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74 Cards in this Set

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What are the types of histamine blockers?
H1 blockers (1/2 generation)
H2 blockers
What 2 serotonin receptors do we use agonists for? antagonists?
5-HT1 and 5-HT4

5-HT2 and 5-HT3
___ is found in neurons, mast cells and is metabolized by monoamine oxidase.
histamine
Diphenhydramine?
Sumatriptan?
First Generation H1
5-HT
Loratadine
dimenhydranate
chlorpheniramine
desloratadine
2nd gen HI
1st gen H1
1st gen H1
2nd gen H1
Fexofenadine and cetirizine?
2nd gen H1
Promethazine and hydroxyzine?
1st gen H1
The 4 places that histamine is stored/released?
GI mucosa, CNS, mast cells, basophils
What immunoglobulin triggers histamine release from mast cells?

What 3 drugs induce histamine release?
IgE

Morphine, penicillin, vancomycin
What effect does histamine have on the Airway, GI, and Blood Vessels?
Bronchoconstriction mainly

Acid secretion D/V

VD/ increased vascular permability
Bronchoconstriction, Intestinal cramps, VD, edema, pain, itching?
H1 receptor on SMOOTH MUSCLE
Controls gastric acid secretion and stimulates cardiac muscle?
H2 receptor
Where are H3 and H4 receptors found?
CNS

Immune system (eosinophils)
used to be used for testing of bronchial hyperactivity and testing gastric acid secretion, but NO LONGER used?
histamine - we mainly used anti-histamines
Histamine has opposite effects on smooth muscle than ___ which is used in life saving anaphylaxis?
epi
___ is useful in asthma prophylaxis (blocks degranulation of mast cells)
cromolyn
which H1 receptor is More lipophilic? 1st of 2nd generation?
1st is more lipophilic

2nd is less lipophilic
Can be used as anti-emetic, parkinson's disease, type-1-hypersensitivity, allergic dermatoses?
H1 receptor antagonists
Can be used for antiparkinsonism (suppresses extrapyramidal symptoms associated with antipsychotic drugs)
dephenhydramine (H1 1st gen)
used to reduce allergic rxns and is very sedating?
diphenhydramine (h1 1st gen)
What drug can potentiate CNS depressants like opiates so you actually need less optiods?
diphenhydramine (h1 1st gen)
Used exclusively for prevention of motion sickness? It's salt anyways
dimenhydranate (dramamine) 1st Gen h1
a drug that is a potent local anesthetic, sedation, and anti-emetic. also weak dopamine antagonist?
promethazine (H1 1st gen)
that is phenergan
SE include neuroleptic malignant syndrome; produces alpha-blockage; orthostatic HypoTension; tachy; dizz
Promethazine (h1 1st gen)

it is phenergan
used mainly to treat general anxiety and reduce alcohol withdrawl?
hydroxyzine (1st gen H1)
What the major difference between H1 1st and 2nd gen antagonists?
2nd generation has much less sedation effects
Are 1st or 2nd generation antihistamines more selective for H1 receptors?
2nd generations are - thats why less sedation b/c don't go to brain
What drug has double the half-life of the 2nd gen H1 Loratadine (clairitin)?
desloratadine (clarinex)
Again where do H1 and H2 act?
H1 = smooth muscle and CNS

H2 = gastric mucosa and cardiac stimulant
H2 receptors mainly act on ___ and have few side effects except what drug?
GI mucosa (blocks g-acid)

cimetidine
Bulimia, panic, OCD, and depression would be associated with?
decreased serotonin levels (5-HT)
The 5-HT1 agonists end in " ----"
tryptans
DOC for acute migraine?
sumatriptan - 5HT1 agonist
inhibit vomiting reflex from chemo?
ondansetron (5HT3) are the setrons
i'm assuming i'm a trip if i don't my medication for my migraine?
sumatriptan
used for chronic constipation and is 5HT4 agonist but restricted use d/t CV toxicity?
Tegaserod
Ergot alkaloids are from wet/spoiled grains and responsible for ____?
st. anthony's fire
ergot alkaloids are partial ___ and ___ agonists?
alpha and 5-HT (serotonin)
an OD can cause ischemia and gangrene; causes VC
ergotamine
powerful uterine contraction and can cause abortion/miscarriage (ergot)
ergonovine
main stay for migraine treatment besides sumatriptan?
ergotamine
used in hyperprolactinemia to reduce prolactin secretion?
bromocriptine
nitropurusside can be used as an antagonist to what drug class?
ergots
What is one of the main effects of serotonin?
bronchospasm
most useful in treatment of carcinoid tumors?
Sumatriptan
what drug can reverse 1 or more smooth muscle effects of circulating histamine?
Epinephrine
many H1 blockers have nonhistamine effects including?
anti-motion sickness effects
if you block H2 receptors what happens to cAMP in the heart?
decreases
toxicities of H2 antihistamines include:
p450 inhibition
what drug is used to treat chemo induced vomiting?
ondansetron
cetirizine is used for? H1 2nd gen
hay fever
which drug is used to treat hyperprolactinemia?
bromocriptine
which drugs are used to treat peptic ulcers?
cimetidine - H2 blocker
cetrizine is used for __ and is a __
cimetidine is a ___ and used for __
2nd Gen H1 - hay fever
H2 - Peptic ulcers
what drug is used for migraines and is not fungus derived?
sumatriptan - 5HT1
what drug is used to reverse ergot induced vasospasm?
nitroprusside
what effect do theophylline, nitro, isoproterenol, and histamine have in common?
Tachycardia
does albuterol have a diuretic effect?
NO
does nedocromil or cromolyn have direct bronchodilator effects?
no they are only prophylactic
what does not play a role in asthma? histamine, leukotriene, antigens, PLA2
histamine
Theophylline is a bronchodilator active by the ___ route
oral
what drug is life saving in status asthmaticus and inhibits PLA2
prednisone
what asthmatic drug has OD toxicity that includes insomnia, arrhythmias, and convulsions?
aminophylline
anti IgE antibody keeps IgE from binding to mast cells; reduces frequency and severity of asthma exacerbations.
omalizumab
stabilizes mast cell and inhibits degranulation? NO use in acute attacks and is DOC for asthma in children
cromolyn
ADR is inhibition of P450; used for prophylactic asthma in children; reversible inhibitor of leukotriene receptors
lukasts (montelukast and zifurlukast)
inhibits 5-lipooxygenase but is extremely hepatotoxic?
zileuton
methylxanthine derivative inhibits phosphodiesterase leading to increased cAMP
theophylline
muscarinic receptor antagonist (m2/m3) used in asthma + COPD
ipratropium
stabilize mast cell and inhibit degranulation; increase mucociliary clearance; NO anti-inflammatory properties so not used for monotherapy in asthma?
beta2 agonists
___ do not effect bronchodilation, they work by decreasing inflammatory cascade; They also inhibit ___
corticosteroids; PLA2
budesonide; beclomethasone, fluticasone
corticosteroid used in asthma
most effective for cough?

most widely used for cough?
opiods

non-opiods (DXM)
a non-narcotic antitussive derivative of procaine used to anesthetize the stretch receptors
benzonatate