Allergic Rhinitis PDF

Overview o Rhinitis is a common disorder and refers to inflammation in the nasal cavity. o Common manifestations can include nasal discharge, itching, sneezing, congestion, and postnasal drip. o Rhinitis can be caused by allergic (hay fever, prennial) or nonallergic. o Based on the relationsh...

Overview o Rhinitis is a common disorder and refers to inflammation in the nasal cavity. o Common manifestations can include nasal discharge, itching, sneezing, congestion, and postnasal drip. o Rhinitis can be caused by allergic (hay fever, prennial) or nonallergic. o Based on the relationship between inflammation in the upper and lower airways, rhinitis is a risk factor for asthma development, and poorly controlled rhinitis can aggravate asthma control.  Overview o Classic signs of allergic airways disease in children: Sniffing and snorting in response to nasal itching and discharge Frequent upward rubbing of the nose (generally with the palm of the hand) is caused by nasal itching Dark circles under the eyes are commonly known as “allergic shiners” and they can be further aggravated by the frequent rubbing of the eyes associated with severe ocular itching  Pharmacotherapy o Antihistamines (Systemic, Local: Intranasal, Eye drop) o Decongestants (Systemic, Local: Intranasal, Eye drop ) o Corticosteroids (Intranasal, Eye drop) o Mast-cell stabilizers (Intranasal, Eye drop) o Anticholinergics agents (Intranasal) o Leukotriene Modifiers (Systemic)  Antihistamines o The term antihistamine, refers to the classic H1-receptor blockers. o Antihistamines are the most common treatment for allergic rhinitis and are effective for relieving sneezing, itching, and rhinorrhea. o They can be divided into first- and second-generation agents. o Although 1st generation drugs are efficacious, their use is limited by anticholinergic, sedative, and performance-impairing effects, which challenge their cost-effectiveness.  Antihistamines o 1st generation agents cross the BBB leading to unwanted adverse effects. o The non-sedating antihistamines (2nd generation agents) do not cross the BBB and therefore are less sedating and preferred for small children and the elderly. o Another advantage of 2nd generation agents is that most products can be dosed once daily to improve patient adherence to therapy.  Intranasal Antihistamines o A potential role for intranasal antihistamines is for patients who do not respond adequately to oral antihistamines. o These are considered to be equal in efficacy to oral 2nd generation agents with a quicker onset of action within 15 to 30 minutes. o Also, they may improve congestion. o The intranasal agents (azelastine and olopatadine) have a faster onset of action than oral agents, but unfortunately require twice daily dosing.  Clinical Uses o Allergic Reactions The sedative effect and the therapeutic efficacy of different agents vary widely among individuals. The clinical effectiveness of one group may diminish with continued use. o Nausea and Vomiting o Insomnia  Clinical Uses o Urticaria (hives) o Angioedema Angioedema is the swelling of the deeper layers of the skin, caused by a build-up of fluid. The symptoms of angioedema can affect any part of the body, but swelling usually affects the eyes and lips.  