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

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Autocoids - Types (3)

Histamine, Eicosanoids and Serotonin are the 3 members of this class of pharmacological agents

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Autocoids - Main Adverse Effect

Anaphylactic Shock is the main adverse effect of this group of pharmacological agents

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Histamine - Structure

This endogenous compound is a monoamine autocoid.

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Histamine - Storage - Cellular

This compound is stored at the cellular level as an inactive complex contained in granules within mast cells and basophils

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Histamine - Storage - Tissues (3)

This compound is stored at the tissue level in the GIT, lung, skins (especially the hands and feet)

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Histamine - Storage - Tissues - GIT - Function

In the GIT, this autocoid serves to induce hydrochloric acid secretion

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Histamine - Storage - Tissues - Lungs - Function

In the lungs, this autocoid serves as bronconstrictor

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Histamine - Storage - Tissues - Skin - Function

In the skin, particularly in the hands and feet, this autcoid serves to dilate the capillaries, resulting in blushing

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Histamine - Storage - Dysfunction

If not stored, this autocoid will be rapidly inactivated by amine oxidase enzymes

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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)

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Histamine - Release - Triggers -Drugs (2)

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

These drugs stimulate IP3 and DAG, thereby increasing calcium concentration and thus the release of stored histamine vesicles.

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Histamine - Receptors - Number of Types

There are four types of receptors for this autocoid

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Histamine - Receptors - H1 - Mechanism

This histamine receptor is membrane bound and Gq-coupled receptors, increasing IP3, DAG and calcium conc.

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Histamine - Receptors - H1 - Locations (7)

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

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

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Histamine - Receptors - H2 - Mechanism

This histamine receptor is membrane bound and Gs-coupled, increasing cAMP conc.

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Histamine - Receptors - H2 - Locations (7)

This histamine receptors is located in the GIT, heart, and sensory nerve endings

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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)

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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

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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

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Antihistaminics – Classification - First Generation – Drugs (10)

This class of antihistaminics includes: Chlorpheniramine, Cyclizine, Cyproheptadine, Diphenhydramine, Dimenhydrinate, Doxepin***, Doxylamine, Hydroxyzine, Meclizine, and Promethazine

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Antihistaminics – Classification - Second Generation – Drugs (8)

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

This second generation antihistaminic was withdrawn from the market because it causes cardiac arrhythmias

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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”.

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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.

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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

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Antihistminics – Mechanism of Action – First Generation Specificity

This class of antihistaminics have more propensity to bind to the non-histamine receptors

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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.

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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.

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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

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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

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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

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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

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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

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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.

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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

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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.

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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.

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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.

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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.

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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

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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.

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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.

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Antihistaminics – Adverse Effects – Sedation – Second Generation - Exception

Certrizine is the sole drug from this class exhibiting the most common side-effect of antihistamines.

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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

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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.

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Antihistaminics – Adverse Effects - Cardiac arrhythmia - Synonym

Torsades de Pointes is a synonym for this adverse effect seen in second generation anti-histaminics.

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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.

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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.

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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.

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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.

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Antihistaminics – Adverse Effects - Drug allergy

This adverse effect is seen with the topical use of antihistaminics.

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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,

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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.

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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.

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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.

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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

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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.

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Antihistaminics – Indications – Allergic Conditions Included

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

Indications of this class of drugs do not include the following allergic conditions: bronchial asthma, or anaphylaxis as they involve multiple mediators beyond histamines.

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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.

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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.

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Antihistaminics – Indications – Common cold*** - Mechanism

Antihistaminics are indicated in this condition due to their anticholinergic properties

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Antihistaminics – Indications – Nausea and vomiting – Scenarios

The following indication of antihistaminics is applicable to pregnancy (morning sickness), and subsequent to chemotherapy or radiation therapy.

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Antihistaminics – Indications – Nausea and vomiting – Chemotherapy

Promethazine is the DOC for this antihistaminic indication.

