Chapter 189 - Antihistamines Flashcards
TABLE 189-1
Basic Pharmacology of Antihistamines
Fill in the blanks
_____ antihistamines are _____ agonists that reversibly bind and stabilize the inactive form of the histamine receptor, thereby favoring the inactive state.
Both H1 and H2 antihistamines are inverse agonists that reversibly bind and stabilize the inactive form of the histamine receptor, thereby favoring the inactive state.
TABLE 189-1
Basic Pharmacology of Antihistamines
Fill in the blanks
_____ agents are relatively lipophilic, which enhances penetration of the blood–brain barrier and leads to sedation.
First-generation H1 agents are relatively lipophilic, which enhances penetration of the blood–brain barrier and leads to sedation.
TABLE 189-1
Basic Pharmacology of Antihistamines
Fill in the blanks
_____ antihistamines may interact with other drugs metabolized by the hepatic cytochrome P450 system leading to drug–drug interactions.
First-generation H1 antihistamines may interact with other drugs metabolized by the hepatic cytochrome P450 system leading to drug–drug interactions.
TABLE 189-1
Basic Pharmacology of Antihistamines
Fill in the blanks
_____ antihistamines have poor penetration of the blood–brain barrier and thus are less sedating.
Second-generation H1 antihistamines have poor penetration of the blood–brain barrier and thus are less sedating.
TABLE 189-1
Basic Pharmacology of Antihistamines
Fill in the blanks
_____ antihistamines bind selectively to peripheral H1 receptors and have fewer CNS effects.
Second-generation H1 antihistamines bind selectively to peripheral H1 receptors and have fewer CNS effects.
TABLE 189-1
Basic Pharmacology of Antihistamines
Fill in the blanks
_____ antihistamines require less hepatic metabolism and thus are less likely to interact with other medications.
Second-generation H1 antihistamines require less hepatic metabolism and thus are less likely to interact with other medications.
TABLE 189-1
Basic Pharmacology of Antihistamines
Fill in the blanks
There is no evidence of _____ or _____ to first-generation or second-generation antihistamines.
There is no evidence of tolerance or tachyphylaxis to first-generation or second-generation antihistamines.
TABLE 189-2 vs TABLE 189-6
Indications for Treatment with H1 Antihistamines vs Dermatologic Indications for Treatment with H2 Antihistamines
Acute urticaria
H1 Antihistamines
TABLE 189-2 vs TABLE 189-6
Indications for Treatment with H1 Antihistamines vs Dermatologic Indications for Treatment with H2 Antihistamines
Chronic idiopathic urticarial
H1 Antihistamines
TABLE 189-2 vs TABLE 189-6
Indications for Treatment with H1 Antihistamines vs Dermatologic Indications for Treatment with H2 Antihistamines
Physical urticarias and dermatographism
H1 Antihistamines
TABLE 189-2 vs TABLE 189-6
Indications for Treatment with H1 Antihistamines vs Dermatologic Indications for Treatment with H2 Antihistamines
Pruritus associated with histamine release
H1 Antihistamines
TABLE 189-2 vs TABLE 189-6
Indications for Treatment with H1 Antihistamines vs Dermatologic Indications for Treatment with H2 Antihistamines
Symptoms of mastocytosis
H1 Antihistamines
TABLE 189-2 vs TABLE 189-6
Indications for Treatment with H1 Antihistamines vs Dermatologic Indications for Treatment with H2 Antihistamines
Acute allergic reactions
H2 Antihistamines
TABLE 189-2 vs TABLE 189-6
