1. New Drugs in Palliative Care
Dr Chloe Webb
Palliative Care Registrar
Beaumont Hospital

2. Drugs Covered Targin Pecfent Effentora Palexia Oxynorm Dispersa
Relistor
Durogesic Dtrans
Buprenorphine
Transtec
Butrans

3. Targin

4. Targin Indication Opioid analgesic
Combines oxycodone with opioid antagonist naloxone
Naloxone is added to counteract opioid-induced constipation
- Blocks the action of oxycodone at opioid receptors locally in the gut.
Oral use
Twice daily dose

5. Targin Recommended starting dose in opioid naïve patients
- 10 mg/5 mg oxycodone/naloxone BD
Max daily dose of Targin - 80 mg/40mg.
If higher doses required – consider administration of supplemental oxycodone hydrochloride prolonged-release at the same time.
Beneficial effect of naloxone hydrochloride on bowel function may be impaired with additional oxycodone

6. PecFent Fentanyl Nasal Spray Indication
Management of breakthrough pain in adults already receiving maintenance opioid therapy for chronic cancer pain
60mg PO morphine daily,
25mcg/hr TD fentanyl,
30mg PO oxycodone daily,
8mg PO hydromorphone daily

7. PecFent Nasal mucosa is highly vascularised with a large surface area
Lipophilic drugs such as fentanyl are rapidly and extensively absorbed
Avoids first pass metabolism and issues with oral pathologies
e.g. nausea / vomiting or dry / ulcerated buccal membrane

8. PecFent Yellow pack – 100mcg/spray strength
Available in two strengths:
Yellow pack – 100mcg/spray strength
Violet pack – 400mcg/spray strength

9. Pecfent Starting dose of 100 mcg (one spray)
Titrated to an “effective dose”
At least 4 hours before further dose of PecFent can be used.
Review background opioid treatment if >4 episodes of breakthrough pain/24hrs

10. Patient Instructions Blow your nose if you feel you need to
Sit down with head upright
Put the nozzle a short distance (about 1 cm) into your nostril
Close the other nostril with a finger from your other hand
Spray (listen for the click)
Stay sitting for at least 1 minute after using the nasal spray
Do not blow your nose straight after using the PecFent nasal spray

11. Effentora

12. Effentora Buccal Fentanyl Indication
Treatment of breakthrough pain in patients with cancer already receiving maintenance opioid therapy for chronic cancer pain.
60mg PO morphine daily,
25mcg/hr TD fentanyl,
30mg PO oxycodone daily,
8mg PO hydromorphone daily

13. Effentora Individually titrated to an “effective”/maintenance dose
The effective dose of Effentora is not predictable from the daily maintenance dose of opioid.
At least 4 hours between doses
May require readjustment of maintenance dose

14. Effentora - Titration 100mcg initially
- If pain still present within 30mins
- Give 2nd same strength Effentora tablet.
Increase dose to the next strength to treat the next episode of pain.
Multiple tablets may be used to treat a single episode of pain
- up to four 100mcgs
- up to four 200mcgs
Doses >800mcgs were not evaluated in clinical studies.

15. Effentora – How to use it!
Blister pack (peel open)
Place tablet above an upper rear molar between cheek and the gum/sublingually
Dissolves/disintergrates in ~15-25mins
Shouldn’t be sucked or chewed
If any tablet remains after 30mins – swallow with a glass of water

16. Palexia

17. Palexia Tapentadol Indication
Relief of moderate to severe acute & chronic pain in adults
µ-opioid receptor agonist & noradrenaline reuptake-inhibition
Nociceptive, neuropathic, visceral and inflammatory pain
Mainly evidence supports use in nociceptive pain conditions including postoperative orthopaedic & abdominal pain, also chronic pain due to osteoarthritis (hip/knee).

