Elevex

Elevex Uses, Dosage, Side Effects, Food Interaction and all others data.

Elevex is a non-selective β-adrenergic receptor blocker. It does not have significant intrinsic sympathomimetic activity, direct myocardial depressant activity or local anaesth activity. Exact mechanism of ocular hypotensive effect is unclear, but it is thought to be related to reduction of aqueous humour formation. β-blockade also causes lowering of BP.

Elevex, when administered by the ophthalmic route, rapidly reduces intraocular pressure. When administered in the tablet form, it reduces blood pressure, heart rate, and cardiac output, and decreases sympathetic activity.. This drug has a fast onset of action, usually occurring within 20 minutes of the administration of an ophthalmic dose. Elevex maleate can exert pharmacological actions for as long as 24 hours if given in the 0.5% or 0.25% doses.

Trade Name Elevex
Availability Prescription only
Generic Timolol
Timolol Other Names Timolol, Timololo, Timololum
Related Drugs amlodipine, aspirin, lisinopril, metoprolol, losartan, furosemide, carvedilol, hydrochlorothiazide, propranolol, atenolol
Type
Formula C13H24N4O3S
Weight Average: 316.42
Monoisotopic: 316.156911344
Protein binding

The plasma protein binding of timolol is not extensive and is estimated to be about 10%.

Groups Approved
Therapeutic Class Drugs for miotics and glaucoma
Manufacturer
Available Country Philippines
Last Updated: September 19, 2023 at 7:00 am
Elevex
Elevex

Uses

Elevex Maleate Ophthalmic Solution is used for the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.

Elevex is also used to associated treatment for these conditions: Increased Intra Ocular Pressure (IOP), Migraine, Ocular Hypertension, Open Angle Glaucoma (OAG)

How Elevex works

Elevex competes with adrenergic neurotransmitters for binding to beta(1)-adrenergic receptors in the heart and the beta(2)-receptors in the vascular and bronchial smooth muscle. This leads to diminished actions of catecholamines, which normally bind to adrenergic receptors and exert sympathetic effects leading to an increase in blood pressure and heart rate. Beta(1)-receptor blockade by timolol leads to a decrease in both heart rate and cardiac output during rest and exercise, and a decrease in both systolic and diastolic blood pressure. In addition to this, a reduction in reflex orthostatic hypotension may also occur. The blockade of beta(2) receptors by timolol in the blood vessels leads to a decrease in peripheral vascular resistance, reducing blood pressure.

The exact mechanism by which timolol reduces ocular pressure is unknown at this time, however, it likely decreases the secretion of aqueous humor in the eye. According to one study, the reduction of aqueous humor secretion may occur through the decreased blood supply to the ciliary body resulting from interference with the active transport system or interference with prostaglandin biosynthesis.

Dosage

Elevex dosage

Eye drops Solution: Initially, instill 1 drop of 0.25% solution bid into the affected eye(s), may increase to 1 drop of 0.5% solution bid if there is inadequate response; decrease to 1 drop once daily if controlled. Do not exceed 1 drop bid of 0.5% solution.

Gel-forming eye drops:0.25% or 0.5% Gel-forming eye drops: Instill 1 drop into the affected eye(s) once daily.

Side Effects

Burning and stinging sensation of the eyes, bradycardia, hypotension, arrhythmia and AV or SA nodal block, CHF, pulmonary oedema, Raynaud's phenomenon, headache, dizziness, fatigue, asthenia, abdominal discomfort, nausea, constipation, hypoglycaemia.

Toxicity

The oral LD50 for timolol maleate is 1028 mg/kg in the rat and 1137 mg/kg in the mouse.

Symptoms of timolol overdose may include dizziness, headache, shortness of breath, bradycardia, in addition to bronchospasm. Sometimes, an overdose may lead to cardiac arrest. An overdose of timolol can be reversed with dialysis, however, patients with renal failure may not respond as well to dialysis treatment.

Precaution

Patients with inadequate cardiac function, DM, myasthenia gravis, cerebrovascular insufficiency, history of atopy. Avoid abrupt withdrawal as it may exacerbate angina symptoms or precipitate MI in patients with coronary artery disease, or precipitate thyroid crisis in patients with thyrotoxicosis. Patients undergoing major surgery. May mask signs of hyperthyroidism and hypoglycaemia. Ophth soln should not be used as monotherapy for angle-closure glaucoma. Renal and hepatic impairment. Pregnancy and lactation.