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Antihistaminics – Indications – Somnifacients

The following drugs are given OTC for this indication of antihistaminics: Diphenhydramine, Doxylamine, Hydroxyzine

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Antihistaminics – Indications – Parkinsonism and extrapyramidal symptoms

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

The following drugs are given for this antihistaminic indication: Dimenhydrinate, Meclizine

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Antihistaminics – Toxicity

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

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

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H2 Receptor Antagonists – drugs (4)

This class of antihistamines include Cimetidine, Ranitidine, Famotidine, Nizatidine

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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

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H2 Receptor Antagonists – Indications

This class of drugs is given OTC predominantly in the treatment of GI disorders,

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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

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Eicosanoids – Structure

These autocoids are a cell-regulating polyunsaturated fatty acid with 20-C structure

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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,

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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

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Eicosanoids – Classification

The following are the three classes of these autocoids: Prostaglandins, Leukotrienes, Thromboxanes

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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)

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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

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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

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Eicosanoids – Classification - Thromboxane and Prostaglandins – TXA2 – Direct Effects

This eicosanoid is a platelet aggregator, and causes bronchoconstriction and vasocontriction.

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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

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Eicosanoids – Classification – Leukotrienes – Mechanism

This subclass of eicosanoids is formed (via hydroperoxides) from the action of lipoxygenases on arachidonic acid.

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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

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Eicosanoids – Classification – Leukotrienes – LTA4, LTC4, and LTD4 – Direct Effects

These LTs cause anaphylaxis and bronchoconstriction (role in asthma)

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Eicosanoids – Pharmacological Effects – Organs (3)

These autocoids have effects on smooth muscle, blood contents, and kidney function

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Eicosanoids – Pharmacological Effects – Locations – Smooth Muscle – Types (4)

These autocoids have effects on the following types of smooth muscle: vascular, bronchial, GIT and uterine

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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.

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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).

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Eicosanoids – Pharmacological Effects – Locations – Smooth Muscle – GIT

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

PGE2 and PGF2 from this class of drugs induces uterine contraction in this condition.

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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.

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Eicosanoids – Pharmacological Effects – Locations – Blood – Functions

The following blood functions are targeted by this autcoid: platelet aggregation, flow, erythropoiesis, inflammatory mediator release.

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Eicosanoids – Pharmacological Effects – Locations – Blood – Functions– Platelet Aggregation

PGE2 and PGI2 inhibit platelet aggregation

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Eicosanoids – Pharmacological Effects – Locations – Blood – Functions– Flow

PGE2 and PGI2 increase blood flow and promote edema

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Eicosanoids – Pharmacological Effects – Locations – Blood – Functions– Erythropoiesis

PGEs induce erythropoiesis by stimulating the renal release of erythropoietin

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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

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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.

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Eicosanoids – Pharmacological Effects – Locations – Kidney – Associated Conditions

Bartter’s syndrome is associated with increased biosynthesis of PGs affecting this organ.

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Eicosanoids – Drugs

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

This class of autocoid-targeting drugs includes Alprostadil, Misoprostol, Dinoprostone, Carboprost, Latanoprost, Epoprostenol

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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.

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Eicosanoids – Drugs - Prostaglandin Analogs – Alprostadil – Indications – PDA – R/As

This PGE1 analog is given continuous iv infusion for this first line treatment.

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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.

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Eicosanoids – Drugs - Prostaglandin Analogs – Misoprostol – Indications

This PGE1 analog is indicated for prevention of NSAID induced gastric ulcers, and as an abortifacient.

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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.

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Eicosanoids – Drugs - Prostaglandin Analogs – Misoprostol – Abortifiacient – Mechanism

This abortifacient dislodges the blastocyst and contracts the uterus.

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Eicosanoids – Drugs - Prostaglandin Analogs – Misoprostol – Abortifiacient – Adjuvant

This PGE1 analog is given orally along with mifepristone (progesterone antagonist) for abortifacient action.

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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.

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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

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Eicosanoids – Drugs - Prostaglandin Analogs – Dinoprostone - R/As (3)

This PGE2 analog is given as vaginal suppositories, gel, and controlled release formulations.

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Eicosanoids – Drugs - Prostaglandin Analogs – Dinoprostone – Contraindications

This PGE2 analog is contraindicated in Pre-term pregnancy

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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).

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Eicosanoids – Drugs - Prostaglandin Analogs – Carboprost – R/A

This PGF2a analog used in pregnancy is given via IM inj

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Eicosanoids – Drugs - Prostaglandin Analogs – Carboprost – Contraindications

This PGF2a analog is contraindicated in pre-term pregnancy

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Eicosanoids – Drugs - Prostaglandin Analogs – Latanoprost – Indications

This PGF2a analog is indicated in open-angle glaucoma

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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).

