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Annex I : CSP Gastrozepin
In PAR:
Proposed CSP with assessor comments, if any
In Draft FAR: Proposed CSP with assessor comments
In FAR: Agreed CSP
Proposed CSP
4.2 POSOLOGY AND METHOD OF ADMINISTRATION
Tablets:
Unless otherwise prescribed, 50 to 150 mg per day in divided doses. In general, 50 mg twice daily,
morning and evening, is recommended. Occasionally it may be necessary for the first 2 or 3 days of
treatment to administer an additional dose at midday. The tablets should be taken approximately 1/2
hour before meals with a little liquid. In spite of a rapid subjective improvement, the patient should in
no case reduce or break off the treatment prescribed by the physician.
Therapy should always be continued with oral pirenzepine dihydrochloride for a period of 4 to 6 weeks.
Ampoules:
Unless otherwise prescribed, one ampoule should be injected intramuscularly or intravenously every
12 hours.
For the prophylaxis and treatment of stress ulcers, administration of one ampoule 3 times daily (every
8 hours) is recommended.
Parenteral pirenzepine dihydrochloride therapy should be continued until symptoms disappear, usually
for 2-3 days, when Pirenzepine can be administered orally.
Note: Intravenous administration should be by slow injection (more than 3 minutes), or preferably
by drip infusion. Intravenous infusion: pirenzepine dihydrochloride solution may be combined with
isotonic saline solution, Ringer solution, 5% laevulose, 5% glucose solution.
Paediatric population
The safety and efficacy of pirenzepine dihydrochloride in paediatric populations aged below 18 years
has not been established.
4.3 CONTRAINDICATIONS
Pirenzepine dihydrochloride should not be used in cases of known hypersensitivity to any of the
components of the drug and in patients with paralytic ileus.
In case of rare hereditary conditions that may be incompatible with an excipient of the product (please
refer to “Special warnings and precautions for use”) the use of this product is contraindicated.
4.4 SPECIAL WARNINGS AND PRECAUTIONS FOR USE
Pirenzepine should be used with caution in patients with:
- glaucoma
- prostatic hypertrophy
- tachycardia
Intravenous injection should always be slow:
1. because of the risk of thrombophlebitis in view of the content of 39,2% propylene glycol
2. in patients with unstable circulation because of high initial pirenzepine plasma concentrations; blood
pressure must be constantly monitored.
Tablets:
Pirenzepine dihydrochloride tablets 25 mg contain 833,64 mg lactose per maximum recommended
daily dose. Patients with rare hereditary conditions of galactose intolerance e.g. galactosaemia, the
Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
Pirenzepine dihydrochloride tablets 50 mg contain 438.78 mg lactose per maximum recommended
daily dose.
Patients with rare hereditary conditions of galactose intolerance e.g. galactosaemia should not take
this medicine.
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Ampoules:
This medicinal product contains less than 1 mmol sodium (23 mg) per single recommended dose, i.e.
essentially “sodium-free”.
4.5 INTERACTION WITH OTHER MEDICINAL PRODUCTS AND OTHER FORMS OF
INTERACTIONS
Concurrent treatment with pirenzepine dihydrochloride and H2-receptor blockers leads to a more
pronounced reduction in gastric acid secretion. The action of anti-inflammatory agents is not impaired
when these are used together with pirenzepine dihydrochloride. On the other hand, gastro-intestinal
tolerance of these products is improved.
4.6 FERTILITY, PREGNANCY AND LACTATION
There is limited data from the use of pirenzepine in pregnant women. Animal studies do not indicate
direct or indirect harmful effects with respect to fertility and reproductive toxicity.
There is evidence that pirenzepine is excreted into breast milk, even though in small amounts.
As a result anticholinergic effects may occur in breast fed infants.
No studies on the effect in human fertility have been conducted.
As a precautionary measure, it is preferable to avoid the use of pirenzepine dihydrochloride during
pregnancy and lactation.
4.7 EFFECTS ON ABILITY TO DRIVE AND USE MACHINES
No studies on the effects on the ability to drive and use machines have been performed. However,
patients should be advised that they may experience undesirable effects such as accommodation
disorders during treatment with pirenzepine dihydrochloride. Therefore, caution should be
recommended when driving a car or operating machinery. If patients experience accommodation
disorders they should avoid potentially hazardous tasks such as driving or operating machinery.
4.8 UNDESIRABLE EFFECTS
Adverse reactions have been ranked under headings of frequency using the following convention:
very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1,000 to <1/100); rare (≥1/10,000 to
<1/1,000); very rare (<1/10,000), not known (cannot be estimated from the available data).
System Organ Class:
MedDRA Term
Immune system disorders:
Anaphylactic reactions
Hypersensitivity
Nervous system disorders:
Headache
Eye disorders:
Accommodation disorders
Cardiac disorders:
Tachycardia
Gastrointestinal disorders:
Dry mouth
Constipation
Diarrhoea
Skin and subcutaneous disorders:
Rash
Renal and urinary disorders:
Urinary retention
Frequency
Not known
Not known
Common
Common
Not known
Very common
Common
Common
Common
Uncommon
4.9 OVERDOSE
Symptoms
If large doses of pirenzepine are ingested the following anticholinergic effects may develop: warm, dry,
flushed skin; dry mouth; mydriasis; delirium; tachycardia; ileus; urinary retention; jerky myoclonic
movements; choreo-athetosis.
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Therapy
Haemodialysis, haemoperfusion, peritoneal dialysis and repeated doses of charcoal are not effective
in removing anticholinergic agents. In case of severe intoxication (e.g. hyperthermia, severe delirium
or tachycardia) a small dose of physostigmine intravenously can be given.
In case of an acute glaucoma episode treatment with miotic drops should be initiated and specialist
advice sought immediately