Posts Tagged ‘Benadryl’

How to treat allergic rhinitis

Monday, May 2nd, 2011

Allergic rhinitis is an IgE-mediated inflammatory disease of the nasal mucosal membranes characterized mainly by sneezing, rhinorrhea, nasal pruritis, and congestion. It is the most common form of rhinitis, affecting 20 to 40 million Americans annually, and it is considered one of the most prevalent chronic diseases in the United States. It is also well documented that allergic rhinitis can negatively impact the quality of life and contribute significantly to loss of work productivity.

Allergic rhinitis may be categorized as seasonal “hay fever” or perennial (when symptoms persist year-round). Often, patients may react to multiple allergens and have seasonal exacerbation of symptoms in addition to perennial rhinitis. Tree, grass, and weed pollens are common seasonal allergens because they become airborne in large concentrations during a particular season of the year. Important perennial allergens include house dust mites, indoor molds, animal dander, and occupational allergens.

Management overview

Treatment options for allergic rhinitis include allergen avoidance, use of pharmacological agents for prevention and control of symptoms, and allergen immunotherapy for desensitization of patients in whom avoidance strategies and pharmacotherapy have failed to produce a satisfactory response.

Allergen avoidance

Whenever possible, environmental control measures should be emphasized as a fundamental part of the treatment plan. For instance, patients with pollen or outdoor mold allergies should remain in closed environments whenever possible. Patients sensitive to dust mites should enclose all mattresses and pillows with allergen-proof casings and eliminate carpeting, if possible, to reduce exposure; bedclothes should be frequently laundered in hot water to remove allergens. Although not always feasible, patients with animal allergies should consider removal of pets from home.

Antihistamines

Antihistamines (H1-antagonists) are typically prescribed as first-line agents for allergic rhinitis. They exert their actions by competitively antagonizing histamine at the H1- receptor sites and thereby suppress symptoms attributable to histamine release, such as sneezing, rhinorrhea, nasal itching, conjunctival itching, and lacrimation.

Antihistamines, however, are generally not effective in alleviating nasal congestion.

First-generation antihistamines

Various 1st-generation antihistamines are widely available with and without prescription. Although effective and economical, the usefulness of these agents is limited by their sedative and anticholinergic properties due to penetration of the central nervous system and poor receptor specificity.

All 1st-generation antihistamines are sedating to some degree and may cause performance impairment in 10% to 40% of users. In general, the ethanolamines (e.g., diphenhydramine) and phenothiazines (e.g., promethazine) are the most sedating. The ethylenedi-amines (e.g., pyrilamine) cause moderate sedation, and the alkylamines (e.g., chlorpheniramine, brompheniramine) are considered the least sedating. The use of lst-generation antihistamines at bedtime, which are less expensive, and newer nonsedating agents during the day has been advocated as a cost-saving strategy. This therapeutic approach may not be cost-effective, however, as residual effects of the bedtime dose may result in daytime sedation and performance impairment.

The anticholinergic effects of 1st-generation antihistamines (dry mucous membranes, urinary retention, blurred vision) may preclude their use in certain patients. Elderly patients are especially sensitive to these adverse effects. These older agents should be used cautiously in patients with narrow angle glaucoma or prostatic hypertrophy or in those taking other medications that may potentiate these side effects.

Although 2nd-generation antihistamines are generally prescribed due to ease of dosing and favorable side-effects profile, clinicians should be cognizant of available non-prescription antihistamines, as many patients may be self-managing with over-the-counter products (see Table 1).

Table 1 Selected 1st-generation antihistamines

1 Generic Brand Usual doses 1
Brompheniramine Dimetane, others 4 mg q 6-8 hours
Extended Release: 12 mg q 12 hours
Chlorpheniramine Chlor-Trimeton, others 4mgq 6-8 hours
Extended Release: 12 mg q 12 hours
Clemastine Tavist, others 1.34-2.68 mg q 12 hours
Diphenhydramine Benadryl, others 25-50 mg q 6-8 hours

Note: available OTC, often in combination with various decongestants, analgesics, and antitussives

Diphenhydramine

Thursday, July 8th, 2010

(British Approved Name, rINN)

Drug Nomenclature

Synonyms: Benzhydramine; Difenhidramina; Difenhydramiini; Difenhydramin; Diphenhydraminum
BAN: Diphenhydramine
INN: Diphenhydramine [rINN (en)]
INN: Difenhidramina [rINN (es)]
INN: Diphénhydramine [rINN (fr)]
INN: Diphenhydraminum [rINN (la)]
INN: Дифенгидрамин [rINN (ru)]
Chemical name: 2-Benzhydryloxy-NN-dimethylethylamine
Molecular formula: C17H21NO =255.4
CAS: 58-73-1
ATC code: D04AA32; R06AA02

Pharmacopoeias. In Japan.

Diphenhydramine Citrate

Drug Approvals

(British Approved Name Modified, rINNM)

Synonyms: Benzhydramine Citrate; Difenhidramina, citrato de
BAN: Diphenhydramine Citrate [BANM]
INN: Diphenhydramine Citrate [rINNM (en)]
INN: Citrato de difenhidramina [rINNM (es)]
INN: Diphénhydramine, Citrate de [rINNM (fr)]
INN: Diphenhydramini Citras [rINNM (la)]
INN: Дифенгидрамина Цитрат [rINNM (ru)]
Molecular formula: C17H21NO,C6H8O7 =447.5
CAS: 88637-37-0
ATC code: D04AA32; R06AA02

Pharmacopoeias. In US.

The United States Pharmacopeia 31, 2008 (Diphenhydramine Citrate). Store in airtight containers. Protect from light.

Diphenhydramine Di(acefyllinate)

Synonyms: Benzhydramine Di(acefyllinate); Bietanautine; Difenhidramina, di(acefilinato) de; Diphenhydramine Di(acephyllinate)
INN: Diphenhydramine Di(acefyllinate) [rINNM (en)]
INN: Di(acefilinato) de difenhidramina [rINNM (es)]
INN: Diphénhydramine Diacéfylline [rINNM (fr)]
INN: Diphenhydramini Diacefyllinas [rINNM (la)]
INN: Дифенгидрамина Диацефиллинат [rINNM (ru)]
Chemical name: Diphenhydramine bis(theophyllin-7-ylacetate)
Molecular formula: C17H21NO,2C9H10N4O4 =731.8
CAS: 6888-11-5
ATC code: D04AA32; R06AA02

Note. The name Etanautine has been applied both to diphenhydramine monoacefyllinate and to ethylbenzhydramine, an antimuscarinic formerly used in the symptomatic treatment of parkinsonism.

