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Reuptake

Consistent with the abiUty of vinpocetine to act as an anticonvulsant is its abiUty to inhibit cellular reuptake of adenosine (15) which has been described as the brain s endogenous anticonvulsant because of its abiUty to inhibit calcium influx. Thus the property of vinpocetine to inhibit adenosine reuptake maybe responsible for the neuroprotective actions of the dmg. [Pg.93]

Dopamine. Dopamine (DA) (2) is an intermediate in the synthesis of NE and Epi from tyrosine. DA is localized to the basal ganglia of the brain and is involved in the regulation of motor activity and pituitary hormone release. The actions of DA are terminated by conversion to dihydroxyphenylacetic acid (DOPAC) by monoamine oxidase-A and -B (MAO-A and -B) in the neuron following reuptake, or conversion to homovanillic acid (HVA) through the sequential actions of catechol-0-methyl transferase (COMT) and MAO-A and -B in the synaptic cleft. [Pg.540]

L-tryptophan by hydroxylation to 5-hydroxy-L-tryptophan by the enzyme, ttyptophan-5-hydroxylase. 5-Hydroxy-L-tryptophan is then rapidly decarboxylated by aromatic-L-amino acid deacarboxylase to 5-HT. The actions of 5-HT as a neurottansmitter ate terminated by neuronal reuptake and metabobsm. [Pg.569]

Beginning in the 1960s, ben2odia2epiae anxiolytics and hypnotics rapidly became the standard prescription dmg treatment. In the 1980s, buspkone [36505-84-7] (3), which acts as a partial agonist at the serotonin [50-67-9] (5-hydroxytryptamine, 5-HT) type lA receptor, was approved as treatment for generali2ed anxiety. More recently, selective serotonin reuptake inhibitors (SSRIs) have been approved for therapy of panic disorder and obsessive—compulsive behavior. [Pg.218]

SSRIs are well tolerated. Adverse effects for compounds in this class include nervousness, tremor, dizziness, headache, insomnia, sexual dysfunction, nausea, and diarrhea. In addition, the tricycHc antidepressant clomipramine (33), which is a potent nonselective serotonin reuptake inhibitor, is approved for treatment of obsessive—compulsive disorder. [Pg.227]

Treatment of Major Depression. Dmgs commonly used for the treatment of depressive disorders can be classified heuristicaHy iato two main categories first-generation antidepressants with the tricycHc antidepressants (TCAs) and the irreversible, nonselective monoamine—oxidase (MAO) inhibitors, and second-generation antidepressants with the atypical antidepressants, the reversible inhibitors of monoamine—oxidase A (RIMAs), and the selective serotonin reuptake inhibitors (SSRIs). Table 4 fists the available antidepressants. [Pg.229]

Venlafaxine (48) is a stmcturaHy novel phenylethylamine derivative that strongly inhibits both noradrenaline and serotonin reuptake. It lacks anticholinergic, antihistaminergic, and antiadrenergic side effects. As compared to placebo, most common adverse events are nausea, somnolence, dizziness, dry mouth, and sweating. Venlafaxine-treated patients also experienced more headaches and nausea, but less dry mouth, dizziness, and tremor than patients treated with comparator antidepressants. [Pg.232]

Other agents are also used for the treatment of manic-depressive disorders based on preliminary clinical results (177). The antiepileptic carbamazepine [298-46-4] has been reported in some clinical studies to be therapeutically beneficial in mild-to-moderate manic depression. Carbamazepine treatment is used especially in bipolar patients intolerant to lithium or nonresponders. A majority of Hthium-resistant, rapidly cycling manic-depressive patients were reported in one study to improve on carbamazepine (178). Carbamazepine blocks noradrenaline reuptake and inhibits noradrenaline exocytosis. The main adverse events are those found commonly with antiepileptics, ie, vigilance problems, nystagmus, ataxia, and anemia, in addition to nausea, diarrhea, or constipation. Carbamazepine can be used in combination with lithium. Several clinical studies report that the calcium channel blocker verapamil [52-53-9] registered for angina pectoris and supraventricular arrhythmias, may also be effective in the treatment of acute mania. Its use as a mood stabilizer may be unrelated to its calcium-blocking properties. Verapamil also decreases the activity of several neurotransmitters. Severe manic depression is often treated with antipsychotics or benzodiazepine anxiolytics. [Pg.233]

Future Outlook for Antidepressants. Third-generation antidepressants are expected to combine superior efficacy and improved safety, but are unlikely to reduce the onset of therapeutic action in depressed patients (179). Many dmgs in clinical development as antidepressive agents focus on estabhshed properties such as inhibition of serotonin, dopamine, and/or noradrenaline reuptake, agonistic or antagonistic action at various serotonin receptor subtypes, presynaptic tt2-adrenoceptor antagonism, or specific monoamine—oxidase type A inhibition. Examples include buspirone (3) (only... [Pg.233]

