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Tapticom, eye drops 0.0015%+0.5% 0.3 ml tube-caps 30 pcs
€31.89
Description
Pharmacodynamics.
The mechanism of action
Tapticom® is a combination medication containing two active ingredients, tafluprost and timolol. The two active ingredients reduce intraocular pressure (IOP) through additional mechanisms of action, and the combined action results in an additional reduction in IOP compared to the action of either substance alone.
Tafluprost is a fluorinated analog of prostaglandin F 2ɑ . Tafluprost acid, the biologically active metabolite of tafluprost, is a highly active selective antagonist of the human prostaglandin FP receptor.
Pharmacodynamic studies in animals show that tafluprost reduces intraocular pressure by increasing uveoscleral fluid outflow in the eye.
Timolol maleate is a non-selective beta-adrenoreceptor. The exact mechanism of action of timolol maleate in reducing intraocular pressure has not yet been fully established, although fluorescein and tonography studies suggest that the main action may be related to reduced fluid production. However, some studies have also shown a slight increase in outflow activation.
Clinical efficacy
In a 6-month study (n = 400) of patients with open-angle glaucoma or ophthalmohypertension and a mean untreated IOP of 24 to 26 mmHg.The IOP-lowering effect of Tuptic® (once daily in the morning) was compared with the combined administration of 0.0015% tafluprost (once daily in the morning) and 0.5% timolol (twice daily). Tapticom® was no less effective (not inferior) than 0.0015% tafluprost and 0.5% timolol, which were used together. The mean daily decrease in WTO relative to initial values was 8 mmHg in both groups with a primary endpoint of 6 months (decreases
were in the range of 7 to 9 mmHg in both groups at different times during the day during the study visits).
In another 6-month study (n = 564), Tuptic® was compared with appropriate monotherapy in patients with open-angle glaucoma or ophthalmohypertension and a mean untreated WTO of 26 to 27 mm Hg. Patients insufficiently controlled with 0.0015% tafluprost (WTO 20 mm Hg or greater with treatment) or 0.5% timolol (WTO 22 mm Hg or greater with treatment) were randomized to treatment with Taptic® or the same monotherapy. The mean daily reduction in WTO with Tapticom® was statistically greater than the mean daily reduction in WTO with tafluprost, which patients received once daily in the morning, or with timolol, which they received twice daily, at visits at 6 weeks, at 3 months (the primary endpoint of effectiveness assessment), and at 6 months. The mean daily reduction in WTO relative to baseline values was 9 mmHg when taking Tapticom® compared with 7 mmHg when taking both monotherapies. The decrease in HF when taking Tapticom® at different times during the day ranged from 8 to 9 mmHg in the comparison group, used tafluprost as monotherapy, and from 7 to 9 mmHg in the comparison group, used timolol as monotherapy.
Summarized data from patients who took Tapticom® and had a high initial WTO of 26 mm Hg (mean daily) or higher in the two baseline studies (n = 168) showed a mean daily reduction in WTO of 10 mm Hg at the primary endpoint (3 or 6 months), ranging from 9 to 12 mm Hg at various times during the day.
pharmacokinetic properties
absorption
. Plasma concentrations of tafluprostoic acid and timolol were examined in healthy volunteers after a single and repeated administration of Tapticom® for eight days (once daily), 0.0015% tafluprost (once daily) and 0.5% timolol (twice daily).The plasma concentration of tafluprostic acid reached its maximum value 10 minutes after the dose and decreased below the lower limit of detection (10 pg/mL) 30 minutes after administration of Tapticom® . The accumulation of tafluprostic acid was insignificant, and the mean urinary concentration of tafluprostic acid (mean AUC 0- last ) (monotherapy: 4.45 + 2.57 pg – h / ml Taptic® : 3.60 + 3.70 pg – h / mL) and mean maximum concentration ( max ) (monotherapy: 23.9 +11.8 pg – mL Taptic® : 18.7 + 11.9 pg – mL) were slightly lower with treatment with Taptic® compared to day 8 monotherapy with tafluprost. Plasma thymolol concentration reached its maximum value at a median T max (median time to reach maximum drug concentration) of 15 and 37.5 minutes after administration of Tuptic® on days 1 and 8, respectively. On day 8, the mean urinary thymolol concentration (mean AUC 0- last ) (monotherapy 5750 + 2440 pg – h / ml Tapticom® 4560 + 2980 pg – h / ml) and mean maximum concentration ( max ) (monotherapy: 1100 + 550 pg / ml Tapticom® 840 + 520 pg / ml) were slightly lower with treatment with Tapticom® compared with thymololol monotherapy. The lower plasma thymolol levels with treatment with Tuptic® are probably related to the once-daily dose of Tuptic® compared to the twice-daily dose of thymolol as monotherapy.
