Klosterfrau taxofit® neo-angin® dolo-angin® neo-bronchol® sinu-panthol® nasic® Soledum® Aria Bedan® Laxacur® Valerian Cynara® Ameu® Kira® Kwai® Ginkyo® Sedonium® MedEctoin

Product Characteristics

1. Drug name
Nasic®
For adults and schoolchildren.

2. Prescription/pharmacy status
Pharmacy-only

3. Qualitative and quantitative composition

3.1 Substance- or indication category
Rhinological agent. Combination of an alpha-sympathicomimetic and a vitamin analogue for topical application to the nasal mucosa. Xylometazoline possesses vasoconstrictor properties and thus reduces mucosal swelling. Dexpanthenol is a derivative of the vitamin, pantothenic acid, that promotes would healing and protects the mucosa.

3.2 Pharmaceutically active ingredients
10 g of solution contains:
10 mg xylometazoline hydrochloride and
500 mg dexpanthenol.

One actuation of 0.1 ml solution (equivalent to 0.10 g) contains 0.1 mg xylometazoline hydrochloride and 5.0 mg dexpanthenol.

3.3 Other ingredients
2 mg benzalkonium chloride, potassium dihydrogen phosphate, sodium monohydrogen phosphate, purified water.

4. Indications
For the reduction of swelling of the nasal mucous membrane in common cold diseases and for supporting healing of skin and mucous membrane lesions, attacks of vasomotoric rhinitis and for treatment of the obstruction of nasal breathing after nasal surgery.

5. Contra-indications
This medication must not be used in the following cases:

• In patients who are hypersensitive to one of the ingredients of Nasic,
• In patients presenting with dry inflammation of the nasal mucosa (Rhinitis sicca),
• In young children under 6 years of age.
  

Due to its benzalkonium chloride content (used as a preservative), Nasic must not be administered to patients with known hypersensitivity to this substance.

This medication must only be given to the following patients after careful assessment of the benefit-risk ratio:

• Patients treated with monoamine oxidase inhibitors (MAO inhibitors) and other drugs with hypertensive potential.
• High intra-ocular pressure, especially narrow-angle glaucoma,
• Severe cardiovascular disorders (e.g. coronary heart disease, hypertension),
• Phaeochromocytoma
• Metabolic disorders (e.g. hyperthyroidism, diabetes).
  

Administration during pregnancy and lactation:
Nasic should not be used during pregnancy due to the lack of relevant studies on the unborn child. Administration during lactation should be avoided as it has not yet been established whether the active ingredient, xylometazoline hydrochloride, diffuses into breast milk.

6. Side effects

Xylometazoline hydrochloride:
Respiratory tract:
Minor transient irritation (burning or dryness of the nasal mucosa) may occur, especially in sensitive patients.

There have been isolated reports of marked mucosal swelling (reactive hyperaemia) once the effect of the medication begins to wane.

Prolonged or frequent use and high dose levels of xylometazoline hydrochloride can lead intranasally to burning or dryness of the mucosa as well as to reactive congestion with Rhinitis medicamentosa. This effect may be apparent after as little as 5 days’ treatment and may trigger permanent mucosal damage with crust formation (Rhinitis sicca).

Nervous system:
There have been occasional or isolated reports of headache, insomnia and fatigue.

Cardiovascular system:
Systemic sympathicomimetic effects such as palpitations, rapid pulse or a rise in blood pressure levels have rarely or occasionally been observed followint topical intranasal application.

Effects on drivers and machine operators:
Systemic effects involving the cardiovascular or central-nervous systems cannot be ruled out following long-term application or administration of high dose levels of Nasic.
In such cases, the ability to drive or operate machinery may be adversely affected.

Dexpanthenol:
Intolerance reactions have been reported in isolated cases.

7. Interactions with other drugs
Xylometazoline hydrochloride:
Concomitant administration of tranylcypromine mono-amine oxidase inhibitors or tricyclic antidepressants may cause a rise in blood pressure levels due to the cardiovascular effects of these substances.