Selected for clinical trials as a compound to calm agitated patients, imipramine was relatively ineffective. However, it was observed to be effective in the treatment of certain depressed patients (38). Early studies on the mechanism of action showed that imipramine potentiates the effects of the catecholamines, primarily norepinephrine. This finding, along with other evidence, led to the hypothesis that the compound exerts its antidepressant effects by elevating norepinephrine levels at central adrenergic synapses. Subsequent studies have shown that the compound is a potent inhibitor of norepinephrine reuptake and, to a lesser extent, the uptake of serotonin, thus fitting the hypothesis that had been developed to explain the antidepressant actions ofMAOIs. [Pg.467]

Desipramine [50-47-5] (35) and nortriptyline [72-69-5] (36) are demethylated derivatives and principal metaboHtes of (32) and (33), respectively. Both compounds possess less sedative and stronger psychomotor effects than the tertiary amine counterparts, probably because tricycHcs containing secondary amine groups generally show greater selectivity for inhibiting the reuptake of norepinephrine compared with the reuptake of serotonin. Protriptyline [438-60-8] (37), a stmctural isomer of nortriptyline, is another important secondary amine that displays a similar clinical profile. [Pg.467]

Selective Serotonin Reuptake Inhibitors. In 1987, the FDA approved fluoxetine [54910-89-3] (42) for use in the treatment of major... [Pg.468]

Most of the widely used antidepressants are tricyclics related to imipramine. A 1-phenyltetrahy-droisoquinoline analogue, nomifensine (60), departs from this structural pattern. Hiarmacologi-cally it inhibits the reuptake of catecholamines such as dopamine at neurons. It can be synthesized by alkylation of 2-nitrobenzyl-methylamine with phenacyl bromide followed by catalytic reduction of the nitro group (Pd-C) and then hydride reduction of the keto moiety to give 59. Strong acid treatment leads to cyclodehydration to nomifensine (60) [17]. [Pg.146]

Antidepressants Noradrenaline/5-HT transporters Na+, K+ channels l Noradrenaline/ 5-HT reuptake l Na+ currents t K+ currents l Excitability of peripheral and central neurons Cardiac arrhythmia, myocardial infarction, sedation, nausea, dry mouth, constipation, dizziness, sleep disturbance, blurred vision... [Pg.76]

Antidepressants are used in the treatment of neuropathic pain and headache. They include the classic tricyclic compounds and are divided into nonselective nor-adrenaline/5-HT reuptake inhibitors (e.g., amitriptyline, imipramine, clomipramine, venlafaxine), preferential noradrenaline reuptake inhibitors (e.g., desipramine, nortriptyline) and selective 5-HT reuptake inhibitors (e.g., citalopram, paroxetine, fluoxetine). The reuptake block leads to a stimulation of endogenous monoaminer-gic pain inhibition in the spinal cord and brain. In addition, tricyclics have NMDA receptor antagonist, endogenous opioid enhancing, Na+ channel blocking, and K+ channel opening effects which can suppress peripheral and central sensitization. Block of cardiac ion channels by tricyclics can lead to life-threatening arrhythmias. The selective 5-HT transporter inhibitors have a different side effect profile and are safer in cases of overdose [3]. [Pg.77]

Sibutramine (Table 1) has been in the market for several years and inhibits the reuptake of serotonin, noradrenaline and, to a lesser extent, dopamine. It acts... [Pg.159]

Mode of action Enzyme inhibition Reuptake inhibition Receptor antagonism... [Pg.159]

The principal mechanism for terminating dopamine signaling is reuptake by the presynaptic neuron via the dopamine transporter (DAT). Dopamine that is not taken up is metabolized by the enzymes monoamine oxidase (MAO) and catechol-O-methyl transferase... [Pg.439]

Cholera toxin-induced diarrhoea 2. Increased AEA levels after administration of cholera toxin to mice, a model of diarrhoea, exert anti-secretory action in the small intestine 2. Inhibitors of cellular reuptake... [Pg.467]


