Information about Xylometazoline

Xylometazoline (Neo-Rinoleina®; Novorin®; Olynth®; Otriven®; Otrivin®; Otrivine®; Xymelin®) is a topical decongestant that is directly dosed into the nose, either as a spray or as drops.

Xylometazoline is marketed under the brand names Otrivine or Otrivin, with the standard adult dose being 0.1% w/v xylometazoline. The dose for children under 12 is 0.05%.

The drug works by constricting the blood vessels in the nose. The vasoconstriction means that there is less pressure in the capillaries and less water can filter out, thus less discharge is made. (If the colour of the nasal passage is observed, it is visibly paler after dosage.)

Xylometazoline is designed to mimic the molecular shape of adrenaline meaning that it binds to the same cell receptors adrenaline does. For this reason, it should not be used by people with high blood pressure, or other heart problems. (It acts mainly on alpha-adrenergic receptors.)

Unfortunately the vessels become resistant to the drug after prolonged dosing. The number of receptors decreases, and when the administration of the drug is ceased, chronic congestion can occur; this is called rhinitis medicamentosa, commonly referred to as rebound congestion. Moreover long-term overdosing can cause degenerative changes in nasal mucous membranes that pose another health problem.

Topical decongestants are decongestants applied directly to the nasal cavity. By applying them directly to the site of action, topical decongestants relieve nasal congestion while reducing the side effects associated with systemically-acting decongestants, such as high blood
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nose is a protuberance in vertebrates that houses the nostrils, or nares, which admit and expel air for respiration in conjunction with the mouth.

In most humans, it also houses the nosehairs, which catch airborne particles and prevent them from reaching the lungs.
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In biology percentage solutions are often preferred to molar ones. A 1% solution would have 1 g of solute dissolved in a final volume of 100 ml of solution. This would be labeled as a weight/volume [w/v] percentage solution.
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Vasoconstriction is a narrowing of the lumen of blood vessels.

Factors

Factors that trigger vasoconstriction are both of exogenous origin, i.e. medication, and as a response from the body itself.

Body mechanisms

Vasoconstriction is a procedure of the body to e.g.
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capillary is used to describe any very narrow tube or channel through which a fluid can pass. See capillary action for details.


Capillaries are the smallest of a body's blood vessels, measuring 5-10 μm, which connect arterioles and venules, and are
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Epinephrine (INN) (IPA: [ˌɛpɪˈnɛfrən]) or adrenaline (European Pharmacopoeia and BAN) (IPA: [əˈdrɛnələn]
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Blood pressure (strictly speaking: vascular pressure) refers to the force exerted by circulating blood on the walls of blood vessels, and constitutes one of the principal vital signs.
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heart is a muscular organ responsible for pumping blood through the blood vessels by repeated, rhythmic contractions, or a similar structure in the annelids, mollusks, and arthropods.
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adrenergic receptors (or adrenoceptors) are a class of G protein-coupled receptors that are targets of the catecholamines. Adrenergic receptors specifically bind their endogenous ligands, the catecholamines adrenaline and noradrenaline (called epinephrine and norepinephrine
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Rhinitis medicamentosa (or RM) is a condition of rebound nasal congestion brought on by extended use of topical decongestants (e.g. oxymetazoline, phenylephrine, and xylometazoline nasal sprays) that work by constricting blood vessels in the lining of the nose.
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The mucous membranes (or mucosae; singular: mucosa) are linings of mostly endodermal origin, covered in epithelium, and are involved in absorption and secretion. They line various body cavities that are exposed to the external environment and internal organs.
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A decongestant is a broad class of medications used to relieve nasal congestion. Generally, they work by reducing swelling of the mucous membranes in the nasal passages.

Mechanism

Most decongestants cause response from adrenoreceptor a1
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A section of the Anatomical Therapeutic Chemical Classification System.

R Respiratory system

R01A Decongestants and other nasal preparations for topical use

R01AA Sympathomimetics, plain

R01AA02 Cyclopentamine
R01AA03 Ephedrine

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Sympathomimetic drugs are substances that mimic the effects of the hormone epinephrine (adrenaline) and the hormone/neurotransmitter norepinephrine (noradrenaline). They all raise blood pressure and are all weak bases.
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Cyclopentamine is a stimulant drug structurally related to methamphetamine, wherein the aromatic phenyl ring is replaced with a cyclopentane ring. Due to its strong vasoconstricting properties, cyclopentamine is typically found in over-the-counter nasal decongestant swabs.
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Ephedrine (EPH) is a sympathomimetic amine similar in structure to the synthetic derivatives amphetamine and methamphetamine. Ephedrine is commonly used as a stimulant, appetite suppressant, concentration aid, decongestant and to treat hypotension associated with regional
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Phenylephrine or Neo-Synephrine is an α-adrenergic receptor agonist used primarily as a decongestant, as an agent to dilate the pupil and to increase blood pressure. Phenylephrine has recently been marketed as a substitute for pseudoephedrine, (e.g.
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Oxymetazoline is a topical decongestant used, in the form of Oxymetazoline hydrochloride, in products such as Nasivion, Vicks Sinex and Afrin. Oxymetazoline is generally available as a nasal spray.
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Tetrahydrozoline is a derivative of imidazoline, which is found in over-the-counter eye drops and nasal sprays. Other derivatives include naphazoline, oxymetazoline, and xylometazoline. Poisoning can result from an overdose.
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Naphazoline (in the hydrochloride form) is the common name for 2-(1-Naphthylmethyl)-2-imidazoline hydrochloride, It is a sympathomimetic agent with marked alpha adrenergic activity. It is a vasoconstrictor with a rapid action in reducing swelling when applied to mucous membrane.
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Tramazoline is a nasal preparation.


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Metizoline is a nasal preparation.


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Tuaminoheptane (or tuamine) is a nasal decongestant drug which is a sympathomimetic stimulant and vasoconstrictor.[1] However it can cause skin irritation,[2] which limits its usefulness as a nasal decongestant.
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Fenoxazoline is a nasal preparation.


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Tymazoline is a nasal preparation.


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Epinephrine (INN) (IPA: [ˌɛpɪˈnɛfrən]) or adrenaline (European Pharmacopoeia and BAN) (IPA: [əˈdrɛnələn]
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allergen.[1]

Sensitivities vary from one person to another and it is possible to be allergic to an extraordinary range of substances.

Types of allergies


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Cromoglicate (INN) (also referred to as cromolyn (USAN) or cromoglycate (former BAN)) is traditionally described as a mast cell stabilizer, and is commonly marketed as the sodium salt sodium cromoglicate.
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Levocabastine is a selective second-generation H1-receptor antagonist used for allergic conjunctivitis.

Levocabastine was discovered at Janssen Pharmaceutica in 1979.

References

  • Pipkorn U, Bende M, Hedner J, Hedner T.

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Azelastine is an antihistamine and mast cell stabilizer available as a nasal spray (Astelin®) for hay fever and as eye drops (Optivar®) for allergic conjunctivitis.

Side effects

Nasal spray


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