Gabapentin 300mg Capsules SMPC - Taj Pharmaceuticals

Gabapentin 300mg capsules SMPC, Taj Pharmaceuticals
Gabapentin Taj Phar ma : Uses, Side Effects, Interactions, Pictures, Warnings, Gabapentin Dosage & Rx Info | Gabapentin Uses, Side Effects -: Indications, Side Effects, Warnings, Gabapentin - Drug Information - Taj Phar ma, Gabapentin dose Taj pharmaceuticals Gabapentin interactions, Taj Phar maceutical Gabapentin contraindications, Gabapentin price, Gabapentin Taj Pharma Gabapentin 300mg capsules SMPC- Taj Phar ma . Stay connected to all updated on Gabapentin Taj Pharmaceuticals Taj phar maceuticals Hyderabad.
which is recommended for adults and

RX adolescents aged 12 years and above. Dosing
instructions for children under 12 years of age
GABAPENTIN are provided under a separate sub-heading later
in this section.
CAPSULES
300MG Table 1
DOSING CHART – INITIAL TITRATION
1.NAME OF THE MEDICINAL PRODUCT
Day 1 Day 2 Day 3
Gabapentin 300mg capsules 300mg once a 300mg two times 300mg three
2. QUALITATIVE AND QUANTITATIVE day a day times a day
COMPOSITION Discontinuation of gabapentin
Each capsule contains 300mg of gabapentin In accordance with current clinical practice, if
gabapentin has to be discontinued it is
Excipients with known effect:
recommended this should be done gradually
Each 300 mg hard capsule contains 50.5mg over a minimum of 1 week independent of the
lactose (as monohydrate). indication.
For the full list of excipients, see section 6.1. Epilepsy
3. PHARMACEUTICAL FORM Epilepsy typically requires long-term therapy.
Dosage is determined by the treating physician
Capsules,hard according to individual tolerance and efficacy.
Size 1, yellow-yellow, hard gelatin capsules Adults and adolescents:
4. CLINICAL PARTICULARS In clinical trials, the effective dosing range was
4.1 Therapeutic indications 900 to 3600mg/day. Therapy may be initiated by
Epilepsy titrating the dose as described in Table 1 or by
administering 300mg three times a day (TID) on
Gabapentin is indicated as adjunctive therapy in Day 1. Thereafter, based on individual patient
the treatment of partial seizures with and without response and tolerability, the dose can be further
secondary generalisation in adults and children increased in 300mg/day increments every 2-3
aged 6 years and above (see section 5.1). days up to a maximum dose of 3600mg/day.
Gabapentin is indicated as monotherapy in the Slower titration of gabapentin dosage may be
treatment of partial seizures with and without appropriate for individual patients. The
secondary generalisation in adults and minimum time to reach a dose of 1800mg/day is
adolescents aged 12 years and above. one week, to reach 2400mg/day is a total of 2
weeks, and to reach 3600mg/day is a total of 3
Treatment of peripheral neuropathic pain weeks.
Gabapentin is indicated for the treatment of Dosages up to 4800mg/day have been well
peripheral neuropathic pain such as painful tolerated in long-term open-label clinical
diabetic neuropathy and post-herpetic neuralgia studies. The total daily dose should be divided in
in adults. three single doses, the maximum time interval
between the doses should not exceed 12 hours to
4.2 Posology and method of administration
prevent breakthrough convulsions.
Posology
Children aged 6 years and above:
For all indications a titration scheme for the
initiation of therapy is described in Table 1,
The starting dose should range from 10 to using smaller dosage strengths or longer
15mg/kg/day and the effective dose is reached intervals between dosage increases.
by upward titration over a period of
Elderly (over 65 years of age)
approximately three days. The effective dose of
gabapentin in children aged 6 years and older is Elderly patients may require dosage adjustment
25 to 35mg/kg/day. Dosages up to 50mg/kg/day because of declining renal function with age (see
have been well tolerated in a long term clinical Table 2). Somnolence, peripheral oedema and
study. The total daily dose should be divided in asthenia may be more frequent in elderly
three single doses, the maximum time interval patients.
between doses should not exceed 12 hours.
Renal impairment
It is not necessary to monitor gabapentin plasma
concentrations to optimize gabapentin therapy. Dosage adjustment is recommended in patients
Further, gabapentin may be used in combination with compromised renal function as described in
with other antiepileptic medicinal products Table 2 and/or those undergoing haemodialysis.
without concern for alteration of the plasma Gabapentin capsules can be used to follow
concentrations of gabapentin or serum dosing recommendations for patients with renal
concentrations of other antiepileptic medicinal insufficiency.
products.
Table 2
Peripheral neuropathic pain DOSAGE OF GABAPENTIN IN ADULTS BASED ON RENAL
Adults Creatinine Clearance (ml/min) Total D
The therapy may be initiated by titrating the ≥80 900-36
dose as described in Table 1. Alternatively, the 50-79 600-18
starting dose is 900mg/day given as three 30-49 300-90
