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Prescribing Information

The prescribing information below relates to the UK only. Please always refer to your local prescribing information

Targinact® (oxycodone hydrochloride/naloxone hydrochloride) Prescribing Information
BuTrans® (buprenorphine) Prescribing Information
OxyContin® (oxycodone hydrochloride) Prescribing Information
Palladone® and Palladone® SR (hydromorphone hydrochloride) Prescribing Information
Penthrox  Essential Information

Targinact Prescribing Information
Targinact® (oxycodone hydrochloride/naloxone hydrochloride)
5 mg/2.5 mg, 10 mg/5 mg, 20 mg/10 mg and 40 mg/20 mg prolonged release tablets

Prescribing Information

United Kingdom

Please read the Summary of Product Characteristics (SPC) before prescribing.

Indications
Severe pain, which can be adequately managed only with opioid analgesics.
Second line symptomatic treatment of patients with severe to very severe idiopathic restless legs syndrome after failure of dopaminergic therapy.
Naloxone is added to counteract opioid-induced constipation by blocking the action of oxycodone at opioid receptors locally in the gut.

Dosage and administration

Analgesia
Adults over 18 years:
Usual starting dose for opioid naïve patients: 10 mg/5 mg taken orally at 12-hourly intervals. Patients already receiving opioids may be started on higher doses depending on their previous opioid experience. Targinact 5 mg/2.5 mg is intended for dose titration when initiating opioid therapy & individual dose adjustment. The dosage is dependent on the severity of the pain and the patient’s previous history of analgesic requirements.

Maximum daily dose of Targinact is 80 mg oxycodone hydrochloride & 40 mg naloxone hydrochloride.

Targinact is not intended for the treatment of breakthrough pain. Please refer to SPC for further details.

Restless Legs Syndrome
Adults over 18 years: Usual starting dose is 5 mg/2.5 mg at 12-hourly intervals. Titration on a weekly basis is recommended in case higher doses are required. The dosage should be adjusted to the sensitivity of the individual patient. 

Maximum daily dose of Targinact is 60 mg oxycodone hydrochloride and 30 mg naloxone hydrochloride.

Targinact is indicated for patients suffering from RLS for at least 6 months who have failed on previous doperminergic therapy. RLS symptoms should be present daily and during daytime (≥ 4 days/week). 

Patients should be clinically evaluated at least 3 monthly.

When no longer required Targinact should be tapered down over a period of approx 1 week to reduce the risk of a withdrawal reaction

Analgesia/Restless Legs Syndrome
Targinact must be swallowed whole & not be broken, chewed or crushed.

Paediatric population:
No data available.

Contra-indications

Hypersensitivity to active substances or excipients, any situation where opioids are contra-indicated, severe respiratory depression with hypoxia and/or hypercapnoea; severe COPD, cor pulmonale, severe bronchial asthma, non-opioid induced paralytic ileus, moderate to severe hepatic impairment. History of opioid abuse.

Precautions and warnings

Respiratory depression, elderly or infirm, opioid-induced paralytic ileus, severely impaired pulmonary function, sleep apnoea, myxoedema, hypothyroidism, adrenocortical insufficiency, toxic psychosis, cholelithiasis, prostate hypertrophy, alcoholism, delirium tremens, pancreatitis, hypo- or hyper-tension, pre-existing cardiovascular diseases, head injury, epileptic disorder, predisposition to convulsions, patients taking MAO inhibitors, history of alcohol/drug abuse, galactose intolerance, Lapp lactase deficiency, glucose-galactose malabsorption, mild hepatic or renal impairment, pre-operative use or within the first 12 - 24 hours post-operatively. Not suitable for treatment of withdrawal symptoms.

Not recommended in cancer associated with peritoneal carcinomatosis or sub-occlusive syndrome in advanced stages of digestive & pelvic cancers. Concomitant use of alcohol and Targinact may increase the undesirable effects of Targinact and should be avoided. Caution advised if combining with other sedating medicinal products due to potential additive effects. Refrain from driving or operating machines if somnolence/sudden sleep onset experienced.

Tolerance and dependence may occur. It may be advisable to taper dose when stopping treatment to prevent withdrawal symptoms.

