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Imipramine Was the First of the _____ Family of Antidepressants to Be Discovered

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Profiling Antidepressants

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  1. Profiling Antidepressants by Charles Vannoy

  2. What are antidepressants??? • Drugs that are used to salve or prevent psychic depression. • Work past altering the way in which specific chemicals, called neurotransmitters, piece of work in our brains (i.e. in the case of depression, some of the neurotransmitter systems don't seem to be working properly). • They increase the activity of these chemicals in our brains

  3. History • Antidepressants were first developed in the 1950s and have been used on a regular basis since and so. • In that location are many dissimilar types, for example, the older tricyclics and the newer SSRIs (Selective Serotonin Reuptake Inhibitors). • These ii types business relationship for about 95% if the antidepressants prescribed. • Now at that place are newer, more popular types, such equally SNRI (Dual Serotonin and Norepinephrine Reuptake Inhibitor) and NDRI (Norepinephrine and Dopamine Reuptake Inhibitor)

  4. Antidepressants Available in the Market (Worldwide)1 • i) Tricyclics and Tetracyclics (TCA) Imipramine Doxepin Desipramine Amoxepine Trimipramine Maprotiline Clomipramine Amitriptyline Nortriptyline Protriptyline • 2) Monoamine Oxidase Inhibitors (MAOIs) Tranylcypramine Phenelzine Moclobemide • 3) Serotonin Selective Reuptake Inhibitors (SSRIs) Fluoxetine Fluvoxamine Sertraline Paroxetine Citalopram • 4) Dual Serotonin and Norepinephrine Reuptake Inhibitor (SNRI) Venlafaxine Duloxetine • 5) Serotonin-two Antogonist and Reuptake Inhibitors (SARIs) Nefazodone Trazodone • six) Norepinephrine and Dopamine Reuptake Inhibitor (NDRI) Bupropion • seven) Noradrenergic and Specific Serotonergic Antidepressant (NaSSAs) Mirtazapine • 8) Noradrenalin Specific Reuptake Inhibitor (NRI) Reboxetine • 9) Serotonin Reuptake Enhancer Tianeptine

  5. Tricyclic Antidepressants (TCAs) • Betwixt 1960 and 1980 tricyclic antidepressants (TCAs) represented the major pharmacological treatment for low. • They have been considered a homogeneous grouping of drugs differing more often than not in their potency to inhibit presynaptic norepinephrine or serotonin uptake and in their propensity for causing variety of unwanted furnishings. • The TCAs induce anticholinergic, antihistaminergic, and cardiotoxic side effects which are related to their action on muscarinic (mainly M1), histamine (H1), adrenergic (α1) receptors and cardiac Na+ and Ca2+ channels.

  6. TCA Drugs • The first tricyclic antidepressant discovered was imipramine, which was discovered accidentally in a search for a new antipsychotic in the belatedly 1950s. • Imipramine hydrochloride is a member of the dibenzazepine group of compounds. It is designated five-[3-( Dimethylamino)propyl]-10,11- ihydro-5H-dibenz [b,1-azepine] Monohydrochloride. Imipramine (Tofranil)

  7. Imipramine (Tofranil) • Imipramine is the prototypic tricyclic antidepressant utilized in the treatment of major depression and exerts its therapeutic efficacy only after prolonged administration. • The mechanism of action of imipramine hydrochloride is non definitely known. Yet, it does not human activity primarily past stimulation of the central nervous system. The clinical event is hypothesized every bit being due to potentiation of adrenergic synapses by blocking uptake of norepinephrine at nerve endings.

  8. Amitriptyline (Elavil, Tryptanol, Endep) • Amitriptyline HCl is 3-(x,11-dihydro-5H-dibenzo [a,d] cycloheptene-v-ylidene)-N,Northward-dimethyl-1-propanamine hydrochloride. Its empirical formula is C20H23N·HCl. Amitriptyline

  9. Amitriptyline cont'd • Amitriptyline HCl is an antidepressant with allaying effects. Its mechanism of action is not known. It is not a monoamine oxidase inhibitor and information technology does not act primarily by stimulation of the cardinal nervous organization. • Amitriptyline inhibits the membrane pump mechanism responsible for uptake of norepinephrine and serotonin in adrenergic and serotonergic neurons. Pharmacologically this action may potentiate or prolong neuronal activity since reuptake of these biogenic amines is important physiologically in terminating transmitting activity. This interference with the reuptake of norepinephrine and/or serotonin is believed by some to underlie the antidepressant activeness of amitriptyline.

