This information is intended for use by health professionals

1. Name of the medicinal product

Methocarbamol Aristo 750 mg Tablets

2. Qualitative and quantitative composition

Each tablet contains 750 mg methocarbamol.

For the full list of excipients, see section 6.1

3. Pharmaceutical form

Tablet

White, slightly convex, oblong tablets (19 mm x 8 mm)

4. Clinical particulars
4.1 Therapeutic indications

Symptomatic treatment of painful muscle tone, especially in the low back region (lumbago).

Methocarbamol is used in adults.

4.2 Posology and method of administration

Posology

Adults should take 1500 mg methocarbamol three times a day.

For initiation of treatment intake of 1500 mg methocarbamol four times a day is recommended. In the case of severe complaints up to 7500 mg methocarbamol may be administered per day.

The duration of administration depends on the symptoms induced by increased muscle tone, but should not exceed 30 days.

Elderly patients

Half the maximum dose or less may be sufficient to produce a therapeutic response.

Patients with hepatic impairment

In patients with chronic hepatic disease the elimination half-life may be prolonged. Therefore, consideration should be given to increasing the dose interval.

Paediatric population

The safety and efficacy of Methocarbamol Aristo in children aged to 12 years and adolescents have not been established.

Method of administration

Methocarbamol Aristo is for oral use.

The tablets should be taken with a sufficient amount of water.

4.3 Contraindications

- Hypersensitivity to the active substance or to any of the excipients listed in section 6.1,

- comatose or pre-comatose states,

- diseases of the central nervous system,

- Myasthenia gravis,

- predisposition for epilepsy

4.4 Special warnings and precautions for use

Methocarbamol should be used with special care in patients with impaired renal function and/or impaired liver function.

Patients should be advised that the intake of alcohol during the treatment with methocarbamol or a combination with other centrally acting agents can lead to an increase in effects.

Interactions with laboratory tests

The urine of some patients receiving methocarbamol has been reported to turn brown, black, blue or green when stored. Methocarbamol may cause colour interference in certain screening tests for hydroxyindolacetic acid (5-HIAA) and for vanillylmandelic acid (VMA).

Methocarbamol Aristo contains sodium

This medicine contains less than 1 mmol sodium (23 mg) per tablet, that is to say essentially 'sodium-free'.

4.5 Interaction with other medicinal products and other forms of interaction

In the case of the concomitant use of methocarbamol and centrally acting medicinal products such as barbiturates, opioids or appetite suppressants pharmacological effects may mutually be enhanced.

If alcohol is taken during treatment with methocarbamol, an increase in effect may occur.

The effects of anticholinergics, e.g. atropine and some psychotropic drugs may be potentiated by methocarbamol. Methocarbamol may decrease the effect of pyridostigmine bromide. Therefore, methocarbamol should not be used in patients who take pyridostigmine for the treatment of Myasthenia gravis.

4.6 Fertility, pregnancy and lactation

Pregnancy

There is no experience concerning the use of methocarbamol during pregnancy. Animal studies have not established the safe use of methocarbamol with regard to effects on pregnancy, embryonic/fetal development, parturition and postnatal development (see section 5.3). The potential risk for humans is not known.

Therefore, methocarbamol should not be used during pregnancy.

Breast-feeding

It is not known whether methocarbamol and/or its metabolites pass into human milk. Methocarbamol and/or its metabolites are excreted into the milk of lactating dogs. Therefore, methocarbamol should not be used by breast-feeding women.

Fertility

No data are available about the influence of Methocarbamol on the human fertility.

4.7 Effects on ability to drive and use machines

Methocarbamol may have an influence on the ability to drive and use machines due to possible undesirable effects.

4.8 Undesirable effects

The following undesirable effects have been reported in the context of treatment with methocarbamol and - as far as information on frequency is stated in the literature - are based on the following groups of frequency:

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)

not known

(frequency cannot be estimated from the available data)

Immune system disorders

Very rare: anaphylactic reaction

Metabolism and nutrition disorders

Very rare: anorexia

Psychiatric disorders

Very rare: restlessness, anxiety, confusion

Nervous system disorders

Rare: headache, dizziness, metallic taste

Very rare: syncope, nystagmus, drowsiness, tremor, convulsions

Not known: sleepiness

Eye disorders

Rare: conjunctivitis

Very rare: blurred vision

Cardiac disorders

Very rare: bradycardia

Vascular disorders

Rare: hypotonia

Very rare: hot flash

Respiratory, thoracic and mediastinal disorders

Rare: swelling of the nasal mucosa

Gastrointestinal disorders

Very rare: feeling sick, vomiting

Skin and subcutaneous tissue disorders

Rare: angioneurotic oedema, pruritus, skin rash, urticaria

Generaldisorders and administration site conditions

Rare: fever

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the yellow card scheme at: www.mhra.gov.uk/yellowcard or search for MHRA Yellow Card in the Google Play or Apple App Store.