Indications for Treatment with H1 Antihistamines vs Dermatologic Indications for Treatment with H2 Antihistamines
Chronic urticaria (as a second-line agent)
H2 Antihistamines
TABLE 189-2 vs TABLE 189-6
Indications for Treatment with H1 Antihistamines vs Dermatologic Indications for Treatment with H2 Antihistamines
Systemic symptoms associated with mastocytosis (especially GI related)
H2 Antihistamines
TABLE 189-3
Dosing Regimens for H1 Antihistamines
CONDITIONS REQUIRING
DOSAGE ADJUSTMENT
Hepatic vs Renal vs Both
Chlorpheniramine
Hepatic impairment
TABLE 189-3
Dosing Regimens for H1 Antihistamines
CONDITIONS REQUIRING
DOSAGE ADJUSTMENT
Hepatic vs Renal vs Both
Cyproheptadine
Hepatic impairment
TABLE 189-3
Dosing Regimens for H1 Antihistamines
CONDITIONS REQUIRING
DOSAGE ADJUSTMENT
Hepatic vs Renal vs Both
Diphenhydramine
Hepatic impairment
TABLE 189-3
Dosing Regimens for H1 Antihistamines
CONDITIONS REQUIRING
DOSAGE ADJUSTMENT
Hepatic vs Renal vs Both
Hydroxyzine
Hepatic impairment
TABLE 189-3
Dosing Regimens for H1 Antihistamines
CONDITIONS REQUIRING
DOSAGE ADJUSTMENT
Hepatic vs Renal vs Both
Tripelennamine
Hepatic impairment
TABLE 189-3
Dosing Regimens for H1 Antihistamines
CONDITIONS REQUIRING
DOSAGE ADJUSTMENT
Hepatic vs Renal vs Both
Acrivastine
Renal impairment
TABLE 189-3
Dosing Regimens for H1 Antihistamines
CONDITIONS REQUIRING
DOSAGE ADJUSTMENT
Hepatic vs Renal vs Both
Azelastine
Renal and hepatic impairment
TABLE 189-3
Dosing Regimens for H1 Antihistamines
CONDITIONS REQUIRING
DOSAGE ADJUSTMENT
Hepatic vs Renal vs Both
Cetirizine
Renal and hepatic impairment
TABLE 189-3
Dosing Regimens for H1 Antihistamines
CONDITIONS REQUIRING
DOSAGE ADJUSTMENT
Hepatic vs Renal vs Both
Desloratadine
Renal and hepatic impairment
TABLE 189-3
Dosing Regimens for H1 Antihistamines
CONDITIONS REQUIRING
DOSAGE ADJUSTMENT
Hepatic vs Renal vs Both
Ebastine
Renal impairment
TABLE 189-3
Dosing Regimens for H1 Antihistamines
CONDITIONS REQUIRING
DOSAGE ADJUSTMENT
Hepatic vs Renal vs Both
Fexofenadine
Renal impairment
TABLE 189-3
Dosing Regimens for H1 Antihistamines
CONDITIONS REQUIRING
DOSAGE ADJUSTMENT
Hepatic vs Renal vs Both
Levocetirizine
Renal and hepatic impairment
TABLE 189-3
Dosing Regimens for H1 Antihistamines
CONDITIONS REQUIRING
DOSAGE ADJUSTMENT
Hepatic vs Renal vs Both
Loratadine
Renal and hepatic impairment
TABLE 189-3
Dosing Regimens for H1 Antihistamines
CONDITIONS REQUIRING
DOSAGE ADJUSTMENT
Hepatic vs Renal vs Both
Mizolastine
Hepatic impairment
TABLE 189-7
Dosing Regimens for H2 Antihistamines
CONDITIONS REQUIRING
DOSAGE ADJUSTMENT
Hepatic vs Renal vs Both
Cimetidine
Renal or hepatic impairment
TABLE 189-7
Dosing Regimens for H2 Antihistamines
CONDITIONS REQUIRING
DOSAGE ADJUSTMENT
Hepatic vs Renal vs Both
Ranitidine
Renal impairment
TABLE 189-7
Dosing Regimens for H2 Antihistamines
CONDITIONS REQUIRING
DOSAGE ADJUSTMENT
Hepatic vs Renal vs Both
Famotidine
Renal impairment
TABLE 189-7
Dosing Regimens for H2 Antihistamines
CONDITIONS REQUIRING
DOSAGE ADJUSTMENT
Hepatic vs Renal vs Both
Nizatidine
Renal impairment
TABLE 189-3 vs TABLE 189-7
Dosing Regimens for H1 Antihistamines vs Dosing Regimens for H2 Antihistamines
1st gen H1 vs 2nd gen H1 vs H2
Chlorpheniramine
1st gen H1
TABLE 189-3 vs TABLE 189-7
Dosing Regimens for H1 Antihistamines vs Dosing Regimens for H2 Antihistamines
1st gen H1 vs 2nd gen H1 vs H2
Cyproheptadine
