Parstelin

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Parstelin uses

Parstelin consists of Tranylcypromine Sulfate, Trifluoperazine Hydrochloride.

Tranylcypromine Sulfate:


SUICIDALITY AND ANTIDEPRESSANT DRUGS

Antidepressants increased the risk compared to placebo of suicidal thinking and behavior (suicidality) in children, adolescents, and young adults in short-term studies of major depressive disorder (MDD) and other psychiatric disorders. Anyone considering the use of Parstelin (Tranylcypromine Sulfate) or any other antidepressant in a child, adolescent, or young adult must balance this risk with the clinical need. Short-term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo in adults beyond age 24; there was a reduction in risk with antidepressants compared to placebo in adults aged 65 and older. Depression and certain other psychiatric disorders are themselves associated with increases in the risk of suicide. Patients of all ages who are started on antidepressant therapy should be monitored appropriately and observed closely for clinical worsening, suicidality, or unusual changes in behavior. Families and caregivers should be advised of the need for close observation and communication with the prescriber. Parstelin (Tranylcypromine Sulfate) is not approved for use in pediatric patients.

DESCRIPTION

Chemically, Parstelin (Tranylcypromine Sulfate) is (±)-trans-2-phenylcyclopropylamine sulfate (2:1).

Each round, dark pink, film-coated tablet is debossed with “250” on one side and “K” on the other side and contains Parstelin (Tranylcypromine Sulfate) equivalent to 10 mg of tranylcypromine. Inactive ingredients consist of colloidal silicon dioxide, croscarmellose sodium, dibasic calcium phosphate anhydrous, magnesium stearate, microcrystalline cellulose, talc, and Opadry® II pink 85F14289. Opadry pink is used for purposes of coating and contains the following: FD&C Red # 40, polyethylene glycol 3350, polyvinyl alcohol, talc, and titanium dioxide.

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ACTION

Tranylcypromine is a non-hydrazine monoamine oxidase inhibitor with a rapid onset of activity. It increases the concentration of epinephrine, norepinephrine, and serotonin in storage sites throughout the nervous system and, in theory, this increased concentration of monoamines in the brain stem is the basis for its antidepressant activity. When tranylcypromine is withdrawn, monoamine oxidase activity is recovered in 3 to 5 days, although the drug is excreted in 24 hours.

INDICATIONS

For the treatment of Major Depressive Episode Without Melancholia.

Parstelin (Tranylcypromine Sulfate) should be used in adult patients who can be closely supervised. It should rarely be the first antidepressant drug given. Rather, the drug is suited for patients who have failed to respond to the drugs more commonly administered for depression.

The effectiveness of Parstelin (Tranylcypromine Sulfate) has been established in adult outpatients, most of whom had a depressive illness which would correspond to a diagnosis of Major Depressive Episode Without Melancholia. As described in the American Psychiatric Association's Diagnostic and Statistical Manual, third edition (DSM III), Major Depressive Episode implies a prominent and relatively persistent (nearly every day for at least 2 weeks) depressed or dysphoric mood that usually interferes with daily functioning and includes at least 4 of the following 8 symptoms: change in appetite, change in sleep, psychomotor agitation or retardation, loss of interest in usual activities or decrease in sexual drive, increased fatigability, feelings of guilt or worthlessness, slowed thinking or impaired concentration, and suicidal ideation or attempts.

The effectiveness of Parstelin (Tranylcypromine Sulfate) in patients who meet the criteria for Major Depressive Episode with Melancholia (endogenous features) has not been established.

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SUMMARY OF CONTRAINDICATIONS

Parstelin (Tranylcypromine Sulfate) should not be administered in combination with any of the following: MAO inhibitors or dibenzazepine derivatives; sympathomimetics (including amphetamines); some central nervous system depressants (including narcotics and alcohol); antihypertensive, diuretic, antihistaminic, sedative, or anesthetic drugs; bupropion HCl; buspirone HCI; dextromethorphan; cheese or other foods with a high tyramine content; or excessive quantities of caffeine.

Parstelin (Tranylcypromine Sulfate) should not be administered to any patient with a confirmed or suspected cerebrovascular defect or to any patient with cardiovascular disease, hypertension , or history of headache.

(For complete discussion of contraindications and warnings, see below.)

CONTRAINDICATIONS

Parstelin (Tranylcypromine Sulfate) is contraindicated:

1. In patients with cerebrovascular defects or cardiovascular disorders

Parstelin (Tranylcypromine Sulfate) should not be administered to any patient with a confirmed or suspected cerebrovascular defect or to any patient with cardiovascular disease or hypertension.

2. In the presence of pheochromocytoma

Parstelin (Tranylcypromine Sulfate) should not be used in the presence of pheochromocytoma since such tumors secrete pressor substances.

3. In combination with MAO inhibitors or with dibenzazepine-related entities

Parstelin (Tranylcypromine Sulfate) should not be administered together or in rapid succession with other MAO inhibitors or with dibenzazepine-related entities. Hypertensive crises or severe convulsive seizures may occur in patients receiving such combinations.

In patients being transferred to Parstelin (Tranylcypromine Sulfate) from another MAO inhibitor or from a dibenzazepine-related entity, allow a medication-free interval of at least a week, then initiate Parstelin (Tranylcypromine Sulfate) using half the normal starting dosage for at least the first week of therapy. Similarly, at least a week should elapse between the discontinuance of Parstelin (Tranylcypromine Sulfate) and the administration of another MAO inhibitor or a dibenzazepine-related entity, or the readministration of Parstelin (Tranylcypromine Sulfate).

The following list includes some other MAO inhibitors, dibenzazepine-related entities and tricyclic antidepressants, and the companies which market them.

Generic Name Source
Furazolidone
Isocarboxazid Marplan® (Oxford Pharm Services)
Pargyline HCl
Pargyline HCl and methyclothiazide
Phenelzine sulfate Nardil® (Pfizer)
Procarbazine HCl Matulane® (Sigma Tau)
Generic Name Source
Amitriptyline HCl (Sandoz)
Perphenazine and amitriptyline HCl (Sandoz)
Clomipramine hydrochloride Anafranil® (Mallinckrodt)
Desipramine HCl (Sandoz)
Imipramine HCl (Sandoz)
Tofranil® (Mallinckrodt)
Nortriptyline HCl (Mylan)
Pamelor® (Mallinckrodt)
Protriptyline HCl Vivactil® (Odyssey Pharmaceuticals, Inc.)
Doxepin HCl Sinequan® (Pfizer)
Carbamazepine Tegretol® (Novartis)
Cyclobenzaprine HCl (Mylan)
Flexeril® (McNeil)
Amoxapine (Watson)
Maprotiline HCl (Mylan)
Trimipramine maleate Surmontil® (Odyssey Pharmaceuticals, Inc.)

4. In combination with bupropion

The concurrent administration of an MAO inhibitor and bupropion hydrochloride (Wellbutrin®, Wellbutrin SR®, Wellbutrin XL®, Zyban®, GlaxoSmithKline) is contraindicated. At least 14 days should elapse between discontinuation of an MAO inhibitor and initiation of treatment with bupropion hydrochloride.

5. In combination with selective serotonin reuptake inhibitors (SSRIs) or selective norepinephrine reuptake inhibitors (SNRIs)

As a general rule, Parstelin (Tranylcypromine Sulfate) should not be administered in combination with any SSRI. There have been reports of serious, sometimes fatal, reactions (including hyperthermia, rigidity, myoclonus, autonomic instability with possible rapid fluctuations of vital signs, and mental status changes that include extreme agitation progressing to delirium and coma) in patients receiving a SSRI (e.g., fluoxetine (Prozac®, Eli Lilly and Company) or a SNRI (e.g., venlafaxine, Effexor®, Effexor XR®, Wyeth) in combination with a monoamine oxidase inhibitor (MAOI), and in patients who have recently discontinued a SSRI or SNRI and are then started on an MAOI. Some cases presented with features resembling neuroleptic malignant syndrome. Therefore, SSRI’s and SNRI should not be used in combination with an MAOI, or within 14 days of discontinuing therapy with an MAOI.

Since fluoxetine and its major metabolite have very long elimination half-lives, at least 5 weeks should be allowed after stopping fluoxetine before starting an MAOI.

At least 2 weeks should be allowed after stopping sertraline (Zoloft®, Pfizer) or paroxetine (Paxil®, GlaxoSmithKline) before starting an MAOI.

