PHRM 311 Lecture Notes - Lecture 3: Rasagiline, Soybean, Doxepin
Document Summary
Blocks neuronal uptake of the biogenic amines, (cid:1009)-ht, na. Ter(cid:415)ary-amines preferen(cid:415)ally block (cid:1009)-ht uptake (sert selec(cid:415)ve) (cid:410)(cid:882)amines. Sec(cid:882)amines (cid:1111) desipramine (pertofrane) (cid:1111) nortriptyline (aventyl) (cid:1111) protriptyline (trip(cid:415)l) Tcas rapidly block uptake but require (cid:1006) (cid:449)eek(cid:400) before clinical improvement in depressed mood is seen. Atypical an(cid:415)depressants drugs (e. g. trazodone, iprindole) do not block biogenic amine uptake, but are clinically e ec(cid:415)ve as an(cid:415)depressants. Monoaminergic neuron"s state of depression (cid:1111) ne (or (cid:1009)-ht) is depleted. Long(cid:882)la(cid:400)(cid:415)ng blockade of the reuptake pump by a tca causes already upregulated receptors to desensi(cid:415)ze or downregulate. Correlates be(cid:425)er in (cid:415)me with the clinical an(cid:415)depressant e ects of tca, maoi, ad, and ect. An(cid:415)cholinergic, muscarinic receptor blockade (cid:1111) cons(cid:415)pa(cid:415)on, blurred vision, dry mouth, dro(cid:449)siness. Amitriptyline (cid:1093) imipramine (cid:1093) doxepin (cid:1093) desipramine (less ses vs. ter(cid:415)ary group) (cid:1005)-receptor blockade (cid:1111) dizziness, orthosta(cid:415)c (postural) hypotension (cid:920) re ex tachycardia, dro(cid:449)siness. H(cid:1005) histamine receptor blockade (cid:1111) weight gain, dro(cid:449)siness. Overdose blocks na(cid:1085) channels (cid:1111) cardiac arrhythmias, seizures.
