Effortil (Etilefrine)
Sympathomimetic agent for orthostatic hypotension
Last reviewed: | Published:
Effortil is a prescription medication containing etilefrine hydrochloride, a sympathomimetic agent used to treat orthostatic hypotension — a condition characterised by a significant drop in blood pressure upon standing. By constricting peripheral blood vessels and enhancing cardiac output, Effortil helps prevent symptoms such as dizziness, palpitations, and fainting episodes during positional changes. It is available as 5 mg tablets and is manufactured by SERB SA.
Key Takeaways
- Effortil (etilefrine) is a sympathomimetic drug that treats orthostatic hypotension by constricting blood vessels and increasing cardiac output.
- Standard adult dose is 1–2 tablets (5–10 mg) taken three times daily; dosage for children depends on age.
- Common side effects include headache, while less common effects include palpitations, tremor, anxiety, and insomnia.
- The drug is contraindicated in hypertension, thyrotoxicosis, phaeochromocytoma, narrow-angle glaucoma, and during the first trimester of pregnancy.
- Multiple drug interactions exist — particularly with thyroid hormones, antidepressants, cardiac glycosides, and diabetes medications.
What Is Effortil and What Is It Used For?
Effortil contains etilefrine hydrochloride, a sympathomimetic agent that stabilises blood pressure in patients who suffer from orthostatic hypotension — the drop in blood pressure that occurs when moving from a lying to a sitting or standing position.
Orthostatic hypotension is a common cardiovascular condition affecting millions of people worldwide. It occurs when the body's mechanisms for maintaining blood pressure during positional changes fail to respond adequately. Patients with this condition frequently experience dizziness, light-headedness, palpitations, visual disturbances, and in severe cases, syncope (fainting) upon standing. These symptoms can significantly impact daily functioning, increase fall risk (especially in the elderly), and reduce overall quality of life.
Effortil works through a dual mechanism of action. As a sympathomimetic agent, etilefrine stimulates both alpha- and beta-adrenergic receptors in the sympathetic nervous system. The alpha-adrenergic stimulation causes vasoconstriction, particularly in the peripheral blood vessels of the lower extremities. This constriction of the venous capacitance vessels in the legs is crucial because it prevents blood from pooling in the lower body when the patient stands up. Simultaneously, the beta-adrenergic stimulation enhances the heart's contractility (positive inotropic effect), increasing the force of each heartbeat and improving cardiac output.
The net result of these combined effects is a more efficient circulatory response to postural changes. The increased venous return from the legs, combined with improved cardiac pumping, maintains adequate cerebral blood flow during standing, thereby preventing or reducing the symptoms of orthostatic hypotension. Unlike some other sympathomimetic agents, etilefrine produces a relatively balanced stimulation of both receptor subtypes, which contributes to a more physiological blood pressure response.
Orthostatic hypotension may occur as a primary autonomic disorder or secondary to various conditions including diabetes, Parkinson's disease, multiple system atrophy, medications (particularly antihypertensives and diuretics), dehydration, and prolonged bed rest. It is particularly common among elderly patients, where the prevalence may exceed 20% in those over 65 years of age. The condition is defined as a sustained reduction in systolic blood pressure of at least 20 mmHg or diastolic blood pressure of at least 10 mmHg within three minutes of standing, as established by international consensus guidelines.
Your physician may prescribe Effortil for conditions other than those described here. Always follow your physician's instructions and the directions provided with your prescription. Do not adjust your dosage or discontinue the medication without consulting your healthcare provider.
What Should You Know Before Taking Effortil?
Before taking Effortil, inform your physician about all existing medical conditions, current medications, and whether you are pregnant or breastfeeding. Several conditions and drug combinations make Effortil use unsafe.
Contraindications
Do not take Effortil if you are allergic to etilefrine hydrochloride or any of the other ingredients in the formulation. The excipients include lactose monohydrate, maize starch, colloidal silicon dioxide, modified starch, sodium metabisulfite (E223), and glyceryl palmitostearate. In addition, Effortil is contraindicated in the following conditions:
- Hypertension — high blood pressure. Effortil raises blood pressure and would worsen this condition.
