Active ingredients: Etizolam
DEPAS 0.5 mg film-coated tablets
DEPAS 1 mg film-coated tablets
DEPAS 0.5 mg / ml oral drops, solution
Why is Depas used? What is it for?
DEPAS is a medicine that contains etizolam, an active ingredient belonging to the benzodiazepine class, drugs that reduce anxiety and help sleep. Benzodiazepines are usually used for severe disorders, which cause severe discomfort or prevent normal activities. daily.
DEPAS is used to treat:
- states of anxiety, which can manifest themselves with rapid heartbeat and agitation, difficulty concentrating or memory lapses, sleep disturbances, sweating, tremors;
- insomnia, a condition in which it is difficult to fall asleep or to maintain adequate sleep.
Contraindications When Depas should not be used
Do not take DEPAS if:
- you are allergic to the active substance or to other medicines belonging to the same class (benzodiazepines) or to any of the other ingredients of this medicine (listed in section 6);
- have severe breathing problems;
- suffer from sleep apnea syndrome (pauses in breathing during sleep);
- suffer from myasthenia gravis, a disease characterized by muscle weakness and fatigue;
- has closed-angle glaucoma, a disease characterized by an increase in pressure inside the eye with possible worsening of vision;
- have severe liver problems.
Precautions for use What you need to know before taking Depas
Talk to your doctor or pharmacist before taking DEPAS if:
- have or have had drug or alcohol addictions;
- have kidney problems;
- have liver problems;
- have had psychiatric disorders or have brain diseases;
- suffer from depression;
- have suicidal thoughts;
- have breathing difficulties;
- have heart problems;
- have reduced muscle tone (hypotonia);
- you are elderly, as this medicine can cause coordination disturbances, increasing the risk of falls.
Other information
- Mental side effects - contact your doctor if you experience side effects such as agitation, irritability, restlessness, aggression, disappointment, anger, nightmares, hallucinations, changes in behavior. These side effects are more likely in children and the elderly.
- Amnesia (total or partial memory loss) - while on DEPAS therapy, you may have difficulty remembering recent episodes or memorizing new information (anterograde amnesia), especially after a few hours of taking the medicine. To reduce this risk, take DEPAS immediately before going to sleep.
- Tolerance - During treatment with DEPAS, you may notice a reduction in the efficacy or duration of the tranquilizing / soporific effect. If this happens, contact your doctor who will assess the need to change your therapy. Do not increase the dose of DEPAS without consulting your doctor, as the use of high doses may cause dependence on the drug (see section 3 - "WARNING").
- Dependence - during therapy with DEPAS, you may develop physical and psychological dependence on this medicine, i.e. the need to use it in increasingly higher doses (tolerance) and regardless of its real need. The risk of dependence increases with increasing dose and duration of treatment, or if you have been addicted to drugs or alcohol. For this reason, DEPAS therapy should be as short as possible (see section 3 - "WARNING"). .
- Withdrawal syndrome - if you have developed addiction and suddenly stop DEPAS therapy or reduce the dose too quickly, withdrawal symptoms such as headache, muscle pain, anxiety, tension, restlessness, confusion and irritability may occur . In severe cases, the following may occur: sensation of perceiving the outside world or oneself in an altered way (derealization and depersonalization), numbness and tingling of the extremities, increased sensitivity to light, noise, sounds and physical contact, hallucinations or epileptic seizures . If this occurs, please contact your doctor (see section 3 - "if you stop taking DEPAS").
- Rebound symptoms - DEPAS treatment should be discontinued gradually, with a progressive decrease in dose. Abrupt discontinuation of therapy may cause the symptoms (insomnia or anxiety) for which you started therapy to return or worsen (see section 3 - "If you stop taking DEPAS").
Children and adolescents
In children and adolescents less than 18 years of age, DEPAS should not be used
Interactions Which drugs or foods can modify the effect of Depas
Tell your doctor or pharmacist if you are taking, have recently taken or might take any other medicines, as some medicines can interact with DEPAS or increase the risk of adverse events, even serious ones. In particular, contact your doctor before taking DEPAS if you are using:
- drugs that act on the nervous system, such as antipsychotics, sedatives, anxiolytics, hypnotics, anesthetics, sedative antihistamines, narcotic analgesics;
- drugs used for depression (antidepressants) such as fluvoxamine maleate or MAOIs;
- drugs used against epilepsies (antiepileptics);
as these medicines can change the effect of DEPAS.
