Farmakologi

Bagian Mata
dr. Ave Olivia Rahman, MSc.
Bagian Farmakologi FKIK UNJA

Daftar Kompetensi
Kompetensi 4A : benda asing, konjungtivitis,
blefaritis, hordeulum, perdarahan
subkonjungtiva, trikiasis, mata kering dsb
Kompetensi 3B : glukoma akut, dsb

1. Conjunctivitis
Inflamation of Conjunctiva
Cause : allergic, infectious (bacterial, viral,
fungal), Chemical (air pollution, chlorine in
swimming pools, and exposure to noxious
chemicals)
Opthalmia neonatorum

Allergic conjunctivitis

Remove (or avoid the irritant).

Cool compresses
Artificial tears
Ophtalmic NSAIDs (Flurbiprofen,
Indomethacine, Ketorolac)
Ophtalmic decongestan and antihistamines.
Persistent allergic conjunctivitis topical
steroid eye drops.

Infectious Conjunctivitis
Bacterial conjunctivitis.
Antibiotic eye drops or ointments.
Bacterial conjunctivitis may improve after three or
four days of treatment, but patients need to take the
entire course of antibiotics to prevent recurrence.

Viral conjunctivitis.
Antibiotics will not cure a viral infection.
Self limited disease
Relieving Symptoms cool compresses and artificial
tear solutions.
For the worst cases topical steroid drops to reduce
the discomfort from inflammation (but not for shorten
the infection)

Chemical conjunctivitis.
Careful flushing of the eyes with saline
Topical steroids.

2. Blepharitis
Inflammation of the eyelids
Bacterial Antibiotics (or combination with
Steroid) topical or systemic

Topical for Eye

1. Drops/ tetes mata
2. Ointment

Tetes Mata/Drops
Mudah, lebih sederhana
1 tetes = 50l ; Kapasitas conjungtival sac = 7-13 l 1
tetes lebih dari cukup
Teknik :

buka kelopak mata bawah teteskan

Tunggu 5-10 menit diantara tetesan berikutnya
Tekan lacrimal sac
Tutup kelopak mata selama 5 menit setelah pemberian
50 % obat masih ada setelah 4 menit pemberian, 10% obat
masuk ke humour aqueous
Tekan duktus nasolakrimalis untuk mengurangi absorbsi
sistemik

Ointment
Meningkatkan waktu kontak obat dengan
permukaan mata peningkatan efek obat
Kekurangan : penglihatan buram sementara.

Pemberian secara Sistemik

Oral, IV, IM, SC
Absorbsi ke jaringan mata kurang baik
dikarenakan retinal vascular endothelium
tight junction blood-ocular barrier
Faktor yang mempengaruhi absorbsi obat
yang diberikan sistemik ke dalam jaringan
mata :
Kelarutan dalam lipid
Ikatan protein
Inflamasi mata

Antibiotik

Penicillins
Cephalosporins
Generasi I : aktif pada gram + dan -; tidak aktif pada MRSA,
Enterobacter, Proteus spp, P aeruginosa, Serratia, enterococci
Generasi II : lebih aktif terhadap gram Generasi III : lebih luas. Cefotaxime penetrasi ke bloodocular
barrier baik.
Generasi IV : lebih luas.
Sulfonamides Chlamydial infections
Tetracyclines gram+ dan , beberapa fungi dan Chlamydia
Chloramphenicol luas.
Aminoglycosides terutama basil gram Vancomycin MRSA, streptococus ; corneal ulcer, endophthalmitis
Macrolides

AntiViral
Acyclovir

Menghambat sintesis DNA virus.

Efektif melawan HSV I & II, HZV
Oral, ointment
untuk herpetic keratitis

Trifluridine
Menghambat sintesis DNA, replikasi RNA
Efektif melawan HSV I & II
Penetrasi ke kornea lebih besar

Ganciclovir

Efektif melawan CMV

Oral, iv, intravitreal
Untuk terapi CMV retinitis
Efek samping : supresi sumsum tulang, gagal ginjal

AntiFungal
Indikasi : ulser kornea fungal, fungal retinitis/endophthalmitis
Sediaan yang sering digunakan :
Polyenes
Merusak membran sel jamur
Cth : Amphotericin B, Natamycin, nystatin
Efek samping : nefrotoksik
Imidazoles
Meningkatkan permeabilitas membran sel jamur
Cth. Miconazole, ketoconazole,fluconazole
Flucytocine
Menghambat sintesis DNA

STEROID
Jangan berikan jika curiga ada infeksi aktif
Efek samping :
OCULAR : Glaucoma, Cataract, Activation of
infection, Delayed wound healing
SYSTEMIC : Peptic ulcer, Hypertension, Increased
blood sugar, Osteoporosis, Mental changes,
Activation of tuberculosis and other infections

Antihistamine
Pyrilamine maleate, pheniraminemaleate,
antazoline phosphate
Can cause sedation, mydriasis and increase
IOP

Mast Cell Stabilizer

Inhibit histamine and vasoactive substance
release from mastcell
Use in chronic cases e.g. vernal and seasonal
allergic conjunctivitis

3. Glukoma

Peningkatan Tekanan Intra Okuler

Produksi >> ekskresi Humour Aquous
Glukoma sudut terbuka
Glukoma sudut tertutup
Tujuan terapi : menurunkan tekanan intra
okuler (TIO) normal 15-20 mmHg

