Paralgin/Paralgin Forte

Paralgin/Paralgin Forte

paracetamol + codeine

Manufacturer:

GoodScience

Distributor:

Mederis
Full Prescribing Info
Contents
Paralgin: Paracetamol, codeine phosphate hemihydrate.
Paralgin Forte:
Paracetamol, codeine phosphate sesquihydrate.
Description
Each tablet contains: Paralgin: Paracetamol 500mg, Codeine phosphate hemihydrate 8mg.
Paralgin Forte: Paracetamol 400mg, Codeine phosphate sesquihydrate 30mg.
Action
Pharmacology: Pharmacodynamics: Paracetamol appears to produce analgesia at a subcorticol site of brain, and may also block pain impulses by a depressant effect on peripheral chemoreceptors, mainly by inhibiting and interfering with the prostaglandin synthesis. Paracetamol lowers body temperature by acting in the hypothalamus to produce antipyresis.
Codeine Phosphate has a central action especially in the cortex, thereby raising the threshold for pain.
Pharmacokinetics: Paracetamol and Codeine phosphate are well absorbed from the gastrointestinal tract. The peak concentrations in plasma are attained in about 1 hour. The half-life is about 1 to 3 hours for Paracetamol and about 2.5 to 3 hours for Codeine Phosphate after therapeutic doses. The duration of action varies between 4-6 hours.
Metabolism and Excretion: Following therapeutic doses, about 80% of the Paracetamol undergoes conjugation with glucoronic acid in the liver, and only 3% is excreted as unchanged drug.
Codeine Phosphate is metabolised in the liver and excreted primarily as an inactive metabolites, two-third of these within 6 hours of ingestion.
Indications/Uses
Paralgin/Paralgin Forte is indicated for the relief of painful disorders such as headache, dysmenorrhea, conditions involving musculoskeletal pain, myalgias, and neuralgias. It is also indicated as an analgesic and antipyretic in conditions accompanied by discomfort and fever, such as the common cold and viral infections.
Paralgin/Paralgin Forte is an effective analgesic after dental work and tooth extractions.
Dosage/Direction for Use
Adults: 1-2 tablets every 4-6 hours.
Children (12-18 year): 1 tablet up to 4 times daily.
Paediatric Population: Children aged less than 12 year: Codeine should not be used in children below the age of 12 years because of the risk of opioid toxicity due to the variable and unpredictable metabolism of codeine to morphine.
Paralgin/Paralgin Forte is contraindicated in children below the age of 12 years for the symptomatic treatment of cold.
Children aged 12 years to 18 years: Paralgin/Paralgin Forte is not recommended for use in children aged 12 years to 18 years with compromised respiratory function.
Route of Administration: Oral.
Overdosage
Paracetamol: 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 have been reported.
Codeine phosphate: Overdosage may produce central nervous stimulation, nausea, drowsiness, respiratory depression, cyanosis, coma. Convulsion may occur in infants and children.
Treatment: General: Aspiration or gastric lavage, followed by oral administration of activated charcoal.
Codeine phosphate: If necessary, combined with anticonvulsant therapy and control of respiration. Antidote, 0.4 mg Naloxone hydrochloride may be given intravenously and repeated every 3-4 minutes until normal respiration is restored. Observed the patient for 24 hours.
Paracetamol: Intravenous administration of 300mg of N-acetylcysteine per kg over 20 hour period or oral treatment with 1330 mg N-acetylcysteine per kg over 72 hour period is accepted. Treatment should be started within 8 hours after overdose but is still indicated at least as late as 24 hours after ingestion.
Contraindications
Hypersentivity to the active ingredients. Acute hepatitis. It should be given with care to patients with impaired kidney or liver function, also patients taking other drugs that affect the liver.
In children below the age of 12 years for the symptomatic treatment of colds due to an increased risk of developing serious and life-threatening adverse reactions.
In all paediatric patients (0-18 years of age) who undergo tonsillectomy or adenoidectomy for obstructive sleep apnoea syndrome due to increased risk of developing serious and life-threatening adverse reactions.
