Active ingredients: Canrenone
LUVION 50 mg Tablets
LUVION 100 mg Capsules, hard
Luvion package inserts are available for pack sizes: - LUVION 50 mg Tablets, LUVION 100 mg Capsules, hard
- LUVION 200 mg / 2ml powder and solvent for solution for injection for intravenous use
Why is Luvion used? What is it for?
PHARMACOTHERAPEUTIC CATEGORY
Potassium sparing diuretics - Aldosterone antagonists.
THERAPEUTIC INDICATIONS
Primary hyperaldosteronism, edematous states due to secondary hyperaldosteronism (congestive heart failure, liver cirrhosis in the ascitic phase, nephrotic syndrome) and essential arterial hypertension where other therapies have not been sufficiently effective or tolerated
Contraindications When Luvion should not be used
Severe hyperkalaemia or hyponatremia. Severe renal insufficiency. Hypersensitivity to the active substance or to any of the excipients.
Precautions for use What you need to know before taking Luvion
Since hyperkalaemia, hyponatremia, azotemic elevations, states of metabolic acidosis can occur during the treatment, it is necessary to check the blood levels of sodium, potassium, chlorine and the alkaline reserve frequently. In the case of surgery, these checks must be performed before the surgery itself. Treatment must be stopped when the sodaemia is lower than 126 mEq / I and the potassium level is higher than 5 mEq / I.
A potassium-rich diet should be avoided during treatment.
In case of concomitant treatment with ACE inhibitors, frequent monitoring of blood potassium levels is recommended.
Interactions Which drugs or foods can change the effect of Luvion
Antihypertensive drugs, especially if ganglionplegic, can be enhanced by the simultaneous administration of the product so that its dosage needs to be adjusted.
Warnings It is important to know that:
Pregnancy and lactation: in pregnant women and in very early childhood, the product should be administered in cases of recognized and elective indication, under the direct supervision of the doctor.
Effects on ability to drive and use machines: The drug does not affect the ability to drive or use machines.
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.
In case of ascertained intolerance to sugars, contact your doctor before taking this medicine.
Dosage and method of use How to use Luvion: Dosage
Adults
In most cases, 50-200 mg per day are sufficient, divided into one or more daily administrations. In severe or resistant cases, this dosage can be increased to 300 mg or more, according to medical prescription.
Overdose What to do if you have taken too much Luvion
The riskiest consequences of overdosing are hyponatremia and hyperkalaemia; the former is characterized by dry mouth, thirst, drowsiness. of dangerous heart rhythms. Hyperkalaemia can be treated promptly by intravenous administration of glucose (20-50%) and insulin (0.25 to 0.5 units per g of glucose). This is a temporary countermeasure, to be repeated if necessary.
Side Effects What are the side effects of Luvion
Many of the adverse reactions listed below are reversible and / or respond to dose reduction.
The reactions listed below are listed in order of decreasing frequency of occurrence: very common (> 1/10), common (> 1/100, 1 / 1,000, 1 / 10,000, <1 / 1,000), very rare (<1 /10,000).
Central and peripheral nervous system disorders
Uncommon: temperature rises, tendency to ataxia.
Rare: somnolence.
Disorders of the digestive system
Rare: nausea, cramp-like abdominal pain.
Skin disorders
Uncommon: allergic rash.
Disorders of the reproductive system
Uncommon: gynecomastia, mild androgenic effects (hirsutism), transient libido disturbances, menstrual irregularities.
Compliance with the instructions contained in the package leaflet reduces the risk of undesirable effects.
It is important to inform the doctor or pharmacist of any undesirable effect, even if not described in the package leaflet.
Expiry and Retention
Check the expiration date indicated on the package.
The expiry date refers to the product in intact packaging, correctly stored. Warning: do not use the medicine after this date.
LUVION 100 mg Capsules, hard: No special storage precautions.
