Tasmar.eu

NAME OF THE MEDICINAL PRODUCT

Tasmar 100 mg film-coated tablets ▼
2.
QUALITATIVE AND QUANTITATIVE COMPOSITION

Each film-coated tablet contains 100 mg tolcapone.
Excipients: Each tablet contains 7.5 mg lactose.
For a full list of excipients, see section 6.1
3. PHARMACEUTICAL

Film-coated tablet.
Pale to light yellow, hexagonal, biconvex, film-coated tablet. “TASMAR” and “100” are
engraved on one side.
4. CLINICAL
PARTICULARS

4.1 Therapeutic
indications

Tasmar is indicated in combination with levodopa/benserazide or levodopa/carbidopa
for use in patients with levodopa-responsive idiopathic Parkinson’s disease and motor
fluctuations, who failed to respond to or are intolerant of other catechol-O-methyl
transferase COMT inhibitors (see section 5.1). Because of the risk of potentially fatal,
acute liver injury, Tasmar should not be considered as a first-line adjunct therapy to
levodopa/benserazide or levodopa/carbidopa (see sections 4.4 and 4.8).
Since Tasmar should be used only in combination with levodopa/benserazide and
levodopa/carbidopa, the prescribing information for these levodopa preparations is also
applicable to their concomitant use with Tasmar.
4.2 Posology and method of administration

The administration of Tasmar is restricted to prescription and supervision by physicians
experienced in the management of advanced Parkinson's disease.
The first dose of the day of Tasmar should be taken together with the first dose of the
day of a levodopa preparation, and the subsequent doses should be given
approximately 6 and 12 hours later. Tasmar may be taken with or without food (see
section 5.2).
The recommended dose of Tasmar is 100 mg three times daily, always as an adjunct
to levodopa/benserazide or levodopa/carbidopa therapy. Only in exceptional
circumstances, when the anticipated incremental clinical benefit justifies the increased
risk of hepatic reactions, should the dose be increased to 200 mg three times daily (see
sections 4.4 and 4.8). If substantial clinical benefits are not seen within 3 weeks of the
initiation of the treatment (regardless of dose) Tasmar should be discontinued.
The maximum therapeutic dose of 200 mg three times daily should not be exceeded,
as there is no evidence of additional efficacy at higher doses.
Liver function should be checked before starting treatment with Tasmar and then
monitored every 2 weeks for the first year of therapy, every 4 weeks for the next 6
months and every 8 weeks thereafter. If the dose is increased to 200 mg tid, liver
enzyme monitoring should take place before increasing the dose and then be
reinitiated following the same sequence of frequencies as above (see sections 4.4 and
4.8).
Tasmar treatment should also be discontinued if ALT (alanine amino transferase)
and/or AST (aspartate amino transferase) exceed the upper limit of normal or
symptoms or signs suggest the onset of hepatic failure (see section 4.4).

Levodopa adjustments during Tasmar treatment:
As Tasmar decreases the breakdown of levodopa in the body, side effects due to
increased levodopa concentrations may occur when beginning Tasmar treatment. In
clinical trials, more than 70 % of patients required a decrease in their daily levodopa
dose if their daily dose of levodopa was >600 mg or if patients had moderate or severe
dyskinesias before beginning treatment.
The average reduction in daily levodopa dose was about 30 % in those patients requiring a levodopa dose reduction. When beginning Tasmar, all patients should be informed of the symptoms of excessive levodopa dosage and what to do if it occurs. Levodopa adjustments when Tasmar is discontinued:
The following suggestions are based on pharmacological considerations and have not
been evaluated in clinical trials. Levodopa dose should not be decreased when Tasmar
therapy is being discontinued due to side effects related to too much levodopa.
However, when Tasmar therapy is being discontinued for reasons other than too much
levodopa, the levodopa dose may have to be increased to levels equal to or greater
than before initiation of Tasmar therapy, especially if the patient had large decreases in
levodopa when starting Tasmar. In all cases, patients should be educated on the
symptoms of levodopa under-dose and what to do if it occurs. Adjustments in levodopa
are most likely to be required within 1-2 days of Tasmar discontinuation.
Patients with impaired renal function (see section 5.2): No dose adjustment of Tasmar
is recommended for patients with mild or moderate renal impairment (creatinine
clearance of 30 ml/min or greater). Patients with severe renal impairment (creatinine
clearance < 30 ml/min) should be treated with caution. No information on the
tolerability of tolcapone in these populations is available (see section 5.2).
Patients with hepatic impairment (see section 4.3): Tasmar is contraindicated for
patients with liver disease or increased liver enzymes.
Elderly patients: No dose adjustment of Tasmar is recommended for elderly patients.
Children and adolescents: Tasmar is not recommended for use in children below the
age of 18 due to insufficient data on safety or efficacy. There is no relevant indication
for use in children and adolescents.

