Last Updated on February 19, 2017 by Dr.Derek Fhisher
Most popular brand: Lexapro
Active ingredient: Escitalopram
Available dosage forms: 5, 10, 20 mg
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Escitalopram general information
Often utilized to heal the sort of depression called Seasonal Affective Disorder (SAD), including ADHD and as part of the stopping smoking programme. It is essentially a mood disorder that has numerous faces, as is the case with a number of other illnesses, for instance diabetes or cardiovascular disease. Actually, studies have demonstrated that one of the most typical triggers of migraine is truly because of stress. This is contained in the listing of depression medication since it’s a psychoactive drug. There are some tests with which the degree of depression and existence of depression could be assessed. Additionally, there are lots of different ways of handling depression and coming out of it.
SSRI medications are often prescribed for treating mood disorders like depression and anxiety. Additionally, This is among the most prescribed depression medicine which is used for treating clinical depression. Some individuals with seasonal affective disorder reap the benefits of treatment with antidepressants, particularly if symptoms are severe. Depression is yet another factor which has been confirmed in order to raise the severity and frequency of migraine attacks.
Being active is actually a healthy and holistic method of curbing stress. They’re also able to stimulate appetite, boost activity levels, as well as strengthen sleep. Even though it is true that exercise plays an essential role within our weight loss as well as weight maintenance, additionally it is known to boost mood. Magnesium deficiency is not uncommon for several surgical weight reduction patients and could lead to depression.
Imipramine is utilized in healing major depression, panic attacks and enuresis. Toxic blood levels can likewise occur if they’re taken with antiarrhythmic drugs. It directly increases the degree of serotonin. Lexapro also contributes to weight gain in certain patients, and weight gain is not uncommon among people who have sleep apnea.
Behavioral treatment seems to have long-lasting advantages. Additionally, they may be contraindicated for individuals with liver or kidney disease. While safer in certain respects compared to the MAOIs, the TCAs aren’t suggested for people who have glaucoma, cardiovascular disease, a history of seizures, hyperthyroidism, or urinary retention. Patients usually notice an improvement in 2-3 weeks and also the full impacts of the medication ought to be felt by 6 weeks.
Treatments are available and with the correct diagnosis you must be able enough to get your own life back to usual. Typically, they may be prescribed for a couple of months if you’re withdrawing from pain relief medications, to help reduce the frequency and seriousness of rebound headaches. At times, doctors may prescribe a mix of medications to accomplish the best results. Most of them are not utilizing any female baldness treatment and just few are aware of the current baldness treatments.
Omega-3 fatty acid supplements are shown to alleviate mild depression or anxiety symptoms in certain studies. This medication impacts the imbalanced neurotransmitters which cause depression. Any imbalance among these various neurotransmitters is the primary source of depression. Consequently, It is important to get sleep disorders treated. If there’s an imbalance within the chemicals, depression sets in and has to be conquered. You may also learn healthful methods to handle SAD and manage stress.
Atypical antidepressants are really so named because they don’t fit into the normal drug classes described above. These drugs are extremely simple to develop into dependent on or addicted to in this category of medications. Sometimes these beta-blockers are prescribed together with antidepressants.
As the majority of people are aware, nibbling on a bar of chocolate may earn a person more relaxed and it’s not merely on account of the sweet delectable taste this treat offers. Everyone you’ll provide you with with a distinct suggestion in accordance with their experience. Drinking water, washing your hands, and receiving enough sleep are important, but the very best thing you could do in order to prevent any type of flu is to enhance your immune system. Reduce or avoid the utilization of caffeine and other stimulants.
When a patient makes the decision to purchase Lexapro, it is likewise best to know its various medical applications. There are many precautions an individual must take before purchasing the medication. They’re also able to interact with several other drugs.
Your behavior at home starts to change in addition to work or with your family members. In summary, you really do not need to silently suffer with SAD. For starters, sleep problems can get worse with SSRI’s. Dawn simulation is just another light treatment, a dim light continues within the morning as you are sleeping, also it gets brighter over time, such as, for instance, a sunrise.
Prior to a patient makes the decision to purchase Lexapro, it is crucial to know its medical uses in addition to the way that it works. If someone makes the decision to acquire Lexapro, it’s always more advisable to find the approval of the doctor first. The aforementioned medicines can be taken just on doctor’s advice.
There are sure chemicals which balance someone’s mental condition. After the stress isn’t resolved, the entire body’s immune apparatus, digestive apparatus, cardiovascular and nervous system may be damaged. Dearth of exercise or walking is among the key causes. Once done, the extra Serotonin is reabsorbed.
