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Piracetam, cinnarizine

Synthesis AKOMP
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2019-09-19
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Clinical Pharmacology

Combitropil is a combination drug with a pronounced antihypoxic, nootropic and vasodilating effect.
Both components mutually potentiate their own anti-hypoxic effect and have a vasodilator effect. The combined drug also contributes to a significant increase in blood flow in the brain. The toxicity of the combination does not exceed the toxicity of the individual components of the drug.

Piracetam is a nootropic agent. It has a positive effect on the metabolic processes of the brain: it increases ATP concentration in brain tissue, enhances the synthesis of RNA and phospholipids, stimulates glycolytic processes, and enhances glucose utilization.
It improves the integrative activity of the brain, contributes to the consolidation of memory, facilitates the learning process.
Changes the speed of propagation of excitation in the brain, improves microcirculation, without exerting a vasodilator action, suppresses the aggregation of activated platelets. It has a protective effect in brain damage caused by hypoxia, intoxication, electroshock; enhances alpha and beta activity, reduces delta activity on EEG, reduces the severity of vestibular nystagmus.
It improves interneuronal transmission and synaptic conduction in neocortical structures, improves mental performance, and improves cerebral blood flow. The effect develops gradually.

Practically does not have a sedative and psychostimulating effect.
Cinnarizine is a selective blocker of slow calcium channels, reduces the entry of Ca2 + into cells and reduces its content in the plasmootremus depot, reduces the tone of arteriole smooth muscle, reduces their response to biogenic vasoconstrictor substances (epinephrine, norepinephrine, dopamine, angiotensin, vasopressin, synephrine, norepinephrine, dopamine, angiotensin, vasopressin, epinephrine, norepinephrine, dopamine, angiotensin, and vasopressin).
It has a vasodilating effect (especially in relation to the vessels of the brain, enhancing the antihypoxic effect of piracetam), without having a significant effect on blood pressure. It shows moderate antihistamine activity, reduces the excitability of the vestibular apparatus, lowers the tone of the sympathetic nervous system. In patients with impaired peripheral blood circulation, it improves the blood supply to organs and tissues (including myocardium), increases post-ischemic vasodilation. Increases the elasticity of erythrocyte membranes, their ability to deform, reduces blood viscosity.

Pharmacokinetics
The combined drug is rapidly and completely absorbed in the gastrointestinal tract. Bioavailability of piracetam - 95%. The therapeutic effect appears after 1-6 hours. The maximum level of cinnarizine in plasma is noted after 1-4 hours, piracetam - after 2-6 hours. Cinnarizine metabolism proceeds completely in the liver (by dealkylation). 60% of cinnarizine in an unchanged form is excreted in the feces, the rest of the amount in the urine as metabolites in about 5 hours. The maximum level of cinnarizine after 1-4 hours is noted not only in the blood, but also in the liver, kidneys, heart, lungs, spleen and in the brain. Associated with 91% of plasma proteins.

Piracetam penetrates the blood-brain barrier, accumulates in the brain tissue within 1-4 hours after ingestion. From the cerebral spinal fluid is displayed much slower than from other tissues. Practically not metabolized. The half-life is 4.5 hours (7.7 hours from the brain). Excreted by the kidneys - 2/3 unchanged for 30 hours.

Indications

  • violations of cerebral circulation (including during cerebral atherosclerosis, ischemic stroke, during follow-up care after hemorrhagic stroke, after TBI);
  • encephalopathies of various genesis;
  • comatose and subcomatose states after intoxication and brain injuries;
  • diseases of the central nervous system, accompanied by a decrease in intellectual-mnestic functions;
  • labyrinthopathies of various genesis (accompanied by dizziness, tinnitus, nystagmus, nausea and vomiting), Meniere's syndrome;
  • depression;
  • psychoorganic syndrome with a predominance of signs of asthenia and adynamia;
  • asthenia of psychogenic origin;
  • prevention of migraine and kinetoses;
  • impaired memory, mental function and concentration;
  • lag of intellectual development in children.

Composition

1 capsule contains:
active substances: cinnarizine - 25 mg, piracetam - 400 mg.
Excipients: microcrystalline cellulose, lactose (milk sugar), magnesium stearate, talc.
composition of gelatin capsule: titanium dioxide, methyl parahydroxybenzoate, propyl parahydroxybenzoate, acetic acid, gelatin.

