Active ingredients: Buprenorphine (Buprenorphine hydrochloride)
TEMGESIC 0.2 mg sublingual tablets
Temgesic package inserts are available for pack sizes:- TEMGESIC 0.2 mg sublingual tablets
- TEMGESIC 0.3 mg / ml solution for injection
Why is Temgesic used? What is it for?
Temgesic sublingual tablets contain buprenorphine which belongs to a group of medicines called analgesics, used for the treatment of acute and chronic pain of medium to high intensity of various origins and types.
Contraindications When Temgesic should not be used
Do not take Temgesic
- if you are allergic to buprenorphine or any of the other ingredients of this medicine (listed in section 6);
- if you suffer from severe breathing problems (respiratory failure);
- if you have severe liver problems (liver failure);
- if you have severe kidney problems (kidney failure) if you have "alcohol intoxication" if you suffer from tremor and delirium due to alcohol withdrawal (delirium tremens);
- in case of simultaneous treatment with antidepressant drugs (anti MAO);
- in case of increased intracranial pressure (intracranial hypertension);
- in the case of children under the age of 12;
- while breastfeeding.
Precautions for use What you need to know before taking Temgesic
Talk to your doctor or pharmacist before taking Temgesic.
Take Temgesic with caution:
- in case of breathing problems (for example chronic obstructive pulmonary disease, asthma, cor pulmonale (enlargement of a part of the heart due to lung disease), reduced respiratory reserve (reduction in the amount of air in the lungs) hypoxia (lack of oxygen), hypercapnia (increased concentration of carbon dioxide in the blood), pre-existing respiratory depression, deviations of the spine which can lead to dyspnoea (difficulty in breathing);
- in case of reduced normal liver function;
- in case of reduced normal function of the kidneys;
- in case of dysfunction of a part of the liver (biliary tract);
- in case of head trauma, intracranial injury or in other brain diseases in which the pressure of the fluid surrounding the brain (cerebrospinal) may be increased or in case of a history of seizures. Temgesic can cause narrowing of the pupil (miosis) and changes in the level of consciousness or in the perception of painful symptoms that would contribute to confusing the diagnosis or hiding the evolution of some pathologies in progress;
- in case of acute abdominal conditions.
Particular caution is advised if you are on ongoing therapy or if you have recently taken medicines with central nervous / respiratory system depressant effects (see "Other medicines and Temgesic")
Central nervous system depression
Buprenorphine can cause an increase in central nervous system depression when taken simultaneously with:
- other medicines used to treat pain (analgesic opioids);
- general anesthetics;
- medicines used to treat symptoms caused by allergic reactions (antihistamines);
- other central nervous system depressants (such as alcohol, benzodiazepines, phenothiazines, tranquilizers, sedatives or hypnotics).
Dependence
After prolonged use it is not recommended to stop treatment abruptly, as it can cause a withdrawal syndrome which can occur later.
Use in opioid-dependent patients
Buprenorphine can cause withdrawal symptoms in opioid-dependent patients who use heroin or who are being treated with addiction medications, such as methadone.
Cardiac pathologies
Like other opioids, buprenorphine can cause a sharp drop in blood pressure upon standing up when transitioning from a sitting or lying position (orthostatic hypotension).
Other warnings for the opioid class
Take buprenorphine with caution if you have:
- elderly or debilitated patients;
- thyroid gland problems (myxedema) or hypothyroidism (reduced thyroid function);
- adrenal gland disorders (eg Addison's disease);
- central nervous system depression or coma;
- psychosis due to drug intoxication or hallucinogens;
- urinary tract problems, especially if related to enlarged prostate (prostatic hypertrophy) or narrowing of the urethra (urethral stricture);
- problems with the biliary tract.
For those who carry out sporting activities: The use of the drug without therapeutic necessity constitutes doping and can in any case determine positive anti-doping tests.
Children and adolescents
Do not give Temgesic to children under the age of 12.
