Estazolam – composition, action, dosage, contraindications, side effects

Proven content

Estazolam is a hypnotic and anticonvulsant drug. It is used primarily in neurology and psychiatry. It is a prescription preparation. The active substance in this medicine is estazolam, which belongs to a group of medicines called benzodiazepines. Estazolam is usually used in cases of difficulty falling asleep, frequent night awakenings or early morning awakenings. What are the contraindications to the use of this drug? How should it be dosed? Can taking it have side effects?

Estazolam – drug characteristics

Estazolam is a hypnotic and anticonvulsant drug. It is used in the treatment of psychiatric and neurological ailments. It is a prescription drug issued by a doctor.

The active substance of the drug is estazolam, which has a hypnotic effect, helps to fall asleep, slightly reduces the tension of skeletal muscles, and also has a weak anticonvulsant effect.

Estazolam drug packaging contains 20 or 28 tablets. They are yellow, round and flat on both sides.

The entity responsible for the production and distribution of the drug Estazolam is Polfa Tarchomin, i.e. Tarchomińskie Zakłady Farmaceutyczne “Polfa” Spółka Akcyjna. Polfa Tarchomin is a Polish pharmaceutical company with its seat in Warsaw. The origins of this company date back to 1823. The Chemical Products Factory was established at that time, later transformed into Przemysłowo-Handlowe Zakłady Chemiczne “Ludwik Spiess i Syn. Polfa Tarchomin was one of the first insulin producers in the world, but also the only producer of penicillin. The company is one of the largest producers of generic drugs in Poland. It produces, among others anti-infective drugs, insulins, psychotropic drugs and dermatological preparations.

In addition, under the name Estazolam, you can buy drugs whose manufacturer and distributor are:

1. Chemical and Pharmaceutical Labor Cooperative ESPEFA – Espefa is a chemical and pharmaceutical labor cooperative that was established in 1946. The founders of the cooperative were three Krakow pharmacists: Stanisław Szymański, Aleksander Kaszycki and Jan Szustow. The seat of the Espefa cooperative is in Kraków;
2. Polfarmex SA – Polfarmex is a Polish pharmaceutical company based in Kutno. The company was founded in 1989 under the name “Polfa – Farmex”. Initially, the concern traded in medicines and imported raw materials. Currently, Polfarmex is a producer of prescription drugs, over-the-counter drugs, dietary supplements and cosmetics. 

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Estazolam – composition and action of the drug

Estazolam is a hypnotic preparation. The active substance, estazolam, is a triazole derivative of benzodiazepine (BZD) with an intermediate duration of action. One tablet contains 2 mg of estazolam.

Estazolam binds to the benzodiazepine receptor (RBZD), which causes a specific reaction in the cell. Benzodiazepine receptors are part of receptors called GABA-A receptors, which are capable of binding many substances, including -aminobutyric acid (GABA). The indirect effect of estazolam is to increase the ability of GABA to bind to the GABA-A receptor. Due to the inhibitory effect of GABA on nerve cells, estazolam exerts an indirect inhibitory effect on the central nervous system.

This drug works primarily to help you sleep. It is also indicated that it may have a sedative and anxiolytic effect. The use of Estazolam may reduce muscle tension and show anticonvulsant properties.

Orally administered estazolam is rapidly absorbed from the gastrointestinal tract. The maximum concentration is reached about 2 hours after administration of the drug. This substance undergoes changes in the liver, including to 4-hydroxyestazolam, which shows little biological activity. The metabolites are mainly excreted via the kidneys in the urine. <4% of the dose is excreted in the faeces.

The other ingredients of Estazolam have:

1. potato starch;
2. sodium carboxymethyl starch (type A);
3. gelatine;
4. quinoline yellow (E 104);
5. talk;
6. magnesium stearate;
7. lactose monohydrate.

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Estazolam – indications for use

Estazolam is a preparation that is used in cases of sleep problems. Your doctor may recommend this medication, especially for the treatment of:

1. difficulty falling asleep;
2. frequent nighttime awakenings;
3. early morning awakenings.

If you want to know how to deal with insomnia, read on: What to do when you cannot sleep? Effective remedies for insomnia

Estazolam – contraindications

The drug Estazolam, despite its effectiveness in combating sleep problems, cannot be used by every patient struggling with this type of ailments.