Piracetam, cinnarizine is marketed under different brands and generic names, and comes in different dosage forms:

Brand nameManufacturerCountryDosage form
Combitropil Synthesis AKOMP Russia capsules
Omaron Nizhpharm Russia pills
Phezam® Balkanpharma Bulgaria capsules

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Piracetam, cinnarizine

Dosage and Administration

Orally, during or after meals.
Adults: 1-2 pills 3 times a day for 1-3 months, depending on the severity of the disease. Perhaps repeated courses of treatment - 2-3 times a year.
Children over 5 years: 1-2 pills 1-2 times a day. Do not use for more than 3 months.
For the prevention of kinetoses: in adults - 1 tablet, in children older than 5 years - 1/2 tablet 30 minutes before the start of the journey, with repeated use (if necessary) every 6-8 hours.
Patients with impaired renal function: in chronic renal failure (creatinine clearance 20-80 ml / min) - 1 tablet 2 times a day.

Adverse reactions

From the central and peripheral nervous system: motor disinhibition, irritability, drowsiness, depression, asthenia, headache. In isolated cases, dizziness, ataxia, exacerbation of epilepsy, extrapyramidal disorders, tremor, imbalance, reduced ability to concentrate, insomnia, agitation, anxiety, hallucinations, increased sexuality.
Since the cardiovascular system: a decrease or increase in blood pressure.
On the part of the digestive system: diarrhea, dry mouth; in rare cases, nausea, vomiting, diarrhea, abdominal pain, cholestatic jaundice.
On the part of the skin: in rare cases, dermatitis, itching, skin rash.
On the part of metabolism: an increase in body weight.
Allergic reactions: angioedema.
Others: increased sweating; in isolated cases - lupus-like syndrome, lichen planus.

Contraindications

Hypersensitivity to the main and / or auxiliary components of the drug; severe liver failure; severe renal failure (creatinine clearance less than 20 ml / min); hemorrhagic stroke; Parkinsonism (including Parkinson’s disease); psychomotor agitation; Huntington's disease; pregnancy; lactation period; children up to 5 years; lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome (the product contains lactose).
Carefully
Liver and / or kidney diseases, chronic renal failure (creatinine clearance 20-80 ml / min); increased intraocular pressure; porphyria; violation of hemostasis; extensive surgical interventions; heavy bleeding; hyperthyroidism; epilepsy; pronounced atherosclerosis of the cerebral vessels; propensity for neurotic reactions.

Drug interactions

With simultaneous use, it is possible to enhance the sedative effect of agents that inhibit the activity of the central nervous system, as well as ethanol, nootropic and antihypertensive agents.
Vasodilating agents enhance the effect of the drug.
Improves tolerability of antipsychotic drugs and tricyclic antidepressants.
With the simultaneous use of piracetam enhances the central effects of thyroid hormones (possible tremor, anxiety, irritability, sleep disturbances); may enhance the effects of oral anticoagulants.

Pregnancy and Lactation

The drug is contraindicated for use during pregnancy and lactation (breastfeeding).

Special instructions

With prolonged use, it is recommended to monitor liver and kidney function (especially in patients with chronic renal failure).

During treatment, patients with arterial hypotension may have a more significant reduction in blood pressure.

Alcohol intake during treatment is not recommended.

Possible distortion of the results of doping tests and allergic skin tests; 4 days prior to the study, the drug should be withdrawn.

Influence on ability to drive motor transport and control mechanisms

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and psychomotor speed.

Overdosage

Symptoms of overdose, mainly due to m-anticholinergic activity of cinnarizine, include: impairment of consciousness, vomiting, extrapyramidal symptoms, low blood pressure. After oral administration of piracetam at a dose of 75 g, diarrhea with blood and abdominal pain was observed.

Treatment: there is no specific antidote.In case of overdose, it is necessary to wash the stomach and take Activated charcoal, to carry out symptomatic and supportive therapy. The effectiveness of hemodialysis for piracetam is 50-60%.

  • Brand name: Combitropil
  • Active ingredient: Piracetam, cinnarizine
  • Dosage form: capsules
  • Manufacturer: Synthesis AKOMP
  • Country of Origin: Russia

Studies and clinical trials of Piracetam, cinnarizine (Click to expand)

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