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Ticket 33.

Question 1. Features of the action and dosage of drugs for various routes of administration.

Question 2. Antipsychotics. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs. The concept of neuroleptanalgesia.

Question 3. Class IV antiarrhythmics (calcium channel blockers). Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

Question 4. Antimicrobial agents - quinolone derivatives. Classification. Mechanism of action. The nature of the action. Spectrum of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

1. Features of the action and dosage of medicinal substances for various routes of administration.

The rate of development of the effect, its severity and duration depends on the routes of administration and dose. Sometimes the route of administration determines the nature of the action. Routes of administration: enteral and parenteral.

Enteral: through the mouth, under the tongue, buccal, into the duodenum, rectally. When administered by mouth, sterility is not required. Absorption more often occurs in the small intestine (large absorption surface and intensive blood supply), the process is relatively slow, first the substances enter the liver, then into the blood. If the drug is destroyed by gastric juice or irritates the mucous membrane, it is prescribed in capsules. When administered under the tongue, absorption is fast, bypasses the hepatic barrier, even at a small dose. Into the 12-finger, the intestine is introduced through a tube. Rectally - enters the bloodstream, bypassing the liver; not affected by gastrointestinal enzymes.

Parenteral: subcutaneous, intramuscular, intravenous, intravenous, intrasternal, intraperitoneal, inhalation, subarachnoid, intrapleural, transdermal, intranasal. Most often under the skin, into a muscle, into a vein (the effect is the fastest). In oil, injected i / m to prolong the effect. Irritating substances in / m and s / c are not administered (necrosis). IV is injected slowly, insoluble compounds, oil solutions (embolism), irritating substances (thrombophlebitis), drugs that cause blood coagulation or hemolysis cannot be injected. In / arter introduction is used in the diagnosis of tumors, blood clots. Intrasternal route is taken if IV is impossible (children, old people). In / peritoneally enter during operations. Inhalation aerosols. Into the islands, poorly penetrating through the BBB, are introduced under the membranes of the brain. Dose - number of in-va for 1 reception. Distinguish between single, daily, doses, course dose (antibiotics), loading dose.

2. Antipsychotics. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs. The concept of neuroleptanalgesia.

Antipsychotics - ggroup of drugs with antipsychotic properties, i.e. the ability to eliminate or suppress the productive symptoms of psychosis in the form of disorders of thinking (delirium), perception (auditory, visual, olfactory hallucinations) and motor activity.

Classification:

BUT. Typical antipsychotics (often cause extrapyramidal disorders)

1.Phenothiazine derivatives: AMINAZINE, TRIFTHAZINE, FLUOROPHENAZINE, ETHAPERAZINE

2. Derivatives of butyrophenone: GALOPERIDOL, DROPERIDOL

3. Derivatives of thioxanthene : CHLORPROTIXENE

B. "Atypical" antipsychotics (do not cause or very rarely cause extrapyramidal disorders)

1. Derivatives of dibenzodiazepine: KLOZAPIN, QUETIAPIN

2. Benzamide derivatives: SULPIRIDE

3. Derivatives of benzisoxazole: RISPERIDON

The main mechanism of action of neuroleptics is blockade of dopamine receptors of the mesolimbic system, this action determines their ability to eliminate delusions, hallucinations, psychomotor agitation... In addition, antipsychotics can block serotonin, histamine, and alpha-adrenergic receptors in the central nervous system....

AMINAZINE has a pronounced effect on the central nervous system, as well as on peripheral innervation, executive organs and metabolism.

AMINAZIN is characterized by antipsychotic and sedative effects, the ability to cause extrapyramidal disorders with prolonged use. In large doses, it pulls out a hypnotic effect. Aminazine causes a decrease in motor activity, inhibits the center of heat regulation, hypotremia is observed, has an antiemetic effect, potentiates the action of neutrotropic drugs (anesthesia, opioid analgesics). Reduces blood pressure.

TRIFTHAZINEcharacterized by more selective than chlorpromazine, antipsychotic effect and less pronounced sedative. Differs in weak hypotensive and muscle relaxant action.

Neuroleptanalgesia is a combined method of intravenous general anesthesia, in which the patient is conscious, but does not experience emotions (neurolepsy) and pain (analgesia).

