Esipral

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

Esipral is a selective inhibitor of serotonin (5-HT) re-uptake. The inhibition of 5-HT re-uptake is the only likely mechanism of action explaining the pharmacological and clinical effects of escitalopram. Esipral has no or low affinity for a number of receptors including 5-HT1A, 5-HT2, DA D1 and D2 receptors, α1-, α2-, β-adrenoceptors, histamine H1, muscarine cholinergic, benzodiazepine and opioid receptors.

Esipral belongs to a class of medications called selective serotonin re-uptake inhibitors (SSRIs). These agents cause an increase in serotonin levels in neuronal synapses by preventing the re-uptake of serotonin (5-HT) into the presynaptic terminals of serotonergic neurons. As compared to other SSRIs, it appears to have a relatively quick onset of effect due to its potency.

SSRIs as a class have been associated with abnormal bleeding, particularly in patients receiving concomitant therapy with other medications affecting hemostasis, and with the development of serotonin syndrome. Use escitalopram with caution in patients with a higher-than-baseline risk of bleeding and in patients receiving concomitant therapy with other serotonergic drugs. Esipral may also cause a discontinuation syndrome with abrupt removal of the drug, and should be slowly tapered if discontinuation of therapy is warranted.

Trade Name Esipral
Availability Prescription only
Generic Escitalopram
Escitalopram Other Names (S)-Citalopram, Escitalopram, Escitalopramum
Related Drugs Rexulti, sertraline, trazodone, alprazolam, duloxetine, hydroxyzine, Lexapro, venlafaxine, Zoloft, citalopram
Type
Formula C20H21FN2O
Weight Average: 324.3919
Monoisotopic: 324.163791509
Protein binding

Escitalopram exhibits relatively low protein binding at approximately 55-56%.

Groups Approved
Therapeutic Class SSRIs & related anti-depressant drugs
Manufacturer
Available Country Finland
Last Updated: September 19, 2023 at 7:00 am
Esipral
Esipral

Uses

Esipral is used for Depressive illness, Generalized anxiety disorder, Obsessive-compulsive disorder, Social anxiety disorder

Esipral is also used to associated treatment for these conditions: Generalized Anxiety Disorder (GAD), Major Depressive Disorder (MDD), Obsessive Compulsive Disorder (OCD)

How Esipral works

Esipral, like other selective serotonin re-uptake inhibitors, enhances serotonergic activity by binding to the orthosteric (i.e. primary) binding site on the serotonin transporter (SERT), the same site to which endogenous 5-HT binds, and thus prevents the re-uptake of serotonin into the presynaptic neuron. Esipral, along with paroxetine, is also considered an allosteric serotonin re-uptake inhibitor - it binds to a secondary allosteric site on the SERT molecule to more strongly inhibit 5-HT re-uptake. Its combination of orthosteric and allosteric activity on SERT allows for greater extracellular 5-HT levels, a faster onset of action, and greater efficacy as compared to other SSRIs. The sustained elevation of synaptic 5-HT eventually causes desensitization of 5-HT1A auto-receptors, which normally shut down endogenous 5-HT release in the presence of excess 5-HT - this desensitization may be necessary for the full clinical effect of SSRIs and may be responsible for their typically prolonged onset of action.

Esipral has shown little-to-no binding affinity at a number of other receptors, such as histamine and muscarinic receptors, and minor activity at these off-targets may explain some of its adverse effects.

Dosage

Esipral dosage

Adults: The initial dose of Esipral Oxalate is 10 mg once daily. (A fixed dose trial of Esipral Oxalate demonstrated the effectiveness of both 10 mg and 20 mg of Esipral Oxalate, but failed to demonstrate a greater benefit of 20 mg over 10 mg.)

If the dose is increased to 20 mg, this should occur after a minimum of one week.

Panic disorder: Adult over 18 years, initially 5 mg once daily increased to 10 mg daily after 7 days; max. 20 mg daily; elderly initially half adult dose, lower maintenance dose may be sufficient;

Social anxiety disorder: Adult over 18 years, initially 10 mg once daily adjusted after 2-4 weeks; usual dose 5-20 mg daily.

Elderly: A single oral dose of 10 mg/day is the recommended dose for most elderly patients. Administered in excess recommended dose has not been yet established.

