3/30/2017 0 Comments Ssri Weight Loss Or GainAntidepressants: Comparison of SSRIs. Selective Serotonin Reuptake Inhibitors (SSRIs) The most significant class of antidepressants marketed in recent years is the selective serotonin reuptake inhibitors (SSRIs). The six SSRIs available in the United States are: citalopram (Celexa)escitalopram (Lexapro)fluoxetine (Prozac)fluvoxamine (Luvox)paroxetine (Paxil)sertraline (Zoloft)The SSRIs represent the first rationally designed class of psychotropic medications. The strategy behind rational drug development is to design a new drug that is capable of affecting a specific neural site of action (eg, uptake pumps, receptors) while avoiding effects on other site of actions. The goal in such development is to produce agents that are more efficacious, safer and better tolerated than older medications. All SSRIs are non- controlled substances. Although all SSRI drugs have the same mechanism of action, each SSRI has slightly different pharmacological and pharmacokinetic characteristics. This leads to differences among the SSRIs in their half- lives, clinical activity, side effects, and drug interactions. There are differences between SSRIs that could be clinically significant. What Is the Best Antidepressant for Weight Loss. Antidepressants and weight gain are linked. Learn which antidepressants likely cause weight gain. How to Counter Weight Gain from Antidepressants. No matter what the cause of the weight gain, the basic formula for weight loss remains. Also, SSRIs have very different molecular structures. Brief history. The first drug in the SSRI class was Prozac (Fluoxetine), which hit the United States market in 1. Prozac was FDA approved in December 2. It is manufactured by Eli Lilly and Company. Zoloft (Sertraline hydrochloride) was the second SSRI to come to market in the United States, and it was approved by the FDA in December 3. Zoloft is manufactured by Pfizer Inc. Paxil (Paroxetine hydrochloride) was the third SSRI to come to market in the United States and was approved by the FDA in December 2. Paxil is manufactured by Glaxo. Smith. Kline. Chemical structure of Paroxetine differs from other SSRIs by having a piperidine ring. Luvox (Fluvoxamine maleate) was the next SSRI FDA approved in December 0. However, now its marketing status is . Starting Antidepressants? About the Weight Gain. Like hair loss during chemotherapy, weight gain while on. You don't agree that Ssri's can cause weight gain? The Latest About Antidepressants and Weight Gain. The drugs with the lowest the rate of weight gain were bupropion (Wellbutrin. Celexa is manufactured by Forest Pharmaceuticals, Inc. Lexapro (Escitalopram oxalate) is the newest and most selective of the SSRIs approved by the FDA in August 1. Lexapro is manufactured by Forest Pharmaceuticals, Inc. Lexapro is a cleaner, improved version of Celexa. It is the active isomer of racemic citalopram. Brief SSRIs comparison table Citalopram (Celexa)Escitalopram (Lexapro)Fluoxetine (Prozac)Paroxetine (Paxil)Sertraline (Zoloft)FDA approval date. July 1. 7, 1. 99. August 1. 4, 2. 00. December 2. 9, 1. December 2. 9, 1. December 3. 0, 1. Pharmaceutical Forms. L5mg, 1. 0mg, 2. 0mg tablets,oral solution 5 mg/5 m. L 1. 0mg tablets, 1. L,weekly capsules 9. L2. 5mg, 5. 0mg, 1. LRecommended dose (for Major Depressive Disorder)2. Neurotransmitters. Research suggests that. SSRIs seem to. relieve symptoms of depression by blocking the reabsorption (reuptake). This leaves more serotonin. SSRIs. are called selective because they seem to affect serotonin significantly. Thus, the medications work by allowing. In due course, the levels of natural serotonin will. SSRI can be reduced and withdrawn. SSRI antidepressants are at least 1. However, SSRIs differ in their potency and selectivity in inhibiting serotonin reuptake and many of them have important effects on other transporters and receptors. Each SSRI has. a unique profile of multiple pharmacologic actions, which. Binding properties of SSRIs. Citalopram (Celexa)most selective serotonin reuptake inhibitor. Escitalopram (Lexapro)most selective serotonin reuptake inhibitor. Fluoxetine (Prozac)least selective serotonin reuptake inhibitornorepinephrine reuptake 1. C receptors 2. 1cytochrome P4. D6cytochrome P4. 50 3. A4 Paroxetine (Paxil)the most potent serotonin reuptake blocker, but has a low selectivity for the serotonin reuptakemuscarinic cholinergic receptors (most potent blocker of muscarinic. SSRIs)histamine H1 receptorsnitric oxide synthasecytochrome P4. D6 Sertraline (Zoloft)the second most potent inhibitor of serotonin reuptake and the second most selective blocker of serotonin over noradrenaline uptakedopamine reuptake (more potent dopamine uptake inhibitor than. SSRIs) 2. 