Hypertension reserpine

At lower doses used for treatment of mild hypertension, reserpine lowers blood pressure by a combination of decreased cardiac output and decreased peripheral vascular resistance. 

A third study (85) enrolled 7825 hypertensive patients (55% males and 45% females) having diastoHc blood pressures (DBP) of 99—104 mm Hg (13—14 Pa) there were no placebo controls. Forty-six percent of the patients were assigned to SC antihypertensive dmg therapy, ie, step 1, chlorthaUdone step 2, reserpine [50-55-5] or methyldopa [555-30-6], and step 3, hydralazine [86-54-4]. Fifty-four percent of the patients were assigned to the usual care (UC) sources in the community. Significant reductions in DBP and in cardiovascular and noncardiovascular deaths were noted in both groups. In the SC group, deaths from ischemic heart disease increased 9%, and deaths from coronary heart disease (CHD) and acute myocardial infarctions were reduced 20 and 46%, respectively. 

Levodopa interacts with many different drugs. When levodopa is used with phenytoin, reserpine, and papaverine, there is a decrease in response to levodopa The risk of a hypertensive crisis increases when levodopa is used with the monoamine oxidase inhibitors (see Chap. 31). Foods high in pyridoxine (vitamin B6) or vitamin B6 preparations reverse the effect of levodopa However, when carbidopa is used with levodopa, pyridoxine has no effect on the action of levodopa hi fact, when levodopa and carbidopa are given together, pyridoxine may be prescribed to decrease the adverse effects associated with levodopa... 

Other Agents Reserpine No recommendations at this time Mental depression May be used in resistant hypertension when combined with a thiazide... 

But that was only one half of the logic behind the chemical-imbalance theory. The other half came from studies of reserpine, a drug that was extracted from Rauvolfia serpentina or the Indian snakeroot plant, which had historically been used to treat snakebite, hypertension, insomnia and insanity. In studies of animals, reserpine was reported to induce sedation and to decrease brain levels of norepinephrine, serotonin and dopamine. Clinical reports indicated that some people became severely depressed when taking reserpine.14 Putting these two findings together, it seemed likely that reserpine made people depressed because it decreased neurotransmitter levels. 

Reserpine A drug extracted from Rauwolfia serpentina which was once clinically used in the treatment of essential hypertension and schizophrenia. 

Because of their reflex cardiac effect, vasodilators, if used alone in the treatment of hypertension, have not been a successful therapeutic tool. However, the reflex tachycardia and increase in cardiac output can be effectively blocked by the therapeutic association with a sympathetic blocker guanethidine, reserpine, methyldopa, or clonidine. More specifically, blockade of the cardiac beta-adrenergic receptors will also prevent the cardiac response to hydralazine. Thus, the therapeutic combination of hydralazine and propranolol can be successfully employed for effective blood pressure reduction(11). 

It is of note that the two drugs ushered in the new era of psychopharmacology. The advent of a host of synthetic antipsychotic agents has diminished the importance of reserpine for this indication. The agent is still frequently prescribed in the treatment of hypertension, as are its closely related congener, res-clnnamine (31), and the semisynthetic compound syrosingopine (32). 

Reserpine is used for treating hypertension however, it is not the drug of choice because of a number of side effects. A number of drugs combined with other hypertensive agents— diuretics in particular—are based on reserpine. Reserpine is prescribed under a number of names, including serpasil, brinerdin, diupres, and others. 

In the sympathetic nervous system there is the possibility to reduce the release of noradrenaline. The alkaloid reserpine is known to interfere with the ability of the postganglionic sympathetic nerves to store noradrenaline. This results in a reduction of the sympathetic tone which is a useful measure in the treatment of essential hypertension. These type of drugs are classified as antisympathotonics. 