Tafluprost and timolol are absorbed through the cornea. In animals, after a single injection, corneal penetration of tafluprost with Tapticom® was similar to that with tafluprost as monotherapy, while timolol penetration was slightly less with Tapticom® compared to that with timolol as monotherapy. As for tafluprostic acid, the 4 h AUC was 7.5 ng – h / ml after administration of Tapticom® and 7.7 ng – h / ml after administration of tafluprost as monotherapy. For timolol, the 4 h AUC was 585 ng – h / mL and 737 ng – h / mL after administration of Tapticom® and timolol monodrug, respectively. The T max for tafluprostic acid was 60 minutes for both Taptic® and the monotherapy with tafluprost, whereas the T max for timolol was 60 minutes for Taptic® and 30 minutes for timolol monotherapy.
The distribution
Tafluprost
Tafluprost. There was no specific distribution of radioactive isotope-labeled tafluprost in the iridium-ciliary zone or vasculature (chorioid) or retinal pigment epithelium in animals, indicating low melanin pigment affinity. In a study with total actoradiography in animals, the highest concentration of radioactivity was observed in the cornea, and then in the eyelids, sclera, and iris. Outside the eye, radioactivity spread to the lacrimal organs, palate, esophagus and gastrointestinal tract, kidneys, liver, gallbladder, and bladder. The in vitro binding of tafluprostic acid to human serum albumin was 99% at a tafluprostic acid concentration of 500 ng/mL.
Timolol
In animals, the maximum level of timolol-labeled radioactivity in the ocular fluid was reached 30 minutes after a single injection of timolol labeled with the radioactive isotope 3 H (0.5% solution: 20 µl/eye) into both eyes. Thymolol is removed from the ocular fluid much faster than from the pigmented iris and ciliary body tissues.
Metabolism
Tafluprost
The major metabolic pathway of tafluprost in humans that has been studied in vitro is hydrolysis to the pharmacologically active metabolite, tafluprostoic acid, which is further metabolized by glucuronidation or beta-oxidation. The beta-oxidation products 1,2-dinor and 1,2,3,4-tetranor of tafluprostic acid, pharmacologically inactive, may be subject to glucuronidation or hydroxylation. The cytochrome P450 (CYP) enzyme system is not involved in the metabolism of tafluprostic acid. According to the results of studies of animal corneal tissue with purified enzymes, the main esterase responsible for esterase hydrolysis to tafluprostic acid is carboxylesterase. Butylcholinesterase, but not acetylcholinesterase, can also contribute to hydrolysis.
Timolol
Timolol is metabolized in the liver, mainly by the enzyme CYP2D6, to inactive metabolites, which are eliminated mainly by the kidneys.
Exhaustion
Tafluprost
. After tafluprost, labeled with the radioactive isotope 3 H (0.005% ophthalmic solution, 5 µl/eye), was injected once daily for 21 days into both eyes in animals, approximately 87% of the total radioactive dose was excreted. The total amount that was excreted with urine was about 27-38% of the dose and about 44-58% of the dose was excreted with feces.
Timolol
The established plasma elimination half-life is approximately 4:00. Timolol is actively metabolized in the liver; metabolites are excreted in the urine along with 20% in unchanged timolol after oral administration.
Indications
Indications
Lowering intraocular pressure (IOP) in adult patients with open-angle glaucoma or ophthalmohypertension who do not respond well to topical monotherapy with beta-blockers or prostaglandin analogues and require combination therapy and for whom preservative-free eye drops are indicated.
