Pharm

Reserpine

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Reserpine, Serpasil

  • Background
  1. Limited use in modern medicine due to adverse effects
  • Indications
  1. No modern day significant indications
  2. Prior use in mental health
  3. Prior use in Hypertension
    1. Typically used with Diuretic to counter fluid retention and augment Blood Pressure control
  • Mechanism
  1. Alkaloid derived from Rauwolfia serpentine and Rauwolfia vomitoria
  2. Lipid soluble and crosses blood-brain barrier
    1. Results in sedation and allows for use in mental health, including as Antipsychotic
  3. Alpha adrenergic uptake inhibitor
    1. Depletes CNS and peripheral Catecholamine stores (Norepinephrine, Serotonin, Dopamine)
      1. Reserpine binds and inactivates Catecholamine pump on Neuron storage vessicles
      2. Catecholamines that fail to enter storage vessicles from cytoplasm, are destroyed (via monoamine oxidase)
      3. Peripheral Nerve terminals are depleted of Norepinephrine, Serotonin, Dopamine
      4. Results in decreased Catecholamine release on nerve depolarization
    2. Antihypertensive
      1. Decreases Peripheral Vascular Resistance
      2. Decreases Heart Rate
      3. Decreases Cardiac Output
  • Pharmacokinetics
  1. Prolonged duration of effects
  2. High bioavailability after oral ingestion
  3. Extensively metabolized
  • Adverse Effects
  1. Increased Cholinergic effects ("SLUDGE + Killer B's")
    1. Parasympathetic predominance when Sympathetic System is blocked
    2. Bradycardia
    3. Bronchoconstriction
    4. Bronchorrhea
    5. Salivation
    6. Lacrimation
    7. Diarrhea
  2. Other effects
    1. Postural Hypotension
    2. Peptic Ulcers
    3. Sedation
    4. Suicidal Ideation
    5. Gynecomastia
  • Drug Interactions
  1. MAO inhibitors
    1. Severe Hypertension
    2. Do not use Reserpine within 2 weeks of a MAO inhibitor
  2. AV Nodal Blockers (e.g. Digitalis, Quinidine, Beta Blockers)
    1. Severe Bradycardia or Heart Block
  3. Direct Acting Catecholamines (e.g. Norepinephrine, Epinephrine)
    1. Reserpine significantly potentiates direct Catecholamine activity
  4. CNS Depressants
    1. Reserpine potentiates activity
  5. Antihypertensives
    1. Reserpine potentiates activity
  • Safety
  1. Lactation: Avoid
  2. Pregnancy: Category C
  • Dosing
  1. Start: 0.05 to 0.1 mg orally daily
  2. Max: 0.25 mg/day
  • References
  1. Olson (2020) Clinical Pharmacology, MedMaster, Miami, p. 64-5
  2. Hamilton (2010) Tarascon Pocket Pharmacopeia, Jones and Bartlett, p. 76