Lofexidine and opioid withdrawal

Cox, Stuart; Alcorn, Ron

doi:10.1016/s0140-6736(95)92593-7

Cited by 15 publications

(9 citation statements)

References 6 publications

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“…The noradrenergic system has been implicated in stress-induced reinstatement of drug seeking. Lofexidine, an α2 adrenergic receptor agonist, reduces opioid withdrawal symptoms by decreasing noradrenergic outflow in the CNS (105). Animal models have demonstrated that lofexidine attenuates footshock-induced reinstatement of drug seeking (106), as administration of α2 adrenergic receptor agonists or selectively lesioning noradrenergic projections to forebrain areas effectively blocks stress-induced reinstatement in rats (106,107).…”

Section: Therapiesmentioning

confidence: 99%

Making a bad thing worse: adverse effects of stress on drug addiction

Cleck¹,

Blendy²

2008

J. Clin. Invest.

105

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Sustained exposure to various psychological stressors can exacerbate neuropsychiatric disorders, including drug addiction. Addiction is a chronic brain disease in which individuals cannot control their need for drugs, despite negative health and social consequences. The brains of addicted individuals are altered and respond very differently to stress than those of individuals who are not addicted. In this Review, we highlight some of the common effects of stress and drugs of abuse throughout the addiction cycle. We also discuss both animal and human studies that suggest treating the stress-related aspects of drug addiction is likely to be an important contributing factor to a long-lasting recovery from this disorder.

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Section: Therapiesmentioning

confidence: 99%

Making a bad thing worse: adverse effects of stress on drug addiction

Cleck¹,

Blendy²

2008

J. Clin. Invest.

105

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“…It is a structural analog of clonidine but has a higher affinity and specificity for alpha (α) two A subtype of the receptors, thereby reducing the sympathetic outflow. This makes it more efficacious and suitable for the treatment of opiate withdrawal [9]. The alpha (α) two A subtype receptor is a Gi protein-coupled receptor.…”

Section: Reviewmentioning

confidence: 99%

Clinical Efficacy and Safety Profile of Lofexidine Hydrochloride in Treating Opioid Withdrawal Symptoms: A Review of Literature

Rehman¹,

Maqsood²,

Bajwa³

et al. 2019

Cureus

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Opioid use disorder (OUD) is a rapidly growing challenge worldwide and is characterized by an increase in dependence on opioids up to a point that a person loses control over the drug use. Multiple drugs are approved for its treatment, including methadone, buprenorphine, and diazepam. Although not approved, clonidine is also used for the treatment of OUD. On May 16, 2018, the United States Food and Drug Administration (FDA) approved a new drug lofexidine hydrochloride for the treatment of opioid withdrawal symptoms. Lofexidine is a centrally acting alpha two receptor agonist. It reduces the neurochemical surge by inhibiting the conversion of adenosine triphosphate (ATP) into cyclic adenosine monophosphate (cAMP) which in turn decrease the sympathetic outflow. This results in the improvement of withdrawal symptoms. When compared with methadone and buprenorphine, it is equally effective in controlling withdrawal symptoms. Its efficacy is also similar to clonidine with a better side effects profile. The adverse effects of lofexidine include bradycardia, hypotension, orthostasis, somnolence, sedation, dry mouth, and rebound elevations in blood pressure and prolongation of QT interval. Lofexidine is contraindicated in patients who are on beta-blockers and angiotensin converting enzyme inhibitors (ACE inhibitors). In our review, we have discussed the clinical efficacy and safety profile of lofexidine in treating opioid withdrawal symptoms and its comparison to other available treatment options.

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“…Approved in the UK as an aid to opioid detoxification, lofexidine is better tolerated and causes less hypotension than clonidine 312. Nevertheless, lofexidine has not been extensively tested for opioid detoxification 313. Guanfacine is a second α 2 ‐adrenergic agonist 314 examined for its ability to attenuate opioid withdrawal.…”

Section: New Approaches For Treatment Of Opiate Dependence and Withdrmentioning

confidence: 99%

Neurobiological Adaptations to Psychostimulants and Opiates as a Basis of Treatment Development

Sevarino

Oliveto

Kosten

2000

Annals of the New York Academy of Sciences

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Abuse of illicit substances, in particular psychostimulants and opiates, is a worldwide public health issue. Chronic use of cocaine and amphetamine causes common neurobiological adaptations that may guide new treatment development. These include perturbations in dopamine and serotonin neurotransmission, leading to trials of antidepressants, and serotonin and dopamine augmentation strategies. The detection of cerebral perfusion abnormalities caused by psychostimulants has led to examination of antiplatelet and excitatory amino acid (EAA) antagonist therapies. Further, development of cocaine vaccines allows for testing of peripheral blockade approaches to cocaine addiction. New approaches to behavioral treatments for cocaine dependence are also reviewed. For opiate dependence, understanding of heroin's effects on μ and κ opiate receptors has led to investigations of the partial μ agonist buprenorphine in opiate maintenance. Evidence for hyper‐excitability of locus coeruleus (LC) noradrenergic neurons and EEA inputs to the LC guides trials of new α2‐adrenergic agonists and EEA antagonists to alleviate opiate withdrawal. Finally, clinical experience with withdrawal from methadone and LAAM has led to trials of antagonist‐accelerated opiate withdrawal. Improved treatment of psychostimulant and opiate addiction is critically needed, and likely to have wide‐reaching impact in health care and society.

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Lofexidine and opioid withdrawal

Cited by 15 publications

References 6 publications

Making a bad thing worse: adverse effects of stress on drug addiction

Making a bad thing worse: adverse effects of stress on drug addiction

Clinical Efficacy and Safety Profile of Lofexidine Hydrochloride in Treating Opioid Withdrawal Symptoms: A Review of Literature

Neurobiological Adaptations to Psychostimulants and Opiates as a Basis of Treatment Development

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