Rispolept
Rispolept: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Rispolept
ATX code: N05AX08
Active ingredient: risperidone (risperidone)
Manufacturer: Janssen Pharmaceutica (Belgium), Janssen-Cilag (Italy)
Description and photo update: 2019-19-08
Prices in pharmacies: from 218 rubles.
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Rispolept is a benzisoxazole derivative, an antipsychotic drug (neuroleptic) with sedative, hypothermic and antiemetic effects.
Release form and composition
Dosage forms of Rispolepta:
- film-coated tablets: oblong, convex on both sides, with a line: 1 mg - white, with the words "1" and "Ris" on one side, 2 mg - light orange, with the words "2" and " Ris "on one side, 3 mg - yellow, with the words" 3 "and" Ris "on one side, 4 mg - green, with the words" 4 "and" Ris "on one side (10 pcs. In blisters, in a cardboard box 2 or 6 blisters);
- oral solution: colorless, transparent (30 or 100 ml in dark glass bottles, in a cardboard box 1 bottle and a graduated pipette).
The active substance is risperidone:
- 1 tablet - 1, 2, 3 or 4 mg;
- 1 ml of solution - 1 mg.
Additional components of the tablets:
- excipients: corn starch, microcrystalline cellulose, hypromellose 2910, lactose monohydrate, magnesium stearate, sodium lauryl sulfate, colloidal silicon dioxide;
- shell composition: propylene glycol, hypromellose 2910, in addition, in tablets 2, 3 and 4 mg - titanium dioxide, talc, dyes (in tablets 2 mg - sunset yellow (E110), in tablets 3 mg - quinoline yellow (E104), in 4 mg tablets - quinoline yellow (E104) and indigo carmine (E132)).
Excipients of the oral solution: purified water, tartaric acid, sodium hydroxide and benzoic acid.
Pharmacological properties
Pharmacodynamics
Risperidone, the active substance of Rispolepta, is a selective monoaminergic antagonist with high affinity for dopamine D 2 and serotonin 5-HT 2 receptors. Also, the active ingredient binds α 1 -adrenergic receptors and more weakly with α 2 -adrenergic receptors and H 1 -histaminergic receptors. The drug is not characterized by tropism for cholinergic receptors.
The substance reduces the severity of the productive symptoms of schizophrenia, but at the same time does not cause significant inhibition of motor activity and induces catalepsy more weakly in comparison with classical antipsychotics. The balanced central antagonism to dopamine and serotonin inherent in Rispolepta reduces the susceptibility to extrapyramidal side effects, as well as expands and enhances the therapeutic effect of risperidone, which allows to cover the affective and negative manifestations of schizophrenia.
Pharmacokinetics
After oral administration, risperidone is completely absorbed, its peak plasma concentrations are observed after about 1–2 hours. The absolute bioavailability of risperidone after oral administration is 70%, relative - when taking Risperidone in the form of tablets is 94% when compared with the drug in the form of a solution. The absorption of the product does not depend on food intake. In most patients, the steady-state concentration (C ss) of risperidone in the body is reached within 1 day, C ss 9-hydroxyrisperidone (the main metabolite of the active substance) - within 4–5 days.
Risperidone is characterized by rapid distribution, with the volume of distribution (V d) equal to 1–2 l / kg. The active substance binds to plasma proteins (albumin and alpha 1- acid glycoprotein) by 90%, and its main metabolite by 77%. The content of risperidone in plasma is directly proportional to the dose taken, which lies in the therapeutic dose range.
Risperidone is metabolized with the participation of the isoenzyme CYP 2D6 to 9-hydroxyrisperidone. This metabolic transformation product exhibits pharmacological action similar to risperidone and forms an active antipsychotic fraction with it. The genes of the isoenzyme CYP 2D6 are characterized by a high level of polymorphism. In the presence of increased metabolism by the CYP 2D6 isoenzyme, risperidone is rapidly biotransformed into 9-hydroxyrisperidone, in the presence of a weak metabolism, this process proceeds much more slowly. Despite the fact that patients with an increased metabolism have a lower concentration of risperidone and a higher concentration of 9-hydroxyrisperidone than patients with a weak metabolism,the active antipsychotic fraction (total pharmacokinetics of 9-hydroxyrisperidone and risperidone) after oral administration is similar in patients with weak and intensive CYP 2D6 metabolism.
