Otolaryngology Book

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Sedating Antihistamine

Aka: Sedating Antihistamine, First Generation Antihistamine, Antihistamine, Chlorpheniramine, Bromopheniramine, Cyproheptadine, Hydroxyzine, Periactin, Atarax, Vistaril
  1. See Also
    1. Non-Sedating Antihistamine
    2. Diphenhydramine (Benadryl)
  2. Mechanism
    1. First Generation Antihistamine
  3. Adverse Effects
    1. Sedation or Paradoxic excitability
    2. Worsens Benign Prostatic Hyperplasia
    3. Worsens Glaucoma
    4. Dizziness
    5. Respiratory depression
    6. Tachycardia
    7. Seizures
    8. QT Prolongation (and Torsades de Pointes)
      1. Especially with Hydroxyzine
    9. Anticholinergic Symptoms
      1. Hallucinations
      2. Blurred Vision
      3. Agitation
  4. Indications
    1. Allergic Rhinitis
    2. Antiemetic
    3. Anaphylaxis
    4. Acute Urticaria
    5. Chronic Urticaria
    6. Anti-pruritic
      1. Suppresses itching, and reduces lesions
      2. Does not completely eradicate
      3. Hydroxyzine (Atarax) is most potent Antihistamine for Pruritus
  5. Preparations: Antihistamine
    1. See Diphenhydramine (Benadryl)
    2. Chlorpheniramine (Chlor-Trimeton)
      1. Dose: 4 mg orally every 4 to 6 hours as needed
    3. Clemastine (Tavist)
      1. Dose: 1.34 mg orally twice daily as needed
    4. Cyproheptadine (Periactin)
      1. Dose: 4 mg orally three times daily as needed
    5. Hydroxyzine (Atarax, Vistaril)
      1. Dose: 0.5 mg/kg up to 25-50 mg orally or intramuscular every 4-6 hours as needed
Medication Costs
chlorpheniramine (on 5/17/2017 at Medicaid.Gov Pharmacy Drug pricing)
CHLORPHENIRAMINE ER 12 MG TAB Generic OTC $0.26 each
cyproheptadine (on 5/17/2017 at Medicaid.Gov Pharmacy Drug pricing)
CYPROHEPTADINE 2 MG/5 ML SYRUP Generic $0.08 per ml
CYPROHEPTADINE 4 MG TABLET Generic $0.44 each
hydroxyzine (on 5/17/2017 at Medicaid.Gov Pharmacy Drug pricing)
HYDROXYZINE 10 MG/5 ML SOLN Generic $0.04 per ml
HYDROXYZINE 10 MG/5 ML SYRUP Generic $0.04 per ml
HYDROXYZINE HCL 10 MG TABLET Generic $0.07 each
HYDROXYZINE HCL 25 MG TABLET Generic $0.08 each
HYDROXYZINE HCL 50 MG TABLET Generic $0.10 each
HYDROXYZINE PAM 100 MG CAP Generic $0.45 each
HYDROXYZINE PAM 25 MG CAP Generic $0.06 each
HYDROXYZINE PAM 50 MG CAP Generic $0.08 each
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information.

Chlorpheniramine (C0008281)

