
  • Skin and Subcutaneous Tissue Disorders: Less common reactions, including skin rashes and itching, are documented.

Serious Reactions and Safety Constraints

The most serious reaction documented is Severe Hypoglycemia, which can lead to life-threatening complications. Furthermore, regulatory advisories note that a potential for increased cardiovascular mortality risk has been associated with the long-term use of the sulfonylurea class.

Specific safety considerations address use in special populations. Due to its predominant excretion through the biliary and fecal routes (approximately 95%), Gliquidone is noted as less likely to accumulate in individuals with mild to moderate renal impairment. However, it is explicitly contraindicated in patients with severe hepatic insufficiency, as well as in cases of known hypersensitivity to the drug or related sulfonamides. Regulatory documents also advise against its use in conditions such as Type 1 Diabetes Mellitus.

Overdose and Emergency Response

Overdose and when to seek help

The official overdose profile for Gliquidone, consistent with its classification as a sulfonylurea, centers entirely on the risk of severe hypoglycemia (abnormally low blood glucose levels). This is the single critical manifestation documented in regulatory sources for overdosage.

Documented Manifestations and Severe Outcomes

Classification Official Regulatory Statement
Primary Manifestation Profound, potentially prolonged hypoglycemia (low blood glucose).
Severe Outcomes Escalation to central nervous system (CNS) effects, including seizures, coma, and risk of permanent neurological damage or death.
Population Note Pediatric exposure to even a single tablet mandates immediate medical attention due to the risk of life-threatening hypoglycemia.

Regulator-Mandated Emergency Actions

Immediate medical attention and hospitalization are required for all confirmed or suspected cases of Gliquidone overdosage. This action is critical because the drug's sustained effect creates a high risk of delayed or recurrent hypoglycemia.

Emergency management documented in official guidelines includes the immediate administration of intravenous glucose (dextrose) to correct low blood sugar. The specific antidote, Octreotide, is listed for use following initial stabilization. To mitigate recurrence risk, mandatory hospital observation for a minimum of 12 to 24 hours is required, regardless of initial symptom severity, as documented in authoritative regulatory standards.

Therapeutic Uses of Gliquidone

Gliquidone is generally categorized as a sulfonylurea used in the management of Type 2 Diabetes Mellitus (T2DM). It is applied when initial management strategies alone are insufficient to meet desired glycemic targets. Its therapeutic benefit helps manage symptoms related to systemic imbalance by supporting overall blood sugar levels, which contributes to easing the overall symptom load related to chronic hyperglycemia.

The therapeutic aims for Gliquidone may assist with addressing symptoms related to chronically elevated blood glucose, postprandial glucose spikes (acute elevations following meals), and supporting the HbA1c level. The drug is commonly used to help with patients with T2DM who also have symptoms linked to organ-specific functional stress or mild to moderate renal impairment.

“Gliquidone supports the stabilization of blood sugar and assists with managing the systemic effects of chronic high glucose levels.”

This profile is considered relevant for patients who require this class of medication to support blood sugar control while remaining a relevant therapeutic option in this specific context, particularly for older adults or those with renal considerations.


Quick Fact: Supportive Management for Postprandial Hyperglycemia Gliquidone is commonly used to help address the specific challenge of glucose spikes that occur after food intake, which supports general well-being during symptomatic phases.

Eligibility and Restrictions for Use

The eligibility for Gliquidone use is strictly defined by regulatory authorities and limited to Adult Patients with Type 2 Diabetes Mellitus.

Absolute Contraindications (Must Not Use)

Use is formally prohibited in the following populations and conditions:

  • Type 1 Diabetes Mellitus and acute metabolic crises, including Diabetic Ketoacidosis or Diabetic Coma.
  • Severe Hepatic Insufficiency or Severe Kidney Failure.
  • Women who are Pregnant or Breastfeeding (Lactating).
  • Known Hypersensitivity to Gliquidone, other Sulfonylureas, or Sulfonamide derivatives.

Population-Specific Rules

Age-Related Eligibility: Gliquidone is approved exclusively for Adult Use. Its safety and efficacy have Not Been Established in Children and Adolescents. Older Adults require special caution due to increased sensitivity.

Organ Function Status: While Severe Hepatic Insufficiency and Severe Kidney Failure are contraindications, use is generally permitted in Mild to Moderate Renal Impairment due to the drug's predominant non-renal clearance profile.

Conditional Restrictions: The medication must be temporarily substituted with insulin during periods of Acute Metabolic Stress, such as severe infection or major surgical intervention.

What should I know about interactions with other medicines?