Clinical Uses o Motion Sickness and Vestibular Disturbances Meniere’s syndrome o Local anesthetics o Increase of appetite  The 1st generation agents o Diphenhydramine (Benadryl®) Tab: 25, 50mg Elixir 12.5mg/5ml Oral solution 12.5mg/5ml Injection 50mg/1ml  Clinical uses Allergic reactions (hives, rhinitis), Allergic coughs Motion sickness Insomnia Local anesthetics Parkinsonism ‫‪Diphenhydramine‬‬ ‫ در بارداری در رده ‪ B‬قرار دارد و در شیر ترشح می شود‪.‬‬ ‫ الگزیر (و گاها محلول خوراکی) جهت تهیه داروی ترکیبی آفت دهان‬ ‫ مصرف در آسم با احتیاط‬ ‫ در بعضی قرص های سرماخوردگی‬ ‫ عدم مصرف به صورت ‪ OTC‬در زیر دو سال‬ ‫‪ ‬آمپول‬ ‫ واکنش های آلرژیک‪ ،‬بیماری مسافرت‪ ،‬واکنش های دیستونی‬ ‫ بعد از تزریق اپی نفرین در درمان شوک آنافیالکسی‬ ‫ به صورت عضالنی و به صورت وریدی‬ ‫ تزریق پوستی و زیر پوستی منجر به ‪local necrosis‬‬ ‫ منع مصرف به عنوان بی حسی موضعی‬ ‫‪Syrup Diphenhydramine compound‬‬ ‫ حاوی دیفن هیدرامین (‪ 12/5‬میلیگرم در ‪ 5‬میلی لیتر) و آمونیوم کلراید (‪ 125‬میلیگرم در ‪ 5‬میلی لیتر)‬ ‫ آنتی هیستامین ‪ +‬خلط آور‬ ‫ شربت دیفن هیدرامین کامپاند در سرفه های خلط دار مورد استفاده قرار می گیرد‪.‬‬  The 1st generation agents o Dimenhydrinate (Dramamine®, Travelin®) Tab: 50 mg Is a salt of diphenhydramine  Clinical uses Nausea and vomiting Dizziness Motion sickness Radiation sickness Morning sickness (Off label) Menier (Off label) ‫‪Dimenhydrinate‬‬ ‫ برای پروفیالکسی ‪ 30‬دقیقه قبل حرکت‬ ‫ سپس هر ‪ 4‬تا ‪ 6‬ساعت در صورت نیاز (حداکثردوز ‪ 400‬میلیگرم)‬ ‫ شروع اثر ‪ 15‬تا ‪ 30‬دقیقه‪ ،‬طول اثر ‪ 4‬تا ‪ 6‬ساعت‬ ‫ مصرف زیر ‪ 2‬سال ممنوع است‪.‬‬ ‫ در شیر ترشح می شود‪.‬‬ ‫ در بارداری ‪ 50‬تا ‪ 100‬میلیگرم هر ‪ 4‬تا ‪ 6‬ساعت‬  The 1st generation agents o Cyproheptadine (Periactin®) Tab: 4 mg Syrup 2mg/5ml Oral solution 2mg/5ml  Clinical uses Allergic reactions (rhinitis, hives, angioedem) Increase appetite (Off label) Migraine headache (Off label) Serotonine syndrome (Off label) Drug-induced sexual disorders (Off label) ‫‪Cyproheptadine‬‬ ‫ به عنوان اشتهاآور برای باالی دو سال‬ ‫ دستور مصرف‪:‬‬ ‫هفته اول‪ :‬هر ‪ 6‬ساعت ‪ 2‬میلی گرم (نصف قرص)‬ ‫هفته دوم‪ :‬هر ‪ 6‬ساعت ‪4‬میلی گرم (یک قرص)‬ ‫ استفاده نادرست در کنار دگزامتازون‬ ‫ اثرات آنتی کولینرژیک متوسط با خواب آوری کم‬ ‫ در بارداری در رده ‪ B‬و در شیردهی منع مصرف دارد‪.‬‬  The 1st generation agents o Hydroxyzine (Atarax®) Tab: 10, 25 mg Syrup 10mg/5ml  Clinical uses Pruritus due to allergic conditions (Dermatitis) Hives Anxiety and insomnia Analgesic effects in combination with opioids (during labor) Nausea and vomiting (injection) ‫‪Hydroxyzine‬‬ ‫ مصرف باالی دو سال‬ ‫ در بارداری در رده ‪ ،C‬در اوایل بارداری مصرف نشود‪.‬‬ ‫ در شیردهی توصیه نمی شود‪.‬‬ ‫ شروع اثر ‪ 15‬تا ‪ 30‬دقیقه‬ ‫ طول اثر خواب آوری ‪ 4‬تا ‪ 6‬ساعت‪ ،‬طول اثر ضدخارش تا ‪ 12‬ساعت‬  The 1st generation agents o Chlorpheniramine (Hisatdic®) Tab: 4 mg Injection 10mg/1ml !