ANTIDIABETIC DRUGS

DAUTI YUNG’ANA RN, BSc

 INTRODUCTION
• Diabetes Mellitus is a disease that occurs as a result of absolute
or relative deficiency of insulin that results in metabolic and
vascular abnormalities.
• The etiologies include Obesity (because chronic calorie intake
and prolonged stimulation of β cell causes a decrease in insulin
receptor and also adipose tissue and muscle are less
sensitive),hereditary,damage of pancreatic tissue, diabetogenic
hormones(like growth hormone, thyroid, epinephrine),
• diabetogenic drugs like Thiazide diuretics, epinephrine,
phenothiazines
• other factors like Pregnancy.
 Cont.
• The common Signs and symptoms include polydipsia,
polyphagia, polyuria, dehydration due to glucosuria.
• Diabetes has dangerous complications: including
ketoacidosis (in types I), hyperglycemic osmolar non
ketotic coma (in type II), cardiovascular (like
atherosclerosis, myocardial infarction,
• Peripheral arterial insufficiency, Anemia, Hypertension,
stroke, nephropathy, retinopathy,
• neuropathy.
 Cont.

• Hypoglycemic Coma is more serious complication which

usually occurs due to excess dose of insulin which produces
severe lowering of blood glucose that may leads to coma.
• The Sign /Symptom are mental confusion in coordination,
paresthesia, convulsion, coma and
• Signs of sympathetic over activity. The aim of treatment is to
restore blood glucose to normal by
• giving glucose 50% 20 – 100 ml IV,
• or glucagon 1mg iv, im, sc
 Insulin
• Insulin is a hormone produced by the beta cells of the pancreas.
• It plays a crucial role in regulating blood sugar levels in the
body.
• It helps facilitate the uptake of glucose by body cells, where it
is used for energy production or stored as glycogen in the liver
and muscles.
• Insulin is essential for maintaining normal blood glucose
levels, preventing hyperglycemia (high blood sugar), and
promoting overall health.
 cont.

• - The main actions of the hormone is exerted on metabolism of

carbohydrate (CHO), fat and
• protein in liver, muscle & adipose tissue.
• Effects of insulin on carbohydrate metabolism;
 teffects of insulin on carbohydrate metabolism:
• Glucose Uptake: Insulin facilitates the uptake of glucose into
cells, particularly muscle and adipose (fat) cells, by promoting
the translocation of glucose transporters (GLUT4) to the cell
membrane. This allows cells to take up glucose from the
bloodstream, reducing blood glucose levels.
• Glycogen Synthesis: Insulin stimulates the synthesis of
glycogen, the storage form of glucose, in the liver and
muscles. When blood glucose levels are high (e.g., after a
meal), insulin signals the liver and muscles to store excess
glucose as glycogen for later use when energy demands
increase.
 cont.
• Gluconeogenesis Inhibition: Insulin inhibits
gluconeogenesis, which is the process of
generating new glucose from non-carbohydrate
precursors, primarily occurring in the liver.
• By suppressing gluconeogenesis, insulin helps
prevent the release of additional glucose into the
bloodstream when it is not needed.
 cont.
• Inhibition of Lipolysis: Insulin inhibits the
breakdown of stored triglycerides (lipolysis) in
adipose tissue. This helps reduce the release of fatty
acids into the bloodstream and promotes the storage
of fat.
• Protein Synthesis: Although not directly related to
carbohydrate metabolism, insulin also promotes
protein synthesis in cells. This is important for overall
tissue maintenance and repair.
 cont.
• Enhanced Glycolysis: Insulin can increase the rate
of glycolysis, which is the breakdown of glucose into
pyruvate within the cell. This provides an immediate
source of energy for various cellular functions.
• Inhibition of Ketogenesis: Insulin inhibits
ketogenesis, the process of producing ketone bodies
from fatty acids.
• This is significant in preventing excessive ketone
production, which can occur during prolonged fasting
or in uncontrolled diabetes.
 Antidiabetogenic drugs

