Autacoids: Functions and Classes
35 Questions
0 Views

Choose a study mode

Play Quiz
Study Flashcards
Spaced Repetition
Chat to Lesson

Podcast

Play an AI-generated podcast conversation about this lesson

Questions and Answers

What is a characteristic of autacoids?

  • They are not involved in physiological processes.
  • They act systemically throughout the body.
  • They have a long duration of action.
  • They act locally near their site of synthesis. (correct)
  • Which class of autacoids includes histamine and serotonin?

  • Polypeptides
  • Lipid-derived autacoids
  • Eicosanoids
  • Biogenic amines (correct)
  • What role does histamine play in the body?

  • Inhibits gastric acid secretion
  • Only acts as a neurotransmitter in the CNS
  • Modulates smooth muscle function (correct)
  • Is a primary hormone for blood pressure regulation
  • Where is histamine synthesized in the body?

    <p>From dietary histidine by histidine decarboxylase (C)</p> Signup and view all the answers

    Which of the following is NOT a lipid-derived autacoids?

    <p>Histamine (C)</p> Signup and view all the answers

    Which of the following statements about serum serotonin distribution and function is correct?

    <p>Platelets store serotonin and release it during activation. (A)</p> Signup and view all the answers

    What is the primary therapeutic use of Metoclopramide?

    <p>Treatment of vomiting disorders. (C)</p> Signup and view all the answers

    Which of the following is a potential adverse effect of Cisapride?

    <p>Diarrhea (C)</p> Signup and view all the answers

    Cyproheptadine is primarily used for which of the following conditions in cats?

    <p>Management of allergic reactions. (A)</p> Signup and view all the answers

    What role does serotonin play in the gastrointestinal tract?

    <p>Regulates GI motility. (C)</p> Signup and view all the answers

    What effect does histamine have on blood pressure?

    <p>It decreases blood pressure by relaxing arterioles. (C)</p> Signup and view all the answers

    Which type of histamine receptor is associated with increased gastric secretion?

    <p>H2 receptor (B)</p> Signup and view all the answers

    Which of the following statements about H1 antihistamines is correct?

    <p>First generation H1 antihistamines can easily cross the blood–brain barrier. (A)</p> Signup and view all the answers

    Which mechanism results in the release of histamine from mast cells?

    <p>Binding of antigenic substances to IgE. (A)</p> Signup and view all the answers

    What is a primary therapeutic use of first-generation H1-antihistamines?

    <p>Prevention of motion sickness (C)</p> Signup and view all the answers

    What is a physiological effect associated with H1 receptor activation?

    <p>Bronchoconstriction and increased mucus secretion. (D)</p> Signup and view all the answers

    Which adverse effect is associated with first-generation H1-antihistamines?

    <p>Sedation (A)</p> Signup and view all the answers

    Which of the following drugs is classified as a first generation H1 antihistamine?

    <p>Diphenhydramine (A)</p> Signup and view all the answers

    What is the mechanism of action for H2-antihistamines like cimetidine?

    <p>Competitively inhibiting H2-receptors in parietal cells (B)</p> Signup and view all the answers

    What is the role of histamine in allergic reactions?

    <p>It activates sensory nerves causing pain and itching. (C)</p> Signup and view all the answers

    Which of the following is an adverse effect of H2-antihistamines?

    <p>Uncommon when used as recommended (C)</p> Signup and view all the answers

    What is the effect of H2 receptor activation on the body?

    <p>Stimulation of gastric secretions. (C)</p> Signup and view all the answers

    Which medication is effective in treating allergic conjunctivitis?

    <p>Cromolyn sodium (D)</p> Signup and view all the answers

    What side effect might result from the antimuscarinic effects of first-generation H1-antihistamines?

    <p>Increased heart rate (C)</p> Signup and view all the answers

    What role do sympathomimetic drugs play in relation to histamine?

    <p>Antagonize histamine's physiological function (A)</p> Signup and view all the answers

    Which patient condition is NOT treated with H1-antihistamines?

    <p>Duodenal ulcers (A)</p> Signup and view all the answers

    What is the primary role of phospholipase A2 in the synthesis of eicosanoids?

    <p>Hydrolyze membrane phospholipids to release arachidonic acid (D)</p> Signup and view all the answers

    Which pharmacologic effect is primarily associated with thromboxane A2 (TXA2)?

    <p>Vasoconstriction and promoting platelet aggregation (B)</p> Signup and view all the answers

    Which of the following is a therapeutic use of PGE and PGF2α analogs?

    <p>Treating gastric ulceration caused by NSAIDs (C)</p> Signup and view all the answers

    Which of the following is NOT a pharmacologic effect of leukotrienes?

    <p>Promoting bronchodilation (A)</p> Signup and view all the answers

    What is the primary function of prostacyclin (PGI2)?

