(+)-Chlorpheniramine

274.79

274.79

247-073-7

3Q9Q0B929N

DTXSID50180225

C61707

OILY LIQUID

R - Respiratory system

16.1

3.81860

1.107g/cm3

CRYSTALS FROM ETHYL ACETATE; MP: 113-115 °C; SPECIFIC OPTICAL ROTATION (DIMETHYLFORMAMIDE): +44.3 DEG @ 25 °C/D, PH OF 1% SOLN 4-5 /D-FORM, MALEATE/

142 °C @ Press: 1.0 Torr

183ºC

1.565

WHITE CRYSTALLINE POWDER; ODORLESS; 1 G SOL IN 4 ML WATER; SOL IN ALC, CHLOROFORM; SLIGHTLY SOL IN BENZENE, ETHER /MALEATE/

D25 +49.8° (c = 1 in DMF)

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).

Despite widespread use, the first generation antihistamines such as brompheniramine and chlorpheniramine have rarely been linked to liver test abnormalities or to clinically apparent liver injury. A single case report of clinically apparent liver injury with jaundice attributed to dexchlorpheniramine was reported from France. The time to onset was 10 days, and the clinical presentation resembled acute viral hepatitis, with marked elevations in serum aminotransferase levels and jaundice. Recovery was rapid and complete, but jaundice and hepatitis recurred within 10 days of restarting. Immunoallergic features (rash, fever, eosinophilia) were absent as were autoantibodies. Interestingly, the patient tolerated other antihistamines (cetirizine) without difficulty.

Concurrent use /of ototoxic medications/ with antihistamines may mask the symptoms of ototoxicity such as tinnitus, dizziness, or vertigo. /Antihistamines/|Concurrent use of monoamine oxidase (MAO) inhibitors with antihistamines may prolong and intensify the anticholinergic and CNS depressant effects of antihistamines; concurrent use is not recommended. /Antihistamines/|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/|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/|Concurrent use /of other photosensitizing medications/ with antihistamines may cause additive photosensitizing effects. /Antihistamines/

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. A paradoxical reaction characterized by hyperexcitability may occur in children taking antihistamines. /Antihistamines/|Dizziness, sedation, confusion, and hypotension may be more likely to occur in geriatric patients taking antihistamines. Geriatric patients are especially susceptible to the anticholinergic side effects, such as dryness of mouth and urinary retention (especially in males), of the antihistamines. If these side effects occur and continue or are severe, medication should probably be discontinued. /Antihistamines/

Brompheniramine and chlorpheniramine maleate are first generation antihistamines that are widely used to treat symptoms of allergic rhinitis and the common cold. Clinically apparent liver injury from brompheniramine or chlorpheniramine must be exceeding rare, if it occurs at all.

Antihistamines

Histamine H1 Antagonists|Antihistamines are indicated in the prophylactic and symptomatic treatment of perennial and seasonal allergic rhinitis, vasomotor rhinitis, and allergic conjunctivitis due to inhalant allergens and foods. /Antihistamines; 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. /Antihistamines; Included in US product labeling/|Antihistamines are also used in the treatment of pruritus associated with pityriasis rosea. /Antihistamines; NOT included in US product labeling/|For more Therapeutic Uses (Complete) data for DEXCHLORPHENIRAMINE (12 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. A paradoxical reaction characterized by hyperexcitability may occur in children taking antihistamines. /Antihistamines/|Dizziness, sedation, confusion, and hypotension may be more likely to occur in geriatric patients taking antihistamines. Geriatric patients are especially susceptible to the anticholinergic side effects, such as dryness of mouth and urinary retention (especially in males), of the antihistamines. If these side effects occur and continue or are severe, medication should probably be discontinued. /Antihistamines/|Prolonged use of antihistamines ... may decrease or inhibit salivary flow, thus contributing to the development of caries, periodontal disease, oral candidiasis, and discomfort. /Antihistamines/|VET: ANTIHISTAMINE DRUGS MAY BE OF SOME USE IN MINIMIZING SERUM REACTIONS BUT ARE OF NO THERAPEUTIC VALUE...& MAY EVEN POTENTIATE TOXIC ACTION OF VENOM... /ANTIHISTAMINES/|For more Drug Warnings (Complete) data for DEXCHLORPHENIRAMINE (13 total), please visit the HSDB record page.

