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