SYSTEMIC PHARMACOLOGY

- RESPIRATORY SYSTEM PHARMACOLOGY

- ENDOCRINE SYSTEM PHARMACOLOGY

RESPIRATORY SYSTEM PHARMACOLOGY

DRUGS ACTING ON THE RESPIRATORY SYSTEM

The respiratory system, which extends from the nose to the pulmonary capillaries, performs
the essential function of gas exchange between the body and its environment. In other
words, it takes in oxygen and expels carbon dioxide. Drugs used to improve respiratory
symptoms are available in inhalation and systemic formulations. These include:

 beta2-adrenergic agonists
 anticholinergics
 corticosteroids
 leukotriene modifiers
 mast cell stabilizers
 methylxanthines
 expectorants
 antitussives
 decongestants.

PHARMACOTHERAPY OF BRONCHIAL ASTHMA

Drug used in the treatment of bronchial asthma can be grouped into three main categories:

1. Bronchodilators

There are three main types of bronchodilators;

 Beta 2- agonists
 Anticholinergic agents
 Methylxantine

A. β- Adrenergic agonists which include: ƒ

i. .Short Acting Drugs; quickly relieve or stop sudden (acute) asthma symptoms. They are
effective for 4 to 6 hours. It is also known as rescue inhaler . Examples are; albuterol,
levalbuterol, terbutalin, metaproterenol

ii. Long Acting Drugs keeps airways open for 12hours.It is used every day to prevent
asthma attacks .Eg are: salmeterol and formoterol

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A. β- ADRENERGIC AGONISTS (SYMPATHOMIMETIC AGENTS)

a) Non- selective- β-agonists

- Epinephrine, ephedrine, isoprotenerol

b). Selective β-agonists

- Salbutamol, terbutaline, metaproterenol, salmeterol, formaterol etc

Mechanism of Action of beta adrenergic agonists

They bind with beta 2 receptor and stimulate adenyl cyclase and increase formation of
cAMP in the airway tissues. Which

- Relax smooth muscles

- Inhibit release of inflammatory mediator or broncho constricting substances from
mast cells.
- Inhibit microvasculature leakage
- Increase mucociliary transport

PHARMACOTHERAPY OF SOME BRONCHODILATORS

i.. ALBUTEROL

Group ; bronchodilators/ beta adrenergic agonist

MOA; they bind to β-2 receptor in the bronchial smooth muscle to increase the synthesis of
adenyl cyclase (which converts ATP to cAMP) causing bronchodilation

INDICATIONS;

- bronchial asthma,
- bronchospasm
- bronchoconstriction

CI;

- Hypersensitivity to the drug

SE;

- tarchyphylaxis
- cardiac arrythmias
- hypoxemia,

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 - tachycardia
- hyperglycemia
- hypokalemia
- hypomagnesemia
- nervousness
- skeletal muscle tremor
- occasional weakness

Dosage ; 4mg/2mg , is mostlly prescribed bd

Nsg implication;

- monitor vital signs

- positioning,
- health education

ii. SALMETEROL

Group;. bronchodilators/ beta adrenergic agonist

MOA; they bind to β-2 receptor in the bronchial smooth muscle to increase the synthesis of
adenyl cyclase (which converts ATP to cAMP) causing bronchodilation

INDICATION;

 Prevention of asthma attack

 Exercise- induced bronchospasm
 Chronic obstructive pulmonary dx( COPD) eg emphysema and chronic bronchitis

CI;

 Allergic reaction
 Worsening asthma symptoms

SE;

 Severe headache
 Blurred vision
 Chest pain
 Fast or irregular heart beat

DOSAGE; Inhalation powder (50mcg). PRN

Nsg implication;

- monitor vital signs

- position ,

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 - health education

iii. EPINEPHRINE

Group; Non selective beta 2 agonist /bronchodilator

MOA ; They bind to β-2 receptor in the bronchial smooth muscle to increase the synthesis of
adenyl cyclase (which converts ATP to cAMP) causing bronchodilation

INDICATION ; Acute asthmatic attack

CI ; -

- hypertension,
- arrhythmia,

SE ; -

- arrhythmia and
- worsening of angina pectoris,
- increase blood pressure
- tremors

Route ; parenteral

Dosage ; 0.1 – 0.25mg IV

Nursing implication ;

- administer slowly
- observe vital signs
- health education

B. METHYLXANTHINES

Methylxanthines, also called xanthines, are used to treat breathing disorders.