2norepinephrine reuptakesigma receptors Approved indications and uses. All the SSRIs are licensed for major depressive disorder and are considered to be the first- line treatments of depression. Each antidepressant produces approximately. However, some differences in the SSRIs efficacy exist. Escitalopram may be superior in efficacy compared with other SSRIs in. Also escitalopram has. Paroxetine, fluoxetine, and sertraline are similar in effectiveness for major depression and depression. Paroxetine is the only SSRI indicated for all five anxiety disorders in addition to major depressive disorder. Fluoxetine has a slower onset of antidepressant effect than other SSRIs. Sertraline. has advantages over paroxetine in the treatment of panic disorder. Interesting and important fact is that SSRI antidepressants are not. Persons who discontinue one SSRI for the lack of tolerability. Comparison of SSRI's side effects. As a group, the SSRIs possess the following adverse effects: nauseasexual dysfunction, including decreased libido, orgasm difficulties, abnormal ejaculationdiarrheaheadachenervousnessinsomniaagitationsweatingdry mouthtachycardiaanorexiaincreased appetiteweight gainanxietyinsomniadrowsiness. While SSRIs do not appear to differ in overall tolerability, the reported incidences of specific side effects vary. Paroxetine and sertraline have been associated. Sexual dysfunction. The SSRIs as a class produce a variety of sexual side effects, including anorgasmia, decreased. Analysis of the clinical trials suggests that fluvoxamine and fluoxetine are less likely to. Paroxetine appears to cause the highest rate of sexual. Citalopram has been associated with loss of libido and may be associated with a relatively higher. The SSRIs are reported to cause sexual dysfunction in the following descending order of frequency: citalopram 7. Paroxetine produces more delay of orgasm or ejaculation than fluvoxamine. Weight gain. Weight gain is another troubling side effect. The SSRIs vary in their effect on the weight. Paroxetine, fluoxetine, citalopram and sertraline have been shown. Fluoxetine, paroxetine, and sertraline delay the onset of REM sleep, and fluoxetine and paroxetine increase awakenings and reduce REM sleep, slow- wave sleep, total sleep time, and sleep efficiency. In contrast, sertraline minimally increases sleep efficiency and reduces nocturnal wakefulness time, which may benefit depressed patients with sleep disturbances. Anticholinergic effects. Paroxetine, like the TCAs desipramine and imipramine, has an in vitro affinity for the muscarinic cholinergic. As a result, paroxetine causes a higher rate of anticholinergic effects, such as dry mouth, constipation. SSRIs. These effects may be particularly difficult to tolerate for elderly. Diarrhea. Sertraline and fluoxetine are more frequently associated with diarrhea due to their greater specificity for serotonin. Recently, sertraline has been. SSRIs. 7. Anxiety, agitation, insomnia. Fluoxetine has been associated with highest rate of anxiety and agitation. Escitalopram and citalopram. The possible increased potential for agitation and/or stimulatory side effects is difficult to put in perspective, as. However, if SSRI- induced agitation. Dry mouth. Citalopram and paroxetine are more likely to cause dry mouth than escitalopram and fluoxetine. Drowsiness, fatigue. Paroxetine has been associated with highest rate of drowsiness, somnolence than other SSRIs. Headache. Sertraline and fluoxetine are associated with higher level of headache. QT interval prolongation. Citalopram has a higher risk of QT interval prolongation than other SSRIs. Discontinuation symptoms (withdrawal)SSRIs aren't considered addictive. However, stopping treatment abruptly or missing several doses can cause discontinuation. All antidepressants do not have the same type or severity of withdrawal symptoms. The incidence of discontinuation syndrome is highest with paroxetine followed by fluvoxamine and sertraline. Citalopram and fluoxetine have a lower occurrence of withdrawal symptoms. Abrupt interruption of antidepressant therapy for 5- 8 days was associated with the emergence of new somatic and psychological symptoms in patients treated with paroxetine and to a lesser degree sertraline, with few symptoms seen with fluoxetine. Pregnancy category. All SSRIs (except paroxetine) are classified as pregnancy Category C, meaning that they may not be safe for use during pregnancy. Paroxetine (Paxil, Paxil CR) is pregnancy Category D medication. Paroxetine may cause heart defects or serious, life- threatening lung problems in newborn babies whose mothers take the medication during pregnancy. Drug interactions. Marked differences exist between the SSRIs with regard to effects on specific CYP enzymes and, thus, the likelihood of clinically important pharmacokinetic drug- drug interactions. The potency of the SSRIs as inhibitors of the metabolism of the P4. P2- D6. varies and is reported in descending order of potency as paroxetine. Paroxetine is the most potent inhibitor of the cytochrome P4. D6 enzyme of all antidepressants. Fluoxetine and. paroxetine are more likely to cause P4. P4. 50 2. D6 isoenzyme (e. IC antiarrhythmics). Drug interactions with clinical consequences usually involve combinations. SSRI with other psychotropics, especially monoamine oxidase inhibitors. MAOIs) and tricyclic antidepressants, clozapine, lithium, methadone. The interaction between MAOIs and SSRIs is the most important drug. SSRI use. This combination may lead to the development. At least 1. 4 days should be allowed after. MAOI. This difference in washout time between fluoxetine and citalopram. SSRI. to an MAOI is one of the key differences between SSRIs. Sertraline, citalopram and escitalopram have the lowest potential for. SSRIs, and are to be preferred in patients. SSRI to other psychotropic medication.
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