Topical Decongestants
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Topical Decongestants
Topical decongestants are decongestants applied directly to the nasal cavity. Their effectiveness by themselves in the common cold appears to have a small benefit in adults. Topical decongestants should only be used by patients for a maximum of 5–7 days in a row, because rebound congestion may occur in the form of rhinitis medicamentosa. When used in adults for a short period of time side effects appear to be few. Mechanism of action Topical decongestants are vasoconstrictors, and work by constricting the blood vessels within the nasal cavity. Examples * Ephedrine * Levomethamphetamine * Naphazoline * Oxymetazoline * Phenylephrine * Pseudoephedrine * Tramazoline * Xylometazoline See also * Decongestant * Nasal irrigation * Nasal spray Nasal sprays are used to deliver medications locally in the nasal cavities or systemically. They are used locally for conditions such as nasal congestion and allergic rhinitis. In some situations, the nasal delivery route is preferred for ...
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Decongestant
A decongestant, or nasal decongestant, is a type of pharmaceutical drug that is used to relieve nasal congestion in the upper respiratory tract. The active ingredient in most decongestants is either pseudoephedrine or phenylephrine (the latter of which has disputed effectiveness). Intranasal corticosteroids can also be used as decongestants and antihistamines can be used to alleviate runny nose, nasal itch, and sneezing. Topical decongestants on topical application as dilute solution (0.05–0.1%) produce local vasoconstriction. Regular use of decongestants for long periods should be avoided because mucosal ciliary function is impaired: atrophic rhinitis and anosmia (loss of the sense of smell) can occur due to persistent vasoconstriction. Decongestants can be absorbed from the nose via an inhaler and produce systemic effects, mainly central nervous system stimulation and rise in blood pressure. These drugs should be used cautiously in hypertensives and in those receivin ...
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Nasal Cavity
The nasal cavity is a large, air-filled space above and behind the human nose, nose in the middle of the face. The nasal septum divides the cavity into two cavities, also known as fossae. Each cavity is the continuation of one of the two nostrils. The nasal cavity is the uppermost part of the respiratory system and provides the nasal passage for inhaled air from the nostrils to the nasopharynx and rest of the respiratory tract. The paranasal sinuses surround and drain into the nasal cavity. Structure The term "nasal cavity" can refer to each of the two cavities of the nose, or to the two sides combined. The lateral wall of each nasal cavity mainly consists of the maxilla. However, there is a deficiency that is compensated for by the perpendicular plate of the palatine bone, the medial pterygoid plate, the labyrinth of ethmoid and the inferior concha. The paranasal sinuses are connected to the nasal cavity through small orifices called Sinus ostium, ostia. Most of these ostia ...
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Common Cold
The common cold or the cold is a viral infectious disease of the upper respiratory tract that primarily affects the respiratory mucosa of the nose, throat, sinuses, and larynx. Signs and symptoms may appear fewer than two days after exposure to the virus. These may include coughing, sore throat, runny nose, sneezing, headache, and fever. People usually recover in seven to ten days, but some symptoms may last up to three weeks. Occasionally, those with other health problems may develop pneumonia. Well over 200 virus strains are implicated in causing the common cold, with rhinoviruses, coronaviruses, adenoviruses and enteroviruses being the most common. They spread through the air during close contact with infected people or indirectly through contact with objects in the environment, followed by transfer to the mouth or nose. Risk factors include going to child care facilities, not sleeping well, and psychological stress. The symptoms are mostly due to the body's i ...
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Rhinitis Medicamentosa
Rhinitis medicamentosa (or RM) is a condition of rebound nasal congestion suspected to be brought on by extended use of topical decongestants (e.g., oxymetazoline, phenylephrine, xylometazoline, and naphazoline nasal sprays) and certain oral medications (e.g., sympathomimetic amines and various 2-imidazolines) that constrict blood vessels in the lining of the nose, although evidence has been contradictory. Presentation The characteristic presentation of RM involves nasal congestion without rhinorrhea, postnasal drip, or sneezing following several days of decongestant use. This condition typically occurs after 5–7 days of use of topical decongestants. Patients often try increasing both the dose and the frequency of nasal sprays upon the onset of RM, worsening the condition. The swelling of the nasal passages caused by rebound congestion may eventually result in permanent turbinate hypertrophy, which may block nasal breathing until surgically removed. Causes Common issues th ...
