Antipsychotic Medications Anti-psychotic Drugs pipotiazine palmitate, Piportil

Antipsychotic: pipotiazine palmitate, Piportil

Generic Name: pipotiazine palmitate
Brand Name(s): Piportil
Common Use: Antipsychotic

Pipotiazine palmitate is the palmitic ester of pipotiazine, a piperidine phenothiazine with antipsychotic properties and weak sedative activity with prolonged duration of action. The onset of action appears usually within the first 2 to 3 days after injection and the effects of the drug on psychotic symptoms are significant within 1 week. Improvement in symptomatology lasts from 3 to 6 weeks, but adequate control may frequently be maintained with one injection every 4 weeks. However, in view of the variations in individual response, careful supervision is required throughout treatment.

The maintenance treatment of chronic non-agitated schizophrenic patients.

Contraindications

Should not be administered in the presence of circulatory collapse, altered states of consciousness or comatose states, particularly when these are due to intoxication with central depressant drugs e.g., alcohol, hypnotics, narcotics. In severely depressed patients, in the presence of blood dyscrasias, liver disease, renal insufficiency, pheochromocytoma, or in patients with severe cardiovascular disorders or a history of hypersensitivity to phenothiazine derivatives.
Phenothiazine compounds should not be used in patients receiving large doses of hypnotics, due to the possibility of potentiation.

Adverse Side Effects

Neurological:
The side effects most frequently reported are extrapyramidal reactions including tremor, rigidity, akathisia, dystonia, dyskinesia, oculogyric crises, opisthotonos, hyperreflexia and sialorrhea which tend to occur in the first few days after an injection. Pipotiazine tends to produce a higher incidence of extrapyramidal reactions than some other phenothiazine derivatives. Extrapyramidal reactions may be alarming, and the patient should be forewarned and reassured. These reactions may tend to subside as treatment is continued but are often dose related and may respond to a reduction of the dose. Antiparkinsonian medication may be required to control serious reactions or, if intractable, the drug may have to be withdrawn. The information available tends to indicate that persistent tardive dyskinesia results from heavy drug overloading of the extrapyramidal system. Therefore, caution should be exercised to avoid overdosing and the optimum dosage should not be exceeded since this will tend to elicit marked extrapyramidal reactions.

Persistent Tardive Dyskinesia:
May occur in patients on long-term therapy or may be observed after drug therapy has been discontinued. The risk seems to be greater in elderly patients on high doses, especially females. 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. These may be accompanied by involuntary movements of the extremities.
There is no known effective treatment for tardive dyskinesia; antiparkinsonian agents usually do not alleviate the symptoms. 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. The physician may be able to reduce the risk of this syndrome by minimizing the unnecessary use of neuroleptic drugs and reducing the dose or discontinuing the drug, if possible, when manifestations of this syndrome are recognized, particularly in patients over the age of 50.

Behavioral:
Sleep disturbances, drowsiness, fatigue, insomnia, and depression have been reported and may, in severe cases, necessitate reduction in dosage. As with other phenothiazine derivatives, reactivation or aggravation of psychotic processes may be encountered.
Paradoxical effects such as agitation, anxiety, restlessness, excitement and bizarre dreams, have been observed in some patients.

Autonomic Nervous System:
Dry mouth, nausea and constipation were most frequently seen during pipotiazine therapy. Tachycardia, hypotension, syncope, dizziness, blurred vision, vomiting, sweating, nasal congestion, and urinary incontinence have also been observed.
Patients with pheochromocytoma, cerebral vascular or renal insufficiency, or a severe cardiac reserve deficiency such as mitral insufficiency appear to be particularly prone to hypotensive reactions with phenothiazine compounds, and should therefore be observed closely when the drug is administered. Should hypotension occur in patients receiving pipotiazine and a vasopressor agent be required, i.v. levarterenol or phenylephrine should be used, and not epinephrine, since phenothiazine derivatives can reverse the pressor effect of the latter drug.
Other autonomic reactions which have occurred with phenothiazines are salivation, polyuria, glaucoma, bladder paralysis, adynamic ileus, and fecal compaction.

Metabolic and Endocrine:
Anorexia, menstrual irregularities, impotence, and increased thirst have been reported with pipotiazine.
Weight changes, increased appetite, peripheral edema, galactorrhea, gynecomastia, false positive pregnancy tests, and changes in libido have also occurred in patients receiving phenothiazine therapy.

Allergic or Toxic:
Pruritus, dermatitis and rash have been observed with pipotiazine. Other allergic reactions reported with phenothiazine derivatives are erythema, urticaria, seborrhea, eczema, exfoliative dermatitis, and photosensitivity. The possibility of an anaphylactoid reaction should be borne in mind.
Blood dyscrasias including leukopenia, agranulocytosis, pancytopenia, thrombocytopenic or nonthrombocytopenic purpura, eosinophilia, and anemia, have been associated with phenothiazine therapy. Routine blood counts are therefore advisable during prolonged therapy. If any soreness of the mouth, gums or throat or any symptoms of upper respiratory infection occur and confirmatory leukocyte count indicates cellular depression, therapy should be discontinued and other appropriate measures instituted immediately.
Cholestatic jaundice and biliary stasis may be encountered, particularly during the first months of therapy, and require immediate discontinuation of treatment.

Miscellaneous:
The following adverse reactions have been reported in patients receiving phenothiazine derivatives: headache, asthma, laryngeal, cerebral and angioneurotic edema, altered cerebrospinal fluid proteins, systemic lupus erythematosus like syndrome, hyperpyrexia, ECG and EEG changes and hypotension severe enough to cause fatal cardiac arrest. Skin pigmentation, epithelial keratopathy, lenticular and corneal deposits have been associated with long-term administration. Sudden, unexpected and unexplained deaths have been reported in hospitalized psychotic patients receiving phenothiazines. Previous brain damage or seizures may be predisposing factors; high doses should be avoided in known seizure patients. Several patients have shown flare-ups of psychotic behaviour patterns shortly before death. Autopsy findings have usually revealed acute fulminating pneumonia or pneumonitis, aspiration of gastric contents or intramyocardial lesions. Potentiation of CNS depressants (barbiturates, narcotics, analgesics, alcohol, antihistamines), may occur.
Local tolerance to pipotiazine is good and reactions at the site of injection are seldom seen.

Overdose

Severe extrapyramidal manifestations, hypotension, lethargy and sedation are most likely to be observed. Initial hospitalization may be required and close medical supervision should be maintained until symptoms are well under control.

Symptomatic and supportive. When a sufficient amount of time has elapsed or when the patient shows signs of relapse, treatment may be resumed at a lower dosage.

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