OBAT TOPIKAL..

Australian Drug Evaluation Committee (1999) yang secara garis besar obat-obat masuk dalam 5 kategori : Kategori A : Obat yang telah dipakai oleh sejumlah wanita hamil dan wanita mampu hamil tanpa disertai kenaikan frekuensi malformasi janin atau pengaruh buruk, baik secara langsung maupun tidak langsung terhadap janin. Contoh obat yang masuk kategori ini misalnya antipiretik parasetamol, antibiotika penisilin, isoniazid, glikosida jantung, eritromisin, bahan-bahan hemopoetik seperti besi dan asam folat, dan lain-lain. Kategori B : Obat-obat dimana pengalaman pemakaian oleh wanita hamil atau mampu hamil masih terbatas tetapi tidak ada kenaikan frekuensi malformasi janin atau pengaruh buruk secara langsung maupun tidak langsung terhadap janin. Karena riwayat pengalaman pemakaian pada manusia terbatas, maka kelompok ini terbagi-bagi berdasarkan penemuan-penemuan studi toksikologi pada binatang. B1 : Penelitian pada binatang tidak menunjukkan adanya kenaikan kejadian kerusakan janin (fetal damage ). Misalnya obat-obat simetidin, dipiridamol, spektinomisin. B2 : penelitian pada binatang tidak memadai dan masih kurang, tetapi data yang ada juga tidak menunjukkan peningkatan kejadian kerusakan janin. Sebagai contoh adalah amfoterisin, dopamine, asetil kistein, alkaloid beladona, dan lain-lain. B3 : penelitian pada binatang menunjukkan peningkatan kejadian kerusakan janin , tetspi belum tentu bermakna pada manusia. Contoh karbamasepin, pirimetamin, griseofulvin, trimetoprim, dan mebendazol. Kategori C : obat-obat yang karena efek farmakologiknya dapat menyebabkan pengaruh buruk pada janin tanpa disertai malformasi anatomik. Pengaruk ini kemungkinan dapat membaik kembali ( reversible ). Misalnya fenotiazin, analgetika narkotika, antiinflamasi non steroid, aspirin, rifampisin, antiaritmia, Cachannel blocker, diuretika dan lain-lain. Kategori D : Obat-obat yang telah menyebabkan kenaikan kejadian malformasi janin pada manusia atau menyebabkan menyebabkan kerusakan pada janin yang tidak dapat membaik lagi. ( ireversibel ). Obatobat ini juga mempunyai efek farmakologik yang merugikan terhadap janin . Contoh : Fenitoin, pirimidon, fenobarbiton, valproat, klonasepam, kinine, kaptopril, obat-obat sitotoksik, antikoagulan, androgen, dan steroid anabolic dan lain-lain. Pemakaian pada kehamilan harus dihindari sedapat mungkin. Kategori X : obat-obat yang telah terbukti mempunyai resiko tinggi untuk dipakai pada kehamilan karena pengaruh yang menetap ( ireversibel ) terhadap janin. Kontraindikasi mutlak pada kehamilan atau kemungkinan hamil. Termasuk disini misalnya isotretionin, dan dietilstilbestrol.

OBAT-OBAT TOPIKAL MATA, TELINGA, RONGGA MULUT DAN KULIT

ANTIBIOTIK DAN ANTISEPTIK TOPIKAL MATA No

Nama

1. Ciprofloxacin Kategori C

2.

Levofloxacin Kategori C

3. Kloramphenikol Kategori C

4.

Gentamycin sulfate Kategori D

Mekanisme

Ciprofloxacin is a broad-spectrum antibiotic of the fluoroquinolone class. It is active against both Gram-positive and Gramnegative bacteria. It functions by inhibiting DNA gyrase, and a type II topoisomerase, topoisomerase IV necessary to separate bacterial DNA, thereby inhibiting cell division.

