4. Funds with vasoactive action
∙ Ca² antagonists + CINNARIZINE (stugerone, vertizin)
∙ Derivatives of alkaloids DIHYDROERGOCRYPTIN
ergot NITSERGOLIN (sermion)
∙ Derivatives of alkaloids CAVINTON (vinpocetine)
periwinkle VINKAMIN (oxybral)
VINCANOR
5. Combined funds
FESAM (PIRACETS + CINNARIZINE)
Mechanisms of action
1. Improving the bioenergetics of the brain.
Nootropic drugs increase the synthesis of ATP and cAMP, glucose utilization, increase glycolysis and aerobic respiration, and promote an increase in the activity of adenylate cyclase (for aging and neuropsychiatric diseases, energy deficiency and a decrease in the activity of adenylate cyclase in neurons are characteristic).
2. Increased synthesis and release of neurotransmitters.
Nootropic drugs activate the synthesis, release and turnover of dopamine, norepinephrine, acetylcholine, inhibit MAO, increase the formation of β - adrenergic receptors, cholinergic receptors and neuronal uptake of choline. In the mechanism of neurotransmitter release, the blockade of potassium channels is important, which facilitates membrane depolarization.
3. Increase in protein synthesis and membrane phospholipids.
Nootropic drugs improve the regeneration of neurons, activate their genome and increase the synthesis of informational neuropeptides, enhance the metabolism of phosphatidylcholine and phosphatidylethanolamine.
4. Improvement of cerebral blood flow and hemorheological parameters.
Nootropic drugs dilate cerebral vessels, improve blood flow in areas of cerebral ischemia, prevent the development of cerebral edema, block platelet aggregation, thrombus formation, improve the elasticity of erythrocytes and microcirculation. Nicotinic acid in PICAMILON has a direct vasodilating and anti-sclerotic effect.
5. Antioxidant action.
Nootropic drugs, inhibiting free radical peroxidation, protect against destruction of phospholipids of neuronal membranes, which facilitates the fixation of memory traces. Lipid peroxidation increases in the brain during organic diseases, aging and stress.
6. Potentiation of non-tropic effects of memory neuropeptides
PIRACETAM, whose pyrrolidone ring does not open to form a linear GABA molecule, is an agonist of receptors that receive signals from memory neuropeptides (fragments of ACTH, vasopressin, substance P). In terms of chemical structure, PIRACETS is similar to the cyclic form of the terminal amino acid of memory neuropeptides - pyroglutamate and affects receptors as an exogenous ligand. Probably, the most important for the mnemotropic action of PIRACETAM is the activation of AMPA - glutamic acid receptors.
∙ mental retardation, cerebral palsy, mental retardation and / or psychomotor development,
prevention of cerebral disorders in newborns from high-risk groups;
∙ atherosclerosis of cerebral vessels, discirculatory and hypertensive encephalopathy,
cerebral stroke and its consequences;
∙ mnestic disorders in alcoholism, epilepsy, neuroinfections;
∙ post-traumatic acute and chronic brain damage;
∙ asthenia and depression in the elderly, senile depression;
∙ neurotic conditions, severe stress with overwork, impaired mental and social adaptation;
∙ dizziness;
∙ coma of vascular, toxic or traumatic etiology;
∙ correction of tics in patients with Tourette's syndrome and attenuation of attention deficit hyperactivity disorder (GUANFACIN in small doses);
∙ Parkinson's disease, moderate cognitive impairment, including those associated with age-related cognitive dysfunction and dyscirculatory encephalopathy, age-related sensorineural hearing loss, restless legs syndrome (PIRIBEDIL);
∙ prevention of motion sickness in children (FENIBUT, AMINALON);
∙ stuttering, tics, enuresis in children (FENEBUT);
∙ Parkinson's disease (PIRIBEDIL).