DEPAS with alcohol
Do not take alcohol or medicines that contain alcohol while taking this medicine, as this may worsen some nervous system side effects (e.g. sedation, sleepiness).
Warnings It is important to know that:
Pregnancy and breastfeeding
Do not take DEPAS if you are pregnant or breastfeeding, unless your doctor tells you to.
If you suspect or are planning to become pregnant, ask your doctor for advice before taking this medicine.
Driving and using machines
DEPAS can cause sedation, memory loss, impaired muscle concentration and function. Take special care before driving or using machines.
DEPAS drops contain ethanol
This medicine contains 8 vol% ethanol (alcohol), eg. up to 252 mg per maximum dose (80 drops), equivalent to 6.4 ml of beer, 2.7 ml of wine per dose. It can be harmful to alcoholics.
To be taken into consideration in pregnant or lactating women, children and high-risk groups such as people with liver disease or epilepsy.
For those who carry out sporting activities, the use of medicines containing ethanol can determine positive doping tests in relation to the alcohol concentration limits indicated by some sports federations.
DEPAS tablets contain 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.
Dose, Method and Time of Administration How to use Depas: Posology
Always take this medicine exactly as your doctor has told you. If in doubt, consult your doctor.
Your doctor will determine the correct dose and duration of treatment. based on the severity of your symptoms and your general condition (for example if you have liver, kidney, lung problems).
If you take DEPAS because you have anxiety
The usual dose is:
half or 1 tablet of 0.5 mg (equal to 0.25 - 0.5 mg), 2-3 times a day
or
10-20 drops (equal to 0.25 - 0.5 mg), 2-3 times a day.
In severe cases, your doctor will prescribe a higher dose:
1 tablet of 1 mg or 2 tablets of 0.5 mg, twice a day (once in the morning and once in the evening).
Your doctor will tell you which tablet or how many drops to use.
The duration of treatment should be as short as possible and should not exceed 8-12 weeks.
If you take DEPAS because you suffer from insomnia
The usual dose is:
1 or 2 tablets of 1 mg or 2 - 4 tablets of 0.5 mg (equal to 1 - 2 mg), in the evening before bedtime;
or
40-80 drops (equal to 1 - 2 mg), in the evening before going to bed.
Your doctor will tell you which tablet or how many drops to use.
The duration of treatment ranges from a few days to 2 weeks, up to a maximum of 4 weeks.
Senior citizens
The doctor will establish a lower dose than those indicated above, keeping within the limits of 1.5 mg per day.
WARNING: Contact your doctor if during treatment with DEPAS, you notice a reduction in the efficacy or duration of the tranquilizing / soporific effect (tolerance). Do not increase the dose of DEPAS without consulting your doctor, as the use of high doses of this medicine may cause dependence on the medicine (see section 2 - "Further information").
Method of administration
DEPAS tablets: take the tablets by mouth by swallowing them with a little water. DEPAS drops: take the drops diluting them in a little water. To open the bottle, press the cap and at the same time unscrew normally; to close the bottle, screw the cap back on completely.
If you forget to take DEPAS
Do not take a double dose to make up for a forgotten dose. Take the missed dose as soon as you remember and continue with your therapy as normal.
If you stop taking DEPAS
Do not stop treatment with DEPAS abruptly, as rebound symptoms or withdrawal symptoms may appear (see section 2 - "Further information"). When it is necessary to stop therapy, the doctor will gradually reduce the dose.
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 Depas
In case of accidental ingestion / intake of an overdose of DEPAS, notify your doctor immediately or go to the nearest hospital.
In the hospital you will be subjected to adequate intervention protocols.
If you take a dose of DEPAS higher than the therapeutic one, you may notice mental confusion with impaired senses (drowsiness) and lethargy. In severe cases, coordination disorders, low blood pressure (hypotension), muscle weakness (hypotonia), difficulty breathing or coma can occur. Excessive doses of this medicine can also cause death.
Side Effects What are the side effects of Depas
Like all medicines, this medicine can cause side effects, although not everybody gets them.