Since the main clinical use for antisympathotonics is in the treatment of essential hypertension, such drugs will be discussed in Chapter 20 in more detail. The alkaloid reserpine from Rauwolfia serpentina was the first drug used clinically to reduce sympathetic tone. Reserpine reduce the ability of storage and release of various transmitters (adrenaline, noradrenaline, serotonine and dopamine) by an irreversible destruction of the axonal vesicle membranes. The duration of the reserpine effect is actually determined by the de novo synthesis of these structure. Beside various central side effects like sedation, depression, lassitude and nightmares the pattern of unwanted effects of reserpine is determined by the shift of the autonomic balance towards the parasympathetic branch myosis, congested nostrils, an altered saliva production, increased gastric acid production, bardycardia and diarrhea. As a consequence of the inhibition of central dopamine release, reserpine infrequently shows Parkinson-like disturbances of the extrapyramidal system. 

The chief use of reserpine is in the treatment of mild to moderate hypertension. As with other sympathetic depressant drugs, tolerance to the antihypertensive effects of reserpine can occur, owing to a compensatory increase in blood volume that frequently accompanies decreased peripheral vascular resistance. Reserpine, therefore, should be used in conjunction with a diuretic. 

Because of its sedative properties, reserpine offers special benefit to hypertensive patients who exhibit symptoms of agitated psychotic states and who may be unable to tolerate therapy with phenothiazine derivatives. 

Paralleling these clinical developments were basic pharmacological studies, which noted that reserpine ( 5, 6, 7 and 8) and a-methyidopa produced depression in patients treated for hypertension ( 9,10 and 11). The fact that the MAOIs and TCAs functionally increased norepinephrine (NE) activity while reserpine lowered its activity led Schiidkraut (12) and Bunney and Davis (13) to independently formulate the NE hypothesis of depression. This same line of reasoning was also applied to serotonin (5-HT) (14, 15). 

Jensen K. Depression in patients treated with reserpine for arterial hypertension. Acta Psychiatr Neuroi Scand 1959 34 195-204. 

Reserpine, an alkaloid extracted from the roots of an Indian plant, Rauwolfia serpentina, was one of the first effective drugs used on a large scale in the treatment of hypertension. At present, it is rarely used owing to its adverse effects. 

Reserpine Blocks vesicular amine transporter in noradrenergic nerves and depletes transmitter stores Reduce all sympathetic effects, especially cardiovascular, and reduce blood pressure Hypertension but rarely used Oral long duration (days) Toxicity Reserpine psychiatric depression, gastrointestinal disturbances ... 

Rauvolfia verticilata (Lour.) Baill. Luo Fu Mu (root) Reserpine, rescinnamine, beta-sitosterol, aricine, vellosimine, peraksine, serpentine, robinin.33-39-510 Treat hypertension, psychosis, schizophrenia. 

Reserpine is a raulwolfia alkaloid isolated from the roots of the plant Rauwolfia Serpentina. It is used for the treatment of mild essential hypertension or psychosis. 

In 1918 the traditional Indian remedy rauwolfia was reported to be useful in the treatment of hypertension. Reexamination of this material led to the isolation of reserpine (28 R1 = Me, R2 = 3,4,5-trimethoxybenzoyl) which was shown in 1952 to have hypotensive and tranquilizing effects. Other alkaloids such as deserpidine (28 R1 = H, R2 = 3,4,5-trimethoxybenzoyl) and rescinnamine (28 R1 = Me, R2 = 3,4,5-trimethoxycinnamoyl) were later isolated. They are useful when alternative, more potent drugs are not well tolerated. 

One method used for the control of hypertension is reduction of the impulses flowing from the CNS to the sympathetic nervous system which controls the tone of the cardiovascular system. The veratrum alkaloids do this at doses that are near the emetic dose, and reserpine acts both centrally and peripherally. The imidazoline clonidine (175) and some analogues in which the chlorine is replaced by fluorine or methyl groups decrease sympathetic outflow and cause vasomotor relaxation. However, they cause sedation, lack of saliva and renewed hypertension on withdrawal of the drug. 

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