Pizotifen 0.5mg Tablets
Out of date information, search anotherSUMMARY OF PRODUCT CHARACTERISTICS
1 NAME OF THE MEDICINAL PRODUCT
Pizotifen 0.5mg Tablets.
2
QUALITATIVE AND QUANTITATIVE COMPOSITION
Each tablet contains Pizotifen Malate BP equivalent to Pizotifen 0.5mg.
Excipients: Each tablet contains 66.87 mg lactose monohydrate For excipients, see section 6.1.
3 PHARMACEUTICAL FORM
Tablets.
Pale cream to yellow circular biconvex film-coated tablets marked “PZT 0.5” on one face.
4 CLINICAL PARTICULARS
4.1 Therapeutic indications
Prophylactic treatment of recurrent vascular headaches, including classical migraine, common migraine and cluster headache (periodic migrainous neuralgia).
4.2 Posology and method of administration
Adults including the elderly: Usually 1.5mg daily. This may be taken as a single dose at night or in three divided doses, using 1.5mg tablets or 0.5mg tablets as appropriate. Dosage should be adjusted to individual patients’ requirements up to a maximum of 4.5mg daily. Up to 3mg may be given as a single daily dose.
Children: Up to 1.5mg daily, usually as a divided dose. Use of the 1.5mg tablets is not recommended but up to 1mg has been given as a single dose at night.
Method of administration: Oral.
4.3 Contra-indications
Hypersensitivity to the drug or any of the other ingredients (see section 6.1).
4.4 Special warnings and precautions for use
Although the anticholinergic activity of Pizotifen is relatively weak, caution is required in the presence of closed angle glaucoma and in patients with a predisposition to urinary retention. Dosage adjustment may be necessary in patients with kidney insufficiency. Pizotifen should be used with caution in patients with a history of epilepsy. With reference to the presence of lactose monohydrate in the formulation, patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
4.5 Interaction with other medicinal products and other forms of interaction
The central effects of sedatives, hypnotics, anti-histamines (including certain common cold preparations) and alcohol may be enhanced by Pizotifen.
Pizotifen antagonizes the hypotensive effect of adrenergic neurone blockers.
4.6 Pregnancy and lactation Pregnancy
As clinical data with Pizotifen in pregnancy are very limited it should only be administered during pregnancy under compelling circumstances.
Lactation
Although the concentrations of Pizotifen measured in the milk of treated mothers are not likely to affect the infant, its use in nursing mothers is not recommended.
4.7 Effects on ability to drive and use machines
Patients should be cautioned about the possibility of drowsiness, somnolence and dizziness and informed of its significance in the driving of vehicles and the operation of machinery.
Patients being treated with Pizotifen and presenting with drowsiness (including somnolence and fatigue) must be instructed to refrain from driving or engaging in activities where impaired alertness may put themselves or others at risk.
4.8 Undesirable effects
The most commonly occurring side effects are drowsiness (including somnolence and fatigue) and an increased appetite which may lead to an increase in body weight. Adverse reactions are ranked under headings of frequency, the most frequent first, using the following convention: Very common (>1/10); common (> 1/100, < 1/10); uncommon (> 1/1000, < 1/100); rare (> 1/10,000, < 1/1000); very rare ( < 1/10,000), including isolated reports.
Nervous system disorders:
Common: Drowsiness (including somnolence), dizziness Rare: Paraesthesia Very rare: Seizures
Eye disorders:
Very Rare: Angle closure glaucoma
Gastrointestinal disorders:
Common: Dry mouth, Nausea Uncommon: Constipation
Psychiatric disorders:
Rare: In children CNS stimulation (e.g. agitation), sleep disorders, depression, and other mood disturbances such as anxiety and aggression, hallucination, insomnia.
Immune system disorders:
Rare: Hypersensitivity reactions, face oedema, urticaria, rash
Metabolism and nutrition disorders:
Very common: Appetite stimulating effect and increase in body weight
Musculoskeletal and connective tissue disorders:
Rare: Myalgia, arthralgia
General disorders and administration site conditions:
Common: Fatigue
Acute withdrawal reactions have been reported following abrupt cessation of pizotifen, therefore, gradual withdrawal is recommended. Withdrawal symptoms include anxiety, tremors, insomnia, nausea, and loss of consciousness.
