Topical Nasal Decongestants by Janet P. Engle, PharmD
Introduction Nasal congestion occurs secondary to engorgement of the nasal vasculature. It is a symptom associated with a variety of ailments including the common cold, allergies, and sinusitis. Topical and oral decongestants can be used to treat this condition. This review focuses on the treatment of nasal congestion with nonprescription topical decongestant products.
Actions and Indications
(I)
NrlR
The active ingredient in currently available topical decongestants is a sympathomimetic amine. Sympathomimetic amines used in topical nasal preparations include: phenylephrine, naphazoline, xylometazoline, tetrahydrozoline, oxymetazoline, ephedrine, levodesoxyephedrine, and propylhexedrine. These drugs stimulate alpha adrenergic receptors in vascular smooth muscle, which results in vasoconstriction. Vasoconstriction allows the engorged nasal membranes to shrink in size and thus decrease stuffiness. Topical nasal decongestants are applied directly to the nasal mucosa and are indicated for the treatment of nasal congestion due to colds, allergies, and sinusitis. Because topical nasal decongestants are applied directly to the congested nostril, the patient has almost immediate relief, whereas oral agents must be absorbed systemically before the patient feels any relief. Because the topical agents are not absorbed systemically when properly administered, patients taking them experience fewer side effects than do patients taking oral agents. However, topical nasal decongestants may cause rebound congestion, an adverse effect not associated with oral agents. Another agent that is often effective in the relief of nasal congestion is topical saline solution. Saline products restore moisture and relieve dry and inflamed nasal membranes resulting from colds, decreased humidity, nasal decongestant overuse, allergies, nosebleeds, and other irritations.
Dosage Forms Nasal decongestants are available in several dosage forms including sprays, drops, and inhalers. There are advantages Vol. NS32, No.5 May 19921409
AMERICAN PHARMACY
and disadvantages to each formulation. Spray: Sprays are preferred for older children and adults. Because these nasal decongestant formulations have a small particle size, the spray can disperse the medication over a larger area of the nasal mucosa thus resulting in better overall decongestion. A spray produces smaller droplets than the drop form. Drops: Generally, drops are not the most effective way to administer a topical decongestant. With drops, the drug is not dispersed as well as with a spray and the entire nasal mucosa may not be covered. If the drops are not adminis-
tered properly, they can more easily pass into the larynx. If swallowed, the drops can cause systemic effects. Drops, however, are the preferred dosage form in small children because of the small size of their nostrils. Jelly: An aqueous jelly dosage form of phenylephrine or ephedrine, not widely used, is no longer available. Inhaler: Desoxyephedrine and propylhexedrine are volatile sympathomimetic amines. These agents are incorporated onto a wick inside a plastic device and the fumes are inhaled. The inhalers are usually only effective for 2-3 months once opened. Loss of potency can occur sooner if
,;sPqsagp Parmi StrentJt" Av,ilable
Duration of Action ,
.c,;125%, 0.16%, 0.2%
short
Alconefrin 12, Neo-Synephrine, Nostril, St. Joseph Measured Dose
short
Va-Tro-Nol Nose Drops
short
Vicks Inhaler
short
Privine
drops; 0.25%, 0.5%, 1% qrops, spray
50 mg cyHndrical plastic'inh&ier
Product
Exam.ple.s
Afr!n, Dllistan Long .. Neo..S¥nephrlne 12 Ht>ut, NostriHa
long
~ctlng,.D'tJration,
not ap.>p.>lioat.>le
AMERICAN PHARMACY
SaHriex: NaSal, Ooean;Mist, .• AYR
May 1992/410 Vol. NS32, No.5
the cap is not replaced tightly after each use. The patient must also have sufficient airflow to distribute the drug throughout the nasal mucosa and gain an optimal effect from the inhaler.
