Promazine

284.4191

284.42

200-382-0

O9M39HTM5W

31447

DTXSID2023517

Oily liq

N - Nervous system

31.8

4.3

Solid

1.133g/cm3

<25 °C

203-210 °C @ Press: 0.3 Torr

203.4ºC

1.6000 (estimate)

H2O: 14.22mg/L(24 ºC)

The product should be stored at controlled room temperature and protected from freezing and light.

LD50 oral in rat: 350mg/kg

Amine odor

Alkaline reaction

9.36None

9.36

161.5 Ų [M+H]+ [CCS Type: TW, Method: Major Mix IMS/Tof Calibration Kit (Waters)]

Decomp at 181 °C (microblock); Hygroscopic; Aq soln are slightly acid to litmus /Hydrochloride/|PRACTICALLY ODORLESS /HYDROCHLORIDE/|pH of 5% soln between 4.2 & 5.2 /Hydrochloride/|White to slightly yellow crystals /Hydrochloride/|1 g dissolves in about 3 ml water /Hydrochloride/

SO7000000

OXIDIZES UPON PROLONGED EXPOSURE TO AIR & ACQUIRES BLUE OR PINK COLOR /HYDROCHLORIDE/

P261, P264, P270, P272, P273, P280, P301+P312, P302+P352, P321, P330, P333+P313, P363, P391, P501

H302

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).

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P261, P264, P270, P272, P273, P280, P301+P312, P302+P352, P321, P330, P333+P313, P363, P391, and P501|Aggregated GHS information provided by 157 companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Side effects include: extrapyramidal symptoms, drowsiness, weight gain, dry mouth, constipation, endocrine effects (such as gynaecomastia and menstrual disturbance), sensitivity to sunlight and haemolytic anaemia.

RABBIT, RAT, & SHEEP TRIALS INDICATE IT MAY HELP REDUCE TOXIC EFFECTS OF CARBON TETRACHLORIDE. ... HAS INCR TOXICITY OF ORGANOPHOSPHORUS OR OTHER ACETYLCHOLINESTERASE INHIBITORS & PROCAINE.|...PHENOTHIAZINES...MAY PRODUCE ADDITIVE HYPOTENSIVE EFFECTS WITH PROPRANOLOL. /PHENOTHIAZINES/|...OTHER ANTIPSYCHOTIC DRUGS ... MAY BLOCK ANTIHYPERTENSIVE EFFECTS OF GUANETHIDINE ... /PHENOTHIAZINES/|Additive QT interval prolongation may increase the risk of ventricular tachycardia when /probucol is used with phenothiazines/. /Phenothiazines/|For more Interactions (Complete) data for PROMAZINE (31 total), please visit the HSDB record page.

LD50 Rat oral 350 mg/kg|LD50 Rat sc 192 mg/kg|LD50 Rat iv 14,500 ug/kg|LD50 Mouse oral 401 mg/kg|For more Non-Human Toxicity Values (Complete) data for PROMAZINE (8 total), please visit the HSDB record page.

94%

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

Used as an adjunct for short term treatment of moderate and severe psychomotor agitation. Also used to treat agitation or restlessness in the elderly.

Antiemetics; Antipsychotic Agents, Phenothiazine; Dopamine Antagonists|EFFECTIVE IN MGMNT OF MANIFESTATIONS OF PSYCHOTIC DISORDERS. IT IS PROBABLY EFFECTIVE FOR...RELIEF OF APPREHENSION PRIOR TO SURGERY, & FOR REDUCING AGITATION & TENSION, ASSOC WITH MILD ALCOHOL WITHDRAWAL UNDER SUPERVISION.|IT IS ALSO SIMILAR TO CHLORPROMAZINE IN ITS ACTIONS, BUT ITS POTENCY...LOWER.|MEDICATION (VET): EXTENSIVE, TO CONTROL INTRACTABLE ANIMALS, RELIEVE PAIN, CONTROL MOTION SICKNESS, FACILITATE HANDLING & EXAMINATION, POTENTIATE GENERAL ANESTHETICS, & ENHANCE BENEFITS OF LOCAL ANESTHETICS. USED TO MINIMIZE WT LOSS & CALM CATTLE DURING SHIPPING, AS SURGICAL AID, IN CALMING WILD OBSTETRICAL PT...|For more Therapeutic Uses (Complete) data for PROMAZINE (7 total), please visit the HSDB record page.

PROMAZINE [SPARINE] IS OBSOLETE BECAUSE IT HAS EXTREMELY WEAK ANTIPSYCHOTIC ACTION & CAUSES GREATER INCIDENCE OF ADVERSE EFFECTS.|...PROMAZINE IS CONTRAINDICATED IN STUPOROUS OR PRECOMATOSE PT, AS WELL AS IN THOSE WITH CARDIAC OR CEREBROVASCULAR INSUFFICIENCY. ANTICHOLINERGIC-LIKE ACTIONS OF PROMAZINE MAY BE DETRIMENTAL IN PT WITH ANGLE-CLOSURE GLAUCOMA.|SINCE THESE AGENTS HAVE ANTIEMETIC PROPERTIES, THEY MAY MASK SIGNS OF DRUG OVERDOSAGE & OBSCURE SYMPTOMS OF BRAIN TUMOR OR INTESTINAL OBSTRUCTION. ... SHOULD ALSO BE USED WITH EXTREME CAUTION IN PT WITH CARDIOVASCULAR DISEASE, IMPAIRED LIVER FUNCTION, OR WITH HISTORY OF GASTRIC ULCER... /PHENOTHIAZINES/|ALTHOUGH SOME OF MORE SERIOUS TOXIC EFFECTS OF CHLORPROMAZINE HAVE NOT BEEN ENCOUNTERED WITH PROMAZINE, IT SHOULD BE USED WITH SAME DEGREE OF CAUTION.|For more Drug Warnings (Complete) data for PROMAZINE (25 total), please visit the HSDB record page.

