SODIUM SULFACIL
SULFADIAZINE SILVER
SULFAMETOXAZOLE / TRIMETOPRIM
SULFAMONOMETOXIN / TRIMETOPRIM
SULFAMETROL / TRIMETOPRIM
Mechanism: It is due to the competitive antagonism of sulfonamides with para-aminobenzoic acid (PABA).prevent the incorporation of PABA into dihydrofolic acid. Along with the noted sulfonamides competitively inhibit dihydropteroate synthetase.
Character: bacteriostatic action.
Effects: anti-inflammatory, neutralize toxins, hypoglycemic effect, diuretic effect, enhance antimicrobial effect.
Spectrum: (wide) 1) bacteria (cocci, Escherichia coli, Shigella, Vibrio cholerae, Clostridia, anthrax pathogens, diphtheria),
2) chlamydia,
3) actinomycetes,
4) protozoa (toxoplasmosis, malaria).
Sulfonamides are especially active against the following microorganisms:
- PNEUMOCOCCOV,
- MENINGOKOKKOV,
-GONOKOKKOV,
-HEMOLYTIC STRETOCOCCUS,
- CAUSES OF BACTERIAL DYSENTERIA
Indications: one. colitis, dysentery, enterocolitis
2. Infections of the biliary and urinary tract.
3. pneumonia, abscesses, bronchitis, pharyngitis, tracheitis, laryngitis.
4. Angina, otitis media, purulent meningitis, conjunctivitis, erysipelas
5. Dermatovenereological diseases (pyoderma, syphilis, gonorrhea, mycoses).
6. Treatment of wounds (only free from pus).
Side effects: Allergy, weakness, agranulocytosis. kidney stones, imbalance of B vitamins, nausea, vomiting, diarrhea, visual impairment
Contraindications: allergic diseases, kidney and blood diseases, pregnancy, children and newborns in the first week of life, glucose-6-phosphate dehydrogenase deficiency, nephrosis, nephritis, acute porphyria, thyrotoxicosis, hypersensitivity to sulfonamides.
Combined preparations of sulfonamides with trimethoprim:sulfatone, poteseptil, bactrim, have high antibacterial activity, are well absorbed in the gastrointestinal tract. Duration - 6-8 hours. Side effects - dyspepsia, allergies, inhibition of hematopoiesis.
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, osnovopol-k psychopharmacol-i, researching the impact of various substances on the digestive system. Ermolyeva - during the Second World War she received penicillin. 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.
Antiparkinsonian drugs - drugs used in Parkinson's disease, tremor palsy in old age, and with complications of drug therapy.
Classification:
1. Drugs that activate dopaminergic effects - levodopa, bromocriptine, selegiline.
2. Agents that inhibit the glutamatergic effect - midantanum.
3. Agents that inhibit the cholinergic effect - cyclodol.
Mechanism of action: in parkinsonism, the dopamine content in the basal ganglia is reduced, the interaction of acetylcholine and dopamine is shifted towards the predominance of cholinergic activity. Alignment of the interaction of 2 mediators is achieved by the use of central anticholinergics, or agents that activate the dopaminergic effect, or by the combined use of these drugs.
Indications: parkinsonism, spastic paralysis associated with damage to the extrapyramidal system.
Side effects: dyspepsia, orthostatic hypotension, mental disorders, movement disorders, arrhythmias.
Contraindications: glaucoma, atrial fibrillation, liver and kidney disease, hypertension.
Levodopa, a precursor of dopamine, penetrates the BBB, where it is converted into dopamine. It especially affects hypokinesia, decreases rigidity and tremor. The most effective remedy. Action in a week. There are many side effects, they decrease with dose reduction.
Bromocriptine - a stimulant of dopamine receptors, reduces prolactin and growth hormone, side effects are often manifested.
Midantan - blocks glutamate receptors, has a beneficial effect on the substantia nigra (decreases in calcium in the cells); causes hypokinesia. The action develops in 1-2 days. There are fewer side effects.
Cyclodol - reduces movement disorders (damage to the extrapyramidal system), effectively reduces tremor.
1) ACE inhibitors and diuretics: ACE inhibitors eliminate the undesirable effects of diuretics: hypokalemia.
Combined drugs: CAPOSID = CAPTOPRIL + DICHLOTHIAZIDE; ENZIX = ENALAPRIL + INDAPAMIDE.
2) Beta-ADRENO-BLOCKER and DIURETIC:
Beta-blockers eliminate the increase in plasma renin activity caused by taking a diuretic. In turn, diuretics control the increase in sodium caused by beta-blockers.
Combination drugs: TENSIMET = PINDOLOL + CLOPAMIDE
3) Beta-ADRENO BLOCKER and BLOCKER of calcium CHANNELS of the dihydropyridine series:
Beta-blockers combine well with calcium antagonists of the dihydropyridine series, since the former reduce cardiovascular resistance and reduce cardiac output, while the latter are peripheral vasodilators and increase cardiac output.
Combined drugs: LOGIMAX = METOPROLOL + FELODIPIN
4) ACE inhibitor and calcium channel blocker:
ACE inhibitors and calcium antagonists lower blood pressure through peripheral vasodilation. The antihypertensive effect of calcium antagonists may be limited due to their stimulation on the RAAS and SAS, due to which edema and tachycardia occur, especially when using calcium antagonists of the dihydropyridine series. The combined use of calcium antagonists with ACE inhibitors helps to reduce these effects.
