Материал: npe

Broad-spectrum anti-herbal remedies

One of the most effective remedies for ascariasis is levamisole (decaris). A single injection of the drug leads to deworming in 90 - 100% of patients, regardless of the degree of their infection. Unlike santonin, the drug acts on ascaris of all age groups. Levamisole is less effective in ankylostomiasis and strongyloidiasis.

The mechanism of the anthelmintic action of levamisole is based on the specific inhibition of the enzyme succinate dehydrogenase, as a result of which the fumarate reduction reaction, which is most important for nematodes, is blocked. It should be borne in mind that levamisole does not affect succinate dehydrogenase in mammals and only inhibits the helminth enzyme.

The main indication for the use of the drug is ascariasis. Treatment with levamisole (unlike treatment with many anthelmintic drugs) does not require preliminary preparation of the patient - a special diet, the use of laxatives, etc. It is used once before bedtime (for adults at a dose of 150 mg). The drug is well tolerated.

In the treatment of cestodoses, the most common remedy is male fern extract, which is highly toxic and requires careful special preparation of the patient. The main active principles of the male fern extract - philicic acid, aspidin and desaspidin - cause paralysis of the neuromuscular apparatus of flatworms.

Treatment is carried out according to a specific scheme, including diet and laxatives. The dose of the extract for adults is up to 8 g. Often there are numerous side effects in the form of nausea, vomiting, abdominal pain, palpitations. Convulsions, collapse, heart failure are possible. These side and toxic effects, as well as certain contraindications, limit the use of male fern preparations.

In modern medical practice, for the treatment of cestodosis, fenasal is mainly used, which is highly effective in theriarynchiasis, diphyllobothriasis and hymenolepiasis. Fenasal paralyzes tapeworms. In addition, it causes the destruction of the integumentary tissues of helminths and reduces their resistance to the action of proteolytic enzymes of the gastrointestinal tract, contributing to the digestion of cestodes (in this regard, phenasal is not recommended for use in teniasis due to the risk of developing cystcercosis).

Treatment with fenasal does not require special preparation of patients. It is usually taken at night after a light dinner at a dose of 3 g (for adults); with hymenolepiasis, a course treatment is carried out.

The drug is well tolerated. The high efficiency of phenasal in cestodosis, the absence of contraindications and pronounced side effects ensures its widespread use in medical practice, not only in adults, but also in children.

Ticket 13

1. Pharmacological work of domestic physiologists and clinicians (IM Sechenov, IP Pavlov, SP Botkin, NI Pirogov)

2. Anticholinesterase drugs. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs. Cholinesterase reactivators. FOS poisoning, assistance measures.

3. Preparations of sex hormones and their antagonists. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

4. Antimalarial drugs. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

1. Pharmacological work of domestic physiologists and clinicians (im Sechenov, ip Pavlov, sp Botkin, ni Pirogov)

Sechenov - pharmacology of neurotropic drugs. In 1866, "Reflexes of the head of the brain."

Pavlov - the founder of psychopharmacology, began his activity in the field of pharmacology in the clinic of S.P. Botkin, where he headed the experimental laboratory for 11 years. There, under the leadership of Pavlov, cardiac glycosides, antipyretics, and a number of ions were studied. For the first time in the history of science, Pavlov and his colleagues studied the effect of substances (bromides, caffeine) on higher nervous activity in healthy animals and in experimentally induced neuroses. Pavlov also studied the effects of various substances - acids, alkalis, ethyl alcohol, bitterness - on digestion.

Botkin - studied cardiotropic drugs. In 1860 he founded a clinical experimental laboratory, where the first Russian studies on clinical pharmacology and a therapy experiment were carried out.

Pirogov - research of drugs for anesthesia. The first operation under anesthesia in 1847 on the battlefield.

2. Anticholinesterase drugs. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs. Cholinesterase reactivators. FOS poisoning, assistance measures.

Anticholinesterase drugs- indirect cholinomimetics. These substances do not act on cholinergic receptors, but block the enzyme acetylcholinesterase, as a result of which acetylcholine is less destroyed, accumulates and stimulates cholinergic receptors.

Mechanism of action:Anticholinesterase agents inhibit acetylcholinesterase, an enzyme that hydrolyzes acetylcholine in the synaptic cleft and blood plasma cholinesterase (butyrylcholinesterase, pseudocholinesterase, pseudocholinesterase). Inhibition of acetylcholinesterase in cholinergic synapses leads to an increase in the concentration of acetylcholine in the synaptic cleft, as a result of which the action of acetylcholine is significantly enhanced and lengthened. Thus, all the effects of anticholinesterase drugs are due to endogenous acetylcholine.

Classification: Reversible cholinesterase blockers

Tertiary amines: Physostigmine is an alkaloid of Calabar beans. Galantamine (nivalin) is an alkaloid of Voronov's snowdrops tubers.

Amiridine is a synthetic derivative of quinoline (it blocks potassium channels).

Tacrine is a synthetic derivative of acridine.

