Composition: Isopropamide is an inherently long-acting synthetic anticholinergic agent that provides 12-hour antisecretory-antispasmodic activity.
Trifluoperazine is a piperazine phenothiazine derivative with antipsychotic and antiemetic properties. The mode of action of phenothiazines has not been definitely established. Like most phenothiazines, trifluoperazine possesses weak anticholinergic and possibly alpha-adrenergic blocking activities.
Indications And Clinical Uses: Stelabid may be employed to advantage in the treatment of a wide range of gastrointestinal disorders, including such conditions as peptic ulcer, gastritis, hyperchlorhydria, functional diarrhea, irritable or spastic colon, pyloroduodenal irritability, pylorospasm, acute nonspecific gastroenteritis, biliary dyskinesia and chronic cholelithiasis, duodenitis, gastrointestinal spasm; it may also be used to treat genitourinary spasm.
Stelabid is particularly indicated where anxiety, tension, worry, or other emotional factors are thought to be wholly or partially responsible for the digestive dysfunction. Since both components of Stelabid are inherently long-acting, a single tablet twice daily (every 12 hours) can provide continuous 24-hour control of symptoms of ulcer and other gastrointestinal disorders.
In addition to the convenience of twice-daily dosage, Stelabid tablets can provide these significant therapeutic advantages: continuous reduction of gastric secretion; continuous inhibition of spasm and motility; continuous relief of anxiety and tension; continuous control of nausea and vomiting.
Contraindications: In comatose states and in the presence of glaucoma, cardiospasm, obstructive uropathy (e.g., bladder neck obstruction due to prostatic hypertrophy) or obstructive lesions of the gastrointestinal tract (as in achalasia, obstructive or paralytic ileus, pyloroduodenal stenosis, etc.), intestinal atony of the elderly or debilitated patient, severe ulcerative colitis, toxic megacolon complicating ulcerative colitis.:
Because of the antiemetic action of the trifluoperazine component, Stelabid should not be used where nausea and vomiting are believed to be evidence of intestinal obstruction or brain tumor.
Precautions: Use with caution in elderly patients, in patients with cardiac impairment, hyperthyroidism, or hiatal hernia associated with reflux esophagitis (anticholinergic drugs may aggravate this condition).
Since the iodine in isopropamide iodide may alter PBI test results.
Clinical experience has demonstrated that trifluoperazine has a wide margin of safety and that there is little likelihood of blood or liver toxicity. However, such adverse effects have been reported, and the physician should be aware of their possible occurrence.
Hypotension has not been a problem with trifluoperazine. Nevertheless, adequate precautions should be taken when the drug is administered to patients with impaired cardiovascular function.
Trifluoperazine therapy may produce an increase in mental and physical activity. In certain instances, this effect may not be desirable. For example, some patients with angina pectoris have complained of increased pain while taking trifluoperazine. Therefore, if Stelabid is used in angina patients, they should be observed carefully and, if an unfavorable response is noted, the drug should be withdrawn.
Trifluoperazine’s potent antiemetic action may mask signs of overdosage of toxic drugs or may obscure the diagnosis of conditions such as intestinal obstruction, and brain tumor.
Pregnancy and Lactation: Use during pregnancy should be restricted to those cases where the potential benefit to the mother outweighs the potential risk to the fetus.
Adequate human data on use during lactation and adequate animal reproduction studies are not available.
Adverse Reactions: May be those of either component. The usual anticholinergic side effects–dry mouth, blurred vision, urinary hesitancy and retention, and constipation–have been encountered with Stelabid. Iodine skin rash may occur rarely. A few patients sensitive to phenothiazine compounds may experience a transient unpleasant agitation, or jitteriness, characterized by restlessness and sometimes by insomnia. These symptoms often disappear spontaneously. Where the effect is particularly bothersome, the concomitant administration of a mild sedative may be helpful.
Phenothiazines can, in some patients on long-term therapy, cause tardive dyskinesia which can last for months or years; the risk appears greater in elderly patients.
Common side effects are:
- Blurred vision;
- Muscle weakness;
- Faintness on standing up;
- Dry mouth;
- Loss of appetite;
- Water retention;
- Eye problems;
- Weight gain;
- Difficulty in urination;
- Abnormally rapid heartbeat;
- Low blood pressure;
- Absence of menstruation;
- Neuroleptic malignant syndrome;
- Blood dyscrasias;
- Dryness of mouth;
- Dilated pupils;
- Rapid pulse;
Symptoms And Treatment Of Overdose: Symptoms may be those of either isopropamide or trifluoperazine overdosage.