Comparison of Available Agents The 50-plus nonprescription products contain various topical decongestants. Characteristics are described in Table 1. Short-acting products: Products classified as short acting have a duration of action of 4-6 hours or less. Ephedrine, naphazoline, phenylephrine, tetrahydrozoline, levodesoxyephedrine, and propylhexedrine are classified as shortacting agents and need to be dosed every 3-6 hours. Intennediate-acting products: Xylometazoline is a nasal decongestant with an intermediate duration of action. This product is effective for 8--10 hours after administration. Long-acting products: The only long-acting topical agent available is oxymetazoline. This agent can be dosed twice daily. Combination Products: Some combination products contain a topical decongestant and a topical antihistamine. Antihistamines, applied topically, have not been shown to have any benefit over the use of a decongestant alone when treating cold symptoms. Addition of an antihistamine increases the likelihood of a hypersensitivity reaction and therefore should not be recommended. 1
with oral decongestants are avoided. Occasionally patients may experience topical effects such as burning, stinging, irritation, sneeZing, and dryness when using these agents. 3 Naphazoline may cause mydriasis (pupil dilation) if absorbed systemically, and therefore is contraindicated in patients with glaucoma. Additionally, patients with cardiovascular disease should use the imidazoline class of sympathomimetic amines (e.g., oxymetazoline, tetrahydrozoline) sparingly.
Choice of Product When pharmacists help patients choose a topical nasal decongestant, several factors should be considered. First, pharmacists should ask the questions listed in Table 2. The patient's responses will determine the best topical agent for the patient. For instance, if the patient indicates that he or she has a history of hypertension and other cardiac problems, the pharmacist in consultation with the patient's physician should recommend a short-acting agent. Although adverse cardiac effects are rare with topical agents, use of a short-acting agent will allow any adverse effects to subside more quickly than a long-acting agent. For the patient who has a history of rebound congestion, proper education and selection of a long-acting product is the prudent choice. Rebound congestion is less likely to occur with the longer acting topical decongestants if they are used properly. 2 Although some patients may prefer the aromatic products that contain menthol, no evidence suggests that there is any additional therapeutic benefit to these products.
Adverse Effects/Prec8utions When topical nasal decongestants are used appropriately, side effects are uncommon. Because very little of the drug is absorbed systemically, adverse reactions that are associated Vol. NS32, No.5 May 1992/411
AMERICAN PHARMACY
Patients who are planning to participate in official athletic events should not use phenylephrine, ephedrine, desoxyephedrine, and propylhexedrine. These drugs are considered stimulants and therefore are banned and tested for in athletes by the U.S. Olympic Committee. Some patients who overuse topical nasal decongestants experience a rebound phenomenon (also termed rhinitis medicamentosa). Rebound congestion can occur if the topical agent is used longer than 3-5 days and is more common with a short-acting agent. When rebound occurs, the patient may note that the drug is not providing adequate relief or that more frequent dosing is needed. The patient may unwittingly increase the dose or frequency of use of the drug thus worsening the rebound and creating a vicious cycle. The nasal membranes become increasingly congested and edematous as the drug's action subsides. Pharmacists should counsel patients about this potential side effect and warn them not to overuse the topical agent. Treatment for rebound congestion is outlined in Table 3. Topical agents should only be used by pregnant women when absolutely necessary when the benefits outweigh the risk. Whether topical decongestants cause harm to the fetus is unknown. However, these drugs can be systemically absorbed, thus caution should be exercised when using a topical agent in a pregnant woman. It is also not known whether topical nasal decongestants are excreted in breast milk; caution should be exercised when administering these agents to a nursing woman. Saline products are a good choice for these women.
should not use any topical decongestant except saline without the advice of a physician. Furthermore, topical decongestants should never be used in children less than 6 months of age. Infants in this age group can only breathe through the nose. If rebound congestion occurs, obstructive apnea can occur. 5 If topical decongestants are necessary, normal saline nose drops should be recommended, not a sympathomimetic amine. Mentholated products should not be used in children less than two years old. Spasms of the glottis and asphyxiation have been reported in infants after application of topical menthol-containing products.
Product Considerations Although only eight sympathomimetic amines and saline products are available for use as topical decongestants , more than 50 nonprescription products are manufactured. The pharmacist should become familiar with a product from each class. It is important to note that products may have similar brand names yet contain different active ingredients (i.e., Neo-Synephrine versus Neo-Synephrine 12 hour; Nostril versus N6strilla). Pharmacists should also be familiar with the types of dosage forms that are available and the types of counseling that should be given with each. Patients who complain of nasal congestion should be asked the questions in Table 2. Once those questions are answered, pharmacists can make an appropriate recommendation. Janet P. Engle, PharmD, is assistant dean and clinical assistant professor ofpharmacy practice, University of Illinois at Chicago.