In women who are breastfeeding.
In patients for whom it is known they are CYP2D6 ultra-rapid metabolisers.
Warnings
This preparation contains PARACETAMOL.
Do not take other paracetamol containing medicines at the same time.
Special Precautions
Do not exceed the recommended dose. At high doses codeine has most of the disadvantages of morphine, including respiratory depression. Codeine can produce drug dependence and therefore has the potential of being abused. Codeine may impair the mental and/or physical abilities required for the performance of potentially hazardous tasks.
Allergy alert: Paracetamol may cause severe skin reactions. Symptoms may include skin reddening, blister or rash. These could be signs of a serious condition. If these reactions occur, stop use and seek medical assistance right away.
Caution is advised when codeine is used in patients with underlying respiratory conditions, including those with asthma and other chronic breathing problems.
Parents and caregiver of paediatric patients should be advised on the possible sign and symptom of respiratory depression in their children such as unusual sleepiness, confusion and difficult or noisy breathing and to seek immediate medical attention if these are observed.
Nursing mothers should also be advised to exercise caution when taking codeine, since codeine's metabolite (morphine) subsequently be found in the breast milk. If the infant shows sign of increased sleepiness, difficulty breastfeeding, breathing difficulties and limpness, immediate medical attention should be sought.
Risks from Concomitant Use with Benzodiazepines: Profound sedation, respiratory depression, coma, and death may result from the concomitant use of Paralgin/Paralgin Forte with benzodiazepines. Observational studies have demonstrated that concomitant use of opioids and benzodiazepines increases the risk of drug-related mortality compared to use of opioids alone. Because of these risks, reserve concomitant prescribing of these drugs for use in patients for whom alternative treatment options are inadequate.
If the decision is made to newly prescribe a benzodiazepine and an opioid together, prescribe the lowest effective dosages and minimum durations of concomitant use.
If the decision is made to prescribe a benzodiazepine in a patient already receiving an opioid, prescribe a lower initial dose of benzodiazepine than indicated in the absence of an opioid, and titrate based on clinical response.
Follow patients closely for signs and symptoms of respiratory depression and sedation. Advise both patients and caregivers about the risks of respiratory depression and sedation when Paralgin/Paralgin Forte is used with benzodiazepines. Advise patients not to drive or operate heavy machinery until the effects of concomitant use of the benzodiazepines have been determined. Screen patients for risk of substance use disorders, including opioid abuse and misuse, and warn them of the risk for overdose and death associated with the use of benzodiazepines (see Interactions).
CYP2D6 metabolism: Codeine is metabolised by the liver enzyme CYP2D6 into morphine, its active metabolite. If a patient has a deficiency or is completely lacking these enzymes an adequate analgesic effect will not be obtained. Estimates indicate that up to 7% of Caucasian population may have this deficiency. However, if the patient is an extensive or ultra-rapid metaboliser there is an increased risk of developing side effects of opioid toxicity even at commonly prescribed doses. These patients convert codeine into morphine rapidly resulting in higher than expected serum morphine levels.
General symptoms of opioids toxicity include confusion, somnolence, shallow breathing, small pupils, nausea, vomiting, constipation and lack of appetite. In severe cases this may include symptoms of circulatory and respiratory depression, which may be life-threatening and very rarely fatal. Estimates of prevalence of ultra- rapid metabolizers in different populations are summarized below: (see table).

