Almirall Limited

Meptid 200 mg Film-Coated Tablets

Each tablet contains 200 mg of meptazinol (as hydrochloride).

Excipient:

Sunset yellow (E110) 2.15 mg

For a full list of excipients, see section 6.1

Film-coated tablet.

Oval, biconvex, orange, film-coated tablets. The tablets are engraved “MPL 023” on one side.

For short term treatment of moderate pain.

Adults

200 mg 3 to 6 hourly as required. Usually 1 tablet 4 hourly.

Elderly

The adult dosage schedule may be used in the elderly.

Children

Meptid tablets have not been evaluated for use in children.

Patients with the following conditions:

- known hypersensitivity to the active ingredient or to any of the excipients

- acute alcoholism and where there is a risk of paralytic ileus

- raised intracranial pressure or head injury (in addition to interfering with respiration, affects pupillary responses vital for neurological assessment)

- acute respiratory depression

- during an asthma attack

- patients on monoamine-oxidase inhibitors (MAOIs) and for 14 days after discontinuing an MAOI. (see section 4.5)

Meptazinol has a favourable respiratory profile but caution should be exercised in patients whose respiratory system is already compromised.

Patients with moderate to severe renal impairment should be given a reduced dose as the effect in these patients may be prolonged and increased. Patients with hepatic impairment should be given a reduced dose as opioid analgesics may precipitate coma in these patients.

Safety in long term use is not known, therefore it is recommended that this drug be used in the treatment of moderate pain, for short periods of time. Repeated administration of opioid analgesics may cause dependence and tolerance (severe withdrawal symptoms if withdrawn abruptly).

Safety for use in myocardial infarction has not been established.

Meptazinol should also be used with caution in patients with the following conditions: hypotension, hypothyroidism, asthma (avoid during an attack), prostatic hypertrophy and convulsive disorders.

Sunset yellow FCF (E 110) can cause allergic-type reactions including asthma. Allergy is more common in those people who are allergic to aspirin.

The following undesirable effects could occur as a result of possible interaction with meptazinol hydrochloride.

Antidepressants: CNS excitation or depression manifesting as hypertension or hypotension may occur if meptazinol is administered to patients receiving MAOIs (including moclobemide). Avoid concomitant use for 14 days after an MAOI is discontinued (see section 4.3). Possible increased sedation if meptazinol is used with tricyclic antidepressants.

Antipsychotics: enhanced sedative and hypotensive effect.

Antivirals: avoid concomitant use with ritonavir as plasma concentration of meptazinol may be increased.

Alcohol: enhanced sedative and hypotensive effect.

Quinolones (ciprofloxacin): avoid premedication with meptazinol as a reduced plasma-ciprofloxacin concentration may be experienced.

Anxiolytics and hypnotics: enhanced sedative effect.

Drugs used in nausea and vomiting: concomitant use of metoclopramide and domperidone may result in antagonism of gastrointestinal side effects.

Ulcer healing drugs: cimetidine may inhibit metabolism of meptazinol resulting in increased plasma concentration.

No clinical data on exposed pregnancies are available.

Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/foetal development, parturition or postnatal development.

Meptazinol should not be used during pregnancy, unless considered essential by the physician.

Meptazinol should not be used during breast-feeding.

Since dizziness and occasionally drowsiness have been reported, patients should be cautioned against driving or operating machinery until it is established that they do not become dizzy or drowsy whilst taking meptazinol.

For very rare reports of psychiatric disorders (hallucination, confusion, depression), causal relationship with meptazinol has not been established and therefore omitted from the above table.

Reactions not already stated which are attributable to opioid analgesics include difficulty with micturition, ureteric or biliary spasm, dry mouth, facial flushing , bradycardia, tachycardia, palpitations, hypothermia, dysphoria, mood changes, miosis, decreased libido or potency, urticaria and pruritus.

Meptid tablets are subject to hepatic first pass metabolism which prevents systemic concentration of the drug reaching levels achieved by parenteral administration.

Recommended treatment includes gastric lavage, supportive therapy and naloxone if required.

In the unlikely event of overdose producing respiratory depression, naloxone is the treatment of choice. Naloxone has a short duration of action in comparison with meptazinol. Repeated administration or administration by continuous intravenous infusion may be considered necessary. The effects are only partially reversed by naloxone.

Meptid (meptazinol) is a centrally acting analgesic belonging to the hexahydroazepine series, which has demonstrated mixed agonist and antagonist activity at opioid receptors.

Receptor binding studies have shown that although meptazinol displays only a low affinity for δ and κ opioid receptor sites, it has a somewhat higher affinity for a subpopulation of μ sites. These binding sites also display a high affinity for the endogenous opioid peptides, and are thought to be responsible for, among other things, analgesia, but not for the mediation of respiratory depression.

A component of its analgesic action is also attributable, in mice at least, to an effect on central cholinergic transmission. In this respect it differs from all conventional analgesic drugs which have been examined.

After oral administration, meptazinol is rapidly absorbed and peak plasma levels are reached within 90 minutes. The plasma elimination half-life is variable (1.4- 4 hours). The peak analgesic effect is seen within 30-60 minutes and lasts about 3 - 4 hours.

The drug is rapidly metabolised to the glucronide, and mostly excreted in the urine.

Standard toxicity tests revealed no unexpected findings of clinical significance.

Tablet Core

Microcrystalline cellulose

Polacrilin potassium (as Amberlite IRP 88)

Magnesium stearate

Tablet Coating

Hypromellose

Macrogol 400

Opaspray Pigment M-1-3476B (orange colour containing sunset yellow FCF [E110], titanium dioxide [E171], hypromellose [E464] and erythrosine lake [E127])

Not applicable.

3 years.

Do not store above 25°C.

Cartons containing PVC blister packs of 6, 28, 56, 100 or 112 tablets.

Not all pack sizes may be marketed.

No special requirements.

Almirall S.A.

Ronda General Mitre, 151

08022 Barcelona

Spain

PA 968/5/2

Date of first authorisation: 24^th May 1983

Date of last renewal: 25^th August 2007

1 August 2010