Lofexidine famously know with its brand name Lucemyra is a drug that is widely used to reduce opioid withdrawal symptoms after a patient stops taking opioid abruptly. Lucemyra is manufactured by WorldMeds and Salix companies based in the United States of America. This drug works by blocking the production of norepinephrine, a hormone that is likened to adrenaline which is known to largely contribute opioid withdrawal symptoms. Lucemyra, as mentioned before is indicated to facilitate discontinuation of opioid use among adults as it drastically helps to reduce the opioid withdrawal symptoms. However, it is only used for a short period of time (Horowitz, Shannon, & Keller, 2018).
Lucemyra belongs to the class of agonist at the α-2A, 2B, and 2C adrenergic receptor subtypes, with the highest activity at the alpha-2A receptor. Basically, Lucemyra is a generic drug that has been historically administered to patients of high blood pressure. In 2018, Lucemyra was approved for Drug Administration and Food in the United States of America. It is first in the class of adrenergic receptor agonist. Just like many other drugs, Lucemyra has common side effects that are associated with its use (Fast, & Fda, 2018).
To start with, patients using Lucemyra are in danger of getting bradycardia, low heartbeat rate –a condition known as hypotension. Lucemyra also causes syncope. Going by this dint, physicians, advanced practices nurses and other healthcare professionals who administer Lucemyra must sensitize patients to check themselves routinely to identify hypotension, orthostasis, bradycardia, and related indications. Moreover, patients are advised to remain hydrated, on the best way to perceive the side effects of hypotension, and how to mitigate the danger of genuine results if hypotension occur. Aside from hypotension, bradycardia, and syncope, Lucemyra have several other side effects (Price, 2018). There are higher chances that the central nervous system (CNS) depression as a result of the simultaneous use of depressants. Most likely Lucemyra potentiates the central nervous system depressive effects which result from depressants like benzodiazepines, barbiturates, and sedative drugs. Consequently, are advised to refrain from and cautiously do activities like the operation of heavy machines, driving and many others until the side effects of Lucemyra are conspicuous.
Another common side effect that patients using Lucemyra may experience is the emergence of discontinuation symptoms. It is recommended that patients only use Lucemyra for a short period of time. However, an abrupt termination Lucemyra’s usage can definitely cause a considerable increase of the blood pressure (Price, 2018). The discontinuation symptoms encompass extremity pain, anxiety, diarrhea, chills, insomnia, and hyperhidrosis. All these symptoms have been repeatedly observed with abrupt cessation of Lucemyra usage. Thereby, it highly recommended that if discontinuing therapy is necessary, then the patient should be subjected to a gradual should be subjected to a gradual dose reduction.
To add on the long list of Lucemyra side effects, patients using Lucemyra are faces a threat of QT prolongation: Since there is an alarming danger of protracting QT interval, it is imperative to avoid prescribing Lucemyra to patients with congenital long QT prolongation. It is also significant to frequently monitor electrocardiographs of patients in great risks of QT prolongation. In addition, Lucemyra elevates the risk of opioid overdose among patients whose opioid prescription is discontinued. It has been noted that if a patient completes opioid discontinuation, they tend to have a decreased tolerance to opioids. Ultimately, such a patient ends up being exposed to a great danger of fatal overdose in case they start using opioids again. This necessitates a comprehensive management strategy that regulates the use of Lucemyra when administered to mitigate the withdrawal symptoms associated with discontinuation of opioids. O A Lucemyra overdose often manifest itself as an acute hypotension, sedation, or bradycardia. In case of intense overdose, it is necessary to do a gastrointestinal lavage where suitable. Dialysis will not expel a significant percentage of overdosed medication. Instances of overdose oblige to commence with general characteristic and then proceed to steady measures in order to rescue the patient.