Caution is advised in treating restless legs syndrome patients with additional sleep apnoea syndrome with Targinact due to the additive risk of respiratory depression. No data about the risk exist because in the clinical trial patients with sleep apnoea syndrome were excluded.

There is no clinical experience with Targinact in the long-term treatment of RLS beyond 1 year.

Interactions

Substances having a CNS-depressant effect (e.g. other opioids, sedatives, hypnotics, anti-depressants, phenothiazines, neuroleptics, anti-histamines and anti-emetics) may enhance CNS-depressant effect of Targinact (e.g. respiratory depression). Alcohol may enhance the pharmacodynamic effects of Targinact; concomitant use should be avoided. Interaction with coumarin anticoagulants may increase/decrease INR. Inhibitors or inducers of CYP3A4 or CYP2D6 may affect the metabolism of oxycodone. Dose titration may be necessary.

Pregnancy and lactation

Not recommended.

Side-effects

Common: decreased/loss of appetite, insomnia, altered mood and personality changes, decreased activity, psychomotor hyperactivity, dizziness, headache, somnolence, vertigo, hot flush, abdominal pain, constipation, diarrhoea, dry mouth, dyspepsia, flatulence, hiccups, vomiting, nausea, pruritus, skin reactions, hyperhidrosis, dysuria, asthenic conditions, fatigue, depressiondisturbance in attention, tremor, paraesthesia, visual impairment, hepatic enzymes increased, chest pain, chills, thirst, pain, blood pressure decreased, blood pressure increased.

Other side effects which are potentially serious: hypersensitivity, anaphylactic response, restlessness, confusion, agitation, reduced libido, depression, euphoric mood, hallucinations, convulsions, speech disorder, syncope, paraesthesia, sedation, drug dependence, migraine, concentration impairment, visual impairment, palpitations, angina pectoris, tachycardia, decrease in blood pressure, increase in blood pressure, dyspnoea, respiratory depression, tooth disorder, dysphagia, ileus, melaena, gingival bleeding, hepatic enzymes increase, cholestasis, biliary colic, urticaria, erectile dysfunction, amenorrhoea, oedema, peripheral oedema, urinary retention, drug withdrawal syndrome, chest pain, injuries from accidents and drug tolerance.

Refer to SPC for further details of other side-effects and oxycodone class-effects.

Legal category

CD (Sch2) POM

Package quantities and price

Blisters of 28 tablets:
5 mg/2.5 mg - £21.16

Blisters of 56 tablets:
10 mg/5 mg - £42.32
20 mg/10 mg - £84.62
40 mg/20 mg - £169.28

Marketing Authorisation numbers

PL 16950/0157-158, PL16950/0161-162

Marketing Authorisation holder

Napp Pharmaceuticals Limited
Cambridge Science Park
Milton Road
Cambridge
CB4 0GW
UK

Tel: 01223 424444

Member of the Napp Pharmaceutical Group.

For medical information enquiries, please contact medicalinformationuk@napp.co.uk

® Targinact, NAPP and the NAPP device (logo) are Registered Trade Marks.

© 2015 Napp Pharmaceuticals Limited.

PI Code UK/TARG-15001. PI Approved May 2015.
Adverse events should be reported. Reporting forms and information can be found at www.mhra.gov.uk/yellowcard. Adverse events should also be reported to Napp Pharmaceuticals Limited on 01223 424444.

BuTrans Prescribing Information

BuTrans® is licensed for the treatment of non-malignant pain of moderate intensity when an opioid is necessary for obtaining adequate analgesia. BuTrans is also known by the name Norspan® in other countries. Please refer to local prescribing information.

BuTrans® 5 µg/h, 10 µg/h and 20 µg/h Transdermal Patch

Prescribing Information

United Kingdom

Please read the Summary of Product Characteristics before prescribing.

Presentation

BuTrans 5 µg/h, 10 µg/h, 20 µg/h.

Transdermal beige patches containing buprenorphine.

Indications

Treatment of non-malignant pain of moderate intensity when an opioid is necessary for obtaining adequate analgesia.

BuTrans  is not suitable for the treatment of acute pain.

Dosage and administration

BuTrans  should be administered every 7 days.

Elderly and adults over 18 years only: Use the 5 µg/h patch for at least the first 3 days of treatment, before increasing the dose if necessary. Do not use more than two patches at a time.