Patient Counseling Information To obtain optimal results from nasal decongestants, the patient should be instructed on the appropriate use of the dosage form chosen. Table 4 outlines specific counseling information for each dosage form. To prevent rebound congestion in patients, pharmacists should counsel patients not to use topical nasal decongestants for more than 3-5 days. The product should be used by only one family member to decrease the chances of cross contamination. The nose dropper or spray tip should not come in contact with the nostrils. If the tip touches the nose, it should be rinsed off immediately with hot water. If the product has turned brown or developed an odor, it should be discarded. Because most products do not allow visual inspection of the product, the patient should check the expiration date before using it. l ,2,4
This series is coordinated by the Section on Clinical/Pharmacotherapeutic Practice in the APhA Academy ofPharmacy Practice and Management. Dennis M. Williams, PharmD, is the editor. Reviewers for this article were Paul Munzenberger, PharmD, associate professor ofpharmacy practice, Wayne State University, Detroit, Mich.; William C. Drake, PharmD, clinical pharmaCist, Option Care, Mt. Clemens, Mich.; and Nicholas G. PopOVich, PhD, professor and associate head, School ofPharmacy and Pharmacal Sciences, Purdue University, West Lafayette, Ind.
References 1. Bryant BG, Lomardi TP. Cold and allergy products. In: Handbook of Nonprescription Drugs, 9th ed. Washington, DC: American Pharmaceutical Association, 1990;133-206. 2. Empey OW, Medder KT. Nasal decongestants. Drugs. 1981;21:438-43. 3. Kastrup EK, Olin BR, eds. Facts and Comparisons. St. Louis, Mo: JB lippincott Co, 1989; 184b. 4.
Pediatric Considerations Children should use topical nasal decongestants with caution. Use of naphazoline and ephedrine is not recommended for use in children less than six years old without the advice of a physician. Children less than two years old AMERICAN PHARMACY
USP Drug Information 1991, vol. lA, IB, Information for the Health Care Professional. Rockville, Md: US Pharmacopeial Convention Inc., 1991.
5. Serrano Murphy VA, Bubica G. General pediatric therapy. In: Applied Therapeutics, The Clinical Use of Drugs, 4th ed. Vancouver, Wash: Applied Therapeutics, Inc., 1988;183{}-1.
May 1992/412 Vol. NS32, No.5
Table 4
Patient Counseling Information on Nasal Decongestants Drops
• Blow your nose . • Squeeze rubber bulb on dropper and withdraw medication from bottle. • Recline on a bed and hang head over the side (preferred) OR tilt head back while standing or sitting. • Place drops into each nostril and gently tilt the head from side to side to distribute the drug. • Keep head tilted back for several minutes after instilling the drops. • Rinse the dropper with hot water.
Spray (Atomizer)
• Blow your nose. • Remove cap from spray container. • For best results, do not shake the squeeze bottle. • Administer one spray with head in upright position. • Sniff deeply while squeezing the bottle. • Wait 3-5 minutes and blow nose. • Administer another spray if necessary. • Rinse the spray tip with hot water taking care not to allow water to enter the bottle. • Replace cap.
Inhalers
• Blow your nose. • Warm inhaler in your hand to increase volatility of the medication. • Remove the protective cap. • Inhale medicated vapor in one nostril while closing off the other nostril, repeat in other nostril. • Wipe the inhaler clean after each use. • Replace cap immediately. • Note: Inhaler loses its potency after 2-3 months even though the aroma may linger.
Vol. NS32, No.5 May 1992/413
Metered Dose Pump (Spray)
• Blow your nose. • Remove the protective cap. • Prime the metered pump by depressing several ti m es (fer fi rst(Jise), pointing away from the face. • Hold the bottle with the thumb at the base and nozzle between first and second fingers.
figure 1
• Insert pump gently into the nose with the head upright. • Depress pump completely and sniff deeply. • Wait 3-5 minutes and then blow nose. • Administer another spray if necessary. !Pill Rinse the spray'if tip with hot water taking care not to allow w 'a ter to enter the bottle. • Replace cap.
