Hereditary Angioedema Treatment Overview
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Questions and Answers

What is the primary role of endotheliin-1 in the human body?

  • It functions as a vasoconstrictor, raising blood pressure. (correct)
  • It enhances endothelial repair processes.
  • It reduces vascular smooth muscle proliferation.
  • It acts as a vasodilator to increase blood flow.

    • Which condition is NOT typically associated with increased production of endotheliin-1?

  • Primary pulmonary hypertension
  • Coronary artery disease
  • Diabetes mellitus (correct)
  • Cardiac hypertrophy

    • Which receptor subtype is primarily associated with the actions of endotheliin-1?

  • ETB receptors
  • ETA receptors (correct)
  • EDAR receptors
  • ETC receptors

    • What is one of the most notable effects of activating ETA receptors?

    <p>Vascular smooth muscle proliferation (B)</p> Signup and view all the answers

    What is the primary tissue where serotonin (5-HT) is stored?

    <p>Entrochromaffin tissue of the GIT (C)</p> Signup and view all the answers

    Which of the following is a potential therapeutic use of a third generation oral B2-receptor antagonist?

    <p>Management of hereditary angioedema attacks (C)</p> Signup and view all the answers

    Which receptor is primarily involved in the role of serotonin related to anxiety and cognitive function?

    <p>5-HT1A (D)</p> Signup and view all the answers

    What condition is NOT typically treated with endotheliin antagonists?

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

    Which of the following statements about endotheliin is true?

    <p>Endotheliin-1 is a potent vasoconstrictor. (A)</p> Signup and view all the answers

    What is the mechanism of action for the 5-HT2C receptor?

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

    Which pharmacological effect is primarily associated with the activation of the 5-HT3 receptor?

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

    In which scenario would you expect an increased level of endotheliin-1 production?

    <p>In conditions of low oxygen through hypoxia (B)</p> Signup and view all the answers

    Which of the following statements about 5-HT1B receptors is true?

    <p>They role in thermoregulation and nociception. (D)</p> Signup and view all the answers

    Which of the following is a known pharmacological action of serotonin acting on 5-HT2A receptors?

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

    What role does the 5-HT4 receptor play in the body?

    <p>Increase in gastrointestinal motility and secretions (A)</p> Signup and view all the answers

    Which receptor type is involved in decreasing cAMP levels?

    <p>5-HT1A (D)</p> Signup and view all the answers

    Which of the following accurately describes the primary therapeutic use of triptans?

    <p>Treatment of acute migraine episodes. (D)</p> Signup and view all the answers

    What is the most likely timeframe for the therapeutic effects of anxiety medications to appear?

    <p>As long as 2 weeks. (B)</p> Signup and view all the answers

    Which of the following statements about Bossentan and Ambrisentan is true?

    <p>Bossentan is a non-selective blocker of both ET_A and ET_B receptors. (D)</p> Signup and view all the answers

    What risk is associated with the 5-HT1B receptor activity of triptans?

    <p>Activation of coronary artery spasms. (C)</p> Signup and view all the answers

    What effect do 5-HT1D receptor activations have in triptans?

    <p>They inhibit inflammation of meninges. (D)</p> Signup and view all the answers

    What role does ATP play in the context of purines as mediators?

    <p>ATP is released by cell lysis or via vesicle exocytosis. (A)</p> Signup and view all the answers

    What is one of the main functions of adenosine as a drug?

    <p>It converts supraventricular tachycardia to sinus rhythm. (A)</p> Signup and view all the answers

    Which of the following drugs is a specific 5-HT4 agonist used to treat irritable bowel syndrome with constipation?

    <p>Tegaserod. (D)</p> Signup and view all the answers

    Which of the following best describes the action of nucleosides and nucleotides in the extracellular environment?

    <p>They serve as mediators for various receptor families. (D)</p> Signup and view all the answers

    What is the primary mechanism of action for triptans in relieving migraine pain?

    <p>Activating 5-HT1B/1D receptors. (C)</p> Signup and view all the answers

    What common misconception might people have about the effectiveness of triptans?

    <p>They always provide immediate relief. (A)</p> Signup and view all the answers

    Which of the following statements about ATP conversion is accurate?

    <p>ATP is converted to ADP and adenosine upon release. (A)</p> Signup and view all the answers

    How is Ambrisentan characterized in terms of receptor selectivity?

    <p>It is a selective ETA receptor blocker. (D)</p> Signup and view all the answers

    Which receptor types does cyproheptadine block?

    <p>5-HT2, H1, and muscarinic receptors. (C)</p> Signup and view all the answers

    What is the immediate effect of administering adenosine to a patient?

    <p>It inhibits AV conduction. (A)</p> Signup and view all the answers

    What distinguishes the action mechanism of ambrisentan from that of other similar drugs?

    <p>Ambrisentan is an oral medication with selective action. (A)</p> Signup and view all the answers

    What is the primary use of selective antagonists at bradykinin B2 receptors?

    <p>To alleviate pain by stimulating sensory nerves (C)</p> Signup and view all the answers

    Which receptor types do atypical antipsychotics primarily block to exert their effects?

    <p>5-HT2A and D2 receptors (D)</p> Signup and view all the answers

    What role do kinins play in the body?

    <p>Stimulating smooth muscle contraction and causing vasodilation (D)</p> Signup and view all the answers

    What is a characteristic of Ondansetron?

    <p>Used to treat nausea and vomiting related to chemotherapy (D)</p> Signup and view all the answers

    What mechanism do kinins utilize to affect blood vessels?

    <p>Activating B2 receptors (D)</p> Signup and view all the answers

    Which agent is considered a second-generation decapeptide acting on bradykinin receptors?

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

    How do selective 5-HT3 receptor blockers function in the gastrointestinal tract?

    <p>By blocking serotonin's action at these receptors (A)</p> Signup and view all the answers

    What effect does the activation of B2 receptors have on capillaries?

    <p>Increases permeability and causes vasodilation (C)</p> Signup and view all the answers

    Bossentan is a selective ETBB blocker.

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

    Ambrisentan is approved for the treatment of pulmonary hypertennsion.

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

    Adenosine is a long-acting purine A receptor antagonist.

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

    ATP is released through exocytosis or cell necrosis.

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

    Nucleotides, like ADP and ATP, act primarily on steroid receptors.

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

    Released ATP is slowly converted to adenosine.

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

    The three purines act on four main families of purine receptors.

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

    Adenosine is given orally to convert supraventricular tachycardia to sinus rhythm.

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

    Serotonin (5-HT) is stored mainly in the enterochromaffin tissue of the GIT and the brain.