Escitalopram *
Description of the active ingredient Escitalopram / Escitalopramum.
Formula: C20H21FN2O • C2H2O4, chemical name: S – (+) – 1 – [3 – (dimethylamino) propyl] – 1 – (p – fluorophenyl) – 5 – ftalankarbonitril (in the form of . oxalate)
Pharmacological group: neurotropic drugs / antidepressant
Mode of action:. antidepressant.
Pharmacological Properties
Escitalopram – antidepressant group of selective serotonin reuptake inhibitors, S – enantiomer of citalopram. It is believed that the mechanism of antidepressant action of escitalopram associated with inhibition of neuronal uptake of serotonin reverse, increasing its concentration in the synaptic cleft, resulting in increased and prolonged serotoninergic activity within the central nervous system. In studies in vivo on animals and in vitro demonstrated the ability of escitalopram highly selectively inhibit reverse neuronal uptake of serotonin in the central nervous system, the re-uptake of dopamine and noradrenaline escitalopram has minimal effect. Escitalopram at least 100 times more potent to inhibit serotonin reuptake than the R – enantiomer. In the simulation, the antidepressant effect of tolerance does not develop during prolonged (up to 5 weeks) to rats. Escitalopram has a very poor ability to communicate or interact with serotonin (5 – HT1-7), histamine (H1-3), dopamine (D1-5), benzodiazepine, muscarinic (M1-5) receptors, alpha – and beta – adrenergic receptors ( antagonism to histamine, muscarinic, adrenergic receptors, presumably, makes a variety of sedatives, anticholinergics, cardiovascular side effects of other psychotropic drugs). Also escitalopram it has a very low affinity or not bind to various ion channels, including sodium, potassium, calcium, chloride channels. The antidepressant effect of escitalopram usually develops after 2 – 4 weeks after initiation of therapy. Maximum therapeutic effect treatment of panic disorders is achieved after about 3 months after starting treatment
When receiving single and multiple doses. (Range 10 – 30 mg per day) has a dose-dependent pharmacokinetics escitalopram and linear. Oral solution and tablets that contain escitalopram oxalate are bioequivalent. Absorption of escitalopram is independent of food intake. Bioavailability is 80%. After a single oral 20 mg, the maximum concentration is reached after about 5 hours. Escitalopram is bound to plasma proteins for about 56%. The equilibrium concentration in serum while taking the drug once a day is set for about 7 days. In young healthy individuals escitalopram plasma concentration at steady state of 2.2 – 2.5 times higher than the concentration in a single dose. The average equilibrium concentration of 50 nmol / l (20 – 125 nmol / L), and reception is achieved at a dose of 10 mg per day. The apparent volume of distribution is 12 – 26 l / kg. Escitalopram is metabolized primarily in the liver with the formation of S – didemetiltsitaloprama (S – DDTST) and S – demetiltsitaloprama (S – DCT). in vitro studies using human liver microsomal enzymes indicate the involvement of isoenzymes CYP2C19 and CYP3A4 in the process of N – demethylation of escitalopram. In human serum escitalopram dominated unchanged. The concentration of S – demetiltsitaloprama serum at steady state is about 1/3 of the level of escitalopram. Level S – didemetiltsitaloprama in most subjects not determined. In in vitro studies have shown that inhibition of the serotonin reuptake escitalopram above that S – demetiltsitaloprama at least 7-fold, and S – didemetiltsitaloprama – 27 times. This indicates that the metabolites do not contribute significantly to the antidepressant action of escitalopram. S – didemetiltsitaloprama and S – demetiltsitaloprama also have a very poor ability to communicate or interact with serotonin (5 – HT1-7), histamine (H1-3), dopamine (D1-5), benzodiazepine, muscarinic (M1-5) receptors, alpha – and beta – adrenergic receptors, it does not bind to various ion channels, including sodium, potassium, calcium, chloride channels. In persons with a weak activity level escitalopram CYP2C19 isozyme may be two times higher than those with a high activity of this isoenzyme. No significant changes in the content of the drug in a weak CYP2D6 isoenzyme activity is not marked. Oral escitalopram clearance is 600 ml / min, of which about 7% – renal clearance. It was revealed that when administered escitalopram determined in the urine as unchanged (approximately 8%) and in the form of the S – demetiltsitaloprama – 10%. The terminal half-life of approximately 27 – 32 hours. In the main metabolites of escitalopram half-life is longer.