Contraindications to the use of Estazolam are:

1. allergic (hypersensitive) to estazolam or other benzodiazepine drugs or any of the ingredients of the drug;
2. severe respiratory failure in the patient;
3. sleep apnea syndrome (frequent short pauses in breathing during sleep);
4. dizziness, balance disorder;
5. disturbances of consciousness;
6. myasthenia gravis, which is a disease that causes muscle weakness and excessive fatigue;
7. acute porphyria, which is a rare blood related metabolic disease;
8. poisoning with alcohol or drugs acting on the central nervous system.

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Estazolam – precautions

Before and during the use of Estazolam, follow the precautions included in the package leaflet.

Particular care should be taken in the following cases:

1. if Estazolam is used for several weeks, its effectiveness may decrease, therefore you should monitor your tolerance to this drug;
2. if Estazolam is used for a long time, psychological and physical dependence may occur. The risk of developing dependence increases with increasing dose and duration of treatment and is greater in patients with drug dependence, alcohol dependence, or patients with personality disorders;
3. if you stop taking your medicine suddenly, you may experience withdrawal symptoms such as headache, muscle aches, increased anxiety, tension, excitement, restlessness, confusion, sleep disturbances, irritability. In more severe cases, the following symptoms are observed: loss of sense of reality, personality disorders, hypersensitivity to sound, touch, light, noise, tingling sensation and numbness in the limbs, hallucinations and delusions, epileptic seizures;
4. Rebound phenomena and anxiety may occur during drug withdrawal. This means a temporary relapse of severe sleep problems. These symptoms are often accompanied by mood changes, restlessness, sleep disturbance and insomnia;
5. the use of this medicine can cause anterograde amnesia, which is the inability to remember what happened after taking the medicine. There may also be episodes of subsequent memory, manifested by difficulties in learning or remembering new information;
6. the use of Estazolam in children and the elderly may increase the risk of abnormal mental and paradoxical reactions, such as: restlessness, agitation, irritability, aggression, anger, rage, delusions, nightmares, hallucinations, psychosis or behavioral disorders;
7. elderly patients should be given lower doses of the drug;
8. patients with liver or kidney failure or chronic respiratory failure should inform their doctor about their diseases before using the drug;
9. depressed patients should inform their doctor about their illness. Such patients should take several medications at the same time. Taking estazolam alone can make your depression symptoms worse and also increase the risk of suicidal thoughts;
10. patients with addictions, especially to alcohol, drugs or medications, should inform their doctor about their addictions. These patients are at greater risk of physical and mental dependence on Estazolam;
11. Patients with porphyria should inform their doctor about this disease before starting treatment with Estazolam. During prolonged treatment with estazolam, your doctor will usually order periodic blood tests (complete blood counts) and urinalysis. 

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Estazolam – dosage and method of use

Always use Estazolam exactly as described in the package leaflet or as directed by your doctor or pharmacist.

For adults, the usual dose is 1 mg to 2 mg (1/2 to 1 tablet) half an hour before bedtime. Estazolam tablets should be taken orally with a little water. Your doctor will start treatment with the lowest effective dose and gradually increase it as necessary. However, treatment should not exceed 7-10 days.

Inappropriate use of Estazolam is considered to be taking more than the recommended dose of the drug or missing the indicated dose during the day.

If the patient takes a higher dose of the drug than recommended by the doctor, symptoms such as disturbance of consciousness, sleepiness, slurred speech may occur. In severe cases of poisoning, the following may occur: ataxia, hypotension, muscle weakness, breathing disorders, coma.

If you forget to take a dose of Estazolam, take the next dose as soon as you remember. However, if it is almost time for your next dose, skip that dose and take the next one as prescribed. If you forget to take two or more doses, contact your doctor.

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Estazolam – side effects

The drug Estazolam, like any other drug, may cause side effects in patients. It is important to report any suspected adverse reactions after authorization of the medicinal product so that the benefit / risk balance of the medicinal product can be monitored.

The frequency classification of adverse body reactions (ADRs) is based on the following principles: very common (≥1 / 10), common (≥1 / 100 to <1/10), uncommon (≥1 / 1 to <000/1), rare (≥ 100 / 1 to <10 / 000), very rare (<1 / 1), not known (cannot be estimated from the available data).

Among the serious side effects are:

1. a severe allergic reaction such as itching, swelling of the lips or tongue or wheezing or shortness of breath. These symptoms have been reported very rarely;
2. confusion, states of excitement and agitation, suicidal depression, restlessness, irritability, delusions, nightmares, hallucinations (seeing or hearing things that are not there), psychosis (loss of contact with reality), unusual behavior. These disorders most often appear after alcohol consumption and the elderly or those with mental illnesses.

