1. Increasing the affinity of GABA to GABAA receptors: Benzodiazepines (diazepam, lorazepam, clonazepam); Phenobarbital; Topiramate
2. Contributing to the formation of GABA and preventing its inactivation: Sodium valproate
3. Interfering with GABA inactivation: Vigabatrin
4. Blocking neuronal and glial uptake of GABA: Tiagabin
5. Enhancing the release of GABA into the synaptic cleft: Gabapentin
1 drugs that reduce the release of glutamate from presynaptic endings: Lamotrigine
2.Media blocking glutamate receptors: Topiramate.
Mechanism of action: inhibit interneuronal transmission of excitation (by all mechanisms described in the classification).
Side effects:
1. Sedation, impaired ability to concentrate and slow down the speed of psychomotor reactions; 2. Dyspeptic disorders (nausea, vomiting, epigastric discomfort); 3. Inhibition of hematopoiesis; 4. Hepatotoxicity (diphenin, sodium valproate); 5. Allergic reactions; 6. Neurotoxicity; 7. Teratogenicity (sodium valproate, diphenin, carbamazepine); 8. Carbamazepine (with prolonged use) - bradycardia, arrhythmia, antidiuretic effect with the appearance of edema, in women - the risk of polycystic ovary disease; 9. Sodium valproate - weight gain, polycystic ovary; 10. Diphenin - gingival hyperplasia; 11. Etosuximide - parkinsonism, photophobia.
Contraindications:
1. Hypersensitivity to the drug; 2. Severe violations of the liver and kidneys; 3. Heart failure, bradycardia; 4. Pregnancy (I trimester); 5. Lactation period; 6. Myasthenia gravis; 7. Diseases of the hematopoietic system; 8. Potentially hazardous activities requiring increased attention and speed of psychomotor reactions.
Classification:
2) Beta-blockers:
1, Cardioselective (beta1> 2)
c) with AGR:
-acebutolol, praktolol
d) without AGR:
-metoprol, talinolol, atenolol, bisoprolol, nebivolol
2, Non-cardioselective (beta1 = 2)
d) with the AGR:
-pindolol, oxprenolol
e) without AGR:
f) –anaprilin, timolol, sotalol
2) Alpha, beta-blockers-cordarone, amiodarone, labetolol
Anaprilin - reduces heart rate and strength, stroke and minute volume, myocardial oxygen consumption. Reduces blood pressure. Relieves an attack of angina pectoris.
Side effects - narrowing of the bronchi.
Contraindications - sinus bradycardia, heart failure, bronchial asthma, diabetes mellitus, pregnancy.
Cordaron - weakly blocks alpha-adrenergic receptors, lowers blood pressure, gently blocks beta-adrenergic receptors - reduces the activity of adenylate cyclase and reduces
AMP. Causes bradycardia, decreased contractility, increased coronary blood flow, decreased oxygen demand. Blocks glucagon receptors (antiarrhythmic action).
Side effects - nausea, allergies.
Contraindications - bradycardia, pregnancy, bronchial asthma, old age, hypothyroidism.
Antiseptics are medicinal substances that suppress microorganisms on the surface of the body, on the skin and mucous membranes.
Compounds of metals: mercury dichloride, silver nitrate, zinc oxide, yellow mercury oxide, copper sulfate, zinc sulfate.
Mechanism of action: interacts with proteins, leading to the appearance of salt-like compounds, albuminates, blocks thiol groups in enzymes, disrupting cellular respiration. In high concentrations, depending on the nature of the metal and acid residue, salt concentration, different effects can occur: astringent, irritating, cauterizing.
Indication: mercury dichloride: for the disinfection of mercury oxide yellow for pustular skin diseases, in eye practice
Silver preparations: in dermatology, ophthalmology, urology, for cauterization of warts, ulcers, erosions.
Side effects: poisoning with mercury compounds (mercuric chloride).
Ticket 49
one. Basic principles and methods of testing new medicinal substances. The concepts of "placebo" and "blind" control. The ethical side of prescribing a placebo.
Principles of clinical research of new drugs: • Selection of a homogeneous population of patients; • Exact e-z b-no and a similar severity of the disease; • Control group b-n; • Similar dosage of drugs;
• Pharmacokinetic research; • Choice of sensitivities of the effects typical for the given island; • Quantification of effects; • Sufficient volume of research for stat processing; • Use of "placebo" and "double-blind method" research; • Comparison with reference drugs of this group; • Simultaneous research of new and reference drugs; • Compliance with ethical principles.
