Corticosteroids/ Hydrocortisone Class (Prednisolone) Group-A6

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CORTICOSTEROIDS/

HYDROCORTISONE CLASS

(PREDNISOLONE)

GROUP-A6
Nadeem Khan
Amber Fatima
Farriha Gul
Aimen Javed GROUP
Laraib Amir Ali MEMBERS
PRESENTED
BY
Nadeem Khan
STERIOD

▣ A steroid is an organic
compound with four rings
arranged in a
specific configuration.

▣ Examples:
□ Dietary lipid e.g. Cholesterol.
□ Hormones e.g. Testosterone.
□ Drugs e.g. Prednisolone.
Steroidal biosynthesis
CLASSIFICATION:

STEROIDS

HORMONES ANDROGEN,
ANDROGENIC/ANABOLIC
CORTICOSTEROID ESTROGEN AND
STEROIDS
PROGESTERON

GLUCOCORTICOID
E.G HYDROCORTISOL,
CORTISOL

MINERALOCORTICOID
E.G ALDOSTERONE
Corticosteroids

▣ Corticosteroids are a class of chemicals that includes the


steroid hormones that are produced
in the ADRENAL CORTEX of
vertebrates.

▣ The adrenal cortex is a factory of


Hormones 10 to 30 different steroids
are produce from this tissue but two
classes are more important

Steroidal class Prototype Physiological effect

Mineralocorticoid Aldosterone Na, K and water hemostasis

Glucocorticoid Hydrocortisone, Cortisol Glucose and other hemostasis


CLASSIFICATION ON BASIS OF
CHEMICAL NATURE:

CORTICOSTEROIDS

GROUP A GROUP B GROUP C GROUP D


HYDROCORTISON ACETONIDES BETAMETHASONE
TYPE ESTERS
E TYPE TYPES

GROUP D1 —
PREDNISOLONE TRIAMCINOLONE BETAMETHASONE HALOGENATED
METHYLPREDNISOLONE BETAMETHASONE (LESS LABILE)
ACETONIDE
PREDNISONE TRIAMCINOLONE SODIUM
ALCOHOL  PHOSPHATE
MOMETASONE DEXAMETHASONE
GROUP D2 —
AMCINONIDE FLUOCORTOLONE
LABILE PRODRUG
BUDESONIDE ESTERS
DESONIDE
CLASSIFICATION ON BASIS OF
ACTION AND FUNCTION:

1. MINERALOCORTICOIDS
• Aldosterone, Deoxy corticosterone,
Fludrocortisone..
2. GLUCOCORTICOIDS
• Cortisol, Cortisone, Prednisone, Prednisolone,
Methylprednisolone, Dexamethasone,
Betamethasone, Triamcinolone
MINERALOOCORTICOI
D
MINERALOOCORTICOID

▣ Adrenocortical hormones
▣ So called because of their effects on minerals in the body
e.g. Na+, Cl-and K+
concentrations in the extracellular fluid. 
▣ Responsible for maintenance of adequate
fluid volume in the extracellular and intravascular fluid co
mpartments
▣ Aldosterone is the prototype of mineralocorticoid
effects
▣ Acts on the distal tubule to enhance absorption of Na+
▣ Increase excretion of K+ and H+
▣ Similar effects occur in colon, sweat gland and salivary
gland
Effects on body.

 Hypoaldosteronism
 Dilutional hyponatraemia,
 Hyperkalamia
 Acidosis
 Massive loss of Na+ and decreased EFC volume (essential
for survival)

 Hyperaldosteronism:
 Positive Na+ balance,
 expansion of ECF,
 increased plasma Na,
 Hypokalaemia
 Alkalosis and
 progressive rise in BP – hypertension, myocardial fibrosis
etc.
GLUCOCORTICOID
2. Glucocorticoids

▣ Glucocorticoids (GCs) are a class of steroid


hormones which bind to the glucocorticoid
receptor (GR).
▣ GRs are widely distributed and located almost
in all cells of the body.
▣ Not stored:
Rate of synthesis = Rate of release
▣ Synthesize rhythmically and controlled by
irregular pulses of ACTH, influenced by light
and major pulses occur early in the morning
and after meals
▣ They are made up of almost 800 amino acids
Actions

On metabolism of glucose ,carbohydrate and fats:

• Increase blood glucose levels in two ways


Promote Gluconeogenesis
Inhibits glucose uptake by cells

• Promote catabolism of proteins . Increase aminoacid and


protein content in cell

• Mobilization and redistribution of fats


EFFECTS ON BODY

Water excretion:
Glucocorticoids play important role in maintaining normal GFR - in
adrenal insufficiency capacity to excrete water is lost – water
intoxication.

