11. AUTOCOIDS

Written and reviewed by Dr. Saint Paul | Pharm.D Graduate from JNTUK | Pharmacy Educator and D.Pharmacy Academic Content Creator

Understanding Autocoids: The “Local Hormones” of the Body

In the world of pharmacology, autocoids occupy a unique space. Derived from the Greek words autos (self) and akos (healing), these are chemical signals produced by cells that act locally at the site where they are released. Unlike systemic hormones that travel through the blood, autocoids are like “neighborhood messengers.”

In this guide, we’ll dive into the three heavyweights of the autocoid world: Histamine, Serotonin, and Prostaglandins.


1. Histamine: The Immune Responder

Histamine is an amine found in nearly all animal tissues, primarily stored in mast cells. It is famous for its role in allergic reactions, but its job is much broader.

Physiological Roles:

  • Cardiovascular: It dilates small arterioles (causing a drop in BP) and increases capillary permeability, leading to Oedema (swelling).
  • Gastric Acid: It is a potent stimulator of stomach acid secretion via H₂ receptors.
  • Nervous System: It stimulates sensory nerves, causing the classic “itch” or pain associated with insect bites.
  • Smooth Muscle: It causes the bronchial muscles to constrict, which is why it’s a major factor in Asthma.

The “Triple Response” of Lewis:

When histamine is injected into the skin, it produces three distinct signs:

  1. Red Spot: Localized vasodilation.
  2. Flare: A brighter red flush caused by axon reflexes.
  3. Wheal: Swelling caused by fluid leaking from capillaries.

2. Antihistamines: H₁ vs. H₂ Blockers

We use drugs called antihistamines to block these effects. They are generally categorized by the receptor they target:

ClassExamplesPrimary Use
1st Gen H₁ BlockersDiphenhydramine, PromethazineAllergies, Motion Sickness, Sleep aid (cause drowsiness).
2nd Gen H₁ BlockersCetirizine, Loratadine, Fexofenadine“Non-drowsy” allergy relief.
H₂ BlockersRanitidine, Famotidine, CimetidineTreating Peptic Ulcers and Gastric Acidity.

3. Serotonin (5-HT): The Mood and Vessel Regulator

5-Hydroxytryptamine (5-HT), commonly known as Serotonin, is a neurotransmitter derived from the amino acid Tryptophan.

Key Functions:

  • CVS: Complex actions that can cause both vasoconstriction and vasodilation.
  • Digestive: Increases intestinal motility; stimulation of 5-HT₃ receptors in the brain leads to nausea and vomiting.
  • CNS: Regulates sleep, mood, appetite, and body temperature.

5-HT Drugs in Clinical Practice:

  • Triptans (Sumatriptan): Selective 5-HT agonists used to stop acute Migraine attacks.
  • Ondansetron: A 5-HT₃ antagonist used to prevent vomiting in cancer patients.
  • SSRIs (Fluoxetine): Antidepressants that increase serotonin activity in the brain.

4. Prostaglandins: The Lipid Signals

Prostaglandins are unique because they are derived from fatty acids (Arachidonic Acid). They act as high-power local signals for inflammation and repair.

Biological Impact:

  • Reproduction: They facilitate labor by dilating the cervix and contracting the uterus.
  • Stomach: They protect the gastric lining by decreasing acid and increasing mucus.
  • Kidneys: They maintain blood flow and regulate the release of renin.
  • Pain: Prostaglandins sensitize nerve endings to pain, which is why Aspirin and NSAIDs work by blocking their synthesis.

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