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Vasoconstrictor
Vasoconstriction is the narrowing of the blood vessels resulting from contraction of the muscular wall of the vessels, in particular the large arteries and small arterioles. The process is the opposite of vasodilation, the widening of blood vessels. The process is particularly important in controlling hemorrhage and reducing acute blood loss. When blood vessels constrict, the flow of blood is restricted or decreased, thus retaining body heat or increasing vascular resistance. This makes the skin turn paler because less blood reaches the surface, reducing the radiation of heat. On a larger level, vasoconstriction is one mechanism by which the body regulates and maintains mean arterial pressure. Medications causing vasoconstriction, also known as vasoconstrictors, are one type of medicine used to raise blood pressure. Generalized vasoconstriction usually results in an increase in systemic blood pressure, but it may also occur in specific tissues, causing a localized reduction in ...
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Ephedrine
Ephedrine is a central nervous system (CNS) stimulant that is often used to prevent low blood pressure during anesthesia. It has also been used for asthma, narcolepsy, and obesity but is not the preferred treatment. It is of unclear benefit in nasal congestion. It can be taken by mouth or by injection into a muscle, vein, or just under the skin. Onset with intravenous use is fast, while injection into a muscle can take 20 minutes, and by mouth can take an hour for effect. When given by injection it lasts about an hour and when taken by mouth it can last up to four hours. Common side effects include trouble sleeping, anxiety, headache, hallucinations, high blood pressure, fast heart rate, loss of appetite, and inability to urinate. Serious side effects include stroke and heart attack. While likely safe in pregnancy, its use in this population is poorly studied. Use during breastfeeding is not recommended. Ephedrine works by increasing the activity of the α and β adrenergic r ...
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Levomethamphetamine
LevomethamphetamineOther names include l-methamphetamine, levodesoxyephedrine, l-desoxyephedrine, levmetamfetamine ( INN and USAN). is the levorotatory (L-enantiomer) form of methamphetamine. Levomethamphetamine is a sympathomimetic vasoconstrictor that is the active ingredient in some over-the-counter (OTC) nasal decongestant inhalers in the United States. Pharmacology Levomethamphetamine crosses the blood-brain-barrier and acts as a TAAR1 agonist, functioning as a selective norepinephrine releasing agent (with few or no effects on the release of dopamine), so it affects the central nervous system, although its effects are qualitatively distinct relative to those of dextromethamphetamine. It does not possess the potential for euphoria or addiction that dextromethamphetamine possesses. Among its physiological effects are the vasoconstriction that makes it useful for nasal decongestion. The elimination half-life of levomethamphetamine is between 13.3 and 15 hours, whereas dext ...
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Naphazoline
Naphazoline is a medicine used as a decongestant, and a vasoconstrictor added to eye drops to relieve red eye. It has a rapid action in reducing swelling when applied to mucous membranes. It is a sympathomimetic agent with marked alpha adrenergic activity that acts on alpha-receptors in the arterioles of the conjunctiva to produce constriction, resulting in decreased congestion. It was patented in 1934 and came into medical use in 1942. Medical uses Nasal administration Nasal decongestant. Ophthalmic drug administration Eye drops (brand names Clear Eyes, and Cleari) narrowing swollen blood vessels ( ophthalmic arteries, and ophthalmic veins) to relieve red eye. Temporary red eye can safely be treated when the cause of the redness is established (eg cannabis induces corneal vasodilation) nsufficient Bibliography However, continuous use is not recommended without knowing an underlying condition. Side effects A few warnings and contraindications that apply to all naphazol ...
