SUMATRIPTAN TABLETS 100MG

Active substance: SUMATRIPTAN SUCCINATE

View full screen / Print PDF » Download PDF ⇩

Transcript
SUMMARY OF PRODUCT CHARACTERISTICS

1

NAME OF THE MEDICINAL PRODUCT
Sumatriptan 100 mg Tablets

2.

QUALITATIVE AND QUANTITATIVE COMPOSITION
Each tablet contains 100 mg sumatriptan (as the succinate).
Also contains: lactose monohydrate. For full list of excipients, see Section 6.1

3.

PHARMACEUTICAL FORM
Film coated tablet.
Sumatriptan 100 mg tablets are white, film-coated, oblong, biconvex tablets.

4.

CLINICAL PARTICULARS

4.1

Therapeutic Indications
Sumatriptan tablets are indicated for the acute relief of migraine attacks, with or
without aura.
Sumatriptan tablets should only be used where there is a clear diagnosis of
migraine.

4.2

Posology and Method of Administration
The tablets should be swallowed whole with water.
Sumatriptan is recommended as monotherapy for the acute treatment of
migraine and should not be given concomitantly with other acute migraine
therapies. If a patient fails to respond to a single dose of sumatriptan there are
no reasons, either on theoretical grounds or from limited clinical experience, to
withhold products containing aspirin or non-steroidal anti-inflammatory drugs
for further treatment of the attack.
Adults only:
Sumatriptan tablets are indicated for the acute intermittent treatment of migraine.
It should not be used prophylactically.

It is advisable that sumatriptan be given as early as possible after the onset of an
attack of migraine but it is equally effective at whatever stage of the attack it is
administered.
The recommended adult dose of oral sumatriptan is a single 50 mg tablet. Some
patients may require 100 mg.
If a patient does not respond to the first dose of Sumatriptan tablets, a second
should not be taken for the same attack. Sumatriptan tablets may be taken for
subsequent attacks.
Patients who respond initially but whose migraine returns may take further doses
in the next 24 hours provided that there is a minimum interval of two hours
between doses. A maximum dose of 300 mg in any 24 hour period should not be
exceeded.
Children (under 18 years):
The safety and effectiveness of sumatriptan in children and adolescents under 18
years has not been established.
Elderly (more than 65 years):
Experience of the use of sumatriptan in patients aged over 65 years is limited.
The pharmacokinetics do not differ significantly from a younger population but,
until further clinical data are available, the use of Sumatriptan tablets in patients
aged over 65 years is not recommended.

4.3

Contraindications
Hypersensitivity to the active substance or to any of the excipients.
Sumatriptan should not be given to patients who have had myocardial
infarction or have ischemic heart disease, coronary vasospasm (Prinzmetal's
angina), peripheral vascular disease or patients who have symptoms or sign
consistent with ischemic heart disease.
Sumatriptan should not be administered to patients with a history of
cerebrovascular accident (CVA) or transient ischemic attack (TIA).
Sumatriptan should not be administered to patients with severe hepatic
impairment.
The use of sumatriptan in patients with moderate and severe hypertension and
mild uncontrolled hypertension is contraindicated.
The concomitant administration of ergotamine or derivatives of ergotamine
(including methysergide) is contraindicated. (See Section 4.5 – Interactions).

Concurrent administration of monoamine oxidase inhibitors and sumatriptan is
contraindicated. Sumatriptan should not be used within two weeks of
discontinuation of therapy with monoamine oxidase inhibitors.
4.4

Special warnings and precautions for use
Sumatriptan should only be used where there is a clear diagnosis of migraine.
Sumatriptan is not indicated for use in the management of hemiplegic, basilar or
ophthalmoplegic migraine.
The recommended doses of sumatriptan should not be exceeded. As with other
migraine therapies, before treating headaches in patients not previously diagnosed as
migraineurs, and in migraineurs who present atypical symptoms, care should be taken
to exclude other potentially serious neurological conditions.
It should be noted that migraineurs may be at risk of certain cerebrovascular events
(e.g. cerebrovascular accident, transient ischemic attack).
Following administration, sumatriptan can be associated with transient symptoms
including chest pain and tightness which may be intense and involve the throat (See
Section 4.8 – Undesirable Effects). Where such symptoms are thought to indicate
ischemic heart disease, no further doses of sumatriptan should be given and
appropriate evaluation should be carried out.
Sumatriptan should not be given to patients with risk factors for ischemic heart
disease without prior cardiovascular evaluation (See Section 4.3 – Contraindications).
Special consideration should be given to postmenopausal women and males over 40
with these risk factors. These evaluations however, may not identify every patient
who has cardiac disease and, in very rare cases, serious cardiac events have occurred
in patients without underlying cardiovascular disease.
Sumatriptan should be administered with caution to patients with controlled
hypertension as transient increases in blood pressure and peripheral vascular
resistance have been observed in a small proportion of patients.
There have been rare post-marketing reports describing patients with weakness,
hyper-reflexia, and in-coordination following the use of a selective serotonin reuptake
inhibitor (SSRI) and sumatriptan. If concomitant treatment with sumatriptan and an
SSRI is clinically warranted, appropriate observation of the patient is advised.
Sumatriptan should be administered with caution to patients with conditions which
may affect significantly the absorption, metabolism or excretion of drugs, e.g.
impaired hepatic or renal function.