Calcium Balance:
Decrease absorption of Ca++ in GIT and increased excretion – calcium
depletion – osteoporosis.

Skeletal muscle:
Normal muscular activity needs Glucocorticoids at its optimum level
Excess level leads to muscular weakness and wasting
Muscular weakness occurs in both Hypocorticism (due to hypodynamic
circulation) and hypercorticism (due to hypokalaemia )

CNS:
Euphoria – in pharmacological doses
Addison's disease – apathy, depression and psychosis
High doses – induce seizure
EFFECTS ON BODY-CONTINUED

CVS:
□ Maintain tone of arterioles and myocardial contractility.

□ Adrenal insufficiency leads to low cardiac output and arteriolar


dilatation and poor response to adrenaline

□ Cardiovascular collapse – along with mineralocorticoids

Blood and lymphoid tissues:


• Destruction of lymphoid tissue – modest in normal persons

• In presence of malignancy of lymphatic cells – lytic actions are


significant (apoptosis) – used in lymphomas (Basis of Use)

• Minor effects on haemoglobin and RBCs – protect against


haemolysis of RBCs – Increase in number of RBCs
Glucocorticoids - Uses
Synthetic Steroidal Preparation

▣ An ideal GC should have no


mineralocorticoid activity.

▣ Structural changes to the basic cortisol


molecule resulted in a number of
compounds with
□ Minimal mineralocorticoid activity
□ Greater potency
□ Longer duration of action
Important Agents

Injectable:
BetamethasoneDexamethasone
Prednisolone Methylprednisolone
Hydrocortisone Triamcinolone

Oral:
BetamethasoneFludricortisone
Prednisolone Prednisone
Methylprednisolone

Topical:
BetamethasoneClobetasol
Flucinolone Mometasone

Inhalation:
Beclomethasone Budesonide
PREDNISOLONE
INTRODUCTION

▣ Origin : Synthetic
▣ Generic Name: Prednisolone
▣ Brand Name: Millipred DP, orapred,
prelone, pediaPred.
▣ Class: Corticosteroid (glucocorticoid)
▣ Mechanism of Action: It works by
modifying the body's immune response to
various conditions and decreasing
inflammation.
▣ Available dosage form and doses:
Tablets USP, 1 mg, 2.5 mg, 5 mg, 10 mg, 20
mg, and 50 mg,
Oral Solution USP, 5 mg per 5 mL and
Intensol™ Oral Solution 5 mg per mL
DOSE:

▣ Adult Dose for Anti-inflammatory:

5 to 60 mg per day in divided doses 1 to 4


times/day.

▣ Adult Dose for Nephrotic Syndrome:

Initial Dose: 2 mg/kg/day QID/TID


Maintenance Dose: 1 to 1.5 mg/kg/dose
given every other day for 4 weeks.
INDICATIONS

PREDNISOLONE
Treating allergies CHEMICAL
Arthritis STRUCTURE

Breathing problems (e.g., asthma)


Certain blood disorders
Collagen diseases (e.g., lupus)
Eye diseases (e.g., keratitis)
Cancer (e.g., leukemia)
Endocrine problems (e.g., adrenocortical
insufficiency)
Intestinal problems (e.g., ulcerative colitis)
Swelling due to certain conditions
Skin conditions (e.g., psoriasis).
CONTRAINDICATIONS:

Patient allergic to any ingredient in


prednisolone
Patient having a systemic fungal infection,
a certain type of malaria, inflammation of
the optic nerve, or herpes infection of the
eye
Patient is scheduled to have a live or
attenuated live vaccination (e.g., smallpox)
Patient is taking mifepristone
PRECAUTIONS

Pregnancy
Medicine
Allergy
Previous heart disease, renal disease, liver
disease, diabetes, underactive thyroid,
adrenal gland problems, mental or mood
problems.
Any recent infection
Weak bones or muscle problems
Recent vaccination
Stomach problem, intestinal problem,
esophagitis.
DRUG DRUG INTERACTION

Some drugs may increase the risk of


prednisolone's side effects such as:

Clarithromycin
Cyclosporine
Estrogens (e.g., estradiol)
Oral contraceptives (e.g., birth control
pills)
Ketoconazole
DRUG DRUG INTERACTION

Some drugs may decrease prednisolone's


effectiveness such as:
Barbiturates (eg, phenobarbital)
Carbamazepine
Ephedrine
Hydantoins (e.g., phenytoin)
Rifampin
DRUG DRUG INTERACTION

The risk of side effects of some drugs may be


increased by prednisolone such as:

Anticholinesterases (e.g., pyridostigmine)