18. Palexia SR Starting dose - 50mg tapentadol BD (12hrs apart).
Increase in increments of 50 mg tapentadol SR twice daily every 3 days
Titrate dose to provide adequate analgesia with minimal undesirable effects
Antiemetic prophylaxis is not usually required
Laxative porphylaxis is not usually required

19. Palexia Non-Opioid Dose Independent Tramadol PO (mg/d) < 400mg
Oxycodone PO (mg/d)
< 40mg
40 – 60mg
60 – 80mg
Morphine PO (mg/d)
< 80mg
80 – 120mg
120 – 160mg
Hydromorphone PO (mg/d)
< 12mg
12 – 16mg
16 – 20mg
Fentanyl TD (µg/h)
< 37.5µg
37.5 – 50µg
50 – 75µg
Buprenorphine TD (µg/h)
< 35µg
35 – 52.5µg
52.5 – 70µg
Palexia SR
50mg BD
100mg BD
150mg BD

20. Oxynorm Dispersa Orodispersible oxycodone Indication
Treatment of severe pain/breakthrough pain
Oral use
Taken every 4-6hours as needed
Dissolves on tongue

21. Relistor Methylnaltrexone bromide Subcutaneous injection Indication
Treatment of opioid-induced constipation in palliative care patients when response to usual laxative therapy has not been sufficient
Given on top of usual laxatives

22. Relistor Dose Recommended dose
- 8 mg (0.4 ml) for patients weighing kg
- 12 mg (0.6 ml) for patients weighing kg
- Patients whose weight falls outside these ranges should be dosed at 0.15 mg/kg.
Induces prompt bowel motion
Single dose alternate days.
Doses may also be given with longer intervals, as per clinical need.
Rotate injection sites (upper arms & legs, abdomen)

23. Relistor
Use with caution in patients with known or suspected GI lesions.
- Increased risk of GI perforation
Advise patients to discontinue and consult their doctor if they develop severe, persistent, and/or worsening abdominal symptoms (GI perforation).
Note concomitant medications [e.g. bevacizumab (AVASTIN), NSAIDs and steroids]

24. Durogesic

25. Durogesic Transdermal fentanyl patch Indication
Management of chronic intractable pain in patients requiring opioid analgesia
Reapplied every 72hours
Initial dose - based on the patient's current opioid use.
Recommended that Durogesic DTrans be used in opioid tolerant patients

26. Durogesic DTrans Opioid-tolerant patients
Use Equianalgesic potency conversion chart to convert from PO/parenteral opioids to Durogesic Dtrans.
Dose may be titrated up or down
- increments of 12/25 µg/h
- achieve the lowest appropriate dose of Durogesic
Dtrans
- depends on response and supplementary analgesic
requirements.

27. Oral 24hr Morphine (mg/day)
Durogesic Dtrans Dose (µg/h)
4 hourly PO morphine (mg) breakthrough
< 44 12
< 7.5
45-89 25
10-15
90-134 37
15-20 50
25-30 62 35 75
40-50
100
55-65
125
70-80
150
85-95
175
200
225
250
275
300

28. Durogesic DTrans Opioid-naïve patients
The normal initial Durogesic DTrans dosage should not exceed 25 µg/h.
Recommended that patients be titrated with low doses of immediate-release opioids (e.g., morphine, oxycodone) to attain equianalgesic dose relative to Durogesic 12/25 µg/h
TD fentanyl is licensed for use as a 1st line strong opioid
severe dysphagia,
renal failure
high risk of diversion and tablet misuse.

29. Durogesic – Patient Instruction
Apply to upper arm or chest area
Don’t apply patch in same place twice in a row
Clean and dry skin
Takes 18-24hr to become therapeutic intially
Open the pouch – tear off edge of pouch
Mind not to tear patch
Peel off backing – try not to touch sticky side
Press onto skin firmly (hold for 30secs)
Wash your hands

30. Butrans & Transtec Transdermal Buprenorphine Indication
Pain of moderate to severe intensity
Alternative to both weak opioids and morphine
Not suitable for the treatment of acute pain
Take into account previous opioid history
Opioid naive pts – prescribe lowest strength (5mcg/h)

31. Buprenorphine Butrans Transtec 7 day patch Doses available
5, 10 and 20mcg/h
Onset of action
18–24h
Peak plasma concentration
3 days
4 day patch
Doses available
35, 52.5, 70mcg/h
Onset of action
21h for 35mcg/h patch;
11h for 70mcg/h patch
Peak plasma concentration
60 hrs

32. Butrans vs Morphine Buprenorphine Morphine 5µg/hr 10mg/24hrs 10µg/hr

33. References
Palliative Care Formulary 3 - Robert Twycross and Andrew Wilcock
Archimedes Pharma
Cephalon
JanssenCilag
Grunenthal
Mundipharma
Wyeth