Mesoridazine

386.581

386.57

5XE4NWM740

186066

DTXSID3023265

Oily product

N - Nervous system

68.1

3.9

Solid

1.3g/cm3

128-131 °C

570.5ºC at 760mmHg

298.9ºC

1.694

7.67e-02 g/L

INJECTION HAS PH OF 4.0-5.0 /BESYLATE/

STABLE IN SOLN OF PH 4.0-6.5; SOLN ARE LIGHT-SENSITIVE /BESYLATE/

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).

Oral LD50 is 560 ± 62.5 mg/kg and 644 ± 48 mg/kg in mouse and rat, respectively. Symptoms of overdose may include emesis, muscle tremors, decreased food intake and death associated with aspiration of oral-gastric contents into the respiratory system.

CHLORPROMAZINE & OTHER ANTIPSYCHOTIC DRUGS...MAY BLOCK ANTIHYPERTENSIVE EFFECTS OF GUANETHIDINE. /CHLORPROMAZINE/|INTERACTIONS BETWEEN CHLORPROMAZINE & AMPHETAMINE, ALTHOUGH NOT DOCUMENTED, MAY APPLY TO OTHER PHENOTHIAZINE DERIV. /PHENOTHIAZINES/|PRETREATMENT WITH 3 MG/KG OF MESORIDAZINE-HCL ORALLY WAS MORE EFFECTIVE THAN THIORIDAZINE-HCL (6 MG/KG) IN DECR D-AMPHETAMINE SULFATE INDUCED BEHAVIOR IN DOGS.|Additive QT interval prolongation may increase the risk of ventricular tachycardia when /probucol is used with phenothiazines/. /Phenothiazines/|For more Interactions (Complete) data for MESORIDAZINE (31 total), please visit the HSDB record page.

LD50 MICE INTRAVENOUS 33 MG/KG /BESYLATE/|LD50 MICE SUBCUTANEOUS 611 MG/KG /BESYLATE/|LD50 MICE ORAL 346 MG/KG /BESYLATE/

4%

PHENOTHIAZINES CROSS PLACENTAL BARRIER & MAY APPEAR IN MILK OF NURSING MOTHERS...PHENOTHIAZINES &...METABOLITES...EXCRETED IN URINE, BILE, & FECES. CERTAIN METABOLITES &...FREE DRUGS...DETECTED IN URINE UP TO 6 MO AFTER THERAPY...DISCONTINUED /HUMAN, ORAL, IM/

Used in the treatment of schizophrenia, organic brain disorders, alcoholism and psychoneuroses.

Antipsychotic Agents, Phenothiazine; Dopamine Antagonists|THE ANTIPSYCHOTIC DRUGS HAVE A HIGH THERAPEUTIC INDEX & ARE REMARKABLY SAFE AGENTS. FURTHERMORE, MOST PHENOTHIAZINES HAVE RELATIVELY FLAT DOSE-RESPONSE CURVE AND CAN BE USED OVER WIDE RANGE OF DOSAGES. ...SIDE EFFECTS ARE OFTEN EXTENSIONS OF MANY PHARMACOLOGICAL ACTIONS OF DRUGS... /PHENOTHIAZINES/|...INDICATED FOR MGMNT OF SCHIZOPHRENIA, ORG BRAIN DISORDERS, SYMPTOMS OF ALC WITHDRAWAL, & PSYCHONEUROSES. CLINICAL STUDIES TO DATE INDICATE THAT MESORIDAZINE BESYLATE HAS LOW INCIDENCE OF ADVERSE REACTIONS COMPARED WITH OTHER PHENOTHIAZINES. /BESYLATE/|8 WK THERAPY WITH THIORIDAZINE & MESORIDAZINE BESYLATE. THIORIDAZINE TREATED PT WERE SUPERIOR TO LATTER TREATED PT. IMPLICATIONS FOR CHEMOTHERAPY OF SCHIZOPHRENICS CONSIDERED.|For more Therapeutic Uses (Complete) data for MESORIDAZINE (6 total), please visit the HSDB record page.

NEUROLEPTIC AGENTS ... SHOULD BE USED WITH EXTREME CAUTION, IF @ ALL, IN UNTREATED EPILEPTIC PT & IN PT UNDERGOING WITHDRAWAL FROM CENTRAL DEPRESSANT DRUGS SUCH AS ALCOHOL, BARBITURATES, OR BENZODIAZEPINES. MOST ANTIPSYCHOTIC DRUGS ... CAN BE USED SAFELY IN EPILEPTICS IF MODERATE DOSES ARE ATTAINED GRADUALLY AND IF CONCOMITANT ANTICONVULSANT DRUG THERAPY IS MAINTAINED. /PHENOTHIAZINES/|PHENOTHIAZINES INHIBIT EJACULATION WITHOUT INTERFERING WITH ERECTION. /PHENOTHIAZINES/|WT GAIN & INCR IN APPETITE OCCUR WITH ALL PHENOTHIAZINES... PERIPHERAL EDEMA OCCURS IN 1-3% OF PT & MAY BE OF ENDOCRINE ORIGIN. /PHENOTHIAZINES/|The antipsychotic drugs are not addicting ... However, some degree of physical dependence may occur, with malaise and difficulty in sleeping developing several days after abrupt discontinuation. Tolerance usually develops to the sedative effects ... over a period of days or weeks. Tolerance ... is demonstrable in behavioral and biochemical experiments in animals ... /Antipsychotic drugs/|For more Drug Warnings (Complete) data for MESORIDAZINE (20 total), please visit the HSDB record page.

