Gabapentin

Aim: To find out whether preoperative gabapentin use had a favorable effect on long term postoperative pain in patients undergoing inguinal herniorraphy.
Methods: Sixty male subjects -aged between 20-40 years- who were scheduled for unilateral inguinal hernioraphy under spinal anesthesia were included in this prospective, randomized, double-blind study. The patients were randomly allocated into two groups: gabapentin group (n=30) received single dose 1.2 g p.o. gabapentin one hour before surgery and placebo group received a placebo capsule instead. Spinal anesthesia was performed with heavy bupivacaine and all operations were
performed by the same surgeon with the same technique. Postoperative analgesia was evaluated during sitting and lying with visual analogue scale. Assessment of postoperative pain on the 1st, 3rd, and 6th months was carried out with an 11-point numerical rating scale (NRS); 0 indicating 'no pain' and 10 indicating 'worst pain imaginable'. Patients who had NRS scores greater than 0 were further evaluated also with regard to the impact of pain on their daily activities.
Results: When compared with placebo group, gabapentin group displayed significantly lower VAS scores (lying and sitting) and total tramadol consumption on the postoperative 8th, 12th,  16th, 20th and 24th hours (p<0.05) and higher postoperative patient satisfaction scores (p<0.05). NRS scores on the postoperative 1st, 3rd and 6th months were lower in group 1 than in group 2 (p<0.05). The number of patients whose daily activities were adversely affected by pain was smaller in  gabapentin group on the first month; however the two groups were found to be similar on the 3rd and 6th months.
Conclusion: We imply that preoperative single dose gabapentin decreases the intensity of acute postoperative pain, tramadol consumption, the incidence and intensity of pain in the  postoperative six months of inguinal herniorraphy.

A facile preparation of 2-aminomethyl-2-tricyclo[3.3.1.1(1,7)]decaneacetic acid hydrochloride 5 (AdGABA) is described. The synthesis of AdGABA involves the hydrogenation of 2-cyano-2-tricyclo[3.3.1.1(1,7)]decaneacetic acid 11, which was synthesized by two different synthetic routes. AdGABA was found to antagonize the pentylenetetrazole (PTZ) and semicarbazide (SCZ) induced tonic convulsions and exhibits analgesic activity in the hot plate test on mice. Although its mechanism of action is quite similar to that proposed previously for gabapentin (interaction with the alpha2delta subunit of the voltage gated Ca2+ channels), further studies were undertaken in order to clarify the precise mechanism of the anticonvulsant and analgesic effects of AdGABA on a molecular level.

Introduction: Inhibiting the pain which affects both the patients and dentists is an important factor during treating dental patients. The aim of this study was to assess the analgesic effect of two medications ibuprofen and gabapentin on the post-endodontic-therapy pain.

Methods: Forty patients who need root canal therapy with Visual Analog Scale (VAS)>40, participated in this double-blind randomized clinical trial study and randomly divided into two groups. The ibuprofen group received 800 mg ibuprofen 1 hour before the treatment and 400 mg at 6, 12 and 24 hours after the treatment procedure, and the other group received 600 mg gabapentin 1 hour before the treatment and 300 mg at 6, 12 and 24 hours after treatment. Patients recorded the intensity of pain via VAS before treatment and every hour for the first 6 h after taking the medication and then every 6 h thereafter for a total of the 48-hour period. (Two tablets of acetaminophen codeine (325mg/20mg) were given to the patients as a rescue dose.

Results: The analgesic effect of gabapentin was significantly higher than ibuprofen in 12h (p=0.035), 24h (p<0.001), and 48 h (p=0.012) after analgesic intake. It has been also shown that both medicines had analgesic effect significantly. (p<0.0001)

Conclusions: Gabapentin had greater analgesic effects on the sample group from 12 h until 48h after taking in comparison with ibuprofen so it seems that it could be an appropriate option for postoperative pain inhibition.

