1. Name Of The Medicinal Product
Covonia Night Time Formula.
2. Qualitative And Quantitative Composition
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Excipients : Each 5ml contains Liquid Maltitol 1.125g, Ethanol (alcohol) 7.3 Vol %
For full list of excipients see section 6.1
3. Pharmaceutical Form
Oral Solution.
4. Clinical Particulars
4.1 Therapeutic Indications
For the night time symptomatic relief of unproductive cough and congestive symptoms associated with colds.
4.2 Posology And Method Of Administration
Posology
Adults, the Elderly and Children over 12 years
3 X 5ml spoonfuls at bedtime. Repeat after 6 hours if required
4.3 Contraindications
Contraindicated in known hypersensitivity to any of the ingredients. Contraindicated in persons under treatment with monoamine oxidase inhibitors or within 2 weeks of discontinuation of MAOI use.
Dextromethorphan, in common with other centrally acting antitussive agents, should not be given to patients in, or at risk of developing, respiratory failure.
Covonia Night Time Formula should not be used in liver dysfunction. It should not be administered to patients where cough is associated with asthma or patients with productive cough.
4.4 Special Warnings And Precautions For Use
Precautions for use
Because of their antimuscarinic properties antihistamines should be used with care in conditions such as closed angle glaucoma, urinary retention, prostatic hyperplasia or pyeloduodenal obstruction. Caution should also be exercised in patients with epilepsy or severe cardiovascular disorders. Caution is needed for the use of dextromethorphan in patients with a history of asthma.
Patients with rare hereditary problems of fructose intolerance should not take this medicine.
It also contains 7.3vol% ethanol (alcohol), i.e. up to 870mg per dose, equivalent to 22ml of beer or 9ml of wine per dose.
Harmful if suffering from alcoholism.
Special warnings
If symptoms persist consult your doctor.
Keep out of the reach and sight of children.
Do not exceed the stated dose.
Causes drowsiness which may continue the next day. If affected to not drive or operate machinery.
Avoid alcoholic drink.
4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction
Dextromethorphan should not be used in persons under treatment with monoamine oxidase inhibitors or within 2 weeks of discontinuation of MAOI use in view of the potential risk of a severe or fatal interaction. Cimetidine inhibits the metabolism of opioid analgesics.
Diphenhydramine has additive sedative effects with alcohol and other CNS depressants. It may also have additive antimuscarinic effects with antimuscarinic drugs.
4.6 Pregnancy And Lactation
Although dextromethorphan and diphenhydramine have been in widespread use for many years, insufficient data are available on their use during pregnancy. Use during pregnancy is inadvisable unless there is a clear need. Caution should, therefore, be exercised by balancing the potential benefits of treatment against any possible hazards.
It is not known if dextromethorphan or its metabolites are excreted in human breast milk. Diphenhydramine is excreted in breast milk but the amount has not been quantified. Covonia Night Time Formula is, therefore, best avoided during breast feeding.
4.7 Effects On Ability To Drive And Use Machines
Diphenhydramine may cause drowsiness, persons so affected should be advised not to drive or to operate machinery.
4.8 Undesirable Effects
Side-effects are uncommon with dextromethorphan. Rarely, drowsiness, nausea, vomiting, dizziness and gastro-intestinal disturbances may occur.
The most common effects of diphenhydramine are drowsiness and a lowered ability to concentrate. Other effects include dizziness, nausea, nervousness, ataxia, abnormal vision, tremor and vomiting. Antimuscarinic effects may include dry mouth, thickened mucous secretions, palpitations and urinary tract dysfunction. Administration of antihistamines has also been associated with rash, angioedema, convulsions and paresthesias.
4.9 Overdose
Acute overdose of dextromethorphan does not usually result in serious signs and symptoms unless very large amounts have been ingested. Signs and symptoms of substantial overdose may include nausea and vomiting, CNS disturbances (hyperexcitability, irritability, mental confusion, lethargy, somnolence, ataxia, auditory and visual hallucinations), nystagmus and respiratory depression.
Mild cases of diphenhydramine overdose are mainly characterised by prominent antimuscarinic effects including dry mouth, headache, nausea, tachycardia and urinary retention. Larger doses produce depression or stimulation of the CNS. In small children, the stimulatory effects predominate and clinical features include hallucinations and convulsions. Adults usually develop drowsiness first, then convulse and lapse into coma at later stage. Fever and flushing is seen in children but is uncommon in adults.
Gastric lavage should be used if indicated. Naloxone has been used successfully as a specific antagonist to dextromethorphan toxicity in children. Convulsions can be controlled with diazepam. Other treatment is supportive and symptomatic and may include artificial respiration, external cooling for hyperpyrexia and intravenous fluids.