LUVION 50 mg Tablets: Do not store above 25 ° C
COMPOSITION
LUVION 50 mg Tablets:
One tablet contains:
Active ingredient: canrenone 50 mg.
Excipients: lactose monohydrate; cornstarch; macrogol 4000; colloidal silica; magnesium stearate
LUVION100 mg Hard capsules:
One capsule contains:
Active ingredient: canrenone 100 mg.
Excipients: lactose monohydrate; cornstarch; macrogol 4000; colloidal silica; magnesium stearate. Composition of the containing capsule: gelatin; titanium dioxide; yellow iron oxide (E172); indigo carmine (E132).
PHARMACEUTICAL FORM AND CONTENT
LUVION 50 mg Tablets: pack of 20 or 40 tablets.
LUVION 100 mg Hard capsules: pack of 10 or 20 capsules.
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
LUVION
02.0 QUALITATIVE AND QUANTITATIVE COMPOSITION
LUVION 50 mg Tablets
One tablet contains:
Active principle: canrenone 50 mg.
LUVION 100 mg Capsules, hard
One capsule contains:
Active principle: 100 mg canrenone.
LUVION 200mg / 2ml powder and solvent for solution for injection for intravenous use
One bottle contains:
Active principle: potassium canrenoate 200 mg.
For excipients, see 6.1.
03.0 PHARMACEUTICAL FORM
Tablets.
Hard capsules.
Powder and solvent for solution for injection for intravenous use.
04.0 CLINICAL INFORMATION
04.1 Therapeutic indications
LUVION 50 mg Tablets and LUVION 100 mg Capsules, hard
Primary hyperaldosteronism, edematous states due to secondary hyperaldosteronism (congestive heart failure, liver cirrhosis in the ascitic phase, nephrotic syndrome) and essential arterial hypertension where other therapies have not been sufficiently effective or tolerated.
LUVION 200 mg / 2 ml powder and solvent for solution for injection for intravenous use
LUVION 200 mg / 2 ml powder and solvent for solution for injection for intravenous use is indicated in all those situations where intravenous administration is required, in particular it is suitable for use in intensive care units and hospitals.
04.2 Posology and method of administration
Adults
LUVION 50 mg Tablets
LUVION 100 mg Capsules, hard
Orally, in most cases 50-200 mg per day are sufficient, divided into one or more daily administrations. In the most severe or resistant cases, this dosage can be increased to 300 mg or more according to medical prescription.
LUVION 200 mg / 2 ml powder and solvent for solution for injection for intravenous use
Intravenously, the dosage should be adjusted by the attending physician according to the patient's condition and response to therapy. In general, the useful doses are between 200 and 600 mg / day (1-3 bottles) intravenously. It is advisable not to exceed the daily dosage of 800 mg. The injection should be made slowly or preferably in perfusion with 5% glucose solution or physiological solution. In the case of direct intravenous injection it is advisable not to inject more than 2 bottles at a time. For any associated treatments, depending on the indications (diuretics, beta-blockers , etc.), the additive effects must be taken into account in the dosage choice.
Shake well during preparation and before use.
04.3 Contraindications
Severe hyperkalaemia or hyponatremia, severe renal insufficiency, hypersensitivity to the active substance or to any of the excipients.
04.4 Special warnings and appropriate precautions for use
Since hyperkalaemia, hyponatremia, azotemic increases, states of metabolic acidosis can occur during the treatment, it is necessary to check the blood levels of sodium, potassium, chlorine and the alkaline reserve frequently. In the event of surgery, these checks must be performed before the surgery itself. Treatment must be stopped when sodiumemia is less than 126 mEq / l and potassium is greater than 5 mEq / l.
A potassium-rich diet should be avoided during treatment.
In case of concomitant treatment with ACE inhibitors, frequent monitoring of blood potassium levels is recommended.
Luvion tablets and Luvion hard capsules contain lactose and are therefore not suitable for people with lactase deficiency, galactosemia or glucose / galactose malabsorption syndrome.