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5-HT reuptake inhibitor

5-HT-selective reuptake inhibitors

Adenosine reuptake inhibitors

Agonists, Antagonists, and Reuptake Blockers

Alkaloids reuptake inhibitors

Amine reuptake blockers

Antidepressants reuptake inhibitors

Antidepressants selective noradrenaline reuptake inhibitor

Antidepressants selective norepinephrine reuptake inhibitors

Antidepressants selective serotonin reuptake

Antidepressants selective serotonin reuptake inhibitors

Antidepressants serotonin reuptake inhibitors

Antidepressants serotonin-norepinephrine reuptake inhibitors

Antidepressants serotonin/noradrenaline reuptake inhibitor

Antipsychotic drugs selective serotonin reuptake inhibitors with

Antipsychotic drugs serotonin reuptake inhibitors

Anxiety selective serotonin reuptake inhibitors

Attention deficit disorder selective norepinephrine reuptake inhibitors

Catecholamine reuptake pump

Children selective serotonin reuptake

DA reuptake

Depression selective noradrenaline reuptake inhibitors

Depression selective serotonin reuptake inhibitors

Depression serotonin reuptake inhibitor

Depressive disorders selective serotonin reuptake inhibitors

Dopamine and norepinephrine reuptake inhibitors

Dopamine release/inhibiting reuptake

Dopamine reuptake

Dopamine reuptake blockers

Dopamine reuptake inhibitors

Dopamine reuptake inhibitors cocaine

Dopamine reuptake transporter

Dopamine- selective reuptake

Dopamine- selective reuptake antidepressants

Dopamine- selective reuptake inhibitors

Drug interactions norepinephrine reuptake inhibitors

Dual serotonin-dopamine reuptake inhibitors

Dual serotonin-norepinephrine reuptake

Dual serotonin-norepinephrine reuptake inhibitors

Fatigue, selective norepinephrine reuptake

Filtration, secretion, reuptake

GABA reuptake inhibitor

Glutamate reuptake

Inhibition serotonin reuptake

Inhibitors, monoamine reuptake

Insomnia selective serotonin reuptake inhibitors

Medication serotonin reuptake inhibitors specific

Medications selective serotonin reuptake inhibitors

Mirtazapine selective serotonin reuptake inhibitors with

Monoamine transporters neurotransmitters reuptake

Monoamine transporters serotonin reuptake inhibitor

NDRIs (norepinephrine dopamine reuptake

NRIs reuptake inhibitors

NSRIs reuptake inhibitors

Nefazodone selective serotonin reuptake inhibitors with

Neurons neurotransmitter reuptake

Neurotransmitter reuptake inhibitor

Neurotransmitters neurotransmitter reuptake

Non-selective Monoamine Reuptake Inhibitor

Nonselective serotonin reuptake

Nonselective serotonin reuptake inhibitors

Noradrenaline reuptake

Noradrenaline reuptake inhibition

Noradrenaline reuptake inhibitors

Noradrenaline reuptake inhibitors NARIs)