AMERICAN PHARMACY
Introduction Nasal congestion occurs secondary to engorgement of the nasal vasculature. It is a symptom associated with a variety of ailments including the common cold, allergies, and sinusitis. Topical and oral decongestants can be used to treat this condition. This review focuses on the treatment of nasal congestion with nonprescription topical decongestant products.
Actions and Indications
(I)
NrlR
The active ingredient in currently available topical decongestants is a sympathomimetic amine. Sympathomimetic amines used in topical nasal preparations include: phenylephrine, naphazoline, xylometazoline, tetrahydrozoline, oxymetazoline, ephedrine, levodesoxyephedrine, and propylhexedrine. These drugs stimulate alpha adrenergic receptors in vascular smooth muscle, which results in vasoconstriction. Vasoconstriction allows the engorged nasal membranes to shrink in size and thus decrease stuffiness. Topical nasal decongestants are applied directly to the nasal mucosa and are indicated for the treatment of nasal congestion due to colds, allergies, and sinusitis. Because topical nasal decongestants are applied directly to the congested nostril, the patient has almost immediate relief, whereas oral agents must be absorbed systemically before the patient feels any relief. Because the topical agents are not absorbed systemically when properly administered, patients taking them experience fewer side effects than do patients taking oral agents. However, topical nasal decongestants may cause rebound congestion, an adverse effect not associated with oral agents. Another agent that is often effective in the relief of nasal congestion is topical saline solution. Saline products restore moisture and relieve dry and inflamed nasal membranes resulting from colds, decreased humidity, nasal decongestant overuse, allergies, nosebleeds, and other irritations.
Dosage Forms Nasal decongestants are available in several dosage forms including sprays, drops, and inhalers. There are advantages Vol. NS32, No.5 May 19921409
AMERICAN PHARMACY
and disadvantages to each formulation. Spray: Sprays are preferred for older children and adults. Because these nasal decongestant formulations have a small particle size, the spray can disperse the medication over a larger area of the nasal mucosa thus resulting in better overall decongestion. A spray produces smaller droplets than the drop form. Drops: Generally, drops are not the most effective way to administer a topical decongestant. With drops, the drug is not dispersed as well as with a spray and the entire nasal mucosa may not be covered. If the drops are not adminis-
tered properly, they can more easily pass into the larynx. If swallowed, the drops can cause systemic effects. Drops, however, are the preferred dosage form in small children because of the small size of their nostrils. Jelly: An aqueous jelly dosage form of phenylephrine or ephedrine, not widely used, is no longer available. Inhaler: Desoxyephedrine and propylhexedrine are volatile sympathomimetic amines. These agents are incorporated onto a wick inside a plastic device and the fumes are inhaled. The inhalers are usually only effective for 2-3 months once opened. Loss of potency can occur sooner if
,;sPqsagp Parmi StrentJt" Av,ilable
Duration of Action ,
.c,;125%, 0.16%, 0.2%
short
Alconefrin 12, Neo-Synephrine, Nostril, St. Joseph Measured Dose
short
Va-Tro-Nol Nose Drops
short
Vicks Inhaler
short
Privine
drops; 0.25%, 0.5%, 1% qrops, spray
50 mg cyHndrical plastic'inh&ier
Product
Exam.ple.s
Afr!n, Dllistan Long .. Neo..S¥nephrlne 12 Ht>ut, NostriHa
long
~ctlng,.D'tJration,
not ap.>p.>lioat.>le
AMERICAN PHARMACY
SaHriex: NaSal, Ooean;Mist, .• AYR
May 1992/410 Vol. NS32, No.5
the cap is not replaced tightly after each use. The patient must also have sufficient airflow to distribute the drug throughout the nasal mucosa and gain an optimal effect from the inhaler.
