FARMAKOLOGI SISTEM SENSORIS Kelainan pada organ sensoris, yaitu mata berdasarkan struktur anatominya, dapat dikelompokkan atas kelainan bagian anterior, tengah dan posterior bola mata dan struktur mata, sedangkan untuk telinga, dikelompokkan atas kelainan telinga luar, tengah dan dalam. Apapun etiologi dari kelainan/penyakit tersebut, obat harus dapat mencapai daerah yang mengalami kelainan (farmakokinetika), baru dapat berkerja mengatasi kelainan tersebut (farmakodinamika). Terdapat beberapa rute yang dapat dipilih untuk memberikan obat dengan bentuk sediaan tertentu. Setipa rute memiliki kelebihan dan kekurangan. Rute-rute tersebut adalah: 1. Topikal : bentuk sediaan obat : tetes (solution dan suspensi), salep 2. Oral : tablet, kapsul, sirup, eliksir 3. Parenteral : a. Intravena, intra muskuler, subkutan, intrakutan
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FARMAKOLOGI
SISTEM SENSORIS
Kelainan pada organ sensoris, yaitu mata berdasarkan
struktur anatominya, dapat dikelompokkan atas kelainan
bagian anterior, tengah dan posterior bola mata dan struktur
mata, sedangkan untuk telinga, dikelompokkan atas kelainan
telinga luar, tengah dan dalam.
Apapun etiologi dari kelainan/penyakit tersebut, obat harus
dapat mencapai daerah yang mengalami kelainan
(farmakokinetika), baru dapat berkerja mengatasi kelainan
tersebut (farmakodinamika). Terdapat beberapa rute yang
dapat dipilih untuk memberikan obat dengan bentuk sediaan
tertentu. Setipa rute memiliki kelebihan dan kekurangan.
Rute-rute tersebut adalah:
1. Topikal : bentuk sediaan obat : tetes (solution dan
suspensi), salep
2. Oral : tablet, kapsul, sirup, eliksir
3. Parenteral :
a. Intravena, intra muskuler, subkutan, intrakutan
Intratympanic ; misalnya gentamicin dan steroid untuk
mengobati penyakit menier (telinga dalam)
Metodenya :
Transtympanic injection atau myringotomy
Silverstein MicroWick ®
Microcatheter implantation
Hydrogel application
Nanoparticles
Langsung ke dalam telinga dalam (intakoklear)
o Metodenya :
Melalui Cochlear Implantation
Melalui osmotic pump
Melalui reciprocating perfusion system
FARMAKOLOGI OBAT MATA
PENGATURAN FUNGSI STRUKTUR PADA MATA OLEH SISTEM SARAF OTONOM
Jaringan
Reseptor Adrenergik (Simpatis)
Reseptor Kolinergik (Parasimpatis)
SUBTIPE RESPON SUBTIPE RESPON
Epitel kornea β2 Belum diketahui Ma Belum diketahui
Endotel kornea β2 Belum diketahui Belum teridentifikasi
Belum diketahui
Otot radial iris α1 Midriasis
Otot spinkter iris
M3 Miosis
Trabecular meshwork
β2 Belum diketahui
Epitel siliaris b α2/β2 Produksi humor Aqueous
Otot siliaris β2 Relaksasi c M3 Akommodasi
Kelenjar Lakrimal
α1 Sekresi M2, M3 Sekresi
Epitel pigmen retina
α1/β2 H2O transport/belum diketahui
a walaupun asetilkolin dan choline acetyltransferase banyak ditemukan di epitel kornea, tetapi fungsi dari neurotrasmitter ini belum diketahui dengan jelas.
b epitel siliaris juga merupakan terget kerja carbonic anhydrase inhibitors. Isoenzim II Carbonic anhydrase, ditemukan pada epitel pigmen dan tidak berpigmen pada epitel siliaris.
cwalupun reseptor β2 adrenergik mengatur relaksasi otot polos badan/corpus siliaris, belum ada data tentang pengaruhnya yang signifikan terhadap proses akomodasi.
