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 |