equally divided doses. Thereafter, based on
15-29 150b -6
individual patient response and tolerability, the
dose can be further increased in 300mg/day <15c 150b -3
increments every 2-3 days up to a maximum a Total daily dose should be administered as
dose of 3600mg/day. Slower titration of three divided doses. Reduced dosages are for
gabapentin dosage may be appropriate for patients with renal impairment (creatinine
individual patients. The minimum time to reach clearance < 79ml/min).
a dose of 1800mg/day is one week, to reach
2400mg/day is a total of 2 weeks, and to reach b The 150mg daily dose to be administered as
3600mg/day is a total of 3 weeks. 300mg every other day.
In the treatment of peripheral neuropathic pain c For patients with creatinine clearance
such as painful diabetic neuropathy and post- <15ml/min, the daily dose should be reduced in
herpetic neuralgia, efficacy and safety have not proportion to creatinine clearance (e.g., patients
with a creatinine clearance of 7.5ml/min should
been examined in clinical studies for treatment
periods longer than 5 months. If a patient receive one-half the daily dose that patients with
a creatinine clearance of 15ml/min receive).
requires dosing longer than 5 months for the
treatment of peripheral neuropathic pain, the Use in patients undergoing haemodialysis
treating physician should assess the patient's
clinical status and determine the need for For anuric patients undergoing haemodialysis
additional therapy. who have never received gabapentin, a loading
dose of 300 to 400mg, then 200 to 300mg of
Instruction for all areas of indication gabapentin following each 4 hours of
In patients with poor general health, i.e., low haemodialysis, is recommended. On dialysis-
body weight, after organ transplantation etc., the free days, there should be no treatment with
gabapentin.
dose should be titrated more slowly, either by
For renally impaired patients undergoing Suicidal ideation and behaviour have been
haemodialysis, the maintenance dose of reported in patients treated with anti-epileptic
gabapentin should be based on the dosing agents in several indications. A meta-analysis of
recommendations found in Table 2. In addition randomised placebo controlled trials of anti-
to the maintenance dose, an additional 200 to epileptic drugs has also shown a small increased
300mg dose following each 4-hour risk of suicidal ideation and behaviour. The
haemodialysis treatment is recommended. mechanism of this risk is not known and the
available data do not exclude the possibility of
Method of administration an increased risk for Gabapentin.
For oral use.
Therefore patients should be monitored for signs
Gabapentin can be given with or without food of suicidal ideation and behaviours and
and should be swallowed whole with sufficient appropriate treatment should be considered.
fluid intake (e.g. a glass of water). Patients (and caregivers of patients) should be
advised to seek medical advice should signs of
4.3 Contraindications suicidal ideation or behaviour emerge.
Hypersensitivity to the active substance or to
any of the excipients listed in section 6.1. Acute pancreatitis
4.4 Special Warnings and precautions for use If a patient develops acute pancreatitis under
treatment with gabapentin, discontinuation of
Drug Rash with Eosinophilia and Systemic gabapentin should be considered (see section
Symptoms (DRESS) 4.8).
Severe, life-threatening, systemic Seizures
hypersensitivity reactions such as Drug rash
with eosinophilia and systemic symptoms Although there is no evidence of rebound
(DRESS) have been reported in patients taking seizures with gabapentin, abrupt withdrawal of
antiepileptic drugs including gabapentin (see anticonvulsants in epileptic patients may
section 4.8). precipitate status epilepticus (see section 4.2).
It is important to note that early manifestations As with other antiepileptic medicinal products,
of hypersensitivity, such as fever or some patients may experience an increase in
lymphadenopathy, may be present even though seizure frequency or the onset of new types of
rash is not evident. If such signs or symptoms seizures with gabapentin.
are present, the patient should be evaluated
As with other anti-epileptics, attempts to
immediately. Gabapentin should be discontinued
withdraw concomitant anti-epileptics in
if an alternative etiology for the signs or treatment refractory patients on more than one
symptoms cannot be established.
anti-epileptic, in order to reach gabapentin
Anaphylaxis monotherapy have a low success rate.
Gabapentin can cause anaphylaxis. Signs and Gabapentin is not considered effective against
symptoms in reported cases have included primary generalized seizures such as absences
difficulty breathing, swelling of the lips, throat, and may aggravate these seizures in some
and tongue, and hypotension requiring patients. Therefore, gabapentin should be used
emergency treatment. Patients should be with caution in patients with mixed seizures
