Fluoxymesterone halotestin is a non-selective fluoxymesterone halotestin blocker of beta-adrenergic receptors. It has no intrinsic sympathomimetic and membrane stabilizing activity.
When applied topically as eye drops reduce both normal and elevated intraocular pressure by decreasing the formation of intraocular fluid. It has no effect on pupil size and accommodation.
The action of the drug is 20 minutes after instillation into conjunctival cavity. The maximum decrease in intraocular pressure occurs within 1-2 hours and lasts for 24 hours.
The local application of timolol fluoxymesterone halotestin rapidly penetrates the cornea. After instillation of eye drops maximum concentration of timolol in the aqueous humor of the anterior chamber is achieved in 1-2 hours.
The small amount reaches the systemic circulation by absorption through the vessels of the conjunctiva, nasal mucosa and lacrimal tract. Withdrawal timolol metabolites is carried out mainly by the kidneys.
In infants and young children the concentration of the active substance substantially exceeds its plasma Cmax in adults.
Indications for use:
- increased intraocular pressure (ocular hypertension);
- open-angle glaucoma;
- afakicheskaya glaucoma and secondary glaucoma other;
- as an additional means for reducing the intraocular pressure in angle-closure glaucoma (in combination with miotikami);
- congenital glaucoma (with failure of other therapeutic measures).
Do not use Arutimol if previously observed raised individual sensitivity to timolol. The drug is also contraindicated in patients with a history of the following diseases are present;
- asthma or other severe chronic obstructive airway disease;
- sinus bradycardia (slow heartbeat);
- atrioventricular block II or III degree;
- severe heart failure;
- cardiogenic shock;
- allergic reaction with generalized skin rash;
- heavy atrophic rhinitis;
- corneal dystrophy.
Arutimol should be used with caution in patients with pulmonary insufficiency, severe cerebrovascular insufficiency, congestive heart failure, diabetes, hypoglycemia, thyrotoxicosis, myasthenia gravis, and while the appointment of other beta-blockers.Pregnancy and lactation:
Sufficient experience with the use of the drug during pregnancy, lactation and children do not have, however, shown that timolol passes the placental barrier and enters the breast milk. Perhaps the use of Arutimola for the treatment of children, pregnant and lactating mothers prescribed by a doctor, if the expected therapeutic effect is greater than the risk of possible side effects.
If the drug is used just before birth or during breastfeeding, the newborn should be closely monitored for several days after birth and during the entire treatment period, drug Arutimol nursing mothers.
Dosage and administration:
At the beginning of therapy instilled 1 drop preparation “Arutimol” 0.25% and 0.5% in the diseased eye two times a day.
If the IOP is normalized with regular use, the dosage should be limited to up to 1 times a day on the 1st drop preparation.
Arutimolom treatment is carried out, as a rule, for a long time.Suspension or change the dosage are carried out only by order of the physician.
Local reactions: irritation and redness of the conjunctiva, eyelid skin, burning and itchy eyes, watery eyes, photophobia, edema of the corneal epithelium, superficial punctate keratopathy, corneal gipostezii, diplopia, ptosis, dry eyes. During the fistuliziruyuschih antiglaukomatoznyh operations may develop choroidal detachment in the postoperative period.
Cardio-vascular system: congestive heart failure, bradycardia, bradyarrhythmia lowering blood pressure collapse, atrioventricular block, cardiac arrest transient ischemic
part of the respiratory system: dyspnea, bronchospasm, pulmonary insufficiency.
CNS: headache, dizziness , weakness, depression, paresthesia.
On the part fluoxymesterone halotestin of the digestive tract: nausea, diarrhea.
Allergic reactions: urticaria, eczema.
Rhinitis, sexual dysfunction, alopecia.
Local use in infants can lead to sleep apnea.
In case of side effects, discontinue use of the drug and how to contact your doctor as soon as possible (ophthalmologist).
Perhaps the development of obscherezorbtivnyh effects typical of beta-blockers: dizziness, headache, arrhythmia, bradycardia, bronchospasm, nausea, vomiting.
Treatment: Immediately rinse eyes with water or saline solution, symptomatic therapy.
You must see your doctor regularly to measure intraocular pressure and corneal examination.
If the patient wears soft contact lenses, he should not use eye drops “Arutimol” 0.25% and 0.5% as a preservative may be deposited in soft contact lenses, and provide adverse effects on the eye tissue.
it should remove hard contact lenses prior to instillation of the drug and to wear them again only after 15 minutes.
Immediately after instillation of the drug may reduce the clarity of vision and slow mental reactions, which may reduce the ability to actively participate in road traffic, maintenance of machines or to perform work without reliable support. To an even greater extent this occurs in the interaction of the drug with alcohol.
When transferring patients to treatment with timolol may need refractive error correction after effects caused by previously used miotikami.
In the case of the upcoming surgery with general anesthesia, it is necessary to cancel the drug for 48 hours.
Interaction with other drugs:
Sharing Arutimola fluoxymesterone halotestin with eye drops containing adrenaline may cause mydriasis.
The specific effect of the drug – reducing the intraocular pressure increases with simultaneous use of eye drops containing epinephrine and pilocarpine, burying in the eyes of the two beta-blockers should not be.
Lowering blood pressure and slowing heart rate may potentiate the joint application of the drug with calcium antagonists, reserpine, and beta-blockers.
Concomitant use with insulin or oral antidiabetic agents may cause hypoglycemia.
timolol increases the effects of muscle relaxants, so requires removal of the drug for 48 hours before the planned surgery with general anesthesia.
These data may relate to drugs that have been applied shortly before.