- Hypotensive dysregulation — high blood pressure when standing compared to sitting or lying (paradoxical response).
- Thyrotoxicosis — overactive thyroid gland. Sympathomimetics can exacerbate the cardiovascular effects of excess thyroid hormones.
- Phaeochromocytoma — a tumour of the adrenal glands that overproduces noradrenaline. Effortil could trigger a hypertensive crisis.
- Narrow-angle glaucoma — Effortil can increase intraocular pressure, worsening this eye condition.
- Prostatic adenoma with urinary retention — benign prostate enlargement causing difficulty urinating.
- Coronary artery disease — increased cardiac demand from Effortil may worsen ischaemia.
- Decompensated heart failure — poorly controlled heart failure.
- Hypertrophic obstructive cardiomyopathy (HOCM) — increased contractility could worsen the obstruction.
- Stenosis of heart valves or central arteries — narrowing of valves or major arteries.
- First trimester of pregnancy — use is contraindicated during the first 12 weeks of gestation.
Warnings and Precautions
Speak to your physician or pharmacist before taking Effortil if you have any of the following conditions, as special monitoring or dose adjustments may be required:
- Cardiac arrhythmias — fast or irregular heart rhythm, or other serious cardiovascular disease. Etilefrine's stimulatory effects on the heart may aggravate existing arrhythmias, potentially leading to haemodynamically significant rhythm disturbances.
- Diabetes mellitus — Effortil can interfere with blood sugar regulation and may reduce the effectiveness of antidiabetic medications. More frequent blood glucose monitoring may be necessary during treatment initiation and dose changes.
- Hyperthyroidism — elevated thyroid hormone levels can enhance the cardiovascular effects of Effortil, increasing the risk of tachycardia and elevated blood pressure beyond the intended therapeutic range.
Patients should also be aware that Effortil is intended to complement, not replace, non-pharmacological management of orthostatic hypotension. Measures such as adequate fluid intake (2–3 litres per day), sufficient dietary salt, wearing compression stockings, elevating the head of the bed, and avoiding rapid position changes remain important components of comprehensive management.
Pregnancy and Breastfeeding
If you are pregnant, think you may be pregnant, are planning to become pregnant, or are breastfeeding, consult your physician or pharmacist before using Effortil. The use of this medication requires careful consideration during these periods.
Pregnancy: Effortil must not be used at all during the first three months (first trimester) of pregnancy. During the second and third trimesters, Effortil should only be used after your physician has carefully weighed the potential benefits against the risks. Sympathomimetic agents may affect uterine blood flow and foetal development, so the decision to use Effortil during pregnancy must be made on an individual basis by a qualified healthcare professional. Animal studies have not been conclusive regarding the teratogenic potential of etilefrine, and there are limited human data available.
Breastfeeding: It is currently unknown whether etilefrine or its metabolites are excreted in human breast milk. Therefore, the potential risk to the nursing infant cannot be fully excluded. Your physician will consider whether to discontinue breastfeeding or to discontinue/withhold Effortil therapy, taking into account the benefit of breastfeeding for the infant and the benefit of therapy for the mother.
Driving and Operating Machinery
Effortil may cause dizziness in some patients. You are personally responsible for assessing whether you are fit to drive motor vehicles or perform tasks that require alertness. Consider the effects and side effects of this medication when making such assessments. If you experience dizziness or any other side effect that impairs your concentration, do not drive or operate heavy machinery. Consult your physician or pharmacist if you are unsure about your fitness to drive.
It is also important to note that the underlying condition being treated — orthostatic hypotension — can itself impair the ability to drive safely. Sudden drops in blood pressure may cause dizziness, visual disturbances, or loss of consciousness, which could have serious consequences while driving. Ensure that your condition is adequately controlled before operating any vehicle or machinery.
How Does Effortil Interact with Other Drugs?
