• Code CAS
Most popular brand: Reminyl
Active ingredient: Galantamine
Available dosage forms: 4, 8 mg
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Galantamine general information
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Nobody should drop hope since it is possible to cure short-term memory loss. Here’s a listing of supplements which may aid in improving short-term memory loss. Following are a few of the tips which can help you reduce the results of tiredness. Thus, it is necessary to speak with a physician for the right dosage and length of memory loss medication. Other medications may be necessary to treat stroke, significant blood pressure, elevated cholesterol, or alternative heart issues. You ought to seek advice from your physician for memory issues.
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Galantamine (Galantamine): instruction, and the use of a formula
Feature substance galantamine
hydrobromide alkaloid isolated from tubers snowdrop Voronov (Galanthus Woronowii A. Los.) . family Amaryllidaceae (Amaryllidaceae) . Contained also in other types of snowdrop kind of Galanthus . The white crystalline powder bitter taste. It is soluble in water, practically insoluble in ethanol.
Mode of action -. Anticholinesterase
reversibly inhibits acetylcholinesterase, enhances and prolongs the effect of endogenous acetylcholine. Facilitates cholinergic pulses, including neuro – muscle, synapse, strengthens the processes of excitation in the reflex zones of the brain and spinal cord. Increases tone smooth and skeletal muscles, stimulates the secretion of digestive glands and sweat. Causes miosis and spasm of accommodation, lowers intraocular pressure with angle-closure glaucoma. When introduced into the conjunctival sac can cause temporary swelling of the conjunctiva. It penetrates through the BBB. increases the excitation processes in the CNS. When used in the treatment of spastic forms of cerebral palsy improves neuro – muscle conductivity increases contractility of the muscles, has a positive effect on mnemonic function. The increased activity of the cholinergic system may improve cognitive function in patients with dementia of the Alzheimer type.
After a single oral dose of 8 mg is rapidly absorbed from the gastrointestinal tract. bioavailability ; about 90%. Ingestion delays absorption (C max is reduced by 25%), but does not affect the completeness of absorption (AUC). T max is achieved through 1.2 hours pharmacokinetics of galantamine are linear in the dose range of 4 –. 16 mg 2 times a day. Binding to plasma proteins ; 18%. The whole blood is advantageously galanthamine shaped elements (52.7%). the concentration ratio of galantamine blood / plasma ; 1.2. The plasma clearance ; about 300 ml / min, volume of distribution ; 175 l. The main routes of metabolism are N – oxidation, N – and O – demethylation, glucuronidation and epimerization. People with active metabolism of CYP2D6 substrates, the most important route of metabolism is O – demethylation. The principal isoenzymes of cytochrome P450 involved in the metabolism of galantamine are CYP2D6 and CYP3A4. In human plasma with fast and slow metabolism constitute the bulk of unmodified galantamine and its glucuronide. In the plasma of people with a fast metabolism is also found glucuronide About – dezmetilgalantamina. Elimination is biphasic, the final T 1/2 ; 7 –. 8 h Renal clearance ; 65 ml / min (20 – 25% of the plasma clearance). Return with urine (90 – 97% of them 18 – 22% in unmodified form for 24) and faeces (2,2 – 6,3%). After a single dose of galantamine in the plasma and slow metabolizers fast none of the active metabolites (norgalantamin, O – demethylgalanthamine and O – demetilnorgalantamin) in unconjugated form is not detected. Norgalantamin detected in plasma after multiple patients receiving galanthamine (not more than 10% of the concentration of galantamine). Patients with Alzheimer galantamine plasma concentration at 30 – 40% higher than in healthy young men. In moderate hepatic insufficiency (7 – 9 points on the scale of Child – Pugh) AUC and T 1/2 is increased by 30%. In patients with moderate renal insufficiency (creatinine clearance 52 – 104 mL / min), plasma concentrations of galantamine increased 38% in severe (creatinine clearance ; 9 – 51 mL / min) ; by 67%.
Application of the substance galantamine
The capsules of prolonged action: dementia of the Alzheimer type mild or moderate in severity, including chronic disorders of cerebral circulation.
Tablets: dementia of the Alzheimer type mild or moderate in severity; polio (immediately after the cessation of the febrile period, and the recovery period and the period of residual effects); myastenia gravis, , progressive muscular dystrophy, myopathy; cerebral palsy; neuritis; sciatica.
