Antidepressants

Citalopram (Celexa)

SSRI; fewer serious drug-drug interactions as compared with other SSRIs due to pharmacologic profile (mirror image sterioisomers)

Escitalopram (Lexapro)

SSRI; good side effect profile; related to citalopram. Approved for treatment of generalized anxiety disorder.

Fluoxetine (Prozac), fluvoxamine (Luvox), paroxetine (Paxil), sertraline (Zoloft)

What SSRIs are approved for treatment of GAD?

Fluoxetine (Prozac) is the only SSRI that is FDA approved for use in children over 8 y.o.

What antidepressant SSRI is approved for use in children/adolescents?

Phnelzine (Nardil); tranylcypromine (Parnate)

What are some monoamine oxidase inhibitors (MAOIs)?

Buproprion (Wellbutrin); duloxetine (Cymbalta); mirtazapine (Remeron); trazodone (Desyrel); venlafaxine (Effexor); desvenlafaxine (Prestiq)

What are some novel antidepressants?

Citalopram (Celexa); escitalopram (Lexapro); fluoxetine (Prozac); fluvoxamine (Luvox); paroxetine (Paxil); sertraline (Zoloft)

What are some selective serotonin reuptake inhibitors (SSRIs)?

Dry mouth, mydriasis, diminished lacrimation, blurred vision, eye pain (report immediately), urinary retention, constipation, anhidrosis, CV effects, orthostatic hypotension, sedation, delirium/mania, increased risk of suicide

What are some side effects of TCAs?

Amitriptyline (Elavil); clomipramine (Anafranil); desipramine (Norpramin); imipramine (Tofranil); nortriptyline (Pamelor, Aventyl)

What are some tricyclic antidepressants (TCAs)?

Common side effects are nausea, dry mouth, diarrhea, thirst, drowsiness, mild hand tremor, polyuria, weight gain, sleeplessness, lightheadedness.

What are the common side effects of lithium?

0.6 to 1.2 mEq/L; optimum is 0.8. Maintenance levels are lower for older adults

What are the desirable maintenance blood levels for lithium?

Therapeutic levels to 300 ng/ml; toxic reactions begin at 450 ng/ml

What are the therapeutic and toxic blood levels for TCAs?

Clomipramine (Anafranil) and fluvoxamine (Luvox)

What are the two drugs considered most effective for OCD?

1.5 mEq/L and above

What blood level of lithium is considered toxic?

Sympathomimetic drugs (amphetamines, epinephrine, cold/diet meds), anticholinergics, anesthetics, antihypertensives, CNS depressants; foods containing tyramine; other MAOIs, TCAs, SSRIs

What drugs/foods should be avoided when MAOIs are used?

50-115 mcg/ML

What is the therapeutic serum level for valproates like divalproex (Depakote)?

Pain medication should be used temporarily and sparingly. SSRIs can help treat anxiety & depression due to high incidence of comorbidity; SSRIs also decrease sensitivity to bodily sensations

What medications are approved for treatment of somatoform disorders?

SSRIs such as fluoxetine (Prozac), paroxetine (Paxil), sertraline (Zoloft), and fluvoxamine (Luvox) are the treatment of choice. TCA clomipramine (Anafranil) also approved for tx, but has more side effects

What medications are used to treat OCD?

SSRIs, mood stabilizers, antianxiety agents; Treatment of comorbid Axis I disorders should be a priority

What medications can address severe, disabling symptoms of personality disorders?

Venlafaxine (Effexor), duloxetine (Cymbalta)

What novel antidepressants (SNRIs) are approved for treatment of GAD?

Activating effects of some SSRIs may precipitate hypomania, mania or suicide

What paradoxical effects can SSRIs produce in pediatric patients?

Lag period of 2-4 weeks. Certain drugs must be avoided, including OTC meds. Abrupt d/c can cause nausea, headache, malaise. Report eye pain immediately. Some side effects lessen after adjusting to medication

What patient teaching should be included when TCAs are prescribed?

Lithium, anticonvulsants, antipsychotics, benzodiazepines, & calcium channel blockers

What types of drugs are used to treat bipolar disorder?

Valproates; i.e. divalproex (Depakote)

anticonvulsant agent used in treatment of bipolar disorder. Rapid onset, well tolerated, with little effect on cognition. Side effects include hair loss, weight gain, tremors, GI upset, dose-related thrombocytopenia. Monitoring of serum levels necessary

Lamotrigine (Lamictal)

anticonvulsant used to treat bipolar disorder. Most common side effect is rash; potential to induce potentially fatal Stevens-Johnson syndrome.

gabapentin (Neurontin)

anticonvulsant used to treat bipolar disorder. Usually used in adjunctive role, not in monotherapy. Effective if pt experiences anxiety.

Carbamazepine (Tegretol)

anticonvulsant used to treat bipolar disorder; effective for most pt that do not respond to valproates or lithium. CBC s/b determined weekly to check for agranulocytosis, and should not be used with SSRIs.

Topiramate (Topamax)

anticonvulsant used to treat bipolar disorder; side effect of weight loss, cognitive dulling.

