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OCULAR PHARMACOLOGY Dr. Jamshed Ahmed Assistant Professor Ophthalmology Unit-II Dow Medical college & Civil Hospital Karachi MEANS OF OCULAR DRUGS ADMINISTRATION EYE DROPS ONITMENTS PERIOCULAR INJECTIONS INTRACAMERAL INTRAVITREAL INJECTIONS SUSTAINED RELEASE PREPARATIONS SYSTEMIC THERAPY INTRAVENOUS INJECTIONS METHODS OF OCULAR DRUG DESIGN AND DELIVERY PRO - DRUGS SUSTAINED RELEASE DEVICES AND GELS COLLAGEN CORNEA SHIELDS LOCAL ANESTHETIC DRUGS Classification 1) Esters a) Esters of benzoic acid Cocaine (topical only) Butacain Benzocaine (topical only) Piperocaine b) Esters of paba 2-Chloroprocaine (Nesacaine) Procaine (Novocain) c) Esters Of Meta Amino Benzoic Acid Propoxycaine (Ravocaine) Butethamine Tetracaine (Pontocaine) Lidocaine (Xylocaine) Bupivacaine Mepivacaine (Carbocaine) Dibucaine 2) Quinolones Centbundine LOCAL ANESTHETICS Topical: Propacaine, Tetracaine. Uses : Applanation tonometry A goniscopy, Aremoval 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 Local Anesthetics Infiltration Anaesthesia Peribulbar. Retrobulbar. Sub tenon. Cause anesthesia and akinesia for intraocular surgery e.g. Lidocaine. bupivacaine Ocular Lubricants Ocular Lubricants Indication ocular irritations in various diseases Dry eyes Commonly available commercial tear substitutes: Systane eye Drops Lacri-Lube Genteal eye drops OCULAR PHARMACOTHERAPEUTICS AUTONOMIC NERVOUS SYSTEM PARASYMPATHETIC (CHOLINERGIC) SYMPATHETIC (ADRENERGIC) PARASYMPATHETIC (CHOLINERGIC) SYSTEM DRUGS AFFECTING THE PARASYMPATHETIC SYSTEM MAY BE: CHOLINERGIC STIMULATING (AGONIST) CHOLINERGIC BLOCKING (ANTAGONIST) ACETYLECHOLINE IS THE NEUROTRANSMITTER THAT STIMULATES TWO MAJOR TYPES OF CHOLINERGIC RECEPTORS: NICOTINIC(LOCATED PREDOMINANTLY IN MOTOR ENDPLATES OF SKELETAL MUSCLES MUSCARINIC(SMOOTH & CARDIAC MUSCLES) CHOLINERGIC STIMULATING DRUGS (AGONIST) DIRECT ACTING CHOLINERGIC DRUG PILOCARPINE CARBACHOL INDIRECTLY ACTING MUSCARINIC AGENTS CHOLINESTERASE INHIBITORS (SAME AS DIRECTLY ACTING CHOLINERGIC AGENTS BUT HAVE LONGER DURATION OF ACTION) TWO CLASSES: • • REVERSIBLE INHIBITORS e.g PHYSOSTIGMINE IRREVERSIBLE INHIBITORS e.g ECOTHIOPHATE DIRECTLY ACTING CHOLINERGIC DRUGS PILOCARPINE ACTIONS: LIKE ACETYLECHOLINE ACTS DIRECTLY ON SMOOTH MUSCLES STIMULATES THE SPHINCTER PUPILLAE MUSCLE (MIOSIS) STIMULATES THE CIRCULAR CILIARY MUSCLE (ACCOMMODATION) STIMULATES THE LONGITUDINAL CILIARY MUSCLE (INCREASES OUT FLOW OF AQUEOUS HUMOR THROUGH TRABECULAR MESHWORK) PILOCARPINE