Active ingredient
Active ingredient
Composition
Composition
1 ml of eye drops contains 0.015 mg of tafluprost and 5 mg of timolol, which corresponds to 6.84 mg of timolol maleate;
excipients :
Glycerin sodium phosphate,
dodecahydrate;
Trilon B,
polysorbate 80,
sodium hydroxide and/or concentrated hydrochloric acid,
water for injection.
How to take, the dosage
How to take, the dosage
The recommended therapy is to put 1 drop of eye drops into the conjunctival sac of the affected eye(s) once a day.
If a dose is missed, treatment should be continued with the next dose as planned. The dose should not exceed one drop in the affected eye(s) once daily.
Tapticom® is a sterile, preservative-free solution. It is intended for single use only, one tube dropper is enough to treat both eyes. Any unused solution or residue must be disposed of immediately.
Elderly Patients
There is no need to change the dosage in elderly patients.
Renal and hepatic impairment
The use of tafluprost and timolol eye drops in patients with renal/hepatic impairment has been investigated, so Tapticom® should be used with caution in these patients.
Method of use
Ophthalmic use
To reduce the risk of darkening of the eyelid skin, patients should wipe excess fluid from the skin.
The systemic absorption is reduced when the eyelids are occluded or closed for 2 minutes.This may result in fewer systemic side effects and increased local activity.
If more than one ophthalmic drug is prescribed, the interval between injections of each of these drugs should be at least 5 minutes.
Contact lenses must be removed prior to eye-drop application and may be reapplied after a minimum of 15 minutes.
Patients should be advised to avoid direct eye contact with the bottle, as this could cause injury to the eye.
Patients should also be informed that ophthalmic solutions, if improperly handled, can become contaminated with common bacteria known to cause eye infections. Using contaminated solutions can result in serious eye damage and subsequent vision loss.
Children.
The safety and efficacy of Tuptic® in children (under 18 years of age) has not been established. Tuptic® is not indicated in children.
Interaction
Interaction
No specific studies of interactions with other medications have been performed.
Possible additional effects resulting in hypotension and/or marked bradycardia when ophthalmic beta-blocker solution is used simultaneously with oral calcium channel blockers, beta-adrenoblockers, antiarrhythmic drugs (including amiodarone), foxglove glycosides, parasympathomimetics, guanethidine.
The oral beta-adrenoblockers may exacerbate “ricochet” hypertension that occurred after clopheline withdrawal.
Augmented effects of systemic beta-blockers (e.g., decreased heart rate, depression) have been reported during combination treatment with CYP2D6 inhibitors (such as quinidine, fluoxetine, paroxetine) and timolol.
Rarely, mydriasis caused by concomitant use of ophthalmic beta-blockers and adrenaline (epinephrine) has been reported.
Contraindications
Contraindications
Allergic reactions to the active ingredients or to any of the excipients of the drug.
An irritation of the respiratory tract, as well as a history of bronchial asthma or bronchial asthma, severe chronic obstructive pulmonary disease.
Sinus bradycardia, sinus node weakness syndrome, as well as sinoatrial block, degree II-III block, which is not controlled by a pacemaker, severe heart failure or cardiogenic shock.
Side effects
Side effects
In clinical trials, more than 484 patients were treated with Taptic® . A common treatment-related adverse reaction reported was conjunctiva/hyperemia. It occurred in approximately 7% of patients enrolled in clinical trials; it was mild in most cases, and in 1.2% of patients it was associated with discontinuation of treatment.
The adverse reactions reported in clinical trials using Tapticom® were limited to those previously reported with either of the active ingredients, tafluprost or timolol. No new adverse reactions specific to Tapticom® were observed in the clinical trials. Most of the adverse reactions reported were ocular, mild to moderate in severity, and were not serious.
Like other topical ophthalmic drugs, tafluprost and timolol are absorbed systemically. This may cause similar adverse reactions to those seen with systemic beta-blockers. The incidence of systemic adverse reactions after topical administration of ophthalmic drugs is lower than when used systemically. The following adverse reactions include those that have been observed within the class of ophthalmic beta-blockers.
These adverse reactions have been reported when taking Tapticom® in clinical trials (within each, the adverse reaction frequency group below is presented in decreasing order of frequency).
The frequency of possible adverse reactions listed below was determined using the following conventions: Very common (â¥1 / 10); common (⥠1/100 to < 1/10); infrequent (â¥1 / 1,000 to < 1/100);rare (â¥1 / 10000 to < 1 / 1,000) very rare (< 1 / 10,000) unknown (frequency cannot be determined based on existing data).