Stop taking DEPAS immediately and contact your doctor if you have:
- severe breathing difficulties with possible alteration of consciousness and mental state (carbon dioxide narcosis);
- fever, muscle stiffness, difficulty swallowing, increased heart rate (tachycardia), change in blood pressure, sweating, possible signs of Neuroleptic Malignant Syndrome;
- breathing difficulties, fever and cough, possible signs of pneumonia;
- muscle weakness and pain, increased creatine kinase and myoglobin in the blood and urine, possible signs of injury to the muscles (rhabdomyolysis);
- yellowing of the skin or eye (jaundice), changes in liver parameters such as increased bilirubin, increased transaminases, increased alkaline phosphatase.
Tell your doctor if you notice during DEPAS therapy:
- drowsiness, reduced emotions, decreased alertness, confusion, speech difficulties, fatigue, headache, dizziness;
- muscle weakness, loss of movement coordination (ataxia);
- thirst, nausea, stomach or bowel upset;
- more or less sudden onset of skin lesions (skin reactions), such as spot or diffuse color changes (rash, erythema);
- vision changes such as double vision, eye problems after exposure to light (photophobia), dry eyes, excessive blinking, persistent and involuntary closing of the eyelids (blepharospasm);
- changes in sex drive, enlarged breasts in men (gynecomastia);
- increased prolactin in the blood (hyperprolactinaemia);
- obstruction of the nose, difficulty in breathing;
- feeling of heart in the throat (palpitations);
- sweating, swelling (edema);
- difficulty urinating.
Other side effects (see section 2 - "Further information")
Some side effects that have occurred with other benzodiazepines may also occur during treatment with DEPAS:
- insomnia and anxiety (rebound symptoms);
- addiction and withdrawal syndrome;
- amnesia (antegrade);
- mental side effects;
- reappearance of a pre-existing depression.
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. You can also report side effects directly via the national reporting system at “www.agenziafarmaco.it/it/responsabili.” By reporting side effects you can help provide more information on the safety of this medicine.
Expiry and Retention
Keep this medicine out of the sight and reach of children.
DEPAS tablets: this medicine does not require any special storage conditions.
DEPAS oral drops, solution: this medicine does not require any special storage conditions.
Do not use 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.
Other information
What DEPAS contains
The active ingredient is: etizolam.
DEPAS 0.5 mg film-coated tablets
One 0.5 mg tablet contains: 0.5 mg of etizolam.
The other ingredients are: magnesium stearate, lactose, microcrystalline cellulose, maize starch, talc, hypromellose, titanium dioxide, macrogol 6000, dimethicone 200.
DEPAS 1 mg film-coated tablets
One 1 mg tablet contains: 1 mg of etizolam.
The other ingredients are: microcrystalline cellulose, lactose, maize starch, talc, magnesium stearate, macrogol 6000, hypromellose, titanium dioxide, dimethicone 200, indigo carmine aluminum lake.
DEPAS 0.5 mg / ml oral drops, solution
1 drop of DEPAS contains: 25 mcg of etizolam; 10 drops contain: 0.25 mg of etizolam.
The other ingredients are: sodium saccharin, glycerol, orange flavor, lemon flavor, caramel flavor, ethanol, propylene glycol.
Description of what DEPAS looks like and contents of the pack
DEPAS 0.5 mg film-coated tablets are available in cartons containing 30 scored coated tablets.
DEPAS 1 mg film-coated tablets are available in cartons containing 15 coated tablets.
DEPAS oral drops, solution is available in a 30 ml bottle fitted with a dropper, with a child resistant closure.
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
DEPAS
02.0 QUALITATIVE AND QUANTITATIVE COMPOSITION
Active principle:
Each 0.5 mg tablet contains etizolam 0.5 mg
Each 1 mg tablet contains etizolam 1 mg
100 ml of oral drops, solution contain etizolam 0.05 g
For the full list of excipients, see section 6.1
03.0 PHARMACEUTICAL FORM
Film-coated tablets; oral drops, solution
04.0 CLINICAL INFORMATION
04.1 Therapeutic indications
Anxiety, tension and other somatic or psychiatric manifestations associated with anxiety syndrome.
Insomnia
Benzodiazepines are only indicated when the disorder is severe, disabling, or makes the subject very uncomfortable.
04.2 Posology and method of administration
Treatment should be started with the lowest recommended dose.
The maximum dose should not be exceeded.
The use of the product is reserved for adult patients.
