Quinidine

Chemical name

(8R,9S)-6'-Метоксицинхона��-9-ол (in the form of sulfate); D. bark bark tree pravovreatmati isomer Black

Gross

C20-H24-N2-O2

Characteristics

The white crystalline powder. Rat in the water (1%).

Of drugs

The drugs-antiaritmicescoe. Applies to Division IA complications funds. Does fast sodium channels. Oppressing automaticity cells drivers rhythm (more subordinate than cells sinusnogo node), reduces the speed of the pulse, anxiety attacks. Provides direct and indirect (antiholinergicescoe) impact on the heart. The direct effect is to reduce the maximum (Phase 0) and diastolicescoy speed depolarization, increases effective refrakternogo period and the length of the building. Antiholinergicescoe effect has been seen in reduced strength wandering nerve (blockade of pulses per okonchaniah parasimpaticakih fibres cardiomiotitah). Stops окислительно-восстан��вительные in the heart Masze.absorbiruetsa in a thin section bowel. Bioavailability - 70-80%. Therapeutic concentrations in the blood of 3-6 µ g / ml (toxic effects in developing content above 8 µ g / ml). The distribution is reduced in patients with heart failure, increased by cirrhosis of the liver. About 80-90% is associated with plasma proteins (mostly albuminom and alfa_1-kislam glikoproteinom); Bonding with the protein decreases in liver diseases is increasing after trauma, surgery, heart failure, and in the face of myocardial infarction. Biotransformiroetsa in the liver, with the participation of oksidazna system, in part to active metabolites. T_1/2 - 4-10 hrs (usually 6-7 hours), increases in old age. 10-50% excreted memory (in the form of constant and in the form of active metabolites), falling down with alkaline reaction urine. The effect occurs after 1-3 hours, the peak of the intake of registered through 1-2 (hinidina sulfate), or 3-4 hrs (hinidina gluconate), and after one hour, with the / m introduction. Duration of a 6-8 (conventional tablets) or 12 hrs (prolongirovanne forms). Reduces HR, down conductivity of AV node and puckam Guisa - Purkinje increases effective refrakterny period predserdiah and jeludockah heart, getting a Micro and QT interval (электрофизиологичес��ие changes more pronounced in the Ischemia, hypoxia, and tachycardia). In healthy people wagoliticeski indirect effect is manifested in sinusnom (increase HR), and AV (increasing conductivity) nodes. Reduces heart force reductions AD system and the joys (particularly in the on / in the introduction). In higher concentrations can cause 1420 blockade sinusnogo and AV nodes of automaticity.

Indications

Adults (prevention and treatment) : frequent najeludockova and ventricular tachycardia (without complete closure hearts), paroxizmalny предсердно-желудочко��ый (nodal) rhythm mertzatelnaya incredible (frequent and constant shape), predserdy fibrillation, less frequently, and ventricular predserdnaya arrythmia.

Restrictions on the use of

Underemployment предсердно-желудочко��ая blockade congenital syndrome interval elongation QT arrhythmia episodes such as "torsade de pointes" (in history), digitalisnaya intoxication, asthma heart failure, hypotension, myocarditis, bronchial asthma, emphysema lungs, miopatia, prostate adenoma cancer, glaucoma, infectious disease with fever, Ray, psoriasis, pregnancy, breast-feeding (at the time of treatment should stop breastfeeding) the liver and kidneys, children's age (for prolonged forms).

Contraindications

Hypersensitivity full предсердно-желудочко��ая blockade (except for the driver artificial heart), the blockade branches beam Guisa, violations vnutrijeludockova conductivity, abberantne rhythms (from shifting mechanism of the AV node or ventricular), cardiogenny shock trombozitopenica purpura amidst reception hinidina or quinine (in history).

Side-Effects

Aritmogenne effects-bear type torsade de pointes, ventricular tachycardia, ventricular fibrillace, blockades, volchanochnopodobnyy syndrome, gipotenzia, fear, dizziness, a bitter taste in his mouth, diarrhoea, loss of appetite, nausea, vomiting, gastralgia, hepatitis, anemia, thrombocytopenia, allergic reactions (increased body temperature, skin rash, urticaria, itching, redness of skin, shortness of breath or breathing difficulty).

