BARBITURATES – AN ABUSE

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Tolerance and dependence:
With regular use tolerance to the effects of barbiturates develops. This in turn may lead to a need for increasing doses of the drug to get the original desired pharmacological or therapeutic effect. Barbiturate use can lead to both psychological and physical dependence and the drugs have a high abuse liability. Psychological addiction to barbiturates can develop quickly. The GABAA receptor, one of barbiturates' main sites of action, is thought to play a pivotal role in the development of tolerance to and dependence on barbiturates, as well as the euphoric "high" that results from their abuse. especially clozapine, olanzapine or low potency phenothiazines eg chlorpromazine as they lower the seizure threshold and can worsen withdrawal effects; if used extreme caution is required.

Overdose:
An overdose results when a person takes a larger-than-prescribed dose of a drug. Symptoms of an overdose typically include sluggishness, incoordination, difficulty in thinking, slowness of speech, faulty judgment, drowsiness or coma, shallow breathing, staggering, and in severe cases coma and death. The lethal dosage of barbiturates varies greatly with tolerance and from one individual to another. Even in inpatient settings, however, the development of tolerance is still a problem, as dangerous and unpleasant withdrawal symptoms can result when the drug is stopped after dependence has developed.

generic structure of a barbiturate, including numbering scheme.

Barbiturates

Short Name

R1

R2

IUPAC Name

Allobarbital

CH2CHCH2

CH2CHCH2

5,5-diallylbarbiturate

Amobarbital

CH2CH3

CH2CH2CH(CH3)2

5-ethyl-5-isopentyl-barbiturate

Aprobarbital

CH2CHCH2

CH(CH3)2

5-allyl-5-isopropyl-barbiturate

Alphenal

CH2CHCH2

C6H5

5-allyl-5-phenyl-barbiturate

Barbital

CH2CH3

CH2CH3

5,5-diethylbarbiturate

Brallobarbital

CH2CHCH2

CH2CBrCH2

5-allyl-5-(2-bromo-allyl)-barbiturate

Phenobarbital

CH2CH3

C6H5

5-ethyl-5-phenylbarbiturate

How is barbiturate abuse diagnosed?
The diagnosis of barbiturate abuse is based on the history of the use of barbiturates by the affected individuals. Additional information about the abuse can be gathered from friends and family members of the affected individuals. Enquiry about the signs and symptoms of abuse is also performed. The pattern of drug use and the dosage commonly consumed can give an idea about the barbiturate abuse. Blood tests and urine tests may be used to detect the presence or levels of these drugs in the body.

How is barbiturate abuse treated?
There are many pharmacological and non-pharmacological modes of treatment that can help the abuser get rid of the above mentioned symptoms. However, the aim of therapy is to stop or control barbiturate abuse. Providing education to the abuser and his caregivers is the major concern of treatment, this also helps in preventing further complications. For the safety of abuser and as a preventionary measure, the physician may ask the abuser not to drive or operate machineries. Initial treatment may require the abuser to be admitted in the hospital to prevent any adverse event when the barbiturate use is stopped completely.

Barbiturate abuse treatment may include any of the following measures:

Detoxification: Detoxification procedure is done to flush out the toxic residues of barbiturates present in the patient’s body. During detoxification, medicines are given to help prevent withdrawal symptoms when the person stops taking barbiturates. The affected persons are also educated about the harms of barbiturate abuse and counseled for stress relief and coping with the problems in hand. You may also be advised to avoid places, people or things that remind about barbiturate use.

Medical treatment: 
The medical treatment in barbiturate abuse is largely symptomatic.

The healthcare provider may give certain medicines to relieve symptoms. These may include medicines to treat anxiety or sleeping problems. The physician may also suggest certain medicines to help control barbiturate abuse and other related problems. The dosage and frequency of the barbiturates may be altered to prevent you from becoming dependent upon these medications.

References:
1. Schears RM. Barbiturates. In: Tintinalli JE, Kelen GD, Stapczynski JS, Ma OJ, Cline DM, eds. Emergency Medicine: A Comprehensive Study Guide . 6th ed. New York, NY: McGraw-Hill; 2004:chap 163.
2. Public Health Service, US Department of Health, Education, and Welfare: Barbiturates as Addicting Drugs, Washington, DC: Publication No. 545, US Government Printing Office.
3. Fraser, H.F., et al:  Chronic Barbiturate Intoxication , Arch Intern Med (Chicago) 194:34-41 ( (July) ) 1954;. Isbell, H.:  Treatment of Barbiturate Addiction , Postgrad Med 9:3 ( (March) ) 1951;.
4 Essig, C.F.:  Failure of Diphenylhydantoin in Preventing Barbiturate Withdrawal Convulsions in Dog , Neurology (Minneap) 12:481-484 ( (July) ) 1962;.
5 Essig, C.F.:  Addictive and Possible Toxic Properties of Glutethimide , Amer J Psychiat 119:10 ( (April) ) 1963;.
6. Essig, C.F.; and Ainslie, J.D.:  Addiction to Meprobamate (Equanil and Miltown) , JAMA 164:1382 ( (July 20) ) 1957;.
7. Essig, C.F.:  Withdrawal Convulsions in Dogs Following Chronic Meprobamate Intoxication , Arch Neurol (Chicago) 80:414-417 ( (Oct) ) 1958;.

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