4. 4= VERY TOXIC: PROBABLE ORAL LETHAL DOSE (HUMAN) 50-500 MG/KG, BETWEEN 1 TEASPOON & 1 OZ FOR 70 KG PERSON (150 LB).|Toxic dose: 100 ug/dL /From table/

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

Promazine belongs to a group of medications known as the phenothiazine antipsychotics. It acts by blocking a variety of receptors in the brain, particularly dopamine receptors. Dopamine is involved in transmitting signals between brain cells. When there is an excess amount of dopamine in the brain it causes over-stimulation of dopamine receptors. These receptors normally act to modify behaviour and over-stimulation may result in psychotic illness. Promazine hydrochloride blocks these receptors and stops them becoming over-stimulated, thereby helping to control psychotic illness. Promazine has weak extrapyramidal and autonomic side effects which lead to its use in the elderly, for restless or psychotic patients. Its anti-psychotic effect is also weaker and it is not useful in general psychiatry.

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.)|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 used to prevent NAUSEA or VOMITING. (See all compounds classified as Antiemetics.)

Absorption may be erratic and peak plasma concentrations show large interindividual differences.|IV ADMIN RESULTS PEAK IN ABOUT 5 MIN, IM IN ABOUT 20-30 MIN, ORAL IN ABOUT 1-2 HR. PARENTERAL EFFECTS ARE MORE PREDICTABLE, & USUALLY REQUIRE ABOUT HALF ORAL DOSAGE FOR SOME COMPARABLE EFFECTS.

Hepatic, primarily to N-desmethylpromazine and promazine sulfoxide.|YIELDS DEMETHYLPROMAZINE, PROMAZINE-N-OXIDE, & PROMAZINE SULFOXIDE IN MAN & IN RAT; YIELDS 3-HYDROXYPROMAZINE & PHENOTHIAZINE IN MAN. /FROM TABLE/|...METAB...BY OXIDATIVE PROCESSES MEDIATED LARGELY BY HEPATIC MICROSOMAL & OTHER DRUG-METABOLIZING ENZYMES. CONJUGATION WITH GLUCURONIC ACID...PROMINENT ROUTE.../PRC: REACTIONS INCL HYDROXYLATION, DEMETHYLATION, SULFOXIDE FORMATION; METABOLIC ALTERATIONS IN SIDE CHAIN MAY ALSO OCCUR/. /PHENOTHIAZINES/|Promazine has known human metabolites that include N-Desmethyl promazine and Promazine 5-sulfoxide.

Promazine is an antagonist at types 1, 2, and 4 dopamine receptors, 5-HT receptor types 2A and 2C, muscarinic receptors 1 through 5, alpha(1)-receptors, and histamine H1-receptors. Promazine's antipsychotic effect is due to antagonism at dopamine and serotonin type 2 receptors, with greater activity at serotonin 5-HT2 receptors than at dopamine type-2 receptors. This may explain the lack of extrapyramidal effects. Promazine does not appear to block dopamine within the tubero-infundibular tract, explaining the lower incidence of hyperprolactinemia than with typical antipsychotic agents or risperidone. Antagonism at muscarinic receptors, H1-receptors, and alpha(1)-receptors also occurs with promazine.|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/

HIGH DOSES...FOR PROLONGED PERIODS...STAR-SHAPED OPACITIES...IN ANTERIOR PORTION OF LENS...VISUAL IMPAIRMENT...EPITHELIAL KERATOPATHY, LACRIMATION...PIGMENTARY RETINOPATHY /CHRONIC TOXICITY, HYDROCHLORIDE/|LONG-TERM ADMIN OF HIGH DOSES...MAY RESULT IN PIGMENT DEPOSITIONS IN...BODY TISSUES...BRAIN, HEART, LIVER, KIDNEYS, RETINA..CORNEA /& SKIN, USUALLY YELLOWISH-BROWN BUT MAY BECOME GREYISH-PURPLE/. OCULAR CHANGES...DEPOSITION OF FINE PARTICULATE MATTER IN LENS & CORNEA /CHRONIC TOXICITY, HYDROCHLORIDE/|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/

Hydrochloride, Promazine

PROMAZINE HYDROCHLORIDE NF...INJECTION NF: 25 & 50 MG/ML, 50 & 100 MG/2 ML, 250 & 500 MG/10 ML; SOLN NF: 30 MG & 100 MG/ML. SYRUP NF: 10 MG/5 ML; TABLETS NF: 10, 25, 50, 100, & 200 MG. /HYDROCHLORIDE/

Incompatibilities: incompatible with alkalies, oxidizing agents, heavy metals.|FDA REGULATIONS ESTABLISH ZERO TOLERANCE FOR ITS RESIDUES ON OR IN UNCOOKED TISSUES OF FOOD PRODUCING ANIMALS.|A FEW AVAIL AGENTS...ARE NOW KNOWN TO HAVE INFERIOR ANTIPSYCHOTIC EFFECTS OR...ARE NO LONGER COMMONLY USED IN PSYCHIATRIC PT. THESE INCL...PROMAZINE...

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