NURSING NSC2500 Assignment: The Drug Glibenclamide

Running head: NURSING
NSC2500
Name of the Student
Name of the University
Author Note

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Abstract
Introduction- Type 2 diabetes mellitus comprises of a plethora of dysfunctions that are
predominantly characterized by hyperglycaemia. They are caused due to a combination of
insufficient secretion of insulin, and resistance to action of the insulin hormone. Majority of the
patients diagnosed with type 2 diabetes are asymptomatic, and their clinical manifestations
comprise of blurred vision, weight loss, polyphagia, polydipsia, and polyuria.
Summary- The drug glibenclamide belongs to the class of sulfonylurea and is administered for
the management of type 2 diabetes. It is generally recommended along with other dietary
modifications and physical activity. It is also recommended in conjunction with other
antidiabetic medications like metformin. However, the drug is typically not recommended for
individuals who are diagnosed with type 1 diabetes mellitus. Its route of administration is
primarily through the mouth. Common side effects of this drug are heartburn and nausea. Serious
side effects might result in low blood sugar and angioedema. Though it is not recommended at
the time of pregnancy, but can be administered during breastfeeding.
Target audience- Australian adults aged more than 40 years who have been diagnosed with type
2 diabetes mellitus are the target audience for this lay article. This can be accredited to the
prevalence of the metabolic condition in the nation, and the lifestyle factors that make Australian
adults susceptible to type 2 diabetes.
Conclusion- It can be concluded that if the nursing professionals administer the drug
glibenclamide to the target population, they would observe an effective reduction in high blood
glucose levels.
Keywords: type 2 diabetes mellitus, glibenclamide, Australia

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Table of Contents
Homeostasis.....................................................................................................................................3
Pathophysiology..............................................................................................................................3
Pharmacology..................................................................................................................................5
Drug name...................................................................................................................................5
Pharmacodynamics......................................................................................................................5
Pharmacokinetics.........................................................................................................................6
Route of Administration..............................................................................................................6
Indications contraindications precautions and side effects..........................................................7
Drug interactions.............................................................................................................................7
Lifestyle modification......................................................................................................................8
Relevance to clinical practice..........................................................................................................8
Conclusion.......................................................................................................................................8

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Homeostasis
The endocrine system has been found to play a significant role in controlling homeostasis
in the human body, due to the action of hormones that help in regulating activity of different
tissues and cells, located in the body. The endocrine system controls the release of hormones in
circulating bloodstream by means of a stimulus. Presence of a stimulus either leads to an increase
or decrease in the secretion of a particular hormone. As a response to a change in stimulus, there
occur variations in the internal state of the body (Hall, 2016). It is commonly referred to as
feedback regulation and encompasses a self adjusting mechanism. Feedback regulation generally
arises when the response of the body to a certain stimulus creates an impact on the originals
stimulus. While negative feedback happens when the original stimulus is reduced due to the
response, positive feedback takes place upon augmentation of original stimulus due to the
response.
Pathophysiology
Type 2 diabetes is also referred to as adult onset diabetes, and refers to a metabolic
syndrome that is predominantly characterized by insulin resistance, high amount of blood sugar,
and comparative lack of insulin hormone in the body. Some of the common signs and symptoms
of this condition include increased thirst, increased hunger, frequent urination, and unexplained
loss of body weight (Zaccardi et al., 2016). Type 2 diabetes can be accredited to inadequate
production of insulin hormone from the beta cells that are located in the Islets of
Langerhans. This results in a pathological condition that is characterized by failure of the cells to
appropriately respond to the hormone insulin. This in turn causes insulin resistance.

