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治療オプション:
Kovalenko Svetlana Olegovna 、薬局による医学的評価、 最終更新日:14.03.2022
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同じ成分を持つトップ20の薬:
テンサリルの使用は、QTc間隔を延長することが知られている他の薬物と組み合わせて、および先天性QT症候群または心不整脈の病歴のある患者では避けてください。.
このアイソザイムを阻害する還元チトクロームP450 2D6アイソザイム活性薬(例:.、フルオキセチンとパロキセチン)および他の特定の薬物(例:.、フルボキサミン、プロプラノロール、およびピンドロール)は、テンサリルの代謝をかなり阻害するようです。. 結果として生じるテンサリルの上昇は、テンサリルに関連するQTc間隔の延長を増大させると予想され、トルサードドポワント型不整脈などの深刻な、潜在的に致命的な心不整脈のリスクを高める可能性があります。. このようなリスクの増加は、テンサリルをQTc間隔を延長する他の薬剤と同時投与することの相加効果からも生じる可能性があります。.
したがって、テンサリルはこれらの薬物や、正常な人口の約7%を占める患者には禁 ⁇ であり、遺伝的欠陥があり、P450 2D6の活性のレベルが低下することが知られています(参照)。 警告。 と。 注意。)。. 他のフェノチアジンと同様に、テンサリルは、薬物誘発性中枢神経系うつ病を含むあらゆる原因による重度の中枢神経系うつ病または ⁇ 睡状態では禁 ⁇ です(参照)。 警告。)。. また、極端な程度の高血圧または低血圧の心臓病は、フェノチアジン投与の禁 ⁇ であることにも注意してください。.
WARNINGS
Potential for Proarrhythmic Effects
DUE TO THE POTENTIAL FOR SIGNIFICANT, POSSIBLY LIFE-THREATENING, PROARRHYTHMIC EFFECTS WITH Tensaril TREATMENT, Tensaril SHOULD BE RESERVED FOR USE IN THE TREATMENT OF SCHIZOPHRENIC PATIENTS WHO FAIL TO SHOW AN ACCEPTABLE RESPONSE TO ADEQUATE COURSES OF TREATMENT WITH OTHER ANTIPSYCHOTIC DRUGS, EITHER BECAUSE OF INSUFFICIENT EFFECTIVENESS OR THE INABILITY TO ACHIEVE AN EFFECTIVE DOSE DUE TO INTOLERABLE ADVERSE EFFECTS FROM THOSE DRUGS. CONSEQUENTLY, BEFORE INITIATING TREATMENT WITH Tensaril, IT IS STRONGLY RECOMMENDED THAT A PATIENT BE GIVEN AT LEAST TWO TRIALS, EACH WITH A DIFFERENT ANTIPSYCHOTIC DRUG PRODUCT, AT AN ADEQUATE DOSE, AND FOR AN ADEQUATE DURATION. Tensaril HAS NOT BEEN SYSTEMATICALLY EVALUATED IN CONTROLLED TRIALS IN THE TREATMENT OF REFRACTORY SCHIZOPHRENIC PATIENTS AND ITS EFFICACY IN SUCH PATIENTS IS UNKNOWN.
A crossover study in nine healthy males comparing single doses of Tensaril 10 mg and 50 mg with placebo demonstrated a dose-related prolongation of the QTc interval. The mean maximum increase in QTc interval following the 50 mg dose was about 23 msec; greater prolongation may be observed in the clinical treatment of unscreened patients.
Prolongation of the QTc interval has been associated with the ability to cause torsade de pointes-type arrhythmias, a potentially fatal polymorphic ventricular tachycardia, and sudden death. There are several published case reports of torsade de pointes and sudden death associated with Tensaril treatment. A causal relationship between these events and Tensaril therapy has not been established but, given the ability of Tensaril to prolong the QTc interval, such a relationship is possible.
Certain circumstances may increase the risk of torsade de pointes and/or sudden death in association with the use of drugs that prolong the QTc interval, including 1) bradycardia, 2) hypokalemia, 3) concomitant use of other drugs that prolong the QTc interval, 4) presence of congenital prolongation of the QT interval, and 5) for Tensaril in particular, its use in patients with reduced activity of P450 2D6 or its co-administration with drugs that may inhibit P450 2D6 or by some other mechanism interfere with the clearance of Tensaril (see CONTRAINDICATIONS and PRECAUTIONS).
It is recommended that patients being considered for Tensaril treatment have a baseline ECG performed and serum potassium levels measured. Serum potassium should be normalized before initiating treatment and patients with a QTc interval greater than 450 msec should not receive Tensaril treatment. It may also be useful to periodically monitor ECG's and serum potassium during Tensaril treatment, especially during a period of dose adjustment. Tensaril should be discontinued in patients who are found to have a QTc interval over 500 msec.
Patients taking Tensaril who experience symptoms that may be associated with the occurrence of torsade de pointes (e.g., dizziness, palpitations, or syncope) may warrant further cardiac evaluation; in particular, Holter monitoring should be considered.