Anxiety, tension and other somatic or psychiatric manifestations associated with the anxiety syndrome:
0.25-0.50 mg two or three times a day; or 2 tablets of 1 mg per day (1 tablet in the morning and 1 tablet in the evening), for more intense disorders.
The dosage can also be taken using the package in drops considering that 10 drops are equal to 0.25 mg.
Treatment should be as short as possible.The patient should be re-evaluated regularly and the need for continued treatment should be carefully considered, particularly if the patient is symptom-free. The overall duration of treatment should generally not exceed 8-12 weeks, including a gradual withdrawal period. In certain cases, extension beyond the maximum treatment period may be necessary, in which case this should not be done without reassessment of the patient's condition.
Insomnia:
1-2 mg (1-2 tablets of 1 mg) before bedtime, depending on individual needs.
The dosage can also be taken using the package in drops considering that 10 drops are equal to 0.25 mg.
Treatment should be as short as possible. The duration of treatment generally ranges from a few days to two weeks, up to a maximum of four weeks, including a gradual withdrawal period. In certain cases, extension beyond the maximum treatment period may be necessary; if so, it should not take place without reassessment of the patient's condition.
In the treatment of elderly patients and for patients with impaired hepatic and / or renal function, the posology must be carefully established by the physician, who will have to evaluate a "possible reduction of the dosages indicated above. In elderly patients, the daily dose should in any case not exceed 1.5 mg.
04.3 Contraindications
Myasthenia gravis (symptoms may be aggravated by the muscle relaxant effect). Hypersensitivity to the active substance or to other benzodiazepines. Hypersensitivity to any of the excipients. Severe respiratory failure. Severe hepatic insufficiency. Sleep apnea syndrome. Acute closed-angle glaucoma (i symptoms could be aggravated by the anticholinergic effect).
04.4 Special warnings and appropriate precautions for use
Tolerance
Some loss of efficacy to the hypnotic effects of benzodiazepines may develop after repeated use for a few weeks.
Dependence
The use of benzodiazepines can lead to the development of physical and psychological dependence on these drugs. The risk of addiction increases with dose and duration of treatment; it is greater in patients with a history of drug or alcohol abuse. Once physical dependence has developed, abrupt termination of treatment will be accompanied by withdrawal symptoms. These may consist of headache, muscle aches, extreme anxiety, tension, restlessness, confusion and irritability. In severe cases the following symptoms may occur: derealization, depersonalization, hyperacusis, numbness and tingling of the extremities, hypersensitivity to light, noise and physical contact, hallucinations or seizures.
Rebound insomnia and anxiety: A transient syndrome in which symptoms leading to treatment with benzodiazepines recur in an aggravated form may occur on discontinuation of treatment. It may be accompanied by other reactions, including mood changes, anxiety, restlessness or disturbances As the risk of withdrawal or rebound symptoms is greater after abrupt discontinuation of treatment, a gradual decrease in dosage is suggested.
Duration of treatment
The duration of treatment should be as short as possible (see section 4.2 "Posology and method of administration") depending on the indication, but should not exceed four weeks for insomnia and eight to twelve weeks for anxiety. including a gradual withdrawal period. Extension of therapy beyond these periods should not occur without reassessment of the clinical situation. It may be helpful to inform the patient when treatment is started that it will be of limited duration and to explain precisely how the dosage should be progressively decreased.
It is also important that the patient is informed of the possibility of rebound phenomena, thus minimizing anxiety about these symptoms should they occur upon discontinuation of the drug.
There is evidence that, in the case of benzodiazepines with a short duration of action, withdrawal symptoms may become manifest within the dosing interval between doses, particularly for high doses.
When using long-acting benzodiazepines, it is important to advise the patient that abrupt change to a short-acting benzodiazepine is inadvisable as withdrawal symptoms may occur.
Amnesia
Benzodiazepines can induce anterograde amnesia. This occurs more often several hours after ingestion of the drug and, therefore, to reduce the risk it should be ensured that patients can have an uninterrupted sleep of 7-8 hours (see section 4.8 "Undesirable effects").
Psychiatric and paradoxical reactions
When benzodiazepines are used it is known that reactions such as restlessness, agitation, irritability, aggression, disappointment, anger, nightmares, hallucinations, psychosis, behavioral changes can occur. Should this occur, the use of the medicinal product should be discontinued. These reactions are more frequent in children and the elderly.
