Drug Class/Mode of administration

Examples of common drugs

Systemic Effect

Contraindications

Ophthalmologic Condition: Glaucoma

α-2 adrenergic agonists

Administration-Topical

• Apraclonidine (more α1 activity)
• Brimonidine (lipophilic, higher CNS penetration)

Cardiovascular:

Bradycardia, hypotension, vasovagal symptoms

GI: Dry mouth and nose (common), abnormal taste

CNS (lipophilic agent only)

CNS depression, somnolence, HA, fatigue^{2,3,4,5,6,8,9}

Do not use in patients taking a MAO inhibitor or with drugs that block re-uptake of epinephrine/ norepinephrine^2,4,5

β- Adrenergic Antagonists (beta-blockers)

Administration -Topical

• Non-selective(β1/2): Levobunolol, Metipranolol,
• Timolol
• Non-selective with intrinsic sympathomim-etic activity: Carteolol
• Selective β-1: Betaxolol

Side effects rare but more common in elderly or fragile patients

-CNS :

anxiety, confusion, fatigue, hallucinations, dysarthria

-Cardiovascular :

Bradycardia, heart block, arrhythmia, syncope, hypotension, dizziness, reduced exercise capacity

-Respiratory :

Bronchospasm, dyspnea, pulmonary failure

-GI: Diarrhea, nausea, cramping

-Endocrine: Reduces HDL, raise triglycerides, sexual dysfunction ^2,3,4,5,6

Decompensated Heart failure

Heart Block (any type)

• safe with functioning pacemaker

History of unexplained syncope, dizziness or pre-syncope

Symptomatic bradycardia

Asthma

β1-selective agent can be used with well controlled mild-moderate disease

COPD

β1-selective likely safe based on systemic use of β1-selective oral agents in COPD patients^3,7,8

Carbonic Anhydrase

Inhibitors

• Oral & Topical

Oral: Acetazolamide

Topical: Brinzolamide, Dorzolamide

Oral Administration:

• Renal: Metabolic acidosis, sodium and potassium wasting (all transient), urolithiasis, renal failure
• GI: Metallic taste (common), nausea, vomiting, diarrhea, constipation, anorexia, GI bleed

-Nervous system: Parasthesias of fingers/toes (very common), confusion, lethargy, somnolence, fatigue

-Hematologic: Aplastic anemia(not dose or time dependent)

Topical Administration: Rarely serious

-More common: Bitter taste, dry mouth

-Rare: headache, nausea, fatigue, skin rash, urolithiasis^2,3,5,9

Oral

l Administration:

Sulfonamide allergy

Reduced kidney function (Dosage needs to be adjusted as acetazolamide plasma concentrations highly dependent on renal excretion)

• Concomitant use of loop or thiazide diuretics increases electrolyte imbalance and risk of nephrolithiasis
• COPD/CO2 retainer (high risk for severe acidosis with metabolic acidosis combined with pre-existing respiratory acidosis)

Topical Administration:

Sulfonamide allergy ^3,4,5,9

Miotics (now rarely used for chronic glaucoma treatment)

Administration: Topical

Direct cholinergic agonist:

• Acetylcholine, Pilocarpine,
• Indirect cholinergic agonist: Carbachol
• Cholinesterase Inhibitor: Echothiophate iodide

Common: periorbital pain/HA(Pilocarpine)

Other systemic effects rare at recommended doses: diaphoresis, nausea, hypersalivation, bradycardia, hypotension, seizures, Hallucinations, coma^2,3,5,6

Avoid depolarizing agents like succinylcholine with use of cholinesterase inhibitors³

Prostaglandin Analogues

(Prostaglandin F2α Receptor Agonist)

Administration-Topical

BimatoprostLatanoprost, Tafluprost, Travoprost, Unoprostone isopropyl

Minimal to no specific Side Effects

Most often reported but non-specific: flu-like/upper respiratory symptoms

Theoretical stimulation of smooth muscle constriction (tracheobronchial, vascular, uterine) ^2,3

Pregnancy

Active ocular inflammation³

Ophthalmologic Condition: Pupillary Dilation

(Secondary to Mydriatic and Cycloplegic Agents; Used for dilation during routine eye exam as well as for ocular inflammatory conditions)

α-agonist

-Topical

Phenylephrine

Hypertension, cardiac arrhythmias, angina, secondary CHF, pulmonary edema, subarachnoid hemorrhage

Rare but serious, occur more frequently in patients with underlying poorly controlled cardiovascular disease³

10% formulation should never be used in patients with ischemic heart disease or hypertension

2.5% formulation generally safe in all but neonates³

Cycloplegics (anti-muscarinic agents)

-Topical

Atropine Cyclopentolate

Scopolamine

Tropicamide

Acute urinary retention in elderly males with prostate enlargement (rare)

Anti-cholinergic effects (dryness of mouth and skin, flushing, fever, irritability, tachycardia, confusion) Rare, occurs with over-dosing^3,5

Well tolerated in all but very young³