Interaction

Although Elevex used alone has little or no effect on pupil size, mydriasis resulting from concomitant therapy with Elevex Maleate and epinephrine has been reported occasionally. Drug interactions of Elevex Maleate have been noticed with concomitant administration of beta-adrenergic blocking agents (both oral and topical), calcium antagonists, catecholamine-depleting drugs, digitalis, quinidin, clonidine, injectable epinephrine.

Food Interaction

No interactions found.

Elevex Alcohol interaction

[Moderate]

Many psychotherapeutic and CNS-active agents (e.g., anxiolytics, sedatives, hypnotics, antidepressants, antipsychotics, opioids, alcohol, muscle relaxants) exhibit hypotensive effects, especially during initiation of therapy and dose escalation.

Coadministration with antihypertensives and other hypotensive agents, in particular vasodilators and alpha-blockers, may result in additive effects on blood pressure and orthostasis.

Caution and close monitoring for development of hypotension is advised during coadministration of these agents.

Some authorities recommend avoiding alcohol in patients receiving vasodilating antihypertensive drugs.

Patients should be advised to avoid rising abruptly from a sitting or recumbent position and to notify their physician if they experience dizziness, lightheadedness, syncope, orthostasis, or tachycardia.

Elevex Cholesterol interaction

[Moderate] Beta-adrenergic receptor blocking agents (aka beta-blockers) may alter serum lipid profiles.

Increases in serum VLDL and LDL cholesterol and triglycerides, as well as decreases in HDL cholesterol, have been reported with some beta-blockers.

Patients with preexisting hyperlipidemia may require closer monitoring during beta-blocker therapy, and adjustments made accordingly in their lipid-lowering regimen.

Elevex multivitamins interaction

[Moderate] ADJUST DOSING INTERVAL: Concurrent administration with calcium salts may decrease the oral bioavailability of atenolol and possibly other beta-blockers.

The exact mechanism of interaction is unknown.

In six healthy subjects, calcium 500 mg (as lactate, carbonate, and gluconate) reduced the mean peak plasma concentration (Cmax) and area under the concentration-time curve (AUC) of atenolol (100 mg) by 51% and 32%, respectively.

The elimination half-life increased by 44%.

Twelve hours after the combination, beta-blocking activity (as indicated by inhibition of exercise tachycardia) was reduced compared to that with atenolol alone.

However, during a 4-week treatment in six hypertensive patients, there was no difference in blood pressure values between treatments.

The investigators suggest that prolongation of the elimination half-life induced by calcium coadministration may have led to atenolol cumulation during long-term dosing, which compensated for the reduced bioavailability.

It may help to separate the administration times of beta-blockers and calcium products by at least 2 hours.

Patients should be monitored for potentially diminished beta-blocking effects following the addition of calcium therapy.

Volume of Distribution

1.3 - 1.7 L/kg

Elevex is distributed to the following tissues: the conjunctiva, cornea, iris, sclera, aqueous humor, kidney, liver, and lung.

Elimination Route

The systemic bioavailability of the ophthalmic eyedrop in one study of healthy volunteers was 78.0 ± 24.5% , indicating that caution must be observed when this drug is administered, as it may be significantly absorbed and have various systemic effects. Another study measured the bioavailability of timolol eyedrops to be 60% in healthy volunteers.

The peak concentration of ophthalmic timolol in plasma, Cmax was about 1.14 ng/ml in most subjects within 15 minutes following the administration of timolol by the ophthalmic route. The mean area under the curve (AUC) was about 6.46 ng/ml per hour after intravenous injection and about 4.78 ng/ml per hour following eyedrop administration.

Half Life

Elevex half-life was measured at 2.9 ± 0.3 h hours in a clinical study of healthy volunteers.

Clearance

One pharmacokinetic study in healthy volunteers measured the total plasma clearance of timolol to be 557 ± 61 ml/min. Another study determined the total clearance 751.5 ± 90.6 ml/min and renal clearance to be 97.2 ± 10.1 ml/min in healthy volunteers.

Elimination Route

Elevex and its metabolites are mainly found excreted in the urine.

Pregnancy & Breastfeeding use

Pregnancy: There are no adequate and well-controlled studies in pregnant women. Elevex should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Lactation: Elevex has been detected in breast milk following oral and ophthalmic drug administration. Because of the potential for serious adverse reactions from Elevex 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.

Contraindication

Elevex is contraindicated in patients with bronchial asthma, a history of bronchial asthma, severe chronic obstructive pulmonary disease, sinus bradycardia, second or third degree atrioventricular block, overt cardiac failure, cardiogenic shock, hypersensitivity to any component of this product.