Method of administration

Tasmar is administered orally three times daily.
Tasmar may be taken with or without food (see section 5.2).
Tasmar tablets are film-coated and should be swallowed whole because tolcapone has
a bitter taste.
Tasmar can be combined with all pharmaceutical formulations of levodopa/benserazide
and levodopa/carbidopa (see also section 4.5).
4.3 Contraindications
• Hypersensitivity to tolcapone or any of its other ingredients. • Evidence of liver disease or increased liver enzymes. • Severe dyskinesia. • A previous history of Neuroleptic Malignant Syndrome (NMS) Symptom Complex and /or non-traumatic Rhabdomyolysis or Hyperthermia. • Treatment with non-selective monoamino oxidase (MAO) inhibitors.
4.4 Special warnings and precautions for use

Tasmar therapy should only be initiated by physicians experienced in the
management of advanced Parkinson’s disease, to ensure an appropriate risk-
benefit assessment. Tasmar should not be prescribed until there has been a
complete informative discussion of the risks with the patient.
Tasmar should be discontinued if substantial clinical benefits are not seen within
3 weeks of the initiation of the treatment regardless of dose.
Liver Injury:
Because of the risk of rare but potentially fatal acute liver injury, Tasmar is only
indicated for use in patients with levodopa-responsive idiopathic Parkinson’s
disease and motor fluctuations, who failed to respond to or are intolerant of
other COMT inhibitors. Periodic monitoring of liver enzymes cannot reliably
predict the occurrence of fulminant hepatitis. However, it is generally believed
that early detection of medicine-induced hepatic injury along with immediate
withdrawal of the suspect medication enhances the likelihood for recovery. Liver
injury has most often occurred between 1 month and 6 months after starting
treatment with Tasmar. Additionally late onset hepatitis after approximately 18
months of treatment has been reported rarely.
It should also be noted that female patients may have a higher risk of liver injury
(see section 4.8).
Before starting treatment: If liver function tests are abnormal or there are signs
of impaired liver function, Tasmar should not be prescribed. If Tasmar is to be
prescribed, the patient should be informed about the signs and symptoms which
may indicate liver injury, and to contact the physician immediately.
During treatment: Liver function should be monitored every 2 weeks for the first
year of therapy, every 4 weeks for the next 6 months and every 8 weeks
thereafter. If the dose is increased to 200 mg tid, liver enzyme monitoring should
take place before increasing the dose and then be reinitiated following the
sequence of frequencies as above. Treatment should be immediately
discontinued if ALT and/or AST exceed the upper limit of normal or if symptoms
or signs suggesting the onset of hepatic failure (persistent nausea, fatigue,
lethargy, anorexia, jaundice, dark urine, pruritus, right upper quadrant
tenderness) develop.

