Protriptyline antidepressant

The antidepressant protriptyline (116) causes skin photosensitization in man. Jones and Sharpies irradiated an aqueous solution of the hydrochloride with a medium-pressure mercury lamp for 16 h and separated the products by preparative TLC. First formed was the epoxide (117) which photohydrated to the diol (118). Also isolated was the enol (119) [84], Earlier, Gasparro and Kochevar had shown that only the hydrochloride was photodegraded under nitrogen in water or ethanol. Three products were isolated and all lysed erythrocytes, but the structure of only one was suggested. This was a cyclobutyl dimer as shown by its mass spectrum and its photolysis back to protriptyline by light of 254 nm. Presumably, a [2 + 2] cycloaddition of the olefine bonds had occurred [85]. 

Be aware that among this class of agents (tri cy cl I c/tet racy cl ic antidepressants), protriptyline has uniquely low dosing (15-40 mg/day for profripfyline compared to 75-300 mg/day for mosf ofher tri cy cl I c/tet racy cl I c antidepressants)... 

On the C=C double bond, 2+2 cycloaddition occurs with conjugated olefins (Scheme 4.6), e.g., with the antidepressant protriptyline (Gasparro and Kochevar, 1982) and in particular with a,P-unsaturated ketones (e.g., with menadione (8), which yields the. vyn-cyclobutane dimer in the solid state and the anti-isomer by irradiation in acetone solution (Scheme 4.7 (Marciniec and Witkowska, 1988). The epoxide is obtained in the presence of oxygen (Jones and Sharpies, 1984) (see later in this chapter for other oxidations). Polar addition to arylalkenes has also been observed,... 

The answer is c. (Hardman, p 436.) The tricyclics and second-generation antidepressants act by blocking serotonin or norepinephrine uptake into the presynaptic terminal. Fluoxetine selectively inhibits serotonin uptake with minimal effects on norepinephrine uptake. Protriptyline, maprotiline, desipramine, and amoxapine have greater effect on norepinephrine uptake... 

Amitriptyline appears to be the tricyclic antidepressant (TCA) of choice, but imipramine, doxepin, nortriptyline, and protriptyline have also been used. 

The most effective treatment for cataplexy is the tricyclic antidepressants, fluoxetine, or venlafaxine. Imipramine, protriptyline, clomipramine, fluoxetine, and nortriptyline are effective in about 80% of patients. 

Tricyclic Antidepressants (TCAs). TCAs were introduced in the 1950s and over the years have become the mainstay of treatment for cataplexy and the other REM-related symptoms. The doses used are usually less than the doses required in the treatment of depression. Imipramine (Tofranil) is the most widely used TCA for narcolepsy and is usually effective at doses from 10 to 75 mg given once a day. Some doctors prefer the TCA protriptyline (Vivactil) because it has mild stimulant effects, but it has not been as widely used or as thoroughly studied in narcolepsy. The common side effects of TCAs are drowsiness, dry mouth, and constipation, but these are usually not a problem at the lower doses used for narcolepsy. Patients should receive a baseline electrocardiograph (EKG) before starting a TCA and should have blood levels of the medication checked periodically. 

Protriptyline (Vivactil) Antidepressant Pyrazinamide (PZA) T uberculostatic Pyridoxine (Vitamin Vitamin B6)... 

Reboxetine is the only selective and reasonably potent noradrenaline reuptake inhibitor available clinically at the present time. Reboxetine has a chemical structure not dissimilar from viloxazine, an antidepressant which was of only limited clinical interest in the 1970s because of its weak efficacy and unacceptable side effects (nausea, vomiting and occasionally seizures). Unlike the secondary amine TCA antidepressants, such as maprotiline, desipramine, nortriptyline and protriptyline, reboxetine does not affect any other transporter or receptor system and therefore is largely devoid of TCA and SSRI-like side effects. In clinical trials, reboxetine has been shown to be as effective as the SSRIs in the... 

There are four classes of antidepressants tricyclic antidepressants (imipramine, trimipramine, amitriptyline, doxepin, desipramine, protriptyline, nortriptyline, amoxapine, maprotiline) monoaminooxidase (MAO) inhibitors (phenelzine, isocarboxazid, tranylcypromine) second-generation antidepressants or atypical antidepressants, which are a chemically dissimilar group of recently proposed drugs (bupropion, trazodone, fluoxetine) and amphetamines and other stimulators of the CNS (dextroamphetamine, methylphenidate). 

Protriptyline is a powerful antidepressant, the mechanism of action of which is not known. It is not a MAO inhibitor and does not stimulate the CNS. It begins to act much faster and acts much longer than imipramine or amitriptyline. Protriptyline does not possess sedative tranquilizing properties. It is used in clinical conditions for treating severe depression. The most common synonyms are concordin, triptil, and vivactil. 

Maprotiline is frequently referred to as a tetracyclic antidepressant. This hybrid drug, containing both elements of classic tricyclic antidepressants and protriptyline elements, is pharmacologically and clinically more similar to imipramine. 

Compounds in this dibenzocycloheptene series also manifest antidepressant activity when the trigonal one-carbon bridge is replaced by tetrahedral carbon. Thus, the reaction of hydrocarbon (24-7) with a metal amide in liquid ammonia leads to the corresponding carbanion (29-1). Treatment of that with the ethyl carbamate from A -methyl-3-chloropropylamine (29-2) leads to the alkylation product. The carbamate protecting group is then removed by sequential saponification with a base followed by acidification. This yields the antidepressant agent protriptyline (29-3) [30]. 