‫در ایران داریم‬ Syrup 2mg/5ml  Clinical uses Allergic reactions (hives, rhinitis, pruritis) Motion sickness In cold tablets and antihistamine decongestant *Amp: IM, IV, SC * Safe during pregnancy NOT lactation  The 1st generation agents o Antihistamine decongestant  The 1st generation agents o Promethazine (Phenergan®) Syrup 5mg/5ml Injection 50mg/2ml (IM)  Clinical uses Allergic reactions (hives, rhinitis, angioedem) Nausea and vomiting (pregnancy) Motion sickness Prevents pain after surgery Sedative * Effect on hCG test (false positive or false negative) * Contraindication under 2 years  The 1st generation agents o Clemastine (Tavegil®) Tab: 1 mg Injection 2mg/2ml  Clinical uses Allergic reactions (hives, rhinitis, angioedem) * Pregnancy B * Contraindication in lactation * Over 6 years old  The 1st generation agents o Cinnarizine (Cinazin®) Tab: 25, 75mg  Clinical uses Vestibular disorders: dizziness, tinnitus, nausea and vomiting, meniere's disease Motion sickness Peripheral vascular disease (CCB) * Pregnancy B * Contraindication in lactation * Over 5 years old  The 2nd generation agents o Cetirizine (Letizen®, Apo Cetirizine®) Tab: 5, 10 mg Softgel 10mg Syrup 5mg/5ml  Clinical uses Allergic reactions (rhinitis, conjunctivitis, hives) * Can be used during pregnancy and lactation * Over 6 months * Once or twice a day  The 2nd generation agents o Loratadine Tab 10 mg ODT 10mg Softgel 10mg (Loratagel®) Syrup 5mg/5ml  Clinical uses Allergic reactions (rhinitis, conjunctivitis, hives) * Can be used during pregnancy and lactation * Over 2 years * Once a day  The 2nd generation agents o Desloratadine (Neotadin®, Lorextadin®) Tab: 5 mg Syrup 2.5mg/5ml  Clinical uses Allergic reactions (rhinitis, conjunctivitis, hives) * Can be used during pregnancy and lactation * Over 6 months * Once or twice a day  The 2nd generation agents o Fexofenadine (Telfast®, Sed off®, Rhinofax®, Fastover®) Tab: 30, 60, 120, 180 mg Oral suspension 30mg/5ml (Kidofast®)  Clinical uses Allergic reactions (rhinitis, conjunctivitis, hives) * During pregnancy C * Over 6 months * Once a day bioavailability  The 2nd generation agents o Ketotifen (Zaditen, Ketof®) Tab 1 mg Syrup 1mg/5ml Oph. Drop 0.025% (Ketoftalmic®)  Clinical uses Asthma in children Allergic reactions (rhinitis, conjunctivitis) * During pregnancy and lactation ??? * Oral: Over 6 months, Oph. Drop: over 3 years * Once a day Intranasal Antihistamines (2nd generation) o Olopatadine (Olantin®, Aleropat®, Sensit-I®) Eye drop 0.1%: children ≥3 years Nasal spray 0.6%: children ≥6 years  Clinical uses Allergic rhinitis: Nasal spray Conjunctivitis: Eye drop * During pregnancy: C Intranasal Antihistamines (2nd generation) o Azelastine (Zelex®) Nasal spray 0.1%  Clinical uses Allergic rhinitis ≥6 months Vasomotor rhinitis ≥12 years During pregnancy and lactation ???? Onset: 15 min PRN * Environmental triggers that affect vasomotor rhinitis patients may include strong odors, cold air exposure, alcohol ingestion, and/or spicy foods.  Pharmacokinetics o The 1st generation H1 blockers enter the CNS readily. o Duration of action : Most of the 1st generation (4–6 hours) 2nd generation (12–24 hours) o The active metabolites of hydroxyzine, terfenadine, and loratadine are available as drugs (cetirizine, fexofenadine, and desloratadine, respectively).  Pharmacodynamics o CNS effects A common effect of 1st generation is sedation. At ordinary dosages, children occasionally manifest excitation rather than sedation. At very high toxic dose levels, marked stimulation, agitation, and even seizures may precede coma. 2nd generation have little or no sedative or stimulant actions.  