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Common name
Fotil (pilocarpine and timolol)
Description
Fotil is used for the treatment of several types of glaucoma to lower intra ocular pressure after ophthalmic surgery, to treat glaucoma after cataract surgery and to lower elevated intra ocular pressure in patients for whom mono therapy is not sufficient.
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Active Ingredients:
pilocarpine and timolol
Therapeutic actions:
Timolol is a nonselective beta-adrenergic receptor blocking agent that does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anesthetic (membrane-stabilizing) activity.
Timolol combines reversibly with a part of the cell membrane, the beta-adrenergic receptor, and thus inhibits the usual biologic response that would occur with stimulation of that receptor. This specific competitive antagonism blocks stimulation of the beta-adrenergic receptors by catecholamines having beta-adrenergic stimulating (agonist) activity, whether these originate from an endogenous or exogenous source. Reversal of this blockade can be accomplished by increasing the concentration of the agonist, which will restore the usual biologic response. Pilocarpine is a parasympathomimetic that directly stimulates cholinergic receptors. It produces contraction of the iris sphincter muscle, resulting in pupillary constriction (miosis); constriction of the ciliary muscle (resulting in increased accommodation) and a reduction in intraocular pressure associated with decreased resistance of aqueous humor outflow. Pilocarpine may also inhibit aqueous humor secretion. Each of the two components decreases elevated intraocular pressure (IOP) by different but complementary mechanisms. Timolol lowers IOP primarily by reducing aqueous humor production. Pilocarpine lowers IOP primarily by enhancing the outflow of aqueous humor from the anterior chamber of the eye. Although pilocarpine, given alone requires administration 4 times a day, it has been shown that when formulated with timolol in Fotil, administration twice daily is adequate.
What is it used for?:
(Indications:)
For the reduction of elevated intraocular pressure in patients whose IOP is not adequately controlled on monotherapy with a beta-adrenergic receptor blocking agent or pilocarpine or when concomitant therapy is appropriate.
Contraindications and cautions:
Bronchospasm, including bronchial asthma, or a history of these conditions, or chronic obstructive pulmonary disease.:Sinus bradycardia, second and third degree atrioventricular block, overt congestive cardiac failure, cardiogenic shock.
Conditions in which miosis is undesirable: malignant glaucoma, peripheral anterior synechia, trauma, acute-inflammatory disease of anterior chamber, glaucoma occurring or persisting after extracapsular cataract extraction when posterior synechia may occur, etc. Hypersensitivity to any component of this product.
Warnings in Clinical States: As with other topically applied ophthalmic drugs, this drug may be absorbed systemically. The same adverse reactions found with systemic administration of beta-adrenergic blocking agents may occur with topical administration. Fotil should be used with caution in patients with diabetes, especially labile diabetes (see Precautions). Following administration of timolol ophthalmic solution, severe respiratory reactions and cardiac reactions have been reported, including death due to bronchospasm in patients with asthma, and rarely death in association with cardiac failure.
Precautions:
Cardiovascular Function: Cardiac failure should be controlled before beginning therapy with Fotil. In patients with a history of cardiac disease, signs of cardiac failure should be watched for and pulse rate should be checked. Because of potential effects of beta-adrenergic blocking agents relative to blood pressure and pulse, these agents should be used with caution in patients with cerebrovascular insufficiency. If signs or symptoms suggesting reduced cerebral blood flow develop following initiation of therapy with Fotil, alternative therapy should be considered. Eye Accommodation: Miosis usually causes difficulty in dark adaptation. Caution should be exercised in night driving and other hazardous activities in poor illumination. Choroidal Detachment: Choroidal detachment has been reported with administration of aqueous suppressant therapy (e.g., timolol, acetazolamide or combination) after filtration procedures. Management of eyes with chronic or recurrent choroidal detachment should include stopping all forms of aqueous suppressant therapy and treating endogenous inflammation vigorously.
Contact Lenses: Fotil contains the preservative benzalkonium chloride which may be deposited in soft contact lenses; therefore, Fotil should not be used while wearing these lenses. The lenses should be removed before application of the drops and not be reinserted earlier than 15 minutes after use. Risk from Anaphylactic Reaction: While taking beta-blockers, patients with a history of atopy or a history of severe anaphylactic reaction to a variety of allergens may be more reactive to repeated challenge with such allergens, either accidental, diagnostic, or therapeutic. These patients may be more resistant to treatment of anaphylactic reactions with the usual doses of epinephrine since timolol may blunt the beta agonist effect of epinephrine. In such cases, alternatives to epinephrine should be considered. Major Surgery: The necessity or desirability of withdrawal of beta-adrenergic blocking agents prior to major surgery is controversial. If necessary during surgery, the effects of beta-adrenergic blocking agents may be reversed by sufficient doses of such agonists as isoproterenol, dopamine, dobutamine or norepinephrine.
Diabetes Mellitus: Beta-adrenergic blocking agents should be administered with caution in patients subject to spontaneous hypoglycemia or to diabetic patients (especially those with labile diabetes) who are receiving insulin or oral hypoglycemic agents. Beta-adrenergic receptor blocking agents may mask the signs and symptoms of acute hypoglycemia.
Thyrotoxicosis: Beta-adrenergic blocking agents may mask certain clinical signs of hyperthyroidism (e.g., tachycardia). Patients suspected of developing thyrotoxicosis should be managed carefully to avoid abrupt withdrawal of beta-adrenergic blocking agents which might precipitate a thyroid storm.
