2. Farmakodinamik
• efek biologis dan terapi obat (mekanisme kerja)
• Sebagian besar obat bekerja dengan mengikat
makromolekul, seperti neurotransmiter, reseptor
hormon atau enzim
• Jika obat tersebut bekerja pada tingkat reseptor,
itu bisa berupa agonis atau antagonis
• Jika obat tersebut bekerja pada tingkat enzim,
itu bisa menjadi aktivator atau inhibitor
3. Farmakokinetik
• Proses absorbsi, distribusi, metabolism, dan ekskresi obat/zat
• Obat dapat didistribusikan ke jaringan mata sebagai:
• Obat lokal
• Tetes mata
• Ointment
• Injeksi periocular
• Injeksi intraocular
• Sistemik
• Oral
• Intravena
4. Drug Delivery in Eyes
Topical Periocular Intraocular Systemic
drop
ointment
gel
Soft contact lens
Subconj.
Subtenon
Peribulbar
Retrobulbar
Intracameral
Intravitreal
oral
intravenous
Intramuscular
5. Faktor-faktor yang mempengaruhi penetrasi
obat lokal ke dalam jaringan mata
• Konsentrasi dan kelarutan obat
• semakin tinggi konsentrasinya, semakin baik
penetrasi mis. pilocarpine 1-4%
• Kekentalan
• penambahan metilselulosa dan polivinil alkohol
meningkatkan penetrasi obat dengan meningk-
atkan waktu kontak dengan kornea dan meng-
ubah epitel kornea
• Kelarutan terhadap lemak
• membran sel epitel banyak mengandung lipid,
sehingga semakin tinggi kelarutan dalam lemak
maka semakin penetrasi semakin baik
6. • Surfaktan
• bahan pengawet yang digunakan dalam sediaan okular mengubah
membran sel dalam kornea dan meningkatkan permeabilitas obat
mis. benzylkonium dan thiomersal
• pH
• pH normal air mata adalah 7,4 dan jika pH obat jauh berbeda,
ini akan menyebabkan reflek pengeluaran air mata
• Tonisitas
• ketika obat alkaloid dimasukkan ke dalam media yang relatif al-
kaloid, proporsi bentuk tidak bermuatan akan meningkat, sehin-
gga lebih banyak penetrasi
• Berat dan ukuran molekul
Faktor-faktor yang mempengaruhi penetrasi
obat lokal ke dalam jaringan mata
7. TOPICAL
Drop (Gutta)- simplest and more convenient
mainly for day time use
1 drop=50 microlitre
Conjuctival sac capacity=7-13 micro liter
so, even 1 drop is more than enough
Method
hold the skin below the lower eye lid
pull it forward slightly
INSTALL 1 drop
measures to increase drop absorption:
-wait 5-10 minutes between drops
-compress lacrimal sac
-keep lids closed for 5 minutes after instillation
8. Ointments
Increase the contact time of ocular medication to ocular surface thus
better effect
It has the disadvantage of vision blurring
The drug has to be high lipid soluble with some water solubility to h
ave the maximum effect as ointment
9. Peri-ocular injections
They reach behind iris-lens diaphragm
better than topical application
E.g. subconjunctival, subtenon, peribu-
lbar, or retrobulbar
This route bypass the conjunctival and
corneal epithelium which is good for dr
ugs with low lipid solubility (e.g. penicil-
lins)
Also steroid and local anesthetics can
be applied this way
10. Periocular
Subconjunctival - To achieve higher concentration
Drugs which can’t penetrate cornea due to large size
Penetrate via sclera
Subtenon— ant. Subtenon– disease ant to the Lens
Post Subtenon– disease posterior to the lens
Retrobulbar-Optic neuritis
Papillitis
Posterior uveitis
Anesthesia
Peribulbar-- anesthesia
11. Intraocular injections
Intracameral or intravitreal
E.g.
– Intracameral acetylcholine (
miochol) during cataract su
rgery
– Intravitreal antibiotics in
cases of endophthalmitis
– Intravitreal steroid in
macular edema
12. Sustained-release devices
These are devices that deliver
an adequate supply of medicat
ion at a steady-state level
E.g.
– Ocusert delivering pilocarpine
– Timoptic XE delivering timolol
– Ganciclovir sustained-release i
ntraocular device
– Collagen shields
13. Common ocular drugs
Antibacterials (antibiotics)
Antivirals
Antifungal
Mydriatics and cycloplegics
Antiglaucoma
Anti-inflammatory agents
Ocular Lubricants
Ocular diagnostic drugs
Local anesthetics
Ocular Toxicology
Corticosteroids
NSAID
15. Antibiotics
Used topically in prophylaxis (pre and postop
eratively) and treatment of ocular bacterial in
fections.