Diphenhydramine Hydrochloride

Drug Approvals

(British Approved Name Modified, rINNM)

Synonyms: Benzhydramine Hydrochloride; Difenhidramin-hidroklorid; Difenhidramina, hidrocloruro de; Difenhidramino hidrochloridas; Difenhydramiinihydrokloridi; Difenhydramin-hydrochlorid; Difenhydraminhydroklorid; Dimedrolum; Diphenhydramini Hydrochloridum; Diphenhydraminium Chloride
BAN: Diphenhydramine Hydrochloride [BANM]
INN: Diphenhydramine Hydrochloride [rINNM (en)]
INN: Hidrocloruro de difenhidramina [rINNM (es)]
INN: Diphénhydramine, Chlorhydrate de [rINNM (fr)]
INN: Diphenhydramini Hydrochloridum [rINNM (la)]
INN: Дифенгидрамина Гидрохлорид [rINNM (ru)]
Molecular formula: C17H21NO,HCl =291.8
CAS: 147-24-0
ATC code: D04AA32; R06AA02
Read code: y00H6 [Nausea]; y01u0 [Antihistamine]

Pharmacopoeias. In China, Europe, Japan, and US. Japan also includes Diphenhydramine Tarmate.

European Pharmacopoeia, 6th ed. (Diphenhydramine Hydrochloride). A white or almost white, crystalline powder. Very soluble in water freely soluble in alcohol. A 5% solution in water has a pH of 4.0 to 6.0. Protect from light.

The United States Pharmacopeia 31, 2008 (Diphenhydramine Hydrochloride). A white, odourless, crystalline powder. It slowly darkens on exposure to light. Soluble 1 in 1 of water, 1 in 2 of alcohol and of chloroform, and 1 in 50 of acetone very slightly soluble in ether and in benzene. Its solutions are neutral to litmus. Store in airtight containers. Protect from light.

Incompatibility. Diphenhydramine hydrochloride has been reported to be incompatible with amphotericin B, cefmetazole sodium, cefalotin sodium, hydrocortisone sodium succinate, some soluble barbiturates, some contrast media, and solutions of alkalis or strong acids.

Adverse Effects and Precautions

As for the sedating antihistamines in general.

Abuse. Reports of the abuse of diphenhydramine hydrochloride.

Extrapyramidal disorders. Reports of dystonic extrapyramidal reactions to diphenhydramine.

Overdosage. In an evaluation of 136 cases, one fatal, of intoxication with diphenhydramine, the plasma concentration was correlated with frequency or extent of symptoms. The most common symptom was impaired consciousness psychosis, seizures, antimuscarinic symptoms such as mydriasis, tachycardia, and tachyarrhythmias, and respiratory failure were also observed. The positive association between dose and frequency and severity of symptoms was confirmed in a more recent study it was also found that severe symptoms were more likely to occur when 1 g or more of diphenhydramine had been taken.

There have been reports’ of rhabdomyolysis as an effect of oral diphenhydramine overdosage. The liberal application of a lotion containing diphenhydramine produced acute delirium with visual and auditory hallucinations in a 9-year-old boy and similar effects were seen in 3 children with varicella-zoster infection following the topical application of diphenhydramine (2 of these children also received oral diphenhydramine).

Porphyria. Diphenhydramine has been associated with acute attacks of porphyria and is considered unsafe in porphyric patients.

Pregnancy. A pregnant woman who was receiving diphenhydramine hydrochloride 150 mg daily for a pruritic rash gave birth to an infant who developed diarrhoea and generalised tremulous-ness 5 days later. The delay in appearance of withdrawal symptoms was considered to be due to reduced activity of glucuronyl conjugating enzymes in the first few days of life. For discussion of the use of antihistamines in pregnancy, including a suggestion of a relationship between inguinal hernia or genito-urinary malformations and diphenhydramine exposure. See also under Interactions, below, for a report of perinatal death possibly associated with temazepam and diphenhydramine.

Interactions

As for the sedating antihistamines in general. Diphenhydramine inhibits the cytochrome P450 isoenzyme CYP2D6 that is partly responsible for the metabolism of some beta blockers including metoprolol and the antidepressantvenlafaxine.

Benzodiazepines. There has been a report suggesting that a reduction in temazepam metabolism caused by diphenhydramine may have contributed to perinatal death after ingestion of these drugs by the mother.

Pharmacokinetics

Diphenhydramine hydrochloride is well absorbed from the gastrointestinal tract, although high first-pass metabolism appears to affect systemic availability. Peak plasma concentrations are achieved about 1 to 4 hours after oral doses. Diphenhydramine is widely distributed throughout the body including the CNS. It crosses the placenta and has been detected in breast milk. Diphenhydramine is highly bound to plasma proteins. Metabolism is extensive. Diphenhydramine is excreted mainly in the urine as metabolites little is excreted as unchanged drug. The elimination half-life has been reported to range from 2.4 to 9.3 hours.

Uses and Administration

Diphenhydramine, a monoethanolamine derivative, is a sedating antihistamine with antimuscarinic and pronounced sedative properties. It is used for the symptomatic relief of allergic conditions including urticaria and angioedema, rhinitis and conjunctivitis, and in pruritic skin disorders. It is also used for its antiemetic properties in the treatment of nausea and vomiting, particularly in the prevention and treatment of motion sickness (when it should be given at least 30 minutes before travelling), and in the treatment of vertigo of various causes. Diphenhydramine is used for its antimuscarin-ic properties in the control of parkin sonism and drug-induced extrapyramidal disorders (although the possibility that diphenhydramine itself may cause extrapyramidal symptoms should be remembered). Diphenhydramine has pronounced central sedative properties and may be used as a hypnotic in the short-term management of insomnia. It is a common ingredient of compound preparations for symptomatic treatment of coughs and the common cold. However, such preparations should be used with caution in children, and generally avoided in those under 2 years of age. It may also be given in combination preparations containing analgesics, particularly paracetamol. Diphenhydramine may be used parenterally as an adjunct in the emergency treatment of anaphylactic shock or when oral therapy is not feasible.

For most indications, diphenhydramine hydrochloride is given in usual oral doses of 25 to 50 mg three or four times daily. The dose for children is 6.25 to 25 mg three or four times daily, or a total daily dose of 5 mg/kg may be given in divided doses. The maximum dose in adults and children is about 300 mg daily. A dose of 20 to 50 mg may be used as ahypnotic in adults and children over 12 years old.

When oral therapy is not feasible, diphenhydramine hydrochloride may be given by deep intramuscular injection or by intravenous injection using concentrations of 1% or 5%. Usual doses are 10 to 50 mg, although doses of 100 mg have been given. No more than 400 mg should be given in 24 hours. Children may be given 5 mg/kg daily in divided doses to a maximum of 300 mg in 24 hours. Diphenhydramine hydrochloride is applied topically, usually in preparations containing 1 to 2% although, as with other antihistamines, there is a risk of sensitisation.

Diphenhydramine citrate is given orally in a dose of 76 mg at night in combination preparations for its hypnotic action. Diphenhydramine di(acefyllinate) is given as an antiemetic for the prevention and treatment of motion sickness. The usual oral dose is 90 to 135 mg, which may be repeated if necessary at intervals of at least 6 hours, to a maximum of 540 mg daily. Other diphenhydramine salts that have been used include the polistirex, the salicylate, and the tannate by mouth, the methylbromide rectally, and the metilsulfate applied topically.

