Chemical formula: C₉H₁₀Cl₂N₄ Molecular mass: 245.109 g/mol PubChem compound: 2216
Apraclonidine interacts in the following cases:
Although no specific drug interactions with topical glaucoma drugs or systemic medicaments were identified in clinical studies of apraclonidine, the possibility of an additive or potentiating effect with CNS depressants (alcohol, barbiturates, opiates, sedatives, anaesthetics) should be considered. There is a theoretical possibility that use of apraclonidine in conjunction with topical sympathomimetics may give rise to a systemic pressor response and blood pressure should be checked initially in patients receiving these drug combinations.
Since apraclonidine may reduce pulse and blood pressure, caution in using drugs such as beta-blockers (ophthalmic and systemic), antihypertensives, and cardiac glycosides is advised. Patients using cardiovascular drugs concurrently with apraclonidine should have pulse and blood pressure frequently monitored. Caution should be exercised with simultaneous use of clonidine and other similar pharmacologic agents.
An additive hypotensive effect has been reported with the combination of systemic clonidine and neuroleptic therapy. Systemic clonidine may inhibit the production of catecholamine in response to insulin-induced hypoglycaemia and mask the signs and symptoms of hypoglycaemia.
Caution in and monitoring of depressed patients are advised since apraclonidine has been rarely associated with depression.
Apraclonidine should be used with caution in patients with a history of angina, severe coronary insufficiency, recent myocardial infarction, overt cardiac failure, hypertension, cardiovascular disease, including apoplexy, cerebrovascular disease, Parkinson’s syndrome, chronic renal failure, Raynaud’s disease or thromboangiitis obliterans.
There are no or limited studies of apraclonidine in pregnant women. Apraclonidine is not recommended during pregnancy.
Animal studies have been conducted which have demonstrated an absence of teratogenic effects in rats and rabbits. Embryotoxicity has been observed when pregnant rabbits were dosed orally with doses of apraclonidine (doses >1.25 mg/kg/day) that were maternally toxic, and administered over the entire period of organogenesis at exposure levels of (mg/kg/day) of >60 times the recommended dosage regimen for apraclonidine eye drops based on a 50kg person.
It is not known if topically applied apraclonidine is excreted in human milk. A risk to newborns/infants cannot be excluded. Breast-feeding should be discontinued during treatment with apraclonidine.
Studies have not been performed to evaluate the effect of topical ocular administration of apraclonidine on male or female fertility. No effect on fertility was observed in rats after oral administration of apraclonidine.
Apraclonidine has a moderate influence on the ability to drive and use machines.
Since clonidine-like drugs may cause dizziness or somnolence, patients so affected are advised not to drive or operate machinery. The attention of drivers and machinery operators should be drawn to the risks related to the use of this drug.
In clinical trials using apraclonidine the most common adverse reactions were ocular hyperaemia, eye pruritus, and conjunctivitis, occurring in approximately 12% to 23% of patients.
The following adverse reactions are classified according to the following convention: very common (≥1/10), common (≥1/100 to <1/10), uncommon (≥1/1,000 to <1/100), rare (≥1/10,000 to <1/1,000), very rare (<1/10,000), or not known (cannot be estimated from the available data). Within each frequency-grouping, adverse reactions are presented in order of decreasing seriousness.
Common: rhinitis
Not known: hypersensitivity
Uncommon: depression, nervousness, insomnia
Common: headache, dysgeusia
Uncommon: dizziness, abnormal coordination, somnolence, paraesthesia
Very common: conjunctivitis, eye pruritus, ocular hyperaemia
Common: eyelid oedema, dry eye, conjunctival follicles, foreign body sensation in eyes, eyelid margin crusting, lacrimation increased, ocular discomfort
Uncommon: mydriasis, keratitis, keratopathy, visual acuity reduced, visual impairment, photophobia, vision blurred, corneal erosion, corneal infiltrates, blepharospasm, blepharitis, eyelid ptosis, erythema of eyelid, eye pain, eye oedema, eyelid disorder, eyelid scales, eye lid retraction, conjunctival vascular disorders, conjunctival oedema, eye discharge, eye irritation
Uncommon: chest pain, oedema peripheral, arrhythmia
Uncommon: vasodilation
Common: nasal dryness
Uncommon: asthma, dyspnoea, rhinorrhoea, parosmia, throat irritation
Common: dry mouth
Uncommon: nausea, constipation
Common: dermatitis
Uncommon: dermatitis contact, face oedema
Uncommon: myalgia
Common: asthenia
Uncommon: malaise, fatigue, irritability
Uncommon: corneal staining
Use of apraclonidine can lead to an ocular intolerance reaction. The mean onset time of these reactions was 44 days (range 1-127 days).
In clinical studies, the overall discontinuation rate related to apraclonidine was 15%. The most commonly reported events leading to discontinuation included (in decreasing order of frequency) ocular hyperaemia, eye pruritus, lacrimation increased, ocular discomfort, eyelid oedema, dry mouth, and abnormal sensation in eye.
The possibility of bradycardia based on apraclonidine’s alpha-2-adrenergic agosnist effect should be considered. Although there were no reports of bradycardia related to apraclonidine Eye Drops from clinical studies, occasional reports have been received through postmarketing surveillance.
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