Quaternary amines:

Neostigmine is a simplified analogue of physostigmine.

Pyridostigmine bromide (Kalimin) is a proserin derivative with a longer lasting effect.

D ystigmina

bromide (ubretide) symmetric bisammonium compounds, according to

Oksazil

Quinotilin activities are superior to proserin.

Irreversible action: Phosphacol, Armin, FOS (phosphorus-organic compounds).

Indications: Glaucoma (increased IOP) using eye drops or ointments

• Atony of the gastrointestinal tract, biliary, urinary tract,

uterus;

• Myasthenia gravis;

• Paresis, paralysis after suffering strokes, brain trauma, neuroinfections, neurosurgical interventions;

• To eliminate the effects of antidepolarizing muscle relaxants;

• Alzheimer's disease (TACRIN, RIVASTIGMINE);

• In case of poisoning with M-anticholinergics, as physiological antagonists.

Side effects: Involuntary twitching of small muscle groups (face, neck, tongue);

Increased irritability, tremors, insomnia;

• Visual impairment in the distance;

• Decreased AV conduction, bradycardia;

• Bronchospasm, bronchorrhea;

• Increased sweating;

• Hypersalivation;

• Spasm of the stomach, intestines, biliary tract;

• Spasms of the urinary tract;

• Strengthening of intestinal motility, diarrhea;

• Increased tone of the uterus;

Contraindications: • Epilepsy

• insomnia

• Heart rate <60 beats per minute, AV blockade

• Myocardial infarction with impaired conduction

• Bronchial asthma

• Peptic ulcer, hyperacid forms of gastritis

• Spasms of the gastrointestinal tract

• Cholelithiasis

• Urolithiasis disease

• Any acute inflammatory processes in the abdominal cavity

• Pregnancy (may cause miscarriage)

Comparative evaluation of drugs: Preparations from the group of tertiary amines are well absorbed from the gastrointestinal tract and penetrate well through the BBB, providing both peripheral and central effects

• Drugs from the group of quaternary amines are less absorbed from the gastrointestinal tract and poorly penetrate the BBB, providing mainly peripheral effects

• FOS do not have an ammonium structure, penetrate well through the BBB

Cholinesterase reactivators: Dipiroxime and isonitrazine. They interact with the residues of FOS associated with acetylcholinesterase, releasing the enzyme and restoring its physiological activity.

FOS poisoning, first aid:

Life-threatening symptoms:

• Severe bradycardia up to cardiac arrest

• Bronchospasm and bronchorrhea, impaired respiratory function

• Convulsions

Specific assistance measures:

• In case of an overdose of reversible drugs, a physiological antagonist is used - the M-anticholinergic antagonist ATROPIN

• In case of an overdose of irreversible drugs (including FOS), use the M-anticholinergic blocker ATROPIN + chemical antagonists (antidotes) - cholinesterase reactivators (DIPYROXIM, IZONITROSIN). Preference is given to ISONITROSINE, because it penetrates well into the central nervous system.

3. Preparations of sex hormones and their antagonists. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

Preparations of hormones of the male sex glands - androgens

Classification

Mechanism of action: Interacting with androgen receptors, it leads to the activation of the expression of certain genes that determine the effect of androgens on the body:

1. Stimulates the development of accessory gonads (prostate gland, seminal vesicles).

2. Promote the formation of voice, larynx, skeleton, muscles, distribution of facial and body hair according to the male pattern.

3. Together with FSH of the pituitary gland, they activate spermatogenesis.

4. Affects the rate of closure of the epiphyseal growth zones.

5. Enhances protein synthesis in muscles, liver and kidneys (pronounced anabolic effect).

Indications for use:

1. Congenital underdevelopment of the sex glands.

2. Eunuchoidism.

3. Impotence.

4. Osteoporosis.

5. Cancer of the breast and ovaries (in women under 60 years of age).

Contraindications:

1. Cancer of the prostate gland.

2. Tumors of the liver.

3. Pregnancy, breastfeeding period.

Side effects

1. Retention of Na + and water in the body.

2. Dizziness.

3. Nausea.

4. Hypertrophy of the prostate.

5. Cholestatic jaundice.

6. Hypercalcemia.

7. Seborrhea, acne.

8. Acceleration of closure of the epiphyses of long bones and growth retardation (in boys with insufficient sexual development).

9. In women - signs of virilization (hair growth on the face, coarsening of the voice).

10. Intensive therapy with androgens can lead to suppression of the gonadotropic function of the pituitary gland, suppression of the functions of the gonads and even their atrophy.

Antiandrogenic agents

Preparations of female sex hormones-estrogens

Anti-estrogen drugs - synthetic compounds of non-steroidal structure, the mechanism of action of which is based on the ability to bind to specific (estrogen) receptors, while in some tissues they act as agonists, and in others - as antagonists.

Clomiphene (clostilbegit, clomid, serophene, serpafar)

Tamoxifen (Nolvadex, Novofen, Tamoxen)