Материал: npe

Toremifen (Fareston)

Raloxifene (Evista)

Clomiphene

In women - anovulatory infertility, dysfunctional uterine bleeding, dysgonadotropic forms of amenorrhea.

In men - androgen deficiency, oligospermia, delayed sexual development in adolescents.

Tamoxifen, toremifene, raloxifene

Postmenopausal women - breast cancer, osteoporosis.

Side effects

1. Ovarian hyperstimulation (lower abdominal pain, flatulence, menorrhagia).

2. Nausea, diarrhea.

3. Flushing of the face.

4. Blurred vision.

5. Disorders of the menstrual cycle.

6. Increase in body weight.

Contraindications

1. Pregnancy.

2. Benign neoplasms.

3. Organic diseases of the central nervous system.

4. Diseases of the liver and kidneys.

5. Ovarian cysts.

6. Bleeding (not related to ovulation).

7. Tendency to thrombosis.

Gestagens

1. Progesterone (progestogel, morning) (inside, i / m, topically)

2. Medroxyprogesterone (Depo-Provera, Provera, Veraplex)

3. (i / m 1 time in 14 days)

4. Oxyprogesterone capronate (hormofort) (i.m. 1 p. In 10-14 days)

5. Pregnin (ethisterone) (by mouth, sublingual)

6. Dydrogesterone (duphaston)

7. Norethisterone (norkolut, primolut-nor)

8. Levonorgestrel (levonova, microlut, mirena, norplant, postinor) (inside, s / c - capsules, intrauterine)

Mechanism of action:Interact with gestagen receptors in target cells (ovaries, mammary glands, hypothalamus, pituitary gland). The most important physiological effect of progesterone is the stimulation of the processes that ensure the onset of pregnancy and its preservation until the onset of labor, the preparation of the uterine endometrium for implantation of a fertilized egg and the creation of the necessary conditions for its development (proliferation of the uterine endometrium, increased activity of the uterine glands). In the mammary glands, after preliminary exposure to estrogen, it activates the development of glandular tissue. They reduce the sensitivity of the uterus to oxytocin and acetylcholine, as a result of which it completely stops spontaneous contractions of the uterus during pregnancy and prevents the development of abortions. They are an antagonist of aldosterone (increases the excretion of Na + and water, delays the excretion of K +).

Indications for use:

1. Amenorrhea.

2. Anovulatory uterine bleeding.

3. Infertility associated with dysfunction of the corpus luteum.

4. Habitual or threatening miscarriage.

5. Algodismenorrhea against the background of hypogenitalism.

6. Endometriosis.

7. For the purpose of contraception.

Side effects:

1. With intramuscular injection:

- thromboembolism, thrombophlebitis;

- galactorrhea;

- cholecystitis, cholestatic hepatitis;

- edema;

- alopecia;

- allergic reactions;

2. When taken orally - sleep disturbances, dizziness, dyspeptic disorders.

Contraindications:

1. Liver dysfunction.

2. Hepatitis.

3. Tendency to thrombosis.

Antigestogenic agents

Mifepristone competitive antagonist of natural progestins.

Apply for early termination of pregnancy (up to 42 days), in rare cases for the treatment of menstrual irregularities.

Side effects: uterine bleeding, discomfort and pain in the lower abdomen, weakness, headache, nausea, vomiting.

Contraindications: pregnancy over 42 days, adrenal insufficiency, impaired hemostasis, anemia.

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

Classification of antimalarial drugs

by chemical affiliation of drugs

Classification of antimalarial drugs

on the spectrum of antimalarial action

By the mechanism of action of group 2: Group 1 includes antimalarial drugs with a strong schizontocidal effect. The mechanism of action of these drugs is not specific. They disrupt the properties of both microbial DNA and human cells. This group includes acriquine, chloroquine, primaquine and quinine.

The drugs of the second group are characterized by schizontocidal action, which occurs rather slowly. Resistance to them develops easily both in experiment and in practice. Their mechanism of action is specific. They competitively displace para-aminobenzoic acid (PABA) from the enzyme systems of the microbial cell, but they cannot perform the function of this metabolite. The drugs either interfere with the conversion of PABA to folic acid, or block dihydrofolic reductase. They have no effect on the cells of the macroorganism. This group includes bigumal, chloridine and their derivatives, as well as sulfonamides.

Indications:

1. For the treatment of malaria in the acute period (malarial fever, malarial coma), hematoschizotropic agents are used

2. For the prevention of distant relapses of the disease (radical cure), patients who have had three or four days of malaria are treated with a histochizotropic agent acting on "dormant" schizonts (hypnozoites) - primaquine, the drug is prescribed according to the scheme.