CONT…. PREPARATION & DOSAGE: 1%, 2%, 3%, 4% USED q.I.d AS MONOTHERAPY OR IN COMBINATION WITH BETA-BLOCKER b.d ADMINISTRATION PILOCARPINE GEL (PILOCARPINE ADSORBED ON TO A PLASTIC GEL). ONCE DAILY AT BED TIME ( SO THAT INDUCED MYOPIA AND MIOSIS LAST ONLY DURING SLEEP) INDICATIONS: PRIMARY OPEN ANGLE GLAUCOMA. DECREASE IOP BY INCREASING OUT FLOW FACILITY PRIMARY CLOSED ANGLE GLAUCOMA. RESULTANT MIOSIS PULLS THE PERIPHERAL IRIS AWAY FROM THE TRABECULUM, THUS OPENING THE ANGLE ACCOMMODATIVE ESOTROPIA PILOCARPINE CONT….. OCULAR SIDE EFFECTS: MIOSIS CATARACTOGENESIS BROW ACHE MYOPIA SHIFT EXACERBATION OF SYSPTOMS OF CATARACT VISUAL PROBLEM IN DIM ILLUMINATION INCREASE INCIDENCE OF RETINAL DETACHMENT SYSTEMIC SIDE EFFECTS: CHOLINERGIC BLOCKING DRUGS (ANTAGONIST) THE MUSCARINIC ACTIONS OF CHOLINERGIC DRUGS ARE ANTAGONIZED BY ATROPINE GROUP OF DRUGS. MEMBERS OF ATROPINE GROUP ARE: ATROPINE HOMATROPINE CYCLOPENTOLATE TROPICAMIDE ATROPINE ACTIONS: DILATATION OF THE PUPIL CYCLOPLEGIA STABILIZES THE BLOOD AQUEOUS BARRIERS DURATION OF ACTION 7-14 DAYS INDICATIONS: CYCLOPLEGIC IN IRIDOCYCLITIS / KERATITIS REFRACTION IN CHILDREN CILIARY BLOCK & RUBEOTIC GLAUCOMA SIDE EFFECTS: SYSTEMIC ABSORPTION ESPECIALLY IN CHILDREN MAY LEAD TO: • FLUSHING, FEVER, TACHYCARDIA & DELIRIUM.PRECIPITATION OF ANGLE CLOSURE GLAUCOMA, MALIGNANT HYPERTHERMIA ATROPINE GROUP OF DRUGS CONT. OTHER DRUGS: HOMATROPINE: • 2 - 5% , ONSET OF ACTION 30 - 60 MIN, DURATION CYCLOPENTOLATE: • 03 DAYS 0.5 - 1%, ONSET OF ACTION 20 - 40 MIN, DURATION 02 DAYS TROPICAMIDE: • 0.5% - 1%, ONSET OF ACTION 20 - 40 MIN, DURATION 4 - 6 HRS SYMPATHETIC (ADRENERGIC) SYSTEM ADRENERGIC NEURONS SECRETE NORADRENALINE AT SYMPATHETIC POST-GANGLIONIC NERVE ENDINGS FOUR MAIN TYPE OF ADRENERGIC RECEPTORS: ALPHA - 1 • • ARTERIOLES, DILATOR PUPILLAE & MULLER MUSCLE STIMULATION- HYPERTION, MYDRIASIS, LID RETRACTION ALPHA - 2 • • INHIBITORY RECEPTORS, ON CILIARY EPITHELIUM STIMULATION - DECREASE AQUEOUS SECRETION UVEOSCLERAL OUT FLOW BETA - 1 PRESENT ON CARDIAC MUSCLES BETA - 2 & INCREASE • • • PRESENT ON BRONCHIAL & CILIARY EPITHELIUM STIMULATION - BRONCHIAL DILATATION, INCREASE AQUEOUS PRODUCTION DIRECT ACTING ALPHA 1 ADRENERGIC AGENTS PHENYLEPHRINE: PREPARATION • 2.5%, 10% EYE DROPS INDICATION • PRIMARY CLINICAL USE IS STIMULATION OF IRIS DILATOR MUSCLE TO PRODUCE MYDRIASIS SIDE EFFECTS • SYSTEMIC ABSORPTION MAY ELEVATE BLOOD PRESSURE ALPHA 2 ADRENERGIC AGONIST BRIMONIDINE 2% b.d ACTION: • DECREASE IOP BY BOTH DECREASING AQUEOUS SECRETION AND ENHANCING