Active ingredients: Orphenadrine (Orphenadrine hydrochloride)
Disipal 50 mg coated tablets
Indications Why is Disipal used? What is it for?
Pharmacotherapeutic group
Ethers chemically related to antihistamines.
THERAPEUTIC INDICATIONS
- Parkinson's disease and syndrome.
- Side effects and neuroleptic extrapyramidal syndrome.
- Dizzy syndromes.
- Spastic and painful contractures of the skeletal muscles.
Contraindications When Disipal should not be used
Hypersensitivity to the active substance or to any of the excipients.
Glaucoma, prostatic hypertrophy, gastrointestinal obstruction, intestinal obstruction or urinary retention of various causes, stenosing peptic ulcer, cardiospasm, myasthenia gravis, tardive dyskinesia, porphyria, history of hypersensitivity to the drug.
Precautions for use What you need to know before taking Disipal
Any increases or decreases in the daily doses of DISIPAL should be done gradually over a few days.
Interactions Which drugs or foods can modify the effect of Disipal
Tell your doctor or pharmacist if you have recently taken any other medicines, even those without a prescription.
The association with other psychotropic drugs requires particular caution and vigilance on the part of the physician to avoid unexpected undesirable effects from interaction.
Increased mutual toxicity has been reported with the concomitant use of orphenadrine and dextrropropoxyphene. Therefore in this case reduce the dosage or stop the administration of one of the two drugs. The concomitant administration of other antimuscarinics may lead to an increase in undesirable effects.
Warnings It is important to know that:
Since the product can cause drowsiness and modify reaction times, those who might drive vehicles of any kind or wait for risky operations or otherwise require integrity of the degree of vigilance must be warned of this.
Caution is required in the treatment of subjects with tachycardia or cardiac arrhythmias.
In patients who smoke twenty or more cigarettes a day, prolonged use of the product may increase the risk of developing lung cancer.
Administer with caution in patients with difficulty in urination, during pregnancy and lactation, and in the presence of cardiovascular disease and hepatic or renal impairment. Administer with caution in elderly patients, as they may prove more predisposed to the onset of undesirable effects at doses optimal clinics. Avoid abrupt discontinuation of treatment. Orphenadrine can be a drug of potential abuse.
Pregnancy and breastfeeding
Pregnancy
Ask your doctor or pharmacist for advice before taking any medicine. Experimentation on animals did not show embryotoxic and teratogenic effects.
Feeding time
However, as with all drugs, caution is advisable during pregnancy and breastfeeding and it is advisable to evaluate any risks with the expected benefit. Therefore, the use of Disipal must be established by the doctor in cases of real need.
Effects on ability to drive and use machines
Since the product can cause drowsiness and modify reaction times, those who may drive vehicles of any kind or wait for risky operations or otherwise require integrity of the degree of vigilance must be warned of this.
Important information about some of the ingredients
Disipal contains sucrose, so if you have been told by your doctor that you have intolerance to some sugars, contact your doctor before taking this medicine.
Dosage and method of use How to use Disipal: Dosage
- Parkinson's disease: start with 2-3 tablets a day and methodically increase (1 tablet every 3 days) until the optimal effect is achieved. The optimal dosage is determined individually and is usually 4-5 tablets a day. The doctor's judgment can be raised up to 6-8 tablets per day The switch from other antiparkinsonian preparations with anticholinergic activity to Disipal should be done by gradually replacing (1 tablet at a time every 3 days) the Disipal preparation used previously.
- Side effects and neuroleptic extrapyramidal syndrome: 2 to 6 tablets per day, adjusting the dosage case by case.
- Dizzy syndromes: start with 1 tablet per day, gradually increasing to 3 tablets per day depending on the severity of the symptoms.
- Contractures of the skeletal muscles: in most cases the dosage of 3 tablets per day is sufficient.
Overdose What to do if you have taken too much Disipal
In case of accidental ingestion / intake of an excessive dose of Disipal, notify your doctor immediately or go to the nearest hospital.
If you have any questions about the use of Disipal ask your doctor or pharmacist.
There are no specific antidotes to orphenadrine hydrochloride. Establish targeted therapeutic measures against those symptoms due to excessive central anticholinergic activity.
Side Effects What are the side effects of Disipal
Like all medicines, Disipal can cause side effects, although not everybody gets them. Dry mouth and accommodation disturbances may occur occasionally as well as insomnia, somnolence, lightheadedness. These disturbances disappear spontaneously or by reducing the dosage.
