Actions of Pendine in details
Pharmacology: Mechanism of Action: Pendine 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: Pendine is absorbed from the gastrointestinal tract (GIT) by means of saturable mechanism. Pendine 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, Pendine bioavailability was unchanged following multiple dose administration. Food has no effect on the rate and extent of absorption.
Distribution: Pendine 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: Pendine 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. Pendine elimination rate constant, plasma and renal clearance are directly proportional to creatinine clearance (CrCl).
Special Populations: Renal Insufficiency: The mean Pendine t½ ranged from about 6.5 hrs (patients with CrCl >60 mL/min) to 52 hrs (CrCl <30 mL/min) and Pendine renal clearance ranged from 90 mL/min (CrCl >60 mL/min) to about 10 mL/min (CrCl <30 mL/min). Pendine dosage should be adjusted in patients with compromised renal function.
Patients on Hemodialysis: In anuric patients, the elimination t½ of Pendine 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 Pendine elimination in anuric patients. Pendine dosage should be adjusted in patients undergoing hemodialysis.
Elderly: The apparent oral clearance (CL/F) of Pendine decreased as age increased, from about 225 mL/min in those <30 years to about 125 mL/min in those >70 years. Reduction of Pendine 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 Pendine (125 mg) appears to increase the amount of Pendine 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 Pendine decreases hydrocodone Cmax and area under the curve (AUC) values in a dose-dependent manner relative to administration of hydrocodone alone. Hydrocodone increases Pendine AUC values by 14%.
Morphine: When morphine 60 mg is administered 2 hrs prior to Pendine 600 mg, the mean Pendine AUC increased by 44% compared to Pendine administered without morphine.
How should I take Pendine?
- Take Pendine exactly as prescribed. Your healthcare provider will tell you how much Pendine to take and when to take it. Take Pendine at the same time each day.
- Do not change your dose or stop taking Pendine without talking with your healthcare provider. If you stop taking Pendine suddenly, you may experience side effects. Talk with your healthcare provider about how to stop Pendine slowly.
- Take Pendine with food one time each day with your evening meal.
- Take Pendine tablets whole. Do not split, crush, or chew Pendine tablets before swallowing.
- Your healthcare provider may change your dose of Pendine. Do not change your dose of Pendine 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 Pendine, 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 Pendine be taken at least 2 hours following administration of the antacid.
Pendine 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 Pendine should not be taken during the day. For best results, take Horizant with food at about 5:00 in the evening.
The Pendine brand of Pendine 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 Pendine for seizures without first talking to your doctor, even if you feel fine. You may have increased seizures if you stop using Pendine 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 Pendine.
Wear a medical alert tag or carry an ID card stating that you take Pendine. Any doctor, dentist, or emergency medical care provider who treats you should know that you take seizure medication.
Use Pendine 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 Pendine.
Store Pendine tablets and capsules at room temperature away from light and moisture.
Store the liquid medicine in the refrigerator. Do not freeze.
Pendine pharmacology
Mechanism Of Action
The mechanism of action by which Pendine exerts its analgesic action is unknown but in animal models of analgesia, Pendine prevents allodynia (pain-related behavior in response to a normally innocuous stimulus) and hyperalgesia (exaggerated response to painful stimuli). Pendine 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). Pendine 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.
Pendine 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, Pendine 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. Pendine did not alter the cellular uptake of dopamine, noradrenaline, or serotonin.
In vitro studies with radiolabeled Pendine have revealed a Pendine 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 Pendine binding, if any, remain to be elucidated. It is hypothesized that Pendine antagonizes thrombospondin binding to α2δ-1 as a receptor involved in excitatory synapse formation and suggested that Pendine may function therapeutically by blocking new synapse formation.
Pharmacodynamics
No pharmacodynamic studies have been conducted with Pendine.
Pharmacokinetics
Absorption And Bioavailability
Pendine is absorbed from the proximal small bowel by a saturable L-amino transport system. Pendine bioavailability is not dose proportional; as the dose is increased, bioavailability decreases.
When Pendine (1800 mg once daily) and Pendine immediate release (600 mg three times a day) were administered with high fat meals (50% of calories from fat), Pendine has a higher Cmax and lower AUC at steady state compared to Pendine immediate release (Table 5). Time to reach maximum plasma concentration (Tmax) for Pendine is 8 hours, which is about 4-6 hours longer compared to Pendine immediate release.
Table 5: Mean (SD) Steady-State Pharmacokinetics for Pendine and Pendine 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 Pendine 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 Pendine. 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
3 consumers reported administration
When best can I take Pendine, on an empty stomach, before or after food?ndrugs.com website users have also released a report stating that Pendine should be taken After food. In any case, this may not be the right description on how you ought to take this Pendine. Kindly visit your doctor for more medical advice in this regard. Click here to see other users view on when best the Pendine can be taken.
| Users | % | ||
|---|---|---|---|
| After food | 1 | 33.3% | |
| Empty stomach | 1 | 33.3% | |
| Before food | 1 | 33.3% | |
Consumer reviews
| IMy friend have hives itchyness and rash on legs after Starting this medication |
Information checked by Dr. Sachin Kumar, MD Pharmacology