4.9 Overdose

Limited information is available on the acute toxicity of methocarbamol. Overdose of methocarbamol is frequently in conjunction with alcohol or other CNS depressants and includes the following symptoms: nausea, drowsiness, blurred vision, hypotension, seizures and coma.

Following oral use of methocarbamol in doses of 22.5 g to 50 g by patients who intended to commit suicide, drowsiness was observed in two patients. Both patients recovered completely within 24 hours.

Treatment of intoxication comprises gastric lavage, symptomatic therapy and monitoring of vital functions.

The benefit of hemodialysis in the treatment of a methocarbamol overdose is not known.

5. Pharmacological properties
5.1 Pharmacodynamic properties

Pharmacotherapeutic group: muscle relaxants, centrally acting agents, carbamic acid esters

ATC code: M03BA03

Methocarbamol is a centrally acting muscle relaxant. Its myotonolytic effect is based on an inhibition of polysynaptic reflex conduction within the spinal cord and subcortical structures. The physiological tone and contractility of skeletal muscle as well as the motility of smooth muscle are not affected by methocarbamol in therapeutic doses which also has no impact on the motor end plate.

5.2 Pharmacokinetic properties

Resorption

After oral administration methocarbamol is absorbed rapidly and completely.

Distribution

The substance can be detected in blood already 10 minutes after intake. Peak plasma levels are achieved after 30 - 60 minutes. Plasma half-life in plasma amounts to approximately 2 hours.

Biotransformation and elimination

Methocarbamol and its two main metabolites are bound to glucuronic and to sulfuric acid and are eliminated nearly exclusively via the kidneys. About half of an applied dose is excreted into urine within 4 hours, only a small part of which is eliminated as unchanged methocarbamol.

Renal impairment

The clearance of methocarbamol in renally impaired patients on maintenance haemodialysis was reduced about 40% compared to a normal population, although the mean elimination half-life in these two groups was similar (1.2 versus 1.1 hours, respectively).

Hepatically impaired

In patients with cirrhosis secondary to alcohol abuse, the mean total clearance of methocarbamol was reduced approximately 70% compared to a normal population (11.9 L/hr), and the mean elimination half-life was extended to approximately 3.4 hours. The fraction of methocarbamol bound to plasma proteins was decreased to approximately 40 to 45% compared to 46 to 50% in an age and weight-matched normal population.

5.3 Preclinical safety data

The acute toxicity of methocarbamol is comparatively low. Signs of intoxication in animal studies are ataxia, catalepsy, convulsions and coma.

Studies on chronic toxicity have not been performed.

Studies in order to determine a potential toxicity on reproduction have not been performed.

In vitro and in vivo studies on genetic toxicity of methocarbamol did not reveal evidence of a mutagenic potential.

Long term studies for evaluation of a carcinogenic potential have not been performed.

6. Pharmaceutical particulars
6.1 List of excipients

Sodium starch glycolate (type A)

Magnesium stearate

Povidone K25

6.2 Incompatibilities

Not applicable.

6.3 Shelf life

3 years

6.4 Special precautions for storage

This medicinal product does not require any special storage conditions.

6.5 Nature and contents of container

PVC/PVDC/aluminium blister

Pack sizes: 20, 50 and 100 tablets

Not all pack sizes may be marketed.

6.6 Special precautions for disposal and other handling

No special requirements.

7. Marketing authorisation holder

Aristo Pharma GmbH

Wallenroder Str. 8-10

13435 Berlin

Germany

8. Marketing authorisation number(s)

PL 40546/0160

9. Date of first authorisation/renewal of the authorisation

Date of first authorisation: 18 August 2018

10. Date of revision of the text

08/01/2020