UVEOSCLERAL OUTFLOW INDICATION: • OPEN ANGLE GLAUCOMA SIDE EFFECTS: • OCULAR S/E IS ALLERGIC CONJUNCTIVITIS. SYSTEMIC S/E INCLUDE XEROSTOMIA, DROWSINESS AND FATIGUE. APRACLONIDINE ACTION: • SIMILAR TO BRIMONIDINE. NOT SUITABLE FOR LONG-TERM USE B / C OF TACHYPHYLAXIS. INDICATION; • AFTER LASER SURGERY ON THE ANTERIOR SEGMENT TO OFFSET AN ACUTE RISE IN IOP. BETA- ADRENERGIC ANTAGONISTS (BETA BLOCKERS) • THESE AGENTS LOWER IOP BY REDUCING AQUEOUS HUMOR PRODUCTION AS MUCH AS 50%. • NONSELECTIVE BETA 1 & BETA 2 ANTAGONIST – TIMOLOL MALEATE 0.25% - 0.5% b.d • OCULAR S/E ALLERGY, CORNEAL PUNCTATE EPITHELIAL EROSIONS AND REDUCED AQUEOUS TEAR SECRETION. • SYSTEMIC S/E BRADYCARDIA & – – – HYPOTENSION FROM BETA 1 BLOCKADE. (CONTRINDICATED CONGESTIVE CARDIAC FAILURE). BRONCHOSPASM MAY BE INDUCED BY BETA 2 BLOCKADE. LEVOBUNOLOL 0.5% ONCE DAILY CARTEOLOL 1%-2% b.d METIPRANOLOL YDROCHLORIDE 0.1%, 0.3% b.d. CARDIOSELECTIVE BETA 1 ANTAGONIST – BETOXOLOL 0.5% • INDICATIONS: – REDUCTION OF IOP IN ALL TYPES OF GLAUCOMA. CARBONIC ANHYDRASE INHIBITORS THESE AGENTS LOWER IOP BY INHIBITING CILIARY BODY CARBONIC ANHYDRASE. TOPICAL AGENTS DORZOLAMIDE 2% t id BRINZOLAMIDE 1% t id OCULAR SIDE EFFECTS: • ALLERGIC CONJUNCTIVITIS CARBONIC ANHYDRASE INHIBITORS CONT. SYSTEMIC AGENTS (useful as short-term treatment) ORAL • PREPARATIONS: • ACETAZOLAMIDE TABLETS • 250mg dose is 250-1000mg • onset of action is within 1 hour, with a peak at 4 hours and a duration up to 12 hours. PARENTAL • I/V INJECTION 500mg ACETAZOLAMIDE • onset of action with in 15-20 minutes. SIDE EFFECTS: • COMMON: – PARAESTHESIAE – MALAISE COMPLEX • UNCOMMON: – GASTROINTESTINAL COMPLEX – RENAL STONE FORMATION – STEVENS - JOHNSON SYNDROME – BLOOD DYSCRASIAS HYPEROSMOTIC AGENTS ACTION INCREASED SERUM OSMOLARITY REDUCES IOP AND VITREOUS VOLUME BY DRAWING FLUID OUT OF THE EYE ACROSS VASCULAR BARRIERS. AGENTS INTRAVENOUS • MANITOL 1g / kg body weight or 5ml / kg body weight. Peak action is achieved in 30 minutes, with a duration of up to 6 hours. • UREA ORAL • GLYCEROL + lemon juice 1g / kg body weight or 2ml / kg body weight. Peak action with in 1 hour, with a duration up to 3 hours. • ISOSORBIDE (non-metabolized sugar) USES (used with care in patients with compromised heart) SHORT-TERM MANAGEMENT OF ACUTE GLAUCOMAS REDUCING VITREOUS VOLUME PRIOR TO CATARACT SURGERY PROSTAGLANDIN ANALOGUES REDUCE IOP BY ENHANCING UVEOSCLERAL OUTFLOW. AGENTS LATANOPROST 0.005% ONCE DAILY • OCULAR SIDE EFFECTS: – CONJUNCTIVAL HYPERAEMIA. – EYELASH LENGTHENING & HYPERPIGMENTATION OF IRIS, LASHES, AND PERIORBITAL SKIN. • SYSTEMIC SIDE EFFECTS: – OCCASIONAL HEADACHE AND UPPER REPIRATORY SYSPTOMS. TRAVOPROST .004% SIMILAR TO LATANOPROST BIMATOPROST 0.3% UVOSCLERAL OUTFLOW + TRABECULAR OUTFLOW. UNOPROSTONE ISOPROPYL 0.15%, b.d. GLUCOCORTICOIDS ACTION: INHIBITION OF ARACHIDONIC ACID RELEASE FROM PHOSPHOLIPIDS AGENTS DEXAMETHASONE 0.1% PREDNISOLONE ACETATE 0.1% FLUOROMETHALONE ACETATE 0.1% TOPICAL TO PREVENT OR SUPRESS CORNEAL GRAFT REJECTION ANT: CHAMBER REACTION AFTER ANT: SEGMENT SURGERY FILTERATION BLEB SCARING IMMUNE OR TRUMATIC IRITIS & UVITIS GLUCOCORTICOIDS SUBCONJUNCTIVAL, ANT & POST SUBTENON INJECTION (Triamcinolone acetonide or methylprednisolone acetate) SEVERE OCULAR INFLAMMATION INTRAVITREAL INJECTION (Triamcinolone acetonide 2mg in 0.05ml) ENDOPHTHALMITIS GLUCOCORTICOIDS SAYSTEMIC THERAPY ORAL 1mg / kg per day • • GIANT CELL ARTERITIS SEVERE OCULAR INFLAMMATIONS INTRAVENOUS • OPTIC NEURITIS GLUCOCORTICOIDS CONT…. ADVERSE EFFECTS OCULAR • GLAUCOMA • POSTERIOR SUBCAPSULAR CATARACTS • EXACERBATION OF BACTERIAL & VIRAL INFECTIONS • PTOSIS • MYDRIASIS • SCLERAL MELTING • EYE SKIN ATROPHY SYSTEMIC • SUPPRESSION OF THE PITUITARY-ADRENAL AXIS • GLUCONEOGENESIS RESULTING FROM • • • • • HYPERGLYCEMIA ASEPTIC NECROSIS OF HIP PEPTIC ULCER DIABETES INSOMNIA REDISTRIBUTION OF FAT FROM THE PERIPHERY TO THE TRUNK ANTIBIOTICS ANTIBACTERIALS PENICILLINS AND CEPHALOSPORINS SULPHONAMIDES TETRACYCLINES CHLORAMPHENICOL AMINOGLYCOSIDES FLUOROQUINOLONES MISCELLANEOUS ANTIBIOTICS • VANCOMYCIN • ERYTHROMYCIN • POLYMYXIN B • BACITRACIN ANTIFUNGAL AGENTS POLYENES IMIDAZOLES FLUCYTOSINE ANTIVIRAL AGENTS TOPICAL ANTIVIRAL AGENTS SYSTEMIC ANTIVIRAL AGENTS PENICILLINS AND CEPHALOSPORINS BETA-LACTUM CONTAINING ANTIBACTERIAL AGENTS BACTERIAL SUSCEPTIBILITY PATTERNS AND RESISTANCE TO BETA-LACTAMSES HAVE DETERMINED THE CLASSIFICATION OF THE CEPHALOSPORINS AS: FIRST GENERATION(activity against gram+ & gram- organisms) • CEPHALEXIN • CEFAZOLINE (fortified topical drops 50mg/ml in bacterial keratitis) SECOND- GENERATION • CEFOXITIN • CEFUROXIME THIRD-GENERATION • CEFOTAXIME – SYSTEMIC (1g I/V b.d IN GONOCOCCAL KERATOCONJUNCTIVITIS) – TOPICAL ( 50 mg/ml for gram -ve coverage in keratitis and endophthalmitis) – INTRAVITREAL( 2mg in 0.1 ml in endophthalmitis) SULPHONAMIDES SULPHONAMIDES ARE ONLY BACTERIOSTATIC AGENTS SUSCEPTIBLE ORGANISMS INCLUDE STREPTOCOCCUS PNEUMONIAE, CORYNEBACTERIUM DIPHTHERIAE, H INFLUENZAE, ACTINOMYCES AND CHLAMYDIA TRACHOMATIS. SULPHACETAMIDE