Same as ciprofloxacin

Chloramphenicol is a bacteriostatic by inhibiting protein synthesis. It prevents protein chain elongation by inhibiting the peptidyl transferase activity of the bacterial ribosome

Gentamicin is a bactericidal antibiotic that works by irreversibly binding the 30S subunit of the bacterial ribosome, interrupting protein synthesis.

Dosis obat

Eye drop 0,3%, botol 5ml

Efek samping

Foreign body sensation, gatal

Eye drop 5mg per ml, botol 5ml

Kabur sementara, nyeri mata

Eye drop 0,5%, botol 5 ml

Mata gatal, merah, iritasi sementara

Eye drop 3ml Salepmata 0,3%

Mata merah, gatal, iritasi sementara

Indikasi

Konjuntivitis, ulkus (strepto,staphylococus, H.influenza dan pseudomonas)

Infeksi ocular eksterna bakteri strepto, staphylococus, H.influenza dan pseudomonas

Infeksi ocular eksterna bakteri strepto , staphylococus, H.influenza dan pseudomonas

Infeksi ocular eksterna bakteri strepto , staphylococus, H.influenza dan pseudomonas

5.

Acyclovir Kategori B

acts as a specific inhibitor of herpes virus DNA polymerase

Eye zalf 3%

Mata merah, gatal, iritasi sementara

Pengobatan keratitis ( virus HSV type I-II )

KORTIKOSTEROID TOPIKAL MATA

No

Nama

Mekanisme

Dosis obat

Efek samping

Indikasi

1.

Betamethasone Kategori C

Betamethasone binds to specific intracellular glucocorticoid receptors and subsequently binds to DNA to modify gene expression. The synthesis of certain antiinflammatory proteins is induced while the synthesis of certain inflammatory mediators is inhibited. As a result, there is an overall reduction in chronic inflammation and autoimmune reactions.

Eye drop 0,1%, botol 5ml

Foreign body sensation, gatal, mata merah, peningkatan TIO

Inflamsi, alergi non-infeksi pada mata

2.

Fluorometholone Kategori C

Corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins

Eye drop 1 mg, per ml , botol 5ml

Mata merah, gatal, iritasi sementara, Peningkatan TIO

Inflamsi , alergi palpebra , konjunctiva bulbar, kornea dan segmen anterior mata

3.

Prednisolone asetate Kategori C

The antiinflammatory actions of glucocorticoids are thought to involve

Eye drop 10mg per tube 0,6ml

Mata gatal, merah, iritasi sementara, peningkatan TIO

Inflamsi , alergi palpebra , konjunctiva bulbar, kornea dan segmen anterior mata

phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.

KOMBINASI KORTIKOSTEROID DAN ANTIBIOTIK MATA

No

Nama

1.

2.

1.

Mekanisme

Dosis obat

Efek samping

Betamethasone + Gentamycin

Eye drop gentamycin 0,5% + betamethasone 0,1% (botol 5ml)

Mata merah, gatal, iritasi sementara, peningkatan TIO

Dexamethasone + Tobramycin

Eye drop dexamethasone 1 mg + tobramycin 3mg (botol 5ml)

Mata merah, gatal, iritasi sementara, peningkatan TIO

OBAT

ANTI

GLAUCOMA

Acetazolamide Kategori C

Inactivates carbonic anhydrase and interferes with the sodium pump, which decreases aqueous humor formation and thus lowers IOP. Systemic effects however include increased renal loss of sodium, potassium, and water secondary to the drug’s renal tubular effects.

Tab 250mg

Asidosis metabolik, hipokalemia, gguan hematologi

Indikasi Infeksi eksterna bola mata (bakteri gram postive dan negative)

Infeksi eksterna bola mata (bakteri gram postive dan negative)

Obat karboik anhidrase in hibitor, menurunkan TIO

2. Latanoprost Kategori ( belum tahu)

3.