Muscle Weakness: Beta-adrenergic blockage has been reported to increase muscle weakness consistent with certain myasthenic symptoms (e.g., diplopia, ptosis and generalized weakness). Timolol has been reported rarely to increase muscle weakness in some patients with myasthenic symptoms. Pregnancy: Fotil has not been studied in human pregnancy. The use of Fotil in pregnancy requires that the anticipated benefit be weighed against potential hazards. The use of systemic beta-blockers is not recommended during pregnancy.
Lactation: Timolol is detectable in human milk. Because of the potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Children: Safety and effectiveness in children have not been established.
Side effects:
Fotil is generally well tolerated.
In clinical studies the adverse experiences reported were mainly well-known pilocarpine side effects: blurring of vision, difficulty with dark adaptation, headache/brow-ache and ocular irritation (see below).
Potential Side Effects: Side effects reported in clinical and post-marketing experience with Timoptic, systemic Blocadren, other timolol maleate formulations and pilocarpine ophthalmic solution may be considered potential side effects of Fotil Ophthalmic Solution. Timolol Maleate Ophthalmic
Solution: The following adverse reactions have been reported with ocular administration of this or other timolol maleate formulation, either in clinical trials or since the drug has been marketed.
Special Senses: signs and symptoms of ocular irritation, including burning and stinging, conjunctivitis, blepharitis, keratitis, decreased corneal sensitivity and dry eyes. Visual Disturbances: including diplopia, ptosis, choroidal detachment following filtration surgery (see Precautions). Tinnitus.
Cardiovascular: Aggravation or precipitation of certain cardiovascular pulmonary and other disorders presumably related to effects of systemic beta blockade has been reported (see Contraindications and Precautions). These include bradycardia, arrhythmia, hypotension, syncope, heart block, cerebrovascular accident, cerebral ischemia, palpitation, cardiac arrest, edema, claudication, Raynaud's phenomenon, cold hands and feet. Congestive heart failure and, in insulin-dependent diabetics, masked symptoms of hypoglycemia have been reported rarely. In clinical trials, slight reduction of the resting heart rate in some patients (mean reduction 2.9 beats/minute, standard deviation 10.2) has been observed. Respiratory: bronchospasm (predominantly in patients with pre-existing bronchospastic disease), respiratory failure, dyspnea, cough.
Miscellaneous: headache, asthenia, fatigue, chest pain.
Integumentary: alopecia, psoriasiform rash or exacerbation of psoriasis.
Hypersensitivity: signs and symptoms of allergic reactions including angioedema, urticaria, localized and generalized rash.
Nervous System/Psychiatric: dizziness, depression, increase in signs and symptoms of myasthenia gravis, insomnia, nightmares, memory loss, paresthesia. Digestive: nausea, diarrhea, dyspepsia, dry mouth.
Urogenital: decreased libido,
Peyronie's disease: systemic lupus erythematous. Timolol-Systemic: Side effects reported in clinical experience with systemic timolol maleate may be considered potential side effects of ophthalmic solution Fotil.
Clinical Laboratory Tests: Clinically important changes in standard laboratory parameters were rarely associated with the administration of systemic timolol maleate. Slight increases in blood urea nitrogen, serum potassium and serum uric acid and triglycerides, and slight decreases in hemoglobin and hematocrit and HDL-cholesterol occurred, but were not progressive or associated with clinical manifestations. Pilocarpine HCl Ophthalmic
Solution: Ocular: ciliary spasm, conjunctival vascular congestion, lacrimation, temporal or supra-orbital headache, induced myopia, reduced visual acuity in poor illumination (especially in the elderly and in patients with lens opacities), retinal detachment (especially in young myopic patients).
Lens opacity may occur with prolonged use of pilocarpine.
Systemic: Extremely rare, but have included hypertension, tachycardia, bronchospasm, pulmonary edema, salivation, sweating, nausea, vomiting and diarrhea.
Interactions:
The use of 2 topical beta-adrenergic blocking agents is not recommended. Beta-adrenergic Blockers: Patients already receiving a beta-blocker systemically and who are given Fotil should be observed for a potential additive effect on the intraocular pressure or on the known systemic effects of beta-blockers (hypotension and/or bradycardia). The concomitant use of 2 topical beta-adrenergic blocking agents is not recommended. Calcium Channel Blockers or Catecholamine-depleting Drugs: Calcium blockers or catecholamine-depleting drugs, such as reserpine, may produce additive effects, hypotension and/or marked bradycardia, with possible vertigo, syncope or postural hypotension. I.V. calcium blockers should be used with caution in patients receiving beta-blockers.
Quinidine: Potentiated systemic beta-blockage (e.g., decreased heart rate) has been reported during combined treatment with quinidine and timolol, possibly because quinidine inhibits the metabolism of timolol via the P450 enzyme, CYP2D6.
Information to Be Provided to the Patient: Patients should be instructed to avoid allowing the tip of the dispensing container to contact the eye or surrounding structures. Ocular solutions, if handled improperly, can become contaminated by common bacteria known to cause ocular infections.
Serious damage to the eye and subsequent loss of vision may result from using contaminated solutions. Patients should also be advised that if they develop an inter current ocular condition (e.g., trauma, ocular surgery or infection), they should immediately seek their physician's advice concerning the continued use of the present multi dose container. There have been reports of bacterial keratitis associated with the use of multiple-dose containers of topical ophthalmic products. These containers had been inadvertently contaminated by patients who, in most cases, had a concurrent corneal disease or a disruption of the ocular epithelial surface. Patients with bronchial asthma, a history of bronchial asthma, severe chronic obstructive pulmonary disease, sinus bradycardia, second- or third-degree atrioventricular block, or cardiac failure should be advised not to take this product (see Contraindications). Patients Wearing Contact
Lenses: Patients should be instructed to remove their lenses before application of the drops and not to re-insert the lenses earlier than 15 minutes after use.
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