Examples of methylxanthines include:

• aminophylline
• anhydrous theophylline
• oxtriphylline.

Aminophylline and oxtriphylline are theophylline derivatives. Theophylline is the most

commonly used oral methylxanthine. Aminophylline is preferred when IV methylxanthine
treatment is required.

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When methylxanthines are given as an oral solution or a rapid release tablet, they’re
absorbed rapidly and completely. They’re converted in the body to an active form, which is
principally theophylline. High-fat meals can increase theophylline concentrations and
increase the risk of toxicity..

Mechanism Of Action:

Inhibition of phosphodiesterases enzyme (leading to increase concentration of cAMP) and

decrease inflammatory mediators from mast cells, resulting in bronchodilation and anti-
inflammatory action on the airways

I. Aminophylline (Diethylamine)

Group ; Bronchodilators

Indication ; - asthmatic attack

- Status asthmaticus
- COPD

CI ;

- Hyperthyroidism
- PUD
- Uncontrolled seizure disorder
- Uncontrolled arrhythmias
- Hypersensitivity

Side Effects

- Anorexia,
- nausea vomiting
- abdominal discomfort
- headache
- anxiety
- insomnia
- seizures
- arrhythmias

Route ; parentarally/oral

Dosages; IV 200 – 500mg, PRN, oral 100 – 300mg. BD

Nursing implication;

- Use full glass of water orally

- IV drug should be diluted in dextrose

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 - Encourage pt to take liberal fluid to decrease mucous viscosity
-

Theophylline is now largely reserved for patients in whom symptoms remain poorly
controlled despite the combination of regular treatment with an inhaled anti- inflammatory
agent and as needed use of a ß2 agonist.

C. ANTICHOLINERGICS AGENTS

Anticholinergics competitively antagonize the actions of acetylcholine and other cholinergic

agonists at receptors. . They are useful as alternative therapies for patients intolerant of β
agonists.

Although oral anticholinergics generally aren’t used to treat asthma and COPD because of
their tendency to thicken secretions and form mucus plugs in the airways. Anticholinergics
agents appear to be of significant value in chronic obstructive pulmonary diseases - perhaps
more than asthma

E.g Ipratropium bromide, atropine sulphate

MODE OF ACTION ANTICHOLINERGIC AGENTS

Anticholinergic agents competitively

 inhibit effect of acetylcholine at cholinergic receptors

 hence block the bronchoconstriction of air way smooth muscle and the increase in
secretion of mucus that occurs in response to vagal activity

1. IPRATROPIUM BROMIDE

Group ;antimuscarinic bronchodilators / anticholinergic

MOA ; Blocks cholinergic agents resulting to relaxation of respiratory tracts and

bronchodilation that enables inspiration and exhalation

INDICATION

- Chronic asthma
- COPD
- Bronchopneumonea

CI;

- Glaucoma
- Paradoxical bronchospasm
- BPH

Dosage;

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 - Adult ; 20 – 40mcg, tds
- Paed ; 20mcg tds

Route; oral/inhalation

SE;

- Constipation
- Tachycardia
- Atrial fibrillation
- Urine retention
- Dry mouth

Nursing implication

• Assess the patient’s respiratory condition before therapy and regularly

thereafter.
• Educate the pt on the drug.
• Be alert for adverse reactions

The addition of ipratropium enhances the bronchodilation produced by nebulized albuterol

in acute severe asthma

3. CORTICOSTEROIDS (ANTI-INFLAMMATORY AGENTS)

Corticosteroids are anti-inflammatory agents available in both inhaled and systemic

formulations for the short- and long-term control of asthma symptoms. This class consists of
many drugs with differing potencies

Corticosteroids commonly used are hydrocortisone, predinisolone, beclomethasone,

triamcinolone, budesonide etc. The drugs can be taken by inhalation as aerosol, oral, or an
IV administration. Used both for treatment and prophylactic purposes

Mechanism Of Action corticosteroid

 inhibition of cytokine and mediator release

 decrease in mucus secretion
 up regulation of β–adrenoceptor numbers
 inhibition of IgE (Immunoglobulinb E) synthesis
 reversing mucosal edema
 decreasing permeability of capillaries
 inhibiting release of leucotrienes

Because of severe adverse effects when given chronically, oral and parenteral
corticosteroids are reserved for patient who need urgent treatment and those who have not
improved with bronchodilator.

