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Analgesics during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Butalbital is a short-acting barbiturate that is contained in a variety (over 40) of available prescription analgesic compounds. Butalbital is usually combined with aspirin or acetaminophen (with or without caffeine). The most common indication for butalbital-containing analgesic compounds is tension headaches. All barbiturates cross the placenta, as do acetaminophen and aspirin. Barbiturate use in the first trimester was not associated with an increase in the frequency of congenital anomalies in exposed offspring. However, barbiturates have been associated with fetal dependence and newborn withdrawal symptoms when used chronically by the mother in the third trimester. Butalbital use during the first trimester in 73 women resulted in increased frequency of congenital heart defects during pregnancy (Browne et al., 2014). In a large birth defects study, a case-control analysis that contained only 8 exposed cases found a significant increase in the frequency of hypospadias (Lind et al., 2013).
Migraine: diagnosis and treatment
Published in Stephen D. Silberstein, Richard B. Upton, Peter J. Goadsby, Headache in Clinical Practice, 2018
Stephen D. Silberstein, Richard B. Upton, Peter J. Goadsby
No randomized, placebo-controlled studies have established the efficacy of butalbital-containing agents in the treatment of acute migraine headaches.64 Because of concerns about overuse, medication–overuse headache, and withdrawal, the use of butalbital–containing analgesics should be limited and carefully monitored. Their use should be limited to situations wherein a more specific or less potentially problematic agent cannot be used or is ineffective. They may be very effective as back-up medications when other migraine medications have failed. For an individual attack, patients should take one or two tablets or capsules, with a maximum of six per attack. The most frequent adverse reactions are drowsiness and dizziness. Drug use should be limited to no more than 2–3 treatment days per week.
Low Back Pain and Sciatica: Pathogenesis, Diagnosis and Nonoperative Treatment
Published in Gary W. Jay, Practical Guide to Chronic Pain Syndromes, 2016
Muscle spasmolytics or “relaxants” are traditionally used to treat painful musculoskeletal disorders, but share sedation and sometimes dizziness as common side effects; therefore, some clinicians prescribe them only at bedtime. Some muscle spasmolytics are also considered potentially addictive and have abuse potential, especially more traditional agents such as diazepam, butalbital, and phenobarbital. Examples of commonly used muscle relaxants include cyclobenzaprine, carisoprodol, methocarbamol, chlorzoxazone, and metaxalone. Benzodiazepines may be appropriate for concurrent anxiety states, and in these cases, clonazepam should be considered. Clonazepam operates via GABA-mediated mechanisms through internuncial neurons of the spinal cord to provide muscle relaxation (58). Another benzodiazepine, tetrazepam, showed strong evidence of efficacy, when compared to placebo, for improving short-term pain and moderate evidence for short-term improvement of muscle spasm, but any data for long-term use was lacking (59). A review and analysis of randomized or double-blinded controlled trials showed that muscle relaxants were effective for management of LBP, but adverse side effects limited their utility (60). A similar comprehensive meta-analysis of the effectiveness of cyclobenzaprine showed evidence to support short-term use (<4 days) citing modest benefit in early LBP, but with the same problematic side effects (61). Tizanidine is a central alpha-2-adrenoreceptor agonist that was developed for the management of spasticity due to cerebral or spinal cord injury, but also has demonstrated efficacy when compared to other muscle spasmolytics (62). Controlled clinical trials have demonstrated clinical efficacy of tizanidine, including reduced analgesic use and muscle spasm, in patients with acute neck and back pain (63, 64).
Recent advancements in tension-type headache: a narrative review
Published in Expert Review of Neurotherapeutics, 2021
Enrico Bentivegna, Michelangelo Luciani, Vincenzo Paragliola, Francesco Baldari, Piera A Lamberti, Giulia Conforti, Valerio Spuntarelli, Paolo Martelletti
There are no comparative studies examining the efficacy of combination analgesics with codeine [89]. Combinations of simple analgesics with codeine or barbiturates should not be used because increase the risk of developing medication-overuse headache. Drugs with psychotropic effects such as opioids and barbiturates are known to increase propensity for overuse, which can cause or contribute to the transformation of episodic TTH to chronic TTH and medication overuse headache [120]. In addition, as these drugs can give toxicity, dependence, and tolerance, neither opioids nor barbiturates should be used in TTH, especially when better options are available such as simple analgesics and combined analgesics containing caffeine. Butalbital in TTH can be considered when these options are ineffective or even relatively contraindicated (e.g. NSAIDs in late pregnancy).
Medication overuse headache: an overview of clinical aspects, mechanisms, and treatments
Published in Expert Review of Neurotherapeutics, 2020
Abouch V. Krymchantowski, Carla C. Jevoux, Ana G. Krymchantowski, Rodrigo Salvador Vivas, Raimundo Silva-Néto
The overuse of symptomatic medications becomes more consistent with the time and is anticipated with increased refractoriness and subsequent escalation of the number of headache days [30]. This clinical behavior was demonstrated elegantly by Bigal et al., who reported in the American Migraine Prevalence and Prevention study (AMPP) that drug combinations with barbiturates (as butalbital) predict the 1-year transformation of episodic migraine to MOH if used 5 or more days per month, opioids if taken 8 or more days per month, and triptans if taken 10 or more days per month. However, nonsteroidal anti-inflammatory drugs (NSAIDs) if used 5 or fewer days per month revealed a protective effect against MOH but could result in medication-overuse headache if taken 10 or more days per month [31].
Extracorporeal elimination of butalbital in acute aspirin–butalbital–caffeine–codeine (Fiorinal with Codeine) poisoning
Published in Clinical Toxicology, 2018
Janelle O. Poyant, Robert Albright, Jeremy Clain, Govind Pandompatam, Erin F. Barreto
Butalbital is a small molecule (approximately 220 Da), with 26% protein binding, 0.8 L/kg volume of distribution and is eliminated nearly 80% unchanged in the urine. The expected peak concentration is 2 mg/L 1.5 h after a 100 mg dose and the reported half-life is 35 h in patients with preserved end organ function [1]. Approximately 8 h after ingestion of 2000mg of butalbital, our patient’s serum concentration was 26.9 mg/L, well in excess of the 10 mg/L threshold for toxicity, with an estimated total body burden of 1076 mg [8]. The total body elimination of butalbital was approximately 60% at the end of the four-hour hemodialysis session. Given the patient’s preserved end organ function, endogenous clearance of butalbital likely continued throughout hemodialysis, which could not be formally quantified with the existing data points. However, given the long endogenous drug half-life (35 h) and the observed butalbital effluent concentrations, extracorporeal removal likely explains the majority of observed total drug clearance during this interval. However, it remains unclear as to why the patient awoke so quickly, approximately 35 minutes, into the hemodialysis session. One potential explanation for improvement in her mental status given the butalbital concentration was still 21.3 mg/L for 2 h into dialysis could have been helped in the removal of salicylate component, although it would be somewhat atypical to experience this degree of cognitive decline in acute salicylate ingestion with a peak concentration <50 mg/dL (< 3.6 mmol/L), and this cannot be speculated from this case report due to the lack of data points collected.