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Saba - Basic Sciences - Semester 4 - Pharm - Blk3 - Lect01

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show Self-remedy is the primary function of this groups of pharmacological agents  
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show Histamine, Eicosanoids and Serotonin are the 3 members of this class of pharmacological agents  
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Autocoids - Main Adverse Effect   show
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show This endogenous compound is a monoamine autocoid.  
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Histamine - Storage - Cellular   show
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Histamine - Storage - Tissues (3)   show
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show In the GIT, this autocoid serves to induce hydrochloric acid secretion  
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Histamine - Storage - Tissues - Lungs - Function   show
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Histamine - Storage - Tissues - Skin - Function   show
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Histamine - Storage - Dysfunction   show
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Histamine - Release - Triggers (5)   show
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show This autocoid is triggered by the release of drugs, among other things, including morphine and tubocurarine.  
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Histamine - Release - Triggers -Drugs - Tubocurarine & Morphine - Mechanism   show
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Histamine - Receptors - Number of Types   show
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show This histamine receptor is membrane bound and Gq-coupled receptors, increasing IP3, DAG and calcium conc.  
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show This histamine receptors is located in the lungs, skin, GIT, heart, brain, leukocytes and vascular smooth muscle  
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Histamine - Receptors - H1 - Functions   show
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show This histamine receptor is membrane bound and Gs-coupled, increasing cAMP conc.  
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show This histamine receptors is located in the GIT, heart, and sensory nerve endings  
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show This histamine receptor serves to induce gastric acid secretion (gastric ulcers), and increase SA nodal rate, positive ionotropism and automaticity (cardiac arrhythmias)  
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Antihistaminics – Classification - Functional differences between 1st and 2nd Generation (2)   show
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show Second generation agents have far fewer autonomic effects (anticholinergic, antiadrenergic effects), and little or no sedative effect compared to the first generation antihistaminics  
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show This class of antihistaminics includes: Chlorpheniramine, Cyclizine, Cyproheptadine, Diphenhydramine, Dimenhydrinate, Doxepin***, Doxylamine, Hydroxyzine, Meclizine, and Promethazine  
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show This class of antihistaminics includes: Acrivastine, Astemizole, Azelastine, Cetirizine, Desloratadine, Fexofenadine, Loratadine, and Terfenadine  
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Antihistaminics – Classification –Second Generation – Terfenadine – Usage Status   show
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show Members of this drug class vary in pharmacokinetic properties, but all require hepatic metabolism, most cross the placental barrier, and many are available OTC, both alone and in combination formulations such as “cold pills” and “sleep aids”.  
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show This class of drugs works primarily by acting as competitive blockers to the following 4 receptor types to varying degree depending upon the agent used: histaminic, cholinergic (atropine-like effects), adrenergic (α-blocker), and serotonergic receptors.  
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Antihistaminics - Mechanism of Action – Primary – Competitive Blocking   show
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Antihistminics – Mechanism of Action – First Generation Specificity   show
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Antihistaminics - Pharmacological Effects – First Generation (7)   show
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Antihistaminics - Pharmacological Effects – First Generation – Drugs with Sedative Effects (5)   show
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Antihistaminics - Pharmacological Effects – First Generation – Drugs with Antiemetic, Antinausea Effects (6)   show
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show The following first generation antihistaminic drugs are used to create a similar effect, aside from anti-allergic effects: Promethazine, Diphenhydramine, Dimenhydrinate  
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show The following first generation antihistaminic drug is used to create a similar effect, aside from anti-allergic effects: Chlorpheniramine  
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show The following first generation antihistaminic drug is the only used to create this additional effect, manifested as postural hypotension, aside from anti-allergic effects: Promethazine  
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show The following first generation antihistaminic drugs are used to create a similar effect, aside from anti-allergic effects: Dimenhydrinate, promethazine  
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show These first generations antihistaminics are likely to create their local anaesthetic effects due to blockade of Na+ channels in excitable tissues.  