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Aerosol treatment is the most effective way to decrease the systemic adverse effect of
corticosteroid therapy

Doses should be decreased after improvement. Regular or controlled therapy is better

maintained with aerosol corticosteroids.

1. HYDROCORTISONE

Group ; anti-inflammatory/corticosteroid

INDICATION;

- Urgent treatment of severe asthma not improved with bronchodilator

- Nocturnal asthma prevention
- Chronic asthma

CI;

- PTB
- Hypersensitivity

Side effects:

- Suppression of the hypothalamic

- pituitary-adrenal axis
- Osteoporosis
- Sodium retention and hypertension
- Cataract
- Impairment of growth in children
- Susceptibility to infection like oral candidiasis, tuberculosis

Dosage; 100 - 200mg PRN

Route; parenteral

Nsg implication ;

- Diet low in sodium and high in K should be recommended

- Monitor vital signs

2. BECLOMETASONE

GROUP ; anti-inflammatory/corticosteroid

MOA ; inhibition of cytokine and mediator release, attenuation of mucus secretion,

upregulation of β–adrenoceptor numbers, inhibition of IgE synthesis, reversing mucosa
edema, decreasing permeability of capillaries, inhibiting release of leucotrienes

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INDICATION;

- Uncontrolled asthma by short acting bête agonist

- Allergic reaction

5. MAST CELL STABILIZERS

Mast cell stabilizers are used for the prevention and long-term control of asthma, especially
in pediatric patients and patients with mild disease. These drugs aren’t effective in the
management of an acute asthma attack. Medications in this class include nedocromil and
cromolyn sodium

Mechanism of action

Stabilize the mast cells so that release of histamine and other mediators is inhibited through
alteration in the function of delayed chloride channel in cell membrane. It has no role once
mediator is released and is used for casual prophylaxis.

CROMOLYN SODIUM

GROUP ; Mast cell stabilizers

INDICATION ;

- Mild/moderate bronchial asthma

- Adjunctive treatment of allergic rhinitis
- Exercise/antigen induced asthma

MOA ; prevents release of inflammatory mediators including histamine and leucotrienes

thereby resulting to bronchodilation

CI ;

- Hypersensitivity

SE ;Depends on the route of admistration

Dosage

- oral 100mg/5ml
- nasal spray ; 5.2mg/ 1 actuation
- inhalation solution ; 10mg/ 1ml

Nsg implication

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 - monitor vital signs
- observe for reaction
-

TREATMENT OF STATUS ASTHMATICS

Status asthmatics Very severe and sustained attack of asthma which fails to respond to
treatment with usual measures

Management includes

 Administration of oxygen
 Frequent or continuous administration of aerosolized ß2 agonists like salbutamol
 Systemic corticosteroid like methyl prednisolone or hydrocortisone IV
 Aminophylline IV infusion
 Iv fluid to avoid dehydration
 Antibiotics in the presence of evidence of infection

DRUGS USED IN MANAGEMENT OF COUGH

ANTI-TUSSIVES

Anti-tussives are drugs used to suppress the intensity and frequency of coughing.
Antitussive drugs suppress or inhibit coughing. They’re typically used to treat dry,
nonproductive coughs. The major antitussives include:

• benzonatate
• codeine
• dextromethorphan hydrobromide
• hydrocodone bitartrate

Cough is a protective reflex, which serves the purpose of expelling sputum and other irritant
materials from the respiratory airway.

Types:

I. Useful productive cough;

- Effectively expels secretions and exudates

II. Useless cough ; Non-productive chronic cough

- Due to smoking and local irritants

Two Types of Anti-tussives:

1. Central anti- tussives

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 - Suppress the medullay cough center and may be divided into two groups:

I. Opoid antitussive e.g. codeine, hydrocodeine, etc

II. Non opoid antitussives e.g. dextromethorphan

2. Peripheral antitussives

Decrease the input of stimuli from the cough receptor in the respiratory passage.

e.g: Demulcents e.g. liquorices lozenges, honey

Demulcents coat the irritated pharyngeal mucosa and exert a mild analgesic effect locally.
CODEINE

Codeine is a narcotic relatively less addicting drug and central antitussive agent and it’s
main side effects are dryness of mouth, constipation and dependence.