Interactions Which drugs or foods may change the effect of Temgesic
Tell your doctor or pharmacist if you are taking, have recently taken or might take any other medicines.
Take Temgesic with caution with the following medicines:
- Benzodiazepines: (used to treat anxiety or sleep disorders): because this association can cause death due to the consequent inability to breathe (central respiratory depression). Consider the extreme danger linked to the "self-administration of benzodiazepines not prescribed during" taking this medicine. The use of benzodiazepines together with this medicine should only be done as directed by your doctor.
- Other medicines which can induce sleepiness and which are used to treat anxiety, problems falling asleep, seizures, pain: because these medicines reduce the level of alertness making it dangerous to drive and use machines. They can also cause central nervous system depression, a very serious condition. Below is an example list of these drugs:
- Other opium-derived medicines (for example: methadone, analgesics)
- Some anesthetics
- Some tranquilizers
- Sedative hypnotics
- Some cough suppressants
- Some antidepressants
- Sedatives antagonists of histamine H1 receptors (used to treat allergic reactions)
- Barbiturates (used to promote sleep or sedation)
- Anxiolytics (used for anxiety) other than benzodiazepines
- Neuroleptics (drugs used to treat psychosis)
- Clonidine (drug used for blood pressure) and similar substances
- Naltrexone (medicine used for opioid addiction): because it can prevent the effects of buprenorphine. When combined with naltrexone, pain treatment with buprenorphine may not be adequate. In addition, naltrexone may trigger the sudden onset of opioid withdrawal symptoms in patients who have developed physical dependence on buprenorphine.
- Other pain relievers (opioid analgesics): The pain relieving effect of these drugs may decrease in patients treated with buprenorphine. In opioid-dependent patients, treatment with buprenorphine may trigger withdrawal symptoms (see also "Warnings and precautions").
- Antiretrovirals (used to treat AIDS), antibiotics (macrolides), antifungals (azoles: used to treat fungal infections), gestodene (used as a contraceptive), OTA (oral anticoagulant therapy, used to prevent or slow blood clotting ) because they can enhance the effects of Temgesic.
- Phenobarbital, carbamazepine, phenytoin (medicines to treat epilepsy) and rifampicin (medicines to treat tuberculosis): they can reduce the effect of buprenorphine.
- Antidepressants: Monoamine oxidase inhibitors (MAOIs) as they can cause increased effects of other opiates. Avoid taking Temgesic at the same time and for two weeks after stopping treatment with antidepressants (MAOIs).
- Halothane (a general anesthetic) and other medicines that reduce the elimination of buprenorphine through the liver: they can increase the effects of Temgesic.
Temgesic and alcohol
Temgesic should not be taken with alcoholic beverages and should be used with caution with alcohol-containing medicines as alcohol increases the sedative effect of buprenorphine (see "Driving and using machines").
Warnings It is important to know that:
Pregnancy and breastfeeding
If you are pregnant or breast-feeding, think you may be pregnant or are planning to have a baby, ask your doctor or pharmacist for advice before taking this medicine.
Pregnancy
Towards the end of pregnancy, high doses of buprenorphine can induce respiratory problems (respiratory depression) in the newborn even after a short period of administration. Prolonged administration of buprenorphine during the last three months of pregnancy can cause withdrawal syndrome in the newborn. The syndrome usually occurs several hours to several days after birth.
Feeding time
Buprenorphine and its metabolic products are excreted in breast milk: buprenorphine should not be used in breastfeeding women (see "Do not take Temgesic").
Driving and using machines
Caution is advised when driving and using machines (see "Other medicines and Temgesic").
Low doses of buprenorphine can cause drowsiness. This effect may be increased when buprenorphine is taken together with alcohol or drugs that affect the central nervous system (see "Other medicines and Temgesic").
Temgesic sublingual tablets contain lactose
This medicinal product contains lactose. If you have been told by your doctor that you have an intolerance to some sugars, contact your doctor before taking this medicinal product.