The second metabolic pathway for risperidone is via N-dealkylation. According to in vitro studies on human liver microsomes, upon reaching clinically significant concentrations of risperidone, there was no inhibition of the metabolism of drugs that are biotransformed under the action of isoenzymes of the P 450 system, such as CYP 2C8 / 9/10, CYP 2A6, CYP 2E1, CYP 1A2, CYP 2D6, CYP 3A5 and CYP 3A4.
7 days after the start of the use of Rispolepta, 70% of the dose taken is excreted in the urine, 14% in the feces. The total urinary concentration of risperidone and 9-hydroxyrisperidone is 35–45% of the dose taken. The rest is represented by inactive metabolites. In patients with psychosis, after oral administration, the half-life (T ½) of risperidone can be approximately 3 hours, the T ½ of the active antipsychotic fraction and 9-hydroxyrisperidone - 24 hours.
In patients with renal failure, a decrease in clearance and an increase in the plasma level of the active antipsychotic fraction by about 60% were recorded.
In the presence of functional disorders of the liver in the blood plasma, an increase in the average concentration of the free fraction of risperidone by 35% was noted.
Plasma concentrations of the active antipsychotic fraction in elderly patients after a single use of the drug were approximately 43% higher, clearance decreased by 30%, and T ½ increased by 38%.
When conducting a population pharmacokinetic analysis, no clear effect of race, gender or smoking on the pharmacokinetic parameters of risperidone and the active pharmacokinetic fraction was identified.
Indications for use
In tablets, Rispolept is used for the relief of acute attacks and long-term maintenance therapy of the following conditions / diseases:
- acute and chronic schizophrenia and other psychotic disorders, accompanied by productive and negative symptoms;
- behavioral disorders in patients with dementia - with disturbances in activity (delirium, agitation), the appearance of psychotic symptoms or signs of aggression (physical violence, outbursts of anger);
- affective disorders in various mental illnesses;
- behavioral disorders in patients (over 15 years old) with a reduced intellectual level or mental retardation in cases where destructive tendencies dominate in the clinical picture (autoaggression, impulsivity, aggression);
- mania for bipolar disorder (as adjuvant therapy to stabilize mood).
In the form of a solution for oral administration, Rispolept is prescribed in the following cases:
- schizophrenia in adults and adolescents from 13 years of age;
- moderate to severe manic episodes associated with bipolar disorder in adults and children over 10 years of age;
- short-term (up to 6 weeks) therapy of persistent aggression in patients with dementia accompanying moderate to severe Alzheimer's disease, which does not lend itself to non-drug methods of correction, and in cases where there is a risk that the patient may harm himself or others;
- short-term (up to 6 weeks) symptomatic therapy of persistent aggression in the structure of behavioral disorder in children from 5 years of age with mental retardation (established in accordance with the DSM-IV Diagnostic and Statistical Manual of Mental Disorders), requiring drug treatment due to the severity of aggression or other destructive behavior (Rispolept is used as part of a comprehensive treatment that includes educational and psychological activities).
Contraindications
- phenylketonuria;
- lactation period;
- children under 5 years old;
- hypersensitivity to any component of the drug.
According to the instructions, Rispolept should be used with caution in the following cases:
- convulsions, including a history of;
- Parkinson's disease;
- disorders of cerebral circulation;
- acute drug overdose;
- intestinal obstruction;
- diffuse Lewy body disease;
- dehydration and hypovolemia;
- brain tumor;
- severe renal / hepatic impairment;
- Reye's syndrome;
- diseases of the cardiovascular system (violations of the conduction of the heart muscle, myocardial infarction, chronic heart failure);
- conditions due to which the development of tachycardia of the "pirouette" type is possible (electrolyte imbalance, bradycardia, concomitant use of drugs that can lengthen the QT interval);
- risk factors for the development of venous thromboembolism;
- drug abuse or drug dependence;
- cerebrovascular dementia in elderly patients;
- pregnancy;
- age up to 15 years (for tablets).