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

    5-HT1A receptors are activated to enhance cognitive function and anxiety regulation.

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

    5-HT3 receptors are primarily involved in nociception and appetite regulation.

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

    5-HT4 receptors increase gastrointestinal motility and secretions.

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

    5-HT2B receptors are linked primarily to smooth muscle contraction and vasodilation.

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

    Serotonin is converted from the amino acid tyrosine and predominately affects the cardiovascular system.

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

    5-HT2A receptors contribute to platelet aggregation.

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

    Tripans primarily treat chronic headaches.

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

    Buspirone acts as an antagonist at the 5-HT1A receptor.

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

    The therapeutic effect of medications for anxiety disorders may take up to 2 weeks to appear.

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

    Activation of 5-HT1D receptors promotes inflammation in the meninges.

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

    Coronary spasms can occur as a side effect of 5-HT1B receptor activity.

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

    Sumatriptan is an example of a 5-HT4 agonist.

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

    Tegaserod is used to decrease gastrointestinal motility.

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

    Cyproheptadine blocks 5-HTT2 receptors among others.

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

    Patients with ischemic heart disease can safely use triptans.

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

    Kininogen is formed from amino acid peptides by the effect of kallikrein enzyme.

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

    Selective antagonists at bradykinin B1 receptors are used primarily to increase capillary permeability.

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

    Olanzapine is a typical antipsychotic that blocks dopamine D2 receptors.

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

    Granisetron and ondansetron are used to treat nausea and vomiting associated with chemotherapy.

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

    Bradykinin acts solely as a vasoconstrictor in the human body.

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

    Activation of B2 receptors in kinins results in smooth muscle contraction.

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

    Atyical antipsychotics are known for their ability to block both 5-HT2A and D2 receptors to improve negative symptoms of schizophrenia.

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

    Icatibant is a first-generation decapeptide that acts as a selective agonist at bradykinin B2 receptors.

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

    Endothelin-1 is known as one of the weakest vasoconstrictors produced by the endothelium.

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

    Endothelin acts on a single subtype of receptors, specifically the ET-TA receptors.

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

    Most of the effects of ET-1 are mediated through ETA receptors present in vascular smooth muscle and other tissues.

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

    Increased production of endothelin-1 is associated with a limited range of cardiovascular diseases.

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

    Endothelin antagonists are primarily used to treat acute hereditary angioedema.

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

    Vascular smooth muscle proliferation is one effect caused by the activation of ET-1 receptors.

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

    The third generation of orally active B2-receptor antagonists is no longer under study.

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

    Primary pulmonary hypertension is one condition linked with increased endothelin-1 production.

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

    What is the primary therapeutic use of triptans?

    <p>The primary therapeutic use of triptans is the treatment of acute migraine.</p> Signup and view all the answers

    What is the role of 5-HT1D receptors when activated by triptans?

    <p>Activation of 5-HT1D receptors inhibits inflammation of meninges and pain transmission.</p> Signup and view all the answers

    Why are triptans contraindicated in patients with ischemic heart disease?

    <p>Triptans can cause coronary spasm due to their action on 5-HT1B receptors, posing a risk to patients with ischemic heart disease.</p> Signup and view all the answers

    How does tegaserod function in gastrointestinal treatment?

    <p>Tegaserod functions as a specific 5-HT4 agonist, increasing gastrointestinal motility.</p> Signup and view all the answers

    What activity do 5-HT1B agonists induce in the cerebral vasculature?

    <p>5-HT1B agonists induce vasoconstriction of dilated cerebral vessels.</p> Signup and view all the answers

    What are the consequences of serotonergic drugs acting as agonists on the 5-HT2A receptor?

    <p>Activation of the 5-HT2A receptor leads to platelet aggregation and vasoconstriction.</p> Signup and view all the answers

    What receptors does cyproheptadine block?

    <p>Cyproheptadine blocks 5-HT2, H1, and muscarinic receptors.</p> Signup and view all the answers

    How do interactions with the CYP450 system affect serotonin's pharmacological actions?

    <p>Interactions with the CYP450 system can potentiate the sedative effects of serotonin drugs when combined with other substances.</p> Signup and view all the answers

    Which receptors are primarily involved in the nociceptive effects of serotonin?

    <p>The 5-HT3 and 5-HT7 receptors are primarily associated with nociception.</p> Signup and view all the answers

    What is the expected timeframe for therapeutic effects of anxiety medications to appear?

    <p>The therapeutic effects may take as long as 2 weeks to appear.</p> Signup and view all the answers

    What percentage of patients typically report relief from migraine pain within 2 hours of triptan use?

    <p>About 50%–80% of patients report relief from pain within 2 hours.</p> Signup and view all the answers

    What is the role of 5-HT4 receptors in the gastrointestinal system?

    <p>5-HT4 receptors increase gastrointestinal motility and secretions.</p> Signup and view all the answers

    Explain how 5-HT1A receptor activation can influence anxiety and cognitive processes.

    <p>Activation of the 5-HT1A receptor enhances both anxiety regulation and cognitive function.</p> Signup and view all the answers

    What pharmacological effect is primarily observed with the antagonism of 5-HT2C receptors?

    <p>Antagonism of 5-HT2C receptors is associated with appetite stimulation and potential weight gain.</p> Signup and view all the answers

    What physiological effects are associated with the activation of ET-1 through ETA receptors?

    <p>Activation of ET-1 through ETA receptors leads to potent vasoconstriction, vascular smooth muscle proliferation, and cardiac hypertrophy.</p> Signup and view all the answers

    Describe the physiological roles of serotonin in both the central nervous system and the gastrointestinal tract.

    <p>In the CNS, serotonin modulates mood and cognition, while in the GIT, it regulates motility and secretion.</p> Signup and view all the answers

    How does the distribution of serotonin in the body impact its functions?

    <p>90% of serotonin is stored in the GIT, influencing gut motility, while the remaining 10% in platelets affects vascular functions.</p> Signup and view all the answers

    Identify one condition where endotheliin-1 production is significantly increased.

    <p>Endotheliin-1 production is notably increased in primary pulmonary hypertension.</p> Signup and view all the answers

    What are the receptor subtypes that endotheliins act upon, and what is their primary impact?

    <p>Endotheliins act on ETA and ETB receptor subtypes, primarily impacting vasoconstriction and blood pressure elevation.</p> Signup and view all the answers

    How does the selectivity of ambrisentan differ from that of bosentan?

    <p>Ambrisentan is a selective ETA receptor blocker, while bosentan is a non-selective blocker of both ETA and ETB receptors.</p> Signup and view all the answers

    What is the significance of the third generation of orally active B2-receptor antagonists?

