Histamine And Serotonin Drugs

Front 1

brompheniramine

Back 1

first gen H1 blocker, anticholinergic activity
IN GENERAL of 1st gen H1 blockers:
rapidly absorbed when taken orally
distributes to most tissues
4-6 hrs duration of action
clinical use: allergic reactions - hay fever, urticaria, not utilized for bronchial asthma
motion sickness- prevention rather than tx, sedative effects, diphenhydramine>cyclizine and meclizine
local anesthetic action - Na channel blockers, diphenhydramine and promethazine are more potent than procaine as local anesthetics
others: antiparkinsonian, anticholinergic, adrenergic-blocking, serotonin-blocking
side effects: slight sedation, anti-muscarinic - urinary retention, blurred vision
interactions: cyp450 inhibition (antifungals), think about sedation when giving other CNS depressants

Front 2

chlorpheniramine

Back 2

first gen H1 blocker, anticholinergic activity
side effects: slight sedation, common component of OTC cold meds

Front 3

clemastine

Back 3

first gen H1 blocker

Front 4

cyclizine

Back 4

first gen H1 blocker, anticholinergic activity
side effects: slight sedation
effects: anti-motion sickness activity

Front 5

cypropheptadine

Back 5

first gen H1 blocker

Front 6

dexchlorpheniramine

Back 6

first gen H1 blocker

Front 7

dimenhydrinate

Back 7

first gen H1 blocker, anticholinergic activity
side effects: marked sedation
effects: anti-motion sickness activity

Front 8

diphenhydramine

Back 8

first gen H1 blocker

Front 9

hydroxyzine

Back 9

first gen H1 blocker

Front 10

meclizine

Back 10

first gen H1 blocker

Front 11

promethazine

Back 11

first generation H1 blocker, anticholinergic activity;
marked sedation, antiemetic, block

Front 12

cetirizine

Back 12

2nd generation H1 blocker, no anticholinergic effects
in general:
12-24 hours duration of action
effects:
allergic reactions - allergic rhinitis and urticaria, not utilized for bronchial asthma
motion sickness - prevention rather than treatment, sedative effects: diphenhydramine > cyclizine and meclizine
local anesthetic action - Na channel blockers, diphenhydramine and prometazine are more potent than procaine as local anesthetics
other effects: antiparkinsonian, anticholinergic, adrenergic blocking, serotonin blocking
toxicity: sedation
drug interactions: cyp450 inhibition (anti-fungals), sedation effect - addnl consideration when given w/ other CNS depressants

Front 13

desloratadine

Back 13

2nd generation H1 blocker, no anticholinergic effects

Front 14

fexofenadine

Back 14

2nd generation H1 blocker, no anticholinergic effects

Front 15

loratadine

Back 15

2nd generation H1 blocker, no anticholinergic effects
longer action

Front 16

azelastine

Back 16

2nd generation H1 blocker, no anticholinergic effects

Front 17

cimetidine

Back 17

H2 blockers
effects: reducing gastric acid secretion - peptic ulcer, GERD, other hypersecretory diseases
little effect on cardiac fxn, intestinal secretion

Front 18

famotidine

Back 18

H2 blockers
effects: reducing gastric acid secretion - peptic ulcer, GERD, other hypersecretory diseases
little effect on cardiac fxn, intestinal secretion

Front 19

nizatidine

Back 19

H2 blockers
effects: reducing gastric acid secretion - peptic ulcer, GERD, other hypersecretory diseases
little effect on cardiac fxn, intestinal secretion

Front 20

ranitidine

Back 20

H2 blockers
effects: reducing gastric acid secretion - peptic ulcer, GERD, other hypersecretory diseases
little effect on cardiac fxn, intestinal secretion

Front 21

cromolyn

Back 21

histamine release inhibitors

Front 22

nedocromil

Back 22

histamine release inhibitors

Front 23

buspirone

Back 23

5-HT receptor agonist
5-HT1A partial agonist
non-benzodiazepine anxiolytic

Front 24

fenfluramine

Back 24

5-HT receptor agonist
5-HT4 agonist

Front 25

dexfenfluramine

Back 25

5-HT receptor agonist
5-HT4 agonist
5-HT2C agonist - appetite suppression, withdrawn due to toxicity

Front 26

cisapride

Back 26

5-HT receptor agonist
5-HT4 agonist
used for the treatment of GERD and motility disorders
available for compassionate use

Front 27

almotriptan

Back 27

selective 5-HT1D and 5-HT1B receptor agonists
other -triptans as well!!!
effects:
counteracts vasodilating peptide calcitonin gene-related peptide (CGRP)
constrict cerebral and meningeal vessels in tx acute migraines
efficacy aginst migraine similar to other classes of drugs
side effects: tingling and warmth sensations, dizziness, muscle weakness, neck pain, chest discomfort (vasospasm, angina)

Front 28

phenoxybenzamine

Back 28

non-selective 5-HT antagonists
5-HT2 antagonist - long acting!! (irreversible (and alpha-adrenergic receptors)

Front 29

cyproheptadine

Back 29

5-HT2 antagonist and H1 receptor antagonist
useful for the smooth muscle effects of carcinoid tumors
serotonin syndrome treatment

Front 30

ondansetron

Back 30

5-HT3 receptor antagonists
other -setrons as well!
used for treatment of nausea/vomiting in cancer chemo

Front 31

dihydroergotamine

Back 31

nonselective 5-HT agonists
limited 5-HT effects
preferred for the treatment of migraine
side effects IN GENERAL:
nausea, vomiting, diarrhea due to increased GIT motility resulting from activation of 5-HT receptors in the CNS and GIT
most serious toxic effect - prolonged vasospasm in the arms/legs, may cause gangrene and amputation
drowsiness and hallucinations occur infrequently

Front 32

ergonovine

Back 32

nonselective 5-HT agonists
most selective for the uterus, if oxytocin fails, is utilized to limit post-partum hemorrhage

Front 33

ergotamine mixtures

Back 33

nonselective 5-HT agonists

Front 34

ergotamine tartrate

Back 34

nonselective 5-HT agonists

Front 35

methylergonovine

Back 35

nonselective 5-HT agonists

Front 36

lysergic acid diethylamine (LSD)

Back 36

nonselective 5-HT agonists
powerful hallucinogen

Front 37

ergotamine

Back 37

nonselective 5-HT agonists
potent vasoconstrictor

Front 38

ergocryptime

Back 38

nonselective 5-HT agonists

Front 39

bromocriptine

Back 39

nonselective 5-HT agonists
in general:
agonists, partial agonists, and antagonists at diverse receptors - alpha adrenergic receptors, 5-HT1A and ID > 5-HT2 and HT3, central dopamine receptors
act at both pre and post-synaptic sites
effects:
CNS - selectivity for pituitary dopamine receptors, suppress prolactin secretion, useful in tx pit tumor

Front 40

cabergoline

Back 40

nonselective 5-HT agonists
effects:
selective for pituitary dopamine receptors, suppress prolactin secretion, useful in tx pituitary tumor

Front 41

tegaserod

Back 41

partial 5-HT4 agonist
utilized for IBS with constipation