Instructions for the use of Rispolepta: method and dosage
Both dosage forms of Rispolepta are intended for oral administration. Food intake does not affect the effectiveness of the drug.
Film-coated tablets
In schizophrenia, adults and children over 15 years of age Rispolept are prescribed: on the first day - 2 mg, on the second day - 4 mg, then the dose is left or adjusted if necessary (frequency of use - 1 or 2 times a day). The optimal daily dose is 4-6 mg. In some cases, it is advisable to increase the dose slowly, as well as the use of lower initial and maintenance doses.
If additional sedation is required, benzodiazepines are prescribed in addition to Rispolept.
The recommended initial dose for the elderly, patients with impaired renal and liver function is 0.5 mg 2 times a day, then the dose can be increased by 0.5 mg 2 times a day until the maximum permissible dose is 1-2 mg 2 times a day. day.
In the treatment of mania in bipolar disorders, at the beginning of therapy, Rispolept is prescribed 2 mg 1 time per day, if necessary, the dose is further increased by 2 mg 1 time in 2 days or less. The optimal daily dose in most cases is 2-6 mg.
Patients with drug dependence and people who abuse drugs are prescribed 2-4 mg per day.
For behavioral disorders in patients with dementia, the initial dose of Rispolepta is 0.25 mg 2 times a day. If necessary, the dose is further increased by 0.25 mg every 2 days or less. Optimal in most cases is a daily dose of 0.5 mg 2 times a day, but sometimes it is required to use 1 mg 2 times a day. After achieving the desired effect, the frequency of administration can be reduced to 1 time per day.
For behavioral disorders in patients with mental retardation and in cases where destructive behavior is leading in the clinical picture of the disease, Rispolept is prescribed:
- patients with a body weight of 50 kg: initial dose - 0.5 mg 1 time per day, then no more than 1 time in 2 days, if necessary, increase the dose by 0.5 mg per day. The optimal daily dose for most patients is 1 mg, although in some cases it may be more preferable to take 0.5 mg per day, and for some patients - 1.5 mg per day;
- patients weighing up to 50 kg: the initial dose is 0.25 mg once a day, then no more than once every 2 days, if necessary, the dose is increased by 0.25 mg per day. The optimal daily dose in most cases is 0.5 mg, although in some cases it may be more preferable to take 0.25 mg per day, and for some patients - 0.75 mg per day.
Oral solution
Recommended doses of Rispolept in schizophrenia:
- adults: on the first day - 2 mg, on the second day - 4 mg, then the dose is left or adjusted, if necessary. The optimal daily dose is 4-6 mg. In some cases, it is advisable to increase the dose more slowly, as well as the use of lower initial and maintenance doses;
- elderly patients: the initial dose is 0.5 mg 2 times a day, if necessary, then the dose is increased by 0.5 mg 2 times a day to a maximum dose of 1-2 mg 2 times a day;
- adolescents from 13 years old: the initial dose is 0.5 mg once a day (morning or evening). If the effect is not enough, the dose is gradually increased - no more than 1 time per day - by 0.5-1 mg per day (provided that Rispolept is well tolerated). The maximum daily dose is 3 mg.
Recommended dosing regimens for manic episodes associated with bipolar disorder:
- adults: the initial dose is 2 mg once a day, if necessary, it is increased by 1 mg once a day. The optimal dose is selected individually and can vary from 1 to 6 mg;
- elderly patients: the initial dose is 0.5 mg 2 times a day, if necessary, then the dose is gradually increased by 0.5 mg 2 times a day until the daily dose is 1-2 mg 2 times a day;
- children from 10 years old: initial dose - 0.5 mg 1 time per day (morning or evening). If the effect is not enough, the dose is gradually increased - no more than 1 time per day - by 0.5-1 mg per day (provided that Rispolept is well tolerated). The maximum recommended daily dose is 1-2.5 mg.