Tapticom® (tafluprostu/ timolol combination)
Nervous system disorders
Infrequently : Headache
Visual organs
Often : Conjunctivae/hyperemia, eye itching, eye pain, changes in eyelashes (increased length, thickness and number of eyelashes), discoloration of eyelashes, eye irritation, feeling of foreign body in eyes, blurred vision, photophobia (photophobia).
Infrequent : unusual sensation in the eye, dry eyes, eye discomfort, conjunctivitis, erythema of the eyelids, eye allergy, eyelid swelling, superficial pitting keratitis, increased lacrimation, anterior chamber inflammation, asthenopia (rapid eye fatigue), blepharitis (inflamed eyelids ).
Additional adverse reactions that have been observed with one of the active substances (tafluprost or timolol) and may also occur with Tapticom® are listed below.
Tafluprost
Visual effects : Decreased visual acuity, increased iris pigmentation, eyelid pigmentation, conjunctival edema, ocular discharge, cellular reaction of anterior chamber moisture, cellular opalescence in the anterior chamber of the eye, allergic conjunctivitis, conjunctival pigmentation, conjunctival follicles, deepening of eyelid sulcus, iritis (iris inflammation) / uveitis (inflammation of the globe choroid).
Skin and skin derivatives : hypertrichosis of the eyelids.
Respiratory system : exacerbation of bronchial asthma, dyspnea (shortness of breath / difficulty breathing).
thymolol
Immune system disorders : signs and symptoms of allergic reactions including angioedema, urticaria, solitary and multiple rashes, anaphylactic reaction, pruritus.
Metabolism and nutrition : hypoglycemia.
Psychiatric disorders : depression, sleep disturbance (insomnia), nightmares, memory loss, nervousness.
Nervous system disorders : dizziness, fainting, paresthesias, increased myasthenia gravis, hemorrhagic stroke, cerebral ischemia.
In visual organs : keratitis, decreased corneal sensitivity, visual disturbances and disorders including changes in refraction (due to myotic withdrawal in some cases), ptosis (eyelid drooping), diplopia (double vision), chorioidal detachment after filter surgery, lacrimation , corneal erosion.
Hearing and balance : ringing/noise in the ears.
Heart : bradycardia, chest pain, palpitations, edema, arrhythmia, congestive heart failure, cardiac arrest, heart block, blockade, heart failure.
Vascular side : hypotension, claudication, Raynaud’s disease, cold extremities (hands and feet).
Respiratory system, chest and mediastinal organs: dyspnea (dyspnea/choking difficulties), bronchospasm (especially in patients with pre-existing bronchospastic disease), breathing disorders, cough.
Digestive system : nausea, dyspepsia (digestive disorders), diarrhea, dry mouth, dysgeusia (taste disorder), abdominal pain, vomiting.
Skin and skin derivatives : alopecia (alopecia), psoriasis-like rash or exacerbation of psoriasis, skin rash.
Muscular and connective tissue disorders: systemic lupus erythematosus, myalgia (muscle pain), arthropathy (joint disease).
Gender and mammary gland disorders: Peyronie’s disease (fibroplastic induration of the penis), decreased libido, sexual dysfunction.
General disorders and reactions at the injection site : asthenia (general weakness) / fatigue, thirst.
Cases of corneal calcification have very rarely been reported due to the use of eye drops containing phosphate in some patients with significant corneal damage.
Overdose
Overdose
Overdose with topical tafluprost is unlikely to occur or to be associated with toxicity.
There have been reports of accidental overdose with timolol resulting in general intoxication symptoms similar to those seen with systemic beta-adrenoblockers, such as dizziness, headache, difficulty breathing (shortness of breath), bradycardia, bronchospasm and cardiac arrest (see also section on adverse reactions).
If an overdose of Tuptic® occurs, treatment should be symptomatic and supportive. Timolol is not actively removed by hemodialysis.
Additional information
| Weight | 0.070 kg |
|---|---|
| Manufacturer | Laboratoire Uniter, France |
| Medication form | eye drops |
| Brand | Laboratoire Uniter |
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