Used orally for the treatment of preseptal
cellulitis
e.g. amoxycillin with clavulonate, cefaclor
Used intravenously for the treatment of
orbital cellulitis
e.g. gentamicin, cephalosporin, vancomycin,
flagyl
Can be injected intravitrally for the treatment
of endophthalmitis
16. Specific antibiotic for almost each organisms
Sulfonamiodes- Chlamydial infections like TRACHOMA
INCLUSION CONJUNCTIVITIS
TOXOPLAMOSIS
Bacterial cell wall syntheis inhibitors-
Penicillin
Cephalosporins
I) first generation- gm + cocci eg cephazolone
ii) second generation Gm –and antistaphylococcal cefuroxime
iii) Third generation Gm – bacilli --ceftriaxones
17. Side effects- allergic reaction
neutropenia
thrombocytopenia
Amino glycosides
mainly against gm negative bacilli
Bacterial protein synthesis inhibitors
Gentamycin—0.3% eye drop
Tobramycin- Pseudomonas 1% eye drop
Neomycin—0.3-0.5% eye drop
18. Tetracycline
Inhibit protein synthesis
active against both gm+ and gm -, some fungi and Chlamydia
Chloromphenicol
Broad spectrum ,bacteriostatic, gm+/gm-, Chlamydia
0.5% Eye drop, ointment
19. Antibiotics
Trachoma can be treated by topi
cal and systemic tetracycline or e
rythromycin, or systemic azithro
mycin.
Bacterial keratitis (bacterial corn
eal ulcers) can be treated by topi
cal fortified penicillins, cephalosp
orins, aminoglycosides, vancomy
cin, or fluoroquinolones.
Bacterial conjunctivitis is usuall
y self limited but topical erythro
mycin, aminoglycosides, fluoroqu
inolones, or chloramphenicol can
be used
20. Antivirals
Acyclovir
3% oinment 5 times-10-14 days
800mg oral 5 times 10-14 days
intravenous for Herpes zoster retinitis
Others
Idoxuridine
Vidarabine
Cytarabine
Triflurothymidine
Gancyclovir
INDICATIONS
HZ keratitis
Viral uveitis
21. ANTIFUNGAL
INDICATIONS
Fungal corneal ulcer
Fungal retinitis/ Endophthalmitis
Commonly used drugs are
Polyenes
– damage cell membrane of susceptible fungi
– e.g. amphotericin B, natamycin, nystatin
– side effect: nephrotoxicity
Imidazoles
– increase fungal cell membrane permeability
– e.g. miconazole, ketoconazole,fluconazile
Flucytocine
– act by inhibiting DNA synthesis
22. Mydriatics and cycloplegics
Dilate the pupil, ciliary muscle paralysis
CLASSIFICATION
Short acting- Tropicamide (4-6 hours)
Intermediate- homatropine ( 24 hours)
Long acting- atropine (2 weeks)
Indications
corneal ulcer
uveitis
cycloplegic refraction
24. Carbonic anhydrase inhibitors
Systemic topical
acetazoamide Dorzolamide
brinzolamide
Mechanism of action---- reduce aqueous humour formation
Side effect
Paresthesiae
Frequent urination
GI disturbances
Hypokalamia
25. Hyperosmotic agent--- iv mannitol
when IOP is very high 60-70
Prostaglandins
Latanoprost (0.005% eye drop)
increased aqueous out flow
Reduced IOP
Side effect– conjunctival redness, iris and periocular pigmentation
hypertrichosis, darkening of iris
35. Ocular diagnostic drugs
Fluorescein dye
– Available as drops or strip
s
– Uses: stain corneal abrasio
ns, applanation tonometry,
detecting wound leak, NL
D obstruction, fluorescein
angiography
– Caution:
• stains soft contact lens
• Fluorescein drops can be
contaminated by Pseudo
monas sp.
36. Ocular diagnostic drugs
Rose bengal stain
– Stains devitalized epithelium
– Uses: severe dry eye, herpetic keratitis
37. Local anesthetics
topical
– E.g. propacaine, tetracaine
– Uses: applanation tonometry, goniscopy, re
moval 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
40. Complications of topical administration
Mechanical injury from the bottl
e e.g. corneal abrasion
Pigmentation: epinephrine-
adrenochrome
Ocular damage: e.g. topical anes
thetics, benzylkonium
Hypersensitivity: e.g. atropine, ne
omycin, gentamicin
Systemic effect: topical phenylep
hrine can increase BP
41. Amiodarone
A cardiac arrhythmia drug
Causes optic neuropathy (mild decreased vision, visual fie
ld defects, bilateral optic disc swelling)
Also causes corneal vortex keratopathy (corneal verticillat
a) which is whorl-shaped pigmented deposits in the corn
eal epithelium
42. Digitalis
• A cardiac failure drug
• Causes chromatopsia (objects appear
yellow) with overdose
43. Chloroquines
• E.g. chloroquine,
hydroxychloroquine
• Used in malaria, rheumatoid
arthritis, SLE
• Cause vortex keratopathy
(corneal verticillata) which is
usually asymptomatic but can
present with glare and
photophobia
• Also cause retinopathy (bull’s
eye maculopathy)
44. Chorpromazine
• A psychiatric drug
• Causes corneal punctate epithelial
opacities, lens surface opacities
• Rarely symptomatic
• Reversible with drug discontinuation
45. Ethambutol
• An anti-TB drug
• Causes a dose-related optic neuropathy
• Usually reversible but occasionally
permanent visual damage might occur