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89 Cards in this Set
- Front
- Back
Measurement of excessive systemic Histamine (systemic mastocytosis)
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Urine Imidazole Acetic Acid (metabolite)
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What is the histamine triple response mediated by H1/H2
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small red spot at the center of an inradermal injection of histamine surrounded by a red edematous wheal
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Distribution of H1?
Mechanism? |
Smooth muscle
Gq, ^IP3/DAG |
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Distribution of H2?
Mechanism? |
Stomach, heart, mast cells
Gs, ^cAMP |
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H3 Distribution?
Mechanism? |
CNS
Gi, decrease cAMP |
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H4 distribution?
Mechanism? |
Leukocytes
Gi, decrease cAMP |
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5-HT1d distribution?
mechanism? |
Brain
Gi, decrease cAMP |
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5-HT2 distribution?
Mechanism? |
Smooth Muscle, Platelets
Gq, ^IP3/DAG vasodilation, diarrhea, bronchoconstriction seen in Carcinoid |
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5-HT3 Distribution?
Mechanism? |
Area Postrema, sensory/enteric
Ligand-Gated Cation Channel fx |
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5-HT4 Distribution?
Mechanism? |
Presynaptic nerve terminals in enteric system
Gs, ^cAMP important in motility |
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Cause of vasodilation and endothelial cell contraction with H1?
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NO release
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Major difference between First and Second generation Antihistamines?
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1st generation causes sedation
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First Generation H1 antagonists
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Dephenhydramine
Chlorpheniramine Cyclizine Promethazine Dimenhydrinate |
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Second Generation H1 Antagonists
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Cetirizine
Fexofenadine Loratadine Desloratadine |
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Why do 1st generation H1 antagonists cause sedation?
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enter CNS, effects similar to muscarinic blockers / a-adrenoreceptor blockers (autonomic receptor antagonists)
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H1 antag used for management of chemotherapy induced vomiting
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Diphenhydramine
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which generation of H1 antagonist is used for motion sickness
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First Generation
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1st Generation H1 Antagonists with most sedating effects
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Diphenhydramine
Promethazine |
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1st generation antagonist with orthostatic hypertension toxicity
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Promethazine
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Why were the 2nd generation H1 antagonists astemizole and terfenadine removed from the market?
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Lethal arrhythmias
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Avoidance of what other drugs with H1 antagonists?
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CYP Inhibitors
Alcohol Benzodiazepines |
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Most toxic H2 antagonist?
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Cimetidine
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Therapeutic use of H2 Antagonists?
mechanism? |
Reduction of Gastric Acid Secretion (ulcers)
prevention, accelerate healing, reduce symptoms |
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Two syndromes where PPis are preferred over H@ antagonists
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GERD
Zollinger-Ellison |
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Cimetidine Toxicity (3)
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CYP Inhibitor
Reduced hepatic blood flow anti-androgen effects |
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What is serotonin derived from?
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Tryptophan
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Detection of excess serotonin (carcinoid)?
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5-HIAA in urine
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First line treatment of Acute Migraine and Cluster Headaches
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-triptans (sumatriptan, naratripan)
5-HT1d AGONISTS |
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5-HT4 agonist in colon removed from market because of cardiac toxicity
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Tegaserod
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Components of Fen-Phen?
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Dexfenfluramine
Phentermine removed because of toxicity, was used for weight loss |
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Common symptoms in Serotonin Syndromes?
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Fever
Encephalopathy Vitals unstable Elevated Enzymes Rigidity |
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Common causes of Serotonin Syndrome
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Serotonin Agonists
D2 Blockers (Haloperidol/-azines) |
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Treatment for Serotonin Syndromes?
(Serotonin Syndrome, Neuroleptic Malignant Syndrome, Malignant Hyperthermia) |
Dantrolene (FA)
Diphenhydramine (Pharm) |
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5-HT2 blockers (3)
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Ketanserin
Phenoxybenzamine Cyproheptadine |
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5-HT3 blockers (antiemetics)
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Ondansetron
Granisetron Dolasetron Alosetron (not antiemetic) |
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Irreversible 5-HT2 blocker
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Phenoxybenzamine
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Clinical use of 5-HT2 antagonists?
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Carcinoid Tumors
Hypertension (+alpha1 receptor blockade) |
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5-HT2 antagonist toxicity?