Dimenhydrinate is diphenhydramine teoclate and mefenidramium metilsulfate is diphenhydramine methyl sulfomethylate.

Preparations

BP 2008: Diphenhydramine Oral Solution

The United States Pharmacopeia 31, 2008: Acetaminophen and Diphenhydramine Citrate Tablets; Acetaminophen, Diphenhydramine Hydrochloride, and Pseudoephedrine Hydrochloride Tablets; Diphenhydramine and Pseudoephedrine Capsules; Diphenhydramine Hydrochloride Capsules; Diphenhydramine Hydrochloride Elixir; Diphenhydramine Hydrochloride Injection

Proprietary Preparations

The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.

Argentina: Benadryl Antialergico¤; Benadryl; Caladryl D; Drepatil¤; Fabolergic; Histaler; Klonadryl; Mudantos H; Australia: Benadryl¤; Nytol¤; Unisom; Austria: Calmaben; Dermodrin; Dibondrin; Histaxin; Noctor; Prurex¤; Sleepia; Belgium: Azaron; Benylin Antihistaminicum; Diphamine; Nuicalm; Nustasium; R Calm; Brazil: Difenidrin; Canada: Aller-Aide; Allerdryl; Allergy Caplets; Allergy Elixir; Allergy Formula¤; Allernix; Benadryl; Calmex; Children‘s Allergy Formula; Clear Caladryl Spray¤; Dormex; Dormiphen; Insomnal; Jack & Jill Bedtime; Nytol; Simply Sleep; Sleep Aid; Sleep-Eze D; Sominex; Unisom-C¤; Unisom; Chile: Jaquedryl; Pasifen¤; Somol; Czech Republic: Benadryl N; Psilo-Balsam; Finland: Benylan¤; France: Benylin¤; Butix; Nautamine; Germany: Benadryl N¤; Betadorm D; Dibadorm N¤; Dolestan; Dormigoa N¤; Dormutil N; Emesan; Halbmond; Hevert-Dorm; Logomed Allergie-Gel¤; Logomed Beruhigungs-Tabletten¤; Logomed Juckreiz¤; Lupovalin¤; Medapur¤; Moradorm-A¤; Moradorm; nervo OPT N; Nytol¤; Pellisal-Gel¤; Pellit Insektenstich, Pellit Sonnenallergie¤; Pheramin N¤; ratioAllerg¤; S.8; Sedativum-Hevert; Sediat; Sedopretten; Sedovegan Novo¤; Sekundal-D¤; Sleepia; Vivinox Sleep stark; Greece: Benadryl; Hong Kong: Benadryl; Calox; Hydramine Cream; Unisom; India: Benadryl; Cofryl; Dimiril¤; Israel: Nytol; Italy: Allergan; Allergina¤; Benadryl¤; Nytol¤; Mexico: Bionaril¤; Difedram¤; Difenhistat¤; Drafen; Histadryl; Indumir; Nytol; Sontedril¤; Tzoali¤; Ulcoid; Unisom; Netherlands: Benylin-Difenhydraminehydrochloride¤; New Zealand: Unisom; Portugal: Benaderma; Codilergi; Russia: Psilo-Balsam (Псило-Бальзам); South Africa: Benadryl¤; Betasleep; Dihydral¤; Nytol¤; Sleepeze-PM; Singapore: Benocten; Paxidorm; Spain: Benadryl; Dormplus¤; Neosayomol; Nytol; Sonodor; Sweden: Benylan¤; Desentol; Switzerland: Bedorma; Benadryl¤; Benocten; Benylin Paediatric¤; Comprimes somniferes “S”; Comprimes somniferes formule 533¤; Dobacen¤; Neo-Synodorm¤; Sleepia; Thailand: Benadryl; United Arab Emirates: Amydramine II; United Kingdom: Adult Chesty Cough; Aller-Eze¤; Child Chesty Cough; Dreemon; Histergan; Mandalyn Paediatric; Medinex¤; Nightcalm; Nytol; Paxidorm; Sleep Aid; Sleepeaze; Sleepia¤; United States: 40 Winks; Aler-Dryl; Allerdryl¤; AllerMax; Altaryl Childrens Allergy; Banophen Allergy; Belix¤; Ben-Allergin¤; Ben-Tann; Bena-D¤; Benadryl Childrens Allergy; Benadryl Itch; Benadryl; Benahist¤; Benoject¤; Bydramine Cough¤; Compoz Night-time Sleep Aid; Dermamycin; Dihydrex¤; Diphen AF; Diphen Cough¤; Diphenhist; Dormarex 2¤; Dormin; DPH¤; Dytan; Dytuss; Genahist; Hydramyn¤; Hyrexin¤; Maximum Strength Sleepinal; Maximum Strength Unisom SleepGels; Miles Nervine; MouthKote P/R¤; Nidryl¤; Nordryl¤; Nytol; Phendry¤; Scot-Tussin Allergy; Siladryl; Silphen; Simply Sleep; Sleep-Ettes D; Sleep-eze 3¤; Sleepwell 2-nite; Snooze Fast; Sominex; Triaminic Cough & Runny Nose; Tusstat; Twilite; Uni-Bent Cough¤; Wehdryl¤; Venezuela: Benadryl; Di-Fedril; Ystal;

