Antazoline

265.35

265.35

202-094-0

DHA8014SS1

DTXSID3022613

C61638

White, crystalline powder

R - Respiratory system

27.6

3.38 (est)

Solid

1.1±0.1 g/cm3

120-122 °C

475.5±38.0 °C at 760 mmHg

241.4±26.8 °C

1.608

In water, 6.63X10+2 mg/L at 30 deg C

Keep in a cool, dry, dark location in a tightly sealed container or cylinder. Keep away from incompatible materials, ignition sources and untrained individuals. Secure and label area. Protect containers/cylinders from physical damage.

2.3X10-8 mm Hg at 25 deg C (est)

LD50 oral in mouse: 398mg/kg

Odorless

Bitter

Henry's Law constant = 6.0X10-11 atm-cu m/mol at 25 °C (est)

pKa = 4.90 (non-cyclic tertiary nitrogen); pKa = 10.68 (tertiary imidazoline nitrogen) (est)

Hydroxyl radical reaction rate constant = 2.4X10-10 cu cm/molecule-sec at 25 °C (est)

S22-S24/25

P261, P264, P270, P271, P280, P301+P312, P302+P352, P304+P340, P305+P351+P338, P312, P321, P322, P330, P332+P313, P337+P313, P362, P363, P403+P233, P405, 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.

The Approved Drug Products with Therapeutic Equivalence Evaluations List identifies currently marketed over-the-counter drug products, incl antazoline, approved on the basis of safety and effectiveness by FDA under sections 505 of the Federal Food, Drug, and Cosmetic Act.

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P261, P264, P270, P271, P280, P301+P312, P302+P352, P304+P340, P305+P351+P338, P312, P321, P322, P330, P332+P313, P337+P313, P362, P363, P403+P233, P405, and P501|Aggregated GHS information provided by 40 companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

The purpose of this study was to investigate the effects of antazoline and ketotifen (two H1 receptor antagonists) on the anticonvulsant activity of antiepileptic drugs against maximal electroshock (MES)-induced convulsions in mice. The following antiepileptic drugs were used: valproate, carbamazepine, diphenylhydantoin and phenobarbital. In addition, the effects of antiepileptic drugs alone or in combination with antazoline or ketotifen were studied on long-term memory (tested in the passive avoidance task) and motor performance (evaluated in the chimney test), acutely and after 7-day treatment with these H1 receptor antagonists. The influence of antazoline and ketotifen on the free plasma and brain levels of the antiepileptics was also evaluated. Antazoline (at 0.5 mg/kg), given acutely and after 7-day treatment, significantly diminished the electroconvulsive threshold. Similarly, ketotifen, after acute and chronic doses of 8 mg/kg markedly reduced the threshold for electroconvulsions. In both cases, antazoline and ketotifen were without effect upon this parameter at lower doses. Antazoline (0.25 mg/kg) significantly raised the ED50 value of carbamazepine against MES (both, acutely and after 7-day treatment). Furthermore antazoline (0.25 mg/kg) also reduced the anticonvulsant activity of diphenylhydantoin, but only after repeated administration, without modifying the brain and free plasma level of this drug. Moreover, valproate and phenobarbital did not change their protective activity when combined with antazoline. ... Only acute antazoline (0.25 mg/kg) applied with valproate impaired the performance of mice evaluated in the chimney test. Ketotifen (4 mg/kg) co-administered with conventional antiepileptic drugs impaired motor coordination in mice treated with valproate, phenobarbital or diphenylhydantoin. Acute and chronic antazoline (0.25 mg/kg) alone or in combination with antiepileptic drugs did not disturb long-term memory, tested in the passive avoidance task. ... The results of this study indicate that H1 receptor antagonists, crossing the blood brain barrier, should be used with caution in epileptic patients. This is because antazoline reduced the protective potential of diphenylhydantoin and carbamazepine.|Imidazoline drugs exert neuroprotective effects in cerebral ischaemia models. They also have effects against mouse cerebellar and striatal neuronal death induced by N-methyl-D-aspartate (NMDA) through the blockade of NMDA currents. Here, we investigated the effects of antazoline on NMDA toxicity and current in rat hippocampal neuronal cultures, and on an in vivo model of status epilepticus. In hippocampal cultures, antazoline (30 uM) decreased NMDA-mediated neurotoxicity and also blocked the NMDA current with voltage-dependent and fast-reversible action (inhibition by 85+ or - 3% at -60 mV). Status epilepticus was induced by injecting pilocarpine (200 nmol) directly into the right pyriform cortex of male adult rats. The rats then received immediately three consecutive i.p. injections at 30-min intervals of either PBS (control group) or antazoline at 10 mg/kg (low-dose group) or at 45 mg/kg (high-dose group). During the 6-hr recording, status epilepticus lasted more than 200 min in all groups. In the high-dose group only, seizures completely ceased 1 hr after the third injection of antazoline, then started again 1 hr later. Rats were killed 1 week later, and Cresyl Violet-stained sections of their brain were analysed for damage quantification. On the ipsilateral side to the pilocarpine injection, pyriform cortex and hippocampal CA1 and CA3 areas were significantly protected in both antazoline-treated groups, whilst prepyriform and entorhinal cortices were only in the high-dose group. On the contralateral side to the pilocarpine injection, only the hippocampal CA3 area was significantly protected in the low-dose group, but all investigated structures were in the high-dose group.In conclusion, antazoline is a potent neuroprotective drug in different models of neuronal primary culture, as previously shown in striatal and cerebellar granule neurons, and here in hippocampal neurons. Antazoline is also neuroprotective in vivo in the intra-pyriform pilocarpine-induced status epilepticus model.