Contra-indications

Known buprenorphine or excipient hypersensitivity, opioid-dependent patients, narcotic withdrawal treatment, respiratory depression, use of monoamine oxidase inhibitors (MAOIs) within the past 2 weeks, myasthenia gravis, delirium tremens.

Precautions and warnings

Convulsive disorders, head injury, shock, reduced consciousness of uncertain origin, intracranial lesions or increased intracranial pressure, severe hepatic impairment, history of drug abuse. Not recommended immediately postoperatively or for situations characterised by a narrow therapeutic index or for rapidly varying analgesic requirements. May affect ability to drive or use machinery.

Interactions

MAOIs, CNS depressants (e.g. benzodiazepines, opioid derivatives, antidepressants, sedatives, alcohol, anxiolytics, neuroleptics, clonidine). CYP 3A4 inhibitors and inducers, products reducing hepatic blood flow (e.g. halothane).

Pregnancy and lactation

BuTrans should not be used during pregnancy or in women of childbearing potential who are not using effective contraception. The use of BuTrans  during lactation should be avoided.

Side-effects

Very common (≥1/10) and common (≥1/100, <1/10) side-effects are anorexia, confusion, depression, insomnia, nervousness, headache, dizziness, somnolence, paraesthesia, vasodilation, dyspnoea, constipation, dry mouth, nausea, vomiting, abdominal pain, diarrhoea, dyspepsia, pruritus, erythema, rash, sweating, exanthema, tiredness, application site reaction, asthenia, pain, peripheral oedema, chest pain.

Uncommon (< 1/100) but potentially serious side-effects are respiratory depression, anaphylactic reaction, anaphylactoid reaction, hypersensitivity, blurred vision, affect lability, agitation, depersonalisation, drug dependence, euphoric mood, hallucinations, mood swings, psychotic disorder, restlessness, balance disorder, migraine, sedation, speech disorder, dysarthria, syncope, eyelid oedema, visual disturbance, vertigo, angina pectoris, palpitations, tachycardia, circulatory collapse, hypertension, hypotension, asthma aggravated, wheezing, hyperventilation, hypoxia, respiratory failure, diverticulitis, dysphagia, ileus, biliary colic, face oedema, urticaria, muscular weakness, urinary retention, micturition disorder, decreased libido, erectile dysfunction, sexual dysfunction, drug withdrawal syndrome, oedema, alanine amintotransferase increased, accidental injury, fall.

Please consult the SPC for details of other side-effects.

Legal category

CD (Sch3) POM

Package quantities and price:
4 individually sealed patches:
5 µg/h transdermal patch £17.60
10 µg/h transdermal patch £31.55
20 µg/h transdermal patch £57.46

Marketing Authorisation numbers

PL 16950/136-138

Marketing Authorisation holder

Napp Pharmaceuticals Limited
Cambridge Science Park
Milton Road
Cambridge CB4 0GW
UK

Tel: 01223 424444

Member of the Napp Pharmaceutical Group

For medical information enquiries, please contact medicalinformationuk@napp.co.uk

Date effective January 2013

® BuTrans and the NAPP device (logo) are Registered Trade Marks.

© 2011 -2012 Napp Pharmaceuticals Limited.

Adverse events should be reported. Reporting forms and information can be found at www.mhra.gov.uk/yellowcard. Adverse events should also be reported to Napp Pharmaceuticals Limited on 01223 424444.

OxyContin Prescribing Information

OxyContin® (oxycodone hydrochloride) 5 mg, 10 mg, 15 mg, 20 mg,
30 mg, 40 mg, 60 mg, 80 mg, 120 mg prolonged release tablets

PRESCRIBING INFORMATION

United Kingdom

Please read the Summary of Product Characteristics (SmPC) before prescribing.

Indications

Moderate to severe pain in patients with cancer or post-operative pain. Severe pain requiring the use of a strong opioid.

Dosage & administration

Tablets must be swallowed whole, and not broken, chewed or crushed.

Elderly and adults over 18 years:

Take tablets at 12-hourly intervals. Dosage is dependent on the severity of pain and the patient’s previous history of analgesic requirements. Not intended for use as a prn analgesic.