At high doses, on the other hand, other symptoms may be observed, such as tachycardia, asthenia, nausea, vomiting, headache, dizziness, constipation, hypersensitivity reactions, itching, hallucinations, tremors, increased ocular tension. Occasionally, especially in the elderly, mental confusion and disorientation may occur. Common side effects are a sense of instability and gastrointestinal disturbances. Uncommon side effects are confusion, nervousness, euphoria, sedation, convulsions and urinary retention, memory disturbances rarely occur.
Compliance with the instructions contained in the package leaflet reduces the risk of undesirable effects. If any of the side effects gets serious or if you notice any side effects not described in this leaflet, please tell your doctor.
Expiry and Retention
EXPIRY: see the expiry date indicated on the package. The date refers to the product in intact packaging, properly stored.
Warning: do not use the medicine after the expiry date indicated on the package.
Keep this medicine out of the reach and sight of children.
Medicines should not be disposed of via wastewater or household waste. Ask your pharmacist how to dispose of medicines you no longer use. This will help protect the environment.
Composition and pharmaceutical form
Composition
Each tablet contains:
Active ingredient: orphenadrine hydrochloride 50 mg. Excipients: microgranular cellulose, microgranular corn starch, stearic acid, magnesium stearate, amorphous silica; excipients for sugaring: shellac, acacia, talc, beta-carotene E160a, sucrose.
Pharmaceutical form and content
Coated tablets - Box of 50 tablets
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
DISIPAL 50 MG COATED TABLETS
02.0 QUALITATIVE AND QUANTITATIVE COMPOSITION
Each tablet contains: orphenadrine hydrochloride 50 mg.
For the full list of excipients, see section 6.1
03.0 PHARMACEUTICAL FORM
Coated tablets.
04.0 CLINICAL INFORMATION
04.1 Therapeutic indications
1. Parkinson's disease and syndrome
2. Side effects and neuroleptic extrapyramidal syndrome
3. Dizzy syndromes
4. Spastic and painful contractures of the skeletal muscles.
04.2 Posology and method of administration
1. Parkinson's disease: start with 2-3 tablets per day and methodically increase (1 tablet every 3 days) until the optimal effect is achieved. The optimal dosage is determined individually and is generally 4-5 tablets per day In the opinion of the doctor it can be increased up to 6-8 tablets per day The switch from other antiparkinsonian preparations with anticholinergic activity to Disipal should be done by gradually replacing (1 tablet at a time every 3 days) the Disipal preparation used previously.
2. Side effects and neuroleptic extrapyramidal syndrome: 2 to 6 tablets per day, adjusting the dosage case by case.
3. Dizziness syndromes: start with 1 tablet per day, gradually increasing to 3 tablets per day depending on the severity of the symptoms.
4. Skeletal muscle contractures: in most cases the dosage of 3 tablets per day is sufficient.
04.3 Contraindications
Hypersensitivity to the active substance or to any of the excipients.
Glaucoma, prostatic hypertrophy, gastrointestinal obstruction, intestinal obstruction or urinary retention of various causes, stenosing peptic ulcer, cardiospasm, myasthenia gravis, history of drug hypersensitivity, tardive dyskinesia and porphyria.
04.4 Special warnings and appropriate precautions for use
Any increases or decreases in the daily doses of Disipal should be done gradually over a few days.
Due to the presence of beta-carotene in the composition, prolonged use of the product may increase the risk of lung cancer in heavy smokers (twenty or more cigarettes a day).
Administer with caution in patients with difficulty in urination, during pregnancy and lactation, and in the presence of cardiovascular disease and hepatic or renal impairment. Administer with caution in elderly patients, as they may prove more predisposed to the onset of undesirable effects at doses optimal clinics. Avoid abrupt discontinuation of treatment. Orphenadrine can be a drug of potential abuse.
Important information about some of the ingredients
Disipal contains sucrose, therefore patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption, or sucrase isomaltase insufficiency, should not take this medicine.
04.5 Interactions with other medicinal products and other forms of interaction
The association with other psychotropic drugs requires particular caution and vigilance on the part of the physician to avoid unexpected undesirable effects from interaction.
Increased mutual toxicity has been reported with concomitant use of orphenadrine and dextrropropoxyphene, so in this case reduce the dosage or discontinue administration of either drug.
The concomitant administration of other antimuscarinics may lead to an increase in undesirable effects.
04.6 Pregnancy and lactation
Experimentation on animals did not show embryotoxic and teratogenic effects.
However, as with all drugs, caution is advisable during pregnancy and breastfeeding and it is advisable to weigh any risks with the expected benefit.
Therefore, the use of Disipal must be established by the doctor in cases of real need.