Mesoridazine, the besylate salt of a metabolite of thioridazine, is a phenothiazine tranquilizer. Pharmacological studies in laboratory animals have established that mesoridazine has a spectrum of pharmacodynamic actions typical of a major tranquilizer. In common with other tranquilizers it inhibits spontaneous motor activity in mice, prolongs thiopental and hexobarbital sleeping time in mice and produces spindles and block of arousal reaction in the EEG of rabbits. It is effective in blocking spinal reflexes in the cut and antagonizes d-amphetamine excitation and toxicity in grouped mice. It shows a moderate adrenergic blocking activity in vitro and in vivo and antagonizes 5-hydroxytryptamine in vivo. Intravenously administered, it lowers the blood pressure of anesthetized dogs. It has a weak antiacetylcholine effect in vitro.

Agents that control agitated psychotic behavior, alleviate acute psychotic states, reduce psychotic symptoms, and exert a quieting effect. They are used in SCHIZOPHRENIA; senile dementia; transient psychosis following surgery; or MYOCARDIAL INFARCTION; etc. These drugs are often referred to as neuroleptics alluding to the tendency to produce neurological side effects, but not all antipsychotics are likely to produce such effects. Many of these drugs may also be effective against nausea, emesis, and pruritus. (See all compounds classified as Antipsychotic Agents.)|Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME. (See all compounds classified as Dopamine Antagonists.)

Well absorbed from the gastrointestinal tract.|TOTAL URINARY & FECAL EXCRETION BY MONKEYS (10 DAY PERIOD) OF THIORIDAZINE WAS 64-76% & 83-92% FOR MESORIDAZINE (FECAL EXCRETION 2-4 TIMES GREATER). GREATER EXCRETION OF LATTER MAY BE DUE TO LESSER OVERALL TISSUE ADSORPTION OR LESS EXTENSIVE ENTERO-HEPATIC CYCLING.|WELL ABSORBED FROM GI TRACT. ONSET & DURATION OF ACTION & METABOLIC FATE... NOT...PRECISELY DETERMINED /HUMAN, ORAL, IM/. IN ANIMAL STUDIES, APPROX 2/3 OF DOSE...EXCRETED IN FECES VIA BILE & 1/3 OF DOSE...EXCRETED IN URINE. /BESYLATE/|PHENOTHIAZINES CROSS PLACENTAL BARRIER & MAY APPEAR IN MILK OF NURSING MOTHERS...PHENOTHIAZINES &...METABOLITES...EXCRETED IN URINE, BILE, & FECES. CERTAIN METABOLITES &...FREE DRUGS...DETECTED IN URINE UP TO 6 MO AFTER THERAPY...DISCONTINUED /HUMAN, ORAL, IM/|PHENOTHIAZINES...ABSORBED WELL FROM GI TRACT & FROM PARENTERAL SITES. GENERALLY...CLEARED FROM PLASMA WITHIN APPROX 3 HR...DISTRIBUTED TO MOST BODY TISSUES...HIGH CONCN OF UNCHANGED DRUG...IN BRAIN...METABOLITES PREDOMINATE IN LUNG, LIVER, KIDNEYS...SPLEEN /HUMAN, ORAL, IM/

THIORIDAZINE-2-SULFOXIDE PROBABLY YIELDS THIORIDAZINE-2,5-DISULFOXIDE IN RAT: ZEHNDER, K ET AL, BIOCHEM PHARMAC, 11, 535 (1962). /FROM TABLE/|Thioridazine 2-sulfoxide is a known human metabolite of Thioridazine.

24 to 48 hours

Based upon animal studies, mesoridazine, as with other phenothiazines, acts indirectly on reticular formation, whereby neuronal activity into reticular formation is reduced without affecting its intrinsic ability to activate the cerebral cortex. In addition, the phenothiazines exhibit at least part of their activities through depression of hypothalamic centers. Neurochemically, the phenothiazines are thought to exert their effects by a central adrenergic blocking action.|...MECHANISM OF ACTION OF ANTIPSYCHOTIC DRUGS WITH RESPECT TO THERAPEUTIC EFFICACY & SIDE EFFECTS MAY RELATE TO INHIBITION OF DOPAMINE ACTIVATION OF ADENYLATE CYCLASE. /PHENOTHIAZINES/

Sudden and unexpected deaths have occurred in patients receiving phenothiazines, especially during long-term administration of the drugs. In some patients, sudden death appeared to result from asphyxia (secondary to failure of the cough reflex) or cardiac arrest. /Phenothiazines/|In general, overdosage of phenothiazines may be expected to produce effects that are extensions of common adverse effects; severe extrapyramidal reactions, hypotension, and sedation have been the principal effects reported. CNS depression progressing to coma with areflexia may occur; patients with early or mild intoxication may experience restlessness, confusion, and excitement. Other reported effects associated with acute phenothiazine overdosage have included tachycardia, ECG changes and cardiac arrhythmias, hypothermia, miosis, tremor, muscle twitching, spasm or rigidity, seizures, muscular hypotonia, ileus, dry mouth, difficulty in swallowing or breathing, cyanosis, and respiratory and/or vasomotor collapse, possibly with sudden apnea. /Phenothiazines/

Mesoridazine

Benzenesulfonate, mesoridazine besylate, NC-123, Lidanar, Lidanil, Serentil. /Besylate/

METHOD FOR HPLC DETERMINATION OF MESORIDAZINE IN WHOLE BLOOD.

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients|Pharmaceuticals