ANTIMIKROBA
Aminoglycosida* Obat Dosage Form Comment
Neomycin Solution and salep and corticosteroid
Only in combination form; greatest potential for sensitivity RX of all in group
Gentamicin Solution and salep and corticosteroid Relatively high corneal toxicity
Tobramycin Solution and salep and corticosteroid Good antipseudomonal activity
Amikacin
No ophthalmic
Excellent for treatment of resistant P. aeruginosa strains; must be extemporaneously prepared in a 6.7-mg/cc solution
*Action: Inhibition of protein synthesis; bactericidal.
Macrolida*
Obat Dosage Form Comment Erytjamomycin
Ophthalmic salep; oral tablets and pediatric suspension
Classic alternative for penicillin-sensitive patients; marked GI upset; med. spectrum
Claritjamomycin Only systemic dosage forms; tablets and pediatric suspension
Long half-life allows twice daily dosing; excellent for Hemophilus
Azitjamomycin Only systemic dosage forms; tablets and pediatric suspension
Long half-life allows daily dosing; Obat of choice for chlamydia in all age groups
*Action: Inhibition of protein synthesis; bacteriostatic and bactericidal activity.
Tetracyclin*† Obat Dosage Form Comments
Tetracycline Ophthalmic suspension and salep; oral capsules and syrup
Effective oral treatment for marginal Staphylococcal blepharitis; alternative treatment for chlamydia
Doxycycline Oral dosage form only
Long half-life allows once or twice daily dosing; OK to take with food; tetracycline of choice
Menitocycline Oral dosage form only
Once to twice daily
Gram (+) and Gram (-) coverage *Action: Inhibition of protein synthesis; bacteriostatic. †WARNING: All tetracyclines are contraindicated in children and pregnant women. Avoid dairy products and antacids with tetracycline. Tetracyclines can produce photosensitivity.
Sulfonamid* Obat Dosage Form Comment
Sulfacetamide Ophthalmic solution and salep and corticosteroid
Marked S. aureus resistance
Sulfasoxazole Opthalmic solution
Same as above; less sting upon instillation than sulfacetamide
Sulfamethoxazole and trimethoprim TMP-SMZ
Oral tablets and suspension
Synergistic combination effectively inhibits folic acid; very effective in treating toxoplasmosis; alternative treatment for chlamydia; avoid in pregnant women and sulfonamide-sensitive patients
*Action: Inhibition of bacterial folic acid synthesis by inhibiting the enzymatic conversion of para-amenitobenzoic acid (PABA) to dihydrofolic acid; bacteriostatic.
Fluoroquinolon* Obat Dosage Form Comment
Ciprofloxacin Ophthalmic solution; oral tablets
Approved for monotherapy of bacterial keratitis; increasing bacterial resistance; incidence of corneal precipitates
Ofloxacin Ophthalmic solution; oral tablets
No corneal precipitates; approved for monotherapy of bacterial keratitis
Norfloxacin Ophthalmic solution; oral tablets
Not approved for bacterial keratitis; useful for bacterial conjuctivitis
Moxifloxacin Ophthalmic solution; oral tablets
Improved Gram (-) and Gram (+) coverage
Gatifloxacin Ophthalmic solution; oral tablets
Improved Gram (-) and Gram (+) coverage
Leuofloxacin Ophthalmic Purified Leuoisomen of Ofloxacin-
solution lower mic-90 than Ofloxacin *Action: Inhibit bacterial reproduction by inhibiting DNA gyrase; bactericidal.
Penicillin*† Obat Dosage Form Comments
Ampicillin Oral tablets, suspension, and injection
First broad-spectrum, semisynthetic penicillin; not effective against β-lactamase-producing bacteria
Amoxicillin Oral tablets and suspension
Pro-Obat of ampicillin, therefore, less GI upset, better absorption and tid vs qid dosing
Dicloxacillin Oral capsules and suspension
Excellent resistance to β-lactamase
Amoxicillin/potassium clavulanate
Oral tablets and suspension
Excellent resistance to β-lactamase, but much more expensive than dicloxacillin
*Action: Inhibit cell-wall synthesis; bactericidal. †WARNING: Approximately 3% of the population (1-10%) reports penicillin sensitivity. A careful history to evaluate for penicillin sensitivity is absolutely necessary prior to their use. Non-penicillinase Staphylococcus and Hemophilus sp. are now the exception. When prescribing penicillins for eye infections commonly caused by these microbes, one should assume that they are β-lactamase-producing strains and select the Obat accordingly.