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Hypotension
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5-HT3 antagonist associated with QRS and QTc prolongation, contraindicated with Heart Disease
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Dolasteron
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5-HT3 antagonist associated with possibly fatal constipation
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Alosetron
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Treatment of women with Irritable Bowel Syndrome associated with diarrhea
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Alosetron
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Chemotherapy and postoperative vomiting treatment
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Odansetron + congeners
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"St. Anthony's Fire"
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Ergot Alkaloid toxicity
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Mechanism of Ergotamine vasoconstriction? Previous use?
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a-receptor blockade
migraine (with caffeine) |
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Ergotamine toxicity?
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Ischemia and gangrene of limbs
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What is used for reduction of postpartum bleeding?
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Ergonovine (or ergotamine)
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What is essential in use of Ergonovine?
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Avoid during pregnancy
DO NOT give until placenta is delivered |
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Used to reduce size or prolactin producing tumors
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Bromocriptine
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What could cause a epidemic ergot toxicity outbreak?
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spoiled grain
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Antitode for Ergot Poisoning?
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Nitroprusside
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Toxicity of Ergots? (3)
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Fibroplasia - hydronephrosis, cardiac valve/conduction malfunction
N/V/D Abortion |
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Ergots with potent D2 effects in the basal ganglia
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Bromocriptine
Pergolide |
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Carcinoid Tumors
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Serotonin excess - bronchoconstriction, diarrhea, flushing
treatment is 5-HT2 antagonists |
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physiologic antagonist of H1 actions on SmM?
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Epinephrine
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blurred vision
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older H1 Antagonists
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Disease caused by excess ergot alkaloids
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St. Anthony's Fire
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Endogenous substances commonly interpreted as histamine, serotonin, PGs, and vasoactive peptides
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Autocoids
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Syndrome of hypersecretion of gastic acid and pepsin usually caused by gastrinoma, associated with severe PUD and diarrhea
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ZE
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Drug that causes contraction of the uterus
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Oxytocin
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Distribution of H1
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Smooth Muscle
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Distribution of H2
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Stomach
Heart Mast Cells |
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Distribution of H3
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CNS
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Prototype antagonist of H1
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Diphenhydramine
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Prototype antagonist of H2 receptors
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Cimetridine
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1st generation antihistamines that is highly sedating
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Diphenhydramine
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1st generation antihistamine that is least sedating
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Chlorpheniramine
Cyclizine |
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2nd Generation antihistamines
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Fexofenadine
Loratadine Cetirizine |
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Generation of antihistamine thathas the mst cNS effects
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First generation, more lipid soluble
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Major indication for H1 receptor antagonist
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Use in IgE mediated allergic reaction
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Antihistamine that can be used for anxiety and insomnia and is not addictive
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Hydroxyzine (atarax)
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H1 antagonist used in motion sickness
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Demnhydrinate
Meclizine (other 1st generations) |
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Most common SE of 1st generation antihistamines
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Sedation
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Lethal arrhythmias resulting from concurrent therapy with azole fungals (CYP3A4 metabolized) and these antihistamines which inhibit 3A4 isoenzyme
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Terfenadine and Astemizole (removed from market)
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H2 blocker that causes the most interactions with other drugs
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Cimetidine
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Clinical use for H2 blockers
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Acid Reflux
Duodenal/Peptic ulcers |
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receptors for serotonin (5-HT1) are located
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Mostly in the brain, and they mediate synaptic inhibition via increased K+ conductance
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5HT-1D agonist used for migraine headaches
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Sumatriptan
Naratriptan Rizatriptan |
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Triptan available in parenteral and nasal formulation
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Sumatriptan
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H1 blocker that is also a serotonin antagonist
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Cyproheptadine
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Agents for reduction of postpartum bleeding
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Oxytocin
Ergonovine Ergotamine |
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Agents used in treatment of carcinoid tumor
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Ketaserin
Cyproheptadine Phenoxybenzamine |
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5HT-3 antagnoist used in chemotherapeutic induced emesis
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Ondansetron
Granisetron Dolasetron Alosetron |
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5HT-3 antagnoist that has been associated with QRS and QTc prolongation and should not be used in patients with heart disease
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Dolasetron
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DOC to treat chemo-induced nausea and vomiting
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Odansetron
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Drug used in ergot alkaloids overdose, ischemia and gangrene
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Nitroprusside
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Reason ergot alkaloids are contraindicated in pregnancy
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Uterine contractions
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SE or ergot alkaloids
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Hallucinations resembling psychosis
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Ergot alkaloid used as an illicit drug
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LSD
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Dopamine agonist used in hyperprolactinemia
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Bromocriptine
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