At least one week should be allowed after stopping a SNRI (e.g., venlafaxine) before starting a MAOI.

6 . In combination with buspirone

Parstelin (Tranylcypromine Sulfate) should not be used in combination with buspirone HCl, since several cases of elevated blood pressure have been reported in patients taking MAO inhibitors who were then given buspirone HCl. At least 10 days should elapse between the discontinuation of Parstelin (Tranylcypromine Sulfate) and the institution of buspirone HCl.

7 . In combination with sympathomimetics

Parstelin (Tranylcypromine Sulfate) should not be administered in combination with sympathomimetics, including amphetamines, which may be found in many herbal preparations as well as over-the-counter drugs such as cold, hay fever or weight-reducing preparations that contain vasoconstrictors.

During therapy with Parstelin (Tranylcypromine Sulfate), it appears that certain patients are particularly vulnerable to the effects of sympathomimetics when the activity of certain enzymes is inhibited. Use of sympathomimetics and compounds such as guanethidine, methyldopa, reserpine, dopamine, levodopa, and tryptophan with Parstelin (Tranylcypromine Sulfate) may precipitate hypertension, headache, and related symptoms. Cerebral hemorrhage may also occur. The combination of MAOIs and tryptophan has been reported to cause behavioral and neurologic syndromes including disorientation, confusion, amnesia, delirium, agitation, hypomanic signs, ataxia, myoclonus, hyperreflexia, shivering, ocular oscillations, and Babinski's signs.

8 . In combination with meperidine

Do not use meperidine concomitantly with MAO inhibitors or within 2 or 3 weeks following MAOI therapy. Serious reactions have been precipitated with concomitant use, including coma, severe hypertension or hypotension, severe respiratory depression, convulsions, malignant hyperpyrexia, excitation, peripheral vascular collapse, and death. It is thought that these reactions may be mediated by accumulation of 5-HT (serotonin) consequent to MAO inhibition.

9 . In combination with dextromethorphan

The combination of MAO inhibitors and dextromethorphan has been reported to cause brief episodes of psychosis or bizarre behavior.

10. In combination with cheese or other foods with a high tyramine content

When excessive amounts of tyramine are consumed in conjunction with tranylcypromine, or within 2 weeks of stopping treatment, a serious and sometimes fatal hypertensive reaction may occur.

Tyramine occurs naturally in some foods or may occur from the bacterial breakdown of protein in foods which are fermented, aged, or spoiled. Foods that have reliably been shown to contain a high tyramine content and may also have been reported to induce a serious hypertensive reaction when consumed with tranylcypromine are:

  • all matured or aged cheeses (note: all cheeses are considered matured or aged except fresh cottage cheese, cream cheese, ricotta, and processed cheese. All non-cheese dairy products can be consumed providing they are fresh)
  • all aged, cured or fermented meat, fish, or poultry (note: meat, fish, or poultry that has not undergone aging, curing or fermenting and that is bought fresh, stored correctly and eaten fresh is not contraindicated)
  • all fermented soybean products (e.g., soy sauce, miso, fermented tofu)
  • sauerkraut
  • fava or broad bean pods
  • banana peel (but not the pulp)
  • concentrated yeast extracts (e.g., Marmite or Vegemite spread)
  • all tap/draught beers (note: some bottled beers, including non-alcoholic beer, may also pose a risk).

Patients should be advised to minimize or avoid use of all alcoholic beverages while taking Parstelin (Tranylcypromine Sulfate). Patients should be advised to adhere to the following dietary guidance about eating fresh foods:

Foods may be deliberately aged as part of their processing and these are contraindicated. Foods may also naturally age over time, even if they are refrigerated. It is therefore extremely important that patients are instructed to buy and eat only fresh foods or those which have been properly frozen. They should avoid eating foods if they are unsure of their storage conditions or freshness and they should be cautious of foods of unknown age or composition even if refrigerated.

The longer food is left to deteriorate and the larger the quantity of food eaten, the greater the potential quantity of tyramine ingested. Where there is any doubt, patients should be advised to either avoid the food or consume it in strict moderation if it is not otherwise contraindicated.

Patients should also be warned that tyramine levels may vary by brand or even batch and a person may absorb different amounts of tyramine from a particular food at different times. Therefore, if they have accidentally consumed a prohibited food on one occasion and not had a reaction, this does not mean that they will not have a serious hypertensive reaction if they consume the same food on a different occasion.

11. In patients undergoing elective surgery

Patients taking Parstelin (Tranylcypromine Sulfate) should not undergo elective surgery requiring general anesthesia. Also, they should not be given cocaine or local anesthesia containing sympathomimetic vasoconstrictors. The possible combined hypotensive effects of Parstelin (Tranylcypromine Sulfate) and spinal anesthesia should be kept in mind. Parstelin (Tranylcypromine Sulfate) should be discontinued at least 10 days prior to elective surgery.

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ADDITIONAL CONTRAINDICATIONS

In general, the physician should bear in mind the possibility of a lowered margin of safety when Parstelin (Tranylcypromine Sulfate) is administered in combination with potent drugs.

  • Parstelin (Tranylcypromine Sulfate) should not be used in combination with some central nervous system depressants such as narcotics and alcohol, or with hypotensive agents. A marked potentiating effect on these classes of drugs has been reported.
  • Anti-parkinsonism drugs should be used with caution in patients receiving Parstelin (Tranylcypromine Sulfate) since severe reactions have been reported.
  • Parstelin (Tranylcypromine Sulfate) should not be used in patients with a history of liver disease or in those with abnormal liver function tests.
  • Excessive use of caffeine in any form should be avoided in patients receiving Parstelin (Tranylcypromine Sulfate).

WARNINGS TO PHYSICIANS

Clinical Worsening and Suicide Risk:

Patients with major depressive disorder, both adult and pediatric, may experience worsening of their depression and/or the emergence of suicidal ideation and behavior (suicidality) or unusual changes in behavior, whether or not they are taking antidepressant medications, and this risk may persist until significant remission occurs. Suicide is a known risk of depression and certain other psychiatric disorders, and these disorders themselves are the strongest predictors of suicide. There has been a long-standing concern, however, that antidepressants may have a role in inducing worsening of depression and the emergence of suicidality in certain patients during the early phases of treatment. Pooled analyses of short-term placebo-controlled trials of antidepressant drugs (SSRIs and others) showed that these drugs increase the risk of suicidal thinking and behavior (suicidality) in children, adolescents, and young adults (ages 18 to 24) with major depressive disorder (MDD) and other psychiatric disorders. Short-term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo in adults beyond age 24; there was a reduction with antidepressants compared to placebo in adults aged 65 and older.

The pooled analyses of placebo-controlled trials in children and adolescents with MDD, obsessive compulsive disorder (OCD), or other psychiatric disorders included a total of 24 short-term trials of 9 antidepressant drugs in over 4,400 patients. The pooled analyses of placebo-controlled trials in adults with MDD or other psychiatric disorders included a total of 295 short-term trials (median duration of 2 months) of 11 antidepressant drugs in over 77,000 patients. There was considerable variation in risk of suicidality among drugs, but a tendency toward an increase in the younger patients for almost all drugs studied. There were differences in absolute risk of suicidality across the different indications, with the highest incidence in MDD. The risk differences (drug vs placebo), however, were relatively stable within age strata and across indications. These risk differences (drug-placebo difference in the number of cases of suicidality per 1,000 patients treated) are provided in Table 1.

Table 1
Age Range Drug-Placebo Difference in Number of Cases of Suicidality per 1,000 Patients Treated
Increases Compared to Placebo
<18 14 additional cases
18 to 24 5 additional cases
Decreases Compared to Placebo
25 to 64 1 fewer case
>65 6 fewer cases

No suicides occurred in any of the pediatric trials. There were suicides in the adult trials, but the number was not sufficient to reach any conclusion about drug effect on suicide.

It is unknown whether the suicidality risk extends to longer-term use, i.e., beyond several months. However, there is substantial evidence from placebo-controlled maintenance trials in adults with depression that the use of antidepressants can delay the recurrence of depression.

All patients being treated with antidepressants for any indication should be monitored appropriately and observed closely for clinical worsening, suicidality, and unusual changes in behavior, especially during the initial few months of a course of drug therapy, or at times of dose changes, either increases or decreases.

