Antazoline is an antihistamine agent used for the symptomatic treatment of nasal congestion and allergic conjunctivitis.
- Generic Name
- DrugBank Accession Number
Antazoline is a 1st generation antihistamine with anticholinergic activity. It is used to relieve nasal congestion. It is also formulated as eye drops with naphazoline to relieve allergic conjunctivitis.
- Small Molecule
- Average: 265.3529
- Chemical Formula
Used to relieve nasal congestion and in eye drops, usually in combination with naphazoline, to relieve the symptoms of allergic conjunctivitis.Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.
- Associated Conditions
- Contraindications & Blackbox Warnings
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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.
- Mechanism of action
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.
Target Actions Organism AHistamine H1 receptorantagonist Humans
- Volume of distribution
- Protein binding
- Not Available
- Route of elimination
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.
Pathway Category Antazoline H1-Antihistamine Action Drug action
- Pharmacogenomic Effects/ADRs
- Not Available
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Acrivastine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Antazoline. Adenosine The risk or severity of QTc prolongation can be increased when Adenosine is combined with Antazoline. Ajmaline The risk or severity of QTc prolongation can be increased when Ajmaline is combined with Antazoline. Alfuzosin The risk or severity of QTc prolongation can be increased when Alfuzosin is combined with Antazoline. Alimemazine The risk or severity of QTc prolongation can be increased when Alimemazine is combined with Antazoline. Amantadine The risk or severity of QTc prolongation can be increased when Amantadine is combined with Antazoline. Amifampridine The risk or severity of QTc prolongation can be increased when Antazoline is combined with Amifampridine. Amiodarone The risk or severity of QTc prolongation can be increased when Antazoline is combined with Amiodarone. Amisulpride The risk or severity of QTc prolongation can be increased when Antazoline is combined with Amisulpride. Amitriptyline The risk or severity of QTc prolongation can be increased when Amitriptyline is combined with Antazoline.Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more
- Food Interactions
- No interactions found.
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Product Ingredients
Ingredient UNII CAS InChI Key Antazoline hydrochloride FP8Q8F72JH 2508-72-7 SWKDMSRRIBZZAY-UHFFFAOYSA-N Antazoline phosphate VPR5FPH326 154-68-7 DUIGUKRYYAGJAF-UHFFFAOYSA-N Antazoline sulfate 6T74I07212 24359-81-7 UWOSJBSLQYMGDL-UHFFFAOYSA-N
- International/Other Brands
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Albalon A Antazoline phosphate (.5 %) + Naphazoline hydrochloride (.05 %) Liquid Ophthalmic Allergan 1978-12-31 2017-07-26 ALOSYN EYE DROPS Antazoline hydrochloride (0.50 MG/ML) + Tetrahydrozoline hydrochloride (0.40 MG/ML) Solution Ophthalmic PETER CHIA MARKETING PTE LTD 2008-01-24 Not applicable Cooper A.R. Antazoline phosphate (5 mg / mL) + Naphazoline hydrochloride (.5 mg / mL) Solution / drops Ophthalmic Coopervision, Inc. 1996-08-14 1998-03-12 Ophtrivin A Ophthalmic Dps Antazoline sulfate (.5 %) + Xylometazoline hydrochloride (.05 %) Solution / drops Ophthalmic Ciba Vision 1992-12-31 2000-11-08 Refresh Eye Allergy Relief Antazoline phosphate (0.51 %) + Naphazoline hydrochloride (0.051 %) Solution Ophthalmic Allergan 2009-02-09 Not applicable Steritears Ar Antazoline phosphate (0.5 %) + Naphazoline hydrochloride (0.05 %) Solution / drops Ophthalmic Laboratoires Sterigen Inc Not applicable Not applicable SULFARHIN BURUN POMADI, 12 G Antazoline (30 mg) + Eucalyptol (100 mg) + Levomenthol (100 mg) + Naphazoline hydrochloride (3 mg) Nasal SANTA FARMA İLAÇ SAN. A.Ş. 2020-08-14 Not applicable SULFARHIN BURUN POMADI, 20 G Antazoline (30 mg) + Eucalyptol (100 mg) + Levomenthol (100 mg) + Naphazoline hydrochloride (3 mg) Nasal SANTA FARMA İLAÇ SAN. A.Ş. 2020-08-14 Not applicable Vasocon A Eye Drops Antazoline phosphate (5 mg / mL) + Naphazoline hydrochloride (.5 mg / mL) Solution / drops Ophthalmic Novartis Ophthalmics Novartis Pharmaceuticals (Canada) Inc 1996-12-31 2005-03-01 Vasocon A Oph Soln Antazoline phosphate (5 mg / mL) + Naphazoline hydrochloride (.5 mg / mL) Solution / drops Ophthalmic Iolab Pharmaceuticals 1988-12-31 1996-09-09
- ATC Codes
- R06AX05 — Antazoline
- R06AX — Other antihistamines for systemic use
- R06A — ANTIHISTAMINES FOR SYSTEMIC USE
- R06 — ANTIHISTAMINES FOR SYSTEMIC USE
- R — RESPIRATORY SYSTEM
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- This compound belongs to the class of organic compounds known as phenylbenzamines. These are aromatic compounds consisting of a benzyl group that is N-linked to a benzamine.