Although very rarely, local disturbances (pain near the injection site, paraesthesia) may occur with Luvion powder and solvent for solution for injection for intravenous use and can be completely avoided by administration by drip.
04.5 Interactions with other medicinal products and other forms of interaction
Antihypertensive drugs, especially if ganglionic, can be enhanced by the simultaneous administration of the product, so it is necessary to adjust the dosage.
04.6 Pregnancy and lactation
In women who are pregnant, breastfeeding and in very early childhood, the product should be administered in cases of recognized and elective indication, under the direct supervision of the doctor.
04.7 Effects on ability to drive and use machines
The drug does not affect the ability to drive or use machines.
04.8 Undesirable effects
Many of the adverse reactions listed below are reversible and / or respond to dose reduction.
The reactions listed below are listed in order of decreasing frequency of occurrence: very common (> 1/10), common (> 1/100, 1 / 1,000, 1 / 10,000,
Central and peripheral nervous system disorders
Uncommon: temperature rises, tendency to ataxia.
Rare: somnolence.
Disorders of the digestive system
Rare: nausea, cramp-like abdominal pain.
Skin disorders
Uncommon: allergic rash.
Disorders of the reproductive system
Uncommon: gynecomastia, mild androgenic effects (hirsutism), transient libido disturbances, menstrual irregularities.
04.9 Overdose
The riskiest consequences of overdosing are hyponatremia and hyperkalaemia; the former is characterized by dry mouth, thirst, drowsiness. of dangerous heart rhythms. Hyperkalaemia can be treated promptly by intravenous administration of glucose (20-50%) and insulin (0.25 to 0.5 units per g of glucose).This is a temporary countermeasure, to be repeated in cases of need.
05.0 PHARMACOLOGICAL PROPERTIES
05.1 Pharmacodynamic properties
Pharmacotherapeutic group: potassium-sparing drugs - aldosterone antagonists.
LUVION 50 mg Tablets and LUVION 100 mg Capsules, hard:
ATC code: C03DA03.
LUVION 200 mg / 2 ml powder and solvent for solution for injection for intravenous use:
ATC code: C03DA02.
Canrenone is a synthetic compound that chemically corresponds to the gamma-lactone of 17beta-hydroxy-3-oxo-17alpha-pregna-4,6-diene-21-carboxylic acid. Structurally it differs from spironolactone due to the absence of the thioacetyl group in position 7 and the presence of a double bond in position 6-7. The canrenone, for the "structural analogy with" aldosterone, acts competitively with the latter by displacing it from the receptor sites (binding sites) that are located in the distal part of the renal tubule and the collecting duct, thus affecting the fine mechanisms of regulation of the character of the urine that is located in these tracts. Canrenone therefore acts by favoring the elimination of sodium and water and limiting the excretion of potassium, so it is indicated in all states of hyperaldosteronism and whenever it is desired to obtain the urinary elimination of sodium without concomitant potassium depletion. The rarity of secondary sexual effects after the administration of canrenone, resulting from the clinical studies carried out so far (interesting for any protracted treatments), has led some authors to assume that canrenone does not cause the destruction of cytochrome P450 at the testicular level, therefore one of the supposed mechanisms of explication of the antiandrogenic activity would be missing
of spironolactone: inhibition of testosterone synthesis. The depletion of water and sodium after administration of canrenone is generally gradual. It is noted that it is not accompanied by potassium loss, and also from the clinical studies carried out so far it is not accompanied, in analogy with spironolactone, by an increase in blood sugar, uricemia and plasma lipids.
05.2 Pharmacokinetic properties
Distribution
Research on the tissue distribution of canrenone has shown that the highest concentrations are found in the liver and kidney.