The following symptoms, anxiety, agitation, panic attacks, insomnia, irritability, hostility, aggressiveness, impulsivity, akathisia (psychomotor restlessness), hypomania, and mania, have been reported in adult and pediatric patients being treated with antidepressants for major depressive disorder as well as for other indications, both psychiatric and nonpsychiatric. 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, there is concern that such symptoms may represent precursors to emerging suicidality.

Consideration should be given to changing the therapeutic regimen, including possibly discontinuing the medication, in patients whose depression is persistently worse, or who are experiencing emergent suicidality or symptoms that might be precursors to worsening depression or suicidality, especially if these symptoms are severe, abrupt in onset, or were not part of the patient's presenting symptoms.

Families and caregivers of patients being treated with antidepressants for major depressive disorder or other indications, both psychiatric and nonpsychiatric, should be alerted about the need to monitor patients for the emergence of agitation, irritability, unusual changes in behavior, and the other symptoms described above, as well as the emergence of suicidality, and to report such symptoms immediately to healthcare providers. Such monitoring should include daily observation by families and caregivers. Prescriptions for Parstelin (Tranylcypromine Sulfate) should be written for the smallest quantity of tablets consistent with good patient management, in order to reduce the risk of overdose.

Screening Patients for 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 an antidepressant alone may increase the likelihood of precipitation of a mixed/manic episode in patients at risk for bipolar disorder. Whether any of the symptoms described above represent such a conversion is unknown. However, prior to initiating treatment with an antidepressant, patients with depressive symptoms should be adequately screened to determine if they are at risk for bipolar disorder; such screening should include a detailed psychiatric history, including a family history of suicide, bipolar disorder, and depression. It should be noted that Parstelin (Tranylcypromine Sulfate) is not approved for use in treating bipolar depression.

Parstelin (Tranylcypromine Sulfate) is a potent agent with the capability of producing serious side effects. Parstelin (Tranylcypromine Sulfate) is not recommended in those depressive reactions where other antidepressant drugs may be effective. It should be reserved for patients who can be closely supervised and who have not responded satisfactorily to the drugs more commonly administered for depression.

Before prescribing, the physician should be completely familiar with the full material on dosage, side effects, and contraindications on these pages, with the principles of MAO inhibitor therapy and the side effects of this class of drugs. Also, the physician should be familiar with the symptomatology of mental depressions and alternate methods of treatment to aid in the careful selection of patients for therapy with Parstelin (Tranylcypromine Sulfate).

Pregnancy Warning:

Use of any drug in pregnancy, during lactation or in women of childbearing age requires that the potential benefits of the drug be weighed against its possible hazards to mother and child.

Animal reproductive studies show that Parstelin (Tranylcypromine Sulfate) passes through the placental barrier into the fetus of the rat, and into the milk of the lactating dog. The absence of a harmful action of Parstelin (Tranylcypromine Sulfate) on fertility or on postnatal development by either prenatal treatment or from the milk of treated animals has not been demonstrated. Tranylcypromine is excreted in human milk.

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WARNING TO THE PATIENT

Patients should be instructed to report promptly the occurrence of headache or other unusual symptoms, i.e., palpitation and/or tachycardia, a sense of constriction in the throat or chest, sweating, dizziness, neck stiffness, nausea, or vomiting.

Patients should be warned against eating the foods listed in Section 11 under CONTRAINDICATIONS while on therapy with Parstelin (Tranylcypromine Sulfate). Also, they should be told not to drink alcoholic beverages. The patient should also be warned about the possibility of hypotension and faintness, as well as drowsiness sufficient to impair performance of potentially hazardous tasks such as driving a car or operating machinery.

Patients should also be cautioned not to take concomitant medications, whether prescription or over-the-counter drugs such as cold, hay fever, or weight-reducing preparations, without the advice of a physician. They should be advised not to consume excessive amounts of caffeine in any form. Likewise, they should inform other physicians, and their dentist, about their use of Parstelin (Tranylcypromine Sulfate).

See PRECAUTIONS - Information for Patients for information regarding clinical worsening and suicide risk.

WARNINGS

Hypertensive Crisis:

The most important reaction associated with Parstelin is the occurrence of hypertensive crises which have sometimes been fatal.

These crises are characterized by some or all of the following symptoms: occipital headache which may radiate frontally, palpitation, neck stiffness or soreness, nausea or vomiting, sweating (sometimes with fever and sometimes with cold, clammy skin) and photophobia. Either tachycardia or bradycardia may be present, and associated constricting chest pain and dilated pupils may occur. Intracranial bleeding, sometimes fatal in outcome, has been reported in association with the paradoxical increase in blood pressure.

In all patients taking Parstelin (Tranylcypromine Sulfate), blood pressure should be followed closely to detect evidence of any pressor response. It is emphasized that full reliance should not be placed on blood pressure readings, but that the patient should also be observed frequently.

Therapy should be discontinued immediately upon the occurrence of palpitation or frequent headaches during therapy with Parstelin (Tranylcypromine Sulfate). These signs may be prodromal of a hypertensive crisis.

Important:

Recommended treatment in hypertensive crises

If a hypertensive crisis occurs, Parstelin (Tranylcypromine Sulfate) should be discontinued and therapy to lower blood pressure should be instituted immediately. Headache tends to abate as blood pressure is lowered. On the basis of present evidence, phentolamine is recommended. (The dosage reported for phentolamine is 5 mg I.V.) Care should be taken to administer this drug slowly in order to avoid producing an excessive hypotensive effect. Fever should be managed by means of external cooling. Other symptomatic and supportive measures may be desirable in particular cases. Do not use parenteral reserpine.

PRECAUTIONS

Hypotension:

Hypotension has been observed during therapy with Parstelin. Symptoms of postural hypotension are seen most commonly but not exclusively in patients with pre-existent hypertension; blood pressure usually returns rapidly to pretreatment levels upon discontinuation of the drug. At doses above 30 mg daily, postural hypotension is a major side effect and may result in syncope. Dosage increases should be made more gradually in patients showing a tendency toward hypotension at the beginning of therapy. Postural hypotension may be relieved by having the patient lie down until blood pressure returns to normal.

Also, when Parstelin (Tranylcypromine Sulfate) is combined with those phenothiazine derivatives or other compounds known to cause hypotension, the possibility of additive hypotensive effects should be considered.

There have been reports of drug dependency in patients using doses of tranylcypromine significantly in excess of the therapeutic range. Some of these patients had a history of previous substance abuse. The following withdrawal symptoms have been reported: restlessness, anxiety, depression, confusion, hallucinations, headache, weakness, and diarrhea.

Drugs which lower the seizure threshold, including MAO inhibitors, should not be used with Amipaque®*. As with other MAO inhibitors, Parstelin (Tranylcypromine Sulfate) should be discontinued at least 48 hours before myelography and should not be resumed for at least 24 hours post-procedure.

MAO inhibitors may have the capacity to suppress anginal pain that would otherwise serve as a warning of myocardial ischemia.

The usual precautions should be observed in patients with impaired renal function since there is a possibility of cumulative effects in such patients.

Older patients may suffer more morbidity than younger patients during and following an episode of hypertension or malignant hyperthermia. Older patients have less compensatory reserve to cope with any serious adverse reaction. Therefore, Parstelin (Tranylcypromine Sulfate) should be used with caution in the elderly population.

Although excretion of Parstelin (Tranylcypromine Sulfate) is rapid, inhibition of MAO may persist up to 10 days following discontinuation.

Because the influence of Parstelin (Tranylcypromine Sulfate) on the convulsive threshold is variable in animal experiments, suitable precautions should be taken if epileptic patients are treated.

Some MAO inhibitors have contributed to hypoglycemic episodes in diabetic patients receiving insulin or oral hypoglycemic agents. Therefore, Parstelin (Tranylcypromine Sulfate) should be used with caution in diabetics using these drugs.

Parstelin (Tranylcypromine Sulfate) may aggravate coexisting symptoms in depression, such as anxiety and agitation.

Use Parstelin (Tranylcypromine Sulfate) with caution in hyperthyroid patients because of their increased sensitivity to pressor amines.

Parstelin (Tranylcypromine Sulfate) should be administered with caution to patients receiving Antabuse®†. In a single study, rats given high intraperitoneal doses of d or l isomers of Parstelin (Tranylcypromine Sulfate) plus disulfiram experienced severe toxicity including convulsions and death. Additional studies in rats given high oral doses of racemic Parstelin (Tranylcypromine Sulfate) and disulfiram produced no adverse interaction.