  10. Side Effects of TCAs • The side furnishings of tricyclic antidepressant may include drowsiness, anxiety, restlessness, dry out rima oris, constipation, urinary retention or difficulty with urination, cognitive and retentivity difficulties, weight gain, sweating, dizziness, decrease in sexual ability and desire, musculus twitches, weakness, nausea, increased center charge per unit and irregular centre rhythms (rare). Some of these side effects chronicle to their anticholinergic properties.

  11. Selective Serotonin Reuptake Inhibitors (SSRIs) • The SSRIs are currently the virtually widely utilized class of antidepressants in clinical practice. • They human action inside the brain to increase the corporeality of the neurotransmitter, serotonin (five-hydroxytryptamine or 5-HT), in the synaptic gap past inhibiting its re-uptake. • Instead of being discovered by accident, SSRIs were specifically designed while considering the biological causes of depression. • SSRIs are described equally 'selective' considering they touch on just the reuptake pumps responsible for serotonin, as opposed to earlier antidepressants, which affect other monoamine neurotransmitters as well. Considering of this, SSRIs lack some of the side effects of the more general drugs.

  12. SSRI Drugs Fluoxetine Sertraline • SSRI drugs include many of the popular drugs on the market today • They include Fluoxetine (Prozac) and Sertraline (Zoloft).

  13. Fluoxetine (Prozac) • Fluoxetine, also known every bit Prozac, was initially approved for treatment of low in Belgium in 198617, and so Eli Lilly'due south Prozac was approved by the FDA on Dec 27th 1987 and introduced in the Usa at the starting time of 1988. • Prozac was the offset of a new class of drugs, called selective serotonin reuptake inhibitors (SSRIs), to be approved for use in the Usa. • Fluoxetine hydrochloride is an antidepressant for oral administration. It is chemically unrelated to tricyclic, tetracyclic, or other bachelor antidepressant agents. Information technology is designated (±)-N-methyl-3-phenyl-three-[(a,a,a-trifluoro-p-tolyl)-oxy]propylamine hydrochloride and has the empirical formula of C17H18F3NO•HCl.

  14. Fluoxetine (Prozac) cont'd • Fluoxetine is a racemic mixture (50/50) of R-fluoxetine and S-fluoxetine enantiomers, where both enantiomers are specific and strong serotonin uptake inhibitors with essentially equivalent pharmacologic action. Simply, the S-fluoxetine enantiomer is eliminated more slowly and is the predominant enantiomer present in plasma at steady state. • The body eliminates Fluoxetine very slowly. The half-life of fluoxetine later a unmarried dose is 2 days and after multiple dosing 4 days. The liver then metabolizes fluoxetine into norfluoxetine, a desmethyl metabolite, which is besides a serotonin reuptake inhibitor; norfluoxetine has an even longer half-life, i.eastward. 8.6 and 9.iii days for single and repeated dosage respectively. • Because fluoxetine'due south metabolism involves the P450IID6 system, concomitant therapy with drugs also metabolized by this enzyme organisation (such as the tricyclic antidepressants) may lead to drug interactions. Hence, the complication of the metabolism of fluoxetine has several consequences that may potentially touch on fluoxetine's clinical apply.

  15. Fluoxetine Dosage and Side Effects • It is marketed in capsules containing 10, 20, or 40 mg of agile ingredient or in tablets containing 10 mg. Dosages in the range of xx-60 mg per solar day are standard, with fourscore mg considered a maximum. • Fluoxetine has a wide range of published interactions, notably with monoamine oxidase inhibitors. Common side-effects include anxiety, restlessness, trembling, weakness, peel rash, anorgasmia, itching, and a subtract in sexual drive.

  16. Sertraline (Zoloft) • Sertraline HCl is a selective serotonin reuptake inhibitor (SSRI) for oral assistants. It is chemically unrelated to other SSRIs, tricyclic, tetracyclic, or other available antidepressant agents. Sertraline hydrochloride has the following chemical proper noun: (1S-cis)-4-(3,4-dichlorophenyl)-1,two,iii,4-tetrahydro-N-methyl-1-nanphthalenamine hydrochloride. The empirical formula is C17H17NCl2·HCl.

