Actions of Proeptatriene in details
Proeptatriene relieves skeletal muscle spasm of local origin without interfering with muscle function. Proeptatriene has not been shown to be effective in muscle spasm due to central nervous system disease. In animal models, Proeptatriene reduced or abolished skeletal muscle hyperactivity. Animal studies indicate that Proeptatriene does not act at the neuromuscular junction or directly on skeletal muscle. Such studies show that Proeptatriene acts primarily within the central nervous system at the brain stem as opposed to the spinal cord level, although an overlapping action on the latter may contribute to its overall skeletal muscle relaxant activity. Evidence suggests that the net effect of Proeptatriene is a reduction of tonic somatic motor activity, influencing both gamma (γ) and alpha (α) motor systems. Pharmacological studies in animals demonstrated a similarity between the effects of Proeptatriene and the structurally related tricyclic antidepressants, including reserpine antagonism, norepinephrine potentiation, potent peripheral and central anticholinergic effects, and sedation. Proeptatriene caused slight to moderate increase in heart rate in animals.
How should I take Proeptatriene?
Take Proeptatriene only as directed by your doctor. Do not take more of it and do not take it more often than your doctor ordered. To do so may increase the chance of serious side effects.
Dosing
The dose of Proeptatriene will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of Proeptatriene. If your dose is different, do not change it unless your doctor tells you to do so.
The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.
- For relaxing stiff muscles:
- For the oral dosage form (tablets):
- Adults and teenagers 15 years of age and older—The usual dose is 10 milligrams (mg) three times a day. The largest amount should be no more than 60 mg (six 10-mg tablets) a day.
- Children and teenagers up to 15 years of age—Dose must be determined by your doctor.
- For the oral dosage form (extended-release capsules):
- Adults—The usual dose is 15 mg once a day. Some patients may require up to 30 mg (one 30 mg capsule or two 15 mg capsules) per day.
- Children—Use and dose must be determined by your doctor.
- For the oral dosage form (tablets):
Missed Dose
If you miss a dose of Proeptatriene, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
Storage
Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.
Ask your healthcare professional how you should dispose of any medicine you do not use.
Keep out of the reach of children.
Do not keep outdated medicine or medicine no longer needed.
Proeptatriene administration
Take this medication exactly as it was prescribed for you. Do not take the medication in larger amounts, or take it for longer than recommended by your doctor. Follow the directions on your prescription label.
Take this medicine with a full glass of water.
Do not crush, chew, break, or open an extended-release capsule. Swallow the pill whole. Breaking or opening the pill may cause too much of the drug to be released at one time.
Proeptatriene is only part of a complete program of treatment that may also include rest, physical therapy, or other pain relief measures. Follow your doctor's instructions.
Store Proeptatriene at room temperature away from moisture, heat, and light.
Proeptatriene pharmacology
Mechanism of Action
Proeptatriene relieves skeletal muscle spasm of local origin without interfering with muscle function. Proeptatriene has not been shown to be effective in muscle spasm due to central nervous system disease. In animal models, Proeptatriene reduced or abolished skeletal muscle hyperactivity. Animal studies indicate that Proeptatriene does not act at the neuromuscular junction or directly on skeletal muscle. Such studies show that Proeptatriene acts primarily within the central nervous system at the brain stem as opposed to the spinal cord level, although an overlapping action on the latter may contribute to its overall skeletal muscle relaxant activity. Evidence suggests that the net effect of Proeptatriene is a reduction of tonic somatic motor activity, influencing both gamma (γ) and alpha (α) motor systems. Pharmacological studies in animals demonstrated a similarity between the effects of Proeptatriene and the structurally related tricyclic antidepressants, including reserpine antagonism, norepinephrine potentiation, potent peripheral and central anticholinergic effects, and sedation. Proeptatriene caused slight to moderate increase in heart rate in animals.
Pharmacokinetics
Absorption
Following single-dose administration of Proeptatriene 15 mg and 30 mg in healthy adult subjects (n=15), Cmax, AUC0-168h and AUC0-∞ increased in an approximately dose-proportional manner from 15 mg to 30 mg. The time to peak plasma Proeptatriene concentration (Tmax) was 7 to 8 hours for both doses of Proeptatriene.
A food effect study conducted in healthy adult subjects (n=15) utilizing a single dose of Proeptatriene 30 mg demonstrated a statistically significant increase in bioavailability when Proeptatriene 30 mg was given with food relative to the fasted state. There was a 35% increase in peak plasma Proeptatriene concentration (Cmax) and a 20% increase in exposure (AUC0-168h and AUC0-∞) in the presence of food. No effect, however, was noted in Tmax or the shape of the mean plasma Proeptatriene concentration versus time profile. Proeptatriene in plasma was first detectable in both the fed and fasted states at 1.5 hours.
When the contents of Proeptatriene capsules were administered by sprinkling on applesauce, it was found to be bioequivalent to the same dose when administered as an intact capsule.
In a multiple-dose study utilizing Proeptatriene 30 mg administered once daily for 7 days in a group of healthy adult subjects (n=35), a 2.5-fold accumulation of plasma Proeptatriene levels was noted at steady-state.
Metabolism and Excretion
Proeptatriene is extensively metabolized and is excreted primarily as glucuronides via the kidney. Cytochromes P-450 3A4, 1A2, and, to a lesser extent, 2D6, mediate N-demethylation, one of the oxidative pathways for Proeptatriene. Proeptatriene has an elimination half-life of 32 hours (range 8-37 hours; n=18); plasma clearance is 0.7 L/min following single dose administration of Proeptatriene.
Special Populations
Elderly
Although there were no notable differences in Cmax or Tmax, Proeptatriene plasma AUC is increased by 40% and the plasma half-life of Proeptatriene is prolonged in elderly subjects greater than 65 years of age (50 hours) after dosing with Proeptatriene compared to younger subjects 18 to 45 years of age (32 hours). Pharmacokinetic characteristics of Proeptatriene following multiple-dose administration of Proeptatriene in the elderly were not evaluated.
Hepatic Impairment
In a pharmacokinetic study of immediate-release Proeptatriene in 16 subjects with hepatic impairment (15 mild, 1 moderate per Child-Pugh score), both AUC and Cmax were approximately double the values seen in the healthy control group. The pharmacokinetics of Proeptatriene in subjects with severe hepatic impairment is not known.
References
- NCIt. "Cyclobenzaprine: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
- EPA DSStox. "Cyclobenzaprine: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).
Reviews
The results of a survey conducted on ndrugs.com for Proeptatriene are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Proeptatriene. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.User reports
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Information checked by Dr. Sachin Kumar, MD Pharmacology