Combined drugs: EQUATOR = LISINOPRIL + AMLODIPINE
5) Angiotensin receptor blocker and diuretic:
Combination drugs: LOZAP PLUS = LOSARTAN + DICHLOTHIAZIDE
6) Angiotensin receptor blocker, calcium channel blocker and diuretic:
Combination drugs: CO-EXFORG = VALZARTAN + AMLODIPINE + DICHLOTHIAZIDE
7) Beta ADRENO BLOCKER + alpha 1- ADRENO BLOCKER.
four. Antiblastoma drugs. Classification. Mechanisms of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.
Classification:
I. Alkylating agents:
a) derivatives of chloroethylamine (mustard gas) - dopane, sarcolysin;
b) derivatives of ethyleneimine - thiophosphamide, benzotef;
c) derivatives of methanesulfonic acid - mielosan.
II. Antimetabolites:
a) folic acid antagonists - methotrexate;
b) purine antagonists - mercaptopurine;
c) pyrimidine antagonists - fluorouracil.
III. Antineoplastic antibiotics - doxorubicin hydrochloride, dactinomycin.
IV. Herbal antineoplastic agents (alkaloids) - vinblastine, vincristine, colhamin.
V. Enzyme preparations with antitumor activity - L-asparaginase.
Vi. Hormonal drugs and their antagonists - phosphestrol, tamoxifen, prednisolone.
Vii. Interferons, interleukins - aldesleukin.
VIII. Preparations of various chemical groups.
a) Platinum preparations - cystplatin or platidiam, polyplatilen, platinum.
b) Urea derivatives - hydroxyurea, lomustine.
c) Triazenes — dacarbazine or DTIK.
Mechanism of action :
Alkylating: impairment of DNA replication due to cross-linking.
Antimetabolites: suppression of the synthesis of purines and NA
Antineoplastic antibiotics: suppression of nc synthesis and function
Plant-based: blocking mitosis at the metaphase stage
Hormonal drugs: suppression of NK synthesis of hormone-sensitive target cells.
Asparaginase enzymes: impaired protein synthesis due to asparagine deficiency
Indications: cisplastin - ovarian cancer, soft tissue sarcoma, breast cancer
Mercaptopurine - acute leukemia
Methotrexate - acute leukemia, breast cancer, uterine chorionepithelioma
Prospidin - laryngeal cancer
Colhamin - skin cancer
Rosevin - chorionepithelioma of the uterus, reticulosarcoma, lymphogranulomatosis
Vincristine - acute leukemia in children
Asparaginase - lymphosarcoma, acute lymphoblastic leukemia, reticulosarcoma
Adriamycin: acute leukemia, reticulosarcoma, lymphogranulomatosis
Glucocorticoids: lymphogranulomatosis, acute leukemia
Side effects: irritation of the gastrointestinal tract, cardio-, hepato-, nephrotoxic, immunosuppressive, mutagenic, teratogenic effects.
Contraindications: oppression of hematopoiesis, acute infections, liver and kidney disease.
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. H-cholinomimetic substances. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Compare the markup of drugs.
- Cititon (ampoules for i / v)
- Lobelin
They work for 5-10 minutes and are available in the form of ampoules for intravenous administration.
Mechanism of action: they have an effect on n-cholinergic receptors in two phases - the stage of excitation is replaced by the stage of oppression. They speed up breathing, constrict blood vessels, increase blood pressure.
Indications: respiratory depression, the threat of stopping it (carbon monoxide poisoning, mechanical asphyxia, drowning), newborn asphyxia, shock, collapse, are part of Lobelin and Tabex tablets, which are used for smoking cessation.
Side effects: nausea, vomiting, weakness, dizziness.
Contraindications: atherosclerosis, high blood pressure, bleeding from large vessels, pulmonary edema.
Lobelin and tsititon are respiratory analeptics of reflex action. In phase I, receptors are excited, the glomeruli of the carotid sinuses are most sensitive - the respiratory center is excited. Excitation of the chromaffin substance of the adrenal glands - an increase in blood pressure (lobelin lowers blood pressure).
Classification:
I - straight lines (heparin, hirudin, sodium citrate);
II - indirect (neodikumarin, syncumar, phenylin).
Mechanism of action: direct - directly affect the coagulation factor in the blood; act quickly. Indirect - they do not affect blood coagulation factors, disrupt the synthesis of coagulation factors in the liver, the effect develops slowly.
Heparin is a mucopolysaccharide. It is synthesized and deposited in mast cells. Action: 1) antithromboplastin, 2) antiprothrombin, 3) antithrombin, 4) reduces platelet aggregation, 5) increases fibrinolysis. Action 1,2,3 - the transformation of prothrombin into thrombin, fibrinogen into fibrin is disrupted. Indications: heart attack, thrombosis, vascular embolism, hemodialysis, blood transfusion, topically for phlebitis. Side effects - allergies, hemorrhages. Cannot be used for bleeding, decreased clotting rate, septic endocarditis, leukemia.
Hirudin - leeches (secrete hirudin); indications: hypertensive crisis, superficial thrombophlebitis.
Na citrate - for blood preservation, mechanism: calcium binding and clotting disorders.