Tardive Dyskinesia
Tardive dyskinesia, a syndrome consisting of potentially irreversible, involuntary, dyskinetic movements may develop in patients treated with 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 antipsychotic treatment, which patients are likely to develop the syndrome. Whether antipsychotic 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 antipsychotic 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 antipsychotic treatment is withdrawn. Antipsychotic 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, antipsychotics should be prescribed in a manner that is most likely to minimize the occurrence of tardive dyskinesia. Chronic antipsychotic treatment should generally be reserved for patients who suffer from a chronic illness that, 1) is known to respond to antipsychotic 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 antipsychotics, 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 Information for Patients and ADVERSE REACTIONS.)
It has been suggested in regard to phenothiazines in general, that people who have demonstrated a hypersensitivity reaction (e.g., blood dyscrasias, jaundice) to one may be more prone to demonstrate a reaction to others. Attention should be paid to the fact that phenothiazines are capable of potentiating central nervous system depressants (e.g., anesthetics, opiates, alcohol, etc.) as well as atropine and phosphorus insecticides. Physicians should carefully consider benefit versus risk when treating less severe disorders. Reproductive studies in animals and clinical experience to date have failed to show a teratogenic effect with Tensaril. However, in view of the desirability of keeping the administration of all drugs to a minimum during pregnancy, Tensaril should be given only when the benefits derived from treatment exceed the possible risks to mother and fetus.
Neuroleptic Malignant Syndrome (NMS)
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.
Central Nervous System Depressants
As in the case of other phenothiazines, Tensaril is capable of potentiating central nervous system depressants (e.g., alcohol, anesthetics, barbiturates, narcotics, opiates, other psychoactive drugs, etc.) as well as atropine and phosphorus insecticides. Severe respiratory depression and respiratory arrest have been reported when a patient was given a phenothiazine and a concomitant high dose of a barbiturate.
PRECAUTIONS
Leukopenia and/or agranulocytosis and convulsive seizures have been reported but are infrequent. In schizophrenic patients with epilepsy, anticonvulsant medication should be maintained during treatment with Tensaril. Pigmentary retinopathy, which has been observed primarily in patients taking larger than recommended doses, is characterized by diminution of visual acuity, brownish coloring of vision, and impairment of night vision; examination of the fundus discloses deposits of pigment. The possibility of this complication may be reduced by remaining within the recommended limits of dosage.
Where patients are participating in activities requiring complete mental alertness (e.g., driving) it is advisable to administer the phenothiazines cautiously and to increase the dosage gradually. Female patients appear to have a greater tendency to orthostatic hypotension than male patients. The administration of epinephrine should be avoided in the treatment of drug-induced hypotension in view of the fact that phenothiazines may induce a reversed epinephrine effect on occasion. Should a vasoconstrictor be required, the most suitable are levarterenol and phenylephrine.
Antipsychotic 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 prescription 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 studies 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.
観察された症状の多くは、以下に説明する副作用の延長です。 悪影響. テンサリルは過剰摂取で有毒である可能性があり、心臓毒性が特に懸念されます。. 過剰摂取患者の頻繁なECGとバイタルサインモニタリングが推奨されます。. 影響が遅延するリスクがあるため、数日間の観察が必要になる場合があります。.
兆候と症状。
フェノチアジンが関与する急性過剰摂取の影響と臨床合併症には、以下が含まれます。
心血管:。 心不整脈、低血圧、ショック、ECGの変化、QTとPRの間隔の増加、非特異的なSTとTの波の変化、徐脈、洞性頻脈、房室ブロック、心室頻脈、心室細動、トルサードドポワント、心筋うつ病。.
中央神経系:。 鎮静、 ⁇ 体外路効果、混乱、興奮、低体温症、高体温症、落ち着きのなさ、発作、失読症、 ⁇ 睡。.
自律神経系:。 散 ⁇ 、縮 ⁇ 、乾燥肌、口渇、鼻づまり、尿閉、かすみ目。.
呼吸器:。 呼吸抑制、無呼吸、肺水腫。.
消化管:。 低運動、便秘、イレウス。.
腎臓:。 乏尿、尿毒症。.
フェノチアジンの毒性用量と血中濃度範囲はしっかりと確立されていません。. テンサリルの毒性血中濃度範囲は1 mg / dLから始まり、2〜8 mg / dLが致死濃度範囲であることが示唆されています。.
治療。
気道を確立し、維持する必要があります。. 適切な酸素化と換気を確保する必要があります。.
心血管モニタリングは直ちに開始する必要があり、不整脈の可能性を検出するための継続的な心電図モニタリングを含める必要があります。. 治療には、電解質異常と酸塩基バランスの修正、リドカイン、フェニトイン、イソプロテレノール、心室ペーシング、および除細動の1つ以上の治療介入が含まれる場合があります。. ジソピラミド、プロカインアミド、およびキニジンは、テンサリルの急性過剰摂取の患者に投与すると、追加のQT延長効果をもたらす可能性があり、避ける必要があります(参照)。 警告。 と。
However, we will provide data for each active ingredient