Side effects:
∙ allergic reactions;
∙ headache, dizziness, weakness;
∙ dyspeptic disorders;
∙ irritability, anxiety, anxiety, insomnia, anxiety, (except for GUANFACIN, Phenibut, Cinnarizin, FESAM);
∙ PIRIBEDIL: orthostatic hypotension, flatulence, hallucinations (in predisposed persons);
∙ GUANFACIN: dry mouth, drowsiness, impotence, depression; sudden withdrawal of the drug can cause a hypertensive crisis;
∙ AMINALON: feeling of heat, fluctuations in blood pressure;
∙ PHENIBUT: drowsiness;
∙ GINKGO BILOBA LEAVE EXTRACT: stomatitis;
∙ PIRACETS: exacerbation of angina pectoris in the elderly, weight loss, aggressive behavior, fluctuations in blood pressure;
∙ PYRIDITOL: rarely - alopecia, arthralgia, thrombocytopenia, agranulocytosis, muscle weakness, paresthesia, taste disturbance, anorexia, diarrhea;
∙ ACEFEN: increased delirium, hallucinations, anxiety in mental patients, provocation of arrhythmias (ACEFEN is cleaved to form n-chlorophenoxyacetic acid and dimethylamineethanol, which acts as a choline antagonist in the synthesis of acetylcholine);
∙ CEREBROLYSIN: fever, hot flashes, confusion, hallucinations (in patients with dementia);
∙ CINNARIZIN: drowsiness, dry mouth, increased sweating, arterial hypotension, redness of the face and skin of the upper body, edema of the lower extremities; the appearance (aggravation) of extrapyramidal disorders in certain elderly patients;
∙ NICERGOLIN: discomfort in the heart or abdomen, orthostatic hypotension, impaired ejaculation, sweating;
∙ KAVINTON, VINKAMIN: arterial hypotension, tachycardia, extrasystole, thrombophlebitis at the injection site, heartburn, dry mouth, skin flushing.
∙ PANTOGAM: ∙ a syndrome similar to Reye's syndrome (encephalopathy and fatty degeneration of internal organs), due to impaired metabolism of carnitine;
∙ FESAM: dry mouth, weight gain, drowsiness, extrapyramidal disorders.
Contraindications
∙ persistent and significant disorders of mental activity and intelligence;
∙ PIRACETS: acute renal failure, diabetes mellitus (granules), childhood (up to 1 year);
∙ PHENIBUT and PANTOGAM: pregnancy and breastfeeding;
∙ PANTOGAM and PICAMILON: acute and chronic kidney disease;
∙ PYRIDITOL and ACEPHENE: mental agitation, epilepsy, increased convulsive readiness, neuroinfections, myasthenia gravis.
Comparative evaluation:they do not have a pronounced psychostimulating or sedative effect. At the same time, they stimulate the transfer of information between the cerebral hemispheres, improve energy and plastic processes in the brain tissue. All nootropic drugs are characterized by low toxicity and good tolerance by patients of different age groups.
Classification:
- narcotic analgesics
- antiarrhythmic
- vasopressor
-beta1-blockers
- anticoagulants
-antiplatelet agents
- fibrinolytic agents
1) Narcotic analgesics - fentanyl, morphine.
Mechanism of action:
1) Suppression of the conduction of pain impulses in the afferent pathways of the central nervous system.
2) Strengthening the inhibitory effect of the descending antinoceptive system on the conduction of pain impulses in the afferent pathways of the central nervous system.
3) Change in emotional assessment of pain.
Side effects - nausea, vomiting, respiratory depression.
Contraindications –Insufficiency of the respiratory center, children and old age, pregnant and lactating.
2) Antiarrhythmic-lidocaine.
Mechanism of action:They make it difficult for Ca to enter the cell. Reduce the automatism of the sinus-atrial node, inhibit conduction, increase the effective refractory period (in the AV node). Because of this, stimuli of excessively high frequencies do not go to the ventricles of the heart, their activity is normalized.
Side effects: ringing in the ears, blurred vision, diarrhea, lowering blood pressure.
Contraindications: atrioventricular block, liver disease.
3) Vasopressor means-mezaton.
4) Beta1-blockers-metoprolol. It is used to reduce the activity of the heart and with tachycardia.
Mechanism of action:blockade of beta-adrenergic receptors of the heart, blood vessels. They cause bradycardia, reduce the force of heart contractions, reduce the minute volume of the heart, blood pressure gradually decreases, the effect develops in 2-3 weeks.
Contraindications: AV block, heart failure, bradycardia.
Side effects: increase bronchial tone, vomiting, bradycardia, allergies.
5) Anticoagulants - unfractionated heparin.
Side effects: allergies, hemorrhages.
Contraindications: bleeding, decreased clotting rate, leukemia.
6) Antiplatelet agents - acetylsalicylic acid.
Side effects: dyspepsia, thrombocytopenia, allergies.
Contraindications: hypersensitivity, aortic aneurysm, heart failure.
