Gabapentin Vaginal Cream

Overview of Gabapentin Vaginal Cream

Dosage Strengths of Gabapentin Vaginal Cream

6% 30 mL Pump

General Information

Containing GABA agonist activity, gabapentin is an analog of the neurotransmitter gamma-aminobutyric acid (GABA). It is particularly helpful in some patients because of its distinctive pharmacokinetic characteristics. High lipid solubility, lack of hepatic metabolism, lack of protein binding, and lack of medication interactions due to enzyme stimulation are all characteristics of gabapentin. Gabapentin, a drug that was first created as an anticonvulsant, has been proven to be useful as an adjunct therapy for the management of partial seizures with or without subsequent generalized tonic-clonic seizures. Additionally, effectiveness in the management of painful neuropathies has been shown. Monotherapy for refractory partial seizure disorders, multiple sclerosis spasticity treatment, and tremor are some of the investigational uses. Additionally, gabapentin appears to be successful in lowering hot flashes in menopausal or breast cancer-afflicted women.1

Topical gabapentin in the treatment of localized and generalized vulvodynia 2

Participants: 150 patients presenting with entry dyspareunia 

Administration: Topical (local) 

Dosage: 2% Cream 

Conclusion: 80% of respondents demonstrated at least a 50% improvement in pain scores. Topical gabapentin seems to be well-tolerated and associated with significant pain relief in women with vulvodynia. 

Contraindications/Precautions

All patients receiving gabapentin or starting antiepileptic drug (AED) therapy should be thoroughly watched for any signs of developing or worsening depression or suicidal thoughts. Instruct patients and caregivers to report any new or worsening depression, suicide thoughts or behavior, self-harming thoughts, or other unexpected changes in mood or behavior very away. Also, inform them of the elevated risk of suicidal thoughts and behaviors. In order to lower the danger of overdose, AEDs should only be provided in the smallest dose that is consistent with good patient management. Epilepsy and numerous other conditions for which AEDs are administered are linked to a higher risk of suicidal ideas and actions. Consider whether the onset of these symptoms in any patient may be related to the condition being treated if suicidal thoughts or conduct appear during therapy. Patients taking AEDs for the treatment of epilepsy, psychiatric illnesses, or other ailments have a higher risk of developing suicidal ideation and conduct (e.g., migraine, neuropathic pain). It is known that the kidneys eliminate gabapentin in large amounts. Patients receiving hemodialysis or other forms of dialysis who have renal impairment or renal failure should adjust their gabapentin dosage. 345 

Pregnancy

There are no adequate and well-controlled studies of gabapentin in pregnant women. Data from cohort studies describing the neonatal risks of gabapentin treatment during pregnancy are inconclusive. Gabapentin actively crosses the placenta. Among 6 neonates born to mothers who were taking gabapentin (doses ranging from 900 to 3,200 mg/day), umbilical cord-to-maternal plasma concentration ratios ranged from 1.3 to 2.11 (mean, 1.74) at delivery. Gabapentin concentrations in the neonates declined to an average of 27% (range, 12% to 36%) of cord blood concentrations at 24 hours postpartum. One infant was born premature at 33 weeks; however, all deliveries were uneventful and all neonates were born in healthy condition.6 In a prospective cohort study, rates of major malformations among neonates were similar between 223 pregnancies with gabapentin exposure and 223 unexposed pregnancies (4.1% exposed vs. 2.5% unexposed, p = 0.555). Major malformations included 2 ventricular septal defects, anencephaly, macrocephaly, microretrognathism, cutis marmorata, pyloric stenosis, bilateral varus clubfoot, and cryptorchidism. In all cases of major malformations, women received concomitant treatment with other medications during pregnancy; therefore, a causal relationship to gabapentin cannot be established. No major malformations occurred in neonates born to women exposed to gabapentin monotherapy during pregnancy (n = 36). There were higher rates of preterm births (10.5% vs. 3.9%, p = 0.019), low birth weight (less than 2,500 g) (10.5% vs. 4.4%, p = 0.033), and admission to neonatal intensive care or special care nursery (38% vs. 2.9%, p less than 0.001) among neonates with gabapentin exposure compared to unexposed neonates. Two cases of possible poor neonatal adaptation syndrome occurred in neonates with gabapentin exposure late in pregnancy compared to no cases among unexposed infants; these 2 neonates were also exposed to other psychotropic medications.7 In a cohort of 39 women who were exposed to gabapentin during their first trimester (97%) and throughout gestation (81.8%), malformations occurred in 3 of 44 live births. Hypospadia was reported in a neonate exposed to gabapentin and valproate; a missing kidney occurred in a neonate exposed to gabapentin and phenobarbital, and a minor malformation of the left external ear canal and 2 small skin tags at the jaw occurred in a neonate exposed to gabapentin and lamotrigine. Since exposure to multiple antiepileptic drugs occurred during these pregnancies, a causal relationship to gabapentin cannot be established. No malformations occurred in 11 patients exposed to gabapentin monotherapy during pregnancy.8 In animal studies, gabapentin has been fetotoxic during organogenesis at doses of 1 to 4 times the maximum recommended human dose on a mg/m2 basis. Delayed ossification of bones in the skull, limbs, and vertebrae were reported when pregnant mice received oral gabapentin (500, 1,000, or 3,000 mg/kg/day) during organogenesis. The no-effect dose for toxicity (500 mg/kg/day) is less than the maximum human recommended dose (MRHD) of 3,600 mg/kg on a body surface area (mg/m2) basis. Increased incidences of hydroureter and/or hydronephrosis were observed at all doses tested in studies in which rats received oral gabapentin (500 to 2,000 mg/kg/day). An increased incidence of fetal loss was also noted at all doses tested when pregnant rabbits were treated with oral gabapentin (60, 300, or 1,500 mg/kg) during organogenesis. Physicians are advised to recommend that pregnant patients receiving gabapentin enroll in the North American Antiepileptic Drug (NAAED) Pregnancy Registry to provide information about the effects of in utero exposure to the drug. Patients must call 1-888-233-2334 to enroll in the registry.3 