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Oxymetazoline
Oxymetazoline, sold under the brand name Afrin among others, is a topical decongestant and vasoconstrictor medication. It is available over-the-counter as a nasal spray to treat nasal congestion and nosebleeds, as eyedrops to treat eye redness due to minor irritation, and (in the United States) as a prescription topical cream to treat persistent facial redness due to rosacea in adults. Its effects begin within minutes and last for up to 6 hours. Intranasal use for longer than three days may cause congestion to recur or worsen, resulting in physical dependence. Oxymetazoline is a derivative of imidazole.PubChem nternet Bethesda (MD): National Library of Medicine (US), National Center for Biotechnology Information; 2004-. PubChem Compound Summary for CID 4636, Oxymetazoline; ited 2021 Apr. 18 Available from: https://pubchem.ncbi.nlm.nih.gov/compound/Oxymetazoline It was developed from xylometazoline at E. Merck Darmstadt by Wolfgang Fruhstorfer and Helmut Müller-Calgan in ...
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Phenylephrine
Phenylephrine is a medication primarily used as a decongestant, to dilate the pupil, to increase blood pressure, and to relieve hemorrhoids. In the United States, it was previously used orally as an over-the-counter decongestant to relieve nasal congestion due to sinusitis, but this use was discontinued in 2007. As of 2022, its use as a nasal decongestant in other applications still persists. Phenylephrine can be taken by mouth, as a nasal spray, given by injection into a vein or muscle, or applied to the skin. Common side effects when taken by mouth or injected include nausea, vomiting, headache, and anxiety. Use on hemorrhoids is generally well tolerated. Severe side effects may include a slow heart rate, intestinal ischemia, chest pain, kidney failure, and tissue death at the site of injection. It is unclear if use during pregnancy or breastfeeding is safe. Phenylephrine is a selective α1-adrenergic receptor agonist which results in the constriction of both arteries and ...
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Pseudoephedrine
Pseudoephedrine (PSE) is a sympathomimetic drug of the phenethylamine and amphetamine chemical classes. It may be used as a nasal/sinus decongestant, as a stimulant, or as a wakefulness-promoting agent in higher doses. It was first characterized in 1889 by the German chemists Ladenburg and Oelschlägel, who used a sample that had been isolated from '' Ephedra vulgaris'' by the Merck pharmaceutical corporation of Darmstadt, Germany. The salts pseudoephedrine hydrochloride and pseudoephedrine sulfate are found in many over-the-counter preparations, either as a single ingredient or (more commonly) in a fixed-dose combination with one or more additional active ingredients such as antihistamines, guaifenesin, dextromethorphan, paracetamol (acetaminophen) or an NSAID (such as aspirin or ibuprofen). Medical uses Pseudoephedrine is a stimulant, but it is well known for shrinking swollen nasal mucous membranes, so it is often used as a decongestant. It reduces tissue hyp ...
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Tramazoline
Tramazoline is a chemical that is used in the form of tramazoline hydrochloride in nasal decongestant preparations. It is an α-adrenergic receptor agonist that inhibits secretion of nasal mucus. It was patented in 1961 and came into medical use in 1962. Brand names *Australia ** Spray-Tish ** Rhinaspray *Austria ** Rhinorix *Belgium ** Rhinospray *Bulgaria ** Muconasal Plus *Czech Republic ** Muconasal Plus *Germany ** Biciron ** Ellatun ** Rhinospray *Hungary ** Rhinospray Plus *Italy ** Rinogutt ** Fexallegra nasale (Tramazoline + Chlorpheniramine Chlorphenamine (CP, CPM), also known as chlorpheniramine, is an antihistamine used to treat the symptoms of allergic conditions such as allergic rhinitis (hay fever). It is taken by mouth. The medication takes effect within two hours and lasts ..., 1 mg/ml + 3.55 mg/ml) *Portugal ** Rhinospray *Romania ** Muconasal Plus (older) ** Muconasal (newer) *Russia ** Adrianol (tramazoline + phenylephrine) ** Lasolvan ...
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