    <p>Inhibit platelet aggregation and cause vasodilatation (B)</p> Signup and view all the answers

    Which compound is a leukotriene receptor antagonist used in asthma treatment?

    <p>Montelukast (Singulair) (A)</p> Signup and view all the answers

    What is the consequence of administering PGF2α drugs?

    <p>Causes bronchoconstriction and asthma (B)</p> Signup and view all the answers

    Which of the following statements is true regarding prostaglandin E2 (PGE2)?

    <p>It induces fever (C)</p> Signup and view all the answers

    Signup and view all the answers

    Flashcards

    What are autacoids?

    A class of chemical messengers that act locally, have a short duration of action, and are involved in physiological and pathological processes.

    What are some examples of autacoids?

    Histamine, serotonin, and angiotensin are examples of autacoids.

    How is histamine synthesized?

    Histamine is synthesized from histidine, an amino acid, via an enzymatic reaction.

    Where is histamine stored and released?

    Mast cells and basophils store and release histamine, which plays a crucial role in allergic reactions.

    Signup and view all the flashcards

    How does histamine affect the stomach?

    Histamine released from the stomach lining helps regulate stomach acid secretion.

    Signup and view all the flashcards

    Histamine

    A chemical compound found in various venoms and insect stings, causing a range of physiological effects.

    Signup and view all the flashcards

    Histamine Release

    A process by which histamine is released from cells, often triggered by immune responses, drugs, or physical injury.

    Signup and view all the flashcards

    H1 Receptor

    A type of histamine receptor that mediates a variety of responses, including smooth muscle contraction, capillary dilation, and vascular permeability.

    Signup and view all the flashcards

    H2 Receptor

    A type of histamine receptor that primarily regulates gastric acid secretion and other actions.

    Signup and view all the flashcards

    H1 Antihistamine

    A type of medication that blocks the effects of histamine by binding to H1 receptors.

    Signup and view all the flashcards

    First Generation H1 Antihistamine

    An H1 antihistamine that readily crosses the blood-brain barrier, often causing side effects such as drowsiness.

    Signup and view all the flashcards

    Second Generation H1 Antihistamine

    An H1 antihistamine that has less impact on the central nervous system, resulting in fewer sedative side effects.

    Signup and view all the flashcards

    Histamine Release Inhibitors

    A group of medications designed to prevent the release of histamine from cells.

    Signup and view all the flashcards

    What are H1-Antihistamines?

    A type of antihistamine that blocks histamine from binding to H1 receptors, which are found on various cells throughout the body, including smooth muscle cells, sensory nerves, and blood vessels. This action reduces the symptoms of allergies, such as sneezing, runny nose, and itching.

    Signup and view all the flashcards

    How do H1-Antihistamines Work?

    H1-antihistamines primarily target H1 receptors, which are involved in the allergic response. They work by preventing histamine from binding to these receptors, thus blocking the signaling cascade that leads to allergy symptoms.

    Signup and view all the flashcards

    What is a common side effect of H1-antihistamines?

    H1-antihistamines can cause drowsiness or sedation. This effect is particularly common with first-generation H1-antihistamines. The mechanism involves the inhibition of histamine-induced signaling in the central nervous system.

    Signup and view all the flashcards

    How do H2-antihistamines work?

    H2-antihistamines, such as cimetidine and ranitidine, work by competitively blocking histamine from binding to H2 receptors, primarily found in the stomach lining. This action reduces gastric acid production.

    Signup and view all the flashcards

    How does Cromolyn sodium work?

    Cromolyn sodium inhibits the release of histamine from mast cells, which are immune cells involved in allergic responses. It does not block histamine receptors directly.

    Signup and view all the flashcards

    How do sympathomimetic drugs work?

    Sympathomimetic drugs, such as epinephrine, phenylephrine, and ephedrine, counteract the effects of histamine by activating alpha and beta adrenoceptors. This action increases blood pressure and relaxes bronchi, effectively opposing histamine's effects.

    Signup and view all the flashcards

    Serotonin (5-HT)

    A neurotransmitter synthesized from tryptophan and involved in regulating mood, sleep, appetite, and other bodily functions.

    Signup and view all the flashcards

    GI Prokinetic

    A medication that increases gastrointestinal (GI) motility by stimulating the release of acetylcholine (Ach), a neurotransmitter responsible for muscle contractions.

    Signup and view all the flashcards

    5-HT4 Agonist

    A type of drug that blocks the effects of serotonin at the 5-HT4 receptors, leading to increased acetylcholine release and improved GI motility.

    Signup and view all the flashcards

    Cyproheptadine

    An antihistamine and 5-HT2 antagonist used to treat various conditions, including feline asthma, hives in horses, and as an appetite stimulant in cats.

    Signup and view all the flashcards

    D2 Receptor Antagonist

    A drug that blocks the effects of dopamine at the D2 receptor, used for various conditions including vomiting, reflux, and gastric stasis.