    <p>The third generation of orally active B2-receptor antagonists may provide therapeutic benefits in treating drug-induced angioedema.</p> Signup and view all the answers

    What are the primary roles of adenosine in pharmacology as mentioned in the content?

    <p>Adenosine acts as a short-acting purine A receptor agonist and is used intravenously to inhibit AV conduction and convert supraventricular tachycardia.</p> Signup and view all the answers

    How does endotheliin-1 contribute to cardiac hypertrophy?

    <p>Endotheliin-1 contributes to cardiac hypertrophy by inducing smooth muscle proliferation and promoting vascular resistance.</p> Signup and view all the answers

    Describe the conversion process of ATP once it is released into the extracellular environment.

    <p>Released ATP is rapidly converted to ADP and then to adenosine through enzymatic degradation.</p> Signup and view all the answers

    What role do endotheliins play in cardiovascular system diseases?

    <p>Endotheliins are implicated in various cardiovascular diseases, including heart failure and atherosclerosis, through their vasoconstrictor effects.</p> Signup and view all the answers

    What are the potential therapeutic focuses for B2-receptor antagonists presently under study?

    <p>The potential therapeutic focuses for B2-receptor antagonists include treatment for hereditary angioedema and drug-induced angioedema.</p> Signup and view all the answers

    What is the significance of nucleotides like ADP and ATP in cellular signaling?

    <p>Nucleotides such as ADP and ATP act as extracellular chemical mediators that engage various purine receptors to exert a range of functions.</p> Signup and view all the answers

    What clinical application involves intravenous adenosine and its mechanism of action?

    <p>Intravenous adenosine is used to convert supraventricular tachycardia to sinus rhythm by inhibiting AV conduction.</p> Signup and view all the answers

    In what way might endotheliin receptor antagonists be beneficial in clinical settings?

    <p>Endotheliin receptor antagonists may be beneficial in clinically managing conditions such as pulmonary hypertension and heart failure.</p> Signup and view all the answers

    In what way do bosentan and ambrisentan differ regarding their receptor targeting?

    <p>Bosentan blocks both ETA and ETB receptors, whereas ambrisentan selectively blocks only the ETA receptor.</p> Signup and view all the answers

    What receptors do atypical antipsychotics primarily block to improve negative symptoms of schizophrenia?

    <p>Atypical antipsychotics primarily block 5-HT2A and dopamine D2 receptors.</p> Signup and view all the answers

    Explain the physiological significance of extracellular ATP and its conversion.

    <p>Extracellular ATP serves as a signaling molecule that, upon release, rapidly converts to ADP and adenosine, influencing various physiological responses.</p> Signup and view all the answers

    What therapeutic effect do purine receptors mediate regarding cardiovascular function?

    <p>Purine receptors mediate actions that can influence heart rate, blood flow regulation, and myocardial oxygen consumption.</p> Signup and view all the answers

    What is the primary therapeutic application of ondansetron in the clinical setting?

    <p>Ondansetron is primarily used to treat nausea and vomiting associated with cancer chemotherapy.</p> Signup and view all the answers

    What physiological effects result from the activation of B2 receptors by kinins?

    <p>Activation of B2 receptors causes vasodilation, increased capillary permeability, and smooth muscle contraction.</p> Signup and view all the answers

    How does icatibant function as a selective antagonistic agent?

    <p>Icatibant acts as a selective antagonist at bradykinin B2 receptors.</p> Signup and view all the answers

    In the context of serotonin receptors, what roles do 5-HT3 blockers play in the gastrointestinal tract?

    <p>5-HT3 blockers prevent nausea and vomiting by acting on the central and peripheral 5-HT3 receptors in the GIT.</p> Signup and view all the answers

    What distinguishes the mechanism of action of atypical antipsychotics from typical ones?

    <p>Atypical antipsychotics preferentially block 5-HT2A receptors along with D2 receptors, unlike typical antipsychotics, which primarily block D2 receptors.</p> Signup and view all the answers

    What enzymatic process creates kinins from kininogen?

    <p>Kinins are formed from kininogen by the action of the kallikrein enzyme.</p> Signup and view all the answers

    What is a significant action of activating bradykinin B2 receptors besides vasodilation?

    <p>Activation of B2 receptors stimulates sensory nerves, causing pain.</p> Signup and view all the answers

    Bossentan is an orally active nonselective blocker of ET ___ and ETBB receptors.

    <p>A</p> Signup and view all the answers

    Ambrisentan is a selective ___ blocker.

    <p>ETA</p> Signup and view all the answers

    ATP is released through exocytosis or cell ___.

    <p>damage</p> Signup and view all the answers

    Adenosine is a short acting purine A receptor ___ that is given by i.v. route.

    <p>agonist</p> Signup and view all the answers

    Released ATP is rapidly converted to ADP and ___.

    <p>adenosine</p> Signup and view all the answers

    Nucleosides and nucleotides act primarily on three main families of ___ receptors.

    <p>purine</p> Signup and view all the answers

    Adenosine is administered to convert supraventricular tachycardia to ___ rhythm in patients.

    <p>sinus</p> Signup and view all the answers

    Drugs acting on purine receptors include adenosine, which inhibits ___ conduction.

    <p>AV</p> Signup and view all the answers

    Endotheliin is a vasoconstricting peptide produced by the ______.

    <p>endothelium</p> Signup and view all the answers

    Endotheliin-1 (ET-1) is one of the strongest ______ currently studied.

    <p>vasoconstrictors</p> Signup and view all the answers

    Increased production of ET-1 has been implicated in a variety of ______ diseases.

    <p>cardiovascular</p> Signup and view all the answers

    Most of ET-1 effects are mediated through ______ receptors present in vascular smooth muscle.

    <p>ETA</p> Signup and view all the answers

    Activation of ETA receptors leads to vascular smooth muscle ______, cardiac hypertrophy, and elevation of blood pressure.

    <p>proliferation</p> Signup and view all the answers

    Endotheliins act on at least 2 subtypes of receptors: ET ______ and ETB.

    <p>TA</p> Signup and view all the answers

    Endotheliin-1 is studied for its effects on diseases like primary pulmonary ______, heart failure, and coronary artery disease.

    <p>hypertension</p> Signup and view all the answers

    A 3rd generation of orally active B2-receptor ______ was developed and is currently under study.

    <p>antagonists</p> Signup and view all the answers

    5-HT is formed from the amino acid ______.

    <p>tryptophane</p> Signup and view all the answers

    Serotonin is primarily stored in the enterochromaffin tissue of the ______.

    <p>GIT</p> Signup and view all the answers

    5-HT acts on at least ______ types of receptors.