instructed to discontinue gabapentin and seek including absences.
immediate medical care should they experience Gabapentin treatment has been associated with
signs or symptoms of anaphylaxis (see section dizziness and somnolence, which could increase
4.8). the occurrence of accidental injury (fall). There
Suicidal ideation and behaviour have also been post-marketing reports of loss of
consciousness, confusion and mental
impairment. Therefore, patients should be
advised to exercise caution until they are gabapentin abuse e.g. drug-seeking behaviour,
familiar with the potential effects of the dose escalation, development of tolerance.
medicinal product.
Laboratory tests
Concomitant use with opioids
False positive readings may be obtained in the
Patients who require concomitant treatment with semi-quantitative determination of total urine
opioids should be carefully observed for signs of protein by dipstick tests. It is therefore
central nervous system (CNS) depression, such recommended to verify such a positive dipstick
as somnolence, sedation and respiratory test result by methods based on a different
depression. Patients who use gabapentin and analytical principle such as the Biuret method,
morphine concomitantly may experience turbidimetric or dye-binding methods, or to use
increases in gabapentin concentrations. The dose these alternative methods from the beginning.
of gabapentin or opioids should be reduced
Gabapentin Accord-UK capsules contain lactose
appropriately (see section 4.5).
Respiratory depression Patients with rare hereditary problems of
galactose intolerance, the total lactase deficiency
Gabapentin has been associated with severe or glucose galactose malabsorption should not
respiratory depression. Patients with take this medicine.
compromised respiratory function, respiratory or
neurological disease, renal impairment, 4.5 Interaction with other medicinal
concomitant use of CNS depressants and the products and other forms of interaction
elderly might be at higher risk of experiencing There are spontaneous and literature case reports
this severe adverse reaction. Dose adjustments of respiratory depression and/or sedation
might be necessary in these patients. associated with gabapentin and opioid use. In
Use in elderly patients (over 65 years of age) some of these reports, the authors considered
this a particular concern with the combination of
No systematic studies in patients 65 years or gabapentin and opioids, especially in elderly
older have been conducted with gabapentin. In patients.
one double blind study in patients with
neuropathic pain, somnolence, peripheral In a study involving healthy volunteers (N=12),
when a 60mg controlled-release morphine
oedema and asthenia occurred in a somewhat
higher percentage in patients aged 65 years or capsule was administered 2 hours prior to a
600mg gabapentin capsule, mean gabapentin
above, than in younger patients. Apart from
these findings, clinical investigations in this age AUC increased by 44% compared to gabapentin
group do not indicate an adverse event profile administered without morphine. Therefore,
different from that observed in younger patients. patients who require concomitant treatment with
opioids should be carefully observed for signs of
Paediatric population CNS depression, such as somnolence, sedation
and respiratory depression and the dose of
The effects of long-term (greater than 36 weeks) gabapentin or opioid should be reduced
gabapentin therapy on learning, intelligence, and appropriately.
development in children and adolescents have
not been adequately studied. The benefits of No interaction between gabapentin and
prolonged therapy must therefore be weighed phenobarbital, phenytoin, valproic acid, or
against the potential risks of such therapy. carbamazepine has been observed.
Abuse and Dependence Gabapentin steady-state pharmacokinetics are
similar for healthy subjects and patients with
Cases of abuse and dependence have been epilepsy receiving these antiepileptic agents.
reported in the post-marketing database.
Carefully evaluate patients for a history of drug Coadministration of gabapentin with oral
abuse and observe them for possible signs of contraceptives containing norethindrone and/or
ethinyl estradiol, does not influence the steady- There are no adequate data from the use of
state pharmacokinetics of either component. gabapentin in pregnant women.
Coadministration of gabapentin with antacids Studies in animals have shown reproductive
containing aluminium and magnesium, reduces toxicity (see section 5.3). The potential risk for
gabapentin bioavailability up to 24%. It is humans is unknown. Gabapentin should not be
recommended that gabapentin be taken at the used during pregnancy unless the potential
earliest two hours following antacid benefit to the mother clearly outweighs the
administration. potential risk to the foetus.
Renal excretion of gabapentin is unaltered by No definite conclusion can be made as to
probenecid. whether gabapentin is associated with an