Timolol Maleate dan Betaxolol Kategori C

Latanoprost is a prostanoid selective FP receptor agonist that is believed to reduce the intraocular pressure (IOP) by increasing the outflow of aqueous humor. Timolol maleate is a beta1 and beta2 (nonselective) adrenergic receptor blocking agent that does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anesthetic (membranestabilizing) activity.

Eye drop 0,005%, botol 2,5ml

Perubahan alis, inflamasi intraokuler, perubahan pigmentasi iris

Analog prostaglandin, menurunkan TIO pasien glaucoma sudut terbuka dan hipertensi okuler

Timolol eye drop 0,25% Betaxolol eye drop 0,5%

Sakit kepala ,mual,pusing, Bradikardi, iritasi mata

Obat beta-blocker, menurunkan TIO pada pasien glaucoma sudut terbuka dan hipertensi okuler

OBAT DEKONGESTAN, ANESTESI DAN ANTI INFLAMASI MATA

No

Nama

1.

Na-diclofenac Kategori C

Mekanisme The primary mechanism responsible for its anti-inflammatory, antipyretic, and analgesic action is thought to be inhibition of prostaglandin synthesis by inhibition of cyclooxygenase (COX). It also appears to exhibit bacteriostatic activity by inhibiting bacterial DNA synthesis

Dosis obat

Efek samping

Eye drop 0,1%, botol 5ml

Rasa tidak nyaman di mata, iritasi mata, peningkatan TIO

Indikasi

Teapi anti-inflamasi post operasi ekstraksi katarak dan operasi kornea

2.

Na-hyaluronate Kategori belum diketahui

functions as a tissue lubricant and is thought to play an important role in modulating the interactions between adjacent tissues. It forms a viscoelastic solution in water.

Eye drop 0,1%, botol 5ml

Mata kering, iritasi mata,mata kabur, gatal

3.

Pemirolast K Kategori belum diketahui

Pemirolast binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine

Eye drop 0,1%, botol 5 ml

Mata gatal, merah, iritasi sementara, discharge pada mata

4.

Tetrakain HCL

Tetracaine is rapidly hydrolyzed by plasma esterases to the following primary metabolites: para-aminobenzoic acid and diethylaminoethanol. The activity of both metabolites is unspecified.

Eye drop 0,5% dalam botol 5ml pantocain 0,5%

Mata merah, nyeri, rasa terbakar

Untuk semua gejala dry eye disease

Terapi konjunctivitis vernal dan alergi

Anestesi lokal rapid untuk prosedur minor cth: ekstraksi benda asing or tonometri

PREPARAT TOPIKAL UNTUK TELINGA

No

Nama

Mekanisme

Dosis obat

Efek samping

Indikasi

1.

Gentamicin Kategori D

Gentamicin is a bactericidal antibiotic that works by irreversibly binding the 30S subunit of the bacterial ribosome, interrupting protein synthesis. This mechanism of action is

Eye drop 3mg per ml, botol 5ml

Iritasi , rasa terbakar, gatal

Infeksi superficial telinga

similar to other aminoglycosides 2.

Ofloxacin Kategori C

3.

Docusate NA

Ofloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase, which allows the untwisting required to replicate one DNA double helix into two

Eye drop 3mg per ml, botol 5ml

Antibiotik untuk infesi telinga pusing sakit kepala

Eye drop 5mg,per botol 10 ml

Mata gatal, merah, iritasi sementara

Terapi topikal antibiotik

Membantu ekstraksi serumen yg mengeras

PREPARAT TOPIKAL UNTUK RONGGA MULUT

No

Nama

Mekanisme

Dosis obat

Efek samping

1.

Dequalinium CL

It disrupts the cell permeability of the bacteria by absorbing onto the bacterial cell surface and diffusing across the membrane. It also binds to the cytoplasmic membrane with subsequent formation of complexes and protein precipitation and lyses the membrane in adequate concentrations, perturbing osmotic exchange

Tab hisap 0,25%

Iritasi lokal

Indikasi

Antiseptik topikal oral, infeksi mulut dan laring

2.