Noradrenaline reuptake inhibitors side effects

Noradrenergic reuptake inhibitors

Norepinephrine Reuptake Inhibitors

Norepinephrine dopamine reuptake inhibitors

Norepinephrine reuptake antagonists

Norepinephrine reuptake bupropion effects

Norepinephrine reuptake inhibitor (SNRI

Norepinephrine reuptake inhibitors, drug

Norepinephrine reuptake transporter

Norepinephrine reuptake with serotonin inhibition

Norepinephrine-reuptake inhibitors pharmacological properties

Norepinephrine-reuptake inhibitors side effects

Obsessive-compulsive disorder selective serotonin reuptake inhibitors

Panic disorder selective serotonin reuptake inhibitors

Pharmacology serotonin reuptake

Posttraumatic stress disorder selective serotonin reuptake inhibitors

Reboxetine selective serotonin reuptake inhibitors with

Reuptake Dual Selective Serotonin Norepinephrine

Reuptake Norepinephrine

Reuptake SSNRI

Reuptake Transporter

Reuptake active transport

Reuptake blocking

Reuptake inhibitor

Reuptake neurotransmitter

Reuptake serotonin

Reuptake tricyclic antidepressant action

Reuptake, dopamine/norepinephrine

Reuptake, dopamine/norepinephrine action terminated

Reuptake, inhibition

SNRI (serotonin norepinephrine reuptake

SNRIs (serotonin-norepinephrine reuptake

SNRIs reuptake inhibitors

SSNRI (selective serotonin norepinephrine Reuptake

SSRIs (selective serotonin reuptake

SSRIs (selective serotonin reuptake side effects

SSRIs (serotonin reuptake

SSRIs (serotonin reuptake side effects

SSRIs reuptake inhibitors

SSRls (selective serotonin reuptake

Schizophrenia Selective serotonin reuptake inhibitors

Selected serotonin reuptake inhibitors

Selective Serotonin-Norepinephrine Reuptake Inhibitors

Selective Serotonine Reuptake Inhibitors

Selective noradrenaline reuptake

Selective noradrenaline reuptake inhibitors

Selective noradrenergic reuptake

Selective noradrenergic reuptake inhibitors

Selective norepinephrine reuptake inhibitors

Selective norepinephrine reuptake inhibitors action

Selective norepinephrine reuptake inhibitors depression

Selective norepinephrine reuptake inhibitors efficacy

Selective norepinephrine reuptake inhibitors response

Selective norepinephrine reuptake inhibitors side effects

Selective serotonin and norepinephrine reuptake inhibitors

Selective serotonin reuptake

Selective serotonin reuptake 5-Hydroxytryptamine

Selective serotonin reuptake Prozac

Selective serotonin reuptake activation effects

Selective serotonin reuptake adverse effects

Selective serotonin reuptake fluoxetine

Selective serotonin reuptake fluoxetine, paroxetine, sertraline)

Selective serotonin reuptake indications

Selective serotonin reuptake inhibitor behavioral

Selective serotonin reuptake inhibitor metabolic

Selective serotonin reuptake inhibitors

Selective serotonin reuptake inhibitors (SSRIs side effects

Selective serotonin reuptake inhibitors . See

Selective serotonin reuptake inhibitors Citalopram Fluoxetine

Selective serotonin reuptake inhibitors Fluvoxamine Paroxetine Sertraline

Selective serotonin reuptake inhibitors MAOIs

Selective serotonin reuptake inhibitors MDMA)

Selective serotonin reuptake inhibitors SSRIs)

