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ANALGESICS

SAFETY CONSIDERATIONS AND


PATIENT FACTORS
TOPICS AT GLANCE
• Overview

• Paracetamol

• NSAIDs

• Patient factors to consider

• Drug interactions
OVERVIEW
• Pain is one of the most common reasons patients seek
medical care
• A study conducted in the Klang Valley showed that2:
– Analgesics were the most common non-prescription
medications used by the general public
– 78.5% of people obtained their medications from pharmacies

• Commonly used oral analgesics are:


– Non-prescription or over-the-counter (OTC) analgesics –
paracetamol and traditional, non-selective NSAIDs (eg, aspirin,
ibuprofen, naproxen)
– Prescription analgesics – cyclooxygenase-2 (COX-2) selective
NSAIDs, also known as COX-2 inhibitors (eg, celecoxib,
etoricoxib)
OVERVIEW
• A common misconception among many consumers is that self-
medicating with OTC analgesics is harmless

• However, there are several potential risks for the consumers:


– Increased risk of severe adverse effects
– Increased risk of drug interactions
– Potential for misuse (eg, incorrect choice, dose or manner of
administration) and abuse (eg, prolonged use, dependence)

• It is estimated that NSAID-related gastrointestinal (GI) bleeding,


myocardial infarction (MI) and stroke caused as many deaths as
road traffic accidents in the UK

• OTC paracetamol rarely causes significant health problems when


used as directed, but can result in serious liver damage in overdose
PARACETAMOL
• An effective analgesic/antipyretic, but does not have anti-inflammatory
activity

• Generally the preferred analgesic for elderly patients (when appropriate),


as they are at greater risk for adverse reactions related to NSAIDs

• Patients should be reminded not to exceed the recommended daily


dosage (maximum 4 g/day). Some recommendations state that self-
treating users should take a maximum dosage of 3 g/day

• At doses greater than 4 g/day, paracetamol is potentially hepatotoxic

• Concurrent use of paracetamol and alcohol can increase the risk of


hepatoxicity

• Paracetamol is contained in many prescriptions and formulations.


NSAIDs
• The risk of side effects of NSAIDs increases with the duration of use and
the dose. Hence, they should usually be used for the shortest period and
at the lowest effective dose.

• Side effects include GI bleeding and perforation, renal dysfunction, and


platelet dysfunction

• NSAIDs increase risk of bleeding and cardiovascular disease (CVD) from


the first day of use. These risks are a lot higher in older people. In
addition, NSAIDs increase the possibility of hypertension in the older
population by 40−70%

• Diclofenac is contraindicated in patients with ischaemic heart disease,


cerebrovascular disease, peripheral arterial disease and heart failure. COX-
2 inhibitors are also contraindicated in established CVD

• NSAIDs are contraindicated in patients with severe heart failure


NSAIDs
• NSAIDs should be used cautiously in patients with risk factors for GI events: a
history of GI bleeding, peptic ulcer, old age, smoking or alcohol use, and prolonged
NSAID use

• Patients at risk of GI ulceration who will benefit from NSAID treatment should
receive gastroprotective treatment such as proton pump inhibitors (PPIs)

• However, PPIs are associated with an increased risk of vitamin and mineral
deficiencies (vitamin B12, vitamin C, calcium, iron, magnesium). PPIs may increase
hip fractures by decreasing calcium absorption; hence they should be used with
caution, and after weighing the benefits against the risks. Antacids and H2-receptor
antagonists offer limited benefits against GI ulcers

• All NSAIDs including COX-2 inhibitors are contraindicated in those with active GI
ulceration or bleeding

• Non-selective NSAIDs and COX-2 inhibitors have the same analgesic efficacy, but
COX-2 inhibitors are associated with a lower risk of serious upper GI side effects
and better overall safety in terms of effects on platelet function
PATIENT FACTORS TO CONSIDER
• As with any medication, the choice of
analgesics should be based on the source,
type and severity of patient’s pain

• Consideration should also be given to


characteristics of the medication, as well as
patient’s age, co-morbid conditions, use of
other medications, and response to previous
treatment
PATIENT FACTORS TO CONSIDER
• Patients taking aspirin for heart protection should
consult their healthcare professionals before
using NSAIDs on a long-term basis. Regular NSAID
use inhibits aspirin’s ability to protect the heart

• Taking an NSAID and low-dose aspirin can also


increase the risk of GI side effects – use only if
really necessary and the patient needs to be
monitored closely
DRUGS INTERACTION
The table below summarizes the interactions between OTC analgesics and commonly used
prescription medications

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