Analgesia:%20New%20Drugs%20Transdermal%20

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Analgesia New DrugsTransdermal Buccal

• Dr Pauline Kane
• Registrar in Palliative Medicine
• Beaumont Hospital
• 17th Sept 2009

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Overview

• Transdermal opioid patches
• Used for stable chronic pain
• Frequently cancer pain is not stable pain
• Transmucosal opioids
• Short acting opioids
• Breakthrough cancer pain
• New drugs

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Indications for Transdermal Opioid Patch

• Indication Chronic pain
• Cannot take oral medications
• Nausea, Vomiting
• Mucositis
• Mouth ulcers
• Dysphagia
• Difficulty taking tablets
• Poor compliance
• Cognitive impairment
• Elderly

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Transdermal route

• Avoidance of hepatic first pass metabolism
• Continuous pain relief
• Improves patient compliance with treatment
• Constant drug delivery providing a more stable
  plasma concentration without peaks
• Ease of administration despite nausea, vomiting
  and difficulties swallowing
• Absorption independent of food or fluid intake

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Transdermal Patches

• Fentanyl patch
• Durogesic
• Matrifen
• Replace patch every 72 hours

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Why fentanyl?

• Fentanyl citrate
• Absorbed easily through skin
• Low risk for skin irritation
• 100 times more potent than morphine
• Less constipating
• Less nausea and vomiting

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Using Fentanyl Patch

• Apply patch to dry, flat, non-hairy skin on torso
  or upper arm
• Press firmly in place with the hand for 30
  seconds to ensure good contact
• Replace patch every 72 hours
• Rotate patch sites
• Avoid same site for several days
• Wait 24 hours before evaluating pain relief

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Fentanyl transdermal patch
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Matrix Patch
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Fentanyl Patch
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Fentanyl transdermal patch

• Equivalence chart Lasts 72 hours

Fentanyl transdermal patch Morphine oral equivalent in 24 hours
12mcg/hr 45mg oral morphine in 24 hours
25mcg/hr 90mg oral morphine in 24 hours
50mcg/hr 180mg oral morphine in 24 hours
75mcg/hr 270mg oral morphine in 24 hours
100mcg/hr 360mg oral morphine in 24 hours
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Other users of fentanyl patches
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Buprenorphine Transdermal Patch

• Butrans lower strength opioid patch
• Replace patch every 7 days
• Transtec higher strength opioid patch
• Replace patch every 3 days

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Butrans Transdermal Patch

• Indication
• Moderate pain unresponsive to non-opioid
  analgesics
• Apply to dry, non-hairy skin on torso or upper
  arm
• Replace patch every 7 days
• Rotate patch site
• Avoid using same area for 3 weeks
• Level of pain relief should not be assessed until
  patch is on for 3 days

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Buprenorphine transdermal patchEquivalence
chart Lasts 7 days
Buprenorphine transdermal patch Butrans Morphine oral equivalent in 24 hours
5mcg/hr 7mg oral morphine in 24 hours
10mcg/hr 14mg oral morphine in 24 hours
15mcg/hr 21mg oral morphine in 24 hours
20mcg/hr 28mg oral morphine in 24 hours
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Transtec transdermal patch

• Indication
• Moderate to severe pain
• Severe pain unresponsive to non-opioid analgesics
• Apply patch every 3 days
• Rotate patches
• Avoid same area for at least 6 days
• Only evaluate pain relief after patch is on for
  at least 24 hours

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Buprenorphine transdermal patchEquivalence
chartLasts 72 hours/3 days
Buprenorphine transdermal patch Transtec Morphine oral equivalent in 24 hours
35mcg/hr 30-60mg oral morphine in 24 hours
52.5mcg/hr 60-90mg oral morphine in 24 hours
70mcg/hr 90-120mg oral morphine in 24 hours
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Buprenorphine transdermal patch

• Rates of absorption increase if skin is warm and
  dilated
• Safe to use in patients with renal impairment
• Not removed in haemodialysis
• Smaller starting doses are advised in hepatic
  impairment highly protein bound drug
• More persistent erythema than with fentanyl
  patches
• Can cause pruritus

