3. Stimulants of respiration. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

Breathing is regulated by the respiratory center (DC) located in the medulla oblongata. DC activity depends on the content of carbon dioxide (CO2) in the blood. With an increase in CO2 level, DC is directly activated; in addition, DC is activated by CO2 reflexively due to stimulation of the chemoreceptors of the carotid glomeruli of the carotid sinus zone (SCZ).

Classification of respiratory stimulants according to the mechanism of action 1. Means that directly activate DC: BEMEGRID, CAFFEINE, ETHIMIZOL 2. Means that stimulate reflexive breathing (H-cholinomimetics): CITIZINE (cytiton), LOBELINA HYDROCHLORIDE 3. Means of mixed action type: , CARBON ACID *, CAMPHORA (camphor) Mechanisms of action: Under the influence of respiratory stimulants, the volume of respiratory movements and their frequency increase. BEMEGRID, CAFFEINE, ETHIMIZOL have a direct stimulating effect on DC. ETIMIZOL activates the subcortical formations of the brain and the centers of the medulla oblongata and differs from typical analeptics in that it has a depressing effect on the cerebral cortex, which justifies its use also in psychiatry; has a stimulating effect on the adrenocorticotropic function of the pituitary gland, what is the reason for its anti-inflammatory effect. In CORDIAMINE, CARBON ACID and CAMPHORA, the central effect is complemented by a stimulating effect on the chemoreceptors of the carotid glomerulus. N-cholinomimetics - CITITONE and LOBELINA HYDROCHLORIDE stimulate DC reflexively. The mechanism of their action lies in the fact that they excite the H-cholinergic receptors of the SCZ, from where afferent impulses enter the medulla oblongata, and increase the activity of the DC. These drugs are ineffective for respiratory depression with hypnotics or anesthetics. hypnotics and anesthetic drugs violate the reflex excitability of DC. H-cholinomimetics act for a short time (5 - 10 min.), The nature of breathing is jerky. If we compare the action of LOBELIN and CITITON, then the advantage is given to CITITON, because in the action of LOBELIN, there are 2 phases: Phase 1 - respiratory depression (due to stimulation of n. Vagus); Phase 2 - stimulation of respiration (due to the stimulation of H-cholinergic receptors). When taking CITITONE, there is no inhibition phase and DC stimulation occurs immediately.

Indications for use. ∙ respiratory depression associated with mild intoxication with opioid analgesics, carbon monoxide, hypnotics drugs of a narcotic type of action;

∙ asphyxia of newborns; ∙ in order to restore the required level of pulmonary ventilation in the post-anesthetic period.

Additional effects: ETIMIZOL has found application in psychiatry as a sedative in conditions accompanied by anxiety; it is used as an anti-inflammatory and anti-allergic agent for arthritis, polyarthritis and some forms of asthma. CORDIAMINE and CAMFORA are used for cardiovascular insufficiency, collapse. CITITONE, LOBELIN and CARBON ACID are also indicated for shock and collapse.

Side effects: ∙ BEMEGRID: nausea, vomiting, muscle twitching, convulsions; ∙ CAFFEINE: state of agitation, insomnia, arrhythmias, increased blood pressure (BP); ∙ ETHIMIZOL: nausea, dyspeptic symptoms, dizziness, anxiety, sleep disturbance, tremors; ∙ CORDIAMINE: convulsions, allergic reactions, pain at the injection site; ∙ CARBON ACID: in high concentrations causes severe acidosis, convulsions and DC paralysis; ∙ CAMPHORA: in rare cases, after the administration of the drug, the formation of an infiltrate (oleoma) is noted, sometimes allergic reactions are possible; ∙ CITITON and LOBELIN: nausea, vomiting, bradycardia, convulsions. Contraindications: ∙ increased mental excitability, epilepsy, convulsive syndrome and / or hyperkinesis in history; ∙ arterial hypertension (AH), essential hypertension (HD), organic diseases of the cardiovascular system (CVS) (including atherosclerosis); ∙ pulmonary edema, bleeding from large vessels (for H-cholinomimetics); ∙ analeptics are contraindicated in case of poisoning with substances that depress the central nervous system, since drugs of this group do not restore breathing and at the same time increase the need for brain tissue for O2.

4. Antibiotics of the group of carbapenems and monobactams. Classification. Mechanism of action. The nature of the action. Spectrum of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

Classification: belong to beta-lactam antibiotics:

1. Carbapenems - imipenem, meropenem, ethapenem.

2. Monobactams - aztreones.

Mechanism: inhibit the synthesis of the cell wall.

Mode of action: bactericidal.

Spectrum of action: Carbapenems - G + and G-, anaerobes. Monobactams: G-

Indications:

CARBAPENEM MONOBACTAMS

hospital pneumonia with exacerbation of chronic bronchitis, community-acquired and hospital pneumonia; pulmonary sepsis with cystic fibrosis, intra-abdominal and gynecological infections; complicated urinary tract infections; urinary tract infections; community-acquired and hospital intra-abdominal infections; infections of the skin, soft tissues, bones and joints; gynecological and obstetric sepsis infections; infections of the skin, soft tissues, bones and joints; diabetic foot; neutropenic fever; endocarditis, sepsis; meningitis and brain abscess; prevention of infectious complications of anesthesia and perioperative infections

Side effects:

o nausea, vomiting, diarrhea, allergic reactions, tremors, convulsions (carbapenems)

o abdominal pain, nausea, vomiting, diarrhea, phlebitis, pain and swelling at the site of intramuscular injection, rare allergic reactions (monobactams)

Contraindications:

o hypersensitivity to β-lactam antibiotics, pregnancy, infants under 3 months of age, breastfeeding (carbapenems)

o hypersensitivity, pregnancy, infants, breastfeeding, with renal failure and cirrhosis, reduce the dose of antibiotic (monobactams)

Imipenem, thienam - resistant to beta-lactamases, is destroyed in the renal tubules.

Meropenem is resistant to beta-lactamases, does not break down in the renal tubules, lasts 8 hours. Aztreonam - resistant to beta-lactamases, does not work on gram (+), in case of urinary tract infections.