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ADM8283 - SECTION 5: THE ATYPICAL TCAs

The early 80's were marked by the introduction of several fairly exotic tricyclic antidepressants that included Anafranil (Clomipramine), Desyrel (Trazodone), and Surmontil (Trimipramine). Anafranil had been used in Europe prior to its introduction into the United States.

Anafranil is a tricyclic that was introduced with a promise of having an effect against obsessive-compulsive disorder. The reason being that, besides mediating norepinephrine as a neurotransmitter, it also blocks serotonin reuptake. While Anafranil is a useful medication, its thunder was stolen by the introduction of the SSRIs shortly after it became available.

Desyrel was introduced in the mid-80's, and while Desyrel has a tricyclic-like structure (actually heterocyclic), I am including it in this discussion because at its introduction it was touted as a new class of medications.

The active ingredients of this medication cause the inhibition of the reuptake of serotonin, as well as potentiating the effectiveness of norepinephrine. There is also evidence that this medication works as an antagonist of serotonin-2, meaning that it works against the uptake of serotonin in specific receptor sites in the brain.

Desyrel for two years in the mid-80's was the most widely prescribed antidepressant. Now Desyrel is not even available as a brand name medication, but is only available as Trazodone - a generic substitute. This is because the medication has proved largely ineffective in the treatment of depression.

However, I use it regularly as a sedative medication, as it is wonderfully effective for sleep. It has the advantage of not being addictive like the hypnotics (Ambien, Sonata, Xanax, Ativan).

Surmontil is another TCA antidepressant that has an unusual chemical action. While it is capable of producing antidepressant effects, the mechanism by which it does this is not entirely clear. While nominally a classical TCA, its antidepressant effect does not seem to be caused by norepinephrine or serotonin reuptake inhibition.

Moreover, it seems to be much more like a neuroleptic drug, such as clozapine, in what is called its receptor affinity. As at least one clinical study has shown, Surmontil may be active as an anti-psychotic. It also increases REM sleep, rather than decreasing it like most of the TCAs.

The best use for this medication is in treating depression with insomnia. It has also been shown to be effective in treating patients whose primary complaint is insomnia, even when depression is not present.

I will not spend a great deal of time discussing these medications beyond this preliminary information. As I mentioned earlier, these medications have been largely replaced by the SSRIs. We will, however, present summary pages for these three atypical TCAs on the pages that follow.

Anafranil Summary Page

Trade Name: Anafranil (1990)........................Chemical Name: Clomipramine
Antidepressant type: TCA......... Usual Dosage: 25-300 mg/qd
Pill sizes and types: 10 mg. - Cream colored, triangular tablet; 25 mg. - Cream colored, round tablet; 50 mg. - Film covered, white, round, biconvex, beveled tablet
How it Works: Inhibits norepinephrine and serotonin uptake. This allows more of these neurotransmitters to act in neurons of the limbic system.
Most Common Uses: Clients with depression, particularly accompanied by anxiety. Also used to treat obsessive-compulsive disorder. Generally, for short-term use only.
When Anafranil is used as opposed to other medications: When patients have depression concurrent with obsessive-compulsive disorder.
Side-effects: Possible extrapyramidal effects. Marked reduction in REM sleep; lowers the convulsive threshold. With high medication doses, sinus tachycardia, myocardia infarction, and stroke. Drowsiness, fatigue, restlessness. Dry mouth, blurred vision, decreased libido, skin rash and photosensitivity, nausea and GI distress are also symptoms.
Contraindications and cautions in use: Not to be taken by clients with known hypersensitivity to TCAs. Not to be taken with MAO medications. Must not be added to medication regimen until other contraindicated medications have cleared metabolically, and other contraindicated medications should not be added until this has cleared system. Not to be taken during the acute recovery phase for myocardial infarction. Must not be taken by clients with glaucoma, or liver or kidney damage. Should not be taken by clients taking thyroid medication. Should be administered carefully with clients with history or urinary retention or elderly patients. Will exaggerate effects of alcohol and other CNS depressants. It has not been established whether it is safe to take this medication during pregnancy. Use during lactation is contraindicated. Withdrawal should be administered gradually.
Comments: This medication has more serotonergic activity than other TCAs, hence its greater effectiveness in treating obsessive-compulsive symptomatology.

Desyrel Summary Page

Trade Name: Desyrel (1982)............................Chemical Name: Trazodone
Antidepressant type: Heterocyclic......... Usual Dosage: 150-450 mg/qd
Pill sizes and types: Round, film-sealed, scored tablets: 50 mg. - orange; 100 mg. - white.
How it Works: The mechanisms of action for this medication are not clearly understood.
Most Common Uses: Relatively ineffective for depression. Used more commonly as sleeping aid.
When Desyrel is used as opposed to other medications: Desyrel is almost never used as an antidepressant.
Side-effects: Significant sedation. Dry mouth, constipation, nausea, dizziness, headache, priapism (an erectile dysfunction). May be contributory to cardiac arrhythmia. May increase seizure activity in patients with prior history of seizure disorders.
Contraindications and cautions in use: May impair mental and/or physical abilities. May exaggerate effects of alcohol, barbiturates and other CNS depressants. It is not clear whether there is an interaction between this medication and MAO inhibitors, so concurrent or overlapping use must be carefully monitored. It has not been established whether it is safe to take this medication during pregnancy. Use during lactation is contraindicated. Use for children under 18 is contraindicated.
Comments: Desyrel is not a particularly effective antidepressant in most cases. It is now more likely to be used as a sleep aid.

Surmontil/Rhotrimine Summary Page

Trade Name: Surmontil/Rhotrimine (1982)................Chemical Name: trimipramine
Antidepressant type: Tetracyclic......... Usual Dosage: 75-150 mg/qd
Pill sizes and types: Capsules: 25 mg. - blue/yellow; 50 mg. - blue/orange; 100 mg. - blue/white.
How it Works: The action of this medication is unclear. While nominally a classical TCA, its antidepressant effect does not seem to be caused by norepinephrine or serotonin reuptake inhibition.
Most Common Uses: Clients with endogenous depression, particularly those with insomnia. Also used to treat insomnia without depression. Also has anti-psychotic properties, so it is used with patients with depression and psychotic features.
When Surmontil is used as opposed to other medications: When depression is present with psychotic or schizoaffective symptomatology.
Side-effects: Drowsiness, weight gain or loss, nausea, dry mouth, decreased libido, irregular heartbeat, high or low blood pressure. Can make user sensitive to sunlight, and can affect ability to perspire.
Contraindications and cautions in use: Not to be taken with MAO medications. Must not be added to medication regimen until other contraindicated medications have cleared metabolically, and other contraindicated medications should not be added until this has cleared system. Not to be taken by people recovering from myocardial infarction. Must not be taken by clients with glaucoma, or liver or kidney damage. Should be taken cautiously by clients taking thyroid medication. Should be administered carefully with clients with history of seizure disorder. Care should be taken when operating dangerous machinery on this medication. It has not been established whether it is safe to take this medication during pregnancy or during lactation. It has not been established whether it is safe for children to take this medication. Withdrawal can occur with sudden discontinuation of this medication.
Comments: Surmontil can be used for treating insomnia even when depression is not present. It may also be of value in treating depression when the patient also shows psychotic or schizoaffective symptomatology.

Review Questions for Section VI

At this point in the training, you should be able to answer the following questions:

1. Given that it was once the most frequently prescribed antidepressant, why has Desyrel been largely discontinued to be used for that purpose?
2. For what group of clients is Surmontil generally used?



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