Long after their antidepressant properties were observed, the tricyclics were discovered to block the reuptake pumps for both serotonin and norepinephrine, and to a lesser extent, dopamine (Figs. 5 — 16, 6—5, and 6—6). Some tricyclics have more potency for inhibition of the serotonin reuptake pump (e.g., clomipramine) others are more selective for norepinephrine over serotonin (e.g., desipramine, maprotilene, nortriptyline, protriptyline). Most, however, block both serotonin and norepinephrine reuptake. 

The dibenzapine derivatives are called tricyclic antidepressants and include imipramine (Tofranil), desipramine (Norpramin), amitriptyline (Elavil), nortriptyline (Aventyl), protriptyline (Vivactil), and doxepin (Adapin). 

Tricyclic antidepressants, like some of the phenothiazine derivatives, are sedative in nature. Those compounds containing a tertiary amine (imipramine, amitriptyline, and doxepin) are the most sedative. Those compounds containing a secondary amine (nortriptyline and desipramine) are less so, and protriptyline has no sedative effect. 

Powder see Cocaine Powder cocaine see Cocaine Pox see Opium Prazepam see Benzodiazepine Prelu-2 see Diet pills Prolixin see Tranquilizers ProSom see Benzodiazepine Protriptyline see Antidepressants Pseudoephedrine see Ephedra Psilocybe mushrooms see Psilocybin Psilocydes see Psilocybin Psychedelic mushrooms see Psilocybin Puffy see PCP (phencyclidine)... 

These result from the drug s sympathoplegic actions. The major adverse effect is postural hypotension. This effect can be almost totally prevented by concomitant administration of a tricyclic antidepressant agent such as protriptyline. Nausea and vomiting may occur after the intravenous administration of a bolus of bretylium. 

Fluoxetine is a selective serotonin-reuptake inhibitor (SSRI) that produces a net increase in (post-synaptic motor neuron) serotonin delivery after 4-6 weeks of use. A double-blind, randomized cross-over trial compared fluoxetine to the tricyclic antidepressant agent protriptyline and placebo in 12 patients with sleep-disordered breathing [52], The group apnea-hypopnea index (AHI) improved with fluoxetine compared to placebo, but there was great variability of response and other measures of disordered sleep did not change. These potentially beneficial results in a small number of patients need to be replicated in well-designed larger studies to support a useful role in clinical practice. 

Since the 1960s, it has been known that imipramine is very effective for reducing cataplexy [99], Tricyclic antidepressants were the first drugs of choice, particularly protriptyline, but the anticholinergic effect led to impotence in more than 40 % of... 

Quantification. Gas Chromatography. In serum protriptyline and other tricyclic antidepressants, detection limit 10 to 20 ng/ ml, AFID—J. Kristinsson, Acta pharmac. tox., 1981, 49, 390-398. 

Gas Chromatography-Mass Spectrometry. In plasma protriptyline and other tricyclic antidepressants, sensitivity 10 ng/ ml—J. T. Biggs et ai, J. pharm. Sci., 1976, 65, 261-268. 

CNS and cardiovascular actions of d,l-methylphenidate could theoretically be enhanced by combination with agents that block norepinephrine reuptake, such as the tricyclic antidepressants desipramine or protriptyline, venlafaxine, duloxetine, atomoxetine, milnacipran, and reboxetine... 

For the expert only a heroic treatment (but potentially dangerous) for severely treatment-resistant patients is to give simultaneously with monoamine oxidase inhibitors for patients who fail to respond to numerous other antidepressants, but generally recommend a different TCA than protriptyline for this use... 

Specific serotonin reuptake inhibitors, as the class name implies, act predominantly by preventing serotonin reuptake and have more limited effects on noradrenaline reuptake. Tricyclic antidepressants in general inhibit noradrenaline reuptake, but effects on serotonin reuptake vary widely desipra-mine and protriptyline have minimal potential for raising serotonin concentrations, whereas clomipramine possesses a greater propensity for blocking serotonin reuptake than for noradrenaline. The... 

Protopam chloride" pralidoxime. protriptyline [ban. inn] (protriptyline hydrochloride [usan] Concordin Vivactil" ) is one of the tricyclic class of monoamine uptake inhibitors, and is used as an oral ANTIDEPRESSANT. 

Clinically important, potentially hazardous interactions with amiodarone, amitriptyline, amoxapine, benzodiazepines, bepridil, clomipramine, clonazepam, clorazepate, delavirdine, desipramine, diazepam, dihydroergotamine, doxepin, ergotamine, fentanyl, flurazepam, imipramine, ixabepilone, lidocaine, lorazepam, methysergide, midazolam, nortriptyline, oxazepam, phenytoin, protriptyline, quazepam, quinidine, rifampin, ritonavir, sildenafil, St John s wort, temazepam, tricyclic antidepressants, trimipramine, vitamin E... 

Clinically important, potentially hazardous interactions with acebutolol, amitriptyline, amoxapine, atenolol, betaxolol, carteolol, clomipramine, desipramine, dexmethylphenidate, doxepin, esmolol, imipramine, insulin detemir, insulin glulisine, metoprolol, nadolol, nortriptyline, oxprenolol, penbutolol, pindolol, propranolol, protriptyline, sulpiride, timolol, tricyclic antidepressants, trimipramine, verapamil... 

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