Nasal spray topical

Rhinitis is characterized by nasal stuffiness with partial or full obstmction, and itching of the nose, eyes, palate, or pharynx, sneezing, and rhinorrhoea. If left untreated it can lead to more serious respiratory diseases such as sinusitis or asthma. Although several types of dmgs are available for treatment, nasal spray topical corticosteroids are widely regarded as the reference standard in rhinitis therapy (250). 

TABLE 2.2 Over-the-Counter Medications with a High Potentiai for Addiction Nasal sprays Topical decongestants can be habit-forming. 

Astemi2ole (10) has further been modified into a series of 4-phenylcyclohexylamine compounds, resulting in the synthesis of cabastine, for example. Cabastine is a highly active compound and its geometric isomers are also active, demonstrating the stereoselectivity of histamine receptors toward chiral ligands. The > S, 4 R-levo antipode of cabastine was the most active, and therefore this isomer, levocabastine (13), has been chosen for further development. Because of high potency, levocabastine has been developed for topical appHcation such as eye drops and nasal spray. 

Antihistamines are drags used to counteract the effects of histamine on body organs and structures. Examples of antihistamines include diphenhydramine (Benadryl), loratadine (Claritin), fexofenadine (Allegra), and cetirizine (Zyrtec). A new antihistamine, deslorata-dine (Clarinex), is die active metabolite of loratadine and is intended to eventually replace loratadine (Claritin). Topical corticosteroid nasal sprays such as fluticasone propionate (Flonase) or triamcinolone ace-tonide (Nasacort AQ) are also used for nasal allergy symptoms. See Chapter 56 for more information on die topical corticosteroids. 

Its contract manufacturing is categorized in two different areas (i) topical compositions, which resemble traditional creams, lotions, and ointments in appearance and use, and (ii) liquid compositions that can be absorbed sublingually, nasal spray products, or liquid ingestion products. 

Over the years it has been interesting to note that many compounded products eventually become commercially available products. Recent examples might include fentanyl lozenges, minoxidil topical solution, nystatin lozenges, clindamycin topical solution, tetracaine-adrenalin-cocaine (TAG) solution, dihydroergotamine mesylate nasal spray, buprenorphine nasal spray, buffered hypertonic saline solution, and erythromycin topical solution as well as numerous other dermatological and pediatric oral liquids and some... 

The inclusion of the a routine microbial limit test in a marketed product stability protocol depends on the pharmaceutical dosage form. Typically, the test would be used only for nonsterile products, especially oral liquids, nasal sprays, and topical liquids, lotions, and creams that have sufficient water activity to support the growth of microorganisms. In contrast, tablets, powder- and liquid-filled capsules, topical ointments, vaginal and rectal suppositories, nonaqueous liquids and inhalation aerosols with a water activity too low to allow for the product to support the growth of microorganisms would not be routinely tested. 

Rhinocort Aqua is the proprietary preparation of a topical nasal spray containing the corticosteroid budesonide and is marketed by AstraZeneca. 

Fluticasone, Nasal (Flonase) [Anti inflammotory/Corticos-teroid] Uses Seasonal all gic rhinitis Action Topical st oid Dose Adults Feds >12 y. 2 sprays/nostril/d Feds 4-11 y. 1-2 sprays/nostril/d Caution [C, M] Contra Primary Rx of status asthmaticus Disp Nasal spray meg SE HA, dysphonia, oral candidiasis Interactions t Effects ketoconazole EMS May... 

Shin disease Topical Apply cream, lotion, or ointment to affected area once a day Nasal polyp Nasal spray 2 sprays in each nostril twice a day... 

Beclomethasone dipropionate, triamcinolone acetonide, budesonide, flunisolide, and mometasone furoate are available as nasal sprays for the topical treatment of allergic rhinitis. They are effective at doses (one or two sprays one, two, or three times daily) that in most patients result in plasma levels that are too low to influence adrenal function or have any other systemic effects. 

Topical administration to the nose The safety of nasal glucocorticoids in the treatment of allergic rhinitis has been reviewed (434,435). The local application of glucocorticoids for seasonal or perennial rhinitis often results in systemic adverse effects. The use of nasal sprays containing a glucocorticoid that has specific topical activity (such as beclomethasone dipropionate or flunisolide) seems to reduce the systemic adverse effects, but they can nevertheless occur, even to the extent of suppression of basal adrenal function in children (436). Local adverse effects include Candida infection, nasal stinging, epistaxis, throat irritation (437), and, exceptionally, anosmia (438). 

Mupirocin (Bactroban) inhibits a specific enzyme responsible for tRNA synthesis in susceptible bacteria. This drug is used topically to treat skin infections caused by Staphylococcus aureus or Streptococcus pyogenes. Likewise, mupirocin can be administered by nasal spray to treat local colonization of S. aureus in the nasal mucosa. This idea may be especially helpful in preventing systemic infection in individuals such as health care workers who are exposed to an outbreak of resistant strains of S. aureus. Local/topical administration of this drug is well tolerated, although some irritation of the skin may occur during topical use, and cough and respiratory irritation can occur when mupirocin is administered by nasal spray. 

It should be noted that many market names are used for all of the antiinflammatories listed in Table 2, depending on market liaisons, generic competition, derivatives such as esters, and the form of the drug product (e.g., topical, inhaler, nasal spray, etc.). For example, Schering s betamethasone 17,21-dipropionate is marketed as Diprosone, and Glaxo s betamethasone-17-valerate was marketed as Betnovate. 

Beclomethasone dipropionate is also used as a nasal spray in the prophylaxis and treatment of allergic and nonallergic rhinitis, and is used topically in the treatment of various skin disorders. It is generally applied as a cream or ointment. Beclomethasone salicylate has also been used topically. 

Combination therapy of topical and systemic drugs is also an important treatment consideration. When symptoms are isolated to the eye, topical treatment is rapid and most efficient. However, in cases of rhinoconjunctivitis, when nasal symptoms are also present, optimum management includes combining topical ophthalmic medications, olopatadine or ketotifen, for example, with a nasal spray or systemic treatment, such as the oral antihistamine desloratadine. For rhinitis, nasal steroids provide a good treatment option. The above approach targets particular areas of involvement by utilizing the most efficacious route of treatment. 

Lunell E, Molander L, Andersson M. Relative bioavaUabil-ity of nicotine from a nasal spray in infectious rhinitis and after use of a topical decongestant. Eur J Clin Pharmacol 1995 48(l) 71-5. 

Almond oil is used therapeutically as an emollient and to soften ear wax. As a pharmaceutical excipient it is employed as a vehicle in parenteral preparations, such as oily phenol injection. It is also used in nasal spray,and topical preparations. Almond oil is also consumed as a food substance, see Section 18. 

GRAS listed. Accepted as a food additive in Europe. Included in the FDA Inactive Ingredients Guide (IM and IV injections, nasal sprays, oral capsules and tablets, and sublingual, rectal, topical, and vaginal preparations). Included in nonparenteral medicines licensed in the UK. Included in the Ganadian List of Acceptable Non-medicinal Ingredients. 

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