INSULIN
• Sources include pork or beef, combination of pork and
beef and also human insulin
(Recombinant DNA technique)
 CONT.
• Type of insulin preparation:
• A. (rapid onset): Eg Regular Insuline
• B.Short acting
• C. Intermediate acting Eg Lente insuline,NPH (Neutral Protamine
Hagedorn) insulin
• D. Long acting E.g Protamine Zn insulin
• Types
• Route
• Onset (hrs)
• peak (hrs)
• Duration (hrs)
 Rapid-acting insulin:
• It starts working within 15 minutes after injection, peaks in
about 1 hour, and remains active for 2 to 4 hours. Examples
include insulin lispro, insulin aspart, and insulin glulisine.
– Presentation: 100units/ml
– for use in diabetic emergencies e.g. diabetic ketoacidosis
and at the time of surgery. clearin color
– ROUTE: s.c, i.m or i.v
• Onset: 4-15 minutes
• peak: 1 (hr)
• Duration 2-4(hrs)
• usually taken at the start of a meal
 Short-acting insulin:
• This type begins working within 30 minutes after injection,
peaks in 2 to 3 hours, and remains effective for approximately
3 to 6 hours. Regular human insulin is an example of short-
acting insulin. clear in color
– Presentation: 100units/ml
– ROUTE: s.c, i.m or i.v
• Onset: 15-30 minutes
• peak: 2-3 (hr)
• Duration 6- 24(hrs)
• taken a short time before the meal
 Intermediate-acting insulin(Lente insuline,NPH ):
• It takes effect in 1 to 3 hours, peaks in 4 to 12 hours, and
continues working for about 12 to 18 hours.
• NPH (Neutral Protamine Hagedorn) insulin is an example of
intermediate-acting insulin. cloudy in color
– Presentation: 100units/ml
– ROUTE: s.c, i.m
• Onset: 1-3 (hrs)
• peak: 4-12 (hr)
• Duration 18(hrs)
• taken in the morning and bedtime
 Long-acting insulin:
• lasts all day; given to patients who have been stabilised.
• 1 hrs 30 minutes onset,no distinct peak and can remain
effective for up to 24 hours.
• Examples include insulin glargine and insulin detemir.
– Presentation: 100units/ml
– ROUTE: s.c, i.m
• Onset: 1hr30minutes
• peak: does not pick
• Duration 24(hrs)
• taken once daily or in the morning and at bed time
 CONT.

• N.B. It is only regular(rapid/short acting) insulin that

can be given by intravenous route.
• Therapeutic use -IDDM, NIDDM (not controlled by diet
and oral hypoglycemic agents), diabetic
• ketoacidosis, Control of diabetes in pregnancy, during
surgery and in infections.
 CONT.

• They are also used in the treatment of hyperkalemia

due to renal failure
• Adverse Reaction: can be categorized as
• Local: Atrophy or hypertrophy at site of injection, local
hypersensitivity and secondary infections.
• Systemic: Hypoglycemic coma and Immunologic
reaction like hypersensitive and insulin resistance
 Administration:
• Insulin is typically administered via subcutaneous injection, but
some formulations can be given through insulin pumps or
intravenous infusion in clinical settings.
• Rotating injection sites is essential to prevent lipohypertrophy
(thickening of the fatty tissue) and ensure proper insulin
absorption.
• Common injection sites include the abdomen, thighs, upper
arms, and buttocks.
• 
 Side effects of insulin
• Hypoglycemia: Low blood sugar can cause shakiness,
sweating, confusion, and rapid heartbeat.
• Weight Gain: Some may experience weight gain due to
increased appetite or more efficient calorie storage.
• Allergic Reactions: Rare, but possible, leading to redness,
swelling, itching, or rash at the injection site.
• Lipodystrophy: Fat redistribution at injection sites can cause
lumpy and thickened skin. Rotate sites to prevent this.
• Hypokalemia: Low potassium levels, resulting in weakness,
fatigue, and muscle cramps.
 cont.
• Injection Site Reactions: Pain, redness, or irritation at the
injection site.
• Hypersensitivity Reactions: Rare, but may include hives,
itching, difficulty breathing, or anaphylaxis.
• Vision Changes: Blood sugar fluctuations can temporarily
affect vision.
• Insulin Resistance: Long-term use may lead to reduced
responsiveness to insulin, requiring higher doses.
• dizzness, dry mouth,increases urination, fat hypertrophy at
injection site
• Edema: Insulin may cause fluid retention, leading to swelling,
especially in the ankles and feet.
 Insulin Storage:
• Insulin should be stored in the refrigerator at a temperature
between 2°C to 8°C (36°F to 46°F). Avoid freezing the insulin,
as it can denature the hormone and render it ineffective.
• Before injection, let the insulin vial or pen warm up to room
temperature to reduce discomfort at the injection site.
• 
 Monitoring:
• Regular blood glucose monitoring is crucial for patients on
insulin therapy.
• It helps assess the effectiveness of treatment and adjust
insulin dosages as needed.
• Monitor for signs of hypoglycemia (low blood sugar) such as
sweating, shakiness, dizziness, confusion, and rapid
heartbeat.
• Promptly treat hypoglycemia with a fast-acting source of sugar,
like glucose tablets or fruit juice.
• 
 nursing implications:
• Teach patients the proper technique for insulin administration
and stress the importance of regular dosing at prescribed
times.
• Emphasize the significance of a balanced diet, regular
exercise, and medication adherence for successful diabetes
management.
• Change injection sites frequently to avoid fat hypertrophy.
• Reduce dose in renal impairment.
• Use the right syringe for the right dose.
• Another nurse to counter check before administering drug.
• Encourage patients to wear medical identification indicating
 cont.
• Ensure accurate insulin dosage and concentration.
• Regularly monitor blood glucose levels and adjust insulin
doses as needed.
• Teach patients to recognize and manage hypoglycemia
and hyperglycemia.
• Assess patients' medical history and health status before
starting insulin.
• Promote proper insulin storage and site rotation for
injections.
• Be aware of potential drug interactions affecting insulin
action or glucose levels.
 II. ORAL HYPOGLYCEMICS

• These are drugs administered orally to lower blood

glucose level used in mild diabetes.
• They are grouped as Sulphonylureas and Biguinides.
 SULPHONYLUREAS

These compounds are chemically related to sulphonamides.