Regarding the so far discussed side effects, it is necessary to enumerate some precautions to patients to avoid the side effects. First, it is crucial to enlighten patients that Lucemyra adversely reduces the pressure of blood. As well patients should be aware of the fact that moving from a prostrate to vertical position might be a heightened risk for getting hypotension and orthostatic effects (Urquhart, 2018). Moreover, patients should be educated patients to remain hydrated, on the most proficient method to perceive side effects of low circulatory strain, and step by step instructions to decrease the danger of genuine results should hypotension happen (for instance, sit or rests, deliberately rise from a sitting or horizontal position). Outpatients should be advised to refrain from Lucemyra dosages while encountering side effects of drastic decrease in blood pressure or bradycardia and immediately inform their doctors.
There are several drugs that cannot be used together with Lucemyra or what are best described as contraindications. It is there indispensable that the manufacturer’s labeling of the drugs is precise. This way, the labels can be in case a more comprehensive information is needed to determine possible interaction with other drugs. This also helps in dose adjustments. Common Lucemyra’s contraindications include Methadone. Both Methadone and Lucemyra (lofexidine hydrochloride) are similar in the sense that they elongate QT interval. It is advisable not to use these two drugs concomitantly. Otherwise, an ECG monitoring is highly recommended. The next drug is Oral Naltrexone. Using Lucemyra and Oral Naltrexone has an effect of decreasing the effectiveness of oral naltrexone. In the case of CYP2D6 Inhibitors, concurrent application of paroxetine occasions saturation of plasma intensities of Lucemyra. A monitor is needed for indications of orthostasis and bradycardia with simultaneous use of a CYP2D6 inhibitor. CNS depressant drugs are other contraindications of Lucemyra whose concurrent application may increase the dangers of a patient experiencing severe side effects of the drug.
The prescription of Lucemyra is not universal for different types of populations or patients. Special considerations are made for different clients which include pediatric patients, geriatric patients, patients with renal dysfunctions, obese patients, and lactating and expectant patients. The special considerations encompass absorption, elimination, metabolism half-life, loading dose, route of drug administration, and steady state. Absorption of the drug is through the mouth bioavailability which is about 90%, the absorption is vigorous in the mouth. (Sevarino, 2017). The elimination of the drug’s by-products or unabsorbed particles is done by the kidney through the excretion process. Lucemyra has a metabolism half-life of about 11 hours and it takes place in the liver.
As mentioned earlier, the prescription of Lucemyra dose should be done with a lot of caution and consideration. The general dose is described as follows: Beginning dosage: Three 0.18-mg tablets (0.54 mg) PO QID (5-6 hours between measurements) amid the time of pinnacle withdrawal symptoms (for the most part the initial 5-7 days after last opioid application). Not to surpass an aggregate day by day dosage of 2.88 mg (16 tablets). No single measurement ought to surpass 0.72 mg (4 tablets). Treatment might be proceeded for up to 14 days with dosing guided by side effects. The measurement ought to be lessened, held, or ended for people who exhibit a more noteworthy affectability. Lower dosages might be proper as opioid withdrawal manifestations wane (Horowitz, Shannon, and Keller, 2018). Cease by progressively diminishing the measurements over a 2-to 4-day time span to alleviate lofexidine withdrawal indications (for instance, decreasing by 1 tablet for every dosage each 1-2 days). Lucemyra is administered orally.
Pediatric Patients
Owing to the fact that these patients reaction to medication is quite unpredictable, accurate dosing, especially for a drug like Lucemyra, is vital due to their small body mass. However, safety and efficacy for administering Lucemyra to pediatric patients have not been established (Horowitz, Shannon, & Keller, 2018).
Geriatric Patients
Like in the case of pediatric patients, there are no studies that have been done to establish efficacy and safety or to mark pharmacokinetics of Lucemyra among geriatric patients. However, it is advisable to take caution when administering the drug to patients of 65 years and above. The dose given to these patients is similar to that given to people suffering from renal dysfunction.