increased risk of congenital malformations when
A slight decrease in renal excretion of taken during pregnancy, because of epilepsy
gabapentin that is observed when it is itself and the presence of concomitant
coadministered with cimetidine is not expected antiepileptic medicinal products during each
to be of clinical importance. reported pregnancy.
4.6 Fertility, Pregnancy and lactation Breast-feeding
Pregnancy
Gabapentin is excreted in human milk. Because
Pregnancy the effect on the breast-fed infant is unknown,
caution should be exercised when gabapentin is
Risk related to epilepsy and antiepileptic administered to a breast-feeding mother.
medicinal products in general Gabapentin should be used in breast-feeding
The risk of birth defects is increased by a factor mothers only if the benefits clearly outweigh the
of 2 – 3 in the offspring of mothers treated with risks.
an antiepileptic medicinal product. Most Fertility
frequently reported are cleft lip, cardiovascular
malformations and neural tube defects. Multiple There is no effect on fertility in animal studies
antiepileptic drug therapy may be associated (see section 5.3).
with a higher risk of congenital malformations
4.7 Effects on ability to drive and use
than monotherapy, therefore it is important that
machines
monotherapy is practiced whenever possible. Gabapentin may have minor or moderate
Specialist advice should be given to women who
influence on the ability to drive and use
are likely to become pregnant or who are of
machines. Gabapentin acts on the central
childbearing potential and the need for nervous system and may cause drowsiness,
antiepileptic treatment should be reviewed when dizziness or other related symptoms.
a woman is planning to become pregnant. No
sudden discontinuation of antiepileptic therapy Even, if they were only of mild or moderate
should be undertaken as this may lead to degree, these undesirable effects could be
breakthrough seizures, which could have serious potentially dangerous in patients driving or
consequences for both mother and child. operating machinery. This is especially true at
Developmental delay in children of mothers the beginning of the treatment and after increase
with epilepsy has been observed rarely. in dose.
It is not possible to differentiate if the 4.8 Undesirable Effects
developmental delay is caused by genetic, social The adverse reactions observed during clinical
factors, maternal epilepsy or the antiepileptic studies conducted in epilepsy (adjunctive and
therapy. monotherapy) and neuropathic pain have been
provided in a single list below by class and
Risk related to gabapentin
frequency (very common (> 1/10); common
Gabapentin crosses the human placenta. (>1/100, <1/10); uncommon (>1/1000, <1/100);
rare (>1/10,000; <1/1,000); very rare Very common: somnolence, dizziness, ataxia,
(<1/10,000). Where an adverse reaction was
seen at different frequencies in clinical studies, it Common: convulsions, hyperkinesias,
was assigned to the highest frequency reported. dysarthria, amnesia, tremor, insomnia, headache,
sensations such as paresthesia, hypaesthesia,
Additional reactions reported from the post- coordination abnormal, nystagmus, increased,
marketing experience are included as frequency decreased, or absent reflexes
'Not known' (cannot be estimated from the
available data) in italics in the list below. Within Uncommon: hypokinesia, mental impairment
each frequency grouping, undesirable effects are Rare: loss of consciousness
presented in order of decreasing seriousness.
Not known: other movement disorders (e.g.
Infections and infestations choreoathetosis, dyskinesia, dystonia),
Very Common: Viral infection Eye disorders
Common: Pneumonia, respiratory infection, Common: visual disturbances such as
urinary tract infection, infection, otitis media amblyopia, diplopia
Blood and the lymphatic system disorders Ear and Labyrinth disorders
Common: leucopenia Common: vertigo
Not known: thrombocytopenia Not known: tinnitus
Immune system disorders Cardiac disorders
Uncommon: allergic reactions (e.g. urticaria) Uncommon: palpitations
Not known: anaphylaxis, Hypersensitive Vascular disorder
syndrome, a systemic reaction with a variable
presentation that can include fever, rash, Common: hypertension, vasodilatation
hepatitis lymphadenopathy, eosinophilia and Respiratory, thoracic and mediastinal
sometimes other signs and symptoms (see disorders
section 4.4).
Common: dyspnoea, bronchitis, pharyngitis,
Metabolism and Nutrition Disorders cough, rhinitis
Common: anorexia, increased appetite Rare: Respiratory depression
Uncommon: hyperglycaemia (most often Gastrointestinal disorders
observed in patients with diabetes)
Common: vomiting, nausea, dental
Rare: hypoglycaemia (most often observed in abnormalities, gingivitis, diarrhoea, abdominal
patients with diabetes) pain, dyspepsia, constipation, dry mouth or
Not known: hyponatraemia throat, flatulence
Psychiatric disorders Uncommon: dysphagia
Common: hostility, confusion and emotional Not known: pancreatitis