04.7 Effects on ability to drive and use machines
Since the product can cause drowsiness and modify reaction times, those who may drive vehicles of any kind or wait for risky operations or otherwise require integrity of the degree of vigilance must be warned of this.
04.8 Undesirable effects
* These disorders disappear spontaneously or by reducing the dosage.
§ Observed in high doses.
° Observed especially in elderly subjects.
04.9 Overdose
There are no specific antidotes to orphenadrine hydrochloride.
Establish targeted therapeutic measures against those symptoms due to excessive central anticholinergic activity.
05.0 PHARMACOLOGICAL PROPERTIES
05.1 Pharmacodynamic properties
Pharmacotherapeutic group: ethers chemically related to antihistamines, ATC code N04AB02
Pharmacological studies in vitro and in vivo have shown that orphenadrine hydrochloride has a powerful anticholinergic activity that occurs mainly at the diencephalic level. The spasmolytic (parasympatholytic) action of orphenadrine is 2 to 4 times greater than that exerted in same experimental conditions from diphenhydramine while its antihistamine activity is much weaker. The peripheral parasympatholytic activity of orphenadrine is weaker than that of atropine. Like scopolamine, orphenadrine blocks the muscarinic receptors of striatal acetylcholine and inhibits the active reuptake of dopamine, thereby enhancing the activity of L-DOPA when the two drugs are administered in combination. on brain biochemistry, orphenadrine has been shown to reduce acetylcholine levels in the rat brain. This activity accompanies the anticholinergic receptor activity. Orphenadrine inhibits the reuptake of biogenic amines (dopamine, serotonin, noradrenaline) with consequent improvement of nerve transmission in the affected brain areas. The enhancement of serotoninergic and noradrenergic activity by orphenadrine is important not only in relation to " antiparkinsonian effect but also to the psychoanaleptic one observed in man. Orphenadrine is also indicated as antivertigenic as it abolishes the hyperactivity of the structures and nervous pathways involved in balance and orientation, as well as as a decontracting of the skeletal muscles.
05.2 "Pharmacokinetic properties
Orphenadrine hydrochloride, administered orally, is rapidly absorbed from the intestine; the amount of orphenadrine that reaches the systemic circulation is estimated to be about 70% of the administered dose. A "first pass" effect in the liver is responsible for the "first pass" effect in the liver. remaining 30%. Orphenadrine hydrochloride is metabolized in the liver through various biotransformation pathways, the most important of which is undoubtedly that of demethylation by microsomal enzymes. Orphenadrine and its main mono-demethyl metabolite are widely distributed and rapidly in all organs, at concentrations higher than those found in plasma at the same times. Orphenadrine crosses the blood brain barrier and the placental barrier.
Urinary excretion of unchanged orphenadrine ranges from 8% to 30% of the administered dose. Bioavailability studies in humans have shown that after a single dose of orphenadrine hydrochloride (1 50 mg coated tablet), peak plasma levels are reached after 4 hours. After a single oral administration, the terminal phase half-life of elimination is 13 to 20 hours and total body clearance of 37 liters / hour. After repeated administration, orphenadrine levels are 2 to 3 times higher and the half-life is approximately twice as prolonged.
05.3 Preclinical safety data
Subacute and chronic toxicity studies on various animal species (rat, mouse, dog) and by various routes of administration have demonstrated the good tolerability of orphenadrine. Orphenadrine hydrochloride is devoid of embryotoxic and teratogenic effects nor does it exhibit mutagenic activity.
06.0 PHARMACEUTICAL INFORMATION
06.1 Excipients
Microgranular cellulose, microgranular corn starch, stearic acid, magnesium stearate, amorphous silica; excipients for sugaring: shellac, acacia, talc, beta-carotene E160a, sucrose.
06.2 Incompatibility
Not relevant.
06.3 Period of validity
3 years.
06.4 Special precautions for storage
No special storage precautions are required.
06.5 Nature of the immediate packaging and contents of the package
Box of 50 coated tablets (2 blisters of 25 slots each).
06.6 Instructions for use and handling
No special instructions.
07.0 MARKETING AUTHORIZATION HOLDER
Astellas Pharma S.p.A. - Via delle Industrie 1 - 20061 Carugate (Milan)
08.0 MARKETING AUTHORIZATION NUMBER
AIC n.013013026
09.0 DATE OF FIRST AUTHORIZATION OR RENEWAL OF THE AUTHORIZATION
Registration: 2 September 1957 - Renewal of authorization: 1 June 2010
10.0 DATE OF REVISION OF THE TEXT
AIFA determination of 6 August 2010