Dexpanthenol:
None reported to date.

8. Warnings
None.

9. Major incompatibilities
None known.

10. Single and daily dosing
Adults and schoolchildren: one actuation of Nasic in each nostril up to 3 times a day. Dosing will depend on individual sensitivity and clinical efficacy.

11. Method and duration of administration
Nasic should not be used for more than 7 days due to the lack of data relating to prolonged application.
The duration of treatment in children should be discussed with the physician.

The bottle should be held upright and the medication sprayed into the nostrils. The patient should inhale gently through the nose as the product is being sprayed.

12. Emergency measures, symptoms and antidotes
Xylometazoline hydrochloride:
The following symptoms may appear following overdose or inadvertent oral administration:
Mydriasis, nausea, vomiting, cyanosis, fever, cramps, tachycardia, cardiac arrhythmia, circulatory collapse, cardiac arrest, hypertension, pulmonary oedema, respiratory disorders and mental disorders.

The following may also occur under certain circumstances: inhibition of CNS functions accompanied by drowsiness, a fall in body temperature, bradycardia, hypotension similar to shock, apnoea and coma.

Therapeutic measures in the event of overdosing:
Give medicinal charcoal, gastric lavage or oxygen therapy. Administration of 5 mg phentolamine in saline solution as a slow i.v. infusion or 100 mg vasopressors is contra-indicated. Lower temperature and administer anticonvulsive therapy if required.

Dexpanthenol:
Pantothenic acid and its derivatives such as dexpanthenol are only very slightly toxic. No measures are required in the event of overdosing.

13. Pharmacological and toxicological properties, pharmacokinetics and bioavailability provided that these data are of therapeutic relevance

13.1 Pharmacological properties
Xylometazoline hydrochloride:
Xylometazoline hydrochloride, an imidazole derivative, is an alpha-adrenergic sympathicomimetic agent. It possesses vasoconstrictor properties and reduces mucosal swelling. The onset of action is usually observed within 5 – 10 minutes and is evident from easier nasal breathing due to diminished mucosal swelling and improved secretion flow.

Dexpanthenol:
Dexpanthenol (D-(+)-panthothenyl alcohol) is the alcoholic analogue of pantothenic acid and, via intermediate conversion, possesses the same biological efficacy as pantothenic acid. It is bound to the dextrorotatory D-configuration. Panthothenic acid and its salts are water-soluble vitamins which are involved in numerous metabolic processes as coenzyme A, e.g. the promotion of protein- and corticoid synthesis and antibody production. Coenzyme A is also involved, amongst other things, in the formation of lipids, via which skin fats fulfil an important protective function, and in the acetylation of aminosugars that help to form various mucopolysaccharides.
Dexpanthenol promotes wound healing and protects the epithelium.
A trophic effect on the skin was observed in dexpanthenol-deficient rats following administration of dexpanthenol.
Dexpanthenol/panthenol can off-set the high pantothenic acid requirements of damaged skin or mucosa when applied externally.

13.2 Toxicological properties

a) Acute toxicity

Xylometazoline hydrochloride:
Acute toxicity studies were carried out in various animal species at different rates of application. Cardinal symptoms included cardiac arrhythmias, tremor, unrest, tonic-clonic spasms, hyperreflexia, dyspnoea and ataxia.

Dexpanthenol:
Pantothenic acid and its derivatives such as dexpanthenol are only very slightly toxic. Acute oral LD50 values of 6.25 g/kg body weight and 3.0 g/kg bodyweight were recorded for dexpanthenol/panthenol in mice and rabbits respectively.

b) Subchronic and chronic toxicity

Xylometazoline hydrochloride:

Studies involving repeated oral dosing to rats (6, 20 and 60 mg/kg/day) and dogs (1, 3 and 10 mg/kg/day) were carried out over a three-month period. Mortality, diminished feed intake, reduced body growth and, following administration of 60 mg/kg/day, slightly depleted blood sugar levels were observed in the rats in all dosing groups. Pathological changes indicated high blood pressure and loss of elasticity of the vascular intima. Only surviving animals in the 6 mg/kg/day dosing group did not present with any pathological changes.

