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Histamine, Serotonin, & the Ergot Alkaloids (Pharmacology) - Coggle…

- - - - Diphenhydramine,
        dimenhydrinate
        
        Clinical Applications
        
        Hay fever, angioedema,
        motion sickness - used orally as OTC sleep aid ,Used parenteral for dystonia.
        
        Pharmacokinetics
        
        Oral, parenteral
        Duration: 6–8 h
        
        Mechanism of Action
        
        Competitive pharmacologic
        block of peripheral and CNS H1 receptors plus α- and M-receptor
        block. Anti-motion sickness effect
        
        Toxicities, Interactions
        
        Sedation, autonomic block
        Rare CNS excitation
      - Promethazine
        
        : H1 blocker with less anti-motion sickness action and more sedative and autonomic effects
      - Chlorpheniramine:
        
        H1 blocker with negligible anti-motion sickness, sedative, and autonomic effects
      - Cyclizine:
        
        : H1 blocker with more anti-motion sickness action and less sedative and autonomic effect
    - - Cetirizine
        
        Mechanism of Action
        
        Competitive pharmacologic
        block of peripheral H1 receptors. No autonomic or anti-motion sickness effects
        
        Pharmacokinetics
        
        Oral
        Duration: 12–24 h
        
        Clinical Applications
        
        Hay fever, angioedema
        
        Toxicities, Interactions
        
        Minimal toxicities
      - Fexofenadine, loratadine, desloratadine
        
        very similar to cetirizine
  - - - Gastroesophageal reflux disease, stress ulcers
    - - Oral, parenteral
        Duration (large doses): 12–24 h
    - - Competitive pharmacologic
        block.No H1, autonomic, or
        anti-motion effects
    - - Cimetidine: drug interactions;
        other H2 blockers much less
    - - Cimetidine famotidine
      - ranitidine
      - nizatidine
- - - - Sumatriptan
        
        Clinical Applications
        
        Migraine and cluster headache
        
        Pharmacokinetics
        
        Oral, inhaled,
        parenteral
        Duration: 2–4 h
        
        Mechanism of Action
        
        5-HT 1D21B Agonist -Cause Vasoconstiction -Modulate Neurotransmitter release
        
        Toxicities, Interactions
        
        Paresthesias, dizziness, chest pain -Possible Coronary Vasospasm.
      - Almotriptan, eletriptan, frovatriptan, naratriptan, rizatriptan, zolmitriptan
        
        very similar to sumatriptan; injectable preparations not available
    - - Tegaserod
        
        Clinical Applications
        
        Constipation-dominant
        irritable bowel syndrome (restricted use)
        
        Pharmacokinetics
        
        Oral
        Duration: 12 h
        
        Mechanism of Action
        
        Partial agonist at 5-HT4 receptors
        
        Toxicities, Interactions
        
        Diarrhea, ischemic colitis
  - - - Granisetron, dolasetron, palonosetron
        
        like ondansetron
      - Alosetron
        
        approved for treatment of diarrhea-predominant irritable bowel syndrome
      - Ondansetron
        
        Mechanism of Action
        
        Pharmacologic antagonist ,Block chemoreceptor trigger zone and enteric nervous system 5HT3 receptors
        
        Clinical Applications
        
        Chemotherapy and postoperative vomiting
        
        Toxicities, Interactions
        
        QT prolongation, possible arrhythmias
        
        Pharmacokinetics
        
        Oral, IV
        Duration: 3–6 h
    - - Ketanserin
        
        Clinical Applications
        
        Hypertension, carcinoid
        tumor (not available in United States)
        
        Mechanism of Action
        
        Competitive 5-HT2 and α1 receptor block
        
        Pharmacokinetics
        
        Oral
        Duration: 12–24 h
        
        Toxicities, Interactions
        
        Hypotension
- - - - Migraine, cluster headache
    - - Oral
        Duration 10–12 h
    - - Partial agonist at 5-HT and α adrenoceptors, especially in vessels
    - - Nausea, vomiting, diarrhea, severe vasospasm
  - - - Partial agonist at 5-HT and α adrenoceptors, especially in uterus
    - - Postpartum uterine bleeding
    - - Oral
        Duration 10–12 h
    - - Nausea, vomiting, diarrhea,
        severe vasospasm
  - - - Clinical Applications
        
        None (abused
        hallucinogen)
      - Pharmacokinetics
        
        Oral
        Duration hours
      - Mechanism of Action
        
        Partial 5-HT2 agonist; CNS
        dopamine D2 agonist
      - Toxicities, Interactions
        
        ANS activation, cardiovascular
        instability
    - - Mechanism of Action
        
        Partial agonist at dopamine
        receptors
      - Clinical Applications
        
        Prolactinemia
      - Pharmacokinetics
        
        Oral
        Duration 10–20 h
      - Toxicities, Interactions
        
        Hallucinations