Dosage and method of use How to use Temgesic: Dosage
Always take this medicine exactly as your doctor or pharmacist has told you. If in doubt, consult your doctor or pharmacist.
Sublingual tablets
The recommended dose is 1-2 tablets (0.2-0.4 mg buprenorphine) to be dissolved under the tongue, every 6-8 hours, or as needed.
Do not chew or swallow the tablets.
If you stop taking Temgesic
It is advisable not to stop treatment abruptly, as it can cause a withdrawal syndrome which can occur later.
If you have any further questions on the use of this medicine, ask your doctor or pharmacist.
Overdose What to do if you have taken too much Temgesic
If you take more Temgesic than you should
Symptoms
If you have taken too much Temgesic this can cause:
- narrowing of the pupil (miosis)
- sedation
- low blood pressure (hypotension)
- sudden drop in blood pressure (cardiovascular collapse)
- severe respiratory problem (respiratory depression) which can progress to "interruption of" respiratory activity (respiratory arrest) with the risk of death
- nausea
- He retched
The main symptoms requiring intervention are respiratory depression, which can progress to respiratory arrest and death, and vomiting.
Treatment
In the event of an overdose, your doctor may give you naloxone (a substance used to counter the effects of opioid overdose) if necessary.
Side Effects What are the side effects of Temgesic
Like all medicines, this medicine can cause side effects, although not everybody gets them.
Below is a summary of the side effects:
Very common side effects (may affect more than 1 in 10 people) include:
- Sedation
- Dizziness
- Nausea
Common side effects (may affect more than 1 in 100 people) include:
- Headache (headache)
- Narrowing of the pupil (miosis)
- Low blood pressure (hypotension)
- Decrease in the amount of air circulating in the lungs (hypoventilation)
- He retched
- Confusion
- Dependence on the drug
- Hallucinations
- Drowsiness
- Dizziness
- Severe breathing problem (respiratory depression)
- Itching
- Rash
- Excessive sweating (hyperhidrosis)
- Lack of efficacy of the drug
- Interactions with other drugs
- Fatigue
Uncommon side effects (may affect more than 1 in 1,000 people) include:
- Euphoria
- Nervousness
- Depression
- Psychotic disorders
- Feeling detached from your body (depersonalization)
- Speech joint disorder (dysarthria)
- Altered feeling in the limbs (paraesthesia)
- Coma
- Tremor
- Blurred vision, double vision (diplopia), visual impairment, inflammation of the conjunctiva (conjunctivitis)
- Ringing in the ears (tinnitus)
- Faster heart beat (tachycardia), decreased heart rate (bradycardia)
- Bluish discoloration of the skin due to insufficient oxygenation of the blood (Cyanosis)
- Heart problems (Wenckebach block, second degree atrioventricular block)
- High blood pressure (hypertension)
- Pallor
- Difficulty in breathing (dyspnea), stopped breathing (apnea)
- Dry mouth (dry mouth), constipation, stomach discomfort (dyspepsia), accumulation of gas in the intestine (flatulence)
- Inability of the bladder to empty (urinary retention)
- Weakness (asthenia)
- Malaise
Rare side effects (may affect more than 1 in 10,000 people) include:
- Allergy (hypersensitivity)
- Loss, reduction of appetite
- Change in mood (dysphoria), agitation
- Convulsions
- Abnormal coordination
- Difficulty falling asleep (insomnia)
- Diarrhea
- Urticaria
- Fainting
Side effects of unknown frequency include:
- Severe allergic reaction which appears rapidly (anaphylactic shock)
- Constriction of the bronchi (bronchospasm)
- Sudden swelling of the skin (angioneurotic edema)
Reporting of side effects
If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet. Side effects can also be reported directly via the national reporting system at www.agenziafarmaco.gov.it/it/responsabili. By reporting side effects you can help provide more information on the safety of this medicine.
Expiry and Retention
Sublingual tablets in PVC / PVDC / Al blisters: Do not store above 25 ° C. Store in the original packaging.