1. CODEINE

Group ; Antitussive/ narcotic

MOA: These drugs act in the central nervous system to raise the cough threshold or act
peripherally in the respiratory tract to reduce the cough (tussal) impulses i.e suppress the
frequency of cough, or both of these actions

INDICATION : narcotics are use to control (dry cough)

DOSE : codeine 10-30mg TID

Route ; oral

SIDE EFFECTS:

- Constipation
- , respiratory
- depression,
- drowsiness

NON-OPIOD/NARCOTICS, these include noscapine, dextromethorphan, chlophedianol (all

indicated in dry cough)

2. NOSCAPINE – depresses the cough centre with no narcortic activity or dependance

properties.

Dosage ; 15-30mg, TDS

Route; oral

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3. DETROMETHORPHAN.

Group ; Anti tussive

Dosage; 10 -20 mg, TDS

Route ; oral

4. CHLORPHEDIANOL - it has slower onset but longer duration of action.

Group ; Antitussive

INDICATION ; Dry cough

Dosage; 20 – 40 mg, TDS

Route; oral

2. MUCOLYTIC AGENTS

i. BROMHEXEINE : is a derivative of vasicine alkloid. It is a potent mucolytic and mucokinetic

agent. It is in form of tablet or syrup

INDICATION; Productive cough

MOA : it breaks or depolarises mucopolysaccharides (network of fibre in tencious sputum)

as well s liberate lysosomal enzymes.

DOSES : 8 mg or 4mg/5ml, TDS

Route ; oral

Ii ACETYLCYSTEINE : its a mucolytic agent as it splits the disulphide bond in mucin or

mucoprotein (carbohydrate polymer of mucus) sputum

DOSE : 200 mg/ml injection in 1, 2, 5 ml ampoules.

Route ;nebulizer or instillation

iii. CARBOCISTEINE : it is same as acetylcysteine but administration is orally. Dose is 250 –

750 mg TDS. Patients chronic bronchitis can benefit from the drug

SIDE EFFECT : irritation, rash

DOSES : 8 mg or 4mg/5ml

EXPECTORANTS

Expectorants increase bronchial secretions, which, in turn, thin mucus so that it’s cleared
more easily out of airways. The most commonly used expectorant are; guaifenesin, (a

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common component of over-the-counter (OTC) cold and flu medications), coflin, emzolyn,
Tussylin, Neofylin, Nomalin

MODE OF ACTION

Expectorants reduce the viscosity of tenatious secretions by irritating the gastric vagal
receptors that stimulate respiratory tract fluid, thus promote ciliary action and facilitates
mucous removal

1. GUAEFENESIN

Group ; Expectorant

MOA; Increases the output respiratory tract fluid by reducing the adhesiveness and surface
tention thereby promoting ciliary action and facilitating mucous removal

INDICATION; Productive cough

CI ; Hypersensitivity

SE ;

• vomiting (if taken in large doses)

• diarrhea
• drowsiness
• nausea
• abdominal pain
• headache
• hives or skin rash

Dosage;

Adult; 10 – 15ml tds

Children ; 2.5 – 5ml tds

Route ; oral

2. EMZOLYN

Group ; Expectorant

MOA; Increases the output respiratory tract fluid by reducing the adhesiveness and surface
tention thereby promoting ciliary action and facilitating mucous removal

INDICATION; Productive cough

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CI ; Hypersensitivity

SE;

• diarrhea
• drowsiness
• nausea
• abdominal pain
• headache
• Vomiting

Dosage; adult; 5 – 10ml tds. Children ;2.5 – 5ml tds

Route ;oral

Nursing implication;

Do not take the drug;

- when or before driving

- when operating machines
- When patient has respiratory distress syndrome

DECONGESTANTS

Decongestants are the drugs that reduce congestion of nasal passages, which in turn open
clogged nasal passages and enhances drainages of the sinuses. e.g phenylephrine,
oxymetazoline etc.

Mechanism of Action

Mucus membrane decongestants are α1 agonists, which produce localized vasoconstriction

on the small blood vessels of the nasal membrane. Reduce congestion in nasal passages.