5. Pharmacological Properties
5.1 Pharmacodynamic Properties
ATC Code: RO5 DA – Opium Alkaloids and Derivatives
Dextromethorphan
Dextromethorphan is a non-opioid, centrally acting cough suppressant. It raises the threshold for the cough reflex in the medulla oblongata. In therapeutic doses, it has no significant analgesic, respiratory depressant, euphoriant or dependence-producing properties. It does not inhibit ciliary function.
Diphenhydramine
Diphenhydramine is an ethanolamine H1 histamine receptor antagonist. It possesses antitussive, sedative, antimuscarinic and antiemetic properties. Antihistamines, like diphenhydramine, are useful for controlling nasal itching, sneezing and rhinorrhoea but are less effective for the relief of nasal congestion.
5.2 Pharmacokinetic Properties
Dextromethorphan
Dextromethorphan is rapidly absorbed from the gastrointestinal tract following oral administration. It is subject to extensive presystematic metabolism resulting in very low peak plasma concentrations of 1.8ng/ml within 2.5 hours of an oral dose. Peak concentrations of the main metabolite, dextrophan occur 1-2 hours after ingestion. The terminal plasma elimination half-life of dextrophan is about three hours.
It is not known if dextromethorphan or dextrophan is excreted into breast milk or crosses the placenta.
Dextromethorphan is extensively metabolised in the liver. It is mainly metabolised to dextrophan by O-demethylation involving the cytochrome P45011D6 isozyme, which is then conjugated by UDP-glucuronosyl transferases. Up to 9% of individuals have been found to be poor metabolisers and the half-life of dextromethorphan may be extremely prolonged in these people.
Less than 1% of the dose of dextromethorphan is excreted in the faeces. Urinary excretion of parent drug and metabolites accounts for up to 50% of the ingested dose over 24 hours.
Diphenhydramine
Diphenhydrainine is well absorbed from the gastrointestinal tract but its availability varies between 26 and 60% due to first pass metabolism. Peak plasma concentrations are achieved about 1 to 4 hours after oral administration. The plasma elimination half-life is 3.3 hours.
Diphenhydramine is widely distributed throughout the body including the CNS. It crosses the placenta and has been detected in breast milk. It is highly (85-98%) bound to plasma proteins.
Orientals have lower plasma levels, lower protein binding and a higher volume of distribution and higher plasma clearance, but not half-life, than Caucasians.
Diphenhydramine is extensively metabolised mainly in the liver. It is N-demethylated to monodesmethyldiphenhydramine and didesmethyldiphenhydramine. The resultant primary amine is oxidatively deaminated to yield the carboxylic acid, diphenylmethoxy acetic acid which may be conjugated with glutamine or glycine.
Diphenhydramine is excreted mainly in the urine with very little excreted as unchanged drug.
5.3 Preclinical Safety Data
Dextromethorphan
A 13 weeks dietary study in rats has shown no evidence of toxicity at the 0.1mg/kg dextromethorphan level. Dextromethorphan has been reported to have no mutagenic potential in two species and no effect on perinatal or postnatal mortality in high doses.
Diphenhydramine
In the rat, administration of 12mg/kg i.p. diphenhydramine hydrochloride has been reported to produce foetal mortality and mortality in the offspring up to the tenth day after birth. Doses up to 20 and 25 times the human dose (on a mg/kg basis) exert no teratogenic effects in rats and rabbits.
There is no evidence for diphenydramine being mutagenic or carcinogenic in man.
6. Pharmaceutical Particulars
6.1 List Of Excipients
Sodium Benzoate
Ethanol (96%)
Hydroxyethylcellulose. (Natrosol G PH).
Povidone K30.
Glycerol.
Liquid Sorbitol Non-Crystallising.
Liquid Maltitol
Saccharin Sodium.
Capsicum Tincture.
Menthol.
Peppermint Oil.
Anise Oil.
Citric Acid Monohydrate.
Macrogol Cetostearyl Ether
Caramel.
Blackcurrant Flavour 1122267 – containing propylene glycol.
6.2 Incompatibilities
None.
6.3 Shelf Life
36 months.
6.4 Special Precautions For Storage
Store below 25°C. Protect from light.
6.5 Nature And Contents Of Container
150ml amber soda glass bottle with 28mm tamper evident child resistant closure with EPE/ Saranex liner.
6.6 Special Precautions For Disposal And Other Handling
Not applicable.
7. Marketing Authorisation Holder
Thornton & Ross Ltd.
Linthwaite Laboratories
Huddersfield
HD7 5QH.
8. Marketing Authorisation Number(S)
PL: 00240/0042
9. Date Of First Authorisation/Renewal Of The Authorisation
23.09.97
10. Date Of Revision Of The Text
04/05/2010
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