Pharmacotherapy of the eye, ear and skin disorders

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

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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.

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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.