Usual starting dose for opioid naïve patients, or patients presenting with severe pain uncontrolled by weaker opioids: 10 mg, 12-hourly. Some patients may benefit from a starting dose of 5 mg to minimise the incidence of side-effects. Opioid naïve patients with mild to moderate renal and/or mild hepatic impairment may be started on 5 mg, 12-hourly and titrated to pain relief. Any dose increases should be made, where possible, in 25%-50% increments. When transferring from morphine, the following ratio should be used as guidance: 10 mg oral oxycodone is equivalent to 20 mg oral morphine. Opioids are not firstline therapy in non-malignant pain, nor are they recommended as the only treatment. The need for continued treatment in non-malignant pain should be assessed at regular intervals.

Children under 18 years:

Not recommended.

Contra-indications

Respiratory depression, head injury, paralytic ileus, acute abdomen, delayed gastric emptying, chronic obstructive airways disease, cor pulmonale, severe bronchial asthma, hypercarbia, known sensitivity to oxycodone or any of the constituents, moderate to severe hepatic impairment, severe renal impairment, chronic constipation, concurrent administration of monoamine oxidase inhibitors or within two weeks of discontinuation of their use, galactose intolerance, lactase deficiency, glucosegalactose malabsorption, any situation where opioids are contraindicated, pre-operative use or use during the first 24 hours post-operatively, pregnancy.

Precautions and warnings

Hypothyroidism, opioid dependent patients, raised intracranial pressure, hypotension, hypovolaemia, toxic psychosis, diseases of the biliary tract, pancreatitis, inflammatory bowel disorders, prostatic hypertrophy, adrenocortical insufficiency, alcoholism, delirium tremens, chronic renal and hepatic disease, severe pulmonary disease, debilitated patients, elderly and infirm patients, history of alcohol and/or drug abuse. Do not use where there is a possibility of paralytic ileus occurring and if this is suspected or occurs during use discontinue immediately. Patients about to undergo additional pain relieving procedures (e.g. surgery, plexus blockade) should not receive OxyContin  tablets for 12 hours prior to the intervention. OxyContin  60 mg, 80 mg and 120 mg tablets should not be used in opioid niaïve patients. OxyContin  tablets should be used with caution following abdominal surgery, and not used until normal bowel function returns. OxyContin  tablets have a similar abuse profile to other strong opioids. OxyContin  tablets must be swallowed whole and not broken, chewed or crushed which leads to a rapid release and absorption of a potentially fatal dose of oxycodone. Concomitant use of alcohol and OxyContin  tablets may increase the undesirable effects of OxyContin  tablets; concomitant use should be avoided.

Interactions

OxyContin tablets, like other opioids, potentiate the effects of transquilisers, anaes thetics, hypnotics, antidepressants, sedatives, phenothiazines, neuroleptic drugs, other opioids, muscle relaxants and antihypertensives. Monoamine oxidase inhibitors are known to interact with narcotic analgesics, producing CNS excitation or depression with hypertensive or hypotensive crisis. Inhibitors of CYP3A4 or CYP2D6 may inhibit the metabolism of oxycodone. Alcohol may enhance the pharmacodynamic effects of OxyContin tablets; concomitant use should be avoided.

Pregnancy and lactation

Not recommended.

Side-effects

Common (≥ 1%): constipation, nausea, vomiting, dry mouth, anorexia, dyspepsia, abdominal pain, diarrhoea, headache, confusional state, asthenic conditions, dizziness, sedation, anxiety, abnormal dreams, nervousness, insomnia, thinking abnormal, somnolence, bronchospasm, dyspnoea, cough decreased, rash, pruritus, hyperhidrosis, chills.

Uncommon (≤ 1%) but potentially serious: anaphylactic reaction, anaphylactoid reaction, hypersensitivity, biliary colic, cholestasis, ileus, gastritis, dysphagia, dental caries, hallucinations, depression, dysphoria, affect lability, mood altered, restlessness, agitation, euphoria, disorientation, amnesia, vision abnormal, vertigo, drug tolerance, drug dependence, drug withdrawal syndrome, paraesthesia, speech disorder, convulsions, urinary retention, ureteral spasm, libido decreased, supraventricular tachycardia, hypotension, orthostatic hypotension, respiratory depression, syncope, oedema, oedema peripheral, increased hepatic enzymes, exfoliative dermatitis, urticaria, amenorrhoea, erectile dysfunction.

