Pharm 3 Test
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| Where does histamine come from? | Mast cells and basophils
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| Where are mast cells located? | Skin, lungs, gastric, mucosa, brain and other tissues
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| What are the two main types of Histamine receptors? | H1 and H2
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| Where are H1 receptors found? | Respiratory tract and in blood vessels
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| Where are H2 receptors found? | Heart,GI tract, and some blood vessels.
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| What type of Histamine receptors affect Peripheral nerves? | It is unclear.
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| What are the effects of Histamine on the respiratory tract? | nasal congestion, increased secretions, bronchoconstriction
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| What are the effects of Histamine on the Blood vessels? | Arteriolar dilation, decreased blood pressure, causes heat and redness, local edema, swelling
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| What are the effects of Histamine on the GI tract? | Increased gastric acid secretion
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| What are the effects of Histamine on the Peripheral nerves? | Stimulate sensation of nerves, cause itching and pain
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| What type of drugs are H1 receptor blocking drugs, agonists or antagonists? | H1 receptor antagonists
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| What is the MOA of H1 receptor blocking drugs? | They bind to the H1 receptor and occupy the receptor preventing the build up of histamine.
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| Do H1 receptors bind to H2 receptors? | Nope
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| What else do H1 receptor blockers block? | Some block MUSCARINIC cholinergic recptors blocking responses caused by Acetylcholine released from cholinergic nerves?
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| What is a cholinergic nerve? | Any nerve, such as autonomic preganglionic nerves and somatic motor nerves, that releases a cholinergic substance at its terminal points.
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| What does antihistamine do to the respiratory tract? | Decreased but thickened secretions, relieves some nasal congestion/inflammation.
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| What does antihistamine do to the blood vessels? | Antagonism of arteriolar dilation
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| What does antihistamine do to the Heart? | Minor effects, heart rate may increase due to antimuscarinic action.
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| What does antihistamine do to the GI tract? | NONE b/c only H2 receptors are involved here.
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| What does antihistamine do to the CNS? | Drowsiness, sedation
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| What does antihistamine do to the Peripheral nerves? | Local anesthetic affect
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| What are some first generation Antihistamines? | Chlorpheniramine, Diphenhydramine
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| Out of Chlorpheniramine and Diphenhydramine, which one has more H1 blocking activity? | Chlorpheniramine
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| Out of Chlorpheniramine and Diphenhydramine, which one has more sedative effects? | Diphenhydramine
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| Out of Chlorpheniramine and Diphenhydramine, which one has more Anticholinergic effects? | Diphenhydramine
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| What are some second generation Antihistamines? | Cetirizine and Loratadine
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| Out of Cetirizine and Loratadine, which one has more H1 Blocking activity? | Cetirizine
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| Out of Cetirizine and Loratadine, which one has more sedative effects? | They both have low to none.
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| Out of Cetirizine and Loratadine, which one has more Anticholinergic effects? | They both have low to none.
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| What are the clinical uses of antihistamines? | Treatment of allergies, motion sickness, N,V, pruritus, rash, sedation.
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| Which antihistamines treats allergies? | Chlorpheniramine, Loratadine, Cetirizine
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| What antihistamine treats motion sickness? | Dimenhydrinate, Promethanzine
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| Which antihistamine treats nausea and vomiting? | Promethazine
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| Which antihistamine treats pruritus and rash? | Cyproheptadine, Clemastine
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| Which antihistamine is for sedation? | Diphenhydramine, Doxylamine
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| What adverse effects do antihistamines produce? | Sedation, dry mouth, blurred vision, urinary retention, decreased GI motility, diarrhea, constipation.
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| What adverse effects do antihistamines produce in children? | May cause CNS stimulation - insomnia, nervousness, tremors.
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| What adverse effects do antihistamines produce the elderly? | Dizziness, confusion, in coordination, fatigue
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| Are more sedative effects seen in first or second generation antihistamines? | First generation
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| What type of drugs are B2 Adrenergic Receptor Agonists? | bronchodilators
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| How are B2 Adrenergic Receptor Agonists taken? | They are inhaled.
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| Name a short and long acting B2 Adrenergic Receptor Agonists. | Albuterol (Short acting) and Salmeterol (Long acting)
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| How do B2 Adrenergic Receptor Agonists work? | They stimulate B2 adrenergic receptors causing relaxation of bronchial smooth muscle.
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| What is the overall effect of B2 Adrenergic Receptor Agonists? | They dilate and increase lung airflow.
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| What causes mast cells to inhibit the release of histamine? | Stimulation of B2 adrenergic receptors.
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| Which B2 Adrenergic Receptor Agonist relieves acute asthma attacks? | Albuterol
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| Which B2 Adrenergic Receptor Agonist prevents asthma? | Salmetrol
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| What are some adverse effects of B2 Adrenergic Receptor Agonists? | Few adverse effects when given by inhalation, muscle tremor, CNS stimulation, use carefully in pts w/ cardiovascular disease and the elderly.
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| Name all of the groups of Bronchodilator drugs? | B2 Adrenergic Receptor Agonists, Methylxanthines, Tiotropium, Leukotriene receptor blockers
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| Theophylline is a Bronchodilator that belongs to what group? | Mehtylxanthines
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| What are Methlxanthines converted into? | Theophylline
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| How do Methlxanthines work? | They inhibit Phosphodiesterase which destroys cAMP.
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| What does cAMP do in the bronchial smooth muscle cells? | Causes relaxation, bronchodilation, and increased pulmonary airflow.
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| How are Methlxanthines taken to reverse ACUTE bronchoconstriction? | IV
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| How are Methlxanthines taken to prevent bronchoconstriction? | Orally
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| What is a normal plasma level of theophylline? | Is varies greatly.
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| What affects theophylline plasma levels and the their therapeutic effects? | Age, drugs, food, disease
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| In which population is the half-life of theophylline increased? | Newborns and elderly causing toxicity and drug overdose.
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| In what population is the half-life of theophylline decreased? | Pt's who smoke.
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| What does a half-life decrease of theophylline do to the drug and plasma levels? | Reduces plasma levels and effectiveness of drug.
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| What are some adverse effects of Methylaxamines? | CNS effects (anxiety, insomnia), gastric upset,N,V, arrhythmia, convulsion.
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| Can Methylaxamines be given to children and the elderly? | Yes but with caution.
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| Can Methylaxamines be given to pt's with ulcer or cardiovascular disease? | Yes but with caution.
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| What is Tiotropium used for? | It decreased bronchoconstriction in COPD.
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| How does Tiotropium work? | It blocks the bronchoconstrictor action of acetylcholine causing bronchodilation.
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| Can Tiotropium be used outside of the lungs? | Limited b/c its poorly absorbed into the circulation.
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| What are some adverse effects of Tiotropium? | Dry mouth, irritation of upper airways, GI upset
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| Name a Leukotriene receptor blocker. | Montelukast (Singular)
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| What are Leukotrienes? | Mediators released from mast cells that cause bronchoconstriction by stimulation leukotriene receptors on the airway and promote airway inflammation.
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| How does Montelukast work? | It blocks leukotriene receptors to cause BRONCHODILATION and reduce inflammatory responses of the airways.
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| How and for how long are Leukotriene receptor blockers given? | Orally and for long term control/prevention of the symptoms of asthma.
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| What contributes to reduced airflow in asthma? | Airway inflammation
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| What are adverse effects of Leukotriene receptor blockers? | HA, GI upset, joint/muscle pain, muscle soreness, RARELY liver damage
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