    Signup and view all the flashcards

    Membrane Phospholipids

    A type of lipid found in cell membranes. It serves as the precursor for arachidonic acid, which is the starting point for the synthesis of eicosanoids.

    Signup and view all the flashcards

    Phospholipase A2

    The enzyme that catalyzes the release of arachidonic acid from membrane phospholipids. This is the first step in the synthesis of eicosanoids.

    Signup and view all the flashcards

    Arachidonic Acid

    A polyunsaturated fatty acid released from membrane phospholipids by the action of phospholipase A2. It is the precursor for the synthesis of eicosanoids, including prostaglandins, thromboxanes, and leukotrienes.

    Signup and view all the flashcards

    Cyclooxygenase (COX)

    An enzyme that catalyzes the conversion of arachidonic acid into prostaglandins and thromboxanes. It is a key enzyme in the synthesis of these eicosanoids.

    Signup and view all the flashcards

    Prostaglandins (PGs)

    A group of eicosanoids produced via the cyclooxygenase pathway from arachidonic acid. They have diverse physiological effects. They are involved in processes like inflammation, pain, fever, and blood clotting.

    Signup and view all the flashcards

    Thromboxanes (TXs)

    A group of eicosanoids produced via the cyclooxygenase pathway from arachidonic acid. They are primarily involved in platelet aggregation and vasoconstriction. They help in blood clotting and wound healing.

    Signup and view all the flashcards

    Leukotrienes (LTs)

    A group of eicosanoids produced via the lipoxygenase pathway from arachidonic acid. These potent mediators of inflammation are primarily associated with allergic reactions, asthma, and inflammation.

    Signup and view all the flashcards

    Lipoxygenase (5-LOX)

    Enzyme that catalyzes the conversion of arachidonic acid into leukotrienes in neutrophils, monocytes, macrophages, mast cells, keratinocytes, lungs, spleen, brain, and heart.

    Signup and view all the flashcards

    Study Notes

    Autacoids

    • Autacoids are biological factors that act locally near their site of synthesis and release.
    • They have a brief duration of action and participate in physiological or pathophysiological processes.
    • Classes of autacoids include biogenic amines, polypeptides, and lipid-derived autacoids (eicosanoids).

    Classes of Autacoids

    • Biogenic amines:
      • Histamine
      • Serotonin (5-hydroxytryptamine, 5-HT)
    • Polypeptides:
      • Angiotensin
    • Lipid-derived autacoids (eicosanoids):
      • Eicosanoids
      • Prostaglandins
      • Leukotrienes
      • Thromboxane

    General Physiologic Function

    • Modulate blood flow in specific tissues
    • Modulate secretory processes (e.g., gastric acid secretion)
    • Modulate smooth muscle function (e.g., vascular and bronchial)
    • Play a key role in allergy, inflammation, pain, and certain types of drug reactions (e.g., anaphylaxis).

    Histamine

    • Biosynthesis: Synthesized from dietary histidine by histidine decarboxylase.
    • Distribution and storage sites:
      • Mast cells and basophils: stored in vesicles
      • Stomach mucosa: causes gastric acid secretion
      • Lungs and skin: release causes allergic responses
      • CNS: acts as a neurotransmitter
      • Many venoms and insect stings contain histamine

    Physiologic and Pathologic Roles of Histamine

    • Stimulates gastric acid secretion
    • Involved in allergic reactions and anaphylactic shock
    • Increases capillary permeability associated with inflammation
    • Decreases blood pressure because it relaxes arterioles
    • Causes bronchial occlusion and increased mucus secretion associated with asthma
    • Causes pain and itching by activating sensory nerves

    Histamine Release

    • Immune (allergy): binding of antigenic substances to IgE on mast cells or basophils causes degranulation and release of histamine associated with hypersensitivity reactions
    • Drugs and chemicals: morphine, tubocurarine, codeine, penicillin
    • Physical injury: heat, cold, trauma
    • Plant and animal stings

    Histamine Receptors

    • H1 Receptor:
      • Signal: Gq protein, phospholipase C
      • Response: contraction of GI muscle, bronchoconstriction, dilation of arterioles and capillaries, increased heart rate, increased vascular permeability
    • H2 Receptor:
      • Signal: Gs protein, adenyl cyclase
      • Response: gastric secretions, salivary secretion, lacrimation

    Histamine Antagonists

    • Receptor antagonist
    • Release inhibitors
    • Physiologic antagonists

    H1 Antihistamines

    • First Generation: Diphenhydramine, Dimenhydrinate, Hydroxyzine, Meclizine, Promethazine, Cyproheptadine.
      • Unionized at physiological pH, easily cross the blood-brain barrier (BBB), therefore produce CNS side effects (sedation)
    • Second Generation: Loratadine, Cetirizine, Fexofenadine.
      • Ionized at physiological pH, difficult to cross BBB, therefore less CNS side effects.

