Nimodipine

Chemical name

1-metilatilovy broadcast 2-метоксиэтил-1,4-дигид��о-2,6-диметил-4-(3-нитроф енил)-3,5-пиридиндикарб оновой acid

Gross

C21-H26-N2-O7

Characteristics

Derived 1,4-digidropiridina. Yellow crystalline powder. Nerastvorim almost in the water.

Of drugs

The drugs-neiroproteguoe, sossoudorasshiratee, antiagregatine. Specific contact located on cell membranes receptor regulating the calcium channel L-tipa. Stops slower current calcium ions in the depolarization phase, reduces the content of calcium in the cells; Relaxes smooth muscle resistance vessels (arteries and arteriol), and extends them. Mostly influence on vessels in the brain, cerebral normalizes blood increases the tolerance to neuronal Ischemia. Provides neiroproteguoe action stabilizes the brain cells. In patients with acute violation of cerebral circulation improves perfuziu damaged and ishemizirovannah of the brain. Injecting introduction to the initial phase of stroke with fewer complications and mortality. Decreases the frequency and severity of ailments after subarahnoidalnogo bleeding as a result of congenital intracranial anevrizma. Improves brain from the bloodstream of patients with gipertoniceski krizom weakens age (in parentheses) neurological symptoms including impaired memory, emotional lability, reduction initiatives. Effective in the prevention of (120 mg / day) and the treatment of migraines and migrenepodobna headache vascular genesis. Decreases round and system AD (may be reflecting tachycardia). It dilatatia coronary vessels, which leads to increased blood flow and increased oksigenation attack. It suppresses or sinusno-predserdny предсердно-желудочко��ый node with a slight negative inotrope Effectom.bystro drawn from the blood. C_max achieved through one hour after taking into and through three mines in the in / in the introduction. In connection with the "first walk" through the liver bioavailability is about 13% (in patients with bleeding subarahnoidalnam to 16%). Associated with the plasma protein up to 95%. T_1/2 of 8-9 hrs (increased by kidney disease and expressed liver failure). Biotransformiroetsa in the liver with the formation of active metabolites. Return with faeces in the form of metabolites (more than 99%) and unaltered with urine (less than 1%). Nimodipin and its metabolites found in the milk of rats at concentrations significantly higher than plasma. Results of a study of chronic toxicity showed that the introduction of 180 mg / kg / day in rats for 2 years and up to 6.25 mg / kg / day dogs for one year did not result in a toxic effects. There is mutagenic (in the Ames test, mikroyadernom test and test dominant letaley yielded negative results). With the mice in the 91 weeks carcinogenicity signs have been detected, but it is reducing life expectancy. In experiments on rabbits, rodents teratogenic effects (stop development of the foetus) treated with a dose of 1 and 10 (but not 3) mg / kg / day from 6 to the 18th day of pregnancy. In rats with a 6 to the 15th day of pregnancy, the dose of 100 mg / kg / day showed signs embrio- and fetotoksicnosti of which stops growth and the increase in the frequency rezorbtion embryo / fetus; in the dose of 30 mg / kg / day stopped foetal development and cause miscarriages.

Indications

Ishemicescoe the cerebral circulation (including the gipertonicescom krize), neurological disorders as a result of acute cerebrovascular due subarahnoidalnam bleeding, senillnaya dementia.

Restrictions on the use of

Gipotenzia (light or moderate), cardiac failure, cardiogenny shock, myocardial infarction with stagnant in the lungs, nerezko expressed by the human liver.

Pregnancy and lactation

Contraindicated in pregnancy. At the time of treatment should stop breastfeeding.

Contraindications

Hypersensitivity expressed gipotenzia, cerebral edema, increased intracranial pressure, severe violations of the liver, liver cancer, pregnancy, breast-feeding.

Specific guidance

Tablets should not be zapiwati greipfrutovm juice (modifies metabolism). We do not recommend a solution from the direct hit by the sunlight, the addition of the solution directly into infuzionnuu bottle or mixed with other drugs. The spread daylight or artificial light injection form can be used for 10 hours without protective measures (ie without glass syringes and tubes connecting dark colour). For injecting must use only systems with plastic tubes because product polivinilhloridom absorbed.

Patient interaction

Indometacin, zimetidin, phenobarbital and simpatomimetiki weaken effect. Do activity gipotenziveh drugs. It increases the likelihood of side effects of cardiac glycosides (and other means of gipokaliemia) hinidina, carbamazepina, cyclosporine, theofillina, valproatov, lithium salts, бета-адреноблокаторо��. Against the backdrop of potentially nefrotoksicnah preparations (aminoglikozida, zefalosporin, furosemide), perhaps the cold water. Do not combine with other blokatorami calcium channel (amlodipin, nifedipin, diltiazem, verapamil), metildopa and with the on / in the introduction бета-адреноблокаторо�� (possibly a significant reduction in AD increased inotroponogo negative actions and the development of cardiac decompensation activities. Troop solution (containing 23.7% alcohol by volume) should not be combined with drugs incompatible with alcohol.

Overdosing

Symptoms : significant reduction in AD tachycardia or aetiology, nausea, gastrointestinal Rasstroistva.lechenie : Removal nimodipina washed stomach and reception activated carbon (with overdose of pills); In / in a release or norarenalina, symptomatic therapy.

Precautions

In patients with impaired renal possibly his progression calling for the lifting of therapy. Be wary award in liver diseases, alcoholism, epilepsy and childhood. It should not be used in conjunction with the drivers of vehicles and people skills relate to the high concentration of attention. If any of the liver (slow metabolism), there is a need to reduce the dose in accordance with the manifestation hypotension or cancel product. The steep declines AD or expressed a headache necessitate the therapy. Treatment is not recommended interrupt in anaesthesia, surgical interventions and angiography.

Dosing and Administration

Inside, prandial (not pills razjevarve), a small amount of fluid in / in the drip, интрацистернально.Ос��рая cerebral ischaemia : 30 mg four times daily for 1 month (maximum). Prophylaxis and treatment of neurological ailments of the cerebral vazospazme because subarahnoidalnogo bleeding : in / in a constant infusions, in the initial dose of 1 mg / h (5 mL / h) for 2 h (approximately 15 µ g / kg / h) then (with good endurance, and the lack of hypotension), 2 mg / h (10 ml / h), which represents about 30 µ g / kg / h. Patients weighing less than 70 kg or unstable AD, in the initial dose of 0.5 mg / h (2.5 ml / h). Injection prevention beginning no later than 4 days and continue for 14 days after bleeding. Treatment has evolved neurological disorders should begin as soon as possible and to hold not less than 5 and not more than 14 days. Troop solution introduces continuous / in the central catheter using infuzing pump and metering valve crane at the same time as one of the following solutions : 5% glucose solution, 0.9% solution of sodium chloride, the solution ringer, ringer solution with magneziei, solution dextran 40, or 6% solution поли(0-2-гидроксиэтил)к рахмала in the ratio of 1:4 (solution nimodipina etc. solution respectively). In an accompanying infusions can be used mannitol, blood or human albumin. To adequately developed solution nimodipina imperative that the restoration within 1 day of the amount of fluid was not less than 1000 ml. After infuzionna therapy, in the interior of the dose of 60 mg six times a day at intervals of 6700 for a period of 7 Dnei.pri Early treatment subarahnoidalnogo bleeding may intratisternalnoe a 20 ml divorced solution (1 ml nimodipina for infusions and 19 ml periods). Senillnaya Dementia : inwards to 30 mg three times daily.

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