  17. Sertraline (Zoloft) cont'd • The mechanism of action of sertraline is presumed to be linked to its inhibition of CNS neuronal uptake of serotonin (5HT). • In vitro studies have shown that sertraline has no significant affinity for adrenergic (alpha1, alpha2, beta), cholinergic, GABA, dopaminergic, histaminergic, serotonergic (5HT1A, 5HT1B, 5HT2), or benzodiazepine receptors; antagonism of such receptors has been hypothesized to be associated with various anticholinergic, sedative, and cardiovascular effects for other psychotropic drugs. Sertraline does non inhibit monoamine oxidase. • Sertraline undergoes extensive first pass metabolism. The master initial pathway of metabolism for sertraline is N-demethylation. Northward-desmethylsertraline has a plasma terminal emptying half-life of 62 to 104 hours.

  18. Sertraline Dosage and Side Furnishings • Sertraline is manufactured past Pfizer as small green 25 mg tablets, blue 50 mg tablets, or off-xanthous 100 mg tablets. It is used in dosages of between 25 mg and a maximum of 200 mg per twenty-four hour period. • It has a number of adverse furnishings including insomnia, asthenia, gastrointestinal complaints, tremours, confusion, and dizziness; it can induce mania or hypomania in around 0.5% of patients. One belongings of sertraline is that it appears to be also a minor inhibitor of dopamine reuptake.

  19. Serotonin and Noradrenaline Reuptake Inhibitors (SNRIs) • Serotonin norepinephrine reuptake inhibitors (SNRIs) are a class of antidepressant used in the treatment of clinical low and other affective disorders. • They act upon two neurotransmitters in the brain that are known to play an important part in mood, namely, serotonin and norepinephrine. This can be contrasted with the more than widely-used selective serotonin reuptake inhibitors (SSRIs), which act but on serotonin. • SNRIs were adult more recently than SSRIs, and there are relatively few of them. Their efficacy as well as their tolerability appears to be somewhat amend than the SSRIs, attributable to their compound effect. • These new drugs, considering of their specificity for the serotonin and norepinephrine reuptake proteins, lack nigh of the agin side effects of tricyclic antidepressants and monoamine oxidase inhibitors.

  20. SNRI Drugs • SNRIs are currently some of the newest antidepressant drugs available on the market, and due to this at that place are only a few selected drugs that have been approved by the FDA for use. Venlafaxine

  21. Venlafaxine (Effexor) • Venlafaxine hydrochloride is a prescription antidepressant commencement introduced by Wyeth in 1993, and marketed under the tradename Effexor®. It is used primarily for the treatment of depression, generalized anxiety disorder, and social anxiety disorder in adults. The chemical structure of Venlafaxine is designated (R/S)-1-[2-(dimethylamino)-1-(4 methoxyphenyl)ethyl] cyclohexanol hydrochloride or (±)-i-[a [α- (dimethylamino)methyl] p-methoxybenzyl] cyclohexanol hydrochloride and information technology has the empirical formula of C17H27NO2 · HCl. • Venlafaxine is the first and most commonly used SNRI.

  22. Venlafaxine (Effexor) cont'd • Venlafaxine has a single chiral centre and exists every bit a racemic mixture of R-(–)- and S-(+)-enantiomers. The R-enantiomer exhibits dual presynaptic inhibition of serotonin and noradrenaline reuptake, while the S-enantiomer is predominantly a serotonin reuptake inhibitor. In vitro, venlafaxine is approximately 3- to v-fold more stiff at inhibiting serotonin than noradrenaline reuptake. It has depression affinity for muscarinic cholinergic, histamine H1 and adrenergic receptors.

  23. Venlafaxine (Effexor) cont'd • The mechanism of the antidepressant action of venlafaxine in humans is believed to be associated with its potentiation of neurotransmitter activeness in the CNS. Venlafaxine and its agile metabolite, O-desmethylvenlafaxine (ODV), are potent inhibitors of neuronal serotonin and norepinephrine reuptake and weak inhibitors of dopamine reuptake. Venlafaxine and ODV have no pregnant affinity for muscarinic, histaminergic, or a-1 adrenergic receptors • Venlafaxine is primarily metabolized by the cytochrome P450 (CYP) 2D6 isoenzyme, with the CYP3A3/4 arrangement providing a secondary metabolic pathway. The drug only modestly inhibits CYP2D6, and its metabolite has no effect on this isozyme.

  24. Venlafaxine Dosage and Side Effects • Prescribed dosages are typically in the range of 75mg-225mg per mean solar day, but higher dosages are sometimes used for the treatment of severe or treatment-resistant low. Because of its relatively short half-life of 4 hours, Effexor should be administered in divided dosages throughout the day. • Side effects may include nausea, dizziness, sleepiness, abnormal ejaculation, sweating,dry out oral cavity, gas or tummy pain, abnormal vision, nervousness, insomnia, loss of appetite, constipation, confusion/agitation, tremors, and drowsiness.