Effortil interacts with multiple drug classes. Inform your physician about all medications you are taking, including prescription, over-the-counter, and herbal products, as several interactions can either enhance or diminish the drug's effects or increase the risk of adverse events.
Drug interactions with Effortil arise from its sympathomimetic mechanism of action. Because etilefrine stimulates adrenergic receptors, any other medication that affects the sympathetic nervous system, cardiovascular function, or metabolic processes may interact with it. Understanding these interactions is essential for safe and effective therapy.
Drugs That May Enhance Effortil's Effects
The following medications can increase the blood pressure-raising effects of Effortil, potentially leading to excessive hypertension, tachycardia, or other cardiovascular complications:
| Drug / Class | Examples | Interaction Effect |
|---|---|---|
| Thyroid hormones | Levothyroxine, liothyronine | Enhanced cardiovascular stimulation; increased risk of tachycardia and hypertension |
| Tricyclic antidepressants | Amitriptyline, clomipramine | Potentiation of sympathomimetic effects due to inhibition of noradrenaline reuptake |
| MAO inhibitors | Moclobemide | Reduced breakdown of catecholamines; risk of hypertensive crisis |
| Antihistamines | Various H1-receptor antagonists | May potentiate the pressor response of sympathomimetics |
| Mineralocorticoids | Fludrocortisone | Additive blood pressure elevation through sodium and water retention |
| Ergot alkaloids | Dihydroergotamine | Combined vasoconstriction can lead to excessive blood pressure increases |
| Anticholinergics | Atropine (including eye drops) | Enhanced cardiovascular effects due to parasympathetic blockade |
Other Important Interactions
Beyond the drugs that enhance Effortil's effects, several other clinically relevant interactions should be considered:
- Cardiac glycosides (e.g. digoxin): High doses of cardiac glycosides combined with Effortil can increase the risk of cardiac arrhythmias. Both drug classes affect cardiac contractility and rhythm, and their combined effects may precipitate ventricular arrhythmias. If concomitant use is unavoidable, close cardiac monitoring with ECG is recommended, and serum digoxin levels should be maintained within the therapeutic range.
- General anaesthetics: Certain anaesthetic agents, particularly halogenated hydrocarbons (halothane, enflurane, sevoflurane), sensitise the myocardium to the effects of sympathomimetics. This combination can increase the risk of serious cardiac arrhythmias during surgery, including ventricular fibrillation. Inform your anaesthetist that you are taking Effortil well in advance of any surgical procedure; the medication may need to be discontinued several days before elective surgery.
- Antidiabetic medications: Effortil may reduce the blood sugar-lowering effect of insulin and oral antidiabetic drugs (metformin, sulfonylureas, SGLT2 inhibitors, etc.) through sympathomimetic stimulation of hepatic glucose production and reduced peripheral glucose uptake. Patients with diabetes should monitor their blood glucose more frequently when starting or stopping Effortil and discuss dose adjustments with their physician.
- Alpha- and beta-blockers: Antihypertensive medications in the alpha-blocker (doxazosin, prazosin, tamsulosin) and beta-blocker (propranolol, metoprolol, bisoprolol) classes can reduce the efficacy of Effortil by blocking the very receptors it stimulates. Additionally, the combination of non-selective beta-blockers with Effortil may cause a paradoxical hypertensive response due to unopposed alpha-adrenergic stimulation. If both medications are necessary, careful dose titration and monitoring are essential.
What Is the Correct Dosage of Effortil?
The standard dose of Effortil varies by age. Always follow your physician's prescription exactly, as individual dosing may differ from the general recommendations below.
Effortil should always be used exactly as prescribed by your physician. The dosage is individually determined based on the severity of orthostatic symptoms, the patient's blood pressure response, and the presence of any comorbid conditions. Treatment should be initiated at the lowest effective dose and adjusted upward only if necessary. Regular follow-up with blood pressure monitoring is recommended, particularly during the first few weeks of treatment.