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show The following first generation antihistaminic drug is the only used to create this additional effect, aside from anti-allergic effects: Cyproheptadine  
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show The following first generation antihistaminic is misused as an appetite stimulant in children and is seen to cause weight gain and increased growth in children.  
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show The following first generation antihistaminic drugs are used to create this additional effect, aside from anti-allergic effects: Diphenhydramine, Promethazine.  
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Antihistaminics - Pharmacological Effects – First Generation – Drugs with Antiparkinsonism Effects – Diphenhydramine and Promethazine   show
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Antihistaminics - Pharmacological Effects – First Generation – Drugs with Antiparkinsonism Effects – Diphenhydramine and Promethazine – Underlying Mechanism   show
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show The adverse effects of this class of drug include sedation, anticholinergic, cardiac arrhythmias, drug allergies, drug interactions, and excitation and convulsions in children, postural hypotension, tinnitus, dizziness, lassitude, incoordination  
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Antihistaminics – Adverse Effects – Sedation – First Generation   show
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show With 1 exception, this side effect is not seen with this generation of antihistamines, because they do not cross BBB at therapeutic doses. They can thus be used while operating machines or driving vehicles.  
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show Certrizine is the sole drug from this class exhibiting the most common side-effect of antihistamines.  
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show This category of adverse effects are seen with this class of anti-autocoids: dry mouth, urinary retention, blurred vision, constipation  
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show This adverse effect is seen with 2 second generation antihistaminics, if given in higher does or even given in normal dose with enzyme inhibitors.  
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Antihistaminics – Adverse Effects - Cardiac arrhythmia - Synonym   show
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Antihistaminics – Adverse Effects - Cardiac arrhythmia – Associated Drugs.   show
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show The following drugs/compounds, if given with 2 second generation antihistaminics, will lead to this adverse effect: Ketoconazole, itraconazole, or macrolide antibiotics (erythromycin), and grapefruit juice.  
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Antihistaminics – Adverse Effects - Cardiac arrhythmia – Enzyme Inhibitors – Mechanism and Reason for Withdrawl   show
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show This second generation antihistaminic,is the and functional anti-allergic medication is the active metabolite of Terfenadine, which has replaced its use, due to its lack of cardiotoxic and sedating effects.  
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Antihistaminics – Adverse Effects - Drug allergy   show
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Antihistaminics – Adverse Effects - Drug interactions – First Generation   show
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Antihistaminics – Adverse Effects - Drug interactions – CNS Depressants (4)   show
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show The drug interactions of this class of antihistaminics includes and reaching toxic levels leading to cardiotoxicity due to inhibited cytochrome P450 action.  
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Antihistaminics – Adverse Effects - Drug interactions – Second Generation – Drugs Involved   show
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show The drugs which interact with this class of antihistaminics do so by inhibiting cytochrome P450 action which leads to a Prolonged QT interval, causing ventricular arrhythmias  
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Antihistaminics – Indications (9)   show
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show Indications of this class of drugs include the following allergic conditions: allergic rhinitis, allergic conjunctivitis, hay fever, urticaria, pruritus,  
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Antihistaminics – Indications – Allergic Conditions Not Included   show
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Antihistaminics – Indications – Allergic Conditions Not Included - Adjuvant   show
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Antihistaminics – Indications – Motion sickness   show
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Antihistaminics – Indications – Common cold*** - Mechanism   show
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show The following indication of antihistaminics is applicable to pregnancy (morning sickness), and subsequent to chemotherapy or radiation therapy.  
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show Promethazine is the DOC for this antihistaminic indication.  
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show The following drugs are given OTC for this indication of antihistaminics: Diphenhydramine, Doxylamine, Hydroxyzine  
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show The following drugs are given for this antihistaminic indication due to their antimuscarinic effects: diphenhydramine, promethazine  
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Antihistaminics – Indications – Vertigo & Meniere’s Disease   show
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show The margin of safety for this class of antihistamines is high, and so chronic toxicity is rare. However, acute poisoning can occur.  