Multi-ingredient Preparations

Australia: Benacine¤; Benadryl Cough Medicine for Children¤; Benadryl for the Family – Dry; Benadryl for the Family Original; Benatuss¤; Benyphed¤; Bidramine¤; Chemists Own Difenacol¤; Delixir¤; Ergodryl¤; Gold Cross Cough Medicine¤; Paedamin; Panadol Night¤; Sedu Caps D¤; Senetuss¤; Austria: Aleot; Asthma Efeum; Benadryl mit Codein¤; Benadryl¤; Benadryl; Caladryl¤; Cathejell; Coldistan; Coldistan; Luuf-Nasenspray; Multodrin; Nisicur; Rhinodrin; Rhinoperd comp; Seltoc; Somnium; Sunsan-Heillotion¤; Tussoretardin; Umadren¤; Canada: Ambenyl¤; Balminil Codeine Night-Time+Expectorant; Balminil Night-Time; Benadryl Allergy/Sinus Headache; Benadryl Decongestant¤; Benylin for Allergies¤; Buckley’s Bedtime; Bye Bye Bite¤; Calamine Antihistamine; Calmasol¤; Calmylin No 4; Calmylin Original with Codeine; Calmylin; Contac Cold & Fever; Contac Cough Cold and Flu Day & Night; Contac Cough, Cold & Flu Nighttime¤; Contac Day & Night Sinus/Allergy¤; Cough Syrup with Codeine; Cough Syrup; Dermarest Plus; DM Cough Syrup¤; DM Plus; Ergodryl; Mandrax¤; Pulmorex DM; Sinutab Extra Strength Daytime/Nightime; Sinutab Nightime; Suppress; Trialyn DM; Tylenol Allergy Sinus (Nighttime); Tylenol Allergy-D; Tylenol Flu (Nighttime Relief); Germany: Anaesthecomp N; Asth-Med¤; Asthmastop¤; Befelka-Asthma N¤; Benadryl mit Codein¤; Benadryl N mit Codein¤; Betadorm-A¤; Betadorm-N¤; Betadorm¤; Biokanol N¤; Cathejell¤; Codyl cum expectorans¤; Dabylen¤; Dexa-Bronchisan¤; Diabenyl-Rhinex¤; Diabenyl¤; Dolestan forte comp¤; DoloVisano¤; Emesan forte¤; Euvegal comp¤; Grippostad¤; Keldrin¤; Kontagripp-RR¤; Kontagripp¤; Lomapect¤; Makatussin forte¤; Novo-Dolestan¤; Older¤; Palacril¤; Pectischoll¤; Pellit dermal Wund- und Heilsalbe¤; Plantival plus¤; Praesidin¤; Psilo-Balsam N¤; Reisedragee Eu Rho¤; Reisegold¤; Ribbeck¤; Sagittacin¤; Solamin¤; Spondylon B¤; Spondylon¤; Stada Reise-Dragees¤; Supertendin 3000¤; Tussoretard¤; Valeriana comp novum; Valeriana forte N¤; VisanoCor N; Vivinox-Schlafdragees¤; Vivisun¤; Zincum val plus¤; Spain: Aerospray Antialergico¤; Aletor Compositum¤; Anafilaxol B¤; Anafilaxol¤; Benadryl Expectorante¤; Benylin A P¤; Bisolvon Compositum; Caladryl; Caladryl; Coduretas¤; Curapic¤; Dexabronchisan¤; Diptol Antihist¤; Disnetam¤; Duponil¤; Isdinex; Maboterpen¤; Nasal Rovi¤; Paidoterin Descongestivo NF; Pulmofasa Antihist¤; Rhinocap; Rino Vitna¤; Rinocusi Descong¤; Rinosular¤; Syner Atom¤; Tabletas Quimpe; Talco Antihistam Calber¤; Talquis Cusi¤; Yafin¤; Switzerland: Barbamin¤; Bellagotin; Beny-Caps a la codeine¤; Benylin a la codeine N; Benylin¤; Broncho-Rivo¤; Broncho-Rivo; Caladryl¤; Cathejell¤; Demoderhin¤; Demostan¤; Detensor; Dobacen plus¤; Dolopyrine¤; Expectorant Cough Syrup¤; Expectoryn Paediatric¤; Expectoryn¤; Histacyl Compositum; Histacyl Cutane¤; Histacylettes; Lunadon; Makatussin Comp; Motolon¤; Neo Makatussin N¤; Nina cum Diphenhydramino¤; Parapic; Pectramin; Pellit¤; Pharmalyn¤; Radix¤; Rhinitin¤; Rivolyn¤; Sedovalin¤; Somnium; Spasmo-Barbamin¤; Spasmo-Barbamine compositum¤; Toquilone compositum; Tossamine plus; United Kingdom: Benadryl Skin Allergy Relief; Benylin 4 Flu¤; Benylin 4 Flu; Benylin Chesty Coughs Original; Benylin Childrens Night Coughs; Benylin Cough & Congestion; Benylin Day & Night; Benylin Decongestant¤; Benylin Dry Coughs Original; Benylin Mentholated Linctus¤; Benylin with Codeine¤; Boots Nightime Cough Syrup 1 Year Plus; Bronalin Expectorant¤; Bronalin Junior¤; Caladryl¤; Cold Relief Night-Time¤; Cough Nurse; Covonia Night-Time; Dolvan; Dozol; Ecdylin¤; Flurex Bedtime¤; Flurex Hot Lemon¤; Guanor¤; Histalix; Lemsip Expectorant¤; Lotussin¤; Mandalyn Expectorant; Medised Infant; Meltus Junior Night Time; Meltus Night Time; Night Cold Comfort¤; Nirolex Night Cold & Flu; Noradran; Owbridges for Children¤; Panadol Night; Propain; Tixycolds; Tixylix Catarrh¤; Tixyplus; Uniflu with Gregovite C; United States: Actifed Allergy; Actifed Sinus Nighttime; Advil PM; Anti-Itch; Arthritis Foundation Nighttime¤; Aspirin Free Anacin PM; Banophen Decongestant; Bayer Select Maximum Strength Night Time Pain Relief; Benadryl Allergy/Cold; Benadryl Allergy/Congestion; Benadryl Allergy/Sinus Headache; Benadryl Cold Nighttime Formula; Benadryl Cold/Flu¤; Benadryl Decongestant; Benadryl Itch; Benadryl Plus¤; Benylin Decongestant¤; Bite & Itch Lotion; Bufferin AF Nite Time; Cala-gen¤; Clearly Cala-gel¤; Cold Control; Contac Day & Night Allergy Sinus; Contac Night Cold & Flu Caplets¤; Dermarest Plus; Dermarest; Di-Delamine; Dytan-CS; Dytan-D; Dytan-HC; Emergent-Ez; Endal-HD; Excedrin PM; Extra Strength Doans PM; Hydro DP; Ivarest; Legatrin PM; Midol PM; MouthKote O/R; MouthKote P/R¤; Night-Time Effervescent Cold¤; Nighttime Pamprin; Sominex Pain Relief; Sting-Eze; Theracof Plus; Tylenol Allergy Complete NightTime; Tylenol Allergy Sinus Day & Night; Tylenol Flu Maximum Strength; Tylenol Flu NightTime; Tylenol PM Extra Strength; Tylenol Severe Allergy; Tylenol Sore Throat Nighttime; Unisom with Pain Relief; Ziradry

Case: Antihistamines. Class

Wednesday, June 2nd, 2010

Histamine, β-aminoethylimidazole, is formed in many tissues by decarboxy-lation of the amino acid L-histidine by the enzyme histidine decarboxylase. Mast cells and basophils are the principal histamine-containing cells in most tissues. Histamine is stored in vesicles in a complex with heparin and released by either an immunologic trigger or following a mechanical or chemical stimulus. Once released, histamine produces a number of responses including local vasodilation, transudation of fluid through endothelial cells, and stimulation of nerve ending, producing pain and itching. In the lung, histamine is a bronchoconstrictor, and this action is magnified in patients with asthma. Histamine has actions in the GI tract and causes contraction of smooth muscle; it is also a potent secretagogue for gastric acid secretion, pepsin, and intrinsic factor. In the brain, histamine acts as a neurotransmitter.