Adults
Adults and children over 7 years
Dose: 1–2 tablets (5–10 mg) three times daily
Tablets should be taken with a glass of water. The total daily dose typically ranges from 15 mg to 30 mg, divided into three doses. Your physician may adjust the dosage based on your individual response and blood pressure measurements. It is generally recommended to take the last dose in the early evening rather than at bedtime, as the stimulant properties of etilefrine may interfere with sleep. Taking the medication approximately 30 minutes before activities that typically provoke symptoms (e.g., getting out of bed in the morning) can optimise its effectiveness.
Children
Children aged 1–7 years
Dose: ½–1 tablet (2.5–5 mg) three times daily
The tablet may be halved along the score line for accurate dosing in younger children. Paediatric dosing should always be determined and supervised by a physician. The total daily dose for this age group ranges from 7.5 mg to 15 mg. Orthostatic hypotension is relatively uncommon in children, and a thorough evaluation for underlying causes should be completed before initiating pharmacotherapy.
Elderly
Elderly patients
Dose: Start with the lowest effective dose (1 tablet three times daily)
Older adults are particularly susceptible to orthostatic hypotension and may benefit significantly from Effortil. However, they are also more sensitive to cardiovascular side effects, including tachycardia and hypertension. Physicians typically initiate therapy at the lower end of the dosing range and titrate upward cautiously while monitoring blood pressure and heart rate in both the sitting and standing positions. Special attention should be paid to potential interactions with other medications commonly used in older adults, including antihypertensives, diuretics, and medications for Parkinson's disease.
Missed Dose
If you forget to take a dose of Effortil, take it as soon as you remember. However, if it is nearly time for your next scheduled dose, skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for a forgotten tablet. Taking too much etilefrine at once can lead to excessive blood pressure elevation and tachycardia. If you frequently forget doses, consider setting reminders or using a pill organiser to help maintain consistent dosing.
Overdose
What Are the Side Effects of Effortil?
Like all medicines, Effortil can cause side effects, although not everyone experiences them. The most frequently reported side effect is headache. Most side effects are mild and tend to diminish as the body adjusts to the medication.
The side effects of Effortil are largely predictable from its sympathomimetic mechanism of action. By stimulating adrenergic receptors throughout the body, etilefrine can produce cardiovascular, neurological, and gastrointestinal effects. The severity and frequency of side effects generally correlate with the dose administered and individual patient sensitivity. If you experience any of the following side effects and they persist or worsen, consult your physician promptly.
Common
May affect up to 1 in 10 users
- Headache
Uncommon
May affect up to 1 in 100 users
- Anxiety
- Insomnia (difficulty falling or staying asleep)
- Tremor (involuntary shaking)
- Restlessness
- Dizziness
- Palpitations (awareness of heartbeat)
- Tachycardia (rapid heart rate)
- Cardiac arrhythmias (irregular heartbeat)
- Nausea
Not Known
Frequency cannot be estimated from available data
- Hypersensitivity reactions (allergic reactions)
- Angina pectoris (chest pain due to reduced cardiac blood flow)
- Elevated blood pressure (hypertension)
- Excessive sweating (hyperhidrosis)
The sympathomimetic nature of etilefrine explains many of the reported side effects. Stimulation of beta-1 receptors in the heart can produce palpitations, tachycardia, and in predisposed individuals, arrhythmias. Central nervous system effects such as headache, anxiety, and insomnia result from adrenergic stimulation in the brain. Nausea is likely mediated through both central and peripheral mechanisms. These effects are dose-dependent and typically more pronounced at the beginning of treatment or after dose increases.
Patients who experience angina pectoris or significant cardiac arrhythmias should discontinue Effortil immediately and seek medical attention. These symptoms may indicate that the cardiovascular stimulation exceeds the patient's cardiac reserve and could precipitate serious complications. Hypersensitivity reactions, although very rare, may be related to the sodium metabisulfite preservative rather than the active ingredient itself. Individuals with a history of asthma or sulfite sensitivity should be particularly vigilant for signs of allergic reactions, including bronchospasm, urticaria, or anaphylaxis.