3. Class IV antiarrhythmics (calcium channel blockers). Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

Substances that block slow calcium channels of the cell membrane, i.e. inhibit the depolarization of cells with a slow electrical response: VERAPAMIL, DILTHIAZEM, BEPRIDIL, GALLOPAMIL, TIAPAMIL

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 the 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 is suppressed in supraventricular tachyarrhythmias.

Indications for use: - prevention and relief of supraventricular tachyarrhythmias.

Side effects: - arterial hypotension; - decrease in atrio-ventricular and ventricular conduction, bradycardia, blockade; - proarrhythmic effect (ventricular tachycardia of the "pirouette" type - can turn into atrial fibrillation and cause sudden death); - decrease in myocardial contractility, worsening of the course of CHF, decompensation of heart failure; - allergic reactions (rash, itching, urticaria).

- verapamil: dizziness, headache, nausea, edema, constipation, gingival hyperplasia;

- diltiazem: dizziness, headache, dermatitis, increased liver enzymes, weakness.

Contraindications: - arrhythmias caused by glycosidic intoxication. - arterial hypotension; - bradycardia, AV blockade (especially 2-3 degrees), SSSU; - CH, CHS; - Acute left ventricular failure (pulmonary edema, cardiogenic shock); - individual intolerance to the drug.

4. Antimicrobial agents-derivatives of quinolone. Classification. Mechanism of action. The nature of the action. Spectrum of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

Antimicrobials are medicines used to treat infections caused by bacteria, fungi, viruses.

Classification:

1.Qinolones of the 1st generation (nalidixic acid, oxolinic acid, pipemidic acid)

2.2 Generation (ciprofloxacin, norfloxacin, ofloxacin, pefloxacin, lomefloxacin)

3.3 generation (sparfloxacin, levofloxacin)

4.4 generation (moxifloxacin, gemifloxacin)

The mechanism of action of all quinolones

- blockade of the enzyme DNA gyrase (gyrus - thread) of the microbial cell. This enzyme cross-links two DNA strands and thus participates in the processes of DNA transcription and replication. When DNA gyrase is inhibited, DNA despiralization occurs. This mechanism provides high selectivity and specificity of the quinolones action.

The nature of the action is bactericidal

All quinolones are incompatible with nitrofurans (efficiency drops sharply)

Spectrum of action I generation

non-fluorinated quinolones

narrow - Gr (-) sticks (E. coli, shigella, salmonella, protea, klebsiella)

Do not create a therapeutic concentration in blood and tissues. They are used for urinary tract infections, as they are completely excreted by the kidneys, creating therapeutic concentrations in the urine

Nalidixic acid (nevigramone, blacks)

Used 4 times a day (T1 / 2 1 - 2 hours). The effectiveness is increased by alkalinization of the urine. Microbial resistance develops rapidly

1st generation

non-fluorinated quinolones

• Indications: Acute cystitis, anti-relapse therapy of chronic pyelonephritis (in acute pyelonephritis, it is ineffective, since the drugs accumulate little in the kidney tissues)

Side effects: Gastrointestinal tract - heartburn, epigastric pain, nausea, vomiting, diarrhea (taken after meals)

CNS - an exciting effect, can manifest itself with tremors, insomnia, paresthesias, a decrease in the seizure threshold

Blood - leukopenia, thrombocytopenia, in patients with genetic deficiency of glucose-6-phosphate dehydrogenase - hemolytic anemia

Liver - cholestatic jaundice, hepatitis

• Contraindications: Fluoroquinolone: ​​History of convulsive syndromes

• Deficiency of the enzyme glucose-6-phosphate dehydrogenase

• Pregnancy (possibly inhibition of the development of cartilage tissue in the fetus)

• Lactation

• Children's age (up to 10 - 12 years old due to the possibility of inhibition of the development of cartilage tissue)

Comparative characteristics:

Nifuroxazide (enterofuril) is used for intestinal infections (acute infectious diarrhea, enterocolitis). Practically not absorbed in the digestive tract. Does not disturb the normal intestinal microflora

Furazolidone is currently used only for giardiasis as a reserve drug. NB! In combination with alcohol, it can cause a teturam-like reaction. Inhibits MAO, therefore, in combination with other MAO inhibitors, sympathomimetics, tricyclic antidepressants and tyramine-containing foods, there is a risk of developing a hypertensive crisis

Nifuratel (makmiror) is used for intestinal infections (acute infectious diarrhea, enterocolitis), giardiasis, intestinal amebiasis, trichomonas vulvovaginitis

Furacilin is used as an antiseptic for treating wounds, skin, mucous membranes, for washing serous and articular cavities.