Information for Patients:

Prescribers or other health professionals should inform patients, their families, and their caregivers about the benefits and risks associated with treatment with Parstelin (Tranylcypromine Sulfate) and should counsel them in its appropriate use. A patient Medication Guide about “Antidepressant Medicines, Depression and Other Serious Mental Illness, and Suicidal Thoughts or Actions” is available for Parstelin (Tranylcypromine Sulfate). The prescriber or health professional should instruct patients, their families, and their caregivers to read the Medication Guide and should assist them in understanding its contents. Patients should be given the opportunity to discuss the contents of the Medication Guide and to obtain answers to any questions they may have. The complete text of the Medication Guide is reprinted at the end of this document.

Patients should be advised of the following issues and asked to alert their prescriber if these occur while taking Parstelin (Tranylcypromine Sulfate).

Clinical Worsening and Suicide Risk:

Patients, their families, and their caregivers should be encouraged to be alert to the emergence of anxiety, agitation, panic attacks, insomnia, irritability, hostility, aggressiveness, impulsivity, akathisia, hypomania, mania, other unusual changes in behavior, worsening of depression, and suicidal ideation, especially early during antidepressant treatment and when the dose is adjusted up or down. Families and caregivers of patients should be advised to look for the emergence of such symptoms on a day-to-day basis, since changes may be abrupt. Such symptoms should be reported to the patient's prescriber or health professional, especially if they are severe, abrupt in onset, or were not part of the patient's presenting symptoms. Symptoms such as these may be associated with an increased risk for suicidal thinking and behavior and indicate a need for very close monitoring and possibly changes in the medication.

Pediatric Use:

Safety and effectiveness in the pediatric population have not been established (see BOX WARNING and WARNINGS TO PHYSICIANS - Clinical Worsening and Suicide Risk ). Anyone considering the use of Parstelin (Tranylcypromine Sulfate) in a child or adolescent must balance the potential risks with the clinical need.

ADVERSE REACTIONS

Overstimulation which may include increased anxiety, agitation, and manic symptoms is usually evidence of excessive therapeutic action. Dosage should be reduced, or a phenothiazine tranquilizer should be administered concomitantly.

Patients may experience restlessness or insomnia; may notice some weakness, drowsiness, episodes of dizziness or dry mouth; or may report nausea, diarrhea, abdominal pain, or constipation. Most of these effects can be relieved by lowering the dosage or by giving suitable concomitant medication.

Tachycardia, significant anorexia, edema, palpitation, blurred vision, chills, and impotence have each been reported.

Headaches without blood pressure elevation have occurred.

Rare instances of hepatitis, skin rash, and alopecia have been reported.

Impaired water excretion compatible with the syndrome of inappropriate secretion of antidiuretic hormone has been reported.

Tinnitus, muscle spasm, tremors, myoclonic jerks, numbness, paresthesia, urinary retention, and retarded ejaculation have been reported.

Hematologic disorders including anemia, leukopenia, agranulocytosis, and thrombocytopenia have been reported.

Post-Introduction Reports:

The following are spontaneously reported adverse events temporally associated with use of Parstelin (Tranylcypromine Sulfate). No clear relationship between Parstelin (Tranylcypromine Sulfate) and these events has been established. Localized scleroderma, flare-up of cystic acne, ataxia, confusion, disorientation, memory loss, urinary frequency, urinary incontinence, urticaria, fissuring in corner of mouth, akinesia.

DOSAGE AND ADMINISTRATION

Dosage should be adjusted to the requirements of the individual patient. Improvement should be seen within 48 hours to 3 weeks after starting therapy.

The usual effective dosage is 30 mg per day, usually given in divided doses. If there are no signs of improvement after a reasonable period (up to 2 weeks), then the dosage may be increased in 10 mg per day increments at intervals of 1 to 3 weeks; the dosage range may be extended to a maximum of 60 mg per day from the usual 30 mg per day.

OVERDOSAGE

Symptoms:

The characteristic symptoms that may be caused by overdosage are usually those described above.

However, an intensification of these symptoms and sometimes severe additional manifestations may be seen, depending on the degree of overdosage and on individual susceptibility. Some patients exhibit insomnia, restlessness and anxiety, progressing in severe cases to agitation, mental confusion, and incoherence. Hypotension, dizziness, weakness, and drowsiness may occur, progressing in severe cases to extreme dizziness and shock. A few patients have displayed hypertension with severe headache and other symptoms. Rare instances have been reported in which hypertension was accompanied by twitching or myoclonic fibrillation of skeletal muscles with hyperpyrexia, sometimes progressing to generalized rigidity and coma.

Treatment:

Because strategies for the management of overdose are continually evolving, it is advisable to contact a Poison Control Center to determine the latest recommendations for the management of an overdose of any drug. Telephone numbers for the certified Poison Control Centers are listed in the Physicians’ Desk Reference (PDR).

Treatment should normally consist of general supportive measures, close observation of vital signs and steps to counteract specific symptoms as they occur, since MAO inhibition may persist. The management of hypertensive crises is described under WARNINGS in the Hypertensive Crisis section.

External cooling is recommended if hyperpyrexia occurs. Barbiturates have been reported to help relieve myoclonic reactions, but frequency of administration should be controlled carefully because Parstelin (Tranylcypromine Sulfate) may prolong barbiturate activity. When hypotension requires treatment, the standard measures for managing circulatory shock should be initiated. If pressor agents are used, the rate of infusion should be regulated by careful observation of the patient because an exaggerated pressor response sometimes occurs in the presence of MAO inhibition. Remember that the toxic effect of Parstelin (Tranylcypromine Sulfate) may be delayed or prolonged following the last dose of the drug. Therefore, the patient should be closely observed for at least a week. It is not known if tranylcypromine is dialyzable.

HOW SUPPLIED

Parstelin (Tranylcypromine Sulfate) Tablets, USP are supplied as round, dark pink, film-coated tablets debossed with “250” on one side and “K” on the other side and contains Parstelin (Tranylcypromine Sulfate) equivalent to 10 mg of tranylcypromine, in bottles of 100 with a desiccant.

10 mg 100's: NDC 49884-032-01

Store at 20º to 25ºC (68º to 77ºF); excursions permitted to 15º to 30ºC (59º to 86ºF).

.

* metrizamide, The Sanofi-Aventis Group

disulfiram, Odyssey Pharmaceuticals, Inc.

MEDICATION GUIDE

Antidepressant Medicines, Depression and Other Serious Mental Illnesses, and Suicidal Thoughts or Actions

Parstelin (Tranylcypromine Sulfate) Tablets, USP

Read the Medication Guide that comes with your or your family member’s antidepressant medicine. This Medication Guide is only about the risk of suicidal thoughts and actions with antidepressant medicines. Talk to your, or your family member’s, healthcare provider about:

  • All risks and benefits of treatment with antidepressant medicines
  • All treatment choices for depression or other serious mental illness

What is the most important information I should know about antidepressant medicines, depression and other serious mental illnesses, and suicidal thoughts or actions?

1. Antidepressant medicines may increase suicidal thoughts or actions in some children, teenagers, and young adults within the first few months of treatment.

2. Depression and other serious mental illnesses are the most important causes of suicidal thoughts and actions. Some people may have a particularly high risk of having suicidal thoughts or actions. These include people who have (or have a family history of) bipolar illness (also called manic-depressive illness) or suicidal thoughts or actions.

3. How can I watch for and try to prevent suicidal thoughts and actions in myself or a family member?

  • Pay close attention to any changes, especially sudden changes, in mood, behaviors, thoughts, or feelings. This is very important when an antidepressant medicine is started or when the dose is changed.
  • Call the healthcare provider right away to report new or sudden changes in mood, behavior, thoughts, or feelings.
  • Keep all follow-up visits with the healthcare provider as scheduled. Call the healthcare provider between visits as needed, especially if you have concerns about symptoms.

Call a healthcare provider right away if you or your family member has any of the following symptoms, especially if they are new, worse, or worry you:

  • Thoughts about suicide or dying
  • Attempts to commit suicide
  • New or worse depression
  • New or worse anxiety
  • Feeling very agitated or restless
  • Panic attacks
  • Trouble sleeping (insomnia)
  • New or worse irritability
  • Acting aggressive, being angry, or violent
  • Acting on dangerous impulses
  • An extreme increase in activity and talking (mania)
  • Other unusual changes in behavior or mood

What else do I need to know about antidepressant medicines?