Changes in clinical-chemical parameters (GPT, CPK, LDH) and in ECG tracings were recorded in dogs in all dosing groups from administration of 3 mg/kg/day and above. Mortalities and weight loss were also observed. Pathological changes to the heart, kidneys, liver and gastro-intestinal tract were observed in the highest dose group. Dose-dependent functional and morphological changes were mainly attributed to persistent vasoconstriction. No animal data are available from studies of the chronic toxicity of xylometazoline hydrochloride.

Mutagenic and tumorigenic potential

Xylometazoline hydrochloride:
Mutagenicity studies involving the Ames test and murine micro-nucleus test proved negative.

No long-term studies have been carried out to determine the tumorigenic potential of xylometazoline.

Dexpanthenol:
There is no evidence of mutagenic or carcinogenic effects.

d) Reproduction toxicity

Xylometazoline hydrochloride:
The reproduction toxicity of xylometazoline hydrochloride has not been adequately investigated. Reduced foetal weight (intrauterine growth retardation) has been observed in rats exposed to this substance during part of the organ growth phase. A contraction-inducing effect has been reported following i.v. injection in laboratory animal studies carried out in guinea-pigs and rabbits.

There is insufficient data regarding the use of this substance during pregnancy and lactation. A study involving 207 pregnant women who may have been exposed to this substance during the first trimester of pregnancy did not indicate any rise in the incidence of deformity (5/207). No studies have been carried out to determine whether or not the substance diffuses into breast milk.

Dexpanthenol:
No information regarding teratogenic effects is available.

13.3 Pharmacokinetics

Xylometazoline hydrochloride:

The quantity absorbed following intranasal application is sometimes adequate to trigger systemic effects, e.g. affecting the central nervous and cardiovascular systems.
No data from human pharmacokinetic studies are available.

Dexpanthenol:
Dexpanthenol is absorbed through the skin and oxidised enzymatically into pantothenic acid in the body and skin. The vitamin is transported in protein-bound form in the plasma. Panthothenic acid is incorporated as a vital component of coenzyme A and can be found throughout the body. More precise studies on skin and mucosal metabolism have not been carried out. Between 60 and 70% of an orally administered dose are eliminated in the urine and 30 to 40% in the faeces.

14. Other information

Reactive hyperaemia of the nasal mucous may occur especially following prolonged administration of and overdosing with sympathicomimetic agents to alleviate mucosal swelling.

This rebound effect causes the airways to constrict so that the patient repeatedly used the medication, resulting in long-term use.

The sequelae range from chronic swelling (Rhinitis medicamentosa) to atrophy of the nasal mucosa (ozena).

In milder cases, the sympathicomimetic agent can be administered to just one nostril and, once the symptoms have waned, to the other nostril in order at least to allow the patient to breathe partly through the nose.

15. Shelf life

The product has a shelf life of 3 years.

Use within 12 weeks of opening.

This medicine should not be used once the expiry date has elapsed.

16. Special storage conditions
None.

17. Pharmaceutical form and pack sizes
Solution: nasal spray
10 ml N1

18. Information last revised in:
August 1999

19. Name or firm and address of pharmaceutical company
Cassella-med
Gereonsmühlengasse 1
50670 Cologne
Tel.: (02 21) 12 01 57
Fax: (02 21) 16 52-5 13

Artesan Pharma
Wendlandstr. 1
29439 Luechow
Tel.: (0 58 41) 9 39 0
Fax: (0- 58 41) 9 39 –0 2 00

For general enquiries, please contact:
Bundesverband der Pharmazeutischen Industrie e.V.
Fachinfo Service (Summary of Product Characteristics)
Postfach 12 65
88322 Aulendorf

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