Side Effects

Esipral is well tolerated by most people. The most commonly reported side-effects of Esipral are nausea, insomnia, problems with ejaculation, drowsiness, increased sweating and fatigue. Most of the side-effects experienced by patients taking Esipral are mild and go away with continued treatment and usually do not cause patients to stop taking Esipral.

Toxicity

Symptoms of overdose may include CNS effects (dizziness, convulsions, coma, somnolence), gastrointestinal distress (nausea, vomiting), and/or cardiac abnormalities (hypotension, tachycardia, ECG changes). There is no specific antidote for escitalopram overdose. Management of overdose should focus on monitoring for cardiac abnormalities and changes to vital signs as well as treatment with supportive measures as indicated. As escitalopram is highly distributed into tissue following oral administration, forced diuresis, dialysis, and other methods of extracting drug from plasma are unlikely to be beneficial.

Precaution

During marketing of escitalopram and other SSRIs and SNRIs (Serotonin and Norepinephrine Reuptake Inhibitors), there have been spontaneous reports of adverse events occurring upon discontinuation of these drugs, particularly when abrupt, including the following: dysphoric mood, irritability, agitation, dizziness, sensory disturbances (e.g., paresthesias such as electric shock sensations), anxiety, confusion, headache, lethargy, emotional lability, insomnia, and hypomania. While these events are generally self-limiting, there have been reports of serious discontinuation symptoms. Patients should be monitored for these symptoms when discontinuing treatment with escitalopram. A gradual reduction in the dose rather than abrupt cessation is recommended whenever possible. If intolerable symptoms occur following a decrease in the dose or upon discontinuation of treatment, then resuming the previously prescribed dose may be considered. Subsequently, the physician may continue decreasing the dose but at a more gradual rate.

Interaction

Esipral should not be started until 2 weeks after stopping an MAOI. Conversely, an MAOI should not be started until at least a week after escitalopram or related antidepressant has been stopped.

Food Interaction

  • Avoid alcohol. The combined use of alcohol with psychotropic medications should be avoided.
  • Take with or without food. The absorption is unaffected by food.

[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents.

Use in combination may result in additive central nervous system depression and
MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol.

Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

Volume of Distribution

Esipral appears to distribute extensively into tissues, with an apparent volume of distribution of approximately 12-26 L/kg.

Elimination Route

Absorption of escitalopram following oral administration is expected to be almost complete, with an estimated absolute bioavailability of approximately 80%. Tmax occurs after about 4-5 hours. Cmax and AUC appear to follow dose proportionality - at steady state, patients receiving 10mg of escitalopram daily had a Cmax of 21 ng/mL and a 24h AUC of approximately 360 ng*h/mL, while patients receiving 30mg daily had a roughly 3-fold increase in both Cmax and 24h AUC, comparatively.

Half Life

The elimination half-life of escitalopram is 27-32 hours, though this is increased by approximately 50% in the elderly and doubled in patients with reduced hepatic function. The elimination half-life of escitalopram's primary metabolite, S-desmethylcitalopram, is approximately 54 hours at steady state.

Clearance

The oral plasma clearance of escitalopram is 600 mL/min, of which approximately 7% is due to renal clearance.

Elimination Route

After oral administration of escitalopram, approximately 8% of the total dose is eliminated in the urine as unchanged escitalopram and 10% is eliminated in the urine as S-desmethylcitalopram. The apparent hepatic clearance of escitalopram amounts to approximately 90% of the total dose.

Pregnancy & Breastfeeding use

Pregnancy: The safety of escitalopram during pregnancy and lactation has not been established. Therefore, escitalopram should not be used during pregnancy unless, in the opinion of the physician, the expected benefits to the patient outweigh the possible hazards to the fetus.

Nursing Mothers: Esipral is excreted in human milk. Esipral should not be given to nursing mothers unless, in the opinion of the physician, the expected benefits to the patient outweigh the possible hazards to the child

Contraindication

Concomitant use in patients taking monoamine oxidase inhibitors (MAOIs) is contraindicated. Concomitant use in patients taking pimozide is contraindicated. Esita is contraindicated in patients with a hypersensitivity to escitalopram or citalopram or any of the inactive ingredients.

Special Warning

Pediatric Use: Safety and effectiveness in children below the age of 18 years have not been established.