Background: It is well known that pain is subjective symptom and postoperative pain continues prevalence worldwide, because despite all the progress has not yet been able to eradicate completely. Objective: To evaluate the adjuvant effect on postoperative pain intensity 600 mg of gabapentin administered preoperatively in patients undergoing abdominal hysterectomy at St. Thomas Hospital from April to August 2014. Methods: An experimental study cohort prospective randomized, controlled, double blind study in patients undergoing abdominal hysterectomy was performed under general anesthesia. Were randomized into two groups: gabapentin group-gabapentin 600 mg (2 hours preoperative) + analgesia morphine through pump patient controlled analgesia (PCA)-and control group-analgesia with morphine via PCA pump; morphine dose was calculated based on weight ranges to 0.016 mg/kg/h. Pain intensity scale with verbal numeric scale (VNS) of 11 points at 2, 6 and 24 hours were evaluated, the number of rescues administered postoperatively was quantified and the prevalence of adverse events in both groups was measured. Results: Seventy-two patients splitted into two homogeneous groups were recruited, the average age was 44.72 ± 6.17 years in gabapentin group and 49.36 ± 9.31 years in control group. As for postoperative pain was statistically significant difference between the two groups (p < 0.05), a difference was found in the VNS of 11 points, 4.27 ± 2.32, 1.94 ± 1.95 and 0.77 ± 1.28 in gabapentin group and 7.13 ± 2.41, 4.5 ± 2.37 y 3.25 ± 2.18 in control group at 2, 6 and 24 hours respectively; the amount of ransom administered by PCA pump during the first 24 postoperative hours was measured was 6.72 ± 5.7 for gabapentin group and 24.13 ± 47.01 for control group, a statistically significant difference (p < 0.05); the prevalence of adverse effects was not statistically significant between groups. Conclusion: These results indicate that gabapentin at doses of 600 mg preoperative is a valid therapeutic option in preoperative analgesia for abdominal hysterectomy. Note that we have yet to elucidate the optimal effective dose and to present lower incidence of adverse effects.

The purpose of this study was to compare the therapeutic effects of gabapentin (GBP) and different doses of rapamycin (RAPA) in an induced sciatic nerve (SN)-injury rat model. Materials and Methods: The study consisted of 7 groups: Control, Sham, High-dose rapamycin (RAPA-H), Low-dose rapamycin (RAPA-L), GBP, DMSO and DMSO+nerve injury (DMSO+NI). Medical treatment was administered intraperitoneally for 30 days after the induction of SN injury. Results: Significant differences (p<0.001 for all) were found in comparisons between the groups in terms of axon diameter, axon number, and neurofilament (NF) and S100 immunointensity. Among the treatment groups, the highest mean axon diameter value, close to that of the Control group, was seen in the RAPA-L group. In terms of axon number, the value closest to that of the Control group was measured in the GBP group. The NF and S100 immunodensity in the RAPA-L group was similar to that of the GBP group. The S100 immunodensity in the RAPA-L group was closest to that of the Control group. The highest conduction velocity and distal latency values were recorded in the RAPA-L group. Conclusion: The histological and electrophysiological findings observed in this study suggest that RAPA-L treatment is a promising alternative to GBP.

The closure related to the COVID-19 pandemic impacted on the management of separation-related disorder in a dog. Eight weeks before the first COVID-19 pandemic closure, the patient, an 8-year-old female neutered cross breed dog weighing 6 kg, was presented for nonstop barking when separated from her owners, 8 hours a day, 5 days each week. Before the first consultation, 4 years of training based on desensitization without medication helped the patient but never lowered the barking beyond two hours a day, which remains way too high to provide a correct quality of life to this dog. The patient welfare was at stake, and the neighborhood complains were growing. The patient was prescribed fluoxetine at 20 mg (3.3 mg/kg) PO q24 h. and trazodone PRN before separation at 25 mg (4.2 mg/kg) PO. A behavioral modification plan based on extinction and calm reinforcement was prescribed. Eight weeks after the treatment onset, just before the first COVID-19 pandemic closure, the dog improved significantly, lowered daily barking up to 15 minutes. During all the successive closures (i.e., one year), the dog was never left alone. When the closures ended, the barking relapsed, straight at the first separation event, reaching 1 to 2 hours daily, even though the fluoxetine had never been interrupted. Therefore, gabapentin was pre- scribed PRN before separation at 100 mg (16.6 mg/kg) in place of trazodone that triggered excitation in the patient when it was previously tried. The behavioral plan was completed with additional conditioning learning before sep- aration. The dog improved quickly to a short tolerable time of barking (i.e., 5 to 10 minutes). This outcome remains stable by the time the paper is written i.e., 3 months after the end of the closure. The patient’s evolution emphasizes two important topics in the treatment of separation-related disorder: firstly, medication is needed for most cases to lower the level of emotional reaction, and secondly, interruption in the exposition to the fearful context may have rebound effects when the context will be encountered again. The long-term effects of the COVID-19 pandemic remains unknown on both human and dog’s welfare. More extensive studies should be conducted to measure its impact on separation-related disorder in dogs.

The suppression of neurovegetative response to laryngoscopy and intubation has been tried out using several pharmacological agents, such as opioids, local anaesthetics, β-blockers and α2 agonists. Gabapentin an anticonvulsant, while esmolol is a cardioselective β1 blocker and a class II antiarrhythmic, they have shown to attenuate pressor response to direct laryngoscopy and tracheal intubation individually. Given these variable characteristics of two drugs, the present study, a prospective randomized double blind aimed to compare their efficacy against haemodynamic response during intubation and laryngoscopy.

