1. Name Of The Medicinal Product
Solpadol 30mg/500mg Effervescent Tablets
2. Qualitative And Quantitative Composition
Active Constituents | |
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For excipients see 6.1
3. Pharmaceutical Form
Effervescent Tablets.
Solpadol Effervescent Tablets are white bevelled-edge tablets scored on one face.
4. Clinical Particulars
4.1 Therapeutic Indications
For the relief of severe pain.
4.2 Posology And Method Of Administration
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Solpadol Effervescent Tablets are for oral administration.
4.3 Contraindications
Hypersensitivity to paracetamol or codeine which is rare.
Hypersensitivity to any of the other constituents.
Conditions where morphine and opioids are contraindicated e.g:
• Acute asthma
• Respiratory depression
• Acute alcoholism
• Head injuries
• Raised intra-cranial pressure
• Following biliary tract surgery
Monoamine oxidase inhibitor therapy, concurrent or within 14 days.
4.4 Special Warnings And Precautions For Use
Each tablet of the soluble formulation contains 388mg sodium (16.87mEquivalents). This sodium content should be taken into account when prescribing for patients in whom sodium restriction is indicated.
As this tablet contains sorbitol, patients with rare hereditary problems of fructose intolerance should not take this medicine.
Codeine is partially metabolised by CYP2D6. If a patient has a deficiency or is completely lacking this enzyme they will not obtain adequate analgesic effects. Estimates indicate that up to 7% of the caucasian population may have this deficiency. However, if the patient is an ultra-rapid metaboliser there is an increased risk of developing side effects of opioid toxicity even at low doses. General symptoms of opioid toxicity include nausea, vomiting, constipation, lack of appetite and somnolence. In severe cases this may include symptoms of circulatory and respiratory depression. Estimates indicate that up to 1 to 2% of the caucasian population may be ultra-rapid metabolisers.
The leaflet will state in the “pregnancy and breast-feeding” subsection of the section 2 “Before taking your medicine”:
Usually it is safe to take Solpadol while breast feeding as the levels of the active ingredients of this medicine in breast milk are too low to cause your baby any problems. However, some women who are at increased risk of developing side effects at any dose may have higher levels in their breast milk. If any of the following side effects develop in you or your baby, stop taking this medicine and seek immediate medical advice; feeling sick, vomiting, constipation, decreased or lack of appetite, feeling tired or sleeping for longer than normal, and shallow or slow breathing.
Care should be observed in administering the product to any patient whose condition may be exacerbated by opioids, particularly the elderly, who may be sensitive to their central and gastro-intestinal effects, those on concurrent CNS depressant drugs, those with prostatic hypertrophy and those with inflammatory or obstructive bowel disorders. Care should also be observed if prolonged therapy is contemplated.
Care is advised in the administration of paracetamol to patients with severe renal or severe hepatic impairment. The hazards of overdose are greater in those with alcoholic liver disease.
Patients should be advised not to exceed the recommended dose and not to take other paracetamol containing products concurrently. Keep the product out of the reach and sight of children.
The risk-benefit of continued use should be assessed regularly by the prescriber.
The leaflet will state in a prominent position in the 'before taking' section:
Do not take for longer than directed by your prescriber.
Taking codeine regularly for a long time can lead to addiction, which might cause you to feel restless and irritable when you stop the tablets.
Taking a pain killer for headaches too often or for too long can make them worse.
The label will state (To be displayed prominently on outer pack (not boxed) :
Do not take for longer than directed by your prescriber as taking codeine regularly for a long time can lead to addiction.
4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction
Paracetamol may increase the elimination half-life of chloramphenicol. Oral contraceptives may increase its rate of clearance. The speed of absorption of paracetamol may be increased by metoclopramide or domperidone and absorption reduced by colestyramine.
The anticoagulant effect of warfarin and other coumarins may be enhanced by prolonged regular use of paracetamol with increased risk of bleeding; occasional doses have no significant effect.
The effects of CNS depressants (including alcohol) may be potentiated by codeine.
4.6 Pregnancy And Lactation
There is inadequate evidence of the safety of codeine in human pregnancy, but there is epidemiological evidence for the safety of paracetamol. Both substances have been used for many years without apparent ill consequences and animal studies have not shown any hazard. Nonetheless careful consideration should be given before prescribing the product for pregnant patients. Opioid analgesics may depress neonatal respiration and cause withdrawal effects in neonates of dependent mothers.
Paracetamol is excreted in breast milk but not in a clinically significant amount.
At normal therapeutic doses codeine and its active metabolites may be present in breast milk at very low doses and is unlikely to adversely affect the breast fed infant.
However, if the patient is an ultra-rapid metaboliser of CYP2D6, higher levels of the active metabolites may be present in breast milk and on very rare occasions may result in symptoms of opioid toxicity in the infant.
If symptoms of opioid toxicity develop in either the mother or the infant, then all codeine containing medicines should be stopped and alternative non-opioid analgesics prescribed. In severe cases consideration should be given to prescribing naloxone to reverse these effects.
4.7 Effects On Ability To Drive And Use Machines
Patients should be advised not to drive or operate machinery if affected by dizziness or sedation.
4.8 Undesirable Effects
Codeine can produce typical opioid effects including constipation, nausea, vomiting, dizziness, light-headedness, confusion, drowsiness and urinary retention. The frequency and severity are determined by dosage, duration of treatment and individual sensitivity. Tolerance and dependence can occur, especially with prolonged high dosage of codeine.
