Opthamet Ophthalmic Solution 0.05%+0.04%
Opthamet Ophthalmic Solution 0.05%+0.04% Uses, Dosage, Side Effects, Food Interaction and all others data.
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.
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.
Tetryzoline, also known as tetrahydrozoline, is a derivative of imidazoline with central and peripheral alpha (α)-adrenergic properties. Available since the 1950s, tetryzoline is a selective α1-receptor agonist that is used as an ocular and nasal decongestant. Tetryzoline is found in a wide array of over-the-counter eye drops, including the most common brand, Visine. Tetryzoline is also found in combination products with other lubricants and anti-irritants, such as povidone, polyethylene glycol 400, dextran, and zinc sulfate. It is also used in combination with other drug classes, such as antihistamines, corticosteroids, and glucocorticoids in other countries. Tetryzoline is also found in nasal spray under the trade name Tyzine, which is used for decongestion of nasal and nasopharyngeal mucosa.
As it causes profound sedation in children and adults, tetryzoline is increasingly becoming scrutinized for possible drug overdose and toxicity from accidental ingestion. It has also been misused for non-therapeutic purposes as a causative drug for several cases of drug-facilitated sexual assault.
Tetryzoline is a sympathomimetic amine and an alpha-adrenergic agonist with vasoconstricting and decongestant properties. It works by constricting the smaller arterioles of the nasal passages and conjunctival blood vessels to ameliorate allergic rhinitis, nasal congestion, and ocular irritation. Tetryzoline is known to cross the blood-brain barrier to work on alpha-2 adrenoceptors and imidazole receptors, causing effects like hypotension, bradycardia, analgesia, hypothermia, sedation, and hypnosis.
| Trade Name | Opthamet Ophthalmic Solution 0.05%+0.04% |
| Generic | Antazoline + Tetryzoline |
| Weight | 0.05%+0.04% |
| Type | Ophthalmic Solution |
| Therapeutic Class | Other ophthalmic preparations |
| Manufacturer | Drug International Ltd. |
| Available Country | Bangladesh |
| Last Updated: | October 19, 2023 at 6:27 am |
Uses
Temporary relief of the signs and symptoms of allergic conjunctivitis including conjunctival hyperaemia, chemosis and itching in adults and children above 2 years of age.Opthamet Ophthalmic Solution 0.05%+0.04% is also used to associated treatment for these conditions: Eye allergyActive, Symptomatic Blepharitis, Blepharitis allergic, Blepharoconjunctivitis, Chalazion, Conjunctivitis, Conjunctivitis allergic, Conjunctivitis, Vernal, Corneal Inflammation, Dacryocystitis, Dry Eyes, Episcleritis, Eye allergy, Eye redness, Eye swelling, Eyelid folliculitis, Keratoconjunctivitis, Nasal Congestion, Ocular Inflammation, Ocular Irritation, Pterygium, Red eye, Rhinopharyngitis, Scleritis, Sinusitis, Acute Rhinitis, Bacterial blepharitis, Conjunctival hyperemia, Eye discomfort, Nasal edema, Redness and itching of the eyes, Sensation of burning in the eyes, Subacute Rhinitis, Ocular vasoconstriction
How Opthamet Ophthalmic Solution 0.05%+0.04% works
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.
Adrenergic receptors are G-protein-coupled receptors (GPCR) that regulate vascular tone: stimulation of alpha-1 adrenergic receptors leads to vasoconstriction. Ocular redness and nasal congestion often result from vasodilation of nasal, conjunctival, and corneal capillary blood vessels. Activation of alpha-1 adrenergic receptors have been therefore associated with a reduction of symptoms of ocular irritation and nasal congestion. Tetryzoline is a selective agonist of alpha-1 adrenergic receptors, causing vasoconstriction and alleviating ocular and nasal symptoms.