If treatment is discontinued: Patients who show evidence of acute liver injury
while on Tasmar and are withdrawn from the medicinal product may be at

increased risk for liver injury if Tasmar is re-introduced. Accordingly, such
patients should not be considered for retreatment.
Neuroleptic Malignant Syndrome (NMS):
In Parkinson`s patients, NMS tends to occur when discontinuing or stopping
dopaminergic-enhancing medications. Therefore, if symptoms occur after
discontinuing Tasmar, physicians should consider increasing the patient’s
levodopa dose (see section 4.2).
Isolated cases consistent with NMS have been associated with Tasmar
treatment. Symptoms have usually onset during Tasmar treatment or shortly
after Tasmar has been discontinued. NMS is characterised by motor symptoms
(rigidity, myoclonus and tremor), mental status changes (agitation, confusion,
stupor and coma), elevated temperature, autonomic dysfunction (labile blood
pressure, tachycardia) and elevated serum creatine phosphokinase (CPK) which
may be a consequence of myolysis. A diagnosis of NMS should be considered
even if not all the above findings are present. Under such a diagnosis Tasmar
should be immediately discontinued and the patient should be followed up
closely.
Before starting treatment: To reduce the risk of NMS, Tasmar should not be
prescribed for patients with severe dyskinesia or a previous history of NMS
including rhabdomyolysis or hyperthermia (see section 4.3). Patients receiving
multiple medications with effects on different central nervous system (CNS)
pathways (e.g. antidepressants, neuroleptics, anticholinergics) may be at greater
risk of developing NMS.

