ANALGESICS AND STEROIDS

E.Jonas
08/01/2025 1
 Learning Tasks

At the end of this session a learner is expected to be able to:

• Define of analgesics
• List commonly used analgesics
• Describe the indication ,mechanism of action and side effects
of non-opioid analgesics (non-steroidal anti-inflammatory
drugs)
• Describe the indication ,mechanism of action and side effects
of opioid analgesics
• List commonly used steroids
• Describe the indications, mechanism of action and side effects
of steroids
08/01/2025 2
Analgesics
Are drugs that relieve pain due to multiple
causes.
 Analgesic drugs act in various ways on the
peripheral and central nervous systems

E.Jonas
08/01/2025 3
 Commonly Used Analgesics

Narcotic (opioids) which act in the central

nervous system and cause drowsiness,i.e
 Pethidine
 Morphine
 Fentanyl
 Codaine

E.Jonas
08/01/2025 4
Non-narcotic non opioids which act chiefly
peripherally
– The commonly used non opioid antipyretics
agents are the Non-steroidal Anti-
inflammatory Drugs/medicines (NSAID)
which have both antipyretic and anti-
inflammatory effect including:
 Aspirin(acetylsalicylic acid, ASA)
 Paracetamol (Acetaminophen)
E.Jonas
08/01/2025 5
  Indomethacin
 Diclofenac
 Ibuprofen

E.Jonas
08/01/2025 6
Indications, Mechanism of Action and Side Effects of Non
Opioid analgesics [Non-steroidal Anti-Inflammatory
Drugs (NSAIDs)

Mechanism of actions of NSAIDs

• The mechanism of action of traditional NSAIDs
involves blockade of the production of
prostaglandins
• This is by inhibition of the enzyme
cyclooxygenase (COX) at the site of injury in
the periphery, thus decreasing the formation of
mediators of pain in the peripheral nervous
system
E.Jonas
08/01/2025 7
 Pharmacological effects of NSAIDs

• Has analgesia effects

– They reduce certain types of pain.
• Has anti-inflammatory effects:
– The drugs modify the inflammatory reactions.
• Antipyretic effect
– The drugs can lower raised body temperature
• All these effects are related to their ability to
inhibit the action of cyclooxygenase on
arachidonic acid.
E.Jonas
08/01/2025 8
 Indications, mechanism of action and
side effects of specific NSAIDS
Aspirin (Acetylsalicylic Acid)
• It is indicated for mild to moderate pain, pyrexia,
rheumatoid arthritis and is also used to reduce
the risk of myocardial infarction and deep
venous thrombosis
• To be given with cautions for a patient with
– Asthma; as it may induce bronchospasm
– Allergic disease
– Hepatic impairment or renal impairment
E.Jonas
08/01/2025 9
• Contra-indications
– It is not advised to give aspirin-containing preparations to
children under 16 years and breast-feeding mothers unless
specifically indicated (as it may precipitate to Reye's
syndrome)
– Asthma
– Peptic ulceration or gastritis and bleeding disorders like
haemophilia
• Interaction
– NSAIDs cause salt retention and therefore reduce potency of
diuretics
E.Jonas
08/01/2025 10
• Dose
– By mouth: 300–900 mg every 6 hours, when
necessary
– Maximum dose is 4g daily

E.Jonas
08/01/2025 11
• Side effects
 Acute renal insufficiency in susceptible patients but
reversible on stopping the drug.
 Chronic use of NSAIDs can cause “ analgesic
nephropathy”:- chronic nephritis and renal papillary
necrosis
 Salicylism:
• Occurs after repeated ingestion of large doses:- tinnitus,
vertigo , decreased hearing, nausea and vomiting
• Reyes’ syndrome – occurs in children
E.Jonas
08/01/2025 12
  Large doses alter the acid-base balance and the
electrolyte balance
 Hyperpyrexia due to increased metabolic rate
 It is a combination of liver disorder and encephalopathy
that can follow an acute viral illness (mortality 20-40%).
 Generally mild and infrequent but high incidence of
gastro-intestinal irritation with slight asymptomatic
blood loss
 Increased bleeding time, bronchospasm and skin
reactions in hypersensitive patients
E.Jonas
08/01/2025 13
 Paracetamol (Acetaminophen)

 Is one of the most commonly used non-narcotic analgesic-

antipyretic agents
 It has relatively weak anti-inflammatory activity
 Dose
 (500mg)by mouth: 0.5–1 g every 6 hours to a maximum 4g daily
 Children 2 months 60 mg for post immunization pyrexia,
repeated once after 6 hours if necessary
 Side effects
– Allergic skin reactions sometimes occur
– Regular intake of large doses over long periods may increase the
risk of kidney damage
E.Jonas
08/01/2025 14
 Ibuprofen

 It has propionic derivates and is a therapeutically

significant anti-inflammatory
 The drug is used also in rheumatoid arthritis (including
juvenile arthritis) and post operative analgesia
 Dosage:
 400mg after every 8 hours and should be taken with food to
avoid gastric irritation
 Side effects
– Acute renal insufficiency in susceptible patients but
reversible on stopping the drug
E.Jonas
08/01/2025 15
 Indomethacin