    <p>7</p> Signup and view all the answers

    5-HT2A receptors are involved in ______ aggregation.

    <p>platelet</p> Signup and view all the answers

    Activation of the 5-HT3 receptor is primarily associated with ______ and vomiting.

    <p>nausea</p> Signup and view all the answers

    5-HT4 receptors increase gastrointestinal motility and secretions through the ______ pathway.

    <p>Gs</p> Signup and view all the answers

    Buspirone activates central 5-HT1A receptors, which are involved in regulating ______.

    <p>anxiety</p> Signup and view all the answers

    The 5-HT2B receptors are primarily found in ______ muscle.

    <p>smooth</p> Signup and view all the answers

    Triptans activate 5-HT1B/1D ______.

    <p>receptors</p> Signup and view all the answers

    The major use of triptans is the treatment of acute ______.

    <p>migraine</p> Signup and view all the answers

    The therapeutic effect of medications for anxiety may take as long as ______ weeks to appear.

    <p>2</p> Signup and view all the answers

    Tegaserod is a specific 5-HT4 ______.

    <p>agonist</p> Signup and view all the answers

    Activation of 5-HT1D receptors inhibits inflammation of ______.

    <p>meninges</p> Signup and view all the answers

    Cyproheptadine blocks 5-HT2, H1, & ______ receptors.

    <p>muscarinic</p> Signup and view all the answers

    About ______% to 80% of patients report relief from pain within 2 hours of taking triptans.

    <p>50</p> Signup and view all the answers

    These drugs are contraindicated in patients with ischemic heart ______.

    <p>disease</p> Signup and view all the answers

    Histamine is used for treatment of ______ symptoms of carcinoid tumors.

    <p>symptoms</p> Signup and view all the answers

    Typical antipsychotics like Olanzapine work by blocking ______ and dopamine receptors.

    <p>5-HT2A</p> Signup and view all the answers

    Ondansetron is primarily used to treat nausea and vomiting associated with ______ chemotherapy.

    <p>cancer</p> Signup and view all the answers

    Kiniins are potent vasodilator peptides formed from protein substrates called ______.

    <p>kininogen</p> Signup and view all the answers

    Activation of B2 receptors causes increased capillary ______ and smooth muscle contraction.

    <p>permeability</p> Signup and view all the answers

    Icatibant is a second-generation decapeptide that acts as a selective ______ at bradykinin B2 receptors.

    <p>antagonist</p> Signup and view all the answers

    Selective 5-HT3 receptor blockers function in the gastrointestinal tract by affecting ______ functioning.

    <p>smooth muscle</p> Signup and view all the answers

    5-HT3 receptor blockers lead to the inhibition of ______ in the central nervous system.

    <p>nausea</p> Signup and view all the answers

    Match the following conditions with their associated treatments or uses:

    <p>Hereditary angioedema = Symptomatic treatment with B2-receptor antagonists Drug-induced angioedema = Injection therapy Ascites = B2-receptor antagonists Pancreatitis = Endothelin antagonists</p> Signup and view all the answers

    Match the following effects of endotheliin-1 with their consequences:

    <p>Vascular smooth muscle proliferation = Increased vascular resistance Cardiac hypertrophy = Elevated blood pressure Vasoconstriction = Decreased blood flow Activation of ETA receptors = Enhanced contraction of smooth muscle</p> Signup and view all the answers

    Match the following diseases with the associated increase in endotheliin-1 production:

    <p>Primary pulmonary hypertension = Increased vascular constriction Heart failure = Elevated cardiac workload Atherosclerosis = Plaque formation Coronary artery disease = Reduced blood supply</p> Signup and view all the answers

    Match the following endothelin isoforms with their primary characteristics:

    <p>Endothelin-1 (ET-1) = Strongest vasoconstrictor Endothelin-2 (ET-2) = Less potent than ET-1 Endothelin-3 (ET-3) = Involved in smooth muscle function ET receptors = Two subtypes: ETA and ETB</p> Signup and view all the answers

    Match the following pharmacological actions with their corresponding receptor types:

    <p>ETA receptor activation = Vasoconstriction ETB receptor activation = Vasodilation B2-receptor antagonist = Reduced edema 5-HT2A receptor activation = Increased neurotransmitter release</p> Signup and view all the answers

    Match the following research areas with their relevance to endothelin:

    <p>Vascular smooth muscle function = Study of ET receptor impact Cardiac hypertrophy = ET-1 role in heart adaptation Pulmonary hypertension = ET-1 as a target for therapy Drug-induced angioedema = Investigating B2-receptor antagonists</p> Signup and view all the answers

    Match the following substances with their main actions in cardiovascular physiology:

    <p>Adenosine = Inhibition of excessive cardiac activity 5-HT = Modulation of mood and vascular tone Endothelin = Stimulation of smooth muscle contraction Kinins = Regulation of blood vessel permeability</p> Signup and view all the answers

    Match the following receptors with their respective mechanisms of action:

    <p>ETA receptors = Potent vasoconstriction ETB receptors = Vasodilation under certain conditions 5-HT1A receptors = Anxiety reduction B2 receptors = Peripheral edema regulation</p> Signup and view all the answers

    Match the following drugs with their receptor selectivity:

    <p>Bossentan = Non-selective ET receptor blocker Ambrisentan = Selective ETA receptor blocker Adenosine = A receptor agonist ATP = Excitatory neurotransmitter</p> Signup and view all the answers

    Match the following purines with their roles in the body:

    <p>Adenosine = Inhibits AV conduction ATP = Stored in vesicles ADP = Converted from ATP AMP = Dephosphorylated from ADP</p> Signup and view all the answers

    Match the following characteristics with the relevant drug:

    <p>Bossentan = Approved for treatment of pulmonary hypertension Ambrisentan = Selective antagonist for ETA Adenosine = Short-acting and given intravenously ATP = Released during tissue damage</p> Signup and view all the answers

    Match the following receptors with their associated functions:

    <p>ETA = Vasoconstriction ETB = Vasodilation A receptors = Control heart rhythm Purine receptors = Wide range of cellular functions</p> Signup and view all the answers

    Match the following conversion processes with the corresponding substances:

    <p>ATP to ADP = Released during exocytosis ADP to Adenosine = Rapidly converted post-release Adenosine to AMP = Dephosphorylation ATP to AMP = Degradative process</p> Signup and view all the answers

    Match the following conditions with the appropriate regulatory substances:

    <p>Supraventricular tachycardia = Adenosine to restore sinus rhythm Pulmonary hypertension = Treatment with Ambrisentan Tissue damage = Release of ATP Cellular function = Action of purines</p> Signup and view all the answers