Patients treated for Parkinson’s Disease with medications that increase central
dopaminergic tone, especially at high doses, have been reported as exhibiting
increased libido, hypersexuality and pathological gambling, generally reversible upon
reduction of the dose or treatment discontinuation.
Dyskinesia, nausea and other levodopa-associated adverse reactions: Patients may
experience an increase in levodopa-associated adverse reactions. Reducing the dose
of levodopa (see section 4.2) may often mitigate these adverse reactions.
Diarrhoea: In clinical trials, diarrhoea developed in 16 % and 18 % of patients receiving
Tasmar 100 mg tid and 200 mg tid respectively, compared to 8 % of patients receiving
placebo. Diarrhoea associated with Tasmar usually began 2 to 4 months after initiation
of therapy. Diarrhoea led to withdrawal of 5 % and 6 % of patients receiving Tasmar
100 mg tid and 200 mg tid respectively, compared to 1 % of patients receiving placebo.
Benserazide interaction: Due to the interaction between high dose benserazide and
tolcapone (resulting in increased levels of benserazide), the prescriber should, until
more experience has been gained, be observant of dose-related adverse reactions
(see section 4.5).
MAO inhibitors: Tasmar should not be given in conjunction with non-selective
monoamine oxidase (MAO) inhibitors (e.g. phenelzine and tranylcypromine). The
combination of MAO-A and MAO-B inhibitors is equivalent to non-selective MAO-
inhibition, therefore they should not both be given concomitantly with Tasmar and
levodopa preparations (see also section 4.5). Selective MAO-B inhibitors should not be
used at higher than recommended doses (e.g. selegiline 10 mg/day) when co-
administered with Tasmar.
Warfarin: Since clinical information is limited regarding the combination of warfarin and
tolcapone, coagulation parameters should be monitored when these drugs are co-
administered.
Special populations: Patients with severe renal impairment (creatinine clearance <30
ml/min) should be treated with caution. No information on the tolerability of tolcapone
in these populations is available (see section 5.2).
Lactose intolerance: Tasmar contains lactose. Patients with hereditary problems of
galactose intolerance, the Lapp lactose deficiency or glucose-galactose malabsorption
should not take this medicine.
4.5 Interaction with other medicinal products and other forms of interaction
Tasmar, as a COMT inhibitor, is known to increase the bioavailability of the co-
adminstered levodopa. The consequent increase in dopaminergic stimulation can lead
to the dopaminergic adverse reactions observed after treatment with COMT inhibitors.
The most common of these are increased dyskinesia, nausea, vomiting, abdominal
pain, syncope, orthostatic complains, constipation, sleep disorders, somnolence,
hallucination.
Levodopa has been associated with somnolence and episodes of sudden sleep onset.
Sudden onset of sleep during daily activities, in some cases without awareness or
warning signs, has been reported very rarely. Patients must be informed of this and
advised to exercise caution while driving or operating machines during treatment with
levodopa. Patients who have experienced somnolence and/or an episode of sudden
sleep onset must refrain from driving or operating machines (see section 4.7).
Furthermore a reduction of levodopa dose or termination of therapy may be
considered.
Catechols and other drugs metabolised by catechol-O-methyltransferase (COMT):
Tolcapone may influence the pharmacokinetics of drugs metabolised by COMT. No
effects were seen on the pharmacokinetics of the COMT substrate carbidopa. An
interaction was observed with benserazide, which may lead to increased levels of
benserazide and its active metabolite. The magnitude of the effect was dependent on
the dose of benserazide. The plasma concentrations of benserazide observed after co-
administration of tolcapone and benserazide-25 mg/levodopa were still within the range
of values observed with levodopa/benserazide alone. On the other hand, after co-
administration of tolcapone and benserazide-50 mg/levodopa the benserazide plasma
concentrations could be increased above the levels usually observed with
levodopa/benserazide alone. The effect of tolcapone on the pharmacokinetics of other
drugs metabolised by COMT such as α-methyldopa, dobutamine, apomorphine,
adrenaline and isoprenaline have not been evaluated. The prescriber should be
observant of adverse reactions caused by putative increased plasma levels of these
drugs when combined with Tasmar.
Effect of tolcapone on the metabolism of other drugs: Due to its affinity for cytochrome
CYP2C9 in vitro, tolcapone may interfere with drugs whose clearance is dependent on
this metabolic pathway, such as tolbutamide and warfarin. In an interaction study,
tolcapone did not change the pharmacokinetics of tolbutamide. Therefore, clinically
relevant interactions involving cytochrome CYP2C9 appear unlikely.
Since clinical information is limited regarding the combination of warfarin and
tolcapone, coagulation parameters should be monitored when these drugs are co-
administered.
Drugs that increase catecholamines: Since tolcapone interferes with the metabolism of
catecholamines, interactions with other drugs affecting catecholamine levels are
theoretically possible.
When Tasmar was given together with levodopa/carbidopa and desipramine, there was
no significant change in blood pressure, pulse rate and plasma concentrations of
desipramine. Overall, the frequency of adverse reactions increased slightly. These
adverse reactions were predictable based on the known adverse reactions to each of
the three drugs individually. Therefore, caution should be exercised when potent
noradrenaline uptake inhibitors such as desipramine, maprotiline, or venlafaxine are
administered to Parkinson’s disease patients being treated with Tasmar and levodopa
preparations.
In clinical trials, patients receiving Tasmar/levodopa preparations reported a similar
adverse reaction profile independent of whether or not they were also concomitantly
administered selegiline (a MAO-B inhibitor).
4.6 Pregnancy
lactation

In rats and rabbits, embryo-foetal toxicity was observed after tolcapone administration
(see section 5.3). The potential risk for humans is unknown.
There are no adequate data from the use of tolcapone in pregnant women. Therefore,
Tasmar should be used during pregnancy only if the potential benefit justifies the
potential risk to the foetus.
In animal studies, tolcapone was excreted into maternal milk.
The safety of tolcapone in infants is unknown; therefore, women should not breast-feed
during treatment with Tasmar.
4.7 Effects on ability to drive and use machines