1st gen H1
TABLE 189-3 vs TABLE 189-7
Dosing Regimens for H1 Antihistamines vs Dosing Regimens for H2 Antihistamines
1st gen H1 vs 2nd gen H1 vs H2
Diphenhydramine
1st gen H1
TABLE 189-3 vs TABLE 189-7
Dosing Regimens for H1 Antihistamines vs Dosing Regimens for H2 Antihistamines
1st gen H1 vs 2nd gen H1 vs H2
Hydroxyzine
1st gen H1
TABLE 189-3 vs TABLE 189-7
Dosing Regimens for H1 Antihistamines vs Dosing Regimens for H2 Antihistamines
1st gen H1 vs 2nd gen H1 vs H2
Tripelennamine
1st gen H1
TABLE 189-3 vs TABLE 189-7
Dosing Regimens for H1 Antihistamines vs Dosing Regimens for H2 Antihistamines
1st gen H1 vs 2nd gen H1 vs H2
Acrivastine
2nd gen H1
TABLE 189-3 vs TABLE 189-7
Dosing Regimens for H1 Antihistamines vs Dosing Regimens for H2 Antihistamines
1st gen H1 vs 2nd gen H1 vs H2
Azelastine
2nd gen H1
TABLE 189-3 vs TABLE 189-7
Dosing Regimens for H1 Antihistamines vs Dosing Regimens for H2 Antihistamines
1st gen H1 vs 2nd gen H1 vs H2
Cetirizine
2nd gen H1
TABLE 189-3 vs TABLE 189-7
Dosing Regimens for H1 Antihistamines vs Dosing Regimens for H2 Antihistamines
1st gen H1 vs 2nd gen H1 vs H2
Desloratadine
2nd gen H1
TABLE 189-3 vs TABLE 189-7
Dosing Regimens for H1 Antihistamines vs Dosing Regimens for H2 Antihistamines
1st gen H1 vs 2nd gen H1 vs H2
Ebastine
2nd gen H1
TABLE 189-3 vs TABLE 189-7
Dosing Regimens for H1 Antihistamines vs Dosing Regimens for H2 Antihistamines
1st gen H1 vs 2nd gen H1 vs H2
Fexofenadine
2nd gen H1
TABLE 189-3 vs TABLE 189-7
Dosing Regimens for H1 Antihistamines vs Dosing Regimens for H2 Antihistamines
1st gen H1 vs 2nd gen H1 vs H2
Levocetirizine
2nd gen H1
TABLE 189-3 vs TABLE 189-7
Dosing Regimens for H1 Antihistamines vs Dosing Regimens for H2 Antihistamines
1st gen H1 vs 2nd gen H1 vs H2
Loratadine
2nd gen H1
TABLE 189-3 vs TABLE 189-7
Dosing Regimens for H1 Antihistamines vs Dosing Regimens for H2 Antihistamines
1st gen H1 vs 2nd gen H1 vs H2
Mizolastine
2nd gen H1
TABLE 189-3 vs TABLE 189-7
Dosing Regimens for H1 Antihistamines vs Dosing Regimens for H2 Antihistamines
1st gen H1 vs 2nd gen H1 vs H2
Cimetidine
H2
TABLE 189-3 vs TABLE 189-7
Dosing Regimens for H1 Antihistamines vs Dosing Regimens for H2 Antihistamines
1st gen H1 vs 2nd gen H1 vs H2
Famotidine
H2
TABLE 189-3 vs TABLE 189-7
Dosing Regimens for H1 Antihistamines vs Dosing Regimens for H2 Antihistamines
1st gen H1 vs 2nd gen H1 vs H2
Ranitidine
H2
TABLE 189-3 vs TABLE 189-7
Dosing Regimens for H1 Antihistamines vs Dosing Regimens for H2 Antihistamines
1st gen H1 vs 2nd gen H1 vs H2
Nizatidine
H2
TABLE 189-4
Factors for Risk-to-Benefit Assessment of
First-generation H1 Antihistamine Therapy
Risk vs Contraindication
History of cardiac arrhythmias, particularly ventricular arrhythmias
Risk
TABLE 189-4
Factors for Risk-to-Benefit Assessment of
First-generation H1 Antihistamine Therapy
Risk vs Contraindication
First trimester of pregnancy
Risk
TABLE 189-4
Factors for Risk-to-Benefit Assessment of
First-generation H1 Antihistamine Therapy
Risk vs Contraindication
Prostatic hypertrophy
Risk
TABLE 189-4
Factors for Risk-to-Benefit Assessment of
First-generation H1 Antihistamine Therapy
Risk vs Contraindication
Narrow-angle glaucoma
Contraindication
TABLE 189-4
Factors for Risk-to-Benefit Assessment of
First-generation H1 Antihistamine Therapy
Risk vs Contraindication
Concomitant use of monoamine oxidase inhibitors
Contraindication