If side effects are bothersome but not severe, your physician may suggest reducing the dose or adjusting the timing of administration. Taking the last dose earlier in the day can help mitigate insomnia, while taking tablets with food may reduce nausea. Most mild side effects diminish within the first one to two weeks of treatment as the body adapts to the medication.
How Should You Store Effortil?
Store Effortil out of the sight and reach of children. No special storage conditions are required beyond standard room temperature recommendations.
Effortil tablets should be stored in their original aluminium/PVC blister packaging to protect them from moisture and light. There are no specific temperature requirements beyond normal room temperature storage (typically 15–25°C or 59–77°F). Do not store in the bathroom or other humid environments, as moisture can degrade the tablets and reduce their efficacy.
Do not use the medication after the expiry date printed on the carton after "EXP." The expiry date refers to the last day of the stated month. Using expired medication may result in reduced effectiveness or potentially altered chemical composition.
Do not dispose of medicines by flushing them down the toilet or throwing them in household waste. Return unused or expired medications to your pharmacy, where they will be disposed of in an environmentally responsible manner through appropriate pharmaceutical waste programmes. Proper disposal helps protect the environment and prevents accidental ingestion by children, pets, or wildlife.
What Does Effortil Contain?
Each Effortil tablet contains 5 mg of etilefrine hydrochloride as the active ingredient, along with several inactive excipients necessary for tablet manufacture.
Active Ingredient
Etilefrine hydrochloride 5 mg per tablet. Etilefrine (also known as ethilefrine) is a synthetic sympathomimetic amine structurally related to adrenaline (epinephrine). It has the chemical name (R)-2-(ethylamino)-1-(3-hydroxyphenyl)ethanol hydrochloride. It acts as a direct-acting sympathomimetic, stimulating alpha-1, beta-1, and beta-2 adrenergic receptors with varying degrees of affinity. Unlike indirect-acting sympathomimetics (such as ephedrine), etilefrine does not rely on the release of endogenous noradrenaline from nerve terminals for its effects.
Inactive Ingredients (Excipients)
- Lactose monohydrate (32 mg) — a sugar used as a filler and binder in tablet manufacturing. Patients with lactose intolerance should be aware of this ingredient.
- Maize starch — used as a disintegrant to help the tablet break apart after ingestion, ensuring proper absorption of the active ingredient.
- Anhydrous colloidal silicon dioxide — a flow agent (glidant) that prevents tablet ingredients from clumping during the manufacturing process.
- Modified starch — used as a binder to help maintain tablet integrity and cohesion.
- Sodium metabisulfite (E223) — an antioxidant preservative that prevents degradation of the active ingredient. In rare cases, this compound may cause hypersensitivity reactions, particularly in patients with asthma or sulfite sensitivity.
- Glyceryl palmitostearate — a lubricant that facilitates the tablet manufacturing process by reducing friction during tablet compression.
Physical Description
Effortil tablets are white, round, biconvex tablets with bevelled edges. One side is scored and marked with "05E/05E." The score line allows the tablet to be divided into two equal halves for accurate dosing, which is particularly useful for paediatric patients who require a 2.5 mg dose. Each tablet has a diameter of 6 mm. Effortil is available in packs of 100 tablets in aluminium/PVC blister packaging, which provides protection against moisture and light.
Frequently Asked Questions
Orthostatic hypotension (also called postural hypotension) is a condition in which blood pressure drops significantly when you stand up from a sitting or lying position. This typically occurs because blood pools in the legs due to gravity, and the body's compensatory mechanisms (vasoconstriction and increased heart rate) fail to respond adequately. Symptoms include dizziness, light-headedness, blurred vision, and fainting. Effortil helps by constricting blood vessels (particularly in the legs) to prevent blood pooling, while simultaneously increasing the heart's pumping force. Together, these effects maintain adequate blood pressure and cerebral blood flow during positional changes.
When taken orally as a tablet, Effortil is absorbed from the gastrointestinal tract and typically begins to exert its effects within 30 to 60 minutes. The peak effect occurs approximately 1 to 2 hours after ingestion. The duration of action for a single dose is generally 4 to 6 hours, which is why the medication is usually taken three times daily to maintain consistent blood pressure support throughout waking hours.