Definition (MSH) A histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than PROMETHAZINE.
Definition (CSP) histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, asthma and in veterinary applications; one of the most widely used of the classical antihistamines.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D002744
SnomedCT 9944001, 372914003
LNC LP16072-8, MTHU006724
English Chlorphenamine, Chlorpheniramine, Chlorprophenpyridamine, 2-Pyridinepropanamine, gamma-(4-chlorophenyl)-N,N-dimethyl-, Chlorpheniramine (Allergy), chlorpheniramines (medication), chlorpheniramine (medication), chlorpheniramines, antihistamines chlorpheniramines, Chlorpheniramine [Chemical/Ingredient], CHLORPHENIRAMINE, 3-(p-Chlorophenyl)-3-(2-pyridyl)-N,N-dimethylpropylamine, Chlorophenylpyridamine, 4-Chloropheniramine, Chloropheniramine, chlorpheniramine, chlorphenamine, Chlorpheniramine (product), Chlorpheniramine (substance)
Swedish Klorfeniramin
Czech chlorfeniramin
Finnish Kloorifeniramiini
Russian KHLORFENAMIN, KHLORFENIRAMIN, KHLORPROFENPIRIDAMIN, ХЛОРПРОФЕНПИРИДАМИН, ХЛОРФЕНАМИН, ХЛОРФЕНИРАМИН
Japanese クロルプロフェンピリダミン, マレイン酸クロルフェニラミン, クロルフェニラミン, クロルフェナミン
Italian Clorprofenpiridamina, Clorofenamina, Clorofeniramina
Spanish Clorfeniramina, Clorprofenpiridamina, Clorofeniramina, Cloroprofenpiridamina, clorfeniramina (producto), clorfeniramina (sustancia), clorfeniramina, Clorfenamina
Polish Chlorfeniramina, Chlorfenamina
French Chlorphénamine, Chlorphéniramine
German Chlorphenamin, Chlorpheniramin, Chlorprophenpyridamin
Portuguese Clorfenamina, Clorfeniramina, Clorprofempiridamina
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Cyproheptadine (C0010620)

Definition (NCI_NCI-GLOSS) A drug that is used to treat asthma, allergies, and colds, and to relieve itching caused by certain skin disorders. It has also been used to stimulate appetite and weight gain, and is being studied in the treatment of weight loss caused by cancer and its treatment. Cyproheptadine belongs to the family of drugs called antihistamines.
Definition (MSH) A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc.
Definition (CSP) serotonin antagonist and histamine H1 blocker used as an antipruritic, appetite stimulant, antiallergic, and to treat the post-gastrectomy dumping syndrome.
Definition (PDQ) The hydrochloride salt of a synthetic methyl-piperidine derivative with antihistaminic and anti-serotoninergic properties. Cyproheptadine competes with free histamine (HA) for binding at HA-receptor sites, thereby competitively antagonizing histamine stimulation of HA-receptors in the gastrointestinal tract, large blood vessels, and bronchial smooth muscle. This agent also competes with free serotonin for binding at serotonin receptor sites. Cyproheptadine exhibits anticholinergic and sedative properties and has been shown to stimulate appetite and weight gain. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=315774&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=315774&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C28949" NCI Thesaurus)
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D003533
SnomedCT 26462003, 372683000
LNC LP18932-1, MTHU006211
English Cyproheptadine, cyproheptadine, Piperidine, 4-(5H-dibenzo(a,d)cyclohepten-5-ylidene)-1-methyl-, Cyproheptadine [Chemical/Ingredient], MK 141, 4-(5H-Dibenzo(a,d)cyclohepten-5-ylidene)-1-methylpiperidine, 5-(1-Methylpiperidylidene-4)-5H-dibenzo(a,d)cyclopheptene, CYPROHEPTADINE, cyproheptadine (medication), antihistamines cyproheptadine, Cyproheptadine (product), Cyproheptadine (substance)
Swedish Cyproheptadin
Czech cyproheptadin
Finnish Syproheptadiini
Russian TSIKLOGEPTADIN, PERITOL, ПЕРИТОЛ, ЦИКЛОГЕПТАДИН
Portuguese Ciproeptadina, Ciproheptadina, Cipro-Heptadina
Polish Cyproheptadyna
Japanese シプロヘプタジン, 塩酸シプロヘプタジン
Spanish ciproheptadina (producto), ciproheptadina (sustancia), ciproheptadina, Ciproheptadina
French Cyproheptadine
German Cyproheptadin
Italian Ciproeptadina
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Histamine H1 Antagonists (C0019592)