OPHTHALMIC SOLUTION 10% -30% USED IN BACTERIAL CONJUNCTIVITIS COMMON SIDE EFFECTS LOCAL IRRITATION ITCHING PERIORBITAL EDEMA TRANSIENT STINGING TETRACYCLINS BROAD-SPECTRUM BACTERIOSTATIC ANTIBIOTICS SYSTEMIC THERAPY USED FOR CHLAMYDIAL INFECTIONS STAPHYLOCOCCAL INFECTIONS OF THE MEIBOMIAN GLANDS TOPICAL THERAPY IN THE FORM OF ONITMNT FOR LOCAL APPLICATION AT THE LID MARGINS IN BLEPHRITIS PRECAUTIONS SHOULD NOT BE GIVEN TO CHILDREN AND PREGNANT WOMENS, BECAUSE IT CAN BE DEPOSITED IN GROWING TEETH, DISCOLOURING THEM. CHLORAMPHENICOL BROAD-SPECTRUM BACTERIOSTATIC AGENTS TOPICAL THERAPY DROPS 0.5% ONITMENTS USES BACTERIAL CONJUNCTIVITIS POSTOPERATIVELY AFTER ANTERIOR SEGMENT SURGERY AMINOGLYCOSIDES BACTERIOCIDAL AGENTS HAVE ACTIVITY AGAINST AEROBIC GRAM NEGATIVE BACILLI INCLUDE: GENTAMICIN • TOPICAL (CONJUNCTIVITIS) – DROPS 0.3% – FORTIFIED DROPS 15mg / ml (1.5%) – ONITMENT0.3% • PERIOCULAR INJECTION (KERATITUS) – 20 mg TOBRAMYCIN • TOPICAL – DROPS 0.3% – FORTIFIED DROPS – ONITMENT 0.3% • USES – CONJUNCTIVITIS/ KERATITIS/ ENDOPHTHALMITIS AMIKACIN • TOPICAL – FORTIFIED DROPS 10mg / ml (KERATITIS/ ENDOPHTHALMITIS) • INTRAVITREAL INJECTION 0.4mg in 0.1ml • USES: – ENDOPHTHALMITIS FLUOROQUINOLONES HIGHLY EFFECTIVE BROAD-SPECTRUM ANTIMICROBIALS AGENTS NORFLOXACIN 0.3% solution. (Conjunctivitis / keratitis) OFLOXACIN 0.3% solution (Conjunctivitis / keratitis) CIPROFLOXACIN 0.3% solution (Conjunctivitis / keratitis ) GATEFLOXACIN MOXI FLOXACIN MISCELLANEOUS ANTIBIOTICS VACOMYCIN BACTERICIDAL FOR MOST GRAM-POSITIVE ORGANISMS PREPARATIONS • DROPS 50mg/ ml infectious keratitis • PERIOCULAR INJECTIONS 25 mg endophthalmitis • INTRVITREAL INJECTIONS 1mg in 0.1 ml endophthalmitis POLYMYXIN (bactericidal) BACITRACIN (inhibits bacterial cell wall synthesis) FUSIDIC ACID (effective against gram +ve organisms) ANTIFUNGAL AGENTS POLYENES ARE TOPICALLY ACTIVE AGAINST A VARIETY OF FILAMENTOUS FUNGI, INCLUDING ASPERGILLUS, FUSARIUM. AGENTS: NATAMYCIN 5% suspension AMPHOTERICIN B reconstituted at 0.25%-0.5% in sterile water IMIDAZOLES MICONAZOLE 1% solution applied topically KETOKONAZOLE 200mg tab for oral therapy in fungal keratitis FLUCYTOSINE oral therapy 50-150mg/kg daily in divided doses. ANTIVIRAL AGENTS TOPICAL ANTIVIRAL AGENTS ACICLOVIR • 3% ONITMENT USED 5 TIMES DAILY IN KERATITIS. GANCICLOVIR • 0.15% GEL USED 5 TIMES DAILY TRIFLUOROTHYMIDINE • 1% DROPS USED EVERY 2 HOURS SYSTEMIC ANTIVIRAL AGENTS (ACUTE HERPES ZOSTER) ACYCLOVIR • 600 mg 5 TIMES A DAY FAMCICLOVIR • 500mg THREE TIMES A DAY THANK YOU