Sublingual tablets in Nylon / Al / PVC blisters: Do not store above 30 ° C. Store in the original packaging.
Keep this medicine out of the sight and reach of children.
Do not take this medicine after the expiry date which is stated on the package. The expiry date refers to the last day of that month.
Do not throw any medicines via wastewater or household waste. Ask your pharmacist how to throw away medicines you no longer use. This will help protect the environment.
Deadline "> Other information
What Temgesic contains
Temgesic 0.2 mg sublingual tablets
The active ingredient is: buprenorphine hydrochloride. One sublingual tablet contains 0.216 mg buprenorphine hydrochloride (equivalent to 0.2 mg buprenorphine base).
The other ingredients are: lactose, maize starch, mannitol, povidone, anhydrous citric acid, anhydrous sodium citrate, magnesium stearate.
Description of what Temgesic looks like and contents of the pack
Temgesic 0.2 mg sublingual tablets
10 sublingual tablets packed in PVC / PVDC / Al blisters.
10 sublingual tablets packed in Nylon / Al / PVC blisters.
Source Package Leaflet: AIFA (Italian Medicines Agency). Content published in January 2016. The information present may not be up-to-date.
To have access to the most up-to-date version, it is advisable to access the AIFA (Italian Medicines Agency) website. Disclaimer and useful information.
01.0 NAME OF THE MEDICINAL PRODUCT -
TEMGESIC
02.0 QUALITATIVE AND QUANTITATIVE COMPOSITION -
TEMGESIC 0.2 mg sublingual tablets
One sublingual tablet contains:
active ingredient: 0.216 mg buprenorphine hydrochloride (equivalent to 0.2 mg buprenorphine base).
Excipients with known effects: lactose 29.842 mg.
TEMGESIC 0.3 mg / ml solution for injection
One ml of solution for injection contains:
active ingredient: buprenorphine hydrochloride 0.324 mg (equivalent to buprenorphine base 0.3 mg).
For the full list of excipients, see section 6.1.
03.0 PHARMACEUTICAL FORM -
Sublingual tablet and solution for injection.
04.0 CLINICAL INFORMATION -
04.1 Therapeutic indications -
Solution injectable
Treatment of acute and chronic pain of high intensity of different origin and type.
Sublingual tablets
Treatment of acute and chronic pain of medium-high intensity of different origin and type.
04.2 Posology and method of administration -
Dosage
Injectable solution
1-2 ampoules (0.3-0.6 mg of buprenorphine), intramuscularly or slowly intravenously, every 6-8 hours or as needed.
Sublingual tablets
1-2 tablets (0.2-0.4 mg of buprenorphine), to be dissolved under the tongue, every 6-8 hours, or as needed. Do not chew or swallow the tablets.
Pediatric population
Temgesic is contraindicated in children below 12 years of age (see section 4.3).
Patients with hepatic impairment
Since the pharmacokinetics of buprenorphine may be altered in patients with hepatic impairment, lower starting doses and "careful dose titration in patients with hepatic impairment may be necessary (see section 4.4).
04.3 Contraindications -
Hypersensitivity to the active substance or to any of the excipients listed in section 6.1.
Severe respiratory failure, severe liver failure, severe renal failure; acute alcoholism or delirium tremens; concomitant treatment with anti-MAO (see section 4.5); intracranial hypertension; children under 12 years of age (see section 4.2); breastfeeding (see section 4.6).
04.4 Special warnings and appropriate precautions for use -
Respiratory depression
Although respiratory depression may occur at doses above the recommended therapeutic range, in some circumstances doses in the recommended therapeutic range may produce clinically significant respiratory depression.
Buprenorphine should be used with caution in patients with impaired respiratory function (e.g., chronic obstructive pulmonary disease, asthma, cor pulmonale, reduced respiratory reserve, hypoxia, hypercapnia or pre-existing respiratory depression, kyphoscoliosis, or spinal deviations which may lead to dyspnea).
Particular caution is advised when administering buprenorphine to patients on therapy or who have recently undergone treatment with drugs with central nervous / respiratory depressant effects (see section 4.5).
