Analgesics

Opioids

Endorphins and enkephalins

Act on specific receptor sites in the CNS that are concerned with pain perception

Function as endogenous analgesics

 

Introduction

Narcotics – a drug which will induce sleep as well as relieve pain

May induce dependence if given in the absence of pain

Do not induce dependence if given in pain

Discovered in the opium poppy

Opium contains morphine, codeine, papaverine and many other alkaloids

 

Morphine

Has an affinity for a number of opioid receptors

mu receptor   -  analgesia                delta receptor -  respiratory depression

kappa             -  sedation                  sigma                           -  hallucinations

Naloxone is an opioid antagonist and may reverse the effects of morphine

 

Other effects

May reduce coughing and thicken bronchial secretions

Produces mental detachment and euphoria which helps to reduce anxiety so may enhance analgesia

May act on the medulla, triggering chemoreceptors to cause nausea and vomiting

May cause constipation by reducing GI motility

High doses usually causes pinpoint pupils

Tolerance develops

 

Administration

10 – 20 mg                                        Fast or slow routs of administration

 

Diamorphine

Heroin                         5 – 10 mg dose         More potent and soluble than morphine

 

Other opioids

Fentanyl (sublimase)   Dextromoramide (palfium)   Dihydrocodeine  (DF 118)

Pethidine  Codeine

 

Non-opioid  analgesics

 

Paracetamol

Does not harm gastric mucosa       Is not anti-inflammatory                     0.5 – 1 g  4 – 6 hourly

 

Adverse effects

May cause hepatonecrotic damage in acute overdose

Antidotes are effective if within 10 – 12 hours of ingestion

Chronic use of several mild analgesics may cause renal damage

Compound analgesics are probably useless so combine paracetamol or aspirin with a full dose of the opioid component

 

NSAIDs

 

Prostaglandins

Damages cell membranes release fatty acids

These are converted to prostaglandins by the enzyme cyclo-oxygenase

Prostaglandins are inflammatory mediators

NSAIDs inhibit the action of cyclo-oxygenase

 
Side effects

Contra-indicated in peptic ulceration          Gastric irritation and bleeding

Nausea and vomiting                                    Worsening of asthma

Hypersensitivity                                             Do not give if patient is sensitive to aspirin

May be highly protein bound so interact with anticoagulants

Different patients respond differently to the various NSAID preparations, the occurrence of side effects is one of the main choice criteria

 
Indications

Pain associated with inflammation

Single dose analgesic effect is similar to paracetamol

Full anti-inflammatory effects may take up to 3 weeks to develop

NASIDs are palliative – they do not effect the underlying disease process

Examples - Ibuprofen, naproxen, diclofenac, indometacin, nabumetone

 

Aspirin

Acetylsalicylic acid                Discovered in Willow bark               Inhibits synthesis of prostaglandins

300 – 600 mg 4 hourly          Inhibits cyclo-oxygenase

 

Side effects

Gastric irritation and bleeding         Give soluble preparations with food

Asthma                                               Hypersensitivity

 
Overdose

Hyperventilation, dizziness, confusion, tinnitus, deafness, hypothrombinaemia, respiratory and cardiovascular complications from acid base disturbance

Haemodialysis may be needed

 
Reye`s syndrome

May occur in children

Acute encephalopathy and fatty degeneration of the liver

Never give aspirin to the under 12s

 
Other effects

Antiplatlet                   Anti-inflammatory                  Antipyretic

 

Gate theory

Regulation of impulses through the substantia gelatinosa from peripheral fibres to the spinal transmitter cells which carries the impulse up to the brain.

 

Substance p may be one of the transmitters involved at this level

 

Endorphin receptors are also involved

 

Inhibition may be ascending or descending

Pain may be blocked at this level