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PubMedDate not supplied

The capillary gas chromatographic determination of trazodone in biological specimens.

A simple and specific method is presented for the capillary gas chromatographic determination of trazodone in postmortem blood and tissues. The drug and trimethobenzamide, which was used as an internal standard, were extracted with 1% isopropanol in n-butyl chloride. Chromatography was accomplished with a short (4-m) methyl silicone capillary column and hydrogen carrier gas. This combination of extraction solvent and chromatographic conditions was demonstrated to be both accurate and precise. Since trazodone is a relatively new drug, additional thin layer and packed column gas chromatographic data is presented to augment the incorporation of trazodone into routine analytical protocols.

Chromatography, Gas↗

PubMed1961

Antagonism of apomorphine-induced pecking in pigeons.

Central nervous system stimulants, tranquillizers and other central nervous system depressants, antiemetics, antihistamine drugs and autonomic blocking agents were examined for their ability to prevent the pecking response in pigeons induced by apomorphine (250 mug/kg intramuscularly). Reduction in the proportion of positive responses or significant increase in the latent period of pecking were taken as the criterion of effectiveness. Protection was afforded by caffeine, lysergic acid diethylamide, morphine, rauwolscine, triflupromazine and yohimbine. In addition, a significant increase in latent period was produced by artane, pentobarbitone, benactyzine, 2-bromolysergic acid diethylamide, cyclizine, diphenhydramine, ergotoxine, hyoscine, promethazine, 5-(2-chloroethyl)-4-methylthiazole and trimethobenzamide. Most of these drugs influenced the pecking and emetic responses to apomorphine in an identical manner. It is possible that identical receptors may be concerned with apomorphine pecking (in pigeons) and emesis (in other species).

Animals↗

PubMed1994

Home administration of intramuscular DHE for the treatment of acute migraine headache.

Dihydroergotamine (DHE) has been used for the treatment of acute migraine headache for almost 50 years. Previous studies have emphasized use in emergency room, inpatient, or office settings. Twenty-nine patients with migraine headache who had failed to obtain relief with conventional therapy were trained to self-administer intramuscular DHE. The patients administered 0.5mg DHE and 100mg trimethobenzamide at the onset of their headache and an additional 0.5mg DHE if satisfactory headache relief was not obtained. Twenty patients were successfully contacted and interviewed. Forty-five percent of the patients had at least 50% relief of headache and continued to use the protocol. Eighty-two percent of patients who initially had at least 50% headache relief continued to use the drug, whereas none of the patients who initially had less than 10% relief continued the protocol. Sixty-one percent of patients whose headaches precluded continuation of activity had at least 50% response to initial treatment, whereas only 29% whose headaches were less severe had this response. Initial response to therapy was predictive of continued use of the treatment protocol and patients who described more severe headache had a higher response to the initial treatment. Thus, home administration of I.M. DHE offers an additional treatment regimen for patients with migraine headache.

Acute Disease↗

PubMed2006

A clinical trial of trimethobenzamide/diphenhydramine versus sumatriptan for acute migraines.

BACKGROUND: Although various classes of medication are used to treat acute migraine in the emergency department (ED), no treatment offers complete pain relief without side effects or recurrence of headache. Consequently, even though several antiemetic medications as well as SQ sumatriptan have demonstrated efficacy and tolerability for the ED treatment of migraine, there remains a need for more effective parenteral therapies. Open-label studies suggest that the combination of trimethobenzamide and diphenhydramine (TMB/DPH) may provide effective relief in a high proportion of migraineurs. OBJECTIVE: To test the hypothesis that ED patients with acute migraine, given intramuscular TMB/DPH, would have a larger reduction in their pain scores than patients given SQ sumatriptan. METHODS: This was an ED-based, randomized, double-blind, "double-dummy" clinical trial comparing 2 parenteral treatments for acute migraine headaches. Subjects received a combination of TMB 200 mg and DPH 25 mg as a single intramuscular injection or 6 mg of SQ sumatriptan. Pain scores, disability scores, associated symptoms, and adverse effects were assessed for 2 hours in the ED and by telephone 24 hours after medication administration. The primary outcome was the between-group difference in reduction of pain intensity as measured by a validated numerical rating scale 2 hours after medication administration. This study was designed to detect superiority of TMB/DPH; therefore, a 1-tailed t-test was used. An interim analysis was planned to terminate the trial if predetermined endpoints in the primary outcome variable were reached. RESULTS: The trial was stopped by the data monitoring committee after 40 subjects were enrolled because a substantial benefit in the primary outcome was found favoring sumatriptan. Baseline pain scores were comparable between the 2 groups. By 2 hours, sumatriptan subjects had improved by a mean of 6.1 and the TMB/DPH subjects had improved by a mean of 4.4 (95% CI for difference of 1.7: -0.1 to 3.4). By 24 hours after medication administration, sumatriptan subjects had a mean improvement from baseline of 4.9 as compared to 5.3 for TMB (95% CI for difference of -0.4: -2.4 to 1.6). The need for rescue medication was comparable between the groups. No serious or frequent adverse effects were noted in either group. CONCLUSIONS: SQ sumatriptan is probably superior to TMB/DPH for treating the pain of acute migraine at 2 hours. However, TMB/DPH was well-tolerated, efficacious, and relieved pain comparably to sumatriptan at 24 hours. TMB/DPH might have a role in select populations in which sumatriptan is contraindicated or likely to be ineffective.