lability, depression, anxiety, nervousness, Hepatobiliary disorders
thinking abnormal
Not known: hepatitis, jaundice
Uncommon: agitation
Skin and subcutaneous tissue disorders
Not known: hallucinations
Nervous system disorders
Common: facial oedema, purpura most often Common: accidental injury, fracture, abrasion
described as bruises resulting from physical
trauma, rash, pruritus, acne Uncommon: fall
Not known: Stevens-Johnson syndrome, Under treatment with gabapentin cases of acute
angioedema, erythema multiforme, pancreatitis were reported. Causality with
gabapentin is unclear (see section 4.4).
alopecia, drug rash with eosinophilia and
systemic symptoms (see section 4.4) In patients on haemodialysis due to end-stage
renal failure, myopathy with elevated creatine
Musculoskeletal, connective tissue and bone
kinase levels has been reported.
disorders
Common: arthralgia, myalgia, back pain, Respiratory tract infections, otitis media,
twitching convulsions and bronchitis were reported only in
clinical studies in children.
Not known: rhabdomyolysis, myoclonus
Additionally, in clinical studies in children,
Renal and urinary disorders aggressive behaviour and hyperkinesias were
reported commonly.
Not known: acute renal failure, incontinence
Reporting of suspected adverse reactions
Reproductive system and breast disorders
Reporting suspected adverse reactions after
Common: impotence
authorisation of the medicinal product is
Not known: breast hypertrophy, gynaecomastia, important. It allows continued monitoring of the
sexual dysfunction (including changes in libido, benefit/risk balance of the medicinal product.
ejaculation disorders and anorgasmia)
4.9 Overdose
General disorders and administration site Acute, life-threatening toxicity has not been
conditions observed with gabapentin overdoses of up to
Very Common: fatigue, fever 49g. Symptoms of the overdoses included
dizziness, double vision, slurred speech,
Common: peripheral oedema, abnormal gait, drowsiness, loss of consciousness, lethargy and
asthenia, pain, malaise, flu syndrome mild diarrhoea.
Uncommon: generalized oedema All patients recovered fully with supportive care.
Not known: withdrawal reactions (mostly Reduced absorption of gabapentin at higher
anxiety, insomnia, nausea, pains, sweating), doses may limit drug absorption at the time of
chest pain. Sudden unexplained deaths have overdosing and, hence, minimize toxicity from
been reported where a causal relationship to overdoses.
treatment with gabapentin has not been Overdoses of gabapentin, particularly in
established. combination with other CNS depressant
Investigations medications, may result in coma.
Common: WBC (white blood cell count) Although gabapentin can be removed by
decreased, weight gain haemodialysis, based on prior experience it is
usually not required.
Uncommon: elevated liver function tests SGOT
(AST), SGPT (ALT) and bilirubin However, in patients with severe renal
impairment, haemodialysis may be indicated.
Not known: blood creatine phosphokinase
increased An oral lethal dose of gabapentin was not
identified in mice and rats given doses as high as
Injury and poisoning 8000mg/kg.
Signs of acute toxicity in animals included A clinical trial of adjunctive treatment of partial
ataxia, laboured breathing, ptosis, hypoactivity, seizures in paediatric subjects, ranging in age
or excitation. from 3 to 12 years, showed a numerical but not
statistically significant difference in the 50%
5. PHARMACOLOGICAL PROPERTIES responder rate in favour of the gabapentin group
5.1 Pharmacodynamic properties compared to placebo. Additional post-hoc
analyses of the responder rates by age did not
Pharmacotherapeutic groups: Other reveal a statistically significant effect of age,
antiepileptics either as a continuous or dichotomous variable
(age groups 3-5 and 6-12 years). The data from
Mechanism of action this additional post-hoc analysis are summarised
Gabapentin readily enters the brain and prevents in the table below:
seizures in a number of animal models of
Response (≥ 50% Improved) by Treatment and Age
epilepsy. Gabapentin does not possess affinity
MITT* Population
for either GABAA or GABAB receptor nor does
it alter the metabolism of GABA. It does not Age Category Placebo Gabapentin P-Value
bind to other neurotransmitter receptors of the < 6 Years Old 4/21 4/17 0.7362
brain and does not interact with sodium (19.0%) (23.5%)
channels. Gabapentin binds with high affinity to
6 to 12 Years 17/99 20/96 0.5144
the α2δ (alpha-2-delta) subunit of voltage-gated
Old (17.2%) (20.8%)
calcium channels and it is proposed that binding
to the α2δ subunit may be involved in *The modified intent to treat population was
gabapentin's anti-seizure effects in animals. defined as all patients randomised to study
Broad panel screening does not suggest any medication who also had evaluable seizure
other drug targets other than α2δ. diaries available for 28 days during both the
baseline and double-blind phases.
Evidence from several pre-clinical models
inform that the pharmacological activity of 5.2 Pharmacokinetic properties
gabapentin may be mediated via binding to α2δ Absorption
through a reduction in release of excitatory
neurotransmitters in regions of the central Following oral administration, peak plasma
nervous system. Such activity may underlie gabapentin concentrations are observed within 2
gabapentin's anti-seizure activity. The relevance to 3 hours.
of these actions of gabapentin to the Gabapentin bioavailability (fraction of dose
anticonvulsant effects in humans remains to be absorbed) tends to decrease with increasing
established. dose. Absolute bioavailability of a 300mg
Gabapentin also displays efficacy in several pre- capsule is approximately 60%. Food, including a
clinical animal pain models. Specific binding of high-fat diet, has no clinically significant effect
gabapentin to the α2δ subunit is proposed to on gabapentin pharmacokinetics.
result in several different actions that may be Gabapentin pharmacokinetics are not affected by
responsible for analgesic activity in animal repeated administration. Although plasma
models. The analgesic activities of gabapentin gabapentin concentrations were generally
may occur in the spinal cord as well as at higher between 2µg/ml and 20µg/ml in clinical studies,
brain centres through interactions with such concentrations were not predictive of safety
descending pain inhibitory pathways. The or efficacy. Pharmacokinetic parameters are
relevance of these pre-clinical properties to given in Table 3.
clinical action in humans is unknown.
Table 3
Clinical efficacy and safety
Summary of gabapentin mean (%CV) steady- In elderly patients, and in patients with impaired
state pharmacokinetic parameters following renal function, gabapentin plasma clearance is
every eight hours administration reduced.
Pharmacokine 300mg 400mg 800mg Gabapentin elimination-rate constant, plasma

