Reserpine

Not to be confused with Reserpidine or Risperidone.
Reserpine
resperine 2D skeletal
resperine 3D BS
Clinical data
Trade namesSerpasil, others
AHFS/Drugs.comConsumer Drug Information
MedlinePlusa601107
License data
Pregnancy
category
  • C
Routes of
administration		Oral
ATC code
Legal status
Legal status
  • Rx-only (banned/discontinued in some countries)
Pharmacokinetic data
Bioavailability50%
Metabolismgut/liver
Elimination half-lifephase 1 = 4.5h,
phase 2 = 271h,
average = 33h
Excretion62% feces / 8% urine
Identifiers
  • methyl (3β,16β,17α,18β,20α)-11,17-dimethoxy-18-[(3,4,5-trimethoxybenzoyl)oxy]yohimban-16-carboxylate and
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.000.044 Edit this at Wikidata
Chemical and physical data
FormulaC33H40N2O9
Molar mass608.688 g·mol−1
3D model (JSmol)
  • [H][C@]26C[C@@H](OC(=O)c1cc(OC)c(OC)c(OC)c1)[C@H](OC)[C@@H](C(=O)OC)[C@@]2([H])C[C@]5([H])c4[nH]c3cc(OC)ccc3c4CCN5C6
  • InChI=1S/C33H40N2O9/c1-38-19-7-8-20-21-9-10-35-16-18-13-27(44-32(36)17-11-25(39-2)30(41-4)26(12-17)40-3)31(42-5)28(33(37)43-6)22(18)15-24(35)29(21)34-23(20)14-19/h7-8,11-12,14,18,22,24,27-28,31,34H,9-10,13,15-16H2,1-6H3/t18-,22+,24-,27-,28+,31+/m1/s1 checkY
  • Key:QEVHRUUCFGRFIF-MDEJGZGSSA-N checkY
  (verify)

Reserpine is a drug that is used for the treatment of high blood pressure, usually in combination with a thiazide diuretic or vasodilator.[1] Large clinical trials have shown that combined treatment with reserpine plus a thiazide diuretic reduces mortality of people with hypertension. Although the use of reserpine as a solo drug has declined since it was first approved by the FDA in 1955,[2] the combined use of reserpine and a thiazide diuretic or vasodilator is still recommended in patients who do not achieve adequate lowering of blood pressure with first-line drug treatment alone.[3][4][5] The reserpine-hydrochlorothiazide combo pill was the 17th most commonly prescribed of the 43 combination antihypertensive pills available in 2012.[6]

The antihypertensive actions of reserpine are largely due to its antinoradrenergic effects, which are a result of its ability to deplete catecholamines (among other monoamine neurotransmitters) from peripheral sympathetic nerve endings. These substances are normally involved in controlling heart rate, force of cardiac contraction and peripheral vascular resistance.[7]

At doses of 0.05 to 0.2 mg per day, reserpine is well tolerated;[8] the most common adverse effect being nasal stuffiness.

Reserpine has also been used for relief of psychotic symptoms.[9] A review found that in persons with schizophrenia, reserpine and chlorpromazine had similar rates of adverse effects, but that reserpine was less effective than chlorpromazine for improving a person's global state.[10]

  1. ^ Tsioufis C, Thomopoulos C (November 2017). "Combination drug treatment in hypertension". Pharmacological Research. 125 (Pt B): 266–271. doi:10.1016/j.phrs.2017.09.011. PMID 28939201. S2CID 32904492.
  2. ^ "Reserpine".
  3. ^ James PA, Oparil S, Carter BL, Cushman WC, Dennison-Himmelfarb C, Handler J, et al. (February 2014). "2014 evidence-based guideline for the management of high blood pressure in adults: report from the panel members appointed to the Eighth Joint National Committee (JNC 8)". JAMA. 311 (5): 507–20. doi:10.1001/jama.2013.284427. PMID 24352797.
  4. ^ Weir MR (August 2020). "Reserpine: A New Consideration of and Old Drug for Refractory Hypertension". American Journal of Hypertension. 33 (8): 708–710. doi:10.1093/ajh/hpaa069. PMC 7402223. PMID 32303749.
  5. ^ Barzilay J, Grimm R, Cushman W, Bertoni AG, Basile J (August 2007). "Getting to goal blood pressure: why reserpine deserves a second look". Journal of Clinical Hypertension. 9 (8): 591–4. doi:10.1111/j.1524-6175.2007.07229.x. PMC 8110058. PMID 17673879.
  6. ^ Wang B, Choudhry NK, Gagne JJ, Landon J, Kesselheim AS (March 2015). "Availability and utilization of cardiovascular fixed-dose combination drugs in the United States". American Heart Journal. 169 (3): 379–386.e1. doi:10.1016/j.ahj.2014.12.014. PMID 25728728.
  7. ^ Forney, Barbara. Reserpine for Veterinary Use Wedgewood Pharmacy. 2001-2002.
  8. ^ Morley JE (May 2014). "Treatment of hypertension in older persons: what is the evidence?". Drugs & Aging. 31 (5): 331–7. doi:10.1007/s40266-014-0171-7. PMID 24668034. S2CID 207489850.
  9. ^ Hoenders HJ, Bartels-Velthuis AA, Vollbehr NK, Bruggeman R, Knegtering H, de Jong JT (February 2018). "Natural Medicines for Psychotic Disorders: A Systematic Review". The Journal of Nervous and Mental Disease. 206 (2): 81–101. doi:10.1097/NMD.0000000000000782. PMC 5794244. PMID 29373456.
  10. ^ Nur S, Adams CE (April 2016). "Chlorpromazine versus reserpine for schizophrenia". The Cochrane Database of Systematic Reviews. 2016 (4): CD012122. doi:10.1002/14651858.CD012122.pub2. PMC 10350329. PMID 27124109.