    Pharmacologic effects of H1-antihistamines

    • Relaxation of contracted bronchiolar smooth muscle
    • Relaxation of contracted intestinal smooth muscle
    • Inhibition of histamine-induced vasodilation and capillary permeability
    • Inhibition of itch sensation
    • Sedation (first-generation H1-antihistamines)
    • Antimuscarinic effects
    • Anti motion sickness (antiemetic) effects

    Therapeutic uses of H1-antihistamines

    • Treatment of allergic conditions (urticaria, pruritus, allergic reactions, anaphylaxis)
    • Prevention of motion sickness
    • Sedation induction

    Adverse effects of H1-antihistamines

    • CNS depression (lethargy, somnolence, ataxia)
    • Antimuscarinic effects (dry mouth, urinary retention, intestinal atony)

    H2-antihistamines (Cimetidine and Ranitidine)

    • Pharmacologic effects: competitively inhibits histamine (H2-receptors) in parietal cells, decreasing gastric acid production
    • Therapeutic uses:
      • Ulcer treatment
      • Erosive gastritis
      • Gastroesophageal reflux
    • Adverse effects: uncommon when used as recommended
    • Drug interactions: inhibits hepatic cytochrome P450 enzymes, prolonging the concentration of drugs metabolized by the liver.

    Inhibitors of histamine release

    • Cromolyn sodium: inhibits histamine release from mast cells
    • Therapeutic uses:
      • Recurrent airway obstruction and heaves in horses
      • Control allergic conjunctivitis (eye drop)
    • Physiologic antagonists to histamine:
    • Sympathomimetic drugs (Epinephrine, Phenylephrine, Ephedrine)

    Serotonin (5-hydroxytryptamine, 5-HT)

    • Biosynthesis: From tryptophan via tryptophan hydroxylase and L-aromatic acid decarboxylase.
    • Distribution and function:
      • GI tract (enterochromaffin cells): regulates motility
      • Platelets: stores 5-HT and upon activation causes vasoconstriction and platelet aggregation.
      • CNS: acts as a neurotransmitter

    Serotonin-receptor modifying drugs

    • GI prokinetic agents: increase GI motility by increasing Ach release.
    • Cisapride: agonist of 5-HT4 receptor which increases Ach release.
      • Therapeutic uses: gastric/intestinal stasis, reflex esophagitis, constipation
      • Adverse effects: diarrhea, abdominal pain
    • Metoclopramide: D2-receptor antagonist and 5-HT3 agonist.
      • Therapeutic uses: vomiting disorders (antiemetic), reflux esophagitis, gastric stasis or hypomotility
      • Adverse effects: restlessness, drowsiness, depression

    Cyproheptadine

    • 5-HT2 antagonist and H1-antihistamine
    • Therapeutic uses: appetite stimulant in cats, treatment of feline asthma and pruritus in cats, managing hives in horses
    • Adverse effects: sedation, anticholinergic activity, lethargy.

    Eicosanoids

    • Derived from membrane phospholipids via phospholipase A2 and arachidonic acid.
    • Pathways include cyclooxygenase (prostaglandins, thromboxanes) and lipoxygenase (leukotrienes).

    Leukotrienes (LTs)

    • Synthesized by lipoxygenase in various cells.
    • Pharmacologic effects: potent vasoconstrictors, potent bronchoconstrictors, increase capillary permeability, increased mucous secretion.
    • LT antagonists (Montelukast) : used in asthma treatment.

    Polypeptides (Angiotensin)

    • Mechanism: A series of reactions starting from renin converting angiotensinogen to angiotensin I, then to angiotensin II in the lungs, which causes the body to retain water and salt, leading to vasoconstriction, increasing blood pressure.
    • Antagonists of the renin-angiotensin system: ACE inhibitors, Beta1-adrenergic antagonists, Angiotensin I (AT1) receptor antagonists, Renin receptor inhibitors.
      • These drugs counteract the effect of the system, reducing blood pressure or blocking sodium absorption.

    Studying That Suits You

    Use AI to generate personalized quizzes and flashcards to suit your learning preferences.

    Quiz Team

    Related Documents

    Pharmacology of Autacoids PDF

    Description

    Explore the fascinating world of autacoids, which are local biological factors pivotal in various physiological processes. This quiz covers their classes, including biogenic amines, polypeptides, and lipid-derived autacoids, along with their general functions like modulating blood flow and secretory processes.

    More Like This

    Autacoids
    30 questions

    Autacoids

    AppreciativeObsidian9065 avatar
    AppreciativeObsidian9065
    Autacoids and Local Hormones Quiz
    5 questions
    Use Quizgecko on...
    Browser
    Browser