Pharmacodynamics o Antiemetic actions Several 1st generation H1 antagonists have significant activity in preventing motion sickness. o Antiparkinsonism effects Diphenhydramine is given parenterally for acute dystonic reactions to antipsychotics.  Pharmacodynamics o Antimuscarinic actions Many 1st generation agents, have significant atropine-like effects on peripheral muscarinic receptors. o Alpha-receptor-blocking actions Especially promethazine This action may cause orthostatic hypotension.  Pharmacodynamics o Serotonin-blocking actions Some 1st generation H1 antagonists (notably cyproheptadine) o Local anesthesia 1st generation H1 antagonists Diphenhydramine and promethazine  Side effects o Sedation 1st generation (Promethazine more and Chlorphenamine less) Cetirizine has more sedation potential than the other 2nd generation agents. o Anticholinergic side effects: 1st generation agents o Intranasal azelastine can also cause local side effects, including nasal irritation, dry mouth, sore throat, and mild epistaxis. 1st generation: Chlorpheniramine 2nd generation: Loratadine & Cetirizine  Decongestants o When the immune system detects the presence of an allergen (a virus or pollen): Blood flow is increased to small blood vessels of nose; this causes swelling Mucous glands within the nose secrete more mucus to trap the allergen; creates a sensation of “stuffiness” o Decongestants: reducing swelling, inflammation and mucus formation within the nasal passages or the eye  Decongestants o Decongestants are classified to: Topical decongestants: sprayed directly in the nose or instilled in the eye Systemic decongestants: Oral agents are often combined with antihistamines o Most decongestants work by activating α1 receptors either by binding directly to them or stimulating the release of NE.  Topical Decongestants o Phenylephrine (Nasophrin®, Decophen®, Ephonix®) Nasal spray: 0.25%, 0.5% (older than 2 years) Nasal drop: 0.25%, 0.5% (older than 2 years) Eye drop: 5%, 0.12% (with Zn) Injection 10mg/1ml  Instill 2 to 3 sprays into each nostril no more than every 4 hours for ≤ 3 days. ‫‪Phenylephrine‬‬ ‫قطره چشمی فنیل افرین موجود در داروخانه به دو صورت وجود دارد‪:‬‬ ‫فنیل افرین ‪( %5‬نئوفرین)‪ :‬هر ‪ 100‬میلی لیتر حاوی ‪ 5‬گرم فنیل افرین است‪.‬‬ ‫فنیل افرین زینک‪ :‬هر ‪ 100‬میلی لیتر حاوی ‪ 0/12‬گرم فنیل افرین و ‪ 0/25‬گرم زینک سولفات است‪.‬‬ ‫فنیل افرین برای ایجاد میدریازیس (جهت انجام معاینات چشم پزشکی یا اعمال جراحی) و برای کاهش خارش و‬ ‫احتقان ملتحمه (سرخی چشم) به علت التهاب یا آلرژی و در گلوکم با زاویه باز استفاده می شود‪.‬‬ ‫زینک سولفات به عنوان قابض عمل کرده و اثرات مفیدی در درمان احتقان چشم دارد‪.‬‬ ‫سولفات روی با اثر قابض خود‪ ،‬ریزش اشک را کاهش می دهد و باعث افزایش اثر فنیل افرین می شود‪.‬‬ ‫قطره چشمی فنیل افرین به هیچ وجه نباید جایگزین قطره های بینی فنیل افرین شود‪.