Tafenoquine Succinate

194.23

194.23

939U7C91AI

1650

Pale Yellow to Light Yellow

N06BA14|N - Nervous system

1.166±0.06 g/cm3(Predicted)

399.2±35.0 °C(Predicted)

13.37±0.50(Predicted)

Store at -20°C

Age, gender, and race do not significantly affect solriamfetol pharmacokinetics and no dose adjustments were made in clinical trials for patients over 65 years. Patients with renal failure experience increases in half life between 1.2 and 3.9 times that in healthy patients. 21% of solriamfetol was removed by hemodialysis, however time to peak concentration was not affected. Solriamfetol is not expected to lead to adverse effects in pregnancy. Maternal and fetal toxicity was seen in animal studies at ≥4 and 5 times the maximum recommended human dose and teratogenicity was seen at 19 and ≥5 times the maximum recommended human dose. Breastfed infants should be monitored for adverse reactions such as agitation, insomnia, anorexia, and reduced weight gain as solriamfetol is present in breast milk. However, there is no currently available data on the effect of solriamfetol in breast milk on breast fed inants. Safety and effectiveness of solriamfetol in pediatric patients has not been established in clinical studies. Solriamfetol does not display different safety or effectiveness in geriatric populations. Dosage adjustments are recommended for patients with eGFR <60mL/min/1.73m^2 and solriamfetol is not recommended for patients with an eGFR <15mL/min/1.73m^2.

In placebo-controlled trials of solriamfetol in patients with narcolepsy, minor serum aminotransferase elevations occurred in a small proportion of patients during therapy, but the rates of enzyme elevations overall were similar to those in placebo recipients. In preregistration trials, there were no instances of clinically apparent liver injury or serum aminotransferase elevations with jaundice attributable to solriamfetol. Since its approval in 2019, there have been no publications describing clinically apparent liver injury due to solriamfetol.

13.3% to 19.4% protein bound over a plasma concentration range of 0.059 to 10.1mcg/mL.

Solriamfetol is indicated for treatment of daytime sleepiness associated with obstructive sleep apnea and narcolepsy, but is not a treatment for the underlying airway obstruction in apnea patients.|FDA Label|Sunosi is indicated to improve wakefulness and reduce excessive daytime sleepiness in adult patients with narcolepsy (with or without cataplexy).Sunosi is indicated to improve wakefulness and reduce excessive daytime sleepiness (EDS) in adult patients with obstructive sleep apnoea (OSA) whose EDS has not been satisfactorily treated by primary OSA therapy, such as continuous positive airway pressure (CPAP). 

Solriamfetol is dopamine and norepinephrine reuptake inhibitor that is used in the therapy of excessive daytime sleepiness and cataplexy in patients with narcolepsy. Solriamfetol has not been associated with serum enzyme elevations during therapy or to instances of idiosyncratic acute liver injury.

CNS Drugs

Solriamfetol weakly binds to dopamine and norepinephrine transporters but not serotonin transporters. Solriamfetol does not bind to dopamine, serotonin, norepinephrine, GABA, adenosine, histamine, orexin, benzodiazepines, or muscarinic and nicotinic receptors. Solriamfetol is also associated with a mean increase of 21 beats per minute (BPM) in heart rate in patients taking 300mg (twice the maximum recommended dose) and 27 BPM in patients taking 900mg (six times the maximum recommended dose). 300mg of solriamfetol does not increase the QTcF interval to a clinically relevant degree.

Oral bioavailability of solriamfetol is approximately 95%. Peak plasma concentration is reached in 2 hours (with a range of 1.25 to 3 hours) in fasted patients. When solriamfetol is taken with a high fat meal, the time to peak plasma concentration increases to 3 hours.|95% of solriamfetol is recovered in urine unchanged by metabolism. Less than 1% of solriamfetol is recovered as N-acetyl solriamfetol.|199L. Other studies have found the volume of distribution to be 158.2L ± 37.3L in fasted subjects and 159.8L ± 38.9L in fed subjects.|Renal clearance is 18.2L/h and total clearance is 19.5L/h. Other studies have found clearance to be 18.4 ± 4.2L/h in fasted subjects and 18.8 ± 4.2L/h in fed subjects.

Solriamfetol does not undergo significant metabolism in humans, though less than 1% of solriamfetol is metabolized to N-acetyl solriamfetol.

7.1 hours. Other studies have found the mean half life to be 6.1 ± 1.2 hours in fasted subjects and 5.9 ± 1.2 hours in fed subjects.

The specific mechanism of action is unknown but it may be through its activity as a dopamine and norepinephrine reuptake inhibitor.

(2R)-2-amino-3-phenylpropyl carbamate

Solriamfetol|1650|Schedule IV - Substances in the DEA Schedule IV have a low potential for abuse relative to substances in Schedule III.|No

Human drugs -> Sunosi -> EMA Drug Category|Psychoanaleptics -> Human pharmacotherapeutic group|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients