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Autocoids - Primary Function
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Pharm - Autocoids

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

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Autocoids - Primary Function Self-remedy is the primary function of this groups of pharmacological agents
Autocoids - Types (3) Histamine, Eicosanoids and Serotonin are the 3 members of this class of pharmacological agents
Autocoids - Main Adverse Effect Anaphylactic Shock is the main adverse effect of this group of pharmacological agents
Histamine - Structure This endogenous compound is a monoamine autocoid.
Histamine - Storage - Cellular This compound is stored at the cellular level as an inactive complex contained in granules within mast cells and basophils
Histamine - Storage - Tissues (3) This compound is stored at the tissue level in the GIT, lung, skins (especially the hands and feet)
Histamine - Storage - Tissues - GIT - Function In the GIT, this autocoid serves to induce hydrochloric acid secretion
Histamine - Storage - Tissues - Lungs - Function In the lungs, this autocoid serves as bronconstrictor
Histamine - Storage - Tissues - Skin - Function In the skin, particularly in the hands and feet, this autcoid serves to dilate the capillaries, resulting in blushing
Histamine - Storage - Dysfunction If not stored, this autocoid will be rapidly inactivated by amine oxidase enzymes
Histamine - Release - Triggers (5) The release of this autocoid is triggered by Type I sensitivity reactions (immunologic; toxins), cold (temperature), drugs (chemical), venoms and trauma (mechanical)
Histamine - Release - Triggers -Drugs (2) This autocoid is triggered by the release of drugs, among other things, including morphine and tubocurarine.
Histamine - Release - Triggers -Drugs - Tubocurarine & Morphine - Mechanism These drugs stimulate IP3 and DAG, thereby increasing calcium concentration and thus the release of stored histamine vesicles.
Histamine - Receptors - Number of Types There are four types of receptors for this autocoid
Histamine - Receptors - H1 - Mechanism This histamine receptor is membrane bound and Gq-coupled receptors, increasing IP3, DAG and calcium conc.
Histamine - Receptors - H1 - Locations (7) This histamine receptors is located in the lungs, skin, GIT, heart, brain, leukocytes and vascular smooth muscle
Histamine - Receptors - H1 - Functions This histamine receptor serves to create bronchial and intestinal smooth muscle contraction, vasodilation, HCL release in the stomach, and create a minor increase in heart contractility, HR and ionotropy
Histamine - Receptors - H2 - Mechanism This histamine receptor is membrane bound and Gs-coupled, increasing cAMP conc.
Histamine - Receptors - H2 - Locations (7) This histamine receptors is located in the GIT, heart, and sensory nerve endings
Histamine - Receptors - H2 - Functions This histamine receptor serves to induce gastric acid secretion (gastric ulcers), and increase SA nodal rate, positive ionotropism and automaticity (cardiac arrhythmias)
Antihistaminics – Classification - Functional differences between 1st and 2nd Generation (2) Unlike first generation antihistaminics, this class of drugs does not penetrate the BBB appreciably and have higher H1 selectivity
Antihistaminics - Classification - Benefit of having 2nd generation over 1st generation Second generation agents have far fewer autonomic effects (anticholinergic, antiadrenergic effects), and little or no sedative effect compared to the first generation antihistaminics
Antihistaminics – Classification - First Generation – Drugs (10) This class of antihistaminics includes: Chlorpheniramine, Cyclizine, Cyproheptadine, Diphenhydramine, Dimenhydrinate, Doxepin***, Doxylamine, Hydroxyzine, Meclizine, and Promethazine
Antihistaminics – Classification - Second Generation – Drugs (8) This class of antihistaminics includes: Acrivastine, Astemizole, Azelastine, Cetirizine, Desloratadine, Fexofenadine, Loratadine, and Terfenadine
Antihistaminics – Classification –Second Generation – Terfenadine – Usage Status This second generation antihistaminic was withdrawn from the market because it causes cardiac arrhythmias
Antihistaminics – Pharmacokinetics 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”.
Antihistaminics - Mechanism of Action 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.
Antihistaminics - Mechanism of Action – Primary – Competitive Blocking Because of their mechanism of action, this class of drugs may therefore may be ineffective at high levels of histamine
Antihistminics – Mechanism of Action – First Generation Specificity This class of antihistaminics have more propensity to bind to the non-histamine receptors
Antihistaminics - Pharmacological Effects – First Generation (7) Members of this class of drugs differ in their propensity for producing following effects in addition to their primary anti-allergic effect: sedation, anti-emetic/nausea, anticholinergic, local anaesthetic, anti-serotonergic, antiparkinsonism.
Antihistaminics - Pharmacological Effects – First Generation – Drugs with Sedative Effects (5) The following first generation antihistaminic drugs are used to create a similar effect, aside from anti-allergic: Chlorpheniramine, Dimenhydrinate, Diphenhydramine, Hydroxyzine, and Promethazine.
Antihistaminics - Pharmacological Effects – First Generation – Drugs with Antiemetic, Antinausea Effects (6) The following first generation antihistaminic drugs are used to create a similar effect, aside from anti-allergic: Cyclizine, Dimenhydrinate, Diphenhydramine, Hydroxyzine, Meclizine, and Promethazine
Antihistaminics - Pharmacological Effects – First Generation – Drugs with Anticholinergic/Atropine-like Effects – High (3) The following first generation antihistaminic drugs are used to create a similar effect, aside from anti-allergic effects: Promethazine, Diphenhydramine, Dimenhydrinate
Antihistaminics - Pharmacological Effects – First Generation – Drugs with Anticholinergic/Atropine-like Effects – Mild (1) The following first generation antihistaminic drug is used to create a similar effect, aside from anti-allergic effects: Chlorpheniramine
Antihistaminics - Pharmacological Effects – First Generation – Drugs with antiadrenergic/alpha-rc antagonist-like effects (1) 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
Antihistaminics - Pharmacological Effects – First Generation – Drugs with local anaesthetic effects The following first generation antihistaminic drugs are used to create a similar effect, aside from anti-allergic effects: Dimenhydrinate, promethazine
Antihistaminics - Pharmacological Effects – First Generation – Drugs with local anaesthetic effects – Likely Mechanism These first generations antihistaminics are likely to create their local anaesthetic effects due to blockade of Na+ channels in excitable tissues.
Antihistaminics - Pharmacological Effects – First Generation – Drugs with Antiserotonergic Effects The following first generation antihistaminic drug is the only used to create this additional effect, aside from anti-allergic effects: Cyproheptadine
Antihistaminics - Pharmacological Effects – First Generation – Drugs with Antiserotonergic Effects – Cyproheptadine 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.
Antihistaminics - Pharmacological Effects – First Generation – Drugs with Antiparkinsonism Effects The following first generation antihistaminic drugs are used to create this additional effect, aside from anti-allergic effects: Diphenhydramine, Promethazine.
Antihistaminics - Pharmacological Effects – First Generation – Drugs with Antiparkinsonism Effects – Diphenhydramine and Promethazine The following first generation antihistaminics are seen to reduce tremor, rigidity and sialorrhea of parkinsonism.
Antihistaminics - Pharmacological Effects – First Generation – Drugs with Antiparkinsonism Effects – Diphenhydramine and Promethazine – Underlying Mechanism The reduced tremor, rigidity and sialorrhea of parkinsonism seen by these first generation antihistaminics are due to their anticholinergic properties.
Antihistaminics – Adverse Effects 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
Antihistaminics – Adverse Effects – Sedation – First Generation This is the most common side effect of this class of anti-histamines, but is more commonly seen with one of the drug generations.
Antihistaminics – Adverse Effects – Sedation – Second Generation 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.
Antihistaminics – Adverse Effects – Sedation – Second Generation - Exception Certrizine is the sole drug from this class exhibiting the most common side-effect of antihistamines.
