Cam-Ap-Es;Demi-Regroton;Diupres-250;Diupres-500;Diutensen-R;Dralserp;Hiserpia;Hydrap-ES;Hydromox R;Hydroserpine Plus (R-H-H);Metatensin #2;Metatensin #4;Naquival;Novoreserpine;Rau-Sed;Regroton;Renese-R;Reserfia;Salutensin;Salutensin-Demi;Sandril;Ser-A-Gen;Serpalan;Serpanray;Serpasil;Serpasil-Apresoline;Serpasil-Esidrix #1;Serpasil-Esidrix #2;Serpate;Serpivite;Unipres;

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. [PubChem]

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• Bell pharmacal corp
• Bowman pharmaceuticals inc
• Bristol myers squibb co
• Cm bundy co
• Eli lilly and co
• Elkins sinn div ah robins co inc
• Everylife
• Halsey drug co inc
• Impax laboratories inc
• Ivax pharmaceuticals inc sub teva pharmaceuticals usa
• Lannett co inc
• Marshall pharmacal corp
• Mk laboratories inc
• Mylan pharmaceuticals inc
• Novartis pharmaceuticals corp
• Panray corp sub ormont drug and chemical co inc
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• Teva pharmaceuticals usa inc
• Vale chemical co inc
• Valeant pharmaceuticals international
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• Watson laboratories inc
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• Whiteworth towne paulsen inc

• Apotheca Inc.
• C.O. Truxton Inc.
• Carlisle Laboratories Inc.
• Dispensing Solutions
• Eon Labs
• H and H Laboratories
• Major Pharmaceuticals
• Murfreesboro Pharmaceutical Nursing Supply
• Physicians Total Care Inc.
• Quality Research Pharmaceutical Inc.
• United Research Laboratories Inc.

Synthesis Reference

Not Available

General Reference

: Five-year findings of the hypertension detection and follow-up program. I. Reduction in mortality of persons with high blood pressure, including mild hypertension. Hypertension Detection and Follow-up Program Cooperative Group. JAMA. 1979 Dec 7;242(23):2562-71. Pubmed : Effects of treatment on morbidity in hypertension. Results in patients with diastolic blood pressures averaging 115 through 129 mm Hg. JAMA. 1967 Dec 11;202(11):1028-34. Pubmed : Prevention of stroke by antihypertensive drug treatment in older persons with isolated systolic hypertension. Final results of the Systolic Hypertension in the Elderly Program (SHEP). SHEP Cooperative Research Group. JAMA. 1991 Jun 26;265(24):3255-64. Pubmed Chobanian AV, Bakris GL, Black HR, Cushman WC, Green LA, Izzo JL Jr, Jones DW, Materson BJ, Oparil S, Wright JT Jr, Roccella EJ: The Seventh Report of the Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure: the JNC 7 report. JAMA. 2003 May 21;289(19):2560-72. Epub 2003 May 14. Pubmed Moser M: “Cost containment” in the management of hypertension. Ann Intern Med. 1987 Jul;107(1):107-9. Pubmed

Type	small molecule

Classes

Alkaloids and Alkaloid Derivatives

Substructures

Carboxylic Acids and Derivatives Benzyl Alcohols and Derivatives Acetates Indoles and Indole Derivatives Benzoates Phenols and Derivatives Pyrroles Alkaloids and Alkaloid Derivatives Ethers Benzene and Derivatives Aliphatic and Aryl Amines Catechols Heterocyclic compounds Aromatic compounds Anisoles Tryptamines and Derivatives Imines Benzoyl Derivatives (Iso)quinolines and Derivatives Phenyl Esters Gallic Acid and Derivatives Piperidines

ANTIHYPERTENSIVES 降血压;