 Indicated in moderate pain and rheumatoid

disease and dysmenorrhea
 Not recommended in children
 Dosage:
 50mg every 8 hours with food
 Side effects
– Skin rashes
– Kidney problems
– Stomach or intestinal bleeding
E.Jonas
08/01/2025 16
 Diclofenac

• Used in the relief of pain and suppression of

inflammation in rheumatic disease, other
musculoskeletal disorders, acute gout, and
post- operative pain
• Dosage:
– 50mg every 8 hours after meals.
– Formulations for deep intramuscular injections
into the gluteal muscles are also available.
E.Jonas
08/01/2025 17
 Indications, Mode of Action and Side
Effects of Opioid Analgesics (Narcotics
Mechanism of action of opioid
• The central nervous system contain a series of receptors
that controls pain known as opiates receptors
• The opioids work by mimicking the endogenous
(meaning produced by the human body) endorphins by
stimulating opioid receptors in the central and peripheral
nervous systems which results in relief of pain
• The opioid receptors are subdivided into four types,mu
(µ), delta (δ),kappa (κ) and epsilon (ε)

E.Jonas
08/01/2025 18
 Morphine

 It controls somatic pain following trauma or surgery.

 Morphine is given through I/V, followed by an anti-
emetic to alleviate severe visceral pain.
 Morphine is also extremely valuable in the treatment of
shock for relieving pain if present and for calming the
patient
Dose:
 Given at a dose of 10-20mg by mouth or by
subcutaneous, I/M or I/V injection, if necessary the dose
is repeated after 4 hours
E.Jonas
08/01/2025 19
 Morphine is the opioid of choice for the oral treatment of severe pain
in palliative care
 Side effects
–
Decreased respiratory effort and low blood pressure
– Nausea and vomiting
– Constipation
– Morphine is addictive and prone to abuse
–
If the dose is reduced after long-term use, opioid withdrawal symptoms may
occur including
• Agitation
• Anxiety
• Muscle pains
• Increased tearing
• Trouble sleeping
E.Jonas
08/01/2025 20
 Pethidine

 Is a synthetic narcotic analgesic

 Commonly used for postoperative pain relief.
 Given at a dose of 50-100mg I/M or by slow I/V
injection; if necessary the dose is repeated after every
4-6 hours in severe pain (A dose of 150mg may be
required).
 It is also particularly useful in the reduction of
severity of labour pain without reducing the force of
contraction of the uterus.
E.Jonas
08/01/2025 21
 Dependence is likely to occur if taken
without caution.
Side effects
– Respiratory depression
– Hypotension
• Pethidine cause more severe hypotension than
morphine
– Nausea
E.Jonas
08/01/2025 22
 List of Commonly Used Steroids with
Anti-inflammatory effects
 These are mostly referred as corticosteroids
 Corticosteroids are man-made drugs that closely resemble
cortisol, a hormone that your adrenal glands produce
naturally
 Corticosteroids are divided into two groups
– Glucocorticoid( Which are anti-inflammatory and ant-
allergy)
• Hydrocortisone
• Prednisolone
– Mineralcorticoids
• Which are for maintaining fluids and electrolyte like aldosterone
E.Jonas
08/01/2025 23
 Corticosteroids

Mechanism of action of glucocorticoids

• Glucocorticoids affect cells by binding to
the glucocorticoid receptor.
• The activated glucocorticoid receptor-glucocorticoid
complex up-regulates the expression of anti-inflammatory
proteins in the nucleus (a process known as transactivation)
• And represses the expression of proinflammatory proteins
in the cytosol by preventing the translocation of other t
ranscription factors from the cytosol into the nucleus (
transrepression)

E.Jonas
08/01/2025 24
Hydrocortisone
 These reduce the inflammatory component in
chronic asthma and are life-saving in status
asthmaticus (acute severe asthma)
 They do not prevent the immediate response to
allergen or other challenges
 The mechanism of action involves decreased
formation of mediators like cytokines and other
inflammatory cells
E.Jonas
08/01/2025 25
 They are given by inhalation (e.g.
beclometasone), or intravenous hydrocortisone
Side effects
 sleep problems (insomnia), mood changes
 acne, dry skin, thinning skin, bruising or discoloration
 slow wound healing
 increased sweating
 headache, dizziness, spinning sensation
 nausea, stomach pain, bloating
E.Jonas
08/01/2025 26
Prednisolone
 Indicated for suppression of inflammatory and
allergic disorders
 Dose:
– 10-20mg orally daily up to 60mg daily. Acute
asthma, 30-40mg daily for few days gradually
reduced when asthma has been reduced
 Precaution, avoid rapid withdraw
 Common side effects includes
E.Jonas
08/01/2025 27
 – Acne.
– Dry or thinning skin.
– Bruising or discoloration of the skin.
– Mild nausea or stomach pain.
– Bloating.
– Sleep problems.
– Mild mood changes.
– Increased sweating
E.Jonas
08/01/2025 28
 Key Points
 Analgesics are drugs that relieve pain due to
multiple causes
 Analgesic drugs act in various ways on the
peripheral and central nervous systems
 Analgesics are of two types narcotics
(opioids) and Non narcotics(Non opioids )
 Steroids that are responsible for anti-
inflammatory effects are the glucocorticoids
E.Jonas
08/01/2025 29
 Evaluation
 What is the most common used
glucocorticoids?
 What is the mode of action of NSAIDs?

E.Jonas
08/01/2025 30