Use, Abuse and Misuse of Trazodone

Abstract

Trazodone is an antidepressant drug, prescribed especially to the adults and the elderly that was first manufactured by Angelini Research Laboratories in Italy in the year 1960, and has since acquired new names based on the manufacturer and enjoys a world wide distribution presently - Use, Abuse and Misuse of Trazodone introduction. Once ingested, the drug specifically targets serotonin, and works towards restoring the normal levels of this chemical, since any imbalance brings about depression. Since the drug is in tablet form, it is ingested, preferably after taking a snack or a meal at the rates of between 150-200 mg per day, divided in two doses. Signs of overdose of the drug include behavioral, mental abnormalities as well as cardiovascular complications.

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USE, ABUSE AND MISUSE OF TRAZODONE

Trazodone is an antidepressant drug that does have different trade names depending on the manufacturer. These names include Molipaxin, Trialodine, Desyrel, Trittico and Trazorel. The drug was first discovered as well as developed by the Angelini Research Laboratories in Italy in the year 1960. Initially, the drug was manufactured by the Bristol-Myers Squibb with the name Trazodone but this has since stopped and in its place as a second generation of the drug is being manufactured. This is done by a number of manufacturing firms spread across many countries in the continent (http://depression.emedtv.com/Trazodone/Trazodone.html). The drug has since been patented and enjoys a world wide usage. The drug was approved by the FDA (Food and Dug Administration) towards the end of 1981. It enjoys a very close association with Nefazodone (Silvestrini, 1989).

This drug is in no way chemically related to either tetracyclic or tricyclic antidepressants. It is a derivative of triazolopyridine, with neither presence of neither amphetamine-like nor monoamine oxidase inhibiting properties. It shows little or no anticholinergic activity. The adverse reactions like hypotension and dryness of the mouth that are often experienced with this drug could be attributed to the blocking activity of the alpha-adrenergic (Haria, Fitton and McTavish, 1994).

The drug is used mostly to treat people, especially adults, with depression. There have been suggestions to the effect that the drug has the capability to both prevent serotonin re-uptake as well as blocking serotonin receptors. It can be used for ‘off-label’ reasons. This means that it can and has been used to treat those conditions that have not been approved by the FDA. The most common usage includes to treat insomnia, alcoholism, panic disorder besides anxiety, which is otherwise referred to as  ‘excessive worry’ (http://depression.emedtv.com/Trazodone/ what-is-Trazodone-used-for.html). The usage of the drug however, is limited to the adults and it strongly that it is not used on either children or teenagers. The drug has also known to be used to restore the normal movement in a person especially after experiencing abnormal and uncontrollable movements resulting from side effects of usage of other drugs as well as to treat schizophrenia, which is defined as a mental disease that causes unusual or rather disturbed thinking, inappropriate or strong emotions besides loss of any interest in life (http://www.nlm.nih.gov/ medlineplus/druginfo/meds/a681038.html#other-uses). The usage is not limited to these diseases as doctors continue to use it to treat various diseases as per their own judgments based on the condition of the patient.

When the drug is taken, it works specifically on serotonin, a chemical found in the brain and is one of the chemicals that help in transmitting messages between the nerves. The drug therefore acts to restore the balance of this chemical serotonin in the brain since any imbalance in the levels of the chemical may result into depression. What the Trazodone does therefore is to help block the re-uptake of the chemical, making it available to the brain nerves, thereby restoring it back to the normal levels. It also has the ability to block some serotonin receptors. This is a sharp contrast with the selective receptors that inhibit the re-uptake of serotonin, otherwise called Selective Serotonin Re-uptake Inhibitors (SSRIs) (http://depression.emedtv.com/Trazodone/what-is-Trazodone-used-for-p2.html#chapter_3).

The drug comes in the form of tablets and therefore is orally administered. It has been realized that the effect of the drug is faster if taken after taking either a snack or a meal since it is the body tends to absorb medication best after ingestion due to the realization plasma peak levels. Within ½ to 2 hours from the time of ingestion (http://www.mentalhealth.com/drug/p30-d03.html#Head_0). The mean elimination half-life of plasma has been found to be 4.4 hours within the first 3 to 10 hours of dosing and between 7-8 hours between after the 10th hour of ingestion to the 34th hour. There is extensive metabolism of the drug, with up to about between 60-70% of the C14-labeled Trazodone being traced in the urine within 2 days after dosage and 29% in the feces after between 60 to 100 hours. This drug is 89-95% bound to protein in vitro at the concentrations achieved with the therapeutic doses (http://www.mentalhealth.com/drug/p30-d03.html#Head_0).

