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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