3. For individual prophylaxis - chloroquine

4. For public prevention (especially three-day malaria) pyrimethamine + sulfadoxine (Fansidar).

5. FROMlaxity of labor; cardiac arrhythmias (in combination with digitalis drugs), whetherfever - derivatives of 4-methanolquinoline.

6. Malaria (tropical, three-day and four-day forms - for treatment and prevention) infectious polyarthritis, ankylosing spondylitis, glomerulonephritis, renal amyloidosis, paroxysmal atrial fibrillation, intestinal and extraintestinal forms of amoebic dysentery - derivatives of 7-chloroquinoline.

Contraindications:

1. Retinal diseases, Psoriasis, Porphyria.

2. Organic heart disease with arrhythmias, diffuse kidney damage, liver dysfunctions, blood diseases, psoriasis, diseases of the retina and cornea of ​​the eye, pregnancy.

3. Diseases of the middle and inner ear, auditory nerve, optic nerve diseases, cardiac decompensation, blood diseases, pregnancy after 4 months.

Side effects:

With long-term use of drugs are possible:

decreased appetite, abdominal pain, erythema, urticaria, headache, dizziness, sometimes tinnitus, sleep disturbances, nausea, vomiting, baldness, hair graying, blurred vision, corneal edema, irreversible changes in the retina (narrowing of the arteries, edema and yellow atrophy spots, scotoma).

Ticket 14

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

2. Local anesthetic substances. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

3. Preparations of fat-soluble vitamins. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

4. Means used in the treatment of protozoal infections (amebiosis, leishmaniasis, giardiasis, trichomonadosis, balantidiasis). Classification. Mechanism 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. Local anesthetic substances. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

Local anesthetics - drugs that reversibly inhibit the excitation of afferent nerve endings, as well as the generation and conduction of nerve impulses along the fibers with the loss of all types of sensitivity.

Mechanism of action: they block voltage-gated sodium channels, prevent both the emergence of an action potential and its conduction.

Classification of local anesthetics

Indications for the use of local anesthetics:

1. Infiltration anesthesia. Apply 0.25-0.5% solutions of procaine, 0.125-0.5% solutions of lidocaine, 0.125-0.25% solutions of bupivacaine. The duration of procaine anesthesia usually does not exceed 20-30 minutes, lidocaine - up to 1 hour, bupivacaine - more than 2 hours.

2. Conductive anesthesia. Use 1-2% solutions of procaine, lidocaine, articaine and 0.25-0.5% solutions of bupivacaine and ropivacaine. When repositioning dislocations, reposition of bone fragments, blockade of the trigeminal nerve, brachial, sacral plexuses.

3. Spinal anesthesia (subdural). It is more often produced with a 2-5% solution of lidocaine, sometimes with a 0.25-0.5% solution of bupivacaine or ropivacaine. In the absence of these drugs, procaine (5% solution) can be used. When carrying out lower-thoracic, urological operations.

4. Terminal anesthesia of the mucous membranes is achieved by using solutions of tetracaine (rarely), lidocaine or trimecaine (with the addition of epinephrine, preferably just before anesthesia).

5. Epidural anesthesia for abdominal operations, in obstetric and gynecological practice, in the postoperative period.

6. Lidocaine, trimecaine with ventricular extrasystole and tachycardia, especially with MI, prevention of ventricular fibrillation.

Comparative evaluation: by duration: long-term - anesthesin, pyromecaine, lidocaine, bupivacaine;

short-acting - cocaine, novocaine, dicaine; toxicity: the most toxic dicain, less toxic - novocaine, mepivacaine, pyromecaine.

Contraindications: hypersensitivity to drugs, decompensated heart failure, severe organic lesions of the central nervous system, septicemia.

Side effects:

1. drowsiness, lethargy, dizziness, impaired consciousness, thermor, convulsions;

2. tachycardia, bradycardia, decreased A, arrhythmias, collapse;

3. blurred vision, diplopia;

4. allergic reactions;

5. respiratory depression.

3. Preparations of fat-soluble vitamins. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

Retinol, Betacarotene (Vitamin A)- found in fish oil, liver, cow oil. Enzymatic cleavage of one beta-carotene molecule leads to the formation of 2 molecules of Vitamin A. Mechanism: plays an important role in redox processes, participates in the synthesis of mucopolysaccharides, proteins, lipids. It is absorbed in the small intestine, enters the liver through the lymphatic pathways, retinol released into the blood in the plasma binds to proteins.