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Chapter 43
Histamine Pharmacology
29
Pharmacology
Professional
03/29/2012

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Term
Ethanolamines (First Generation H1-Antihistamines)
Definition
Mech: Binds to inactive H1 and prevents its activation
Drugs: Diphenhydramine, Carbinoxamine, Clemastine, Dimenhrydrinate
APP: Allergic rhinitis, Anaphylaxis, Insomnia, Motion sickness, Parkinsonism, Urticaria
AE: Sedation, Dizziness, Pupillary dilation, dry eyes and mouth, Urinary retention
Term
Diphenhydramine
Definition
Class: Ethanolamine (1st generation)
CI: Newborns or premauter infants, and nursing mothers
TC: Available as oral solid or liquid, intramuscular, intravenous and topical
TC: May raise Thioridazine plasma levels, increasing the risk of arrhythmias
Term
Carbinoxamine
Definition
Class: Ethanolamine (1st generation)
CI: Acute asthma attack, MAOI therapy, peptic ulcers, severe coronary artery disease and hypertension, and urinary incontinence
Term
Clemastine
Definition
Class: Ethanolamines (1st generation)
CI: Lactation, LRT symptoms, MAOI therapy, and newborn or premature infants
Term
Dimenhydrinate
Definition
Class: Ethanolamine (1st generation)
CI: Hypersensitivity to itself
Term
Ethylenediamines (First Generation H1-Antihistamines)
Definition
Drugs: Pyrilamine and Tripelennamine
APP: Allergic rhinitis, Anaphylaxis, Insomnia, Motion sickness, Parkinsonism, Urticaria
AE: Sedation, Dizziness, Pupillary dilation, dry eyes and mouth, Urinary retention
Term
Pyrilamine
Definition
Class: Ehtylenediamines (1st generation)
CI: Hypersensitivity to itself
TC: Available as oral solid or liquid, intramuscular, intravenous, and topical.
TC: May raise Thioridazine levels, increasing risk of arrhythmias
Term
Tripelennamine
Definition
Class: Ehtylenediamines (1st generation)
CI: Glaucoma, peptic ulcers , prostatic hypertrophy, bladder neck obstruction, pyloroduodenal obstruction
TC: Available as oral solid or liquid, intramuscular, intravenous, and topical.
TC: May raise Thioridazine levels, increasing risk of arrhythmias
Term
Alkylamines (First Generation H1-Antihistamines)
Definition
Mech: Binds to inactive H1 and prevents its activation
Drugs: Chlorpheniramine and Brompheniramine
APP: Allergic rhinitis, Anaphylaxis, Insomnia, Motion sickness, Parkinsonism, Urticaria
AE: Sedation, Dizziness, Pupillary dilation, dry eyes and mouth, Urinary retention
Term
Chlorheniramine
Definition
Class: Alkylamines (1st generation)
CI: Hypersensitivity to itself
TC: Available as oral solid or liquid, intramuscular, intravenous, and topical.
TC: May raise Thioridazine levels, increasing risk of arrhythmias
Term
Brompheniramine
Definition
Class: Alkylamines (1st generation)
CI: Focal CNS lesions, concurrent MAOI therapy
TC: Available as oral solid or liquid, intramuscular, intravenous, and topical.
TC: May raise Thioridazine levels, increasing risk of arrhythmias
Term
Piperidines (First Generation H1-Antihistamines)
Definition
Mech: Binds to inactive H1 and prevents its activation
Drugs: Cyproheptadine and Phenindamine
APP: Allergic rhinitis, Anaphylaxis, Insomnia, Motion sickness, Parkinsonism, Urticaria
AE: Sedation, Dizziness, Pupillary dilation, dry eyes and mouth, Urinary retention
Term
Cyproheptadine
Definition
Class: Piperidines (1st generation)
CI: Angle-closure glaucoma, newborn or premature infants, nursing mothers, stenosing peptic ulcer
TC: Available as oral solid or liquid, intramuscular, intravenous, and topical.
TC: May raise Thioridazine levels, increasing risk of arrhythmias
Term
Phenindamine
Definition
Class: Piperidines (1st generation)
CI: Children under 12
TC: Available as oral solid or liquid, intramuscular, intravenous, and topical.
TC: May raise Thioridazine levels, increasing risk of arrhythmias
Term
Promethazine
Definition
Class: Phenothiazines (1st generation)