Ticket 34

1) Development of pharmacology in Russia. Pharmacology and its legal significance. Treating the recipe as a legal document.

2) Sleeping pills. Classification of hypnotics by chemical structure. Mechanism of action. Side effects. Contraindications. Comparative evaluation of drugs. Possibilities for the development of addiction.

3) Antihypertensive drugs that affect the renin-angiotensin system. Classification. Mechanism of action. Side effects. Contraindications Comparative evaluation of drugs.

4) Antiviral agents. Classification. Mechanism of action. the nature of the action. Indications for use. Side effects. Contraindications Comparative characteristics of drugs.

1) Development of pharmacology in Russia. Pharmacology and its legal significance. Treating the recipe as a legal document.

It has long been treated by healers, magicians, wanderers. The monks actively collected and systematized the available knowledge. In the 11th century - the herbalist "Izbornik Svyatoslav", in the 16th century - the herbalist "Blagoprokhladny Vertograd" In the 16th century, the 1st pharmacy was opened in Moscow, in the 17th century, the Pharmaceutical Order was established. Pharmaceutical gardens appeared (cultivating medicinal plants). In 1778, the 1st State Pharmacopoeia (list of medicines) was published in Latin, in 1866 - in Russian. At the beginning of the 19th century, scientific pharmacology began to develop. Nelyubin is an exploration of the Caucasian water miner. Zabelin - founded a pharmaceutical laboratory in St. Petersburg. Pelican - studied fur-m d-i curare and strophanth preparations. Iovskiy published a textbook on pharmacology in 1835. Dogel - pharmacol-I CCC. Pirogov - research of drugs for anesthesia. Sechenov - pharmacol-I of neurotropic agents. Botkin studied cardiotropic drugs. Pavlov studied cardiac glycosides, antipyretic,

The State Pharmacopoeia contains a list of drugs produced in the country, indicating the approved nomenclature, chemical structure of the connection, as well as standards, norms and methods, on the basis of which the quality of drugs is controlled, the correct dosage.

Prescription is an important section of pharmacology that studies methods of making and prescribing medicinal forms. The most important doctor's document. Mistakes can cause irreparable damage to the patient. The doctor is legally responsible for the prescribed prescription. Often a recipe is a financial document.

2.Sleeping drugs. Classification by chemical structure. Mechanism of action. Side effects. Contraindications Comparative evaluation. Possibilities for the development of addiction.

Sleeping pills are medicinal substances that cause a person to experience a state close to natural sleep.

It is used for insomnia to facilitate falling asleep and to ensure a normal duration of sleep.

Classification:

I. hypnotics with a non-narcotic type of action:

1. Benzodiazepine receptor agonists:

1) Derivatives of benzodiazepine - short-acting triazolam,

medium duration of action-lorazepam, lorazepam, nitrazepam, long-acting-phenazepam, diazepam.

2) Preparations of different chemical structures: zopiclone, zolpidem, zaleplon.

2. Agonists of melatonin receptors (synthetic analogs of melatonin): ramelteon, melaxen.

3. Blockers of H1 - histamine receptors (ethanolamine derivative): doxylamine, donormil.

II.Sleeping drugs with a narcotic type of action:

1. Heterocyclic compounds (derivatives of barbituric acid): phenobarbital, sodium ethaminal.

2. Compounds of the aliphatic series: chloral hydrate, sodium oxybutyrate, bromized.

The mechanism of action of benzodiazepine derivatives and drugs of different chemical structure: They interact with benzodiazepine receptors, increase their sensitivity to GABA, melatonin receptor agonists are analogous to the hormone melatonin, the main function of which is the regulation of biological rhythms. The drugs stimulate melatonin receptors, histamine receptor blockers block these receptors and cholinergic receptors in the reticular formation and enhance inhibitory processes, aliphatic compounds are converted in the central nervous system into an inhibition mediator - GABA.