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Applied Pharmacy Practice > Minor Ailments - OTC analgesics (Pain killers) > Flashcards

Minor Ailments - OTC analgesics (Pain killers) Flashcards

1
Q

What is pain?

A
  • An unpleasant sensory and emotional experience associated with, or resembling that associated with, actual or potential tissue damage
  • A personal experince nfluenced by biological, psychological, & social factors
  • A person’s report of an experince as pain should be respected
    *
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2
Q

Nociception & pain

A
  • Pain & nociception are different - Pain cannot be
    inferred solely from activity in sensory neurons
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2
Q

What is Nociception?

A
  • When a noxious stimuli (e.g., tissue injury or temperature
    extremes) activate nociceptors (pain receptors, sensory neurons with specialised nerve endings widely distributed in skin, tissues, muscles, joints, visceral organs) & their pathways
  • Nociception is like the body’s alarm system, detecting potential harm
  • Pain is the feeling we experience in response to that alarm.
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2
Q

Classification of Pain BY TYPE

A
  1. Nociceptive – arising from pain receptors (e.g., twisted ankle)
  2. Neuropathic (nerve pain/neuralgia) – arising from nervous system (e.g.,trigeminal neuralgia, shingles)
  3. Pain with no apparent cause
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2
Q

Pain is…

A
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3
Q

Classification of Pain BY DURATION

A
  1. Acute (short-term) – hours to days, expectation that pain is time limited (e.g., twisted ankle, tooth extraction, post operative pain)
  2. Persistent or Chronic (long-term) – months to years (e.g., arthritis)
  3. Recurrent or Intermittent – comes and goes (e.g., back pain)
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4
Q

Classification of Pain BY CONDITIONS

A
  • headache
  • arthritis
  • musculoskeletal injury
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5
Q

What is Nociceptive Pain?

A
  • Arising from activation of pain receptors (nociceptors)
  • 2 types Somatic & Visceral
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6
Q

Somatic nociceptive pain

A
  • In the skin & musculoskeletal
  • Injury to skin, muscles, bone, joint and connective tissue
  • Pain may be described as dull or aching if in deep tissue, or sharp & pricking if under the skin
    *
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7
Q

Visceral nociceptive pain

A
  • Injury to internal organs (e.g., intestine or gall bladder)
  • Pain tends to be poorly localised & may be cramping
  • More dispersed
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8
Q

What is Neuropathic Pain?

A
  • Arising from damage or disturbance of function of a nerve
  • often described as unfamiliar pain, which may be burning or like electricity
  • may be associated with sensitivity of the skin
  • Can’t be managed using OTC meds
  • Needs to be referred
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9
Q

Neuropathic Pain may be associated with

A

Trauma:
may follow nerve damage or compression
* usually, the injury that starts the pain involves the peripheral nerves or the central nervous system
* changes in nervous system that sustain pain even after an injury heals
* Trauma heals but pain may still continue
**Diff types of disease or conditions **:
* Neuropathic pain syndromes
* Diabetes (diabetic neuropathy)
* Shingles (postherpetic neuralgia)
* Trigeminal neuralgia
* Post-stroke pain
* Complex regional pain syndromes = reflex sympathetic dystrophy (RSD) = causalgia)

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10
Q

Pharmacological Management (OTC analgesics)

A

Non-opioid:
* Paracetamol
* NSAIDS = Aspirin , ibuprofen , Diclofenac, naproxen
Opiod
* Codeine
* Dihydrocodeine
Compound analgesics:
* Non-opioid & opioid (e.g., co-codamol, co-
dydramol)
* Non-opioid & Non-opioid (e.g., ibuprofen/paracetamol 200/500)
Topical preparations
* NSAIDs
* Rubefacients ( increase blood flow to the area)
* Anti-inflammatories for local mouth pain (e.g., benzydamine)