tic parameter (N = 7) (N = 14) (N=14) clearance, and renal clearance are directly
proportional to creatinine clearance.
Mea %C Mea %C Mea %C
n V n V n V Gabapentin is removed from plasma by
Cmax (μg/ml) 4.02 (24) 5.74 (38) 8.71 (29) haemodialysis. Dosage adjustment in patients
with compromised renal function or undergoing
tmax (hr) 2.7 (18) 2.1 (54) 1.6 (76) haemodialysis is recommended (see section 4.2).
T1/2 (hr) 5.2 (12) 10.8 (89) 10.6 (41)
Gabapentin pharmacokinetics in children were
AUC (0-8) 24.8 (24) 34.5 (34) 51.4 (27) determined in 50 healthy subjects between the
μg•hr/ml) ages of 1 month and 12 years. In general, plasma
Ae% (%) NA NA 47.2 (25) 34.4 (37) gabapentin concentrations in children > 5 years
Cmax = Maximum steady state plasma of age are similar to those in adults when dosed
concentration on a mg/kg basis.
tmax = Time for Cmax In a pharmacokinetic study in 24 healthy
T1/2 = Elimination half-life paediatric subjects aged between 1 month and 48
AUC(0-8) = Steady state area under plasma months, an approximately 30% lower exposure
concentration-time curve from time 0 to 8 hours (AUC), lower Cmax and higher clearance per
postdose body weight have been observed in comparison
Ae% = Percent of dose excreted unchanged into to available reported data in children older than
the urine from time 0 to 8 hours postdose 5 years.
NA = Not available
Distribution Linearity/Non-linearity
Gabapentin is not bound to plasma proteins and Gabapentin bioavailability (fraction of dose
has a volume of distribution equal to 57.7 litres. absorbed) decreases with increasing dose which
In patients with epilepsy, gabapentin imparts non-linearity to pharmacokinetic
concentrations in cerebrospinal fluid (CSF) are parameters which include the bioavailability
approximately 20% of corresponding steady- parameter (F) e.g. Ae%, CL/F, Vd/F.
state trough plasma concentrations. Gabapentin Elimination pharmacokinetics (pharmacokinetic
is present in the breast milk of breast-feeding parameters which do not include F such as CLr
women. and T1/2), are best described by linear
pharmacokinetics. Steady state plasma
Biotransformation gabapentin concentrations are predictable from
single-dose data.
There is no evidence of gabapentin metabolism
in humans. Gabapentin does not induce hepatic 5.3 Preclinical safety data
mixed function oxidase enzymes responsible for
drug metabolism. Carcinogenesis
Elimination Gabapentin was given in the diet to mice at 200,