• Regular prolonged use of codeine/DHC is known to lead to addiction and tolerance. Symptoms of restlessness and irritability may result when treatment is then stopped.
• Prolonged use of a painkiller for headaches can make them worse.
Adverse effects of paracetamol are rare:
- Immune system disorders
- Hypersensitivity including skin rash may occur.
- Not know: Anaphylactic shock, angioedema.
There have been reports of blood dyscrasias including thrombocytopenia and agranulocytosis, but these were not necessarily causally related to paracetamol.
Very rare occurrence of pancreatitis.
4.9 Overdose
Codeine:
The effects of Codeine overdosage will be potentiated by simultaneous ingestion of alcohol and psychotropic drugs.
Symptoms
Central nervous system depression, including respiratory depression, may develop but is unlikely to be severe unless other sedative agents have been co-ingested, including alcohol, or the overdose is very large. The pupils may be pin-point in size; nausea and vomiting are common. Hypotension and tachycardia are possible but unlikely.
Management
Management should include general symptomatic and supportive measures including a clear airway and monitoring of vital signs until stable. Consider activated charcoal if an adult presents within one hour of ingestion of more than 350 mg or a child more than 5 mg/kg.
Give naloxone if coma or respiratory depression is present. Naloxone is a competitive antagonist and has a short half-life so large and repeated doses may be required in a seriously poisoned patient. Observe for at least 4 hours after ingestion, or 8 hours if a sustained release preparation has been taken.
Paracetamol:
Patients in whom oxidative liver enzymes have been induced, including alcoholics and those receiving barbiturates and patients who are chronically malnourished, may be particularly sensitive to the toxic effects of paracetamol in overdose.
Symptoms
Symptoms of paracetamol overdosage in the first 24 hours are pallor, nausea, vomiting, anorexia and abdominal pain. Liver damage may become apparent 12 to 48 hours after ingestion. Abnormalities of glucose metabolism and metabolic acidosis may occur. In severe poisoning, hepatic failure may progress to encephalopathy, coma and death. Acute renal failure with acute tubular necrosis may develop even in the absence of severe liver damage. Cardiac arrhythmias and pancreatitis have been reported.
Liver damage is likely in adults who have taken 10g or more of paracetamol. It is considered that excess quantities of a toxic metabolite (usually adequately detoxified by glutathione when normal doses of paracetamol are ingested), become irreversibly bound to liver tissue.
Management
Immediate treatment is essential in the management of paracetamol overdose. Despite a lack of significant early symptoms, patients should be referred to hospital urgently for immediate medical attention and any patient who has ingested around 7.5g or more of paracetamol in the preceding 4 hours should undergo gastric lavage. Administration of oral methionine or intravenous N-acetylcysteine which may have a beneficial effect up to at least 48 hours after the overdose, may be required. General supportive measures must be available.
5. Pharmacological Properties
5.1 Pharmacodynamic Properties
Pharmacotherapeutic group: Anilides, Paracetamol combinations
ATC Code: NO2B E51
Paracetamol is an analgesic which acts peripherally, probably by blocking impulse generation at the bradykinin sensitive chemo-receptors which evoke pain. Although it is a prostaglandin synthetase inhibitor, the synthetase system in the CNS rather than the periphery appears to be more sensitive to it. This may explain paracetamol's lack of appreciable anti-inflammatory activity. Paracetamol also exhibits antipyretic activity.
Codeine is a centrally acting analgesic which produces its effect by its action at opioid-binding sites (μ-receptors) within the CNS. It is a full agonist.
5.2 Pharmacokinetic Properties
Following oral administration of two effervescent tablets (i.e., a dose of paracetamol 1000mg and codeine 60mg) the mean maximum plasma concentrations of paracetamol and codeine were 20.4μg/ml and 218.8ng/ml respectively. The mean times to maximum plasma concentrations were 0.34 hours for paracetamol and 0.42 hours for codeine phosphate.
The mean AUC for the 10 hours following administration was 50.0μg/ml per hour for paracetamol and 450.0ng/ml per hour for codeine.
The bioavailabilities of paracetamol and codeine phosphate when given as the combination are similar to those when they are given separately.
5.3 Preclinical Safety Data
There are no preclinical data of relevance which are additional to that already included in other sections of the SPC.
6. Pharmaceutical Particulars
6.1 List Of Excipients
Sodium bicarbonate
Anhydrous citric acid
Anhydrous sodium carbonate
Sorbitol powder
Saccharin sodium
Povidone
Dimeticone
Sodium lauril sulfate.
6.2 Incompatibilities
None known.
6.3 Shelf Life
4 years.
6.4 Special Precautions For Storage
Do not store above 25°C.
6.5 Nature And Contents Of Container
PPFP strips in cardboard containers.
Pack sizes: 32 and 100 tablets.
6.6 Special Precautions For Disposal And Other Handling
Solpadol Effervescent Tablets should be dissolved in half a tumblerful of water before taking.
7. Marketing Authorisation Holder
Sanofi-aventis
One Onslow Street
Guildford
Surrey
GU1 4YS, UK
8. Marketing Authorisation Number(S)
PL 04425/0636
9. Date Of First Authorisation/Renewal Of The Authorisation
4th December 2008
10. Date Of Revision Of The Text
2 November 2011
LEGAL STATUS
POM
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