Apraclonidine
Anton C. de Groot in Monographs in Contact Allergy, 2021
Apraclonidine is a clonidine derivative with selective α2-adrenergic agonistic activity. Upon ocular administration, apraclonidine enhances aqueous humor uveoscleral outflow and decreases aqueous production by vasoconstriction, thereby decreasing intraocular pressure (IOP). Apraclonidine is used for prevention or reduction of intraoperative and postoperative increases in intraocular pressure before and after ocular laser surgery. It has also application as a short-term adjunctive therapy in patients with open-angle glaucoma who are on maximally tolerated medical therapy requiring additional IOP reduction. In pharmaceutical products, apraclonidine is employed as apraclonidine hydrochloride (CAS number 73218-79-8, EC number not available, molecular formula C9H11Cl3N4) (1).
Medical Therapy for Glaucoma
Neil T. Choplin, Carlo E. Traverso in Atlas of Glaucoma, 2014
Both apraclonidine and brimonidine have been approved by the USFDA for three times daily administration. These agents are commonly prescribed twice daily due to the poor compliance with t.i.d. dosing. IOP should be evaluated in the afternoon to determine whether t.i.d. dosing would be beneficial in an individual patient. Side effects include dry mouth, fatigue, drowsiness, systemic hypotension, and ocular allergy, which occur in about 12% of patients receiving brimonidine and up to 35% of patients receiving apraclonidine (Figure 14.10). An allergic response to apraclonidine does not preclude the use of brimonidine. Between 10% and 20% of patients with a documented ocular allergic response to apraclonidine developed an allergy to brimonidine. Brimonidine was formulated in concentrations of 0.15% and 0.1% to reduce the rate of allergy.
Medicolegal considerations of cosmetic treatment with botulinum toxin injections
Anthony V. Benedetto in Botulinum Toxins in Clinical Aesthetic Practice, 2017
Since brow depressors are generally weakened when treating glabellar lines, ptosis of the upper eyelid can occasionally result following improper injection technique in this region. This may occur as late as 2 weeks after injection. Ptosis is caused by migration of toxin through the orbital septum weakening the levator palpebrae superioris. It has been suggested that patients remain in an upright position for 3–4 hours following injection to lessen the risk of eyelid ptosis. There is, however, no scientific data to support this notion and this author no longer provides such advice to his patients.9 Active contraction of the muscles under treatment may increase the uptake of toxin and decrease its diffusion. Ptosis can be treated with apraclonidine 0.5% eye drops. Apraclonidine is an alpha2-adrenergic agonist, which causes Müller's muscle to contract. It should be noted that apraclonidine is contraindicated in patients with documented hypersensitivity. Phenylephrine 2.5% can be used when apraclonidine is not available. Phenylephrine is contraindicated in patients with narrow-angle glaucoma and in patients with aneurysms.
Ocular Surface Disease and Anti-Glaucoma Medications: Various features, Diagnosis, and Management Guidelines
Published in Seminars in Ophthalmology, 2023
Sowmya Andole, Sirisha Senthil
Topical beta-blockers can cause medication-induced adverse effects on the eyelids and conjunctiva. Apraclonidine can cause contact dermatitis of the periocular area and eyelids.7 Contact dermatitis occurs due to a portion of the drug binds to the dermal protein to form a complex hapten, which sensitizes the individual. When the drug is re-instilled it induces a delayed hypersensitivity reaction, which is the cause for allergy. Apraclonidine can also cause ectropion of the eyelid which progressed to cicatricial ectropion in some patients.20,21 In individuals with preexisting lid laxity, tissue edema due to allergy can worsen the preexisting problem resulting in ectropion. Chronic allergy with skin excoriation can also cause fibrotic changes and tissue shortening that can lead to ectropion.
Selective Laser Trabeculoplasty for Steroid-Induced Ocular Hypertension following Endothelial Keratoplasty
Published in Current Eye Research, 2022
Max Davidson, Eran Berkowitz, Harry Roberts, Ahmed Wanas, James Myerscough
Pilocarpine 2% and apraclonidine 1% were instilled into the treated eye 15–30 minutes before the procedure. A frequency doubled, Q-switched Nd:YAG laser was used, emitting a wavelength of 532 nm, coupled to a slit lamp delivery system (SeLecTor Deux, Lightmed corporation, CA, USA). It operates with a single pulse of 3 ns duration and a spot size of 400 µm. The initial laser energy was set at 0.5 mJ and a single laser pulse was delivered at the 12 o’clock position. If no bubble was observed, the energy was increased by 0.1 mJ increments until bubble formation. This energy level is considered the threshold energy. Recommended energy settings for conventional treatment are levels 0.1 mJ less than the threshold energy. A cut-off energy was set at 1.2 mJ even when no obvious reaction was observed. SLT was delivered to 360° of the trabecular meshwork. 100 non-overlapping shots (25 per quadrant) were used, using a gonioscopy lens.
Systemic side effects of glaucoma medications
Published in Clinical and Experimental Optometry, 2022
Amirmohsen Arbabi, Xuan Bao, Wesam Shamseldin Shalaby, Reza Razeghinejad
Apraclonidine stimulates alpha-1 and alpha-2 adrenoreceptors. Apraclonidine is a para-amino derivative of clonidine (a blood pressure-lowering medication), and contrary to brimonidine, it does not pass easily through the blood-brain barrier.38 The chances for having the systemic side effects of dry mouth, fatigue, dizziness, and drowsiness are lower than that of brimonidine.6 Apraclonidine use is limited to preventing temporarily intraocular pressure spikes after anterior segment laser procedures because of the high risk of tachyphylaxis (loss of intraocular pressure-lowering effect following repeated exposure to the drug) and allergic conjunctivitis.39,40
Related Knowledge Centers
- Sympathomimetic Drug
- Glaucoma
- Alpha-2 Adrenergic Receptor
- Agonist
- Intraocular Pressure
- Eye Surgery
- Horner'S Syndrome
- Anisocoria
- Clonidine
- Brimonidine