5. 5= EXTREMELY TOXIC: PROBABLE ORAL LETHAL DOSE (HUMAN) 5-50 MG/KG, BETWEEN 7 DROPS & 1 TEASPOONFUL FOR 70 KG PERSON (150 LB). /ANTIHISTAMINICS/

Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood. (See all compounds classified as Histamine H1 Antagonists.)

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/

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. Also, the anticholinergic actions of most antihistamines provide a drying effect on the nasal mucosa. /Antihistamines/|DEXCHLORPHENIRAMINE MALEATE ANTAGONIZES MANY OF CHARACTERISTIC EFFECTS OF HISTAMINE.|WHEN TESTED IN DOGS, ANTIHISTAMINIC POTENCY OF DEXTRO ISOMER WAS 100 TIMES GREATER THAN THAT OF LEVO ISOMER, & 2.5 TIMES GREATER THAN RACEMIC FORM. ON CIRCUS-MOVEMENT ATRIAL FLUTTER, LEVO FORM WAS 1.4 & 2.3 TIMES THAT OF RACEMIC & DEXTRO CMPD.|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/|For more Mechanism of Action (Complete) data for DEXCHLORPHENIRAMINE (7 total), please visit the HSDB record page.

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/

SYMPTOMATOLOGY: 1. CENTRAL NERVOUS DEPRESSION IS USUALLY DOMINANT REACTION IN ADULTS; IT IS EVIDENCED BY DROWSINESS, LETHARGY, FATIGUE, HYPNOSIS, & COMA. RELATED NERVOUS SYMPTOMS INCL VERTIGO, ATAXIA, TINNITUS, & BLURRED VISION. /ANTIHISTAMINICS/|SYMPTOMATOLOGY: 2. CENTRAL NERVOUS HYPEREXCITABILITY OFTEN FOLLOWS INITIAL SEDATION; IN CHILDREN EXCITEMENT IS OFTEN FIRST EVIDENCE OF POISONING. STIMULANT PHASE BRINGS TREMORS, ANXIETY, INSOMNIA, EXCITEMENT, HALLUCINATIONS, DELIRIUM, TOXIC PSYCHOSIS & CONVULSIONS... /ANTIHISTAMINES/|SYMPTOMATOLOGY: 3. DANGEROUS HYPERPYREXIA MAY OCCUR IN POISONED CHILDREN... 4. GASTROINTESTINAL REACTIONS INCL DRY MOUTH, ANOREXIA, NAUSEA, VOMITING, ABDOMINAL DISTRESS, CONSTIPATION, &/OR DIARRHEA. /ANTIHISTAMINICS/|SYMPTOMATOLOGY: 5. TERMINAL PHASE IS ONE OF SEVERE CENTRAL NERVOUS DEPRESSION, WITH DEATH FROM RESP ARREST OR CARDIOVASCULAR COLLAPSE. /ANTIHISTAMINICS/|For more Human Toxicity Excerpts (Complete) data for DEXCHLORPHENIRAMINE (9 total), please visit the HSDB record page.

dexchlorpheniramine

ESSENTIALLY 100% AS AN ANTIHISTAMINE (MALEATE, 1976)

SYRUP NF: 2 MG/5 ML; TABLETS NF: 2 MG|Chlo-amine, Fortamine, Isomerine, Phenamin, Phendextro, Polaramine, Polaronil, Sensidyn /d-Form maleate/

AOAC Method 981.24, Chlorpheniramine maleate in drug tablets, autoanalyzer with spectrophometry, detection limit not reported. /Maleate/|AOAC Method 981.26, Pseudoephedrine HCl and Triprolidine HCl or Chlorpheniramine maleate in drug combinations, reverse-phase liquid chromatography using ion pairing, detection limit not reported. /Maleate/|AOAC Method 958.10, Antihistamines in drugs in presence of aspirin, phenacetin and caffein, spectrophotometry, detection limit not reported. /Maleate/

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