Click on icon to see table/diagram/image

Post-operative use in children: There have been reports in the published literature that codeine given post-operatively in children after tonsillectomy or adenoidectomy for obstructive sleep apnoea, led to rare, but life-threatening adverse events including death. All children received doses of codeine that were within the appropriate dose range; however there was evidence that these children were either ultra-rapid or extensive metabolizers in their ability to metabolize codeine to morphine.
Children with compromised respiratory function: Codeine is not recommended for use in children in whom respiratory function might be compromised including neuromuscular disorders, severe cardiac or respiratory conditions, upper respiratory or lung infections, multiple trauma or extensive surgical procedures. These factors may worsen symptoms of morphine toxicity.
Serotonin Syndrome with Concomitant Use of Serotonergic Drugs: Cases of serotonin syndrome, a potentially life-threatening condition, have been reported during concurrent use of Paralgin/Paralgin Forte with serotonergic drugs (See Interactions). This may occur within the recommended dosage range.
Serotonin syndrome symptoms may include mental-status changes (e.g. agitation, hallucinations, coma), autonomic instability (e.g. tachycardia, labile blood pressure, hyperthermia), neuromuscular aberrations (e.g. hyperreflexia, incoordination) and/or gastrointestinal symptoms (e.g. nausea, vomiting, diarrhea) and can be fatal (See Interactions). The onset of symptoms generally occurs within several hours to a few days of concomitant use, but may occur later than that. Discontinue Paralgin/Paralgin Forte if serotonin syndrome is suspected.
Adrenal Insufficiency: Cases of adrenal insufficiency have been reported with opioid use, more often following greater than one month of use. Presentation of adrenal insufficiency may include non-specific symptoms and signs including nausea, vomiting, decreased appetite, fatigue, weakness, dizziness, and low blood pressure. If adrenal insufficiency is suspected, confirm the diagnosis with diagnostic testing as soon as possible. If adrenal insufficiency is diagnosed, treat with physiologic replacement dosing of corticosteroids. Wean the patient off of the opioid to allow adrenal function to recover and continue corticosteroid treatment until adrenal function recovers. Other opioids may be tried as some cases reported use of a different opioid without recurrence of adrenal insufficiency. The information available does not identify any particular opioids as being more likely to be associated with adrenal insufficiency.
Sexual Function/Reproduction: Long term use of opioids may be associated with decreased sex hormone levels and symptoms such as low libido, erectile dysfunction, or infertility (See Postmarketing Experience under Adverse Reactions.)
Use In Pregnancy & Lactation
Pregnancy: 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.
As a precautionary measure, use of Paralgin/Paralgin Forte should be avoided during the third trimester of pregnancy and during labor.
Breastfeeding: Paralgin/Paralgin Forte is contraindicated in women during breastfeeding.
At normal therapeutic doses codeine and its active metabolite 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 metabolizer of CYP2D6, higher levels of the active metabolite, morphine, may be present in breast milk and on very rare occasions may result in symptoms of opioid toxicity in the infant, which may be fatal.
Adverse Reactions
Mild drowsiness. Sensitive patients may experience constipation and biliary dyskinesia. High doses of paracetamol may increase the activity of coumarin anticoagulant.
Cutaneous hypersensitivity reactions including skin rashes, angioedema, Stevens Johnson Syndrome/Toxic Epidermal Necrolysis have been reported.
Codeine phosphate potentiates the effect of alcohol and other central depressive drugs. Other adverse reactions include allergic reaction, euphoria, dysphoria, abdominal pain and pruritus.
Postmarketing Experience: Serotonin syndrome: (See Precautions).
Adrenal insufficiency: (See Precautions).
Androgen deficiency: Cases of androgen deficiency have occurred with chronic use of opioids. Chronic use of opioids may influence the hypothalamic-pituitary-gonadal axis, leading to androgen deficiency that may manifest as low libido, impotence, erectile dysfunction, amenorrhea, or infertility. The causal role of opioids in the clinical syndrome of hypogonadism is unknown because the various medical, physical, lifestyle, and psychological stressors that may influence gonadal hormone levels have not been adequately controlled for in studies conducted to date. Patients presenting with symptoms of androgen deficiency should undergo laboratory evaluation.
Infertility: Chronic use of opioids may cause reduced fertility in females and males of reproductive potential. It is not known whether these effects on fertility are reversible.
Drug Interactions
Codeine is indicated in patients older than 12 years of age for the treatment of acute moderate pain which is not considered to be relieved by other analgesics such as Paracetamol or Ibuprofen (alone).
Benzodiazepines: Due to additive pharmacologic effect, the concomitant use of opioids with benzodiazepines increases the risk of respiratory depression, profound sedation, coma and death.
The concomitant use of opioids and benzodiazepines increases the risk of respiratory depression because of actions at different receptor sites in the central nervous system that control respiration. Opioids interact primarily at μ-receptors, and benzodiazepines interact at GABAA sites. When opioids and benzodiazepines are combined, the potential for benzodiazepines to significantly worsen opioid-related respiratory depression exists.
Reserve concomitant prescribing of these drugs for use in patients for whom alternative treatment options are inadequate (See Precautions).
Limit dosage and duration of concomitant use of benzodiazepines and opioids, and follow patients closely for respiratory depression and sedation.
Serotonergic Drugs: The concomitant use of opioids with other drugs that affect the serotonergic neurotransmitter system has resulted in serotonin syndrome. If concomitant use is warranted, carefully observe the patient, particularly during treatment initiation and dose adjustment. Discontinue Paralgin/Paralgin Forte if serotonin syndrome is suspected. Examples of serotonergic drugs are selective serotonin reuptake inhibitors (SSRIs), serotonin and norepinephrine reuptake inhibitors (SNRIs), tricyclic antidepressants (TCAs), triptants, 5-HT3 receptor antagonists, drugs that affect the serotonin neurotransmitter system (e.g. mirtazapine, trazodone, tramadol), monoamine oxidase (MAO) inhibitors (those intended to treat psychiatric disorders and also others, such as linezolid and intravenous methylene blue) (See Precautions.)
Storage
Store in a dry place at below 30°C protect from direct light and humidity.
Shelf-Life: Paralgin - 3 years.
Paralgin Forte - 4 years.
ATC Classification
N02AJ06 - codeine and paracetamol ; Belongs to the class of opioids in combination with other non-opioid analgesics. Used to relieve pain.
Presentation/Packing
Paralgin tab (white, round convex, 13mm diameter, inscribed with "SL" on one side) 100 x 10's. Paralgin Forte tab (white, round convex, 12mm diameter inscribed with "SL" on one side and breakline on the other) 2 x 15's, 60 x 15's.
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