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Insulin resistance predominantly occurs within the fat tissue, muscles and liver. The
insulin hormone when present in the liver normally triggers inhibition of glucose
release. Nonetheless, when insulin resistance occurs, the liver fails to appropriately trigger the
release of glucose in circulating bloodstream. The proportion of beta cell dysfunction versus
insulin resistance differs amid people (Czech, 2017). While some individuals predominantly
suffering from insulin resistance and negligible defects, in relation to insulin secretion,
others report minor insulin resistance to an absence of appropriate insulin.
Some mechanism that are connected with the onset and progress of type 2 diabetes are an
increase in the degradation of lipids that are present within fat cells, high levels of glucagon in
the circulating bloodstream, lack of metabolic hormone incretin that is responsible for decreasing
the level of blood glucose after consumption of a meal, an increase in salt and water retention by
the kidneys, and insufficient control of metabolism, typically by the central nervous system
(Nauck & Meier, 2016). In addition, the metabolic syndrome has also been associated with
single-nucleotide polymorphisms (SNPs) in genes that are responsible for insulin resistance and
beta-cell function. Some of the common polymorphisms occur in the genes TCF7L2, MTNR1B,
DGKB, FSADS1, HHEX, and WFS1 (Nguyen-Tu et al., 2017; Votsi et al., 2017). Amino acid
metabolism has also been found to directly influence the onset and progress of type 2
diabetes. Risk of suffering from the condition increases manifold amongst normal glycaemic
individuals who report high concentration of fasting plasma of three amino acids that are
phenylalanine, isoleucine,and tyrosine (Nie et al., 2018). This condition is also associated with
various health complications like cardiovascular risk, cognitive decline, renal failure, and partial
or complete loss of vision (Ekoru et al., 2019).

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Pharmacology
Drug name
The drug glibenclamide has the chemical formula C23H28ClN3O5S. It is sold under the
brand names Daonil, Gliben-J, Micronase, Euglucon, Gilemal, Diabeta, Glidanil, Glybovin,
Maninil, Glynase, and Semi-Daonil. The drug belongs to the category of sulfonylurea and is
commonly administered for the management of type 2 diabetes mellitus (Prescriber’s Digital
Reference, 2020).
Pharmacodynamics
Also referred to as glyburide, the drug has been identified as a second generation
sulfonylurea that is predominantly responsible for stimulating secretion of insulin, which in turn
is mediated by closure of the potassium channels that are ATP-sensitive, and located on the beta
cells of the Islets of Langerhans. This eventually results in an augmentation in intracellular
concentration of calcium and potassium ions. Glibenclamide has been found to have a prolonged
duration of action, and is commonly administered once each day (Drug Bank, 2020). It is also
associated with a wide therapeutic index and the administration dosage can be as low as 0.75 mg
or as high as 10 mg.
The ATP sensitive potassium channels that are existing on the beta cells of the pancreas
are typically referred to as sulfonylurea receptor 1 (SUR1). Under circumstances when the
concentration of glucose is extremely low, the SUR1 receptor remains open, thereby facilitating
efflux of potassium ions, with the aim of reaching a membrane potential of an estimated -70mV
(Hardin & Jacobs, 2019). Typically the receptor is found to close in response to a high
concentration of glucose, following which the membrane potential gradually becomes less

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negative that leads to depolarization of the cell. The voltage gated calcium channels eventually
open and trigger entry of calcium into the cell. An upsurge in intracellular concentration of
calcium stimulates insulin release. The drug bypasses the aforementioned procedure by forcing
closure of the SUR1 receptor, and stimulates an increase in insulin secretion (Drug Bank, 2020).
Pharmacokinetics
Elderly patients who are administered the drug reach a Cmax of roughly 211-315ng/mL,
together with Tmax of approximately 0.9-1.0h. In contrast, younger patients reach Cmax of
approximately 144-302ng/mL, in addition to a Tmax of around 1.3-3.0h. Patients administered
glyburide report AUC of 348ng*h/mL. A volume distribution of 19.3-52.6L is observed in
elderly patients, when compared to 21.5-49.3L in younger patients (Drug Bank, 2020). The drug
is99.9% bound to plasma protein, with >98% that binds to serum albumin.
Glibenclamide is primarily metabolized by CYP3A4, in addition to CYP3A7, CYP2C19,
CYP2C9, and CYP3A5. In contrast to other sulfonylureas, it is found to be 50% eliminated in
urine, with the remaining 50% in fecal matter. Glibenclamide is predominantly eliminated in the
form of the metabolite 4-trans-hydroxyglyburide. A terminal elimination half life of
approximately 4.0-13.4h and 4.0-13.9h is observed in older and younger patients, respectively.
Moreover, while young patients report a clearance of roughly 2.47-4.11L/h, it is found to be
2.70-3.55L/h in the elderly patients (Drug Bank, 2020).
Route of Administration
The drug is taken through the mouth in the form of tablets.