Overdose may produce respiratory depression, pin-point pupils, hypotension and hallucinations. Circulatory failure and somnolence progressing to stupor or deepening coma, skeletal muscle flaccidity, bradycardia and death may occur in more severe cases. The effects of overdosage will be potentiated by the simultaneous ingestion of alcohol or other psychotropic drugs.

Please refer to the SmPC for a full list of side-effects.

Tolerance and dependence may occur. It may be advisable to taper the dose when stopping treatment to prevent withdrawal symptoms.

Legal category

CD (Sch2) POM

Package quantities and price

5 mg – £12.52 (28 tablets)
10 mg – £25.04 (56 tablets)
15 mg – £37.41 (56 tablets)
20 mg – £50.08 (56 tablets)
30 mg – £74.81 (56 tablets)
40 mg – £100.19 (56 tablets)
60 mg – £149.66 (56 tablets)
80 mg – £200.39 (56 tablets)
120 mg – £299.31 (56 tablets)

Marketing Authorisation numbers

PL 16950/0097-0100, 0123, 0139-0141, 0150

Marketing Authorisation holder

Napp Pharmaceuticals Limited
Cambridge Science Park
Milton Road
Cambridge CB4 0GW
UK

Tel: 01223 424444

Member of the Napp Pharmaceutical Group

For medical information enquiries, please contact medicalinformationuk@napp.co.uk

® OxyContin  and the NAPP device are Registered Trade Marks.

© 2011 – 2012 Napp Pharmaceuticals Limited

European Patent (UK) 0 253 104

European Patent (UK) 0 576 643

European Patent Application No. 96102992.3

Adverse events should be reported. Reporting forms and information can be found at www.mhra.gov.uk/yellowcard. Adverse events should also be reported to Napp Pharmaceuticals Limited on 01223 424444.

Palladone and Palladone SR Prescribing Information

Palladone® capsules 1.3 mg and 2.6 mg
Palladone® SR capsules 2 mg, 4 mg, 8 mg, 16 mg, 24 mg

Prescribing Information

United Kingdom

Please read the Summary of Product Characteristics before prescribing.

Indications

For the relief of severe pain in cancer.

Dosage and administration

Palladone capsules can be swallowed whole or their contents can be sprinkled onto cold soft food. The contents of Palladone SR capsules must be swallowed whole and not chewed or crushed.

Adults and children over 12 years: The normal starting dose is one Palladone capsule 1.3 mg, 4-hourly or, alternatively, one Palladone SR capsule 4 mg, 12-hourly.
Increasing severity of pain will require increased dosage of hydromorphone to achieve the desired relief.
Elderly and patients with renal impairment: These patients may require a lower dosage than adults to achieve adequate analgesia.
Children under 12 years: not recommended.

Contra-indications

Hypersensitivity to hydromorphone or any of the capsule ingredients.
Respiratory depression with hypoxia or elevated blood carbon dioxide levels, pregnancy, coma, acute abdomen, hepatic impairment, paralytic ileus, concurrent administration of monoamine oxidase inhibitors or within 2 weeks of discontinuation of their use, raised intracranial pressure or head injury, patients with convulsive disorders or acute alcoholism, pre-operative use of the SR capsules.

Precautions and warnings

Respiratory depression, severely impaired pulmonary function, toxic pyschosis, delirium tremens, pancreatitis, hypothyroidism, hypotension with hypovolaemia, chronic obstructive airways disease, renal or adrenocortical insufficiency, prostatic hypertrophy, shock or reduced respiratory reserve. Hydromorphone is not recommended in the first 24 hours post-operatively. After this time use with caut on, particularly following abdominal surgery. Do not use where there is the possibility of paralytic ileus occurring. Patients about to undergo cordotomy or other pain relieving surgical procedures should not receive the SR capsules for 24 hours before surgery, and the normal release capsules for 4 hours before surgery. Tolerance and dependence may occur. It may be advisable to taper dose when stopping treatment to prevent withdrawal symptoms. Hydromorphone has a morphine-like abuse profile. Use with particular care in patients with a history of alcohol and drug abuse.