Oxcarbazepine (Trileptal)

anticonvulsant used to treat bipolar disorder; similar to carbamazepine (Tegretol), but with less side effects.

diphenhydramine (Benedryl)

antihistamine; effective for most parkinsonian-like disorders. Can cause considerable sedation in some.

Lithium

considered gold standard for treatment of bipolar disorder. Naturally occurring; similar to sodium. Used for tx & prophylaxis of manic phase of manic-depressive illness. Inhibits release of norepinephrine, serotonin, & dopamine while facilitating reuptake into presynaptic terminals. Given PO. Not metabolized; renal disease will lengthen half-life. Contraindicated in pt with impaired renal function, cardiovascular disease. Slow onset—2 weeks.

Serotonin syndrome

fatal side effect of mixing SSRIs w/ MAOIs or any other drugs that boost intrasynaptic serotonin; hyperthermia, rigidity, cognitive impairments, autonomic symptoms

Fluoxetine (Prozac)

first SSRI developed, frequently prescribed. Beyond typical use, also approved for tx of bulimia, premenstrual dysphoric disorder, pain mgmt., smoking cessation. Long half-life (10 days+) makes it ideal for pt who forget to take meds on time; missed dose not crucial. Drugs that have high probability of SSRI interactions s/b held for up to 6 weeks as this SSRI washes out of the system. Available in once-weekly formulation; fairly inexpensive.

benztropine (Cogentin)

most frequently prescribed anticholinergic. Used to treat all parkinsonian-like disorders, including drug-induced EPSEs. Dosages—1 to 4 mg qd/bid; PO, IM, or IV. Not recommended for pt. w/ TD. For acute dystonic reactions, give 1 to 2 mg IM, then 1 to 2 mg PO bid, if needed.

Tricyclic antidepressants (TCAs)

nonselective inhibition of norepinephrine and serotonin. Because of non-selectivity, cause many side effects. Used to be gold treatment of depression. Lag period of 2-4 weeks before antidepressant effect occurs. Effects—sedation (therapeutic effect), alleviation of lethargy, anxiety reduction, urinary hesitancy. Long half-life usually allow once-daily dosing. Side effects—anticholinergic (dry mouth, decreased sweating, constipation, bladder dysfunction); cardiac (tachycardias, arrhythmias, delay in conduction); orthostatic hypotension; suicide due to energizing effect. Serious interactions when given with MAOIs, sympathomimetics (cardiac arrhythmias), Warfarin (increased bleeding), antipsychotics, anticholinergics, CNS depressants.

Venlafaxine (Effexor)

novel antidepressant (SNRIs). Drugs appear to combine best qualities of TCAs and SSRIs. Few side effects should occur, but documented to increase BP at higher doses; also insomnia. Lower potential for drug interaction than other antidepressants.

duloxetine (Cymbalta)

novel antidepressant (SNRIs). Drugs appear to combine best qualities of TCAs and SSRIs. Low side-effect profile, but can cause insomnia and GI effects.

Mirtazapine (Remeron)

novel antidepressant; faster onset of action than SSRIs; also used to reduce SSRI induced sexual dysfunction. Prominent side effects—sedation and weight gain, increase in serum cholesterol level.

Buproprion (Wellbutrin)

novel antidepressant; only antidepressant w/ dopamine reuptake inhibition; does not affect serotonin systems. Proven to be an effective replacement for/addition to SSRIs when sexual dysfunction occurs. Narrow therapeutic index, but less lethal than MAOIs/TCAs.

Trazodone (Desyrel)

novel antidepressant; seldom prescribed as antidepressant but frequently prescribed for sleep in depressed individuals. Second most commonly prescribed drug for insomnia. Adverse reaction is priapism.

Monoamine oxidase inhibitors (MAOIs)

only antidepressants that inhibit neurotransmitter breakdown as their primary mechanism of action. Usually administered to hospitalized pt or to individuals who can be closely supervised. Phenelzine (Nardil) and tranylcypromine (Parnate) are two most used. Usually only prescribed after other antidepressants have failed due to serious adverse reactions to this class of meds (hypertension). 2-4 weeks for antidepressant effect to occur. Side effects -CNSS, CV, anticholinergic side effects. Serious life-threatening reaction when used w/ certain drugs/foods (tyramine). CNS hyperstimulation might occur causing agitation, hypomania, full schizophrenic episodes. Hypotension.

Paroxetine (Paxil)

potent SSRI; also approved for panic attacks. Short half-life, poses fewer problems than other SSRIs if needs to be d/c. Common side effect is nausea. Shown to be effective for prevention of depressive relapse. Can be given once daily. Causes sexual side effects. May be teratogenic.

Selective serotonin reuptake inhibitors (SSRIs)

selectively block reuptake of serotonin. First-line agent for tx of depression. Side effects—significant sexual dysfunction, GI symptoms, apathy, insomnia, anxiety. Slow onset (2-4 weeks), which s/b considered if pt is suicidal; combination w/ MAOIs produces serotonin syndrome, which is fatal. Low potential for OD

Sertraline (Zoloft)

widely marketed SSRI; second SSRI to be used in US. Can be given once daily w/out regard to meals. Sexual dysfunction in men and women, which typically returns in 2-3 days after d/c.