Interactions with other medicines and products

The regulatory profile for Gliquidone establishes documented interaction patterns based on metabolic clearance and additive pharmacodynamic effects. All statements reflect information explicitly noted in official government prescribing documents.

Documented Interaction Patterns

Interaction Type Interacting Substance / Category Official Outcome Statement
Pharmacokinetic (PK) Rifamycins (e.g., Rifampicin) Co-administration leads to decreased plasma concentrations of Gliquidone due to the induction of hepatic enzymes, including CYP3A4 and CYP2C9.
Pharmacodynamic (PD) Other Glucose-Lowering Medicinal Products Co-administration results in an additive effect, increasing the potential risk of hypoglycaemia.

No medicinal products are listed as formal, absolute contraindications in the available prescribing information. The official documents do not list mandatory timing-separation rules or specific interactions with food, alcohol, or herbal products for Gliquidone.

This interaction structure focuses on the risk of altered drug exposure and functional synergy. The CYP enzyme induction by Rifamycins can result in a loss of Gliquidone's expected blood glucose control. Conversely, combining Gliquidone with other agents that lower blood sugar enhances the overall glucose-reducing effect. The interaction constraints are tied to these specific metabolic and functional pathways.

Mechanism of Action

Gliquidone's primary molecular interaction involves binding to the sulfonylurea receptor 1 ( SUR1) subunit of the ATP-sensitive potassium ( KATP) channel in pancreatic beta-cells. This inhibitory action blocks potassium efflux, leading to the depolarization of the cell membrane, which serves as the electrochemical trigger for the downstream events.

The membrane depolarization immediately causes the opening of voltage-dependent calcium channels ( VDCCs) and the influx of calcium ions ( Ca^2+). The resulting spike in intracellular Ca^2+ is the definitive molecular signal that triggers the fusion of insulin-filled vesicles with the cell membrane, thereby accomplishing insulin exocytosis.

The system-level effect is the drug-induced increase in circulating insulin. This elevated insulin enhances glucose uptake by peripheral tissues and suppresses the liver's glucose production (hepatic glucose output), leading to a reduction in blood glucose concentration throughout the body.

Dosage and Administration Information

Administration Guidelines for Gliquidone

Gliquidone is an oral hypoglycemic agent taken as a tablet, and its use follows established protocols. The administration route is exclusively oral, consistent with its form. The following parameters summarize the dosing and scheduling:

Instruction Category Regimen Principle
Route of Administration The medication is taken orally as a 30 mg tablet.
Dosing Schedule Initial: 15 mg once daily. Maintenance: Typically 45 mg to 60 mg daily. The Maximum Daily Dose is not to exceed 180 mg.
Timing with Meals Must be taken before meals. For divided regimens, the largest single portion is generally administered before breakfast.
Frequency Pattern Once daily for initial or lower doses; divided into 2 or 3 doses when the total amount exceeds 60 mg.

The overall usage protocol involves a gradual titration process where the dose is systematically increased using increments (e.g., 15 mg to 30 mg) until the individual therapeutic requirement is identified, adhering to the maximum single dose limit of 60 mg. This titration ensures the medicine is administered at the lowest effective amount.

A key procedural instruction relates to its use in patients with renal function compromise. Due to its primary excretion through the biliary and fecal routes, the risk of drug accumulation is low. Despite this, dose reduction may still be deemed necessary in cases of severe renal function compromise. It is a procedural instruction that a missed dose must not be doubled, and should instead be skipped if the next scheduled dose is near.

Recent Clinical Evidence

Research evidence / Overview of Studies for Gliquidone

Evidence for Use in Type 2 Diabetes Mellitus (T2DM)

Research has explored Gliquidone's clinical evaluation for blood glucose management in Type 2 Diabetes Mellitus. The evidence base includes Randomized Controlled Trials (RCTs) and comparative clinical studies that were conducted during its clinical evaluation in adult populations. These studies primarily focused on measuring changes in key glycemic biomarkers, such as the HbA1 c level (a long-term measure of blood sugar control) and immediate levels of Fasting Plasma Glucose (FPG) and Postprandial Glucose (PPG).

In these research contexts, the studies monitored blood sugar patterns over defined time intervals, typically comparing Gliquidone's use against control groups or other glucose-lowering medications. The collected data reported patterns related to HbA1 c and plasma glucose values. Research explored secondary endpoints, including the tracking of certain lipid markers and body weight change, as part of the metabolic profile evaluated during the study period.

The data for definitive, long-term outcomes, such as the prevention of complications like heart problems or strokes, are not fully established through extensive Gliquidone-specific trials, which largely relied on surrogate markers like HbA1 c. The evidence also includes limited comparative data against many of the newer classes of contemporary diabetes treatments.