Interactions

Major and minor tranquillisers, anaesthetics, barbiturates, antiemetics, antidepressants, alcohol, neuroleptics, hypnotics, other opioids, monoamine oxidase inhibitors and sedatives may interact with hydromorphone, and potentiate the effects of either drug, e.g. sedation, respiratory depression, etc. Alcohol may enhance the pharmacodynamic effects of Palladone SR capsules; concomitant use should be avoided.

Pregnancy and lactation

Not recommended

Side-effects

Common: hypotension, constipation, dry mouth, nausea, vomiting, asthenic conditions, dizziness, somnolence, confusion, urinary retention, pruritus, rash and sweating

Uncommon but potentially serious: biliary colic, paralytic ileus, drug withdrawal syndrome, drug tolerance, peripheral oedema, hypersensitivity reactions (including oropharyngeal swelling), convulsions, agitation, blurred vision, dysphoria, euphoria, myoclonus, sedation, hallucination, urticaria and respiratory depression.

Refer to SPC for further details of other side-effects and hydromorphone class-effects.

Legal category:

CD (Sch 2) POM.

Package quantities and price:
Blister packs of 56 capsules.
Palladone capsules 1.3 mg – £8.82
Palladone capsules 2.6 mg – £17.64
Palladone SR capsules 2 mg – £20.98
Palladone SR capsules 4 mg – £28.75
Palladone SR capsules 8 mg – £56.08
Palladone SR capsules 16 mg – £106.53
Palladone SR capsules 24 mg – £159.82

Marketing authorisation numbers

Palladone capsules 1.3 mg, 2.6 mg – PL 16950/0049 – 0050
Palladone SR capsules 2 mg, 4 mg, 8 mg, 16 mg, 24 mg – PL 16950/0051 – 0055

Marketing authorisation holder

Napp Pharmaceuticals Limited
Cambridge Science Park
Milton Road
Cambridge CB4 0GW
UK

Tel: 01223 424444

Member of the Napp Pharmaceutical Group

For medical information enquiries, please contact medicalinformationuk@napp.co.uk

Date of preparation:
November 2015

Palladone, NAPP and the NAPP device (logo) are Registered Trade Marks.

© 2015 Napp Pharmaceuticals Limited.

Adverse events should be reported. Reporting forms and information can be found at www.mhra.gov.uk/yellowcard. Adverse events should also be reported to Napp Pharmaceuticals Limited on 01223 424444.

PI Code: UK/PAL-15001
PI Approved November 2015

Penthrox Essential Information

Penthrox 3mL inhalation vapour, liquid

ESSENTIAL INFORMATION

Presentation

Each vial of Penthrox contains 3mL of methoxyflurane 99.9%, a clear almost colourless, volatile liquid, with a characteristic fruity odour. Each Penthrox combination pack consists of one 3mL bottle, one Penthrox inhaler and one Activated Carbon (AC) chamber.

Indication:

Emergency relief of moderate to severe pain in conscious adult patients with trauma and associated pain.

Dosage and administration:

Penthrox should be self-administered under a supervision of a person trained in its administration, using the hand held Penthrox inhaler

Adults: One bottle of 3mL Penthrox to be vaporised in a Penthrox inhaler. On finishing the 3mL dose another 3mL may be used. The dose should not exceed 6mL in a single administration. Methoxyflurane may cause renal failure if the recommended dose is exceeded. The lowest effective dosage to provide analgesia should be used. Onset of pain relief is rapid and occurs after 6-10 inhalations. Patients are able to titrate the amount of Penthrox inhaled and should be instructed to inhale intermittently to achieve adequate analgesia. Continuous inhalation provides analgesic relief for up to 25-30 minutes; intermittent inhalation may provide longer analgesic relief. Administration on consecutive days is not recommended and the total dose to a patient in a week should not exceed 15mL.

Children: Penthrox should not be used in children under 18 years of age.

Contraindications:

Use as an anaesthetic agent; hypersensitivity to Penthrox or any fluorinated anaesthetic; malignant hyperthermia: patients with known or genetically susceptible to malignant hyperthermia or a history of severe adverse reactions in either patient or relatives; patients who have a history of showing signs of liver damage after previous methoxyflurane use or halogenated hydrocarbon anaesthesia; clinically significant renal impairment; altered level of consciousness due to any cause including head injury, drugs, or alcohol; clinically evident cardiovascular instability; clinically evident respiratory depression.