Specific groups of patients
Benzodiazepines should not be given to children without careful consideration of the actual need for treatment as the safety of the drug in children has not been determined; treatment duration should be as short as possible. Elderly people should take a reduced dose as this may occur. some adverse reactions such as motor ataxia (see section 4.2 "Posology and method of administration"). Likewise, a lower dose is suggested for patients with chronic respiratory insufficiency due to the risk of respiratory depression.
Benzodiazepines are not indicated in patients with severe hepatic insufficiency as they can precipitate encephalopathy. Benzodiazepines are not recommended for the primary treatment of psychotic illness.
Benzodiazepines should not be used alone to treat depression or anxiety associated with depression (suicide can be precipitated in such patients). Benzodiazepines should be used with extreme caution in patients with a history of drug or alcohol abuse.
Depas should be administered with caution in subjects with organic brain disorders, renal or hepatic disorders and hypotonia, as potentiation of the effect of the medicinal product may occur in such patients.
Caution should also be used with people with heart disease as the medicine can lead to a lowering of blood pressure and this effect may be aggravated in this group of patients.
Depas 0.5 mg film-coated tablets and Depas 1 mg film-coated tablets contain lactose, therefore they are not suitable for individuals with Lapp lactase deficiency, galactosemia or glucose / galactose malabsorption syndrome.
04.5 Interactions with other medicinal products and other forms of interaction
Concomitant intake with alcohol should be avoided. The sedative effect may be enhanced when the medicinal product is taken in conjunction with alcohol. This adversely affects the ability to drive or use machines.
Association with CNS depressants: the central depressive effect may be enhanced in cases of concomitant use with antipsychotics (neuroleptics), hypnotics, anxiolytics / sedatives, antidepressants, narcotic analgesics, antiepileptics, anesthetics and sedative antihistamines. In these conditions somnolence may occur. , hypotension, ataxia and disturbances of consciousness.
In the case of narcotic analgesics, an increase in euphoria can occur, leading to an increase in psychic dependence.
Combination with drugs that affect liver enzymes: Compounds that inhibit certain liver enzymes, especially cytochrome P450, may increase the activity of benzodiazepines. To a lesser extent this also applies to benzodiazepines which are metabolized only by conjugation.
Etizolam is metabolised in the liver by cytochromial isoenzymes CYP2C9 and CYP3A4. Among the drugs capable of inhibiting the metabolism of etizolam, with consequent increase in its plasma concentrations and possible enhancement of its effects, is fluvoxamine maleate. Caution is therefore recommended, reducing the dose, in the association of the latter with etizolam.
Association with monoamine oxidase inhibitors (MAO): monoamine oxidase inhibitor drugs can inhibit the metabolization of etizolam in the liver which causes a prolongation of the half-life and an increase in blood concentration. The use of these drugs can enhance the "effect of" etizolam and excessive sedation, coma, seizures, arousal etc may occur.
04.6 Pregnancy and breastfeeding
If the product is prescribed to a woman of childbearing potential, she should contact her doctor, both if she intends to become pregnant, and if she suspects that she is pregnant, regarding discontinuation of the medicine.
If, for serious medical reasons, the product is administered during the last period of pregnancy or during labor, at high doses, effects on the newborn may occur such as reduced activity, decreased sucking, lethargy, tachycardia, apnea, cyanosis, vomiting, increased of serum CK, hypothermia, hypotonia and moderate respiratory depression due to the pharmacological action of the drug.
In addition, infants born to mothers who have taken benzodiazepines chronically during late pregnancy may develop physical dependence and may be at some risk for developing withdrawal symptoms in the postnatal period and have symptoms such as apnea, cyanosis, decreased sucking, reduced activity and withdrawal syndrome (irritability, tremor, hypertonus). Since benzodiazepines are excreted in breast milk, they should not be given to breastfeeding mothers. If etizolam is needed, the patient should stop breastfeeding as the medicine can pass into breast milk and block the baby's weight gain. It can also cause worsening of jaundice.
04.7 Effects on ability to drive and use machines
Sedation, amnesia, impaired concentration and muscle function can adversely affect the ability to drive and use machines. If sleep duration has been insufficient, the likelihood of impaired alertness may be increased (see 4.5 "Interactions with other medicinal products and other forms of interaction").
