Dr Chloe WebbPalliative Care Registrar

Beaumont Hospital

Drugs CoveredTarginPecfentEffentoraPalexiaOxynorm DispersaRelistor

Durogesic DtransBuprenorphine

TranstecButrans

Targin

Targin IndicationOpioid analgesicCombines oxycodone with opioid antagonist

naloxoneNaloxone is added to counteract opioid-

induced constipation- Blocks the action of oxycodone at opioid receptors locally in the gut.

Oral useTwice daily dose

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

PecFentFentanyl Nasal Spray

IndicationManagement 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

PecFentNasal 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 pathologiese.g. nausea / vomiting or dry / ulcerated buccal

membrane

PecFentAvailable in two

strengths:Yellow pack –

100mcg/spray strength

Violet pack – 400mcg/spray strength

PecfentStarting 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

Patient InstructionsBlow your nose if you

feel you need toSit down with head

uprightPut 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

Effentora

EffentoraBuccal Fentanyl

IndicationTreatment 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

EffentoraIndividually titrated to an

“effective”/maintenance doseThe 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

Effentora - Titration100mcg 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.

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 ~15-25minsShouldn’t be sucked or chewedIf any tablet remains after 30mins –

swallow with a glass of water

Palexia

PalexiaTapentadol

IndicationRelief 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).

Palexia SRStarting 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

PalexiaNon-Opioid Dose

Independent

Tramadol PO (mg/d)

< 400mg 400 – 600mg 600mg

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

Oxynorm DispersaOrodispersible oxycodone

Indication Treatment of severe pain/breakthrough pain

Oral useTaken every 4-6hours as neededDissolves on tongue

RelistorMethylnaltrexone

bromideSubcutaneous injection

IndicationTreatment of opioid-

induced constipation in palliative care patients when response to usual laxative therapy has not been sufficient

Given on top of usual laxatives

Relistor DoseRecommended dose

- 8 mg (0.4 ml) for patients weighing 38-61 kg - 12 mg (0.6 ml) for patients weighing 62-114 kg- Patients whose weight falls outside these ranges should be dosed at 0.15 mg/kg.

Induces prompt bowel motionSingle dose alternate days. Doses may also be given with longer intervals,

as per clinical need.Rotate injection sites (upper arms & legs,

abdomen)

RelistorUse 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]

Durogesic

Durogesic Transdermal fentanyl patch

IndicationManagement of chronic intractable pain in

patients requiring opioid analgesia

Reapplied every 72hoursInitial dose - based on the patient's current

opioid use. Recommended that Durogesic DTrans be used

in opioid tolerant patients

Durogesic DTransOpioid-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.

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

135-189 50 25-30

190-224 62 35

225-314 75 40-50

315-404 100 55-65

405-494 125 70-80

495-584 150 85-95

585-674 175 100-110

675-764 200 115-125

765-854 225 130-140

855-944 250 145-155

945-1034 275 160-170

1035-1124 300 175-185

Durogesic DTransOpioid-naïve patientsThe 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.

Durogesic – Patient InstructionApply to upper arm or chest areaDon’t apply patch in same place twice in a rowClean and dry skinTakes 18-24hr to become therapeutic intially

1.Open the pouch – tear off edge of pouch2.Mind not to tear patch3.Peel off backing – try not to touch sticky side4.Press onto skin firmly (hold for 30secs)5.Wash your hands

Butrans & TranstecTransdermal Buprenorphine

IndicationPain of moderate to severe intensityAlternative to both weak opioids and morphineNot suitable for the treatment of acute pain

Take into account previous opioid historyOpioid naive pts – prescribe lowest strength

(5mcg/h)

BuprenorphineButrans Transtec7 day patch

Doses available 5, 10 and 20mcg/h

Onset of action18–24h

Peak plasma concentration3 days

4 day patch

Doses available35, 52.5, 70mcg/h

Onset of action21h for 35mcg/h patch;11h for 70mcg/h patch

Peak plasma concentration60 hrs

Butrans vs MorphineBuprenorphine Morphine

5µg/hr 10mg/24hrs

10µg/hr 20mg/24hrs

20µg/hr 30mg/24hrs

35µg/hr 40mg/24hrs

52.5µg/hr 80mg/24hrs

70µg/hr 100mg/24hrs

ReferencesPalliative Care Formulary 3 - Robert Twycross

and Andrew Wilcockwww.palliativedrugs.comwww.medicines.ieArchimedes PharmaCephalonJanssenCilag GrunenthalMundipharmaWyeth