    Match the following drug routes with their administration forms:

    <p>Adenosine = Intravenous Ambrisentan = Oral ATP = Exocytosis Bossentan = Oral</p> Signup and view all the answers

    Match the following statements about drug actions with the corresponding drug:

    <p>Adenosine = Acts as a short-acting purine A receptor agonist Bossentan = Non-selective blocker of ET receptors Ambrisentan = Selective for ETA receptors ATP = Rapid conversion post-release to other substances</p> Signup and view all the answers

    Match the 5-HT receptor subtypes with their primary effects:

    <p>5-HT1A = Role in anxiety and cognitive function 5-HT2A = Platelet aggregation 5-HT3 = Nausea and vomiting 5-HT4 = Increased GIT motility</p> Signup and view all the answers

    Match the pharmacological actions of serotonin with their mechanisms:

    <p>5-HT1B = Decreased cAMP 5-HT2B = Increased IP3 5-HT5A = Decreased cAMP 5-HT6 = Increased cAMP</p> Signup and view all the answers

    Match the following medications with their primary uses:

    <p>Triptans = Treatment of acute migraine Tegaserod = Treatment of irritable bowel syndrome with constipation Cyproheptadine = Blocks 5-HT2, H1, &amp; muscarinic receptors Anxiolytics = Treatment of anxiety disorders</p> Signup and view all the answers

    Match the clinical uses of 5-HT agonists with their corresponding drug:

    <p>Buspirone = Anxiety treatment via 5-HT1A receptor activation Triptans = Migraine relief via vasoconstriction Ondansetron = Nausea and vomiting control Citalopram = Depression treatment via serotonin reuptake inhibition</p> Signup and view all the answers

    Match the receptor types with their locations:

    <p>5-HT1A = CNS and cranial blood vessels 5-HT2A = Platelets 5-HT3 = Area postrema 5-HT4 = CNS and enteric nervous system</p> Signup and view all the answers

    Match the receptor types with their effects:

    <p>5-HT1B = Causes vasoconstriction of dilated cerebral vessels 5-HT1D = Inhibits inflammation of meninges 5-HT4 = Increases gastrointestinal motility 5-HT2 = Mediates various central nervous system effects</p> Signup and view all the answers

    Match the interactions that potentiate the effects of 5-HT activity:

    <p>Hypnotics = Increased sedation effect Alcohol = Enhanced sedative effect CYP450 inhibitors = Increased drug metabolism Monoamine oxidase inhibitors = Increased 5-HT levels</p> Signup and view all the answers

    Match the side effects with the respective medication:

    <p>Triptans = Coronary spasm contraindication Tegaserod = Gastrointestinal-related adverse effects Cyproheptadine = Drowsiness due to H1 receptor blockade Anxiolytics = Potential for dependence</p> Signup and view all the answers

    Match the action with the corresponding receptor type:

    <p>5-HT1B receptor activation = Vasoconstriction 5-HT1D receptor activation = Reduced pain transmission 5-HT4 receptor activation = Enhanced gastric motility 5-HT2 receptor blockade = Prevention of serotonin-related side effects</p> Signup and view all the answers

    Match the 5-HT receptor subtypes to their signal transduction pathways:

    <p>5-HT1A = Gi pathway 5-HT2A = Gq pathway 5-HT3 = Na+ ion channel 5-HT4 = Gs pathway</p> Signup and view all the answers

    Match the pharmacological actions with the appropriate drug:

    <p>Sumatriptan = Migraine relief via 5-HT1B/1D activation Zolmitriptan = Migraine relief with quicker onset Naratriptan = Longer duration of migraine action Cyproheptadine = Antihistamine effect and 5-HT blockade</p> Signup and view all the answers

    Match the 5-HT receptor subtype with its characteristic dysfunction when activated:

    <p>5-HT2C = Hallucinations 5-HT1D = Nociception 5-HT1B = Vasoconstriction 5-HT4 = Increased gastrointestinal secretions</p> Signup and view all the answers

    Match the conditions treated with the respective drug:

    <p>Triptans = Acute migraines Tegaserod = Irritable bowel syndrome with constipation Cyproheptadine = Allergic reactions and appetite stimulation Anxiolytics = Chronic anxiety disorders</p> Signup and view all the answers

    Match the condition associated with 5-HT receptors with its related effects:

    <p>Anxiety = Increased 5-HT1A activity Migraine = 5-HT1B receptor activation Nausea = 5-HT3 receptor involvement Constipation = 5-HT4 receptor stimulation</p> Signup and view all the answers

    Match the mechanism of action with the corresponding drug:

    <p>Triptans = Activate 5-HT1B/1D receptors Tegaserod = 5-HT4 agonism Cyproheptadine = Blocks multiple receptor types Anxiolytics = Enhances GABAergic activity</p> Signup and view all the answers

    Match the type of receptor with its primary function:

    <p>5-HT1B = Vasoconstriction of cerebral vessels 5-HT1D = Inhibition of pain pathways 5-HT4 = Promotion of gastric motility 5-HT2 = Role in mood and cognition</p> Signup and view all the answers

    Match the pharmacological agents with their primary uses:

    <p>Olanzapine = Treatment of schizophrenia Ondansetron = Nausea &amp; vomiting during chemotherapy Icatibant = Selective antagonist at bradykinin receptors Granisetron = Management of gastrointestinal symptoms</p> Signup and view all the answers

    Match the receptor type with its main action:

    <p>5-HT2A receptors = Blockade leads to improvement of negative symptoms in schizophrenia B1 receptors = Involved in regulation of vascular permeability D2 receptors = Inhibition decreases dopamine activity in the CNS B2 receptors = Causes vasodilation and smooth muscle contraction</p> Signup and view all the answers

    Match the substance with its characteristic effect:

    <p>Kinins = Vasodilator peptides causing pain Kallikrein = Enzyme that releases kinins from kininogen 5-HT3 receptors = Involved in mediating nausea and vomiting Atypical antipsychotics = Block 5-HT2A and D2 receptors</p> Signup and view all the answers

    Match the drug with its mechanism of action:

    <p>Icatibant = Selective antagonist of bradykinin B2 receptors Granisetron = Blocks 5-HT3 receptors centrally Ondansetron = Selective blockade in the chemoreceptor trigger zone (CTZ) Olanzapine = Blocks dopamine and serotonin receptors</p> Signup and view all the answers

    Match the therapeutic application with the drug:

    <p>Ondansetron = Chemotherapy-induced nausea Icatibant = Acute treatment of bradykinin-related angioedema Granisetron = Prevention of chemotherapy-related vomiting Olanzapine = Management of psychotic disorders</p> Signup and view all the answers

