Drug abuse and headache.

Elkind AH.

New York Medical College, Valhalla.

Substance abuse has been reported frequently in chronic headache patients. The problem exists in most Western countries. Abuse of various compounds frequently leads to a state of dependency. Prescription as well as over-the-counter agents are often abused. Aspirin, acetaminophen, and caffeine are the most frequently abused compounds. Butalbital, ergot alkaloids, NSAIDS, and narcotic and oral or intranasal sympathomimetics are often abused. Patients with chronic daily headache complain of symptoms that may suggest a mixed-type headache. Features of migraine and muscle contraction headache often coexist in these individuals. It has been suggested that the most frequent cause for the transformation of a periodic headache into a daily headache is substance abuse. Substance abuse and drug dependency have multiple causes, and the etiology will reside with the compounds that are used to excess. The problem may arise as a result of poor instructions from the physician, improper diagnosis with gradual escalation in amounts of drug consumed, or a reinforcement mechanism and a brain stimulation-reward effect. The brain reward system has been studied with narcotics and psychomotor stimulants. It may be activated to a lesser degree with ergotamine, barbiturates, and other abused substances. The long-term effects of substance abuse are contingent on the compounds that are used. They may result in organ damage, medical complications, vascular injury, and a refractory state with chronic headache that eludes successful management of the headache disorder. Patients exhibit a less-than-satisfactory quality of life and are often depressed. Treatment includes outpatient care in cooperative, less dependent patients. Often patients will require inpatient management in order to discontinue use of the abused agents. Pharmacologic agents, behavior modification, psychotherapy, dietary intervention, and acupuncture may be necessary to treat the patient. Each patient must be treated by an interested physician, and the patient will require one or more of the preceding measures for a successful outcome. Often abused compounds must be discontinued in order to obtain a satisfactory response in an individual with chronic headache.

Source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=&dopt=Abstract butalbital fioricet barbiturate




Identification and differentiation of barbiturates, other sedative-hypnotics and their metabolites in urine integrated in a general screening procedure using computerized gas chromatography-mass spectrometry.

Maurer HH.

Institut fur Pharmakologie und Toxikologie, Universitat des Saarlandes, Homburg/Saar, F.R.G.

A gas chromatographic-mass spectrometric procedure is described for the identification and differentiation of sedative-hypnotics and their metabolites in urine. The following 24 barbiturates and thirteen other hypnotics could be detected: acecarbromal, allobarbital, amobarbital, aprobarbital, barbital, brallobarbital, bromisoval, (sec)butabarbital, butalbital, butobarbital, carbromal, clomethiazole, crotylbarbital, cyclobarbital, cyclopentobarbital, diethylallylacetamide, dipropylbarbital, glutethimide, guaifenesin, ethinamate, heptabarbital, hexobarbital, meprobamate, methaqualone, metharbital, methohexital, methylphenobarbital, methyprylone, pentobarbital, phenobarbital, propallylonal, pyrithyldione, secobarbital, thiobutabarbital, thiopental, vinbarbital and vinylbital. The procedure presented is integrated in a general screening procedure (general unknown analysis) for several groups of drugs detecting over 300 drugs and over 1000 of their metabolites. It includes cleavage of conjugates by acid hydrolysis, isolation by liquid-liquid extraction, derivatization by acetylation, separation by capillary gas chromatography, and identification by computerized mass spectrometry. Using mass chromatography with the selected ions m/z 83, 117, 141, 167, 169, 207, 221 and 235, the presence of barbiturates, other hypnotics and/or their metabolites was indicated. The identity of positive signals in the reconstructed mass chromatograms was confirmed by a visual or computerized comparison of the stored full mass spectra with the reference spectra. The sample preparation, mass chromatograms, reference mass spectra and gas chromatographic retention indices are documented.

Source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=&dopt=Abstract butalbital fioricet barbiturate




A protocol for butalbital, aspirin and caffeine (BAC) detoxification in headache patients.

Sands GH.

Department of Neurology, Long Island Jewish Medical Center, Albert Einstein College of Medicine, Jamaica, N.Y.