Antihistaminics – Adverse Effects - Anti-cholinergic effects This category of adverse effects are seen with this class of anti-autocoids: dry mouth, urinary retention, blurred vision, constipation
Antihistaminics – Adverse Effects - Cardiac arrhythmia This adverse effect is seen with 2 second generation antihistaminics, if given in higher does or even given in normal dose with enzyme inhibitors.
Antihistaminics – Adverse Effects - Cardiac arrhythmia - Synonym Torsades de Pointes is a synonym for this adverse effect seen in second generation anti-histaminics.
Antihistaminics – Adverse Effects - Cardiac arrhythmia – Associated Drugs. Terfenadine and Astemizole are the second generation antihistaminics seen to cause this adverse effect at higher doses or if given with enzyme inhibitors.
Antihistaminics – Adverse Effects - Cardiac arrhythmia – Enzyme Inhibitors 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.
Antihistaminics – Adverse Effects - Cardiac arrhythmia – Enzyme Inhibitors – Mechanism and Reason for Withdrawl This adverse effect will results from the addition of enzyme inhibitors to 2 second generation antihistaminics as they inhibit CYP3A family of enzymes, leading to increased blood concentration the drugs.
Antihistaminics – Adverse Effects - Cardiac arrhythmia –Drugs – Fexofenadin 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.
Antihistaminics – Adverse Effects - Drug allergy This adverse effect is seen with the topical use of antihistaminics.
Antihistaminics – Adverse Effects - Drug interactions – First Generation The drug interactions of this class of antihistaminics includes potentiation of the effects of all other CNS depressants,
Antihistaminics – Adverse Effects - Drug interactions – CNS Depressants (4) The CNS depressants whose effects are potentiated by this class of drugs include Benzodiazepines, barbiturates, alcohol, and antipsychotics. This is particularly true of the first generation of this class.
Antihistaminics – Adverse Effects - Drug interactions – Second Generation The drug interactions of this class of antihistaminics includes and reaching toxic levels leading to cardiotoxicity due to inhibited cytochrome P450 action.
Antihistaminics – Adverse Effects - Drug interactions – Second Generation – Drugs Involved The drugs which interact with terfenadine and astemizole, of this class of antihistaminics, to create cardiac arrhythmias include Erythromycin, Clarithromycin, Ketoconazole.
Antihistaminics – Adverse Effects - Drug interactions – Second Generation – Mechanism 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
Antihistaminics – Indications (9) Indications of this class of drugs include allergic conditions, motion sickness, nausea and vomiting, common cold, pre-operation sedation, sleep-disorders, parkinsonism, EPS, and vertigo.
Antihistaminics – Indications – Allergic Conditions Included Indications of this class of drugs include the following allergic conditions: allergic rhinitis, allergic conjunctivitis, hay fever, urticaria, pruritus,
Antihistaminics – Indications – Allergic Conditions Not Included Indications of this class of drugs do not include the following allergic conditions: bronchial asthma, or anaphylaxis as they involve multiple mediators beyond histamines.
Antihistaminics – Indications – Allergic Conditions Not Included - Adjuvant Epinephring, a physiological antagonist, is indicated in this manner for bronchial asthma and anaphylaxis, as opposed to this class of drugs.
Antihistaminics – Indications – Motion sickness Although scopolamine is the first-line drug, this class of drugs can also be used to prevent motion sickness, and includes Diphenhydramine, Dimenhydrinate, Cyclizine, Meclizine, and Promethazine. most effective if administered before the trip.
Antihistaminics – Indications – Common cold*** - Mechanism Antihistaminics are indicated in this condition due to their anticholinergic properties
Antihistaminics – Indications – Nausea and vomiting – Scenarios The following indication of antihistaminics is applicable to pregnancy (morning sickness), and subsequent to chemotherapy or radiation therapy.
Antihistaminics – Indications – Nausea and vomiting – Chemotherapy Promethazine is the DOC for this antihistaminic indication.
