Dopamine
Biochemist Saransk
1798 Items
2019-09-19
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Clinical Pharmacology
Cardiotonic, hypertensive, vasodilator, diuretic. Stimulates beta-adrenoreceptors (in small and medium doses) and alpha-adrenoreceptors (in large doses). Improving systemic hemodynamics leads to a diuretic effect. It has a specific stimulating effect on postsynaptic dopamine receptors in the smooth muscles of the blood vessels and kidneys. At low doses (0.5–3 mcg / kg / min), it acts primarily on dopamine receptors, causing dilation of the renal, mesenteric, coronary and cerebral vessels. Expansion of the renal vessels leads to increased renal blood flow, increased glomerular filtration rate, increased diuresis and excretion of sodium; Mesenteric vessels are also dilated (thus, the effect of dopamine on the renal and mesenteric vessels differs from that of other catecholamines). In low and medium doses (2-10 μg / kg / min), it stimulates postsynaptic beta1-adrenoreceptors, which causes a positive inotropic effect and an increase in the minute blood volume (IOC). Systolic blood pressure (BP) and pulse pressure may increase; however, diastolic blood pressure does not change or slightly increases. Total peripheral vascular resistance (OPS) usually does not change. Coronary blood flow and myocardial oxygen consumption, as a rule, increase. At high doses (10 mcg / kg / min or more), alpha1-adrenoreceptor stimulation prevails, causing an increase in OPSS, heart rate (HR) and narrowing of the renal vessels (the latter may decrease previously increased renal blood flow and diuresis). Due to an increase in IOC and OPSS, both systolic and diastolic blood pressure increases. The beginning of the therapeutic effect is within 5 minutes on the background of intravenous administration and lasts for 10 minutes.
Indications
Shock of various genesis (cardiogenic shock, postoperative, hypovolemic, infectious - toxic, anaphylactic shock, hypovolemic (only after the recovery of circulating blood volume); acute cardio - vascular insufficiency, syndrome of "low cardiac output" in cardiac patients, arterial hypertension.
Composition
Active substance:dopamine hydrochloride - 40 g
Excipients: sodium metabisulfite, hydrochloric acid 0.1 M solution, water for injection up to 1 l.
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Dosage and Administration
IV the drip. The dose is set individually, depending on the severity of the shock and the patient's response to treatment. To enhance diuresis and to obtain an inotropic effect (an increase in the contractile activity of the myocardium), it is administered at a rate of 100-250 μg / min (1.5-3.5 μg / kg / min) (low dose range). With intensive surgical therapy - 300-700 mcg / min (4-10 mcg / kg / min) (medium dose range); with septic shock - 750–1500 mcg / min (10.5–21 mcg / kg / min) (maximum dose range). In order to affect blood pressure, it is recommended to increase the dose to 500 mcg / min or more, or with a constant dose of dopamine, norepinephrine (norepinephrine) is additionally prescribed at a dose of 5 mcg / min and the patient weighs about 70 kg. If a heart rhythm disturbance occurs, regardless of the dose used, a further dose increase is contraindicated. Children are given a dose of 4-6 (maximum 10) mcg / kg / min. Unlike adults, in children the dose should be increased gradually, that is, starting from the smallest dose. The rate of administration should be selected individually for optimal patient response. In most patients, it is possible to maintain a satisfactory condition with the use of dopamine doses of less than 20 mcg / kg / min. Duration of use: the duration of the infusion depends on the individual characteristics of the patient. There is a positive experience with an infusion of up to 28 days. After stabilization of the clinical situation, the abolition of the drug produced gradually.
Adverse reactions
On the part of the cardiovascular system: less often - angina, tachycardia or bradycardia, palpitations, chest pain, increased or decreased blood pressure, conduction disturbances, expansion of the QRS complex, vasospasm, when used in high doses - ventricular arrhythmia.
On the part of the digestive system: more often - nausea, vomiting.
On the part of the nervous system: more often - headache; less often - anxiety, motor restlessness, tremor.
Allergic reactions: in patients with bronchial asthma - bronchospasm, shock.
Other: less often - shortness of breath, azotemia, piloerection, rarely - polyuria (when administered in low doses).
Local reactions: when the drug gets under the skin - skin necrosis, s / c fiber.