Acute Disease↗

PubMedDate not supplied

Inappropriate medication prescribing for the elderly by office-based physicians.

OBJECTIVE: To estimate the prevalence of inappropriate medications prescribed by office-based physicians for patients 65 years or older. DESIGN: A nationwide cross-sectional survey of office visits by the elderly. SETTING: The National Ambulatory Medical Care Survey (NAMCS) 1992, a national probability sample survey of office visits by ambulatory patients within the continental US. SUBJECTS: A national probability sample of patients 65 years or older visiting office-based physicians. National estimates are based on the National Center for Health Statistics weighting procedure for the NAMCS sample. MAIN OUTCOME MEASURES: Prevalence of 20 inappropriate medications that should be entirely avoided in the elderly, using criteria developed by a panel of national experts in geriatric medicine and geriatric pharmacology. RESULTS: In the US during 1992, an estimated 8.47 million (95% CI 7.66 million to 9.28 million) office visits by the elderly indicated prescribing of at least 1 of the 20 inappropriate medications. Approximately 7.75 million (95% CI 6.98 million to 8.52 million) visits by the elderly involved 1 inappropriate medication and 0.72 million (95% CI 0.51 million to 0.93 million) visits included 2 inappropriate medications. According to the NAMCS, office-based physicians prescribed at least 1 inappropriate medication to 7.58% of the elderly who received prescriptions. The most frequently prescribed inappropriate medications were propoxyphene, amitriptyline, dipyridamole, diazepam, and chlorpropamide. Elderly patients rarely received prescriptions from office-based physicians for drugs such as secobarbital, isoxsuprine, trimethobenzamide, and carisoprodol. Furthermore, office-based physicians did not prescribe cyclandelate, pentobarbital, or phenylbutazone for the elderly. CONCLUSIONS: The prescribing of inappropriate medications by office-based physicians raises concerns regarding the quality of care for the elderly in ambulatory settings. The crux of improving patient care in ambulatory settings rests with collaborative efforts between physicians and pharmacists.

Aged↗

PubMed2004

Rapid treatment of "wearing off" in Parkinson's disease.

Patients with advanced Parkinson's disease (PD) may develop a variety of motor complications associated with levodopa therapy. Motor fluctuations, such as early morning akinesia and "wearing-off," may respond to individualized medical management with titrated combinations of levodopa, dopamine agonists, COMT inhibitors and amantadine. Often with disease progression, dyskinesias and unpredictable, rapid "off" periods will also emerge. These motor complications are less amenable to traditional anti-parkinson therapy manipulation. This manuscript reviews approaches for "rescue" therapy in PD patients with "wearing off," sudden "offs," early morning akinesia, and variable response to individual doses of oral medications. Strategies for preparing and administering liquid levodopa are discussed within the context of gastric emptying, intestinal absorption, and active transport across the blood brain barrier. In addition other levodopa preparations in early development, including the orally administered levodopa methyl ester and the potential for a subcutaneously administered levodopa ethyl ester are reviewed. Furthermore, practical guidelines regarding the dosing, administration, use of the antiemetic trimethobenzamide (Tigan), time to "on," duration of benefit, and potential side effects associated with subcutaneously injected apomorphine are provided.

Antiemetics↗

PubMed2004

Practical considerations in the use of apomorphine injectable.

This manuscript provides a practical summary of guidelines for institution of apomorphine subcutaneous injectable therapy, including patient education, pre-treatment issues, dosage titration and side-effect care. The timing of each injection is crucial if an impending "off" period is to be averted. Patients need to be aware of symptoms of an approaching "off" period, and the injection should be administered at the onset or ideally, in anticipation of an "off" episode. Patients being considered for apomorphine treatment should undergo pre-treatment assessment and optimization of ongoing oral therapy prior to initiation. Education and counseling regarding the benefits of apomorphine can often alleviate this. In addition, and where available, it is beneficial to provide the patient and caregiver(s) with additional written information and videos provided by the manufacturer demonstrating the operation of the pump or pen injection systems. Once a patient has been assessed as being a suitable candidate for apomorphine, an apomorphine challenge is performed to determine responsiveness and guide appropriate dosing, establish an individual dose, and to observe for side effects, such as nausea, postural hypotension, excessive somnolence, or dyskinesia. Three days prior to the challenge, domperidone 20 mg tid or trimethobenzamide (Tigan) 300 mg tid is recommended. Potential side effects include yawning, dopaminergic side effects, such as dyskinesias, nausea, orthostatic hypotension, confusion, hallucinations, somnolence and rarely, hypersexuality or other behavioral disturbances, and skin nodule formation.

Antiemetics↗

PubMed1993

Treatment of nausea and vomiting in pregnancy.

The nausea and vomiting that often accompany early pregnancy may be ameliorated if the patient eats small portions of food at frequent intervals, increases the amount of carbohydrates and decreases the amount of fat, and avoids bothersome food odors. When these strategies fail, antiemetic drugs such as pyridoxine and phosphorated carbohydrate solution may help, as well as doxylamine, promethazine or trimethobenzamide. When drugs are considered for use in pregnant patients, the safety of the patient and the fetus must always come first.

Decision Trees↗

PubMed1963