  • Never stop an antidepressant medicine without first talking to a healthcare provider. Stopping an antidepressant medicine suddenly can cause other symptoms.
  • Antidepressants are medicines used to treat depression and other illnesses. It is important to discuss all the risks of treating depression and also the risks of not treating it. Patients and their families or other caregivers should discuss all treatment choices with the healthcare provider, not just the use of antidepressants.
  • Antidepressants have other side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
  • Antidepressant medicines can interact with other medicines. Know all of the medicines that you or your family member takes. Keep a list of all medicines to show the healthcare provider. Do not start new medicines without first checking with your healthcare provider.
  • Not all antidepressant medicines prescribed for children are FDA approved for use in children. Talk to your child’s healthcare provider for more information.

This Medication Guide has been approved by the U.S. Food and Drug Administration for all antidepressants.

Manufactured by:

Par Pharmaceutical

Chestnut Ridge, NY 10977

Revised: 01/16

OS032-01-1-12

Trifluoperazine Hydrochloride:


INDICATIONS AND USAGE

For the management of schizophrenia.

Parstelin (Trifluoperazine Hydrochloride) HCl is effective for the short-term treatment of generalized non-psychotic anxiety. However, Parstelin (Trifluoperazine Hydrochloride) HCl is not the first drug to be used in therapy for most patients with non-psychotic anxiety because certain risks associated with its use are not shared by common alternative treatments (i.e., benzodiazepines).

When used in the treatment of non-psychotic anxiety, Parstelin (Trifluoperazine Hydrochloride) HCl should not be administered at doses of more than 6 mg per day or for longer than 12 weeks because the use of Parstelin (Trifluoperazine Hydrochloride) HCl at higher doses or for longer intervals may cause persistent tardive dyskinesia that may prove irreversible (see WARNINGS ).

The effectiveness of Parstelin (Trifluoperazine Hydrochloride) HCl as a treatment for non-psychotic anxiety was established in a four-week clinical multicenter study of outpatients with generalized anxiety disorder (DSM-III). This evidence does not predict that Parstelin (Trifluoperazine Hydrochloride) HCl will be useful in patients with other non-psychotic conditions in which anxiety, or signs that mimic anxiety, are found (i.e., physical illness, organic mental conditions, agitated depression, character pathologies, etc.).

Parstelin (Trifluoperazine Hydrochloride) HCl has not been shown effective in the management of behavioral complications in patients with mental retardation.

CONTRAINDICATIONS

A known hypersensitivity to phenothiazines, comatose or greatly depressed states due to central nervous system depressants and, in cases of existing blood dyscrasias, bone marrow depression and pre-existing liver damage.

WARNINGS

Increased Mortality in Elderly Patients with Dementia-Related Psychosis

Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Parstelin hydrochloride is not approved for the treatment of patients with dementia-related psychosis.

Tardive Dyskinesia

Tardive dyskinesia, a syndrome consisting of potentially irreversible, involuntary, dyskinetic movements, may develop in patients treated with neuroleptic (antipsychotic) drugs. Although the prevalence of the syndrome appears to be highest among the elderly, especially elderly women, it is impossible to rely upon prevalence estimates to predict, at the inception of neuroleptic treatment, which patients are likely to develop the syndrome. Whether neuroleptic drug products differ in their potential to cause tardive dyskinesia is unknown.

Both the risk of developing the syndrome and the likelihood that it will become irreversible are believed to increase as the duration of treatment and the total cumulative dose of neuroleptic drugs administered to the patient increase. However, the syndrome can develop, although much less commonly, after relatively brief treatment periods at low doses.

There is no known treatment for established cases of tardive dyskinesia, although the syndrome may remit, partially or completely, if neuroleptic treatment is withdrawn. Neuroleptic treatment itself, however, may suppress (or partially suppress) the signs and symptoms of the syndrome and thereby may possibly mask the underlying disease process. The effect that symptomatic suppression has upon the long-term course of the syndrome is unknown.

Given these considerations, neuroleptics should be prescribed in a manner that is most likely to minimize the occurrence of tardive dyskinesia. Chronic neuroleptic treatment should generally be reserved for patients who suffer from a chronic illness that 1) is known to respond to neuroleptic drugs, and 2) for whom alternative, equally effective, but potentially less harmful treatments are not available or appropriate. In patients who do require chronic treatment, the smallest dose and the shortest duration of treatment producing a satisfactory clinical response should be sought. The need for continued treatment should be reassessed periodically.

If signs and symptoms of tardive dyskinesia appear in a patient on neuroleptics, drug discontinuation should be considered. However, some patients may require treatment despite the presence of the syndrome.

For further information about the description of tardive dyskinesia and its clinical detection, please refer to the sections on PRECAUTIONS and ADVERSE REACTIONS .

Neuroleptic Malignant Syndrome

A potentially fatal symptom complex sometimes referred to as Neuroleptic Malignant Syndrome (NMS) has been reported in association with antipsychotic drugs. Clinical manifestations of NMS are hyperpyrexia, muscle rigidity, altered mental status and evidence of autonomic instability (irregular pulse or blood pressure, tachycardia, diaphoresis, and cardiac dysrhythmias).

The diagnostic evaluation of patients with this syndrome is complicated. In arriving at a diagnosis, it is important to identify cases where the clinical presentation includes both serious medical illness (e.g., pneumonia, systemic infection, etc.) and untreated or inadequately treated extrapyramidal signs and symptoms (EPS). Other important considerations in the differential diagnosis include central anticholinergic toxicity, heat stroke, drug fever and primary central nervous system (CNS) pathology.

The management of NMS should include 1) immediate discontinuation of antipsychotic drugs and other drugs not essential to concurrent therapy, 2) intensive symptomatic treatment and medical monitoring, and 3) treatment of any concomitant serious medical problems for which specific treatments are available. There is no general agreement about specific pharmacological treatment regimens for uncomplicated NMS.

If a patient requires antipsychotic drug treatment after recovery from NMS, the potential reintroduction of drug therapy should be carefully considered. The patient should be carefully monitored, since recurrences of NMS have been reported.

An encephalopathic syndrome (characterized by weakness, lethargy, fever, tremulousness and confusion, extrapyramidal symptoms, leukocytosis, elevated serum enzymes, BUN and FBS) has occurred in a few patients treated with lithium plus a neuroleptic. In some instances, the syndrome was followed by irreversible brain damage. Because of a possible causal relationship between these events and the concomitant administration of lithium and neuroleptics, patients receiving such combined therapy should be monitored closely for early evidence of neurologic toxicity and treatment discontinued promptly if such signs appear. This encephalopathic syndrome may be similar to or the same as neuroleptic malignant syndrome (NMS).

Patients who have demonstrated a hypersensitivity reaction (e.g., blood dyscrasias, jaundice) with a phenothiazine should not be re-exposed to any phenothiazine, including Parstelin (Trifluoperazine Hydrochloride) HCl, unless in the judgment of the physician, the potential benefits of treatment outweigh the possible hazard.

Parstelin (Trifluoperazine Hydrochloride) HCl may impair mental and/or physical abilities, especially during the first few days of therapy. Therefore, caution patients about activities requiring alertness (e.g., operating vehicles or machinery).

If agents such as sedatives, narcotics, anesthetics, tranquilizers, or alcohol are used either simultaneously or successively with the drug, the possibility of an undesirable additive depressant effect should be considered.

Usage In Pregnancy

Safety for the use of Parstelin HCl during pregnancy has not been established. Therefore, it is not recommended that the drug be given to pregnant patients except when, in the judgment of the physician, it is essential. The potential benefits should clearly outweigh possible hazards. There are reported instances of prolonged jaundice, extrapyramidal signs, hyperreflexia or hyporeflexia in newborn infants whose mothers received phenothiazines.

Reproductive studies in rats given over 600 times the human dose showed an increased incidence of malformations above controls and reduced litter size and weight linked to maternal toxicity. These effects were not observed at half this dosage. No adverse effect on fetal development was observed in rabbits given 700 times the human dose nor in monkeys given 25 times the human dose.