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10
Q

Paracetamol containing products

A
  • Solpadine Plus = codeine + caffeine + paracetamol
  • Solpadeine Max = paracetamol + codeine 8 mg per tab
  • Solpadeine Max Soluble = paracetamol + codeine + caffeine
  • Solpadeine headache = caffeine + paracetamol
  • Syndol = sedative antihistamine + codeine, caffeine + paracetamol
  • Feminax period pain = codeine + paracetamol
  • Paramol = dihydrocodeine + paracetamol
  • Migraleve pink = paracetamol + sedative antihistamine + codeine
  • Migraleve yellow = codeine + paracetamol
  • Panadol night pain = paracetamol + sedative antihistamine
  • Panadol ultra = codeine + paracetamol
  • Nurmol = Ibuprofen + paracetamol
  • Caffine = stimulant = 100mg + caffine + standard dose of common analgesic gives a small but significant improvement to analgesic effect
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10
Q

WHO three-step analgesic ladder for pain management

A
  • Developed for cancer pain
  • Adjuvants = antidepressants, anticonvulsants, antispasmodics, muscle relaxant, bisphosphonate or corticosteroid)
  • Used OTC
    1. STEP 1= Mild pain = non-opiod (e.g.,paracetamol, NSAID)(± adjuvant)
    Step up if persisits or increases
    2. STEP 2 = Moderate pain = Weak opioid
    (e.g., codeine) ± non-opioid (± adjuvant)
    Step up if persisits or increases
    3. STEP 3= Moderate to severe pain = Strong opioid (e.g., morphine) ± non-opioid (± adjuvant)
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11
Q

What is Paracetamol?

A
  • Synthetic non-opioid = acts in CNS (CNS COX inhibitor)
  • Antipyretic analgesic=decrease fever+body temp
  • no peripheral COX inhibition
  • Dosen’t reduce inflammation
  • Increases prostaglandins production
  • Prostaglandins = lower threshold for pain
  • paracetamol stops this
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12
Q

Paracetamol

A
  • Mild to moderate pain
  • Drug of choice for fever & pain for people with bleeding disorders, peptic ulcers
  • Available OTC as an oral (GSL, P) or rectal suppository (P) formulation
  • Well absorbed orally:
  • Peak plasma concentrations in 30-60 minutes
  • Plasma half-life 2-4 hours
  • Side effects few, uncommon
  • oral adult does = 500 -1000mg every 4-6 hrs (max 4g in 24 hrs)
  • Oral paediatric dose by age (suspension)
13
Q

Paracetamol Hepatotoxicity (1)

A
  • Paracetamol is metabolised in the liver via glucuronidation & sulfation pathway.
  • 0ver 80% of paracetamol goes through these 2 pathways
  • A tiny amount goes through an enzyme= cytochrome P450 in the liver & produces a highly toxic metabolite (NAPQI)
  • Mopped up in cells by glutathione
  • Taking too much paracetamol saturates the 2 pathways so more paracetamol gets pushed through cytochrome p450 = More NAPQI
  • NAPQI causes cell death & necrosis
  • Potential for liver failure if untreated
  • Treatment IV acetylcysteine
14
Q

OTC Paracetamol Sales

A
  • law= pharmacies may not sell more than 100 non-effervescent tablets/capsules to a person at any one time
  • Most OTC pack sizes are 16 or 32 dose units
  • 96 = max number that can be sold
  • No legal limits on the quantity of OTC effervescent tablets, powders, granules or liquids
  • MHRA= no more than two packs should be supplied at any one time
15
Q

Paracetamol Hepatotoxicity (2)

A
  • Normal therapeutic doses can affect those w/ low glutathione stores = Old age, malnutrition, fasting/anorexia, or use of enzyme inducing drugs can cause more damage,chronic alcohol abuse or w/ glutathione synthesis deficiency.
  • Chronic use of alcohol or s/ meds = increase activity of CYP450 = increase NAPQI
  • US FDA = limits prescription combination products to 325 mg paracetamol
16
Q

Non-Steroidal Anti-Inflammatory Drugs (NSAIDs)

A
  • NSAIDs available OTC
    Aspirin:
  • 75mg = for blood thinning = GSL & P med
  • 300-900mg every 4-6 hrs= for pain
  • Oral 300 mg GSL (Pack size 16)
  • Oral 300 mg P (Pack size 32)
  • By law - no more than 100 non-effervescent tablets or capsules can be sold to a person at any one time
    Diclofenac:
  • Topical gel 2.32% P/GSL & 1.16% GSL
  • Medicated plaster 140 mg (up to 7 days ) = GSL
    ibuprofen:
  • Oral 200mg GSL (Pack size 16)
  • Oral 400mg P (Pack size 24, 48, 84)
  • Oral suspension 100 mg per 5 mL P & GSL
  • Topical gel 5% & 10% P & GSL
    Naproxen:
  • Oral 250 mg P (Pack size 9) for dysmenorrhoea
    (period pain & cramps)
  • Can only be sold OTC for period pain
17
Q