No studies on the effects of Tasmar on the ability to drive and use machines have been
performed.
There is no evidence from clinical studies that Tasmar adversely influences a patient’s
ability to drive and use machines. However patients should be advised that their ability
to drive and operate machines may be compromised due to their Parkinson’s disease
symptoms.
Tasmar, as a COMT inhibitor, is known to increase the bioavailability of the co-
adminstered levodopa. The consequent increase in dopaminergic stimulation can lead
to the dopaminergic side effects observed after treatment with COMT inhibitors.
Patients being treated with Levodopa and presenting with somnolence and/or sudden
sleep episodes must be informed to refrain from driving or engaging in activities where
impaired alertness may put themselves or others at risk of serious injury or death (e.g.
operating machines) until such recurrent episodes and somnolence have resolved (see
also section 4.4).
4.8 Undesirable
The most commonly observed adverse reactions associated with the use of Tasmar, occurring more frequently than in placebo-treated patients are listed in the table below. However, Tasmar, as a COMT inhibitor, is known to increase the bioavailability of the co-adminstered levodopa. The consequent increase in dopaminergic stimulation can lead to the dopaminergic side effects observed after treatment with COMT inhibitors. The most common of these are increased dyskinesia, nausea, vomiting, abdominal pain, syncope, orthostatic complaints, constipation, sleep disorders, somnolence, hallucination. The only adverse reactions commonly leading to discontinuation of Tasmar in clinical trials was diarrhoea (see section 4.4). Very common (>1/10) Common (>1/100 to <1/10) Uncommon (>1/1,000 to < 1/100) Rare (>1/10,000 to <1/1,000) Very rare (<1/10,000), not known (cannot be estimated from the available data) Experience with Tasmar obtained in parallel placebo-controlled randomised studies in patients with Parkinson’s disease is shown in the following table, which lists adverse reactions with a potential relationship to Tasmar. Summary of potentially Tasmar-related adverse reactions, with crude incidence rates for the phase III placebo-controlled studies: System organ class
Incidence
Adverse Events
mediastinal disorders Gastrointestinal disorders System organ class
Incidence
Adverse Events
tissue disorders Renal and urinary disorders Common
Increases to more than three times the upper limit of normal (ULN) in alanine
aminotransferase (ALT) occurred in 1 % of patients receiving Tasmar 100 mg three
times daily, and 3 % of patients at 200 mg three times daily. Increases were
approximately two times more likely in females. The increases usually appeared within
6 to 12 weeks of starting treatment, and were not associated with any clinical signs or
symptoms. In about half the cases, transaminase levels returned spontaneously to
baseline values whilst patients continued Tasmar treatment. For the remainder, when
treatment was discontinued, transaminase levels returned to pre-treatment levels.
Rare cases of severe hepatocellular injury resulting in death have been reported during
marketed use (see section 4.4).
Isolated cases of patients with symptoms suggestive of Neuroleptic Malignant
Syndrome Symptom Complex (see section 4.4) have been reported following
reduction or discontinuation of Tasmar and following introduction of Tasmar when this
was accompanied by a significant reduction in other concomitant dopaminergic
medications. In addition, rhabdomyolysis, secondary to NMS or severe dyskinesia, has
been observed.

Urine discoloration:
Tolcapone and its metabolites are yellow and can cause a
harmless intensification in the colour of the patient’s urine.
4.9 Overdose

Isolated cases of either accidental or intentional overdose with tolcapone tablets have
been reported. However clinical circumstances of these cases were so diverse, that no
general conclusions can be drawn from the cases.
The highest dose of tolcapone administered to humans was 800 mg three times daily,
with and without levodopa coadministration, in a one week study in healthy elderly
volunteers. The peak plasma concentrations of tolcapone at this dose were on average
30 µg/ml (compared to 3 and 6 µg/ml with 100 mg tid and 200 mg tid of tolcapone
respectively). Nausea, vomiting and dizziness were observed, particularly in
combination with levodopa.
Management of overdose: Hospitalisation is advised. General supportive care is
indicated. Based on the physicochemical properties of the compound, haemodialysis is
unlikely to be of benefit.