Patients with known hypersensitivity to sulphonamides may exhibit an allergic
reaction following administration of sumatriptan. Reactions may range from
cutaneous hypersensitivity to anaphylaxis. Evidence of cross-sensitivity is limited,
however, caution should be exercised before using sumatriptan in these patients.
Undesirable effects may be more common during concomitant use of triptans and
herbal preparations containing St John's Wort (Hypericum perforatum).
These tablets contain lactose. Patients with rare hereditary problems of galactose
intolerance, lactase deficiency or glucose-galactose malabsorption should not take
this medicine.

4.5

Interactions with other medicinal products and other forms of interactions
Studies in healthy subjects show that sumatriptan do not interact with
propranolol, pizotifen or alcohol.
Sumatriptan has the potential to interact with MAOIs, ergotamine and
derivatives of ergotamine. The increased risk of coronary vasospasm is a
theoretical possibility and concomitant administration is contra-indicated. (see
also Section 4.3 – Contraindications).
Prolonged vasospastic reactions have been reported with ergotamine. As these
effects may be additive, 24 hours should elapse before sumatriptan can be
taken following any ergotamine-containing preparation. Conversely,
ergotamine-containing preparations should not be taken until 6 hours have
elapsed following sumatriptan administration.
An interaction may occur between sumatriptan and MAOIs and concomitant
administration is contra-indicated (see Section 4.3 – Contraindications).
Rarely, an interaction may occur between sumatriptan and SSRI's (see Section
4.4 – Special Warnings and Special Precautions for Use).

4.6

Pregnancy and Lactation
Post-marketing data from the use of sumatriptan during the first trimester in over
1,000 women are available. Although these data contain insufficient information
to draw definitive conclusions, they do not point to an increased risk of
congenital defects. Experience with the use of sumatriptan in the second and
third trimester is limited.
Evaluation of experimental animal studies does not indicate direct teratogenic
effects or harmful effects on peri- and postnatal development. However, embryo
foetal viability might be affected in the rabbit (see Section 5.3 – Preclinical
Safety Data).

Administration of sumatriptan should only be considered if the expected benefit
to the mother is greater than any possible risk to the foetus.
It has been demonstrated that following subcutaneous administration,
sumatriptan is excreted into breast milk. Infant exposure can be minimised by
avoiding breast feeding for 24 hours after treatment.
4.7

Effects on ability to drive and use machines
Drowsiness may occur as a result of migraine or its treatment with Sumatriptan
tablets. Caution is recommended in patients performing skilled tasks, e.g.
driving or operating machinery.

4.8

Undesirable effects
General
The following symptoms are usually transient and may be intense and can
affect any part of the body including the chest and throat; pain, sensations of
tingling, heat, heaviness, pressure or tightness. The following symptoms are
mild to moderate in intensity and transient: flushing, dizziness and feelings of
weakness.
Fatigue and drowsiness have been reported.
Cardiovascular
Hypotension, bradycardia, tachycardia, palpitations.
Transient increases in blood pressure arising soon after treatment have been
recorded. In extremely rare cases, serious coronary events have been reported
which have included cardiac arrhythmias, ischaemic ECG changes, coronary
artery vasospasm or myocardial infarction. (see Section 4.3 –
Contraindications and Section 4.4 – Special Warnings and Special
Precautions for Use).
There have also been rare reports of Raynaud's phenomenon and ischaemic
colitis.
Gastrointestinal
Nausea and vomiting occurred in some patients but the relationship to
sumatriptan is not clear.
CNS
There have been rare reports of seizures following use of sumatriptan.
Although some have occurred in patients with either a history of seizures or
concurrent conditions predisposing to seizures there are also reports in patients
where no such predisposing factors are apparent.

Eye Disorders
Patients treated with sumatriptan rarely exhibit visual disorders like flickering
and diplopia. Additionally, cases of nystagmus, scotoma and reduced vision
have been observed. Very rarely, loss of vision has occurred, which is usually
transient. However, visual disorders may also occur during a migraine attack
itself.
Hypersensitivity/skin
Hypersensitivity reactions ranging from cutaneous hypersensitivity to, in rare
cases, anaphylaxis.
Laboratory values
Minor disturbances in liver function tests have occasionally been observed.

4.9

Overdosage
Doses in excess of 400 mg orally were not associated with side effects other than
those mentioned.
If overdosage occurs, the patient should be monitored for at least ten hours and
standard supportive treatment applied as required.
It is unknown what effect haemodialysis or peritoneal dialysis has on the plasma
concentrations of sumatriptan.