Types of NSAID’s

A
  • Irreversible COX inhibitor (aspirin)
  • Reversible COX inhibitors (e.g., ibuprofen, diclofenac, naproxen)
17
Q

NSAID’s

A
  • Used to decrease pain, inflammation & high temp
  • Antipyretic analgesic = decreases fever
  • Act on peripheral COX inhibition = anti-inflammatory activity
18
Q

NSAID’s side effects (1)

A
  • Inhibition of Peripheral COX causes side effects
    1. Gastrointestinal:
  • Prostaglandins affects how thick the lining of our stomach is
  • reduces cytoprotective gastrointestinal prostaglandins
  • increases risk of gastritis, peptic ulcers, bleeding
    2. Renal:
  • Reduces blood flow through the kidneys
  • reduce prostaglandins = dilate the renal artery= decrease renal lood flow activates Renin Angiotensin-Aldosterone System to retain sodium and water= increase bp
    3. Cardiovascular:
  • decrease prostaglandin = * Tip the clotting cascade towards clotting = increases risk of thrombotic event
  • Lowest with ibuprofen & naproxen so oral diclofenac is not sold OTC
18
Q

NSAID’s side effects (2)

A

Hypersensitivity:
* increased risk in people w/ asthma = s/ are intolerant
* trigger bronchospasm
Specific issues with aspirin (acetylsalicylic acid)
* Linked with Reye’s syndrome = rare condition causing liver and brain damage= Not for children & babies
* Aspirin overdose can be fatal (salicylism – tinnitus, vertigo, deafness, nausea, vomiting & eventually seizures or coma)

18
Q

OTC Opioids

A
  • Strongest pain med available OTC
  • Opioid analgesics bind opioid receptors (mu, kappa, delta) in the brain, spinal cord & GI tract
  • S/ are not pain meds = antitussive, supress coughing e.g codeine, dextromethorphan - no analgesic action
  • Antidiarrhoeal (loperamide, acts on Mu receptors in gut, doesn’t cross blood brain barrier so not an analgesic)= slows gut motility
19
Q

OTC Opioid analgesics

A
  • Codeine & dihydrocodeine available as compound oral formulations = P:
  • combined with paracetamol
    • codeine (co-codamol 8/500)
    • dihydrocodeine (co-dydramol)
  • used for = short-term treatment of acute
    moderate pain not relieved by paracetamol or aspirin or ibuprofen alone
  • Only for children 12+ years & adults
  • Pack sizes 32+ = POM ( includes effervescent tablets)
  • cna causse addiction = 3 day use ONLY
19
Q

CYP2D6 polymorphisms

A
  • Converts codeine into morphine
  • Side effects = respiratory depression ( hypoventillation = breathe too slowly) + Sedation ( drowsiness)
  • Poor metabolisers (5-10% of people) – unable to convert – little analgesic benefit but still get side effects
  • Intermediate metabolisers (2-11% of people) – little analgesic benefit but still get side effects
  • Extensive metabolisers (77-92% of people) – ~10% conversion to morphine = analgesic benefit
  • Ultra-rapid metabolisers (1-2% of people) – efficient conversion can lead to morphine toxicity. Life-threatening
    opioid toxicity reported in adults receiving low dose of codeine (75 mg per day) = why codeine isn’t given to children
20
Q

OTC Opioids: Codeine

A
  • Codeine = pro drug = has v/ minimal anagelsic activity on its own
  • Metabolised by cytochrome P450 into morphine = the active drug
  • If you have polymorphism in your cytochrome P450 you will not really fell the effects of codeine but you will get the side effects.
21
Q

OTC Opioids: Codeine & Dihydrocodeine side effects

A
  • Euphoria ( decrease anxiety) = Addictive
  • Sedation
  • Decrease Gut motility (constipation)
  • Respiratory depression
  • Nausea & vomiting
  • Confusion (especially in elderly)
22
Q

OTC Opioids: Dihydrocodeine

A
  • Dihydrocodeine (+ metabolites) has
    analgesic action
  • Elevate the pain threshold
  • Alter reaction to pain
23
Q

Why oral formulations?

