Reserpine - instructions for use, doses, side effects, contraindications

Clinical and pharmacological group: & nbsp

Included in the formulation

АТХ:

C.02.A.A Rawwolfia alkaloids

C.02.A.A.02 Reserpine

Pharmacodynamics:

Depletion of the norepinephrine depot (destruction in the axoplasm of the MAO) inpostganglionic sympathetic nerve endings by blocking the vesicular transport (sympatholytic action, sustained reduction in blood pressure), reducing the level of noradrenaline (sedative effect), serotonin (depressing action) and dopamine (antipsychotic effect) in brain neurons.

Pharmacokinetics:

Absorption is fast. F 50%. Does not bind to plasma proteins. Biotransformation in the liver. Half-life. Initial 4.5 hr, the final - 45-168 hours, with chronic renal insufficiency - 87-323 h slow elimination: kidneys 8% as metabolites, <1% in unmodified form with the faeces> 60% in the form of unchanged substance. Not removed by hemodialysis.

Indications:

Arterial hypertension.

ICD-10

IX.I10-I15.I10 Essential [primary] hypertension

Contraindications:

Depression, gastric ulcer and duodenal ulcer in acute ulcerative colitis in the acute phase of bronchial asthma, bradycardia, severe diseases of the cardiovascular system, atherosclerosis, cerebral vascular nephrosclerosis, pregnancy, lactation. Do not apply before electropulse therapy.

Pregnancy and lactation:

Contraindicated in pregnancy and during breastfeeding.

Recommendations FDA category C.

Dosing and Administration:

Individual. In adults, use in a dose of 200-500 mcg / day, if necessary, increase the dose. The maximum daily dose is 1 mg.

Children can use in a dose of 80-400 mcg / day in 2-4 doses, depending on the age.

Side effects:

From the cardiovascular system: bradycardia; when used in high doses - increased symptoms of angina pectoris.

From the digestive system: nausea, vomiting, diarrhea, abdominal pain; with prolonged use in high doses may impair liver function.

From the side of the central nervous system and the peripheral nervous system: drowsiness, fatigue, depressive conditions, puffiness and dryness of mucous membranes; when used in high doses - nightmarish dreams, the development of symptoms of Parkinsonism.

From the urinary system: retention of urine, increased frequency of urination.

Dermatological reactions: herpes, itching.

Other: weight gain, decreased libido, decreased potency.

Overdose:

Symptoms: dizziness, severe drowsiness, redness of the skin, narrowed pupils,slow pulse (indirect cholinomimetic action).

Treatment: symptomatic. Observation - at least 72 hours.

Interaction:

β-Adrenoblockers - mutual enhancement of pharmacological effects.

Adreno- and sympathomimetics - mutual decrease in activity.

Alcohol and drugs that depress the central nervous system - Increased depressive effect.

Antihypertensive drugs - potentiation of antihypertensive effect.

Anticholinergics - decrease in the effect on gastric secretion.

Bromocriptine - a decrease in the effect on the level of prolactin, a correction of the dose of bromocriptine is necessary.

MAO inhibitors, including selegiline; also furazolidone and procarbazine - sudden hypertension and hyperpyrexia. Do not recommend applying reserpine during treatment with MAO inhibitors and for 1 week after their cancellation.

Levodopa - decrease in effect, requires an increase in the dose of levodopa.

NSAIDs, especially indomethacin, - reduction of antihypertensive effect.

Cardiac glycosides, quinidine pro - arrhythmic effect.

Means that cause extrapyramidal disorders - Potentiation of extrapyramidal disorders.

Special instructions:

Sympatholytics is referred to second-line drugs for hypertension and psychosis due to numerous side effects and low efficiency.

Monitoring: regular monitoring of blood pressure.

Distinctive features:

Rauwolfia alkaloid serpentine (Rauwolfia serpentina Benth).

Impotence and erectile dysfunction are more pronounced in comparison with captopril.

The effect on the central nervous system is dose-dependent, often manifested when doses above 0.5 mg / day are used.

Instructions

Reserpine (Reserpinum)