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89 Cards in this Set

  • Front
  • Back
Measurement of excessive systemic Histamine (systemic mastocytosis)
Urine Imidazole Acetic Acid (metabolite)
What is the histamine triple response mediated by H1/H2
small red spot at the center of an inradermal injection of histamine surrounded by a red edematous wheal
Distribution of H1?
Mechanism?
Smooth muscle
Gq, ^IP3/DAG
Distribution of H2?
Mechanism?
Stomach, heart, mast cells
Gs, ^cAMP
H3 Distribution?
Mechanism?
CNS
Gi, decrease cAMP
H4 distribution?
Mechanism?
Leukocytes
Gi, decrease cAMP
5-HT1d distribution?
mechanism?
Brain
Gi, decrease cAMP
5-HT2 distribution?
Mechanism?
Smooth Muscle, Platelets
Gq, ^IP3/DAG

vasodilation, diarrhea, bronchoconstriction seen in Carcinoid
5-HT3 Distribution?
Mechanism?
Area Postrema, sensory/enteric
Ligand-Gated Cation Channel fx
5-HT4 Distribution?
Mechanism?
Presynaptic nerve terminals in enteric system
Gs, ^cAMP

important in motility
Cause of vasodilation and endothelial cell contraction with H1?
NO release
Major difference between First and Second generation Antihistamines?
1st generation causes sedation
First Generation H1 antagonists
Dephenhydramine
Chlorpheniramine
Cyclizine
Promethazine
Dimenhydrinate
Second Generation H1 Antagonists
Cetirizine
Fexofenadine
Loratadine
Desloratadine
Why do 1st generation H1 antagonists cause sedation?
enter CNS, effects similar to muscarinic blockers / a-adrenoreceptor blockers (autonomic receptor antagonists)
H1 antag used for management of chemotherapy induced vomiting
Diphenhydramine
which generation of H1 antagonist is used for motion sickness
First Generation
1st Generation H1 Antagonists with most sedating effects
Diphenhydramine
Promethazine
1st generation antagonist with orthostatic hypertension toxicity
Promethazine
Why were the 2nd generation H1 antagonists astemizole and terfenadine removed from the market?
Lethal arrhythmias
Avoidance of what other drugs with H1 antagonists?
CYP Inhibitors
Alcohol
Benzodiazepines
Most toxic H2 antagonist?
Cimetidine
Therapeutic use of H2 Antagonists?

mechanism?
Reduction of Gastric Acid Secretion (ulcers)

prevention, accelerate healing, reduce symptoms
Two syndromes where PPis are preferred over H@ antagonists
GERD
Zollinger-Ellison
Cimetidine Toxicity (3)
CYP Inhibitor
Reduced hepatic blood flow
anti-androgen effects
What is serotonin derived from?
Tryptophan
Detection of excess serotonin (carcinoid)?
5-HIAA in urine
First line treatment of Acute Migraine and Cluster Headaches
-triptans (sumatriptan, naratripan)

5-HT1d AGONISTS
5-HT4 agonist in colon removed from market because of cardiac toxicity
Tegaserod
Components of Fen-Phen?
Dexfenfluramine
Phentermine

removed because of toxicity, was used for weight loss
Common symptoms in Serotonin Syndromes?
Fever
Encephalopathy
Vitals unstable
Elevated Enzymes
Rigidity
Common causes of Serotonin Syndrome
Serotonin Agonists
D2 Blockers (Haloperidol/-azines)
Treatment for Serotonin Syndromes?

(Serotonin Syndrome, Neuroleptic Malignant Syndrome, Malignant Hyperthermia)
Dantrolene (FA)

Diphenhydramine (Pharm)
5-HT2 blockers (3)
Ketanserin
Phenoxybenzamine
Cyproheptadine
5-HT3 blockers (antiemetics)
Ondansetron
Granisetron
Dolasetron
Alosetron (not antiemetic)
Irreversible 5-HT2 blocker
Phenoxybenzamine
Clinical use of 5-HT2 antagonists?
Carcinoid Tumors
Hypertension