Indication	Foe the treatment of hypertension
Pharmacodynamics	Reserpine is an adrenergic blocking agent used to treat mild to moderate hypertension via the disruption of norepinephrine vesicular storage. The antihypertensive actions of Reserpine are a result of its ability to deplete catecholamines from peripheral sympathetic nerve endings. These substances are normally involved in controlling heart rate, force of cardiac contraction and peripheral resistance.
Mechanism of action	Reserpine's mechanism of action is through inhibition of the ATP/Mg2+ pump responsible for the sequestering of neurotransmitters into storage vesicles located in the presynaptic neuron. The neurotransmitters that are not sequestered in the storage vesicle are readily metabolized by monoamine oxidase (MAO) causing a reduction in catecholamines.
Absorption	Not Available
Volume of distribution	Not Available
Protein binding	62%
Metabolism	Not Available
Route of elimination	Reserpine is extensively metabolized to inactive compounds. It is slowly excreted via the urine and feces.
Half life	Not Available
Clearance	Not Available
Toxicity	Possible human carcinogen. May cause reproductive harm. ORL-RAT LD50 420 mg/kg; IPR-RAT LD50 44 mg/kg; IVN-RAT LD50 15 mg/kg; ORL-MUS LD50 200 mg/kg; SCU-MUS LD50 52 mg/kg; IPR-RBT LD50 7 mg/kg
Affected organisms	Humans and other mammals
Pathways	Not Available

Properties
State	solid
Experimental Properties	Property Value Source melting point 264.5 °C PhysProp water solubility 73 mg/L (at 30 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992) logP 3.2 Not Available pKa 6.6 MERCK INDEX (1996)
Predicted Properties	Property Value Source water solubility 1.13e-02 g/l ALOGPS logP 4.05 ALOGPS logP 3.53 ChemAxon logS -4.7 ALOGPS pKa (strongest acidic) 16.29 ChemAxon pKa (strongest basic) 7.56 ChemAxon physiological charge 1 ChemAxon hydrogen acceptor count 8 ChemAxon hydrogen donor count 1 ChemAxon polar surface area 117.78 ChemAxon rotatable bond count 10 ChemAxon refractivity 161.42 ChemAxon polarizability 66.05 ChemAxon

Drug	Interaction
Dobutamine	Increased arterial pressure
Dopamine	Increased arterial pressure
Ephedra	Increased arterial pressure
Ephedrine	Increased arterial pressure
Epinephrine	Increased arterial pressure
Fenoterol	Increased arterial pressure
Iobenguane	May diminish the therapeutic effect and increase chances of producing a false negative imaging result of Iobenguane as it depletes or inhibit reuptake of noradrenaline stores
Isoproterenol	Increased arterial pressure
Mephentermine	Increased arterial pressure
Metaraminol	Increased arterial pressure
Methoxamine	Increased arterial pressure
Norepinephrine	Increased arterial pressure
Orciprenaline	Increased arterial pressure
Phenylephrine	Increased arterial pressure
Phenylpropanolamine	Increased arterial pressure
Pirbuterol	Increased arterial pressure
Procaterol	Increased arterial pressure
Pseudoephedrine	Increased arterial pressure
Salbutamol	Increased arterial pressure
Terbutaline	Increased arterial pressure
Tetrabenazine	Reserpine may increase the adverse/toxic effects of tetrabenazine as they have similar pharmacologic properties. Concomitant therapy is contraindicated.
Topotecan	The p-glycoprotein inhibitor, Reserpine, may increase the bioavailability of oral Topotecan. A clinically significant effect is also expected with IV Topotecan. Concomitant therapy should be avoided.
Tranylcypromine	Addition of Reserpine to Tranylcypromine therapy may induce paradoxical Reserpine effects, including peripheral hypertension and central exciation. Close monitoring for adverse effects is required. Addition of Tranylcypromine to Reserpine therapy may be less of a concern.
Treprostinil	Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Triprolidine	The CNS depressants, Triprolidine and Reserpine, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.

• Magnesium, potassium and zinc needs increased.
• Take with food to reduce irritation. Avoid alcohol.