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Indications contraindications precautions and side effects
The drug is considered suitable for the management of patients who suffer from type 2
diabetes, when dietary modification and physical exercise are not sufficient for reducing the
blood glucose level. Administration of this drug is particularly recommended for individuals who
are aged over 40 years, and have blood glucose levels not more than 10 mmol/l in fasting phase
(Drug Bank, 2020). It is generally indicated alone or as a combination product, along with
metformin in order to enhance glycaemic control amongst adults, who have been diagnosed with
type 2 diabetes mellitus. The drug is particularly contraindicated amongst patients who are
suffering from diabetic ketoacidosis, with or without, and type 1 diabetes mellitus (Prescriber’s
Digital Reference, 2020). In addition, it must not be administered to patients with severe
infection, major surgery, or severe trauma.
Allergic reactions like myalgia, arthralgia, angioedema, and vasculitis have also been
reported upon administration of this drug. Adverse effects of the drugs that are frequently
reported comprise of weight gain, bloating, heartburn, nausea, and vomiting. The drug also
results in medication induced hyperglycemia. It also leads to the onset of cholestatic jaundice
(Drug Bank, 2020). Glibenclamide is not recommended for patients suffering from G6PD
deficiency, since it might results in acute hemolysis. Furthermore, it is not recommended for
administration at the time of pregnancy, however can be given during breastfeeding.
Drug interactions
Approximately 450 drugs have been identified to directly interact with glyburide. It is
associated with 20 major drug interactions. In addition, 39 minor and 391 moderate drug
interactions have also been recognised. Some of the most common drugs that interact with

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glyburide are Actos (pioglitazone), Benadryl (diphenhydramine), Aspir 81 (aspirin), Januvia
(sitagliptin), Lasix (furosemide), Lipitor (atorvastatin), Vitamin D3 (cholecalciferol), Vitamin
B12 (cyanocobalamin), Fish Oil (omega-3 polyunsaturated fatty acids), Tylenol
(acetaminophen), Cymbalta (duloxetine),and Plavix (clopidogrel) (Drugs.com, 2020).
Lifestyle modification
Engagement in physical exercise and adherence to a healthy diet are the cornerstone of
diabetes care. Physical exercise has been found to significantly enhance blood glucose control.
Aerobic exercise not only helps in production of HbA1c, but significantly improves insulin
sensitivity (Liubaoerjijin et al., 2016). A diabetic diet comprises of restriction of calories and
saturated fat consumption, in order to promote weight loss. It also focuses on more consumption
of whole grains, leafy vegetables and fruits, and effectively manages blood sugar levels
(Esposito et al., 2017).
Relevance to clinical practice
The target audience for this article is type 2 diabetes affected adults. Relevance of the
aforementioned findings to clinical practice can be credited to the widespread prevalence of the
metabolic condition in Australia. Approximately 1 million adults that accounted for 5% of the
total population had type 2 diabetes in 2017-18, with the proportion being slightly greater for
males, in comparison to their female counterparts (6% vs. 4%, respectively) (AIHW, 2019).
Conclusion
Thus, it can be concluded that if the nursing professionals focus on administration of
glibenclamide for adults aged more than 40 years, it would prove effective in diabetes

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management. Poor health literacy has been correlated with non-compliance to medical regimen
and treatment plans, poor participation in self management, expensive healthcare cost,
augmented risk of recurrent hospitalization and even mortality. In addition, the information
shared on the drug will not only increase health literacy among the patients, but also enhance
their health outcomes.

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Czech, M. P. (2017). Insulin action and resistance in obesity and type 2 diabetes. Nature
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