(+alpha1 receptor blockade)
5-HT2 antagonist toxicity?
Hypotension
5-HT3 antagonist associated with QRS and QTc prolongation, contraindicated with Heart Disease
Dolasteron
5-HT3 antagonist associated with possibly fatal constipation
Alosetron
Treatment of women with Irritable Bowel Syndrome associated with diarrhea
Alosetron
Chemotherapy and postoperative vomiting treatment
Odansetron + congeners
"St. Anthony's Fire"
Ergot Alkaloid toxicity
Mechanism of Ergotamine vasoconstriction? Previous use?
a-receptor blockade

migraine (with caffeine)
Ergotamine toxicity?
Ischemia and gangrene of limbs
What is used for reduction of postpartum bleeding?
Ergonovine (or ergotamine)
What is essential in use of Ergonovine?
Avoid during pregnancy
DO NOT give until placenta is delivered
Used to reduce size or prolactin producing tumors
Bromocriptine
What could cause a epidemic ergot toxicity outbreak?
spoiled grain
Antitode for Ergot Poisoning?
Nitroprusside
Toxicity of Ergots? (3)
Fibroplasia - hydronephrosis, cardiac valve/conduction malfunction
N/V/D
Abortion
Ergots with potent D2 effects in the basal ganglia
Bromocriptine
Pergolide
Carcinoid Tumors
Serotonin excess - bronchoconstriction, diarrhea, flushing

treatment is 5-HT2 antagonists
physiologic antagonist of H1 actions on SmM?
Epinephrine
blurred vision
older H1 Antagonists
Disease caused by excess ergot alkaloids
St. Anthony's Fire
Endogenous substances commonly interpreted as histamine, serotonin, PGs, and vasoactive peptides
Autocoids
Syndrome of hypersecretion of gastic acid and pepsin usually caused by gastrinoma, associated with severe PUD and diarrhea
ZE
Drug that causes contraction of the uterus
Oxytocin
Distribution of H1
Smooth Muscle
Distribution of H2
Stomach

Heart
Mast Cells
Distribution of H3
CNS
Prototype antagonist of H1
Diphenhydramine
Prototype antagonist of H2 receptors
Cimetridine
1st generation antihistamines that is highly sedating
Diphenhydramine
1st generation antihistamine that is least sedating
Chlorpheniramine
Cyclizine
2nd Generation antihistamines
Fexofenadine
Loratadine
Cetirizine
Generation of antihistamine thathas the mst cNS effects
First generation, more lipid soluble
Major indication for H1 receptor antagonist
Use in IgE mediated allergic reaction
Antihistamine that can be used for anxiety and insomnia and is not addictive
Hydroxyzine (atarax)
H1 antagonist used in motion sickness
Demnhydrinate
Meclizine

(other 1st generations)
Most common SE of 1st generation antihistamines
Sedation
Lethal arrhythmias resulting from concurrent therapy with azole fungals (CYP3A4 metabolized) and these antihistamines which inhibit 3A4 isoenzyme
Terfenadine and Astemizole (removed from market)
H2 blocker that causes the most interactions with other drugs
Cimetidine
Clinical use for H2 blockers
Acid Reflux
Duodenal/Peptic ulcers
receptors for serotonin (5-HT1) are located
Mostly in the brain, and they mediate synaptic inhibition via increased K+ conductance
5HT-1D agonist used for migraine headaches
Sumatriptan
Naratriptan
Rizatriptan
Triptan available in parenteral and nasal formulation
Sumatriptan
H1 blocker that is also a serotonin antagonist
Cyproheptadine
Agents for reduction of postpartum bleeding
Oxytocin
Ergonovine
Ergotamine
Agents used in treatment of carcinoid tumor
Ketaserin
Cyproheptadine
Phenoxybenzamine
5HT-3 antagnoist used in chemotherapeutic induced emesis
Ondansetron
Granisetron
Dolasetron
Alosetron
5HT-3 antagnoist that has been associated with QRS and QTc prolongation and should not be used in patients with heart disease
Dolasetron
DOC to treat chemo-induced nausea and vomiting
Odansetron
Drug used in ergot alkaloids overdose, ischemia and gangrene
Nitroprusside
Reason ergot alkaloids are contraindicated in pregnancy
Uterine contractions
SE or ergot alkaloids
Hallucinations resembling psychosis
Ergot alkaloid used as an illicit drug
LSD
Dopamine agonist used in hyperprolactinemia
Bromocriptine