Mech: Binds to inactive H1 and prevents its activation

APP: Allergic rhinitis, Anaphylaxis, Insomnia, Motion sickness, Parkinsonism, Urticaria

AE: Sedation, Dizziness, Pupillary dilation, dry eyes and mouth, Urinary retention, PHOTOSENSITIVITY AND JAUNDICE

CI: COMATOSE STATES, ASTHMA + LRT INFECTIONS, CHILDREN UNDER 2, AND SUBCUTANEOUS OR INTRA-ARTERIAL INJECTION

TC: USED TO RELIEVE PREOPERATIVE ANXIETY AND POST OPERATIVE NAUSEA AND VOMITTING
Term
Piperazines (First generation)
Definition
Drugs: Hydroxyzine, Cyclizine, Meclizine
Mech: Binds to inactive H1 and prevents its activation
APP: Pruritis, Alcohol withdrawal, anxiety, vomitting, motion sickness, and vertigo
AE: Sedation, Dizziness, Pupillary dilation, dry eyes and mouth, Urinary retention
Term
Hydroxyzine
Definition
Class: Piperazines (1st generation)
APP: Pruritus, Alchohol withdrawal, anxiety, and vomitting
CI: Early pregnancy
TC: Antipuritic
Term
Cyclizine and Meclizine
Definition
Class: Piperazines (1st generation)
APP: Motion sickness, vertigo
CI: Hypersensitivity to self
Term
Doxepin
Definition
Class: Tricyclic dibenzoxepins (1st generation)
Mech: Binds to inactive H1 and prevents its activation
APP: Anxiety, Depression, and Pruritis
AE: Hypertension, hypotension, agranulocytosis, thrombocytopenia, worsening depression, suicidal thoughts, weight gain, etc..
CI: Glaucoma and Urinary retention
TC: Tricyclic antidepressant, and can cause confusion and disorientation in non depressed patients
Term
Piperazines (Second generation)
Definition
Drugs: Cetirizine and Lecocetirizine

Mech: Binds to inactive H1 and prevents its activation
APP: Allergic Rhinitis and Uticaria

AE: Somnolence, dry mouth, headache, fatigue (less than other piperazines)
CI: Allergies to self
Term
Cetirizine and Lecocetirizine
Definition
Class: Piperazines (2nd generation)
APP: Allergic Rhinitis and Uticaria
Term
Acrivastine
Definition
Class: Alkylamine (2nd generation
Mech: Binds to inactive H1 and prevents its activation

APP: Allergic Rhinitis
AE: Somnolence, dry mouth, headache, fatigue

CI: Concurrent MAOI therapy, severe coronary artery disease and severe hypertension
TC: Less anticholinergic effects than first generation
Term
Piperidines (second generation)
Definition
Drugs: Loratadine, Desloratadine, Levocabastine, Eebastine, Mizolastine, Fexofenadine
Mech: Binds to inactive H1 and prevents its activation
APP: Allergic rhinitis and Urticaria
AE: Somnolence, dry mouth, headache, fatigue
Term
Levocabastine
Definition
Class: Piperidines (2nd generation)
APP: Allergic rhinitis and Urticaria
CI: Soft contact lenses
Term
Azelastine
Definition
Class: Second generation Phthalazinones
Mech: Binds to inactive H1 and prevents its activation

APP: Allergic Rhinitis, VASOMOTOR RHINITIS, Allergic Conjunctivitis
AE: Somnolence, dry mouth, headache, fatigue, BITTER TASTE AND EPISTAXIS

CI: Concurrent use of Alcohol or CNS depressants
TC: Nasal Spray or ophthalmic solution
Term
Olopatadine
Definition
Class: Tricyclic dibenzozipins (2nd generation)
Mech: Binds to inactive H1 and prevents its activation

APP: Allergic Rhinitis and Allergic Conjunctivitis
AE: Somnolence, dry mouth, headache, fatigue, BITTER TASTE AND EPISTAXIS

CI: Concurrent use of Alcohol or CNS depressants
TC: Nasal Spray or ophthalmic solution
Term
Imidazole acetic acid
Definition
The compound in the urine used to measure histamine levels
Term
Hystidine decarboxylase
Definition
Activated for the ingestion of food
Term
Loratadine, Desloratadine, Ebastine, Mizolastine, and Fexofenadine
Definition
Class: Piperidines (2nd generation)
APP: Allergic rhinitis and Urticaria
CI: Hypersensitivity to drug
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