Antihistaminics – Indications – Somnifacients The following drugs are given OTC for this indication of antihistaminics: Diphenhydramine, Doxylamine, Hydroxyzine
Antihistaminics – Indications – Parkinsonism and extrapyramidal symptoms The following drugs are given for this antihistaminic indication due to their antimuscarinic effects: diphenhydramine, promethazine
Antihistaminics – Indications – Vertigo & Meniere’s Disease The following drugs are given for this antihistaminic indication: Dimenhydrinate, Meclizine
Antihistaminics – Toxicity The margin of safety for this class of antihistamines is high, and so chronic toxicity is rare. However, acute poisoning can occur.
Antihistaminics – Toxicity - Acute poisoning The follow effects of acute poisoning are seen with this class of anthistamines: dilated pupils, dry mouth, urinary retention, sinus tachycardia, CNS effects like-hallucinations, excitement, ataxia, convulsions, Coma and Death
H2 Receptor Antagonists – drugs (4) This class of antihistamines include Cimetidine, Ranitidine, Famotidine, Nizatidine
H2 Receptor Antagonists – Mechanism of Action This class of antihistamines act as competitive antagonists at the H2-receptors, which predominate in the gastric parietal cell
H2 Receptor Antagonists – Indications This class of drugs is given OTC predominantly in the treatment of GI disorders,
H2 Receptor Antagonists – Indications – GI Disorders Treated The GI disorders treated by this class of drugs includes heart burn, acid-induced indigestion, gastric and duodenal ulcers and hypersecretory states such as Zollinger-Ellison syndrome
Eicosanoids – Structure These autocoids are a cell-regulating polyunsaturated fatty acid with 20-C structure
Eicosanoids – Synthesis These autocoids are primarily synthesized from arachidonic acid and released by action of phospholipase A2 from lipids in cell membranes “on demand” in response to stimuli,
Eicosanoids – Synthesis – Stimuli (5) Stimuli that cause the on-demand synthesis and release of these autocoids include IgE-mediated reactions, inflammatory mediators, trauma, heat, and toxins
Eicosanoids – Classification The following are the three classes of these autocoids: Prostaglandins, Leukotrienes, Thromboxanes
Eicosanoids – Classification– Thromboxane and Prostaglandins– Mechanism This subclass of eicosanoids is composed of unsaturated fatty acid derivatives formed (via endoperoxides) from the actions of cyclooxygenases (COXs)
Eicosanoids – Classification - Thromboxane and Prostaglandins – Mechanism - COX 1 – location This enzyme involved in eicosanoid synthesis is constitutively expressed in most tissues including platelets and stomach, where it acts to synthesize thromboxane and cytoprotective PGs, respectively
Eicosanoids – Classification - Thromboxane and Prostaglandins – Mechanism - COX 2 – location This enzyme involved in eicosanoid synthesis is expressed in the brain and kidney and on demand at sites of inflammation
Eicosanoids – Classification - Thromboxane and Prostaglandins – TXA2 – Direct Effects This eicosanoid is a platelet aggregator, and causes bronchoconstriction and vasocontriction.
Eicosanoids – Classification - Thromboxane and Prostaglandins – PGE2 and PGF2α – Associated Conditions Both of these eicosanoids are seen to increase in primary dysmenorrhea. Therapeutic effects of NSAIDs may be due to inhibition of their synthesis
Eicosanoids – Classification – Leukotrienes – Mechanism This subclass of eicosanoids is formed (via hydroperoxides) from the action of lipoxygenases on arachidonic acid.
Eicosanoids – Classification – Leukotrienes – LTB4 – Direct Effects This LT is an Inflammatory mediator, acting as a neutrophil chemoattractant that activates PMNs and leads to (+) Free radical formation cell damage
Eicosanoids – Classification – Leukotrienes – LTA4, LTC4, and LTD4 – Direct Effects These LTs cause anaphylaxis and bronchoconstriction (role in asthma)
Eicosanoids – Pharmacological Effects – Organs (3) These autocoids have effects on smooth muscle, blood contents, and kidney function
Eicosanoids – Pharmacological Effects – Locations – Smooth Muscle – Types (4) These autocoids have effects on the following types of smooth muscle: vascular, bronchial, GIT and uterine
Eicosanoids – Pharmacological Effects – Locations – Smooth Muscle – Vascular The prostaglandins PGE2 and PGI2 are potent vasodilators in most vascular beds, while the thromboxane TXA2 is potent vasoconstrictor.