Options pharmacokinetics of escitalopram are comparable after single and repeated administration of the drug in people over 65 years old and young people. When receiving 10 mg escitalopram elderly about 50% increased half-life and area under the curve of concentration – time, the maximum concentration was unchanged
There were no differences in the values ​​of area under the concentration -. Time of maximum concentration, half-life in depending on the floor.
There is no information about the parameters of the pharmacokinetics of escitalopram in patients with severe renal insufficiency (with creatinine clearance less than 20 ml / min).
For most patients with impaired hepatic function The recommended dose is 10 mg escitalopram.
Indications
The depression, major depressive disorder, panic disorder (including with agoraphobia), generalized anxiety disorder.
How to use and dosages of escitalopram
Escitalopram is taken by mouth, with or without food once a day. Depending on the indication of the initial dose of 5 – 10 mg per day, the dose may be increased if necessary up to a maximum dose of 20 mg per day
For patients older than 65 years, the daily dose necessary to decrease by 50%: the initial dose is. 5 mg per day with a maximum – 10 mg per day
in patients with impaired hepatic function recommended starting dose for the first 14 days of treatment was 5 mg per day, more depending on the individual response of the patient the dose may be increased..
dose adjustments are not required in case of violation of renal function and mild to moderate severity.
The course of therapy lasting, established by the attending physician.
Depression and certain other psychiatric disorders are associated with an increased risk of suicide. When receiving antidepressants for treatment of major depressive disorder and other psychiatric disorders observed increased risk of suicidality (suicidal ideation, suicide attempts) compared with placebo in children, adolescents and young adults (18 to 24 years). It is necessary to evaluate the possible risk in the appointment of escitalopram or any other antidepressant in patients age groups. In adult patients older than 24 years at risk of suicidality antidepressants did not increase compared to placebo and in patients older than 65 years – is reduced, it is shown in short-term studies. During treatment with antidepressants should be closely monitored patients of all ages for the early detection of clinical deterioration, unusual changes in behavior or suicidal. Persons caring for patients and relatives of patients should be aware of the need for careful monitoring of patients and timely medical information. Escitalopram is not indicated for use in patients under 18 years.
At joint use of medicines from the group of SSRIs together with monoamine oxidase inhibitors were reported in patients developing serious, including fatal, reactions, including rigidity, hyperthermia , myoclonus, altered mental status (including excessive agitation, up to delirium and coma), unstable vital signs with possible rapid fluctuations. Also, these reactions were reported at the beginning of receiving monoamine oxidase inhibitors shortly after discontinuation of therapy with selective serotonin reuptake inhibitors. In some cases, the symptoms were similar to neuroleptic malignant syndrome. Also, limited information obtained in animal studies on the joint use of selective serotonin reuptake inhibitors and monoamine oxidase inhibitors, which show synergistic action of these drugs in relation to driving behavior and elevated blood pressure. Therefore it is impossible to combine escitalopram and monoamine oxidase inhibitors, or assign it within the first 14 days after their cancellation. Upon completion of a course of therapy with escitalopram and needed a break, at least 14 days prior to receiving monoamine oxidase inhibitors.
The doctor, who appoints escitalopram for long-term treatment, should periodically evaluate the usefulness of escitalopram for each patient, in spite of the fact that the efficiency of use of escitalopram for maintenance therapy in the treatment of depression has been demonstrated in a placebo -. controlled study lasting 36 weeks
patients who are taking escitalopram and other selective serotonin reuptake inhibitor, together with serotonergic agents, serotonin syndrome may develop. Caution should be used in conjunction with drug escitalopram, which have serotonergic activity. A combination of symptoms such as tremor, agitation, hyperthermia, myoclonus may indicate the development of serotonin syndrome. If this happens, the selective serotonin reuptake inhibitors and serotonergic drugs should be stopped immediately and symptomatic therapy is appointed.
There is information about the appearance of patients with reactions that are caused by the cancellation of escitalopram therapy or other selective serotonin reuptake inhibitors or reuptake inhibitors serotonin and norepinephrine, especially at sharp cancellation of the drug. These symptoms include: irritability, dysphoria, agitation, sensory disorders (including paraesthesia, electric shock sensation), dizziness, anxiety, headache, confusion, stupor, insomnia, emotional lability, hypomania. Therefore, to reduce the dose or cancel escitalopram should be gradually (for at least 1 – 2 weeks). To reduce the risk of withdrawal symptoms, while necessary to monitor the patient’s condition
There are reports of bleeding in patients when taking psychotropic drugs that affect on the reuptake of serotonin. It should warn patients about the need to be careful at simultaneous use of escitalopram with nonsteroidal anti-inflammatory drugs, including aspirin, or other drugs acting on the coagulation.
