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Monographs of Topical Drugs that Have Caused Contact Allergy/Allergic Contact Dermatitis
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Orphenadrine (2-methyldiphenhydramine) is a tertiary amino compound which is the phenyl-o-tolylmethyl ether of 2-(dimethylamino)ethanol. It has a role as a NMDA receptor antagonist, a H1-receptor antagonist, an antiparkinson drug, a parasympatholytic, a muscle relaxant, a muscarinic antagonist and an antidyskinesia agent. Orphenadrine is indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomfort associated with acute painful musculoskeletal conditions. In pharmaceutical products, orphenadrine is employed as orphenadrine citrate (CAS number 4682-36-4, EC number 225-137-5, molecular formula C24H31NO8) or as orphenadrine hydrochlo- ride (CAS number 341-69-5, EC number 206-435-4, molecular formula C18H24ClNO) (1).
Nonopiate Analgesics and Adjuvants
Published in Gary W. Jay, Practical Guide to Chronic Pain Syndromes, 2016
Orphenadrine citrate (Norflex, Norgesic) is a centrally acting skeletal muscle relaxant with anticholinergic properties thought to work by blocking neuronal circuits, the hyperactivity of which may be implicated in hypertonia and spasm. It is available in injectable and oral formulations. The IM dose of Norflex is 2 mg, while the intravenous dosage is 60 mg in aqueous solution. The oral formulation (Norflex) is given in 100-mg tablets—one tablet every 12 hours. Norgesic is a combination form, including caffeine and aspirin and should be given one or two tablets every six to eight hours. Norgesic Forte, a stronger combination, is given one half to one tablet every six to eight hours. Because of its anticholinergic effects, it should be contraindicated in patients with glaucoma, prostatic enlargement, or bladder outlet obstruction. Its major side effects are also secondary to its anticholinergic properties and include tachycardia, palpitations, urinary retention, nausea, vomiting, dizziness, constipation, and drowsiness. It may also cause confusion, excitation, hallucinations, and syncope.
Nonopiate Analgesics and Adjuvants
Published in Gary W. Jay, Clinician’s Guide to Chronic Headache and Facial Pain, 2016
Orphenadrine citrate (Norflex, Norgesic) is a centrally acting skeletal muscle relaxant with anticholinergic properties thought to work by blocking neuronal circuits, the hyperactivity of which may be implicated in hypertonia and spasm. It is available in injectable and oral formulations. The IM dose of Nor-flex is 2 mg, while the intravenous dosage is 60 mg in aqueous solution. The oral formulation (Norflex) is given in 100-mg tablets—one tablet every 12 hours. Norgesic is a combination form, including caffeine and aspirin and should be given one or two tablets every six to eight hours. Norgesic Forte, a stronger combination, is given one half to one tablet every six to eight hours. Because of its anticholinergic effects, it should be contraindicated in patients with glaucoma, prostatic enlargement, or bladder outlet obstruction. Its major side effects are also secondary to its anticholinergic properties and include tachycardia, palpitations, urinary retention, nausea, vomiting, dizziness, constipation, and drowsiness. It also cause confusion, excitation, hallucinations, and syncope.
Twenty-four-hour postoperative orphenadrine and ketorolac infusion efficiently precedes orphenadrine-diclofenac infusion as an opioid-sparing analgesic modality after mastectomy
Published in Egyptian Journal of Anaesthesia, 2023
Yehya Shahin Dabour, Ahmed Said Elnoury, Ahmed Abouelgheit Daoud
Orphenadrine citrate is a centrally acting muscle relaxant with anti-muscarinic effects and was used for Parkinsonism treatment and alleviation of the antipsychotic drug-induced neuroleptic syndrome [7]. Earlier studies reported the analgesic effectiveness of the combination of orphenadrine-paracetamol in neck pain [8] and the opioid-sparing effect of the combination of orphenadrine/diclofenac (O/D combination) after unilateral total hip arthroplasty [9]. Thereafter, another study observed no improvement in pain intensity or physical functioning tests after the administration of four intravenous drugs including the O/D combination for patients with chronic low-back pain [10]. On contrary, a recent study documented the effectiveness of the infusion of an O/D combination for the relief of acute back musculoskeletal pain syndrome [4]. These discrepant results indicated the effectiveness of infusion of O/D combination for the management of acute not for chronic pain, however, depending on these results other combinations may be more effective.
Prevalence and pattern of substance use and misuse among anesthesia health-care personnel in Jordan
Published in Journal of Substance Use, 2019
Shahd Al-Maaz, Rana Abu-Dahab, Munir Shawagfeh, Mayyada Wazaify
Other documented drugs of abuse were combination of chlorpheniramine and orphenadrine/paracetamol. This documentation was by a resident who stated in the questionnaire that he used these two drugs for their mind-altering effect. This draws the attention back to the fact that OTC drug abuse should not be overlooked. The literature documented more than 80 cases of death due to orphenadrine overdose in the late 90s which led to its removal from the Scandinavian countries’ market later on (Gjerden, Bramness, & Slørdal, 2009). However, it is still considered an OTC drug in some other countries (Gjerden et al., 2009). Orphenadrine is an anticholinergic drug derived from diphenhydramine a first-generation antihistamine (Gjerden et al., 2009). It has several therapeutic indications such as Parkinson disease and muscle pain. However, anticholinergic drugs also have been documented as drugs of abuse since they can cause euphoria and hallucinations (Caplan, Epstein, Quinn, Stevens, & Stern, 2007). Abusers have different routes of administration for these drugs such as oral and intravenous routes to reach the euphoric effect (Caplan et al., 2007).
Can we estimate the critical micelle concentration of amphiphilic drug bases from molecular connectivity indices?
Published in Pharmaceutical Development and Technology, 2018
Wiebke Saal, Nicole Wyttenbach, Jochem Alsenz, Martin Kuentz
Despite of the research progress in drug aggregation, there are still many open questions of high relevance to pharmaceutics. It would be of great interest to identify surfactant-like compounds early on and to estimate their CMC values based on molecular structure only. As an example of molecular association of an amphiphilic base, orphenadrine HCl with an aggregation number of seven molecules, is displayed in Figure 1 (Attwood & Florence 1983). The given molecular arrangement is a proposal of how a likely structure can be visualized. The protonated amine forms a polar head group that protrudes into the aqueous phase where it interacts with anions. An aggregation structure of a drug like orphenadrine HCl is expected to be less ordered than structures of typical surfactant micelles. Many surfactants build rather ordered micelles due to their well-defined hydrophobic tails that can be simple unbranched alkanes. By contrast, a typical amphiphilic drug like, for example, orphenadrine has a rather complex hydrophobic moiety. Also the separation of polar head and lipophilic tail group is often not simple compared to other surfactant structures. However, despite of such differences between drugs and surfactants, it is an interesting approach to learn from recent advances in the surfactant sciences as they can lead to innovative and hypothesis-driven research about amphiphilic pharmaceuticals.