The actions of histamine are mediated by four distinct membrane receptors that are coupled to G-proteins. The H: receptor, located in smooth muscle cells, endothelium, and brain, is coupled to increased diacylglycerol and Ca2+ release. The H2 receptor is located in gastric mucosa mast cells, immune cells, and brain, and is coupled to increased cAMP. There is no clinical pharmacology yet for H3 (located in the brain and peripheral neurons) or H4 (found on eosinophils and neutrophils) receptors, but both of these receptors are targets for therapeutic agents and are under intense investigation. Histamine itself has a variety of untoward effects and is useful only diagnostically to assess bronchial hyperreactivity.

Antihistamines

Compounds that block the active state of histamine H: receptors have been used for years and are widely marketed both as prescription and over-the-counter medications. The current group of available drugs can be divided into first-generation and second-generation agents. In general, first-generation agents can cross the blood-brain barrier, and they have a number of effects in the brain, including sedation and reduction in nausea. Table Currently available antihistamines lists some currently used H: antagonists.

Table: Currently available antihistamines

Chemical class Drug Antichol activity Comment
First-Generation Antihistamines
Ethanolamines Diphenhydramine

Doxylamine

Carbinoxamine

+++ I
Ethylamine diamines Pyrilamine

Tripelennamine

+

+

Piperazines Cyclizine

Meclizine

Hydroxyzine

nil

nil

I
Alkylamines Chlorpheniramine

Brompheniramine

+

+

I
Phenothiazines Promethazine

Cyproheptadine

+++

+

I
Second-generation Antihistamines
Piperidines Fexofenadine

Loratadine

nil

nil

Piperazines Cetirizine

Levocetirizine

nil

nil

Alkylamines Acrivastine nil
Phthalazinones Azelastine nil

I = available in an injection preparation; ANTI-CHOL = Anticholinergic

All of these drugs block the action of H1 receptors, and they do not possess significant affinity for the H2 receptor. However, many of the first-generation agents have significant anticholinergic activity, and this is responsible for a significant degree of their central effects. Second-generation agents are less lipid-soluble and do not penetrate the blood-brain barrier and hence have much fewer central adverse effects.

The major use of H1-receptor blockers is in the treatment of allergic reactions. Histamine is released by IgE-sensitized cells, especially mast cells and antihistamines can reduce the rhinitis, conjunctivitis, sneezing, and urticaria associated with this reaction. They are most effective in acute allergic reactions with a relatively low antigen burden, and effectiveness diminishes in chronic disorders. Antihistamines are not effective as monotherapy for bronchial asthma. Antihistamines are marketed for treatment of the common cold, but they have very limited effectiveness in this application and their adverse effects (e.g., sedation) outweigh their benefit. Some of the first-generation agents, especially dimenhydrinate, meclizine, cyclizine, and promethazine, are useful for the prophylaxis of motion sickness and vertigo. Promethazine is the most potent in this regard but has pronounced sedative activity that limits its usefulness. The sedating action of some antihistamines has been exploited in their use as sleeping aids.

Diphenhydramine is the most commonly used antihistamine in sleeping preparations. The major adverse effect of the first-generation agents is sedation. The anticholinergic activity produces atropine-like effects including dry mouth, urinary retention, and cough. Second-generation agents avoid these effects but do have adverse effects such as headache, back pain, and in the GI tract cause nausea, loss of appetite, and constipation or diarrhea. Of the presently available second-generation antihistamines, cetirizine causes the highest incidence of fatigue and somnolence (approximately 10%); loratadine appears to have the lowest incidence of this effect (approximately 1-2%). These agents may produce cardiovascular adverse effects such as hypotension, bradycardia or tachycardia, and electrocardiograph (ECG) changes.

Administration

All of the agents listed in Table Currently available antihistamines are available for oral use, and some of the first-generation agents are available for parenteral use. Topical application of diphenhydramine is useful in the treatment of minor allergic dermatologic reactions. Azelastine is administered by nasal spray.

Pharmacokinetics

Following oral administration, the Hj antagonists reach peak levels in about 2-3 hours and last 6-24 hours depending on the agent.

H2-Receptor Antagonists

Histamine is a potent gastric acid secretagogue and this action is mediated by histamine H2 receptors. Cimetidine, ranitidine, nizatidine, and famotidine are H2-specific antagonists and are used to treat gastroesophageal reflux disease and peptic ulcers.

Case: Antihistamines. Questions – Answers

Hay fever in practice. Case 1

Thursday, May 27th, 2010

A young man presents in late May. He asks what you can recommend for hay fever. On questioning, he tells you that he has not had hay fever before, but some of his friends get it and he thinks he has the same thing. His eyes have been itching a little and are slightly watery, and he has been sneezing for a few days. His nose has been runny and now feels quite blocked. He will not be driving, but is a student at the local sixth-form college and has exams coming up next week. He is not taking any medicines.

The pharmacist’s view

This young man is experiencing the classic symptoms of hay fever for the first time. The nasal symptoms are causing the most discomfort; he has had rhinorrhoea and now has congestion, so it would be reasonable to recommend a corticosteroid nasal spray, provided he is aged 18 years or over. If he is under 18 years, an oral or topical antihistamine could be recommended, bearing in mind that he is sitting for exams soon and so any preparation that might cause drowsiness is best avoided. His eyes are slightly irritated, but the symptoms are not very troublesome. You know that he is not taking any other medicines, so you could recommend acrivastine, loratadine or cetirizine. If the symptoms are not better in a few days, he should see the doctor.

The doctor’s view

A corticosteroid nasal spray is likely to be more effective. If he cannot use the OTC product because he is under 18 years, acrivastine (Benadryl), loratadine (Claritin) or cetirizine (Zyrtec) would be worth a try. Even though they are generally non-sedating, they can cause drowsiness in some patients. The student should be advised not to take his first dose just before the exam. If his symptoms do not settle, then referral is appropriate. He may benefit from sodium cromoglicate eye drops if his eye symptoms are not fully controlled by the antihistamine. It is often worthwhile trying an older antihistamine as an alternative because some people are unaffected by the sedative properties.

DIPHENHYDRAMINE

Monday, May 24th, 2010

DIPHENHYDRAMINE

(dye-fen-HYE-dra-meen)

Other Names for this Medication: Benadryl (Brand Name)

Appearance

Capsules: Small white and pink capsule (25 mg, 50 mg) – Other brands may have a different appearance

Elixir: Red liquid containing 2.5 mg Diphenhydramine per ml

Injectable: Syringes, vials containing 50 mg/ml

Why this Medication is Used

Diphenhydramine is an antihistamine which can be used to treat allergy symptoms and to help prevent nausea and vomiting caused by chemotherapy. It may also be used to prevent reactions to other drugs.

How do you take this Medication

Capsules should be swallowed with a full glass of water. Elixir should be measured using an oral syringe to get accurate dose.

Precautions

• Tell your doctor if you are pregnant or breast feeding.

• Tell your doctor if you have narrow-angle glaucoma, prostate problems, bladder obstruction, peptic ulcer, asthma, high blood pressure or thyroid problems. Any of these conditions could affect therapy with this medication.