With persistent aggression in patients with dementia due to Alzheimer's disease, at the beginning of treatment, 0.25 mg is prescribed 2 times a day. If necessary, the dose is gradually increased - no more than 1 time in 2 days - by 0.25 mg 2 times a day. In most cases, the optimal dose of Rispolepta is 0.5 mg 2 times a day, however, some patients may need to increase the dose to 1 mg 2 times a day. The duration of treatment for these patients should not exceed 6 weeks.
Recommended dosages of Rispolepta for incessant aggression in the structure of conduct disorder in children 5-18 years old:
- patients with a body weight of 50 kg: the initial dose is 0.5 mg once a day, if necessary, gradually - more often than once every 2 days - the dose is increased by 0.5 mg per day. In most cases, the optimal daily dose is 1 mg, but some patients need 0.5 mg per day, and some patients may need 1.5 mg per day;
- patients weighing up to 50 kg: the initial dose is 0.25 mg once a day, then no more than once every 2 days, if necessary, the dose is increased by 0.25 mg per day. The optimal daily dose in most cases is 0.5 mg, although in some cases it may be more preferable to take 0.25 mg per day, and for some patients - 0.75 mg per day.
For patients with kidney disease, the initial and maintenance doses of Rispolepta are halved, and the increase in dosage is carried out at long intervals.
For patients in whom Rispolept causes persistent drowsiness, it is recommended to divide the daily dose into 2 doses.
Side effects
- from the nervous system: very often (> 1/10 cases) - parkinsonism, drowsiness, headache, sedation; often (> 1/100 and 1/1000 and 1/10 000 and <1/1000 cases) - head tremor, diabetic coma, neuroleptic malignant syndrome, cerebrovascular disorders;
- mental disorders: very often - insomnia; often - agitation, anxiety, sleep disturbances, restlessness; infrequently - lethargy, mania, nervousness, decreased libido, confusion; rarely - flattening of affect, anorgasmia;
- from the skin and subcutaneous tissues: often - rash, erythema; infrequently - acne, acne, alopecia, discoloration of the skin, itching, skin disorder, dry skin, skin lesions, hyperkeratosis, seborrheic dermatitis; rarely - dandruff; very rarely (<1/10 000 cases) - Quincke's edema;
- violations of laboratory and instrumental parameters: often - an increase in body weight, an increase in the level of prolactin; infrequently - an increase in body temperature, an increase in cholesterol concentration, a decrease in the level of hemoglobin and the number of leukocytes in the blood, deviations in the electrocardiogram (including lengthening the QT interval), an increase in the level of creatine phosphokinase, the number of eosinophils in the blood, the level of transaminases; rarely - an increase in the concentration of triglycerides, a decrease in body temperature;
- on the part of the cardiovascular system: often - arterial hypertension, tachycardia; infrequently - blockade of the His bundle, impaired cardiac conduction, palpitations, atrial fibrillation, atrioventricular block; rarely - pulmonary embolism, sinus bradycardia, deep vein thrombosis;
- from the gastrointestinal tract: often - hypersalivation, dry mouth, abdominal pain, stomach discomfort, diarrhea / constipation, dyspepsia, vomiting, nausea; infrequently - flatulence, gastritis, fecaloma, fecal incontinence, dysphagia, gastroenteritis; rarely - cheilitis, edema of the lips, pancreatitis, intestinal obstruction;
- from the organ of hearing: infrequently - pain and noise in the ears;
- from the musculoskeletal system and connective tissue: often - arthralgia, back pain, pain in the extremities; infrequently - muscle pain in the chest, neck pain, joint stiffness, joint swelling, myalgia, muscle weakness, poor posture; rarely - rhabdomyolysis;
- mediastinal disorders, respiratory and thoracic disorders: often - pain in the larynx and pharynx, cough, shortness of breath, nasal congestion, nosebleeds; infrequently - dysphonia, respiratory failure, aspiration pneumonia, airway obstruction, pulmonary congestion, wheezing, wet wheezing; rarely - hyperventilation, sleep apnea syndrome;
- vascular disorders: infrequently - hot flashes, hypotension, orthostatic hypotension;
- hepatobiliary disorders: rarely - jaundice;
- from the endocrine system: rarely - a violation of the production of antidiuretic hormone;
- on the part of the kidneys and urinary tract: often - enuresis; infrequently - dysuria, pollakiuria, urinary incontinence, urinary retention;