Injection: in Neurology ; traumatic injuries of the nervous system, cerebral palsy, spinal cord (myelitis, polio, polio form of tick-borne encephalitis), mononevrit, polyneuritis, polyneuropathy, polyradiculitis, Guillain – Barre syndrome, idiopathic facial nerve palsy, myopathy, bedwetting. In anesthesiology and surgery: as an antagonist of non-depolarizing muscle relaxants and in the treatment of post-operative intestinal atony and urinary bladder. In the physiotherapy: in the form of iontophoresis for diseases of the peripheral nervous system. In toxicology: intoxication anticholinergic drugs. morphine and its analogs. In radiology: to improve the diagnosis of the digestive system, including gallbladder.
Hypersensitivity, epilepsy, hyperkinesis, asthma, angina pectoris, bradycardia, congestive heart failure, AV block, hypertension, chronic obstructive pulmonary disease, mechanical intestinal obstruction, obstructive pulmonary disease or recent myocardial surgery on the digestive tract. obstructive disease or recent myocardial surgery on the urinary tract or prostate, renal insufficiency (creatinine clearance less than 9 ml / min), severe hepatic dysfunction (more than 9 points on the scale of Child – Pugh), children up to 1 year (for a solution) up to 9 years (for tablets).
Restrictions on the use
General anesthesia, sick sinus syndrome, concomitant use of drugs. slowing of heart rate (digoxin, beta – blockers), light to moderate hepatic dysfunction and / or kidney problems; for oral forms (optional): gastric ulcer and duodenal ulcer; tablet (optional): gluten enteropathy (due to the presence of the drug wheat starch), lactose deficiency, galactosemia, malabsorption syndrome, glucose – galactose (the drug includes lactose).
Application of pregnancy and breastfeeding
When pregnancy is possible if the potential benefit to the mother outweighs the potential risk to the fetus.
Category effects on the fetus by FDA ; B.
Women treated with galantamine should refrain from breast-feeding (it is not known whether galantamine is excreted in breast milk).
Side effects of substance galantamine
From the cardio – vascular system and blood (blood, hemostasis): decrease or increase in blood pressure. Orthostatic hypotension, heart failure, edema, AV block, atrial flutter or atrial fibrillation, prolongation of the interval QT. ventricular and supraventricular tachycardia, supraventricular arrhythmias, flushing, bradycardia, myocardial ischemia or infarction, thrombocytopenia, purpura, anemia.
From the digestive tract: nausea, vomiting, abdominal pain, diarrhea, bloating, indigestion, gastro – intestinal discomfort, anorexia, gastritis, dysphagia, dry mouth, excessive salivation, diverticulitis, gastroenteritis , duodenitis, hepatitis, perforation of the esophageal mucosa, bleeding from the upper and lower gastrointestinal tract. increase in liver transaminases.
From the musculo – skeletal system: muscle cramps, muscle weakness.
With the genitourinary system: incontinence, hematuria, urinary frequency, urinary tract infection, urinary retention, kalkulez, renal colic.
From the nervous system and sensory organs: tremor, syncope, lethargy, dysgeusia, visual and auditory hallucinations, behavioral reactions, including agitation / aggression; transient ischemic attack or stroke; fatigue, headache, dizziness, somnolence, insomnia, convulsions, muscle cramps, paresthesias, ataxia, hypo – or hyperkinesis, depression (very rare ; to suicide), apathy, paranoid reactions, delirium, apraxia, aphasia, impaired vision ( spasm of accommodation), tinnitus (rarely).
Other: chest pain, excessive sweating, fever, weight loss, nosebleeds, rhinitis, dehydration (in rare cases ; with the development of renal failure), bronchospasm, increased libido, hypokalemia, increase the level of sugar or alkaline phosphatase in the blood.
It is an antagonist of morphine and its structural analogs against inhibitory action on the respiratory center. Restores nerve – muscle conductivity blocked kurarepodobnymi means antidepolyarizuyuschego action (tubocurarine, etc.). It enhances the effect of depolarizing muscle relaxant (Ditilin). Holinoliticaskie means (. Atropine, etc.) eliminate the peripheral effects of galantamine muskarinopodobnye, Curariform substances and ganglioplegic ; nikotinopodobnye.
The aminoglycosides may reduce the therapeutic effect of galantamine. PM. reduce heart rate (digoxin, beta – blockers), ; the risk of worsening bradycardia. Cimetidine may increase the bioavailability of galantamine.