04.8 Undesirable effects
Depas is generally well tolerated. However, the following side effects may appear: drowsiness (during the day if the product is used for sleep disorders), dulling of emotions, decreased alertness, confusion, speech disturbances, fatigue, headache, dizziness, muscle weakness, ataxia , ocular disorders, double vision, thirst, nausea and skin rash. These phenomena occur mainly at the beginning of therapy and usually disappear with subsequent administrations.
Other adverse reactions have occasionally been reported including: gastrointestinal disturbances, hyperprolactinaemia, changes in libido, erythema and skin reactions, sensation of difficulty in breathing, palpitations, gynaecomastia, bleferospasms (if eye symptoms such as excessive blinking are observed , photophobia and dry eyes, intervene with the appropriate therapy), sweating, edema, urination disorders and nasal obstruction.
Amnesia
Anterograde amnesia can also occur at therapeutic dosages, the risk increases at higher dosages. Amnesic effects may be associated with behavioral changes (see 4.4 "Special warnings and precautions for use").
Depression
During the use of benzodiazepines a pre-existing depressive state can be unmasked. Benzodiazepines or benzodiazepine-like compounds can cause reactions such as: restlessness, agitation, irritability, aggression, disappointment, anger, nightmares, hallucinations, psychosis, behavioral changes. they can be quite serious.
They are more likely in children and the elderly.
Dependence
The use of benzodiazepines (even at therapeutic doses) can lead to the development of physical dependence: discontinuation of therapy can cause rebound or withdrawal phenomena such as convulsive attacks, delirium, tremor, insomnia, anxiety, hallucinations, etc. (see 4.4 "Special warnings and precautions for use"). Psychic dependence can occur. Abuse of benzodiazepines has been reported.
The following adverse reactions of unknown incidence were also observed:
Respiratory depression, CO2 narcosis : Respiratory depression and CO2 narcosis may occur in patients with severely impaired respiratory function. If any of these symptoms occur, take appropriate measures, such as airway control and ventilation.
Neuroleptic malignant syndrome: this syndrome may be caused by concomitant use with antipsychotics and other drugs, abrupt dose reduction and discontinuation of administration. If fever, severe muscle stiffness, dysphagia, tachycardia, changes in blood pressure, sweating, increased blood cells appear and serum CK levels (CPK), etc., the drug must be discontinued and total body measures, such as body cooling and hydration, must be taken. In addition, if this syndrome occurs, renal hypofunction with myoglobinuria may appear .
Rhabdomyolysis: this disease is characterized by myalgia, weakness, increased levels of CK (CPK) and myoglobin, in the blood / urine. If rhabdomyolysis occurs, discontinue drug administration and take appropriate therapeutic measures.
Interstitial pneumonia: interstitial pneumonia may occur. In the event of fever, cough, dyspnoea, and abnormal chest sounds (crackles), discontinue drug administration and take a chest x-ray. Adopt appropriate therapeutic measures, such as administering adrenocorticoid hormones.
Abnormal liver function, jaundice: liver function disorders (increased AST (GOT), ALT (GPT),? -GT, LDH, ALP, bilirubin, etc.) and jaundice may occur; the patient should be carefully monitored and, in case of abnormal test results, the treatment should be stopped.
04.9 Overdose
As with other benzodiazepines, an overdose is not expected to be life-threatening unless concomitant other CNS depressants (including alcohol) are taken.
In the treatment of overdose of any drug, the possibility that other substances have been taken at the same time should be considered.
Benzodiazepine overdose usually results in varying degrees of central nervous system depression ranging from "drowsiness to coma. In mild cases, symptoms include drowsiness, mental confusion, and lethargy. In severe cases, symptoms may include ataxia, hypotonia. , hypotension, respiratory depression, rarely coma and very rarely death.
Following an overdose of oral benzodiazepines, vomiting should be induced (within one "hour) if the patient is conscious or gastric lavage, with respiratory protection undertaken, if the patient is unconscious.
If no improvement is observed with stomach emptying, activated charcoal should be given to reduce absorption. Special attention should be paid to respiratory and cardiovascular functions in emergency therapy.
"Flumazenil" can be useful as an antidote.
05.0 PHARMACOLOGICAL PROPERTIES
05.1 Pharmacodynamic properties
Pharmacotherapeutic group: Anxiolytics, benzodiazepine derivatives.