- from the reproductive system and mammary glands: infrequently - gynecomastia, galactorrhea, amenorrhea, vaginal discharge, menstrual disorder, sexual dysfunction, ejaculation disorder, erectile dysfunction; rarely priapism;
- hematological disorders and disorders of the lymphatic system: infrequently - thrombocytopenia, anemia; rarely - agranulocytosis, granulocytopenia;
- metabolic and nutritional disorders: often - decreased / increased appetite; infrequently - hyperglycemia, diabetes mellitus, polydipsia, anorexia; rarely - water intoxication, hypoglycemia; very rarely, diabetic ketoacidosis;
- from the immune system: infrequently - hypersensitivity; rarely - anaphylactic reaction, drug hypersensitivity;
- infections: often - ear infections, sinusitis, upper respiratory tract infections, bronchitis, influenza, pneumonia, urinary tract infections; infrequently - localized infections, otitis media, tonsillitis, acrodermatitis, viral infections, eye infections, inflammation of the subcutaneous fat, onychomycosis, cystitis; rarely - chronic otitis media;
- ophthalmic disorders: often - conjunctivitis, blurred vision; infrequently - photophobia, edema of the eye area, discharge from the eyes, increased lacrimation, blurred vision, redness of the eyes, dry eyes; rarely - glaucoma, decreased visual acuity, intraoperative syndrome of flabby iris, involuntary rotation of the eyeballs;
- general disorders: often - asthenia, fatigue, pain in the chest area, pyrexia, generalized edema, peripheral edema; infrequently - chills, sluggishness, feeling unwell, gait disturbance, thirst, facial swelling, chest discomfort, flu-like condition; rarely - withdrawal syndrome, hypothermia, cold extremities.
Overdose
Symptoms of risperidone overdose may be its already known side reactions, manifested in a more pronounced form, such as sedation, drowsiness, arterial hypotension, tachycardia, extrapyramidal symptoms. It is also possible to develop seizures and lengthen the QT interval with the combined use of risperidone and paroxetine in doses exceeding those prescribed by the doctor.
In case of acute overdose, the likelihood of the interaction of several drugs taken in too high doses should not be excluded.
In this condition, it is required to restore and maintain a clear airway in order to ensure adequate ventilation and adequate oxygen supply. In the case when less than 1 hour has passed from the moment of taking Rispolept, it is recommended to wash the stomach (if the patient is unconscious - after intubation) and take activated charcoal in combination with a laxative. ECG monitoring is shown to detect possible arrhythmias.
There is no specific antidote for risperidone, therefore, appropriate symptomatic therapy is necessary. To eliminate arterial hypotension and vascular collapse, intravenous fluids and / or sympathomimetic agents are prescribed. If severe extrapyramidal symptoms occur, anticholinergic drugs are used. The patient requires constant medical supervision until the symptoms of intoxication are completely removed.
special instructions
Before prescribing Rispolept to children and adolescents with mental retardation, it is necessary to conduct a thorough assessment of their condition in order to exclude social or physical reasons for their aggressive behavior, such as pain or inadequate requirements of the social environment.
In schizophrenia, at the initial stage of treatment with Rispoleptom, it is recommended to gradually cancel the previous drugs used, if it is clinically justified. Patients who are transferred from the depot of forms of antipsychotic drugs are recommended to start taking Rispolept instead of the next scheduled injection. Patients receiving antiparkinsonian drugs should periodically assess the need for their use.
In the case of orthostatic hypotension, it is necessary to reduce the dose of Rispolept.
During treatment, it is recommended to refrain from overeating due to the likelihood of weight gain.
Until an individual's sensitivity to risperidone is established, driving a car and performing other potentially hazardous activities that require speed of reactions and high concentration of attention should be avoided.
Application during pregnancy and lactation
There have been no fully-fledged controlled studies on the use of Rispolept during pregnancy. In the post-marketing period, the appearance of reversible extrapyramidal symptoms in a newborn after his mother took risperidone in the last trimester of pregnancy was noted. As a consequence, in such cases, newborns require careful monitoring.