Eicosanoids – Pharmacological Effects – Locations – Smooth Muscle – Bronchial smooth muscle 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).
Eicosanoids – Pharmacological Effects – Locations – Smooth Muscle – GIT PGs PGE2 and PGI2 inhibit acid and pepsinogen secretion, and increase mucus secretion (cytoprotection)
Eicosanoids – Pharmacological Effects – Locations – Smooth Muscle – Uterine smooth muscle - Pregnant PGE2 and PGF2 from this class of drugs induces uterine contraction in this condition.
Eicosanoids – Pharmacological Effects – Locations – Smooth Muscle – Uterine smooth muscle – non-Pregnant PGI2 and PGE2 cause relaxation, while PGF2 causes contraction and LTs- potent stimulators of uterine smooth muscle in this condition.
Eicosanoids – Pharmacological Effects – Locations – Blood – Functions The following blood functions are targeted by this autcoid: platelet aggregation, flow, erythropoiesis, inflammatory mediator release.
Eicosanoids – Pharmacological Effects – Locations – Blood – Functions– Platelet Aggregation PGE2 and PGI2 inhibit platelet aggregation
Eicosanoids – Pharmacological Effects – Locations – Blood – Functions– Flow PGE2 and PGI2 increase blood flow and promote edema
Eicosanoids – Pharmacological Effects – Locations – Blood – Functions– Erythropoiesis PGEs induce erythropoiesis by stimulating the renal release of erythropoietin
Eicosanoids – Pharmacological Effects – Locations – Blood – Functions– Immunity HPETE stimulates release of histamine, PGI2 and PGD inhibit histamine release. PGEs also potentiate the effect of other inflammatory agents such as bradykinin
Eicosanoids – Pharmacological Effects – Locations – Kidney 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.
Eicosanoids – Pharmacological Effects – Locations – Kidney – Associated Conditions Bartter’s syndrome is associated with increased biosynthesis of PGs affecting this organ.
Eicosanoids – Drugs This class of autocoids is targeted by the following drugs: prostaglandin analogs, Leukotriene-Targeting Drugs, and Thromboxane-A2 Targeting Drugs.
Eicosanoids – Drugs - Prostaglandin Analogs This class of autocoid-targeting drugs includes Alprostadil, Misoprostol, Dinoprostone, Carboprost, Latanoprost, Epoprostenol
Eicosanoids – Drugs - Prostaglandin Analogs – Alprostadil - Indications This PGE1 analog is indicated in maintaining patency of ductus arteriosus, and as second line treatment for erectile dysfunction.
Eicosanoids – Drugs - Prostaglandin Analogs – Alprostadil – Indications – PDA – R/As This PGE1 analog is given continuous iv infusion for this first line treatment.
Eicosanoids – Drugs - Prostaglandin Analogs – Alprostadil – Indications – ED – R/As This PGE1 analog is either Injected into the corpus cavernosus or implanted as a pellet suppository into the urethra for this second-line treatment.
Eicosanoids – Drugs - Prostaglandin Analogs – Misoprostol – Indications This PGE1 analog is indicated for prevention of NSAID induced gastric ulcers, and as an abortifacient.
Eicosanoids – Drugs - Prostaglandin Analogs – Misoprostol – Gastric Ulcer Prevention – Mechanism This PGE1 analog produces cytoprotective action on the gastric mucosa by increasing bicarbonate and mucous secretion, and by inhibiting acid secretion.
Eicosanoids – Drugs - Prostaglandin Analogs – Misoprostol – Abortifiacient – Mechanism This abortifacient dislodges the blastocyst and contracts the uterus.