Non-teratogenic Effects

Neonates exposed to antipsychotic drugs, during the third trimester of pregnancy are at risk for extrapyramidal and/or withdrawal symptoms following delivery. There have been reports of agitation, hypertonia, hypotonia, tremor, somnolence, respiratory distress and feeding disorder in these neonates. These complications have varied in severity; while in some cases symptoms have been self-limited, in other cases neonates have required intensive care unit support and prolonged hospitalization.

Parstelin (Trifluoperazine Hydrochloride) Hydrochloride should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nursing Mothers

There is evidence that phenothiazines are excreted in the breast milk of nursing mothers. Because of the potential for serious adverse reactions in nursing infants from Parstelin (Trifluoperazine Hydrochloride), a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

PRECAUTIONS

General

Given the likelihood that some patients exposed chronically to neuroleptics will develop tardive dyskinesia, it is advised that all patients in whom chronic use is contemplated be given, if possible, full information about this risk. The decision to inform patients and/or their guardians must obviously take into account the clinical circumstances and the competency of the patient to understand the information provided.

Thrombocytopenia and anemia have been reported in patients receiving the drug. Agranulocytosis and pancytopenia have also been reported – warn patients to report the sudden appearance of sore throat or other signs of infection. If white blood cell and differential counts indicate cellular depression, stop treatment and start antibiotic and other suitable therapy.

Jaundice of the cholestatic type of hepatitis or liver damage has been reported. If fever with grippe-like symptoms occurs, appropriate liver studies should be conducted. If tests indicate an abnormality, stop treatment.

One result of therapy may be an increase in mental and physical activity. For example, a few patients with angina pectoris have complained of increased pain while taking the drug. Therefore, angina patients should be observed carefully and, if an unfavorable response is noted, the drug should be withdrawn.

Because hypotension has occurred, large doses and parenteral administration should be avoided in patients with impaired cardiovascular systems. To minimize the occurrence of hypotension after injection, keep patient lying down and observe for at least 1/2 hour. If hypotension occurs from parenteral or oral dosing, place patient in head-low position with legs raised. If a vasoconstrictor is required, norepinephrine bitartrate and phenylephrine HCl are suitable. Other pressor agents, including epinephrine, should not be used as they may cause a paradoxical further lowering of blood pressure.

Since certain phenothiazines have been reported to produce retinopathy, the drug should be discontinued if ophthalmoscopic examination or visual field studies should demonstrate retinal changes.

An antiemetic action of Parstelin HCl may mask the signs and symptoms of toxicity or overdosage of other drugs and may obscure the diagnosis and treatment of other conditions such as intestinal obstruction, brain tumor and Reye’s Syndrome.

With prolonged administration at high dosages, the possibility of cumulative effects, with sudden onset of severe central nervous system or vasomotor symptoms, should be kept in mind.

Neuroleptic drugs elevate prolactin levels; the elevation persists during chronic administration. Tissue culture experiments indicate that approximately one-third of human breast cancers are prolactin-dependent in vitro, a factor of potential importance if the prescribing of these drugs is contemplated in a patient with a previously detected breast cancer. Although disturbances such as galactorrhea, amenorrhea, gynecomastia and impotence have been reported, the clinical significance of elevated serum prolactin levels is unknown for most patients. An increase in mammary neoplasms has been found in rodents after chronic administration of neuroleptic drugs. Neither clinical nor epidemiologic studies conducted to date, however, have shown an association between chronic administration of these drugs and mammary tumorigenesis; the available evidence is considered too limited to be conclusive at this time.

Chromosomal aberrations in spermatocytes and abnormal sperm have been demonstrated in rodents treated with certain neuroleptics.

Because phenothiazines may interfere with thermoregulatory mechanisms, use with caution in persons who will be exposed to extreme heat.

As with all drugs which exert an anticholinergic effect, and/or cause mydriasis, Parstelin (Trifluoperazine Hydrochloride) should be used with caution in patients with glaucoma.

Phenothiazines may diminish the effect of oral anticoagulants.

Phenothiazines can produce alpha-adrenergic blockade.

Concomitant administration of propranolol with phenothiazines results in increased plasma levels of both drugs.

Antihypertensive effects of guanethidine and related compounds may be counteracted when phenothiazines are used concurrently.

Thiazide diuretics may accentuate the orthostatic hypotension that may occur with phenothiazines.

Phenothiazines may lower the convulsive threshold; dosage adjustments of anticonvulsants may be necessary. Potentiation of anticonvulsant effects does not occur. However, it has been reported that phenothiazines may interfere with the metabolism of phenytoin and thus precipitate phenytoin toxicity.

Drugs which lower the seizure threshold, including phenothiazine derivatives, should not be used with metrizamide. As with other phenothiazine derivatives, Parstelin (Trifluoperazine Hydrochloride) HCl should be discontinued at least 48 hours before myelography, should not be resumed for at least 24 hours postprocedure, and should not be used for the control of nausea and vomiting occurring either prior to myelography or postprocedure with metrizamide.

The presence of phenothiazines may produce false positive phenylketonuria (PKU) test results.

Long-Term Therapy

To lessen the likelihood of adverse reactions related to cumulative drug effect, patients with a history of long-term therapy with Parstelin (Trifluoperazine Hydrochloride) HCl and/or other neuroleptics should be evaluated periodically to decide whether the maintenance dosage could be lowered or drug therapy discontinued.

Leukopenia, Neutropenia and Agranulocytosis

In clinical trial and post-marketing experience, events of leukopenia/neutropenia and agranulocytosis have been reported temporally related to antipsychotic agents. Possible risk factors for leukopenia/neutropenia include preexisting low white blood cell count (WBC) and history of drug induced leukopenia/neutropenia. Patients with a preexisting low WBC or a history of drug induced leukopenia/neutropenia should have their complete blood count (CBC) monitored frequently during the first few months of therapy and should discontinue Parstelin (Trifluoperazine Hydrochloride) HCl at the first sign of a decline in WBC in the absence of other causative factors. Patients with neutropenia should be carefully monitored for fever or other symptoms or signs of infection and treated promptly if such symptoms or signs occur. Patients with severe neutropenia (absolute neutrophil count <1000/mm3) should discontinue Parstelin (Trifluoperazine Hydrochloride) HCl and have their WBC followed until recovery.

ADVERSE REACTIONS

Drowsiness, dizziness, skin reactions, rash, dry mouth, insomnia, amenorrhea, fatigue, muscular weakness, anorexia, lactation, blurred vision and neuromuscular reactions.

Extrapyramidal Symptoms

These symptoms are seen in a significant number of hospitalized mental patients. They may be characterized by motor restlessness, be of the dystonic type, or they may resemble parkinsonism.

Depending on the severity of symptoms, dosage should be reduced or discontinued. If therapy is reinstituted, it should be at a lower dosage. Should these symptoms occur in children or pregnant patients, the drug should be stopped and not reinstituted. In most cases, barbiturates by suitable route of administration will suffice. (Or, injectable diphenhydramine hydrochloride may be useful.) In more severe cases, the administration of an anti-parkinsonism agent, except levodopa, usually produces rapid reversal of symptoms. Suitable supportive measures such as maintaining a clear airway and adequate hydration should be employed.

Dystonia

Class Effect: Symptoms of dystonia, prolonged abnormal contractions of muscle groups, may occur in susceptible individuals during the first few days of treatment. Dystonic symptoms include: spasm of the neck muscles, sometimes progressing to tightness of the throat, swallowing difficulty, difficulty breathing, and/or protrusion of the tongue. While these symptoms can occur at low doses, they occur more frequently and with greater severity with high potency and at higher doses of first generation antipsychotic drugs. An elevated risk of acute dystonia is observed in males and younger age groups.

Motor Restlessness

Symptoms may include agitation or jitteriness and sometimes insomnia. These symptoms often disappear spontaneously. At times these symptoms may be similar to the original neurotic or psychotic symptoms. Dosage should not be increased until these side effects have subsided.

If this phase becomes too troublesome, the symptoms can usually be controlled by a reduction of dosage or change of drug. Treatment with anti-parkinsonian agents, benzodiazepines or propranolol may be helpful.

Pseudo-parkinsonism

Symptoms may include: mask-like facies; drooling, tremors; pill-rolling motion; cogwheel rigidity; and shuffling gait. Reassurance and sedation are important. In most cases, these symptoms are readily controlled when an anti-parkinsonism agent is administered concomitantly. Anti-parkinsonism agents should be used only when required. Generally, therapy of a few weeks to two to three months will suffice. After this time patients should be evaluated to determine their need for continued treatment. Occasionally it is necessary to lower the dosage of Parstelin (Trifluoperazine Hydrochloride) HCl or to discontinue the drug.