Sefalosforin*
Obat Dosage Form Comments FIRST GENERATION
Cephalexin Oral capsules and suspension
Inexpensive alternative in penicillin-sensitive patients
Cefazolin Powder for injection
Used to formulate fortified topical antibitotic to treat bacterial keratitis
SECOND GENERATION
Cefaclor Oral tablets and suspension
Excellent action against Hemophilus influenzae;
Cefuroxime Oral and IV Same as above Note: Approximately 3-15% of the population that reports penicillin sensitivity will also exhibit sensitivity to the cephalosporins. First-generation cephalosporins show excellent activity against β-lactamase-producing Gram (+) microbes, but limited Gram (-) activity.
Second-generation cephalosporins are quite useful in managing Hemophilus influenzae, which is particularly common in children. They also have the advantage of twice-daily dosing. A simple way to remember the spectrum of activity of the second-generation cephalosporin agents is by the pneumonic HENPEK: H: Hemophilus E: Enterococci N: Neisseria P: Proteus E: E. Coli K: Klebsiella
*Action: Inhibit cell-wall synthesis; greater resistance to β-lactamase than some of the penicillins.
Chloramphenicol*† Obat Dosage Form Comment
Chloramphenicol Ophthalmic solution and salep; oral capsule and suspension
High lipid solubility; excellent corneal penetration; low corneal toxicity; crosses blood-brain barrier—useful in meningitis
*Action: Inhibition of protein synthesis; bacteriostatic. †WARNING: Chloramphenicol can produce dose-related CNS toxicity in children or adults with reduced hepatic microsomal activity. Both topical and systemic chloramphenicol can produce aplastic anemia. This is a potentially fatal, nondose-related reaction.
Bacitracin*
Obat Dosage Form Comments Bacitracin Ophthalmic salep Useful for Gram (+) species Powder for
injection Can be prepared as fortified solution for treatment of bacterial keratitis
*Action: Inhibition of cell-wall synthesis; bactericidal. Bacitracin is used in combination with a variety of other topical ophthalmic agents. It is primarily used in these products to enhance their ability to kill Gram (+) (staphylococcal and streptococcal sp.). Products that contain bacitracin include: Polysporin ophthalmic salep; Polytrim ophthalmic solution; Neosporin ophthalmic salep.
Polymyxin B* Obat Dosage Form Comments
Polymyxin B
Combined with other agents in a variety of ophthalmic products
Very effective against Gram (-) bacteria, particularly P. aeruginosa
*Action: Cell-wall inhibitor; bactericidal.
Polymyxin B is used in combination with other antibacterial agents to enhance their spectrum of activity.
It is particularly useful against Gram (-) organisms, in particular P. aeruginosa. Polymyxin B combination products include: Polysporin ophthalmic salep; Terramycin with polymyxin B ophthalmic salep; Neosporin ophthalmic solution; Neosporin ophthalmic salep.
Vancomycin* Obat Dosage Form Comments
Vancomycin No ophthalmic dosage form; oral capsules and powder for injection
Major ophthalmic use is as topical prepared from powder to manage resistant Staphylococcus sp.; oral Obat of choice to manage C. dificile infection
aMydriasis dan cycloplegia, atau paralisis akomodasi pada mata manusia, terjadi [ada pemberian satu tetets atropine 1%, scopolamine 0.5%, homatropine 1%, cyclopentolate 0.5% or 1%, dan tropicamide 0.5% or 1%.
Midriasis rekoveri yaitu ukuran pupil kembali ke normal, yaitu sekitar 1 mm.
