Download Antidepressants - Psychiatry - Lecture Slides and more Slides Psychology in PDF only on Docsity! Antidepressants Docsity.com Classic & New Antidepressants – 5-HT Reuptake Inhibitors (SSRI) • Fluoxetine (& R-FLX), Paroxetine, Sertraline, Fluvoxamine, Citalopram – NE/5-HT Reuptake Inh. (SNRI) • Venlafaxine, Milnacipran, Duloxetine – DA/NE Reuptake Inh.: Bupropion – 5-HT Rec. Modulators: Trazodone, Nefazadone – Pre, Post-Synaptic agonist/antag: Mirtazapine – NE Reuptake Inh. Old:TCA, New: Reboxetine – MAO inhibitors: (reversible & not) Docsity.com SSRIs • Treatment of acute & maintenance depr. (prevent relapse & recurrence) • Relapse: 1 yr 2 yr – 70% 80% placebo – 50% 70% psychotherapy – 20% 20% SRI Docsity.com SSRIs • Absolute contraindication in combination w MAOI or L-Triptophan (5-HT syndr) • Fluoxetine longest t1/2: 9-11 days, the others 20-24 hrs • SRI good GI absorb, Liver metabolized – Prozac & Paxil p450 2D6; Luvox, Zoloft 3A4 Docsity.com SSRIs Side Effects • Usually safe & well tolerated – CNS • Nervousness, jitteriness • Insomnia (Proz) / sedation (Pax, Luv), fatigue • Headaches, Tremmors – GI • Naus / Vom 11-16%, Diarr (Zol), Constip (Pax), anorexia (Pro), dry mouth • Caution in Hepatic Disease – Sexual 5-HT2 (25-50%) • delayed orgasm, libido, erection/lubrication – Induction of Mania – Pregnancy: Fluoxetine OK, others no data Docsity.com SNRIs: Venlafaxine [Effexor] • XR & Regular (t1/2=5 hrs) available • Potent 5-HT, NE uptake inh. • Prot. Binding (27%), low p450 problems • SE SRI-like: N/V, dizziness, sedation • Dosage: – 37.5 bid, optimal dose 175-225 – XR 37.5 qd 5-7 d., 75 qd, 150 qd after wk 3 – Monitor Blood Pressure Docsity.com Bupropion [Wellbutrin] • DA Agonist • Structure similar to amphetamine – decrease sleep & appetite, Tx ADHD • Liver metab, kidney excreted • t1/2: 8-12 hrs (bid, tid) • Indications: Depression & ADHD • Risk of Seizures @ 450-600 mg/d – Single dose <150, >4hrs apart – Max dose 400 mg/d Docsity.com Bupropion: SE • N, V, sleep, restlessness, irritab, agit – No sexual SE • Do not use with MAOI • Delirium, psychosis, dyskinesias combined w DA agonists (amantadine, L-dopa, bromocriptine) • Risk of Seizures • Contraind. Hx HI, brain tumor, Sz threshold Docsity.com Mirtazapine [Remeron] • Presynaptic alpha2 blockade – (blocks feedback that release of NE, 5-HT) • Postsynap 5-HT2 block: sexual SE • Postsynap 5-HT3 block: N,V,HA • 5-HT to 5-HT1antidepressant effect) • SE: Sedation, Constipation, Wt gain • Dose: 15 mg/ hs, max 45 mg/d Docsity.com Tricyclics, Tetracyclics (TCA) • Secondary Amines: – Desipramine [Norpramin], Nortryptiline [Pamelor], protryptiline [Vivactil] • Tertiary Amines: – IMI [Tofranil], Amitriptiline [Elavil], Doxepin [Sinequan], Clomipramine [Anafranil (SRI)] • Tetracyclic: Amoxapine [Asendin] Docsity.com TCAs • Action: Blockade of – reuptake of NE & 5-HT – Muscarinic, Histamine, Alpha Adrenergic • 2nd amines safer & better tolerated • Clomipramine most SRI, Doxepine most anticholinergic • Start & Stop slowly • Monitor plasma levels Docsity.com TCAs: Interactions • P450 2D6 • Cimetidine, Quinidine, SsRI, antipsychotics, antiarrithmics TCA • Smoking, Li, Cl Hydrate TCA levels • Additive effects CNS depressants: – EtOH, benzos, opioids, hypnotics, OTC decongestants Docsity.com MAO-inhibitors (MAOIs) Phenelzine [Nardil], Trancypromine [Parnate] • Must: LOW TYRAMINE DIET: no cheese, smoked/aged meats, wine, beans, liver • Avoid: • OTC decongestants (OK ASA, tylenol, ibuprofen, benadryl, plain robotussin) • Diet pills (ephedrine) • DA agonists (Bupropion) • SSRIs, Venlafaxine, most TCAs • L-Tryptophan • Antihypertensives & Diuretics • Narcotics Docsity.com MAOIs • Tyramine (BP) metabolized GI MAO • Hypertensive Crisis: • headache, N, V, stiff neck, photophobia, diaphoresis, palpitations • Serotonin Syndrome: • autonomic instability, hyperthermia, myoclonus, confusion, delilrium, coma • No longer first line, but very effective • SE: orthostasis, sedation, sex dysfx,wt Docsity.com