Definition (NCI) Any agent that binds to the histamine H1 receptor, thereby antagonizing histamine mediated allergic reactions, such as bronchoconstriction, vasodilation and up-regulated capillary permeability.
Definition (NCI_NCI-GLOSS) A type of drug that blocks the action of histamines, which can cause fever, itching, sneezing, a runny nose, and watery eyes. Antihistamines are used to prevent fevers in patients receiving blood transfusions and to treat allergies, coughs, and colds.
Definition (MSH) Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.
Concepts Pharmacologic Substance (T121)
MSH D006634
SnomedCT 349955005, 373228009
English Antihistaminics, H1, H1 Antihistaminics, H1 Receptor Blockaders, Histamine H1 Receptor Blockaders, Receptor Blockaders, H1, Histamine H1 Receptor Antagonists, Antagonists, Histamine H1, Antagonists, Histamine H1 Receptor, Blockaders, Histamine H1 Receptor, H1 Antagonists, Histamine, Histamine H1 Blockers, Antihistamine, Histamine H1 Antagonists, HISTAMINE RECEPTOR ANTAGONISTS H1, BLOCKADERS HISTAMINE H1 RECEP, ANTIHISTAMINICS H 01, H1 RECEPT BLOCK, HISTAMINE H1 ANTAG, HISTAMINE H1 RECEPT ANTAG, HISTAMINE ANTAGONISTS H 001, RECEPT BLOCK H1, HISTAMINE H1 RECEPT BLOCK, HISTAMINE RECEPTOR BLOCKADERS H1, HISTAMINE H1 BLOCK, ANTAG HISTAMINE H1 RECEPT, ANTAG HISTAMINE H1, H1 blockers, histamine H1 receptor blockaders, antihistaminic h1, h1 antihistamine, h1 blockers, antihistamine h1, antihistamines h1, h1 blocker, antihistamine, H1 antihistamine, H1 antihistamine (product), H1 antihistamine (substance), H-1 Receptor Antagonist, Histamine-1 Receptor Antagonist
French Antagonistes des récepteurs histaminergiques H1, Antihistamines H1, Antihistaminiques des récepteurs H1, Anti-histaminiques H1, Anti-histamines H1, Antihistaminiques H1, Antagonistes H1
Swedish Histamin H1-blockerare
Czech histamin H1 - antagonisté, histaminové H1-receptory - blokátory
Finnish Histamiini-H1-salpaajat
German Antagonisten, Histamin H1-Rezeptor-, Antagonisten, Histamin H1-, Histamin-H1-Rezeptor-Antagonisten, Histamin-H1-Rezeptorblocker, H1-Rezeptorblocker, Histamin H1-Blocker, ANTIHISTAMINIKA H 01, HISTAMIN REZEPTORENBLOCKER H1, HISTAMIN REZEPTOREN ANTAGONISTEN H1, HISTAMIN ANTAGONISTEN H 001, Antihistaminika, H1-, Histamin-H1-Antagonisten
Russian ANTIGISTAMINNYE H1 SREDSTVA, BLOKATORY GISTAMINOVYKH H1-RETSEPTOROV, GISTAMINA H1 ANTAGONISTY, ANTIGISTAMINNYE SREDSTVA, GISTAMINOVYKH H1-RETSEPTOROV ANTAGONISTY, GISTAMINOVYKH H1-RETSEPTOROV BLOKATORY, ANTIGISTAMINNYE SREDSTVA KLASSICHESKIE, PROTIVOGISTAMINNYE SREDSTVA, АНТИГИСТАМИННЫЕ H1 СРЕДСТВА, АНТИГИСТАМИННЫЕ СРЕДСТВА, АНТИГИСТАМИННЫЕ СРЕДСТВА КЛАССИЧЕСКИЕ, БЛОКАТОРЫ ГИСТАМИНОВЫХ H1-РЕЦЕПТОРОВ, ГИСТАМИНА H1 АНТАГОНИСТЫ, ГИСТАМИНОВЫХ H1-РЕЦЕПТОРОВ АНТАГОНИСТЫ, ГИСТАМИНОВЫХ H1-РЕЦЕПТОРОВ БЛОКАТОРЫ, ПРОТИВОГИСТАМИННЫЕ СРЕДСТВА
Japanese 古典的抗ヒスタミン薬, ヒスタミンH1拮抗剤, ヒスタミンH1遮断薬, ヒスタミンH1受容体拮抗薬, ヒスタミンH1受容体遮断剤, 抗ヒスタミン剤H1, 古典的抗ヒスタミン剤, ヒスタミンH1受容器遮断薬, ヒスタミンH1アンタゴニスト, ヒスタミンH1受容体遮断薬, H1受容体拮抗薬, H1ブロッカー, H1受容体拮抗剤
Croatian HISTAMIN H1 ANTAGONISTI
Polish Antagoniści histaminy H1, Leki przeciwhistaminowe H1, Antyhistaminiki H1, Leki antyhistaminowe H1, Blokery receptora H1 histaminy, Antyhistaminiki klasyczne
Portuguese Bloqueadores dos Receptores Histamínicos H1, Antagonistas dos Receptores H1 de Histamina, Antagonistas dos Receptores Histamínicos H1, Bloqueadores dos Receptores H1 de Histamina, Anti-Histamínicos H1
Spanish Bloqueadores de los Receptores Histamínicos H1, Antagonistas de los Receptores Histamínicos H1, Bloqueadores de los Receptores H1 de Histamina, antihistamínico H1 (producto), antihistamínico H1 (sustancia), antihistamínico H1, Antagonistas del Receptor H1 de Histamina, Antihistamínicos H1
Italian Antagonisti dell'istamina H1
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Hydroxyzine (C0020404)