Comparison of Available Agents The 50-plus nonprescription products contain various topical decongestants. Characteristics are described in Table 1. Short-acting products: Products classified as short acting have a duration of action of 4-6 hours or less. Ephedrine, naphazoline, phenylephrine, tetrahydrozoline, levodesoxyephedrine, and propylhexedrine are classified as shortacting agents and need to be dosed every 3-6 hours. Intennediate-acting products: Xylometazoline is a nasal decongestant with an intermediate duration of action. This product is effective for 8--10 hours after administration. Long-acting products: The only long-acting topical agent available is oxymetazoline. This agent can be dosed twice daily. Combination Products: Some combination products contain a topical decongestant and a topical antihistamine. Antihistamines, applied topically, have not been shown to have any benefit over the use of a decongestant alone when treating cold symptoms. Addition of an antihistamine increases the likelihood of a hypersensitivity reaction and therefore should not be recommended. 1
with oral decongestants are avoided. Occasionally patients may experience topical effects such as burning, stinging, irritation, sneeZing, and dryness when using these agents. 3 Naphazoline may cause mydriasis (pupil dilation) if absorbed systemically, and therefore is contraindicated in patients with glaucoma. Additionally, patients with cardiovascular disease should use the imidazoline class of sympathomimetic amines (e.g., oxymetazoline, tetrahydrozoline) sparingly.
Choice of Product When pharmacists help patients choose a topical nasal decongestant, several factors should be considered. First, pharmacists should ask the questions listed in Table 2. The patient's responses will determine the best topical agent for the patient. For instance, if the patient indicates that he or she has a history of hypertension and other cardiac problems, the pharmacist in consultation with the patient's physician should recommend a short-acting agent. Although adverse cardiac effects are rare with topical agents, use of a short-acting agent will allow any adverse effects to subside more quickly than a long-acting agent. For the patient who has a history of rebound congestion, proper education and selection of a long-acting product is the prudent choice. Rebound congestion is less likely to occur with the longer acting topical decongestants if they are used properly. 2 Although some patients may prefer the aromatic products that contain menthol, no evidence suggests that there is any additional therapeutic benefit to these products.
Adverse Effects/Prec8utions When topical nasal decongestants are used appropriately, side effects are uncommon. Because very little of the drug is absorbed systemically, adverse reactions that are associated Vol. NS32, No.5 May 1992/411
AMERICAN PHARMACY
Patients who are planning to participate in official athletic events should not use phenylephrine, ephedrine, desoxyephedrine, and propylhexedrine. These drugs are considered stimulants and therefore are banned and tested for in athletes by the U.S. Olympic Committee. Some patients who overuse topical nasal decongestants experience a rebound phenomenon (also termed rhinitis medicamentosa). Rebound congestion can occur if the topical agent is used longer than 3-5 days and is more common with a short-acting agent. When rebound occurs, the patient may note that the drug is not providing adequate relief or that more frequent dosing is needed. The patient may unwittingly increase the dose or frequency of use of the drug thus worsening the rebound and creating a vicious cycle. The nasal membranes become increasingly congested and edematous as the drug's action subsides. Pharmacists should counsel patients about this potential side effect and warn them not to overuse the topical agent. Treatment for rebound congestion is outlined in Table 3. Topical agents should only be used by pregnant women when absolutely necessary when the benefits outweigh the risk. Whether topical decongestants cause harm to the fetus is unknown. However, these drugs can be systemically absorbed, thus caution should be exercised when using a topical agent in a pregnant woman. It is also not known whether topical nasal decongestants are excreted in breast milk; caution should be exercised when administering these agents to a nursing woman. Saline products are a good choice for these women.
should not use any topical decongestant except saline without the advice of a physician. Furthermore, topical decongestants should never be used in children less than 6 months of age. Infants in this age group can only breathe through the nose. If rebound congestion occurs, obstructive apnea can occur. 5 If topical decongestants are necessary, normal saline nose drops should be recommended, not a sympathomimetic amine. Mentholated products should not be used in children less than two years old. Spasms of the glottis and asphyxiation have been reported in infants after application of topical menthol-containing products.
Product Considerations Although only eight sympathomimetic amines and saline products are available for use as topical decongestants , more than 50 nonprescription products are manufactured. The pharmacist should become familiar with a product from each class. It is important to note that products may have similar brand names yet contain different active ingredients (i.e., Neo-Synephrine versus Neo-Synephrine 12 hour; Nostril versus N6strilla). Pharmacists should also be familiar with the types of dosage forms that are available and the types of counseling that should be given with each. Patients who complain of nasal congestion should be asked the questions in Table 2. Once those questions are answered, pharmacists can make an appropriate recommendation. Janet P. Engle, PharmD, is assistant dean and clinical assistant professor ofpharmacy practice, University of Illinois at Chicago.