Dosage
Opthamet Ophthalmic Solution 0.05%+0.04% dosage
Adults and adolescents: 1 drop 2 to 3 times daily upto 14 days. Children (Older than 2 years of age): No specific studies are available in this patient group. For possible systemic effects, the dosage should exceed to 1 to 2 drops per day. Children (Below 2 years of age): Not to be used in children below 2 years of age.The eye drop should not be used for longer periods than 14 days as this may cause rebound hyperemia and toxic follicular conjunctivitis.Side Effects
The most common adverse effect is burning/stinging upon installation, which is mild and transient in nature.Toxicity
The Lowest published toxic dose (TDLo) of tetryzoline in children following oral administration is 175 mg/kg. Oral LD50 is 785 mg/kg in rats and 345 mg/kg in mice. Intraperitoneal LD50 is 122 mg/kg in rats and 110 mg/kg in mice. Subcutaneous LD50 is 500 mg/kg in rats.
Overdose following accidental oral ingestion in children may lead to profound sedation, possibly accompanied by profuse sweating, hypotension, and shock. In adults, hypertension, bradycardia, drowsiness, and rebound hypotension may be observed, in addition to a shock-like syndrome with hypotension and bradycardia. In one case, cardiovascular effects persisted for 36 hours after unintentional ingestion of tetrahydrozoline. Profound sedation has occurred in adults following accidental oral ingestion due to poisoning.
Overdose should be managed with supportive treatment, with the patient kept warm. Fluid maintenance therapy may be initiated if necessary. The respiratory rate dropping to 10 or below should be responded with oxygen therapy and respiratory assistance. Blood pressure should be carefully monitored to prevent a hypotensive crisis. There is no known antidote to tetryzoline overdose; however, one case report illustrates the successful use of naloxone in reversing the clinical signs and symptoms of tetryzoline overdose in a child. Naloxone has been used to revere clonidine overdose. The exact mechanism of action of naloxone as an antidote is not fully understood; however, it is understood that clonidine and tetryzoline work to inhibit central sympathetic outflow by activating alpha-2 adrenoceptors and inducing endogenous opiate release, which naloxone works to antagonize.
Precaution
The eye drop should be used with caution in elderly patients with severe cardiovascular disease, including arrhythmia, poorly controlled hypertension or diabetes.Interaction
Sympathomimetic agents may cause a hypertensive crisis if used during treatment with MAOIs. Concomitant use with MAOIs is therefore contraindicated. Sedating anti-histamines can enhance the sedating effects of CNS depressant including alcohol, hypnotics, opioid analgesics, anxiolytic sedatives and anti-psycotics. They also have an additive anti-muscarinic action with other anti muscarinic drugs, such as atropine and antidepressantVolume of Distribution
No information is available.
Elimination Route
When consumed orally, tetryzoline is rapidly absorbed from the gastrointestinal tract and can cross the blood-brain barrier. Following ocular administration of 0.05% tetryzoline, Cmax ranged from 0.068 to 0.380 ng/mL.
Half Life
Following ocular administration of 0.05% tetryzoline, the mean serum half-life was approximately 6 hours.
Clearance
No information is available.
Elimination Route
Following ocular administration of 0.05% tetryzoline, tetryzoline was detected in urine at 24 hours.
Pregnancy & Breastfeeding use
No clinical data on exposed pregnancies are available. The eye drops should only be used if the potential benefits outweigh the risks to the fetus or infant. It is not known whether the either of the active substances of the eye drop passes into breast milk. Caution should be exercised when using the product during breast-feeding.Contraindication
Known hypersensitivity to Antazoline/ Tetryzoline or to any of the excipients. Concomitant use with Monoamine Oxidase Inhibitors (MAOI).Acute Overdose
A topical overdose of this ophthalmic solution may be flushed from the eye with warm tap water.Storage Condition
The drug is to be used within 30 days after first opening. Store at 15-25° C. Protect from light. The bottle is to be closed strongly immediately after use. keep out of reach of children.Innovators Monograph
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