Patients presenting with the physical and / or pharmacological risk factors described above should be monitored and a dose reduction may be considered.
Central nervous system depression
Concomitant use of buprenorphine with other opioid analgesics, general anesthetics, antihistamines, benzodiazepines, phenothiazines, other tranquilizers, sedatives / hypnotics or other central nervous system depressant drugs (including alcohol) may result in increased central nervous system depression (see section 4.5).
When such combination therapy is envisaged, it is particularly important that the dose of one or both drugs be reduced.
Dependence
Buprenorphine is a partial agonist that binds to µ (mu) -opioid receptors and chronic administration produces opioid-type addiction. Animal studies as well as clinical experience have shown that buprenorphine can be addictive, but at a lower level than a full agonist (eg morphine).
Following chronic use, abrupt discontinuation of treatment is not recommended, as it may cause a withdrawal syndrome whose onset may be delayed.
In sensitive patients, addiction can lead to self-administration of the drug even in the absence of pain.
Use in opioid-dependent patients
Buprenorphine-based analgesic products may induce withdrawal symptoms in opioid-dependent patients undergoing treatment with complete opioid agonists such as methadone or using heroin.
Similarly, buprenorphine as an analgesic should be prescribed with caution to persons known to abuse drugs or to patients with a history of opioid dependence. Prior to treatment with buprenorphine-based analgesic drugs in patients with a history of opioid abuse or misuse, the level of opioid dependence should be assessed (see section 4.5).
Hepatic impairment
Elevated plasma levels of buprenorphine have been found in patients with moderate and severe hepatic impairment. Patients should be monitored for signs and symptoms of toxicity or overdose caused by increased buprenorphine levels (see section 4.2). TEMGESIC should be used with caution in patients with moderate hepatic impairment. In patients with severe impairment. hepatic use of buprenorphine is contraindicated (see section 4.3).
Renal impairment
30% of the administered dose is eliminated by the kidney. The metabolites of buprenorphine accumulate in patients with renal impairment. Caution is recommended in dosing in patients with renal impairment.
Biliary tract dysfunction
Buprenorphine has been found to increase intracoledocal pressure in a similar manner to other opioid analgesics; therefore it should be administered with caution in patients suffering from biliary tract dysfunction.
Use in outpatients
Buprenorphine may impair the mental or physical abilities required for carrying out potentially hazardous activities such as driving vehicles or using machines. Patients should be properly informed (see section 4.7).
Cardiovascular effects
As with other opioids, buprenorphine can induce orthostatic hypotension.
Head trauma and increased intracranial pressure
Buprenorphine, like other potent opioids, can increase CSF pressure and should therefore be used with caution in patients with head injury, intracranial injury, and other conditions where CSF pressure may be increased or if there is a history of seizures. convulsive.
As with other mu-opioid receptor agonists, buprenorphine can induce myosis and changes in the level of consciousness or pain perception as a symptom of a disease, which can interfere with patient assessment, confuse the diagnosis or hide the clinical course of disease. concomitants.
Acute abdominal conditions
As with other mu-opioid receptor agonists, administration of buprenorphine may confound the diagnosis or clinical course of patients with acute abdominal conditions.
Other warnings for the opioid class
Buprenorphine should be administered with caution in elderly or debilitated patients or in patients with the following conditions:
- myxedema or hypothyroidism
- adrenocortical insufficiency (for example, Addison's disease)
- CNS depression or coma
- toxic psychosis
- prostatic hypertrophy or urethral stricture
- biliary tract dysfunction
Important information about some of the excipients
The sublingual tablets contain lactose. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency, or glucose-galactose malabsorption should not take this medicine.
04.5 Interactions with other medicinal products and other forms of interaction -
Benzodiazepines
The combination of buprenorphine and benzodiazepines may increase respiratory depression of central origin with possible fatal outcome. There have been reports of deaths and coma when buprenorphine was used in combination with benzodiazepines or when buprenorphine was taken improperly for intravenously in combination with benzodiazepines.