Tardive Dyskinesia

As with all antipsychotic agents, tardive dyskinesia may appear in some patients on long-term therapy or may appear after drug therapy has been discontinued. The syndrome can also develop, although much less frequently, after relatively brief treatment periods at low doses. This syndrome appears in all age groups. Although its prevalence appears to be highest among elderly patients, especially elderly women, it is impossible to rely upon prevalence estimates to predict at the inception of neuroleptic treatment which patients are likely to develop the syndrome. The symptoms are persistent and in some patients appear to be irreversible. The syndrome is characterized by rhythmical involuntary movements of the tongue, face, mouth or jaw (e.g., protrusion of tongue, puffing of cheeks, puckering of mouth, chewing movements). Sometimes these may be accompanied by involuntary movements of extremities. In rare instances, these involuntary movements of the extremities are the only manifestations of tardive dyskinesia. A variant of tardive dyskinesia, tardive dystonia, has also been described.

There is no known effective treatment for tardive dyskinesia; anti-parkinsonism agents do not alleviate the symptoms of this syndrome. If clinically feasible, it is suggested that all antipsychotic agents be discontinued if these symptoms appear. Should it be necessary to reinstitute treatment, or increase the dosage of the agent, or switch to a different antipsychotic agent, the syndrome may be masked.

It has been reported that fine vermicular movements of the tongue may be an early sign of the syndrome and if the medication is stopped at that time the syndrome may not develop.

Adverse Reactions Reported with Parstelin HCl or Other Phenothiazine Derivatives

Adverse effects with different phenothiazines vary in type, frequency, and mechanism of occurrence, i.e., some are dose-related, while others involve individual patient sensitivity. Some adverse effects may be more likely to occur, or occur with greater intensity, in patients with special medical problems, e.g., patients with mitral insufficiency or pheochromocytoma have experienced severe hypotension following recommended doses of certain phenothiazines.

Neuroleptic Malignant Syndrome (NMS) has been reported in association with antipsychotic drugs. (See WARNINGS .)

Not all of the following adverse reactions have been observed with every phenothiazine derivative, but they have been reported with one or more and should be borne in mind when drugs of this class are administered: extrapyramidal symptoms (opisthotonos, oculogyric crisis, hyperreflexia, dystonia, akathisia, dyskinesia, parkinsonism) some of which have lasted months and even years – particularly in elderly patients with previous brain damage; grand mal and petit mal convulsions, particularly in patients with EEG abnormalities or history of such disorders; altered cerebrospinal fluid proteins; cerebral edema; intensification and prolongation of the action of central nervous system depressants (opiates, analgesics, antihistamines, barbiturates, alcohol), atropine, heat, organophosphorus insecticides; autonomic reactions (dryness of mouth, nasal congestion, headache, nausea, constipation, obstipation, adynamic ileus, ejaculatory disorders/impotence, priapism, atonic colon, urinary retention, miosis and mydriasis); reactivation of psychotic processes, catatonic-like states; hypotension (sometimes fatal); cardiac arrest; blood dyscrasias (pancytopenia, thrombocytopenic purpura, leukopenia, agranulocytosis, eosinophilia, hemolytic anemia, aplastic anemia); liver damage (jaundice, biliary stasis); endocrine disturbances (hyperglycemia, hypoglycemia, glycosuria, lactation, galactorrhea, gynecomastia, menstrual irregularities, false positive pregnancy tests); skin disorders (photosensitivity, itching, erythema, urticaria, eczema up to exfoliative dermatitis); other allergic reactions (asthma, laryngeal edema, angioneurotic edema, anaphylactoid reactions); peripheral edema; reversed epinephrine effect; hyperpyrexia; mild fever after large I.M. doses; increased appetite; increased weight; a systemic lupus erythematosus-like syndrome; pigmentary retinopathy; with prolonged administration of substantial doses, skin pigmentation, epithelial keratopathy, and lenticular and corneal deposits.

EKG changes – particularly nonspecific, usually reversible Q and T wave distortions – have been observed in some patients receiving phenothiazine tranquilizers. Although phenothiazines cause neither psychic nor physical dependence, sudden discontinuance in long-term psychiatric patients may cause temporary symptoms, e.g., nausea and vomiting, dizziness, tremulousness.

Note: There have been occasional reports of sudden death in patients receiving phenothiazines. In some cases, the cause appeared to be cardiac arrest or asphyxia due to failure of the cough reflex.

OVERDOSAGE

Symptoms

Primarily involvement of the extrapyramidal mechanism producing some of the dystonic reactions described above. Symptoms of central nervous system depression to the point of somnolence or coma. Agitation and restlessness may also occur. Other possible manifestations include convulsions, EKG changes and cardiac arrhythmias, fever, and autonomic reactions such as hypotension, dry mouth and ileus.

Treatment

It is important to determine other medications taken by the patient since multiple dose therapy is common in overdosage situations. Treatment is essentially symptomatic and supportive. Early gastric lavage is helpful. Keep patient under observation and maintain an open airway, since involvement of the extrapyramidal mechanism may produce dysphagia and respiratory difficulty in severe overdosage. Do not attempt to induce emesis because a dystonic reaction of the head or neck may develop that could result in aspiration of vomitus. Extrapyramidal symptoms may be treated with anti-parkinsonism drugs, barbiturates, or diphenhydramine hydrochloride. See prescribing information for these products. Care should be taken to avoid increasing respiratory depression. If administration of a stimulant is desirable, amphetamine, dextroamphetamine, or caffeine with sodium benzoate is recommended. Stimulants that may cause convulsions (e.g., picrotoxin or pentylenetetrazol) should be avoided.

If hypotension occurs, the standard measures for managing circulatory shock should be initiated. If it is desirable to administer a vasoconstrictor, norepinephrine bitartrate and phenylephrine HCl are most suitable. Other pressor agents, including epinephrine, are not recommended because phenothiazine derivatives may reverse the usual elevating action of these agents and cause a further lowering of blood pressure.

Limited experience indicates that phenothiazines are not dialyzable.

DOSAGE AND ADMINISTRATION

Adults

Dosage should be adjusted to the needs of the individual. The lowest effective dosage should always be used. Dosage should be increased more gradually in debilitated or emaciated patients. When maximum response is achieved, dosage may be reduced gradually to a maintenance level. Because of the inherent long action of the drug, patients may be controlled on convenient b.i.d. administration; some patients may be maintained on once-a-day administration.

When Parstelin HCl is administered by intramuscular injection, equivalent oral dosage may be substituted once symptoms have been controlled.

Note: Although there is little likelihood of contact dermatitis due to the drug, persons with known sensitivity to phenothiazine drugs should avoid direct contact.

Elderly Patients

In general, dosages in the lower range are sufficient for most elderly patients. Since they appear to be more susceptible to hypotension and neuromuscular reactions, such patients should be observed closely. Dosage should be tailored to the individual, response carefully monitored, and dosage adjusted accordingly. Dosage should be increased more gradually in elderly patients.

Non-psychotic Anxiety

Usual dosage is 1 or 2 mg twice daily. Do not administer at doses of more than 6 mg per day or for longer than 12 weeks.

Psychotic Disorders

ORAL: Usual starting dosage is 2 mg to 5 mg b.i.d..

Most patients will show optimum response on 15 mg or 20 mg daily, although a few may require 40 mg a day or more. Optimum therapeutic dosage levels should be reached within two or three weeks.

Psychotic Children

Dosage should be adjusted to the weight of the child and the severity of the symptoms. These dosages are for children ages 6 to 12, who are hospitalized or under close supervision.

ORAL: The starting dosage is 1 mg administered once a day or b.i.d. Dosage may be increased gradually until symptoms are controlled or until side effects become troublesome.

While it is usually not necessary to exceed dosages of 15 mg daily, some older children with severe symptoms may require higher dosages.