The therapy escitalopram reported cases of hyponatremia. Cases of hyponatremia and syndrome of inappropriate secretion of antidiuretic hormone were noted in the treatment of racemic citalopram. All patients returned to normal state when canceling escitalopram or citalopram and / or medical intervention.
In patients with depression treated with escitalopram, mania / hypomania has been noted. Escitalopram should be administered with caution to patients with mania in history. Escitalopram should be repealed in the development of mania.
There have been cases of seizures during clinical trials of escitalopram. Therefore, caution should appoint escitalopram in patients with a history of seizures. It should stop taking the drug with seizure development.
Limited clinical experience in the use of escitalopram in the presence of patients with comorbidity. It should be used with caution escitalopram in patients with diseases that are accompanied by violation of hemodynamics, or metabolism. In patients with unstable heart disease or myocardial infarction was not carried out systematic observations, because these patients were excluded from clinical studies premarketingovyh.
In animal shows low capacity citalopram cause addiction research. Not conducted systematic observations in humans to evaluate the feasibility of escitalopram induce tolerance, abuse, physical dependence. For patients who have a history of abusing drugs, require careful observation.
In controlled trials of escitalopram number of elderly patients was insufficient to adequately assess the safety and efficacy of escitalopram, depending on age. We can not exclude the possibility of increased sensitivity in some patients to escitalopram.
Some patients with panic disorder at the beginning of therapy with escitalopram may be exacerbated anxiety, usually disappearing within the next 2 weeks of treatment. To reduce the likelihood of developing anxiety is necessary to use low initial doses.
Escitalopram can increase glucose levels in the blood in diabetes mellitus, which may require changes in dosage of hypoglycemic agents.
During treatment with escitalopram is recommended to refuse to perform potentially hazardous activities requiring increased attention and psychomotor speed reactions (including vehicle control).
Contraindications
Hypersensitivity, co-administration of monoamine oxidase inhibitors, age under 18 years, pregnancy, breastfeeding.
Restrictions on the use
Kidney failure, manic disorder, hypomania, pharmacologically uncontrolled epilepsy, diabetes, depression with suicidal attempts, advanced age, liver cirrhosis, liver failure, bleeding tendency; concomitant use with drugs that reduce the seizure threshold; cause hyponatremia; metabolized by CYP2C19 with the system.
Pregnancy and breastfeeding
The use of escitalopram during pregnancy is possible if the supposed effect of treatment for the mother above the possible risk to the fetus. Strictly controlled and adequate studies safety of escitalopram were not carried out in pregnant women.
In studies in pregnant rats administered escitalopram, since late pregnancy until weaning, at doses of 6, 12, 24, 48 mg / kg day. At a dose of 48 mg / kg per day (about 24 times the maximum recommended human dose, calculated in mg / m2) had stunted growth, increased offspring mortality toxicity parent organism (clinical signs, reduction in food intake and body weight gain ). The dose of 12 mg / kg per day, at which no negative effects were observed, approximately 6 times the maximum recommended human dose, calculated in mg / m2.
Also, pregnant rats were administered the drug during the period of organogenesis at doses 56, 112 or 150 mg / kg per day. At doses of 112 or 150 mg / kg per day (about 56 times the maximum recommended human dose – 20 mg per day, calculated in mg / m2) had weight loss and ossification delay fruit. At all doses, the toxicity observed for the maternal organism (clinical signs, reduction in food intake and body weight gain). The dose of 56 mg / kg per day, at which no impact on fetal development, about 28 times the maximum recommended human dose, calculated in mg / m2. Under one of the doses tested (up to more than 75 times the maximum recommended human dose, based in mg / m2) showed no teratogenicity.
In newborns who were exposed to escitalopram at the end of III trimester of pregnancy, developed complications which required tube feeding, respiratory support, prolongation of hospitalization. These complications can develop immediately after delivery. Reported symptoms included: cyanosis, respiratory distress, apnea, unstable temperature, convulsions, difficulty in feeding, hypoglycemia, vomiting, hypotonia, tremor, hyperreflexia, nervous excitement, constant crying, irritability. These symptoms are associated with the direct toxic effects of the drug, or are manifestations of withdrawal reactions in the newborn.
Overdose
There is no specific antidote.
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