Acute Overdose

There have been reports of inadvertent overdosage with Elevex Ophthalmic Solution resulting in systemic effects similar to those seen with systemic beta-adrenergic blocking agents such as dizziness, headache, shortness of breath, bradycardia, bronchospasm, and cardiac arrest.

Storage Condition

Store between 15-30° C. Avoid freezing and protect from light.

Innovators Monograph

You find simplified version here Elevex

Elevex contains Timolol see full prescribing information from innovator Elevex Monograph, Elevex MSDS, Elevex FDA label

FAQ

What is timolol used for?

Elevex is used to treat glaucoma, a condition in which increased pressure in the eye can lead to gradual loss of vision.Elevex is in a class of medications called beta-blockers. It works by decreasing the pressure in the eye.

Is taking Elevex safe?

Elevex may cause heart failure in some patients. Check with your doctor right away if you are having chest pain or discomfort, dilated neck veins, extreme fatigue, irregular breathing, an irregular heartbeat, swelling of the face, fingers, feet, or lower legs, weight gain, or trouble breathing.

What are the common side effects of Elevex?

the common side effects of Elevex are include:

  • wheezing, chest pain, trouble breathing, slow heartbeats;
  • a light-headed feeling, like you might pass out;
  • muscle weakness;
  • depressed mood, confusion, hallucinations, unusual thoughts or behavior; or.
  • numbness or cold feeling in your hands and feet

Can Elevex be used long term?

Long term used Elevex reduced intraocular pressure by 31%. There were no changes in visual acuity, visual field, excavation and degeneration of the optic disc, or slit lamp examination findings.

Can you use Elevex at night?

Elevex don't work at night, Elevex which has a substantial effect when tested during the day, has been found to have no measurable effect at night.

Does Elevex raise blood sugar?

Elevex may cause changes in your blood sugar levels. Also may cover up signs of low blood sugar, such as a rapid pulse rate.

What happens if I miss my Elevex?

If you forget your dose , it's okay to make up for it as soon as you remember it. If you miss your morning dose, use your drops the moment you remember them, even if it's later in the day. If you miss your night-time dose, do it the next morning, but never instil two drops to make up for the missed dose.

Is Elevex safe during pregnancy?

Elevex should be used during pregnancy only if the possible benefit outweighs the possible risk to the unborn baby.Elevex should be given to a pregnant woman only if clearly needed.

Is Elevex safe during breastfeeding?

Ophthalmic use of Elevex  by the mother should pose little risk to the breastfed infant, although some guidelines state that gel formulations are preferred over solutions.

Can I drink alcohol with Elevex?

Elevex alone can cause drowsiness, dizziness or fainting, lightheadedness and blurred vision. Drinking alcohol while taking Elevex can increase the drowsiness and dizziness which in turn increase the risk of accidental injury.

Can I drive after taking alcohol?

It takes most people 1 to 2 hours to process one standard drink. That means after 3 standard drinks you should wait at least 3 hours before driving.

Does Elevex make I gain weight?

Elevex doesn't typically cause you to gain weight or have more body fat.

How long should I close my eyes after eye drops?

After the drop goes in, keep your eye closed for about thirty seconds to help it absorb properly.

Does Elevex affect heart rate?

Ophthalmic Elevex significantly decreased resting and maximal exercise heart rate after the first dose and maximal exercise heart rate during chronic dosing.

Can Elevex cause cough?

Elevex may causes cough ,upset stomach, skin rash or worsening psoriasis, sleep problems.

Who should not take Elevex?

You should not use this medicine if you are allergic to Elevex, or if you have: asthma or severe chronic obstructive pulmonary disease.

Can Elevex cause blindness?

Serious damage to the eye and possible loss of vision may result from using contaminated eye medicines.

Is Elevex used for hypertension?

Elevex is used alone or together with other medicines such as hydrochlorothiazide to treat high blood pressure (hypertension). High blood pressure adds to the workload of the heart and arteries. If it continues for a long time, the heart and arteries may not function properly.

Is Elevex a selective beta blocker?

Elevex is a non-selective beta adrenergic blocker used in the treatment of elevated intraocular pressure in ocular hypertension or open angle glaucoma.

What happens if I stop taking Elevex?

Do not stop taking Elevex  without talking to your doctor first. If Elevex is stopped suddenly, it may cause chest pain or heart attack in some people.

*** Taking medicines without doctor's advice can cause long-term problems.
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