Cases of respiratory and cardiovascular collapse have been reported in patients receiving therapeutic doses of diazepam and analgesic doses of buprenorphine; consequently, the dosage should be limited and this combination should be avoided especially in cases where there is a risk of misuse. Patients should use benzodiazepines together with this medicinal product only as prescribed (see section 4.4).
Alcohol
Buprenorphine should not be taken with alcoholic beverages or medicines containing alcohol. Alcohol increases the sedative effect of buprenorphine (see section 4.7).
Other central nervous system depressants
The combination of buprenorphine and other central nervous system depressant medicinal products increases central nervous system depression. The reduced level of alertness can make driving and use of machines dangerous (see section 4.7). Examples of central nervous system depressants include other opium derivatives (e.g. methadone, analgesics), anesthetics, phenothiazines, other tranquilizers, sedative hypnotics, cough suppressants, some antidepressants, sedatives, H1 receptor antagonists, barbiturates, anxiolytics other than benzodiazepines, neuroleptics, clonidine and related substances.
Naltrexone
Naltrexone is an opioid antagonist capable of antagonizing the pharmacological effects of buprenorphine. Patients treated with naltrexone may not achieve adequate analgesic effect with buprenorphine. Patients who have developed physical dependence on buprenorphine may experience sudden onset of opioid withdrawal symptoms.
Other opioid analgesics
The analgesic effects of a complete opioid agonist may be diminished by competition from the partial agonist buprenorphine. Adequate analgesia may be difficult to achieve when a complete opioid agonist is administered to patients treated with buprenorphine. For patients who have developed addiction to complete opioid agonists, administration of the partial agonist buprenorphine may trigger withdrawal symptoms (see also section 4.4 "Use in opioid dependent patients"). There is a possible risk with the use of a complete opioid agonist. of overdose especially when trying to counteract the effects of the partial agonist buprenorphine or when plasma levels of buprenorphine are decreasing.
CYP3A4 inhibitors
An interaction study of buprenorphine with ketoconazole (a potent CYP3A4 inhibitor), showed an increase in the Cmax and AUC (area under the curve) of buprenorphine (approximately 50% and 70% respectively) and to a lesser extent , of norbuprenorphine. Patients receiving Temgesic should be closely monitored and dose reduction may be required when co-administered with potent CYP3A4 inhibitors (e.g. HIV protease inhibitors, azole antifungals such as ketoconazole or itraconazole, antibiotics macrolides, gestodene, TAO).
CYP3A4 inducers
Concomitant use of CYP3A4 inducers and buprenorphine may reduce plasma concentrations of buprenorphine, potentially resulting in suboptimal treatment. Patients on buprenorphine should be carefully monitored if such inducers (eg, phenobarbital) are administered concomitantly. , carbamazepine, phenytoin, rifampicin) The dose of buprenorphine or the CYP3A4 inducer may need to be adjusted accordingly.
Monoamine oxidase inhibitors (MAOIs)
Based on experience with morphine, concomitant use of MAOIs with buprenorphine may exacerbate the effect of opioids. Avoid concomitant administration and within two weeks of stopping MAO treatment (see section 4.3).
Other interactions
Halothane is known to decrease hepatic elimination. Since hepatic elimination plays an important role in the overall elimination of buprenorphine (≥ 70%), lower starting doses and careful dose titration may be required in the concomitant use of halothane and medicinal products that reduce hepatic clearance. .
04.6 Pregnancy and breastfeeding -
Pregnancy
There are no adequate and well-controlled studies in pregnant women. Animal studies have shown reproductive toxicity (see section 5.3).
Products containing low doses of buprenorphine should only be used during pregnancy if the possible benefits outweigh the potential risks to the fetus.
