Methdilazine hydrochloride

332.89100

332.11100

214-967-3

169091

DTXSID3025548

LIGHT-TAN, CRYSTALLINE POWDER|CRYSTALS FROM ISOPROPYL ALCOHOL

2934300000

31.78000

5.04590

Methdilazine hydrochloride is a white microcrystalline powder with a slight odor. pH (1% aqueous solution) 4.8-6. (NTP, 1992)

187.5-189 °C

430.4ºC at 760mmHg

214.1ºC

1.642

1 G IN 2 ML WATER, 2 ML ALC, 6 ML CHLOROFORM, MORE THAN 10,000 ML ETHER

1.3E-07mmHg at 25°C

SLIGHT, CHARACTERISTIC

BITTER, ANESTHETIC

BETWEEN 4.8 AND 6.0 (1 IN 100 SOLN)

Water soluble. pH (1% aqueous solution) 4.8-6 (NTP, 1992).

Amines, Phosphines, and Pyridines

METHDILAZINE HYDROCHLORIDE is sensitive to exposure to light. (NTP, 1992) An acidic salt. Materials in this group are generally soluble in water. The resulting solutions contain moderate concentrations of hydrogen ions and have pH's of less than 7.0. They react as acids to neutralize bases. These neutralizations generate heat, but less or far less than is generated by neutralization of inorganic acids, inorganic oxoacids, and carboxylic acid. They usually do not react as either oxidizing agents or reducing agents but such behavior is not impossible.

NONH for all modes of transport

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).

Flash point data for this chemical are not available; however, it is probably combustible. (NTP, 1992)

Fires involving this material can be controlled with a dry chemical, carbon dioxide or Halon extinguisher. (NTP, 1992)

SMALL SPILLS AND LEAKAGE: If you spill this chemical, you should dampen the solid spill material with water, then transfer the dampened material to a suitable container. Use absorbent paper dampened with water to pick up any remaining material. Seal your contaminated clothing and the absorbent paper in a vapor-tight plastic bag for eventual disposal. Wash all contaminated surfaces with a soap and water solution. Do not reenter the contaminated area until the Safety Officer (or other responsible person) has verified that the area has been properly cleaned. STORAGE PRECAUTIONS: You should protect this material from exposure to light and store it in a refrigerator. (NTP, 1992)

RECOMMENDED RESPIRATOR: Where the neat test chemical is weighed and diluted, wear a NIOSH-approved half face respirator equipped with an organic vapor/acid gas cartridge (specific for organic vapors, HCl, acid gas and SO2) with a dust/mist filter. (NTP, 1992)

METHDILAZINE HYDROCHLORIDE (3 MG/KG IP) POTENTIATED THE PENTOBARBITONE INDUCED HYPNOSIS IN RATS.|Concurrent use /with alcohol or other CNS depression-producing medications/ may potentiate the CNS depressant effects of either these medications or antihistamines; also, concurrent use of maprotiline or tricyclic antidepressants may potentiate the anticholinergic effects of either antihistamines or these medications. /Antihistamines, phenothiazine-derivative/|Concurrent use /with amphetamines/ may decrease stimulant effects of amphetamines since phenothiazine derivatives produce alpha-adrenergic blockage. /Antihistamines, phenothiazine-derivative/|Anticholinergic effects may be potentiated when /anticholinergics or other medications with anticholinergic activity/ are used concurrently with antihistamines; patients should be advised to report occurrence of gastrointestinal problems promptly since paralytic ileus may occur with concurrent therapy. /Antihistamines, phenothiazine-derivative/|For more Interactions (Complete) data for METHDILAZINE HYDROCHLORIDE (21 total), please visit the HSDB record page.

Use is not recommended in newborn or premature infants because this age group has an increased susceptibility to anticholinergic side effects, such as central nervous system excitation, and an increased tendency toward convulsions. /Antihistamines, phenothiazine-derivative/|The use of phenothiazine-derivative antihistamines is not recommended in infants up to 3 months of age, because of the possible absence or deficiency of detoxifying enzyme and inefficient renal function usually noted in this age group. Also, increased susceptibility to dystonias has been reported in newborn or premature infants, acutely ill or dehydrated children, and children with acute infections who have received phenothiazine medication. /Antihistamines, phenothiazine-derivative/

Histamine H1 Antagonists|A PHENOTHIAZINE ANTIHISTAMINIC EFFECTIVE FOR THE SYMPTOMATIC RELIEF OF URTICARIA. IT HAS ALSO BEEN USED FOR THE THERAPY OF MIGRAINE HEADACHE.|Antihistamines are indicated in the symptomatic treatment of perennial and seasonal allergic rhinitis, vasomotor rhinitis, and allergic conjunctivitis due to inhalant allergens and foods. /Antihistamines, phenothiazine-derivative; Included in US product labeling/|Antihistamines are indicated for the symptomatic treatment of pruritus associated with allergic reactions and of mild, uncomplicated allergic skin manifestations of urticaria and angioedema, in dermatographism, and in urticaria associated with transfusions. Methdilazine is also indicated in the treatment of pruritus associated with pityriasis rosea. /Antihistamines, phenothiazine-derivative; Included in US product labeling/|For more Therapeutic Uses (Complete) data for METHDILAZINE HYDROCHLORIDE (7 total), please visit the HSDB record page.