7) Fibrinolytics:
Mechanism:1) act directly on the fibrin clot, promote thrombus lysis. Profibrinolysin penetrates deep into the clot, fibrinolysin acts superficially. 2) promote the conversion of profibrinolysin into fibrinolysin.
Side effects: bleeding, lowering blood pressure, fever, allergies.
Contraindications: bleeding, peptic ulcer, fibrinogenopenia.
four)Antibiotics from the group of macrolides and aminoglycosides. Classification. Mechanism of action. The nature of the action. Spectrum of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.
Macrolides are low-toxic agents for oral administration for infections caused by G + bacteria and intracellular microorganisms.
IV. MACROLIDES
I generation Natural ERYTHROMYCIN OLEANDOMYCIN
II generation Natural SPIRAMYCIN (Rovamycin) JOSAMYCIN MIDECAMYCIN (Macropen) Semi-synthetic ROXITROMYCIN (Rulide) CLARITROMYCIN (Klacid, Fromilide)
III generation Semi-synthetic AZITROMYCIN (sumamed)
Mechanism of AB action - inhibit microbial cell protein synthesis
Macrolides, depending on the type of microorganism and dose, can have a bracteriostatic or bactericidal effect. Spectrum of action: staphylococcus, streptococcus, pneumococcus, meningococcus, gonococcus, corynebacterium diphtheria, clostridium gas gangrene
Macrolides are prescribed orally and some intravenously (erythromycin).
Macrolides:
- have a mucoregulatory effect
- weaken the inflammatory reaction as a result of inhibition of the synthesis of PG, LTE and IL
- about immunomodulatory properties
Indications for use:
- infections of the upper and lower respiratory tract
- whooping cough and its prevention
- diphtheria
- infections of the skin and soft tissues
- other functions of the oral cavity
- trachoma
- sexually transmitted infections
Side-by-side:
- nausea, vomiting
- cramping abdominal pain
- fever
- jaundice
- with i / v - thrombophlebitis,
Hearing impairment
Contraindications:
- hypersensitivity
- pregnancy
- breast-feeding
II. AMINOGLICOSIDES
I generation STREPTOMYCIN NEOMYCIN CANAMYCIN MONOMYCIN
II generation GENTAMYCIN TOBRAMYCIN NETILMYCIN (netromycin)
III generation AMIKACIN
There are 3 generations of aminoglycoside antibiotics (classification):
- I generation - streptomycin, kanamycin, neomycin (used only for local action);
- II generation - gentamicin, tobramycin, amikacin;
- III generation - netilmicin (has less oto- and vestibulotoxicity).
Streptomycin and kanamycin suppress mycobacterium tuberculosis, streptomycin is active against brucella, the causative agents of plague and tularemia. The most sensitive to neomycin are Escherichia coli, Klebsiella, Enterococcus, Proteus and Enterobacter species. Antibiotics of the II - III generation are toxic for E. coli, Klebsiella, Serration, Pseudomonas aeruginosa, Proteus species, Enterobacter and Acinetobacter. All aminoglycosides inhibit 90% of Staphylococcus aureus strains. Resistance to aminoglycosides is characteristic of anaerobic bacteria, hemolytic streptococci, and pneumococci.
The bactericidal effect of aminoglycosides is due to the formation of abnormal proteins and the detergent effect on the lipoprotein cytoplasmic membrane of microorganisms.
Antibiotics of the β-lactam group, inhibiting the synthesis of the cell wall, potentiate the antimicrobial effect of aminoglycosides. Levomycetin, blocking transport systems in the cytoplasmic membrane, weakens their action.
When these antibiotics are taken by mouth, dyspeptic disorders are common. Anaphylactic shock is mainly caused by streptomycin sulfate, which in this respect is in second place after penicillin preparations.
Aminoglycosides can disturb hearing, balance (in 10 - 25% of patients), kidney function, and cause neuromuscular blockade. At the beginning of aminoglycoside therapy, tinnitus appears.
Aminoglycosides are contraindicated in hypersensitivity, botulism, myasthenia gravis, Parkinson's disease, drug parkinsonism, hearing and balance disorders, severe kidney disease. Their use during pregnancy is allowed only for health reasons. During treatment, breastfeeding is stopped.
Indications:Tuberculosis-streptomycin, kanamycin; plague streptomycin; tularemia-streptomycin, gentamicin, brucellosis-streptomycin
purulent-septic diseases - sepsis, peritonitis, meningitis, abscess;
postoperative infectious complications;