ATC code: N05BA
DEPAS (Etizolam) is the progenitor of an original chemical class of diazepines, the thienotriazolodiazepines.
The thiophene ring, which replaces the benzene ring, makes the molecule more easily oxidizable and therefore more rapidly metabolized in the organism; the risk of accumulation is thus considerably reduced, even in prolonged treatments. etizolam has been shown to have a powerful anxiolytic action (about 6 times higher than that of diazepam).
Etizolam also determines, especially at higher dosages, a reduction in the time of falling asleep, an increase in the total duration of nighttime sleep and a reduction in the number of awakenings. This hypno-inducing effect is not accompanied by a significant reduction in slow sleep.
The decrease in REM activity is not followed, on suspension of administration, by a compensatory increase (rebound phenomenon).
In some pharmacological studies (brain monoamine turnover in animals and EEG drug studies in healthy volunteers), etizolam has shown that
qualitative characteristics similar to those observed with some antidepressant drugs (tricyclics). Etizolam was found to have no significant action on the cardiovascular and respiratory systems.
05.2 Pharmacokinetic properties
In humans, after a single administration, etizolam is completely and rapidly absorbed from the gastrointestinal tract and reaches the maximum blood concentration after 3.2 hours. The plasma protein binding is in the order of 93% . The elimination half-life in humans is 6.2 hours. Therefore, etizolam should be classified in the context of diazepines with a medium-short half-life.
Following repeated administration of a 1 mg tablet three times / day, from 30 minutes to 1 hour after a meal, the plasma concentration of the drug, in the patients considered, was similar after 7, 14 and 28 days. This finding therefore suggests that etizolam, at the doses used in the clinic, exhibits linear kinetics. After absorption, etizolam is rapidly and extensively metabolised in the liver (by hydroxylation and oxidation) and then conjugated with glucuronic acid. The unchanged drug and its metabolites are excreted by the kidney.
05.3 Preclinical safety data
Acute toxicity (single administration):
Chronic toxicity (repeated administrations)
In the long-term toxicity studies conducted on various animal species using high doses (up to 50 mg / kg in the rat and up to 10 mg / kg in the dog) no particular pathological lesions or dysfunctions affecting organs or systems were found, nor did any significant alterations in biohumoral indices emerge. In all cases, mortality never significantly differed from that expected for this type of test.
06.0 PHARMACEUTICAL INFORMATION
06.1 Excipients
0.5 mg film-coated tablets
Magnesium stearate, lactose, microcrystalline cellulose, corn starch, talc, hypromellose, titanium dioxide, macrogol 6000, dimethicone 200.
1 mg film-coated tablets
Microcrystalline cellulose, lactose, corn starch, talc, magnesium stearate, macrogol 6000, hypromellose, titanium dioxide, dimethicone 200, indigo carmine aluminum lake.
0.5 mg / ml oral drops, solution
Sodium saccharin, glycerol, orange flavor, lemon flavor, caramel flavor, ethyl alcohol, propylene glycol.
06.2 Incompatibility
None.
06.3 Period of validity
3 years in intact packaging.
06.4 Special precautions for storage
No special storage precautions.
06.5 Nature of the immediate packaging and contents of the package
Film-coated tablets: Opaque diophanate blister
Drops: amber glass vial with dropper and difficult to open closure
0.5 mg film-coated tablets - 30 divisible tablets
1 mg film-coated tablets - 15 tablets
0.5 mg / ml oral drops, solution - 30 ml bottle
06.6 Instructions for use and handling
No special instructions
07.0 MARKETING AUTHORIZATION HOLDER
Abbott S.r.l. - S.R. 148 Pontina km 52 snc, 04011 Campoverde di Aprilia (LT)
08.0 MARKETING AUTHORIZATION NUMBER
0.5 mg film-coated tablets - 30 tablets - AIC n. 025640057 - September 1989
1 mg film-coated tablets - 15 tablets - AIC n. 025640071 - October 1991 0.5 mg / ml oral drops, solution - 30 ml bottle - AIC n. 025640069 - September 1989
09.0 DATE OF FIRST AUTHORIZATION OR RENEWAL OF THE AUTHORIZATION
18-02-1988/31-05-2010
10.0 DATE OF REVISION OF THE TEXT
April 2012
