tolvon, the forgetted antidepressant drug

Tolvon

mianserin hydrochloride

Uses of Tolvon:

Tolvon is used for the treatment of depression.  Its active substance belongs to the piperazino-azepine group of compounds which are chemically not related to the tricyclic antidepressants (TAD’s).1

This medication is sometimes prescribed for other uses; ask your doctor or pharmacist for more information.1

How to Take Tolvon:

Take this medicine as directed. It can be taken with or without food. A dose lower than the normal maintenance dose may be sufficient for a satisfactory clinical response. Do not stop taking this medicine abruptly without consulting with your doctor.1

Presentation

30mg tablet: white, oval, biconvex, coded CT/7 on one side, ORGANON on the other side.2

Each film-coated tablet contains 30mg of mianserin hydrochloride.2

Actions

Mianserin, the active component of TOLVON, belongs to the piperazino-azepine group of compounds, which are chemically not related to the tricyclic antidepressants (TCAs). Its structure lacks the basic side-chain, which is considered to be responsible for the anticholinergic activity of the TCAs. TOLVON increases central noradrenergic neurotransmission by alph₂-autoreceptor blockade and noradrenaline-reuptake inhibition. In addition, interactions with serotonin receptors in the central nervous system have been found. Human pharmaco-EEG studies have confirmed the antidepressant profile of TOLVON. The antidepressant efficacy of TOLVON has been demonstrated in placebo-controlled trials and has been shown to be similar to other currently used antidepressants. Moreover, it possesses anxiolytic and sleep improving properties, which are of value in treating patients with anxiety or sleep disturbances associated with depressive illness. The histamine H₁ and alpha₁-antagonistic activity of TOLVON is thought to be responsible for its sedative properties.2

TOLVON is well tolerated, also by the elderly and by patients with cardiovascular disease. At therapeutically effective doses TOLVON has virtually no anticholinergic activity and has practically no effect on the cardiovascular system. As compared to the TCAs, it causes less cardiotoxic effects on overdose. TOLVON does not antagonize the action of sympathicomimetic agents and antihypertensive medicines, which interact with adrenergic receptors (e.g. bethanidine) or alpha₂-receptors (e.g. clonidine, methyldopa).2

Pharmacokinetics

After oral administration of TOLVON the active constituent, mianserin is rapidly and well absorbed, reaching peak plasma levels within 3 hours. The bioavailability is approx. 20%. Binding of mianserin to plasma proteins is approx. 95%. The half-life of elimination (21-61 hours) is sufficient to justify once-a-day dosing. Steady-state plasma levels are reached within 6 days. Mianserin is extensively metabolized and eliminated via the urine and faeces within 7-9 days. Major pathways of biotransformtion are demethylation and oxidation, followed by conjugation.2

Warnings and precautions for Tolvon:

• TOLVON may potentiate the central nervous depressant action of alcohol and patients should be advised to avoid taking alcohol during treatment.
• Talk with your physician or pharmacist if you are taking other medications.
• TOLVON, like other antidepressants, may precipitate hypomania in susceptible subjects with bipolar depressive illness. In such a case treatment with TOLVON should be withdrawn.
• In general, depressed patients treated with antidepressants should avoid the performance of such hazardous tasks as driving a motor vehicle or operating machinery.
• When treating patients with diabetes or cardiac, hepatic or renal insufficiency, normal precautions should be exercised and the dosages of any concomitant therapy kept under review. Patients with narrow angle glaucoma or symptoms suggestive of prostatic hypertrophy should also be monitored even though anticholinergic side-effects are not anticipated with TOLVON therapy.2

Administration

The tablets should be taken orally, if necessary with fluid, and swallowed without chewing.