5. PHARMACOLOGICAL

PROPERTIES

5.1 Pharmacodynamic
properties

Pharmaco-therapeutic group: Anti-Parkinson drugs, other dopaminergic agents, ATC
code: NO4BX01.
Tolcapone is an orally active, selective and reversible catechol-O-methyltransferase
(COMT) inhibitor. Administered concomitantly with levodopa and an aromatic amino
acid decarboxylase inhibitor (AADC-I), it leads to more stable plasma levels of
levodopa by reducing metabolism of levodopa to 3-methoxy-4-hydroxy-L-phenylalanine
(3-OMD).
High levels of plasma 3-OMD have been associated with poor response to levodopa in
Parkinson’s disease patients. Tolcapone markedly reduces the formation of 3-OMD.
Clinical pharmacology

Studies in healthy volunteers have shown that tolcapone reversibly inhibits human
erythrocyte COMT activity after oral administration. The inhibition is closely related to
plasma tolcapone concentration. With 200 mg tolcapone, maximum inhibition of
erythrocyte COMT activity is, on average, greater than 80 %. During dosing with
Tasmar 200 mg three times daily, erythrocyte COMT inhibition at trough is 30 % to
45 %, with no development of tolerance.
Transient elevation above pretreatment levels of erythrocyte COMT activity was
observed after withdrawal of tolcapone. However, a study in Parkinson’s patients
confirmed that after treatment discontinuation there was no significant change in
levodopa pharmacokinetics or in patient response to levodopa compared to
pretreatment levels.
When Tasmar is administered together with levodopa, it increases the relative
bioavailability (AUC) of levodopa approximately two-fold. This is due to a decrease in
clearance in L-dopa resulting in a prolongation of the terminal elimination half-life (t )
of levodopa. In general, the average peak levodopa plasma concentration (Cmax) and the time of its occurrence (tmax) were unaffected. The onset of effect occurs after the first administration. Studies in healthy volunteers and parkinsonian patients have confirmed that the maximum effect occurs with 100 – 200 mg tolcapone. Plasma levels of 3-OMD were markedly and dose-dependently decreased by tolcapone when given with levodopa/AADC-I (aromatic amino acid decarboxylase - inhibitor) (benserazide or carbidopa). Tolcapone’s effect on levodopa pharmacokinetics is similar with all pharmaceutical formulations of levodopa/benserazide and levodopa/carbidopa; it is independent of levodopa dose, levodopa/AADC-I (benserazide or carbidopa) ratio and the use of sustained-release formulations. Clinical studies Double blind placebo controlled clinical studies have shown a significant reduction of approximately 20 % to 30 % in OFF time and a similar increase in ON time, accompanied by reduced severity of symptoms in fluctuating patients receiving Tasmar. Investigator’s global assessments of efficacy also showed significant improvement. A double-blind trial compared Tasmar with entacapone in Parkinson's disease patients who had at least three hours of OFF time per day while receiving optimised levodopa therapy. The primary outcome was the proportion of patients with a 1 or more hour increase in ON time (see Table 1). Table 1: Primary and Secondary Outcome of Double-blind Trial
Entacapone
Primary Outcome
Number (proportion) with ≥1 hour ON time response
Secondary Outcome
primary and secondary outcome
5.2 Pharmacokinetic
properties
In the therapeutic range, tolcapone pharmacokinetics are linear and independent of levodopa/AADC-I (benserazide or carbidopa) coadministration. Absorption: Tolcapone is rapidly absorbed with a tmax of approximately 2 hours. The absolute bioavailability of an oral administration is around 65 %. Tolcapone does not accumulate with three times daily dosing of 100 or 200 mg. At these doses, Cmax is approximately 3 and 6 µg/ml, respectively. Food delays and decreases the absorption of tolcapone, but the relative bioavailability of a dose of tolcapone taken with a meal is still 80 % to 90 %. Distribution: The volume of distribution (Vss) of tolcapone is small (9 l). Tolcapone does not distribute widely into tissues due to its high plasma protein binding (>99.9 %). In
vitro
experiments have shown that tolcapone binds mainly to serum albumin.
Metabolism/Elimination: Tolcapone is almost completely metabolised prior to excretion,
with only a very small amount (0.5 % of dose) found unchanged in urine. The main
metabolic pathway of tolcapone is conjugation to its inactive glucuronide. In addition,
the compound is methylated by COMT to 3-O-methyl-tolcapone and metabolised by
cytochromes P450 3A4 and P450 2A6 to a primary alcohol (hydroxylation of the methyl
group), which is subsequently oxidised to the carboxylic acid. The reduction to a
putative amine, as well as the subsequent N-acetylation, occurs to a minor extent. After
oral administration, 60 % of drug-related material is excreted into urine and 40 % into
faeces.
Tolcapone is a low-extraction-ratio drug (extraction-ratio = 0.15), with a moderate
systemic clearance of about 7 L/h. The t1/2 of tolcapone is approximately 2 hours.