• Tell your doctor if you are taking other prescription medication as well as over the counter medication. Diphenhydramine can cause drowsiness which could be a problem when combined with other drugs which have a similar effect (such as sleeping pills or cough and cold medicines).

• DO NOT drive if you feel drowsy after taking Diphenhydramine.

• DO NOT drink alcoholic beverages while taking Diphenhydramine.

• Store capsules, liquids in a cool dry place. Keep out of the reach of children.

For more information on this medication, please call your doctor or nurse.

SIDE EFFECTS PREVENTION WHAT YOU SHOULD DO
MORE COMMON:
Sleepiness

• Dizziness

• Dryness of mouth

• Maintain regular bedtime hours. If possible schedule a nap after taking your pills.

• Get up from bed slowly

• Rest. Don’t drive a car or operative machinery if you are sleepy.

• Tell your doctor or nurse if this becomes a problem

• Suck on ice chips, suck hard, sugarless candy to promote saliva

LESS COMMON:
Fast or irregular heartbeat

• Blurred vision, headache, trouble with sleeping

• Diarrhea

• Restlessness, nervousness

• Limit hot, spicy, and fried foods; limit foods and drinks with caffeine. • Tell your doctor or nurse as soon as possible

• Tell your doctor or nurse if it becomes a problem

• Drink plenty of fluids. Phone your doctor if diarrhea lasts longer than 24 to 48 hours or you feel weak.

• Tell your doctor or nurse if it becomes a problem

The Etiology of Allergy

Wednesday, April 14th, 2010

The allergic response is a defensive reaction of the immune system against certain innocuous substances – called allergens – that the body mistakes for harmful parasites. An estimated 20% to 25% of Americans suffer from this misguided reaction against inoffensive substances that include pollens, animal danders, foods, insects and their venoms, and medications. The economic cost alone to our society is billions of dollars for medical care.

Symptoms of allergy are highly varied, because different allergens stimulate the immune system at different sites in the body. The respiratory system is the most common site of allergic reactions, with allergens in the upper airways causing sneezing and nasal congestion (allergic rhinitis, including hay fever), while allergens in the lower airways cause bronchoconstriction and wheezing (asthma). Food allergens cause immune activation in the gastrointestinal (GI) tract, leading to nausea, vomiting, abdominal cramps, and diarrhea. Local immune activation in the skin results in contact dermatitis. The most serious form of allergic reaction – anaphylaxis – occurs when an allergen enters the circulation and causes allergic manifestations at sites distant from the site of entry. In severe anaphylaxis, normal bodily functions are so disrupted that the patient may die.

Physiologically, the allergic response occurs in three stages: sensitization, mast cell activation, and prolonged immune activation. During Stage 1, when the allergen first meets the immune system, no allergic reaction is produced; instead, the system is primed for subsequent encounters with that particular allergen. Macrophages degrade the allergen and display the fragments to T lymphocytes (T cells); T cells secrete interleukin-4, which promotes maturation of B lymphocytes into plasma cells; plasma cells secrete immunoglobulin E (IgE) antibodies specific for that allergen. These antibodies attach to receptors on circulating basophils and on mast cells (immune cells derived from the bone marrow that reside close to blood vessels and the epithelium).

Stage 2 represents a later encounter between the allergen and the immune system. The allergen binds to IgE antibodies on mast cells. When it connects with two IgE molecules, the result is the activation of various enzymes that induce mast cell granules to release their contents – substances such as histamine, platelet-activating factor, prostaglandins, and leukotrienes – and these substances trigger the allergy attack. Individuals prone to allergies are known to have abnormally high levels of IgE antibodies.

Stage 3 is characterized by prolonged immune activation. Tissue mast cells and neighboring cells synthesize chemotactic and adhesion molecules that induce circulating basophils, eosinophils, and other cells to migrate into that tissue, generating a new wave of symptoms. These recruited cells secrete chemicals of their own that sustain inflammation, cause tissue damage, and recruit other immune cells.

Anaphylaxis occurs when an acute, explosive release of mediators from mast cells causes severe allergic symptoms within minutes of allergen exposure. Anaphylaxis is a medical emergency; without prompt medical attention, death can occur soon after the onset of symptoms. Shock is the major cause of death, although swelling of the vocal cords can kill by closing off the trachea. Other common reactions include pruritus (itching), urticaria (hives), and bronchoconstriction. GI manifestations can also occur, although they are less common. Symptoms may be preceded by an aura, and patients who suffer from recurrent anaphylactic episodes report that the particular symptoms experienced are almost always the same with each attack. Treatment is usually with an injection of epinephrine to inhibit mediator release, open airways, and block vasodilation.

For decades, allergies have been treated with antihistamines, but today researchers at pharmaceutical and biotechnology companies are looking well beyond histamine. They are investigating drugs to block the activity of a wide variety of mediators of the allergic response, including leukotrienes, prostaglandins, cytokines (interleukins, platelet-activating factor, and granulocyte-macrophage colony stimulating factor), adhesion molecules (integrins, selectins, and immunoglobulin adhesion molecules), and the enzymes involved in their production. Enzymes targeted for inhibition include 5-lipoxygenase (involved in the synthesis of leukotrienes), phospholipase A2 (involved in the secretion of both leukotrienes and prostaglandins), protein kinase C (involved in mast cell degranulation), serine protease tryptase (involved in the kinin cascade), and tyrosine kinase (involved in IgE activity). Ultimately, it should be possible to tailor allergy therapy to the individual patient, selecting drugs to alleviate a symptom complex or combat a particular allergen.

Plant allergies: profilins, hay fever, and food hypersensitivities

Plants represent the most common source of allergens. Two major types of allergic reactions triggered by plant allergens are respiratory symptoms from pollen inhalation and GI symptoms from the ingestion of plant foods (fruits, vegetables, grains, and nuts). Both types of allergic response are widespread, and they cross-react; patients with pollen sensitivities often report food allergies, and vice versa. Moreover, pollen immunotherapy (injection with increasing doses of the allergen) has been shown to reduce food hypersensitivity in children.

The most common manifestation of pollen sensitivity – seasonal allergic rhinitis or hay fever – affects some 15% of Americans. (A second type of allergic rhinitis, which is usually perennial rather than seasonal, includes reactions to such “indoor allergens” as animal danders and the house dust mite). Allergic rhinitis is not a dangerous condition, but it causes considerable misery and can lead to complications such as sinusitis, polyps, and asthma. The diagnosis is confirmed by skin testing; a positive result is signalled by the development of a wheal-and-flare reaction after the subcutaneous injection of very small quantities of the suspected allergen. Treatment is with antihistamines or, when these agents are ineffective, inhaled corticosteroids. Severe cases are treated with immunotherapy. These “allergy shots” can be helpful, but protection is rarely complete.