Towards the end of pregnancy, high doses of buprenorphine can induce respiratory depression in the newborn even after a short period of administration. Prolonged administration of buprenorphine during the last three months of pregnancy may cause withdrawal syndrome in the newborn (eg, hypertonia, neonatal tremor, neonatal agitation, myoclonus or convulsions). The syndrome usually occurs several hours to several days after birth.
Due to the long half-life of buprenorphine, neonatal monitoring for several days at the end of pregnancy should be considered to prevent the risk of respiratory depression or withdrawal syndrome in neonates.
Feeding time
Since buprenorphine and its metabolites are excreted in breast milk, buprenorphine should not be used in lactating women (see section 4.3).
04.7 Effects on ability to drive and use machines -
Low doses of buprenorphine can cause drowsiness. This effect is likely to be more pronounced when buprenorphine is taken together with alcohol or drugs that exert a depressive action on the central nervous system (see section 4.5). Caution is advised when driving vehicles and using machinery.
04.8 Undesirable effects -
Data derived from clinical studies
Summary of the safety profile
The most frequently reported adverse reactions during clinical trials were sedation, dizziness, dizziness and nausea.
Tabulated list of adverse reactions
Table I summarizes the adverse reactions reported in clinical trials. The frequency of possible side effects listed below is defined using the following convention: Very common (≥1 / 10), Common (≥1 / 100,
Adverse drug reactions are presented by MedDRA system organ class, in internationally agreed order based on preferred term and frequency of reporting.
Post-marketing data
Tabulated list of adverse reactions
Below is a list of the most commonly reported adverse reactions during post-marketing surveillance. This includes events occurring in at least 1% of reports from healthcare professionals and considered to be expected.
These adverse drug reactions are presented according to the MedDRA system organ class, in the internationally agreed order of the preferred term.
* Events with unknown frequency of post-marketing reports, however these events are included in Table 2 based on the severity of the manifestations.
Reporting of suspected adverse reactions
Reporting of suspected adverse reactions occurring after authorization of the medicinal product is important as it allows continuous monitoring of the benefit / risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the national reporting system. "address www.agenziafarmaco.gov.it/it/responsabili.
04.9 Overdose -
Symptoms
Manifestations of acute overdose include miosis, sedation, hypotension, cardiovascular collapse, respiratory depression, and death. Nausea and vomiting may be observed.
The main symptoms requiring intervention are respiratory depression which can progress to respiratory arrest and death, and vomiting.
Treatment
In the event of an overdose, general emergency measures should be instituted paying particular attention to the patient's respiratory and cardiac status.
Symptomatic treatment of respiratory depression should be carried out by implementing general resuscitation measures. Patent airways and assisted or controlled ventilation must be ensured. The patient must be transferred to an environment equipped with a resuscitation facility. If the patient vomits, care should be taken to prevent aspiration of the vomitus.
The use of an opioid antagonist (eg naloxone) is recommended despite the modest effect it may have in counteracting the respiratory symptoms of buprenorphine compared to that exerted against complete opioid agonists.
Naloxone may not be effective in resolving the respiratory depression produced by buprenorphine; therefore, the primary management of overdose should be to re-establish adequate ventilation, through mechanical ventilation, if necessary.
Naloxone can be cleared more rapidly than buprenorphine, resulting in the return of previously controlled buprenorphine overdose symptoms.
The long duration of action of buprenorphine should be taken into account in determining the duration of treatment needed to counter the effects of an overdose.
05.0 PHARMACOLOGICAL PROPERTIES -
05.1 "Pharmacodynamic properties -
Pharmacotherapeutic group:
analgesics, opioids, oripavine derivatives.
ATC code: N02AE01.
The active ingredient of Temgesic is buprenorphine hydrochloride, a recently synthesized central analgesic, with partial agonist-antagonist characteristics. Temgesic represents an original drug, with high analgesic power, prolonged duration of action and low risk of creating addiction. The drug is therefore a valid alternative to morphine and other opioid analgesics in the treatment of acute and chronic pain of various types and etiology and of medium-high intensity.