It is recommended the dosage of Trazodone should be started at very low levels, and gradually increasing the quantities, while observing the response of the patient and any evidence of side effect or rather signs of intolerance. While increasing the dosage, one should take into account the fact that sometimes there is usually a lag in response to the therapy and increasing the levels of the dosage does not work to shorten the latent period. For the adults, the mostly advised dose should be between 150-200 mg divided into two or three doses daily and taken shortly after ingestion. This helps minimize the chances of adverse reactions. At the initial stages, the dosage can be increased in the bits of about 50 mg up to the levels of 300 mg divided in two doses daily, depending on the tolerance level of the patient. This may climb to as high as 400 mg while a level of 600 mg daily is quite rare but may be necessary for the hospitalized patients.

During the administration of this therapy, such effects like drowsiness may dictate that a better proportion of the drug is taken at bed time or the dosage is reduced altogether. The dosage may be reduced gradually once the desired results have been achieved. The rate of reduction as well depends on the patient’s response to the therapy. For the elderly, they should be put on the dosage that is half that recommended for the adults, with any adjustments made based on the response to the therapy (http://www.mentalhealth.com/drug/p30-d03.html#Head_0).

While under the therapy, some side effects can be developed in the process. These include behavioral ones like drowsiness, dizziness, insomnia, anger, anxiety and tension, hallucinations and delusions, and difficulty in concentration. There is also confusion, nightmares, restlessness as well memory impairment. The mouth of the patient dries coupled with congestion of the nose, blurred vision, abnormal sweating, as well as increased frequency of urination. Sometimes the patient develops cardiovascular complications like hypertension, shortness of the breath as well as prolonged P-R interval. Some neurological problems may also arise. These include, but not limited to headache, numbness, involuntary movements, tremor as well as stiffness of the muscle. There is also the chance of developing gastrointestinal complications like nausea, anorexia, diarrhea and increased appetite. There can be weight loss and gain, irregularities in the menstrual cycle, inhibition of ejaculation as well as increased libido (http://www.cochrane.org/reviews/en/ab004990.html).

Overdose of the drug also brings with it a fair share of complications. Mostly it leads to severity of the above mentioned side effects like hypertension and sedation. There was a reported case of a patient wanting to commit suicide with symptoms of weakness and drowsiness about 3 hours after 7.5 g of the drug. This represented about 12.5 times the maximum amount an individual can ingest in any single day. In this case, the person was never able to recover. However, there has never been a recorded case of death resulting accidental or deliberate overdosing (http://www.mentalhealth.com/drug/p30-d03.html#Head_6).

So far there is no known antidote for the drug in the event of overdose. In the event that a person overdoses, the first step that should be taken is rushing the patient to the hospital where he/she shall be admitted for close observation by the doctors. During this time, the stomach should be emptied by gastric lavage. Also, there can be forceful diuresis so as to facilitate the removal of the drugs from the stomach and in the body system.

The drug is manufactured by mixing a number of elements which gives it the effects that it is usually associated with once ingested. The drug is made into tablets that are shipped under favorable environmental conditions like temperature range for effective results as well as the humidity. As a rule of thumb, most drugs, whether on transit of storage, would usually require a cool and a dry place.

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

References

Haria M, Fitton A, McTavish D (Apr 1994). “Trazodone. A review of its pharmacology,            therapeutic use in depression and therapeutic potential in other disorders”. Drugs

Aging 4 (4): 331–55. PMID 8019056

http://depression.emedtv.com/Trazodone/ what-is-Trazodone-used-for.html. Cited  on

10th December,2008

http://depression.emedtv.com/Trazodone/what-is-Trazodone-used-for-p2.html#chapter_3.

Cited  on 10th December,2008

http://www.cochrane.org/reviews/en/ab004990.html. Cited  on 10th December,2008

http://www.mentalhealth.com/drug/p30-d03.html#Head_0 . Cited on 10thDecember,2008

http://www.mentalhealth.com/drug/p30-d03.html#Head_6. Cited  on 10th December,2008

http://www.nlm.nih.gov/medlineplus/druginfo/meds/a681038.html#other-uses . Cited  on

10thDecember,2008

Silvestrini B (1989). “Trazodone: from the mental pain to the “dys-stress” hypothesis of

depression”. Clin Neuropharmacol 12 (Suppl 1): S4–10. PMID 2568177. Cited  on 10th December,2008

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