II. Background

  1. Limited use in modern medicine due to adverse effects

III. 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

V. 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

VI. Pharmacokinetics

  1. Prolonged duration of effects
  2. High bioavailability after oral ingestion
  3. Extensively metabolized

VII. 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

VIII. 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

IX. Safety

  1. Lactation: Avoid
  2. Pregnancy: Category C

X. Dosing

  1. Start: 0.05 to 0.1 mg orally daily
  2. Max: 0.25 mg/day

XI. References

  1. Olson (2020) Clinical Pharmacology, MedMaster, Miami, p. 64-5
  2. Hamilton (2010) Tarascon Pocket Pharmacopeia, Jones and Bartlett, p. 76

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Ontology: Reserpine (C0035179)

Definition (NCI) An alkaloid, derived from the roots of Rauwolfia serpentine and vomitoria, and an adrenergic uptake inhibitor with antihypertensive effects. Reserpine is lipid soluble and can penetrate blood-brain barrier. This agent binds and inhibits catecholamine pump on the storage vesicles in central and peripheral adrenergic neurons, thereby inhibiting the uptake of norepinephrine, dopamine serotonin into presynaptic storage vesicles. This results in catecholamines and serotonin lingering in the cytoplasm where they are destroyed by intraneuronal monoamine oxidase, thereby causing the depletion of catecholamine and serotonin stores in central and peripheral nerve terminals. Depletion results in a lack of active transmitter discharge from nerve endings upon nerve depolarization, and consequently leads to a decreased heart rate and decreased arterial blood pressure as well as sedative effects.
Definition (MSH) An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.
Definition (CSP) alkaloid isolated from the root of Rauwolfia species, used as an antihypertensive and sedative.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D012110
SnomedCT 363523003, 387447004, 78379001
English Reserpine, Yohimban-16-carboxylic acid, 11,17-dimethoxy-18-((3,4,5-trimethoxybenzoyl)oxy)-, methyl ester, (3beta,16beta,17alpha,18beta,20alpha)-, (3beta,16beta,17alpha,18beta,20alpha)-11,17-Dimethoxy-18-[(3,4,5-trimethoxybenzoyl)oxy]yohimban-16-carboxylic Acid Methyl Ester, reserpine, reserpine (medication), Reserpine [Chemical/Ingredient], RESERPINE, Reserpine - chemical, Reserpine - chemical (substance), Reserpine (product), Reserpine (substance)
Swedish Reserpin
Czech reserpin
Finnish Reserpiini
Russian REZERPIN, RESTSINNAMIN, SIRINGOPIN, SIROSINGOPIN, РЕЗЕРПИН, РЕСЦИННАМИН, СИРИНГОПИН, СИРОСИНГОПИН
Japanese レセルピン
Croatian REZERPIN
Polish Rezerpina, Serpazyl
Spanish reserpina - sustancia química (sustancia), reserpina - sustancia química, reserpina (producto), reserpina (sustancia), reserpina, Reserpina
French Réserpine
German Reserpin
Italian Reserpina
Portuguese Reserpina

Ontology: Serpasil (C0729168)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D012110
English Serpasil