Warnings and Precautions:

Methoxyflurane causes significant nephrotoxicity at high doses. Nephrotoxicity is also related to the rate of metabolism. Drugs that induce hepatic enzymes and subgroups of people with genetic variations that may result in fast metaboliser status may increase the risk of toxicity with methoxyflurane. The lowest effective dose should be administered especially in the elderly or patients with other known risk factors of renal disease. Methoxyflurane should be used cautiously in patients with conditions that would pre-dispose to renal injury. Penthrox should be used with caution in patients with underlying hepatic conditions or with risks for hepatic dysfunction. Previous exposure to halogenated hydrocarbon anaesthetics especially if the interval is less than 3 months, may increase the potential for hepatic injury. Cautious clinical judgement should be exercised when Penthrox is to be used more frequently than on one occasion every 3 months. Caution required in the elderly due to possible reduction in blood pressure. Potential CNS effects such as sedation, euphoria, amnesia, ability to concentrate, altered sensorimotor co-ordination and change in mood are also known class-effects. The CNS effects can be a risk factor for potential abuse. The Activated Carbon (AC) Chamber should be used to adsorb exhaled methoxyflurane reducing the risk of occupational exposure. Penthrox is not appropriate for providing relief of break-through pain/exacerbations in chronic pain conditions or for the relief of trauma related pain in closely repeated episodes for the same patient.

Interactions

There are no reported drug interactions when used at the analgesic dosage (3 – 6 mL). Enzyme inducers can increase the rate of methoxyflurane metabolism. Enzyme inducers for CYP 2E1 (e.g. alcohol or isoniazid) and CYP 2A6 (e.g. phenobarbital or rifampicin should be avoided concomitantly with methoxyflurane as they may increase its potential toxicity. Concomitant use of Penthrox with CNS depressants, such as opioids, sedatives or hypnotics, general anaesthetics, phenothiazines, tranquillisers, skeletal muscle relaxants, sedating antihistamines and alcohol may produce additive depressant effects. Concomitant use of methoxyflurane with antibiotics known to have a nephrotoxic effect (e.g. tetracycline, gentamicin, colistin, polymyxin B and amphotericin B) should be avoided as there may be an additive effect on nephrotoxicity. Sevoflurane anaesthesia should be avoided following the use of Penthrox, as sevoflurane increase serum fluoride levels and methoxyflurane nephrotoxicity is associated with raised serum fluoride.

Fertility, pregnancy and lactation

No clinical data on effects of methoxyflurane on fertility are available. As with all medicines care should be exercised when administered during pregnancy especially the first trimester. There is insufficient information on the excretion of methoxyflurane in human milk. Caution should be exercised when methoxyflurane is administered to a nursing mother.

Effects on ability to drive and use machines

Methoxyflurane may have a minor influence on the ability to drive and use machines. Patients should be advised not to drive or operate machinery if they are feeling drowsy or dizzy.

Undesirable effects

Common: Amnesia, anxiety, depression, dizziness, dysarthria, dysgeusia, euphoria, headache, sensory neuropathy, somnolence, hypotension, coughing, dry mouth, nausea, feeling drunk sweating. Uncommon but potentially serious: paresthesia, diplopia. Post-marketing experience: Rare (≥1/10,000 to <1/1,000) reports of hepatic failure/hepatitis have been observed with analgesic use of methoxyflurane. Other events linked to the methoxyflurane use in analgesia (in addition to the reactions from clinical trials listed above), including reports from the literature include: drowsiness, agitation, restlessness, dissociation, affect lability, disorientation, altered state of consciousness, choking, hypoxia, oxygen saturation decreased, blood pressure fluctuation, vomiting, hepatitis, increased liver enzymes, jaundice, liver injury, increased serum uric acid, urea nitrogen and creatinine, renal failure, blurred vision, nystagmus. Refer to SmPC for further details of other uncommon side-effects.

Legal category: POM

Shelf life: 36 months

Special precautions for storage: No special temperature storage conditions. Penthrox should be kept in a locked cabinet, and should not be left on an open shelf.

Date of preparation: June 2016

Adverse events should be reported. Reporting to the applicable regulatory authorities should be in accordance with National Requirements and to the applicable holder of the marketing authorisation for Penthrox, details of which can be found on product packaging and/or inserts

PI Code: MINT/PROX-16003

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