The abuse of the combination drug containing butalbital 50 mg, aspirin 325 mg and caffeine 40 mg (or BAC), is commonly recognized by headache specialists as causing headaches. Despite this widespread problem, there is not a published treatment regimen for the BAC detoxification of patients. I describe such a protocol which was used four times in three patients. These patients fulfilled the diagnostic criteria of the IHS Headache Classification for headaches induced by chronic substance abuse (8.2) and analgesics abuse headache (8.2.2). These patients took between 150 and 420 BAC/month for 2-15 years. Two patients had previously undergone inpatient detoxification. One patient unsuccessfully tried detoxification twice as an outpatient. All patients were required to have psychological support prior to hospitalization for this protocol. BAC was discontinued. A pentobarbital challenge test corroborated butalbital dosage. The patients were given phenobarbital and caffeine which were tapered over several days. Dihydroergotamine (DHE) with metoclopramide was used (Raskin). Propranolol 60 mg bid was started. No narcotics were permitted. After hospital discharge, patients were allowed to continue subcutaneous DHE, as needed. One patient restarted BAC use after 8 months without it. The other two patients were still BAC free 18 and 14 months after detoxification.

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Simultaneous liquid-chromatographic determination of 12 common sedatives and hypnotics in serum.

Kabra PM, Koo HY, Marton LJ.

We present a method for simultaneously determining 12 hypnotics and sedatives (primidone, methyprylon, phenobarbital, butabarbital, butalbital, ethchlorvynol, pentobarbital, amobarbital, phenytoin, glutethimide, secobarbital and methaqualone) in 200 microliter of serum. Serum proteins are precipitated with an acetonitrile solution containing 5-(4-methylphenyl)-5-phenylhydantoin, the internal standard. The drugs are eluted from a reversed-phase column with a mobile phase consisting of an acetonitrile/phosphate buffer, at a flow rate of 3.0 ml/min. The eluted drugs are detected by their absorption at 195 nm; their quantities are estimated from their peak heights. Each analysis requires no longer than 30 min at the optimum column temperature of 50 degrees C. The lower limit of detection for all of these drugs is less than 10 ng/sample for drug standard. A sensitivity of 1.0 mg/liter of serum is attained routinely for each of the drugs. Analytical recoveries for the 12 drugs varied from 94 to 112%, with good day-to-day precision (CV between 3.8 and 10.4%). Of more than 35 drugs tested for possible interference, only ethotoin interferes with the analysis of phenobarbital.

Source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=&dopt=Abstract butalbital fioricet barbiturate




Optimized procedure for lamotrigine analysis in serum by high-performance liquid chromatography without interferences from other frequently coadministered anticonvulsants.

Torra M, Rodamilans M, Arroyo S, Corbella J.

Toxicology Unit and Neurology Service, Hospital Clinic, Facultat de Medicina, Universitat de Barcelona, Spain.

The authors have developed a simple isocratic high-pressure liquid chromatographic (HPLC) assay for the simultaneous determination of lamotrigine and other frequently coadministered antiepileptic drugs in serum samples. Lamotrigine extraction was performed on a reversed-phase Oasis HBL preparation column. The eluates containing butalbital as internal standard were separated with a 7-microm Chromsystems C18 250 x 4.0 mm I.D. reversed-phase column at a temperature of 40 degrees C using a mobile phase consisting of pH 3.8 phosphate-acetonitrile buffer (55:45, v/v), at a flow rate of 0.8 mL/min. Ultraviolet detection was carried out at 210 nm. Measurement of the peak:height ratio allowed quantitative determination of the samples. The method was linear over a concentration range of 0.2 to 20 microg/mL for lamotrigine. Recovery was >90%. Within-day and between-day coefficients of variation ranged from 1.8% to 6.7%. The mean lamotrigine concentration was 8.01 +/- 5.63 microg/mL. After studying sera from 130 patients treated with lamotrigine the authors confirmed that associated antiepileptic therapy affected the serum lamotrigine levels, which were significantly higher in patients under valproic acid treatment.

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