Clinical uses:

Used in congestion associated with rhinitis, hay fever, allergic rhinitis and to a lesser extent
common cold. Drugs can be administered nasally or orally for longer duration of action.
Classification:

1. Short acting decongestants administered topically

– phenylepherne, phenylpropanolamine

2. Long acting decongestants administered orally

- ephedrine, pseudoephedrine, naphazoline

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3. Long acting topical decongestants;

 Xylometazoline
 oxymetazolin

Side effects:

 Rebound nasal congestion

 Ischemic changes in mucus membranes
 Nasal burning, stinging, dryness
 Tachycardia, arrhythmia, nervousness, restlessness, insomnia, blurred vision

Contraindications

1. Hypertension, severe coronary artery disease

LEUKOTRIENES

Leukotriene modifiers are used for the prevention and long-term control of mild asthma.
There are two types:

• Leukotriene receptor antagonists include zafirlukast and montelukast.

• Leukotriene formation inhibitors include zileuton.

Leukotrienes (LT) are fatty acid-derived mediators containing a conjugated triene structure.
They are formed when arachidonic acid is liberated from the cell membrane of cells, as a
result of cell activation by allergic or other noxious stimuli.

ZAFIRLUKAST

Group ; Leukotrienes receptor antagonist

MOA ; It blocks cysteinnyl leukotriene in the airways thereby enhancing respiration in

asthmatic patients

Indication ; prevention and long-term control of mild asthma.

CI ;

- Hypersensitivity
- Pregnancy
- Renal impairment
- Unstable asthma

SE;

• headache
• dizziness

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 • nausea and vomiting
• myalgia
• cough

Dosage ; 20mg twice daily for adult and 12year child

Route; oral

Nsg implication ;

- to be taken before meal for rapid absorption

- to be taken with full glass of water to prevent abdominal upset
- advise patient to avoid hazardous activities
- monitor vital signs

ENDOCRINE PHARMACOLOGY
The endocrine system consists of glands, which are specialized cell clusters, and hormones,
the chemical transmitters secreted by the glands in response to stimulation
Together with the central nervous system, the endocrine system regulates and integrates
the body’s metabolic activities and maintains homeostasis (the body’s internal equilibrium).
The drug types that treat endocrine system disorders include:
I. ANTIDIABETIC DRUGS
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.
The common Signs and symptoms include
- Polydipsia

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 - Polyphagia
- Polyuria
- Dehydration due to glucosuria.
Diabetes has dangerous complications: including
- Ketoacidosis (in types I)
- Hyperglycemic osmolal non ketotic coma (in type II)
- Cardiovascular (like atherosclerosis, myocardial infarction, peripheral arterial
insufficiency, Anemia, Hypertension,stroke), nephropathy, retinopathy, neuropathy.

It can be classified as:

 Type I: IDDM (or Juvenile type) occurs predominantly in children and young adults who
have no insulin secretion
 Type II: NIDDM (or maturity onset type) usually occur after the age of 40years.
Diabetic ketoacidosis (DKA) is serious complication of diabetes. It is severe metabolic
disturbance due to insulin deficiency, which results in hyperglycemia, ketonimia and later
acidosis. It is characterized by headache, nausea, vomiting, rapid pulse, dry skin, deep
breathing, and change in mentation.

ANTIDIABETOGENIC DRUGS
I. INSULIN
Sources include pork or beef, combination of pork and beef and also human insulin
(Recombinant DNA technique)
Actions: -
- Insulin lower blood glucose level through increasing utilization of glucose by
peripheral tissue and promoting synthesis and storage of glycogen
- The main actions of the hormone are exerted on metabolism of carbohydrate
(CHO), fat and protein in liver, muscle & adipose tissue.
Effects of insulin
Carbohydrate metabolism

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- Liver: it increases glycogen synthesis from glucose and glucose utilization while
decreases gluconeogenesis and glycogenolysis
- Muscle: it increases glucose uptake, glucose utilization and glycogen synthesis.
- Adipose tissue: it increases glucose uptake and glycerol synthesis
Fat metabolism
- Liver: it increases lipogenesis
- Adipose tissue: it increases synthesis of triglycerides and synthesis of fatty acid

