Actions of Pms-Gabapentin in details
Pharmacology: Mechanism of Action: Pms-Gabapentin has proven affinity for special site in brain tissues eg, neocortex and hippocampus. Though exact mechanism of its central nervous system (CNS) depressant and anticonvulsant activity is not fully understood, it is thought to be activated through peptide binding sites (receptor). It also has analgesic activity.
Pharmacokinetics: Absorption: Pms-Gabapentin is absorbed from the gastrointestinal tract (GIT) by means of saturable mechanism. Pms-Gabapentin bioavailability is not dose proportional ie, as dose is increased, bioavailability is decreased. Absolute bioavailability of 300-mg oral dose is approximately 60%. At doses of 300 and 400 mg, Pms-Gabapentin bioavailability was unchanged following multiple dose administration. Food has no effect on the rate and extent of absorption.
Distribution: Pms-Gabapentin circulates largely unbound (<3%) to plasma proteins. It is distributed into breast milk and has a volume of distribution equal to 57.7 L.
Metabolism and Elimination: Pms-Gabapentin is not appreciably metabolized and is eliminated from the systemic circulation by renal excretion as unchanged drug. Elimination t½ ranges from 5-7 hrs and is unaltered by dose or following multiple dosing. Pms-Gabapentin elimination rate constant, plasma and renal clearance are directly proportional to creatinine clearance (CrCl).
Special Populations: Renal Insufficiency: The mean Pms-Gabapentin t½ ranged from about 6.5 hrs (patients with CrCl >60 mL/min) to 52 hrs (CrCl <30 mL/min) and Pms-Gabapentin renal clearance ranged from 90 mL/min (CrCl >60 mL/min) to about 10 mL/min (CrCl <30 mL/min). Pms-Gabapentin dosage should be adjusted in patients with compromised renal function.
Patients on Hemodialysis: In anuric patients, the elimination t½ of Pms-Gabapentin on a nondialysis day was about 132 hrs; during dialysis the apparent t½ was reduced to 3.8 hrs. Thus, hemodialysis has a significant effect on Pms-Gabapentin elimination in anuric patients. Pms-Gabapentin dosage should be adjusted in patients undergoing hemodialysis.
Elderly: The apparent oral clearance (CL/F) of Pms-Gabapentin decreased as age increased, from about 225 mL/min in those <30 years to about 125 mL/min in those >70 years. Reduction of Pms-Gabapentin dose may be required in patients who have age-related compromised renal function.
Drug-Drug Interactions: Naproxen: Co-administration of naproxen sodium (250 mg) with Pms-Gabapentin (125 mg) appears to increase the amount of Pms-Gabapentin absorbed by 12-15%. These doses are lower than the therapeutic doses for both drugs. The magnitude of interaction within the recommended dose is not known.
Hydrocodone: Co-administration of Pms-Gabapentin decreases hydrocodone Cmax and area under the curve (AUC) values in a dose-dependent manner relative to administration of hydrocodone alone. Hydrocodone increases Pms-Gabapentin AUC values by 14%.
Morphine: When morphine 60 mg is administered 2 hrs prior to Pms-Gabapentin 600 mg, the mean Pms-Gabapentin AUC increased by 44% compared to Pms-Gabapentin administered without morphine.
How should I take Pms-Gabapentin?
- Take Pms-Gabapentin exactly as prescribed. Your healthcare provider will tell you how much Pms-Gabapentin to take and when to take it. Take Pms-Gabapentin at the same time each day.
- Do not change your dose or stop taking Pms-Gabapentin without talking with your healthcare provider. If you stop taking Pms-Gabapentin suddenly, you may experience side effects. Talk with your healthcare provider about how to stop Pms-Gabapentin slowly.
- Take Pms-Gabapentin with food one time each day with your evening meal.
- Take Pms-Gabapentin tablets whole. Do not split, crush, or chew Pms-Gabapentin tablets before swallowing.
- Your healthcare provider may change your dose of Pms-Gabapentin. Do not change your dose of Pms-Gabapentin without talking to your healthcare provider.
- If you miss a dose, take it as soon as you remember with food. If it is almost time for your next dose, just skip the missed dose. Take the next dose at your regular time. Do not take two doses at the same time.
- If you take too much Pms-Gabapentin, call your healthcare provider or poison control center, or go to the nearest emergency room right away.
- If you are taking an antacid containing aluminum hydroxide and magnesium hydroxide, it is recommended that Pms-Gabapentin be taken at least 2 hours following administration of the antacid.
Pms-Gabapentin administration
Take exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.
The Horizant brand of Pms-Gabapentin should not be taken during the day. For best results, take Horizant with food at about 5:00 in the evening.
The Pms-Gabapentin brand of Pms-Gabapentin can be taken with or without food.
