Butaperazine

409.592

409.59

211-493-9

TXP4T9106S

DTXSID1022712

N - Nervous system

2934300000

52.1

4.85040

MP: 180-182 °C /Maleate/

270-280 °C @ Press: 0.05 Torr

SOL OF THE FREE BASE IN ARTIFICIAL INTESTINAL JUICE WAS 283 MG/100 ML AT PH 6, DECR TO 4.9 MG/100 ML AT PH 8

PRACTICALLY ODORLESS & HAS MODERATELY BITTER TASTE, NOT APPRECIABLY HYGROSCOPIC /MALEATE/|BRIGHT-YELLOW POWDER /MALEATE/|Crystals from carbon tetrachloride /Maleate/

UNSTABLE IN LIGHT (SUBJECT TO OXIDATIVE DEGRADATION) & EXCESSIVE HEAT /MALEATE/

SRP: At the time of review, criteria for land treatment or burial (sanitary landfill) disposal practices are subject to significant revision. Prior to implementing land disposal of waste residue (including waste sludge), consult with environmental regulatory agencies for guidance on acceptable disposal practices.

Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended; 21 U.S.C. 321-392).

THE PHENOTHIAZINES WITH LOW POTENCY...MARKEDLY AFFECT THE ACTIONS OF A NUMBER OF OTHER DRUGS, & COGNIZANCE MUST BE TAKEN OF THIS FACT. ... PATIENTS SHOULD ALSO BE WARNED TO EXPECT ENHANCEMENT OF THE EFFECTS OF ALCOHOL. ...THE PHENOTHIAZINES CAN PROMOTE HYPOTENSION, POSSIBLY DUE TO THEIR ALPHA-ADRENERGIC BLOCKING PROPERTIES. THUS, THE INTERACTION BETWEEN PHENOTHIAZINE AND ANTIHYPERTENSIVES CAN BE QUITE UNPREDICTABLE.|...CONTRAINDICATED IN COMATOSE PT WHO HAVE RECEIVED LARGE AMT OF CENTRAL NERVOUS SYSTEM DEPRESSANT DRUGS (...BARBITURATES, NARCOTICS, ETC)... /PHENOTHIAZINES/|ROUTINE ADMIN OF ANTIPARKINSONISM AGENTS SHOULD BE AVOIDED WITH MOST ANTIPSYCHOTIC DRUG REGIMENS. /PHENOTHIAZINES/|...PHENOTHIAZINES...MAY PRODUCE ADDITIVE HYPOTENSIVE EFFECTS WITH PROPRANOLOL. /PHENOTHIAZINES/|For more Interactions (Complete) data for BUTAPERAZINE (37 total), please visit the HSDB record page.

PHENOTHIAZINES ... MAY APPEAR IN MILK OF NURSING MOTHERS... /PHENOTHIAZINES, HUMAN, ORAL, IM/

Antipsychotic Agents, Phenothiazine|THE PHENOTHIAZINES ARE INDICATED FOR THE MANAGEMENT OF MANIFESTATIONS OF PSYCHIATRIC DISORDERS. /PHENOTHIAZINES/|...SOME CONGENERS, PARTICULARLY POSITION 10-SUBSTITUTED PIPERAZINE DERIV, POSSESS EFFECTIVE ANTIPSYCHOTIC ACTIVITY BUT LACK SEDATIVE PROPERTY. /PIPERAZINE PHENOTHIAZINES/|IN TREATMENT OF ACUTE PSYCHOSES, ONE SHOULD INCR THE DOSE OF ANTIPSYCHOTIC DRUG AS RAPIDLY AS FEASIBLE, OVER A FEW DAYS AT MOST, TO ACHIEVE CONTROL OF SYMPTOMS. THE DOSE IS THEN ADJUSTED DURING THE NEXT SEVERAL WEEKS AS THE PATIENT'S CONDITION WARRANTS. /PHENOTHIAZINES/|For more Therapeutic Uses (Complete) data for BUTAPERAZINE (9 total), please visit the HSDB record page.

SAFE USE...DURING PREGNANCY HAS NOT BEEN ESTABLISHED WITH RESPECT TO POSSIBLE ADVERSE EFFECTS ON FETAL DEVELOPMENT. ...PHENOTHIAZINES...SHOULD BE USED WITH EXTREME CAUTION IN PT WITH HISTORY OF GLAUCOMA OR PROSTATIC HYPERTROPHY. /PHENOTHIAZINES/|... PHENOTHIAZINES ... SHOULD BE USED WITH EXTREME CAUTION, IF AT ALL, IN UNTREATED EPILEPTIC PATIENTS & IN PATIENTS UNDERGOING WITHDRAWAL FROM CENTRAL DEPRESSANTS SUCH AS ALCOHOL, BARBITURATES, AND BENZODIAZEPINES. /PHENOTHIAZINES/|A VARIETY OF NEUROLOGICAL SYNDROMES, INVOLVING PARTICULARLY THE EXTRAPYRAMIDAL SYSTEM, OCCUR ... THESE REACTIONS ARE PARTICULARLY PROMINENT DURING TREATMENT WITH THE HIGH-POTENCY AGENTS (TRICYCLIC PIPERAZINES AND BUTYROPHENONES). /PIPERAZINE PHENOTHIAZINES/|THERAPEUTIC DOSES OF PHENOTHIAZINES MAY CAUSE FAINTNESS, PALPITATION, ... NASAL STUFFINESS, DRY MOUTH, BLURRED VISION, CONSTIPATION, AND, IN MALES WITH PROSTATISM, URINARY RETENTION. MOST TROUBLESOME SIDE EFFECT IS ORTHOSTATIC HYPOTENSION, WHICH MAY RESULT IN SYNCOPE. /PHENOTHIAZINES/|For more Drug Warnings (Complete) data for BUTAPERAZINE (8 total), please visit the HSDB record page.

TOLERANCE TO ANTIPSYCHOTIC DRUGS & CROSS-TOLERANCE AMONG AGENTS ... DEMONSTRABLE IN BEHAVIORAL & BIOCHEM EXPT IN ANIMALS, PARTICULARLY THOSE DIRECTED TOWARD EVALUATION OF BLOCKADE OF DOPAMINERGIC RECEPTORS IN BASAL GANGLIA. ... ONE CORRELATE OF TOLERANCE IN FOREBRAIN DOPAMINERGIC SYSTEMS IS DEVELOPMENT OF DISUSE SUPERSENSITIVITY OF THOSE SYSTEMS ... THIS MECHANISM MAY UNDERLIE ... WITHDRAWAL-EMERGENT DYSKINESIAS (CHOREOATHETOSIS ON ABRUPT DISCONTINUATION OF ANTIPSYCHOTIC DRUGS, ESP FOLLOWING PROLONGED USE OF HIGH DOSES ...). /PHENOTHIAZINES/

NEUROLEPTIC CONCN-THERAPEUTIC RESPONSE CURVES EXAMINED FOR BUTAPERAZINE IN 10 SCHIZOPHRENIC PT DURING FIRST 12 DAYS OF TREATMENT. RESULTS SHOWED BUTAPERAZINE BOUND TO RED BLOOD CELLS WAS MORE STRONGLY CORRELATED WITH THERAPEUTIC RESPONSE THAN WAS PLASMA CONCN.|IN A STUDY ON 2 GROUPS OF NONRESPONDING SCHIZOPHRENICS AND ONE GROUP OF CLINICALLY RESPONDING PT WITH AFFECTIVE DISORDERS, THE NONRESPONDERS HAD 2 TO 7 TIMES LOWER LEVELS OF BUTAPERAZINE, 40 MG TWICE DAILY, IN PLASMA AND RED BLOOD CELLS AFTER A SINGLE DOSE OR CHRONIC DOSING.|EIGHT OF 10 CHRONIC SCHIZOPHRENIC PT RECEIVED A 40 MG LOADING DOSE OF BUTAPERAZINE AND THEN WERE TITRATED UNTIL A THERAPEUTIC RESPONSE WAS OBTAINED. THRICE DAILY USE OF THE DRUG SHOWED A HIGHER WHOLE BLOOD STEADY STATE DRUG PLASMA LEVEL THAN THE ONCE A DAY USE OF THE SAME TOTAL DAILY DOSE.