Na Hyaluronate

Sodium hyaluronate functions as a tissue lubricant and is thought to play an important role in modulating the interactions between adjacent tissues. It forms a viscoelastic solution in water

Obat kumur 0,025%, botol 80ml

Rasa kebas mulut

Pencegahan sariawan, gingivitis

3.

Povidone iodine

Povidone iodine is a broad spectrum microbicide that destroys microbial protein and DNA. It has excellent in vitro antimicrobial activity and is indicated for preoperative preparation of the periocular region and irrigating the ocular surface

Obat kumur 1%, botol 200ml

Rasa kebas mulut

Antiseptik lokal untuk terapi tambahan infeksi dan inflamsi rongga mulut dan tenggorokan

Hexetidine is a bactericidal and fungicidal antiseptic w/ a broad spectrum antimicrobial activity against gm +ve and gm ve bacteria, yeasts (e.g. Candida albicans) and fungi.

Obat kumur 0,1%

Rasa kebas dimulut

Antiseptik lokal untuk terapi tambahan infeksi, inflamasi rongga mulut

The antiinflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins which, through inhibition of

Pasta oral base 0,1%, tube 5gr

Rasa berminyak, rasa kering dan kasar, atrofi mukosa oral

4.

5.

Hexetidine

Triamcinolone acetonide Kategori C

Terapi adjuvant untuk lesi inflamasi oral dan lesi ulserasi di rongga mulut

arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes.

ANTIBIOTIK TOPIKAL KULIT

No

Nama

Mekanisme

Dosis obat

Efek samping

Indikasi

1.

Fusidic acid

Elongation factor G (EF-G) is a bacterial protein that is necessary for translocation on the bacterial ribosome after peptide bond formation during protein synthesis. Fusidic acid binds to this protein and the ribosome thereby inhibiting further bacterial protein synthesis

Salep 2% tube 5/10/15gr

Iritasi kulit ringan

Antibiotik topikal Infeksi kulit yg disebabkn oleh bacteri Staphy dan strepto

2.

Silver sulfadiazin Kategori B

Silver sulfadiazine acts only on the cell membrane and cell wall to produce its bactericidal effect. Silver sulfadiazine's effectiveness may possibly be from a synergistic interaction, or the action of each component.

Krim 1%, tube 35gr

Perubahan warna pada kulit , rasa terbakar

Antibiotik topikal untuk terapi wound sepsis pd pasien luka bakar

3.

Muporicin Kategori B

Mupirocin apparently exerts its antimicrobial activity by reversibly inhibiting isoleucyl-transfer RNA, thereby

Krim 2%, tube 5gr

Iritasi lokal,sakit kepala

Antibiotik topikal Infeksi kulit yg disebabkn oleh bacteri Staphy dan strepto

inhibiting bacterial protein and RNA synthesis. Mupirocin has excellent in vitro activity against staphylococci and most streptococci but less activity against other gram-positive and gram-negative bacteria. 4.

Clindamycin Kategori B

Clindamycin has a primarily bacteriostatic effect. It is a bacterial protein synthesis inhibitor by inhibiting ribosomal translocation, in a similar way to macrolides.

Topikal gel 1% tube 10gr

Rasa terbakar, gatal , kulit kering, iritasi lokal

5.

Azelaic acid Kategori B

azelaic acid manifests its antibacterial effects by inhibiting the synthesis of cellular protein in anaerobic and aerobic bacteria, especially Staphylococcus epidermidis and Propionibacterium acnes

Krim 20% tube 10 gr

Rasa terbakar, gatal , kulit kering, iritasi lokal

Antibiotik topikal untuk penanganan acne

Krim topikal kulit untuk penanganan acne

ANTI-JAMUR TOPIKAL KULIT

No

Nama

Mekanisme

Dosis obat

Efek samping

Indikasi

1.

