Chapter 49

Drugs Affecting Blood Glucose Levels

ASHA RUSSEL
ASST. SCIENCE TUTOR ‘A’
 Insulins
• Synthetic insulin (exogenous) acts in the same manner as endogenously
produced insulin.

• Human-sourced insulin (produced by rDNA technology or genetic

engineering) is considered the standard therapy.

• Insulin is available as rapid-, short- (also known as “regular”),

intermediate-, and long-acting types.

• Prototype insulin: Short-acting regular insulin (Novolin-R, Humulin-R).

 Regular Insulin: Core Drug
Knowledge
Pharmacotherapeutics:
• Type I & II DM.

• Used only to correct a current glucose elevation or an expected rise after

eating.

• Not used to control the glucose level all day due to its short duration of
action.

• Also indicated for patients with hyperkalemia (because an infusion of glucose

and insulin produces a shift of potassium into cells and lowers serum potassium
levels).
 Regular Insulin: Core Drug
Knowledge
Pharmacokinetics:

• Absorption: SC (slow, steady)

• Metabolism: Liver, Kidneys

• Excretion: Kidneys
 Regular Insulin: Core Drug
Knowledge
Pharmacodynamics:
• Insulin’s effects are tissue specific.
• It facilitates membrane transport of glucose (and some other amino acids
and ions) into muscle, adipose, and connective tissue cells and into
leukocytes.
• Injected insulin mimics the effect of endogenous insulin.
 Regular Insulin: Core Drug
Knowledge
Contraindications:
• Sensitivity

• Hypoglycemia

Precautions:
• Pregnancy
 Regular Insulin: Core Drug
Knowledge
Adverse Effects:

• Hypoglycemia

• Lipodystrophy
 Regular Insulin: Core Drug
Knowledge
Drug Interactions:
• Alcohol
• Beta Blockers
• Dobutamine
• Niacin
• MAOIs
• Thiazide Diuretics
• Tetracycline
 Regular Insulin: Core Drug
Knowledge
Patient and family education:
• Teach patients and families the signs and symptoms of hypoglycemia.

• Alert patients and families to the signs and symptoms of out-of-control

diabetes, such as hyperglycemia, polydipsia, polyphagia, and polyuria.

• It is important to caution patients to avoid OTC medications and herbal or

dietary supplements without first consulting the prescriber.

Pg. No: 1055

Noninsulin Antidiabetic Medications
I. SULFONYLUREAS:

• Prototype drug: Glyburide

 Drugs Closely Related to Glyburide: Glimepiride
Glimepiride:
• There are two other second-generation sulfonylurea drugs, glipizide and
glimepiride.

• Absorption: Delayed by approximately 40 minutes when taken with food.

More effective when given 30 minutes before a meal.

• Metabolism: Liver (via the CYP2C9 pathway)

• Excretion: Fecal and Renal

• Precaution: Pregnancy
 Noninsulin Antidiabetic Medications
II. NONSULFONYLUREAS:
• The nonsulfonylurea antidiabetics comprises of different classes considered
by their mode of action:
Improving insulin action
Delaying the digestion of carbohydrates

• Prototype drug: Metformin (Glucophage), a biguanide, works by improving

insulin action
 Metformin: Core Drug Knowledge
Pharmacotherapeutics:
• It is used as an adjunct to diet and exercise to lower blood glucose in type
2 diabetes.

• It is usually the drug of first choice to use in type 2 diabetes.

 It is not a hypoglycemic agent because it does not stimulate insulin

secretion.

• It is an antihyperglycemic or “insulin sensitizer” agent.

 Metformin: Core Drug Knowledge
Pharmacokinetics:
• Administration: Oral.

• Absorption: GIT – slow & incomplete (bioavailability 50% to 60%).

• Metabolism: Liver.

• Excretion: Kidneys.
 Metformin: Core Drug Knowledge
Pharmacodynamics:
• Metformin works by decreasing hepatic glucose production, decreasing
intestinal absorption of glucose, and enhancing insulin sensitivity in
adipose and skeletal muscle tissue, increasing glucose uptake into those
cells.

• As a result, insulin resistance is lessened.

• In addition, metformin lowers triglyceride levels and total and low-density

lipoprotein (LDL) cholesterol levels, and it promotes weight loss.
 Metformin: Core Drug Knowledge
Contraindications:
• Hepatic disease
• Alcoholism
May predispose patients to lactic acidosis
• Acute or Chronic metabolic acidosis
• Chronic heart failure

Precautions:
• Pregnancy
 Metformin: Core Drug Knowledge
Adverse Effects:
• Lactic acidosis (rare, serious, potentially lethal adverse effect)
• Anorexia
• Nausea and vomiting
• Weight loss
• Abdominal discomfort
• Dyspepsia
• Flatulence
• Diarrhea and
• Metallic taste sensation
 Metformin: Core Drug Knowledge
Drug Interactions:
• It may interact with contrast media used for radiographic procedures.
 Metformin: Core Drug Knowledge
Patient and family education:

• Teach patients to take metformin with meals, morning and evening.

• Emphasize that patients should not use alcohol while taking metformin.

Pg. No: 1058-1059 (Box: 49.4)

 Glucose-Elevating Agents
• Glucagon is a hyperglycemic polypeptide hormone produced by the alpha
cells of the pancreatic islets of Langerhans.

• Its physiologic effect is generally the opposite of that of insulin.

• Glucagon is the body’s first line of defense against hypoglycemia.

• The main stimulus to glucagon secretion is a decrease in intracellular glucose

concentrations that usually occurs as a result of a drop in serum blood sugar.

• Glucagon (GlucaGen) is used in unconscious patients to reverse insulin

overdose.
 Glucagon: Core Drug Knowledge
Pharmacotherapeutics:
• Hypoglycemia

• Used in unconscious patients to reverse insulin overdose.

 Glucagon: Core Drug Knowledge
Pharmacokinetics:
• T½: 3 to 10 minutes

• Metabolism: Liver

• Excretion: Urine & Bile

 Glucagon: Core Drug Knowledge
Pharmacodynamics:
• It increases blood glucose levels by stimulating glycogenolysis in the
peripheral tissues.

• Exerts a positive inotropic and chronotropic effect on the heart (increasing

heart contraction and heart rate).
 Glucagon: Core Drug Knowledge
Contraindications:
• Hypersensitivity
• Insulinoma (also known as hyperinsulinism), a tumor of the functional islet
cells.
• Pheochromocytoma (causes catecholamine release).

Precautions:
• Pregnancy
• Lactation
 Glucagon: Core Drug Knowledge
Adverse effects:

• Hypotension

• Respiratory distress

• Nausea and vomiting

• Hypokalemia in over dosage

 Glucagon: Core Drug Knowledge
Drug Interactions:

• Oral Anticoagulants.
 Glucagon: Core Drug Knowledge
Patient and Family Education:
• Emphasize to patients and family members measures to prevent
hypoglycemic reactions from insulin.
• Instruct family members in the proper technique for emergency
administration of glucagon.

Pg. No: 1064