Protein metabolism
- Liver: it increases protein catabolism
- Muscle: it increases amino acid uptake and protein synthesis
Other metabolic effect:
- It increases uptake of K+ and Ca++ into cells
- synthesis of nucleic acids
Factors that increase insulin demand:
- Infection
- surgery
- pregnancy
- drugs (those that antagonize actions of insulin glucocorticoids, thyroid hormone,
adrenaline
Type of insulin preparation:
 Short acting (rapid onset)
 Intermediate acting
 Long acting
1. SHORT ACTING
- It is absorbed quickly from fat tissue into blood stream
- Used to control blood sugar during meals and snacks
- To correct high blood sugar
- This type of insulin are administered 15 minutes before meal and have a plasma
peak level of 1-2hours with a duration of action of 4-6hours
Examples ;
Rapid acting insulin( Insulin Aspart, Insulin Lyspro)

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2. INTERMEDIATE ACTING INSULIN
- It is absorbed more slowly and lasts longer
- Used to control blood sugar overnight, while fasting and between meals
- This type of insulin are administered 1 hour before meal and have a plasma peak
level of 4-10 hours with a duration of over 12 hour
Examples; Lente insulin, NPH(Neutral Protamine Hagedorn) Insulin

3. LONG - ACTING INSULIN

- It is absorbed slowly, has a minimum peak effect and a stable plateau effect that
lasts most of the day
- Used to control blood sugar overnight, while fasting and between meals
- This type of insulin are administered 1hour 30 minutes before meal with no plasma
peak level but have a duration of action over 24hours.

Examples; Protamine Zn Insulin, Glargine insulin, Detemir Insulin

TYPES ROUTE ONSET in hrs DURATION(hrs)

1. Regular insulin IV, SC , IM ¼-1 4–6
2. Lente insulin SC, IM 1- 2 12 - 24
3.Protamine Zn SC, IM 4- 8 24
Insulin

N.B. It is only regular 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.
- Hyperkalaemia due to renal failure
Adverse Reaction: can be categorized as

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Local:
- Atrophy or hypertrophy at site of injection
- local hypersensitivity and secondary infections.
Systemic:
- Hypoglycemic coma
- Immunologic reaction like hypersensitivity
- Insulin resistance

II. ORAL HYPOGLYCEMIC

These are drugs administered orally to lower blood glucose level used in mild diabetes. Oral
hypoglycaemic drugs are useful in type 2 diabetes as adjuncts to continued dietary restraint.
They fall into four groups:
 Sulphonylureas and related drugs
 Biguanides
 Thiazolidinediones (glitazones)
 α-glucosidase inhibitors (acarbose)
1. SULPHONYL UREAS
Sulfanyl ureas are oral hypoglycaemic agent that act on beta cell of the pancreas to increase
insulin secretion. Example are glibenclamide, glipizide
These classified into ;
- First generation: Tolbutamide, Chlorpropamide
- Second generation: Glibenclamide, Glipizide
Mechanism of action
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)
INDICATION: Mild diabetes mellitus in old patients (type II)
1.GLIBENCLAMIDE (DUONIL)

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Group : Sulfanylureas
M.O.A It act on beta cell of the pancreas to increase insulin secretion.
Side effect
- Nausea
- dizziness and
- hypoglycemia
Contraindication type one diabetes melietus
Dosage 5mg/tablet
Nursing implications
monitor patent blood glucose level
Other sulfanyl ureas include Glipizide
2. BIGUANIDES
These are oral hypoglycemic agent that increase the sensitivity of insulin to its receptors at
tissue level. Example
METFORMIN (GLUCOPHAGE )
Group ; Biguanide/ Oral hypoglycemic agent
Indication type 2 diabetes
Contra indication :
- type 1 diabetes
- gestational diabetes
M.O.A it increase the sensitivity of insulin to its receptors at tissue level there by facilitating
glucose uptake by the body cell.
Side effect:
- lactic acidosis
- nausea vomiting
Dosage 500mg/tablet
Nursing implications monitor patient blood glucose level
3.THIAZOLIDINEDIONES (GLITAZONES)
Glitazones (e.g. piolitazone, rosiglitazone) were developed from the chance finding that a
fibrate drug increased insulin sensitivity
Glitazones lower blood glucose and haemoglobin A1c (HbA1c) in type 2 diabetes mellitus
patients who are inadequately controlled on diet alone or diet and other oral hypoglycaemic