HOW SUPPLIED

Parstelin (Trifluoperazine Hydrochloride) hydrochloride tablets, USP are available as:

1 mg: Round, film-coated, lavender colored tablets, debossed GG 51 on one side and 1 on the reverse side, and supplied as:

NDC 0781-1030-01 bottles of 100

NDC 0781-1030-05 bottles of 500

NDC 0781-1030-10 bottles of 1000

NDC 0781-1030-13 unit dose packages of 100

2 mg: Round, film-coated, lavender colored tablets, debossed GG 53 on one side and 2 on the reverse side, and supplied as:

NDC 0781-1032-01 bottles of 100

NDC 0781-1032-05 bottles of 500

NDC 0781-1032-10 bottles of 1000

NDC 0781-1032-13 unit dose packages of 100

5 mg: Round, film-coated, lavender colored tablets, debossed GG 55 on one side and 5 on the reverse side, and supplied as:

NDC 0781-1034-01 bottles of 100

NDC 0781-1034-05 bottles of 500

NDC 0781-1034-10 bottles of 1000

NDC 0781-1034-13 unit dose packages of 100

This strength tablet for use only in severe neuropsychiatric conditions.

10 mg: Round, film-coated, lavender colored tablets, debossed GG 58 on one side and 10 on the reverse side, and supplied as:

NDC 0781-1036-01 bottles of 100

NDC 0781-1036-05 bottles of 500

NDC 0781-1036-10 bottles of 1000

NDC 0781-1036-13 unit dose packages of 100

This strength tablet for use only in severe neuropsychiatric conditions.

Store at 20°-25°C (68°-77°F). Protect from moisture.

Dispense in a tight, light-resistant container.

03-2011M

7193

Sandoz Inc.

Princeton, NJ 08540

NDC 0781-1030-01

Parstelin (Trifluoperazine Hydrochloride)

Hydrochloride

Tablets, USP

1 mg

Rx only

100 Tablets

SANDOZ

NDC 0781-1032-01

Parstelin (Trifluoperazine Hydrochloride)

Hydrochloride

Tablets, USP

2 mg

Rx only

100 Tablets

SANDOZ

NDC 0781-1034-01

Parstelin (Trifluoperazine Hydrochloride)

Hydrochloride

Tablets, USP

5 mg

Rx only

100 Tablets

SANDOZ

NDC 0781-1036-01

Parstelin (Trifluoperazine Hydrochloride)

Hydrochloride

Tablets, USP

10 mg

Rx only

100 Tablets

SANDOZ

Parstelin pharmaceutical active ingredients containing related brand and generic drugs:

Active ingredient is the part of the drug or medicine which is biologically active. This portion of the drug is responsible for the main action of the drug which is intended to cure or reduce the symptom or disease. The other portions of the drug which are inactive are called excipients; there role is to act as vehicle or binder. In contrast to active ingredient, the inactive ingredient's role is not significant in the cure or treatment of the disease. There can be one or more active ingredients in a drug.


Parstelin available forms, composition, doses:

Form of the medicine is the form in which the medicine is marketed in the market, for example, a medicine X can be in the form of capsule or the form of chewable tablet or the form of tablet. Sometimes same medicine can be available as injection form. Each medicine cannot be in all forms but can be marketed in 1, 2, or 3 forms which the pharmaceutical company decided based on various background research results.
Composition is the list of ingredients which combinedly form a medicine. Both active ingredients and inactive ingredients form the composition. The active ingredient gives the desired therapeutic effect whereas the inactive ingredient helps in making the medicine stable.
Doses are various strengths of the medicine like 10mg, 20mg, 30mg and so on. Each medicine comes in various doses which is decided by the manufacturer, that is, pharmaceutical company. The dose is decided on the severity of the symptom or disease.


Parstelin destination | category:

Destination is defined as the organism to which the drug or medicine is targeted. For most of the drugs what we discuss, human is the drug destination.
Drug category can be defined as major classification of the drug. For example, an antihistaminic or an antipyretic or anti anginal or pain killer, anti-inflammatory or so.


Parstelin Anatomical Therapeutic Chemical codes:

A medicine is classified depending on the organ or system it acts [Anatomical], based on what result it gives on what disease, symptom [Therapeutical], based on chemical composition [Chemical]. It is called as ATC code. The code is based on Active ingredients of the medicine. A medicine can have different codes as sometimes it acts on different organs for different indications. Same way, different brands with same active ingredients and same indications can have same ATC code.


Parstelin pharmaceutical companies:

Pharmaceutical companies are drug manufacturing companies that help in complete development of the drug from the background research to formation, clinical trials, release of the drug into the market and marketing of the drug.
Researchers are the persons who are responsible for the scientific research and is responsible for all the background clinical trials that resulted in the development of the drug.


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References

  1. Dailymed."TRANYLCYPROMINE SULFATE TABLET [PAR PHARMACEUTICAL, INC.]". https://dailymed.nlm.nih.gov/dailym... (accessed August 28, 2018).
  2. Dailymed."TRIFLUOPERAZINE HYDROCHLORIDE TABLET, FILM COATED [SANDOZ INC]". https://dailymed.nlm.nih.gov/dailym... (accessed August 28, 2018).
  3. Dailymed."TRIFLUOPERAZINE HYDROCHLORIDE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailym... (accessed August 28, 2018).

Frequently asked Questions

Can i drive or operate heavy machine after consuming Parstelin?

Depending on the reaction of the Parstelin after taken, if you are feeling dizziness, drowsiness or any weakness as a reaction on your body, Then consider Parstelin not safe to drive or operate heavy machine after consumption. Meaning that, do not drive or operate heavy duty machines after taking the capsule if the capsule has a strange reaction on your body like dizziness, drowsiness. As prescribed by a pharmacist, it is dangerous to take alcohol while taking medicines as it exposed patients to drowsiness and health risk. Please take note of such effect most especially when taking Primosa capsule. It's advisable to consult your doctor on time for a proper recommendation and medical consultations.

Is Parstelin addictive or habit forming?

Medicines are not designed with the mind of creating an addiction or abuse on the health of the users. Addictive Medicine is categorically called Controlled substances by the government. For instance, Schedule H or X in India and schedule II-V in the US are controlled substances.

Please consult the medicine instruction manual on how to use and ensure it is not a controlled substance.In conclusion, self medication is a killer to your health. Consult your doctor for a proper prescription, recommendation, and guidiance.

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Review

sdrugs.com conducted a study on Parstelin, and the result of the survey is set out below. It is noteworthy that the product of the survey is based on the perception and impressions of the visitors of the website as well as the views of Parstelin consumers. We, as a result of this, advice that you do not base your therapeutic or medical decisions on this result, but rather consult your certified medical experts for their recommendations.

Visitor reports

Visitor reported useful

No survey data has been collected yet

Visitor reported side effects

No survey data has been collected yet

One visitor reported price estimates

What is your opinion about drug cost? Did you feel the cost is apt, or did you feel it is expensive?
The report given by the sdrugs.com website users shows the following figures about several people who felt the medicine Parstelin is expensive, and the medicine is not expensive. The results are mixed. The perception of the cost of the medicine to be expensive or not depends on the brand name of the medicine, country, and place where it is sold, and the affordability of the patient. You can choose a generic drug in the place of the branded drug to save the cost. The efficiency of the medicine will not vary if it is generic or a branded one.
Visitors%
Not expensive1
100.0%

Four visitors reported frequency of use

How often in a day do you take the medicine?
Are you taking the Parstelin drug as prescribed by the doctor?

Few medications can be taken Once in a day more than prescribed when the doctor's advice mentions the medicine can be taken according to frequency or severity of symptoms. Most times, be very careful and clear about the number of times you are taking the medication. The report of sdrugs.com website users about the frequency of taking the drug Parstelin is mentioned below.
Visitors%
Once in a day2
50.0%
Twice in a day2
50.0%

Visitor reported doses

No survey data has been collected yet

Two visitors reported time for results

What is the time duration Parstelin drug must be taken for it to be effective or for it to reduce the symptoms?
Most chronic conditions need at least some time so the dose and the drug action gets adjusted to the body to get the desired effect. The stastistics say sdrugs.com website users needed 1 month to notice the result from using Parstelin drug. The time needed to show improvement in health condition after using the medicine Parstelin need not be same for all the users. It varies based on other factors.
Visitors%
1 month1
50.0%
> 3 month1
50.0%

Visitor reported administration

No survey data has been collected yet

Two visitors reported age

Visitors%
16-291
50.0%
6-151
50.0%

Visitor reviews


There are no reviews yet. Be the first to write one!


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The information was verified by Dr. Rachana Salvi, MD Pharmacology

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