Pharmacotherapy of the eye, ear and skin disorders

Sutomo Tanzil Department of Pharmacology, Faculty of Medicine, Sriwijaya University


Fig. 9.2 Rang & Dale pg 124 .

a state known as cycloplegia. The constrictor muscle is more powerful and receives parasympathetic innervation. while antimuscarinic drugs fix the lens for far objects with blurring of near vision. It has a parasympathetic (PS) nerve supply and contracts in response to PS stimulation.Ocular physiology/pharmacology • Vision depends upon the eye converting light falling on the retina into an electrical signal to the brain • The ciliary muscle is a circular smooth muscle attached to the lens. . • Pupil size is determined by 2 smooth muscle layers of the iris. The radial (dilator) muscle is sympathetically innervated (α1-receptors). • Muscarinic agonists fix the lens for near vision.

a response mediated by the PS nervous system • Mydriasis has the effect of moving the iris towards the cornea and narrowing the anterior angle between the iris and the cornea.Ocular physiology/pharmacology • Miosis occurs in response to muscarinic agonists • Mydriasis can occur in response muscarinic antagonists or to α1-adrenoceptor agonists. that may cause prrogressive loss of vision . • The intraocular pressure rises if drainage of the aqueous humour is impaired. • Miosis also accompanies accommodation for near vision. This can reduce aqueous humour outflow through the canal of Schlemm. leading to the occurrence of glaucoma.


these drugs have been largely replaced by topical beta-blockers and prostaglandin derivatives.echothiophate). For chronic glaucoma. . carbachol) or cholinesterase inhibitors (physostigmine. glaucoma was treated w/ either direct agonists (pilocarpine. • Acute angle-closure glaucoma is a medical emergency that is frequently treated initially w/ drugs but usually requires surgery for permanent correction (iridectomy).Clinical pharmacology of the cholinomimetics • In the past.

brinzolamide. travoprost). muscarinic agonists (pilocarpine). . timolol). dipivefrine). α2agonists (brimonidine. α2-agonists (brimonidine. dipivefrine). carbonic anhydrase inhibitors ( acetazolamide. dorzolamide).Drugs used for chronic th/of simple (open-angle) glaucoma • Reducing aqueous humour production : BB (betaxolol. • Increasing aqueous humour outflow : Pg derivatives ( latanoprost.

. local stinging. • The other drugs are usually added to first-line th/ for patients who have an inadequate response. and painful ciliary spasm) • Acute closed-angle glaucoma is a medical emergency and the patient should be referred to a specialist. transient blurred vision.Choice of th/for simple glaucoma • BB and Pg analogues are first-line treatments. They are not considered first-line treatment because of limited efficacy (carbonic anhydrase inhibitors) or a high incidence of local adverse effects (eg. because they are effective and have less ADRs.

opening of trabecular meshwork. • Prostaglandins (eg. increased outflow • α-agonists (eg. travoprost): increased outflow .latanoprost. betaxolol) : decreased aqueous secretion from ciliary epithelium • Diuretics(eg.brimonidine): decreased aqueous secretion • Beta-blockers (eg.acetazolamide) : decreased aqueous secretion due to lack of bicarbonate ions.dipivefrine) : increased outflow • α2-agonists (eg.pilocarpin): ciliary muscle contraction.timolol.Mechanisms of action of drugs used in open-angle glaucoma • Cholinomimetics(eg.

cyclopentolate. eg. phenylephrine. such as homatropine. • α1-agonists. tropicamide • Antimuscarinics should never be used for mydriasis unless cycloplegia or prolonged action is required. homatropine.The clinical pharmacology of antimuscarinics • Atropine. • It is also used to prevent synechia (adhesion) formation in uveitis and iritis. The longer-lasting preparation. . are valuable for this indication. produce a shortlasting mydriasis that is usually sufficient for funduscopic examination.

Carbonic anhydrase inhibitors • Acetazolamide (oral). brinzolamide (eye drops). dorzolamide (eye drops) • Inhibition of carbonic anhydrase results in reduced formation of aqueous humour • Used in the th/of glaucoma in patients who are BB resistant or in whom a BB is contraindicated • Acetazolamide is a sulfonamide derivative. do not use it in people w/ a history of severe allergy to sulfonamide . therefore.

• NSAIDs : diclofenac. flurbiprofen & ketorolac • Artificial tears : hydroxypropyl methylcellulose. or formation of a ‘steroid cataract’ • Antiallergics : antazoline • Local anaesthetics : lidocaine/oxybuprocaine for tonometry.Other topical applications for the eye • Antibacterials : gentamicin. chloramphenicol. fusidic acid. Prolonged use can lead to thinning of the sclera or cornea. neomycin & chlortetracycline • Antivirals : acyclovir • Corticosteroids : dexamethasone. carbomers . removal of cataracts.

intravitreal injection of bevacizumab/ranibizumab (vascular growth factor inhibitors) . photodynamic th/ using photosensitizing agent verteportin.ARMD (age-related macular degeneration) • Dry (non-exudative) form : 85-90% of cases • Wet (exudative) form produces severe loss of vision in 70% of eyes within 2 years • Th/:high-dose of anti-oxidants. laser photocoagulation of neovascular tissue.

cerebellopontine angle tumours . vestibular neuronitis. migraine. brainstem ischaemia. benign positional vertigo. temporol lobe epilepsy. usually perceived as spinning.Vertigo • Hallucination of motion. which is generated in the vestibular system of the inner ear • Caused by Meniere’s disease. multiple sclerosis.

Neurochemistry of vertigo • • • • • Glutamate (excitatory via NMDA ) Acetylcholine (excitatory via M2 ) GABA (inhibitory via GABAA & GABAB) Histamine (excitatory via H1 & H2) NA (modulation of vestibular sensory transmission) • Dopamine (excitatory) .

promethazine.Drugs for TH/ of Vertigo • Antihistamine (cyclizine. most widely used) • Antimuscarinic (hyoscine) • Benzodiazepine (short-term for severe vertigo) • Cimetidine. • H-receptor agonist (betahistine) • D-receptor antagonist (prochlorprazine) .

• AHs . vasodilators and antiparkinsonians can cause vertigo. vestibular apparatus can be ablated w/ local delivery of gentamicin . effectively treated w/ vestibular exercises • Meniere’s disease : promethazine. Furosemide & HCT can be attempted for persistent synptoms. or w/ surgical treatment. • For refractory symptoms. . cinnarizine or prochlorprazine. • Betahistine is often co-prescribed w/ a diuretic.vertigo : less responds to drugs.neuronitis) : antiemetic agents • Benign parox.Management of vertigo • Acute vertigo (vest.

they do not make a mess. . absorbed more quickly into the skin • Lotions : liquids. used on wet surfaces and hairy areas.Skin pharmacology • Topical preparations have two components : a base and the active ingredients. such as a corticosteroid or an antifungal • Ointments : greases such as white/yellow paraffin • Pastes : suspension of powder in an ointment • Creams : emulsions of water with a grease. less greasy than ointments.