    Match the effect with the corresponding receptor:

    <p>5-HT3 receptor activation = Nausea and vomiting sensation B1 and B2 receptors = Vascular effects and smooth muscle contraction D2 receptor blockade = Decreased dopamine-related symptoms 5-HT2A receptor blockade = Reduction of schizophrenia symptoms</p> Signup and view all the answers

    Match the peptide with its description:

    <p>Bradykinin = Causes vasodilation and increases pain sensitivity Kinins = Potent vasodilator peptides derived from kininogen Kallikrein = Enzyme that converts kininogen to bradykinin B2 receptors = Key targets for bradykinin action in the vascular system</p> Signup and view all the answers

    Match the agent with its specific receptor target:

    <p>Icatibant = Bradykinin B2 receptor Ondansetron = 5-HT3 receptor Olanzapine = 5-HT2A receptor and D2 receptor Granisetron = 5-HT3 receptor</p> Signup and view all the answers

    Study Notes

    Hereditary Angioedema and Treatment

    • Injection used for symptomatic treatment of acute attacks in hereditary angioedema.
    • Potential application in drug-induced angioedema, ascites, and pancreatitis.
    • A third generation of orally active B2-receptor antagonists is currently under study.

    Endothelins

    • Endothelin is a vasoconstricting peptide produced by the endothelium.
    • Three isoforms exist; Endothelin-1 (ET-1) is one of the strongest vasoconstrictors under investigation.
    • Endothelins affect two receptor subtypes: ET_A and ET_B.
    • Most effects of ET-1 are mediated through ETA receptors in vascular smooth muscle tissues.
    • Activation of ET-1 receptors triggers vasoconstriction, smooth muscle proliferation, cardiac hypertrophy, and increased blood pressure.
    • High production of ET-1 is linked to various cardiovascular diseases such as primary pulmonary hypertension, heart failure, atherosclerosis, and coronary artery disease.
    • Bosentan is a non-selective oral blocker of ETA and ET_B receptors; ambrisentan selectively blocks ETA receptors.
    • Both drugs are approved for treating pulmonary hypertension.

    Purines as Mediators

    • Nucleosides (e.g., adenosine) and nucleotides (e.g., ADP, ATP) serve as extracellular mediators.
    • ATP is stored in vesicles, released via exocytosis or tissue damage, and is rapidly converted to ADP and adenosine.
    • Purines act on three main families of purine receptors with diverse functions.

    Adenosine

    • Short-acting purine A receptor agonist administered intravenously to inhibit AV conduction.
    • Effective in converting supraventricular tachycardia to sinus rhythm in non-asthmatic patients.
    • Associated with orthostatic hypotension, particularly in patients with liver disease.
    • Withdrawn from the market due to dangerous interactions, especially with sedatives and alcohol affecting the CYP450 system.

    Serotonin (5-Hydroxytryptamine; 5-HT)

    • 5-HT derived from tryptophan, primarily stored in enterochromaffin tissue (90%) and platelets (10%).
    • Functions as a neurotransmitter in various CNS areas.
    • No clinically useful drugs directly affect its synthesis or metabolism, but many drugs target 5-HT receptors.
    • 5-HT acts on multiple receptor subtypes with various distribution and effects, influencing anxiety, appetite, thermoregulation, and pain perception.

    5-HT Agonists in Clinical Use

    • Buspirone activates central 5-HT_1A receptors for anxiety disorder treatment, effects may take up to two weeks.
    • Triptans (e.g., sumatriptan, zolmitriptan) activate 5-HT_1B/1D receptors, primarily used for acute migraine relief with 50-80% effectiveness within 2 hours. Contraindicated in ischemic heart disease due to potential coronary spasms.
    • Tegaserod selectively stimulates 5-HT_4 receptors to increase GI motility, useful for irritable bowel syndrome with constipation.

    5-HT Antagonists in Clinical Use

    • Cyproheptadine blocks 5-HT_2, H1, and muscarinic receptors, indicated for carcinoid tumor symptoms and as an antihistamine.
    • Atypical antipsychotics (e.g., Olanzapine, Risperidone) block 5-HT_2A and dopamine D2 receptors, addressing negative symptoms of schizophrenia.
    • Ondansetron and Granisetron selectively block 5-HT_3 receptors to treat nausea and vomiting linked to cancer chemotherapy.

    Kinins

    • Kinins are potent vasodilator peptides formed from kininogen by kallikrein.
    • They act on B1 and B2 receptor subtypes; B2 activation leads to vasodilation, increased capillary permeability, and smooth muscle contraction.
    • Icatibant is a second-generation decapeptide acting as a selective antagonist at bradykinin B2 receptors, administered subcutaneously.

    Hereditary Angioedema and Treatment

    • Injection used for symptomatic treatment of acute attacks in hereditary angioedema.
    • Potential application in drug-induced angioedema, ascites, and pancreatitis.
    • A third generation of orally active B2-receptor antagonists is currently under study.

    Endothelins

    • Endothelin is a vasoconstricting peptide produced by the endothelium.
    • Three isoforms exist; Endothelin-1 (ET-1) is one of the strongest vasoconstrictors under investigation.
    • Endothelins affect two receptor subtypes: ET_A and ET_B.
    • Most effects of ET-1 are mediated through ETA receptors in vascular smooth muscle tissues.
    • Activation of ET-1 receptors triggers vasoconstriction, smooth muscle proliferation, cardiac hypertrophy, and increased blood pressure.
    • High production of ET-1 is linked to various cardiovascular diseases such as primary pulmonary hypertension, heart failure, atherosclerosis, and coronary artery disease.
    • Bosentan is a non-selective oral blocker of ETA and ET_B receptors; ambrisentan selectively blocks ETA receptors.
    • Both drugs are approved for treating pulmonary hypertension.

    Purines as Mediators

    • Nucleosides (e.g., adenosine) and nucleotides (e.g., ADP, ATP) serve as extracellular mediators.
    • ATP is stored in vesicles, released via exocytosis or tissue damage, and is rapidly converted to ADP and adenosine.
    • Purines act on three main families of purine receptors with diverse functions.

    Adenosine

    • Short-acting purine A receptor agonist administered intravenously to inhibit AV conduction.
    • Effective in converting supraventricular tachycardia to sinus rhythm in non-asthmatic patients.
    • Associated with orthostatic hypotension, particularly in patients with liver disease.
    • Withdrawn from the market due to dangerous interactions, especially with sedatives and alcohol affecting the CYP450 system.