5.

PHARMACOLOGICAL PROPERTIES

5.1

Pharmacodynamic properties
Pharmacotherapeutic group: Analgesics: Selective 5-HT1 receptor agonists.
ATC code: N02C C01
Sumatriptan has been demonstrated to be a specific and selective 5Hydroxytryptamine1 (5HT1D) receptor agonist with no effect on other 5HT
receptor (5-HT2-5-HT7) subtypes. The vascular 5-HT1D receptor is found
predominantly in cranial blood vessels and mediates vasoconstriction. In
animals, sumatriptan selectively constricts the carotid arterial circulation but
does not alter cerebral blood flow. The carotid arterial circulation supplies
blood to the extracranial and intracranial tissues such as the meninges and
dilatation of and/or oedema formation in these vessels is thought to be the
underlying mechanism of migraine in man.
In addition, evidence from animal studies suggests that sumatriptan inhibits
trigeminal nerve activity. Both these actions (cranial vasoconstriction and

inhibition of trigeminal nerve activity) may contribute to the anti-migraine
action of sumatriptan in humans.
Clinical response begins around 30 minutes following a 100 mg oral dose.
Although the recommended dose of oral sumatriptan is 50 mg, migraine
attacks vary in severity both within and between patients. Doses of 25-100 mg
have shown greater efficacy than placebo in clinical trials, but 25 mg is
statistically significantly less effective than 50 and 100 mg.

5.2

Pharmacokinetic properties
Following oral administration, sumatriptan is rapidly absorbed, 70% of
maximum concentration occurring at 45 minutes. After 100 mg dose, the
maximum plasma concentration is 54 ng/ml. Mean absolute oral
bioavailability is 14% partly due to presystemic metabolism and partly due to
incomplete absorption. The elimination phase half-life is approximately 2
hours, although there is an indication of a longer terminal phase. Plasma
protein binding is low (14-21%), mean volume of distribution is 170 litres.
Mean total plasma clearance is approximately 1160 ml/min and the mean renal
plasma clearance is approximately 260 ml/min. Non-renal clearance accounts
for about 80% of the total clearance. Sumatriptan is eliminated primarily by
oxidative metabolism mediated by monoamine oxidase A. The major
metabolite, the indole acetic acid analogue of sumatriptan is mainly excreted
in the urine, where it is present as a free acid and the glucuronide conjugate. It
has no known 5HT1 or 5HT2 activity. Minor metabolites have not been
identified. The pharmacokinetics of oral sumatriptan do not appear to be
significantly affected by migraine attacks.
In a pilot study, no significant differences were found in the pharmacokinetic
parameters between the elderly and young healthy volunteers.

5.3

Preclinical Safety Data
Sumatriptan was devoid of genotoxic and carcinogenic activity in in-vitro
systems and animal studies.
In a rat fertility study oral doses of sumatriptan resulting in plasma levels
approximately 200 times those seen in man after a 100 mg oral dose were
associated with a reduction in the success of insemination.
This effect did not occur during a subcutaneous study where maximum plasma
levels achieved approximately 150 times those in man by the oral route.
In rabbits embryo lethality, without marked teratogenic defects, was seen. The
relevance for humans of these findings is unknown.

6.

PHARMACEUTICAL PARTICULARS

6.1

List of Excipients
Tablet:
Lactose monohydrate, microcrystalline cellulose, croscarmellose sodium,
magnesium stearate, purified talc, colloidal anhydrous silica.
Film coat:
Hypromellose, macrogol, purified talc, titanium dioxide (E171), triethyl
citrate.

6.2

Incompatibilities
Not applicable

6.3

Shelf Life
2 years.

6.4

Special Precautions for Storage
No special storage conditions.

6.5

Nature and Contents of Containers
Polyamide/Alu/PVC/Alu blister packs in a cardboard carton with Patient
Information Leaflet. Pack sizes may include 1, 2, 3, 4, 6, 12, 18 or 20 tablets.
Not all pack sizes may be marketed.

6.6

Instructions for use and handling
No special requirements.

7.

MARKETING AUTHORISATION HOLDER
Consilient Health Ltd.
5th Floor, Beaux Lane House
Mercer Street Lower
Dublin 2
Ireland

8.

MARKETING AUTHORISATION NUMBER
PL 24837/0002

9

DATE OF FIRST AUTHORISATION/RENEWAL OF THE
AUTHORISATION

19th May 2006

10.

DATE OF REVISION OF THE TEXT
4th May 2006

Expand view ⇕

Source: Medicines and Healthcare Products Regulatory Agency

Disclaimer: Every effort has been made to ensure that the information provided here is accurate, up-to-date and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. This information has been compiled for use by healthcare practitioners and consumers in the United States. The absence of a warning for a given drug or combination thereof in no way should be construed to indicate that the drug or combination is safe, effective or appropriate for any given patient. If you have questions about the substances you are taking, check with your doctor, nurse or pharmacist.

Hide
(web5)