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drugs. An effect on mortality or diabetic complications has yet to be established, but they
have rapidly become very widely used.
MECHANISM OF ACTION GLITAZONES
Bind to the peroxisome-proliferating activator receptor γ (PPARγ), a nuclear receptor found
mainly in adipocytes and also in hepatocytes and myocytes. It works slowly, increasing the
sensitivity to insulin possibly via effects of circulating fatty acids on glucose metabolism
PIOGLITAZONE
Group; GLITAZONES
MOA; Bind to the peroxisome-proliferating activator receptor γ (PPARγ), a nuclear receptor
found mainly in adipocytes and also in hepatocytes and myocytes. It works slowly,
increasing the sensitivity to insulin possibly via effects of circulating fatty acids on glucose
metabolism
INDICATION; TYPE 2 D/M
CI;
- Patient with hepatic impairment
- Hypersensitivity
- pregnancy
SE;
- blurred vision
- flushed and dry skin
- headache
- increased thirst
- increase voiding
- muscles pain
Dosage ; 15mg,30mg, 45mg
15 – 30mg daily
Route ; orally
Nursing implications monitor patient blood glucose level
4. Α-GLUCOSIDASE INHIBITORS
Are used in type 2 diabetes mellitus in patients who are inadequately controlled on diet
alone or diet and other oral hypoglycaemic agents. Eg Acarbose is a reversible competitive

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 inhibitor of intestinal α-glucoside hydrolases and delays the absorption of starch and
sucrose, but does not affect the absorption of ingested glucose.
ACARBOSE
Group ; α-glucosidase inhibitors the digestion of CHO
MOA ; Delays the digestion of CHO,slows glucose absorption resulting in a reduction of
postprandial glucose blood concentration
INDICATION; Type 2 D/M
CI ;
- diabetes ketoacidosis
- liver cirrhosis
- inflammatory bowel dx
- hypersensitivity
SE;
- Diarrhoea,
- gas,
- abdominal discomfort
Dosage; 25, 50 and 100mg respectively
 Initially 25mg orally 8hlrly
 Can be increased to 50 or 100mg 8hrly at 4 to 8weeks interval based on 1hr postprandial
glucose
Route; oral
Nursing implications monitor patient blood glucose level
DRUGS USED IN THE TREATMENT OF HYPOTHYROIDISM
Hypothyroidism is condition in which the thyroid gland does not produce enough thyroid
hormone. The drugs that be used in the treatment of this, include;thyroxine sodium,
Liothyroxine
1. THYROXINE SODIUM (LEVOTHYROXINE SODIUM)
GROUP ; Thyroid drug
INDICATION; Hypothyroidisim
CI;
- Thyrotoxicosis,
- d/m,

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 - d/ insipidus,
- pregnancy,
- cvs dx,
- breastfeeding,
- hypopituitarism

DOSAGE; adult; 50 to 100mcg daily for 3 weeks

For neonate/children; 5 to 10mcg
Route; oral
SE;
- angina pain
- arrhythmias
- palpitation
- Diarrhoea
- vomiting.
- Tremor
- insomnia,
- headache etc
MOA;After entering cells it is converted to T3, which binds to the thyroid hormone nuclear
receptor and the ligand–receptor complex increases transcription of genes involved in the
following cellular functions
- stimulation of metabolism – raised basal metabolic rate;
- promotion of normal growth and maturation, particularly of the central nervous system
and skeleton;
- sensitization to the effects of catecholamines.
Nursing implication
- Start with small dose
- Administer on empty stomach in the morning
- Educate the patient
- Assess vital signs
- Asses for weigh reduction
DRUGS USED IN THE TREATMENT OF HYPERTHYRODISM

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 Antithyroid drugs include:
 Thiourea compounds, e.g. , carbimazole propylthiouracil, methimazole
 Ionic inhibitors, e.g. , potassium percholate, potassium thiocyanate
 Iodide, e.g. , Lugol’s iodine, potassium iodide
 Radioactive iodine
CARBIMAZOLE
GROUP ; Anti thyroid
MOA; It is carbethoxy derivatives of methimazole, which is converted to its active form of
methimazole, prevents the thyroid peroxidase enzyme from coupling and iodinating the
tyrosine residues on thyroglobulin, thereby reducing the production of the thyroid
hormones T3 and T4
INDICATION; Thyrotoxicosis
CI;
- Tracheal obstruction,
- breatfeeding,
- pregnancy
Dosage; 20 - 60mg daily for 4 – 8weeks
Child; 15mg dly
Route; oral
SE;
- nausea,
- headache,
- arthralgia.
- alopecia.
- hepatitis,
- blood disorder
PROPYLTHIOURACIL
Group; anti thyroid
INDICATION; Hyperthyroidism
MOA; , prevents the thyroid peroxidase enzyme from coupling and iodinating the tyrosine
residues on thyroglobulin, thereby reducing the production of the thyroid hormones T3 and
T4