Metabolism
Canrenone is formed "in vivo" by hydrolysis of the acetyl-mercaptan group of spironolactone. The data relating to the experiences of pharmacokinetics in dogs and humans show that only a part of spironolactone is transformed into canrenone, a product of biotransformation that is certainly active. A part of spironolactone (about 20%) instead undergoes hydroxylation and sulfurization processes , etc., with the formation of secondary metabolites.
Elimination
The t½ of the canrenone is around 18 hours. The excretion in 72 hours takes place partly by the urinary route and partly by the fecal route.
05.3 Preclinical safety data
Toxicity after single and repeated administration
Acute and chronic toxicity studies, conducted on different animal species, show a clear separation between pharmacologically active and toxic dosages. In particular, the LD50 in acute oral treatment was 1370 mg / kg in mice, 1200 mg / kg in rats. Prolonged treatment did not affect the behavior of the animals. There were no significant changes in haematological values between the control groups and the groups treated with canrenone.
06.0 PHARMACEUTICAL INFORMATION
06.1 Excipients
LUVION 50 mg Tablets
Lactose monohydrate, corn starch, macrogol 4000, colloidal silica, magnesium stearate.
LUVION 100 mg Capsules, hard
Lactose monohydrate, corn starch, macrogol 4000, colloidal silica, magnesium stearate.
Composition of the capsule: gelatin, titanium dioxide, indigo carmine (E132), yellow iron oxide (E172).
LUVION 200 mg / 2 ml powder and solvent for solution for injection for intravenous use
One bottle of powder contains: 10 mg trometamol.
One ampoule of solvent contains: 2 ml water for injections.
06.2 Incompatibility
None known.
06.3 Period of validity
3 years.
06.4 Special precautions for storage
Luvion 100 mg Hard capsules, LUVION 200 mg / 2 ml, powder and solvent for solution for injection for intravenous use:
No special storage precautions.
Luvion 50 mg Tablets:
Do not store above 25 ° C.
06.5 Nature of the immediate packaging and contents of the package
Luvion 50 mg Tablets: carton containing two or four aluminum / PVDC / PVC blisters of 10 tablets each.
Luvion 100 mg Hard capsules: carton containing one or two aluminum / polyethylene blisters of 10 capsules each.
LUVION 200 mg / 2 ml, powder and solvent for solution for injection for intravenous use: carton containing 6 bottles of 200 mg of powder + 6 solvent ampoules of 2 ml.
06.6 Instructions for use and handling
No particular education.
07.0 MARKETING AUTHORIZATION HOLDER
Therabel GiEnne Pharma S.p.A. - Via Robert Koch, 1/2 - 20152 Milan.
08.0 MARKETING AUTHORIZATION NUMBER
Luvion 50 mg Tablets - 20 Tablets: A.I.C. N ° 024273082 *
Luvion50 mg Tablets - 40 Tablets: A.I.C. N ° 024273094
Luvion 100 mg Hard capsules - 10 capsules: A.I.C. N ° 024273043 *
Luvion 100 mg Hard Capsules - 20 Capsules: A.I.C. N ° 024273056
LUVION 200 mg / 2 ml, powder and solvent for solution for injection for intravenous use, 6 vials of 200 mg powder + 6 vials of 2 ml solvent: A.I.C. N ° 024273070
09.0 DATE OF FIRST AUTHORIZATION OR RENEWAL OF THE AUTHORIZATION
First authorization :
Luvion 50 mg Tablets - 20 Tablets: 04/04/2003
Luvion 50 mg Tablets - 40 Tablets: 04/04/2003
Luvion 100 mg Capsules, hard - 10 capsules: 08/24/1982
Luvion 100 mg Capsules, hard - 20 capsules: 08/24/1982
LUVION 200 mg / 2 ml, powder and solvent for solution for injection for intravenous use, 6 vials of 200 mg powder + 6 vials of 2 ml solvent: 6/12/2000
Renewal : 1/06/2010
10.0 DATE OF REVISION OF THE TEXT
October 2013