Eicosanoids – Drugs - Prostaglandin Analogs – Misoprostol – Abortifiacient – Adjuvant This PGE1 analog is given orally along with mifepristone (progesterone antagonist) for abortifacient action.
Eicosanoids – Drugs - Prostaglandin Analogs – Misoprostol – Contraindications This PGE1 analog should not be given for gastric ulcer treatment unless a pregnancy test has been done and is negative.
Eicosanoids – Drugs - Prostaglandin Analogs – Dinoprostone – Indications (4) This PGE2 analog is used for cervical ripening prior to labor induction, induction of labor, evacuation of the uterine contents in case of missed abortion, and removal of benign hydatidiform mole
Eicosanoids – Drugs - Prostaglandin Analogs – Dinoprostone - R/As (3) This PGE2 analog is given as vaginal suppositories, gel, and controlled release formulations.
Eicosanoids – Drugs - Prostaglandin Analogs – Dinoprostone – Contraindications This PGE2 analog is contraindicated in Pre-term pregnancy
Eicosanoids – Drugs - Prostaglandin Analogs – Carboprost – Indications (2) This PGF2a analog is indicated in the control of postpartum bleeding, especially in patients unresponsive to ergometrine and oxytocin, and for termination of pregnancy (abortifacient).
Eicosanoids – Drugs - Prostaglandin Analogs – Carboprost – R/A This PGF2a analog used in pregnancy is given via IM inj
Eicosanoids – Drugs - Prostaglandin Analogs – Carboprost – Contraindications This PGF2a analog is contraindicated in pre-term pregnancy
Eicosanoids – Drugs - Prostaglandin Analogs – Latanoprost – Indications This PGF2a analog is indicated in open-angle glaucoma
Eicosanoids – Drugs - Prostaglandin Analogs – Latanoprost – Indications – Open Angle Glaucoma - Mechanism This PGF2a analog works for the following condition by (+) the aqueous humor outflow via the uveoscleral pathway and (-) intraocular pressure (IOP).
Eicosanoids – Drugs - Prostaglandin Analogs – Latanoprost – R/A This PGF2a analog used in open angle glaucoma is given via IM inj.
Eicosanoids – Drugs - Prostaglandin Analogs – Latanoprost – Similar Drugs (3) Similar drugs to this PGF2a analog include Bimatoprost, Travaprost, and Unoprostone
Eicosanoids – Drugs - Prostaglandin Analogs – Latanoprost – Adverse Effects This PGF2a analog can change the color of the iris permanently by increasing the amount of melanin.
Eicosanoids – Drugs - Prostaglandin Analogs – Epoprostenol – Synonym This PGI2 analog is also known as Prostacyclin
Eicosanoids – Drugs - Prostaglandin Analogs – Epoprostenol – Indications This PGI2 analog is used to treat pulmonary hypertension.
Eicosanoids – Drugs - Prostaglandin Analogs – Epoprostenol – Pulmonary Hypertension - Mechanisms This PGI2 analog is helpful in the treatment of this condition by dilating pulmonary blood vessel.
Eicosanoids – Drugs - Prostaglandin Analogs – Epoprostenol – M/A This PGI2 analog is administered by Continuous IV infusion to treat pulmonary hypertension.
Eicosanoids – Drugs - Prostaglandin Analogs – Epoprostenol – Adverse Effects This PGI2 analog can adversely cause tachycardia and hypotension.
Eicosanoids – Drugs - Leukotriene Inhibitors – Types This group of eicosanoid-targeting drugs contains the following types: glucocorticoids, zileuton, Zafirlukast and “-lukasts”
Eicosanoids – Drugs - Leukotriene Inhibitors – Types – Glucocorticoids - Indications This type of LT inhibitor is indicated for anti-inflammatory and immunosuppressive effects through it’s reduction of phospholipase A2 activity.