Definition (CHV) a kind of antihistamine and mild anti-anxiety drug
Definition (NCI) A piperazine derivative with antihistamine, antiemetic, and anxiolytic properties. Hydroxyzine's antihistaminic effect is due to its metabolite, cetirizine, a potent H1 receptor antagonist and selective inhibitor of peripheral H1 receptors. This agent competes with histamine for binding at H1-receptor sites on the effector cell surface. The sedative properties of hydroxyzine occur as a result of suppression of certain subcortical regions of the brain. Secondary to its central anticholinergic actions, hydroxyzine may be effective as an antiemetic.
Definition (MSH) A histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D006919
SnomedCT 372856003, 80165005
LNC LP15171-9, MTHU002560
English Hydroxyzine, 2-(2-(4-((4-Chlorophenyl)phenylmethyl)-1-piperazinyl)ethoxy)ethanol, Ethanol, 2-(2-(4-((4-chlorophenyl)phenylmethyl)-1-piperazinyl)ethoxy)-, Hydroxyzine [Chemical/Ingredient], hydrOXYzine, HydrOXYzine, hydroxyzine, HYDROXYZINE, Hydroxyzine (product), Hydroxyzine (substance)
Swedish Hydroxizin
Czech hydroxyzin
Finnish Hydroksitsiini
Russian GIDROKSIZIN, ГИДРОКСИЗИН
Japanese アタラックス-P, ヒドロキシジンパモ酸塩, パモ酸ヒドロキシジン, アタラックスP, ジスロンP, 塩酸ヒドロキシジン, ジスロン, アタラックス, ヒドロキシジン, ハタナジン, ヒドロキシジン塩酸塩
Spanish hidroxizina (sustancia), hidroxicina (producto), hidroxicina, hidroxizina, hidroxizina (producto), Hidroxizina, Hidroxicina, hidroxicina (sustancia)
Polish Hydroksyzyna
French Hydroxyzine
German Hydroxyzin
Italian Idrossizina
Portuguese Hidroxizina
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Periactin (C0031017)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D003533
English periactin, Periactin
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Atarax (C0684229)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D006919
English atarax, Atarax
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Vistaril (C0936278)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D006919
English vistaril, Vistaril
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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