IT SHOULD NOT BE GIVEN CONCOMITANTLY WITH OTHER PHENOTHIAZINES, ANTIHISTAMINES, OR MAO INHIBITORS.|IT IS CONTRAINDICATED IN ASTHMA, NARROW-ANGLE GLAUCOMA, AND NEWBORN INFANTS; ALSO IN ACUTELY ILL OR DEHYDRATED CHILDREN, BECAUSE OF THE GREATER SUSCEPTIBILITY TO DYSTONIAS WITH PHENOTHIAZINES.|Phenothiazines have been reported to cause jaundice and extrapyramidal symptoms in infants whose mothers received these medications during pregnancy. /Antihistamines, phenothiazine-derivative/|Small amounts of antihistamines may be distributed into breast milk; use is not recommended in nursing mothers because of the risk of adverse effects, such as unusual excitement or irritability, in infants. Antihistamines may inhibit lactation because of their anticholinergic actions. /Antihistamines, phenothiazine-derivative/|For more Drug Warnings (Complete) data for METHDILAZINE HYDROCHLORIDE (18 total), please visit the HSDB record page.

Well absorbed after oral administration. /Antihistamines, phenothiazine-derivative/|The H1 antagonists are well absorbed from the GI tract. Following oral administration, peak plasma concn are achieved in 2 to 3 hr and effects usually last 4 to 6 hr; however, some of the drugs are much longer acting ... . /Histamine Antagonists: H1 Antagonists/|... H1 antagonists are eliminated more rapidly by children than by adults and more slowly in those with severe liver disease. /Histamine Antagonists: H1 Antagonists/

MAIN SITE OF METABOLIC TRANSFORMATION IS LIVER. /ANTIHISTAMINES/|H1 blockers are among the many drugs that induce hepatic microsomal enzymes, and they may facilitate their own metabolism. /Histamine Antagonists: H1 Antagonists/

Antihistamines used in the treatment of allergy act by competing with histamine for H1-receptor sites on effector cells. They thereby prevent, but do not reverse, responses mediated by histamine alone. Antihistamines antagonize, in varying degrees, most of the pharmacological effects of histamine, including urticaria and pruritus. In addition, the anticholinergic actions of most antihistamines provide a drying effect on the nasal and oral mucosa. /Antihistamines, phenothiazine-derivative/|H1 antagonists inhibit most responses of smooth muscle to histamine. Antagonism of the constrictor action of histamine on respiratory smooth muscle is easily shown in vivo and in vitro. /Histamine Antagonists: H1 Antagonists/|H1 antagonists strongly block the action of histamine that results in increased permeability and formation of edema and wheal. /Histamine Antagonists: H1 Antagonists/|Within the vascular tree, the H1 antagonists inhibit both the vasoconstrictor effects of histamine and, to a degree, the more rapid vasodilator effects that are mediated by H1 receptors on endothelial cells. Residual vasodilatation reflects the involvement of H2 receptors on smooth muscle and can be suppressed only by the concurrent administration of an H2 antagonist. Effects of the histamine antagonists on histamine-induced changes in systemic blood pressure parallel these vascular effects. /Histamine Antagonists: H1 Antagonists/|Many of the H1 antagonists tend to inhibit responses to acetylcholine that are mediated by muscarinic receptors. These atropine-like actions are sufficiently prominent in some of the drugs to be manifest during clinical usage ... . /Histamine Antagonists: H1 Antagonists/

SYMPTOMS: Symptoms of exposure to this compound may include drowsiness, dizziness, lassitude, tinnitus, incoordination, fatigue, blurred vision, euphoria, diplopia, nervousness, insomnia, tremors, grand mal seizures, catatonic-like states, neuritis and hysteria. It may cause bradycardia, cardiac arrest, anorexia, epigastric distress, constipation, dry mouth, urticaria, dermatitis, asthma, laryngeal edema, photosensitivity, lupus erythematous-like syndrome, anaphylactoid reactions, leukopenia, agranulocytosis, thrombocytopenic purpura and jaundice of the obstructive type. In children, symptoms may include excitation, hallucinations, convulsions and sudden death. In elderly people, it may cause hypotension, syncope, toxic confusional states, excessive sedation, extrapyramidal signs, akathisia and persistent dyskinesia. ACUTE/CHRONIC HAZARDS: When heated to decomposition this compound emits toxic fumes of nitrogen oxides and hydrochloric acid. (NTP, 1992)