Terapi Glukoma Sudut Terbuka

1. Menurunkan produksi humour aquous
a) -blockers (ex. Timolol, betaxolol)
b) 2-agonists (apraclonidine, brimonidine)
c) inhibitor carbonic anhydrase (dorzolamide,
brinzolamide)
2. Memfasilitasi drainase melalui trabecular meshwork
a) Parasympathomimetics/agonist Cholinergic (ex.
pilocarpine)
3. Memfasilitasi drainase melalui uveoscleral route
a) Derivat prostaglandin (lanatoprost and
bimatoprost)

Terapi Glukoma Sudut Tertutup

1. Menurunkan produksi humour aquous
a) osmotic agents
b) -blockers
2. Operasi

Obat Antiglukoma: 1. Beta blockers

Selective : betaxolol, etc
Non selective : timolol, etc
Mekanisme : menurunkan produksi aqueous humour
menurunkan IOP
Efek samping :
Lokal : Irritation, Frontal headache, Iris cyst,
Follicular conjunctivitis.
Sistemik : Bradycardia, Sweating, Anxiety

2. Alpha2 agonists
Brimonidine, Apraclonidine
Actions : decrease aqueous production, and increase
uveoscleral outflow
Side Effect :
local: reaksi alergi, midriasis, lid retraction,
conjunctival blanching
systemic: oral dryness, headache, fatigue, drowsiness,
orthostatic hypotension, vasovagal attacks
Contraindications : Infants, MAO inhibitors users

3. Carbonic anhydrase inhibitors

Systemic : Acetazoamide
Topical : Dorzolamide, Brinzolamide
Actions : decrease aqueous production
Side Effects: Paresthesiae, Frequent
urination, GI disturbances, Hypokalamia

4. Derivate Prostaglandins

Latanoprost (0.005%)
Bimatoprost (0.03%)
Travoprost (0.004%)
Action : increase humour aqueous out flow
Side Effect: conjunctival congestion, iris and
periocular, pigmentation, hypertrichosis,
darkening of iris

5. Osmotic Agent
Mekanisme aksi : Dehidrasi cavum vitreous
menurunkan IOP.
Glycerine 100%
Efek samping nausea, hyperglycemia
Efek dalam 30 min dan durasi 56 jam

Mannitol 20% IV
Efek samping fluid overload; kontraindikasi pada
gagal jantung
dosis 12 g/kg IV dalam 30 min.
Efek dalam 2060 min dan durasi 26 jam

6. Agonist Kolinergik
A. Parasimpatomimetic Direct acting
Obat : pilocarpine, acetylcholine (miochol), carbachol
(miostat)
Mekanisme :
Miosis dengan kontraksi iris sphincter muscle
Meningkatkan aqueous outflow melalui trabecular
meshwork dengan cara kontraksi longitudinal ciliary
muscle
Akomodasi dengan kontraksi circular ciliary muscle

Efek samping:
Local: myopia, headache, cataract, miotic cysts, retinal
detachment (jarang)
Sistemik : lakrimasi, salivasi,berkeringat, spasm bronkial,
mual, muntah, diare, urinary urgensi

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B. Indirect Acting (antikolinesterase)
Lebih poten dengan durasi kerja lebih panjang
Reversibel inhibitors : cth. Physostigmine
Digunakan dalam terapi glaucoma dan dapat
menyebabkan efek samping SSP

4. Anestesi Lokal
Topical
E.g. propacaine, tetracaine, procaine, chloroprocaine,
benoxinate, cocaine
Uses: applanation tonometry, gonioscopy, removal of
corneal foreign bodies, removal of sutures, examination
of patients who cannot open eyes because of pain
Adverse effects: toxic to corneal epithelium, allergic
reaction rarely

Orbital infiltration
Peribulbar or retrobulbar
Cause anesthesia and akinesia for intraocular surgery
E.g. Lidocaine, bupivacaine, Mepivacaine

5. Midriatikum dan Cycloplegics

Mydriaticum Mydriasis (melebarkan pupil)
Cycloplegia Paralisis otot siliaris kehilangan
daya akomodasi
Golongan Antagonist Kolinergik :
Tropicamide, cyclopentolate, homatropine,
scopolamine, atropine

Klasifikasi :
Short acting : Tropicamide (46 jam)
Intermediate : Homatropine ( 24 jam)
ong acting :Atropine (2 minggu )

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Side Effets :
Lokal: allergic reaction, blurred vision
Sistemik : nausea, vomiting, pallor, vasomotor
collapse, constipation, urinary retention, dan
confusion, pada anak : flushing, fever,
tachycardia, delerium
Indication :
Topical mydriatic eye examination, to treat
inflammatory eye conditions such as iritis and
cyclitis.

Ocular Toxicology
Complications of Topical Administrations
Mechanical injury from the bottle e.g. corneal
abrasion
Pigmentation: epinephrineadrenochrome
Ocular damage: e.g. topical anesthetics,
benzylkonium
Hypersensitivity
Cataract ex. Steroid
Systemic effect

Agents that can Cause Toxic Optic Neuropathy

Methanol
Ethylene glycol (antifreeze)
Chloramphenicol
Isoniazid
Ethambutol
Digitalis
Chloroquine
Streptomycin
Amiodarone
Quinine
Vincristine and methotrexate (chemotherapy medicines)
Sulfonamides
Melatonin with Zoloft (sertraline, Pfizer)