Generic Name:  Reserpine.

Trade Name    : Reserpine , Serpasil.

Drug Class  : Peripherally acting sympathetic inhibitors, Antiadrenergic agents.

Forms of The Drug

  • Tablet: 0.1mg , 0.25mg.

Mechanism of Action.

The mechanism of action of reserpine revolves around its ability to interfere with the storage and release of neurotransmitters, specifically norepinephrine and dopamine, within nerve cells (neurons). Neurons communicate with each other through the release and reception of these chemical messengers, known as neurotransmitters, at specialized junctions called synapses. This communication is essential for various physiological processes, including the regulation of blood pressure and mood.

Reserpine’s mechanism of action can be summarized as follows:

  1. Vesicular Monoamine Transporter (VMAT) Inhibition: Inside nerve cells, norepinephrine and dopamine are stored in vesicles (small membrane-bound sacs) within the cytoplasm. These vesicles protect neurotransmitters from being prematurely released. Reserpine acts by inhibiting the function of a protein called the vesicular monoamine transporter (VMAT), specifically VMAT2. VMAT2 is responsible for packaging neurotransmitters into vesicles. By inhibiting VMAT2, reserpine prevents the packaging of norepinephrine and dopamine into vesicles, thus reducing their storage.
  2. Depletion of Neurotransmitter Stores: With VMAT2 inhibited, the stored norepinephrine and dopamine are gradually depleted. As a result, there are fewer neurotransmitters available for release when nerve cells receive signals to communicate. This depletion of neurotransmitter stores has an impact on the overall functioning of the sympathetic nervous system, which plays a key role in regulating blood pressure, heart rate, and other physiological responses.
  3. Reduction of Sympathetic Activity: The sympathetic nervous system is responsible for the “fight or flight” response, which involves increasing heart rate, constricting blood vessels, and elevating blood pressure. By reducing the availability of norepinephrine, a key neurotransmitter in the sympathetic nervous system, reserpine dampens the activity of this system. This leads to relaxation of blood vessels and a decrease in blood pressure.

Indications

  1. Hypertension (High Blood Pressure).
  2. Psychiatric Disorders.
  3. Hypertensive Crises.
  4. Tourette Syndrome.

Contraindications

  1. Depression and Mental Health Disorders.
  2. Peptic Ulcer Disease.
  3. Parkinson’s Disease.
  4. Pregnancy and Breastfeeding.
  5. Severe Cardiovascular Disease.
  6. History of Drug Allergies.
  7. Renal Impairment.
  8. Concurrent Use with Monoamine Oxidase Inhibitors (MAOIs).

Side Effects

  1. Angina.
  2. Bradycardia.
  3. Anorexia.
  4. Peripheral edema.
  5. Syncope.
  6. Premature ventricular contractions.
  7. Dizziness.
  8. Depression.
  9. Lethargy.
  10. Pruritus.
  11. Weight gain.
  12. Thrombocytopenia purpura.
  13. Gynecomastia.
  14. Rash.
  15. Nightmare.
  16. Nervousness.
  17. Paradoxical anxiety.
  18. Tardive dyskinesia.
  19. GI hypersecretion.
  20. Impotence.
  21. Blurred vision.
  22. Optic atrophy.
  23. Decreased libido.
  24. Nasal congestion.

Drug Interaction

Other drugs that can interact with it.

  1. Monoamine Oxidase Inhibitors (MAOIs).
  2. Antihypertensive Medications.
  3. Central Nervous System Depressants.
  4. Tricyclic Antidepressants (TCAs).
  5. Levodopa and Dopamine Agonists.
  6. Sympathomimetic Agents: Drugs that mimic the effects of sympathetic nervous system activation, such as decongestants and certain asthma medications.
  7. Lithium.
  8. Warfarin.
  9. CNS Stimulants: Stimulant medications, like amphetamines and certain ADHD medications.
  10. Potassium-Depleting Diuretics.

Precautions

  1. Pregnancy: Category C.
  2. Lactation: Reserpine is a medication that is excreted into breast milk, and its use during lactation can have potential effects on both the nursing infant and the mother. Therefore, the decision to use reserpine during breastfeeding should be made with careful consideration of the benefits and risks involved.

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