2. Counterarkinsonian funds. Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.

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.

3. Rational combination and combined drugs for the treatment of hypertension. Explain the rationality of the application.

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.