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