The onset of the analgesic effect is evident 10-15 min after intravenous administration, while intramuscular or sublingual action appears after about 20 min. The effect lasts for about 6-8 hours.
The sublingual route is of choice in the therapy of chronic pain.
The results obtained in numerous clinical studies testify to the good tolerability of Temgesic at the recommended doses and its wide therapeutic margin.
05.2 "Pharmacokinetic properties -
Buprenorphine is rapidly absorbed after both oral and parenteral administration.
Peak plasma is reached after approximately 6 min for intramuscular administration and approximately 2 hours after oral (sublingual) administration.
The half-life t½ varies from 1 to 3 hours after intramuscular or intravenous administration.
In vitro studies with human plasma proteins have shown a high protein binding (about 96%), especially to alpha and beta-globulin fractions.
05.3 Preclinical safety data -
Acute toxicity (LD50)
mouse (M) i.v. 24 mg / kg; (F) 29 mg / kg; mouse (M) i.p. 135 mg / kg; (F) 110 mg / kg; mouse i.m> 600 mg / kg; mouse s.c. > 600 mg / kg; mouse (M) os 260 mg / kg; rat (M) i.v. 38 mg / kg; rat (M) i.p. 197 mg / kg; (F) 207 mg / kg; rat (M) os> 600 mg / kg; rat (F) s.c. > 600 mg / kg.
DLM: rabbit i.v. 75 mg / kg.
Toxicity for prolonged administration
rat W i.m., 6 months; olive baboon, 6 months - 5 mg / kg / day
no toxic effects reported related to the drug
Teratogenesis
rat SD i.m. and s.c .; rabbit DB i.m. and s.c.
no teratogenic or foetotoxic effects observed up to a dose of 5 mg / kg / day
Mutagenic activity: absent both in vitro and in vivo.
06.0 PHARMACEUTICAL INFORMATION -
06.1 Excipients -
Sublingual tablets
lactose, corn starch, mannitol, povidone, anhydrous citric acid, anhydrous sodium citrate, magnesium stearate.
Solution injectable
glucose monohydrate, water for injections.
06.2 Incompatibility "-
None known.
06.3 Period of validity "-
Sublingual tablets in PVC / PVDC / Al blisters: 1 year.
Sublingual tablets in Nylon / Al / PVC blister and solution for injection: 3 years.
06.4 Special precautions for storage -
Sublingual tablets in PVC / PVDC / Al blisters:
Do not store above 25 ° C. Store in the original package.
Sublingual tablets in Nylon / Al / PVC blister packs:
Do not store above 30 ° C. Store in the original package.
Injectable solution:
Do not store above 30 ° C. Store in the original package in order to protect from light.
06.5 Nature of the immediate packaging and contents of the package -
The clear glass vials are packaged in a PVC box and inserted together with the package leaflet in a lithographed cardboard box.
Pack of 5 ampoules of 1 ml.
The tablets are packaged in opaque PVC / PVDC / Al blister or Nylon / Al / PVC blister, which is inserted together with the package leaflet in a lithographed cardboard box.
Packs of 10 tablets of 0.2 mg.
Not all pack sizes may be marketed.
06.6 Instructions for use and handling -
No special instructions.
07.0 HOLDER OF THE "MARKETING AUTHORIZATION" -
Indivior UK Limited
103-105 Bath Road
Slough - Berkshire
SL1 3UH United Kingdom
08.0 MARKETING AUTHORIZATION NUMBER -
TEMGESIC 0.2 mg sublingual tablets in PVC / PVDC / Al blisters AIC: 025215029
TEMGESIC 0.2 mg sublingual tablets in Nylon / Al / PVC blisters AIC: 025215043
TEMGESIC 0.3mg / ml solution for injection AIC: 025215017
09.0 DATE OF FIRST AUTHORIZATION OR RENEWAL OF THE AUTHORIZATION -
Date of first authorization: 03 May 1984
Date of most recent renewal: 01 June 2010
10.0 DATE OF REVISION OF THE TEXT -
AIFA Determination of 21 December 2015