Waktu yang dibutuhkan obat untuk menimbulkan midriasi maksimal dan rekoveri (kembali ke keadaan normal) secara berturut-turut; atropine, 30 - 40 menit dan 7 - 10 hari; scopolamine, 20 - 130 menit dan 3 - 7 hari; cyclopentolate, 30 - 60 menit dan 1 hari; tropicamide, 20 - 40 menit dan 6 jam.
Waktu yang butuhkan untuk menimbulkan siklopegi dan untuk rekoveri: atropine, 60 - 180 menit dan 6 to 12 hari; scopolamine, 30 - 60 menit dan 3 7 hari; homatropine, 30 - 60 menit dan 1 to 3 hari; cyclopentolate, 25 - 75 menit dan 6 jam - 1 hari; tropicamide, 30 menit dan 6 jam.
CYCLOPLEGIC (SIKLOPLEGIK)
Indikasi penggunaan Cycloplegic (sikloplegik), a/l:
1. Strabismus (khususnya esotropia) 2. Amblyopia 3. Anisometropia 4. Pseudomyopia 5. Hyperopia yang berhubungan dengan esophoria atau
gangguan akomodasi
Perbandingan antara obat Cycloplegic
Obat Dosis Onset (mula
kerja) Cyclopelgia
Durasi (lama kerja)
Cycloplegia
Tropicamide 1% 1 tetes, diulangi setelah 5 menit 20-30 menit 4-8 jam
Cyclopentolate 0.5% and 1.0%
1 tetes, diulangi setelah 5 menit 20-45 menit 8-24 jam
Homatropine 5% 1 tetes, diulangi setelah 5 menit 30-60 menit 24-48 jam
Scopolamenite 0.25%
1 tetes, diulangi setelah 20 menit 30-60 menit 5-7 hari
Atropine 0.5% salep 1/4″ salep 30-60 menit 10-14 hari
Akwa Tears White petrolatum, meniteral oil, lanolin
Tidak ada
Dey-Lube White petrolatum Tidak ada
Duolube White petrolatum, meniteral oil
Tidak ada
Duratears Naturale
White petrolatum, meniteral oil, lanolin
Methylparaben, propylparaben
Hypotears Salep
White petrolatum, meniteral oil
Tidak ada
Lacri-Lube NP White petrolatum, meniteral oil, lanolin
Tidak ada
Lacri-Lube S.O.P.
White petrolatum, meniteral oil, lanolin Chlorobutanol
Refresh PM White petrolatum, meniteral oil, lanolin Tidak ada
DEKONGESTAN
Mekanisme kerja dari dekongestan adalah mengaktifkan reseptor
alfa 1 saraf simpatis
pada pembuluh darah, sehingga terjadi vasokonstriksi yang
akhirnya mengurangi gejala
hiperemia dan edema.
Decongestan*
Obat Dosis dan
bentuk sediaan
Catatan
TOPIKAL
Phenyephrine
0.12% OTC solution
2.5% RX solution
Semua dekongestan dikontraindikasikan pada kasus glaukoma sudut tertutup, ,hipertensi sitemik unstable, dan penggunan obat golongan MAO inhibitors. Penggunaan yang berlebihan dapat memicu
hiperemia (rebound hyperemia)
Naphazoline
0.0125-0.03% OTC solution 0.1% RX solution
Derivat Imidazole
Oxymetazolone 0.025% OTC solution
Dekongestan yang paling lama masa kerjanya
Tetrahydrozoline 0.05% OTC solution
ORAL
Pseudoephedrine
Tablet oral, sirup (pediatrik) : 30- dan 60-mg
Kontraindikasi pada penderita hipertensi dan kelainan jantung heart disease and hypertension
OBAT GLAUKOMA
Patofisiologi secara umum glaukoma adalah terjadinya peningkatan
tekanan intraokuler akibat ketidakseimbangan antara produksi
humor aquous dengan penyaliran humour aquous, baik penyaliran
antara kamera okuli posterior ke anterior, maupun dari mata ke