    Serotonin (5-Hydroxytryptamine; 5-HT)

    • 5-HT derived from tryptophan, primarily stored in enterochromaffin tissue (90%) and platelets (10%).
    • Functions as a neurotransmitter in various CNS areas.
    • No clinically useful drugs directly affect its synthesis or metabolism, but many drugs target 5-HT receptors.
    • 5-HT acts on multiple receptor subtypes with various distribution and effects, influencing anxiety, appetite, thermoregulation, and pain perception.

    5-HT Agonists in Clinical Use

    • Buspirone activates central 5-HT_1A receptors for anxiety disorder treatment, effects may take up to two weeks.
    • Triptans (e.g., sumatriptan, zolmitriptan) activate 5-HT_1B/1D receptors, primarily used for acute migraine relief with 50-80% effectiveness within 2 hours. Contraindicated in ischemic heart disease due to potential coronary spasms.
    • Tegaserod selectively stimulates 5-HT_4 receptors to increase GI motility, useful for irritable bowel syndrome with constipation.

    5-HT Antagonists in Clinical Use

    • Cyproheptadine blocks 5-HT_2, H1, and muscarinic receptors, indicated for carcinoid tumor symptoms and as an antihistamine.
    • Atypical antipsychotics (e.g., Olanzapine, Risperidone) block 5-HT_2A and dopamine D2 receptors, addressing negative symptoms of schizophrenia.
    • Ondansetron and Granisetron selectively block 5-HT_3 receptors to treat nausea and vomiting linked to cancer chemotherapy.

    Kinins

    • Kinins are potent vasodilator peptides formed from kininogen by kallikrein.
    • They act on B1 and B2 receptor subtypes; B2 activation leads to vasodilation, increased capillary permeability, and smooth muscle contraction.
    • Icatibant is a second-generation decapeptide acting as a selective antagonist at bradykinin B2 receptors, administered subcutaneously.

    Hereditary Angioedema and Treatment

    • Injection used for symptomatic treatment of acute attacks in hereditary angioedema.
    • Potential application in drug-induced angioedema, ascites, and pancreatitis.
    • A third generation of orally active B2-receptor antagonists is currently under study.

    Endothelins

    • Endothelin is a vasoconstricting peptide produced by the endothelium.
    • Three isoforms exist; Endothelin-1 (ET-1) is one of the strongest vasoconstrictors under investigation.
    • Endothelins affect two receptor subtypes: ET_A and ET_B.
    • Most effects of ET-1 are mediated through ETA receptors in vascular smooth muscle tissues.
    • Activation of ET-1 receptors triggers vasoconstriction, smooth muscle proliferation, cardiac hypertrophy, and increased blood pressure.
    • High production of ET-1 is linked to various cardiovascular diseases such as primary pulmonary hypertension, heart failure, atherosclerosis, and coronary artery disease.
    • Bosentan is a non-selective oral blocker of ETA and ET_B receptors; ambrisentan selectively blocks ETA receptors.
    • Both drugs are approved for treating pulmonary hypertension.

    Purines as Mediators

    • Nucleosides (e.g., adenosine) and nucleotides (e.g., ADP, ATP) serve as extracellular mediators.
    • ATP is stored in vesicles, released via exocytosis or tissue damage, and is rapidly converted to ADP and adenosine.
    • Purines act on three main families of purine receptors with diverse functions.

    Adenosine

    • Short-acting purine A receptor agonist administered intravenously to inhibit AV conduction.
    • Effective in converting supraventricular tachycardia to sinus rhythm in non-asthmatic patients.
    • Associated with orthostatic hypotension, particularly in patients with liver disease.
    • Withdrawn from the market due to dangerous interactions, especially with sedatives and alcohol affecting the CYP450 system.

    Serotonin (5-Hydroxytryptamine; 5-HT)

    • 5-HT derived from tryptophan, primarily stored in enterochromaffin tissue (90%) and platelets (10%).
    • Functions as a neurotransmitter in various CNS areas.
    • No clinically useful drugs directly affect its synthesis or metabolism, but many drugs target 5-HT receptors.
    • 5-HT acts on multiple receptor subtypes with various distribution and effects, influencing anxiety, appetite, thermoregulation, and pain perception.

    5-HT Agonists in Clinical Use

    • Buspirone activates central 5-HT_1A receptors for anxiety disorder treatment, effects may take up to two weeks.
    • Triptans (e.g., sumatriptan, zolmitriptan) activate 5-HT_1B/1D receptors, primarily used for acute migraine relief with 50-80% effectiveness within 2 hours. Contraindicated in ischemic heart disease due to potential coronary spasms.
    • Tegaserod selectively stimulates 5-HT_4 receptors to increase GI motility, useful for irritable bowel syndrome with constipation.

    5-HT Antagonists in Clinical Use

    • Cyproheptadine blocks 5-HT_2, H1, and muscarinic receptors, indicated for carcinoid tumor symptoms and as an antihistamine.
    • Atypical antipsychotics (e.g., Olanzapine, Risperidone) block 5-HT_2A and dopamine D2 receptors, addressing negative symptoms of schizophrenia.
    • Ondansetron and Granisetron selectively block 5-HT_3 receptors to treat nausea and vomiting linked to cancer chemotherapy.

    Kinins

    • Kinins are potent vasodilator peptides formed from kininogen by kallikrein.
    • They act on B1 and B2 receptor subtypes; B2 activation leads to vasodilation, increased capillary permeability, and smooth muscle contraction.
    • Icatibant is a second-generation decapeptide acting as a selective antagonist at bradykinin B2 receptors, administered subcutaneously.

    Hereditary Angioedema and Treatment

    • Injection used for symptomatic treatment of acute attacks in hereditary angioedema.
    • Potential application in drug-induced angioedema, ascites, and pancreatitis.
    • A third generation of orally active B2-receptor antagonists is currently under study.

    Endothelins

    • Endothelin is a vasoconstricting peptide produced by the endothelium.
    • Three isoforms exist; Endothelin-1 (ET-1) is one of the strongest vasoconstrictors under investigation.
    • Endothelins affect two receptor subtypes: ET_A and ET_B.
    • Most effects of ET-1 are mediated through ETA receptors in vascular smooth muscle tissues.
    • Activation of ET-1 receptors triggers vasoconstriction, smooth muscle proliferation, cardiac hypertrophy, and increased blood pressure.
    • High production of ET-1 is linked to various cardiovascular diseases such as primary pulmonary hypertension, heart failure, atherosclerosis, and coronary artery disease.
    • Bosentan is a non-selective oral blocker of ETA and ET_B receptors; ambrisentan selectively blocks ETA receptors.
    • Both drugs are approved for treating pulmonary hypertension.