Asthma is a more serious condition, and it is increasing in both incidence and severity. The incidence of asthma and death due to asthma rose dramatically worldwide during the 1980s, presumably because of the worldwide increase in environmental pollutants and allergens. In the United States, asthma and associated mortality increased by 60% during the decade. The condition now costs society about $4 billion annually. Approximately 10% of children have asthma (which may resolve after adolescence), and up to 10% of patients acquire asthma in adulthood. As with allergic rhinitis, there are two types: extrinsic (an offending allergen can be identified) and intrinsic (no substance can be identified that induces the IgE antibody production). Asthmatics show a characteristic airway hypersensitivity (exaggerated response to bronchoconstricting substances, including cold air) and inflammation of the airways. Acute exposure to an allergen further constricts airways that are already partially occluded by the inflammatory process. Treatment is with bronchodilators to relieve acute bronchoconstriction and antiinflammatory steroids to treat the underlying inflammation.

Food allergies are also fairly common, at least in children. Youngsters are most often allergic to proteins in milk, eggs, or nuts (especially peanuts). The reaction may be subtle, such as a skin rash, and difficult to diagnose. When a skin test is positive, it is best to confirm the diagnosis with a double-blind food challenge (feed a capsule of allergen or placebo to the child on Day 1, then alternate allergens and placebo on subsequent days).

Food allergies in adults are fairly uncommon, but they are easier to diagnose because urticaria, rhinitis, asthma, or anaphylaxis usually develop within minutes after ingestion of even a very small quantity of a particular food. Diagnosis can be confirmed by skin testing. Some patients have a delayed reaction to foods (the response occurs 1 or more days after exposure), and sometimes symptoms affect other organs. Diagnosis requires a food challenge. Only 1% to 2% of adults suffer from food allergies, although studies have shown that about 25% of Americans believe they have food allergies that cause a broad range of vague conditions (fatigue, depression, irritability). The most common severe food allergy in adults is to peanuts. Often this allergy appears during childhood and is not outgrown (unlike milk allergy, which is fairly common in children but is usually outgrown).

Many allergic individuals react to both pollens and foods. For example, patients with grass pollen allergy report adverse reactions to specific plant foods (peanuts, garlic, tomato, onion, and various fruits). Patients with latex allergy report cross-reactions to avocados, bananas, and chestnuts. Some latex-sensitive patients may become anaphylactically allergic to fresh fruits. In the “latex- fruit syndrome,” 52% of latex-allergic patients had allergies to fruits, and systemic anaphylaxis occurred in 36%. The fruit allergy may show up first, followed by latex allergy on exposure to latex.

Several investigators have explored the association between pollen allergies and plant food allergies. There is evidence that a family of proteins called profilins, which are present in many plant species, are capable of acting as pan- allergens. Profilin sensitization from birch tree pollen and other pollens has been shown to cross-react with sensitization to many fresh fruits and vegetables. Profilins are usually destroyed by heat, which explains why patients who are anaphylactically sensitive to fresh fruits and vegetables can tolerate these foods when they are cooked. Unfortunately, commercial extracts of fruits and vegetables cannot be used diagnostically for skin testing because profilins are so unstable.

Latex allergy: increasing cause of anaphylaxis

Latex is an emulsion of rubber globules derived from the milky sap of plants of the Euphorbiacea family. It has been widely used for decades in the manufacture of paints, adhesives, gloves, balloons, and other products, yet only within the last 15 years or so has it been recognized as a cause of serious allergic reactions. The major allergen appears to be part of a protein referred to as rubber elongation factor. This protein fragment is an increasingly common and often unrecognized cause of contact dermatitis, pruritus, urticaria, conjunctivitis, rhinitis, and asthma. In recent years, a number of cases of latex-induced anaphylaxis have been described, and several patients have died.

Latex sensitization occurs when the allergen comes into contact with skin (intact or denuded) or the mucosa. Repeated exposure to latex is thus the primary risk factor. Individuals at increased risk include latex industry workers, health-care personnel who wear latex gloves, patients who undergo frequent operations, and patients with neural tube defects (NTD). Also at increased risk are atopic individuals, who have a predisposition to allergic reactions in general. In one study, 36.4% of subjects who had been exposed to latex and who were atopic had immediate cutaneous reactivity to latex, compared with 9.44% of atopic subjects who had not been exposed to latex, 6.85% of subjects who had been exposed but were not atopic, and 0.37% of nonexposed, nonatopic subjects.

The prevalence of latex allergy in the general population is 1%. By comparison, 3% to 9% of health-care workers who must wear latex gloves are allergic to latex. Even members of the hospital housekeeping staff are at increased risk of latex hypersensitivity. Sussman et al. screened 50 members of the housekeeping staff at the University of Toronto Medical Center and skin-tested 20 with possible atopy or symptoms suggestive of latex allergy. Four of the 20 tested positive for latex allergy, an 8% prevalence overall among the housekeeping staff. The patients with positive results all reported extensive exposure to latex gloves and recalled symptoms compatible with latex allergy (hand dermatitis, rhinoconjunctivitis).

NTD patients appear to have a predisposition to latex allergy that goes beyond clinical exposure. In one study, 72% of spina bifida patients had a history of clinical latex allergy and tested positive for latex IgE antibody. By comparison, patients with other neurological problems (spinal cord injury, stroke) and clinical exposure to latex did not show this increased incidence.

Recently Masood et al. described two patients with unrecognized latex hypersensitivity who had an anaphylactic attack that was initially diagnosed as a drug reaction. The first patient was a physician who received an injection of tetanus toxoid for an accidental needle stick; 24 hours later she experienced the abrupt onset of lightheadedness, dyspnea, wheezing, chest tightness, throat tightness, and a rash (generalized, pruritic, and erythematous). Symptoms resolved after treatment with corticosteroids and histamine-1 and -2 blockers. Presumptive diagnosis was anaphylaxis due to tetanus toxoid or possibly due to allergic response to an almond pastry consumed one hour before the anaphylactic episode.

A week later the patient was evaluated at the Northwestern University Allergy-Immunology Service. Tetanus toxoid was thought to be an unlikely cause of the anaphylaxis because of the length of time (24 hours) between injection and anaphylaxis. Almond sensitivity was also ruled out because a skin test was negative to almonds. At that time, a diagnosis of allergic rhinitis and asthma was made, and the patient was found to be skin-test positive to multiple allergens. On questioning, the patient recalled that she had put on a pair of latex gloves two minutes before the anaphylactic reaction. She also described a history of reactions to latex gloves (erythema and urticaria of the hands), and skin testing showed latex hypersensitivity (dilution 1:100,000 wt/vol). She was advised to avoid latex and carry a prefilled epinephrine syringe. Several weeks later she had a second anaphylactic episode – with dyspnea, wheezing, chest tightness, and lightheadedness – after exposure to latex gloves. Symptoms resolved with epinephrine (Adrenalin), prednisone (Deltasone, Liquid Pred), and diphenhydramine (Benadryl).