Other side effects that may be caused by the use of Estazolam are:

1. change in the number of certain blood cells;
2. rashes, itching, hives;
3. lack of appetite;
4. paradoxical reactions – psychomotor restlessness, insomnia, increased excitability and aggressiveness, muscle tremors, convulsions. Paradoxical reactions most often occur after alcohol consumption, in elderly patients and in patients with mental illnesses;
5. psychological and physical dependence may develop during treatment with estazolam in therapeutic doses. Sudden discontinuation of treatment may cause withdrawal symptoms. Patients abusing alcohol or drugs are more prone to develop addiction. Pre-existing, undiagnosed depression may become apparent during treatment with estazolam;
6. feeling sleepy, dizzy, slower reaction may occur during the first few days of treatment;
7. sleepiness, memory problems, impaired coordination, speech disorders, changes in sex drive;
8. visual disturbances (blurred, double vision);
9. slow heart rate, chest pain;
10. a slight decrease in blood pressure;
11. stomach discomfort, dry mouth;
12. slight elevation of liver enzymes, liver dysfunction with development of jaundice (yellowing of the skin, whites of the eyes);
13. muscle tremors, muscle relaxation;
14. urinary retention, urinary incontinence;
15. menstrual disorders;
16. general weakness, fainting.

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Estazolam – interactions with other drugs

Before starting treatment with Estazolam, please inform your doctor or pharmacist about all the medicines you are taking or have taken recently. You should also inform what medications the patient plans to take in the near future.

Drugs that Estazolam may interact with include:

1. fluvoxamine, fluoxetine and other drugs used to treat mental illness;
2. drugs for the treatment of insomnia;
3. medicines for allergic diseases that can cause drowsiness;
4. epilepsy medicines (e.g. carbamazepine, phenytoin, hydantoin);
5. drugs for stomach and duodenal ulcers (e.g. cimetidine, omeprazole, cisapride);
6. rifampicin (a medicine to treat tuberculosis);
7. ketoconazole (an antifungal medicine);
8. drugs used for general anesthesia;
9. strong painkillers (e.g. morphine, codeine);
10. skeletal muscle relaxants (e.g. Baclofen);
11. medicines for Parkinson’s disease (e.g. levodopa);
12. alcohol: drinking alcohol while taking Estazolam may increase its effect and lead to paradoxical reactions such as psychomotor agitation or aggressive behavior.

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Estazolam and pregnancy and breastfeeding

The use of any medications or dietary supplements during pregnancy requires consultation with the attending physician. If you are pregnant or breastfeeding, think you may be pregnant or are planning to have a baby, ask your doctor or pharmacist for advice before taking Estazolam.

Estazolam passes into breast milk. If administration of the drug is necessary, breast-feeding should be discontinued.

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Estazol – price

The price of the drug Estazolam may differ depending on the city in which the antibiotic will be purchased or the pharmacy chosen by the patient. The price of the product also depends on the manufacturer responsible for the distribution of the drug and the number of tablets contained in the package.

1. Estazolam TZF 20 tablets – about PLN 8-9;
2. Estazolam TZF 28 tablets – about PLN 11-12;
3. Estazolam Espefa 20 tablets – about 6 zlotys;
4. Estazolam Espefa 28 tablets – about 7 zlotys;
5. Estazolam Polfarmex 20 tablets – approx. PLN 5-6;
6. Estazolam Polfarmex 28 tablets – about PLN 8-9.

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Estazolam – substitutes

Products that have the same international name and exist in the same form do not have to be substitutes, because the use of a given drug is determined by the content of the active substance, i.e. the dose of the drug.

It should be remembered that even when the dose of the active substance is similar, the patient may not always use the substitute, because he may be allergic to any of the other excipients of the drug.

Therefore, before using a substitute for Estazolam, read the package leaflet or consult your doctor or pharmacist.

Among the active substances that show an effect similar to Estazolam, the following are mentioned:

1. alprazolam — np. Afobam, Xanax, Zomiren;
2. bromazepam — for example Bromox, Lexotan, Seven;
3. chlordiazepoxide – e.g., Elenium;
4. diazepam — np. Relanium, Neorelium, Relsed;
5. klobazam – np. Friesian;
6. klorazepam — np. Chloranxen, Tranxene,
7. lorazepam — n.p. Lorabex, Temelor;
8. lormetazepam – e.g. Noctofer;
9. medazepam – e.g., Rudotel;
10. midazolam — np. Buccolam, Dromicum, Midanium;
11. nitrazepam — np. Nomefren;
12. oksazepam — np. Oxazepam;
13. temazepam — np. Signopam.

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