Timolol (When ATH C07AA06)

When ATH:
C07AA06

Characteristic.

Тимолола малеат и гемигидрат — белый кристаллический порошок без запаха. The hemihydrate form slightly soluble in water, readily soluble in alcohol; in the form of maleate salt acid is soluble in water, methanol, alcohol.

Pharmacological action.
Gipotenzivnoe, antianginalnoe, antiarrhythmic, protivoglaukomnoe.

Application.

Inside: arterial hypertension, gipertroficheskaya cardiomyopathy, mitral valve prolapse, angina, prevention of recurrent myocardial infarction, migraine (prevent attacks), essential tremor, alarm. Locally: elevated intraocular pressure, glaucoma (otkratougolnaya, secondary, when aphakia and others.).

Contraindications.

For the purpose inside and locally: hypersensitivity, bronchial asthma (incl. history), chronic obstructive pulmonary disease, cardiogenic shock, acute and chronic heart failure, AV block II-III degrees, sinoatrialynaya blockade, sinusovaya bradycardia (less than 45-50 beats. / min), sick sinus syndrome; when applied topically: degenerative diseases of the cornea, severe allergic inflammation of the nasal mucosa, lactation, natural infancy (premature and newborn babies).

Restrictions apply.

Emphysema, nonallergic chronic bronchitis, vasomotor rhinitis, Raynaud's disease, liver dysfunction and / or kidney, Acidosis, diabetes, gipoglikemiâ, hyperthyroidism, myasthenia, advanced age, pregnancy, for systemic administration - infancy (Safety and efficacy have not determined).

Pregnancy and breast-feeding.

Maybe, if the effect of therapy outweighs the potential risk to the fetus.

Category actions result in FDA - C. (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)

At the time of treatment should stop breastfeeding.

Side effects.

From the nervous system and sensory organs: dizziness, headache, asthenia, fatiguability, sleep disturbance, insomnia, nightmares, depression, excitation, hallucinations, kratkovremennaya amnesia, disorientation in space, paraesthesia, increased symptoms of myasthenia gravis; noise in ears; eye irritation, blurred vision, diplopia, ptosis, dryness of mucous membranes of the eyes; when applied topically: transient blurred vision (from 30 from to 5 min - 6%), burning and itchy eyes, foreign body sensation in the eye, changes in refraction and visual acuity, lacrimation, photophobia, reduction in corneal sensitivity, edema of the corneal epithelium, inflammation of the eyelid margins, conjunctivitis, .Aloe, superficial punctate keratopathy, keratit.

From the respiratory system: nasal congestion, chest pain, cough, breathlessness, suffocation, bronchospasm (possible death), respiratory insufficiency.

Cardio-vascular system (hematopoiesis, hemostasis): heartbeat, simptomaticheskaya bradycardia, arrhythmia, OF блокада, cardiac arrest, heart failure (possible death), gipotenziya, collapse, Raynaud's syndrome, cold extremities, exacerbation of intermittent claudication, transient ischemic attack, cerebral ischemia, syncope, a decrease in hemoglobin, gematokrita.

From the digestive tract: dry mouth, anorexia, dyspepsia, nausea, vomiting, diarrhea.

For the skin: rash, hives, exacerbation of psoriasis, itch, prurigo, alopecia.

Other: angioedema, withdrawal, weight change, lupus syndrome, the weakening of the libido, impotence, Peyronie's disease, hyperkalemia, hyperuricemia, hypertriglyceridemia.

Cooperation.

Increases (mutually) the likelihood of violations of automaticity, conductivity and contractility of the heart on the background of amiodarone, simpatolitikov, diltiazema, verapamil, quinidine medicines; the risk of hypotension and cardiac decompensation - against the background of dihydropyridine calcium antagonists, Anesthetic. NSAIDs weaken hypotensive effect. The local application is compatible with miotocs and carbonic anhydrase inhibitors. Simultaneous use of eye drops, containing epinephrine or norepinephrine, can cause mydriasis. Epinephrine- and pilokarpinsoderzhaschie eyedrops potentiate reduction of intraocular pressure. With simultaneous systemic and local application of beta-blockers may mutual reinforcement effects.

Overdose.

Symptoms: dizziness, headache, nausea and vomiting, bradycardia, arrhythmia, acute heart failure, bronchospasm.

Treatment: using eye drops - immediately washing with water or saline eye. Ingestion - gastric lavage, administration of activated charcoal, simptomaticheskaya therapy: atropyn, beta-agonists (Isoprenaline, izadrin), glucagon hydrochloride, systemic vasopressor agents (norepinephrine, doʙutamin), beta2-adrenomimetiki (with bronchospasm); cardiac glycosides, Diuretic, aminofillin (Heart failure); oxygen therapy; may conduct pacing. Hemodialysis maloeffyektivyen.

Dosing and Administration.

Inside: with hypertension 10 mg 2 once a day, if necessary, increase the dose at weekly intervals up to a maximum daily - 60 mg. Prevention of recurrent myocardial infarction - after 1-4 weeks after the first infarct 10 mg 2 once a day. The maximum daily dose - 30 mg (10 mg in the morning and 20 mg in the evening). Preventing migraine attacks - the initial dose of 10 mg 2 once a day. The maximum daily - 30 mg (10 mg in the morning and 20 mg in the evening).

Konъyunktyvalno, in the affected eye, adult and children by 1 drop of 0.25% to 0.5% solution 1-2 times a day for 6 Sun (no more). After stabilization of intraocular pressure - of 1 drop 1 once a day.

Precautions.