Evidence for Use in T2DM with Kidney Considerations

This area of research was explored due to its metabolic characteristics, which differ from some other medications in the sulfonylurea class regarding the pathway for drug clearance. Research has included Pharmacokinetic/Pharmacodynamic (PK/PD) Studies and Specialist Comparative Clinical Trials designed to evaluate the drug's action and clearance in individuals with reduced kidney function.

The findings indicate that in the observed populations, there was minimal evidence of drug accumulation in the plasma when used in those with mild to moderate kidney impairment, which was observed in some studies that examined its clearance pathway, known to be predominantly non-renal.


Duration of Evidence and Long-Term Follow-up

The typical follow-up durations in the key clinical studies that were evaluated were often short- to intermediate-term, with many trials reporting on periods spanning six months. While these short-term studies help show what has been observed so far regarding immediate blood sugar control, there is limited information for long-term outcomes regarding the durability of blood sugar control or the drug's contribution to chronic complication prevention over many years.


Special Populations Included in Clinical Studies

The clinical evidence primarily focuses on adults with T2DM. The use of Gliquidone in older adults was also observed in studies. However, dedicated evidence regarding other special populations, such as pediatric patients or pregnant individuals, remains insufficient, meaning the results apply only to the adult and defined comorbidity populations studied.


Unanswered Questions and Research Gaps

Sample sizes were modest and follow-up durations were limited in many historical trials, which impacts the certainty regarding rare or late-onset outcomes. A major gap exists in the comparative evidence against newer, contemporary diabetes medications. The lack of extensive, high-certainty data on macrovascular and microvascular outcomes highlights an area where further long-term research is needed to provide greater clarity.

Frequently Asked Questions (FAQ)

Common questions about Gliquidone (FAQ)

Q: How quickly should Gliquidone start working after I begin taking it?

A: Regulatory documents describe Gliquidone as being rapidly and almost completely absorbed once taken orally. Its effect on the body's blood sugar levels typically lasts for several hours following administration. The drug’s elimination from the body is relatively quick, with an elimination half-life generally ranging from approximately 1.5 to 8 hours.


Q: What makes Gliquidone different from Metformin?

A: Gliquidone and Metformin are distinct medications used for diabetes, belonging to different pharmacological classes. Official documents state that Gliquidone is a sulfonylurea that works by stimulating insulin release from the pancreas. Metformin, a biguanide, primarily reduces the amount of sugar produced by the liver. They achieve blood sugar control through different mechanisms.


Q: Is Gliquidone the same as other 'sulfonylurea' medicines?

A: Gliquidone is classified within the sulfonylurea drug class. However, it is primarily distinguished from many other medications in this group by the way the body eliminates it. Official information indicates Gliquidone is predominantly cleared through the biliary and fecal routes (non-renal), meaning it relies very little on the kidneys for removal.


Q: Why do some people say Gliquidone is better for kidney issues?

A: This characteristic is related to its unique metabolism. Because the drug is primarily cleared through non-renal routes, official formularies and guidelines cite Gliquidone as the preferred sulfonylurea choice for individuals with mild to moderate kidney impairment. This characteristic reduces the risk of the medication building up in the body.


Q: Is it true that Gliquidone has a lower risk of hypoglycemia than some older drugs?

A: Hypoglycemia (low blood sugar) is a commonly reported adverse effect associated with Gliquidone. However, clinical studies assessed by regulatory bodies have noted that Gliquidone has been associated with less frequent instances of hypoglycemia when compared to some older medications in the same class, specifically glibenclamide.


Q: Can Gliquidone cause weight gain or weight loss?

A: Official safety documentation reports that Gliquidone is associated with weight gain, which is classified under Metabolism and Nutrition Disorders. The available regulatory documents do not list or track weight loss as an adverse reaction.


Q: Is it common to feel dizzy or shaky when taking Gliquidone?

A: Dizziness and shakiness are common signs associated with hypoglycemia, or low blood glucose. Hypoglycemia is listed in regulatory documents as the most frequent and clinically significant adverse reaction associated with Gliquidone use.


Q: Are there any foods I should specifically avoid while on Gliquidone?

A: Official regulatory documents and prescribing information do not specify a list of foods to avoid, nor do they detail mandatory avoidance rules or specific interactions with general food products. The usage protocol requires the drug to be taken before meals.


Q: Is Gliquidone safe to use if I have high blood pressure?

A: Official documents focus on Gliquidone’s use for Type 2 Diabetes and list specific contraindications, such as severe liver failure. The available regulatory information does not contain specific guidance regarding its use in patients with co-morbid high blood pressure (hypertension).


Q: Is Gliquidone approved for use in children?

