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BBC Pharm

Ch. 48: antidepressants

signs and symptoms of depression? feelings of sadness, hoplessness, despair, and the inability to experience pleasure in usual activities (anhedonia)
biogenic amine theory.. .depression is due to the deficiency of monoamines such as NE, seratonin at their key sites in the brain.
all antidepressants do this... potentiate (either directly or indirectly) the actions of NE, dopamine, and/or seratonin in the brain.
TCAs? use? severe major depressive disorder.
TCAs include... amitryptyline, clomipramine, despiramine, imipramine.
MOA of TCAs? work to elevate mood, improve alertness, increase physical activity, and reduce morbid preoccupation. they have no effect in normal individuals. they block reuptake of Ne, and SERT, increasing neurologic response. they also block muscarinic, alpha, H1rece
can physical and psychological dependence occur with antidepressants? yes
onset of action of TCAs? slow onset of action, requireing two or more weeks before onset of action.
side effects of TCAs? anticholinergic effects due to muscarinic antagonism; these effects include xerostomia, constipation, urinary retention, aggravation of glaucoma, blurred vision, risk of seizures. others include reflex tachycardia and orthostatic hypotension
TCAs relatively contraindicated in.. manic depressive (bipolar) patients and in suicidal patients (they can easily kill themselves by overdosing)
TCAs may also be used for.. enuresis (because they cause contraction of the internal sphincter of the urinary bladder-all due to strong anticholinergic action)
MOA of SSRI? block re-uptake of seratonin. they are preferred by most non specialists, mostly becuase htey have fewer side effects. t
indications for SSRIs? depression, bulemia nervosa, OCD, anorexia, panic disorder, diabetes related neuropathy, PMS.
side effects of SSRIs? loss of libido, delayed ejaculation, weight gain, anorgasmia, overdose may cause seizures.
examples of SSRIs? citalopram, escitalopram, fluoxetine, paroxetine, sertraline
SSRIs should be avoided in... third trimester of pregnancy because they hav ebeen associated with multiple neonatal complications, including neonatal pulmonary hypertension and a range of gastrointestinal problems.
which SSRI should not be used any time during pregnancy? paroxetine
how should you discontinue SSRIs? dose may be tapered gradually to avoid withdrawal symptoms.
MAO inhibitors include... phenelzine, isocarboxazid, tranylcypromine.
MOA of MAOIs? inactivate MAO, allowing transmitters to escape degradation and to leak into the synaptic cleft. they are indicated for phobias and depressed patients unresponsive or allergic to TCAs or SSRIs or who have a strong axxiety component tot heir problems.
MAOIs can be use din conjunciton with... SSRIs, SNRIs, or TCAs., and there has to be at least a two week period of "wash out" (ex: no drug administratoin)_ between the use of MAois and these antidepressants.
what is MAO? mitochondrial enzyme found in neural and other tissues, such as gut and liver. it functions as a "safety valve" to oxidatively deaminate and inactivate any excess neurotransmitter molecules (NE, DA, SERT) that may leak out of hte vseicles into cell cytopl
MAO degrades what tyramine. thats why MAOIs have a high drug/drug and drug/food interaction. as a result, there are strict dietary restirctions for those taking MAOIs.
those taking MAOIs may not consume... with high tyramine content (cheese, beer, wine, and chicken liver. doing so may lead to hypertensive crisis (the high catecholamine levels resuilt in tachycardia, HTN, cardiac arrhythmias, and stroke.
side effects of MAOIs? constipation, blurred vision, xerostomia, drowsiness, and dysuria.
MAOIs are contraindicated in these patients.. those who refuse to eliminate tyramine from their diet, such as suicidal patients.
SNRIs include... desvenlafaxine, velafaxine, duloxetine.
MOA of SNRI? prevent seratonin and norepinepherine reuptake at the level of the synapse. like with SSRI, triptans and MAOIs should be avoided in order to prevent the possibility of serotonin syndrome. likewise, like SSRIs, these should not be used during the 3 TM preg
blocks reuptake of norepinephrine and the reuptake of seratonin with three times more effect on the latter. it has a strucutre similar to that of amphetamine, accounting for it sactivating action o n patients. used for major depressive disorder. velafaxine
this is the antidepressant most likely to induce mania in susceptible patients. side effects includ ehadache, weight loss, loss of libido, and increased BP. latter effect makes this drug unsuitable for patietns with hypertension. velafaxine
patients using venlafaxine can prodoce a positive test for.. PCP.
inhibits reuptake of both NE and SERT, and also has weka reuptake inhibition activity on dopamine. it is used for both major depressive disorder as well as diabetes associated neuropathic pain. duloxetine
duloxetine is contraindicated in who? those with renal disease, liver failure, and heavy alcohol use.
atypical andidepressant that works to block reuptake of NE and Dopamine, with twice as much effect on the latter; it is also a nicotinic agonist buproprion.
buproprion used for..? major depressive disorder. it is effective for monotherapy, but also is particularly helpful as an adjunctive medication in thise not fully responsive to SSRi therapy.
buproprion is especially useful for thes patients.. smoking cessation and seasonal affective disorder.
does buprioprion lower seizure threshold? yes, but when used at recommended doses, its propensity to cuase seizure is similar to that observed with other antidepressants. does not cause weight gain or sexual dysfunction, can cause dry mouth, tinnitus, and nausea.
buproprion can promote... hallucinations and psychosis which can often be ameliorated by reducing the dose. cases of hypertension have also been reported.
Created by: aferdo01