A
  • Soluble, quicker acting & particularly if nausea present
  • Maximum dosing of paracetamol:
  • ± NSAID (with all cautions & warnings of side effects)
  • ± codeine (warn constipation & drowsiness)
  • ± antiemetic (for migraine with nausea/vomiting only)
  • Small dose of codeine may have only a small additional analgesic effect but
    cause additional side-effects (e.g., counsel re. constipation)
  • Caffeine containing preparations may have a small additional analgesic effect ( 100 mg)
23
Q

OTC Consultation Questioning about Pain

A
23
Q

OTC Management of Acute Pain

A
  • Explore symptoms
    Red flags for referral:
  • Bleeding
  • Seizure, dizziness, impaired consciousness, numbness
  • Visual disturbance
  • Fever (potential infection)
  • Gradual onset (chronic condition e.g. osteoarthritis)
  • Neck pain or stiffness with photophobia (meningitis)
  • Progressive or persistent headache
  • Sudden onset severe headache
  • Weight loss
  • 1st-line treatment depends on presenting complaint, intercations & preferences
23
Q

Common Presenting Complaints (2)

A

Lower back pain:
* 60-80% of people will experience at some stage & 20% of population will consult GP
* Staying active beneficial – exercise/movement
* NSAIDs are first-line at lowest dose compatible with any comorbidities. NICE guideline NG59 2016 (revised 2020)
**Activity-related soft tissue injuries/ sports injuries **:

or topical NSAID's as well
23
Q

Common Presenting Complaints ( 1)

A

Headache(usually self-limiting):
Primary
* Tension headache
* Migraine
* Cluster headache
Secondary (caused by
infection, neoplasm, trauma etc)
* Sinus pain (sinusitis)
* Temporal arteritis
Dysmenorrhoea = (menstrual/period pain)
* Cramps in muscular wall of womb → compression of blood vessels → reduced
oxygen → release of prostaglandins → pain
* Cramping, spreading to back & sometimes to thighs
* Ibuprofen or naproxen (only OTC indication is period pain)
Mouth Pain ( toothache)
* Systemic therapy - use max. paracetamol, be careful with NSAIDs as people tend to
reduce their diet and over-do analgesics for toothache
* Refer to dentist - Antibiotics may be required for infection
- Temporary relief possible from topical preparations (e.g. local anaesthetic gels & benzydamine – numbness & inflammation)

23
Q

Topical Formulations

A
  • Do not use the 2 together
    • NSAID (ibuprofen, diclofenac) creams & gels:
  • As effective as oral NSAIDs for musculoskeletal pain (Clinical trial data)
  • Some systemic absorption
  • caution with people with hypersensitivity
  • reduced risk of systemic side effects
  • Drug appears to concentrate in the affected tissues (where applied)
    Rubefacients (methyl salicylates, menthol, capsaicin):
  • Also known as counter-irritants
  • Cause vasodilation – sensation of warmth- mild skin irritation = distracts from pain
  • Rare adverse effects
  • not enough evidence to support use of methyl salicylate rubefacients for chronic or acute pain
24
Q

Tension headache

A

symptoms*
* Mild to moderate pain
* Tight band around head
* dull ache
* constant pressure
Causes
* Lack of sleep
* stress
* alcohol
* dehydration
treatment:
* Paracetamol
* aspirin
* ibuprofen

25
Q

cluster headache

A

sytmptoms:
* Severe unilateral pain above and within eye and temporal origin.
* multiple headaches one after the other.
causes:
* associations with lacrimation and rhinitis.
* lack of sleep
* dehydration
* alcohol.
treatments
* NSAIDS
* Paracetamol
* opioids

26
Q

migrane

A

symptoms:
* Unilateral pulsing or throbbing.
* Nausea
* vomiting
* light sensitivity
**causes **:
some triggers:
* Sleep disruption
* dehydration
* hormone fluctuations
**tratment **:
- NSAID’s
- paractetamol

27
Q

Medication overuse headache

A

symtoms:
* Dull, tension-type headaches.
causes:
* overuse of OTC pain relievers( more than 15 days in a month) i.e ibuprofen.

Applied Pharmacy Practice (19 decks)

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