Contraindications
Hypersensitivity to the drug (including other sympathomimetics), idiopathic hypertrophic subaortic stenosis, thyrotoxicosis, pheochromocytoma, angle-closure glaucoma, benign prostatic hyperplasia with clinical manifestations, tachyarrhythmia, ventricular fibrillation It should not be prescribed for arrhythmias in combination with monoamine oxidase inhibitors, with cyclopropane and halogen-containing means for anesthesia.
Drug interactions
With the simultaneous appointment of dopamine and guanethidine, sympathomimetic effects are enhanced. Patients who are treated with monoamine oxidase inhibitors need a significant reduction in the dose of dopamine (up to about 1/10 of the normal dose). The simultaneous administration of dopamine and diuretic agents may entail a summing and potentiating effect. Interactions between dopamine and tricyclic antidepressants, painkillers (increased tendency to cardiac arrhythmias) and phenytoin (lowering blood pressure and bradycardia) are also known. In combination with ergot alkaloids, dopamine can lead to maximum narrowing of peripheral vessels, which creates the danger of gangrene.
Pregnancy and Lactation
During pregnancy, the drug should be used only if the benefit to the mother outweighs the possible risk to the fetus.
Special instructions
With increased pre- and afterloading to the myocardium, a combination with nitroglycerin or sodium nitroprusside is recommended for unloading the heart.
Overdosage
Symptoms: excessive increase in blood pressure, peripheral arterial spasm, tachycardia, ventricular premature beats, angina pectoris, dyspnea, headache, psychomotor agitation.
Treatment: due to the rapid elimination of dopamine from the body, these phenomena are stopped when the dose is reduced or the administration is discontinued, with short-acting alpha-blockers (with an excessive increase in blood pressure) and beta-blockers (with rhythm disturbances).
- Brand name: Dopamine Hydrochloride
- Active ingredient: Dopamine
- Dosage form: Concentrate for preparation of solution for intravenous administration.
- Manufacturer: Biochemist Saransk
- Country of Origin: Russia
Studies and clinical trials of Dopamine (Click to expand)
- Dopamine D4 receptor variant in Africans, D4Valine194Glycine, is insensitive to dopamine and clozapine: Report of a homozygous individual
- Further association study on dopamine D2 receptor variant S311C in schizophrenia and affective disorders
- Lack of association between dopamine D2 receptor gene Cys311 variant and schizophrenia
- Lack of imprinting of the human dopamine D4 receptor (DRD4) gene
- No evidence for a major gene effect of the dopamine D4 receptor gene in the susceptibility to Gilles de la Tourette syndrome in five Canadian families
- Association study between schizophrenia and dopamine D3 receptor gene polymorphism
- Dopamine transporter gene polymorphism and psychiatric symptoms seen in schizophrenic patients at their first episode
- No evidence of association between structural polymorphism at the dopamine D3 receptor locus and alcoholism in the Japanese
- No evidence for association of dopamine D2 receptor variant (Ser 311/Cys311) with major psychosis
- No association of dopamine D2 receptor molecular variant Cys311 and schizophrenia in Chinese patients
- Systematic screening for mutations in the 5′-regulatory region of the human dopamine D1 receptor (DRD1) gene in patients with schizophrenia and bipolar affective disorder
- Assessment of association of D3 dopamine receptorMscI polymorphism with schizophrenia: Analysis of symptom ratings, family history, age at onset, and movement disorders
- Dopamine DRD2/Cys311 is not associated with chronic schizophrenia
- Lack of association betweenTaqI A1 allele of dopamine D2 receptor gene and alcohol-use disorders in Atayal natives of Taiwan
- Association study of schizophrenia and the dopamine D3 receptor gene locus in two independent samples
- Possible locus for bipolar disorder near the dopamine transporter on chromosome 5
- Further evidence of no association between Ser9Gly polymorphism of dopamine D3 receptor gene and schizophrenia
- Genotypic association between dopamine transporter gene polymorphisms and schizophrenia
- Linkage study of the dopamine D5 receptor gene and Gilles de la Tourette syndrome
- Rapid molecular haplotyping of the first exon of the human dopamine D4 receptor gene by heteroduplex analysis
- Dopamine D2 receptor gene and alcoholism among four aboriginal groups and Han in Taiwan
- No evidence of association between dopamine D3 receptor gene and bipolar affective disorder
- D2 dopamine receptor polymorphism and brain regional glucose metabolism
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