The combination of opioids and central nervous system depressants such as benzodiazepines and barbiturates has an additive effect on the frequency of oversedation and respiratory depression requiring naloxone use in hospitalized patients. Gabapentinoids (gabapentin and pregabalin) are frequently prescribed with opioids for their opioid-sparing and adjuvant analgesic effects. There is limited literature on the risk of respiratory depression due to the combination of opioids and gabapentinoids requiring naloxone administration. This retrospective study evaluated patients who were prescribed opioids and at least one dose of naloxone between March 1, 2014 and September 30, 2016. The primary objective of this study was to compare the frequency of respiratory depression among patients who received naloxone and opioids (non-gabapentinoid group) with those who received naloxone, opioids, and gabapentinoids (gabapentinoid group). Secondary objectives included comparing the association of ove...

Background and Objective: Pain after tonsillectomy is one of the most common complications. This study was done to compare the effect of Gabapentin and promethazine as premedication to reduce pain after tonsillectomy.
Methods: This clinical trial study was performed on 104 patients aged 7-15 years who were candidate for tonsillectomy. Patients were randomly divided into gabapentin and promethazine groups. The first group received oral gabapentin 20 mg/kg/bw, and the second group was treated with promethazine syrup 0.5 mg/kg/bw one hour before anesthesia. Pain score was recorded based on the MOPS index and recorded and compared during 3, 6, 12, and 24 hours after surgery.
Results: The mean±SD of pain severity in the intervention group with promethazine at 3, 6, 12 and 24 hours after surgery were 1.35±0.84, 0.9±0.87, 0.25±0.52, 0.04±0.19, respectively. Pain severity was 1.58±0.98, 1.13±0.91, 0.69±0.27, and 0.06±0.24 in gabapentin group, respectively. There was no significant difference between pain score of two groups in 3, 6, 12 and 24 hours after surgery.
Conclusion: Gabapentin and promethazine as premedication have a similar analgesic effect in patients after tonsillectomy.
Keywords: Tonsillectomy [MeSH], Gabapentin [MeSH], Promethazine [MeSH], Pain [MeSH],

In the present study, gabapentin (GBP), an anticonvulsant drug used as an analgesic to control the neuropathic pains, was incorporated with cellulose acetate (CA) and gelatin (Gel) in order to develop a potential scaffold for neural tissue engineering applications. The wet-electrospinning method was used to produce the drug-loaded three-dimensional scaffolds from CA/Gel [1:1 (w/w)] solution in the water/ethanol (3:7) (v/v) coagulation baths containing 3%, 6% and 12% (w/v) of GBP. The scaffolds were evaluated regarding their morphology, contact angle, porosity, tensile strength and cellular response. The scaffold obtained from 6% (w/v) GBP bath was chosen as the optimum scaffold for further in vivo study in a sciatic nerve defect model in Wistar rats. The results of sciatic functional index, hot plate latency, weight-loss percentage of the wet gastrocnemius muscle and the histopathological examination using hematoxylin-eosin staining demonstrated that the GBP-containing scaffold significantly enhanced the regeneration of the created injury, which demonstrates its applicability for neural tissue engineering applications.

Gabapentin has shown to be effective in animals and humans with acute postoperative and chronic pain. Yet the mechanisms by which gabapentin reduces pain have not been fully addressed. The current study performed in vivo microdialysis in the locus coeruleus (LC) in normal and spinal nerve ligated (SNL) rats to examine the effect of gabapentin on extracellular glutamate concentration and its mechanisms of action with focus on presynaptic GABA-B receptors, astroglial glutamate transporter-1 (GLT-1), and interactions with α2δ subunits of voltage-gated Ca 2+ channels and endogenous noradrenaline. Basal extracellular concentration and tissue content of glutamate in the LC were greater in SNL rats than normal ones. Intravenously administered and LC-perfused gabapentin increased extracellular glutamate concentration in the LC. The net amount of glutamate increased by gabapentin is larger in SNL rats compared with normal ones, although the percentage increases from the baseline did not differ. The gabapentin-related α2δ ligand pregabalin increased extracellular glutamate concentration in the LC, whereas another α2δ ligand, 3-exo-aminobicyclo [2.2.1] heptane-2-exo-carboxylic acid (ABHCA), did not. Selective blockade by the dihydrokainic acid or knock-down of GLT-1 by the small interfering RNA abolished the gabapentin-induced glutamate increase in the LC, whereas blockade of GABA-B receptors by the CGP-35348 and depletion of noradrenalin by the dopamine-β-hydroxylase antibody conjugated to saporin did not. These results suggest that gabapentin induces glutamate release from astrocytes in the LC via GLT-1-dependent mechanisms to stimulate descending inhibition. The present study also demonstrates that this target of gabapentin in astrocytes does not require interaction with α2δ subunits in neurons.