If you break a tablet and take one half of it, take the other half at your next dose. Any tablet that has been broken should be used as soon as possible or within a few days.
Measure liquid medicine with a special dose-measuring spoon or cup, not a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist for one.
Do not stop taking Pms-Gabapentin for seizures without first talking to your doctor, even if you feel fine. You may have increased seizures if you stop using Pms-Gabapentin suddenly. You may need to use less and less before you stop the medication completely.
Contact your doctor if your seizures get worse or you have them more often while taking Pms-Gabapentin.
Wear a medical alert tag or carry an ID card stating that you take Pms-Gabapentin. Any doctor, dentist, or emergency medical care provider who treats you should know that you take seizure medication.
Use Pms-Gabapentin regularly to get the most benefit. Get your prescription refilled before you run out of medicine completely.
This medication can cause unusual results with certain medical tests. Tell any doctor who treats you that you are using Pms-Gabapentin.
Store Pms-Gabapentin tablets and capsules at room temperature away from light and moisture.
Store the liquid medicine in the refrigerator. Do not freeze.
Pms-Gabapentin pharmacology
Mechanism Of Action
The mechanism of action by which Pms-Gabapentin exerts its analgesic action is unknown but in animal models of analgesia, Pms-Gabapentin prevents allodynia (pain-related behavior in response to a normally innocuous stimulus) and hyperalgesia (exaggerated response to painful stimuli). Pms-Gabapentin prevents pain-related responses in several models of neuropathic pain in rats and mice (e.g., spinal nerve ligation models, spinal cord injury model, acute herpes zoster infection model). Pms-Gabapentin also decreases pain-related responses after peripheral inflammation (carrageenan footpad test, late phase of formulin test), but does not alter immediate pain-related behaviors (rat tail flick test, formalin footpad acute phase). The relevance of these models to human pain is not known.
Pms-Gabapentin is structurally related to the neurotransmitter GABA (gamma-aminobutyric acid), but it does not modify GABAA or GABAB radioligand binding, it is not converted metabolically into GABA or a GABA agonist, and it is not an inhibitor of GABA uptake or degradation. In radioligand binding assays at concentrations up to 100 μM, Pms-Gabapentin did not exhibit affinity for a number of other receptor sites, including benzodiazepine, glutamate, N-methyl-D-aspartate (NMDA), quisqualate, kainate, strychnine-insensitive or strychnine-sensitive glycine; alpha 1, alpha 2, or beta adrenergic; adenosine A1 or A2; cholinergic, muscarinic, or nicotinic; dopamine D1 or D2; histamine H1; serotonin S1 or S2; opiate mu, delta, or kappa; cannabinoid 1; voltage-sensitive calcium channel sites labeled with nitrendipine or diltiazem; or at voltage-sensitive sodium channel sites labeled with batrachotoxinin A20-alpha-benzoate. Pms-Gabapentin did not alter the cellular uptake of dopamine, noradrenaline, or serotonin.
In vitro studies with radiolabeled Pms-Gabapentin have revealed a Pms-Gabapentin binding site in areas of rat brain including neocortex and hippocampus. A high-affinity binding protein in animal brain tissue has been identified as an auxiliary subunit of voltage-activated calcium channels. However, functional correlates of Pms-Gabapentin binding, if any, remain to be elucidated. It is hypothesized that Pms-Gabapentin antagonizes thrombospondin binding to α2δ-1 as a receptor involved in excitatory synapse formation and suggested that Pms-Gabapentin may function therapeutically by blocking new synapse formation.
Pharmacodynamics
No pharmacodynamic studies have been conducted with Pms-Gabapentin.
Pharmacokinetics
Absorption And Bioavailability
Pms-Gabapentin is absorbed from the proximal small bowel by a saturable L-amino transport system. Pms-Gabapentin bioavailability is not dose proportional; as the dose is increased, bioavailability decreases.
When Pms-Gabapentin (1800 mg once daily) and Pms-Gabapentin immediate release (600 mg three times a day) were administered with high fat meals (50% of calories from fat), Pms-Gabapentin has a higher Cmax and lower AUC at steady state compared to Pms-Gabapentin immediate release (Table 5). Time to reach maximum plasma concentration (Tmax) for Pms-Gabapentin is 8 hours, which is about 4-6 hours longer compared to Pms-Gabapentin immediate release.
Table 5: Mean (SD) Steady-State Pharmacokinetics for Pms-Gabapentin and Pms-Gabapentin Immediate Release in Plasma of Healthy Subjects (Day 5, n = 21)
References
- DailyMed. "GABAPENTIN: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
- NCIt. "Gabapentin: 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. "Gabapentin: 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 Pms-Gabapentin 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 Pms-Gabapentin. 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
