ANALGESICS AND STEROIDS

• Total Session Time: 120 minutes

• Prerequisites: None
 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
 Definition of Analgesics

• Analgesics
• Are drugs that relieve pain due to multiple causes
– Analgesic drugs act in various ways on the peripheral and
central nervous systems
• Commonly Used Analgesics
• Narcotic (opioids) which act in the central nervous
system and cause drowsiness,i.e
– Pethidine
– Morphine
– Fentanyl
– Codaine
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)
• Indomethacin
• Diclofenac
• Ibuprofen
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
 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.
 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
 Cont…
• 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
• Dose
– By mouth: 300–900 mg every 6 hours, when necessary
– Maximum dose is 4g daily
 Cont…
• 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
 Cont…
• Reyes’ syndrome – occurs in children
– 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
 Cont…
• 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
 Cont..
• 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
 Cont…
• Side effects
– Acute renal insufficiency in susceptible patients but
reversible on stopping the drug
• Indomethacin
• Indicated in moderate pain and rheumatoid disease and
dysmenorrhea
• Not recommended in children
• Dosage:
– 50mg every 8 hours with food
 Cont…
• Side effects
– Skin rashes
– Kidney problems
– Stomach or intestinal bleeding
• 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.
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)
•
 Cont..
• 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 month or by subcutaneous, I/M or
I/V injection, if necessary the dose is repeated after 4 hours.
• Morphine is the opioid of choice for the oral treatment of
severe pain in palliative care
 Cont..
• 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
• 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.
• Dependence is likely to occur if taken without caution.
 Cont..
• Side effects
– Respiratory depression
– Hypotension
• Pethidine cause more severe hypotension than
morphine
– Nausea
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
 Indications, Mode of Action and Side Effects of
Steroids(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 transcription factors from the cytosol into the
nucleus (transrepression
 Cont..
• 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
• They are given by inhalation (e.g. beclometasone), or
intravenous hydrocortisone
 Cont..
• 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
 Cont..
• 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
• Acne.
• Dry or thinning skin.
• Bruising or discoloration of the skin.
• Mild nausea or stomach pain.
• Bloating.
• Sleep problems.
• Mild mood changes.
• Increased sweating
 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