Selective serotonin reuptake inhibitors about

Selective serotonin reuptake inhibitors action

Selective serotonin reuptake inhibitors administration

Selective serotonin reuptake inhibitors adverse effects

Selective serotonin reuptake inhibitors alprazolam

Selective serotonin reuptake inhibitors amphetamines

Selective serotonin reuptake inhibitors analysis

Selective serotonin reuptake inhibitors and

Selective serotonin reuptake inhibitors anxiety disorders

Selective serotonin reuptake inhibitors anxiety from

Selective serotonin reuptake inhibitors anxiety with

Selective serotonin reuptake inhibitors anxiolytics

Selective serotonin reuptake inhibitors benzodiazepines

Selective serotonin reuptake inhibitors buspirone

Selective serotonin reuptake inhibitors characteristics

Selective serotonin reuptake inhibitors chemical structures

Selective serotonin reuptake inhibitors children

Selective serotonin reuptake inhibitors citalopram

Selective serotonin reuptake inhibitors classification

Selective serotonin reuptake inhibitors clinical trials

Selective serotonin reuptake inhibitors clozapine

Selective serotonin reuptake inhibitors death

Selective serotonin reuptake inhibitors depression from

Selective serotonin reuptake inhibitors discontinuation

Selective serotonin reuptake inhibitors discontinuation syndrome

Selective serotonin reuptake inhibitors dosing

Selective serotonin reuptake inhibitors drug administration

Selective serotonin reuptake inhibitors drug interactions

Selective serotonin reuptake inhibitors drug overdose

Selective serotonin reuptake inhibitors drug withdrawal

Selective serotonin reuptake inhibitors drugs

Selective serotonin reuptake inhibitors during pregnancy

Selective serotonin reuptake inhibitors effects

Selective serotonin reuptake inhibitors efficacy

Selective serotonin reuptake inhibitors enantiomers

Selective serotonin reuptake inhibitors enhanced

Selective serotonin reuptake inhibitors escitalopram

Selective serotonin reuptake inhibitors extended-release

Selective serotonin reuptake inhibitors fluoxetine

Selective serotonin reuptake inhibitors fluvoxamine

Selective serotonin reuptake inhibitors gastrointestinal

Selective serotonin reuptake inhibitors general

Selective serotonin reuptake inhibitors haloperidol

Selective serotonin reuptake inhibitors hyponatremia with

Selective serotonin reuptake inhibitors immediate

Selective serotonin reuptake inhibitors in children

Selective serotonin reuptake inhibitors in children and adolescents

Selective serotonin reuptake inhibitors in obsessive-compulsive disorder

Selective serotonin reuptake inhibitors indications

Selective serotonin reuptake inhibitors interactions

Selective serotonin reuptake inhibitors labeling

Selective serotonin reuptake inhibitors lactation

Selective serotonin reuptake inhibitors limits

Selective serotonin reuptake inhibitors lithium

Selective serotonin reuptake inhibitors liver

Selective serotonin reuptake inhibitors long-term effects

Selective serotonin reuptake inhibitors mediation

Selective serotonin reuptake inhibitors metabolism

Selective serotonin reuptake inhibitors moclobemide

Selective serotonin reuptake inhibitors monoamine oxidase

Selective serotonin reuptake inhibitors mood disorders from

Selective serotonin reuptake inhibitors nefazodone

Selective serotonin reuptake inhibitors nervous system

Selective serotonin reuptake inhibitors olanzapine

Selective serotonin reuptake inhibitors overdose

Selective serotonin reuptake inhibitors overview

Selective serotonin reuptake inhibitors paroxetine

Selective serotonin reuptake inhibitors pharmacodynamic

Selective serotonin reuptake inhibitors pharmacokinetic

Selective serotonin reuptake inhibitors pharmacology

Selective serotonin reuptake inhibitors pindolol

Selective serotonin reuptake inhibitors risperidone

Selective serotonin reuptake inhibitors second-generation effects

Selective serotonin reuptake inhibitors selectivity differences

Selective serotonin reuptake inhibitors sertraline

Selective serotonin reuptake inhibitors structure

Selective serotonin reuptake inhibitors suicidality from

Selective serotonin reuptake inhibitors toxicity

Selective serotonin reuptake inhibitors tramadol

Selective serotonin reuptake inhibitors trazodone

Selective serotonin reuptake inhibitors tricyclic antidepressant interactions with

Selective serotonin reuptake inhibitors tricyclic antidepressants

Selective serotonin reuptake inhibitors triptans

Selective serotonin reuptake inhibitors venlafaxine

Selective serotonin reuptake inhibitors with stimulants

Selective serotonin reuptake inhibitors withdrawal

Selective serotonin reuptake inhibitors withdrawal from

Selective serotonin reuptake inhibitors, 128 sumatriptan

Selective serotonin reuptake interactions

Selective serotonin reuptake management

Selective serotonin reuptake pharmacological properties

Selective serotonin reuptake receptor

Selective serotonin reuptake risks

Selective serotonin reuptake side effects

Selective serotonin reuptake with antipsychotics

Selective serotonin reuptake with monoamine oxidase

Selective serotonin reuptake with tricyclic antidepressants

Selective serotonin reuptake withdrawal

Serotonin and noradrenalin reuptake

Serotonin and noradrenalin reuptake inhibitors

Serotonin and noradrenaline reuptake

Serotonin and noradrenaline reuptake inhibition

Serotonin and noradrenaline reuptake inhibitors

Serotonin and norepinephrine reuptake inhibitors

Serotonin and norepinephrine reuptake inhibitors SNRIs)

Serotonin antagonist reuptake inhibitor

Serotonin antagonists and reuptake inhibitors

Serotonin neuronal reuptake

Serotonin noradrenaline reuptake

Serotonin noradrenergic reuptake inhibitors

Serotonin norepinephrine reuptake inhibitors

Serotonin reuptake blocked

Serotonin reuptake channel

Serotonin reuptake enhancers

Serotonin reuptake inhibitors

Serotonin reuptake inhibitors agitation caused

Serotonin reuptake inhibitors effects

Serotonin reuptake inhibitors patients with depression

Serotonin reuptake inhibitors receptor specificity

Serotonin reuptake inhibitors seizures caused

Serotonin reuptake inhibitors toxicity

Serotonin reuptake inhibitors, selective dosage

Serotonin reuptake inhibitors, selective interaction with other drugs

Serotonin reuptake inhibitors, selective pharmacokinetics

Serotonin reuptake inhibitors, selective side effects

Serotonin reuptake transporter

Serotonin reuptake transporters (SERT

Serotonin-norepinephrine reuptake

Serotonin-norepinephrine reuptake dosage

Serotonin-norepinephrine reuptake inhibitor SNRI)

Serotonin-norepinephrine reuptake inhibitor drug

Serotonin-norepinephrine reuptake inhibitors SNRIs)

Serotonin-norepinephrine reuptake pharmacokinetics

Serotonin-norepinephrine reuptake relative potency

Serotonin-norepinephrine reuptake side effects

Serotonin-selective reuptake additional indications

Serotonin-specific reuptake inhibitor

Serotonin/noradrenaline reuptake inhibitors

Serotonin/noradrenaline reuptake inhibitors SNRIs)

Side effects reuptake inhibitors

Social anxiety disorder selective serotonin reuptake inhibitors

Specific serotonin reuptake

Specific serotonin reuptake inhibitors (SSRIs

Subject selective serotonin reuptake inhibitors

Suicide selective serotonin reuptake

Trazodone selective serotonin reuptake inhibitors with

Tricyclic antidepressants selective serotonin reuptake inhibitor interactions

Tyramine reuptake

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