Inhibitors of CYP2D6 and CYP3A4 isoenzymes of cytochrome P450 may increase the AUC of galantamine while their application. Galantamine AUC increased by 30 and 40% when it is applied simultaneously with paroxetine and ketoconazole, respectively. With the simultaneous use of erythromycin galantamine AUC increased by 10%. Inhibitors of CYP2D6 isoenzyme (amitriptyline, fluoxetine, fluvoxamine, paroxetine, quinidine) reduce the clearance of galantamine 25 – 33%. Galantamine enhances the inhibitory effect of ethanol on the CNS and sedatives.
Symptoms: muscle weakness or fasciculations, severe nausea, vomiting, crampy abdominal pain, increased salivation, lacrimation, incontinence, severe sweating, decreased blood pressure. bradycardia, collapse and convulsions. Severe muscle weakness in conjunction with tracheal mucosa hypersecretion and bronchospasm, may lead to lethal blockade of the respiratory tract.
Post-marketing experience (Random receiving 32 mg): the development of torsades ventricular tachycardia, prolongation of the QT interval. ventricular tachycardia with transient loss of consciousness.
Treatment: gastric lavage (if swallowed), symptomatic therapy, administration of anticholinergics ; Atropine (0,5 – 1,0 mg / w); the frequency and size of subsequent doses depend on the dynamics of clinical status.
Dosing and Administration
P / to the in / m. w / w. transdermally (by iontophoresis), inside . Dose picked individually, taking into account the patient’s age, the nature of the disease, the efficacy and tolerability of the drug. At the beginning of treatment prescribed minimum effective dose and gradually increase it.
Inside, the daily dose for adults is 10 – 40 mg of 2 – 4 admission. When myastenia gravis daily dose divided into 3 admission. In the treatment of Alzheimer’s type dementia, the recommended starting dose is 8 mg / day ; 4 mg 2 times a day, after 4 weeks of moving to a maintenance dose of ; 16 mg (8 mg 2 times a day), which take at least 4 weeks. The issue of increasing the maintenance dose up to the maximum (24 mg / day) should be decided after an assessment of the clinical situation (achieved effect and tolerability). In the transition from the preparation in the form of tablets taken two times per day for a dosage form as capsules prolonged action taken one time a day, the total daily dose is to remain unchanged.
N / a, Adults: 2,5 – 10 mg of 1 – 2 times a day, the maximum single and daily dose of 10 mg and 20 mg, respectively. P / to the children: 1 – 2 times a day, aged 1 – 2 years ; by 0,25 – 1,0 mg / day. 3 – 5 years ; 0,5 – 5,0 mg / day. 6 – 8 years ; 0,75 – 7,5 mg / day. 9 – 11 years ; 1,0 – 10,0 mg / day. 12 – 15 ; 1,25 – 12,5 mg / day. 15 – 16 ; 12,5 – 20,0 mg / day. Greater dose is divided into 2 daily administration. The duration of treatment depends on the characteristics and severity of the disease, most of ; 40 – 60 days, the treatment can be carried out 2 – 3 times with intermediate periods in 1 – 2 months.
In / in. as an antagonist muscle relaxants antidepolyarizuyuschih: adult ; 10 – 20 mg / day. children from 1 year ; 1 – 2 mg, 3 – 5 years ; 1,5 – 3 mg, 6 – 8 years ; 2 – 5 mg, 9 – 11 years ; 3 – 8 mg, 12 – 15 ; 5 & ndash; 10 mg.
V / m. When X-ray is used in adults at a dose of 1 – 5 mg. In diseases of the peripheral nervous system and for the treatment of nocturnal enuresis in children is applied in the form of iontophoretic dose of 1 – 2 ml 0.25% solution.
Precautions substance galantamine
Serious skin reactions
In patients receiving galantamine in the form of tablets or capsules, sustained-release, have been reported serious skin reaction (Stevens – Johnson and acute generalized exanthematous pustulosis).
It is necessary to inform patients and caregivers for them that the use of galantamine should be discontinued at the first appearance of skin rash, except in cases where it is obvious that the rash is not associated with the use of this drug. If you notice any serious skin reactions should not reopen the application of galantamine and consider alternative therapies.
In case of violation of physical activity is recommended to combine treatment with physiotherapy treatments (massage, physiotherapy), which should begin in 1 – 2 hours after administration of galantamine.
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