LD50 Mouse 398 mg/kg|LD50 Mouse ip 100 mg/kg|LD50 Mouse sc 135 mg/kg

Paradoxic stimulation may occasionally occur, especially at high doses and in children or the elderly. The sedative effects may diminish after a few days of therapeutic use. /Antihistamines/|Antazoline was reported to be a hemolytic agent in subjects deficient in glucose-6-phosphate dehydrogenase but only in conjunction with other factors such as infection.

Used to relieve nasal congestion and in eye drops, usually in combination with naphazoline, to relieve the symptoms of allergic conjunctivitis.

Anti-Allergic Agents; Histamine H1 Antagonists|Antazoline ... is an antihistamine used orally and also in eyedrops ...|In two independent studies including 25 subjects each, naphazoline caused significant whitening (but did not prevent itching) in the histamine-induced red, itchy eye. Antazoline inhibited itching (but not redness) to a significant degree in the same model. The combination of naphazoline and antazoline produced significant whitening and inhibition of itching in all eyes challenged by histamine. The combination of the two drugs was more effective than either component alone in preventing redness. The antihistamine and combination of antihistamine/vasoconstrictor were equally effective in arresting itching.|Antazoline is an ethylenediamine derivative with the properties and uses of the antihistamines. It is one of the least active of the commonly used antihistamines and has a short duration of action. It has local anaesthetic and also some anticholinergic properties. It is claimed to be less irritating to the tissue than most other antihistamines.|For more Therapeutic Uses (Complete) data for ANTAZOLINE (9 total), please visit the HSDB record page.

Other common adverse reactions include dizziness, tinnitus, blurred vision, euphoria, incoordination, anxiety, insomnia, tremor, nausea, vomiting, constipation, diarrhea, epigastric discomfort, dry mouth, and cough. Infrequently, urinary retention, palpitation, hypotension, headache, hallucination, psychosis, ... may occur. Rarely, leukopenia, agranulocytosis, hemolytic anemia, allergic reactions, dysrhythmias, dyskinesia, seizures, paraesthesia, paralysis, hepatitis, ... are noted../Antihistamines/|In therapeutic use, the adverse effects are similar for most members of the group. The most common side effect of the sedating antihistamines is central nervous system depression. Effects range from slight drowsiness to deep sleep and include lassitude, dizziness, and incoordination. Paradoxic stimulation may occasionally occur, especially at high doses and in children or the elderly. The sedative effects may diminish after a few days of therapeutic use. /Antihistamines/

Antazoline is a histamine H1 receptor antagonist. It selectively bind to but does not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine.

Agents that are used to treat allergic reactions. Most of these drugs act by preventing the release of inflammatory mediators or inhibiting the actions of released mediators on their target cells. (From AMA Drug Evaluations Annual, 1994, p475) (See all compounds classified as Anti-Allergic Agents.)|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.)