Breastfeeding

Gabapentin is excreted in human breastmilk. A breast-feeding infant could be exposed to a maximum gabapentin dose of approximately 1 mg/kg/day. The effects of gabapentin on the breast-fed infant and milk production are unknown. 34 Because of the potential for adverse reactions in breast-feeding infants, discontinue breast-feeding or gabapentin enacarbil, taking into account the importance of the drug to the mother. 5 For other gabapentin products, consider the developmental and health benefits of breast-feeding along with the mother's clinical need for gabapentin and any potential adverse effects on the breast-fed infant from gabapentin or the underlying maternal condition. Only use gabapentin in breast-feeding women if the benefits clearly outweigh the risks. 34 The infant dose of gabapentin excreted in breast milk was examined in 4 infants, 3 of which were 2 to 3 weeks of age and 1 who was approximately 3 months old. The average daily maternal dosage of gabapentin was 1,575 mg (range, 600 to 2,100 mg/day). A single milk sample was obtained approximately 10 to 15 hours after the last dose. Assuming a breast milk consumption of 150 mL/kg/day, the relative infant dose of gabapentin was estimated to be 0.2 to 1.3 mg/kg/day, which approximates 1.3% to 3.8% of the weight-adjusted maternal dose. At 2 to 3 weeks after delivery, 2 infants had detectable gabapentin plasma concentrations that were under the normal range of quantification, and 1 had an undetectable concentration. At 3 months, the gabapentin plasma concentration in another infant was under the normal range of quantification. No adverse effects were reported. 9 

Adverse Reactions/Side Effects

Gabapentin Vaginal Cream may relieve symptoms associated with vulvodynia and Provoked Vestibulodynia.

This cream is formulated to act locally so side effects are generally minimal, but may include skin irritation, headache, dizziness, and somnolence. However, possible side effects include but are not limited to those of each of the cream’s components. The side effects of these compounds in combination have not been studied.

Call your health care provider immediately if you are experiencing any signs of an allergic reaction: skin rash, itching or hives, swelling of the face, lips, or tongue, blue tint to skin, chest tightness, pain, difficulty breathing, wheezing, dizziness, red, swollen painful area on the leg.

Storage

Store this medication in its original container at 68°F to 77°F (20°C to 25°C) and away from heat, moisture and light. Keep all medicine out of the reach of children. Throw away any unused medicine after the beyond-use date. Do not flush unused medications or pour down a sink or drain.

  • 1. Nelson HD, Vesco KK, Haney E, et al. Nonhormonal therapies for menopausal hot flashes: systematic review and meta-analyses. JAMA 2006;295:2057-71.
  • 2. Boardman LA, Cooper AS, Blais LR, Raker CA. Topical gabapentin in the treatment of localized and generalized vulvodynia. Obstet Gynecol. 2008 Sep;112(3):579-85.
  • 3. a. b. c. d. Neurontin (gabapentin) package insert. New York, NY: Pfizer; 2017 Oct.
  • 4. a. b. c. Gralise (gabapentin) extended-release tablets. Menlo Park, CA: Depomed Inc; 2012 Apr.
  • 5. a. b. Horizant (gabapentin enacarbil) extended-release tablets. Research Triangle Park, NC: GlaxoSmithKline; 2013 May.
  • 6. Ohman I, Vitols S, Tomson T. Pharmacokinetics of gabapentin during delivery, in the neonatal period, and lactation: does a fetal accumulation occur during pregnancy? Epilepsia 2005;46:1621-1624.
  • 7. Fujii H, Goel A, Bernard N, et al. Pregnancy outcomes following gabapentin use: results of a prospective comparative cohort study. Neurology 2013;80:1565-1570.
  • 8. Montouris G. Gabapentin exposure in human pregnancy: results from the Gabapentin Pregnancy Registry. Epilepsy Behav 2003;4:310-317.
  • 9. Ohman I, Vitols S, Tomson T. Pharmacokinetics of gabapentin during delivery, in the neonatal period, and lactation: does a fetal accumulation occur during pregnancy? Epilepsia 2005;46:1621-1624..

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