Boxed Warnings
Warnings. Limitations of use. Because of the risks associated with the use of opioids, DBL Pethidine Hydrochloride Injection should only be used in patients for whom other treatment options, including non-opioid analgesics, are ineffective, not tolerated or otherwise inadequate to provide appropriate management of pain (see Section 4.4 Special Warnings and Precautions for Use).
Hazardous and harmful use. DBL Pethidine Hydrochloride Injection poses risks of hazardous and harmful use which can lead to overdose and death. Assess the patient's risk of hazardous and harmful use before prescribing and monitor the patient regularly during treatment (see Section 4.4 Special Warnings and Precautions for Use).
Life-threatening respiratory depression. Serious, life-threatening or fatal respiratory depression may occur with the use of DBL Pethidine Hydrochloride Injection. Be aware of situations which increase the risk of respiratory depression, modify dosing in patients at risk and monitor patients closely, especially on initiation or following a dose increase (see Section 4.4 Special Warnings and Precautions for Use).
Concomitant use of benzodiazepines and other central nervous system (CNS) depressants, including alcohol. Concomitant use of opioids with CNS depressants medicines, such as other opioid analgesics, benzodiazepines, gabapentinoids, cannabis, sedatives, hypnotics, tricyclic antidepressants, antipsychotics, antihistamines, centrally-active anti-emetics, general anaesthetics, tranquilisers, or other central nervous system (CNS) depressants, including alcohol, may result in profound sedation, respiratory depression, coma, and death. Limit dosages and durations to the minimum required; and monitor patients for signs and symptoms of respiratory depression and sedation. Caution patients not to drink alcohol while using DBL Pethidine Hydrochloride Injection (see Section 4.4 Special Warnings and Precautions for Use).
1 Name of Medicine
DBL Pethidine Hydrochloride Injection.
2 Qualitative and Quantitative Composition
DBL Pethidine Hydrochloride Injection is a sterile, clear solution of pethidine hydrochloride in water for injections. The 50 mg/1 mL and 100 mg/2 mL presentations contain sodium hydroxide. The pH of the injection ranges between 3.5 and 6.0.
DBL Pethidine Hydrochloride Injection is a white crystalline powder, very soluble in water and freely soluble in alcohol.
For the full list of excipients, see Section 6.1 List of Excipients.
3 Pharmaceutical Form
DBL Pethidine Hydrochloride Injection is a sterile, clear solution.
4 Clinical Particulars
4.9 Overdose
Symptoms. Opioid analgesic overdosage usually produces central nervous system depression ranging from stupor to a profound coma, respiratory depression which may progress to Cheyne-Stokes respiration and/or cyanosis, cold clammy skin and/or hypothermia, flaccid skeletal muscles, bradycardia and hypotension. In patients with severe overdosage, particularly following rapid intravenous administration of an opioid, apnoea, circulatory collapse, cardiac arrest, respiratory arrest and death may occur.
Complications such as pneumonia, shock and/or pulmonary oedema may also prove fatal. Although miosis (pupillary constriction) is characteristic of overdosage with morphine derivatives and methadone, mydriasis may occur in terminal narcosis or severe hypoxia. Overdosage of DBL Pethidine Hydrochloride Injection may produce mydriasis rather than miosis.
Toxic effects of DBL Pethidine Hydrochloride Injection may be excitatory, especially in patients who have developed tolerance to the depressant effects of the drug. These patients may exhibit dry mouth, increased muscular activity, muscle tremors and twitches, tachycardia, delirium with disorientation, hallucinations and, occasionally, grand mal seizures.
Treatment. In overdosage, if necessary, establish an airway and institute assisted or controlled ventilation.
Circulation should be maintained with infusions of plasma or suitable electrolyte solution. If consciousness is impaired and respiration depressed, an opioid antagonist should be administered. Naloxone, a pure antagonist, is now the treatment of choice. Consult naloxone (or nalorphine) product information. Administer IV naloxone (e.g. 0.4 mg) which may be repeated at 2 to 3 minute intervals. For children, the initial dose recommended is 0.01 mg/kg naloxone. In neonates, a more rapid and improved antagonism was noted after 0.02 mg/kg was administered. A response should be seen after 2 or 3 doses. Note the duration of action of naloxone is usually shorter than that of DBL Pethidine Hydrochloride Injection and thus the patient should be carefully observed for signs of CNS depression returning. An opioid antagonist should not be administered in the absence of clinical signs of respiratory or cardiovascular depression.
Note. In an individual physically dependent on opioids, the administration of the usual dose of an opioid antagonist will precipitate an acute withdrawal syndrome. The severity of this syndrome will depend on the degree of physical dependence and the dose of antagonist administered. The use of opioid antagonists in such individuals should be avoided if possible. If an opioid antagonist must be used to treat serious respiratory depression in the physically dependent patient, the antagonist should be administered with extreme care and only 10 to 20% of the usual initial dose administered.
For information on the management of overdose, contact the Poisons Information Centre on 13 11 26 (Australia).
5 Pharmacological Properties
5.3 Preclinical Safety Data
Genotoxicity. No data available.
Carcinogenicity. No data available.
6 Pharmaceutical Particulars
6.7 Physicochemical Properties
Chemical structure.
https://stagingapi.mims.com/au/public/v2/images/fullchemgif/CSPETHCL.gif Chemical name: ethyl 1-methyl-4-phenylpiperidine-4-carboxylate hydrochloride.
Molecular weight: 283.8.
CAS number. 50-13-5.
7 Medicine Schedule (Poisons Standard)
Schedule 8 (controlled drug).
Summary Table of Changes
https://stagingapi.mims.com/au/public/v2/images/fulltablegif/DBLPETST.gif