• The daily dose can be taken either in divided doses or preferably (in view of a favourable effect on sleep) as a single dose at night.
• Treatment with an adequate dose should result in a positive response within 2-4 weeks. In case of an insufficient response the dose can be increased. If there is no response within a further 2-4 weeks, then treatment should be stopped.
• It is recommended to maintain antidepressant treatment for 4-6 months after clinical improvement has occurred.
• Abrupt discontinuation of treatment with TOLVON very rarely causes withdrawal symptoms.2

How to Store Tolvon:

Store below 25°C. Keep this medication in the container it came in, tightly closed, and out of the reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom). Throw away any medication that is outdated or no longer needed. Talk to your pharmacist about the proper disposal of your medication.1

Clinical Worsening and Suicide Risk

Patients of any age with Major Depressive Disorder may experience worsening of their depression and/or the emergence of suicidal ideation and behaviour (suicidality), whether or not they are taking antidepressant medications, and this risk may persist until significant remission occurs. Patients should be closely monitored, especially at the beginning of therapy or when the dose is changed, until such improvement occurs.2

There has been a long-standing concern that some antidepressants may have a role in the emergence of suicidality in some patients. The possible risk of increased suicidality in patients applies to all classes of antidepressant medicines, as available data are not adequate to exclude this risk for any antidepressant. Therefore, consideration should be given to changing the therapeutic regimen, including possibly discontinuing the medication, in patients whose depression is persistently worse or whose emergent suicidality is severe, abrupt in onset, or was not part of the patient’s presenting symptoms. Generally, when stopping an antidepressant, doses should be tapered rather than stopped abruptly.2

The following symptoms, anxiety, agitation, panic attacks, insomnia, irritability, hostility (aggressiveness), impulsivity, akathisia (psychomotor restlessness), hypomania and mania, have been reported in adult and paediatric patients being treated with antidepressants for major depressive disorder as well as for other indications, both psychiatric and non-psychiatric. Although a causal link between the emergence of such symptoms and either the worsening of depression and/or the emergence of suicidal impulses has not been established, consideration should be given to changing the therapeutic regimen, including possibly discontinuing the medication, in patients for whom such symptoms are severe, abrupt in onset, or were not part of the patient’s presenting symptoms.2

Because of the possibility of co-morbidity between major depressive disorder and other psychiatric and non-psychiatric disorders, the same precautions observed when treating patients with major depressive disorder should be observed when treating patients with other psychiatric and non-psychiatric disorders.

Mania and Bipolar Disorder

A major depressive episode may be the initial presentation of bipolar disorder. It is generally believed (though not established in controlled trials) that treating such an episode with any antidepressant alone may increase the likelihood of a mixed/manic episode in patients at risk for bipolar disorder. Prior to initiating treatment with an antidepressant, patients should be adequately screened to determine if they are at risk for bipolar disorder. It should be noted that TOLVON is not approved for use in treating bipolar depression.2

• Bone marrow depression, usually presenting as granulocytopenia or agranulocytosis, has been reported during treatment with TOLVON. These reactions have occurred most commonly after 4-6 weeks of treatment and were generally reversible on stopping treatment; they have been observed in all age groups but appear to be more common in the elderly. If a patient shows fever, sore throat, stomatitis or other signs of infection, treatment should be stopped and a full blood count should be obtained.
• TOLVON, like other antidepressants, may precipitate hypomania in susceptible subjects with bipolar depressive illness. In such a case treatment with TOLVON should be discontinued.
• When treating patients with diabetes or cardiac disease, hepatic or renal insufficiency, normal precautions should be exercised and the dosages of any concomitant therapy kept under review.
• Patients with narrow angle glaucoma or symptoms suggestive of prostatic hypertrophy should also be monitored even though anticholinergic side effects are not anticipated with TOLVON therapy.
• Granulocytopenia, agranulocytosis and thrombocytopenia have been reported during treatment with TOLVON. Because most of the cases occurred in the first three months of treatment, the Medicines Adverse Reactions Committee has recommended that there should be intensive clinical monitoring of the patient in the first three months with blood counts at a minimum of once per month. Patients should be warned to report symptoms or signs of sore throat, mouth ulcers, bowel upset or fever, to stop the medication immediately and to seek a consultation with the prescribing doctor.
• Treatment should be discontinued if jaundice occur.
• Treatment should be discontinued if convulsions occur.2

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