600, and 2000mg/kg/day and to rats at 250,
Gabapentin is eliminated unchanged solely by 1000, and 2000mg/kg/day for two years. A
renal excretion. The elimination half-life of statistically significant increase in the incidence
gabapentin is independent of dose and averages of pancreatic acinar cell tumours was found only
5 to 7 hours. in male rats at the highest dose. Peak plasma
drug concentrations in rats at 2000mg/kg/day are
10 times higher than plasma concentrations in
humans given 3600mg/day. The pancreatic
acinar cell tumours in male rats are low-grade teratology study, and 500, 1000, and
malignancies, did not affect survival, did not 2000mg/kg/day in a perinatal and postnatal
metastasize or invade surrounding tissue, and study. The significance of these findings is
were similar to those seen in concurrent unknown, but they have been associated with
controls. The relevance of these pancreatic delayed development. These doses are also
acinar cell tumours in male rats to carcinogenic approximately 1 to 5 times the human dose of
risk in humans is unclear. 3600 mg on a mg/m2 basis.
Mutagenesis In a teratology study in rabbits, an increased
incidence of post-implantation foetal loss,
Gabapentin demonstrated no genotoxic
occurred in pregnant rabbits given 60, 300, and
potential. It was not mutagenic in vitro in 1500mg/kg/day during organogenesis. These
standard assays using bacterial or mammalian doses are approximately 0.3 to 8 times the daily
cells. Gabapentin did not induce structural human dose of 3600mg on a mg/m2 basis.
chromosome aberrations in mammalian cells in
vitro or in vivo, and did not induce micronucleus The margins of safety are insufficient to rule out
formation in the bone marrow of hamsters. the risk of these effects in humans.
Impairment of Fertility 6. PHARMACEUTICAL PARTICULARS
No adverse effects on fertility or reproduction
6.1 List of excipients
were observed in rats at doses up to 2000mg/kg Lactose Monohydrate
(approximately five times the maximum daily
human dose on a mg/m2 of body surface area Maize Starch
basis).
Talc
Teratogenesis
Capsule shell
Gabapentin did not increase the incidence of
Titanium dioxide, E171
malformations, compared to controls, in the
offspring of mice, rats, or rabbits at doses up to Yellow iron oxide, E172
50, 30 and 25 times respectively, the daily
human dose of 3600mg, (four, five or eight Gelatin
times, respectively, the human daily dose on a Printing ink
mg/m2 basis).
Shellac, E904
Gabapentin induced delayed ossification in the
skull, vertebrae, forelimbs, and hind limbs in Propylene glycol, E1520
rodents, indicative of foetal growth retardation. Black iron oxide, E172
These effects occurred when pregnant mice
received oral doses of 1000 or 3000mg/kg/day Potassium hydroxide, E525
during organogenesis and in rats given
6.2 Incompatibilities
2000mg/kg prior to and during mating and
Not applicable.
throughout gestation. These doses are
approximately 1 to 5 times the human dose of 6.3 Shelf life
3600mg on a mg/m2 basis. 3 years.
No effects were observed in pregnant mice given 6.4 Special precautions for storage
500mg/kg/day (approximately 1/2 of the daily Do not store above 25°C.
human dose on a mg/m2 basis).
Store in the original package in order to protect
An increased incidence of hydroureter and/or from moisture
hydronephrosis was observed in rats given
2000mg/kg/day in a fertility and general 6.5 Nature and contents of container
reproduction study, 1500mg/kg/day in a
Aluminium/transparent PVC blisters