AFTER CHRONIC ADMIN OF PIPERAZINE-SUBSTITUTED PHENOTHIAZINE DRUGS...TO RATS, TISSUES CONTAINED DRUG METABOLITES, IN WHICH PIPERAZINE RING FISSION BY MULTIPLE OXIDATIVE N-DEALKYLATION HAD OCCURRED TO GIVE SUBSTITUTED ETHYLENEDIAMINE. /PIPERAZINE PHENOTHIAZINES/|IN RATS & DOGS, PRINCIPAL FECAL METABOLITES OF BUTAPERAZINE DIMALEATE RESULT FROM HYDROXYLATION OF PHENOTHIAZINE RING-SYSTEM & OXIDATIVE N-DEMETHYLATION. BUTAPERAZINE SULFOXIDE, BUTAPERAZINE SULFONE, & REDN PRODUCT OF BUTYRYL SIDE-CHAIN CARBONYL GROUP MAKE UP MINOR METABOLITES. /DIMALEATE/

BUTAPERAZINE (10-60 MG ORALLY) HAD AVG PEAK SERUM LEVELS OF 215 NG/ML IN HUMANS AND AN INITIAL RAPID PHASE HALF-LIFE OF 4 HR AND A SLOWER PHASE HALF-LIFE OF 12 HR. SERUM BUTAPERAZINE LEVELS WERE PROPORTIONAL TO THE DOSE ADMINISTERED.

THERE IS AN ADENYLATE CYCLASE IN LIMBIC SYSTEM, AS WELL AS IN CAUDATE NUCLEUS, THAT IS SPECIFICALLY ACTIVATED BY DOPAMINE. ...ACTIVATION OF...ENZYME IS... BLOCKED BY...PHENOTHIAZINES. ...THERAPEUTIC EFFICACY & SIDE EFFECTS MAY RELATE TO INHIBITION OF DOPAMINE ACTIVATION OF ADENYLATE CYCLASE. /PHENOTHIAZINES/|...PHENOTHIAZINES, BLOCK DOPAMINE RECEPTORS & INCR TURNOVER RATE OF DOPAMINE IN CORPUS STRIATUM. INCR TURNOVER RATE IS BELIEVED TO BE RESULT OF NEURONAL FEEDBACK MECHANISM. ...FIRING OF.../IDENTIFIED DOPAMINERGIC NEURONS IN SUBSTANTIA NIGRA & VENTRAL TEGMENTAL AREAS/ IS INCR BY ANTIPSYCHOTIC PHENOTHIAZINES. /PHENOTHIAZINES/

EXTRAPYRAMIDAL SYMPTOMS...RELIEVED WITH BARBITURATES, METHYLPHENIDATE HYDROCHLORIDE...ANTI-PARKINSON DRUGS...BENZTROPINE MESYLATE...TRIHEXYPHENIDYL HYDROCHLORIDE...DIPHENHYDRAMINE HYDROCHLORIDE...IN SEVERE CASES, SUPPORTIVE THERAPY...MAINTAINING CLEAR AIRWAY & ADEQUATE HYDRATION. /HYDROCHLORIDE/

butaperazine

TABLETS: 5, 10, & 25 MG (OF BASE AS MALEATE). /MALEATE/

A FEW AVAIL AGENTS...ARE NOW KNOWN TO HAVE INFERIOR ANTIPSYCHOTIC EFFECTS OR...ARE NO LONGER COMMONLY USED IN PSYCHIATRIC PT. THESE INCL BUTAPERAZINE...

SUBSTRATES: HUMAN PLASMA & RED BLOOD CELLS; DETERMINATIVE PROCEDURE: GAS CHROMATOGRAPHY.|GAS LIQUID CHROMATOGRAPHY AND RADIORECEPTOR ANALYSIS OF BUTAPERAZINE IN HUMAN PLASMA ARE COMPARED.|DETECTION OF BUTAPERAZINE BY UV ABSORPTION SPECTROPHOTOMETRY OR AMPEROMETRY IN BLOOD AND PLASMA IS DESCRIBED. UV ABSORPTION IS SUITABLE DOWN TO 10 NG/ML. BELOW THIS LEVEL AMPEROMETRY IS PREFERABLE.|FLUOROMETRIC METHOD DESCRIBED FOR DETERMINATION OF BUTAPERAZINE IN PLASMA & RED BLOOD CELLS.

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