4.9 Overdose
Symptoms of overdosage may include drowsiness, dizziness, hypotension, dryness of the mouth, confusion, excitatory states (in children), ataxia, nausea, vomiting, dyspnoea, cyanosis, tachycardia, convulsions (particularly in children), coma and respiratory paralysis. Treatment should be directed to the elimination of the drug by gastric lavage in case of very recent uptake, diuresis or administration of activated charcoal. Severe hypotension must be corrected (cave: adrenaline may produce paradoxical effects). Excitatory states or convulsions may be treated with short-acting barbiturates or benzodiazepines. General surveillance measures are indicated including monitoring of the cardiovascular and respiratory systems.
5 PHARMACOLOGICAL PROPERTIES
5.1 Pharmacodynamic properties
ATC Code: N02C X01
Pizotifen has powerful antiserotonin and antitryptaminic properties, marked antihistaminic effects and some antagonistic activity against kinins. It also possesses weak anticholinergic effects and sedative properties.
Pizotifen also possesses appetite-stimulating properties.
The prophylactic effect of Pizotifen in migraine is associated with its ability to modify the humoral mechanisms of headache.
It inhibits the permeability-increasing effect of serotonin and histamine on the affected cranial vessels, thereby checking the transudation of plasmakinin so that the pain threshold of the receptors is maintained at ‘normal’ levels. In the sequence of events leading to the migraine attack, depletion of plasma serotonin contributes to loss of tone in the extracranial vessels. Pizotifen inhibits serotonin re-uptake by the platelets, thus maintaining plasma serotonin and preventing the loss of tone and passive distension of the extracranial arteries.
5.2 Pharmacokinetic properties
Pizotifen is well absorbed from the gastro-intestinal tract with over 80% being absorbed. Absorption is relatively fast with an absorption half-life of 0.5 to 0.8 hours. Peak plasma concentrations occur approximately 5 hours after oral administration. Over 90% of Pizotifen is bound to plasma proteins. The metabolism of Pizotifen is extensive with 55% excreted as metabolites. Less than 1% is excreted unchanged. Over half a dose is excreted in the urine, chiefly as metabolites; a significant proportion is excreted in the faeces. Pizotifen is metabolised with a half-life of about 1 hour. The primary metabolite of Pizotifen, N-glucuronic conjugate, has a long elimination half-life of about 23 hours.
5.3 Preclinical safety data
No preclinical data relevant to prescriber.
PHARMACEUTICAL PARTICULARS
6
6.1 List of excipients
Lactose Monohydrate Microcrystalline Cellulose Magnesium Stearate Hypromellose (E464)
Titanium Dioxide (El71)
Macrogol
Iron Oxide Yellow (El72)
Quinoline Yellow Aluminium Lake (B 104) Iron Oxide Black (El72)
6.2 Incompatibilities
Not applicable
6.3 Shelf life
24 months
6.4 Special precautions for storage
Store below 25°C. Keep the tablets in the original package.
6.5 Nature and contents of container
Pizotifen Tablets BP 0.5mg will be packed into either of the following presentations:
Blister strips constructed of 250pm PVC with a 60g/m2 PVdC coating and 20pm aluminium foil with a heat sealing lacquer. The blister strips are packed into a cardboard carton. Each carton contains 28 or 84 tablets.
Polypropylene containers fitted with a polyethylene cap and a tamper-evident tear strip. Each container holds 84 tablets.
Not all pack sizes may be marketed
Instructions for use/handling
6.6
No special requirements
Any used product or waste material should be disposed of in accordance with local requirements.
7. MARKETING AUTHORISATION HOLDER
Tillomed Laboratories Limited
3 Howard Road
Eaton Socon
St Neots
Cambridgeshire
PE19 8ET
UK
8. MARKETING AUTHORISATION NUMBER(S)
PL 11311/0379
9 DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION
07/05/2009