Aspirin
Diuretics (e.g., hydrochlorothiazide,
furosemide)
Methotrexate
Mifepristone
Quinolone antibiotics (e.g., ciprofloxacin)
Ritodrine
Live or attenuated live vaccines
DRUG DRUG INTERACTION

Effectiveness of some drugs may be


decreased by prednisolone such as:
Anticoagulants (e.g., warfarin)
Hydantoins (e.g., phenytoin)
Killed or inactivated vaccines
WARNING

Avoid contact with people who have colds


or infections.
If you are taking prednisolone regularly
over a long period of time, carry an ID card
at all times that says you take
prednisolone.
Do not receive a live vaccine (eg, measles,
mumps, smallpox) while you are taking
prednisolone.
Tell your doctor or dentist that you take
prednisolone before you receive any
medical or dental care, emergency care, or
surgery.
WARNING

Diabetes patients - Prednisolone may affect your


blood sugar. Check blood sugar levels closely. Ask
your doctor before you change the dose of your
diabetes medicine.
Lab tests, including adrenal function tests, may
be performed while you use prednisolone. These
tests may be used to monitor your condition or
check for side effects.
Caution is advised when using prednisolone in
CHILDREN; they may be more sensitive to its
effects.
Corticosteroids may affect growth rate in CHILDREN
and teenagers in some cases. They may need
regular growth checks while they take prednisolone.
COMMON SIDE EFFECTS

Acne Increased
Clumsiness appetite
Dizziness Increased
Facial flushing sweating
Feeling of a Nausea
whirling motion Nervousness
General body Sleeplessness
discomfort Upset stomach
Headache
SEVERE SIDE EFFECTS

Severe allergic reactions Increased hunger, thirst, or


(rash; hives; itching; urination; mental or mood
difficulty breathing changes (eg, depression)
Tightness in the chest Muscle pain, weakness, or
swelling of the mouth, face, wasting; seizures
lips, or tongue Severe nausea or vomiting
Black, tarry stools Shortness of breath
Changes in body fat Signs of infection (e.g., fever,
Changes in menstrual period chills, persistent sore throat)
Changes in skin color Sudden severe dizziness or
chest pain headache
easy bruising or bleeding Swelling of ankles, feet, or
Unusual weight gain hands
Vision changes or other eye Tendon or bone pain
problems Thinning of skin
Unusual skin sensation
Vomit that looks like coffee
grounds.
STORAGE

Store prednisolone at room temperature


20 and 25 degrees C.
Store in a tightly closed container.
Store away from heat, moisture, and light.
Keep prednisolone out of the reach of
children and away from pets.
CLINICAL CASE
STUDY
CASE I

▣ A 60-year-old woman with a 3-year history of


diabetes is seen for worsening dyspnea and
cough.

▣ She has had chronic obstructive pulmonary


disease (COPD) since age 55.

▣ She is started on albuterol and begun on a


course of prednisone at 40 mg/day for 3 days,
tapering over 2 weeks.

▣ On day 3, she calls to report that her blood


GLUCOSE LEVEL IS 350 MG/DL AT 4:00 P.M.
WHY..??

▣ This patient has had type 2 diabetes


adequately controlled with diet for the past
few years. Her blood glucose levels increased
markedly with the addition of prednisone. The
typical characteristics of hyperglycemia
induced by corticosteroids include minimal
effect on fasting blood glucose levels and an
exaggeration in postprandial blood
glucose elevations. Patients with pre-
existing diabetes can have profound increases
in blood glucose.
CASE II

▣ Thirty four-year-old female experienced joint


stiffness, skin nodules, weight loss, and fever. 

▣ Diagnosed with Rheumatoid arthritis and


prescribed prednisolone for reducing
Inflammation.

▣ In Follow-up, found improved arthritis but


central obesity, increased thirst and urination,
and Blood sugar level of 210 mg/dL.
CONTD:

▣ Diagnosed with Cushing’s disease and


diabetes due to Prednisolone.

▣ Stopped the steroids.

▣ A month later, into emergency


room because of a very low blood pressure
and cardiovascular collapse.

▣ ER physician diagnosed her with adrenal


insufficiency.
WHY…???

▣ Adrenal insufficiency secondary to her


steroids being abruptly discontinued

▣ This condition occurs when the adrenal glands


fail to produce steroid hormones such as
cortisol and aldosterone. These patients will
typically present with hypoglycemia,
dehydration, weight loss, disorientation,
weakness, fatigue, hypotension,
cardiovascular collapse, muscles, nausea,
vomiting, and diarrhea.
TREATMENT:

▣ Maintained on prednisone again to prevent


further adrenal damage.

▣ Tapper the dosages


Thanks
!
Any questions?

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