According to the results of animal studies, no teratogenic effect was found in risperidone, but a different toxic effect on the reproductive system was revealed. The possible risk to humans has not been identified. Taking Rispolept during pregnancy is allowed only when the intended benefits of the treatment for the woman far outweigh the possible threat to the health of the fetus. If it is necessary to cancel the drug during pregnancy, discontinue drug therapy gradually, reducing the dosage and increasing the intervals between doses.
It has been experimentally established that risperidone and its active metabolite pass into breast milk in animals. It is also known that, in small quantities, these substances penetrate into human milk. Data on the possible adverse effects of risperidone in infants have not been provided. In view of the above, if it is necessary to take Rispolept during lactation, the issue of breastfeeding should be decided, taking into account the potential risk to the child.
Pediatric use
The pharmacokinetics of the active antipsychotic fraction, risperidone and 9-hydroxyrisperidone in children are comparable to those in adults.
It is not recommended to take Rispolept for children under 5 years of age due to the lack of data on its use in patients of this age category.
With impaired renal function
Since in patients with impaired renal function, the ability to excrete the active antipsychotic fraction is reduced, the initial and maintenance doses should be halved in accordance with the indications. Increasing the dose in patients of this group should be carried out more slowly than in patients with normal renal function.
In severe renal failure, Rispolept should be used with extreme caution.
For violations of liver function
In patients with impaired liver function, the concentration of the free fraction of risperidone in the blood is increased. Taking into account the indications, it is recommended for such patients to reduce the initial and maintenance dose of the drug by half, and then to gradually increase it.
Patients with severe hepatic impairment need to take Rispolept with caution.
Use in the elderly
In view of the limited experience with the use of risperidone in elderly patients, this group of patients should be careful during the period of therapy, especially when taking Risperidone by elderly people with cerebrovascular dementia.
Drug interactions
Rispolept should be used with caution in combination with other centrally acting drugs and ethanol.
Carbamazepine and, presumably, other inducers of hepatic enzymes contribute to a decrease in the concentration of the active antipsychotic fraction of risperidone in plasma.
Fluoxetine can increase the plasma concentration of risperidone, but it has a lesser effect on the concentration of the active antipsychotic fraction.
With the simultaneous use of antihypertensive drugs, the severity of the decrease in blood pressure increases.
Clozapine decreases the clearance of risperidone.
Rispolept reduces the effectiveness of levodopa and other dopamine agonists.
Analogs
Rispolept's analogs are: Invega, Abilify, Xeplion, Amdoal, Zilaxera, Aripiprazole, Rispolept Kviklet, Leptinorm, Rezalen, Rileptid, Risset, Rispaxol, Ridonex, Risperidon, Speridan, Torendo.
Terms and conditions of storage
Keep out of reach of children at a temperature of 15-30 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Rispolept
On medical forums, reviews about Rispolept are very contradictory. One group of patients who took the drug and the parents of children who received this drug note its significant therapeutic effect, provided that the dose is correctly selected by a qualified specialist. The reviews indicate the effectiveness of the neuroleptic in the relief of pronounced manifestations of autoaggression in children and elderly patients, the decrease in psycho-productive symptoms caused by the drug, and its good tolerance. However, many also recommend that Rispolept be combined with behavioral therapy and other rehabilitation programs, since the remedy only relieves symptoms, but does not cure the disease itself.
Another group of patients is extremely negative about the use of Rispolept. According to their reviews, the drug has a short-term and weak effect, suppresses the emotional-volitional sphere of a person, with prolonged use is addictive, leads to a large number of undesirable reactions (drowsiness, significant weight gain, increased pressure, in children - enuresis). The disadvantage of Rispolepta is also considered its high cost.
Price for Rispolept in pharmacies
The approximate price for Rispolept is:
- film-coated tablets: dosage of 2 mg - 500–580 rubles, dosage of 4 mg - 950–1150 rubles per package containing 20 pieces;
- oral solution (1 mg / ml): 1100-1330 rubles per bottle containing 30 ml.
Rispolept: prices in online pharmacies
Drug name Price Pharmacy |
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Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!