• First generation: Tolbutamide, Chlorpropamide 100-250mg
od 500mg in severe diabetes
• Second generation: Glibenclamide (Doanil) 5mg daily ,
Glipizide
• Mechanism: hypoglycemic action is due to Stimulation of
insulin release from β cell, Depression
• of glucagon secretion, Increase number of insulin
receptor, Reduce insulin output from liver
• (Decrease hepatic gluconeogenesis and glycogenolysis)
 CONT.

• Pharmacokinetics: They are rapidly absorbed from the

gastrointestinal tract. They are also extensively plasma
protein bound and are mainly metabolized in the liver.
• Use: Mild diabetes mellitus in old patients (type II)
• Adverse reaction: The toxicity of these compounds is
remarkably low. The important toxic effects include:
hypoglycemia, allergic skin rash and bone marrow
depression, cholestatic
• jaundice (esp. chlorpropamide)
 CONT.
• Side effects: Gastric irritation, prolonged hypoglycemia (esp.
chlorpropamide), large doses cause
• confusion, vertigo ( loss of balance), ataxia, leukopenia,
aggranulocytosis, thrombocytopenia, and teratogenecity
• Drug interaction:
• 1. Hypoglycemia is enhanced by sulphonamides, phenylbutazone
• 2. Alcohol produces “Disulfirum” like action (flushing of the face,
severe headache,
• vomiting etc.)
• 3. Sulphonylureas increase anticoagulant effect of oral
anticoagulant
• 4. Thiazides oppose the action of sulphonylureas.
 BIGUINIDES
• They potentiate the hypoglycemic action of insulin and
sulphonyl ureas but they don’t produce clinical
hypoglycemia in diabetics.
• Biguanides include drugs like metformin and
phenformin
• Mechanism: They do not stimulate the release of
insulin. They increase glucose uptake in
• skeletal muscle, and have effects on glucose
absorption and hepatic glucose production.
• They also enhance anaerobic glycolysis.
 CONT.

• Pharmacokinetics: Phenformin and metformin

are rapidly absorbed from the gastrointestinal
• tract. Metformin is largely excreted unchanged in
the urine and has a longer duration of action.
• Side effects: Nausea, vomiting, anorexia,
diarrhea, abdominal cramp, lactic acidosis (esp.
• phenformin)
 cont.
• Phenformin 200 – 400MG BID
• ROUTE; ORAL
• Contraindications; insulin dependent diabetes, diabetic
coma, ketoacidosis, trauma, severe infection, heart failure,
renal or hepatic impairment
• Metformin 500mg od
• Take the drug with meal
 CONT.

• Use: Obese diabetics (uncontrolled by diet alone),

Supplement to sulphonyl urea
• Contraindication: Diabetes with hepatic, renal
insufficiency, In IDDM, NIDDM (with
• infection, fever, surgery) and during pregnancy
• They have no value in diabetes complicated by
acidosis or coma
• GLUCAGON
TX OF HYPOGLYCAEMIA
• Indications: hypoglacimia
• Cautions: insulinoma, glucagonoma;
• ineffective in chronic hypoglycaemia, starvation, and adrenal
insufficiency
• Contra-indications: phaeochromocytoma
• Side-effects: nausea, vomiting, abdominal pain,
• hypokalaemia, hypotension, rarely hypersensitivity reactions
• Route/Dose Insulin-induced hypoglycaemia, by subcutaneous,
• intramuscular, or intravenous injection, ADULT and
• CHILD over 8 years (or body-weight over 25 kg),1 mg; CHILD under 8
years (or body-weight under 25 kg), 500 micrograms; if no response
within 10 minutes intravenous glucose must be given
 TX Chronic hypoglycaemia
• Diazoxide, administered by mouth, is useful in the
• management of patients with chronic hypoglycaemia
• from excess endogenous insulin secretion, either from
• an islet cell tumour or islet cell hyperplasia. It has no
• place in the management of acute hypoglycaemia.
• DIAZOXIDE
• Indications: chronic intractable hypoglycaemia (for
• use in hypertensive crisis.
 cont.
• Cautions: ischaemic heart disease, pregnancy, labour,
impaired renal function
• monitor blood pressure; during prolonged use monitor white
cell and platelet count, and in children,regularly assess growth,
bone, and psychological development;
• Side-effects anorexia, nausea, vomiting, hyperuricaemia,
hypotension, oedema, tachycardia, arrhythmias,
• DoseBy mouth, ADULT and CHILD, initially 5 mg/kg daily in
 the end
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