The second patient was a nurse who had a series of anaphylactic attacks before latex allergy was identified. Her first attack, which occurred 1 hour after ibuprofen ingestion, was characterized by tongue swelling, dyspnea, and throat tightness. Symptoms resolved after therapy with epinephrine, diphenhydramine, and prednisone. Thereafter the patient avoided nonsteroidal antiinflammatory agents, but episodes of anaphylaxis continued. An allergist suspected food allergies, and the patient tested positive on skin prick for multiple allergens (eggs, wheat, chocolate, chicken, and cow’s milk). Even when these foods were avoided, she had recurrent episodes of abdominal pain, diarrhea, diaphoresis, and total body urticaria.

Evaluation at Northwestern Allergy-Immunology Service disclosed that these episodes were correlated with latex exposure. At that point she recalled that merely holding latex IV tubing or an IV bag would result in red, swollen, pruritic hands, while rubbing her eye after removing latex gloves would cause facial swelling and hives, chest tightness, and dyspnea. “The patient was so sensitive,” said Masood et al., “that on several occasions the powder presumably aerosolized from a colleague removing latex gloves would cause acute wheezing, abdominal pain, and pruritic erythema.”

At Northwestern, the nurse was retested for those foods previously identified as triggering her allergic reactions – eggs, chocolate, chicken, codfish, cow’s milk, mustard, mushrooms – and the skin test results were all negative. This time, the tester used vinyl gloves to avoid contaminating the tests, as the doctors suspected that the initial positive results were because the skin tests were administered with latex gloves.

These suspicions were confirmed when the nurse tested positive to a latex glove extract at a dilution of 1:1,000,000 wt/vol. (The solution was prepared by cutting a latex glove into pieces, soaking the pieces in phosphate buffered saline for 12 hours, centrifuging, and running the supernatant through a 0.22-micron filter.) The patient was advised to resume a normal diet, avoid latex, and take hydroxyzine on work days. Because the avoidance of latex in a hospital is next to impossible, she continued to have local cutaneous reactions.

Vinyl gloves are an alternative to latex, although they are not as effective as latex for protecting against acquisition of the human immunodeficiency virus. A better solution may be to use cotton or vinyl glove liners under latex gloves. Masood et al. concluded, “Latex must be considered as a “hidden” cause of anaphylaxis, particularly in health care workers.”

Anaphylaxis after barium enema

Anaphylaxis during barium enema procedures is not uncommon. Symptoms are usually attributed to allergy to latex in the barium enema device. Recently Tarlo et al. described a patient with anaphylactic symptoms during a barium enema procedure that had been ordered for the evaluation of gastrointestinal symptoms (nausea, vomiting, abdominal bloating, and diarrhea). Within minutes of receiving the enema, the patient had abdominal cramps and mild generalized pruritus, which progressed to generalized urticaria, hypotension, chest tightness, wheezing, cyanosis, and transient loss of consciousness. She was treated for anaphylaxis and released a day later. At first, latex-induced anaphylaxis was suspected, but the barium enema delivery set was found to be free of latex. Subsequent skin testing failed to demonstrate latex sensitivity; however, a skin prick test with the barium enema solution yielded positive results. The manufacturer provided individual components of the barium enema solution for skin prick testing, and the patient was found to be allergic to carrageenan used as a suspending agent in the solution.

Carrageenans are gelatinous substances obtained originally from Irish moss (a species of seaweed), and currently obtained from a number of species of marine algae. Carrageenans are commonly used as emulsifying and suspending agents in pharmaceuticals, foods (ice cream, cream, chocolate milk, yogurt, frozen treats, salad dressings, and barbecue sauces), cosmetics, and polishes, and as clarifying agents in beverages.

On questioning, the patient recalled that her GI symptoms were worse after ingestion of certain milk products (ice cream, yogurt, and chocolate milk), although she tolerated plain milk. She was advised to avoid eating carrageenan- containing products. It is interesting that the patient underwent a barium enema procedure for the evaluation of GI symptoms, and the barium solution itself provided the clue for diagnosis.

Drugs in Allergic Disorders

Wednesday, February 17th, 2010

Allergy refers to a broad state of altered reactivity to a foreign substance, resulting from prior experience with the same substance. Used today, the term allergy generally refers to the unfavorable clinical consequences of an antigen-antibody interaction. Although the term allergic disorder implies an immune mechanism, in many allergic disorders, most notably bronchial asthma and atopic dermatitis, non-immune mechanisms may be of great importance. Many of the clinical conditions being treated by an allergist may be aggravated by non-immune factors such as pollution, psychic stress, cold air, and exertion -for example, exercise-induced asthma. We must always remember that there are three main principles in the therapy of allergic diseases:

1. Most important: avoidance of allergens and irritants known or suspected to be causing or aggravating the disorder.

2. The use of pharmacologic agents, restricted to as few as possible.

3. The use of specific immunotherapy or hyposensitization.

We must use a drug appropriate to the patient’s symptoms; antihistamines, for example, are useful for ear and nose complaints as well as pruritis of the skin (i.e. urticaria, eczema).

Drugs Used in the Treatment of Allergic Disorders

Antihistamines have been used in the treatment of allergic conditions for the past 30 years. They compete with the histamine released through either an antigen-antibody reaction, by physical trauma or by a histamine-liberating agent (eg. morphine, codeine). This histamine is released from the mast cells. The antihistamines compete for the cellular receptor sites, but they do not combine with the histamines in vivo or in vitro.

There are many commercially available antihistamines, which can be classified into five major groups. Physicians should be familiar with one member of each group. If the initial drug chosen does not give a good therapeutic response, use an antihistamine in another group. At times, it is necessary to try an antihistamine of one group after another, often in various combinations with sympathomimetic agents, to obtain reasonable results.

The classes of antihistamines are as follows:

1. Ethanolamines, e.g. diphenhydramine (Benadryl), dosage five mg/kg/day in three or four divided doses. A side effect is marked sedation.

2. Ethylenediamine; e.g. tripelennamine (Pyribenzamine), dosage five mg/kg/day in three or four divided doses. Side effects include moderate sedation.

3. Alkylamine; e.g. chlorpheniramine (Chlor-Tripolon), dosage 0.3 mg/kg/day in three or four divided doses. There is minimal sedation.

4. Piperazines; e.g. hydroxyzine (Atarax).

5.Phenothiazine, e.g. promethazine (Phenergan), dosage 0.5 mg/kg before retiring or 0.3 mg/kg/day. This has side effects of marked sedation.

Remember that antihistamines compete with the histamine already released in the body of the cell receptors, thus blocking the effect of the released histamine on the effector organs. Antihistamines do not combine chemically with the histamine, and they do not interfere with the antigen antibody reaction.

The sympathomimetic amine drugs or beta adrenergic agonists and theophylline are useful bronchodilators for bronchospasm.

The antibiotics used for infection in an allergic individual are tetracycline after age seven (five to ten mg/kg every six hours) and erythromycin, an unusually safe drug, orally, 10 mg/kg every six hours.

Steroids are used for more severe and acute symptoms.