    Purines as Mediators

    • Nucleosides (e.g., adenosine) and nucleotides (e.g., ADP, ATP) serve as extracellular mediators.
    • ATP is stored in vesicles, released via exocytosis or tissue damage, and is rapidly converted to ADP and adenosine.
    • Purines act on three main families of purine receptors with diverse functions.

    Adenosine

    • Short-acting purine A receptor agonist administered intravenously to inhibit AV conduction.
    • Effective in converting supraventricular tachycardia to sinus rhythm in non-asthmatic patients.
    • Associated with orthostatic hypotension, particularly in patients with liver disease.
    • Withdrawn from the market due to dangerous interactions, especially with sedatives and alcohol affecting the CYP450 system.

    Serotonin (5-Hydroxytryptamine; 5-HT)

    • 5-HT derived from tryptophan, primarily stored in enterochromaffin tissue (90%) and platelets (10%).
    • Functions as a neurotransmitter in various CNS areas.
    • No clinically useful drugs directly affect its synthesis or metabolism, but many drugs target 5-HT receptors.
    • 5-HT acts on multiple receptor subtypes with various distribution and effects, influencing anxiety, appetite, thermoregulation, and pain perception.

    5-HT Agonists in Clinical Use

    • Buspirone activates central 5-HT_1A receptors for anxiety disorder treatment, effects may take up to two weeks.
    • Triptans (e.g., sumatriptan, zolmitriptan) activate 5-HT_1B/1D receptors, primarily used for acute migraine relief with 50-80% effectiveness within 2 hours. Contraindicated in ischemic heart disease due to potential coronary spasms.
    • Tegaserod selectively stimulates 5-HT_4 receptors to increase GI motility, useful for irritable bowel syndrome with constipation.

    5-HT Antagonists in Clinical Use

    • Cyproheptadine blocks 5-HT_2, H1, and muscarinic receptors, indicated for carcinoid tumor symptoms and as an antihistamine.
    • Atypical antipsychotics (e.g., Olanzapine, Risperidone) block 5-HT_2A and dopamine D2 receptors, addressing negative symptoms of schizophrenia.
    • Ondansetron and Granisetron selectively block 5-HT_3 receptors to treat nausea and vomiting linked to cancer chemotherapy.

    Kinins

    • Kinins are potent vasodilator peptides formed from kininogen by kallikrein.
    • They act on B1 and B2 receptor subtypes; B2 activation leads to vasodilation, increased capillary permeability, and smooth muscle contraction.
    • Icatibant is a second-generation decapeptide acting as a selective antagonist at bradykinin B2 receptors, administered subcutaneously.

    Hereditary Angioedema and Treatment

    • Injection used for symptomatic treatment of acute attacks in hereditary angioedema.
    • Potential application in drug-induced angioedema, ascites, and pancreatitis.
    • A third generation of orally active B2-receptor antagonists is currently under study.

    Endothelins

    • Endothelin is a vasoconstricting peptide produced by the endothelium.
    • Three isoforms exist; Endothelin-1 (ET-1) is one of the strongest vasoconstrictors under investigation.
    • Endothelins affect two receptor subtypes: ET_A and ET_B.
    • Most effects of ET-1 are mediated through ETA receptors in vascular smooth muscle tissues.
    • Activation of ET-1 receptors triggers vasoconstriction, smooth muscle proliferation, cardiac hypertrophy, and increased blood pressure.
    • High production of ET-1 is linked to various cardiovascular diseases such as primary pulmonary hypertension, heart failure, atherosclerosis, and coronary artery disease.
    • Bosentan is a non-selective oral blocker of ETA and ET_B receptors; ambrisentan selectively blocks ETA receptors.
    • Both drugs are approved for treating pulmonary hypertension.

    Purines as Mediators

    • Nucleosides (e.g., adenosine) and nucleotides (e.g., ADP, ATP) serve as extracellular mediators.
    • ATP is stored in vesicles, released via exocytosis or tissue damage, and is rapidly converted to ADP and adenosine.
    • Purines act on three main families of purine receptors with diverse functions.

    Adenosine

    • Short-acting purine A receptor agonist administered intravenously to inhibit AV conduction.
    • Effective in converting supraventricular tachycardia to sinus rhythm in non-asthmatic patients.
    • Associated with orthostatic hypotension, particularly in patients with liver disease.
    • Withdrawn from the market due to dangerous interactions, especially with sedatives and alcohol affecting the CYP450 system.

    Serotonin (5-Hydroxytryptamine; 5-HT)

    • 5-HT derived from tryptophan, primarily stored in enterochromaffin tissue (90%) and platelets (10%).
    • Functions as a neurotransmitter in various CNS areas.
    • No clinically useful drugs directly affect its synthesis or metabolism, but many drugs target 5-HT receptors.
    • 5-HT acts on multiple receptor subtypes with various distribution and effects, influencing anxiety, appetite, thermoregulation, and pain perception.

    5-HT Agonists in Clinical Use

    • Buspirone activates central 5-HT_1A receptors for anxiety disorder treatment, effects may take up to two weeks.
    • Triptans (e.g., sumatriptan, zolmitriptan) activate 5-HT_1B/1D receptors, primarily used for acute migraine relief with 50-80% effectiveness within 2 hours. Contraindicated in ischemic heart disease due to potential coronary spasms.
    • Tegaserod selectively stimulates 5-HT_4 receptors to increase GI motility, useful for irritable bowel syndrome with constipation.

    5-HT Antagonists in Clinical Use

    • Cyproheptadine blocks 5-HT_2, H1, and muscarinic receptors, indicated for carcinoid tumor symptoms and as an antihistamine.
    • Atypical antipsychotics (e.g., Olanzapine, Risperidone) block 5-HT_2A and dopamine D2 receptors, addressing negative symptoms of schizophrenia.
    • Ondansetron and Granisetron selectively block 5-HT_3 receptors to treat nausea and vomiting linked to cancer chemotherapy.

    Kinins

    • Kinins are potent vasodilator peptides formed from kininogen by kallikrein.
    • They act on B1 and B2 receptor subtypes; B2 activation leads to vasodilation, increased capillary permeability, and smooth muscle contraction.
    • Icatibant is a second-generation decapeptide acting as a selective antagonist at bradykinin B2 receptors, administered subcutaneously.

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    Description

    This quiz covers the symptomatic treatment of acute attacks of hereditary angioedema, including the use of injections and third-generation orally active B2-receptor antagonists. It also discusses related conditions like drug-induced angioedema and vasoconstrictors such as endothelins. Test your knowledge on these important treatments and their applications.

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