Patient interaction

Increases effect anti proximity, miorelaksantov reduces - antimiasteniceskih funds betanekola, bretilia (ornida). Substances podschelacivate urine (antatsidnye means containing calcium or magnesium, carboangidraza inhibitors, citrata, sodium bicarbonate), and kalisodergaszczye drugs increased toxicity, pimozid, etc. antiaritmiki - proaritmogennouu activity, and fenotiazina rezerpin - cardiodepressiu. Antiholinergicakie funds (atropine, platifillin) weaken wagotonizirute properties; Holinomimeticalkie (acetylcholine, pilocarpine, proserin) increase. Zimetidin reduces overall Cl and lengthens T_1/2 (oppressing mikrosomaiona liver enzymes), stimulants pechenerngo metabolism (phenobarbital, phenytoin, rifampicin) - cut. Ranitidine-produces jeludockove ekstrasistola (including type bigeminii). The risk of poisoning increases hinidine against Black.

Overdosing

Symptoms : oppression heart of predserdy fibrillation with ventricular Tachycardia possible hinidinovy shock (asistolia and heavy rhythm testing), a decline AD, diplopia, dizziness, ringing in the ears, loss Sluha.lechenie : with the recent admission of drug-washing stomach or vomiting induction; Oxygen, hypertensive funds preparations acidifying urine, IVL, elektrocardiostimulyatsia in / with the introduction of liquids Hepatology.

Precautions

Doses individually selected on the basis of clinical response. Before treatment should appoint a test dose (200 mg) inwards for the переносимости.Поскол��ку quinidine has the potential cardiotoksicski action (especially in doses above 2.4 g / day), with a long-term need regular blood tests, EKG monitoring (extension of Micro 25% initial sign of intoxication, more than 50% toxaemia), the liver and kidneys, AD (especially in the on / managed) potassium level hinidina and in the serum (if daily intake into more than 2 g and Injecting application). Older patients with the human liver and kidneys dose should be reduced because of the risk Koumoulyatsii.sleduet be careful when concomitant surgical interventions. Absorption and the declining while ingestion protivodiareynah and antatsidnykh funds (except gel aluminium hydroxide), in patients with heart failure, as in the / m introduction gipokaliemii, hypoxia and violations Khs.sleduet bear in mind that antiholinergicakie properties (in particular giposalivation) can lead (especially in older patients) to the development of caries, Diseases okolozubnykh tissue kandidozu mouth and the emergence of unpleasant sensations in his mouth.

Dosing and Administration

Inside, for one hour before or two hours after meals, with a full glass of water (with the need to reduce irritating to the mucous membrane of blood from milk); Tablets prolonged action should not be nutcracker or tooth. Hinidina sulfate (tablets and capsules), 300 mg four times a day. In paroxizmah najeludockova tachycardia - 400-600 mg, repeated every 2-3 hours before cupping hysteria. In paroxizmah mertzatelna adults-200 mg every 2-3 h (only 5-8 times a day), which supports the dose-300 mg 3-4 times a day. An alternative scheme : 400 mg, and if not attack kupirovan-200 mg every hour prior to the termination of attack or a common one dose and the lack of side effects from the first dose in the next admission may be increased to 600 mg. The maximum dose of four grams Sutki.hinidina sulfate (pills prolonged action) 300-600 mg every 8 to 12 C.hinidina gluconate (slowly released tablets), table 1-2. through 8-12 hours, in order to maintain sinusovogo rhythm after conversion-2 table. every 12 hours, or between 0.5-2 table. eight hours; supporting dose-1 table. a day if necessary every six hours Hinidina gluconate (for the liver) : In / m, the initial dose of 600 mg, the 400 mg every two hours, with the effect of reducing the dose; In / in 800 mg in 40 ml of 5% glucose solution at the rate of 1 ml / min (Required ECG monitoring and AD). Hinidina poligalactouronat 1-3 table. (tentatively designated receiving 100 mg hinidina sulfate) in 3-4 minutes 3-4 times a day. If necessary, in the next day each tretya-chetvertaya single dose increased by 0.5-1 table. to restore sinusovogo rhythm or a toxic effects. Supporting dose-1 table. 2-3 times per Deny.obychnaya dose for children : inward, in terms of conventional tablets : hinidina sulfate-6 mg / kg or 180 mg / m ^ 2 5 times a day, hinidina poligalactouronat - 8.25 mg / kg and 247.5 mg / m ^ 2 5 times a day.

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