Antazoline binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine.|Antihistamine drugs are competitive, reversible inhibitors of the action of histamine at the H1 receptor. /Antihistamines/

Most patients require only symptomatic and supportive care. Treatment is focused on controlling agitation, maintaining airway, reversing hyperthermia, and supporting hemodynamic function. Gastrointestinal decontamination is not essential, but if not more than 1 hours has elapsed since ingestion of the drug, activated charcoal may be considered. In view of the potential cardiac toxicity in addition to maintenance of the airway, breathing, and circulatory status of the patients, observation for dysrhythmia is warranted. Clinical assessment for signs that may indicated impending seizure activity (hypertonicity, hyperreflexia, or myoclonic jerking) is important. ... /Antihistamines/|Basic treatment: Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if needed. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary ... . Monitor for shock and treat if necessary ... . Anticipate seizures and treat if necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with 0.9% saline (NS) during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 ml/kg up to 200 ml of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool ... . Cover skin burns with dry sterile dressings after decontamination ... . /Poisons A and B/|Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in severe respiratory distress. Positive-pressure ventilation techniques with a bag valve mask device may be beneficial. Consider drug therapy for pulmonary edema ... . Consider administering a beta agonist such as albuterol for severe bronchospasm ... . Monitor cardiac rhythm and treat arrhythmias as necessary ... . Start IV administration of D5W /SRP: "To keep open", minimal flow rate/. Use 0.9% saline (NS) or lactated Ringer's if signs of hypovolemia are present. For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload ... . Treat seizures with diazepam or lorazepam ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Poisons A and B/

/SIGNS AND SYMPTOMS/ In human eyes 0.75% solution between pH 5 and pH 8 was about the maximum suitable for clinical use. Oral administration of 400 mg antazoline hydrochloride per day for five days to patients with normal eyes caused no change in intraocular pressure or tonographic measurements. /Antazoline hydrochloride/|/SIGNS AND SYMPTOMS/ Allergic thrombocytopenic purpura and agranulocytosis have been reported. Transient dizziness and anorexia have followed the intravenous administration of antazoline, and cardiac arrest has occurred.|/SIGNS AND SYMPTOMS/ A report of interstitial pneumonitis, with fever, rash, and dyspnea, after antazoline; the condition recurred after challenge.|/CASE REPORTS/ Antazoline (Antistina) induced thrombocytopenic purpura occurring on three occasions in a 21 year old woman is reported. After withdrawal of the drug therapy the patient recovered promptly. In vitro investigation demonstrated the presence of an antibody in serum, which in association with antazoline caused complement fixation when added to test platelets. Also platelet agglutinins could be detected in the patient's serum when antazoline was added. The reactions were drug specific and they could still be demonstrated 9 months after the last exposure to the drug.|For more Human Toxicity Excerpts (Complete) data for ANTAZOLINE (6 total), please visit the HSDB record page.

Analergine

Oral tablets; 100, 200 mg Arithmin, Lammett.|Antistin-Privine (Ciba, UK). An aqueous iso-osmotic solution containing antazoline 0.5% and naphazoline nitrate 0.025%. For allergic conditions of the nose. /Antazoline sulfate/|Trade names: Ocuclear Eye Drops (Schering), Visine L.R. Eye Drops (Pfizer).

Diode array detection of low level co-eluting species in high-performance liquid chromatography.|Determination of naphazoline nitrate and antazoline sulfate in pharmaceutical combinations by reversed-phase high performance liquid chromatography. /Antazoline sulfate/|Analyte: antazoline phosphate; matrix: chemical identification; procedure: infrared absorption spectrophotometry with comparison to standards /antazoline phosphate/|Analyte: antazoline phosphate; matrix: chemical identification; procedure: thin-layer chromatography with comparison to standards /antazoline phosphate/|For more Analytic Laboratory Methods (Complete) data for ANTAZOLINE (8 total), please visit the HSDB record page.

A computerized gas chromatography-mass spectrometric procedure for the toxicological detection of the ethylenediamine and piperazine antihistamines and their metabolites in urine. /Ethylenediamine & piperazine antihistamines/

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