A: Gliquidone is approved exclusively for use in Adults with Type 2 Diabetes Mellitus. Its safety and effectiveness have not been established in children and adolescents, and it is not authorized for use in pediatric populations.


Q: What is the longest period of time people typically stay on Gliquidone?

A: Official regulatory documents do not define a typical maximum duration for the use of Gliquidone. The clinical studies assessed in regulatory reviews primarily focused on short- to intermediate-term observation periods, often six months or less.


Q: Can Gliquidone be stopped suddenly, or does it require tapering off?

A: Official documentation provides instructions for administration and handling missed doses, but does not contain specific instructions for how the medication should be stopped, whether suddenly or gradually (tapering). Discontinuing or changing the treatment protocol is part of clinical management.


Q: Does Gliquidone have a 'black box' warning in official documents?

A: Regulatory documents include a safety advisory indicating that a potential for increased cardiovascular mortality risk has been associated with the long-term use of the sulfonylurea class of drugs. Gliquidone's safety profile reflects this class-based constraint, based on studies of related medications.


Q: What is the research evidence about Gliquidone's effect on heart health?

A: Official research summaries state that definitive, long-term data regarding Gliquidone’s impact on major cardiovascular outcomes, such as the prevention of heart problems or strokes, are not fully established through extensive Gliquidone-specific trials. Evidence is primarily based on surrogate markers of blood sugar control.


Q: Is Gliquidone habit-forming or addictive?

A: Gliquidone is classified as an oral medicine for blood sugar control and is not listed in regulatory documents as a controlled substance. Official information does not classify the drug as being habit-forming or having dependence potential.


Q: Does Gliquidone affect vision or eye health?

A: Official safety documentation for Gliquidone does not list specific adverse effects related to vision or eye health among its documented Adverse Reaction Groupings.


Q: Can Gliquidone affect the results of certain lab tests?

A: Reports of elevated liver enzymes have been noted in the safety profile under the Hepatobiliary Disorders section. However, official regulatory documents do not contain specific warnings about Gliquidone interfering with the results of general laboratory tests.


Q: Are there different forms of Gliquidone, like extended-release?

A: Regulatory documentation describes Gliquidone exclusively as a single-ingredient tablet intended for oral intake. Official prescribing information does not describe any other forms, such as extended-release or modified-release formulations.


Q: Does Gliquidone interact with antibiotics?

A: Yes, Gliquidone has a documented pharmacokinetic interaction with a specific class of antibiotics known as Rifamycins (e.g., Rifampicin). This interaction can decrease the concentration of Gliquidone in the body, potentially reducing its effectiveness in controlling blood glucose.


Q: Can Gliquidone be crushed or split if I have trouble swallowing pills?

A: Official administration guidelines confirm the route of administration is oral, using a tablet. However, the regulatory documents do not provide instruction or guidance regarding the physical manipulation, such as crushing or splitting, of the tablets.


Q: What should I know about Gliquidone if I have a sulfur allergy?

A: Gliquidone is a sulfonylurea, a class chemically related to sulfonamide derivatives. It is formally prohibited (contraindicated) in patients with a known hypersensitivity to Gliquidone itself, other Sulfonylureas, or related Sulfonamide derivatives.


Q: What are the official restrictions for driving or operating machinery while taking Gliquidone?

A: Official documents do not list specific legal or mandatory restrictions for driving or operating machinery. However, official advisories relate the risk of hypoglycemia (low blood sugar) to potential effects on concentration and alertness.


Q: Does Gliquidone contain lactose or gluten?

A: Official documents describe the drug as a tablet containing the active ingredient and 'solid pharmaceutical excipients' (non-active components). They do not always explicitly list all common excipients such as lactose or gluten in the summary documents.


Q: Does Gliquidone affect fertility?

A: Official information provides specific guidance and contraindications for women who are pregnant or breastfeeding. However, current regulatory documentation does not contain specific information regarding the effects of Gliquidone on human fertility.

How should Gliquidone be stored and disposed of?

Storage and Disposal of Gliquidone

Official Storage Requirements

Gliquidone tablets must be stored according to regulatory specifications to ensure stability and efficacy. The medication must be kept at room temperature, defined as below 25^circC (77°F). Tablets must remain in their original container and should not be used past the printed expiration date.

  • Required Temperature: Below 25^circC (77^circF)
  • Container: Keep in original packaging.
  • Child Safety: Must be kept out of the sight and reach of children.

Disposal Instructions

Proper waste management is required for unused or expired Gliquidone. The medicine must not be discarded in household trash or disposed of via wastewater, sinks, or toilets. Unwanted tablets should be returned to a pharmacist or an authorized local collection program for controlled pharmaceutical waste disposal.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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