Isopropamide: May include dryness of mouth, dysphagia, thirst, blurred vision, dilated pupils, photophobia, fever, rapid pulse and respiration, disorientation. Depression and circulatory collapse may result from severe overdosage.
Trifluoperazine: Primarily, involvement of the extrapyramidal mechanism(s) producing some of the dystonic reactions to a more marked degree. Lesser degrees of overdosage may cause muscular twitching, drowsiness or dizziness. Symptoms of gross overdosage may include CNS depression, weakness, tremor, torticollis and dystonia. Agitation and restlessness may occur. Salivation, dysphagia, or disturbances of gait may also be present.
Treatment: Essentially symptomatic and supportive. Early gastric lavage is helpful. Do not attempt to induce emesis because a dystonic reaction of the head or neck may develop that could result in aspiration of vomitus.
Force fluids by mouth or, if necessary, by i.v. administration of glucose 10% in water.
Respiratory depression should be treated promptly by the use of oxygen and stimulants.
If marked excitement is present, one of the short-acting barbiturates or chloral hydrate may be used. Otherwise, do not administer sedation.
Hyperpyrexia may be treated with physical cooling measures.
If hypotension occurs, the standard measures for managing circulatory shock should be initiated, e.g., i.v. fluids and/or vasoconstrictors. If it is desirable to administer a vasoconstrictor, norepinephrine or phenylephrine is 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. If administration of a stimulant is desirable, amphetamine or caffeine and sodium benzoate is recommended. Stimulants that may cause convulsions (e.g., picrotoxin or pentylenetetrazol) should be avoided. Extrapyramidal symptoms may be treated with antiparkinsonism drugs (except levodopa), barbiturates or diphenhydramine.
While pilocarpine or similar drugs are sometimes recommended for the relief of dry mouth, many authorities feel that these drugs are not indicated, since they relieve the minor peripheral effect but do not influence the more serious central effects, and thus may merely mask signs of drug activity.
If photophobia occurs, the patient should be kept in a darkened room.
It is not known whether isopropamide is dialyzable. Limited experience indicates that phenothiazines are not dialyzable.
Dosage And Administration: Adults: 1 tablet twice daily (every 12 hours). The No. 2 strength is recommended for the majority of patients. Where there is relatively little psychic distress, the No. 1 strength may be preferred. Stelabid Forte will be especially useful for those patients in whom a greater degree of antispasmodic and antisecretory action is desired.
Availability And Storage: No. 1: Each round, biconvex, maize-colored, film-coated tablet, monogrammed SKF P90, contains: trifluoperazine 1 mg (present as trifluoperazine HCl 1.18 mg) and isopropamide 5 mg (present as isopropamide iodide 6.8 mg). Nonmedicinal ingredients: candelilla wax, cellulose, cosmetic ochre no. 3506, lactose, magnesium stearate, Opadry clear, Opadry yellow, sodium starch glycolate and talc. Energy: 1.63 kJ (0.39 kcal). Lactose: 94.5 mg. Sodium: <1 mmol (0.0875 mg). Bottles of 100.
No. 2: Each round, biconvex, maize-colored, film-coated tablet, monogrammed SKF P91, contains: trifluoperazine 2 mg (present as trifluoperazine HCl 2.36 mg) and isopropamide 5 mg (present as isopropamide iodide 6.8 mg). Nonmedicinal ingredients: candelilla wax, cellulose, cosmetic ochre no. 3506, lactose, magnesium stearate, Opadry clear, Opadry yellow, sodium starch glycolate and talc. Energy: 2.24 kJ (0.53 kcal). Lactose: 129.7 mg. Sodium: <1 mmol (0.105 mg). Bottles of 100.
Forte: Each round, biconvex, maize-colored, film-coated tablet, monogrammed SKF P92, contains: trifluoperazine 2 mg (present as trifluoperazine HCl 2.36 mg) and isopropamide 7.5 mg (present as isopropamide iodide 10.2 mg). Nonmedicinal ingredients: candelilla wax, cellulose, cosmetic ochre no. 3506, lactose, magnesium stearate, Opadry clear, Opadry yellow, sodium starch glycolate and talc. Energy: 2.99 kJ (0.712 kcal). Lactose: 173.3 mg. Sodium: <1 mmol (0.175 mg). Bottles of 100.
Additional Info: This instruction for use is given in informative purposes. Every application of this medicine should be approved by your healthcare provider. Only he is able to define the right dosage, side effects and contraindications.
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