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Transdermal Opioid Patches

• Important to remember that the patches contain a
  significant dose of morphine
• In patients who are opioid naïve
• Commence at lowest dose
• Remember buprenorphine 5mcg/hr patch morphine
  7mg/24 hours orally
• Remember fentanyl 12mcg/hr patch morphine
  40mg/24 hours orally
• Important to check daily that patch is still in
  place

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Cautionary Use of Opioid Transdermal Patches

• COPD or other medical conditions predisposing to
  respiratory depression eg. Myasthenia gravis
• Elderly
• Cachetic
• Debilitated
• Susceptibility to hypercapnia CO2 retention
• Raised intracranial pressure
• Impaired consciousness
• Coma
• Brain tumour
• Caution in bradyarrhythmias

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Precautions

• Lack of appreciation that fentanyl is a strong
  opioid analgesic
• Inappropriate use for short-term, intermittent or
  post-operative pain in opioid naive patients
• Lack of patient education re safe use, storage
  disposal
• Lack of awareness of signs of overdose
• Lack of awareness of increased absorption of
  opioid if skin under patch becomes vasodilated
  eg. Febrile patients, or by an external heat
  source eg. Electric blankets, sauna

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Breakthrough Cancer Pain

• Incident pain predictable
• Voluntary onset with activity such as walking
• Involuntary onset with activity such as
  coughing
• Procedural onset related to intervention such
  as
• wound dressing
• Spontaneous pain - unpredictable

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Breakthrough Cancer Pain

• Rapid onset
• Short duration
• 1 min to 2-3 hours

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Fentanyl for breakthrough pain

• Indication Patient has been on long acting
  opioid medication of the following strength for
  chronic cancer pain for at least a week
• Oral morphine 60mg/day
• Transdermal fentanyl 25mcg/hr
• Oxycodone 30mg/day
• Oral hydromorphone 6mg/day
• An equianalgesic dose of another opioid
• Can commence on short acting opioid for
  breakthrough pain

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Buccal Fentanyl Actiq

• First transmucosal fentanyl preparation
• Lozenge on a stick
• Fentanyl in hard sweet matrix
• Lozenge placed inside cheek and moved constantly
  up and down, and changed at intervals to other
  cheek
• Aim to consume lozenge in 15 mins

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Transmucosal routes

• Buccal
• Effentora
• Place tablet in upper portion of buccal cavity
  above upper rear molar between cheek and gum
• Less permeable
• 75 is actually swallowed, reducing
  bioavailability
• Prolonged contact with mucosa and lozenge
  problematic if inflamed mucosa

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Transmucosal routes

• Sublingual
• Abstral
• Place tablet under tongue
• Rapid absorption
• Highly vascularised under the tongue
• Highly permeable
• High bioavailability

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TransmucosalNasal route

• Nose has surface area of 150-180cm2
• Continuous mucus in nose limits drug uptake to
  about 15mins
• Rhinitis does not affect it
• Convenient to use in those with nausea, vomiting,
  dry mouth syndrome or mucositis
• Nasalfent
• Not reimbursed on GMS

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Directions for Use

• Wait 4 hours between doses
• No food/drink while tablet in mouth
• Tablet disintegration takes 15-30 mins

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Buccal and Sublingual Medication

• Do not suck/chew/swallow as this decreases plasma
  concentration
• Xerostomia drink water prior to tablet
  placement
• Mouth ulcers
• Mucositis

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Transmucosal fentanyl citrate

• 25 of dose is absorbed rapidly into systemic
  circulation
• Pain relief in 5-10 mins
• Remainder is swallowed or absorbed more slowly
• This is subject to hepatic first pass metabolism
• Only 1/3 of this amount is available
  systemically, 25 of the total dose

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Fentanyl for Breakthrough Pain

• Use with caution
• Highly addictive
• Irish Medicines Board have 6 recorded cases of
  addiction to Actiq
• Only use for breakthrough pain caused by cancer

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Conclusion

• Transdermal patches
• Indication
• Chronic pain poorly controlled on non-opioid
  analgesics
• Start on lowest dose in opioid naïve patients
• Transmucosal route
• Indication
• Only used for breakthrough pain secondary to
  cancer
• Highly addictive

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