A placebo is taken when the element of suggestion plays a role in the effect. Placebo drugs do not contain. In the case of "blind control", the patient alternates between medicine and placebo in a sequence unknown to him, only the attending physician knows when the patient is taking a placebo. In case of "double blind control" the third person knows about it. This principle of research allows you to objectively assess the e-v-v.
2. HISTORY OF DISCOVERY OF ANESTHESIS (MORTON, PIROGOV). THE CONCEPT OF BIOLOGICAL AND MEDICAL ANESTHESIA. CLASSIFICATION OF DRUGS FOR ANESTHESIA. MECHANISM OF ACTION OF INHALATION ANESTHESIC PREPARATIONS. SIDE EFFECTS. CONTRAINDICATIONS. COMPARATIVE EVALUATION OF PREPARATIONS.
1846 - the discovery of anesthesia. Morton (1819-69) was an American dentist who first introduced ether anesthesia into a surgeon's practice. Pirogov (1810-81) - Russian surgeon and anatomist, the main field of military surgery. For the first time he performed an operation under anesthesia on the battlefield (1847).
Classification of drugs for anesthesia.
Gaseous substances: nitrous oxide, cyclopropane, xenon.
Non-navigational : derivatives of barbituric and thiobarbituric acids: thiopental sodium, thiobutal, hexenal
Steroids: Predion.
GHB salts: sodium oxybutyrate.
Others: propofol, propanidide, ketamine.
Anesthesia is a condition characterized by the shutdown of consciousness, suppression of sensitivity, reflex reactions, and decreased tone of skeletal muscles.
The actions of anesthetic drugs are associated with the fact that they inhibit the interneuronal transmission of excitation in the central nervous system. Dysfunction of the membrane. One of the manifestations of the interaction of drugs for anesthesia with the postsynaptic neuronal membrane is a change in the permeability for ion channels (for example, for K ions), which disrupts the process of depolarization, and, consequently, interneuronal impulse transmission.
Receptor component of the action of drugs for anesthesia. All inhalation (volatile) and non-inhalation drugs (except for ketamine) in narcotic concentrations interact with GABA receptors, potentiating their action. Nitrous oxide does not affect gamk. Ketamine is an NMDA receptor antagonist. The same receptors are blocked by xenon. Ftorotane is widely used. It is characterized by high drug activity, a short stage of arousal. anesthesia is easily controlled, after the patient stops inhaling fluorothane, awakening will occur in 3-5 minutes. In terms of fire, it is safe. Has no irritating effect on the mucous membrane of the respiratory tract (unlike ether)
Respiratory side effects of fluorothane: moderately inhibits the respiratory center.
CCC: weakens myocardial contractility, reduces stroke volume, lowers blood pressure. The mechanism of hypotension is associated with inhibition of the vasomotor center and impaired transmission of vasoconstrictor impulses in the ganglia and the endings of sympathetic nerves., Cardiac arrhythmias are possible.
Kidneys: fluorothane reduces renal blood flow, SKF, diuresis, respectively.
Liver: with a healthy liver does not cause significant changes, is contraindicated in persons with liver disease. Ether. It has a pronounced narcotic activity, sufficient arcotic breadth, relatively low toxicity. Less manageable. Irritates mucous membranes, causes a pronounced stage of arousal, explosive. Side effects: profuse secretion of the salivary and bronchial glands (the result of irritation of the mucous membranes), aspiration with vomit, which interferes with airway patency, bradycardia and even cardiac arrest due to reflex excitement of the vagus nerve. Ether is administered only against the background of premixing. Ether promotes the release of catecholamines from the adrenal medulla. This can lead to an increase in glycogenolysis, hyperglycemia (therefore, contraindicated in diabetes mellitus)
On CVS: increased stroke and minute volume of the heart, increased heart rate, moderate narrowing of the peripheral vasculature. Liver: hepatotoxic (but less than fluorothane),
Kidneys: decreased renal blood flow, skf, urine output.
Metabolism: a pronounced change in metabolism due to hyperglycemia, increased lactic acid, pyruvic acidosis.
In the postoperative period, vomiting is noted.