Patient Counseling Information To obtain optimal results from nasal decongestants, the patient should be instructed on the appropriate use of the dosage form chosen. Table 4 outlines specific counseling information for each dosage form. To prevent rebound congestion in patients, pharmacists should counsel patients not to use topical nasal decongestants for more than 3-5 days. The product should be used by only one family member to decrease the chances of cross contamination. The nose dropper or spray tip should not come in contact with the nostrils. If the tip touches the nose, it should be rinsed off immediately with hot water. If the product has turned brown or developed an odor, it should be discarded. Because most products do not allow visual inspection of the product, the patient should check the expiration date before using it. l ,2,4
This series is coordinated by the Section on Clinical/Pharmacotherapeutic Practice in the APhA Academy ofPharmacy Practice and Management. Dennis M. Williams, PharmD, is the editor. Reviewers for this article were Paul Munzenberger, PharmD, associate professor ofpharmacy practice, Wayne State University, Detroit, Mich.; William C. Drake, PharmD, clinical pharmaCist, Option Care, Mt. Clemens, Mich.; and Nicholas G. PopOVich, PhD, professor and associate head, School ofPharmacy and Pharmacal Sciences, Purdue University, West Lafayette, Ind.
References 1. Bryant BG, Lomardi TP. Cold and allergy products. In: Handbook of Nonprescription Drugs, 9th ed. Washington, DC: American Pharmaceutical Association, 1990;133-206. 2. Empey OW, Medder KT. Nasal decongestants. Drugs. 1981;21:438-43. 3. Kastrup EK, Olin BR, eds. Facts and Comparisons. St. Louis, Mo: JB lippincott Co, 1989; 184b. 4.
Pediatric Considerations Children should use topical nasal decongestants with caution. Use of naphazoline and ephedrine is not recommended for use in children less than six years old without the advice of a physician. Children less than two years old AMERICAN PHARMACY
USP Drug Information 1991, vol. lA, IB, Information for the Health Care Professional. Rockville, Md: US Pharmacopeial Convention Inc., 1991.
5. Serrano Murphy VA, Bubica G. General pediatric therapy. In: Applied Therapeutics, The Clinical Use of Drugs, 4th ed. Vancouver, Wash: Applied Therapeutics, Inc., 1988;183{}-1.
May 1992/412 Vol. NS32, No.5
Table 4
Patient Counseling Information on Nasal Decongestants Drops
• Blow your nose . • Squeeze rubber bulb on dropper and withdraw medication from bottle. • Recline on a bed and hang head over the side (preferred) OR tilt head back while standing or sitting. • Place drops into each nostril and gently tilt the head from side to side to distribute the drug. • Keep head tilted back for several minutes after instilling the drops. • Rinse the dropper with hot water.
Spray (Atomizer)
• Blow your nose. • Remove cap from spray container. • For best results, do not shake the squeeze bottle. • Administer one spray with head in upright position. • Sniff deeply while squeezing the bottle. • Wait 3-5 minutes and blow nose. • Administer another spray if necessary. • Rinse the spray tip with hot water taking care not to allow water to enter the bottle. • Replace cap.
Inhalers
• Blow your nose. • Warm inhaler in your hand to increase volatility of the medication. • Remove the protective cap. • Inhale medicated vapor in one nostril while closing off the other nostril, repeat in other nostril. • Wipe the inhaler clean after each use. • Replace cap immediately. • Note: Inhaler loses its potency after 2-3 months even though the aroma may linger.
Vol. NS32, No.5 May 1992/413
Metered Dose Pump (Spray)
• Blow your nose. • Remove the protective cap. • Prime the metered pump by depressing several ti m es (fer fi rst(Jise), pointing away from the face. • Hold the bottle with the thumb at the base and nozzle between first and second fingers.
figure 1
• Insert pump gently into the nose with the head upright. • Depress pump completely and sniff deeply. • Wait 3-5 minutes and then blow nose. • Administer another spray if necessary. !Pill Rinse the spray'if tip with hot water taking care not to allow w 'a ter to enter the bottle. • Replace cap.
AMERICAN PHARMACY