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Antihistaminics – Toxicity - Acute poisoning   show
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show This class of antihistamines include Cimetidine, Ranitidine, Famotidine, Nizatidine  
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show This class of antihistamines act as competitive antagonists at the H2-receptors, which predominate in the gastric parietal cell  
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H2 Receptor Antagonists – Indications   show
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H2 Receptor Antagonists – Indications – GI Disorders Treated   show
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Eicosanoids – Structure   show
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Eicosanoids – Synthesis   show
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Eicosanoids – Synthesis – Stimuli (5)   show
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Eicosanoids – Classification   show
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show This subclass of eicosanoids is composed of unsaturated fatty acid derivatives formed (via endoperoxides) from the actions of cyclooxygenases (COXs)  
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Eicosanoids – Classification - Thromboxane and Prostaglandins – Mechanism - COX 1 – location   show
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show This enzyme involved in eicosanoid synthesis is expressed in the brain and kidney and on demand at sites of inflammation  
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Eicosanoids – Classification - Thromboxane and Prostaglandins – TXA2 – Direct Effects   show
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Eicosanoids – Classification - Thromboxane and Prostaglandins – PGE2 and PGF2α – Associated Conditions   show
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Eicosanoids – Classification – Leukotrienes – Mechanism   show
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Eicosanoids – Classification – Leukotrienes – LTB4 – Direct Effects   show
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show These LTs cause anaphylaxis and bronchoconstriction (role in asthma)  
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show These autocoids have effects on smooth muscle, blood contents, and kidney function  
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show These autocoids have effects on the following types of smooth muscle: vascular, bronchial, GIT and uterine  
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show The prostaglandins PGE2 and PGI2 are potent vasodilators in most vascular beds, while the thromboxane TXA2 is potent vasoconstrictor.  
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show The PGs PGE2 and PGI2 relax bronchial and tracheal muscle. Representatives from all three classes eicos - PGF2α, LTs and TXs- are potent brochoconstrictors. Leutkotrienes LTC4 and LTD4 are components of slow-reacting substance of anaphylaxis (SRS-A).  
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show PGs PGE2 and PGI2 inhibit acid and pepsinogen secretion, and increase mucus secretion (cytoprotection)  
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Eicosanoids – Pharmacological Effects – Locations – Smooth Muscle – Uterine smooth muscle - Pregnant   show
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Eicosanoids – Pharmacological Effects – Locations – Smooth Muscle – Uterine smooth muscle – non-Pregnant   show
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Eicosanoids – Pharmacological Effects – Locations – Blood – Functions   show
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show PGE2 and PGI2 inhibit platelet aggregation  
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Eicosanoids – Pharmacological Effects – Locations – Blood – Functions– Flow   show
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show PGEs induce erythropoiesis by stimulating the renal release of erythropoietin  
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show HPETE stimulates release of histamine, PGI2 and PGD inhibit histamine release. PGEs also potentiate the effect of other inflammatory agents such as bradykinin  
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show The PG’s PGE2 and PGI2 increase RBF and also stimulate renin secretion. PGEs inhibit water reabsorption induced by AD. TXA2 decreases RBF and GFR.  
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Eicosanoids – Pharmacological Effects – Locations – Kidney – Associated Conditions   show
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show This class of autocoids is targeted by the following drugs: prostaglandin analogs, Leukotriene-Targeting Drugs, and Thromboxane-A2 Targeting Drugs.  
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Eicosanoids – Drugs - Prostaglandin Analogs   show
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Eicosanoids – Drugs - Prostaglandin Analogs – Alprostadil - Indications   show
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show This PGE1 analog is given continuous iv infusion for this first line treatment.  
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show This PGE1 analog is either Injected into the corpus cavernosus or implanted as a pellet suppository into the urethra for this second-line treatment.  
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Eicosanoids – Drugs - Prostaglandin Analogs – Misoprostol – Indications   show
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Eicosanoids – Drugs - Prostaglandin Analogs – Misoprostol – Gastric Ulcer Prevention – Mechanism   show
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show This abortifacient dislodges the blastocyst and contracts the uterus.  
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show This PGE1 analog is given orally along with mifepristone (progesterone antagonist) for abortifacient action.  