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 CI ;
- huge goitre
- pregnancy
- breastfeeding
- hepatic impairment
Dosage ; adult 300 – 600mg daily, may reduced gradually to maintenance dose of 50 150mg
dly ( until patient becomes euthyroid dose)
Route ; oral
SE
- nausea
- arthralgia,
- headache
- pruritis
- alopecia,
- cutaneous vasculitis
- tyhrombocytopenia
- hepatic necrosis
Nursing implication
- Assess for blood thyroxine estimation
- Educate the patient
- Assess vital signs
- Asses for weight reduction
ADRENCORTCCAL HORMONES
Adenocortical hormones control the metabolism of carbohydrate (CHO), protein, fat and
water /electrolytes
Adencortical hormones are classified into:
 Glucocorticoid - Cortisone - Hydrocortisone (Cortisol)
 Mineralocorticoid - Aldosterone – Desoxycorticosterone
 Sex Hormone - Estrogen - Androgen
Glucocorticoids
The important glucorticoid secreted in man is hydrocortisone. It posseses some
mineralocorticoid activity as well.

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 Cortisone is less potent and is converted to hydrocortisone by liver.
They are classified as
 Short acting e.g cortisone, hydrocortisone
 Intermediate acting e.g predinsolone, triamcinolone
 Long acting e.g dexamethasone, betamethasone)

Dexamethasone and betamethasone have got a high glucorticoid activity while cortisone
and hydrocortisone have high mineralocorticoid action. Therapeutic activity in inflammatory
disorder is proportional to the glucocorticoid activity.
Actions on CHO metabolism:
- antinsulinic effect
- decreases Peripheral utilization of glucose
- , - increases gluconeogenesis
- promote glycogen storage
Protein metabolism:
- Inhibit protein synthesis,
- Increases catabolism
- Fat metabolism:
- Interferes with fat storage causing deposits with characteristic distribution (neck,
supraclavicular area, and face
Electrolyte and H2O metabolism
- Sodium and water retention
- Hypokalmia Suppression of pitutary adenocortical
SYSTEMS;
CNS:
- Euphoria and stimulation
CVS:
- Restore vascular reactivity
GIT:
- Increase gastric acid secretion
Blood:
- Increase number of RBC,

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 Hypercoagulability Uric acid:
- Increased excretion
Calcium metabolism:
- increased Ca++excretion,
- interfere with Ca++ absorption

Antinflammatory:
- Inhibit exudation,
- capillary dilatation,
- migration of phagocyte, fibroblast,
- inhibit fibrous tissue formation
Antiallergic:
- Absorption and fate: through inhibition of antibody production suppress tissue
inflammatory response.
It has fair absorption,
- bound to α -globuin (transcortin).
- And in the liver, cortisone is converted into hydrocortisone. 140
Therapeutic use
1) Replacement therapy:
1. In Addisons disease and Addisonian crisis
2) Antinflammatory: in conditions like Collagen disease (rheumatoid carditis, arthritis),
3) Hypersensitivity reactions: (Bronchial Asthma, status asthmatic), Blood disease due to circulating
antibodies (autoimmune disease), Skin disease (eczema), Eye disease (allergic inflammation of the
eye), Nephrotic syndrome, Acute gout.
4) Immunosuppression: In tissue / organ transplantation
Nursing implication
- Check weight for fluid retention –
- Test urine for sugar –
- Follow blood pressure through measurement and
- check bones by X-ray for osteoporosis
- Doses should be tapered slowly (Don’t stop abruptly)
- Increase dose in surgery, infection
- Encourage diet rich in K+ , protein and adequate calcium, low Nacl

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- Rule- out infection before initiation of treatment
Side effects: -
- Due to prolonged use:
- Weight gain and
- edema
- hypokalmia,
- hyperglycemia,
- osteoporosis,
- psychiatric disturbance
- , susceptibility to infection (like TB),
- peptic ulceration
- , cushing syndrome,
- retarded growth

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