Before starting treatment should be compensated heart failure. During therapy monitoring heart rate, BP and the early detection of symptoms of heart failure. Violation of the liver and kidneys necessitate dose reduction. Should be abolished for 48 hours before surgery. Mask symptoms (taxikardiju) hypoglycemia in patients receiving oral antidiabetic agents and insulin and a thyrotoxicosis (sudden removal may cause thyrotoxic crisis). Perhaps the increased severity of hypersensitivity reactions and the lack of effect of conventional doses of epinephrine with aggravated allergic history. To reduce suction after instillation into the eye should be 1-2 minutes to press a finger on the tear duct at the inner corner of the eye. With the use of angle-closure glaucoma is only possible in conjunction with miotocs. Instilled etc.. The drug is recommended at least 10 minutes before application of timolol.

When applied topically, it is necessary to control the function of tearing, the integrity of the cornea, and the field of view 1 once every 6 months, and the intraocular pressure (through 4 weeks after start of therapy). During treatment is permitted only wearing hard contact lenses (should be removed prior to instillation and again put through 15 m). When transferring a patient with an ophthalmic treatment etc.. Beta-blockers stop taking the previous drug and the next day prescribed timolol. In case of cancellation of other glaucoma medications needed during 1 daily use of both agents (under the control of intraocular pressure) and then continue the use of timolol. Be wary of during the drivers of vehicles and people, skills relate to the high concentration of attention.

Cautions.

Before burying the bottle to turn sharply and shake (no more 1 times). During treatment may change the test results in laboratory studies.

Cooperation

Active substanceDescription of interaction
AkarʙozaFMR. Against the background of systemic effects of timolol enhanced effect; the combined appointment of caution (may mask the symptoms of hypoglycemia).
AmiodaroneFMR: synergism. It enhances systemic effects and increases (especially when on / in) the chance of developing a deep bradycardia, suppression of sinus rhythm and AV blockade.
VerapamilFMR: synergism. Enhances systemic effects, increased risk of adverse effects on heart rate, AV conduction and / or cardiac contractility, the possibility of excessive hypotension, tyazhelaya bradycardia, OF блокада, until complete cardiac arrest.
GlimepirideFMR. Against the background of systemic effects of timolol enhanced effect; the combined appointment of caution (may mask the symptoms of hypoglycemia).
GlipizideFMR: synergism. Against the background of systemic effects of timolol enhanced effect; with a joint appointment caution (possible masking of the early symptoms of hypoglycemia).
DigoxinFMR. Strengthens (mutually) deterioration of AV conduction.
DiltiazemFMR: synergism. Enhances systemic effects, increased risk of adverse effects on heart rate, AV conduction and / or cardiac contractility, the possibility of excessive hypotension, tyazhelaya bradycardia, OF блокада, until complete cardiac arrest.
IndomethacinFMR: antagonizm. Reduces the risk of hypotension (It inhibits the synthesis of prostaglandins in the kidneys and inhibits sodium and fluid).
Insulin aspartFMR: synergism. Against the background of systemic effects of timolol enhanced effect; simultaneous use may mask early symptoms of hypoglycemia.
Insulin dvuhfaznыy [human genetic engineering]FMR: synergism. Against the background of systemic effects of timolol enhanced effect; concomitant use may mask early symptoms of developing hypoglycemia.
KlonidinFMR. Against the background of systemic effects of timolol increases the risk of violating the regulation of blood pressure; exacerbates bradycardia and AV block increases the probability.
MetforminFMR: synergism. Against the background of systemic effects of timolol enhanced effect; the combined appointment of caution (possible masking of symptoms of hypoglycaemia, in particular tachycardia).
NaproxenFMR: antagonizm. Weakens the risk of hypotension.
NimodipineFMR: synergism. Strengthens (mutually) systemic effects, possible deterioration of AV conduction and ventricular contractility, development of hypotension; combined use is not recommended.
NifedipineFMR: synergism. Strengthens (mutually) systemic effects, possible deterioration of AV conduction and ventricular contractility, development of hypotension; combined use is not recommended.
NorepinephrineFMR. When instilled in the eye effect weakens myotic (possible mydriasis).
OctreotideFMR: synergism. May exacerbate systemic effects (bradycardia, arrhythmia, asequence).
PilokarpinFMR: synergism. In the form of eye drops strengthens (mutually) lowering intraocular pressure, when administered systemically increases the probability of conduction disturbances.
PioglitazoneFMR. Against the background of systemic effects of timolol enhanced effect; joint application requires caution: may mask the symptoms of hypoglycemia.
RepaglinideFMR: synergism. Against the background of systemic effects of timolol enhanced effect; combined appointment requires caution: possible masking of symptoms of hypoglycaemia (in particular tachycardia).
RisperidoneFMR: synergism. Against the background of systemic effects of timolol enhanced hypotensive effect.
RifampicinFKV. It accelerates biotransformation and lowers blood.
RosiglitazoneFMR. Against the background of systemic effects of timolol enhanced effect; with a joint appointment caution (may mask the symptoms of hypoglycemia).
FelodipineFMR: synergism. Strengthens (mutually) systemic effects, It increases the likelihood of the risk of AV conduction disorders, left ventricular failure.
PhenylbutazoneFMR: antagonizm. It weakens the possible antihypertensive effect.
QuinidineFMR: synergism. Enhances systemic effects, increases (mutually) the likelihood of violations of automaticity, conduction and myocardial contractility.
CelecoxibFMR: antagonizm. It weakens the possible antihypertensive effect.
EpinephrineFMR. When instilled in the eye increases intraocular pressure reduction and causing mydriasis.

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