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Eicosanoids – Drugs - Prostaglandin Analogs – Latanoprost – R/A

This PGF2a analog used in open angle glaucoma is given via IM inj.

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Eicosanoids – Drugs - Prostaglandin Analogs – Latanoprost – Similar Drugs (3)

Similar drugs to this PGF2a analog include Bimatoprost, Travaprost, and Unoprostone

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Eicosanoids – Drugs - Prostaglandin Analogs – Latanoprost – Adverse Effects

This PGF2a analog can change the color of the iris permanently by increasing the amount of melanin.

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Eicosanoids – Drugs - Prostaglandin Analogs – Epoprostenol – Synonym

This PGI2 analog is also known as Prostacyclin

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Eicosanoids – Drugs - Prostaglandin Analogs – Epoprostenol – Indications

This PGI2 analog is used to treat pulmonary hypertension.

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Eicosanoids – Drugs - Prostaglandin Analogs – Epoprostenol – Pulmonary Hypertension - Mechanisms

This PGI2 analog is helpful in the treatment of this condition by dilating pulmonary blood vessel.

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Eicosanoids – Drugs - Prostaglandin Analogs – Epoprostenol – M/A

This PGI2 analog is administered by Continuous IV infusion to treat pulmonary hypertension.

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Eicosanoids – Drugs - Prostaglandin Analogs – Epoprostenol – Adverse Effects

This PGI2 analog can adversely cause tachycardia and hypotension.

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Eicosanoids – Drugs - Leukotriene Inhibitors – Types

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

This type of LT inhibitor is indicated for anti-inflammatory and immunosuppressive effects through it’s reduction of phospholipase A2 activity.

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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.

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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.

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Eicosanoids – Drugs - Thromboxane Inhibitors –Indication

This type of anti-eicosanoid drug is indicated in the prophylaxis of MI’s

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Eicosanoids – Drugs - Thromboxane Inhibitors – example

Aspirin is an example of this anti-eicosanoid drug

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Serotonin – Chemical Formula

The Chemical Formula of this autcoid is 5-hydroxytryptamine

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Serotonin – Synthesis and Storage - Location

This autcocoid is synthesized and stored in GI cells, neurons, and platelets

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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

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Serotonin –Metabolism

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

This autocoid metabolite serves as a marker for carcinoid and acts on several classes of 5-HT receptors

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Serotonin –Mechanism of Action – Receptors

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

5-HT3 receptor functions as a directed coupled ion channel making it different in this way amongst its class of receptors.

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Serotonin –Mechanism of Action – Receptors - Location - 5HT1

5HIAA acts on this receptor located in CNS and smooth muscle

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Serotonin – Mechanism of Action – Receptors - Location - 5HT2

5HIAA acts on this receptor located in CNS and in the periphery

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Serotonin – Mechanism of Action – Receptors - Location - 5HT3

5HIAA acts on this receptor located in Area postrema, peripheral sensory and enteric nerves

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Serotonin – Mechanism of Action – Receptors - Location - 5HT4

5HIAA acts on this receptor located in GI smooth muscle and myenteric nerves

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Serotonin – Drugs – Agonists (4)

The following drugs have this relationship to serotonin receptors: Buspirone, cisaprid, sumatriptan and tegasirod

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Serotonin – Drugs – Agonists - Buspirone - Indications

This 5-HT1A partial agonist is indicated in Generalized Anxiety Disorder

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Serotonin – Drugs – Agonists - Cisapride - Indications

This 5-HT4 receptor agonist is indicated in GERD and gastrointestinal hypomobility as a prokinetic agent.

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Serotonin – Drugs – Agonists - Sumatriptan - Indications

This 5-HT1D/1B agonist is indicated in the abortive treatment of Migraine headache

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Serotonin – Drugs – Agonists – Tegaserod – Indications

This 5-HT4 agonist is indicated in the treatment of IBS with constipation.

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Serotonin – Drugs – Antagonists (4)

The following drugs have this relationship to serotonin receptor: clozapine, cyproheptadine, methysergide, and ondansetron

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Serotonin – Drugs – Antagonists - Clozapine - Indications

This 5-HT2a receptor antagonist is indicated in the treatment of schizophrenia

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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

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Serotonin – Drugs – Antagonists - Methysergide – Indications

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

This 5-HT3 receptor antagonists is indicated in the treatment of nausea and vomiting – both chemotherapy and radiation induced as well as postoperative emesis.

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