Apraclonidine

Registered South African indications:

• Control or prevention of postsurgical elevations in intraocular pressure (1%)
• Lowering intraocular pressure (adjunctive use) (0.5%)
• Glaucoma (short-term adjunctive therapy) (0.5%)

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Hypersensitivity to systemic clonidine
• Children
• History of severe or unstable and uncontrolled cardiovascular disease including severe uncontrolled arterial hypertension
• Coadministration with monoamine oxidase inhibitors  
• Coadministration with systemic sympathomimetics
• Coadministration with tricyclic antidepressants

Cautions 

• Pregnancy
• Breastfeeding
• Renal impairment (including chronic renal failure)
• Hepatic impairment
• History of vasovagal attacks
• History of angina
• Severe coronary insufficiency
• Recent myocardial infarction
• Overt cardiac failure
• Hypertension
• Cardiovascular disease
• Apoplexy
• Cerebrovascular disease
• Parkinson's syndrome
• Raynaud's disease
• Thromboangiitis obliterans
• Depression
• End stage glaucoma
• Treatment >1 month
• Concomitant use of contact lenses
• May impair ability to drive and operate machinery

Forms avail. in SA and covered in this monograph: opd

Control or prevention of postsurgical elevations in intraocular pressure that occur in patients after anterior segment laser surgery

10mg/1ml (1%)

• Ophthalmic (opd): 1 drop into affected eye(s), 1hr prior to surgery; Repeated immediately upon completion of surgery

Nasolacrimal occlusion or gently closing the eyelid after instillation is recommended to reduce the systemic absorption and side effects

If for any reason, the drop of apraclonidine 1% does not remain in the eye, repeat the dose by placing another drop in the eye

Short-term adjunctive therapy of chronic glaucoma in patients on maximally tolerated medical therapy who require additional intraocular pressure reduction to delay laser treatment or glaucoma surgery
Adjunctive use in lowering intraocular pressure

5mg/1ml (0.5%)

• Ophthalmic (opd): 1 drop into affected eye(s), 8hrly; Max duration: 1 month

A 5 min interval between instillation of each medication should be observed to prevent washout of the previous dose. Eye ointments should be applied last

If for any reason, the drop of apraclonidine 0.5% does not remain in the eye, repeat the dose by placing another drop in the eye

See additional prescribing points

Contraindicated

Pregnancy 

• Caution
• 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 >1.25mg/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. The potential risk for humans is unknown

Breastfeeding 

• Caution; not recommended
• It is not known if topically applied apraclonidine is excreted in human milk. A risk to the newborns/infants cannot be excluded
• Breastfeeding should be discontinued during treatment with apraclonidine

Fertility

• 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

Renal Impairment

• Caution; no information available
  Use with caution in chronic renal failure and monitor cardiovascular parameters closely

Hepatic Impairment 

• Caution; no information available
  Monitor cardiovascular parameters closely

Elderly 

• No dose adjustment recommended

Porphyria Information

• Not porphyrinogenic (NP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Insomnia
• Abnormal dreams
• Vasovagal syncope
• Paraesthesia
• Decreased libido
• Irritability
• Postural dizziness
• Hypoaesthesia
• Headache
• Fatigue
• Depression
• Nervousness
• Abnormal coordination
• Somnolence
• Asthenia
• Hot and cold flushes

Cardiovascular Disorders

• Bradycardia
• Palpitations
• Orthostatic hypotension
• Hypotension
• Hypertension
• Chest pain
• Irregular heart rate
• Peripheral oedema
• Arrhythmia
• Vasodilation

Respiratory Disorders

• Dyspnoea
• Increased upper airway secretion
• Nasal discomfort
• Nasal dryness
• Rhinitis
• Asthma
• Rhinorrhoea
• Parosmia
• Throat irritation

Gastrointestinal Disorders

• Diarrhoea
• Nausea and vomiting
• Abdominal pain
• Stomach discomfort
• Dry mouth
• Constipation

Skin and Subcutaneous Tissue Disorders

• Hyperhidrosis
• Pruritus
• Contact dermatitis
• Face oedema

Musculoskeletal Disorders

• Pain in extremities
• Myalgia

Immune, Blood and Lymphatic Disorders

• Hypersensitivity

Sensory Disorders 

• Ocular hyperaemia
• Conjunctival haemorrhage
• Mydriasis
• Eye inflammation
• Upper lid elevation
• Hypotony of eye
• Reduced visual acuity
• Dim vision
• Blurred vision
• Eye allergy
• Eye pruritis
• Dry eye
• Eye irritation
• Ocular discomfort
• Punctate keratitis
• Abnormal sensation in eye
• Eyelid retraction
• Conjunctival blanching
• Dysgeusia
• Conjunctivitis
• Eyelid oedema
• Conjunctival follicles
• Eyelid margin crusting
• Increased lacrimation
• Eye pruritus
• Keratitis
• Keratopathy
• Photophobia
• Corneal erosion
• Corneal infiltrates
• Blepharospasm
• Blepharitis
• Eyelid ptosis
• Eyelid erythema
• Eyelid scales
• Conjunctival vascular disorders
• Conjunctival oedema
• Eye discharge
• Corneal staining

• Monoamine oxidase inhibitors
• Topical and systemic sympathomimetics
• Tricyclic antidepressants
• Central nervous system depressants
• Alcohol
• Barbiturates
• Opiates
• Sedatives
• Anaesthetics
• Systemic clonidine
• Neuroleptic therapy
• Beta blockers (ophthalmic and systemic)
• Cardiac glycosides  
• Antihypertensives

• Intraocular pressure

None routine. Specific cases may require

• Cardiovascular examination
• Mental status

Apraclonidine 0.5% for short-term adjunctive therapy of chronic glaucoma

• The addition of apraclonidine to patients already using two aqueous suppressing agents (i.e. beta-blockers plus carbonic anhydrase inhibitor) as part of their maximally tolerated medically therapy may not provide additional benefit
• This is because apraclonidine is an aqueous suppressing drug and the addition of a third aqueous suppressant may not significantly reduce intraocular pressure
• The maximum recommended duration of therapy is one month due to loss of effect over time (tachyphylaxis). However, some patients may benefit from treatment with apraclonidine for longer periods

Apraclonidine is a relatively selective alpha-2-adrenergic agonist which does not possess significant membrane stabilising (local anaesthetic) activity. When instilled into the eye, apraclonidine has the action of reducing intraocular pressure. Ophthalmic apraclonidine has minimal effect on cardiovascular parameters. Aqueous fluorophotometry studies in man suggest that the mechanism of the ocular hypotensive action of apraclonidine is related to a reduction in aqueous formation.

Eye drops (per ml) 5mg

• Iopidine 0.5% (Novartis South Africa) originator

Eye drops (per ml) 10mg

• Iopidine 1% (Novartis South Africa) originator