Effortil can be used for extended periods under medical supervision. However, the need for continued treatment should be reassessed regularly by your physician. Long-term use requires periodic monitoring of blood pressure and heart rate to ensure the medication remains appropriate. Some patients may develop tolerance over time, requiring dose adjustments. Non-pharmacological measures such as adequate hydration, compression stockings, and gradual position changes should be employed alongside medication therapy to optimise outcomes.
Elderly patients can benefit from Effortil, as orthostatic hypotension is particularly prevalent in older adults, affecting over 20% of those over 65 years of age. However, they may be more sensitive to the cardiovascular side effects of sympathomimetic agents. Physicians typically start with the lowest effective dose (5 mg three times daily) and increase gradually if needed. Regular monitoring of blood pressure, heart rate, and cardiac rhythm is important. Elderly patients often take multiple medications, making drug interaction assessment essential before starting Effortil.
Alcohol consumption is generally not recommended when taking Effortil. Alcohol is a vasodilator, meaning it widens blood vessels and can lower blood pressure. This directly counteracts the therapeutic effect of Effortil, potentially worsening orthostatic hypotension symptoms. Additionally, both alcohol and Effortil can cause dizziness, and the combination may increase the risk of falls, particularly in elderly patients. If you choose to consume alcohol, do so in moderation and discuss the implications with your physician.
If you feel that the effect of Effortil is too weak or too strong, consult your physician. Do not adjust the dosage on your own. Your physician may increase the dose, add other measures (such as increased fluid and salt intake, compression stockings, or physical counter-manoeuvres), or consider alternative medications such as midodrine or fludrocortisone. Sometimes the underlying cause of orthostatic hypotension (e.g. dehydration, medication side effects, or autonomic neuropathy) needs to be addressed for optimal results.
References
- European Medicines Agency (EMA). Summary of Product Characteristics: Effortil (etilefrine hydrochloride). SERB SA. Last updated 2021.
- World Health Organization (WHO). WHO Model List of Essential Medicines, 23rd List. Geneva: WHO; 2023.
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- Ricci F, De Caterina R, Fedorowski A. Orthostatic Hypotension: Epidemiology, Prognosis, and Treatment. Journal of the American College of Cardiology. 2015;66(7):848-860.
- Metzler M, Duerr S, Granata R, Krismer F, Robertson D, Wenning GK. Neurogenic orthostatic hypotension: pathophysiology, evaluation, and management. Journal of Neurology. 2013;260(9):2212-2219.
- Shibao C, Lipsitz LA, Biaggioni I. Evaluation and treatment of orthostatic hypotension. Journal of the American Society of Hypertension. 2013;7(4):317-324.
- British National Formulary (BNF). Sympathomimetics, vasoconstrictor. National Institute for Health and Care Excellence (NICE). Accessed 2026.
- European Society of Cardiology (ESC). 2018 ESC/ESH Guidelines for the Management of Arterial Hypertension. European Heart Journal. 2018;39(33):3021-3104.
- Lahrmann H, Cortelli P, Hilz M, Mathias CJ, Struhal W, Tassinari M. EFNS guidelines on the diagnosis and management of orthostatic hypotension. European Journal of Neurology. 2006;13(9):930-936.
- Gibbons CH, Schmidt P, Biaggioni I, et al. The recommendations of a consensus panel for the screening, diagnosis, and treatment of neurogenic orthostatic hypotension and associated supine hypertension. Journal of Neurology. 2017;264(8):1567-1582.
Editorial Team
This article was written by the iMedic Medical Editorial Team, comprising licensed physicians with specialisations in clinical pharmacology, cardiology, and internal medicine. All content is reviewed according to international medical guidelines from the WHO, ESC, and EMA.
Our editorial process follows the GRADE evidence framework and adheres to the principles of evidence-based medicine. All medical claims are supported by peer-reviewed literature and official product information documents. The editorial team declares no conflicts of interest and receives no pharmaceutical company funding.