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Eicosanoids – Drugs - Prostaglandin Analogs – Misoprostol – Contraindications   show
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Eicosanoids – Drugs - Prostaglandin Analogs – Dinoprostone – Indications (4)   show
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show This PGE2 analog is given as vaginal suppositories, gel, and controlled release formulations.  
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Eicosanoids – Drugs - Prostaglandin Analogs – Dinoprostone – Contraindications   show
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Eicosanoids – Drugs - Prostaglandin Analogs – Carboprost – Indications (2)   show
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Eicosanoids – Drugs - Prostaglandin Analogs – Carboprost – R/A   show
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show This PGF2a analog is contraindicated in pre-term pregnancy  
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Eicosanoids – Drugs - Prostaglandin Analogs – Latanoprost – Indications   show
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Eicosanoids – Drugs - Prostaglandin Analogs – Latanoprost – Indications – Open Angle Glaucoma - Mechanism   show
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show This PGF2a analog used in open angle glaucoma is given via IM inj.  
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show Similar drugs to this PGF2a analog include Bimatoprost, Travaprost, and Unoprostone  
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show This PGF2a analog can change the color of the iris permanently by increasing the amount of melanin.  
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show This PGI2 analog is also known as Prostacyclin  
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Eicosanoids – Drugs - Prostaglandin Analogs – Epoprostenol – Indications   show
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Eicosanoids – Drugs - Prostaglandin Analogs – Epoprostenol – Pulmonary Hypertension - Mechanisms   show
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show This PGI2 analog is administered by Continuous IV infusion to treat pulmonary hypertension.  
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show This PGI2 analog can adversely cause tachycardia and hypotension.  
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show This group of eicosanoid-targeting drugs contains the following types: glucocorticoids, zileuton, Zafirlukast and “-lukasts”  
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Eicosanoids – Drugs - Leukotriene Inhibitors – Types – Glucocorticoids - Indications   show
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show This type of LT inhibitor is indicated in the treatment of asthma due to its reduction of LTs through inhibition of lipoxygenase.  
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show These types of LT inhibtors are indicated in asthma treatment due to their ability to antagonize LT receptors.  
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Eicosanoids – Drugs - Thromboxane Inhibitors –Indication   show
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show Aspirin is an example of this anti-eicosanoid drug  
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show The Chemical Formula of this autcoid is 5-hydroxytryptamine  
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show This autcocoid is synthesized and stored in GI cells, neurons, and platelets  
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Serotonin – Synthesis and Storage – Distribution   show
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show This autocoid is metabolized by MAO type A into 5-hydroxyinolacteic acid (5HIAA) – a marker for carcinoid  
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Serotonin –Metabolism - 5HIAA – function   show
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show This autocoid metabolite works on 7 receptor subtypes, almost all of which are G-protein coupled,  
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Serotonin –Mechanism of Action – Receptors - Exception   show
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show 5HIAA acts on this receptor located in CNS and smooth muscle  
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Serotonin – Mechanism of Action – Receptors - Location - 5HT2   show
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show 5HIAA acts on this receptor located in Area postrema, peripheral sensory and enteric nerves  
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show 5HIAA acts on this receptor located in GI smooth muscle and myenteric nerves  
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Serotonin – Drugs – Agonists (4)   show
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Serotonin – Drugs – Agonists - Buspirone - Indications   show
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show This 5-HT4 receptor agonist is indicated in GERD and gastrointestinal hypomobility as a prokinetic agent.  
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show This 5-HT1D/1B agonist is indicated in the abortive treatment of Migraine headache  
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Serotonin – Drugs – Agonists – Tegaserod – Indications   show
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Serotonin – Drugs – Antagonists (4)   show
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Serotonin – Drugs – Antagonists - Clozapine - Indications   show
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Serotonin – Drugs – Antagonists - Cyproheptadine – Indications   show
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show This 5-HT2 receptor antagonist is indicated in the treatment of Carcinoid syndrome, and migraines (prophylactically).  
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Serotonin – Drugs – Antagonists - Ondansetron – Indications   show
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