Eicosanoids – Drugs - Leukotriene Inhibitors – Types – Zileuton – Indications This type of LT inhibitor is indicated in the treatment of asthma due to its reduction of LTs through inhibition of lipoxygenase.
Eicosanoids – Drugs - Leukotriene Inhibitors – Types – Zafirlukast and “-lukasts” – Indications These types of LT inhibtors are indicated in asthma treatment due to their ability to antagonize LT receptors.
Eicosanoids – Drugs - Thromboxane Inhibitors –Indication This type of anti-eicosanoid drug is indicated in the prophylaxis of MI’s
Eicosanoids – Drugs - Thromboxane Inhibitors – example Aspirin is an example of this anti-eicosanoid drug
Serotonin – Chemical Formula The Chemical Formula of this autcoid is 5-hydroxytryptamine
Serotonin – Synthesis and Storage - Location This autcocoid is synthesized and stored in GI cells, neurons, and platelets
Serotonin – Synthesis and Storage – Distribution 90% of this autcoid is found in the enterochromaffin cells of the GIT, while 10% Is found in platelets and other tissues including brain
Serotonin –Metabolism This autocoid is metabolized by MAO type A into 5-hydroxyinolacteic acid (5HIAA) – a marker for carcinoid
Serotonin –Metabolism - 5HIAA – function This autocoid metabolite serves as a marker for carcinoid and acts on several classes of 5-HT receptors
Serotonin –Mechanism of Action – Receptors This autocoid metabolite works on 7 receptor subtypes, almost all of which are G-protein coupled,
Serotonin –Mechanism of Action – Receptors - Exception 5-HT3 receptor functions as a directed coupled ion channel making it different in this way amongst its class of receptors.
Serotonin –Mechanism of Action – Receptors - Location - 5HT1 5HIAA acts on this receptor located in CNS and smooth muscle
Serotonin – Mechanism of Action – Receptors - Location - 5HT2 5HIAA acts on this receptor located in CNS and in the periphery
Serotonin – Mechanism of Action – Receptors - Location - 5HT3 5HIAA acts on this receptor located in Area postrema, peripheral sensory and enteric nerves
Serotonin – Mechanism of Action – Receptors - Location - 5HT4 5HIAA acts on this receptor located in GI smooth muscle and myenteric nerves
Serotonin – Drugs – Agonists (4) The following drugs have this relationship to serotonin receptors: Buspirone, cisaprid, sumatriptan and tegasirod
Serotonin – Drugs – Agonists - Buspirone - Indications This 5-HT1A partial agonist is indicated in Generalized Anxiety Disorder
Serotonin – Drugs – Agonists - Cisapride - Indications This 5-HT4 receptor agonist is indicated in GERD and gastrointestinal hypomobility as a prokinetic agent.
Serotonin – Drugs – Agonists - Sumatriptan - Indications This 5-HT1D/1B agonist is indicated in the abortive treatment of Migraine headache
Serotonin – Drugs – Agonists – Tegaserod – Indications This 5-HT4 agonist is indicated in the treatment of IBS with constipation.
Serotonin – Drugs – Antagonists (4) The following drugs have this relationship to serotonin receptor: clozapine, cyproheptadine, methysergide, and ondansetron
Serotonin – Drugs – Antagonists - Clozapine - Indications This 5-HT2a receptor antagonist is indicated in the treatment of schizophrenia
Serotonin – Drugs – Antagonists - Cyproheptadine – Indications This 5-HT2 receptor antagonists is indicated in the treatment of Carcinoid syndrome, pruritus and urticarial as well as anorexia nervosa
Serotonin – Drugs – Antagonists - Methysergide – Indications This 5-HT2 receptor antagonist is indicated in the treatment of Carcinoid syndrome, and migraines (prophylactically).
Serotonin – Drugs – Antagonists - Ondansetron – Indications This 5-HT3 receptor antagonists is indicated in the treatment of nausea and vomiting – both chemotherapy and radiation induced as well as postoperative emesis.
Created by: mprentic12
 

 



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