Hepatic impairment: Because of the risk of liver injury observed during post-marketing
use, Tasmar is contraindicated in patients with liver disease or increased liver
enzymes. A study in patients with hepatic impairment has shown that moderate non-
cirrhotic liver disease had no impact on the pharmacokinetics of tolcapone. However, in
patients with moderate cirrhotic liver disease, clearance of unbound tolcapone was
reduced by almost 50 %. This reduction may increase the average concentration of
unbound drug two-fold.

Renal impairment: The pharmacokinetics of tolcapone has not been investigated in
patients with renal impairment. However, the relationship of renal function and
tolcapone pharmacokinetics has been investigated using population pharmacokinetics
during clinical trials. The data of more than 400 patients have confirmed that over a
wide range of creatinine clearance values (30-130 mL/min) the pharmacokinetics of
tolcapone are unaffected by renal function. This could be explained by the fact that only
a negligible amount of unchanged tolcapone is excreted in the urine, and the main
metabolite, tolcapone-glucuronide, is excreted both in urine and in bile (faeces).

5.3 Preclinical safety data

Preclinical data reveal no special hazard for humans based on conventional studies of
safety pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential,
toxicity to reproduction.

Carcinogenesis, mutagenesis:
3 % and 5 % of rats in the mid- and high- dose groups,
respectively, of the 24-month carcinogenicity study were shown to have renal epithelial
tumours (adenomas or carcinomas). However, no evidence of renal toxicity was
observed in the low-dose group. An increased incidence of uterine adenocarcinomas
was seen in the high-dose group of the rat carcinogenicity study. There were no similar
renal findings in the mouse or dogs carcinogenicity studies.
Mutagenesis: Tolcapone was shown not to be genotoxic in a complete series of
mutagenicity studies.
Toxicity to reproduction: Tolcapone, when administered alone, was shown to be neither
teratogenic nor to have any relevant effects on fertility.
6. PHARMACEUTICAL
PARTICULARS

6.1 List of excipients

Tablet core:
Calcium hydrogen phosphate
Microcrystalline cellulose
Polyvidone K30
Sodium starch glycollate
Lactose
Talc
Magnesium stearate.
Film-coat:
Hydroxypropylmethylcellulose
Talc
Yellow iron oxide
Ethylcellulose
Titanium dioxide
Triacetin
Sodium lauryl sulfate
6.2 Incompatibilities

Not applicable

6.3 Shelf


5 years
6.4 Special precautions for storage

This medicinal product does not require any special storage conditions
6.5 Nature and contents of container

Tasmar is available in PVC/PE/PVDC blisters (pack sizes of 30 and 60 film-coated
tablets) and in amber glass bottles without desiccant (pack sizes of 30, 60 and 100
film-coated tablets).
Not all pack sizes may be marketed.
6.6 Special precautions for disposal

No special requirements.
7.
MARKETING AUTHORISATION HOLDER

Meda AB
Pipers väg 2A
S-170 09 Solna
Sweden
8.
MARKETING AUTHORISATION NUMBERS

EU/1/97/044/001-3, 7-8
9.
DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION

Date of first authorisation: 27 August 1997
Renewal of the authorisation: 31 August 2004
Date of latest renewal: 2 October 2009

10. DATE OF REVISION OF THE TEXT
22 January 2009

Source: http://www.tasmar.eu/professionals/pdf/SMPC/PI-Tasmar100mg-en.pdf

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