‬‬ ‫‪Nasal (Spray, solution): 0.25, 0.5%‬‬ ‫‪Nasal Drop: 0.25, 0.5%‬‬ ‫‪Ophthalmic drop: 10%‬‬  Topical Decongestants o Naphazoline Nasal spray: 0.05% (Naprisol®, Decofzol®) Nasal drop: 0.05% Opht. Drop 0.1% (Naprivin®)  older than 12 years  Topical Decongestants o Naphazoline + Antazoline (Anaprivine®) Opht. Drop: 0.05% + 0.5%  every 6 hours  Antazoline is an antihistamine agent  Topical Decongestants o Oxymetazoline (Rinozoline®, Oxynose®, Oxynix®, Congestop®) Nasal spray: 0.05%  Instill 2 to 3 sprays into each nostril twice daily (maximum dose: 2 doses/24 hours)  Duration: generally limit to 3 to 5 days  older than 6 years  ‫مقایسه اسپری های بینی ضد احتقان از نظر طول اثر‪:‬‬ ‫اکسی متازولین > نفازولین > فنیل افرین‬ ‫اکسی متازولین‪ :‬هر ‪ 12‬ساعت‬ ‫نفازولین‪ :‬هر ‪ 6‬ساعت‬ ‫فنیل افرین‪ :‬هر ‪ 4‬ساعت‬ ‫همگی به مدت ‪ 3‬روز (نهایتا ‪ 5‬روز)‬  Topical Decongestants o Sodium Chloride (Normonix®,Rinosaltin®,DB saline®, Decosaline®) Nasal spray: 0.65% Nasal drop: 0.65% Oph.drop: 5% (Natrisalt®) Oph.oint: 5% Inhalation solution 7%  Can be used during pregnancy and lactation  Topical Decongestants  Intranasal saline In patients with only mild symptoms, saline irrigation (administered as frequently as needed) is helpful. Irrigating the nasal cavities with saline reduces postnasal drainage, remove secretions, and rinses away allergens and irritants. Saline irrigations can be used immediately prior to administration of other intranasal agents, so that the mucosa is freshly cleansed when the medication are introduced. ‫)®‪Dexpanthenol 3% (Desviva‬‬ ‫شکل دارویی‪ :‬اسپری بینی‬ ‫ماده مؤثره‪ :‬دکسپانتنول‬ ‫مقدار و نحوه مصرف‪ :‬بزرگساالن و کودکان باالی یک سال‪،‬‬ ‫یک پاف در هر سوراخ بینی ‪ 4‬بار در روز‬ ‫مکانیسم اثر‪ :‬دکسپانتنول یک ماده موثره طبیعی و از مشتقات پنتوتنیک اسید (ویتامین ب‪)5‬‬ ‫می باشد که موجب تسریع در بهبود زخم ها‪ ،‬خشکی موکوس بینی‪ ،‬کاهش پوسته های موجود‬ ‫در آن و عملکرد نرمال اپیتلیوم در نتیجه خشکی ناشی از شرایط آب و هوایی و یا‬ ‫عمل جراحی می گردد‪.‬‬  Systemic Decongestants o Phenylephrine, Pseudoephedrine Should be used with caution in elderly patients and in those with hyperthyroidism, cardiovascular disease, diabetes, glaucoma, and pregnant women Pseudoephedrine is restricted because it is used in the illegal manufacture of methamphetamine.  Systemic Decongestants o Pseudoephedrine Syrup 30mg/5ml  α1 and 2 agonist  Dose Max: 240mg  Contraindication: pregnancy (1st trimester, under 4 years)  Systemic Decongestants  GELOFEN-SINUS®, Tedaphen Sinus® Ibuprofen 200mg Phenylephrine 5mg  One of the best medicine for sinus congestion and headache  Adverse effects o Adverse effects with systemic (not topical) decongestants: Cardiovascular stimulation: elevated blood pressure, tachycardia, palpitations CNS stimulation: restlessness, insomnia, anxiety, tremors, fear, or hallucinations o Children and older adults are more likely than persons in other age groups to experience adverse effects.  Adverse effects o Adverse effects specifically related to topical decongestants: burning, stinging, sneezing, local dryness o Rhinitis medicamentosa (RM)—also known as; rebound congestion is inflammation of the nasal mucosa caused by the overuse of topical nasal/ophthalmic decongestants (NOT oral agents). It classifies as a subset of drug-induced rhinitis.  Adverse effects o How to treat rebound congestion? The first step is to stop using decongestant nasal spray Trying nasal corticosteroids for 1 week or oral pseudoephedrine for few days  Intranasal corticosteroids o The most effective medication class o Useful for more sever or persistent symptoms o Appropriate for all symptoms o Bioavailability: Beclomethasone (23%) Budesonide (11%) Mometasone, Fluticasone (