Miconazole Kategori C

Miconazole interacts with 14α demethylase, a cytochrome P-450 enzyme necessary to convert

Krim 2% (tube 5/10/15/20 gr)

Iritasi , rasa terbakar kadangkadang

Infeksi kulit dan kuku yg disebabkan oleh oleh dermatifa, yeast dan jamur lain

lanosterol to ergosterol. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents 2.

Ketokonazole Ketegori C

Ketoconazole is an imidazole antimycotic. Its fungistatic effect is based primarily on enzyme inhibition due to a bond with the cytochrome P450. It thus inhibits, amongst others, biosynthesis of ergosterol and thereby alters the permeability of the fungal cell membranes.

Krim 2% tube 5gr

Iritasi lokal, gatal,nyeri

Infeksi jamur dermatofita dan non-dermatofita ( tinea, dermatitis soboroik, tinea vesikolor

3.

Ciclopirox Kategori B

ciclopirox act through the chelation of polyvalent metal cations, such as Fe3+ and Al3+. These cations inhibit many enzymes, including cytochromes, thus disrupting cellular activities such as mitochondrial electron transport processes and energy production.

Krim 1% tube 10gr

Iritasi lokal, gatal,nyeri

Infeksi jamur pada kuku terutama yg disebabkan oleh TRICHOPHYTON RUMBRUM

4.

Terbinafine HCL

Terbinafine is hypothesized to act by inhibiting

Krim 1% tube 10gr

Iritasi lokal, gatal,nyeri

Infeksi jamur dermatofita dan non-dermatofita ( tinea, dermatitis soboroik,

squalene monooxygenase, thus blocking the biosynthesis of ergosterol, an essential component of fungal cell membranes. 5.

Clotrimazole Kategori B

clotrimazole interferes in the lipid synthesis of fungi and thus causes an alteration of the permeability of the cell walls. Especially when high doses are applied

tinea vesikolor

Krim 1% tube 5gr

Iritasi lokal, gatal, nyeri

Infeksi jamur dermatofita dan non-dermatofita ( tinea, dermatitis soboroik, tinea vesikolor)

KORTIKOSTEROID TOPIKAL KULIT

No

Nama

Mekanisme

Dosis obat

Efek samping

Indikasi

1.

Hydrocortisone Kategori C, Kategori D untuk trims 1

Hydrocortisone binds to the cytosolic glucocorticoid receptor. After binding the receptor the newly formed receptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements (GRE) in the promoter region of the target genes.

Krim 1% tube 5gr Krim 2,5% tube 10gr

Iritasi lokal,gatal, nyeri, kering

Inflamsi kulit, gejala pruritus pada kulit yg responsif terhdp kortikosteroid topikal

2.

Betamethasone Kategori C Kategori D untuk trims 1

Betamethasone is a glucocorticoid receptor agonist. This leads to changes in

Krim 0,05% tube 5gr

Iritasi lokal,gatal, nyeri, kering

Inflamsi kulit, gejala pruritus pada kulit yg responsif terhdp kortikosteroid topikal pd pasien 13thn dan keats

genetic expression once this complex binds to the GRE. 3.

Desoximethasone Kategori C

desoximetasone has antiinflammatory, antipruritic, and vasoconstrictive properties. Mechanism of the antiinflammatory activity of topical steroids in the treatment of steroidresponsive dermatoses, in general, is uncertain. However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins.

Krim 0,25% tube 5gr

Rasa terbakar,gatal, iritasi lokal, kering

Inflamsi kulit, gejala pruritus pada kulit yg responsif terhdp kortikosteroid topikal

4.

Clobetasol Propionate Kategori C

clobetasol propionate has antiinflammatory, antipruritic, and vasoconstrictive properties. The mechanism of the anti-inflammatory activity of the topical steroids, in general, is unclear. However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins.

Krim 0,05% tube 5gr

Rasa terbakar,gatal, iritasi lokal,kering

Kortikosteroid topikal super-high potent, terapi untuk inflamasi dan gejala pruritus pd kulit yg responsif pada kortikosteroid