Each pack will contain either 30, 50, 60, 100 or
120 capsules.
Each blister strip will contain 10 capsules.
Not all pack sizes may be marketed.
6.6 Special precautions for disposal and
other handling
No special requirements.
7. MANUFACTURER:
Manufactured in India by:

TAJ PHARMACEUTICALS LTD.
Mumbai, India
At: 615, GIDC, Kerala, Bavla, Dist. Ahmedabad
438225, Gujarat, INDIA
This leaflet was last revised in October 2019

Gabapentin 300mg Capsules SMPC - Taj Pharmaceuticals

Uploaded by

Document Information

Original Title

Copyright

Available Formats

Share this document

Share or Embed Document

Sharing Options

Did you find this document useful?

Is this content inappropriate?

Copyright:

Available Formats

Gabapentin 300mg Capsules SMPC - Taj Pharmaceuticals

Uploaded by

Copyright:

Available Formats

Gabapentin 300mg capsules SMPC, Taj Pharmaceuticals

which is recommended for adults and

Psychiatric disorders Uncommon: dysphagia

Common: hostility, confusion and emotional Not known: pancreatitis

Pharmacokine 300mg 400mg 800mg Gabapentin elimination-rate constant, plasma

Elimination Gabapentin was given in the diet to mice at 200,

Aluminium/transparent PVC blisters

Manufactured in India by:

This leaflet was last revised in October 2019

You might also like