Antihistamines & Corticosteroids, and NSAIDs Flashcards Preview

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Flashcards in Antihistamines & Corticosteroids, and NSAIDs Deck (14):
1

Carbinoxamine, Dimenhydrinate, Diphenhydramine

-Ethanolamine antihistamines that have anticholinergic properties alone with H1 antagonism
-Cause sedation, carbinoxamine=slight-moderate, dimenhydrinate and diphenhydramine=marked sedation and anti motion sickness activity
-Tox-urinary retention, blurred vision. nonallergic rhinnorea
-Diphenhydramine can be used as an antiparkinsonism drug and as local anesthetic w/promethiazine

2

MOA of antihistamines

All are H1 antagonists, so their effects are mediated via H2 receptors

3

Hydroxyzine, cyclizine, meclizine

-Piperazine antihistamines
-cause sedation
-cyclizine is the best antihistamine for motion sickness
-meclizine is long acting

4

Brompheniramine, chlorpheiramine

-alkylamine antihistamines that cause slight sedation

5

promethazine

-H1 blocker with less anti-motion sickness action and more sedative and autonomic effects
-has an alpha blocking effect that makes it useful as a local anesthetic and antiemetic

6

cyproheptadine

-H1 antagonist and serotonin 5-ht2 antagonist
-used in carcinoid tumor
-Useful in limiting serotonin effects of bronchospasm and cold induced urticaria

7

Second generation antihistamines-fexofenadine, loratadine, cetirizine

-less distribution into the CNS-->less sedation than 1st generation antihistamines
-metabolized by cyp3a4-c
-used for allergic rhinitis and chronic urticaria

8

Bradykinin, kallidin

-↑ IP3, DAG, cAMP, NO. Dilates arterioles, increases capillary permeability, stimulates sensory nerve endings
-kallidin is a precursor to bradykinin

9

Short acting Glucocorticoids-hydrocortisone, prednisone, methylprednisolone

-Inhibition of phospholipase A2, reduces expression of
cyclooxygenase
-Treatment of severe refractory chronic asthma
-Oral, Duration: 12–24 h

10

Intermediate-acting glucocorticoids-triamcinolone, betamethasone, dexamethasone

-Inhibition of phospholipase A2, reduces expression of
cyclooxygenase
-Give betamethasone to mother if delivery is expected before 34 weeks because it has increased transger across placenta as compared to cortisol

11

Glucocorticoids available as an aerosol-beclomethasone, bedesonide, flunisolide, fluticasone

-MOA-Inhibition of phospholipase A2, reduces expression of cyclooxygenase
-Uses-Prophylaxis of asthma: drugs of choice
-Inhalation, Duration: 10–12 h
-Tox-Pharyngeal candidiasis, minimal systemic steroid
toxicity (eg, adrenal suppression)

12

Mast cell degranulation inhibitors-cromolyn, nedocromil

-mainly for exercise induced asthma, chronic use may slightly reduce bronchial reactivity, NO effect on smooth muscle tone-do not reverse asthmatic bronchospasm, only for prophylactic use, can give to those w/ steroid phobia
-Reduce release of inflammatory and bronchoconstrictor mediators from sensitized mast cells
-Uses-Rarely used prophylaxis of asthma;
-cromolyn also used for ophthalmic, nasopharyngeal, and
gastrointestinal allergy
-Inhaled aerosol for asthma, cromolyn local application
for other applications, Duration: 3–6 h
-Tox-Cough

13

Leukotriene pathway drugs-zileuton, montelukast, zafirlukast

-Principal advantage is that they're taken orally and are therefore great for kids that poorly comply/no need to worry about growth restriction from steroids
-Pharmacologic antagonists at LTD4 receptors Inhibitor of lipoxygenase, reduces synthesis of leukotrienes
-Prophylaxis of asthma
-Oral Duration: 12–24 h
-Tox-Elevation of liver enzymes

14

Omalizumab

-Binds IgE antibodies on mast cells; reduces reaction to
inhaled antigen
-Uses-Prophylaxis of severe, refractory asthma not
responsive to all other drugs
-Parenteral, administered as several courses of injections, Extremely expensive
-long-term toxicity not yet
well documented