  25. Norepinephrine and Dopamine Reuptake Inhibitor (NDRI) • These are a course of antidepressants that are not really categorized as a special group of antidepressants. • The but antidepressant in this group is Bupropion, which is an antidepressant of the aminoketone class, chemically unrelated to tricyclics or SSRIs. It is similar in structure to the stimulant cathinone, and to phenethylamines in full general.

  26. Bupropion (Wellbutrin, [SR], [Xl]) • Bupropion was first synthesized by Burroughs Research in 1966, and patented by Burroughs-Wellcome (later Glaxo-Wellcome) in 1974. It was approved by the FDA in 1985 and marketed under the name Wellbutrin as an antidepressant. • Bupropion is designated as (±)-1-(3-chlorophenyl)-ii-[(ane,1-dimethylethyl)amino]-1-propanone hydrochloride. The empirical formula is C13H18ClNO·HCl. Bupropion

  27. Bupropion (Wellbutrin, [SR], [XL]) cont'd • Bupropion is a selective catecholamine (norepinephrine and dopamine) reuptake inhibitor. It has merely a small effect on serotonin reuptake. It does non inhibit MAO. The actual mechanism behind bupropion'south action is not known, but it is thought to be due to the effects on dopaminergic and noradrenergic mechanisms. • Bupropion is metabolised in the liver. Information technology has at least three agile metabolites; hydroxybupropion, threohydrobupropion and erythrohydrobupropion. These active metabolites are farther metabolised to inactive metabolites and eliminated through excretion into the urine. The one-half-life of bupropion is 20 hours as is hydroxybupropion'south. Threohydrobupropion's half-life is 37 hours and erythrohydrobupropion'southward 33 hours.

  28. Bupropion and its Metabolites

  29. Bupropion Dosage • Wellbutrin pills are available in three forms: firsthand release, sustained release (SR) and extended release (40). Generic forms of immediate and sustained release are available.

  30. Bupropion Side Effects • Common side furnishings include dry mouth, tremors, anxiety, loss of ambition, agitation, dizziness, headache, excessive sweating, increased risk of seizure, and indisposition. Bupropion causes less insomnia if it is taken just before going to bed. • Sexual side effects unremarkably accompanying SSRI'south exercise non back-trail bupropion. Interestingly, patients commonly report increased libido, perhaps evidence of its dopaminergic properties.

  31. Conclusion • Over the by half century there have been many new advances in antidepressants. Continued progress in understanding the neurobiology of antidepressant drugs volition pb to further identification of the phenomenon of how the drugs act and piece of work and development of more constructive and faster acting therapeutic agents. • Each twenty-four hour period looks brighter and brighter for the advancement of newer and better antidepressants.

  32. References • (one) Ayflegül, Y., Saffet, A.M., Tamam, 50. Mechanism of deportment of antidepressants: beyond the receptors.Klinik Psikofarmakoloji Bulteni, (2002), 12(4), 194-200. • (2)Wellbutrin. GlaxoSmithKline. 15 November 2004 <http://u.s.a..gsk.com/products/assets/us_wellbutrinXLpdf> • (3) Bupropion. Wikipedia Online Encyclopedia. fourteen Oct 2004 http://en.wikipedia.org/wiki/Bupropion • (4) Bupropion. Clinical Pharmacology. ten November 2004 http://www.rxlist.com/cgi/generic/buprop_cp.htm • (5) Wellbutrin. 2004. Encyclopedia of Medicine. HealthSquare. 14 October 2004 http://www.healthsquare.com/newrx/WEL1488.HTM • (vi) Fluoxetine. Wikipedia Online Encyclopedia. fourteen Oct 2004 <http://en.wikipedia.org/wiki/Fluoxetine> • (vii) Fluoxetine. Clinical Pharmacology. eleven Nov 2004 http://www.rxlist.com/cgi/generic/fluoxetine_cp.htm • (eight) Prozac. 2004. Encyclopedia of Medicine. HealthSquare. 14 October 2004 <http://www.healthsquare.com/newrx/PRO1362.HTM> • (9) Venlafaxine. Wikipedia Online Encyclopedia. 9 Nov 2004 http://en.wikipedia.org/wiki/Venlafaxine • (10) Venlafaxine. Clinical Pharmacology. 12 Nov 2004 <http://www.rxlist.com/cgi/generic/venlafax_cp.htm> • (eleven) Wellington K, Perry CM. Venlafaxine Extended Release: A Review of its Use in the Management of Major Low.CNS Drugs (2001), 15, 643-669

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