Nitrous oxide. Immediate onset of anesthesia, without arousal stage. This is the effect of low plasma solubility. Because of this, the patient awakens quickly. Penetrates quickly into the central nervous system. Used for pain relief in myocardial infarction, severe trauma, childbirth, etc. the main disadvantage: low drug activity. Therefore, it is necessary to combine with other anesthetic drugs. Should not be used for long-term analgesia. In the postoperative period, nausea and vomiting may occur. Respiration: does not irritate mucous membranes. CVS: not accompanied by changes in heart function. Liver: does not cause Kidney: a transient decrease in urine output is due to constriction of the renal arteries, an increase in the production of ADH. Metabolism: does not cause Blood system: use of nitrous oxide for a long time may cause thrombocytopenia,
Derivatives |
No additional properties |
With additional properties |
phenylalkylamine |
Verapamil, diphril |
Tiapamide, falipamide |
dihydropyridine |
Nifedipine, amlodipine, isradipine, nimodipine, felodipine |
niguldipine |
Benzodiazepine |
diltiazem |
|
Blockers of different chemical structures |
Mibefradil (coronary selective, Does not reduce myocardial contractility, does not inhibit peristalsis) |
bepridil |
Mechanism of action: Class IV drugs selectively block slow Ca channels and Ca2 + current into myocardiocytes. Under physiological conditions, a slow Ca2 + current is involved only in depolarization of the sinus and atrioventricular nodes, but with arrhythmias it also appears in the altered myocardium of the atria and ventricles.
Among Ca antagonists, drugs of the verapamil and diltiazem groups have an antiarrhythmic effect. These drugs reduce the transmembrane resting potential and lengthen the refractory period, as a result conduction slows down and the automatism of the sinus node decreases, the mechanism of recurrent excitation in supraventricular tachyarrhythmias is suppressed.
Indications for use
- prevention and relief of supraventricular tachyarrhythmias.
Side effects
GENERAL +:
- verapamil: edema, constipation, gingival hyperplasia;
- diltiazem: dermatitis, increased liver enzymes, weakness.
Contraindications
GENERAL +:
- arrhythmias caused by glycoside intoxication.
4. Antibiotics of the cephalosporin group. Classification. Mechanism of action. The nature of the action. Spectrum of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.
Classification: a) I generation (with high activity against G + bacteria): cefazolin, cephalothin, cefapirin, cefradine, cephalexin; b) Generation II (highly active against G-bacteria): cefamandol, cefuroxime, cefaclor, cefoxitin, cefmetazole c) generation III (highly active against Pseudomonas aeruginosa): cefotaxime, ceftazidime, cefoperazone, cefixime; d) IV generation (active against bacteroids and other anaerobes): cefpirome
Mechanism: inhibit the synthesis of peptidoglycan of the cell wall, inhibit the synthesis of murein. prevent the formation of peptide bonds due to transpeptidase. Nature: bactericidal action. I - act on gram (+) and some gram (-) and do not act on Pseudomonas aeruginosa, Proteus, bacteroids; II - act on gram (+) and some gram (-), proteus and enterobacteria, do not act on Pseudomonas aeruginosa; III - stronger by gram (-), penetrate the BBB; IV - act on gram (+), Pseudomonas aeruginosa, gram (-)
Spectrum: wide. Penicillinase resistant, but destroyed by beta-lactamase (I).
Indicationsi: urinary, respiratory tract infections; meningitis; prevention of septic complications during surgery; pyelonephritis, cystitis; streptococcal tonsillopharyngitis; exacerbation of chronic bronchitis; community-acquired pneumonia requiring hospitalization; community-acquired infections of the skin and soft tissues of mild to moderate severity; infections against the background of neutropenia and immunodeficiency states; sepsis
Side effects: allergies; kidney damage; diarrhea; bleeding; thrombocytopenia; dysbiosis; pseudomembranous colitis
Contraindications: hypersensitivity; pregnancy; breast-feeding; diseases of the gastrointestinal tract; bleeding
Cefazolin - penetrates the placental barrier, lasts 6-8 hours.
Cefuroxime - resistant to beta-lactamases, penetrates the BBB, lasts 6-8 hours.
Ceftriaxone - resistant to beta-lactamases, penetrates the BBB, acts for 24 hours.
Cefepim - resistant to beta-lactamases, penetrates the BBB, lasts 12 hours