- Organic compounds
- Super Class
- Benzene and substituted derivatives
- Sub Class
- Direct Parent
- Alternative Parents
- Dialkylarylamines / Benzylamines / Aniline and substituted anilines / Aralkylamines / Imidolactams / Imidazolines / Propargyl-type 1,3-dipolar organic compounds / Carboximidamides / Carboxamidines / Azacyclic compounds / Organopnictogen compounds / Hydrocarbon derivatives show 2 more
- 2-imidazoline / Amidine / Amine / Aniline or substituted anilines / Aralkylamine / Aromatic heteromonocyclic compound / Azacycle / Benzylamine / Carboximidamide / Carboxylic acid amidine / Dialkylarylamine / Hydrocarbon derivative / Imidolactam / Organic 1,3-dipolar compound / Organic nitrogen compound / Organoheterocyclic compound / Organonitrogen compound / Organopnictogen compound / Phenylbenzamine / Propargyl-type 1,3-dipolar organic compound / Tertiary aliphatic/aromatic amine / Tertiary amine show 12 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- tertiary amino compound, aromatic amine, imidazolines (CHEBI:84115)
- Affected organisms
- Humans and other mammals
- CAS number
- InChI Key
- IUPAC Name
- Synthesis Reference
Miescher, K. and Klarer, W.; US. Patent 2,449,241; September 14,1948: assigned to Ciba Pharmaceutical Products, Inc.
- General References
- Figus M, Fogagnolo P, Lazzeri S, Capizzi F, Romagnoli M, Canovetti A, Iester M, Ferreras A, Rossetti L, Nardi M: Treatment of allergic conjunctivitis: results of a 1-month, single-masked randomized study. Eur J Ophthalmol. 2010 Sep-Oct;20(5):811-8. [Article]
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- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Treatment Paroxysmal Atrial Fibrillation (PAF) 1
- Not Available
- Not Available
- Dosage Forms
Form Route Strength Solution Ophthalmic 0.50 MG/ML Solution / drops Conjunctival Solution / drops Ophthalmic Solution Ophthalmic Solution / drops Intraocular Liquid Ophthalmic
- Not Available
- Not Available
- Experimental Properties
Property Value Source melting point (°C) 227-229 Miescher, K. and Klarer, W.; US. Patent 2,449,241; September 14,1948: assigned to Ciba Pharmaceutical Products, Inc. water solubility 663 mg/L (at 30 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992)
- Predicted Properties
Property Value Source Water Solubility 0.114 mg/mL ALOGPS logP 3.22 ALOGPS logP 2.88 Chemaxon logS -3.4 ALOGPS pKa (Strongest Basic) 9.24 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 27.63 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 82.89 m3·mol-1 Chemaxon Polarizability 30.11 Å3 Chemaxon Number of Rings 3 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon
- Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9699 Blood Brain Barrier + 0.9578 Caco-2 permeable - 0.5076 P-glycoprotein substrate Substrate 0.7167 P-glycoprotein inhibitor I Non-inhibitor 0.8782 P-glycoprotein inhibitor II Inhibitor 0.59 Renal organic cation transporter Inhibitor 0.8403 CYP450 2C9 substrate Non-substrate 0.798 CYP450 2D6 substrate Substrate 0.6581 CYP450 3A4 substrate Non-substrate 0.6963 CYP450 1A2 substrate Non-inhibitor 0.9045 CYP450 2C9 inhibitor Non-inhibitor 0.919 CYP450 2D6 inhibitor Inhibitor 0.8932 CYP450 2C19 inhibitor Non-inhibitor 0.9644 CYP450 3A4 inhibitor Non-inhibitor 0.952 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8681 Ames test Non AMES toxic 0.788 Carcinogenicity Non-carcinogens 0.896 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 2.4576 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.5401 hERG inhibition (predictor II) Inhibitor 0.5709
- Mass Spec (NIST)
- Not Available
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available GC-MS Spectrum - EI-B GC-MS splash10-001i-9000000000-1eb3fa441bd25a0e41a3 Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
- Pharmacological action
- General Function
- Histamine receptor activity
- Specific Function
- In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
- Gene Name
- Uniprot ID
- Uniprot Name
- Histamine H1 receptor
- Molecular Weight
- 55783.61 Da
- Swiader MJ, Luszczki JJ, Wielosz M, Czuczwar SJ: Effect of histamine receptor antagonists on aminophylline-induced seizures and lethality in mice. Pharmacol Rep. 2005 Jul-Aug;57(4):531-5. [Article]
Drug created at October 14, 2010 20:06 / Updated at January 02, 2022 11:57