EYES: First check the victim for contact lenses and remove if present. Flush victim's eyes with water or normal saline solution for 20 to 30 minutes while simultaneously calling a hospital or poison control center. Do not put any ointments, oils, or medication in the victim's eyes without specific instructions from a physician. If symptoms (such as redness or irritation) develop, immediately transport the victim to a hospital. SKIN: IMMEDIATELY flood affected skin with water while removing and isolating all contaminated clothing. Gently wash all affected skin areas thoroughly with soap and water. If symptoms such as redness or irritation develop, IMMEDIATELY call a physician and be prepared to transport the victim to a hospital for treatment. INHALATION: IMMEDIATELY leave the contaminated area; take deep breaths of fresh air. If symptoms (such as wheezing, coughing, shortness of breath, or burning in the mouth, throat, or chest) develop, call a physician and be prepared to transport the victim to a hospital. Provide proper respiratory protection to rescuers entering an unknown atmosphere. Whenever possible, Self-Contained Breathing Apparatus (SCBA) should be used; if not available, use a level of protection greater than or equal to that advised under Protective Clothing. INGESTION: DO NOT INDUCE VOMITING. If the victim is conscious and not convulsing, give 1 or 2 glasses of water to dilute the chemical and IMMEDIATELY call a hospital or poison control center. Be prepared to transport the victim to a hospital if advised by a physician. If the victim is convulsing or unconscious, do not give anything by mouth, ensure that the victim's airway is open and lay the victim on his/her side with the head lower than the body. DO NOT INDUCE VOMITING. IMMEDIATELY transport the victim to a hospital. (NTP, 1992)

THERE IS NO SPECIFIC THERAPY FOR ANTIHISTAMINE POISONING, AND TREATMENT IS ALONG GENERAL SYMPTOMATIC AND SUPPORTIVE LINES. ... SHOULD BREATHING FAIL, MECH SUPPORT OF VENTILATION OFFER SAFER AND ... EFFECTIVE MEANS OF MAINTAINING RESP THAN USE OF ANALEPTICS WHICH ARE PRONE TO INITIATE OR INTENSIFY CONVULSIVE PHASE. /ANTIHISTAMINES/

ADVERSE EFFECTS INCLUDE DROWSINESS, DIZZINESS, GASTROINTESTINAL DISTURBANCES, DRYNESS OF THE MUCOUS MEMBRANES, HEADACHE AND SKIN RASH. EXTRAPYRAMIDAL SYMPTOMS HAVE ALSO BEEN REPORTED. OTHER UNTOWARD REACTIONS MAY INCLUDE THOSE FOR PHENOTHIAZINES IN GENERAL.|In acute poisoning with H1 antagonists, their central excitatory effects constitute the greatest danger. The syndrome includes hallucinations, excitement, ataxia, incoordination, athetosis, and convulsions. Fixed, dilated pupils with a flushed face, together with sinus tachycardia, urinary retention, dry mouth, and fever, lend the syndrome a remarkable similarity to that of atropine poisoning. Terminally, there is deepening coma with cardiorespiratory collapse and death, usuallY within 2 to 18 hours. Treatment is along general symptomatic and supportive lines. /Histamine Antagonists: H1 Antagonists/|... SIDE EFFECTS INCL DRYNESS OF ... RESP PASSAGES, SOMETIMES INDUCING COUGH; URINARY FREQUENCY & DYSURIA; PALPITATION; HYPOTENSION; HEADACHE; TIGHTNESS OF CHEST; TINGLING, HEAVINESS, & WEAKNESS OF HANDS. ... ALLERGIC DERMATITIS IS NOT UNCOMMON. /ANTIHISTAMINES/|IN SMALL CHILD ... SYNDROME OF POISONING INCL ... ATAXIA, INCOORDINATION, ATHETOSIS ... FIXED, DILATED PUPILS WITH FLUSHED FACE ... ARE COMMON. /ANTIHISTAMINES/|ALTHOUGH H1-BLOCKING DRUGS HAVE RELATIVELY HIGH MARGIN OF SAFETY, ACUTE POISONING WITH THEM IS COMMON. ... IN CHILDREN, 20 TO 30 TABLETS OR CAPSULES OF MOST COMMERCIALLY AVAILABLE ANTIHISTAMINES REPRESENTS LETHAL OR NEAR-LETHAL DOSE. /ANTIHISTAMINES/

methdilazine

ND /METHDILAZINE/

Dibosyn, Disyncran, Tacaryl

OFFICIAL PHENOTHIAZINE ASSAY PROCEDURES WERE IMPROVED BY MODIFYING EXTRACTION PROCEDURES. A SPECIFIC OXIDATION PROCEDURE WITH UV OR FLUORESCENCE MEASUREMENT INCLUDED FILTRATION THROUGH A CELITE COLUMN AND OXIDATION WITH PERACETIC ACID. THE ABSORBANCE AND FLUORESCENCE INTENSITY OF THE PHENOTHIAZINE SULFOXIDES FORMED REACH A MAX IN APPROX 3 MIN AND THE RATIOS OF STANDARD AND SAMPLE ABSORBANCES ARE CONSTANT FOR ABOUT 3 HR.|A COLORIMETRIC METHOD FOR THE ANALYSIS OF METHDILAZINE HYDROCHLORIDE DOSAGE FORMS WAS BASED ON THE ACID DYE TECHNIQUE WHICH FORMS A STABLE CHLOROFORM YELLOW COMPLEX WITH BROMOTHYMOL BLUE AT PH 2.8 WHICH IS QUANTITIATED AT 415 NM.

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