Patients with Renal Dysfunction
While renal dysfunction impedes the clearance of Lucemyra, it shows less effect on the highest plasma intensity than on AUC values after one dose. It is recommended that the dose is adjusted based on the degree of impairment as clinical pharmacologists suggest. It is also significant to note that just a very small fraction Lucemyra dose is removed when a typical dialysis is underway. As such, no extra dose should be administered when a dialysis session has ended (Horowitz, Shannon, & Keller, 2018). Essentially, Lucemyra may be administered even if the dialysis period is not timed. Clinically, pertinent QT elongation may happen in subjects with renal dysfunction. The dose is adjusted as follows: Mild or moderate (eGFR 30-89.9 mL/min/1.73 m²): 2 tablets QID (1.44 mg/day), Severe (eGFR <30 mL/min/1.73 m²), ESRD, or dialysis: 1 tablet QID (0.72 mg/day), Maybe administered without regard to timing of dialysis
Patients with Liver Dysfunction
Liver dysfunction or hepatic impairment is known to slow slows the removal of Lucemyra but it also shows less effect on the highest plasma intensity than on AUC values after one dose, just like in the case of renal impairment (Horowitz, Shannon, & Keller, 2018). Similarly, dosage adjustments are highly recommended to be done based on the degree of hepatic impairment Clinically, pertinent QT elongation may happen in subjects with liver dysfunction The dose is adjusted as follows: Moderate (Child-Pugh score 7-9): 2 tablets QID (1.44 mg/day), Severe (Child-Pugh score >9): 1 tablet QID (0.72 mg/day)
Obese Patients
Obese patients experience alterations in their pharmacokinetics and pharmacodynamics responses to medication. Several comorbidities and transformed nutritional status are major concerns when treating obese patients. As such, they need an accurate dose, especially for Lucemyra –a drug which may have fatal side effects (Horowitz, Shannon, & Keller, 2018).
Pregnancy/ Lactation
In these two population, administering Lucemyra is quite challenging as the life of the fetus must be considered for the case of expectant patients. Similarly, the life of the breastfeeding child must be considered for lactating mothers. The safety and efficacy of Lucemyra’s administration among these populations have not been established. However, extensive research in animal reproduction has revealed some meaningful information that may be relevant to these populations (Horowitz, Shannon, & Keller, 2018). When Lucemyra is administered orally, at stage of organogenesis, to expectant rabbits as well as rats, it causes a decline in weight of the fetus but increases fetal resorptions.
At the point when oral lofexidine is administered from the earliest starting point of organogenesis all the way to lactation, expanded miscarriages as well as litter misfortune were noted alongside diminished suitability and lactation records. The posterity showed delays in sexual development, sound-related disconcert, and surface correcting. All the impacts happened at conditions below those in human beings (Horowitz, Shannon, & Keller, 2018). There is no certified information in regards to the nearness of Lucemyra efficacy and safety in lactating mothers and their babies, or the impacts on drain generation. Importantly, safety measures and precautions should be observed when Lucemyra is managed to a nursing mother.
References
Fast, A., & Fda, F. (2018). NEW DRUG UPDATE. Ophthalmology.
Horowitz, B., Shannon, A., & Keller, L. (2018) US WORLDMEDS AND SALIX ANNOUNCE US LAUNCH OF LUCEMYRA™(lofexidine) 0.18 MG TABLETS.
Price, L. H. (2018). Lofexidine: Less than meets the eye. The Brown University Psychopharmacology Update, 29(9), 7-7.Traynor, K. (2018). FDA approves nonopioid medication for managing opioid withdrawal.
Sevarino, K. (2017). Medically Supervised opioid withdrawal during treatment for addiction. UpToDate, Saxon, A. Hermann, R (Ed), UpToDate, Waltham, MA.(Accessed on January 1 2016). Google Scholar.
Urquhart, L. (2018). Regulatory watch: FDA new drug approvals in Q2 2018.
