Drugs used in diabetes mellitus

Drugs used in DM..

• Diabetes Mellitus is a disease that occurs as a result
of absolute or relative deficiency of insulin that
results in metabolic and vascular abnormalities
• Upon ingestion of carbohydrates, insulin is released
into the blood and promotes uptake and utilization of
glucose in specific organs, namely, the heart, adipose
tissue, and skeletal muscle.
• The etiologies (causative factors) include
 Obesity: 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 (from family)
 damage of pancreatic tissue
 Other factors: Pregnancy
• The common signs and symptoms include
• Polydepsia, Polyphagia, Polyuria, dehydration due to
glucosuria
• Type I: occurs predominantly in children and young adults
who have no insulin secretion.
• It is also called insulin dependent diabetes mellitus (IDDM)
• Insulin replacement therapy is necessary to sustain life
• Type II: (or maturity onset type) usually occur after the age of
40years.
• It is also known as non-insulin dependent diabetes mellitus
(NIDDM)
• Characterized by tissue resistance to the action of insulin
combined with a relative deficiency in insulin secretion.
• Gestational Diabetes Mellitus: Defined as any
abnormality in glucose levels noted for the first
time during pregnancy.
• The complications of diabetes mellitus are:
• Ketoacidosis (in types I): is serious complication
of diabetes due to insulin deficiency
– Management includes Regular (soluble) insulin IV
infusion
• Hypoglycemic coma : due to excess dose of
insulin
– Management includes giving glucose or glucagon
 Symptom of hypoglycemia
• Difficulty concentrating
• Difficulty in speaking
• Blurred vision
• Incoordination
• Confusion
• Loss of consciousness
• Seizure
• - Give 04 teas spoon of sugar diluted in water -
Monitor every 20-30 minutes
• - If no improvement repeat the above
• - Once blood sugar improves, the patient
must take a meal or snack
• Alternatives: regular soft drinks - 200ml of
Mirinda® or Cola® contains about 20gram
sugar can replace the above
• Drugs used for treatment of DM include:
• Insulin
• The goal of insulin therapy is to replicate normal
physiologic insulin secretion and replace the
background or basal (overnight, fasting, and between-
meal) as well as bolus or prandial (mealtime) insulin.
• Sources of insulin: naturally from pork or beef, and also
human
• Actions: lower blood glucose level through increasing
utilization of glucose by peripheral tissue and
promoting synthesis and storage of glycogen
• short-acting, with rapid onset of action
– Regular Insulin
• intermediate-acting
– NPH (neutral protamine Hagedorn)
• long acting, with slow onset of action
– Insulin glargine; Protamine Zn insulin, Insulin
detemir
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Insulin types with their routes of
administration
Types Routes of administration

Regular Insulin IV, SC, IM

Lente insulin SC, IM

Protamine Zn insulin SC, IM

GD
N.B. Only regular insulin can be given by intravenous route

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• Examples of recommended insulin regimens
 Short acting insulin mixed with intermediate - acting insulin: twice
daily (before meals) Mixed NPH and regular insulin -70/30 (70% NPH & 30% regular)
 Short acting insulin mixed with intermediate acting insulin before
breakfast: Short-acting insulin before evening meal; and Intermediate-
acting insulin: at bed time
 Short-acting insulin: three times daily (before breakfast, midday and
evening meal)
 Intermediate - acting insulin at bedtime
 Intermediate-acting insulin with or without short-acting insulin once
daily either before breakfast or at bedtime suffices for some patients
with type II diabetes who need insulin, sometimes in combination with
oral hypoglycemic drugs.
• Indication:
 Treatment of type I DM,
 Treatment of type II DM not controlled by other agents
 Management of diabetic ketoacidosis
 Control of diabetes in pregnancy, during surgery and in
infections
• Adverse Reaction and complication:
• Hypoglycemia (reduced blood glucose)
• Hypertrophy (increase size) at site of injection
– Hypersensitivity reaction (insulin allergy)
 Oral hypoglycemic drugs
 MOA:increase insulin secretion
• These are antidiabetic drugs administered orally 30 minutes
before meal
• They lower blood glucose level and used in mild diabetes
 Glibenclamide (Tablet, 5mg): 2.5 mg/d-20 mg/d
 Glipizide: Tablet, 2.5mg, 5mg, 10mg
 Glimperide: Tablet, 1mg, 2mg, 4mg
 Side effect :hypoglycemia ,weight gain
 Biguanides
 MOA: work by preventing the production of glucose in the liver,
improving the body’ssensitivity towards insulin receptor
 They potentiate the hypoglycemic action of insulin and
sulphonylureas
 The only commercially available biguanides is metformin.
 Metformin (500mg-1000mg bid after meal) is effective as
monotherapy (alone) and in combination with nearly every other
therapy for type 2 diabetes
 Combinations of metformin in conjunction with glipizide, and
glyburide are available
 ADE:Nausea, vomiting, stomach upset, diarrhea, gas, weakness, or
a metallic taste in the mouth may occured
Anti-thyroid drugs
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Anti-thyroid drugs
• The normal thyroid gland secretes sufficient
amounts of the thyroid hormones
triiodothyronine (T3) and tetraiodothyronine (T4,
thyroxine)
– to normalize growth and development, body
temperature, and energy levels.

GD
• Hypothalamic  Thyroid-releasing hormone
(TRH) stimulates
• Pituitary
– Thyroid-stimulating hormone (TSH) release,
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CONT…
• TSH stimulates T4and T3 synthesis and
release from the thyroid, and they in turn
inhibit both TRH and TSH synthesis and
release.

GD
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 hyperthyrodism
• Weight loss despite increased appetite
• Excessive sweating
• Heat intolerance
• Palpitations( increase heart rate)
• Menstrual irregularity , mainly
oligomenorrhea
• Increased hair loss
• In thyroiditis there could be neck pain
 hypothyrodism
• Intolerance to cold environments,
constipation
• weight gain
• hair loss
• dry skin
• Hoarse voice
• lethargy, memory loss, depressed
reflexes(decrease heart rate)
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Thyroid hormones and anti-thyroid
I. Thyroid hormone preparations include:
thyroxine sodium
– Used in hypothyroidism (reduced secretion of
thyroid hormones)
II. Anti-thyroid drugs include:

GD
– Propylthiouracil(less cross placenta), methimazole,
carbimazole, Lugol‘s iodine, potassium iodide,
propranolol, metoprolol
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Anti-thyroid and thyroid preparations with their specific indication

Preparation Indication Dosage forms Remarks

Iodine + Potassium thyrotoxicosis (preoperative) Solution, 5% + 10% Can decrease the

Iodide size of the gland

Carbimazole Hyperthyroidism Tablet, 5mg Contraindicated

during pregnancy

Propranolol Tachycardia due to Injection 1mg/ml in Replaced by

thyrotoxicosis 1ml ampoule, Tablet, 10mg, metoprolol for

40mg

GD
asthmatic patients

Propylthiouracil Hyperthyroidism Tablet, 25mg, 50mg, preferred to

100mg carbimazole in

pregnancy

Thyroxine Sodium Hypothyroidism Tablet, 0.05mg, 0.1mg

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