Geriatric patients: Esipral pharmocokinetics in subjects age 65 and over were compared to younger subjects in a single and multi-dose study. No overall differences in safety or effectiveness between this group and the younger subjects was observed, but greater sensitivity of some elderly individuals ca

Storage Condition

Store in a cool and dry place below 30º C. Protect from light.

Innovators Monograph

You find simplified version here Esipral

Esipral contains Escitalopram see full prescribing information from innovator Esipral Monograph, Esipral MSDS, Esipral FDA label

FAQ

What is Esipral used for?

Esipral is mainly used to treat major depressive disorder or generalized anxiety disorder. Esipral is often used to treat depression and is sometimes used for anxiety, obsessive compulsive disorder or panic attacks.

How safe is Esipral?

For most people, Esipral is safe to take for a long time. A few people may get sexual side effects, such as problems getting an erection or a lower sex drive. In some cases these can continue even after stopping the Esipral.

How does Esipral work?

Esipral work by increasing the levels of a mood-enhancing chemical called serotonin in the brain.

What are the common side effects of Esipral?

Common side effects of Esipral are include:

Headache, nausea, diarrhea, dry mouth, increased sweating, feeling nervous, restless, fatigue, or having trouble sleeping (insomnia). These will often improve over the first week or two as you continue to take the medication.

Is Esipral safe during pregnancy?

Esipral has been linked to a very small increased risk of problems for your unborn baby. But if your depression isn't treated during pregnancy, this can also increase the chance of problems. You may need to take Esipral during pregnancy if you need it to remain well.

Is Esipral safe during breastfeeding?

The study shows that Esipral is safe for use during breastfeeding. Because its absolute infant dose is lower than that for an equivalent antidepressant dose of Esipral, it may be preferred over  Esipral in treating depression in lactating women.

Can I drink alcohol with Esipral?

You should avoid or limit the use of alcohol while being treated with Esipral.

Can I drive after taking Esipral?

Esipral might be best to stop driving and cycling for the first few days of treatment until you know how this medicine makes you feel.

When should be taken of Esipral?

You can take Esipral at any time of day, as long as you stick to the same time every day. If you have trouble sleeping, it's best to take it in the morning.

Can I take Esipral on an empty stomach?

You can take it with or without food.

How long does Esipral take to work?

Esipral usually takes 4 to 6 weeks for Esipral to work.

How long can I take Esipral?

Most people take Esipral for at least six months after they feel well again. This is to help guard against symptoms returning.

Can Esipral hurt me?

Esipral can cause a severe allergic reaction. Symptoms can include: trouble breathing. swelling of your face, tongue, eyes, or mouth.

Who should not take Esipral?

You should not take Esipral if you're hypersensitive to Esipral oxalate, meaning that you have a known allergy to the medication and experience symptoms of allergic reaction, such as difficulty breathing or swelling of the face, mouth, or tongue.

Is Esipral bad for my memory?

Esipral had no significant effect on WM accuracy or reaction time. Preliminary analysis of the imaging data revealed no significant differences in memory load dependent activation between conditions.

What happen If I oversose on Esipral?

Major manifestations of Esipral overdose were serotonin toxicity, QT prolongation, and bradycardia. The study suggests a potential for cardiac arrhythmias in escitalopram overdose.

What happen If I missed Esipral?

Missing doses of Esipral may increase your risk for relapse in your symptoms. Stopping Esipral abruptly may result in one or more of the following withdrawal symptoms: irritability, nausea, feeling dizzy, vomiting, nightmares, headache, and/or paresthesias.

What happens if I miss one day of my dose?

If you do miss 1 of your doses, skip the missed dose and take your next dose at the usual time. Do not take a double dose to make up for the dose you missed.

Can I take Esipral at night?

You can take Esipral at any time of day, as long as you stick to the same time every day. If you have trouble sleeping, it's best to take it in the morning.

Does barnd cause anxiety?

Low levels of Esipral in the brain may cause depression, anxiety, and sleep trouble. 

Can Esipral affect my heart?

Citalopram and Esipral, which fall into this drug group, can trigger a heart rhythm disturbance, a new study in the British Medical Journal shows.

Will Esipral affect my fertility?

Esipral use in women with a history of anxiety or depression diminishes natural fertility.

Can Esipral damage my kidneys?

If you taken Esipral without consultation with your physician, can cause kidney damage.

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